About Me

I offer 12 years of experience in Teaching, Research and Publications.Presently working as Assistant Professor at Prince Sattam Bin Abdulaziz University, Saudi Arabia.
  • Scored 99.35 percentile (All India rank 75) in GATE (2005), conducted by Indian Institute of Technology (IIT), Mumbai.
  • Recipient of University Grants Commission (UGC) Scholarship for pursuing M. Pharm course (2005-2007).
  • Got 10th rank in All India Entrance Test for admission in M. Pharm. conducted by MAHE (Manipal Academy of Higher Education) in 2005.

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Year 2020
Hepatoprotective activity of depsidone enriched Cladonia rangiferina extract against alcohol-induced hepatotoxicity targeting cytochrome P450 2E1 induced oxidative damage
Article
Mar 2020
Alcoholic liver disease (ALD) is a broad-spectrum disorder, covering fatty liver, cirrhosis, alcoholic hepatitis and in extreme untreated condition hepatocellular carcinoma (HCC) may also develop. Cladonia rangiferina (CR) is a class of lichen having a broad spectrum of pharmacological activity. It is used like traditional natural sources in ancient times in India, China, Sri Lanka, etc. Folkloric record about CR has reported their use as an antimicrobial, antitumor, antioxidant, anti-inflammatory activities, etc. Hence, the present study was requested to ascertain the effect of the ethanolic extract of Cladonia rangiferina (CRE) on alcohol-induced hepatotoxicity. The animals were evaluated for the estimation of the liver in vivo biochemical antioxidant parameters. The liver tissues were further evaluated histopathologically and western blotting examination for localization of apoptotic gene expression that plays a pivotal role in hepatotoxicity. The results of this study reveal that CRE proves to be helpful in the treatment of alcohol-induced hepatotoxicity and oxidative stress. Results of different markers have shown that among all, CRE has demonstrated the best hepatoprotective activity. These observations say about the importance of the components of the extract. The ameliorative action of CRE in alcoholic liver damage may exist due to antioxidant, anti-inflammatory, and anti-apoptotic activities.
The pyrethroid toxicants are found as remnants of agricultural crops pesticides and as ingredients of commercially available insecticides. The present work demonstrates the toxic effects of the high-contents pyrethroids available in different insecticidal products and studies the protective effects of ascorbic acid and α-tocopherol through histopathological observations of the damages to the affected tissues of liver, lungs, heart, kidneys, and brain. The ascorbic acid showed complete recovery as comparable to the control groups for liver and heart's tissue damages, while α-tocopherol was very effective in significantly ameliorating the damages in kidneys, lungs, and the brain tissues of the experimental animals when compared with the control groups in their respective set of experiments. The high levels of tissue damages recovery by the ascorbic acid and α-tocopherol suggests their prophylactic use for subjects under the exposure of pyrethrins.
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The current study proposed the in vivo antidepressant and anxiolytic activities of the aqueous extract from Solanum melongena fruits (AESM) in mice. The mice were administered with AESM 100 and 200 mg/kg, p.o. for anxiolytic (elevated plus maze test (EPMT) and locomotor action), and antidepressant (forced swimming test (FST) and tail suspension test (TST) activities. The possible mechanism of action of Solanum melongena fruits was also analyzed by measuring the level of serotonin (5HT), monoamine oxidase enzyme (MAO-A) and GABA activity in the blood of experimental animals. When mice were treated for seven days with 100 (*** P < 0.01) and 200 mg / kg, AESM p.o. and 2 mg / kg, diazepam p.o. (*** P < 0.001) showed significant increases in the average time expended and the number of entries into the open arms of the EPMT, as compared to control group in dose dependent fashion. However, when mice were treated with standard Imipramine (10 mg/kg) (***P < 0.001), AESM 100 mg/kg (**P < 0.01) and 200 mg/kg (*P < 0.05) after day 7, there was significant reduction in locomotor activity in both TST and FST in dose dependent fashion. Monoamine oxidase - A level in the entire brain of mice were significantly reduced when pretreated with AESM 100 and 200 mg/kg, p.o. for 7 days as compared to control group in dose dependent fashion. The mechanisms of action of antidepressant effect of Solanum melongena fruits extract act by increasing serotonin and also GABA. Moreover, the extract also decreased the MAO-A enzyme in the experimental animals. These results demonstrated that both of these doses. Of aqueous extract from Solanum melongena fruits possess potential antidepressant activities in dose dependent fashion.
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Year 2019
In this study, some new essential amino acid-benzofuran-acetamide/propanamide/butanamide hybrid derivatives were synthesized. The structures of the synthesized compounds were confirmed on the basis of their elemental and spectral analyses. Their anti-seizure activity was investigated using maximal electroshock seizure (MES) and subcutaneous metrazol (scMET) seizure tests in mice. Neurotoxicity (NT) of the synthesized compounds was also determined by the rotarod test. Derivatives exhibited favorable protection in both MES and scMET tests with high safety levels in NT test. The derivatives have proven significant activity in mice and could be suggested as potential anticonvulsant lead compounds. All leucine-chlorobenzoyl benzofuran-acetamide/propanamide/ butanamide hybrid derivatives (7b, 7b, and 8b) showed significant anticonvulsant activity in MES model. Compound 8b also demonstrated potent anticonvulsant activity against scMET test. The compound 8b showed maximum activity and would be considered as a lead for further optimization as anticonvulsant agent.
Traditional pertinence: Argyreia speciosa Sweet (Linn.), belongs to the family convolvulaceae, a traditional Indian medicinal herb, has been used to treat acute/chronic ulcers, gonorrhea, rheumatoid arthritis and several nervous disorders having a long history. Aim of the study: A broad spectrum approach of this work was to find out the antioxidant activity of Argyreia speciosa seeds, in vitro and in vivo antioxidant assay were performed. Material and methods: Total phenolic content (TPC), reducing power (RP), antioxidant activity (AOA), O 2 · - (superoxide anion), DPPḢ (1,1-diphenyl-2-picrylhydrazyl) and ˙OH (hydroxyl) radicals scavenging activities, GSH (glutathione), CAT (catalase), SOD (superoxide dismutase) and LPO (lipid peroxidase) are the major parameters which were studied for determining in vitro and in vivo antioxidant property of seed extract & their six fractions obtained from A. speciosa. Carbon tetrachloride (CCl4) induced rat model was used to determine in vivo antioxidant assay of extract and its fractions. Results: Butanol fraction (AS-BF) showed strong antioxidant property and protected oxidative DNA damage. AS-BF was found best as compared to all other fraction for determining antioxidant property of seeds with the reduction in lipid peroxide formation and increment in GSH, CAT and SOD. AS-BF showed the presence of phenolic compounds viz. gallic acid, chlorogenic acid, and ellagic acid. Conclusion: From these results, it was proved that A. speciosa seeds prevent tissue damage due to oxidative stress with strong antioxidant activity.
Free radicals are the byproducts of physiological aerobic cellular metabolism. Intrinsic antioxidant system plays its pivotal function in prevention of any loss due to free radicals. Though, incorporation or excess production of free radicals from environment to living system or imbalanced defense mechanism of antioxidant system leads to severe consequences like neuro-degeneration. Sensory or functional loss occurs in neural cells in neurodegenerative diseases. Besides numerous other genetic or environmental factors, oxidative stress is the major cause which leads to damage of neurons and production of neurodegenative diseases. However, oxygen is vital for existence, excessive reactive oxygen species production and imbalanced metabolism leads to a variety of diseases such as aging, Parkinson’s disease, Alzheimer’s disease, and many other neurodegenative diseases. Free radicals toxicity contributes to DNA and proteins damage, tissue damage, inflammation and consequent cellular apoptosis. Neuroprotection is a broad term commonly used to refer therapeutic strategies that can prevent, delay or even reverse neuronal damage. Since thousands of years, lots of medicinal plants have been used in a group of herbal preparations of Ayurveda (Indian traditional health care system) named Rasayana because of the antioxidant principles present in it, responsible for their medicinal use in neurodegenerative diseases. This work constitutes a literature review on natural products contain antioxidant principles used in the treatment of neurodegenerative disease.
Wound healing is a complex process in which injured skin and tissues repaired by interaction of a complex cascade of cellular events that generates resurfacing, reconstitution and restoration of the tensile strength of injured skin. It follows β-catenin, extracellular signal regulated kinase (ERK) and Akt signaling pathways. Aegle marmelos L., generally known as bael is found to act as anti-inflammatory, antioxidant and anti-ulcer agent. Furthermore, studies have demonstrated that this Indian traditional medicinal plant, A. marmelos flower extract (AMF) was used for wound injury. Henceforth, the current study was investigated to ascertain the effect of its active constituents in vitro wound healing with mechanism involve in migration of cells and activation of β-catenin in keratinocytes, inhibition of PGE2 in macrophages and production of collagen in fibroblasts. We have taken full thickness wound of rats and applied AMF for 2 weeks. Cutaneous wound healing activity was performed using HaCaT keratinocytes, Hs68 dermal fibroblasts and RAW264.7 macrophages to determine cell viability, nitric oxide production, collagen expression, cell migration and β-catenin activation. Results shows that AMF treated rats demonstrated reduced wound size and epithelisation was improved, involved in keratinocytes migration by regulation of Akt signaling, beta-catenin and extracellular signal-regulated kinase (ERK) pathways. AMF and its active constituent's increased mRNA expression, inhibited nitric oxide, PGE2 release, mRNA expression of mediators in RAW 264.7 macrophages and enhances the motility of HaCaT keratinocytes in vitro wound healing of rats.
The aim of the current study was to evaluate and compare the toxicities of different types of mosquito repellents i.e. coils, mats and liquid vapors in animal models. Different types of mosquito repellents including liquid vaporizers, coils and mats have been extensively used by the people to get protection from the mosquitoes and diseases associated with them. The active constituents of these repellents include; allethrins, pyrethrins, paraffin and various other derivatives, are well known for their toxicities. Exposure of albino mice to these repellents for 3 h per day over a period of 20 days produced significant toxicological effects on vital body organs including; liver, lungs, kidneys, brain and heart. The order of toxicity of different repellents on nervous and hepatic tissues was found to be: Coil > Liquid > Mat while in renal and cardiac tissues, the coil was again found to be the most toxic one, mat with medium toxicity whereas liquid as least toxic (Coil > Mat > liquid). Lungs tissues are almost equally affected by all the repellants. On the basis of current findings, it has been concluded that exposure to various types of mosquito repellents can be deleterious to health and can cause various health related issues by producing pathological changes in the vital organs.
Year 2018
The aim of this study was to investigate the anticonvulsant and neuroprotective effects of methanolic extract of Cinnamomum camphora leaves (MECC) in albino wistar rats against maximal electroshock seizure (MES) and seizures induced by pentylenetetrazol (PTZ) models. Acetylcholinesterase (AChE) activity and oxidative stress parameters like malondialdehyde (MDA) and reduced glutathione (GSH) were estimated in the brains after completion of the anticonvulsant studies. MECC (50 and 120 mg/kg b.w., p.o.) exhibited anticonvulsant activity as indicated by significant (P < 0.05, P < 0.01) reduction in the duration of hind limb tonic extensor phase in MES induced seizure model and significantly (P < 0.05, P < 0.01) increased the time of onset of clonic convulsion, decreased the duration of seizures, increased the % protection and decreased the percent mortality in a dose dependent manner. MECC (50 and 120 mg/kg b.w., p.o.) exhibited neuroprotective activity as indicated by significant reduction in MDA levels, AChE activity and increased GSH level also in a dose dependent manner. These results indicate that MECC may exert anticonvulsant and neuroprotective effects which may be attributed to the increase in the level of GABA, inhibition of AChE and inflammation and antioxidant activity in the brain.
Background: Histone deacetylase 1 (HDAC1) over expression is responsible for carcinogenesis by promoting epigenetic silence of tumour suppressor genes. Thus, HDAC1 inhibitors has came out as the potential therapeutic leads against multiple human cancers, as they can block the activity of particular HDACs, renovate the expression of several tumour suppressor genes and bring about cell differentiation, cell cycle arrest and apoptosis. Methods: The present research work comprises of atom-based 3D-QSAR, docking, molecular dynamic simulations and DFT (density functional theory) studies on a diverse series of hydroxamic acid derivatives as selective HDAC1 inhibitors. Two pharmacophoric models were generated and validated by calculating the enrichment factors with the help of decoy set. The Four different 3D-QSAR models i.e., PLS (partial least square) model, MLR (multiple linear regression) model, Field based model and GFA (Genetic function approximation) model were developed using 'PHASE' v3.4 (Schrödinger) and Discovery Studio (DS) 4.1 software and validated using different statistical parameters like internal and external validation. Results & discussion: The results showed that the best PLS model has R2=0.991 and Q2=0.787, the best MLR model has R2= 0.993 and Q2= 0.893, the best Field based model has R2= 0.974 and Q2= 0.782 and the best GFA model has R2= 0.868 and Q2= 0.782. Cross-validated coefficient, (rcv2) of 0.967, 0.926, 0.966 and 0.829 was found for PLS model, MLR, Field based and GFA model, respectively indicating the satisfied correlativity and prediction. The docking studies were accomplished to find out the conformations of the molecules and their essential binding interactions with the target protein. The trustworthiness of the docking results was further confirmed by molecular dynamics (MD) simulations studies. Density Functional Theory (DFT) study was performed which promptly optimizes the geometry, stability and reactivity of the molecule during receptor ligand interaction. Thus, present research work provides spatial fingerprints which would be beneficial for the development of potent HDAC1 inhibitors.
Histone deacetylase inhibitors (HDACi) have demonstrated as an emerging class of anticancer drugs involved in regulation of gene expression and chromatin remodeling thus indicating valid targets for different types of cancer therapeutics. The pan-deacetylase inhibitor panobinostat (Farydac®, LBH589) is developed by Novartis Pharmaceuticals and a newly US FDA approved drug for the multiple myeloma. It is under clinical investigation for a range of hematological and solid tumors worldwide in both oral and intravenous formulations. Panobinostat inhibits tumor cell growth by interacting with acetylation of histones and nonhistone proteins as well as various apoptotic, autophagy-mediated targets and various tumorigenesis pathways involved in the development of cancer. The current article summarizes the status of panobinostat in gastrointestinal cancers. Preclinical and clinical data suggest that panobinostat has potential inhibitory activity in hepatocellular, pancreatic, colorectal, gastric and gastrointestinal stromal tumors. Clinical evaluations of panobinostat are currently underway. Herein, we have also reviewed the rationale behind the combination therapy under the trials and possible future prospective for the treatment of GI tumors.
Year 2017
Total extracts of Drechslera rostrata and Eurotium tonophilum in addition of two isolated compounds from their cultures [di-2-ethylhexyl phthalate (H1) and 1,8-Dihydroxy-3-methoxy-6-methyl-anthraquinone (H2)] were tested for their antitumor activity using four human carcinoma cell lines. Antitumor activity was assessed by performing MTT assay to check the % cell viability. The % viability of HCT-116 (colon carcinoma), HeLa (cervical carcinoma), HEp-2 (larynx carcinoma) and HepG-2 (hepatocellular carcinoma) cells decreased after treatment with Drechslera rostrata and Eurotium tonophilum extracts, these effects were ranged from 059.0± 0.1 to 217.0 ± 0.3 μg/ml on all types of cancer cells. The best activity was recorded for Eurotium tonpholium extract (054.5 ± 0.3, 059.0 ± 0.5 and 059.0 ± 0.1 for HEp-2, Hela, and HepG-2 respectively). The isolated compounds (H1&H2) were found to be responsible about the activities because they recorded the lowest IC50 on tested cell lines with range of 9.5-20.3 μg/ml. Vinblastine sulphate was used as a reference standard and showed in vitro anticancer activity. This study demonstrated that all extracts and isolated compounds have antitumor activity against HCT-116, HeLa, HEp-2 and HepG-2 cells.
ABSTRACT: To study the analgesic and antipyretic activities of ethanolic extract of Bambusa arundinacea leaves (EEBA) in rats by using models tail immersion test, hot plate test and brewer’s yeast pyrexia model. Methods: The dried powdered leaves were extracted with ethanol and the resultant extract was subjected for phytochemical investigation to identify different phytoconstituents. Analgesic activity of the ethanolic extract of B. arundinacea leaves at a dose of 100mg/kg b.w., p.o. and 200mg/kg b.w., p.o. were evaluated against the standard drug Diclofenac sodium at a dose of 10mg/kg b.w., i.p. by tail immersion test and hot plate test. Antipyretic activity of EEBA (100 mg/kg and 200 mg/kg) was assessed by using brewer’s yeast pyrexia model in rats against the standard drug Paracetamol (150 mg/kg, p.o.). Results: Preliminary phytochemical investigations showed the presence of flavonoids, alkaloids, steroids, carbohydrates, proteins and amino acids, tannins and phenolic compounds as major secondary metabolites. The results showed that in tail immersion and hot plate test, EEBA has shown significant (P < 0.05) increase in the latency period at both high and low doses indicating analgesic activity. EEBA (100 mg/kg and 200 mg/kg) also significantly (P < 0.0001) reduced brewer’s yeast induced pyrexia in rats. Conclusion: These results demonstrated that the ethanolic extract of Bambusa arundinaceae leaves exhibited significant analgesic and antipyretic activities at 100 mg/kg and 200 mg/kg in dose dependent manner.
Aim: To evaluate the antihypertensive effect of ethanolic extract of seeds of Phaseolus vulgaris Linn. (EEPV) on high salt diet induced hypertension in male rats. Methods: Male wistar rats (180-200g) received high salt diet (8% NaCl) and 1% saline water for 6 weeks, then cannulated for dosing of Enalapril, angiotensin converting enzyme inhibitor (0.5 mg/kg, i.v.) in standard group and EEPV (50 and 100 mg/kg, i.v.) in test group and measured mean blood pressure, systolic blood pressure, diastolic blood pressure and heart rate with the help of Power Lab 6 Pro after 60 minutes of treatment. Results: Elevated blood pressure of the animals was significantly (P < 0.05) decreased by EEPV (100 mg/kg, i.v). Enalapril, at the dose of 0.5 mg/kg, i.v. showed significant (P < 0.05) reduction in the elevated blood pressure. The antihypertensive activity of ethanolic extract of seeds of Phaseolus vulgaris Linn. may be due to the action on rennin-angiotensin system. The antihypertensive activity of EEPV might also be explained by the presence of phytochemical constituents like flavanoids and saponins in the plant. Conclusion: The work demonstrated that the concomitant administration of high-salt and EEPV elicits prevention of high salt-induced hypertension in rats. Overall, results justify and support the use of Phaseolus vulgaris Linn. as antihypertensive medicine.
Infertility refers to the biological inability of an individual to contribute to conception over the course of one year. Male infertility refers to a male’s incapability to cause pregnancy in a fertile female. Approximately 15% of couples are affected by infertility and among them 40–50% cases are attributed to male infertility. Male infertility is mainly categorized into Azoospermia (AS) and Coital infertility (CI). Many studies have supported that different factors such as varicocele, testicular failure, endocrine dysfunction, genital tract infection, testicular disturbances, testicular cancer, hormonal disturbances, retrograde ejaculation, prolonged exposure to heat, obesity, older age, smoking, alcohol, heavy metals, pesticides, oxidative stress, genetic factors and different environmental and nutritional factors reversibly or irreversibly influence male fertility. Male infertility can be diagnosed by different tools. Diagnosing male infertility problems usually involves physical examination, semen analysis, hormone tests, testicular biopsy, urine test etc. There are different pharmacological, non-pharmacological, combination and ethno-pharmacological treatment options for male infertility. The infertility of known etiology has considerable treatment success rate. However, genetic or idiopathic male infertility has optimized and empirical approach. This review summarizes classification, causes, diagnosis and treatment of male infertility. The article is based on English peer-reviewed articles located on Scopus, Pubmed, ScienceDirect etc.
ABSTRACT: Aim: The present study provides a scientific evaluation for the wound healing activity of methanolic extract of Ziziphus xylopyrus (Retz) Willd leaves (MEZX). Methods: Incision and excision wound models were used to evaluate the wound healing activity of MEZX on Wistar rats. In each model, animals were divided into four groups of 6 animals each. In both model, Group I was assigned as control (ointment base). Group II and III were treated with 5%w/w and 10% w/w MEZX topical ointment respectively. Group IV was treated with standard nitrofurazone ointment (0.2% w/w). The parameters recorded were percentage of wound contraction, epithelialisation period and tensile strength. Results: It was noted that the effect produced by MEZX ointment showed significant (P < 0.001) healing in all wound models when compared with the control group. All parameters such as wound contraction, epithelialisation period and tensile strength showed significant (P < 0.001) changes when compared with the control. MEZX stimulates wound contraction, decreases epithelialisation period and increases tensile strength. Conclusion: This study suggests that MEZX possesses wound healing activity against Incision and excision wound.
In chemotherapy for tuberculosis, leprosy, cancer and stress conditions the immune system are impaired and suppressed. In such situations the effect of adaptogenic phytoconstituents are essential for healthy blood to support optimal oxygen carrying capacity which is important for stamina. The aim of this review is to bring together most of the available scientific research related to adaptogens, those are plant-derived biologically active substances. Adaptogens are the substances that appear to induce a state of non-specific increase of resistance of the organism to diverse assaults that threaten internal homeostasis and improve physical endurance. Supplementation with various plant materials which are the source of vitamins, acids, minerals and other phytoconstituents has been evaluated for their adaptogenic activity during exposure to a stressful environment. This review has been compiled using references from major databases such as Chemical Abstracts, Science Direct, Medicinal and Aromatic Plants Abstracts, SciFinder, PubMed, Dr. Duke′s Phytochemical and Ethnobotanical Databases. Nature is a rich source of biological and chemical diversity and a number of plants in the world have been used in traditional medicine remedies. This work constitutes a literature review on medicinal plants with its chemical constituents showing adaptogenic properties. Various medicinal plants with its phytochemical constituentsareshowing adaptogenic properties and it is used during chemotherapy in which the immune system are impaired and suppressed.
Year 2016
Background and Objective: The present study was aimed to investigate the effect of polyherbal formulation Rumalaya Forte on experimentally induced insulin resistant myocardial infarction in rats. Materials and Methods: The effect of polyherbal formulation Rumalaya Forte (160 and 320 mg kg⁻¹ b.wt.,p.o.) was studied on the high fat diet induced insulin resistant myocardial infarction animal model. Vitamin E (100 mg kg⁻¹ b.wt.,p.o.) was used as standard. The study was evaluated with the help of various biochemical parameters and histopathological examination. Results: Results showed that the Rumalaya Forte treatment prevented myocardial infarction,increase in blood glucose level,body weight and weight gain due to antioxidant property and showed a significant dose dependent decrease in the parameters like alanine aminotransferase,aspartate aminotransferase,creatinine phosphokinase,total cholesterol,total triglycerides,weight and number of adipocytes and in infarction size. The histopathological examination also reveals the significant protection in the Rumalaya Forte treated group with a minimal or no red coloration in a dose dependent manner. Rumalaya Forte 160 mg kg⁻¹ b.wt.,p.o. groups showed relatively less disruption of myofibers with Rumalaya Forte 320 mg kg⁻¹ b.wt.,p.o. and vitamin E showing maximum fiber integrity. Rumalaya Forte 320 mg kg⁻¹ b.wt.,p.o. was found to be more effective compared to Rumalaya Forte 160 mg kg⁻¹ b.wt.,p.o. Conclusion: The pleiotropic effect of Rumalaya Forte can be utilized as add on therapy for treatment of myocardial infarction.
Abstract : a native plant of Indo-Malaysia is best known for its fruits, which contain about 75 percent juicy edible pulp. The acidic pulp is a common ingredient in culinary preparations such as condiments, curries, beverages, jams in countries where the plant grows naturally. The fruit is pickled in salt solution which is rich of minerals, acids, phenolic compounds, terpenoids, flavonoids, vitamins, peptides and sugars. Ripe fruit is full of acids and micro and macro nutrients which combine well with sugars, and used to prepare a variety of jam. It is now considered as a valuable source of several unique products for the medicines against various diseases and also for the development of some industrial products. The present review includes comprehensive information on the chemical constituents , traditional uses, pharmacological actions and nutraceutical values of raw material and processed products. Karonda is relatively a new item yet to explore the full potential and a fruit that needs promotion and publicity in the international markets.
A series of N-(2-(benzoyl/4-chlorobenzoyl)-benzofuran3-yl)-2-(substituted)-acetamide derivatives (4a-l, 5a-l) was synthesized in good yield. All synthesized compounds were in agreement with elemental and spectral data. The anticonvulsant activity of all synthesized compounds was assessed against the maximal electroshock induced seizures (MES) model in mice. Neurotoxicity was evaluated using the rotarod method. The majority of compounds exhibited anticonvulsant activity at a dose of 30 mg kg–1 body mass during 0.5–4 h, indicating their ability to prevent seizure spread at low doses. Relative to phenytoin, [N-(2-(4-chlorobenzoyl)benzofuran-3-yl)-2- (cyclohexyl(methyl)amino)-acetamide] (5i) and [N-(2-(4- chlorobenzoyl)benzofuran-3-yl)-2-(4-methylpiperidin-1- yl)-acetamide] (5c) demonstrated comparable relative anticonvulsant potency of 0.74 and 0.72, respectively, whereas [(N-(2-(4-chlorobenzoyl)benzofuran-3-yl)-2-(4- (furan-2-carbonyl)-piperazin-1-yl)-acetamide] (5f) exhibited the lowest relative potency of 0.16. The ALD50 of tested compounds ranged from 1.604 to 1.675 mmol kg–1 body mass. The ED50 of synthesized compounds ranged from 0.055 to 0.259 mmol kg–1 (~23.4 to 127.6 mg kg–1) body mass. The pharmacophore mapping of the examined compounds on standard drugs (phenobarbital, phenytoin, ralitolin and carbamazepine) strongly suggests that these compounds may exert their anticonvulsant activity via the same established mechanism as that of known drugs.
Carissa carandas Linn. (Karonda) a native plant of Indo-Malaysia is best known for its fruits, which contain about 75 percent juicy edible pulp. e acidic pulp is a common ingredient in culinary preparations such as condiments, curries, beverages, jams in countries where the plant grows naturally. e fruit is pickled in salt solution which is rich of minerals, acids, phenolic compounds, terpenoids, avonoids, vitamins, peptides and sugars. Ripe fruit is full of acids and micro and macro nutrients which combine well with sugars, and used to prepare a variety of jam. It is now considered as a valuable source of several unique products for the medicines against various diseases and also for the development of some industrial products. e present review includes comprehensive information on the chemical constit-uents, traditional uses, pharmacological actions and nutraceutical values of raw material and processed products. Karonda is relatively a new item yet to explore the full potential and a fruit that needs promotion and publicity in the international markets.
Please check my researchgate profile to know more about this topic.
Please check my researchgate profile to know more about this topic.
Please check my researchgate profile to know more about this topic.
Please check my researchgate profile to know more about this topic.
Please check my researchgate profile to know more about this topic.
The present study provides a scientific assessment for the wound healing potential of methanolic extract of Calophyllum inophyllum Linn. bark (MECI). Excision, incision and dead space wound model were inflicted upon four groups of six rats each. In excision and incision wound model, Group I was assigned as control (ointment base). Group II and III were treated with 5% and 10% MECI topical ointment respectively. Group IV was treated with standard nitrofurazone ointment (0.2%). In dead space wound model Group I was assigned as control (1% w/v CMC). Group II and III were treated with 200 and 400 mg/kg b.w., p.o. MECI, respectively. Group IV was treated with standard nitrofurazone ointment (0.2%). The parameters observed were percentage of wound contraction, epithelialization period, tensile strength and hydroxyproline content. Treatment with 10% MECI topical ointment exhibited significant (P < 0.0001) wound healing activity in excision and incision wound model, whereas 400 mg/kg b.w., p.o. MECI extract exhibited significant (P < 0.0001) wound healing activity in dead space wound model. MECI stimulates wound contraction, decreases epithelialization period, and increases tensile strength and hydroxyproline content. KEY WORDS: Excision wound model, incision wound model, dead space wound model, Calophyllum inophyllum Linn.
The present study provides a scientific assessment for the hypoglycemic effect of methanolic extract of Callicarpa macrophylla fruits (MECM) on STZ-induced diabetic rats. Diabetes was induced in Wistar rats by intraperitoneal injection of STZ at a dose of 55 mg/kg body weight for 7 days. Methanolic extract of Callicarpa macrophylla fruits [100 and 200 mg/kg b.w., (p.o.)] was administered to STZ-induced diabetic rats for 14 days. The effect of MECM on blood glucose, serum lipid profile and HbA1c was studied in diabetic rats. Metformin was used as a reference hypoglycemic drug. In OGTT, oral administration of MECM (200 mg/kg b. w., P < 0.05) and metformin (11.3 mg/kg b.w., P < 0.01) showed significant decrease in the blood glucose levels at 60 min. The administration of MECM (100 and 200 mg/kg b.w.) resulted in a significant dose-dependent decrease (P < 0.001) in blood glucose level in STZ-induced Type 2 diabetic rats. Further MECM showed antihyperlipidemic activity as evidenced by significant decrease (P < 0.001) in serum TC, TG, LDL-C, VLDL-C levels coupled together with elevation of HDL-C level (P < 0.001) in STZ-induced Type 2 diabetic rats. HbA1c significantly decreased with MECM (200 mg/kg b.w. and 100 mg/kg b.w., P < 0.01) in STZ-induced diabetic rats. The results suggest that the methanolic extract of Callicarpa m
A series of N-(2-(benzoyl/4-chlorobenzoyl)-benzofuran- 3-yl)-2-(substituted)-acetamide derivatives (4a-l, 5a-l) was synthesized in good yield. All synthesized compounds were in agreement with elemental and spectral data. The anticonvulsant activity of all synthesized compounds was assessed against the maximal electroshock induced seizures (MES) model in mice. Neurotoxicity was evaluated using the rotarod method. The majority of compounds exhibited anticonvulsant activity at a dose of 30 mg kg-1 body mass during 0.5-4 h, indicating their ability to prevent seizure spread at low doses. Relative to phenytoin, [N-(2-(4-chlorobenzoyl)benzofuran-3-yl)-2-(cyclohexyl( methyl) amino)-acetamide] (5i) and [N-(2-(4-chlorobenzoyl)benzofuran-3-yl)-2-(4-methylpiperidin-1- yl)-acetamide] (5c) demonstrated comparable relative anticonvulsant potency of 0.74 and 0.72, respectively, whereas [(N-(2-(4-chlorobenzoyl)benzofuran-3-yl)-2-(4-(furan-2-carbonyl)-piperazin-1-yl)-acetamide] (5f) exhibited the lowest relative potency of 0.16. The ALD50 of tested compounds ranged from 1.604 to 1.675 mmol kg
The present study provides a scientific assessment for the wound healing potential of methanolic extract of Calophyllum inophyllum Linn. bark (MECI). Excision, incision and dead space wound model were inflicted upon four groups of six rats each. In excision and incision wound model, Group I was assigned as control (ointment base). Group II and III were treated with 5% and 10% MECI topical ointment respectively. Group IV was treated with standard nitrofurazone ointment (0.2%). In dead space wound model Group I was assigned as control (1% w/v CMC). Group II and III were treated with 200 and 400 mg/kg b.w., p.o. MECI, respectively. Group IV was treated with standard nitrofurazone ointment (0.2%). The parameters observed were percentage of wound contraction, epithelialization period, tensile strength and hydroxyproline content. Treatment with 10% MECI topical ointment exhibited significant (P < 0.0001) wound healing activity in excision and incision wound model, whereas 400 mg/kg b.w., p.o. MECI extract exhibited significant (P < 0.0001) wound healing activity in dead space wound model. MECI stimulates wound contraction, decreases epithelialization period, and increases tensile strength and hydroxyproline content. KEY WORDS: Excision wound model, incision wound model, dead space wound model, Calophyllum inophyllum Linn.
Hepatotoxicity implies chemical-driven liver damage. Certain medicinal agents, when taken in overdoses and sometimes even when introduced within therapeutic ranges, may injure the organ.The current study was done to investigate the hepatoprotective effect of Polyherbal formulation Mentat against CCl 4 induced hepatotoxicity in rats. Sprague-Dawley rats (male) weighing 200-250 g was used. Hepatotoxicity was induced by administration of 50% CCl 4 in olive oil intraperitoneally every 72 hr for 10 days. Silymarin was used as standard in dose of (0.5 ml/100 g b.w.) and the test drug Mentat was used in dose of (2 ml/kg) was orally administered before or after CCl 4 treatment in various groups. Serum glutamic oxaloacetic transaminase (SGOT), Serum glutamic pyruvic transaminase (SGPT), Alkaline phosphatase (ALP), Total bilirubin (TB) parameters were estimated. Serum SGOT, SGPT, ALP and TB activities significantly decreased (p < 0.05) as compared to CCl 4 treated group. The present study demonstrated that Mentat possesses hepatoprotective effects against CCl 4 induced hepatotoxicity and that the effects are both preventive and curative.
Year 2015
Objective: The investigate the antidiabetic and antihyperlipidemic effect of ethanolic extract of Alocasia indica (EEAI) rhizomes in high-fat diet/streptozotocin (HFD/STZ) and STZ/nicotinamide-induced Type 2 diabetic rats. Methods: Diabetes was induced in male Wistar rats by the administration of a HFD for 15 days/STZ (35 mg/kg b.w., i.p.) and STZ (60 mg/kg b.w., i.p.)/nicotinamide (110 mg/kg b.w., i.p.). EEAI (100 and 200 mg/kg b.w., p.o.) was administered to diabetic rats for 28 days in HFD/STZ-induced Type 2 diabetic rats and for 15 days in STZ/nicotinamide-induced Type 2 diabetic rats. The effect of EEAI on blood glucose and body weight was studied in Type 2 diabetic rats. All these effects were compared with glibenclamide (5 mg/kg b.w., p.o.) as a reference antidiabetic drug. Results: The administration of the EEAI (100 and 200 mg/kg b.w., p.o.) resulted in a significant decrease in blood glucose level and significant increase in body weight in the HFD/STZ and STZ/nicotinamide-induced Type 2 diabetic rats. Further EEAI showed antihyperlipidemic activity as evidenced by significant decrease in serum total cholesterol, triglycerides, low-density lipoprotein cholesterol (LDL-C), very LDL-C levels coupled together with elevation of high-density lipoprotein cholesterol level in diabetic rats in the HFD/STZ and STZ/nicotinamide-induced Type 2 diabetic rats. Conclusion: The results suggest that the EEAI rhizomes possess a promising effect on the HFD/STZ and STZ/nicotinamide-induced Type 2 diabetes. © 2014, Asian Journal of Pharmaceutical and Clinical Research. All Rights Reserved.
Objective: The aim of the present study was a comparative study of neuroprotective effect of telmisartan and donepezil against lipopolysaccharide (LPS)-induced neuroinflammation in mice. Methods: In this study, we investigated the comparative effect of telmisartan (5 mg/kg, p.o.) and donepezil (5 mg/kg, p.o.) in systemic inflammation induced by LPS, ibuprofen (40 mg/kg, p.o.) was used as standard. Mice were treated with a single i.c. injection of LPS (5 μg/5 μl/kg), after 7 days the animal behavior was evaluated by testing specific cognitive functions, on Morris water maze and Pole climbing test. Biochemical estimation for glutathione (GSH), malondialdehyde (MDA) and tumor necrosis factor alpha (TNF-α) was done by enzyme-linked immunosorbent assay plate reader. Results: The neuroprotective effect of telmisartan (5 mg/kg) and donepezil (5 mg/kg) in LPS induced neuroinflammation in mice was compared. Oral administration of telmisartan (5 mg/kg) for 7 days shows a better result in Morris water maze and pole climbing test, in comparison of donepezil. It also increases the level of GSH and decreases the level of MDA and TNF-α in mice brain. Conclusion: The present study demonstrates that telmisartan and donepezil reduces LPS-induced microglial activation, beta-amyloid generation, central nervous system cytokine production, and behavioral symptoms of sickness. In comparative study of telmisartan and donepezil, telmisartan shows significant decrease in escape latency time and transfer latency time in comparison of donepezil. Therefore, telmisartan is more effective as the comparative of donepezil. © 2015, Asian Journal of Pharmaceutical and Clinical Research. All Rights Reserved.
Background: Bauhinia racemosa Lam (BR), an ethnomedicinally important plant is used in various indigenous systems of medicine for the cure of variety of ailments. Its bark is reported to have antifilarial, abortifacient, anthelmintic, analgesic, antipyretic, antimalarial, anti-ulcerogenic, hepatoprotective and various other pharmacological activities. Maintaining quality standards of herbal drugs is the need of today, because of its increasing demand. Aims: The present study was designed to set standard phytochemical and analytical profile of the bark of BR. Materials and Methods: Pharmacognostical, physicochemical and fluorescence parameters along with pH value of the bark of BR were determined. HPTLC fingerprinting was carried out by the CAMAG HPTLC system. Results: The loss on drying, total ash, water-soluble ash, acid-insoluble ash, yield of alcohol-soluble crude extracts, yield of water-soluble crude extracts and pH (1% aqueous extract) were found to be 9.1%, 12.5%, 1.5%, 3.0%, 9.25%, 12.5% w/w and 6.96 respectively. Phytochemicals like carbohydrate, steroid, saponin, alkaloid, anthraquinone glycosides, flavonoid and phenolic compounds were found to be present in the methanolic extract. The fluorescence seen in UV light was of different colour in different solvents. 5 peaks were revealed in HPTLC analysis at wavelength 254 nm with max Rf values in the range of 0.47 to 0.94. A peak with max Rf value of 0.55 comparable to that of quercetin was obtained suggesting the presence of quercetin like flavonoid. Conclusions: The present study will help the future scientists for the correct identification, quality and purity of BR bark or pharmaceutical preparations prepared from it.
The comparative study of neuroprotective effect of angiotensin converting enzyme inhibitors against scopolamine-induced neuroinflammation in albino Wistar rats was studied. Male albino rats were administered with scopolamine to induce memory impairment. The standard nootropic agent, piracetam (200 mg/kg b.w., [i.p.]), perindopril (0.1 mg/kg b.w., [i.p.]), enalapril (0.1 mg/kg b.w., [i.p.]), and ramipril (0.1 mg/kg b.w., [i.p.]) were administered in different group of animals for 5 days. On 5(th) day, scopolamine (1 mg/kg b.w., i.p.) was administered after 60 min of the last dose of test drug. Memory function was evaluated in Morris water maze (MWM) test and pole climbing test (PCT). Biochemical estimations like glutathione (GSH), malondialdehyde (MDA), and acetylcholinesterase activity in the brain were estimated after completion of behavior study. All three test groups shows improvement in learning and memory in comparison to control group. Perindopril treated group showed a more effective significant decrease in escape latency time and transfer latency time compared to enalapril and ramipril treated group on day 4 in MWM test and PCT, respectively. Perindopril shows a significant reduction in MDA level and acetylcholinesterase activity and a significant rise in GSH level compared to enalapril and ramipril. The finding of this study indicates that Perindopril is more effective in memory retention compared to enalapril and ramipril.
Aim: Hormone replacement therapy was considered a safe treatment for short-term therapy. But, because of adverse outcomes such as increased risk of endometrial and breast cancer, stroke and pulmonary thrombo-embolism after its long-term use, women turned to use natural health remedies. Thus, the estrogenic activity of 70% hydro-alcoholic extract of Artocarpus lakoocha fruit (HEAL) was evaluated. Materials and Methods: HEAL was subjected to phytochemical analysis as per standard protocol. Estrogenic potential of HEAL was performed by uterotropic assay, vaginal cytology and measurement of vaginal opening at different doses of 200 mg/kg, 400 mg/kg and 600 mg/kg bw po in Sprague-Dawley (SD) rats and compared with standard drug β-estradiol (2 mg/kg bw, po). Ovariectomized immature and mature female SD rats were administered with HEAL for 7 days. Results: It showed the presence of tannins, saponins, triterpenes, flavonoids, steroids and alkaloids as major secondary metabolites in HEAL. Dose of 600 mg/kg administered in ovariectomized immature and mature female SD rats resulted in significant increase in the uterine wet weight of 219.60±8.71 mg and 906.19±26.91 mg respectively when compared with that of control rats of 110.55±1.16 mg and 505.66±27.38 mg respectively. Only cornified epithelial cells were seen in HEAL-treated rats at the dose of 600 mg/kg indicating the presence of estrogen. Significant vaginal opening was also seen in HEAL-treated rats at the dose of 600 mg/kg. Conclusion: It was concluded that HEAL possess promising estrogenic activity.
Bauhinia racemesa Lam, a small deciduous tree belonging to the family Caesalpiniaceae, is traditionally used in the indigenous system of medicine Ayurveda, Unani and Sidha for the treatment of several ailments like headache, fever, skin and blood diseases, jaundice, chronic dysentery, diarrhoea, and leucorrhoea, infection of malaria, boil, glandular swelling, tumors and cancer. It is also used to cure scorpion bite, to relief food poisoning in cattle and as contraceptive by women. In order to reveal full pharmacological and therapeutic potentials, the aim of the present review was focused on the assessment of its current medicinal uses, phytochemistry, pharmacology and toxicology. Literature survey on scientific journals, books as well as electronic sources was performed. It showed that this plant is of an immense value because of its various potent pharmacological actions shown by it and several pharmacologically active principles like galactolipids, racemosol, de-O-methylracemosol, pacharin, resveratrol which have been isolated from it. It will be definitely useful to explore it for further research to be carried out on this medicinal plant.
Majority of the antidepressant drugs improve depressive symptoms, but they exert multiple unwanted side effects. The search for more efficacious and well tolerated drugs is in progress. Owning to this, the present study was designed to evaluate the antidepressant activity of alcoholic extract of the fruits of Osmanthus fragrans (AEFOF) in mice. It was evaluated using the Tail Suspension Test (TST), Forced Swimming Test (FST) and influence on spontaneous locomotor activity (SLMA) in mice. The AEFOF (75 mg kg-1, peroral (po) and 150 mg kg-1, po) was administered orally in separate groups of Swiss mice for 14 days in TST and FST tests and for 7 successive days in SLMA test. The AEFOF showed a dose dependant reduction in duration of immobility in mice. The dose of 150 mg kg-1 of AEFOF significantly reduced the immobility time of mice in both FST and TST without any significance effect on locomotor activity of mice. The efficacy of extract was found to be comparable to fluoxetine (20 mg kg-1, po). It was found to be toxicologically safe with no deaths of mice when administered orally at the dose of 2000 mg kg-1. From the present study, it can be concluded that the AEFOF possess potent antidepressant activity as shown by the TST and FST tests and is toxicologically safe
To study the estrogenic activity of the hydro-alcoholic extract of Bambusa arundinaceae leaves (HEBA) in female Wistar rats. The dried powdered leaves were extracted with hydroalcoholic mixture (60%), and the resultant extract was subjected for phytochemical analyses to identify different phytoconstituents. HEBA were administered to ovariectomized rats for 7 days at three different doses (viz., 200, 300, 400 mg/kg body weight, p.o.) and their estrogenic activity were compared with each of daily treatment with 0.2 mg/kg body weight, i.p. conjugated equine estrogen as a positive control or olive oil as a negative control. Estrogenic activity was evaluated by doing uterotropic assay, vaginal cytology and measurement of vaginal opening in female Wistar rats. Oral administration of HEBA in ovariectomized immature and mature female Wistar rats in a dose of 400 mg/kg b.w. resulted in significant increase in the uterine wet weight (in mg) (224.82 ± 7.01) and (912.25 ± 27.22) when compared with ovariectomized control rats (111.52 ± 3.17) and (506.67 ± 21.39). HEBA (400 mg/kg b.w., p.o.) treated rats, showing only cornified epithelial cells which was an indication of the presence of the estrogen and also showed 100% vaginal opening. It was observed that HEBA possess significant estrogenic activity at 400 mg/kg b.w., p.o. which was evident by uterotropic assay, measurement of vaginal opening, and histopathological changes.
Year 2014
Cucurbita maxima (CM) seed oil is commonly used in Indian folk medicine to treat various ailments. We have investigated the effect of CM seed oil on memory impairment induced by scopolamine in rats. Male adult Wistar rats were administered scopolamine 1 mg/kg body weight, i.p. or 1.25 mg/kg body weight, s.c. to induce memory impairment. The nootropic agent piracetam 100 mg/kg body weight, i.p. and CM seed oil 100 and 200 mg/kg body weight, p.o. were administered daily for five consecutive days. The memory function was evaluated in the Morris water maze (MWM) test, the social recognition test (SRT), the elevated plus maze (EPM) test, and the pole climbing test (PCT). Acetylcholinesterase (AChE) activity and oxidative stress parameters were estimated in the cortex, hippocampus, and cerebellum of the brains after completion of the behavioural studies. The effects of scopolamine on the levels of the tumour necrosis factor alpha (TNF-alpha) transcript were also investigated. Scopolamine caused memory impairment in all the behavioural paradigms along with a significant increase in the AChE activity and oxidative stress in the brain. Scopolamine also caused a significant increase in the expression of TNF-alpha in the hippocampus. CM seed oil exhibited antiamnesic activity as indicated by a significant reduction in the latency time in the MWM test and decreased social interaction during trial 2 in the SRT. Further, treatment with CM seed oil significantly decreased the AChE activity and malondialdehyde levels and increased the glutathione level in brain regions. CM seed oil also significantly decreased the expression of TNF-alpha in the hippocampus. The effect of CM seed oil on behavioural and biochemical parameters was comparable to that observed in rats treated with piracetam. These results indicate that CM seed oil may exert antiamnesic activity which may be attributed to the inhibition of AChE and inflammation as well as its antioxidant activity in the brain.
Cucurbita maxima (CM) seed oil is commonly used in Indian folk medicine to treat various ailments. We have investigated the effect of CM seed oil on memory impairment induced by scopolamine in rats. Male adult Wistar rats were administered scopolamine 1 mg/kg body weight, i.p. or 1.25 mg/kg body weight, s.c. to induce memory impairment. The nootropic agent piracetam 100 mg/kg body weight, i.p. and CM seed oil 100 and 200 mg/kg body weight, p.o. were administered daily for five consecutive days. The memory function was evaluated in the Morris water maze (MWM) test, the social recognition test (SRT), the elevated plus maze (EPM) test, and the pole climbing test (PCT). Acetylcholinesterase (AChE) activity and oxidative stress parameters were estimated in the cortex, hippocampus, and cerebellum of the brains after completion of the behavioural studies. The effects of scopolamine on the levels of the tumour necrosis factor alpha (TNF-α) transcript were also investigated. Scopolamine caused memory impairment in all the behavioural paradigms along with a significant increase in the AChE activity and oxidative stress in the brain. Scopolamine also caused a significant increase in the expression of TNF-α in the hippocampus. CM seed oil exhibited antiamnesic activity as indicated by a significant reduction in the latency time in the MWM test and decreased social interaction during trial 2 in the SRT. Further, treatment with CM seed oil significantly decreased the AChE activity and malondialdehyde levels and increased the glutathione level in brain regions. CM seed oil also significantly decreased the expression of TNF-α in the hippocampus. The effect of CM seed oil on behavioural and biochemical parameters was comparable to that observed in rats treated with piracetam. These results indicate that CM seed oil may exert antiamnesic activity which may be attributed to the inhibition of AChE and inflammation as well as its antioxidant activity in the brain.
ABSTRACT: When designing small molecules to interact with the targets, oneshould consider stereo selectivity. As considerations for exploring structurespace evolve, chirality is increasingly important. Binding affinity for a chiraldrug can differ for diastereomers and between enantiomers. For the virtualscreening and computational design stage of drug development, this problemcan be compounded by incomplete stereochemical information in structurelibraries leading to a "coin toss" as to whether or not the "ideal" chiral structureis present. Creating every stereoisomer for each chiral compound in a structurelibrary leads to an exponential increase in the number of structures resulting inpotentially unmanageable file sizes and screening times. Therefore, only keychiral structures, enantiomeric pairs based on relative stereochemistry need beincluded, and lead to a compromise between exploration of chemical space andmaintaining manageable libraries. In clinical environments, enantiomers ofchiral drugs can have reduced, no, or even deleterious effects. This underscoresthe need to avoid mixtures of compounds and focus on chiral synthesis.Governmental regulations emphasizing the need to monitor chirality in drugdevelopment have increased. The United States Food and Drug Administrationissued guidelines and policies in 1992 concerning the development of chiralcompounds. These guidelines require that absolute stereochemistry be known forcompounds with chiral centers and that this information should be establishedearly in drug development in order that the analysis can be considered valid.From exploration of structure space to governmental regulations it is clear thatthe question of chirality in drug design is of vital importance
Objective: The present work was undertaken to investigate the effects of aqueous extract from Cinnamomum tamala leaf in experimentally induced hyperlipidemia in rats. Materials and methods: The antihyperlipidemic effect of aqueous extract from Cinnamomum tamala leaf (CTLE) was evaluated in male albino rats of Wistar strain at two graded doses levels viz. 200 and 400 mg/kg of body weight. The following two models were used for the antihyperlipidemic activity, high fat diet and Triton X-100-induced hyperlipidemia in rat. CTLE (200 mg/kg, b.w. & 400 mg/kg, b.w.) was administered orally for 28 days in high fat diet and 7 days in Triton X-100 (100 mg/kg, i.p.) induced hyperlipidemia in rat. The efficacy of CTLE was compared to Standard Atorvastatin (30 mg/kg, p.o.) in high fat diet and Atorvastatin (10 mg/kg, p.o.) in Triton X-100-induced hyperlipidemia. Effect of CTLE on serum lipid profile like TC, TG, HDL-C, weight gain and LDL-C, and biochemical parameters like SGOT and SGPT were estimated. Result: CTLE significantly reduced the TC, TG, LDL-C and increase the HDL-C in both high fat diet & Triton X-100-induced hyperlipidemic rats. The increase in weight in rats administered with CTLE was less when compared to rats fed with high-fat diet and Triton X-100. The levels of SGOT and SGPT have been significantly (P < 0.001) decreased by the administration of CTLE in the experimental groups. The efficacy of CTLE was found to be comparing to Atorvastatin (30 mg/kg, p.o.) in high fat diet and Atorvastatin (10 mg/kg, p.o.) in Triton X-100-induced hyperlipidemia. CTLE showed a significant antihyperlipidemic effect in both high fat diet and Triton X-100-induced hyperlipidemic rats in a dose-dependent manner during 28 days and 7 days of treatment period. Conclusion: The results demonstrate that the CTLE has a definite antihyperlipidemic potential.
Year 2013
A series of 12, N-(2-benzoylbenzofuran-3-yl)-3-(substituted)propanamide analogs was designed and synthesized to meet the pharmacophore requirement essential for anticonvulsant activity. All the compounds were characterized by IR, 1H NMR and mass spectral data followed by their anticonvulsant evaluation according to the Antiepileptic Drug Development Program (ADD) protocol. The present study has proved the hypothesis concerning the pharmacophore model with essential binding sites. N-(2-benzoylbenzofuran-3-yl)-3-(4-(2-fluorophenyl)piperazin-1-yl) propanamide, 6h was found to be the most active compound in both maximal electroshock seizure (MES) and subcutaneous metrazol (scMET) seizure test at 30 and 100 mg/kg respectively at 0.5 and 4.0 h.
Alzheimer’s disease (AD) is a neurodegenerative disorder clinically characterized by progressive loss of cognitive abilities such as memory, speaking and problem solving. Scopolamine model is based on cholinergic hypofunction and widely used as experimental model of memory impairment in the antidementic drug development. Present study investigated the effect of ethanolic extract of Bambusa arundinacea leaves (EEBA) on scopolamine induced memory impairment in rats using Morris water maze (MWM) and social recognition tests (SRT). The results showed that EEBA prevented scopolamine induced amnesia in both the behavioural paradigms, MWM and SRT, in rats. Further, the antiamnesic effect of EEBA was associated with significant reduction in oxidative stress and AChE activity in rat brain regions. Preventive administration of EEBA for 5 days dose-dependently ameliorated scopolamine induced memory impairment in rats. In MWM test, EEBA caused significant reduction in latency to reach hidden platform in comparison to the scopolamine treated group indicating successful learning. These results suggested that the antiamnesic effect of EEBA on scopolamine induced memory deficit may be mediated via facilitation of the central cholinergic nervous system. Administration of EEBA showed dose dependent inhibition of scopolamine induced elevation of AChE activity. The inhibition of AChE by EEBA could lead to increased ACh level in brain which may be responsible for its antiamnesic effect. The standard drug piracetam also reduced AChE activity in rat brain regions. In conclusion, this study clearly shows the antiamnesic effect of ethanolic extract of Bambusa arundinacea leaves which may be attributed to its antioxidant and anti-AChE effects. Though the exact mechanism for antioxidant and AChE inhibition by EEBA is not known but it can be attributed to the presence of various phytoconstituents as revealed in our preliminary investigation. However, further investigations are warranted to evaluate the exact mechanism of neuroprotective effect of EEBA and the phytoconstituents responsible for the observed effects.
Anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. The goal of an anticonvulsant is to suppress the rapid and excessive firing of neurons that start a seizure. The use of current antiepileptic drugs has been questioned due to the non selectivity of the drugs and the undesirable side effects posed by them. This lead to the search for antiepileptic compounds with more selective activity and lower toxicity continues to be an area of investigation in medicinal chemistry. Semicarbazones are compounds which are synthesized by the condensation of semicarbazide and aldehydes/ketones. The literature survey revealed that semicarbazones had been emerged as a compound with broad range of activities including anticonvulsant, antitubercular, anticancer and antimicrobial activity. In this review chemistry and anticonvulsant activity of semicarbazone analogues are discussed.
Year 2012
A series of N-(2-benzoylbenzofuran-3-yl)-4-(substituted) butanamides (IVa-f) were synthesized and evaluated for anticonvulsant activity and neurotoxicity. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. All the compounds was found active in MES tests. Compounds IVb, IVc, IVd and IVf were found to be potent and had activity at lower dose of 30mg/ kg in MES-test. Compounds IVa and IVe were less toxic as compared with the standard drug phenytoin.
A series of N-(2-benzoylbenzofuran-3-yl)-4-(substituted)butanamides (IIIa-f) were synthesized in good yield and evaluated for anticonvulsant activity and neurotoxic study. The identity of the synthesized compounds was confirmed on the basis of their elemental analysis and spectral data. In anti-MES test compounds IIIb, IIIc, IIId and IIIf showed potent activity. Compounds IIIa and IIIe were less toxic as compared with the standard drug phenytoin.
Year 2011
1,3,4-Thiadiazole nucleus exhibited remarkable pharmacological activities. Literature indicates that compounds having 1,3,4-Thiadiazole nucleus have wide range of pharmacological activities that include antibacterial, antifungal, antitubercular, antiviral, antileishmanial, anti-inflammatory, analgesic, CNS depressant, anticonvulsant, anticancer, antioxidant, antidiabetic, molluscicidal, antihypertensive, diuretic. The present review provides a broad view of the antimicrobial activity possessed by compounds having a 1,3,4-Thiadiazole nucleus.
Lawsonia inermis L. is a much branched glabrous shrub or small tree (2-6 m in height), cultivated for its leaves although stem bark, roots, flowers and seeds have also been used in traditional medicine. The plant is reported to contain Lawsone, Esculetin, Fraxetin, Isoplumbagin, Scopoletin, Betulin, Betulinic acid, Hennadiol, Lupeol, Lacoumarin, Laxanthone, Flavone glycosides, Two pentacytic triterpenes. The plant has been reported to have analgesic, hypoglycemic, antimalarial, hepatoprotective, nootropic, immunostimulant, anti-inflammatory, antibacterial, antimicrobial, antifungal, antiviral, antiparasitic, antitrypanosomal, antidermatophytic, antioxidant, anthelmintic, antifertility, tuberculostatic and anticancer properties. It is now considered as a valuable source of unique natural products for development of medicines against various diseases and also for the development of industrial products. This review gives a view mainly on the traditional uses, phytochemistry and pharmacological actions of the plant.
Traditional Medicines derived from medicinal plants are used by about 60% of the world’s population. This review focuses on Herbal drugs used in the treatment of Anxiety disorder. Anxiety disorders, including generalized anxiety disorder (GAD), panic disorder, post-traumatic stress disorder (PTSD), and obsessive compulsive disorder (OCD), are the most prevalent behavioral disorders in the United States, affecting 17.2% of the population. The use of herbal supplements to treat anxiety has been increasing and the mechanisms of action of several are being elucidated. A list of medicinal plants with proven antianxiety effects used in treatment of Anxiety is compiled. These include, Citrus paradise, Cirsium rivulare, Drymaria cordata, Colocasia esculenta, Souroubea sympetala, Rollinia mucosa, Aethusa cynapium, Uncaria rhynchophylla, Cinnamomum cassia, Gastrodia elata, Apocynum venetum, Turnera aphrodisiaca, Scutellaria lateriflora, Valeriana officinalis, Galphimia glauca etc.
Benzofuran display a diverse array of pharmacological activities. The purpose of this review is to provide an overview of the pharmacological activities of Benzofuran. Literature indicates that compounds having Benzofuran nucleus have wide range of therapeutic uses that include antibacterial, antifungal, anti-inflammatory, analgesic, antidepressant, anticonvulsant, antitumor, imaging, Anti-HIV, antidiabetic, antitubercular, antioxidant and miscellaneous activity. ________________________________________
Year 2010
A new series of N-aryl/alkylidene-4-(5-bromo-1,3-dioxo-1,3-dihydro-2H- isoindol-2-yl) butanoyl hydrazones (4a-I) were synthesized and evaluated for their anticonvulsant activity in MES test according to the protocols of Antiepileptic Drug Development (ADD) programme of National Institute of Health (NIH, Bethesda, USA). The most active compounds of the series were 4f and 4i at the dose of 30 mg/kg (i.p.) 0.5 hr, after administration. In neurotoxic screen (NT), all the compounds were found to be devoid of neurotoxicity at 30 mg/kg (i.p.).
Viruses are particles which can specifically infect many kinds of organisms such as bacteria, plants, animals and humans. These organisms are called host cells. Recently, bacteriophages, viruses specifically infecting bacteria, have become interesting to replace antibiotics to treat diseases in animals and humans caused by pathogenic bacteria infections. This article briefly describes about the discovery of bacteriophages, and their therapeutic uses in animals and humans
Year 2009
Purpose: To investigate the effect of amitriptyline (Ami) and sertraline (Sert) in diabetes neuropathy. Methods: Diabetes was induced in 3 groups of rats (n=6) with streptozotocin (STZ, 55mg/kg, i.p.). Two of the groups of diabetic rats received amitriptyline (15 mg/kg, p.o) and sertraline (30 mg/kg, p.o.) while another 2 groups (n=6) received the same drug treatment without prior administration of STZ. A normal group (n=6) of rats and STZ-induced group (n=6) of diabetic rats served as controls. The blood glucose, glycosylated hemoglobin (GHb), pain sensitivity and neuromuscular strength in all the rats were determined. Results: Ami (15mg/kg, p.o.) produced severe hyperglycemia (p < 0.01) whereas Sert (30mg/kg, p.o.) produced significant hypoglycaemia in the diabetic rats. Ami significantly increased the GHb% level while Sert had no significant effect. Both Ami and Sert raised the grip strength that was significantly reduced by STZ. When administered for 3 weeks, Ami and Sert increased the STZ induced reduction of the grip strength in the diabetic rats (p< 0.01). STZ (55mg/kg, i.p) increased the pain sensitivity. Pain sensitivity was significantly reduced by Ami (15 mg/kg, p.o, administered for 3 weeks) in the diabetic rats but marginally reduced in the normal group. However 3-week administration of Sert (30 mg/kg, p.o.) significantly reduced the pain sensitivity in both the diabetic and normal rats (p < 0.01) when compared with STZ treated group. Conclusion: Sertraline could offer a good choice in the treatment of diabetic neuropathy particularly in patients with depression being treated with amitriptyline.
A new series of 1,2,3-triazole derivatives were synthesized and the structures of these compounds were established by means of IR, 1H NMR, and elemental analysis. All the compounds (4a-p) were screened for antifungal, antiinflammatory and analgesic activity. Some of the synthesized compounds showed moderate to good antiinflammatory and analgesic activity.
A series of 4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-butyryl N-(substituted phenyl) amides (3a-I) were synthesized and evaluated for their anticonvulsant activity in MES test according to the protocols of Antiepileptic Drug Development (ADD) programme of National Institutes of Health (NIH, Bethesda, USA).The most active compounds of the series were 3a, 3c, 3d, 3f, 3g, 3i and 3k at the dose of 30 mg/kg (i.p.) 0.5 h and 4 h after administration. In neurotoxic screen (NT), 3d, 3i and 3k were less toxic when compared with the other compounds.
Year 2008
Syn: Horseradish tree, Drumstick tree, Never Die tree, West Indian Ben tree, and Radish tree Plants have played a significant role in maintaining human health and improving the quality of human life for thousands of years and have served humans well as valuable components of medicines, seasonings, beverages, cosmetics and dyes. Herbal medicine is based on the premise that plants contain natural substances that can promote health and alleviate illness. In recent times, focus on plant research has increased all over the world and a large body of evidence has collected to show immense potential of medicinal plants used in various traditional systems. Today, we are witnessing a great deal of public interest in the use of herbal remedies. Further more many western drugs had their origin in plant extract. There are many herbs, which are predominantly used to treat cardiovascular problems, liver disorders, central nervous system, digestive and metabolic disorders. Given their potential to produce significant therapeutic effect, they can be useful as drug or supplement in the treatment / management of various diseases. Herbal drugs or medicinal plants, their extracts and their isolated compound(s) have demonstrated spectrum of biological activities. Such have been used and continued to be used as medicine in folklore or food supplement for various disorders. Ethnopharmacological studies on such herbs/medicinally important plants continue to interest investigators throughout the world.
... Galacturonic acid, arabinose, galactose, rhamnose and glucose, mannose, neutral sugars, xylose and protein Lai et al. (2006) and Jawaid et al. (2015a, b, c) 105. benzyl isothiocyanate, niazirin, niazirinin and niaziminin A and B Sutalangka et al. (2013) and Kamal and Jawaid (2008) cure for patients suffering with them. In traditional system of medicines, various natural products have been used for neuroprotection. ...

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