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Asian Pacific Journal of Tropical Biomedicine 2018年第7期8卷 352-359页

作者： Amit D.Kandhare Anwesha A.Mukherjee Subhash L.Bodhankar Department of Pharmacology Poona College of Pharmacy Bharati Vidyapeeth Deemed University

Objective: To evaluate the protective effect of morin against pentylenetetrazol(PTZ)-induced tonic-clonic convulsions in mice. Methods: Swiss albino mice(18-22 g) was used to induce convulsions by intraperitoneal(i.p.) administration of PTZ(90 mg/kg). Mice were either pretreated with morin(10, 20 and 40 mg/kg) or vehicle(distilled water, 10 mg/kg) 45 min before PTZ administration. Various behavioral and biochemical parameters were assessed. Results: PTZ administration resulted in significant production(P<0.001) of tonic-clonic conclusion and mortality in mice. PTZ-induced increase in the duration of convulsion, onset of convulsion and mortality was inhibited significantly by morin(20 and 40 mg/kg) administration. The PTZinduced decrease in brain GABA, dopamine and Na+K+ATPase levels and increase in xanthine oxidase activity were inhibited significantly by morin(20 and 40 mg/kg) treatment. The increased levels of malondialdehyde and nitric oxide level were significantly decreased by morin(20 and 40 mg/kg) treatment. Also, reduced levels of superoxide dismutase and glutathione were increased significantly by morin treatment. Conclusions: Results of the present study indicate that morin showed its anti-convulsant effect via modulating the levels of brain GABA, Na^+K^+ATPase, and oxido-nitrosative stress. Thus, morin can be a potential candidate for further clinical evaluations as an anti-epileptic agent.

关键词： Brain GABA Epilepsy Morin Nitric oxide Pentylenetetrazol Oxidative stress Xanthine oxidase

Determination of the mitigating effect of colon-specific bioreversible codrugs of mycophenolic acid and aminosugars in an experimental colitis model in Wistar rats

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World Journal of Gastroenterology 2018年第10期24卷 1093-1106页

作者： Shakuntala Santosh Chopade Suneela Sunil Dhaneshwar Department of Pharmaceutical Chemistry Poona College of Pharmacy Bharati Vidyapeeth University

AIM To design colon-targeted codrugs of mycophenolic acid(MPA) and aminosugars as a safer option to mycophenolate mofetil(MMF) in the management of inflammatory bowel disease. METHODS Codrugs were synthesized by coupling MPA with aminosugars(D-glucosamine and D-galactosamine) using EDCI coupling. The structures were confirmed by infrared radiation, nuclear magnetic resonance, mass spectroscopy and elemental analysis. The release profile of codrugs was extensively studied in aqueous buffers, upper gastrointestinal homogenates, faecal matter and caecal homogenates(in vitro) and rat blood(in vitro). Anti-colitic activity was assessed in 2,4,6-trinitrobezenesulfonic acid-induced colitis in Wistar rats by the estimation of various demarcating parameters. Statistical evaluation was performed by applying one-way and two-way ANOVA when compared with the disease *** The prodrugs resisted activation in HCl buffer(pH 1.2) and stomach homogenates of rats with negligible hydrolysis in phosphate buffer(p H 7.4) and intestinal homogenates. Incubation with colon homogenates(in vitro) produced 76% to 89% release of MPA emphasizing colon-specific activation of codrugs and the release of MPA and aminosugars at the site of action. In the in vitro studies, the prodrug of MPA with D-glucosamine(MGLS) was selected which resulted in 68% release of MPA in blood. in vitro studies on MGLS revealed its colon-specific activation after a lag time of 8 h which could be ascribed to the hydrolytic action of N-acyl amidases found in the colon. The synthesized codrugs markedly diminished disease activity score and revived the disrupted architecture of the colon that was comparable to MMF but superior to MPA. CONCLUSION The significant attenuating effect of prodrugs and individual aminosugars on colonic inflammation proved that the rationale of the codrug approach is valid.

关键词： Mycophenolic acid Mutual prodrug Inflammatory bowel disease Mycophenolate mofetil

Flood basalt hosted palaeosols:Potential palaeoclimatic indicators of global climate change

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Geoscience Frontiers 2014年第6期5卷 791-799页

作者： M.R.G.Sayyed Department of Geology Poona College (University of Pune)CampPune 411 001MaharashtraIndia

Since continental sediments （in addition to the marine geological record） offer important means of deciphering environmental changes, the sediments hosted by the successive flows of the continental flood basalt provinces of the world should be treasure houses in gathering the palaeoclimatic data. Palaeosols developed on top of basalt flows are potentially ideal for palaeoenvironmental reconstructions because it is easy to determine their protolith geochemistry and also they define a definite time interval. The present paper summarizes the nature of the basalt-hosted palaeosols formed on the flood basalts provinces from different parts of the ~lobe havin~ different ages.

关键词： Continental flood basalts Palaeosols Weathering Palaeoclimates Global change

Marker-based standardization and investigation of nutraceutical potential of Indian propolis

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Journal of Integrative Medicine 2017年第6期15卷 483-494页

作者： nanaware sadhana sathiyanarayanan lohidasan kakasaheb ramoo mahadik department of pharmaceutical chemistry bharati vidyapeeth universitypoona college of pharmacyPune 411038MaharashtraIndia

OBJECTIVE： Propolis, a resinous material collected by honey bees from various plants, has been explored globally for its medicinal and nutritional properties. However, research over Indian propolis is at infancy. This study was designed to investigate nutraceutical potential of Indian propolis. METHODS： In the present study, propolis extract was standardized with respect to markers caffeic acid phenethyl ester, caffeic acid, galangin, luteolin, curcumin, apigenin, pinocembrin and quercetin by new high-performance thin-layer chromatographic （HPTLC） methods. The physico-chemical analysis, residues analysis and in vitro antioxidant activity analysis were performed. Nutraceutical value was examined in terms of fats, fibers, minerals, proteins, polysaccharides, total carbohydrates, and energy value. RESULTS： The developed HPTLC methods were found to be simple, reliable accurate, and the validation parameters were within the limits of the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use guidelines. Macerated ethanolic extract of propolis （MEEP） was found to have polyphenolic content of （20.99 ＋ 0.24） mg/g and flavonoids content of （8.39 ＋ 0.04） mg/g. MEEP was found to comprise of （283.33 ＋ 51.31） g/kg fats, （30.07 ＋ 7.30） g/kg fibers, （102.56 ＋ 2.84） g/kg proteins and （389.36 ＋ 57.50） g/kg carbohydrate with a calorie value of （38 409.33 ＋ 6 169.80） kJ/kg. It was found that Indian propolis exhibited high nutraceutical value and showed absence of pesticides and heavy metals. The MEEP showed in vitro antioxidant activity with inhibitory concentration of （12.24 ＋ 4.64） pg/mL. CONCLUSION： The present work explores Indian propolis as a potential nutritious candidate. The proposed analytical methods can be applied in future screening of the quality of Indian propolis.

关键词： propolis high-performance thin-layer chromatography nutraceutical value antioxidant activity

Understanding peroral absorption:regulatory aspects and contemporary approaches to tackling solubility and permeability hurdles

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Acta Pharmaceutica Sinica B 2017年第3期7卷 260-280页

作者： Prachi B.Shekhawat Varsha B.Pokharkar Department of Pharmaceutics Poona College of PharmacyBharati Vidyapeeth Deemed UniversityErandwaneKothrudPune 411038India

Oral drug absorption is a process influenced by the physicochemical and biopharmaceutical properties of the drug and its inter-relationship with the gastrointestinal tract. Drug solubility, dissolution and permeability across intestinal barrier are the key parameters controlling absorption. This review provides an overview of the factors that affect drug absorption and the classification of a drug on the basis of solubility and permeability. The biopharmaceutical classification system(BCS) was introduced in early90's and is a regulatory tool used to predict bioavailability problems associated with a new entity, thereby helping in the development of a drug product. Strategies to combat solubility and permeability issues are also discussed.

关键词： BCS Solubility Permeability Formulation strategies Factors affecting absorption

Investigation of mitigating effect of colon-specific prodrugs of boswellic acid on 2,4,6-trinitrobenzene sulfonic acidinduced colitis in Wistar rats: Design, kinetics and biological evaluation

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World Journal of Gastroenterology 2017年第7期23卷 1147-1162页

作者： Ajinkya Sarkate Suneela S Dhaneshwar Department of Pharmaceutical Chemistry Poona College of PharmacyBharati Vidyapeeth UniversityMaharashtra 411038India

To develop a colon-targeting bioreversible delivery system for β-boswellic acid (BBA) and explore utility of its prodrugs in 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis in *** of 4 co-drugs of BBA with essential amino acids was achieved by CDI coupling, followed by their spectral characterization. In vitro kinetics were studied by HPLC in aqueous buffers, homogenates of gastrointestinal tract and fecal matter. In vivo kinetic studies were performed in Wistar rat plasma, urine and feces. The prodrugs were screened in TNBS-induced colitis modeled Wistar rats. Statistical significance was assumed at P < 0.05, P < 0.01, P < 0.001 when compared with disease controls using one-way and two-way *** were stable in 0.05 mol/L HCl buffer (pH 1.2) and stomach homogenates. Negligible hydrolysis was observed in phosphate buffer and intestinal homogenates. Substantial release (55%-72% and 68%-86%) of BBA was achieved in rat fecal matter and homogenates of colon. In vivo studies of BBA with L-tryptophan (BT) authenticated colon-specific release of BBA. But, surprisingly substantial concentration of BBA was seen to reach the systemic circulation due to probable absorption through colonic mucosa. Site-specifically enhanced bioavailability of BBA could be achieved in colon, which resulted in demonstration of significant mitigating effect on TNBS-induced colitis in rats without inducing any adverse effects on stomach, liver and pancreas. Prodrug of BT was found to be 1.7% (P < 0.001) superior than sulfasalazine in reducing the inflammation to colon among all prodrugs *** outcome of this study strongly suggests that these prodrugs might have dual applicability to inflammatory bowel disease and chronotherapy of rheumatoid arthritis.

关键词： Inflammatory bowel disease Boswellic acid Complementary and alternative medicine Colon-targeting Mutual prodrugs Amino acids TNBS-induced colitis

Reviving Fertility:Phytochemicals as Natural Allies in the Fight against Non-genetic Male Infertility

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Clinical Complementary Medicine and Pharmacology 2024年第1期4卷 112-128页

作者： Vivek P.Chavda Shreya S Sonak Pankti C.Balar Krupa Vyas Pranali Palandurkar Komal Mule Krishna Patel Vivek Hala Dixa A.Vaghela Devarshi Acharya Akta Vaishnav Jimil Gandhi Vasso Apostolopoulos Department of Pharmaceutics and Pharmaceutical Technology L M College of PharmacyAhmedabadGujarat 380008India Bharati Vidyapeeth university’s poona College of Pharmacy ErandwaneKothrudPune 411038India Pharmacy section L M College of PharmacyAhmedabadGujarat 380008India university Department of Pharmaceutical Sciences R.T.M Nagpur 440033India Department of Pharmaceutics Khyati College of PharmacyAhmedabad 380009India IICISST Sardar Patel UniversityVallabh Vidyanagar 388120India Institute for Health and Sport Immunology and Translational ResearchVictoria UniversityMelbourneVIC 3030Australia Immunology Program Australian Institute for Musculoskeletal ScienceMelbourneVIC 3021Australia

Background:Male infertility poses a growing challenge to the healthcare system,with its prevalence on the *** lifestyle,food,and addictions such as smoking,alcoholism,*** the *** several approaches are being investigated to prevent and treat this condition,each therapeutic approach has its *** medications continue to play a crucial role in the healthcare *** recent years,there has been a shift towards determining the efficacy of phytochemicals(or,herbal drugs)as ***:To evaluate the effect of various herbs,plant,metabolites,or a part of plant in management of non-genetic male ***:The male infertility-associated keywords were searched in PubMed,excluding those non-English writen papers.A total of 146 pertinent and closely connected records were included for full reading and inclusion in the systemic ***:The manuscript focuses on individual herbal drug components,their active ingredients,their role in improving the condition and quality of life,and decreasing the prevalence of male ***:Herbal medicinal plants show promising outcomes to treat male *** alternatives are appealing and have regained *** future holds promise for some of these herbal treatments to advance with many showing improved outcomes in males with infertility issues.

关键词： Male infertility Plant-based management Phytochemical Herbal drug Traditional Chinese medicine

Naringin ameliorates acetic acid induced colitis through modulation of endogenous oxido-nitrosative balance and DNA damage in rats

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The Journal of Biomedical Research 2014年第2期28卷 132-145页

作者： Venkatashivam Shiva Kumar Anuchandra Ramchandra Rajmane Mohammad Adil Amit Dattatraya Kandhare Pinaki Ghosh Subhash Laxman Bodhankar Department of Pharmacology Poona College of PharmacyBharati Vidyapeeth Deemed University

The aim of this study was to evaluate the effect of naringin on experimentally induced inflammatory bowel dis- ease in rats. Naringin （20, 40 and 80 mg/kg） was given orally for 7 days to Wistar rats before induction of colitis by intrarectal instillation of 2 mL of 4% （v/v） acetic acid solution. The degree of colonic mucosal damage was analyzed by examining mucosal damage, ulcer area, ulcer index and stool consistency. Intrarectal administration of 4% acetic acid resulted in significant modulation of serum alkaline phosphatase, lactate dehydrogenase, superoxide dismutase （SOD）, glutathione （GSH）, malondialdehyde （MDA） and myeloperoxidase （MPO） content along with colonic nitric oxide （NO）, xanthine oxidase （XO） level and protein carbonyl content in the colonic tissue as well as in blood. Naringin （40 and 80 mg/kg） exerted a dose dependent （P 〈 0.05） ameliorative effect, as it significantly increased hematological parameter as well as colonic SOD and GSH. There was a significant （P 〈 0.05） and dose dependant inhibition of macroscopical score, ulcer area along with colonic MDA, MPO activity by the 7 days of pretreatment of naringin （40 and 80 mg/kg）. Biochemical studies revealed a significant （P 〈 0.05） dose dependant inhibition in serum alkaline phosphatase （ALP） and lactate dehydrogenase （LDH） levels by pretreatment of naringin. Increased levels of colonic NO, XO, protein carbonyl content and DNA damage were also sig- nificantly decreased by naringin pretreatment. The findings of the present investigation propose that naringin has an anti-inflammatory, anti-oxidant and anti-apoptotic potential effect at colorectal sites as it modulates the production and expression of oxidative mediators such as MDA, MPO, NO and XO, thus reducing DNA damage.

关键词： acetic acid, apoptosis, fluorimetric analysis of DNA unwinding, inflammatory bowel disease, my-eloperoxidase, naringin, nitrite/nitrate, oxidative stress porotein carbonyl content, vascular permeability, xanthineoxidase

Amelioration of hepatotoxicity by biocleavable aminothiol chimeras of isoniazid: Design, synthesis, kinetics and pharmacological evaluation

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World Journal of Hepatology 2018年第7期10卷 496-508页

作者： Neha Vithal Bhilare Suneela Sunil Dhaneshwar Kakasaheb Ramoo Mahadik Department of Pharmaceutical Chemistry Poona College of Pharmacy Bharati Vidyapeeth University

AIM To overcome the hazardous effects on liver caused by long-term use of antitubercular agent isoniazid(INH) by developing a novel hepatoprotective prodrug strategy by conjugating INH with aminothiols as antioxidant promoities for probable synergistic *** INH was conjugated with N-acetyl cysteine(NAC) and N-(2)-mercaptopropionyl glycine using the SchottenBaumann reaction and with L-methionine using Boc-anhydride through a biocleavable amide linkage. Synthesized prodrugs were characterized by spectral analysis, and in vitro and in vivo release studies were carried out using HPLC. Their hepatoprotective potential was evaluated in male Wistar rats by performing liver function tests, measuring markers of oxidative stress and carrying out histopathology *** Prodrugs were found to be stable in acidic(pH 1.2) and basic(pH 7.4) buffers and in rat stomach homogenates, whereas they were hydrolysed significantly(59.43%-94.93%) in intestinal homogenates over a period of 6 h. Upon oral administration of prodrug NI to rats, 52.4%-61.3% INH and 47.4%-56.8% of NAC were recovered in blood in 8-10 h. Urine and faeces samples pooled over a period of 24 h exhibited 1.3%-2.5% and 0.94%-0.9% of NAC, respectively, without any presence of intact NI or INH. Prodrugs were biologically evaluated for hepatoprotective activity. All the prodrugs were effective in abating oxidative stress and re-establishing the normal hepatic physiology. The effect of prodrug of INH with NAC in restoring the levels of the enzymes superoxide dismutase and glutathione peroxidase and abrogating liver damage was noteworthy especially. CONCLUSION The findings of this investigation demonstrated that the reported prodrugs can add safety and efficacy to future clinical protocols of tuberculosis treatment.

关键词： Aminothiols antioxidants N-acetyl cysteine N-(2-mercaptopropionyl)glycine isoniazid L-methionine liver injury tuberculosis

Association of smoking, alcohol and NSAIDs use with expression of cag A and cag T genes of Helicobacter pylori in salivary samples of asymptomatic subjects

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Asian Pacific Journal of Tropical Biomedicine 2012年第6期2卷 479-484页

作者： Pinaki Ghosh Subhash Laxmanrao Bodhankar Department of Pharmacology Poona College of Pharmacy Bharati Vidyapeeth Deemed University

Objective:To determine the association of smoking, alcohol and nonsteroidal anti-inflammatory drugs(NSAIDs) use with presence and virulence of Helicobacter pylori(H. pylori) infection in a representative sample of a random adult population of asymptomatic ***:Non virulent 16S rRNA and virulent cag A and T genes from salivary samples of 854 asymptomatic subjects were determined using polymerase chain reaction. The presence and absence of virulent and non virulent infection was statistically compared with consumption of smoking, alcohol and NSAID ***:The prevalence of infection in male and female subjects was found to be 69.25% and 66.90%, respectively. The prevalence of infection in the population of asymptomaticsubjects with respect to consumption of alcohol was as follows: current(31.22%), former(52.20%) and never(43.58%). The prevalence of infection in the population of asymptomatic subjects withrespect to smoking of cigarettes was as follows: current(88.80%), former(57.14%) and never(33.33%).The prevalence of infection in the subject population consuming NSAIDs and not consuming NSAIDs frequently was found to be 82.75%and 21.16%, respectively. Virulence in male and femalesubjects was found to be 60.00%and 50.00%, respectively. The presence of virulent infection in the population of asymptomatic subjects with respect to consumption of alcohol was as follows:current(28.57%), former(40.15%) and never(50.00%). The prevalence of virulent infection in the population of asymptomatic subjects with respect to smoking of cigarettes was as follows: current(79.32%), former(75.00%) and never(50.00%). The prevalence of virulent infection in the subject population consuming NSAIDs and not consuming NSAIDs frequently was found to be 88.23% and 66.66%, ***:It can be concluded that smoking and NSAIDs consumption are aggravating factors for virulence ofH. pylori and alcohol can inhibitH. pyloriin fection in asymptomatic subjects.

关键词： Smoking Alcohol NSAIDs Helicobacter pylori Cag A Cag T 16S rRNA PCR Agarose gel electrophoresis Virulence Prevalence Infection Asymptomatic