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antitubercular activity of the semi-polar extractives of Uvaria rufa

Asian Pacific Journal of Tropical Medicine 2012年第10期5卷 777-780页

作者： Allan Patrick G Macabeo Florie A Tudla Karsten Krohn Scott G Franzblau Organic Synthesis and Phytochemistry Laboratory Research Center for the Natural SciencesUniversity of Santo TomasEspana Blvd.Manila 1015Philippines Institut fr Organische Chemie Universitat RegensburgUniversitatsstrasse 3193053 RegensburgGermany Institut fr Organische Chemie Universitat PaderbornGermany Institute for Tuberculosis Research College of PharmacyUniversity of Illinois.IL 60085USA

Objective:To investigate the inhibitory activity of the chloroform extract,petroleum ether and chloroform sub-extracts,lead-acetate treated chloroform extract,fractions and secondary metabolites of Uvaria rufa(***) against Mycobacterium tuberculosis(***) H_(37)Rv. Methods:The antituberculosis susceptibility assay was earried out using the colorimetric Microplate Alamar blue assay(MABA).In addition,the cytotoxicity of the most active fraction was evaluated using the VERO cell toxicity ***:The in vitro inhibitory activity against *** H_(37)Rv increased as purification progressed to fractionation(MIC up to 23μg/mL). The chloroform extract and its sub-extracts showed moderate toxicity while the most active fraction from chloroform sub-extract exhibited no cytotoxicity against VERO ***, the lead acetate-treated crude chloroform extract and its fractions showed complete inhibitions (100%) with MIC values up to 8μg/*** screening of the most active fraction showed,in general,the presence of terpenoids,steroids and phenolic *** of the antimycobacterial activity of known secondary metabolites isolated showed no promising inhibitory activity against the test ***:The present results demonstrate the potential of *** as a phytomedicinal source of compounds that may exhibit promising antituberculosis *** addition,elimination of polar pigments revealed enhanced inhibition against *** H_(37)*** several compounds known for this plant did not show antimycobacterial activity,the obtained results are considered sufficient reason for further study to isolate the metabolites from *** responsible for the antitubercular activity.

关键词： Uvaria rufa antitubercular Mycobacterium tuberculosis H_(37)Rv

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Effect of antitubercular treatment on the pregnancy outcomes and prognoses of patients with genital tuberculosis

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Frontiers of Medicine 2019年第1期13卷 121-125页

作者： Jing Yue Bo Zhang Mingyue Wang Junning Yao Yifan Zhou Ding Ma Lei Jin Reproductive Medicine Center Tongji HospitalTongji Medical CollegeHuazhong University of Science and TechnologyWuhan 430030China Department of Gynecology and Obstetrics Tongji HospitalTongji Medical CollegeHuazhong University of Science and TechnologyWuhan 430030China

This retrospective study aims to demonstrate the effect of antitubercular treatment (ATT) on the pregnancy outcomes and prognoses of patients with genital tuberculosis (GTB) who had received laparoscopy and/ or hysteroscopy. This study included 78 patients with infertility and who were diagnosed with GTB through laparoscopy and/or hysteroscopy over the period of November 2005 to October 2015? The recruited patients were divided into ATT and nonATT groups on the basis of ATT duration. The GTB recurrence rates, menstrual patterns, and pregnancy outcomes of the patients were determined at follow-up. Among the 78 patients, 46 received ATT and 32 did not receive ATT. The menstrual volumes of patients in the ATT group significantly decreased relative to those of patients in the nonATT group. GTB did not recur among all patients regardless of treatment. A total of 11 pregnancies (36.7%) in the ATT group and 19 pregnancies (63.3%) in the nonATT group were observed. Pregnancy rates significantly differed (P = 0.002) between the two *** may decrease the menstrual volume and pregnancy rates of patients who were diagnosed with GTB through laparoscopy and/or hysteroscopy. In addition, ATT did not improve the prognosis of patients with chronic GTB.

关键词： antitubercular treatment pregnancy prognosis genital tuberculosis

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Synthesis and biological evaluation of new 13-n-nonylprotoberberine derivatives as antitubercular agents

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Acta Pharmaceutica Sinica B 2013年第1期3卷 38-45页

作者： Yinghong Li Yanxin Liu Yanxiang Wang Sheng Tang Danqing Song Institute of Medicinal Biotechnology Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China

Tuberculosis is a serious threat to public health throughout the world.A series of new l3-n-nonylprotoberberine derivatives was designed,synthesized and evaluated for anti-mycobacterial activity against Mycobacterium tuberculosis strain H_(37)*** compounds(2,11a-c,11g,13d,15c)exhibited excellent anti-tubercular activity with an MIC below 1.0μg/***,compound 13d showed potential antibacterial effect against both drug-susceptible and multidrug-resistant(MDR)*** with MIC ranges of 0.0625-1.0μg/*** results suggest a mode of action different from that of the current anti-mycobacterial drugs rifampicin and ***,compound 13d is an attractive lead compound for the development of new antitubercular agents.

关键词： 13-n-nonylberberine antitubercular Structure-activity rela-tionship MIC Drug-resistant

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Evaluation of antihepatotoxic potential of Solanum xanthocarpum fruit extract against antitubercular drugs induced hepatopathy in experimental rodents

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Asian Pacific Journal of Tropical Biomedicine 2012年第6期2卷 454-460页

作者： Talib Hussain Ramesh K Gupta Sweety K Mohd Sajid Khan Md Sarfaraj Hussain Md Arif Arshad Hussain Md Faiyazuddin Chandana Venkateswara Rao Pharmacognosy and Ethnopharmacology Division National Botanical Research Institute Department of Pharmacology and Toxicology Faculty of Pharmacy Integral University Department of Pharmacology Royal College of Pharmacy and Health Sciences Department of Biotechnology Integral University

Objective:To assess the hepatoprotective effect of Solanum xanthocarpum(S. xanthocarpum) fruit extract against antitubercular drug-induced liver toxicity in experimental ***:Ethanolic(50%) fruit extract ofS. xanthocarpum(100, 200 and 400 mg/kg bw) was administered daily for 35 days in experimental animals. Liver toxicity was induced by combination of three antitubercular drugs [isoniazid(I) 7.5 mg/kg, rifampicin(R) 10 mg/kg and pyrazinamide(P) 35 mg/kg] given orally as suspension for 35 days in rats. The hepatoprotective activity was assessed using various biochemical parameters like aspartate aminotransferase(AST), alanine aminotransferase(ALT), alkaline phosphatise(ALP), total bilirubin(TBL), albumin(ALB), total protein(TP), lactate dehydroginase(LDH), and serum cholesterol(CHL). Meanwhile,in vivoantioxidant activities as lipid peroxidation(LPO), reduced glutathione(GSH), superoxide dismutase(SOD) and catalase(CAT) were measured in rat liver homogenate. The biochemical observations were supplemented by histopathological ***:The results demonstrated that treatment ***(P<0.05-P<0.001) and dose-dependently prevented drug induced increase in serum levels of hepatic enzymes. Furthermore,S. xanthocarpumsignificantly(up toP<0.001) reduced the LPO in the liver tissue and restored activities of defence antioxidant enzymes GSH, SOD and CAT towards normal levels. Histopathology of the liver tissue showed that S. xanthocarpumattenuated the hepatocellular necrosis and led to reduction in inflammatory cells ***:The results of this study strongly indicate the protective effect of S. xanthocarpumagainst liver injury which may be attributed to its hepatoprotective activity, and thereby scientifically support its traditional use.

关键词： Solanum xanthocarpum Rifampicin Isoniazid Pyrazinamide Antioxidant Antihepatotoxicity Hepatoprotective effect antitubercular drug Liver toxicity Liver injury Biochemical parameter Histopathology

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Design, Synthesis and Biological Evaluation of Novel antitubercular Agents by Combining Pyrazoline and Benzoxazole Pharmacophores

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International Journal of Organic Chemistry 2016年第3期6卷 157-176页

作者： Hemal M. Soni Popatbhai K. Patel Mahesh T. Chhabria Ashish K. Patel Dharmraj N. Rana Pathik S. Brahmkshatriya M/S Piramal Enterprises Ltd. Piramal Discovery Solutions Plot No. 18 Pharmaceutical Special Economic Zone Village Matoda Ta. Sanand Ahmedabad India M.G. Science Institute Opp. Gujarat University Navrangpura Ahmedabad India Department of Pharmaceutical Chemistry L. M. College of Pharmacy Navrangpura Ahmedabad India Oxygen Healthcare Res. Pvt. Ltd. Plot No. 35 Panchratna Industrial Estate Near IBP Laxminarayan Petrol Pump Changodar Ahmedabad India

Various recent reports on Tuberculosis have alarmed an increase in the patient class and subsequent death rates across the globe. Over and above the spread of more dangerous and fatal forms of tuberculosis like MDR-TB i.e. multiple-drug resistance tuberculosis, XDR-TB i.e. extensively-drug resistance tuberculosis & TDR-TB i.e. total-drug resistance tuberculosis has forwarded an urgent need to discover novel antitubercular agents. The current work is aimed at combining two previously well-known pharmacophores (pyrazoline and benzoxazole nucleus) in order to design and synthesize a series of novel benzoxazole-based pyrazoline derivatives. The synthesized target compounds were structurally confirmed by LCMS, 1H-NMR and 13C-NMR analysis. The target compounds were In vitro evaluated against M. tuberculosis H37Rv strain, multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB) strains. The In vitro screening results depicted that majority of the target compounds displayed potent activity with MIC in a range of ~0.8 to 6.25 μg/mL. Many compounds were found to be more potent than isoniazid against MDR-TB with MIC value 3.12 μg/mL and XDR-TB with MIC value 12.5 μg/mL. Cytotoxicity assay of these active compounds on VERO cell lines also displayed good selectivity index.

关键词： antitubercular Benzoxazole Pyrazoline Pharmacophore Microplate Alamar Blue Assay

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Synthesis and Evaluation of 2-Amino-4H-Pyran-3-Carbonitrile Derivatives as antitubercular Agents

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Open Journal of Medicinal Chemistry 2013年第4期3卷 128-135页

作者： Chunxia Chen Minghui Lu Zhihui Liu Junting Wan Zhengchao Tu Tianyu Zhang Ming Yan Guangzhou Chest Hospital Guangzhou China Institute of Drug Synthesis and Pharmaceutical Process School of Pharmaceutical Sciences Sun Yat-sen University Guangzhou China State Key Laboratory of Respiratory Diseases Guangzhou Institutes of Biomedicine and Health Chinese Academy of Science Guangzhou China

A series of 2-amino-4H-pyran-3-carbonitrile derivatives were designed and synthesized. Their antitubercular activities were evaluated against autoluminescent M. tuberculosis H37Ra and standard strain M. tuberculosis H37Rv. No obvious antitubercular activities could be observed (MIC > 10 ug/mL). The results are in sharp contrast with the previously reported data.

关键词： 2-Amino-4H-Pyran-3-Carbonitrile Synthesis antitubercular Activity

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Synthesis of New Mannich Products Bearing Quinoline Nucleous Using Reusable Ionic Liquid and antitubercular Evaluation

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Green and Sustainable Chemistry 2015年第4期5卷 137-144页

作者： Hitendra M. Patel Department of Chemistry Sardar Patel University Vallabh Vidyanagar India

A series of Mannich products bearing quinoline nucleus was synthesized, characterized, and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. The results showed that compounds 4b, and 4d found most active with percentage inhibition of 95, and 96, respectively, at minimum inhibitory concentration (MIC) of >6.25 μg/mL, among the synthesized compounds. Whereas, compounds 4a, 4c, 4e, and 4f exhibited considerable antitubercular activity with percentage inhibition of 71, 79, 55, and 68, respectively, at MIC of >6.25 μg/mL. The structures of synthesized compounds were elucidated by various spectroscopic tools like IR, 1H NMR, 13C NMR, mass and elemental analysis.

关键词： antitubercular Activity Green Synthesi Mannich Products Mycobacterium tuberculosis Quinoline Spectroscopic Tools

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Hepatoprotective properties of oleanolic and ursolic acids in anti-tubercular drug-induced liver damage

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Asian Pacific Journal of Tropical Medicine 2016年第7期9卷 625-632页

作者： Gabriel A.Gutiérrez-Rebolledo Georgina A.Siordia-Reyes Mariana Meckes-Fischer Adelina Jiménez-Arellanes Unidad de Investigación Médica en Farmacología (UIMF) UMAE Hospital de EspecialidadesCentro Médico Nacional-Siglo XXI (CMN-SXXI)Instituto Mexicano del Seguro Social (IMSS) Servicio de Patología UMAE Hospital de PediatríaCMN-SXXIIMSS Centro de Diagnóstico en Metabolismo Energético y Medicina Mitocondrial A.C.

Objective:To estimate to what extent the mixture of ursolic acid and oleanolic acid,in addition to the antitubercular standard regime,affects the hepatotoxicity ***:Liver injury was induced in male BALB/c mice by administering,per os and daily for 11 weeks,a combination of anti-Tubercular(anti-TB) agents Rifampicin(10 mg/kg),Isoniazid(10 mg/kg),and Pyrazinamide(30 mg/kg).The ursolic acid and oleanolic acid mixture at doses of 100 or 200 μg/mouse/day was subcutaneously injected throughout the entire study period(11 weeks).Biochemical and hematological analysis was supplemented by liver histological ***:Animals treated with the mixture of triterpenic acids exhibited significantly decreased aspartate transaminase and alanine aminotransferase levels and amelioration of the histopathological alterations produced by the anti-TB ***:The triterpene mixture is able to prevent the steatosis induced by the anti-TB drugs.

关键词： Ursolic acid Oleanolic acid Hepatoprotector effect antitubercular drugs Triterpenes

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Synthesis and Biological Study of Some 4-oxo-Thiazolidine Derivatives of 2-Aminothiazole

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Chinese Journal of Chemistry 2011年第5期29卷 1001-1010页

作者： Samadhiya Pushkal Sharma Ritu Srivastava Santosh K. Srivastava Savitri D. Synthetic Organic Chemistry Laboratory Department of Chemistry Dr. H.S. Gour University (A Central University) Sagar M.P. 470003 India

Conventional and microwave assisted synthesis of new series of N-[2-{2-（substituted phenyl）-4-oxo- 5-（substituted benzylidene）-1,3-thiazolidine}-iminoethyl]-2-aminothiazole 5a-Sin have been developed. The cycloaddition reaction of thioglycolic acid with N-{2-（substituted benzylidenehydrazino）-ethyl}-2-aminothiazole 3a--3m in the presence of anhydrous ZnC12 afforded new heterocyclic compounds N-[2-{2-（substituted phenyl）- 4-oxo-l,3-thiazolidine}-iminoethyl]-2-aminothiazole 4a---4m. The later product on treatment with several selected substituted aromatic aldehydes in the presence of C2HsONa undergoes Knoevenagel reaction to yield 5a--Sin. The structures of compounds 1, 2, 3a--3m, 4a---4m and 5a--Sm were confirmed by IR, IH NMR, 13C NMR, FAB-Mass and chemical analysis. All above compounds were screened for their antimicrobial activities against some selected bacteria and fungi and antituberculosis study against M. tuberculosis.

关键词： conventional microwave synthesis 2-aminothiazole 4-oxo-thiazolidine antimicrobial antitubercular

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Ascorbic acid ameliorates isoniazid-rifampicin-induced hepatocellular damage in rats

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iLIVER 2022年第1期1卷 72-77页

作者： Shubham Patel Aman Chaturvedi Nazneen Dubey Abhishek Shrivastava Aditya Ganeshpurkar Shri Ram Institute of Technology-Pharmacy JabalpurIndia

Background:Phyto-constituents are widely recognized for hepatoprotective *** acid is extensively studied for the radical scavenging *** objective of the present study was to evaluate the hepatoprotective effect of ascorbic acid against isoniazid and rifampicin-induced liver damage in ***:Wistar rats were used in the present ***-cellular damage was produced by the administration of isoniazid(100 mg/kg)and rifampicin(100 mg/kg)for 21 *** acid was administered in the dose of 50,100,and 200 mg/kg body *** the end of the study,blood was collected and biochemical studies were performed to determine antioxidant ***:Ascorbic acid administration(50,100,and 200 mg/kg body weight)caused restoration of serum glutamic oxaloacetic transaminase,serum glutamic-pyruvic transaminase,and serum alkaline *** level of superoxide dismutase and catalase were also restored due to the administration of ascorbic *** was a decrement in the expression of tumor necrosis factor-α,interleukin-1β,interleukin-6,malondialdehyde and nitric ***:The outcome of the study established ascorbic acid as a notable hepatoprotective *** radical scavenging and cytokine suppression effect is the possible mechanism associated with the hepatoprotective effect of ascorbic acid.

关键词： Liver Toxicity antitubercular Peroxidation Cytokines Ascorbic acid

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