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Evaluation of Antimycobacterial Activity of Higenamine Using Galleria mellonella as an In Vivo Infection Model

Natural Products and Bioprospecting 2018年第1期8卷 63-69页

作者： Paul Erasto Richard Sunguruma Joan J.Munissi Victor Wiketye Charles de Konig Atallah F.Ahmed National Institute for Medical Research P.O.Box 9653Dar Es SalaamTanzania Department of Chemistry University of Dar es SalaamDar Es SalaamTanzania School of Chemistry Witwatersrand UniversityJohannesburgRepublic of South Africa Department of Pharmacognosy College of PharmacyKing Saud UniversityP.O.Box 2457Riyadh 11451Saudi Arabia

The Phytochemical investigation on MeOH extract on the bark of Aristolochia brasiliensis Mart.&Zucc(Aristolochi-aceae)led to the isolation of major compound(1)as light brown grainy *** compound was identified as 1-(4-hydroxybenzyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol(higenamine)on the basis of spectroscopic analysis,including 1D and 2D NMR *** compound was evaluated for its antimycobacterial activity against mycobacterium indicus pranii(MIP),using Galleria mellonella larva as an in vivo infection *** survival of MIP infected larvae after a single dose treatment of 100 mg/kg body weight of higenamine was 80%after 24 *** the compound exhibited a dose dependent activity,as evidenced by the reduction of colony density from 10^(5) to 10^(3) CFU for test concentrations of 50,100,150 and 200 mg/kg body weight *** IC50 value for higenamine was 161.6 mg/kg body weight as calculated from a calibration *** analysis showed that,a complete inhibition of MIP in the *** could be achieved at 334 mg/kg body *** the fact that MIP has been found to be highly resistant against isoniazid(INH)in an in vitro assay model,in this study the microbe was highly susceptible to this standard anti-TB *** isolation of higenamine from the genus Aristolochia and the method used to evaluate its in vivo antimycobacterial activity in *** are herein reported for the first time.

关键词： Aristolochia brasiliensis Galleria mellonella Higenamine Isoniazid mycobacterium indicus pranii Antimycobacterial activity

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