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

作　　者：Paul Erasto Richard Sunguruma Joan J.Munissi Victor Wiketye Charles de Konig Atallah F.Ahmed 

机构地区：[1]National Institute for Medical Research,P.O.Box 9653,Dar Es Salaam,Tanzania [2]Department of Chemistry,University of Dar es Salaam,Dar Es Salaam,Tanzania [3]School of Chemistry,Witwatersrand University,Johannesburg,Republic of South Africa [4]Department of Pharmacognosy,College of Pharmacy,King Saud University,P.O.Box 2457,Riyadh 11451,Saudi Arabia

出　　处：《Natural Products and Bioprospecting》2018年第1期63-69,共7页应用天然产物（英文）

基　　金：supported by the International Foundation for Science(IFS)Grant Number J/4894-2.

摘　　要：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 crystals.The 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 spectroscopy.The compound was evaluated for its antimycobacterial activity against Mycobacterium indicus pranii(MIP),using Galleria mellonella larva as an in vivo infection model.The survival of MIP infected larvae after a single dose treatment of 100 mg/kg body weight of higenamine was 80%after 24 h.Quantitatively 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 respectively.The IC50 value for higenamine was 161.6 mg/kg body weight as calculated from a calibration curve.Further analysis showed that,a complete inhibition of MIP in the G.mellonella could be achieved at 334 mg/kg body weight.Despite 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 drug.The isolation of higenamine from the genus Aristolochia and the method used to evaluate its in vivo antimycobacterial activity in G.mellonella are herein reported for the first time.

关 键 词：Aristolochia brasiliensis Galleria mellonella HIGENAMINE ISONIAZID Mycobacterium indicus pranii Antimycobacterial activity 

分 类 号：O62[理学—有机化学]