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来自波多黎各萨波特卡(豆科)根部的两种杀锥虫二肽。

Two trypanocidal dipeptides from the roots of Zapoteca portoricensis (Fabaceae).

作者信息

Nwodo Ngozi Justina, Okoye Festus Basden C, Lai Daowan, Debbab Abdessamad, Brun Reto, Proksch Peter

机构信息

Department of Pharmaceutical and Medicinal Chemistry, University of Nigeria, 410001 Nsukka, Enugu State, Nigeria.

Department of Pharmaceutical and Medicinal Chemistry, Nnamdi Azikiwe University, 420281 Awka, Anambra State, Nigeria.

出版信息

Molecules. 2014 Apr 25;19(5):5470-7. doi: 10.3390/molecules19055470.

Abstract

Zapoteca portoricensis (Jacq) HM Hernández is used with remarkable efficacy in ethnomedicinal management of tonsillitis in the Eastern part of Nigeria. Previous pharmacological studies have validated the antiinflammatory and antimicrobial activities of the crude extract. In this study, two dipeptides, saropeptate (aurantiamide acetate) and anabellamide, were isolated from the methanol root extract of Zapoteca portoricensis and their chemical structures deduced by one dimensional and two dimensional NMR and mass spectrometry. These compounds were isolated for the first time from this plant, and no report has been found on their previous isolation from the genus Zapoteca. Evaluation of their trypanocidal activity showed that compound 1 exhibited potent activity against Trypanosoma brucei rhodesiense with an IC50 value of 3.63 μM and selectivity index of 25.3.

摘要

波多黎各萨波特卡(Zapoteca portoricensis (Jacq) HM Hernández)在尼日利亚东部用于扁桃体炎的民族药用管理,疗效显著。先前的药理学研究已证实该粗提物具有抗炎和抗菌活性。在本研究中,从波多黎各萨波特卡的甲醇根提取物中分离出两种二肽,即肌肽(aurantiamide acetate)和anabellamide,并通过一维和二维核磁共振及质谱推断其化学结构。这些化合物首次从该植物中分离得到,且未发现之前从萨波特卡属分离出它们的报道。对其杀锥虫活性的评估表明,化合物1对布氏罗得西亚锥虫具有强效活性,IC50值为3.63 μM,选择性指数为25.3。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b2e8/6270954/1fc0e864a4e1/molecules-19-05470-g001.jpg

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