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基于高效液相色谱的 和 中抗原生动物化合物的活性分析

HPLC-Based Activity Profiling for Antiprotozoal Compounds in and .

作者信息

Mahmoud Abdelhalim Babiker, Danton Ombeline, Kaiser Marcel, Khalid Sami, Hamburger Matthias, Mäser Pascal

机构信息

Parasite Chemotherapy Unit, Swiss Tropical and Public Health Institute, Basel, Switzerland.

Faculty of Science, University of Basel, Basel, Switzerland.

出版信息

Front Pharmacol. 2020 Aug 14;11:1246. doi: 10.3389/fphar.2020.01246. eCollection 2020.

Abstract

In a screening of Sudanese medicinal plants for antiprotozoal activity, the chloroform fractions obtained by liquid-liquid partitioning from ethanolic extracts of fruits of var. and stems of Roth ex Schult. exhibited activity against axenically grown amastigotes. This antileishmanial activity was localized by HPLC-based activity profiling. Targeted preparative isolation afforded flavonoids -, 3-methoxy-4-hydroxybenzoic acid (), and benzyltetrahydroisoquinoline alkaloids laudanine () and laudanosine () from , and pinoresinol (), isorhamnetin (), (-)-pseudosemiglabrin (), and kaempferol () from The antiprotozoal activity of - against (axenic and intracellular amastigotes), (bloodstream forms), and (erythrocytic stages), and the cytotoxicity in L6 murine myoblast cells were determined . Quercetin-3,7-dimethylether () showed the highest activity against axenic (IC 4.5 µM; selectivity index [SI], 12.3), (IC 7.3 µM; SI, 7.6), and (IC, 2.4 µM; SI, 23.2). The congener ayanin () exhibited moderate antileishmanial (IC, 8.2 µM; SI, 12.2), antiplasmodial (IC, 7.8 µM; SI, 12.9), and antitrypanosomal activity (IC, 11.2 µM; SI, 8.9). None of the compounds showed notable activity against the intramacrophage form of .

摘要

在对苏丹药用植物进行抗原生动物活性筛选时,通过液-液分配从var.果实和Roth ex Schult.茎的乙醇提取物中获得的氯仿馏分,对无菌培养的无鞭毛体表现出活性。这种抗利什曼原虫活性通过基于高效液相色谱的活性分析进行定位。靶向制备分离从[植物名称未给出]中得到了黄酮类化合物-、3-甲氧基-4-羟基苯甲酸()、苄基四氢异喹啉生物碱劳丹宁()和劳丹诺辛(),从[植物名称未给出]中得到了松脂醇()、异鼠李素()、(-)-假半光苏木精()和山奈酚()。测定了-对[寄生虫名称未给出](无菌和细胞内无鞭毛体)、[寄生虫名称未给出](血流形式)和[寄生虫名称未给出](红细胞阶段)的抗原生动物活性以及在L6小鼠成肌细胞中的细胞毒性。槲皮素-3,7-二甲醚()对无菌的[寄生虫名称未给出](IC 4.5 μM;选择性指数[SI],12.3)、[寄生虫名称未给出](IC 7.3 μM;SI,7.6)和[寄生虫名称未给出](IC,2.4 μM;SI,23.2)表现出最高活性。同系物阿亚宁()表现出中等的抗利什曼原虫活性(IC,8.2 μM;SI,12.2)、抗疟活性(IC,7.8 μM;SI,12.9)和抗锥虫活性(IC,11.2 μM;SI,8.9)。这些化合物均未对[寄生虫名称未给出]的巨噬细胞内形式表现出显著活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4fba/7456963/6cfa2ea7977d/fphar-11-01246-g001.jpg

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