Antitrypanosomal sesquiterpene lactones from Saussurea costus

被引：67

作者：

Julianti, Tasqiah ^{[3
]}

Hata, Yoshie ^{[4
]}

Zimmermann, Stefanie ^{[2
]}

Kaiser, Marcel ^{[2
,5
]}

Hamburger, Matthias

Adams, Michael ^{[1
]}

机构：

[1] Univ Basel, Inst Pharmaceut Sci, Div Pharmaceut Biol, CH-4056 Basel, Switzerland

[2] Swiss Trop & Publ Hlth Inst, Dept Med Parasitol & Infect Biol, CH-4002 Basel, Switzerland

[3] Pancasila Univ, Fac Pharm, Jakarta 12640, Indonesia

[4] Univ Nacl Colombia, Dept Pharm, Bogota, Colombia

[5] Univ Basel, CH-4051 Basel, Switzerland

来源：

FITOTERAPIA | 2011年 / 82卷 / 07期

关键词：

Saussurea costus; Asteraceae; Sesquiterpene lactones; Trypanosoma brucei rhodesiense; HPLC-based activity profiling; ANTIPROTOZOAL ACTIVITY; TRYPANOSOMA-BRUCEI; TUMOR INHIBITORS; DEHYDROCOSTUSLACTONE; RHODESIENSE; COSTUNOLIDE; CRUZI;

D O I：

10.1016/j.fitote.2011.05.010

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

In the course of a larger screen of 1800 plant and fungal extracts, the ethyl acetate extract of Saussurea costus roots potently inhibited the growth of Trypanosoma brucei rhodesiense. Subsequent HPLC based activity profiling led to the identification of the sesquiterpene lactones arbusculin B (1), alpha-cyclocostunolide (2), costunolide (3), and dehydrocostuslactone (4). They were tested for in vitro antitrypanosomal activities and cytotoxicity alongside the structurally related sesquiterpene lactones parthenolide (5), zaluzanin D (6), and eupatoriopicrin (7), and had IC50S between 0.8 and 22 mu M. Cytotoxic IC50S were from 1.6 to 19 mu m, and selectivity indices from 0.5 to 6.5. (C) 2011 Elsevier B.V. All rights reserved.

引用

页码：955 / 959

页数：5

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