Antitrypanosomal sesquiterpene lactones from Saussurea costus |
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| Authors: | Julianti Tasqiah Hata Yoshie Zimmermann Stefanie Kaiser Marcel Hamburger Matthias Adams Michael |
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| Affiliation: | aDivision of Pharmaceutical Biology, University of Basel, CH-4056 Basel, Switzerland;bDepartment of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, CH-4002 Basel, Switzerland;cFaculty of Pharmacy, Pancasila University, 12640 Jakarta, Indonesia;dDepartment of Pharmacy, National University of Colombia, Carrera 30 45-03, Bogotá, Colombia;eUniversity of Basel, CH-4051 Basel, Switzerland |
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| Abstract: | 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), α-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 μM. Cytotoxic IC50s were from 1.6 to 19 μM, and selectivity indices from 0.5 to 6.5. |
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| Keywords: | Saussurea costus Asteraceae Sesquiterpene lactones Trypanosoma brucei rhodesiense HPLC-based activity profiling |
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