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Antiprotozoal activity-based profiling of a dichloromethane extract from anthemis nobilis flowers

De Mieri, Maria and Monteleone, Giannicola and Ismajili, Isidor and Kaiser, Marcel and Hamburger, Matthias. (2017) Antiprotozoal activity-based profiling of a dichloromethane extract from anthemis nobilis flowers. Journal of natural products, 80 (2). pp. 459-470.

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Official URL: http://edoc.unibas.ch/54726/

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Abstract

A dichlomethane extract of Anthemis nobilis flower cones showed promising in vitro antiprotozoal activity against Trypanosoma brucei rhodesiense and Leishmania donovani, with IC50 values of 1.43 ± 0.50 and 1.40 ± 0.07 μg/mL, respectively. A comprehensive profiling of the most active fractions afforded 19 sesquiterpene lactones, including 15 germacranolides, two seco-sesquiterpenes, one guaianolide sesquiterpene lactone, and one cadinane acid. Of these, 13 compounds were found to be new natural products. The compounds were characterized by extensive spectroscopic data analysis (1D and 2D NMR, HRMS, circular dichroism) and computational methods, and their in vitro antiprotozoal activity was evaluated. The furanoheliangolide derivative 15 showed high potency and selectivity in vitro against T. b. rhodesiense bloodstream forms (IC50 0.08 ± 0.01 μM; SI 63). In silico calculations were consistent with the drug-like properties of 15.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Kaiser, Marcel
Item Type:Article, refereed
Publisher:American Society of Pharmacognosy
ISSN:0163-3864
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:23 May 2017 09:31
Deposited On:23 May 2017 09:31

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