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Sci. Pharm. 2011, 79(1), 137-144; doi:10.3797/scipharm.1012-10

Antitrypanosomal and Cytotoxic Activities of 22-Hydroxyclerosterol, a New Sterol from Allexis cauliflora (Violaceae)

1
Laboratory of Medicinal Chemistry & Pharmacognosy, Department of Organic Chemistry, Faculty of Sciences, University of Yaoundé I, Box 812 Yaoundé, Cameroon
2
UMR 5068, LSPCMIB, Université Paul Sabatier, Bât. II R1, 118 Route de Narbonne, 31062 Toulouse, Cedex 4, France
3
Research Unit for Tropical Diseases, de Duve Institute, TROP 74.39, Avenue Hippocrate 74, B-1200 Brussels, Belgium
4
Max Planck Institute for Chemical Ecology, Beutenberg Campus, Hans-Knöll-Str. 8, D-07745 Jena, Germany
*
Author to whom correspondence should be addressed.
Received: 12 December 2010 / Accepted: 3 February 2011 / Published: 7 February 2011
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Abstract

In the search for new antiparasitic natural compounds from the medicinal plants from Cameroon, the new 22-hydroxyclerosterol, established as such on the basis of detailed chemical and spectroscopic analysis, was isolated from the hexane extract of the stem bark of Allexis cauliflora together with the known clerosterol. 22-Hydroxyclerosterol inhibited the growth of Trypanosoma brucei brucei cells with an ED50 value of 1.56 μM. The compound was also established as an uncompetitive inhibitor of the glycolytic enzyme PGI of T. brucei (Ki’= 3 ± 1 μM), an uncompetitive inhibitor of mammalian rabbit muscles’ enzyme PyK (Ki’= 26 ± 3 μM) and a mixed inhibitor of PyK of Leishmania mexicana (Ki’= 65 ± 10 μM; Ki= 24 ± 5 μM).
Keywords: Clerosterol; Enzyme inhibitor; Trypanocide; Trypanosoma brucei; Stigmastane sterols; Cytotoxicity; NMR; Structure elucidation; Natural products Clerosterol; Enzyme inhibitor; Trypanocide; Trypanosoma brucei; Stigmastane sterols; Cytotoxicity; NMR; Structure elucidation; Natural products
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

NGANSO, Y.O.D.; NGANTCHOU, I.E.W.; NKWENOUA, E.; NYASSE, B.; DENIER, C.; HANNERT, V.; SCHNEIDER, B. Antitrypanosomal and Cytotoxic Activities of 22-Hydroxyclerosterol, a New Sterol from Allexis cauliflora (Violaceae). Sci. Pharm. 2011, 79, 137-144.

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