Evaluation of antiprotozoal and antimycobacterial activities of the resin glycosides and the other metabolites of Scrophularia cryptophila

Tasdemir, D., Brun, R., Franzblau, S.G., Sezgin, Y. and Çalıs, I. (2008) Evaluation of antiprotozoal and antimycobacterial activities of the resin glycosides and the other metabolites of Scrophularia cryptophila. Phytomedicine, 15 (3). pp. 209-215. 10.1016/j.phymed.2007.07.032.

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DOI: 10.1016/j.phymed.2007.07.032

Abstract

Resin glycosides are secondary metabolites exclusive to the convolvulaceous plants. In this study, crypthophilic acids A-C (1-3), the first resin glycosides occurring in another family (Scrophulariaceae), and the other constituents of Scrophularia cryptophila were examined for in vitro antiprotozoal and antimycobacterial potentials. Except for crypthophilic acid B (2), all tested compounds exhibited growth-inhibitory effect against Trypanosoma brucei rhodesiense, with l-tryptophan (6) and buddlejasaponin III (7) being the most potent ones (IC(50)'s 4.1 and 9.7 microg/ml). In contrast, the activity towards Trypanosoma cruzi was poor, and only crypthophilic acid C (3), 6 and 7 were trypanocidal at concentrations above 40 microg/ml. With the exception of 2 and 6, all compounds were active against Leishmania donovani. Harpagide (4) and 3 emerged as the best leishmanicidal agents (IC(50)'s 2.0 and 5.8 microg/ml). Only compounds 3, 6 and 7 showed antimalarial activity against Plasmodium falciparum with IC(50) values of 4.2, 16.6 and 22.4 microg/ml. Overall the best and broadest spectrum activity was presented by compounds 3 and 7, as they inhibited all four parasitic protozoa. None of the isolates had significant activity against Mycobacterium tuberculosis (MICs >100 microg/ml) or were toxic towards mammalian (L6) cells. This is the first report of antiprotozoal activity for natural resin glycosides, as well as for harpagide (4), acetylharpagide (5), tryptophan (6) and buddlejasaponin III (7).

Item Type:Article
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry
ID Code:2592
Journal or Publication Title:Phytomedicine
Deposited By:Library Staff
Deposited On:01 Dec 2011 17:50
Last Modified:01 Dec 2011 17:50

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