title: Evaluation of antiprotozoal and antimycobacterial activities of the resin glycosides and the other metabolites of Scrophularia cryptophila.
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).
authors.affiliation: Centre for Pharmacognosy and Phytotherapy, School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, UK. deniz.tasdemir@pharmacy.ac.uk
authors.forename: Deniz
authors.initials: D
authors.lastname: Tasdemir
authors.forename: Reto
authors.initials: R
authors.lastname: Brun
authors.forename: Scott G
authors.initials: SG
authors.lastname: Franzblau
authors.forename: Yükselen
authors.initials: Y
authors.lastname: Sezgin
authors.forename: Ihsan
authors.initials: I
authors.lastname: Calis
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000302:isolation & purification / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000302:isolation & purification / Q000494:pharmacology*; D002460:Cell Line; D056890:Eukaryota / Q000187:drug effects*; D006027:Glycosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D057889:Iridoid Glycosides; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D035261:Plant Components, Aerial / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D011714:Pyrans; D051381:Rats; D012503:Saponins; D032266:Scrophularia / Q000737:chemistry*; D014364:Tryptophan
chemical_list: D000900:Anti-Bacterial Agents; D000981:Antiprotozoal Agents; D006027:Glycosides; D057889:Iridoid Glycosides; D010936:Plant Extracts; D011714:Pyrans; D012503:Saponins; C104869:buddlejasaponin; C517584:crypthophilic acid A; C517585:crypthophilic acid B; C517586:crypthophilic acid C; D014364:Tryptophan; C033250:harpagide