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New Antiprotozoal Sesquiterpene Derivatives From Dorema Glabrum Fisch & C.A.Mey Publisher Pubmed



Delnavazi MR1 ; Ebrahimi SN2 ; Hadjiakhoondi A1 ; Yassa N1
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Authors Affiliations
  1. 1. Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Department of Phytochemistry, Medicinal Plants and Drugs Research Institute, Shahid Beheshti University, G.C, Evin, Tehran, Iran

Source: Fitoterapia Published:2023


Abstract

Seven undescribed sesquiterpene derivatives, Azerins A-G (3–6, 8, 14 and 15), three known sesquiterpene phenols, kopetdaghin A (1), kopetdaghin B (2) and latisectin (7), together with five known sesquiterpene coumarins (9–13), were isolated from the roots of Dorema glabrum. The structures were elucidated by comprehensive 1D- and 2D-NMR spectral analysis as well as HR-ESI-MS. Compounds were assessed for their in vitro antiprotozoal activity against Trypanosoma brucei rhodesiense, T. cruzi, Leishmania donovani, and Plasmodium falciparum. Cytotoxic potentials of the compounds were also tested on L6 rat skeletal myoblasts. Azerin G (15) showed a potent preferential growth inhibitory activity against T. b. rhodesiense with IC50 value of 0.01 μM and selectivity index of 329. Compounds 1, 4, 7 and 8 were also found as the most active compounds with selective growth inhibitory effects toward P. falciparum with selectivity indices ranging from 11.6 to 16.7 (IC50: 1.8–24.6 μM). © 2023 Elsevier B.V.
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