Author/Authors :
Ayatollahi, Abdul Majid Phytochemistry Research Center and School of Pharmacy - Shahid Beheshti University of Medical Sciences, Tehran , Zarei, Mohammad Phytochemistry Research Center and School of Pharmacy - Shahid Beheshti University of Medical Sciences, Tehran , Memarnejadian, Arash Department of hepatitis and AIDS - Institute Pasture of Iran, Tehran , Ghanadian, Mustafa Department of Pharmacognosy, Isfahan Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan , Heydarian Moghadam, Mohammad Department of Audiology - school of Rehabilitation - Shahid Beheshti University of Medical Sciences, Tehran , Kobarfard, Farzad Department of Medicinal chemistry - School of Pharmacy - Shahid Beheshti University of Medical Sciences, Tehran
Abstract :
Phytochemical investigation of the aerial parts of Euphorbia erythradenia Bioss.
(Euphorbiaceae), one of Iranian endemic Euphorbias, with particular attention to triterpene
constituents, using methanol solvent extraction was carried out. Five known triterpenes,
including four cycloartanes and oleanolic acid, were isolated for the first time and identified
using NMR and spectrometric Mass techniques. Anti HIV activity of the isolated triterpenes and
ingenoid diterpenes was evaluated using single cycle replicable HIV-1 (SCR HIV-1) virions.
Molecular features of the most active compound (IC50 = 0.008 μM, CC50 = 3.264 μM, TI =
380.64), which showed higher therapeutic index than nevirapine, was assessed using molecular
docking. Docking studies demonstrated three hydrogen bonds between HIV-1 virion protease
active site and this compound with a distance less than 3 A° which can be responsible for the
observed anti HIV-1 activity.
Keywords :
Euphorbia erythradenia , triterpene , NMR , anti HIV , docking
