Discovery and synthesis of novel beesioside I derivatives with potent anti-HIV activity.

ABSTRACT: In this study, 12 known cycloartane triterpenoids (1-12) with four different skeletons isolated from the roots of Souliea vaginata were screened for the first time for in vitro anti-HIV activity using AZT as a standard. Among the compounds, beesioside I (1) showed the highest potency against HIV-1_NL4-3 with an EC₅₀ value of 2.32 μM (CC₅₀ > 40 μM). Preliminary structure-activity relationship (SAR) studies on 1 indicated that simple modification of its aglycone (13) could significantly influence the antiviral activity. Particularly, the introduction of an acyl group at the C-3 position of 13 led to significant improvement in both anti-HIV potency and selectivity index. Among all synthetically modified derivatives, compound 13g was the most potent compound wit

SUBMITTER: Wu H 

PROVIDER: S-EPMC6464118 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature