Identification of compounds from the plant species Alepidea amatymbica active against HIV

As Alepidea amatymbica is commonly used and accepted as medicinal plant in South Africa for various indications, the scientific basis of its anecdotally described, putative anti-HIV properties was investigated. To this aim, we used an accelerated extraction-purification approach; extracts and therein sub-fractions of A. amalymbica were assessed in a cell-based assay targeting the replication of prototypic CXCR4-tropic (NL4-3) or CCR5-tropic (NL-AD87) HIV-1 strains. Sub-fractions of the extracts were generated through semi-preparative high performance liquid chromatography (HPLC) fractionation into triplicates of 96-well microtitre plates; they were then separately subjected to biological analysis and ultra performance liquid chromatography (UPLC) time-of-flight (TOF) analysis. A correlation plot was generated between the biological and chemical data to identify the biologically active compounds in those fractions that showed significant selective anti-HIV activity. The results indicated that rosmarinic acid was present in the wells that showed promising anti-HIV activity in vitro indicating that this compound is at least in part responsible for the antiviral properties of the A. amatymbica extracts. However, compared to standard retroviral inhibitor the anti-HIV activity of the pure compound was found to be only quite moderate. Nevertheless, the accelerated approach described herein increases the efficiency of screens towards identifying drug candidates much earlier in the discovery stage. (C) 2013 SAAB. Published by Elsevier B.V. All rights reserved.