Tubulin polymerization-stimulating activity of Ganoderma triterpenoids

This study was conducted to evaluate the effect ofGanoderma triterpenoids on tubulin polymerization. A total of twenty-four compounds were investigated using an in vitro tubulin polymerization assay. Results showed that most of the studied triterpenoids exhibited microtuble-stabilizing activity to different degrees. Among the investigated compounds, ganoderic acid T-Q, ganoderiol F, ganoderic acid S, ganodermanontriol and ganoderic acid TR were found to have the highest activities. A structure –activity relationship (SAR) analysis was performed. Extensive investigation of the SAR suggests the favorable structural features for the tubulin polymerization-stimulating activity of lanostane triterpenes. These findings would be helpful for further studies on the potential mechanisms of the an ticancer activity ofGanoderma triterpenoids and give some indications on the design of tubulin-targeting anticancer agents.
Source: Journal of Natural Medicines - Category: Drugs & Pharmacology Source Type: research

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