What question did this study set out to answer?

The aim is to evaluate the cytotoxicity of bisabolane derivatives on tumor cell lines while maintaining selectivity for healthy cells.

January 1, 1993

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Key Points

The aim is to evaluate the cytotoxicity of bisabolane derivatives on tumor cell lines while maintaining selectivity for healthy cells.
Isolated brasilamide E from Paraconiothyrium brasiliense on solid substrates.
Designed and synthesized 27 derivatives of brasilamide E.
Assessed cytotoxicity against six tumor cell lines and NIH3T3 cells.
Compound 12b demonstrated remarkable potency against MCF-7, HeLa, and HO8910 cells with IC50 values of 0.13-0.25 μM.
Brasilamide E showed IC50 values of 8.47-18.00 μM against MCF-7 cells.
Both brasilamide E and compound 12b were non-toxic to NIH3T3 cells.

Abstract

Brasilamide E (1) is a bisabolane sesquiterpenoid isolated from the solid-substrate fermentation cultures of a plant endophytic fungus Paraconiothyrium brasiliense. The compound specifically inhibited proliferation of the MCF-7 cells, but did not show cytotoxicity towards the negative controls HaCaT and NIH3T3 cells (IC50>50 μM). To improve its potency while maintain selectivity, a total of 27 derivatives of 1 were designed, synthesized, and evaluated for in vitro cytotoxicity against six tumor cell lines and the negative control NIH3T3 cells. Among these compounds, compound 12b showed significantly improved potency against the MCF-7, HeLa, and HO8910 cells with IC50 values of 0.13-0.25 μM compared to 1 (IC50 8.47-18.00 μM), and remained nontoxic to the NIH3T3 cells.

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