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Ganoboninketals A-C, Antiplasmodial 3,4-seco-27-Norlanostane Triterpenes from Ganoderma boninense Pat

Significance statement

Ganoderma mushrooms have been widely used as herbal medicines for the treatment of various diseases in China. In order to elucidating the chemical basis of their medical application, three new nortriterpenes, ganoboninketals A-C, featuring rearranged highly complex polycyclic systems were isolated from the medicinal mushroom Ganoderma boninense. In vitro, these compounds showed antiplasmodial activity against Plasmodium falciparum with IC50 values range of 1.7-7.9 μM. Ganoboninketals A and C also displayed weak cytotoxicity against A549 cell line with IC50 values of 47.6 and 35.8 μM, respectively. Ganoboninketals B showed weak cytotoxicity towards HeLa cell line with an IC50 value of 65.49 μM. All the three compounds were also evaluated for their NO inhibitory activity in the LPS-induced macrophages. The futher SAR (structure and activity relationship) investigation and in vivo experiments is continuous in our group. All the recent study and further research will efficiently feedback the application of the medicinal mushroom.

Ganoboninketals A-C, Antiplasmodial 3,4-seco-27-Norlanostane Triterpenes from Ganoderma boninense Pat. Global Medical Discovery

Journal Reference

Ma K, Ren J, Han J, Bao L, Li L, Yao Y, Sun C, Zhou B, Liu H. J Nat Prod. 2014 Jul 30.

State Key Laboratory of Mycology, Institute of Microbiology, Chinese Academy of Sciences , Beijing, 100101, People’s Republic of China.

Abstract

Three new nortriterpenes, ganoboninketals A-C (1-3), featuring rearranged 3,4-seco-27-norlanostane skeletons and highly complex polycyclic systems were isolated from the medicinal mushroom Ganoderma boninense. The structures of the new metabolites were established by spectroscopic methods. The absolute configurations in 1-3 were assigned by electronic circular dichroism (ECD) calculations. Compounds 1-3 showed antiplasmodial activity against Plasmodium falciparum with IC50 values of 4.0, 7.9, and 1.7 μM, respectively. Compounds 1 and 3 also displayed weak cytotoxicity against A549 cell line with IC50 values of 47.6 and 35.8 μM, respectively. Compound 2 showed weak cytotoxicity toward HeLa cell line with an IC50 value of 65.5 μM. Compounds 1-3 also presented NO inhibitory activity in the LPS-induced macrophages with IC50 values of 98.3, 24.3, and 60.9 μM, respectively.

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