Indole Diterpene Derivatives from the Aspergillus flavus GZWMJZ-288, an Endophytic Fungus from Garcinia multiflora.

Autor:	Wang, Dongyang, Zhuang, Xiaohong, Yin, Ying, Wu, Dan, He, Wenwen, Zhu, Weiming, Xu, Yanchao, Zuo, Mingxing, Wang, Liping
Předmět:	ENDOPHYTIC fungi INDOLE derivatives GARCINIA MOLECULAR docking BIOACTIVE compounds ASPERGILLUS flavus ASPERGILLUS
Zdroj:	Molecules; Dec2023, Vol. 28 Issue 23, p7931, 12p
Abstrakt:	A new indole diterpene, 26-dihydroxyaflavininyl acetate (1), along with five known analogs (2–6) were isolated from the liquid fermentation of Aspergillus flavus GZWMJZ-288, an endophyte from Garcinia multiflora. The structures of these compounds were identified through NMR, MS, chemical reaction, and X-ray diffraction experiments. Enzyme inhibition activity screening found that compounds 1, 4, and 6 have a good binding affinity with NPC1L1, among which compound 6 exhibited a stronger binding ability than ezetimibe at a concentration of 10 µM. Moreover, compound 5 showed inhibitory activity against α-glucosidase with an IC50 value of 29.22 ± 0.83 µM, which is 13 times stronger than that of acarbose. The results suggest that these aflavinine analogs may serve as lead compounds for the development of drugs targeting NPC1L1 and α-glucosidase. The binding modes of the bioactive compounds with NPC1L1 and α-glucosidase were also performed through in silico docking studies. [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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