| Summary: | A new indole diterpene, 26-dihydroxyaflavininyl acetate (<b>1</b>), along with five known analogs (<b>2</b>–<b>6</b>) were isolated from the liquid fermentation of <i>Aspergillus flavus</i> GZWMJZ-288, an endophyte from <i>Garcinia multiflora</i>. The structures of these compounds were identified through NMR, MS, chemical reaction, and X-ray diffraction experiments. Enzyme inhibition activity screening found that compounds <b>1</b>, <b>4</b>, and <b>6</b> have a good binding affinity with NPC1L1, among which compound <b>6</b> exhibited a stronger binding ability than ezetimibe at a concentration of 10 µM. Moreover, compound <b>5</b> showed inhibitory activity against <i>α</i>-glucosidase with an IC<sub>50</sub> 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 <i>α</i>-glucosidase. The binding modes of the bioactive compounds with NPC1L1 and α-glucosidase were also performed through in silico docking studies.
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