β-amyrin heptadecanoate, a new oleanane triterpenoid with α-glucosidase inhibitory and cytotoxic activities from the leaves of Averrhoa bilimbi L.

Chúng tôi vui mừng thông báo rằng TS. Hoàng Lê Thụy Thùy Trang và các đồng nghiệp gần đây đã xuất bản công trình của họ có tựa đề "β-amyrin heptadecanoate, a new oleanane triterpenoid with α-glucosidase inhibitory and cytotoxic activities from the leaves of Averrhoa bilimbi L." in the Natural Product Research

Tóm tắt:

A previously unreported oleanane triterpenoid, β-amyrin heptadecanoate (1), was isolated from the leaves of Thai Averrhoa bilimbi (Oxalidaceae), along with five known compounds, β-amyrin (2), β-sitosterol (3), β-sitosterol-D-glucoside (4), β-sitosteryl oleate (5), and α-tocopherol (6). Their structures were elucidated through spectroscopic analysis, including extensive NMR and HRESIMS, and by comparison with the previous literature. All isolated compounds were evaluated for their α-glucosidase inhibitory and cytotoxic activities. Compound 6 exhibited the highest α-glucosidase inhibition (IC₅₀ of 0.72 ± 1.02 µM), significantly outperforming the standard acarbose (IC₅₀ of 82.00 ± 0.24 μM). Furthermore, compound 4 demonstrated the most potent cytotoxicity against HeLa cells (IC₅₀ of 34.92 ± 0.45 μM), while compound 3 exhibited the strongest cytotoxicity towards A549 cells (IC₅₀ of 9.17 ± 0.30 μM). Additionally, a molecular docking study was conducted on the active α-glucosidase inhibitors to estimate their binding affinities and to identify the ligand-binding sites within the enzyme.