从果实中提取的具有葡萄糖苷酶抑制和抗菌活性的苯甲酰基间苯三酚：体外和计算研究。
-Glucosidase Inhibitory and Antimicrobial Benzoylphloroglucinols from Fruits: In Vitro and In Silico Studies.
机构信息
Faculty of Pharmacy, Ton Duc Thang University, Ho Chi Minh City 700000, Vietnam.
Institute of Research and Development, Duy Tan University, Da Nang 550000, Vietnam.
出版信息
Molecules. 2022 Apr 15;27(8):2574. doi: 10.3390/molecules27082574.
α-Glucosidase plays a role in hydrolyzing complex carbohydrates into glucose, which is easily absorbed, causing postprandial hyperglycemia. Inhibition of α-glucosidase is therefore an ideal approach to preventing this condition. A novel polyprenylated benzoylphloroglucinol, which we named schomburgkianone I (), was isolated from the fruit of , along with an already-reported compound, guttiferone K (). The structures of the two compounds were determined using NMR and HRESIMS analysis, and comparisons were made with previous studies. Compounds and exhibited potent -glucosidase inhibition (IC of 21.2 and 34.8 µM, respectively), outperforming the acarbose positive control. Compound produced wide zones of inhibition against and (of 21 and 20 mm, respectively), compared with the 19 and 20 mm zones of compound , at a concentration of 50 µg/mL. The MIC value of compound against was 13.32 µM. An in silico molecular docking model suggested that both compounds are potent inhibitors of enzyme α-glucosidase and are therefore leading candidates as therapies for diabetes mellitus.
α-葡萄糖苷酶在将复杂碳水化合物水解成葡萄糖方面发挥作用，葡萄糖很容易被吸收，导致餐后高血糖。因此，抑制α-葡萄糖苷酶是预防这种情况的理想方法。一种新型的多聚异戊二烯基苯甲酰基间苯三酚，我们将其命名为 schomburgkianone I ()，是从 的果实中分离出来的，同时还分离出了一种已经报道过的化合物，guttiferone K ()。这两种化合物的结构通过 NMR 和 HRESIMS 分析确定，并与以前的研究进行了比较。化合物 和 表现出很强的 -葡萄糖苷酶抑制活性（IC 分别为 21.2 和 34.8 µM），优于阿卡波糖阳性对照。化合物 在 50 µg/mL 浓度下对 和 的抑制带宽度分别为 21 和 20 mm，而化合物 的抑制带宽度分别为 19 和 20 mm。化合物 对 的 MIC 值为 13.32 µM。基于计算机的分子对接模型表明，这两种化合物都是α-葡萄糖苷酶的有效抑制剂，因此是治疗糖尿病的候选药物。
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