Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand.
Department of Pharmacology and Toxicology, University of Utah, Salt Lake City, UT 81112, USA.
Molecules. 2022 Apr 7;27(8):2393. doi: 10.3390/molecules27082393.
Bioactive compounds from medicinal plants are good alternative treatments for T2DM. They are also sources of lead molecules that could lead to new drug discoveries. In this study, Craib. stem, a traditional Thai medicinal plant for detoxification, was extracted into five fractions, including crude extract, BsH, BsD, BsE, and BsW, by ethanolic maceration and sequential partition with hexane, dichloromethane, ethyl acetate, and water, respectively. Among these fractions, BsE contained the highest amounts of phenolics (620.67 mg GAE/g extract) and flavonoids (131.35 mg QE/g extract). BsE exhibited the maximum inhibitory activity against α-glucosidase (IC 1.51 ± 0.01 µg/mL) and DPP-IV (IC 2.62 ± 0.03 µg/mL), as well as dominantly promoting glucose uptake on 3T3-L1 adipocytes. Furthermore, the four compounds isolated from the BsE fraction, namely resveratrol, epicatechin, quercetin, and gallic acid, were identified. Quercetin demonstrated the highest inhibitory capacity against α-glucosidase (IC 6.26 ± 0.36 µM) and DPP-IV (IC 8.25 µM). In addition, quercetin prominently enhanced the glucose uptake stimulation effect on 3T3-L1 adipocytes. Altogether, we concluded that quercetin was probably the principal bioactive compound of the stem for anti-diabetic, and the flavonoid-rich fraction may be sufficiently potent to be an alternative treatment for blood sugar control.
药用植物中的生物活性化合物是治疗 T2DM 的良好替代疗法。它们也是潜在的先导化合物的来源,可以促进新药的发现。在这项研究中,Craib. 茎是一种传统的泰国民间解毒药用植物,通过乙醇浸提和依次用正己烷、二氯甲烷、乙酸乙酯和水萃取,将其分为五个部分,包括粗提物、BsH、BsD、BsE 和 BsW。在这些部分中,BsE 含有最高量的酚类(620.67 mg GAE/g 提取物)和类黄酮(131.35 mg QE/g 提取物)。BsE 对 α-葡萄糖苷酶(IC 1.51 ± 0.01 µg/mL)和 DPP-IV(IC 2.62 ± 0.03 µg/mL)表现出最大的抑制活性,以及在 3T3-L1 脂肪细胞上显著促进葡萄糖摄取。此外,从 BsE 部分分离出的四种化合物,即白藜芦醇、表儿茶素、槲皮素和没食子酸,已被鉴定。槲皮素对 α-葡萄糖苷酶(IC 6.26 ± 0.36 µM)和 DPP-IV(IC 8.25 µM)的抑制能力最高。此外,槲皮素显著增强了对 3T3-L1 脂肪细胞的葡萄糖摄取刺激作用。总的来说,我们得出结论,槲皮素可能是 Craib. 茎用于抗糖尿病的主要生物活性化合物,而富含类黄酮的部分可能足以作为控制血糖的替代治疗方法。