Institute of Research and Development, Duy Tan University, Da Nang 550000, Vietnam.
Department of Science and Technology, Tay Nguyen University, Buon Ma Thuot 630000, Vietnam.
Molecules. 2018 Aug 2;23(8):1928. doi: 10.3390/molecules23081928.
α-Glucosidase inhibitors (aGIs) have been used as an effective therapy for type-2 diabetes, which remains a global health issue. The aim of this study was to achieve bioactivity-guided isolation, identification and evaluation of hypoglycemic compounds from Champ. trunk bark (ELCTB). Eleven active compounds were isolated and identified as walterolactone A/B β-d-pyranoglucoside (), 1-β-d-glucopyranosyloxy-3,5-dimethoxy-4-hydroxybenzene (), (-)-gallocatechin (), schweinfurthinol 9--β-d-pyranoglucoside (), 1--(3-methyl)-butenoyl-myo-inositol (), leonuriside (), (+)-catechin (), methyl galloate (), (-)-catechin (), and condensed tannins ( and ). Of these 11, novel 4 compounds (, , , and ) were found as new α-glucosidase inhibitors. Notably, in vitro results indicated that compounds , , ⁻, , and showed potent activity (IC = 0.076-31 µg/mL), and their activities were at a higher level than that of acarbose, a commercial inhibitor (IC = 1345 µg/mL). In animal tests, the major inhibitor, condensed tannin (), demonstrated significant reduction of plasma glucose in mice with no symptoms of diarrhea at the dose of 100 mg/kg bw. The results suggest that Champ. is a rich source of bioactive compounds for development as health food or drugs with potent hypoglycemic effect. The results of this study also enriched the current novel biological activities of constituents from species.
α-葡萄糖苷酶抑制剂(aGIs)已被用作治疗 2 型糖尿病的有效疗法,而 2 型糖尿病仍是一个全球性的健康问题。本研究的目的是从 Champ. 树干皮(ELCTB)中实现基于生物活性的分离、鉴定和评估降血糖化合物。分离并鉴定了 11 种活性化合物,分别为瓦尔特内酯 A/B β-D-吡喃葡萄糖苷()、1-β-D-吡喃葡萄糖氧基-3,5-二甲氧基-4-羟基苯()、(-)-表儿茶素()、schweinfurthinol 9--β-D-吡喃葡萄糖苷()、1--(3-甲基)-丁烯酰基-肌醇()、莱菔硫烷()、(+)-儿茶素()、没食子酸甲酯()、(-)-儿茶素()和缩合单宁(和)。在这 11 种化合物中,有 4 种(、、、)是新的α-葡萄糖苷酶抑制剂。值得注意的是,体外实验结果表明,化合物、、、和具有很强的活性(IC = 0.076-31 µg/mL),其活性高于阿卡波糖(商业抑制剂,IC = 1345 µg/mL)。在动物试验中,主要抑制剂缩合单宁()在 100 mg/kg bw 剂量下对小鼠没有腹泻症状,能显著降低血浆葡萄糖。结果表明,Champ. 是一种丰富的生物活性化合物来源,可开发为具有降血糖作用的保健品或药物。本研究结果还丰富了当前从 种属中获得的成分的新型生物活性。