Zhang Guoying, Liu Liying, Jia Wenjing, Wang Luya, Tao Jihong, Zhang Wei, Yue Huilan, Zhang Dejun, Zhao Xiaohui
Research Centre for High Altitude Medicine, Key Laboratory of High Altitude Medicine (Ministry of Education), Key Laboratory of Applied Fundamentals of High Altitude Medicine (Qinghai-Utah Joint Research Lab for High Altitude Medicine), Laboratory for High Altitude Medicine of Qinghai Province, Qinghai University, Xining 810001, China.
Qinghai Provincial Center for Drug Evaluation and Inspection, Xining 810007, China.
Pharmaceuticals (Basel). 2025 Jul 23;18(8):1087. doi: 10.3390/ph18081087.
Reducing postprandial blood glucose (PBG) is a crucial strategy for treating diabetes and minimizing the risk of complications. Developing efficient and safe -glycosidase inhibitors from natural products to lower PBG has attracted much attention. L. (SP), a traditional herbal medicine of North American Indigenous tribes, has efficacy of treating metabolic diseases, but its hypoglycemic activity and bioactive components have not been fully studied. In vitro -glucosidase inhibition and in vivo sucrose/maltose/starch tolerance assays were performed to assess the hypoglycemic effects of SP extracts, and UPLC-Triple-TOF-MS/MS analysis was used to tentatively identify its chemical structure composition. In vitro enzyme inhibition and molecular docking were used to verify the effective ingredients. In vitro hypoglycemic activities of four extracts of SP (SP-10/SP-40/SP-60/SP-C) showed that SP-10 exhibited strong -glucosidase (sucrase and maltase) inhibitory effects with IC of 67.81 μg/mL and 62.99 μg/mL, respectively. Carbohydrate tolerance assays demonstrated that SP-10 could significantly reduce the PBG levels of diabetic mice, with a significant hypoglycemic effect at a dosage of 20 mg/kg. A total of 26 constituents, including 11 caffeoylquinic acids (CQAs) and 15 flavonol glycosides, were tentatively identified by mainly analyzing secondary MS fragmentation. Moreover, three CQAs rich in SP-10, namely chlorogenic acid (CGA), neochlorogenic acid (NCGA), and cryptochlorogenic acid (CCGA), may be the main hypoglycemic substances, as evidenced by their inhibitory effects on sucrase and maltase. The -glucosidase inhibitory effects of SP extract both in vitro and in vivo and its active ingredients were systematically studied for the first time. Results indicated that SP extract, rich in CQAs, had significant hypoglycemic activity, supporting the considerable potential of SP as hypoglycemic functional food or cost-effective therapeutic agents for diabetes treatment.
降低餐后血糖（PBG）是治疗糖尿病和降低并发症风险的关键策略。从天然产物中开发高效、安全的α-糖苷酶抑制剂以降低PBG已引起广泛关注。北美原住民部落的传统草药L.（SP）具有治疗代谢疾病的功效，但其降血糖活性和生物活性成分尚未得到充分研究。进行了体外α-葡萄糖苷酶抑制和体内蔗糖/麦芽糖/淀粉耐受性试验，以评估SP提取物的降血糖作用，并采用超高效液相色谱-三重四极杆飞行时间质谱联用（UPLC-Triple-TOF-MS/MS）分析初步鉴定其化学结构组成。利用体外酶抑制和分子对接来验证有效成分。SP的四种提取物（SP-10/SP-40/SP-60/SP-C）在体外的降血糖活性表明，SP-10对α-葡萄糖苷酶（蔗糖酶和麦芽糖酶）具有较强的抑制作用，IC50分别为67.81μg/mL和62.99μg/mL。碳水化合物耐受性试验表明，SP-10能显著降低糖尿病小鼠的PBG水平，在20mg/kg剂量时具有显著的降血糖作用。通过对二级质谱碎片进行主要分析，初步鉴定出共26种成分，包括11种咖啡酰奎宁酸（CQA）和15种黄酮醇苷。此外，SP-10中富含的三种CQA，即绿原酸（CGA）、新绿原酸（NCGA）和隐绿原酸（CCGA），可能是主要的降血糖物质，它们对蔗糖酶和麦芽糖酶的抑制作用证明了这一点。首次系统研究了SP提取物在体外和体内的α-葡萄糖苷酶抑制作用及其活性成分。结果表明，富含CQA的SP提取物具有显著的降血糖活性，支持SP作为降血糖功能食品或具有成本效益的糖尿病治疗药物的巨大潜力。
