School of Biomedical Sciences, Ulster University, Coleraine, BT52 1SA, Co, Londonderry, Northern Ireland, United Kingdom.
Department of Integrated Bioscience, Graduate School, Konkuk University, Chungju, 27478, Republic of Korea.
J Ethnopharmacol. 2020 May 10;253:112647. doi: 10.1016/j.jep.2020.112647. Epub 2020 Feb 6.
Hibiscus rosa-sinensis (HRS) is a tropical flowery plant, widely distributed in Asian region and an important traditional medicine used in many diseases including cough, diarrhoea and diabetes.
Hibiscus rosa-sinensis (HRS) leaves have been reported to possess anti-hyperglycaemic activity, but little is known concerning the underlying mechanism. This study investigated effects of ethanol extract of HRS on insulin release and glucose homeostasis in a type 2 diabetic rat model.
MATERIALS & METHODS: Effects of ethanol extract of grinded H. rosa-sinensis (HRS) leaves on insulin release, membrane potential and intracellular calcium were determined using rat clonal β-cells (BRIN-BD11 cells) and isolated mouse pancreatic islets. Effects on DPP-IV enzyme activity were investigated in vitro. Acute effects of HRS on glucose tolerance, gut perfusion in situ, sucrose content, intestinal disaccharidase activity and gut motility were measured. Streptozotocin induced type 2 diabetic rats treated for 28 days with ethanol extract of HRS leaf (250 and 500 mg/kg) were used to assess glucose homeostasis.
HRS, significantly increased insulin release from clonal rat BRIN-BD11 cells and this action was confirmed using isolated mouse pancreas islets with stimulatory effects equivalent to GLP-1. HRS induced membrane depolarization and increased intracellular Ca in BRIN BD11 cells and significantly inhibited DPP-IV enzyme activity in vitro. HRS administration in vivo improved glucose tolerance in type 2 diabetic rats, inhibited both glucose absorption during gut perfusion and postprandial hyperglycaemia and it reversibly increased unabsorbed sucrose passage through the gut following sucrose ingestion. HRS decreased intestinal disaccharidase activity and increased gastrointestinal motility in non-diabetic rats. In a chronic 28-day study with type 2 diabetic rats, HRS, at 250 or 500 mg/kg, significantly decreased serum glucose, cholesterol, triglycerides and increased circulating insulin, HDL cholesterol and hepatic glycogen without increasing body weight.
These data suggest the antihyperglycaemic activity of HRS is mediated by inhibiting carbohydrate digestion and absorption, while significantly enhancing insulin secretion in a dose dependent manner. This suggests that HRS has potential as a novel antidiabetic therapy or a dietary supplement for the treatment of type 2 diabetes.
木槿(HRS)是一种热带花卉植物,广泛分布于亚洲地区,是一种重要的传统药物,用于治疗咳嗽、腹泻和糖尿病等多种疾病。
木槿(HRS)叶已被报道具有降血糖活性,但对于其潜在机制知之甚少。本研究旨在探讨 HRS 乙醇提取物对 2 型糖尿病大鼠模型胰岛素分泌和葡萄糖稳态的影响。
采用大鼠克隆β细胞(BRIN-BD11 细胞)和分离的小鼠胰腺胰岛,测定 HRS 叶研磨乙醇提取物对胰岛素释放、膜电位和细胞内钙的影响。体外研究 DPP-IV 酶活性的影响。急性 HRS 对葡萄糖耐量、原位肠道灌注、蔗糖含量、肠双糖酶活性和肠道蠕动的影响。用链脲佐菌素诱导 2 型糖尿病大鼠,用 HRS 叶乙醇提取物(250 和 500mg/kg)治疗 28 天,评估葡萄糖稳态。
HRS 显著增加了克隆大鼠 BRIN-BD11 细胞的胰岛素释放,这一作用在使用刺激作用相当于 GLP-1 的分离小鼠胰腺胰岛时得到了证实。HRS 诱导 BRIN BD11 细胞的膜去极化和细胞内钙增加,并在体外显著抑制 DPP-IV 酶活性。HRS 体内给药可改善 2 型糖尿病大鼠的葡萄糖耐量,抑制肠道灌注时的葡萄糖吸收和餐后高血糖,并可可逆地增加蔗糖摄入后未吸收的蔗糖通过肠道的传递。HRS 降低了非糖尿病大鼠的肠双糖酶活性和胃肠道蠕动。在 28 天的 2 型糖尿病大鼠慢性研究中,HRS 以 250 或 500mg/kg 的剂量给药,可显著降低血清葡萄糖、胆固醇、甘油三酯,增加循环胰岛素、高密度脂蛋白胆固醇和肝糖原,而不增加体重。
这些数据表明,HRS 的降血糖活性是通过抑制碳水化合物消化和吸收,同时以剂量依赖的方式显著增强胰岛素分泌来介导的。这表明 HRS 具有作为新型抗糖尿病治疗或 2 型糖尿病治疗的膳食补充剂的潜力。