Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav St., 1000, Sofia, Bulgaria.
Department of Pharmacognosy, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav St., 1000, Sofia, Bulgaria.
Food Chem Toxicol. 2019 Oct;132:110678. doi: 10.1016/j.fct.2019.110678. Epub 2019 Jul 16.
Geigeria alata Benth. & Hook.f. ex Oliv. & Hiern (Asteraceae) is used in Sudanese folk medicine for treatment of diabetes. The study aimed to estimate the acute oral toxicity of trans-3,5-dicaffeoylquinic acid (3,5-diCQA) from G. alata roots and to assess its antihypeglycemic, antioxidant and antihypertensive effects on chemically-induced diabetic spontaneously hypertensive rats (SHRs). The structure of 3,5-diCQA was established by NMR and HRMS spectra. Type 2 diabetes was induced by intraperitoneal injection of streptozotocin. 3,5-diCQA was slightly toxic with LD = 2154 mg/kg. At 5 mg/kg 3,5-diCQA reduced significantly (p < 0.05) the blood glucose levels by 42%, decreased the blood pressure by 22% and ameliorated the oxidative stress biomarkers reduced glutathione, malondialdehyde, and serum biochemical parameters. The beneficial effect on antioxidant enzymes was evidenced by the elevated glutathione peroxidase, glutathione reductase, and glutathione S-transferase activitiy in the livers of diabetic animals. 3,5-diCQA prevents the histopathological changes related to diabetes and hypertension. 3,5-diCQA was more potent α-glucosidase inhibitor (IC 27.24 μg/mL) than acarbose (IC 99.77 μg/mL). The antihyperglycemic action of the compound was attributed to the α-glucosidase inhibition. The beneficial effects of 3,5-diCQA on streptozotocin-induced diabetic hypertensive rats support the traditional use of G.alata for the management of diabetes.
锯齿状 Geigeria alata Benth. & Hook.f. ex Oliv. & Hiern(菊科)的根在苏丹民间医学中用于治疗糖尿病。本研究旨在评估锯齿状 Geigeria alata 根中反式-3,5-二咖啡酰奎宁酸(3,5-diCQA)的急性口服毒性,并评估其对化学诱导的糖尿病自发性高血压大鼠(SHRs)的抗高血糖、抗氧化和降压作用。3,5-diCQA 的结构通过 NMR 和 HRMS 谱确定。2 型糖尿病通过腹腔注射链脲佐菌素诱导。3,5-diCQA 略有毒性,LD=2154mg/kg。3,5-diCQA 以 5mg/kg 给药可使血糖水平显著降低(p<0.05)42%,血压降低 22%,并改善还原型谷胱甘肽、丙二醛和血清生化参数等氧化应激生物标志物。抗氧化酶活性升高表明 3,5-diCQA 对糖尿病动物肝脏中的谷胱甘肽过氧化物酶、谷胱甘肽还原酶和谷胱甘肽 S-转移酶具有有益作用。3,5-diCQA 可预防与糖尿病和高血压相关的组织病理学变化。3,5-diCQA 是比阿卡波糖(IC 99.77μg/mL)更强的α-葡萄糖苷酶抑制剂(IC 27.24μg/mL)。该化合物的降血糖作用归因于其对α-葡萄糖苷酶的抑制作用。3,5-diCQA 对链脲佐菌素诱导的糖尿病高血压大鼠的有益作用支持了 Geigeria alata 用于糖尿病治疗的传统用途。