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Trans-3,5-dicaffeoylquinic acid from Geigeria alata Benth. & Hook.f. ex Oliv. & Hiern with beneficial effects on experimental diabetes in animal model of essential hypertension

Simeonova, Rumyana, Vitcheva, Vessela, Zheleva-Dimitrova, Dimitrina, Balabanova, Vessela, Savov, Ionko, Yagi, Sakina, Dimitrova, Bozhana, Voynikov, Yulian, Gevrenova, Reneta
Food and chemical toxicology 2019 v.132 pp. 110678
Geigeria, acarbose, acute oral toxicity, animal disease models, antihypertensive effect, antioxidant enzymes, biomarkers, blood glucose, blood pressure, enzyme inhibition, enzyme inhibitors, glutathione, glutathione peroxidase, glutathione transferase, glutathione-disulfide reductase, glycemic effect, histopathology, hypertension, inhibitory concentration 50, intraperitoneal injection, lethal dose 50, liver, malondialdehyde, mass spectrometry, medicinal plants, noninsulin-dependent diabetes mellitus, nuclear magnetic resonance spectroscopy, oxidative stress, rats, roots, streptozotocin, traditional medicine
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 LD50 = 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 (IC50 27.24 μg/mL) than acarbose (IC50 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.