Hydroxytyrosol nicotinate, a new multifunctional hypolipidemic and hypoglycemic agent

• Published in: Biomedicine & pharmacotherapy Vol. 99; pp. 715 - 724
• Main Authors: Xie, Yun-Dong, Chen, Zi-Zhang, Li, Na, Lu, Wen-Fang, Xu, Yan-Hong, Lin, Yuan-Yuan, Shao, Li-Hua, Wang, Qiu-Tang, Guo, Li-Ying, Gao, Yu-Qiong, Yang, Guang-De, Li, Yi-Ping, Bian, Xiao-Li
• Format: Journal Article
• Language: English
• Published: France Elsevier Masson SAS 01.03.2018
• Subjects: Animals; Antiglycation; Antioxidant; Antioxidants - administration & dosage; Antioxidants - chemistry; Antioxidants - pharmacology; Blood Glucose - drug effects; Diabetes Mellitus, Experimental - drug therapy; Diabetes Mellitus, Type 2 - drug therapy; Hydroxytyrosol nicotinate; Hyperlipidemias - drug therapy; Hypoglycemia; Hypoglycemic Agents - administration & dosage; Hypoglycemic Agents - chemistry; Hypoglycemic Agents - pharmacology; Hypolipidemia; Hypolipidemic Agents - administration & dosage; Hypolipidemic Agents - chemistry; Hypolipidemic Agents - pharmacology; Inhibitory Concentration 50; Lipids - blood; Male; Mice; Niacin - administration & dosage; Niacin - chemistry; Niacin - pharmacology; Oxidative Stress - drug effects; Phenylethyl Alcohol - administration & dosage; Phenylethyl Alcohol - analogs & derivatives; Phenylethyl Alcohol - chemistry; Phenylethyl Alcohol - pharmacology; Rats; α-glucosidase inhibition; α-glucosidase inhibition; Hydroxytyrosol nicotinate; Antiglycation; Antioxidant; Hypoglycemia; Hypolipidemia; glucosidase inhibition
• ISSN: 0753-3322; 1950-6007
• DOI: 10.1016/j.biopha.2018.01.123

[Display omitted] Hydroxytyrosol (HT) is a natural polyphenol antioxidant that exists in olive oil. In the study of multifunctional hypolipidemic of nicotinic derivatives, we found that hydroxytyrosol nicotinate (HT-N) incorporation of niacin with HT displayed α-glucosidase inhibitory activities in vitro, such as yeast α-glucosidase (IC50 = 117.72 μM) and rat intestinal α-glucosidases maltase (IC50 = 31.86 μM) and sucrase (IC50 = 22.99 μM), and had a good control of postprandial blood glucose (PBG). HT-N shown significantly hypoglycemic action by 16.9% and protection of pancreatic tissue in type 2 diabetic mellitus (T2DM) mouse model. HT-N also shown a potent antioxidant activity and property of anti-glycation in vitro, which were benefit for ameliorating diabetic complications. Moreover, HT-N exhibited much significant hypolipidemia, lowering plasma triglyceride (TG), total cholesterol (TC), and malonaldehyde (MDA) by 34.6%, 45.8% and 32.1% respectively, in hyperlipidemic mice induced by Triton WR 1339. The results indicated that HT-N has hypolipidemic, hypoglycemic and antioxidant actions. All these properties could be conducive to amelioration of oxidative stress, hyperlipidemia, and diabetes that HT-N may serve as a multifunctional potential therapeutic strategy in diabetic patients with hyperlipidemia.