Borapetoside E, a Clerodane Diterpenoid Extracted from Tinospora crispa, Improves Hyperglycemia and Hyperlipidemia in High-Fat-Diet-Induced Type 2 Diabetes Mice

  • J Nat Prod. 2017 Aug 25;80(8):2319-2327. doi: 10.1021/acs.jnatprod.7b00365.
Yuhui Xu  1  2 Yanfen Niu  1  2  3 Yuan Gao  4  5 Fang Wang  1  2 Wanying Qin  1  2 Yanting Lu  1  2 Jing Hu  1  2 Li Peng  1  2 Jikai Liu  6 Wenyong Xiong  1  2
Affiliations
  • 1. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences , Kunming 650201, People's Republic of China.
  • 2. University of the Chinese Academy of Sciences , Beijing 100049, People's Republic of China.
  • 3. Engineering Research Center, Kunming Medical University , Kunming 650500, People's Republic of China.
  • 4. BioBioPha Co., Ltd , Kunming 650201, People's Republic of China.
  • 5. Deparment of Chemical Engineering, Yibin University , Yibin 644000, People's Republic of China.
  • 6. School of Pharmaceutical Sciences, South-Central University for Nationalities , Wuhan 430074, People's Republic of China.
Abstract

An insidious increase in the incidence of obesity, Insulin resistance, and hyperlipidemia has led to an epidemic of type 2 diabetes worldwide. Tinospora crispa (T. crispa) is a familiar plant traditionally used in herbal medicine for diabetes; however, the major active ingredients of this plant are still unclear. In this study, we identified the therapeutic effects of borapetoside E, a small molecule extracted from T. crispa, in high-fat-diet (HFD)-induced obesity in mice. The therapeutic effects of borapetoside E in HFD-induced obese mice were assessed physiologically, histologically, and biochemically following intraperitoneal injection. Furthermore, we analyzed the expression of glucose and lipid metabolism-related genes and proteins in borapetoside E-treated obese mice. Compared with vehicle-treated mice, borapetoside E markedly improved hyperglycemia, Insulin resistance, hepatic steatosis, hyperlipidemia, and oxygen consumption in obese mice, and the effects were comparable to or better than the drug metformin. In addition, borapetoside E suppressed the expression of sterol regulatory element binding proteins (SREBPs) and their downstream target genes related to lipid synthesis in the liver and adipose tissue. Borapetoside E showed beneficial effects in vivo, demonstrating that borapetoside E may be a potential therapy for the treatment of diet-induced type 2 diabetes and related metabolic syndromes.

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