Anti-diabetic effect of three new norditerpenoid alkaloids in vitro and potential mechanism via PI3K/Akt signaling pathway
文献类型:期刊论文
作者 | Tang, D (Tang, Dan); Chen, QB (Chen, Qi-Bin); Xin, XL (Xin, Xue-Lei); Aisa, HA (Aisa, Haji-Akber); Aisa, HA; Xin, XL |
刊名 | BIOMEDICINE & PHARMACOTHERAPY |
出版日期 | 2017 |
卷号 | 87期号:3页码:145-152 |
关键词 | Diabetes Norditerpenoid alkaloids Anti-diabetic activity Glucose metabolism Protein tyrosine phosphatase 1B PI3K/Akt signaling pathway |
通讯作者 | Xin, XL ; Aisa, HA |
英文摘要 | Diabetes is a metabolic disease with the characteristic of high blood glucose (hyperglycemia). In our previous study, we found that nigelladines A-C (compounds A-C), three norditerpenoid alkaloids from the seeds of Nigella glandulifera Freyn (Ranunculaceae) exhibited protein of tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro. In the present study, we further investigated their anti-diabetes activities in L6 moytubes and illuminated the mechanisms of action of compounds A-C. Several parameters of glucose metabolism such as glucose consumption, glycogen content and hexokinase activity were increased by compounds A-C. The results suggested that compounds A-C improved glucose metabolism through promoting synthesis of glycogen. Expression of PTP1B protein was inhibited by compounds A-C in L6 moytubes. PI3K-dependent Akt phosphorylation was found to be activated by compounds A-C and completely blocked by wortmannin (a PI3K inhibitor). Moreover, the insulin-mediated induction of insulin receptor substrate-1 (IRS-1) and glycogen synthase kinase-3 beta (GSK-3 beta) were also suppressed by wortmannin. Western blot results indicated that compounds A-C-induced IRS-1/ Akt activation was likely a consequence of PTP1B inhibition. Compounds A-C promoted glycogen synthesis through Akt-mediated GSK3 phosphorylation. Therefore, activation of PI3 K/Akt insulin signaling pathway and suppression of PTP1B is the molecular mechanism that contributes to the antidiabetic effect of compounds A-C in cellular models. The three alkaloids potentially serve as lead compounds for the development of antidiabetic drugs. |
收录类别 | SCI |
WOS记录号 | WOS:000395525600016 |
源URL | [http://ir.xjipc.cas.cn/handle/365002/4747] |
专题 | 新疆理化技术研究所_省部共建新疆特有药用资源利用重点实验室 |
通讯作者 | Aisa, HA; Xin, XL |
作者单位 | 1.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Chem Arid Zone, Urumqi 830011, Peoples R China 2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100039, Peoples R China |
推荐引用方式 GB/T 7714 | Tang, D ,Chen, QB ,Xin, XL ,et al. Anti-diabetic effect of three new norditerpenoid alkaloids in vitro and potential mechanism via PI3K/Akt signaling pathway[J]. BIOMEDICINE & PHARMACOTHERAPY,2017,87(3):145-152. |
APA | Tang, D ,Chen, QB ,Xin, XL ,Aisa, HA ,Aisa, HA,&Xin, XL.(2017).Anti-diabetic effect of three new norditerpenoid alkaloids in vitro and potential mechanism via PI3K/Akt signaling pathway.BIOMEDICINE & PHARMACOTHERAPY,87(3),145-152. |
MLA | Tang, D ,et al."Anti-diabetic effect of three new norditerpenoid alkaloids in vitro and potential mechanism via PI3K/Akt signaling pathway".BIOMEDICINE & PHARMACOTHERAPY 87.3(2017):145-152. |
入库方式: OAI收割
来源:新疆理化技术研究所
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