基于苯并呋喃的色烯并查耳酮的抗高血糖和抗血脂异常活性的设计、合成及评价
Design, synthesis, and evaluation of benzofuran-based chromenochalcones for antihyperglycemic and antidyslipidemic activities.
作者信息
Korthikunta Venkateswarlu, Singh Rohit, Srivastava Rohit, Pandey Jyotsana, Srivastava Atul, Chaturvedi Upma, Mishra Akansha, Srivastava Arvind K, Tamrakar Akhilesh K, Tadigoppula Narender
机构信息
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute Lucknow (U.P.) - 226031 India
Academy of Scientific and Innovative Research (AcSIR) Sector 19 Kamla Nehru Nagar Ghaziabad-201002 India.
出版信息
RSC Med Chem. 2023 Jan 21;14(3):470-481. doi: 10.1039/d2md00341d. eCollection 2023 Mar 22.
A series of benzofuran-based chromenochalcones (16-35) were synthesized and evaluated for and antidiabetic activities in L-6 skeletal muscle cells and streptozotocin (STZ)-induced diabetic rat models, respectively, and further dyslipidemia activity of the compounds was evaluated in a Triton-induced hyperlipidemic hamster model. Among them, compounds 16, 18, 21, 22, 24, 31, and 35 showed significant glucose uptake stimulatory effects in skeletal muscle cells and were further evaluated for efficacy. Compounds 21, 22, and 24 showed a significant reduction in blood glucose levels in STZ-induced diabetic rats. Compounds 16, 20, 21, 24, 28, 29, 34, 35, and 36 were found active in antidyslipidemic studies. Furthermore, compound 24 effectively improved the postprandial and fasting blood glucose levels, oral glucose tolerance, serum lipid profile, serum insulin level, and the HOMA-index of db/db mice, following 15 days of successive treatment.
合成了一系列基于苯并呋喃的色烯查耳酮（16 - 35），并分别在L - 6骨骼肌细胞和链脲佐菌素（STZ）诱导的糖尿病大鼠模型中评估其抗糖尿病活性，还在 Triton 诱导的高脂血症仓鼠模型中评估了这些化合物的抗血脂异常活性。其中，化合物16、18、21、22、24、31和35在骨骼肌细胞中显示出显著的促进葡萄糖摄取的作用，并进一步评估了其疗效。化合物21、22和24在STZ诱导的糖尿病大鼠中显示出血糖水平显著降低。在抗血脂异常研究中发现化合物16、20、21、24、28、29、34、35和36具有活性。此外，连续治疗15天后，化合物24有效改善了db/db小鼠的餐后和空腹血糖水平、口服葡萄糖耐量、血清脂质谱、血清胰岛素水平和HOMA指数。
Zotero 插件