Laboratory of Drugs Discovery, Department of Biological Sciences and Health, Federal University of Amapá, Macapá, Brazil.
Division of Post-Grade, University of the Sierra, Ixtlán de Juárez, México.
J Biomol Struct Dyn. 2021 Feb;39(3):1017-1028. doi: 10.1080/07391102.2020.1724567. Epub 2020 Feb 13.
The objectives of this study were to extract and purify Bixin from the seeds of and to evaluate its hypoglycemic activity , as well as, to conduct an study of selectivity on peroxisome proliferator-activated receptors via molecular docking and molecular dynamics simulations. Oral administration of Bixin (10 mg/kg) significantly reduced their glucose level that was alloxan-induced diabetic rats. Bixin showed selectivity on peroxisome proliferator-activated receptors (PPARs), particularly by the peroxisome proliferator-activated receptor gamma (PPARγ), which supports the hypoglycemic activity of Bixin. From the results obtained, it can be inferred that Bixin presents hypoglycemic characteristics, which was confirmed by the results obtained from the and tests. Bixin may act by other pathways to control blood glucose and thus it is possible that it presents a different toxicity profile than troglitazone, rosiglitazone and pioglitazone. However, more studies on the activity and toxicity of Bixin are needed to evaluate for further clinical use. Communicated by Ramaswamy H. Sarma.
本研究的目的是从 种子中提取和纯化胭脂树素，并评价其降血糖活性，以及通过分子对接和分子动力学模拟对过氧化物酶体增殖物激活受体进行选择性研究。胭脂树素（10mg/kg）口服给药可显著降低链脲佐菌素诱导的糖尿病大鼠的血糖水平。胭脂树素对过氧化物酶体增殖物激活受体（PPARs）具有选择性，特别是对过氧化物酶体增殖物激活受体γ（PPARγ），这支持了胭脂树素的降血糖活性。从所得结果可以推断，胭脂树素具有降血糖特性，这从 和 试验的结果得到了证实。胭脂树素可能通过其他途径来控制血糖，因此它的毒性谱可能与曲格列酮、罗格列酮和吡格列酮不同。然而，需要更多关于胭脂树素活性和毒性的研究来评估其进一步的临床应用。Ramaswamy H. Sarma 通讯。
