Centro de Investigación en Biotecnología Aplicada, Instituto Politécnico Nacional, Tlaxcala 90700, Mexico.
Centro Tlaxcala de Biología de la Conducta, Universidad Autónoma de Tlaxcala, Tlaxcala 90070, Mexico.
Molecules. 2023 Jul 30;28(15):5760. doi: 10.3390/molecules28155760.
Among antihyperglycemic drugs used for treating diabetes, α-glucosidase inhibitors generate the least adverse effects. This contribution aimed to evaluate the potential antidiabetic activity of L. by testing its in vitro α-glucosidase inhibition and in vivo antihyperglycemic effects on rats with streptozotocin (STZ)-induced diabetes. Better inhibition of α-glucosidase was found with the methanol extract versus the n-hexane and dichloromethane extracts. The methanol extract of the flowers (RCFM) was more effective than that of the leaves (RCHM), with an IC of 7.3 ± 0.17 μg/mL for RCFM and 112.0 ± 1.23 μg/mL for RCHM. A bioactive fraction (F89s) also showed good α-glucosidase inhibition (IC = 3.8 ± 0.11 μg/mL). In a preliminary study, RCHM and RCFM at 150 mg/kg and F89s at 75 mg/kg after 30 days showed a significant effect on hyperglycemia, reducing glucose levels (82.2, 80.1, and 84.1%, respectively), and improved the lipid, renal, and hepatic profiles of the rats, comparable with the effects of metformin and acarbose. According to the results, the activity of L. may be mediated by a diminished rate of disaccharide hydrolysis, associated with the inhibition of α-glucosidase. Thus, L. holds promise for the development of auxiliary drugs to treat diabetes mellitus.
在用于治疗糖尿病的抗高血糖药物中，α-葡萄糖苷酶抑制剂产生的不良反应最少。本研究旨在通过检测其对链脲佐菌素（STZ）诱导的糖尿病大鼠的体外α-葡萄糖苷酶抑制作用和体内降血糖作用，来评估 L. 的潜在抗糖尿病活性。与正己烷和二氯甲烷提取物相比，甲醇提取物对α-葡萄糖苷酶的抑制作用更好。花的甲醇提取物（RCFM）比叶的甲醇提取物（RCHM）更有效，RCFM 的 IC 为 7.3±0.17μg/mL，RCHM 的 IC 为 112.0±1.23μg/mL。一个生物活性部分（F89s）也表现出良好的α-葡萄糖苷酶抑制作用（IC=3.8±0.11μg/mL）。在初步研究中，RCHM 和 RCFM 以 150mg/kg 和 F89s 以 75mg/kg 给药 30 天后，对高血糖有显著作用，分别降低葡萄糖水平（82.2%、80.1%和 84.1%），并改善了大鼠的脂质、肾脏和肝脏状况，与二甲双胍和阿卡波糖的效果相当。根据结果，L.的活性可能是通过减少二糖水解的速率介导的，这与α-葡萄糖苷酶的抑制有关。因此，L.有希望开发辅助治疗糖尿病的药物。
