Elhady Sameh S, Youssef Fadia S, Alahdal Abdulrahman M, Almasri Diena M, Ashour Mohamed L
Department of Natural Products, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Department of Pharmacognosy, Faculty of Pharmacy, Ain-Shams University, Abbasia, Cairo 11566, Egypt.
Plants (Basel). 2021 Oct 30;10(11):2351. doi: 10.3390/plants10112351.
Lam. is an ornamental evergreen shrub with few reports concerning its phytoconstituents and biological activities. Herein, the antihyperglycaemic activity of leaves methanol extract (BIT) was evaluated for the first time using in vitro and in vivo studies. Molecular modelling was performed for its major phytoconstituents that were further subjected to ADME/TOPAKT (absorption, distribution, metabolism, excretion and toxicity) prediction. BIT revealed considerable reduction in glucose concentration by 9.93% at 50 μg/mL using 3T3-L1 adipocyte culture. It displayed substantial inhibition versus -glucosidase and -amylase with IC 205.2 and 385.06 μg/mL, respectively. In vivo antihyperglycaemic activity of BIT and the ethyl acetate fraction (BIE) was performed using streptozotocin-induced diabetes in rat model. BIT and BIE effectively ameliorate oxidative stress markers in addition to reducing serum blood glucose by 56.08 and 54.00%, respectively, and are associated with a substantial increase in serum insulin by 4.1 and 12.7%, respectively. This can be attributed to its richness with polyphenolic compounds comprising flavonoids, phenolic acids, phenyl propanoids and iridoids. Molecular docking showed that verbascoside and kaempferol displayed the highest fitting within human -amylase (HA) and human -glucosidase (HG) active sites, respectively. They showed reasonable pharmacokinetic, pharmacodynamic and toxicity properties, as revealed by ADME/TOPKAT study.
拉姆(Lam.)是一种观赏性常绿灌木,关于其植物成分和生物活性的报道较少。在此,首次通过体外和体内研究评估了叶片甲醇提取物(BIT)的降血糖活性。对其主要植物成分进行了分子建模,并进一步对其进行了ADME/TOPAKT(吸收、分布、代谢、排泄和毒性)预测。使用3T3-L1脂肪细胞培养,BIT在50μg/mL时显示葡萄糖浓度显著降低了9.93%。它对α-葡萄糖苷酶和α-淀粉酶表现出显著抑制作用,IC50分别为205.2和385.06μg/mL。使用链脲佐菌素诱导的大鼠糖尿病模型对BIT和乙酸乙酯馏分(BIE)进行了体内降血糖活性研究。BIT和BIE除了分别使血清血糖降低56.08%和54.00%外,还有效改善了氧化应激标志物,并且分别使血清胰岛素显著增加了4.1%和12.7%。这可归因于其富含包括黄酮类、酚酸、苯丙烷类和环烯醚萜类在内的多酚化合物。分子对接表明,毛蕊花糖苷和山奈酚分别在人α-淀粉酶(HA)和人α-葡萄糖苷酶(HG)活性位点显示出最高的契合度。ADME/TOPKAT研究表明,它们具有合理的药代动力学、药效学和毒性特性。