全球糖尿病统计数据的持续增长预示着生产力和寿命的下降,因此,它需要更有效和安全的治疗选择,值得关注的疾病。虽然一些关于抗糖尿病植物的报道,包括HuraCrepitans,可用,目前仍然缺乏关于克氏螺旋体的整体抗糖尿病特性及其相关并发症的信息。这项研究评估了Huracrepitans甲醇提取物的体外抗糖尿病潜力,在体内,和硅方法。提取物显示出剂量依赖性的体外作用,在150和300mg/kg体重下,链脲佐菌素(STZ)诱导的糖尿病大鼠的空腹血糖水平分别降低了47.97%和65.34%,分别。同样,提取物增加了血清和胰腺胰岛素水平,并通过降低胆碱酯酶的表达水平显着改善神经元氧化应激和炎症,NF-κB,和COX-2在高血糖大鼠脑中的表达。血清血脂异常,肝脏,和肾脏生物标志物指数,提取物也显着减轻了糖尿病大鼠的血液学改变。几个组成部分,主要是萜烯,在提取物中鉴定。为了进一步预测药物的相似性,药代动力学,和化合物的结合特性,进行了计算机模拟分析。Ergosta-2,24-dien-26-石油酸,18-(乙酰氧基)-5,6-环氧-4,22-二羟基-1-氧代-,三角洲。-内酯-4.beta。,显示乙酰胆碱酯酶的最高对接分数,丁酰胆碱酯酶,α-淀粉酶,和核因子-kB的值为-12.4、-10.9、-10.3和-9.4kcal/mol,而ergost-25-ene-6,12-dione,3,5-二羟基-,(3)beta。,5.阿尔法。)最高的是环氧合酶-2(-9.0千卡/摩尔)。排名靠前的化合物还表现出显著的口服药物相似性,药代动力学,和安全属性。总之,我们的数据为Huracrepitans改善糖尿病及其相关并发症的潜力提供了临床前证据.
The continual increase in global diabetic statistics portends decreased productivity and life spans, thus making it a disease of concern requiring more effective and safe therapeutic options. While several reports on antidiabetic plants, including Hura crepitans, are available, there is still a dearth of information on the holistic antidiabetic properties of H. crepitans and its associated complications. This study evaluated the antidiabetic potential of methanolic extract of Hura crepitans using in vitro, in vivo, and in silico approaches. The extract revealed a dose-dependent in vitro effect, with a 47.97 % and 65.34 % decrease in the fasting blood sugar levels of
streptozotocin (STZ) induced diabetic rats at 150 and 300 mg/kg BW, respectively. Likewise, the extract increased serum and pancreatic insulin levels, and significantly ameliorated neuronal oxidative stress and inflammation by reducing the expression levels of cholinesterase, NF-κB, and COX-2 in the brain of hyperglycemic rats. Serum dyslipidemia, liver, and kidney biomarker indices, and hematological alterations in diabetic rats were also significantly attenuated by the extract. Several constituents, mainly terpenes, were identified in the extract. To further predict the drug-likeness, pharmacokinetics, and binding properties of the compounds, in silico analysis was conducted. Ergosta-2,24-dien-26-oicacid,18-(acetyloxy)-5,6-epoxy-4, 22-dihydroxy-1-oxo-,delta.-lactone-4.beta., displayed the highest docking scores for acetylcholinesterase, butyrylcholinesterases, alpha-amylase, and nuclear factor-kB with values of -12.4, -10.9, -10.3, and -9.4 kcal/mol, while ergost-25-ene-6,12-dione,3,5-dihydroxy-, (3.beta.,5.alpha.) topped for cyclooxygenase-2 (-9.0 kcal/mol). The top-ranked compounds also presented significant oral drug-likeness, pharmacokinetics, and safety properties. Altogether, our data provide preclinical evidence of the potential of Hura crepitans in ameliorating diabetes and its associated complications.