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来自(Wall. ex Miq.)的三萜内酯榕诺内酯的抗糖尿病活性:体外、体内和分子方法

Antidiabetic Activity of Ficusonolide, a Triterpene Lactone from (Wall. ex Miq.): , , and Approaches.

作者信息

Din Ala Ud, Khan Maria, Shah Muhammad Zahir, Rauf Abdur, Rashid Umer, Khalil Anees Ahmed, Zaman Khair, Al-Awthan Yahya S, Al-Duais Mohammed A, Bahattab Omar, Mujawah Adil A H, Muhammad Naveed

机构信息

Department of Chemistry, Bacha Khan University Charsadda, Charsadda 24420, Khyber Pakhtunkhwa, Pakistan.

Key Laboratory of Synthetic and Natural Fucntional Molecule, North West University, Xian 710127, P. R. China.

出版信息

ACS Omega. 2021 Oct 5;6(41):27351-27357. doi: 10.1021/acsomega.1c04230. eCollection 2021 Oct 19.

Abstract

Diabetes is a chronic condition which is locally managed through the stem of . To find the exact chemical constituent responsible for this activity, a triterpene lactone (ficusonolide) isolated from was studied for antidiabetic potential through the antidiabetic paradigm employing L-6 cells and an antidiabetic assay against non-insulin-dependent rats. The results on glucose uptake in the L-6 cell line indicated that ficusonolide has enhanced the uptake of glucose by 53.27% over control at a dose of 100 μg/mL, while at doses of 50 and 25 μg/mL, the glucose uptake was enhanced by 22.42 and 14.34%, respectively. The extract of (100 mg/kg) and ficusonolide (50 mg/kg) demonstrated a significant ( < 0.001) decline in streptozotocin-induced hyperglycemia of diabetic rats. Ficusonolide displayed conspicuous inhibitory activity against the molecular docking studies with proteins such as dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase subjected to molecular targets. Detailed computational and structural insights affirmed promising interactions between target proteins and ficusonolide. In conclusion, the plant and its isolated compound have significant antidiabetic activity with a possible mechanism of interaction with DPP-IV, PTP-1B, α-glucosidase, and α-amylase.

摘要

糖尿病是一种慢性疾病,可通过……的茎进行局部管理。为了找到负责此活性的确切化学成分,对从……中分离出的一种三萜内酯(榕叶内酯)进行了研究,通过使用L-6细胞的抗糖尿病范式以及针对非胰岛素依赖型大鼠的抗糖尿病测定法来评估其抗糖尿病潜力。在L-6细胞系中对葡萄糖摄取的结果表明,在100μg/mL的剂量下,榕叶内酯使葡萄糖摄取量比对照提高了53.27%,而在50和25μg/mL的剂量下,葡萄糖摄取量分别提高了22.42%和14.34%。……的提取物(100mg/kg)和榕叶内酯(50mg/kg)使糖尿病大鼠链脲佐菌素诱导的高血糖症显著(<0.001)下降。榕叶内酯对诸如二肽基肽酶-IV(DPP-IV)、蛋白酪氨酸磷酸酶1B(PTP-1B)、α-葡萄糖苷酶和α-淀粉酶等蛋白质的分子对接研究显示出明显的抑制活性。详细的计算和结构分析证实了靶蛋白与榕叶内酯之间有良好的相互作用。总之,该植物及其分离出的化合物具有显著的抗糖尿病活性,其与DPP-IV、PTP-1B、α-葡萄糖苷酶和α-淀粉酶相互作用的可能机制存在。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ca6c/8529651/ea46dfd6a21c/ao1c04230_0002.jpg

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