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通过计算机模拟和体内试验分析角鲨烯的降血糖活性。

Analysis of Antidiabetic Activity of Squalene via In Silico and In Vivo Assay.

机构信息

Department of Pharmacology and Therapeutic, Faculty of Medicine, Universitas Sumatera Utara, Medan 20155, Sumatera Utara, Indonesia.

Department of Pharmacology, Faculty of Pharmacy, Universitas Sumatera Utara, Medan 20155, Sumatera Utara, Indonesia.

出版信息

Molecules. 2023 Apr 27;28(9):3783. doi: 10.3390/molecules28093783.

Abstract

Squalene has been tested widely in pharmacological activity including anticancer, antiinflammatory, antioxidant, and antidiabetic properties. This study aims to examine antidiabetic activity of squalene in silico and in vivo models. In the in silico model, the PASS server was used to evaluate squalene antidiabetic properties. Meanwhile, the in vivo model was conducted on a Type 2 Diabetes Mellitus (T2DM) with the rats separated into three groups. These include squalene (160 mg/kgbw), metformin (45 mg/kgbw), and diabetic control (DC) (aquades 10 mL/kgbw) administered once daily for 14 days. Fasting Blood Glucose Level (FBGL), Dipeptidyl Peptidase IV (DPPIV), leptin, and Superoxide Dismutase (SOD) activity were measured to analysis antidiabetic and antioxidant activity. Additionally, the pancreas was analysed through histopathology to examine the islet cell. The results showed that in silico analysis supported squalene antidiabetic potential. In vivo experiment demonstrated that squalene decreased FBGL levels to 134.40 ± 16.95 mg/dL. The highest DPPIV level was in diabetic control- (61.26 ± 15.06 ng/mL), while squalene group showed the lowest level (44.09 ± 5.29 ng/mL). Both metformin and squalene groups showed minor pancreatic rupture on histopathology. Leptin levels were significantly higher ( < 0.05) in diabetic control group (15.39 ± 1.77 ng/mL) than both squalene- (13.86 ± 0.47 ng/mL) and metformin-treated groups (9.22 ± 0.84 ng/mL). SOD activity were higher in both squalene- and metformin-treated group, particularly 22.42 ± 0.27 U/mL and 22.81 ± 0.08 U/mL than in diabetic control (21.88 ± 0.97 U/mL). In conclusion, in silico and in vivo experiments provide evidence of squalene antidiabetic and antioxidant properties.

摘要

角鲨烯在药理学活性方面进行了广泛的测试,包括抗癌、抗炎、抗氧化和抗糖尿病特性。本研究旨在体内和体内模型中检查角鲨烯的抗糖尿病活性。在体内模型中,使用 PASS 服务器评估角鲨烯的抗糖尿病特性。同时,将糖尿病模型分为三组,即角鲨烯(160mg/kgbw)、二甲双胍(45mg/kgbw)和糖尿病对照组(10mL/kgbw 水),每天给药一次,共 14 天。测量空腹血糖水平(FBGL)、二肽基肽酶 IV(DPPIV)、瘦素和超氧化物歧化酶(SOD)活性,以分析抗糖尿病和抗氧化活性。此外,通过组织病理学分析胰腺,检查胰岛细胞。结果表明,体内分析支持角鲨烯的抗糖尿病潜力。体内实验表明,角鲨烯可将 FBGL 水平降低至 134.40±16.95mg/dL。DPPIV 水平最高的是糖尿病对照组(61.26±15.06ng/mL),而角鲨烯组最低(44.09±5.29ng/mL)。二甲双胍和角鲨烯组的组织病理学均显示胰腺破裂较小。瘦素水平在糖尿病对照组(15.39±1.77ng/mL)明显高于角鲨烯组(13.86±0.47ng/mL)和二甲双胍组(9.22±0.84ng/mL)(<0.05)。SOD 活性在角鲨烯和二甲双胍治疗组中均较高,尤其是 22.42±0.27U/mL 和 22.81±0.08U/mL,高于糖尿病对照组(21.88±0.97U/mL)。总之,体内和体内实验为角鲨烯的抗糖尿病和抗氧化特性提供了证据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17c/10180456/5084bf64c376/molecules-28-03783-g001.jpg

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