Pharmacology and Toxicology Department, Faculty of Pharmacy, Zagazig University, Egypt.
Pharmacognosy Department, University of Sana'a, Pharmacy College, Yemen.
J Ethnopharmacol. 2023 Jun 12;309:116310. doi: 10.1016/j.jep.2023.116310. Epub 2023 Feb 28.
Aloe vera (L.) Burm.f. is widely used in various traditional systems of medicine worldwide. Since over 5000 years ago, several cultures have used A. vera extract medicinally for conditions ranging from diabetes to eczema. It has been shown to reduce the symptoms of diabetes by enhancing insulin secretion and protecting pancreatic islets.
This research study aimed to investigate the in-vitro antioxidant effect, the acute oral toxicity, and the possible pharmacological in-vivo anti-diabetic activity with histological examination of the pancreas of the standardized deep red A. vera flowers methanolic extracts (AVFME).
The liquid-liquid extraction procedure and TLC technique were used to investigate chemical composition. Total phenolics and flavonoids in AVFME were quantified by Folin-Ciocalteu and AlCl colorimetric methods, respectively. The present study involved evaluating the in-vitro antioxidant effect of AVFME using ascorbic acid as the reference standard, an acute oral toxicity study by using thirty-six albino rats and different concentrations of AVFME (200 mg/kg, 2, 4, 8 and 10 g/kg b.w.). Furthermore, the in-vivo anti-diabetic study was performed on alloxan-induced diabetes in rats (120 mg/kg, I.P.) and two doses of AVFME (200 and 500 mg/kg b.w., orally) were used as compared to glibenclamide (5 mg/kg, orally) as a standard hypoglycemic sulfonylurea medication. A histological examination of the pancreas was performed.
AVFME resulted in the highest phenolic content of 150.44 ± 4.62 mg gallic acid equivalent per gram (GAE/g) along with flavonoid content of 70.38 ± 0.97 mg of quercetin equivalent per gram (QE/g). An in-vitro study revealed that the antioxidant effect of AVFME was strong as ascorbic acid. The results of the in-vivo studies showed that the AVFME didn't cause any apparent toxicity signs or death in all groups at different doses which proves the safety of this extract with a wide therapeutic index. The antidiabetic activity of AVFME demonstrated a considerable drop in blood glucose levels as glibenclamide, without severe hypoglycemia or significant weight gain which is considered an advantage of AVFME over glibenclamide use. The histopathological study of pancreatic tissues confirmed the protective effect of AVFME on the pancreatic beta-cells. The extract is proposed to have antidiabetic activity through inhibition of α-amylase, α-glucosidase, and dipeptidyl peptidase IV (DPP-IV). Molecular docking studies were conducted to understand possible molecular interactions with these enzymes.
AVFME represents a promising alternative source of active constituents against diabetes mellitus (DM) based on its oral safety, antioxidant, anti-hyperglycemic activities, and pancreatic protective effects. These data revealed the antihyperglycemic activity of AVFME is mediated by pancreatic protective effects while significantly enhancing insulin secretion through increasing functioning beta cells. This suggests that AVFME has the potential as a novel antidiabetic therapy or a dietary supplement for the treatment of type 2 diabetes (T2DM).
库拉索芦荟(L.)Burm.f. 在世界范围内广泛应用于各种传统医学体系。几千年来,一些文化已经将库拉索芦荟提取物用于治疗从糖尿病到湿疹等多种疾病。它已被证明通过增强胰岛素分泌和保护胰岛来减轻糖尿病的症状。
本研究旨在研究标准化深红色库拉索芦荟花甲醇提取物(AVFME)的体外抗氧化作用、急性口服毒性以及可能的体内抗糖尿病活性,并进行胰腺组织学检查。
采用液-液萃取程序和 TLC 技术研究化学成分。AVFME 中的总酚和类黄酮分别用 Folin-Ciocalteu 和 AlCl 比色法进行定量。本研究通过使用抗坏血酸作为参考标准评估 AVFME 的体外抗氧化作用,通过使用三十六只白化大鼠和不同浓度的 AVFME(200mg/kg、2、4、8 和 10g/kg bw)进行急性口服毒性研究。此外,还在四氧嘧啶诱导的糖尿病大鼠(120mg/kg,IP)上进行了体内抗糖尿病研究,并将 200 和 500mg/kg bw 的两种 AVFME 剂量与格列本脲(5mg/kg,口服)作为标准磺酰脲类降血糖药物进行比较。对胰腺进行了组织学检查。
AVFME 的酚含量最高,为 150.44±4.62mg 没食子酸当量/克(GAE/g),类黄酮含量为 70.38±0.97mg 槲皮素当量/克(QE/g)。体外研究表明,AVFME 的抗氧化作用与抗坏血酸一样强。体内研究结果表明,AVFME 在不同剂量下均未引起任何明显的毒性迹象或死亡,证明了该提取物具有广泛的治疗指数和安全性。AVFME 的抗糖尿病活性显示出血糖水平的显著下降,与格列本脲相当,没有严重的低血糖或体重显著增加,这被认为是 AVFME 优于格列本脲使用的优势。胰腺组织的组织病理学研究证实了 AVFME 对胰岛β细胞的保护作用。该提取物被提议通过抑制α-淀粉酶、α-葡萄糖苷酶和二肽基肽酶 IV(DPP-IV)发挥抗糖尿病作用。进行了分子对接研究以了解与这些酶的可能分子相互作用。
AVFME 代表了一种有前途的抗糖尿病活性成分的替代来源,基于其口服安全性、抗氧化、抗高血糖活性和胰腺保护作用。这些数据显示,AVFME 的抗高血糖活性是通过胰腺保护作用介导的,同时通过增加功能β细胞显著增强胰岛素分泌。这表明 AVFME 具有作为新型抗糖尿病疗法或治疗 2 型糖尿病(T2DM)的饮食补充剂的潜力。