Ezzat Shahira Mohammed, Abdel Motaal Amira, El Awdan Sally Abdel Wanees
a Department of Pharmacognosy, Faculty of Pharmacy , Cairo University , Cairo , Egypt.
b Department of Pharmacology , National Research Centre , Giza , Egypt.
Pharm Biol. 2017 Dec;55(1):1931-1936. doi: 10.1080/13880209.2017.1343358.
Balanites aegyptiaca Del. (Zygophyllaceae) fruits are well-known antidiabetic drug in Egyptian folk medicine. Nevertheless, its mechanism of action is still unclear.
Searching for the possible mechanisms of action of the plant and identification of its bioactive compounds.
A bio-guided protocol based on the evaluation of α-glucosidase (AG) and aldose reductase (AR) inhibitory activities was adopted to isolate the biologically active compounds from the methanol extract (MeEx). An in vivo antidiabetic study was conducted for the active extract, fraction and compound using streptozotocin-induced diabetic male albino Wistar rats at two dose levels (100 and 200 mg/kg.b/wt) for 2 weeks.
Three compounds were isolated and identified: a sterol, (1) stigmasterol-3-O-β-d-glucopyranoside; a pregnane glucoside, (2) pregn-5-ene-3β,16β,20(R)-trio1-3-O-β-d-glucopyranoside; a furostanol saponin, (3) 26-(O-β-d-glucopyranosyl)-22-O-methylfurost-5-ene-3β,26-diol-3-O-β-d-glucopyranosyl-(1 → 4)-[α-l-rhamnopyranosyl-(1 → 2)]-β-d-glucopyranoside. Only compound 3 possessed significant AG and AR inhibitory activities (IC = 3.12 ± 0.17 and 1.04 ± 0.02 μg/mL, respectively), while compounds 1 and 2 were inactive. The in vivo antidiabetic study revealed that MeEx and furostanol saponin 3 possessed significant activities at a dose of 200 mg/kg through reducing the fasting plasma glucose level by 46.14% and 51.39%, respectively, as well as reducing the total cholesterol by 24.44% and 31.90%, respectively. Compound 3 also caused increment in insulin and C-peptide levels by 63.56% and 65%, respectively.
We presented a scientific base for using Balanites aegyptiaca, and shed the light on one of its saponins, as an antidiabetic agent in fasting and postprandial hyperglycaemia along with the improvement of diabetic complications.
埃及蒺藜(蒺藜科)果实是埃及民间医学中著名的抗糖尿病药物。然而,其作用机制仍不清楚。
探寻该植物可能的作用机制并鉴定其生物活性化合物。
采用基于α-葡萄糖苷酶(AG)和醛糖还原酶(AR)抑制活性评估的生物导向方案,从甲醇提取物(MeEx)中分离生物活性化合物。使用链脲佐菌素诱导的糖尿病雄性白化Wistar大鼠,以两种剂量水平(100和200 mg/kg体重)对活性提取物、馏分和化合物进行为期2周的体内抗糖尿病研究。
分离并鉴定出三种化合物:一种甾醇,(1)豆甾醇-3-O-β-D-吡喃葡萄糖苷;一种孕烷糖苷,(2)孕-5-烯-3β,16β,20(R)-三醇-3-O-β-D-吡喃葡萄糖苷;一种呋甾烷醇皂苷,(3)26-(O-β-D-吡喃葡萄糖基)-22-O-甲基呋甾-5-烯-3β,26-二醇-3-O-β-D-吡喃葡萄糖基-(1→4)-[α-L-鼠李吡喃糖基-(1→2)]-β-D-吡喃葡萄糖苷。只有化合物3具有显著的AG和AR抑制活性(IC分别为3.12±0.17和1.04±0.02μg/mL),而化合物1和2无活性。体内抗糖尿病研究表明,MeEx和呋甾烷醇皂苷3在200 mg/kg剂量下具有显著活性,分别使空腹血糖水平降低46.14%和51.39%,总胆固醇分别降低24.44%和31.90%。化合物3还使胰岛素和C肽水平分别升高63.56%和65%。
我们为使用埃及蒺藜提供了科学依据,并阐明了其一种皂苷作为抗糖尿病药物在空腹和餐后高血糖中的作用,以及对糖尿病并发症的改善作用。