Department of Pharmacognosy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Batterjee Medical College, Jeddah, Saudi Arabia.
J Pharm Pharmacol. 2020 Dec;72(12):1830-1839. doi: 10.1111/jphp.13358. Epub 2020 Aug 27.
This study aimed to explore the pharmacological properties of pinoresinol-4-O-β-D-glucopyranoside (PG), isolated from prunes.
In-vitro antioxidant activity was assessed using ferric reducing antioxidant power (FRAP) and 2,2'-azino-bis [3-ethylbenzothiazoline-6-sulfonic acid]-diammonium salt (ABTS) assays. In-vivo hepatoprotective activity was evaluated using CCl -induced hepatotoxicity mouse model. The antihyperglycaemic activity was determined in vitro using α-glucosidase and α-amylase inhibiting activity and in vivo using streptozotocin-treated model. Molecular modelling was done on α-amylase, α-glucosidase, aldose reductase and peroxisome proliferator-activated receptor gamma.
Pinoresinol-4-O-β-D-glucopyranoside showed promising antioxidant activity in FRAP and ABTS assays with total antioxidant capacity equal 418.47 and 1091.3 µmol/g in terms of ascorbic acid, respectively. PG (50 mg/kg b.w.) exhibited a hepatoprotective activity in vivo as it lowered AST and ALT levels. PG showed a potent in-vitro antihyperglycaemic activity as it inhibited α-glucosidase with an IC value of 48.13 μg/ml. PG caused a prominent decline in serum glucose level by 37.83% in streptozotocin-treated mice with promising elevation in insulin level of 25.37%. Oxidative stress markers were reduced by PG, and it showed a high fitting on α-amylase and α-glucosidase active sites.
Pinoresinol-4-O-β-D-glucopyranoside is a natural entity combating oxidative stress, hepatic damage and diabetes.
本研究旨在探索从李脯中分离得到的松脂醇-4-O-β-D-吡喃葡萄糖苷(PG)的药理学特性。
采用铁还原抗氧化能力(FRAP)和 2,2'-联氮-双(3-乙基苯并噻唑啉-6-磺酸)-二铵盐(ABTS)测定法评估体外抗氧化活性。采用 CCl 诱导的肝损伤小鼠模型评价体内肝保护活性。采用α-葡萄糖苷酶和α-淀粉酶抑制活性的体外法和链脲佐菌素处理模型的体内法测定降血糖活性。采用分子对接方法对α-淀粉酶、α-葡萄糖苷酶、醛糖还原酶和过氧化物酶体增殖物激活受体γ进行研究。
松脂醇-4-O-β-D-吡喃葡萄糖苷在 FRAP 和 ABTS 测定中表现出有前景的抗氧化活性,其总抗氧化能力分别相当于抗坏血酸的 418.47 和 1091.3µmol/g。PG(50mg/kg b.w.)在体内表现出肝保护活性,因为它降低了 AST 和 ALT 水平。PG 在体外表现出很强的降血糖活性,因为它抑制α-葡萄糖苷酶的 IC 值为 48.13μg/ml。PG 使链脲佐菌素处理的小鼠的血清葡萄糖水平显著降低了 37.83%,同时胰岛素水平升高了 25.37%。PG 降低了氧化应激标志物的水平,并在α-淀粉酶和α-葡萄糖苷酶的活性部位具有很高的拟合度。
松脂醇-4-O-β-D-吡喃葡萄糖苷是一种对抗氧化应激、肝损伤和糖尿病的天然物质。