Department of Botanical and Environmental Sciences, Guru Nanak Dev University, Amritsar, Punjab, 143005, India.
Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab, 143005, India.
BMC Complement Altern Med. 2019 Mar 25;19(1):74. doi: 10.1186/s12906-019-2482-z.
Different plant parts of Roylea cinerea (D. Don) Baill. (Lamiaceae), Clematis grata Wall. (Ranunculaceae), Cornus capitata Wall. (Cornaceae) are traditionally used in the management of diabetes and various other diseases.
The air-dried plant parts from different plants were coarsely powdered and macerated in methanol to obtain their crude extracts. The crude extracts were evaluated for their α-glucosidase inhibitory activity. On the basis of results obtained, the methanolic crude extract of Cornus capitata Wall. was further sequentially fractionated in hexane, diethyl ether, ethyl acetate, n-butanol. Fractions obtained were also evaluated for their α-glucosidase inhibitory potential. The kinetic study was performed using Lineweaver Burk plot to evaluate the type of inhibition. Furthermore, in silico analysis was also carried with active sites of the enzyme (PDB ID: 3WY1) using Autodock4.
Among all the plant extracts, Cornus capitata extract showed maximum inhibitory activity. Therefore its methanolic extract was further fractionated with the help of different solvents and the maximum activity was shown by the ethyl acetate fraction (IC 50 μg/mL). Kinetic analysis indicated that Vmax and Km were increased indicating a competitive type of inhibition. In docking studies, among different constituents known in this plant, betulinic acid showed minimum binding energy (- 10.21 kcal/mol). The kinetic and docking studies have strengthened the observation made in the present study regarding the α-glucosidase inhibitory activity of Cornus capitata.
The study provided partial evidence for pharmacological basis regarding clinical applications of Cornus capitata in the treatment of diabetes suggesting it to be a suitable candidate for the treatment of postprandial hyperglycemia.
罗雷莱属（D. Don）的不同植物部位（唇形科）、Clematis grata Wall.（毛茛科）和Cornus capitata Wall.（山茱萸科）的植物部分在传统上用于治疗糖尿病和各种其他疾病。
将不同植物的干燥植物部分粗粉化并在甲醇中浸渍以获得其粗提取物。评估粗提取物的α-葡萄糖苷酶抑制活性。根据获得的结果，进一步对 Cornus capitata Wall.的甲醇粗提取物进行正己烷、二乙醚、乙酸乙酯、正丁醇的顺序分段。还评估了获得的馏分的α-葡萄糖苷酶抑制潜力。使用 Lineweaver Burk 图进行动力学研究，以评估抑制类型。此外，还使用 Autodock4 对酶的活性部位（PDB ID：3WY1）进行了计算机模拟分析。
在所研究的所有植物提取物中，Cornus capitata 提取物显示出最大的抑制活性。因此，进一步用不同溶剂对其甲醇提取物进行分段，其中乙酸乙酯级分显示出最大活性（IC 50 μg/mL）。动力学分析表明，Vmax 和 Km 增加，表明存在竞争性抑制。在对接研究中，在所研究的植物中的不同成分中，桦木酸显示出最低的结合能（-10.21 kcal/mol）。动力学和对接研究加强了本研究中关于 Cornus capitata 的α-葡萄糖苷酶抑制活性的观察结果。
该研究为 Cornus capitata 在治疗糖尿病中的临床应用提供了部分药理学依据，表明它是治疗餐后高血糖的合适候选药物。
