Department of Pharmaceutical Chemistry, College of Pharmacy, Najran University, Najran, Saudi Arabia.
Department of Pharmacognosy, College of Pharmacy, Najran University, Najran, Kingdom of Saudi Arabia.
BMC Complement Med Ther. 2022 Jun 13;22(1):154. doi: 10.1186/s12906-022-03639-5.
The study was planned to investigate the phytochemicals, antidiabetic and antioxidant studies of A. consanguineum.
The preliminary studies were performed on crude extract and different solvent fractions. Based on the potency, the chloroform fraction was semi-purified to phyto-fractions CHF-1 - 5. Furthermore, CHF-3 was subjected to isolation of pure compounds using column chromatography. The α-glucosidase, α-amylase and antioxidant assays (DPPH, ABTS, HO) were performed on all samples. The in-vivo experiments on compounds 1 and 2 were also performed using oral glucose tolerance test. Docking studies were performed on α-glucosidase and α-amylase targets.
Among all fractions, the chloroform fraction exhibited excellent activities profile giving IC values of 824, 55, 117, 58 and 85 μg/ml against α-glucosidase, α-amylase, DPPH, ABTS and HO targets respectively. Among the five semi-purified chloroform phyto-fractions (CHF-1-5), CHF-3 was the leading fraction in activities giving IC values of 85.54, 61.19 and 26.58 μg/ml against α-glucosidase, α-amylase and DPPH respectively. Based on the overall potency and physical amount of CHF-3, it was subjected to purification to get compounds 1 and 2. The two compounds were also found potent in in-vitro activities. The observed IC values for compound 1 were 7.93, 28.01 and 6.19 μg/ml against α-glucosidase, α-amylase and DPPH respectively. Similarly, the compound 2 exhibited IC of 14.63, 24.82 and 7.654 μg/ml against α-glucosidase, α-amylase and DPPH respectively. Compounds 1 and 2 were potent in decreasing the blood glucose levels in experimental animals. Compounds 1 and 2 also showed interactions with the respective enzymes with molecular docking.
We can conclude that A. Consanguineum is a rich source of natural antidiabetic agents. Bioguided isolation of compound 1 and 2 showed potential inhibitions in all tested in-vitro antidiabetic targets. Further, both the compounds were also able to decrease the blood glucose levels in experimental animals.
本研究旨在研究 A. consanguineum 的植物化学成分、抗糖尿病和抗氧化作用。
对粗提取物和不同溶剂级分进行初步研究。根据活性，氯仿级分被半纯化至植物级分 CHF-1-5。此外，CHF-3 还通过柱层析进行了纯化合物的分离。所有样品均进行α-葡萄糖苷酶、α-淀粉酶和抗氧化剂（DPPH、ABTS、HO）测定。还对化合物 1 和 2 进行了口服糖耐量试验的体内实验。对α-葡萄糖苷酶和α-淀粉酶靶标进行了对接研究。
在所有级分中，氯仿级分表现出极好的活性谱，对α-葡萄糖苷酶、α-淀粉酶、DPPH、ABTS 和 HO 靶标，IC 值分别为 824、55、117、58 和 85μg/ml。在五个半纯化的氯仿植物级分（CHF-1-5）中，CHF-3 是活性最强的级分，对α-葡萄糖苷酶、α-淀粉酶和 DPPH 的 IC 值分别为 85.54、61.19 和 26.58μg/ml。基于 CHF-3 的整体效力和物理量，它被纯化以获得化合物 1 和 2。这两种化合物在体外活性中也表现出很强的活性。化合物 1 的观察到的 IC 值分别为 7.93、28.01 和 6.19μg/ml，对α-葡萄糖苷酶、α-淀粉酶和 DPPH 均有抑制作用。同样，化合物 2 对α-葡萄糖苷酶、α-淀粉酶和 DPPH 的 IC 值分别为 14.63、24.82 和 7.654μg/ml。化合物 1 和 2 能有效降低实验动物的血糖水平。化合物 1 和 2 还与相应的酶进行了分子对接，表现出相互作用。
我们可以得出结论，A. Consanguineum 是天然抗糖尿病药物的丰富来源。化合物 1 和 2 的生物导向分离显示出对所有测试的体外抗糖尿病靶标有潜在的抑制作用。此外，这两种化合物都能降低实验动物的血糖水平。
