Department of Pharmaceutical Chemistry, College of Pharmacy, Najran University, Najran, Saudi Arabia.
Department of Pharmacy, University of Swabi, Swabi, KP, Pakistan.
BMC Complement Med Ther. 2021 Oct 27;21(1):270. doi: 10.1186/s12906-021-03443-7.
Diabetes mellitus is a common disease effecting the lifestyles of majority world population. In this research work, we have embarked the potential role of crude extracts and isolated compounds of Notholirion thomsonianum for the management diabetes mellitus.
The crude extracts of N. thomsonianum were initially evaluated for α-glucosidase, α-amylase and antioxidant activities. The compounds were isolated from the activity based potent solvent fraction. The structures of isolated compounds were confirmed with NMR and MS analyses. The isolated compounds were tested for α-glucosidase, α-amylase, protein tyrosine phosphatase 1B (PTP1B) and DPPH activities. The molecular docking studies were carried out to find the binding interactions of isolated compounds for α-glucosidase, α-amylase and PTP1B.
Initially, we screened out crude extracts and subfractions of N. thomsonianum against different in-vitro targets. Among all, Nt.EtAc was observed a potent fraction among all giving IC values of 67, 70, < 0.1, 89 and 16 μg/mL against α-glucosidase, α-amylase, DPPH, ABTS and HO respectively. Three compounds (Nt01, Nt02 and Nt03) were isolated from Nt.EtAc of N. thomsonianum. The isolated compounds Nt01, Nt02 and Nt03 exhibited IC values of 58.93, 114.93 and 19.54 μM against α-glucosidase, while 56.25, 96.54 and 24.39 μM against α-amylase respectively. Comparatively, the standard acarbose observed IC values were 10.60 and 12.71 μM against α-glucosidase, α-amylase respectively. In PTP1B assay, the compounds Nt01, Nt02 and Nt03 demonstrated IC values of 12.96, 36.22 and 3.57 μM in comparison to the standard ursolic acid (IC of 3.63 μM). The isolated compounds also gave overwhelming results in DPPH assay. Molecular docking based binding interactions for α-glucosidase, α-amylase and PTP1B were also encouraging.
In the light of current results, it is obvious that N. thomsonianum is potential medicinal plant for the treatment of hyperglycemia. Overall, Nt.EtAc was dominant fraction in all in-vitro activities. Three compounds Nt01, Nt02 and Nt03 were isolated from ethyl acetate fraction. The Nt03 specifically was most potent in all in-vitro assays. The molecular docking studies supported our in-vitro results. It is concluded that N. thomsonianum is a rich source of bioactive antidiabetic compounds which can be further extended to in-vivo based experiments.
糖尿病是影响多数世界人口生活方式的常见疾病。在这项研究工作中，我们研究了角叉菜胶和分离化合物对糖尿病的潜在作用。
首先对角叉菜胶的粗提取物进行α-葡萄糖苷酶、α-淀粉酶和抗氧化活性评价。从活性基础强溶剂部分分离化合物。通过 NMR 和 MS 分析确定分离化合物的结构。对分离出的化合物进行α-葡萄糖苷酶、α-淀粉酶、蛋白酪氨酸磷酸酶 1B（PTP1B）和 DPPH 活性测试。进行分子对接研究，以发现分离化合物与α-葡萄糖苷酶、α-淀粉酶和 PTP1B 的结合相互作用。
最初，我们筛选了角叉菜胶的粗提取物和亚馏分，以对抗不同的体外靶标。其中，Nt.EtAc 是所有馏分中最有效的，对α-葡萄糖苷酶、α-淀粉酶、DPPH、ABTS 和 HO 的 IC 值分别为 67、70、<0.1、89 和 16μg/mL。从角叉菜胶的 Nt.EtAc 中分离出三种化合物（Nt01、Nt02 和 Nt03）。分离出的化合物 Nt01、Nt02 和 Nt03 对α-葡萄糖苷酶的 IC 值分别为 58.93、114.93 和 19.54μM，而对α-淀粉酶的 IC 值分别为 56.25、96.54 和 24.39μM。相比之下，标准阿卡波糖对α-葡萄糖苷酶和α-淀粉酶的 IC 值分别为 10.60 和 12.71μM。在 PTP1B 测定中，化合物 Nt01、Nt02 和 Nt03 分别表现出 12.96、36.22 和 3.57μM 的 IC 值，而标准熊果酸的 IC 值为 3.63μM。分离出的化合物在 DPPH 测定中也取得了压倒性的结果。基于分子对接的α-葡萄糖苷酶、α-淀粉酶和 PTP1B 的结合相互作用也令人鼓舞。
根据目前的结果，显然角叉菜胶是治疗高血糖的潜在药用植物。总的来说，Nt.EtAc 是所有体外活性中最主要的部分。从乙酸乙酯部分分离出三种化合物 Nt01、Nt02 和 Nt03。在所有体外试验中，Nt03 是最有效的。分子对接研究支持我们的体外结果。可以得出结论，角叉菜胶是一种丰富的具有抗糖尿病活性的化合物来源，可以进一步扩展到基于体内的实验。
