Al Rabani Hamida K M, Khan Ajmal, Rizvi Tania Shamim, Ali Liaqat, Hussain Javid, Mabood Fazal, Halim Sobia Ahsan, Khalid Asaad, Al-Harrasi Ahmed
Department of Biological Sciences and Chemistry, University of Nizwa, Nizwa-616, Sultanate of Oman.
Natural and Medical Sciences Research Center, University of Nizwa, Nizwa-616, Sultanate of Oman.
Curr Top Med Chem. 2025;25(3):311-317. doi: 10.2174/0115680266318007240924174634.
The aim of the current study was to explore the anti-diabetic potential of .
All the fractions of were evaluated for α-glucosidase inhibition, followed by bioassay-guided isolation which resulted in a new sesquiterpenoid, as a potential α-glucosidase inhibitor.
The preliminary screening showed that all the fractions including -hexane (38.0 ± 1.38 μg/mL), dichloromethane (92.6 ± 6.18 μg/mL), ethyl acetate (29.2 ± 0.51 μg/mL) and -butanol (361.8 ± 5.80 μg/mL) displayed significant α-glucosidase inhibitory activity. The activity-directed fractionation and purification of ethyl acetate fraction led to the isolation of one new sesquiterpenoid, Jardenol (1), and two known metabolites: -stitosterol-3--glucopyranoside (2) and β-Sitosterol (3). To the best of our knowledge, these metabolites have not been isolated from this plant previously. The structure of the new metabolite 1 was confirmed through 1D and 2D NMR spectroscopy, and MS analysis. Compound 1 showed significant α-glucosidase inhibition with an IC value of 138.2 ± 2.43 μg/mL as compared to positive control acarbose (IC = 942.0 ± 0.60 μg/mL). Additionally, in-silico docking was employed to predict the binding mechanism of compound 1 in the active site of the target enzyme, α-glucosidase. The docking results suggested that the compound forms strong interactions at the catalytic site of α-glucosidase.
The results of the present study indicated that the newly purified secondary metabolite, Jardenol, can be a promising anti-diabetic compound.
本研究旨在探索……的抗糖尿病潜力。
对……的所有馏分进行α-葡萄糖苷酶抑制活性评估，随后通过生物活性导向分离得到一种新的倍半萜类化合物，作为潜在的α-葡萄糖苷酶抑制剂。
初步筛选表明，所有馏分，包括正己烷（38.0±1.38μg/mL）、二氯甲烷（92.6±6.18μg/mL）、乙酸乙酯（29.2±0.51μg/mL）和正丁醇（361.8±5.80μg/mL）均表现出显著的α-葡萄糖苷酶抑制活性。对乙酸乙酯馏分进行活性导向的分级分离和纯化，得到一种新的倍半萜类化合物Jardenol（1）以及两种已知代谢产物：豆甾醇-3-O-β-葡萄糖苷（2）和β-谷甾醇（3）。据我们所知，这些代谢产物此前未曾从该植物中分离得到。通过一维和二维核磁共振光谱以及质谱分析确定了新代谢产物1的结构。与阳性对照阿卡波糖（IC50 = 942.0±0.60μg/mL）相比，化合物1表现出显著的α-葡萄糖苷酶抑制活性，IC50值为138.2±2.43μg/mL。此外，采用计算机模拟对接来预测化合物1在靶酶α-葡萄糖苷酶活性位点的结合机制。对接结果表明该化合物在α-葡萄糖苷酶的催化位点形成了强相互作用。
本研究结果表明，新纯化的次生代谢产物Jardenol可能是一种有前景的抗糖尿病化合物。
