Dhanasekaran Sivaraman, Jeyabalan Srikanth, Choudhury Abbas Alam, Rajeswari Vijayarangan Devi, Ramanathan Gnanasambandan, Thamaraikani Tamilanban, Sekar Mahendran, Subramaniyan Vetriselvan, Shing Wong Ling
Department of Biotechnology, School of Energy Technology, Pandit Deendayal Energy University, Gandhinagar, Gujarat, India.
Department of Pharmacology, Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research, Chennai, Tamil Nadu, India.
Cell Biochem Biophys. 2025 Jun;83(2):1657-1675. doi: 10.1007/s12013-024-01575-4. Epub 2024 Oct 9.
Type 2 diabetes (T2D), also known as non-insulin-dependent diabetes mellitus, represents the prevailing manifestation of diabetes, encompassing a substantial majority of cases, ~90-95%. Plant-derived antidiabetic leads are being intensively explored due to their safety and effectiveness. The main objective of the present study is to evaluate the anti-diabetic potential of the traditional formulation Karisalai Karpam through in-vitro and in-silico investigations. The in-vitro and in-silico investigation of traditional polyherbal preparation Karisalai Karpam (KK) chooranam were performed to ascertain its inhibitory potential against α-amylase and α-glucosidase enzymes along with antioxidant (DPPH and ABTS) and phytochemical analysis. The results of enzyme inhibitory activity of KK witnessed highest activity against α-glucosidase enzyme with a percentage inhibition of 84.66 ± 2.50% (IC,187.9 ± 5.79 μg/ml) followed by moderate level of α-amylase inhibition exhibited with 72.94 ± 3.66% (IC, 241.6 ± 9.76 μg/ml). Additionally, the strongest antioxidant activity was observed in quenching DPPH (IC,154.8 ± 14.53 μg/ml) and ABTS radicals (IC,148.6 ± 29.74 μg/ml). The outcome of the molecular docking studies indicated that among the 17 compounds analysed, the lead such as acalyphin, apigenin, humulene, and indirubin exhibited a prominent binding affinity over the residual binding site of α-glucosidase. It's important to note that the catalytic site of the enzyme α-amylase is primarily occupied by amyrin, apigenin, arjunolic acid, β-sitosterol, geraniol, and tricetin. In conclusion, the formulation KK demonstrates robust alpha-glucosidase and alpha-amylase inhibitory activity. It's also worth noting that the formulation exhibits noteworthy antioxidant properties, which could provide additional health benefits. The binding mode and energies of the identified phytochemicals against the target enzymes further support the formulation's antidiabetic potential.
2型糖尿病（T2D），也称为非胰岛素依赖型糖尿病，是糖尿病的主要表现形式，占大多数病例，约90-95%。由于其安全性和有效性，植物源抗糖尿病先导物正在被深入研究。本研究的主要目的是通过体外和计算机模拟研究来评估传统制剂卡里萨莱卡尔帕姆的抗糖尿病潜力。对传统多草药制剂卡里萨莱卡尔帕姆（KK）乔拉纳姆进行了体外和计算机模拟研究，以确定其对α-淀粉酶和α-葡萄糖苷酶的抑制潜力以及抗氧化（DPPH和ABTS）和植物化学分析。KK的酶抑制活性结果显示，对α-葡萄糖苷酶的活性最高，抑制率为84.66±2.50%（IC，187.9±5.79μg/ml），其次是对α-淀粉酶的中度抑制水平，抑制率为72.94±3.66%（IC，241.6±9.76μg/ml）。此外，在淬灭DPPH（IC，154.8±14.53μg/ml）和ABTS自由基（IC，148.6±29.74μg/ml）方面观察到最强的抗氧化活性。分子对接研究结果表明，在所分析的17种化合物中，如刺萼龙葵素、芹菜素、葎草烯和靛玉红等先导物对α-葡萄糖苷酶的残余结合位点表现出显著的结合亲和力。需要注意的是，α-淀粉酶的催化位点主要被羽扇豆醇、芹菜素、熊果酸、β-谷甾醇、香叶醇和三羟基黄酮占据。总之，制剂KK表现出强大的α-葡萄糖苷酶和α-淀粉酶抑制活性。还值得注意的是，该制剂具有显著的抗氧化特性，这可能带来额外的健康益处。所鉴定的植物化学物质与靶酶的结合模式和能量进一步支持了该制剂的抗糖尿病潜力。
