Madeswaran Arumugam, Tamilazhagan Selvam, Mohan Sellappan
Department of Pharmacology, Karpagam College of Pharmacy, affiliated to the Tamil Nadu Dr. M.G.R. Medical University, Coimbatore, Tamil Nadu, India.
BioTechnologia (Pozn). 2024 Dec 19;105(4):355-365. doi: 10.5114/bta.2024.145256. eCollection 2024.
Colorectal cancer is one of the most prevalent malignancies worldwide and a leading cause of mortality. Chemotherapy medications are often limited in use due to issues like drug resistance, P-glycoprotein efflux, and relapse of chemotherapy. In this study, we formulated a nanosuspension with curcumin and nimbin to address these limitations and assessed its anticancer potential using molecular docking and MTT assay.
docking and ADMET analyses targeted proteins implicated in colorectal cancer, with doxorubicin as the standard. The docking studies were conducted using AutoDock 4.2, while anticancer activity was assessed through the MTT assay in HCT 116 cell lines.
docking of curcumin and nimbin showed significant interactions with target proteins compared to the standard. ADMET analysis indicated favorable Caco-2 permeability and intestinal absorption of the selected phytoconstituents. The MTT assay demonstrated concentration-dependent cell viability inhibition in HCT 116 cell lines treated with the nanosuspension, with an IC value of 30%.
The curcumin-nimbin loaded nanosuspension demonstrated promising anticancer activity against HCT 116 cell lines in both and studies. Further studies are required to evaluate the anticancer effect of curcumin-nimbin loaded nanosupension through clinical and preclinical studies for the progress of potential formulation in the treatment of colorectal cancer.
结直肠癌是全球最常见的恶性肿瘤之一,也是主要的死亡原因。由于耐药性、P-糖蛋白外排和化疗复发等问题,化疗药物的使用往往受到限制。在本研究中,我们制备了一种含有姜黄素和印楝素的纳米混悬液以解决这些局限性,并使用分子对接和MTT试验评估其抗癌潜力。
以阿霉素为标准,对与结直肠癌相关的靶向蛋白进行对接和ADMET分析。使用AutoDock 4.2进行对接研究,同时通过MTT试验在HCT 116细胞系中评估抗癌活性。
与标准相比,姜黄素和印楝素的对接显示与靶蛋白有显著相互作用。ADMET分析表明所选植物成分具有良好的Caco-2通透性和肠道吸收性。MTT试验表明,用纳米混悬液处理的HCT 116细胞系中,细胞活力受到浓度依赖性抑制,IC值为30%。
在分子对接和MTT试验中,负载姜黄素-印楝素的纳米混悬液对HCT 116细胞系均显示出有前景的抗癌活性。需要进一步研究通过临床和临床前研究来评估负载姜黄素-印楝素的纳米混悬液在结直肠癌治疗中潜在制剂进展的抗癌效果。