Singh Monika, Sachdeva Monika, Kumar Nitin
Department of Pharmacology, I.T.S. College of Pharmacy, Ghaziabad, U.P., Affiliated with Dr. A.P.J. Abdul Kalam Technical University, Lucknow, India.
Department of Pharmacy, Raj Kumar Goel Institute of Technology, Ghaziabad U.P., Affiliated with Dr. A.P.J. Abdul Kalam Technical University, Lucknow, India.
Curr Pharm Biotechnol. 2025;26(5):778-794. doi: 10.2174/0113892010314594240816050240.
This study aimed to determine the phytoconstituents of Crateva religiosa bark (CRB) and evaluate the hypolipidemic effect of bioactive CRB extract by preventing adipocyte differentiation and lipogenesis.
After performing the preliminary phytochemicals screening, the antioxidant activity of CRB extracts was determined through a DPPH (2, 2-diphenyl-1-picrylhydrazyl) assay. Ethyl acetate extract (CREAE) and ethanol extract (CRETE) of CRB were selected for chromatographic evaluation.
The antihyperlipidemic potential was analyzed by molecular docking through the PKCMS software platform. Further, a 3T3-L1 cell line study sulforhodamine B assay and western blotting was performed to confirm the prevention of adipocyte differentiation and lipogenesis.
The total phenolic contents in CREAE and CRETE were estimated as 29.47 and 81.19 μg/mg equivalent to gallic acid, respectively. The total flavonoid content was found to be 8.78 and 49.08 μg/mg, equivalent to quercetin in CREAE and CRETE, respectively. CRETE exhibited greater scavenging activity with the IC value of 61.05 μg/ mL. GC-MS analysis confirmed the presence of three bioactive molecules, stigmasterol, gamma sitosterol, and lupeol, in CRETE. Molecular docking studies predicted that the bioactive molecules interact with HMG-CoA reductase, PPARγ, and CCAAT/EBP, which are responsible for lipid metabolism. In vitro, Sulforhodamine B assays revealed that CRETE dose-dependently reduced cell differentiation and viability. Cellular staining using 'Oil Red O' revealed a decreased lipid content in the CRETE-treated cell lines. CRETE significantly inhibited the induction of PPARγ and CCAAT/EBP expression, as determined through protein expression via western blotting.
The influence of CRETE on lipid metabolism in 3T3-L1 cells is potentially suggesting a new approach to managing hyperlipidemia.
本研究旨在确定十字花科植物树波罗树皮（CRB）的植物成分，并通过预防脂肪细胞分化和脂肪生成来评估具有生物活性的CRB提取物的降血脂作用。
在进行初步的植物化学物质筛选后，通过DPPH（2,2-二苯基-1-苦基肼）测定法测定了CRB提取物的抗氧化活性。选择CRB的乙酸乙酯提取物（CREAE）和乙醇提取物（CRETE）进行色谱评估。
通过PKCMS软件平台进行分子对接分析抗高血脂潜力。此外，进行了3T3-L1细胞系研究、磺基罗丹明B测定和蛋白质免疫印迹，以确认对脂肪细胞分化和脂肪生成的预防作用。
CREAE和CRETE中的总酚含量分别估计为29.47和81.19μg/mg，相当于没食子酸。发现总黄酮含量分别为8.78和49.08μg/mg，相当于CREAE和CRETE中的槲皮素。CRETE表现出更强的清除活性，IC值为61.05μg/mL。气相色谱-质谱分析证实CRETE中存在三种生物活性分子，豆甾醇、γ-谷甾醇和羽扇豆醇。分子对接研究预测，这些生物活性分子与负责脂质代谢的HMG-CoA还原酶、PPARγ和CCAAT/EBP相互作用。在体外，磺基罗丹明B测定显示CRETE剂量依赖性地降低细胞分化和活力。使用“油红O”进行的细胞染色显示，CRETE处理的细胞系中脂质含量降低。通过蛋白质免疫印迹法测定，CRETE显著抑制PPARγ和CCAAT/EBP表达的诱导。
CRETE对3T3-L1细胞脂质代谢的影响可能为管理高脂血症提供一种新方法。
