Department of Biomedicine and Health Informatics, Green Innovations Group (PDGIG), Faculty of Pharmacy Silpakorn University, Nakhon Pathom 73000, Thailand.
Department of Chemistry, Faculty of Science, Silpakorn University, Nakhon Pathom, 73000, Thailand.
Acta Pharm. 2024 Mar 30;74(1):67-79. doi: 10.2478/acph-2024-0004. Print 2024 Mar 1.
Although the anticancer activity of was already observed, the chemical entity responsible for this activity remained unidentified. In this study, the cytotoxic activity of two furanocoumarin compounds, .., 5-methoxy--3-(3-methyl-2,3-dihydroxybutyl)-psoralen () and 5-methoxy-3-(3-methyl-2,3-dihydroxybutyl)-psoralen diacetate () isolated from ethyl acetate fraction of (whole plant) was investigated in several cancer cell lines including HN22, MDA-MB-231, HCT116, and HT29. The results revealed that compound exhibited cytotoxic activity, particularly against colorectal cancer cell lines HCT116 and HT29. The interplay between compound and irinotecan (Iri) showed synergism against HCT116, which was analyzed by CompuSyn software. The simulation revealed that, at the molar ratio of Iri: of 1:40, the concentration predicted to achieve a 90 % inhibitory effect when used in the combination would be ~28- and ~4-fold lower than the concentration of compound and Iri, resp., when used individually. Finally, the percentage of apoptotic cells in the HCT116 line treated with the combination was markedly higher than in the cells treated with the individual agent (60 % apoptotic cells for the combination compared to 17 and 45 % for Iri and compound monotherapy, resp). In conclusion, our results identified compound as a plant-derived compound exhibiting anticancer properties that can act synergistically with Iri and warranted further research to assess the potential of this synergism for colorectal cancer treatment.
尽管已经观察到 的抗癌活性，但负责这种活性的化学实体仍然未被确定。在这项研究中，从 （全草）的乙酸乙酯部分分离得到的两种呋喃香豆素化合物...... ，5-甲氧基-3-（3-甲基-2,3-二羟基丁基）-补骨脂素（）和 5-甲氧基-3-（3-甲基-2,3-二羟基丁基）-补骨脂素二乙酸酯（）对包括 HN22、MDA-MB-231、HCT116 和 HT29 在内的几种癌细胞系的细胞毒性活性进行了研究。结果表明，化合物 表现出细胞毒性活性，特别是对结直肠癌细胞系 HCT116 和 HT29。通过 CompuSyn 软件分析，化合物 与伊立替康（Iri）之间的相互作用表现出对 HCT116 的协同作用。模拟表明，在伊立替康：化合物 的摩尔比为 1:40 时，当联合使用时，预计达到 90 %抑制作用的浓度将比单独使用时化合物 和伊立替康的浓度分别低约 28-和 4 倍。最后，用组合处理的 HCT116 系中凋亡细胞的百分比明显高于用单个药物处理的细胞（组合处理的细胞中有 60 %凋亡细胞，而单独用伊立替康和化合物处理的细胞分别有 17 %和 45 %凋亡细胞）。总之，我们的研究结果确定了化合物 是一种具有抗癌特性的植物衍生化合物，它可以与伊立替康协同作用，并进一步研究了这种协同作用在结直肠癌治疗中的潜力。
