Department of Chemical Pathology, School of Medical Sciences, Universiti Sains Malaysia Health Campus, 16150 Kubang Kerian, Kelantan, Malaysia.
BMC Complement Altern Med. 2010 Aug 5;10:42. doi: 10.1186/1472-6882-10-42.
The leaves of Strobilanthes crispus (S. crispus) which is native to the regions of Madagascar to the Malay Archipelago, are used in folk medicine for their antidiabetic, diuretic, anticancer and blood pressure lowering properties. Crude extracts of this plant have been found to be cytotoxic to human cancer cell lines and protective against chemically-induced hepatocarcinogenesis in rats. In this study, the cytotoxicity of various sub-fractions of dichloromethane extract isolated from the leaves of S. crispus was determined and the anticancer activity of one of the bioactive sub-fractions, SC/D-F9, was further analysed in breast and prostate cancer cell lines.
The dichloromethane extract of S. crispus was chromatographed on silica gel by flash column chromatography. The ability of the various sub-fractions obtained to induce cell death of MCF-7, MDA-MB-231, PC-3 and DU-145 cell lines was determined using the LDH assay. The dose-response effect and the EC50 values of the active sub-fraction, SC/D-F9, were determined. Apoptosis was detected using Annexin V antibody and propidium iodide staining and analysed by fluorescence microscopy and flow cytometry, while caspase 3/7 activity was detected using FLICA caspase inhibitor and analysed by fluorescence microscopy.
Selected sub-fractions of the dichloromethane extract induced death of MCF-7, MDA-MB-231, PC-3 and DU-145 cells. The sub-fraction SC/D-F9, consistently killed breast and prostate cancer cell lines with low EC50 values but is non-cytotoxic to the normal breast epithelial cell line, MCF-10A. SC/D-F9 displayed relatively higher cytotoxicity compared to tamoxifen, paclitaxel, docetaxel and doxorubicin. Cell death induced by SC/D-F9 occurred via apoptosis with the involvement of caspase 3 and/or 7.
A dichloromethane sub-fraction of S. crispus displayed potent anticancer activities in vitro that can be further exploited for the development of a potential therapeutic anticancer agent.
原产于马达加斯加至马来群岛地区的美丽异木棉的叶子，在民间医学中用于治疗糖尿病、利尿、抗癌和降低血压。已发现该植物的粗提取物对人癌细胞系具有细胞毒性，并可预防大鼠化学诱导的肝癌发生。在这项研究中，测定了从美丽异木棉叶中分离出的二氯甲烷提取物的各种亚馏分的细胞毒性，并进一步分析了一种生物活性亚馏分 SC/D-F9 在乳腺癌和前列腺癌细胞系中的抗癌活性。
用硅胶快速柱色谱法对美丽异木棉的二氯甲烷提取物进行色谱分离。用 LDH 测定法测定得到的各亚馏分诱导 MCF-7、MDA-MB-231、PC-3 和 DU-145 细胞系细胞死亡的能力。测定活性亚馏分 SC/D-F9 的剂量反应效应和 EC50 值。用 Annexin V 抗体和碘化丙啶染色检测细胞凋亡，并通过荧光显微镜和流式细胞术进行分析，而用 FLICA 半胱天冬酶抑制剂检测半胱天冬酶 3/7 的活性，并通过荧光显微镜进行分析。
所选二氯甲烷提取物的亚馏分诱导 MCF-7、MDA-MB-231、PC-3 和 DU-145 细胞死亡。亚馏分 SC/D-F9 一致杀死乳腺癌和前列腺癌细胞系，EC50 值较低，但对正常乳腺上皮细胞系 MCF-10A 无细胞毒性。与他莫昔芬、紫杉醇、多西他赛和阿霉素相比，SC/D-F9 显示出相对更高的细胞毒性。SC/D-F9 诱导的细胞死亡通过涉及半胱天冬酶 3 和/或 7 的细胞凋亡发生。
美丽异木棉的二氯甲烷亚馏分在体外表现出很强的抗癌活性，可以进一步开发用于潜在的抗癌治疗药物。
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