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In vitro cytotoxic and anticlastogenic activities of saxifragifolin B and cyclamin isolated from Cyclamen persicum and Cyclamen libanoticum

机译:仙客来和仙客来分离的虎耳草素B和仙客来的体外细胞毒性和抗肿瘤活性。

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Context: The genus Cyclamen L. (Primulaceae) is rich in saponins known to have interesting biological activities.Objective: To isolate saxifragifolin B and cyclamin, two triterpene saponins, from Cyclamen libanoticum Hildebr and Cyclamen persicum Mill, and to assess their cytotoxic, clastogenic/aneugenic, and anticlastogenic effects, as well as antioxidant potential.Materials and methods: Saxifragifolin B and cyclamin were tested for their cytotoxicity against SK-BR-3, HT-29, HepG2/3A, NCI-H1299, BXPC-3, 22RV1, and normal DMEM cell lines using WST-1 assay. Their clastogenic/aneugenic activities and anticlastogenic effects against the anticancer drug mitomycin C were assessed by the in vitro micronucleus assay in CHO cells. Their antioxidant capacities were determined using Fe2+-chelating and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assays.Results: Both saponins were described for the first time in Cyclamen libanoticum. They showed strong cytotoxic activities against the tested cancer cell lines. Saxifragifolin B was found to be 56- and 37-times more active than mitomycin C against breast adenocarcinoma (SK-BR-3) and lung carcinoma (NCI-H1299), respectively. Also, saxifragifolin B did not induce micronuclei formation and prevented cells from mitomycin C clastogenic effect. Cyclamin induced a significant increase of micronucleated cells after metabolic activation with S9 mix, and did not possess any anticlastogenic activity. Both molecules exhibited low antioxidant activities as compared to reference compounds.Discussion and conclusions: This study showed the remarkable cytotoxic activity of saxifragifolin B, especially against breast adenocarcinoma and lung carcinoma and its chemoprotective activity against mitomycin C. Thus, saxifragifolin B could be suggested as a potential cytotoxic drug with a preventive effect against possible exposures to genotoxic agents.
机译:背景:仙客来(Cyclamen L.)(Primulaceae)富含已知具有有趣生物活性的皂苷目的:从仙客来(Cyclamen libanoticum Hildebr)和仙客来(Cyclamen persicum Mill)中分离出saxifragifolin B和cyclamin这两种三萜皂苷,并评估它们的细胞毒性,杀伤力材料和方法:测试了沙西fragifolin B和cyclamin对SK-BR-3,HT-29,HepG2 / 3A,NCI-H1299,BXPC-3、22RV1的细胞毒性,以及使用WST-1分析的正常DMEM细胞系。通过体外CHO细胞中的微核试验,评估了它们的抗肿瘤/促血管生成活性和抗肿瘤药丝裂霉素C的抗肿瘤作用。用Fe 2 + -螯合剂和1,1-二苯基-2-吡啶并肼基(DPPH)自由基清除法测定了它们的抗氧化能力。结果:这两种皂苷首次在仙客来中被描述。他们对测试的癌细胞系显示出强大的细胞毒活性。 Saxifragifolin B在乳腺腺癌(SK-BR-3)和肺癌(NCI-H1299)中的活性分别比丝裂霉素C高56倍和37倍。此外,虎耳草苦参素B不诱导微核形成,并且防止细胞受到丝裂霉素C的致死作用。在用S9混合物代谢激活后,Cyclamin诱导微核细胞显着增加,并且不具有任何抗成弹性的活性。讨论和结论:这项研究表明saxifragifolin B具有显着的细胞毒性活性,尤其是对乳腺癌,肺癌和对丝裂霉素C的化学保护活性。一种潜在的细胞毒性药物,具有预防可能暴露于遗传毒性剂的作用。

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