González María Laura, Joray Mariana Belén, Laiolo Jerónimo, Crespo María Inés, Palacios Sara María, Ruiz Gustavo Miguel, Carpinella María Cecilia
Fine Chemical and Natural Products Laboratory, School of Chemistry, IRNASUS-CONICET, Catholic University of Córdoba, Avda. Armada Argentina 3555, X5016DHK Córdoba, Argentina.
Herbarium Marcelino Sayago, School of Agricultural Science, Catholic University of Córdoba, Avda. Armada Argentina 3555, X5016DHK Córdoba, Argentina.
Evid Based Complement Alternat Med. 2018 May 10;2018:9185935. doi: 10.1155/2018/9185935. eCollection 2018.
Plants are a significant reservoir of cytotoxic agents, including compounds with the ability to interfere with multidrug-resistant (MDR) cells. With the aim of finding promising candidates for chemotherapy, 91 native and naturalized plants collected from the central region of Argentina were screened for their cytotoxic effect toward sensitive and MDR P-glycoprotein (P-gp) overexpressing human leukemia cells by means of MTT assays. The ethanol extracts obtained from , , , , , , and presented outstanding antiproliferative activity at 50 g/mL, with inhibitory values from 93 to 100%, when tested on the acute lymphoblastic leukemia (ALL) cell line CCRF-CEM and the resistant derivative CEM-ADR5000, while 70-90% inhibition was observed against the chronic myelogenous leukemia (CML) cell K562 and its corresponding resistant subline, Lucena 1. Subsequent investigation showed these extracts to possess marked cytotoxicity with IC values ranging from 0.37 to 29.44 g/mL, with most of them being below 7 g/mL and with ALL cells, including the drug-resistant phenotype, being the most affected. extract found to be one of the most effective and bioguided fractionation yielded helenalin . The sesquiterpene lactone displayed IC values of 0.63, 0.19, 0.74, and 0.16 g/mL against K562, CCRF-CEM, Lucena 1, and CEM/ADR5000, respectively. These results support the potential of these extracts as a source of compounds for treating sensitive and multidrug-resistant leukemia cells and support compound as a lead for developing effective anticancer agents.
植物是细胞毒性剂的重要储存库，包括具有干扰多药耐药（MDR）细胞能力的化合物。为了寻找有前景的化疗候选药物，通过MTT试验，对从阿根廷中部地区收集的91种本地和归化植物进行了筛选，以检测它们对敏感和过表达MDR P-糖蛋白（P-gp）的人白血病细胞的细胞毒性作用。从[植物名称1]、[植物名称2]、[植物名称3]、[植物名称4]、[植物名称5]、[植物名称6]和[植物名称7]中获得的乙醇提取物在50μg/mL时表现出出色的抗增殖活性，在急性淋巴细胞白血病（ALL）细胞系CCRF-CEM和耐药衍生物CEM-ADR5000上进行测试时，抑制值为93%至100%，而在慢性粒细胞白血病（CML）细胞K562及其相应的耐药亚系Lucena 1上观察到70-90%的抑制率。随后的研究表明，这些提取物具有显著的细胞毒性，IC50值范围为0.37至29.44μg/mL，其中大多数低于7μg/mL，并且所有细胞，包括耐药表型，受到的影响最大。[植物名称8]提取物被发现是最有效的之一，通过生物导向分级分离得到了海伦内酯。倍半萜内酯对K562、CCRF-CEM、Lucena 1和CEM/ADR5000的IC50值分别为0.63、0.19、0.74和0.16μg/mL。这些结果支持了这些提取物作为治疗敏感和多药耐药白血病细胞的化合物来源的潜力，并支持化合物[具体化合物名称]作为开发有效抗癌药物的先导化合物。
