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Cajamolides A-N: Cytotoxic and anti-inflammatory sesquiterpene lactones from Calea jamaicensis
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2021-09-11 , DOI: 10.1016/j.bioorg.2021.105351
Maria-Eleni Grafakou 1 , Christina Barda 2 , George A Karikas 3 , Joerg Heilmann 4 , Helen Skaltsa 2
Affiliation  

In the search for bioactive compounds from natural sources against cancer and inflammation, Calea jamaicensis (L.) L., a plant endemic to Panama, was investigated. Using multiple chromatographic steps, seventeen sesquiterpene lactones together with nine chromene derivatives were isolated from the non-polar extract of the plant. Among them, fourteen sesquiterpene lactones and three chromanes are described herein for the first time. Structure elucidation was achieved by extensive spectroscopic analysis and comparison with reported data. The isolated sesquiterpene lactones were tested against HeLa, SK-MEL-28 and HePG2 cancerous cell lines for their cytotoxic effects, as well as in the ICAM-1 assay for their anti-inflammatory potential. This study revealed strong cytotoxic agents on the one hand and strong inhibitors on the other. The compounds inhibited the TNF-α induced ICAM-1 expression on the endothelial HMEC-1 cells in a dose-dependent manner and with no toxicity observed on this non-cancerous cell line. In addition to the well-known cytotoxic activities of sesquiterpene lactones, further exploration may offer a novel therapeutic approach to cope with inflammatory diseases and the genus Calea may serve as a biobank for the isolation of potential phytopharmaceuticals, which could be utilized as leads in drug discovery and therapy.



中文翻译:

Cajamolides AN:来自 Calea jamaicensis 的细胞毒性和抗炎倍半萜内酯

在从天然来源中寻找抗癌和炎症的生物活性化合物时,Calea jamaicensis(L.) L.,一种巴拿马特有的植物,接受了调查。使用多个色谱步骤,从植物的非极性提取物中分离出 17 种倍半萜内酯和 9 种色烯衍生物。其中,14种倍半萜内酯和3种色满是本文首次描述。结构解析是通过广泛的光谱分析和与报告数据的比较来实现的。分离的倍半萜内酯针对 HeLa、SK-MEL-28 和 HePG2 癌细胞系的细胞毒性作用进行了测试,并在 ICAM-1 分析中测试了它们的抗炎潜力。该研究一方面揭示了强细胞毒剂,另一方面揭示了强抑制剂。这些化合物以剂量依赖性方式抑制内皮 HMEC-1 细胞上 TNF-α 诱导的 ICAM-1 表达,并且在该非癌细胞系上未观察到毒性。除了倍半萜内酯众所周知的细胞毒活性外,进一步的探索可能会提供一种新的治疗方法来应对炎症性疾病和属Calea可用作分离潜在植物药物的生物库,可用作药物发现和治疗的先导物。

更新日期:2021-09-27
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