Department of Pharmacognosy & Chemistry of Natural Products, Faculty of Pharmacy, School of Health Sciences, National & Kapodistrian University of Athens, Greece; Chair of Pharmaceutical Biology, Faculty of Pharmacy and Chemistry, University of Regensburg, Germany.
Department of Pharmacognosy & Chemistry of Natural Products, Faculty of Pharmacy, School of Health Sciences, National & Kapodistrian University of Athens, Greece.
Bioorg Chem. 2021 Nov;116:105351. doi: 10.1016/j.bioorg.2021.105351. Epub 2021 Sep 11.
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.
在从天然来源寻找抗癌和抗炎的生物活性化合物的过程中，对巴拿马特有植物 Jamaican Calea（L.）L. 进行了研究。通过多种色谱步骤，从植物的非极性提取物中分离出十七种倍半萜内酯和九种色烯衍生物。其中，十四种倍半萜内酯和三种色烯是首次在此描述。通过广泛的光谱分析和与报道数据的比较，确定了结构。分离出的倍半萜内酯被测试对 HeLa、SK-MEL-28 和 HePG2 癌细胞系的细胞毒性作用，以及在 ICAM-1 测定中对其抗炎潜力的影响。这项研究揭示了一方面是强大的细胞毒性剂，另一方面是强大的抑制剂。这些化合物以剂量依赖的方式抑制 TNF-α 诱导的内皮 HMEC-1 细胞上的 ICAM-1 表达，并且在这种非癌细胞系上没有观察到毒性。除了倍半萜内酯众所周知的细胞毒性活性外，进一步的探索可能为应对炎症性疾病提供一种新的治疗方法，并且 Calea 属可能成为分离潜在植物药的生物库，这些植物药可以用作药物发现和治疗的先导物。
