Department of Chemistry, Faculty of Art and Science, University of Petra, Amman961343, Jordan.
Faculty of Medicine, The University of Jordan, Amman11942, Jordan.
Z Naturforsch C J Biosci. 2021 Mar 29;76(5-6):243-250. doi: 10.1515/znc-2020-0281. Print 2021 May 26.
Column chromatography (CC) analysis of methanol and butanol extracts of the aerial parts of well as the methanol extract of its latex, led to the isolation of cardenolides, of which the structures were elucidated by NMR and HRESIMS spectroscopy. They also revealed several triterpenes and flavonoid glycoside. Based on the antiproliferative activity reported for cardenolides, the activity of calotropin and calotoxin was tested against two common cancer cell lines, human triple-negative breast cancer cell line (MDA-MB-231) and human lung adenocarcinoma cell line (A549). The high toxicity of the latex also encouraged performing the same test on the same cancer cell lines. The anti-proliferative activity of calotropin and calotoxin was compared to the methanol extract and the wax of the latex. The results showed that calotropin and calotoxin have significant cytotoxicity against MDA-MB-231 and A549 cell lines ranging from 0.046 to 0.072 μM compared to the methanol extract and the wax of its latex ranging from 0.47 to 58.41 μM. Moreover, the results showed lower toxicity of all treatments to the human skin fibroblasts compared to the toxicity to both MDA-MB-231 and A549 cancer cells lines except the higher toxicity of Methanolic extracts of latex to the MDA-MB-231 cells. In conclusion, is a medicinal plant with a wide spectrum of cardinolides including calotropin and calotoxin, which are promising agents for targeted cancer phytotherapy.
柱层析（CC）分析甲醇和正丁醇提取物以及其乳汁的甲醇提取物，导致分离出强心苷，其结构通过 NMR 和 HRESIMS 光谱阐明。它们还揭示了几种三萜和黄酮糖苷。基于报道的强心苷的抗增殖活性，对 calotropin 和 calotoxin 的活性进行了测试，以对抗两种常见的癌细胞系，人三阴性乳腺癌细胞系（MDA-MB-231）和人肺腺癌细胞系（A549）。乳胶的高毒性也鼓励在相同的癌细胞系上进行相同的测试。calotropin 和 calotoxin 的抗增殖活性与甲醇提取物和乳胶的蜡进行了比较。结果表明，calotropin 和 calotoxin 对 MDA-MB-231 和 A549 细胞系具有显著的细胞毒性，其范围从 0.046 到 0.072 μM，而甲醇提取物和乳胶的蜡的范围从 0.47 到 58.41 μM。此外，与 MDA-MB-231 和 A549 癌细胞系相比，所有处理对人皮肤成纤维细胞的毒性较低，除了乳胶的甲醇提取物对 MDA-MB-231 细胞的毒性更高。总之，是一种具有广泛强心苷的药用植物，包括 calotropin 和 calotoxin，它们是针对癌症植物疗法的有前途的药物。
