Column chromatography (CC) analysis of methanol and butanol extracts of the aerial parts of Calortopis procera as well as the methanol extract of its latex, led to the isolation of 8 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 C. procera latex to the MDA-MB-231 cells. In conclusion, C. procera is a medicinal plant with a wide spectrum of cardinolides including calotropin and calotoxin, which are promising agents for targeted cancer phytotherapy.

中文翻译：

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来自 Calortopis procera 地上部分的抗癌 Cardenolides

Calortopis procera 地上部分的甲醇和丁醇提取物以及其乳胶的甲醇提取物的柱色谱 (CC) 分析导致分离出 8 种cardenolides，其结构通过NMR 和HRESIMS 光谱进行阐明。他们还发现了几种三萜和类黄酮糖苷。基于对cardenolides 的抗增殖活性的报道，测试了calotropin 和calotoxin 对两种常见癌细胞系、人三阴性乳腺癌细胞系 (MDA-MB-231) 和人肺腺癌细胞系 (A549) 的活性。乳胶的高毒性也鼓励对相同的癌细胞系进行相同的测试。将卡洛托品和卡洛毒素的抗增殖活性与甲醇提取物和乳胶蜡进行比较。结果表明，与甲醇提取物及其乳胶蜡的范围为 0.47 至 58.41 μM 相比，calotropin 和 calotoxin 对 MDA-MB-231 和 A549 细胞系具有显着的细胞毒性，范围为 0.046 至 0.072 μM。此外，结果表明，与对 MDA-MB-231 和 A549 癌细胞系的毒性相比，所有治疗对人皮肤成纤维细胞的毒性较低，但 C. procera 乳胶的甲醇提取物对 MDA-MB-231 的毒性较高细胞。总之，C. procera 是一种药用植物，含有广泛的心内酯，包括卡洛托品和卡洛毒素，它们是靶向癌症植物疗法的有前途的药物。072 μM 与甲醇提取物及其乳胶蜡相比，范围为 0.47 至 58.41 μM。此外，结果表明，与对 MDA-MB-231 和 A549 癌细胞系的毒性相比，所有治疗对人皮肤成纤维细胞的毒性较低，但 C. procera 乳胶的甲醇提取物对 MDA-MB-231 的毒性较高细胞。总之，C. procera 是一种药用植物，含有广泛的心内酯，包括卡洛托品和卡洛毒素，它们是靶向癌症植物疗法的有前途的药物。072 μM 与甲醇提取物及其乳胶蜡相比，范围为 0.47 至 58.41 μM。此外，结果表明，与对 MDA-MB-231 和 A549 癌细胞系的毒性相比，所有治疗对人皮肤成纤维细胞的毒性较低，但 C. procera 乳胶的甲醇提取物对 MDA-MB-231 的毒性较高细胞。总之，C. procera 是一种药用植物，含有广泛的心内酯，包括卡洛托品和卡洛毒素，它们是靶向癌症植物疗法的有前途的药物。