| 摘要: | 金剛纂（火巷，Euphorbia neriifolia Linn) 廣泛分佈於亞洲，在民間醫學中常用於治療與炎症、糖尿病和癌症等等相關的疾病。從金剛纂莖的乙醇萃取二氯甲烷層中分離出十四個未曾報告過6/6/6/5四環三?化合物，包括十二個大戟烷型（Euphane type）四環三?化合物Neritriterpenols A-B、Neritriterpenols D-H和Neritriterpenols J-N等，以及兩個甘遂烷型(Tirucallane type)四環三?化合物Neritriterpenol C和 Neritriterpenol I，另外從乙酸乙酯層中首次分離出三個已知的甲基鞣花酸衍生物：分別為3,3',4-tri-O-methyl-4'-O-rutinosyl ellagic acid、3,3'-di-O-methylellagic acid、和 3,3',4'-tri-O-methyl ellagicacid。使用 MTT測定，結果表明，在甲基鞣花酸衍生物處理48小時後對A549和MCF-7細胞顯示出更有效的抑制作用。此外，3,3',4'-tri-O-methylellagic acid對A549 和MCF-7細胞顯示隨劑量增加導致晚期細胞凋亡更顯著分別為97%與93%。結果指出Neritriterpenols A-G三?類化合物在人類肺癌、結腸腺癌、乳腺癌和肝細胞癌中具有抗癌活性。初步SAR研究表明甘遂 烷型和大戟烷型三?類化合物在C17的側鏈上含有雙鍵或不飽和基團，會促進生物活性和加強抗癌效用。透過測量 Neritriterpenols H-N 對IL-6和TNF-α抗炎活性的抑制作用。有趣的是，Neritriterpenol H 與 Neritriterpenols J-N 對LPS誘導的IL-6表現出選擇抑制作用，Neritriterpenol I 表現出對IL-6和TNF-α抑制作用。顯示金剛纂的萃取物，具有抗發炎活性以及抑制癌症細胞株A549、MCF-7和Hep G2細胞生長及造成細胞凋亡，並通過Caspase實驗，會經由caspase-9誘導的粒線體裂變參與細胞凋亡機轉，可有效的抑制腫瘤生長並能誘導細胞株造成的凋亡現象，以達到調節保護功能。
Euphorbia neriifolia L., is widely distributed in Asia and commonly used in folk medicine to treat ailments related to inflammation, diabetes, and canc er, among others. Fourteen previously unreported 6/6/6/5 tetracyclic triter penoids were isolated from the ethanol-extracted dichloromethane layer of E. neriifolia stem, including twelve euphane type triterpenoids for Neritriter penols A-B, Neritriterpenols D-H and Neritriterpenols J-N, and two tirucallane type triterpenols Neritriterpenol C and Neritriterpenol I, in addition to three known methyl ellagic acid derivatives: 3,3',4-tri-O-methyl-4'-O-rutinosyl ellagic acid, 3,3'-di-O-methylellagic acid, and 3,3',4'-tri-O-methyl ellagic acid. Using the MTT assay, it was shown that methyl ellagic acid derivatives showed more potent inhibitory effects on A549 and MCF-7 cells after 48 hours of treatment. In addition, 3,3',4'-tri-O-methylellagic acid on A549 and MCF-7 cells showed that the dose-increased lead to late cell apoptosis was more significant, 97% and 93%, respectively. The results indicate that Neritriterpenols A-G triterpenoids have anti-cancer activity in human lung, colon adenocarcinoma, breast and hepatocellular carcinoma. Preliminary SAR studies have shown those triterpenoids contain double bonds or unsaturated groups on the side chain of C17, which will promote biological activity and enhance anti-cancer effects. Inhibition of IL-6 and TNF-α anti-inflammatory activity. Interestingly, Neritriterpenol H and Neritriterpenols J-N showed selective inhibition of IL-6. Neritriterpenol I showed inhibition of IL-6 and TNF-α. E. neriifolia extracts shown with anti-inflammatory activity and inhibits the growth and apoptosis of cancer cell lines A549, MCF-7 and Hep G2 cells. Through the Caspase experiment, it will participate in apoptosis through mitochondrial fission induced by caspase-9 which can effectively inhibit tumor growth and induce apoptosis caused by cell lines, so as to achieve the regulation and protection function. |
