Elhady Sameh S, Eltamany Enas E, Shaaban Amera E, Bagalagel Alaa A, Muhammad Yosra A, El-Sayed Norhan M, Ayyad Seif N, Ahmed Amal A M, Elgawish Mohamed S, Ahmed Safwat A
Department of Natural Products, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Department of Pharmacognosy, Faculty of Pharmacy, Suez Canal University, 41522 Ismailia, Egypt.
Plants (Basel). 2020 Aug 14;9(8):1031. doi: 10.3390/plants9081031.
Phytochemical study of aerial parts afforded six compounds; Intermedeol (1), 5α-hydroperoxy-β-eudesmol (2), 5,7-dihydroxy-3,3',4'-trimethoxyflavone (3), 5,7,4'-trihydroxy-3,6,3'-trimethoxyflavone (jaceidin) (4), eudesm-11,13-ene-1β,4β,7α-triol (5) and 1β,4β,7β,11-tetrahydroxyeudesmane (6). These compounds were identified based on their NMR spectral data. The isolated compounds were tested for their cytotoxicity against liver cancer cell line (HepG2) and breast cancer cell line (MCF-7). Jaceidin flavonoid (4) exhibited the highest cytotoxic effect in vitro. Therefore, both of jaceidin and extract were evaluated for their in vivo anti-tumor activity against Ehrlich's ascites carcinoma (EAC). Compared to control group, jaceidin and extract decreased the tumor weight, improved the histological picture of tumor cells, lowered the levels of VEGF and ameliorate the oxidative stress. Molecular docking and in silico studies suggested that jaceidin was a selective inhibitor of VEGF-mediated angiogenesis with excellent membrane permeability and oral bioavailability.
Intermedeol（1）、5α-氢过氧基-β-桉叶醇（2）、5,7-二羟基-3,3',4'-三甲氧基黄酮（3）、5,7,4'-三羟基-3,6,3'-三甲氧基黄酮（紫铆亭）（4）、桉叶-11,13-烯-1β,4β,7α-三醇（5）和1β,4β,7β,11-四羟基桉叶烷（6）。这些化合物是根据它们的核磁共振光谱数据鉴定出来的。对分离得到的化合物进行了针对肝癌细胞系（HepG2）和乳腺癌细胞系（MCF-7）的细胞毒性测试。紫铆亭类黄酮（4）在体外表现出最高的细胞毒性作用。因此，对紫铆亭和提取物都进行了针对艾氏腹水癌（EAC）的体内抗肿瘤活性评估。与对照组相比，紫铆亭和提取物降低了肿瘤重量，改善了肿瘤细胞的组织学图像，降低了血管内皮生长因子（VEGF）水平并减轻了氧化应激。分子对接和计算机模拟研究表明，紫铆亭是VEGF介导的血管生成的选择性抑制剂，具有出色的膜通透性和口服生物利用度。
