Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Biomedical Research Section, Nawah Scientific, Mokattam, Cairo, Egypt.
Sci Rep. 2019 Feb 11;9(1):1746. doi: 10.1038/s41598-018-36089-6.
Hepatocellular carcinoma (HCC) is progressively increasing tumor with lack of accurate prognosis and inadequate systemic treatment approaches. Solanum sp. (such as Solanum melongena) is a folk herb which is reported to possess anticancer properties. In a continuity for our interest in pursuing the anticancer activity of compounds isolated from the fruit peels of Solanum melongena, the HPLC profiling and ESI-MS assessment for the methanolic extract evidenced the presence of bioactive glycoalkaloids (solasonine, solasodine and solamargine). These glycoalkaloids were isolated, purified and proved to possess in vitro cytotoxicity against human liver cancer cell lines (Huh7 and HepG2). Herein, we investigated the potential mechanism of action of these compounds using DNA content flow-cytometry and apoptosis/necrosis differential anaylsis using annexin-V/FITC staining. Solasonine, solasodine and solamargine inducd significant antiproliferative effect against liver cancer cells (Huh7 and HepG2) which was attributed to cell cycle arrest at S-phase. Solamargine, solasodine and solasonine induced significant apoptosis in Huh7 cells. Only solamargine-induced cell cycle arrest, was reflected as apoptotic cell killing effect against HepG2 cells. In conclusion, glycoalkaloids derived from Solanum melongena and particularly, solamargine are promising antiproliferative agents with potential anticancer effects.
肝细胞癌 (HCC) 是一种逐渐增长的肿瘤,缺乏准确的预后和不充分的系统治疗方法。茄属植物(如茄子)是一种民间草药,据报道具有抗癌特性。为了延续我们对从茄子果皮中分离出的化合物的抗癌活性的兴趣,HPLC 分析和 ESI-MS 评估表明,该甲醇提取物中含有生物活性的糖苷生物碱(茄碱、茄啶和澳洲茄碱)。这些糖苷生物碱被分离、纯化,并被证明对人肝癌细胞系(Huh7 和 HepG2)具有体外细胞毒性。在此,我们使用 DNA 含量流式细胞术和使用 Annexin-V/FITC 染色进行凋亡/坏死差异分析,研究了这些化合物的潜在作用机制。茄碱、茄啶和澳洲茄碱对肝癌细胞(Huh7 和 HepG2)表现出显著的抗增殖作用,这归因于 S 期的细胞周期停滞。澳洲茄碱、茄啶和茄碱诱导 Huh7 细胞发生显著的细胞凋亡。只有澳洲茄碱诱导的细胞周期停滞,反映为对 HepG2 细胞的细胞凋亡杀伤作用。总之,茄属植物衍生的糖苷生物碱,特别是澳洲茄碱,是具有潜在抗癌作用的有前途的增殖抑制剂。