Zhao Ming, Bai Liming, Toki Asami, Hasegawa Ryo, Sakai Jun-ichi, Hasegawa Toshiaki, Ogura Hirotsugu, Kataoka Takao, Bai Yuhua, Ando Mariko, Hirose Katsutoshi, Ando Masayoshi
College of Chemistry and Chemical Engineering, Qiqihar University, 30 Wenhuadajie, Qiqihar, Heilongjiang Province, China.
Chem Pharm Bull (Tokyo). 2011;59(3):371-7. doi: 10.1248/cpb.59.371.
A new cardenolide diglycoside (1) was isolated from Nerium oleander together with ten known cardenolide diglycosides 2-11. The structure of compound 1 was established on the basis of their spectroscopic data. The in vitro anti-inflammatory activity of compounds 1-11 was examined on the basis of inhibitory activity against the induction of the intercellular adhesion molecule-1 (ICAM-1). Compounds 2-5 were active at an IC(50) value of less than 0.8 µM. The cytotoxicity of compounds 1-11 was evaluated against three human cell lines normal human fibroblast cells (WI-38), malignant tumor cells induced from WI-38 (VA-13), and human liver tumor cells (HepG2). Compound 3 was active toward VA-13 cells, and compounds 2-5 were active toward HepG2 cells at IC(50) values of less than 1.3 µM. The multidrug resistance (MDR)-reversal activity of compounds 1-11 was evaluated on the basis of the amount of calcein in MDR human ovarian cancer 2780AD cells in the presence of each compound. Compounds 1 and 8 showed moderate effects on calcein accumulation.
从夹竹桃中分离出一种新的强心苷二糖苷（1）以及十种已知的强心苷二糖苷2 - 11。化合物1的结构根据其光谱数据确定。基于对细胞间黏附分子-1（ICAM - 1）诱导的抑制活性，检测了化合物1 - 11的体外抗炎活性。化合物2 - 5在IC（50）值小于0.8 μM时具有活性。评估了化合物1 - 11对三种人类细胞系的细胞毒性，即正常人成纤维细胞（WI - 38）、由WI - 38诱导的恶性肿瘤细胞（VA - 13）和人肝癌细胞（HepG2）。化合物3对VA - 13细胞有活性，化合物2 - 5对HepG2细胞有活性，IC（50）值小于1.3 μM。基于在每种化合物存在下多药耐药（MDR）人卵巢癌2780AD细胞中钙黄绿素的量，评估了化合物1 - 11的多药耐药逆转活性。化合物1和8对钙黄绿素积累显示出中等效果。
