Department of Pharmaceutical Sciences, Tohoku University Hospital, 1-1 Seiryo-machi, Aoba-ku, Sendai, Miyagi 980-8574, Japan.
J Nat Med. 2011 Jan;65(1):237-40. doi: 10.1007/s11418-010-0476-8. Epub 2010 Nov 2.
Hydrolysis of oleoside-type secoiridoid glucosides, oleuropein (1) and ligustroside (2), in the presence of β-glucosidase provided their aglycones, named (5S,8R,9S)-7-3,4-dihydroxyphenethyl elenolate (3) and (5S,8R,9S)-7-4-hydroxyphenethyl elenolate (4), respectively. The structures of 3 and 4 were identified by spectroscopic means and optical rotation measurements. Evaluation of the cytotoxic and epidermal growth factor receptor (EGFR) tyrosine kinase inhibitory activities of compounds 1-4 showed that compounds 3 and 4 exhibited moderate cytotoxicity against a disease-oriented panel of 39 human cancer cell lines in vitro, whereas compound 3 inhibited the enzyme.
在β-葡萄糖苷酶的存在下水解齐墩果烷型环烯醚萜葡萄糖苷，橄榄苦苷（1）和毛蕊花糖苷（2），分别得到它们的配基，分别命名为（5S，8R，9S）-7-3,4-二羟基苯乙基烯醇（3）和（5S，8R，9S）-7-4-羟基苯乙基烯醇（4）。通过光谱手段和旋光测量确定了 3 和 4 的结构。对化合物 1-4 的细胞毒性和表皮生长因子受体（EGFR）酪氨酸激酶抑制活性进行评估，结果表明化合物 3 和 4 对体外疾病导向的 39 个人类癌细胞系panel 具有中等的细胞毒性，而化合物 3 抑制了该酶。
