School of Pharmacy and Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya, Japan.
Biol Pharm Bull. 2011;34(8):1330-3. doi: 10.1248/bpb.34.1330.
Allergy-preventive activity of flower buds of Lonicera japonica THUNB. was found in the 35% EtOH extract (LJ) using an in vivo assay, The assay system uses monitoring of a decrease in blood flow (BF) in the tail vein of mice subjected to sensitization with hen-egg white lysozyme (HEL). Bioassay-guided fractionation of the 35% EtOH extract led to isolation of chlorogenic acid (1) and three known iridoid derivatives, loganin (2), secoxyloganin (3) and sweroside (4), all of which inhibited the BF decrease. This suggested that the flower buds of L. japonica and compounds isolated from them have allergy-preventive properties. The structure-activity relationship of iridoid derivatives, morroniside (5), geniposide (6), asperuloside (7), aucubin (8) and catalpol (9), were also tested using the same bioassay method. Compounds 2-5 and 9 having the sp(3) atom at C-8 showed an allergy-preventive effect, while compounds 6, 7 and 8 having a double bond at C-7, C-8 did not.
采用体内试验发现，金银花花蕾的 35%乙醇提取物（LJ）具有抗过敏活性。该试验系统采用监测卵清溶菌酶（HEL）致敏小鼠尾静脉血流量（BF）的降低来进行。35%乙醇提取物的生物活性导向分离得到绿原酸（1）和三种已知的环烯醚萜苷类衍生物，即獐牙菜苦苷（2）、龙胆苦苷（3）和梓醇苷（4），它们均能抑制 BF 的降低。这表明金银花花蕾及其分离得到的化合物具有抗过敏活性。采用相同的生物测定方法还测试了环烯醚萜苷类化合物莫诺苷（5）、京尼平苷（6）、獐牙菜苷（7）、梓醇（8）和毛蕊花糖苷（9）的结构-活性关系。具有 sp(3)原子在 C-8 位的化合物 2-5 和 9 表现出抗过敏作用，而具有 C-7、C-8 位双键的化合物 6、7 和 8 则没有。
