Lee Chan Woo, Park Nok Hyun, Kim Jin Woong, Um Byung Hun, Shpatov A V, Shults E E, Sorokina I V, Popov S A
Amore-Pacific Co. R&D Center, 314-1, Bora-dong, Giheung-gu, Yongin-si, Gyeonggi-Do, 446-729, Republic of Korea.
Bioorg Khim. 2012 May-Jun;38(3):374-81. doi: 10.1134/s1068162012030028.
Accessible triterpenoids of ursane and lupane series, the flavonoid dihydroquercetin and their synthetic derivatives with polar substituentss were tested in vitro for inhibition of collagenase 1 (MMP-1) in UVB irradiation assay. Ursolic acid and uvaol disuccinate were the most active inhibitors in the ursane series. In the lupane series, the best inhibition was manifested by carboxymethyl ester of betulonic acid and betulin succinates. Down- regulation of MMP-1 by dihydroquercetin and its synthetic derivatives surpassed the activity of a standard (retinoic acid).
对乌苏烷和羽扇豆烷系列中易获取的三萜类化合物、类黄酮二氢槲皮素及其带有极性取代基的合成衍生物进行了体外测试,以检测其在紫外线B照射试验中对胶原酶1(基质金属蛋白酶-1,MMP-1)的抑制作用。熊果酸和乌索酸二琥珀酸酯是乌苏烷系列中活性最强的抑制剂。在羽扇豆烷系列中,桦木酸羧甲基酯和桦木醇琥珀酸酯表现出最佳的抑制作用。二氢槲皮素及其合成衍生物对MMP-1的下调作用超过了标准品(视黄酸)的活性。