曲酸三肽的固相合成及其酪氨酸酶抑制活性、储存稳定性和毒性
Solid-phase synthesis of kojic acid-tripeptides and their tyrosinase inhibitory activity, storage stability, and toxicity.
作者信息
Kim Hanyoung, Choi Jaehui, Cho Jin Ku, Kim Sun Yeou, Lee Yoon-Sik
机构信息
School of Chemical Engineering, Seoul National University, Seoul 151-744, South Korea.
出版信息
Bioorg Med Chem Lett. 2004 Jun 7;14(11):2843-6. doi: 10.1016/j.bmcl.2004.03.046.
A small library of kojic acid-tripeptides (Ko-X1X2X3) was prepared by solid-phase parallel synthesis and assayed to evaluate their tyrosinase inhibitory activity. Most of the kojic acid-tripeptides showed better activities than kojic acid. Kojic acid-FWY was the best compound, and it exhibited 100-fold tyrosinase inhibitory activity compared with kojic acid. In addition, their storage stabilities were approximately 15 times higher and their toxicity was lower than that of kojic acid.
通过固相平行合成制备了一个小的曲酸-三肽库（Ko-X1X2X3），并对其进行了测定以评估它们的酪氨酸酶抑制活性。大多数曲酸-三肽显示出比曲酸更好的活性。曲酸-FWY是最佳化合物，与曲酸相比，它表现出100倍的酪氨酸酶抑制活性。此外，它们的储存稳定性约高15倍，毒性低于曲酸。
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