Matsuda Hisashi, Nakashima Souichi, Oda Yoshimi, Nakamura Seikou, Yoshikawa Masayuki
Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Japan.
Bioorg Med Chem. 2009 Aug 15;17(16):6048-53. doi: 10.1016/j.bmc.2009.06.057. Epub 2009 Jun 30.
The 80% aqueous acetone extract from the rhizomes of Alpinia officinarum, a Chinese medicinal herb, were found to inhibit melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells. Among the constituents isolated, four diarylheptanoids [5-hydroxy-1,7-diphenyl-3-heptanone, 7-(4('')-hydroxy-3('')-methoxyphenyl)-1-phenylhept-4-en-3-one, 5-hydroxy-7-(4('')-hydroxy-3('')-methoxyphenyl)-1-phenyl-3-heptanone, and 3,5-dihydroxy-1,7-diphenylheptane] and two flavonol constituents (kaempferide and galangin) inhibited melanogenesis with IC(50) values of 10-48microM, and several structural requirements of the active constituents for the inhibition were clarified. In addition, 7-(4('')-hydroxy-3('')-methoxyphenyl)-1-phenylhept-4-en-3-one, kaempferide, and galangin inhibited mRNA expression of tyrosinase and tyrosinase-related proteins-1 and -2, and the protein level of a microphthalmia-associated transcription factor.
中药高良姜根茎的80%丙酮水提取物被发现可抑制茶碱刺激的小鼠B16黑色素瘤4A5细胞中的黑色素生成。在所分离出的成分中，四种二芳基庚烷类化合物[5-羟基-1,7-二苯基-3-庚酮、7-(4''-羟基-3''-甲氧基苯基)-1-苯基庚-4-烯-3-酮、5-羟基-7-(4''-羟基-3''-甲氧基苯基)-1-苯基-3-庚酮和3,5-二羟基-1,7-二苯基庚烷]以及两种黄酮醇成分（山柰酚和高良姜素）抑制黑色素生成，IC(50)值为10 - 48微摩尔，并阐明了活性成分抑制作用的几个结构要求。此外，7-(4''-羟基-3''-甲氧基苯基)-1-苯基庚-4-烯-3-酮、山柰酚和高良姜素抑制酪氨酸酶、酪氨酸酶相关蛋白-1和-2的mRNA表达以及小眼畸形相关转录因子的蛋白水平。
