Kim Jang Hoon, Han Kyung-Sook, Lee Eun-Song, Kim Yong-Goo, Kim Yong-Il, Cheon Jae-Young, Jung Hyun-Ju, Kim Ki Mo, Lee Ik Soo
Department of Herbal Crop Research, National Institute of Horticultural & Herbal Science, RDA, Eumsung, Chungbuk 27709, Republic of Korea.
Department of Oriental Pharmacy, Wonkwang-Oriental Medicines Research Institute, Wonkwang University, Sinyong-dong, Iksan 570-749, Republic of Korea.
Int J Biol Macromol. 2024 Dec;282(Pt 2):136939. doi: 10.1016/j.ijbiomac.2024.136939. Epub 2024 Oct 28.
Tyrosinase is an enzyme involved in melanin production. To identify inhibitors of this enzyme in natural products, extracts and fractions of hemp seed husk were screened for tyrosinase inhibition. Phenylpropionamides 1-9, which were isolated from the ethyl acetate fraction, had inhibitory effects; compounds 3 and 4 had the greatest inhibitory effects. Cannabisin A (3) was a non-competitive and cannabisin B (4) was a competitive inhibitor. The binding sites and interactions of each inhibitor on tyrosinase were calculated by computational chemistry. Potential inhibitor 3 decreased the melanin content and tyrosinase activity in B16F10 melanoma cells. Therefore, cannabisin A (3) has potential as a tyrosinase inhibitor.
酪氨酸酶是一种参与黑色素生成的酶。为了鉴定天然产物中该酶的抑制剂，对麻籽壳提取物和馏分进行了酪氨酸酶抑制筛选。从乙酸乙酯馏分中分离出的苯丙酰胺1-9具有抑制作用；化合物3和4的抑制作用最强。大麻素A（3）为非竞争性抑制剂，大麻素B（4）为竞争性抑制剂。通过计算化学计算了每种抑制剂在酪氨酸酶上的结合位点和相互作用。潜在抑制剂3降低了B16F10黑色素瘤细胞中的黑色素含量和酪氨酸酶活性。因此，大麻素A（3）具有作为酪氨酸酶抑制剂的潜力。
