کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1356554 | 981130 | 2009 | 7 صفحه PDF | دانلود رایگان |
Six 1,3-diphenylpropanes exhibiting inhibitory activities against both the monophenolase and diphenolase actions of tyrosinase were isolated from the methanol (95%) extract of Broussonetia kazinoki. These compounds, 1–6, were identified as kazinol C (1), D (2), F (3), broussonin C (4), kazinol S (5) and kazinol T (6). The latter two species (5 and 6) emerged to be new 1,3-diphenylpropanes which we fully spectroscopically characterized. The IC50 values of compounds (1, 3–5) for monophenolase inhibition were determined to range between 0.43 and 17.9 μM. Compounds 1 and 3–5 also inhibited diphenolase significantly with IC50 values of 22.8, 1.7, 0.57, and 26.9 μM, respectively. All four active tyrosinase inhibitors (1, 3–5) were competitive inhibitors. Interestigly they all mainfested simple reversible slow-binding inhibition against diphenolase. The most potent inhibitor, compound 4 diplayed the following kinetic parameters k3 = 0.0993 μM−1 min−1, k4 = 0.0048 min-1, and Kiapp = 0.0485 μM.
Extract of Broussonetia kazinoki gave six tyrosinase inhibitory 1,3-diphenylpropanes which showed simple reversible slow-binding inhibition against diphenolase.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 1, 1 January 2009, Pages 35–41