Anthraquinones from Polygonum cuspidatum as tyrosinase inhibitors for dermal use.
Four anthraquinones, physcion (1), emodin (2), citreorosein (3) and anthraglycoside B (6), and two stilbenes, resveratrol (4), and piceid (5), were isolated previously from the root of Polygonum cuspidatum. These bioactive compounds were examined for their antityrosinase potency. No antityrosinase activity was detected with treatment using stilbenes. On the other hand, the anthraquinones showed moderate to strong inhibition of tyrosinase. Physcion exhibited the most potent tyrosinase inhibition among the four anthraquinones examined, which was comparable to kojic acid. The ability of anthraquinones to permeate the skin was also examined. Based on the same thermodynamic activity, physcion showed a higher permeation compared with emodin (48-fold), suggesting it as a potent candidate for dermal use. As naturally occurring tyrosinase inhibitors, anthraquinones from P. cuspidatum may be useful as skin-whitening agents to inhibit tyrosinase for dermal use.
Leu
Yann-Lii
YL
Natural Products Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan.
Hwang
Tsong-Long
TL
Hu
Jiuan-Wen
JW
Fang
Jia-You
JY
D000818:Animals; D000880:Anthraquinones / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D020405:Dermis / Q000378:metabolism; D045468:Fallopia japonica / Q000737:chemistry*; D015394:Molecular Structure; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010455:Peptides / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D012869:Skin Absorption; D013552:Swine
D000880:Anthraquinones; D010455:Peptides; D014442:Monophenol Monooxygenase