Inhibitory effects of 5-chloroacetyl-2-piperidino-1,3-selenazole, a novel selenium-containing compound, on skin melanin biosynthesis.
OBJECTIVE
Increased production and accumulation of melanin leads to many hyperpigmentation disorders such as melasma, freckles and geriatric pigment spots. Thus, there is a need for the development of depigmenting agents. Based on our previous reports, selenium derivatives as anti-melanogenic lead compounds could be very important. The aim of this study was to investigate the depigmenting effect of novel selenium-containing compounds.


METHODS
The inhibitory effects of 5-chloroacetyl-2-piperidino-1,3-selenazole (CS1), a novel selenium-containing compound, on melanogenesis were investigated in B16F10 melanoma cells and cultured brownish guinea pig skin tissue with alpha-melanocyte-stimulating hormone stimulation.


RESULTS
We found that CS1 inhibited melanin production in B16F10 cells by suppressing tyrosinase activity and its protein expression. In addition, Western blotting analysis revealed that CS1 suppressed the expression of tyrosinase-related protein (TRP)-1 and TRP-2. Therefore, the depigmenting effect of CS1 might have been due to inhibition of tyrosinase activity and expression of melanogenic enzymes. Furthermore, CS1 had inhibitory effects on melanin biosynthesis of primary cultured skin of brownish guinea pig.


CONCLUSIONS
The results suggested that CS1 could be a useful candidate for the treatment of skin hyperpigmentation.
Lee
Eunjoo H
EH
Graduate School of East-West Medical Science, Kyung Hee University, Yongin-si, Gyeonggi-do, Republic of Korea.
Lim
Yu-Ji
YJ
Ha
Sang Keun
SK
Kang
Tong Ho
TH
Koketsu
Mamoru
M
Kang
Chulhun
C
Kim
Sun Yeou
SY
Park
Ji-Ho
JH
D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D015536:Down-Regulation / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005656:Fungal Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D006168:Guinea Pigs; D017495:Hyperpigmentation / Q000188:drug therapy; D019746:Intramolecular Oxidoreductases / Q000378:metabolism; D008543:Melanins / Q000096:biosynthesis* / Q000378:metabolism; D008545:Melanoma / Q000201:enzymology / Q000378:metabolism; D008562:Membrane Glycoproteins / Q000378:metabolism; D051379:Mice; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors / Q000378:metabolism; D009924:Organ Culture Techniques; D016566:Organoselenium Compounds / Q000494:pharmacology*; D009994:Osmolar Concentration; D010088:Oxidoreductases / Q000378:metabolism; D018036:Selenium Compounds / Q000494:pharmacology; D012867:Skin / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D014407:Tumor Cells, Cultured; D000521:alpha-MSH / Q000494:pharmacology
C551990:5-chloroacetyl-2-piperidino-1,3-selenazole; D004791:Enzyme Inhibitors; D005656:Fungal Proteins; D008543:Melanins; D008562:Membrane Glycoproteins; D016566:Organoselenium Compounds; D018036:Selenium Compounds; D000521:alpha-MSH; D010088:Oxidoreductases; C079621:Tyrp1 protein, mouse; D014442:Monophenol Monooxygenase; D019746:Intramolecular Oxidoreductases; C042501:dopachrome isomerase