title: Effects of hydroquinone and its glucoside derivatives on melanogenesis and antioxidation: Biosafety as skin whitening agents.
abstract: OBJECTIVE
  The biosafety of hydroquinone and its derivatives as skin whitening agent remains controversial. Here, we investigated the effects of hydroquinone, arbutin, and deoxyarbutin (d-arb) on melanogenesis and antioxidation using cultured melan-a melanocytes in the presence or absence of ultraviolet A (UVA)-induced oxidative stress and determined whether d-arb enables to be an alterative to hydroquinone and arbutin for skin whitening use.
  
  
  METHODS
  d-arb was synthesized in this study by removing all hydroxyl groups from the glucose side-chain of arbutin. Tyrosinase activity was measured by (14)C-tyrosine incorporation, the intracellular reactive oxygen species (ROS) level was monitored by H(2)DCFDA fluorescence labeling, and the cell viability was determined by MTT assay in murine melan-a melanocytes treated with hydroquinone, arbutin and deoxyarbutin in the presence or absence of UVA-induced oxidative stress.
  
  
  RESULTS
  The cytotoxicity of hydroquinone and arbutin except for d-arb was increased while the cells exposed to a nontoxic dose (3J/cm(2)) of UVA irradiation. Suppressed ROS generation was noted by the treatment of d-arb to compare with arbutin and hydroquinone. All three compounds had a similar inhibition on tyrosinase activity in dose-dependent manners with two- to three-fold decreases over the untreated control. There was no change in expression of tyrosinase protein in cells treated with arbutin or hydroquinone, but a decreased protein expression of tyrosinase was seen in deoxyarbutin-treated cells.
  
  
  CONCLUSIONS
  Deoxyarbutin exerts potent tyrosinase inhibition, lessened cytotoxicity, and certain antioxidation potential, may serve as an effective and safe alternative to hydroquinone for use in skin whitening.
authors: Department of Dermatology, Renmin Hospital of Wuhan University, China.
authors: Zhi-Ming
authors: ZM
authors: Hu
authors: Qiong
authors: Q
authors: Zhou
authors: Tie-Chi
authors: TC
authors: Lei
authors: Shen-Feng
authors: SF
authors: Ding
authors: Shi-Zheng
authors: SZ
authors: Xu
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000494:pharmacology; D001104:Arbutin / Q000031:analogs & derivatives / Q000494:pharmacology; D002460:Cell Line; D006873:Hydroquinones / Q000494:pharmacology*; D008543:Melanins / Q000096:biosynthesis*; D008544:Melanocytes / Q000187:drug effects* / Q000378:metabolism / Q000528:radiation effects; D051379:Mice; D008810:Mice, Inbred C57BL; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors / Q000378:metabolism; D018384:Oxidative Stress / Q000187:drug effects* / Q000502:physiology; D017382:Reactive Oxygen Species / Q000037:antagonists & inhibitors / Q000378:metabolism*; D012880:Skin Pigmentation / Q000187:drug effects* / Q000502:physiology; D014466:Ultraviolet Rays / Q000009:adverse effects
chemical_list: D000975:Antioxidants; D006873:Hydroquinones; D008543:Melanins; D017382:Reactive Oxygen Species; D001104:Arbutin; D014442:Monophenol Monooxygenase; C504954:deoxyarbutin; C031927:hydroquinone