title: Design, synthesis and evaluation of PEGylated lipoic acid derivatives with functionality as potent anti-melanogenic agents.
abstract: The novel PEGylated lipoic acid (LA) derivatives with functionality were synthesized in satisfactory yield by simple procedures and evaluated about its anti-melanogenic activity on the B16F10 melanoma cells. Grafting a PEG moiety onto the carboxyl group of LA has reduced the cell cytotoxicity and provided the water solubility and functionality to incorporate the other bioactive moieties. We have found that derivatives showed inhibition of melanin formation by up to 36.5% at 0.1 mM, whereas LA decreased the melanin formation by 8.6%. In addition, it also inhibits at least 86.4% UV-induced MMP-1 expression at 0.1 mM which is higher than LA. These data suggest that the novel PEGylated LA derivatives with functionality may thus serve as a potentially effective anti-melanogenic and anti-aging agent.
authors: Department of Bionanochemistry, Wonkwang University, Iksan, Chonbuk 570-749, Republic of Korea. chichonglu@hotmail.com
authors: Chichong
authors: C
authors: Lu
authors: Bo-Mi
authors: BM
authors: Kim
authors: Kyu Yun
authors: KY
authors: Chai
mesh_terms: D000818:Animals; D002460:Cell Line; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D005786:Gene Expression Regulation / Q000187:drug effects / Q000528:radiation effects; D006801:Humans; D020781:Matrix Metalloproteinase 1 / Q000235:genetics; D008543:Melanins / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D051379:Mice; D011092:Polyethylene Glycols / Q000737:chemistry*; D008063:Thioctic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D014466:Ultraviolet Rays
chemical_list: D008543:Melanins; D011092:Polyethylene Glycols; D008063:Thioctic Acid; D020781:Matrix Metalloproteinase 1