Penetration enhancement in mouse skin and lipolysis in adipocytes by TAT-GKH, a new cosmetic ingredient.
Since the basic domain of human immunodeficiency virus type I (HIV-1) transactivator of transcription (TAT) protein was reported to possess the ability to traverse biological membranes efficiently, various therapeutic proteins have been attached to TAT for the purpose of therapy. In this study, the tripeptide GKH (glycine-lysine-histidine) derived from parathyroid hormone (PTH), known as lipolytic peptide, was attached to 9-poly lysine (TAT) to be used as a cosmetic ingredient in slimming products. TAT-GKH at 10(-5) M induced approximately 37.6% and 41.5% maximal lipolytic effects in cultured 3T3-L1 differentiated adipocytes and in epididymal adipocytes isolated from rats, respectively, compared with basal lipolysis. The lipolytic effect of GKH was not changed by TAT-GKH fusion. In cytotoxicity tests, there was no cytotoxicity in any dose concentration of TAT-GKH. We confirmed that TAT-GKH induced lipolytic activity by GKH without cytotoxicity and with the possibility of its use as a safe cosmetic ingredient. TAT-GKH elevated penetration into excised hairless mice skin 36 times more efficiently than GKH. TAT-GKH can be used as a cosmetic ingredient in slimming products, with both penetration enhancement and lipolytic effect without cytotoxicity.
Lim
Jun Man
JM
Cosmetic R&D Center, LG Household & Healthcare Research Park 84, Jang-dong, Yusong-gu, Taejon 305-343, Korea.
Chang
Min Youl
MY
Park
Sun Gyoo
SG
Kang
Nae Gyu
NG
Song
Young Sook
YS
Lee
Young Hwa
YH
Yoo
Young Chang
YC
Cho
Wan Goo
WG
Choi
Soo Young
SY
Kang
She Hoon
SH
D017667:Adipocytes / Q000378:metabolism*; D000595:Amino Acid Sequence; D000818:Animals; D002478:Cells, Cultured; D003358:Cosmetics / Q000737:chemistry*; D008066:Lipolysis; D008297:Male; D051379:Mice; D009842:Oligopeptides / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000378:metabolism*
D003358:Cosmetics; D009842:Oligopeptides; C481804:lysyl-lysyl-lysyl-lysyl-lysyl-lysyl-lysyl-lysyl-lysyl-glycyl-lysyl-histidine