In vitro and in vivo prolonged biological activities of novel vitamin C derivative, 2-O-alpha-D-glucopyranosyl-L-ascorbic acid (AA-2G), in cosmetic fields.
The biological activity of the novel vitamin C derivative, 2-O-alpha-D-glucopyranosyl-L-ascorbic acid (AA-2G), was evaluated in vitro and in vivo. The percutaneous absorption of AA-2G was determined in five Japanese males. The excretion of ascorbic acid (AA) in the subjects administered AA-2G was sustained for a longer period than in the subjects administered ascorbic acid 2-phosphate (AA-2P), which is a conventional vitamin C derivative. An analysis of the distribution of AA in the skin showed that small black specks assumed to be AA were observed in the epidermis even 3 d after applying AA-2G. The melanin synthesis in B16 melanoma cells was inhibited more by AA-2G than by AA-2P, and AA-2G also prevented more UV-induced damage of human skin keratinocytes and fibroblasts than AA-2P did. From these in vivo and in vitro results, it is supposed that the conversion of AA-2G to AA is sustained for a long time compared with that of AA-2P, and that AA-2G is an effective and available compound having vitamin C activity in human subjects.
Kumano
Y
Y
Shiseido Research Center, Yokohama, Japan.
Sakamoto
T
T
Egawa
M
M
Iwai
I
I
Tanaka
M
M
Yamamoto
I
I
D000042:Absorption; D001205:Ascorbic Acid / Q000031:analogs & derivatives* / Q000032:analysis / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D002478:Cells, Cultured; D003358:Cosmetics; D004817:Epidermis / Q000378:metabolism; D006801:Humans; D017665:Hydroxyl Radical / Q000378:metabolism; D015603:Keratinocytes / Q000187:drug effects / Q000528:radiation effects; D015227:Lipid Peroxidation / Q000187:drug effects; D008297:Male; D008543:Melanins / Q000096:biosynthesis; D008545:Melanoma / Q000378:metabolism; D012867:Skin / Q000737:chemistry / Q000378:metabolism; D013471:Sunburn / Q000517:prevention & control; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured; D014466:Ultraviolet Rays
D003358:Cosmetics; D008543:Melanins; C065378:ascorbic acid 2-O-glucoside; D017665:Hydroxyl Radical; D001205:Ascorbic Acid