Kojyl cinnamate ester derivatives promote adiponectin production during adipogenesis in human adipose tissue-derived mesenchymal stem cells.
The subcutaneous fat tissue mass gradually decreases with age, and its regulation is a strategy to develop anti-aging compounds to ameliorate the photo-aging of human skin. The adipogenesis of human adipose tissue-mesenchymal stem cells (hAT-MSCs) can be used as a model to discover novel anti-aging compounds. Cinnamomum cassia methanol extracts were identified as adipogenesis-promoting agents by natural product library screening. Cinnamates, the major chemical components of Cinnamomum cassia extracts, promoted adipogenesis in hAT-MSCs. We synthesized kojyl cinnamate ester derivatives to improve the pharmacological activity of cinnamates. Structure-activity studies of kojyl cinnamate derivatives showed that both the α,β-unsaturated carbonyl ester group and the kojic acid moiety play core roles in promoting adiponectin production during adipogenesis in hAT-MSCs. We conclude that kojyl cinnamate ester derivatives provide novel pharmacophores that can regulate adipogenesis in hAT-MSCs.
Skin Research Institute, AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do 446-729, Republic of Korea.
Ho Sik
HS
Rho
Natural Products Research Institute, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.
Soo Hyun
SH
Hong
School of Mechanical Engineering, Yonsei University, Seoul, Republic of Korea.
Jongho
J
Park
School of Mechanical Engineering, Yonsei University, Seoul, Republic of Korea.
Hyo-Il
HI
Jung
Skin Research Institute, AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do 446-729, Republic of Korea.
Young-Ho
YH
Park
Skin Research Institute, AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do 446-729, Republic of Korea.
John Hwan
JH
Lee
Skin Research Institute, AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do 446-729, Republic of Korea. Electronic address: ssshin@amorepacific.com.
Song Seok
SS
Shin
Natural Products Research Institute, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea. Electronic address: minsoo@alum.mit.edu.
Minsoo
M
Noh
D050156:Adipogenesis / Q000187:drug effects*; D052242:Adiponectin / Q000378:metabolism*; D000273:Adipose Tissue / Q000166:cytology*; D002478:Cells, Cultured; D002934:Cinnamates / Q000737:chemistry* / Q000494:pharmacology*; D004952:Esters / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D059630:Mesenchymal Stem Cells / Q000166:cytology / Q000187:drug effects*; D011753:Pyrones / Q000737:chemistry / Q000494:pharmacology
D052242:Adiponectin; D002934:Cinnamates; D004952:Esters; D011753:Pyrones; C011890:kojic acid
Adipogenesis; Cinnamic acid; Human mesenchymal stem cells; Kojyl cinnamate ester