|
KMID : 0043320140370020175
|
|
Archives of Pharmacal Research
2014 Volume.37 No. 2 p.175 ~ p.185
|
|
|
Inhibition of c-Kit signaling by diosmetin isolated from Chrysanthemum morifolium
|
|
Lee Seong-Jin
Jung Tae-Hoon
Kim Ho-Jeong
Jeong Dae-Young
Choi Gil-Don
Park Woo-Kyu
Kong Jae-Yang
Jin Mu-Hyun
Cho Hee-Yeong
|
|
|
Abstract
|
|
|
|
The interaction of stem cell factor (SCF) with its cognate receptor c-Kit is closely associated with the survival and maturation of melanocytes. To investigate novel depigmentation agents, we screened 2,000 plant extracts for c-Kit inhibitors to identify active small molecules by using time-resolved fluorescence enzyme assays. For the active extracts identified as inhibitors of c-Kit enzyme, we evaluated the effects of the active extracts and isolated flavonoids on c-Kit phosphorylation in MO7e/melanocytes. Anti-melanogenic activity was also examined in melanocytes and melanoderm model. The flavonoids such as diosmetin, apigenin, acacetin and luteolin isolated from Chrysanthemum morifolium were found to be active in inhibiting c-Kit both at enzyme and cellular levels. In addition, these flavonoids attenuated SCF-induced proliferation of human primary melanocytes without toxicity and suppressed ultraviolet (UV) B irradiation-mediated melanin synthesis significantly. Among the active flavonoids, diosmetin was found to inhibit SCF-induced melanogenesis in a human melanoderm model. These results strongly suggest that C. morifolium extract and diosmetin have potential to suppress SCF-/UVB-induced melanogenesis, and could be developed as anti-pigmentation agents.
|
|
|
KEYWORD
|
|
|
c-Kit, Flavonoid, Diosmetin, Depigmentation, Chrysanthemum morifolium
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
  
|