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A61K 8197(2006.01) A61Q 19102 (2006.01) A61Q 19108 (2006.01) PCT/KR2010/002388 2010

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f"'l (54) Title: COSMETIC MATERIAL COMPOSITION

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(57) Abstract: The present invention relates to cosmetic material compositions for skin whitening or skin anti-aging containing Averrhoa bilimbi extract as an active ingredient. The active ingredient of each composition further contains selectively at least one f"'l selected from the group consisting of Gynura procumbens extract and Gynura pseudochina extract. According to the cosmetic ma"l""'"i terial composition of the present invention, skin function can be effectively improved without skin irritation through, for example, ......... enhancing skin whitening or preventing the aging of skin.

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(57) .a ~Al: i".- ~I§,'"'_ ~ '8 llj (Averrhoa bilimbi) 4-~% g_ % iL Ad~ _(J_5'_ Wt"} ';::: ILl1f- v] ~ % .:§}7:J-li 5::Ad% EE';::: ILl 4-~% f"'l 1f- iiJ--"=-.:§}% .:§}7:J-li 5::Ad%01] ~~ 3:!_(J_5'_, 5::Ad%E1 %iLAd~,'"'_ <2I'ljz-j_(J_5'_,{{*Li='4(Gynuraprocumbens) 3J q~~] '4(Gynura pseudochina) 4-~% 5'_ 0] if-oj:.a cir01P'l <2 I'lj-'8. 1 ~ 0] AJ-g_ 1:-1 W%[ 'T'- ~) q. i".- ~I§ E1 .:§}7:J-li 5::Ad%01] u] 2~, ILl1f- A}~ g_ % ~t"}A] ~_(J_~Al.£ oj] ~ ~ oj ILl1f- v] ~ ~:.a EE';::: ILl1f- -"=-.:§}lJ-A]~ ~"5B ILl1f- 7] ~ l ~ g_ iLJI}z-j_(J_5'_7B<2A]~ 'T'- ~)q.

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~ _S:_A10}Al1 (tyrosinasejj']: ';:= 1L~7} £II}-=tl ~(dopaquinone) 4 g_ A~Ad A17'1$, £II}-=tl ~ 2___s:_ E1 A}%{}:& ~ g JI} 1L~ ~ g g_ 7~~=1 :g-% W ~11 ~ 2} \::l 01 Jf<;>l A~ Ad -'8_ rt. u:}2}Ai, ~ ~~ 2___s:_ II1Jf-~ 0 1 ~ 711sq ';:= ~ g_ ~71 _<f1 il}~ ~ 2} \::l A~AdJI}fia % ~Jf-~g g_ A1-o~il}~ ~2}\::l WAdA}~11~ ~~A17'1';:= tiJ'ij01 <i1 T sq $ ~lt. 019} :Q-o1 WAd JI}fia g_ A1-O~ ';:= ~ 2___s:_ ~ ~ J±~ <;>l r il} ~?1 u1 ~~li_s:_';:= tl1Ej-"i0_C7} ~lrt.
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ingredientj.s.-"] ~

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-'8_ rt. 019} :Q-,?_ Al1 x9l 71 ~,?_ 3711

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[12]

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pseudochina) 4-~% [17] ()l4~ 4-~%JI} 4-~%~

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[J± 1]

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3J ~

w%~Pi

ll_s:_~2};W(Procollagen) ~ '-6l=ldAverrhoa bilimbi) (

A~

'o'?_ ~~Bil}u:j, %*y:9t(Gynuraprocumbens)9t ~ W -5J EB 7}:AJ"li-,?_~2};W 7}

T 7}7-1 4-~%~

WAd

g_ ~ 7}A17l ';: lLJI} ~ L}£j-~ ~ q.

[33] [34] [35] rA]~ oj] 21 %471] L1] ] ~(MMP-l)~ 0 Al~,?_ 2.5 %~ Jf-EBo} AJ%o}Allx~ l:lB °Jil}~ q.

~7;a 01 W%-tl

Ai -0]*
DMEM(Dulbecco's Modified Eagle's 70-80% ~W%~

Media) l:lB 7-17} W%-tl 96:g- IraJtl-l:lB OJ71(96-well microtiter platelv] <;>l Zl-~ 5,000 All /:g-(well) 01 sqs=.~ ~$, x

Ads=.

7-}~ u]17J}7-1

J:c.1

$ %*y:9t(Gynura B~ %~

procumbens), q~ 3%JI}

r:ll9t(Gynura pseudochina) 4%g_ 10ppm*s=._s:_

3J

~'-6l=ld(Averrhoabilimbi)

3J

24Al Zl- %<;>l- ~1:c.1 ~ AJ~ ~ _2__s:_ 01%7} #: RPN2610)~

-f-, Allx
'0 ~

l:lB 0J~ g_ ~B..<f-1 q. ~B..<f-1 All l:lB il}~ ~ x 0J~ g_

~2}711 L1l 17'- ~ 0 ~2}711L110l7'-

0l%il}~

Ad 71 T (Ul-;:;-o}~ ~II}U}Al= A}. Catalog A~Ad Ads=.~ ~Adil}~q. ~A11~}

{1_ Al il}~ q. 3Al Zl~$ ~~ qAl g_ ~~,?_

~2} 711 1l 17'- <5J 117}TI- ~ il}711s=.x -tl 96-:g- IraJtl-(96-well plate) ~l ~B..<f-1 All L0 ~ -tl x l:lB 0J~ g_ ~ $ 3Al Zl- %<;>l- <5J~ -<5J~11 g g_ <5J_g.5:~Pi ~ ~~Bol %~A17l$, xtH-~g_ 405nm~Pi ~ %s=.~ [36] [37] [38] [39] ~W-tl 2~} ~2};W

-f-

<5J~11 96-:g- IraJtl-(96-wellplate)~1 ~ % ~%~ ~g(~~)g_ ~%s=.~ ~~ %7-1A17l~ ~%111~ ~g

15~Zl- ~ g Al ~ q. 15~
qA11M~{lg_ x tH-~ g_ ~ u:j ~ g ~ ~

-f- ~~

g_ ~ ~ {1_ _g.~Pi 15~Zl- ~~

f>~ ~

Ad s=.~l 4- ~~
J

u:}2} x tH-~ ~

Ad s=.7} r] 2711 L}£j-\i-q.

°l%il}~

![l_96-:g-IraJtl-(96-wellplate)~

Ad ill $,

il}71

1~l ~ -oB~2}711 L1l 17'- ~ 0 ~JI}~

WAd Ad s=.~

111lil} ~ q. 01 u]15:Ad % g_ ~1:c.1 { il}7-1'2l,?_ r ~ ~B..<f-1-tl x l:lB ~ ~ ~ g All oJ ~5:r_2__s:_ il}~q.

f>~ il}~

J± 2~1 L}£j-~_2_u:j, Allx-&Ad g_ $?1~

* s=.~Pi Al ~ g_ ~

q. ~ %s=./~5:r~ ~ %s=.)X100

[4-~~
[J± 2]

1]

~2}711L110l7'- ~~Ads=.(%)=(%~~l:c.1Allxr~

6
WO 2010/120150

rcr IKR201

0/002388

Al~%~ l::ll),~21 ~ uv )'121 i~l Ell 9~ <±

G. procumbens G. pseudochina A. bilimbi +(2)( 1: 1) T (;)(1 : 1) :\-----",+<Q_.)'
(1)
:,

% 2} 711111 0l-:z.

l=ll-~ o-l 2. '--'--,

Al17~ C 0

__l_

(0/<) 0

100 152.4 84.3 79.4 88.1 101.5 101.6 101.9 104.6 102.5
4-~%

/2\
-

/4:
\,---/

+3)(1 : 1)

(2)

+:?i+('3{ I:. 1: 1) \')/

\~/

[40]
II

3±2_s:_Jf-El ~y

~l';: tl}9}:Q-0l, B~

3J

~W%~Pl7]~ 7}:Ad-

ull~_s:_ g_

_s:_ llo}All(MMP-1)~ E

71-O~ A]7'1';: lLJI}7} Y-Ej-Y- u:j, %*y:9}(Gynura ~W%o]

procumbens), q~T:l]9}(Gynurapseudochina)~ Y-Ej-~~q. [41] [42] [43] rAJ~ oj] 31 Melan-a cell% oJ % ~l- ~

"li-,?_ ~Ad

4~ A~ Ad Qj Al] Ira 7}
2

4 All5:B

4-~%

3J

~W%g_

A]~%~_S:_ il}~ 10 % FBS7} W%B

DMEM_2__s:_ -well plate(melanin 7a ~)~l 6 96-well plate(MTTassay)~l C02 incubator(MCO-20AIC, theophylline 0] W%B A]~%~ g_ ~7}il}~
jl

104 celllwell(final volume 3 ml), 37°C, 5%

2 X 103 cell/well (final volume 200 ul)_S:_ ~jl Sanyo)~P1

A~

24A]

Zl- l:l~°Jil}~

q. l:l~ oJ

.-f- l:l~ 7-]~

All71il} jl 10% FBS, 2 uM a-MSH(Melanocyte DMEMl:l~7-]~ 3~Zl- u~~ ~l:c.1il}~q.

stimulating hormone), 2 mM 5~~~~16-wellplate~P1l:l~oJB Chemical Co.)% ~ g_ ~1:c.1 il}~ All:±

_s:_ l:l~ ~ 7-]_s:_ A}%il} jl l:l~ 7-]~l

l:l~ 7-]~ All71il} jl 0.25% trypsin-EDTA(Sigma pellet g_ §1 yil}

1.5 ml tube.s', ~ 7~ 10,000rpm_2__s:_ 10~Zl- ~{J~:c.1 il}~ ~ ~ ~ pellet g_ 60°C~P1 A]li~

Ad- ~ ~
~~

g_ All71~q.

Z25:A] Zl.-f-

IN NaOH 100 ul ~ qg ELISAreader Ad-7] ~21\::l W~JI}

J

All:±~ ~21\::lg_ ~~q. ~ %.5:..~ ~7ail}~ ~7}il}7-] il}7] 2] All (%) ~

0] %~ g_ PBS_s:_§1~A]Zl

475nm~P1 4-~%g_ ~7ail}~q. [44] [45]

~21\::l A~Ad71-o~~g_ Til}~q.

'2l,?_

All:±~ ~5:r_2__s:_ il}~ ~5:r~P1~

tll JJl il}~ {1_ ~ %~ ~ ~

4 \::l A~ Ad

71-O~ 7a.5:..~ ~ 7a il}~ ul ~ lLJI} ~

y~~
=

1~1 U:}21~21\::l

A~Ad

~All~g_

Jjl{}il}~

~JI}~

3±

3~1 Y-Ej-~~q.

[y~~
~

4 \::lA~ Ad ~

100

(4A]~

%~ ~ ~ % .5:../~ 5:r

~ ~ %.5:..X 100)

7
WO 2010/120150

rcr IKR201
A~

0/002388

[46] [47]

[3:i 3] ~ 2} \::l

Ad ~ A111LJI}
7-1
.x_ c

!-1c5i L-' LI22

l~

2)- \:l

)'1-1 ),1 oo

/'1 o~%(%

O --"-

control)

l::l1,~21 ~ )
J_'_

tI

~17}
\'

42.3% 67.8% 48.5% 42.4% 31.7% 49.3% 47.5% 39.6% 58.4%

~] 7-1 A}
-, l__:_
L_~

50ppl11 50ppl11 50ppl11

l-H1 2}4;:- H 2.

G. procumbens G. pseudochina A. bilimbi (2) :3)

50ppm 50ppl11 50ppl11 50ppl11 50ppl11 50ppl11

5)
_/

+(2)(1: 1)

:1':+:'5\1' . 1) \,')/

~6) +(3)( 1: 1)

~3)+:2'+/'5\
_j

'<}_i

1'• 1: 1)

[48]

~4- ~l';: tl}9}:Q-0l, B~ 4-~% 3J ~W%~Pi p1~1LJI}7} Jf--4-Wg ~ 4- ~l_2._u=1, % %*y:9}(Gynuraprocumbens), J q~T:119}(Gynura pseudochina), ~ 1.EJ l=ldA verrhoa bilimbi) 3 % ~ ~ W 4-~ % °1 7}AJ "li-,?_ ~ 2} \::l (
A~

3:i3_s:_Jf-El

Ad ~ A11 ~

_!;!_~

q.
u:}~

[49]

[50]

A11-5Joj1~{i~il}L},II1Jf-7ro 5: d %,?_ ~ G1 7}7-1 A11-5J _2.__S:_ % 7} '0 il} u:j, 01 ';: ~ ~~ g g o} \::l B7-1 T~11~ _2.__S:_ ~ il}$7-} Wo1 q. {i
A

il}71~1 ~~~~1

5:Ad%~

7~~%

~Aa

il}$7-}

Wo 1

[51] [52] [53]

[A11-5J oj11] ~ il}71 ~ 3:i9}

0J~AJ4-(~3._S:_~) :Q-01 ~ 0J~AJ4- ~ ~AJ~

l=lJ'ij ~1 u:}2}

A115:il}~ q.

8
WO 2010/120150
PCT/KR2010/002388

~ lfiI'

4.0

7}JI ~

~r;il-~

~E;:;l

e t::.1'11

5.0

c}oJ

[54]

[55] [56]

[A11-5J oj1 2] *<i1~AJ4-e- Zl_s:_~) il}71 ~ J±9} :Q-01 *<i1~AJ4- ~

~/-J~ 1=lJ'ij u:}2} ~1

2.0 3.0

A115:il}~

q.

2.0
2,0 0.1 0.2
0.4

10.0 0,1 to 100 [57]

[58] [59]

[A11-5J oj1 3] ~ °J3 '-El il}71 ~ J±9} :Q-01 ~ °J3 '-El g_

~/-J~ 1=lJ'ij u:}2} ~1

A115:il}~

q.

9
WO 2010/120150
PCT/KR2010/002388

~ ~ l!:lJ (Averrhoa bilimbi)

+'f~

2.0

[60] [61]

[A11-5J oj1 4] p}A}7-13 '-El

ii}71~

J±9} :Q-01 p}A}7-13'-El g_ ~/-J~ l::lJ-'ij~l u:}2} A115:ii}~rt.

[62] ~ ~ l!:lJ (Averrhoa bi1i1llbi)+i~~

LO
10.0 1.5 2.0

0.8
40.0 5.0 4.0 5.0 3.0 3.0

OJ
to 100

[63] [64] [65]

[A11-5J oj1 5] ~

ii}71 ~ J±9} :Q-01 ~ g_ ~/-J~ l::lJ-'ij ~1 u:}2} A115:ii}~

rt.

10
WO 2010/120150

rcr IKR201

0/002388

"if*4Q}(Gynura procumbens] ~~ ~\?J lolJ (Ave1'1"hoabilimbi) ~~%

..

1.0 13.. 0 0.2 5.. 0 0.1 6.0

0.3 0.3
to 100

[66] [67] [68]

[A11-5J oj1 6] A,1! il}71~ J±9} :Q-01 A,1!

g_ ~/-J~ 1=lJ'ij ~1u:}2}A115:il}~

~~. 0.5

q.

;>;:}*Lf!?i-(Gynura procumbens)

t:f~ rfl!?}(Gynura

~ ~ va lolJ (Averrhoe

pseudoehina) bilimbi)

~'I' %
0.05 5.0 0.3 5.0 0.5 0.3
to 100

[69]

~~~o14f~~°1=~Pi ~/-J~ ;q~g_ 7}~A}2}~/-J71 ~%g_ tl}%_2__s:_~ ~~~ ~9~~Pi qOJ~ g % 3J ~-5J g_ f>~il}';: 017}'oW ~o1q. ~

11 WO 2010/120150

rcr IKR201

0/002388

~ '-6l=ld (A verrhoa bilimbi) u1 ~% g:_~ II1Jf- <5Jx~%

A111

4-~% ~AJli

g_ % lL

Ad ~

_2__s:_± Will ~ :

II1 Jf-

5::Ad%.

<5J~1 ~l°1J'i , AJ71 % lL Ad ~,?_ %*y:9t(Gynura procumbens) 4-~% 3J q~ T:119t(Gynura pseudochina) 4-~% _s:_0 Pf-e>l ~ r~Pi <'i ~-'8_
1% 01AJ g_ Li :± Will ~ ~ g_ ~ ~ _2__s:_ll ~ ~AJ li 5::Ad %. i

<5J~1 ~le>l Ai , AJ71 % lL Ad ~,?_ %*y:9t(Gynura

A11 2

procumbens)

4-~%JI}

~ '-6l=ld (A verrhoa
pseudochina) A11 3

bilimbi) 4-~%, ~

g:_ ~

q~

T:119t(Gynura

4-~%JI}

'-6l=ld (Averrhoa

bilimbi) 4-~%

g_

:± Will ~ ~ g_ ~ ~ _2__s:_ll ~ ~AJ li S:Ad %. i

<5J~1 ~le>l Ai , AJ71 %lL Ad~,?_ %2Jtl1 ~ 71~_2__s:_ 1: 5 ~7-15: 1~ tl1~_s:_ ~ W -'8_ 4-~% g_ :± Will ~ ~ g_ ~ ~ _2__s:_l}~ ~AJ li 5:Ad %. i A11 <5J~1 ~l Ai , 2 e>l AJ71 % lL Ad ~,?_ %*y:9t(Gynura procumbens) 4-~%, q~ T:119t(Gynura pseudochina) 4-~% 3J ~ '-6l=ld (A verrhoa bilimbi)
4-~% A11 5

g_ :± Wil} ~ ~ g_ ~ ~ _2__s:_l}~ ~AJ li 5:Ad %. i

~ 71 ~ _2__s:_ -5: 1-5: 1-5~ 1 ~ ~ g_ ~ ~ _2__s:_l}~ i
A~

<5J~1 ~le>l Ai , AJ71 % lL Ad ~,?_ %2Jtl1 ~ W -'8_ 4-~% g_ :± Wil} A111 <5J~1 ~l Ai , e>l AJ71 5:Ad %,?_ ~ 2} \::l ~
A111

tl1~ _s:_

~AJ li 5:Ad %.

~ A11 1~ II1 Jf- u1 ~ lLJI} ~ ~ ~ A ~ g_ ~ ~ _2__s:_l}~ ~AJ li 5:Ad %. i

A~

Ad g_

<5J~1 ~le>l Ai , AJ71 5:Ad %,?_ ~2};W(collagen) ll_S:_E110}A11(MMP-l)~ ~Ad g_

A111

WAd

g_ ~

7-i-o~il}~

7}A171 II1Jf- <5Jx~

$,

ulPg- _s:_
~~

lLJI}~

<5J~1 ~le>l Ai , AJ71 % lL Ad ~,?_ 5:Ad % % %2J

g_ 71 ~ _2__s:_.1 ~ 7-1 5%2J%_s:_ 0