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Antiemetic activity of effective extract and bioactive compounds in ginger

生姜中有效部位及相关活性成分的止呕作用研究



全 文 :2016
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Vol41,No.5 March,2016
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(gingeretherextract,GEE)
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HT3ÍöqŠ| SR57227A‘ M3æ‰ÍöqŠ|š9æ‰(carbachol)閎=ö%xµ½Ž%&。’yàº
GEE(25,50,100mg·kg-1)3
ñ| {íîà{wswxŸW°nŒŽ 
(P<001),
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mg·kg-1)3
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(P<001);RPHPLC
Å(’yóC
,GEE
$;­,B

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6gingerol,8gingerol,6shogaol,10gingerol;
o
5HT3ÍöqŠ| SR57227AG±¯ 1×10
-5
mol·L-1
‘
M3æ‰ÍöqŠ| carbacholG±¯ 10
-4mol·L-1
O

‡×ù‚
GEE(23,46,115mg·L-1),6gin
gerol,8gingerol,6shogaol,10gingerol(1,2,5μmol·L-1)íî_þ=ö%xµŽÇw½!æ(P<005,P<001)。
,úîj

©V$ŽBW1X
GEE
ËÌ$Ž;­‡
6gingerol,8gingerol,6shogaol,10gingerol
Ö©[\Éʎfôî
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5HT3‘ M3æ‰ÍöBZ。

qrs
] 
©V

BW1X

°Â‡

[\ÉÊ

Íö

tu)(
] 20150908

vwxT
] 
@`‹Œü¨g*xy
(81102728)

yzA{
] 
eüý

͗°

ΟéÏj
,Tel:(025)85811513,Email:kewei_31@163com

A{„…
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,Tel:15996258093,Email:463158101@qqcom
Antiemeticactivityofefectiveextractandbioactivecompoundsinginger
HUXuxin,LIUXiao,CHUYu,CHENWenxing,ZHANGKewei,WUHao
(ColegeofPharmacology,NanjingUniversityofChineseMedicine,Nanjing210023,China)
[Abstract] Toinvestigatetheantiemeticefectoftheactiveextract(gingeretherextract,GEE)anditsbioactivecompoundsingin
ger,thepicavomitingmodelinratsandthegastricemptyingmodelinmicewereusedtoobservetheantiemeticefectofGEEincispla
tininducedpicaandgastricemptying,andthemaincomponentsinGEEweredetectedbyRPHPLC;invitro,theantagonistefectof
GEEandthefourcomponentsinitwereexploredbythecontractionofguineapigileuminducedbySR57227AandcarbacholThere
sultsshowedthattheamountofKaoliningestedbyratsweredeclinedsignificantlyinalthethreegroupsofGEE(25,50,100mg·
kg-1)(P<001),whilecisplatininducedgastricemptyinginmicewasalsosuppressedinalthethreegroups(P<001),and
6gingerol,8gingerol,10gingeroland6shogaolwerefoundmainlyinGEEbyRPHPLC;themaximumcontractionofisolatedguinea
pigileumcouldbereducedbyadditionofGEE(23,46,115mg·L-1),6gingerol,8gingerol,10gingerolor6shogaol(1,2,5
μmol·L-1)whentheconcentrationofSR5727Awas1×10-5mol·L-1andthatofcarbacholwas1×10-4mol·L-1(P<005,
P<001)Inconclusion,5HT3andM3receptorscouldbeantagonizedbyGEEanditsbioactivecompounds6gingerol,8gingerol,
10gingeroland6shogaol,whichmaybecorelatedwiththeantiemeticmechanismofgingermayberelatedtoit
[Keywords] ginger;efectiveextract;activecompounds;antiemetic;receptor
doi:10.4268/cjcmm20160524
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ñ¶ËÉ#
5mg·kg-1,24h
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:x€Ì!šØ
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1h,
ú•
ï{Ö

ÌSx{íñ¶ËÉ#
7mg·kg-1,40
min
H

|ª:x«€
004%
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02mL,15
·509·
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Vol41,No.5 March,2016
min
Hú¯

-€C¤
5mL
½ú*Ž:Æ;$

Ê
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*$

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NaHCO3Í+Œl pHË 60~65,-¼w
+2
12000r·min-1
=S
3min,
ã.à-¼w+
200μL¤ 96ÕÙ8,Ê$–‚(×à+±(uý
560nm)。
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±

ºÕµW}Ž°þîο€Ì!Žï

€µ
W}

€$ºÕà+±

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×100%。
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°W+Y>ç¶(×
GEE
$Ž;­‡
241 
>çIJ
 AgilentTCC18>ç–(46
mm×250mm,5μm);¥ŠY“”(C)*(A),±

(0~15min,85% ~50% A;15~45min,50%
A;45~65min,50% ~20% A;65~67min,20% ~
0% A;67~70min,0% A;70~72min,0% ~85%
A;72~85min,85% ~85% A);
ö쥠
10
mL·min-1;
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280nm。
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±ÄÍ+
 
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6gin
gerol,8gingerol,6shogaol,10gingerol


ã.³
×

Fô,
6gingerol850mg·L-1,8gingerol323mg
·L-1,6shogaol609mg·L-1,10gingerol350mg·
L-1
Žíñ±ÄÍ+

ɯíñ±Ä`õ+

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(Í+
 
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10
mL
 Ÿ$

ùëÐË2±

>?
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ɯ(Í
+

¼(ýÏ
045μmòÕ¥íÒ¥。
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ËÌ$Ž;­#ö‡±
SR57227A
Ë
š9æ‰
(carbachol)
Q=ö%xµ½Ž%&
251 
=ö%xµŽôõ
 
%xðW
24h,
]
ð*

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+{7

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ñÏ
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1g
ýÜm

ц
20min,
Þǁ½!×

ãml–µðH

Û
!¼nTU

252 SR57227A
Ë
carbachol
ŽÇ3| M•
 
=ö%xµŽôõ•¶
241
£L•¶

ц
20min,
Þǁ½!×

ãml–µðH

Û!T
U

‡×/$ù‚]| 

’G±
1×10-8~
1×10-3mol·L-1)
Ž
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carbachol,
Èù
!–ùǎÑ큽!æ

253 GEE
ËÌ$Ž;­#ö‡±
SR57227A
Ë
carbachol
Q=ö%xµ½Ž%&
 
=ö%
xµŽôõ•¶
241
£L•¶

ц
20min
H

‡×O>Ð$ù‚]G±Ž
GEE
ËÌ$
;­#ö‡
01mL
H

ц
15min,
‡‡×ù‚
SR57227A
Ë
carbachol01mL。
Èù!–ùǎ
Ñ큽!æ

26 
^Ž‡§
Ž Îq2 珋x±sóº,^ Ž‡§²Ê SPSS
150
^ŽqJ$Ž#®ì•K‡§
(OneWay
ANOVA)。
Ì${ʧëMÊ
Dunnetttests
ÅU
±=‰¼núÈ
,P<005¯
KÿB^Žd¿

3 
’y
31 GEE
±É#QwxÿW$Ž%&
ñ¶ËÉ#H

wxÿW°nŒŽ à{w
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(P<001);GEE
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ªšØ{§ë


{ÂKÿ
(P<001),

1。
ó
1 GEE
±É#øQwxÿW$Ž%&
(珋x±s,n=6)
Table1 EfectofGEEoncisplatininducedPICArats(珋x±s,
n=6)


/mg·kg-1
°nŒŸW 
/g
•ïW.ŸW 
/g
•ï
- 0018±0005 33104±2116
šØ
5 0817±0118 12808±2006
d¸Eµ
08 0207±0038 23329±3321
GEE
þ| 
25 0579±01291) 20166±21331)
GEE
$| 
50 0465±00781) 21219±12621)
GEE
°| 
100 0411±00621) 22981±24961)
  


ªšØ{§ë
1)P<001(
ó


)。
32 GEE
±É#Q:x€Ì!Ž%&
ñ¶ËÉ#H

:x€8µW}à{wù

GEE
þ

$

°| {íçCà±¾É#øQŽ:
x€Ì!Kô

ªšØ{Y§

x{Ž€8µW}à
{ws
(P<001),

2。
33 
°W+Y>ç¶(×
GEE
$Ž;­‡
‡×-íñ±ÄÍ+‘(Í+x
10μL,
¼((×

’yàº
GEE
$;­,B
6gingerol,8
gingerol,10gingerol,6shogaol
„‡

xq
1。
34 SR57227A
Ë
carbachol
ŽÇ3| M•
SR57227A
Ë
carbachol
±=ö%xµŽ%&
·609·
þõ[„

©V$BW1XËYZ°Â‡Ž[\Éʘ™
  ó2 GEE±É#øQ:x€Ì!Ž%&(珋x±s,n=8)
Table2 EfectofGEEongastricemptyingincisplatintreated
mice(珋x±s,n=8)


/mg·kg-1 A €µW}/%
•ï
- 0085±0008 893±087
šØ
7 0509±0039 5344±412
d¸Eµ
12 0247±0032 2599±334
GEE
þ| 
50 0345±00341) 3615±3691)
GEE
$| 
100 0296±00351) 3126±3791)
GEE
°| 
200 0282±00271) 2968±2931)
16gingerol;28gingerol;36shogaol;410gingerol。
q
1 
±Ä
(A)
Ë©V“yÑ-.
(B)
Ž
HPLC
q
Fig1 HPLCchromatogramsofreference(A)andginger
etherextract(B)
o[×é18´Š| YZÂ

Èù‡×^ë
1×
10-9~1×10-3mol·L-1
Ž
SR57227A
Ë
carbachol
±=ö%xµÑ큽!掓_

’yóC

r
SR57227A
Ž’G±¯
1×10-9,1×10-8mol·L-1
O

±=ö%xµŽ½,¤àB%&

úOŽÑ
큽!æª=ö%xµ•ï©ÈuŠOŽÑí
½!æYr

(
SR57227A
G±Žwù

=ö%
xµŽÑ큽!æ*+w&

r
SR57227A
Ž
’G±¯
1×10-5mol·L-1
Ë2¼O=ö%xµ
Ž½!æ0Y±‹×

ØÔÇw¹

Ý2’G±
1×10-5mol·L-1
¯
SR57227A
ŽÇ3| 

r
car
bachol
Ž’G±¯
1×10-9,1×10-8mol·L-1
O

±=ö%xµŽ½,¤àB%&

úOŽÑ
큽!æª=ö%xµ•ï©ÈuŠOŽ
Ñ큽!æYr

(
carbachol
G±Žwù

=ö%xµŽÑ큽!æ*+w&

r
car
bachol
Ž’G±¯
1×10-4mol·L-1
Ë2¼O=
ö%xµŽ½!æ0Y±‹×

ØÔÇw
¹

Ý2’G±
1×10-4mol·L-1
¯
carbachol
Ž
Ç3| 

xq
2。
q
2 SR57227A(A)
‘
carbachol(B)
G±±=ö%xµ
½Ž%&
(珋x±s,n=8)
Fig2 Doseefectcurveofguineapigileumcontractionin
ducedbySR57227A(A)andcarbachol(B)invitro(珋x±s,
n=8)
35 GEE
±
SR57227A
Ë
carbachol
Q=ö%xµ
½Ž%&
o]ù‚
GEE,
G‡×ù‚
1×10-5mol·L-1
SR57227A
‘
1×10-4mol·L-1carbachol01mL
H

=ö%xµ½ŽÑí!æêÎÇw¹

r
GEE
’G±¯
1×23mg·L-1
O
,GEE
îà{_þ
SR57227A
Ë
carbachol
Q=ö%xµ½Ñí!
æ
(P<005);
r
GEE
’G±¯
46mg·L-1
O

GEE
îà{_þ
SR57227A
Ë
carbachol
Q=ö%
xµ½Ñí!æ
(P<001);
r
GEE
’G±¯
115mg·L-1
O
,GEE
îà{_þ
SR57227A
Ë
carbachol
Q = ö % x µ  ½ Ñ í ! æ
(P<001),

3。
36 6gingerol,8gingerol,6shogaol
‘
10gingerol
±
SR57227A
Ë
carbachol
Q=ö%xµ½Ž
%&
¼ÁTU˜™$mŠ
GEE
þ

$

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Vol41,No.5 March,2016
  ó3 GEE± SR57227AË carbacholQ=ö%xµ½
Ž%&
(珋x±s,n=8)
Table3 TheantagonistefectofGEEonthecontractionof
guineapigileuminducedbySR57227Aorcarbachol(珋x±s,n=8)

’G±
/mg·L-1 SR57227A/g carbachol/g
šØ
- 2641±0332 3582±0394
GEE 23 2232±02432) 2919±02282)
46 1863±01871) 2513±01191)
115 1498±02191) 2364±02631)
  


ªšØ{§ë
1)P<001,2)P<005(
ó


)。
îà{_þ
SR57227A
Ë
carbachol
øQŽ=ö%x
µ½Ñí!æ

°W+Y>ç¶Å(’ymŠ
GEE
$;­,B
6gingerol,8gingerol,10gingerol,
6shogaol
„‡

ÝB㭇ױn

ñ#ö‡
¼n=ö%xµTU

o]ù‚
6gingerol,
8gingerol,6shogaol
‘
10gingerol,
G‡×^ë
1×
10-5mol·L-1SR57227A
‘
1×10-4mol·L-1car
bachol01mL
H

=ö%xµ½ŽÑí!æê
ÎÇw¹
。6gingerol
$

°| 
(2,5μmol·L-1)
’G±{íî2à{_þ
SR57227A
Q=ö%xµ
½Ñí!æ
(P<001),1μmol·L-1| ’G
±{bçà{_þ
SR57227A
Q=ö%xµ½
Ñí!æ
,6gingerol
x| 
(1,2,5μmol·L-1)’
G±{íî2à{_þ
carbachol
øQŽ=ö%x
µ½Ñí!æ
(P<001);8gingerol
x| 
(1,2,5μmol·L-1)’G±{íî2à{_þ
SR57227A
Ë
carbachol
øQŽ=ö%xµ½Ñ
í!æ
(P<005,P<001);6shogaol
x| 
(1,2,
5μmol·L-1)’G±{íî2à{_þ SR57227A
Ë
carbachol
Q=ö%xµ½Ñí!æ
(P<
005,P<001);10gingerol
x| 
(1,2,5μmol·
L-1)
’G±{íî2à{_þ
SR57227A
Ë
carba
chol
ø Q Ž = ö % x µ  ½ Ñ í ! æ
(P<001),

4。
4 
À
\¯«[ñð-ŽÎËÒÓ

;­:ã¶ÅÒ
¯_àÍJ
(CTZ)、
ý0uf

8ĄW‚=ŠÉ
ʤ¶”\¯$Êé–\¯

_‘,.É#„î^
5HT
8€Øí8Ž¯°¿j‘,
5HT
ŽÖt
Ë$Ê1XñÏ~¥ 

¥ Ž
5HT
Ï=ŠWv
@B

Úq
CTZ
‘\¯$ʎ
5HT3ÍöùQ
[11]。M3æ‰ÍöE>æo¤€BÑmc,  ó 4  6gingerol,8gingerol,6shogaol‘ 10gingerol±
SR57227A
Ë
carbachol
Q=ö%xµ½Ž%&
(珋x±s,
n=8)
Table4 Theantagonistefectof6gingerol,8gingerol,6shog
aoland10gingerolonthecontractionofGuineapigileumin
ducedbySR57227Aorcarbachol(珋x±s,n=8)

’G±
/μmol·L-1 SR57227A/g carbachol/g
šØ
- 2603±0321 3524±0387
6gingerol 1 2334±0246 2814±02991)
2 1879±03131) 2416±01981)
5 1786±01981) 1875±02751)
8gingerol 1 2235±03872) 2987±02872)
2 1954±03111) 2632±03121)
5 1813±02761) 2423±01521)
6shogaol 1 2034±02541) 2843±02531)
2 1854±03011) 2421±03911)
5 1415±02761) 1993±02431)
10gingerol 1 2143±03231) 2793±03261)
2 1739±02931) 2532±02251)
5 1317±02251) 2432±02611)
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Ú«n•šØoTUÒÓ$Ñ
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§üöìëw

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‘<ŠÚqíç·v
wxÖ©ÿW$

Ÿ‚š–Â.Ÿü°nŒ
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羗zοŠ.€Ì!‹
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GEE(25,50,100
mg·kg-1)
xG±| {íçCàwsÉ#øQw
xŸW°nŒŽ 
(P<001),
O
GEE(50,100,
200mg·kg-1)
xG±| {íçCà±¾É#ø
QŽ:x€Ì!Kô
(P<001),
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GEE
Ž[
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4(¬{Ê°W+Y>綱
GEE
$Ž;­‡¼n‡§Å(


GEE
;­,B

/VÔ쐇
,6gingerol,8gingerol,6shogaol
‘
10gingerol,
ª%8›!&m„Ž˜™’yY
[Q
[1415]。
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þõ[„

©V$BW1XËYZ°Â‡Ž[\Éʘ™
%֛
AbdelAziz
„Ž˜™àº
,6gingerol,
8gingerol,6shogaol
‘
10gingerol
îçmBÁ¾
5HT3ÍöŽÉÊ
[16]。
4(¬{Ž˜™’yàº
,GEE
ËÌ$Ž#ö
‡
6gingerol,8gingerol,6shogaol
‘
10gingerol
o
]| ’G±Líî2à{_þ
SR57227A
‘
carbachol
øQ=ö%xµ½ŽÑ큽!æ
(P<005,P<001),
-´[× WZŸ

Ѻ

©
V$Ž
GEE
1XËÌ$ø,BŽ
6gingerol,8gin
gerol,6shogaol
‘
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îç«ÌmB¾\¯
ÉʎW².Ÿ

n..Ÿ@îçÃR
5HT3Íö,
ßîçÃR
M3æ‰Íö。
4(¬{ŽËU’yóC

©Vîç@ÒÉÊ
¤
5HT
Íö‘
M3æ‰Íö8ù–ξ\¯ÉÊ,
©V$,BŽ°Â.Ÿ@çÃR
5HT3Íö(‹À
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),
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|}?~

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