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黄花稔属化学成分与药理作用研究进展(英文)



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(收稿日期 2009-11-18)
Advances in research of chemical constituents and
pharmacological activities of genus Sida Linn.
SUN Lu-lu1 , WANG Ji-hui2 , YAN Bin2 , XU Ling-chuan2*
(1.Qingdao Huashi Guofeng M edical Co., L td., Qingdao 266071 , China;2.Faculty o f Pharmacy ,
Shandong Univer sity o f T raditional Chinese Medicine , Jinan 250355 , China)
Abstract: Acco rding to studie s of last three decade s , S id a Linn.contains many kinds o f chemi-
cal consti tuents , primarily including alkaloids , steroids and so on.Plants of different species of
Sida Lnn.are w idely used in Tradit ional Chinese M edicine fo r the t reatment of asthma , renal in-
f lammation , colds , feve r , headache and ulce rs.In foreign countries , Sida acuta Burm.f., a spe-
cies of this genus , i s used to t reat malaria , and the active component cryptolepine is considered to
have ant i-inflammato ry , anti-malarial , anti-tumor and hypog lycemic ef fects.In China , consti tu-
tions of the aerial part of S.szechuensis Matsuda has been analy zed.8 steroids , 1 steroidal sapo-
nin , 1 f lav onoid g lycoside , 1 mono terpene , and 1 indole alkaloid have been ex tracted and isola-
ted.The antibacte rial experiments of it s ethano l ex tract have also been conducted.This paper
gives an overview of chemical consti tutions and pharmacolo gical activit ies of Sida Linn.plants ,
so as to provide more reference fo r further development and ut ilization of genus S ida Linn.
Key words:Sida Linn;chemical consti tuents;pharmacolog ical activi ties
黄花稔属化学成分与药理作用研究进展
孙璐璐1 ,王集会2 ,闫 滨2 ,徐凌川2*
(1.青岛华氏国风医药有限责任公司 ,山东 青岛 266071;2.山东中医药大学药学院 , 山东 济南 250355)
摘 要:黄花稔属 S ida Linn.植物含有甾醇类 、生物碱类等多种化学成分。该属的多种植物作为传统中药广泛用
于治疗哮喘 、肾炎 、感冒 、发烧 、头痛 、溃疡等。在国外 , 用该属植物黄花稔 Sida acuta Burm.f.治疗疟疾。对其有
效成分白叶藤碱(cryptolepine)进行了较深入的研究 ,认为该成分有抗炎 、抗疟 、抗肿瘤 、降血糖等作用。国内对拔
22 现代药物与临床  Drugs &Clinic  2010年第 25卷第 1 期
*    *通讯作者 徐凌川 ,教授 ,从事中药资源与鉴定的教学和研究工作。 E-mai l:xulingchuan518@sina.com
毒散 S.szechuensis Matsuda 的地上部分进行了化学成分研究 , 从中提取 、分离到 8 个甾醇类化合物 、1 个甾体皂
苷 、1 个黄酮苷 、1 个单萜 、1 个吲哚类生物碱 , 并对其乙醇提取物做了抗菌实验。综述了该属植物化学成分和药理
活性研究概况 ,为进一步开发 、利用该属植物资源提供参考。
关键词:黄花稔属;化学成分;药理活性
中图分类号:R282.71   文献标识码:A   文章编号:1674-5515(2010)01-0022-05
  The Sida Linn.i s a genus of herbs and sub-
shrubs in M alv aceae family.There are about 90
species , mainly dist ributed in the t ropics and sub-
t ropics and some in temperate regions.From
Southw est to No rth China , there are 13 species
and 4 va riants such as S.rhombi folia L ., S.
alni f ol ia L., S.chinensis Retz., S.cordi folia
L., S.subcordata Span , S .parvi folia DC., S.
acuta Burm.f.and S .szechuensis Matsuda.Al-
though there are pharmacological and pharmacody-
namic studie s on some o f them , repo rts on their
chem ical constituents are still rare.Studies in Chi-
na mainly fo cus on S.szechuensis Matsuda , whi le
studies in foreign countries of ten fo cus on S .acuta
Burm.f.Acco rding to the study repo rts , the main
activ e consti tuents of S id a Linn.are alkaloids and
steroids.Pharmacolo gical e xperiments have show n
that plants of Sida Linn.have a wide range o f
functions such as ant i-inflammation , antibacte ria ,
hemostasis , anti-malarial , anti-tumo r , and hypo-
g lycemic ef fect.
1 Chemical constituents
1.1 Steroids and their derivatives
From S.carpini folia L., the steroid com-
pounds ecdy sone and ecdy steroid can be ext rac-
ted[ 1] .From S .szechuensis , seven steroid com-
pounds can be ext racted , including β-si to sterol ,
daucostero l , polypodine A , polypodine B , α-ecdy-
sone(1), β-ecdysone (2), and 5β ,20R-dihydroxy-
α-ecdysone (3)[ 2-3] .From S.spinosa L., five ster-
oid compounds can be ext racted , including 20-hy-
droxy-24-hydroxymethyl ecdysone (4), 20-hydroxy-
ecdy sone (5), turkesterone (6), markisterone (7),
20-hydroxyecdy sone-20 , 22-monoacetonide(8)[ 4] .
These compounds are mainly ecdy sterone and
their derivatives.A new steroid compound has
been ext racted f rom ethano l ex tract o f the aerial
parts o f S.sz echuensis by Li[ 5] .It is identified as
2β , 3β , 14α, 20R , 21 , 22R , 24-heptahydroxycholest-
7-en-6-one (9).This new steroid compound is one
of the pharmaco logically effect ive consti tuents of
the genus.
Li′s[ 5] experiments pro ve that steroid com-
pounds 2β , 3β , 14α, 20R ,21 , 22R , 24-heptahydro xy-
cholest-7-en-6-one (10)and 3-O-β-D-g lucopy rano-
side-α-ecdysone (11) are the majo r antibacterial
consti tuents of S.szechuensis.Structure s of com-
pounds 1 —11 w ere show n in Fig.1.
1.2 Alkaloid compounds
From S.cordi f ol ia , three alkaloids can be
ex t racted , including quinazolines alkaloids , car-
boxy lated t ryptamines and β-phenethy lamines[ 6] .
The same alkaloids can be ext racted f rom o ther
four species o f S ida Linn., such as S .acuta , S.
hum ilis , S.rhombi folia and S.spinosa[ 7] .Alka-
loid is ano ther ef fective consti tuent of pharmaco-
logical activi ties of S ida Linn.Besides , the related
studies show that cryptolepine (12 , Fig.1), ex-
t racted f rom S.acuta , has a significant antimala-
rial ef fect
[ 8] .
1.3 Monoterpene
There is only one chemical constituent of
mono terpene , which is loliolide (13).The st ruc-
ture w as elucidated as follow ing (Fig .1).
1.4 Flavonoid
There is only one chem ical consti tuent of f la-
vonoid , astragalin 6″-O-(4-hydro xycinnamoy l)
(14).The structure is elucida ted as fo llow ing
(Fig.1).
1.5 Scopoletin
There is only one chemical consti tuent of sco-
poletin.I t i s 6-methoxy-7-hydro xycoumarin (15),
also called scopo lamine.The st ructure is elucida-
ted as follow ing (Fig.1)
23现代药物与临床  Drugs &Clinic  2010年第 25卷第 1 期
Fig.1 Structures of compounds 1—15
24 现代药物与临床  Drugs &Clinic  2010年第 25卷第 1 期
2 Pharmacological activities
2.1 Anti-inflammatory and antibacterial effects
The ex tracts of the stems , leaves , ro ots o f S.
cord i f olia have obvious anti-inflammato ry
ef fects[ 9] .The ethy l acetate ex tract of the ro ots
can inhibi t the inflammato ry edema of male Wistar
mouse significant ly.The ex t racts o f S.rhombi fo-
lia , ext racted w ith methanol , hexane , chloro fo rm ,
e thyl acetate and n-butanol respectively , all have
ant i-inflammato ry ef fects , which are generally
weake r than tho se of S .cordi folia and S .acu-
ta[ 10] .However , the n-butano l ex t ract has anti-in-
f lammato ry ef fect as g ood as that of phenylbuta-
zone[ 11] .
The ethanol ex tract of the aerial parts of S.
acuta has significant antibacterial ef fects.E thyl
acetate ex tract , ex tracted f rom the ethanol ex tract
of S.szechuensis , has a remarkable antibacterial
function
[ 9] .
2.2 Hypoglycemic effect
The methano l ex t ract of S.cordi folia has a
significant ef fect of decreasing blo od g lucose con-
centration.A fter administ ration of methanol ex-
t ract , blood g luco se concentration is lowe red to a
minimum value 2 h later , and returns to no rmal 6
h later.In the Gluco se To le rance Test (GT T),
gluco se to le rance curve demonst rates a typical in-
hibi to ry ef fect compared w i th the contro l group in
30 min.In addition , al l the ext racts o f stems ,
leaves and roots of S .cordi folia have good hypo-
g lycemic ef fects[ 9] .
2.3 Anti-malarial activity
S.acuta show s a significant anti-malarial ac-
tivity.Fur ther chemical screening demonst rates
that the mechanism is related to it s alkaloid pro-
po rtionately
[ 8] .
2.4 Hemostatic activity
The ethano l ex t ract of S .acuta has obvious
hemostatic ef fect during the t reatment of bleeding
caused by snakes biting[ 12] .The w ate r ex t ract o f
S.szechuensis has certain ef fect of hemostasis.
2.5 Analgesic effect
All ex t racts o f stems , leaves and ro ots o f S.
cordi folia have good analgesic ef fects
[ 9] .The w a-
ter ex tract of the plant can inhibit co lic distor tion
of mice induced by acetic acid.The w ater ex t ract
of S.szechuensis display s certain analg esic func-
tions in several m ice experiments
[ 13] .The animal
experiments show that the ex t ract of S .acuta also
has analgesic effect
[ 14] .
2.6 Anti-tumor activity
Cryptolepine isolated f rom the roo ts of S.
acuta has good anti-tumor effects[ 15] .The com-
pound can bind tight ly to DNA betw een base pai r ,
and behave as a typical inte rcalating agent , so as to
stabili ze the topoisomerase Ⅱ-DNA covalent com-
plex .It i s a potential inhibi to r of topoisomerase
Ⅱ.Some of it s analogues can stabili ze telomeric G-
Ⅳ burgdorferi , and inhibi t telomerase.These re-
sults demonst rate that cryptolepine may be deve-
lo ped into a good ant i-tumor drug.
2.7 Other pharmacodynamic activities
Both methanol and w ater e xt racts of S.
cordi folia have significant funct ion of resisting liv-
er tox icity induced by CCl4 , paracetamol and ri-
fampin
[ 16] .The ethy l acetate ext ract of S.rhombi-
f ol ia has an ef fect o f av oiding injury
[ 11] .The ethy l
acetate ex t ract of S.pak istanica can relieve spas-
ti sm
[ 17] .
3 Discussion
China ow ns abundant specie s resource of g e-
nus Sida Linn., most o f them distribute in pro-
vinces southern Yang zi river , in north china exi ts
only one species S ida sp inosa L.Compared to fo r-
eign countries rare studies have been done about
this g enus in China.It i s necessary to cont inue to
research the genus , to elucida te act ive compounds
and mechanisms.A persistent st rive from pharma-
cists w ill be done in developing clinic drugs coinci-
ding t raditional therapies.
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(收稿日期 2009-07-31)
瑞香狼毒的化学成分 、生物活性及应用研究进展
刘文程 , 王 臣*
(哈尔滨师范大学生命科学与技术学院 , 黑龙江 哈尔滨 150025)
摘 要:瑞香狼毒为传统中药 , 性味苦平 ,有杀菌 、杀虫 、散结 、逐水 、止痛 、祛痰等功效。近几十年来 , 国内外对其化
学成分 、生物活性及应用等方面进行了较深入的研究并取得显著成果。综述了瑞香狼毒的化学成分 、生物活性及
应用的研究进展 ,为进一步开发这味传统中药提供参考。
关键词:瑞香狼毒;化学成分;生物活性;应用
中图分类号:R282.71   文献标识码:A   文章编号:1674-5515(2010)01-0026-05
Research on chemical constituents , bioactivity , and
application of Stellera chamae j asme
LIU Wen-cheng , WANG Chen
(Colleg e of L ife Science and Technology , Harbin No rmal University , Harbin 150025 , China)
Abstract:S tel lera chamaejasme L ., a t raditional Chinese medicinal material , is bit ter and neutral in
nature.It has many functions such as killing bacte ria and insects , relieving pain and elimina ting phlegm.
There is a significant prog ress on researches of S.chamejasme L .This article summarizes the studies on
26 现代药物与临床  Drugs &Clinic  2010年第 25卷第 1 期
*    基金项目 哈尔滨师范大学博士科研启动基金项目
 作者简介 刘文程(1983—),男 ,硕士研究生 ,研究方向为植物生物学。 T el:13845169150 , E-m ail:lw c472789659@yah oo.com .cn