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Advances on the chemical constituents and pharmacological effects of Chinese sweet tea (Rubus Suavissimus)

甜茶化学成分及药理作用研究进展



全 文 :广 西 植 物 Guihaia Jan.2013,33(1):136-142           http://journal.gxzw.gxib.cn 
DOI:10.3969/j.issn.1000-3142.2013.01.025
颜小捷,卢凤来,李典鹏.甜茶化学成分及药理作用研究进展[J].广西植物,2013,33(1):136-142
Yan XJ,Lu FL,Li DP.Advances on the chemical constituents and pharmacological effects of Chinese sweet tea(Rubus Suavissimus)[J].Guihaia,
2013,33(1):136-142
Advances on the chemical constituents and
pharmacological effects of Chinese
sweet tea(Rubus Suavissimus)
YAN Xiao-Jie1,2,LU Feng-Lai 1,LI Dian-Peng1*
(1.Guangxi Key Laboratory of Functional Phytochemicals Research and Utilization,Guangxi
Institute of Botany,Chinese Academy of Sciences,Guilin 541006,China;2.College
of life sciences,Guangxi Normal University,Guilin 541004,China)
Abstract:Sweet tea is a kind of rare wild sweet smeling plant,mainly containing rich nutritious constituents,such as
rubusoside,tea polyphenol,flavonoids and other active components.Its chemical constituents and pharmacological
effects in nearly years were reviewed,so as to facilitate the further research and more extensive applications.
Key words:sweet tea;rubusoside;tea polyphenol;flavonoid;pharmacological effects
CLC Number:Q949.9  Document Code:A  Article ID:1000-3142(2013)01-0136-07
甜茶化学成分及药理作用研究进展
颜小捷1,2,卢凤来1,李典鹏1*
(1.广西植物功能物质研究与利用重点实验室(广西植物研究所),广西 桂林541006;
2.广西师范大学 生命科学学院,广西 桂林541004)
摘 要:甜茶是一种价值较高的天然保健饮料植物,其营养成分丰富,尤其富含甜茶素、茶多酚和黄酮等主要
活性成分。综述了近年来甜茶化学成分及其药理作用的研究状况,以便于更深入的研究和更广泛的应用。
关键词:甜茶;甜茶素;茶多酚;黄酮;药理作用

  Rubus species have traditionaly been used in ther-
apeutics and showed anti-bacterial,anti-cancer,anti-
spasmodic,anti-diabetes insipidus and anti-anemia
properties(Patel et al.,2004).Rubus suavissimus S.
Lee is one of the most popular perennial shrubs in the
Rubus family.The tea plant has a wide distribution in
southwestern China,especialy in Guangxi of China.
Due to its intense natural sweetness,it is often caled
‘tian cha’or‘Chinese sweet tea’(Liu et al.,2006).It
has been applied as a folk medicine to‘nourish the kid-
ney’,lower blood pressure,fal blood sugar and treat
various diseases for a long time in China.Its leaves
have also been used as an herbal medicine to aleviate
pulmonary pressure,clear internal heat,relieve cough
and reduce the secretion of phlegm(Liu et al.,2006).
Recently,the sweet tea has been known al over
the world because of its hot-water extract(tenryocha).
The tenryocha has attracted a great deal of public at-
tention in Japan,since it has been suggested by Ukai
(1997)that the tenryocha was efective in the preven-
tion of polinosis.Nakahara(1998)reported that the
most important anti-alergic and anti-inflammatory ac-
* 收稿日期:2012-05-25  修回日期:2012-07-17
基金项目:广西自然科学基金(桂科自0991228);桂林市科技攻关项目(20110107-3)
作者简介:颜小捷(1985-),女,广西玉林人,硕士,主要从事植物资源开发与利用研究,(E-mail)xiaojie128@126.com。
*通讯作者:李典鹏,博士,研究员,从事中药、天然药物和植物化学研究,(E-mail)ldp@gxib.cn。
tive constituent was a GOD type tetrametric elagitan-
nin(sanguin H-11).Tenryocha was active in inhibi-
ting angiogenesis,which could cause weight loss and
suppress adipogenesis.Other studies demonstrated
that the tenryocha was able to inhibit the activity of
NF-κB andα-amylase activity(Liu et al.,2005;Li et
al.,2007),while these indexes are closely related to
treating or regulating glucose metabolism.Last but
not least,observations indicated that the residents of
these areas,who consumed Chinese sweet tea,were
generaly healthier and had less incidence of cancer and
other serious diseases.
R.suavissimus has so many pharmacological sani-
tarian functions,owing to its rich pharmacological com-
ponents.So far,it has been reported that there are va-
rious chemical compositions in sweet tea,which include
the sweet tea glucosides,flavonoids,polyphenols,and
so on(Tan,2008).In recent years,the medicinal func-
tions of sweet tea have aroused wide attention from
scholars at home and abroad.Now the chemical con-
stituents and pharmacological efects of in nearly years
were reviewed in this paper.
1 Chemical constituents of sweet tea
1.1Rubusosides
Various studies on chemical constituents of sweet
tea had been undertaken in the past and many biologi-
caly active compounds were obtained.Early studies
mainly focused on the sweetener in sweet tea,which is
attributed to diterpene glucosides(Patel et al.,2004).
Rubusoside(desglucosylstevioside),where the major
sweet principle comes from,is widely used as a natural
sweetener for seasoning and additive in food industry
(Fig.1).It is the principal ent-kaurene glycoside from
R.suavissimus and its sweetness intensity is 115times
sweeter as sucrose at a concentration of 0.025%w/w,
but it has some bitterness and a perceptible aftertaste.
Other diterpene glucosides of sweet tea include the
sweet glycosides(Fig.1):suaviosides A,B,G,H,I and
J,and the bitter glycosides:suaviosides C1,D2and F as
wel as the tasteless:suaviosides D1and E(Ohtani et
al.,1992).However,the sweetness intensities of the
sweet glycosides had not been determined and they
were limited in the leaves and fruits of R.suavissimus
(Chou et al.,1987),and undetectable in the roots.In-
stead,triterpene glucosyl esters,such as the suavissi-
moside F1,were specificaly isolated from the roots of
R.suavissimus(Gao et al.,1985).Besides that,it is of
interest to note that no other species,either the genera
Stevia or Rubus,appear to biosynthesize the sweet tas-
ting ent-kaurene glycosides in significant amounts
(Kinghomet al.,1998).
1.2Polyphenols
Although the quality of the extract was tradition-
aly determined on the basis of sweetness intensity,the
extract is now measured according to the presence of
other bioactive components.Sugimoto(2001)report-
edthat seven polyphenolic compounds were found from
the leaves of sweet tea,including cafeic acid,galic
acid,elagic acid,brevifolin carboxylic acid,2-pyrone-4,
6-dicarboxylic acid,sanguisorbic acid dilactone and 1-α-
galoyl-2,3-(S)-hexahydroxy-diphenoyl-D-glucose.Six
new elagitannins herein named rubusuavins A-F along
with seven known tannins from the dried leaves of R.
suavissimus were separated(Li et al.,2007).Ru-
busuavin A was characterized as 1-O-galoyl-2,3-O-
(S)-HHDP-4,6-O-(S)-sanguisorboyl-β-D-glucopyr-
anose.Rubusuavins B,C,and E were dimeric,trimer-
ic,and tetrameric elagitannins respectively,in which
the sanguisorboyl groups were connected to elagitan-
nin units.Rubusuavins D and F were desgaloyl deriv-
atives of rubusuavins C and E(Fig.2).In addition,
the known tannins were identified as strictinin,pedun-
culagin,sanguin H-5,sanguin H-6,1-desgaloyl san-
guin H-6,1(β)-O-galoyl pedunculagin and lamber-
tianin A by direct comparison of their spectral and
physical data with those of authentic samples.Fur-
thermore,Wei et al.(2006)reportedthat antialergic
active components in sweet tea were guided by Mor-
gan-Elson method.By using the methods of thin layer
chromatography(TLC),ultraviolet spectrum(UV),
infrared spectroscopy(IR)and high performance liquid
chromatography(HPLC),hydrolysable elagitannin
was determined to be the antialergic active component
in sweet tea.And its molecular weight is 10-30kD and
7311期           颜小捷等:甜茶化学成分及药理作用研究进展
Fig.1 Structures of rubusoside and other diterpene glucosides
configuration base unit is C6-C3-C6.
Plant polyphenols are economicaly important and
make major contributions to the colour,flavour,and
taste of food and drink.Pharmaceutical uses of poly-
phenols are very wide,and the astringent action seems
to be the main one.Other uses include the treatment
of wounds,burn and inflammation.Galic acid is one
polyphenolic compound and combined with ursolic,and
19α-hydroxyasiatic acids may have potent antibacterial
activity.It is one of the active compounds,which is re-
sponsible for the anti-angiogenic efect,too.Sanguin
H-6is another polyphenolic compound with astringent
properties as a mouth gargle and for children’s stom-
ach disorders(Patel et al.,2004;Liu et al.,2006).
1.3Flavonoids
Flavonoid is the important chemical composition
in the sweet tea,which is one of the active ingredients.
In recent years,scientists found that sweet tea fla-
vonoids components not only had anti-alergic,anti-in-
flammatory and analgesic activities,but also resistant to
fatty liver,aging resistance,the dilation of blood ves-
sels,microcirculation(Huang et al.,2010).In addi-
tion,it showed some pharmacological efects,such as
preventing arteriosclerosis,reducing blood fat and dia-
betic complications,enhancing the synergy antitumor
drugs(Wang et al.,2007).However,there were just a
few reports related to the existence of the flavonoids in
the sweet tea,and fewer reports about the monomer
flavonoid compound.Chen et al.(2005)confirmed that
the sweet tea contained flavonoid glucosides,whose be-
sibufogenin were quercetin and kaempferol,with the
content of 4.25%and 3.21%,respectively.Zhang
(2006)isolated the sweet tea to get a besibufogenin
monomer compound,which was named Quercetin-3-β-
D-galactoside(Fig.3).
1.4Other components
Lüet al.(2007)and Wang et al.(2007,2008)i-
solated eight compounds from the leaves of sweet tea
for the first time,which were ent-13-hydroxy-kauran-
16-en-19-oic acid;ent-13,17-dihydroxy-kauran-15-en-
19-oic acid;ent-16α,17-dihydroxy-kauran-19-oic acid;
ent-16β,17-dihydroxy-kauran-19-oic acid;ent-16β,17-
dihydroxy-kauran-3-one;ent-kauran-3α,16β,17-3-tri-
ol;ent-kauran-16-en-19-oic-13-O-β-D-glucoside;ent-
kauran-16β,17-diol-3-one-17-O-β-D-glucoside.
Tan(2008)and Luo(2010)reportedthat twelve
compounds were isolated and purified from the chloro-
form extract of the R.suavissimus,using silica gel col-
umn chromatography and recrystalization techniques.
Ten compounds were obtained from the leave of sweet
831 广 西 植 物                  33卷
Fig.2 Structures of rubusuavins A-F
tea for the first time,which were n-dotriacontanol,n-
dotriacontanoi acid,n-hentriacontane,oleanolic acid,ur-
solic acid,palmitic acid,palmic acid,2α-hydroxyursolic
acid,triacontanol andβ-sitosterol.
2 Pharmacological researches of
sweet tea
  Although many studies on the Chinese sweet tea
currently focused on the chemical analysis,a validated
and thorough study relating to the in vivo studies was
scarce.So it brings up another question whether these
bioactive components found in the leaves of sweet tea
are oraly active and can produce a positive response in
live animals.
2.1Toxicologic studies
The sweet tea is investigated to be a low toxicity,
9311期           颜小捷等:甜茶化学成分及药理作用研究进展
Fig.3 The chemical structures of flavonoids of sweet tea
light side efect material(Liao et al.,1981).Besides,
Liang et al.(2003)studied the acute and chronic toxici-
ty of the sweet tea.They found that the sweet tea had
no toxicity on the development,hematology,function of
the liver and kidney and histology in rats.
2.2Pharmacology studies
2.2.1Decreasing sugar or lowing hypocholesterol re-
searches In recent years,people found that the sweet
tea polyphenols could inhibit theα-amylase activity by
reducing sugar in clinical(Li et al.,2007).Middle and
high dose groups showed no efect on lipid.That is to
say low concentration of the sweetener has the efect of
decreasing hypocholesterol.It suggested a guidance for
clinical treatment of hyperlipidemia.Its mechanism
may be relevant to improve the lecithin cholesterol acyl
transferase activity of the rats serum.Tian et al.
(2001)studied the rubusoside on gluconeogenesis and
blood lipid metabolism in mice.The result showed that
the gluconeogensis could beinhibited by rubusoside ob-
viously at a rate of 17.32%.The level of blood sugar
could be reduced significantly by rubusoside a rate of
18.47%,and the level of serum triglyceride markedly
at a rate of 30.08%and it also reduced the content of
serum cholesterol.In addition,Tian et al.(2003)in-
vestigated the anti-hyperglycemic efect of rubusoside
and its mechanism on streptozotocin(STZ)-induced di-
abetic rats.The results showed that compared with the
diabetic model control group,rubusoside could decrease
the level of serum glucose significantly,increase the a-
bility of anti-oxidation and stimulate the secretion of
insulin in STZ-induced diabetic rats.It means that the
action of rubusoside on secretion of insulin can be ex-
plained for the anti-hyperglycemic efect.The efect of
rubusoside on blood sugar metabolism may be related
to stimulate beta cels secrete insulin.Its mechanism
needs further research.Liang et al.(2008)have studied
the efects of robusoside on glycemia in diabetic rats
induced by aloxan.The results indicated robusoside
could significantly reduce both the blood glucose and
the level of plasma glucagon,serum total cholesterol,
triglyceride,low-density-lipoproteincholesterol.Mean-
while,it could enhance serum insulin and high-density-
lipoproteincholesterol in diabetic rats.It means that
robusoside has efects on decreasing the blood glucose
concentration,which may be explained for its increase of
insulin secretion and inhibition of glucagon secretion.
To sum up,the sweet tea cannot only control
blood sugar,but also can lower blood lipids.There-
fore,the sweet tea may reduce diabetic complication
and atherosclerosis,has an efect on the prevention and
treatment of disease of heart head blood-vessel of some
significance.
2.2.2Anti-alergy or anti-inflammatory researches 
Teng et al.(2008)evaluated the anti-alergy of the
sweet tea polyphenols.The influence of polyphenols
were detected using mouse passive skin alergy test,
mouse ear edema test,rat capilary permeability test of
histamine-induced skin and DTH(delayed-type hyper-
sensitivity)by DNCB(dinitrochlorobenzene).The re-
sults showed that the sweet tea had strong efects on
anti-inflammatory and anti-alergy.
Wang et al.(2010)investigated the anti-inflam-
matory efects of the extract of sweet tea.The extract
of sweet tea could conspicuously inhibit the increase of
vasopermeability and acute ear sweling induced by
croton oil in mice,and mice paw sweling induced by
carrageenan.Furthermore,the sweet tea extract also
showed depressant efect on the release of NO and
genes expression of iNOS mRNA in mouse peritoneal
macrophages.It indicated the extract of sweet tea had
conspicuous anti-inflammatory efects.The mechanism
of action may be associated with its inhibition efects
on the release of NO and mRNA expression of iNOS.
2.2.3Other researches Zhong et al.(2010)revealed
that the extract of sweet tea had cough-relieve action
on experimental cough in mice caused by dense ammo-
041 广 西 植 物                  33卷
nia water,and could significantly increase outage of
phenlored in breathe path,inhibit ear sweling of mice
induced by xylene,decrease body twisting times of mice
induced by acetic acid and inhibit spontaneous activity.
Al these suggest that the extract of sweet tea have ac-
tions of relieving a cough,reducing phelm,anti-inflam-
mation,sedation and analgesia.
Liu et al.(2009)reported that R.suarissimus
saponin inhibited streptococcus mutans adhering.It
may be an anticariogenic agent and a sugar substitute.
Li et al.(2009)analyzed that rubusoside by-product
had high anti-alergic and antioxidant activity.Anti-al-
lergic and antioxidant capacity of sweet tea had signifi-
cant correlation with the content of total phenol of by-
product,which had no significant correlation with the
content of rubusoside.Wu et al.(2010)studied the
anti-tumor efect in vitro of total flavone fromR.sua-
vissimus could inhibit the proliferation of S180,H22
and L1210in vitro,while the best inhibitory efect on
H22and folowing on S180.The sweet tea extract had
an inhibitory efect on the contraction of rabbit smal
intestine smooth muscles in vitro,and it had a certain
antagonism on acetylcoline(Zhao et al.,2010).
3 Prospect
Sweet tea is a kind of rare wild sweet smeling
plants,mainly containing rich nutritious constituents,
such as rubusoside,tea polyphenol,flavonoids and oth-
er active components.Rubusoside is a kind of natural
sweetener with high sweet degree,low energy and non-
toxic.It can control blood sugar and reduce blood fat
efect,so is expected to replace sugar to become a ideal
health care sweet taste additives(Liu et al.,2009).
Sweet tea flavonoids components not only have antiox-
idant,inhibition of lipid peroxidation activities,but also
have restraining fatty liver,aging resistance,cardiovas-
cular disease and cancer prevention functions.Tea
polyphenols not only have the activities of clearing the
free radicals and antioxidation,but also has good efect
in the anti-bacterial,anti-viral and anti-tumor and so on
(Wang et al.,2007).
The sweet tea,Stevia rebaudiana and Siraitia gros-
venori are the three sweet plants in Guangxi.Sweet
flavours could beextracted from the sweet plant and a-
mong them the sweet tea tastes best flavour(Tan,
2008).At present,in order to partly replace sugar in
food additive,some natural,high sweetness and low en-
ergy sweeteners are studied and developed by the sci-
entists around the world.Now the sweet tea has many
sanitarian functions and natural non-toxic,high sweet,
low thermal properties.It hasmedicine sweetness,
sugar,teatriple eficacy and has acquired the Ameri-
can FDA certificate.In Japan,it is recommended as the
second generation health drink and is a sugar and drug
substitute,which the developed countries are vigorous-
ly looking for(Li et al.,2006).It has been used as an
herbal ingredient in decoctions to‘clear internal heat’,
to‘relieve stress on the lungs’,to reduce the secretion
of phlegm,and to relieve cough.It has also been used as
a traditional remedy to treat diabetes,hypertension,and
atherosclerosis,to maintain healthy kidneys and so on.
In recent years,the sweet tea not only has been popular
in the Japanese market,but also in Europe,the Middle
East and the other countries.And with people’s living
standard rising and health awareness enhancing,the
sweet tea market prospects and research prospects wil
be more broad(Tan,2008).
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