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Rubia cordifolia: a review

Authors:
  • Gokhale Education Society's Sir Dr. M.S. Gosavi College of Pharmaceutical Education & Research, Nashik, Maharashtra
  • Mahatma Gandhi Vidyamandir's Pharmacy College, Nashik, Maharashtra, INDIA
  • Rajarshi Shahu College of pharmacy

Abstract

Medicinal herbs are significant source of synthetic and herbal drugs. In the commercial market, medicinal herbs are used as raw drugs, extracts or tinctures. Isolated active constituents are used for applied research. For the last few decades, phytochemistry (study of plants) has been making rapid progress and herbal products are becoming popular. According to Ayurveda, the ancient healing system of India, the classical texts of Ayurveda, Charaka Samhita and Sushruta Samhita were written around 1000 B.C. The Ayurvedic Materia Medica includes 600 medicinal plants along with therapeutics. Herbs like turmeric, fenugreek, ginger, garlic and holy basil are integral part of Ayurvedic formulations. The formulations incorporate single herb or more than two herbs (poly-herbal formulations). Medicinal herb contains multitude of chemical compounds like alkaloids, glycosides, saponins, resins, oleoresins, sesquiterpene, lactones and oils (essential and fixed). Today there is growing interest in chemical composition of plant based medicines. Several bioactive constituents have been isolated and studied for pharmacological activity. R. cordifolia is an important medicinal plant commonly used in the traditional and Ayurvedic system of medicine for treatment of different ailments. This review illustrates its major constituents, pharmacological actions substantiating the claims made about this plant in the traditional system of medicine and its clinical applications.
2009 Kyung Hee University Press 1
Oriental Pharmacy and Experimental Medicine 2009 9(1), 1-13
www.opem.org
OPEM
Review
Rubia cordifolia: a review
Rupali Patil*, Mahalaxmi Mohan, Veena Kasture and Sanjay Kasture
MGVs Pharmacy College, Panchavati, Nashik 422 003, Maharashtra State, India
Received for publication December 17, 2007; accepted November 25, 2008
SUMMARY
Medicinal herbs are significant source of synthetic and herbal drugs. In the commercial market,
medicinal herbs are used as raw drugs, extracts or tinctures. Isolated active constituents are used
for applied research. For the last few decades, phytochemistry (study of plants) has been making
rapid progress and herbal products are becoming popular. According to Ayurveda, the ancient
healing system of India, the classical texts of Ayurveda, Charaka Samhita and Sushruta Samhita
were written around 1000 B.C. The Ayurvedic Materia Medica includes 600 medicinal plants
along with therapeutics. Herbs like turmeric, fenugreek, ginger, garlic and holy basil are integral
part of Ayurvedic formulations. The formulations incorporate single herb or more than two herbs
(poly-herbal formulations). Medicinal herb contains multitude of chemical compounds like
alkaloids, glycosides, saponins, resins, oleoresins, sesquiterpene, lactones and oils (essential and
fixed). Today there is growing interest in chemical composition of plant based medicines. Several
bioactive constituents have been isolated and studied for pharmacological activity. R. cordifolia is
an important medicinal plant commonly used in the traditional and Ayurvedic system of
medicine for treatment of different ailments. This review illustrates its major constituents,
pharmacological actions substantiating the claims made about this plant in the traditional system
of medicine and its clinical applications.
Key words: Rubia cordifolia; Ayurveda; Clinical applications
INTRODUCTION
The family Rubiaceae comprises of about 450
genera and 6500 species and includes trees, shrubs
and herbs (Williams, 2002). Rubia comprises about
60 species. R. cordifolia Linn. (Rubiaceae) is a perennial
climber with very long, cylindrical, flexuose roots
with a thin red bark (Kirtikar and Basu, 1980). In
Sanskrit it is known as Manjistha. This plant has
very long, cylindrical, and flexuous roots with a
thin red colored bark (Anonymous, 1999). Stems
often have a long, rough, grooved, woody base.
Plants belonging to this family are known to
contain substantial amounts of anthraquinones,
especially in the roots (Thomson, 1971; Anonymous,
1999). Flowers are small, white or greenish in
terminal panicles or cymes. Fruits are globose, dark
purplish or black (Williams, 2002). It is distributed
throughout the lower hills of Indian Himalayas in
the North and Western Ghats in the South, and
Japan, Indonesia, Ceylon, Malay, Peninsula, Java
*Correspondence: Rupali Patil, MGVs Pharmacy College,
Panchavati, Nashik-422003 Maharashtra, India. E-mail:
ruupalipatil@rediffmail.com
DOI 10.3742/OPEM.2009.9.1.001
2009 Oriental Pharmacy and Experimental Medicine 9(1), 1-13
2Rupali Patil et al.
and Tropical Africa in moist temperature and
tropical forest, upto an altitude of 3500 m. (Kirtikar
and Basu, 1980; Khare, 2004).
R. cordifolia is used traditionally in the treatment
of liver fluke, dysentery, maggots, wounds and
intestinal worms in animals (Jha, 1992). It is used in
the treatment of skin disorders and has anticancer
activity (Chopra et al., 1957; Adwankar and Chitnis,
1982; Williams, 2002). Roots have tonic, astringent,
antidysenteric, antiseptic, and deobstruent properties.
They are used in rheumatism. Roots are active
against Staphylococcus aureus. Paste of root is
used for application in ulcers, inflammations, and
skin conditions. A decoction of leaves and stems is
used as a vermifuge (Williams, 2002). Scientific
studies show that the anthraquinones of the Rubiaceae
family exhibit some interesting in vivo biological
activities, such as antimicrobial (Sittie et al., 1999),
antifungal (Rath et al., 1995), hypotensive, analgesic
(Younos et al., 1990), antimalarial (Adwankar and
Chitnis, 1982; Koumaglo et al., 1992), antioxidant
(Tripathi et al., 1997), antileukemic and mutagenic
functions (Chang et al., 1995; Ismail et al., 1997).
Apart from its medicinal value, this plant has also
been used as natural food colorants and as natural
hair dye (Samatha et al., 1996). R. cordifolia is often
used in formulations to treat uterine and ovarian
cancer (Halpern, 2004).
Ayurvedic Properties (Williams EM; CHEMEXIL)
Rasa: Kashaya (astringent), tikta (bitter), madhur
(sweet)
Guna: Guru (heavy), ruksha (dry)
Veerya: Ushna (hot)
Vipaka: Katu (pungent)
Dosha: Pacifies kapha and pitta
Karma: Varnya, Jwarhara, Mutrajanya, Swwdajanana,
Twachya
Chemical constituents
Quinones
The plant contains quinines, mainly anthraquinone
glycosides and include 1-hydroxy 2-methoxy
anthraquinone, 1, 4- dihydroxy-2- methyl-5-methoxy
anthraquinone, 1,3- dimethoxy 2- carboxy
anthraquinone and rubiadin) (Dosseh et al., 1981).
Iridoids
6-methoxygeniposidic acid is found along with
manjistin, garancin and alizarin (Wu et al., 1991).
Oleananes triterpinoid
Rubiprasin A, B, and C along with arborane
triterpinoids, like rubiarbonol A, B, C, D, E and F
have been isolated (Itokawa et al., 1989; Itokawa et
al., 1990).
Bicyclic hexapeptides
The compounds having antitumour activity have
been isolated and identified chemically. (Morita et
al., 1992; Takeya et al., 1993).
Anthraquinones
The coloring matter present in the roots of R. cordifolia is
a mixture of purpurin (trihydroxy anthraquinone)
and manjistin (xanthopurpurin-2-carboxylic acid).
The roots contain small amounts of xanthopurpurin or
purpuroxanthin and pseudopurpurin (purpurin-3-
carboxylic acid) (Anonymous, 1999). The plant also
contains dihydromollugin, mollugin, rubilactone
(Hoa LK et al., 2001). Purpurin, belonging to the
lipocalin family of proteins, is a fast dye for cotton
printing and forms complexes with various metal
ions. It is a glycosaminoglycan binding protein as
well as a retinol binding protein.
Alizarin, or 1, 2-dihydroxyanthraquinone or
mordant red, is the red dye originally derived from
the root of the madder plant. In 1869, it became the
first natural pigment to be duplicated synthetically.
The word alizarin is derived from the Arabic word
al-usara, which means juice.
R. cordifolia yielded anthraquinones namely, 1-
hydroxy-2 carboxy 3-methoxyanthraquinone, 1-
hydroxy-2 methyl 6 or 7-methoxy- anthraquinones.
The other compounds were oleanolic acid acetate,
β-sitosterol, and scopoletol. Ten fatty acids with
Rubia cordifolia: a review 3
2009 Oriental Pharmacy and Experimental Medicine 9(1), 1-13
saturated and unsaturated long chains were also
identified (Vidal-Tessier et al., 1986).
The methanol extract of R. cordifolia roots
contains 2 naphthaquinones (Koyama et al., 1992).
2-carbamoyl/2-caurbomyl-3-methoxy-1,4- naphtha-
quinones and 2-carbamoyl-3-hydroxy-1,4- naphtha-
quinones.
Anthraquinones from R. cordifolia:
Alizarin (1, 2-dihydroxy-9,10-anthracenedione)
Purpurin (1, 2, 4-trihydroxyanthracene-9, 10-Dione)
Rubicordifolin
No R R
1 COOMe OH Mollugin
2 COOMe OH Furomollugin
3 COOMe OH Rubilactone
4 COOMe OMe Methylfuromollugin
5 COOMe OMe Mollugin methyl ether
6 COOMe OH Dihydromollugin
7 COOMe OAc Acetylmollugin
8COOCH
CH CH(CH )OMe # I
9 COOMe OCH Ph # II
10 C OOMe OMe Dihydromollugin methyl ether
11 COOMe OMe Methylrubilactone
12 CO OH OM e 2, 2-Dimethyl-6-methoxy-2H-naph-
tho-[1,2-b]pyran-5-carboxylic acid
#I - Isopentyl 2, 2-dimethyl-6-methoxy-2H-naphtho-[1,2-b] pyran-5-car
boxylate
#II - Methyl 2, 2-dimethyl-6-benzoxy-2H-naphtho-[1,2-b] pyran-5-carbox
ylate (Morita et al., 1992).
Qiao et al. (1990) isolated 12 compounds from roots of R.cordifolia of which
9 compounds have been characterized by chemical and spectroscopic
methods as -
1. Alizarin
2. 1-hydroxy-2-methyl-9,10-anthraquinone
3. 1,3,6-trihydroxy-2-methyl-9,10-anthraquinone-3-O-(6’-o-acetyl)-alpha-L-
rhamnosyl (1 to 2) – beta- D-glucoside
4. 1,3,6-trihydroxy-2-methyl-9,10-anthraquinone-3-O-alpha-L-rhamnosyl
(1 to 2)–beta- D-glucoside
5. 1,3,6-trihydroxy-2-methyl-9,10-anthraquinone-3-O-(6’-o-acetyl)-beta-D-
glucoside
6. 2-carbomethoxy-3-pr enyl-1-4-naphthohydroquinone di-beta-D-glucoside
7. Rubimallin
8. β-sitosterol
9. Damosterol
2009 Oriental Pharmacy and Experimental Medicine 9(1), 1-13
4Rupali Patil et al.
Bicyclic hexapeptides from R. cordifolia:
RA-XIV
RA-XVI (Takeya et al., 1993)
Traditional uses in different systems of herbal
medicine
Unani system of medicine
R. cordifolia has been prescribed for paralysis, dropsy,
jaundice, amenorrhoea, urinary tract obstructions,
skin disorders of many varieties, menstrual disorders
(excessive or painful bleeding), renal stone, urinary
disorders and blood detoxification (www.
raynaudshern.com).
Chinese system of medicine: Roots help menstrual
flow, promote blood circulation, promote urination,
stop coughing blood or vomiting blood, nose bleeding.
The plant is also useful in treatment of missing
menses due to blood stasis, cold damp heat bi
(pain and inflammation caused by bleeding and
blood circulation stasis), injuries from impacts and
in jaundice and edema (www.alternativehealing.org).
Ethnoveterinary usage
R. cordifolia is used in the treatment of liver fluke,
dysentery, maggots, wounds and intestinal worms
in animals (Jha, 1992).
Pre-Clinical Studies
In vitro studies
Rubia cordifolia: a review 5
2009 Oriental Pharmacy and Experimental Medicine 9(1), 1-13
Calcium channel blocker(s) in R. cordifolia
The calcium channel antagonistic activity of a
crude root extract of R. cordifolia was tested in
isolated tissue preparations. The extract (0.1 - 3
mg/ml) augmented spontaneous contractions of
guinea pig atria, rabbit jejunum and rat uterus in a
concentration-dependent manner. In rabbit aorta,
the extract inhibited norepinephrine-(10 fM) and
KCl (80 mM) induced contractions. Spontaneous
movements of rabbit jejunum were abolished in a
calcium-free solution. Addition of calcium (25 fg/ml)
restored the spontaneous movements. When tissues
were pretreated with plant extract (1 mg/ml) or
verapamil (0.5 fg/ml), addition of calcium failed to
restore spontaneous contractions. These results
indicate that the extract exhibits spasmolytic activity
similar to that of verapamil suggestive of presence
of calcium channel blocker- like constituent(s)
(Gilani et al., 1994).
Anti-acne property
Propionibacterium acnes, an anaerobic pathogen,
plays an important role in the pathogenesis of acne
by inducing certain inflammatory mediators.
These mediators include reactive oxygen species
(ROS) and pro-inflammatory cytokines. In the
study, ROS, interleukin-8 (IL-8) and tumor necrosis
factor-Y (TNF-Y) were used as the major criteria for
the evaluation of anti-inflammatory activity. The
polymorphonuclear leukocytes (PMNL) and monocytes
were treated with culture supernatant of P. acnes in
the presence or absence of herb. It was found that
R. cordifolia caused a statistically significant
suppression of ROS from PMNL. Thus, R. cordifolia
Table 1. Some of the ayurvedic preparations containing R. cordifolia Linn. (Rubiaceae)
Sr. no. Name of preparation Indications Citations
1 Aswagandharistam
Epilepsy, faintness, fatigue, psychic problems, piles,
indigestion, rheumatic complaints etc. Improves mem-
ory power.
Baishajyaratnavali
2 Chandanasavam
Burning micturition, leucorrhocat etc. Improves body
strength and digestive system. Keeps the body cool
and also maintain good general health.
Yogaratnakaram
3 Devadarvarishtam Diabetes, rheumatic complaints, sprue syndrome,
piles, difficult urination, skin diseases etc. Baishajyaratnavali
4 Eladyarishtam Chickenpox, skin diseases like urticaria, dermatitis
and allergic itching Yogaratnakaram
5 Gulguluthikthkarishtam
Recommended in acute rheumatic conditions, chronic skin
diseases, sinusitis, lymph adunosis, diseases related with
head, neck and throat, abscess and obesity.
Ashtangahridayam
6 Madhookasavam Diabetes, skin diseases, sprue syndrome and oedema.
Also as a tonic for general well-being. Ashtangahridayam
7 Manjishtasavam For all types of skin diseases and vatha sonitha,
especially for vitiated pitha and kapha vikaras. Ashtangahridayam
8 Nimbamrithasavam
Recommended in acute rheumatic conditions, skin
diseases, and sinusitis, obesity, and lymph adenoids
around neck, diseases related with head, neck and
throat abscess.
Ashtangahridayam
9 Useerasavam For burning sensation of head and body, vertigo,
disturbed sleep, tachycardia etc. Yogaratnakaram
10 Jaatyaadi ghrita Applied externally for chronic and septic ulcers Ashtaanga Hridaya
11 Phal kalyaan ghrita Used for amenorrhea and uterine affections Bhaishajya Ratnaavali
12 Majishthaadi taila Used for headache Sahasrayoga
2009 Oriental Pharmacy and Experimental Medicine 9(1), 1-13
6Rupali Patil et al.
showed anti-inflammatory activity by suppressing
the capacity of P. acnes-induced ROS and pro-
inflammatory cytokines, the two important
inflammatory mediators in acne pathogenesis (Jain
and Basal, 2003).
Antimicrobial action
R. cordifolia is used as a dye from natural sources
therefore a study was taken up to test if some
natural dyes have inherent antimicrobial activity
with a view to develop protective clothing from
these. R. cordifolia was tested against common
pathogens Escherichia coli, Bacillus subtilis, Klebsiella
pneumoniae, Proteus vulgaris and Pseudomonas aeruginosa.
The textile material impregnated with these natural
dyes, however, showed less antimicrobial activity,
as uptake of these dyes in textile material is below
MIC. The antibacterial activity of the extracts of R.
cordifolia roots prepared with solvents of different
successive polarities was evaluated by the agar-
well diffusion method. It inhibited both gram
positive and gram negative strains (Singh et al.,
2005; Vlietinck, 1995). Many compounds were
isolated, established by chemical and spectroscopic
methods from the roots of R. cordifolia L. Some of
the compounds showed certain antibacterial activities
(Qiao et al., 1990). In one study some antimicrobial
agents, emodin and physcion were isolated as the
most active constituents (Basu et al, 2005).
In vivo studies
Antidiabetic Action
The antidiabetic action of R. cordifolia Linn (Rubiaceae)
aqueous root extract (RCAREt) was examined in
streptozotocin (STZ)-induced diabetic rat model.
Serum glucose, total cholesterol and triglycerides,
hematological parameters, and liver and kidney
transaminases in normal, STZ diabetic, and RCAREt-
treated diabetic rats were measured. The observed
hyperglycemia, hypertriglyceridemia, enhanced
transaminases of liver and kidney, hypochromic
microcytic anemia, and loss of body weight in STZ
diabetic rats were normalized by RCAREt treatment,
whereas the hypercholesterolemia was not rectified.
The beneficial effect of RCAREt treatment might be
due to different types of active principles, each with a
single or a diverse range of biological activities (Baskar
et al., 2006). The effect of ethyl acetate fraction of
roots of R. cordifolia (RCEAF) was investigated on
blood glucose level and glucose utilization to find
out the mechanism of action of the extract. Ethanolic
extract of roots of R. cordifolia L. was reported to be
hypoglycemic and it was fractionated by column
chromatography. Single dose study of RCEAF (50,
100 and 200 mg/kg, p.o.) was carried out in i)
normal fasted ii) oral glucose tolerance test (OGTT)
iii) alloxan (120 mg/kg, s.c.)- induced diabetic rats.
Repeated dose study of RCEAF (100 and 200 mg/kg,
p.o.) was carried out for two weeks. It was found
that, oral pre-treatment with RCEAF induced a
significant (P< 0.05) decrease in blood glucose
levels as compared to diabetic control rats. In the
same line an in vitro experiment showed that
insulin (0.05 IU/mL) increased glucose utilization
by an isolated rat diaphragm. Alone RCEAF (25
mg/mL) as well as combination of RCEAF (25
mg/mL) and insulin (0.05 IU/mL) showed a
marked increase (P < 0.05) of glucose uptake. This
exhibited the extra- pancreatic effect of the RCEAF.
Further studies with estimation of insulin and
insulin receptor may give more insight into the
mechanism of the antidiabetic activity of the R.
cordifolia (Somani et al., 2006). Administration of the
alcoholic extract of roots of R. cordifolia showed
significant hypoglycemic effect in alloxan induced
diabetic rats (Patil et al., 2006).
Anti-oxidant activity
Prolonged oral treatment of rats with ethanol (2 g/kg
of 20% w/v) significantly increased the levels of
lipid peroxidase (LPO), decreased the activities of
superoxide dismutase (SOD) and catalase (CAT)
and reduced the content of glutathione (GSH). The
concurrent treatment of ethanol-administered rats
with R. cordifolia prevented these above mentioned
ethanol-induced changes in the markers of oxidative
Rubia cordifolia: a review 7
2009 Oriental Pharmacy and Experimental Medicine 9(1), 1-13
stress. Influences of R. cordifolia on ethanol-induced
changes were comparable with those produced by
vitamin E and C treatment (Joharanpurkar et al., 2003).
Rubiadin, a dihydroxy anthraquinone, isolated
from alcoholic extract of R. cordifolia, possesses potent
antioxidant property. It prevents lipid peroxidation
induced by FeSO4 and t-butylhydroperoxide (t-
BHP) in a dose-dependent manner. The percent
inhibition was more in the case of Fe2+ induced
lipid peroxidation. The antioxidant property of the
preparation was better than the EDTA, Tris,
mannitol, Vitamin E and p-benzoquinone (Tripathi
et al., 1997).
Antiproliferative activity
The antiproliferative property of R. cordifolia extract
has been studied on two different cell types, A-431
cells (epidermal carcinomoid cells) and 3T3 fibroblast
cells. A fraction of R. cordifolia significantly inhibited
the incorporation of 3H-thymidine induced by
fetal bovine serum, in a dose-dependent manner. It
also inhibited the phorbol 12-myristate 13-acetate
(PMA)-induced expression of c-fos genes in A-431
cells. Inhibition of DNA synthesis underlies the
mechanism for its antiproliferative properties
(Tripathi et al., 1998).
Hepatoprotective Activity
The hepatoprotective activity of an aqueous-
methanol extract of R. cordifolia was investigated
against acetaminophen and CCl4-induced hepatic
damage. Acetaminophen produced 100% mortality
at a dose of 1 g/kg in mice while pretreatment of
animals with R. cordifolia extract reduced mortality
to 30%. Acetaminophen at a dose of 640 mg/kg
produced liver damage in rats as manifested by the
rise in serum levels of glutamic oxaloacetic transaminas e
(SGOT) and glutamate pyruvate transaminase (SGPT).
Pretreatment of rats with R. cordifolia extract lowered
significantly the SGOT and SGPT levels. Similarly,
hepatotoxic dose of CCl4 raised the SGOT and
SGPT levels respectively compared with respective
control. The same dose of R. cordifolia was able to
prevent significantly the CCl4-induced rise in
serum enzymes and the estimated values of SGOT
and SGPT. Moreover, it prevented CCl4-induced
prolongation in pentobarbital-induced sleep
confirming the hepatoprotective effects of the
extract (Gilani et al., 1995).
The hepatoprotective activity of rubiadin was
evaluated against carbon tetrachloride (CCl4)-induced
hepatic damage in rats. Rubiadin at a dose of 50,
100 and 200 mg/kg was administered orally once
daily for 14 days. The substantially elevated serum
enzymatic activities of SGOT, SGPT, serum alkaline
phosphatase (SALP) and γ-glutmyltransferase (γ-GT)
due to carbon tetrachloride treatment were dose
dependently restored towards normalization.
Meanwhile, the decreased activities of glutathione
S-transferase and glutathione reductase were also
restored towards normal. In addition, rubiadin also
significantly prevented the elevation of hepatic
melondialdehyde formation and depletion of
reduced glutathione content in the liver of CCl4
intoxicated rats in a dose dependent manner.
Silymarin used as reference standard also exhibited
significant hepatoprotective activity on post treatment
against carbon tetrachloride induced hepatotoxicity in
rats. The biochemical observations were supplemented
with histopathological examination of rat liver
sections. The results of this study strongly indicate
that rubiadin has a potent hepatoprotective action
against carbon tetrachloride induced hepatic
damage in rats (Mohana et al., 2006).
Anti-platelet activating factor activity
R. cordifolia is clinically used for the purification of
blood by the physicians of the Indian Systems of
Medicine. The effect of the partially purified
fraction of this whole plant had been studied on
rabbit platelets. It inhibited the platelet aggregation
induced by PAF (platelet activating factor) but not
thrombin. PAF (platelet activating factor) is a
phospholipids involved in thrombosis, allergy and
nervous disorders. R. cordifolia extract also inhibited
the binding of 3H labeled-PAF to the platelets in
2009 Oriental Pharmacy and Experimental Medicine 9(1), 1-13
8Rupali Patil et al.
the dose-dependent manner. Thus it appears that
R. cordifolia inhibits action of PAF at its receptor
level either by its blocking or by desensitization
(Tripathi et al., 1993).
Antitumour activity
The cyclic hexapeptides and quinones of Rubia
exhibited a significant anticancer activity against
various proliferating cells. The hexapeptides showed
potent antitumour activity by binding to eukaryotic
80S ribosomes resulting in inhibition of aminoacyl
-tRNA binding and peptidyl – tRNA translocation,
thus leading to the stoppage of protein synthesis
(Morita, 1992, Morita, 1993, Itokawa, 1993). The
antitumor activity of RA-700, a cyclic hexapeptide
isolated from R. cordifolia, was evaluated in
comparison with deoxy-bouvardin and vincristine
(VCR). The antitumor activity of RA-700 was
similar to that of deoxy-bouvardin and VCR
against P388 leukemia. As with deoxy-bouvardin
and VCR, the therapeutic efficacy of RA-700 depends
on the time schedule. RA-700 showed marginal
activity against L1210 leukemia (50% ILS), similar
to that of deoxy-bouvardin but inferior to that of
VCR. RA-700 inhibited Lewis tumor growth in the
early stage after tumor implantation, whereas
deoxy-bouvardin and VCR did not. A slight
reduction of peripheral WBC counts was observed
with the drug, but no reduction of RBC and
platelet counts. Bilirubin, creatinine, GPT and GOT
levels in plasma did not change with the administration
of the drug (Kato, 1987). The anticancer as well as
antiviral property had been reviewed (Rastogi and
Dhawan, 1990). From the chloroform fraction of R.
cordifolia roots three constituents were isolated
namely mollugin, furomollugin and dehydro-a-
lapchone. Mollugin has shown inhibition of passive
cutaneous anaphylaxis (PCA) and protection of
mast cell degranulation in rats. It also exhibited
considerable activity against lymphoid leukemia
(P338) in mice (Gupta, 1999). The R. cordifolia
extract had shown a mitodepressive effect on the
rate of cell division in bone marrow cells of Swiss
male mice. This exposure-time-dependent reduction
was attributed to the effect of inhibiting protein
synthesis, suggesting probable effect of Rubia
extract on the biosynthesis of certain amino acids
as well as RNA synthesis (Abderrahman, 2004). R.
cordifolia had shown an increase in leukocyte count
in leucopenia (Zhang, 1983).
The cytotoxic action of R. cordifolia had been
evaluated with DNA Topoisomerases I and II
inhibition and cytotoxicity of constituents isolated
from the roots was tested. Topoisomerases I and II
inhibitory activities were measured by assessing
the relaxation of supercoiled pBR 322 plasmid
DNA. The tetrazolium-based colorimetric assay
(MTT assay) was used for the cytotoxicity towards
human colon carcinoma (HT-29), human breast
carcinoma (MCF-7) and human liver carcinoma
(HepG2) cell lines. Seven compounds were isolated
possessing cytotoxic activity (Son JK, 2006). Anti-
tumor activity of RC-18, a pure isolate from R.
cordifolia, was repeatedly tested in different sets of
experiments on a spectrum of experimental murine
tumors, viz P388, L1210, L5178Y, B16 melanoma,
Lewis lung carcinoma and sarcoma-180. RC-18
exhibited significant increase in life span of ascites
leukemia P388, L1210, L5178Y and a solid tumor
B16 melanoma. However, it failed to show any
inhibitory effect on solid tumors, Lewis lung
carcinoma and sarcoma 180. Promising results
against a spectrum of experimental tumors suggested
that RC-18 may lead to the development of a
potential anti-cancer agent (Adwankar and Chitnis,
1982). The anticancer activity of extracts of R.
cordifolia, tested against the P388 tumor system in
BDF1 mice, compared well with that of the positive
control, 5-fluorouracil (Adwankar et al., 1980).
Anti-inflammatory activity
R. cordifolia is considered to be traditionally useful
as an analgesic, astringent, external application in
inflammations, ulcers and skin diseases (Khalid,
1995). The plant is also claimed to relieve the
symptoms of pruritus, burning and exudation
Rubia cordifolia: a review 9
2009 Oriental Pharmacy and Experimental Medicine 9(1), 1-13
from skin (Nadkarni, 1976). During studies in
patients with eczema, the topical application of the
plant showed a 50 % reduction in the severity score
within 4 days, the oedema, exudation and itching
being significantly relieved (Bapalal, 1965). R.
cordifolia was studied for the anti-inflammatory
effect in rats with carrageenan paw oedema. The
plant showed significant anti-inflammatory activity at
a dose of 10 and 20 ml/kg of the water extracts. The
activity was comparable to that of phenylbutazone (100
mg/kg) (Antarkar et al, 1983). R. cordifolia inhibited
the lipoxygenase enzyme pathway and the production
of cumene hydroperoxides. The lipoxygenase
pathway catalyses the production of various
inflammatory mediators such as the leukotrienes
which are involved in asthma, arthritis, and other
inflammatory disorders (Tripathi et al, 1995).
Radioprotective effect
The radioprotective potential of alcoholic extract of
root of R. cordifolia was studied by survival,
hemopoietic cell protection and micronucleus
assay. The LD50 value for the alcoholic root extract
was found to be 1200 mg/kg body weight at 72 h
post irradiation. A significant radiation protection
(67%) as assessed by increased animal survival was
observed when R. cordifolia extract was administered
intraperitoneally, 90 min. before the radiation
exposure. Besides, the extract also inhibited
radiation induced lipid peroxidation measured by
the inhibition of thiobarbituric acid reactive
substance (TBARS). The R. cordifolia extract at a
selected dose of 460 mg/kg body weight was
effective in protecting the radiation induced
suppression of endogenous colony forming units
in spleen. A significant inhibition of radiation-
induced micronuclei formation was observed
when R. cordifolia extract was administered 90 min
prior to irradiation. Thus, it appears that the
alcoholic root extract of R. cordifolia provides
significant protection against radiation induced
lipid peroxidation, hemopoietic injury and genotoxicity.
The mechanism of action of R. cordifolia extract
appears to be through its anti-oxidant, metal
chelation and anti-inflammatory property (Tripathi
and Singh, 2007).
Anti-proliferative property
Psoriasis is a chronic inflammatory skin disorder,
which affects approximately 2 - 3% of the population
worldwide. Traditionally, herbal medicines have
been extensively used to treat psoriasis and
produced promising clinical results; however, the
underlying mechanisms of action have not been
systematically investigated. Roots of R. cordifolia L
were extracted with 80% aqueous ethanol. The dry
extract was evaluated for anti-proliferative activity
by microplate SRB and MTT assays. It was found
to have significant anti-proliferative effect, as
measured by MTT assay. R. cordifolia did not exert
cytotoxicity to this human fibroblast cell line (Tse et
al., 2006). The antiproliferative property of R.
cordifolia (Rubiaceae) extract was also tested on A-
431 cells (epidermal carcinomoid cells) and 3T3
fibroblast cells. It was observed that a fraction of R.
cordifolia significantly inhibited the incorporation
of [3H]-thymidine, induced by fetal bovine serum,
in a dosedependent manner. It also inhibited the
PMA (phorbol 12- myristate 13-acetate) induced
expression of c-fos genes in A-431 cells. It appears
that inhibition of DNA synthesis underlies the
mechanism for its antiproliferative properties
(Tripathi and Shukla, 1998).
Inhibitory action on nitric oxide production
R. cordifolia is used for prevention and treatment of
inflammatory diseases, therefore water and methanol
extracts of R. cordifolia were screened for their
inhibitory effects on nitric oxide (NO) production
in lipopolysaccharide (LPS)-stimulated J774.1
macrophages and in LPS/interferon (IFN)-B-
stimulated mouse peritoneal exudate macrophages.
The methanol extract R. cordifolia, showed significant
inhibition in J774.1 macrophages, while in mouse
peritoneal exudate macrophages, water extract of
R. cordifolia inhibited the nitric oxide (NO)
2009 Oriental Pharmacy and Experimental Medicine 9(1), 1-13
10 Rupali Patil et al.
production. Water extract of R. cordifolia showed
inhibition on iNOS mRNA expression (Tezuka et
al., 2001). The inhibition of NO is found to be a key
mediator in the phenomenon of inflammation.
Thus R. cordifolia was evaluated for inhibitory
activity on NO produced in-vitro from sodium
nitroprusside, and in LPS-activated murine peritoneal
macrophages, ex vivo (Basu and Hazra, 2006). The
inhibition of NO synthesis was correlated with the
reduction of iNOS protein expression through
Western blot. Notable NO scavenging activity was
exhibited in vitro by extracts of R. cordifolia (IC50 < 0.2
mg/mL). It showed marked inhibition (60 - 80%),
ex vivo, at a dose of 80 ug/mL without appreciable
cytotoxic effect on the cultured macrophages.
Immunoblot analysis confirmed that the modulatory
effect of the samples had occurred through suppression
of iNOS protein suggestive of potential inhibition
of NO production.
Wound healing activity
Several drugs of plant, mineral and animal origin
are described in the Ayurveda for their wound
healing properties under the term vranaropaka.
R. cordifolia was also found to be effective in
experimental models (Biswas and Mukherjee, 2003).
Anti-allergic activity
Alcoholic extract of R. cordifolia inhibited passive
cutaneous anaphylaxis (PCA) in the mouse and rat
(Gupta et al., 1993).
Anticonvulsant activity
Triterpenes isolated from the acetone soluble part
of petroleum ether extract of R. cordifolia inhibited
seizures induced by maximum electroshock (MES),
electrical kindling, pentylenetetrazol (PTZ), and
lithium-pilocarpine. However seizures induced by
strychnine were not inhibited (Kasture et al., 2000).
Pentobarbitone-induced sleep
Mice treated orally with triterpenes isolated from
the petroleum ether extract of R. cordifolia significantly
prolonged the pentobarbitone-induced sleeping
time (Kasture et al., 2000).
Antinociceptive activity
Mice treated with triterpenes isolated from the
petroleum ether extract of R. cordifolia exhibited
significant antinociceptive activity as indicated by
increase in the reaction time in the hot plate
analgesiometer (Kasture et al., 2000).
Anxiolytic activity
Mice treated with triterpenes isolated from the
petroleum ether extract of R. cordifolia exhibited
anxiogenic activity by remaining for most of the
time in the closed arm 38. Whereas, the ethanolic
extract exhibited anxiolytic activity as indicated by
a significant increase in open arm occupancy
(Kasture et al., 2000).
Nootropic activity
Alcoholic extract of roots of R. cordifolia decreased
transfer latency in the elevated plus maze paradigm
suggesting nootropic activity. Alcoholic extract of
R. cordifolia antagonized amnesic effect of scopolamine
(Patil et al., 2006).
Effect on motor co-ordination
Alcoholic extract of roots of R. cordifolia significantly
decreased the fall off time when placed on rotarod
rotating at the speed of 20 rev/min (Patil et al., 2006).
Antistress activity
Alcoholic extract of roots of R. cordifolia significantly
decreased ulcer index, acidity, plasma corticosterone
level, brain content of dopamine in a dose-dependent
manner in animals under cold restraint stress
(CRS) when compared with diazepam. Alcoholic
extract of R. cordifolia increased brain content of
GABA in dose-dependent manner in CRS treated
animals (Patil et al., 2006).
Effect on baclofen induced catatonia
Alcoholic extract of R. cordifolia potentiated baclofen-
Rubia cordifolia: a review 11
2009 Oriental Pharmacy and Experimental Medicine 9(1), 1-13
induced catatonia (Patil et al., 2006).
Clinical studies
Eczema
During recent studies in patients with eczema, the
topical application of the plant showed a 50%
reduction in the severity score within 4 days, the
oedema, exudation and itching being significantly
relieved (Antarkar et al., 1978).
Phase I Study of RA-700
Phase I clinical study was conducted on an
antitumour substance RA-700 isolated from Rubia
akane or R. cordifolia. This clinical study was
carried out in 6 institutions. The effects of a single
dose administration and 5-day administration
were evaluated in 14 patients. RA-700 was given
from 0.2 to 1.4 mg/M2 in single i.v. dose and from
0.4 to 2.0 mg/M2 in 5-day i.v. dose schedule. Nausea,
vomiting, fever, stomachache, mild hypotension
and slight abnormality of electrocardiogram were
observed. In pharmacokinetic study, the elimination
half-lives (t1/2) of RA-700 in plasma were: 55 min
of alpha-phase and 3.9 h of beta-phase by single
dose study, and 23 - 25 min of alpha-phase and
6 - 14 h of beta-phase by 5-day schedule study.
Accumulation was not found in 5-day schedule
administration and metabolites were not observed
in plasma and urine. It seems that RA-700 was
metabolized by the liver and excreted in the feces.
In conclusion, the maximum tolerated dose was 1.4
mg/M2 for 5-day schedule administration (Majima et
al., 1993).
Inhibition of Hepatitis B Surface Antigen Secretion
on Human Hepatoma Cells by Components of R.
cordifolia
The antiviral activity in the roots of R. cordifolia was
examined, and three naphthohydroquinones,
furomollugin, mollugin, and rubilactone were
isolated from it. Furomollugin and mollugin strongly
suppressed the secretion of hepatitis B surface
antigen (HBsAg), furomollugin and mollugin showed
IC50 = 2.0 μg/mL, in human hepatoma Hep3B cells
while having little effect on the viability of the cells.
A 6-hydroxy group and a pyran or furan ring
contribute to suppressive effect of furomollugin
and mollugin (Ho et al., 1996).
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... In Ayurveda, R. cordifolia has been used as a coloring agent for medicinal oils, and applied externally to inflamed areas, ulcers and fractures. R. cordifolia root has been treated various chronic inflammations (Deshkar et al., 2008;Patil et al., 2009). A paste made from honey is applied to the skin to remove brown spots, freckles and other skin discoloration and is used to promote wound healing (Adwankar et al., 1980;Pawar et al., 2009). ...
... In Uganda medicine, traditional healers use the drug to treat tuberculosis cases. In the Philippines medicine, root decoction of R. cordifolia is used to treat urinary tract disorders (Patil et al., 2009). In traditional Asian medicine, the roots of R. cordifolia have become an important drug for the treatment of abnormal uterine bleeding (AUB), purpura lupus erythematosus, hemorrhage syndrome, arthritis, kidney stones, hemostasis, hysteresis, and psoriasis (Chang et al., 2000;Basu et al., 2005;Tse et al., 2007;Son et al., 2008;Wang K. et al., 2020). ...
Article
Full-text available
Rubia cordifolia (family: Rubiaceae) L (R. cordifolia) is a perennial botanical drug climbing vine. As the main part of the traditional Chinese medicine, the rhizome has a long history. A great number of literary studies have reported that it can be used for the improvement of blood circulation, hemostasis, activation of collaterals, etc. When it comes to the wide application of R. cordifolia in traditional medicine, we systematically review its traditional uses, phytochemistry and pharmacological effects. Literatures were systematically searched using several scientific databases, including China National Knowledge Infrastructure (CNKI), Baidu Scholar, PubMed, Web of Science, and other professional websites. Kew Botanical Garden and the iPlant were used for obtaining the scientific names and plant images of R. cordifolia. In addition, other information was also gathered from books including traditional Chinese herbal medicine, the Chinese Pharmacopoeia, and Chinese Materia Medica. So far, many prescriptions containing R. cordifolia have been widely used in the clinical treatment of abnormal uterine bleeding, primary dysmenorrhea and other gynecological diseases, allergic purpura, renal hemorrhage and other diseases. The phytochemistry studies have reported that more than 100 compounds are found in R. cordifolia, such as bicyclic peptides, terpenes, polysaccharides, trace elements, flavonoids, and quinones. Among them, quinones and peptides are the types of components with the highest contents in R. cordifolia. The modern pharmacological studies have revealed that R. cordifolia and its derived components have anti-tumor, anti-oxidative, anti-platelet aggregation, and anti-inflammatory effects. However, most studies are preclinical. The pharmacological mechanism of R. cordifolia has not been thoroughly studied. In addition, there are few pharmacokinetic and toxicity studies of R. cordifolia, therefore the clinical safety data for R. cordifolia is lacking. To sum up, this review for the first time summarizes a systemic and integrated traditional uses, chemical compositions, pharmacological actions and clinical applications of R. cordifolia, which provides the novel and full-scale insight for the drug development, medicinal value, and application of R. cordifolia in the future.
... usage -Comme quelques autres espèces du genre, R. cordifolia, -la garance indienne -, était souvent cultivée, surtout en Inde jusqu'au XIX e siècle, pour obtenir un colorant rouge à partir de ses racines. L'espèce joue aussi un rôle en médecine ayurvédique (voir Patil & al. 2009). En Afrique, sa culture n'a pas été pratiquée (voir Zimudzi 2005). ...
... Ici, nous suivons Verdcourt (1976) et Puff (1984 qui ont proposé de considérer les populations africaines subsahariennes, relativement homogènes morphologiquement, comme représentant une seule sous-espèce. Patil & al. (2009), Puff (1984, Verdcourt (1975Verdcourt ( , 1976Verdcourt ( , 1989, Zimudzi (2005). ...
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... Changes in duration of cycle, duration of flow and amount of flow was achieved in 66.7%, 96.7%, 86.7% patients respectively, and weight reduction in 60% patients (Table 7). hepato-protective activity, anti-cancer, antioxidant, anti-inflammatory, insulin sensitizer and stimulating effect on uterine muscle fibres due to presence of active ingredient such as cinnamic acid, cinamaldehyde, eugenol, essential oil, tanins, rubiadin, methanol extract [34][35][36] alloxan, triterpenoids, rubimalin saponins, Anthraquinone and their glycosoids, quinone and flavonoids, [37] Finally, it can be concluded that the research drug formulation studied can be used as alternate remedy in PCOD patients, as it has significant effect in menstrual cyclicity by reduction of weight and probably by improving the insulin resistance in PCOD. ...
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... An earlier study reported that rubiadin possesses strong antioxidant property and hence inhibit the lipid peroxidation process which is induced by FeSO 4 and t-butyl-hydroperoxide [37]. Rubiadin also possesses strong anti-inflammatory, immune-modulatory, anticonvulsant, anxiolytic, and anti-diabetic activity [38]. In earlier finding, rubiadin and rubiadin 1-methyl ether were proved to be good constituents of Morinda citrofolia. ...
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Plants and their bioactive compounds are used in medicinal practices since ancient times. The Himalayan region possesses a large number of medicinal plants, which have been used to prevent and cure several human diseases. Diabetes is a major public health problem, which affects millions of people worldwide. Due to its complexity and impact on whole body hemodynamics, there is no cure for any type of diabetes, and most of the available drugs only help manage the symptoms to a certain extent. Moreover, the development of drug with lesser or no side effects is still a challenge to the medical system. Plant products and their derived active compounds can be possible alternatives for the treatment of diabetes without much adverse effects. Therefore, analysis on such plants and their metabolites has become important. However, routine efforts to identify the plant-based active compounds are not sufficient and there is a need for more rigorous scientific validation to ensure their efficacy, safety, and consistency. In addition, analysis of the chemical structure of a bioactive compound and its relationship with biological activity (structure–activity relationship or SAR) is crucial as it allows the modification of the bioactive compound by changing its chemical structure; this can be considered as a powerful tool in the discovery of drugs, which are very selective and have less side effects. Although several plant-based medicines are being used traditionally for treating diabetes and have been scientifically validated, their mechanism of action is yet to be defined. Here, we review several plant species of the Himalayan region that can be effectively used to treat diabetes and their bioactive compounds having antidiabetic properties and discuss their structure–activity relationship and probable molecular mechanism underlying these properties.
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