GILOY (TINOSPORA CORDIFOLIA)
Chakralakshanika (Sanskrit),Gulancha (Bengali), Gurcha (Hindi),Galac (Gujarati), Thippateega (Telugu), Amrutavalli (Kannada), Amrita,Gilo (Kashmiri), Chittamrutu (Malayalam), Gulvel (Marathi), Guluchi (Oriya), Gilo (Punjabi), Seendal,Seendil,Kodi(Tamil), Siddhilata,Amarlata (Assamese) Heartleaf Moonseed, Tinospora (English). Guduchi, the Sanskrit name, means one which protects the entire
body. The term amrita is
attributed to its ability to impart youthfulness, vitality and longevity. The
chemical constituents present in this shrub belong to different classes, such
as alkaloids, diterpenoid lactones, glycosides, steroids, sesquiterpenoid,
phenolics, aliphatic compounds and polysaccharides. Various properties of T.
cordifolia, described in ancient
texts of Ayurveda, like Rasayana, Sangrahi, Balya,
Agnideepana, Tridoshshamaka, Dahnashaka, Mehnashaka, Kasa-swasahara,
Pandunashaka, Kamla-Kushta-Vataraktanashaka, Jwarhara, Krimihara, Prameha,
Arshnashaka, Kricch-Hridroga nashak,
etc., are acquiring scientific validity through modern research adopting
"reverse pharmacological" approach.
Ayurvedic Properties of T. Cordifolia (Guruchi)
|
Rasa
|
Guna
|
Virya
|
Vipaka
|
Prabhava
|
|
Tikta, Kasya
|
Laghu, Guru, Snigdha
|
Usna
|
Madhur
|
Vishaghna
|
|
Bitter, Astringent
|
Light, Heavy, Unctuous
|
Hot potency
|
Neutral
|
Anti-toxic
|
Various Action & Indication of Guruchi According to
Different Ayurvedic Classical Text
|
Karma /Action
|
Indication /Uses
|
Classical Ayurvedic Reference
|
|
Rasayana, Sangrahi, Balya, Agnidipana,
Tridoshshamaka
|
Daha, Meha, Kasa, Pandu, Kamla, Kushta,
Vatarakta, Jwara, Krimi, Prameha, Swas, Arsha, Kriccha, Hridroga
|
Bhav
Prakash Nighantu, Guduchyadi Varga; 8-10
|
|
Vata-Pitta-Kaphanashak, Trishnanashaka,
Agnideepaka
|
Jwara, Chardi, Daha
|
Astang
Sangrah Sutrasthan 7-149, 16-10
|
|
Sangrahi, Vatahara, Agnideepana, Shlesm-Shonit-
Prashamana
|
Vivandha
|
Charak
samhita Sutrastana 25-40
|
|
Tridoshnashaka, Vishaghni, Jwara-bhootaghni
|
Jwara, Daha, Trishna, Vatarakta, Prameha, Pandu,
Bhrama, Balipalita
|
Raja
Nighantu Guduchyadi Varga 17,18
|
|
Dipana, Grahi
|
Kasa, Pandu, Jwara
|
Ark
Prakash Tritiya Shatak
|
|
Balya, Tridoshnashaka
|
Laghujwara, Meha, Daha, Kasa, Pandu, Vitsarana
(Atisara)
|
Siddh
Bheshaja Mani Mala, Dwitiya guccha 70
|
|
Tridoshghni, Grahi, Rasayana, Dipana
|
Jwara, Daha, Kamla, Vatarakta
|
Shodhal
Nighantu, Guna Sangraha, Guduchyadi Varga-120
|
|
Sangrahi, Balya, Agnidipana
|
Kamla, Kushta, Vatarakta, Jwara, Pitta, Vivandha,
Krimi
|
Madan
Pal Nighantu, Harityakadi Varga-39,40,41
|
|
Sangrahi, Vrishya, Balya, Rasayana, Dipana,
Chakshusya, Vayah-Sthapana, Medhya, Tridoshanashaka
|
Kushta, Krimi, Chardi, Daha, Vatarakta, Pandu,
Jwara, Kamla, Meha, Trishna, Kasa
|
Kaidev
Nighantu, Aushadhi Varga-9,10,11
|
|
Tridoshanashaka, Aayushyaprada, Medhya, Sangrahi
|
Jantu, Raktarsha, Raktavata, Kandu, Visarpa,
Kushta, Visha, Bhoota, Valipalita, Chardi, Meha, Jwara
|
Dhanvantari
Nighantu, Guduchyadi- 5,6,7,8
|
|
Grahi, Balya, Rasayana, Dipana, Hriddhya,
Aayushyaprada, Chakshusya, Tridoshaghna
|
Jwara, Chardi, Kamla, Daha, Trisha, Bhrama,
Pandu, Prameha, Kasa, Kushta, Krimi, Vatarakta, Kandu, Meda, Visarpa, Aruchi,
Hikka, Arsha, Mutrakriccha, Pradara, Somroga
|
Shaligram
Nighantu, Guduchyadi Varga-251,252,253
|
|
Pitta-Kaphapaha
|
Vataja Granthi, Vataja Galganda
|
Sushrut
Samhita, Sutra 46:270, Chiki. 18: 5, 46
|
Phytochemical Characterization
A large number of chemicals are present in T. Cordifolia,
belonging to different classes such as alkaloids, diterpenoid lactones,
glycosides, steroids, sesquiterpenoid, phenolics, aliphatic compounds and
polysaccharides. Leaves of this plant are rich in protein (11.2%), calcium and
phosphorus. Four new clerodane furano diterpene glucosides (amritosides A, B, C
and D) are also found as their acetates from stems. The glycosyl component of a
polysaccharide from T. cordifolia has been isolated,
purified, methylated, hydrolyzed, reduced and acetylated. The partially
methylated alditol acetate (PMAA) derivative thus obtained has been subjected
to Gas Chromatography-Mass Spectrometry (GC-MS) studies. The following types of
linkages were found: terminal-glucose, 4-xylose, 4-glucose, 4, 6-glucose and 2,
3, 4, 6-glucose. Callus and cell suspension cultures have been established from
the stem explants of the plant. Accumulation of berberine and jatrorrhizine
(protoberberine alkaloids) was observed in both callus and cell suspension
cultures. The signaling mechanism of the novel (1, 4)-alpha-D-glucan (RR1)
isolated from T. cordifolia was investigated in macrophages
to evaluate its immune stimulating properties. An arabinogalactan has been
isolated from the dried stems and examined by methylation analysis, partial
hydrolysis and carboxyl reduction. Purified polysaccharide showed polyclonal
mitogenic activity against B-cells; their proliferation did not require
macrophages. Phytochemical characterization includes a test for one of the
phytochemical components, namely, tinosporaside (limits, 0.03% to 0.04%).
Chemical Constituents of Guruchi/Giloy
|
Types of Phytochemicals
|
Active Principles
|
Part in Which Present
|
|
Alkaloids (Tikta-Bitter Principle)
|
Berberine,
Palmatine, Tinosporine, Magnoflorine, Choline, Jatrorrhizine, 1, 2-Substituted
pyrolidine, tembeterine, Tembetarine, Tinosporin, Isocolumbin,
Tetrahydropalmatine
|
Stem & Root
|
|
Glycosides
|
18-norclerodane
glucoside, Furanoid diterpene glucoside, Tinocordiside, Tinocordifolioside,
Cordioside, Cordifolioside A, Cordifolioside B, Cordifoliside C,
Cordifoliside D, Cordifoliside E Syringin, Syringin-apiosylglycoside,
Palmatosides C, Palmatosides F
|
Stem
|
|
Diterpenoid
lactones
|
Furanolactone,
Clerodane derivatives and [(5R,10R)-4R-8R-dihydroxy-2S-3R:15,16-
diepoxy-cleroda-13 (16), 14-dieno-17,12S: 18,1S-dilactone] and Tinosporon,
Tinosporides, and Jateorine, Columbin
|
Whole Plant
|
|
Steroids
|
β -sitosterol,
δ-sitosterol, 20 β- Hydroxyecdysone, Ecdysterone, Makisterone A,
Giloinsterol.
|
Aerial part &
Stem
|
|
Sesquiterpenoid
|
Tinocordifolin.
|
Stem
|
|
Aliphatic compound
|
Octacosanol,
Heptacosanol,
|
Whole plant
|
|
Lignans
|
3 (a,
4-dihydroxy-3-methoxybenzyl)-4-(4-hydroxy-3-methoxybenzyl), (S)
|
Root
|
|
Others
|
Nonacosan-15-one, 3,(α,4-di
hydroxy-3-methoxy-benzyl)-4-(4- Compounds hydroxy-3-methoxy-benzyl)-tetrahydrofuran,
Jatrorrhizine, Tinosporidine, Cordifol, Cordifelone, N-trans-feruloyl
tyramine as diacetate, Giloin, Giloinin, Tinosporic acid.
|
Whole plant &
Root
|
Active Compound Present in Plant Part & Their
Biological Activity
The
plant exhibited multiple biological activities due to diverse chemical
constituents present in it. The biologically active chemical molecules are
present in different parts of the Guruchi.
That is the explanation for curing various ailments in human being using a
different part of the miraculous plant from the ancient ages.
|
Active Compound
|
Present in Part
|
Biological Activity
|
|
Terpenoids
|
Stem
|
Respiratory
tract infection, skin disease, Anti-hyperglycemic property.
|
|
Alkaloids
|
Stem
& Root
|
Anti-cancer
property, Antioxidant activity.
|
|
Lignans
|
Root
|
Anti-neoplastic
property, Antioxidant activity.
|
|
steroids
|
Arial
part of stem
|
Anti-stress
activity.
|
|
Other
|
Wh.
Part of Plant
|
Antidote
to snakebite and scorpion sting, Analgesic and Neuro pharmacological
activities, Diabetes, Rheumatoid arthritis, Gout, Cancer, high cholesterol
content, antipyretic, anti leprotic, radio protective
|
Phytoconstituents & Their Activity
|
Chemical compound
|
Class
|
Activity
|
|
Berberine,
choline, Tembetarine, Tinosporin, Palmitine, Jatrorrhizine
|
Alkaloids
|
Neuroprotective
effect
|
|
Berberine,
Palmatine, Tembatarine, Magnoflorine, Tinosporin, Isocolumbin
|
Alkaloids
|
Aphrodisiac
property
|
|
Cordifolioside
A, Tinocordiside, Syrigin
|
Glycosides
|
Immunomodulatory
activity
|
|
Berberine
|
Alkaloids
|
Antidyslipidemic
activity
|
|
(-)Epicatechin,
Tinosporin, Isocolumbin, Palmatine
|
Alkaloid,
Di-terpenoid lactone
|
Antioxidant
activity
|
|
Furanolactone,
Tinosporin, Tinosporide, Jateorine, Columbin, Clerodane derivatives
|
Diterpenoid
lactones
|
Anti-inflammatory
activity
|
|
Epoxyclerodane
diterpene
|
Terpenoids
|
Gastroprotective
activity
|
|
Cordifolioside
A
|
Terpenoids
|
Radioprotective
& cytoprotective activity
|
|
Tincordin,
Tinosporide, Columbin, 8-hydroxy columbin
|
Terpenoid,
Diterpenoid lactone
|
Antifeedant
activity
|
|
Tinosporin,
Isocolumbin, Palmatine, Magnoflorin, Tetrahydropalmatine
|
Alkaloids,
Terpenoids
|
Ameliorative
effect
|
|
Furanolactone,
Tinosporin, Tinosporide, Jateorine, Columbin, Clerodane derivatives
|
Alkaloids,
Terpenoids
|
Cardioprotective
effect
|
|
Magnoflorin,
Tinosporin, Isocolumbin, Palmatine, Tetrahydropalmatine
|
Alkaloids,
Terpenoids
|
Hepatoprotective
activity
|
|
Berberine, Choline,Tembetarine,Magnoflorine, Tinosporin,
Palmetine, Isocolumbin, Aporphine alkaloids,
Jatrorrhizine,Tetrahydropalmatine
|
Alkaloids
|
Antipsychotic
activity
|
|
Tinosporin,
berberine, Jatrorrhizine
|
Alkaloids
|
Anti-depressant
activity
|
|
Magnoflorine,
palmatine, Tinocordiside, Cordifolioside A
|
Alkaloids,
Terpenoids
|
Anticancer
activity
|
|
Β-
sitosterol, Makisterone A, Giloinsterol
|
Steroids
|
Antiarthritic
activity
|
|
Berberine,
choline, Tembetarine, Palamtine, Jatrorrhizine
|
Alkaloids
|
Antidiabetic
activity
|
|
Furanolactone,
Tinosporon, Jateorine, Columbin
|
Diterpenoid
lactones
|
Antimicrobial
activity
|
Pharmacological Activities of Guruchi Extracts
|
Plant Part
|
Extraction
|
Activity
|
|
Aerial
parts
|
Ethanol
extract
|
Neuroprotective
effect
|
|
Root
|
Ethanol
& aqueous extracts
|
Antiulcer
activity
|
|
Whole
plant
|
Ethanol
& aqueous extract
|
Antidiarrhoel
activity
|
|
Whole
plant
|
Ethanol
extract
|
Analgesic
activity
|
|
Whole
plant
|
Aqueous
& hydro alcoholic extract
|
Aphrodisiac
property
|
|
Whole
plant
|
Aqueous
extract
|
Immunomodulatory
activity
|
|
Whole
plant
|
Ethanol
extract
|
Antioxidant
activity
|
|
Stem
|
Aqueous
extract
|
Anti-inflammatory
activity
|
|
Whole
plant
|
Ethanol
extract
|
Nootropic
effect
|
|
Stem
|
Ethanol
extract
|
Radioprotective
& Cytoprotective activity
|
|
Whole
plant
|
Chloroform
extract
|
Antifeedant
activity
|
|
Root
|
Ethanol
extract
|
Ameliorative
effect
|
|
Whole
plant
|
Alcohol
extract
|
Cardioprotective
effect
|
|
Whole
plant
|
Aq.
extract
|
Hepatoprotective
activity
|
|
Stem
|
Aq.
extract
|
Hypoglycemic
activity
|
|
Stem
|
Aqueous
& ethanol extract
|
Antipsychotic
activity
|
|
Whole
plant
|
Pet.ether
extract
|
Antidepressant
activity
|
|
Stem
|
Ethanol
extract
|
Antiosteoporotic
activity
|
|
Aerial
parts
|
DCM
extract
|
Antineoplastic
activity
|
|
Stem
|
Methanol
extract
|
Antifertility
effect
|
|
Stem
|
Hydroalcoholic
extract
|
Antiasthamatic
activity
|
|
Stem
|
Aqueous
alcoholic extract
|
Antitumor
activity
|
|
Stem
|
Aqueous
extract
|
Diabetic
neuropathy
|
|
Aerial
parts
|
Ether
extract
|
Hepatocellular
carcinoma
|
|
Stem
|
Ethanolic
extract
|
Antimalarial
activity
|
|
Stem
|
Aqueous
& ethanolic extract
|
Antibacterial
activity
|
|
Stem
|
Aqueous
& ethanolic extract
|
Anticancer
activity
|
|
|
Formulation
guduchi ghrita
|
Antipyretic
activity
|
Immunomodulatory Activity
Active
compounds 11-hydroxymustakone, N-methyl-2-pyrrolidone, N-formylannonain,
cordifolioside A, magnoflorine, tinocordiside and syringin has potential
immunomodulatory and cytotoxic effects. Their function is boosting the
phagocytic activity of macrophages, production of reactive oxygen species (ROS)
in human neutrophil cells, enhancement in nitric oxide (NO) production by
stimulation of splenocytes and macrophages indicative of anti-tumor effects.
Aqueous Tinospora extracts
has been also found to influence the cytokine production, mitogenicity,
stimulation and activation of immune effector cells. Tinospora cordifolia extracts has effect in
up-regulation of IL-6 cytokine, resulting in acute reactions to injury,
inflammation, activation of cytotoxic T cells, and B cell differentiation.
Active compounds in aqueous extracts like alkaloids, di-terpenoid lactones,
glycosides, steroids, sesquiterpenoid, phenolics, aliphatic compounds or
polysaccharides is effective for cytotoxic action. Dry stem crude extracts
of Tinospora cordifolia with
a polyclonal B cell mitogen, G1-4A on binding to macrophages have been found to
enhance immune response in animal by inducing secretion of IL-1, together with
activation of macrophages. In various clinical researches Tinospora cordifolia in
prevention of oxidative damage also exist. The (1,4)-alpha-d-glucan
(alpha-d-glucan), derived Tinospora
cordifolia has shown to activate human lymphocytes with
downstream synthesis of the pro- and anti-inflammatory cytokines, in vitro. Synergistic effects of
compounds in the immunomodulatory activity of Tinospora cordifolia are found.
In Ayurveda T. Cordifolia is believed
to have rasayana (rejuvenating), balya (tonic), vayahsthapana (anti-aging), aayushyaprada (increases
the lifespan), vrishya (aphrodisiac) and chakshusya (useful
in eye disorders) properties. The alcoholic and aqueous extracts of T.
cordifolia are reported to have beneficial effects on the immune
system and have been tested successfully for their immunomodulatory activity.
The degradation of proteins due to photosensitization as assessed by Sodium
dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) was effectively
reduced by simultaneous treatment with G1-4A/PPI (partially purified
immunomodulator) from T. cordifolia during
photosensitization. The novel (1, 4)-alpha-D-glucan derived from the plant
activates the immune system through the activation of macrophages via TLR6
signaling, NFkappaB translocation and cytokine production. Tinospora
cordifolia differentially regulate elevation of cytokines as
evidenced by the increased production of antiangiogenic agents IL-2 and tissue
inhibitor of metalloprotease-1 (TIMP-1) in the B16F10-injected, extract-treated
animals. The observed antiangiogenic activity of the plant T.
cordifolia is related to the regulation of the levels of cytokines
and growth factors in the blood. The aqueous extract of T. cordifolia was
found to enhance phagocytosis in vitro. The aqueous and ethanolic extracts also induced an increase in
antibody production in vivo.
T. cordifolia extract (TCE) treatment caused significant
reduction in eosinophil count and improved hemoglobin in HIV patients. Diabetic
patients with foot ulcers on T. cordifolia as an adjuvant
therapy showed significantly better final outcome with improvement in wound
healing. It also stimulates proliferation in splenocytes in a dose-dependent
manner.
Kapil et al. studied
the syringin (TC-4) and cordiol (TC-7) isolate from T. cordifolia inhibited
the in-vitro immune hemolysis of antibody-coated sheep
erythrocytes by guinea pig serum. Immune hemolysis was reduced due to
inhibition of the C3-convertase of the classical complement pathway. The
compounds of T. cordifolia rise to significant
increases in IgG antibodies in guinea pig serum. Cordioside (TC-2),
cordiofolioside A (TC-5) and cordiol (TC-7) activated macrophase with
increasing incubation times. Sharma et al., isolated and characterised
different classes of active compounds found their immunomodulatory activity.
Anti-Oxidant
Activity
The anti-oxidant capacity of Tinospora
cordifolia stem methanol extracts administered orally increased the
erythrocytes membrane lipid peroxide and catalase activity. Guruchi Willd.(Menispermaceae)
extracts possess possible inhibitors of aldose reductase and anti-oxidant
agents thereby reducing chemotoxicity induced by free radicals.
TCE has been reported of its strong free radical scavenging
properties against superoxide anion (O2-), hydroxyl
radicals (OH), NO radical, and peroxynitrite anion (ONOO-). Tinospora
cordifolia lowers the levels of malondialdehyde and ROS and the
higher levels of GSH and total thiols. The protective effects of Tinospora
cordifolia could be observed even in the fetal milieu, with higher
levels of anti-oxidant molecules and enzymes.
Tinospora cordifolia has the ability to
scavenge free radicals generated during aflatoxicosis. It shows
protection against aflatoxin-induced nephrotoxicity due to the presence of
alkaloids such as a choline, tinosporin, isocolumbin, palmatine,
tetrahydropalmatine, and magnoflorine.
Mehra et al.,
prepared the formulation and evaluated its antioxidant activity by DPPH
(1-diphenyl-2-picrylhydrazyl) free radical scavenging method. They estimated
the total flavonol and total phenolic content. Using the result of the
formulation showed potent antioxidant activity and inhibitory concentration (IC50)
at 5 μg/ml as compared to standard drug ascorbic acid .
George et al., reported
the methanolic, ethanolic, and water extracts of T. cordifolia for
their antioxidant activity, in which the stemic ethanol extract increased the
erythrocytes membrane lipid peroxide, catalase activity and decrease the
superoxide dismutase, glutathione peroxidase in alloxan-induced diabetic rats.
The leaves extract of methanol, partitioned in water with ethyl acetate and
butanol at 250 mg/ml, and showed their antioxidant activity; extracts of
methanol phosphomolybdenum and metal chelating activity were high followed by
ethyl acetate, butanol, and water extract. It also decrease level of free
radical species of diabetic rat and up-regulate the anti-oxidant enzyme,
scavenging activity for free radical of methanol extract was high compared with
phenol extract. This plant modifies the different
enzymatic system which controls the production of these reactive species and
maintains the oxidative load by regulating the lipid peroxidation process and
glutathione level.
Premnath et al., dried
the leave of T. cordifolia and powdered and extracted
with chloroform, methanol, ethanol hexane, and water. Antioxidant assay by
different in-vitro models, lipid peroxidation inhibitory
activity, DPPH radical scavenged, and superoxide radical scavenging activity.
Other solvent extracts showed weak antioxidant activity, whereas ethanol
extract had high antioxidant activity. The results suggested that the antioxidant
compound are better in ethanol extract, and there is a direct correlation
between the total polyphenols extracted and its anti-oxidant activity.
T. cordifolia is mentioned as vishaghni,
vishahara and tridoshashamaka in various texts of Ayurveda. A
significant increase in the concentration of thiobarbituric acid-reactive
substances (TBARS) in brain, along with its decrease in heart, was observed in
diabetic rats. Tinospora cordifolia treatment decreased the
concentrations of glutathione reductase (GSH) and decreased activities of
superoxide dismutase (SOD), catalase and glutathione peroxidase (GPx) in the
tissues of body. The herb also exhibited strong free radical-scavenging
properties against reactive oxygen and nitrogen species as studied by electron
paramagnetic resonance spectroscopy. Aqueous extract of T. cordifolia inhibited
Fenton (FeSO4) reaction and radiation - mediated 2-deoxyribose degradation in a
dose-dependent fashion, with an IC50 value of 700 µ/ml for both fenton and
radiation-mediated 2-DR degradation. Similarly, it showed a moderate but
dose-dependent inhibition of chemically generated superoxide anion at 500 µ/mL
concentration and above, with an IC50 value of 2000 µ/mL. In various
studies, T. cordifolia was found effective in iron-mediated
lipid damage and gamma-ray-induced protein damage, amelioration of
cyclophosphamide-induced toxicity, alteration of lethal effects of gamma rays,
induction of enzymes of carcinogen/drug metabolism and inhibition of lipid
peroxidation, free radical generation and lipid peroxidation during
oxygen-glucose deprivation, and nitric oxide scavenging effects. The extract
of T. cordifolia has demonstrated antioxidant action in the
alloxan induced diabetes model as well.
Anti-Diabetic Activity
The stem of Tinospora cordifolia is
widely used in the therapy of diabetes by regulating the blood glucose in
traditional folk medicine of India. It has been reported to mediate its
anti-diabetic potential through mitigating oxidative stress (OS), promoting
insulin secretion and also by inhibiting gluconeogenesis and glycogenolysis,
thereby regulating blood glucose. Alkaloids, tannins, cardiac glycosides,
flavonoids, saponins, and steroids as the major phytoconstituents of Tinospora
cordifolia have been reported to play an anti-diabetic role.
The isoquinoline alkaloid rich fraction from stem, including,
palmatine, jatrorrhizine, and magnoflorine have been reported for
insulin-mimicking and insulin-releasing effect both in vitro and in
vivo. Oral treatments of root extracts have been reported to regulate
blood glucose levels, enhance insulin secretion and suppress OS markers.
Initiation and restoration of cellular defence anti-oxidant markers including
superoxide dismutase (SOD), glutathione peroxidase (GPx) and glutathione (GSH),
inhibition of glucose 6-phosphatase and fructose 1, 6-diphosphatase,
restoration of glycogen content in liver was reported in in vitro studies.
The crude stem ethyl acetate, dichloromethane (DCM), chloroforms and hexane
extracts of Tinospora cordifolia inhibited the enzyme's
salivary and pancreatic amylase and glucosidase thus increasing the
post-prandial glucose level and finds potential application in treatment of
diabetes mellitus.
The protective effects of TCE were reported in presence
of higher levels of anti-oxidant molecules and enzymes. TCE has been shown to
significantly counterbalance the diabetes-associated OS in the maternal liver
by lowering the levels of malondialdehyde and ROS and the increased levels of
GSH and total thiols.
The anti-diabetic activities are due to
alkaloids (Magnoflorine, Palmetine, Jatrorrhizine), tannins, cardiac
glycosides, flavonoids, saponins, etc. The crude extract of the stem in ethyl
acetate, dichloromethane (CDM), chloroform and hexane was studied for
inhibition of the alpha-glucosidase enzyme. The activity of the enzyme
inhibited hypoglysomic action in diabetic animal and normal animals. The
aqueous extract was studied in the rats, without the addition of Tinospora
cordifolia extract increase in glucose by 21.3%, insulin by 51.5%,
triglycerides by 54.12%, and glucose-insulin index by 59.8 when plant
containing extract was given. The fructose-induced abnormalities in the liver
involving lipid peroxidation, protein carbonyl groups, GSH levels, and
enzymatic antioxidants decreased. From Guduchi Prasant et al.,
isolated alkaloids, cardiac glycosides, saponins, flavonoids, tannins, and
steroids that contains anti-diabetic property. Alkaloids from that plant showed
insulin-mediated actions due to insulin hormone. Gestational diabetes can increase the GSH
content and other reactive species that can act as a threat to the mother as
well as the fetus. The study based upon the pregnant rat using T. cordifolia was incorporated in the daily diet
to a diabetic-pregnant rat (streptozocin-induced diabetes), which showed a
protective effect by reducing the oxidative load thereby preventing the
relative incidence of diseases and any birth defect.
The root extract of Guduchi showed an
antihyperglycemic effect in the alloxan-induced diabetic model by decreasing
its excess glucose level in urine as well as in normal. Hyponidd is reported,
and it maintained the oxidative load by decreasing reactive species and reduced
the glucose-mediated hemoglobin count. when the tested of ‘Dihar’ for one and a
half month in streptozotocin-induced diabetic model decreased the urea as well
as creatinine amount in the blood with an increase in enzyme activities.
Anti Microbial Activity
The methanol extracts of Tinospora cordifolia has
been found to have potential against microbial infections. The anti-bacterial
activity of Tinospora cordifolia extracts has been assayed
against Escherichia coli, Staphylococcus aureus, Klebsiella
pneumoniae, Proteus vulgaris, Salmonella typhi, Shigella flexneri, Salmonella
paratyphi, Salmonella typhimurium, Pseudomonas aeruginosa, Enterobacter
aerogene, and Serratia
marcesenses (Gram-positive bacteria). In animal trial, TCE has been
reported to function in bacterial clearance and improved phagocytic and
intracellular bactericidal capacities of neutrophils. TCE has been reported of
immunostimulant properties on macrophages. Intra-mammary infusion of
hydro-methanolic extracts of Tinospora cordifolia treatment
showed enhanced phagocytic activity of polymorphonuclear cells in bovine
subclinical mastitis.
T. cordifolia with
different solvents on different micro-organism shows good antifungal and
antibacterial activity. The aqueous, ethanol and acetone extract of T. cordifolia inhibited
the activity on clinical isolates of urinary pathogens Klebsiella
pneumoniae and Pseudomonas aeruginosa. Singh et al., has
reported silver nanoparticles from the stem of T. cordifolia, which
possess antibacterial activity against the different strains of bacterias.
Allemailem et al., have reported the antifungal activity
of T. cordifolia, which was determined using the agar
well plate diffusion method. Agarwal et al., studied in-vitro extract
of T. cordifolia was obtained using 100% ethanol by
maceration process. They prepared ethylic extract seven different
concentrations and tested against S. mutans in
brain–heart infusion agar medium. Plates were incubated aerobically at 37 °C
for 48 h, using Vernier caliper and measured the zone of inhibition. 0.2%
chlorhexidine and dimethylformamide were used as positive and negative
controls, respectively. This experiment data were analysed by
descriptive-analytic tests. Which shows the maximum antibacterial activity
of T. cordifolia a volume of 40 μl at 2% concentration
with a zone of inhibition of 19 mm. A 30 μl volume of 0.2% chlorohexidine shows
a zone of inhibition of 28 mm, and dimethylformamide shows no zone of
inhibition. Khan et al.,
reported the antifungal activity TCAE (Tinospora cordifolia aqueous
extract) was tested for in-vitro against the isolates of
different Aspergillum species.
Anti-Osteoporotic
Activity
Abiramasundari et al., reported T. cordifolia affect
the proliferation, differentiation, and mineralization of bone-like matrix on
osteoblast model systems in-vitro and hence finds potential
application as an anti-osteoporotic agent. Alcoholic extract of T. cordifolia has
been shown to stimulate the growth of osteoblasts, increasing the
differentiation of cells into the osteoblastic lineage and also increasing the
mineralization of bone-like matrix. Ecdysteroids isolated from
the plant have been reported of protein anabolic and anti-osteoporotic effects
in mammals. Beta-Ecdysone (Ecd) from T. cordifolia extracts
have been reported to induce a significant increase in the thickness of joint
cartilage, induce the osteogenic differentiation in mouse mesenchymal stem
cells and to
relieve osteoporosis in osteoporotic animal models. Further 20-OH-β-Ecd isolated from T. cordifolia has
been found for its anti-osteoporotic effects, thus highlighting the role
of guruchi in the treatment of osteoporosis and
osteoarthritis.
Anti
Stress Activity
Sarma et al., reported ethanolic extract of T. cordifolia at
the dose of 100 mg/kg gives significant anti-stress activity in all parameters
compared with standard drug diazepam (dose of 2.5 mg). The plant extract gives
a moderate degree of behavior disorders and mental deficit response. The
clinical research showed the improved I. Q level of patients. In Ayurveda, it
acts as Medhya Rasayana or brain tonic by increasing mind power like memory and
recollection.
Effect
on Hepatic disorder
Protective Effects of Tinospora cordifolia water
extract (TCE) on Hepatic and Gastrointestinal Toxicity was found by
Sharma et al., a significant increase in the levels of
gamma-glutamyl transferase, aspartate transaminase, alanine transaminase,
Triglyceride, Cholesterol, HDL and LDL (P < 0.05) in alcoholic sample
whereas their level get downregulated after TCE intervention, patients showed
the normalized liver function of T. cordifolia stand to
relieve the symptoms.
Effect on Wound healing
Shanbhag
T et al., The
present study was aimed at evaluating the wound healing profile of alcoholic
extract of T. cordifolia and its effect on
dexamethasone suppressed healing. Incision, excision, and dead space of the
wound models were employed to investigate the wound healing potential of the
plant increased tensile strength extract of T. cordifolia may
be attributed to the promotion of collagen synthesis. The extract of T. cordifolia did
not reverse dexamethasone suppressed wound healing.
Anti-HIV Activity
Giloy has been shown
to demonstrate a decrease in the recurrent resistance of HIV virus thus
improving the therapeutic outcome. Anti-HIV effects of TCE was revealed by
reduction in eosinophil count, stimulation of B lymphocytes, macrophages and
polymorphonuclear leucocytes and hemoglobin percentage thus, revealing its
promising role of application in management of the disease.
Kalikae et al., showed that the root extract of T. cordifolia affects
the immune system of HIV positive patient. The stem extract of Tinospora
cordifolia reduces the ability of eosinophil count, stimulation of B
lymphocytes, macrophages, level of hemoglobin, and polymorphonuclear
leucocytes.
Anti-Toxic Effects
It exhibited
protective effects by lowering thiobarbituric acid reactive substances (TBARS)
levels and enhancing the GSH, ascorbic acid, protein, and the activities of
anti-oxidant enzymes viz., SOD, CAT, GPx, Glutathione S-transferase (GST) and
glutathione reductase (GR) in kidney. Alkaloids such as a choline, tinosporin,
isocolumbin, palmatine, tetrahydropalmatine, and magnoflorine from Tinospora
cordifolia showed protection against aflatoxin-induced
nephrotoxicity. Oral administration of plant extracts prevented the occurrence
of lead nitrate induced liver damage. Synergistic administration of aqueous
extract of stem and leaf along with the lead nitrate increased the activities
of SOD and CAT and decreased the levels of AST, ALT, ALP, and ACP enzymes.
Protective role of aqueous extract of stem and leaves of Tinospora
cordifolia overcoming the toxic effects of lead is shows as its
effects on the hematological values. Cyclophosphamide, an anti-cancer drug
reduce the GSH content in both bladder and liver and lowered levels of cytokines
Inerferon-γ and IL-2 an increased levels of pro-inflammatory cytokine TNF-α.
This effect could be reversed on Tinospora cordifolia treatment
indicating the role of Tinospora cordifolia in overcoming
cyclophosphamide induced toxicities in cancer treatment.
Anti
Cancer Activity
The anti-cancer
effects of Tinospora cordifolia are mostly studied in animal models. TCE have been shown to
have a radioprotective role by significantly increase in body weight, tissue
weight, testes-body weight ratio and tubular diameter and inhibit the harmful
effects of sub-lethal gamma radiation on testes in male Swiss albino mice. In
pre-irradiating mice, TCE significantly affected radiation induced rise in
lipid peroxidation and resulted in the decline of GSH concentration in testes.
Pre-treatment of HeLa cells by TCE have been shown to decrease the cell
viability, increase LDH and decrease in GSH S-transferase activity. Dihydrotestosterone
in TCE has been shown to stimulate the growth and proliferation of Human LNCaP
cells (which are androgen-sensitive human prostate adenocarcinoma cells).
Androgenic compounds in TCE act via androgen receptor. Newly isolated compounds
like (5R, 10R)-4R, 8R-dihydroxy-2S, 3R: 15, 16-diepoxycleroda-13 (16), 17, 12S:
18,1S-dilactone (ECD), a diterpenoid from Tinospora cordifolia has
been found for its chemopreventive potential in diethylnitrosamine (DEN)
induced hepatocellular carcinoma (HCC) by decreasing anti-oxidant activities
and detoxification enzymes like GSH, GPx and subsequent increase in the
activities of the hepatic markers ((Serum glutamic oxaloacetic
transaminase)SGOT, (Serum Glutamic Pyruvate Transaminase) SGPT, LDH) and
decreased serum transaminase level thus confirming its anti-tumor effects and
promising application as a potent chemo preventive drug for HCC.
The radiosensitizing
activity of DCM extract of Tinospora cordifolia has been
found in Ehrlich ascites carcinoma (EAC) mice enabling tumor-free survival via
depletion of GSH and glutathione-S-transferase by elevated levels of lipid
peroxidation and DNA damage to tumor cells. TCE hexane fraction has been shown
to block the G1 phase in EAC mice and cause apoptosis by the formation of apoptotic
bodies, nuclear condensation, activation of caspase-3, decreased cell number
and ascites volume, increased expression of pro-apoptotic gene, Bax,
and decreased expression of anti-apoptotic gene. TCE could induce a reduction
of papillomas, tumor yield, tumor burden, and tumor weight while increase phase
II detoxifying enzymes in skin carcinoma animal models. The effect of a
hydroalcoholic (80% ethanol: 20% distilled water) extract of aerial roots
of guruchi on animal trial revealed a significant increase
in acid-soluble sulfhydryl (-SH), cytochrome P (450)
contents, and enzyme activities of cytochrome P (450) reductase, cytochrome b5
reductase, GST, DT-diaphorase (DTD), SOD, catalase, GPX, and GR activity in the
liver highlighting the chemopreventive role of guruchi against
carcinogenicity.
In vivo anti-angiogenic
activity of TCE in B16-F10 melanoma was detected by increased levels of
pro-inflammatory cytokines, including IL-1 β, IL-6, TNF-α, granulocyte
monocyte-colony stimulating factor (GM-CSF) and the vascular endothelial cell
growth factor (VEGF), increased production of anti-angiogenic agents IL-2 and
tissue inhibitor of metalloprotease-1 (TIMP-1) in the B16-F10 extract-treated
animals. The polysaccharide fraction from guruchi was found
to be very effective in reducing the metastatic potential of B16-F10 melanoma
cells. Markers of neoplastic development were reduced significantly in the
treated animals compared with the untreated control animals.
Most of the synthetic
chemotherapeutic agents suffer from toxic side effects. The effect of Guduchi
extracts was comparable or better than doxorubicin treatment.
Other
Effect
A dose dependent reduction in infarct size and in lipid
peroxide levels of serum and heart tissue were observed with the prior treatment
of Tinospora cordifolia.
The activation of macrophages by cytotoxic T cells leads to increase in GM-CSF
which leads to leucocytosis and improved neutrophil function. Octacosanol
isolated from Tinospora cordifolia inhibits proliferation of
endothelial cells and Ehrlich ascites tumor cells, inhibits neovascularization
induced by angiogenic factors in chick chorioallantoic membrane and
cornea in vivo angiogenesis assays and also inhibits
secretion of ascites fluid in the growing tumor cells in vivo by
inhibiting activity of matrix metalloproteinases (MMPs) and translocation of
transcription factor nuclear factor-kappa-B (NF-κB) to nucleus. The in
vivo administration of alcoholic extract of Tinospora
cordifolia has been found to increase bone marrow derived macrophages
in bearing Dalton's lymphoma. The polyherbal preparations Caps HT2 of Tinospora
cordifolia, could reduce plasma recalcification time and enhanced the
release of lipoprotein lipase enzyme. Other polyherbal HP-1 has hepatocurative
and anti-oxidant efects.
A plant with as diverse a role as Tinospora cordifolia is a versatile resource for all forms of life. There are reports as already discussed that the plant extracts have active compounds in the form of alkaloids, glycosides, lactones and steroids. All these active compounds have immunomodulatory and physiological roles of different types, thereby demonstrating the diverse versatility of the plant. Studies need to be conducted with aspects how the active compounds actually interact with the living systems and affects the structure-function relationships. Crystal structures of the membrane bound receptors and the activation of the downstream signaling cascades and the changes in the immediate environment of the site of action can lead us into identification of novel perspectives into our understanding of nature. The search into the vivacious sources of nature can also lead us into differential interactions among the evolutionarily related groups of organisms. The future scope of the review remains in exploiting the biochemical and signaling pathways of the active components of Tinospora thus, enabling effective disease targeting. With so much to offer to the scientific world of medicine, the plant Giloy truly acts as an incredible source.
Tinospora cordifolia has an importance in traditional ayurvedic medicine used for ages in the treatment of fever, jaundice, chronic diarrhea, cancer, dysentery, bone fracture, pain, asthma, skin disease, poisonous insect, snake bite, eye disorders. Recent reports have shown the compounds and their biological roles in Tinospora cordifolia extract. Such properties may be exploited for production of new formulations, which may be better and promising over conventional one. Although genetically diverse and reports of application of tissue culture based propagation of Tinospora exist, effective conservation strategies of the germplasm for such an economically important medicinal plant with many biological role remains yet to be accomplished.
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