Daaru-Haridraa (Berberis aristata)
Daaru-Haridraa (Berberis aristata)
Introduction
Daaru-Haridraa
AKA Barberry in the West is a common garden bush. Daaru- Haridra (Berberis aristata) occupied an important place in Ayurveda. In Ayurveda its
pleiotropic properties were harnessed to treat a variety of ailments. In the
Middle East, Barberry (Berberis aristata)
attained the status of “medicine” in ancient times, since Egyptian pharaohs and
queens used Barberry with fennel seeds to prevent and ward off the plague. In
Egypt, it is still in vogue for fevers associated with pestilence. In the
medieval times, it was recommended for liver and gallbladder disorders. For
many years, in Europe and America, it has been used for the treatment of fever,
disorders of the stomach, loss of appetite, diarrhea and to improve ‘energy’
and well being. In Russia, it has been used for inflammations and high arterial
tension. In Italy, it is known as “Holy Thorn”. The Italians believe that the
plant is wrapped in Christ’s thorns he wore around his skull. Early physicians
thought that the yellow wood of Barberry could allay jaundice. This belief was
based on the philosophy of the doctrine of signatures. Native American
Indians used Daaru-Haridraa in cases of general debility and as an appetizer.
The colonists used the root of the herb as bitter tonic. In traditional folk
medicine, Barberry is used to improve appetite, to treat fever, diarrhea and to
increase vitality. [1]. [2]
The
philosophy of the “Doctrine of
Signatures”, dating from the time of Dioscurides
and Galen, states that, herbs that resemble various parts of the body can be
used to treat ailments of that part of the body. A theological justification
offered by botanists like William Coles for this philosophy, was that God would
have wanted to show men what plants would be useful for treating ailments of
various parts of the body. “It was reasoned that the Almighty must have set his
sign upon the various means of curing disease which he provided.” Since the
wood of the tree Daaru-Haridraa AKA Barberry (Berberis aristata) is yellow in color, early physicians used it to
treat jaundice. (Daaru stands for wood and Haridraa for yellow color resembling
the color of Haridraa i. e. Turmeric)
There
is no scientific evidence to prove the “Doctrine
of Signatures”. Scientists therefore see the doctrine as a superstition.
[3]
Other Names
Latin/Botanical/Scientific: Berberis aristata
Sanskrit: Daaru-Haridraa,
Daaru-Peetaa, (Peetaa-Daaru?), Darvi,
English: Indian
Berberry
Bengali: Daaruharidraa
Gujarati: Daaru-Haldar.
Hindi: Daaru-Haldee, Kashmal, (According
to indiabiodivesrsity.org) Chitra
Kannada: Daaruhaldi, Maradarishana, Maradarishina
Kashmiri : Rassashud
Malayalam : Maramanjal, Maramannal
Marathi: Daaru-Halad, Raswat
Oriya: Daaruhalidi, Daaruharidraa
Punjabi: Sumalu
Tamil: Gangeti,
Varatiu manjal
Telugu:
Manupasupu
Urdu: Darhald
Taxonomic Classification
Kingdom: Plantae
Unranked: Angiosperm (According to indiabiodivesrsity.org) Phylum: Tracheophyta)
Unranked: Eudicots
Division: Magnoliophyta
Class: Magnoliopsida
Order: Ranunculales
Family: Berberidaceae
Genus : (According to
indiabiodivesrsity.org : Berberis)
Species :
(According
to indiabiodivesrsity.org : Berberis
aristata)
Berberis aristata also known as Indian Barberry or Tree Turmeric
belongs to the genus Berberis. The genus comprises of approximately
450-500 species of deciduous evergreen shrubs found in the temperate climate. [6]
Geographical distribution
Berberis aristata is native to the Himalayas and Nepal. The herb also
grows in Nilgiri range in Southern India. The shrub is found in the temperate
and sub-tropical regions of Asia, Europe and America. Mostly it is found in
Nepal and wet zone of Sri Lanka, grown in Nilgiris and all over temperate
Himalayas. It is also said to be native to Europe. It is now naturalized and
cultivated in North America. Now it is a common garden bush. It grows in the
form of a deciduous shrub in almost any garden in Britain and Europe. It also
grows in hard gravelly soils of northern US regions and in the rich soils of
the Western states. It blossoms in mid-spring, to the beginning of summer. [7]
Plant Morphology
Plant Root
Stem Leaves
Flowers Fruits
Seeds
Images of Daaruharidra (Berberis aristata)
Macroscopic
Characteristics
Daaruharidra is a large, deciduous,
erect spiny shrub, growing in thick horny clumps reaching between 3 and 8 feet
in height. The roots and stems are burgeoning (flourishing) with the potent
alkaloid berberine, making its stems appear to be ‘Turmeric-colored’. [11]
Root is cylindrical, yellow in color, thick, woody, covered with a thin
brittle bark; more or less knotty, much
branched, externally light yellowish brown, longitudinally wrinkled and scaly,
fracture (rupture of cells or tissues) hard and tough
Stem is red when the plant is
young, getting darker as the plant grows older. It is from 3 to 8 feet in
height. The twigs are whitish to pale yellowish brown in color; available in pieces of variable length and
thickness
Bark is about 0.4 to 0.8 cm thick woody,
soft pale yellow to brown outside and deep yellow inside. It is covered with
three branched thorns which are modified leaves, and can be peeled by hand in
longitudinal strips.
Leaves are arranged in tufts of 5 to 8, obovate,
approximately 5 cm long and 2 cm broad, simple, deep green in color on the
dorsal and light green on the ventral surface, leathery in texture, toothed,
with several indentations along the margin.
Flowers are stalked, complete, hermaphrodite and yellow in
color. They form a simple corymbose or racemose inflorescence with 11 to 16
flowers per raceme. They are arranged along a central stem. The Calyx yellow in
color having 3 large and 3 small sepals which are yellow in color,
actinomorphic (i. e. characterized by radial symmetry, such as a starfish or
the flower of a daisy), caduceus (the staff carried by Hermes in Greek
mythology) or caducous (an organ or part easily detached and shed at an early
stage), 4 to 5 mm long. The Corolla is polypetalous with 6 petals, yellow 4 to
5 mm long. The Androecium (the male reproductive structure) is polyandrous,
adnate (attached squarely and firmly to the stem), contains 6 stamens and are 6
mm long. The Gynecium (the female reproductive structure) is one, 4 to 5 mm
long with a short style and a broad stigma.
The
plant flowers between March and April.
Fruits are edible berries, succulent, bright red in color,
ovoid, smooth, acidic when raw, rich in vitamin C, have medicinal properties.
The berries are 7 mm long and 4 mm in diameter, weighing about 227 mg and 237 ml
in volume, aconite violet in color. They start ripening from the second week of
May and continue to do so throughout June.
Seeds two to five in number, varying in color from
yellow to pink, each weighing about 25 mg and about 29 ml in volume. [12],
[13], [14], [15], [16], [17]
Microscopic Characteristics
Stem- Shows rhytidoma (outer bark) with cork
consisting of 3-45 rectangular, yellow colored, thin-walled cells, arranged
radially. The sieve elements are irregular in shape, thin-walled, a few cells
containing yellowish-brown contents. The phloem fibers are arranged in tangential rows,
consisting of 1-4 cells, each fiber short thick-walled, spindle-shaped,
lignified having wide lumen; half inner portion of rhytidoma traversed by
secondary phloem rays that run obliquely consisting of radially elongated
parenchymatous cells having single prismatic crystals of calcium oxalate, a few
cells of rhytidoma also contain prismatic crystals of calcium oxalate. The stone
cells are also found scattered in phloem ray cells in groups, rarely single,
mostly elongated, a few rounded, arranged radially, some of which contain a
single prism of calcium oxalate crystals. The secondary phloem is a broad zone,
consisting of sieve elements and phloem fibers, traversed by multi seriate
phloem rays. The sieve elements are arranged as tangential
bands and tangentially compressed cells alternating with single to five rows of
phloem fibers. The phloem fibers short, lignified, thick-walled having pointed
ends. The secondary xylem are broad consisting of xylem vessels, tracheids,
xylem fibers and traversed by multi seriate xylem rays. The xylem vessels are
numerous, small to medium sized, distributed throughout xylem region in singles
or in groups. The groups of vessels are usually arranged radially. The isolated
vessels are cylindrical with rounded or projected at one or both ends with
spiral thickening. The xylem fibers numerous, lignified, large, thick-walled
with wide lumen and pointed tips. The xylem rays are quite distinct, straight,
multi seriate, consisting of radially arranged rectangular cells, each ray
30-53 cells high, 8-12 cells wide. Few ray cells contain brown contents.
Powder- Yellow in color shows mostly fragments of
cork cells, sieve elements, yellow colored phloem fibers which are entire or in
pieces. The stone cells are in singles or in groups. There are numerous
prismatic crystals of calcium oxalate. The xylem vessels have spiral thickening.
They are thick-walled, lignified xylem fibers and ray cells. [18], [19]
When observed under microscope using chloral hydrate
solution the powder shows following diagnostic characters—
Abundant thin-walled parenchyma, fragments of yellowish-brown
cork, spherical or ovoid orange-brown granular masses
When examined under microscope using 50% v/v
solution of glycerol, the powder shows simple, small and spherical to ovoid
starch granules. [20]
Parts Used
Bark,
root, stem, seed and fruit.
Rasaut/
Rasaanjana: Root bark and lower stem
are boiled with water, strained and condensed till a semi solid mass is
obtained which is known as Rasaut. The extract called Rasaanjana is also used
for medicinal purpose.
Phytochemistry
The
main active ingredients of this plant are isoquinoline alkaloids. They are
found in the root, bark, stem, and berries. They are:
Alkaloids:
Berberine,
oxyberberine, berbamine, epiberberine, oxyberberine, berberrubine, beraromoline,
protoberberine (Karachine), dihydrokakarachine,
taximaline, palmatine, jatrorrhizine, oxycanthine, bervulcine,
columbamine, isotetrandine and vulcracine, dehydrocaroline, pakistanine, 1-O
methyl pakistanine, pseudo palmatine chloride and pseudoberberinr chloride.
Pharmacological
actions of almost all chemical constituents of B. aristata are same as
those of berberine. Hence pharmacology of berberine is discussed in detail.
Other ingredients:
Carbohydrates,
organic acids like chelidonic acid, citric acid and malic acid, resin, tannin,
pectin, polyphenolic compounds, some vitamins and mineral elements [21], [22]
Identity,
Purity and Strength
(1)
Foreign
matter: Not more than 2
percent
Total
ash: Not more than 14 percent
Acid-insoluble
ash: Not more than 5 percent
Alcohol-soluble
extractive: Not less than 6 percent
Water-soluble extractive: Not less than 8 percent [23]
(2) Standards accepted by
I. P. in 2010
Foreign organic matter: Not
more than 2.0 percent
Ethanol-soluble extractive:
Not
less than 2.0 percent
Water-soluble extractive: Not less
than 6.0 percent
Total ash: Not
more than 5.0 percent
Acid-insoluble ash: Not
more than 1.0 percent
Heavy metals: 1.0g complies with the limit test for heavy metals
Loss on drying: Not more
than 12.0 percent determined on 5.0 g by drying in oven at 1050
(scale not mentioned)
Microbial contamination: Complies with the microbial contamination tests.
Assay: Standardized as determined by liquid chromatography.
Daaruharidraa Roots contain Not less than 0.70 percent of
berberine, and Stems Not less than 0.5 percent of berberine, calculated
on the dried basis.
Storage: Should be protected from heat, moisture, attack of
insects and rodents. [24]
Cytological
Identity
The
number of chromosomes in Daaruharidraa (Berberis aristata DC) is 6 [25]
Genetic study
With the help of molecular techniques like Random
Amplified Polymorphic DNA (RAPD), Amplified Fragment Length Polymorphic DNA
(AFLP), Restricted Length Polymorphic DNA (RFLP) and Inter Simple Sequence
Repeat (ISSR) etc, the identification of plant species has now become very
accurate. [26]
Safety Tests
No
safety data for each specific species of herb is available. Here are general
guidelines:
Heavy Metals:
Arsenic: Not more than 5.0 mg/kg
Mercury: Not
more than 0.5mg/kg
Lead: Not
more than 10.0 mg/kg
Chromium: Not
more than 0.3 mg/kg
Microbial Limits:
Total
bacterial count: Not more than 105cfu/g
Total
yeast and mould count: Not more than 104cfu/g
Bile
tolerant gram negative bacteria: Not more than 104cfu/g
Specific
Pathogens:
Salmonella spp:
Absent in 25 g
Escherichia
coli: Absent in 1g
Staphylococcus
aureus: Absent in 1g
Pseudomonas
aeruginosa: Absent in 1g [27]
Properties
and Pharmacology
Ayurvedic properties
Ganas
(Classical Categories)
The herb belongs to the following ganas (classical groups)
Charaka Ganas: Arshoghna (Cures Hemorrhoids), Kandughna (Anti
pruritic, Respites itching), Lekhaniya (Reduces weight, Reduces fat, Relieves
obesity)
Energetics
Rasa
of the Fruit: Madhura (Sweet), Amla (Sour).
Weerya (Energy State): Ushna (Hot)
Gunas (Qualities):
Laghu (Light), Rooksha (Dry)
Effects
on Doshas: Pitta,
Kapha
Actions
on Dhatus: (Tissues): Meda
(Adipose Tissue), Rasa (Lymph) and Rakta (Blood)
Effects
on Srotas (Systems): Annawaha (GI System), Rasawaha (Lymphatic System)
Ayurvedic
Actions
Deepana:
Appetizer
Jwaraghna:
Antipyretic
Kaphaghna:
Allays
catarrh
Katupaushtic: Acrid, spicy, pungent tonic
Netrya: Beneficial for the eyes
Paachana:
Digestive
(Digestant)
Pitta
saaraka: Increases the flow of bile
Rochana:
Improves
taste
Shothahara:
Reduces swelling reduces edema
Swedajanak:
Diaphoretic
(Promotes sweating)
Trishna
nigrhana: Reduces thirst, controls
thirst, quenches thirst
Yakruduttejaka:
Stimulates the functions of the liver
Warnya:
Improves
the complexion
Wedanaasthaapana: Anti-nociceptive (Analgesic)
Wrana
shodhana: Wound cleanser, vulnerary
Wrana
ropana: a wound healer [28]
It
is anti-inflammatory (shothaghna) and analgesic on topical application,
vulnerary (heals wounds), antipruritic, liver stimulant, appetizer,
antidiarrheal, laxative, antitussive (kaasaghna), anti-asthmatic, styptic
(stops bleeding), raktashodhana (blood purifier), rasaayana (rejuvenating and
adaptogenic).
As
its properties resemble to those of Haridraa (C. longa), Maharshi Charaka the noted Ayurvedic physician describes
them together as Haridraa-dwaya (the duo of Haridraa). He makes a special
mention about Daaru-Haridraa (B. aristata)
as ‘stanya shodhana’ (one which purifies breast milk), lekhana (emaciating), arshoghna
(antihemorrhoidal), kaamalaahara (allays, relieves jaundice), kandughna
(anti-pruritic, allays itching), swedala (diaphoretic), rasaayana (rejuvenating
and adaptogenic) [29], [30], [31]
Modern View
B. aristata is anti-inflammatory, anti-pyretic, analgesic,
antiscorbutic, antiseptic, vulnerary, appetizer, laxative, hepatoprotectant and
emmenagogue.
Berberine
Molecular formula: C20H18NO4
Structural formula:
[32]
Berberrine is a strongly yellow colored, crystalline
alkaloid. Under UV light berberine shows a strong yellow fluorescence.
Berberine is a quaternary ammonium salt from protoberberine group of
isoquinoline alkaloids. [33]
Phytopharmacology of berberine is also described in
detail in the chapter on Guduchee (T. cordifolia)
Pharmacodynamics/ Pharmacokinetics of Berberine
No pharmacokinetic data on animal studies about
Daaruharidraa (Berberis aristata) is available. However, in humans, oral
administration of 1.2 g of berberine significantly delays small intestinal
transit time. [34]
Absorption: Eight hours after
administration of 500 mg/ kg of berberine to infant rabbits, the blood
concentration was 0.8 microgram/ml. Berberine can be absorbed through skin [35]
Metabolism: Peak concentration of
berberine reaches after 12 hours in the muscles and liver.
Distribution: In rats, after the oral dose
of 0.1g/kg maximum serum concentration is 0.083mcg/ml and time to maximum
concentration is 2.4 hours. The blood levels plateau at 4 to 24 hours. [36]
Excretion: Berberine is excreted through urine and feces. The
elimination half-life of berberine in rats is between 5 and 6 hours, peak
urinary excretion is between 12 and 24 hours while peak fecal excretion is seen
after 48 hours. [37], [38]
Anti-inflammatory activity of Berberine
Berberine inhibits activator protein-1activity which
is essential for inflammation.
Berberine inhibits cyclo-oxygenase-2 (COX-2) enzyme.
Berberine significantly inhibits interleukin-1
(IL-1) and interleukin-8 (IL-8) and decreases leukotriene formation.
Berberine significantly decreases leukotriene
formation and monocyte production. It inhibits PGE2 generation by monocytes.
By decreasing vascular permeability, berberine
inhibits inflammatory edema. [39]
Anti-oxidant activity of Berberine
Berberine has anti-oxidant effects in the riboflavin
system. In xanthine oxidase system its anti-oxidant effect is greater than that
of vitamin E. It exhibits anti-oxidant activity via inhibition of lipooxygenase
and lipid peroxidation. [40]
Immunomodulating activity of Berberine
Berberine shows significant inhibition of mitogen
induced lymphocyte transformation.
Berberine inhibits
neutrophil adherence and chemotaxis. [41]
Anti-microbial activity of Berberine
Berberine has significant anti-microbial activity
against Gram positive and Gram negative bacteria and fungi. [42]
In vivo study with white mice berberine showed
antibacterial activity against Streptococcus pneumoniae. [43]
In vitro (in mice) methyl
extract of berberine demonstrated ‘cidal’ activity against T. vaginalis, G.
lamblia, and E. histolytica. [44]
Berberine sulphate
is bactericidal against Vibrio cholera at 35 mcg/ml concentration, against
Staphylococcus aureus at 50mcg/ml concentration and Streptococcus
pyogenes at 30mcg/mL concentration. Berberine also shows anti-bacterial
activity against Escherichia coli, Shigella dysenteriae, Salmonella
paratyphi and various Klebsiella species. Berberine sulphate also exhibits
antimicrobial activity against Gram-positive, Gram-negative bacteria, fungi and
protozoal organisms through the inhibition of RNA and protein synthesis. [45],
[46]
In
an in vitro study, berberine was shown to suppress the growth of Helicobacter
pylori in a dose dependant manner. [47]
Actions of Berberine on Nervous System
To evaluate cholinergic activity of berberine, in
one study, berberine was administered to rats at the dose of 0.1 g/kg and 0.5/kg
for 14 days. This treatment improved scopolamine-induced amnesia in rats. This
effect was augmented by physostigmine and neostygmine. [48]
Berberine has muscle
relaxant effect on smooth muscles. In one study at the dose of 20mcg/kg body
weight berberine sulphate blocked the response of ileum, trachea and rectal
muscles to acetylcholine. [49]
In animal study berberine sulphate produced sedation
and potentiated the sedative effects of pentobarbitone. [50]
In mice berberine has shown to lower rectal
temperature, reduce spontaneous motor activity and prolong
hexobarbitone-induced sleeping time. [51]
Actionsons of Berberine on Endocrine
System
In an animal study berberine has been shown to
inhibit parathyroid hormone-stimulated bone resorption. At doses of
30-50mg/kg/day berberine prevents the decrease in bone mineral density of
lumbar vertebrae in oophorectomised rats and induces apoptosis of osteoclastic
cells. [52]
Actions of Berberine on GI system:
Given orally to mice at doses of 0.06 mg to 20 mg/kg
daily decreases the frequency of purging by delaying intestinal motility. In
mice at doses of 40 and 80 mg/kg bodyweight berberine sulphate decreases the
occurrence of purging induced by castor oil. [53], [54]
By delaying intestinal motility berberine shows
anti-diarrheal activity. Berberine significantly inhibited the actions of Vibrio
cholera enterotoxin and E. coli enterotoxin when administered before
or up to four hours after toxin injection.
In experimental studies berberine reduced the
secretion of water, sodium, chloride and bicarbonate induced by cholera-toxin
in rat ilea. It also inhibited the secretary response to E. coli
enterotoxin.
Results suggest that the antidiarrheal property of
berberine is mediated via its ability to delay the small intestinal transit. [55],
[56], [57]
Actions of berberine on hepato-biliary system:
Berberine increases the secretion of bilirubin in
rats with hyperbilirubinemia but this effect diminishes on continued
administration of berberine. [58]
However a recent study shows that berberine displaces
bilirubin from albumin in both in vitro and in animal studies, resulting
in an increase in serum total and direct bilirubin concentrations. [59]
In an in vitro study, berberine has been
shown to be hepatoprotective when administered twice a day for two days before
receiving toxic doses of paracetamol. [60]
CCl4 is a known hepatotoxic agent. The
CCl4 toxicity is manifested by elevation of liver enzymes and
histological changes in the hepatic tissue. On administration of berberine the
elevated levels of liver enzymes come to normal and histological study shows
reversal of the damage. Berberine at the dose 10mg/kg markedly attenuates the
expression of TNF-α, COX-2 and iNOS. Thus berberine inhibits the inflammatory
response of CCl4 toxicity in the liver. [61]
At doses of 2mg/kg intramuscularly or 3mg/kg orally
thrice a day berberine prevents the development of amoebic hepatitis in hamsters.
[62]
For
in vitro study of anti-hepatitis B activity of berberine, HepG2.2.15 cell
model was selected. The result of the study revealed that berberine can inhibit
hepatitis B virus in vitro. The antiviral effect may be related to AP-1
up-regulation and CHOP down regulation. Further study is necessary to confirm
the mechanism of anti-hepatitis B activity of berberine. However in Feb. 2010,
the researchers have applied for patent for this work. [63]
On
Feb 20, 2013, the application for a patent (Code No C12) was rejected. [64]
The
precise mechanism of development of non alcoholic fatty liver disease (NAFLD)
is not understood. Obesity, dyslipidemia, insulin resistance, deposition of
intra hepatic fat and inflammation are crucial players in the process of NAFLD.
NAFLD is the hepatic manifestation of obesity and metabolic syndrome.
By
correcting hyperlipidemia, berberine strongly reduces storage of fat in the
liver. Treatment with berberine for sixteen weeks alleviates hepatic steatosis.
Berberine also reduces hyperlipidemia in statin-intolerant subjects. Diabetes
predisposes to steatosis. Berberine reduces the insulin resistance, controls
diabetes, and prevents hepatic steatosis. Further berberine prevents the
development of obesity, insulin resiastance and reverts hypertriglycerinemia to
normal levels. Thus berberine prevents and arrests the progression of fatty
degeneration of the liver. Investigations show that berberine supplement
reduces alanine and aspertate transaminases in type 2 diabetes, indicating the
restoration of liver function. Furthermore, berberine has been shown to reduce
liver necrosis in NAFLD and in steatosis due to hepatitis C infection. The
recent literature suggests that berberine may be integrated into glucose and
lipid regulation for combating NAFLD and metabolic syndrome. [65]
Actions of berberine on
Cardiovascular System (CVS)
Berberine
extract inhibits adrenalin-induced aortic contraction, improves the left
ventricular function in dogs with failing heart, decreases the peripheral
resistance, increases significantly the cardiac output and ejection fraction.
It also exhibits anti-arrhythmic activity and restores normal sinus rhythm.
[66]
The
bolus dose of 1mg/kg of berberine sulfate injection administered to rats one
minute after undergoing coronary artery occlusion significantly reduced early
mortality from ventricular fibrillation. [67]
Berberine
sulfate decreases the blood pressure in experimental animals. The effect is
dose-dependent. This hypotension is not inhibited by atropine, mepyramine
maleate, propranolol and phenoxybenzamine. [68]
In
rats at 20mg/kg berberine inhibits platelet-activating factor. It inhibits
platelet aggregation caused by ADP, arachidonic acid and collagen. [69]
Antineoplastic
activity of berberine
Berberine inhibits etoposide and campothecin induced DNA
fragmentation and apoptosis of thymocytes.
Berberine inhibits activator protein-1 activity which is
essential for carcinogenesis.
After 3 days of continuous exposure in vitro,
berberine significantly inhibited hepatoma cell growth in a dose-dependent
manner. It also inhibited the release of α fetoprotein after 18 hours of
exposure. [70]
Oxyberberine
Molecular formula: C20H17NO5
Structural formula:
Oxyberberine and berlambine
are synonyms. Pharmacology of oxyberberine is similar to that of berberine. [71]
Berbamine
Molecular
formula: C37H40N2O6
Structural
formula:
Berbamine is anti-inflammatory and anti-oxidant. It
prevents ventricular fibrillation by means of inhibition of sodium and calcium
overload. It exhibits anti-arrhythmic effect. It is calcium channel blocker and
vasodilator. [72], [73], [74]
At the dose of 25 mg/kg dose berbamine shows
immunosuppressant effect. [75]
At 10mg/kg dose berbamine inhibits neutrophil
adherence and chemotaxis.
At higher doses splenic cells are suppressed. Berbamine
significantly inhibits mitogen induced lymphocyte transformation. [76]
Berbamine
inhibits the tumor necrosis factor and platelet activating factor in a dose
dependant manner. [77]
Berberrubine
(Hydrochloride)
Molecular formula: C19H16NO4
Structural formula:
Pharmacology of berberrubine
hydrochloride is similar to that of berberine, but berberrubine hydrochloride
has predominantly anti-tumor activity. [79]
Aromoline
Molecular formula: C36H38N2O6
Structural formula:
[80]
Pharmacology of aromoline is
similar to berberine. In addition it shows vasodilator, anti-hihtaminic,
anti-amoebic and anti-plasmodial activity. [81]
Protoberberine (Karachine)
Molecular formula: C26H27NO5
Structural formula:
Berberine, Protoberberine and Palmatine belong to
isoquinoline alkaloids.
The
protoberberine alkaloids display a broad range of pharmacological activities as
mentioned in folk medicine in China, India and many other Asian countries.
They
inhibit acetylcholine esterase comparable to physostigmine. [84]
In a comparative study protoberberine was shown to
inhibit lipoxygenase and lipid peroxidation leading to its antioxidant
properties. The antioxidant activity of oxyberberine, corytuberine and
columbamine is stronger than berberine. [85]
Protoberberine alkaloids showed anti-hepatitis B
actions when tested with HepG2.2.15 cell line in vitro. [86]
Palmatine
Molecular formula: C21H24NO4+
Structural formula:
Palmatine
is a protoberberine alkaloid found in many plants. This has been used to treat
inflammations, hypertension, dysentery, jaundice and liver diseases.
This
compound has a potential for the treatment of flavivirus infection. [87], [88]
Jatrorrhizine
Molecular formula: C20H20NO4
Structural formula:
Jatrorrhizine
is a protoberberine alkaloid found in many plants. It shows anti-inflammatory,
antibacterial, antiviral, antifungal and anti-parasitic activity. In large
doses (50-100 mg/kg), in rats it reduces blood sugar. It improves blood flow in
chemically poisoned rat liver. It interferes with multidrug resistant (MDR)
cancer cells. Its synthetic derivative has stronger antibacterial activity. [89]
Chelidonic acid
Molecular formula: C7H4O6
Structural formula:
Chelidonic acid exhibits anti
allergic activity. It decreases Ig E levels, decreases eosinophils and mast
cells in the nasal mucosa in allergic rhinitis. [90], [91]
Oxycanthine
Molecular formula: C37H40N2O6 [91]
Structural formula:
Oxycanthine is also
spelled as Oxyacanthine. Oxycanthine exhibits anti-bacterial activity. Its pharmacological
actions are similar to that of berberine but oxycanthine is much less
effective. [92]
Columbamine
Molecular formula: C20H20NO4
Structural formula
[93]
Columbamine inhibits
proliferation and neovascularization of metastatic osteosarcoma. Columbamine
induces cell cycle arrest at the G2/M transition. Columbamine inhibits U2OS
cell-mediated neovascularization. Thus Berberis aristata that contains
columbamine can be a future anticancer drug. [94]
Isotetrandine
Molecular formula: C38H42N2O6
Structural formula:
Isotetrandrine
can enhance the cytotoxicity of doxorubicin. Researchers suggest that
isotetrandrine might become a candidate for multidrug resistant cancers. [96]
Some Testiminials
from Modern research
Hepatoprotective
Activity
Berberine is the prime important pharmacologically
active molecule in all the species of Berberis. Hence the pharmacology
of Daaruharidraa (Berberis aristata) is the pharmacology of berberine.
It is described in detail above. However in the experimental studies where all
parts of the herb are used to observe the pharmacological actions are described
here.
Berberis aristata protects the liver from CCl4 toxicity.
This activity is mediated through inhibition of microsomal drug metabolizing
enzyme. [97]
Often Berberis vulgaris and Berberis
aristata are used as synonyms for Barberry. Berberis vulgaris
exhibits anti-hepatitis C activity. This effect is attributed to
immunostimulant potential as it enhances the phagocytic activity of mononuclear
cells in the blood. [98]
To
evaluate anti-cirrhotic activity of Daaruharidraa (Berberis aristata),
cirrhosis was induced in rats by using Dimethylnitrosamine. The cirrhosis was
proved by elevated liver enzymes, hematological abnormalities and histological
changes. The oral administration of Ethanolic Extract of Berberis aristata
(EEBA) and Aqueous Extract of Berberis aristata (AEBA) at the dose of
200mg/kg, decreased the size of cirrhotic nodules, improved the biochemical and
hematological parameters. These results were compared with the dose of 100mg/kg
of silymarin, the standard drug used as a hepatoprotectant. The results showed
that EEBA and AEBA exhibit anti-cirrhosis activity similar to silymarin.
However EEBA is more effective than AEBA.[99]
In one study Earlich-Ascites-Carcinoma was induced in
Swiss albino mice by injecting 106 cell/ml of tumor cell suspension.
EEBA and AEBA were used to treat these animals. Daaruharidraa (Berberis
aristata) improved the general condition of the animals. The animals gained
weight. The survival of the animals was prolonged. But these results were
inferior to the anti-tumor effect of 3.5 mg/kg dose of cisplatin. Of the two extracts of Daaruharidraa
(Berberis aristata), EEBA was more effective. [100]
Culinary
Uses
The
fruits are eaten as dessert. They are succulent, sweet and contain nutrients
and antioxidants. The roots and fruits are used to prepare alcoholic drinks.
The acidic flower buds are made into sauce.
Medicinal Actions and Uses
Traditional Uses
Daaruharidraa
(B. aristata) is used externally to treat skin inflammations, contusions,
wounds and ulcers. To treat conjunctivitis, trachoma and ophthalmic conditions
“Rasaanjana” is used.
Internally
it is used to treat PUO, malaria, to quench excessive thirst, to improve
appetite, to treat diarrhea, jaundice, to eliminate poisons and toxins, for
bronchitis, bronchial asthma, for urinary problems, menstrual problems, to
treat gynecological problems etc.
Daaruharidraa
(Berberis aristata) has been in use worldwide for the treatment of
diarrhea, diseases of the liver and gallbladder. It is used as a bitter tonic,
stomachic, cholagogue, antiperiodic and alterative in cases of remittent and
intermittent fevers.
In
India, its preparation ‘Rasaut’ mixed with honey is used for mukhapaaka
(stomatitis, aphthous ulcers), abrasions and ulcerations of the skin. [101]
Ayurvedic Usages
Internal-It is indicated for liver disorders, arsha (bleeding
hemorrhoids), paandu (anemia), kaamalaa (jaundice), agnimaandya (loss of
appetite), aruchi (loss of taste), rakta pitta (bleeding disorder), rakta
pradara (menorrhegia), shweta pradara (leucorrhea), kushtha (leprosy), kandu
(itching), jwara (PUO).
External- Netra vikaara (ophthalmic
disorders especially inflammatory or infective such as conjunctivitis), karna
shoola (ottalgia), pooti karna (purulent discharge from the ear), gandamaalaa
(cervical lymphadenitis mostly tubercular), bhagandara (fistula), mukharoga
(stomatitis).
Daarwyaadi Ghana Sattwa
watee (Tablet from Ayurvedic Medicine): has been used in Shwetapradara
(Leucorrhea) and other diseases.
Ayurvedic
practitioners use it to treat jaundice, enlargement of liver and spleen (portal
hypertension). [102]
Usages in Modern Medicine
B. aristata contains berberine. It can therefore be used to treat
all the ailments where berberine is used. Pharmacological actions and medicinal
usages of berberine have been discussed in detail in the chapter on Guduchee (T. cordifolia).
Here
are some more usages
1. Stomatitis, glossitis, gingivitis,
dyspepsia, hyperacidity, diarrhea, IBD,
helminthiasis
2. Viral hepatitis
3. Dermatitis, psoriasis
4. Vaginitis, leucorrhea
5. Toxic shock syndrome
6. Pharyngitis, bronchitis
7. Dyslipidemia.
8. Diabetes [103]
Toxicity
LD50 value of berberine in mice was
found to be 25.3 mg/kg I. P. But in human beings berberine is free from
any serious toxicity.
In
larger doses B. aristata can be toxic
giving rise to symptoms such as vomiting, severe diarrhea, excessive sweating,
lethargy, nose bleed, severe hypotension, skin and eye irritation and urinary
problems. In such cases the drug or any preparations containing B. aristata should be withdrawn.
Standardized
extracts of the plant can cause stomach upset and should not be used for more
than two weeks at a time.
Contraindications
It is contraindicated for infants and young children. In pregnant women
it can cause uterine contractions and in first trimester can cause abortion. It
is contraindicated during lactation.
It is toxic to growing sperm cells. Hence males of reproductive age
group should not use it as it may contribute to sterility.
Drug Interactions
It interacts with doxycycline, tetracycline. Interactions with other
antibiotics should also be borne in mind.
Preparations and Dosages
Any form of the preparation should not
be taken for more than five days at a time.
Decoction: To make decoction, take a teaspoon of bark, and 100 to
150 ml of water, bring to boiling, leave for 10 to 15 minutes.
Dose: 50 to 100 ml
Decoction of
the Stem: 5 to 15 ml.
Extracts: Standardized to contain 5 to 10% alkaloids, with a
total of approximately 500 mg of berberine is the recommended dosage; 1-3 g
(CCRAS); extract of dried stem- 5-10 ml decoction; API Vol. II
Fruit
Powder: 5 to 10 grams
Powder of
the Stem: 3 to 6 Grams
Root bark
juice: 12 to 24 ml
Tincture: 2 to 5 ml to be taken 15 to 20 minutes before meal,
thrice a day
Tea: To make tea, take 2 to 4 grams of Barberry root or 1
to 2 teaspoonful berries, steep in 150 ml of water for 10 to 15 minutes. Take
one cup three times a day. It can be used as mouth wash or for gargle to allay
sore throat.
Dry
Extract: 250 to 500 mg three times a day
Ointment: To make ointment use 10% extract. For psoriasis apply
three times a day
For older patients (above 65 years of age) use lower
doses
Rasaanjana
Daarwyaadi
Kwaath (Water decoction): 10 to 20
ml. once or twice a day, before or after food as directed by Ayutvedic doctor
Daarwyaadi
Kashaaya (Water decoction): 10 to 20
ml. once or twice a day, before or after food as directed by Ayutvedic doctor.
[104]
Daarwyaadi
Leha (Paste for oral use): Dose not found
Dashaanga
Lepa (Paste for External Application)
Daarwyaadi
Taila (Oil preparation)
Capsules:
Daaru-Haridraa paste is used for conjunctivitis. In ophthalmic conditions
the paste is applied around eyes. It is also use to treat chancroid ulcers,
goiter, fistula and erysipelas.
Daaru-Haridraa rasaanjan combined with rose
water is used to treat ear ache and
ear discharge.
Daaru-Haridraa douche is used to treat vaginal discharges. [105], [106],
[107]
Rasaut: A
very valuable preparation Rasaut is prepared from
Daaruharidraa. For preparing Rasaut, the bark of the root and of
the lower part of the stem is boiled in water. The solution is then strained
and evaporated till a semi-solid mass, Rasaut, is obtained. Rasaut
is freely soluble in water. It is mixed with butter and alum or with
lime-juice or opium and is applied externally to the eyelids to cure ophthalmia
and other eye diseases. It is mild laxative, tonic and is useful in curing
ulcers and fevers. [108]
References
3. http://en.wikipedia.org/wiki/Doctrine_of_signatures
4. The Ayurvedic Pharmacopoeia of India Part I,
Volume II
8. google images
10. www.alibaba.com
13.
Papiya Mitra Mazumdar, Saumya Das, Manas Kumar Das; Phyto-Pharmacology of Berberis aristata DC: A Review, Journal of Drug
Delivery and Therapeutics, Vol. 1, no 2 , 2011.
HERBS AND HERBAL PRODUCTS,
Ayurvedic Pharmacopoeia of India Vol. 1-6, IP 2010;
16. Sharma Komal et al, Berberis aristata: A Review; IJRAP 2011 2(2):
383-388
17. The Ayurvedic Pharmacopoeia of India, Part 1,
Volume 2
18. The Ayurvedic
Pharmacopoeia of India, Part 1, Volume 2
21.
http://www.sigmaaldrich.com/life-science/plant-profiler/berberis-aristata
22. Sharma Komal et al, IJRAP
2011, 2 (2): 383-388
24. Herbs and Herbal Products,
Ayurvedic pharmacopoeia of India vol. 1-6, IP 2010;
http://www.ipc.gov.in/writereaddata/linkimages/admin9640017989.pdf
25. Chromosome Count Data
Base, http://ccdb.tau.ac.il/Angiosperms
26.
http://shodhagana.inflibnet.ac.in/bitstream/10603/4494/8/08_chapter%202.pdf
HERBS AND HERBAL PRODUCTS, Ayurvedic
Pharmacopoeia of India Vol.
1-6, IP 2010;
34. Yuan J, Shen XZ,
Zhu XS, Effect of berberine on transit time of human small intestine; Zhongguo
Zhong, 1994; 14 (12): 718-720
35. Bhide M. B., Chavan S. R., Datta N. K.; bsorption, distribution and
excretion of berberine, Indian J Med Res, 1969; 57(11): 2128-2131
36.
http://www.sigmaaldrich.com/life-science/plant-profiler/berberis-aristata
37. Bhide M. B., Chavan S. R., Datta N. K.; bsorption, distribution and
excretion of berberine, Indian J Med Res, 1969; 57(11): 2128-2131
38.
http://www.sigmaaldrich.com/life-science/plant-profiler/berberis-aristata
39.
http://www.sigmaaldrich.com/life-science/plant-profiler/berberis-aristata
40. Haisong J et al, Scavenging effect of berbamine on active oxygen
radicals in phorbol ester-stimulated human polymorphoneuclear leukocytes;
Biochemical Pharmacology 1990; 39(11): 1673
41.
http://www.sigmaaldrich.com/life-science/plant-profiler/berberis-aristata
42. Freile ML et al
Antimicrobial activity of aqueous extracts of berberine isolated from Berberis
heterophylla. Fitoterapia 2003; 74 (7-8): 702-705
43. Hashmi K, Hafiz A; In vivo antibacterial activity of Berberis
asiatica, J Pak Med Assoc 1986; 36(1): 5-7
44. Kaneda Y, Tanaka T
and Saw T, Effects of berberine, a plant alkaloid, on the growth of anaerobic
protozoa in axenic culture. Tokai J Exp Clin Med 1990; 15(6): 417-423
45. Amin A et al, Berberine sulphate: antimicrobial
activity, bioassay and mode of action, Can J Microbiol 1969; 15(9): 1067-1076
46. Sun D et al, Berberine
sulphate blocks the adherence of Streptococcus pyogenes to epithelial cells,
fibronectin and hexadecane, Antimicrobial Agents and Chemotherapy 1988; 32(9):
1370-1374
47. Chung JG et al, Inhibitory
actions of berberine on growth and aryl-amine N-acetyltransferase activity in
strains of Helicobacter pylori from peptic ulcer patients, International
Journal of Toxicology 1999; 18:35
48. http://www.sigmaaldrich.com/life-science/nutrition-research/learning-center/plant-profiler/berberis-aristata.html
49. Kulkarni S.K., Dandiya P. C.,
Varandani N. L. Pharmacological investigations of berberine sulphate Jpn J
Pharmacol 1972; 22(1): 11-16
50. Shanbhag S. M., Kulkarni H. J., Gaitonde B. B. Pharmacological
actions of berberine on the central nervous system Jpn J Pharmacol 1970; 20(4):
482-487
In mice berberine has shown to lower rectal temperature, reduce
spontaneous motor activity and prolong hexobarbitone-induced sleeping time.
[51]
51. Sabir M and Bhide NK, Study of some pharmacological actions of
berberine. Ind J Physiol and Pharmac 1971; 15(3): 111-132
52. Li H et al, The effect of kampo formulae on bobe resorption in
vitro and in vivo. ll. Detailed study of berberine. Biol Pharm Bull 1999;
22(4): 391-396
53. Akhtar M. H., Sabir M, Bhide
N. K.; Possible mechanism of antidiarrhoeal effect of berberine, Indian J Med
Res 1979; 70: 233-241
54. Zhang M. F. and Shen Y. Q.
Antidiarrheal and anti-inflammatory effects of berberine; Zhongguo Yao Li Xue
Bao 1989; 10(2):174-176
55. Sack RB, Froehlich JL, Berberine inhibits intestinal secretory
response of Vibrio cholera and Escherichia coli enterotoxins, Infect Immun
1982; 35(2):471-475
56. Swabb EA, Tai YH, Jordan L; Reversal of cholera toxin-induced
secretion in rat ileum by luminal berberine, Am J Physiol 1981; 241; (3):
G248-G252
57.http://www.sigmaaldrich.com/life-science/nutrition-research/learning-center/plant-profiler/berberis-aristata.html
58. Chan MY, The effect of berberine on bilirubin excretion in the rat;
Comp Med East West 1977; 5(2): 161-168
59. Chan E, Displacement of bilirubin from albumin by berberine, Biol
Neonate 1993; 63(4): 201-208
60. Gilani AH and Janbaz
KH; Prevention of acetaminophen-induced
liver damage by Berberis aristata
leaves; Biochem Soc Trans 1992; 20(4): 347S
61. Robert Domitrovic et al, Hepatoprotective activity of berberine is
mediated by inhibition of TNF-α, COX-2 and iNOS expression in CCL4- intoxicated
mice; Toxicology Volume 280 Issue 1-2; 4 February 2011, Pages 33-43.
62. Subbaiah TV and Amin AH; Effect of berberine sulphate on Entamoeba
histolytica, Nature 1967; 215(100): 527-528
63. http://www.google.com/patents/CN101642454A?cl=en
Feb. 10, 2010
65. Yang Liu et al, Update on
Berberine in Nonalcoholic Fatty Liver Disease; Evidence-Based
Complimentary and Alternative Medicine; Volume 2013, Article ID 308134, 8
pages; http://dx.doi.org/10.1155/2013/308114
66. Wang et al Effects of
berberine on delayed after-depolarizations in ventricular muscles in vitro and
in vivo, Journal of Cardiovascular Pharmacology 1994; 23(5): 716-722
67. Ribeiro LG et al,
Beneficial effects of berberine on early mortality after experimental coronary
artery occlusion in rats, Circulation 1982; 66: II-56
68. Sabir M and Bhide N. K.
Study of some pharmacological actions of berberine, Ind J Physiol and Pharmac
1971; 15(3):111-132
69. Wu JF, Liu TP, Effects of
berberine on platelet-aggregation and plasma levels of TXB2 and
6-keto-PGF1 alpha in rats with reversible middle cerebral artery occlusion, Yao
Xue Xue Bao 1995; 30(2): 98-102
70. http://www.sigmaaldrich.com/life-science/nutrition-research/learning-center/plant-profiler/berberis-aristata.html
71.
http://www.medicinabiomolecular.com.br/biblioteca/pdfs/Cancer/ca-2158.pdf
72. http://en.wikipedia.org/wiki/Berbamine
73. http://www.chemblink.com/products/15401-69-1.htm
75. Luo C et
al, Study on the immunosuppressive effects of berbamine and its mechanism.
Phytotherapy Research 1997; 11: 585-587
76. Li SY et
al; Anti-inflammatory and immunosuppressive properties of the
bis-benzylisoquinolins: in vitro comparisons of tetrandrine and berbamine, Int
J Immunopharmacology 1989; 11(4):395-401
77.
http://www.sigmaaldrich.com/life-science/plant-profiler/berberis-aristata
78. http://www.chemblink.com/products/15401-69-1.htm
79. Hoshi A, Ikekawa T, Ikeda Y, Shirakawa S, Ligo M,
Antitumor activity of berberubbine derivatives; Gann. 1976 Apr 67(2): 321-5
80. http://www.chemicalbook.com
81. http://books.google.co.in
84. Koji SHIGETA et al,
Bioscience, Biotechnology and Biochemistry, Vol.66, 2002, No. 11
85. Misik V et al; Lipoxygenase inhibition and antioxidant properties
of protoberberinr and aporphine alkaloids isolated from Mahonia aquifolium;
Planta Med 1995; 61(4): 372-373
86. Li HL et
al, Alkaloids from Corydalis saxicola and their anti-hepatitis B virus
activity; Chem Biodivers. 2008 May; 5(5): 777-83.
87.
http://en.wikipedia.org/wiki/Palmatine,
90. http://en.wikipedia.org/wiki/Chelidonic_acid
91. Hyun-A Oh et al, International
Immunopharmacology, Volume 11, Issue 1, January 2011
[93] pubchem.ncbi.nlm.nih.gov/compound/Columbamine
[94] Bao M et al, Columbamine suppresses the
proliferation and neovascularization of metastatic osteosarcoma U20S cells with
low toxicity; Toxicol Lett 2012 Dec 17; 215(3):174-80
[95] Pubchem.ncbi.nlm.nih.gov/compound/457825
[96] Wang TX, Yang XH,
Reversal effect of isotetrandrine, an isoquinoline alkaloid extracted from
Caulis Mahoniae, on P-glycoprotein-mediated doxorubicin-resistance in human
breast cancer (MCF-7/DOX)cells, Yao Xue Xue Bao 2008 May; 43(5): 461-6
[97] Gilani AH and Janbaz
KH; Prevention of acetaminophen-induced
liver damage by Berberis aristata leaves; Biochem Soc Trans 1992; 20(4): 347S
[98]Doaa Ghareb et al,
Biological assessment of Berberis vulgaris and its constituent berberine:
Antibacterial, antifungal and anti-hepatitis C virus (HCV) effect; Journal of
Medicinal Plants Research, Vol. 7(21), pp 1529-1536, June 2013. http://www.academicjournals.org/JMPR
[99] Ajmire, Prashant V,
Effect of Ber DC, Against Diethylnitrosamine Induced Liver Cirrhosis in Rat
Model; Journal of Pharmacy Research; Nov 2011, Vol. 4 Issue 11, p4015.
[100] Pai
KS, Srilatha P et al, Anticancer activity of Berberis aristata in Earlich
ascites carcinoma-bearing mice: a preliminary study; Pharm Biol. 2012 Mar;
50(3): 270-7
[102]
http://jddtonline.info/index.php/jddt/article/view/34/25
[103] http://en.wikipedia.org/wiki/Berberis_aristata
[104] http://ayurmedinfo.com
[105]
http//www.evaidyaji.com
[106]
http//www.ayurviki.info/wiki/daruharidra
[107]
http://www.ayurveda.hu/api/API-Vol-2.pdf
Comments