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Therapeutic Bio-screening of the Bioactive Ingredients of Berberis vulgaris

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Abstract

Barberry (Berberis vulgaris L.; family Berberidaceae) is a well known plant with traditional herbal medical history. The objectives of the present study were to explore the phytochemical constituents of barberry and to bioscreen its crude extracted bioactive ingredients. The effect of barberry's ingredients on lipid peroxidation in chicken liver and human semen acetylcholinesterase (AChE) and -gulcosidase activities were spectrophotometrically determined. Our results showed that barberry contains a 71% total phenolic content, including alkaloids (2.6%), flavonoids (4.9%) and saponin (0.3%). Barberry extract showed potent antioxidative capacity through a decrease in thiobarbituric acid reactive species (TBARS) in liver homogenate, human seminal plasma and spermatozoa by 62.5, 72.6 and 96.5%, respectively. Hepatic -glucosidase activity was enhanced by 51.4% while AChE activity was inhibited by 71%. This work demonstrates the potential of the bioactive ingredients of barberry on suppressing lipid peroxidation, suggesting a promising use in the treatment of hepatic oxidative stress, Alzheimer and idiopathic male factor infertility.
Received: 1 February, 2010. Accepted: 10 August, 2010. Original Research Paper
Functional Plant Science and Biotechnology ©2011 Global Science Books
Therapeutic Bio-screening of the
Bioactive Ingredients of Berberis vulgaris
Mohamed El Sayed1 Doaa A. Ghareeb1 Ashraf A. Khalil2 Eman M. Sarhan1*
1 Bioche mistry Depart ment, Facult y of Sci ence, Alexandria Unive rsity, Egypt
2 Department of Protein Technology, Mubarak City for Scientific Research, Borg Elarab, Alexandria, Egypt
Corresponding author: * eman_sarhan@hotmail.com
ABSTRACT
Barberry (Berberis vulgaris L.; family Berberidaceae) is a well known plant with traditional herbal medical history. The objectives of the
present study were to explore the phytochemical constituents of barberry and to bioscreen its crude extracted bioactive ingredients. The
effect of barberry’s ingredients on lipid peroxidation in chicken liver and human semen acetylcholinesterase (AChE) and -gulcosidase
activities were spectrophotometrically determined. Our results showed that barberry contains a 71% total phenolic content, including
alkaloids (2.6%), flavonoids (4.9%) and saponin (0.3%). Barberry extract showed potent antioxidative capacity through a decrease in
thiobarbituric acid reactive species (TBARS) in liver homogenate, human seminal plasma and spermatozoa by 62.5, 72.6 and 96.5%,
respectively. Hepatic -glucosidase activity was enhanced by 51.4% while AChE activity was inhibited by 71%. This work demonstrates
the potential of the bioactive ingredients of barberry on suppressing lipid peroxidation, suggesting a promising use in the treatment of
hepatic oxidative stress, Alzheimer and idiopathic male factor infertility.
_____________________________________________________________________________________________________________
Keywords: acetylcholinesterase, Berberidaceae, idiopathic male, oxidative stress
Abbreviations: AChE, Acetylcholine esterase; BHT, butylated hydroxytoluene; BRB-chloride, berberine chloride; dH2O, distilled
water; TBA, thiobarbituric acid; TBARS, thiobarbituric acid reactive species; TCA, trichloroacetic acid; -GI, -glucosidase inhibitor
INTRODUCTION
Nature has been a source of medicinal agents since the
beginning of time. The World Health Organization (WHO)
estimates that herbal medicine is still the most common
source for primary health care of about 75-80% of the
world’s population, mainly in the developing countries,
because of better cultural acceptability, better compatibility
with the human body and fewer side effects (Yadav and
Dixit 2008). In ancient oriental medicine, root, leaves,
aerial part and even the whole plant have been used to treat
various diseases (Mohamed et al. 2010). Herbal medicine
offers therapeutics for age-related disorders like memory
loss, osteoporosis, immune disorders, etc. for which no
modern medicine is available (Kamboj 2000). Natural pro-
ducts play an important role in drug development programs
of the pharmaceutical industry (Baker et al. 1995), where
over 50% of all modern clinical drugs are of natural product
origin (Stuffness and Douros 1982). The amazing structural
diversity among their active components make them a use-
ful source of novel therapeutic compounds, thus researchers
with interest in natural products have intensified their
efforts towards scientific evaluation of traditional medicines
(Saeed et al. 2007). Furthermore, medical effects are not
necessarily restricted to a single plant chemical, since the
biological activity and clinical value of the whole plant, as
in medicinal herbalism, is also being pursued (Hanachi and
Golkho 2009).
Berberis vulgaris L. is considered as one of a well
known medicinal plant with traditional herbal medical his-
tory and used by many civilizations as a curative herbal
remedy in homeopathic systems of medicine (Ivanovska
and Philipov 1996). The identification of certain alkaloids
and phenolic compounds in barberry somehow provides an
alternative method for medicine and remedies. Those thera-
peutic compounds could lead to the development of new
drugs derived from that plant, which is believed to be safer
and more effective (Hanachi et al. 2008).
Studies carried out on the chemical composition of bar-
berry show that the most important constituents are isoqui-
noline alkaloids such as berberine, berbamine and palma-
tine (Tab l e 1). Berberine represents one of the most studied
among the naturally occurring protoberberine alkaloids
since it possesses a wide range of biochemical and pharma-
cological activities against cardiac disease, stroke, diabetes,
hyperlipidemia, chronic inflammation (Zhu and Qian 2006),
hypertension, tumors and HIV (Wongbutdee 2008). Bar-
berry also has anti-protozoal, chloretic, cholagogue, cardio-
tonic, anti-cholinergic, anti-arrhythmic effects and anti-
platelet aggregation (Tab l e 2) (Wongbutdee 2008).
The nutritional values such as vitamin components and
antioxidant compounds in barberry plant might be invalua-
®
Tab le 1 Compounds isolated from Berberis vulgaris.
Compound Nature Reference
Aromoline Alkaloid Koike et al. 1982
Berbamine Alkaloid Akasu et al. 1976; Wong et al. 1992
Berberine Alkaloid Wu et al. 1977; Yesilada et al. 2002;
Wa ng et al. 2004; Sudheer et al. 2006
Berlambine Alkaloid Gasparec et al. 1982
Bervulcine Alkaloid Werner 1963
Columbamine Alkaloid Pavelka and Smekal 1976
Hydroxycanthine Alkaloid Hagen et al. 1989
Isocorydine Alkaloid Marsaioli et al. 1979
Oxyberberine Alkaloid Cushman and Dekow 1979
Oxycanthine Alkaloid Hearth et al. 1987
Palmatine Alkaloid Pavelka and Smekal 1976
Quercentin Flavonoid Wu et al. 1977
Rutin Flavonoid Gasparec et al. 1982
(-)-tejedine Alkaloid Kametani et al. 1969
Yatrorizine Alkaloid Gasparec et al. 1982
Aqueous crude extract Fatehi et al. 2005
Functional Plant Science and Biotechnology 5 (Special Issue 1), 63-68 ©2011 Global Science Books
ble for treating diseases. Barberry not only exhibited vary-
ing degrees of antioxidant properties, but antioxidant capa-
cities also varied according to solvents used for the extrac-
tion method (Maznah et al. 1999).
The aim of this study was to explore the phytochemical
constituents of barberry and to bioscreen its crude extracted
bioactive ingredients (Fig. 1). An innovative method was
designated to investigate the effect of barberry's' extracts on
the seminal antioxidant capacity.
Tab le 2 The pharmacological effects of Berberis vulgaris (NAPALERT; Natural Products Alert Database).
System Effect Part of
plant
Preparation Reference
Dried root Alkaloid fraction NAPALERT Cardiovascular Hypotensive activity
Dried fruit Aqueous extract Fatehi-Hassanabad et al. 2005
Gastrointestinal Gastric secretory stimulation Root Ethanol–H2O (67%) extract NAPALERT
Choleretic activity in rat Dried root NAPALERT
Choleretic activity Stem bark NAPALERT
Increases tone of the digestive tract and gives rise t
o
increased and irregular peristalsis
Dried root
Total alkaloids
NAPALERT
Anticholinergic activity in guinea pig ileum Dried fruit Decoction NAPALERT
Menstruation induction effect in guinea pig Stem Ethanol (95%) extract NAPALERT
Endocrine
Uterine stimulant effect in cat, rabbit and guinea-pig Leaf Ethanol-acetone (50%) extract NAPALERT
Antibody formation suppression in mouse Dried root Alkaloid fraction APALERT Immune system
Antiinammatory activity Root Alkaloid fraction Ivanovska and Philipov 1996
Complement alternative pathway inhibition Ethanol (100%) extract Ivanovska and Philipov 1996Organisms
Delayed type cutaneous hypersensitivity inhibition
Root
Alkaloid fraction and ethanol
(95%) extract Alkaloid fraction
NAPALERT
Dried bark Alkaloid fraction NAPALERT Antipyretic activity in rat
Dried fruit Ethanol (95%) extract NAPALERT
Narcotic antagonist activity Dried root NAPALERT
Central nervous
system
Sedative Fruit Fatehi-Hassanabad et al. 2005
Renal Diuretic activity in rat Dried bark Alkaloid fraction NAPALERT
Toxicity assessment in mouse – LD50= 520.0 mg/kg NAPALERT Other
Toxicity assessment in mouse – LD50= 2.6 ± 0.22
g/kg b.w.
Dried root Alkaloid fraction
Peychev 2005
Crude methanolic (95%) extraction Male
reproduction
Idiopathic male factors due to oxidative damage Root
Crude acetic acid (5%) extraction
El-Sayed et al. 2010
Raw material Crude extract
Solubilization of powdered
crude and standard
extracts.
Assessment criteria
1
st
screening lab sca le.
Qualitative phytochemical
screening.
Raw material
Air-dried and well
crushed barberry
(Berberis vulgaris L.
family Ber beridaceae)
roots
alkaloids, phobatannins,
saponnins, flavonoids,
steroids, terpenoids and
cardiac glycosides.
saponnins, alkaloid,
flavonoids, total
phenolics.
Quantitative
phytochemical screening.
-
----------------------------------------------------------------------------------------------------
-
2
nd
screening lab scale.
Raw material
Air-dried and well crushed
barberry (Berberis vulgaris L.
family Berberid aceae) roots
Berberine chloride (used as
standrad reference material).
Ethanol 95%
In vitro activity on liver
homogenate
-TBARS.
- AchE activity.
- -glucosidase acti vity.
In vitro activity on
seminal aliquots
-TBARS.
This step depended on
results obtained from
liver homogenate.
Methanol 95%
Ex.MeOH
Acetic acid 5%
Ex.AcOH
Methanol 95%
St.MeOH
Acetic acid 5%
St.AcOH
Bioactivity of extract preparations on
various biological systems
Fig. 1 Experimental design: Phytochemical screening, extraction, solubilization and assessment of barberry bioactive ingredients. St.MeOH,
standard dissolved in methanol; St.AcOH, standard dissolved in acetic acid; Ex.MeOH, barberry extract dissolved in methanol; Ex.AcOH, barberry
extract dissolved in acetic acid.
64
Bioscreening of barberry. El Sayed et al.
MATERIALS AND METHODS
Materials and chemicals
Barberry were collected from the fields and authenticated by Prof.
Salma Eldareir, Botany Department, Alexandria University, Egypt.
Firstly, the intact plant was removed from the soil, roots were
washed more than once and the plant was firmly pressed between
paper towels. Then the plant roots were separated, packed within
sealable plastic bags and kept out of direct sunlight. Seminal plas-
ma of healthy individuals and spermatozoa samples were collected
by Dr. Sherif S Said (Integrated Sterility Centre of Alexandria,
Egypt). Liver was obtained from Balady (BB) chicken, one of the
local Egyptian chicken strains, and then 1 g was homogenized in 9
mL 0.1 M phosphate buffer, pH 7.4 and stored at -20°C. Trichloro-
acetic acid (TCA), thiobarbituric acid (TBA), berberine chloride,
butylated hydroxytoluen (BHT), acetylthiocholine iodide (ACTI),
p-nitrophenyl--D-glucopyranoside (PNPG) and 5,5-dithiobis 2-
nitrobenzoic acid (DTNB), were purchased from Sigma Chemical
Co. (St. Louis, Mo, USA). HAM’s Nutrient Mixture F-10 was pur-
chased from Euro-Lone Chemical Co. (UK.). Organic solvents of
HPLC-grade like ethanol 95%, methanol and petroleum ether were
brought from Merck (USA). All other chemicals and reagents were
of analytical grade.
Phytochemical screening of barberry
Plant roots were separated and dried at room temperature, pow-
dered, sieved, and stored prior to further use. Dried barberry roots
were phytochemically screened for alkaloids, phobatannins, sapo-
nins, flavonoids, steroids, terpenoids and cardiac glycosides (Ede-
oga et al. 2005).
Extraction of barberry materials
The dried powdery roots of barberry was exhaustively defatted
with petroleum ether and subjected to steam distillation method
for ethanolic gradient extraction with Soxhlet apparatus (Upad-
hyay and Dhawan 1998). The ethanolic extract was concentrated
to minimum volume using rotary evaporator (Büchi, Switzerland)
then lyophilized (DISHI, DS-FD-SH10, Xi’an Heb Biotechnology
Co, China) to obtain a powder extract of barberry (25%). Both bar-
berry powder and berberine chloride (as a standard) were solubi-
lized at 0.1% in two organic solvents with different polarities:
methanol (95%) and acetic acid (5%). The barberry extract were
kept at -20°C until subjected to further biochemical analysis.
In vitro induction of lipid peroxidation in biological
systems
In vitro lipid peroxidation was induced in three biological systems
such as chicken liver, healthy human seminal plasma and sperma-
tozoa as described by Tappel and Zalkin (1959) with some modi-
fications as follows:
1. Lipid peroxidation in liver homogenate
2 mL of barberry extract (test), the organic solvent (control) or
distilled water (dH2O) (blank) were incubated with equal volume
of liver homogenate for about 45 min at 37°C. In vitro tissue lipid
peroxidation was induced by adding H2O2 and ferrous sulphate
(FeSO4·7H2O) at a final concentration of 1 and 0.5 mM, respec-
tively, in both test and control reaction mixtures. After an incuba-
tion period of about 30 min at 37°C, BHT at a final concentration
of 0.02% was added and mixed carefully to stop the peroxidation
reaction. The mixtures were centrifuged at 3000 rpm for 15 min,
and then 1 mL of the resultant supernatant was mixed with 1 mL
of TCA (15%) followed by centrifugation at 3000 rpm for 10 min.
2. Lipid peroxidation in seminal plasma and spermatozoa
100 μL of each prepared extract (test), organic solvent (control) or
saline (blank) were incubated for 15 min with an equal volume of
healthy Egyptian human semen samples followed by addition of
400 μl of HAM’s Nutrient Mixture F-10. Then the reaction mix-
tures were centrifuged under cooling at 3000 rpm for 30 min.
Supernatants were carefully separated from the spermatozoa's
pellets. Then, spermatozoa's pellets were suspended in about 500
μL of sodium phosphate buffer, 0.1 M, pH 7.4. For 500 μL semi-
nal plasma (supernatant) or the suspended spermatozoa’s pellet, 1
mL of TCA (15%) was added and the solutions were centrifuged at
-4°C for 10 min to obtain protein free supernatant.
Biochemical assays
1. Determination of AChE activity
AChE activity was measured according to the method of Ellman et
al. (1961). 130 L phosphate buffer (0.1 M pH 7.4) were added to
a mixture of 20 L of liver homogenate and 20 L of barberry
extract (test) or organic solvent (control), then incubated for 45
min at 37°C. 5 L of substrate ACTI (75 mM) were added, mixed
well and incubated for 15 min at 37°C. 60 L DTNB (0.32 mM)
were added and left for 5 min. The absorbance was measured at
405 nm and the specific activity was calculated.
2. Determination of -glucosidase activity
Method mentioned by Han and Srinivasan (1969) was carried out
with a slight modification to estimate the effect of barberry extract
on -glucosidase (EC 3.2.1.20) activity. 100 L of barberry extract
(test), organic solvents (control) or dH2O (blank) were diluted with
2.5 mL 0.1 M phosphate buffer pH 7.4. 100 L of liver homo-
genate were added, mixed well and incubated in a water bath with
the reaction mixture at 30°C for 5 min. 500 L PNPG, 5 mM, was
added and the reaction was allowed to proceed for 15 min. The
reaction was stopped by the addition of 2 mL of 1 M Na2CO3. The
producing color was spectrophotometrically detected at 400 nm. A
unit of enzyme activity was defined as nmoles of p-nitrophenol
released/min.
3. Determination of TBARS level in induced lipid
peroxidation
TBARS was determined in liver, protein free supernatant of semi-
nal plasma and spermatozoa samples according to the method des-
cribed by Tappel and Zalkin (1959). 1 mL of protein free super-
natant was mixed with 500 μL TBA (0.7%), heated in boiling
water bath for 45 min, cooled and the colour in the supernatant
was dead at 532 nm. The TBARS level was calculated against
with a control without the extract according to the following equa-
tion: TBARS level (nmol/ml) = At / 0.156.
Statistical analysis
Data are expressed as the standard deviation S.D. One-way analy-
sis of variance (ANOVA) followed by Student Newman-Keul’s
test, which was provided by Primer of Biostatistics program (Ver-
sion 5). The differences were considered statistically significant at
P < 0.05.
RESULTS AND DISCUSSION
Preliminary phytochemical screening of barberry’s roots re-
vealed the presence of alkaloids, flavonoids, saponin, phe-
nolic contents, terpenoids and cardiac glycosides. However,
steroid and phobatannins were not detected. The percentage
of alkaloids, flavonoids, saponin and total phenolic content
were 2.55, 4.9, 0.3 and 70.9%, respectively (Tabl e 3 ). All
these phytochemical constituents would act in synergy in
Tab le 3 Quantitative phytochemical screening of barberry*.
Components** % Concentration ±SD
Saponin 0.3 ± 0.5
Alkaloid 2.6 ± 0.4
Flavonoid 4.9 ± 0.5
Total phenolic content 71 ± 11
* Values are expressed as % of dry raw weight
** Data expressed as ± standard deviation "SD", P < 0.001.
65
Functional Plant Science and Biotechnology 5 (Special Issue 1), 63-68 ©2011 Global Science Books
order to increase barberry’s bioactivity such as antioxidant,
antimicrobial, anticholinergic, anti-diabetic, etc. (Wongbut-
dee 2008). Barberry polysaccharides, cardiac glycosides
were clinically used to increase contractile force in patients
with cardiac disorders through a mechanism of action invol-
ving inhibition of the plasma membrane Na+/K+-ATPase
leading to alterations in intracellular K+ and Ca2+ levels
(McConkey et al. 2000; Reuter et al. 2001).
The barberry crud extract and berberine chloride solu-
tion were prepared at a concentration of (0.1%) in methanol
or acetic acid to explore polarity dependent effects.
Anticholinergic activity of the study preparations is
shown in Fig. 2, where the acetic acid preparations of bar-
berry crude extract and berberine chloride were significantly
inhibited the AChE activity by 71 and 80.6%, respectively.
These potent anticholinergic properties of barberry are due
to its polyphenolic derivatives. Hence barberry might have
a therapeutic potential for the treatment of Alzheimer’s dis-
ease. Ghareeb et al. (2010) stated that barberry has a com-
petitive inhibitory ability suggesting its use to alleviate over
activity of AChE in dementia patients.
The methanolic and acetic acid preparations of the plant
crude extract increased the -glucosidase activity by 175.4
and 51.4%, respectively, at P < 0.005 (Fig 3). The great
enhancement for -glucosidase enzyme activity provides an
effective way in enzyme replacement therapy of glycogen
storage disease type II that caused by lysosomal acid []-
glucosidase deficiency, where patients have a rapidly fatal
or slowly progressive impairment of muscle function (Bij-
voet et al. 1998).
As shown in Fig. 4, acetic and methanolic extracts of
barberry were potent inhibitors of lipid peroxidation in-
duced by Fe2+ and H2O2 in liver homogenate, healthy human
seminal plasma and spermatozoa.
Experiments were done to demonstrate the hepatopro-
tective potential of barberry extracts. Both crude extract and
berberine chloride dissolved in acetic acid showed a
significant decrease at P < 0.005 in liver TBARS by 62.5
and 74.1%, respectively, compared to those dissolved in
methanol. This variation in the bioactivity between the two
different preparations could be a result of polarity dif-
ference between acetic acid and methanol where organic
acids’ polarity is much greater than that for alcohols. That
observation is supporting by the hypothesis of the ability for
most polar solvents to dissolve the most polar bioactive
ingredient (Sarker and Nahar 2007).
Hanachi and Golkho (2009) reported that the most polar
solvent dissolving several compounds of different polarity
such as acids, sugars or glycosides which may be contri-
buted to the total phenolic content of the extract and repre-
sented the highly antioxidant properties. Depending on this
we speculated that acetic acid extract preparations exhibited
appreciable antioxidantive activity against the generation of
cellular oxidized lipid particles. Therefore, acetic acid ex-
tract was selected for further experiments carried out on
human seminal plasma and spermatozoa.
We noticed that acetic acid barberry extract was signi-
ficantly decreased the TBARS level in seminal plasma and
spermatozoa by 72.58 and 96.46%, respectively. This sig-
nificant antioxidant activity of barberry could be attributed
to its high contents of active phytochemicals as previously
mentioned. Furthermore, our data reflecting the possibility
6.79±0.47
23.44±9.39
70.98±2.79
80.61±4.35
0
10
20
30
40
50
60
70
80
90
% Inhibition
methanolic barberry extract methanolic berberine chloride preparation
acetic acid barberry extract acetic acid berberine chloride preparation
Fig. 2 Effect of the prepared extracts (methanolic and acetic acid) on hepatic AChE. Values represent the mean of three replicates ± standard
deviation (SD) (P < 0.05).
175.40±13.60
628.30±10.67
51.40±3.07
270.04±7.29
0
100
200
300
400
500
600
700
% Inhibition
methanolic barberry extract m ethanolic berberine chloride preparation
acetic acid barberry extract acetic acid berberine chloride preparation
Fig. 3 Effect of the prepared extracts (methanolic and acetic acid) on hepatic -Glucosidase activity. Values represent the mean of three replicates ±
standard deviation (SD), significant difference detected at P < 0.05.
66
Bioscreening of barberry. El Sayed et al.
use of barberry extract as a natural antioxidant agent for
treatment of idiopathic male factor infertility as well as in
assisted reproductive technology (Tab l e 3 ).
CONCLUDING REMARKS
The data obtained support the hypothesis that the bioactive
ingredients of barberry have beneficial effects on sup-
pressing hepatic and seminal lipid peroxidation. Barberry
displaying such capacities may be used in treatment of
hepatic, cardiovascular, hyperglycemic and Alzheimer dis-
eases as well as idiopathic male factor infertility. Further
studies will be carried out to identify and characterize the
potential bioactive phytochemicals of barberry.
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60.08±3.30
62.50±8.83
68.75±8.8
0
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Hepatic t iss ue homoge nat e
% Inhibition
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72.58±0.38
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69.94±0.89
0
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Seminal plasma Seminal spermatozoa
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A
B
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... Herbal medicine has received great deal of attention for its cultural acceptability, better adaptability to human body, and less side effects. 4,5 Despite the fact that the discovery and processing of plant-derived medicinal products are associated with challenges such as limited access, successful identification of materials, and conservation of wild species, the natural products are still easily applicable, cheap, available, and less toxic. Different natural phytochemicals, as one of the several biologically active compounds, have been studied extensively in the field of cancer treatment. ...
... Herbal medicine has received great deal of attention for its cultural acceptability, better adaptability to human body, and less side effects. 4,5 Despite the fact that the discovery and processing of plant-derived medicinal products are associated with challenges such as limited access, successful identification of materials, and conservation of wild species, the natural products are still easily applicable, cheap, available, and less toxic. Different natural phytochemicals, as one of the several biologically active compounds, have been studied extensively in the field of cancer treatment. ...
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Cancer, even currently, is one of the main reasons for mortality and morbidity, worldwide. In recent years, a great deal of effort has been made to find efficient therapeutic strategies for cancer, however, particularly with regards to side effects and the possibility of complete remission. Berberine (BBR) is a nature-driven phytochemical component originated from different plant groups such as Berberis vulgaris, Berberis aquifolium, and Berberis aristata. BBR is a well-known nutraceutical because of its wide range of pharmacological activities including anti-inflammatory, antidiabetic, antibacterial, antiparasitic, antidiarrheal, antihypertensive, hypolipidemic, and fungicide. In addition, it exhibits inhibitory effects on multiple types of cancers. In this review, we have elaborated on the anticancer effects of BBR through the regulation of different molecular pathways such as: inducing apoptosis, autophagy, arresting cell cycle, and inhibiting metastasis and invasion.
... The World Health Organization (WHO) estimates that herbal medicine is the most common source for primary health care for 75-80% of the world's population, mainly in the developing countries, because of better cultural acceptability, better compatibility with the human body and fewer side effects (El-Sayed et al. 2011). In recent times, there is an increasing interest in discovering natural antioxidants, especially those of plant origin. ...
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Berberis vulgaris (barberry) is a plant belonging to the Berberidaceae family and its medicinal properties have been known since ancient times. In this study, we have evaluated the antioxidant activity of fruit, leaves, root bark, and branch bark extracts of B. vulgaris, depending on the habitat and maturity by five methods: 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity; 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) cation decolorization activity; total reducing power; cupric ion reducing antioxidant power; and the ferric ion reducing antioxidant power. Also, we determined the total phenolic and flavonoid contents. Of the analyzed extracts, the highest phenolic and flavonoid content was found in the extract of the fruit, 494 ± 2 µg GAE/mg dry extract weight and 2170 ± 4 µg RE/mg dry extract weight, respectively. Depending on the method used for the assay, the plant extracts show different antioxidant capacities but there is a certain pattern. All of the antioxidant assays have indicated the high antioxidant activity of B. vulgaris extracts. The extract of fruit stood out with the highest antioxidant activity while the bark of the roots of wild plants had the lowest activity. The study enhanced using chemometric analysis and cluster analysis was used to investigate the similarities between analyzed extracts.
... Previous studies have shown berberine as one of the main active compounds of B. vulgaris [43,44]. Berberine demonstrated antiplatelet aggregation potential through inhibition of TXA2 induced by ADP, AA, and collagen [45]. ...
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Coronary artery disease is the leading cause of mortality and morbidity worldwide. The pathogenesis is mainly due to atherosclerosis, plaque rupture, and platelet thrombus formation. The main risk factors for coronary artery disease include obesity, hypercholesterolemia, smoking, diabetes, and high blood pressure. As a part of disease management, treatment options using anticoagulant and antiplatelet drugs can be applied with addition to lipid-lowering medication. However, medicinal plants comprising antiatherothrombotic effects can be used as options to combat the disease rather than drug therapies with lesser adverse effects. Therefore, the haematological effect of Berberis vulgaris L. , Teucrium polium L., and Orthosiphon stamineus Benth extracts was studied using in vitro model to prevent and to treat coronary atherothrombotic disease. The aqueous, methanol, and polysaccharide extracts of B. vulgaris, T. polium, and O. stamineus, respectively, were studied for their anticoagulant and antiplatelet effect on human whole blood. Extracts were subjected to the prothrombin time (PT) and activated partial thromboplastin time (APTT) test for anticoagulant activity. The antiplatelet activity was investigated using an electrical impedance method. B. vulgaris aqueous extract (BVAE), B. vulgaris polysaccharide extract (BVPE), T. polium aqueous extract (TPAE), and T. polium polysaccharide extract (TPPE) significantly prolonged the coagulation time in a concentration-dependent manner ( p <0.05). The administration of BVAE demonstrated the most effective antiplatelet activity against platelet aggregation caused by arachidonic acid (AA) and collagen. These antiplatelet activities may correspond to the presence of higher total phenolic compound, which thus inhibit the platelet aggregation activity. In conclusion, these findings provide strong evidence on the antiatherothrombotic effect of BVAE and TPAE.
... Dissimilarities in phytochemical constituents could justify the difference in IC 50 values compared to our findings. In a previous study, the phytochemical quantification of the ethanolic extract of Berberis vulgaris has shown a total phenol content of 71% including flavonoids (4.9%) and alkaloids (2.6%) [19]. From this result we note that the total phenolic and flavonoid amounts differ from one species to another and from one region to another which could influence the effectiveness of the plant. ...
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According to the World Health Organization, leishmaniasis remains a major worldwide public health problem. The province of Sefrou located in the center of Morocco is a focus of cutaneous leishmaniasis. The present study aims at evaluating the antileishmanial potential of Berberis sp., Crataegus oxyacantha, Cistus salviifolius, Ephedra altissima and Lavandula dentata frequently used by the local population. Methanolic extracts were tested against the promastigote form of Leishmania tropica, Leishmania major and Leishmania infantum using tetrazolium-based colorimetric (MTT) assay. The total phenol and flavonoids content of all extracts were determined using the Folin–Ciocalteu reagent, aluminum chloride, and potassium acetate solutions respectively. The plant extracts exhibited antileishmanial activity with variability depending on the tested strain and the plant species compared to Glucantime® used as control (IC50 (the half maximal inhibitory concentration) > 1,000 μg/mL). The best inhibition was observed with Berberis sp., against Leishmania major (IC50 = 394.40 ± 3.02 μg/ml), and Ephedra altissima (reported for the first time) against Leishmania infantum (IC50 = 490.84 ± 3.15 μg/mL). Leishmania tropica has shown the same sensitivity behavior toward the five extracts (in average IC50 = 540 ± 11.20 μg/mL). The total phenolic content was higher for Crataegus oxyacantha and Cistus salviifolius (140.67 ± 3.17 μg eq Gallic Acid (GA)/ mg of Extract (E) and 133.83 ± 9.03 μg eq GA/mg of E respectively), while flavonoid was higher for Cistus salviifolius and Lavandula dentata (57.92 ± 2.46 μg eq Quercetin (Que)/ mg of Extract (E) and 41.53 ± 1.74 μg eq Que/mg of E). All the tested extracts present some promising aspects that may cure cutaneous leishmaniasis in the center of Morocco; further bioguided assays are needed to isolate the fractions and the bioactive molecule.
... The percentage of tannins is roughly similar in several species of Berberis; however, the root of B. microphylla contained a higher percentage of tannins than those described for B. aristata (0.6%), B. asiatica (1.7%), B. chitria (0.73%), and B. lyceum (0.96%) [35]. Moreover, the percentage of saponins is greater in B. microphylla than in B. vulgaris (0.3%) [36]. No significant differences were found in both extracts tested for these phytochemical groups. ...
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Berberis microphylla is a native species located in the Chilean-Argentinean Patagonia mainly used for medicinally purposes by indigenous from this region (Aónikenk, Selk’nam, Kawésqar) due to its astringent, antipyretic, analgesic, antibacterial, and antiviral properties. The phytochemical constituents of the root of Berberis microphylla were determined. The samples of ethanolic and methanolic extracts of B. microphylla root were tested perform phytochemical analyses and quantification of the most important components. The phytochemical screening of both extracts showed the presence of alkaloids, flavonoids, glycosides, cardiac glycosides, saponins, terpenes and tannins, which are known for their pharmacological importance. Quantification of the major phytochemicals groups showed that the ethanolic extract contains 3.9% of alkaloids, 0.46% flavonoids, 9.53% tannins and 3.60% saponins. Similarly, the methanolic extract contains 6.61% alkaloids, 0.41% flavonoids, 7.40% tannin and 1.43% saponins. In conclusion, this would be the first time reporting the presence of tannins, flavonoids and saponins in this plant. The medicinal properties of root of Berberis microphylla may be due to the presence secondary metabolites.
... The hexane fraction of the crude methanol extract was the most active fraction, with an IC50 value of 72 μg/mL from the shade dried plant material (Kolář et al. 2010). Berberine, the active compounds of B. vulgaris extract, showed a significant antioxidant abilitiy through a reduction in the concentration of an oxidizing agent having reactive species, especially on hydroxyl and DPPH radicals (El-Sayed et al. 2011) and Cannabisin G and (±)lyoniresinol were responsible for the antioxidant activity root bark extract (Tomoska et al. 2008). Recently, Hosseinihashemi et al. (2015) found that acetone extract of inner bark of B. vulgaris was the most active as an antioxidant agent at 98.61%, and the activity was higher than the value of vitamin C (93.03%) at the concentration of 0.16 mg/mL. ...
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Extracts from the woody stem of Berberis vulgaris were analyzed for their antioxidant capacity using the 2,2-dipheny-1-picrylhydrazyl (DPPH) method and compared with ascorbic acid (AA) and butylated hydroxytoluene (BHT). The most active extracts were analyzed for their chemical composition using gas chromatography-mass spectrometry. Acetone extract was found to be moderately active as an antioxidant agent at 47.6%, which was lower than the value of vitamin C (84.8%) at the concentration of 0.16 mg/mL. The major components identified in the acetone extract of the stem wood were 4-vinylguaiacol (75.5%) and D-mannoheptulose (8.8%). The dissolved water:methanol (1:1 v/v) partitioned from acetone extract afforded 12 fractions; among which, fraction F11 was found to have good antioxidant capacity (64.3%) at the concentration of 0.16 mg/mL. The major compounds identified in F11 were 3,4-dimethylthioquinoline (37.7%), methyl (1,2-dihydro-2-oxo-1-acenaphthylidene)acetate (19.9%), and α-cyclohexyl-3-furanmethanol (15.3%). It can be suggested that extracts of B. vulgaris wood may have a potential source of antioxidant compounds useful for new drugs from the natural basis.
... The inhibition of platelet aggregation is dose dependent from 10 to 30 mg/kg, giving the maximum inhibition of 52.5% [12]. There is also another report of inhibitory effects on AA metabolism and calcium influx, partial agonist activity on platelet 2-adrenoceptors using Berberis vulgaris extract [13]. ...
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Coronary atherothrombotic diseases such as coronary artery disease, peripheral vascular disease, cerebrovascular disease, and heart failure are the serious concerns of the thrombus formed in blood vessels. Anticoagulant and antiplatelet drugs are the cornerstones of the management of these diseases. To prevent the recurrence of these diseases, double antiplatelet drugs such as aspirin and clopidogrel has been the standard management in most hospitals. However, aspirin resistance and clopidogrel inefficient effects due to noncompliance with double drugs regimen can cause a sinister effect on patients. Medicinal plants serve as a greater resource for new medication and their potential currently became a topic of interest to the researchers all over the world. Traditionally, certain herbs have been used as a treatment for heart diseases but have been investigated for their antiplatelet properties. This current review explained few traditional antithrombotic herbals and their antiplatelet properties in vitro and in vivo and this is to be deeply discussed in further research.
... Previously, the hexane fraction of the crude methanol extract from the shade dried plant material was the most active fraction, with an IC50 of 72 μg/mL (Kolář et al. 2010), in the case of inhibition with acetylcholinesterase. Berberine and methanolic barberry crude extract showed a significant reduction in their antioxidant abilities and radicals scavenging effects, especially on hydroxyl and DPPH radicals (El-Sayed et al. 2011). Furthermore, B. vulgaris extract, as well as berberine chloride, inhibited DPPH oxidation in the range of 13 to 46% more than control level (Abd . ...
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Full-text available
Extracts from the inner stem bark of Berberis vulgaris were analyzed for their antioxidant activity using the 1,1-dipheny-2-picrylhydrazyl (DPPH) method and compared with ascorbic acid (AA) and butylated hydroxytoluene (BHT). The most active extracts were analyzed for their chemical composition using gas chromatography-mass spectrometry. Acetone extract was found to be the most active as an antioxidant agent at 98.61%, which was higher than the value of vitamin C (93.03%) at the concentration of 0.16 mg/mL. The major components identified in the acetone extract were tetracosanoic acid, methyl ester (26.36%), followed by phthalic acid, diisooctyl ester (20.93%), 1,2-bis(trimethylsiloxy) ethane (10.26%), and 1,2-benzendicarboxylic acid, diisononyl ester (8.70%). The dissolved water:methanol (1:1 v/v) partitioned from acetone extract afforded 12 fractions; among them, fraction F11 was found to have good antioxidant activity (95.41%) at the concentration of 0.16 mg/mL. The major compounds identified in F11 were N-methyl-4-(hydroxybenzyl)-1,2,3,4-tetrahydroisoquinoloine (28.82%), 9-α-hydroxy-17β-(trimethylsilyl-oxy)-4-anderostene-3-methyloxime (13.97%), ribitol, pentaacetate (9.76%), 1-methyl-4-[4,5-dihydroxyphenyl]-hexahydropyridine (6.83%), and 2-ethylacridine (4.77%).
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Common barberry, or Berberis vulgaris (Berberidaceae), has been shown to possess multiple pharmacological activities. The present study evaluated the relaxant effect of a hydroalcoholic extract of B. vulgaris on rat tracheal smooth muscle (TSM) as well as possible molecular mechanisms. TSM samples were stimulated by 10 μM methacholine or 60 mM potassium chloride (KCl), and the effects of cumulative concentrations of the extract (0.1, 0.4, 1.6, 6.5 mg/mL) and of theophylline (0.2, 0.4, 0.6 and 0.8 mM) were examined. To assess the possible mechanism(s) of the plant relaxant effect, this effect was also examined on tissue incubated with atropine, chlorpheniramine, propranolol, diltiazem, glibenclamide, indomethacin, ω-nitro-L-arginine methyl ester (L-NAME) and papaverine. The results showed concentration-dependent relaxant effects of B. vulgaris on non-incubated TSM contracted by KCl and methacholine (P < 0.05 to P < 0.001). There was no significant difference in the relaxant effects of B. vulgaris between non-incubated tissue and tissue incubated with chlorpheniramine, propranolol, indomethacin, diltiazem, glibenclamide or papaverine. However, the relaxant effects of 1.6 and 6.5 mg/mL of B. vulgaris on tissue incubated with L-NAME and of 6.5 mg/mL of the extract on tissue incubated with atropine were significantly lower than on non-incubated tissue (P < 0.05). The EC50 value of B. vulgaris on tissue incubated with chlorpheniramine was significantly higher than the non-incubated TSM (P < 0.05). A relatively effective relaxant effect of B. vulgaris comparable to that of theophylline was shown. Muscarinic receptor blockade and nitric oxide production have been suggested as possible mechanisms for the relaxant effect.
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SUMMARY The aim of the present study was to evaluate traditional antidiabetic folklore claim of Berberis lycium Royle (BlR). Hypoglycemic effect of powdered root bark of BlR (250, 500 mg/kg body weight) was evaluated in both normal and diabetic rabbits. Gliclazide was used as positive control. Antidiabetic effects of different extracts were also determined. Hypoglycemic activity of water extract showing maximal effect was compared with and without different doses of insulin. Phytochemical tests were carried out on water extract. Both doses of crude drug significantly (P
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The widespread use of medicinal plants for health purposes has increased dramatically due to their great importance to public health. In this study, the levels of phenolic, flavonoid, β-carotene and lycopene compounds of Anastatica hierochuntica and Hyphaene thebaica were determined. The plant extracts were evaluated for their antioxidant activities using various antioxidant methodologies: (i) scavenging of free radicals using 2, 2-diphenyl-1-picrylhydrazyl, (ii) metal ion chelating capacity, and (iii) scavenging of superoxide anion radical. The antimicrobial activity of both plant extracts was evaluated against a panel of microorganisms using the agar disc diffusion method. The total phenolic content (51.97 and 64.9 mg/g dry weight in A. hierochuntica and H. thebaica, respectively) was significantly (p � 0.05) different. The antioxidant activity increased with an increase in concentration. The plant extracts were more active against Gram-positive bacteria than Gram-negative bacteria. Also, the antimicrobial activity of H. thebaica was higher than that of A. hierochuntica methanolic extracts. This study reveals that the consumption of these plants would exert several beneficial effects by virtue of their antioxidant and antimicrobial activities.
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Berberis vulgaris is widely spread on the Balkan Peninsula. There are few studies on its effect on the cardiovascular system. The method of Litchfield and Wilcoxon was used to determine LD50 per os of B. vulgaris on mice. B. vulgaris has LD50 = 2.6 ± 0.22 g/kg b.w. dry drug of mice. After venous application on 10% infuse of the plant was observed a long time hypotensive effect - 62.6% ± 6.9 versus the initial arterial pressure, considered as (taken as) 100%. The hypertensive effect of Barium dichloridum is eliminated by B. vulgaris (10 mg/kg b.w., i.v.) - arterial pressure is reduced respectively from 138±14 mmHg to 68±8 mmHg (p < 0.001). B. vulgaris is moderately toxic. It contains biologically active agents (substances). Long time hypotensive effect results after venous application, evidence of its direct myotropic effect.
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Berberine is a well-known plant alkaloid with a long history of medicinal use in Ayurvedic, Chinese, and South Asian traditional medicine. It can be found in the roots, rhizomes, and the bark of a number of plants. Plant extracts and decoctions involving berberine have demonstrated significant antimicrobial activity against a variety of organisms, intestinal parasite infections, and ocular trachoma infections. Positive action has been recorded against hypertension, tumors, inflammation, and HIV. It also has anti-protozoal, chloretic, cholagogue, cardiotonic, anti-cholinergic, anti-arrhythmic effects, and anti-platelet aggregation. This original review of berberine outlines its physiological effects.
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Added tocopherol was effective both in inhibiting lipide peroxidation and stabilizing DPNH-cytochrome c reductase in isolated mitochondria. Vitamin E-deficient rabbits had livers showing in vivo lipide peroxidation and increased lability of their isolated mitochondria. This liver damage may be a primary cause of other vitamin E-deficiency syndromes.
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Cardiac glycosides are used clinically to increase contractile force in pa- tients with cardiac disorders. Their mechanism of action is well established and involves inhibition of the plasma membrane Na1/K1-ATPase, leading to alterations in intracellular K1 and Ca21 levels. Here, we report that the cardiac glycosides oleandrin, ouabain, and digoxin induce apoptosis in an- drogen-independent human prostate cancer cell lines in vitro. Cell death was associated with early release of cytochrome c from mitochondria, followed by proteolytic processing of caspases 8 and 3. Oleandrin also promoted caspase activation, detected by cleavage poly(ADP-ribose) polymerase and hydrolysis of a peptide substrate (DEVD-pNA). Comparison of the rates of apoptosis in poorly metastatic PC3 M-Pro4 and highly metastatic PC3 M-LN4 subclones demonstrated that cell death was delayed in the latter because of a delay in mitochondrial cytochrome c release. Single-cell imaging of intracellular Ca 21 fluxes demonstrated that the proapoptotic effects of the cardiac glycosides were linked to their abilities to induce sustained Ca21 increases in the cells. Our results define a novel activity for cardiac glycosides that could prove relevant to the treatment of metastatic prostate cancer.
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We found alpha-glucosidase inhibitory (alpha-GI) effect of metal ions and their complexes which showed the high blood glucose lowering effect in diabetic model animals. The Cu(II) ion and its complexes showed strong alpha-GI activity greater than clinically used acarbose in in vitro studies. Furthermore, in in vivo experiments, alpha-GI action was newly discovered in normal ddy mice. These results suggested that one of action mechanisms of the anti-diabetic metal ions and complexes is related to the alpha-GI effects.