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A review on advancements in ethnomedicine and phytochemistry of Tribulus terrestris-a plant with multiple health benefits

Authors:
  • Department of Pharmacy

Abstract

Tribulus terrestris (TT) Linn. is an annual medicinal plant that belongs to the Zygophyllaceae family. TT has been mainly planted in the subtropical regions of Pakistan, India, China, Mexico, Spain and South America. It has been extensively used to improve physical performance and sexual functions in men. All parts of the plant have been used as a traditional medicine in various regions of the world. The plant contains phytochemicals like flavonoids and saponins that possess pharmacological activities. As an example, the saponins present in TT possess anti-proliferative and anti-tumor function. The fruit of the plant is used for the treatment of abdominal and urogenital infections. The present study aims to summarize the pharmacological, traditional, medicinal and therapeutic potential of TT.
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REVIEW PAPER OPEN ACCESS
A review on advancements in ethnomedicine and
phytochemistry of
Tribulus terrestris
- a plant with multiple
health benefits
Farooq Azam1, Samia Munier1, Maliha Batool2, Bashir Ahmad3, Ghazanfar Abbas4*
1Institute of Pharmacy, Physiology and Pharmacology, University of Agriculture, Faisalabad,
Pakistan
2Department of Veterinary Pathobiology, Texas A&M University, College Station, Texas, United
States
3Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan
4Institute of Microbiology, University of Agriculture, Faisalabad, Pakistan
Key words: Tribulus terrestris, Ethnomedicine, Traditional uses.
http://dx.doi.org/10.12692/ijb/14.1.21-37
Abstract
Tribulus terrestris (TT) Linn. is an annual medicinal plant that belongs to the Zygophyllaceae family. TT has
been mainly planted in the subtropical regions of Pakistan, India, China, Mexico, Spain and South America. It
has been extensively used to improve physical performance and sexual functions in men. All parts of the plant
have been used as a traditional medicine in various regions of the world. The plant contains phytochemicals like
flavonoids and saponins that possess pharmacological activities. As an example, the saponins present in TT
possess anti-proliferative and anti-tumor function. The fruit of the plant is used for the treatment of abdominal
and urogenital infections. The present study aims to summarize the pharmacological, traditional, medicinal and
therapeutic potential of TT.
* Corresponding Author: Ghazanfar Abbas dr.ghazanfaruaf@gmail.com
International Journal of Biosciences | IJB |
ISSN: 2220-6655 (Print), 2222-5234 (Online)
http://www.innspub.net
Vol. 14, No. 1, p. 21-37, 2019
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2019
Introduction
The traditional medicine has been popular among the
majority of world, despite of great progress in modern
medicine. According to the World Health
Organization (WHO), 80% of the world population
relies on conventional medications for primary health
care and a major portion of the conventional
treatments incorporate plant extracts or their
dynamic constituents.
Since old times ,the traditional medicinal plants have
been used for the common well-being as well as for
treatment of infections (Shinwari et al., 2011).
Approximately 35,000 of plant breeds has been
utilized by humans for therapeutic purposes.
Tribulus terrestris L., member of family
Zygophyllaceae, locally named as Bakhra (Hussain et
al., 2010), Bhakra Bakhro (Qureshi et al., 2011),
konda (in Pashto) in Pakistan and Gokshur or
Gokharu (Chhatre et al., 2014) in India, AlQutub and
Qutiba in Iraq (Al-Yaweret al., 2008), Dagunro,
Dareisa (Yoruba), Tisadu, Hanathakama (Hausa),
Kaije (Kanuri) in Nigeria (Afolayan et al., 2009),
usually familiar as puncture vine, goat head, devil’s
horn and yellow vine.
Latin title Tribulus initially implied the caltrop (a
spiky weapon). The Greek word, τπίβολορ (Angelova
et al., 2013), which means 'water-chestnut', in Latin it
is interpreted as tribulos(Al-Bayati & Al-Mola, 2008).
TT is broadly dispersed in tropical, sub-tropical and
mellow calm districts. Tribulus consists of 25 species
out of which many are considered harmful weeds.
This is because the sharp edges of tribulus fruits pose
a risk, to grazing creatures (Hashim et al., 2014).
Taxonomical classification
TT belongs to kingdom Plantae, division
Phanerogams and subdivision Angiospermae. Its
class is Dicotyledonae, subclass Polypetalae, series
Disciflorae having order Giraniales, family
Zygophyllaceae, genus Tribulus and species terrestris
Linn. (Chhatre et al., 2014).
Botanical description
TT is a little plush, bushy and flat or horizontal herb.
At early stage of development, the root of TT is slim,
stringy, round, hollow and light brown in color. The
stem length is about 2 meters long, leaves are inverse
and brief approximately 1.25cm in length. Fruits
contain rough projections and are wooded around 1
cm in breadth which possesses spikes about 6 mm
long. It has 2 unequal sets of spines. The wooded star-
shaped arrangement known as carpels of about 5-7
mm in length and 5-6 mm in width encased seeds. In
every carpel, there are 5 seeds and every seed is 1.5-3
mm long and yellow in color. Cleared upon evaluation
that every plant possesses around 2000 seeds. TT is
described by small (8-15 mm diameter) yellow petal
flowers and thorny fruits. TT is bitter in taste
(Perveenet al., 2007; Zadehet al.2013;Hashim et al.,
2014).
Habitat
TT is a local plant of tropical locales of Southern,
Western and Eastern Asia, Southern Europe,
Australia, and Africa (Al-Ali et al., 2003). TT
massively develops in moderately hot dry tropical
zone everywhere in the world. The plant requires
good health and light finished land for development.
Broadly it is found in developed crops, gardens,
dismissed zone, overgrazed meadows and roadsides
(Hashim et al., 2014).
Chemical constituents
TT is a valuable herb frequently used in natural
medication and is found in different parts of the
world. Furostanol and spirostanol saponins of
chlorogenin, diosgenin, gitogenin, hecogenin,
tigogenin, neogitogenin, neotigogenin, ruscogenin,
and neohecogenin and sarsasapogenin sorts are
chiefly found in TT. Four types of sulphated saponins
are also isolated from TT (Kostova et al., 2005).
TT consists of alkaloids, saponins, flavonoids,
steroids, estradiol, cinammic acid amides and
lignanamides (Bourke et al., 1992; Renet al., 1994; Li
et al.,1998). The compounds present in the
methanolic extracts of TT are inositol, palmitic acid,
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estradiol, linoleic acid, stearic acid and beta-sitosterol
and these were identified by gas-chromatography and
mass spectrometry (GC-MS) analysis (Abirami et al.,
2011).
TT flavonoids are chiefly derived from kaempferol,
isorhamnetin andquercetin. Quercetin, isoquercitrin,
quercetin-3-O-gent, quercetin-3-O-rha-gent,
quercetin-3-O-gent-7-O-glu and rutin, are flavonoids
having basic parent structure of quercetin(QU et al.,,
2007; Alavia et al., 2008). Isorhamnetin,
isorhamnetin-3-O-gent, isorhamnetin-3-O-glu,
isorhamnetin3, 7-di-O-glu,isorhamnetin-3-O-gent-7-
O-glu, isorhamnetin-3-O-p-coumarylglu,
isorhamnetin-3-O-gent-7-O-glu, and isorhamnetin-3-
O-rutinoside are flavonoids with basic parent
structure of isorhamnetin(Kostovaet al., 2002; Sunet
al., 2002; Zhu et al., 2017). Kaempferol, kaempferol-
3-O-gent, kaempferol-3-O-glu, kaempferol-3-O-gent-
7-O-glu, kaempferol-3-O-rutinoside and tribuloside
contain flavonoids containing basic parent structure
of kaempferol (Alavia et al., 2008; Su et al., 2009).
Tribulusin A, tribulusamide C, tribulusterine,
terrestriamide, harman, harmine , harmmol, N-trans-
caffeoylyramine, N-transcoumaroyltyramine, are the
main alkaloids isolated from fruits, leaves and stems
of TT (Ren et al., 1994; Alavia et al., 2008).
TT contains some additional ingredients like amino
acids, organic acids and many other substances.
Amino acids include alanine and threonine (Zhu et
al., 2017). TT also contains 4-ketopinoresinol (Lv et
al., 2008), coumarin, physcion, emodin and uracil
nucleic acid (Liu et al., 2003, Zhu et al., 2017).
Organic acids include vanillic acid, benzoic acid, 2-
methyl benzoic acid (Zhu et al., 2017), palmitic acid
monoglyceride, succinic acid, tribulus acid,
docosanoic acid, (Chenet al.,2000) andferulic acid
(Lv et al., 2008).
Phytochemistry and Pharmacology
Furostanol and spirostanol saponins are studied as
most valuable chemicals of TT. Steroidal saponins
have been separated from the plant with the
assistance of splash reagent are 108, out of which 50
types are furostane saponins and 58 types are
spirostane saponins. Due to the presence of
anisaldehyde reagent, both furostanol and spirostanol
saponins provide yellow stains on thin layer
chromatography (TLC). In contrast, with Ehrlich’s
reagent, furostaol saponins give red color (Cai et al.,
2001). The aerial portion of TT contains steroidal
saponins, such as protodioscin and protogracilin.
These are primary components of the plant with
unique biological activities (Gautam et al., 2018;
Obreshkova et al., 1998; De-Combarieu et al., 2003).
Saponins showed extremely low absorption within the
brief wavelength range so high-performance liquid
chromatography (HPLC) is preferred over ultraviolet
(UV) spectroscopy (Ganzera et al., 2001). Different
chromatographic methods utilized for partition of a
saponin blend into individual components that
includes thin layer chromatography on typical and
reversed-phase i.e. HPLC in one or two-dimensional
modes (Mutilate et al., 1998). HPLC on reversed-
phase columns is the foremost effective and most
regularly utilized method. With the advancement of
later unused procedure for discovery with evaporative
light scattering detector (ELSD) gives an important
implies for division and confinement of saponins
(Kostovaet al.,, 2005).
Crude saponin fractions of TT were exposed to
column chromatography (CC) by silica gel along with
a slope CHCl3MeOHH2O. For pure saponins
production, a few fractions are at that point
chromatographed by column chromatography on gel
and medium pressure liquid chromatography (MPLC)
pre-packed column with MeOHH2O (Wu et al.,
1996). Saponin fractions chromatographed by micro
porous gum column (eluting with water, 50, 70 and
90% EtOH) and consequent silica gel column
chromatography (CHCl3-MeOH-H2O), MPLC (H2O
MeOH angle) and gel filtration on Sephadex G-25
with H2O (Xu et al., 2000).
The crude saponin fractions of TT was isolated by
exposure with evaporating light scattering (ELS),
HPLC through employing a reversed phase (RP-18)
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column and as mobile phase water-acetonitrile
gradient. Basic examination and partition of
furostanol saponins in extricates was done by
employing an acetonitrile and gradient of 0.1% formic
corrosive (v/v) in water (De Combarieu et al., 2003).
HPLC-ESI-MS (high-performance liquid
chromatography-electrospray ionization-mass
spectrometry) strategy for subjective investigation of
saponin blends was also utilized (Mulinacci et al.,
2003). On thin layer chromatography with Herlich’s
spray reagent furostanol saponins were effectively
found out through color response they showed,
reversed-phase and normal-phase silica gel column
chromatography were also utilized for unrefined
divisions of TT (Wang et al., 2009).
Traditional uses
Uses of this plant are traditionally opted by different
nations as TT is utilized as a folk medication for
diverse purposes and therapies. Previous studies
show sundry therapeutic worth of TT as a well-known
source to cure an assortment of distinctive infection
conditions in Greece, China, and India. TT is either
used as herb or as a primary component for the
propagation of many medications and for edible
supplements such as physical revival, treatment of
kidney problems, liver, immune system and
cardiovascular system(Tilwari et al., 2011).
Due to diversity of compounds extracted from this
plant, its uses are extended from local to systemic
illnesses. It is used as a folk medication for an
aesthetic stimulant, expanded muscle vigor, sexual
strength, aphrodisiac(Zheleva-Dimitrova et al., 2012;
Angelova et al., 2013), nutritive and in medications of
urinary diseases, cough and heart illnesses(Hashim et
al., 2014).In addition, It also has diuretic (Angelova et
al., 2013), , antiurolithic (Anandet al., 1994;
Shirfuleet al., 2011), immunomodulatory (Tilwari et
al., 2011), antidiabetic, absorption enhancing,
hypolipidemic (Samani et al., 2016),
hepatoprotective, analgesic, central nervous system,
cardio tonic, anti-inflammatory(Heidari et al., 2007;
Borran et al., 2017), antispasmodic, anticancer,
antibacterial (Gopinath et al., 2012), anthelmintic,
larvicidal, and anticariogenic activities (Chhatre et al.,
2014).
It is a magnificent herb demonstrated for its sundry
therapeutic activities which can be securely utilized
for sundry sicknesses (Fatima et al., 2014). Table 1
shows a vast range of therapeutic activities of
different parts of plant and the whole plant extract.
Sexual disorders
Steroidal saponins present in TT extract basically
include protodioscin, diosgenin, and dioscin
altogether enhance the testosterone levels and indeed
having an impact on estrogen, pregnenolone, and
progesterone to provoke sexual conduct (Adimoelja et
al., 1997). Protodioscin (5, 6-dihydroprotodioscin,
neoprotodioscin) (Martino-Andrade et al., 2010) is a
phytochemical agent categorized into steroidal
saponins and present mainly in aerial portion of TT
plant in various concentrations (Adimoeljaet al.,
2000). And clinical studies proved that it enhances
sexual desire and upgrade erection by the change of
protodioscin into dehydroepiandrosterone (DHEA)
(Fatima et al., 2014). Protodioscin also enhance
dehydroepiandrosterone, luteinizing hormone and
testosterone level. Dehydroepiandrosterone is a
potent form attain from testosterone that provokes
sexual desire, have a role in muscle expansion and red
blood cells manufacturing (Arsyad et al., 1996). To
treat infertility in males it increments the caliber of
dehydroepiandrosterone. In Europe and USA, various
formulations have been retailed that possess TT
extricates utilized, to enhance sexual desire, as a food
additive (De Combarieu et al., 2003, Mulinacci et al.,
2003) and for many other types of diseases (Hashim
et al., 2014).For a long period of time,TT is famous as
a routine medication deals with male infertility
because of the presence of protodioscin, a furostanol
saponin. Protodioscin have fortifying impact on
spermatogenesis by means of Luteinizing Hormone
(LH) invigorating the discharge of male hormone
testosterone (Gauthaman et al., 2002, Gauthaman et
al., 2008).By the utilization of TT extricates, there
was an increment in dihydrotestosterone,
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dehydroepiandrosterone and testosterone level that
regulate sex drive and play an important role in
amount and quality of sperms(Neychevet al.,2005).
Effect on erectile dysfunction (ED)
Male weakness or erectile dysfunction (ED) is
characterized as the failure of a man to attain and
keep up an erection adequate for commonly palatable
intimacy with his mate. To defeat the issue of erectile
dysfunction different common sexual enhancer
possibilities are favored (Xu et al., 2010).
Table 1. Useful activities/effects of different parts of Tribulus terrestris.
Part(s) of TT
Activity
Reference(s)
Plant dry extract
Anticancer
Pavin et al., 2018
Roots
Anti-cholestrolemic
(Fatima et al., 2014).
Leaves
Larvicidal
(Singh et al., 2008; Mitra et al., 2012; Zhu et al., 2017).
Leaves
Antidiabetic
(Amin et al., 2006).
Leaves and fruits
Anti-inflammatory
(Baburao et al., 2009; Borran et al., 2017).
Fruits
Aphrodisiac
(GamalEl Din et al., 2018, Singh et al., 2012).
Fruits
Antiurolithic
(Anand et al., 1994; Shirfule et al., 2011).
Fruits
Anti-cholinergic
(Fatima et al., 2014).
Fruits
Hypolipidemic
(Khan et al., 2011; Rahmathulla et al., 2013).
Fruits
Analgesic
(Heidari et al., 2007; Borran et al., 2017).
Fruits
Antiurolithic
(Anand et al., 1994; D. K. Sharma, 2017).
Fruits
Antioxidant
(Reshma et al., 2016; Borran et al., 2017).
Fruits
Learning and memory
(Prabhu et al., 2014).
Fruits
Against acute pancreatitis
(Borran et al., 2017).
Fruits and seeds
Diuretic
(Al-Ali et al., 2003; Chhatre et al., 2012).
Fruits and roots
Central nervous system
(Adaikan et al., 2000).
Fruits and stems
Cytotoxic
(Sun et al., 2003).
Fruits and leaves
Antifungal
(Al-Bayati & Al-Mola, 2008).
Fruits, stems, roots,
whole plant
Apoptosis inducer
(Basaiyye et al., 2018)
Fruits, stems, roots
Anti-cancerous
(Kostova et al., 2005; Manish et al., 2009; Kim et al., 2011).
Fruits, roots, stems
and leaves
Antimicrobial, Antibiotic
(Arulmozhi et al., 2018.Adaikan et al., 2000, Al-Bayati et al.,
2008; Baburao et al., 2009).
Whole plant
Neuropathic pain relieving
Gautam et al., 2018
Fruits, whole plant
Renoprotective effect
Jiang et al., 2018
Fruits, whole plant
Antihypertensive
(Phillips et al., 2006).
Aerial parts of plant
As food supplements
(De Combarieu et al., 2003).
Aerial parts of plant
Against acute kidney injury
(Najafi et al., 2014).
Aerial parts of plant
Erectile dysfunction
(Kalamegam et al.,2008).
Whole plant
Immunomodulatory
(Tilwari et al., 2011).
Whole plant
Anthelminthic
(Deepak et al., 2002).
Whole plant
Estrogenic
(Fatima et al., 2014).
Whole plant
Smooth & skeletal muscle
relaxant
(Fatima et al., 2014).
Whole plant
Anti-spasmodic
(Fatima et al., 2014).
The etiologies related with erectile dysfunction are
chronic medical conditions, psychosexual
components and a few ways of life. Conventional
treatment alternatives for erectile dysfunction include
the utilize of innate therapeutic plants
(phytotherapy), creatures (zootherapy), and other
worldliness, whereas nontraditional choices
incorporate the routine, standard practice such as
drug treatment, behavioral and mental counseling
(Afolayan et al., 2009).
In primates, rabbits and rats, hormonal impacts of TT
have been studied in order to evaluate its
effectiveness within the management of erectile
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2019
dysfunction. For this purpose, both acute and chronic
administration of TT at various concentrations was
given. In primates for acute study, TT extricates were
managed intravenously with a dosage of 7.5, 15 & 30
mg/kg. In rabbits and normal rats for chronic study,
TT extricates were managed orally with a dosage of
2.5, 5 & 10 mg/kg up to 8 weeks. Blood tests were
performed by using radioimmunoassay in order to
determine dihydrotestosterone (DHT),
dehydroepiandrosterone sulphate (DHEAS), and
testosterone (T) levels. It was found that DHT,
DHEAS, and T level increased significantly in both
acute and chronic administration of TT mainly due to
the presence of steroidal saponin protodioscin (Qi et
al., 2018, Kalamegam et al., 2008).
In another study, to assess TT impact for the
treatment of erectile dysfunction a placebo-controlled
study i.e. randomized and two fold blind was
performed previously containing thirty healthy men
of ≥ 40 years of age, which have been chosen from
100 patients complaining ED. Serum testosterone and
International Index of Erectile Function (IIEF-5) was
gotten after 30 days of study and before
randomization of groups. Two randomized groups of
15 patients each i.e. control group and study group
made. For thirty days both groups got 800 mg of TT
partitioned into two doses/day. Results showed an
advancement within the reaction of both groups
before getting the capsules, p-value = 0.0004,
compared with amount gotten within the first IIEF-5
(Santos et al., 2014).
TT administered for management of erectile
dysfunction as a “prompt therapy” worldwide. For 14
days TT dosage of 2 mg /kg body weight was given
daily to adult male mouse. For histochemical,
histological and morphometrical studies showed
significant increase in the number of spermatids,
sperms, spermatocytes, and interstitial cells while
thickness of seminiferous tubule was significantly
increased. It was concluded that TT extracts given to
adult male mouse involved in spermatogenesis (Al-
Yawer et al., 2008).
In a study on organ bath, corpus carvenosum muscles
showed a concentration-dependent relaxation impact
when applied TT extricates on it. When compared
with the control group in vivo study revealed that oral
administration of the TT extricates for one month
appeared a noteworthy concentration-dependent
increment in an intracavernous pressure (Doet al.,,
2013). Subsequently, TT extracts helpful in treating
erectile dysfunction here mechanism of action
involved was the response route of nitrous oxide or
nitric oxide synthase (NO/NOS) in carpus
carvenosum endothelium.
It locally infuses in adjoining smooth muscle cells and
ties with intracellular receptor i.e. guanylate cyclase
(Burnettet al., 1997).This will leads to the
conformational shift in turn enzyme activation occur
that convert guanosine triphosphate into cyclic
guanosine monophosphate (cGMP) that further
functioned by a cGMP-dependent protein kinase, in
this way corporal smooth muscle’s contractile
condition coordinate (Hedlund et al., 2000).
Spermatogenic effect
Interestingly the plant extract showed positive effect
on sperm formation in controlled studies. Effects of
TT extracts was examined on the primary
spermatocyte in rat. Researchers found that TT can
improve male reproductive system and can be used in
treatment of male infertility by affecting the testis
spermatocyte. Studies show that TT plant due to the
presence of saponins increases discharge of
luteotropic hormone in distinction to pituitary gland.
Luteotropic hormone is also a special stimulant for
production of testosterone and hence can improve
sexual functions through increased sperm production,
improved erectile function and increased libido.
Furostanol is one of the saponins in TT that have
stimulant effect on spermatogenesis and significantly
improves the quality and quantity ofsperm (Karimi et
al.,2011). TT greatly increases the number of
spermatids and sperms as well as increase in number
of interstitial (Leyding) cells due to the presence of
steroid saponin (Al-Yawer et al., 2008).
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Effect on testicular development
The effects of TT extracts was investigated on
testicular expansion and body weight of prepubescent
rats. In a study conducted on ten rats of two-week-
old, divided into 2 groups i.e. control group (A) and
experimental group (B). TT extracts were given orally
at a dosage of 70 mg/kg every day for twenty days to
group B. On 34th day rats were weighed and
sacrificed and their testes were removed for further
microscopic studies. Then independent-samples t-test
statistical analysis was done. Group B that received
TT extracts revealed a statistically significant increase
in the mean body (p 0.05). After examining the
histological slides of testes, it was revealed that by
treating with TT extracts seminiferous tubules
possess initial spermatids and showed significant
increment in it. The conclusion was that TT has a
complex provoking impact on germinative and
endocrine capacities of testicles(Bashiret al., 2009).
Aphrodisiac effect
The plant extracts have strong aphrodisiac effect. To
show up the aphrodisiac effect of TT, a study was
conducted on mature Sprague-Dawley rats, splitted
into five groups each group contain eight rats and
these groups were treated with distilled dihydrogen
monoxide include castrated and normal rats, treated
with TT include castrated rats at a dosage of 5 mg/kg
body weight one daily dose given orally, treated with
testosterone include castrated and normal rats at a
dosage of 10 mg/ kg body weight given
subcutaneously for two weeks. Rats include in the
castrated group showed a comprehensive decline in
sexual behavior parameters that are intromission
frequency (IM) and mount frequency (MF) while
showed increments in intromission latency (IL),
mount latency (ML), ejaculation latency (EL) and
post ejaculation interval (PEI). A significant
increment in intracavernous pressure (ICP) and
prostate weight was concluded (Gauthamanet
al.,2002).
Antihypertensive effect
The fruit extract of TT is known of have strong
antihypertensive effect. In as study 2K1C hypertensive
rats were examined through assessment of rotating
and local angiotensin-converting enzyme (ACE)
action in heart, lung, aorta, and kidney, it showed TT
have an antihypertensive mechanism. Rats were
divided into four groups; treated with TT,
hypertensive, sham and control groups. Firstly, rats
got hypertension through incision utilizing silver clip
on renal artery. After four weeks of incision TT fruits
lyophilized liquid extricates were given orally for four
weeks at a dosage of 10 mg/kg of body weight to 2K1C
hypertensive rats. Angiotensin-converting enzyme
action checked through high-performance liquid
chromatography (HPLC) and blood pressure through
the tail-cuff method. In 2K1C rats, systolic blood
pressure (SBP) was significantly raised in comparison
with control rats and angiotensin-converting enzyme
and serum action in kidney, lung, heart, and aorta
was significantly raised in comparison with normal
rats. Hypertensive rats treated with TT when
examined their systolic blood pressure was
significantly reduced and angiotensin-converting
enzyme action was also significantly reduced in
comparison with hypertensive rats.
It was concluded that TT showed significantly
reduced blood pressure in rats having renovascular
hypertension (Sharifi et al., 2003).
Aqueous and methanolic extracts of TT were used to
examine perfused mesenteric vascular bed and rat
blood pressure.
It was revealed that methanolic extricates are more
potent than aqueous extricates, these extricates
reduced blood pressure in dosage reliant pattern and
have an antihypertensive impact. Mechanism of
action involved in it was membrane hyperpolarization
and relaxation of arterial smooth muscles via nitric
oxide discharge(Phillips et al., 2006).
Antioxidant activity
TT herbaceous preparations showed antioxidant
activity that assessed by utilizing 2,2′-azino-bis
(3ethylbenzothiazoline-6-sulfonic acid) di-
ammonium salt-free radicals, 1,1-diphenyl-2-
picrylhydrazyl (DPPH),inhibition of lipid
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2019
peroxidation via ferric thiocyanate and ferric reducing
antioxidant power (FRAP). Overall quantity of
flavonoids and polyphenols were concluded utilizing
AlCl3 and Folin Chiocalteu reagent. It was concluded
that TT herbaceous preparations showed significant
antioxidant potential and restrained lipid
peroxidation. The overall tested models exhibited
powerful FRAP action and restrained lipid
peroxidation organization. The complete amount of
flavonoids ranged in between 0.36 % ± 0.004 % to
0.58 % ± 0.01 % while complete quantity of
polyphenols ranged in between 2.73 % ± 0.007 % to
3.17 % ± 0.008 %. Hence for that reason the entire
analysis helpful to clear the pharmacological potential
of TT plant (Zheleva-Dimitrova et al., 2012).
Antimicrobial activity
Methanolic extracts of the TT has in vitro
antibacterial effect against gram negative bacteria
including Klebsiella, E. coli, Pseudomonas
aeruginosa, and Proteus vulgaris and also against
gram positive bacteria i.e. Staphylococcus aureus. TT
exhibited significant effects across all bacteria
(Arulmozhi et al., 2018). The detailed action was due
to spirosaponins display within the herb(Ajaibet al.,
2010). TT fruit bodies were utilized in this think
about, to synthesized silver nanoparticles the dried
fruit body extricate was blended with silver nitrate.
The dynamic phytoconstituents found in TT were
responsible for the speedy reduction of silver particle
(Ag+) into metallic silver nanoparticles (Ag0).
Nuclear constrain magnifying lens, Transmission
Electron Magnifying instrument (TEM), UVvisible
spectroscopy, Fourier Transform Infrared (FTIR)
spectroscopy, X-ray diffraction (XRD) were presently
utilized for inspection of silver nanoparticles. The
round molded silver nanoparticles diameter was in
the range of 1628 nm. Moreover, the diffraction
design affirmed that a higher proportion of silver with
fine particles was formed. KirbyBauer strategy was
used to examine the antibacterial activity of
manufactured nanoparticles having clinically
restrained multi-drug safe microbes like Escherichia
coli, Pseudomonas aeruginosa, Bacillus subtilis,
Staphylococcus aureus and Streptococcus pyogens.
It was concluded that silver nanoparticles of TT plant
are less extravagant and fast and have wide utilization
in antibacterial therapy in cutting edge medicine
(Gopinath et al., 2012).
When TT methanolic extricates of various portions
including roots, stems, leaves, and fruits were
examined across bacteria including Pseudomonas
aeruginosa, Staphylococcus aureus, Escherichia coli,
Enterococcus faecalis and Pseudomonas aeruginosa
showed significant antibacterial action through
utilizing agar diffusion test and broth dilution test. It
was concluded that 4 mg/mL was the minimum
inhibitory concentration (MIC) value of methanolic
extricates of roots across Escherichia coli,
Staphylococcus aureus, and Enterococcus faecalis
while 2 mg/mL was across Pseudomonas aeruginosa.
2 mg/mL was the MIC of stems, leaves, and fruits
methanolic extricates of TT across each bacterium.
Agar diffusion test revealed that methanolic extricates
of all portion of TT showed significant antibacterial
action across each bacterium.
It was examined TT clearly showed antibacterial
action across extremely pervasive gram-negative
bacteria i.e. Escherichia coli in urinary tract diseases
(Kianbakht et al., 2003).
As a supplement used by athlete
Physical action is extensively recommended through
world health organization (WHO) for the reluctance
of their benefits, well performance and lifestyle
diseases; therefore, the nourishing supplements and
convenient diet is employed in addition with herbs
which can be effectively exhibited. TT as it enhances
the testosterone level and is furthermore available to
athletes and these are also convenient backups of the
banned fascinated drugs which are easily available in
retails in an abundant form or an alternate form of
supplements (Pokrywka et al., 2014).
The primary purpose is to enhance testosterone
androgenic and anabolic activity via stimulating
internal testosterone propagation. TT in athletes is
confidentially used (Maughanet al., 2007).
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Azam et al.
Int. J. Biosci.
2019
Anti-hyperglycemic and anti-hyperlipidemic effects
Hydro alcoholic extracts of TT showed a significant
antidiabetic activity. In a study for three months a
thousand mg/day hydro alcoholic extracts of TT
evaluated on lipid profile and serum glucose of
ninety- eight randomly allocated women with
diabetes mellitus.
In diabetic women, TT produced a significant total
cholesterol, low-density lipoprotein and blood glucose
decreasing impact in comparison to placebo
(p<0.05).TT group became substantially decreased in
comparison with placebo, whereas no extensive
impact changed was determined inside the high-
density lipoprotein levels and triglyceride levels
(Samani et al., 2016).
Conservational impact of TT against diabetes mellitus
(DM) was investigated. Rats were divided into 6
groups of 3 diabetic and 3 non-diabetic categories and
separately deal with glibenclamide, normal saline or
TT up to thirty days. First diabetic group was treated
with saline; second diabetic group was treated with
glibenclamide at dosage of 10mg/kg of body weight;
third diabetic group was treated with TT extracts at
dosage of 2g/kg of body weight, whereas the first,
second and third non-diabetic groups were treated
with saline solution, glibenclamide and TT extricates
all at once.
At the end of experiment for morphological and
biochemical investigation liver and serum specimens
were composed. Levels of creatinine, alanine
aminotransferase (ALT), reduced glutathione and
malondialdehyde (MDA) were analyzed in the liver.
It was concluded TT extracts fundamentally reduced
the serum creatinine and ALT levels in diabetic
groups, the reduced MDA level in liver in both groups
i.e. diabetic and non-diabetic (Amin et al., 2006).
In diabetic mice, methanolic extracts of TT showed a
fundamental reduction in blood glucose quantity at a
dosage of 50 mg/kg of body weight, after 4 and 6
hours of cure in comparison to diabetic mice i.e.
untreated. It was concluded that a significant
reduction in total cholesterol TC, serum triglycerides
TAG and low-density lipoprotein cholesterol LDL
revealed in comparison to untreated diabetic
mice(Hussainet al., 2009).
TT fruits aqueous extract was investigated as its
impact on cholesterol persuaded hyperlipidemia in
rats. It was concluded that aqueous extracts at dosage
of 580 mg/kg of body weight produced fundamental
decrease in different biochemical parameters likevery
low density lipoproteins (VLDL), low density
lipoproteins (LDL), alanine (AL),triglycerides (TG)
and increment in high density lipoproteins(HDL)
quantity as compared to aqueous extracts at dosage of
300 mg/kg of body weight (Khan et al., 2011).
Cytological and genetic effects
TT fruits aqueous extrication was utilized and a study
was conducted for determination of genetic impacts
via cytogenetic approaches and comet test. For
twenty-four hours TT extricates at a dosage of 10, 20,
40 and 80 mg/L utilized, a high dosage i.e. 80 mg/L
showed significant increment in comet cells. Due to
high dosage of TT and micronuclei, chromosomal
irregularity in a manner of stickiness, necrotic cells,
chromosomal gap, and fragmentation showed and
incremented(Qari et al., 2017).
Larvicidal and repellent effect
The larvicidal and repellent effect of the crude
ethanol, Crude acetone-petroleum ether and ethanol
extricate of TT leaves were used across mature
mosquito and third instar larvae to examine repellent
and larvicidal impacts. It was determined that Aedes
aegypti (Diptera: Culicidae) was a vector of dengue
fever. Hence concluded that petroleum ether extricate
was more competent having LC50 64.6A ppm after
that acetone extricates having LC50 173.2A ppm and
ethanolic extricates having LC50 376.4A ppm came in
a pattern. In comparison with commercially available
dosage form i.e. N, N-diethyl-3-methylbenzamide
(DEET) that possess 100% repellence action, it was
examined that at the same dosage the petroleum
ether extracts were the only extracts that showed
100% repellence action or astringent prevention in
30
Azam et al.
Int. J. Biosci.
2019
comparison to other extracts of TT plant(El-Sheikhet
al., 2016).
Anti-urolithiatic potential
To treat urinary ailment containing urolithiasis,
aqueous extricates of TT fruits were manufactured by
maceration then decoction was done for production of
a mother extracts that was ready to utilize for
polarity-occupied fractionations.
In kidney stones calcium oxalate can be a main sort of
precious stone that has been categorized into two
sorts; calcium oxalate dehydrate (COD) and calcium
oxalate monohydrate stones (COM). For years, in the
treatment of urinary stones plants got preference in
use.
The watery extracts of TT fruits considered to assess
the antiurolithiatic activity by using peculiar samples.
TT kidney stones inhibitory strength has been proved
in common initial kidney stones and nucleation. It
was concluded that for urolithiasis, an n-butanol
fragment in TT possess a higher amount of tannic
corrosive, diosgenin and quercetin showed defensive
scope instead of curative claim (Sharmaet al., 2017).
α-glucosidase inhibitory potential
Different studies were being conducted to illustrate
the α-glucosidase inhibitory potential of TT extricates
but the main component that is the cause of this
inhibition was still unknown but the studies
performed showed the inhibition mechanism. When
fragmentation of TT was done the idea was drawn
from this fragmentation that derivatives of three
cinnamic acid amide (13) were probably the effective
ingredients involved across α-glucosidase inhibition.
There was a leading structure in it that was N-trans-
coumaroyltyramine 1, exhibited significant inhibition
of α-glucosidase. In addition to it, cinnamic acid
amide A-ring possess hydroxyl group and α, β-
unsaturation carbonyl group that considered to have
discriminating functions in α-glucosidase inhibition.
When molecular sampling study did it showed that
interaction of hydrogen bond between inhibitors and
enzymes and π-π interaction was basically considered
for inhibitory activities (Song et al., 2016).
Analgesic effect
An investigation of methanolic extricates showed
analgesic activity in an albino mouse that was
confirmed through formalin and tail flick assay.
Intraperitoneal injection of percolated extracts was
given to mice at a dosage of 50,100 200,400 and 800
mg/kg of body weight.
It was concluded that at a dosage of 100 mg/kg of
body weight percolated extracts showed maximum
consequential analgesic activity(Heidari et al., 2007).
Urogenital effect
Aqueous extract of TT was found to have positive
impact on reproductive system. Aqueous extracts
content are phytoestrogen and its metabolites which
exert an estrogenic effect (Zadehet al., 2013;
Hajmohamadiet al., 2013).In a study of reproductive
system of mature albino mice, It was observed that
TT revealed significant increment in diameter of adult
follicles, the increment in luteinizing hormone and
follicle stimulating hormone levels, number of
growing follicles, endometrial glands diameter and
endometrial lining cells height increment in
luteinizing hormone and follicle stimulating hormone
levels, and reduction in estradiol level.
Cardiotonic activity
The saponins contents of TT extracts has been of
interest due to their pharmacological behavior for
heart diseases. Plant extract was used to treat
coronary heart disease (CHD). Saponins have
potential to dilate coronary artery and improve
coronary circulation. It was concluded in a clinical
study of 406 CHD patients that 82.3% was the
complete effective rate of remission of angina pectoris
(chest pain due to CHD) that was greater in
comparison to the control group i.e. 67.2%. Similarly,
52.7% was the efficacious rate of ECG improvement
that was also greater in comparison to the control
group i.e. 35.8%. It was concluded that it was one the
best medicine to treat angina pectoris without any
adverse reactions on renal functions, blood system
and hepatic functions (Wang et al., 1990).
31
Azam et al.
Int. J. Biosci.
2019
Conclusion
TT is an acknowledged plant utilized in indigenous
medication; in addition, folk medicine also claims
uses, especially as an aphrodisiac; analgesic,
antibiotic, antifungal, antioxidant, anti-inflammatory
activity and effective in urogenital system, nervous,
cardiovascular, and musculo-skeletal system.
Chemically, TT contains different biologically
effective phytochemicals containing alkaloids,
flavonoids, linoleic acid, palmitic acid, estradiol,
saponins, stearic acid, and Beta-sitosterol etc. TT is
very useful in various diseases for which there are
significant scientific reports and data available. Thus,
it is considered as an important herb with diverse
pharmacological activities, which is very beneficial to
mankind. Furthermore, Intensive research is required
to explore the hidden benefits of plant especially root
extracts.
References
Abirami P, Rajendran A. 2011. GC-MS Analysis of
Tribulus terrestris. Asian Journal of Plant Science and
Research 1, 13-16.
Adaikan P, Gauthaman K, Prasad R, Ng S.
2000. Proerectile pharmacological effects of Tribulus
terrestris extract on the rabbit corpus cavernosum.
Annals of the Academy of Medicine, Singapore 29,
22-26.
Afolayan AJ, Yakubu MT. 2009. Erectile
dysfunction management options in Nigeria.The
journal of sexual medicine 6, 1090-1102.
http://dx.doi.org/10.1111/j.1743-6109.2008.01064.x
Ajaib M, Khan Z, Khan N, Wahab M. 2010.
Ethnobotanical studies on useful shrubs of district
Kotli.Azad Jammu & Kashmir, Pakistan, Pakistan
Journal of Botany 42, 1407-1415.
Al-Ali M, Wahbi S, Twaij H, Al-Badr A. 2003.
Tribulus terrestris: preliminary study of its diuretic
and contractile effects and comparison with Zea
mays. Journal of Ethnopharmacology 85, 257-260.
http://dx.doi.org/10.1016/S0378-8741(03)00014-X
Al-Bayati FA, Al-Mola HF. 2008. Antibacterial
and antifungal activities of different parts of Tribulus
terrestris L. growing in Iraq. Journal of Zhejiang
University Science B9, 154-159.
http://dx.doi.org/10.1631/jzus.B0720251
Al-Yawer M, Hassan A, Haddad F, Al-Anee H,
Al-Khateeb E. 2008. Effects of AL-Qutub (Tribulus
terrestris) on the Spermatogenesis of the Mouse
Testis: Histological, Histochemical and
Morphometrical Studies. Journal of the Faculty of
Medicine Baghdad 50, 246-254.
Alavia SHR, Matin YM, Hadjiaghaee R, Ajani
Y. 2008. Flavonoid Glycosides from Tribulus
terrestris L. orientalis. Iranian Journal of
Pharmaceutical Sciences 4, 231-236.
Amin A, LotfyM, Shafiullah M, Adeghate E.
2006. The protective effect of Tribulus terrestris in
diabetes. Annals of the New York Academy of
Sciences 1084, 391-401.
http://dx.doi.org/10.1196/annals.1372.005
Anand R, Patnaik G, Kulshreshtha D, Dhawan
B. 1994. Activity of certain fractions of Tribulus
terrestris fruits against experimentally induced
urolithiasis in rats. Indian journal of experimental
biology 32, 548-552.
Angelova S, Gospodinova Z, Krasteva M,
Antov G, Lozanov V, Markov T, Bozhanov S,
Georgieva E, Mitev V. 2013. Antitumor activity of
Bulgarian herb Tribulus terrestris L. on human breast
cancer cells. Journal of BioScience & Biotechnology 2,
25-32.
Arulmozhi P, Vijayakumar S, Kumar T. 2018.
Phytochemical analysis and antimicrobial activity of
some medicinal plants against selected pathogenic
microorganisms. Microbial pathogenesis 123, 219-
226.
http://dx.doi.org/10.1016/j.micpath.2018.07.009
32
Azam et al.
Int. J. Biosci.
2019
Baburao B, Rajyalakshmi G, Venkatesham A,
Kiran G, Shyamsunder A, Gangarao B. 2009.
Anti-inflammatory and antimicrobial activities of
methanolic extract of Tribulus terrestris Linn
plant.International Journal of Chemical Sciences 7,
1867-1872.
http://dx.doi.org/10.1080/01443615.2018.1445706
Basaiyye SS, Naoghare PK, Kanojiya S, Bafana
A, Arrigo P, Krishnamurthi K, Sivanesan S.
2018. Molecular mechanism of apoptosis induction in
Jurkat E6-1 cells by Tribulus terrestris alkaloids
extract. Journal of traditional and complementary
medicine 8, 410-419.
http://dx.doi.org/10.1016/j.jtcme.2017.08.014
Bashir A, Tahir M, Samee W, Munir B. 2009.
Effects of Tribulus terrestris on testicular
development of immature albino rats.Biomedica 25,
63-68.
Bayati Zadeh J. 2013. Physiological and
pharmaceutical effects of Tribulus terrestris as a
multipurpose and valuable medicinal plant.
International Journal of Advanced Biological and
Biomedical Research 1, 556-562.
Borran M, Minaiyan M, Zolfaghari B,
Mahzouni P. 2017. Protective effect of Tribulus
terrestris fruit extract on cerulein-induced acute
pancreatitis in mice. Avicenna journal of
phytomedicine 7, 250.
Bourke C, Stevens G, CARRIGAN MJ. 1992.
Locomotor effects in sheep of alkaloids identified in
Australian Tribulus terrestris.Australian veterinary
journal 69, 163-165.
http://dx.doi.org/10.1111/j.1751-0813.1992.tb07502.x
Burnett AL. 1997. Nitric oxide in the penis:
physiology and pathology.The Journal of urology 157,
320-324.
http://dx.doi.org/10.1016/S0022-5347(01)65369-2
Cai L, Wu Y, Zhang J, Pei F, Xu Y, Xie S, Xu D.
2001. Steroidal saponins from Tribulus
terrestri.Planta medica 67, 196-198.
http://dx.doi.org/10.1055/s-2001-11650
Chen H, Chen Q, Xuan W. 2000. A new organic
acid from Tribulus terrestris. Academic Journal of
Second Military Medical University 11.
Chhatre S, Nesari T, Somani G, Kanchan D,
Sathaye S. 2014. Phytopharmacological overview of
Tribulus terrestris.Pharmacognosy reviews 8, 45-51.
http://dx.doi.org/10.4103/0973-7847.125530
Chhatre S, Nesari T, Somani G, Kenjale R,
Sathaye S. 2012. Comparative evaluation of diuretic
activity of different extracts of Tribulus terrestris
fruits in experimental animals. International Journal
of Research in Phytochemistry and Pharmacology 3,
129-133.
DeCombarieu E, Fuzzati N, Lovati M, Mercalli
E. 2003. Furostanol saponins from Tribulus
terrestris.Fitoterapia 74, 583-591.
http://dx.doi.org/10.1016/S0367-326X(03)00152-7
Deepak M, Dipankar G, Prashanth D, Asha M,
Amit A, Venkataraman B. 2002. Tribulosin and
β-sitosterol-D-glucoside, the anthelmintic principles
of Tribulus terrestris.Phytomedicine 9, 753-756.
http://dx.doi.org/10.1078/094471102321621395
Do J, Choi S, Choi J, Hyun JS. 2013. Effects and
mechanism of action of a Tribulus terrestris extract
on penile erection. Korean journal of urology 54, 183-
188.
http://dx.doi.org/10.4111/kju.2013.54.3.183
El-Sheikh TM, Al-Fifi ZI, Alabboud MA. 2016.
Larvicidal and repellent effect of some Tribulus
terrestris L.,(Zygophyllaceae) extracts against the
dengue fever mosquito, Aedes aegypti (Diptera:
Culicidae). Journal of Saudi Chemical Society 20, 13-
19.
http://dx.doi.org/10.1016/j.jscs.2012.05.009
33
Azam et al.
Int. J. Biosci.
2019
Ganzera M, Bedir E, Khan I. 2001.
Determination of steroidal saponins in Tribulus
terrestris by reversedphase highperformance liquid
chromatography and evaporative light scattering
detection. Journal of Pharmaceutical Sciences 90,
1752-1758.
http://dx.doi.org/10.1002/jps.1124
Gautam M, Ramanathan M. 2018. Saponins of
Tribulus terrestris attenuated neuropathic pain
induced with vincristine through central and
peripheral mechanism. Inflammopharmacology 1-12.
http://dx.doi.org/10.1007/s10787-018-0502-0
Gauthaman K, Adaikan P, Prasad R. 2002.
Aphrodisiac properties of Tribulus Terrestris extract
(Protodioscin) in normal and castrated rats.Life
sciences 71, 1385-1396.
http://dx.doi.org/10.1016/S0024-3205(02)01858-1
Gauthaman K, Ganesan AP. 2008. The hormonal
effects of Tribulus terrestris and its role in the
management of male erectile dysfunctionan
evaluation using primates, rabbit and
rat.Phytomedicine 15, 44-54.
http://dx.doi.org/10.1016/j.phymed.2007.11.011
Gopinath V, MubarakAli D, Priyadarshini S,
Priyadharsshini NM, Thajuddin N, Velusamy
P. 2012. Biosynthesis of silver nanoparticles from
Tribulus terrestris and its antimicrobial activity: a
novel biological approach,Colloids and Surfaces B.
Biointerfaces 96, 69-74.
http://dx.doi.org/10.1016/j.colsurfb.2012.03.023
Hajmohamadi S. 2013. Physiological and
pharmaceutical effects of tribulus terrestris as a
multipurpose and valuable medicinal plant.
International Journal of Advanced Biological and
Biomedical Research 1, 1289-1295.
Hashim S, Bakht T, Marwat KB, Jan A. 2014.
Medicinal properties, phyto-chemistry and
pharmacology of tribulus terrestris L.
(Zygophyllaceae). Pakistan Journal of Botany 46,
399-404.
Hedlund P, Aszódi A, Pfeifer A, Alm P,
Hofmann F, Ahmad M, Fässler R, Andersson
KE. 2000. Erectile dysfunction in cyclic GMP-
dependent kinase I-deficient mice. Proceedings of the
National Academy of Sciences 97, 2349-2354.
http://dx.doi.org/10.1073/pnas.030419997
Heidari M, Mehrabani M, Pardakhty A,
Khazaeli P, Zahedi M, Yakhchali M, Vahedian
M. 2007. The analgesic effect of Tribulus terrestris
extract and comparison of gastric ulcerogenicity of
the extract with indomethacine in animal
experiments. Annals of the New York Academy of
Sciences 1095, 418-427.
http://dx.doi.org/10.1196/annals.1397.045
Hussain AA, Mohammed AA, Ibrahim HH,
Abbas AH. 2009. Study the biological activities of
Tribulus terrestris extracts. World Acadamy of
Science Engineering and Technology 57, 433-435.
Hussain K, Nisar MF, Majeed A, Nawaz K,
Bhatti KH. 2010. Ethnomedicinal survey for
important plants of Jalalpur Jattan, district Gujrat,
Punjab, Pakistan.Ethnobotanical Leaflets 2010, 11.
Jiang YH, Jiang LY, Wu S, Jiang WJ, Xie L, Li
W, Yang CH. 2018. Proteomic analysis reveals the
renoprotective effect of Tribulus terrestris against
obesity-related glomerulopathy in rats. Biological and
Pharmaceutical Bulletin b18-00304.
http://dx.doi.org/10.1248/bpb.b18-00304
Karimi JH, Malekzadeh SS, Hoshmand F. 2011.
The effect of the Tribulus terrestris extract on
spermatogenesis in the rat. Journal of Jahrom
University of Medical Sciences 9, 8-13.
http://dx.doi.org/10.29252/jmj.9.4.8
Khan S, Kabir H, Jalees F, Asif M, Naquvi K.
2011. Antihyperlipidemic potential of fruits of
34
Azam et al.
Int. J. Biosci.
2019
Tribulus terrestris linn. Internnational Journal of
Biomedical Research 2, 98-101.
Kianbakht S, Jahaniani F. 2003. Evaluation of
antibacterial activity of Tribulus terrestris L. growing
in Iran.Iranian Journal of Pharmacology and
Therapeutics 2, 22-20.
Kim HJ, Kim JC, Min JS, Kim M-j, Kim JA,
Kor MH, Yoo HS, Ahn JK. 2011. Aqueous extract
of Tribulus terrestris Linn induces cell growth arrest
and apoptosis by down-regulating NF-κB signaling in
liver cancer cells.Journal of ethnopharmacology 136,
197-203.
http://dx.doi.org/10.1016/j.jep.2011.04.060
Kostova I, Dinchev D. 2005. Saponins in Tribulus
terrestrischemistry and bioactivity.Phytochemistry
reviews 4, 111-137.
http://dx.doi.org/10.1007/s11101-005-2833-x
Kostov I, Dinchev D, Rentsch GH, Dimitrov V,
Ivanova A. 2002. Two new sulfated furostanol
saponins from Tribulus terrestris. Zeitschrift für
Naturforschung C 57, 33-38.
http://dx.doi.org/10.1515/znc-2002-1-206
Li JX, Shi Q, Xiong Q-B, Prasain JK, Tezuka Y,
Hareyama T, Tanaka K, Namba T, Kadota S.
1998. Tribulusamide A and B, new hepatoprotective
lignanamides from the fruits of Tribulus terrestris:
indications of cytoprotective activity in murine
hepatocyte culture.Planta medica 64, 628-631.
http://dx.doi.org/10.1055/s-2006-957535
Lubna FM, Arshiya SM, Saad AM, Shabiya SM.
2014. Pharmacological activities of Tribulus terrestris.
World Journal of Pharmacy and Pharmaceutical
Sciences 4, 136-150.
Manish K, Meenaksh P, Ravindra S, Ashok K.
2009. Evaluation of radiomodulatory influence of
Tribulus terrestris root extract against gamma
radiation: hematological, biochemical and cytogenetic
alterations in Swiss albino mice.Pharmacologyonline
1, 1214-1228.
Maughan RJ, Depiesse F, Geyer H. 2007. The
use of dietary supplements by athletes.Journal of
sports sciences 22, 95-113.
http://dx.doi.org/10.1080/0264041031000140581
Mitra N, Mohammad-Mehdi D, Reza ZM. 2012.
Tribulus Terrestris L.(Zygophyllaceae) Flavonoid
Compounds. International Journal of Modern Botany
2, 35-39.
http://dx.doi.org/10.5923/j.ijmb.20120203.01
Najafi H, Firouzifar MR, Shafaat O, Ashtiyani
SC, Hosseini N. 2014. Protective effects of Tribulus
terrestris L extract against acute kidney injury
induced by reperfusion injury in rats. Iranian journal
of kidney diseases 8, 292.
Neychev VK, Mitev VI. 2015.Pro-sexual and
androgen enhancing effects of Tribulus terrestris
L.:Fact or fiction. Journal of ethnopharmacology 179,
345-355.
http://dx.doi.org/10.1016/j.jep.2015.12.055
Obreshkova D, Pangarova T, Mitkov S,
Dinchev D. 1998. Comparative analytical
investigation of Tribulus terrestris
preparations.Farmacija 45, 10-12.
Pavin NF, Izaguirry AP, Soares MB, Spiazzi
CC, Mendez ASL, Leivas FG, Cibin FWS. 2018.
Tribulus terrestris Protects against Male
Reproductive Damage Induced by Cyclophosphamide
in Mice. Oxidative medicine and cellular longevity
2018.
http://dx.doi.org/10.1155/2018/5758191
Perveen A, Abid R, Fatima R. 2007. Stomatal
types of some dicots within flora of Karachi,
Pakistan.Pakistan Journal of Botany 39, 1017.
Phillips OA, Mathew KT, Oriowo MA. 2006.
Antihypertensive and vasodilator effects of
35
Azam et al.
Int. J. Biosci.
2019
methanolic and aqueous extracts of Tribulus
terrestris in rats.Journal of ethnopharmacology 104,
351-355.
http://dx.doi.org/10.1016/j.jep.2005.09.027
Pokrywka A, Obmiński Z, Malczewska-
Lenczowska J, Fijatek Z, Turek-Lepa E,
Grucza R. 2014. Insights into supplements with
Tribulus terrestris used by athletes.Journal of human
kinetics 41, 99-105.
http://dx.doi.org/10.2478/hukin-2014-0037.
Prabhu N, Hadigal S. 2014. Effect of Tribulus
terrestris on learning and memory in wistar
rats.journal of Pharmacognosy and Phytochemistry 6,
68-71.
http://dx.doi.org/10.5530/pj.2014.4.10
Qari SH, El-Assouli S. 2017. Evaluation of
cytological and genetic effects of Tribulus terrestris
fruit aqueous extract on cultured human
lymphocytes. Saudi Journal of Biological Sciences.
http://dx.doi.org/0.1016/j.sjbs.2017.01.012.
Qi P, Zheng Y, Shen Y, Wang J, Bi Q, Feng R,
Wu W. 2018. Characterization and discrimination of
steroidal saponins in Tribulus terrestris L. and its
three different aerial parts by Cheimical profiling with
chemometrics analysis. Journal of separation science.
http://dx.doi.org/10.1002/jssc.201800513
QU NN, YANG SS. 2007. Extraction and
Determination of Chemical Constituents of
Flavonides in Tribulus terrestris L.Journal of
Liaoning University of Traditional Chinese Medicine
3, 122.
Qureshi R, Maqsood M, Arshad M, Chaudhry
AK. 2011. Ethnomedicinal uses of plants by the
people of Kadhi areas of Khushab, Punjab, Pakistan.
Pakistan Journal of Botany 43, 121-133.
Rahmathulla S. 2013. Effect of Tribulus terrestris
fruit aqueous extract on hyperlipidaemia and
maintenance of liver architecture in isoproterenol-
induced myocardial infarction in rats. International
Journal of Pharma and Bio Sciences 4, 983-992.
http://dx.doi.org/10.1.1.432.3509
Ren Y, Chen H, Yang G, Zhu H. 1994. Isolation
and identification of a new derivative of cinnamic
amide from Tribulus terrestris.Acta Pharmaceutica
Sinica 29, 206.
Reshma P, Sainu NS, Mathew AK, Raghu K.
2016. Mitochondrial dysfunction in H9c2 cells during
ischemia and amelioration with Tribulus terrestris L.
Life sciences 152, 220-230.
http://dx.doi.org/10.1016/j.lfs.2016.03.055
Samani NB, Jokar A, Soveid M, HeydariM,
Mosavat SH. 2016. Efficacy of Tribulus terrestris
extract on the serum glucose and lipids of women
with diabetes mellitus. Iranian journal of medical
sciences 41, S5.
Santos JC, Reis L, Destro-Saade R, Luiza-Reis
A, Fregonesi A. 2014. Tribulus terrestris versus
placebo in the treatment of erectile dysfunction: a
prospective, randomized, double-blind study. Actas
Urológicas Españolas (English Edition) 38, 244-248.
http://dx.doi.org/10.1016/j.acuroe.2014.03.009
Sharifi AM, Darabi R, Akbarloo N. 2003. Study
of antihypertensive mechanism of Tribulus terrestris
in 2K1C hypertensive rat.Journal of Life Sciences 73,
2963-2971.
http://dx.doi.org/10.1016/j.lfs.2003.04.002
Sharma DK. 2017. Enumerations on phytochemical
and pharmacological properties of tribulus terrestris
LINN: Indian Viagra. Asian Journal of Science and
Technology 8, 6462-6267.
Sharma I, Khan W, Ahmad S. 2017. In vitro and
ex vivo approach for anti-urolithiatic potential of
bioactive fractions of gokhru with simultaneous
HPLC analysis of six major metabolites and their
exploration in rat plasma.Pharmaceutical biology 55,
701-711.
36
Azam et al.
Int. J. Biosci.
2019
http://dx.doi.org/10.1080/13880209.2016.1266671
Shinwari ZK, Qaiser M. 2011. Efforts on
conservation and sustainable use of medicinal plants
of Pakistan.Pakistan Journal of botany 43, 5-10.
Shirfule A, Sangamwar A, Khobragade C. 2011.
Exploring glycolate oxidase (GOX) as an antiurolithic
drug target: Molecular modeling and in vitro inhibitor
study. International journal of biological
macromolecules 49, 62-70.
http://dx.doi.org/10.1016/j.ijbiomac.2011.03.016
Singh S, Nair V, Gupta YK. 2012. Evaluation of
the aphrodisiac activity of Tribulus terrestris Linn. in
sexually sluggish male albino rats. Journal of
pharmacology & pharmacotherapeutics 3, 43.
http://dx.doi.org/10.4103/0976-500X.92512
Singh S, Raghavendra K, Singh R, Mohanty S,
Dash A. 2008. Evaluation of Tribulus terrestris Linn
(Zygophyllaceae) acetone extract for larvicidal and
repellence activity against mosquito vectors. The
Journal of communicable diseases 40, 255-261.
Song YH, Kim DW, Curtis-Long MJ, Park C,
Son M, Kim JY, Yuk HJ, Lee KW, Park KH.
2016. Cinnamic acid amides from Tribulus terrestris
displaying uncompetitive α-glucosidase inhibition.
European journal of medicinal chemistry 114, 201-
208.
http://dx.doi.org/10.1016/j.ejmech.2016.02.044
Su L, Feng SG, Qiao L, Zhou YZ, Yang RP, Pei
YH. 2009. Two new steroidal saponins from Tribulus
terrestris.Journal of Asian natural products research
11, 38-43.
http://dx.doi.org/10.1016/j.steroids.2008.12.008
Sun B, Qu W, Bai Z. 2003. The inhibitory effect of
saponins from Tribulus terrestris on Bcap-37 breast
cancer cell line in vitro.Zhong yao cai Zhongyaocai
Journal of Chinese medicinal materials 26, 104-106.
Sun W, Gao J, Tu G, Guo Z, Zhang Y. 2002. A
new steroidal saponin from Tribulus terrestris
Linn.Natural Product Letters 16, 243-247.
http://dx.doi.org/10.1080/10575630290020541
Tharakan B, Manyam BV. 2005. Botanical
therapies in sexual dysfunction.Phytotherapy
Research 19, 457-463.
http://dx.doi.org/10.1002/ptr.1634
Tilwari A, Shukla N, Devi PU. 2011. Effect of five
medicinal plants used in Indian system of medicines
on immune function in Wistar rats. African Journal of
Biotechnology 10, 16637-16645.
http://dx.doi.org/10.5897/AJB10.2168
Wang B, Ma L, Liu T. 1990. 406 cases of angina
pectoris in coronary heart disease treated with
saponin of Tribulus terrestris. Zhong xi yi jie he za zhi
Chinese journal of modern developments in
traditional medicine 10, 85-87, 68.
Wang J, Zu X, Jiang Y. 2009. Five furostanol
saponins from fruits of Tribulus terrestris and their
cytotoxic activities. Natural product research 23,
1436-1444.
http://dx.doi.org/10.1080/14786410902940990
Xu YX, Chen H-S, Liang H-Q, Gu ZB, Liu WY,
Leung WN, Li TJ. 2000. Three new saponins from
Tribulus terrestris.Planta medic 66, 545-550.
http://dx.doi.org/10.1055/s-2000-8609
Xu Y, Liu Y, Xu T, Xie S, Si Y, Liu Y, Zhou H,
Liu T, Xu D. 2010. A new furostanol glycoside from
Tribulus terrestris.Molecules 15, 613-618.
http://dx.doi.org/10.3390/molecules15020613
Yang Q, Yang C. 2000. A New Steroidal saponin
from Chlorophytum malayense.Acta Botanica
Yunnanica 22, 191-196.
Zheleva-Dimitrova D, Obreshkova D,
Nedialkov P. 2012. Antioxidant activity of tribulus
terrestris a natural product in infertility
37
Azam et al.
Int. J. Biosci.
2019
therapy.Internatinal Journal of Pharmacy and
Pharmaceutical Sciences 4, 508-511.
Zhu W, Du Y, Meng H, Dong Y, Li L. 2017. A
review of traditional pharmacological uses,
phytochemistry, and pharmacological activities of
Tribulus terrestris.Chemistry Central Journal 11, 60.
http://dx.doi.org/10.1186/s13065-017-0289-x
... Male infertility short review [5] 2019 Phytochemistry and ethnomedicine NS brief presentation of constituents [12] 2019 Male infertility NS [13] 2019 Phytochemistry and pharmacology 1965-2017 [14] 2020 Phytochemistry and pharmacology NS the review is based mostly on ...
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The general spread of Tribulus terrestris L. (South Africa, Australia, Europe, and India), the high content of active ingredients (in particular sterol saponins, as well as flavonoids, tannins, terpenoids, phenol carboxylic acids, and alkaloids), and its frequent uses in folk medicine, and as food supplements highlight the importance of evaluating its phytopharmacological properties. There are miscellaneous hypotheses that the species could have a high potential for the prevention and improvement of various human conditions such as infertility, low sexual desire, diabetes, and inflammatory diseases. Worldwide, numerous herbal supplements are commercialized with indications mostly to improve libido, sexual performance in both sexes, and athletic performance. Phytochemical studies have shown great disparities in the content of active substances (in particular the concentration of furostanol and spirostanol saponoside, considered to be the predominant active ingredients related to the therapeutic action). Thus, studies of experimental pharmacology (in vitro studies and animal models in vivo) and clinical pharmacology (efficacy and safety clinical trials) have sometimes led to divergent results; moreover, the presumed pharmacodynamic mechanisms have yet to be confirmed by molecular biology studies. Given the differences observed in the composition, the plant organ used to obtain the extract, the need for selective extraction methods which are targeted at the class of phytocompounds, and the standardization of T. terrestris extracts is an absolute necessity. This review aims to highlight the phytochemical, pharmacological, and toxicological properties of T. terrestris, with a focus on the contradictory results obtained by the studies conducted worldwide.
... Каротиноиды: в листьях -α-каротин; фенолкарбоновые кислоты: в плодах -феруловая, пгидроксибензойная; алкалоиды: трибулусамид С, трибулусерин, трибулусин, гармин, гарман; другие компоненты включают органические кислоты, аминокислоты; из органических кислот: бензойная, ваниловая, феруловая, янтарная кислоты. Основными аминокислотами являются аланин и треонин, кроме того, содержатся кумарин, эмодин и физион [6,[14][15][16][17]. ...
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Tribulus terrestris L. is a well‐known medicinal plant from subtropical areas. In China Pharmacopoeia, only the fruit of T. terrestris is recorded to be the medicinal part. But some pharmaceutical preparations and food supplements made of total saponins of aerial part of T. terrestris including fruits, stems, leaves have been commercially available. However, steroidal saponins in different parts have not been studied extensively. So differentiating three parts and ensuring reasonable application of T. terrestris has been an important issue. Herein, we developed an integrated platform based on components profiling and chemometrics analysis to comparatively characterize and investigate steroidal saponins in three parts. As a result, a total of 84 steroidal saponins were characterized or tentatively identified, including 20 compounds reported for the first time. A clear separation of the three parts was achieved by partial least squares discriminant analysis based on the identified saponins, and 17 saponins were screened as biomarkers. Support vector machines model established based on 17 markers showed excellent predication accuracy of 100%. Finally, different distribution of steroidal saponins in three parts was showed obviously by Heatmap visualization. These results provide promising perspectives for quality control of Chinese Medicine, especially those with different medical parts. This article is protected by copyright. All rights reserved
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Context: Tribulus terrestris L. (Zygophyllaceae) fruits have long been used in traditional systems of medicine for the treatment of various urinary diseases including urolithiasis. Objective: To explore the anti-urolithiatic potential of gokhru and to develop an analytical method for quantitative estimation of metabolites for its quality control. Materials and methods: Aqueous extract of gokhru fruit was prepared through maceration followed by decoction to produce a mother extract, which was further used for polarity-based fractionations. In vitro and ex vivo anti-urolithiatic activity of mother extract and fractions at different concentration (100–1000 μg/mL) were carried out using aggregation assay in synthetic urine and in rat plasma, however, nucleation assay for 30 min was done using confocal microscopy. A simultaneous HPLC method has been developed for quantification of diosgenin, catechin, rutin, gallic acid, tannic acid and quercetin in mother extract and in fractions. Results: The extraction resulted in 14.5% of w/w mother extract, however, polarity-based fractionation yielded 2.1, 2.6, 1.5, 1.3 and 6.1% w/w of hexane, toluene, dichloromethane (DCM), n-butanol and water fractions, respectively. In vitro and ex vivo studies showed a significant anti-urolithiatic potential of n-butanol fraction. Further, HPLC analysis revealed significantly (p < 0.01) higher content of quercetin (1.95 ± 0.41% w/w), diosgenin (12.75 ± 0.18% w/w) and tannic acid (9.81 ± 0.47% w/w) in n-butanol fraction as compared to others fractions. Discussion and conclusion: In vitro and ex vivo studies demonstrated potent anti-urolithiatic activity of n-butanol fraction which can be developed as new phytopharmaceuticals for urolithiasis. HPLC method can be used for quality control and pharmacokinetic studies of gokhru.
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Aims: The present study investigates the protective effect of partially characterized Tribulus terrestris L. fruit methanol extract against mitochondrial dysfunction in cell based (H9c2) myocardial ischemia model. Main methods: To induce ischemia, the cells were maintained in an ischemic buffer (composition in mM -137 NaCl, 12 KCl, 0.5 MgCl2, 0.9 CaCl2, 20 HEPES, 20 2-deoxy-d-glucose, pH-6.2) at 37°C with 0.1% O2, 5% CO2, and 95% N2 in a hypoxia incubator for 1h. Cells were pretreated with various concentrations of T. terrestris L. fruit methanol extract (10 and 25μg/ml) and Cyclosporin A (1μM) for 24h prior to the induction of ischemia. Key findings: Different parameters like lactate dehydrogenase release, total antioxidant capacity, glutathione content and antioxidant enzymes were investigated. Studies were conducted on mitochondria by analyzing alterations in mitochondrial membrane potential, integrity, and dynamics (fission and fusion proteins - Mfn1, Mfn2, OPA1, Drp1 and Fis1). Various biochemical processes in mitochondria like activity of electron transport chain (ETC) complexes, oxygen consumption and ATP production was measured. Ischemia for 1h caused a significant (p≤0.05) increase in LDH leakage, decrease in antioxidant activity and caused mitochondrial dysfunction. T. terrestris L. fruit methanol extract pretreatment was found effective in safeguarding mitochondria via its antioxidant potential, mediated through various bioactives. HPLC of T. terrestris L. fruit methanol extract revealed the presence of ferulic acid, phloridzin and diosgenin. Significance: T. terrestris L. fruit ameliorate ischemic insult in H9c2 cells by safeguarding mitochondrial function. This validates the use of T. terrestris L. against heart disorders.
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The α-glucosidase inhibitory potential of Tribulus terrestris extracts has been reported but as yet the active ingredients are unknown. This study attempted to isolate the responsible metabolites and elucidate their inhibition mechanism of α-glucosidase. By fractionating T. terristris extracts, three cinnamic acid amide derivatives (1-3) were ascertained to be active components against α-glucosidase. The lead structure, N-trans-coumaroyltyramine 1, showed significant inhibition of α-glucosidase (IC50 = 0.42 μM). Moreover, all active compounds displayed uncompetitive inhibition mechanisms that have rarely been reported for α-glucosidase inhibitors. This kinetic behavior was fully demonstrated by showing a decrease of both Km and Vmax, and Kik/Kiv ratio ranging between 1.029 and 1.053. We progressed to study how chemical modifications to the lead structure 1 may impact inhibition. An α, β-unsaturation carbonyl group and hydroxyl group in A-ring of cinnamic acid amide emerged to be critical functionalities for α-glucosidase inhibition. The molecular modeling study revealed that the inhibitory activities are tightly related to π-π interaction as well as hydrogen bond interaction between enzyme and inhibitors.
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The present study investigates the protective effects of Tribulus terrestris Fruit aqueous Extract (TTFAEt) in myocardially infarcted rats. The oral administration of TTFAEt to rats for 40 days afforded good protection against isoproterenol-induced alterations, like Hyperlipidemia: the disorders of lipid metabolism have been ranked as one of the greatest risk factors contributing to the prevalence and severity of atherosclerosis, stroke and coronary heart diseases. Cardiac levels of lipid peroxidation (LPO) as well as the activities of antioxidant enzymes like Superoxide dismutase (SOD), Catalase (CAT), glutathione peroxidase (GPx), Glutathione-S-transferase (GST). Antioxidants can prevent reactive oxygen species-mediated damage and thus may have potential application in the prevention and cure of such diseases. Myocardial infarction produces a significant abnormal liver functioning. Liver tissue marker enzymes like alanine aminotransferase (ALT), aspartate aminotransferase (AST) and lactate dehydrogenase (LDH). The protective effect of TTFAEt was further supported by the reversal of isoproterenol-induced histological changes in the liver. The results suggest that TTFAEt protect the heart and circulatory system and also hepatoprotective and thereby maintain the near normal architecture of liver tissue.