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

  • Department of Pharmacy


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.
Azam et al.
Int. J. Biosci.
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,
2Department of Veterinary Pathobiology, Texas A&M University, College Station, Texas, United
3Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan
4Institute of Microbiology, University of Agriculture, Faisalabad, Pakistan
Key words: Tribulus terrestris, Ethnomedicine, Traditional uses.
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
International Journal of Biosciences | IJB |
ISSN: 2220-6655 (Print), 2222-5234 (Online)
Vol. 14, No. 1, p. 21-37, 2019
Azam et al.
Int. J. Biosci.
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.,
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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Int. J. Biosci.
estradiol, linoleic acid, stearic acid and beta-sitosterol
and these were identified by gas-chromatography and
mass spectrometry (GC-MS) analysis (Abirami et al.,
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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Int. J. Biosci.
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.,
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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Int. J. Biosci.
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
Plant dry extract
Pavin et al., 2018
(Fatima et al., 2014).
(Singh et al., 2008; Mitra et al., 2012; Zhu et al., 2017).
(Amin et al., 2006).
Leaves and fruits
(Baburao et al., 2009; Borran et al., 2017).
(GamalEl Din et al., 2018, Singh et al., 2012).
(Anand et al., 1994; Shirfule et al., 2011).
(Fatima et al., 2014).
(Khan et al., 2011; Rahmathulla et al., 2013).
(Heidari et al., 2007; Borran et al., 2017).
(Anand et al., 1994; D. K. Sharma, 2017).
(Reshma et al., 2016; Borran et al., 2017).
Learning and memory
(Prabhu et al., 2014).
Against acute pancreatitis
(Borran et al., 2017).
Fruits and seeds
(Al-Ali et al., 2003; Chhatre et al., 2012).
Fruits and roots
Central nervous system
(Adaikan et al., 2000).
Fruits and stems
(Sun et al., 2003).
Fruits and leaves
(Al-Bayati & Al-Mola, 2008).
Fruits, stems, roots,
whole plant
Apoptosis inducer
(Basaiyye et al., 2018)
Fruits, stems, roots
(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
(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
(Tilwari et al., 2011).
Whole plant
(Deepak et al., 2002).
Whole plant
(Fatima et al., 2014).
Whole plant
Smooth & skeletal muscle
(Fatima et al., 2014).
Whole plant
(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
Azam et al.
Int. J. Biosci.
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
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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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).
Azam et al.
Int. J. Biosci.
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
Azam et al.
Int. J. Biosci.
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
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).
Azam et al.
Int. J. Biosci.
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
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phytochemistry, and pharmacological activities of
Tribulus terrestris.Chemistry Central Journal 11, 60.
... 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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Tríbulus terrestris L. , an annual herb belonging to the Zygophyllaceae family and growing in moderate and tropical climates, has a rich chemical composition of biologically active substances and chemical elements. The aim of the work is a phytochemical study of Tribulus terrestris L. growing in different geographical zones. Materials and methods. The objects of study were herb specimens of Tribulus terrestris L. collected in different habitats. The samples of the raw materials were shade-dried. The determination of saponins in the raw materials, was carried out by high performance liquid chromatography with a mass spectrometric detection (HPLC-MS / MS). The study of the qualitative and quantitative composition of the elements was carried out on an X-ray fluorescence spectrometer. Results. The saponins had been studied by HPLC-MS/MS, according to which in all the studied samples, dioscin and protodioscin were found. Their retention times coincided with the retention times of dioscin and protodioscin standards. It has been established that among the macroelements of Tríbulus terrestris L. , potassium and calcium are mostly accumulated. They account for about 90% of the total content of the elements in the plant. It has been revealed that the distribution of macroand microelements in the plant, varies significantly depending on their place and growing conditions. Conclusion. The maximum dioscin content was observed in the samples harvested in Moldova, and the minimum – in the samples from the nursery garden of the All-Russian Scientific Research Institute of medicinal and aromatic plants. The largest amount of protodioscin was found out in the samples from the Crimea, and the minimum – in the samples from Moldova. The carried out study of the elements content of Tríbulus terrestris L. showed that the habitats (geographical zones) in which the studied samples of raw materials had been were collected, affect the accumulation of the elements by the plant. Based on the data obtained, biological absorption series have been compiled for the samples from each habitat.
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The current experiment aimed to investigate the effects of TT powder on performance parameters and functional tests, as well as on morphological and histological changes in the liver, kidney and ileum in broiler chickens. Commercial broilers (total = 168 females) were used, equally divided into three dietary treatments (C = 0.0, T1 = 0.75, and T2 = 1.5 g/kg diet). The growth performance (1–35 days of age), absolute and relative weight, liver and kidney functional tests, intestinal morphology (14 and 35 days of age), and histomorphology of the ileum (35 days of age) were evaluated. At 35 days of age, histopathological changes in the ileum, liver, and kidney were also examined. The results showed that the growth performance and absolute and relative weights of the liver and kidney had no negative effects when dietary supplementation with TT powder was given at 0.75 g/kg diet (T1), whereas a decrease was observed at T2 (p < 0.05). Liver and kidney functional tests showed no significant effects in all feed treatments (14 days), while T1 showed lower (p < 0.05) ALT and AST levels (35 days). T1 exhibited higher weights, lengths, and weight-to-length ratios of the small intestine, and relative lengths of the duodenum (p < 0.05). Histomorphometric measurements of the ileum were higher (p < 0.05) in chickens fed the 0.75 g TT/kg diet, and except for in the goblet cell count and epithelial thickness, there were no differences between treatments (p > 0.05). In T1, hepatocytes were more normal but hepatic sinusoids were dilated, whereas in T2, lymphocytes had infiltrated around the central vein and lining endothelial cells had been lost. The kidney was improved in T1 and T2 compared with the control group. Ileal villi were shorter in T2, and some villi fused with enterocyte necrosis and inflammatory cells accumulated in the lumen. We concluded that TT powder (0.75 g/kg feed) has a safe effect and is healthy for broilers.
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Tribulus terrestris (TT) has been considered as a potential stimulator of testosterone production, which has been related with steroidal saponins prevailing in this plant. Cyclophosphamide (CP) is the most commonly used anticancer and immunosuppressant drug, which causes several toxic effects, especially on the reproductive system. Patients who need to use CP therapy exhibit reduced fertility or infertility, which impacts both physically and emotionally on the decision to use this drug, especially among young men. We hypothesized that the treatment with TT dry extract would protect the male reproductive system against CP toxicity. Mice received dry extract of TT (11 mg/kg) or vehicle by gavage for 14 days. Saline or CP was injected intraperitoneally at a single dose (100 mg/kg) on the 14th day. Animals were euthanized 24 h after CP administration, and testes and epididymis were removed for biochemical and histopathological analysis and sperm evaluation. The dry extract of TT was evaluated by HPLC analysis and demonstrated the presence of protodioscin (1.48%, w / w ). CP exposure increased lipid peroxidation, reactive species, and protein carbonylation and altered antioxidant enzymes (SOD, CAT, GPx, GST, and GR). Moreover, acute exposure to CP caused a reduction on 17 β -HSD activity, which may be related to the reduction in serum testosterone levels, histopathological changes observed in the testes, and the quality of the semen. The present study highlighted the role of TT dry extract to ameliorate the alterations induced by CP administration in mice testes, probably due to the presence of protodioscin.
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The current study was carried out to evaluate the genotoxic aspects of the aqueous extracts of the Tribulus terrestris fruits by comet assay and cytogenetic procedures conditions on cultured human peripheral blood lymphocyte. After the treatment of the lymphocytes with four concentrations of the aqueous fruit extract of T. terrestris (10, 20, 40 and 80 mg/L) for 24 hours it was noticed that, the presence of micronuclei and/or chromosomal aberration were monitored and a significant increase of comet cells at high concentration of T. terrestris extract 80 mg/L. Also, this study showed that the presence of micronuclei, chromosomal aberration as a chromosomal gap, fragmentation, stickiness and necrotic cells were appeared and increased with high concentrations of T. terrestris fruits extract (40-80 mg/L). On the other hand, no significant difference was observed with the low concentration of the extract (10-20 mg/L) as compared with control. The current study refers to the ability of the extract of T. terrestris fruits to do damage in the target DNA at the higher concentrations. Thus, it could be considered that the aqueous extracts of the T. terrestris fruits have genotoxic effect in the therapeutic protocols if it used in high doses.
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In this study, root, leaf and fruit flavonoids of Tribulus terrestris L. are co mpared. Aqueous-ethanolic extracts of collected plant material were examined to practice flavonoid detection, isolation and identificat ion by 2-dimensional paper chromatography, thin layer ch ro matography and available references. Voucher specimen was prepared for reference as herbariu m voucher. Results showed chrysin was just identified in fruit while root and leaf had not any chrysin. Also flavone C and C-/O-glycosides were not found in leaf and fruit whereas root of the species had flavonoid sulphates and aglycones in addition to flavone C and C-/O-glycosides.
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
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.
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.
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.
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.