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Ali Esmail Al-Snafi. / Journal of Pharmaceutical Biology, 5(2), 2015, 93-98.
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Journal of Pharmaceutical Biology
www.jpbjournal.com e-ISSN - 2249-7560
Print ISSN - 2249-7579
THE PHARMACOLOGICAL IMPORTANCE OF ASPARAGUS
OFFICINALIS - A REVIEW
Ali Esmail Al-Snafi
Department of Pharmacology, College of Medicine, Thi qar University, Nasiriyah, Iraq.
ABSTRACT
Asparagus officinalis contained steroid saponins including asparagosides A, B, D, F, G, H, I, the bitter steroid
saponins, amino acids, fructans (asparagose and asparagosine), ferulic acid, minerals, vitamins and flavonoids. It exerts
anticancer, antimicrobial, antioxidant, hypolipidemic, antidiabetic and many other effects. This paper will highlight the
chemical constituents and the pharmacological effects of Asparagus officinalis.
Keywords: Asparagus officinalis, pharmacology, chemical constituents.
INTRODUCTION
Plant derivates had been employed by population
to prevent different kind of diseases for centuries. The
knowledge of plant properties was acquired by ancient
civilization that passed down from generation to
generation until today. Asparagus officinalis contained
steroid saponins including asparagosides A, B, D, F, G,
H, I, the bitter steroid saponins, amino acids, fructans
(asparagose and asparagosine), ferulic acid, minerals,
vitamins and flavonoids. It exerts anticancer,
antimicrobial, antioxidant, hypolipidemic, antidiabetic
and many other effects. This paper will highlight the
chemical constituents and the pharmacological effects of
Asparagus officinalis.
Synonyms
Asparagus caspius Hohen.; Asparagus
longifolius Fisch. ex Steud.; Asparagus officinalis var.
caspius (Hohen.) Asch. & Graebn.; Asparagus officinalis
subsp. officinalis ; Asparagus polyphyllus Steven ex
Ledeb [1].
Taxonomical Classification
Kingdom: plantae
Division: tracheophyta
Subdivision: spermatophytina
Class: magnoliopsida
Superorder: lilianae
Order: asparagales
Family: asparagaceae (also placed in: lamiaceae)
Subfamily: asparagoideae
Genus: asparagus
Species: Asparagus officinalis [2].
Common names
Arabic: Ehlilaj aswad, Helion, Dhagboth, Akla, al theeb;
Chinese: Shi diao bai; English: Asparagus, Garden
asparagus, White asparagus, Sparrow grass and Common
asparagus; German: Spargel; French: Asperge; Italian:
Asparagio; Japanese: Oranda-kiji-kakushi; Portuguese:
Espargo; Spanish: Espárrago, Esparraguera, and Swedish:
Sparris [1].
Description
It is perennial herb. Rootstock creeping, thick,
tuberously swollen, short-jointed. Height: 60–150 cm
(24–60 in.). Stem many-branched, 2–6 needle-like shoots
in whorls. Flower: Perianth regular (actinomorphic),
whitish–greenish yellow, 4–6 mm (0.16–0.24 in.) wide,
fused, 6-lobed. Male flowers‟ perianth narrowly
campanulate, female and bisexual flowers almost
spherical. Stamens 6. Gynoecium fused, single-styled.
Flowers solitary or in pairs–whorls of a few flowers in
leaf axils. Leaves: Rudimentary, scale-like. Axillary
shoots needle-like, whorled. Fruit: Round, initially green,
when ripe orange, 6–10 mm (0.24–0.4 in.) wide berry [3-
4].
Corresponding Author:- Ali Esmail Al-Snafi Email:- aboahmad61@yahoo.com
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Distribution
The plant was distributed in Central and
Southern Europe, the Middle East, Western Siberia and
Northern Africa. It was cultivated in many places [1]. It
was now distributed in: Algeria, Morocco, Tunisia
(Africa); Afghanistan, Iran, Iraq, Lebanon, Syria,
Turkey, Armenia, Azerbaijan, Georgia, Russian
Federation, Kazakhstan, Mongolia and China (Asia);
Denmark, Austria, Belgium, Czechoslovakia,
Germany, Hungary, Netherlands, Poland, Switzerland,
Belarus, Moldova, Ukraine, Albania, Bulgaria, Former
Yugoslavia, Greece, Italy, Romania, France, Portugal,
Spain, Finland, Norway, Sweden, Estonia, Latvia and
Lithuania (Europe) ; USA and Canada (Northern
America); Bolivia, Ecuador, Argentina and Uruguay
(Southern America) ; as well as Australia and New
Zealand [1].
Traditional uses
Traditionally, the roots were used for non-
specific inflammatory diseases of the efferent urinary
tract and for prevention of kidney and bladder stones
(irrigation therapy), dropsy, rheumatic conditions, liver
disease, bronchial asthma and gout. In Chinese medicine,
the root was also used to treat irritable cough, coughing
with blood, dry mouth and throat, and constipation [1].
Part used: The herb, rhizome and root were used
medicinally [1].
Chemical constituents
Asparagus officinalis contained steroid saponins
including asparagosides A, B, D, F, G, H, I, the bitter
steroid saponins, amino acids, fructans (asparagose and
asparagosine), ferulic acid and flavonoids (quercetin, rutin
hyperoside, and isoquercitrin) [1-3]. Among 23
commonly consumed vegetables, the highest antioxidant
activity based on dry weight was seen in asparagus [8].
The most abundant known flavonoid in asparagus is rutin
[9], it represented 60-80% of the total phenolic content of
purple and green asparagus extracts (10). It was observed
that rutin in green spears of 12 asparagus hybrid lines,
ranging from 0.015 to 0.45% of fresh weight. The level of
rutin varies with asparagus genotype as well as the tissue
location. For instance, rutin has been found to be more
abundant at the upper portions of the spears, while the
bottoms of asparagus contain a very small quantity of
rutin (less than 0.01% of fresh weight from three lines of
sampled asparagus) [11].
Shao et al., isolated two oligofurostanosides
from the seeds of Asparagus officinalis, and their
structures characterized as 3-O-[alpha-L-
rhamnopyranosyl-(1-->2)- (alpha-L-rhamnopyranosyl-(1-
->4))-beta-D-glucopyranosyl]-26-O-[ beta- D- gluco
pyranosyl] -(25R) -22 alpha-methoxyfurost-5-ene-3
beta,26-diol(methyl protodioscin) and its corresponding
22 alpha-hydroxy analogue (protodioscin) [12].
New asparagusic acid anti-S-oxide methyl ester
and asparagusic acid syn-S-oxide methyl ester, a new
acetylenic compound, 2-hydroxyasparenyn {3„,4„-trans-
2-hydroxy-1-methoxy-4- [ 5-(4-methoxyphenoxy ) -3-
penten -1-ynyl] - benzene}, as well as eleven known
compounds, asparenyn, asparenyol, (±)-1-monopalmitin,
ferulic acid, 1,3-O-di-p-coumaroylglycerol, 1-O-feruloyl-
3-O-p-coumaroylglycerol, blumenol C, (±)-
epipinoresinol, linoleic acid, 1,3-O-diferuloylglycerol,
and 1,2-O-diferuloylglycerol, were isolated from an ethyl
acetate-soluble fraction of the methanol extract of the
aerial parts of Asparagus officinalis [13].
Two major anthocyanins (A1 and A2) were also
isolated from peels of the spears of Asparagus officinalis.
A1 was identified as cyanidin 3-[3''-(O-beta-d-gluco
pyranosyl)-6''-(O-alpha-l-rhamnopyranosyl)-O-beta-d-
glucopyranoside], whereas A2 was cyanidin 3-rutinoside,
which was widely distributed in higher plants. Oxygen
radical absorbance capacity assays proved their high
antioxidant activities [14].
Sun et al., isolated a new steroidal saponin,
yamogenin II, with a unique aglycone moiety, and a
structure of (25S)-spirostan-5-ene-3β-ol-3-O-α-L-
rhamnopyranosyl-(1,2)-[α-L-rhamno pyranosyl- (1,4)]-β-
D-glucopyranoside from the dried stems of Asparagus
officinalis [15]. Furthermore, more saponins were isolated
from the plant included (25R)-furost-5-en-3β,22,26-triol-
3-O-[α-L-rhamnopyranosyl-(1→4)-β-D-glucopyranoside]
-26-O-β-D-glucopyranoside, (25R)-furostane-3β,22,26-
triol-3-O-[α- L-rhamnopyranosyl- (1→4) -β-D-
glucopyranoside] -26-O-β-D-glucopy ranoside, and
(25S)-furostane-3β,22,26-triol-3-O- [α-L-rhamno
pyranosyl-(1→4)-β-D-glucopyranoside]-26-O-β-D-
glucopyranoside, and 3-O-[{α-L-rhamnopyranosyl-
(1→2)} {α-L-rhamnopyranosyl-(1→4)}-β-D-
glucopyranosyl]-(25S)-spirost-5-ene-3β-ol. They were
identified as key bitter compounds in the edible spears of
Asparagus officinalis, they showed human bitter
recognition thresholds between 10.9 and 199.7 μmol/l
(water) [16].
Many carotenoid pigments were isolated from
the ripe and unripe fruits of Asparagus officinalis, these
included capsanthin, capsorubin, capsanthin 5, 6-epoxide,
antheraxanthin, violaxanthin, neoxanthin, mutatoxanthin
epimers, zeaxanthin, lutein, β-cryptoxanthin, β-carotene,
and some cis [17].
Nutritional analysis showed that the plant
contained water 93.5 %, total protein 1.91%, fat 0.16%,
carbohydrates 2.04%, total dietary fiber 1.31% total
nitrogen 0.31% [18].
The amino acid and mineral contents were
found to be much higher in the leaves than the shoots. The
following amino acids were founds in the young shoots
and leaves (mg /Kg) respectively: aspartic acid 921.17
and 4369.47 , asparagine 653.68 and 6967.50, threonine
61.21 and 611.20, serine 112.67 and 845.45, glutamic
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acid 501.35 and 2933.77, proline undetectable in both,
glycine 87.41 and 744.80, alanine 143.53 and 919.58,
valine 113.80 and 835.70, isoleucine 65.82 and 574.49,
leucine 106.94 and 995.94, tyrosine undetectable and
416.76, phenylalanine 95.54 and 517.61, histidine 190.16
and 590.94, lysine 40.85 and 1009.01, arginine 62.11 and
933.21, cysteine 108.19 and 347.14, methionine
undetectable and 145.71, tryptophan undetectable and
227.21. Minerals detected in the young shoots and leaves
were included respectively (mg /Kg): calcium 45.2 and
139, phosphorus 96.1 and 501.6, potassium 251.3 and
2574.8, iron 2.7 and 8.5, sodium 120.7 and 281.6.
Young shoots and leaves also contained protein 3000 and
20200, carbohydrate 2600 and 31600, vitamin B2 0.16
and 0.45 mg/kg respectively [19].
PHARMACOLOGICAL EFFECTS
Antidiabetic effects
Streptozotocin-induced diabetic rats were treated
with a methanolic extract of Asparagus officinalis seeds
(250 and 500 mg/kg per day) or glibenclamide for
28 days. Treatment of the diabetic rats with the Asparagus
officinalis extract at doses of 250 and 500 mg/kg
suppressed the elevated blood glucose in a dose- and
time-dependent manner. The 500 mg/kg, but not
250 mg/kg, dose significantly improved serum insulin
levels in the diabetic rats. The insulin: glucose ratio was
significantly increased at both doses in the A. officinalis-
treated rats. Both qualitative and quantitative
improvements in β-cell function were found in the islets
of the A. officinalis-treated rats. The extract showed
potent antioxidant activity in an in vitro assay and also
improved the total antioxidant status in vivo. In most
cases, the efficacy of A. officinalis (500 mg/kg) was very
similar to a standard anti-diabetic drug, glibenclamide
[20].
The hypoglycaemic effect of the aqueous extract
of asparagus by-product (AEA) was also evaluated in a
streptozotocin (STZ)-induced diabetic rat model.
Continuous administration of AEA for 21 days
significantly decreased fasting serum glucose and
triglyceride levels but markedly increased body weight
and hepatic glycogen level in diabetic rats. In an oral
glucose tolerance test, both the blood glucose level
measured at 30, 60 and 120 min after glucose loading and
the area under the glucose curve showed a significant
decrease after AEA treatment [21].
Anticancer, antioxidant and hypolipidemic effects
The plant exerted anticancer effects, the
anticancer activity of Asparagus officinalis may be
occurred via: (1) an antimutagenic effect – preventing
genetic mutations which can directly precede the earliest
stages of cancer development.(2) the promotion of
(cellular phase II detoxifying enzymes) which (facilitate
the removal of drugs and xenobiotic compounds) that are
carcinogenic and supporting overall liver function. (3)
synergistically enhancing the antioxidant activity of other
plant foods. (4) the inhibition of chronic inflammation
(cycooxygenase-2 suppression) which is thought to play a
role in tumor development. (5) the promotion of healthier
digestion and immune function [6].
Asparagus saponins inhibited the growth of
HepG2 cells in a dose-dependent manner. The median
inhibitory concentration (IC50) was 101.15 mg/l at 72
hours exposure. The apoptosis morphology at 72 hours of
treatment was obvious, showing cell protuberance,
concentrated cytoplasm, and apoptotic bodies. The
apoptotic rates at 72 hours were 30.9%, 51.7%, and
62.1% (for saponin concentrations of 50, 100 and 200
mg/l respectively). Treatment with Asparagus saponins
for 24 hours increased the intracellular level of reactive
oxygen species and Ca2+, lowered the pH, activated
intracellular mitochondrial permeability transition pore,
and decreased membrane potential in a dose-dependent
manner. Treatment also increased the activity of caspase-
9 and caspase-3, down-regulated the expression of Bcl2,
up-regulated the expression of Bax, and induced release
of CytC and activation of caspase-3[22].
The crude saponins from the shoots (edible part)
of asparagus were found to have antitumor activity. The
asparagus crude saponins inhibited the growth of human
leukemia HL-60 cells in culture and macromolecular
synthesis in a dose and time dependent manner. The
asparagus crude saponins at 75–100μg/ml range were
cytostatic. Its concentrations greater than 200 μg/ml were
cytocidal to HL-60 cells. The asparagus crude saponins at
6 μg/ml concentration inhibited the synthesis of DNA,
RNA and protein in HL-60 cells by 41, 5, and 4%
respectively, and at 50 μg/ml by 84, 68 and 59%
respectively. The inhibitory effect of asparagus crude
saponins on DNA synthesis was irreversible [23].
Shao et al., isolated two oligofurostanosides
from the seeds of Asparagus officinalis with cytotoxic
activity. They inhibited the growth of human leukemia
HL-60 cells in culture and macromolecular synthesis in a
dose-dependent manner. The inhibitory effect on DNA
synthesis was found to be irreversible [12].
Treatment of HepG2 human hepatoma cells with
the leaf extract of Asparagus officinalis suppressed more
than 70% of the intensity of hydrogen peroxide (1mM)-
stimulated DCF fluorescence, a marker of reactive oxygen
species. Cellular toxicities induced by treatment with
hydrogen peroxide, ethanol, or tetrachloride carbon were
also significantly alleviated in response to treatment with
the extracts of A. officinalis leaves and shoots.
Additionally, the activities of 2 key enzymes that
metabolize ethanol, alcohol dehydrogenase and aldehyde
dehydrogenase, were upregulated by more than 2-fold in
response to treatment with the leaf- and shoot extracts
[19].
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Saponins from old stems of asparagus (SSA)
exerted potential inhibitory activity on tumour growth and
metastasis. SSA suppressed cell viability of breast, colon
and pancreatic cancers in a concentration-dependent
manner, with half-maximum inhibitory concentrations
ranging from 809.42 to 1829.96 µg/ml. However, SSA
was more functional in blocking cell migration and
invasion as compared with its cytotoxic effect, with an
effective inhibitory concentration of 400 µg/ml. A
mechanistic study showed that SSA markedly increased
the activities of Cdc42 and Rac1 and decreased the
activity of RhoA in cancer cells [24].
One new (Sarsasapogenin O) and seven known
steroids were isolated from the roots of Asparagus
officinalis L. These compounds together with nine
steroids which were previously isolated from this plant,
were tested for cytotoxic activity. Among them, eight
compounds displayed significant cytotoxicities against
human A2780, HO-8910, Eca-109, MGC-803, CNE,
LTEP-a-2, KB and mouse L1210 tumor cells [25].
The antioxidant activity of asparagus juice was
analyzed by 2,2„-diphenyl-l-picrylhydrazyl and 2,2„-
azinobis(3-ethylbenzothiazoline-6-sulfonic acid) methods.
The enzymes, with the exception of pectinase from
Rhizopus sp., contained rutinase, which hydrolyzed rutin
to quercetin. Asparagus juice treated with viscozyme had
the highest quercetin content without exhibiting a
significant increase in the antioxidant activity. For a
pectinase from Aspergillus niger, the antioxidant activity
of asparagus juice was markedly reduced [7].
Sakaguchi et al., found that anthocyanins A1
and A2 isolated from the spears of Asparagus officinalis
were acting as antioxidants [6]. The potential effect of
different concentrations of freeze-dried Asparagus
officinalis (500, 250, and 125 mg/Kg of body weight/day)
was evaluated on oxidative status and lipid profile in rats
fed a cholesterol-rich diet. After five weeks of treatment,
doses of 250 and 500 mg/Kg of asparagus were
significantly reduced total cholesterol and LDL
cholesterol levels. Atherogenic index was also
significantly reduced in a dose-dependent manner by
administrating freeze-dried asparagus. A beneficial effect
was observed in the HDL cholesterol levels in asparagus-
fed groups, although the increase was not significant.
Consumption of asparagus also improved antioxidant
status (superoxide dismutase and catalase enzymes), and
protected against lipid peroxidation [26].
The antioxidant effects of Asparagus officinalis
was investigated using superoxide dismutase, erythrocyte
haemolysis and 2,2- diphenyl-1-picrylhydrazil free radical
scavenging methods. The highest antioxidant capacity
was obtained from the in vivo grown plant extract
followed by in vitro grown plant extract in all three
examined assays [27].
The hypolipidemic effect of n-butanol extract
from asparagus by-products was evaluated in mice fed a
high-fat diet. Asparagus butanol extract significantly
decreased the levels of body weight gain, serum total
cholesterol and low density lipoprotein cholesterol; it
dramatically increased the high density lipoprotein level
when administered at three different doses (40, 80 or
160 mg/kg bw) for 8 weeks in hyperlipidemic mice. In
addition, asparagus butanol extract decreased the levels
of alanine transaminase, aspartate transaminase and
alkaline phosphatase in serum. Superoxide dismutase
activity and the total antioxidation capacity were
evidently increased; in addition, the malondialdehyde
level and the distribution of lipid droplets were reduced in
liver cells of asparagus butanol extract -treated mice [28-
29].
Antimicrobial effects
The antibacterial potential of the ethanolic
extracts of in vitro grown A. officinalis as well as
ethanolic extract of undifferentiated callus cells of A.
officinalis were studied using the paper disc diffusion
method against two gram-negative pathogenic bacteria
(Escherichia coli and Pseudomonas aeruginosa) and two
gram-positive pathogenic bacteria (Staphylococcus aureus
and Bacillus cereus) . Antibacterial effect recorded only
for callus extract (100 mg/ml) against Bacillus cerus. The
rest of the extracts showed no antimicrobial activity in the
same concentration against any of the tested pathogenic
bacteria [27].
However Naema et al., found that aqueous
extract of Asparagus officinalis showed a wide zone of
inhibition when tested against E. coli growth in a
concentration of 5% [30].
The saponin fraction of the Asparagus
officinalis exerted antifungal activity [31-32].
Effect on colitis
The effects of cooked whole asparagus and its
purified bioactive, rutin, were studied on colitis symptoms
and disease progression in mice. C57BL/6 mice were fed
a basal diet supplemented with 2% asparagus or 0.025%
rutin for 3 weeks. Colitis was induced by 2% dextran
sodium sulfate in drinking water for 7 days. Asparagus
diet was determined to contain higher antioxidant
capacities than rutin diet through antioxidant assays.
During active colitis, consumption of asparagus alleviated
some clinical symptoms (stool consistency, stool blood,
and spleen hypertrophy) of colitis. In recovery, asparagus-
fed mice were improving in terms of regenerating crypts,
surface epithelial, and goblet cells, potentially due to its
rutin content [33].
Other pharmacological effects
Asparagus officinalis increased the clearance rate
of charcoal particles and the weight of immune organs in
mice, it exerted antifatigue effects, enhanced anoxia
tolerance, induced analgesia and improved memory, as
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well as decreased the contents of lipid peroxide in
plasma, liver and brain of the animal [34].
Jang et al., examined Asparagus officinalis for
its inhibitory effects against both cyclooxygenase-1 and -
2. They found that linoleic acid was the most active
compound [13].
The protecting effect of asparagus on the rat liver
injured by CCl4 (5%) poured into the stomach was
investigated in rats. Compared with control, the contents
of serum glutamic-pyruvic transaminase (SGPT) and
malondialdehyde (MDA) were lower, and the content of
liver superoxide dismutase (SOD) was higher in
asparagus treated group [35].
Aqueous extract of Asparagus officinalis caused
relaxation of spontaneous contractions of isolated smooth
muscle of rabbit jejunum [14]. Asparagus officinalis also
induced diuretic effects [36].
Contraindications and adverse effects
No health hazards or side effects are known in
conjunction with the proper administration of designated
therapeutic dosages. Because of the irritating effect of
saponin, the drug should not be administered in the
presence of kidney diseases. In the case of reduced
cardiac and/or kidney function, irrigation therapy should
not be attempted. The berries were considered poisonous
[5].
Dosage Root: 3-5g powder [37]. A typical single dose is
800 mg of the plant. The cut rhizome was used as teas for
internal use [5].
CONCLUSION
Asparagus officinalis is a plant with wide range
of chemical constituents which exerted many
pharmacological effects. There is a great promise for
development of novel drugs from Asparagus officinalis
to treat human diseases as a result of its effectiveness and
safety.
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