Phytochemistry and pharmacognosy.

Abstract

During the past 50 years there have been tremendous advances in chemical and biological techniques of analysis that have transformed research in pharmacognosy. The PSE has regularly held symposia of relevance to pharmacognosy and some of these are briefly reviewed in the area of natural products from higher plants. These symposia have charted the developments that link pharmacognosy with phytochemistry and illustrate the application of increasingly more sophisticated analytical techniques to the discovery of biologically active compounds. Plants have yielded clinical drugs, either as natural product molecules, or as synthetic modifications, particularly for chemotherapeutic treatment of cancer and malaria. Aspects of biotechnology, traditional medicines and herbal medicinal products are briefly discussed.

Full text

Page 1

Research J. Pharmacognosy and Phytochemistry 2009; 1(3): 169-172 Deenanath Jhade et. al






A Pharmacological
spinosus


Deenanath Jhade*, Dheeraj Ahirwar, Ritesh Jain, Neeraj Kumar
Sharma and Sandeep Gupta


School of Pharmacy, Chouksey Engineering College, Bilaspur (C.G.),
495001 India.


ABSTRACT
In this paper
phytoconstituent studies and safety profile of Amaranthus spinosus are
presented. Through this review auther wish to attract the attention of nature
product researchers throughout the world to explore this potential plant
systemically. Perliminary work has been reported on Antiprotozoal activity,
Anti-inflammatory activity, Antioxidant properties, Anti-malarial activity,
Analgesic properties,
Properties, Antifertility activity, Anti-diabetic, anti-hyperlipidemic and
spermatogenic effects. Therefore A. spinosus hold a great potential for in
depth biological evaluation. Even, no work has ever been carried out for
standaridizing this potentially useful plant.

Keywords: Amaranthus spinosus, ethanopharmacology, clinical study.

INTRODUCTION
Amaranthus spinosus Linn. (Family: Amaranthaceae) is commonly known
as ‘‘Kate Wali Chaulai (Kanatabhajii)” in ‘Hindi”, also used as vegetable
and cultivated throughout in India, Sri Lanka and many tropical countries
(1). The juice of A. spinosus is used by tribal of Kerala, India to prevent
swelling around stomach while the leaves are boiled without salt and
consumed for 2–3 days to cure jaundice (2). Plant as one of the vegetable
have high concentration of antioxidant components (3) and high nutritive
values due to presence of fibre, proteins and high concentration of
essential amino acids, especially lysine (4).

The liver regulates several important metabolic functions and the hepatic
injury is associated with distortion of these metabolic functions (5). Thus,
liver diseases remain one of the serious health problems. In spite of
tremendous strides in the modern medicine, there are not much drugs
available for the treatment of liver diseases. There are a number of
medicinal preparations recommended in the Indian traditional system of
medicine ‘‘Ayurveda” for the treatment of liver diseases. There are
scientific claims to offer significant relief as hepatoprotective (6). A. spinosus
is used as antiinflammatory, antimalarial, antibacterial, antimicrobial,
antidiuretic, antiviral and in hepatic disorders (7,8,9). Water extract of plant
showed significant immunostimulating activity (10) and stem extract showed
antimalarial activities (11). A. spinosus have several active constituents like
alkaloids, flavonoids, glycosides, phenolic acids, steroids, amino acids,
terpenoids, lipids, saponins, betalains, b-sitosterol, stigmasterol, linoleic
acid, rutin, catechuic tannins and carotenoids. The betalains in stem bark
of A. spinosus were identified as amaranthine, isoamaranthine,
hydroxycinnamates, quercetin and kaempferol glycosides (12,13,14). It also
contains amaranthoside, a lignan glycoside, amaricin, a coumaroyl
adenosine along
glycinebetaine and trigonelline (15,16). Betalains are well known for their
antioxidant, anticancer, antiviral and antiparasitosis properties (17). Many
betalain containing species are used as popular medicinal plants to treat
various kinds of ailments such as hepatic disorders, malaria, jaundice and
scanty urine or to cure wounds (18).
169



ISSN 0975- 2331
Research Journal of
Pharmacognosy and
Phytochemistry. 1(3): Nov. – Dec
2009, 169-172






Review Article



















Corresponding Author:
Deenanath Jhade
School of Pharmacy, Chouksey
Engineering College,
(C.G.), 495001 India.
E-mail:
deenasiper_2006@yahoo.co.in
Ph: 07752-409486.




Received on 14.09.2009
Accepted on 15.10.2009
© A&V Publication all right
reserved

Bilaspur


Review :
Amaranthus
traditional, clinical potential, ethanopharmacology,
Immuno-modulatory properties, Haematology
with stigmasterol glycoside, betaine such as

Page 2

Research J. Pharmacognosy and Phytochemistry 2009; 1(3): 169-172 Deenanath Jhade et. al

PHARMACOLOGICAL ACTIVITY:
Antiprotozoal activity (19):
The dichloromethane extract of A. spinosus (2 mg/mL)
was moderately inhibited to Blastocystis hominis, a
common human protozoan. The reference anti-
protozoan agent, metronidazole (40 µg/mL) killed 97%
of the protozoan and inhibited all protozoan samples at
concentrations of 1.25-20 µg/mL .

Anti-inflammatory activity (13):
The anti-inflammatory property of methanolic extract of
A. spinosus leaves was studied in different animal
models. A. spinosus extract (25-100 mg/kg) significantly
inhibited carrageenan-induced rat paw edema and
produced significant inhibition of acetic acid-induced
increase in vascular permeability indicating that the
extract has anti-inflammatory activity. In the cotton
pellet granuloma test, rats were treated orally with the
extract for 4 consecutive days after the subcutaneous
implantation of a sterile pellet. The highest dose of the
extract (100 mg/kg) was able to significantly reduce the
post-implantation weight of cotton pellets compared to
controls indicating its effectiveness against acute
inflammation.

Severe gastric erosion was seen in rats given the
extract (50 and 100 mg/kg) repeatedly for 4 days, which
may reflect its ability to inhibit prostaglandin synthesis.
This was not seen in the controls or with a lower dose of
the extract (25 mg/kg). The extract (25-100 mg/kg) also
delayed castor oil-induced diarrhea in rats, which was
postulated to reflect its prostaglandin synthesis inhibitory
activity.

Antioxidant properties (20):
The antioxidant capacity of A. spinosus was studied in
roadside plants which were postulated to be
continuously exposed to the high levels of nitrogen
oxides and sulphur dioxide from automobile emissions.
A. spinosus was shown to possess a very good free
radical scavenging system for combating air pollution
through analysis of the enzymes superoxide dismutase,
catalase, ascorbate peroxidase, glutathione reductase
and phenolic peroxidase activities. Amaranthaceae
plants contain betalain pigments which showed strong
antioxidant activities by the DPPH assay. Their EC50
values range from 3.4 to 8.4 µM. The antioxidant
activity of A. spinosus extract may be due to its betalain
content.

Anti-malarial activity:
1. The aqueous extract of A. spinosus bark obtained
from mature stems was screened for antimalarial
properties in mice inoculated with erythrocytes
parasitized with Plasmodium berghei. The bark extract
showed a dose-dependent antimalarial activity in a 4-
day suppressive antimalarial assay using chloroquine as
the reference antimalarial drug. ED50 values for the
antimalarial activities of the extract and chloroquine
were 789.4 and 14.6 mg/kg, respectively (19).

2. Extracts obtained from two Burkinabe folk medicine
plants, spiny amaranth (Amaranthus spinosus L.,
Amaranthaceae) was screened for antimalarial
properties with the aim of testing the validity of their
traditional uses. The plant extracts showed significant
antimalarial activities in the 4-day suppressive
antimalarial assay in mice inoculated with red blood
170

cells parasitized with Plasmodium berghei berghei. ED50
value was found 789 and 564 mg/kg for Amaranthus
spinosus. Moreover the tested vegetal material showed
only low toxicity 1450 mg/kg as LD50 for Amaranthus
spinosus (11).

Analgesic properties (13):
Methanolic extract of A. spinosus leaves (25-100 mg/kg)
produced a dose-dependent decrease in acetic acid-
induced writhing with the highest dose producing an effect
(56.2% inhibition of writhing) which was comparable to
that of 5 mg/kg indomethacin (58.4% inhibition of writhing)
. These doses of the extract also reduced the licking time
at the late phase (20 minutes post formalin), not the early
phase of the formalin-induced paw licking assay in mice.
These results indicate that A. spinosus extract has
analgesic activity. Positive results in the late phase of the
formalin test indicate that the extract inhibited pain which
was associated with inflammation.

Immuno-modulatory properties(21).:
The aqueous extract of A. spinosus leaves showed
immuno-modulatory effects by significantly stimulating
splenocyte proliferation in primary splenocytes from
female BALB/c mice. The extract stimulated isolated B
lymphocytes, not T lymphocytes, in a dose response
manner. The water extract (1250 µg/mL) elicited a much
higher proliferation rate in bulk splenocytes than in
isolated purified B and T cells, suggesting some sort of
interaction between these cells. Thus, the immuno-
stimulating effects of the water extract may lead to B
lymphocyte activation which will subsequently, through
secondary signaling, lead to T lymphocyte proliferation. A
novel immuno-stimulatory protein (GF1) with a molecular
weight of 313 kDa was obtained after sequential
purification of the water extract. GF1, which was assumed
to be a glycoprotein and was heat labile, had an immuno-
stimulatory activity which was 309 times higher than that
of the water extract.

Haematology Properties (22):
Ethanol extract of Amaranthus spinosus leaf (EEAL) was
administered orally to growing pigs to determine its effects
on the haematological characteristics-packed cell volume
(PCV) red blood cell (RBC) and white blood cell (WBC)
counts, and haemoglobin (HB) concentration. Eighteen
growing pigs were randomly allotted to two treatments with
each treatment replicated thrice. Pigs in treatment 1 were
administered with EEAL. Treatment 2 served as control
receiving no treatment. Results showed that there were
significant (P<0.05) reduction in the PCV, RBC and Hb of
the pigs administered with EEAL seven days post
treatment and their weight gains significantly (P<0.05)
improved. Amaranthus spinosus, although an active
vermifuge should be used in animals with adequate
precaution to avoid any probable toxic effects.

Hepatoprotective activity (23):
The hepatoprotective and antioxidant activity of 50%
ethanolic extract of whole plant of Amaranthus spinosus
(ASE) was evaluated against carbon tetrachloride (CCl4)
induced hepatic damage in rats. The ASE at dose of 100,
200 and 400 mg/kg were administered orally once daily for
fourteen days. The substantially
enzymatic levels of serum glutamate oxaloacetate
transaminase (AST), serum
transaminase (ALT), serum alkaline phosphatase (SALP)
and total bilirubin were restored towards normalization
elevated serum
glutamate pyruvate

Page 3

Research J. Pharmacognosy and Phytochemistry 2009; 1(3): 169-172 Deenanath Jhade et. al

significantly by the ASE in a dose dependent manner.
Higher dose exhibited significant hepatoprotective
activity against carbon tetrachloride induced
hepatotoxicity in rats. The biochemical observations
were supplemented with histopathological examination
of rat liver sections. Meanwhile, in vivo antioxidant
activities as malondialdehyde (MDA), hydroperoxides,
reduced glutathione (GSH), superoxide dismutase
(SOD) and catalase (CAT) were also screened which
were also found significantly positive in a dose
dependent manner. The results of this study strongly
indicate that whole plants of A. spinosus have potent
hepatoprotective activity against carbon tetrachloride
induced hepatic damage in experimental animals. This
study suggests that possible mechanism of this activity
may be due to the presence of flavonoids and phenolics
compound in the ASE which may be responsible to
hepatoprotective activity.

Antifertility activity (24):
The Anti-fertility screening after ingestion of aqueous
and ethanolic extracts of Amaranthus spinosus Linn
roots have been investigated in pregnant rats. The
ingestion of 125, 150 and 175 mg/kg body weight of
alcoholic extracts of the plant from day one to day five
of pregnancy by female rats did cause significant
pregnancy interception. On other hand the ingestion of
125mg/kg body weight of aqueous and alcoholic
extracts of plant from day 11 to day 15 of pregnancy did
not cause significant pregnancy interception. However,
the ingestion of 150 and 175 mg/kg body weight of
alcoholic extracts of plant drugs exhibited significant
pregnancy interceptory affect. The alcoholic extracts of
selected ethno medicinal plants possessing more
pregnancy interception than aqueous extracts.

Anti-diabetic, anti-hyperlipidemic and
spermatogenic effects (25)
Anti-diabetic, anti-hyperlipidemic and spermatogenic
effects were studies with methanolic extract of stem of
Amaranthus spinosus Linn (Family: Amaranthaceae) in
diabetic rats. In streptozotocin (STZ)-induced diabetic
rats, it was observed that both the standard drug
(Glibenclamide) and methanolic extract of Amaranthus
spinosus Linn. Significantly exhibited control of blood
glucose level on a 15day model. Further, the methanolic
extract also showed significant anti hyperlipidemic and
spermatogenic effects in STZ-induced diabetic rats. The
methanolic extract has also accelerated the process of
spermatogenesis by increasing the sperm count and
accessory sex organ weights. The present investigation
of the plant established some pharmacological evidence
to support the folklore claim that it is used as an anti-
diabetic.

Toxicities (26-29):
The aqueous extract of the bark of A. spinosus has a
relatively low toxicity LD50 value of 1450 mg/k A.
spinosus was reportedly the culprit in cases of
spontaneous poisoning of cattle in Brazil during a
severe drought. Clinical signals appeared after 30 days
in 11 out of 35 adult cows and 8 out of 20 yearling
calves which were introduced into a 15 ha maize
plantation heavily infested with A. spinosus. However,
only one calf died within 3-7 days. The clinical signs
were depression, anorexia, marked weight loss, foul-
smelling diarrhea occasionally tinged with blood, and
subcutaneous oedema. Sub acute cases showed
171

distended abdomens, the animals were reluctant to stand
and walked with difficulty. Sloughing of the hooves
occurred in some animals. The main post-mortem findings
in 5 animals were moderately pale and swollen kidneys,
perirenal oedema and varying degrees of oedema in
several tissues and cavities. In some cases petechiae
and suffusions were associated with the subcutaneous
oedema. The mucosa of the digestive system showed
necrotic glossitis, oesophagitis and pharyngitis, abomasal
hemorrhages and button-like ulcerations in the large
intestine. The contents of ileum, colon and rectum were
blood stained. Hemorrhagic diathesis was apparent by the
presence of intra-abdominal hematomas. Histologically,
there was marked tubular nephrosis associated with
epithelial regeneration and hyaline intra-tubular casts. The
mucosal lesions consisted of large necrotic areas in the
epithelium which extended into the lamina propria and
were associated with inflammatory reaction with massive
infiltrations of mastocytes. The omasal mucosa had
selective necrosis of the basal layer cells. Renal failure
was suggested as the primary lesion which triggered the
other changes.

A. spinosus also caused an outbreak of acute poisoning in
ewes in southern Brazil. The clinical signs were uremic
halitosis, loss of ruminal motility, dispnoea and abortion.
The kidneys showed pale red spots, white streaks
extending from the cortex to medulla and congestion.
Histologically, there was severe acute tubular nephrosis,
dispersed foci of coagulative necrosis in the liver, areas of
coagulative necrosis in the myocardium and acute
incipient interstitial pneumonia
bronchopneumonia. Hyperkalemia secondary to renal
insufficiency was the underlying cause of myocardial
coagulative necrosis observed in seven sheep.

CONCLUSION:
Literature reveled that Amaranthus spinosus Scintifically
roported for Antiprotozoal activity, Anti-inflammatory
activity, Antioxidant properties, Anti-malarial activity,
Analgesic properties, Immuno-modulatory properties,
Haematology Properties, Antifertility activity, Anti-diabetic,
anti-hyperlipidemic and spermatogenic effects, and
traditionally it is used to prevent swelling around stomach,
jaundice, cure wounds. A. spinosus have several active
constituents like alkaloids, flavonoids, glycosides, phenolic
acids, steroids, amino acids, terpenoids, lipids, saponins,
betalains, b-sitosterol, stigmasterol, linoleic acid, rutin,
catechuic tannins and carotenoids.

REFERENCES:
1. Kirtikar KR and Basu BD. Indian Medicinal Plants. Oriental
Enterprises, New Connaught Place, Dehradun, Uttranchal,
India. 2001; 2 (1): 2832–2836.
2. Hema ES, Sivadasan M and Anil KN. Studies on edible
species of Amaranthacea and Araceae used by Kuruma and
Paniya tribes in Wayanad
Ethnobotany. 2006; 18: 122–126.
3. Odhav B, Beekrum S, Akula US, and Baijnath H. Preliminary
assessment of nutritional value of traditional leafy vegetables
in KwaZulu-Natal, South Africa. Journal of Food Composition
and Analysis. 2007; 20: 430–435.
4. Teutonico RA, Knorr D. Amaranth: composition, properties
and applications of a rediscovered food crop. Food
Technology. 1985; 39: 49–60.
5. Wolf PL. Biochemical diagnosis of liver diseases. Indian
Journal of Clinical Biochemistry. 1999; 14: 59–90.
6. Rao GMM, Rao ChV, Pushpangadan P and Shirwaikar A.
Hepatoprotective effects of rubiadin: a major constituent of
and secondary
district, Kerala, India.

Page 4

Research J. Pharmacognosy and Phytochemistry 2009; 1(3): 169-172 Deenanath Jhade et. al

7. Rubia cordifolia Linn. Journal of Ethnopharmacology. 2006;
103: 484–490.
8. Olajide O. Ogunleye B and Erinle T. Antiinflammatory
properties of Amaranthus spinosus leaf extract. Pharmaceutical
Biology. 2004; 42: 521–525.
9. Stintzing FC, Kammerer D, Schieber A, Hilou A, Nacoulma O
and Carle R.. Betacyanins and phenolic compounds from
Amaranthus spinosus and Boerhaavia erecta. Zeitschrift fur
Naturforschung. 2004; 59: 1–8.
10. Van Dunen MB. Activite antimicrobienne de Boerhaavia diffusa
L. (Nyctagynaceae). Pharmacopée et Médecine Traditionnelle
Africaines. 1985; 3: 23–25.
11. Lin BF, Chiang BL and Lin JY. Amaranthus spinousus water
extract directly stimulates proliferation of B-lymphocytes in vitro.
International Immunopharmacology. 2005; 5: 711–722.
12. Hilou A, Nacoulma OG and Guiguemde TR. In vivo antimalarial
activities of extracts from Amaranthus spinosus L. and
Boerhaavia erecta L. in mice. Journal of Ethnopharmacology.
2006; 103: 236–240.
13. Srinivasan K, Kaul CL and Ramarao P. Partial protective effect
of rutin on multiple low dose streptozotocin-induced diabetes in
mice. Indian Journal of Pharmacology. 2005; 37: 327–328.
14. Ibewuike JC, Ogundaini AO, Bohlin L and Ogungbamila FO.
Antiinflammatory activity of selected Nigerian medicinal plants.
Nigerian Journal of Natural Products and Medicine. 1997; 1:
10–14.
15. Rastogi RP, Mehrotra BN. Compendium of Indian medicinal
plants. CDRI and NISCAIR, Lucknow. 1999; 2: 38.
16. Blunden G, Yang M, Janicsak MI and Carabot-Cuervo A.
Betaine distribution in the Amaranthaceae. Biochemical
Systematics and Ecology. 1999; 27: 87–92.
17. Azhar-ul-Haq M, Afza N, Khan SB and Muhammad P.
Coumaroyl adenosine and lignan glycoside from Amaranthus
spinosus Linn. Polish Journal of Chemistry. 2006; 80: 259–263.
18. Kapadia G, Tokuda H, Harukuni K, Takao M and Nishino H.
Chemoprevention of lung and skin cancer by Beta vulgaris
(beet) root extract. Cancer Letters. 1996; 100: 211–214.
19. Berghofer E. and Schoenlechner R. Grain amaranth. In: Belton,
P.S., Taylor, J.R.N. (Eds.), Pseudocereals and Less Common
Cereals. Grain Properties and Utilisation Potential. Springer,
Berlin, Heidelberg, New York. 2002: 219–260.
20. Lin B, Chiang B and Lin J. Amaranthus spinosus water extract
directly stimulates proliferation of B lymphocytes in vitro.

172

International Immunopharmacology. 2005: 711– 722.
21. Cai Y, Sun M and Corke H. Antioxidant activity of
betalains from plants of the amaranthaceae. J Agric
Food Chem. 2003: 50-51.
22. Mandal M and Mukherji S. A study on the activities of a
few free radicals scavenging enzymes present in five
roadside plants. J Environ Biol. 2001: 301-305.
23. Olufemi BE, Assiak IE, Ayonde GO and Onigemo MA.
Studies on the effects of Amaranthus spinosus leaf
extract on the haematology of growing pigs. African
Journal of Biomedical Research. 2003; 6: 149-150.
24. Hussain Z, Amresh G and Singh S. Hepatoprotective
activity of Amaranthus spinosus in experimental
animals. Food Chem Toxicol. 2008; 22: 3417-21.
25. Satyanarayana T, Chowdary KA, Chinna Eswaraiah M.
and Bharathi A. Anti-Fertility Screening of Selected
Ethno Medicinal Plants. Phcog Mag. 2008; 4 (15): 51.
26. Sangameswaran B and Jayakar B. Anti-diabetic, anti-
hyperlipidemic and spermatogenic
Amaranthus spinosus Linn. on streptozotocin-induced
diabetic rats. Journal of Natural Medicines. 2008; 62(1):
79-82.
27. Cai Y, Sun M and Corke H. Antioxidant activity of
betalains from plants of the amaranthaceae. J Agric
Food Chem. 2003: 50-51.
28. O Sharma S, Kathuriaw PC, Guptaz CK, Nordling K,
Ghosh B and Singh AB. Total serum immunoglobulin E
levels in a case–control study in asthmatic/allergic
patients, their family members, and healthy subjects
from India. Clinical and Experimental Allergy. 2006;
36:1019–1027.
29. Sheeja K, Guruvayoorappan C and Kuttan G,
Antiangiogenic activity of Andrographis paniculata
extract and andrographolide. Int Immunopharmacol.
2007: 211-21.
30. Thisoda P, Rangkadilok
Worasuttayangkurn L. Ruchirawat S and Satayavivad J.
Inhibitory effect of Andrographis paniculata extract and
its active diterpenoids on platelet aggregation. Eur J
Pharmacol. 2006; 12 :39-45.

effects of
N, Pholphana N,