Achyranthes aspera Linn. (Amaranthaceae alt. Alternanthera)

Synonyms

Achyranthes indica (L.) Mill, Achyranthes obtusifolia Lam., Achyranthes futicosa, Centrostachys aspera, Standl., Cyathula geniculata, Lour., Desmochaeta repens, Llanos.

Vernacular Names:

Malaysia: No documentation
Indonesia: Jarong, Jarongan, Jarong Lalaki, Remek Getih, Daun Sangketan, Nyarang (Jawa), Sui In Sui, Sangko, Hidung (Sulawesi), Sai Rai, Dodinga (Maluku)
English: Rough Chaff Tree, Prickly Chaff Flower
Trinidad and tobago: Man Better Man [1]
India: Aparmarga (Ayurvedic), Apamarg (Sanskrit), Aghedo and Aghedi (Gujarati), Chirchira, Chirchitta (Hindi ), Uttarani, Kempu Uttarani(Kannada language), Naayuruvi (Tamil), Soh-berthid (Jaintia tribes), Poolaippoo, Abora, Mnyoli, Muyon, Nara
Ethiopia: Telenge, Ambulale, Mat'oya, T'elenji, Telenzje. [2],[3]
Pakistan: Puthkanda. [4]

General Information

Description

A perennial stiff erect herb, measuring 1-5 feet in tall with simple elliptic leaves, single green to pink ovate flower, small fruits (2.5-3mm) found throughout India, Africa, Asia and South America, generally in hot climates.  It is a common weed found on the way side and at waste lands. [5]

Achyranthes aspera is small, much branched, monoecious perennial subshrub up to 0.8-1 x 0.8m. Rootstock stout, woody. Stems somewhat succulent at first, ribbed, becoming basally woody with age, densely covered in velutinous, appressed hairs. Leaves opposite, densely clustered toward branch tips 45-50 x 25-30mm, spreading to decurved, mostly broadly ovate, ovate-orbicular or elliptic; apex blunt to abruptly sub acute, sometimes very shortly apiculate; base attenuate; lamina somewhat fleshy, purple-grey, veins often purple, abaxial and adaxial surfaces silky canescent, margins crenulate to crenate. Petioles 5-10mm long, pink, fleshy, velutinous, basal abscission zone present.  Inflorescence a terminal erect spike, 150-200mm long; peduncle 15mm long, fleshy, white-villous; spike rachis fleshy, white-villous to purple-villous; flowers bisexual, retrorse, sessile, c. 180-200 per spike, these spaced initially at 10-mm intervals along rachis, diminishing rapidly to <1-mm intervals toward inflorescence apex. [6]

The bract persistent on rachis, ovate to lanceolate 3-3.5 x 0.5-1mm, strongly retrorse, chartaceous, weakly keeled near apex only, pale white, margins entire, apex acute, sometimes with a small, 0.1-0.2mm long pale yellow mucro.  Bracteoles 2; abscissing with senescent flowers; broadly ovate, 0.2-1mm long, chartaceous hyaline, lustrous, pale caramel; margins entire; strongly keeled, keel lustrous, caramel brown, extending well beyond bract as a hardened, channelled, strongly recurved, falcate spine 4-5mm long.  Perianth segments (sepals) 5, lanceolate, central portion pale  caramel-brown but distinctly pink tinged, margins pale yellow or off-white opaque, hyaline; segments sub equal, 4.5-6mm, channelled.  Stamens 4, connate at base, the filaments 0.5-1mm, alternating with 4 narrowly spathulate, 0.4 x 0.6mm, white-hyaline, petaloid, fimbriate-margined pseudostaminodes; anthers 0.4-0.6mm, yellow, bilocular, dehiscing via longitudinal slits; pollen yellow.  Style 0.6-1mm, pink to pale orange, arising from a fleshy papillate style base 0.8mm diammetre; stigma brown, truncate.  Utricle 2-2.5mm long, dark brown, turbinate, hartaceous, surmounted by the dry, somewhat woody, style base. Seed 1.2-1.8 x 0.9-1.2mm, ovoid to ellipsoid, dark chestnut brown. [6]

Plant Part Used

Leaves, roots, twigs and seeds. [2]

Chemical Constituents

A. aspera contains a water-soluble base, betaine; a chloroform-soluble base which was a mixture of two uncharacterized alkaloidal entities. The ethanol extract contained alkaloids and saponins but were devoid of flavonoids and tannins.  The shoot contained an aliphatic dihydroxyketone, 36,47-dihydroxyhenpentacontan-4-one; tritriacontanol; an essential oil; a long chain alcohol, 17-pentatriacontanol; 27-cyclohexylheptacosan-7-ol; 16-hydroxy-26-methylheptacosan-2-one; 4-methylheptatriacont-1-en-10-ol and tetracontanol-2.  Ecdysterone was found in the seeds, stem, leaves and root.  Pentatriacontan, 6-pentatriacontanone, hexatriacontane and triacontane were isolated from the chloroform extract of the stem. Flavonoids and alkaloids were found in the inflorescence. [5]

The seeds contained protein with calorific value of 3.92/g, similar to Bengal gram in terms of amino acid contents of leucine, isoleucine, phenylalanine and valine while tryptophan and sulphur amino acid (methionine and cystine) contents were higher than in most pulses.  The seeds were deficient in arginine, lysine and threonine contents in comparison to whole egg protein. [5]  A saponin, oleanolic acid-oligosaccharide was found in defatted seeds with the sugar moiety being of glucose, galactose, xylose and rhamnose.  Two oleanolic acid based saponins, a-L-rhamnopyranosyl (1→4)-b-D-glucopyranosyl (1→4)-b-Dglucuronopyranosyl (1→3)-oleanolic acid and b-D-galactoyranosyl (1→28) ester saponin were found in the seeds. The genin was oleanolic acid. Theseeds contain hexatriacontane, 10-octacosanone and 10-triacosanone and 4-triacontanone. The unripe fruit contains saponins which were identified as b-D-glucopyranosyl ester of a-L-rhamnopyranosyl (1→4)-b-D-glucuronopyranosyl (1→3)-oleanolic acid and b-D-glucopyranosyl ester of a-L-rhamnopyranosyl (1→4)- b-D-glucopyranosyl (1→4) b-D-glucuronopyranosyl (1→3)- oleanolic acid, oleanolic acid and amino acids. [5],[7]  The unripe seeds contained oleanolic acid, oleanolic acid-based saponins and amino acids. [7]

The root contains oleanolic acid as the aglycone from the saponin, alkaloids but no flavonoids. Similarly, the shoots are devoid of flavonoids but contain saponins and alkaloids.  Others found alkaloids in the roots but no saponin and tannins while a  preliminary study showed the roots  to contain alkaloids, flavonoids, saponins, steroids and terpenoids but no glycosides.  b-Sitosterol was isolated from the root. [5]

The saponins from the MeOH extract of the aerial parts of A. aspera are b-D-glucopyranosyl 3b-[O-a-L-rhamnopyranosyl-(1→3)-O-b-D-glucopyranuronosyloxy]machaerinate, b-D-glucopyranosyl 3b-[O-b-D-galactopyranosyl-(1→2)-O-a-D-glucopyranuronosyloxy]machaerinate, b-D -glucopyranosyl 3b [O-a-l-rhamnopyranosyl-(1→3)-O-b-D-glucopyranuronosyloxy]oleanolate, b-D -glucopyranosyl 3-b-[O-b-D -galactopyranosyl-(1→2) -b-D-d-glucopyranuronosyloxy]oleanolate, b-D -glucopyranosyl 3b-[O-b-D -glucopyranuronosyloxy] oleanolate.  Machaerinic acid is 3b,21b-dihydroxyolean-12-en-28-oic acid while oleanolic acid is 3b-hydroxyolean-12-en-28-oic acid. [3]

The roots contained ecdysterone and oleanolic acid while the leaves and stems also contain ecdysterone.  Leaves and roots contained betaine type alkaloids or betalaine, while an aliphatic dihydroxyketone (36,47-dihydroxyhenpentacontan-4-one) was isolated from the shoots. [7]  The content of oleanolic acid in A. aspera root was found to be 0.054% as determined by dual-wavelength TLC-scanning. [8]

A. aspera powder contained high levels of manganese, magnesium, zinc, calcium and phosphorus in comparison to those of common vegetables and plants. [4]

Traditional Use:

A. aspera used in Chinese folk medicine as an antipyretic, an anti-inflammatory agent, a diuretic and for the treatment of constipation, fever (especially malarial fever), bronchitis, sprains, dysentery, asthma, hypertension, diabetes and as wound dressing. [3],[5],[7],[9],[10]  The whole plant is used in the treatment of diabetes and as a blood purifier. [4] The extract that is obtained by boiling A. aspera material is used by the Masai of Sekenani valley, Kenya, to treat malaria. [11]

The roots are used in infantile diarrhea and cold. [5],[10] The dry leaves are powdered and mixed with honey for use in the early stages of asthma while the seeds are used as an emetic. [5],[7]  The seeds, leaves and twigs have been used for treatment of renal dropsy and bronchial diseases. [4] The Chakma community in Arunachal Pradesh, India uses A. aspera to treat urinary disorders. [12]

It is an antifertility herb in Ethiopia where the leaf, root and seed extracts are used for antifertility effects, for placental retention and in postpartum bleeding. [2] In India, it is used as an abortifacient and for contraception besides for the treatment of renal dropsy, bronchial afflictions and leprosy.  In rural Indonesia, the extracted leaf juice is taken to prolong the duration between births while pregnant mothers are forbidden from taking the juice. [13] A. aspera is used by Latin American and Caribbean women for menstrual pain and unspecified female complaints.  It was given a level 3 validity based on the fulfillment of the following criterium: "If in addition to the ethnobotanical data, phytochemical or pharmacological information also validates the use in Trinidad, A. aspera may exert a physiological action on the patient and is more likely to be effective than those at the lowest level of validity". [1] In Trinidad, A. aspera is used for venereal diseases while in Nepal it is used to facilitate parturition. [1]

A. aspera is also believed to have cardiac stimulant, astringent, diuretic, antiperiodic and purgative actions. [5],[14]  It is also used as an  antiarthritic, estrogenic, antileprotic, antispasmodic, antibacterial and antiviral agent, for the treatment of asthmatic cough, snakebite, hydrophobia, urinary calculi, rabies, influenza, piles, renal dropsy, gonorrhea and abdominal pain. [5]

A paste of the leaves is applied topically to treat cuts and wounds. [15] The fresh leaves are chewed to treat herpes zoster. [16] The pills (1–2 g each) are made from the crushed leaves which are then applied on boils twice daily until healing occurs. [12] The people of the Coastal regions of Cape Comorin, India, use the plant to treat eye burns [12] The whole plant is dried and burnt to an ash which is then mixed with common salt and massaged onto the gums and tooth area to relieve toothache while the stem is used as a tooth brush. [17]

For veterinary purposes, the crushed leaves are used as a dressing to promote blood clotting. [16]

Pre-Clinical Data

Pharmacology

 Effects on thyroid hormones activity

 The leaf extract at 200 mg/kg body weight equivalent to 3 g/kg body weight of dry powder, given daily via oral dosing (p.o.) for 7 days caused a significant increase in serum T3 and T4 concentrations and the T3:T4 ratio in male rats. [14] These rats also showed significant increases in their body weights, hepatic protein content and serum glucose levels as compared to untreated rats.

 Antifertility activity

The methanolic extract of A. aspera leaves (3 and 5.5 g/kg body weight, p.o.) showed anti-fertility activity, with the higher dose significantly reducing the survival of rat fetuses.  A lower dose of the leaf methanolic extract (1 g/kg) significantly increased the uterine wet weight of bilaterally ovariectomized female rats and the pituitary wet weight of female rats although serum estradiol and progesterone concentrations remained unaffected. [2] The n-butanol fraction of the aerial parts of A. aspera (75 mg/kg dose, p.o.) prevented pregnancy in adult female rats when administered on days 1-5 post-coitum. [18] At the contraceptive dose, potent estrogenic activity was shown by the extract in ovariectomized immature female rats, with 100% uterine weight gain seen at 1/15th of this dose. Based on this, the estrogenic activity of the extract was calculated as 1/2750th that of ethinyl estradiol.  The extract (up to 300 mg/kg dose) was ineffective in hamsters. [18] Besides, no anti fertility activity was observed in rats or hamsters given the aqueous extract of the aerial parts. [5]

The single doses of the extracted leaf juice (3,10, 30 & 50%) were administered to female mice at 0, 24, 36 and 48 h after the appearance of vaginal plugs while the controls were given normal saline.  The leaf juice produced a dose-dependent reduction in the total number of zygotes starting from the 10% dose while 100% inhibition was elicited by the higher doses (30 and 50%).  Similarly, an increase in egg cell and embryo abnormalities were observed beginning from the 10% dose. [13]

The ethanol extract of the roots (200 mg/kg body weight, p.o., administered from days 1 through 7 of pregnancy) was 100% antifertility in female rats, showing both anti-implantation and abortifacient activities. The implantations were inhibited in 5 out of the 6 rats tested while the one animal that experienced implantation did not proceed to litter.  The effect of the extract was reversible as upon subsequent mating, all animals delivered normal litters.  The uterotrophic potency of the extract was about 95% that of ethinyl estradiol.  The extract significantly increased the uterine weight of immature rats and increased the uterus diameter, the endometrial thickness and epithelial cornification.  No anti-estrogenic activity was exhibited by the extract (200 mg/kg) upon concurrent administration with ethinyl estradiol (1 µg/rat/day). [19]

The whole plant, especially the benzene extract was abortifacient in mice with maximum activity observed at 50 mg/kg of body weight. [20] There were no estrogenic, antiestrogenic, or androgenic effects of the herb in the mice.  Abortion was not prevented by the co-administration of progesterone or pituitary extract.  Maximal abortifacient activity was located in the fraction eluted with 50 percent benzene in petroleum ether. [5]  The abortifacient activity of A. aspera may be specie-specific as the effect was not seen in rats given a 50 mg/kg dose on the 6th or 7th day of mating while oral administration of the extract (50 mg/kg) on the 8th day post-coitum in rabbits prevented pregnancy. [20]

The benzene extract (50 mg/kg, p.o.) of the stem bark of A. aspera showed 100% protection from pregnancy when administered at 1 or 6 days post-coitum in mice. The extract was equally effective in rabbits on day 8 of pregnancy.  The other extracts of the stem bark, i.e. the chloroform, alcohol and petroleum ether extract that were administered at 1 or 6 days post-coitum in mice were ineffective at preventing pregnancy with success ranging from 50% with the chloroform extract to less than 28% with the petroleum ether extract.  No anti-implantation activity was seen when the benzene extract was administered at 6-7 days post-coitum in rats.  A 50% ethanol extract (200 mg/kg) that was administered to rats at 1-7 days post-coitum was inactive. [21]

Inhibition of male reproductive ability activity

The 50% ethanolic extract elicited reproductive toxicity in male rats which may result from suppression of androgen synthesis. The treated rats had reduced sperm count, reduced weight of epididymis, reduced serum testosterone and reduced testicular 3b-hydroxysteroid dehydrogenase activity.  However, sperm motility and HMG CoA reductase activity were unaffected.  There were increases in the testicular cholesterol level, incorporation of labelled acetate into cholesterol, 17-ketosteroids in urine and hepatic and fecal bile acids. [22]

A composite plant extract which was composed of the 50% ethanolic extracts of Stephania hernandifolia (Menispermaceae) leaves and A. aspera roots (in a ratio of 1:3 by weight) showed potential contraceptive spermicidal activity in vitro. The extract (0.08-0.32 g/mL) slowed sperm motility in a concentration-dependent manner with the highest concentration causing total immobilisation of sperms within 2 min, probably by injuring the plasma membrane. The composite extract was spermicidal, sperms were killed after 30 min treatment with the highest concentration of 0.32 g/mL. [23]

Antihyperlipidemic activity and inhibition of liver lipid peroxidation activity

The alcoholic extract (100 mg/kg) showed anti-hyperlipidemic effect in triton-induced hyperlipidemic rats following acute or chronic administration for 30 days. [5] The total serum cholesterol, phospholipid, triglyceride and total lipids were significantly lowered following acute or chronic treatment while hepatic lipids were significantly lowered after chronic administration of the extract.  The mechanism was thought to involve rapid excretion of bile acids leading to lowered absorption of cholesterol.  Other investigators reported that the leaf methanolic extract (1 g/kg) showed a hypolipidemic effect on HDL but not on the other lipids [2] while male rats that were administered with the leaf extract (200 mg/kg, p.o.) daily for 7 days showed reduced lipid peroxidation in the liver. [14]

Antidiabetic activity

The powdered whole plant of A. aspera (2, 3 & 4 g/kg) and its water and methanol extracts (at doses equivalent to 4 g/kg) caused dose-dependent reductions in blood glucose levels in normal and alloxan diabetic rabbits with acetohexamide used as the standard antidiabetic drug.  The rapid hypoglycemic effect of A. aspera in both normal and alloxan-diabetic rabbits was attributed to its high content of elements. [4]

Antitumor promoter activity

A. aspera methanolic leaf extract, its alkaloid and the non-alkaloid fraction showed antitumor promoter activity as they significantly inhibited Epstein–Barr virus early antigen activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate in Raji cells. The non-alkaloid fraction which contained mainly non-polar compounds had the most significant inhibitory activity (96.9%; 60% viability) while the total methanolic extract showed pronounced anticarcinogenic effect (76%) in the in vivo two-stage mouse skin carcinogenesis model. [7] 

Immunostimulatory activity

Indian major carp, Catla catla which was fed with a diet that contained the seed extract of A. aspera (0.5%) experienced enhanced specific and non-specific immunity as revealed by higher serum antibody levels and higher serum anti-proteases than control fish. [10],[24]  The treated fish showed enhanced serum globulin levels and higher RNA/DNA ratio in the spleen and kidneys than the controls. [24] Besides showing significant enhancement of bovine serum albumin (BSA)-specific antibody titers at days 7, 14 and 21 post-immunization, fish that were fed a diet which contained the seed for 4 weeks showed more efficient antigen clearance than the controls as BSA was found in very low amounts on day 14, while at day(s) 21 and 28, the BSA particles were scarcely found. [10]

The administration of A. aspera extracts with ovalbumin (OVA) lead to enhanced induction of OVA-specific humoral antibody response in mice in a dose-dependent manner. There were significant elevations of IgM, IgG 1 and IgG 3 antibodies although the anti-OVA PCA titers were suppressed.  When tested in different strains of mice, the extract elicited significant elevations of the OVA-specific IgG antibody response in all strains.  The seed and root extracts showed relatively higher activity than extracts from the other plant parts. [5]

A. aspera (0.5%) that was incorporated into the diet also protected rohu (Labeo rohita) fingerlings from bacterial infection with A. hydrophilaA. aspera caused increased superoxide anion production and enhanced serum bactericidal activity and levels of lysozyme, alkaline phosphatase (ALP), serum protein, albumin:globulin ratio in comparison to controls.  Liver marker enzymes, aspartate transaminase and alanine aminotransferase, were low in the treated fingerlings as compared to the elevated levels seen in controls which also showed higher cumulative mortalities (77%) up to day 9 of infection.  In comparison, A. aspera showed a dose-dependent protection against the bacterial infection in L. rohita. [25] The serum antiproteases level of fish fed with a diet which contained the aqueous root extract of A. aspera was significantly enhanced compared to fish fed the control diet. [26] This indicates that A. aspera enhanced the non-specific immunity of the fish as antiproteases are components of the nonspecific immunity of vertebrates. Theimmunostimulatory activity of the root extract which was incorporated into the diet (0.5%) of rohu fish was also shown by feeding the fish the diet for 4 weeks followed by immunisation with chicken red blood cells.  The A. aspera-fed fish showed significantly higher spleen RNA/DNA ratio, higher antigen-specific antibody response and total serum globulin levels that the controls. [27]

Anti-inflammatory activity

 The ethanolic extract of A. aspera (100 - 500 mg/kg) showed anti-inflammatory and anti-arthritic activity as shown by significant inhibition of carrageenan and Freund's adjuvant-induced paw edema. [5],[28],[29]  The extract (125 - 500 mg/kg) produced a dose-dependent inhibition of carrageenan-induced rat paw edema with a median effective concentration (EC50) of 266 mg/kg body weight.  Extract doses of 375 and 500 mg/kg inhibited carrageenan-induced rat paw oedema at 3 h by 65 and 72%, respectively.  The same doses of the extract caused 40 and 45% reduction, respectively, in the granuloma weight of a subacute model of cotton pellet granuloma produced by implantation of sterile cotton in the axilla of albino male rats.  The standard antiinflammatory drug used was diclofenac sodium. [29]

Achyranthine, a water soluble alkaloid isolated from A. aspera, showed significant anti-inflammatory activity against carrageenan-induced foot oedema, granuloma pouch, formalin-induced arthritis and adjuvant arthritis in rats although the activity was less than those of phenylbutazone and betamethasone, standard antiinflammatory agents.  The significant reductions in the weights of the adrenal gland, thymus and spleen were produced by achyranthine while adrenal ascorbic acid and cholesterol contents were raised by it, effects that were similar to those of betamethasone, the standard drug.  The food intake was reduced although there was no significant effect on urinary and fecal output and mortality rate.  The achyranthine produced gastric ulcers with minimum incidence as compared to phenylbutazone and betamethasone which caused maximum incidence. [5]

A polyherbal preparation which consisted of 20% Rhus succidanea L, Acanthaceae (galls), 15% Solanum xanthocarpum Schood et Wender, Solanaceae (roots), 20% Tylophora indica Bum F., Asclepidiaceae (leaves), 25% Albizzia lebbeck Benth, Leguminoceae(bark), 5% Glycyrrhiza glabra L., Papilionaceae (roots) and 5% Achyranthes aspera L., Amaranthaceae (leaves) showed significant protection against bronchoconstriction that was induced by acetylcholine and histamine aerosols in guinea pigs. [30] The preparation also showed anti-anaphylactic activity.  The mechanisms involved mast cell stabilization, inhibition of pulmonary eosinophilia, H1 antihistaminic, antimuscarinic and direct sympathomimetic activities.

Antimicrobial activity

The achyranthine and the entire plant showed antibacterial activity against Staphylococcus aureus, Streptococuss heamolyticus and Bacillus typhosus.  The alcoholic and the aqueous extracts of the leaves were antibacterial against S. aureus and E. coli while the seeds showed antibacterial activity against B. subtilis, Pseudomonas cichorii and Salmonella typhimurium.  The 80 percent ethanolic extract of the leaves and stems (25 mg/ml) inhibited B. subtilis and S. aureus. [5]

The aqueous extract of the fresh leaves of A. aspera which was prepared by grounding the leaves with distilled water followed by lyophilisation did not produce any antibacterial effects against 10 different bacterial strains (Alkaligens viscolactis, Aeromonas hydrophilla, Cytophage species, Escherichia coli, Klebsiella aerogenas, Pseudomonas aeruginosa, Vibrio parahaemolytica, Vibrio damsela, Bacillus cereus, Streptococcus pyogens). [31]  In an earlier study, the aqueous leaf extract of A. aspera showed activity against P. vulgaris at high concentrations of 4000 and 5000 ppm. Similar results were reported with the aqueous flower extract. [32]

 Inhibition of angiotensin converting enzyme activity

The water, ethanol and acetone extracts of the whole plant did not exhibit appreciable angiotensin converting enzyme inhibitor (ACEI) activity in screening tests as the percentage inhibition of ACEI by these extracts were 11, 25 and 24%, respectively. [33]

Inhibition of mineralization and demineralization activity

A. aspera is a component of a herbal preparation known as Cystone (The Himalaya Drug Co., India).  Cystone contains A. aspera (16 mg/tablet) besides other herbs (Didymocarpus pedicellata, Saxifraga ligulata, Rubia cordifolia, Cyperus scariosus, Onosma bracteatum, Vernonia cinerea, purified Shilajeet, Hajrul yahood bhasma (prepared with Ocimum basilicum, Tribulus terrestris, Mimosa pudica, Dolichos biflorus, Pavonia odorata, Equisetum arvense, Tectona grandis seed).  The aqueous extract of Cystone, was antimineralisation as it was able to inhibit the initial deposition of Ca2+ and HPO42– ions to a matrix.  The aqueous extract also stimulated the demineralization of matrix-bound minerals. [34] These data provided some evidence of Cystone’s clinical uitility in treatment of kidney stones.

Diuretic activity

 The cystone (400 & 500 mg/kg, p.o.) produced a significant increase in urine volume and also significantly increased sodium, potassium and calcium excretion when given to rats. The total protein in the blood of the rats was significantly decreased by the higher dose (500 mg/kg, p.o.).  The effects produced by lower doses were slight or not significant [35]

Toxicities

A. aspera powdered plant, up to 8 g/kg orally, did not cause any adverse effects in an acute toxicity study in rabbits which were observed for a week after dosing. [4]

The ethanol extract (200 mg/kg body weight) of the roots showed no toxic effects in rats [19] although reproductive toxicity was seen in male rats given the 50% ethanolic extract. [22]  The benzene extract (50 mg/kg, p.o.) of the stem bark of A. aspera did not show estrogenic, anti-estrogenic or androgenic effects in mice although the n-butanol fraction of the aerial parts (75 mg/kg dose, p.o.) showed potent estrogenic activity in ovariectomized immature female rats. [18]

A single administration of A. aspera (1000 mg/kg of body weight) to mice did not cause toxicity.  Similarly, administration of a dose of 75 mg/kg every 21 days for 6 months to mice did not result in toxicity. [20],[21]  A. aspera (10 or 25 mg/kg) when fed to 15 mated female mice on day 6 of gestation, did not exhibit a teratogenic effect as 3 generations of the offspring showed no malformations. [20]

The alkaloid was isolated and subjected to acute, subacute and chronic toxicity testing in rats. The acute toxicity testing showed the alkaloid (6.0 mg/kg) to cause a slight increase in sedation and slight loss of righting reflex which was marked at 7.0 mg/kg. The higher doses caused significant loss of righting reflex, respiratory depression, increased sedation and diarrhea. The subacute toxicity testing (5.0 and 6.0 mg/kg) caused significant sedation and hypnosis, respiratory depression, and loss of righting reflex.  The higher dose caused increase in salivation and diarrhea.  Chronic administration with 3.0 mg/kg dose produced sedation and hypnosis, salivation, diarrhea, significantly depressed respiration and loss of body weight. [5]

The intraperitoneal administration of Cystone (500 mg/kg) did not cause toxicity as no deaths were seen within 24 h nor were there any changes in the heart rate or respiration. [35]

Genotoxicities and Mutagenicity Studies

No documentation

Clinical Data

Clinical Trials

Adverse Effects in Human:

Cardiovascular toxicity was reported in a 57 years old man who took more than 1000 mL of a decoction of A. aspera.  The man was found unconscious in his bathroom. Hypotension and bradycardia were present.  He recovered 4 d later after dopamine and supportive care without any further cardiac abnormalities. [36]

Use in Certain Conditions

Pregnancy / Breastfeeding

In rural Indonesia, pregnant mothers are cautioned against taking the herb due to its abortifacient effect. [13]

Age Limitations

Neonates / Adolescents

No documentation

Geriatrics

No documentation

Chronic Disease Conditions

No documentation

Interactions

Interactions with drugs

No documentation

Interactions with Other Herbs / Herbal Constituents

No documentation

Contraindications

Contraindications

No documentation

Case Reports

Use of Cystone in nephro-ureterolithiasis

Cystone showed promise as conservative remedy for urolithiasis as patients given this preparation showed significant reductions in oxalic acid and calcium excretion after one and two months, respectively while phosphorus excretion was significantly raised.  [37],[38]  In addition several patients voided stones during treatment with Cystone.  It is promoted as a safe and proven remedy for urolithiasis, crystalluria, urinary tract infections and in oedema and as a mild diuretic. [39]

The effectiveness of Cystone in nephro-ureterolithiasis was determined in 100 cases of the condition. Seventy-nine percent (19 of 25 cases) of the group of patients who were given Cystone (2 tablets 3 times a day for a period of 2 to 6 months and plenty of oral fluids passed the stone thus averting an operation while 24% (6 of 25 cases) had to be operated on.  In patients who were given a similar regiment of Cystone but were also put on forced diuresis (5% dextrose and dextrose saline and intermittent frusemide), there was an 80% response (20 out of 25 cases) in expelling stones while the rest (5 out of 25 cases) had to undergo surgery.  Of the nephrolithiasis patients who were given antispasmodics and oral fluids, 20% (5 out of 25 cases) expelled the stones, 80% (20 of 25 cases) underwent surgery.  About similar results were obtained in 25 cases of nephro-ureterolithiasis who were given antispasmodics and forced diuresis, only 7 cases (28%) responded to the treatment and 18 cases (72%) had to undergo surgery.  The effectiveness of Cystone was attributed to its diuretic and spasmolytic action, effect on crystalloid and colloid balance and its disintegrating action on the binding mucin. [40]

Twenty two urinary cases of renal calculus [2], ureteric calculus [6], vesical calculus [6], ureteric colic [2], cystitis [7], crystalluria [2], were treated with Cystone, 2 tablets thrice daily, for up to 3 months. The results showed that Cystone was effective at causing the expulsion of urinary stones of less than 0.5 cm in diameter and also relieves the burning sensation during micturition. [41]

 Use of Cystone in urinary disorders

Fifty patients with urinary disorders were given Cystone on a regiment of 2 tablets three times a day for 3 to 6 months and were followed up weekly. The urinary disorders were 25 cases of renal, ureteric and vesical calculi; 3 cases of crystalluria; 10 cases of cystitis; 2 cases of pyelitis; 3 cases of oedema due to nephritis and 7 cases of oedema due to cirrhosis of liver and tuberculosis.  One hundred percent recovery were obtained in all the cases except for the last as a patient who suffered from cirrhosis of liver and tuberculosis showed no improvement with Cystone.  None of the patients showed untoward toxic, short term or long term effects. [39]

Forty eight Indian stone formers experienced hyperoxaluria that was effectively controlled by Cystone (2 tablets, 3 times a day for 4-8 weeks with avoidance of oxalate-rich foods). [42]

 Use of A. aspera in the treatment of leprosy

 The 19 patients with positive stain smear were given an oral decoction of A. aspera.  The herb showed beneficial effects particularly in treatment of subacute and mild reactions in leprosy.  The concurrent administration of A. aspera decoction and the antileprosy drug diaminodiphenylsulphone (DDS) led to a decreased incidence of reactions and faster improvement without toxic effects. [5]

Use of ‘Kshaarasootra’ in the treatment of fistula-in-ano

‘Kshaarasootra’ is an Ayurvedic medicated thread which was prepared by coating with the latex of Euphorbia neriifolia, the alkaline powder of A. aspera and Curcuma longa.  A multicentric randomized controlled trial conducted in India on 265 patients with fistula-in-ano showed the thread to be efficacious in comparison to conventional surgery (237 patients) with better long term outcome as there was only 4% recurrence in the former group as compared to 11% recurrence in the latter when 150 patients from each group were followed for 1 year.  However, longer healing time of 8 weeks was observed with the thread as compared to 4 weeks following surgery. [5]

Use of A. aspera in the treatment of bronchial asthma

The 15 cases of bronchial asthma were treated three times a day with betel leaves which had been smeared with a preparation of A. aspera root in oil which was soaked in cow urine.  Symptoms of wheezing, gasping, dyspnoea, sneezing and cough disappeared in most cases, this was accompanied by a fall in total WBC, eosinophil counts and ESR. [5]

Read More

  1) Botanical Info

References

    1. Lans C. Ethnomedicines used in Trinidad and Tobago for reproductive problems. Journal of Ethnobiology and Ethnomedicine, 3:13, 2007.
    2. Shibeshi W, Makonnen E, Zerihun L, Debella A. Effect of Achyranthes aspera L. on fetal abortion, uterine and pituitary weights, serum lipids and hormones.  African Health Sciences, 6(2): 108-112, 2006
    3. Michl G, Abebe D, Bucar F, Debella A, Kunert O,  Schmid MG, Mulatu E, Haslinger E.  New triterpenoid saponins from Achyrantes aspera Linn.  Helvetica Chimica Acta, 83: 359-363, 2000.
    4. Akhtar MS & Iqbal J.  Evaluation of the hypoglycaemic effect of Achyranthes aspera in normal and alloxan-dibetic rabbits.  Journal of Ethnopharmacology,31: 49 – 57, 1991.
    5. Goyal BR, Goyal RK, Mehta AA.  Phyto-pharmacology of Achyranthes aspera : A Review.  Pharmacognosy Reviews, 1(1): Jan- May, 2007.
    6. De Lange PJ, Scofield RP, Greene T.  Achyranthes aspera (Amaranthaceae): A new indigenous addition to the flora of the Kermadec Islands group.  New Zealand Journal of Botany, 42: 167–17, 2004.
    7. Chakraborty A, Brantnera A, Mukainakab T, Nobukunib Y, Kuchideb M, Konoshimac T, Tokudab H, Nishinob H.  Cancer chemopreventive activity of Achyranthes aspera leaves on Epstein–Barr virus activation and two-stage mouse skin carcinogenesis.  Cancer Letters 177: 1–5, 2002.
    8. Li X, Hu S. [Determination of oleanolic acid in the root of Achyranthes bidentata Bl. from different places of production by TLC-scanning]. Zhongguo Zhong Yao Za Zhi. 20(8):459-60, 511; 1995.
    9. Leikin & Palouchek (eds). Poisoning & Toxicology Handbook, 4th Edition. p. 941
    10. Chakrabarti R, Vasudeva RY. Achyranthes aspera stimulates the immunity and enhances the antigen clearance in Catla catla.  International Immunopharmacology, 6: 782– 790, 2006.
    11. Bussmann RW, Gilbreath GG, Solio J, Lutura M, Lutuluo R, Kunguru K, Wood N,  Mathenge SG.  Plant use of the Maasai of Sekenani Valley, Maasai Mara, Kenya.  Journal of Ethnobiology and Ethnomedicine 2006.
    12. Sajem AL, Gosai K. Traditional use of medicinal plants by the Jaintia tribes in North Cachar Hills district of Assam, northeast India.  Journal of Ethnobiology and Ethnomedicine, 2:33, 2006.
    13. Wurlina dan Sastrowardoyo W.  Pengaruh perasan Achyranthes aspera Linn. terhadap perkembangan embrio (cleavage) mencit (Mus musculus).  Jurnal Penelitian Medika Eksakta, 3(3): 264-273, 2002.
    14. Tahiliani P and Kar A. Achyranthes aspera elevates thyroid hormone levels and decreases hepatic lipid peroxidation in male rats.  Journal of Ethnopharmacology, 71: 527–532, 2000.
    15. Muthu C, Ayyanar M, Raja N, Ignacimuthu S.  Medicinal plants used by traditional healers in Kancheepuram. District of Tamil Nadu, India.  Journal of Ethnobiology and Ethnomedicine, 2:43,  2006. doi:10.1186/1746-4269-2-43.
    16. Teklehaymanot T and Giday M.  Ethnobotanical study of medicinal plants used by people in Zegie Peninsula, Northwestern Ethiopia.  Journal of Ethnobiology and Ethnomedicine, 3:12, 2007.
    17. Hebbar SS, Harsha VH, Shripathi V, G.R. Hegde GR.  Ethnomedicine of Dharwad district in Karnataka, India - plants used in oral health care.  Journal of Ethnopharmacology 94: 261–266, 2004.
    18. Wadhwa V, Singh MM, Gupta DN, Singh C, Kamboj VP. Contraceptive and hormonal properties of Achyranthes aspera in rats and hamsters. Planta Med. 52(3):231-3, 1986.
    19. Vasudeva N and  Sharma SK.  Post-coital antifertility activity of Achyranthes aspera Linn. root.  Journal of Ethnopharmacology 107:179–181, 2006.
    20. Pakrashi A, Bhattacharya N. Abortifacient principle of Achyranthes aspera Linn.  Indian J Exp. Biol., 15(10):856-8, 1977.
    21. Kamboj VP,  Dhawan BN. Research on plants for fertility regulation in India. Journal of Ethnopharmacology, 6: 191–226: 1982.
    22. Sandhyakumary K, Boby RG, Indira M. Impact of feeding ethanolic extracts of Achyranthes aspera Linn. on reproductive functions in male rats. Indian J Exp Biol. 40(11):1307-9, 2002.
    23. Paul D, Bera S, Jana D, Maiti R, Ghosh D. In vitro determination of the contraceptive spermicidal activity of a composite extract of Achyranthes aspera and Stephania hernandifolia on human semen. Contraception 73:284–288, 2006.
    24. Vasudeva RY, Chakrabarti R. Stimulation of immunity in Indian major carp Catla catla with herbal feed ingredients.  Fish & Shellfish Immunology, 18: 327-334, 2005.
    25. Rao YV, Das BK, Jyotyrmayee P, Chakrabarti R. Effect of Achyranthes aspera on the immunity and survival of Labeo rohita infected with Aeromonas hydrophila.  Fish & Shellfish Immunology 20: 263-273, 2006.
    26. Rao YV,  Chakrabarti R. Enhanced anti-Proteases in Labeo Rohita fed with diet containing herbal ingredients.  Indian Journal of Clinical Biochemistry, 19(2): 132-134, 2004.
    27. Rao YV,Romesh M, Singh A, Chakrabarti R. Potentiation of antibody production in Indian major carp Labeo rohita, rohu, by Achyranthes aspera as a herbal feed ingredient. Aquaculture, 238: 67–73,2004b.
    28. Gokhale AB, Damre AS, Kulkami KR, Saraf MN.  Preliminary evaluation of anti-inflammatory and anti-arthritic activity of S. lappa, A. speciosa and A. asperaPhytomedicine, 9(5): 433-7, 2002.
    29. Vetrichelvan T and Jegadeesan M. Effect of alcohol extract of Achyranthes aspera Linn. on acute and subacute inflammation. Phytother. Res. 17,77–79,2003.
    30. Shah GB and  Parmar NS.  Antiasthmatic property of polyherbal preparation E-721 B.  Phytother. Res. 17, 1092–1097, 2003.
    31. Samy RP, Ignacimuthu S, Raja DP. Preliminary screening of ethnomedicinal plants from India. Journal of Ethnopharmacology, 66: 235–240, 1999.
    32. Samy RP, Ignacimuthu S, Sen A. Screening of 34 Indian medicinal plants for antibacterial properties. Journal of Ethnopharmacology 62: 173–182, 1998.
    33. Nyman U,Joshi P,  Madsen LB, Pedersen TB, Pinstrup M, Rajasekharan S,  George V, Pushpangadan P.  Ethnomedical information and in vitro screening for angiotensin-converting enzyme inhibition of plants utilized astraditional medicines in Gujarat, Rajasthan and Kerala (India). Journal of Ethnopharmacology, 60:247–263, 1998.
    34. Jethi RK, Duggal B, Sahota RS, Gupta M, Sofat IB.  Effect of the aqueous extract of an Ayurvedic compound preparation on mineralization and demineralization reaction.  Indian Journal of Medical Research, 78: 422-425, 1983.
    35. Phukan DP,Deka A, Choudhury AK. Pharmacological and clinical study on Cystone.  Probe XVII (1): 25-29, 1977.
    36. Han ST, Un CC. Cardiac toxicity caused by Achyranthes aspera.  Vet Hum Toxicol., 45(4):212-3, 2003.
    37. Singh PP, Pendse AP, Goyal A, Ghosh R, Srivastava AK and Kumawat JL.  Blood and urine chemistry of stone formers in local population and evaluation of Cystone treatment.  Indian Drugs, 7: 264, 1983.
    38. Singh PP, Singh NB, Singh LBK.  Effect of Cystone treatment on urinary excretion of calcium, oxalic acid and uric acid in stone-formers.  The Antiseptic, 30(5): 234, 1983b.
    39. Chatterjee BN.  Role of Cystone in various urinary disorders.  Probe: XXII(1): 27-30, 1982.
    40. Misgar MS.  Controlled trial in 100 cases with nephro-uretero-lithiasis by Cystone - An indigenous drug and other advocated methods. Current Medical Practice, (1982): May.
    41. Gupta PD & Singh LM.  A clinical trial of Cystone tablets in the treatment of various urinary disorders .  Probe, XV(2): 108-112, 1976.
    42. Pendse AK, Ghosh R, Goyal A, Singh PP.  Effect of indigenous drugs on idiopathic hyperoxaluria in stone formers.  Asian Medical Journal,2: 136, 1984.