Ethnobotanical, pharmacological and phytochemical  review on Butea monosperma Linn

 

1Chandan Das*, 2Sujit Dash, 3Durga Charan Sahoo, 1Arnabaditya Mohanty

1The Pharmaceutical College, Samaleswari Vihar, Tingipali, Barpali, Bargarh-768 029, Odisha. India.

2Institute of Pharmacy and Technology, Salipur, Cuttack-754 202, Odisha. India.

3Dadhichi College of Pharmacy, Vidya Vihar, Sundargram, Cuttack-754 002, Odisha, India.

 

ABSTRACT:

Butea monosperma, a popular Indian medicinal plant, has long been used in Ayurvedic system of medicine. In sanskrit it is called as ‘Palasa’. The plant has been found to possess diverse number of pharmacological activities. The present paper gives an account of  updated information on its phytochemical and pharmacological activities. The review reveals that wide range of phytochemical constituents have been isolated from the plant and it possess important activities like diarrhoea, dysentery, inflammation, ringworm, aphrodisiac, anthelmentic, tumor, piles and ulcer, cold, cough, menstrual disorder, analgesic and diuretic. Various other activities like hepatoprotective, osteoprotective, anti-inflammatory, antihyperglycemic, antifilaria, antioxidant, anthelmentic, antimicrobial, anticonvulsant, antifertility and aphrodisiac been reported. These reports are very encouraging and indicate that herb should be studied more extensively for its therapeutic benefits.

 

KEYWORDS: Butea monosperma, ethnobotanical, phytoconstituents and pharmacological activities

 

INTRODUCTION:

A deciduous tree with a somewhat crooked trunk, up to 15 m in height and 1.6-2.0 m (sometimes up to 3.8 m) in girth; commonly found throughout India, except in the arid regions. Bark bluish grey or light brown; leaves long-petiole, 3-foliate, leaflets coriaceous, broadly obovate from a cuneate or deltoid base, glabrescent above, densely finely silky below; flower buds dark brown, flowers bright orange-red, sometimes yellow, in 15 cm long racemes on bare branches; pods pendulous, silky-tomentose, 10-13 cm long, containing one seed at its apex; seeds flat, reniform, 3.3-3.8 cm X 2.2-2.5 cm. The fresh juice (gum) is applied to ulcers and in relaxed, congested, and septic sore throat. The gum is powerful astringent; it is given internally for diarrhea and dysentery, phthisis and haemorrhage from stomach and bladder; its infusion is occasionally employed as a local application in leucorrhoea. A solution of gum is applied to bruises and erysipelatous inflammation and ringworm. The bark is reported to possess astringent, bitter, pungent, alternative, aphrodisiac and anthelmintic properties It is useful in tumour, bleeding piles and ulcer. The decotion is prescribed in cold, cough, fever, various form of haemorrhage, in menstrual disorders and in the preparation of tonics and elixirs. The roots are useful in elephantiasis and in curing night blindness and other defects of sight The root bark is used as an aphrodisiac and as analgesic and anthelmintic. It is also applied in sprue, piles, ulcers, tumours and dropsy The leaves are used as astringent, tonic, diuretic and aphrodisiac properties. They are used to cure boils, pimples and tumours haemorrhoids and are internally given in flatulent colic, worm and pile.

 

 

 


The flowers are reported to possess astringent, diuretic, depuretive, aphrodisiac and tonic properties; they are used as an emmenagogue, and as poultice in orchitis and to reduce swellings, for bruises and sprains. They are also effective in leprosy, leucorrhoea and gout. Seeds are reported to possess aperient and rubefacient properties. A decotion of the seeds is given in gravel1.

 

PHARMACOLOGICAL STUDY

Hepatoprotective activity

Hepatoprotective activity was evaluated by taking aqueous extract of flowers of B. monosperma (Fabaceae) at different dose levels (200, 400, 800mg/kg, p.o.) for its protective efficacy against CCl4 (1.5ml/kg i.p.) induced acute liver injury to validate its use in traditional medicines. The CCl4 administration altered various biochemical parameters, including serum transaminases, protein, albumin, hepatic lipid peroxidation, reduced glutathione and total protein levels, which were restored towards control by therapy of B. monosperma Adenosine triphosphatase and glucose-6-phosphatase activity in the liver were decreased significantly in CCl4 treated animals. Therapy of B. monosperma showed its protective effect on biochemical and histopathological alterations at all the three doses in dose dependent manner. B. monosperma extract possess modulatory effect on drug metabolizing enzymes as it significantly decreased the hexobarbitone induced sleep time and increased excretory capacity of liver which was measured by BSP retention. Histological studies also supported the biochemical finding and maximum improvement in the histoarchitecture was seen at higher dose of BM extract2.

 

In the present study the alcoholic extract of B. monosperma used seems to offer dose-dependent protection and maintain the structural integrity of hepatic cells. Thioacetamide (TAA) was used to induce tumor promotion response and oxidative stress and caused significant depletion in the detoxification and antioxidant enzyme armory with concomitant elevation in malondialdehyde (MDA) formation, hydrogen peroxide (H2O2) generation, ornithine decarboxylase (ODC) activity and unscheduled DNA synthesis. B. monosperma pretreatment at two different doses restored the levels of the above-said parameters (p < 0.001) in a dose-dependent manner. This was evident from the significant reduction in TAA-induced serum GOT, GPT, Lactate dehydrogenase (LDH) and gamma-Glutamyl transpeptidase activity (GGT) activities (p < 0.001). These investigations validate the use of B. monosperma in liver disorders by Ayurvedic physicians. Overall results indicate that the methanolic extract of B. monosperma possesses hepatoprotective effects and also it might suppress the promotion stage via inhibition of oxidative stress and polyamine biosynthetic pathway3.

 

Hepatic carcinogenesis property

The effects of Butea monosperma extract on hepatic carcinogenesis and on tumor promoter induced markers and oxidative stress in male Wistar rats was carried out. Treatment of male Wistar rats for five consecutive days with 2-AAF i.p. induced significant hepatic toxicity, oxidative stress and hyperproliferation. Pretreatment of B. monosperma extract (100 and 200 mg/kg body weight) prevented oxidative stress by restoring the levels of antioxidant enzymes and also prevented toxicity at both doses. The promotion parameters induced (ornithine decarboxylase activity and DNA synthesis) by 2-AAF administration in diet with partial hepatectomy (PH) were also significantly suppressed dose dependently by B. monosperma. Thereafter, we proceeded with studies on rat liver carcinogenesis. After fourteen days of DEN treatment, dietary administration of 2-AAF with PH resulted in a 100% incidence of tumors in the animals. B.monosperma caused reduction in the number of tumors rat and percentage of tumor bearing rats at the end of the study, as confirmed histologically. B. monosperma extract is a potent chemopreventive agent which suppresses 2-AAF-induced hepatic carcinogenesis and oxidative damage in Wistar rats. The protective activity of the plant might be due to the two major constituents (butrin and isobutrin)4.

 

Osteoprotective activity

The skeletal effects of Butea total extract (BTE) and its acetone soluble fraction (ASF) from B. monosperma, which is rich in methoxyisoflavones, was studied on ovariectomized (OVx) rats, a model for postmenopausal bone loss. BTE (1.0 g kg d) and ASF (100 mg kg d) were given orally for 12 weeks to adult OVx rats. The sham-operated and ovariectomy + vehicle groups served as controls. Bone mineral density, osteoid formation (mineral apposition rate and bone formation rate), bone microarchitecture, and bone turnover/resorption markers were studied. Phytoestrogens in rats given BTE and ASF were analyzed by high-performance liquid chromatography. One-way analysis of variance was used to test significance of effects. OVx rats treated with either BTE or ASF exhibited increased bone mineral density in trabecular bones and improved trabecular microarchitecture compared with the ovariectomy + vehicle group. ASF treatment was more efficient than BTE treatment in maintaining trabecular microarchitecture. Serum osteocalcin and urinary type 1 collagen levels in OVx rats treated with either BTE or ASF were significantly lower than those of the ovariectomy + vehicle group. ASF treatment led to increased mineral apposition rate and bone formation rate compared with ovariectomy + vehicle, whereas BTE had no such effect. In the uterotropic assay, BTE was mildly estrogenic in adult OVx rats. In immature rats, BTE exhibited both estrogenicity and antiestrogenicity. ASF had neither uterine estrogenicity nor antiestrogenicity. Analysis of phytoestrogens revealed significant enrichment of cladrin, isoformononetin, and medicarpin in ASF over BTE. Derived from B monosperma, ASF at a 10-fold lower dose than that of BTE was effective in preventing OVx-induced bone loss and stimulated new-bone formation5.

 

Cajanin and isoformononetin obtained from stem-bark extract of B. monosperma, two structurally related methoxyisoflavones were studied for their effects in osteoblasts. Cajanin had strong mitogenic as well as differentiation-promoting effects on osteoblasts that involved subsequent activation of MEK-Erk and Akt pathways. On the other hand, isoformononetin exhibited potent anti-apoptotic effect in addition to promoting osteoblast differentiation that involved parallel activation of MEK-Erk and Akt pathways. Unlike genistein or daidzein, none of these two compounds appear to act via estrogen receptors in osteoblast. Once daily oral (by gavage) treatment for 30 consecutive days was given to recently weaned female Sprague-Dawley rats with each of these compounds at 10.0 mg kg(-1) day(-1) dose. Cajanin increased bone mineral density (BMD) at all skeletal sites studied, bone biomechanical strength, mineral apposition rate (MAR) and bone formation rate (BFR), compared with control. BMD levels at various anatomic positions were also increased with isoformononetin compared with control however, its effect was less potent than cajanin. Isoformononetin had no effect on the parameters of bone biomechanical strength although it enhanced MAR and BFR compared with control. Isoformononetin had very mild uterotrophic effect, whereas cajanin was devoid of any such effect. Our data suggest that cajanin is more potent than isoformononetin in accelerating peak bone mass achievement. To the best of our knowledge, this work represents the first attempt to elucidate structure-activity relationship between the two methoxylated isoflavones regarding their effects in osteoblasts and bone formation6.

 

Anticancer activity

Dried flowers of B. monosperma were extracted with water. The extract was tested for its anti-proliferative, pro-apoptotic and anti-carcinogenic effects in hepatoma cell lines. The chemopreventive and anti-angiogenic effects of the extract were evaluated by its daily oral administration in a HBV-related X15-myc mouse model of hepatocellular carcinoma (HCC). Treatment with the aqueous extract inhibited cell proliferation and accumulation of cells in G1 phase. This was accompanied by a marked reduction in the levels of activated Erk1/2 and SAPK/JNK and induction of apoptotic cell death. Oral administration of the extract in transgenic mice conferred hepatoprotection as is evident from normal serum ALT levels and improved liver histopathology and lowered serum VEGF level. The ability of aqueous extract of B. monosperma flowers to impose growth arrest and trigger pro-apoptotic death in cell culture strongly correlated with its strong chemopreventive effect in vivo when given orally7.

 

Butein, a flavonoid is isolated from the bark of Rhus verniciflua Stokes and the flowers of B. monosperma, which is known to be a potential therapeutic drug for treating inflammation and cancer. This study examined the potential suppressive effect of the flavonoid on phorbol 12-myristate 13-acetate (PMA)-induced COX-2 expression in the non-tumorigenic MCF-10A and cancerous MCF-7 breast cells. Immunoblot and mRNA analyses revealed that butein at or below 10 μM significantly inhibited PMA-induced COX-2 expression in these breast cells. The blocking of the PKC signaling pathway appeared to be the underlying mechanism. Butein treatment reduced the amount of phospho-mitogen activated protein kinase (MAPK) ERK-1/2, and the total activity of PKC. Activated ERKs might trigger the transcriptional activation of COX-2. Reporter gene assays as well as electrophoretic mobility shift assays (EMSA) illustrated that butein inhibited transcription of this gene. This study showed that butein down-regulated PMA-induced COX-2 expression in both cancerous and non-cancerous breast cells, and such findings could provide the basis for pharmaceutical development of butein8.

 

Anti-inflammatory activity

Polyphenols--butrin, isobutrin, isocoreopsin, and butein--were isolated from BME by preparative thin layer chromatography and their purity and molecular weights were determined by liquid chromatography/mass spectrometry analysis. The results showed that butrin, isobutrin, and butein significantly reduced the phorbol 12-myristate 13-acetate and calcium ionophore A23187-induced inflammatory gene expression and production of TNF-alpha, IL-6, and IL-8 in HMC-1 cells by inhibiting the activation of NF-kappaB. In addition, isobutrin was most potent in suppressing the NF-kappaB p65 activation by inhibiting IkappaBalpha degradation, whereas butrin and butein were relatively less effective. In vitro kinase activity assay revealed that isobutrin was a potent inhibitor of IkappaB kinase complex activity. This is the first report identifying the molecular basis of the reported anti-inflammatory effects of BME and its constituents butrin, isobutrin, and butein. The novel pharmacological actions of these polyphenolic compounds indicate potential therapeutic value for the treatment of inflammatory and other diseases in which activated mast cells play a role9.

The anti-inflammatory activity was studied by taking methanolic extract of B. monosperma flowers (MEBM) against carrageenan induced paw edema and cotton pellet granuloma in albino rats. In carrageenan induced paw edema, MEBM at oral doses of 600 mg/kg and 800 mg/kg, dose-dependently inhibited the paw edema. In cotton pellet induced granuloma, MEBM at the same doses was found to significantly inhibit granuloma tissue formation, including significant reduction in levels of serum lysosomal enzymes (SGOT, SGPT and ALP) and lipid peroxides as compared to control10.

 

Antihyperglycemic activity

Antihyperglycemic activity was evaluated on flowers of B. monosperma. Daily treatment of alloxan-induced diabetic animals with 50% ethanolic extract of B. monosperma flowers (BMEE) for 45 days significantly lowered blood glucose level thereby preventing steep onset of hyperglycemia which was observed after alloxan administration and maintained body weight and blood glucose level close to the values observed in normal control and glibenclamide-treated diabetic mice. Moreover, the level of serum total cholesterol, triglyceride, low-density lipoprotein and very low-density lipoprotein cholesterol were also lowered, whereas the level of high-density lipoprotein cholesterol, which was reduced in untreated diabetic animals, was significantly elevated. Oxidative damage in the liver, pancreas and kidneys of diabetic mice as evidenced by a marked increment in the level of thiobarbituric acid reactive substances and also a distinct diminution in glutathione content was nullified by BMEE. Activities of antioxidant enzymes were also assessed in all the experimental groups. These enzymes registered a decline in their activity in diabetic animals thus revealing the damaging effects of free radicals generated due to alloxan exposure but their activities were reverted towards near normal range in BMEE-administered mice thus indicating the antioxidant efficacy of the drug in resisting oxidative damage11.

 

Protective effect of ethanolic extract of B. monosperma leaves (BMEE) was evaluated on diabetes and diabetes-induced oxidative stress was in alloxan (ALXN)-induced diabetic male adult mice. Experimental animals were divided into three groups viz., I, II, and III. Diabetes mellitus (DM) was induced in groups II and III mice by a single intraperitoneal injection of alloxan (150 mg/kg body wt). Group I (control mice) received an equal volume of normal saline. Group III mice were further treated with BMEE (300 mg/kg body wt, p.o.) for a period of 45 days. Body weight and fasting blood glucose (FBG) levels were measured at periodic intervals during the test period. At the end of treatment period, blood was collected by cardiac puncture under mild ether anesthesia and serum was isolated to analyze its lipid profile i.e. serum total cholesterol (TC), triglyceride (TG), high density lipoprotein (HDL), low density lipoprotein (LDL) and very low density lipoprotein (VLDL). The homogenates of hepatic, pancreatic and renal tissues were also analyzed for both enzymatic and non-enzymatic antioxidants, such as superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), reduced glutathione (GSH), thiobarbituric acid reactive substances (TBARS) and total protein (TP). Alloxan injection resulted in a significantly (P < 0.05) increased concentration of FBG level. Besides, the levels of enzymatic and nonenzymatic antioxidants were decreased and TBARS level increased significantly (P < 0.05) in hepatic, pancreatic and renal tissues. Also, serum TC, TG, LDL and VLDL-cholesterol level elevated significantly (P < 0.05), whereas HDL-cholesterol reduced significantly (P < 0.05) in group II (alloxan-treated diabetic control). The FBG level decreased significantly (P < 0.05) after 45 days treatment of BMEE from 172 to 117.143 mg/dl, as compared to normal control (79.286 mg/dl). The activities of antioxidant enzymes (CAT and GSH-Px) and GSH level in hepatic, pancreatic and renal tissues also increased significantly (P < 0.05) in BMEE-treated mice, but the activity of SOD was not improved significantly. BMEE treatment also reduced the TBARS levels and lowered serum lipid profile significantly (P < 0.05). The findings of the present study indicated significant hypoglycemic and anti-oxidant activity in B. monosperma leaves, thus lends credence to its folklore use in the management and/or control of type-2 DM12.

The oral administration of the ethanolic extract of the B. monosperma seeds (300 mg/kg b.w.) exhibited significant antidiabetic, hypolipaemic and antiperoxidative effects in non-insulin dependent diabetes mellitus rats13.

 

The antihyperglycemic activity of the ethanolic extract of Butea monosperma (BMEE) was studied in glucose-loaded and alloxan-induced diabetic rats. Single dose treatment of BMEE (200 mg/kg, p.o.) significantly improved glucose tolerance and caused reduction in blood glucose level in alloxan-induced diabetic rats. Repeated oral treatment with BMEE (200 mg/kg/day) for 2 weeks significantly reduced blood glucose, serum cholesterol and improved HDL-cholesterol and albumin as compared to diabetic control group14.

 

Antifilarial activity 

The in vitro antifilarial effect of four herbal plants was screened on Brugia malayi. Motility of microfilariae of B. malayi after incubation for 48 h with aqueous/methanol extracts of Vitex negundo L. (roots), B. monosperma L. (roots and leaves), Ricinus communis L. (leaves), and Aegle marmelos Corr. (leaves) was explored in the concentration range of 20 to 100 ng/ml for possible antifilarial effect by comparing with suitable solvent control. B. monosperma leaves and roots, Vitex negundo root and Aegle marmelo leaves showed significant inhibition of motility of microfilariae as compared to controls whereas inhibitory activity demonstrated by Ricinus communis L. leaves was not significant. Antifilarial effects imparted by all these extracts were found to be a function of their relative concentrations. Inhibitory concentrations (IC (50)) for the plant extracts with significant antifilarial activity against Brugia malayi microfilariae in in vitro system have been derived to be 82, 83 and 70 ng/ml for Vitex negundo L., B. monosperma L. and Aegle marmelos Corr. respectively. The present study recorded significant antifilarial effect of all plant extracts studied except for Ricinus communis L. leaves and contributes to the development of database for novel drug candidates for human lymphatic filariasis15.

 

Antioxidant activity

Free radical scavenging activities were evaluated by using ethyl acetate, butanol and aqueous fractions derived from total methanol extract of B. monosperma flowers for using different in vitro models like reducing power assay, scavenging of 2,2 diphenyl-1-picrylhydrazyl (DPPH) radical, nitric oxide radical, superoxide anion radical, hydroxyl radical and inhibition of erythrocyte hemolysis using 2, 2' azo-bis (amidinopropane) dihydrochloride (AAPH). Methanol extract along with its ethyl acetate and butanol fractions showed potent free radical scavenging activity, whereas aqueous fraction was found to be devoid of any radical scavenging properties. The observed activity could be due to the higher phenolic content in the extracts (16.1, 25.29, and 17.74% w/w in methanol extract, ethyl acetate and butanol fractions respectively). HPTLC fingerprint profile of the ethyl acetate and butanol fractions were developed which would serve as reference standard for quality control of the extracts16.

 

Anthelmintic activity

Seeds of B. monosperma administered as crude powder (CP) at doses of 1, 2 and 3 g/kg to sheep naturally infected with mixed species of gastrointestinal nematodes exhibited a dose and a time-dependent anthelmintic effect. The maximum reduction of 78.4% in eggs per gram of feces (EPG) was recorded on day 10 after treatment with 3 g/kg. Levamisole (7.5 mg/kg), a standard anthelmintic agent, exhibited 99.1% reduction in EPG17.

 

The methanol extract of B. monosperma seeds, tested in vitro, showed significant anthelmintic activity18.

 

Anti-diarrhoeal activity 

The anti-diarrhoeal potential of the ethanolic extract of stem bark of B monosperma (Lam) Kuntz was evaluated by using several experimental models in Wistar albino rats. The extract inhibited castor oil induced diarrhoea and PGE (2) induced enteropooling in rats; it also reduced gastrointestinal motility after charcoal meal administration. The results obtained establish the efficacy and substantiate the use of this herbal remedy as a non-specific treatment for diarrhoea in folk medicine19.

 

Wound healing activity 

The present investigation was undertaken to determine the efficacy of topical administration of an alcoholic bark extract of B. monosperma   on cutaneous wound healing in rats. Full-thickness excision wounds were made on the back of rat and B. monosperma extract was administered topically. The granulation tissue formed on days 4, 8, 12 and 16 (post-wound) was used to estimate total collagen, hexosamine, protein, DNA and uronic acid. The extract increased cellular proliferation and collagen synthesis at the wound site, as evidenced by increase in DNA, total protein and total collagen content of granulation tissues. The extract treated wounds were found to heal much faster as indicated by improved rates of epithelialization and wound contraction, also confirmed by histopathological examinations. Also, the tensile strength of drug-treated wounds was increased significantly. In addition, we show that B. monosperma possesses antioxidant properties, by its ability to reduce lipid peroxidation. The results clearly substantiate the beneficial effects of the topical application of B. monosperma in the acceleration of wound healing20.

 

Antimicrobial activity 

Fifty four plant extracts (methanol and aqueous) were assayed for their antimicrobial activity against multi-drug resistant Salmonella typhi. Strong antibacterial activity was shown by the methanol extracts of Aegle marmelos, Salmalia malabarica, Punica granatum, Myristica fragrans, Holarrhena antidysenterica, Terminalia arjuna and Triphal (mixture of Emblica of ficinalis, Terminalia chebula and Terminalia belerica). Moderate antimicrobial activity was shown by Picorhiza kurroa, Acacia catechu, Acacia nilotica, Cichorium intybus, Embelia ribes, Solanum nigrum, Carum copticum, Apium graveolens, Ocimum sanctum, Peucedanum graveolens and Butea monosperma21.

 

The antimicrobial efficiency of seed oil of B. monosperma was studied by the filter paper disk method against several human pathogenic bacteria and fungi. The oil showed a significant bactericidal and fungicidal effect22.

 

Anticonvulsant activity 

The petroleum ether extract was fractionated by column chromatography using solvents of varying polarity such as n-hexane, n-hexane:ethyl acetate, ethyl acetate, and methanol. The anticonvulsive principle of B. monosperma was found to be a triterpene (TBM) present in the n-hexane:ethyl acetate (1:1) fraction of the petroleum ether extract. TBM exhibited anticonvulsant activity against seizures induced by maximum electroshock (MES) and its PD (50) was found to be 34.2+/-18.1 mg/kg. TBM also inhibited seizures induced by pentylenetetrazol (PTZ), electrical kindling, and the combination of lithium sulfate and pilocarpine nitrate (Li-Pilo). However, TBM was not effective against seizures induced by strychnine and picrotoxin. TBM exhibited depressant effect on the central nervous system. After repeated use for 7 days, the PD (50) (MES) of TBM increased to 51.5+/-12.1 mg/kg. Similarly, after repeated use of TBM, the duration of sleep induced by pentobarbital was not reduced significantly. Further studies are required to investigate its usefulness in the treatment of epilepsy23.

 

The ethanolic extracts of leaves of Albizzia lebbeck and flowers of Hibiscus rosa sinesis and the petroleum ether extract of flowers of B. monosperma exhibited anticonvulsant activity. The bioassay guided fractionation indicated that the anticonvulsant activity lies in the methanolic fraction of chloroform soluble part of ethanolic extract of the leaves of A. lebbeck, acetone soluble part of ethanolic extract of H. rosasinesis flowers and acetone soluble part of petroleum ether extract of B. monosperma flowers. The fractions protected animals from maximum electro shock, electrical kindling and pentylenetetrazole-induced convulsions in mice. The fractions also inhibited convulsions induced by lithium-pilocarpine and electrical kindling. However, they failed to protect animals from strychnine-induced convulsions. The fractions antagonised the behavioral effects of D-amphetamine and potentiated the pentobarbitone-induced sleep. The fractions raised brain contents of gamma-aminobutyric acid (GABA) and serotonin. These fractions were found to be anxiogenic and general depressant of central nervous system24.

 

Antifertility activity 

The effect of three compounds (clomiphene citrate, centchroman, embelin) and plant-derived methanolic extracts (Abutilon indicum and B. monosperma) was studied on uterotropic and uterine peroxidase activities in ovariectomized rats. It was observed that these two parameters were highly correlated in response to treatment with these test materials and also to estradiol. It was suggested that the uterine peroxidase assay could be utilized as a biochemical parameter in the screening of new antifertility agents for their estrogenic/antiestrogenic properties25.

 

Butin isolated from the seeds of B. monosperma and administered orally to adult female rats at the doses of 5, 10 and 20 mg/rat from day 1 to day 5 of pregnancy showed anti-implantation activity in 40%, 70% and 90% of the treated animals, respectively. At lower doses, there was a dose-dependent termination of pregnancy and reduction in the number of implantation sites. In ovariectomized young female rats, the butin exhibited estrogenic activity at comparable anticonceptive doses, but was devoid of anti-estrogenic activity. Butin is a weak estrogen in that a significant uterotrophic effect was discerned even at 1/20th the anticonceptive dose26.

 

The petroleum ether, alcoholic and aqueous extracts of Apium graveolens Linn., Butea monosperma Lam. Kuntz., and Gossypium herbaceum Linn., the aqueous extract of Aloe Barbadensis Mill. Syn., and the juice of unripe fruits of Ananas comosus were tested on albino rats by a method which detects any antizygotic, blastocystotoxic, antiimplantation, and early abortifacient activity. The extracts were administered for 1-7 days. The dosages for A. graveolens, B. monosperma, and G. herbaceum were 100 mg/kg. 50 ml of A. comosus juice was administered daily. Dosages of 100, 200, and 500 mg/kg of A. barbadensis were given. With the exception of A. comosus, none of the plants showed any antiimplantation activity. The juice of the unripe fruits of A. comosus demonstrated encouraging antiimplantation activity showing 40% of implants only27.

 

Aphrodisiac activity 

The extract (400 mg/kg body wt./day) was administered orally by gavage for 28 days. Mount latency (ML), intromission latency (IL), ejaculation latency (EL), mounting frequency (MF), intromission frequency (IF), ejaculation frequency (EF) and post-ejaculatory interval (PEI) were the parameters observed before and during the sexual behavior study at day 0, 7, 10, 14, 21, and 28. The extract reduced significantly ML, IL, EL and PEI (p < 0.05). The extract also increased significantly MF, IF and EF (p < 0.05). These effects were observed in sexually active and inactive male rats28.

 

PHYTOCHEMISTRY

An isocratic, reversed phase, high-performance liquid chromatographic (HPLC) method was developed for the determination of the marker compounds K052 (iso-formononetin), K054 (methoxy derivative) and K080 (formononetin) in NP-1, an anti-osteoporotic plant product from B.  monosperma. The separation was achieved on a C18 column with a mobile phase consisted of a mixture of 0.05M potassium dihydrogen phosphate containing 0.1% v/v triethyl amine (pH adjusted to 2.5 with phosphoric acid) buffer and acetonitrile (70:30 v/v), at a flow rate of 1.5 mL/min. The retention times of K054, K080 and K052 were about 13, 21 and 23 min, respectively. The effluents were monitored at 254 nm. The calibration curves were linear over the concentration ranges of 2.7-21.3, 2.1-33.6 and 2.8-22.4 microg/mL for K054, K052 and K080, respectively. The limits of detection were 0.42, 0.53 and 0.56 microg/mL, respectively. The accuracies and precisions in all cases were less than 5% in the calibration range29.

 

One new dihydrochalcone, dihydromonospermoside (7), was isolated from the flowers of Butea monosperma together with three known chalcones, butein (2), monospermoside (4) and isoliquiritigenin (8), one flavone, 7,3',4'-trihydroxyflavone (6), four flavanones, (-)-butin (1a), (-)-butrin (3a), (+)-isomonospermoside (5b) and (-)-liquiritigenin (9a), and three isoflavones, formononetin (10), afrormosin (11) and formononetin-7-O-beta-D-glucopyranoside (12). The structure of the new compound was elucidated by spectroscopic techniques whereas those of the known compounds were identified by comparisons of spectroscopic and some physical data with those of reported compounds. The absolute configurations at the 2-position of the flavanones 1a, 3a, 5b and 9a were established to be 2S, 2S, 2R and 2S, respectively, by circular dichroism spectral measurements and were confirmed by comparison of the optical rotations with those of reported values and by enzymic hydrolysis of the glucosides to the corresponding aglycones. The isolated flavonoids exhibited varying antimycobacterial activity with the chalcone 2 being the most active compound (MIC 12.5 microg/ml)30.

 

Three new compounds named buteaspermin A (1), buteaspermin B (2) and buteaspermanol (3), along with 19 known compounds were isolated and identified. The structure of compounds 1-22 were established on the basis of their spectroscopic data. The isolated compounds 2-17 were evaluated using neonatal (1-3 day old) rat calvaria derived primary osteoblast cultures. Five of these compounds 7, 10-13 showed promising osteogenic activity, attributed to increased osteoblast proliferation, differentiation and mineralization as evidenced by marked increase in expression of alkaline phosphatase, an early phase differentiation marker, and alizarin Red S staining of osteoblasts cultured for 48 h and von Kossa silver staining of nodules formed 15 days after culture with these compounds. Quantification of mineralization by optical density measurement of Alizarin Red S extracted from stained osteoblasts cultured for 7 days in presence of these compounds showed significant (P<0.05, vs corresponding vehicle control group) increase in mineralization. On the basis of biological results, structure-activity relationships are discussed31.

 

Stigmasterol was isolated from the bark of B. monosperma and evaluated for its thyroid hormone and glucose regulatory efficacy in mice. Its administration at 2.6 mg/kg/d for 20 days reduced serum triiodothyronine (T(3)), thyroxin (T(4)) and glucose concentrations as well as the activity of hepatic glucose-6-phophatase (G-6-Pase) with a concomitant increase in insulin indicating its thyroid inhibiting and hypoglycemic properties. A decrease in the hepatic lipid peroxidation (LPO) and an increase in the activities of catalase (CAT), superoxide dismutase (SOD) and glutathione (GSH) suggested its antioxidative potential. The highest concentration tested (5.2 mg/kg) evoked pro-oxidative activity32.

 

A new bioactive flavone glycoside was isolated from the methanol soluble fraction of the flowers of B. monosperma O. Kuntze, which was identified as 5,7-dihydroxy-3,6,4'-trimethoxyflavone-7-O-alpha-L-xylopyranosyl-(1-->3)-O-alpha-L-arabinopyranosyl-(1-->4)-O-beta-D-galactopyranoside (1) by several colour reactions, chemical degradations and spectral analysis. The compound 1 shows antimicrobial activity against various fungal species33.

 

Fatty acid composition of seeds from the fruits of B. monosperma, Jatropha glandulifera and Portulaca oleracea of three different families, namely Papilionaceae, Euphorbiaceae and Portulaceae were determined through Gas Liquid Chromatography to find novel natural sources of essential fatty acids for human health and of economic interest. Comparative studies were also performed to ascertain the utilization of each species for domestic as well as industrial purpose and the quality parameters developed can be utilized as marker characters for the aforesaid seeds used by the pharmaceutical industries34.

A potential antiviral flavone glycoside was isolated from the seeds of B. monosperma O. Kuntze and its structure determined as 5,2'-dihydroxy-3,6,7-trimethoxyflavone-5-O-beta-D-xylopyranosyl-(1-->4)-O-beta-D-glucopyranoside (1) by various spectral analysis and chemical degradations35.

 

The oligosaccharide specificity of newly isolated B. monosperma agglutinin (BMA) was determined by two-dimensional lectin affinity electrophoresis of alpha-fetoprotein (AFP) with concanavalin A, lentil lectin, erythroagglutinating  phytohemagglutinin and Allomyrina dichotoma lectin, of which the specificities to known AFP oligosaccharides had been established. Effects of neuraminidase treatment on the reactivities of AFP to the lectins were also studied. The results indicated that BMA had the highest affinity for the exposed Gal residues of nonreducing termini of biantennary complex-type oligosaccharides, and that the affinity was reduced to zero in the following order by the presence of monosialyl residue of the Man alpha1->3 arm, monosialyl residue of the Man alpha1->6 arm, monosialyl residue of the Man alpha 1->3 arm and bisecting G1cNAc, and disialyl residues. BMA did not recognize Neu5Ac alpha2->6 and Neu5Ac alpha2->3 substitutions of Gal. These characteristics of BMA were shown to be useful in identifying malignancy-associated alteration of AFP sugar chains36.

 

The petroleum and ethyl acetate extracts of the stem bark from B. monosperma displayed antifungal activity against Cladosporium cladosporioides. The active constituent of low polarity was isolated by bioassay-monitored chromatographic fractionation, and identified as (-)-medicarpin by comparison of physical data. The antifungal activity of (-)-medicarpin was found to be greater than that of Benlate, a standard fungicide, while    (-)-medicarpin acetate also exhibited significant activity against C. cladosporiodes37.

 

Stigmasterol, stigmasterol-betaD-glucopyranoside and nonacosanoic acid, two new compounds were isolated from the stems of B. monosperma have been characterised as 3alpha-hydroxyeuph-25-ene and 2,14-dihydroxy-11,12-dimethyl-8-oxo-octadec-11-enylcyclohexane+++ by spectral data and chemical studies38.

 

MISCELLANEOUS

An Ayurvedic herbal medicine, prepared from Piper longum (Pippali) and B. monosperma, and prescribed for the treatment of chronic dysentery and worm infestations was tested for anti-giardial and immuno-stimulatory activity in mice, infected with Giardia lamblia trophozoites. It produced up to 98% recovery from the infection. The rasayana had no killing effect on the parasite in vitro. It induced significant activation of macrophages as evidenced by increased macrophage migration index (MMI) and phagocytic activity. Enhancement of host resistance could be one of the possible mechanisms contributing towards the recovery of animals from the giardial infection39.

 

CONCLUSION:

The pharmacological studies reported in the present review confirm the therapeutic value of B. monosperma. Thus, activity guided phytochemical and pharmacological studies may lead to development of novel agents for various disorders.

 

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Received on 17.03.2012

Modified on 28.03.2012

Accepted on 05.04.2012                                               

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Research J. Pharmacology and Pharmacodynamics. 4(3): May-June, 2012, 150-157