Journal of Pharmaceutical Biology

Ali Esmail Al-Snafi. / Journal of Pharmaceutical Biology, 5(4), 2015, 240-253.

Journal of

Pharmaceutical Biology

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e-ISSN - 2249-7560 Print ISSN - 2249-7579

THE PHARMACOLOGICAL IMPORTANCE OF BRASSICA NIGRA AND BRASSICA RAPA GROWN IN IRAQ Ali Esmail Al-Snafi* Department of Pharmacology, College of Medicine, Thi qar University, Nasiriyah, Iraq. ABSTRACT Brassica nigra and Brassica rapa are the members of Brassica genus (Family: Brassicaceae) which grown in Iraq. The previous studies showed that Brassica nigra possessed antioxidant, anti-inflammatory, antiepileptic, antidiabetic and many other pharmacological effects, while, Brassica rapa exerted cytotoxic, mutagenic, hepato-protective, nephroprotective, lung protective, antiobesity, antidiabetic, antioxidant, immunological, anti-inflammatory, cardiovascular and hypolipidemic effects. This review will highlight the chemical constituents and pharmacological effects of these plants. Keywords: Brassica nigra, Brassica rapa, Pharmacology, Chemical constituents. INTRODUCTION Medicinal plants are the oldest form of healthcare known to mankind. Medicinal plants had been used by all cultures throughout history. The World Health Organization (WHO) estimates that 80 percent of the world population, presently use herbal medicine for some aspect of primary health care. Plants are a valuable source of a lot of secondary metabolites, which exerted a wide range of pharmacological effects [1-57]. The major pharmaceutical companies are currently conducting extensive research on plant materials to introduced new drugs in the medical practice. Brassica nigra and Brassica rapa are the members of Brassica genus (Family: Brassicaceae) which grown in Iraq. This review will highlight the chemical constituents and pharmacological effects of these plants. Brassica nigra Synonyms: Brassica nigra var. abyssinica A. Braun, Sinapis nigra L [58]. Taxonomic classification Kingdom: Plantae, Phylum: Spermatophyta, Subphylum: Angiospermae, Class: Dicotyledonae, Family: Brassicaceae (alt. Cruciferae) Tribe: Brassiceae, Genus: Brassica, Sepeies: Brassica nigra [59-60]. Common names

Arabic: khardal, khardal aswad; Chinese: hei jie; English: black mustard, brown mustard, red mustard; French: moutarde noire; Germany: Schwarzer Senf, Senf- Kohl, Senfkohl; Italy: senape near; Japanese: kuro-garashi; Netherlands: zwarte Mosterd; Philippines: mustasa; Portuguese: mostarda-negra; Spanish: mostaza negra; Sweden: svartsenap[59-60]. Distribution: Black Mustard grows in temperate regions worldwide [61]. It is distributed in Africa: Algeria, Egypt, Libya, Morocco, Tunisia, Eritrea, Ethiopia; Asia: Afghanistan, Cyprus, Iran, Iraq, Palstine, Lebanon, Syria, Turkey, Armenia, Kazakhstan, China; Europe: Ireland, United Kingdom, Austria, Belgium, Czech Republic, Germany, Hungary, Netherlands, Poland, Slovakia, Switzerland, Belarus, Moldova, Russian Federation, Ukraine, Albania, Bosnia and Herzegovina, Bulgaria, Croatia, Greece, Italy, Macedonia, Montenegro, Romania, Serbia, Slovenia, Denmark; Norway, France, Spain; Australia: Australia, New Zealand; Northern America: USA, Mexico, Canada; Southern America: Ecuador, Peru, Argentina and Chile [60]. Traditional uses The plant was used in the treatment of rheumatism, as an agent to reduce congestion in internal organs. In addition, it was applied in neuralgia and spasms, alopecia, epilepsy, snakebite, and toothache. It

Corresponding Author:- Ali Esmail Al-Snafi Email:- [email protected] 240 | P a g e


was also used to treat carcinoma and throat tumors. A liquid prepared from the seed, when gargled, is said to help tumors of the sinax. The seed was eaten as a tonic and appetite stimulant. Hot water poured onto bruised mustard seeds makes a stimulating foot bath and can also be used as an inhaler where it acts to throw off a cold or dispel a headache. Mustard oil is said to stimulate hair growth. Mustard is also recommended in hiccup. It was also considered antiseptic [62]. Brassica nigra is also traditionally used as simple rubefacient, diuretic, emetic, pneumonia, bronchitis, nerve stimulant and vesicant [63]. Description Brassica nigra, black mustard, is an annual herbaceous plant. It grows up to 2 m (a little over 6 ft), with many branches. The lower leaves are dentate (toothed), pinnatifid (deeply lobed) or lyrate (deeply lobed, but with an enlarged terminal lobe and smaller lateral lobes), and are often hairy, at least on the underside. Upper leaves on flowering stems are narrow and oblong. In contrast to many Brassica species, the leaves are little if at all glaucous (waxy). The yellow, four-parted and cross-shaped flowers, occur in many racemes (spike-like cluster) and produce 4-sided siliques capsular fruit that dehisces (splits open) when mature that may be up to 2.5 cm (1 in) long. Each silique contains 2 to 12 or more reddish brown to black round seeds. A single plant may produce thousands of seeds, which must be harvested by hand or mechanically before they fully ripen, because the siliques spontaneously split and disperse the seeds when they are mature [64]. Part used: The medicinal parts were the seeds from which oil is extracted [61]. Chemical constituents Phytochemical screening showed that the plant contained alkaloids, flavonoids, glycosides, carbohydrates, sinapine, myrosin, sinigrin, inosite, albumins, gums and colouring matters. The total phenol content in the plant was 6.67 mg/g of galic acid. It contained fatty oil (30-35%), proteins (40%), phenyl propane derivatives: including sinapine (choline ester of sinapic acid, 1%), and glucosinolates: chiefly sinigrin (allylglucosinolates, 1-5%). Grinding the seeds into powder and then rubbing with warm water releases the volatile mustard oil, allylisothiocyanate [65-68]. Total phenol content of methanol extract was found to be 171.73± 5.04 gallic acid equivalents and the total flavonoid content was 7.45 ± 0.0945 quercetin equivalents. The predominant phenolic compounds determined by HPTLC were gallic acid, followed by quercetin, ferulic acid, caffeic acid and rutin [69]. Hussien et al., found that the callus obtained from hypocotyl explants of Brassica nigra was rich in secondary metabolites as they gave positive results for testes of volatile oils, anthraquinones, flavonoids and

tannins. The total phenolics were higher in calli obtained under light incubation conditions than calli obtained under dark incubation conditions or the mother plant parts from which calli were induced [70]. Pharmacological effects Antioxidant effect The total antioxidant capacity of the extract was found to be 97.08 mg/g of ascorbic acid. Brassica nigra showed IC 50 value of 63.09μg/ml whereas the standard antioxidant showed IC50 value 14.45 μg/ml in DPPH method. The standard antioxidants ascorbic acid, galic acid and quercetin showed the reducing power 485.75%, 736.30% and 763.01%, respectively whereas Brassica nigra showed the value 263.69%. IC50 value in NO scavenging activity of the extract was found to be 118.21 μg/ml whereas ascorbic acid showed the value 5.47 μg/ml and quercetin had the value 15.24 μg/ml [65]. The antioxidant activity of methanol extract of Brassica nigra seeds, and leaves was demonstrated with a wide range of concentration, 10-500 µg/ ml. It was increased with the increase in concentration [69]. Callus obtained from hypocotyl explants of Brassica nigra was investigated for its antioxidant activity and antibacterial activity against 4 pathogenic bacterial strains (E. coli, Staphylococcus aureus, Ps. Aureogenosa and K. pneumonia). It was generally observed that antioxidant activity and antibacterial activity were higher in calli obtained under light incubation conditions than calli obtained under dark incubation conditions or the mother plant parts from which calli were induced. It is also observed that older calli accumulated more amounts of total phenolics, exhibited higher antioxidant activity and stronger antibacterial activity [70]. Anti-inflammatory effect The effect of Brassica nigra seed extracts on arthritic rats were assessed by the various models. In arthritic rats, inflammation reached maximum on day 3 and maintained till day 9. Paw maintained its inflammation till day 14. A significant reduction was recorded in the extracts treated group. Ankle diameter reached maximum on day 7 and maintained its inflammation till day 14. A non-significant reduction was observed in the extracts treated group [67]. In vivo and in vitro anti-inflammatory activity of the crude extract was evaluated using carrageenan induced rat paw edema and protease enzyme inhibition assay. In vivo anti-inflammatory test of the ethanolic extract of Brassica nigra (500 mg/kg) gave 17.9% inhibition whereas standard phenylbutazone (100mg/kg) gave 39.38%. In vitro anti-inflammatory test of Brassica nigra by protease inhibition method also gave 42.57% inhibition of trypsin at dose 250 μg/ml [65]. Volatile oil of mustard is an extremely diffusible 241 | P a g e


and penetrating irritant, quickly exciting heat and burning pain through its dilating action upon the peripheral vessels and irritation of the sensory nerve endings. If too long applied it will blister, and cause inflammation, sloughing and deep ulceration; and not infrequently gangrene. To a degree local anesthesia is produced in some instances and the patient is then not aware of the possible destruction of tissue. When the treatment removed in time only induration is caused, followed sometimes by desquamation. Mustard applied in the same manner acts similarly but more slowly and with gradually increased intensity [71]. Antiepileptic effect The antiepileptic activity of methanolic extract of Brassica nigra seeds was investigated on maximal electroshock induced seizures (MES), Pentylene tetrazole (PTZ), Picrotoxin (PIC) and biccuculine induced seizures in mice. It was found that the extract (200 and 400 mg/kg, orally), significantly prolonged the onset of tonic seizures and reduced the duration of incidence of seizures in PTZ, PIC and biccuculine induced seizure models, while in MES model, the extract showed significant effect in abolishing tonic hind limb extensions by inhibiting voltage dependant Na+ channels or by blocking glutaminergic excitation mediated by the N-methyl- Daspartate (NMDA) receptor [66]. The anti-epileptic effect of the methanolic extract of Brassica nigra seeds (75, 150 and 300 mg/Kg; ip) was evaluated in pentylentetrazole (PTZ) - induced kindling in mice. The methanolic extract of Brassica nigra seed reduced the intensity and duration of seizure. In addition, the Brassica nigra extract increased the SOD and NO levels and decreased the MDA level in the brain tissues [72]. Antidiabetic effect In streptozotocin induced diabetic rats treated with aqueous, ethanol, acetone and chloroform extracts of the seeds of Brassica nigra, the increase in serum glucose value between 0 and 1 hr of glucose tolerance test (GTT) was the least (29 mg/dl) in aqueous extract treated animals, while it was 54, 44 and 44mg/dl with chloroform, acetone and ethanol extracts respectively. In addition the effective dose of aqueous extract was found to be 200 mg/kg body weight in GTT. Administration of 200 mg/kg body weight of aqueous extract to diabetic animals once daily for one month brought down fasting serum glucose (FSG) levels . The glycosylated hemoglobin (HbA1c) and serum lipids in the treated group were much less than untreated diabetic controls [73]. Aqueous extract of Brassica nigra (AEBN) has been shown to have good antidiabetic effect along with significant decrease (p 35%, respectively) in the same concentration range [126]. Lung protective effect The effect of the aqueous extract of Brassica rapa chinensis was studied against bleomycin (BLM) induced pulmonary fibrosis. Aqueous extract of Brassica rapa chinensis (250, 500 mg/kg, po) showed significant protective effect against BLM induced pulmonary fibrosis in rats by normalizing the levels of glycoproteins (hexose, hexosamine and sialic acid) and improving the activity of Catalase (CAT) and Superoxide dismutase (SOD). The extract also improved pulmonary glutathione (GSH) content and depleted the lipid peroxidation levels in a dose dependent manner. The histopathological analysis also reveal the reversal of the lung architecture to near normal upon administration of plant extract [127]. Cardiovascular and hypolipidemic effects Crude extract and fractions of Brassica rapa was screened against human platelet aggregation induced by two different aggregating agents and further delineated their underlying signal transduction pathways. Furthermore, Brassica rapa was screened for the presence of calcium channel blocking potential. The results showed that Brassica rapa blocked calcium channel opening as indicated by its effects on KCl-induced contraction in guinea pig ileum and this activity was distributed into various fraction of Brassica rapa except ethyl acetate fraction which did not show any significant calcium channel blocking activity. Platelet aggregation induced by arachidonic acid (AA), platelet activating factor (PAF) and agonists of protein kinase C (PKC) and inositol triphosphate (IP3) was inhibited by various fractions of Brassica rapa with different potencies, suggesting that phyto compounds responsible for these 247 | P a g e


effects are differentially concentrated in various fractions [128]. The effect of different doses of turnip juice on blood lipid changes was studied in hypercholesterolemic rabbits. Extract was given in as 100, 200, 400 mg / kg body weight of the rabbits. The results showed that the turnip root extract can prevent the occurrence of atherosclerotic in hypercholesterolemic rabbits which may be due to flavonoids and vitamins contents [129]. Caulilexin C , indoleacetonitrile and arvelexin isolated from the root of Brassica rapa (at a concentration of 100 μg/ml) showed an inhibitory activity on human Acyl CoA: cholesterol transferase 1 (hACAT1) by 54.6±6.0%, 69.2±4.7% and 68.6±3.7%, and on human Acyl CoA: cholesterol transferase 2 (hACAT2) by 4.8±13.4%, 45.6±4.8% and 39.5±4.3%, respectively [107]. Effect on obesity and metabolic syndrome The influence of ethanolic extracts of Brassica campestris spp. rapa roots (EBR) on obesity was examined in imprinting control region (ICR) mice fed a high-fat diet (HFD) and in 3T3-L1 adipocytes. The molecular mechanism of the anti-obesity effect of EBR was investigated in 3T3-L1 adipocytes as well as in HFDfed ICR mice. In the obese mouse model, both weight gain and epididymal fat accumulation were highly suppressed by the daily oral administration of 50 mg/kg EBR for 8 weeks, whereas the overall amount of food intake was not affected. EBR treatment induced the expression in white adipocytes of lipolysis-related genes, including beta3-adrenergic receptor (beta3-AR), hormonesensitive lipase (HSL), adipose triglyceride lipase, and uncoupling protein 2. Furthermore, the activation of cyclic AMP-dependent protein kinase, HSL, and extracellular signal-regulated kinase was induced in EBRtreated 3T3-L1 cells. The lipolytic effect of EBR involved beta3-AR modulation, as inferred from the inhibition by the beta3-AR antagonist propranolol. Accordingly, EBR may have potential as a safe and effective anti-obesity agent via the inhibition of adipocyte lipid accumulation and the stimulation of beta3-AR-dependent lipolysis [130]. The role of turnip (Brassica rapa) on fructoseinduced metabolic syndrome(MS) was studied in rats . MS was induced by administration of fructose as 10% solution in drinking water for 8 weeks. Three groups of rats were administered fructose as 10% solution in drinking water for 8 weeks. One served as fructose fed

control while the remaining two groups were treated with metformin (10 mg/kg/day) and turnip (400 mg/kg/day) for two weeks. At the end of the experiment, blood samples were withdrawn for estimation of markers related to MS. Induction of MS was associated with increased body weight gain and elevated levels of blood glucose, MDA, nitric oxide, total triglycerides and total cholesterol. It also reduced levels of blood GSH and liver glycogen. Brassica rapa attenuated most of the changes associated with MS. It reduced weight gain and blood glucose, MDA, nitric oxide, total triglycerides and total cholesterol. It also elevated blood GSH and liver glycogen [131]. Anti-inflammatory effect Arvelexin also inhibited LPS-induced NO and prostaglandin E2 production through the suppression of iNOS and COX-2 at the level of gene transcription. In addition, arvelexin inhibited NF- ҝB dependent inflammatory responses by modulating a series of intracellular events of IҝB kinase (IKK)-inhibitor ҝBα (IkBα)- NF- ҝB signaling. Moreover, arvelexin inhibited IKKβ -elicited NF- ҝB activation as well as iNOS and COX-2 expression. Serum levels of NO and inflammatory cytokines and mortality in mice challenged injected with LPS were significantly reduced by arvelexin [132]. Contraindications and side effects No health hazards were recorded with the proper administration of designated therapeutic dosages of the oil. However, Rapeseed oil, when ingested in high dosages over an extended period of time, is cardiotoxic [83]. Brassica and related species contain sulfur compounds (glucosinolates) that can irritate the digestive tracts or create thyroid problems in livestock if consumed in large quantities over time[84]. Dosage: Seed 500mg-1g paste [100]. CONCLUSION The previous studies showed that Brassica nigra possessed antioxidant, anti-inflammatory, antiepileptic, antidiabetic and many other pharmacological effects, while, Brassica rapa exerted cytotoxic, mutagenic, hepato-protective, nephro-protective, lung protective, antiobesity, antidiabetic, antioxidant, immunological, anti-inflammatory, cardiovascular and hypolipidemic effects. This review will highlight the chemical constituents and pharmacological effects of these plants.

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