Pharmacognostical and Pharmacological Profile of Barleria prionitis Root

Umesh Dhaked¹*, Gaurav Nama¹, Devendra P. Singh²_, Amit K. Mishra² and Nitin Kumar²

¹School of Pharmaceutical Sciences, Jaipur National University, Jaipur- 302025, (Raj), India

²Bhagwant Institute of Pharmacy, Muzaffarnagar (U.P.), India

ABSTRACT:

Barleria prionitis Root or Vajradanti is a herb used in cure of various ailments traditionally. Barleria prionitis Root or Vajradanti is used locally on skin to expel out spine from the skin, in acute stages of cyst in blood vessels, in glandular swellings, as diuretic, rich in potassium salts and in bronchial asthma etc. Pharmacologically, Barleria prionitis Root or Vajradanti possesses Antifertility effects, Antiarthritic activity, Inhibitory activity against glutathione S-transferase. (GST) and acetyl cholinesterase (AChE) inhibitory activity, Antiviral activity.

KEYWORDS: Barleria prionitis Root, Pharmacological activities,Traditional uses

INTRODUCTION:

Indian traditional system of medicines is classified mainly into ayurveda, siddha and unani systems. The medicinal plants play a major role and constitute the backbone of the traditional medicine.The evaluation of these medicines is mostly based on phytochemical, pharmacological and allied approaches including various instrumental techniques like Chromatography, microscopy and others.^{1, 2}

Plants are considered to be medicinal if it possesses pharmacological activities of possible therapeutic use. These activities are often known as a result of millennia of trial and error, but they have to be carefully investigated if we wish to develop new drugs that meet the criteria of modern treatment. The goals of research in this field are especially:

1. The identification of the active principles of medicinal plants, and investigation of the extracts in order to ensure that they are safe, effective and of having constant activity.

2. The isolation of these active principles and the determination of their structure, in order that they may be synthesized, structurally modified, or simply extracted more efficiently.³

Most of the medicinally active substances identified in the 19^th and 20^th centuries were used in the form of crude extract. A large portion of the Indian population even today depends on the Indian system of medicine “Ayurveda” an ancient science of life. The well known treatises in Ayurveda are Charaka samhita and Sushrutha samhita.⁴

Medicinal plants represent only a valuable part of India’s biodiversity but also a source of great knowledge. The WHO have listed 21,000 plants that are used as medicine around the world. India has a rich medicinal plants flora of some 2500 species and out of these 150 species are used commercially on a fairly large scale.

India has 16 Agro climatic zones and medicinal plants are distributed across diverse habitats and landscapes. Nearly 70% of India’s medicinal plants are found in the tropical areas mostly in the various forest types across the western and Eastern Ghats. Nearly 30% of medicinal plants having high medicinal importance occur in temperate and alpine region.⁵

Barleria prionitis or porcupine flower, also called espinosa umbrella   and picanier jaune, is a flowering, spiny invader that reaches 1.5 mt. in heightand 2.5 cm. in basal diameter. It has a tap and lateral root system. Leaves are elliptic to oblong.6-12cm.Long.

This is an erect, smooth, branched shrub, 1-2m height, with slender, axillary spines; the flowers are yellow and axillary,

Barleria prionitis or porcupine flower grows in a wide variety of well – drained soils derived from igneous, metamorphic (including ultramafics) and sedimentary (including lime stone) rocks.

Barleria prionitis Linn. (Family-Acanthaceae) commonly known as Vajradanti.²

Fig.1 Barleria prionitis

Synonyms:⁶

Barleria hystrix , Barrliera prionitis,  Blanco prionitis hytrix miq.

Vernacular name:⁷

English:     Porcupine flower

Hindi:        Vajardanti

Bengali:     Kantajant

Sanskrit:    Ananta, Sahachara, shvetapushpa, pitapushpaka

Telgu:        Gobbi

Uriya:        Dasokoranti, kurunta

Tamil:       Kodippachalai, kunda

Scientific classification:

Kingdom           :    Plantae

Subkingdom     :    Trachaeobionta

Division            :   Magnoliophyta

Class                  :   Magnoliopsida

Subclass             :   Asteridae

Order                 :    Scrophulariales

Family               :    Acanthaceae

Genus                :    Barleria

Species       : prionitis

Chemical constituents: Flavonoid glycoside-scutellarein-7- neohesperidoside, iridoid glycoside-barlerin and acetylbarlerin and a new acylated flavanoid glycoside luteoline-7-0-(2”-0-p-coumaroyl)-b-D-glycopyranoside, Alkaloids, B-Sitosterol, Potassium are reported. ⁸

Ayurvedic properties:⁸

Rasa                 :           Tikta,Madhura

Guna                :           Snigdha,Loghu

Veerya             :            Ushna

Vipaka             :            Katu

Doshaghnatya :           Kaphavatashamaka

Rogaghnata      :             Kasa,

Karma              :             Vatakaphashamaka

Pharmacognostical studies are as follows:⁹

1. Periderm of stem bark subtended by 5-7 layers of tabular collenchyma.

2. Phloem ray of stem heterogeneous type I(Jane 1956) with uniseriate and multiseriate rays, 8-16  and 8-25 cells high respectively, 23 celled broad.

3. Granular and needle shaped calcium oxalate crystals filling up many cells in almost all tissues of barks.

4. In root bark a yellowish cork and sometimes a new phellogen layer separating the outer and inner cortex.

5. Root-wood cells containing a blackish brown content.

Medicinal uses:

Traditional Uses: Almost all the parts of Barleria prionitis have medicinal importance and used traditionally for the treatment of various ailments. Root extract of Barleria prionitis is applied locally on Skin to Expel out spine from the skin.¹⁰

The Barleria prionitis oil prepared with whole plant is indicated for external application during acute stages of cyst in blood vessels.¹⁰

Root paste of plant Barleria prionitis is applied over boils and glandular swellings, plants leaves, roots, and flowering tops of Barleria prionitis are diuretic, rich in potassium salts.  Leaves and stem of Barleria prionitis showed presence of iridoids, glucosides, barlerin and acetyl barlerin.The presence of  b-sitosterol is reported in Barleria prionitis Ash obtained mixed with honey is given in bronchial asthma^{. 1}

Roots are used in cough as tonic, as Diuretic and as antimicrobial The ayurvedic pharmacopoeia of India recommends oil extracts of Barleria prionitis for arresting graying of hair. According to ayurvedic pharmacopoeia therapeutic uses of Barleria prionitis is Kustha, Kandu, Vatarakta, Palit.²

During gout, Whole plant paste is applied externally as an ointment. To increase sexual vigour, Seed Extract is administered daily once for a Fortnight. For curing mouth Ulcers, Leaves are chewed and sap is swallowed; for oedema, Seed paste is taken daily once until it is cured while during toothache, leaf paste is applied over the affected area.¹²

PHARMACOLOGICAL USES:

GST INHIBITORY ACTIVITY: The crude extract of Barleria prionitis exhibited GST inhibitory activity with an IC50 value of 160µg/ml. crude Ethanolic extract of Barleria prionitis have resulted in the isolation of six natural products. balarenone (1), pipataline (2), lupeol (3), prioniside A (4), prionisideB (5), and prioniside C (6). Compounds 1, 4, 5, and 6 were new natural products, while 2 and 3 were known compounds. Compounds 1–6 showed GST inhibitory activity with IC50 values of 48.50, 57.0, 60.0, 49.26, 22.91, and 12.44 μM, respectively. Compounds 1–6 were also screened for AChE inhibitory activity and found to be active in this bioassay with IC50 values of 200.09, 135.00, 89.97, 175.98, 133.46, and 50.03 μg/ml, Respectively. Pipataline (2) was isolated on a large scale, and it exhibited moderate bioactivity in both of our enzyme inhibition assays. We attempted to study its structure–activity relationships (SARs) by preparing its different structural analogs (7–8). 7,8-Epoxypipataline (7) was synthesized by doing an epoxidation reaction on the C-7/C-8 double bond of Pipataline (2) using m-chloroperbenzoic acid. Compound 7 was further reacted with 20 % ammonium hydroxide solution using household microwave radiation as a catalyst to afford 7-amino-8- hydroxypipataline (8). Both of these compounds were found to be active in AChE inhibition assay with IC50 values of 164.00 and 36.75, respectively. This SAR study suggested that the AChE inhibitory activity of compound 8 was significantly increased as compared to parent compound 2, and this increase in bioactivity may be due to the presence of an amino functionality at C-7.¹³

Antifertility effects of Barleria prionitis: Oral administration of root extract of Barleria prionitis Linn. To male rats (100 mg/rat per day) for the period of 60 days did not cause body weight loss. The root extract brought about an interference with spermatogenesis. The round spermatids were decreased by 73.6%. no significant change was found in the population of secondary spermatocytes. The extract reduced the fertility of male rats by 100%.cross sectional surface area of sartoli cells and mature laydig cells numbers were significantly reduced to 36.9%. the total protein, sialic acid contents of the testis, epididymides, seminal vesicle andprostate were reduced. Testicular glycogen contents were low. Antifertility effects of Barleria prionitis seemed to be mediated by disturbances in testicular somatic cells functions (leydig and sertoli cells) resulting in the physio-morphological events of spermatogenesis.¹⁴

Antiarthritic activity: ‘TAF’ fraction from the methanolic-water extract plant Barleria prionitis Linn. Was evaluated for antiinflammatory and anti- arthritic activities against different acute and chronic animal test models. It exhibited significant antiinflammatory activity against different inflammagens like carrageenan, histamine and dextran. Significant anti-arthritic activity was observed in adjuvant-induced polyarthritis test in rats.’TAF’ also showed inhibition of vascular permeability and leucocytes migration in vivo into the site of inflammatory insult.¹⁵

Inhibitory activity against glutathione S-transferase.(GST) and acetyl cholinesterase (AChE): Phytochemical studies on the Ethanolic extract of plant Barleria prionitis of Srilanka origin have resulted in the isolation of new compound, barlerone (1) , along with 3 known compound ,pipataline(2) lupeol (3), 13,14-seco-stigmasta-5,14-diene-3-ol (4) the structures of 1-4 were elucidated with the aid of extensive NMR spectroscopic studies. Compounds 1-4 showed moderate inhibitory activity against glutathione S- transferase.(GST) and acetyl cholinesterase (AChE ).¹⁶

Antiviral activity: Two new iridoids glycosides (1 and 2), together with the known compounds barlerin (3) and verbascoside (4), were isolated from Barleria prionitis . the new iridoid glycosides were  determined to be 6-O-trans-p-coumaroyl-8-0acetylshanzhiside methyl ester (1) and its cis isomer (2) by using spectroscopic, especially 2D NMR . 3: 1 mixture of 1 and 2 was shown to have potent in vitro activity against respiratory syncytial virus.¹⁷

Hepatoprotective Activity: synergistic composition of Bioactive fraction isolated from Barleria prionitis linn and a method of treatment for hepatotoxicity immune-deficiency and fatigue activity.¹⁸

CONCLUSION:

Thorough screening of literature available on Barleria prionitis it is found to be very useful in cure of various diseases. The Pharmacological studies prove the Medicinal importance of plant Barleria prionitis. The Phytochemical and Phytoanalytical studies may lead to development of novel agents for various diseases. Synthesis of the active constituents can lead to development of promising Pharmacological actions.

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Received on 31.01.2011

Accepted on 28.02.2011

© A&V Publication all right reserved

Research Journal of Pharmacognosy and Phytochemistry. 3(3): May- June 2011, 108-111