Pharmacological investigation of Calotropis gigantea:

 A benevolent herb of Nature

 

 Prativa Biswasroy, Sthitapragnya Panda, Debajyoti Das, Durga Madhab Kar, Goutam Ghosh*

School of Pharmaceutical Sciences, Siksha ‘O’ Anusandhan (Deemed to be University),

Kalinga Nagar, Bhubaneswar, Odisha, 751003

*Corresponding Author E-mail: goutamghosh@soa.ac.in

 

ABSTRACT:

In ancient time, human beings worshiped plants, which are extensively essence for medicinal properties in every other way. India is the largest producer of medicinal herbs and is appropriately called the botanical garden of the world. Calotropis gigantea or Crown flower belongs to Asclepiadaceae family, is one such plant with unique properties used alone or with other medicinal to treat common diseases. Herbal medicines exhibit a remarkable therapeutic diversity. According to ayurveda, dried whole plant is used as a good tonic, anthelmintic and expectorant. The powdered root is used to treat asthma, leprosy, bronchitis, while the latex used to treat vertigo, baldness, hair loss, rheumatoid. Besides its traditional uses, calotropis is used as homeopathic medicines. The extracts from different parts of the plant have significant therapeutic values.  In order to make these remedies acceptable to modern medicines, there is a need to scientifically evaluate them to identify the active principles and understand the pharmacological actions like anti-fertility, anti-inflammatory, anti-bacterial, anti-microbial, antioxidant, antiulcer, antipyretic, hepatoprotective. The present review summarizes the information concerning the mythological significance, ayurvedic significance, origin, pharmacognostical description, phytoconstituents, biological activities, with ethnopharmacological significance of Calotropis gigantea.

 

KEYWORDS: Calotropis gigantea, Phytoconstituents, Ethnopharmacology, Biological activities.

 

 


INTRODUCTION:

India being a tropical country is blessed with natural resources and ancient knowledge for its judicious utilization1. The medicinal plant is exploited as a great environmental and biological diversity compared with the rest of the world2. Natural products are gaining their revival as many allopathic drugs causing severe side effects and toxic effects. World Health Organization (WHO) heavily promotes the use of herbal drugs as an alternative medicinal practice in the developing countries3. Around 45% of flowering plants are estimated to have medicinal importance. India ranks tenth among the plant rich countries of the world and fourth among the Asian countries4. India is the largest producer of medicinal herbs and is appropriately called the botanical garden of the world4,5. Calotropis gigantea is one of the precious medicinal herbs in that garden commonly known as arka6.

 

Traditionally, it is believed that, when this herb is used judicially and clocking with the basic principles, they produce tremendous therapeutic effects6,7. In Sanskrit, arka means “radiance of the Sun” which signifies it’s capability to treat many diseases with just a simple touch. Calotropis is available in two varieties such as Calotropis gigantean and Calotropis procera. Calotropis gigantea is known as “Sweta arka” (white flowered) and Calotropis procera as “Raktha arka” (purple flowered)8. Both of them are often similar in their botanical aspects and also have similar pharmacological effects. Among the two varieties, Rakta arka (Calotropis procera) is more toxic and is assumed even more poisonous than cobra venom9-10.

 

MYTHOLOGICAL SIGNIFICANCE:                

Calotropis gigantea, a crown flower having a pretty purple colored, slightly scented flower with sweet and agreeable smell11. However, in India, among the general public, it is believed that arka is a white flower with bluish tinge matched the bluish hue of Shiva’s throat & is offered to Lord Shiva on auspicious days. Arka is another name for Lord Surya as mentioned in Hindu epic Suryashtotra.  Once when the gods were performing a sacrificial ritual for Lord Surya, some of the milk spilled over the earth. From that spilled milk, sprang a plant which the gods called as arka12.

 

ORIGIN AND GEOGRAPHICAL DISTRIBUTION:

Calotropis gigantea is native to Asia and South-East Asia and has been introduced in the Pacific Islands, Australia, Central and northern South America and Africa as an ornamental herb. However, its distribution is not completely known, and it probably occurs in other countries as well13.

 

TAXONOMICAL HIERARCHY14-16:

Kingdom

:

Plantae

Order

:

Gentianales

Family

:

Apocynaceae

Subfamily

:

Asclepiadoideae

Genus

:

Calotropis

Species

:

C. gigantea

 

VERNACULAR NAMES17-19:

English

:

Madar, Giant Milk-weed, Roostertree, Mudar plant

Sanskrit

:

Alarka, Rajaarka, Shvetarka, asuka, Mandaar, Bhasvanmuula, Dinesh, Prabhakar

Unani

:

Madaar, Aak

Siddha

:

Erukku

French

:

Calotrope, Pomme de Sodome

German

:

WahreMudarpflanzer, Gomeiner

Italian

:

Calotropo

Bengali

:

Aaknad

Telugu

:

Jilledu, Mandaram

Punjabi

:

Ak

Arab

:

Ushar

Persian

:

Kharak

 

PHRAMACOGNOSTICAL DESCRIPTION:

Whole plant20:

Large shrub or small tree up to 4–10 m tall, much-branched at base, stems erect, up to 20 cm in diameter; bark pale grey, longitudinally cracked; young shoots woolly hairy; latex in all parts.

 

Leaves21:

The leaf is simple, decussate and sessile. Leaf blade is ovate to obovate in shape with entire margin without any stipules. The leaf is 10-20 cm. long.

 

Flowers22:

Flower consists of five pointed petals each 3-5 cm in diameter, purplish or white in umbellate lateral cymes and a small "crown" rising from the center which holds the stamens, having clusters of waxy flowers that are either white or lavender in colour..

 

Fruits23:

The fruits having are boat-shaped, , 9-10 cm long, small, thick green with seeds in fleshy follicles covered with white woolly pubescence and  a pair of follicles, with tapering at both ends.

 

Seeds24:

Ovoid shape, 5–6mm long with 2–3cm long coma at one end.

 

Figure1. Macroscopic view of plant parts a) Leaves b) Flower c) Fruit d) Seed e) Latex


PHYTOCONSTITUENTS AND BIOLOGICAL ACTIVITIES20-33:

Table 1. List of phytoconstituents present in the plant Calotropis gigntea

Plant parts

Chemical constituents

Structure

Biological activity

Whole

Plant

Diterpenoid Lactones25

Furanolactone,

Clerodane derivatives

Tinosporon,

Tinosporides,

Jateorine, Columbin

 

Furanolactone               Columbin    

1.    Vasorelaxant

2.    Induce contractions

3.    Inhibits Ca+2 influx

4.    Anti-inflammatory

5.    Anti-microbial

6.    Antihypertensive

7.    Anti-viral

8.    Induce apoptosis in Leukemia

Aliphatic Compound26,28

Octacosanol,

Heptacosanol

Nonacosan-15-one

Dichloromethane.

 

Octacosanol

1.      Anti-nociceptive

2.      Anti-inflammatory

3.      Protection against 6-hydroxy-dopamine induced Parkinsonisms in rats.

Stem

Glycosides22,23,29

18-Norclerodane

glucoside, Furanoid diterpene glucoside,

Tinocordiside,

Tinocordifolioside,

Cordioside, Cordifolioside

Syringin, Syringinapiosyl glycoside, Pregnane glycoside, Palmatosides,

Cordifolioside A, B, C, D and E

 

Cordifolioside A           Syringin

1.      Treats neurological disorders like ALS (Amyotrophic lateral sclerosis)

2.      Parkinsonism

3.      Dementia

4.      Motor and cognitive deficits and neuron loss in spine and hypothalamus,

5.      Immunomodulation,

6.      Inhibits NF-kband, act as nitric oxide scavenger to show anticancer activity.

Root

Alkaloids25-27,30-33

Berberine, Choline,

Tembetarine, Magnoflorine,

Tinosporin, Palmetine,

Isocolumbin, Aporphine

alkaloids, Jatrorrhizine,

Tetrahydropalmatine

 

Magnoflorine                        Berberine

1.      Viral infections

2.      Cancer

3.      Diabetes

4.       Inflammation

5.      Neurological disorders

6.      Immunomodulatory condition

7.      Psychiatric condition

 

ETHNOPHARMACOLOGICAL PROPERTIES:

Various parts of the plant contain immense medicinal property.

Table 2. Ethnopharmacological properties of Calotropis gigntea

Sl. No.

Plant parts

Medicinal uses33-36

1

Leaf

Skin ulcers, Leprosy, eye problems

2

Flower

Bile suppression, elimination of intestinal worms, coughs, colds and asthma

3

Bark

Analgesic, curative of fever, neurodermatitis, syphilis,(powdered bark) diarrhoea, dysentery, elephantiasis, leprosy,(stem bark) expectorant, and is used for dysentery, spleen complaints, convulsions, lumbago, scabies, ringworm, pneumonia.

4

Fruit

Piles, intestinal worms, eye problems, diabetes, abortive (fruit pulp).

5

Latex

Dysentery, leprosy, elephantiasis, epilepsy, asthma

6

Bud

Earache (Juice of young buds).

7

Seed

Leprosy and intestinal worms.

 

Table 3. Various uses of Calotropis gigntea in Ayurvedic medicine practice

Plant parts used

Disease

Medicinal therapy39-40

Flower

Coughs, Asthma

In inhalation therapy (smoke from the bark is inhaled). Flowers are collected, dried in sun shade, made into fine powder.1-2 pinches of this is mixed with little rock salt powder and used for chewing or else this combination can be taken along with warm water.

Leaves

Swelling

3-4 mature leaves of arka are collected and warmed in its ventral side (fine area). Little sesame oil is applied over it & placed over the swelling or inflamed area. 5-6 days regular fomentation helps to reduce the swelling effectively.

Joints

Mature leaves are made into fine paste without adding water. If necessary salt may be added to it. This paste is applied over inflamed joints. 2-3 days medication helps to reduce the pain and swelling very effectively.

Muscular pain, eczema

Leaves (50gm) are made into paste mixing sesame oil (200ml) and water (200ml) and are cooked till the water evaporates completely. It is filtered and stored. This can be applied over the painful joints as well as muscular pains.

 


Figure 2. Percentage view of reported works on plant parts of Calotropis gigantea

AYURVEDIC SIGNIFICANCE37-38:

In the Sanskit text, it is known as Arka and have the numerous beneficial effects in the treatment of both externally (Ksharasutra) and internally. The physists of ayurveda classified this herb under different classes based on their potency as given below31-32:

Charak  :               Bedaniya, Svedopaga, Vamonopaga

Susruta  :               Arkadi, Adhobahagahara,

Vaghata :              Arkadi

 

In Ayurvedic System of Medicine, the properties of this plant describe as Guna (Quality), Laghu (lightness), Ruksha (dryness), Tikshan, Rasa (Taste), Katu (pungent), Tikta (bitter), Vipak (Metabolism), Katu Virya (Potency), Ushan (Hot potency): Effect on Tridosha.

PHARMACOLOGICAL ACTIVITIES:

The phytochemical screening reveals the presence of numerous potent phytoconstituents which are responsible for its diversified pharmacological activities. The plant has much captivate due to following activities. From the literature survey it signifies different activities such as analgesic, anthelmintics, anti-asthmatics, anti-arthritic, anti-bacterial, anti-cancer, anti-convulsant, antidiabetics, anti-diarrhoeal, anti-histaminic, anti-inflammatory, anti-pyretic, anti-oxidant, anti-ulcer, cardioprotective, hepatoprotective, and wound healing. These activities were equally contributed to various plant parts such as flower, leaves, stems, roots, and latex (figure no. 2) and different biological activities were tabulated in table no 3.41-50


 

Table 4. Various pharmacological activities of Calotropis gigantea

Plant parts

Type of extract

Activity reported

Experimental design

Importance finding

Reference

 

Flower  

Ethanol extract

Analgesic

In-vivo acetic acid induced writhing, hot plate method (90 min).

250, 500 mg/kg showed 20.97% and 43% analgesia.

Pathak51 and Argal (2007)

Petroleum ether, ethanol (95%), water

Anti-asthmatic

In-vivo mast cell degranulation.

95% ethanol extract showed 72.25 % & 77.14 % protection at 400 and 600 mg/kg doses respectively.

Vadnere et52 al. (2010)

Methanol

extract

Anti-bacterial

In-vitro disk diffusion assay.

Highest inhibition against Escherichia coli (14 mm), Salmonella typhi (14 mm) and Shigellasonnei (11mm).

Jayakumar53 et al. 2010

Ethylacetate

extract

Anti-cancer

In-vivo effect on cell growth inhibition time.

200 mg/kg showed highest 71.24% inhibition of the Ehrlich′s carcinoma cells proliferation.

Habib et54 al. (2010)

Chloroform

extract

 

Anti-diabetic

Streptozotocin induced model.

LPO, SGPT, SGOT, alkaline phosphatase, cholesterol and triglyceride were decreased significantly  by the leaf and flower extracts.

Rathod55 et al. (2009b)

Alcoholic ,

aqueous  

Anti-helmintic

In-vivo Pheretima posthuma (earthworm) tested for paralysis and death time.

The aqueous 100 mg/kg exhibited 12 min for paralysis of earthworm and 21 min for death.

Argal56 and Pathak (2007)

Chloroform and ethanol extracts

Anti-infla-mmatory

In-vivo carrageen induced rat paw-oedema, cotton pellet induced granuloma model.

Both chloroform and ethanolic extracts reduced dry weight granuloma.

Kshirsagar57 et al. (2008)

Methanolic
extract

Anti-oxidant

In-vitro radical scavenging assays.

Stem showed antioxidant activity 31.43% 40.89% and 65.89%  at different dose levels(400, 600 and 800 mg/kg)

Jayakumar53 et al. 2010

Ethyl acetate

extract

Anti-tumor

In-vivo ehrlich′s ascites carcinoma model.

200 mg/kg (i.p) showed highest inhibition (71.24%) against Ehrlich′s ascites carcinoma cell lines.

Habib et al. 58 2010

Ethanolic

extract

Hepatoprotective

In-vitro paracetamol induced hepatotoxicity.

Significant decrease in serum enzyme levels, when animal were treated with ethanol extract.

Kshirsagar59 et al. (2009)

Leaves

Aqueous extract

Anti-bacterial

Agar well diffusion method.

Highest antibacterial activity reported for  for Escherichia coli and least for Klebsiella pneumonia.

Kumar 60et al. (2010)

Aqueous extract

Anti-bacterial

In-vivo artemianauplii hatching test and brine shrimp method.

Lower concentration (5 mg/ml) decreased no. of colonies, higher concentration(20 mg/ml) showed complete inhibition of Vibrio alginolyticus.

Baskaralinga61m et al. 2012

Hexane and

Methanol

extracts

Anti-bacterial

In-vitro agar well diffusion method

Zone of inhibitions for Escherichia coli, Bacillus subtiis and Staphylococcus aureu were found to be 23.5, 12. 5 and 16.5 mm respectively.

Jain62 et al. 2010

Methanolic

extract

 

Anti-bacterial

In-vitro disc diffusion assay

Highest inhibition against Escherichia coli, Salmonella typhi and least inhibition against Shigella sonnei.

Jayakumar63 et al. 2010

Hydro-alcoholic extract (70:30)

Anti-oxidant

In-vitro DPPH free radical scavenging, Nitric oxide scavenging, reducing power assay, In-vitro assay for total phenolics, flavonoids, tannin contents (Folin–Ciocalteu reagent).

% age inhibition of free radicals in DPPH (85.17%) in nitric oxide scavenging assay (54.55%), TPC (6374.17 mg gallic acid equivalent/dry weight), tannins (0.52% mg gallic acid equivalent/dry weight) and flavonoids (46.9771.95 mg quercetin equivalent/ dry weight) were reported in the hydro-alcoholic extract (70:30).

Singh64 et al. (2010)

Pet. ether

Chloroform

Acetone

Methanol

extracts

Hepato-protective

In-vivo carbon tetrachloride induced hepatotoxicity.

ALP levels were decreased significantly by chloroform & methanol extracts. SGPT levels were significantly reduced by silymarin, methanol & chloroform extracts.

Usmani65 and Kushwaha, 2010a

Methanol,

acetone

pet.ether

chloroform

extracts

 

In-vivo acetaminophen induces hepatotoxicity.

 

Silymarin, chloroform and methanol extracts showed significant decrease in SGPT. Methanol extract and Silymarin showed significant decrease in SGOT, ALP and bilirubin levels.

Usmani66 and Kushwaha (2010b)

Root

Methanolic

extract

Anti-asthmatic

Nitric oxide and Total Protein analysis, Measurement of lung wet/dry (W/D) weight.

200 and 400 mg/kg, p.o. significantly decreased the count of eosinophils, neutron-phils, lympocytes and total leucocyte count in the bronchoalveolar lavage.

The nitric oxide and total protein levels in bronchoalveolar lavage are decreased

Bulani67 et al.

(2011)

Root bark

Ethanol extract

 

In-vivo histamine induced contractions, broncho-constriction haloperidol induced catalepsy and passive paw anaphylaxis.

Histamine induced contraction was decreased at 200 mg/kg of ethanol extract.   300 and 200 mg/kg extract showed potent activity in haloperidol induced catalepsy and paw oedema model.

Mayee68 et al.

(2011)

Root bark

Methanol

extract

Anti-cancer

 In vivo ehrlich ascites carcinoma study.

Methanol extract at 10 and 20 mg/kg, increased the life span by 43.90% and 57.07%, respectively.

Habib69 and

Karim (2011)

Root bark

Ethanolic extract

 

Anti-fungal

In-vitro disc diffusion assay.

Ethanolic extract showed antifungal activity against Aspergillus niger and Trichoderma harzianum.

Habib70 et al.

(2009)

Root bark

Methanol

Extract

Anti-tumor

In-vivo EAC in swiss albino mice.

Methanol extract and chloroform soluble fraction significantly increased the life span by 43.90% at 20 mg/kg’

Habib71 and

Karim (2011)

Peeled roots

Methanol

extract

CNS activity

In-vivo eddy′s hot plate, acetic acid induced writhings, locomotor activity, antianxiety activity, motor co-ordination activity, pentyl-enetetrazole induced convulsions.

No toxicity signs; In hot plate method maximum analgesic activity was observed after 30 min, in Acetic acid induced writhing Methods it showed a significant decrease at a dose of 500 mg/kg. But locomotor activity decreased at 250 & 500 mg/kg. The anticonvulsant activity was significant at 250 & 500 mg/kg.

Argal72 and

Pathak, 2006

Root bark

Ethanolic
extract

Cytotoxic

In-vitro brine shrimp lethality bioassay.

Ethanol extract at LD50 of 66.86 mg/ml was active.

Habib70 et al.

2009

 

 

 

 

 

 

 

Latex

 

 

 

 

 

 

 

 

 

Anti-arthritic

In-vivo Freud's complete adjuvant induced arthritis.

 

The levels were significantly increased in Hb, RBC, EPO, PCV, WBC, platelet count and ESR, decreased in  ALP, AST and ALT and  controlled in  TC, HDL, LDL, VLDL, TG, PL and FFA level.

Saratha73 and

Subramanian

(2012)

Aqueous

extract

Anti-bacterial

In-vitro well diffusion method.

In Aqueous extract there is a high MIC for Staphylococcus aureus (30.71), B. cereus (16.71) and Escherichia coli (24.67).

Kumar74 et al.

2010b

 

 

In-vitro, modified agar well diffusion.

It was reported that maximum inhibitory activity was shown by latex against Escherichia coli, Bacillus cereus Staphylococcus aureus.

Kumar75 et al.

2010

Ethanolic

extract

Anti-fungal

In-vitro disc diffusion.

 

Antifungal activity and MIC showed highest in Candida Albicans (3mg/disc.) and Saccharomyces cerevisiae (8mg/ml) respectively, whereas lowest in Saccharomyces cerevisiae (3mg/disc.)  and    Candida Albicans(1g/ml) respectively.

Saratha76 and

Subramanian

(2010)

 

Wound Healing

In-vivo acute dermal toxicity,

(Incision & excision).

No toxicity signs; at 200 mg/kg significant wound healing reduced to 83.42%.

Nalwaya77 et al. 2009

Stem barks

Water extracts

Anti- convulsant

In-vivo maximum electroshock test (MES), pentylene tetrazole induced seizures (PTZ) study.

In both MES and PTZ the percentage incidence of convulsions showed decreased to 16% and 41% respectively.

Karki78 and Babu

(2010)

Ethanolic

extract

 

In-vivo carbon tetra chloride induced liver injury model.

In ethanol extract the parameters such as AST, ALT and LPO were significantly decreased and antioxidant parameters such as GSH, GPX, SOD and catalase levels were increased.

 

Lodhi79 et al.

2009

Water: ethanol(1:1)

Anti-pyretic

In-vivo acute toxicity study.

Stem bark extract (400 mg/kg i.p) significantly, lower the body temperature as well as rectal temperature.

Chitme80 et al. 2005

 


CONCLUSION:

Nature is the big basket of full of medicinal herbs which are benevolent to human kind since, time immemorial. Since last few decades, there is a rapid occurrence of the deadliest diseases across the world; it forced us to reinvestigate the plant profile systematically. One such plant is reviewed, i.e., Calotropis gigantea. The literature survey shows that a limed work has been reported in the latex part. This milkweed (arka) shows a numerous biological activities. Still there is very few mechanistic pharmacological investigation works were documented.  In this review, the percentage of the research work in respect to different plant parts was documented. This informative article also emphasize the absence of pharmacological activity study on plant parts like stem bark, flower twig etc.  Henceforth, this review article may play a significant role in near future to explore the novel therapeutic phytoconstituents.

 

ACKNOWLEDGMENT:

The authors are grateful to School of Pharmaceutical Sciences (Deemed to be University) for providing necessary facilities.

 

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Received on 06.11.2018           Modified on 21.01.2019

Accepted on 10.03.2019         © RJPT All right reserved

Research J. Pharm. and Tech. 2020; 13(1): 461-467.

DOI: 10.5958/0974-360X.2020.00090.6