A Comprehensive Overview of the Pharmacological Impacts, Active Phytochemical Elements, and Pharmacognostic attributes of
Calotropis gigantea

 

Parthika Patel*, Isha Patel

Department of Pharmaceutics, SSR College of Pharmacy, Silvassa - 396230, India.

*Corresponding Author E-mail: parthikapatelssrcp@gmail.com

 

ABSTRACT:

A botanical survey and comprehensive information about the Calotropis gigantea plant are included in this article. Recent years have seen a great deal of research on potential medical uses for it utilising cutting-edge scientific methods. Numerous bioactive substances that were extracted from various plant parts have been discovered and subjected to pharmacological analysis. This plant is a wonderful source of pharmaceutical compounds because of its therapeutic characteristics. Studies conducted in preclinical settings have demonstrated the potential benefits of extracts from Calotropis gigantea for the treatment of inflammatory diseases, diabetes, and cancer. To assess the safety and effectiveness of medications based on Calotropis gigantea for use in humans, additional study is necessary to clarify the underlying mechanisms of action. More studies into its pharmacological characteristics may lead to the creation of innovative medications and efficient treatments for a range of illnesses. This paper compiles information on the pharmacology, phytochemistry, biological activity, ethnobotany, and toxicity of C. gigantea.

 

KEYWORDS: Calotropis gigantea, Pharmacological activities, Phytochemical elements, Therapeutic uses, Toxicity.

 

 


INTRODUCTION:

Calotropis gigantea, also known as Arka, is a significant Ayurvedic drug that has been used in a country namely, India since ancient times.1 It was first mentioned by Hindu authors, and the plant's ancient name, Arka, refers to the fact that the plant was used for in sacrificial rites including- upon prosperous moments, Lord Shiva is presented Akra coupled with exceedingly poisonous Dhatura (in botanical terms known as Datura metel) flowers.

 

 

Also the shrub is commonly observed on the grounds of Indian temples. Two common species of CalotropisCalotropis gigantea (Linn.) R.Br. and Calotropis procera (Ait.) R.Br.—are both species that are commonly found in India. Calotropis gigantea is ever-green perennial potential shrub generally found in tropical regions like India, Southern China, Malaysia, etc. It is also known as crown flower, giant milkweed, and shallow wort. It’s popularly called ‘rui’ and ‘akra’ in other languages i.e., Marathi and Hindi in parts of India. It's utilized as a traditional herb for medicine all throughout the world.2

 

It typically reaches a height of about 2.5-4m, and it belongs to the family of Apocynaceae. Its bark is yellowish white, its stems are milky, and its oval leaves are light green. Because it generates a lot of latex, it is well-known and goes by the name milkweed and swallowwort. Many biologically active substances, such as tannins, glycosides, and many proteins, are found in latex.3

Calotropis is a multipurpose medicinal plant whose powerful therapeutic characteristics have been used for ages to treat a wide range of health issues, according to their pharmacological implementation. Its applications span a wide spectrum, from alleviating bronchitis, pain, and asthma to tackling more complex conditions like leprosy, ulcers, piles, and spleen disorders. Additionally, it has been relied upon to combat tumors, liver ailments, abdominal discomfort, and dyspepsia, while also serving as a remedy for common afflictions such as colds, fever, diarrhea, rheumatism, indigestion, eczema, and jaundice. The plant's various components each offer unique healing capabilities. Calotropis oil is used to cure Hemiplegia by massaging onto paralyzed limbs, is believed to stimulate circulation and promote mobility. Finally, the purgative qualities of Calotropis are harnessed through the consumption of its juice, aiding in digestive cleansing and detoxification.4

 

In addition, these perennial flowers are used in many kinds of floral arrangements in Thailand. They were also claimed to have been a favorite of the Hawaiian queen Liliuokalani, who wore them strung into leis and considered them a symbol of royalty.

 

 

Figure 1. Stem, leaves and flowers of Calotropis gigantea.

Figure 2. Flowers of Calotropis gigantea.

 

PHARMACOGNOSTIC ATTRIBUTES OF CALOTROPIS GIGANTEA-

The term "pharmacognostic attributes" refers to a plant's therapeutic qualities and traits that are pertinent to its application in complementary and alternative medicine. These characteristics are essential for classifying, assessing, and guaranteeing the efficacy of therapeutic plants. Morphological characteristics, microscopic features, chemical composition, pharmacological activities, toxicity, and geographic distribution are the primary pharmacognostic properties. Additionally, its synonyms, taxonomy, and conventional applications are also mentioned.

 

 

 

 

Synonyms of Calotropis gigantea:

Table 1. List of synonyms of Calotropis gigantea.

Sr.

No.

Category of synonyms

Synonyms of Calotropis gigantea

1

Homotypic Synonyms

Madorius giganteus (L.) Kuntze

Asclepias gigantea L.

2

Heterotypic Synonyms

Periploca cochinchinensis Lour.

Streptocaulon cochinchinense

3

Regional synonyms5

Bengali- Akanda Phool

Gujarati- Aakando

English- Bowstring hemp, crownplant, crown flower.

Indonesia- Bidhuri, sidaguri, rubik.

Philippines- kapal-kapal.

Thailand- Po thuean, paan thuean.

French- Mercure vegetal.

 

Taxonomical classification:6

Table 2. Taxonomical classification of Calotropis gigantea.

Kingdom

Plantae

Super division

Spermatophyta

Class

Dicotyledons

Series

Bicarpellate

Order

Gentianales

Family

Apocynaceae

Genus

Calotropis

Species

Calotropis gigantea

 

Biological distribution:

The Asclepiadaceae family comprises 180 genera and 2200 species, which is primarily found across tropical as well as subtropical regions of the world. Plant is native to the Monsoonal areas of Afro-Asia and widely available throughout India, from which it expanded towards the Arabian Peninsula, northwest Africa (Mauritania, Senegal), and Kanyakumari, Bangladesh, Burma, and Pakistan. Sub-Himalayan tracts are where the plants are most numerous. It also demonstrates the occurrence of flowers in Islands of Mascarene, subtropical America, and Australia's arid regions. It is a native plant to India that rises to a height of 1,300 meters above sea level in semi-arid climates with 150–1000 mm of yearly rainfall. A vast variety of soil textures and changes in the ecoclimate are tolerable to plants., and they can flourish on sand with an annual rainfall of 350–450 mm (low rainfall), overly drained soils as well as abandoned land. Plant seeds are spread by animals and the air. 7

 

It can withstand heat, humidity, salinity in the soil, and salt spray from the beach well. It is an extremely adaptive plant that can tolerate 2000 mm of precipitation annually and spreads quickly in an open environment with no competition. It thrives in overgrazed native fields, grasslands, and degraded roadside ditches. It exhibits remarkable adaptation to biological structures.8 When damaged, the roots easily produce suckers that grow back quickly and produce adventitious shoots.9

 

 

 

When exposed to temperature fluctuations between 25 and 45 degrees Celsius, Calotropis gigantea's pH fluctuates between 7.2 and 8.1; at 45 degrees Celsius or higher, a stable pH of 8.1 was found.10 It's unclear if this indicates overcrowding. It is an odd plant that grazing animals do not eat. The plant with a waxy film covering its broad, thick leaves is an example of a xerophytic adaptation with a multipored root system.

 

Cultivation and collection:

The cultivation occurs due to free floating seeds in the air. Calotropis has been grown for its fibers at a distance of 1-1.5 meters throughout the region of South America and Caribbean Islands.

 

 

In large-scale plant multiplication, stem and root cuttings are an excellent method of vegetative propagation. When grown, annual yields of up to 500 kg/ha are predicted. It is better to have one harvest per season as opposed to two or three, as the former saves total energy expenditure in the form and processing facilities. It works well for intense energy harvesting in somewhat dry or dry settings wherein coldness isn't an obstacle to growth.11

 

Macroscopic characteristics:12

Calotropis gigantea is a straight shrub and well branched. Calotropis gigantea is bulky shrub; grows like a small tree with clusters of waxy flowers whitish in color. It is a multi-flowered plant.


 

Table 3. Macroscopic characteristics of Calotropis gigantea.

Sr.

No.

Part of the Plant

Macroscopic characteristics

1

Root

The roots of C. gigantea are round, spherical, convoluted, and repeatedly branching. Fissured and corky, yellowish-colored bark covers the root system. The root system is 3–10 cm in diameter and has an inside color of stoneware white. There is also an abundant production of pale latex from cuts or wounds in the bark.

2

Root Bark

The root system's bark is short, curled, and peels off at regular intervals. It is 2-4 mm thick, highly mucilaginous, and tastes bitter. The outside of the bark is yellowish grey and the inside is yellowish white in color.

3

Flower

Calotropis gigantea flowers include a delicate crown at the center of each bloom, which houses the stamens. In nature, flowers are bracteates, actinomorphic, bisexual, and pentamerous (having five pointed petals). flowers that lack scent. The peduncled cyme of the flower emerges from nodes and shows up at the terminal.

4

Calyx

Polysepalous, five lobed, glabrescent, and rapidly joined at the base. The androecium includes 5 gynandrous stamens with consistent and dithecous anther which makes sound.

5

Leaves

The plant has oval, milky, pale green, yellowish-green leaves. The leaves are 5 to 30 X 2.5 to 16 centimeters and are simple, subsessile, opposite decussate, exstipulate, elliptic in nature. The leaf's apex is quickly edged to become cordate at the base side and apiculate. Calotropis gigantea leaf in its entirety, with white, short, tomentose petioles at the borders.

6

Seeds

Calotropis gigantea seeds are small, flat, oblong, and have white, silky hair on one side that measures around 3–4 cm in length. Its seeds freely float in the air.

 

Table 4. Microscopic characteristics of Calotropis gigantea.

Sr. No.

Part of the Plant

Microscopic characteristics

1

Root

In the transverse section, the cork is an upper outermost circular layer consisting of 15 to 20 rectangular cell arrangement without any intracellular space in compact manner. Large numbers of starch grains are present in cells of cortex section. Parenchymatic cells are asymmetrical and irregular in shape and have laciferous tubes and a badge of calcium oxalate.

2

Leaves

In the transverse section, both surfaces of leaves have epidermal cells, which are shielded from the elements by a thick layer of cuticle that is striated and rigid. Also, xylem consists of vessels and tracheid.

3

Stem

It consists of epidermis, cortex, and endodermis. Epidermis is considered to be the outermost layer with thick cuticles. Cortex is present below epidermis, and it is collenchymatous in nature. Endodermis cells are an arrangement of uniform cells that form a curved ring surrounding the system of arteries and veins.

 


Chemical constituents:14–16

Table 5. Calotropis gigantea consists of following chemical constituents.

Sr. No.

Chemical constituents

1

Alkaloids

2

Carbohydrates

3

Glycosides

4

Saponins

5

Fixed oils and fats

6

Phenolic compounds and tannins

7

Proteins and free amino acids

8

Gums and mucilage

9

Sterols

10

Volatile oils

 

 

 

Microscopic characteristics:13

Cellular features and tissues that are essential for differentiating between plant species can be seen by microscopy. This involves looking for distinctive cellular patterns or structures on the surface of leaves, stems, and other plant parts.

 

Traditional uses:17

Table 6. Traditional uses of different parts of Calotropis gigantea.

Sr.

No.

Part of the Plant

Traditional uses

1

Latex and Leaves

Swelling, Joint pain, wound healing

2

Stem

Skin diseases, Leprosy, Intestinal worms, Leukoderma

3

Root

Elephantiasis, Cough, Diarrhea, Leprosy, Asthma, Rheumatism

Toxicity of Calotropis gigantea:18–22

The plant is poisonous throughout, with the stems and roots being more so than the leaves. Indigenous people have fashioned toxic arrows for hunting using the latex from plants. The plant Calotropis is poisonous. Calactin, calotropin, uscharin, and calotoxin are the active principles.

 

When cut, the stem and leaves produce a viscous, milky fluid. Reversible vision loss and toxic keratoconjunctivitis are reported to be caused by the milky latex sap of Calotropis gigantea. Crown flower keratitis is an uncommon ailment that typically arises from inadvertent contact with the sap in the eyes. Crown flower keratitis can occur when you touch the sap and then the ocular surface when crafting a Hawaiian lei flower necklace. Reduced vision acuity and corneal stromal oedema are the consequences of damage (poisoning) to the corneal endothelium. Despite the corneal endothelium suffering some irreversible damage, as evidenced by a lower number of endothelial cells and an uneven shape.

 

Thereby latex appears to be quite harmful to people's eyes; it has an ophthalmic toxic impact that reduces vision and induces photophobia. When accidentally falls onto the skin, it produces vesication and redness. When used orally, the juice causes vomiting, diarrhea, dilated pupils, tetanic convulsions, collapse, and death in addition to an unpleasant, bitter taste and burning sensation in the stomach and throat. Six to twelve hours is the deadly time.

 

Calotropis gigantea is more toxic than Calotropis procera and is said to be even more lethal than cobra venom. The poisonous principles are calcin, uscharin, calcotropin, calcotropage, and calcotoxin. Owing to its irritant, neurotoxic, and anticholinergic properties, milk can be toxic and can manifest in various deadly forms. Serum contains 3% quantities of gigantin, an exceedingly toxic toxin.

 

Active phytochemical elements of Calotropis gigantea:23–26

Table 7. List of active chemical compounds found in different portions of the Calotropis gigantea species.

Sr. No.

Part of plant

Active phytochemical constituent

1.

Leaves

  Amyrin

  Amyrin acetate

  Urosolic acid

  Cardenolides

  Calotropin

  Calotropagenin

  β-sitosterol

2.

Latex

  Caoutchouc

  Calotropin

  0.15% Calotoxin

  0.15% Calactin

  0.45% Uscharin

  Trypsin

  Voruscharin

  Uzarigenin

  Syriogenin

  Proceroside

3.

Flowers

  Akundarin

  α-calotropeol

  β-calotropeol

  Amyrin

  Mudarine

  Asclepin

  Lupeol

  Gigantin

  Giganteol

  Isogigenteol

4.

Bark

  Calotropterpenyl ester

  Calotropursenyl acetate

  Calotrofriedelenyl acetate

  Akundarol isovalerate

  Mundarol isovalerate

  Quercetin -3- rutinoside

 

Pharmacological impacts of Calotropis gigantea:27–50

Anti diarrheal activity

CNS activity

Wound healing activity

Pro-coagulant activity

Antimalarial activity

Analgesic activity

Anti oxidant activity

Vaso dilation effect

Anti microbial activity

Anti pyretic activity

Hepatoprotective activity

Anti inflammatory activity

Anti asthematic activity

 

      Anti-diarrheal activity:

Calotropis gigantea blocks the release of prostaglandins from the intestinal mucosa thereby improving intestinal motility and secretion. The plant Calotropis gigantea greatly lessens the frequency and intensity of diarrhea. Calotropis gigantea reverses the mechanism which causes diarrhea by activating the chloride ion channel, which causes the chloride ion to be effluxes from the cell and causes a large outflow of water towards the lumen of the intestines.

 

      CNS activity:

Calotropis gigantea extract boosted neuron growth at an early stage. Calotropis gigantea exhibits enhanced axon and dendrite dimensions, numerals, and order of branches. Calotropis gigantea produces a few neuropharmacological effects, including analgesic, antidepressant, sedative and hypnotic, antianxiety, and neurogenesis, because it includes the flavonoids chrysin and apigenin.

 

      Wound healing activity:

Calotropis gigantea acting as a Pro healer. Calotropis gigantea accelerates the epithelization process and raises the concentration of collagen, both of which aid in the healing of wounds. Calotropis gigantea raises hydroxyproline levels, which aids in collagen formation even more. Calotropis gigantea latex exhibits remarkable wound healing properties. C. gigantea’s latex was tested for wound healing activities in albino rats using excision and incision models. At 200 mg/kg/day dose, C. gigantea latex significantly improved wound healing, resulting in an 83.42% reduction in wound area compared to 76.22% for controls. Wounds treated with extract have a faster epithelization rate than controls.

 

      Pro-coagulant activity:

It’s claimed that C. gigantea latex has procoagulant properties. The latex extract of Calotropis gigantea hydrolyses human fibrinogen, casein, and crude fibrin in a dose-dependent manner. Latex extract hydrolyzes the different components of fibrinogen and vice versa. Fibrin clots are highly hydrolyzed compared to papain and trypsin. The latex of C. gigantea contains highly proteolytic proteins and are responsible for its procoagulant properties.

 

      Anti-malarial activity:

Malaria is a fatal parasite illness that causes death. Antimalarial activity against Plasmodium falciparum and Plasmodium berghei was demonstrated by Calotropis gigantea. Excellent Anti plasmodial action is demonstrated by Calotropis gigantea against plasmodium falciparum, which is susceptible to chloroquine. This action is produced against Plasmodium species.

 

      Analgesic activity:

Numerous preclinical studies have reported the analgesic efficacy of Calotropis gigantea flower extractions made with alcohol. The hotplate technique and the acetic acid-based writhing models are employed to study activity. Root peel extract of Calotropis gigantea also produces analgesic activity. An oral dosage of ethanolic extract of C. gigantea flower significantly reduced writhing and delayed paw licking.

 

      Antioxidant activity:

ROS are extremely reactive oxygen-bearing molecules, including free radicals. ROS can cause damage to biological components such as membrane phospholipids, proteins, and nucleic acids. ROS plays an important part in the progression of many illnesses. It’s observed that C. gigantea leaves have antioxidant properties. Additionally, it has been found that Calotropis gigantea lowers oxidative stress in Type II diabetes mellitus due to the existence of free radicals.

 

      Vasodilation effect:

Calotropis gigantea latex is a well-known source of active ingredients with a variety of biological functions, including the regulation of the heart muscle. The plant exhibits high dilatory activity at a fixed dose, possibly due to the presence of protein in raw latex extract with a strong basic character. Research indicates that the main way latex affects the cardiovascular system is through altering the permeability of cations (Ca, Na), which then activates the Calcium channels within the cardiac muscles promote blood circulation. Consequently, the dilating features most probably account for the latex's pharmacological effects.

 

      Anti-microbial activity:

Calotropis gigantea has been shown to have cytotoxic, antimicrobial, and antibacterial properties. Calotropis gigantea Linn's leaves and flower extract, in aqueous, methanolic, and ethanolic forms, exhibit strong antibacterial activity against Staphylococcus aureus. A water-based extract of C. gigantea latex has been shown to inhibit S. aureus, B. cereus, E. coli, and C. krusei. C. gigantea has been shown to have antifungal efficacy against plants pathogenic fungus such as Fusarium mangiferae, which pose a significant danger to mango agriculture.

 

      Hepatoprotective activity:

A study found that an ethanol-based extract of C. gigantea stems is capable of safeguarding male Wistar rats' livers from carbon tetrachloride-induced impairment. The extract helps safeguard rats from damage caused by oxidative stress. The leaf extracts in methanol and chloroform have excellent hepatoprotective properties. The extract effectively protected the liver and caused AST, ALT, and lipid peroxide levels to drop considerably.

 

      Antipyretic activity:

Calotropis gigantea extract from roots is predicted to provide an antipyretic action against fever due to the TAB vaccination as well as fever induced by yeast suggests that Calotropis gigantea may one day be developed into a potent and less costly antipyretic. The extract, administered intraperitoneally at doses of 200 and 400 mg/kg body weight, effectively decreased fever and restored normal body temperature.

 

      Anti-inflammatory activity:

The release of different chemical mediators is the cause of inflammation. The main culprit behind inflammation is prostaglandins. It has been discovered that Calotropis gigantea lowers prostaglandins and mediators that cause inflammation. An ethanol-based extract of C. gigantea demonstrated anti-inflammatory action against carrageenan-induced paw edema to Wistar albino rats. Oral dosing of 400mg/kg of C. gigantea demonstrated considerable anti-inflammatory efficacy, exceeding the effectiveness of 100mg/kg of Ibuprofen.

 

 

      Anti-asthmatic activity:

Calotropis gigantea demonstrated anti-asthmatic efficacy during OVA-induced asthma. Calotropis gigantea was tested at doses of 100, 200, and 400 mg/kg for its effects upon cells in the body, catalysts, and histopathology. Plant concentrate may help cure asthma. In bronchoalveolar lavage fluids, Calotropis gigantea may have an influence on the suppression of neutrophils, lymphocytes, and eosinophils (p<0.05). This plant, Calotropis gigantea, exhibits broncho-relaxation. The roots of Calotropis gigantea are said to contain α- and β-amyrin, which have anti-lipoxygenase properties.

 

CONCLUSION:

In recent years, ethnomedicine research has garnered increased attention, shedding light on the often-overlooked health benefits of plants. Pharmacological investigations into Calotropis gigantea have affirmed its therapeutic potential, solidifying its status as a valuable medicinal plant with diverse health-promoting properties. The exploration of modern pharmaceuticals derived from C. gigantea presents a promising avenue for addressing various health ailments, given the pharmaceutical community's interest in harnessing natural sources for drug discovery. A comprehensive research and development initiative is imperative to safeguard Calotropis gigantea, enhance its economic viability, and fully exploit its medicinal potential. The toxicity of Calotropis gigantea presents significant hazards. Its cardiac glycosides have the potential to seriously harm both humans and animals, causing gastrointestinal distress and even fatal heart abnormalities. To reduce the risk of accidental poisoning and minimize its health effects, proper handling and knowledge are essential.

 

 

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Received on 08.04.2024      Revised on 06.12.2024

Accepted on 14.05.2025      Published on 06.10.2025

Available online from October 13, 2025

Asian J. Pharm. Res. 2025; 15(4):396-402.

DOI: 10.52711/2231-5691.2025.00062

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