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Exploring the Potential
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Chapter 14
of Calotropis procer
a in
Pharmacological Approaches
PoonamBansal, SunaynaChoudhary, TanviTaneja, SonaliSangwan, BhupeshGupta, SoniyaGoyal, RamanKumar and PoojaSharma
Abstract
Medicinal plants have been a source of treatments for many ailments for thousands of years. The WHO estimates that  of worldwide population use traditional medi­cines to treat common health issues. Plant derived bioactive substances constitute  of Western medications. The increase in incidents of emerging medical challenges, including post-COVID syndrome, rising multidrug-resistant (MDR), and many more, has raised annual fatalities. To address these issues, novel medications and strategic approaches are urgently required. Designing novel drugs relies on exploring medicinal plants, which have great scope in combating diseases. Calotropis procera is a medicinal plant belongs to Apocynaceae family and subfamily Asclepiadoideae that have been exploring for developing novel drugs. C. procera consists of numerous phytochemicals including flavonoids, terpenoids, cardenolides, steroids and oxypregnanes. Therefore, its phytoconstituents have been used to treat a variety of conditions including cancer, asthma, epilepsy and snake bite. C. procera is reported to have anti-inflammatory, anti- tumor, anthelmintic, antibacterial, antinociceptive and antimalarial properties. Roots, leaves and flower of C. procera have been used in wide range of ethnomedicinal and pharmacological actions including leukoderma, malaria and eczema. Recent ongoing techniques including computational tools using the phytoconstituents of C. procera against various diseases will open up avenues for developing novel drugs.
Keywords: Calotropis procera, anti-inflammatory, antibacterial, antimalarial, drugs
. Introduction
For thousands of years, plants have been the only source of treatments to treat both human and animal illnesses []. Medicinal plants (MPs) are the primary source of basic healthcare in underdeveloped nations [,]. According to World Health Organization (WHO), approximately  of the world’s population relies on traditional medicines, primarily on MPs, for their everyday health problems. Also,  of Western medications contain bioactive substances derived from plants[].
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Adramatic increase in fungal diseases over the past few decades has caused the dispersion of fungal spores across the soil and the environment. As a result of exces­sive fungal spore exposure, numerous illnesses, such as sinusitis, lung infections, and skin infections, are reported to be increased in people with impaired immune systems []. Similar to fungal diseases, microbial diseases have historically been the leading cause of mortality []. Currently, multidrug-resistant (MDR is solely to blame for about , of the , annual deaths caused by resistant infections. By , drug-resistant illnesses will result in  million annual fatalities [].
To address antibiotic resistance, new medications and alternative therapies (like traditional plant-based medicines, bacteriophage therapies, and combinational thera­pies) are urgently required [,]. World Health Organization strongly emphasizes developing novel antibiotics to combat resistant diseases []. Since the dawn of civi­lization, phytochemicals such as alkaloids, terpenoids, tannins, steroids, coumarins, and flavonoids derived from medicinal plants have a great scope to combat diseases. Essential oils and phenolic acids from Petroselinum crispum, Levisticum officinale Koch, Ocimum basilicum, Thymus vulgaris, Syzygium aromaticum alter the physiology of bacteria such as Bacillus cereus, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, and Salmonella by increasing cell permeability, altering the bacterial cell wall and membrane integrity, losing ATP, and inhibiting protein synthesis.
Compared to synthetic antimicrobials, medicinal plants are thought to have fewer side effects and exhibit varying degrees of efficacy against microbial infections [,,]. Co-administration of antibiotics and non-antibiotic substances breaks down resistance and is a successful strategy for enhancing or restoring antibiotic efficacy []. This chapter describes the morphological description of C. procera and its phytochemical constituents or pharmacological properties described briefly.
. Calotropis procera
The plants Calotropis procera referred to as “Raktha Arka”, in traditional Ayurvedic medicine. It serves a variety of functions. The plant fibers are used to make baskets, ropes, bags, and nets. The wood serves as both fuel and building material. The leaves of the plant serve as the animal’s food. The plant’s latex is a crucial component of many folk medicines. The common names [] of the plant are summarized in
Table  . The taxonomic classification of C. procera is tabulated in Tabl e .
Country Nam es
India Sanskrit- Arka, Ganarupa, Mandara, Vasuka, Svetapushpa, Sadapushpa, Alarka, Pratapass
Hindi- Aak, Madar
Kannada- Ekka
Tamil and Malayalam- Erukku
Telugu- Jilledi, Puvvu
Malaysia Remiga, Rembega, Kemengu
Indonesia Sundanese and Madurese- Bidhuri
Javanese- Sidaguri
Aceh- Rubik
Philippines Tagalog- Kapal-kapal
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Country Nam es
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Laos Kok May, Dok Kap, Dok Hak
Thailand Northern- Po Thuean, Paan Thuean
Central- Rak
Vietnam Bootng, Lashen, Nam Tit Bat
French Faux arbre de soie, Mercure vegetal
English Giant Indian milked weed, Madar and Sodom apple
Turkey Ipekag
Arab Oshar or Ushar
Persia Kharak
Pushto Spalmai
Table 1. Vernacular names of C. procera.
Taxonomic classification
Kingdom: Plantae
Subkingdom: Tracheobionta
Super division: Spermatophyta
Division: Magnoliophyta
Class: Magnoliopsida
Order: Gentianales
Family: Asclepiadaceae
Genus: Calotropis
Species: C. procera
Table 2. Taxonomic classification of C. procera.
. Distribution
Calotropis procera is a perennial plant belonging to the family Apocynaceae. The plant is abundant in Asia, America, Africa, Afghanistan, Algeria, Burkina Faso, Cameroon, Chad, Cote d’Ivoire, the Democratic Republic of the Congo, Egypt, Eritrea, Ethiopia, Gambia, Ghana, Guinea-Bissau, Pakistan, and India. It thrives as a wild shrub across Punjab, especially on plain pastures and roads []. Calotropis grows wild up to  meters (msl) throughout the nation [] and is tolerant to salt, and likes disturbed environments. It readily establishes as a weed along deteriorated roadways, lagoon edges, and overgrazed native grasslands and is propagated by seeds spread by wind and animals. It prefers abandoned agriculture sites and frequently predominates there, especially in places with disturbed sandy soils and little rainfall. It is believed to be a sign of overcrowding. It is the first vegetation to grow on arid soil and is tolerant of drought []. The xerophytic adaptations include the presence of latex, a profoundly branching root system, and thick leaves covered with wax.
The vegetative characteristics of plant are summarized in Table  [].
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Vegetative characters Description
Habit Shrub or a small tree up to .m (max.m) height.
Roots Simple, branched, woody at base and covered with a fissured; corky
Leaves Opposite-decussate, simple, sub sessile, extipulate; blade-oblong
Flowers Bracteate, complete, bisexual, actinomorphic, pentamerous,
Floral characteristics Inflorescence- A dense, multiflowered, umbellate, peducled cymes,
Calyx Sepal five, Polysepalous, five lobed, shortly united at the base,
Corolla Petals five, gamopetalous, five lobed, twisted aestivation.
Androecium Stamens five, gynandrous, anther dithecous, coherent.
Gynoecium Bicarpellary, apocarpus, styles are united at their apex, peltate
Fruit A simple, fleshy, inflated, subglobose to obliquely ovoid follicle up
Seeds Many, small, flat, obovate, ×mm, compressed with silky white
bark; branches somewhat succulent and densely white tomentose; early glabrescent. All parts of the plant exude white latex when cut or broken.
obovate to broadly obovate, –×.–.cm, apex abruptly and shortly acuminate to apiculate, base cordate, margins entire, succulent, white tomentose when young, later glabrescent and glacouse.
hypogynous, pedicellate, pedicel –cm long.
arising from the nodes and appearing axillary or terminal.
glabrescent, quincuncial aestivation.
stigma with five lateral stigmatic surfaces. Anthers adnate to the stigma forming a gynostegium.
to cm or more in diameter.
pappus, cm or more long.
Table 3. Vegetative characters of C. procera.
. Phytochemistry of C. procera
C. procera contains cardenolide, triterpenoids, alkaloids, resins, anthocyanins, and other compounds. In addition to this it also contains hydrocarbons, saturated and un saturated fatty acids. Different phytoconstituents isolated from different parts of
C.procera were tabulated in Table .
Plant part Compounds present References
Leaves a-amyrin []
a-amyrin-acetate
β-sitosterol
Urosolic acid
Cardenolide []
Calotropin []
Calotropagenin []
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Plant part Compounds present References
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Latex Caoutchouc []
Calotoxin []
Calactin []
Uscharin
Trypsin []
Voruscharin
Uzariginin
Syrioginin []
Proceroside []
Flower Queretin--ratinoside []
Sterol []
D-arabinose []
Glucosamine []
L-rhamnose []
Bark Triterpenes []
Pentacyclic triterpinoides []
Calotropursenyl acetate []
Apundarol isovalerate []
Querecetin--rutinoside []
Table 4. Phytoconstituents of C. procera.
. Traditional uses
Ancient Egyptians utilized C. procera as a medicinal plant throughout the Neolithic period in Egypt. The plant is a part of Greco-Arab medicine [] and is traditionally used across  nations worldwide. The plant is also used in Ayurveda, Siddha, Unani, and Sudanese traditional systems of medicine. It is important to note that C. procera has been used more commonly to treat a variety of infectious disorders that may be generally divided into five categories:
. Leprosy, boils, carbuncles, scabies, leishmaniasis, and infections of the skin,
mouth, and teeth are examples of skin and dermal infections.
. Respiratory infections include pneumonia, bronchitis, bronchial asthma, cough.
. GIT infections include dysentery, diarrhea, cholera, gastritis, colitis, and worms.
. GU infections include chronic renal failure and leucorrhea.
. Systemic infections include malaria and both internal (oral) and external
(topical) preparations have used C. procera.
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Parts Uses
Leaves In leukoderma (skin disease); an antidote for rabies; prompt healing; applied for a poultice;
Flower Treat skin and gum infections; used in dysentery and antidote for scorpion bite.
Root Used as a digestive; to treat body pain, malaria, eczema, leprosy elephantiasis, asthma,
Table 5. Ethnomedicinal uses of C. procera.
treat migraine, fever, eczema, leprosy, elephantiasis, asthma, cough, and rheumatism).
cough, and rheumatism.
However, given its increased usefulness in treating cutaneous infections, external or topical applications are more prevalent. Ethnomedicinal uses of Calotropis procera are summarized in Table .
. Medicinal activity
This highly effective shrub is used in numerous widespread and traditional medicines to treat various illnesses like fever, leprosy, eczema, diarrhea, dysentery, and jaundice [,]. The plant has reported anti-inflammatory, anti-tumor, anthel­mintic, hepatoprotective, antioxidant, anticonvulsant, antibacterial, oestrogenic, antinociceptive, and antimalarial properties (Figure ).
. Antioxidant activity
The anti-inflammatory and anti-hyperglycemic effects of Calotropis procera’s dry latex (DL) were demonstrated in rats that had been given an alloxan-induced diabetes model. In daily oral treatment of DL at dosages of  and mg/kg, a dose-dependent drop in blood sugar and an increase in hepatic glycogen content were seen. Additionally, DL slowed the loss of body weight in diabetic animals and decreased their daily water intake to levels comparable to those of rodents without diabetes. Additionally, in rats with alloxan-induced diabetes, DL reduced the levels of thiobarbituric acid-reactive substances (TBARS) while increasing the levels of endogenous antioxidants like catalase, glutathione, and superoxide dismutase (SOD). Comparable to glibenclamide, a popular anti-diabetic drug, DL proved effective as an antioxidant and an anti-diabetic agent [].
The antioxidant activity (free radical scavenging capacity) of the methanolic extract of C. procera roots was evaluated by the in-vitro DPPH scavenging assays. The IC value was found below μg/ml, indicating the plant’s potent antioxidant activity.
. Antimicrobial activity
Calotropis procera seeds were extracted using chloroform and methanol and have been tested on a paper disc for possible in vitro antibacterial activity. The chloroform extract of the seeds showed superior antibacterial action []. The stems, fruit, leaves, and flowers of C. procera, as well as its n-hexane, ether, chloroform, and water fraction, were extracted with  methanol and water, and their antibacterial activity was inves­tigated. The antibacterial and antifungal effects of the plant fractions were evaluated
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Figure 1.
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Health benefits of C. procera.
using Klebsiella pneumoniae and Aspergillus niger, respectively. The test extracts with a concentration of mg/mL were used in the study. On Muller Hinton agar for bacteria and Yeast Peptone Glucose (YPG) agar for fungi, which had previously been seeded with the microbial inocula of . MacFarland density, a volume of L of each exam­ined extract sample was detected. The inhibition zones on the inoculation plates were measured in mm after a -hour period of °C incubation. The plant’s flower extract showed the greatest antibacterial activity in the n-hexane and ether fractions.
. Anti-inflammatory activity
The anti-inflammatory impact of C. procera was tested using the various acute and chronic models of inflammation. Oral administration of dried latex of C. procera significantly inhibited edema formation induced by carrageenan and Freund’s Adjuvant []. The plant also has potent anti-inflammatory effects against cotton pellets and carrageenan-induced granulomas in albino Wistar rats. The methanolic extracts