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Research: Pharmacological properties of Datura stramonium

Pharmacological properties of Datura stramonium L. as a potential medicinal tree: An overview
Priyanka Soni,1,* Anees Ahmad Siddiqui,2 Jaya Dwivedi,3 and Vishal Soni1

Datura stramonium (D. stramonium) is a widespread annual plant from the Solanaceae family. It is one of the widely well known folklore medicinal herb. It is a wild growing flowering plant and was investigated as a local source for tropane alkaloids which contain a methylated nitrogen atom (N-CH3) and include the anti-cholinergic drugs atropine, and scopolamine. From ancient civilization it was traditionally used for religious visionary purposes throughout the world and used by witchcraft in medieval Europe. The god lord Shiva was known to smoke Cannabis and Datura. People still provide the small thorn apple during festivals and special days as offerings in Shiva icons at temples. An extract made from the leaves is taken orally for the treatment of asthma and sinus infections, and stripped bark are applied externally to treat swellings, burns and ulcers. The incidence of D. stramonium poisoning is sporadic with a cluster of poisoning cases in the 1990s and 2000s, the United States media reported some cases occurring mostly among adolescents and young adults dying or becoming seriously ill from ingesting. Some medicinal uses of the plant are its anti-inflammatory property of all parts of the plant, stimulation of the central nervous system, respiratory decongestion, treatment of dental and skin infections, alopecia and in the treatment of toothache. It is a hallucinogenic plant that causes serious poisoning. Consumption of any part of the plant may result in a severe anticholinergic reaction that may lead to toxicity and occasionally cause diagnostic difficulties. Cases of poisoning have been reported after eating the berries. Death may occur from heart failure after ingesting 125 seeds, because the seeds contain the highest concentration and has a rapid onset of action, thus may be potentially useful as an alternative to atropine for the treatment of the muscarinic symptoms of organophosphate toxicity and some of central anticholinergic effects. The wide distribution, the strong toxicity and the potential for occurrence in foodstuffs are responsible for the numerous incidents in humans[2]. Datura genus distributes over tropical and warm temperate regions of the world. About ten species of Datura are found, of which Datura anoxia and D. stromonium are most important drug plants. Datura has long been known as a medicinal plant and as a plant hallucinogen all over the world. Pre-historic use of Datura in medicinal and ceremonial rituals could be observed in aboriginal in Indian sub-continent[3]. The therapeutic activities of most plants are due to the presence of one or more of such components like alkaloids, tannins, saponins and cardiac glycosides. The phytochemical screening revealed the presence of saponins, tannins, steroids, alkaloids, flavonoids, phenols and glycosides[4].Atropine and scopolamine are competitive antagonists of muscarinic cholinergic receptors and are central nervous system depressants. All parts of the plant are toxic, but the highest amount of alkaloids is contained in the ripe seeds[4],[5]. Many cases of accidental poisoning by D. stramonium have been reported when these plants were eaten accidentally[6].

Ethnomedical uses

Plant derived drugs come into use in the modern medicine through the uses of plant material as indigenous cure in folklore or traditional systems of medicine. The leaves of D. stromonium L. are used for the relief of headache and vapours of leaf infusion is used to relive the pain of rheumatism and gout. The smoke from the burning leaf is inhaled for the relief of asthma and bronchitis. European remedy of D. stromonium for haemorrhoid is to steam the part over boiling water containing leaf. The fruit juice is applied to the scalp for the treatment of falling hair and dandruff. It is also applied to smooth painful wounds and sores. Seeds and leaves of D. stromonium were used to sedate hysterical and psychotic patients, also to treat insomnia. D. stromonium was used as hallucinogenic drug. It is also used to relax the smooth muscles of the bronchial tube and asthmatic bronchial spasm. It was reported that D. stromonium was used internally to treat madness, epilepsy and depression. Externally it forms the basis of ointment for burns and rheumatism[12]. It is also used in the treatment of parkinsonism and hemorrhoids. Its leaves, applied after roasting, are useful in relieving pain. The bitter narcotic plant relieves pain and encourages the healing process. The seeds of the plant are medicinally the most active. Externally, the plant is used as a poultice in treating fistulas, abscesses wounds and severe neuralgia. Scopolamine is also found in the plant, which makes it a potent cholinergic-blocki hallucinogen that has been used to calm schizoid patients. Its leaves, containing hyoscyamine and atropine, can be used as an immensely powerful mind-altering drug. The seeds of Datura are analgesic, anthelmintic and anti-inflammatory and as such, they are used in the treatment of stomach and intestinal pain that results from worm infestation, toothache, and fever from inflammation. The juice of its fruit is applied to the scalp, to treat dandruff and falling hair. The growing plant works as an insect repellant, which protects neighboring plants from insects[2]. D. stromonium is mostly used as anthelmintics and antiparasitic in Marche, Abruzzo and Latium. Records of continued use of the plant in these sectors was collected from farmers and shepherds (mostly old people)[4],[13].

Phytochemicals

The major tropane alkaloids hyoscyamine and scopolamine and several minor tropane alkaloids have been identified in Datura species. Typical examples of minor alkaloids in D. stramonium are tigloidin, aposcopolamine, apoatropin, hyoscyamine N-oxide and scopolamine N-oxide17-20. 6â-ditigloyloxytropane and 7-hydroxyhyoscyamine are reported for the first time in this species[2].

Distribution of hyoscyamine and scopolamine in D. stromonium was studied. The production of hycyamine and scopolamine in D. stromonium has been investigated in the different plant parts, at different stages of their life cycle. The maximum contents were found in the stems and leaves of young plants, hyocyamine being always the predominate component. These compounds were included in many pharmacopieas because of their anticholinergic activities[4].

D. stromonium contain variety of alkaloids including atropine, hyoscamine and scopolamine[14].

Sixty-four tropane alkaloids have been detected from D. stramonium. Two new tropane alkaloids, 3-phenylacetoxy-6, 7-epoxynortropane and 7-hydroxyapoatropine were tentatively identified. The alkaloids scopoline, 3-(hydroxyacetoxy) tropane, 3-hydroxy-6-(2-methylbutyryloxy) tropane, 3â-tigloyloxy-6-hydroxytropane, 3, 7-dihydroxy-6-tigloyloxytropane, 3-tigloyloxy-6-propionyloxytropane, 3 phenylacetoxy-6,7-epoxytropane, 3-phenylacetoxy-6-hydroxytropane, aponor scopolamine, 3â, 6â-ditigloyloxytropane and 7-hydroxyhyoscyamine are reported for the first time for this species. Other alkaloids found in D. stramonium include[15]: Hygrine, 3á, 6â-Ditigloyloxy-7-hydroxytropane, 6-Hydroxyhyoscyamine, Pseudotropine, 3á-Tigloyloxytropane, Hydroxy-6-tigloyloxytropane, Phenylacetoxytropane, 3-Tigloyloxy-6-(2-methylbutyryloxy) tropane, Hyoscyamine, 3-Tigloyloxy-6-isovaleroyloxy-7-hydroxytropane, Scopolamine, Tropinone, Scopine, 6-Hydroxyacetoxytropane, 3,6-Diacetoxytropane, 3-Tigloxyloxy-6-acetoxytropane, 3-Tigloyloxy-2-methylbutyryloxytropane, 3á, 6â-Ditiglotoxytropane, 3-Acetoxy-6-isobutyryloxytropan, 3-(2-Phenylpropionyloxy) tropane, Littorine, 6-Hydroxyapoatropine, 3â, 6â-Ditigloyloxy-7-hydroxytropane, 3-Tropoyloxy-6-acetoxytropane, 3,6-Dihydroxytropane, 3â-Tigloyloxytropane, 3-Tigloyloxy-6-propionyloxy-7- hydroxytropane, 3á-Apotropoyloxytropane, Aposcopolamine, 3â, 6â-Ditigloyloxytropane, 3-(3′-Acetoxytropoyloxy) tropane, 3á-Tigloyloxy-6-hydroxytropane, Tropine, 3-Acetoxytropane, 3-Hydroxy-6-acetoxytropane, 3-Hydroxy-6-methylbutyryloxytropane, 3-Tigloloxy-6-isobutyryloxytropane, Aponorscopolamine, 7-Hydroxyhyoscyamine, Meteloidine, 3â, 6â-Ditigloyloxytropane.

The phytochemical analysis of the plant revealed that D. stramonium contained saponins, tannins and alkaloids and glycosides. The secondary metabolites identified in the plant materials in the study of Banso A and Adeyemo S showed antimicrobial activity[16].

Pharmacological activity

Antiasthmatic activity

D. stromonium in asthma treatment and possible effects on prenatal development was studied. Exposure of the foetus to D. stromonium when a mother use it for asthma, will cause a continuous release of acetylcholine, resulting in the desensitization of nicotinic receptors, this could ultimately result in permanent damage to the foetus. Therefore we conclude that this African herbal remedy should be used with caution during pregnancy[17].

Anticholinergic activity

The alkaloids found in D. stramonium, are organic esters used clinically as anticholinergic agents. Jimson weed has been reported as a drug of abuse and has been involved in the accidental poisoning of humans and animals. Symptoms of acute jimson weed poisoning included dryness of the mouth and extreme thirst, dryness of the skin, pupil dilation and impaired vision, urinary retention, rapid heartbeat, confusion, restlessness, hallucinations, and loss of consciousness. The anticholinergic syndrome results from the inhibition of central and peripheral muscarinic neurotransmission[18]–[20].

Acaricidal, repellent and oviposition deterrent properties

The ethanol extracts obtained from both leaf and seed in D. stromonium (Solanaceae) were investigated for acaricidal, repellent and oviposition deterrent properties against adult two-spotted spider mites (T. urticae Koch) (Acari: Tetranychidae) under laboratory conditions. Leaf and seed extracts, which were applied in 167.25 and 145.75 g/L concentrations, respectively (using a Petri leaf disc-spray tower method), caused 98% and 25% mortality among spider mite adults after 48 h. These results suggest that D. stramonium extracts could be used to manage the two-spotted spider mite[21].

Antimicrobial Activity

The methanol extracts of D. stromonium and Datura inoxia showed activity against Gram positive bacteria in a dose dependent manner. Little or no antimicrobial activity was found against Escherichia coli and Psuedomonas aeruginosa[22]. The anti-microbial activity of combined crude ethanolic extract of D. stromonium, Terminalia arjuna and Withania somnifera in cup plate diffusion method for antibacterial and antifungal activity. The extracts were subjected to screening to detect potential antimicrobial activity against Staphylococcus aureus, Bacillus subtilus, Escherichia coli, Klebsiella pneumoniae, Micrococcus luteus and Candida albicans with compare Ciprofloxacin standard drug[23].

Anticancer activity

An integrated approach is needed to manage cancer using the growing body of knowledge gained through scientific developments. Thousands of herbal and traditional compounds are being screened worldwide to validate their use as anti-cancerous drugs. D. stromonium in therapeutic dose of 0.05-0.10 g was used to cure cancer. Likely unsafeproduce vomiting, hypertension, loss of consciousness may lead to coma but may interact with anti-cholinergic drugs[24].

Antiinflamatory activity

Coriandrum sativum (C. sativum), D. stromonium and Azadirachta indica (A. indica) are traditionally used in treatment of inflammation. Ethanolic extracts of fruits of C. sativum, leaves of D. stromonium. Ethanolic extracts of fruits of C. sativum, leaves of D. stromonium and A. indica were subjected to preliminary screening for anti-inflammatory activity in albino rats. All ethanolic extracts exhibited significant anti-inflammatory activity comparable to the standard drug diclofenac sodium against carrageenan induced rat paw edema method. Among these plant A. indica showed maximum anti-inflammatory activity per hour[25].

Larvicidal and mosquito repellent activities

Ethanolic extracts of leaves of D. stromonium were evaluated for larvicidal and mosquito repellent activities against Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus. The LD50 values for larvicidal activity were found to be 86.25, 16.07 and 6.25 mg/L against Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus respectively. The ethanolic leaves extract of D. stromonium provided complete protection time (mosquito repellency) of 2.7, 71.7 and 117.7 min against Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus at higher concentration (1%)[26].

Pesticide toxicity

Extract of D. stromonium was effective in countering the toxicity of the cypermethrin pesticide toxicity[27].

Antifungal activity

Antifungal activity of a concoction brewed from D. stromonium, Calotropis gigantea, A. indica (neem) and cow manure (T1) followed by methanol-water (70/30 v/v) extracts of D. stromonium, Calotropis gigantea and A. indica T2 against Fusarium mangiferae. The study proved that the concoction-brewed compost T1 is effective, inexpensive, easy to prepare and constitutes a sustainable and eco-friendly approach to control floral malformation in mango when it is sprayed at bud break stage and again at fruit set stage[28].

Vibriocidal activity

A simple in vitro screening assay was employed for the standard strain of Vibrio cholerae, 12 isolates of Vibrio cholerae non-O1, and Vibrio parahaemolyticus. Aqueous and organic solvent extracts of different parts of the plants were investigated by using the disk diffusion method. Extracts from 16 medicinal plants were selected on account of the reported traditional uses for the treatment of cholera and gastrointestinal diseases, and they were assayed for vibriocidal activitie. The results indicated that Lawsonia inermis, Saraca indica, Syzygium cumini, Terminalia belerica, Allium sativum, and D. stromonium served as broad-spectrum vibriocidal agents[29].

Toxicity studies

Toxicity studies of ethanol extract of the leaves of D. stromonium in rats. Two doses of 50 and 200 mg/kg of the extract were administered to the rats for five weeks. Parameters studied were the indices of liver and kidney function and some biochemical and haematological parameters. Feed intake, final body weight, serum AST, ALT, billurubin, total protein, urea and the electrolyte studied were not affected by the extract administration. Serum creatinine levels were however significantly raised in the rats administered with ethanol extract at the dose of 200 mg/kg body weight. The biochemical and haematological parameters were also affected[30]. The effects of acute, subacute and chronic administration of alkaloids atropine and scopolamine, the main constituents of the active principle of D. stromonium, with toxic properties, were studied in male Albino Wistar rats. After acute i.p. administration of dose 100 mg/kg of total alkaloids to the seeds of D. stramonium, there were no remarkable changes in general appearance and no deaths occurred in any experimental group. Twenty four hour after total alkaloids of seeds, a significant reduction in indices of liver, spleen brain and kidney function and some biochemical and haematological parameters were observed. The red blood cells, hematocrit, hemoglobin and white blood cells were significantly higher in the treated groups than the control group. Subacute study for four weeks showed no resulting mortality or signs of toxicity. In chronic study, the synthetic alkaloids administered i.p. at daily doses of 4.2 mg/kg of atropine and 1.6 mg/kg of scopolamine, did not produce death. However diarrhoea and hypoactivity were observed. The relative weight of liver was significantly less than that of the control group[31].

Biopesticide with antifungal activity

Biopesticides (leaf extracts) obtained from eight plants (Vitex negundo, Polyathia longifolia, Vinca rosea, Withania somnifera, Lawsonia inermis, Adhotoda zylanica, D. stromonium and Hyptis suaveolens) showed antifungal activities against the fungal pathogen (Fusarium oxysporum) of wilt of pigeon pea (Cajanus cajan L.). Both in vivo and in vitro higher concentration of ethanotic leaf extracts of all eight plants showed complete inhibition in linear growth and sporulation in test fungi[32].

Protective agent in severe organophosphate toxicity

Treatment of patients following an organophosphate (OP) exposure can deplete a hospital’s entire supply of atropine. Given the possibility of multiple severe exposures after a terrorist attack using OP nerve agents, there exists a need for either greater atropine stores or the development of alternative antidotes. Jimsonweed (D. stromonium) contains atropine and other anticholinergic compounds and is common and readily available. It is used recreationally for its central anticholinergic effects and is easy to be made into an extract by boiling the crushed seeds. The extract has rapid onset of effects and may be useful for treatment of OP poisoning. Pretreatment with D. stromonium extracts significantly increases survival following severe dichlorvos exposure[33].

Safety aspect

Careful consideration of the toxicity of the plant is required before its use. Its ingestion induces characteristic symptoms. The mouth becomes dry, an intense thirst develops, the vision gets blurred with prominent mydriasis and the heart rate increases. This is followed by hallucinations, delirium, and loss of motor coordination which may lead to command ultimately to death by respiratory failure[34].

Quantitative standards

Dosage: 50-100 mg of dried leaf or the same amount in infusion.
Total ash: Not more than 20.0%.
Total alkaloid: Not less than 0.05% calculated as hyoscyamine.
Foreign matter: Not more than 3.0% of stem having a diameter exceeding 5 mm.
Acid insoluble ash: Not more than 4.0%.

Conclusion

Present review gives a broad information about the bioactive constituents, ethnopharmacology along with the scientifically claimed medicinal uses of D. stramonium. Several alkaloids, carbohydrates, fat, proteins and tannins have been reported to be present in different parts of D. stramonium. The plant shows various types of activities such as analgesic and antiasthamatic activity which may be due to the presence of the investigated active chemical constituents. The pharmacological studies so far have been performed in vitro and in vivo. Therefore, there is a need of investigation and quantification of phytoconstituents and pharmacological profile.

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