Celastrus Paneculatus 

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Oxidative stress in brains of male rats intoxicated with aluminium and neuromodulating effect of Celastrus Paniculatus Alcoholic Seed Extract. 
A genetically stable rooting protocol for propagating a threatened medicinal plant—Celastrus paniculatus

CELASTRUS PANICULATUS, AN ENDANGERED INDIAN MEDICINAL PLANT WITH MIRACULOUS COGNITIVE AND OTHER THERAPEUTIC PROPERTIES:

AN OVERVIEW

 

NEHA ARORA AND SHASHI PANDEY-RAI*

Laboratory of Morphogenesis, Centre of Advance Study in Botany, Faculty of Science, Banaras Hindu University, Varanasi-221005

 

ABSTRACT

    Celastrus paniculatus is an Indian medicinal plant which has been used for thousands of years in the traditional Ayurvedic system of medicine. It is fast gaining importance in the primary healthcare systems as well as in herbal drug formulations. Oil obtained from the seeds of the plant is reported to be highly beneficial in stimulating intellect and sharpening the memory. It also acts as a potential nervine tonic, rejuvenator and an anti-depressant. Moreover, the plant possesses a strong antioxidant as well as free radical scavenging activity. C. paniculatus has also been exploited for its potential role in the management of neurodegenerative diseases and other neuronal disorders such as Alzheimer’s disease. Oil being a powerful stimulant for neuromuscular system is also used for the treatment of rheumatism, gout and paralysis. This review aims at exploring the detailed phytochemical composition, pharmacological properties as well as therapeutic applications of different parts of C. paniculatus. KEYWORDS: Celastrus paniculatus, nervine tonic, antioxidant, phytochemicals, therapeutic properties.

INTRODUCTION

    Celastrus paniculatus is an unarmed woody climbing shrub commonly known as Malkangni, Kangani, Jyotishmati, Sphutabandhani, Svarnalota, Black-Oil tree, Intellect tree, Climbing-staff plant. It grows throughout India up to a height of almost 1,800-2,000 meters. This deciduous vine can grow to a very large size. It belongs to the class Angiospermae and family Celastraceae (Figure 1). The base stem of this shrub grows up to 10 centimeters in diameter and 6 meters in length. Being a rambler by nature, it produces many woody branches that cling to surrounding flora for support (Figure 2). The stem has a rough, pale or reddish brown exfoliating bark covered densely with small elongated white lenticels. The inner bark is light and cork like with yellow sapwood. The leaves are simple, broad, and oval, obovate or elliptic in shape, leathery and smooth, alternately arranged on short petioles with toothed margins1 . They grow on singular stems ranging from light to dark green color. The flowers are tiny with 3.8 mm diameter, whitish green to yellow green in color and grow on the top of the main stalk in terminal drooping panicles of 5-20 cm length. Capsules of the plant are depressed, globose, tri-lobed, bright yellow colored with 1-1.3 cm diameter, containing 3-6 seeds per capsule/ seed pod which are enclosed by an orange-red aril. The seeds are small and oval shaped growing in round pods that gradually change from a light yellow to a deep red color as they mature (Figure 3). They are known to cause yelloworange stains on anything their oils come into contact with. Parts of the plant which are generally used for their economic importance include seeds, bark and leaves. 

    Endangerd species C. paniculatus is a rare and endangered medicinal plant distributed throughout India mostly in tropical forests and subtropical Himalayas. Recent studies show that the wild populations of the plant in India are at high risk2 . The species is vulnerable in Western Ghats of south India5 . It is reported to be critically endangered (CR) in Uttar Pradesh and Uttrakhand6 . Seed and Oil Studies of C. paniculatus C. paniculatus seeds and oil extracted from them have long been regarded to be highly beneficial and medicinally effective. The seeds yield as much as 52% oil by weight, and it is in this oil that numerous alkaloids are found, compounds such as celastrine and paniculatin. The seeds are highly rich in fatty acids. Percentage composition of four lipid fractions of the seeds viz. normal triglycerides, polar triglycerides, polar nonglyceridic ester, and nonpolar nonglyceridic ester is given in Figure 4. Major component acids in these fractions are palmitic, stearic, oleic, linoleic, and linolenic. The major molecular species constituting the normal triglycerides are: palmito-oleo-palmitin (6.8%), palmito-oleo-stearin (5.6%), palmitodiolein (14.7%), palmito-oleo-linolein (7.0%), stearo-diolein (6.1%), triolein (8.0%) and dio-leo-linolein (7.6%)7 . They are generally known to stimulate intellect and sharpen the memory. Seeds are used as expectorant as well as brain and liver tonic. They also cure joint-pains, paralysis and weakness. Oil of C. paniculatus is cold-pressed raw herbal oil expressed from the seeds of the plant which follows different procedures of extraction. Oil is stomachic, tonic, good for cough and asthma; used in leprosy, cures headache and leucoderma. Studies reveal that the oil has an efficient therapeutic effect on the central nervous system.

    Uses of seeds and oil of C. paniculatus Uses Seed Oil Used as/ for Appetizer, emetic, expectorant, sodorific, aphrodisiac, powerful brain and liver tonic8 , stimulate intellect and sharpen memory, thermogenic, emollient, nervine, stimulant, anti-inflammatory, diuretic, emmenagogue, diaphoretic, febrifuge, digestive, laxative, useful in abdominal disorders Intellect promoting, shows beneficial effect on the learning and memory process in mentally retarded children9 ; thermogenic and rubefacient, stomachic, tonic, useful in abdominal disorders, enriches blood; powerful stimulant for neuromuscular system Used against Seeds used externally on foul, indolent ulcers and scabies; useful both as an external and internal remedy in rheumatism, gout, paralysis, leprosy10 and weakness. Used against pruritis, skin diseases, leucoderma, cephalalgia, arthralgia, asthma, cardiac debility, inflammation, stranguary, neuropathy, amenorrhoea, dysmenorrhoea, epilepsy Used to treat beri-beri (vitamin B1 deficiency disease1,11; powerful against malaria; useful in treating ADD, anxiety, "brain fog", etc.; works against cough and asthma; cures headaches and leucoderma.

    Phytochemistry of C. paniculatus Different parts of the plant when extracted in different solvents give various fractions of active components, which are discussed in Figure 513 . The seeds of C. paniculatus contain brownish yellow oil, with a higher proportion of acetic and benzoic acids in addition to other fatty acids, as well as a crystalline substance tetracasanol and sterol14,15. A new sesquiterpene ester Malkangunin and three sesquiterpene alkaloids namely celapanin, celapanigin, celapagin have been isolated from the plant16. The sesquiterpene alkaloids are derived from a new sesquiterpene tetra-ol (celapanol) which is alternately esterified with acetic, benzoic, nicotinic and β-furoic acids 17 . The various mineral elements in the plant have been reported as sodium, magnesium, aluminium, potassium, calcium, vanadium, chromium, manganese, iron, cobalt, nickel, copper, zinc, molybdenum, silver while strontium and cerium were found to be absent 18 . Besides these, oil of the plant also comprises of proteins, carbohydrates, fats (saturated fats, polyunsaturated fats, monounsaturated fats) and Vitamin C. The 50% ethanolic extract of plant (excluding root) shows 3.52% presence of tannins 19 . Table 5 gives the detailed description of the compounds and their active components present in the plant.

    Traditional use For thousands of years, Ayurvedic medicine has used the Celastrus seeds for their potent medicinal properties. They were used for many different ailments and were administered as powerful brain tonic, appetite stimulant as well as emetic. They helped in overcoming physical weakness and mental confusion; played an important role in alleviating asthma symptoms, reducing headaches and joint pains due to arthritis. Men used them as potent balm that worked as sexual stimulant like modern phosphodiesterase inhibitors. In India, ayurvedic doctors of Bastar region in Chhattisgarh, used to prescribe Celastrus seeds to the patients suffering from forgetfulness in the dosage of one seed daily in their diet and then gradually increasing it up to 100 seeds per day. Traditional healers have used Celastrus oil for centuries to increase mental acuity, improve memory and intellect as well as retention and recalling power; and to alleviate mental fatigue, stress and minor joint pains. People using the oil were able to learn new information more quickly and were able to accurately and efficiently recall that information over longer periods of time. They used to call it ‘magzsudhi’ or brain clearer. Small quantities of the oil have long been consumed in healthy diet as a supplement to improve dream recall and to help induce lucid dreams. Use of the oil in a pomatum made by mixing one part of the oil in 8 parts of butter for application to the head has also been a common practice30 . Therapeutic uses of C. paniculatus C. paniculatus L. has a remarkable therapeutic value. Popularly being described as Jyotishmati, this plant has an important role in enhancing cognitive function and the natural luminosity (jyoti) of the mind (mati). It is a warming herb used internally in the treatment of inflammation of muscles and joints, including rheumatism, gout and paralysis31. The seeds are used to heal indolent ulcers and sores, as well as infectious skin conditions such as scabies in the form of a poultice3 . Medicated oil extracted from the seeds of the plant is used for topical application as a rubifacient and stimulant. Consumption of half a teaspoon of the oil daily or its application on the head acts as a brain stimulant to improve memory31. Similarly, a smaller dose of 4-10 drops of the expressed oil can be used in relieving mental exhaustion. Recent medical research on small mammals has proven the efficacy of the oil obtained from the seeds in lowering blood pressure, increasing alertness, and improving problem solving skills, possibly due to its powerful antioxidant action in the blood. Celastrus oil (in doses of 10-15 drops) supplemented with benzoin, cloves, nutmeg and mace helps in combating beri-beri, a disease of the peripheral nervous system associated with vitamin B-1 (thiamine) deficiency3 . The oil being a powerful stimulant is also used as an ointment for relieving rheumatic pains inflicted by malaria. Figure 6 illustrates the various therapeutic applications of the plant.

    Active components and therapeutic uses of different parts of C. paniculatus Plant part Bio-active component Therapeutic Uses Leaves Saponin Responsible for ant-microbial and anti-fungal activity; used for decoctions and teas; ease cough and fight infections, acts as emmenagogue Root bark β-sitosterol, Celastrol, Pristimerin, Zeylasterone, Zeylasteral; Terpenes Used to treat malaria Seed/ Seed oil Acetic and benzoic acids in addition to other fatty acids; crystalline substance tetracasanol and sterol14,15; Alkaloids Celastrine and Paniculatin Used to treat infections; have sedative and antidepressant actions; possess emetic, diaphoretic, febrifugal and nervine properties; sharpens memory; cure sores, ulcers; mosquitoes repellent; alkaloid fractions have tranquilizing properties.; oil enriches blood.

    Therapeutic uses of the plant Learning and memory Studies conducted on cognitive functions of rats using the aqueous extract of seeds of C. paniculatus indicate that the aqueous extract improved learning and memorizing capacity. It selectively reverses the impairment in spatial memory produced by acute central muscarinic receptor blockade, but is not related to an anticholinesterase-like action32. The oil extracted from the seeds was studied for its effect on learning and a significant improvement was observed in the retention ability of the Celastrus-treated rats compared with the saline administered controls. Sedation and convulsion Studies indicate a sedative property of the oil in cats, monkeys, mice and rats, and an anticonvulsant effect in rats33 . Antioxidant Methanolic extract of C. paniculatus demonstrates a dose-dependent free radical scavenging capacity and a protective effect on DNA cleavage, confirmed by a significant protective effect on H2O2- induced cytotoxicity and DNA damage in human non-immortalized fibroblasts34 . Analgesic and Anti-inflammatory A methanolic extract of the flowers of C. paniculatus exhibits analgesic and antiinflammatory activities in the hot water tail immersion test in mice and carrageenan induced pedal edema in rats35 . Hypolipidaemic 50% ethanolic seed extract was demonstrated to reduce serum cholesterol and LDLcholesterol levels by 60.10% and 71.70%, respectively. Increased faecal excretion of cholesterol suggests modulation of adsorption is affected36 . Anti-arthritic activity The body weight loss and swelling of the paw in rats during the secondary lesions found during the arthritic condition was corrected on treatment with petroleum ether and alcoholic extracts of the seeds, the study being a supporting evidence for the anti-arthritic activity37.  Anti-fertility The seed oil in a dose of 0.2 ml/animal/48 h to adult albino rats for 30 days showed antispermatogenic effects caused due to vacuolization of seminiferous tubules, germ cell depletion and exfoliation resulting into an arrest in spermatogenesis38 . Wound healing activity Lupeol, a triterpene compound isolated from petroleum ether extract of leaves exhibited a remarkable wound healing activity with a high rate of wound contraction39 . Anti-malarial activity Chloroform extract of the root bark containing a quinonoid triterpene, pristimerin was witnessed to have the highest antimalarial activity40 . Anti-bacterial activity The seed oil as well as the aqueous extract has an effective antibacterial activity against numerous microbes viz. Micrococcus pyogenes, Bacillus subtilis, B. cereus, Corynebacterium diphtheriae, Salmonella typhosa, S. paratyphi, S. dysentrica, S. marcescens Escherichia coli, Proteus vulgaris, P. morganii Pseudomonas pyocyana, P. aeruginosa Staphylococcus aureus, S. lutea and Klebsiella pneumonia41,42 . Anti-fungal activity The plant extracts had a strong inhibitory activity against several fungi like Trichophyton mentagrophytes, T. rubrum, T. soudanense, Candida albicans, Torulopsis glabrata, and Candida krusei, Aspergillus niger, A. flavus, Penicillium sp. and Trichoderma sp43 . Pharmacological studies Celastrus seed oil is used in several diseases like sciatica, lumbago, paralysis, arthritis and facial palsy for massage, which has proved to be very beneficial. Due to its remarkable brain stimulating and antioxidant effects, its effect was tested against immobilization-induced stress in albino mice. The crude C. paniculatus seed oil administered orally, intramuscularly (i.m.) and intraperitoneal (i.p.) in a dose of 1 g/kg produced sedation in rats and showed a significant reduction of movement in mice. The seed oil given as emulsion showed tranquilizing effect on adrenaline and amphetamine-induced excitement in mice33. Aqueous seed extract at a dose of 200 mg/kg body weight of rat, administered for 14 days has been observed to have an improvement on learning and memory. It has also exhibited antioxidant properties by decreasing lipid peroxidation and augmenting endogenous antioxidant enzymes in brain. Aqueous extract of the plant at 100, 200 and 300mg/kg doses once a day for 21 days, was investigated for its cognitive enhancing and antioxidant property in model of alzheimer’s disease in rats. It was found to be effective in preventing the cognitive deficits as well as the oxidative stress caused by ICV streptozotocin in rats44 . The seed extract has been extensively investigated in several laboratories for their neuropharmacological effects and a number of preclinical reports are available confirming their nootropic action45 but the exact mechanism of its action is still uncertain. It has been suggested that the plant exhibits neuroprotective and cognitive enhancing effects due to its antioxidative property and its capacity to modulate the cholinergic system13 .

    Dosage All the products of the plant used clinically are considered safe with low toxicity. Freshly powdered seed at the dose of 1-3 g and freshly crushed seed (tincture) at the dose 1-3 ml, twice or thrice daily is an effective dose. 10-12 seeds of Celastrus up to 100 a day, can be chewed at a time without any harmful effect. Oral administration of Celastrus oil up to the highest dose of 5 g/kg body weight does not produce mortality or any toxic effect on the normal behavior of the rats. It even did not impair motor coordination at any dose level12 . 2-10 drops of oil consumed twice a day is considered to be the standard dosage46, whereas, 10-15 drops twice daily acts as a powerful stimulant unattended by subsequent exhaustion1 . Recent studies Celastrus has long been used in Ayurvedic medicine for its potent medicinal properties, modern medicinal studies have only confirmed the miraculous potential of Celastrus seeds in supporting mental function. According to the recent study conducted on albino rats, oil extracted from the seeds of C. paniculatus was observed to have remarkable effects on the contents of norepinephrine (NE), dopamine (DA) and serotonin (5-HT) in the brain12 . Significant improvement was observed in the retention ability of the drug treated rats. These data indicate that Celastrus oil causes an overall decrease in the turnover of all the three central monoamines and implicate the involvement of these aminergic systems in the learning and memory process34 . Ongoing research There are researches being conducted to find out the possibility that anticancer drugs like pristimerin, which is derived from the seeds of the Celastrus plant, may be an effective means of treating or inhibiting the growth of specific types of cancer cells. H. Yang et.al.47, who conducted the research on pristimerin has found it to be quite active against nine cancer cell lines. Many more such researches are still going on and the potential health benefits of C. paniculatus looks very promising.

 

 

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