Celastrus

Celastrus (Celastrus paniculatus Willd.): A Comprehensive Reference

1. Identity and Botanical Classification

Botanical and Scientific Names

Celastrus paniculatus Wild. belongs to the family Celastraceae. The full binomial authority is Celastrus paniculatus Willd., named after the German botanist Carl Ludwig Willdenow. Its family classification is Celastraceae. In Ayurveda it is known as the "Tree of life" and "Elixir of life," and is commonly referred to as Malkangani in Hindi and Jyotishmati in Sanskrit. It is also commonly known as the Black-Oil Tree, Intellect Tree, and Climbing-Staff Plant. In Thai traditional medicine it is known as Kra-Thong-Lai.

Morphology and Geographic Distribution

Celastrus paniculatus is an evergreen climbing shrub of great significance in the traditional Indian systems of medicine, including Ayurveda, Unani, and Siddha. It is native to India and Southeast Asia and is also found in parts of Taiwan. In summer, the plant bears small greenish-yellow flowers grouped in panicles — hence the species epithet paniculatus — and the fruit capsules are bright orange when mature, splitting open to reveal seeds coated in a fleshy aril.

Parts Used and Common Preparations

Ayurvedic practitioners primarily harvest the seeds and extracts from the kernel, valuing them for nervine tonics; more rarely, the bark and leaves find use in traditional preparations. The seeds and their oil are extensively used to treat neurological disorders such as cognitive dysfunction, paralysis, epilepsy, insomnia, and other ailments like rheumatism, arthritis, sciatica, and leprosy. As a dietary supplement, users either eat the seeds or crush them into powders and make tea; capsules are also available. A safe and effective dose of celastrus is unknown due to a lack of clinical research; commercially available supplements usually contain 400–500 mg of Celastrus paniculatus powder per capsule.

Celastrus paniculatus is considered an endangered medicinal plant. The plant is widely used for its medicinal properties, mainly to extract the seed oil; the seeds are harvested indiscriminately from wild populations, making the species highly vulnerable and highly endangered.

2. Traditional and Historical Use

Ayurveda (India)

C. paniculatus, mentioned in Ayurveda as the "Tree of life," was in use from time immemorial to treat brain-related disorders and to enhance learning and memory; Ayurveda recognized it as Jyotishmati. According to Ayurveda, depending upon the dose regimen, C. paniculatus was used as a stimulant nerve tonic or sedative.

Jyotishmati is a combination of the words "enlightens" (Jyoti) and "brain functions" (mati), meaning "enlightens the psychomotor function." The seed oil (Jyotishmati taila) is well renowned for its intellect-promoting (medhya) properties and is used as a brain tonic to boost intelligence and improve memory.

Jyotishmati's legacy stretches back to ancient Sanskrit texts; the Charaka Samhita, dating around 300–200 BCE, mentions Celastrus paniculatus under treatments for forgetfulness and nervous disorders.

It is considered in Ayurveda to stimulate medha (intellect) and promote smruti (memory), and Ayurveda thus recognizes it as Jyotishmati. It is a well-known Ayurvedic Medhya Rasayana (nervine tonic), used extensively as a neuroprotective and memory enhancer and in different central nervous system disorders.

Celastrus paniculatus (Malkangni) is used in Ayurveda as a nervine tonic, tranquilizer, and diuretic, and in rheumatism, gout, leprosy, and asthma.

Traditional Chinese Medicine and Other Asian Traditions

In China, plants of the genus Celastrus, including C. paniculatus, have been used as natural insecticides and also as important folk medicine to treat fever, chill, joint pain, edema, rheumatoid arthritis, and bacterial infection.

Among Thai traditional medicines for treatment of intermittent fever, C. paniculatus — known as Kra-Thong-Lai — is reputed for its medicinal value; the root, stem, and leaves were prescribed for dysentery, diarrhea, and fever. Northeast folk medicine practitioners prescribed stems as a lactogogue, and the powdered root barks pressed into pills were commercially sold as a treatment for malaria.

Tribal and Ethnobotanical Uses

In the tribal district (Jashpur) of Chhattisgarh, India, tribal people use traditional methods to extract C. paniculatus oil, and it is commonly used by tribes for the treatment of various diseases including headache, muscular spasm, and local inflammations.

C. paniculatus seed oil has a long history and has been reported to improve memory processes in rats, to be beneficial to psychiatric patients, and to have increased the I.Q. of mentally retarded children.

3. Key Constituents and Active Compounds

More than 80 phytoconstituents have been reported from this plant, including wifornine F, malkanguniol, celapanigin, zeylasterone, pristimerin, and lupeol.

Various sesquiterpenoid polyalcohols and esters (malkanguniol, malkangunin, polyalcohol A–D, celapnin); alkaloids (paniculatine, celastrine); phenolic triterpenoids (celastrol, paniculatadiol); fatty acids (oleic, linoleic, linolenic, palmitic, stearic, and lignoceric acid); and agarofuran derivatives have been isolated from the seeds and seed oil of C. paniculatus.

C. paniculatus is a rich source of several secondary metabolites, including β-dihydroagarofuranoid sesquiterpenes; alkaloids (celastrine, celapanin, celapagin, and paniculatine); flavonoids; terpenoids (β-amyrin, lupeol, pristimerin); sterols (β-sitosterol, campesterol, stigmasterol, α-tocopherol, γ-tocopherol); fatty acids (palmitic, stearic, oleic, linoleic, linolenic acids); and non-fatty acids (benzoic acid, cinnamic acid).

Alkaloids, tannins, saponins, steroids, terpenoids, flavonoids, phlobatannins, and cardiac glycoside distribution have been assessed and compared across different parts of Celastrus paniculatus. All plant parts were found to contain alkaloids and tannins on a large scale.

The seed oil contains a number of fatty acids, including oleic, linoleic, linolenic, palmitic, stearic, benzoic, and acetic acids as volatile acids, and their glycerol esters, mainly α,α′-dipalmitoyl glycerol.

From the whole plant, three new β-dihydroagarofuranoid sesquiterpenes have been isolated, of which the major constituent is (1α,2α,8β,9β)-1,8-bis(acetyloxy)-2,9-bis(benzoyloxy)-14-hydroxy-β-dihydroagarofuran.

This plant possesses strong antioxidant activity — including total flavonoid content, total phenolic content, nitric oxide scavenging activity, and free radical scavenging activity — and exhibits multiple pharmacological activities including cognition-enhancing, neuroprotective, antipsychotic, anti-depressant, antibacterial, anti-arthritic, anti-malarial, analgesic, anti-inflammatory, anti-fertility, cardiovascular, locomotor, anxiolytic, wound healing, anti-spasmodic, hypolipidemic, anti-cancerous, and iron-chelating activity.

4. Mechanisms of Action

Cholinergic and Neurotransmitter Modulation

Estimation of acetylcholinesterase enzyme in rat brain supports memory enhancement by reducing acetylcholinesterase activity; the aqueous extract of Celastrus paniculatus seed has dose-dependent cholinergic activity, and the mechanism by which it enhances cognition may be due to increased acetylcholine levels in the rat brain.

An older rodent study demonstrated that seed oil extracted from C. paniculatus influenced learning and memory in a passive avoidance task in albino rats and affected the contents of norepinephrine (NE), dopamine (DA), and serotonin (5-HT) in the brain.

Antioxidant and Neuroprotective Mechanisms

Aqueous, methanolic, chloroform, and petroleum ether extracts of seeds were investigated for their effect on cognitive function in rats; only the aqueous seed extract (200 mg/kg body weight for 14 days) showed an improvement in learning and memory in both shuttle-box and step-through paradigms. Treatment stimulated a significant decrease in brain levels of malondialdehyde, with simultaneous significant increases in levels of glutathione and catalase, indicating an antioxidant effect.

Seed oil and organic extracts protected neuronal cells against H₂O₂-induced toxicity in part by virtue of their antioxidant properties and their ability to induce antioxidant enzymes; notably, the seed oil, which exhibited the least antioxidant properties among the preparations tested, was the most effective in preventing neuronal cells against H₂O₂- and glutamate-induced toxicities, suggesting additional mechanisms beyond free-radical scavenging.

A significant antioxidant activity of the plant has been suggested as the major mechanism for its memory-enhancing and neuroprotective activities.

Glutamate Receptor Modulation

The primary mechanisms of action of Celastrus paniculatus include its antioxidant activity, modulation of glutamate receptors, and potential inhibition of acetylcholinesterase.

Anti-inflammatory and NF-κB Pathway

Celastrus paniculatus oil has been utilized as a tranquilizer and memory enhancer; one study investigated its neuropharmacological activity and efficacy in ameliorating scopolamine-induced cognitive impairment in rats via NF-κB–mediated neuroinflammation and synaptic plasticity pathways.

Anxiolytic and Serotonergic Mechanisms

Celastrus oil, extracted from seeds of C. paniculatus and tested at two dose levels (1 and 1.5 g/kg), exhibited significant anxiolytic activity and did not produce tolerance; the non-sedative nature and reversal of buspirone-induced behaviour in open-field exploration point to a serotonergic mechanism underlying the anxiolysis.

Apoptosis and Cell Signaling in Cancer Models

Western blot analysis established that the major β-dihydroagarofuranoid sesquiterpene constituent has the ability to target a broad range of signaling effectors related to survival and cell-cycle progression, including Akt, NF-κB, p53, and MAP kinases; flow cytometry analysis indicates increased reactive oxygen species production in response to this compound, suggesting a pleiotropic mode of mechanism that underlies its antiproliferative activity in MCF-7 breast cancer cells.

5. Scientific Evidence by Area of Use

5.1 Cognition, Memory, and Learning

This is the most extensively studied domain for C. paniculatus. As a traditional Ayurvedic medicinal plant used for centuries as a memory-enhancing agent, the seed extract has been extensively investigated in several laboratories for its neuropharmacological effects, and a number of reports confirm nootropic action; researchers have also evaluated the anti-inflammatory, anticonvulsant, and other pharmacological effects of CP preparations.

Animal evidence: The aqueous seed extract was administered orally to rats at 350 and 1,050 mg/kg and to mice at 500 and 1,500 mg/kg, with results compared to piracetam (100 mg/kg) as a standard drug; in elevated plus maze and sodium nitrite–induced amnesia models, C. paniculatus extract showed statistically significant improvement in memory compared to controls.

C. paniculatus oil has been reported to have neuroprotective and antioxidant activities; in a rodent model designed to assess its neuroprotective effects on stress-associated cognitive dysfunctions, stressed rats receiving CP oil at 400 or 600 mg/kg intraperitoneally for 14 days were compared to normal and vehicle-treated control rats. Chronic stress increased anxiety-like behavior in the elevated plus maze, and chronic C. paniculatus treatment to stressed rats decreased anxiety behavior in these animals.

Parkinson's disease model (in vitro): Parkinson's disease is induced by the death of dopaminergic neurons; as no studies had previously analyzed the neuroprotective effect of CP seeds on PD, one study aimed to investigate this using an in vitro MPP+-induced PD model, examining the effect of CP seed extract on the expression levels of apoptotic marker proteins including Bcl-2 and its upstream pathway protein glycogen synthase kinase-3β (GSK-3β) in human neuroblastoma SH-SY5Y cells.

Epilepsy model: Cognitive deficit is one of the common comorbidities accompanying epilepsy; one study evaluated the effect of C. paniculatus seed extract on seizure severity and cognitive deficit following a PTZ-induced chemical kindling model, developed by daily administration of a sub-convulsive dose of PTZ (30 mg/kg) for four weeks. C. paniculatus (500 mg/kg) alone and in combination significantly reduced seizure scores; biochemical analysis showed elevated antioxidant markers (GSH, CAT, and SOD) and elevated dopamine levels; and C. paniculatus also significantly protected against neuronal loss in the hippocampus and frontal cortex. The authors concluded it may have potential to treat epilepsy and associated cognitive deficits.

Huntington's disease model: One study evaluated CP against 3-nitropropionic acid (3-NP)–induced Huntington's disease-like symptoms in Wistar male rats; the ethanol extract of CP seeds (CPEE), standardized on the basis of linoleic acid content (6.42%), was administered at 100 and 200 mg/kg orally for 20 days, with its various fractions at smaller doses, and effects assessed on locomotor activity, grip strength, gait pattern, cognitive dysfunction, and biochemical oxidative damage parameters.

Human/clinical evidence: Currently, no human studies have examined the safety or effectiveness of celastrus. Although specific effect sizes in humans are inadequately documented, animal studies demonstrate significant positive outcomes for those with cognitive impairments or neurological disorders; the clinical significance of the observed benefits in humans still requires extensive research. One registered trial exists as a protocol: a randomized, active-controlled, double-blind equivalence trial enrolling a total of 70 patients between 20–50 years of age with mild-to-moderate anxiety (HAM-A score less than 24) was registered; patients in one group received sertraline capsules 50 mg at bedtime and in the comparison group received Jyotishmati capsules 500 mg twice daily after food with water for 60 days. This trial had not yet published results at the time of this writing.

Overall evidence strength for cognition: Preliminary to moderate. Evidence is almost entirely from animal models and in vitro systems. No completed, published human randomized controlled trials on cognitive outcomes have been identified.

5.2 Anxiety and Mood

Celastrus seeds have been reported to possess anxiolytic and antistress activities in the scientific literature. The non-sedative nature and reversal of the anxiolytic property of the 5-HT1A partial agonist buspirone in the open field test point to a serotonergic mechanism underlying the anxiolysis. Studies showing antidepressant-like and anxiolytic activity in animal models provide scientific backing for the traditional adaptogenic applications of this herb.

Evidence strength for anxiety/mood: Preliminary. Confined to animal and in vitro studies. One clinical trial protocol (vs. sertraline) has been registered but results are not yet available in the published literature.

5.3 Neuroprotection and Neurodegeneration

Celastrus paniculatus seed extract exhibits neuroprotective effects against MPP+-induced apoptotic cell death via GSK-3β in a Parkinson's disease model.

The anti-Alzheimer activity of the crude methanolic extract of C. paniculatus has been demonstrated through strong DPPH free radical scavenging as well as inhibition of authentic peroxynitrite activity and total reactive oxygen species generation; additionally, CP has a protective action against 3-NP–induced Huntington's disease–like symptoms due to its strong antioxidant effect.

Evidence strength for neuroprotection: Preliminary. All studies are animal or cell-culture based. No human trials on neurodegeneration have been published.

5.4 Anti-inflammatory and Analgesic Activity

Pharmacological studies suggest that the oil obtained from the seeds of CP possesses sedative and anticonvulsant properties; analgesic and anti-inflammatory effects of a CP seed methanolic extract were reported in mice and rats by Ahmad et al. (1994).

The crude extracts and isolated constituents have exhibited a wide range of in vitro and in vivo pharmacological effects including anti-rheumatoid arthritis, anti-inflammatory, and antioxidative activities.

Evidence strength for anti-inflammation/analgesia: Preliminary. Studies are preclinical (animal and in vitro only).

5.5 Hypolipidemic and Cardiovascular Effects

One study evaluated the hypolipidemic effect of methanolic extract of C. paniculatus in experimentally induced hypercholesterolemic rats; hypercholesterolemia was induced by high-fat diet; oral administration of 50% methanolic seed extract at an optimized dose of 65 mg/kg substantially reduced plasma total cholesterol, triglycerides, and LDL cholesterol, with the atherogenic index and liver weight also showing significant decreases and HDL cholesterol substantially increasing.

Furthermore, the activities of HMG-CoA reductase, glucose 6-phosphate dehydrogenase, and malate dehydrogenase were significantly reduced; histological studies showed less cholesterol deposits in the aorta of animals fed with seed extract compared to the induced hypercholesterolemic animals not given the supplement.

Evidence strength for lipid lowering/cardiovascular: Preliminary. Evidence is animal-based only.

5.6 Anticancer Activity

Celastrus paniculatus is a traditional medicinal plant with diverse pharmacological activities; from the whole plant, three new β-dihydroagarofuranoid sesquiterpenes were isolated, and the major constituent suppressed the viability of MCF-7 breast cancer cells with an IC₅₀ of 17±1 μM.

Evidence strength for anticancer: Very preliminary. Findings are from cell culture (in vitro) only and have not been replicated in animal studies or human trials.

5.7 Gastrointestinal Activity

Borelli et al. (2009) documented a potent relaxant effect of Celastrus paniculatus extract in rat and human ileum. The pharmacological actions documented in the literature include gastroprotective and anti-ulcerative properties at the cellular and molecular level.

Evidence strength for gastrointestinal: Very preliminary. Includes one ex vivo human tissue study and preclinical reports.

6. Body Systems and Health Areas of Association

• Central Nervous System: Memory enhancement, cognition, anti-stress, neuroprotection, anticonvulsant, sedative and tranquilizing properties. The Jyotishmati oil extracted from the seeds is known to have an effect on the central nervous system; it is used to treat acute and chronic immobilization stress, and the oil possesses sedative and anticonvulsant properties.
• Musculoskeletal System: Anti-arthritic and anti-rheumatic use documented in both Ayurvedic and Chinese traditions.
• Cardiovascular System: Hypolipidemic and antiatherosclerotic activities demonstrated in animal models.
• Gastrointestinal System: Antispasmodic, gastroprotective, and laxative properties noted in traditional use and some preclinical work.
• Reproductive System: Antispermatogenic effects observed in animal studies; traditional aphrodisiac claim.
• Immune/Inflammatory System: Anti-inflammatory, analgesic, antimalarial, and antibacterial properties identified in preclinical studies.

7. Dosage Forms and Reported Dosages

The following dosages are reported only as they appear in cited scientific or traditional sources and do not represent clinical recommendations.

Dosages Used in Animal/Preclinical Research

• The aqueous seed extract was administered orally in two different doses to rats (350 and 1,050 mg/kg) and to mice (500 and 1,500 mg/kg), and results were compared to piracetam (100 mg/kg) as a standard drug.
• The aqueous seed extract at 200 mg/kg body weight for 14 days showed improvement in learning and memory; further experiments were conducted using 100, 200, and 300 mg/kg doses.
• Rats were subjected to restraint stress for 21 days (6 h/day) and then treated with C. paniculatus at 400 or 600 mg/kg intraperitoneally for 14 days.
• CPEE at 100 and 200 mg/kg and its various fractions (petroleum ether at 40 mg/kg, ethyl acetate at 2.5 mg/kg, n-butanol at 7 mg/kg, and aqueous at 18 mg/kg) were administered orally for 20 days in the Huntington's disease model.
• In the hypolipidemic study, oral administration of methanolic seed extract (50%) at an optimized dose of 65 mg/kg body weight was used.
• In the anxiolytic study, Celastrus oil was tested at two dose levels: 1 and 1.5 g/kg.

Dosages Used or Proposed in Human Contexts

• In the registered clinical trial protocol for anxiety, Jyotishmati capsules at 500 mg were administered twice daily after food with water for 60 days.
• A safe and effective dose is unknown due to a lack of clinical research; commercially available supplements usually contain 400–500 mg of Celastrus paniculatus powder per capsule, with manufacturers recommending 1 to 2 capsules per day.
• The minimum effective dose of Celastrus paniculatus has not been determined in human studies; traditional medicine practices use this herb without standardized dosing protocols, and optimal dosage ranges remain unclear.

8. Safety Considerations and Interactions

Preclinical Toxicity Data

One preclinical study evaluated the toxicity profile of C. paniculatus in Swiss albino mice, divided into groups receiving CP seed oil orally at doses of 300, 2,000, and 5,000 mg/kg body weight for both acute and subacute toxicity studies in accordance with OECD guidelines No. 423; special attention was given during the first 4 hours and daily thereafter for a total of 14 days. Celastrus paniculatus seed oil was found safe up to 2,000 mg/kg in acute toxicity studies; behavioral and physical parameters showed no significant toxicity signs in treated mice.

One research report indicated that C. paniculatus seed extract can produce undesirable effects on the liver, but that these changes can be reversed completely 45 days after cessation of treatment; separately, CP oil was found to be safe and did not affect behavior or impair motor coordination up to a dose of 5 g/kg in rats.

Antispermatogenic (Reproductive) Toxicity

Biochemical, histochemical, and histological studies of the effects of an oily extractive from seeds of C. paniculatus on the testes and liver of adult rats demonstrated that the testes of treated animals showed vacuolization, germ cell depletion, and arrest of spermatogenesis; the livers revealed focal necrosis in animals receiving 0.2 ml intraperitoneally every other day for 30 days, but 45 days post-treatment these lesions were absent, with intermediate repair and regenerative changes apparent at 30 days post-treatment. The results indicate that C. paniculatus oil may have antifertility effects and that the degenerative changes seen in the liver are reversible with time.

One rat study suggested that Celastrus paniculatus seed extract may impair sperm development, but more research is needed to confirm this effect and determine its relevance to human use.

General Safety and Human Data Gaps

The purported health benefits of C. paniculatus are only supported by limited animal and cell studies; currently, no human studies have examined the safety or effectiveness of celastrus.

The level of research on Celastrus paniculatus is moderate; most studies have been conducted on animals or in vitro, and further human trials are required to establish its efficacy and safety for broader use.

Potential Drug Interactions

Celastrus paniculatus may interact with cholinergic medications and supplements, as it can affect acetylcholine levels in the brain. Given its documented serotonergic anxiolytic mechanism, caution in combination with serotonergic drugs can also be inferred from preclinical data, though no human interaction studies have been published.

Conservation and Quality Concerns

Celastrus paniculatus is considered an endangered medicinal plant. Its endangered status raises concerns about authentication and adulteration in commercial supplement supply chains, a factor not systematically studied in the clinical context.

References

• An extensive review on phytochemistry and pharmacological activities of Indian medicinal plant Celastrus paniculatus Willd — PubMed (Wiley, Phytotherapy Research, 2022)
• Celastrus paniculatus: Traditional uses and Ethnobotanical study — ResearchGate (2015)
• Traditional uses, secondary metabolites, and pharmacology of Celastrus species — ScienceDirect (2019)
• Nootropic activity of Celastrus paniculatus seed — PubMed (Pharmaceutical Biology, 2010)
• Antioxidant property of Celastrus paniculatus Willd.: a possible mechanism in enhancing cognition — PubMed (Journal of Ethnopharmacology, 2002)
• Neuroprotective effect of Celastrus paniculatus on chronic stress-induced cognitive impairment — PMC (Indian Journal of Pharmacology, 2016)
• Celastrus paniculatus oil ameliorates NF-KB mediated neuroinflammation and synaptic plasticity in the scopolamine-induced cognitive impairment rat model — PubMed (Metabolic Brain Disease, 2023)
• Protective effect of Celastrus paniculatus on cognitive function in glutamate-induced brain-injured mice — PubMed (2022)
• Neuroprotective Effect of Celastrus Paniculatus Seed Extract on Epilepsy and Epilepsy-associated Cognitive Deficits — PubMed (2023)
• Celastrus paniculatus seed water soluble extracts protect against glutamate toxicity in neuronal cultures from rat forebrain — PubMed (Journal of Ethnopharmacology, 2004)
• Celastrus paniculatus seed oil and organic extracts attenuate hydrogen peroxide- and glutamate-induced injury in embryonic rat forebrain neuronal cells — ScienceDirect (Phytomedicine, 2006)
• Ameliorating effect of Celastrus paniculatus standardized extract and its fractions on 3-nitropropionic acid induced neuronal damage in rats — PMC (2018)
• Celastrus paniculatus seed extract exhibits neuroprotective effects against MPP+-induced apoptotic cell death via GSK-3β in a Parkinson's disease model — PMC (2024)
• Cytotoxic constituents from Celastrus paniculatus induce apoptosis and autophagy in breast cancer cells — PubMed (Phytochemistry, 2013)
• Hypolipidemic Effect of Celastrus paniculatus in Experimentally Induced Hypercholesterolemic Wistar Rats — PMC (Indian Journal of Clinical Biochemistry, 2010)
• Antispermatogenic action of Celastrus paniculatus seed extract in the rat with reversible changes in the liver — PubMed (Journal of Ethnopharmacology, 1990)
• Evaluation of comparative efficacy of Celastrus paniculatus (Jyotishmati) capsule versus sertraline capsule in the management of generalized anxiety disorder: protocol for a randomized controlled trial — PMC (2024)
• Toxicity Profile of Celastrus Paniculatus Seeds: A Preclinical Study — ResearchGate (Asian Journal of Pharmaceutical and Clinical Research, 2020)
• Phytochemical Composition, Pharmacological Properties, and Therapeutic Applications of Celastrus paniculatus — Bentham Science (Current Traditional Medicine, 2021)
• Ethno botanical study and traditional uses of Celastrus paniculatus — IJISET (2015)
• Anti-anxiety activity of Celastrus paniculatus seeds — ResearchGate (2003)
• Effects of Celastrus paniculatus on passive avoidance performance and biogenic amine turnover in albino rats — PubMed (1995)