Gen info
- Celastrus, commonly referred to as staff vine, staff tree, or bittersweet, is a genus in the family Celastraceae, which comprises about 30-40 species of shrubs and vines with a wide distribution in East Asia, Australasias, Africa, and the Americas.
- Etymology: The genus name Celastrus derives from Greek word kelastros, the name of another tree. The species epithet paniculatus,means 'panicles' referring to the "flower clusters".
- Used for thousand of years in the traditional Indian System of Medicine: Ayurveda, Unani, and Siddha.
 Botany
Bilogo is a smooth woody vine, reaching a length of 4 to 10 meters. Branches are pendulous. Leaves are ovate to elliptic-ovate, 5 to 12 centimeters long, toothed at the margins. Flowers are numerous, greenish or greenish white, borne on lax, pendulous panicles, 7 to 18 centimeters long and about 5 millimeters in diameter. Fruit is ovoid or subglobose, 7 to 9 millimeters long, yellow, three-celled and usually three-seeded. Seeds are red and surrounded by a fleshy aril.
Distribution
- Native to the Philippines.
-
In thickets and second-growth forests at low altitudes in Cagayan, Isabela, Ilocos Norte, Nueva Viscaya, Pangasinan, Bulacan, Bataan, Rizal, and Cavite Provinces in
Luzon; and in Mindoro, Palawan, and Mindanao.
- Also native to Andaman Is., Assam, Bangladesh, Cambodia, China, Christmas Is., Himalaya, Hainan, India, Jawa, Laos, Lesser Sunda Is., Malaya, Myanmar, Nepal, Sri Lanka, Sulawesi, Sumatera, Taiwan, Thailand, Vietnam. (18)
Constituents
-
Seeds yield an oil, a bitter resinous principle, tannin and ash.
- Oil from seeds yield alkaloids celastrine and paniculatin in varying amounts.
- Destructive distillation of seeds yield oleum nigrum – an empyreumatic black oil.
- Fatty oil contains colasterol and a coloring matter, chromagen.
- A study of the leaves suggested a small amount of scarcely poisonous alkaloid and a glucoside.
- Analysis of the percentages of individual acids in seed fat showed: formic, 1.5; acetic, traces; benzoic, 3.4; palmitic, 31.2, stearic, 3.5; oleic, 22.5; linoleic, 15.7; linolenic, 22.2.(5)
- Phytochemical screening of different plant parts yielded alkaloids tannins and fixed oils in water PE, ethanol and chloroform extracts; carbohydrates and saponins in water extract, sterols and triterpenoids in water and ethanol extracts.
 - GC-MS study of essential oil of seeds showed an oil yield of 0.09% (v/w) with a total of 56 constituents identified, comprising 99.2% of total oil. Major components were palmitic acid (38.61%), phytol (11.72%), erucic acid (6.99%), trans-beta-copaene (4.78%) , and linalool (3.97%). (see study below) (19)
- In a study for phenolic acid (µg/g dry wt), crude extract yielded benzoic acid 3629.70, gallic acid 393.40, and tannic acid 3652.20. (see study below) (26)
- Phytochemical screening of various solvent extracts of leaves showed steroids and terpenoids in both petroleum ether and ethyl acetate extracts while the methanol extract yielded steroid, terpenoid, carbohydrate, alkaloid, saponin, and phenolic compounds. (30)
- Phytochemical screening of water, petroleum ether, ethanol and chloroform extracts of leaves yielded alkaloids, tannins, fixed oils
in W, PE, E, and C extracts, steroid and terpenoids in W and E, flavonoids, carbohydrates, saponins, and phenolic compounds in water extract. (39)
- Study of seed oil by solvent extraction and GC-MS yielded crude fatty oil at 45.5% in the mature seeds on dry weight basis, and identified 14 compounds, constituting 97.57% of the oil. The oil was rich in unsaturated fatty acids (70.11%) with saturated fatty acids (25.2%). Main fatty acids were oleic acid (54.42%), palmitic acid (20.0%), linoleic acid (15.51%), and stearic acid (4.18%), with four minor fatty acids. Study yielded four novel compounds not previously reported: 1,4-benzenediol (0.46%), cinnamic acid (0.15%), 2,6-di-tert-butyl-p-benzoquinone (0.03%), butylated hydroxytoluene (0.4%), and eudalene (0.16%).
(48)
Properties
- Oil considered a nerve-stimulant and brain tonic, alterative, stimulant.
- Seeds considered aphrodisiac, appetizer, anti-inflammatory, brain tonic,expectorant, intellect- and memory-promoting, emetic, expectorant, liver tonic, stimulant, sudorific.
- Studies have shown anti-inflammatory, antioxidant, analgesic, anticonvulsant, neuroprotective, memory-enhancing, nephroprotective, antidepressant, anthelmintic, immunomodulatory, intestinal relaxant properties.
Parts used
Seeds, leaves, bark, oil.
Uses
Folkloric
- Pulverized seeds used as antirheumatic; also used for cases of paralysis.
- Leaves used for dysentery.
- Decoction of seeds, with or without aromatics, used for rheumatism, gout, paralysis and gout.
- Boiled seeds used for body and mind purification and blood cleansing.
- Oil, with benzoin, nutmegs, cloves and mace, used as a remedy for beriberi; also used as a powerful stimulant.
- Oil used as ointment for malarious rheumatic pains and for paralysis.
- Root and leaf sap used as antidote for snake bite poisoning.
- In Ayurveda, bark considered as abortifacient; the leaves and leaf sap used as antidote to opium poisoning. Also used as brain tonic, appetite stimulant, and emetic.(1)
- In Greco-Arabic Yunani medicine, seed oil used to treat physical weakness, mental confusion, asthma, headaches, joint pains and arthritis. Also used as a sexual stimulant.
- In India, used for memory difficulties, to improve memory recall and retention.
- In Kerala, India, plant widely used for many human diseases and health disorders. Roots used for purifying the blood, eradicating stomach parasites; root paste for skin disease, ground roots for burns and boils; mixed with C. asiatica as an intellect enhancing tonic. Crush bark stem used as antidote to cobra venom; bark decoction used as abortifacient. Leaves used as anthelmintic; leaf juice locally for earaches; leaf juice for memory power; fried leaves with flowers of H. rosa-sinensis to induce menstruation. Seed oil used for skin diseases, rheumatism, arthritis and various inflammatory conditions; also used for diabetes, beri-beri, asthmatic cough and chest pains. (14)
- Used for leprosy by tribal people of Myong district in Assam, India. Powdered seeds and oil are applied to affected parts. (28)
- In Himalayan medicine, used for treatment of hemorrhoids, gout, rheumatism, cold, dysentery, diarrhea, leprosy, and snake bites. In India, fruit juice used as cardiotonic and seeds as appetizer. Paste of fruit mixed with warm mustard oil and applied to the scalp. In Uttar Pradesh, powdered root used for treatment of cancerous tumors. In Madya Pradesh, root powder and decoction of seeds used to treat rheumatism. Powdered bark taken with cow's milk once a day for a month to cure leucorrhea. (32)
- Poultice of roots used to treat headaches. Crushed roots used for pneumonia. Roots used to treat dysmenorrhea and to induce fertility. Also used for dysentery, diarrhea, fever. Powdered root bark used for treatment of malaria. Root decoction used as brain tonic for depression; also as laxative for cleaning the digestive system. Root bark is abortifacient and depurative. Powdered root used for treatment of tumor. In India, root or root bark paste applied on forehead of children to cure boils. Herbal mix of root of C. paniculatus and Piper longam used for leucorrhea and spermatorrhea. Powdered root or root bark taken with cow's milk once daily for a month to treat leucorrhea. (45)
- Poultice of leaves used for headaches. Leaf sap used as antidote for opium poisoning. Dried leaves used for inducing menstruation. Herbal mixture of powdered leaves, fruits, flowers, and seeds taken regularly to treat mental disorders and increase mental power. Boiled leaves applied externally to swellings and fractures. (45)
Studies
• Phytochemicals: Analysis of seeds yielded terpenes, carbohydrates, saponins, flavonoids, alkaloids and glycosides. (1)
• Antioxidant: Study of aqueous extracts have shown antioxidant activity, augmented endogenous antioxidant enzymes and decreased lipid peroxidation in rat brain.
• Nootropic Effect / Memory Enhancing / Seed: Study evaluated an aqueous seed extract for effects on memory and learning using elevated plus maze and passive avoidance test in a rat model. Piracetam was used as standard drug. Results showed dose-dependent cholinergic activity with a statistical improvement in memory processing compared to control. The mechanism of cognition enhancement may be due to increased acetylcholine level in the rat brain. (2)
• Cognitive Enhancing / Antioxidant / Seeds: Study evaluated various extracts of seeds for their effect on cognitive function in rats. Results showed the aqueous extract of C paniculatus seed has cognitive-enhancing properties and an antioxidant effect might be involved. (7)
• Learning and Memory / Oil: Study data indicates CP oil causes an overall decrease in the turnover of all three central monoamines and suggests involvement of these aminergic systems in the learning and memory process.
• Analgesic / Anti-Inflammatory / Flowers: A study on the methanol extract of flowers showed C paniculatus had both analgesic and anti-inflammatory activities. (3)
• Cognitive Enhancement / Neuroprotection / Seed Oil: Study evaluated the seed oil of Celastrus paniculatus on its effect on the learning process in adult male Wistar rats. Results showed decrease in AChE activity in treated animals leading to increased cholinergic activity in the brain. There was significant decrease in AChE activity assayed from the hypothalamus, frontal cortex and hippocampus of the rat brain. (4)
• Neuroprotective / Glutamate Induced Toxicity: Study on neuronal cultures from rat forebrain to evaluate CP neuroprotective effects showed the water soluble extracts protected against glutamate-induced toxicity by modulation of glutamate receptor function. (6)
• Antibacterial / Antifungal: Study on different leaf extracts showed CP possesses remarkable microbial toxic activity against human and agricultural pathogens. (8)
• Anthelmintic / Oil: Study of the four seed oils from four medicinal plants, including C paniculatus, on the anthelmintic activity against Pheretima posthuma, showed all of them exhibited moderate to significant anthelmintic activity. Piperazine was the standard reference drug. (9)
• Anti-Inflammatory / Seeds: Study of seeds by carrageenan-induced paw edema method on albino rats showed anti-inflammatory activity. Seeds yielded two alkaloids: celastrine and paniculatine. (13)
• Immunomodulatory / Seeds: Study evaluated the immunomodulatory property of a petroleum ether extract of seeds. Results suggested stimulation of humoral immunity as indicated by increase in antibody titer and cell mediated immunity by mean percentage increase in paw volume. There was also increase in immunological, hematological, and oxidative stress parameters in a pyrogallol-induced immunosuppression model in rats. Results showed significant immunomodulatory and antioxidant activity. (15)
• Intestinal Relaxant Effect / Sesquiterpene / Seed Oil: Study evaluated a methanol seed extract for in vivo effects on isolated preparations of rat intestine. Three new sesquiterpene polyol esters were isolated. Results showed a relaxant effect. Three new sesquiterpene polyol esters were isolated, which in synergy with yet undetected compounds, may be responsible for the relaxant effect. (16)
• Neuroprotective / Cortico-Hippocampal Salvage in Chronic Aluminum Induced Neurodegeneration / Seed Oil: Study of C. paniculatus seed oil showed a significant prevention in the onset of aluminum-induced neural insult and overall systemic oxidative stress in an animal model of senile dementia of Alzheimer's type in male Wistar rats. Study concludes that C. paniculatus is a putative decelerator of A1-mediated Alzheimer's like pathobiology. (17)
• Antioxidant / Anti-Inflammatory / Seeds: Study evaluated the essential oil of seeds. Antioxidant activity was evaluated by DPPH, TEAC, FRAP, and lipoxygenase inhibition assays. Chloroform extract of seeds showed high total phenolic content and exhibited strong antioxidant potential. An aqueous extract of seeds showed strong anti-inflammatory properties. (see constituents above) (19)
• Nootropic Effect / Whole Plant: Study evaluated the nootropic activity of C. paniculata whole plant methanolic extract using different rat models. Results showed significant improvement in learning and memory of rats as indicated by decline in transfer latency using elevated plus maze and decrease in escape latency during training and retrieval using morris water maze. The activity was attributed to inhibition of brain AChE activity. (20)
• Hypolipidemic: Study evaluated the hypolipidemic effect of methanolic extract of Celastrus paniculatus in experimentally induced hypercholesteroolemic rats induced by a high fat diet. Results showed significant decrease total cholesterol, triglycerides and LDL with substantial increase in HDL, together with a significant decrease in atherogenic index. (21)
• Effect on Immobilization Stress / Jyothismati Oil / Seed: Jyothismati oil extracted from Celastrus paniculatus seeds was shown to be efficient in treating experimentally induced acute and chronic stress in albino mice. (22)
• Neuromodulating Effect / Aluminum Induced Neurotoxicity / Seeds: Study investigated the preventive potential of alcoholic seed extract in aluminum induced neurotoxicity in cerebral cortex, hippocampus and cerebellum of rat brain. Treatment increased the antioxidant status and activities of membrane bound enzymes and decreased the level of LPO and activities of marker enzymes. Results suggest the seed extract has potential in counteracting the damage inflicted by aluminum on rat brain regions. (23)
• Analgesic / Leaves: Study evaluated different solvent extracts of C. paniculatus leaves for analgesic potential by acetic acid induced writhing assay in Swiss albino mice. All test extracts exhibited significant analgesic activity—the methanol extract was most potent followed by ethyl acetate and petroleum ether extracts. (24)
• Antidepressant / Seed Oil: Study evaluated the antidepressant-like effect of C. paniculatus seed oil in young Swiss albino mice subjected to chronic unpredictable mild stress using models of forced swim test (FST) and sucrose preference test. Results showed significant antidepressant activity in both unstressed and chronic unpredictable mild stressed mice probably due to inhibition of MAO-A activity, decrease in plasma nitrite levels, and scavenging of free radicals. (25) Celastrus paniculatus seed oil produced significant antidepressant-like effect in mice possibly through interaction with dopamine D2, serotonergic and GABA B receptors, as well as inhibition of MAO-A activity and decrease in plasma corticosterone levels. (37)
• Antifungal / Seed Oil: In a study of methanolic crude extract of A. calamus, T. cordifolia and Celetrus paniculatus for antifungal activity, C. paniculatus showed better activity against Alternaria solani and Helminthosporium sp. (see constituents above) (26)
• Relaxant Effect on Rat and Human Ileum: Study evaluated the relaxing action of methanolic extract prepared from seeds of C. paniculatus in rat ileum . CPE exerted a a powerful myogenic and L-type Ca(2+)-dependent relaxing effect in isolated rat ileum. Human ileum was also sensitive to the inhibitory effect of CPE. If confirmed, data could explain the traditional use of the herb for intestinal spasms. (27)
• Effect on Pain and Inflammation / Seeds: Study of alcoholic extract of Celastrus paniculatus seeds in experimentally induced pain and inflammation in Swiss albino mice showed significant antinociceptive and anti-inflammatory effects. Antinociceptive activity was evaluated by tail immersion, hot plate, and acetic acid-induced writhing while anti-inflammatory activity was evaluated by carrageenan-induced acute plantar inflammation. (29)
• Antispermatogenic
/ Reversible Liver Changes / Antifertility Effect / Seed: Study evaluated the effect of oily seed extractives of Celastrus paniculatus on biochemical, histochemical, and histological studies on testes and liver of adult rats. Extract treated animals showed vacuolization, germ depletion, and arrest of spermatogenesis. Livers showed areas of focal necrosis. Intermediate repair and regenerative changes were noticed 30 days post treatment. Results suggest C, pelastrus oil may have used antifertility effects with hepatic degenerative changes that are reversible with time. (31)
• Topical Gel Formulations / Anti-Inflammatory: Study evaluated prepared topical gel formulations from a methanolic fraction of fresh oil from seeds, using Carbomer-940, propylene glycol, and glycerin. Evaluation of selected gel formulations showed the average content of methanol extract was well within ±5% w/w limits, and topical administration induced a dose-dependent reduction in inflammation on carrageenan induced rat paw edema. (34)
• Oil Extraction / Seeds: Study reports on the procedures used by the Pawra tribal community for extraction of medicinal oil from seeds or whole plants. Oils extracted are used mainly for external applications like Celastrus paniculatus for joint pain, cognition enhancement and hair problems. The extraction of oil from C. paniculatus seed is described. The red colored oil obtained can be stored for one year. From one kilogram of seeds, about 300 gm of oil can be extracted. (35)
• Anti-Alzheimer / Antioxidant / Seed: Crude methanolic extract and organic soluble fractions of C. paniculatus seed were evaluated for antioxidant and anti-Alzheimer activity. The extracts showed prominent DPPH free radical scavenging activity, inhibition of peroxynitrite and inhibition of total ROS generation. The EtOAc fraction showed significant (p<0.001) cholinesterase/s (ChEs) inhibitory effects with IC50 ranging between 134.7-227.5 µg/ml for AChE and 209.6-562.1 µg/ml for BChE. (36)
• Neuroprotective Effect of Celestrus paniculatus on Chronic Stress-Induced Cognitive Impairment: Studies have reported the chronic stress result in impaired spatial learning and working memory and enhanced anxiety-like behavior. Chronic treatment with C. paniculatus oil improved cognitive abilities in chronically stressed rats. Results suggest a novel perspective and potential of herbal therapy on stress-induced cognitive dysfunctions. (38)
•
Celapanin / Sesquiterpene / Leaves: Study isolated a sesquiterpene derivative, celapanin, from the acetone soluble fraction of ethanol extract of C. paniculatus leaves. The crude ethanol extract and compound was tested against 30 clinical strains including gram-negative P. aeruginosa and K. pneumonia and gram-positive S. aureus. Results showed promising antibacterial activity against gram-positive S. aureus, comparative with standard drug ciprofloxacin. (40)
• Effect of Seed Oil on Spatial and Fear Memory / Scopolamine Induce Amnesia / Seed Oil: Study evaluated the memory enhancing effect of C. paniculatus seed oil using elevated plus maze and passive avoidance tests to test spatial and fear memory, respectively. Seed oil was mixed with equal amount of pure ghee and administered orally to mice. Piracetam was used as standard nootropic while scopolamine was used as amnesic agent. Results showed significant memory enhancement compared to the scopolamine group. C paniculatus effect and combination of CP plus piracetam was comparable to piracetam alone. Results suggest the seed oil has memory enhancing effect with potential as drug in treatment of dementia. (41)
• Mitigation of Monosodium Induced Impairments in Human Neuronal Cells IMR-32 / Seeds: Study evaluated aqueous extracts of seeds for its neuroprotective efficacy against adverse effects of monosodium glutamate (MSG) in neuroblastoma cell line IMR-32. Results showed significant inhibition of DPPH and NO radicals. The AE not only enhanced antioxidant activity but also reduced free radical mediated cytotoxicity of MSG in IMR-32 cells, along with reduction of DNA damage in neuronal cells due to free radical toxicity of MSG. Results conclude AE is an effective and potent neuroprotective herb to mitigate MSG induced neuronal impairment in IMR-32 cells. (42)
• Skin Penetration and Stability Enhancement by
HPßCD Inclusion Complex / Cosmetic Application / Seed Oil: Study evaluated the encapsulation of CP seed oil in 2-hydroxypropyl-ß-cyclodextrin (HBßCD) cavities and investigated its biologic activity, physiochemical stability and skin penetration. Results suggest the CPSO-HBßCD inclusion complex may be beneficial for development of cosmeceutical products. (43)
• Effect on Seminal Vesicles / Seed Oil: Study evaluated the effects of oil extracted from seeds of C. paniculatus on seminal vesicles of male mature albino rats. Histology showed involution of the gland. Histochemically, there was statistically significant increase of lipids in the glandular epithelium.
(44)
• Nephroprotective / Lead Acetate-Induced Toxicity / Seeds: Study evaluated the nephroprotective activity of ethanolic extract of seeds against lead acetate (LA) induced nephrotoxicity in Wistar rats. Extract treatment at 800 mg/kbw significantly down-regulated serum urea, creatinine, and KIM 1 levels and level of oxidative stress markers, Histological and immunohistochemistry showed significant change in the cytoarchitecture of renal tissue thereby revealing the pro-active role of C. paniculatus seeds in nephrotoxicity. (46)
• Silver Nanoparticles / Antibacterial / Leaf and Callus: Study reports on the protocol for synthesis of AgNPs from invivo leaf and invitro developed callus extract of C. paniculatus. Both extracts showed great antibacterial potential as evidenced by zone of inhibitions for both gram-positive and gram-negative bacteria. AgNPs from the callus extract showed better results with 24.00 ± 1.00 mm ZOI. (47)
• Amelioration of LPS-Induced Lung Inflammation / Seed Oil: Study evaluated the effect of C. paniculatus seed oil on lipopolysaccharide (LPS)-induced mice model of respiratory inflammation. Results showed significant reduction in neutrophil infiltration following CP oil treatment for one month, along with significant decreases in ROS generation. Study suggests C. paniculatus seed oil seems to reduce oxidative stress by inhibiting the generation of reactive oxygen species in LPS-induced lung inflammation. (49)
• Neuroprotective / Epilepsy and Epilepsy-Associated Cognitive Deficits / Seed: Study evaluated the effect of Celastrus paniculatus seed extract (alone or in combination with sodium valproic acid and Pergolide) on seizure severity and cognitive deficit following pentylenetetrazole (PTZ)-induced chemical kindling model using behavioral parameters, Morris water maze test (MWM), grip strength test (GPS), brain superoxide dismutase (SOD), catalase, reduced glutathione (GSH) and dopamine level. Results showed significantly reduced seizure score, mean latency time, distance traveled in MWM, elevated antioxidant markers (GSH, catalase, SOD, and dopamine levels). C. paniculatus and combination therapy also significantly (p<0.05) protected against neuronal loss in hippocampus and frontal cortex by H&E staining. Results suggest potential for the treatment of epilepsy and associated cognitive deficits. (50)
Availability
Wild-crafted.
Oil, seeds, tinctures, and extracts in the cybermarket.
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