Phytochemistry and pharmacology of Celastrus paniculatus Wild: a nootropic drug

C. paniculatus is a rich source of several secondary metabolites……The various study shows that the extracts and active constituent of this plant possess potent nootropic activity. Besides nootropic activity, it has also been reported for anti-Alzheimer, anticonvulsant, antidepressant, antioxidant, analgesic, anti-inflammatory, antiarthritic, gastroprotective, anti-psoriatic, wound healing, antibacterial, antimalarial, and several other properties.

J Complement Integr Med  2021 Sep 15;20(1):24-46.  doi: 10.1515/jcim-2021-0251. eCollection 2023 Mar 1

Lipid Reducing

In comparison to the induced hypercholesterolemic animal group, oral treatment of methanolic seed extract (50%) of Celastrus paniculatus at the optimal dose of 65 mg/kg body weight significantly lowered plasma total cholesterol, triglycerides, and LDL cholesterol with results that were comparable to the conventional hypocholesterolemic medication and practically identical to the control group.

Patil, R H , Prakash K, Maheshwari V L, Hypolipidemic Effect of Celastrus paniculatus in Experimentally Induced Hypercholesterolemic Wistar Rats, Ind J Clin Biochem 25, 2010;405–410, https://doi.org/10.1007/s12291-010-0050-x.

Anxiety Reducing

In a staircase test in mice, Celastrus paniculatus plant extract reduced the beginning of action in pentobarbitoneinduced sleep, increased the overall duration of sleep and demonstrated anxiolytic effects.

Ramamoorthy Rajkuma, Elavarasan P K, Suresh S, Bhojraj S. Evaluation of anxiolytic potential of Celastrus oil in rat models of behaviour, Fitoterapia, 2007; 78(2):120-124, ISSN 0367- 326X, https://doi.org/10.1016/j.fitote.2006.09.028

Brain Enhancing (Nootropic)

Aqueous extract of Celastrus paniculatus seeds has dose-dependent cholinergic activity which improved memory performance in rats and mice.  It is estimated that increased acetylcholine level in rat brain may be the mechanism by which Celastrus paniculatus enhances cognition.

Bhanumathy M, Harish S, Shivaprasad N, Sushma G, Nootropic activity of Celastrus paniculatus seed. Pharmaceutical Biology, 2010;48(3):324-327.

Cardiovascular Improvement

The crude CP seed oil administered as emulsion (50-100 mg/kg) produced a gradual fall in cardiac output, bradycardia and marked increase in pulse pressure on isolated heart lung preparation in cat. A similar action with 1 g of emulsified oil was also observed in dogs.

Bhanumathy M, Chandrasekar S B, Chandur Uma, Somasundaram T. Phyto-pharmacology of Celastrus paniculatus: An Overview. International Journal of Pharmaceutical Sciences and Drug Research 2010;2(3):176- 181, ISSN 0975-248X.

Neuroprotective Activity & Free Radical Scavenging

Protective effect on H2O2 -induced cytotoxicity and freeradical scavenging action, which is dose dependent were shown by Celastrus paniculatus methanolic extract. It also showed damage of DNA in non-immortalized fibroblasts of human beings.31 Water extract of Celastrus paniculatus, reduced lipid peroxidation and increased the enzyme catalase activity (which is antioxidant in nature), as a result it protected cultured neuronal cells of forebrain.32 CP water extract showed neuroprotective action against toxicity caused by glutamate in neuronal cultures and reversibly inhibited N-methyl-D-aspartate-activated whole currents.33 It was reported that Chronic oral administration of oil of Celastrus paniculatus seeds (50, 200, or 400 mg/kg) for 14 days time period has reversed the scopolamine (0.5 mg/kg)-induced learning deficits completely.

Bhagya V, Thomas Christofer, B. S. Shankaranarayana Rao, Neuroprotective effect of Celastrus paniculatus on chronic stress-induced cognitive impairment, Indian J Pharmacol 2016;48:687-93.

Analgesic and Anti-inflammatory Activity

Methanolic extract of flowers of Celastrus paniculatus was prepared by extraction by using absolute methanol. Hot water tail immersion test in mice and carrageenan induced paw edema in rats are the tests which are employed in this procedure. Prepared extract was tested for oral analgesic and anti-inflammatory activity. This study reported that CP had analgesic and anti-inflammatory both activities.

Ahmad F, Khan R A, Rasheed S, Preliminary screening of methanolic Extracts of Celastrus paniculatus and Tecomella undulata for analgesic and anti- inflammatory activities, Journal of Ethnopharmacology, 1994;42(3):193-198, ISSN 0378-8741.

Anti-Alzheimer Activity

The anti-alzheimer (AD) activity of the crude methanolic extract of Celastrus paniculatus plant as well as its organic soluble fraction was investigated. The extracts demonstrated strong DPPH free radical scavenging activity as well as inhibition of authentic peroxynitrite (ONOO-) activity and total reactive oxygen species (ROS) generation.

Badrul A, Ekramul H, Anti-Alzheimer and Antioxidant Activity of Celastrus paniculatus Seed, Iranian Journal of Pharmaceutical Sciences, 2011;7(1):49-56

Anti-depressant Activity

It is reported that both stressed as well as unstressed mice in FST showed significant decrease in the immobility period when administered Celastrus paniculatus seed oil in doses 50, 100 and 200 mg/kg b.w. by p.o. route for 14 succesive days and hence showed significant effect just like an antidepressant.

Valecha R, Dhingra D, Antidepressant-like Activity of Celastrus paniculatus Seed Oil in Mice Subjected to Chronic Unpredictable Mild Stress, British Journal of Pharmaceutical Research, 2014;4(5):576-593.

Antioxidant Activity

It is reported that Methanol, ethyl acetate, pet ether and water extracts of Celastrus paniculatus seed have antioxidant capacity. The findings show that the extracts have antioxidant potential.

Zohera F, Habib M, Imam M, Mazumder M, Rana M, Comparative Antioxidant Potential of Different Extracts of Celastrus paniculatus Willd. Seed, Stamford Journal of Pharmaceutical Sciences, 3(1): 68-74, https://doi.org/10.3329/sjps.v3i1.6802.

Anti-Arthritic Activity

It is reported that petroleum ether fraction (PCP or Petroleum ether extract of dried seeds) produced from Celastrus paniculatus, when given to rats in doses 200mg/kg and 400 mg/kg, significantly suppressed swelling in a dose-dependent manner, thereby reducing the arthritic score in the FCA-injected paw (P < .01). It considerably decreased arthritic progression with respect to paw swelling, arthritic score, immune organ indices and body weight. This result was connected with considerable suppression of overproduction of inflammatory cytokines (TNF-α and IL-6), oxidative stress indicators (MDA and NO) and cellular enzyme (AST, ALT and ALP) levels compared to arthritic mice without therapy.

Kothavade P S, Bulani V D, Deshpande Padmini D, Chowdhury Amrita S, Archana R. Juvekar Archana R, The petroleum ether fraction of Celastrus paniculatus Willd. seeds demonstrates anti-arthritic effect in adjuvant-induced arthritis in rats, Journal of Traditional Chinese Medical Sciences, 2015;2(3):183-193, ISSN 2095-7548, https://doi.org/10.1016/j.jtcms.2016.02.004.

Gastroprotective and Anti-ulcer Activity

Celastrus paniculatus seed oil (CPO) in rats when used against various gastric ulcer models, reported to have gastroprotective and antiulcer properties.

Palle Suresh, Kanakalatha, Kavitha C N, Gastroprotective and Antiulcer Effects of Celastrus paniculatus Seed Oil against Several Gastric Ulcer Models in Rats, Journal of Dietary Supplement, 2018;15:4, 373- 385, DOI: 10.1080/19390211.2017.1349231.