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Review
. 2023 Jul 5;13(7):1514.
doi: 10.3390/life13071514.

Triterpenes as Potential Drug Candidates for Rheumatoid Arthritis Treatment

Affiliations
Review

Triterpenes as Potential Drug Candidates for Rheumatoid Arthritis Treatment

Célia Faustino et al. Life (Basel). .

Abstract

Rheumatoid arthritis (RA) is a chronic autoimmune inflammatory disease characterized by joint inflammation, swelling and pain. Although RA mainly affects the joints, the disease can also have systemic implications. The presence of autoantibodies, such as anti-cyclic citrullinated peptide antibodies and rheumatoid factors, is a hallmark of the disease. RA is a significant cause of disability worldwide associated with advancing age, genetic predisposition, infectious agents, obesity and smoking, among other risk factors. Currently, RA treatment depends on anti-inflammatory and disease-modifying anti-rheumatic drugs intended to reduce joint inflammation and chronic pain, preventing or slowing down joint damage and disease progression. However, these drugs are associated with severe side effects upon long-term use, including immunosuppression and development of opportunistic infections. Natural products, namely triterpenes with anti-inflammatory properties, have shown relevant anti-arthritic activity in several animal models of RA without undesirable side effects. Therefore, this review covers the recent studies (2017-2022) on triterpenes as safe and promising drug candidates for the treatment of RA. These bioactive compounds were able to produce a reduction in several RA activity indices and immunological markers. Celastrol, betulinic acid, nimbolide and some ginsenosides stand out as the most relevant drug candidates for RA treatment.

Keywords: betulinic acid; celastrol; ginsenosides; inflammation; rheumatoid arthritis; saponins; triterpenes.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 2
Figure 2
Structures of pentacyclic triterpenes (113) with activity on RA.
Figure 3
Figure 3
Structures of tetracyclic (1415) and rearranged triterpenes (1619) with activity on RA.
Figure 4
Figure 4
Structures of triterpenic saponins (2031) with activity on RA.
Figure 4
Figure 4
Structures of triterpenic saponins (2031) with activity on RA.
Figure 5
Figure 5
Structures of ginsenosides (3236) with activity on RA.
Figure 1
Figure 1
Structures of the main tetracyclic and pentacyclic triterpene skeletons.
Figure 6
Figure 6
Main modes of action of anti-RA triterpenoids. Created with BioRender.com (accessed on 14 June 2023).

References

    1. Newman D.J., Cragg G.M. Natural Products as Sources of New Drugs over the Nearly Four Decades from 01/1981 to 09/2019. J. Nat. Prod. 2020;83:770–803. doi: 10.1021/acs.jnatprod.9b01285. - DOI - PubMed
    1. Cragg G.M., Newman D.J. Natural products: A continuing source of novel drug leads. Biochim. Biophys. Acta Gen. Subj. 2013;1830:3670–3695. doi: 10.1016/j.bbagen.2013.02.008. - DOI - PMC - PubMed
    1. Newman D.J., Cragg G.M. Natural Products as Sources of New Drugs from 1981 to 2014. J. Nat. Prod. 2016;79:629–661. doi: 10.1021/acs.jnatprod.5b01055. - DOI - PubMed
    1. Newman D.J. Natural products and drug discovery. Natl. Sci. Rev. 2022;9:nwac206. doi: 10.1093/nsr/nwac206. - DOI - PMC - PubMed
    1. Atanasov A.G., Zotchev S.B., Dirsch V.M., Orhan I.E., Banach M., Rollinger J.M., Barreca D., Weckwerth W., Bauer R., Bayer E.A., et al. Natural products in drug discovery: Advances and opportunities. Nat. Rev. Drug Discov. 2021;20:200–216. doi: 10.1038/s41573-020-00114-z. - DOI - PMC - PubMed

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