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Article

Isolation and In Vitro Activity of Sesquiterpene Lactones from Eremanthus crotonoides as SARS-CoV-2 Protease Inhibitors and Cytotoxic Agents

by
Patricia Homobono Brito de Moura
1,2,
Natalie Giovanna da Rocha Ximenes
1,
Beatriz Bastos Santos
1,
Carla Monteiro Leal
1,
Larissa Esteves Carvalho Constant
3,
Stephany da Silva Costa
3,
Shaft Corrêa Pinto
4,
Michelle Frazao Muzitano
4,
Diego Allonso
5,
Ludger A. Wessjohann
2,* and
Ivana Correa Ramos Leal
1,*
1
Laboratory of Natural products and Biological Assays, Natural Products and Food Department, Pharmacy Faculty, Center of Health Sciences, Federal University of Rio de Janeiro (UFRJ), Rio de Janeiro 21941-902, RJ, Brazil
2
Leibniz Institute of Plant Biochemistry, Department of Bioorganic Chemistry, Weinberg 3, 06120 Halle, Germany
3
Laboratory of Biotechnology and Tissue Bioengineering, Institute of Biophysics Carlos Chagas Filho, Center of Health Sciences, Federal University of Rio de Janeiro (UFRJ), Rio de Janeiro 21941-902, RJ, Brazil
4
Laboratory of Bioatives Products, Institute of Pharmaceutical Sciences, Federal University of Rio de Janeiro (UFRJ), Macaé 27933-378, RJ, Brazil
5
Department of Pharmaceutical Biotechnology, Pharmacy Faculty, Center of Health Sciences, Federal University of Rio de Janeiro (UFRJ), Rio de Janeiro 21941-902, RJ, Brazil
*
Authors to whom correspondence should be addressed.
Molecules 2025, 30(20), 4053; https://doi.org/10.3390/molecules30204053
Submission received: 4 August 2025 / Revised: 9 September 2025 / Accepted: 17 September 2025 / Published: 11 October 2025
(This article belongs to the Special Issue Plant Metabolites: Isolation, Phytochemistry, and Biological Activities)
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Abstract

The Jurubatiba Sandbank National Park (PARNA Jurubatiba) is an ecological reserve characterized by harsh environmental conditions, including low rainfall, high sun exposure, and sandy soil. Among its native vegetation, Eremanthus crotonoides stands out for its richness in flavonoids, phenolic compounds, and sesquiterpene lactones. The objective of this study was to isolate and quantify sesquiterpene lactones from this species using 1H NMR and to investigate their anti-SARS-CoV-2 potential and cytotoxicity against cancer cells. UPLC-(ESI)-MS/MS analyses enabled metabolite annotation, and semi-preparative HPLC-DAD allowed the isolation of centratherin and goyazensolide, which were identified by 1D and 2D NMR. In vitro assays showed that centratherin at 10 µM concentration reduced the viability of PC-3 and HCT-116 cancer cells by 100%, while goyazensolide had no noteworthy effects. Furthermore, enzymatic inhibition assays on SARS-CoV2 targets revealed that centratherin exhibited a lower apparent IC50 of 12 µM against PLpro, while goyazensolide was more active against 3CLpro, with an IC50 of 71 µM. Notably, the dichloromethane fraction demonstrated promising activity against both enzymes, with IC50 values of 30 µM for PLpro and 11 µM for 3CLpro. This study reports, for the first time, the isolation of goyazensolide from E. crotonoides and highlights the potential of both sesquiterpene lactones as SARS-CoV-2 enzyme inhibitors. In contrast to centratherin, goyazensolide fortunately had almost no cytotoxic effects at inhibition concentration on the cells tested. This shows that anticancer and anti-SARS effects can be separated and should have different SARs, an important prerequisite for further development.
Keywords: centratherin; cytotoxicity; Eremanthus crotonoides; goyazensolide; sesquiterpene lactones; SARS-CoV-2 centratherin; cytotoxicity; Eremanthus crotonoides; goyazensolide; sesquiterpene lactones; SARS-CoV-2

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MDPI and ACS Style

de Moura, P.H.B.; Ximenes, N.G.d.R.; Santos, B.B.; Leal, C.M.; Constant, L.E.C.; Costa, S.d.S.; Pinto, S.C.; Muzitano, M.F.; Allonso, D.; Wessjohann, L.A.; et al. Isolation and In Vitro Activity of Sesquiterpene Lactones from Eremanthus crotonoides as SARS-CoV-2 Protease Inhibitors and Cytotoxic Agents. Molecules 2025, 30, 4053. https://doi.org/10.3390/molecules30204053

AMA Style

de Moura PHB, Ximenes NGdR, Santos BB, Leal CM, Constant LEC, Costa SdS, Pinto SC, Muzitano MF, Allonso D, Wessjohann LA, et al. Isolation and In Vitro Activity of Sesquiterpene Lactones from Eremanthus crotonoides as SARS-CoV-2 Protease Inhibitors and Cytotoxic Agents. Molecules. 2025; 30(20):4053. https://doi.org/10.3390/molecules30204053

Chicago/Turabian Style

de Moura, Patricia Homobono Brito, Natalie Giovanna da Rocha Ximenes, Beatriz Bastos Santos, Carla Monteiro Leal, Larissa Esteves Carvalho Constant, Stephany da Silva Costa, Shaft Corrêa Pinto, Michelle Frazao Muzitano, Diego Allonso, Ludger A. Wessjohann, and et al. 2025. "Isolation and In Vitro Activity of Sesquiterpene Lactones from Eremanthus crotonoides as SARS-CoV-2 Protease Inhibitors and Cytotoxic Agents" Molecules 30, no. 20: 4053. https://doi.org/10.3390/molecules30204053

APA Style

de Moura, P. H. B., Ximenes, N. G. d. R., Santos, B. B., Leal, C. M., Constant, L. E. C., Costa, S. d. S., Pinto, S. C., Muzitano, M. F., Allonso, D., Wessjohann, L. A., & Leal, I. C. R. (2025). Isolation and In Vitro Activity of Sesquiterpene Lactones from Eremanthus crotonoides as SARS-CoV-2 Protease Inhibitors and Cytotoxic Agents. Molecules, 30(20), 4053. https://doi.org/10.3390/molecules30204053

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