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Volume 26
Issue 16
10.3390/ijms26167765
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Review

Anticancer Activity of the Marine-Derived Compound Bryostatin 1: Preclinical and Clinical Evaluation

by
Tomasz Kowalczyk
1,*,
Marek Staszewski
2,
Magdalena Markowicz-Piasecka
3,
Joanna Sikora
4,
Catarina Amaro
5,
Laurent Picot
6 and
Przemysław Sitarek
7,*
1
Department of Molecular Biotechnology and Genetics, Faculty of Biology and Environmental Protection, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland
2
Department of Synthesis and Technology of Drugs, Medical University of Lodz, Muszynskiego 1, 90-151 Lodz, Poland
3
Department of Applied Pharmacy, Medical University of Lodz, Muszynskiego 1, 90-151 Lodz, Poland
4
Department of Bioinorganic Chemistry, Medical University of Lodz, Muszynskiego 1, 90-151 Lodz, Poland
5
Students Research Group (Erasmus student), Department of Medical Biology, Medical University of Lodz, 90-151 Lodz, Poland
6
Littoral Environnement et Sociétés UMRi CNRS 7266 LIENSs, La Rochelle Université, 17042 La Rochelle, France
7
Department of Medical Biology, Medical University of Lodz, Muszynskiego 1, 90-151 Lodz, Poland
*
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2025, 26(16), 7765; https://doi.org/10.3390/ijms26167765
Submission received: 1 July 2025 / Revised: 31 July 2025 / Accepted: 9 August 2025 / Published: 11 August 2025
(This article belongs to the Special Issue IJMS 25th Anniversary: Updates and Progress on Bioactives and Nutraceuticals)
Versions Notes

Abstract

Bryostatin 1, a natural macrolide isolated from Bugula neritina, is a potent modulator of protein kinase C (PKC) isoforms with promising anticancer properties. In numerous in vitro studies, bryostatin 1 has been shown to inhibit tumor cell proliferation and induce differentiation and apoptotic cell death in a wide range of cell lines, including leukemia, lymphoma, glioma, and solid tumors such as ovarian and breast cancer. Its antitumor activity, both as monotherapy and in combination with conventional chemotherapy, has been confirmed in in vivo models, where synergistic effects have been observed, including sensitization of tumor cells to cytostatic agents. Despite promising preclinical findings, phase I and II clinical trials have not yielded the expected results, suggesting limited efficacy of the macrolide as a single agent with a relatively favorable safety profile. Current research directions focus on optimizing dosing regimens, combining bryostatin 1 with other anticancer drugs and identifying predictive biomarkers of response. This article reviews the current state of knowledge on the anticancer effects of bryostatin 1, analyzing available data from in vitro, in vivo, and clinical trials and discussing potential directions for further translational research.
Keywords: Bugula neritina; Bryostatin 1; modulator of protein kinase C; anticancer effect; clinical trials Bugula neritina; Bryostatin 1; modulator of protein kinase C; anticancer effect; clinical trials

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MDPI and ACS Style

Kowalczyk, T.; Staszewski, M.; Markowicz-Piasecka, M.; Sikora, J.; Amaro, C.; Picot, L.; Sitarek, P. Anticancer Activity of the Marine-Derived Compound Bryostatin 1: Preclinical and Clinical Evaluation. Int. J. Mol. Sci. 2025, 26, 7765. https://doi.org/10.3390/ijms26167765

AMA Style

Kowalczyk T, Staszewski M, Markowicz-Piasecka M, Sikora J, Amaro C, Picot L, Sitarek P. Anticancer Activity of the Marine-Derived Compound Bryostatin 1: Preclinical and Clinical Evaluation. International Journal of Molecular Sciences. 2025; 26(16):7765. https://doi.org/10.3390/ijms26167765

Chicago/Turabian Style

Kowalczyk, Tomasz, Marek Staszewski, Magdalena Markowicz-Piasecka, Joanna Sikora, Catarina Amaro, Laurent Picot, and Przemysław Sitarek. 2025. "Anticancer Activity of the Marine-Derived Compound Bryostatin 1: Preclinical and Clinical Evaluation" International Journal of Molecular Sciences 26, no. 16: 7765. https://doi.org/10.3390/ijms26167765

APA Style

Kowalczyk, T., Staszewski, M., Markowicz-Piasecka, M., Sikora, J., Amaro, C., Picot, L., & Sitarek, P. (2025). Anticancer Activity of the Marine-Derived Compound Bryostatin 1: Preclinical and Clinical Evaluation. International Journal of Molecular Sciences, 26(16), 7765. https://doi.org/10.3390/ijms26167765

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