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Your search keyword '"José E. Rodríguez-Borges"' showing total 4 results
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4 results on '"José E. Rodríguez-Borges"'

1. Coelenterazine Derivatives as Potential Drugs for Photodynamic Therapy

Author

Daiane Nascimento Maronde, Ivo E. Sampaio-Dias, Luís Pinto da Silva, Leandro M. O. Lourenço, and José E. Rodríguez-Borges

Subjects
cancer, coelenterazine (Clz), photodynamic therapy (PDT), photosensitizer (PS), Medicine
Abstract

Cancer is one of the main leading causes of death worldwide, and its treatment is highly complex and known to cause serious side effects for patients. Photodynamic therapy (PDT) has gained a worldwide impact as a promising alternative strategy to overcome or minimize these potential side effects observed in conventional therapeutical approaches. This therapy is a minimally invasive treatment that combines a photosensitizer (PS), visible light, and molecular oxygen (3O2). When excited, the PS interacts with 3O2 to generate reactive oxygen species (ROS), mainly as singlet oxygen (1O2) which, in turn, induces cytotoxic effects in cancer cells. In a recent study led by our research group, coelenterazine (Clz) analogues have shown relevant cell-selective toxicity in different cancer cell lines, such as breast, liver, prostate, and neuroblastoma, without cytotoxic effects in the corresponding non-tumoral cells. Based on these results, this work aims to synthesize a new series of Clz-inspired PS derived from pyrazine scaffold, a common precursor for the synthesis of Clz and its structure-related analogues. Herein, we describe some methodological approaches for the synthesis of pyrazine-based precursors with high chemical yields and their chemical characterization for the assembly of Clz analogues. Currently, these compounds are being studied for the assembly of new PS with potential application for PDT.

Published
2022
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4. Discovery of the Anticancer Activity for Lung and Gastric Cancer of a Brominated Coelenteramine Analog

Author

Patricia González-Berdullas, Renato B. Pereira, Cláudia Teixeira, José Pedro Silva, Carla M. Magalhães, José E. Rodríguez-Borges, David M. Pereira, Joaquim C. G. Esteves da Silva, Luís Pinto da Silva, Faculdade de Farmácia, Faculdade de Ciências, and Universidade do Minho

Subjects
cancer, Coelenterazine, Coelenteramine, Coelenteramide, bioluminescence, chemiluminescence, anticancer therapy, Lung Neoplasms, Molecular Structure, Organic Chemistry, Antineoplastic Agents, Apoptosis, General Medicine, Catalysis, Computer Science Applications, Inorganic Chemistry, Structure-Activity Relationship, Stomach Neoplasms, Cell Line, Tumor, Humans, Physical and Theoretical Chemistry, Molecular Biology, Lung, Spectroscopy, Cell Proliferation
Abstract

Supplementary Materials: The following supporting information can be downloaded at: https: //www.mdpi.com/article/10.3390/ijms23158271/s1., Cancer is still a challenging disease to treat, both in terms of harmful side effects and therapeutic efficiency of the available treatments. Herein, to develop new therapeutic molecules, we have investigated the anticancer activity of halogenated derivatives of different components of the bioluminescent system of marine Coelenterazine: Coelenterazine (Clz) itself, Coelenteramide (Clmd), and Coelenteramine (Clm). We have found that Clz derivatives possess variable anticancer activity toward gastric and lung cancer. Interestingly, we also found that both brominated Clmd (Br-Clmd) and Clm (Br-Clm) were the most potent anticancer compounds toward these cell lines, with this being the first report of the anticancer potential of these types of molecules. Interestingly, Br-Clm possessed some safety profile towards noncancer cells. Further evaluation revealed that the latter compound induced cell death via apoptosis, with evidence for crosstalk between intrinsic and extrinsic pathways. Finally, a thorough exploration of the chemical space of the studied Br-Clm helped identify the structural features responsible for its observed anticancer activity. In conclusion, a new type of compounds with anticancer activity toward gastric and lung cancer was reported and characterized, which showed interesting properties to be considered as a starting point for future optimizations towards obtaining suitable chemotherapeutic agents., The Portuguese “Fundação para a Ciência e Tecnologia“ (FCT) is acknowledged for funding project PTDC/QUI-QFI/2870/2020, the R&D Units CIQUP (UIDB/00081/2020), GreenUPorto (UIDB/05748/2020), LAQV/REQUIMTE (UIDB/50006/2020), and the Associated Laboratory IMS (LA/P/0056/2020). L. Pinto da Silva acknowledges funding from FCT under the Scientific Employ ment Stimulus (2021.00768.CEECIND). Patricia González-Berdullas acknowledges funding for her postdoctoral position in the framework of project PTDC/QUI/QFI/2870/2020. Carla Magalhães acknowledges FCT for her PhD grant (SRFH/BD/143211/2019). Renato B. Pereira acknowledges PRIMA Foundation (H2020- PRIMA 2018—Section 2, Project MILKQUA) and FCT (PTDC/QUI QFI/2870/2020) for the funding.

Published
2022
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