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Abstract
Xanthone derivatives have shown promising antitumor properties, and 1-carbaldehyde-3,4-dimethoxyxanthone (1) has recently emerged as a potent tumor cell growth inhibitor. In this study, its effect was evaluated (MTT viability assay) against a new panel of cancer cells, namely cervical cancer (HeLa), androgen-sensitive (LNCaP) and androgen-independent (PC-3) prostate cancer, and nonsolid tumor derived cancer (Jurkat) cell lines. The effect of xanthone 1 on macrophage functions was also evaluated. The effect of xanthone 1-conditioned THP-1 human macrophage supernatants on the metabolic viability of cervical and prostate cancer cell lines was determined along with its interference with cytokine expression characteristic of M1 profile (IL-1 ≤ β; TNF-α) or M2 profile (IL-10; TGF-β) (PCR and ELISA). Nitric oxide (NO) production by murine RAW264.7 macrophages was quantified by Griess reaction. Xanthone 1 (20 µM) strongly inhibited the metabolic activity of the cell lines and was significantly more active against prostate cell lines compared to HeLa (p < 0.05). Jurkat was the cell most sensitive to the effect of xanthone 1. Compound 1-conditioned IL-4-stimulated THP-1 macrophage supernatants significantly (p < 0.05) inhibited the metabolic activity of HeLa, LNCaP, and PC-3. Xanthone 1 did not significantly affect the expression of cytokines by THP-1 macrophages. The inhibiting effect of compound 1 observed on the production of NO by RAW 264.7 macrophages was moderate. In conclusion, 1-carbaldehyde-3,4-dimethoxyxanthone (1) decreases the metabolic activity of cancer cells and seems to be able to modulate macrophage functions.
| Original language | English |
|---|---|
| Article number | 3721 |
| Journal | Molecules |
| Volume | 26 |
| Issue number | 12 |
| DOIs | |
| Publication status | Published - 2 Jun 2021 |
Keywords
- 1-carbaldehyde-3,4-dimethoxyxanthone
- Antitumor
- Cervical cancer
- Prostate cancer
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CBQF Multianual Funding: Centre for Biotechnology and Fine Chemistry
Cortez, J., Pintado, M. M., Morais, A. M. M. B., Ribeiro, A. B., Ferreira, A. C., Castro, P. M. L., Villamor, A. L., Oliveira, A. L., Oliveira, A. L. S., Amaro, A. L., Paulo, A., Gomes, A. M., Marques, A., Carvalho, A. P., Monforte, A. R., Madureira, A. R., Oliveira, A. S., Ferreira, A. S., Rangel, A. O. S. S., Oliveira, C., Oliveira, C., Pereira, C. F., Santos, C. S. D., Amorim, C. L., Oliveira, C., Manaia, C., Silva, C. L. M., Monteiro, C. M., Machado, D., Campos, D., Oliveira, D., Valente, D., Cardoso, E., Costa, E. M. A. D., Pinto, E., Alexandre, E., Carsanba, E., Coscueta, E., Raposo, M. F. D. J., Tavaria, F., Voss, G. B., Moreira, H., Campos, I., Tomada, I., Moreira, I. S., Vaz-Moreira, I., Fundo, J. F., Barbosa, J. I. B., Pereira, J. O., Durão, J. R. D. O., Costa, J. R., Fernandes, J. C., Ferreira, J., Silva, J. A., Couto, J. A., Oliveira, L., Pimentel, L., Rodríguez-Alcalá, L. M., Hogg, C., Poças, M. D. F., Miller, F. A., Brassesco, M. E., Mota, I., Ramos, I. N., Vasconcelos, I., Monteiro, M. J., Amorim, M., Roriz, M., Silva, M., Correia, M., Silva, M. N. D., Alves, M., Vasconcelos, M., Ramos, O. L., Costa, P., Gibbs, P., Teixeira, P., Ramos, P., Rodrigues, P. M., Carvalho, P., Mesquita, R., Barros, R., Morais, R. M. S. C., Magalhães, R. M. B. D. S., Borges, S. C. F., Correia, S., Silva, S. B. D., Silva, S., Moreira, S. A. M., Pedrosa, S., Pereira, S., Vidigal, S., Pedro, T., Ribeiro, T., Deuchande, T., Brandão, T. R. S., Resende, T., Hogg, T., Ferreira, V., Viseras, A. D., Soares, A. M. S., Oliveira, A. S., Uribe, B., Pais-Vieira, C., Ferreira, C., Sousa, C. C. S., Kumla, D., Carsanba, E., Lopes, G. L. L., Ribeiro, I. M. M. V. P., Cruz, I. B. D., Barbosa, J. C., Oliveira, L., Mendes, M. A. R., Boas, A. V., Cassoni, A. C., Lopes, A., Pintado, A. I. E., Sousa, A. P., Faustino, M., Salsinha, A. S., Couto, A. T., Macieira, A., Horta, B. M., Maciel, C., Rodrigues, C. M., Bernardes, B. G., Silva, B., Costa, C., Costa, C. M., Serafim, C., Santos, D., Antunes, F., Vieira, E., Ferreira, H., Moreira, I. A., Vieira, I. R. D. F., Rocha, J., Henggeler , J., Miranda, J., Oliveira, M., Lopes, M. T. B. V., Silva, N., Carvalho, N., Costa, P., Nova, P., Sousa, P., Silva, P., Gómez-García, R., Freixo, R., Marçal, S., Cunha, S. A. S., Sousa, S., Pereira, S. A., Ghalamara, S., Vilela, T., Lopes, A., Lopes, A. I., Linhares, A. L. S., Vilas-Boas, A. M., Teixeira, A. M. R., Mendes, A. R., Oliveira, A. S., Sousa, A. S. D. S., Sousa, A. S. D. S., Martins, A. P., Veiga, A., Bernardes, B. G., Silva, B., Fernandes, A., Miranda, C., Dias, C. L. A., Neto, C. C., Castro, C. M. O., Oliveira, D. F., Rodrigues, D., Magalhães, D. D. S., Almeida, D., Castro, D., Costa, E. C. L. D., Darú, F. A., Bastos, F., Teixeira, F. D. S., Ferreira, F., Fortunato, G., Araújo-Rodrigues, H., Osorio Pérez, J. R., Silveira, J. F., Silva, J. A., Soares, J. C., Carvalho, L. C., Castro, L. M. G., Machado, M., Carvalho, M. J., Nazareth, M., Veiga, M., Coelho, M., Carvalho, M. I. P. D., Mendes, M., Ramos, M. A. M., Silva, T., Resende, T., Fontes, A. L., Neves, D. I. S. C. D., Cachetas, D. M., Silva, G. A. D. R. & Morais, R. M. S. C.
1/01/20 → 31/12/23
Project: Research