Bioassay-Guided Procedure Coupled with HR-ESIMS Dereplication for Isolation of Antiproliferative Bromo-Tyramine Derivative from .
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| Format: | Artículo científico |
| Sprache: | en |
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Marine drugs
2025
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| author | Esposito, Germana Ponticelli, Maria Milella, Luigi Lela, Ludovica Teta, Roberta Pawlik, Joseph R Russo, Daniela Costantino, Valeria |
| author_facet | Esposito, Germana Ponticelli, Maria Milella, Luigi Lela, Ludovica Teta, Roberta Pawlik, Joseph R Russo, Daniela Costantino, Valeria Esposito, Germana Ponticelli, Maria Milella, Luigi Lela, Ludovica Teta, Roberta Pawlik, Joseph R Russo, Daniela Costantino, Valeria |
| collection | PubMed - marine biology |
| contents | Bioassay-Guided Procedure Coupled with HR-ESIMS Dereplication for Isolation of Antiproliferative Bromo-Tyramine Derivative from . Esposito, Germana Ponticelli, Maria Milella, Luigi Lela, Ludovica Teta, Roberta Pawlik, Joseph R Russo, Daniela Costantino, Valeria Humans Hep G2 Cells Cell Proliferation Apoptosis Antineoplastic Agents Tyramine Animals Biological Assay Spectrometry, Mass, Electrospray Ionization The marine environment is vital for sustaining life on Earth and offers a significant, untapped source of bioresources that could enhance the blue economy. The present investigation used our protocol to quickly identify bioactive molecules in organic extracts. This procedure combines a bioassay-guided approach with the dereplication of mass data through bioinformatic analysis. This approach identified the compound ,,-trimethyl-3,5-dibromotyramine, a bromo-tyramine analog that showed promising antiproliferative activity on HepG2 cell lines, with an IC value of 37.49 ± 1.94 μg/mL after 24 h. Furthermore, the evaluation of related gene expression confirmed the mechanism of cell death to be apoptosis. ,,-trimethyl-3,5-dibromotyramine increased the expression of pro-apoptotic -cell lymphoma 2-associated X protein (BAX) and Poly (ADP-ribose) polymerase (PARP-1) cleavage (c-PARP-1) and downregulated the anti-apoptotic β-cell lymphoma 2 (BCL-2) and phospho-Akt (p-AKT). This report presents ,,-trimethyl-3,5-dibromotyramine from and its antiproliferative activity against the HepG2 cell line. |
| format | Artículo científico |
| id | pubmed_40422777 |
| institution | PubMed |
| language | en |
| publishDate | 2025 |
| publisher | Marine drugs |
| record_format | pubmed |
| spellingShingle | Bioassay-Guided Procedure Coupled with HR-ESIMS Dereplication for Isolation of Antiproliferative Bromo-Tyramine Derivative from . Esposito, Germana Ponticelli, Maria Milella, Luigi Lela, Ludovica Teta, Roberta Pawlik, Joseph R Russo, Daniela Costantino, Valeria Humans Hep G2 Cells Cell Proliferation Apoptosis Antineoplastic Agents Tyramine Animals Biological Assay Spectrometry, Mass, Electrospray Ionization Bioassay-Guided Procedure Coupled with HR-ESIMS Dereplication for Isolation of Antiproliferative Bromo-Tyramine Derivative from . Esposito, Germana Ponticelli, Maria Milella, Luigi Lela, Ludovica Teta, Roberta Pawlik, Joseph R Russo, Daniela Costantino, Valeria Humans Hep G2 Cells Cell Proliferation Apoptosis Antineoplastic Agents Tyramine Animals Biological Assay Spectrometry, Mass, Electrospray Ionization The marine environment is vital for sustaining life on Earth and offers a significant, untapped source of bioresources that could enhance the blue economy. The present investigation used our protocol to quickly identify bioactive molecules in organic extracts. This procedure combines a bioassay-guided approach with the dereplication of mass data through bioinformatic analysis. This approach identified the compound ,,-trimethyl-3,5-dibromotyramine, a bromo-tyramine analog that showed promising antiproliferative activity on HepG2 cell lines, with an IC value of 37.49 ± 1.94 μg/mL after 24 h. Furthermore, the evaluation of related gene expression confirmed the mechanism of cell death to be apoptosis. ,,-trimethyl-3,5-dibromotyramine increased the expression of pro-apoptotic -cell lymphoma 2-associated X protein (BAX) and Poly (ADP-ribose) polymerase (PARP-1) cleavage (c-PARP-1) and downregulated the anti-apoptotic β-cell lymphoma 2 (BCL-2) and phospho-Akt (p-AKT). This report presents ,,-trimethyl-3,5-dibromotyramine from and its antiproliferative activity against the HepG2 cell line. |
| title | Bioassay-Guided Procedure Coupled with HR-ESIMS Dereplication for Isolation of Antiproliferative Bromo-Tyramine Derivative from . |
| topic | Humans Hep G2 Cells Cell Proliferation Apoptosis Antineoplastic Agents Tyramine Animals Biological Assay Spectrometry, Mass, Electrospray Ionization |
| url | https://pubmed.ncbi.nlm.nih.gov/40422777/ |