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Your search keyword '"Márcia Campos Aguiar"' showing total 3 results
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3 results on '"Márcia Campos Aguiar"'

1. Ring-Fused meso-Tetraarylchlorins as Auspicious PDT Sensitizers: Synthesis, Structural Characterization, Photophysics, and Biological Evaluation

Author

Mafalda Laranjo, Nelson A. M. Pereira, Andreia S. R. Oliveira, Márcia Campos Aguiar, Gonçalo Brites, Bruno F. O. Nascimento, Beatriz Serambeque, Bruna D. P. Costa, João Pina, J. Sérgio Seixas de Melo, Marta Pineiro, M. Filomena Botelho, and Teresa M. V. D. Pinho e Melo

Subjects
chlorins, photodynamic therapy, photosensitizer, subcellular accumulation, cancer, Chemistry, QD1-999
Abstract

Novel 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-fused meso-tetraarylchlorins, with different degrees of hydrophilicity (with methyl ester, hydroxymethyl, and carboxylic acid moieties), have been synthesized and their photophysical characterization as well as in vitro photocytotoxicity assessment against human melanoma and esophageal and bladder carcinomas was carried out. An integrated analysis of the photosensitizers’ performance, considering the singlet oxygen generation data, cell internalization, and intracellular localization, allowed to establish relevant structure-photoactivity relationships and the rationalization of the observed photocytotoxicity. In the diacid and monoalcohol series, chlorins derived from meso-tetraphenylporphyrin proved to be the most efficient photodynamic therapy agents, showing IC50 values of 68 and 344 nM against A375 cells, respectively. These compounds were less active against OE19 and HT1376 cells, the diacid chlorin with IC50 values still in the nano-molar range, whereas the monohydroxymethyl-chlorin showed significantly higher IC50 values. The lead di(hydroxymethyl)-substituted meso-tetraphenylchlorin confirmed its remarkable photoactivity with IC50 values below 75 nM against the studied cancer cell lines. Subcellular accumulation of this chlorin in the mitochondria, endoplasmic reticulum, and plasma membrane was demonstrated.

Published
2022
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2. Ring-Fused

Author

Mafalda, Laranjo, Nelson A M, Pereira, Andreia S R, Oliveira, Márcia, Campos Aguiar, Gonçalo, Brites, Bruno F O, Nascimento, Beatriz, Serambeque, Bruna D P, Costa, João, Pina, J Sérgio, Seixas de Melo, Marta, Pineiro, M Filomena, Botelho, and Teresa M V D, Pinho E Melo

Abstract

Novel 4,5,6,7-tetrahydropyrazolo[1,5

Published
2022

3. Platinum(II) ring-fused chlorins as efficient theranostic agents: Dyes for tumor-imaging and photodynamic therapy of cancer

Author

Ana Cristina Gonçalves, Marta Pineiro, Gonçalo Brites, Maria Filomena Botelho, Ana Bela Sarmento-Ribeiro, Bruno F.O. Nascimento, Mafalda Laranjo, Teresa M. V. D. Pinho e Melo, Nelson A. M. Pereira, João Casalta-Lopes, Ana Brito, and Márcia Campos Aguiar

Subjects
Esophageal Neoplasms, medicine.medical_treatment, Photodynamic therapy, 01 natural sciences, Optical imaging, chemistry.chemical_compound, Coordination Complexes, Drug Discovery, polycyclic compounds, Hydroxymethyl, Cytotoxicity, Melanoma, Luminescence imaging, 0303 health sciences, Molecular Structure, Optical Imaging, General Medicine, Animal models, Porphyrins, chemistry.chemical_element, Antineoplastic Agents, Ring (chemistry), Photosensitizers, Structure-Activity Relationship, 03 medical and health sciences, Pt(II) chlorins, Cell Line, Tumor, medicine, Humans, Cell Proliferation, Fluorescent Dyes, Platinum, 030304 developmental biology, Pharmacology, Dose-Response Relationship, Drug, 010405 organic chemistry, Bladder carcinoma, Organic Chemistry, Cancer, Theranostics, medicine.disease, Combinatorial chemistry, 0104 chemical sciences, Oesophageal carcinoma, Photochemotherapy, Urinary Bladder Neoplasms, chemistry, Chlorin, Drug Screening Assays, Antitumor
Abstract

The discovery of Pt-chlorin-type theranostic agents is described. Luminescent Pt(II) 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-fused chlorins, with different degrees of hydrophilicity, have been synthesized and their in vitro photocytotoxicity against human melanoma, oesophageal and bladder carcinomas was studied. A di(hydroxymethyl)-substituted chlorin was identified as a privileged molecule to explore imaging-guided photodynamic therapy. In addition to the high activity as PDT agent and absence of cytotoxicity per se, this molecule showed the ideal photophysical and photochemical properties. In vivo studies using a A375 melanoma mouse model, proved the extraordinary properties of this chlorin as a luminescent probe and the ability to impair tumor growth, making image guided treatment and follow up a possibility.

Published
2020
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