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1.
Bioorg Chem ; 145: 107206, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38367428

RESUMO

Photothermal therapy (PTT) has attracted extensive attention in cancer treatment. Heptamethine cyanine dyes with near-infrared (NIR) absorption performance have been investigated for PTT. However, they are often accompanied by poor photostability, suboptimal photothermal conversion and limited therapeutic efficacy. The photophysical properties of fluorescent organic salts can be tuned through counterion pairing. However, whether the counterion can influence the photostability and photothermal properties of heptamethine cyanine salts has not been clarified. In this work, we investigated the effects of eleven counter anions on the physical and photothermal properties of NIR-II heptamethine cyanine salts with the same heptamethine cyanine cation. The anions have great impacts on the physiochemical properties of dyes in solution including aggregation, photostability and photothermal conversion efficiency. The physical tuning enables the control over the cytotoxicity and phototoxicity of the dyes. The selected salts have been demonstrated to significantly suppress 4T1 breast tumor growth with low toxicity. The findings that the counterion has great effects on the photothermal properties of cationic NIR-II heptamethine cyanine dyes will provide a reference for the preparation of improved photothermal agents through counterion pairing with possible translation to humans.


Assuntos
Carbocianinas , Terapia Fototérmica , Sais , Humanos , Sais/farmacologia , Corantes/química , Ânions , Corantes Fluorescentes/farmacologia , Corantes Fluorescentes/química
2.
J Biophotonics ; 16(12): e202300193, 2023 12.
Artigo em Inglês | MEDLINE | ID: mdl-37556310

RESUMO

Colorectal cancer is a prevalent malignancy globally, often linked to chronic colitis. Terahertz technology, with its noninvasive and fingerprint spectroscopic properties, holds promise in disease diagnosis. This study aimed to explore terahertz technology's application in colitis-associated cancer using a mouse model. Mouse colorectal tissues were transformed into paraffin-embedded blocks for histopathological analysis using HE staining. Terahertz transmission spectroscopy was performed on the tissue blocks. By comparing terahertz absorption differences, specific frequency bands were identified as optimal for distinguishing cancerous and normal tissues. The study revealed that terahertz spectroscopy effectively differentiates colitis-related cancers from normal tissues. Remarkably, 1.8 THz emerged as a potential optimal frequency for diagnosing colorectal cancer in mice. This suggests the potential for rapid histopathological diagnosis of colorectal cancer using terahertz technology.


Assuntos
Neoplasias Colorretais , Espectroscopia Terahertz , Humanos , Espectroscopia Terahertz/métodos , Neoplasias Colorretais/diagnóstico
3.
Arch Pharm (Weinheim) ; 356(7): e2200673, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37160703

RESUMO

Tetrahydro-ß-carbolines (THßCs) are a kind of natural alkaloids with multiple pharmaceutical activities. Herein, a focused compound library derived from THßCs was synthesized and their anticancer activities were studied in several cancer cell lines. Among them, three compounds showed considerable anticancer activities with low micromolar to submicromolar IC50 values. The abilities to induce apoptosis and alter mitochondrial membrane potential levels, which are comparable to those of the commercial anticancer drug adriamycin, were confirmed by one representative compound (21) on the B16/F10 cell line. Our preliminary structure-activity relationship studies indicated that alkylamines with suitable lengths are very important for potency improvement.


Assuntos
Alcaloides , Antineoplásicos , Quinolinas , Relação Estrutura-Atividade , Quinolinas/farmacologia , Antineoplásicos/farmacologia , Apoptose , Alcaloides/farmacologia , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Proliferação de Células , Estrutura Molecular
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