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轴向二取代硅(IV)酞菁作为用于抗菌和抗癌光动力及声动力疗法的强效敏化剂

Axially Disubstituted Silicon(IV) Phthalocyanine as a Potent Sensitizer for Antimicrobial and Anticancer Photo and Sonodynamic Therapy.

作者信息

Wysocki Marcin, Ziental Daniel, Biyiklioglu Zekeriya, Jozkowiak Malgorzata, Dlugaszewska Jolanta, Piotrowska-Kempisty Hanna, Güzel Emre, Sobotta Lukasz

机构信息

Chair and Department of Inorganic and Analytical Chemistry, Poznan University of Medical Sciences, Rokietnicka 3, 60-806 Poznan, Poland.

Doctoral School, Poznan University of Medical Sciences, Bukowska 70, 60-812 Poznan, Poland.

出版信息

Int J Mol Sci. 2025 Aug 1;26(15):7447. doi: 10.3390/ijms26157447.

DOI:10.3390/ijms26157447
PMID:40806575
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12347415/
Abstract

The unique properties of phthalocyanines (Pcs), such as strong absorption, high photostability, effective singlet oxygen generation, low toxicity and biocompatibility, versatile chemical modifications, broad spectrum of antimicrobial activity, and synergistic effects with other treatment modalities, make them a preferred superior sensitizer in the field of antimicrobial photodynamic therapy. The photodynamic and sonodynamic activity of 3-(3-(diethylamino)phenoxy)propanoxy substituted silicon(IV) Pc were evaluated against bacteria and cancer cells. Stability and singlet oxygen generation upon light irradiation and ultrasound (1 MHz, 3 W) were assessed with 1,3-diphenylisobenzofuran. The phthalocyanine revealed high photostability in DMF and DMSO, although the singlet oxygen yields under light irradiation were low. On the other hand, the phthalocyanine revealed excellent sonostability and caused a high rate of DPBF degradation upon excitation by ultrasounds at 1 MHz. The silicon phthalocyanine presented significant bacterial reduction growth, up to 5 log against MRSA and upon light excitation, whereas the sonodynamic effect was negligible. The phthalocyanine revealed high activity in both photodynamic and sonodynamic manner toward hypopharyngeal tumor (FaDu, 95% and 42% reduction, respectively) and squamous cell carcinoma (SCC-25, 96% and 62% reduction, respectively). The sensitizer showed ca. 30% aldehyde dehydrogenase inhibition in various concentrations and up to 85% platelet-activating factor acetylhydrolase for 0.25 μM, while protease-activated protein C was stimulated up to 66% for 0.75 μM.

摘要

酞菁(Pcs)具有独特的性质,如强吸收性、高光稳定性、有效的单线态氧生成能力、低毒性和生物相容性、多样的化学修饰、广谱抗菌活性以及与其他治疗方式的协同效应,使其成为抗菌光动力疗法领域中首选的优质敏化剂。评估了3-(3-(二乙氨基)苯氧基)丙氧基取代的硅(IV)酞菁对细菌和癌细胞的光动力和声动力活性。用1,3-二苯基异苯并呋喃评估光照和超声(1MHz,3W)照射下的稳定性和单线态氧生成情况。该酞菁在N,N-二甲基甲酰胺和二甲基亚砜中显示出高光稳定性,尽管光照下的单线态氧产率较低。另一方面,该酞菁显示出优异的声稳定性,在1MHz超声激发下导致二苯基苯并呋喃的降解率很高。该硅酞菁在光照激发下对耐甲氧西林金黄色葡萄球菌呈现出显著的细菌生长抑制,高达5个对数级,而声动力效应可忽略不计。该酞菁在光动力和声动力方面对下咽肿瘤(FaDu细胞,分别减少95%和42%)和鳞状细胞癌(SCC-25细胞,分别减少96%和62%)均显示出高活性。该敏化剂在不同浓度下显示约30%的醛脱氢酶抑制作用,对于0.25μM的浓度,血小板活化因子乙酰水解酶的抑制率高达85%,而对于0.75μM的浓度,蛋白酶激活蛋白C的刺激率高达66%。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df82/12347415/b4255b251405/ijms-26-07447-g006.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df82/12347415/705c7789755e/ijms-26-07447-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df82/12347415/797c4950ce7a/ijms-26-07447-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/df82/12347415/98ec0a452177/ijms-26-07447-g003.jpg
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Eur J Med Chem. 2025 Mar 5;285:117214. doi: 10.1016/j.ejmech.2024.117214. Epub 2024 Dec 27.
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Non-peripheral octasubstituted zinc(II) phthalocyanines bearing pyridinepropoxy substituents - Antibacterial, anticancer photodynamic and sonodynamic activity.带有吡啶丙氧基取代基的非外围八取代锌(II)酞菁 - 抗菌、抗癌光动力和声动力活性。
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Arginine mediated photodynamic therapy with silicon(IV) phthalocyanine photosensitizers.
精氨酸介导的含硅四氮杂卟啉光敏剂光动力疗法。
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Photodynamic inactivation of pathogenic Gram-negative and Gram-positive bacteria mediated by Si(IV) phthalocyanines bearing axial ammonium units.轴向季铵盐取代的 Si(IV)酞菁光动力灭活致病性革兰氏阴性和革兰氏阳性菌
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