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-(2-溴苯基)-2-羟基苯甲酰胺衍生物及其包合物的抗菌和抗炎活性

Antimicrobial and Anti-Inflammatory Activity of -(2-Bromo-phenyl)-2-hydroxy-benzamide Derivatives and Their Inclusion Complexes.

作者信息

Ienașcu Ioana Maria Carmen, Căta Adina, Lazăr Antonina Evelina, Țolea Nick Samuel, Rusu Gerlinde, Sfîrloagă Paula, Moşoarcă Cristina, Chiș Adriana Aurelia, Morgovan Claudiu, Danciu Corina, Muntean Delia, Popescu Iuliana, Pop Raluca

机构信息

National Institute of Research and Development for Electrochemistry and Condensed Matter, 144 Dr. A. P. Podeanu, 300569 Timişoara, Romania.

Department of Pharmaceutical Sciences, Faculty of Pharmacy, "Vasile Goldiş" Western University of Arad, 86 Liviu Rebreanu, 310045 Arad, Romania.

出版信息

Pharmaceutics. 2025 Jul 2;17(7):869. doi: 10.3390/pharmaceutics17070869.

DOI:10.3390/pharmaceutics17070869
PMID:40733078
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12300325/
Abstract

: In order to enhance the biological activity, novel complexes of -(2-bromo-phenyl)-2-hydroxy-benzamide derivatives and β-cyclodextrin were obtained. : The inclusion complexes were characterized using spectral and thermal analyses. The antimicrobial activity was determined using the disk diffusion agar method, and completed with the minimum inhibitory concentration (MIC) values obtained by the broth microdilution method. The in vitro anti-inflammatory activity was evaluated using the protease inhibition assay. : The computed supramolecular architectures of the inclusion complexes showed that the most stable molecular arrangements correspond to the models in which the -(2-bromo-phenyl)-2-hydroxy-benzamide derivatives are partially included in the cyclodextrin cavity. The antimicrobial screening showed that the compounds were active against Gram-positive bacteria (MIC = 2.5-5.0 mg/mL). Also, the evaluation of the proteinase inhibitory activity showed that the IC values of the title compounds (0.04-0.07 mg/mL) were much lower than that of the acetylsalicylic acid (0.4051 ± 0.0026 mg/mL) used as positive control, proving their superior efficiency in inhibiting trypsin activity. : The complexation proved to be beneficial for both antimicrobial and anti-inflammatory effects.

摘要

为了提高生物活性,制备了新型的α-(2-溴苯基)-2-羟基苯甲酰胺衍生物与β-环糊精的复合物。采用光谱和热分析对包合物进行了表征。采用纸片扩散琼脂法测定抗菌活性,并用肉汤微量稀释法获得的最低抑菌浓度(MIC)值进行补充。采用蛋白酶抑制试验评价体外抗炎活性。计算得到的包合物超分子结构表明,最稳定的分子排列对应于α-(2-溴苯基)-2-羟基苯甲酰胺衍生物部分包合在环糊精腔内的模型。抗菌筛选表明,这些化合物对革兰氏阳性菌有活性(MIC = 2.5 - 5.0 mg/mL)。此外,蛋白酶抑制活性评价表明,标题化合物的IC值(0.04 - 0.07 mg/mL)远低于用作阳性对照的乙酰水杨酸(0.4051 ± 0.0026 mg/mL),证明其在抑制胰蛋白酶活性方面具有更高的效率。结果表明,络合作用对抗菌和抗炎作用均有益。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/3afbe9215ecd/pharmaceutics-17-00869-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/fa7b625d74d1/pharmaceutics-17-00869-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/7b5e1e8a0c66/pharmaceutics-17-00869-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/c42528ee31db/pharmaceutics-17-00869-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/37686f8b3b7c/pharmaceutics-17-00869-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/c67fd64849f5/pharmaceutics-17-00869-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/5d34607c7098/pharmaceutics-17-00869-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/5c037c19a649/pharmaceutics-17-00869-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/09938ce904fc/pharmaceutics-17-00869-g008a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/a72fba262655/pharmaceutics-17-00869-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/d3614d341020/pharmaceutics-17-00869-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/d1aad2ff5f76/pharmaceutics-17-00869-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/2a02104e3af6/pharmaceutics-17-00869-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/3afbe9215ecd/pharmaceutics-17-00869-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/fa7b625d74d1/pharmaceutics-17-00869-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/7b5e1e8a0c66/pharmaceutics-17-00869-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/c42528ee31db/pharmaceutics-17-00869-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/37686f8b3b7c/pharmaceutics-17-00869-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/c67fd64849f5/pharmaceutics-17-00869-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/5d34607c7098/pharmaceutics-17-00869-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/5c037c19a649/pharmaceutics-17-00869-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/09938ce904fc/pharmaceutics-17-00869-g008a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/a72fba262655/pharmaceutics-17-00869-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/d3614d341020/pharmaceutics-17-00869-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/d1aad2ff5f76/pharmaceutics-17-00869-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/2a02104e3af6/pharmaceutics-17-00869-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8a62/12300325/3afbe9215ecd/pharmaceutics-17-00869-g013.jpg

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