Selected N-Terpenyl Organoselenium Compounds Possess Antimycotic Activity In Vitro and in a Mouse Model of Vulvovaginal Candidiasis.
Selected N-Terpenyl Organoselenium Compounds Possess Antimycotic Activity In Vitro and in a Mouse Model of Vulvovaginal Candidiasis.
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选定的N-替苯基有细胞烯化合物在体外和小鼠外阴阴道念珠菌病模型中具有抗菌毛活性。
DOI：
10.3390/molecules28217377
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发表时间：
2023-10-31
期刊：
影响因子：
--
通讯作者：
Billack B
中科院分区：
文献类型：
--
作者：
Liang X;Pacuła-Miszewska AJ;Obieziurska-Fabisiak M;Vartak R;Mao G;Patel K;Fedosova NU;Ścianowski J;Billack B
本工作通过测定一系列N-萜基有机硒化合物（CHB 1 -6）对氟康唑敏感株（S1）和耐药株（S2）的最小抑菌浓度（MIC），评价了它们的抗真菌活性。白色念珠菌）。MIC筛选中最具活性的化合物是CHB 4和CHB 6，然后评估其在人宫颈癌细胞（KB-3-1）中的细胞毒性，发现其对真菌具有选择性。接下来，使用重建的3D人表皮研究CHB 4和CHB 6的皮肤刺激性，并且认为这两种化合物对表皮是安全的。使用外阴阴道念珠菌病（VVC）的小鼠模型，CHB 4和CHB 6都通过减少阴道的酵母菌定植、减轻对阴道粘膜的损伤和减少组织中髓过氧化物酶（MPO）表达的丰度而表现出抗霉菌功效，表明炎症反应减少。总之，CHB 4和CHB 6在体外和小鼠VVC模型中表现出抗真菌活性，代表了两种新的有前途的抗真菌剂。
In the present work, a series of N-terpenyl organoselenium compounds (CHB1-6) were evaluated for antimycotic activity by determining the minimum inhibitory concentration (MIC) for each compound in fluconazole (FLU)-sensitive (S1) and FLU-resistant (S2) strains of Candida albicans (C. albicans). The most active compounds in the MIC screen were CHB4 and CHB6, which were then evaluated for cytotoxicity in human cervical cancer cells (KB-3-1) and found to be selective for fungi. Next, CHB4 and CHB6 were investigated for skin irritation using a reconstructed 3D human epidermis and both compounds were considered safe to the epidermis. Using a mouse model of vulvovaginal candidiasis (VVC), CHB4 and CHB6 both exhibited antimycotic efficacy by reducing yeast colonization of the vaginal tract, alleviating injury to the vaginal mucosa, and decreasing the abundance of myeloperoxidase (MPO) expression in the tissue, indicating a reduced inflammatory response. In conclusion, CHB4 and CHB6 demonstrate antifungal activity in vitro and in the mouse model of VVC and represent two new promising antifungal agents.
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影响因子：
5.6
作者：
Mal'tseva VN;Goltyaev MV;Turovsky EA;Varlamova EG
通讯作者：
Varlamova EG
影响因子：
3.5
作者：
Pacula, Agata J.;Kaczor, Katarzyna B.;Scianowski, Jacek
通讯作者：
Scianowski, Jacek
影响因子：
14.3
作者：
Garland, Megan;Hryckowian, Andrew J.;Bogyo, Matthew
通讯作者：
Bogyo, Matthew
DOI：
10.1016/j.nano.2021.102428
发表时间：
2021-07-28
影响因子：
5.4
作者：
Menon, Suvidha;Vartak, Richa;Billack, Blase
通讯作者：
Billack, Blase
影响因子：
5.4
作者：
Menon S;Liang X;Vartak R;Patel K;Di Stefano A;Cacciatore I;Marinelli L;Billack B
通讯作者：
Billack B