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S-benzyldithiocarbazate imine coordinated metal complexes kill Candida albicans by causing cellular apoptosis and necrosis.
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2020-03-17 , DOI: 10.1016/j.bioorg.2020.103771
Manzoor Ahmad Malik 1 , Shabir Ahmad Lone 2 , Mohmmad Younus Wani 3 , Md Ikbal Ahmed Talukdar 1 , Ovas Ahmad Dar 1 , Aijaz Ahmad 4 , Athar Adil Hashmi 1
Affiliation  

Development of new chemotherapeutic agents and strategies are urgently needed to curb and halt the growing menace caused by hard-to-treat microbes. Coordination of metals to bioactive organic ligands is now considered to be an efficient strategy for delivering bioactive compounds inside the microbial cell membranes. Metal complexes have been effectively used to treat many dreadful diseases were other treatment modalities had failed. Use of metal complexes to treat microbial infections is now conceived to be an alternative and efficient strategy. Towards this, some new homoleptic transition metal complexes, obtained by coordination of metal ions to bioactive S-benzyldithiocarbazate Schiff-base ligands were evaluated for their anti-Candida activity and their potential to disrupt the membrane architecture. The complexes displayed remarkable antifungal activity against a wide spectrum of fluconazole susceptible and resistant Candida albicans isolates, with Ni complex (dtc3) being highly active with minimum inhibitory concentration (MIC) values ranging from 1 to 32 µg/mL. Cell viability assay confirmed the fungicidal activity of these metal complexes, especially the complex dtc3. These metal complexes kill Candida albicans by inducing cellular apoptosis and necrosis thereby causing phosphatidylserine externalization as revealed by Annexin V-FITC and propidium iodide staining assays.

中文翻译:

S-苄基二硫代氨基甲酸酯亚胺配位的金属配合物通过引起细胞凋亡和坏死杀死白色念珠菌。

迫切需要开发新的化学治疗剂和策略,以遏制和制止难以治疗的微生物所造成的日益严重的威胁。金属与生物活性有机配体的配位现在被认为是在微生物细胞膜内部递送生物活性化合物的有效策略。金属配合物已被有效地用于治疗许多可怕的疾病,而其他治疗方式均告失败。现在认为使用金属络合物治疗微生物感染是一种替代且有效的策略。为此,通过金属离子与生物活性S-苄基二硫代氨基甲酸酯席夫碱配体的配位获得了一些新的均化过渡金属络合物的抗念珠菌活性和破坏膜结构的潜力。该复合物对各种氟康唑敏感和耐药的白色念珠菌分离物均显示出显着的抗真菌活性,其中镍复合物(dtc3)具有很高的活性,最小抑菌浓度(MIC)值为1至32 µg / mL。细胞活力测定证实了这些金属配合物,特别是配合物dtc3的杀真菌活性。这些金属配合物通过诱导细胞凋亡和坏死而杀死白色念珠菌,从而引起磷脂酰丝氨酸的外在化,如膜联蛋白V-FITC和碘化丙啶染色测定所揭示的。细胞活力测定证实了这些金属配合物,特别是配合物dtc3的杀真菌活性。这些金属配合物通过诱导细胞凋亡和坏死而杀死白色念珠菌,从而引起磷脂酰丝氨酸的外在化,如膜联蛋白V-FITC和碘化丙啶染色测定所揭示的。细胞活力测定证实了这些金属配合物,特别是配合物dtc3的杀真菌活性。这些金属配合物通过诱导细胞凋亡和坏死而杀死白色念珠菌,从而引起磷脂酰丝氨酸的外在化,如膜联蛋白V-FITC和碘化丙啶染色测定所揭示的。
更新日期:2020-03-19
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