Actinomycetes Bioprospecting Lab, Centre for Research in Infectious Diseases (CRID), School of Chemical and Biotechnology, SASTRA University, Tirumalaisamudram, Thanjavur, Tamilnadu, 613401, India.
Department of Chemistry, School of Chemical and Biotechnology, SASTRA University, Tirumalaisamudram, Thanjavur, Tamilnadu, 613401, India.
Sci Rep. 2017 Nov 13;7(1):15400. doi: 10.1038/s41598-017-15500-8.
Cryptococcus neoformans infection is quite complex with both host-pathogen interaction and host immune profile determining disease progress and therapeutic outcome. Hence in the present study, the potential utility of (E)-5-benzylidenedihydrofuran-2(3 H)-one (compound-6) was explored as an effective anticryptococcal compound with immunomodulatory potential. The efficacy of compound-6 in pulmonary cryptococosis model using H99 strain was investigated. The effective dose was found to provide 100% survival, with a significant reduction of yeast burden in lungs and brain. The biodistribution analysis provided evidence for the presence of higher concentration of compound-6 in major organs including lungs and brain. In addition, compound-6 treated mice had significantly higher expression of IL-6, IL-4 and IFN-γ in lung and brain. Similarly, elevated expression of TNF-α, IL-β1 and IL-12 were observed in lungs, suggesting the protective host response against C. neoformans. The reduction and clearance of fungal load in systemic organs and mouse survival are notable results to confirm the ability of compound-6 to treat cryptococcosis. In conclusion, the low molecular weight (174 Da), lipophilicity, its ability to cross blood brain barrier, and facilitating modulation of cytokine expression are the added advantages of compound-6 to combat against disseminated cryptococosis.
新型隐球菌感染非常复杂,宿主-病原体相互作用和宿主免疫谱决定疾病的进展和治疗结果。因此,在本研究中,探索了(E)-5-亚苄基二氢呋喃-2(3H)-酮(化合物 6)作为具有免疫调节潜力的有效抗隐球菌化合物的潜在用途。使用 H99 株研究了化合物 6 在肺部隐球菌病模型中的疗效。发现有效剂量可提供 100%的存活率,并显著降低肺部和脑部的酵母负荷。生物分布分析为化合物 6 在包括肺和脑在内的主要器官中存在更高浓度提供了证据。此外,化合物 6 处理的小鼠在肺和脑中具有显著更高水平的 IL-6、IL-4 和 IFN-γ 表达。同样,在肺部观察到 TNF-α、IL-β1 和 IL-12 的表达升高,表明宿主对新型隐球菌有保护反应。系统器官中真菌负荷的减少和清除以及小鼠的存活率是显著的结果,证实了化合物 6 治疗隐球菌病的能力。总之,低分子量(174Da)、亲脂性、穿过血脑屏障的能力以及促进细胞因子表达的调节是化合物 6 对抗播散性隐球菌病的附加优势。