Piperidine based 1,2,3-triazolylacetamide derivatives induce cell cycle arrest and apoptotic cell death in Candida auris

金念珠菌 细胞凋亡 活力测定 最小抑制浓度 细胞周期检查点 哌啶 细胞周期 程序性细胞死亡 耳毒性 药理学 化学 抗真菌 生物 微生物学 生物化学 顺铂 立体化学 抗菌剂 遗传学 化疗
作者
Vartika Srivastava,Mohmmad Younus Wani,Abdullah S. Al‐Bogami,Aijaz Ahmad
出处
期刊:Journal of Advanced Research [Elsevier]
卷期号:29: 121-135 被引量:14
标识
DOI:10.1016/j.jare.2020.11.002
摘要

Introduction: The fungal pathogen Candida auris, is a serious threat to public health and is associated with bloodstream infections causing high mortality particularly in patients with serious medical problems. As this pathogen is generally resistant to all the available classes of antifungals, there is a constant demand for novel antifungal drugs with new mechanisms of antifungal action. Objective: Therefore, in this study we synthesised six novel piperidine based 1,2,3-triazolylacetamide derivatives (pta1-pta6) and tested their antifungal activity and mechanism of action against clinical C. auris isolates. Methods: Antifungal susceptibility testing was done to estimate MIC values of piperidine derivatives following CLSI recommended guidelines. MUSE Cell Analyzer was used to check cell viability and cell cycle arrest in C. auris after exposure to piperidine derivatives using different kits. Additionally, fluorescence microscopy was done to check the effect of test compound on C. auris membrane integrity and related apoptotic assays were performed to confirm cellular apoptosis using different apoptosis markers. Results: Out of the six derivatives; pta1, pta2 and pta3 showed highest active with MIC values from 0.24 to 0.97 μg/mL and MFC ranging from 0.97 to 3.9 μg/mL. Fungicidal behaviour of these compounds was confirmed by cell count and viability assay. Exposure to test compounds at sub-inhibitory and inhibitory concentrations resulted in disruption of C. auris plasma membrane. Further in-depth studies showed that these derivatives were able to induce apoptosis and cell cycle arrest in S-phase. Furthermore, the compounds demonstrated lower toxicity profile. Conclusion: Present study suggests that the novel derivatives (pta1-pta3) induce apoptotic cell death and cell cycle arrest in C. auris and could be potential candidates against C. auris infections.
最长约 10秒,即可获得该文献文件

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
大幅提高文件上传限制,最高150M (2024-4-1)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
海绵宝宝前列腺儿完成签到,获得积分10
16秒前
在水一方应助科研通管家采纳,获得10
31秒前
suepisode完成签到 ,获得积分10
34秒前
tmobiusx完成签到,获得积分10
35秒前
Tttttttt完成签到,获得积分10
41秒前
汉堡包应助Bgeelyu采纳,获得10
43秒前
51秒前
Bgeelyu完成签到,获得积分10
53秒前
Bgeelyu发布了新的文献求助10
56秒前
croissante完成签到 ,获得积分10
1分钟前
Ding完成签到,获得积分10
1分钟前
btcat完成签到,获得积分10
1分钟前
寒冷的断秋发布了新的文献求助150
1分钟前
沙里飞完成签到 ,获得积分10
1分钟前
是我呀小夏完成签到 ,获得积分10
1分钟前
lvvvvvv完成签到,获得积分10
2分钟前
cyskdsn完成签到 ,获得积分10
2分钟前
铜豌豆完成签到 ,获得积分10
2分钟前
Hank完成签到 ,获得积分10
2分钟前
张亮完成签到 ,获得积分10
2分钟前
Singularity应助科研通管家采纳,获得30
2分钟前
Singularity应助科研通管家采纳,获得30
2分钟前
joeqin完成签到,获得积分10
2分钟前
maggiexjl完成签到,获得积分10
2分钟前
小杨完成签到 ,获得积分10
3分钟前
搜集达人应助夏添采纳,获得10
3分钟前
慧喆完成签到 ,获得积分10
3分钟前
可靠谷蓝完成签到 ,获得积分10
3分钟前
木光完成签到,获得积分20
3分钟前
太拗口哟完成签到,获得积分10
3分钟前
3分钟前
六等于三二一完成签到 ,获得积分10
4分钟前
榆木小鸟完成签到 ,获得积分10
4分钟前
任性星星完成签到 ,获得积分10
4分钟前
lyk完成签到 ,获得积分10
4分钟前
123完成签到 ,获得积分10
4分钟前
李浅墨完成签到 ,获得积分10
4分钟前
WLX001完成签到 ,获得积分10
4分钟前
Singularity应助科研通管家采纳,获得10
4分钟前
小马甲应助科研通管家采纳,获得10
4分钟前
高分求助中
Sustainability in Tides Chemistry 2800
The Young builders of New china : the visit of the delegation of the WFDY to the Chinese People's Republic 1000
Rechtsphilosophie 1000
Bayesian Models of Cognition:Reverse Engineering the Mind 888
Defense against predation 800
Very-high-order BVD Schemes Using β-variable THINC Method 568
Chen Hansheng: China’s Last Romantic Revolutionary 500
热门求助领域 (近24小时)
化学 医学 生物 材料科学 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 基因 遗传学 催化作用 物理化学 免疫学 量子力学 细胞生物学
热门帖子
关注 科研通微信公众号,转发送积分 3137039
求助须知:如何正确求助?哪些是违规求助? 2788025
关于积分的说明 7784284
捐赠科研通 2444088
什么是DOI,文献DOI怎么找? 1299724
科研通“疑难数据库(出版商)”最低求助积分说明 625536
版权声明 601010