Discovery of Short Peptides Exhibiting High Potency against Cryptococcus neoformans

被引：37

作者：

Mahindra, Amit ^{[1
]}

Bagra, Nitin ^{[1
]}

Wangoo, Nishima ^{[2
]}

Khan, Shabana I. ^{[3
]}

Jacob, Melissa R. ^{[3
]}

Jain, Rahul ^{[1
]}

机构：

[1] Natl Inst Pharmaceut Educ & Res, Dept Med Chem, Sect 67, Sas Nagar 160062, Punjab, India

[2] Panjab Univ, Ctr Nanosci & Nanotechnol, Sect 14, Chandigarh 160014, India

[3] Univ Mississippi, Sch Pharm, Natl Ctr Nat Prod Res, University, MS 38677 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2014年 / 5卷 / 04期

关键词：

Antifungal peptides; microwave; TEM; C; neoformans; arylation; ANTIMICROBIAL PEPTIDES; AMPHOTERICIN-B; ANTIFUNGAL; LIPOPEPTIDES; MECHANISMS; UPDATE;

D O I：

10.1021/ml500011v

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Rapid increase in the emergence of resistance against existing antifungal drugs created a need to discover new structural classes of antifungal agents. In this study we describe the synthesis of a new structural class of short antifungal peptidomimetcis, their activity, and plausible mechanism of action. The results of the study show that peptides lie and Ware more potent than the control drug amphotericin B, with no cytotoxicity to human cancer cells and noncancerous mammalian kidney cells. The selectivity of peptides to fungus is depicted by transmission electron microscopy studies, and it revealed that lie possibly disrupts the model membrane of the fungal pathogen.

引用

页码：315 / 320

页数：6

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