Table 2.
Class | Peptide | Source | Activity spectrum | Mechanism of action | Approval/Use | Ref |
---|---|---|---|---|---|---|
I | Gramicidin | Bacillus brevis | Gram +/− pathogens | Forms an ion channel in membranes. | Ophthalmic use as solutions/drops (1940s) | [85] |
II | Nisin | Lactococcus lactis | Gram +pathogens | Binds lipid II and inhibits cell wall synthesis. | Food preservative (1969, WHO; 1988, FDA) | [86] |
III | Bacitracin | Bacillus subtilis | Gram +/− pathogens | Inhibits cell wall and peptidoglycan synthesis. | Powder form (before 1982) | [87] |
III | Polymyxin B | Bacillus polymyxa | Gram− pathogens (e.g., P. aeruginosa) | Damages membranes | Aerosporin injection (before 1982); endotoxin removing (2003) | [88] |
III | Colistin, or polymyxin E | Paenibacillu s polymyxa | Pseudomon as and Acinetobacter sp. | Damages membranes | Suspension/drops (1982) | [89] |
III | Daptomycin | Streptomyces roseosporus. | Gram+ MRSA | Damages membranes | Treat complicated skin infection (2003, FDA). | [90] |
III | Echinocandin2 | Glarea lozoyensis; Coleophoma empedra; A. nidulans | Fungi (C. albicans) | Inhibits the synthesis of glucan and cell wall. | FDA approved | [91] |
IV | Gramicidin S | Bacillus brevis | Gram+/− pathogens | Disrupts the outer membrane. | Wound infections (1942, Soviet Union) | [92] |
I | Pexiganan (Magainin) | Xenopus laevis | Diabetic foot ulcers | Membranes | Phase III | [93] |
I | Omiganan (indolicidin) | Bos taurus | Rosacea | Membrane/DNA | Phase II | [94] |
I | OP-145 (LL-37) | Homo sapiens | Chronic middle ear infection | Membranes | Phase I/II | [94] |
I | PXL01 (lactoferricin) | Homo sapiens | Prevention of postsurgical adhesion formation | Repressing proinflammatory cytokine secretion and promoting fibrinolysis. | Phase II | [94] |
I | PAC-113 (histatin 3) | Homo sapiens | Oral candidiasis | Membranes/Inhibiting cytokine production. | Phase II | [94] |
II | Iseganan/IB-367 (protegrin-1) | Sus scrofa | Oral mucositis | Membranes | Phase III | [94] |
II | Novexatin/NP-213 (defensin) | Homo sapiens | Fungal nail infection | Membrane lysis | Phase II | [94] |
III | Iturin A (lipopeptide) | Bacillus subtilis | Fungi; G +/− bacteria | Forms ion conducting pores in membranes. | Preclinical | [95] |
III | Ramoplanin | Actinoplanes sp. ATCC 33076. | Gram+ bacteria | Inhibits cell wall synthesis. | VRE (Phase III); C. difficile (Phase II). | [96] |
III | WAP-8294A2 (Lotilibcin) | Lysobacter sp. | Gram+ bacteria (VRE and MRSA) | Interacts with membranes. | Systemic infection (Phase I/II) | [97] |
IV | Valinomycin | Streptomyces tsusimaensis; S. fulvissimus | Gram+ bacteria; Fungi (C. albicans) | Forms a K+ ion channel in membranes. | Not available | [98] |
Data from http://www.accessdata.fda.gov/scripts/cder/ob/search_product.cfm; https://clinicaltrials.gov/; https://pubchem.ncbi.nlm.nih.gov/; http://aps.unmc.edu/AP.
The FDA-approved echinocandins are seminsynthetic lipopeptides derived from caspofungin, micafungin, and anidulafungin.