The antimicrobial peptides LL-37, KR-20, FK-13 and KR-12 inhibit the growth of a sensitive and a metronidazole-resistant strain of Trichomonas vaginalis

Article

作者: Ramírez-Ledesma, María G ; Rodríguez, Mayra C ; Avila, Eva E ; Alva-Murillo, Nayeli

The parasite Trichomonas vaginalis is the aetiologic agent of trichomoniasis, the most common non-viral sexually transmitted disease worldwide. This infection often remains asymptomatic and is related to several health complications. The traditional treatment for trichomoniasis uses drugs of the 5-nitroimidazole family, such as metronidazole; however, scientific reports indicate an increasing number of drug-resistant strains. Antimicrobial peptides could be an alternative or complementary treatment. In this sense, one attractive candidate is the human cathelicidin, being LL-37 its active form. LL-37 possesses microbicidal activity against many microorganisms such as bacteria, Candida albicans, and Entamoeba histolytica. Shorter sequences derived from this peptide, such as KR-20, FK-13 and KR-12, have been shown to possess a higher microbicidal effect than LL-37. In this study, we determined the activity of LL-37 and its derivatives against T. vaginalis, which was unknown. The results showed that the four peptides (LL-37, KR-20, FK-13-NH₂ and KR-12) decreased the viability of T. vaginalis on a 5-nitroimidazole-sensitive and a 5-nitroimidazole-resistant strain; however, KR-20 was the most effective peptide, followed by FK-13-NH₂. Low concentrations of all peptides showed a better effect when combined with metronidazole in the sensitive and resistant T. vaginalis strains. These results are promising for potential future therapeutic uses.

2019-08-01·Journal of Cardiovascular Translational Research3区 · 医学

KC21 Peptide Inhibits Angiogenesis and Attenuates Hypoxia-Induced Retinopathy

3区 · 医学

Article

作者: Wu, Yih-Jer ; Yeh, Hung-I ; Chen, Chun-Wei ; Chen, Min-Che ; Wang, Shin-Wei ; Su, Cheng-Huang ; Tien, Ting Yi ; Lu, Chi-Sheng ; Wang, Bo-Jeng ; Hsieh, Chin-Ling ; Lee, Yi-Nan

Desmogleins (Dsg2) are the major components of desmosomes. Dsg2 has five extracellular tandem cadherin domains (EC1-EC5) for cell-cell interaction. We had previously confirmed the Dsg2 antibody and its epitope (named KC21) derived from EC2 domain suppressing epithelial-mesenchymal transition and invasion in human cancer cell lines. Here, we screened six peptide fragments derived from EC2 domain and found that KR20, the parental peptide of KC21, was the most potent one on suppressing endothelial colony-forming cell (ECFC) tube-like structure formation. KC21 peptide also attenuated migration but did not disrupt viability and proliferation of ECFCs, consistent with the function to inhibit VEGF-mediated activation of p38 MAPK but not AKT and ERK. Animal studies showed that KC21 peptides suppressed capillary growth in Matrigel implant assay and inhibited oxygen-induced retinal neovascularization. The effects were comparable to bevacizumab (Bev). In conclusion, KC21 peptide is an angiogenic inhibitor potentially useful for treating angiogenesis-related diseases.

2014-09-01·Antimicrobial Agents and Chemotherapy2区 · 医学

Derivatives of the Mouse Cathelicidin-Related Antimicrobial Peptide (CRAMP) Inhibit Fungal and Bacterial Biofilm Formation

2区 · 医学

Article

作者: Thevissen, Karin ; Dovgan, Barbara ; Cammue, Bruno P. A. ; Fröhlich, Mirjam ; Robijns, Stijn ; Steenackers, Hans ; Verstraeten, Natalie ; Luyten, Walter ; De Brucker, Katrijn ; Vanderleyden, Jos ; Michiels, Jan ; Delattin, Nicolas ; Landuyt, Bart ; Schoofs, Liliane

ABSTRACT We identified a 26-amino-acid truncated form of the 34-amino-acid cathelicidin-related antimicrobial peptide (CRAMP) in the islets of Langerhans of the murine pancreas. This peptide, P318, shares 67% identity with the LL-37 human antimicrobial peptide. As LL-37 displays antimicrobial and antibiofilm activity, we tested antifungal and antibiofilm activity of P318 against the fungal pathogen Candida albicans . P318 shows biofilm-specific activity as it inhibits C. albicans biofilm formation at 0.15 μM without affecting planktonic survival at that concentration. Next, we tested the C. albicans biofilm-inhibitory activity of a series of truncated and alanine-substituted derivatives of P318. Based on the biofilm-inhibitory activity of these derivatives and the length of the peptides, we decided to synthesize the shortened alanine-substituted peptide at position 10 (AS10; KLKKIAQKIKNFFQKLVP). AS10 inhibited C. albicans biofilm formation at 0.22 μM and acted synergistically with amphotericin B and caspofungin against mature biofilms. AS10 also inhibited biofilm formation of different bacteria as well as of fungi and bacteria in a mixed biofilm. In addition, AS10 does not affect the viability or functionality of different cell types involved in osseointegration of an implant, pointing to the potential of AS10 for further development as a lead peptide to coat implants.

100 项与 KR20 相关的药物交易

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