Enhanced antimicrobial activity of novel synthetic peptides derived from vejovine and hadrurin

Sánchez-Vásquez, Lorenzo; Silva-Sánchez, Jesús; Jiménez-Vargas, Juana María; Rodrı́guez-Romero, Adela; Muñóz-Garay, Carlos; Rodrı́guez, Marı́a C.; Gurrola, Georgina B.; Possani, Lourival D.

doi:10.1016/j.bbagen.2013.01.028

Cited by 27 publications

(24 citation statements)

References 52 publications

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“…Recently, using a rational approach, several variants were designed using vejovine and its homolog hadrurin as templates, with the aim of improving their antimicrobial and hemolytic properties. Indeed, the variants resulted more potent than the parental peptides against the same Gram-negative multidrug resistant strains (with MICs of 0.8e25 mM), and also less hemolytic (HC 50 up to 900 mM), which represents a dramatic improvement in their therapeutic indexes (Sanchez-Vasquez et al, 2013). This work constitutes an encouraging example of the results that can be achieved by the rational design of novel prospective antimicrobial peptides with potential clinical applications using the natural scorpion AMPs as scaffolds.…”

Section: Antibacterial Peptidesmentioning

confidence: 69%

“…The other report involved the above-mentioned AMPs derived from vejovine and hadrurin, which displayed antibacterial activity. When their antimalarial activity was tested, the results showed that some of the designed variants inhibited the formation of ookinetes from P. berghei by 40% at 5 mM, doubling this percentage when the concentration was increased to 25 mM (Sanchez-Vasquez et al, 2013).…”

Section: Antimalarial Peptidesmentioning

confidence: 99%

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Scorpion venom components as potential candidates for drug development

Ortíz

Gurrola

Schwartz

et al. 2015

Toxicon

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268

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Scorpions are well known for their dangerous stings that can result in severe consequences for human beings, including death. Neurotoxins present in their venoms are responsible for their toxicity. Due to their medical relevance, toxins have been the driving force in the scorpion natural compounds research field. On the other hand, for thousands of years, scorpions and their venoms have been applied in traditional medicine, mainly in Asia and Africa. With the remarkable growth in the number of characterized scorpion venom components, several drug candidates have been found with the potential to tackle many of the emerging global medical threats. Scorpions have become a valuable source of biologically active molecules, from novel antibiotics to potential anticancer therapeutics. Other venom components have drawn attention as useful scaffolds for the development of drugs. This review summarizes the most promising candidates for drug development that have been isolated from scorpion venoms.

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Section: Antibacterial Peptidesmentioning

confidence: 69%

Section: Antimalarial Peptidesmentioning

confidence: 99%

Scorpion venom components as potential candidates for drug development

Ortíz

Gurrola

Schwartz

et al. 2015

Toxicon

Self Cite

268

218

View full text Add to dashboard Cite

show abstract

“…To make cationic α‐helical AMPs useful as therapeutic agents against human pathogens, they must have both high antimicrobial potency and the ability to distinguish microbial cells from mammalian cells on the basis of their different membrane lipid compositions. Thus, AMPs displaying low or no hemolytic activity would be potent candidates for use as therapeutic agents …”

Section: Introductionmentioning

confidence: 99%

Effect of alanine, leucine, and arginine substitution on antimicrobial activity against candida albicans and action mechanism of a cationic octadecapeptide derived from α‐amylase of rice

et al. 2016

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AmyI-1-18, an antimicrobial peptide, is a cationic α-helical octadecapeptide derived from α-amylase of rice (Oryza sativa L. japonica) that contains four cationic amino acid residues (two arginines and two lysines). To enhance the antifungal activity of AmyI-1-18 against Candida albicans, 11 analogs bearing substitutions with alanine, leucine, and/or arginine, which were designed on the basis of the helical wheel projection of AmyI-1-18, were synthesized, and their antifungal activity was investigated. The antifungal activities of four analogs obtained by replacing arginine or lysine with alanine were significantly reduced. The results suggested that the cationic arginine and lysine residues in AmyI-1-18 are important for its antifungal activity. The antifungal activities of two single leucine-substituted analogs were not improved, but among three single arginine-substituted analogs, AmyI-1-18(D15R) had approximately a twofold higher antifungal activity [50% growth-inhibitory concentration (IC ): 31 μM] than AmyI-1-18 (IC : 64 μM) and exhibited low hemolytic activity (4% at 100 μM). Flow cytometric analysis using propidium iodide revealed that the antifungal activity of AmyI-1-18(D15R) was dependent on its membrane-disrupting activity in a manner different from that of AmyI-1-18. Further enhancement of the cationicity and hydrophobicity of AmyI-1-18(D15R) resulted in no improvement in antifungal activity and a significant increase in hemolytic activity. In this study, the results demonstrated that the antifungal activity of AmyI-1-18 against C. albicans was enhanced through increasing its membrane-disrupting activity by replacing aspartic acid at position 15 with arginine without a significant increase in hemolytic activity. © 2016 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 106: 219-229, 2016.

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“…For cationic α‐helical AMPs to be useful as therapeutic agents against human pathogens, they must have both high antimicrobial potency and the ability to distinguish microbial cells from mammalian cells on the basis of their different membrane lipid compositions. Thus, AMPs displaying low or no hemolytic activity would be attractive candidates for use as therapeutic agents …”

Section: Introductionmentioning

confidence: 99%

Antimicrobial activity and mechanism of action of a novel cationic α‐helical octadecapeptide derived from α‐amylase of rice

et al. 2015

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AmyI-1-18, an octadecapeptide derived from α-amylase (AmyI-1) of rice (Oryza sativa L. japonica), is a novel cationic α-helical antimicrobial peptide (AMP) that contains two lysine and two arginine residues. The antimicrobial activity of AmyI-1-18 against human pathogens was quantitatively evaluated using a chemiluminescence method that measures ATP derived from viable cells. Of the ten kinds of human pathogens, AmyI-1-18 exhibited antimicrobial activity against nine. Its 50% growth-inhibitory concentrations (ICs50 ) against Porphyromonas gingivalis, Propionibacterium acnes, Pseudomonas aeruginosa, Candida albicans, and Streptococcus mutans were 13, 19, 50, 64, and 77 μM, respectively. AmyI-1-18 had little or no hemolytic activity even at 500 μM, and showed negligible cytotoxicity up to 1200 μM. The degree of 3,3'-dipropylthiadicarbocyanine iodide release from P. gingivalis cells induced by the addition of AmyI-1-18 was significantly lower than that induced by the addition of melittin. Flow cytometric analysis showed that the percentages of P. aeruginosa, S. mutans, and C. albicans cells stained with propidium iodide (PI), a DNA-intercalating dye, were 89%, 43%, and 3%, respectively, when AmyI-1-18 was added at a concentration equal to its 4×IC50 . Therefore, the antimicrobial activity of AmyI-1-18 against P. aeruginosa and S. mutans appears to be mainly attributable to its membrane-disrupting activity. In contrast, its antimicrobial activity against P. gingivalis and C. albicans most likely depends upon interactions with intracellular targets other than their cell membranes. Collectively, these results indicate that AmyI-1-18 is useful as a safe and potent AMP against the pathogens described above in many fields of healthcare.

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Enhanced antimicrobial activity of novel synthetic peptides derived from vejovine and hadrurin

Cited by 27 publications

References 52 publications

Scorpion venom components as potential candidates for drug development

Scorpion venom components as potential candidates for drug development

Effect of alanine, leucine, and arginine substitution on antimicrobial activity against candida albicans and action mechanism of a cationic octadecapeptide derived from α‐amylase of rice

Antimicrobial activity and mechanism of action of a novel cationic α‐helical octadecapeptide derived from α‐amylase of rice

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