scholarly journals Bioevaluation of Ranatuerin-2Pb from the Frog Skin Secretion of Rana pipiens and its Truncated Analogues

Biomolecules ◽  
2019 ◽  
Vol 9 (6) ◽  
pp. 249 ◽  
Author(s):  
Zhou ◽  
Shi ◽  
Zhong ◽  
Ye ◽  
Ma ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Broad Spectrum ◽  
Rana Pipiens ◽  
Galleria Mellonella ◽  
Skin Secretion ◽  
Bacterial Killing ◽  
Structure Activity ◽  
Promising Agent ◽  
Large Numbers ◽  
Relationship Of

Antimicrobial peptides (AMPs) are considered as a promising agent to overcome the drug-resistance of bacteria. Large numbers of AMPs have been identified from the skin secretion of Rana pipiens, including brevinins, ranatuerins, temporins and esculentins. In this study, the cDNA precursor of a broad-spectrum antimicrobial peptide, ranatuerin-2Pb, was cloned and identified. Additionally, two truncated analogues, RPa and RPb, were synthesised to investigate the structure-activity relationship of ranatuerin-2Pb. RPa lost antimicrobial activity against Candida albicans, MRSA, Enterococcus faecalis and Pseudomonas aeruginosa, while RPb retained its broad-spectrum antimicrobial activity. Additionally, ranatuerin-2Pb, RPa and RPb demonstrated inhibition and eradication effects against Staphylococcus aureus biofilm. RPb showed a rapid bacterial killing manner via membrane permeabilization without damaging the cell membrane of erythrocytes. Moreover, RPb decreased the mortality of S. aureus infected Galleria mellonella larvae. Collectively, our results suggested that RPb may pave a novel way for natural antimicrobial drug design.

scholarly journals Study on the Structure-Activity Relationship of an Antimicrobial Peptide, Brevinin-2GUb, from the Skin Secretion of Hylarana guentheri

Antibiotics ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 895
Author(s):  
Yaxian Lin ◽  
Siyan Liu ◽  
Xinping Xi ◽  
Chengbang Ma ◽  
Lei Wang ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibiotic Resistance ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Resistant Bacteria ◽  
Skin Secretion ◽  
Structure Activity ◽  
Active Fragments ◽  
Net Charges ◽  
Relationship Of

Antimicrobial peptides (AMPs) are considered potential alternatives to antibiotics due to their advantages in solving antibiotic resistance. Brevinin-2GUb, which was extracted from the skin secretion of Hylarana guentheri, is a peptide with modest antimicrobial activity. Several analogues were designed to explore the structure–activity relationship and enhance its activity. In general, the Rana box is not an indispensable motif for the bioactivity of Brevinin-2GUb, and the first to the 19th amino acids at the N-terminal end are active fragments, such that shortening the peptide while maintaining its bioactivity is a promising strategy for the optimisation of peptides. Keeping a complete hydrophobic face and increasing the net charges are key factors for antimicrobial activity. With the increase of cationic charges, α-helical proportion, and amphipathicity, the activity of t-Brevinin-2GUb-6K (tB2U-6K), in combatting bacteria, drastically improved, especially against Gram-negative bacteria, and the peptide attained the capacity to kill clinical isolates and fungi as well, which made it possible to address some aspects of antibiotic resistance. Thus, peptide tB2U-6K, with potent antimicrobial activity against antibiotic-resistant bacteria, the capacity to inhibit the growth of biofilm, and low toxicity against normal cells, is of value to be further developed into an antimicrobial agent.

SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIP OF NEW BENZIMIDAZOLE DERIVATIVES AS ANTIMICROBIAL AGENTS

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (03) ◽  
pp. 25-29
Author(s):  
S. G Jadhav ◽  
◽  
S. R. Pattan
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
Antimicrobial Agents ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Benzimidazole Derivatives ◽  
Structure Activity ◽  
Relationship Of

A new series of substituted benzimidazole derivatives were synthesized and the structures of these compounds were established on the basis of spectral data. The title compounds were evaluated for antimicrobial activity. Some of these compounds have shown excellent antimicrobial activity.

scholarly journals Evaluating the Bioactivity of a Novel Broad-Spectrum Antimicrobial Peptide Brevinin-1GHa from the Frog Skin Secretion of Hylarana guentheri and Its Analogues

Toxins ◽  
2018 ◽  
Vol 10 (10) ◽  
pp. 413 ◽  
Author(s):  
Qi Chen ◽  
Peng Cheng ◽  
Chengbang Ma ◽  
Xinping Xi ◽  
Lei Wang ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Peptide ◽  
Broad Spectrum ◽  
Hemolytic Activity ◽  
High Performance ◽  
Disulfide Bridge ◽  
Reversed Phase ◽  
Central Position ◽  
Skin Secretion ◽  
Mass Spectral

Many antimicrobial peptides (AMPs) have been identified from the skin secretion of the frog Hylarana guentheri (H.guentheri), including Temporin, Brevinin-1, and Brevinin-2. In this study, an antimicrobial peptide named Brevinin-1GHa was identified for the first time by using ‘shotgun’ cloning. The primary structure was also confirmed through mass spectral analysis of the skin secretion purified by reversed-phase high-performance liquid chromatography (RP-HPLC). There was a Rana-box (CKISKKC) in the C-terminal of Brevinin-1GHa, which formed an intra-disulfide bridge. To detect the significance of Rana-box and reduce the hemolytic activity, we chemically synthesized Brevinin-1GHb (without Rana-box) and Brevinin-1GHc (Rana-box in central position). Brevinin-1GHa exhibited a strong and broad-spectrum antimicrobial activity against seven microorganisms, while Brevinin-1GHb only inhibited the growth of Staphylococcus aureus (S. aureus), which indicates Rana-box was necessary for the antimicrobial activity of Brevinin-1GHa. The results of Brevinin-1GHc suggested transferring Rana-box to the central position could reduce the hemolytic activity, but the antimicrobial activity also declined. Additionally, Brevinin-1GHa demonstrated the capability of permeating cell membrane and eliminating biofilm of S. aureus, Escherichia coli (E. coli), and Candida albicans (C. albicans). The discovery of this research may provide some novel insights into natural antimicrobial drug design.

Antimicrobial Activity of Kaurane Diterpenes against Oral Pathogens

2008 ◽  
Vol 63 (5-6) ◽  
pp. 326-330 ◽  
Author(s):  
Sergio R. Ambrosio ◽  
Niege A. J. C. Furtado ◽  
Dionéia C. R. de Oliveira ◽  
Fernando B. da Costa ◽  
Carlos H. G. Martins ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Lactobacillus Casei ◽  
Periodontal Diseases ◽  
Significant Activity ◽  
Streptococcus Sobrinus ◽  
Methyl Ester Derivative ◽  
Structure Activity ◽  
Structural Differences ◽  
Oral Pathogens ◽  
Relationship Of

Two kaurane diterpenes, ent-kaur-16(17)-en-19-oic acid (KA) and 15-β-isovaleryloxy-entkaur- 16(17)-en-19-oic acid (KA-Ival), isolated from Aspilia foliacea, and the methyl ester derivative of KA (KA-Me) were evaluated against oral pathogens. KA was the most active compound, with MIC values of 10 μg mL-1 against the following microorganisms: Streptococcus sobrinus, Streptococcus mutans, Streptococcus mitis, Streptococcus sanguinis, and Lactobacillus casei. However, KA did not show significant activity against Streptococcus salivarius and Enterococcus faecalis, with MIC values equal to 100 and 200 μg mL-1, respectively. Our results show that KA has potential to be used as a prototype for the discovery of new effective anti-infection agents against microorganisms responsible for caries and periodontal diseases. Moreover, these results allow to conclude that minor structural differences among these diterpenes significantly influence their antimicrobial activity, bringing new perspectives to studies on the structure-activity relationship of this type of metabolites with respect to caries and periodontal diseases.

Structure–Activity Relationship of a Broad-Spectrum Insect Odorant Receptor Agonist

2012 ◽  
Vol 7 (10) ◽  
pp. 1647-1652 ◽  
Author(s):  
Robert W. Taylor ◽  
Ian M. Romaine ◽  
Chao Liu ◽  
Poornima Murthi ◽  
Patrick L. Jones ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Receptor Agonist ◽  
Odorant Receptor ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of
Sign in / Sign up

Export Citation Format

Share Document