Dual Antimicrobial and Anticancer Activity of Membrane-Active Peptide BP52.

The linear undecapeptide BP52 was previously reported to have antibacterial activity against phytopathogenic bacteria species. Due to the structural similarities to naturally occurring cationic helical antimicrobial peptides, it was speculated that this peptide could potentially target microbial pathogens and cancer cells found in mammals. Consequently, this study aims to further investigate the structural and biological properties of this peptide. Our findings indicate that BP52 exhibits strong antimicrobial and anticancer activity while displaying relatively low levels of hemolytic activity. Hence, this study suggests that BP52 could be a potential lead compound for drug discovery against infectious diseases and cancer. Besides, new insights into the relationships between the structure and the multifunctional properties of antimicrobial peptides were also explored.

Cyclotides: The next generation in biopesticide development for eco-friendly agriculture.

Chemical pesticides remain the predominant method for pest management in numerous countries. Given the current landscape of agriculture, the development of biopesticides has become increasingly crucial. The strategy empowers farmers to efficiently manage pests and diseases, while prioritizing minimal adverse effects on the environment and human health, hence fostering sustainable management. In recent years, there has been a growing interest and optimism surrounding the utilization of peptide biopesticides for crop protection. These sustainable and environmentally friendly substances have been recognized as viable alternatives to synthetic pesticides due to their outstanding environmental compatibility and efficacy. Numerous studies have been conducted to synthesize and identify peptides that exhibit activity against significant plant pathogens. One of the peptide classes is cyclotides, which are cyclic cysteine-rich peptides renowned for their wide range of sequences and functions. In this review, we conducted a comprehensive analysis of cyclotides, focusing on their structural attributes, developmental history, significant biological functions in crop protection, techniques for identification and investigation, and the application of biotechnology to enhance cyclotide synthesis. The objective is to emphasize the considerable potential of cyclotides as the next generation of plant protection agents on the global scale.

Reducing Self-Assembly by Increasing Net Charge: Effect on Biological Activity of Mastoparan C.

The ability of amphipathic peptides to arrange themselves in aqueous solutions, known as self-assembly, has been found to reduce the effectiveness of these peptides in interacting with cell membranes. Therefore, minimizing their tendency to self-assemble could be a potential strategy for enhancing the pharmacological properties of antimicrobial peptides (AMPs). To explore this idea, this study prepared a series of natural peptides mastoparan C (MPC) with increased net charge and hydrophilicity via alanine-to-lysine substitution and investigated the impact on the biological activity. The preliminary data suggested the influence of both the overall positive charge and the position of a lysine residue on the self-assembly of MPC and its derivatives. Besides, the analogue MPC-A5K,A8K displayed higher anticancer activity and comparable antimicrobial activity with significantly lower hemolysis than MPC. Hence, reducing self-assembly by expanding the cationic area could be a promising approach for developing potent and selective AMPs.

Effect of substituting glutamine with lysine on structural and biological properties of antimicrobial peptide Polybia-MP1.

The natural antimicrobial peptide Polybia-MP1 is a promising candidate for developing new treatment therapy for infection and cancer. It showed broad-spectrum antimicrobial and anticancer activity with high safety on healthy cells. However, previous sequence modification usually resulted in at least one of two consequences: a notable increase in hemolytic activity or a considerable decrease in activity against Gram-negative bacteria and cancer cells. Herein, a new approach was applied by replacing the amino acid Glutamine at position 12 with Lysine and generating the MP1-Q12K analog. Our preliminary data suggested an enhancement in antibacterial and antifungal activity, whereas the anticancer and hemolytic activity of the two peptides were comparable. Moreover, MP1-Q12K was found to be less self-assembly than Polybia-MP1, which further supports the enhancement of antimicrobial properties. Hence, this study provides new information regarding the structure-activity relationships of Polybia-MP1 and support for the development of potent, selective antimicrobial peptides.

Comparison between Three Techniques for Determining Glomerular Filtration Rates: 99mTc-Diethylene Triamine Penta-Acetic Acid Renography, Double Plasma Sampling Method, and Single Plasma Sampling Method in Vietnamese Patients.

Glomerular filtration rate (GFR) is an important indicator of renal function. Many methods have been developed to determine GFR in clinical examinations. This study aims to correlate between radionuclide plasma sampling methods (single and double blood samples, in vitro methods) and in vivo Gate's method using 99mTc-diethylene triamine penta-acetic acid (99mTc-DTPA) renography. MATERIALS AND METHODS: 43 patients underwent this study, including 31 renal donors (Group 1) and 12 patients with obstructive uropathy (Group 2). All patients were administered with a range of 5-7 mCi of 99mTc-DTPA. Then, renography performed simultaneously after injection and GFR calculation followed by Gate's method. Blood samples were collected at 60- and 120-min postinjection, samples were counted by a thyroid uptake system, and GFR was calculated using a single plasma sample method (SPSM) and a double plasma sample method (DPSM). RESULTS: The mean GFRs calculated by Gate's method in Groups 1 and 2 were 85.8 ± 18.2 ml/min and 118.4 ± 13.9 ml/min, respectively. Meanwhile, using the in vitro blood sampling methods (DPSM and SPSM), the mean GFRs in Group 1 were 73.8 ± 15.4 ml/min and 56.4 ± 20.9 ml/min, respectively, and in Group 2 were 116.8 ± 12.9 ml/min and 106.3 ± 18.5 ml/min, respectively. There is a high correlation between Gate's method and DPSM in two groups (r = 0.86 and 0.72, respectively), and a moderate correlation was found between Gate's method and SPSM in both groups (r = 0.49 and r = 0.37, respectively). The two in vitro methods (DPSM and SPSM) revealed that moderate correlation in both groups (r = 0.74 and r = 0.67, respectively) was observed. CONCLUSION: Renography is a simple method but considered inaccurate for GFR determination. However, in vitro plasma sampling is rarely used in Vietnam. In this study, Gate's method correlated well with DPSM and tended to overestimate GFR. Further, the in vitro methods can be applied to correct the in vivo method as a confirmatory test in some cases.

Benzo[d]thiazole-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl as potent selective lasB quorum sensing inhibitors of Gram-negative bacteria.

Quorum sensing is a well-known term for describing bacterial cell-cell communication. Bacteria use quorum sensing pathways to respond to external factors such as nutrient availability, defense mechanisms, and coordinate host toxic behaviors such as biofilm formation, virulence production, and other pathogenesis. Discovery of novel compounds which inhibit quorum sensing without being antibiotic are currently emerging fields. Herein, the library of fifteen benzo[d]thiazole/quinoline-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl compounds was designed, synthesized and evaluated to find novel quorum sensing inhibitors. Firstly, compounds were evaluated for their growth inhibitory activities at high concentrations up to 1000 µg mL-1 toward Pseudomonas aeruginosa. Under our conditions, twelve compounds showed moderate growth inhibitory activities in the concentration tested. To our delight, three compounds 3, 6 and 7 do not affect the growth of the bacteria which were chosen for the evaluation of quorum sensing inhibitor activities. In the LasB system, our compounds 3, 6, 7 showed promising quorum-sensing inhibitors with IC50 of 115.2 µg mL-1, 182.2 µg mL-1 and 45.5 µg mL-1, respectively. In the PqsR system, no activity observed suggesting that the selectivity of the compound toward the LasB system. In addition, 7 showed the moderate anti-biofilm formation of Pseudomonas aeruginosa. Docking studies revealed that 3, 6 and 7 binding to the active site of Pseudomonas aeruginosa quorum sensing LasR system with better affinity compared to reference compounds 4-NPO. Finally, computation calculations suggest that compounds are a good template for further drug development.

Correction: Benzo[d]thiazole-2-thiol bearing 2-oxo-2-substituted-phenylethan-1-yl as potent selective lasB quorum sensing inhibitors of Gram-negative bacteria.

[This corrects the article DOI: 10.1039/D1RA03616E.].