The effect of elongation of a peptide substituent with ArgSer motif on the antimicrobial properties of hemin derivatives

2018 ◽  
Vol 22 (12) ◽  
pp. 1060-1071
Author(s):  
Sergey V. Blagodarov ◽  
Galina A. Zheltukhina ◽  
Sergey V. Yeremin ◽  
Ekaterina S. Babicheva ◽  
Elena P. Mirchink ◽  
...  

The natural metalloporphyrin hemin possesses a number of properties that determine its attractiveness as a basis for creating potential medicines. The development of research in this area is restrained by hemin’s pronounced toxicity, mainly in relation to normal red blood cells, and also by its water insolubility. We previously synthesized amino acid and peptide hemin derivatives with sufficient water solubility and in some cases high antimicrobial (antibacterial and antifungal) potency [1, 2]. In order to establish the relationship between structure and function, this paper studies the peptide substituent in hemin derivatives (HD) elongated by multiplying the -ArgSer- motif and its effect on the biological and physicochemical properties of their aqueous solutions. A nonlinear nonmonotonic dependence of their physicochemical properties and biological potency on the HD concentration and the length of peptide substituent was revealed based on calculations of hydrophilic properties of substituents in HD and a study by electron and laser correlation spectroscopy of their properties in aqueous solutions.

Marine Drugs ◽  
2018 ◽  
Vol 16 (10) ◽  
pp. 381 ◽  
Author(s):  
Gabriel Matos ◽  
Paulina Schmitt ◽  
Cairé Barreto ◽  
Natanael Farias ◽  
Guilherme Toledo-Silva ◽  
...  

Anti-lipopolysaccharide factors (ALFs) are antimicrobial peptides with a central β-hairpin structure able to bind to microbial components. Mining sequence databases for ALFs allowed us to show the remarkable diversity of ALF sequences in shrimp. We found at least seven members of the ALF family (Groups A to G), including two novel Groups (F and G), all of which are encoded by different loci with conserved gene organization. Phylogenetic analyses revealed that gene expansion and subsequent diversification of the ALF family occurred in crustaceans before shrimp speciation occurred. The transcriptional profile of ALFs was compared in terms of tissue distribution, response to two pathogens and during shrimp development in Litopenaeus vannamei, the most cultivated species. ALFs were found to be constitutively expressed in hemocytes and to respond differently to tissue damage. While synthetic β-hairpins of Groups E and G displayed both antibacterial and antifungal activities, no activity was recorded for Group F β-hairpins. Altogether, our results showed that ALFs form a family of shrimp AMPs that has been the subject of intense diversification. The different genes differ in terms of tissue expression, regulation and function. These data strongly suggest that multiple selection pressures have led to functional diversification of ALFs in shrimp.


Author(s):  
Patricia G. Arscott ◽  
Gil Lee ◽  
Victor A. Bloomfield ◽  
D. Fennell Evans

STM is one of the most promising techniques available for visualizing the fine details of biomolecular structure. It has been used to map the surface topography of inorganic materials in atomic dimensions, and thus has the resolving power not only to determine the conformation of small molecules but to distinguish site-specific features within a molecule. That level of detail is of critical importance in understanding the relationship between form and function in biological systems. The size, shape, and accessibility of molecular structures can be determined much more accurately by STM than by electron microscopy since no staining, shadowing or labeling with heavy metals is required, and there is no exposure to damaging radiation by electrons. Crystallography and most other physical techniques do not give information about individual molecules.We have obtained striking images of DNA and RNA, using calf thymus DNA and two synthetic polynucleotides, poly(dG-me5dC)·poly(dG-me5dC) and poly(rA)·poly(rU).


2019 ◽  
Vol 10 ◽  
pp. 1864-1872
Author(s):  
Prof. Teodora P. Popova

The effect of ionized aqueous solutions (anolytes and catholyte) in the processing of fruits (cherries, morellos, and strawberries) for decontamination has been tested. Freshly prepared analytes and catholyte without the addition of salts were used, as well as stored for 7 months anolytes, prepared with 0.5% NaCl and a combination of 0.5% NaCl and 0.5% Na2CO3. The anolyte prepared with a combination of 0.5% NaCl and 0.5% Na2CO3, as well as the anolyte obtained with 0.5% NaCl, exhibit high antimicrobial activity against the surface microflora of strawberries, cherries, and sour cherries. They inactivate E. coli for 15 minutes. The other species of the fam. Enterobacteriaceae were also affected to the maximum extent, as is the total number of microorganisms, especially in cherries and sour cherries. Even stored for 7 months, they largely retain their antimicrobial properties. Anolyte and catholyte, obtained without the addition of salts, showed a lower effect on the total number of microorganisms, but had a significant effect on Gram-negative bacteria, and especially with regard to the sanitary indicative E. coli.


2018 ◽  
Vol 18 (9) ◽  
pp. 797-807 ◽  
Author(s):  
Paula dos Passos Menezes ◽  
Francielly de Oliveira Araujo ◽  
Tatianny Araujo Andrade ◽  
Igor Araujo Santos Trindade ◽  
Heitor Gomes de Araujo-Filho ◽  
...  

Background: Some research studies have shown that Lippia pedunculosa essential oil (EOLP) has interesting biological activities. However, its low water solubility is the main challenge to achieve its therapeutic potential. In this context, Cyclodextrins (CDs) have been widely used in order to overcome this problem due to your capability to improve the physicochemical properties of drugs. Objective: In this perspective, the main goal of this study was to investigate how the improvement of the physicochemical properties of inclusion complexes (EOLP and β-CD) enhance the antinociceptive effect in mice. Methods: To achieve that, we prepared samples by Physical Mixture (PM), Paste Complexation (PC) and Slurry Complexation (SC) methods, followed by their physicochemical characterization. In addition, it was evaluated if the use of β-CD enhances the antinociceptive effect of EOLP in mice. Results: The analysis showed that rotundifolone (72.02%) was the major compound of EOLP and we found out based on DSC results that β-CD protected it from oxidation. In addition, TG techniques demonstrated that the best inclusion methods were PC and SC, due to their greater weight loss (10.8 and 11.6%, respectively) in the second stage (171-312°C), indicating that more complexed oil was released at the higher temperature than oil free. Other characteristics, such as changes in the typical crystalline form, and reduced particle size were observed by SEM and laser diffraction, respectively. The SC was the most effective complexation method, once the presence of rotundifolone was detected by FTIR. Based on that, SC method was used in all mice tests. In this regard, the number of paw licks was reduced for both compounds (all doses), but EOLP was more effective in reducing the nociceptive behavior. Conclusion: Therefore, CDs seem not to be a good tool to enhance the pharmacological properties of EOs rich in peroxide compounds such as rotundifolone.


2020 ◽  
Vol 17 (9) ◽  
pp. 1084-1101
Author(s):  
Tingjuan Wu ◽  
Xu Yao ◽  
Guan Wang ◽  
Xiaohe Liu ◽  
Hongfei Chen ◽  
...  

Background: Oleanolic Acid (OA) is a ubiquitous product of triterpenoid compounds. Due to its inexpensive availability, unique bioactivities, pharmacological effects and non-toxic properties, OA has attracted tremendous interest in the field of drug design and synthesis. Furthermore, many OA derivatives have been developed for ameliorating the poor water solubility and bioavailability. Objective: Over the past few decades, various modifications of the OA framework structure have led to the observation of enhancement in bioactivity. Herein, we focused on the synthesis and medicinal performance of OA derivatives modified on A-ring. Moreover, we clarified the relationship between structures and activities of OA derivatives with different functional groups in A-ring. The future application of OA in the field of drug design and development also was discussed and inferred. Conclusion: This review concluded the novel achievements that could add paramount information to the further study of OA-based drugs.


1979 ◽  
Vol 44 (1) ◽  
pp. 167-173 ◽  
Author(s):  
Slavomír Bystrický ◽  
Rudolf Kohn ◽  
Tibor Sticzay

The CD spectra of aqueous solutions of homopolymeric sodium oligogalacturonates and D-galacturonans of polymerization degree n = 1-64, as well as lower calcium oligogalacturonates (n = 1-5) were measured. Chiroptic properties were correlated with the polymerization degree in terms of optical superposition of monomeric unit increments. Interpretation of obtained data, respecting further physicochemical properties entitles to conclude that the conformation of macromolecules of D-galacturonan in solution is close to helical structure.


1992 ◽  
Vol 57 (8) ◽  
pp. 1739-1746
Author(s):  
Katarína Škvareninová ◽  
Štefan Baláž ◽  
Ernest Šturdík ◽  
Miroslav Veverka ◽  
Jana Adamcová ◽  
...  

In the series of cephalosporin derivatives, consisting of eight 7-(R1-CH2-CO-NH)cephalosporanic acids and of seven analogical compounds with 3-acetoxymethyl replaced by 3-CH3, physicochemical properties, which are expected to play a role in their antibacterial effects (the transport rate parameters and partition coefficients in the systems 1-octanol-water and 1-octanol-buffer, dissociation constants of the 4-carboxyl group, reactivity towards L-glutathione imitating the nucleophilic groups of the cell components and hydrolysis rate parameters), were determined. Linear dependences were observed between the partition coefficients and the π-constants of the varying substituents as well as between reactivity towards SH-groups of L-glutathione and OH-groups. The relationship between the transport rate parameters and partition coefficients, both measured in buffered as well as non-buffered system, was described by a common non-linear equation.


Author(s):  
J. Donald Boudreau ◽  
Eric Cassell ◽  
Abraham Fuks

This book reimagines medical education and reconstructs its design. It originates from a reappraisal of the goals of medicine and the nature of the relationship between doctor and patient. The educational blueprint outlined is called the “Physicianship Curriculum” and rests on two linchpins. First is a new definition of sickness: Patients know themselves to be ill when they cannot pursue their purposes and goals in life because of impairments in functioning. This perspective represents a bulwark against medical attention shifting from patients to diseases. The curriculum teaches about patients as functional persons, from their anatomy to their social selves, starting in the first days of the educational program and continuing throughout. Their teaching also rests on the rock-solid grounding of medicine in the sciences and scientific understandings of disease and function. The illness definition and knowledge base together create a foundation for authentic patient-centeredness. Second, the training of physicians depends on and culminates in development of a unique professional identity. This is grounded in the historical evolution of the profession, reaching back to Hippocrates. It leads to reformulation of the educational process as clinical apprenticeships and moral mentorships. “Rebirth” in the title suggests that critical ingredients of medical education have previously been articulated. The book argues that the apprenticeship model, as experienced, enriched, taught, and exemplified by William Osler, constitutes a time-honored foundation. Osler’s “natural method of teaching the subject of medicine” is a precursor to the Physicianship Curriculum.


Foods ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 86
Author(s):  
So-Ra Yoon ◽  
Yun-Mi Dang ◽  
Su-Yeon Kim ◽  
Su-Yeon You ◽  
Mina K. Kim ◽  
...  

Capsaicinoid content, among other factors, affects the perception of spiciness of commercial kimchi. Here, we investigated whether the physicochemical properties of kimchi affect the spicy taste of capsaicinoids perceived by the tasting. High-performance liquid chromatography (HPLC) was used to evaluate the capsaicinoid content (mg/kg) of thirteen types of commercial kimchi. The physicochemical properties such as pH, titratable acidity, salinity, free sugar content, and free amino acid content were evaluated, and the spicy strength grade was determined by selected panel to analyze the correlation between these properties. Panels were trained for 48 h prior to actual evaluation by panel leaders trained for over 1000 h according to the SpectrumTM method. Partial correlation analysis was performed to examine other candidate parameters that interfere with the sensory evaluation of spiciness and capsaicinoid content. To express the specific variance after eliminating the effects of other variables, partial correlations were used to estimate the relationships between two variables. We observed a strong correlation between spiciness intensity ratings and capsaicinoid content, with a Pearson’s correlation coefficient of 0.78 at p ≤ 0.001. However, other specific variables may have influenced the relationship between spiciness intensity and total capsaicinoid content. Partial correlation analysis indicated that the free sugar content most strongly affected the relationship between spiciness intensity and capsaicinoid content, showing the largest first-order partial correlation coefficient (rxy/z: 0.091, p ≤ 0.01).


e-Polymers ◽  
2020 ◽  
Vol 20 (1) ◽  
pp. 154-161 ◽  
Author(s):  
Gao Yurong ◽  
Li Dapeng

AbstractCorn starch/polyvinyl alcohol (PVA)/glycerol composite films incorporated with ε-polylysine were prepared, and their properties were investigated. The Fourier-transform infrared (FTIR) spectroscopy indicated that the interactions happened between the amino group of ε-polylysine and hydroxyl group starch/PVA composite films. X-ray diffraction (XRD) analysis showed that the addition of ε-polylysine decreased the intensity of all crystal peaks. Thermogravimetric (TGA) analysis suggested that ε-polylysine improved the thermal stability of composite films. Scanning electron microscopic (SEM) analysis showed that the upper surface of composite films incorporated with ε-polylysine presented more compact and flat surface. The antimicrobial activity of the composite film progressively increased with the increasing of ε-polylysine concentration (P < 0.05). The tensile strength, elongation at break and water absorption significantly increased, whereas water solubility decreased with the increasing of ε-polylysine concentration (P < 0.05). Therefore, the corn starch/PVA/glycerol composite films incorporated with ε-polylysine had good mechanical, physical and antimicrobial properties and could have potential application as a novel antimicrobial packaging material.


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