scholarly journals Natural and Synthetic Halogenated Amino Acids—Structural and Bioactive Features in Antimicrobial Peptides and Peptidomimetics

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7401
Author(s):  
Mario Mardirossian ◽  
Marina Rubini ◽  
Mauro F. A. Adamo ◽  
Marco Scocchi ◽  
Michele Saviano ◽  
...  
Keyword(s):  
Amino Acids ◽  
Antimicrobial Peptides ◽  
Mode Of Action ◽  
Biological Effects ◽  
3D Structure ◽  
Surface Characteristics ◽  
Antimicrobial Drugs ◽  
Antibiotic Resistant ◽  
Physico Chemical ◽  
Proteins And Peptides

The 3D structure and surface characteristics of proteins and peptides are crucial for interactions with receptors or ligands and can be modified to some extent to modulate their biological roles and pharmacological activities. The introduction of halogen atoms on the side-chains of amino acids is a powerful tool for effecting this type of tuning, influencing both the physico-chemical and structural properties of the modified polypeptides, helping to first dissect and then rationally modify features that affect their mode of action. This review provides examples of the influence of different types of halogenation in amino acids that replace native residues in proteins and peptides. Examples of synthetic strategies for obtaining halogenated amino acids are also provided, focusing on some representative compounds and their biological effects. The role of halogenation in native and designed antimicrobial peptides (AMPs) and their mimetics is then discussed. These are in the spotlight for the development of new antimicrobial drugs to counter the rise of antibiotic-resistant pathogens. AMPs represent an interesting model to study the role that natural halogenation has on their mode of action and also to understand how artificially halogenated residues can be used to rationally modify and optimize AMPs for pharmaceutical purposes.

Characterizing the structure–function relationship reveals the mode of action of a novel antimicrobial peptide, P1, from jumper ant Myrmecia pilosula

2017 ◽  
Vol 13 (6) ◽  
pp. 1193-1201 ◽  
Author(s):  
Tien-Sheng Tseng ◽  
Keng-Chang Tsai ◽  
Chinpan Chen
Keyword(s):  
Public Health ◽  
Antimicrobial Peptide ◽  
Structure Function ◽  
Mode Of Action ◽  
Antimicrobial Drugs ◽  
Antibiotic Resistant ◽  
Structure Function Relationship ◽  
Microbial Infections ◽  
Resistant Strains ◽  
Function Relationship

Microbial infections of antibiotic-resistant strains cause serious diseases and have a significant impact on public health worldwide, so novel antimicrobial drugs are urgently needed.

Antimicrobial Peptides: A Promising Avenue for Human Healthcare

2020 ◽  
Vol 21 (2) ◽  
pp. 90-96 ◽  
Author(s):  
Girish M. Bhopale
Keyword(s):  
Antimicrobial Peptides ◽  
Antimicrobial Peptide ◽  
Antimicrobial Agents ◽  
Current Status ◽  
Antimicrobial Drugs ◽  
Spectrum Activity ◽  
Low Levels ◽  
Human Healthcare ◽  
Broad Spectrum Activity ◽  
Promising Avenue

Antimicrobial drugs resistant microbes have been observed worldwide and therefore alternative development of antimicrobial peptides has gained interest in human healthcare. Enormous progress has been made in the development of antimicrobial peptide during the last decade due to major advantages of AMPs such as broad-spectrum activity and low levels of induced resistance over the current antimicrobial agents. This review briefly provides various categories of AMP, their physicochemical properties and mechanism of action which governs their penetration into microbial cell. Further, the recent information on current status of antimicrobial peptide development, their applications and perspective in human healthcare are also described.

Multi-Epitope Vaccines (MEVs), as a Novel Strategy Against Infectious Diseases

2020 ◽  
Vol 17 (5) ◽  
pp. 354-364
Author(s):  
Mohammad Mahmoudi Goumari ◽  
Ibrahim Farhani ◽  
Navid Nezafat ◽  
Shirin Mahmoodi
Keyword(s):  
Infectious Diseases ◽  
Epitope Prediction ◽  
Cost Effective ◽  
Antimicrobial Drugs ◽  
Antibiotic Resistant ◽  
Time Consumption ◽  
Preclinical Evaluation ◽  
Structural Evaluation ◽  
Novel Strategy ◽  
Epitope Vaccines

Infectious diseases have caused historical pandemics in the world. Three strategies, including sanitation programs, antimicrobial drugs, and vaccines are considered for the prevention and treatment of infectious diseases. Today, some infectious diseases cause millions of mortalities universally. Due to the emergence of antibiotic-resistant pathogens, as well as some limitations of traditional vaccines, focusing on novel strategies is essential. Multi-Epitope Vaccines (MEVs), as a novel strategy, have been designed based on immunoinformatics methods; epitope prediction by authentic servers, attachment of epitopes using proper linkers, physicochemical, immunological and structural evaluation by bioinformatics tools that are basic stages in MEVs designing. Advantages such as cost-effective, high safety, less time consumption in designing, the application of natural adjuvants, and satisfactory preclinical evaluation outstand MEVs than other types of vaccines. Therefore, MEVs are promising vaccines against resistant diseases such as lower respiratory infection and diarrhea.

Standard manufacturing process of Lekhana Putapaka

2017 ◽  
Vol 2 (1) ◽  
Author(s):  
Rejoice N. Macwan ◽  
Vaishnav P. U. ◽  
L. B. Singh ◽  
B. L. Umrethiya ◽  
B. D. Kalasariya
Keyword(s):  
Amino Acids ◽  
Specific Gravity ◽  
Blood Vessels ◽  
Manufacturing Process ◽  
Solid Content ◽  
Burning Sensation ◽  
Wild Animals ◽  
Chemical Parameters ◽  
Eye Disorders ◽  
Physico Chemical

Putapaka is one of the best local and effective applications for the treatment of eye disorders. Putapaka when used properly then it will treat burning sensation, inflammation, pain, feeling of friction, discharges, itching sensation, stickiness, muddy secretions and congestion of blood vessels. In classics there are three types of Putapaka are described Snehana Putapaka, Lekhana Putapaka and Ropana Putapaka. Lekhana Putapaka is prepared mainly with the help of Lekhana Dravyas. It is used for scrapping of the Doshas. Lekhana Putapaka is composed of the liver and flesh of wild animals with the drugs of Lekhana group and Lauha Bhasma, Tamra Bhasma, Shankha Bhasma, Saindhava, Samudrafena, Kasisa, Srotanjana and Dadhi Mastu. In this study, the ingredients for Lekhana Putapaka has been taken as per the reference of Sushruta Samhita but prepared by some modification (in pressure cooker). The yield of three batches of Putapaka was 85ml, 90ml and 100 ml respectively. The physico-chemical parameters like pH, specific gravity and solid content and phytochemical parameters like glycocides, saponin, tannin, steroids, amino acids, proteins etc has been carried out.

Synthesis and characteristics of ethylenediamine-N,N'-di-S-α-isovalerate and isomers of its cobalt(III) complexes

1982 ◽  
Vol 47 (1) ◽  
pp. 210-216 ◽  
Author(s):  
Milan Strašák ◽  
František Bachratý ◽  
Jaroslav Majer
Keyword(s):  
Amino Acids ◽  
Absolute Configuration ◽  
Electronic Absorption ◽  
Electronic Absorption Spectra ◽  
Chemical Parameters ◽  
Methyl Group ◽  
Nmr Data ◽  
Physico Chemical ◽  
Natural Amino Acids ◽  
C Nmr

The synthesis and physico-chemical parameters are described of a new complexone based on natural amino acids, viz. ethylenediamine-N,N'-di-S-α-isovalerate (SS-EDDIV). 1H- and 13C-NMR data revealed that the methyl group in the substance are not equivalent. The isomers of the cobalt(III) complex with the asymmetric tetradentate SS-EDDIV ligand were prepared and separated; their characteristics are given. The absolute configuration of two of the five theoretically feasible isomers was determined based on their electronic absorption spectra and circular dichroism data.

Vasopressin and oxytocin analogs with interchanged sequence of amino acids in positions 7 and 8. synthesis and biological effects

1981 ◽  
Vol 46 (9) ◽  
pp. 2136-2139 ◽  
Author(s):  
Ivo Bláha ◽  
Viktor Krchňák ◽  
Milan Zaoral
Keyword(s):  
Amino Acids ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Biological Effects ◽  
Free Flow ◽  
Protecting Groups ◽  
Pressor Effect ◽  
Phase Synthesis ◽  
Antidiuretic Effect

p-Toluenesulfonyl-S-benzylcysteinyl-tyrosyl-phenylalanyl-glutaminyl-asparaginyl-S-benzylcysteinyl-NG-p-toluenesulfanylarginyl-prolyl-glycineamide (I) and S-benzylcysteinyl-tyrosyl-isoleucyl-glutaminyl-asparaginyl-S-benzylcysteinyl-leucyl-prolyl-glycine amide (III) were prepared by solid phase synthesis. After removal of the protecting groups, closure of the disulfide ring, and purification by continuous free-flow electrophoresis [arginine7, proline8]vasopressin (II) and [leucine7, proline8]oxytocin (IV) were obtained. The antidiuretic effect of II is markedly higher than its pressor effect; IV possesses c. 6% of the uterotonic and c. 10% of the galactogogous effect of oxytocin.

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