Antibacterial Potential of a Novel Peptide from the Consensus sequence of Dermaseptin Related Peptides Secreted by Agalychnis annae

Author(s):  
Ya’u Sabo Ajingi ◽  
Auwal Muhammad ◽  
Pongsak Khunrae ◽  
Triwit Rattanarojpong ◽  
Kovit Pattanapanyasate ◽  
...  

Background: The consistently increasing reports of bacterial resistance and the reemergence of bacterial epidemics have inspired the health and scientific community to discover new molecules with antibacterial potential continuously. Frog-skin secretions constitute bioactive compounds essential for finding new biopharmaceuticals. The exact antibacterial characterization of dermaseptin related peptides derived from Agalychnis annae is limited. The resemblance in their conserved and functionally linked genomes indicates an unprecedented opportunity to obtain novel bioactive compounds. Objective: In this study, we derived a novel peptide sequence and determined its antibacterial potentials. Method: Consensus sequence strategy was used to design the novel and active antibacterial peptide named 'AGAAN' from skin secretions of Agalychnis annae. The In-vitro activities of the novel peptide against some bacterial strains were investigated. Time kill studies, DNA retardation, cytotoxicity, beta-galactosidase, and molecular computational studies were conducted. Results: AGAAN inhibited P. aeruginosa, E. faecalis, and S. typhimurium at 20 µM concentration. E. coli and S. aureus were inhibited at 25 µM, and lastly, B. subtilis at 50 µM. Kinetics of inactivation against exponential and stationary growing bacteria was found to be rapid within 1-5 hours of peptide exposure, depending on time and concentration. The peptide displayed weak hemolytic activity between 0.01%–7.31% at the antibacterial concentrations. AGAAN efficiently induced bacterial membrane damage with subsequent cell lysis. The peptide's DNA binding shows that it also targets intracellular DNA by retarding its movement. Our in-silico molecular docking analysis displayed a strong affinity to the bacterial cytoplasmic membrane. Conclusion: AGAAN exhibits potential antibacterial properties that could be used to combat bacterial resistance.

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2028
Author(s):  
Son Thai Thai Le ◽  
Dávid Páll ◽  
Erzsébet Rőth ◽  
Tuyen Tran ◽  
Nóra Debreczeni ◽  
...  

Pleuromutilin is a fungal diterpene natural product with antimicrobial properties, semisynthetic derivatives of which are used in veterinary and human medicine. The development of bacterial resistance to pleuromutilins is known to be very slow, which makes the tricyclic diterpene skeleton of pleuromutilin a very attractive starting structure for the development of new antibiotic derivatives that are unlikely to induce resistance. Here, we report the very first synthetic modifications of pleuromutilin and lefamulin at alkene position C19–C20, by two different photoinduced addition reactions, the radical thiol-ene coupling reaction, and the atom transfer radical additions (ATRAs) of perfluoroalkyl iodides. Pleuromutilin were modified with the addition of several alkyl- and aryl-thiols, thiol-containing amino acids and nucleoside and carbohydrate thiols, as well as perfluoroalkylated side chains. The antibacterial properties of the novel semisynthetic pleuromutilin derivatives were investigated on a panel of bacterial strains, including susceptible and multiresistant pathogens and normal flora members. We have identified some novel semisynthetic pleuromutilin and lefamulin derivatives with promising antimicrobial properties.


Author(s):  
Elhassan Benyagoub ◽  
Nouria Nabbou ◽  
Dalila Razni ◽  
Snoussi Moghtet

Objective: The purpose of this work is to study the biological activity of Anastatica hierochuntica L., against nine bacterial strains responsible for women’s uro-genital infection (UGI).Methods: The plant was collected from Tindouf region (far southwest Algeria). In this study, we performed an evaluation of antibacterial activity of three macerates of two vegetative parts (seeds and stems) by two methods (disc and wells diffusion methods), with a description of the antibiotic resistance profile of isolated bacterial strains by antibiogram method.Results: According to the results, the antibiotic resistance profile of the tested bacterial strains showed an increased resistance against several antibiotics families. The evaluation of the antibacterial potential of macerates showed that methanolic and aqueous macerates of the seeds were more active against Gram-positive bacteria compared to Gram-negative bacteria.Conclusion: The preliminary results of this study allowed us to predict that natural substances in the plant can be considered as an important source to possess compounds with significant antibacterial properties and thus suggest their application in the pharmaceutical industry.


2021 ◽  
Vol 14 (9) ◽  
pp. 839
Author(s):  
Nauman Nazeer ◽  
Juan Carlos Rodriguez-Lecompte ◽  
Marya Ahmed

This study involves the design and development of disulfide bridge-linked antimicrobial peptides using the host defense protein Angiogenin 4 (chAng4) as a template. The mini peptides derived from chAng4 (mCA4s) were evaluated for their antibacterial efficacies in various pathogenic bacterial strains, and the role of the oxidation state of thiols in the peptide sequence and its implication on antibacterial properties were explored. A remarkable property of these synthetic mCA4 peptides is their capability to flocculate bacteria and mediate bacterial-specific killing, in the absence of any other external stimulus. mCA4s were further evaluated for their cellular uptake, hemolytic activities, toxicities, and immunomodulatory activities in different eukaryotic cell lines. The results indicate that disulfide bridge-containing cationic amphipathic peptides show superior antibacterial efficacies, are nontoxic and nonhemolytic, and mediate bacterial flocculation and killing, in the absence of external stimuli.


2016 ◽  
Vol 5 (12) ◽  
pp. 5138
Author(s):  
Shyamji Shukla* ◽  
Priyanka Soni ◽  
Harish K. Kewat

There is an alarming increase in the problem of resistance towards antibiotics amongst most of the pathogenic bacterial strains in recent years. This has drawn the attention of researchers around the world to search for novel and eco-friendly antibacterial compounds. Several biological sources have been explored in this respect but medicinal plants have taken a centre stage out of all. Plants have been known as a reservoir of number of bioactive compounds specially the antibacterial ones since time immemorial. Therefore, the present investigation was undertaken to analyze the antibacterial potential of the medicinal plant Achyranthes aspera. This study revealed that highest antibacterial activity was observed in the methanolic extract of stem against almost all test Bacteria. It showed maximum activity against E.coli (30 mm), followed by S. aureus (28 mm), Enterococcus sp.(25mm), Salmonella typhi ( 20 mm) and least activity was recorded in same extract against K.pneumoniae (6 mm). Four phytochemicals were screened in various solvent extracts. They are alkaloid, flavonoids, saponins and tannins.


2021 ◽  
Vol 16 (1) ◽  
pp. 1934578X2098774
Author(s):  
Jinpeng Zou ◽  
Yang Liu ◽  
Ruiwei Guo ◽  
Yu Tang ◽  
Zhengrong Shi ◽  
...  

The drug resistance of Pseudomonas aeruginosa is a worldwide problem due to its great threat to human health. A crude extract of Angelica dahurica has been proved to have antibacterial properties, which suggested that it may be able to inhibit the biofilm formation of P. aeruginosa; initial exploration had shown that the crude extract could inhibit the growth of P. aeruginosa effectively. After the adaptive dose of coumarin was confirmed to be a potential treatment for the bacteria’s drug resistance, “coumarin-antibiotic combination treatments” (3 coumarins—simple coumarin, imperatorin, and isoimperatorin—combined with 2 antibiotics—ampicillin and ceftazidime) were examined to determine their capability to inhibit P. aeruginosa. The final results showed that (1) coumarin with either ampicillin or ceftazidime significantly inhibited the biofilm formation of P. aeruginosa; (2) coumarin could directly destroy mature biofilms; and (3) the combination treatment can synergistically enhance the inhibition of biofilm formation, which could significantly reduce the usage of antibiotics and bacterial resistance. To sum up, a coumarin-antibiotic combination treatment may be a potential way to inhibit the biofilm growth of P. aeruginosa and provides a reference for antibiotic resistance treatment.


Marine Drugs ◽  
2021 ◽  
Vol 19 (2) ◽  
pp. 83
Author(s):  
Alfredo García-de-Vinuesa ◽  
Montserrat Demestre ◽  
Arnau Carreño ◽  
Josep Lloret

Although knowledge of the bioactive compounds produced by species inhabiting coastal waters is increasing, little is known about the bioactive potential produced by marine species occupying deeper habitats with high biodiversity and productivity. Here, we investigate about the bioactive potential of molecules produced by species that inhabit the crinoid beds, a poorly known essential fish habitat affected by trawling, wherein large amounts of commercial and noncommercial species are discarded. Based on a trawl survey conducted in 2019, 14% of the 64 species discarded on crinoid beds produce molecules with some type of bioactive potential, including; soft corals (Alcyonium palmatum); tunicates (Ascidia mentula); bony fish, such as horse mackerel (Trachurus trachurus); European hake (Merluccius merluccius); and chondrichthyans, such as small-spotted catshark (Scyliorhinus canicula). In addition, 16% of the discarded species had congeneric species that produce compounds with bioactive potential, indicating that such species might also possess similar types of bioactive molecules. Molecules with antioxidant, antitumour, antihypertensive, and antibacterial properties were the most frequent, which could provide the basis for future research aiming to discover new marine-based drugs and compounds for other human uses. Among all species or genera that produce compounds with bioactive potential, 68% presented medium or high vulnerability to trawling. Results show that the discarded catch contains many species, which produce different bioactive compounds that represent an added-value resource. These results highlight the importance of manage properly crinoid beds, to ensure that species that produce molecules with bioactive potential inhabiting these habitats are protected.


Author(s):  
Inna V. Fadeeva ◽  
Margarita A. Goldberg ◽  
Ilya I. Preobrazhensky ◽  
Georgy V. Mamin ◽  
Galina A. Davidova ◽  
...  

AbstractFor bone replacement materials, osteoconductive, osteoinductive, and osteogenic properties are desired. The bacterial resistance and the need for new antibacterial strategies stand among the most challenging tasks of the modern medicine. In this work, brushite cements based on powders of Zinc (Zn) (1.4 wt%) substituted tricalcium phosphate (β-TCP) and non-substituted β-TCP were prepared and investigated. Their initial and final phase composition, time of setting, morphology, pH evolution, and compressive strength are reported. After soaking for 60 days in physiological solution, the cements transformed into a mixture of brushite and hydroxyapatite. Antibacterial activity of the cements against Enterococcus faecium, Escherichia coli, and Pseudomonas aeruginosa bacteria strains was attested. The absence of cytotoxicity of cements was proved for murine fibroblast NCTC L929 cells. Moreover, the cell viability on the β-TCP cement containing Zn2+ ions was 10% higher compared to the β-TCP cement without zinc. The developed cements are perspective for applications in orthopedics and traumatology.


2021 ◽  
Vol 11 (9) ◽  
pp. 4315
Author(s):  
Emanuel Vamanu ◽  
Laura Dorina Dinu ◽  
Cristina Mihaela Luntraru ◽  
Alexandru Suciu

Bioactive compounds and phenolic compounds are viable alternatives to antibiotics in recurrent urinary tract infections. This study aimed to use a natural functional product, based on the bioactive compounds’ composition, to inhibit the uropathogenic strains of Escherichia coli. E. coli ATCC 25922 was used to characterize the IVCM (new in vitro catheterization model). As support for reducing bacterial proliferation, the cytotoxicity against a strain of Candida albicans was also determined (over 75% at 1 mg/mL). The results were correlated with the analysis of the distribution of biologically active compounds (trans-ferulic acid-268.44 ± 0.001 mg/100 g extract and an equal quantity of Trans-p-coumaric acid and rosmarinic acid). A pronounced inhibitory effect against the uropathogenic strain E. coli 317 (4 log copy no./mL after 72 h) was determined. The results showed a targeted response to the product for tested bacterial strains. The importance of research resulted from the easy and fast characterization of the functional product with antimicrobial effect against uropathogenic strains of E. coli. This study demonstrated that the proposed in vitro model was a valuable tool for assessing urinary tract infections with E. coli.


Biomedicines ◽  
2021 ◽  
Vol 9 (2) ◽  
pp. 210
Author(s):  
Arleta Waszczykowska ◽  
Dominik Żyro ◽  
Justyn Ochocki ◽  
Piotr Jurowski

The use of silver preparations in medicine is becoming increasingly popular. The basic aim of this evaluation was to review the literature on the clinical (in vivo) and antibacterial potential of silver preparations in ophthalmic diseases. The second goal was to summarize the results of experimental research on the use of silver preparations in ophthalmology. The third objective was to present a method for stabilizing eye drops containing silver (I) complex. Analysis of the pH stability of the silver (I) complex with metronidazole in the prepared dosage form (eye drops) was carried out. Most silver preparations are clinically used for topical application. Few experimental results indicate the usefulness of intraocular or systemic administration of silver (I) preparations as an alternative or additional therapy in infectious and angiogenic eye diseases. The development of a new formulation increases the stability of the dosage form. New forms of silver (I) products will certainly find application in the treatment of many ophthalmic diseases. One of the most important features of the silver (I) complex is its capacity to break down bacterial resistance. The new eye drops formula can significantly improve comfort of use. Due to their chemical nature, silver (I) compounds are difficult to stabilize, especially in the finished dosage form.


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