In Vitro and In Vivo Bioactivity of Tricalcium Phosphate and Fluoroapatite Nanoparticles for Medical Implants

2020 ◽  
Vol 12 (1) ◽  
pp. 101-109
Author(s):  
H. Algarni ◽  
Ibrahim Alshahrani ◽  
Essam H. Ibrahim ◽  
Refaat A. Eid ◽  
Mona Kilany ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Activities ◽  
Potential Candidate ◽  
Medical Implants ◽  
Splenic Cells ◽  
Acute Cytotoxicity ◽  
Good Potential ◽  
Sbf Solution

A novel 40P2O5–20Na2O–10Ca(OH)2–20CaCl2–6.0ZnO–2.0BaF2–2.0TiO2 (BGBaFTi) bioglasses is prepared. The reaction of the glasses in SBF solution is characterized by XRD and SEM indicated that the carbonate hydroxyapatite has formed rapidly on the glasses. BGBaFTi bioglasses was tested for its antimicrobial activity, anti-proliferative/cytotoxicity against normal and activated splenic cells in vitro and in vivo. This results showed that BGBaFTi has antimicrobial activities against Gram negative and positive bacteria as well as fungi. We found that the antimicrobial activity of nanoparticles of BGBaFTI is high than the normal powder of it. Moreover BGBaFTi (powder and nanoparticle) with cytotoxic effect on normal splenic cells was investigated. The products of activated splenic cells did not cause any changes in the structure of BGBaFTi. It did not cause any acute cytotoxicity or lysis to RBCs which was not affected by lytic products of immune cells. The bioactivity and biocompatibility of the present glasses use it a good potential candidate in the field of tissue engineering.

Synthesis of Novel 3(N,N-dialkylamino)alkyl/phenyl Substituted Thieno [2,3-d]pyrimidinones as H1-Anti-Histaminic and Antimicrobial Agents

2019 ◽  
Vol 15 (1) ◽  
pp. 63-70
Author(s):  
Shiv Dev Singh ◽  
Arvind Kumar ◽  
Firoz Babar ◽  
Neetu Sachan ◽  
Arun Kumar Sharma
Keyword(s):  
Antimicrobial Activity ◽  
Potassium Hydroxide ◽  
Antimicrobial Agents ◽  
Pyrimidine Ring ◽  
Antimicrobial Activities ◽  
Screening Methods ◽  
Chlorpheniramine Maleate ◽  
In Vivo Screening

Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial activity. Objective: Synthesis of novel 3(N,N-dialkylamino)alkyl/phenyl substituted thieno[2,3-d]pyrimidinones as H1-anti-histaminic and antimicrobial agents. Methods: A series of 3-[(N,N-dialkylamino)alkyl/phenyl]-2-(1H)thioxo-5,6,7,8-tetrahydrobenzo(b) thieno(2,3-d)pyrimidine-4(3H)-ones[4a-d], their oxo analogous [5a-d] and 3-[(N,N-dialkylamino)alkyl]- 2-chlorophenyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidine- 4 (3H)-ones[6a-d]derivative were synthesized from 2-amino-4,5,6,7-tetrahydrobenzo(b)thiophene-3-carboxylic acid by nucleophilic substitution of different N,N-dialkyl alkylene/phenylene diamines on activated 3-acylchloride moiety followed by cyclocondensation with carbon disulfide and ethanolic potassium hydroxide to get [4a-d] and in second reaction by condensation with 4-chlorobenzoyl chloride to get [6a-d] by single pot novel innovative route. The oxo analogous [5a-d] were prepared by treating derivatives [4a-d] with potassium permagnate in ethanolic KOH. The synthesized compound were evaluated for H1-antihistaminic and antimicrobial activities. Results: All synthesized compounds exhibited significant H1-antihistaminic activity by in vitro and in vivo screening methods and data were verified analytically and statistically. The compound 4a, 4b, 5a and 5b showed significant H1-antihistaminiic activity than the reference standard chlorpheniramine maleate. The compound 6d, 6c, 5c and 4c exhibited significant antimicrobial activity.

scholarly journals DESIGN AND SYNTHESIS OF NOVEL 1-((DIMETHYLAMINO)METHYL)-3-(4-(3-(SUBSTITUTE DPHENYL)-4-OXOTHIAZOLIDIN-2-YL)PHENYLIMINO)-5-NITROINDOLIN-2-ONES AS POTENT ANTITUBERCULAR AGENTS

2019 ◽  
pp. 200-207
Author(s):  
KOSARAJU LAHARI ◽  
RAJA SUNDARARAJAN
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Mannich Bases ◽  
Proton Nuclear Magnetic Resonance ◽  
Design And Synthesis ◽  
Group Variation

Objective: Isatins have emerged as antimicrobial agents due to their broad spectrum of in vitro and in vivo antimicrobial activities. In addition, thiazolidinone also reported to possess various biological activities particularly antimicrobial activity. Due to the importance, we planned to synthesize compounds with isatin functionality coupled with thiazolidinone as possible antitubercular and antimicrobial agents which could furnish better therapeutic results. Methods: In vitro Mycobacterium tuberculosis method and agar streak dilution test are used to estimate antitubercular and antimicrobial potency of title analogs, respectively. Minimum inhibitory concentration of entire title compounds was determined against all tested microorganism such as M. tuberculosis, four Gram-positive, three Gram-negative bacteria, and two fungi. Results: A series of new thiazolidinone substituted Schiff and Mannich bases of 5-nitroisatins were designed and synthesized by a multistep synthesis from isatin. Structures of synthesized compounds are characterized using Fourier-transform infrared, proton nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis. Mild to good antitubercular and antimicrobial activity was showed by synthesized 5-nitroisatin analogs. The relationship between the biological activity and the functional group variation of the tested compounds was discussed. Conclusion: 3-(4-(3-(4-Aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethyl amino)methyl)-5-nitroindolin-2-one 6 and 3-(4-(3- (2-aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethylamino)methyl)-5-nitroindolin-2-one 13 were found to be the most potent compounds of this series which might be extended as a novel class of antimicrobial agents.

scholarly journals The Pomegranate: Effects on Bacteria and Viruses That Influence Human Health

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Amy B. Howell ◽  
Doris H. D'Souza
Keyword(s):  
Antimicrobial Activity ◽  
Foodborne Pathogens ◽  
Clinical Results ◽  
Multidrug Resistant ◽  
Antimicrobial Activities ◽  
Oral Bacteria ◽  
Resistant Bacteria ◽  
Wide Range

Pomegranates have been known for hundreds of years for their multiple health benefits, including antimicrobial activity. The recent surge in multidrug-resistant bacteria and the possibility of widespread global virus pandemics necessitate the need for additional preventative and therapeutic options to conventional drugs. Research indicates that pomegranates and their extracts may serve as natural alternatives due to their potency against a wide range of bacterial and viral pathogens. Nearly every part of the pomegranate plant has been tested for antimicrobial activities, including the fruit juice, peel, arils, flowers, and bark. Many studies have utilized pomegranate peel with success. There are various phytochemical compounds in pomegranate that have demonstrated antimicrobial activity, but most of the studies have found that ellagic acid and larger hydrolyzable tannins, such as punicalagin, have the highest activities. In some cases the combination of the pomegranate constituents offers the most benefit. The positive clinical results on pomegranate and suppression of oral bacteria are intriguing and worthy of further study. Much of the evidence for pomegranates’ antibacterial and antiviral activities against foodborne pathogens and other infectious disease organisms comes fromin vitrocell-based assays, necessitating further confirmation ofin vivoefficacy through human clinical trials.

Exploitation of the Antioxidant Potential of Geranium Macrorrhizum (Geraniaceae): Hepatoprotective and Antimicrobial Activities

2012 ◽  
Vol 7 (12) ◽  
pp. 1934578X1200701 ◽  
Author(s):  
Niko S. Radulović ◽  
Milan B. Stojković ◽  
Snežana S. Mitić ◽  
Pavle J. Randjelović ◽  
Ivan R. Ilić ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Plant Species ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
Antioxidant Potential ◽  
Human Pathogens ◽  
Methanol Extracts

In this study we evaluated in vitro (radical scavenging) and in vivo (hepatoprotective effect) antioxidant activities and antimicrobial properties of the extracts of the above- and underground parts of Geranium macrorrhizum L. (Geraniaceae), an ethnopharmacologically renowned plant species. The antioxidant activity and total phenol and flavonoid contents of four different solvent extracts were evaluated by seven different methods. The methanol extracts, administered i.p. to rats (120-480 mg/kg), were evaluated for hepatoprotective activity in a CCl4-induced hepatotoxicity model. The same extracts were tested for antimicrobial activity against seven bacterial and two fungal species. The administered methanol extracts with the highest antioxidant potential showed a significant dose-dependent hepatoprotective action against CCl4-induced liver damage in both decreasing the levels of liver transaminases and bilirubin and in reducing the extent of morphological malformations of the liver. The leaf methanol extract displayed a very strong antibacterial activity, especially against Staphylococcus aureus, with low minimal inhibitory and bactericidal concentrations. These results justify the frequent use of this plant species in folk medicine. Besides the known astringent effect, one can expect that the observed antimicrobial activity against several human pathogens contributes to the wound healing properties of this plant.

scholarly journals In Vivo Pharmacodynamics of β-Lactams/Nacubactam against Carbapenem-Resistant and/or Carbapenemase-Producing Enterobacter cloacae and Klebsiella pneumoniae in Murine Pneumonia Model

Antibiotics ◽  
2021 ◽  
Vol 10 (10) ◽  
pp. 1179
Author(s):  
Mao Hagihara ◽  
Hideo Kato ◽  
Toshie Sugano ◽  
Hayato Okade ◽  
Nobuo Sato ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Klebsiella Pneumoniae ◽  
Treatment Options ◽  
Enterobacter Cloacae ◽  
Antimicrobial Activities ◽  
Combination Therapies ◽  
Carbapenem Resistant ◽  
Combination Regimens

Carbapenem-resistant Enterobacterales (CRE) and carbapenemase-producing Enterobacterales (CPE) have become global threats. CRE− and CPE− derived infections have been associated with high mortality due to limited treatment options. Nacubactam is a β-lactamase inhibitor and belongs to the new class of diazabicyclooctane. The agent has an in vitro antimicrobial activity against several classes of β-lactamase-producing Enterobacterales. This study evaluated antimicrobial activity of combination therapies including β-lactams (aztreonam, cefepime, and meropenem) and nacubactam against four Enterobacter cloacae and six Klebsiella pneumoniae isolates with murine pneumonia model. Based on changes in bacterial quantity, antimicrobial activities of some regimens were assessed. Combination therapies including β-lactams (aztreonam, cefepime, and meropenem) with nacubactam showed enhanced antimicrobial activity against CRE E. cloacae (−3.70 to −2.08 Δlog10 CFU/lungs) and K. pneumoniae (−4.24 to 1.47 Δlog10 CFU/lungs) with IMP-1, IMP-6, or KPC genes, compared with aztreonam, cefepime, meropenem, and nacubactam monotherapies. Most combination therapies showed bacteriostatic (−3.0 to 0 Δlog10 CFU/lungs) to bactericidal (<−3.0 Δlog10 CFU/lungs) activities against CRE isolates. This study revealed that combination regimens with β-lactams (aztreonam, cefepime, and meropenem) and nacubactam are preferable candidates to treat pneumonia due to CRE and CPE.

scholarly journals Antioxidant and antimicrobial responses associated with in vitro salt stress of in vitro and in vivo grown Pistacia khinjuk stocks

2020 ◽  
Vol 48 (4) ◽  
pp. 1885-1900
Author(s):  
Emine AYAZ TİLKAT ◽  
Nesrin HAŞİMİ ◽  
İbrahim S. KURU ◽  
Veysel SÜZERER
Keyword(s):  
Antimicrobial Activity ◽  
Biological Activity ◽  
Antioxidant Activities ◽  
Leaf Explants ◽  
Antimicrobial Activities ◽  
Activity Level ◽  
Total Phenolic ◽  
Leaf Extracts

P. khinjuk Stocks, known as Bıttım or Buttum in Turkey, is a member of the Anacardiaceae family. The essential oil of khinjuk pistachio has been used to treat various illnesses because of their anti-inflammatory, anticancer, antipyretic, antibacterial, anthelmintic, antiviral effects in various folk medicines. At the same time, fruits of khinjuk pistachio are used as edible wild fruits. In this study, it was aimed to determine and compare the antibacterial, antioxidant activities and total phenolic and flavonoid amounts of different parts (root, stem and leaf explants) of in vivo (grown naturally) and in vitro derived khinjuk pistachio plants under salt (NaCl) stress. Ethanol extracted explants were used for performing biological and chemical parameters. According to the results, generally, in vivo samples shows higher antioxidant and antimicrobial activity besides the higher number of phenolic compounds than their counterparts in vitro. We have also determined that the biological activity of in vitro salt elicited explants was higher than in vitro control explants. Generally, both female and male in vivo samples have higher antioxidants (DPPH, ABTS, CUPRAC) and antimicrobial activities than in vitro samples. The various plant parts (root, stem, leaf) belonging to both in vivo and in vitro samples have different biological activity level. In terms of antimicrobial activity, female plant extracts are more active than all other tested extracts. As a result, although increased salinity values significantly reduced antimicrobial activity, it is determined that 100 mM NaCl applications to in vitro leaf extracts exhibited moderate antimicrobial activity against S. aureus and C. albicans.

scholarly journals ANTIMICROBIAL ACTIVITY OF CALLYSPONGIA DIFFUSA (MARINE SPONGE) ASSOCIATED ENDOPHYTIC BACTERIA L STRAINS

2017 ◽  
Vol 9 (7) ◽  
pp. 90
Author(s):  
Vijayanand B. Warad ◽  
Prasanna Habbu ◽  
Rajesh Shastri
Keyword(s):  
Antimicrobial Activity ◽  
Marine Sponge ◽  
Pathogenic Bacteria ◽  
Antimicrobial Activities ◽  
Bioactive Metabolites ◽  
Haemolytic Activity ◽  
Chloroform Fraction ◽  
Callyspongia Diffusa

Objective: To screen the antimicrobial activity Of Callyspongia Diffusa (Marine Sponge) Associated Endophytic Bacterial Strains.Methods: We have isolated endophytic bacterias CDB-1 and CDB-2 from marine sponge Callyspongia diffusa and identified as Pseudomonas taiwanensis strain and Lysinibacillussphaericus strain respectively by the phylogenetic analysis. Fractions of CDB-1 and CDB-2 were screened for in vitro and in vivo antimicrobial activities against pathogenic bacteria and mycobacterium tuberculosis H37 RV strain by Minimum Inhibitory Concentration (MIC) method.Results: The lowest MIC against Kleibesella pnumoniae, Escherichia coli and Enterococcus feacalis was found to be 0.2 µg/ml and 0.4 µg/ml respectively for CDB-2. A significant antifungal activity was observed against Candida albicans (0.2-0.8 µg/ml) and Aspergillus niger (0.2-0.4 µg/ml). Further, Chloroform fraction of CDB-1 and ethyl acetate fraction of CDB-2 have shown significant anti-tubercular activity against the tested organism with MIC of 6.25µg/ml. This was supported by in vivo antimicrobial activity against K. Pneumonia infection in mice and least haemolytic activity against erythrocytes was observed. Compared to chloramphenicol.Conclusion: In this study, we have reported the marine natural species offer a rich source of bioactive metabolites that can exploit to develop novel, useful and potential therapeutic agents.

scholarly journals Assessment of in vitro and in vivo Antimicrobial Activity of an Isonitrosomalononitrile Silver(I) Salt

2021 ◽  
Vol 3 (1) ◽  
Author(s):  
Colmont M ◽  
Brunel JM
Keyword(s):  
Antimicrobial Activity ◽  
Animal Model ◽  
Galleria Mellonella ◽  
Silver Salt ◽  
Antimicrobial Activities ◽  
Water Soluble ◽  
Gram Positive ◽  
Minimum Inhibitory Concentrations

The design and evaluation of antimicrobial activities of an isonitrosomalononitrile silver(I) salt was reported. This highly stable water-soluble silver salt shows Minimum Inhibitory Concentrations (MIC) values ranging from 0.15 to 5 µg/mL towards both sensitive and resistant Gram-positive and negative bacteria. Furthermore, this silver salt has been investigated for its ability to treat a S. aureus infected Galleria mellonella larvae animal model with promising results. Thus, our results demonstrated that 80% of the treated larvae survived after 24h with respect to 10% of the untreated ones, respectively.

scholarly journals High-throughput screening and rational design of biofunctionalized surfaces with optimized biocompatibility and antimicrobial activity

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Zhou Fang ◽  
Junjian Chen ◽  
Ye Zhu ◽  
Guansong Hu ◽  
Haoqian Xin ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
High Throughput ◽  
High Throughput Screening ◽  
Rational Design ◽  
Click Reaction ◽  
Reaction Times ◽  
Great Promise ◽  
Biomaterial Surfaces

AbstractPeptides are widely used for surface modification to develop improved implants, such as cell adhesion RGD peptide and antimicrobial peptide (AMP). However, it is a daunting challenge to identify an optimized condition with the two peptides showing their intended activities and the parameters for reaching such a condition. Herein, we develop a high-throughput strategy, preparing titanium (Ti) surfaces with a gradient in peptide density by click reaction as a platform, to screen the positions with desired functions. Such positions are corresponding to optimized molecular parameters (peptide densities/ratios) and associated preparation parameters (reaction times/reactant concentrations). These parameters are then extracted to prepare nongradient mono- and dual-peptide functionalized Ti surfaces with desired biocompatibility or/and antimicrobial activity in vitro and in vivo. We also demonstrate this strategy could be extended to other materials. Here, we show that the high-throughput versatile strategy holds great promise for rational design and preparation of functional biomaterial surfaces.

scholarly journals Targeting Toll-Like Receptor 2: Polarization of Porcine Macrophages by a Mycoplasma-Derived Pam2cys Lipopeptide

Vaccines ◽  
2021 ◽  
Vol 9 (7) ◽  
pp. 692
Author(s):  
Giulia Franzoni ◽  
Antonio Anfossi ◽  
Chiara Grazia De Ciucis ◽  
Samanta Mecocci ◽  
Tania Carta ◽  
...  
Keyword(s):  
Mhc Class Ii ◽  
Macrophage Polarization ◽  
Surface Protein ◽  
Antimicrobial Activities ◽  
Toll Like Receptor ◽  
Activation Markers ◽  
Class I Mhc ◽  
Toll Like Receptor 2

Toll-like receptor 2 (TLR2) ligands are attracting increasing attention as prophylactic and immunotherapeutic agents against pathogens and tumors. We previously observed that a synthetic diacylated lipopeptide based on a surface protein of Mycoplasma agalactiae (Mag-Pam2Cys) strongly activated innate immune cells, including porcine monocyte-derived macrophages (moMΦ). In this study, we utilized confocal microscopy, flow cytometry, multiplex cytokine ELISA, and RT-qPCR to conduct a comprehensive analysis of the effects of scalar doses of Mag-Pam2Cys on porcine moMΦ. We observed enhanced expression of activation markers (MHC class I, MHC class II DR, CD25), increased phagocytotic activity, and release of IL-12 and proinflammatory cytokines. Mag-Pam2Cys also upregulated the gene expression of several IFN-α subtypes, p65, NOS2, and molecules with antimicrobial activities (CD14, beta defensin 1). Overall, our data showed that Mag-Pam2Cys polarized porcine macrophages towards a proinflammatory antimicrobial phenotype. However, Mag-Pam2Cys downregulated the expression of IFN-α3, six TLRs (TLR3, -4, -5, -7, -8, -9), and did not interfere with macrophage polarization induced by the immunosuppressive IL-10, suggesting that the inflammatory activity evoked by Mag-Pam2Cys could be regulated to avoid potentially harmful consequences. We hope that our in vitro results will lay the foundation for the further evaluation of this diacylated lipopeptide as an immunopotentiator in vivo.

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