Polymeric prodrugs for selective delivery to prostate tumours and heterocyclic isoform-selective inhibitors of nitric oxide synthase

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Knowledge, attitudes and behavior regarding antibiotics use and misuse among adults in the community of Jordan. A pilot study

AbstractFactors associated with antibiotic use, resistance and safety have been well recognized worldwide in the literature. Nevertheless, only few studies have been conducted in Jordan in this area. The aim of this study was to assess knowledge, behavior and attitude toward antibiotics use among adult Jordanians. The study represents a cross sectional survey using an interviewer administered questionnaire. Data collected from a random sample of 1141 adult Jordanians, recruited at different settings, regarding their knowledge about the effectiveness of, resistance toward, and self medications with antibiotics against bacterial, viral and parasitic diseases. 67.1% believed that antibiotics treat common cold and cough. 28.1% misused antibiotics as analgesics. 11.9% of females showed inadequate knowledge about the safe use of antibiotics during pregnancy and nursing. 28.5% kept antibiotics at home for emergency use and 55.6% use them as prophylaxis against infections. 49.0% use left-over antibiotics without physicians’ consultation while 51.8% use antibiotics based on a relative advice. 22.9% of physicians prescribe antibiotics over the phone and >50.0% routinely prescribe antibiotics to treat common cold symptoms.Our findings indicated that young adults showed unsatisfactory knowledge of proper antibiotic use. Therefore, there is an urge for educational programs using all media means

The validity of topical drug therapy for otitis media with effusion

Otitis media with effusion is difficult to diagnose, since the course of the disease is mostly asymptomatic, while the initial stage of the disease is very similar to Eustachiitis or the pre-perforative stage of acute otitis media. At this stage, dysfunction of the auditory tube and negative pressure in the tympanic cavity creates the conditions for the production of transudate, which clinically, in addition to hearing loss, is accompanied by soreness, a feeling of congestion, pressure, fluid transfusion in the ear. When conducting local medical procedures, they are primarily guided by the condition of the mucous membrane of the eustachian tube, nasopharynx and nasal cavity, but changes in the eardrum are no less important. Thus, the use of topical analgesics with an anti-inflammatory effect becomes no less relevant in the treatment.A literature review was carried out with an analysis of scientific research data on the use of a topical combination drug that has a local anesthetic and anti-inflammatory effect in the treatment of diseases of the external and middle ear.Analysis of the literature showed that the use of lidocaine-phenazone-containing drops promotes rapid regression of the inflammation in the external auditory canal and the tympanic membrane, as well as relieving of pain. It can be used both in children (including newborns) and in adults who are suffering from otitis media but with intact tympanic membrane, including otitis media with effusion.Combined topical drugs containing lidocaine-phenazone demonstrate efficacy and safety in the treatment of catarrhal and otitis media with effusion in all age groups

Rapid Colorimetric Detection of Pseudomonas aeruginosa in Clinical Isolates Using a Magnetic Nanoparticle Biosensor

A rapid, sensitive, and specific colorimetric biosensor based on the use of magnetic nanoparticles (MNPs) was designed for the detection of Pseudomonas aeruginosa in clinical samples. The biosensing platform was based on the measurement of P. aeruginosa proteolytic activity using a specific protease substrate. At the N-terminus, this substrate was covalently bound to MNPs and was linked to a gold sensor surface via cystine at the C-terminus of the substrates. The golden sensor appears black to naked eyes because of the coverage of the MNPs. However, upon proteolysis, the cleaved peptide–MNP moieties will be attracted by an external magnet, revealing the golden color of the sensor surface, which can be observed by the naked eye. In vitro, the biosensor was able to detect specifically and quantitatively the presence of P. aeruginosa with a detection limit of 102 cfu/mL in less than 1 min. The colorimetric biosensor was used to test its ability to detect in situ P. aeruginosa in clinical isolates from patients. This biochip is anticipated to be useful as a rapid point-of-care device for the diagnosis of P. aeruginosa-related infections

DESIGN, SYNTHESIS AND BIOLOGICAL SCREENING OF AMINOACETYLENIC TETRAHYDROPHTHALIMIDE ANALOGUES AS NOVEL CYCLOOXYGENASE (COX) INHIBITORS

Objective: To design and synthesise a new amino acetylenic tetrahydro phthalimide derivative and investigate their selective inhibitory activity to COXs.Methods: Aminoacetylenic tetrahydro phthalimide derivatives were synthesised by alkylation of tetrahydro phthalimide with propargyl bromide afforded 2-(prop-2-yn-1-yl)-2,3,3a,4,7,7a-hexahydro-1H-isoindole-1,3-dione. The alkylated tetrahydro phthalimide was subjected to Mannich reaction afforded the desired amino acetylenic tetra phthalimide derivatives (AZ 1-6). The elemental analysis was indicated by the EuroEA elemental analyzer and biological characterization was via IR, 1H-NMR, [13]C-NMR, DSC was determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer and DMSO-d6 as a solvent, molecular docking was done using the Autodock Tool software (version 4.2). ChemBioDraw was used in the drawing of our schemes.Results: The IR, 1H-NMR, 13C-NMR, DSC and elemental analysis were consistent with the assigned structures. The designers of the compounds as COXs inhibitor activity were based on the nationalisation of the important criteria that provide effective inhibitory binding with COXs–receptor. The results indicated that the synthesised compounds (AZ1-6) showed a close similarity in the binding affinity to both COXs and may be more specific to COX-1. AZ-5 showed the highest % of inhibition for COX-1 even better than aspirin. Which may suggest that the aryl group is required for COX-2 inhibition.Conclusion: For the first time, we indicate the requirement of aromaticity in COX-2 structural inhibitory activity.Â

The relevance of topical drugs endaural use in otosurgical practice

Introduction. Preoperative, in particular, antiseptic, preparation of the external auditory canal (EAC) is an important issue for the otosurgeon to take in mind, especially with endaural approach.The aim of the study is to assess the skin microbiota of the EAC and the effectiveness of antiseptic treatment before endaural intervention.Materials and methods. A prospective study including 19 patients who underwent ear surgery by endaural approach: 10 stapedoplasty; 9 tympanoplasty. Ear swabs culture were taken from all the patients preoperatively and after removing the tamponade. Of the 10 patients with otosclerosis, 5 underwent skin preparation with 10% povidone iodine and a swab culture.Results. According to the microbiological examination results, Staphulacoccus Auricularis prevailed in the first smear - 52.6%. In 5 patients with otosclerosis, in comparison to the 1st swab: one case with absence of microorganisms growth, in the other 4 -decrease in the degree of contamination by half. In the 3rd swab, there was no growth in these patients and in the rest, who didn't undergo antiseptic preparation. Patients, without antiseptic preparation of the ear canal, after tympanoplasty (9 patients) in the second smear, had an increase of contamination (from 105 to 106 CFU/ml).Conclusions. Analysis of the microbiome before and after the operation revealed the growth of predominantly (94.7%) opportunistic microorganisms. Preoperative antiseptic preparation reduces the degree of contamination of the skin, which, in our opinion, prevents complications and improves the healing process

Rapid Colorimetric Detection of Pseudomonas aeruginosa in Clinical Isolates Using a Magnetic Nanoparticle Biosensor

A rapid, sensitive, and specific colorimetric biosensor based on the use of magnetic nanoparticles (MNPs) was designed for the detection of Pseudomonas aeruginosa in clinical samples. The biosensing platform was based on the measurement of P. aeruginosa proteolytic activity using a specific protease substrate. At the N-terminus, this substrate was covalently bound to MNPs and was linked to a gold sensor surface via cystine at the C-terminus of the substrates. The golden sensor appears black to naked eyes because of the coverage of the MNPs. However, upon proteolysis, the cleaved peptide-MNP moieties will be attracted by an external magnet, revealing the golden color of the sensor surface, which can be observed by the naked eye. In vitro, the biosensor was able to detect specifically and quantitatively the presence of P. aeruginosa with a detection limit of 102 cfu/mL in less than 1 min. The colorimetric biosensor was used to test its ability to detect in situ P. aeruginosa in clinical isolates from patients. This biochip is anticipated to be useful as a rapid point-of-care device for the diagnosis of P. aeruginosa-related infections

Synthesis of N-(Methoxycarbonylthienylmethyl)thioureas and Evaluation of Their Interaction with Inducible and Neuronal Nitric Oxide Synthase

Two isomeric N-(methoxycarbonylthienylmethyl)thioureas were synthesised by a sequence of radical bromination of methylthiophenecarboxylic esters, substitution with trifluoroacetamide anion, deprotection, formation of the corresponding isothiocyanates and addition of ammonia. The interaction of these new thiophene-based thioureas with inducible and neuronal nitric oxide synthase was evaluauted. These novel thienylmethylthioureas stimulated the activity of inducible Nitric Oxide Synthase (iNOS)