Molecules, Vol. 25, Pages 878: Antibacterial Activity and Pharmacokinetic Profile of a Promising Antibacterial Agent: 22-(2-Amino-phenylsulfanyl)-22-Deoxypleuromutilin

In this study, the effectiveness and safety of amphenmulin were further investigated. Amphenmulin showed excellent antibacterial activity against MRSA (minimal inhibitory concentration = 0.0156~8 µg/mL) and performed time-dependent growth inhibition and a concentration-dependent postantibiotic effect (PAE). Acute oral toxicity test in mice showed that amphenmulin was a practical non-toxic drug and possessed high security as a new drug with the 50% lethal dose (LD50) above 5000 mg/kg. The pharmacokinetic properties of amphenmulin were then measured. After intravenous administration, the elimination half-life (T1/2), total body clearance (Clβ), and area under curve to infinite time (AUC0→∞) were 1.92 ± 0.28 h, 0.82 ± 0.09 L/h/kg, and 12.23 ± 1.35 μg·h/mL, respectively. After intraperitoneal administration, the T1/2, Clβ/F and AUC0→∞ were 2.64 ± 0.72 h, 4.08 ± 1.14 L/h/kg, and 2.52 ± 0.81 μg·h/mL, respectively, while for the oral route were 2.91 ± 0.81 h, 6.31 ± 2.26 L/h/kg, 1.67 ± 0.66 μg·h/mL, respectively. Furthermore, we evaluated the antimicrobial activity of amphenmulin in an experimental model of MRSA wound infection. Amphenmulin enhanced wound closure and promoted the healing of wound, which inhibited MRSA bacterial counts in the wound and decreased serum ...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research

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ConclusionsThe recommendations provided in this document are intended to assist the clinician in optimizing vancomycin for the treatment of invasive MRSA infections in adult and pediatric patients. An AUC/MIC by broth microdilution (BMD) ratio of 400 to 600 (assuming MICBMD of 1 mg/L) should be advocated as the target to achieve clinical efficacy while improving patient safety for patients with serious MRSA infections. In such cases, AUC ‐guided dosing and monitoring is the most accurate and optimal way to manage vancomycin therapy.
Source: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy - Category: Drugs & Pharmacology Authors: Tags: Special Article Source Type: research
To evaluate nasal carriage, antibiotic susceptibility and molecular characteristics of methicillin-resistant Staphylococcus aureus (MRSA), as well as the risk factors of MRSA colonization, in human immunodeficien...
Source: BMC Infectious Diseases - Category: Infectious Diseases Authors: Tags: Research article Source Type: research
This cohort study evaluates the association of persistent Staphylococcus aureus colonization and household environmental contamination with recurrent skin and soft tissue infection in households with children with community-associated methicillin-resistant S aureus (MRSA) skin and soft tissue infection.
Source: JAMA Pediatrics - Category: Pediatrics Source Type: research
This study was conducted to determine the frequency of S. aureus nasal carriage in hemodialysis patients (HD) and health-care workers (HCW) at the main dialysis center of Bam city, located in southeast of Iran. In this cross-sectional study, a total of 52 nasal swabs were obtained from health-care workers and hemodialysis patients to detect methicillin-sensitive S. aureus (MSSA) isolates. The resistance to different antibacterial agents was determined by disk diffusion method. Also, Panton-Valentine Leukocidin (PVL) - encoding gene as well as Staphylococcal protein A (spa) type were determined. The nasal carriage rate of S...
Source: Pathogens and Global Health - Category: International Medicine & Public Health Tags: Pathog Glob Health Source Type: research
Abstract Polyketide-terpenoid hybrid compounds are one of the largest families of meroterpenoids, with great potential for drug development for resistant pathogens. Genome sequence analysis of secondary metabolite gene clusters of a phytopathogenic fungus, Bipolaris sorokiniana 11134, revealed a type I polyketide gene cluster, consisting of highly reducing polyketide synthase, non-reducing polyketide synthase, and adjacent prenyltransferase. MS- and UV-guided isolations led to the isolation of ten meroterpenoids, including two new compounds: 19-dehydroxyl-3-epi-arthripenoid A (1) and 12-keto-cochlioquinone A (2). ...
Source: Applied Microbiology and Biotechnology - Category: Microbiology Authors: Tags: Appl Microbiol Biotechnol Source Type: research
Planta Med DOI: 10.1055/a-1130-4856Recently, the isolation and elucidation of a series of polyhydroxyanthraquinones were reported from an organic extract of a solid phase culture of an endophytic fungus, Penicillium restrictum (strain G85). One of these compounds, ω-hydroxyemodin (1), showed promising quorum-sensing inhibition against clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) in both in vitro and in vivo models. The initial supply of 1 was 19 mg, and this amount needed to be scaled by a factor of 30 to 50 times, in order to generate material for further in vivo studies. To do so, ...
Source: Planta Medica - Category: Drugs & Pharmacology Authors: Tags: Original Papers Source Type: research
Abstract Staphylococcus aureus is the most common pathogen involved in skin infections worldwide, regardless of the patient's age, the climate or geographical area. The main skin clinical manifestations can be linked to a few toxins produced by the bacteria, which give rise to a rich and varied clinical spectrum. Panton Valentine leucocidin, exfoliatins, enterotoxins and toxin shock syndrome toxin 1 are the main toxins involved in most dermatological manifestations associated with S. aureus. Other less frequent cutaneous manifestations can occur in endocarditis, bacteraemia or related to a contiguity focus. Curren...
Source: Acta Dermato-Venereologica - Category: Dermatology Authors: Tags: Acta Derm Venereol Source Type: research
Publication date: Available online 22 March 2020Source: Clinical Epidemiology and Global HealthAuthor(s): Hadi Safdari, Ehsan Aryan, Hamid Sadeghian, Seyyedeh Fatemeh Shams, Mahdi Aganj
Source: Clinical Epidemiology and Global Health - Category: Epidemiology Source Type: research
This study shows that phosphonopeptides, including alafosfalin, may have a therapeutic role to play in an era of increasing antibacterial resistance.
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research
This study focuses on estimating the prevalence of MRSA in shrines, a place where human and animal interaction is frequent, sharing antibiotic-resistant bacteria, antibiotic-resistant genes, and diseases. A total of 120 environmental swabs were collected from targeted areas during the study period, March 2018 to May 2018. Staphylococcus aureus was identified by growth on mannitol salt agar (MSA), and MRSA by growth on mannitol salt agar containing 4 μg Oxacillin, Gram staining, and conventional biochemical test. Isolates of S. aureus were characterized by antibiotic susceptibility testing using the disc diffusion...
Source: International Journal of Microbiology - Category: Microbiology Tags: Int J Microbiol Source Type: research
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