rifampin and 1-1-diphenyl-2-picrylhydrazyl

Surgical sutures are vulnerable to bacterial infections and biofilm formation. At the suture site, pain and undesirable, excess inflammation are additionally detrimental to wound healing. The development of a polymerized cyclodextrin (pCD) coated surgical suture introduces the capability to locally deliver both anti-inflammatory and anti-microbial drugs throughout the phases of acute and chronic healing. Local delivery allows for the improvement of wound healing while reducing related systemic side effects and drug resistance. Through testing, it has been shown that the fabrication of our pCD coating minimally affects the suture's mechanical properties. In vitro studies show measurable and consistent drug delivery for nearly 5 weeks. The therapeutic level of this delivery is sufficient to show inhibition of bacterial growth for 4 weeks, and free-radical scavenging (an in vitro anti-inflammatory activity approximation) for 2 weeks. With this pCD coating technique, we maintain clinical performance standards while also introducing a long-term dual delivery system relevant to the wound healing timeframe. © 2019 Wiley Periodicals, Inc. J Biomed Mater Res Part A, 2019.

Topics: Anti-Infective Agents; Anti-Inflammatory Agents; Biphenyl Compounds; Coated Materials, Biocompatible; Cyclodextrins; Drug Delivery Systems; Drug Liberation; Free Radical Scavengers; Microbial Sensitivity Tests; Picrates; Polymerization; Resveratrol; Rifampin; Solvents; Staphylococcus aureus; Sutures; Tensile Strength; Wound Healing

We investigated the prooxidant effects of bisphenol A (BPA) phenoxyl radicals in comparison with the phenoxyl radicals of 3-tert-butyl-4-hydroxyanisole (BHA), 2,6-di-tert-butyl-methylphenol (BHT) and 4-tert-butylphenol (TBP). The phenoxyl radicals, generated in situ by 1-electron oxidation of the corresponding phenol, were allowed to react with reduced nicotinamide adenine dinucleotide phosphate (NADPH) and rifampicin. The antioxidant activity of various phenols was examined based on the reduction of 2,2'-diphenyl-1-picrylhydrazyl radical (DPPH). It was found that the prooxidant activity of BPA phenoxyl radicals far exceeded those of BHA and BHT of phenoxyl radicals. Unlike Trolox, BPA showed minimal DPPH scavenging activity. The strong prooxidant properties of BPA phenoxyl radicals propelled us to study the markers of cellular oxidative stress in GT1-7 hypothalamic neurons exposed to BPA. It was observed that neuronal cells exposed to BPA had increased generation of intracellular peroxides and mitochondrial superoxide ([Formula: see text]). The formation of peroxides and [Formula: see text] were time- and dose-dependent and that co-incubation with N-acetyl-l-cysteine or Trolox greatly lowered their levels. The results of the present study are consistent with emerging evidence that human populations (non-institutionalized) having higher levels of urinary BPA also have increased levels of oxidative stress markers and are prone to higher risk of cardiovascular diseases, diabetes and abnormalities in hepatic enzymes.

Topics: Animals; Benzhydryl Compounds; Biphenyl Compounds; Butylated Hydroxyanisole; Butylated Hydroxytoluene; Cell Culture Techniques; Cell Line; Free Radicals; Mice; Mitochondria; Molecular Structure; NADP; Neurons; Oxidants; Oxidation-Reduction; Oxidative Stress; Peroxides; Phenols; Picrates; Rifampin; Superoxides

The antioxidant activities of different drugs like acetylsalicylic acid, nimesulide, dapsone, methlydopa, rifampicin and the well known antioxidants ascorbic acid and quercetin were assessed using the stable free radical alpha,alpha-diphenyl-beta-picrylhydrazyl (DPPH). DPPH is easily soluble at lower concentrations in methanol. It has a deep violet color. The changes in color are monitored calorimetrically. The measurements were made using HPLC at wavelengths 256 nm and 517 nm. The interactions between different drugs with DPPH were studied. All the compounds tested reduced DPPH. This method can be used to investigate oxygen free radical scavenging activity of drug candidates.

Topics: Antioxidants; Ascorbic Acid; Aspirin; Biphenyl Compounds; Chromatography, High Pressure Liquid; Dapsone; Free Radicals; Methyldopa; Picrates; Quercetin; Rifampin; Spectrophotometry, Ultraviolet; Sulfonamides

DPPH (alpha,alpha-diphenyl-beta-picryl hydrazyl) (CAS 217-591-8), a stable free radical can be used to determine the antioxidant activity (AOA) of some drugs. In the present study the DPPH method was used for the first time to test AOA of dapsone (CAS 80-08-0), clofazimine (CAS 2030-63-9) and rifampicin (CAS 13282-42-1) in vitro and deproteinated blood method. Ascorbic acid (CAS 50-81-7) was used as a control in the study, which showed concentration-dependent antioxidant activity. Rifampicin showed a per se effect but it showed concentration dependent decrease in the DPPH absorbance. Ascorbic acid, dapsone and rifampicin showed DPPH scavenging activity both in vitro and deproteinated blood method. Clofazimine did not have any influence on DPPH. This method may be extended to different drugs for testing their AOA in biological fluids.

Topics: Adult; Antioxidants; Ascorbic Acid; Bepridil; Biphenyl Compounds; Clofazimine; Dapsone; Humans; Leprostatic Agents; Male; Oxidation-Reduction; Picrates; Rifampin; Spectrophotometry, Ultraviolet