Feasibility of the use of Lentinula edodes mycelium in terbinafine remediation

A detailed understanding of the fate of xenobiotics introduced into the environment and the mechanisms involved in their biotransformation, biodegradation, and biosorption is essential to improve the efficiency of remediation techniques. Mycoremediation is a form of bioremediation technique that has become increasingly popular in recent years as fungi are known to produce various effective extracellular enzymes that have the potential to neutralize a wide variety of xenobiotics released into the environment. Hence, mycoremediation appears to be a promising technique for the removal of a wide array of toxins and pharmaceutical residues from a damaged environment and wastewater. This study primarily aimed to investigate whether white-rot fungus (Lentinula edodes) can be utilized for the bioremediation of common antifungal agent terbinafine, which is mainly available in the market as powder or cream. The cultures of L. edodes were cultivated in the medium containing terbinafine powder or terbinafine 1% cream, each at a final concentration of 0.1 mg mL−1. The addition of terbinafine in powder form have a negative effect on biomass growth (p < 0.05). The total amount of terbinafine in the dry weight of mycelium after culture was estimated to be 7.63 ± 0.45 mg and 12.52 ± 2.46 mg for powder and cream samples, respectively. In addition, there were no traces of terbinafine in any of the samples of medium used for culturing L. edodes after the experimental duration period. The biodegradation products of terbinafine were identified for the first time using UPLC/MS/MS. The biodegradation of terbinafine resulted in the loss of 1-naphthylmethanol, which occurred via oxidative deamination, N-demethylation, or tert-butyl group hydroxylation. The results of the study demonstrate that L. edodes mycelium can be effectively used for the remediation of terbinafine

Determination of fluconazole and its oxidation products with kinetic evaluation under potassium permanganate treatment in acidic solutions by ultra performance liquid chromatography-tandem mass spectrometry

For the determination of fluconazole (FLU) oxidation stability under permanganate treatment at the acidic pH, a sensitive, reproducible, and stability-indicating ultra-performance liquid chromatographyñmass spectrometry (UPLC/MS) method was developed. Three additional products (tR = 5.79, 6.98, 7.54) were observed besides the FLU (tR = 6.22). The proposed method was used to study the kinetics of FLU oxidative degradation. An oxidation process followed the kinetics of the second-order reaction. The degradation rate constant and the corresponding half-life obtained for the FLU oxidative degradation were 0.5626 h-1 and 16.69 h, respectively. The putative oxidation products were characterized and their fragmentation pathways, on a basis of MS/MS data, were proposed

Binding of 1-[3-(4-tert-butyl-phenoxy)propyl]piperidine, a new non imidazole histamine H3 receptor antagonist to bovine serum albumin

The degree of binding of a drug to plasma proteins has a significant effect on its distribution, elimination, and pharmacological effect since only the unbound fraction is available for distribution into extra-vascular space. The binding of DL76 (1-[3-(4-tert-butyl-phenoxy)propyl]piperidine) to bovine serum albumin (BSA) was studied in vitro by equilibrium dialysis at 37OC and pH 7.4 over the concentration range of 0.32ñ317.18 μM and at a physiological protein concentration of 602 μM. Drug concentrations were determined by validated LC/MS/MS method. Nonlinear regression analyses of the data pointed to a single class of binding sites (m = 1) with a dissociation constant of DL76 equal 49.20 μM. Scatchard plot concave-down curve might indicate positive cooperativity, which was confirmed by the Hill plot with the slope higher than one

Determination of "in vitro" metabolism of a new non-imidazole histamine H3 receptor antagonist 1-[3-(4-tert-butylphenoxy) propyl]piperidine

Early understanding of the pharmacokinetics of drug candidates is essential during the evaluation of drug development process. DL76 1-[3-(4-tert-butylphenoxy)propyl]piperidine is a novel promising non-imidazole H3 receptor antagonist. The presented study was undertaken to compare with each other the predicted hepatic clearance values of DL76 calculated, using two most common mathematical models ìwell-stirredî and ìparallel tubeî, based on the data obtained in in vitro experiments. The metabolic intrinsic clearance of DL76 equaled to 0.4848 mL/min/mg protein was scaled up and the values of hepatic clearance estimated from ìwellstirredî and ìparallel tubeî models were 55.47 mL/min/kg and 58.80 mL/min/kg, respectively. They were further compared with pharmacokinetic parameters calculated based on the concentration-time profile obtained following intravenous administration of DL76 to rats at the dose of 6 mg/kg. The estimated systemic serum clearance value of 144.5 mL/h/kg and blood clearance value of 81.17 mL/min/kg indicate the potential extrahepatic metabolism of the investigated compound. This study demonstrates the utility of rat liver microsomes for the prediction of DL76 hepatic clearance

Semiautomatic and fully functional electrochemical microanalyzer BO-05 suitable for scientific, didactic, and analytical applications : the use in the potentiometric analysis of drugs

This article presents the potentiometric method of determination of chlorides using the original BO-05 electrochemical microanalyzer. The quantification of chlorides is one of the frequently performed methods, both in the indirect determination of active pharmaceutical ingredients (API) and impurities in pharmaceutical raw materials, pharmacopoeial substances or pharmaceutical formulations as well. Successfully validated method was used to the analysis of chlorides in the preparations containing verapamil hydrochloride in form of tablets Staveran® and Verapamil® . The mean content of the studied API calculated to one tablet was close to the declared and equal to 123.6±1.5 mg and 122.6±1.1 mg, respectively. The presence of excipients have no significant impact on the final results. Thus shown that the electrochemical microanalyzer BO-05 is suitable for scientific, didactic and analytical applications

Semiautomatic and fully functional electrochemical microanalyzer BO-05 suitable for scientific, didactic, and analytical applications: The use in the potentiometric analysis of drugs

This article presents the potentiometric method of determination of chlorides using the original BO-05 electrochemical microanalyzer. The quantification of chlorides is one of the frequently performed methods, both in the indirect determination of active pharmaceutical ingredients (API) and impurities in pharmaceutical raw materials, pharmacopoeial substances or pharmaceutical formulations as well. Successfully validated method was used to the analysis of chlorides in the preparations containing verapamil hydrochloride in form of tablets Staveran® and Verapamil®. The mean content of the studied API calculated to one tablet was close to the declared and equal to 123.6±1.5 mg and 122.6±1.1 mg, respectively. The presence of excipients have no significant impact on the final results. Thus shown that the electrochemical microanalyzer BO-05 is suitable for scientific, didactic and analytical applications