This study was conducted to evaluate the degradation of aromatic dyes and the production of ligninolytic enzymes by 10 white rot fungi. The results of this study revealed that Pycnoporus cinnabarinus, Pleurotus pulmonarius, Ganoderma lucidum, Trametes suaveolens, Stereum ostrea and Fomes fomentarius have the ability to efficiently degrade congo red on solid media. However, malachite green inhibited the mycelial growth of these organisms. Therefore, they did not effectively decolorize malachite green on solid media. However, P. cinnabarinus and P. pulmonarius were able to effectively decolorize malachite green on solid media. T. suaveolens and F. rosea decolorized methylene blue more effectively than any of the other fungi evaluated in this study. In liquid culture, G. lucidum, P. cinnabarinus, Naematoloma fasciculare and Pycnoporus coccineus were found to have a greater ability to decolorize congo red. In addition, P. cinnabarinus, G. lucidum and T. suaveolens decolorized methylene blue in liquid media more effectively than any of the other organisms evaluated in this study. Only F. fomentarius was able to decolorize malachite green in liquid media, and its ability to do so was limited. To investigate the production of ligninolytic enzymes in media containing aromatic compounds, fungi were cultured in naphthalene supplemented liquid media. P. coccineus, Coriolus versicolor and P. cinnabarinus were found to produce a large amount of laccase when grown in medium that contained napthalene.
Coloring Agents ; Congo Red ; Coriolaceae ; Fungi ; Humans ; Laccase ; Methylene Blue ; Naphthalenes ; Ostrea ; Pleurotus ; Pycnoporus ; Reishi ; Rosaniline Dyes ; Trametes

OBJECTIVETo study albumin adduct with naphthalene metabolites, namely 1,2-naphthoquinone (1,2-NPQ) and 1,4-naphthoquinone (1,4-NPQ), as a potential biomarker for intermediate/long-term exposure to polycyclic aromatic hydrocarbons (PAH) in coke oven workers.

METHODSTwenty-eight coke oven workers and 22 control workers were recruited from a cokery. Spot urine and venous blood samples were collected from the workers after four continuously working days and personal information was obtained by questionnaire. Plasma albumin adduct was detected with gas chromatography-mass spectrometry.

RESULTSAlbumin adduct with 1,2- & 1,4-NPQ (1,2-NPQ and 1,4-NPQ), respectively, were detected in all coke oven workers and controls. Median plasma level of 1,2-NPQ-Alb in coke oven workers was significantly higher than that in controls (76.6 pmol/g vs. 44.9 pmol/g, P < 0.01). However, there was no significant difference in plasma median level of 1,4-NPQ-Alb between the two groups (48.6 pmol/g vs. 44.2 pmol/g, P > 0.05). Plasma level of 1,2-NPQ-Alb was significantly higher than that of 1,4-NPQ-Alb in coke oven workers. Urine levels of naphthalene, 1-naphthol, 2-naphthol and 1-pyrenol in coke oven workers correlated significantly with their plasma level of 1,2-NPQ-Alb (Pearson coefficient of correlation greater than 0.371, P < 0.01), but did not do significantly with 1,4-NPQ-Alb.

CONCLUSIONPlasma level of 1,2-NPQ-Alb could effectively reflect their magnitude of personal internal dose of exposure to air PAH, so it could be used as a potential biomarker to evaluate their intermediate/long-term exposure to PAH in coke oven workers.

Air Pollutants, Occupational ; adverse effects ; Albumins ; Biomarkers ; blood ; Coke ; DNA Adducts ; Humans ; Male ; Naphthalenes ; metabolism ; Naphthoquinones ; blood ; Occupational Exposure

BACKGROUND: A fixed-dose combination gel with adapalene 0.1% and benzoyl peroxide (BPO) 2.5% has been developed for once-daily treatment of acne. It is known to be effective to reduce inflammatory and non-inflammatory lesions, but there have been no study in Korean yet. OBJECTIVE: The aim of this study was to evaluate the efficacy and safety of adapalene 0.1%-BPO 2.5% fixed-dose combination gel (adapalene-BPO) for the treatment of mild to moderate severity acne in Korean. METHODS: In total, 64 patients with mild to moderate severity acne were enrolled. Adapalene-BPO was applied to face once daily at night. The efficacy assessment was performed at baseline and monthly for 3 months: inflammatory lesions (IL), non-inflammatory lesions (NIL), total lesions (TL) were counted and median percentage changes of each lesion were measured for 3 months with patient satisfaction and adverse events questionnaire. RESULTS: Of the 64 patients enrolled, 58 have completed 3-month treatments. Adapalene-BPO showed early onset of action with significant reduction in inflammatory, non-inflammatory, and total lesion counts. The median percentage reduction of mild group from baseline to 3rd month was greater than moderate group in IL, NIL, and TL counts (71.1% vs 65%/61.4% vs 56.4%/67.7% vs 62% reduction). Also, patient satisfaction score improved and significant reduction of Korea Acne Grading System (KAGS) was noted in both groups. All the reported adverse events were mild. CONCLUSION: This study shows that adapalene-BPO is an effective and safe treatment regimen for both mild and moderate acne. It has a better effect for treating mild severity acne than moderate acne with reduction of the IL, NIL, and TL counts and greater patient satisfaction.
Acne Vulgaris ; Benzoyl Peroxide ; Humans ; Korea ; Naphthalenes ; Patient Satisfaction ; Adapalene

Highly reactive zinc metal was prepared by electrolysis of a N,N-dimethylformamide (DMF) solution containing naphthalene and a supporting electrolyte in a one-compartment cell fitted with a platinum cathode and a zinc anode. This highly reactive electrogenerated zinc (EGZn/Naph) was used for transformation of ethyl 2-bromoacrylate into the corresponding organozinc compound, which can not be achieved by the use of usual zinc metals. Reaction of the organozinc compounds thus prepared with various aryl halides in the presence of 5 mol% of palladium catalyst gave the corresponding cross-coupling products in high yields. These cross-coupling reactions were successfully applied to a synthesis of the precursor of anti-inflammatory agents such as ibuprofen, naproxen, cicloprofen and suprofen.
Anti-Inflammatory Agents, Non-Steroidal/*chemical synthesis ; Catalysis ; Electrolysis ; Ibuprofen/chemical synthesis ; Naphthalenes ; Naproxen/chemical synthesis ; Prodrugs/*chemical synthesis ; Propionic Acids/chemical synthesis ; Suprofen/chemical synthesis ; Zinc/*pharmacology

Simvastatin, a semisynthetic derivertive of lovastatin, is an important drug for the treatment of hypercholesteromia, and is traditionally prepared by direct alkylation of lovastatin. Chemical reaction conditons are very rigid, and the final product is difficult to purify, also the pressure of labor protection and environment protection is very high. Recently, with the devolpement in the research of lovastatin biosynthesis, more and more attention has been paid to simvastatin biosynthesis. This paper compared the chemical and biological routes in simvastatin production. Simvastatin could be produced by direct fermentation with combinational biosynthesis method, and could also be synthesized from monacolin J with acyltransferase LovD.
Acyltransferases ; genetics ; metabolism ; Anticholesteremic Agents ; metabolism ; Catalysis ; Escherichia coli ; genetics ; metabolism ; Fermentation ; Lovastatin ; analogs & derivatives ; biosynthesis ; Naphthalenes ; metabolism ; Simvastatin ; metabolism ; Transformation, Bacterial

AIMTo study the metabolites of R, S-1-(2-methoxypheyl)-4-[3-(naphthal-yl-oxy)-2-hydroxypropyl] -piperazine, (naftopidil, NAF), a novel antihypertensive drug in rat plasma.

METHODSThe rat plasma samples were analyzed by LC/MS after oral administration of NAF. According to MS relativity of metabolites and parent compound (NAF) and metabolic rule of compound with similar structure, the structure of potential metabolites were postulated. Phase I metabolites were identified by HPLC/MS and by comparison with authentic standards, phase II conjugates were indirectly identified with beta-D-glucuronidase in presence or absence of glucuronidase selective inhibitor D-saccharric acid beta-1,4-Lactone.

RESULTSPhase I metabolites desmethyl-naftopidil (DMN), (phenyl) hydroxynaftopidil (PHN), (naphthyl) -hydroxy-naftopidil (NHN) were separated and identified in rat plasma by comparison with reference substances, phase II conjugates, NAF and NHN glucuronide conjugates were separated and tentatively identified by hydrolysis with glucuronidase, the aglycones, NAF and NHN, were identified in rat plasma.

CONCLUSIONThe major metabolic pathway of NAF in rat plasma should be the hydroxylation of the phenyl or nephthyl moiety of NAF and demethylation of NAF. Therefore, (naphthyl) hydroxyl-metabolite and NAF followed by conjugation with beta-glueuronic acid.

Animals ; Antihypertensive Agents ; blood ; metabolism ; Chromatography, High Pressure Liquid ; Gas Chromatography-Mass Spectrometry ; Male ; Naphthalenes ; blood ; metabolism ; Naphthols ; blood ; metabolism ; Piperazines ; blood ; metabolism ; Rats ; Rats, Sprague-Dawley

Air ; analysis ; Chromatography, Gas ; methods ; Naphthalenes ; analysis ; Workplace

[Ca2+]i transients by reverse mode of cardiac Na+/Ca2+ exchanger (NCX1) were recorded in fura-2 loaded BHK cells with stable expression of NCX1. Repeated stimulation of reverse NCX1 produced a long-lasting decrease of Ca2+ transients ('rundown'). Rundown of NCX1 was independent of membrane PIP2 depletion. Although the activation of protein kinase C (PKC) was observed during the Ca2+ transients, neither a selective PKC inhibitor (calphostin C) nor a PKC activator (PMA) changed the degrees of rundown. By comparison, a non-specific PKC inhibitor, staurosporine (STS), reversed rundown in a dose-dependent and reversible manner. The action of STS was unaffected by pretreatment of the cells with calphostin C, PMA, or forskolin. Taken together, the results suggest that the stimulation of reverse NCX1 by STS is independent of PKC and/or PKA inhibition.
Forskolin ; Fura-2 ; Membranes ; Naphthalenes ; Protein Kinase C ; Staurosporine

Human ; Female ; Adult ; Lacquer ; Morpholines ; Nails ; Naphthalenes ; Onychomycosis ;

We have developed a rapid and high throughput lipase-ANS (8-Anilino-l-naphthalenesulfonic acid) assay to evaluate the thermo-stability of lipases based on the ANS fluorescence signal's increasing and shifting when this small fluorescence probes binds to lipase. The testing lipase samples were incubated at a temperature range of 25 degrees C to 65 degrees C for 30 min before mixed with ANS solution (0.20 mg/mL lipase and 0.05 mmol/L ANS in the buffer of 20 mmol/L Tris-HCl, 100 mmol/L NaCl, pH 7.2) in a cuvette or microplate. Fluorescence signals of the samples were measured at EX 378 nm, EM 465 nm with a fluorescence photometer or a plate reader, and Tm was calculated with the software of GraphPad Prism5.0. The Tm values of several mutants of Penicillium expansum lipase (PEL) were measured with this ANS assay and conventional method simultaneously and the results show that Tm values are comparative and consistent between these methods, suggesting that the lipase-ANS assay is a reliable, rapid and high throughput method for lipase thermo-stability measurement.
Anilino Naphthalenesulfonates ; chemistry ; Enzyme Stability ; High-Throughput Screening Assays ; methods ; Hot Temperature ; Lipase ; metabolism ; Spectrometry, Fluorescence