• Archives of Pharmacal Research
• /
• v.28 no.2
• /
• pp.159-163
• /
• 2005

The effects of sedative peptide alkaloids from Zizyphus species on calmodulin- dependent protein kinase II were investigated. Protein kinase II activity was assayed on the basis of its ability to activate tryptophan 5-monooxygenase as its substrate in the presence of calmodulin. All thirteen alkaloids tested were stronger inhibitors than chlorpromazine ($IC_50,\;98{\mu}M$) on calmodulin-dependent protein kinase II. Among them, the most potent inhibitor was daechuine S27 ($IC_{50},\;2.95{\mu}M$), which was stronger than pimozide ($IC_{50},\;15.0{\mu}M$).

• Toxicological Research
• /
• v.11 no.2
• /
• pp.205-213
• /
• 1995

This study was undertaken to investigate the effects of organic solvents on xenobiotic metabollzing enzyme system in vivo by meaas of experimental conditions i.e. (1) single group which was treated by benzene (B), toluene (T) and xylene (X), respectively, (2) combination group which was treated by mixture of benzene+toluene (BT), benzene+xylene (BX), and toluene+xylene (TX), respectively, (3) mixture group which was treated by benzene+ toluene+xylene mixture (M), and to interpreat the interaction between the organic solvents metabolizing enzymes. 1. The contents of cytochrome P-450 in liver microsomes were increased (p < 0.01) in organic solvents treated groups, and the contents of cytochrome P-450 were increased by following order of B < T < M < BT=BX < X < TX. 2. The activity of cytochrome P-450 dependent AHHase was significantly higher in organic solvents treated groups than in control group (p < 0.01), and the activity of AHHase was increased by following order of B < T < BT=BX=TX=xylene < M. 3. The activity of NADPH P-450 reductase was significantly higher in organic solvents treated groups than in control group (p < 0.01), and the order of M < combinated group < X < T

• BMB Reports
• /
• v.30 no.4
• /
• pp.237-239
• /
• 1997

The effects of trichloroethylene (TRI) on the induction of cytochrome P-450 (CYP) and several other related enzymes in Sprague Dawley rats were investigated Rats were treated with TRI 150. 300. 600 mg/kg body weight in corn oil intra peritoneally once a day for 2 days. The total contents of microsomal CYP and cytochrome $b_5\;(b_5)$ decreased with the increase of TRI concentration. but the activity of p-nitrophenol hydroxylase increased with the increase of TRI dosage (p<0.05). Western blot analysis which utilized monoclonal antibodies against CYP2E1 also showed a significant increase in the CYP2E band density. The increase of the activity of pentoxyresolufin-O-deethylase also was observed with the TRI treatment (p<0.05) although there was no significant increase in the cytochrome CYP2B1/2 in Western blotting The TRI did not affect the induction of aryl hydrocarbon hydroxylase. These findings suggest that the CYP2E1 is the primary enzyme which could be induced by TRI treatment in rats.

• Korean journal of applied entomology
• /
• v.32 no.2
• /
• pp.225-235
• /
• 1993

This study was carried out to investigate effects of diazinon, an organophosphate, and nicotine, a plant~originated toxic chemical, on larval mortality and activity of cytochrome P-45D monooxygenases, a major detoxifwation enzyme system, in Helicoverpa assulta and Spodoptera exigua. Diazinon treatment gave a higher mortaliLy to H. assulta larvae than S. exigua larvae. In contrast to the case of diazinon, nicotine caused a higher mortahty to S. exigua than to H. assulla larvae. It was partly due to the fact that nicotine induced the actiVIty of midgut cytochrome P-450 monooxygenases (MFO) more than diazinon did in If assulta larvae. When If. aSSlllta larvae were reared on their host p\am. NicotwlIa tuoocum leaves, other componentS were mostly metabolized with the exception of dietary nicotine.

• Journal of Microbiology and Biotechnology
• /
• v.30 no.5
• /
• pp.777-784
• /
• 2020

Self-sufficient P450s, due to their fused nature, are the most effective tools for electron transfer to activate C-H bonds. They catalyze the oxygenation of fatty acids at different omega positions. Here, two new, self-sufficient cytochrome P450s, named 'CYP102A15 and CYP102A170,' from polar Bacillus sp. PAMC 25034 and Paenibacillus sp. PAMC 22724,respectively, were cloned and expressed in E. coli. The genes are homologues of CYP102A1 from Bacillus megaterium. They catalyzed the hydroxylation of both saturated and unsaturated fatty acids ranging in length from C₁₂-C₂₀, with a moderately diverse profile compared to other members of the CYP102A subfamily. CYP102A15 exhibited the highest activity toward linoleic acid with K_m 15.3 μM, and CYP102A170 showed higher activity toward myristic acid with Km 17.4 μM. CYP10A170 also hydroxylated the Eicosapentaenoic acid at ω-1 position only. Various kinetic parameters of both monooxygenases were also determined.

• Toxicological Research
• /
• v.13 no.4
• /
• pp.385-391
• /
• 1997

Inductive effects of cytochrome P450 2B1 by $\alpha$- and $\beta$-ionone were characterized in individual liver lobes of male Sprague Dawley rats. When rats were administered ionones orally at 100, 300, and 600 mg/kg for 24 hr, cytochrome P450 2B1 was induced dose-dependently in liver S-9 fractions as measured by P450 2B-specific monooxygenases and Western immunoblotting. The activity of P450 1A- and P450 2B-specific monooxygenases was differentially expressed in each lobe of normal liver. In addition, the monooxygenase activity was induced by $\alpha$- and $\beta$-ionone with different potency in each lobe of the liver. Our present results indicate that the different induction of P450s by $\alpha$- and $\beta$-ionone in each lobe may explain different susceptibilities of rat liver lobes to certain hepatotoxicants which require metabolic activation for their toxicity and that $\alpha$- and $\beta$-ionone may be useful model inducers of P450 2B1 in studying the toxic mechanism of certain toxicants which may require the metabolic activation by P450.

• Biomolecules & Therapeutics
• /
• v.21 no.1
• /
• pp.72-78
• /
• 2013

This work aimed to assess some pharmacological activities of P. leptostachya var. asiatica Hara. The dried roots of P. leptostachya var. asiatica Hara were extracted with 70% ethanol to generate the powdered extract, named PLE. Anti-angiogenic activity was detected using chick chorioallantoic membrane (CAM) assay. In vitro anti-inflammatory activity was evaluated via analyzing nitric oxide (NO) content, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells. Antioxidant activity was determined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay and reactive oxygen species (ROS) level in the stimulated macrophage cells. Matrix metalloproteinase-9 (MMP-9) and -2 (MMP-2) activities in the culture media were detected using zymography. PLE exhibits an anti-angiogenic activity in the CAM assay, and displays an inhibitory action on the generation of NO in the LPS-stimulated macrophage cells. In the stimulated macrophage cells, it is able to diminish the enhanced ROS level. It can potently scavenge the stable DPPH free radical. It suppresses the induction of iNOS and COX-2 and the enhanced MMP-9 activity in the stimulated macrophage cells. Both monooxygenase and oxidase activities of tyrosinase were strongly inhibited by PLE. Taken together, the dried roots of P. leptostachya var. asiatica Hara possess anti-angiogenic, anti-inflammatory, antioxidant and skin whitening activities, which might partly provide its therapeutic efficacy in traditional medicine.

• Proceedings of the Korean Society of Soil and Groundwater Environment Conference
• /
• 2003.04a
• /
• pp.188-191
• /
• 2003

Sing]e-well-push-pull tests were developed for use in assessing the feasibility of in-situ aerobic cometabolism of chlorinated aliphatic hydrocarbons (CAHs). The series includes Transport tests, Biostimulation tests, and Activity tests. Transport tests are conducted to evaluate the mobility of solutes used in subsequent tests. These included bromide or chloride (conservative tracers), propane (growth substrate), ethylene, propylene (CAH surrogates), dissolved oxygen (electron acceptor) and nitrate (a minor nutrient). Tests were conducted at an experimental well field of Oregon State University. At this site, extraction phase breakthrough curves for all solutes were similar, indicating apparent conservative transport of the dissolved gases and nitrate prior to biostimulation. Biostimulation tests were conducted to stimulate propane-utilizing activity of indigenous microorganisms and consisted of sequential injections of site groundwater containing dissolved propane and oxygen. Biostimulation was detected by the increase in rates of propane and oxygen utilization after each injection. Activity tests were conducted to quantify rates of substrate utilization and to confirm that CAH-transforming activity had been stimulated. In particular, the transformation of injected CAH surrogates ethylene and propylene to the cometabolic byproducts ethylene oxide and propylene oxide provided evidence that activity of the monooxygenase enzyme system, responsible for aerobic cometabolic transformations of CAHs had been stimulated. Estimated zero-order transformation rates decreased in the order propane > ethylene > propylene. The series of push-pu3l tests developed and field tested in this study should prove useful for conducting rapid, low-cost feasibility assessments for in situ aerobic cometabolism of CAHs.

• Korean Journal of Environmental Agriculture
• /
• v.11 no.2
• /
• pp.109-115
• /
• 1992

In order to investigate waether soil microorganism prefer diazinon to humic substances as their substate, the growth of soil bacteria and the activities of monooxygenase and ${\alpha}-,{\beta}-esterase$ were measured after treatment of diazinon and humic substances in defined medium at $30{\pm}1^{\circ}C$. Also, the degradation rate of diazinon was determined by addition of humic substances to the medium. The number of soil bacteria was increased from 1 day and 3 days after the treatment with humic substances and diazinon, respectively. And it showed about 1.5 times more with humic substances than diazinon at 10 days. Monooxygenase(MO) activity with the treatment of humic substances was higher than diazinon until 3 days after treatment in the order of HA > FA > humin. Esterase(ES) activity with the treament of humin and HA was higher than dizainon from 5 dyas, but FA was much similar to diazinon. The degradation rate of diazinon showed more persistancy by addition of humic substances ; 51.4% with humin treatment, 58.9% with HA, 62.4% with FA and 71.9% in control at 10 days after treatment. Therefore, as soil microorganisms perfer humic substances to diazinon, the degreadation rate of diazinon might be delayed by addition of humic stbstances in submerged soil.

• Korean Journal of Fisheries and Aquatic Sciences
• /
• v.35 no.2
• /
• pp.185-190
• /
• 2002

This study was carried out to measure the in vitro interaction of trialkyltin with the microsomal monooxygenase (MFO) system of the clam, Coelomactra antiquata. Cytochrome P450 (CYP) level and 7-ethonvesorufin-O-deethylase (EROD) activity were invetigated in the microsome isolated from digestive gland of the clam (C. antiquata) exposed to tributyltin chloride (TBTC), bis-tributyltinoxide (TBTO) and triphenyltin chloride (TPTC). The specific contents of CYP in clam microsome exposedto 0.4 mM TBTC, TBTO and TPTC for 20 minutes were decreased 52, 72 and $40\%$, respectively, compared to control group. The EROD activities also were inhibited by exposure to TBTO ($92\%$) and TPTC ($85\%$) except for TBTC, The level of CYP and the EROD actintles were decreased according to the OTC exposure concentrations. The toxic effects on the level of CYP and the EROD activities were in order of TPTC>TBTC>TBTO in this study. The measurement of CYP level and EROD activity could be applied as a biomarker for environmental study.