• Archives of Pharmacal Research
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• 제29권8호
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• pp.685-690
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• 2006

The effect of a main constituent ginsenoside Rg5 isolated from red ginseng and its metabolite ginsenoside Rh3 in a chronic dermatitis model was investigated. Ginsenosides Rg5 and Rh3 suppressed swelling of oxazolone-induced mouse ear contact dermatitis. These ginsenosides also reduced mRNA expressions of cyclooxygenase-2, interleukin $(IL)-1{\beta}$, tumor necrosis factor $(TNF)-{\alpha}$ and interferon $(IFN)-{\gamma}$. The inhibition of ginsenoside Rh3 was more potent than that of ginsenoside Rg5. These findings suggest that ginsenoside Rh3 metabolized from ginsenoside Rg5 may improve chronic dermatitis or psoriasis by the regulation of $IL-1{\beta}$ and $TNF-{\alpha}$ produced by macrophage cells and of $IFN-{\gamma}$ produced by Th cells.

• 한국환경성돌연변이발암원학회지
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• 제19권1호
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• pp.34-38
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• 1999

Fumonisin B1 is a secondary metabolite of Fusarium moniliforme, a contaminant of corn and corn product. Fumonisin B1 has been shown to be responsible for major toxicological effects of the fungus in rats, horses, and pigs. Fumonisin B1 induced λ DNA fragmentation, which was increased with incubation time, reducing agent NADPH and metal ion (Cu2+). The DNA damage was inhibited by dimethyl sulfoxide (DMSO) or mannitol as radical scavenger for free radicals. DNA fragmentation, induced by fumonisin B1 in the presence of 1 mM NADPH and 0.1 mM CuCl2, was inhibited by 100 mM DMSO. By the in vitro reaction of fumonisin B1 with supercoiled plasmid pBR322 DNA, plasmid DNA was relaxed, eventually linearized in the agarose gel electrphoresis. From rifampicin sensitive E. coli CSH138 in bacterial mutagenesis system, the rifampicin resistant E. coli mutants were obtained by fumonisin B1. These results suggest that fumonisin B1 may be a possible environmental mutagen in bacterial mutagen assay system.

• 한국가축번식학회지
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• 제3권2호
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• pp.32-41
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• 1979

A series of experiment was conducted to determine the concentrations of progesterone and estradiol and metabolite contents in the serum of 26 Korean native cows raised at Alpine Experiment Station during the period of late pregnancy. Blood samples were collected by jugular puncture from individual cow at 5 day intervals from 30 days prepartum to 5 days prepartum and daily collected from 5 days prepartum to the day of parturition. Progesterone and estradiol concentrations in the serum were analyzed by Radioimmunoassay (R.I.A) method and serum metabolite contents were analyzed by autoanalzer MT II system. The following are summary of the results obtained: 1. Progresterone concentrations during the late preganacy were maintained at high level (5.12-11.70ng/$m\ell$) from 30 days prepartum to 8 days prepartum and fell rapidly from 5.12$\pm$1.07ng/$m\ell$ at 2 dyas prepartum to 1.48$\pm$0.32ng/$m\ell$ at 24 hrs prepartum. 2. Estradiol levles during the late pregancy increased gradually from 33.76$\pm$13.64pg/$m\ell$ at 30 days prepartum to 92.15$\pm$11.91pg/$m\ell$ at 11-15 days prepartum and increased thereafter sharply to a ranges of 161.76-238.4pg/$m\ell$ and were maintained at this increased levle until 24 hrs prepartum and decreased to 91.40pg/$m\ell$ at the parturition. 3. The correlation coefficients were found to be 0.2440 for cholesterol-progesterone relationship and -0.2552 for cholesterol-estradiol relationship, but there were statistically insignificant. 4. The changes in total protein contents during the late pregnancy were similar patterns to those of globulin and were maintained at high level only from 15 days to 5 days prepartum. 5. Glutamic oxaloacetate transaminase (GOT) levels were increased from 59.80$\pm$3.56u/$\ell$ at 90 days prepartum to 93.32$\pm$7.27u/$\ell$ at the day of parturition, but alkaline phosphatase levels were remained steady. 6. The levels of blood urea nitrogen, glucose and calcium remained almost constant during the late pregnancy. However, glucose concentration increased around the time of parturition.

• Journal of Ginseng Research
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• 제44권6호
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• pp.770-774
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• 2020

Background: Fermentation has been shown to improve the biological properties of plants and herbs. Specifically, fermentation causes decomposition and/or biotransformation of active metabolites into high-value products. Polyacetylenes are a class of polyketides with a pleiotropic profile of bioactivity. Methods: Column chromatography was used to isolate compounds, and extensive NMR experiments were used to determine their structures. The transformation of polyacetylene in red ginseng (RG) and the production of cazaldehyde B induced by the extract of RG were identified by TLC and HPLC analyses. Results: A new metabolite was isolated from RG fermented by Chaetomium globosum, and this new metabolite can be obtained by the biotransformation of polyacetylene in RG. Panaxytriol was found to exhibit the highest antifungal activity against C. globosum compared with other major ingredients in RG. The fungus C. globosum cultured in RG extract can metabolize panaxytriol to Metabolite A to survive, with no antifungal activity against itself. Metabolites A and B showed obvious inhibition against NO production, with ratios of 42.75 ± 1.60 and 63.95 ± 1.45% at 50 µM, respectively. A higher inhibitory rate on NO production was observed for Metabolite B than for a positive drug. Conclusion: Metabolite A is a rare example of natural polyacetylene biotransformation by microbial fermentation. This biotransformation only occurred in fermented RG. The extract of RG also stimulated the production of a new natural product, cazaldehyde B, from C. globosum. The lactone in Metabolite A can decrease the cytotoxicity, which was deemed to be the intrinsic activity of polyacetylene in ginseng.

• Journal of Ginseng Research
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• 제38권3호
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• pp.203-207
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• 2014

Background: There is limited understanding of the effect of dietary components on the absorption of ginsenosides and their metabolites into the blood. Methods: This study investigated the pharmacokinetics of the ginseng extract and its main constituent ginsenoside Rb1 in rats with or without pretreatment with a prebiotic fiber, NUTRIOSE, by liquid chromatography tandem mass spectrometry. When ginsenoside Rb1 was incubated with rat feces, its main metabolite was ginsenoside Rd. Results: When the intestinal microbiota of rat feces were cultured in vitro, their ginsenoside Rd-forming activities were significantly induced by NUTRIOSE. When ginsenoside Rb1 was orally administered to rats, the maximum plasma concentration (Cmax) and area under the plasma drug concentratione-time curve (AUC) for the main metabolite, ginsenoside Rd, were $72.4{\pm}31.6ng/mL$ and $663.9{\pm}285.3{\mu}g{\cdot}h/mL$, respectively. When the ginseng extract (2,000 mg/kg) was orally administered, Cmax and AUC for ginsenoside Rd were $906.5{\pm}330.2ng/mL$ and $11,377.3{\pm}4,470.2{\mu}g{\cdot}h/mL$, respectively. When ginseng extract was orally administered to rats fed NUTRIOSE containing diets (2.5%, 5%, or 10%), Cmax and AUC were increased in the NUTRIOSE receiving groups in a dose-dependent manner. Conclusion: These findings reveal that intestinal microflora promote metabolic conversion of ginsenoside Rb1 and ginseng extract to ginsenoside Rd and promote its absorption into the blood in rats. Its conversion may be induced by prebiotic diets such as NUTRIOSE.

• Journal of Microbiology and Biotechnology
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• 제31권4호
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• pp.601-609
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• 2021

Erythrobacter species are extensively studied marine bacteria that produce various carotenoids. Due to their photoheterotrophic ability, it has been suggested that they play a crucial role in marine ecosystems. It is essential to identify the genome sequence and the genes of the species to predict their role in the marine ecosystem. In this study, we report the complete genome sequence of the marine bacterium Erythrobacter sp. 3-20A1M. The genome size was 3.1 Mbp and its GC content was 64.8%. In total, 2998 genetic features were annotated, of which 2882 were annotated as functional coding genes. Using the genetic information of Erythrobacter sp. 3-20A1M, we performed pan-genome analysis with other Erythrobacter species. This revealed highly conserved secondary metabolite biosynthesis-related COG functions across Erythrobacter species. Through subsequent secondary metabolite biosynthetic gene cluster prediction and KEGG analysis, the carotenoid biosynthetic pathway was proven conserved in all Erythrobacter species, except for the spheroidene and spirilloxanthin pathways, which are only found in photosynthetic Erythrobacter species. The presence of virulence genes, especially the plant-algae cell wall degrading genes, revealed that Erythrobacter sp. 3-20A1M is a potential marine plant-algae scavenger.

• Archives of Pharmacal Research
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• 제29권3호
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• pp.241-248
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• 2006

Angiotensin converting enzyme (ACE) inhibitors have cardioprotective effects in different species including human. This cardioprotective effect is mainly due to the inhibition of bradykinin (BK) degradation rather than inhibition of the conversion of angiotensin I to angiotensir. II. Bradykinin, a nonapeptide, has been considered to be the potential target for various enzymes including ACE, neutral endopeptidase 24.11, carboxypeptidase M, carboxypeptidase N, proline aminopeptidase, endopeptidase 24.15, and meprin. In the present study, the coronary vascular beds of Sprague Dawley rat isolated hearts were perfused (single passage) with Krebs solution alone or with different concentrations of BK i.e. $2.75{\times}10^{-10},\;10^{-7},\;10^{-6}\;and\;10^{-5}M$ solution. Percent degradation of BK was determined by radioimmunoassay. The degradation products of BK after passing through the isolated rat-hearts were determined using RP-HPLC and mass spectroscopy. All the four doses of BK significantly decreased the perfusion pressure during their passage through the hearts. The percentage degradation of all four doses was decreased as the concentration of drug was increased, implying saturation of a fixed number of active sites involved in BK degradation. Bradykinin during a single passage through the hearts degraded to give [1-7]-BK as the major metabolite, and [1-8]-BK as a minor metabolite, detected on HPLC. Mass spectroscopy not only confirmed the presence of these two metabolites but also detected traces of [1-5]-BK and arginine. These findings showed that primarily ACE is the major cardiac enzyme involved in the degradation of bradykinin during a single passage through the coronary vascular of bed the healthy rat heart, while carboxypeptidase M may have a minor role.

• Bulletin of the Korean Chemical Society
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• 제29권5호
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• pp.985-987
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• 2008

Parathion is an organophosphate pesticide being legally applied for the purpose of agriculture and is being manufactured in Korea. A gas chromatography/mass spectrometric method was developed for the determination of parathion urinary metabolite, p-nitrophenol. p-Nitrophenol was extracted from weak acidic urine, and then measured by gas chromatography-mass spectrometry (selected ion monitoring). The recovery of pnitrophenol in the overall procedure was 88.2%. The detection limit of the assay was 1.0 $\mu$ g/L based upon assayed urine of 2.0 mL. The method was applied to the determination of p-nitrophenol in urine of workers of a parathion industry. Spot urines of workers of a parathion industry were sampled at the end of shift and pnitrophenol was analyzed using above developed method. p-Nitrophenol could be detected in all of the urine samples at concentrations varying from 3.0 to 681 $\mu$ g/L.

• Toxicological Research
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• 제5권1호
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• pp.9-15
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• 1989

The effect of butylated hydroxytoluene (BHT) and its major metabolite, 3, 5-di-tert-butyl-4-hydroxybenzoic acid (BHT-acid) on the uptake of taurocholate into hepatocytes was studied using the primary culture of rat hepatocytes. Hepatocyte were isolated by an in situ collagenase perfusion technique and maintained as a monolayer in serum-free meadia for 24 hours before use. The uptake of taurocholate was saturable with an apparent Km of 12.8+2.8 MuM and Vmax of 0.18+0.01 nmol/mg/min. Both BHT and BHT-acid inhibited the hepatocellular uptake of taurocholate when they were added to the culture.

• The Korean Journal of Physiology and Pharmacology
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• 제5권2호
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• pp.165-175
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• 2001

Background: Recent in vivo experimental evidence suggests that isoflurane-induced cardioprotection may involve $K_{ATP}$ channel activation. However, it was demonstrated that isoflurane inhibited $K_{ATP}$ channel activities in the inside-out patch mode. To explain this discrepancy, the present investigation tested the hypothesis that a metabolite of isoflurane, trifluoroacetic acid (TFA), contributes to isoflurnae-induced cardioprotection via $K_{ATP}$ channel activation during myocardial ischemia and reperfusion. Methods: Single ventricular myocytes were isolated from rabbit hearts by an enzymatic dissociation procedure. Patch-clamp techniques were used to record single-channel currents. $K_{ATP}$ channel activities were assessed before and after the application of TFA with the inside-out patch mode. Results: TFA enhanced channel activity in a concentration-dependent fashion. The concentration of TFA for half-maximal activation and the Hill coefficient were 0.03 mM and 1.2, respectively. TFA did not affect the single channel conductance of $K_{ATP}$ channels. Analysis of open and closed time distributions showed that TFA increased burst duration and decreased the interburst interval without changes in open and closed time distributions shorter than 5 ms. TFA diminished ATP sensitivity of $K_{ATP}$ channels in a concentration-response relationship for ATP. Conclusions: TFA, a metabolite of isoflurane, enhanced $K_{ATP}$ channel activity in a concentration-dependent fashion. These results imply that TFA could mediate isoflurane-induced cardioprotection via $K_{ATP}$ channel activation during myocardial ischemia and reperfusion.