• Title/Summary/Keyword: in vitro metabolite

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In Vitro and in Vivo Metabolism of Salsolinol, on Endogenous Isoquinoline Neurotoxin, in Rats

  • Rhee, Hee-Kyung;Kwon, Oh-Seung;Ryu, Jae-Chun
    • Environmental Mutagens and Carcinogens
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    • v.21 no.1
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    • pp.30-33
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    • 2001
  • Salsolinol (1-methyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline, SAL), a dopaminergic isoquinoline neurotoxin, has been implicated to contribute the etiology of Parkinson's disease and neuropathology of chronic alcoholism. In our previous results, SAL was reported to have the mutagenicity and clastogenicity not in bacteria but in mammalian cells, and its genotoxic potential was known to be potentiated in the presence of rat liver S-9 fraction. This may indicate that some metabolite(s) of SAL was involved in the mutagenic potentials. To investigate the SAL metabolites, the metabolism studies of SAL were conducted in vitro rat liver S-9 fraction and in vivo using rats by high performance liquid chromatography and gas chromatography/mass spectrometry. The methylated metabolite of SAL was found in urine of rats, while the same methylating form of metabolite was not produced from the in vitro metabolism system using rat liver S-9 fraction.

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In Vitro Sex Steroid Metabolism in Red Spotted Grouper, Epinephelus akaara during Oocyte Maturation

  • Hwang, In Joon;Baek, Hea Ja
    • Development and Reproduction
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    • v.25 no.2
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    • pp.75-82
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    • 2021
  • We studied steroid metabolites produced from red-spotted grouper ovarian follicles during maturation. Oocytes with 350-500 ㎛ diameter were in vitro incubated in the presence of [3H] 17α-hydroxyprogesterone as a precursor. Steroid metabolites were extracted from incubated media and oocytes. The extracts were separated and identified using thin layer chromatography, high performance liquid chromatography and gas chromatography-mass spectrometry. The identified metabolites were androstenedione (A4), testosterone (T) and estrone (E1). The metabolites of A4 was dominant in all size of oocytes and it was the highest in 480 ㎛ diameter oocytes. The metabolites of two progestins, 17α,20β-dihydroxy-4-pregnen-3-one and 17α,20α-dihydroxy-4-pregnen-3-one were detected in the oocytes less than 480 ㎛ diameter although they were not identified definitely. In the oocytes of 480 ㎛ diameter, metabolite of progestin was the highest, and germinal vesicle (GV) was still in the middle of cytoplasm. In the oocytes of 500 ㎛ diameter, GV was began to migrate and the major metabolites were A4 and E1. The metabolite of E1 was detected in all size of oocytes and it was higher than that of E2. These results suggest that oocytes of 480 ㎛ diameter are the transitional stage involving steroidogenic shift to final oocyte maturation and potential function of E1 during maturation process.

Antiallergic Activities of Daidzein, a Metabolite of Puerarin and Daidzin Produced by Human Intestinal Microflora

  • Park, Eun-Kyung;Choo, Min-Kyung;Kim, Dong-Hyun
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.225.1-225.1
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    • 2003
  • To evaluate the antiallergic activities of puerarin and daidzin from the rhizome of Pueraria lobata, in vitro and in vivo inhibitory activities of these compounds and their metabolite daidzein were measured. Daidzein exhibited potent inhibitory activity on the B-hexosaminidase release induced by DNP-HSA and potently inhibited the PCA reaction in mice. (omitted)

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In Vitro Bactericidal and Anticancer Activity of New Metabolite, ARK42, Isolated from Aspergillus repens K42

  • Park, Je-Won;Song, Beom-Seok;Ryu, Do-Jin;Lee, Chan;Kim, Young-Bae
    • Journal of Microbiology and Biotechnology
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    • v.12 no.6
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    • pp.1017-1021
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    • 2002
  • A novel antibacterial metabolite, ARK42, was elated from a xerophilic fungal strain K42, and Identified as Aspergillus repens based on its morphological characteristics. The metabolite exhibited antibacterial activities towards Staphylococcus aureus, Bacillus cereus, and Pseudomonas aeruginosa, with MICs of 25, 12.5, and $3.125{\mu}g/ml$, respectively, and killed Pseudomonas aeruginosa with minimal bactericidal concentration (MBC) of $12.5{\mu}g/ml$. Furthermore, anticancer activities were demonstrated against human colon cancer DLD- 1 and lung cancer LXFL529 cells with an $IC_50$ of 10 and $1{\mu}g/ml$, respectively.

Effect of Ginseng Extracts on the Binding to DNA of Benzo(a)pyrene Metabolites in uitro in Rats (DNA와 Benzo(a)pyrene 대사물질 결합형성에 미치는 인삼 추출물의 영향)

  • 박진규;고지훈
    • Journal of Ginseng Research
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    • v.13 no.1
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    • pp.37-41
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    • 1989
  • Reactive metabolites generated by benzo(a)pyrene(BP) monooxygenase(AHH) interact with nucleophiles in DNA and cause mutation and carcinogenesis. We studied the effect of Panax ginseng C.A. Meyer, which induce epoxide hydratase(EH) activity without concomitant induction of AHH activity, on the binding of BP metabolites to DNA in uitro in Sprague Dawley rats. DNA-BP metabolite adducts can be resolved into at least five distinct peaks by elution of a Sephadex LH-20 column with a water methanol gradieNt. These peaks are arbitrarily designated A(most polar) through I(least polar). Of the 5 peaks tentatively assigned to 7,8 biol-9,10-oxide(A),7,8·oxide(B),4,5-oxide(C), and further metabolites of 9-OH-BP(D & E), peaks A, C, D, and I were reduced to 70, 85, 80, and 30% of controls, respectively, and there was no significant change in peak B. In connection with this DNA binding study, BP metabolizing enzymes including AHH, EH, demethylase(DM) activity and cyt. P-450 contents were also investigated in order to compare the BP treated control with ginseng and BP treated test groups. The results showed that the EH activity was increased by 139% over the BP control, the Cyt. P-450 content was increased by 180% over the control value, and DM and AHH activities were also increased to some degree for the BP test group, but there was no significant effect of the ginseng treatment.

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Ginseng Intestinal Bacterial Metabolite IH901 as a New Anti-Metastatic Agent

  • Hideo Hasegawa;Sung, Jong-Hwan;Huh, Jae-Doo
    • Archives of Pharmacal Research
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    • v.20 no.6
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    • pp.539-544
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    • 1997
  • Anti-metastatic activities of IH901, an intestinal bacterial metabolic derivative formed from Ginseng protopanaxadiol saponins, was determined in vitro and in vivo. Under in vitro conditions, IH901 inhibited the migration of bovine aortic endothelial cells 25 times stronger than suramin and suppressed the invasion of HT1080 human fibrosarcoma cells into reconstituted basement membrane components of Matrigel 1000 times stronger than RGDS peptide. IH901 also showed inhibitory effect on type-IV collagenase secretion from HT 1080 cells and platelet aggregation. When the anti-metastatic activity of IH901 was evaluated in comparison with that of 5-FU using a spontaneous lung metastatic model of Lewis lung carcinoma, the administration of IH901 (10 mg/kg p. o.) to tumor-bearing mice led to a significant decrease in lung metastasis (43% of untreated control), which was slightly more effective than that obtained with 5-FU (56% of control). Thus, IH901 seems to exhibit its anti-metastatic activity partly through the inhibition of tumor invasion which results from the blockade of type IV collagenase secretion and also through anti-platelet and anti-angiogenic activities.

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Investigation of Varied MR Spectra by TE and Metabolite Amount in the Localized Voxel using the MR Cone-shape Phantom (자기공명분광법에서 TE와 Voxel 내의 대사물질 양에 따른 스펙트럼 변화 평가에 관한 연구)

  • Woo, Dong-Cheol;Kim, Sang-Soo;Rhim, Hyang-Shuk;Jahng, Geon-Ho;Choe, Bo-Young
    • Progress in Medical Physics
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    • v.18 no.3
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    • pp.179-185
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    • 2007
  • The purpose of this study is to investigate the spectra of a magnetic resonance spectroscopy (MRS) in accordance with the variance of TE and the volumes of metabolites in a localized voxel for the quality assurance using a designed single voxel spectroscopy QA phantom. Because a cone-shade phantom is designed as the volume of metabolite in a localized voxel is changeable, we try to analyze the peaks of each metabolite (NAA, Cr, Cho, Lac, etc.) in accordance with metabolite volume in a localized voxel as well as echo time (TE). All data were obtained using a 3T MRI/MRS machine and analyzed using $jMRUI^{(R)}$. The results of this study show that TE is in inverse proportion to the noise of MRS and the longer TE and the less metabolite volume in the localized voxel, the peak intensities of each metabolite decrease. In case of the lactate, its peak was observed on the all TE only if the greatest metabolite is included in the localized voxel. Then, the intensity of a metabolite is more sensitive to the metabolite volume in the localized voxel than the TE. These obtained in vitro MRS data is provide the guideline that is important for in vivo metabolite quantification. But, in the edge of cone-shape vial air bubbles were observed and spectrum could not obtained. Therefore our cone-shape MRS phantom needs to be modified in order to solve these problems.

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Pharmacokinetics of ginsenoside Rb1 and its metabolite compound K after oral administration of Korean Red Ginseng extract

  • Kim, Hyung-Ki
    • Journal of Ginseng Research
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    • v.37 no.4
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    • pp.451-456
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    • 2013
  • Compound K is a major metabolite of ginsenoside Rb1, which has various pharmacological activities in vivo and in vitro. However, previous studies have focused on the pharmacokinetics of a single metabolite or the parent compound and have not described the pharmacokinetics of both compounds in humans. To investigate the pharmacokinetics of ginsenoside Rb1 and compound K, we performed an open-label, single-oral dose pharmacokinetic study using Korean Red Ginseng extract. We enrolled 10 healthy Korean male volunteers in this study. Serial blood samples were collected during 36 h after Korean Red Ginseng extract administration to determine plasma concentrations of ginsenoside Rb1 and compound K. The mean maximum plasma concentration of compound K was $8.35{\pm}3.19$ ng/mL, which was significantly higher than that of ginsenoside Rb1 ($3.94{\pm}1.97$ ng/mL). The half-life of compound K was 7 times shorter than that of ginsenoside Rb1. These results suggest that the pharmacokinetics, especially absorption, of compound K are not influenced by the pharmacokinetics of its parent compound, except the time to reach the maximum plasma concentration The delayed absorption of compound K support the evidence that the intestinal microflora play an important role in the transformation of ginsenoside Rb1 to compound K.

Biotransformation of a Fungicide Ethaboxam by Soil Fungus Cunninghamella elegans

  • PARK, MI-KYUNG;KWANG-HYEON LIU;YOONGHO LIM;YOUN-HYUNG LEE;HOR-GIL HUR;JEONG-HAN KIM
    • Journal of Microbiology and Biotechnology
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    • v.13 no.1
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    • pp.43-49
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    • 2003
  • Metabolism of a new fungicide ethaboxam by soil fungi was studied. Among the fungi tested, Cunninghamelia elegans produced metabolites from ethaboxam, which were not found in the control experiments. M5, a major metabolite from ethaboxam was firmly identified as N-deethylated ethaboxam by LC/MS/MS and NMR. N-Deethylated ethaboxam has been found as a single metabolite in in vitro metabolism with rat liver microsomes. Ml was proved to be 4-ethyl-2-(ethylamino)-1,3-thiazole-5-carboxamide (ETC) by comparing with the authentic compound. In addition, M2, M3, and M4, and M6 were tentatively Identified by LC/MS/MS as hydroxylated and methoxylated ethaboxams, respectively. Production of the major metabolite, N-deethylated ethaboxam, by the fungus suggested that C. elegans would be an efficient eukaryotic microbial candidate for evaluating xenobiotic-driven mammalian risk assessment.

Influence of Mineral Salts on Shoot Growth and Metabolite Biosynthesis in Tea Tree (Camellia sinensis L.)

  • Kim, Yong Duck;Yun, Jae Gill;Seo, Yeong Rong;Karigar, Chandrakant S.;Choi, Myung Suk
    • Horticultural Science & Technology
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    • v.33 no.1
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    • pp.106-113
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    • 2015
  • Effects of mineral salts (N, P, K, $Ca^{2+}$, $Mg^{2+}$, and $Fe^{3+}$) on the shoot growth and metabolite production of tea tree were studied using in vitro culture techniques. Among mineral s alts, ${H_2PO_4}^-$ was the most important for enhanced growth rate of tea tree, while $Mg^{2+}$ and $Ca^{2+}$ did not affect plant growth. Removal of ${NH_4}^+$ and $NO_3$ from the culture medium enhanced shoot multiplication compared to other treatments. Metabolite production was variable depending on mineral types and concentration. Removal of $Ca^{2+}$ decreased the production of caffeine; however, other treatments did not influence its production. $Ca^{2+}$, ${NH_4}^+$ and $Fe^{3+}$ were important factors for catechin production in tea tree. These results can be used as the basis for development of technical soil controls suitable for tea tree cultivation in the future.