• 제목/요약/키워드: in vitro metabolite

검색결과 150건 처리시간 0.025초

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

  • Rhee, Hee-Kyung;Kwon, Oh-Seung;Ryu, Jae-Chun
    • 한국환경성돌연변이발암원학회지
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    • 제21권1호
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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
    • 한국발생생물학회지:발생과생식
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    • 제25권2호
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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
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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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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    • 제12권6호
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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.

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

  • 박진규;고지훈
    • Journal of Ginseng Research
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    • 제13권1호
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    • pp.37-41
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    • 1989
  • Benzo(a)pyrene(BP)의 monooxygenase(AHH)에 의해서 생성된 반응성 대사물질들의 in vitro DNA와의 결합 및 BP 대사에 관여하는 효소들의 활성도에 미치는 인삼 물추출물의 영향을 조사하였으며, DNA-BP metabolite adduct들은 Sephadex LH-20 column으로 chromatography하여 5개의 major peak 들을 얻었다. 이 peak 들을 극성이 큰 순서대로 A부터 E까지 임의로 정하고 5개의 peak들을 7,8-diol-9,10-oxide(A), 7,8-oxide(B). 4,5-oxide(C), 9-HO-BP(D & E) adduct들로 잠정적으로 확인하였다. Peak A, C, D 그리고 E는 각각 대조군의 30, 15, 20 그리고 30%로 감소되었으며 peak B는 의미있는 변화를 보이지 않았다. DNA-BP 결합 억제와 관련하여 in vitro와 in vivo 투여시의 경향이 유사하여 EH의 활성도만 BP투여 대조군보다 38%정도 의미있게 유도되었다.

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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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    • 제20권6호
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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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자기공명분광법에서 TE와 Voxel 내의 대사물질 양에 따른 스펙트럼 변화 평가에 관한 연구 (Investigation of Varied MR Spectra by TE and Metabolite Amount in the Localized Voxel using the MR Cone-shape Phantom)

  • 우동철;김상수;임향숙;장건호;최보영
    • 한국의학물리학회지:의학물리
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    • 제18권3호
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    • pp.179-185
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    • 2007
  • 본 연구는 자기공명분광법(Magnetic Resonance Spectroscopy: MRS)에 있어서 기존 개발된 Multi-Voxel Spectroscopy (MVS)을 위한 MR 원뿔형 팬톰을 Single voxel spectroscopy (SVS)용으로 개선하여 선정된 Voxel내의 대사물질의 양과 TE 변화에 따른 스펙트럼의 변화를 관찰하였다. 원뿔형 팬톰은 Voxel를 선정하는 위치에 따라서 그 안에 포함되는 대사물질의 양을 변화시킬 수 있다는 점에 착안하여 Voxel안에 포함되는 뇌대사물질의 양과 TE시간에 따른 각 대사물질(NAA, Cr, Cho, Lac 등)의 Peak에 대한 정량적인 분석을 시도하였다. 실험은 3T MRI/MRS 장비에서 이루어졌고, 데이터를 분석하는데 $jMRUI^{(R)}$라는 프로그램이 사용되었다. 실험 및 분석 결과 대체로 Echo Time (TE)가 커질수록 잡음이 감소하는 경향을 확인할 수 있었고 또한 TE가 커질수록, Voxel 안의 뇌대사물질의 양이 적을수록 각 대사물질의 peak intensity가 감소하는 것을 관찰할 수 있었다. 특히 Lactate의 경우, 정위선정된 Voxel안에 가장 많은 양의 대사물질이 포함되었을 때만 스펙트럼 분석이 가능한 정도의 Peak intensity를 얻을 수 있었고 대부분의 TE에서 분석 가능한 것으로 보아 각 대사물질의 intensity는 TE보다는 Voxel내의 대사물질의 양에 더욱 민감하다는 결론을 도출 할 수 있었고, 이러한 Lac에 대한 in vitro 데이터는 정량분석 시에 있어서 in vivo상에서 대사물질의 정량화를 하는 데 있어서 중요한 가이드라인을 제시할 것으로 예상된다. 그러나, 원뿔의 모서리 부분에 표면장력에 의하여 수많은 공기방울이 MR image상에서 관찰되고 또한 MRS상에서 그 스펙트럼을 얻을 수 없었는데 이는 앞으로 원뿔형 MRS 팬톰을 구조적, 기술적으로 더욱 개선해야 할 여지를 남겨두고 있다.

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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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    • 제37권4호
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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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    • 제13권1호
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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
    • 원예과학기술지
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    • 제33권1호
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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.