• 제목/요약/키워드: metabolite M1

검색결과 284건 처리시간 0.025초

Thalictrum rugosum 세포배양에서 식물생장 조절물질이 세포증식 및 Berberine 생산에 미치는 영향 (Effectcs of Plant Growth Regulators on Growth and Berberine Production in Cell Suspension Cultures of Thalictrum rugosum)

  • 김동일
    • 한국미생물·생명공학회지
    • /
    • 제18권4호
    • /
    • pp.327-330
    • /
    • 1990
  • Thalictrum rugosum 세포배양에서 여러 가지 식물생장 조절물질이 세포증식 및 berberine 생산에 미치는 영향을 조사하였다. 조사된 식물생장 조절물질들 중에서 indole-3-acetic acid(IAA)가 berberine 생산에 가장 적합함을 알 수 있었고 그 최적농도는 1$\mu \textrm m$ 이었다. 비교 기준인 2,4-D의 사용결과에 비할 때 60이상의 생산량 상승효과가 있었으며, cytokinin인 6-benzylaminopurine(BA)를 동시에 사용하는 것보다 IAA만을 단독으로 사용하는 것이 더 효과적이다.

  • PDF

Anti-Allergic Activity of 18$\beta$-Glycyrrhetinic acid-3-O-$\beta$-D-glucuronide

  • Park, Hae-Young;Park, Sung-Hwan;Yoon, Hae-Kyung;Han, Myung-Joo;Kim, Dong-Hyun
    • Archives of Pharmacal Research
    • /
    • 제27권1호
    • /
    • pp.57-60
    • /
    • 2004
  • Glycyrrhizin (18$\beta$-glycyrrhetinic acid-3-O-$\beta$-D-glucuronopyranosyl-(1$\rightarrow2)-\beta$-D-glucuronide, GL) was transformed to 18$\beta$-glycyrrhetinic acid-3-O-$\beta$-D-glucuronide (GAMG) by Streptococcus LJ-22. The antiallergic activities of GL and GAMG was measured using a RBL cell assay system and contact hypersensitivity model mice. GAMG exhibited anti-allergic activity with $IC_{50}$ values of 0.28 mM. GAMG, which is sweeter than GL, and 18$\beta$-glycyrrhetinic acid, which is a GAMG metabolite by human intestinal bacteria, also inhibited the passive cutaneous anaphylaxis and skin contact inflammation. In conclusion, GAMG may be useful as a new sweet food additive and an anti-allergic agent.

생체시료에서 GC/MS에 의한 에틸렌글리콜 및 대사체인 글리콜산 동시분석 (Simultaneous analysis of ethylene glycol and glycolic acid in bio-specimens by GC/MS)

  • 이준배;박미정;성태명;최병하;유재훈;손성건;팽기정
    • 분석과학
    • /
    • 제23권6호
    • /
    • pp.544-550
    • /
    • 2010
  • 담홍색 열매체유를 포도주로 오인하고 음용하여 사망한 변사사건에서 열매체유 중 39%의 에틸렌글리콜을 확인하였다. 열매체유는 물을 열전달 매체로 사용하였을 경우 고온에서 발생되는 고압 수증기에 의한 문제를 피하기 위하여 사용되는 열전달 매체로 주로 광유계 또는 에틸렌글리콜을 사용하는 것으로 알려져 있다. 부검을 통한 혈액 및 기타 조직 등의 변사자 생체시료에서 중수소로 치환된 에틸렌글리콜을 내부표준물질로 하여 아세토니트릴로 추출, 정제 및 질소 기류하에서 농축한 다음 1% TMCS가 함유된 BSTFA로 유도체화하여 에틸렌글리콜과 그 대사체인 글리콜산을 GC/MS에 의하여 동시 분석하였다. 약 0.2 g의 생체시료에 대하여 0.5 M의 HCl 용액 $50\;{\mu}L$를 이용한 산성조건에서 추출하였으며 무수 황산나트륨을 단계적으로 처리하여 수분제거를 하였고 혈액에서 $2,755\;{\mu}g/mL$의 에틸렌글리콜과 $174\;{\mu}g/mL$의 글리콜산 및 기타 시료에서 $860\;{\mu}g/g\sim1,290\;{\mu}g/g$의 에틸렌글리콜과 $93\;{\mu}g/g\sim134\;{\mu}g/g$의 글리콜산을 검출하였다. 특히 신장 조직에서 이와 관련된 대사체인 옥살산염으로 추정되는 결정이 관찰되었다.

Accurate mass 및 isotope ratio 측정을 위한 GC-TOF 질량분석기에서의 화학적 이온화방법 (Development of chemical ionization method in a GC-TOF mass spectrometer for accurate mass and isotope ratio measurement)

  • 정주희;나윤철;황금숙;신정화;안윤경
    • 분석과학
    • /
    • 제24권1호
    • /
    • pp.15-23
    • /
    • 2011
  • 본 연구에서는 미지 대사물질 동정을 위해 GC-TOF/MS의 양이온 화학적 이온화 방법(positive chemical ionization, $CI^+$)을 이용, 정확한 질량 값(accurate mass)과 동위원소 비(isotope ratio) 측정을 위한최적 조건을 확립하였다. 분자이온 $[M+H]^+$ 세기를 증가시킬 수 있는 high mass tune 방법이 사용되었으며, 화합물들의 분리 및 감도에 따른 검출조건이 고려되어 졌다. 24종의 trimethylsilyl (TMS)기로 유도체화 된 표준 대사물질들을 분석한 결과 $[M+H]^+$의 경우 이론 값 과의 절대평균오차는 6.8 ppm이였으며, 동위원소 비(M+1/M, M+2/M)의 경우는 각각 1.5%와 1.7%였다. 얻어진 질량 값과 동위원소 비를 원소조성 알고리즘에 적용한 결과 21개의 화합물의 구조식이 2순위 내에서 일치하였다.

산화된 low density lipoprotein (LDL)에 의해 유도된 내피세포의 손상에 대한 마늘 대사산물인 allylmercaptan의 보호 효과 (Protection Effects of Allylmercaptan, Metabolite of Garlic on Endothelial Cell Injury Induced by Oxidized Low Density Lipoprotein)

  • 양승택
    • 생명과학회지
    • /
    • 제20권11호
    • /
    • pp.1595-1602
    • /
    • 2010
  • Low density lipoprotein (LDL)의 산화는 동맥경화의 유발과 진행에 결정적 역할을 하는 것으로 알려져 있다. 본 연구에서는 마늘의 주요 대사산물인 allylmercaptan의 산화 low density lipoprotein에 의해 손상된 내피세포의 보호효과에 대하여 실험하였다. Allylmercaptan의 항산화 활성은 thiobarbituric acid substance (TBARS)로 측정하였다. Allylmercaptan은 0.1, 1 및 10 mM의 농도에서 $Cu^{2+}$에 의해 유도된 LDL의 산화를 용량의존적으로 억제하였다. 폐동맥 내피세포를 $37^{\circ}C$, 5% $CO_2$ 상태에서 24시간 동안 미리 배양시킨 후 세측한 다음 다시 24시간 동안 0.1 mg/ml oxidized LDL (ox-LDL)을 첨가하여 배양하였다. 이 때 ox-LDL이 Lactate dehydrogenase (LDH)의 방출과 glutathione (GSH)를 감소시키는 원인으로 세포막 손상의 지표로 LDH와 GSH 함량을 조사하였다. 본 실험 결과 allylmercaptan을 일정 농도 별로 endothelial cell에 첨가하여 배양했을 때 LDH의 방출과 GSH의 감소를 현저하게 억제하였다. Peroxide를 형광분석법으로 24 well plate에서 직접 측정한 결과 allylmercaptan이 폐동맥 내피세포 내에서 ox-LDL 유도 peroxide의 방출을 억제하였다. 그리고 allylmercaptan은 과산화수소의 소거능도 있었다. 본 실험결과 allylmercaptan은 ox-LDL 유도 폐동맥 내피세포를 보호할 수 있었으므로 allylmercaptan은 동맥경화의 예방에 유용할 것으로 생각된다.

Metabolism of a New Neuroprotective Agent for Ischemia-Reperfusion Damage, KR-31543 in the Rats using Liquid Chromatography/Electrospray Mass Spectrometry

  • Kim, John;Ji, Hye-Young;Lee, Seung-Seok;Yoo, Sung-Eun;Kim, Sun-Ok;Lee, Dong-Ha;Lim, Hong;Lee, Hye-Suk
    • Archives of Pharmacal Research
    • /
    • 제25권5호
    • /
    • pp.664-668
    • /
    • 2002
  • KR-31543,(2S,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(2-methyl-2H-tetrazol-5-ylmethyl)amino]-3,4-dihydro-2-dimethoxymethyl-3-hydroxy-2-methyl-2H-1-benzopyran is a new neuroprotetive agent for ischemia-reperfusion damage. The in vitro and in vivo metabolism of KR-31543 in rats has been studied by LC-electrospray mass spectrometry. Rat liver microsomal incubation of KR-31543 in the presence of NADPH resulted in the formation of a metabolite M1. M1 was identified as N-(4-chlorophenyl)-N-(2-methyl-2H-tetrazol-5-ylmethyl)amine on the basis of LC-MS/MS analysis with the synthesized authentic standard. Rat CYP3A1 and 3A2 are the major CYP isozymes involved in the formation of M1.

Intragastrically Applicated CCl4-Thiopental Sodium Enhanced Lipid Peroxidation and Liver Fibrosis (Cirrhosis) in Rat: Malonedialdehyde as a Parameter of Lipid Peroxidation Correlated with Hydroxyproline as a Parameter of Collagen Synthesis (Deposition)

  • Kim, Ki-Young;Cho, Syung-Eun;Yu, Byung-Soo
    • Toxicological Research
    • /
    • 제25권2호
    • /
    • pp.71-78
    • /
    • 2009
  • We investigated the pathogenesis of liver tissue damage during the lipid peroxidation and fibrogenesis with the observation of correlations between the parameters of collagen synthesis (and deposition) and lipid peroxidation in liver fibrosis (cirrhosis) rats. Rats were randomly divided into two groups, normal and $CCl_4$-thiopental sod. intoxicated group. And the one group was treated intragastrically with the mixture of $CCl_4$-thiopental sod. 3 times per week for 3 weeks. The liver tissue and sera were used for the measurement of hydroxyproline (HYP), malonedialdehyde (MDA) and superoxide dismutase (SOD). Biochemical parameters such as aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), total-bilirubin and blood urea nitrogen (BUN) were measured. Additionally, the expression of collagen ${\alpha}1$(III) and $\beta$-actin mRNA was observed by RTPCR. The histological change in liver tissue was also observed by Masson's trichrome and H&E staining. Correlation analysis was carried by Spearman's rho method. All biochemical parameters except total-bilirubin were significantly higher in the $CCl_4$-thiopental sod. treated group than that of the normal group (p < 0.01). In the $CCl_4$-thiopental sod. treated group, Hyp as a parameter of collagen synthesis (deposition) and MDA as a metabolite of lipid peroxidation, were significantly elevated by 1.98 and 2.11 times higher than that of the normal group (p < 0.001) respectively. The activity of SOD in the $CCl_4$-thiopental sod. treated group is decreased significantly by 44.8% (p < 0.001). And collagen ${\alpha}1$(III) mRNA was more expressed in the $CCl_4$-thiopental sod. treated group than that of the normal group. However, the expression of $\beta$-actin mRNA is showed similar in both of groups. A good correlation was observed between the content of hyp and MDA concentration (r = 0.70, n = 40) in the two groups. And the correlation between the levels of hyp and SOD (r = -0.71, n = 25) is also reliable. However, no correlation were observed between MDA concentration and SOD (r = -0.40, n = 25) in the two groups. Elevated levels of MDA in $CCl_4$-thiopental sod. treated rats indicated enhancement of lipid peroxidation, which is accompanied by a decrease in SOD activity. Moreover, we could confirm that the parameters of collagen synthesis (and deposition) is in good correlation with the metabolite of lipid peroxidation (MDA) and the lipid peroxidation antagonizing enzyme (SOD). Hence, we propose that (1) lipid peroxidation and collagen synthesis (and deposition) could be enhanced by intragastrically application of $CCl_4$-thiopental sod. during a short terms. And (2) the intoxication of $CCl_4$-thiopental sod. could be used for monitoring of lipid peroxidation and collagen synthesis (and deposition) for test of antioxidant and antifibrotic agent.

Characterization of Deoxypodophyllotoxin Metabolism in Rat Liver Microsomes

  • Lee, Sang-Kyu;Jun, In-Hye;Kang, Mi-Jeong;Jeon, Tae-Won;Kim, Ju-Hyun;Seo, Young-Min;Shin, Sil;Choi, Jae-Ho;Jeong, Hye-Gwang;Lee, Seung-Ho;Jeong, Tae-Cheon
    • Biomolecules & Therapeutics
    • /
    • 제16권3호
    • /
    • pp.190-196
    • /
    • 2008
  • Deoxypodophyllotoxin (DPT) is a medicinal herb product isolated from Anthriscus sylvestris. DPT possesses beneficial activities in regulating immediate-type allergic reaction and anti-inflammatory activity through the dual inhibition of cyclooxygenase-2 and 5-lipoxygenase. In the present study, the metabolism of DPT was further characterized in rat liver microsomes isolated from male Sprague Dawley rats. The metabolism of DPT was NADPH-dependent. In addition, when liver microsomes were incubated with SKF-525A, a well-known CYP inhibitor, in the presence of $\beta$-NADPH, the metabolism of DPT was significantly inhibited. Using enriched rat liver microsomes, the anticipated isoforms of cytochrome P450s (CYPs) in the metabolism of DPT were partially characterized. Phenobarbital-induced microsomes increased in the formation of metabolite M1. The metabolite M3 was only produced in the enriched microsomes isolated from dexamethasone-treated rats. The results indicated that the metabolism of DPT would be CYP-dependent and that CYP2B and CYP3A might be important in the metabolism of DPT in rats.

Inhibitory Effect of Ginsenosides on NMDA Receptor-mediated Signals in Rat Hippocampal Neurons

  • Kim Sunoh;Choo Min-Kyung;Nah Seung-Yeol;Kim Dong-Hyun;Rhim Hyewhon
    • 고려인삼학회:학술대회논문집
    • /
    • 고려인삼학회 2002년도 학술대회지
    • /
    • pp.531-544
    • /
    • 2002
  • Ginseng is the best known and most popular herbal medicine used worldwide. Ameliorating effects of ginseng were observed on the models of scopolamine-induced, aged or hippocampal lesioned learning and memory deficits. Further beneficial effects of ginseng were observed on neuronal cell death associated with ischemia or glutamate toxicity. In spite of these beneficial effects of ginseng on the CNS, little scientific evidence shows at the cellular level. In the present study, we have employed cultures of rat hippocampal neurons and examined the direct modulation of ginseng on NMDA receptor-induced changes in $[Ca^{2+}]_i$ and -gated currents using fura-2-based digital imaging and perforated whole-cell patch-clamp techniques, respectively. We found that ginseng total saponins inhibited NMDA-induced but less effectively glutamate-induced increase in $[Ca^{2+}]_i$ Ginseng total saponins also modulated $Ca^{2+}$ transients evoked by depolarization with 50 mM KCI along with its own effects on $[Ca^{2+}]_i$. Among ginsenosides tested, ginsenoside $Rg_3$ was found to be the most potent component for ginseng actions on NMDA receptors. Furthermore, we examined the inhibitory effects ofbiotransformants of ginsenosides on NMDA receptor using purified stereoisomers of ginsenosides. 20(S)-ginsenoside $Rg_3$ and its metabolite, 20(S)-ginsenoside $Rh_3$, produced the strongest inhibition while 20(S)-ginsenoside $Rh_1$ and Compound K produced the moderate inhibition on NMDA-induced increase in $[Ca^{2+}]_i$. The data obtained suggest that the inhibition of NMDA receptors by ginseng, in particular by 20(S)-ginsenoside $Rg_3$ and its metabolite, 20(S)-ginsenoside $Rh_2$, could be one of mechanisms for ginsengmediated neuroprotective actions.

  • PDF

제주도 방선균 유래 oxazolomycin 계열 KSM-2690 B의 구조 결정과 항균활성에 관한 연구 (Structure Elucidation and Antibacterial Activity of Oxazolomycin Family KSM-2690 B Derived from Actinomycete Collected in Jeju Island)

  • 정형주;김주영;엄수현;문규호
    • 생약학회지
    • /
    • 제54권1호
    • /
    • pp.16-20
    • /
    • 2023
  • KSM-2690 B (1), a peptide-polyketide hybrid compound, was discovered from an actinomycete strain (CJD 1) isolated from Dong-Baek hill on Jeju Island, Republic of Korea. The chemical structure of 1 was identified by using NMR, MS, and UV spectroscopic analyses. Careful analysis of 1D and 2D NMR data revealed that KSM-2690 (1) has an oxazole ring, a β-lactone-γ-lactam spirocycle ring, and both triene and diene structures. KSM-2690 B (1) showed inhibitory activities against E. coli at 200 ㎍/mL.