• 제목/요약/키워드: Hepatic uptake

검색결과 123건 처리시간 0.02초

아시클로버-아시알로페투인 접합체의 간 포획 및 안정성 (Hepatic Uptake and Stability of Acyclovir-Asialofetuin Conjugate)

  • 손성호;허근;이영대;오두만;용철순
    • Journal of Pharmaceutical Investigation
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    • 제27권1호
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    • pp.1-10
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    • 1997
  • For the purpose of improving the chemotherapeutic index of acyclovir(ACV), it was conjugated with asialofetuin(AF), which has been reported to enter into hepatocytes. When $[H^3]$ acyclovir in itself or its conjugate were administered to rats, the latter was taken up more selectively by the liver than any other tissues. The stability of ACVMP-AF conjugate in phosphate buffer (pH 5.0) and rat liver homogenate showed a pseudo-first order profile. ACVMP-AF, however, was relatively stable in pH7.4 phosphate buffer and rat plasma. The conjugate was added to the isolated rat hepatocyte and cellular uptake was monitored by scintillation counting for up to 6 hours at $37^{\circ}C$. Hepatocytes incubated with the conjugate exhibited radioactivities significantly enhanced over control levels dose-dependently, i.e., a 3-40 fold increase in radioactivities was observed over controls at the conjugate concentrations of $0.1-10\;{\mu}g/ml$. The AUQ in the liver, kidney, spleen, intestine and lung was higher in treatment with ACVMP-AF than that in treatment with ACV. In treatment with ACVMP-AF, the weighted-average overall drug targeting efficiency(Te) for the liver was higher than in treatment with ACV(57.00 vs 13.31 %), and the weighted-average tissue exposure(Re) was 5.03 for the liver. These results indicated that ACVMP-AF conjugate was rapidly taken up by hepatocytes and could be an efficient and selective hepatic targeting system.

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염산의 항비타민제인 9-Methyl Folate가 흰쥐의 엽산대사에 미치는 영향 (9-Methyl Folate, an Antagonist of Folic Acid : Ist Effect on the Metabolism of Folic Acid in the Rat)

  • 민혜선
    • Journal of Nutrition and Health
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    • 제24권4호
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    • pp.337-343
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    • 1991
  • 엽산의 항비타민제인 9-methyl folate가 흰 쥐의 엽산 대사에 미치는 영향을 조사하기 위하여, Sprague-dawley 암컷 쥐를 엽산 결핍식이군, 대조군, x-methyl folate 투여군으로 나누어 실험하였다. 9-methyl folate는 실험동물에게 엽산 결핍증을 유발시키는 x-methyl folate의 성분 가운데 주된 항비타민제이며, 본 실험에서는 식이 1kg당 5g의 x-methyl folate를 첨가하였다. x-methyl folate를 실험동물에게 먹였을 때 히스티딘의 산화속도와 간장내의 엽산 농도가 크게 저하되었으며, $[^{3}H]folate$를 복강에 투여한 후 24시간 내에 간장에 보유되는 엽산의 양도 x-methyl folate 투여군에 있어 유의적인 감소를 보였다. 이 실험 결과에서 9-methyl folate는 흰 쥐에 있어 엽산이 간으로 유입되어 보유되는 과정을 저해하므로써 간장 내의 엽산의 양을 저하시키며, 그 결과 히스티딘의 산화속도도 저하된 것으로 보인다.

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숫컷 생쥐에서 타우린 투여에 의한 간내 글루타치온의 감소 (Reduction of Hepatic Glutathione by Acute Taurine Treatment in Male Mice)

  • 이선영;곽혜은;김영철
    • 약학회지
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    • 제47권4호
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    • pp.218-223
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    • 2003
  • Effect of taurine treatment on metabolism of glutathione (GSH) was studied in adult male ICR mice. An acute injection of taurine (250 mg/kg, ip) resulted in a significant decline of hepatic GSH level at t = 6 hr, but plasma GSH level was not altered. The activity of GSH-related enzyme in liver, such as GSH peroxidase, GSSG reductase, GSH S-transferases, ${\gamma}$-glutamylcysteine synthetase or ${\gamma}$-glutamyltranspeptidase, was not affected by taurine at t = 2.5 or 6 hr. Plasma cysteine and cystine levels were elevated rapidly following taurine treatment. Hepatic cysteine level was decreased by taurine, reaching a level approximately 70% of control at t = 4 and 6 hr. In conclusion, the results indicate that an acute dose of taurine decreases hepatic GSH level by reducing the availability of cysteine, an essential substrate for synthesis of this tripeptide in liver. It is also suggested that taurine may decrease the cysteine uptake by competing with this S-amino acid for a non-specific amino acid transporter.

MICROCIRCULATORY ABERRATIONS IN THE ISOLATED PERFUSED RAT LIVER INDUCED BY SODIUM CYANIDE, ANOXIA OR ACETAMINOPHEN

  • Jung, Kihwa
    • Toxicological Research
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    • 제5권1호
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    • pp.27-35
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    • 1989
  • When acetaminophen (25mM) was introduced into the perfused rat liver, the hepatic O2 uptake was rapidly inhibited first and then later slow-down. The rapid inhibition was found to be due to mitochondrial blockade, whereas the so-called slow inhibition" was associated with microcirulatory aberrations as evidenced by inhomogneous staining of the liver tissue by trypan blue infusion (0.1%). NaCN (0.5mM) also caused rapid and slow respiratory inhibitions, giving heterogeneous trypan blue staining.ning.

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$^{99m}Tc$-colloid 섭취를 보인 췌장의 도세포종 : 증례보고 (Radiocolloid Uptake in the Pancreas Islet Cell Tumor: Case Report)

  • 양우진;정수교;연수경;신경섭;박용휘
    • 대한핵의학회지
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    • 제28권1호
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    • pp.145-147
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    • 1994
  • Colloid uptake in various hepatic conditions such as focal nodular hyperplasia, regenerating nodules in the cirrhotic liver, hamartoma, hemangioma and rarely hepatoma has been documented. Extrahepatic tumors may show colloid uptake and they include splenic hemangioma, malignant fibrous histiocytoma, breast carcinoma and Kaposi's sarcoma. The mechanism of colloid uptake in those lesions is associated with phagocytic activity in or around the tumors. We report a pancreas islet cell tumor that showed colloid uptake on $^{99m}Tc$-phytate liver scan without histologic evidence of phagocytosis by tumor cells or infiltration of phagocytes in the tumor Microscopically the tumor was highly vascular and showed diffuse hemorrhage throughtout the tumor. We postulated that extravasation of the colloid into the tumor insterstitium caused nonspecific colloid uptake in this tumor. It is expected that hemorrhagic tumor may show nonspecific colloid uptake without phagocytosis in or about the lesion.

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골스캔에서 우연히 발견된 간혈관종 (Incidental Visualization of Hepatic Hemangioma by Tc-99m-HDP Bone Scan)

  • 정용안;오주현;김정호;유이령;김성훈;손형선;정수교
    • 대한핵의학회지
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    • 제39권4호
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    • pp.266-267
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    • 2005
  • Hepatic hemangioma is the most common benign liver tumor and must be considered in the differential diagnosis of other space occupying hepatic masses. A 54-year-old man was referred to evaluate bone metastases of lung adenocarcinoma. In our case, we thought that a focal hepatic uptake in the bore scan was a metastatic lesion, because of underlying lung adenocarcinoma. However, the findings of abdominal CT and Tc-99m RBC scan results were deemed to be characteristic of hepatic hemangioma. The biopsy of the lesion was not performed.

Evaluation of Fishmeal Supplement with Net Nitrogen Flux by the Portal-drained Viscera and the Liver in Mature Sheep

  • Fukuma, T.;Taniguchi, K.;Obitsu, T.
    • Asian-Australasian Journal of Animal Sciences
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    • 제18권9호
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    • pp.1255-1261
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    • 2005
  • The objective of this study was to evaluate the net flux response of nitrogen compounds (alpha-amino N, ammonia N, urea N, essential amino acids) across the portal-drained viscera (PDV), liver and total splanchnic tissues of mature wethers to increasing level of dietary fishmeal (FM) supplementation. Four wethers (average body weight, 64 kg) with chronic indwelling catheters into the portal, hepatic and mesenteric veins and the abdominal aorta were used in a 4${\times}$4 Latin square design. A basal diet consisting of 0.7 hay and 0.3 concentrate was fed twice daily with a fixed amount at 1.4 times maintenance energy (1.3 kg/day on a dry matter basis). The supplementation proportion of FM as treatment was 0, 0.03, 0.06 and 0.09 to the amount of the basal diet to contain 119, 137, 154 and 170 g crude protein per kg dietary dry matter, respectively. Blood flows through PDV and liver did not differ (p>0.05) among the treatments. Both net PDV release and hepatic uptake of alpha amino acid N increased linearly (p<0.05) in response to increased dietary FM, which resulted in similar total splanchnic release of alpha-amino N among the treatments. Similarly, increased dietary FM increased net PDV absorption and hepatic removal of ammonia N linearly (p<0.05). Hepatic synthesis and total splanchnic release of urea N increased linearly (p<0.01) with increased dietary FM, but PDV uptake of urea N did not respond to increased dietary FM. Linear regression equations between the increases in FM N intake and PDV net flux indicated that 0.34 and 0.30 of FM N was absorbed in the form of alpha-amino N and ammonia N, respectively. The results demonstrated that FM supplementation provides more alpha-amino N than ammonia N to the liver, but the alpha-amino acid N absorption is less than the expected metabolizable protein N from FM supplementation.

음이온계 약물의 간수송과정에 있어서 대향수송의 약물동력학적 모델링 및 시뮬레이션 (Pharmacokinetic Modelling and Simulation of the Counter-transport in the Hepatic Transport of Organic Anions)

  • 송석길;이준섭;정연복
    • 약학회지
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    • 제49권4호
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    • pp.275-283
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    • 2005
  • The purpose of the present study was to kinetically investigate the carrier-mediated uptake in the hepatic transport of organic anions, and to simulate the 'in vivo counter-transport' phenomena, using kinetic model which was developed in this study. The condition that the mobility of carrier-ligand complex is greater than that of free carrier is not essential for the occurrence of 'counter-transport' phenomenon. To examine the inhibitory effects on the initial uptake of organic anions by the liver, it is necessary to judge whether the true counter-transport mechanism (trans-stimulation) is working or not. Effects of bromophenol blue (BPB) or bromosulfophthalein (BSP) on the plasma disappearance curves of a 1-anilino-8-naphthalene sulfonate (ANS) were then kinetically analyzed based on a flow model, in which the ligand is eliminated only from the peripheral compartment (liver compartment). Moreover, 'in vivo counter-transport' phenomena were simulated based on the perfusion model which incorporated the carrier-mediated transport and the saturable intracellular binding. The 'in vivo counter-transport' phenomena in the hepatic transport of a organic anions were well demonstrated by incorporating the carrier-mediated process. However, the 'in vivo counter-transport' phenomena may be also explained by the enhancement of back diffusion due to the displacement of intracellular binding. In conclusion, one should be more cautious in interpreting data obtained from so-called 'in vivo counter-transport' experiments.

A Case of Gastric Large Cell Neuroendocrine Carcinoma with Multiple Liver Metastasis Treated with Hepatic Artery Infusion Chemotherapy Followed by Surgery

  • Sung Bum Kim;Kook Hyun Kim;Tae Nyeun Kim
    • Journal of Digestive Cancer Research
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    • 제3권1호
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    • pp.26-29
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    • 2015
  • A 73-year-old male visited our hospital with a complaint of general weakness. He underwent pyloric preserving pancreas-toduodenectomy due to ampullary cancer three years ago. Abdominal computed tomography scan at initial visit revealed multiple hepatic masses. A PET-CT scan showed multiple FDG uptakes at whole liver. He underwent hepatic artery infusion chemotherapy (HAIC) for five cycles. During the first cycle of HAIC, he developed gastric ulcer bleeding and endoscopic hemostasis was done successfully. Esophagogastroduodenoscopy after the 5th cycle of HAIC revealed ulcer scar at gastric angle. PET-CT scan at 12 months showed no FDG uptake at liver, but a focal FDG uptakes at stomach and peri-gastric lymph nodes were newly developed. Esophagogastroduodenoscopy revealed about 3 cm sized mass at gastric angle. He underwent surgery and pathologic examination revealed large cell neuroendocrine carcinoma. We report a case of gastric large cell neuroendocrine carcinoma with liver metastasis treated with HAIC followed by surgery.

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정상 한국인 대퇴골두의 $^{99m}Tc-Tin$ Colloid 섭취율 ($^{99m}Tc-Tin$ Colloid Uptake Ratio of Femoral Head in Healthy Korean)

  • 지원희;손형선;김춘열;박용휘
    • 대한핵의학회지
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    • 제23권2호
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    • pp.215-218
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    • 1989
  • Tc-99m-tin colloid distribution in the hip is studied in 76 patients with no hepatic and hip disorder, because knowledge of normal uptake pattern in the hip is important in evaluation of femoral head vasculature after a fracture. The uptake in femoral head is decreased or disappeared with increasing age due to conversion of red marrow to white marrow.

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