• Title/Summary/Keyword: Efflux system

Search Result 72, Processing Time 0.021 seconds

Evaluating the Regulation of P-glycoprotein by Phytochemicals Using Caco-2 Cell Permeability Assay System

  • Choi, Ran Joo;Kim, Yeong Shik
    • Natural Product Sciences
    • /
    • v.20 no.1
    • /
    • pp.1-6
    • /
    • 2014
  • P-glycoprotein (P-gp) is a permeability glycoprotein also known as multidrug resistance protein 1 (MDR1). P-gp is an ATP-binding cassette (ABC) transporter that pumps various types of drugs out of cells. These transporters reduce the intracellular concentrations of drugs and disturb drug absorption. The Caco-2 cell permeability assay system is an effective in vitro system that predicts the intestinal absorption of drugs and the functions of enzymes and transporters. Rhodamine-123 (R-123) and digoxin are well-known P-gp substrates that have been used to determine the function of P-gp. Efflux of P-gp substrates by P-gp has been routinely evaluated. To date, a number of herbal medicines have been tested with Caco-2 cell permeability assay system to assess bioavailability. There are growing efforts to find phytochemicals that potentially regulate P-gp function. The Caco-2 cell permeability assay system is a primary strategy to search for candidates of P-gp inhibitors. In this mini review, we have summarized the P-gp modulation by herbal extracts, decoctions or single components from natural products using Caco-2 cell permeability assays. Many natural products are known to regulate P-gp and herbal medicines could be used in combination with conventional drugs to enhance bioavailability.

Effect of Probenecid on Tetraethylammonium (TEA) Transport Across Basolateral Membrane of Rabbit Proximal Tubule

  • Choi, Tae-Ryong;Kim, Yong-Keun
    • The Korean Journal of Physiology
    • /
    • v.30 no.2
    • /
    • pp.249-256
    • /
    • 1996
  • The effect of probenecid on the transport of tetraethylammonium (TEA) was studied in renal cortical slices and isolated membrane vesicles to investigate the interaction of organic anion with the organic cation transport system in proximal tubule. Probenecid reversibly inhibited TEA uptake by renal cortical slices in a dose-dependent manner over the concentration range of 1 and 5 mM. The efflux of TEA was not affected by the presence of 3 mM probenecid. Kinetic analysis indicated that probenecid decreased Vmax without significant change in Km. Probenecid inhibited significantly tissue oxygen consumption at concentrations of 3 and 5 mM. However, probenecid did not significantly reduce TEA uptake in brush border and basolateral membrane vesicles prepared from renal cortex even at a concentration as high as 10 mM. These results indicate that probenecid reduces TEA uptake in cortical slices by inhibiting tissue metabolism rather than by an interaction with the organic ration transporter.

  • PDF

PUM: Processing Unit Module Design of Intrusion Detector for Large Scale Network (대규모 네트워크를 위한 침입 탐지결정모듈 설계)

  • 최인수;차홍준
    • Journal of the Korea Society of Computer and Information
    • /
    • v.7 no.2
    • /
    • pp.53-58
    • /
    • 2002
  • the popularity of uses for internet has been needed to information security. thereforce, intrusion, information leakage and modification, change or intentional efflux to computer system aspects of information security have been resulted in requirement of intrusion detection from outer at user authentication. this problem Presents design of PUM(Processing Unit Module) which analyze both the host log generated by sever host systems that various case for intellectualized intrusion method and network_packet on networks in large scale network.

  • PDF

Specific Inhibition of Polar Auxin Transport by n-Octanol in Maize Coleoptiles (옥수수(Zea mays L.) 자엽초 조직 절편에서 n-Octanol에 의한 옥신 극성 이동 억제)

  • 윤인선
    • Journal of Plant Biology
    • /
    • v.36 no.1
    • /
    • pp.67-74
    • /
    • 1993
  • Both polar and gravity-induced lateral transport of auxin was markedly reduced in corn coleoptile segments by octanol treatment. Octanol enhance net auxin uptake without affecting that of benzoic acid, suggesting that the effect did not result from a nonspecific action on general membrane permeability. Since naphthylphthalamic acid (NPA) action on both transport and net uptake of auxin was substantially decreased in the presence of octanol, a specific interaction of octanol with the NPA site (efflux carrier) can be postulated. Studies on in vitro binding of NPA to membrane vesicles indicated that octanol did not interfere with NPA binding. When basipetal transport of auxin was impared by plasmolysis, octanol still inhibited auxin transport in the plasmolyzed tissues. The results ruled out the possibility of octanol acting at the plasmodesmata. Kinetic analysis of growth indicated that IAA-sustained growth was rapidly blocked by octanol implicating a common system by which auxin transport is linked to auxin action. Possible mechanisms for octanol action will be discussed.

  • PDF

Transport Properties of Aromatic Amino Acids by Amino Acid Transporter TAT1 (아미노산 수송체 TAT1에 의한 방향족 아미노산의 수송특성)

  • 김윤배;김명수;윤정훈;박주철;국중기;정해만;최봉규;정규용;김종근
    • Journal of the Korean Society of Food Science and Nutrition
    • /
    • v.31 no.5
    • /
    • pp.775-781
    • /
    • 2002
  • The T-type amino acid transporter 1 (TATI) is a Na$^{+}$-independent amino acid transporter which selectively trans- ports aromatic amino acids subserving the amino acid transport system T. To understand the transport properties of aromatic amino acids by human TAT1 (hTATl ), we have examined the hTATl -mediated aromatic amino acid transports using a Xenopus laeuis oocyte expression system. When expressed in Xenopin laeuis oocytes, hTATl induced L- [$^{14}$ C]tryptophan transport which was not dependent on Na$^{+}$ or Cl$^{[-10]}$ in the medium. Uptake was time-dependent and exhibited a linear dependence on incubation time up to 30 min. The L- ($^{14}$ C)tryptophan uptake was highly inhibited by L-isomers of tryptophan, tyrosine and phenylalanine, whereas other L-amino acids did not inhibit hTATl -mediated L- ($^{14}$ C)tryptophan uptake. The hTATl induced the relatively low-affinity transport of aromatic amino acids such as L- ($^{14}$ C)tryptophan, L- ($^{14}$ C)tyrosine and L- ($^{14}$ C)phenylalanine (Km values: 450~750 $\mu$M), consistent with the properties of classical amino acid transport system T. The L- ($^{14}$ C)tryptophan uptake did not show any remarkable pH dependence within the pH range of 5.5 to 8.5. The time-dependent efflux of L- ($^{14}$ C)tryptophan was detected from the oocytes expressing hTATl, which was not affected by the presence or absence of L-tryptophan in the extracellular medium, indicating that hTATl-mediated transport is due to the facilitated diffusion. Expression of hTATl in Xenopu laevis oocytes induced the transport of tryptophan, tyrosine and phenylalanine, indicating that hTATl is a transporter subserving system T These results suggest that hTATl has essential roles in the absorption of aromatic amino acids from epithelial cells to the blood stream. Hecause hTATl is proposed to be crucial to the efficient absorption of aromatic amino acids from intestine and kidney, its defect such as blue diaper syndrome could be involved in the disruption of aromatic amino acid transport.ort.

Net Ecosystem Productivity Determined by Continuous Measurement Using Automatic Sliding Canopy Chamber

  • Kim, Gun-Yeob;Lee, Seul-Bi;Lee, Jong-Sik;Choi, Eun-Jung
    • Korean Journal of Soil Science and Fertilizer
    • /
    • v.45 no.6
    • /
    • pp.1179-1186
    • /
    • 2012
  • For better understanding of carbon cycle dynamics of an agro-ecosystem, an accurate assessment of seasonal and daily $CO_2$ flux is essential to understand the relationship between various environmental factors and crop productivity. We developed the automatic sliding canopy chamber (ASCC) system that measured continuous net ecosystem productivity (NEP) over whole growing season under the natural meteorological rhythm. The ASCC was composed of two main parts which were sliding part for measuring NEP, and automatic opening and closing chamber (AOCC) for measuring soil respiration (SR) on the soil surface. The ASCC was developed by using open flow method for measuring soil $CO_2$ efflux. The disturbance of natural meteorological condition was minimized by opening the base frames. In the field test with barley (Hordeum vulgare L.), NEP was calculated at $140mg\;CO_2\;m^{-2}h^{-1}$ on a clear day using continuous data and eliminated the possibility of overestimate about 16% using one hour data during the day time. Unlike other small scale chamber system, installation on cropping-field made it possible to take any modifications which might be caused by natural environmental condition.

Accumulation of Uric Acid in Rabbit Kidney Cortical Slices (가토 신피질 절편에서 Uric Acid 이동)

  • Yee, Sung-Tae;Lim, Chae-Joon;Woo, Jae-Suk;Kim, Yong-Keun
    • The Korean Journal of Physiology
    • /
    • v.21 no.2
    • /
    • pp.283-289
    • /
    • 1987
  • Uric acid transport across the basolateral membrane of renal proximal tubules was studied in rabbit kidney cortical slices. Uric acid uptake was greater under $O_2$ atmosphere compared to under $N_2$ atmosphere, and was increased with $Na^{2+}$ concentration in incubation medium. Uric acid inhibited PAH uptake but not TEA uptake and did trans-stimulated PAH efflux. PAH also inhibited uric acid uptake. Uric acid uptake was inhibited by harmaline, ouabin, SITS, DIDS and pyrazinoic acid. The inhibition of PAH uptake by these inhibitors also was reasonably comparable to that of uric acid uptake. These results suggest that uric acid was transported across the basolateral membrane of renal tubule by a carrier-mediated process which was by a common transport system with PAH in rabbit.

  • PDF

Immunochemical Studies for the Characterization of Purified $(Na^+,\;K^+)-ATPase$ and Its Subunits with a Special Reference of Their Effect on Monovalent Cation Transport in Reconstituted $(Na^+,\;K^+)-ATPase$ Vesicles

  • Rhee, H.M.;Hokin, L.E.
    • The Korean Journal of Pharmacology
    • /
    • v.26 no.1
    • /
    • pp.35-49
    • /
    • 1990
  • A highly purified $(Na^+,\;K^+)-ATPase$ from the rectal gland of Squalus acanthias and from the electric organ of Electrophorus electricus has been used to raise antibodies in rabbits. The 97,000 dalton catalytic subunit and glycoprotein derived from the rectal gland of spiny shark were also used as antigens. The two $(Na^+,\;K^+)-ATPase$ holoenzymes and the two shark subunits were antigenic. In Ouchterlony double diffusion experiments, these antibodies formed precipitation bands with their antigens. Antibodies prepared against the two subunits of shark holoenzyme also formed precipitation bands with their antigens and shark holoenzyme, but not with eel holoenzyme. These observations are in good agreement with inhibitory effect of these antibodies on the catalytic activity of $(Na^+,\;K^+)-ATPase$ both from the shark and the eel, since there is very little cross-reaction between the shark anticatalytic subunit antibodies and the eel holoenzyme. The maximum antibodies titer of the anticatalytic subunit antibodies is found to be 6 weeks after the initial single exposure to this antigen. Multiple injections of the antigen increased the antibody titer. However, the time required to produce the maximum antibody titer was approximately the same. These antibodies also inhibit catalytic activity of $(Na^+,\;K^+)-ATPase$ vesicles reconstituted by a slow dialysis of cholate after solubilization of the enzyme in a presonicated mixture of cholate and phospholipid. In these reconstituted $(Na^+,\;K^+)-ATPase$ vesicles, effects of these antibodies on the fluxes of $Na^+$, $Rb^+$, and $K^+$ were investigated. Control or preimmune serum had no effect on the influx of $^{22}Na^+$ or the efflux of $^{86}Rb^+$. Immunized sera against the shark $(Na^+,\;K^+)-ATPase$ holoenzyme, its glycoprotein or catalytic subunit did inhibit the influx of $^{22}Na^+$ and the efflux of $^{86}Rb^+$. It was also demonstrated that these antibodies inhibit the coupled counter-transport of $Na^+$ and $K^+$ as studied by means of dual labeling experiments. However, this inhibitory effect of the antibodies on transport of ions in the $(Na^+,\;K^+)-ATPase$ vesicles is manifested only on the portion of energy and temperature dependent alkali metal fluxes, not on the portion of ATP and ouabain insensitive ion movement. Simultaneous determination of effects of the antibodies on ion fluxes and vesicular catalytic activity indicates that an inhibition of active ion transport in reconstituted $(Na^+,\;K^+)-ATPase$ vesicles appears to be due to the inhibitory action of the antibodies on the enzymatic activity of $(Na^+,\;K^+)-ATPase$ molecules incorporated in the vesicles. These findings that the inhibitory effects of the antibodies specific to $(Na^+,\;K^+)-ATPase$ or to its subunits on ATP and temperature sensitive monovalent cation transport in parallel with the inhibitory effect of vesicular catalytic activity by these antibodies provide direct evidence that $(Na^+,\;K^+)-ATPase$ is the molecular machinery of active cation transport in this reconstituted $(Na^+,\;K^+)-ATPase$ vesicular system.

  • PDF

Effect of Relative Humidity on Calcium Uptake of Tomato Plant (상대(相對) 습도(濕度)가 토마토의 Ca흡수(吸收)에 미치는 영향(影響))

  • Cho, Ill-Hwan
    • Korean Journal of Soil Science and Fertilizer
    • /
    • v.30 no.2
    • /
    • pp.178-183
    • /
    • 1997
  • The effect of different relative humidity(RH) of atmosphere on the uptake of calcium by tomato plant was investigated through an experiment in the protected cultivation system. The RH regime was imposed by humidifiying by humidifier in one plot, and by mulching the ridge to cut down the evaporation of water to lower the RH, in another plot. During the course of plant growth, RH in the humidified plot, at noon, was about 70%, while in non-humidufied plot, RH was about 50%. The humidification also resulted in the lowering of temperature significantly(by about, $3.1^{\circ}C$). This higher RH of atmosphere under humidifying treatment, resulted in the increase in the water efflux rate of root significantly(greater by 0.24g/g dry root/h than that under mulching treatment). Relatively severe occurrence of blossom end rot(23%) was observed in the humidifying treatment, while no such symptom occurred in mulching plot. The efflux rates of Ca, K and Mg were found to be higher in the humidifying plot. It was also observed that the concentrations of Ca, Mg and K in the xylem solution was 2-4 times higher than that of gydroponic solution. This suggested that the occurrence of blossom end rot, under high RH of atmosphere, would not be due to the decrease in the uptake of Ca per se, by tomato plant, but due to anomalies in the distribution of it within the plant.

  • PDF

Evolution and Changes of Coastal Topography due to Jetty Construction at Namdae River Mouth (도류제 건설 후 남대천 하구의 해안선 생성 및 변화)

  • Kim, In Ho;Lee, Seong Dae
    • KSCE Journal of Civil and Environmental Engineering Research
    • /
    • v.28 no.3B
    • /
    • pp.315-321
    • /
    • 2008
  • Recently, in the light of environments and utilization, countermeasures to preserve beaches in coastal area are required without depending on such as jetties and breakwaters. The necessity of integrated sand management including not only coastal sediment but also sediment discharge from hinterland rivers is increased so as to establish long-term counterplan for sediment transport. In this regard, the following subjects are examined in this study; efficient ways for discharged sand to be transported from a river to the neighboring coast, the river terrace occurrence and its growth at the river delta, measures to improve storage efficiency of the discharged sand and measures to prevent the sand resources from being discharged into the deep sea during flooding. In recent, A jetty of 260 m length was constructed at Namdae River mouth in the year of 2005 as a countermeasure against the occurrence of sand-bar at river mouth and its close. In this study, a series of numerical experiments were carried out to investigate the characteristics of sediment transport and morphological change due to the construction of jetty at the entrance of Namdae River mouth. Firstly, The sand discharge from Namdae River is quantified by one-dimensional numerical analysis assuming the mixed sand of three different particle diameters. Then, in order to understand the transport behavior of the sand discharge from river and river mouth phenomena the numerical experiments were then conducted to examine the flow behaviors of river efflux and wind generated circulations in coastal area. And, after establishing the numerical model system, which predicts the sea bed changes obtained from the flux model combining with the wave propagation, wave-induced currents and sediment transport models, the sediment transport in the vicinity of Namdae River mouth is analyzed.