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PubMed2004

Capillary electrophoretic studies on the migration behavior of cationic solutes and the influence of interactions of cationic solutes with sodium dodecyl sulfate on the formation of micelles and critical micelle concentration.

The migration behavior of cationic solutes and influences of the interactions of cationic solutes with sodium dodecyl sulfate (SDS) on the formation of micelles and its critical micelle concentration (CMC) were investigated by capillary electrophoresis at neutral pH. Catecholamines and structurally related compounds, including epinephrine, norepinephrine, dopamine, norephedrine, and tyramine, which involve different extents of hydrophobic, ionic and hydrogen-bonding interactions with SDS surfactant, are selected as cationic solutes. The dependence of the effective electrophoretic mobility of cationic solutes on the concentration of surfactant monomers in the premicellar region provides direct evidence of the formation of ion-pairs between cationic solutes and anionic dodecyl sulfate monomers. Three different approaches, based on the variations of either the effective electrophoretic mobility or the retention factor as a function of surfactant concentration in the premicellar and micellar regions, and the linear relationship between the retention factor and the product of a distribution coefficient and the phase ratio, were considered to determine the CMC value of SDS micelles. The suitability of the methods used for the determination of the CMC of SDS with these cationic solutes was discussed. Depending on the structures of cationic solutes and electrophoretic conditions, the CMC value of SDS determined varies in a wide concentration range. The results indicate that, in addition to hydrophobic interaction, both ionic and hydrogen-bonding interactions have pronounced effects on the formation of SDS micelles. Ionic interaction between cationic solutes and SDS surfactant stabilizes the SDS micelles, whereas hydrogen-bonding interactions weakens the solubilization of the attractive ionic interaction. The elevation of the CMC of SDS depends heavily on hydrogen-bonding interactions between cationic solutes and SDS surfactant. Thus, the CMC value of SDS is remarkably elevated with catecholamines, such as epinephrine and norepinephrine, as compared with norephedrine. In addition, the effect of methanol content in the sample solution of these cationic solutes on the CMC of SDS was also examined.

Cations↗
PubMed1967

Discrimination between alkali metal cations by yeast. II. Cation interactions in transport.

K(+) is a competitive inhibitor of the uptake of the other alkali metal cations by yeast. Rb(+) is a competitive inhibitor of K(+) uptake, but Li(+), Na(+), and Cs(+) act like H(+). At relatively low concentrations they behave as apparent noncompetitive inhibitors of K(+) transport, but the inhibition is incomplete. At higher concentrations they inhibit the remaining K(+) transport competitively. Ca(++) and Mg(++) in relatively low concentrations partially inhibit K(+) transport in an apparently noncompetitive manner although their affinity for the transport site is very low. In each case, in concentrations that produce "noncompetitive" inhibition, very little of the inhibiting cation is transported into the cell. Competitive inhibition is accompanied by appreciable uptake of the inhibiting cation. The apparently noncompetitive effect of other cations is reversed by K(+) concentrations much higher than those necessary to essentially "saturate" the transport system. A model is proposed which can account for the inhibition kinetics. This model is based on two cation-binding sites for which cations compete, a carrier or transporting site, and a second nontransporting (modifier) site with a different array of affinities for cations. The association of certain cations with the modifier site leads to a reduction in the turnover of the carrier, the degree of reduction depending on the cation bound to the modifier site and on the cation being transported.

Biological Transport↗
PubMed1997

[Elution behaviors of cations on the serial columns combining a cation exchange column with an ion exclusion column].

The elution behaviors of cations (Na+, NH4+, K+, Ca2+ and Mg2+) on the serially connected cation exchange column (ICS-C25) and ion exclusion column (TSKgel OApak-A) were investigated. As shown in Figure 1, three peaks were observed for each cation when a mixture of tartaric acid (TA) and 2,6-pyridinedicarboxylic acid (PDC) was used as eluent. In ion exchange chromatography, the background conductivity (G0) of carboxylic acid (HR) eluent which is based on the dissociation of HR, can be expressed as follows: G0 = C0H lambdaH + C0R lambdaR (1) where C0H and C0R are the initial concentration, lambdaH and lambdaR are the equivalent concentration of H+ and R-, respectively. The concentration of eluent anion R- in mobile phase is reduced when the cations (M) are eluted from cation exchange column, because the R- forms some complexes with the cations. At this time, the conductivity (G) of the eluent will be G = CM lambdaM + (C0R - C'R) lambdaR + (C0H - CM) lambdaH (2) where CM is the concentration of cations, and C'R is a reduce of R-. The peaks on chromatogram results from a change in conductance (deltaG), and in the conditions of the paper. DeltaG = G - G0 = CM (lambdaM - lambdaH) - C'TA lambdaTA - C'PDC lambdaPDC (3). On the ion exclusion column, the eluent anion TA and PDC were retained at different capacity factor by an ion exclusion mechanism while the cations have not any retention. That is to say, the first peak of each cation is caused by elution of the cation and the depletion of eluent ion (H+) in the mobile phase. The second and third peaks have appeared corresponding to the depletion of TA and PDC anion in mobile phase, respectively.

English Abstract↗
PubMed2000

Simultaneous ion-exclusion/cation-exchange chromatography of anions and cations in acid rain waters on a weakly acidic cation-exchange resin by elution with sulfosalicylic acid.

A simple, selective, and sensitive method for the simultaneous determination of anions (sulfate, nitrate, and chloride) and cations (sodium, ammonium, potassium, magnesium, and calcium) in acid rain waters was developed using ion-exclusion/ cation-exchange chromatography with conductimetric detection. A weakly acidic cation-exchange resin column (Tosho TSKgel OA-PAK-A) and a sulfosalicylic acid-methanol-water eluent was used. With a mobile phase comprising 1.25 mM sulfosalicylic acid in methanol-water (7.5:92.5) at 1.2 ml/min, simultaneous separation and detection of the above anions and cations was achieved in about 30 min. Linear calibration plots of peak area versus concentration were obtained over the concentration ranges 0-1.0 mM for anions (R=0.9991) and 0-0.5 mM for cations (R=0.9994). Detection limits calculated at S/N=3 ranged from 4.2 to 14.8 ppb for the anions and from 2.4 to 12.1 ppb for the cations. The reproducibility of retention times was 0.14-0.15% relative standard deviation (RSD) for anions and 0.18-0.31% for cations, and reproducibility of chromatographic peak areas was 1.22-1.75% RSD for anions and 1.81-2.10% for cations. The method was applied successfully to the simultaneous determination of anions and cations in aerosols transported from mainland China to central Japan, as determined by a meteorological satellite data analyzer.

Anions↗
PubMed2001

Comparison of "type I" and "type II" organic cation transport by organic cation transporters and organic anion-transporting polypeptides.

Previous inhibition studies with taurocholate and cardiac glycosides suggested the presence of separate uptake systems for small "type I" (system1) and for bulky "type II" (system2) organic cations in rat hepatocytes. To identify the transport systems involved in type I and type II organic cation uptake, we compared the organic cation transport properties of the rat and human organic cation transporter 1 (rOCT1; hOCT1) and of the organic anion-transporting polypeptides 2 and A (rat Oatp2; human OATP-A) in cRNA-injected Xenopus laevis oocytes. Based on characteristic cis-inhibition patterns of rOCT1-mediated tributylmethylammonium and Oatp2-mediated rocuronium uptake, rOCT1 and Oatp2 could be identified as the organic cation uptake systems1 and 2, respectively, in rat liver. While hOCT1 exhibited similar transport properties as rOCT1, OATP-A- but not Oatp2-mediated rocuronium uptake was inhibited by the OATP-A substrate N-methyl-quinidine. The latter substrate was also transported by rOCT1 and hOCT1, demonstrating distinct organic cation transport activities for rOCT1 and Oatp2 and overlapping organic cation transport activities for hOCT1 and OATP-A. Finally, the data demonstrate that unmethylated quinidine is transported by rOCT1, hOCT1, and OATP-A at pH 6.0, but not at pH 7.5, indicating that quinidine requires a positive charge for carrier-mediated uptake into hepatocytes. In conclusion, the studies demonstrate that in rat liver the suggested organic cation uptake systems1 and 2 correspond to rOCT1 and Oatp2, respectively. However, the rat-based type I and II organic cation transporter classification cannot be extended without modification from rat to human.

Androstanols↗
PubMed2003

Cationic lipids and cationic ligands induce DNA helix denaturation: detection of single stranded regions by KMnO4 probing.

Cationic lipids and cationic polymers are widely used in gene delivery. Using 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) as a cationic lipid, we have investigated the stability of the DNA in DOTAP:DNA complexes by probing with potassium permanganate (KMnO4). Interestingly, thymidines followed by a purine showed higher susceptibility to cationic ligand-mediated melting. Similar studies performed with other water-soluble cationic ligands such as polylysine, protamine sulfate and polyethyleneimine also demonstrated melting of the DNA but with variations. Small cations such as spermine and spermidine and a cationic detergent, cetyl trimethylammonium bromide, also rendered the DNA susceptible to modification by KMnO4. The data presented here provide direct proof for melting of DNA upon interaction with cationic lipids. Structural changes subsequent to binding of cationic lipids/ligands to DNA may lead to instability and formation of DNA bubbles in double-stranded DNA.

Base Sequence↗
PubMed1992

Dietary cation-anion balance and cation source effects on production and acid-base status of heat-stressed cows.

Two 4 x 4 replicated Latin square studies, each containing 8 lactating Holstein cows, were conducted simultaneously in south Georgia during the summer. The effects of dietary cation source (Na or K) and increasing dietary cation-anion balance (milliequivalents of Na + K - Cl per kilogram of feed DM) within cation source (control = 120.4 meq/kg of feed DM; Na source = 219.7, 347.8, 464.1 meq/kg of feed DM; K source = 231.2, 352.6, 456.0 meq/kg of feed DM) were determined on performance and acid-base chemistry during hot, humid weather. Cow body temperatures were elevated by environmental conditions but were not affected by dietary cation-anion balance. Differences in body temperature from dietary cation source probably were related to differences in cow BW. Intake of DM increased linearly, but yields of milk and FCM did not change with increasing dietary cation-anion balance, and cation source had no effect. Milk fat and protein percentages were not altered by dietary cation-anion balance, and greater milk fat and protein percentages from cows offered the Na versus K source diets probably were due to differences between cows in the two Latin squares. Alterations in blood acid-base chemistry with increasing dietary cation-anion balance were as expected. Greater blood buffering capacity, indicated by blood base excess and bicarbonate content, may be responsible for the improved feed intake.

Acid-Base Equilibrium↗
PubMed1987

Absorptive-mediated endocytosis of cationized albumin and a beta-endorphin-cationized albumin chimeric peptide by isolated brain capillaries. Model system of blood-brain barrier transport.

Cationized albumin (pI greater than 8), unlike native albumin (pI approximately 4), enters cerebrospinal fluid (CSF) rapidly from blood. This suggests that a specific uptake mechanism for cationized albumin may exist at the brain capillary wall, i.e. the blood-brain barrier. Isolated bovine brain capillaries rapidly bound cationized [3H]albumin and approximately 70% of the bound radioactivity was resistant to mild acid wash, which is assumed to represent internalized peptide. Binding was saturable and a Scatchard plot gave a maximal binding capacity (Ro) = 5.5 +/- 0.7 micrograms/mgp (79 +/- 10 pmol/mgp), and a half-saturation constant (KD) = 55 +/- 8 micrograms/ml (0.8 +/- 0.1 microM). The binding of cationized [3H]albumin (pI = 8.5-9) was inhibited by protamine, protamine sulfate, and polylysine (molecular weight = 70,000) with a Ki of approximately 3 micrograms/ml for all three proteins. The use of cationized albumin in directed delivery of peptides through the blood-brain barrier was examined by coupling [3H]beta-endorphin to unlabeled cationized albumin (pI = 8.5-9) using the bifunctional reagent, N-succinimidyl 3-(2-pyridyldithio)proprionate. The [3H]beta-endorphin-cationized albumin chimeric peptide was rapidly bound and endocytosed by isolated bovine brain capillaries, and this was inhibited by unlabeled cationized albumin but not by unconjugated beta-endorphin or native bovine albumin. Cationized albumin provides a new tool for studying absorptive-mediated endocytosis at the brain capillary and may also provide a vehicle for directed drug delivery through the blood-brain barrier.

Animals↗
PubMed2003

A ring walk of methylene groups in toluene radical cations. An extension of the toluene-cycloheptatriene rearrangement of aromatic radical cations. Theory and experiment.

The minimum energy reaction pathway (MERP) of the toluene-cycloheptatriene radical cation rearrangement (TOL/CHT-rearrangement) has been calculated by the UHF and DFT model at the level UHF/6-311+G(3df,2p)//UHF/6-31G(d) and B3LYP/6-311+G(3df,2p)//B3LYp/6-31G(d), respectively, including the ring walk of the substituent by a 1,2-shift around the aromatic ring. This ring walk corresponds to interconversion of distonic ions and norcaradiene radical cations (the two intermediates of the TOL/CHT-rearrangement) by making and breaking of the external C-C bonds of the cyclopropane moiety of the intermediate norcaradiene structure. For toluene radical cation 1, UHF calculations adequately reproduce earlier results(4) and show, that the ring walk of the CH(3)-substituents requires slightly more energy than formation of the cycloheptatriene radical cation. By the DFT model, the distonic ion, which is formed initially by a 1,2-H shift from CH(3) to the benzene ring, is not stable but the transition state of an interconversion of norcaradiene radical cations along a ring walk of the CH(3) substituent. The activation energy for this ring walk exceeds that for formation of the cycloheptatriene radical cation by c. 30 kJ mol(-1). Thus, isomerization of 1 by a ring walk of the CH(3)-substituent competes with the TOL/CHT-rearrangement likely only for excited 1. The calculation was repeated for the MERPs of a TOL/CHT-rearrangement of para-xylene radical cation 5 and ethylbenzene radical cation 2, yielding basically the same results as for 1. According to the calculation, polar substituents alter significantly the relative energies of the competing routes of isomerization. For benzylcyanide 3 (X = CN), the activation energy for a ring walk of the NC-CH(2)-substituent is distinctly below that of a ring enlargement. For benzyl methyl ether 4 (X = OCH(3)), the distonic intermediate along the UHF-MERP is unusually stable. Further, the 7-methoxy-norcaradiene radical ion is unstable and corresponds to a transition state between isomeric distonic intermediates differing by a 1,2-shift of the side chain. In contrast, the 7-methoxy-norcaradiene radical ion is the only intermediate of the DFT-MERP, and the distonic ion is the transition state for a 1,2-shift of the cyclopropane ring. A ring walk of the CH(3)OCH(2)-substituent is much more favorable than formation of a 7-methoxy-cycloheptatriene radical cation in both MERPs. The findings of the theoretical calculation are substantiated by the mass spectrometric fragmentations of meta- and para-methoxymethylated 1-phenylethanols 8 and 9 and of para-methoxymethyl substituted benzyl ethyl ether 10 and benzyl n-propyl ether 11. Important fragmentation routes of metastable molecular ions of these compounds correspond to elimination of alcohols. Use of deuterated derivatives shows that the elimination occurs by a "false" ortho-effect which requires migration of a ROCH(2)-substituent around the benzene ring. Results of particular interest are obtained for the asymmetric bis-ethers 10 and 11. Here, the MIKE spectra of the molecular ions of deuterated analogs reveal a selective ring walk of the C(2)H(5)OCH(2)- and n-C(3)H(7)OCH(2)-side chain, respectively.

Journal Article↗
PubMed1999

An energy-barrier model for the permeation of monovalent and divalent cations through the maxi cation channel in the plasma membrane of rye roots.

The depolarization-activated, high-conductance "maxi" cation channel in the plasma membrane of rye (Secale cereale L.) roots is permeable to a wide variety of monovalent and divalent cations. The permeation of K+, Na+, Ca2+ and Ba2+ through the pore could be simulated using a model composed of three energy barriers and two ion binding sites (a 3B2S model), which assumed single-file permeation and the possibility of double cation occupancy. The model had an asymmetrical free energy profile. Differences in permeation between cations were attributed primarily to differences in their free energy profiles in the regions of the pore adjacent to the extracellular solution. In particular, the height of the central free energy peak differed between cations, and cations differed in their affinities for ion binding sites. Significant ion repulsion occurred within the pore, and the mouths of the pore had considerable surface charge. The model adequately described the diverse current vs. voltage (I/V) relationships obtained over a wide variety of experimental conditions. It described the phenomena of non-Michaelian unitary conductance vs. activity relationships for K+, Na+ and Ca2+, differences in selectivity sequences obtained from measurements of conductance and permeability ratios, changes in relative cation permeabilities with solution composition, and the complex effects of Ba2+ and Ca2+ on K+ currents through the channel. The model enabled the prediction of unitary currents and ion fluxes through the maxi cation channel under physiological conditions. It could be used, in combination with data on the kinetics of the channel, as input to electrocoupling models allowing the relationships between membrane voltage, Ca2+ influx and Ca2+ signaling to be studied theoretically.

Barium↗
PubMed1983

Adsorption of reovirus to clay minerals: effects of cation-exchange capacity, cation saturation, and surface area.

The adsorption of reovirus to clay minerals has been reported by several investigators, but the mechanisms defining this association have been studied only minimally. The purpose of this investigation was to elucidate the mechanisms involved with this interaction. More reovirus type 3 was adsorbed, in both distilled and synthetic estuarine water, by low concentrations of montmorillonite than by comparable concentrations of kaolinite containing a mixed complement of cations on the exchange complex. Adsorption to the clays was essentially immediate and was correlated with the cation-exchange capacity of the clays, indicating that adsorption was primarily to negatively charged sites on the clays. Adsorption was greater with low concentrations of clays in estuarine water than in distilled water, as the higher ionic strength of the estuarine water reduced the electrokinetic potential of both clay and virus particles. The addition of cations (as chloride salts) to distilled water enhanced adsorption, with divalent cations being more effective than monovalent cations and 10(-2) M resulting in more adsorption than 10(-3) M. Potassium ions suppressed reovirus adsorption to montmorillonite, probably by collapsing the clay lattices and preventing the expression of the interlayer-derived cation-exchange capacity. More virus was adsorbed by montmorillonite made homoionic to various mono-, di-, and trivalent cations (except by montmorillonite homoionic to potassium) than by comparable concentrations of kaolinite homoionic to the same cations. The sequence of the amount of adsorption to homoionic montmorillonite was Al greater than Ca greater than Mg greater than Na greater than K; the sequence of adsorption to kaolinite was Na greater than Al greater than Ca greater than Mg greater than K. The constant partition-type adsorption isotherms obtained when the clay concentration was maintained constant and the virus concentration was varied indicated that a fixed proportion of the added virus population was adsorbed, regardless of the concentration of infectious particles. A heterogeneity within the reovirus population was indicated.

Adsorption↗
PubMed1999

Simultaneous determination of anions and cations by ion-exclusion chromatography-cation-exchange chromatography with tartaric acid/18-crown-6 as eluent.

Ion-exclusion chromatography-cation-exchange chromatography was developed for the simultaneous separation of common inorganic anions and cations (Cl-, NO3- and SO4(2-); Na+, NH4+, K+, Mg2+ and Ca2+) on a weakly acidic cation-exchange column by elution with weak acid. Generally, the resolution among these monovalent cations was only moderate, thereby hindering the determination of these analytes in natural-water samples. Therefore, 18-crown-6 was added to the eluent to improve the resolution. A good separation of these anions and cations on a weakly acidic cation-exchange column was achieved in 30 min by elution with 5 mM tartaric acid/6 mM 18-crown-6/methanol-water (7.5:92.5). The ion-exclusion chromatography-cation-exchange chromatography method developed here was successfully applied to the separation of major anions and cations in an environmental water sample.

Anions↗
PubMed2006

Isomerization and fragmentation reactions of gaseous dimethyl phenylarsane radical cations and methyl phenylarsenium cations. A study by tandem mass spectrometry and density functional theory calculations.

The unimolecular reactions of the radical cation of dimethyl phenylarsane, C6H5As(CH3)2, 1*+ and of the methyl phenylarsenium cation, C6H5As+CH3, 2+, in the gas phase were investigated using deuterium labeling and methods of tandem mass spectrometry. Additionally, the rearrangement and fragmentation processes were analyzed by density functional theory (DFT) calculations at the level UBHLYP/6- 311+G(2d,p)//UBHLYP/5-31+G(d). The molecular ion 1*+ decomposes by loss of a .CH3 radical from the As atom without any rearrangement, in contrast to the behavior of the phenylarsane radical cation. In particular, no positional exchange of the H atoms of the CH3 group and at the phenyl ring is observed. The results of DFT calculations show that a rearrangement of 1*+ by reductive elimination of As and shift of the CH3 group is indeed obstructed by a large activation barrier. The MIKE spectrum of 2+ shows that this arsenium cation fragments by losses of H2 and AsH. The fragmentation of the trideuteromethyl derivative 2-d3+ proves that all H atoms of the neutral fragments originate specifically from the methyl ligand. Identical fragmentation behavior is observed for metastable m-tolyl arsenium cation, m-CH3C6H4As+H, 2tol+. The loss of AsH generates ions C7H7+ which requires rearrangement in 2+ and bond formation between the phenyl and methyl ligands prior to fragmentation. The DFT calculations confirm that the precursor of this fragmentation is the benzyl methylarsenium cation 2bzl+, and that 2bzl+ is also the precursor ion fo the elimination of H2. The analysis of the pathways for rearrangements of 2+ to the key intermediate 2bzl+ by DFT calculations show that the preferred route corresponds to a 1,2-H shift of a H atom from the CH3 ligand to the As atom and a shift of the phenyl group in the reverse direction. The expected rearrangement by a reductive elimination of the As atom, which is observed for the phenylarsenium cation and for halogeno phenyl arsenium cations, requires much more activation enthalpy.

Arsenic↗
PubMed2000

Mechanism of electrogenic cation transport by the cloned organic cation transporter 2 from rat.

The organic cation transporter 2 (OCT2) is expressed in plasma membranes of kidney and brain. Its transport mechanism and substrates are debated. We studied substrate-induced changes of electrical current with the patch clamp technique after expression of rat OCT2 in oocytes. Activation of current, corresponding to efflux, was observed for small organic cations, e.g. choline. In contrast, the bigger cations quinine and tetrabutylammonium elicited no change in current. However, transport of choline could be inhibited by applying quinine or tetrabutylammonium to the cytoplasmic side. Inhibition of organic cation efflux by quinine was competitive with substrates. Quinine at the inside also inhibited substrate influx from the outside. Current-voltage analysis showed that both maximal turnover and apparent affinity to substrates are voltage-dependent. Substrate-induced currents with organic cations on both membrane sides reversed as predicted from the Nernst potential. Our results clearly identify the electrochemical potential as driving force for transport at neutral pH and exclude an electroneutral H(+)/organic cation(+) exchange. We suggest the existence of an electroneutral organic cation(+) exchange and propose a model for a carrier-type transport mechanism.

Animals↗
PubMed2002

Basic concepts of "cation pool" and "cation flow" methods and their applications in conventional and combinatorial organic synthesis.

Carbocations have been generally considered to be relatively unstable and transient species. But the "cation pool" method enables the easy accumulation of carbocations in conventional reaction media such as dichloromethane. In the "cation pool" method, carbocations are generated by low-temperature electrochemical oxidation and accumulated in a solution. In the next step, the carbocations thus produced are allowed to react with various nucleophiles. Combinatorial parallel synthesis based upon the "cation pool" method has also been developed. The applicability of the "cation pool" method depends upon the stability of the cation that is accumulated. This problem can be overcome by the "cation flow" method. In the "cation flow" method, carbocations are generated in a microflow electrochemical system. Short residence times and efficient temperature control of the microflow system are advantageous. Combinatorial sequential synthesis has been achieved based on the "cation flow" method.

Journal Article↗
PubMedDate not supplied

Transport of small organic cations in the rat liver. The role of the organic cation transporter OCT1.

The kidneys and the liver are the principal organs for the inactivation of circulating organic cations. Recently, an organic cation transporter (OCT1) has been cloned from rat kidney. In order to answer the question whether OCT1 is involved also in hepatic uptake of organic cations, the pharmacological characteristics of organic cation transport in hepatocytes were compared to the characteristics of transiently expressed OCT1. Primary cultures of rat hepatocytes avidly accumulated the small organic cation 3H-1-methyl-4-phenylpyridinium (3H-MPP+). At equilibrium, the hepatocytes accumulated 3H-MPP+ 56-fold. Initial rates of specific 3H-MPP+ transport in hepatocytes were saturable. The half-saturating concentration was 13 mumol/l. 3H-MPP+ transport was sensitive to quinine (Ki = 0.79 mumol/l) and cyanine863 (Ki = 0.097 mumol/l). Quinine and cyanine863 are known inhibitors of type I hepatic transport of cationic drugs and of renal excretion of organic cations, respectively. To compare the functional characteristics of 3H-MPP+ transport in hepatocytes with those of OCT1, OCT1 has been heterologously expressed and characterized in a mammalian cell line (293 cells). Initial rates of 3H-MPP+ transport were saturable, the Km being 13 mumol/l. The rank order of inhibitory potencies of various inhibitors was almost identical in hepatocytes and 293 cells transiently transfected with OCT1. There was a positive correlation between the Ki's for the inhibition of 3H-MPP+ transport in isolated hepatocytes and transfected 293 cells (r = 0.85; P < 0.01; n = 8). The results indicate that OCT1 is functionally expressed not only in the kidney but also in hepatocytes where it is responsible for the transport of small organic cations which, in the past, have been classified as type I substrates.

Animals↗
PubMed1985

Modulation of locomotor activity of polymorphonuclear cells by cationic substances and cationic lysosomal fractions from human neutrophils.

Seven cationic substances--human and egg-white lysozyme, RNase, protamine, histone, poly-L-lysine and poly-L-arginine; five cationic lysosomal fractions from human polymorphonuclears (PMNs); RNA; poly-L-glutamic acid; DNA; heparin; endotoxin; mastocytotropic agent compound 48/80; and cytochalasin B were tested for the influence on chemotaxis and random migration of human PMNs using under-agarose migration and Boyden chambers with two filters and [51Cr]PMNs. The above substances were either preincubated with PMNs, added to chemoattractants, or used instead of chemoattractants. In under-agarose migration method chemotaxis was inhibited by 11-35% when egg-white lysozyme, protamine, heparin, endotoxin, or compound 48/80 was added to the cells. High concentration of cytochalasin B inhibited chemotaxis by 73%. Cationic fractions I and V and low concentration of cytochalasin B enhanced chemotaxis by 11%, 41%, and 30%, respectively. When human and egg-white lysozyme, DNA, or cytochalasin B was added to the chemoattractants, motility of PMNs was inhibited. Cationic fractions II and V from human PMNs, when used as chemoattractants, enhanced cellular motility by 143-167%. Random migration was enhanced by heparin and inhibited by cytochalasin B and by cationic fractions from human PMNs. These findings suggest that various cationic and anionic substances and cationic fractions from human PMNs have heterogeneous influence on random migration and chemotactic activity of human PMN. Analysis relating chemotaxis to phagocytosis and to intracellular bactericidal activity (ICBA) has shown several patterns. Protamine, poly-L-lysine, poly-L-arginine, and agent compound 40/80 all inhibit chemotaxis and enhance phagocytosis and ICBA; cationic fractions II and V enhanced all three functions, whereas cytochalasin B suppressed phagocytosis and ICBA and had concentration-dependent modulatory influence on chemotaxis. It implies diverse mechanisms of action and possible impact on inflammatory reactions.

Chemotaxis↗