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H Endou

Publications and source records attributed to H Endou.

At least 73 records · Page 4Linked to original sources

Recent advances in molecular mechanisms of nephrotoxicity.

Numerous drugs and endogenous compounds are efficiently excreted from the renal proximal tubule via two carrier-mediated pathways, that are organic anion and organic cation transport systems. Since most nephrotoxicants are taken up into renal target cells for further actions, these transport systems seem to be an early event for nephrotoxicity. Recent advances in nephrotoxicity are molecular cloning of several transporters related to important toxic compounds in the kidney. An organic cation transporter 1 (OCT1) was cloned in 1994. On the other hand, we recently isolated a complementary DNA that encodes an organic anion transporter 1 (OAT1) as an anion/dicarboxylate exchanger of the basolateral membrane of proximal tubule. Transepithelial secretion of organic anion consists of an influx of anionic substrates into the cell through the basolateral membrane and their efflux to the urine across the apical membrane. OAT1 displays a remarkably wide substrate specificity, including endogenous substrates, a variety of drugs with different structures and natural toxins. We further isolated homologs of OAT series such as liver-specific OAT2 and kidney-, liver- and brain-expressing OAT3. Because the amino acid sequence of OAT1 shows 38% identity to OCT1, a newly defined 'multispecific organic ion transporter superfamily' will provide potential tools to assess mechanisms of many nephrotoxicants including drugs and xenobiotics, and contribute also in understanding more precisely nephrotoxic mechanisms of chemicals.

Animals↗

Molecular cloning and characterization of high-affinity carnitine transporter from rat intestine.

Carnitine is an essential component for mitochondrial beta-oxidation of fatty acid. Using the degenerate primers designed for organic anion transporters and an organic cation transporter, we isolated a novel cDNA encoding a carnitine transporter (CT1) from rat intestine. CT1 encodes a 557-amino-acid protein with 12 putative membrane-spanning domains. When expressed in Xenopus oocytes, CT1 mediated a high-affinity transport of L-carnitine (Km = 25 microM). The replacement of extracellular sodium with Li reduced CT1-mediated L-carnitine uptake to 19.8%. CT1 did not transport typical substrates for either organic anion or organic cation transporters, such as p-aminohippurate and tetraethylammonium. Octanoylcarnitine, acetylcarnitine, and gamma-butyrobetaine showed potent inhibitory effects on CT1-mediated L-carnitine uptake; betaine and d-carnitine showed moderate inhibition. CT1 mRNA was strongly expressed in the testis, colon, kidney, and liver and weakly in the skeletal muscle, placenta, small intestine, and brain. No CT1 expression was detected in the heart, spleen, or lung. The present study provides the molecular basis of carnitine transport in the body.

Amino Acid Sequence↗

Expression cloning and characterization of a transporter for large neutral amino acids activated by the heavy chain of 4F2 antigen (CD98).

A cDNA was isolated from rat C6 glioma cells by expression cloning which encodes a novel Na+-independent neutral amino acid transporter designated LAT1. For functional expression in Xenopus oocytes, LAT1 required the heavy chain of 4F2 cell surface antigen (CD98), a type II membrane glycoprotein. When co-expressed with 4F2 heavy chain, LAT1 transported neutral amino acids with branched or aromatic side chains and did not accept basic amino acids or acidic amino acids. The transport via LAT1 was Na+-independent and sensitive to a system L-specific inhibitor 2-aminobicyclo-(2,2,1)-heptane-2-carboxylic acid. These functional properties correspond to those of the classically characterized amino acid transport system L, a major nutrient transporter. In in vitro translation, LAT1 was shown to be a nonglycosylated membrane protein consistent with the property of 4F2 light chain, suggesting LAT1 is at least one of the proteins formerly referred to as 4F2 light chain. LAT1 exhibits relatively low but significant amino acid sequence similarity to mammalian cationic amino acid transporters and amino acid permeases of bacteria and yeasts, indicating LAT1 is a new member of the APC superfamily. Because of highly regulated nature and high level of expression in tumor cell lines, LAT1 is thought to be up-regulated to support the high protein synthesis for cell growth and cell activation. The cloning of LAT1 is expected to facilitate the research on the protein-protein interaction in the transporter field and to provide a clue to the search for still unidentified transporters.

Amino Acid Sequence↗

Identification of multispecific organic anion transporter 2 expressed predominantly in the liver.

In the present study, we demonstrate that NLT (novel liver-specific transport protein) is a multispecific organic anion transporter of the liver. The amino acid sequence of NLT shows 42% identity to that of the renal multispecific organic anion transporter, OAT1. When expressed in Xenopus laevis oocytes, NLT mediated uptake of organic anions, such as salicylate, acetylsalicylate, PGE2, dicarboxylates and p-aminohippurate. [14C]Salicylate uptake via NLT was saturable (Km = 88.8 +/- 23.4 microM) and sodium-independent. Expression of the mRNA of NLT was detected in the liver and kidney (liver >> kidney). We propose that NLT be renamed OAT2.

Animals↗

Involvement of macromolecule synthesis, endonuclease activation and c-fos expression in cisplatin-induced apoptosis of mouse proximal tubule cells.

We have previously demonstrated that cisplatin-induced nephrotoxicity is associated with the induction of apoptosis using mouse renal cells derived from the terminal proximal tubule (S3) which is the major target site of cisplatin-induced injury. The purpose of this study was to elucidate the intracellular mechanisms leading to the cisplatin-induced apoptosis of S3 cells. Actinomycin D (an inhibitor of RNA synthesis), cycloheximide (an inhibitor of protein synthesis) and aurintricarboxylic acid (an endonuclease inhibitor) reduced the extent of DNA fragmentation, a biochemical parameter of apoptosis, in cisplatin-treated S3 cells. Furthermore, cisplatin-induced apoptosis of S3 cells was accompanied by an increase in the level of c-fos mRNA expression, which is inhibited by pretreatment of the cells with actinomycin D, but not with cycloheximide or aurintricarboxylic acid. In contrast, outer medullary collecting duct cells treated with cisplatin exhibited morphological changes characteristic of apoptosis and an increase in the level of c-fos mRNA expression, but no increase in the extent of DNA fragmentation. In conclusion, the synthesis of macromolecules such as RNA and protein, endonuclease activation and c-fos expression appear to be involved in the intracellular pathways leading to the induction of apoptosis in cisplatin-treated S3 cells. In addition, the response to cisplatin may be different in different cells.

Animals↗

Involvement of H2O2 production in cisplatin-induced nephrotoxicity.

The purpose of this study was to elucidate the involvement of H2O2 production in cisplatin-induced nephrotoxicity. The S3 cells were more sensitive than OMCT cells in cell viability and H2O2 production during cisplatin treatment. The cytotoxicity and H2O2 production induced by cisplatin were terminated by treatment with catalase. In conclusion, we emphasize the importance of the hydroxy radical in cisplatin nephrotoxicity.

Animals↗

Distinct interleukin-1beta-converting enzyme family proteases mediate cisplatin- and staurosporine-induced apoptosis of mouse proximal tubule cells.

Interleukin-1beta converting enzyme (ICE) family proteases (caspases) are known to be implicated as important effectors of apoptotic pathways. The purpose of this study was to elucidate the role of ICE family proteases in apoptosis of mouse cells derived from the terminal proximal tubule (S3) treated with cisplatin, an anti-tumor drug, or staurosporine, a protein kinase C inhibitor. For this purpose, we measured the activities of ICE family proteases and examined the effects of tetrapeptide and viral ICE family protease inhibitors on the activities of ICE family proteases in and the degree of apoptosis of S3 cells treated with cisplatin and staurosporine. RT-PCR analysis revealed that S3 cells as well as mouse kidney express mRNA for ICE and CPP32, an ICE family protease. Results of enzymatic analysis, determination the degree of DNA fragmentation and cytotoxicity test suggest that CPP32 mediates cisplatin-induced apoptosis of S3 cells, whereas ICE family proteases other than CPP32 mediate staurosporine-induced apoptosis of S3 cells. In conclusion, distinct ICE family proteases mediate apoptosis of mouse proximal tubule cells depending on the stimuli to which the cells are exposed.

Animals↗

Establishment of a mouse clonal early proximal tubule cell line and outer medullary collecting duct cells expressing P2 purinoceptors.

The purpose of this study was to establish tubule cells expressing P2 purinoceptors. Use of the polymerase chain reaction coupled with reverse transcription showed that mouse clonal early proximal tubule (S1) cell line (NF-5) and outer medullary collecting tubule (OMCT) cells expressed mRNA for P2X4, P2Y1 and P2Y2 purinoceptors. ATP and its analogues induced a dose-dependent increase in cytosolic free calcium concentration ([Ca2+]i) in both NF-5 and OMCT cells. ATP enhanced [3H]-thymidine uptake by both NF-5 and OMCT cells in a dose-dependent manner. In conclusion, NF-5 and OMCT cells can be used in the further analysis of the function and regulation of activity and expression of P2 purinoceptors in the renal tubule.

Adenosine Triphosphate↗

P2 purinoceptor localization along rat nephron and evidence suggesting existence of subtypes P2Y1 and P2Y2.

Effects of extracellular ATP on intracellular free calcium concentration([Ca2+]i) were examined in rat single nephron segments using the fura 2-AM. ATP (10 ¿M) induced a significant transient increase in [Ca2+]i in the glomerulus, the early proximal convoluted tubule (S1), the cortical collecting tubule (CCT), and the outer medullary collecting tubule (OMCT). The magnitude of the response was the greatest in the OMCT among four segments. ATP induced an increase in the [Ca2+]i in a dose-dependent manner in S1 and OMCT. In the OMCT, ATP caused a biphasic increase in [Ca2+]i consisting of an initial rapid rise and a sustained phase. Removal of calcium from the medium resulted in an attenuation of the sustained phase of [Ca2+]i and an approximately 30% reduction in the height of the initial [Ca2+]i peak in response to 10 ¿M ATP. Effects of ATP, its analogs, and its metabolites were tested in the S1 and OMCT. ATP, 2-methylthio-ATP (2-MeS-ATP), ADP, and UTP increased [Ca2+]i dose dependently. AMP and adenosine did not affect [Ca2+]i in the S1 and OMCT. The ATP- or 2-MeS-ATP-induced [Ca2+]i increase was inhibited by the pretreatment of the S1 and OMCT with suramin or reactive blue 2. Neomycin, a phospholipase C inhibitor, attenuated the ATP-induced [Ca2+]i increase. To investigate the hormonelike action of ATP in OMCT, a heterologous cross desensitization was performed. The pretreatment of OMCT with ATP inhibited increases in vasopressin-, ANG II-, endothelin-1-, or bradykinin-induced[Ca2+]i increase. These findings suggest that ATP might affect the above peptidyl agonist-activated calcium mobilizations.

Adenosine↗

Cloning, functional characterization, and localization of a rat renal Na+-dicarboxylate transporter.

We report here the isolation, functional characterization, tissue distribution, and membrane localization of rat renal Na+-dicarboxylate transporter (rNaDC-1). rNaDC-1 consists of 2,245 nucleotides, and the deduced amino acid sequence showed 73% and 75% identity to rabbit and human NaDC-1, respectively. When expressed in Xenopus laevis oocytes, rNaDC-1 mediated sodium-dependent uptake of di- and tricarboxylates. Substrates of rNaDC-1 evoked inward currents in oocytes expressed with rNaDC-1; succinate, alpha-ketoglutarate, and glutarate were relatively high-affinity substrates, and citrate was a low-affinity substrate of rNaDC-1. The coupling ratio of citrate to charge was determined to be 1:1 at pH 7.4; influx of one positive charge per citrate molecule suggests a symport of three Na+ with a divalent citrate. Expression of rNaDC-1 mRNA was detected in the kidney and the small and large intestines. Immunohistochemistry using polyclonal antibodies raised against the 14 amino acids at the COOH terminus of rNaDC-1 revealed that rNaDC-1 is localized exclusively in the luminal membrane of S2 and S3.

Amino Acid Sequence↗

Distributional patterns of phospholipase C isozymes in rat kidney.

As the first step to investigate the physiological function of phospholipase C (PLC), we determined the distribution patterns of PLC isozymes in normal rat kidneys using Western blotting analysis and immunohistochemistry. Western blotting analysis was performed in four regions (cortex, outer stripe and inner stripe of the outer medulla, and the inner medulla). PLC-beta1 and beta3 were detected in the inner stripe of the outer medulla and the inner medulla. PLC-gamma1 was distributed homogeneously along the corticomedullary axis. PLC-gamma2 was observed in the medulla and PLC-delta1 showed a gradual increase from the cortex to the inner medulla. In contrast, no PLC-beta4 was detected in all regions. On immunohistochemistry, the immunoreactivities to PLC antibodies were observed as follows: PLC-beta1, from the thick ascending limb (TAL) to the inner medullary collecting tubule (IMCT); PLC-beta3, in the glomerulus (Glm), the ascending thin limb (ATL) and the collecting tubule; PLC-beta4, Glm, the proximal convoluted tubule (PCT), ATL, the distal convoluted tubule, the connecting tubule, and the collecting tubules; PLC-gamma1, PCT, TAL and IMCT; PLC-delta1, homogeneously from PCT to IMCT. PLC-beta3 immunoreactivities were detected in the nuclei of the TAL, ATL, outer medullary collecting tubule (OMCT) and IMCT. PLC-beta4 and gamma2 were observed in Glm, MTAL, ATL, OMCT and IMCT. These results suggest the intrarenal site-specific existence of PLC isozymes that may regulate kidney functions through the PLC-mediated signal transductions.

Animals↗

[SMANCS/TAE for hepatocellular carcinoma: comparison with SMANCS/TAI].

To evaluate the effects of SMANCS/TAE for hepatocellular carcinoma, AFP reduction rates, tumor reduction rates of SMANCS/TAE were compared with those of SMANCS/TAI. SMANCS is a stylene-maleic acid neocarzinostatin. TAE means transcatheter arterial embolization with gelatin sponge after SMANCS infusion and TAI means transcatheter arterial infusion of only SMANCS-iodized oil suspension. For evaluation of the AFP reduction rate, 13 SMANCS/TAEs were compared with 32 SMANCS/TAIs. In these cases, pretreatment serum AFP levels were higher or equal to 100 ng/ ml. The average dose of SMANCS/TAE was 4.2 +/- 1.8 (S. D) mg and that of SMANCS/TAI was 3.9 +/- 1.8 (S. D) mg (N. S: t-test, p = 0.59). Student's t-test revealed that the AFP reduction rate of SMANCS/TAE was not significantly superior to that of SMANCS/TAI (p = 0.78), and both AFP reduction rate of SMANCS/TAE and SMANCS/ TAI were not correlated with the dose of SMANCS. Tumor reduction rates of 12 SMANCS/TAEs and 14 SMANCS/TAIs on CT examination were calculated. The average dose of SMANCS/TAE was 4.5 +/- 1.9 (S. D) mg and that of SMANCS/TAI was 3.8 +/- 2.1 (S. D) mg (N. S: t-test, p = 0.29). The average tumor reduction rate of SMANCS/TAE was 25.3 +/- 30.1 (S. D)% and of SMANCS/TAI was 13.8 +/- 29.1%. Student's t-test revealed the tumor reduction rate of SMANCS/TAE was not significantly larger than that of SMANCS/TAI (p = 0.33). AFP reduction rate and tumor reduction rate of SMANCS/TAE were not significantly different from those of SMANCS/TAI. Although the number of cases was not enough, these results suggest SMANCS/TAI should be applied for treatment of hepatocellular carcinoma rather than SMANCS/ TAE.

Adult↗

Tissue specific variants of glutamate transporter GLT-1.

cDNA cloning of glutamate transporter GLT-1 from mouse brain and liver has revealed that 5'-ends of the messages are different between brain and liver. In addition, one of the GLT-1 cDNAs isolated from liver has been found to possess a 3'-end different from those of the others. Reverse transcription polymerase chain reaction (RT-PCR) amplification using primers specific for altered 5'-ends has confirmed that brain and liver messages possess their own specific 5'-ends. Both of the two 3'-ends have been demonstrated by RT-PCR to be present not only in liver but also in brain, indicating both brain and liver GLT-1 possess two types of 3'-ends. Although functional properties are not changed by the alteration of N-termini and C-termini when expressed in Xenopus laevis oocytes, co-expression of two liver type GLT-1 with different C-termini (mGLT-1A and mGLT-1B) has been found to result in the increase in Vmax of transport without changing Km. These results suggest the tissue specific alternative splicing at 5'-ends of GLT-1 messages and the interesting association of spliced variants with different C-termini.

ATP-Binding Cassette Transporters↗

Expression cloning and characterization of a novel multispecific organic anion transporter.

Numerous drugs and endogenous compounds are efficiently excreted from the renal proximal tubule via carrier-mediated pathways. Transepithelial excretion of organic anions occurs via their accumulative transport from the blood into the proximal tubule cells across the basolateral membrane and subsequent secretion into the urine through the apical membrane. Here we report on the isolation of a novel complementary DNA from rat kidney that encodes a 551-amino acid residue protein (OAT1) with 12 putative membrane-spanning domains. When expressed in Xenopus laevis oocytes, OAT1 mediated sodium-independent para-aminohippurate (PAH) uptake (Km = 14.3 +/- 2.9 microM). The uptake rate of PAH was increased by the outwardly directed dicarboxylate gradient, consisting with the idea that OAT1 is an organic anion/dicarboxylate exchanger. OAT1 displayed remarkably wide substrate selectivity, covering endogenous substrates such as cyclic nucleotides, a prostaglandin and uric acid, and a variety of drugs with different structures (e.g. antibiotics, a nonsteroidal anti-inflammatory drug, diuretics, an antineoplastic drug, and a uricosuric drug). The Northern blot analysis and in situ hybridization revealed that OAT1 is exclusively expressed in the particular segment of the proximal tubule in the kidney. These data suggest that OAT1 is a multispecific organic anion transporter at the basolateral membrane of the proximal tubule. Isolation of OAT1 will facilitate elucidation of the molecular basis of drug kinetics and the development of new drugs lacking unwanted side effects.

Amino Acid Sequence↗

Intranephron distribution of cysteine S-conjugate beta-lyase activity and its implication for hexachloro-1,3-butadiene-induced nephrotoxicity in rats.

The intranephron distribution of two major cysteine S-conjugate beta-lyases was determined in order to clarify the role of these enzymes in promoting the nephrotoxicity associated with certain halogenated xenobiotics. Various nephron segments [i.e., glomerulus, early, middle, and terminal portions of the proximal tubule (S1, S2, and S3 respectively), the thick ascending limb, the distal tubule, and the collecting tubule] were isolated by microdissection from collagenase-treated rat kidneys. Each segment was dissected in Hanks' solution, solubilized with Triton X-100, and applied to a micropolyacrylamide gel constructed with a continuous gradient. The gels were subjected to electrophoresis and then incubated in the dark in a solution containing S-(1,2 dichlorovinyl)-L-cysteine (DCVC), a sodium alpha-keto-gamma-methiolbutyrate, phenazine methosulfate, and nitro-blue tetrazolium. The position of cysteine S-conjugate beta-lyase- and L-amino acid oxidase activities in the gels was revealed by the presence of blue formazen dye bands. The relative intensities of the bands were determined by optical scanning with a microdensitometer. Three bands were detected: band I (M(r) approximately 330,000) corresponds to a recently described high M(r) cysteine S-conjugate beta-lyase whereas band III (M(r) approximately 90,000) corresponds to a lower M(r) cysteine S-conjugate beta-lyase (identical to cytosolic glutamine transaminase K). Band II (M(r) approximately 240,000) corresponds to L-amino acid oxidase (a unique activity of the B isoform of rat kidney L-hydroxy acid oxidase). beta-lyase activity with DCVC as substrates was detected in the S1, S2, and S3 segments of the nephron but not in other regions of the kidney. The activity was in the order: S2 = S3 > S1. In another series of experiments, rats were killed 24 h after treatment with hexachloro- 1,3-butadiene (HCBD). In whole kidney homogenates the relative intensity of band III (per 22.2 micrograms tissue wet weight) after a 30 min incubation was induced significantly (by 50%), but the relative intensities of the other two bands were unchanged. On the other hand, in proximal tubules isolated from HCBD-treated rats the relative intensities (per 5 mm of nephron) of peak I of S2, peak II of S3, and peak III of S3 were significantly reduced by 28, 33, and 72%, respectively. These findings suggest that the low M(r) beta-lyase is induced by HCBD and that impaired cell function in the segments (especially S3) results in proteins leaking out of the target cells. To examine the relationship between the nephrotoxic effect of HCBD and cysteine S-conjugate beta-lyase activity, the intracellular ATP:protein ratio was quantitated in each nephron segment and in whole kidney homogenates. In HCBD-treated rats the ATP:protein ratio of the S1, S2, and S3 segments was unchanged, decreased by approximately 50%, and increased by approximately 30% respectively. In the kidney homogenates of HCBD-treated rats the ATP content was decreased by 32%. However, the loss of ATP was significantly less when the rats were pretreated with aminooxyacetate (a general inhibitor of pyridoxal 5'-phosphate-dependent enzymes, including beta-lyase) 1 h before HCBD administration. The results strongly suggest that HCBD is converted to toxic metabolites within the kidney and that this process leads to metabolic derangement and reduction of ATP in susceptible kidney cells.

Adenosine Triphosphate↗