Journal of pharmacobio-dynamics最新文献_第3页

Hypocholesterolemic effect of ursodeoxycholylcysteic acid in hamsters fed a high cholesterol diet. 熊脱氧胆酰半胱氨酸对高胆固醇饮食仓鼠的降胆固醇作用。

Journal of pharmacobio-dynamics Pub Date : 1992-10-01 DOI: 10.1248/bpb1978.15.573

H Shimizu, M Yoshii, A Seki, M Une, T Hoshita

引用次数: 3

Clastogenicity of aporphine alkaloids in vitro. 阿啡类生物碱的体外致裂性。

Journal of pharmacobio-dynamics Pub Date : 1992-09-01 DOI: 10.1248/bpb1978.15.501

S Tadaki, T Nozaka, S Yamada, M Ishino, I Morimoto, A Tanaka, J Kunitomo

引用次数: 13

Mechanisms of intestinal absorption of the antibiotic, fosfomycin, in brush-border membrane vesicles in rabbits and humans. 抗生素磷霉素在兔和人的刷边膜囊中的肠道吸收机制。

Journal of pharmacobio-dynamics Pub Date : 1992-09-01 DOI: 10.1248/bpb1978.15.481

T Ishizawa, S Sadahiro, K Hosoi, I Tamai, T Terasaki, A Tsuji

{"title":"Mechanisms of intestinal absorption of the antibiotic, fosfomycin, in brush-border membrane vesicles in rabbits and humans.","authors":"T Ishizawa, S Sadahiro, K Hosoi, I Tamai, T Terasaki, A Tsuji","doi":"10.1248/bpb1978.15.481","DOIUrl":"https://doi.org/10.1248/bpb1978.15.481","url":null,"abstract":"In order to clarify the mechanism of intestinal absorption of an antibiotic, fosfomycin (FOM), the uptakes of FOM by rabbit and human small intestinal brush-border membrane vesicles (BBMV) were studied. The initial uptake of FOM by BBMV at 15 s was saturable at a higher concentration of FOM. The kinetic parameters at 37 degrees C of the saturable uptake expressed by the Michaelis-Menten equation were Kt = 5.17 mM and Jmax = 3.88 nmol/15 s/mg protein for rabbits, and Kt = 4.03 mM and Jmax = 1.90 nmol/15 s/mg protein for humans. The most efficient uptake was observed in the presence of both inward-directed Na(+)- and H(+)-gradients in both mammals. The uptake of FOM was inhibited by inorganic phosphate, FOM glycol which is a degradation product of FOM in the gastric juice and specific inhibitors of phosphate transport such as arsenate and phosphonoacetic acid. These findings confirmed that FOM absorption from rabbit and human small intestines is associated with the phosphate transport system. These transport phenomena of FOM are in close agreement with those obtained previously in rat BBMV studies. Judging from the results obtained for three mammalian species, rat, rabbit and human, it was concluded that carrier-mediated transport via the phosphate transport system is a very important pathway of intestinal absorption of FOM.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":"15 9","pages":"481-9"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.481","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12461412","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 31

Electrical stimulation-evoked release of endogenous taurine from slices of the hippocampus, cerebral cortex and cerebellum of the rat. 电刺激诱发大鼠海马、大脑皮层和小脑切片内源性牛磺酸的释放。

Journal of pharmacobio-dynamics Pub Date : 1992-09-01 DOI: 10.1248/bpb1978.15.519

T Kubo, A Takano, N Tokushige, N Miyata, M Sato, S Hatakeyama

引用次数: 10

Cyclic AMP mimics IL-1 action in augmenting the differentiation of a mouse myeloid leukemic cell line (M1). 环状AMP模拟IL-1的作用，增强小鼠髓性白血病细胞系(M1)的分化。

Journal of pharmacobio-dynamics Pub Date : 1992-09-01 DOI: 10.1248/bpb1978.15.491

K Onozaki, K Kato, S Inui, Y Takuwa, Y Akiyama

{"title":"Cyclic AMP mimics IL-1 action in augmenting the differentiation of a mouse myeloid leukemic cell line (M1).","authors":"K Onozaki, K Kato, S Inui, Y Takuwa, Y Akiyama","doi":"10.1248/bpb1978.15.491","DOIUrl":"https://doi.org/10.1248/bpb1978.15.491","url":null,"abstract":"We have shown previously that recombinant human interleukin 1(IL-1) and interleukin 6 (IL-6) inhibited the proliferation of a mouse myeloid leukemic cell line (M1), and that IL-6 induced differentiation of the cells into macrophage-like cells and that IL-1 augmented this differentiation. Using this model we investigated the action mechanisms of IL-1 and IL-6. IL-6, but not IL-1, stimulated prostaglandin E2 (PGE2) production. The differentiative effect of IL-6 however, was not suppressed by indomethacin, although PGE2 induction by IL-6 was completely inhibited. Exogenously added PGE2 neither augmented the differentiative effect of IL-6 nor induced differentiation in combination with IL-1. Therefore, stimulation of PGE2 production did not appear to be essential for differentiative effects of these cytokines. Dibutyryl cAMP, 8-Br-cAMP and two adenylate cyclase-activating reagents, cholera toxin (CT) and forskolin (FK), all exhibited the similar augmenting effects as IL-1. These reagents augmented M1 cell differentiation by IL-6, and they did not induce differentiation in combination with IL-1. cAMP derivatives, CT, FK, IL-1 and IL-6 all inhibited the proliferation of M1 cells. CT and FK increased the intracellular cAMP levels. However, neither IL-1 nor IL-6 increased the cAMP levels. In contrast to the cAMP derivatives and reagents that activate adenylate cyclase activity, phorbol 12-myristate 13-acetate (PMA) and calcium ionophore neither induced nor augmented the differentiation in combination with either IL-1 or IL-6. Intracellular Ca2+ concentration was not altered by IL-1 or IL-6 suggesting that Ca2+/Calmodulin kinase and protein kinase C activation are not involved in this signal transduction pathway. Therefore, the present study suggests that IL-1 exhibits an effect similar to that of cAMP without affecting intracellular cAMP level.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":"15 9","pages":"491-500"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.491","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12510696","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3

Activation of hepatic microsomal glutathione S-transferase of rats by a glutathione depletor, diethylmaleate. 谷胱甘肽消耗物马来酸二乙酯对大鼠肝微粒体谷胱甘肽s转移酶的激活作用。

Journal of pharmacobio-dynamics Pub Date : 1992-09-01 DOI: 10.1248/bpb1978.15.473

Y Aniya, M Teruya

{"title":"Activation of hepatic microsomal glutathione S-transferase of rats by a glutathione depletor, diethylmaleate.","authors":"Y Aniya, M Teruya","doi":"10.1248/bpb1978.15.473","DOIUrl":"https://doi.org/10.1248/bpb1978.15.473","url":null,"abstract":"The effect of glutathione depletor diethylmaleate on rat hepatic glutathione S-transferase and glutathione peroxidase was studied in vivo and in vitro. When diethylmaleate (600 mg/kg) was given i.p. to rats, liver glutathione was depleted within 2 h and recovered to the control level 5 h after diethylmaleate treatment. Both glutathione S-transferase and peroxidase activities in microsomes, not in cytosol, were markedly increased during glutathione depletion and only glutathione S-transferase activity remained at high levels after recovery of the glutathione content. The increase in microsomal glutathione S-transferase and peroxidase activities with concomitant exhaustion of glutathione was also observed by perfusion of the isolated liver with diethylmaleate (10 mM). When liver microsomes were incubated with diethylmaleate in vitro at 37 degrees C, glutathione S-transferase, but not peroxidase, activity was increased; the increase was not reversed by dithiothreitol. These results indicate that diethylmaleate activates microsomal glutathione S-transferase by direct reaction to the enzyme during glutathione depletion and suggest that glutathione S-transferase activity and glutathione peroxidase activity in the microsomal enzyme may be differently regulated.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":"15 9","pages":"473-9"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.473","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12461410","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Increases in urinary enzyme excretion in rats depleted of glutathione inhibited by scavenger of oxygen free radicals. 氧自由基清除剂抑制谷胱甘肽耗竭大鼠尿酶排泄的增加。

Journal of pharmacobio-dynamics Pub Date : 1992-09-01 DOI: 10.1248/bpb1978.15.513

M Gemba, T Yamaguchi, K Kambara, A Suzuki, Y Kawai

{"title":"Increases in urinary enzyme excretion in rats depleted of glutathione inhibited by scavenger of oxygen free radicals.","authors":"M Gemba, T Yamaguchi, K Kambara, A Suzuki, Y Kawai","doi":"10.1248/bpb1978.15.513","DOIUrl":"https://doi.org/10.1248/bpb1978.15.513","url":null,"abstract":"Urinary excretion of enzymes by rats was assessed after glutathione (GSH) was depleted by treatment with a mixture of the GSH depletors D,L-buthionine-S,R-sulfoximine (BSO) and diethylmaleate (DEM). Renal GSH was low 2 h after treatment and later returned to the control level. The urinary excretion of gamma-glutamyltranspeptidase (gamma-GTP) and N-acetyl-beta-D-glucosaminidase (NAG) remained high for at least 3 d after the injection of BSO (100 mg/kg) and DEM (0.5 ml/kg), with no effect on the blood urea nitrogen level. N,N'-Dimethylthiourea (DMTU), a scavenger of oxygen free radicals, inhibited this increase in the urinary excretion of gamma-GTP. DMTU also inhibited the increase in cisplatin-induced NAG excretion caused by the GSH depletors. These results suggested that the urinary excretion of these enzymes is an index of renal tubular injury caused by short-term depletion of renal GSH, and that the generation of free radicals may be involved in renal tubular injury during GSH depletion or caused by cisplatin together with GSH depletors.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":"15 9","pages":"513-8"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.513","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12536601","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 8

Changes in the levels of rat interleukin 8/CINC and gelatinase in the exudate of carrageenin-induced inflammation in rats. 大鼠角叉菜胶诱导炎症渗出液中白细胞介素8/CINC和明胶酶水平的变化。

Journal of pharmacobio-dynamics Pub Date : 1992-09-01 DOI: 10.1248/bpb1978.15.461

H Nakagawa, A Ikesue, H Kato, H Debuchi, K Watanabe, S Tsurufuji, M Naganawa, M Mitamura

{"title":"Changes in the levels of rat interleukin 8/CINC and gelatinase in the exudate of carrageenin-induced inflammation in rats.","authors":"H Nakagawa, A Ikesue, H Kato, H Debuchi, K Watanabe, S Tsurufuji, M Naganawa, M Mitamura","doi":"10.1248/bpb1978.15.461","DOIUrl":"https://doi.org/10.1248/bpb1978.15.461","url":null,"abstract":"A sensitive enzyme-linked immunosorbent assay (ELISA) for rat interleukin 8/cytokine-induced neutrophil chemoattractant (CINC) has been established by using biotin-conjugated anti-CINC rabbit IgG. The biotin-streptavidin sandwich ELISA detected CINC at concentrations from 3 pg/ml up to 30 ng/ml. The concentration of CINC in the pouch fluid (exudate) of rat carrageenin-induced inflammation was measured by the ELISA. After a time lag of about 2 h, neutrophils steadily accumulated in the carrageenin/air-pouch until 8 h. Similarly, the CINC level of exudate increased after about a 2-h lag, and reached a maximum (134 ng/ml) at 8 h, and thereafter decreased to a negligible concentration at 24 h after carrageenin injection. In association with the rise in CINC level, the concentration of exudate 96-kDa gelatinase corresponding to neutrophil gelatinase/type IV collagenase increased with time. The results suggest that CINC contributes, at least in part, to the neutrophil migration into the inflammatory lesion of the carrageenin-induced inflammation in rats.","PeriodicalId":16743,"journal":{"name":"Journal of pharmacobio-dynamics","volume":"15 9","pages":"461-6"},"PeriodicalIF":0.0,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1248/bpb1978.15.461","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12510695","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 33

Overestimation of the lipoprotein fractional catabolic rate (FCR) measured in short duration experiments. 在短时间实验中测量的脂蛋白分数分解代谢率(FCR)的高估。

Journal of pharmacobio-dynamics Pub Date : 1992-09-01 DOI: 10.1248/bpb1978.15.541

G Champarnaud, K Ouguerram, T Magot, C Lutton

引用次数: 2

Enantioselective oral bioavailability of 0-isovaleryl propranolol as a potential prodrug of propranolol. 0-异戊酰普萘洛尔作为普萘洛尔潜在前药的口服生物利用度。

Journal of pharmacobio-dynamics Pub Date : 1992-09-01 DOI: 10.1248/bpb1978.15.535

M Shameem, T Imai, M Otagiri

引用次数: 0