Polish journal of pharmacology最新文献

{"title":"Effects of enoxaparin on histomorphometric parameters of bones in rats.","authors":"Joanna Folwarczna,&nbsp;Waldemar Janiec,&nbsp;Marta Gawor,&nbsp;Maria Pytlik,&nbsp;Ilona Kaczmarczyk-Sedlak,&nbsp;Barbara Nowińska","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Enoxaparin sodium is a low-molecular-weight heparin. It is not clear whether the risk of development of osteoporosis after administration of low-molecular-weight heparins is lower than after administration of standard heparin. The aim of the present study was to investigate the effects of enoxaparin on histomorphometric parameters of bones in female Wistar rats (13-15 weeks old at the beginning of the experiment). Enoxaparin was administered at doses of 1000 anti-Xa IU/kg sc daily or 2000 anti-Xa IU/kg sc daily for 4 weeks. Bone mass, mineral and calcium content (in the tibia, femur and L-4 vertebra), length and diameter in the tibia and femur, and histomorphometric parameters of the tibia (periosteal and endosteal transverse growth, width of periosteal and endosteal osteoid, area of the transverse cross-section of the cortical bone in the diaphysis and area of the transverse cross-section of the marrow cavity) and the femur (width of epiphyseal and metaphyseal trabeculae, width of epiphyseal cartilage) were examined. Enoxaparin, administered at doses of 1000 anti-Xa IU/kg sc daily or 2000 anti-Xa IU/kg sc daily for 28 days, induced osteopenic changes in the rat skeletal system. The changes observed in bone histomorphometric parameters indicate that enoxaparin caused the inhibition of bone formation and intensification of bone resorption.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 4","pages":"451-7"},"PeriodicalIF":0.0,"publicationDate":"2004-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24792475","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}

{"title":"Calcium channel antagonists attenuate cross-sensitization to the locomotor effects of nicotine and ethanol in mice.","authors":"Grazyna Biała,&nbsp;Barbara Weglińska","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The present study was focused on evaluation of locomotor cross-sensitization between nicotine and ethanol in mice. First, we demonstrated that, after 5 daily injections, nicotine (0.5 mg/kg, ip) produced sensitization to its own locomotor stimulant effect. Moreover, nicotine-experienced mice manifested an enhanced response to ethanol challenge (2 g/kg, ip) indicating the development of cross-sensitization between nicotine and ethanol in mice. Additionally, the L-type voltage-dependent calcium channel antagonists: verapamil and diltiazem, but not nimodipine, at the dose of 20 mg/kg, injected before the ethanol challenge, blocked the expression of this cross-sensitization. These findings support the hypothesis that similar neural calcium-dependent mechanisms are involved in the sensitization to locomotor stimulant effects of nicotine and ethanol and point to certain differences in acute behavioral effects of various classes of calcium channel inhibitors.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 4","pages":"391-7"},"PeriodicalIF":0.0,"publicationDate":"2004-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24792581","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}

{"title":"Pertussis toxin-sensitive G protein modulates the ability of histamine to stimulate cAMP production in the chick pineal gland.","authors":"Jolanta B Zawilska,&nbsp;Jolanta Rosiak,&nbsp;Jerzy Z Nowak","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Histamine (HA) is a potent stimulator of cAMP synthesis in various structures of chick brain, including the pineal gland. The action of HA is mediated by specific, membrane bound H(2)-like receptors, whose pharmacological profile is different from that described for H(2) receptors in mammalian tissues. In this work, we analyzed the effects of cholera toxin (CTX) and pertussis toxin (PTX), well-known modulators of G(s) and G(i)/G(o) protein, respectively, on the stimulatory action of HA on cAMP synthesis in the chick pineal gland organ cultures. HA and its two biologically active methylated derivatives, 2-methylHA and 4-methylHA, markedly increased cAMP content in the chick pineal glands. Pretreatment of the chick pineal glands with CTX potently stimulated basal cAMP production. In CTX-pretreated glands, elevations of cAMP synthesis evoked by HA, 2-methylHA and 4-methylHA were additive to those produced by CTX, which is an observation suggesting that H(2)-like HA receptors in the chicken pineal gland are not coupled to G(s) proteins. Pretreatment of the chick pineal glands with PTX significantly enhanced the stimulatory effect of HA and, to a greater extent, 2-methylHA on cAMP production. The enhancing action of PTX on the HA-evoked cAMP formation was not modified by mepyramine, a selective H(1)-type HA receptor antagonist. It is suggested that in the chick pineal gland, a population of HA receptors is coupled to G(i) (or G(o)) protein. Stimulation of these receptors would tonically suppress the activity of the cAMP generating system functionally linked to H(2)-like HA receptors.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 4","pages":"407-13"},"PeriodicalIF":0.0,"publicationDate":"2004-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24792582","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}

{"title":"Cytotoxic and proapoptotic effects of new Pd(II) and Pt(II)-complexes with 3-ethanimidoyl-2-methoxy-2H-1,2-benzoxaphosphinin-4-ol-2-oxide.","authors":"Elzbieta Budzisz,&nbsp;Urszula Krajewska,&nbsp;Marek Rózalski","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The new palladium (II) and platinum (II) complexes 2 and 3 with 3-ethanimidoyl-2-methoxy-2H-1,2-benzoxaphospinin-4-ol-2-oxide 1 were synthesized and their physicochemical and pharmacological properties were determined. The cytotoxic effects of these complexes were examined on the two human leukemia cell lines, HL-60 and NALM-6. Pd-complex 2 and Pt-complex 3 exerted significant cytotoxic activity. The effects exhibited by these two complexes were comparable to those reported for cis-platin and carboplatin. On the other hand, ligand 1 was not cytotoxic. As determined by caspase-3 activity assay, compounds 2 and 3 differed slightly in their mode of induction of the programmed cell death.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 4","pages":"473-8"},"PeriodicalIF":0.0,"publicationDate":"2004-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24793541","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}

{"title":"Effects of retinol on development of osteopenic changes induced by bilateral ovariectomy in rats.","authors":"Maria Pytlik,&nbsp;Urszula Cegieła,&nbsp;Joanna Folwarczna,&nbsp;Waldemar Janiec,&nbsp;Wojciech Pytlik","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Skeletal disorders occurring in experimental model of osteopenia caused by bilateral ovariectomy in rats are similar to those observed in postmenopausal women. Retinol is a commonly used vitamin, especially by elderly people. The role of retinol in bone remodeling is not well-established. The aim of the present study was to investigate the effect of retinol administered at doses of 700 IU/kg p.o. daily and 3500 IU/kg p.o. daily for 28 days on the development of osteopenia induced by bilateral ovariectomy in 3-month-old Wistar rats. The experiments were carried out on 4 groups of animals: I (C)--sham-operated control rats, II (OVX)--ovariectomized control rats, III (OVX + R700)--OVX rats treated with retinol (700 IU/kg p.o. daily), IV (OVX + R3500)--OVX rats treated with retinol (3500 IU/kg p.o. daily). Body mass gain, bone mass, mineral and calcium content in the tibia, femur and L-4 vertebra, histomorphometric parameters of the right tibia (width of osteoid, periosteal and endosteal transverse growth, the area of the transverse cross section of the bone marrow and cortical bone) and the right femur (width of epiphyseal and metaphyseal trabeculae, width of epiphyseal cartilage), and mechanical properties of the femur were investigated. Bilateral ovariectomy induced osteopenic skeletal changes in mature female rats. Retinol at doses of 700 IU/kg p.o. daily and 3500 IU/kg p.o. daily decreased bone mass (statistically significantly after treatment with 3500 IU/kg p.o. daily). Retinol at both doses caused statistically significant increases in the width of periosteal osteoid, and, at a dose of 3500 IU/kg p.o. daily, of endosteal osteoid. The increase in the width of osteoid may be the effect of disorder of its mineralization, as the decreases in bone mineral and calcium content were also noted. In mechanical tests of the femur, dose-dependent decreases in the ultimate load, the breaking load and the deformation caused by the applied load were observed after administration of retinol (in comparison with the OVX control rats). Concluding, retinol (especially administered at the dose of 3500 IU/kg daily) intensified the changes in the osseous system caused by estrogen deficiency in rats.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 3","pages":"345-52"},"PeriodicalIF":0.0,"publicationDate":"2004-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24582440","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}

{"title":"Inhibition of DNA topoisomerase I and II, and growth inhibition of MDA-MB-231 human breast cancer cells by bis-benzimidazole derivatives with alkylating moiety.","authors":"Krzysztof Bielawski,&nbsp;Sławomir Wołczyński,&nbsp;Anna Bielawska","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The purpose of the present study was to identify the cellular processes and targets affected by treatment with bis-benzimidazole derivatives with chloroalkyl and bromoalkyl moieties (1-4) in the estrogen receptor-negative MDA-MB-231 human breast cancer cells. Treatment of the cells revealed that these compounds inhibited DNA synthesis and irreversibly inhibited the proliferative activity of the cells. All drugs 1-4 inhibited relaxation of pBR 322 DNA induced by both topoisomerases, although topoisomerase I was 2- to 9-fold more sensitive than topoisomerase II. This suggests that DNA-binding may be implicated in the cytotoxicity of bis-benzimidazole derivatives with alkylating moiety, possibly by inhibiting interactions between topoisomerases and their DNA targets.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 3","pages":"373-8"},"PeriodicalIF":0.0,"publicationDate":"2004-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24583721","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}

{"title":"Potential antipsychotic and extrapyramidal effects of (R,S)-3,4-dicarboxyphenylglycine [(R,S)-3,4-DCPG], a mixed AMPA antagonist/mGluR8 agonist.","authors":"Krystyna Ossowska,&nbsp;Małgorzata Pietraszek,&nbsp;Jadwiga Wardas,&nbsp;Stanisław Wolfarth","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>An involvement of glutamatergic transmission in schizophrenia has been postulated for several years. According to that view, hypofunction of NMDA receptors and a compensatory increase in glutamate release which overstimulates non-NMDA receptors contributes to psychotic symptoms. Therefore, potential antipsychotic drugs are searched for among compounds which block AMPA receptors and inhibit glutamate release. (R,S)-3,4-dicarboxyphenylglycine [(R,S)-3,4-DCPG] is a mixed antagonist of AMPA receptors and agonist of an autoreceptor, i.e. metabotropic glutamate receptor 8. The aim of the study was to look for putative antipsychotic properties of (R,S)-3,4-DCPG in the model of locomotor stimulation induced by amphetamine or phencyclidine in mice. Moreover, a risk of extrapyramidal side-effects induced by this compound was examined, as capability to induce catalepsy in the bar test and to increase the proenkephalin mRNA expression, measured autoradiographically in striatal slices by in situ hybridization. (R,S)-3,4-DCPG (80 mg/kg i.p.) decreased the amphetamine (2.5 mg/kg s.c.)-but not phencyclidine (3 mg/kg s.c.)-induced hyperactivity. That dose of (R,S)-3,4-DCPG did not decrease the spontaneous locomotor activity of mice. However, a dose of 100 mg/kg ip of that compound evoked catalepsy and enhanced the catalepsy and striatal proenkephalin mRNA expression induced by haloperidol (1-2 mg/kg i.p.). The study seems to suggest that (R,S)-3,4-DCPG may possess antipsychotic properties at doses close to those evoking extrapyramidal side-effects which speaks for its rather typical than atypical neuroleptic profile.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 3","pages":"295-304"},"PeriodicalIF":0.0,"publicationDate":"2004-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24582434","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}

{"title":"Effect of etoposide on the processes of osseous tissue remodeling in rats.","authors":"Urszula Cegieła,&nbsp;Joanna Folwarczna,&nbsp;Maria Pytlik,&nbsp;Waldemar Janiec","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In the course of tumor metastases into bones, the process of resorption is intensified both as a result of direct influence of tumor cells on normal bone cells, and as a result of bone cell stimulation by cytokines and growth factors, which leads to pathological remodeling of osseous tissue and, in majority of cases, to the development of systemic hypercalcemia. Clinical observations and in vitro research show that also cytostatic drugs may disturb remodeling of bone tissue and cause osteopenia, mostly as a result of their direct effect on osteoblasts. The aim of this study was to investigate in vivo the effect of etoposide on the processes of bone tissue remodeling in rats by assessing macrometric and histomorphometric parameters, as well as mechanical properties of the femur. The tests were carried out on male Wistar rats of initial body mass between 280-310 g, which were divided into three groups (n = 8): I--control group of rats, which were given 0.9% NaCl solution every 7 days (C group), II--rats which were administered etoposide at the dose of 25 mg/kg p.o. every 7 days (E-25 group), III--rats which were given etoposide at one dose of 50 mg/kg i.v. (E-50 group). The experiment lasted 4 weeks. At the end of the experiment, the animals were killed by spinal cord displacement and the following values were determined: the mass, mineral and calcium content in the tested bones, length and diameter of long bones, transverse cross-section surface of tibial cortical bone and marrow cavity, transverse growth of the tibia and width of periosteal and endosteal osteoid in the tibia, as well as the width of osseous trabeculae, the width of epiphysial cartilage and mechanical properties of the femur. The tests showed that etoposide administered every 7 days at the dose of 25 mg/kg p.o. or at one dose of 50 mg/kg i.v. over the period of 28 days, disturbed osseous tissue remodeling processes in rats as a result of impeding the process of bone formation, which led to the impairment of the process of mineralization, weakening mechanical endurance of the femur, and to the development of osteopenia.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 3","pages":"327-36"},"PeriodicalIF":0.0,"publicationDate":"2004-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24582438","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}

{"title":"Preliminary phenotypic characterization of the Warsaw High Preferring (WHP) and Warsaw Low Preferring (WLP) lines of rats selectively bred for high and low ethanol consumption.","authors":"Wanda Dyr,&nbsp;Wojciech Kostowski","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The Warsaw High Preferring (WHP) and Warsaw Low Preferring (WLP) lines were bred from Wistar foundation stock to obtain lines of rats that differ in their preference for ethanol (EtOH) solutions. The WHP line has met major criteria for an animal model of alcoholism. The WHP rats voluntarily drink excessive amounts of alcohol while the WLP rats consume negligible amounts of alcohol. These patterns of EtOH consumption are stable in time and independent of the manner of access to EtOH solutions. Notably, when exposed to the increasing EtOH concentrations both WHP and unselected Wistar rats gradually increased total EtOH intake. In contrast, WLP rats when exposed to the increasing concentrations of EtOH consumed almost negligible amounts of EtOH. Furthermore, the WHP rats show an increased responsiveness to the stimulatory effects of low dose of EtOH.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 3","pages":"359-65"},"PeriodicalIF":0.0,"publicationDate":"2004-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24583717","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}

{"title":"3Alpha,7alpha-dihydroxy-12-oxo-5beta-cholanate as blood-brain barrier permeator.","authors":"Momir Mikov,&nbsp;Slavko Kevresan,&nbsp;Ksenija Kuhajda,&nbsp;Vida Jakovljević,&nbsp;Velibor Vasović","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The aim of the study was to test the efficacy of 3alpha,7alpha-dihydroxy-12-oxo-5beta-cholanate as a blood-brain barrier (BBB) permeator by examining its effect on quinine uptake into the central nervous system in rats, analgesic action of morphine, and on the sleeping time induced by pentobarbital. The obtained results indicate that sodium 3alpha,7alpha-dihydroxy-12-oxo-5beta-cholanate can be considered as modifier of BBB permeability, as it exhibited a promoting effect in all three tests. In the test of quinine uptake, methyl ester of 3alpha,7alpha-dihydroxy-12-oxo-5beta-cholanoic acid (included in the study for comparison) did not show a promoting effect, which can suggest its specific action.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 3","pages":"367-71"},"PeriodicalIF":0.0,"publicationDate":"2004-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24583719","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}