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991.
Otagiri Masaki Yamamichi Ryuji Marayama Toru Imai Teruko Suenaga Ayaka Imamura Yorishige Kimachi Kazuhiko 《Pharmaceutical research》1989,6(2):156-159
The interactions of acidic and basic drugs with 1-acid glycoprotein (1-AGP) were investigated using circular dichroism (CD) measurements. Extrinsic Cotton effects were generated by the binding of drugs to 1-AGP. The CD data suggested the presence of a single binding site on the 1-AGP molecule. The induced ellipticities of the acidic drug–1-AGP system decreased with increasing pH, while the ellipticities for the basic drugs increased with pH. The ellipticities for all drugs were reduced by the addition of fatty acids. Furthermore, the induced ellipticities decreased in the presence of cesium chloride for basic drugs bound to 1-AGP. The extrinsic Cotton effects therefore appear to result from hydrophobic interaction with 1-AGP for the acidic drugs and from hydrophobic and electrostatic interactions for the basic drugs. 相似文献
992.
van Hoogdalem Ewoud J. Heijligers-Feijen Cornelia D. de Boer Albertus G. Verhoef J. Coos Breimer Douwe D. 《Pharmaceutical research》1989,6(1):91-95
The stability of the neuroleptic peptide des-enkephalin--endorphin (DEE; Org 5878) in the rectal lumen and the rectal bioavailability of DEE were investigated in conscious rats. Furthermore, the influence of peptidase inhibition, peptidase saturation, and absorption enhancement on DEE bio-availability were evaluated. Na2EDTA (0.25%, w/v) prolonged the degradation half-life of DEE in the ligated colon from 33 ± 7 to 93 ± 45 min. Without adjuvant, tritium-labeled DEE was absorbed from the rat rectum to a very low extent (0–4%). After administration of an excess of unlabeled DEE or with Na2EDTA, comparable results were obtained. The medium-chain glyceride preparation MGK markedly enhanced the rectal DEE bioavailability, up to 8–20%, which was further increased to 10–44% by coadministration of Na2EDTA. No substantial influence of varying the rectal delivery rate was observed. The results suggest that absorption enhancement and enzyme inhibition both are essential for effective increase of rectal peptide bioavailability. 相似文献
993.
Problems associated with the use of 5-iodo-2-deoxyundine (IDU) in the treatment of herpes simplex keratitis can be attributed largely to the polar nature of IDU resulting in its poor permeability across the lipoidal epithelial layer of the corneal membrane. Five aliphatic 5-esters of IDU were synthesized and evaluated as prodrugs for potential use in the treatment of deep ocular infections such as stromal keratitis, iritis, and even retinitis. A parabolic relationship between in vitro corneal membrane permeability and carbon chain length of prodrugs is evident. For a given prodrug, enzymatic hydrolysis proceeded most readily in iris–ciliary body, followed by cornea and aqueous humor. An increase in carbon chain length made the prodrugs more enzymatically labile but more resistant to chemical hydrolysis at pH 7.4 and 34°C. The 5-butyryl ester of IDU exhibited an approximately fourfold increase in aqueous humor IDU concentration relative to IDU at 25 min following instillation of 25-µl 5 mM solutions. 相似文献
994.
Wen FQ Kohyama T Sköld CM Zhu YK Liu X Romberger DJ Stoner J Rennard SI 《Inflammation》2002,26(6):279-290
TGF- is thought to play a central role in pulmonary fibrosis inducing fibroblast differentiation and extracellular matrix synthesis. In human lung fibroblasts, it is still unclear how various TGB- isoforms affect TGF- production and whether glucocorticoids, commonly used agents to treat fibrotic lung disease, modulate these processes. To this end, human fetal lung fibroblasts (HFL-1) were cultured with various concentrations of glucocorticoids (budesonide, dexamethasone or hydrocortisone) with and without TFG-1, -2, and -3. TGF- mRNA was assessed by real time RT-PCR. Smad 2, 3, and 4 and AP-1 complex (c-fos and c-Jun) cellular localization were evaluated by immunostaining. TGF-2 and -3 stimulated TGF-1 production significantly (p < 0.01 relative to control). TGF-1 stimulated TGF-2 production (p < 0.01 relative to control). TGF-3 was undetectable. Glucocorticoids significantly inhibited TGF-1 and -2 production and reduced expression of the upregulated TGF-1 and -2 mRNA induced by exogenous TGF-1, -2 or -3 (p < 0.01 for each) but had no effect on Smads. Although c-jun-related nuclear staining was not intensified in TGF--stimulated cells, it was reduced by glucocorticoids. Thus, TGF- isoforms may stimulate production of various TGF- isoforms in the lung. Glucocorticoids then may block TGF- production by modulating mRNA levels and c-Jun. 相似文献
995.
目的 :通过测定妊高征 (PIH)患者红细胞免疫粘附 (RCIA)调节因子活性 ,探讨PIH患者红细胞免疫功能改变的原因。方法 :测定 40例PIH患者和 30例正常孕妇的RCIA促进因子活性和抑制因子活性及红细胞补体受体花环率(RBCC3bRR% )、红细胞免疫复合物花环率 (RBCICR % )。结果 :与正常孕妇相比 ,PIH患者RCIA抑制因子活性明显升高 ,RBCC3bRR%及RBCICR %明显降低 (P <0 .0 1) ,RCIA促进因子活性无明显变化 (P >0 .0 5 )。结论 :PIH患者红细胞免疫功能原发低下 ,其原因可能与RCIA抑制因子活性增高有关 相似文献
996.
A female patient with a clinical picture of Turner's syndrome had five separate malignant tumors (three squamous cell carcinomas of the tongue, a colon cancer, and a glioblastoma multiforme). Her peripheral blood cells showed a 45,X/46,XXp-/46,XX/47,XXX mosaicism. The findings are discussed in relation to other extragonadal tumors in Turner's syndrome reported to-date. 相似文献
997.
Effects of chemical mediators of anaphylaxis on ciliary function 总被引:2,自引:0,他引:2
Adam Wanner M.D. David Maurer Ph.D. William M. Abraham Ph.D. Zsolt Szepfalusi Marek Sielczak M.D. 《The Journal of allergy and clinical immunology》1983,72(6):663-667
We assessed the effects of selected chemical mediators of anaphylaxis on CBF in vitro. Ciliated epithelial cells were obtained from the trachea of conscious sheep with a cytology brush and suspended in a perfusion chamber containing KH. Ciliary activity was viewed microscopically and recorded on videotape for subsequent slow-motion analysis of CBF. Prostaglandin E1 (10(-8) M to 10(-6) M), prostaglandin E2 (10(-10) M to 10(-6) M), and leukotriene-C4 (10(-8) M) increased CBF between 7% and 33%. Histamine caused ciliostimulation only at the relatively high concentrations above 10(-5) M (7% increase in CBF), whereas prostaglandin F2 alpha (10(-10) M and 10(-6) M) was without effect. In no preparation was ciliary discoordination observed. These findings indicate that several chemical mediators of anaphylaxis stimulate CBF and that the previously described impairment of mucociliary transport in stable allergic asthma or antigen-induced bronchoconstriction is probably not caused by a primary alteration of ciliary function. 相似文献
998.
Francois B. Michel M.D. Jean Bousquet M.D. Philippe Greillier M.D. Michle Robinet-Levy Ph.D. Yves Coulomb Sc.D. 《The Journal of allergy and clinical immunology》1980,65(6):422-430
Total serum IgE levels were determined in 136 newborns and their mothers and in 54 of their fathers, using the paper radioimmunosorbent test (PRIST) technique. IgE specific antibodies for house dust (Dermatophagoides pteronyssinus), orchard grass, timothy grass, and cow's milk were measured with the radioallergosorbent test (RAST). One hundred thirty-three RAST assays were negative in newborns, and in three cases RAST for cow's milk was positive. Cord blood IgE ranged from 0 to 5.5 IU/ml (mean 0.32 ± 0.54 IU/ml); levels were significantly (p < 0.05) higher when maternal IgE was over 100 IU/ml and when mothers had received progesterone therapy during the pregnancy. Salbutamol administration or tobacco smoking during pregnancy did not influence newborn IgE. A clinical follow-up study was conducted in 83 infants for 9 mo. Nine infants developed definite atopic disease, and possible allergic diseases were noted in eight other infants. The IgE level at birth appeared to be more predictive for the development of allergy in infancy than the family history. 相似文献
999.
Sen Pathak 《Cancer Genetics and Cytogenetics》1980,1(3):281-289
Cytogenetic analysis using C-, G-, and Ag-nucleolus organizer region (NOR) staining techniques, performed on established cell lines as well as directly processed breast tumor effusions, revealed that: 1) chromosome No. 1 is involved in translocation; 2) based on 1q translocation chromosome, breast tumors could be classified into two groups; and 3) double minutes and homogeneously staining regions may be present in breast tumor cells in vivo as well as in vitro, and that homogeneously staining regions may exhibit some heterogeneity in staining. 相似文献
1000.
Allegria Kessous Pierre Colombies Martine Sudries Georges Bourrouillou Jacques Pris Danielle Clement 《Cancer Genetics and Cytogenetics》1980,2(4):335-337
This report describes a new case of chronic myeloid leukemia with an unusual Philadelphia chromosome translocation involving chromosomes No. 4,9, and 22; t(4,9,22) (q31;q34;q11). 相似文献