Purification of 2-deoxy-2-dansylamido-D-glucose by affinity chromatography on a lectin-loaded agarose column.

A method is demonstrated to purify 2-substituted derivatives of glucose and sterically related sugars by affinity chromatography on Con A-sepharose. The method seems to be of rather general applicability.     

Purification of 2-deoxy-2-dansylamido-D-glucose by affinity chromatography on a lectin-loaded agarose column

Summary A method is demonstrated to purify 2-substituted derivatives of glucose and sterically related sugars by affinity chromatography on Con A-sepharose. The method seems to be of rather general applicability.     

Effect of dibutyryl cyclic AMP and analogs on the rate of contractions of myocytes in culture.

2O, 6N-butyryl, 3', 5'-cyclic monophosphate (dibu cAMP) when added to fetal rat heart cells in culture inhibits myocyte contraction. This inhibition is 100, 84 and 51% complete when the dibu cAMP concentration used is 2, 0.2 and 0.02 mM, respectively. The potency of dibu cAMP derivatives in myocyte contraction inhibition follows the order, dibu cAMP greater than 6N-bu cAMP greater than 2O-bu cAMP = AMP greater than butyrate. The inhibition caused by the first three chemicals is greater than 70%.     

Correlation between 3',5', c-AMP levels and thyrotropin in separated rat pituitary thyrotropic cells.

The correlation between 3',5', c-AMP levels, TSH content and secretion of separated thyrotropic cells was studied. Incubation of the separated cells with 1, 10 and 100 ng of TRH does not change the 3',5',c-AMP levels, despite the significant rises of the TSH level. Dibutyryl c-AMP causes rise in TSH content, with no indication of its secretion. PGE2 10(-5) increased 3'5',c-AMP levels with no change in the content or secretion of TSH in separated thyrotropic cells.     

Biological activity of precocene analogues onLocusta migratoria

Summary Structure-optimization studies of C-5-C-8-substituted precocene (P) analogues revealed that 1) compounds disubstituted asymmetrically at C-6, C-7 had an anti-allatal effect only if the C-6 side-group was shorter than that at C-7, 2) in the case of C-5, C-7 disubstitution, activity was enhanced by Me at C-5 whereas MeO caused inactivity. Effects of various other substitutions are also discussed.     

链霉素诱导的2型糖尿病大鼠模型的肾脏功能变化

目的通过观察链霉素诱导的2型糖尿病大鼠模型肾脏功能的变化,以探讨此种模型是否适用于糖尿病肾损害的研究。方法采用链脲佐菌素(streptozotocin,STZ)辅以高脂饮食建立2型糖尿病大鼠模型,筛选造模成功的大鼠为糖尿病组,并与正常大鼠比较,造模后8周观察两组大鼠血糖、血尿素氮(blood urea nitrogen,BUN)、血肌酐(creatinine,CR)、血糖基化终末产物(Advanced glycation end products,AGE)、尿微量白蛋白、肾重指数的变化以及AGE受体(Receptor of AGE,RAGE)、蛋白激酶C(protein kinase C,PKC)、蛋白激酶A(protein kinase A,PKA)在肾脏的表达变化。结果糖尿病组的血糖、血尿素氮、血肌酐、血AGE、尿微量白蛋白以及肾重指数均明显高于正常组(P0.05),RAGE、PKC的mRNA以及蛋白表达水平均较正常组高(P0.05),PKA的mRNA和蛋白表达水平则较正常组低(P0.05)。结论 STZ诱导的2型糖尿病大鼠模型在造模后第8周肾脏功能存在明显的损害,并且导致肾脏损害的上游重要介质RAGE、PKC、PKA在第8周都有着明显的变化。此种模型能够用于糖尿病肾损害的研究,并且是观察中早期糖尿病肾病的较好的模型。     

Antihypertensive and other cardiovascular effects of 2-(3-pyridyl)- and 2-(4-pyridyl)-4-trifluoromethylimidazoles.

2 new 4-trifluoromethylimidazole derivatives were found which lowered mean arterial pressure in renal and spontaneously hypertensive (SH) rats by the oral route. In SH rats, compounds A and B were 0.1 and 0.3 times, respectively, as potent as hydralazine. No tolerance development was observed in SH rats with either compound over a 1-week period. In anesthetized dogs, both compounds lowered arterial pressure and peripheral vascular resistance but increased cardiac output. By intraarterial administration, both compounds increased femoral arterial blood flow. These findings represent discovery of a new class of vasodilator durgs.     

La pression intrarénale chez l'homme

Summary The intrarenal pressure has been determined in man using a needle of the lumbal puncture type connected with a mercury manometer. Preliminary results in 8 patients with various renal diseases indicate no significant difference between cases of glomerulonephritis, acute anuria, chronic pyelonephritis and normal or almost normal kidneys. Our values are comprised between 23.5 and 41.5 mm of mercury, with an average of 34 mm. A possible correlation with the mean blood pressure is suggested by our data: intrarenal pressure =0.19 mean blood pressure +9.0. In one case, renal decapsulation had no influence on the intrarenal pressure.     

Antihypertensive and other cardiovascular effects of 2-(3-pyridyl)- and 2-(4-pyridyl)-4-trifluoromethylimidazoles

Summary 2 new 4-trifluoromethylimidazole derivatives were found which lowered mean arterial pressure in renal and spontaneously hypertensive (SH) rats by the oral route. In SH rats, compounds A and B were 0.1 and 0.3 times, respectively, as potent as hydralazine. No tolerance development was observed in SH rats with either compound over a 1-week period. In anesthetized dogs, both compounds lowered arterial pressure and peripheral vascular resistance but increased cardiac output. By intraarterial administration, both compounds increased femoral arterial blood flow. These findings represent discovery of a new class of vasodilator drugs.Deceased, May 31, 1978.     

Teratogenicity screening in standardized chick embryo culture: effects of dexamethasone and diphenylhydantoin

Teratogenic and toxic effects of DXM and DPH were tested using a standardized chick embryo culture. Survival, growth and malformations were scored with respect to the drug concentrations used. DXM (greater than 10(-8) mol/l) inhibited the differentiation of the extraembryonic blood circulation and induced craniofacial anomalies. DPH (greater than 1.5 10(-5) mol/l) induced cardiomegaly, craniofacial and somitic anomalies. Both drugs were lethal at 10(-3) mol/l. Comparison of results obtained with 8 drugs shows that the method has a good discriminative power and specificity and that it can be used as a simple, reliable and economical primary screening test, making it possible to reduce the use of animals in toxicological studies.     

Hemmungswirkungen verschiedener Indophenole auf die Wasserstoff-peroxydzersetzung durch Blutkatalase

Summary Some indophenol derivatives inhibit strongly the activity of blood catalase. These effects were investigated quantitatively and compared with similar effects due to other oxidizing and reducing agents.     

The special Sm core structure of the U7 snRNP: far-reaching significance of a small nuclear ribonucleoprotein

The polypeptide composition of the U7 small nuclear ribonucleoprotein (snRNP) involved in histone messenger RNA (mRNA) 3' end formation has recently been elucidated. In contrast to spliceosomal snRNPs, which contain a ring-shaped assembly of seven so-called Sm proteins, in the U7 snRNP the Sm proteins D1 and D2 are replaced by U7-specific Sm-like proteins, Lsm10 and Lsm11. This polypeptide composition and the unusual structure of Lsm11, which plays a role in histone RNA processing, represent new themes in the biology of Sm/Lsm proteins. Moreover this structure has important consequences for snRNP assembly that is mediated by two complexes containing the PRMT5 methyltransferase and the SMN (survival of motor neurons) protein, respectively. Finally, the ability to alter this polypeptide composition by a small mutation in U7 snRNA forms the basis for using modified U7 snRNA derivatives to alter specific pre-mRNA splicing events, thereby opening up a new way for antisense gene therapy.     

Changes in the activities of protein kinase modulators in the cerebellum of mice due to ethanol, caffeine, or phenobarbital administration.

Decreased activities of both the inhibitory modulator of adenosine 3':5'-monophosphate (cAMP)-dependent protein kinase (A-PK) as well as the stimulatory modulator of guanosine 3':5'-monophosphate (cGMP)-dependent protein kinase (G-PK) from the mouse cerebellum were noted due to the administration of excessive doses of ethanol, caffeine, and phenobarbital for up to 28 days. The dose-dependent of the inhibition of A-PK or the stimulation of G-PK was observed as a function of the amount of protein kinase modulators in the cerebellum of mice receiving different doses of ethanol.     

Brain cyclic nucleotide and energy metabolite responses to subanesthetic and anesthetic concentrations of halothane

Adult rats were exposed to 0.5, 1.0 and 1.5% halothane, delivered in air, for 1 h. Whole brain 3',5'-cyclic adenosine monophosphate (cAMP) of halothane-exposed rats showed only a slight increase relative to control values. 3',5'-Cyclic guanosine monophosphate (cGMP) was increased significantly in halothane-exposed rats, and the response was directly related to the halothane concentrations. Adenosine triphosphate (ATP) and phosphocreatine (PC) remained unchanged relative to control values. Correspondence of these values to apparent discrepancies in the literature is discussed.     

解聚复肾宁对糖尿病肾病大鼠TNF—OL、MCP-1的影响

目的观察解聚复肾宁（Jiejufushenning,JJFSN）对糖尿病（Diabetes mellitus,DM）大鼠肾组织肿瘤坏死因子-α（Tumorneerosisfactor-alpha,TNF-α）、单核细胞趋化蛋白-1（Monocyte chemoattractant protein-1,MCP-1）和血清TNF-α的影响,探讨其肾保护作用机制。方法腹腔注射链脲佐菌素（Streptozotocin,STZ）建立SD大鼠DM模型,将成模DM大鼠随机分为3组：DM模型组（B组）、JJFSN组（C组）、厄贝沙坦（Irbesartan）组（D组）,另设正常对照组（A组）。采用相应干预措施处理12周。常规方法测定12周末各组大鼠空腹血糖（FBG）、血尿素氮（BUN）、血肌酐（Scr）、肾重／体重（KW／BW）、24h尿蛋白（24huFro）;放免法测血清TNF-α含量：免疫组织化学方法测肾组织TNF—Ot、MCP-1的表达;PAS染色评估细胞外基质;电镜观察肾组织超微结构改变。结果与A组相比．B组大鼠FBG、BUN、Scr、KW／BW、24huPro及血清TNF-α升高（P〈0．05）,肾组织TNF—Ot、MCP-1表达明显增高（P〈0．05）;肾组织超微结构明显异常;C组和D组上述指标显著改善（P〈0．05）,肾组织超微结构异常改善。结论竹FSN能延缓DM大鼠肾损害进程,其机制可能与抑制TNF-α、MCP-1上调有关。     

Darstellung von Derivaten des 6-Chlor-17β-acetoxy-Δ 5-androsten-7-on

Summary 6-Chloro-17-acetoxy-5-androsten-7-one and some of its derivatives have been prepared from ⁵-steroids by a synthesis involving elimination of the substituent from position 3, introduction of a 7-keto group by allyloxidation and chlorination of the resulting compound with sulphuryl chloride.     

Molecular cloning of a cDNA encoding alpha-glucosidase in the digestive gland of the shrimp, Litopenaeus vannamei

The complete sequence of the 3-kb cDNA and the 5' genomic structure are reported for the gene encoding the shrimp alpha-glucosidase. Alpha-glucosidase cDNA was isolated from a shrimp digestive gland cDNA library. The 2830-base pair cDNA contains an open reading frame that encodes 919 amino acids. The shrimp alpha-glucosidase cDNA shows a high level of identity with that of the human sucrase-isomaltase, human maltase-glucoamylase, and human acid lysosomal alpha-glucosidase, indicating that the protein shares the same structural domains. The similarities among these proteins are found as clusters and characterize the glycosyl hydrolase family 31. To our knowledge, this is the first report to describe a satellite sequence in the 5' genomic structure before the TATA box in an invertebrate sequence.     

Maternal influences on cardiovascular pathophysiology.

Elevated blood pressure (BP) is of special clinical significance because of its association with pathophysiologies such as heart disease, renal failure, and stroke. We described the development of a protocol for use with hypertensive rats in which prepubertal exposure to a high salt (8% NaCl) diet results in a pathophysiological syndrome including rapid increase in BP, failure to maintain normal weight gain, renal damage, cerebrovascular lesions, and early mortality. These phenomena are described for the inbred spontaneously hypertensive rat (SHR), and for reciprocal F1 hybrids of a cross between SHR and the Dahl salt-sensitive (SS/Jr) inbred strain. The study with reciprocal F1s revealed striking effects of maternal environment on pathophysiological response to a high salt diet. F1s nurtured by SHR mothers weighed less at 35 days of age, and after exposure to the high salt diet suffered more rapid BP increases, greater incidence of stroke, body weight loss, and mortality, than F1s nurtured by SS/Jr dams. These results suggest that maternal mediation of the nutritional status of the animal may play an important role in determining susceptibility to elevated BP and subsequent pathophysiology associated with exposure to a high salt diet. The implication of these findings for human hypertension is briefly discussed.     

Detection of pyrimidine 5'-nucleotidase deficiency using 1H- or 31P-nuclear magnetic resonance

We describe here a further Japanese family with pyrimidine 5'-nucleotidase (P5'N) deficiency diagnosed using a nuclear magnetic resonance (NMR) spectrum, in Kumamoto prefecture where two families having the disease have been reported before. The specific spectra in 1H-NMR of P5'N deficient erythrocytes were due to three methyl protons of CDP-choline at 3.22 ppm and to H-2, H-8 and ribose-1' of pyrimidine nucleotide phosphate(s) in the lower fields (at 5.82 and 8.00 ppm). The other specificities in 31P-NMR spectra were due to CDP-choline, CDP-ethanolamine and UDP-glucose. Those spectra were not detected in other types of hemolytic anemia.