Studies on the synthesis of oligonucleotides containing photoreactive nucleosides: 2-azido-2'-deoxyinosine and 8-azido-2'-deoxyadenosine

Oligonucleotides containing the photoreactive nucleosides 2-azido-2'-deoxyinosine and 8-azido-2'-deoxyadenosine have been prepared using protected 2-fluoro-2'-deoxyinosine and 8-bromo-2'-deoxyadenosine phosphoramidites. After the assembly of the oligonucleotides, the nucleoside derivatives are converted to the corresponding azido derivatives by treatment with lithium azide in dry DMF. Deprotection of oligonucleotides carrying these azidonucleosides is performed with concentrated ammonia at room temperature.     

Studies of gamma-oryzanol (1). Effects on stress-induced ulcer

In clinical trials, it is well known that gamma-oryzanol is effective against the syndromes of autonomic nervous unbalance and climacteric disorders. The authors studied the action of gamma-oryzanol on restraint, water-immersion stress ulcer under various conditions in rats. The drug, given 1 to 100 mg/kg s.c. daily for five days, reduced the ulcer index dose-dependently, and slightly prevented the rate of increase in serum level of 11-OHCS. These effects were observed in adrenalectomized as well as sham operated rats. It is likely that the antiulcerogenic action of gamma-oryzanol is due to participation of the autonomic nervous system, but not the hypophyseoadrenal axis.     

Stepwise synthesis of oligonucleotides. XXII. The synthesis of Tpsi-loop fragments of yeast tRNAIVal and their analogs

The method of the combined use of nucleolytic enzymes was used for the synthesis of Tpsi-loop fragments of yeast valine tRNA and their analogs. Dinucleoside monophosphates, trinucleoside diphosphates and tetranucleoside triphosphates having the sequences of fragments 54-57 and 59-62 or their analogs were synthesized.     

Studies on stannous fluoride toothpaste and gel (1). Antimicrobial properties and staining potential in vitro

Although there is evidence that endogenous opioids, and in particular beta-endorphin (beta-EP), may mediate some of the suppressive effects of hyperprolactinemia on the hypothalamic-pituitary-gonadal (HPG) axis, there is controversy about the effects of prolactin (PRL) on beta-EP and its precursor, proopiomelanocortin (POMC), in the hypothalamus. In this study we have therefore examined the effects of chronic peripheral and intracerebroventricular (i.c.v.) infusion of ovine PRL on POMC gene expression and beta-EP levels in the medial basal hypothalamus (MBH) of castrated male and female rats. Endogenous pituitary and plasma PRL levels were determined by RIA with an antiserum to rat PRL which does not crossreact with oPRL. Suppression of endogenous rPRL levels was used as a confirmation of the biological effectiveness of the infused oPRL. POMC mRNA was measured in the MBH by solution hybridization assay. In the first experiment oPRL (5 microg/microl/h) or vehicle was infused for 2 weeks by osmotic minipump into the right lateral ventricle of ovariectomized rats. The mean plasma concentration of rPRL declined from 3.7+/-1.0 ng/ml in the controls to 1.4+/-0.13 ng/ml in the oPRL infused animals (P<0.05); pituitary rPRL content similarly decreased from 39.1+/-4.6 microg to 20.4+/-3.7 microg (P<0.02). There was no significant change in the concentration of POMC mRNA or beta-EP in the MBH of the oPRL treated animals. In the second experiment oPRL was infused for 1 week into the third ventricle of orchiectomized rats. Again despite a fall in endogenous PRL levels, there was no significant change in POMC or beta-EP in the MBH. In the third experiment oPRL was infused subcutaneously into orchiectomized rats for 2 weeks. Mean plasma oPRL levels were 150+/-7.3 ng/ml after 1 week and 58+/-7.5 ng/ml after 2 weeks. Pituitary rPRL content was again suppressed in the oPRL treated animals but no change in POMC or beta-EP was detected in the MBH. We conclude that oPRL can be infused both peripherally and centrally for up to 2 weeks with resulting suppression of endogenous pituitary PRL content and release. Under these conditions no effects on the concentrations of POMC mRNA or beta-EP could be demonstrated in the hypothalamus. These results suggest that either PRL has nongenomic effects on hypothalamic beta-EP or that endogenous opioids other than beta-EP mediate the suppressive effects of PRL on the HPG axis.     

Physicochemical interaction and structure development during the formation of metal gas-transfer coatings on diamond (review). 1. Kinetics

Work devoted to studying the phase composition and thickness of chromium, titanium, molybdenum, vanadium, and tungsten coatings which form on diamond powder during vacuum annealing of this powder mixed with chromium powder or oxidized powders of Ti, Mo, V, and W is analyzed. Coatings consist of metal (Cr, Ti, Mo, V, W) and carbide (Cr₇C₃, Cr₃C₂, TiC, -Mo₂C, V₂C, VC, W₂C, WC) phases. Diffusion of carbon during coating growth with increased metallizing time and temperature causes carbidization of chromium, titanium, and vanadium (it causes a reduction in the content of metal phase and an increase in carbide phases is coatings), growth of higher carbides (Cr₃C₂, VC, WC) at the expense of lower carbides (Cr₇C₃, V₂C, W₂C), and filling of carbon vacancies in the lattices of TiC and VC. Saturation of coatings with carbides correlates with the temperature-time range in which a further increase in coating weight slows down.Translated from Poroshkovaya Metallurgiya, No. 7(355), pp. 34–40, July, 1992.     

Regulation of ribosomal RNA synthesis and processing during inhibition of protein synthesis by 1,3-bis(2-chloroethyl)-1-nitrosourea

The antineoplastic agent BCNU (1,3-bis(2-chloroethyl)-1nitrosourea) at a concentration of 25 mug/ml inhibits initiation of protein synthesis in HeLa cells. At this low concentration of the drug, the rate of synthesis of 45S ribosomal precursor RNA (pre-rRNA) is selectively inhibited without a marked inhibition of nucleoplasmic RNA. The inhibitory effects of the drug are readily reversible upon removal of BCNU from the growth medium. Pulse-chase analysis of the labeled nucleolar RNA in sucrose-gradients and acrylamide gels indicated that the 45S pre-rRNA synthesized before the addition of BCNU matures normally in the presence of the inhibitor. However, the processing of precursor RNA molecules synthesized following the addition of the drug is inhibited when incubation is continued on in the presence of 25 mug/ml BCNU. Since the formation of mature ribosomes is blocked by BCNU, the data would suggest that the effectiveness of the drug as a potent cell growth inhibitor may result from its inhibition of ribosome formation induced by inhibition of protein synthesis.     

Studies on the testis of the camel (Camelus dromedarius). III. Histochemical observations

The histochemical localization of carbohydrates and lipids and some oxidative, hydrolytic and steroid-linked enzymes has been studied in the testis of the camel with particular reference to the effect of the season on the distribution of these substances. PAS-positive, but diastase-resistant, material was seen mainly in the wall of blood vessels and in the boundary tissues of the seminiferous tubules, tubuli recti and rete testis. Clear cyclical changes were seen for glycogen in the lining epithelium of the seminiferous tubules. Glycogen was most abundant in early stages and very scanty or absent in the late stages of the cycle of the seminiferous epithelium. Numerous small lipid droplets were seen in the interstitial cells and towards the lumen of the seminiferous tubules that contain elongate spermatids or spermatozoa. Large lipid droplets were also demonstrable in the basal layer of the seminiferous epithelium and in the cytoplasmic debri. Alkaline phosphatase was demonstrated in the boundary tissues of the seminiferous tubules, tubuli recti and reti testis and in the cells bordering the lumen of the seminiferous tubules. Succinate and lactic dehydrogenases showed similar patterns of distribution in the interstitial elements and intratubularly. delta5-3beta hydroxysteroid dehydrogenase was exclusively demonstrated in the interstitial cells. 17beta-hydroxysteroid dehydrogenase could not be demonstrated. The season seems to have no effect on the distribution of all these substances. The possible significance of all these findings is discussed.     

Antisense oligonucleotides, a novel tool for the control of cytokine effects on human cartilage. Focus on interleukins 1 and 6 and proteoglycan synthesis

OBJECTIVE: To prevent the negative effects of interleukin-1 (IL-1) and IL-1-induced IL-6 on cartilage proteoglycan (PG) synthesis, we used an antisense oligonucleotide (ASO) specific for IL-6 messenger RNA (mRNA) to inhibit IL-6 production. METHODS: Explants of human articular cartilage were cultured in the presence or absence of IL-6-ASO, IL-1, and exogenous IL-6. As metabolic parameters, cartilage production of IL-6 was determined in the B9 bioassay and PG as incorporation of 35SO4. RESULTS: The IL-6-ASO prevented IL-1-induced production of IL-6 in the cartilage explants, as well as IL-1-induced inhibition of PG synthesis. This inhibition was restored, despite the presence of IL-6-ASO, when exogenous IL-6 was added. A control ASO (not specific for IL-6 mRNA) was not effective. CONCLUSION: The IL-6-ASO used can penetrate the extracellular matrix of articular cartilage, enter the chondrocytes, and inhibit the IL-1-induced production of IL-6. Furthermore, IL-6-ASO can prevent the IL-1-induced inhibition of cartilage PG synthesis. The effect of exogenous IL-6 shows that IL-1 requires IL-6 for inhibition of PG synthesis.     

Examining the beneficial components of groups: Commentary on Estabrooks and Carron (2000) and Terry et al. (2000).

This article discusses specific areas of cohesion research and expands the focus by examining other research on the beneficial components of therapeutic group processes. Exploring the P. C. Terry et al (see record 2000-12222-004) article and other outcome-based studies in the field provides direction for future research on group cohesion and other therapeutic factors. Similarly, the excellent piece of measurement development by P. A. Estabrooks and A. V. Carron (see record 2000-12222-003) generates discussion of issues in relation to other group measurement research. Cautions about producing research with limited generalizability are discussed in the context of unifying a broad spectrum of group investigations. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Non-Carbon Nanotubes (Review). Part 2. Types and Structure

Various types and structures of synthesized non-carbon nanotubes (N-NT) based on carbonitrides B _x C _y N _z , boron nitride BN, sulfides WS₂, MoS₂, selenides NbSe₂, halides NiCl₂, transition metal oxides SiO₂, TiO₂, MoO₃, V₂O₅ are considered, as well as theoretically predicted N-NT based on P, Si, Ge, and III-V semiconductors. General criteria for the stability of non-carbon nanotubes are analyzed.     

Non-Carbon Nanotubes (Review). Part 2. Types and Structure

Various types and structures of synthesized non-carbon nanotubes (N-NT) based on carbonitrides B _x C _y N _z , boron nitride BN, sulfides WS₂, MoS₂, selenides NbSe₂, halides NiCl₂, transition metal oxides SiO₂, TiO₂, MoO₃, V₂O₅ are considered, as well as theoretically predicted N-NT based on P, Si, Ge, and III-V semiconductors. General criteria for the stability of non-carbon nanotubes are analyzed.

     

Studies on synthesis and fluorescent property of rare earth complexes RE（ABMF）2AA and copolymers RE（ABMF）2AA-co-MMA

Four new complexes RE(ABMF)2AA (RE=Sm, Eu, Tb, Dy) were synthesized by the reaction of RECl3·6H2O with acrylic acid (HAA) and 1-(2-furyl)-3-phenyl-1,3-propanedione (ABMF). The copolymerization of the rare earth complexes with methyl methacrylate was studied by using 2,2-azobis-isobutyronitrile as an initiator. The composition and structure of the four complexes were characterized by elemental analysis, UV-vis and FTIR. The glass transition temperature and molecular weight of the copolymers were determined. Photoluminescent measurement showed that ligand ABMF could efficiently transfer the energy to Sm3+ and Eu3+ ions in the complexes and sensitize the luminescence of the rare earth ions, but could not sensitize Tb3+ and Dy3+ ions. As a result, both Sm3+ and Eu3+ complexes emitted the characteristic fluorescence of Sm3+ and Eu3+ ions due to the f-f transitions. The four copolymers could emit strong fluorescence of the rare earth ions.     

Pharmacological studies of 4-ethoxy-2-methyl-5-morpholino-3(2H)-pyridazinone (M73101). (1). Analgesic activity (author's transl)

The analgesic activity and the mode of action of M73101, a new analgesic anti-inflammatory agent, were investigated in mice and rats and compared to those of reference drugs. M73101 showed a marked analgesic activity against noxious stimuli induced by pressure (Haffner method and Randall-Selitto method), thermal (hot plate method), electric and chemical (acetic acid-stretching method and bradykinin-induced responses) stimulation, in a manner similar to those of basic anti-inflammatory drugs (BAD) such as aminopyrine, mepirizole, tiaramide HCl, and benzydamine HCl. The activities of M73101 were equal to and/or more potent than those of BAD, and more potent than those of acidic anti-inflammatory drugs. In addition, the analgesic activity of M73101 was not decreased by the pretreatment with levallorphan and showed no cross-tolerance to morphine in mice, indicating that the analgesic properties of M73101 differ from those of morphine. On the other hand, the analgesic activity of M73101 as well as BAD was decreased by repeated oral administration in mice, and the potency was weaker than mepirizole. Furthermore, the muscle relaxant effect of M73101 obtained by inclined screen test in mice was the weakest among the BAD, suggesting that analgesic activity of M73101 is not related to the muscle relaxant property. These results indicate that M73101 may be useful for clinical application as an anti-inflammatory drug possessing remarkable analgesic activity.     

Solid-phase synthesis of oligonucleotides containing site-specific N-(2'-deoxyguanosin-8-yl)-2-(acetylamino)fluorene adducts using 9-fluorenylmethoxycarbonyl as the base-protecting group

Eight oligodeoxyribonucleotides containing a site-specific N-(2'-deoxyguanosin-8-yl)-2-(acetyl-amino)fluorene (dG-C8-AAF) adduct were prepared successfully by solid-phase DNA synthesis using the 2-cyanoethyl N,N-diisopropylphosphoramidites of dA, dC, dG, dT, and dG-C8-AAF, with 9-fluorenyl-methoxycarbonyl (Fmoc) as the base-protecting group. The oligonucleotides were deprotected and released from the support by 1:9 piperidine/MeOH at room temperature for 22-36 h or by 1:1 diisopropylamine in MeOH at 55 degrees C for 15 h, purified by HPLC, and fully characterized. About 6 mg of HPLC-purified d[GTGGCG(C8-AAF)CCAAGT] and 7 mg of d[GTGATG(C8-AAF)ATAAGT] were obtained from the 10-mumol-scale synthesis, and their 1D 1H NMR spectra were consistent with the presence of a dG-C8-AAF adduct. The dG-C8-AAF oligonucleotides were also deacetylated to afford the corresponding dG-C8-AF oligonucleotides. d[GTGGCG(C8-AAF)CCAAGT] formed stable 1:1 duplexes with both the fully complementary 12-mer and a GC-deleted (across the adduct) 10-mer complement, and identical melting temperatures were observed for both duplexes. The multidimensional NMR study of these duplexes is presently under investigation.