Biomedical subjects

R Zhao

Publications and source records attributed to R Zhao.

At least 127 records · Page 7Linked to original sources

PubMed1998

[Effects of dopexamine on cardiac hemodynamics during myocardial ischemia in rats and in comparison with fenoldopam and procaterol].

The effect of dopexamine hydrochloride(DPX) on cardiac hemodynamics during acute myocardial ischemia (AMI) was studied in rats and compared with those of fenoldopam hydrochloride(FODA) and procaterol hydrochloride (PCT). The results showed that i.v. DPX remarkably attenuated the increases of total peripheral resistance(TPR) and left ventricular end-diastolic pressure and the decreases of + dp/dt max caused by ischemia, while DPX showed no significant effect on mean arterial pressure(MAP). Although FODA was more potent than DPX in attenuating the increase of TPR and the decrease of myocardial contractility caused by ischemia, it significantly decreased MAP. The effects of PCT on all these variables were the smallest among the 3 agents. The results suggest that DPX has a better prospect in the treatment of ischemic heart disease in view of its actions of decreasing TPR, mild increase of myocardial contractility, without MAP decrease and myocardial oxygen consumption increase.

Adrenergic beta-2 Receptor Agonists↗

PubMed1998

[Effects of l-stepholidine on the peripheral vascular dopamine DA1 and DA2 receptor subtypes].

The effects of l-stepholidine(l-SPD) on peripheral vascular dopamine DA1 and DA2 receptors were studied using isolated vascular rings in rabbits. It was shown that (1) l-SPD(0.1-10 mumol.L-1) shifted the dose-response curves to the right in a nonparallel fashion and decreased the maximal response (Emax) of both the fenoldopam(FODA, a selective DA1 agonist)-induced and the propyl-buty-dopamine(PBDA, a selective DA2 agonist)-induced vasorelaxation showing a non-competitive antagonistic action. The pD2 values of l-SPD for FODA in the renal, pulmonary and mesenteric arteries were 5.43, 5.48 and 5.58, respectively. The pD2 values for PBDA in the mesenteric and femoral arteries were 5.35 and 5.89, respectively. The potencies of its antagonistic action were comparable to SCH23390, a selective DA1 antagonist, and to domperidone, a selective DA2 antagonist. (2) l-SPD(0.1-100 mumol.L-1) per se was also found to induce slight but dose-related vasorelaxations in the renal and pulmonary arteries displaying its DA1 agonistic activity. Its pD2 values were 4.98 and 5.02, respectively. However, its Emax were considerably smaller than that of FODA. These results suggest that l-SPD is a mixed peripheral DA1 and DA2 receptor antagonists and weak DA1 receptor agonist with pharmacological property of dual action.

Animals↗

PubMed1998

[Investigation of hepatitis G virus and human immunodeficiency virus infections in 831 healthy youths].

Antibodies to hepatitis G virus(HGV) and human immunodeficiency virus(HIV) by EIA were investigated in 831 healthy youths from 6 provinces. The results showed that the anti-HGV IgG positive rate was 2.53% (21/831). In 21 anti-HGV IgG positive sera, HGV RNA was detected in 8 sera by reverse transcription polymerase chain reaction(RT-PCR). The anti-HIV was negative in 827 sera. The data suggest that HGV infection actually exist in healthy youths.

Adolescent↗

PubMed1998

[Math-model of efficient cultivation of Angelica sinensis].

Using two-time general rotation-constitution design, the math-mdele has been founded about Angelica sinensis prodution efficiency and quantity of nitrogen, phosphorus and potassium to use by doing experiments in many different spots and production demonstration for testing and verifying. Accordin to the modle, computer is used to simulate the better, through which people can get fresh Chinese angelica over 500 Kg per mu and also net income over 500 yuan per mu. It shows that this is the best combination. 95% density riliability for this plan is 6860-7600 plants, pure nitrogen 18.75-22.2 Kg, P2O5 9.1-11.1 Kg and K2O 4.46-5.37 Kg One mu. Proportion for nitrogen, phosphorus, potassium is 1:0.49:0.24.

Angelica↗

PubMed1998

Synthesis, topoisomerase I inhibitory activity and in vitro cytotoxicity of camptothecin derivatives bearing five-membered heterocycle containing 10-substituents.

A series of new camptothecin derivatives bearing certain five-membered heterocycles was synthesized and evaluated for in vitro cytotoxic activity. The cytotoxicity results show that camptothecin derivatives bearing pyrrole and thiophene rings were more potent than camptothecin, whereas those bearing furan were less active than camptothecin. Agarose gel electrophoresis shows different inhibitory activities of the camptothecin analogs towards topoisomerase I DNA cleavage. The pyrrole-containing compounds inhibit topoisomerase I DNA cleavage more strongly than camptothecin, but the thiophene and furan compounds do not show any inhibitory activities for DNA cleavage functions of topoisomerase I. Polyacrylamide gel sequencing electrophoresis shows that the pyrrole compounds induce single-strand breaks after incubating with a labeled DNA fragment. The results suggest that the pyrrole compounds fit the compound-enzyme-DNA complex better than camptothecin and the other analogs.

Animals↗

PubMed1997

Impact of overexpression of the reduced folate carrier (RFC1), an anion exchanger, on concentrative transport in murine L1210 leukemia cells.

Transport of reduced folates in murine leukemia cells is mediated by the bidirectional reduced folate carrier (RFC1) and independent unidirectional exit pumps. RFC1 has been proposed to be intrinsically equilibrating, generating transmembrane gradients by exchange with inorganic and organic anions. This paper defines the role of high level carrier expression, through transfection with RFC1 cDNA, on concentrative transport of the folate analog, methotrexate (MTX) in murine L1210 leukemia cells. RFC1 was expressed in the MTXrA line, which lacks a functional endogenous carrier to obtain the MTXrA-R16 clonal derivative. Influx was increased approximately 9-fold in MTXrA-R16 cells without a change in Km. The efflux rate constant was increased by a factor of 5.1 relative to L1210 cells, and this resulted in only a 2.1-fold increase in the steady-state level of free intracellular MTX, [MTX]i, when [MTX]e was 1 microM. The concentrative advantage for RFC1 (the ratio of [MTX]i in MTXrA-R16 to L1210 cells) increased from 1.8 at 0.1 microM MTX to 3.8 at an [MTX]e level of 30 microM. Augmented transport in MTXrA-R16 cells was accompanied by a 2-fold increase in accumulation of MTX polyglutamate derivatives and a approximately 50% decrease in the EC50 for 5-formyltetrahydrofolate and folic acid and the MTX IC50 relative to L1210 cells. These alterations paralleled changes in [MTX]i and not the much larger change in influx at low [MTX]e levels, consistent with the critical role that free intracellular folates and drug play in meeting cellular needs for folates and as a determinant of antifolate activity, respectively. The data indicate that RFC1 produces a large and near symmetrical increase in the bidirectional fluxes of MTX resulting in only a small increase in the transmembrane chemical gradient at low extracellular folate levels. Hence, increased expression of RFC1, alone, may not be an efficient adaptive response to folate deprivation, and other factors may come into play to account for the marked increases in concentrative folate transport which occur when cells are subjected to low folate-selective pressure.

Animals↗

PubMed1997

The refined structure of human rhinovirus 16 at 2.15 A resolution: implications for the viral life cycle.

BACKGROUND: Rhinoviruses belong to the picornavirus family and are small, icosahedral, non-enveloped viruses containing one positive RNA strand. Human rhinovirus 16 (HRV16) belongs to the major receptor group of rhinoviruses, for which the cellular receptor is intercellular adhesion molecule-1 (ICAM-1). In many rhinoviruses, one of the viral coat proteins (VP1) contains a hydrophobic pocket which is occupied by a fatty acid-like molecule, or so-called 'pocket factor'. Antiviral agents have been shown to bind to the hydrophobic pocket in VP1, replacing the pocket factor. The presence of the antiviral compound blocks uncoating of the virus and in some cases inhibits receptor attachment. A refined, high-resolution structure would be expected to provide further information on the nature of the pocket factor and other features previously not clearly identified. RESULTS: The structure of native HRV16 has been refined to a resolution of 2.15 A. The hydrophobic pocket in VP1 is observed in two alternative conformations. In one of these, the pocket is filled by a pocket factor and the protein structure is similar to virus-antiviral compound complexes. In the other conformation, the hydrophobic pocket is collapsed and empty. RNA bases stack against both a tryptophan and a phenylalanine residue on the internal surface of the viral capsid. Site-directed mutagenesis of the tryptophan, which is conserved across the picornaviruses, to nonconservative residues results in non-viable virus. Five symmetry-related N termini of coat protein VP4 form a ten-stranded, antiparallel beta barrel around the base of the icosahedral fivefold axis. The N termini of VP1 are amphipathic alpha helices, which stack on the outside of this beta barrel. The N termini of VP1 and VP4 have not been observed previously in rhinovirus structures. CONCLUSIONS: The observation of a partially occupied hydrophobic pocket in HRV16 forms a missing link between HRV14, which is always observed with no pocket factor in the native form, and rhinovirus 1A and other picornaviruses (e.g. poliovirus, coxsackievirus) which contain pocket factors. The pocket factor molecules probably regulate viral entry, uncoating and assembly. Picornavirus assembly is known to proceed via pentamers, therefore, the interaction of RNA with the conserved tryptophan residues across twofold axes between pentamers may play a role in picornavirus assembly. The positioning of a cation on the icosahedral fivefold axes and the structure of the N termini of VP4 and VP1 around these axes suggest a mechanism for the uncoating of rhinoviruses.

Amino Acid Sequence↗

PubMed1997

Enhanced DNA alkylation activities of Hoechst 33258 analogues designed for bioreductive activation.

A series of analogues of Hoechst 33258, designed to be subject to bioreductive activation, were synthesized, and interactions between these compounds and pBR322 DNA were investigated. Compounds containing a quinone group reacted with DNA via two possible pathways in the presence of reductants NADH or NADPH: radical cleavage and DNA alkylation. The corresponding dimethoxy compounds, which are not subject to reduction, showed very weak DNA binding ability. The strength of alkylation reaction of the quinone derivatives is related to leaving group ability. Furthermore, the quinone compounds preferentially alkylate DNA at 5'-CG and TG sequences rather than at the AT sites preferred as binding sites of Hoechst 33258.

Alkylation↗

PubMed1997

Camptothecin and minor-groove binder hybrid molecules: synthesis, inhibition of topoisomerase I, and anticancer cytotoxicity in vitro.

The synthesis, characterization, inhibitory activity against topoisomerase I, and biological evaluation of a series of 14 camptothecin derivatives of polypyrrolecarboxamide (lexitropsin) conjugates of two structural classes: (A) camptothecin-NHCO-lexitropsin 44-51 and (B) camptothecin-CONH-lexitropsin 38-43 are described. All 16 compounds tested, 14 conjugates plus two functionalized camptothecin controls, inhibit topoisomerase I in the concentration range 1.12-16.6 microM that divide into three distinct categories based on activity. The most active enzyme inhibitors belong to structure class A with either cationic dimethylaminium or neutral amide end groups. Generally class B conjugates are less effective in inhibiting topoisomerase I. Cytotoxic potencies of the drugs was tested against four representative human tumor cell lines: SKOV3, SKLVB, HT29, and KB. All 16 drugs gave measurable IC50 values against the KB cell line and fell into two categories with IC50 values of 0.049-0.66 microM (largely structure class B) and 1.0-48 microM (largely class A). Thus the class B conjugates, while less potent against the enzyme, contain two of the most potent drugs, 38 and 39, against KB cell lines. In contrast, in the case of the cell lines SKOV3 and HT29 there was a general correlation between the better topoisomerase inhibitors and their cell cytotoxicities.

Adenocarcinoma↗

PubMed1997

Cations in human rhinoviruses.

All known crystal structures of rhinoviruses have some uninterpreted electron density on their fivefold axes at a distance of about 152 +/- 3 A from the viral center. This density had been assumed to be a Ca2+ ion, based on its shape, height, and the presence of Ca2+ ions in the crystallization solutions. Difference electron density maps between EGTA-soaked crystals of human rhinovirus 14 (HRV14), as well as HRV16, and their corresponding native structures show that this density is an EGTA-chelatable ion. Analysis of the coordination geometry indicates that the ions in HRV3, HRV14, and HRV1A could be Ca2+ and the ion in HRV16 might be Zn2+. These cations may play a role in regulation of rhinovirus stability, although the loss of the ion itself does not seem sufficient to lead to viral disassembly.

Calcium↗

PubMed1997

[Comparison of plasma thyroxin and insulin concentrations between 10-day old layer and broiler chickens].

In this study both sexes of 10 day old layer and broiler chickens were used to investigate plasma circulating concentrations of 3,3'-5-triiodothyronine (T3), thyroxine (T4) and insulin by using the radioimmunoassay (RIA) methods. The results were as follows: serum T3 concentration was higher in broilers than that in layers (P < 0.01), especially a significant difference between male strains was seen in this experiment (P < 0.001), and the levels of plasma insulin was significantly higher in male broilers than that in male layers (P < 0.001), however, no clear differences in plasma T4 was seen between strains and sexes (P > 0.05). In addition, there were sex differences in T3 and insulin levels in layers, that is to say, those in the female layers was higher than those in the male layers, but no clear deifference was seen between sexes in broilers. A significant positive correlation between T3, insulin and their weight gained (P < 0.05). The results suggest that the levels of serum T3 and Insulin may influence the various growth rate during early posthatch development in layers and broilers.

Animals↗

PubMed1997

[Somatostatin and its secretory cells in tumor surrounding mucosa in colorectal cancer patients and its significance].

The somatostatin (SS) levels in tumor surrounding mucosae were determined by RIA, and the SS secretory cells in these tissues were observed by immunocytochemistry in colorectal cancer patients. The mean SS level was higher in cancer-adjacent mucosa (CAM, 0-2 cm from the tumor) than in cancer-distant mucosa (CDM, about 5 cm from the tumor), and in CAM without atypical hyperplasia than in such mucosa with different grades of atypical hyperplasia (P < 0.01). In CAMs, there was a very significant negative correlation between the SS level and cell dysplasia (P < 0.01). The form and location of SS cells in all tumor surrounding mucosae were similar to the normal. Both the mean SS cell number and total positive degree were very significantly higher in CAM than CDM (P < 0.01). SS levels in CAMs were correlated positively with the SS cell numbers and the total positive degrees in CAM (P < 0.01). It is concluded that the elevation of SS level in CAM is mainly caused by the increase of SS cells, which secrete more SS. The change of SS in colorectal cancer surrounding mucosa may play an important role in inhibiting the development of CAM atypical hyperplasia or the tumor, and is a local defensive reaction in the body.

Cell Count↗

PubMed1997

[In situ hybridization for interleukin 4 and interleukin 5 messenger RNA in asthma].

The actual mechanism by which a group of asthmatics were resistant to glucocorticoids therapy remains poorly understood. Previous in vitro studies suggested that the pattern of cytokine gene expression may play a role in determining steroid resistance. In the current study, we used the technique of mRNA in situ hybridization to examine whether peripheral blood mononuclear cells (PBMCs) from steroid-resistance (SR) asthmatics vs. Steroid-sensitive (SS) asthmatics expressed different patterns of cytokines, particularly after treatment with steroid. PBMCs from SR patients did not differ significantly from those of SS in terms of their number expressing Interleukin (IL)-4 mRNA and IL-5 mRNA (P > 0.05) by culture alone. There were no differences in the number of PBMCs expressing IL-4 mRNA and IL-5 mRNA (P > 0.05) between incubation in the absence and presence of dexamethasone (DXM, 10(-7) mol/L) in SR. SS patients had a significant dicrease in the number of PBMCs expressing IL-4 mRNA and IL-5 mRNA (P < 0.01) after culture in the presence of DXM as compared with incubation in media alone. Our findings indicate that SR asthma is associated with a dysregulation of the expression of the genes encoding for IL-4 and IL-5.

Adult↗

PubMed1997

[The effects of Gu Chi Gao on IL-8 in GCF of periodontitis].

In order to find a new treatment of periodontitis, this paper studied the effects of Gu Chi Gao on IL-8 in gingival crevicular fluid (GCF) of periodontitis. One tooth was selected from every patient in 24 patients with adult periodontitis. After supragingival scaling, the patients were divided into two groups randomly. One group was treated with Gu Chi Gao, while the other group was untreated as control group. All patients were examined after one month. GCF samples were collected with 2 mm x 20 mm Whatman I filter paper stripes and IL-8 in the GCF samples were detected by the method of ELISA. The result demonstrated that the levels of GCF and IL-8 in the treated group were lower than that of control group (P < 0.01), it suggests that Gu Chi Gao may inhibit the production of IL-8 and GCF.

Adult↗

PubMed1997

[The expression of IL-1 alpha gene in gingival tissue].

IL-1 is secreted by a variety of cells and plays an important role in the network of cytokines. In this study, the expression of IL-1 alpha in gingival tissue was determined with reverse transcription-polymerase chain reaction (RT-PCR). The PCR-product was confirmed by DNA sequencing. The results showed that IL-1 alpha transcription was detected in all 5 inflammatory gingival tissue samples, but it was not delected in the normal gingival tissue samples and in the samples after treatment. These findings suggested that IL-1 alpha may be a specific indicator of periodontal disease, and a potential mediator in pathogenesis of periodontitis.

Gene Expression↗

PubMed1997

[9-cis retinoic acid induces apoptosis in HL-60 cells].

OBJECTIVE: To investigate the apoptosis of HL-60 cells induced by 9-cis retinoic acid (9-cis RA), and illustrate the possible molecular mechanism. METHODS: Apoptosis was detected by morphological observation, DNA electrophoresis and flow cytometric cell cycle analysis. Bcl-2 expression was detected by flow cytometry. RESULTS: 9-cis RA initiated apoptosis of HL-60 cells after inducing them irreversibly commited to differentiation. Bcl-2 was downregulated during the differentiation and apoptosis process. 9-cis RA was more potent than all-trans retinoic acid (ATRA) did in inducing terminal differentiation associated apoptosis and in downregulation of Bcl-2 expression. CONCLUSION: 9-cis RA can induce apoptosis in HL-60 cells. Downregulation of Bcl-2 expression appears to play an important role in the apoptosis of the differentiated leukemic cells.

Alitretinoin↗

PubMed1997

[Scale-up preparation of hydrophobic interaction chromatographic packing materials based on inorganic matrix].

Based on inorganic matrix controlled pore glass (CPG) and macro-pore silica sphere, by using polyethylene glycol (PEG 1000) as a ligand, a preparation method of hydrophobic interaction chromatographic (HIC) packing material was improved by adding a proper catalyst during the bonding process. The packing material can be synthesized in a scale-up batch, for example 150g for each batch, both for analytical and preparative columns. The retention of proteins, such as cytochrome C (Cyt-C), chymotrypsingen-A (Chy-A), lysozyme (Lys) and ribonuclease(Rnase), is increased with the increasing of (NH4)2SO4 concentration in the eluant 2.5 mol/L of salt concentration for the mobile phase was chosen by considering the separation efficiency and equipment life. After comparing the effect of pH for the retention of proteins it is found that the proteins are well separated at pH 7. The time of linear gradient elution program was optimized in considering the separation efficiency and speed. It is better to take 30 minutes of the gradient program for the separation. Six standard proteins can be well separated with the high-performance HIC column in the linear gradient elution program from 2.5 to 0 mol/L of (NH4)2SO4 in 50 mmol/L of phosphate buffer solution within 30 minutes. Cyt-C, Rnase, Lys and Chy-A can be separated by the HIC column based on CPG matrix. Six proteins, Cyt-C, Rnase, Lys, Chy-A, insulin(Ins) and lipase (Lip) can be well separated on the column based on silica matrix with gradient elution program. The recovery of trypsin detected with BAEE method is over 95% after purification with the HIC column.

Chromatography↗

PubMed1997

[A gas chromatographic method for determination of Butyraldehyde as a product of butanol biotransformation in rat liver].

Analysis of butyraldehyde obtained by the interaction of butanol with cytochrome P450 II E1 in rat liver microsomes prepared by centrifugation and with the NADPH added is described in this paper. The biotransformation rate of butanol into butyraldehyde can be used as an index for the assessment of the enzyme activity of cytochrome P450 II E1. A headspace gas chromatograghic method to determine the butyraldehyde has been developed. The detection limit and CV of this method for butyraldehyde in microsomes were 0.7 micromol/L and 8.1%-9.3% respectively. The recovery was 85.3%. The results show that this is a rapid and sensitive method with less interferences and fairly good precision. The method developed has made a reliable analytical methodological foundation for the assessment of the enzyme activity of cytochrome P450 II E1.

Aldehydes↗