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1.
J Obstet Gynaecol Res ; 49(6): 1514-1524, 2023 Jun.
Article in English | MEDLINE | ID: mdl-36895137

ABSTRACT

BACKGROUND: Abnormalities of the fetal cardiovascular system caused by fetal growth restriction (FGR) may lead to adverse outcomes. The fetal cardiac function assessment is of great significance for treatment selection and prognostic evaluation of fetuses with FGR. OBJECTIVE: This study aimed to explore the value of fetal HQ analysis based on speckle tracking imaging (STI) to evaluate the global and regional cardiac function of fetuses with early-onset or late-onset FGR. METHODS: From June 2020 to November 2022, 30 pregnant women with early-onset FGR (21-38 gestational weeks) and 30 pregnant women with late-onset FGR (21-38 gestational weeks) in the Department of Ultrasound, Shandong Maternal and Child Health Hospital were enrolled. Also, 60 healthy volunteer pregnant women were enrolled as two control groups according to the principle of matching gestational weeks (21-38 gestational weeks). The fetal cardiac functions, including fetal cardiac global spherical index (GSI), left ventricular ejection fraction (LVEF), fractional area change (FAC) of both ventricles, global longitudinal strain (GLS) of both ventricles, 24-segmental fractional shortening (FS), 24-segmental end-diastolic ventricular diameter (EDD), and 24-segmental spherical index (SI), were assessed using fetal HQ. The standard biological values of fetuses and Doppler blood flow parameters of fetuses and mothers were measured. The estimated fetal weight (EFW) measured by the last prenatal ultrasound was calculated, and the weights of newborns were followed up. RESULTS: Among early FGR, late FGR and total control group, significant differences were found in global cardiac indexes of right ventricle (RV), left ventricle (LV) and GSI. For the segmental cardiac indexes, there are significant differences in three groups except parameter of LVSI. Compared with the control group at the same gestational week, the Doppler indexes including MCAPI and CPR in both the early-onset FGR group and the late-onset FGR group were significantly different. The intra- and inter-observer correlation coefficients of RV FAC, LV FAC, RV GLS, and LV GLS were good. Further, the intra- and inter-observer variability in FAC and GLS was small, as analyzed using the Bland-Altman scatter plot. CONCLUSIONS: Fetal HQ software based on STI showed that FGR affected the global and segmental cardiac function of both ventricles. FGR no matter early-onset or late-onset altered Doppler indexes significantly. The FAC and the GLS had satisfactory repeatability in evaluating fetal cardiac function.


Subject(s)
Fetal Growth Retardation , Fetal Heart , Child , Infant, Newborn , Pregnancy , Female , Humans , Fetal Growth Retardation/diagnostic imaging , Stroke Volume , Fetal Heart/diagnostic imaging , Ventricular Function, Left , Prenatal Care , Ultrasonography, Prenatal/methods
2.
Int J Clin Pharmacol Ther ; 60(4): 188-191, 2022 Apr.
Article in English | MEDLINE | ID: mdl-34889734

ABSTRACT

Dexmedetomidine-related polyuria has been observed in animal experimental studies, while only limited cases have been reported in humans. Thus, this rare effect is not well recognized. Herein, we report the case of a 26-year-old man who underwent total thyroidectomy and experienced intraoperative dexmedetomidine-related polyuria, which was subsequently resolved using pituitrin. Moreover, we review the current literature on dexmedetomidine-related polyuria and analyze the potential mechanisms of this rare effect.


Subject(s)
Dexmedetomidine , Animals , Dexmedetomidine/adverse effects , Humans , Polyuria/chemically induced , Thyroidectomy
3.
Nature ; 528(7580): 108-10, 2015 Dec 03.
Article in English | MEDLINE | ID: mdl-26605521

ABSTRACT

The formation of relativistic jets by an accreting compact object is one of the fundamental mysteries of astrophysics. Although the theory is poorly understood, observations of relativistic jets from systems known as microquasars (compact binary stars) have led to a well established phenomenology. Relativistic jets are not expected to be produced by sources with soft or supersoft X-ray spectra, although two such systems are known to produce relatively low-velocity bipolar outflows. Here we report the optical spectra of an ultraluminous supersoft X-ray source (ULS) in the nearby galaxy M81 (M81 ULS-1; refs 9, 10). Unexpectedly, the spectra show blueshifted, broad Hα emission lines, characteristic of baryonic jets with relativistic speeds. These time-variable emission lines have projected velocities of about 17 per cent of the speed of light, and seem to be similar to those from the prototype microquasar SS 433 (refs 11, 12). Such relativistic jets are not expected to be launched from white dwarfs, and an origin from a black hole or a neutron star is hard to reconcile with the persistence of M81 ULS-1's soft X-rays. Thus the unexpected presence of relativistic jets in a ULS challenges canonical theories of jet formation, but might be explained by a long-speculated, supercritically accreting black hole with optically thick outflows.

4.
Chem Biodivers ; 18(4): e2001012, 2021 Apr.
Article in English | MEDLINE | ID: mdl-33644937

ABSTRACT

Chemical investigation of the ethanol extract of the branch and leaves of Illicium majus resulted in the isolation of four new phenylpropanoid glycosides (1-4) and one new phenolic glycoside (9), along with 13 known ones. Spectroscopic techniques were used to elucidate the structures of the new isolates such as 3-[(2R,3S)-7-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-3-(hydroxymethyl)-2,3-dihydro-1-benzofuran-5-yl]propyl ß-D-glucopyranoside (1), [(2R,3S)-7-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-5-(3-hydroxypropyl)-2,3-dihydro-1-benzofuran-3-yl]methyl 2-O-α-L-rhamnopyranosyl-ß-D-glucopyranoside (2), [(2R,3S)-7-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-5-(3-hydroxypropyl)-2,3-dihydro-1-benzofuran-3-yl]methyl 2-O-α-L-rhamnopyranosyl-ß-D-xylopyranoside (3), 3-[(2R,3S)-3-({[2-O-(4-O-acetyl-α-L-rhamnopyranosyl)-ß-D-xylopyranosyl]oxy}methyl)-7-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-2,3-dihydro-1-benzofuran-5-yl]propyl acetate (4), and 4-(2-hydroxyethyl)phenyl 3-O-ß-D-glucopyranosyl-ß-D-glucopyranoside (9). Free radical scavenging activities of the isolates were elucidated through the DPPH assay method. The most active compounds, 1-O-caffeoyl-ß-D-glucopyranose (17) and soulieana acid 1 (18), exhibited moderate radical scavenging activities (IC50 =37.7±4.4 µM and IC50 =97.2±3.4 µM, respectively). The antibacterial activities of the isolates against Staphylococcus aureus and Escherichia coli were also assessed, and no activity was shown at the measured concentration (<32 µg/mL).


Subject(s)
Anti-Bacterial Agents/pharmacology , Antioxidants/pharmacology , Glycosides/pharmacology , Illicium/chemistry , Propanols/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/isolation & purification , Antioxidants/chemistry , Antioxidants/isolation & purification , Biphenyl Compounds/antagonists & inhibitors , Dose-Response Relationship, Drug , Escherichia coli/drug effects , Glycosides/chemistry , Glycosides/isolation & purification , Microbial Sensitivity Tests , Molecular Structure , Picrates/antagonists & inhibitors , Propanols/chemistry , Propanols/isolation & purification , Staphylococcus aureus/drug effects
5.
Nature ; 503(7477): 500-3, 2013 Nov 28.
Article in English | MEDLINE | ID: mdl-24284727

ABSTRACT

There are two proposed explanations for ultraluminous X-ray sources (ULXs) with luminosities in excess of 10(39) erg s(-1). They could be intermediate-mass black holes (more than 100-1,000 solar masses, M sun symbol) radiating at sub-maximal (sub-Eddington) rates, as in Galactic black-hole X-ray binaries but with larger, cooler accretion disks. Alternatively, they could be stellar-mass black holes radiating at Eddington or super-Eddington rates. On its discovery, M 101 ULX-1 had a luminosity of 3 × 10(39) erg s(-1) and a supersoft thermal disk spectrum with an exceptionally low temperature--uncomplicated by photons energized by a corona of hot electrons--more consistent with the expected appearance of an accreting intermediate-mass black hole. Here we report optical spectroscopic monitoring of M 101 ULX-1. We confirm the previous suggestion that the system contains a Wolf-Rayet star, and reveal that the orbital period is 8.2 days. The black hole has a minimum mass of 5 M sun symbol, and more probably a mass of 20 M sun symbol-30 M sun symbol, but we argue that it is very unlikely to be an intermediate-mass black hole. Therefore, its exceptionally soft spectra at high Eddington ratios violate the expectations for accretion onto stellar-mass black holes. Accretion must occur from captured stellar wind, which has hitherto been thought to be so inefficient that it could not power an ultraluminous source.

6.
Zhonghua Nan Ke Xue ; 25(9): 843-847, 2019 Sep.
Article in Zh | MEDLINE | ID: mdl-32233214

ABSTRACT

Spermatogenesis and sperm maturation are closely related to temperature and require a temperature slightly lower than the normal body temperature. Therefore, high temperature is an important external factor affecting sperm function, and the studies on the underlying mechanisms are of great significance for the treatment of male infertility, improvement of in vitro sperm preservation and further elucidation of spermatogenesis and sperm maturation. It is known currently that the influence of high temperature on sperm involves genetic material, morphology, survival rate, motility and fertility, most of which have been found in various species and may be attributed to the conserved common process or common substances in spermatogenesis and maturation. An overwhelming majority of the influencing factors produce negative effects and a very few have positive ones, and their action mechanisms are mostly unknown. This review summarizes the results of current studies on the effect of high temperature on spermatogenesis and sperm maturation and on the sperm function in various species.


Subject(s)
Hot Temperature , Infertility, Male , Spermatogenesis , Spermatozoa/pathology , Animals , Humans , Male
7.
Sichuan Da Xue Xue Bao Yi Xue Ban ; 49(2): 163-168, 2018 Mar.
Article in Zh | MEDLINE | ID: mdl-29737053

ABSTRACT

The 21th century is the century of exploring and utilizing the underground space. In the future, more and more people will spend more and more time living or/and working in the underground space. However,we know little about the effect on the health of human caused by the underground environment. Herein,we systematically put forward the strategic conception of the deep-underground medicine,in order to reveal relative effects and mechanism of the potential factors in the deep underground space on human's physiological and psychological healthy,and to work out the corresponding countermeasures. The original deep-underground medicine includes the following items. ①To model different depth of underground environment according to various parameters (such as temperature,radiation,air pressure, rock,microorganism), and to explore their quantitative character and effects on human health and mechanism. ② To study the psychological change, maintenance of homeostasis and biothythm of organism in the deep underground space. ③ To learn the association between psychological healthy of human and the depth, structure, physical environment and working time of underground space. ④ To investigate the effect of different terrane and lithology on healthy of human and to deliberate their contribution on organism growth. ⑤ To research the character and their mechanism of growth,metabolism,exchange of energy,response of growth, aging and adaptation of cells living in deep underground space. ⑥ To explore the physiological feature,growth of microbiome and it's interaction with host in the deep underground space. ⑦ To develop deep-underground simulation space, the biologically medical technology and equipments. As a research basis,a deep-underground medical lab under a rock thickness of about 1 470 m has been built,which aims to operate the research of the effect on living organism caused by different depth of underground environment.


Subject(s)
Biomedical Research/trends , Confined Spaces , Humans
8.
Molecules ; 22(9)2017 Sep 05.
Article in English | MEDLINE | ID: mdl-28872607

ABSTRACT

A series of sulfanilamide-1,2,3-triazole hybrids were designed by a molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, MCF-7 and PC-3). The detailed structure-activity relationships for these sulfanilamide-1,2,3-triazole hybrids were investigated. All these sulfanilamide-1,2,3-triazole hybrids exhibited moderate to potent activity against all cell lines. In particular 4-methyl-N-((1-(3-phenoxybenzyl)-1H-1,2,3-triazol-4-yl)methyl)benzenesulfonamide (11f) showed the most potent inhibitory effect against PC-3 cells, with an IC50 value of 4.08 µM. Furthermore, the tubulin polymerization inhibitory activity in vitro of compound 11f was 2.41 µM. These sulfanilamide hybrids might serve as bioactive fragments for developing more potent antiproliferative agents.


Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Cell Proliferation/drug effects , Sulfanilamides/chemical synthesis , Sulfanilamides/pharmacology , Tubulin Modulators/chemical synthesis , Tubulin Modulators/pharmacology , Antineoplastic Agents/administration & dosage , Cell Line, Tumor , Drug Design , Drug Screening Assays, Antitumor , Humans , Structure-Activity Relationship , Sulfanilamides/administration & dosage , Triazoles/administration & dosage , Triazoles/chemical synthesis , Triazoles/pharmacology , Tubulin/metabolism , Tubulin Modulators/administration & dosage
9.
Am J Physiol Lung Cell Mol Physiol ; 311(3): L581-9, 2016 09 01.
Article in English | MEDLINE | ID: mdl-27448664

ABSTRACT

Dendritic cells and CD8(+) T cells participate in the pathology of chronic obstructive pulmonary disease, including emphysema, but little is known of the involvement of the CD40/CD40L pathway. We investigated the role of the CD40/CD40L pathway in Tc1 cell differentiation induced by dendritic cells in a mouse model of emphysema, and in vitro. C57BL/6J wild-type and CD40(-/-) mice were exposed to cigarette smoke (CS) or not (control), for 24 wk. In vitro experiments involved wild-type and CD40(-/-) dendritic cells treated with CS extract (CSE) or not. Compared with the control groups, the CS mice (both wild type and CD40(-/-)) had a greater percentage of lung dendritic cells and higher levels of major histocompatability complex (MHC) class I molecules and costimulatory molecules CD40 and CD80. Relative to the CS CD40(-/-) mice, the CS wild type showed greater signs of lung damage and Tc1 cell differentiation. In vitro, the CSE-treated wild-type cells evidenced more cytokine release (IL-12/p70) and Tc1 cell differentiation than did the CSE-treated CD40(-/-) cells. Exposure to cigarette smoke increases the percentage of lung dendritic cells and promotes Tc1 cell differentiation via the CD40/CD40L pathway. Blocking the CD40/CD40L pathway may suppress development of emphysema in mice exposed to cigarette smoke.


Subject(s)
CD40 Antigens/physiology , CD40 Ligand/physiology , Dendritic Cells/physiology , Pulmonary Emphysema/immunology , Smoke/adverse effects , Animals , CD8-Positive T-Lymphocytes , Cell Differentiation , Cells, Cultured , Cytokines/biosynthesis , Cytokines/genetics , Lung/immunology , Lung/metabolism , Lung/pathology , Lymphocyte Count , Mice, Inbred C57BL , Mice, Knockout , Pulmonary Emphysema/etiology , Pulmonary Emphysema/metabolism , Signal Transduction , Smoking/adverse effects , T-Box Domain Proteins/genetics , T-Box Domain Proteins/metabolism , Nicotiana/adverse effects
10.
Zhonghua Nan Ke Xue ; 21(8): 708-12, 2015 Aug.
Article in Zh | MEDLINE | ID: mdl-26442297

ABSTRACT

OBJECTIVE: To explore the correlation of the gene polymorphisms of Toll-like receptor 2 ( TLR2) and TLR4 with the susceptibility and recurrence of condyloma acuminatum (CA). METHODS: Using Snapshot, we detected the gene polymorphisms of TLR2 597(T/C), 1350(T/C), 15607(A/G), and 2258(G/A) and TLR4 896(A/G) and 1196(C/T) in the peripheral blood of 140 CA patients and 105 HPV-negative controls. We made comparisons between the CA patients and controls as well as between the cases of recurrent CA and those of non-recurrence at 6 months after treatment. RESULTS: There were 72, 48, and 20 cases of genotype TT, TC, and CC of TLR2 597 (T/C), respectively, in the CA patients, as compared with 71, 31, and 3 cases in the controls. The gene frequency of mutant C was 31. 43% in the patients, significantly higher than 17.62% in the controls (χ2 = 12.04, P < 0.01), and it was 38.68% in the recurrent cases, remarkably higher than 27.01% in the non-recurrent cases (χ2 = 4.16, P < 0.05). There were 74, 49, and 17 cases of genotype TT, TC, and CC of TLR2 1350( T/C), respectively, in the CA patients, as compared with 73, 29, and 3 cases in the controls. The gene frequency of mutant C was 29. 64% in the patients, significantly higher than 16. 67% in the controls (χ2 =11.05, P < 0.01), and it was 36.79% in the recurrent cases, markedly higher than 25. 29% in the non-recurrent cases (χ2 = 4.18, P < 0.05). There were 44, 66, and 30 cases of genotype AA, AG, and GG of TLR2 15607(A/G), respectively, in the CA patients, as compared with 26, 58, and 21 cases in the controls. There was no significant difference in the gene frequencies of mutant G between the two groups (χ2 = 0.33, P > 0.05). No mutant genes of TLR2 2508 (G/A) or TLR4 896(A/G) and 1196(C/ T) were detected in either the CA patients or the controls. Linkage disequilibrium analysis showed a tight linkage between TLR2 597 (T/C) and 1350(T/C) (D' = 1, r2 = 0.93). CONCLUSION: TLR2 597(T/C) is tightly linked to 1350(T/C), which is correlated with both the susceptibility and the recurrence of condyloma acuminatum.


Subject(s)
Condylomata Acuminata/genetics , Gene Frequency , Polymorphism, Genetic , Toll-Like Receptor 2/genetics , Toll-Like Receptor 4/genetics , Aged , Case-Control Studies , Genetic Linkage , Genetic Predisposition to Disease , Genotype , Humans , Recurrence
11.
J Craniofac Surg ; 24(5): 1526-9, 2013 Sep.
Article in English | MEDLINE | ID: mdl-24036719

ABSTRACT

OBJECTIVE: To study the effectiveness and safety of acellular dermal matrix (ADM) graft in preventing Frey syndrome after parotid neoplasm surgery, we reviewed foreign reported clinical randomized controlled trials systematically. Based on this review, we aimed to assess the effectiveness of ADM graft and provide reliable evidence for clinical application. METHODS: We reviewed foreign-language databases, such as MEDLINE, applied meta-analysis with Rev.Man 5, and drew forest plots with odds ratio as effect size. RESULTS: Three trials were recruited. The morbidity of Frey syndrome in experimental group was significantly lower than that in control on both subjective index and objective index, with odds ratios at 0.03 (95% confidence interval, 0.01-0.11) and 0.03 (95% confidence interval, 0.01-0.12), respectively. There was no significant difference between ADM group and blank control in total adverse reactions and complication incidence, whereas results differed for a kind of specific adverse reaction or complication. CONCLUSIONS: Based on existing research data, implanting ADM could effectively prevent Frey syndrome, and its poor prognosis effects did not significantly increase, which suggested that its total safety was reliable. Nevertheless, further investigations about the difference on a specific adverse reaction or complication were still needed.


Subject(s)
Acellular Dermis , Parotid Neoplasms/surgery , Skin Transplantation/methods , Sweating, Gustatory/prevention & control , Humans , Postoperative Complications/prevention & control , Treatment Outcome
12.
Molecules ; 18(10): 11866-72, 2013 Sep 26.
Article in English | MEDLINE | ID: mdl-24077171

ABSTRACT

Two new monoterpenes, p-mentha-1(7),8-dien-2-O-ß-D-glucoside and trans-2,4-dihydroxy-2,4-dimethyl-trans-1-acetic acid γ-lactone were isolated from the fruits of Illicium lanceolatum along with trans-2,4-dihydroxy-2,4-dimethyl-cis-1-acetic acid γ-lactone, (1R,2R,4R)-8-p-menthen-1,2-diol, trans-sobrerol, (1S,2S,4R)-p-menthane-1,2,8-triol and (1S, 2S, 4R, 8R)-p-menthane-1,2,9-triol. The structures of the isolates were confirmed by spectroscopic analysis and they showed no inhibitory effects on the in vitro growth of microbial organisms (Escherichia coli, Staphyloccocus aureus, Bacillus subtilis) at less than 1.0 mg/mL.


Subject(s)
Fruit/chemistry , Illicium/chemistry , Monoterpenes/chemistry , Plant Extracts/chemistry , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/pharmacology , Bacillus subtilis/drug effects , Escherichia coli/drug effects , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Models, Chemical , Models, Molecular , Molecular Conformation , Molecular Weight , Monoterpenes/isolation & purification , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Spectrometry, Mass, Electrospray Ionization , Staphylococcus aureus/drug effects
13.
Zhonghua Yi Xue Za Zhi ; 93(2): 123-7, 2013 Jan 08.
Article in Zh | MEDLINE | ID: mdl-23648349

ABSTRACT

OBJECTIVE: To determine the impact on tyrosinase expression and export from endoplasmic reticulum by inhibition of 26S proteasome. METHODS: Western blot was used to detect 26S proteasome from 8 vitiligo patients and 4 healthy controls. Melanocytes were incubated with proteasome inhibitor (lactacystin) and further detected as follows: cell survival by MTT assay, proteasome activity with fluorescence, ultrastructure observation with electron microscope, co-localization of tyrosinase and calreticulin (endoplasmic reticulum marker) by confocal laser scanning microscopy and 26S proteasome and tyrosinase with Western blot. RESULTS: The 26S proteasome expression level from lesions of vitiligo (1.05 ± 0.40) was significantly lower than the donor sites (1.82 ± 0.88) and the healthy controls (1.88 ± 0.16) (P < 0.05). But no significant difference existed between the latter two groups (P > 0.05). Compared to the untreated group, a 12-h incubation of 10 µmol/L lactacystin showed inhibitory effects on melanocytes (0.999 ± 0.110 vs 1.372 ± 0.127, P < 0.05) and significantly decreased proteasome activity (0.234 ± 0.019 vs 1, P < 0.01). Expansion rate of endoplasmic reticulum in the lactacystin group (1.91 ± 0.17) was significantly higher than that of the untreated cells (1.17 ± 0.11) (P < 0.05). More tyrosinase co-localized with calreticulin in endoplasmic reticulum in lactacystin-treated cells was observed than that of the untreated group. Compared with the untreated group, significantly decreased levels of tyrosinase (146 ± 10 vs 269 ± 8, P < 0.01) and tyrosinase activity (0.159 ± 0.017 vs 0.221 ± 0.019, P < 0.01) were shown in the lactacystin group (P < 0.05). CONCLUSIONS: Significantly decrease of 26S proteasome is found in lesions of vitiligo patients. Inhibition of 26S proteasome may lead to expansion of endoplasmic reticulum of melanocytes, impact export of tyrosinase from melanocyte endoplasmic reticulum and expression of tyrosinase.


Subject(s)
Acetylcysteine/analogs & derivatives , Endoplasmic Reticulum/metabolism , Melanocytes/drug effects , Melanocytes/metabolism , Monophenol Monooxygenase/metabolism , Proteasome Endopeptidase Complex/metabolism , Acetylcysteine/pharmacology , Adult , Case-Control Studies , Cells, Cultured , Cysteine Proteinase Inhibitors/pharmacology , Female , Humans , Male , Melanocytes/cytology , Vitiligo/metabolism , Vitiligo/pathology , Young Adult
14.
Bioorg Med Chem Lett ; 22(5): 2015-9, 2012 Mar 01.
Article in English | MEDLINE | ID: mdl-22335895

ABSTRACT

Haspin is a serine/threonine kinase that phosphorylates Thr-3 of histone H3 in mitosis that has emerged as a possible cancer therapeutic target. High throughput screening of approximately 140,000 compounds identified the beta-carbolines harmine and harmol as moderately potent haspin kinase inhibitors. Based on information obtained from a structure-activity relationship study previously conducted for an acridine series of haspin inhibitors in conjunction with in silico docking using a recently disclosed crystal structure of the kinase, harmine analogs were designed that resulted in significantly increased haspin kinase inhibitory potency. The harmine derivatives also demonstrated less activity towards DYRK2 compared to the acridine series. In vitro mouse liver microsome stability and kinase profiling of a representative member of the harmine series (42, LDN-211898) are also presented.


Subject(s)
Carbolines/chemistry , Carbolines/pharmacology , Intracellular Signaling Peptides and Proteins/antagonists & inhibitors , Protein Kinase Inhibitors/chemistry , Protein Kinase Inhibitors/pharmacology , Protein Serine-Threonine Kinases/antagonists & inhibitors , Animals , Carbolines/metabolism , Humans , Intracellular Signaling Peptides and Proteins/metabolism , Mice , Microsomes, Liver/metabolism , Models, Molecular , Protein Kinase Inhibitors/metabolism , Protein Serine-Threonine Kinases/metabolism , Protein-Tyrosine Kinases/antagonists & inhibitors , Protein-Tyrosine Kinases/metabolism , Structure-Activity Relationship , Dyrk Kinases
15.
Yi Chuan ; 34(10): 1298-303, 2012 Oct.
Article in Zh | MEDLINE | ID: mdl-23099786

ABSTRACT

Neutrophils provide the first line of defense against invading pathogens and have been reported to play a key role in bovine mammary immune. To examine the differential expression of proteins in neutrophils between clinical mastitis and healthy dairy cows, a 2-dimensional electrophoresis gel map with high repeatability was constructed for bovine neutrophils. From this map, seven differentially expressed proteins were identified by MALDI-TOF MS which are believed to be involved in pathways such as cell metabolism, oxidative stress, and inflammatory reaction. The differentially expressed proteins identified in this study may provide the basis for bovine mastitis resistance breeding research.


Subject(s)
Blood Proteins/analysis , Mastitis, Bovine/blood , Neutrophils/chemistry , Animals , Cattle , Electrophoresis, Gel, Two-Dimensional , Female , Proteomics , Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
16.
Zhonghua Jie He He Hu Xi Za Zhi ; 35(11): 824-7, 2012 Nov.
Article in Zh | MEDLINE | ID: mdl-23290037

ABSTRACT

OBJECTIVE: To investigate the impact of treatment with low dose roxithromycin on clinical symptoms and CT scores in patients with stable bronchiectasis. METHODS: Fifty patients with bronchiectasis in stable condition were randomly assigned to a control group and a treatment group. Patients in the control group received ambroxol hydrochloride tablet 90 mg 3 times a day. Patients in the treatment group received roxithromycin disperse tablet 0.15 g every day and ambroxol hydrochloride tablet 90 mg 3 times a day. The course of treatment lasted for 6 months. Quality of life was assessed using St. George's respiratory questionnaire (SGRQ). The British Medical Research Council (MRC) dyspnea scale was used to assess the degree of dyspnea. The score for CT evaluation of the thorax, quality of life and SGRQ were performed for all patients before and after the treatment. RESULTS: After 6 months, the scores for quality of life (48 ± 13) were lower compared to that (58 ± 15) before treatment in the control group; however, the scores for bronchial wall thickening of bronchiectasis (1.8 ± 0.5) were higher than that (1.8 ± 0.4) before study. The scores for the extent of bronchiectasis (2.7 ± 1.6), the bronchial wall thickening of bronchiectasis (1.3 ± 0.4) and the global CT score (6.7 ± 2.5) were reduced after treatment as compared to those before treatment [(4.8 ± 2.3), (1.8 ± 0.5), (9.5 ± 3.3)] in the treatment group, (all P < 0.01). The degree of dyspnea (1.3 ± 0.4) and quality of life (42 ± 12) were lower than those before treatment [(1.89 ± 0.45), (56 ± 15)] in the treatment group. Furthermore, the scores for extent of bronchiectasis (2.7 ± 1.6), the scores for the bronchial wall thickening of bronchiectasis (1.3 ± 0.4) and the global CT score (6.7 ± 2.5) in the treatment group were significantly improved as compared with those [(4.8 ± 2.0), (1.8 ± 0.5), (9.7 ± 3.6)] in the control group respectively after treatment. At the same time, the degree of dyspnea (1.3 ± 0.4) in the treatment group was significantly improved as compared with that (1.7 ± 0.4) in the control group after treatment. CONCLUSIONS: The scores for the bronchial wall thickening of bronchiectasis were increased in patients with stable bronchiectasis. Low dose roxithromycin combined with ambroxol hydrochloride significantly improved degree of dyspnea, reduced scores for extent of bronchiectasis, scores for the bronchial wall thickening of bronchiectasis and the global CT score as compared to treatment with ambroxol hydrochloride alone in patients with bronchiectasis in stable condition.


Subject(s)
Anti-Bacterial Agents/administration & dosage , Bronchiectasis/drug therapy , Roxithromycin/administration & dosage , Adult , Aged , Ambroxol/administration & dosage , Ambroxol/therapeutic use , Anti-Bacterial Agents/therapeutic use , Bronchi/drug effects , Bronchi/pathology , Dyspnea/drug therapy , Female , Humans , Male , Middle Aged , Quality of Life , Roxithromycin/therapeutic use
17.
Chem Biodivers ; 8(4): 692-8, 2011 Apr.
Article in English | MEDLINE | ID: mdl-21480515

ABSTRACT

Two new lignans, dihydrodehydrodiconiferyl alcohol 9-O-ß-D-(3″-O-acetyl)-xylopyranoside (1) and threo-4,9,9'-trihydroxy-3,3'-dimethoxy-8-O-4'-neolignan 7-O-α-rhamnopyranoside (2) were isolated from Illicium henryi, together with ten known compounds, 3-12. Their structures were elucidated by extensive spectroscopic analyses. The anti-hepatitis B virus (anti-HBV) activity of compounds 1-12 inhibiting HBV surface antigen (HBsAg) and HBV e antigen (HBeAg) secretion on Hep G2.2.15 cell line was evaluated. (-)-Dihydrodehydrodiconiferyl alcohol (4) showed moderate inhibitory activity on both HBsAg and HBeAg secretion with IC(50) values of 0.06 and 0.53 mM, respectively.


Subject(s)
Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Hepatitis B virus/drug effects , Hepatitis B/drug therapy , Illicium/chemistry , Lignans/chemistry , Lignans/pharmacology , Antiviral Agents/isolation & purification , Hep G2 Cells , Humans , Lignans/isolation & purification , Molecular Structure , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Extracts/pharmacology
18.
Bioorg Med Chem Lett ; 20(12): 3491-4, 2010 Jun 15.
Article in English | MEDLINE | ID: mdl-20836251

ABSTRACT

Haspin is a serine/threonine kinase required for completion of normal mitosis that is highly expressed during cell proliferation, including in a number of neoplasms. Consequently, it has emerged as a potential therapeutic target in oncology. A high throughput screen of approximately 140,000 compounds identified an acridine analog as a potent haspin kinase inhibitor. Profiling against a panel of 270 kinases revealed that the compound also exhibited potent inhibitory activity for DYRK2, another serine/threonine kinase. An optimization study of the acridine series revealed that the structure-activity relationship (SAR) of the acridine series for haspin and DYRK2 inhibition had many similarities. However, several structural differences were noted that allowed generation of a potent haspin kinase inhibitor (33, IC50 <60 nM) with 180-fold selectivity over DYRK2. In addition, a moderately potent DYRK2 inhibitor (41, IC50 <400 nM) with a 5.4-fold selectivity over haspin was also identified.


Subject(s)
Acridines/pharmacology , Intracellular Signaling Peptides and Proteins/antagonists & inhibitors , Protein Serine-Threonine Kinases/antagonists & inhibitors , Protein-Tyrosine Kinases/antagonists & inhibitors , Acridines/chemical synthesis , Humans , Inhibitory Concentration 50 , Protein Kinase Inhibitors/chemical synthesis , Protein Kinase Inhibitors/chemistry , Structure-Activity Relationship , Dyrk Kinases
19.
Planta Med ; 76(2): 152-8, 2010 Feb.
Article in English | MEDLINE | ID: mdl-19670158

ABSTRACT

Five new sesquiterpene lactones, henrylactones A-E ( 1- 5), together with ten known compounds: cycloparvifloralone ( 6), tashironin ( 7), tashironin A ( 8), neoanisatin ( 9), anisatin ( 10), anislactone B ( 11), 7- O-acetylanislactone B ( 12), merrillianolide ( 13), cyclomerrillianolide ( 14) and pseudomajucin ( 15), were isolated from the stems and roots of ILLICIUM HENRYI. Their structures were elucidated based on extensive spectroscopic data analyses. Among them, henrylactone A ( 1) is a novel sesquiterpene with a dilactone moiety and its structure was confirmed by X-ray diffraction. Sesquiterpene lactones 1- 15 were tested for their anti-hepatitis B virus (HBV) activities. The most active compound, tashironin ( 7), exhibited an IC (50) value of 0.48 mM (SI = 6.3) inhibiting on HBV surface antigen (HBsAg) secretion and an IC (50) value of 0.15 mM (SI = 20.1) inhibiting on HBV e antigen (HBeAg) secretion using HBV transfected Hep G2.2.15 cell line.


Subject(s)
Antiviral Agents/isolation & purification , Hepatitis B virus/drug effects , Hepatitis B/drug therapy , Illicium/chemistry , Plant Extracts/chemistry , Antiviral Agents/pharmacology , Antiviral Agents/therapeutic use , Hep G2 Cells , Hepatitis B Surface Antigens/metabolism , Hepatitis B e Antigens/metabolism , Humans , Lactones/isolation & purification , Lactones/pharmacology , Lactones/therapeutic use , Molecular Structure , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Plant Roots , Plant Stems , Sesquiterpenes/isolation & purification , Sesquiterpenes/pharmacology , Sesquiterpenes/therapeutic use
20.
Planta Med ; 76(13): 1464-7, 2010 Sep.
Article in English | MEDLINE | ID: mdl-20195962

ABSTRACT

Bioassay-guided fractionation of the ethanol extract of the leaves and stems of Illicium simonsii led to the isolation of two new compounds, simonin A (1) and 1-hydroxyl-2- O- ß- D-6'-acetyl-glucopyranosyl-4-allylbenzene (2), along with eight known compounds. Their structures were elucidated by spectroscopic analysis. The isolates were tested for anti-oral microbial activity using a microdilution method. Compounds 1 and 3- 6 showed significant activities against oral microbial organisms (Actinomyces viscosus, Streptococcus mutans, Streptococcus sanguis, and Actinomyces naeslundii), with minimum inhibitory concentration (MIC) values ranging from 1.95 to 31.25 µg/mL in vitro.


Subject(s)
Allyl Compounds/isolation & purification , Anti-Bacterial Agents/isolation & purification , Bacteria/drug effects , Glucosides/isolation & purification , Illicium/chemistry , Mouth/microbiology , Plant Extracts/chemistry , Xanthenes/isolation & purification , Allyl Compounds/pharmacology , Anti-Bacterial Agents/pharmacology , Glucosides/pharmacology , Microbial Sensitivity Tests , Molecular Structure , Plant Extracts/pharmacology , Plant Leaves , Plant Stems , Propanols/isolation & purification , Propanols/pharmacology , Xanthenes/pharmacology
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