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1.
Proc Natl Acad Sci U S A ; 121(12): e2320232121, 2024 Mar 19.
Article in English | MEDLINE | ID: mdl-38478684

ABSTRACT

The chemisorption energy of reactants on a catalyst surface, [Formula: see text], is among the most informative characteristics of understanding and pinpointing the optimal catalyst. The intrinsic complexity of catalyst surfaces and chemisorption reactions presents significant difficulties in identifying the pivotal physical quantities determining [Formula: see text]. In response to this, the study proposes a methodology, the feature deletion experiment, based on Automatic Machine Learning (AutoML) for knowledge extraction from a high-throughput density functional theory (DFT) database. The study reveals that, for binary alloy surfaces, the local adsorption site geometric information is the primary physical quantity determining [Formula: see text], compared to the electronic and physiochemical properties of the catalyst alloys. By integrating the feature deletion experiment with instance-wise variable selection (INVASE), a neural network-based explainable AI (XAI) tool, we established the best-performing feature set containing 21 intrinsic, non-DFT computed properties, achieving an MAE of 0.23 eV across a periodic table-wide chemical space involving more than 1,600 types of alloys surfaces and 8,400 chemisorption reactions. This study demonstrates the stability, consistency, and potential of AutoML-based feature deletion experiment in developing concise, predictive, and theoretically meaningful models for complex chemical problems with minimal human intervention.

2.
Anesthesiology ; 2024 May 16.
Article in English | MEDLINE | ID: mdl-38758221

ABSTRACT

BACKGROUND: Preventing emergence delirium is a clinical goal for pediatric anesthesia, yet there is no consensus on its prevention. This study investigated the hypothesis that a continuous infusion or a single bolus of remimazolam can reduce the incidence of emergence delirium in children. METHODS: A hundred and twenty children aged 1-6 years old were randomly and equally allocated into three groups: group RC, which received a continuous infusion of remimazolam at 1 mg kg -1 h -1; group RB, which received a single bolus of remimazolam at 0.2 mg kg -1 at the beginning of wound closure; and group C, which received a continuous infusion of saline at 1 mL kg -1 h -1 and single bolus of saline at 0.2 mL kg -1 at the beginning of sutures. The primary outcome was the incidence of emergence delirium assessed by pediatric anesthesia emergence delirium (PAED) scale. Secondary outcomes included the number of rescues propofol administrations in the post-anesthesia care unit (PACU), recovery time, end-tidal sevoflurane concentration when maintaining BIS within the range of 40-60, and adverse events. RESULTS: The incidence of emergence delirium in group RC (5%, vs. group C, risk ratio, 0.14; 95% CI, 0.04 to 0.59; P=0.001) and group RB (7.7%, vs. group C, risk ratio, 0.22; 95% CI, 0.07 to 0.71; P=0.003) was significantly lower compared with group C (32.5%). Propofol was given to 2 patients in each of groups RC and RB to treat delirium and to 10 patients in group C (group RC vs. group C, risk ratio, 0.20; 95% CI, 0.05 to 0.86; P=0.012; group RB vs. group C, risk ratio, 0.21; 95% CI, 0.05 to 0.88; P=0.014). No differences in the recovery time and adverse effects were detected. CONCLUSIONS: Both continuous infusion and single bolus administration of remimazolam can effectively reduce the occurrence of emergence delirium in children.

3.
Sheng Li Xue Bao ; 76(2): 247-256, 2024 Apr 25.
Article in Zh | MEDLINE | ID: mdl-38658374

ABSTRACT

This study aimed to investigate the effect of exosomes derived from bone marrow mesenchymal stem cells (BMSCs-EXO) on lung ischemia-reperfusion injury (IRI) in rats and to explore the role of miR-335. The model of rat lung IRI was established by clipping the hilum of left lung for 60 min and opening for 180 min. Forty Sprague-Dawley rats were randomly divided into sham group, IRI group, IRI+PBS group, IRI+EXO group, and IRI+miR-335 inhibitor EXO (IRI+inhibitor-EXO) group (n = 8). Rats in the sham group underwent thoracotomies without IRI. Rats in the IRI group were used to establish IRI model without any additional treatment. In the IRI+PBS, IRI+EXO, and IRI+inhibitor-EXO groups, the rats were used to establish IRI model and given PBS, EXO from BMSCs without any treatment, and EXO from BMSCs with miR-335 inhibitor treatment before reperfusion, respectively. Blood gases were analyzed during the experiment. Lung tissue wet/dry ratio (W/D), interleukin 1ß (IL-1ß), tumor necrosis factor α (TNF-α), myeloperoxidase (MPO), malondialdehyde (MDA), and superoxide dismutase (SOD) were measured at the end of reperfusion. Mitochondria were observed by electron microscopy and the Flameng scores were counted. Lung histopathology and apoptosis (TUNEL staining) were observed by light microscopy, and the lung injury scores (LIS) and apoptosis index (AI) were detected. The miR-335 expression was detected by RT-qPCR, and the expression of caspase-3, cleaved-caspase-3, caspase-9, cleaved-caspase-9, and NF-κB proteins were detected by Western blot at the end of reperfusion. The results showed that compared with the sham group, the oxygenation index, pH, and base excess (BE) were significantly lower in the IRI group and IRI+PBS group after reperfusion, whereas those indices were significantly higher in the IRI+EXO group than those in the IRI+PBS group (P < 0.05). Compared with the sham group, there were significant increases in W/D, IL-1ß, TNF-α, MPO, MDA, LIS, AI, Flameng score, caspase-3, cleaved-caspase-3, caspase-9, and cleaved-caspase-9, however significant decreases in the SOD, miR-335 and NF-κB in the IRI group (P < 0.05). These indices in the IRI and IRI+PBS groups showed no significant differences. Compared with the IRI+PBS group, there were significant decreases in W/D, IL-1ß, TNF-α, MPO, MDA, LIS, AI, Flameng score, caspase-3, cleaved-caspase-3, caspase-9, and cleaved-caspase-9, however significant increases in the SOD, miR-335 and NF-κB in the IRI+EXO group (P < 0.05). While, the changes of the above mentioned indices were reversed in the IRI+inhibitor-EXO group compared with IRI+EXO group, which were still better than those in the IRI+PBS group (P < 0.05). The results suggest that BMSCs-EXO could attenuate lung IRI in rats, activate NF-κB pathway, and maintain mitochondrial stability by up-regulating miR-335.


Subject(s)
Exosomes , Mesenchymal Stem Cells , MicroRNAs , NF-kappa B , Rats, Sprague-Dawley , Reperfusion Injury , Animals , Reperfusion Injury/metabolism , MicroRNAs/metabolism , MicroRNAs/genetics , Rats , Mesenchymal Stem Cells/metabolism , NF-kappa B/metabolism , Exosomes/metabolism , Male , Lung/metabolism , Lung/pathology , Signal Transduction , Bone Marrow Cells/metabolism , Apoptosis , Lung Injury/metabolism , Lung Injury/etiology , Tumor Necrosis Factor-alpha/metabolism
4.
Br J Anaesth ; 131(5): 914-920, 2023 11.
Article in English | MEDLINE | ID: mdl-37739904

ABSTRACT

BACKGROUND: The pharmacokinetic properties of the new benzodiazepine remimazolam have been studied only in adults. We investigated the pharmacokinetics of remimazolam after i.v. infusion in anaesthetised paediatric patients. METHODS: Twenty-four children (2-6 yr, ASA physical status 1-2, BMI 15-18 kg m-2) undergoing general anaesthesia with sevoflurane were enrolled. During surgery, remimazolam was administered as an i.v. infusion over 1 h at 5 mg kg-1 h-1 for 5 min, followed by 1.5 mg kg-1 h-1 for 55 min. Plasma concentrations of remimazolam and its metabolite CNS7054 were determined from arterial blood samples using ultra-high performance liquid chromatography-mass spectrometry. Pharmacokinetic modelling was performed by population analysis. RESULTS: Pharmacokinetics were best described by a three-compartment model for remimazolam and a two-compartment model for CNS7054 linked by a transit compartment. Remimazolam showed a high clearance of 15.9 (12.9, 18.2) ml kg-1 min-1 (median, Q25, Q75), a small central volume of distribution of 0.11 (0.08, 0.14) L kg-1 and a short terminal half-life of 67 (49, 85) min. The context-sensitive half-time after an infusion of 4 h was 17 (12, 21) min. The metabolite CNS7054 showed a low clearance of 0.89 (0.33, 1.40) ml kg-1 min-1, a small central volume of distribution of 0.011 (0.005, 0.016) L kg-1, and a long terminal half-life of 321 (230, 770) min. CONCLUSIONS: Remimazolam in children was characterised by a high clearance and short context-sensitive half-time. When normalised to weight, pharmacokinetic properties were similar to those reported for adults. CLINICAL TRIAL REGISTRATION: ChiCTR2200057629.


Subject(s)
Anesthesia, General , Benzodiazepines , Adult , Child , Humans , Infusions, Intravenous , Kinetics
5.
Clin Lab ; 69(11)2023 Nov 01.
Article in English | MEDLINE | ID: mdl-37948495

ABSTRACT

BACKGROUND: This study was designed to compare the body fluid module of Sysmex XN9000 (XN-BF) with optical microscopy (OM) for cerebrospinal fluid (CSF) analysis after two-step cell slide centrifuge (TSCSC), defining the best procedure for CSF optical microscopy analysis. METHODS: Items of RBC, WBC enumeration and differentiation were observed. The cell count and morphologic evaluation of the cellular composition by OM was carried out both with and without two-step cell slide centrifuge (TSCSC) and were compared the data with XN-BF. RESULTS: There were 69.98 ± 4.94 RBC and 36.98 ± 3.39 WBC in one OSCSC microscopic field whereas there were 96.35 ± 5.41 RBC and 66.15 ± 4.85 WBC in one TSCSC microscopic field in the same sample (*200). There was a statistical difference between those two methods (p = 0.000). Excellent correlation was found between total cell count with both OM and XN-BF. The R2 value for RBC and WBC counts were 0.99 and 0.96, respectively. For WBC differential, the R2 values were 0.98 for PMN and 0.70 for MN. Correlation of MN was poorer than PMN. As far as the tumor cell, phagocyte, and plasma cell with high fluorescence were concerned, OM were not consistent with XN-BF. CONCLUSIONS: The TSCSC procedure contributes to the separation of cells and other ingredients. XN-BF displays excellent performance at RBC and WBC cell count except for mononuclear cells, tumor cells, phagocytes, and leukemia cells. which makes it just a practical alternative to total cell (WBC, RBC) count for CSF samples. Detailed morphologic workup of CSF samples is mandated in all cases with meningoencephalitis, elevated cell count, sub-arachnoid hemorrhage and meningeal carcinomatosis, the TSCSC procedure is recommended.


Subject(s)
Body Fluids , Microscopy , Humans , Leukocyte Count , Leukocytes , Cell Differentiation , Cerebrospinal Fluid , Reproducibility of Results
6.
BMC Biotechnol ; 22(1): 26, 2022 09 08.
Article in English | MEDLINE | ID: mdl-36076195

ABSTRACT

BACKGROUND: With the growing concern for the environment, there are trends that bio-utilization of keratinous waste by keratinases could ease the heavy burden of keratinous waste from the poultry processing and leather industry. Especially surfactant-stable keratinases are beneficial for the detergent industry. Therefore, the production of keratinase by Bacillus cereus YQ15 was improved; the characterization and use of keratinase in detergent were also studied. RESULTS: A novel alkaline keratinase-producing bacterium YQ15 was isolated from feather keratin-rich soil and was identified as Bacillus cereus. Based on the improvement of medium components and culture conditions, the maximum keratinase activity (925 U/mL) was obtained after 36 h of cultivation under conditions of 35 °C and 160 rpm. Moreover, it was observed that the optimal reacting temperature and pH of the keratinase are 60 °C and 10.0, respectively; the activity was severely inhibited by PMSF and EDTA. On the contrary, the keratinase showed remarkable stability in the existence of the various surfactants, including SDS, Tween 20, Tween 60, Tween 80, and Triton X-100. Especially, 5% of Tween 20 and Tween 60 increased the activity by 100% and 60%, respectively. Furtherly, the keratinase revealed high efficiency in removing blood stains. CONCLUSION: The excellent compatibility with commercial detergents and the high washing efficiency of removing blood stains suggested its suitability for potential application as a bio-detergent additive.


Subject(s)
Bacillus cereus , Detergents , Animals , Bacillus cereus/metabolism , Detergents/chemistry , Enzyme Stability , Feathers/metabolism , Hydrogen-Ion Concentration , Keratins/metabolism , Peptide Hydrolases/metabolism , Polysorbates , Surface-Active Agents , Temperature
7.
BMC Biotechnol ; 22(1): 30, 2022 10 27.
Article in English | MEDLINE | ID: mdl-36303174

ABSTRACT

BACKGROUND: An important conceptual advance in health and the environment has been recognized that enzymes play a key role in the green processing industries. Of particular interest, chitosanase is beneficial for recycling the chitosan resource and producing chitosan oligosaccharides. Also, chitosan gene expression and molecular characterization will promote understanding of the biological function of bacterial chitosanase as well as explore chitosanase for utilizing chitosan resources. RESULTS: A chitosanase-producing bacterium TY24 was isolated and identified as Bacillus cereus. Moreover, the chitosanase gene was cloned and expressed in Escherichia coli. Sequence analysis reveals that the recombinant chitosanase (CHOE) belongs to the glycoside hydrolases 8 family. The purified CHOE has a molecular weight of about 48 kDa and the specific activity of 1150 U/mg. The optimal pH and temperature of CHOE were 5.5 and 65 °C, respectively. The enzyme was observed stable at the pH range of 4.5-7.5 and the temperature range of 30-65 °C. Especially, the half-life of CHOE at 65 °C was 161 min. Additionally, the activity of CHOE was remarkably enhanced in the presence of Mn2+, Cu2+, Mg2+ and K+, beside Ca2+ at 5 mM. Especially, the activity of CHOE was enhanced to more than 120% in the presence of 1% of various surfactants. CHOE exhibited the highest substrate specificity toward colloid chitosan. CONCLUSION: A bacterial chitosanase was cloned from B. cereus and successfully expressed in E. coli (BL21) DE3. The recombinant enzyme displayed good stability under acid pH and high-temperature conditions.


Subject(s)
Bacillus cereus , Chitosan , Bacillus cereus/genetics , Bacillus cereus/metabolism , Chitosan/metabolism , Escherichia coli/genetics , Escherichia coli/metabolism , Glycoside Hydrolases/chemistry , Cloning, Molecular , Hydrogen-Ion Concentration
8.
Lasers Med Sci ; 37(2): 1069-1079, 2022 Mar.
Article in English | MEDLINE | ID: mdl-34213684

ABSTRACT

The aim of this study is to evaluate whether the blood perfusion to tissues for detecting ischemic necrosis can be quantitatively monitored by spatial frequency domain imaging (SFDI) and laser speckle imaging (LSI) in a skin flap mouse model. Skin flaps were made on Institute of Cancer Research (ICR) mice. Using SFDI and LSI, the following parameters were estimated: oxyhemoglobin (HbO2), deoxyhemoglobin (Hb), total hemoglobin (THb), tissue oxygen saturation (StO2), and speckle flow index (SFI). Histologically, epithelium thickness, collagen deposition, and blood vessel count of skin flap tissues were analyzed. Then, the correlation of SFDI and histological results was assessed by application of Spearman rank correlation method. As the result, the number of blood vessels and the percentage of collagen areas showed significant difference between the necrotic tissue group and the non-necrotic one. Especially, the necrotic tissue had a complete epithelial loss and loses its normal structure. We identified that SFDI/LSI parameters were significantly different between non-necrotic and necrotic tissue groups. Especially, all SFDI and LSI parameters measured on the 1st day after surgery showed significant difference between necrotic tissue and non-necrotic tissue. In addition, the number of blood vessel and percentage of collagen area were positively correlated with HbO2 and StO2 among SFDI/LSI parameters. Meanwhile, the number of blood vessel and percentage of collagen area showed the negative correlation with Hb. By applying SFDI and LSI simultaneously to the skin flap, we could quantitatively monitor the blood perfusion and the tissue condition which can help us to detect ischemic necrosis objectively in early stage.


Subject(s)
Optical Imaging , Oxyhemoglobins , Animals , Disease Models, Animal , Mice , Necrosis , Optical Imaging/methods , Perfusion , Skin/pathology
9.
Clin Lab ; 67(12)2021 Dec 01.
Article in English | MEDLINE | ID: mdl-34910424

ABSTRACT

BACKGROUND: The pathogen detection rate of traditional ink staining procedure (TISP) is low. METHODS: A modified ink staining procedure (MISP) was created to accumulate pathogen by using cell slide centrifuge. Items of RBC, WBC, and cryptococcus were observed. RESULTS: There were 79.98 ± 54.94 RBC and 126.98 ± 36.39 WBC in one MISP microscopic field whereas there were only 3.35 ± 2.41 RBC and 6.15 ± 1.85 WBC in one TISP microscopic field in the same sample (*200). There was statistical difference between those two methods (p = 0.000). There were 40.78 ± 13.23 mL cryptococcus in CSF processed by MISP whereas there were only 2.10 ± 1.10 mL cryptococcus in the same CSF processed by TISP. There was statistical difference between those two methods. CONCLUSIONS: The modified ink staining procedure contributes to the separation of cells and pathogens (such as cryptococcus).


Subject(s)
Cryptococcus , Centrifugation , Cerebrospinal Fluid , Ink , Staining and Labeling
10.
Molecules ; 26(18)2021 Sep 17.
Article in English | MEDLINE | ID: mdl-34577134

ABSTRACT

Solid waste silica fume was used to replace fly ash by different ratios to study the early-age hydration reaction and strength formation mechanism of concrete. The change pattern of moisture content in different phases and micro morphological characteristics of concrete at early age were analyzed by low field nuclear magnetic resonance (LF-NMR) and scanning electron microscope (SEM). The results showed that the compressive strength of concrete was enhanced optimally when the replacement ratio of solid waste silica fume was 50%. The results of LF-NMR analysis showed that the water content of modified concrete increased with the increase of solid waste silica fume content. The compressive strength of concrete grew faster within the curing age of 7 d, which means the hydration process of concrete was also faster. The micro morphological characteristics obtained by SEM revealed that the concrete was densest internally when 50% fly ash was replaced by the solid waste silica fume, which was better than the other contents.

11.
Psychiatr Q ; 92(4): 1645-1656, 2021 12.
Article in English | MEDLINE | ID: mdl-34159503

ABSTRACT

The efficacy and safety of adjunctive nonconvulsive electrotherapy (NET) for patients with depression are undetermined. This systematic review was conducted to examine the efficacy and safety of adjunctive NET for patients with depression. Chinese (WanFang and Chinese Journal Net) and English (PubMed, EMBASE, PsycINFO and the Cochrane Library) databases were systematically searched from their inception until Jan 27, 2021 by three independent investigators. One randomized controlled trial (RCT) with 3 treatment arms (n = 108) and two observational studies (single-group, before-after design, n = 31) were included. In the RCT, the antidepressant efficacy of NET on depression was similar to that of electroconvulsive therapy (ECT) (P > 0.05) but with significantly fewer neurocognitive impairments as measured by the Repeatable Battery for the Assessment of Neuropsychological Status (RBANS) (P < 0.05). In two observational studies, the 17-item Hamilton Depression Rating Scale (HAMD-17) scores decreased significantly from baseline to post-NET (all Ps < 0.05), without adverse neurocognitive effects. In the RCT, adverse drug reactions (ADRs) were not separately reported among the 3 treatment arms but a similar rate of discontinuation was reported. The currently available limited evidence from 3 studies suggests that NET as an adjunctive treatment may be a safe, well-tolerated, effective therapy for depression without serious neurocognitive impairments.


Subject(s)
Electric Stimulation Therapy , Electroconvulsive Therapy , Antidepressive Agents , Depression/therapy , Humans
12.
Br J Clin Pharmacol ; 86(1): 85-92, 2020 01.
Article in English | MEDLINE | ID: mdl-31656042

ABSTRACT

AIMS: Dexmedetomidine is highly specific α2-adrenoceptor agonist. A single bolus of dexmedetomidine can achieve clinical therapeutic effect. Therefore, it is essential to know the safety margin between the clinical effectiveness dosages of dexmedetomidine and its side effect. METHODS: A total of 42 patients who underwent elective thyroidectomy were enrolled in this study. Dexmedetomidine was given as a single bolus injection 30 min towards the end of surgery. The up-and-down sequential schedule was used in this study. The starting dose of dexmedetomidine was set at 0.1 µg/kg in the first patient and the next patient would then receive a dose of dexmedetomidine decremented by 0.05 µg/kg if the prior patient's baseline heart rate (HR) had a decrease of ≥20% and/or mean arterial blood pressure (MAP) increase or decrease of ≥20%, otherwise, the following patient would receive an incremental 0.05 µg/kg dose of dexmedetomidine. The analytic techniques of linear, linear-logarithmic, exponential regressions and centred isotonic regression were used to determine the ED50 of dexmedetomidine and the residual standard errors were calculated for the comparison of goodness of fit among the different models. RESULTS: The median (interquartile range [range]) lowest HR was 57 beats/min (53-63.3[46-76]) with an average HR decrease of 8.0 beats/min (5-13 [4 to 23]). The median (interquartile range [range]) highest MAP was 98 mmHg (91.8-105 [83-126]) with a MAP increase of 10.0 mmHg (6.8-18.0 [2-24]). The ED50 (95% confidence interval) from 4 different statistical approaches (linear, linear-logarithmic, exponential regressions and centred isotonic regression) were 0.262 µg/kg (0.243, 0.306), 0.252 µg/kg (0.238, 0.307), 0.283 µg/kg (0.238, 0.307), and 0.278 µg/kg, respectively. Among the 4 models, the exponential regression had the least residual standard error (0.03618). CONCLUSION: The ED50 derived from 4 statistical models for an intravenous bolus of dexmedetomidine without significant haemodynamic effects was distributed in a narrow range of 0.252-0.283 µg/kg, and the exponential regression was the model to best match the study data.


Subject(s)
Dexmedetomidine , Adult , Anesthesia, General , Heart Rate , Hemodynamics , Humans , Hypnotics and Sedatives/pharmacology
13.
Sensors (Basel) ; 20(11)2020 Jun 05.
Article in English | MEDLINE | ID: mdl-32517133

ABSTRACT

We study wireless indoor positioning systems where multiple synchronized infrastructure devices simultaneously receive signals from an object of interest whose arrival times are measured. The positioning performance is degraded by unresolvable channel multipath and non-line-of-sight (NLOS) reflctions which cause a bias in the time difference of arrival (TDOA) measurements. In order to reduce the negative effect of multi-path, a Multi-Path Map (MPM) method based on spatial domain modeling principle in the reverse positioning framework with good robustness is proposed. Meanwhile, an improved non-linear iterative algorithm with height component constrained which reduces the complexity is introduced to calculate the coordinates so that the performance of the MPM can be verified. By using the MPM measurements as pre-calibration information to compensate the TDOA observed value, the accuracy of the cooperative location based on a UWB device is 6.45 cm, which achieves 63% improvement than that of none MPM used.

14.
Clin Lab ; 65(1)2019 Jan 01.
Article in English | MEDLINE | ID: mdl-30775888

ABSTRACT

BACKGROUND: In order to increase the detection rate of pathogenic microorganisms in CSF, an improved specimen handling procedure (ISHP) was created. METHODS: This study enrolled encephalitis and control groups, both groups were handled with traditional specimen handling procedure (TSHP) and ISHP. Glutaraldehyde was added to the ISHP. Observed items included: total protein, glucose, chloride, adenosine deaminase, lactate dehydrogenase, sediment, cell and pathogen, Pandy's test. RESULTS: Sediment test of CSF: There was 1 specimen in 10 control specimens tested by TSHP in which Pandy's test was positive; there were 2 specimens tested by ISHP which could see sediment by eye. There was no statistical difference between those two methods (p = 1.000, Table 1). Ten specimens in 23 of the encephalitis group processed by TSHP were positive with Pandy's test; 23 specimens processed by ISHP could all see sediments by eye (Figure 1). There was a statistical difference between the two methods (p = 0.000, Table 1). Pathogen test of CSF: no pathogen was found in the control group processed by TSHP and ISHP. No pathogen was found in the encephalitis group specimens processed by TSHP. Pathogen tests were positive in 7 encephalitis specimens processed by ISHP (p = 0.009, Table 1), which were confirmed as Rickettsia spp. by Gimenze stain (Figure 1B), IFA (Figure 2). CONCLUSIONS: The results revealed that ISHP contributes to the separation of cells, pathogens (such as Rickettsia), and proteins.


Subject(s)
Infectious Encephalitis/cerebrospinal fluid , Rickettsia Infections/cerebrospinal fluid , Rickettsia/physiology , Specimen Handling/methods , Adolescent , Adult , Aged , Aged, 80 and over , Child , Female , Humans , Infectious Encephalitis/diagnosis , Infectious Encephalitis/microbiology , Male , Microscopy, Fluorescence , Middle Aged , Rickettsia Infections/diagnosis , Rickettsia Infections/microbiology , Young Adult
15.
Mol Pharm ; 13(4): 1242-50, 2016 Apr 04.
Article in English | MEDLINE | ID: mdl-26824303

ABSTRACT

Major limitations of camptothecin anticancer drugs (toxicity, nonselectivity, water insolubility, inactivation by human serum albumin) may be improved by creating glucuronide prodrugs that rely on beta-glucuronidase for their activation. We found that the camptothecin derivative 5,6-dihydro-4H-benzo[de]quinoline-camptothecin (BQC) displays greater cytotoxicity against cancer cells than the clinically used camptothecin derivatives SN-38 and topotecan even in the presence of human serum albumin. We synthesized the prodrug BQC-glucuronide (BQC-G), which was 4000 times more water soluble and 20-40 times less cytotoxic than BQC. Importantly, even in the presence of human serum albumin, BQC-G was efficiently hydrolyzed by beta-glucuronidase and produced greater cytotoxicity (IC50 = 13 nM) than camptothecin, 9-aminocamptothecin, SN-38, or topotecan (IC50 > 3000, 1370, 48, and 28 nM, respectively). BQC-G treatment of mice bearing human colon cancer xenografts with naturally or artificially elevated beta-glucuronidase activity produced significant antitumor activity, showing that BQC-G is a potent prodrug suitable for selective intratumoral drug activation.


Subject(s)
Glucuronides/chemistry , Glucuronides/pharmacology , Prodrugs/chemistry , Prodrugs/pharmacology , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Camptothecin/analogs & derivatives , Camptothecin/chemistry , Camptothecin/pharmacology , Cell Line, Tumor , Cell Survival/drug effects , Colonic Neoplasms/drug therapy , Female , Glucuronidase/metabolism , Glucuronides/therapeutic use , Humans , Irinotecan , Mice , Mice, Inbred BALB C , Prodrugs/metabolism , Prodrugs/therapeutic use , Topotecan/chemistry , Topotecan/pharmacology
16.
Zhongguo Zhong Yao Za Zhi ; 41(12): 2208-2212, 2016 Jun.
Article in Zh | MEDLINE | ID: mdl-28901061

ABSTRACT

To reveal the relationship between endophytic fungi and the functional components, saccharides and flavonoids in the mycelia or fermented liquor of 21 endophytic fungi in D.officinale were detected using HPLC and UV spectrophotometer.The results showed that the ethyl acetate extracts from 21 fungal strains all contain flavonoids.According to the chromatographic retention time of HPLC and UV spectra characteristics of flavonoids, strain DO49 was found produce naringenin, strains DO23, DO81 and DO83 were found produce rutin.The water-soluble extracts from 21 strains all had polysaccharides.However, there was difference in the composition of monosaccharides derived from polysaccharides among different strains.According to the composition of monosaccharides and the peak area ratio of mannose and glucose, the fungal strains including DO23, DO26, DO81, DO54, DO55, DO83 product polysaccharides associated with D.officinale were selected.In conclusion, based on the saccharides and flavonoids, the excellent endophytic fungal strains DO23, DO81 and DO83 were selected, which could produce the same flavonoids and similar polysaccharides in D.officinale.


Subject(s)
Dendrobium/microbiology , Flavonoids/analysis , Fungi/chemistry , Polysaccharides/analysis , Endophytes/chemistry
17.
Environ Sci Technol ; 49(6): 3653-61, 2015 Mar 17.
Article in English | MEDLINE | ID: mdl-25655234

ABSTRACT

Water-sediment exchange is a fundamental component of oxyanion cycling in the environment. Yet, many of the (im)mobilization processes overlay complex spatial and temporal redox regimes that occur within millimeters of the interface. Only a few methods exist that can reliably capture these porewater fluxes, with the most popular being high-resolution diffusive gradients in thin films (HR-DGT). However, functionality of HR-DGT is restricted by the availability of suitable analyte binding agents within the sampler, which must be simple to cast and homogeneously distributed in the binding layer, exhibit adequate sorption capacities, be resistive to chemical change, and possess a very fine particle size (≤10 µm). A novel binding layer was synthesized to meet these requirements by in situ precipitation of zirconia into a precast hydrogel. The particle diameter≤0.2 µm of zirconia in this precipitated gel was uniform and at least 50-times smaller than the conventional molding approach. Further, this gel had superior binding and stability characteristics compared with the commonly used ferrihydrite HR-DGT technique and could be easily fabricated as an ultrathin gel (60 µm) for simultaneous oxygen imaging in conjunction with planar-optodes. Chemical imaging of anion and oxygen fluxes using the new sampler were evaluated on Lake Taihu sediments.


Subject(s)
Anions/analysis , Chemical Precipitation , Geologic Sediments/chemistry , Imaging, Three-Dimensional , Oxygen/analysis , Water Pollutants, Chemical/analysis , Water/chemistry , Zirconium/chemistry , Diffusion , Environment , Gels , Hydrogen-Ion Concentration , Kinetics , Osmolar Concentration , Spectrophotometry, Atomic , Time Factors
18.
Chem Biodivers ; 12(9): 1349-55, 2015 Sep.
Article in English | MEDLINE | ID: mdl-26363879

ABSTRACT

Three new polyketides, named daldinone F (1), nodulisporin G (2), and dalmanol C (3), together with five known compounds, 4-8, were isolated from cultures of Daldinia eschscholzii. The structures of the new compounds were elucidated by extensive NMR and MS analyses. Compound 1 showed moderate cytotoxic activity against SW480 cancer cells with an IC50 value of 9.59 µM, and its absolute configuration was determined by single crystal X-ray diffraction.


Subject(s)
Polyketides/analysis , Xylariales/chemistry , Crystallography, X-Ray , Magnetic Resonance Spectroscopy , Models, Molecular
19.
J Asian Nat Prod Res ; 17(2): 143-8, 2015.
Article in English | MEDLINE | ID: mdl-25402226

ABSTRACT

Two new tricycloalternarenes I (1) and J (2), together with five known derivatives (3-7), were isolated from the culture of marine fungus Alternaria sp. The structures were elucidated by a combination of spectroscopic approach ((1)H, (13)C NMR, HMBC, COSY, and NOESY) and the low-temperature (100 K) single-crystal X-ray crystallography analysis. The antimicrobial assays of tricycloalternarenes I (1) and J (2) were tested.


Subject(s)
Alternaria/chemistry , Anti-Bacterial Agents/isolation & purification , Terpenes/isolation & purification , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Bacillus subtilis/drug effects , China , Crystallography, X-Ray , Marine Biology , Microbial Sensitivity Tests , Molecular Structure , Mycobacterium smegmatis/drug effects , Nuclear Magnetic Resonance, Biomolecular , Streptococcus pyogenes/drug effects , Terpenes/chemistry , Terpenes/pharmacology
20.
Paediatr Anaesth ; 24(5): 505-9, 2014 May.
Article in English | MEDLINE | ID: mdl-24708453

ABSTRACT

BACKGROUND: The objective of this study was to determine ED50 and ED95 of remifentanil for intubation combined with propofol in nonparalyzed Chinese children. METHODS: Forty-seven American Society of Anesthesiologists Class I children aged 4-11 years weighing 14-33.5 kg underwent general anesthesia with 2.5 mg·kg(-1) of intravenous propofol followed by remifentanil in Wenzhou, China. The initial dose of remifentanil was 2.5 µg·kg(-1) injected over 60 s. Intubation was attempted 30 s after the completion of remifentanil injection. Level of difficulty to intubate was graded on a scoring system. If the initial intubation condition was deemed satisfactory, subsequent remifentanil doses were decreased by 0.25 µg·kg(-1). If the intubating condition was deemed unsatisfactory, subsequent remifentanil doses were increased by 0.25 µg·kg(-1). Mean arterial pressure, heart rate, and pulse oximetry were documented before and after induction, immediately after intubation, and 1 min after intubation. RESULTS: The ED50 of remifentanil used to render a satisfactory intubating condition used in combination with 2.5 mg·kg(-1) of propofol in nonparalyzed Chinese children was 2.30 µg·kg(-1) (95% confidence interval: 2.28-2.31 µg·kg(-1)), and the ED95 is 2.75 µg·kg(-1) (95% confidence interval: 2.59-3.35 µg·kg(-1)). These doses were lower than previously reported. CONCLUSION: When used in combination with 2.5 mg·kg(-1) of intravenous propofol, ED50 and ED95 of remifentanil for adequate intubation in nonparalyzed children were lower than previously reported, at 2.30 and 2.75 µg·kg(-1), respectively.


Subject(s)
Anesthetics, Intravenous/administration & dosage , Intubation, Intratracheal/methods , Piperidines/administration & dosage , Analysis of Variance , Anesthetics, Combined/administration & dosage , Blood Pressure/drug effects , Child , Child, Preschool , China , Dose-Response Relationship, Drug , Female , Heart Rate/drug effects , Humans , Male , Propofol/administration & dosage , Remifentanil
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