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1.
J Sci Food Agric ; 104(6): 3570-3584, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38150568

ABSTRACT

BACKGROUND: Tea pests pose a significant threat to tea leaf yield and quality, necessitating fast and accurate detection methods to improve pest control efficiency and reduce economic losses for tea farmers. However, in real tea gardens, some tea pests are small in size and easily camouflaged by complex backgrounds, making it challenging for farmers to promptly and accurately identify them. RESULTS: To address this issue, we propose a real-time detection method based on TP-YOLOX for monitoring tea pests in complex backgrounds. Our approach incorporates the CSBLayer module, which combines convolution and multi-head self-attention mechanisms, to capture global contextual information from images and expand the network's perception field. Additionally, we integrate an efficient multi-scale attention module to enhance the model's ability to perceive fine details in small targets. To expedite model convergence and improve the precision of target localization, we employ the SIOU loss function as the bounding box regression function. Experimental results demonstrate that TP-YOLOX achieves a significant performance improvement with a relatively small additional computational cost (0.98 floating-point operations), resulting in a 4.50% increase in mean average precision (mAP) compared to the original YOLOX-s. When compared with existing object detection algorithms, TP-YOLOX outperforms them in terms of mAP performance. Moreover, the proposed method achieves a frame rate of 82.66 frames per second, meeting real-time requirements. CONCLUSION: TP-YOLOX emerges as a proficient solution, capable of accurately and swiftly identifying tea pests amidst the complex backgrounds of tea gardens. This contribution not only offers valuable insights for tea pest monitoring but also serves as a reference for achieving precise pest control. © 2023 Society of Chemical Industry.


Subject(s)
Algorithms , Trees , Humans , Farmers , Gardening , Tea
2.
Nat Mater ; 15(2): 235-42, 2016 Feb.
Article in English | MEDLINE | ID: mdl-26595119

ABSTRACT

Fluorescent imaging of biological systems in the second near-infrared window (NIR-II) can probe tissue at centimetre depths and achieve micrometre-scale resolution at depths of millimetres. Unfortunately, all current NIR-II fluorophores are excreted slowly and are largely retained within the reticuloendothelial system, making clinical translation nearly impossible. Here, we report a rapidly excreted NIR-II fluorophore (∼90% excreted through the kidneys within 24 h) based on a synthetic 970-Da organic molecule (CH1055). The fluorophore outperformed indocyanine green (ICG)-a clinically approved NIR-I dye-in resolving mouse lymphatic vasculature and sentinel lymphatic mapping near a tumour. High levels of uptake of PEGylated-CH1055 dye were observed in brain tumours in mice, suggesting that the dye was detected at a depth of ∼4 mm. The CH1055 dye also allowed targeted molecular imaging of tumours in vivo when conjugated with anti-EGFR Affibody. Moreover, a superior tumour-to-background signal ratio allowed precise image-guided tumour-removal surgery.


Subject(s)
Benzopyrans/pharmacology , Carcinoma, Squamous Cell/pathology , Fluorescent Dyes/pharmacology , Indoles/pharmacology , Neoplasms, Experimental/pathology , Phenylpropionates/pharmacology , Thiadiazoles/pharmacology , Animals , Benzopyrans/chemistry , Benzopyrans/urine , Cell Line, Tumor , Diagnostic Imaging/methods , Female , Humans , Indoles/chemistry , Indoles/urine , Male , Mice , Mice, Inbred BALB C , Mice, Inbred C57BL , Spectroscopy, Near-Infrared
3.
Neurol Sci ; 38(1): 33-40, 2017 Jan.
Article in English | MEDLINE | ID: mdl-27785579

ABSTRACT

Dozens of observational studies and two meta-analyses have investigated the association of migraine with the risk of stroke, but their results are inconsistent. We aimed to quantitatively evaluate the relationship between migraine and stroke risk by performing a meta-analysis of prospective cohort studies. PubMed and Embase were searched through July 2016 to identify studies that met pre-stated inclusion criterion and reference lists of retrieved articles were also reviewed. Information on the characteristics of the included study, risk estimates, and control for possible confounding factors were extracted independently by two authors. The random-effects model was used to calculate the pooled risk estimates. Eleven prospective cohort studies involving 3371 patients with stroke and 2,221,888 participants were included in this systematic review. Compared with non-migraineurs, the pooled relative risks of total stroke, hemorrhagic stroke, and ischemic stroke for migraineurs were 1.55 [95% confidence interval (CI) 1.38-1.75], 1.15 (95% CI 0.85-1.56), and 1.64 (95% CI 1.22-2.20), respectively. Exception of any single study did not materially alter the combined risk estimate. Integrated epidemiological evidence supports that migraine should be associated with the increased risk of total stroke and ischemic stroke, but the relationship between migraine and the risk of hemorrhagic stroke is not of certainty.


Subject(s)
Migraine Disorders/epidemiology , Stroke/epidemiology , Humans , Incidence , Risk
4.
Nanomedicine ; 12(7): 1795-1803, 2016 10.
Article in English | MEDLINE | ID: mdl-27184095

ABSTRACT

Alginate/chitosan nanocomposite particles (GSNO-acNCPs), i.e. S-nitrosoglutathione (GSNO) loaded polymeric nanoparticles incorporated into an alginate and chitosan matrix, were developed to increase the effective GSNO loading capacity, a nitric oxide (NO) donor, and to sustain its release from the intestine following oral administration. Compared with free GSNO and GSNO loaded nanoparticles, GSNO-acNCPs promoted 2.7-fold GSNO permeation through a model of intestinal barrier (Caco-2 cells). After oral administration to Wistar rats, GSNO-acNCPs promoted NO storage into the aorta during at least 17h, as highlighted by (i) a long-lasting hyporeactivity to phenylephrine (decrease in maximum vasoconstrictive effect of aortic rings) and (ii) N-acetylcysteine (a thiol which can displace NO from tissues)-induced vasodilation of aorxxtic rings preconstricted with phenylephrine. In conclusion, GSNO-acNCPs enhance GSNO intestinal absorption and promote the formation of releasable NO stores into the rat aorta. GSNO-acNCPs are promising carriers for chronic oral application devoted to the treatment of cardiovascular diseases.


Subject(s)
Nanocomposites , Nitric Oxide/metabolism , Polymers , S-Nitrosoglutathione/pharmacokinetics , Animals , Aorta , Caco-2 Cells , Humans , Intestinal Absorption , Rats , Rats, Wistar
5.
Mol Pharm ; 12(3): 675-83, 2015 Mar 02.
Article in English | MEDLINE | ID: mdl-25584860

ABSTRACT

Due to overexpression of glycyrrhetinic acid (GA) receptor in liver cancer cells, glycyrrhetinic acid modified recombinant human serum albumin (rHSA) nanoparticles for targeting liver tumor cells may result in increased therapeutic efficacy and decreased adverse effects of cancer therapy. In this study, doxorubicin (DOX) loaded and glycyrrhetinic acid modified recombinant human serum albumin nanoparticles (DOX/GA-rHSA NPs) were prepared for targeting therapy for liver cancer. GA was covalently coupled to recombinant human serum albumin nanoparticles, which could efficiently deliver DOX into liver cancer cells. The resultant GA-rHSA NPs exhibited uniform spherical shape and high stability in plasma with fixed negative charge (∼-25 mV) and a size about 170 nm. DOX was loaded into GA-rHSA NPs with a maximal encapsulation efficiency of 75.8%. Moreover, the targeted NPs (DOX/GA-rHSA NPs) showed increased cytotoxic activity in liver tumor cells compared to the nontargeted NPs (DOX/rHSA NPs, DOX loaded recombinant human serum albumin nanoparticles without GA conjugating). The targeted NPs exhibited higher cellular uptake in a GA receptor-positive liver cancer cell line than nontargeted NPs as measured by both flow cytometry and confocal laser scanning microscopy. Biodistribution experiments showed that DOX/GA-rHSA NPs exhibited a much higher level of tumor accumulation than nontargeted NPs at 1 h after injection in hepatoma-bearing Balb/c mice. Therefore, the DOX/GA-rHSA NPs could be considered as an efficient nanoplatform for targeting drug delivery system for liver cancer.


Subject(s)
Antineoplastic Agents/administration & dosage , Doxorubicin/administration & dosage , Liver Neoplasms, Experimental/drug therapy , Nanocapsules/chemistry , Animals , Antineoplastic Agents/pharmacokinetics , Doxorubicin/pharmacokinetics , Drug Delivery Systems , Glycyrrhetinic Acid/chemistry , HeLa Cells , Hep G2 Cells , Humans , Liver Neoplasms, Experimental/metabolism , Magnetic Resonance Spectroscopy , Male , Mice , Mice, Inbred BALB C , Mice, Nude , Microscopy, Electron, Transmission , Nanocapsules/administration & dosage , Nanocapsules/ultrastructure , Recombinant Proteins/chemistry , Serum Albumin/chemistry , Tissue Distribution , Xenograft Model Antitumor Assays
6.
BMC Pregnancy Childbirth ; 15: 343, 2015 Dec 22.
Article in English | MEDLINE | ID: mdl-26694165

ABSTRACT

BACKGROUND: Few studies on cluster-based synthetic effects of multiple risk factors for birth defects have been reported. The present study aimed to identify maternal exposure clusters, explore the association between clusters of risk factors and birth defects, and further screen women with high risk for birth defects among expectant mothers. METHODS: Data were drawn from a large-scale, retrospective epidemiological survey of birth defects from 2006 to 2008 in six counties of Shanxi Province, China, using a three-level stratified random cluster sampling technique. Overall risk factors were extracted using eight synthetic variables summed and examined as a total risk factor score: maternal delivery age, genetic factors, medical history, nutrition and folic acid deficiency, maternal illness in pregnancy, drug use in pregnancy, environmental risk factors in pregnancy, and unhealthy maternal lifestyle in pregnancy. Latent class cluster analysis was used to identify maternal exposure clusters based on these synthetic variables. Adjusted odds ratios (AOR) were used to explore associations between clusters and birth defects, after adjusting for confounding variables using logistic regression. RESULTS: Three latent maternal exposure clusters were identified: a high-risk (6.15%), a moderate-risk (22.39%), and a low-risk (71.46%) cluster. The prevalence of birth defects was 14.08%, 0.85%, and 0.52% for the high-, middle- and low-risk clusters respectively. After adjusting for maternal demographic variables, women in the high-risk cluster were nearly 31 times (AOR: 30.61, 95% CI: [24.87, 37.67]) more likely to have an infant with birth defects than low-risk women. CONCLUSIONS: A high-risk group of mothers in an area with a high risk for birth defects were screened in our study. Targeted interventions should be conducted with women of reproductive age to improve neonatal birth outcomes in areas with a high risk of birth defects.


Subject(s)
Congenital Abnormalities/epidemiology , Congenital Abnormalities/etiology , Folic Acid Deficiency , Maternal Age , Maternal Exposure , Pregnancy Complications , Adult , China , Cluster Analysis , Female , Humans , Infant , Life Style , Logistic Models , Mass Screening , Odds Ratio , Pregnancy , Retrospective Studies , Risk Factors
7.
Molecules ; 20(9): 17585-600, 2015 Sep 23.
Article in English | MEDLINE | ID: mdl-26404228

ABSTRACT

A novel series of benzenesulfonamide derivatives containing 4-aminobenzenesul-fonamide and α-amides branched valproic acid or 2,2-dimethylcyclopropanecarboxylic acid moieties were synthesized and screened for their anticonvulsant activities in mice maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) test. The activity experimental study showed that 2,2-dipropyl-N¹-(4-sulfamoylphenyl)malonamide (18b) had the lowest median effective dose (ED50) of 16.36 mg/kg in MES test, and 2,2-dimethyl-N-(4-sulfamoylphenyl)cyclopropane-1,1-dicarboxamide (12c) had the lowest ED50 of 22.50 mg/kg in scPTZ test, which resulted in the protective indexe (PI) of 24.8 and 20.4, respectively. These promising data suggest the new compounds have good potential as new class of anticonvulsant agents with high effectiveness and low toxicity for the treatment of epilepsy.


Subject(s)
Anticonvulsants/chemical synthesis , Seizures/drug therapy , Sulfonamides/chemical synthesis , Animals , Anticonvulsants/administration & dosage , Anticonvulsants/chemistry , Disease Models, Animal , Male , Mice , Molecular Structure , Seizures/etiology , Structure-Activity Relationship , Sulfonamides/administration & dosage , Sulfonamides/chemistry , Benzenesulfonamides
8.
Angew Chem Int Ed Engl ; 54(20): 5981-4, 2015 May 11.
Article in English | MEDLINE | ID: mdl-25800807

ABSTRACT

Small-molecule-based multimodal and multifunctional imaging probes play prominent roles in biomedical research and have high clinical translation ability. A novel multimodal imaging platform using base-catalyzed double addition of thiols to a strained internal alkyne such as bicyclo[6.1.0]nonyne has been established in this study, thus allowing highly selective assembly of various functional units in a protecting-group-free manner. Using this molecular platform, novel dual-modality (PET and NIRF) uPAR-targeted imaging probe: (64)Cu-CHS1 was prepared and evaluated in U87MG cells and tumor-bearing mice models. The excellent PET/NIRF imaging characteristics such as good tumor uptake (3.69%ID/g at 2 h post-injection), high tumor contrast, and specificity were achieved in the small-animal models. These attractive imaging properties make (64)Cu-CHS1 a promising probe for clinical use.


Subject(s)
Alkynes/chemistry , Cyclooctanes/chemistry , Molecular Imaging , Molecular Probes/chemistry , Neoplasms, Experimental/diagnosis , Alkynes/pharmacokinetics , Animals , Cell Line, Tumor , Cyclooctanes/pharmacokinetics , Disease Models, Animal , Humans , Mice , Molecular Probes/pharmacokinetics , Molecular Structure , Positron-Emission Tomography , Sulfhydryl Compounds/chemistry , Sulfhydryl Compounds/pharmacokinetics
9.
Biomed Chromatogr ; 28(7): 1036-40, 2014 Jul.
Article in English | MEDLINE | ID: mdl-24375717

ABSTRACT

Nifedipine is a dihydropyridine calcium channel blocker used widely in the management of hypertension and other cardiovascular disorders. In this work, a simple, rapid and sensitive liquid chromatography/tandem mass spectrometry method was developed and validated to determine nifedipine in dog plasma using nimodipine as the internal standard. Chromatographic separation was carried out on a C8 column. The mobile phase consisted of a mixture of acetonitrile, water and formic acid (60:40:0.2, v/v/v) at a flow rate of 0.5 mL/min. Detection was performed on a triple quadrupole tandem mass spectrometer in selected reaction monitoring mode via an atmospheric pressure chemical ionization source. The method has a lower limit of quantification of 0.20 ng/mL with consumption of plasma as low as 0.05 mL. The linear calibration curves were obtained in the concentration range of 0.20-50.0 ng/mL (r = 0.9948). The recoveries of the liquid extraction method were 74.5-84.1%. Intra-day and inter-day precisions were 4.1-8.8 and 6.7-7.4%, respectively. The quantification was not interfered with by other plasma components and the method was applied to determine nifedipine in plasma after a single oral administration of two controlled-release nifedipine tablets to beagle dogs.


Subject(s)
Chromatography, High Pressure Liquid/methods , Nifedipine/blood , Tandem Mass Spectrometry/methods , Animals , Dogs , Linear Models , Male , Nifedipine/chemistry , Nifedipine/pharmacokinetics , Reproducibility of Results , Sensitivity and Specificity
10.
Gait Posture ; 99: 9-13, 2023 01.
Article in English | MEDLINE | ID: mdl-36283302

ABSTRACT

BACKGROUND: Selective motor control (SMC) is a fundamental component of typical human motion. As a result of brain damage, impaired SMC often leads to difficulties with coordination, balance, gait efficiency and symmetry. RESEARCH QUESTION: What is the association between impaired SMC and lower limb motor ability, functional balance and gait performance in children with bilateral spastic cerebral palsy (CP)? METHODS: Thirty-six children (aged 5-16 years) with spastic bilateral CP in Gross Motor Function Classification System (GMFCS) level I to II were included in this study. SMC was assessed using Selective Control Assessment of the Lower Extremity (SCALE). Gross motor function was assessed using Gross Motor Function Measure-88 items D and E dimension (GMFM-88 D&E). Functional balance was assessed using Pediatric Balance Scale (PBS) and Timed Up and Go Test (TUG). Gait quality was assessed using Edinburg Visual Gait Score (EVGS) and 10-Meter Walk Test (10MWT). Spearman's rank correlation analyses were used to determine the association between SMC and other factors. RESULTS: Correlation analyses showed that SCALE was strongly positively correlated with GMFM-88 (D&E) (rs=0.756, p < 0.001), PBS (rs=0.769, p < 0.001), and height-normalized fast walking speed (rs=0.632, p < 0.001), and strongly negatively correlated with TUG (rs=-0.766, p < 0.001) and EVGS (rs=-0.893, p < 0.001). SIGNIFICANCE: Lower extremity SMC deficits are associated with poor gross motor function and balance control, more severe overall gait deviations and decreased fast walking speed in children with bilateral spastic CP. Physical therapy should include interventions that promote selective motor control in order to improve overall functional ability.


Subject(s)
Cerebral Palsy , Child , Humans , Postural Balance , Muscle Spasticity , Time and Motion Studies , Gait
11.
J Asian Nat Prod Res ; 12(3): 185-93, 2010 Mar.
Article in English | MEDLINE | ID: mdl-20390763

ABSTRACT

Aesculetin (1) is an important coumarin found in various plant materials. It has been shown to have antiproliferative effects on several types of human cancer cells, but its effect on cervical cancer cells in vitro is unknown. In this study, we investigated that the cytotoxic effect of 1 on a non-cancer cell line (293) was smaller than on a tumor cell line (HeLa). This is the first report showing the possible mechanism of antiproliferative effect of 1 for the prevention of cervical cancer in cell culture models. It was found that 1 inhibited cell viability by inducing apoptosis, as evidenced by the formation of apoptotic bodies, generation of reactive oxygen species (ROS), and the accumulation of cells in the sub-G1 phase. Treatment with compound 1 decreased the cell growth in a dose-dependent manner with an IC(50) value of 37.8 microM. Aesculetin-induced apoptosis was correlated with mitochondrial dysfunction (DeltaPsi(m)), leading to the release of cytochrome c from the mitochondria to the cytosol, as well as the proteolytic activation of caspases in HeLa cells. These results indicate that 1 induces apoptosis in HeLa cells through a ROS-mediated mitochondrial dysfunction pathway.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Apoptosis/drug effects , Mitochondria/drug effects , Umbelliferones/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Bisbenzimidazole , Caspases/drug effects , Caspases/metabolism , Cytochromes c/metabolism , Drug Screening Assays, Antitumor , Female , HeLa Cells , Humans , Mitochondria/enzymology , Mitochondria/physiology , Models, Biological , Molecular Structure , Plants, Medicinal/chemistry , Tumor Cells, Cultured , Umbelliferones/chemistry , Uterine Cervical Neoplasms
12.
Chem Commun (Camb) ; (9): 1037-9, 2009 Mar 07.
Article in English | MEDLINE | ID: mdl-19225628

ABSTRACT

4alpha-Aminosteroids were synthesized by the substitution of a 2alpha-bromo ketone using K(2)CO(3) as an activator; 4beta-aminosteroids were synthesized in excellent yields by a highly regioselective and trans-stereospecific ring opening of a steroidal 3,4alpha-epoxide using ZnCl(2)-H(2)O as a catalyst.


Subject(s)
Androstanes/chemical synthesis , Steroids/chemical synthesis , Androstanes/chemistry , Catalysis , Ketones/chemistry , Steroids/chemistry , Zinc/chemistry
13.
Food Chem Toxicol ; 45(10): 2040-6, 2007 Oct.
Article in English | MEDLINE | ID: mdl-17597278

ABSTRACT

Cremanthodium humile (C. humile) is a traditional herbal medicine for treatment of inflammation. Based on initial screening results, the purpose of this study was to evaluate the cytotoxic effect on four human cancer cell lines and one non-cancer cell line (293), then to determine the possible mechanisms of cell death elicited by the extract of C. humile on Hela cells. We have found the ether extract of C. humile (CH-EE) strongly decreased the survival rate of the four human tumor cell lines: Hela, A549, HepG2 and SW480. The cytotoxic effect of CH-EE on 293 was smaller than on tumor cell lines. Flow cytometry assays and nuclear staining showed that CH-EE induced apoptosis in Hela cells. This process was accompanied by the collapse of mitochondrial membrane potential, the release of cytochrome c and the activation of caspase-3/7 and -9. Furthermore, CH-EE generated reactive oxygen species (ROS) in Hela cells. These results indicate that CH-EE induces apoptosis in Hela cells through a ROS-mediated mitochondrial dysfunction pathway.


Subject(s)
Apoptosis/drug effects , Asteraceae/chemistry , Blotting, Western , Caspases/metabolism , Cell Cycle/drug effects , Cell Survival/drug effects , Chromatography, High Pressure Liquid , Cytochromes c/metabolism , DNA Fingerprinting , HeLa Cells , Humans , Indicators and Reagents , Membrane Potentials , Microscopy, Fluorescence , Mitochondria/drug effects , Plant Extracts/pharmacology , Reactive Oxygen Species/metabolism
14.
Chem Biodivers ; 4(9): 2198-209, 2007 Sep.
Article in English | MEDLINE | ID: mdl-17886838

ABSTRACT

Three hydrazone ligands, H2L1-H2L3, made from salicylaldehyde and ibuprofen- or naproxen-derived hydrazides, were prepared and transformed into the corresponding copper(II) complexes [Cu(II)L1] x H2O, [Cu(II)L2], and [(Cu(II))2(L3)2] x H2O x DMF (Scheme). The X-ray crystal structure of the last-mentioned complex was solved (Fig. 1), showing a square-planar complexation geometry, and the single units were found to form a one-dimensional chain structure (Fig. 2). The interactions of these complexes with CT-DNA were studied by different techniques, indicating that they all bind to DNA by classical and/or non-classical intercalation modes.


Subject(s)
Aldehydes/chemistry , Hydrazones/chemistry , Intercalating Agents/chemistry , Organometallic Compounds/chemistry , Copper/chemistry , Crystallography, X-Ray , DNA/chemistry , Hydrazones/chemical synthesis , Intercalating Agents/chemical synthesis , Molecular Structure , Organometallic Compounds/chemical synthesis
15.
Steroids ; 71(11-12): 979-83, 2006 Nov.
Article in English | MEDLINE | ID: mdl-16973198

ABSTRACT

The microbial transformation of androst-4-ene-3,17-dione (I) by the fungus Beauveria bassiana CCTCC AF206001 has been investigated using pH 6.0 and 7.0 media. Two hydroxylated metabolites were obtained with the pH 6.0 medium. The major product was 11alpha-hydroxyandrost-4-ene-3,17-dione (II) whereas the minor product was 6beta,11alpha-dihydroxyandrost-4-ene-3,17-dione (III). On the other hand, four hydroxylated and/or reduced metabolites were obtained with the pH 7.0 medium. The major product was 11alpha,17beta-dihydroxyandrost-ene-3-one (V) and the minor products were 17beta-hydroxyandrost-ene-3-one (IV), 6beta,11alpha,17beta-trihydroxyandrost-ene-3-one (VI) and 3alpha,11alpha,17beta-trihydroxy-5alpha-androstane (VII). The products were purified by chromatographic methods, and were identified on the basis of spectroscopic methods. This fungus strain is clearly an efficient biocatalyst for 11alpha-hydroxylation and reduction of the 17-carbonyl group.


Subject(s)
Androstenedione/metabolism , Beauveria/metabolism , Androstenedione/chemistry , Animals , Molecular Structure
16.
Carbohydr Polym ; 154: 1-7, 2016 Dec 10.
Article in English | MEDLINE | ID: mdl-27577889

ABSTRACT

This paper addressed the application of hydroxyethyl pachyman (HEP) as a novel matrix for sustained - release tablets, using diclofenac sodium (DS) as a model drug. The studies showed the HEP tablets prepared by wet granulation had much slower drug release as compared to those prepared by direct compression. Meanwhile, increasing the percentage of HEP in the formulations caused a decrease in drug release rates. Moreover, DS release from the HEP tablets was much higher at high pH (6.8) than that at low pH (1.2). Morphology studies proved the HEP tablet formed a continuous gel layer with porous inner structure in the dissolution media. Analysis of DS release profiles revealed that diffusion and matrix erosion occurred in simulated intestinal fluid(SIF, pH=6.8) for all the tablets. The experimental results predict HEP has a potential as a hydrophilic matrix in tablets to prolong drug release.


Subject(s)
Excipients/chemistry , Glucans/chemistry , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Delayed-Action Preparations/chemistry , Diclofenac/chemistry , Drug Liberation , Hydrogen-Ion Concentration , Hydrophobic and Hydrophilic Interactions , Tablets
17.
Chem Biol Drug Des ; 87(5): 773-83, 2016 May.
Article in English | MEDLINE | ID: mdl-26684806

ABSTRACT

Neuromuscular blocking agents are widely used as an anesthesia auxiliary in surgery, which induce relaxation of skeletal muscles by blocking signal transmission at the neuromuscular junction. Many neuromuscular blocking agents s were developed over the past decades, but none of them fully meets the needs of the clinic by various reasons. In this study, a series of quaternary ammonium steroidal neuromuscular blocking agents were synthesized and evaluated on isolated mouse phrenic nerve-hemidiaphragms for their bioactivities. The initial separation of mono- and bis-quaternary ammonium compounds turned out to be very challenging on regular silica gel chromatography. Therefore, a facile purification method, in which the silica gel was pretreated with methanolic sodium bromide solution, was finally achieved. Compounds 3g (0.36 µm) and 4g (0.37 µm) exhibited excellent neuromuscular blocking activities, which were about sixfold to sevenfold higher in potency than that of rocuronium (2.50 µm). In addition, other bis-quaternized compounds also showed good potencies close to that of rocuronium. Furthermore, the preliminary structure-activity relationship of this series was also elucidated. Benzyl group was found to be a promising quaternary group in this series.


Subject(s)
Ammonium Compounds/pharmacology , Neuromuscular Blocking Agents/pharmacology , Steroids/pharmacology , Magnetic Resonance Spectroscopy , Spectrometry, Mass, Electrospray Ionization
18.
Article in English | MEDLINE | ID: mdl-16463690

ABSTRACT

Data communication and sharing of five level network of Public Health Information System, i.e. nation, province, district (city), county, and town, as far as to the countryside level were described, and how to apply the three solutions, i.e. Access VPN, Intranet VPN, and Extranet VPN of VPN technique to achieve the appropriation of the public network was also presented.


Subject(s)
Computer Communication Networks/organization & administration , Public Health Informatics/methods , User-Computer Interface , China , Humans
19.
Yao Xue Xue Bao ; 40(9): 825-9, 2005 Sep.
Article in Zh | MEDLINE | ID: mdl-16342685

ABSTRACT

AIM: Nucleoside analogues have become the most promising candidates of anti-HBV drugs. In this study, beta-L-D4A was synthesized and explored its inhibitiory action against hepatitis B virus (HBV) in 2. 2. 15 cells derived from HepG2 cells transfected with HBV genome. METHODS: beta-L-D4A was stereo-controlled synthesized from D-glutamic acid, and the structure was identified by IR, 1H NMR and MS. 2. 2. 15 Cells were placed at a density of 5 x 10(4) per well in 12-well tissue culture plates, and treated with various concentrations of beta-L-D4A for 6 days. At the end, medium was processed to obtain virions by a polyethlene glycol precipitation method. At the same time, intracellular DNA was also extracted and digested with Hind III. Both of the above DNA were subjected to Southern blot, hybridized with a 32P-labeled HBV probe and autoradiographed. The intensity of the autoradiographic bands was quantitated by densitometric scans of computer and EC50 was calculated. 2. 2. 15 cells were also seeded in 24-well tissue culture plates, and cytotoxicity with different concentrations was examined by MTT method. IC50 was calculated. RESULTS: The synthesized compound structure conformed with beta-L-D4A; Autoradiographic bands showed similar for supernatant and intracellular HBV DNA. Episomal HBV DNA was inhibited in a dose-dependent manner. EC50 0.2 micromol x L(-1). The experiment of cytotoxicity gained IC50 200 micromol x L(-10. CONCLUSION: beta-L-D4A has been synthesized successfully. beta-L-D4A possessed potent inhibitory effect on replication of HBV in vitro with low cytotoxicity, TI value was 1 000. It is expected to be developed clinically into a new anti-HBV drug.


Subject(s)
Antiviral Agents/chemical synthesis , Dideoxyadenosine/analogs & derivatives , Hepatitis B virus/drug effects , Virus Replication/drug effects , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Cell Line, Tumor , Cell Proliferation/drug effects , DNA Replication/drug effects , DNA, Viral/drug effects , Dideoxyadenosine/chemical synthesis , Dideoxyadenosine/chemistry , Dideoxyadenosine/pharmacology , Genome, Viral , Hepatitis B virus/genetics , Hepatitis B virus/physiology , Humans , Liver Neoplasms/pathology , Transfection
20.
Drug Des Devel Ther ; 9: 791-8, 2015.
Article in English | MEDLINE | ID: mdl-25709403

ABSTRACT

BACKGROUND: A novel lovastatin (LVT)-loaded poly(lactic acid) microsphere suitable for oral administration was developed in this study, and in vitro and in vivo characteristics were evaluated. METHODS: The designed microspheres were obtained by an improved emulsion-solvent evaporation method. The morphological examination, particle size, encapsulation ratio, drug loading, and in vitro release were characterized. Pharmacokinetics studies were used to show that microspheres possess more advantages than the conventional formulations. RESULTS: By using the emulsion-solvent evaporation method, it was simple to prepare microspheres and easy to scale up production. The morphology of formed microspheres showed a spherical shape with a smooth surface, without any particle aggregation. Mean size of the microspheres was 2.65±0.69 µm; the encapsulation efficiency was 92.5%±3.6%, and drug loading was 16.7%±2.1%. In vitro release indicated that the LVT microspheres had a well-sustained release efficacy, and ex vivo studies showed that after LVT was loaded to microspheres, the area under the plasma concentration-time curve from zero to the last measurable plasma concentration point and the extrapolation to time infinity increased significantly, which represented 2.63-fold and 2.49-fold increases, respectively, compared to suspensions. The rate of ex vivo clearance was significantly reduced. CONCLUSION: This research proved that poly(lactic acid) microspheres can significantly prolong the drug circulation time in vivo and can also significantly increase the relative bioavailability of the drug.


Subject(s)
Drug Delivery Systems , Lactic Acid/administration & dosage , Lovastatin/administration & dosage , Microspheres , Polymers/administration & dosage , Administration, Oral , Animals , Biological Availability , Drug Stability , Lactic Acid/chemistry , Lactic Acid/pharmacokinetics , Lovastatin/chemistry , Lovastatin/pharmacokinetics , Molecular Conformation , Particle Size , Polyesters , Polymers/chemistry , Polymers/pharmacokinetics , Rats , Surface Properties
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