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1.
Org Lett ; 25(47): 8489-8494, 2023 Dec 01.
Article in English | MEDLINE | ID: mdl-37966853

ABSTRACT

A new electrophilic trifluoromethylselenolation reagent, N-trifluoromethylselenophthalimide (Phth-SeCF3), was developed. A strategy for the synthesis of 4-trifluoromethylselenolated isoxazoles through electrophilic trifluoromethylselenolation cyclization has been established by using Phth-SeCF3 as an electrophilic reagent. Moreover, this protocol has the features of broad substrate scope, good functional group tolerance, and high yields.

2.
Entropy (Basel) ; 25(7)2023 Jul 17.
Article in English | MEDLINE | ID: mdl-37510021

ABSTRACT

In this paper, we investigate an uncertainty diagram and Kirkwood-Dirac (KD) nonclassicality based on discrete Fourier transform (DFT) in a d-dimensional system. We first consider the uncertainty diagram of the DFT matrix, which is a transition matrix from basis A to basis B. Here, the bases A, B are not necessarily completely incompatible. We show that for the uncertainty diagram of the DFT matrix, there is no "hole" in the region of the (nA,nB) plane above and on the line nA+nB=d+1. Then, we present where the holes are in the region strictly below the line and above the hyperbola nAnB=d. Finally, we provide an alternative proof of the conjecture about KD nonclassicality based on DFT.

3.
Transl Cancer Res ; 12(2): 340-350, 2023 Feb 28.
Article in English | MEDLINE | ID: mdl-36915585

ABSTRACT

Background: To investigate the clinical and neuroimaging characteristics of leukoencephalopathy among children with acute lymphoblastic leukemia (ALL), especially after chemotherapy. Methods: Clinical data for 17 pediatric patients with leukoencephalopathy and 17 matched controls were retrospectively analyzed. All participants were children with ALL admitted to the Children's Hospital of Soochow University from May 2011 to April 2021. The data mainly consisted of general information, laboratory studies, and imaging diagnostic results. Results: Overall, 94.12% of the patients experienced neurological symptoms. The most common symptoms were seizure (7/17, 41.18%), nausea (5/17, 29.41%), vomiting (5/17, 29.41%), paralysis (5/17, 29.41%), and numbness (4/17, 23.53%). On neuroimaging, multiple and irregular lesions were observed, distributed mainly in the periventricular area (9/17, 52.94%), parietal lobe (6/17, 35.29%), and basal ganglia (5/17, 29.41%). Moreover, there were significant differences in serum sodium (P=0.0001), C-reactive protein (P=0.0124) and blood pressure (P=0.0271) between patients with and without leukoencephalopathy. After aggressive treatment, the clinical symptoms (12/17, 70.59%) and imaging lesions (11/13, 84.62%) gradually improved in most patients. Conclusions: Chemotherapy is an important risk factor related to leukoencephalopathy. Although the clinical symptoms of leukoencephalopathy vary widely, there is a high degree of consistency in its radiological features. Abnormal laboratory results may also help the identification of leukoencephalopathy. Early detection and treatment can improve brain development in the long term.

4.
Ying Yong Sheng Tai Xue Bao ; 34(1): 18-24, 2023 Jan.
Article in English | MEDLINE | ID: mdl-36799372

ABSTRACT

The variations in soil nitrification and denitrification processes, together with the abundances of functional microbes were investigated in Cunninghamia lanceolata plantations with different stand ages of 5, 8, 21, 27, and 40 years old. The results showed that the net nitrification rate fluctuated with increasing forest ages, with that of 8-year- and 27-year-old C. lanceolata plantations being significantly lower than other stand ages. The abundance of ammonia-oxidizing archaea (AOA) amoA in the 27-year-old plantation was significantly lower than that of the 40-year-old plantation, while there was no significant difference among the other stand ages. There was no significant difference in the abundance of AOB amoA gene, denitrifying functional genes or soil denitrification potential among different stand ages. The results of stepwise regression analysis showed that the abundance of AOA amoA gene was not significantly affected by soil physical and chemical properties. In addition, the abundance of AOB was positively associated with soil total carbon content and soil pH. The abundance of denitrifying functional genes including narG, nirK and nosZ increased with increasing soil pH. The abundance of nirK and nirS was influenced by soil total carbon. Stand age influenced soil net nitrification rate through the AOA amoA abundance. Moreover, soil denitrification potential was directly affected by stand age, or indirectly affected by stand age through soil microbial biomass carbon, soil pH and denitrifying gene abundance of narG and nirK. Compared with the denitrification process, soil nitrification and associated AOA amoA gene abundance were more sensitive to the development of C. lanceolata plantations. The rotation period sould be appropriately extended to reduce the risk of nitrogen losses resulting from soil nitrification.


Subject(s)
Cunninghamia , Nitrification , Soil/chemistry , Denitrification , Cunninghamia/genetics , Archaea/genetics , Ammonia , Carbon , Soil Microbiology , Oxidation-Reduction
5.
Transl Pediatr ; 11(9): 1502-1509, 2022 Sep.
Article in English | MEDLINE | ID: mdl-36247893

ABSTRACT

Background: Hand, foot, and mouth disease (HFMD) caused by coxsackievirus A6 (CV-A6) has become prevalent in many parts of the world. It is commonly referred to as atypical HFMD which more likely to present as bullous lesions. Compared with traditional HFMD, its misdiagnosis rate is relatively high, which brings difficulties to clinical diagnosis. We retrospectively analyze the clinical characteristics of children with HFMD with bullous lesions caused by CV-A6. Methods: The study included 68 children with atypical HFMD caused by CV-A6 who were hospitalized from 2018 to 2020. Data of the children including age, sex, month of HFMD onset, the morphologies and distribution of rashes, the details of fever, the presence or absence of onychomadesis, and laboratory test results were analyzed and compared between an infant group (<1 year), a toddler group (1-<3 years), and a preschool group (3-<6 years). Results: Of the 68 children, 67 were younger than 5 years old, with a male to female ratio of 1.62:1. The disease peaked in the period from June to September. With 75.0% of the infant group had more than three kinds of rashes; 95.0% of the preschool group had rashes in more than five locations. These differences were statistically significant (P<0.05). All children had fever. The peak fever in the toddler group was lower (P=0.033). No critical cases were observed in any of the groups. Of the 61 children who were successfully followed up, 68.9% developed onychomadesis within 2-3 weeks. The proportion of cases with abnormal liver function was 83.3%, 41.7%, and 10.0% in the infant, toddler, and preschool groups (P<0.001). The proportion of cases with increased serum creatine kinase MB isoenzyme (CK-MB) were significantly higher in the toddler group (P<0.05). Conclusions: Atypical HFMD caused by CV-A6 infection usually occurred in children under 5 years old. The morphologies of the rashes in the infant group changed more, while the rashes in the preschool group was more widely distributed. The incidence of critical cases was low. More than half of the cases can develop onychomadesis in the recovery period. Organ damage was relatively mild in the preschool group.

6.
J Org Chem ; 87(19): 13089-13101, 2022 10 07.
Article in English | MEDLINE | ID: mdl-36170059

ABSTRACT

A practical strategy for the synthesis of spiro[5.5]trienones-fused selenocyanates and spiro[4.5]trienones-fused selenocyanates through electrophilic selenocyanogen cyclization and dearomative spirocyclization is reported. This approach was conducted under mild conditions with broad substrate scope and good functional group tolerance. The utility of this procedure is exhibited in the late-stage functionalization of nature product and drug molecules.


Subject(s)
Spiro Compounds , Cyanates , Cyclization , Molecular Structure , Selenium Compounds , Spiro Compounds/chemistry
7.
Zhongguo Zhong Yao Za Zhi ; 47(13): 3481-3487, 2022 Jul.
Article in Chinese | MEDLINE | ID: mdl-35850799

ABSTRACT

The index weight coefficients were determined by comparing the analytic hierarchy process(AHP), the criteria importance through inter-criteria correlation(CRITIC), and the AHP-CRITIC mixed weighting method. The comprehensive scores of index components(echinacoside, salvianolic acid B, paeoniflorin, and ointment yield) of each group in the orthogonal test were compared to optimize the extraction process of Congrong Shujing Granules. The results showed that the AHP-CRITIC mixed weighting method scientifically optimized the extraction process. To be specific, the decoction pieces should be added with the 6-fold amount of water and extracted twice, 1 h each time. After three verification tests, the average mass fractions of echinacoside, salvianolic acid B, and paeoniflorin were 0.72, 9.34, and 5.92 mg·g~(-1), respectively, and the average ointment yield was 47.18%. As verified by the AHP-CRITIC mixed weighting method and the orthogonal test, the optimized extraction process of Congrong Shujing Granules was stable and feasible and could be applied to industrial production.


Subject(s)
Drugs, Chinese Herbal , Ointments , Water
8.
Front Neurol ; 13: 824268, 2022.
Article in English | MEDLINE | ID: mdl-35620787

ABSTRACT

Objective: In order to analyze the clinical characteristics of epileptic seizures in children with acute lymphoblastic leukemia (ALL) during treatment. Methods: The clinical and imaging data of children diagnosed as ALL with epilepsy seizures from January 2013 to December 2020 were retrospectively analyzed. Results: A total of 2217 children with ALL were admitted during the study, of whom 229 (10.33%) had epileptic seizures after ALL treatment. Among them, 45 (19.65%) were in the high-risk group and 184 (80.35%) were in the low-risk group. Epileptic seizures mainly occurred in the induction remission period (24.02%), maintenance treatment period (25.33%) and after bone marrow transplantation (21.40%). The common causes were MTX-related demyelinating encephalopathy (34.06%) and reversible posterior encephalopathy syndrome (PRES) (25.3%). The first symptom was mainly convulsion (34.50%). The first attack had a comprehensive attack and partial attack. Most patients stop themselves. 30 cases (13.10%) had acute recurrence of epilepsy (recurrence within 3 months after the first attack), and 49 cases (25.76%) had neurological dysfunction after follow-up. 36 cases developed symptomatic epilepsy. Among the 130 children who completed the follow-up, 78 (60.00%) had no obvious neurological sequelae, and 52 (40.0%) had neurological sequelae. Among the 52 cases, there were 34 cases of mild sequelae and 18 cases of severe sequelae, including 8 cases of epilepsy combined with cognitive impairment. Conclusion: Epileptic seizure is a common neurological complication during ALL treatment. The etiology and associated manifestations of the first epileptic seizure are diverse. Early neuroimaging and EEG examination are helpful for early diagnosis and treatment.

9.
Med Sci Monit ; 27: e931427, 2021 Aug 09.
Article in English | MEDLINE | ID: mdl-34366426

ABSTRACT

BACKGROUND Acute chemical liver injury needs to be further explored. The present study aimed to compare the effects of intraperitoneal injection with carbon tetrachloride on acute liver toxicity after 24 h in male and female Kunming mice. MATERIAL AND METHODS In this study, female and male mice were simultaneously divided into 3 different groups. Each group was treated differently, and after 24 h, blood samples were collected to check for changes in the activity of alanine aminotransferase (ALT) and aspartate aminotransferase (AST), which were used to assess liver toxicity. Liver samples were used for hematoxylin-eosin staining, and periodic acid Schiff reagent staining was performed to detect the pathological changes of each group. The expression level of biomarker molecules in liver cells was also systematically analyzed. RESULTS Our results showed that, compared with male mice, female mice showed more serious damage: reduced glycogen and higher degree of necrosis, and the levels of heatshock protein 27 (HSP27), heat-shock protein 70 (HSP70), proliferating cell nuclear antigen (PCNA) and B cell lymphoma/lewkmia-2 (Bcl-2) were significantly lower than in the male group (P<0.05 or P<0.01), while the results of Bcl-2-associated X protein (Bax), cysteinyl aspartate specific proteinase 3 (Caspase3), and cytochrome P450 2E1 (CYP2E1) were the opposite (P<0.05 or P<0.01). CONCLUSIONS The findings from this study showed that, compared with male mice, at 24 h after CCl4 toxicity, female mice showed more severe changes of hepatocyte necrosis and PAS-positivity, with significantly reduced expression of HSP27, HSP70, PCNA, and Bcl-2, and significantly increased expression of Bax, caspase-3, and CYP2E1.


Subject(s)
Carbon Tetrachloride Poisoning/diagnosis , Carbon Tetrachloride/toxicity , Chemical and Drug Induced Liver Injury/diagnosis , Animals , Carbon Tetrachloride/administration & dosage , Carbon Tetrachloride Poisoning/etiology , Carbon Tetrachloride Poisoning/pathology , Chemical and Drug Induced Liver Injury/etiology , Chemical and Drug Induced Liver Injury/pathology , Disease Models, Animal , Female , Hepatocytes/drug effects , Hepatocytes/pathology , Humans , Injections, Intraperitoneal , Liver/drug effects , Liver/pathology , Male , Mice , Necrosis/chemically induced , Necrosis/diagnosis , Severity of Illness Index , Sex Factors , Toxicity Tests, Acute/methods
10.
Res Vet Sci ; 139: 18-24, 2021 Oct.
Article in English | MEDLINE | ID: mdl-34229107

ABSTRACT

An experiment was conducted to investigate the effects of glutamine (Gln) on the lymphocyte proliferation and intestinal immune relevant gene expression in broilers infected with Salmonella Enteritidis. 240 1-day-old broilers were divided randomly into four groups in a completely randomized design, each of which had 6 replicates. Birds were reared in battery cages for 21 days. The experimental groups were as follows: control group (unchallenged group, CON), basal diet; Salmonella Enteritidis challenged group (challenged with 2.0 × 104 CFU/mL of Salmonella Enteritidis, SCC), basal diet; Gln 1, basal diet plus Salmonella Enteritidis challenged plus Gln at 0.5% diet; Gln 2, basal diet plus Salmonella Enteritidis challenged plus Gln at 1.0% diet. The results showed that Salmonella Enteritidis infection led to some decrease in the relative weight of spleen and bursa (except at 21 d), lymphocyte percentage, number of proliferation peripheral blood T and B lymphocytes, and increased the heterophil percentage, H/L ratio, mRNA expression levels of TNF-α, NF-κB p65, IL-1ß, IL-6, and IL-8 in the jejunal and ileal mucosa compared with the measurements of these parameters in the CON group at d 4, 7, 14, and 21 (p < 0.05). On the other hand, chickens fed the Gln showed improved the relative weight of spleen and bursa, increased the lymphocyte percentage, number of proliferation peripheral blood T and B lymphocytes, and decreased the heterophil percentage, H/L ratio, and immune relevant gene expression in the jejunal and ileal mucosa compared with the measurements of these parameters in the SCC group (p < 0.05). These results suggest that Gln as a feed additive could be effective for reducing the detrimental effects of Salmonella Enteritidis infection, and increase the intestinal immune barrier function of broilers.


Subject(s)
Dietary Supplements , Glutamine , Poultry Diseases , Salmonella Infections, Animal , Animal Feed/analysis , Animals , Cell Proliferation , Chickens , Diet/veterinary , Gene Expression , Glutamine/pharmacology , Lymphocyte Count , Poultry Diseases/drug therapy , Salmonella enteritidis
11.
Zhongguo Zhong Yao Za Zhi ; 46(10): 2481-2488, 2021 May.
Article in Chinese | MEDLINE | ID: mdl-34047094

ABSTRACT

The paclitaxel-loaded and folic acid-modified poly(lactic-co-glycolic acid) nano-micelles(PTX@FA-PLGA-NMs) were prepared by the emulsion solvent evaporation method, and the parameters of paclitaxel-loaded nano-micelles were optimized with the particle size and PDI as evaluation indexes. The morphology of the nano-micelles was observed by transmission electron microscopy(TEM), and the stability, drug loading and encapsulation efficiency were systematically investigated. In vitro experiments were performed to study the cytotoxic effects of nano-micelles, apoptosis, and cellular uptake. Under the optimal parameters, the nano-micelles showed the particle size of(125.3±1.2) nm, the PDI of 0.086±0.026, the zeta potential of(-20.0±3.8) mV, the drug loading of 7.2%±0.75%, and the encapsulation efficiency of 50.7%±1.0%. The nano-micelles were in regular spherical shape as observed by TEM. The blank FA-PLGA-NMs exhibited almost no inhibitory effect on the proliferation and growth of tumor cells, while the drug-loaded nano-micelles and free PTX exhibited significant inhibitory effects. The IC_(50) of PTX@FA-PLGA-NMs and PTX was 0.56 µg·mL~(-1) and 0.66 µg·mL~(-1), respectively. The paclitaxel-loaded nano-micelles were potent in inhibiting cell migration as assessed by the scratch assay. PTX@FA-PLGA-NMs had good pro-apoptotic effect on cervical cancer HeLa cells and significantly promoted the uptake of HeLa cells. The results of in vitro experiments suggested that PTX@FA-PLGA-NMs could target and treat cervical cancer HeLa cells. Therefore, as nanodrug carriers, PTX@FA-PLGA-NMs with anti-cancer activity are a promising nano-system for improving the-rapeutic effects on tumors.


Subject(s)
Antineoplastic Agents, Phytogenic , Uterine Cervical Neoplasms , Antineoplastic Agents, Phytogenic/pharmacology , Cell Line, Tumor , Drug Carriers , Female , Folic Acid , Glycolates , HeLa Cells , Humans , Micelles , Paclitaxel , Particle Size , Uterine Cervical Neoplasms/drug therapy
12.
Acta Pharmacol Sin ; 42(5): 832-842, 2021 May.
Article in English | MEDLINE | ID: mdl-33824461

ABSTRACT

Nanomedicine has attracted increasing attention and emerged as a safer and more effective modality in cancer treatment than conventional chemotherapy. In particular, the distinction of tumor microenvironment and normal tissues is often used in stimulus-responsive drug delivery systems for controlled release of therapeutic agents at target sites. In this study, we developed mesoporous silica nanoparticles (MSNs) coated with polyacrylic acid (PAA), and pH-sensitive lipid (PSL) for synergistic delivery and dual-pH-responsive sequential release of arsenic trioxide (ATO) and paclitaxel (PTX) (PL-PMSN-PTX/ATO). Tumor-targeting peptide F56 was used to modify MSNs, which conferred a target-specific delivery to cancer and endothelial cells under neoangiogenesis. PAA- and PSL-coated nanoparticles were characterized by TGA, TEM, FT-IR, and DLS. The drug-loaded nanoparticles displayed a dual-pH-responsive (pHe = 6.5, pHendo = 5.0) and sequential drug release profile. PTX within PSL was preferentially released at pH = 6.5, whereas ATO was mainly released at pH = 5.0. Drug-free carriers showed low cytotoxicity toward MCF-7 cells, but ATO and PTX co-delivered nanoparticles displayed a significant synergistic effect against MCF-7 cells, showing greater cell-cycle arrest in treated cells and more activation of apoptosis-related proteins than free drugs. Furthermore, the extracellular release of PTX caused an expansion of the interstitial space, allowing deeper penetration of the nanoparticles into the tumor mass through a tumor priming effect. As a result, FPL-PMSN-PTX/ATO exhibited improved in vivo circulation time, tumor-targeted delivery, and overall therapeutic efficacy.


Subject(s)
Antineoplastic Agents/therapeutic use , Arsenic Trioxide/therapeutic use , Breast Neoplasms/drug therapy , Drug Carriers/chemistry , Nanoparticles/chemistry , Paclitaxel/therapeutic use , Acrylic Resins/chemistry , Acrylic Resins/pharmacokinetics , Acrylic Resins/toxicity , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacokinetics , Apoptosis/drug effects , Arsenic Trioxide/pharmacokinetics , Breast Neoplasms/pathology , Cell Proliferation/drug effects , Cetrimonium/chemistry , Cetrimonium/toxicity , Drug Carriers/pharmacokinetics , Drug Carriers/toxicity , Drug Liberation , Female , G2 Phase Cell Cycle Checkpoints/drug effects , Human Umbilical Vein Endothelial Cells , Humans , MCF-7 Cells , Mice, Inbred ICR , Nanoparticles/toxicity , Oligopeptides/chemistry , Oligopeptides/pharmacokinetics , Oligopeptides/toxicity , Paclitaxel/chemistry , Paclitaxel/pharmacokinetics , Porosity , Silicon Dioxide/chemistry , Silicon Dioxide/pharmacokinetics , Silicon Dioxide/toxicity , Xenograft Model Antitumor Assays
13.
Ying Yong Sheng Tai Xue Bao ; 31(11): 3851-3858, 2020 Nov.
Article in Chinese | MEDLINE | ID: mdl-33300736

ABSTRACT

Investigating the response of soil microbial biomass and ecological stoichiometry to tree species transition is of great significance for understanding soil nutrient cycling and availability in forest ecosystems. We measured soil microbial biomass carbon (MBC), nitrogen (MBN), phosphorus (MBP) and their stoichiometry across 0-40 cm soil depth between Mytilaria laosensis and Cunninghamia lanceolata plantations by the chloroform fumigation extraction method, which were replanted after the harvest of C. lanceolata plantation. The results showed that soil MBC in the 0-10 cm layer and soil MBN and MBP in the 0-20 cm layer under the M. laosensis were significantly higher than those under the C. lanceolata. The MBC/MBP in the 0-20 cm layer and MBN/MBP in the 10-20 cm layer were significantly lower under the M. laosensis plantation. The MBC/MBN showed no significant differences between the two forests. Soil moisture, organic carbon, total nitrogen, total phosphorus, available phosphorus were positively correlated with MBC, MBN and MBP, but negatively correlated with MBC/MBP and MBN/MBP. Results of stepwise linear regression analysis showed that MBN and MBP were mainly affected by soil total nitrogen and available phosphorus, while MBC/MBP and MBN/MBP were mainly driven by available phosphorus and organic carbon, respectively. Our results indicated that tree species transition from C. lanceolata to M. laosensis could increase soil microbial biomass in the surface layers, accelerate soil nutrients turnover and enhance soil nutrient supply. The increases of MBP under M. laosensis indicate alleviation of soil phosphorus limitation for tree growth.


Subject(s)
Cunninghamia , Ecosystem , Soil , Soil Microbiology , Trees
14.
Epilepsy Behav ; 110: 107192, 2020 09.
Article in English | MEDLINE | ID: mdl-32580088

ABSTRACT

OBJECTIVE: Children with epilepsy exhibit a significantly higher risk for attention-deficit hyperactivity disorder (ADHD), which is often associated with lower quality of life. In this study, we aimed to identify molecular mechanisms associated with both epilepsy and ADHD. MATERIALS AND METHODS: Gene expression profiles of GSE12457 and GSE47752 were downloaded from the gene expression omnibus (GEO) database. Differentially expressed genes (DEGs) were separately screened in epilepsy and ADHD samples and compared with controls. Weighted gene coexpression network analysis (WGCNA) was used to identify candidate modules associated with the two disorders. Functional annotation and analysis of hub genes and molecular complex detection (MCODE) was also performed. RESULTS: Three modules closely related to epilepsy and ADHD were screened using WGCNA; DEGs in this module were involved in the synaptic vesicle cycle, axon and neuron regeneration, and neurotransmission. The Dlg4 and Vamp2 genes were selected as common candidate factors in epilepsy and ADHD pathogenesis. CONCLUSION: Dlg4 and Vamp2 could play essential roles in comorbidity between epilepsy and ADHD.


Subject(s)
Attention Deficit Disorder with Hyperactivity/genetics , Disks Large Homolog 4 Protein/genetics , Epilepsy/genetics , Protein Array Analysis/methods , Vesicle-Associated Membrane Protein 2/genetics , Attention Deficit Disorder with Hyperactivity/diagnosis , Attention Deficit Disorder with Hyperactivity/epidemiology , Child , Comorbidity , Epilepsy/diagnosis , Epilepsy/epidemiology , Female , Gene Regulatory Networks/genetics , Humans , Male
15.
Epilepsy Res ; 163: 106328, 2020 07.
Article in English | MEDLINE | ID: mdl-32283447

ABSTRACT

OBJECTIVE: Recurrent seizures can cause brain damage and affect the cognitive outcome, particularly in developing children. We aimed to determine the effects of recurrent seizures on the expression of gamma-aminobutyric acid A receptor (GABAAR) α1 and γ2 subunit and neurodevelopment in immature rats. The role of the GABAAR agonist clonazepam and antagonist/partial agonist flumazenil in seizure-induced brain injury was also studied. METHODS: Recurrent seizures (RS) were induced by flurothyl inhalation in immature rats. Clonazepam (CZP) and flumazenil (FMZ) were administered to modulate GABAAR subunit expression in different experimental groups. Neurobehavioral changes and GABAAR α1 and γ2 subunit expression were studied. RESULTS: Inhalation of flurothyl for five days triggered RS and caused reflex delay, inability to adapt to new environments in adulthood, and deficits in long-term learning and memory ability in rats. Down-regulation of GABAAR α1 and γ2 subunits occurred after seizure onset and persisted for a long time. CZP treatment decreased the expression of GABAAR α1 and γ2 subunits and delayed neurodevelopment of the immature rats, whereas FMZ did not show any significant effects. CONCLUSIONS: Changes in GABAAR α1 and γ2 subunit expression and neurodevelopment were related to recurrent seizures and administration of CZP. Thus, GABAAR α1 and γ2 subunits likely play a significant role in the development of immature rats with RS and provide a novel target for therapeutic intervention.


Subject(s)
Brain Injuries/drug therapy , Epilepsy, Generalized/drug therapy , Hippocampus/drug effects , Receptors, GABA-A/metabolism , Seizures/metabolism , Animals , Brain/drug effects , Brain/metabolism , Brain Injuries/metabolism , Epilepsy, Generalized/metabolism , Female , Flurothyl/pharmacology , Hippocampus/metabolism , Male , Rats, Wistar , Seizures/drug therapy , gamma-Aminobutyric Acid/metabolism , gamma-Aminobutyric Acid/pharmacology
16.
J Nat Prod ; 83(4): 1238-1248, 2020 04 24.
Article in English | MEDLINE | ID: mdl-32223193

ABSTRACT

Seven new daphnane-type diterpenoids, daphgenkins A-G (1-7), and 15 known analogues (8-22) were isolated from the flower buds of Daphne genkwa. Their structures and absolute configurations were elucidated by spectroscopic data and calculated ECD analyses. The cytotoxicities of all daphnane-type diterpenoids (1-22) obtained were evaluated against three human colon cancer cell lines (SW620, RKO, and LoVo). Compounds 1, 12, and 13 exhibited cytotoxic effects against the SW620 and RKO cell lines, with IC50 values in the range of 3.0-9.7 µM. The most active new compound, 1, with an IC50 value of 3.0 µM against SW620 cells, was evaluated further for its underlying molecular mechanism. Compound 1 induced G0/G1 cell cycle arrest, leading to the induction of apoptosis in SW620 cells. Also, it induced cancer cell apoptosis by an increased ratio of Bax/Bcl-2, activated cleaved caspase-3 and caspase-9, and upregulated PARP. Finally, compound 1 significantly inhibited PI3K/Akt/mTOR signaling in SW620 cells. Together, the results suggest that compound 1 may be a suitable lead compound for further biological evaluation.


Subject(s)
Antineoplastic Agents/pharmacology , Colonic Neoplasms/physiopathology , Daphne/chemistry , Diterpenes/pharmacology , Proto-Oncogene Proteins c-bcl-2/metabolism , TOR Serine-Threonine Kinases/metabolism , Antineoplastic Agents/chemistry , Antineoplastic Agents/isolation & purification , Apoptosis/drug effects , Caspase 3/chemistry , Caspase 3/metabolism , Cell Cycle Checkpoints/drug effects , Colonic Neoplasms/drug therapy , Diterpenes/chemistry , Diterpenes/isolation & purification , Humans , Molecular Structure , Phosphatidylinositol 3-Kinases/chemistry , Phosphatidylinositol 3-Kinases/metabolism , Proto-Oncogene Proteins c-akt/chemistry , Proto-Oncogene Proteins c-akt/metabolism , Proto-Oncogene Proteins c-bcl-2/chemistry , Signal Transduction/drug effects , TOR Serine-Threonine Kinases/chemistry
18.
J Synchrotron Radiat ; 26(Pt 6): 2075-2080, 2019 Nov 01.
Article in English | MEDLINE | ID: mdl-31721753

ABSTRACT

The upgrade of the laser pump time-resolved X-ray probes, namely time-resolved X-ray absorption spectroscopy (TR-XAS) and X-ray diffraction (TR-XRD), implemented at the Beijing Synchrotron Radiation Facility, is described. The improvements include a superbunch fill, a high-efficiency fluorescence collection, an efficient spatial overlap protocol and a new data-acquisition scheme. After upgrade, the adequate TR-XAS signal is now obtained in a 0.3 mM solution, compared with a 6 mM solution in our previous report. Furthermore, to extend application in photophysics, the TR-XAS probe is applied on SrCoO2.5 thin film. And for the first time, TR-XAS is combined with TR-XRD to simultaneously detect the kinetic trace of structural changes in thin film.

19.
Medicine (Baltimore) ; 98(29): e16460, 2019 Jul.
Article in English | MEDLINE | ID: mdl-31335704

ABSTRACT

BACKGROUND: Lumbar fusion is considered to the gold standard for treatment of spinal degenerative diseases but results in adjacent segment degeneration and acquired spinal instability. Total disc replacement is a relatively new alternative avoiding the occurrence of the above complications. The systematic review and meta-analysis was designed to evaluate whether total disc replacement exhibited better outcomes and safety. METHODS: PubMed, Web of Science, Embase, the Cochrane Library, Chinese National Knowledge Infrastructure Database(CNKI), Wangfang database, and VIP database were searched for RCTs comparing total disc replacement with lumbar fusion. All statistical analyses were carried out using the RevMan5.3 and STATA12.0 software. RESULTS: Of 1116 citations identified by our search strategy, 14 RCTs met the inclusion criteria. Compared to lumbar fusion, total disc replacement significantly improved ODI, VAS, SF-36, patient satisfaction, overall success, reoperation rate, ODI successful, reduced operation time, shortened duration of hospitalization, decreased postsurgical complications. However, total disc replacement did not show a significant difference regarding blood loss, consumption of analgesics, neurologic success and device success with lumbar fusion. And charges were significantly lower for total disc replacement compared with lumbar fusion in the 1-level patient group, while charges were similar in the 2-level group. CONCLUSION: Total disc replacement is recommended to alleviate the pain of degenerative lumbar diseases, improve the state of lumbar function and the quality of life of patients, provide a high level of security, have better health economics benefits for 1-level patients.


Subject(s)
Intervertebral Disc Degeneration/surgery , Lumbar Vertebrae/pathology , Spinal Fusion , Total Disc Replacement , Humans , Intervertebral Disc Degeneration/diagnosis , Randomized Controlled Trials as Topic , Spinal Fusion/adverse effects , Spinal Fusion/methods , Total Disc Replacement/adverse effects , Total Disc Replacement/methods , Treatment Outcome
20.
J Nanosci Nanotechnol ; 19(2): 956-962, 2019 02 01.
Article in English | MEDLINE | ID: mdl-30360179

ABSTRACT

The basic problems of the low dissolution rate of Tanshinone IIA (TSN) and the instability and precipitation of sodium tanshinone IIA sulfonate (STS) injection limit their usage in clinical. For these facts, the study aims to improve the dissolution rate of TSN and to enhance the sustained release effects of TSN and STS by using SBA-15 mesoporous molecular sieve as a drug carrier. Furthermore, controlling the pore size of SBA-15 and using different loaded methods to achieve expectations and provide a novel scheme for existing Danshen formulations. The effect of loading methods on drug loading efficiency (DL%), as well as the influence of the pore size of SBA-15s, the drug polarities and release mediums on drug loading and release behaviors were analyzed. It was found that the DL% was enhanced with the enlargement of the pore size, and was higher of TSN than STS. The in vitro tests of drug-loaded SBA-15s confirmed that the dissolution rate of TSN was improved obviously as compared with pure TSN. Moreover, SBA-15s prolonged the release times up to 12 h of TSN and 60 h of STS and promoted the sustained-release behaviors by decreasing the pore size. To ascertain the kinetic mechanisms of these samples, the Korsmeyer-Peppas release model was employed and the fitted results indicated that TSN/SBA-15s followed Fickian diffusion and non-Fickian transport was the predominant kinetic release mechanisms for STS/SBA-15s.

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