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Sesquiterpenoids are widely found in nature, while nitrobenzoyl sesquiterpenoids are relatively rare. Twelve natural nitrobenzoyl sesquiterpenoids were all derived from marine Aspergillus fungi, which are typical natural products with marine characteristics. These natural products exhibit good antitumor, antiviral, and inhibition of osteoclast differentiation activity, especially in the treatment of osteoclast-related diseases, showing good medicinal development value. This article reviews the natural product sources, chemical structure, chemical synthesis, biosynthesis, bioactivity, and pharmacological mechanisms of nitrobenzoyl sesquiterpenoids and predicts and discusses their absorption, distribution, metabolism, excretion, toxicity (ADME/T), and drug-likeness, providing a comprehensive understanding of the natural products of nitrobenzoyl sesquiterpenoids from marine sources and their potential for pharmaceutical development.
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Epilepsy is a common neurological disease,has the characteristics of recurrent attacks and long-term treatment,thus bringing great pressure to patients and their families.Therefore,it is particularly important to do a good job of disability assessment.In recent years,with the development of the discipline,academic organizations such as the International League Against Epilepsy(ILAE)and China Association Against Epilepsy(CAAE)have successively updated the definition and diagnostic criteria of epilepsy and seizures.However,some items of epilepsy in the current Criteria for Disability Rating of Military Personnel(Trial)issued by People's Liberation Army(PLA)in 2011 can no longer meet the latest guidelines at home and abroad.Therefore,we suggest that the items related to epilepsy in the Criteria for Disability Rating of Military Personnel(Trial)should be revised to ensure that the disability evaluation being completed fairly and successfully.
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Objective: To analyze the epidemiological characteristics of imported COVID-19 cases and the effect of vaccination on virus load and disease severity of the cases in Beijing. Methods: The data of the imported COVID-19 cases in Beijing were collected from the National Notifiable Infectious Disease Reporting System of China Information for Disease Control and Prevention and Epidemiology investigation. The data were processed and analyzed by Excel 2010 and SPSS 22.0. Results: From June 1 to September 30, 2021, a total of 171 imported COVID-19 cases were reported in Beijing, of which 66.67% (114/171) were asymptomatic. The cases were mainly from the Philippines, the United Arab Emirates, the United Kingdom and the Russian Federation, accounting for 67.84% (116/171). The male to female ratio of the cases was 2∶1 (114∶57). The median age M (Q1, Q3) of the cases was 28 (23, 36) years. The cases of Chinese accounted for 80.12% (137/171). The sequencing of the whole genome of the virus in 47 imported COVID-19 cases showed that the proportion of Delta variant was 76.60% (36/47). The COVID-19 vaccination coverage rate in the cases was 60.82% (104/171), but the full vaccination coverage rate was 53.80% (92/171). In the imported COVID-19 cases, 13.53% (23/170) were screened to be SARS-CoV-2 nucleic acid positive on the day when they arrived in Beijing, and all the cases were positive for 2019-nCoV nucleic acid within 28 days. The severity of the disease was higher in the unvaccinated group than in the partially vaccinated group and fully vaccinated group (P<0.001). In the unvaccinated group, there were 1 severe case and 1 critical case. The median Ct values M (Q1, Q3) of N gene and ORFlab gene in unvaccinated group were 32.51 (23.23, 36.06) and 32.78 (24.00, 36.38), respectively. There was no significant difference in the median of double-gene Ct value between the partially vaccinated group and the fully vaccinated group. Conclusions: During the study period, most of the imported COVID-19 cases in Beijing were asymptomatic. No matter vaccinated or not, the viral loads in the COVID-19 cases were similar, but the vaccination could reduce the severity of the disease.
Subject(s)
Female , Humans , Male , Beijing , COVID-19/epidemiology , COVID-19 Vaccines , Nucleic Acids , SARS-CoV-2ABSTRACT
Two new isomeric modified tripeptides, aspergillamides C and D (compounds 1 and 2), together with fifteen known compounds (compounds 3-17), were obtained from the marine sponge-derived fungus Aspergillus terreus SCSIO 41008. The structures of the new compounds, including absolute configurations, were determined by extensive analyses of spectroscopic data (NMR, MS, UV, and IR) and comparisons between the calculated and experimental electronic circular dichroism (ECD) spectra. Butyrolactone I (compound 11) exhibited strong inhibitory effects against Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) with the IC being 5.11 ± 0.53 μmol·L, and acted as a noncompetitive inhibitor based on kinetic analysis.
Subject(s)
Animals , 4-Butyrolactone , Chemistry , Pharmacology , Aspergillus , Chemistry , Chemistry Techniques, Analytical , Dipeptides , Chemistry , Pharmacology , Enzyme Inhibitors , Chemistry , Pharmacology , Indoles , Chemistry , Pharmacology , Molecular Structure , Mycobacterium tuberculosis , Peptides , Chemistry , Pharmacology , Polyketides , Chemistry , Pharmacology , Porifera , Microbiology , Protein Tyrosine Phosphatases , ChemistryABSTRACT
A new polyketide:3R, 5R-(-)-talaroflavone (2), along with 15 known compounds were isolated from a EtOAc extract of a sponge-derived fungus Alternaria sp. F49. Compounds 1-2 and 3-4 were separated as two pairs of enantiomers by chiral HPLC from Ⅰ and Ⅱ. The structures of compounds 1-16 were elucidated by means of NMR and MS. Furthermore, the absolute configurations of compounds 1-2 were determined by single crystal X-ray diffraction experiment and CD analyses. Compounds 6, 8-10 were isolated from this genus (Alternaria sp.) for the first time. Compound 16 showed moderate COX-2 enzyme inhibitory activity with IC50of 7.3 μmol·L-1.
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To investigate cytotoxic secondary metabolites of Micrococcus sp. R21, an actinomycete isolated from a deep-sea sediment (-6 310 m; 142 degrees 19. 9' E, 10 degrees 54. 6' N) of the Western Pacific Ocean, column chromatography was introduced over silica gel, ODS, and Sephadex LH-20. As a result, eight compounds were obtained. By mainly detailed analysis of the NMR data, their structures were elucidated as cyclo(4-hydroxy-L-Pro-L-leu) (1), cyclo(L-Pro-L-Gly) (2), cyclo( L-Pro-L-Ala) (3), cyclo( D-Pro-L-Leu) (4), N-β-acetyltryptamine (5), 2-hydroxybenzoic acid (6), and phenylacetic acid (7). Compound 1 exhibited weak cytotoxic activity against RAW264. 7 cells with IC50 value of 9.1 μmol x L(-1).
Subject(s)
Animals , Mice , Biological Factors , Chemistry , Metabolism , Pharmacology , Cell Survival , Macrophages , Cell Biology , Magnetic Resonance Spectroscopy , Mass Spectrometry , Micrococcus , Chemistry , Genetics , Metabolism , Molecular Structure , Phylogeny , Seawater , Microbiology , Secondary MetabolismABSTRACT
<p><b>OBJECTIVE</b>To study the nature of the residue hard tissue after liposuction in lipoma and its role in lipoma recurrence.</p><p><b>METHODS</b>The residue hard tissue after liposuction was collected for histologic study, including HE-staining and immunohistochemistry with antibody of stem cell marker (CD29 and CD44). The average density and area of positive cells were analyzed statistically.</p><p><b>RESULTS</b>The residue hard tissue had a medium hardness. The center tissue was light yellow surrounding by soft, loose, irregular and cord-like tissue. The normal fat tissue is light yellow with a soft and unanimous texture. HE-staining showed abundant stromas in residue hard tissue, with lots of fibroblast-like cells locating among adipocytes. The cytoplasm was less with large and blue-staining nucleus. In normal fat tissue, the fat cells were uniform which were round or polygon. The stromas was less and the fibroblast-like cells were comparatively less. The slices were stained with antibody (CD29, CD44) of stem cell marker. The density and area of positive cells were much more in residue hard tissue than those in normal adipose tissue. Two Independence Samples T test were as follows: (t'CD29 = 9.931, P = 0.000; (t'CD44 =10.171, P = 0.000 for density; and (t'CD29 = 7.761, P = 0.000; tt'CDRR = 6.639, P = 0.000 for area. The difference was significant.</p><p><b>CONCLUSIONS</b>Abundant fibroblast-like cells that are signed by the marker of stem cells exist in residue hard tissue. Those cells are proven to be lipoma derived stem cells (LDSCs) which may play an role in lipoma recurrence after lipoma liposuction.</p>
Subject(s)
Humans , Adipocytes , Cell Biology , Pathology , Adipose Tissue , Pathology , Lipectomy , Lipoma , Pathology , General Surgery , Recurrence , Stem Cells , PathologyABSTRACT
<p><b>OBJECTIVE</b>To compare the penetration abilities of resin infiltration into proximal lesions in primary molars with those of adhesive in vitro.</p><p><b>METHODS</b>Thirty-two extracted or exfoliated primary molars showing proximal white spot lesions were selected. Roots of the teeth were removed, and the crowns were cut across the white spot lesions perpendicular to the surface. Cut surfaces were examined (by stereo microscopy) and classified with respect to histological lesion extension (C1-C4): lesions confined to the outer half on enamel (C1), lesions confined to the inner half on enamel (C2), lesions confined to the outer half on dentin (C3), lesions extending into the inner half of dentin (C4). Corresponding lesion halves were etched for 120 s with 15% hydrochloric acid gel and were subsequently treated with either adhesive or resin infiltration. Specimens were observed with laser scanning confocal microscope (LSCM) in dual fluorescence mode. In confocal microscopic images, lesion depth and penetration depth of the resin infiltration or the adhesive in corresponding halves were measured, and penetration percentages were calculated respectively. Differences of the data between two groups were analyzed by Wilcoxon signed rank test. Variations of histological caries extensions were detected with Kruskal-Wallis H test.</p><p><b>RESULTS</b>At the same grading level (C1-C3) in histological caries extension, penetration depths of the resin infiltration group and the adhesive group were 240 (230, 260) µm vs 190 (150, 210) µm, 405 (300, 523) µm vs 180 (160, 200) µm, and 590 (430, 640) µm vs 180 (160, 200) µm respectively. There was significant statistical difference in the data between two groups (P < 0.05). Statistically significant difference in penetration depths of the resin infiltration group (at C1-C3) were found (P < 0.01). At the same grading level (C1-C3) in histological caries extension, percentage penetrations of the resin infiltration group and the adhesive group were [100.0% (96.2%, 100.0%)], [99.1% (95.7%, 100.0%)], [82.0% (81.1%, 92.2%)] and [79.2% (68.4%, 87.5%)], [41.8% (29.1%, 74.5%)], [30.2% (29.2%, 39.6%)], respectively. The difference between the above data was also significant (P < 0.05). Percentage penetrations of the resin infiltration group at C1 and C2 level was higher than those at C3 level (P < 0.05).</p><p><b>CONCLUSIONS</b>The resin infiltration is capable of penetrating almost completely into proximal lesions in primary molars.</p>
Subject(s)
Humans , Acid Etching, Dental , Methods , Composite Resins , Chemistry , Dental Caries , Pathology , Therapeutics , Dental Cements , Chemistry , Dental Enamel , Pathology , Dental Enamel Permeability , Hydrochloric Acid , Pharmacology , Molar , Pathology , Surface Properties , Tooth, Deciduous , PathologyABSTRACT
<p><b>OBJECTIVE</b>Continuous spike-and-wave during slow wave sleep (CSWS) syndrome is one of the presentations of electrical status epilepticus during sleep (ESES). The purpose of this study was to investigate the characteristics of CSWS syndrome in children.</p><p><b>METHODS</b>Between 2007 and 2009, a total of 778 nocturnal long-term or 24-hr video-EEG records were included. The EEG, clinical and neuroimaging characteristics were studied in children who met standard criteria for CSWS.</p><p><b>RESULTS</b>Nine children met standard criteria for CSWS in video-EEGs. Their ages ranged 6 to 13 years. Their EEGs were characterized by continuous spike-and-wave (SW) discharges during non-rapid eye movement (NREM) sleep, accounting for 85%-100% of the period of NREM sleep. Clinically, these children had various types of epileptic seizures and exhibited different degrees of neuropsychiatric impairments, language dysfunction, and/or behavioral disturbances. Neuroimaging abnormalities were found in 6 cases, including atelencephalia or atrophy, gray matter heterotopia and leucomalacia.</p><p><b>CONCLUSIONS</b>This study indicates the characteristics of CSWS syndrome in clinical manifestations, EEG and neuroimaging examinations. This will be helpful in understanding CSWS syndrome.</p>
Subject(s)
Adolescent , Child , Humans , Electroencephalography , Sleep , Physiology , Status Epilepticus , Diagnosis , Drug Therapy , SyndromeABSTRACT
In order to analyze the molecular epidemiology of A (H1N1) influenza virus in 2009, the complete genome sequences of influenza strains from different host sources downloaded from the NCBI were analyzed on genetic evolution by DNAstar software in this research. The results showed that 79 mutation sites of new A (H1N1) influenza virus were observed compared to previous human A (H1N1) influenza strain, including 14 mutation sites new in all A (H1N1) influenza sources and 37 mutation sites only observed in swine strain. A significant difference was represented in antigenic sites between new A (H1N1) influenza strain and the previous human A (H1N1) strain. This phenomenon shows the new A (H1N1) influenza strain is either originated from the recombination of human and swine strain or from the infection in pig populations and gradual mutation to human tansmission, which remains to be further studied.
Subject(s)
Animals , Humans , Birds , Databases, Nucleic Acid , Evolution, Molecular , Hemagglutinin Glycoproteins, Influenza Virus , Classification , Genetics , Influenza A Virus, H1N1 Subtype , Genetics , Influenza in Birds , Virology , Influenza, Human , Virology , Orthomyxoviridae Infections , Virology , Phylogeny , Swine , Swine Diseases , VirologyABSTRACT
<p><b>OBJECTIVE</b>To develop an HPLC-ELSD method for determination of vetatramine. in Veratrum nigrum.</p><p><b>METHOD</b>The analy fical column was Shim-pack ODS - C18 (4.6 mm x 250 mm, 4 microm) column, the mobile phase was acetonitrile-water (containing 0.1% triethylamine) (50:50), at a flow rate of 0.8 mL x min(-1). The temperature of drift tube was 90 degrees C and the gas flow was at the rate of 2.5 L x min(-1).</p><p><b>RESULT</b>The calibration curve was linear in the range of 0.36-3.6 microg (r = 0.999 8). The average recovery was 100.9% (RSD 2.3%, n = 6). The contents of veratramine in Veratrum nigrum. from the ten different sources were determined.</p><p><b>CONCLUSION</b>The method may be used as a accurate and reproducible way to determine the content of veratramine in V. nigrum.</p>
Subject(s)
Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Chemistry , Linear Models , Reproducibility of Results , Sensitivity and Specificity , Veratrum , Chemistry , Veratrum AlkaloidsABSTRACT
<p><b>OBJECTIVE</b>To investigate the clinical characteristics and analyze spastin gene mutation on a kindred with hereditary spastic paraplegia (HSP).</p><p><b>METHODS</b>All family members were studied through clinical examinations. The proband and another two patients in this kindred were subjected to electromyography (EMG) examinations. The proband was subjected to thoracic MRI examination too. Mutation analysis of spastin gene was screened by polymerase chain reaction combined with DNA sequencing in the proband and his father.</p><p><b>RESULTS</b>All patients in the kindred manifested as classical HSP. Thoracic MRI revealed atrophies of the spinal cord in the proband. No abnormal spastin gene mutation was detected in these two patients.</p><p><b>CONCLUSION</b>This kindred has typical clinical manifestations of HSP. The pathogenesis has no association with mutation of the exons of spastin gene.</p>
Subject(s)
Adult , Aged , Aged, 80 and over , Female , Humans , Male , Middle Aged , Young Adult , Adenosine Triphosphatases , Genetics , Base Sequence , DNA Mutational Analysis , Electromyography , Exons , Genetics , Family Health , Magnetic Resonance Imaging , Mutation , Pedigree , Polymerase Chain Reaction , Spastic Paraplegia, Hereditary , Genetics , Pathology , SpastinABSTRACT
<p><b>OBJECTIVE</b>To explore the clinical value of 64-slice spiral CT for spinal structure assessment in elderly patients with osteoporosis.</p><p><b>METHODS</b>The computed radiography (CR) films and 64-slice spiral CT isotropic scanning images of 40 patients who had been diagnosed as osteoporosis by dual-energy X-ray absorptiometry (DXA) were retrospectively analyzed. The patients were divided into two groups according to their T-scores by DXA: group A (T-score was -1.0 - (-2.5)); and B group (T-score was below -2.5).</p><p><b>RESULTS</b>The diagnostic results of axial CT images combined with multi-planar reconstruction (MPR) was negatively correlated with the measurement results of DXA in the diagnosis of spinal osteoporosis, and such correlation was higher in group B than in group A. Compared with CR films, axial CT images combining with MPR showed superior effectiveness in the diagnosis of osteoporosis.</p><p><b>CONCLUSIONS</b>64-slice spiral CT is better than CR in diagnosis of osteoporosis. CT-MPR and 3D reconstruction not only can be used to diagnose osteoporosis early, but also to observe the changes of skeleton's shape and overall structure.</p>
Subject(s)
Aged , Female , Humans , Male , Middle Aged , Image Processing, Computer-Assisted , Methods , Lumbar Vertebrae , Diagnostic Imaging , Pathology , Osteoporosis , Diagnostic Imaging , Retrospective Studies , Tomography, Spiral ComputedABSTRACT
Objective To find out the prevalence rate of epilepsy,its treatment gap and quality of life of epilepsy patients in rural areas of Tibet Autonomous Region (TAR).Methods Cluster sampling was adopted to conduct a door-to-door epidemiological survey among 14 822 rural population in Gangka town, Zhaxigang and Quzika village located in Medrogongka and Markham counties of TAR.The quality of life was measured by the 31-item quality of life in epilepsy inventory (QOLIE-31).Results Thirty-seven epilepsy patients were diagnosed as convulsive epileptic patients,and the prevalence was 0.25%.Thirty-five patients (94.59%) were diagnosed as active epilepsy,with a prevalence rate of 0.24%.Only one patient took standard Western Medicine within a week before the survey,and the treatment gap of the active epilepsy was 97.1%.The average QOLIE-31 total score was 42.15?17.63,and the lowest subcomponent score was 22.59?20.31 for seizure worry with the highest subcomponent score 85.83?18.59 for medication effects. Age,occupation,education,economic status,age at epilepsy onset and seizure frequency were significantly correlated with low QOLIE-31 scores (P