The pandemic of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has caused a serious impact on global public health and the economy. SARS-CoV-2 infiltrates host cells via its surface spike protein, which binds to angiotensin-converting enzyme 2 on the host cell membrane. As a result, small molecules targeting spike protein have emerged as a hotspot in anti-SARS-CoV-2 drug research. Activity screening is an important step in seeking small molecule drugs. Therefore, this article aims to review the biological activity evaluation methods of small molecule inhibitors targeting SARS-CoV-2 spike protein, with the goal of laying the foundation for the discovery of new anti-SARS-CoV-2 drugs.

Objective To establish a Real-time Taqman probe technique system to detect the mtDNA 1555A > G mutation in deaf population. Methods Primers and Taqman probes for mtDNA 1555A > G mutation were designed and synthesized. The technique system for detecting mtDNA 1555A > G mutation using Real-time Taqman probes was established. Then the reliability of the technique was tested in 132 patients with severe to profound hearing loss who were detected for the mtDNA 1555A > G mutation by sequencing, Kit method and Real-time Taqman probe technique at the same time. Finally, the results by the above three ways were compared. Results Thirty-two cases with mtDNA 1555A > G mutation were found by the technique of Real-time Taqman probe. These findings coincided with the results from sequencing and Kit method completely. Both the false positive rate and the false negative rate were zero. Conclusions The technique possesses the merits of accuracy, conveniency, high sensitivity, high specificity and intuitionistic results, etc. Importantly, the Real-time Taqman probe technique only needs 1.5 hours to detect the 1555A > G mutation and it saves 4. 5 hours for one reaction compared with the Kit method popularly used nowadays. The technique system of detecting mtDNA 1555A > G mutation is reliable. It's suitable for large-scale detecting and preventive diagnosis of mtDNA 1555A > G mutation.

OBJECTIVETo probe the function of interleukin-17 (IL-17) in rheumatoid arthritis (RA) patients of accumulated dampness-heat obstruction in joints syndrome (ADOJS) by detecting levels of IL-17 in serum and the synovial fluid and analyzing its correlation with erythrocyte sedimentation rate (ESR) and C reactive protein (CRP).

METHODSFrom January 2011 to January 2013, recruited were 90 RA inpatients of ADOJS at Department of Integrative Medical Rheumatism, General Hospital of Chengdu Military Region, of which 28 patients had knee joint effusion. Besides, 30 healthy volunteers who received physical examination at our hospital were recruited as the normal control group, and 30 patients with osteoarthritis (OA) who had knee joint effusion were recruited as the synovial fluid control group. The expression levels of IL-17 in serum and the synovial fluid were detected by enzyme linked immunosorbent assay (ELISA), and contents of ESR and CRP were detected in RA patients. Then correlation analyses were performed between levels of IL-17 and contents of ESR and CRP.

RESULTSCompared with the normal serum control group, the expression levels of IL-17 in serum of RA patients significantly increased (P < 0.05). Compared with the serum of RA patients and the synovial fluid of OA patients, the expression levels of IL-17 in the synovial fluid of RA patients significantly increased (P < 0.05). The expression levels of IL-17 in serum of RA patients were not correlated with ESR or CRP (r = 0.092, -0.082; P > 0.05), and the expressional levels of IL-17 in the synovial fluid of RA patients were not correlated with ESR or CRP (r = 0.113, -0.034; P > 0.05).

CONCLUSIONSIL-17 was the main effector cytokine of Th17 cells. The expressional levels of IL-17 significantly increased in serum and the synovial fluid of RA patients of ADOJS, but with no correlation to ESR or CRP. It indicated that IL-17 participated in the occurrence and development of RA. Concrete mechanisms needed to be further proved in larger samples.

Aged ; Arthritis, Rheumatoid ; blood ; diagnosis ; metabolism ; Blood Sedimentation ; C-Reactive Protein ; metabolism ; Case-Control Studies ; Female ; Humans ; Interleukin-17 ; blood ; metabolism ; Male ; Medicine, Chinese Traditional ; Middle Aged ; Synovial Fluid ; metabolism

OBJECTIVETo study the effect of bitter-cold herbs easing dampness method (BCHEDM) plus Sanhuang Yilong Decoction (SYD) combined with methotrexate (MTX) on expression levels of interleukin-1 (IL-1), IL-6, and IL-17 in rheumatoid arthritis (RA) patients of accumulated dampness-heat syndrome (ADHS).

METHODSFrom January 2011 to January 2013 recruited were 90 RA inpatients of ADHS at Department of Integrative Medicine on Rheumatoid Disease, General Hospital of Chengdu Military Region. They were assigned to the treatment group (45 cases) and the control group (45 cases) according to the random digit table produced by SPSS 11.5 Software. Patients in the treatment group were treated by heavy bitter-cold herbs plus SYD combined with MTX, while those in the control group were treated by MTX alone. Expressional levels of IL-1, IL-6, and IL-17 in serum were detected by enzyme linked immunosorbent assay (ELISA) before treatment, at week 2 and 4 after treatment. Erythrocyte sedimentation rate (ESR), C-reactive protein (CRP), and disease activity score in 28 joints (DAS28) were detected as well.

RESULTSAfter two or four weeks of treatment, ESR, CRP, and DAS28 decreased more in the treatment group than in the control group with statistical difference (P < 0.05, P < 0.01). After four weeks of treatment, IL-1, IL-6, IL-17, ESR, CRP, and DAS28 in the treatment group were all lower than before treatment and those of the control group at corresponding time points with statistical difference (P < 0.01).

CONCLUSIONSYD combined MTX could play roles of improving inflammatory indices within 2 weeks, and inhibiting the expression of IL-1, IL-6, and IL-17 within 4 weeks.

Arthritis, Rheumatoid ; blood ; drug therapy ; immunology ; Blood Sedimentation ; C-Reactive Protein ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Hot Temperature ; Humans ; Interleukin-1 ; blood ; Interleukin-17 ; blood ; Interleukin-6 ; blood ; Methotrexate ; therapeutic use ; Syndrome ; Treatment Outcome

AIMTo study the role of oxidative stress in the initiation and development of diabetic neuropathy.

METHODSThe diabetic rats were induced with streptozotocin (STZ). The malondialdehyde (MDA) level, total superoxide dismutase (SOD) and Na(+) -K(+) -ATPase activity were measured in the sciatic nerves at various stages of diabetes. The correlation of the MDA level and Na(+) -K(+) -ATPase activity was analyzed in diabetic rats. The pathological changes of sciatic nerve at diabetic various stages were examined by light microscopy.

RESULTSThe MDA level increased significantly in diabetic sciatic nerves as compared to controls at all time intervals. Total SOD activity increased significantly in diabetic sciatic nerves as compared to controls at one month of diabetes and progressively decreased at three/six months of diabetes. Na(+) -K(+) -ATPase activity progressively decreased at three/six months of diabetes. The correlation analysis indicated that the Na(+) -K(+) -ATPase activity was negative correlation with the MDA level in the diabetic rats. Histopathological study of the diabetic sciatic nerves showed that the pathological changes were observed at 3 months of diabetes, the changes were more serious as the diabetic duration was longer.

CONCLUSIONOxidative stress is found to occur during the early stages of STZ-induced diabetes (no neuropathy) and this state is maintained after initiation of neuropathy. The decreased Na(+) -K(+) -ATPase activity is associated with oxidative stress in the diabetic rats. Therefore, oxidative stress plays an important role in the initiation and development of diabetic neuropathy.

Animals ; Diabetes Mellitus, Experimental ; physiopathology ; Diabetic Neuropathies ; physiopathology ; Male ; Oxidative Stress ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Sciatic Nerve ; enzymology ; Sodium-Potassium-Exchanging ATPase ; metabolism ; Superoxide Dismutase ; metabolism

AIM To study the chemical constituents from Magnolia grandiflora L..METHODS The ethyl acetate fracion of 70％ acetone extract from M.grandiflora leaves was isolated and purified by silica,Sephadex LH-20 and MCI column,then the structures of obtained compounds were identified by spectral data.RESULTS Twelve compounds were isolated and identified as 10α-methoxyalloaromadendra-4β-ol (1),spathulenol (2),aromadendra-4β,10β-diol (3),aromadendra-4β,10α-diol (4),9-oxonerolidol (5),9-hydroxynerolidol (6),3,7-dimethylocta-1,5E-diene-3,7-diol (7),phytol (8),α-tocopherol (9),elemicin (10),syringaresinol (11),yangambin (12).CONCLUSION Compounds 1,3-6,8 are isolated from genus Magnolia for the first time,compounds 7,9,10,12 are first isolated from this plant.

OBJECTIVETo determine the effect of tension relaxation by small needle knife on the muscle tension and morphology changes of nerve terminals when sustained pressure was applied to muscular tissue.

METHODSRat gracilis muscles were exposed to pressure in vivo at 70 kPa for 2 hours. Sixty rats were divided into three groups: normal, control and experiment group respectively. In all rats except the six normal ones, the lower legs were considered as the control group, and the right left as experiment group. At day 1, 2 and 3, 9 rats from the two groups were randomly selected and sacrificed in order to determine the muscle tension change. At the same time, muscle histology and morphology changes of nerve terminals were observed.

RESULTSAbnormal tension increased in muscles under compression of 70 kPa. At the 1st and 2nd days, there were no significant differences between the two groups. Compared with control group, the tension was lower in experiment group, and there was statistically significant difference (P < 0.01) between the two groups. Exposure of striated muscle tissue to intensive and prolonged compression may pathologically alter its microstructure. Histological evaluation showed that this stiffening accompanied extensive necrotic damage. The changes could not be found in the nerve terminals.

CONCLUSIONDeep muscle tissue that undergoes prolonged compression may significantly increase its stiffness during acute injury. Tension relaxation applied by small needle knife can effectively reduce the mechanical load which is harmful to the whole tissue.

Animals ; Biomechanical Phenomena ; Female ; Male ; Medicine, Chinese Traditional ; Muscle Tonus ; Muscle, Skeletal ; innervation ; pathology ; physiology ; Nerve Endings ; pathology ; Pain Management ; Rats ; Rats, Sprague-Dawley

A phytochemical investigation on the stems of Garcinia bracteata collected from Xishuangbanna resulted in the isolation of a new flavone. By analysis of the HRESIMS, IR, UV, 1D and 2D NMR spectra, the structure of the new compound was determined as 7-methoxy-4',6-dihydroxy-8-isobutyryl-flavone(1). Compound 1 was also tested for its anti-tobacco mosaic virus(TMV) activity. Results suggested the 1 possessed remarkable anti-TMV activity, with an inhibition rate of 28.2%.
Antiviral Agents ; chemistry ; isolation & purification ; pharmacology ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Flavones ; chemistry ; isolation & purification ; pharmacology ; Garcinia ; chemistry ; Magnetic Resonance Spectroscopy ; Plant Leaves ; chemistry ; Tobacco Mosaic Virus ; drug effects ; growth & development

OBJECTIVETo introduce a method applied in computer aided design and computer aided manufacture (CAD-CAM) of removable partial denture framework for rehabilitating edentulous arch of Kennedy Class II and found a basis for this project.

METHODSPoint cloud data of dental stone model was obtained by laser scanning. The following processes were made: drawing framework outline on the reconstructed triangle mesh model, picking up and processing its inner side data as the data of tissue surface, shelling it for 3-D model of framework, and transferring the data to rapid prototyping equipment for manufacture.

RESULTS3-D model of the removable partial denture framework was preliminarily accomplished. The resin framework used as a sacrificial pattern was manufactured with the rapid prototyping equipment. The fit between resin framework and plaster model was good.

CONCLUSIONSThis method, as an integrated procedure including data acquisition, 3-D computer modeling and fabrication by rapid prototyping, is feasible to implement CAD-CAM of removable partial denture framework.

Computer-Aided Design ; Dental Casting Technique ; Dental Prosthesis Design ; methods ; Denture, Partial, Removable ; Imaging, Three-Dimensional

OBJECTIVESTo explore the effects of endotoxemia on gluconeogenesis in livers and kidneys during acute hepatic failure.

METHODTwenty-four healthy male SD rats were randomly divided into four groups (6 rats in each group) and all of them were injected intraperitoneally with solutions: group I with normal saline, group II with 400 mg/kg of D-galactosamine (D-GaLN), group III with 400 mg/kg of D-GaLN plus 50 microg/kg lipopolysaccharide(LPS), and group IV with 400 mg/kg of D-GaLN plus 500 microg/kg LPS. At 6 hours after the administration of different solutions intraperitoneally, blood samples were collected to examine blood urea nitrogen (BUN) and serum creatinine. Realtime PCR was used to study the expression of phosphoenolpyruvate carboxykinase (PEPCK) in the livers and kidneys.

RESULTSNo endotoxemia developed in group I or group II but it was evident in group III and group IV. The level of endotoxemia in group IV was higher than in group III (8.05+/-0.43, 3.50+/-2.25, P<0.05). After 6 hours of administration of LPS in group IV, hypoglycemia appeared, and blood glucose was normal in the other three groups. BUN and serum creatinine were all normal in the four groups, except that blood urea nitrogen was elevated in group IV. The mRNA of PEPCK in livers decreased gradually in all the four groups (2.54+/-1.32 vs 1.87+/-0.15 vs 0.91+/-0.13 vs 0.44+/-0.42, P<0.05). In the kidneys there was no change in the expression of PEPCK in group I and group II (0.75+/-0.03 and 0.77+/-0.04, P>0.05), but it increased in group III (0.75+/-0.03 vs 1.63+/-0.86, P<0.05), and decreased in group IV (0.75+/-0.03 vs 0.13+/-0.07, P<0.05).

CONCLUSIONDuring acute hepatic failure severe endotoxemia would damage the function of gluconeogenesis in livers and kidneys by inhibiting transcription of PEPCK and this can induce hypoglycemia.

Animals ; Endotoxemia ; metabolism ; Gluconeogenesis ; Kidney ; metabolism ; Liver ; metabolism ; Liver Failure, Acute ; metabolism ; Male ; Phosphoenolpyruvate Carboxykinase (GTP) ; metabolism ; Rats ; Rats, Sprague-Dawley