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.

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

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

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.

Atrial Fibrillation ; etiology ; Humans ; Recurrence ; Sleep Apnea, Obstructive ; complications

OBJECTIVETo observe the clinical effect of indwelling the anterior urethral stent in the treatment of anterior urethral stricture.

METHODSWe included 38 patients with anterior urethral stricture in the treatment group, and another 38 in the control, the former treated by indwelling the anterior urethral stent, and the latter by urethral dilatation. Then we analyzed the clinical results by comparing the Qmax, urinary hesitancy and numbers of urethral dilations between the two groups.

RESULTSCompared with the controls, the patients of the treatment group showed an obvious increase in Qmax, a significant decrease in the number of urethral dilatations, and a marked improvement of the quality of life. Six months after the stent removal, there were significantly more patients with Qmax > 15 ml/s in the treatment group than in the control (P < 0.05).

CONCLUSIONIndwelling the anterior urethral stent is a desirable option for the treatment of anterior urethral stricture, which is simple, safe, effective and reliable, and can be applied to general clinical practice.

Adolescent ; Adult ; Aged ; Child ; Child, Preschool ; Humans ; Male ; Middle Aged ; Stents ; Treatment Outcome ; Urethra ; surgery ; Urethral Stricture ; surgery

Catheter Ablation ; Child ; Heart Septal Defects, Atrial ; surgery ; Humans ; Imaging, Three-Dimensional ; Male ; Tachycardia, Supraventricular ; surgery ; Tomography, X-Ray Computed

OBJECTIVETo investigate the influence of persistent rapid atrial pacing on the levels of connexin 43 (Cx43) and type III collagen in pulmonary vein and atrium in a canine model.

METHODSSixteen mongrel dogs were divided into rapid atrial pacing (RAP) group (n = 8) and normal control group (n = 8) randomly. In the RAP group, atrial pacing was performed with a rate of 400 bpm for 10 weeks to establish atrial fibrillation model. The tissues of left superior pulmonary vein (LSPV), left atrial free wall (LAFW) and right atrial appendage (RAA) were collected from each dogs. The levels of Cx43 and type III collagen were measured in each tissue.

RESULTSTen weeks later, persistent atrial fibrillation was induced in all dogs in RAP group. The level of Cx43 in RAP group was higher than that in normal control group (LSPV: 3370.91 +/- 275.11 vs 1405.82 +/- 90.38, P < 0.05; LAFW: 2448.68 +/- 272.10 vs 1467.12 +/- 147.93, P < 0.05, RAA: 2331.96 +/- 199.61 vs 1288.27 +/- 216.22, P < 0.05). The level of Cx43 in LSPV was higher than that in LAFW and RAA in RAP group, whereas the difference between LAFW and RAA was not significant in RAP group. The quantities of type III collagen in RAP group were higher than those in normal control group (LSPV: 3301.97 +/- 309.70 vs 1404.56 +/- 178.02, P < 0.05; LAFW: 2477.86 +/- 190.43 vs 1479.20 +/- 187.17, P < 0.05; RAA: 2045.92 +/- 139.43 vs 1417.07 +/- 139.43, P < 0.05). The quantities of type III collagen in LSPV was higher than those in LAFW and RAA in RAP group.

CONCLUSIONSPersistent rapid atrial pacing could increase the levels of Cx43 and type III collagen in pulmonary vein and atrium in a canine model of atrial fibrillation. The levels of Cx43 and type III collagen in pulmonary vein were higher than those in atrium. This findings indicated that pulmonary vein may be a crucial regions in maintaining atrial fibrillation.

Animals ; Atrial Fibrillation ; metabolism ; physiopathology ; Cardiac Pacing, Artificial ; methods ; Collagen Type III ; blood ; Connexin 43 ; blood ; Disease Models, Animal ; Dogs ; Female ; Male ; Pulmonary Veins ; metabolism ; physiopathology