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.

ObjectiveTo investigate the effects of mefformin on the levels of serum retinol-binding protein 4 (RBP-4),high sensitive C reactive protein (hs-CRP) and tumor necrosis factorα (TNF-α) in patients with impaired glucose tolerance(IGT) and metabolic syndrome(MS). MethodsSixty patients with IGT and MS were divided into mefformin treatment group (30 cases) and life-style intervention group (30 cases) by random digits table. Body mass index (BMI),the levels of HbAic, HOMA-IR, blood fat, RBP-4,hs-CRP, TNF- α were measured both before and 16 weeks after treatment in the two groups and compared.ResultsThe levels of HbA1c, HOMA-IR, RBP-4, hs-CRP and TNF- α were significantly lower in mefformin treatment group than those in life-style intervention group [(5.09 + 0.26 )％ vs. (5.69 ± 0.49 )％, 2.95 ± 0.63vs. 3.49 ± 0.78, ( 18.69 ± 6.50) mg/L vs.(26.20 ± 6.97) mg/L, (2.37 ± 0.53) mg/L vs.(2.99 ± 0.57) mg/L,(9.49 ± 2.37) μ g/L vs. ( 14.33 ± 2.62) μ g/L] (P ＜ 0.01 ). The results of multiple linear regression showed that correlations were found between the changes of RBP-4 and BMI,HOMA-IR,hs-CRP,TNF-α(β =0.284,0.506,0.274,0.230,P ＜0.01 ),and HOMA-IR was the most important limiting factor. Conclusions Mefformin can improve insulin sensitivity of the patients with IGT and MS, and depress the levels of RBP-4,hs-CRP and TNF- α. Meanwhile mefformin has anti-inflammatory effect.

Human sTNFR1 (soluble tumor necrosis factor receptor 1) gene was amplified by RT-PCR from Hela cells. A recombinant expression vector of sTNFR1-MBP was constructed in pMAL-c2x, and transformed into E. Coli JM109.It was sequenced and confirmed to be identifical to the sTNFR1 gene in data bank. Recombinant protein sTNFR1-MBP was induced by IPTG and purified by Amylose resin Affinity Chromatography. sTNFR1-MBP was binded to sTNFR1's antibody in Western-blotting. From MTT assays, the results showed that sTNFR1-MBP could effectively block the cytotoxicity mediated by TNF?on QSG7701 cells. Annexin V-FITC staining and flowcytometry were used to observe the recombinant protein's anti-apoptosis capacity and the recombinant protein has marked anti-apoptosis effect in vitro.sTNFR1-MBP had good biological activity and it will be employed in further study.

Objective:To investigate the clinical characteristics of patients infected with Brucella Melitensis ( B. Melitensis) type 1 and type 3 in Hulunbuir, Inner Mongolia Autonomous Region. Methods:A retrospective analysis method was used to collect clinical medical records of patients with brucellosis admitted to Hulunbuir People's Hospital from June 2013 to August 2017, and 71 patients with brucellosis positive in blood culture and identified by polymerase chain reaction (PCR) and AMOS-PCR were selected as the study subjects. According to the identification results, they were divided into B. Melitensis type 1 and type 3 groups. General information, epidemiological characteristics, clinical characteristics, laboratory examinations, complications and efficacy of the two groups were compared. Results:Among 71 patients with brucellosis, 22 cases were B. Melitensis type 1, including 16 males and 6 females, aged (39.91 ± 16.04) years old; 49 cases were B. Melitensis type 3, including 34 males and 15 females, aged (40.67 ± 18.72) years old. There were no significant differences in gender composition and age between the two groups (χ 2 = 0.081, t = 0.166, P > 0.05). There were 10 cases(45.5%) of B. Melitensis type 1 patients living in agricultural areas, 10 cases (45.5%) in pastoral areas, and 2 cases (9.1%) in cities; there were 40 cases (81.6%) of B. Melitensis type 3 patients living in agricultural areas, 7 cases (14.3%) in pastoral areas and 2 cases (4.1%) in cities, and the difference between regions was statistically significant (χ 2 = 9.276, P < 0.05). Testicular swelling and pain symptoms [22.7% (5/22), 6.1% (3/49)] in B. Melitensis type 1 and type 3 patients were compared, the difference was statistically significant (χ 2 = 4.187, P < 0.05); other clinical features were compared, the differences were not statistically significant ( P > 0.05). There were no significant differences in white blood cell count (WBC) and platelet count (PLT) decreased, erythrocyte sedimentation rate (ESR), C-reactive protein (CRP), alanine aminotransferase (ALT) and aspartate aminotransferase (AST) increased between the two groups ( P > 0.05). The number of complications in B. Melitensis type 1 and type 3 patients were 12 cases (54.5%) and 14 cases (28.6%), respectively, and the difference between the two groups was statistically significant (χ 2 = 4.413, P < 0.05). Ten cases (45.5%) of B. Melitensis type 1 patients were cured, 12 cases (54.5%) were improved, 34 cases (69.4%) of B. Melitensis type 3 patients were cured, 15 cases (30.6%) were improved, and there were no invalid or relapsed patients in both groups, the difference in curative effect between the two groups was statistically significant (χ 2 = 3.690, P < 0.05). Conclusions:In Hulunbuir, Inner Mongolia Autonomous Region, there are differences in the living areas of B. Melitensis type 1 and type 3 patients. The B. Melitensis type 1 patients are prone to testicular swelling and pain and brucellosis complications.

Objective To study the balance function of normal persons and to explore the differences in gender and age groups.Methods Forty parameters of 445 normal persons(16-70 years old, 205 of male, 240 of female ) were detected by static posturography while they were in seat, double foot standing with opening and closing eyes, and single foot standing with opening eyes. The results of male and female, standing with opening eyes and closing eyes, left foot standing and right foot standing were compared.Results Everyone's center of gravity was distributed in A zone while they were in seat. At standing with opening eyes and closing eyes, the center of gravity in A zone were in 429 subjects( 96.4%) and 436 subjects( 98.0%). Most parameters showed significant difference between the women and the men, opening eyes and closing eyes, left foot standing and right foot standing, different age groups. The stability in closing eyes was better than that in opening eyes, right foot standing was better than left foot standing. Most values of 20—39 years old group were the best, 70—79 years old group were the worst.Conclusion Static posturography can evaluate human balance function objectively and quantitatively. The stability is related to age and gender. To judge the balance function, the subject's age and sex must be taken into account.

As an important part of Chinese medicinal materials, uncommon-territorial herbs are also the most complex parts in the herbal medicine markets. Through years of investigation on the key markets of Chinese herbal medicine, the meaning of uncommon-territorial herbs, their historical evolution, origin and characteristics were clarified in this paper, and some countermeasures were put forward for its development.
Biological Evolution ; China ; Drugs, Chinese Herbal ; chemistry ; history ; Herbal Medicine ; history ; History, 20th Century ; History, 21st Century ; History, Ancient ; Medicine, Chinese Traditional ; history ; Plants, Medicinal ; chemistry ; growth & development

OBJECTIVETo investigate the chemical constituents of effective part of Epimedium brevicornum.

METHODThe sample was extracted with ethanol and purified by macroporous resin. The structures were identified by HPLC-MS3 experiments.

RESULTNine compounds were identified from the effective part of E. brevicornum.

CONCLUSIONThe method is simple and rapid for the identification of the flavonoids from E. brevicornum.

Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Epimedium ; chemistry ; Flavonoids ; chemistry ; isolation & purification ; Molecular Structure ; Plants, Medicinal ; chemistry ; Reproducibility of Results

The preliminary metabolic profile of total diterpene acid (TDA) isolated from Pseudolarix kaempferi was investigated by using in vivo and in vitro tests. Pseudolaric acid C2 (PC2) was identified as the predominant metabolite in plasma, urine, bile and feces after both oral and intravenous administrations to rats using HPLC-UV and HPLC-ESI/MS(n), and demethoxydeacetoxypseudolaric acid B (DDPB), a metabolite proposed to be the glucoside of PC2 (PC2G), as well as pseudolaric acid C (PC), pseudolaric acid A (PA), pseudolaric acid A O-beta-D glucopyranoside (PAG), pseudolaric acid B O-beta-D glucopyranoside (PBG) and deacetylpseudolaric acid A (DPA) originated from TDA could also be detected. It was demonstrated by tests that the metabolism of TDA is independent of intestinal microflora, and neither of pepsin and trypsin is in charge of metabolism of TDA, TDA is also stable in both pH environments of gastric tract and intestinal tract. The metabolites of TDA in whole blood in vitro incubation were found to be PC2, DDPB and PC2G, which demonstrated that the metabolic reaction of TDA in vivo is mainly occurred in blood and contributed to be the hydrolysis of plasma esterase to ester bond, as well as the glucosylation reaction. These results clarified the metabolic pathway of TDA for the first time, which is of great significance to the in vivo active form and acting mechanism research of P. kaempferi.
Animals ; Chromatography, High Pressure Liquid ; Diterpenes ; metabolism ; Glucosides ; metabolism ; Hydrolysis ; Mass Spectrometry ; Metabolic Networks and Pathways ; Pinaceae ; chemistry ; Rats

Adult ; China ; Genes, Viral ; Genotype ; Hepacivirus ; genetics ; Hepatitis C ; virology ; Humans ; Methadone ; therapeutic use ; Middle Aged ; Opioid-Related Disorders ; virology

Recombination plasmid pMM085 possessed both immunogens heat-labile enterotoxin(LT) and fimbriae antigen K88 of enterotoxigenic Escherichia coli (ETEC). Althouth vaccine strain MM-3 carrying pMM085 had good effect to protect piglets against diarrhea due to ETEC infections,it was not ideal live vaccine for pMM085 bringing chloramphenicol resistance gene (cat). To solve the problem,the host-plasmid balanced lethal system was introduced which including the replacement of cat gene by asd gene and transformation the new plasmid to the strain X6097 which asd gene was knocked out in its chromosome. Considering pMM085 was a big plasmid (23kb) and traditional genetic manipulations was not easy to carry on,?-Red recombination system was adopt in this work to realize the replacement of cat gene by asd gene. The results indicated that ?-Red recombination system was convenient and efficient to reconstruct big plasmid.