Medicinal chemistry strategies in seeking coronavirus inhibitors / 药学学报

The epidemic caused by coronavirus poses a serious threat to human health, but there is no specific drug or vaccine for the treatment of this kind of virus infection. Herein, this article selects typical case studies in recent years and reviews the medicinal chemistry strategies of anti-SARS-CoV, MERS-CoV and other coronavirus drugs from the perspective of medicinal chemistry, and tries to provide some clues to current drug research againstSARS-CoV-2.

Research on antitumor active components and mechanisms of natural products / 药学学报

Tumor, especially malignant tumor has become one of the major diseases, a serious threat to the health of people around the world. Modern clinical practice shows that the natural active products extracted from traditional Chinese medicine, marine medicine and other natural drugs, such as terpenes, alkaloids, polysaccharides, volatile oils and peptides, can effectively inhibit the growth of tumor cells. In this paper, the active components of natural antitumor products in recent years were summarized and their related mechanism was elucidated, so as to provide theoretical basis for the further development of natural antitumor drugs.

Exploration of the mechanisms of Ge Gen Decoction against influenza A virus infection / 中国天然药物

Ge Gen Decoction (GGD), a Traditional Chinese Medicine prescription, is mainly used to treat infectious respiratory diseases and can relieve the symptoms of influenza A virus (IAV) infection. However, the underlying mechanism of GGD against IAV infection remains unclear. In this study, we found that GGD had moderate anti-IAV activity in vitro. GGD was more effective when given before the viral infection and targeted the viral attachment and replication stages rather than the internalization stage. In vivo, GGD treatment reduced thevirus titers of lung tissue significantly and improved the survival rate, lung index, and pulmonary histopathological changes in H1N1-infected mice. We observed the changes in several key immuno-related indexes in GGD administrated H1N1-infected mice with anti-IAV drug oseltamivir phosphate as the control. GGD treatment decreased the expression of TNF-α and improved Th1/Th2 immune balance to reduce the excessive immune response in H1N1-infected mice. Besides, the expression of the toll-like receptor 7 signaling pathway in H1N1-infected mice decreased after GGD treatment. Our results showed that GGD has anti-IAV activity and can modulate the immune system to relieve lung inflammation.

Gut microbiota analysis and its significance in vasovagal syncope in children / 中华医学杂志(英文版)

BACKGROUND@#Vasovagal syncope (VVS) is common in children and greatly affect both physical and mental health. But the mechanisms have not been completely explained. This study was designed to analyze the gut microbiota in children with VVS and explore its clinical significance.@*METHODS@#Fecal samples from 20 VVS children and 20 matched controls were collected, and the microbiota were analyzed by 16S rRNA gene sequencing. The diversity and microbiota compositions of the VVS cases and controls were compared with the independent sample t test or Mann-Whitney U test. The correlation between the predominant bacteria and clinical symptoms was analyzed using Pearson or Spearman correlation test.@*RESULTS@#No significant differences in diversity were evident between VVS and controls (P > 0.05). At the family level, the relative abundance of Ruminococcaceae was significantly higher in VVS children than in controls (median [Q1, Q3]: 22.10% [16.89%, 27.36%] vs. 13.92% [10.31%, 20.18%], Z = -2.40, P  4, P < 0.05). The relative abundance of Ruminococcaceae in VVS patients was positively correlated with the frequency of syncope (r = 0.616, P < 0.01). In terms of its correlation with hemodynamics, we showed that relative abundance of Ruminococcaceae was negatively correlated with the systolic and diastolic pressure reduction at the positive response in head-up tilt test (HUTT; r = -0.489 and -0.448, all P < 0.05), but was positively correlated with the mean pressure drop and decline rate (r = 0.489 and 0.467, all P < 0.05) as well as diastolic pressure drop and decline rate at the HUTT positive response (r = 0.579 and 0.589, all P < 0.01) in VVS patients.@*CONCLUSION@#Ruminococcaceae was the predominant gut bacteria and was associated with the clinical symptoms and hemodynamics of VVS, suggesting that gut microbiota might be involved in the development of VVS.

Association between Nonalcoholic Fatty Liver Disease and Carotid Artery Disease in a Community-Based Chinese Population: A Cross-Sectional Study / 中华医学杂志(英文版)

<p><b>Background</b>Nonalcoholic fatty liver disease (NAFLD) is one of the most common chronic liver diseases with a high prevalence in the general population. The association between NAFLD and cardiovascular disease has been well addressed in previous studies. However, whether NAFLD is associated with carotid artery disease in a community-based Chinese population remained unclear. The aim of this study was to investigate the association between NAFLD and carotid artery disease.</p><p><b>Methods</b>A total of 2612 participants (1091 men and 1521 women) aged 40 years and older from Jidong of Tangshan city (China) were selected for this study. NAFLD was diagnosed by abdominal ultrasonography. The presence of carotid stenosis or plaque was evaluated by carotid artery ultrasonography. Logistic regression was used to analyze the association between NAFLD and carotid artery disease.</p><p><b>Results</b>Participants with NAFLD have a higher prevalence of carotid stenosis (12.9% vs. 4.6%) and carotid plaque (21.9% vs. 15.0%) than those without NAFLD. After adjusting for age, gender, smoking status, income, physical activity, diabetes, hypertension, triglyceride, waist-hip ratio, and high-density lipoprotein, NAFLD is significantly associated with carotid stenosis (odds ratio [OR]: 2.06, 95% confidence interval [CI]: 1.45-2.91), but the association between NAFLD and carotid plaque is not statistically significant (OR: 1.10, 95% CI: 0.8-1.40).</p><p><b>Conclusion</b>A significant association between NAFLD and carotid stenosis is found in a Chinese population.</p>

Endometrial MicroRNA Signature during the Window of Implantation Changed in Patients with Repeated Implantation Failure / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>At present, a diagnostic tool with high specificity for impaired endometrial receptivity, which may lead to implantation failure, remains to be developed. We aimed to assess the different endometrial microRNA (miRNA) signatures for impaired endometrial receptivity by microarray analysis.</p><p><b>METHODS</b>A total of 12 repeated implantation failure (RIF) patients and 10 infertile patients, who conceived and delivered after one embryo transfer attempt, were recruited as RIF and control groups, respectively. Endometrial specimens from the window of implantation (WOI) were collected from these two groups. MiRNA microarray was conducted on seven and five samples from the RIF and control groups, respectively. Comparative, functional, and network analyses were performed for the microarray results. Quantitative real-time polymerase chain reaction (PCR) was performed on other samples to validate the expression of specific miRNAs.</p><p><b>RESULTS</b>Compared with those in the control group, the expression levels of 105 miRNAs in the RIF group were found to be significantly up- or down-regulated (at least 2-fold) by microarray analysis. The most relevant miRNA functional sets of these dysregulated miRNAs were miR-30 family, human embryonic stem cell regulation, epithelial-mesenchymal transition, and miRNA tumor suppressors by tool for annotations of microRNA analysis. Network regulatory analysis found 176 miRNA-mRNA interactions, and the top 3 core miRNAs were has-miR-4668-5p, has-miR-429, and has-miR-5088. Expression levels of the 18 selected miRNAs in new samples by real-time PCR were found to be regulated with the same trend, as the result of microarray analysis.</p><p><b>CONCLUSIONS</b>There is a significant different expression of certain miRNAs in the WOI endometrium for RIF patients. These miRNAs may contribute to impaired endometrial receptivity.</p>

Advances in high-throughput transcriptome research of traditional Chinese medicines / 中国中药杂志

Traditional Chinese medicine is a treasure of Chinese culture, absorbing the wisdom of the Chinese people. Continuous application of new technologies makes traditional Chinese medicine research advance with the times. After several years of development, high-throughput transcriptome study has become a mature research tool in biology. This paper reviewed the advances in medicine transcriptome study, and compared two sequencing platforms, Roche's GS FLX platform and Illumina's HiSeq 2000 platform. Moreover, this paper introduced medicine transcriptome analysis process, with Panax quinquefolius and Lonicera japonica for examples, showing the characteristics of traditional Chinese medicine transcriptome studies. High-throughput transcriptome studies facilitate traditional Chinese medicine research with overall understand of functional genes, give clear elucidation of metabolic pathways, lay molecular foundation for the traditional Chinese medicine research and offer modern interpretation for traditional Chinese medicine theory. However, the current study faces several difficulties, including weak molecular basis, high sequencing cost and staff shortages in data anaysis. In the future, with the development in sequencing technology, the combination of transcriptome and other genomics, such as proteome and metabolome, will lay a solid foundation for the new high-throughput screening and developing model for the traditional Chinese medicine industry.

Effect of fluoride on expression of telomerase reverse transcriptase expression and proliferating cell nuclear antigen in germ cells of rats' testes / 中华劳动卫生职业病杂志

<p><b>OBJECTIVE</b>To study the damages of fluoride on the male reproductive system in rat testes.</p><p><b>METHODS</b>A total of 30 male SD rats were randomly divided into control group, high, low dose fluorine treated groups, which were given normal saline ,20 mg/kg sodium fluoride, and 10mg/kg sodium fluoride respectively. After 39 days the change of the weight of rats and the number of sperms were observed. The change of telomerase reverse transcriptase(TERT) and proliferating cell nuclear antigen (PCNA) were observed by using in situ hybridization and radioimmunoassay respectively.</p><p><b>RESULTS</b>The weight was (273.39 +/- 20.68), (240.00 +/- 21.39) g in NaF treated groups, which was lower than that in control group(P < 0.05); The rate of TERT expression in germ cells of testes in NaF treated groups was (13.89 +/- 4.86)% and (6.33 +/- 4.42)% respectively, which was significantly lower than that in control group (P < 0.05). The rate of PCNA expression in germ cells of tests in NaF treated groups was (0.71 +/- 0.05)%, (0.60 +/- 0.08)% respectively, which also was significant lower than that in control group(P < 0.05). The number of sperms was (18.31 +/- 1.20)10(10)/L, (9.17 +/- 1.38)10(10)/L, which was lower than that in control group (P < 0.05).</p><p><b>CONCLUSION</b>Fluorine possibly damages the male reproductive system by reducing the expression of TERT and PCNA.</p>

Finding potential ligands for PDZ domains by tailfit, a JAVA program / 中国医学科学杂志(英文版)

<p><b>OBJECTIVE</b>To deduce all potential ligands undiscovered experimentally by searching all the proteins containing same C-termini, which can bind a certain PDZ domain.</p><p><b>METHODS</b>We developed a JAVA program for searching short exact sequence matches at C-terminus. According to the known C-termini, which PDZ domains recognized experimentally, Swissprot database has been searched by this program for all potential ligands.</p><p><b>RESULTS</b>Some PDZ domains may have more potential ligand proteins, which are undiscovered yet experimentally. These bioinformatic results also provide clues for studying functions of hypothetical proteins and PDZ domains' protein interactions in many different organisms.</p><p><b>CONCLUSION</b>The results may provide useful clues for discovering potential functions of hypothetical proteins and new functions of known proteins.</p>