A new xanthone from the Polygala tenuifolia Willd. of northern Shaanxi / 药学学报

Ten compounds were isolated and purified from ethanol extracts of dried roots bark of Polygala tenuifolia Willd. by various chromatography techniques such as silica gel and Sephadex LH-20. Their structures were identified by analysis of physicochemical properties and spectral data, and determined as β-sitosterol (1), tenuifolin (2), 6-methoxy coumarin (3), 7-phenyl-1-hydroxy-2,3,6-trimethoxyxanthone (4), 1,8-dihydroxy-3,4,7-trimethoxyanthone (5), mangiferin (6), quercetin-3-O-β-D-glucoside (7), rutin (8), syringaldehyde (9), salicylicacid (10). Among them, compounds 3, 4 and 5 were isolated from the genus of Ploygala for the first time and compound 4 was a new xanthone. The acetylcholinesterase inhibitory activities of compounds 3, 4 and 5 were evaluated by Ellman colorimetric method, compounds 3 and 5 exhibited moderate inhibitory activity, compound 4 exhibited weak inhibitory activity.

A new diphenyl butanedione from Astragalus membranaceus of northern Shanxi / 药学学报

Seven compounds were isolated from Astragalus membranaceus of northern shaanxi by silica gel and Sephadex LH-20 column chromatographies. Their chemical structures were identified on the basis of their physical and chemical properties. These compounds were elucidated as astragaloside IV (1), formononetin (2), calycosin (3), 1-(4-hydroxyphenyl)-4-(2,4-hydroxyphenyl)-2-hydroxy-1,4-but anedione (4), (E)-4-methylcinnamic acid (5), quercetin (6), and uridine (7). Compound 4 is a new compound and compound 5 was isolated from the plants of Astragalus Linn. for the first time. The results of in vitro antitumor activity assay showed that compound 4 could inhibit the proliferation of A549 with IC50 values of 11.41 μmol·L-1.

Cyclodextrin-active natural compounds in food applications: a review of antibacterial activity.

Many natural compounds have excellent activity against different bacteria. However, their food use to inhibit the bacteria is often limited by poor water solubility, or instability to light, heat, oxygen, and other environmental factors. Cyclodextrin combines with these natural compounds could not only overcome these shortcomings, but also increase the antibacterial ability of active compounds. This review focuses on the following aspects of active natural compounds in cyclodextrin-based food: the preparation, food applications, and their possible antibacterial mechanisms of different systems. Both cyclodextrin and its derivatives are able to selectively combine with different guest molecules, such as terpenes, phenols and flavonoids, as well as essential oil and other plant extract. Finally, the opportunities and future challenges of active natural compounds in cyclodextrin-based food are outlined and proposed.

Identification of APEX2 as an oncogene in liver cancer.

BACKGROUND: DNA damage is one of the critical contributors to the occurrence and development of some cancers. APEX1 and APEX2 are the most important molecules in the DNA damage, and APEX1 has been identified as a diagnostic and prognostic biomarker in liver hepatocellular carcinoma (LIHC). However, the expression of APEX2 and its functional mechanisms in LIHC are still unclear. AIM: To examine the expression of APEX2 and the potential mechanism network in LIHC. METHODS: We conducted a pan-cancer analysis of the expression of APEX1 and APEX2 using the interactive TIMER tool. GEO datasets, including GSE14520, GSE22058, and GSE64041, were used to compare the APEX2 expression level in tumor tissues and adjacent non-tumor tissues. Then, we calculated the 5-year survival rate according to the web-based Kaplan-Meier analysis. We included the TCGA liver cancer database in GSEA analysis based on the high and low APEX2 expression, showing the potential mechanisms of APEX2 in LIHC. After that, we conducted Pearson correlation analysis using GEPIA2. Next, we performed quantitative polymerase chain reaction (qPCR) assay to examine the APEX2 levels in normal liver cell line LO2 and several liver cancer cell lines, including HepG2, Huh7, SMMC7721, and HCCLM3. APEX2 in HCCLM3 cells was knocked down using small interfering RNA. The role of APEX2 in cell viability was confirmed using CCK-8. Dual-luciferase reporter assay was performed to examine the promoter activity of CCNB1 and MYC. RESULTS: APEX1 and APEX2 are both highly expressed in the tumor tissues of BLCA, BRCA, CHOL, COAD, ESCA, HNSC, LIHC, LUAD, LUSC, READ, and STAD. APEX2 overexpression in LIHC was validated using GSE14520, GSE22058, and GSE64041 datasets. The survival analysis showed that LIHC patients with high expression of APEX2 had a lower overall survival rate, even in the AJCC T1 patients. High level of APEX2 could indicate a lower overall survival rate in patients with or without viral hepatitis. The GSEA analysis identified that kinetochore and spindle microtubules are the two main cellular components of APEX2 in GO Ontology. APEX2 was also positively associated with molecular function regulation of chromosome segregation and DNA replication. The results of KEGG analysis indicated that APEX2 expression was positively correlated with cell cycle pathway and pro-oncogenic MYC signaling. Pearson correlation analysis showed that APEX2 had a significant positive correlation with CCNB1 and MYC. APEX2 level was higher in liver cancer cell lines than in normal liver LO2 cells. Small interfering RNA could knock down the APEX2 expression in HCCLM3 cells. Knockdown of APEX2 resulted in a decrease in the viability of HCCLM3 cells as well as the expression and promoter activity of CCNB1 and MYC. CONCLUSION: APEX2 is overexpressed in LIHC, and the higher APEX2 level is associated with a worse prognosis in overall survival. APEX2 is closely involved in the biological processes of chromosome segregation and DNA replication. APEX2 expression is positively correlated with the pro-oncogenic pathways. Knockdown of APEX2 could inhibit the cell viability and CCNB1 and MYC pathways, suggesting that APEX2 is an oncogene in LIHC, which could be a potential pharmaceutic target in the anti-tumor therapy.

Analysis of 4 imaging features in patients with COVID-19.

BACKGROUND: The aim of this was to analyze 4 chest CT imaging features of patients with coronavirus disease 2019 (COVID-19) in Shenzhen, China so as to improve the diagnosis of COVID-19. METHODS: Chest CT of 34 patients with COVID-19 confirmed by the nucleic acid test (NAT) were retrospectively analyzed. Analyses were performed to investigate the pathological basis of four imaging features("feather sign","dandelion sign","pomegranate sign", and "rime sign") and to summarize the follow-up results. RESULTS: There were 22 patients (65.2%) with typical "feather sign"and 18 (52.9%) with "dandelion sign", while few patients had "pomegranate sign" and "rime sign". The "feather sign" and "dandelion sign" were composed of stripe or round ground-glass opacity (GGO), thickened blood vessels, and small-thickened interlobular septa. The "pomegranate sign" was characterized as follows: the increased range of GGO, the significant thickening of the interlobular septum, complicated with a small amount of punctate alveolar hemorrhage. The "rime sign" was characterized by numerous alveolar edemas. Microscopically, the wall thickening, small vascular proliferation, luminal stenosis, and occlusion, accompanied by interstitial infiltration of inflammatory cells, as well as numerous pulmonary interstitial fibrosis and partial hyaline degeneration were observed. Repeated chest CT revealed the mediastinal lymphadenectasis in one patient. Re-examination of the NAT showed another positive anal swab in two patients. CONCLUSION: "Feather sign" and "dandelion sign" were typical chest CT features in patients withCOVID-19; "pomegranate sign" was an atypical feature, and "rime sign" was a severe feature. In clinical work, accurate identification of various chest CT signs can help to improve the diagnostic accuracy of COVID-19 and reduce the misdiagnosis or missed diagnosis rate.

Selective modifications at the different positions of cyclodextrins: a review of strategies.

Cyclodextrins (CDs) are natural, nontoxic, and biodegradable macrocyclic oligosaccharides. As supramolecular hosts, CDs have numerous applications in many aspects. However, nonsubstituted CDs have the disadvantages of solubility, unspecific recognition sites, and weak interactions with guest molecules. Therefore, new CD-based derivatives are successfully designed, synthesized, and widely used in various fields. This contribution outlines the research progress in CD derivatives. In particular, this review emphasizes the synthesis and application of CDs modified through functionalization in definite positions, random substitution, and reconstruction of the skeleton. At the end of this review, a summary and future directions are presented.

CircRNA_100290 promotes colorectal cancer progression through miR-516b-induced downregulation of FZD4 expression and Wnt/ß-catenin signaling.

Accumulating evidence indicates that circular RNAs (circRNA) exert crucial functions in the development and advance of cancers. CircRNA_100290 has been reported to promote proliferation in oral cancer. However, whether it participates in colorectal cancer (CRC) remains unclear. Here, our report showed that circRNA_100290 level was significantly increased in CRC tissues and cell lines. Besides, circRNA_100290 expression was positively correlated with tumor metastasis while inversely correlated with prognosis. Silencing circRNA_100290 markedly reduced cell proliferation rate, inhibited migration and invasion abilities, but promoted apoptosis in vitro. Mechanistically, our data revealed circRNA_100290 was a competing endogenous RNA (ceRNA) of FZD4 by sponging miR-516b, leading to activation of Wnt/ß-catenin pathway. Rescue assay indicated that FZD4-induced activation of ß-catenin pathway is indispensable for the function of circRNA_100290 in CRC. In summary, our study for the first time revealed a novel regulatory loop of circRNA_100290/miR-516b/FZD4/Wnt/ß-catenin implicated in CRC progression.

Polyelectrolyte-protected Dual-color-quantum-dot Assembled Silica Nanoparticles and Their Application in Simultaneous Fluorescence Determination of e Antigen and Surface Antigen of Hepatitis B.

Cationic poly-diallyldimethylammonium (PDADMAC), green CdTe quantum dots (QDs) or red CdS coated CdTe QDs, and anionic polyacrylic acid (PAA) were respectively assembled on the nano-carrier SiO2 to prepare green fluorescence composite nanoparticles (GF-QDs) and red ones (RF-QDs) with the structure SiO2/PDADMAC/QD/PDADMAC/PAA. The sandwich structure "PDADMAC/QD/PDADMAC" on the nano-carrier not only realized the protection to fluorescence of QDs but also avoided the fluorescence shielding of silica shell for the assembled QDs. In 7 days, the diluent solutions of GF-QD and RF-QD all have a very stable fluorescence. On the contrary, the fluorescence of diluent solutions of red and green QDs reduced by 75.99 and 94.35%, respectively. Indeed, they have not fluorescent shielding and have a very slight fluorescent enhancement. Based on GF-QD and RF-QD, the simultaneous determination of Hepatitis B e antigen and surface antigen has been established. Their determination in buffer and plasma all showed good precision and accuracy.

YAF2 promotes tumor cell proliferation via targeting cyclin D1 expression / 基础医学与临床

Objective To explore the molecular mechanism by which YY1 associated factor 2(YAF2) up-regulates cyclin D1 expression in tumor cells as well as the effect of YAF2-cyclin D1 regulatory loop on tumor cell prolifera-tion. Methods Overexpression and knockdown experiments combined with Western blot and real-time quantitative PCR were used to detect the expression of YAF2 and cyclin D1;Dual luciferase reporter assay was performed to in-vestigate the effect of YAF2 on cyclin D1 promoter activity;Flow cytometry analysis was carried out to elucidate the effect of YAF2 on cell cycle progression through targeting cyclin D1;Colony formation assay was employed to deter-mine cell proliferation under different YAF2 and cyclin D1 expression level. Results YAF2 upregulated the ex-pression of cyclin D1 at both the mRNA(P<0.05) and protein level;YAF2 activated the promoter activity of cyc-lin D1 (P<0.05);YAF2 silencing increased significantly the proportion of cells in G0/G1phase(P<0.0001) and reduced the proportion of cells in S phase by regulating cyclin D1 (P<0.002); YAF2 facilitated the cell colony formation via targeting cyclin D1(P<0.05). Conclusions In tumor cells,YAF2 promotes the expression of cyclin D1,and enhances cell cycle progression and cell proliferation.

Cyclodextrin-Catalyzed Organic Synthesis: Reactions, Mechanisms, and Applications.

Cyclodextrins are well-known macrocyclic oligosaccharides that consist of α-(1,4) linked glucose units and have been widely used as artificial enzymes, chiral separators, chemical sensors, and drug excipients, owing to their hydrophobic and chiral interiors. Due to their remarkable inclusion capabilities with small organic molecules, more recent interests focus on organic reactions catalyzed by cyclodextrins. This contribution outlines the current progress in cyclodextrin-catalyzed organic reactions. Particular emphases are given to the organic reaction mechanisms and their applications. In the end, the future directions of research in this field are proposed.

Ran binding protein 9 (RanBPM) binds IFN-λR1 in the IFN-λ signaling pathway.

Like the type I interferons (IFNs), the recently discovered cytokine IFN-λ displays antiviral, antiproliferative, and proapoptotic activities, mediated by a heterodimeric IFN-λ receptor complex composed of a unique IFN-λR1 chain and the IL-10R2 chain. However, the molecular mechanism of the IFN-λ-regulated pathway remains unclear. In this study, we newly identified RAN-binding protein M (RanBPM) as a binding partner of IFN-λR1. The interaction between RanBPM and IFN-λR1 was identified with a glutathione S-transferase pull-down assay and coimmunoprecipitation experiments. IFN-λ1 stimulates this interaction and affects the cellular distribution of RanBPM. However, the interaction between RanBPM and IFN-λR1 does not correlate with their conserved TRAF6-binding sites. Furthermore, we also found that RanBPM is a scaffolding protein with a modulatory function that regulates the activities of IFN-stimulated response elements. Therefore, RanBPM plays a novel role in the IFN-λ-regulated signaling pathway.

Application of bandage contact lens in pterygium excision combined with conjunctival transplantation / 国际眼科杂志(Guoji Yanke Zazhi)

AIM:To evaluate the application and effect of bandage contact lens in pterygium excision combined with conjunctival transplantation (CAT).METHODS:In a prospective, randomized, controlled clinical study, 110 patients (110 eyes) diagnosed with primary pterygium were collected in PLA NO.474 Hospital from January 2015 to January 2016.The 110 patients enrolled in the study in turn, and divided into two groups by the odd and even number.The odd number divided into bandage contact lens group (CAT + bandage contact lens, n=55), while the even number divided into control group (CAT, n=55).Visual analog scale (VAS) and corneal irritation were evaluated on 1, 3 and 7d after operation.Cornea fluorescent staining testing was carried out on 3d after operation.Following-up all the patients with 1a at least observed the recurrence of pterygium.RESULTS:The score of VAS in bandage contact lens group less than that in control group on 1d (4.13±2.06 vs 5.80±1.93, t=4.391, P<0.001) and 3d (2.09±1.36 vs 3.65±1.65, t=5.422, P<0.001) after operation, while there was no significant difference between two groups on 7d (t=1.295, P=0.198) after operation.The corneal irritation in bandage contact lens group less than that in control group on 1d and 3d after operation (P<0.05), while there was no significant difference between two groups on 7d after operation (P=0.052).Cornea fluorescent staining testing area in bandage contact lens group was less than that in control group on 7d after operation (0.33±0.37mm2 vs 2.73±2.21mm2, t=7.921, P<0.01).There was no significant difference in recurrence rate between two groups after 1a operation (P=1.000).CONCLUSION:Bandage contact lens could significantly release pain and corneal irritation, promote the healing of the corneal epitheliums in the defected area, and increase the postoperative comfort level in patients after operation.

Multiple analytical methods for identification and quality evaluation of Fritillariae Thunbergii Bulbus based on biological single molecules by high-performance liquid chromatography.

Quantitative analysis for biological single molecules in Fritillariae Thunbergii Bulbus and identification method by chemometrics was established by using high-performance liquid chromatography. Amino acids, nucleosides, and nucleobases were quantitatively analyzed, and 11 peaks were selected for species identification. A Common pattern was established for chemometrics, and then similarity analysis, principal component analysis, and hierarchical cluster analysis heatmap were applied, and the results indicated that species were ideally identified from the adulterants as Fritillariae Cirrhosae Bulbus. This evaluation method was valuable for further quality control to select the characteristic components.

Discontinued cardiovascular drugs in 2015.

INTRODUCTION: About 10,000 compounds will be tested for an individual drug to eventually reach the market. It might be helpful recapitulating previous failures and identifying the main factors of the disappointments. AREAS COVERED: In this review, the author(s) detailed the 7 cardiovascular compounds discontinued after reaching animal studies or Phase I-III clinical trials during 2015. Meanwhile, the reasons for these discontinuations were reported. Among these drugs, most discontinuations (6 drugs) were attributed to lack of efficacy. In general, failures due to lack of efficacy and safety demonstrate the need for the development of more predictive animal models. However, recent related studies showed that the absence of toxicity in animals provided little or virtually no evidential weight that adverse drug reactions would also be absent in humans. In this case, microdosing and collaborating more closely with biotech companies may be the better choices to improve the success ratio. EXPERT OPINION: Future researches may benefit from the seven developments and investigators conducting similar studies may learn from these failures.

Combination with Chemometrics and Quantification for Quality Evaluation and Variety Identification of Flos Chimonanthi Praecocis by HPLC.

Flos Chimonanthi Praecocis (FCP) is one of the popular traditional Chinese medicines, which have been widely used in China. Inconspicuous appearance differences are disadvantageous for identification, and it is difficult to evaluate the quality of FCP using the current methods. In this article, a simple method that combined chemometrics and quantitative analysis was established. The samples were obtained from three typical varieties for fingerprint analysis by high-performance liquid chromatography. Contents of rutin and quercetin were determined, and then a common pattern with 16 characteristic peaks was applied for principal component analysis, similarity analysis, and the hierarchical cluster analysis heatmap (HCA heatmap) to characterize the similarity and differences among samples for identification. Furthermore, seven characteristics peaks with higher loading values were selected for chemometrics analysis after dimensionality reduction to reduce analytical difficulty, and the new common pattern showed the similar identification effects. Overall, combination with chemometrics and quantitative analysis would provide a useful and simple method for quality control of FCP in the future.

Chimeric groin free flaps: Design and clinical application.

BACKGROUND: Reconstruction of composite extremity defects or through-and-through oral defects remains challenging for surgeons. Chimeric flaps are ideal for repairing these lesions. In this article, we report the design of various chimeric groin free flaps for the reconstruction of both complex oral and extremity defects in 18 patients. METHODS: Between 2010 and 2014, 18 patients with composite tissue defect or two defects in the extremities or head and neck region, underwent reconstruction with cutaneous-cutaneous, musculo-cutaneous, or osteo-cutaneous chimeric groin free flaps. The size and pedicles length of the chimeric groin flaps based on the superficial circumflex iliac artery (SCIA) were tailored to the lesions. Patient-reported post-operative outcomes at the out-patient department were evaluated. RESULTS: The types of chimeric groin free flaps included cutaneous-cutaneous (n = 12), musculo-cutaneous (n = 1), and osteo-cutaneous (n = 5) flaps. Three to four SCIA branches (mean: 3.33) could be used for flap design. The cutaneous flap size ranged from 1.5 cm × 6 cm to 11 cm × 30 cm, and the bone flap size ranged from 1 cm × 1.5 cm to 2.5 cm × 6 cm. All flaps survived, and no significant complications developed at recipient or donor sites. Functional recovery after reconstruction was satisfactory in most patients after a mean of 17.27 months (ranging 2-42 months) of follow-up. CONCLUSION: The innovative flap technique presented herein has advantages including greater reliability, as well as the ability to tailor the dimensions and flap paddles to specific lesions and reconstruct two defects or one composite defect using only one (chimeric) flap.

[Effect of Heat-Clearing and Detoxifying Health Function of Lonicera japonica in Rats Based on Metabonomics].

Objective: To study the metabonomics for heat-clearing and detoxifying health function of Lonicera japonica in rats. Methods: Male Wistar rats were treated with decoction of Lonicera japonica through intragastric for 5 d. GC-MS was used to detect the changes in rats serum metabolites. Mass spectrometry analysis,PCA and other technologies were used to analyze the differences among their metabolites,and analyzed the endogenous product. Results: There was a decline trend in citric acid cycle intermediates of Lonicera japonica treated group. On the contrary,amino acids and fatty acid intermediate product showed significant elevation,which revealed that the pathway of tricarboxylic acid cycle has been inhibited,and consistented with heat-clearing and detoxifying effect of Lonicera japonica. Conclusion: The metabonomics method by detecting the low-molecular-weight compounds can evaluate the heat-clearing and detoxifying health function of Lonicera japonica.

Practice and effect of reading report activities on college-to-undergraduate nursing students in adult higher education / 医学研究生学报

Objective To discuss the pattern and effect of reading report activities on college-to-undergraduate nursing students in adult higher education. Methods We chose 154 college-to-undergraduate nursing students in adult higher education who studied at our department from 2009 to 2012 as control group, meanwhile the experimental group consisted of 168 college-to-undergrad-uate nursing students in adult higher education who studied at our department from 2013 to 2014.We used thefive-in-oneteaching method involving relevant scientific knowledge training, tutorial system, group report meeting, exchange of excellent reading report and score checking to train the experimental group, while the control group was still trained by primary method which was relevant scientific knowledge teaching and discussion of excellent reading report. Results The reading reports wrote by the students in the experimental group were superior to those wrote by the control group (P<0.001);The experimental group had better scores in the achievements of scientific knowledge and theory (P<0.001); The self-assessment of experimental group students in the ability of literature review, reading and analysis was higher than that of the control group (P<0.001).As to the effects of reading report such as enhancing scien-tific awareness, expanding scope of knowledge and so on, the experimental group had a obvious advantage over the control group ( P<0.001). Conclusion The five-in-onetraining pattern in the reading report activities involving relevant scientific knowledge training, tutorial system, group report meeting, exchange of excellent reading report and score checking can effectively improve the scientif-ic awareness of college-to-undergraduate nursing students in adult higher education, which is conductive to establish the basis of nurs-ing scientific research, guide the clinical nursing work and improve the comprehensive quality of students.

[Identification of two varieties of Citri Fructus by fingerprint and chemometrics].

Citri Fructus identification by fingerprint and chemometrics was investigated in this paper. Twenty-three Citri Fructus samples were collected which referred to two varieties as Cirtus wilsonii and C. medica recorded in Chinese Pharmacopoeia. HPLC chromatograms were obtained. The components were partly identified by reference substances, and then common pattern was established for chemometrics analysis. Similarity analysis, principal component analysis (PCA) , partial least squares-discriminant analysis (PLS-DA) and hierarchical cluster analysis heatmap were applied. The results indicated that C. wilsonii and C. medica could be ideally classified with common pattern contained twenty-five characteristic peaks. Besides, preliminary pattern recognition had verified the chemometrics analytical results. Absolute peak area (APA) was used for relevant quantitative analysis, results showed the differences between two varieties and it was valuable for further quality control as selection of characteristic components.