The 1,2,3-thiadiazole-carboxylate moiety was reported to be an important pharmacophore of plant activators.In this study,a series of novel plant activators based on ...thieno2,3-d-1,2,3-thiadiazole-6-carboxylate were designed and synthesized and their biological activity as plant activators was studied.The structures of the novel compounds were identifed by1H NMR,19F NMR and HRMS.The in vivo bioassay showed that these novel compounds had good effcacy against seven plant diseases.Especially,compounds 1a and 1c were more potent than the commercialized plant activator BTH.Almost no fungicidal activity was observed for the active compounds in the in vitro assay,which matched the requirements as plant activators.
Previous studies have shown that 5-hydroxymethylfurfural, a compound extracted from wine- processed Fructus corni, has a protective effect on hippocampal neurons. The present study was designed to ...explore the related mechanisms. Our study revealed that high and medium doses （10, 1 μmol/L） of 5-hydroxymethylfurfural could improve the morphology of H2O2-treated rat hippocampal neurons as revealed by inverted phase-contrast microscopy and transmission electron microscopy. MTT results showed that incubation with high and medium doses of 5-hydroxymethylfurfural caused a significant increase in the viability of neuronal cells injured by H2O2. Flow cytometry assays con- firmed that H2O2 could induce cell apoptosis, while high and medium doses of 5-hydroxymethylfurfural had a visible protective effect on apoptotic rat hippocampal neurons. Real-time PCR and western blot analysis showed that high and medium doses of 5-hydroxymethylfurfural prevented H2O2-induced up-regulation of p53, Bax and caspase-3 and an- tagonized the down-regulation of Bcl-2 induced by H2O2 treatment. These results suggested that 5-hydroxymethylfurfural could inhibit apoptosis of cultured rat hippocampal neurons injured by H2O2 via increase in Bcl-2 levels and decrease in p53, Bax and caspase-3 protein expression levels.
Started from salicylic acid（SA） and related commercialized plant activators,based on molecular threedimensional shape and pharmacophore similarity comparison（SHAFTS）,a new lead compound benzotriazole ...was predicted and a series of benzotriazole derivatives were designed and synthesized.The bioassay showed that benzotriazole had high activity against a broad spectrum of diseases including fungi and oomycetes in vivo,but no activity in vitro.And the introduction of proper groups at the1＇-position and 5＇-position was beneficial to the activity.So,they had the potential to be exploited as novel plant activators.
Simple sequence repeats (SSR) have been widely used as molecular markers due to their abundance and high polymorphism. However, up to now, the SSR markers had not been developed in the obligate ...biotrophic phytopathogenic fungus, Blumeria graminis f.sp. tritici. From (AC)10 and (AG)10 enriched genomic libraries for Bgt, 25 primer pairs were designed using the FIASCO (fast isolation by AFLP of sequences containing repeats) protocol. Five primer pairs exhibited polymorphism with allelic diversity from two to seven alleles and produced 29 alleles in a survey of 90 isolates collected from six provinces (cities) in China, while the others displayed monomorphic. Levels of observed heterozygosity ranged from 0.000-0.044 (mean 0.025) and expected heterozygosity ranged from 0.297-0.816 (mean 0.538). These molecular markers provide a novel source to genetic diversity assays and to genetic and physical mapping of Bgt. SSR markers of Bgt need to be further explored.
Objective To quantitatively evaluate the contamination area and risk of a live pathogen during tissue homogenization by either ultrasonic processor or tissue disperser.Methods A recombinant Herpes ...Simplex Virus（rHSV） containing GFP gene was used as the index virus,and fresh liver tissue from healthy mice was used as simulated specimen.After 10% liver homogenate was mixed with rHSV（100 TCID50/0.1 mL） in a 5 mL tube,the stability of rHSV in liver homogenate and influences of an ultrasonic processor and a tissue disperser on viral infectivity were determined by GFP expressions in cell cultures.The contaminating areas of live viruses during homogenization were evaluated by a cell culture-based sedimentary.The contamination radii were counted by measurement of the distance between the operator and the farthest GFP positive well.Results The infectivity of rHSV in 10% liver homogenate maintained almost unchanged after it was incubated at room temperature for 30 min.Treatment with an ultrasonic processor clearly dropped down the virus infectivity,while a disperser not.Obvious spills and slashes of live viruses were observed in processes of homogenization with those two apparatuses.The contamination radii are positively related with sample volume,output energy of operator and handling time.Conclusion Homogenizing infectious samples with an ultrasonic processor and a tissue disperser at commonly used conditions caused obvious spills and splashes of live viruses,which possesses high risk to induce Laboratory acquired infections（LAIs）.
Due to its particular structure and electronic properties originating from nitrogen doping, nitrogen doped graphene prepared by thermally annealing graphite oxide with melamine shows high ...electrocatalytic activity towards the oxidation of ascorbic acid, dopamine and uric acid. A novel NG-based electrochemical sensor has been fabricated and successfully used to simultaneously determine these biomolecules with high sensitivity and selectivity. Display omitted
► Nitrogen doped graphene (NG) prepared thermally using melamine precursor. ► NG shows highly electrocatalytic activity toward small biomolecules. ► The electrocatalytic activity depends on the doped nitrogen amount. ► NG based electrochemical biosensor detects ascorbic acid, uric acid and dopamine with high sensitivity and selectivity.
Nitrogen doped graphene (NG) was prepared by thermally annealing graphite oxide and melamine mixture. After characterization by atomic force microscopy and X-ray photoelectron spectroscopy etc., the electrochemical sensor based on NG was constructed to simultaneously determine small biomolecules such as ascorbic acid (AA), dopamine (DA) and uric acid (UA). Due to its unique structure and properties originating from nitrogen doping, NG shows highly electrocatalytic activity towards the oxidation of AA, DA and UA. The electrochemical sensor shows a wide linear response for AA, DA and UA in the concentration range of 5.0×10−6 to 1.3×10−3M, 5.0×10−7 to 1.7×10−4M and 1.0×10−7 to 2.0×10−5M with detection limit of 2.2×10−6M, 2.5×10−7M and 4.5×10−8M at S/N=3, respectively. These results demonstrate that NG is a promising candidate of advanced electrode material in electrochemical sensing and other electrocatalytic applications.
For locally advanced rectal cancer (LARC) patients who receive neoadjuvant chemoradiotherapy (nCRT), there are no reliable indicators to accurately predict pathological complete response (pCR) before ...surgery. For patients with clinical complete response (cCR), a "Watch and Wait" (W&W) approach can be adopted to improve quality of life. However, W&W approach may increase the recurrence risk in patients who are judged to be cCR but have minimal residual disease (MRD). Magnetic resonance imaging (MRI) is a major tool to evaluate response to nCRT; however, its ability to predict pCR needs to be improved. In this prospective cohort study, we explored the value of circulating tumor DNA (ctDNA) in combination with MRI in the prediction of pCR before surgery and investigated the utility of ctDNA in risk stratification and prognostic prediction for patients undergoing nCRT and total mesorectal excision (TME). We recruited 119 Chinese LARC patients (cT3-4/N0-2/M0; median age of 57; 85 males) who were treated with nCRT plus TME at Fudan University Shanghai Cancer Center (China) from February 7, 2016 to October 31, 2017. Plasma samples at baseline, during nCRT, and after surgery were collected. A total of 531 plasma samples were collected and subjected to deep targeted panel sequencing of 422 cancer-related genes. The association among ctDNA status, treatment response, and prognosis was analyzed. The performance of ctDNA alone, MRI alone, and combining ctDNA with MRI was evaluated for their ability to predict pCR/non-pCR. The model combining ctDNA and MRI improved the predictive performance compared with the models derived from individual information, and combining ctDNA with HR_feature can stratify patients with a high risk of recurrence. Therefore, ctDNA can supplement MRI to better predict nCRT response, and it could potentially help patient selection for nonoperative management and guide the treatment strategy for those with different recurrence risks.
Background and Aim
Considering the limitation of varying acid suppression of proton pump inhibitors, this study was aimed to assess the efficacy, safety, and dose–effect relationship of keverprazan, ...a novel potassium‐competitive acid blocker, in the treatment of duodenal ulcer (DU) compared with lansoprazole.
Methods
A randomized, double‐blind, double‐dummy, multicenter, low‐dose, high‐dose, and positive‐drug parallel‐controlled study was conducted to verify the non‐inferiority of keverprazan (20 or 30 mg) to lansoprazole of 30 mg once daily for 4 to 6 weeks and dose–effect relationship of keverprazan in the treatment of patients with active DU confirmed by endoscopy.
Results
Of the 180 subjects randomized, including 55 cases in the keverprazan_20 mg group, 61 cases in the keverprazan_30 mg group, and 64 cases in the lansoprazole_30 mg group, 168 subjects (93.33%) completed the study. The proportions of healed DU subjects in the keverprazan_20 mg, keverprazan_30 mg, and lansoprazole_30 mg groups were respectively 87.27%, 90.16%, and 79.69% at week 4 (P = 0.4595) and were respectively 96.36%, 98.36%, and 92.19% at week 6 (P = 0.2577). The incidence of adverse events in the keverprazan_20 mg group was lower than that in the lansoprazole_30 mg (P = 0.0285) and keverprazan_30 mg groups (P = 0.0398).
Conclusions
Keverprazan was effective and non‐inferior to lansoprazole in healing DU. Based on the comparable efficacy and safety data, keverprazan of 20 mg once daily is recommended for the follow‐up study of acid‐related disorders. (Trial registration number: ChiCTR2100043455.)
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