OBJECTIVE: To design and synthesize phenylpyridine substituted semicarbazides and investigate their in vitro antitumor activities. METHODS: The target compounds were synthesized from acetophenone through condensation, cyclization,hydrazinolysis and reaction with isocyanates. The synthesized compounds were screened for their anticancer potential against different cancer cells viz human hepatocelular carcinoma (QGY-7703), non-small cell lung (NCl-H460) and human breast (MCF-7) cancer cell lines by MTT assay. RESULTS Sixteen novel compounds were obtained, and their structures were characterized by 1H-NMR, 13C-NMR and HRMS. In vitro bioassay indicated that most compounds had a certain degree of antitumor activity. Compound 51 displayed the most potential anticancer activity against these cancer cell lines with IC50 value of 9.15, 10.45 and 12.50 μmol·L-1, respectively. CONCLUSION: The series of compounds show preferable antitumor activities, which are worthy of further study.

Objective To investigate the efficacy and toxicity of neoadjuvant regional arterial chemotherapy in the treatment of advanced gastric cancer. Methods The clinical data of 158 patients with advanced gastric cancer and with the same clinical stages who were admitted to Renji Hospital of Shanghai Jiaotong University from February 2002 to May 2005 were retrospectively analysed. Preoperative regional arterial chemotherapy was applied to 76 patients (test group) and the remaining 82 patients only received surgical treatment (control group). The chemotherapy regimen was epirubicin (50 mg/m2) + cisplatin (60 mg/m2) + 5-fluorouracil (1000 mg/m2).This regimen was modified to oxaliplatin (130 mg/m2) + 5-fluorouracil (1000 mg/m2) since 2003, and surgery was performed 6-11 days after the chemotherapy. All patients received postoperative intravenous chemotherapy.The clinical effects, radical resection rate, operative complications and long-term survival of the two treatment methods were evaluated. All data were analysed using the chi-square test and Kaplan-Meier analysis. Results The radical resection rate was significantly higher at 86% (65/76) in the test group compared with 71% (58/82)in the control group ( x2 = 5.01, P ＜ 0. 05 ). The toxicity of the chemotherapy in the test group was mild. The postoperative complication rate was 20% (15/76) in the test group and 16% (13/82) in the control group, with no significant difference between the two groups (x2 = 0.41, P＞0.05). The median survival time was 41 months in the test group and 23 months in the control group. The 5-year overall survival rate was higher in the test group (44.6%) than that in the control group (29.1%) (x2 =3.95, P＜0. 05). Conclusions Neoadjuvant regional arterial chemotherapy is well tolerated by patients with advanced gastric cancer. It is also effective for increasing the radical resection rate and improving the long-term survival.

Objective: To describe the CT features and clinical characteristics of pediatric patients with coronavirus disease 2019 (COVID-19).Method: A total of 9 COVID-19 infected pediatric patients were included in this study.Clinical history,laboratory examination,and detailed CT imaging features were analyzed.All patients underwent the first CT scanning on the same day of being diagnosed by realtime reverse-transcription polymerase chain reaction (rRT-PCR).A low-dose CT scan was performed during follow-up.Results: All the child patients had positive results.Four patients had cough and one patient had fever.One patient presented both cough and fever.Two children presented other symptoms like sore throat and stuffy nose.One child showed no clinical symptom.Five patients had positive initial CT findings with subtle lesions like ground-glass opacity (GGO) or spot-like mixed consolidation.Three patients were reported with negative results in the initial and follow-up CT examination.One patient was reported with initial negative CT findings but turning positive during the first follow-up.All patients had absorbed lesions on follow-up CT images after treatment.Conclusion: Pediatric COVID-19 patients have certain imaging and clinical features as well as disease prognosis.Children with COVID-19 tend to have normal or subtle CT findings and relatively better outcome.

Objective·To establish a nomogram for the differential diagnosis of early systemic lupus erythematosus(SLE)and other autoimmune diseases based on laboratory indications,and to evaluate its efficacy.Methods·A total of 535 SLE patients admitted to the First Hospital of Lanzhou University from January 2017 to December 2021 were selected as SLE group,and 535 patients with other autoimmune diseases during the same period were selected as control group.Basic information and laboratory test indicators of the SLE group and control group were collected and compared.The SLE group and control group were randomly assigned to the training set and the validation set at a ratio of 7∶3,respectively.LASSO regression method and multivariate Logistic regression were used to select the main risk factors of SLE.The nomogram for differential diagnosis of early SLE(SLE nomogram)was established according to the selected main risk factors.Bootstrap method was used to conduct internal repeated sampling for 1 000 times to calibrate the nomogram.The receiver operator characteristic curve(ROC curve)and decision curve analysis(DCA)were performed to evaluate the differential diagnosis ability and the value in clinical application of SLE nomogram,respectively.The"DynNom"package of R language was used to convert the nomogram into an electronic calculator,and its consistency with SLE nomogram was verified by data from 3 groups of patients.Results·LASSO regression and multivariate Logistic regression identified six major risk factors for SLE,including antinuclear antibody(ANA),anti-double-stranded DNA(anti-dsDNA)antibody,anti-ribonucleoprotein antibody/anti-Simth antibody(anti-nRNP/Sm),anti-ribosomal P protein(anti-P)antibody,anti-nucleosome antibody(ANuA)and urinary protein(PRO),which were used to construct the SLE nomogram.The calibration curve of the SLE nomogram had standard errors of 0.009 and 0.015 in the training set and validation set,respectively,and its area under the curve(AUC)was 0.889 and 0.869,respectively.The results of DCA showed that when the risk threshold of SLE nomogram was 0.15?0.95,the model achieved more net benefit.The prediction results of the electronic calculator showed that when ANA(titer 1∶100)was positive in SLE patient No.1,the prevalence was 0.166;when both ANA(titer 1∶100)and ANuA(titer 1∶100)were positive in patient No.2,the prevalence was 0.676;when all of PRO,ANA(titer 1∶100),ANuA(titer 1∶100)and anti-P antibody(titer 1∶100)were positive in patient No.3,the prevalence was 0.990,which was consistent with the differential diagnosis results of the SLE nomogram.Conclusion·The established SLE nomogram based on ANA,anti-dsDNA antibody,anti-nRNP/Sm,anti-P antibody,ANuA and PRO and its conversion into an electronic calculator can effectively distinguish early SLE from other autoimmune diseases,and have important clinical application value.

Objective To analyze the clinical value of 1.5T MRI DWI and SWI sequence in the diagnosis of cerebral infarction and cerebral hemorrhage.Methods A total of 28 patients with cerebral infarction were selected as control group,and 28 patients with cerebral hemorrhage were selected as observation group.The PHILPS 1.5T magnetic resonance imaging system was applied.The patients were examined by T1WI and T2WI sequence scanning,and DWI and SWI sequence images were obtained.In the two groups,lesions around the center and different characteristics of SWI and DWI were observed and compared,and the measurement of peripheral lesions were measured for calculating the central area of the PV and ADC.Results There was no significant difference between T1WI and T2WI in patients with cerebral hemorrhage and cerebral infarction,but there was significant difference between DWI sequence and DWI sequence.MRI routine examination showed that there were no significant differences in detection rates of T1WI sequence and T2WI sequence between two groups,but the detection rate of DWI sequence in the observation group was significantly lower than the control group,while detection rate of DWI sequence was significantly higher than the control group(P<0.05).The central area of ADC in the observation group was significantly better than that in the control group,and the PV value of the hematoma area was significantly lower than that of the control group(P<0.05).Conclusion Collections of DWI and SWI images of cerebral infarction and cerebral hemorrhage by magnetic resonance prove that there are significant differences between characteristics of two images.

Objective To analyze the clinical value of 1.5T MRI DWI and SWI sequence in the diagnosis of cerebral infarction and cerebral hemorrhage.Methods A total of 28 patients with cerebral infarction were selected as control group,and 28 patients with cerebral hemorrhage were selected as observation group.The PHILPS 1.5T magnetic resonance imaging system was applied.The patients were examined by T1WI and T2WI sequence scanning,and DWI and SWI sequence images were obtained.In the two groups,lesions around the center and different characteristics of SWI and DWI were observed and compared,and the measurement of peripheral lesions were measured for calculating the central area of the PV and ADC.Results There was no significant difference between T1WI and T2WI in patients with cerebral hemorrhage and cerebral infarction,but there was significant difference between DWI sequence and DWI sequence.MRI routine examination showed that there were no significant differences in detection rates of T1WI sequence and T2WI sequence between two groups,but the detection rate of DWI sequence in the observation group was significantly lower than the control group,while detection rate of DWI sequence was significantly higher than the control group(P<0.05).The central area of ADC in the observation group was significantly better than that in the control group,and the PV value of the hematoma area was significantly lower than that of the control group(P<0.05).Conclusion Collections of DWI and SWI images of cerebral infarction and cerebral hemorrhage by magnetic resonance prove that there are significant differences between characteristics of two images.

Objective The purpose of study was to evaluate the safety and effectiveness of theblood-letting and herbal-cupping therapy for lumbar spinal stenosis.Methods A multi-center prospective case series was performed.The LSS patients meeting the inclusion criteria received 8 treatments as a course and 4 courses in total.The primary outcomes were the symptom severity and physical function scale ofthe Swiss Spinal Stenosis Measurement (SSM,total score 0-5 for each domain).The secondary outcomes were thethe 12-item short form health survey (SF-12,total score 0-100),and Oswestry disability index (ODI,total score 0-100) at time of baseline,completion of last treatment of each course.The minimal clinically important differences (MCIDs) were calculated for estimating the percentage of improvement in the population.The adverse events were reported at any time of the intra-and post-operation.This was a phrase analysis of the studyat seven months.Results Forty-eight patientswere included,with 64.6％ (31/48) of LSS showing neurogenic claudication (walking distance ≤200 m).The average age was 63.1 ± 11.7 years,19 (39.6％) female,and the average BMI was 25.3 ± 3.3 kg/m2.The scores of symptom severity scale of SSM were 2.8 ± 0.6,2.6 ± 0.7,2.3 ± 0.6,1.9 ± 0.2 at baseline,1st,2nd,3rd course,and the scores of physical function scale were 2.5 ± 0.8,2.4 ± 0.7,2.1 ± 0.5,1.8 ± 0.3,and all the changes between baseline and each course showed significant improvement.The patient satisfaction of SSM,ODI and SF-12 showed significantimprovements after the 1st,2nd,3rd course (P＜0.05).The SF-12 subgroup physical composite scores after 3rd course and mental composite score after 1st showed no significant improvement.The minimal clinically important difference for the “SymptomSeverity scale” in the SSM was achieved withimprovement of 18.8％,40.6％,83.3％ in the LSS patient population after 1st,2nd,3rd course;and the "physical function scale" in SSM was achieved withimprovement of 22.9％,31.3％,50.0％.A total of 15 patients felt pain when they were micro-punctured with little blood at first time,but the symptom wereimmediately relieved without any treatment.Conelusions The Blood-letting and herbal-cupping therapy could benefit patients with lumbar spinal stenosis after third course of treatment in the fields of symptom relief and quality of life with no severe adverse event.However,this was a phrase analysis,so more evidence of this study and large comparative researches should be warranted in future.

Objective To explore the intestinal barrier regulation effect of Butuyajie recipe on antibiotic-associated diarrhea rats.Methods 60 SD male rats were randomly divided into blank group,model group,positive drug group(1 g·kg-1),and high-dose,medium-dose and low-dose groups of Butuyajie recipe(40.5,20.25,10.125 g·kg-1).The model was replicated by intragastric administration of lincomycin hydrochloride(5 g·kg-1)for 7 consecutive days.After successful modeling,the materials were obtained after drug intervention for 7 days.Intestinal pathological morphology was observed by HE staining.ELISA kit to detect DAO,MPO,LPS.Take each organ tissue to detect bacterial translocation.Feces were collected for 16S rRNA gene high-throughput sequencing analysis.Results Compared with the normal group,the serum levels of DAO,MPO and LPS in the model group were significantly increased(P<0.001,P<0.01),and the sIgA content in the intestinal mucosa was significantly decreased(P<0.001).Promote intestinal bacterial translocation(P<0.001,P<0.01).The diversity of intestinal flora was significantly reduced,and the levels of intestinal microflora and genera were significantly changed.Butuyajie recipe can reduce the content of DAO,MPO and LPS(P<0.001,P<0.01,P<0.05),significantly increase the content of sIgA(P<0.01,P<0.05),and effectively inhibit the translocation of intestinal bacteria(P<0.001,P<0.01,P<0.05).At the same time,it corrects the intestinal microecological structure by increasing Firmicutes,inhibiting the proportion of Bacteroidetes and Proteobacteria,and regulating Lactobacillus,Sphingomonas,Pseudomonas,and Enterobacter.Conclusion Butuyajie recipe can reduce the permeability of intestinal mucosa,reduce the translocation of intestinal flora,protect the intestinal immune barrier,regulate the diversity of intestinal flora structure,improve the intestinal microecological disorder,and can effectively treat antibiotic-associated diarrhea.

Objective In order to explore the preventive effect and potential mechanism of Dai medicine Shenyeshan leech on chronic renal failure(CRF).The rat model of chronic renal failure was induced and replicated by adenine,and the pharmacodynamics and mechanism of CRF prevention and treatment were discussed.Methods SD rats were randomly divided into normal group,model group,Yougui pill group,high-dose alcohol extract group,middle-dose group,low-dose group.Prophylactic administration was performed 5 days before modeling,and starting from the 6th day,rats in the model group and each administration group were given 1.0%adenine by gavage in the morning,and drug treatment was given in the afternoon for 15 days.24 hours after the last administration,urine specific gravity(SG)was determined by refraction method;urine creatinine(Ucr)and 24-hour proteinuria(PRO)were determined by biochemical analyzer;red blood cell count(RBC),platelet number(Plt)were determined by cell analyzer,hemoglobin(HGB),mean platelet volume(Mpv),mean corpuscular volume(Mcv).Enzyme-linked immunosorbent assay kits were used to determine blood urea nitrogen(BUN),serum creatinine(Scr)content and urinary α1-microglobulin(α1-MG),kidney injury molecule-1(KIM-1)expression.Hematoxylin-eosin staining was used to observe the pathological morphology of rat kidneys,and immunohistochemical staining was used to analyze the expression of aquaporin 2(AQP2),transforming growth factor-β1(TGF-β1),and hypoxia-inducible factor(HIF-1α)-related proteins.Results Compared with the model group,the rats were significantly improved in various symptoms such as lethargy,sluggish reaction,yellow and rough coat with falling off,and the pathological morphology of the kidneys after administration.Blood routine indexes RBC,HGB,Mpv,Mcv levels increased,Plt level decreased.The 24-hour total urine volume decreased significantly(P<0.05),and the SG in the low-dose group increased significantly(P<0.05).When URO=3.2 μmol·L-1,urinary PRO could be recovered to negative after drug treatment.The levels of renal function injury indexes BUN,α1-MG and KIM-1 were significantly decreased(P<0.05,P<0.01,P<0.001);the renal index and Ccr levels of the rats in the administration group were significantly improved(P<0.05,P<0.01).At the same time,the related AQP2,TGF-β1 and HIF-1α protein expressions were improved.To sum up,it can be seen that the leech of the kidney leaf mountain can improve the renal histopathology and various indicators of chronic renal failure rats,reduce the degree of renal injury and renal fibrosis,and has a positive effect on the prevention and treatment of CRF in rats.

Objective To explore the effect and possible mechanism of petroleum ether extract from Gastrodia elata on A amyloid β-protein deposition in Caenorhabditis elegans(C.elegans).Methods C.elegans was used as the model organism,and the experiment was divided into blank group(Control group),GEPEE 0.5 mg·mL-1 group and GEPEE 1 mg·mL-1 group.The effects of GEPEE on paralysis,life span,oxidative stress,heat stress,reactive oxygen species(ROS)level and Aβ aggregation of C.elegans were investigated,qRT-PCR was used to detect the changes of gene expression related to insulin/IGF-1 signaling pathway(IIS)in C.elegans.The main components were analyzed by high performance liquid chromatography(HPLC).Results Compared with Control group,GEPEE could significantly improve the paralysis phenotype of C.elegans(P<0.01),prolong the lifespan of C.elegans(P<0.01),enhance the motility of C.elegans(P<0.01),and increased the resistance to external oxidative stress(P<0.01),the stress ability of high temperature(P<0.01),improved the deposition of Aβ in vivo(P<0.01),decreased the ROS content in C.elegans(P<0.01),decreased the expression levels of Aβ and DAF-2(P<0.01),increased the expression levels of DAF-16 and its target genes SOD-3,GSH-Px,HSF-1 and its target gene HSP-16.2,SKN-1 and its target gene GST-4(P<0.01).Its main components were p-hydroxybenzyl alcohol and p-ethoxylbenzyl alcohol by HPLC.This study showed that GEPEE can reduce Aβ-induced toxicity in CL4176 C.elegans by reducing ROS level in vivo,increasing antioxidant level and regulating IIS pathway.Conclusion GEPEE can inhibit the toxicity of Aβ protein,and its mechanism is related to the regulation of IIS signaling pathway.