A series of novel 4-substituted-3-nitrobenzamide derivatives were designed and synthesized. The structures of the target compounds were confirmed with 1H NMR, 13C NMR, MS and element analysis. Anti-tumor activities against HCT-116, MDA-MB435 and HL-60 cell lines in vitro were evaluated by SRB assay. The results indicated most of the target compounds exhibited potent anti-tumor activity. Compound 4a showed the most potent inhibitory activities against three cancer cell lines with the GI50 values of 1.904-2.111 micromol x L(-1). Compounds 4g, 41-4n exhibited more potent inhibitory activities against MDA-MB435 and HL-60 cell lines with the GI50 values of 1.008-3.586 micromol x L(-1) and 1.993-3.778 micromol x L(-1), respectively. The structure-activity relationship of these compounds is discussed preliminarily.
Antineoplastic Agents ; chemical synthesis ; pharmacology ; Benzamides ; chemical synthesis ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; Drug Design ; HL-60 Cells ; Humans ; Inhibitory Concentration 50 ; Structure-Activity Relationship

To report the clinical course of 5 cases of pediatric plastic bronchitis and review the related literature.A total of 113 cases of pediatric plastic bronchitis occurring in China from 2000 to 2012 were retrieved through the databases of CNKI and Wanfang Med Online.Retrospective analyses were performed for the main symptoms,courses,etiologies,imaging findings,histopathological classifications,therapies and prognosis of 118 cases.Pediatric plastic bronchitis was one of critical diseases.Most of them had a rapid onset and a mortality rate.Bronchoscopy examination was essential for definite diagnosis and effective treatment.Airway management and chest physiotherapy were primary adjuvant tools.Early diagnosis and bronchoscopic treatment might result in improved prognosis.

Objective:To investigate the impact of aging on the correlation between the intestinal microorganism Akkermansia and obesity, and to analyze the features of the correlation in the elderly population. Methods:This was a cross-sectional study.A total of 6896 cases were collected from the Guangdong intestinal microbiome in 2018, aged 18-94 years old, including 3806 females, 1641 cases with abdominal obesity(23.7%)and 707 cases with systemic obesity(10.3%). The 16S rRNA sequencing data were from individuals of Cantonese descent.The abundance of Akkermansia was calculated after data cleaning, clustering and annotation.The type of abdominal obesity or systemic obesity was diagnosed based on the standards of the Working Group on Obesity in China(2002). According to the five quintiles of the abundance of Akkermansia, subjects were divided into Q1~Q5(Q1-Q4: n=1379, Q5: n=1380). Logistic regression was used to study the relationship between Akkermansia and obesity after adjusting for common confoundors such as gender.Subjects were subgrouped into two types of age groups: the <65 group(n=5467)and the ≥65 group(n=1519); the <70 group(n=6136)and the ≥70 group(n=850). Age windows were used to analyze changes in characteristics of this relationship with increasing age. Results:There were significant differences in age and gender among different Akkermansia groups( t/ χ2=3.51, -5.03, P<0.01). Logistic regression analysis showed that after adjusting for two main confounding factors, age and gender, the risk of systemic obesity and abdominal obesity gradually decreased from Q2 to Q5 group, compared with Q1 group( P<0.001). The correlation between Akkermansia and obesity decreased with age.The protective effect of Akkermansia on obesity was weaker in the ≥65 and ≥70 groups, respectively, than in the <65 and <70 groups. Conclusions:Akkermansia is a protective factor for obesity, but the protective effect is affected by aging and weakened in the elderly.

Objective To investigate the clinical value of prenatal MRI in the diagnosis and differential diagnosis of congenital bronchopulmonary sequestration (BPS). Methods From January 2009 to December 2014, 16 fetuses with BPS were diagnosed by fetal MRI in Huzhou Maternity and Child Care Hospital and Shanghai Children′s Medical Center Affiliated to Shanghai Jiaotong University School of Medicine. The clinical data of these cases were analyzed retrospectively. All were singleton pregnancy, and MRI was carried out within 24-48 hours after routine prenatal ultrasound. All the neonates underwent postnatal enhanced CT scan or surgical biopsy after birth, and the results were compared to prenatal MRI diagnosis. Results (1)With prenatal MRI, 16 cases were diagnosed BPS. The lesions located in left lung in 10 cases, and right lung in 6 cases. As the scope of the lesion, 3 cases located in the whole left lung, 6 cases limited to the left lower lobe, and 1 case was subdiaphragmatic on the left side. 2 cases located in the whole right lung and 4 cases limited to the right lower lobe. One case complicated oligoamnios, and one had pleural effusion. Supplying vessels could be found in 14 cases.(2)When the postnatal results were compared with prenatal MRI, 15 cases were comfirmed as BPS (15/16), including 10 intralobar cases 5 extralobar cases. One that was diagnosed as BPS by prenatal MRI was confirmed to be congenital cystic adenomatoid malformation (CCAM) by pathology. The accuracy of prenatal MRI diagnosis of BPS was 15/16. Prenatal ultrasound missed one case and misdiagnosed two cases, as one was mistakened as CCAM and the other as cystic teratoma. Conclusion Prenatal MRI has good clinical value in the diagnosis and differential diagnosis of fetal BPS.

Background and purpose:Edible fungi has shown powerful potential in health care. This study aimed to explore the anti-tumor and immunoenhancement effects of combination of extraction from edible fungi. Methods:C26 cells has been xenografted into mice, and the animal models were randomly divided into control group, prevention group, treatment group and cyclophosphamide group. Mice were given the combination of extraction from edible fungi every day after vaccination of C26 cells into mice, except the prevention group which has been given the combination of extraction from edible fungi two weeks before vaccination. Two weeks after being planted, all the mice were killed and the tumor inhibition rates were studied. The immune function was measured by T lymphocyte transforming assay and NK killing assay. Results:There were signif icant difference in terms of tumor weight between prevention group and control group. The prevention group mice display improved T lymphocyte transforming assay and NK killing ability. Conclusions:The combination of extraction from edible fungi has remarkable inhibitory effects on C26 carcinoma in mice and can enhance immunity against mice with C26 carcinoma.

Objective To evaluate the therapeutic effects of somatostatin(stilamin)and rhubarb for severe acute pancreatitis(SAP).Method A total of 42 patients with SAP received traditional treatment in combination with somatostatin(stilamin)and rhubarb,and compared with 40 SAP patients with routine treatment.The changes of acute physiology and chronic health evaluationⅡ(APACHEⅡ),serum amylas,serum creatinine,blood calcium,blood glucose,white blood cell count,the duration of abdominal pain,abdominal bulge,fast and hospital stay,complications,morlality and operation rate on the fist day,third day and fifth day were compared between two groups.Results Somatostatin and rhubarb reduced the complications,operation rate and mortality, and shortened the duration of abdominal pain,abdominal bulge,fast and hospital stay.Conclusions Combination of somatostatin and rhubarb is effective in the treatment of SAP patients.

A series of [1,3]dioxolo[4,5-f]isoindolone derivatives were designed, synthesized and evaluated as inhibitors of acetylcholinesterases (AChE). Furthermore, their effects on memory impairment of mice induced by scopolamine were investigated with step-through test. The results suggested that most of the target compounds exhibited potential inhibition on AChE with IC50 values at micromolar range. Compounds I1 (IC50 value of 0.086 μmol · L(-1)) and I2 (IC50 value of 0.080 μmol · L(-1)) showed the strongest AChE inhibitory activity, which are equipotent to donepezil (IC50 value of 0.094 μmol · L(-1)). Moreover, compounds I1-I4 could improve the memory impairment induced by scopolamine in mice.
Animals ; Cholinesterase Inhibitors ; chemical synthesis ; chemistry ; Dioxoles ; chemical synthesis ; chemistry ; Drug Design ; Indans ; Inhibitory Concentration 50 ; Isoindoles ; chemical synthesis ; chemistry ; Memory Disorders ; drug therapy ; Mice ; Piperidines ; Scopolamine Hydrobromide

Objective To determine the epidemiological features of hand-foot-and-mouth disease (HFMD) outbreaks and the genetic characteristics of enterovirus type 71 (EV71) isolates from patients in Lianyungang, Jiangsu province in May, 2008. Methods Epidemiological, microbiological, cellular and molecular methods were performed to investigate pathogens and to describe the homogeneity of isolated strains. Results 21 cases were reported in this HFMD outbreak with the attack rate as 20.0%. 3 EV71 virus strains were isolated from 10 stool samples. The nucleotide and amino acid homogeneity of these 3 Jiangsu strain with Anhui Fuyang strains were 97.9%-100.0% and 99.7%-100.0%, respectively. These 4 Jiangsu strains were within genotype C sub-geno group C4 in phylogenetic tree. Data from the follow-up study showed that shedding of EV71 and Coxsackie A 16 virus (CA 16) in the latent period appeared in the outbreak of HFMD. Human beings could be infected by both EV71 virus and CA16 at the same time and could also carry the two viruses. We also discovered that EV71 virus could be expelled out of the human body through stool in the fast week and last for 10 weeks. Conclusion The recently identified EV71 isolates from this HFMD outbreak belonged to sub-geno group CA. Facts as: the release of viruses in the latent period, co-infection or coexisting of two viruses at the same time and super long period of expulsion of toxin exist in EV71 and CA16 did exist.

The study aimed to investigate the impact of intraclot recombinant tissue-type plasminogen activator (rt-PA) on perihematomal edema (PHE) development in patients with intracerebral hemorrhage (ICH) treated with minimally invasive surgery (MIS) and the effects of intraclot rt-PA on the 30-day survival. We reviewed the medical records of ICH patients undergoing MIS between October 2011 and July 2013. A volumetric analysis was done to assess the change in PHE and ICH volumes at pre-MIS (T1), post-MIS (T2) and day 10-16 (T3) following diagnostic computed tomographic scans (T0). Forty-three patients aged 52.8±11.1 years with (n=30) or without rt-PA (n=13) were enrolled from our institutional ICH database. The median rt-PA dose was 1.5 (1) mg, with a maximum dose of 4.0 mg. The ratio of clot evacuation was significantly increased by intraclot rt-PA as compared with controls (77.9%±20.4% vs. 64%±15%; P=0.046). From T1 to T2, reduction in PHE volume was strongly associated with the percentage of clot evacuation (ρ=0.34; P=0.027). In addition, PHE volume was positively correlated with residual ICH volume at the same day (ρ ranging from 0.39-0.56, P<0.01). There was no correlation between the cumulative dose of rt-PA and early (T2) PHE volume (ρ=0.24; P=0.12) or delayed (T3) PHE volume (ρ=0.19; P=0.16). The 30-day mortality was zero in this cohort. In the selected cohort of ICH patients treated with MIS, intraclot rt-PA accelerated clot removal and had no effects on PHE formation. MIS aspiration and low dose of rt-PA seemed to be feasible to reduce the 30-day mortality in patients with severe ICH. A large, randomized study addressing dose titration and long-term outcome is needed.