In order to search for new antiplatelet agents with higher potency, a series of tetramethylpyrazine ( TMP) /chalcone hybrids ( 2-26) were synthesized and evaluated based on the principle of bioisostere and hybrid-ization. They exerted inhibitory activity against adenosine diphosphate ( ADP )-induced and arachidonic acid ( AA)-induced platelet aggregation to varied extent. Among them, compound 8 was the most potent with IC50 of 0. 14 mmol/L on ADP-induced platelet aggregation ( 9. 1 folds of TMP and 10. 5 folds of chalcone ) and 0. 09 mmol/L on AA-induced platelet aggregation ( 8. 8 folds of TMP and 10. 0 folds of chalcone) , which was superior to clinically used anti-platelet drug aspirin ( ASP, IC50 =0. 15 mmol/L) .

Background and purpose:Gastric-type endocervical adenocarcinoma(G-EAC)is a rare variant of endocervical adenocarcinoma,characterized by atypical clinical manifestations and elusive lesions.Due to these factors,G-EAC is prone to being missed or misdiagnosed,significantly impacting the prognosis.Lobular endocervical glandular hyperplasia(LEGH)and atypical LEGH(aLEGH)are considered to be precancerous lesions of G-EAC.These conditions also present overlapping clinical,pathologic and imaging manifestations,making it challenging to differentiate between them preoperatively.The purpose of this study was to investigate the correlation between magnetic resonance imaging(MRI)findings of cystic-solid lesions in the cervix and their underlying pathology in order to enhance the accuracy of distinguishing between LEGH and G-EAC,ultimately aiding in the early diagnosis and appropriate management of these conditions.Methods:Clinical,imaging and pathological data of 37 LEGH and 53 G-EAC patients who attended the Obstetrics and Gynecology Hospital of Fudan University from July 2016 to August 2023 were collected.Analysis was conducted using Pearson Chi-square χ2,Fisher's exact tests and so on.Multivariate analyses were performed using logistic regression.Receiver operating characteristic(ROC)curves were used for performance evaluation.Results:In this study,differences in age,symptoms,extent,size,composition,degree of enhancement,cervical stromal ring,endometrium invasion,pelvic lymph nodes enlargement,and hydrohystera were statistically significant between the two groups(P＜0.05).In the LEGH and aLEGH groups,lesions were primarily localized to the epithelial layer of the endocervical canal.These lesions were predominantly simple cystic(32/37),and the cystic walls often displayed significant enhancement(31/37).In contrast,the G-EAC group presented with lesions involving the myometrium of the uterine cervix(42/53).These lesions were characterized by a solid component in the majority of cases(52/53),a tendency for the disappearance of the cervical stromal ring(46/53).Logistic regression analysis revealed that among the MRI features,lesion composition(OR=50.064)and incomplete cervical stromal ring(OR=40.180)were significant predictors for G-EAC.ROC analysis,incorporating lesion size,composition,enhancement degree,cervical stromal ring,and endometrial involvement,yielded an area under curve(AUC)of 0.970(95%CI:0.931-1.008).Conclusion:Combining multiple MRI features of cystic-solid lesions in the cervix aids in distinguishing between LEGH and G-EAC.

The novel oleanolic acid derivatives 2a-2e were synthesized by introducing an α, β-unsaturated ketone moiety to C-ring of oleanolic acid(OA)via a nine-step reaction sequence, yielding an active CDDO-Me analogue(1), followed by coupling of C3-OH of 1 with various aliphatic and aromatic carboxylic acids, respectively. Derivatives 3a-3e were synthesized by substituting C-1 of compounds 2a-2e with bromine. The target compounds were characterized by IR, MS and 1H NMR spectra. All the target compounds showed strong inhibitory effects against two tumor cell lines(HepG2 and A549)to a varying extent. The anti-proliferative activities of active compounds 3b and 3c(IC50=6. 13±1. 16 μmol/L and IC50=5. 49±1. 03 μmol/L, respectively)against HepG2 and A549 were more potent than compound 1 and comparable to the positive control CDDO-Me. In addition, all the target compounds displayed much weaker anti-proliferative activity against the two tumor cell lines than that against normal BEAS-2B cells. Compound 3c showed ten-fold selective inhibition against HepG2 relative to BEAS-2B cells, and is thus worthy of further study.

Objective:To investigate the spectrum of pathogenic agents in pediatric patients with acute respiratory infections (ARI) during the outbreak of coronavirus infectious diseases 2019 (COVID-19).Methods:Three groups of children were enrolled into the prospective study during January 20 to February 20, 2020 from Capital Institute of Pediatrics, including children in the exposed group with ARI and epidemiological history associated with COVID-19 from whom both pharyngeal and nasopharyngeal swabs were collected, children in the ARI group without COVID-19 associated epidemiological history and children in the screening group for hospital admission, with neither COVID-19 associated epidemiological history nor ARI. Only nasopharyngeal swabs were collected in the ARI group and screening group. Each group is expected to include at least 30 cases. All specimens were tested for 2019-nCoV nucleic acid by two diagnostic kits from different manufacturers. All nasopharyngeal swabs were tested for multiple respiratory pathogens, whilst the results from the ARI group were compared with that in the correspondence periods of 2019 and 2018 used by t or χ 2 test. Results:A total of 244 children were enrolled into three groups, including 139 males and 105 females, the age was (5±4) years. The test of 2019-nCoV nucleic acid were negative in all children, and high positive rates of pathogens were detected in exposed (69.4%, 25/36) and ARI (55.3%, 73/132) groups, with the highest positive rate for mycoplasma pneumoniae (MP) (19.4%, 7/36 and 17.4%, 23/132, respectively), followed by human metapneumovirus (hMPV) (16.7%, 6/36 and 9.8%, 13/132, respectively). The positive rate (11.8%, 9/76) of pathogens in the screening group was low. In the same period of 2019, the positive rate of pathogens was 83.7% (77/92), with the highest rates for respiratory syncytial virus (RSV) A (29.3%, 27/92), followed by influenza virus (Flu) A (H1N1) (19.6%, 18/92) and adenovirus (ADV) (14.1%, 13/92), which showed significant difference with the positive rates of the three viruses in 2020 (RSV A: χ 2=27.346, P<0.01; FluA (H1N1): χ 2=28.083, P<0.01; ADV: χ 2=7.848, P=0.005) . In 2018, the positive rate of pathogens was 61.0% (50/82), with the highest rate for human bocavirus (HBoV) (13.4%, 11/82) and followed by ADV (11.0%, 9/82), and significant difference was shown in the positive rate of HBoV with that in 2020 (χ 2=6.776, P=0.009). Conclusions:The infection rate of 2019-nCoV is low among children in Beijing with no family clustering or no close contact, even with epidemiological history. The spectrum of pathogens of ARI in children during the research period is quite different from that in the previous years when the viral infections were dominant. MP is the highest positively detected one among the main pathogens during the outbreak of COVID-19 in Beijing where there is no main outbreak area.