Structure modification and anti-tumor activity evaluation on sesquiterpene lactones TBA and TBB from Sphagneticola trilobata.

Thirteen sesquiterpene lactone derivatives were designed and synthesised using the sesquiterpene lactone epimers TBA and TBB as the parent molecules, isolated from Sphagneticola trilobata. Their structures were elucidated by extensive spectroscopic studies and chemical evidence. Furthermore, the structures of 1a, 4b and 5a were confirmed by X-ray single-crystal diffraction analyses. All of the compounds were further examined for their in vitro antiproliferative activity against human cancer cell lines HeLa and MCF-7. Unfortunately, the activity of all derivatives were weaker than that of the parental compounds.

Value of DNA Repair Gene and TP53 Co-mutation in Predicting Effect of Immunotherapy on Lung Adenocarcinoma / 肿瘤防治研究

Objective To explore the value of DNA repair genes (DRGs) in predicting the effect of immunotherapy on lung adenocarcinoma based on second-generation sequencing technology. Methods The data of lung adenocarcinoma were obtained from the Cancer Genome Atlas, including the testing cohort and the validation cohort. In the testing set, according to the cut-off value of tumor mutational burden (TMB) score 15, the patients with lung adenocarcinoma were divided into two groups: the low TMB score group and the high TMB score group. And we analyzed the relation between TMB and the overall survival of lung adenocarcinoma patients. KRAS and TP53 co-mutation was used as the standard control, the differences in the mutation count and TMB score between only DRGs mutation group and KRAS or TP53 co-mutation groups were analyzed. In the validation cohort, the differences between DRGs and KRAS or TP53 co-mutation groups in TMB, tumor neoantigen burden and PFS were analyzed. Results The patients with TP53/DRGs co-mutation had higher mutation count and TMB score than those patients with only TP53 or DRGs mutation (P < 0.05). The patients with TP53/DRGs co-mutation had higher mutation count and TMB score than those patients with KRAS/TP53 co-mutation (P=0.037, P=0.044). In validation cohort analysis, the TP53/DRGs co-mutation patients also showed higher tumor neoantigens, higher TMB and longer progression-free survival than those patients with only TP53 or DRGs or KRAS/TP53 co-mutation groups. Conclusion TP53/DRGs co-mutation may be served as a pair of potential biomarkers for predicting the efficacy of immunotherapy on lung adenocarcinoma.

Design, synthesis and biological activity evaluation of a new class of 2,4-thiazolidinedione compounds as insulin enhancers.

Diabetes mellitus (DM) is a global disease with a high incidence of type 2 diabetes. Current studies have shown that insulin enhancers play an important role in the treatment of type 2 diabetes and have great importance in the improvement of type 2 diabetes. In this research, Rosiglitazone was taken as the lead compound, and the structure was modified by using the bioisostere principle, and a new class of 2,4-thiazolanedione compound was designed and synthesised. The novel series of compounds were studied for their biological activities in vitro and in vivo. In vitro tests, the biological activities showed that the target compounds have good selective activation of peroxisome-proliferator-activated receptor γ (PPARγ), such as the compounds 6a, 6e, 6f, 6g and 6i, especially the compound 6e to PPARγ was EC50 = 0.03 ± 0.01 µmol/L in vitro. Then, in vivo biological activities' test results showed that the tendency of increasing in blood sugar had an obvious inhibiting effect, and had a significant insulin hypoglycaemic effect of enhancing and extending the exogenous. In addition, the results of cytotoxicity tests and acute toxicity tests (LD50) showed that these compounds belong to the low toxicity compounds.

The features and diagnostic value of CT in cystitis glandularis / 中国基层医药

Objective To investigate the features and diagnostic value of computed tomography ( CT) in cys-titis glandularis .Methods The CT images and clinical data of 9 patients with cystitis glandularis confirmed by histol-ogy were studied retrospectively .Results The characteristics of cystitis glandularis ( location,shape,density and the relationship with adjacent tissues)were clearly displayed on CT.The lesion was located in the bladder trigone(n=5), right anterior wall(n=1),left posterior wall(n=2),diffuse lesion(n=1).According to the shape,8 lesions showed mass type,the range of these lesions were limited and some lesions were combined with cystic degeneration ,only one lesion showed a diffusely thickened bladder wall .After enhancement ,CT value increased from 14.0-45.0 HU to 25.0-62.0 HU.Conclusion CT has high sensitivity and accurate in diagnosis of cystitis glandularis .

The characterization on the site of vindoline binding to human serum albumin / 药学学报

In this paper, the fluorogenic property of vindoline was exploited and, as a probe, used to analyze the interaction of vindoline with HSA by fluorescence and absorption spectra in combination with molecular modeling under a simulated physiological conditions. The evidences from synchronous fluorescence and absorption spectroscopes showed the effect of vindoline on the microenvironment around HSA in aqueous solution. Data obtained by the fluorescence spectroscopy indicated that binding of vindoline with HSA leads to dramatic enhancement of the fluorescence emission intensity. The binding constants and the number of binding sites between vindoline and HSA at different temperatures (303, 310 and 317 K) were calculated according to the data obtained from fluorescence titration. Molecular docking was performed to reveal the possible binding mode or mechanism and suggested that vindoline can bind strongly to HSA. It is considered that vindoline binds to HSA mainly by a hydrophobic interaction and there are four hydrogen bonds interactions between the drug and the residues Ala291, Arg222, Arg218 and Lys195, separately. Fluorescent displacement measurements confirmed that vindoline bind HSA on site II. The thermodynamic parameters obtained (the enthalpy change deltaH0 and the entropy change deltaS0 were calculated to be -10.30 kJ x mol(-1) and 79.98 J x mol(-1) x K(-1), respectively, according to the Van't Hoff equation) suggested that hydrophobic and electrostatic interaction is the predominant intermolecular forces stabilizing the complex.

Clinical evaluation with pediatric clinical illness scores and pediatric risk of mortality in PICU / 中国小儿急救医学

Objective To evaluate the use of pediatric clinical illness score(PCIS) and pediatric risk of mortality(PRISM) in severe cases in pediatric intensive care unit(PICU). Methods 580 patients were divid-ed into groups according to PICS results, death and the numbers of organ failure. Severity, mortality were ana-lyzed. PRISM scores were also investigated in these groups respectively. Results The PRISM score of the ex-tremely-severe group was higher than that of the severe group and the non-severe group(P<0.01). The mean value of scores in death group was higher than that in survival group(P<0.01). The PRISM scores was in-creasing along with the growing numbers of organ failure (P<0.05). Conclusion Both PCIS and PRISM scores have good clinical value in assessing the severity and risk of death in patients in PICU.

STUDY ON THE ESSENTIAL OIL COMPONENTS IN THYMUS QUINQUECOSTATUS CELAK / 药学学报

AIM　To analyse the essential oil components of Thymus quinquecostatus Celak. METHODS　Gas chromatography/mass spectrometry were used. RESULTS　A total of 78 components were separated. 34 of them were identified, which accounted for 95.93% of the total peak area. The main constituents are o-cymene, carvacrol, caryophyllene, 2-isopropyl-1-methoxy-4-methylbenzene and γ-terpene. CONCLUSION　Thymus quinquecostatus Celak has perfume and medical development value.

Disposal of Essential Oil During Preparation Process of Solid Preparations Containing Ligusticum Chuanxiong and Angelica Dahurica / 中国药房

OBJECTIVE:To discuss the disposal of essential oil in the preparation process of solid preparations containing Ligusticum chuanxiong and Angelica dahurica.METHODS:Based on pertinent literature in recent years,the disposal of essential oil in the preparation process of solid preparations containing Ligusticum chuanxiong and Angelica dahurica was discussed from aspects of chemical components,pharmacology and extraction process etc.RESULTS & CONCLUSION:It is necessary to combine research on preparation process with the pharmacological effect and pharmacodynamic action,and to formulate effective measures to control quality of the essential oil during the whole preparation process to facilitate a solution for the disposal of essential oil.