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Two isopentenyl resorcinols, peperobtusin B and peperobtusin C, have been isolated from Peperomia tetraphylla. Their structures were determined on the basis of spectroscopic methods, especially 1H ...

PurposeTo develop a risk stratification system that can predict axillary lymph node (LN) metastasis in invasive breast cancer based on the combination of shear wave elastography (SWE) and conventional ultrasound.Materials and MethodsA total of 619 participants pathologically diagnosed with invasive breast cancer underwent breast ultrasound examinations were recruited from a multicenter of 17 hospitals in China from August 2016 to August 2017. Conventional ultrasound and SWE features were compared between positive and negative LN metastasis groups. The regression equation, the weighting, and the counting methods were used to predict axillary LN metastasis. The sensitivity, specificity, and the areas under the receiver operating characteristic curve (AUC) were calculated.ResultsA significant difference was found in the Breast Imaging Reporting and Data System (BI-RADS) category, the “stiff rim” sign, minimum elastic modulusof the internal tumor and peritumor region of 3 mm between positive and negative LN groups (p < 0.05 for all). There was no significant difference in the diagnostic performance of the regression equation, the weighting, and the counting methods (p > 0.05 for all). Using the counting method, a 0–4 grade risk stratification system based on the four characteristics was established, which yielded an AUC of 0.656 (95% CI, 0.617–0.693, p < 0.001), a sensitivity of 54.60% (95% CI, 46.9%–62.1%), and a specificity of 68.99% (95% CI, 64.5%–73.3%) in predicting axillary LN metastasis.ConclusionA 0–4 grade risk stratification system was developed based on SWE characteristics and BI-RADS categories, and this system has the potential to predict axillary LN metastases in invasive breast cancer.

GPR35受体是G蛋白偶联受体家族中的孤儿受体, 它的很多生物学功能还不是很清楚. 寻找发现GPR35受体的配体对于GPR35受体的生物学及药理学研究具有重要意义. 本研究利用无标记细胞靶点药理学筛选技术, 系统研究了天然黄酮类化合物对GPR35受体的激动活性, 新发现了草质素和异补骨脂二氢黄酮具有GPR35受体激动活性, 其中草质素 EC 50=(1.452±0.093) μmol/L, 是最具药物开发潜力的一个GPR35受体激动剂.

Background: Danshen is an important traditional Chinese medicine (TCM) used for the treatment of cardiovascular and cerebrovascular diseases. Separation and analysis of its components have been widely investigated. However, the systematical two dimensional liquid chromatography (2D-LC) methods have not been developed to comprehensively separate and characterize its components. Objective: In this work, double off-line 2D-LC methods were aimed to develop for the systematical separation of compounds from Danshen. Methods: Using solid phase extraction (SPE), the Danshen extract was divided into a medium-polar fraction (Sample I) and a weak-polar fraction (Sample II) according to their polarities. Based on reversed-phase liquid chromatography (RPLC) and hydrophilic interaction liquid chromatography (HILIC) modes, a 2D-HILIC × RPLC system and a 2D-RPLC × RPLC system were designed for the separation of Sample I and Sample II, respectively. According to reversed-phase and HILIC columns selectivities characterized in our previous reports, ZIC-HILIC and XTerra C18 were employed to build the 2D-HILIC × RPLC system and Click TE-CD and XTerra C18 for the 2D-RPLC × RPLC system, respectively. Results: The 2D-HILIC × RPLC and 2D-RPLC × RPLC systems exhibited excellent orthogonality for the separation of Sample I and Sample II, respectively. Their orthogonalities were 88.42% and 63.24%. Based on these double 2D-LC systems combined with mass spectrometry, at least 200 compounds were found and 33 compounds of them were identified, including 16 phenolic acids and 17 diterpenoid quinines. Conclusion: These results suggest that these two off-line 2D-LC methods are effective for the separation and characterization of components in Danshen.

Traditional Chinese medicines (TCMs) have been used in the clinic for thousands of years. Their reliable therapeutic efficacies are closely related to their multi-target mechanisms of action (MOAs). Discovery of these targets is important for understanding their clinical features. Danshen is the dried root of Salvia miltiorrhiza, a Traditional Chinese Medicine (TCM) used for the treatment of cardiovascular and cerebrovascular diseases. Although its clinical features are well recognized, the targets of its active constituents are poorly understood. Here, a label-free cell phenotypic assay was used to investigate the potential targets of the phenolic acids in danshen. Pharmacological profiling of 10 known phenolic acids in danshen using HT-29 and A431 cells revealed that lithospermic acid, salvianolic acid A, salvianolic acid B, salvianolic acid C and danshensu all displayed agonistic activity towards GPR35; however, salvianolic acid A and salvianolic acid C at high doses were also active in altering intracellular Ca2+ via another unknown target. Since GPR35 has been implicated in inflammation and cardiovascular diseases, the discovery of GPR35 as one target of the phenolic acids in danshen was useful for elucidating their mechanisms of action in the treatment of these diseases. This study also highlights the potential of label-free cell phenotypic assays for discovering multiple targets of TCMs.