Convenient synthesis of N-alkyl-3,1-benzoxazin-2-ones from carbamate protected anthranil aldehydes and ketones via one-step alkylation/alkoxy rearrangement.

A practical and step-economical protocol was developed to prepare N-alkyl-3,1-benzoxazin-2-one derivatives from anthranil aldehydes and ketones via one-step alkylation/alkoxy rearrangement, where three new chemical bonds and one ring were constructed in a single step. Control studies revealed a stepwise mechanism and that the alkoxy rearrangement was an intermolecular process.

High expression of PPM1G is associated with the progression and poor prognosis of hepatocellular carcinoma.

BACKGROUND: PPM1G, a member of the serine/threonine protease family, dephosphorylates various proteins and may be involved in cancer development. The role and mechanism of PPM1G in HCC still needs to be verified. OBJECTIVE: This study aims to explore the role of PPM1G in the occurrence, development and prognosis of HCC. METHODS: Using bioinformatics (UALCAN, cBioPortal, Linkedomics, STRING and GSEA) to analyze the expression of PPM1G mRNA in HCC, its clinical relevance and possible involved signaling pathways. The expression of PPM1G protein was determined by immunohistochemistry in 311 cases of HCC to evaluate the association between PPM1G and clinical features and prognosis. RESULTS: The expression of PPM1G was significantly upregulated in HCC (P< 0.001), correlated with the metastasis (P= 0.020), pathological grade of HCC (P= 0.032), microvascular invasion (P= 0.040), and HBV infection (P= 0.041). Cox multivariate regression showed high expression of PPM1G was an independent prognostic factor for HCC. Its role in HCC may relate to methylation and frequency mutation. Furthermore, the database showed PPM1G is involved in the signal pathway such as cell cycle, WNT pathway, and mTOR pathway in HCC. CONCLUSION: PPM1G showed an essential function involving in tumor-related pathways in HCC, providing a biological basis for targeted treatment of HCC clinically.

High Expression of SLC41A3 Correlates with Poor Prognosis in Hepatocellular Carcinoma.

PURPOSE: SLC41A3 is a member of the solute carrier family 41 (SLC41) and is involved in many cellular processes as a magnesium ion transporter. Although it plays an important role in cancer formation and development, the correlation between the expression of SLC41A3 and the occurrence and prognosis of hepatocellular carcinoma (HCC) remains unclear. Therefore, this study was focused on the evaluation of the relationship between SLC41A3 and the development and prognosis of HCC. PATIENTS AND METHODS: Firstly, we collected the mRNA expression of SLC41A3 in HCC through the platform of Oncomine. Then, the subgroups of HCC were performed by the UALCAN website and the prognosis of HCC was analyzed by Kaplan-Meier Plotter database. Subsequently, immunohistochemistry (IHC) method was used to detect SLC41A3 expression in 323 clinically confirmed HCC samples and 184 non-cancerous liver tissues. Finally, function enrichment analysis was done using the LinkInterpreter module in LinkedOmics, and gene set enrichment analysis (GSEA) was performed using TCGA data set. RESULTS: The Oncomine database and immunohistochemical (IHC) showed higher SLC41A3 expression in HCC tissue compared to normal tissue. The expression of SLC41A3 was significantly correlated with tumor metastasis, Edmondson grade, microvascular invasion, and AFP level. Kaplan-Meier and Cox regression analyses verified that high SLC41A3 expression is a significant prognostic factor for reduced overall survival in HCC patients. CONCLUSION: Our results demonstrated that high expression of SLC41A3 was the predictor of poor prognosis in HCC patients, suggesting that this protein may be a potential target for HCC therapy.

KLF7 Affects Development of Broiler Adipose Tissue by Inhibiting Hypoxia￣Inducible Factor 1 Alpha Transcription / 中国生物化学与分子生物学报

Krüppel-like factor 7 (KLF7) is a negative regulator of adipogenesis, whereas hypoxia-inducible factor 1 (HIF1) promotes anoxic-induced adipose tissue development in mammals. Our previous ChIP-seq analysis showed that one of the KLF7 binding peaks was present upstream of hypoxia-inducible factor 1 alpha (HIF1α), indicating that KLF7 may regulate HIF1α transcription. For this purpose, ChIP-PCR was used to verify ChIP-seq results, which showed that KLF7 directly bound to the HIF1α upstream region. Dual luciferase reporter and qRT-PCR results showed that KLF7 overexpression significantly decreased the luciferase reporter activity of HIF1α (- 4 432/- 4 182) (P < 0. 01) and inhibited HIF1α expression. After the deletion of KLF7 binding motif “TGCGCAGCAA” (- 4 300/-4 290) predicted by bioinformatics, the luciferase reporter activity of HIF1α (-4 432/-4 182) was significantly enhanced compared with wild-type plasmid (P<0. 01). Furthermore, Northeast Agricultural University broiler lines divergently selected for abdominal fat content (NEAUHLF) at the age of 1-7 weeks from the 19

Application of central composite design in optimization of the formulation of aspirin ointment / 中国药学杂志

OBJECTIVE: To optimize the formulation of aspirin ointment. METHODS: With cumulative permeation quantity within 6 h and shin irritation as indexes, the method of central composite design was used to optimize the formulation of aspirin ointment, taking the most important three ingredients including sodium lauryl sulfale(X1), sodium citrate (X2) and triethanolamine (X3) as the study subjects. RESULTS: The optimized formulation of aspirin ointment was composed of 1.41% sodium lauryl sulfate, 3.5% sodium citrate and 3.0% triethanolamine. Three batches of aspirin ointment were prepared using the optimized formulation, for which the average cumulative permeation quantity within 6 h was 990.18 μg · cm-2, and no obvious shin irritation was observed. CONCLUSION: Central composite design is successfully used lo optimize the formulation of aspirin ointment.