Acid/Base-Co-catalyzed Formal Baeyer-Villiger Oxidation Reaction of Ketones: Using Molecular Oxygen as the Oxidant.

A novel acid/base-co-catalyzed formal Baeyer-Villiger oxidation of various ketones using O2 as the sole oxidant under metal-free conditions has been developed for the first time. The reaction tolerates a wide range of ketones and anilines and provides a simple and efficient method for the construction of various amides and isoquinolin-1-ones from the reactions of ketones with anilines in a single step.

Thermally induced formal [4+2] cycloaddition of 3-aminocyclobutenones with electron-deficient alkynes: facile and efficient synthesis of 4-pyridones.

A thermally induced novel formal [4+2] cycloaddition of cyclobutenones with electron-deficient alkynes under metal-free conditions has been developed for the first time. The reaction can proceed in a highly regioselective manner and provides a straightforward and efficient method for the synthesis of 4-pyridone derivatives from readily available starting materials in a single step.

[Expression Changes of ß-catenin and P-GSK-3ß in Patients with Mantle Cell Lymphoma].

OBJECTIVE: This study was purposed to detect the expressions of ß-catenin and P-GSK-3 ß in Wnt signaling pathway of patients with mantle cell lymphoma(MCL), and investigate its relationship with the pathogenesis of MCL. METHODS: The expression levels of ß -catenin protein and P-GSK-3 protein in mantle cell lymphoma and hyperplastic lymphadenitis were detected by using anti-ß-catenin, P-GSK-3ß polyclonal antibody and S-P staining technique. RESULTS: The abnormal expression of ß-catenin protein(73.33%) in mantle cell lymphoma group was significantly higher than that (6.7%) in reactive lymph node hyperplasia group (P<0.05); and the positive rate of P-GSK-3 ß(66.67%) in mantle cell lymphoma group was significantly higher than that (16.67%) in reactive hyperplasia of lymph node group (P<0.05). Spearman correlation analysis showed that there was obvious positive correlation (R=0.852, P<0.01). CONCLUSION: The abnormal high expressions of ß-catenin and P-GSK-3 ß protein have been confirmed to appeare in mantle cell lymphoma.

[Antiproliferative Effect of Specific Inhibitor XAV939 for ß-catenin on MCL Jeko-1 Cells].

OBJECTIVE: To investigate the effect of short hairpin RNA (shRNA) and XAV939, a specific inhibitor for ß-catenin, on growth and apoptosis of mantle cell lymphoma(MCL) Jeko-1 cell line. METHODS: ß-catenin shRNA eukaryotic expression vector was transfected into Jeko-1 cells, the antiproliferative effect of shRNA on Jeko-1 cells was detected by RT-PCR and Western blot. The proliferation inhibitory rate of Jeko-1 cells treated by different doses of XAV939 was assayed by MTT method; the level of apoptosis of Jeko-1 cells was detected by flow cytometry; the expression levels of apoptosis-related protein BCL-2, BAX, CyclinD1, C-MYC and Caspase-3 in Jeko-1 cells were determined by Western blot. RESULTS: The expression of ß-catenin mRNA and growth of Jeko-1 cell line were inhibited by shRNA; after Jeko-1 cells treated with 0,2 and 8 µmol/L XAV939 for 48 hours, the cell proliferation rate decreased, while the cell apoptosis rate increased, the expressions of apoptosis-related protein BCL-2, CyclinD1 and C-MYC were down-regulated, on the contrary, the expression of BAX and caspase-3 were up-regulated. CONCLUSION: The specific inhibition of ß-catenin can inhibit Jeko-1 cell proliferation and promote the cell apoptosis.

[Study on aberration in histone methylation and acetylation in acute leukemia].

OBJECTIVE: To study the aberration in histone H3K4 and H3K9 methylation and H3 and H4 acetylation in human acute leukemia (AL) cells. METHODS: The histone H3K4 and H3K9 methylation and H3 and H4 acetylation were detected by Western blot in 34 AL patients and 13 controls (9 non leukemia patients, 4 healthy volunteers). RESULTS: The level of H3K4 methylation was significantly lower in 19 AL patients than in non leukemia (0.220 ± 0.096 vs 0.447 ± 0.186, P < 0.01), while the level of H3K9 methylation was significantly higher (0.409 ± 0.106 vs 0.168 ± 0.015, P < 0.01); Both level of histone H3 and H4 acetylation in 15 AL patients were significantly lower (H3: 0.128 ± 0.013 vs 0.386 ± 0.104, H4: 0.096 ± 0.008 vs 0.341 ± 0.096, respectively, both P < 0.01). CONCLUSION: Aberration of histone methylation and deficient histone acetylation in AL may represent the markers for an aberrant post-translational modification of histones and chromatin structure. It might be a potential epigenetic target for anti-leukemia agent.