Visible-light enabled room-temperature dealkylative imidation of secondary and tertiary amines promoted by aerobic ruthenium catalysis.

Employing sulfonyl azide as a nitrogen donor, a visible-light-enabled aerobic dealkylative imidation of tertiary and secondary amines involving C(sp3)-C(sp3) bond cleavage with moderate to excellent yields at room temperature is described. It has been demonstrated that this imidation could take place spontaneously upon visible-light irradiation, and could be facilitated considerably by a ruthenium photocatalyst and oxygen. An alternative mechanism to the previous aerobic photoredox pathway has also been proposed.

Evaluation of Two Parts of Lithocarpus polystachyus Rehd. from Different Chinese Areas by Multicomponent Content Determination and Pattern Recognition.

The purpose of this work is to establish a new method using high-performance liquid chromatography-diode array detection (HPLC-DAD) with chemometrics analysis to determine the content of catechin, isoquercetin, astragalin, phloridzin, trilobatin, and phloretin for one flavanol and five flavonoids, filter out the key compounds, and evaluate the quality of 26 batches of tender leaves and flower spikes of Lithocarpus polystachyus Rehd. (LP) from ten areas in China. The result showed that the HPLC-DAD method had excellent performance for accurate quantification analysis. S3 (tender leaf from Lushan, Sichuan) had the highest contents for six measured chemicals with trilobatin content of up to 27.82% in dry weight. S22 (flower spike from Liangping, Chongqing) had the highest content of phloridzin (up to 7.28%). All samples were divided into three types based on spatial distribution using principal component analysis. The result showed that the tender leaves and flower spikes from the same areas had many similar properties, and there were significant differences between the samples from different regions. Furthermore, phloridzin and trilobatin were identified as chemical markers for quality evaluation of two parts with different tender leaves and flower spikes of LP from geographical areas by orthogonal partial least squares discrimination analysis. These results will be helpful to establish an effective and comprehensive evaluation system of the development and utilization of LP resources.

Metal-free C-H amination of arene with N-fluorobenzenesulfonimide catalysed by nitroxyl radicals at room temperature.

A TEMPO-catalysed direct amination of arene through C-H bond cleavage employing N-fluorobenzenesulfonimide (NFSI) as the amination reagent in good to excellent yields with broad arene scope in the absence of any metal, ligand or additive is reported. Unlike previous transition metal-catalysed aminations in which high reaction temperatures are usually necessary, this novel reaction at room temperature is the first example of C-H amination with NFSI that is realised via organocatalysis. The probable mechanism of this concise amination is also proposed.

[Proliferation regulation effect of cyclin G1 antisense oligodeoxy-nucleotides with liposomal transfection on HL-60 cell].

To investigate the effect of cyclin G1 antisense oligodeoxynucleotide (ASON) with liposomal transfection on mediating proliferation of HL-60 cell, the cyclin G1 ASON with liposomal transfection was used in vitro in co-culture with HL-60 cell, the protein and mRNA expression levels of cyclin G1 were measured by immunocytochemistry assay and RT-PCR. The cell apoptosis was detected by electron microscopy, in situ cell apoptosis detection kit (POD), DNA gel electrophoresis and flow cytometry (FCM). The results showed that in the cyclin G1 ASON group the protein and mRNA expression of cyclin G1 were significantly inhibited as compared with sense oligodeoxynucleotide (SON) group and blank group. When the ASON concentration increased, the proliferation ratio of HL-60 cell and CFU of HL-60 were also significantly inhibited. There was apoptosis of HL-60 cell. In conclusion, cyclin G1 ASON can specifically inhibit its protein and mRNA expression levels as well as the HL-60 cell proliferations and can accelerate the apoptosis of leukemia cells with concentration-dependent effect of ASON.

[Effect of liposomal transfection of cyclin A antisense oligodeoxynucleotide (ASON) on HL-60 cell proliferation and apoptosis].

OBJECTIVE: To explore the effect of liposomal transfection of cyclin A antisense oligodeoxynucleotide (ASON) on HL-60 cell proliferation and apoptosis. METHODS: By liposomal transfection, cyclin A ASON was co-cultured with HL-60 cells, the cell growth curve was determined by MTT assay and cell apoptosis electron-microscopy in situ cell apoptosis detection kit (POD), the protein and mRNA of cyclin A and bcl-2 were measured by FACS and RT-PCR, the role of cyclin A ASON in the development of leukemia was tested by the tumor formation in nude mice. RESULTS: (1) In the cyclin A ASON liposomal transfection group (group A), the proliferation of HL-60 cell was significantly inhibited as compared to those in cyclin A ASON group (group B) (68.9% vs 24.8%) (P < 0.01). (2) The expressions of cyclin A and bcl-2 of group A were significantly lower than those in the control group (1.1% vs 38.8%, P < 0.01; 21.9% vs 65.0%, P < 0.01, respectively), and the DNA ladder and apoptosis body was displayed. (3) In group A, the rate of tumor formation in nude mice was lower, the time for tumor formation was longer and the volume of tumor was smaller than those in control group. CONCLUSION: Liposomal transfection of cyclin A ASON can inhibit in vitro proliferation of leukemia cells and induce in vivo apoptosis of the tumor cell, which might provide a new target for gene therapy.

[Effect of cyclin G1 antisense oligodeoxynucleotides (ASON) on the growth of HL-60 cells in nude mice].

OBJECTIVE: To study the inhibition effect of cyclin G(1) antisense oligodeoxynucleotides (ASON) on the growth of HL-60 cells in nude mice. METHODS: (1) Nude mice were divided into control group, sense oligodeoxynucleotides (SON) group and ASON group. After (60)Co radiation, with HL-60 cells SON group and ASON group were subcutaneously innoculated; (2) The weight and volume of tumors were continually measured; (3) The morphology of tumor cells was observed by microscope; (4) The protein and mRNA expression levels of cyclin G(1) were determined by flow cytometry (FCM) and reverse transcription polymerase chain reaction (RT-PCR); (5) The cell apoptosis was detected by electron microscopy and FCM. RESULTS: (1) The inhibition rate of tumor in ASON group was 69.4%. In ASON group, the wight and volume of tumor were significantly lower than those in SON group and control group. (2) The HL-60 cells in ASON group showed morphologically smaller nuclei, less mitosis, less heteromorphosis and apoptosis. CONCLUSION: The cyclin G(1) ASON can inhibit the growth of HL-60 cells in nude mice and induce apoptosis.