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To analyze various compositions of urinary stones using revolution spectral CT (rapid kV switching dual-energy CT) in vivo. 202 patients with urinary stones underwent spectral CT before surgery. Zeff peak, overall scope and CT values were detected. Moreover, water/iodine attenuating material images were obtained. Removed stones were subjected to infrared spectroscopy after surgery. The results of infrared spectroscopy were compared with CT. 28 stones (14.08%) with single composition, 165 stones with two mixed compositions (81.68%), and 9 stones with three mixed compositions (4.46%) were observed. When Zeff peaks of stones with single/mixed compositions were summarized together, 146 peaks of calcium oxalate monohydrate, 119 peaks of calcium oxalate dihydrate, 55 peaks of carbapatite, 38 peaks of urate, 16 peaks of struvite, and 11 peaks of brushite were totally observed. 93.8% of calcium oxalate monohydrate had Zeff peaks between 13.3 and 14.0. 91.6% of calcium oxalate dihydrate had peaks between 12.0 and 13.3. For carbapatite, 90.9% of stones had peaks from 14.0 to 15.0. A total of 94.8% of urate had peaks between 7.0 and 11.0. 93.8% of struvite had peaks between 11.0 and 13.0, and 90.9% of brushite had peaks between 12.0 and 14.0. Moreover, densities of urate, struvite and brushite were low density in iodine-based images and high-density in water-based images. The in-vivo analysis of spectral CT in urinary stone revealed characteristics of different compositions, especially mixed compositions. An in-vivo predictive model may be constructed to distinguish stone compositions.

A series of 1-cyano-2-amino-benzimidazole derivatives were synthesized and evaluated for their cytotoxic activities in vitro against three human cancer cell lines (human lung carcinoma cell line: A549, human leukemia cell line: K562, and human prostate cancer cell line: PC-3). Most of these compounds showed potent activities against these tumor cell lines, especially against A549 and K562 cell lines. The preliminary structure–activity relationships of 1-cyano-2-amino-benzimidazole derivatives were also discussed. The cell cycle analysis was carried out in K562 cells and the results showed that compound 4d caused a marked increase of cells in G 2/M phase.

An efficient copper-catalyzed, microwave-assisted, one-pot reaction has been developed for synthesis of 3,4-diaryl isoquinolines. The reaction was performed in two steps via a CuI/2,2′-biimidazole-catalyzed tandem process from N-tert-butyl-o-iodobenzaldimine and a terminal aryl alkyne, followed by addition of an aryl iodide. A variety of 3,4-diaryl isoquinolines have been obtained in moderate to good yields.

Semi-synthesis of paclitaxel was achieved in four steps from 10-deacetylbaccatin III (10-DAB III). The key steps are the regioselective protection at the hydroxyl group at C-7 of 10-DAB III, using 1,1′-thiocarbonyldiimidazole as a selective reagent, and the deprotection of the protected paclitaxel with a mixture of p -toluenesulfonic acid and 0.1 mol/L aqueous hydrochloride.

As a step toward understanding the structure and function of phospholipase A2(PLA2), we isolated several novel cDNAs encoding Agkistrodon halys Pallas PLA2 isoenzymes including B-PLA2, Asn49-PLA2, A-PLA2, A′-PLA2 and BA1-PLA2 by polymerase chain reaction with oligonucleotide primers corresponding to the N- and C-terminus of these enzymes. The amino acid sequences of A-PLA2 deduced from cDNA are consistent with that isolated from venom except for four residues. Asn49–PLA2 and B-PLA2 are highly similar (>95%), but the critical residue Asp49 in the active centre of B-PLA2 is replaced by Asn49 in Asn49–PLA2. The N-terminal residues (1–24) of BA1-PLA2 shows high similarity to that of B-PLA2 which has strong ability to hemolyze erythrocytes, while its C-terminal residues (72–125) are the same as that of A-PLA2 which can inhibit platelet aggregation. The successful cloning of these isoenzymes not only provide excellent native material to study the structure-function relationship of PLA2s, but also to disclose the genesis of structural diversity of PLA2s, namely DNA modification and gene rearrangement. The cloned cDNA for A-PLA2 has been expressed in E. coli. By Q-Sepharose column chromatography, denaturation–renaturation and FPLC, we obtained the active recombinant protein with the initiator Met. This is the first report of the production of an active recombinant PLA2 with the initiator Met.

To investigate the transcription of cytoskeleton protein genes in differentiation of neurons from mouse embryonic stem (ES) cells induced by all-trans retinoic acid (RA), and to explore the possibility of setting up a method to screen small molecules with promoting or inhibiting effect.The hanging drop method was employed for embryonic body formation to mimic embryo development in vivo. Reverse transcriptase PCR (RT-PCR) was performed to investigate mRNA expression of the neuron-specific cytoskeleton proteins including Mtap2, Nefm and beta-tubulin III which were regarded as the inducing effect indexes of RA. Morphological evaluation and immunocytochemistry staining were conducted to identify the neural derivatives. Moreover, the inducing effects of six synthetic molecules were further evaluated.RA up-regulated the mRNA expression of Mtap2 and Nefm, especially Mtap2 increased by 1.27 times, which was consistent with the morphological alteration. However, there was no significant changes of beta-tubulin III expression. With addition of the six synthetic molecules, the transcription of Mtap2 was inhibited, while the Nefm mRNA expression was up-regulated in some degree, especially for molecule 1 and 3 that was increased by 1.4 and 1.2 times, which, however, was not parallel to the morphological changes.The transcriptional levels of Mtap2 and Nefm are both up-regulated in the RA-induced differentiation of ES cells towards neurons. The up-regulation of Mtap2 is consistent with the morphological alteration, which might be the key landmark in the RA-induced differentiation of ES cells into neurons.

First strand cDNA synthesis was primed with synthetic oligonucleotide from total RNA extracted from the gland of the snake Agkistrodon halys Pallas. The pro-BPLA(2) gene was then amplified by PCR and cloned into the pBS-ks vector. Its nucleotide sequence has been determined by analyzing the DNA sequence of three colonies containing the pro-BPLA(2) gene. The deduced amino acid sequence consists of 138 amino acids and agrees with the partly known amino acid sequence except for seven amino acid residues. The successful cloning of the BPLA(2) gene not only has made the determination of its total amino acid sequence possible, but also provided a good basis for further research work in the protein engineering of functional peptides from snakes.