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Chen Y.,Beijing Laviana Pharmatech Co.
Frontiers of Chemistry in China | Year: 2011

G protein-coupled receptors (GPCRs) are involved in the control of every aspect of our behavior and physiology. GPCR can be involved in pathological processes as well and are linked to numerous diseases, including cardiovascular and mental disorders, retinal degeneration, cancer, and AIDS. This article reviews the methods of approaching photo-affinity labeling strategy to obtain the possible G protein-coupled receptors's binding site. © Higher Education Press and Springer-Verlag Berlin Heidelberg 2011. Source


Li W.,Jilin University | Li W.,Beijing Laviana Pharmatech Co. | Yin J.Y.,Jilin University | Cong Z.Y.,Jilin University | And 4 more authors.
Chemistry of Natural Compounds | Year: 2013

Six dammarane ginsenosides, 20(R)-dammar-25-ethoxy-3β,12β,20- triol (1), 3β,6α,12β-triol22,23,24,25,26,27-hexanordammaran-20- one (2), dammar-(E)-20(22)-ene-3β,12β,25-triol (3), 20(S)-dammar-3β,12β,20,25-tetrol (4), and 20(R)-protopanaxadiol (5), 20(R)-protopanaxatriol (6), were isolated from the acid hydrolysate of Panax ginseng. Compound 1 was only mentioned in a patent literature, and there is no spectroscopic data elsewhere. This paper is the first to elucidate the structure of compound 1 on the basis of spectroscopic evidence. The biological activities of compounds 1-6, crude ginsenosides, and the ginsenoside-hydrolysate were determined in human colon carcinoma cell. Compounds 1-3 and the ginsenoside-hydrolysate exhibited anti-human colon carcinoma cell activity, with IC50 of 66.1, 72.4, 50.1, and 25.7 μg/mL, respectively. © 2013 Springer Science+Business Media New York. Source


Liu J.,Jilin University | Yang Y.,Jilin University | Yin J.,Jilin University | Li W.,Jilin University | And 8 more authors.
Chemistry of Natural Compounds | Year: 2014

Bioassay-guided fractionation of the cytotoxic acid hydrolysate of the total ginsenosides of Panax ginseng C. A. Meyer (Araliaceae) afforded a new ginsenoside, (20S,22S)-dammar-22,25-epoxy-3β,12β,20-triol (1), along with five known ginsenosides, 20R,24R-dammar-20(24)-epoxy-3β,12β,25-triol (2), 20R-panaxdiol (3), dammar-(E)-20(22)-ene-3β,12β,25-triol (4), 20R-protopanaxadiol (5), and 20R-dammar-25-ethoxy- 3β,12β,20-triol (6). Their structures were elucidated on the basis of spectroscopic data. Among the compounds isolated, compound 1 showed strong cytotoxic activity against human cancer cell lines SW1116, HCT116, and A549. © 2014 Springer Science+Business Media New York. Source


Yan Z.,Tianjin Medical University | Yan Z.,Key Laboratory of Cancer Prevention and Therapy | Zhu Z.,Tianjin Medical University | Zhu Z.,Key Laboratory of Cancer Prevention and Therapy | And 6 more authors.
Molecular Cancer | Year: 2013

Background: Wnt/β-catenin signaling is a highly conserved pathway in organism evolution and is important in many biological processes. Overactivation of Wnt/β-catenin signaling is closely related to tumor development and progression. To identify potent small molecules that can fight aberrant Wnt/β-catenin-mediated cancer, we synthesized a novel pyrazoline derivative (N-(4-hydroxybenzyl)-1,3,4-triphenyl-4,5-dihydro-1H-pyrazole-5-carboxamide, BHX) to block Wnt signaling, and determined the absolute configuration of its precursor (ethyl 1,3,4-triphenyl-4,5-dihydro-1H-pyrazole-5-carboxylate). We then evaluated the inhibitory effect of BHX in vitro and in vivo.Results: Cell proliferation was assessed in three human cancer cell lines (A549, HT29, and MGC803) in the presence and absence of BHX using MTS assays. BHX effectively inhibited A549, HT29, and MGC803 cell proliferation with IC50 of 5.43 ± 1.99, 6.95 ± 0.24, and 7.62 ± 1.31 μM, respectively. BHX significantly induced apoptosis and G1 phase arrest in A549 and MGC803 cells. The β-catenin protein level was markedly reduced in A549 and MGC803 cells under BHX treatment. The inhibitory effect of BHX in vivo was investigated using a mouse xenograft model. A549 xenograft growth was suppressed by 50.96% in nude mice treated continuously with 100 mg/kg BHX for 21 d. Weight remained almost unchanged, which indicates the low toxicity of the compound.Conclusions: Our data suggest that BHX is a new drug candidate for cancer treatment because of its potent effect on the Wnt/β-catenin pathway and low toxicity. © 2013 Yan et al.; licensee BioMed Central Ltd. Source


Gu J.,Beijing Laviana Pharmatech Co. | Wang M.-X.,Beijing Laviana Pharmatech Co. | Chen W.-T.,Beijing Laviana Pharmatech Co. | Zhou Y.,Beijing Laviana Pharmatech Co. | And 5 more authors.
Xiandai Huagong/Modern Chemical Industry | Year: 2012

Corning continuous-flow microchannel reactor G1 has been applied to upgrade a conventional HATP batch process. The effects of solvent, temperature, molar ratio, and retention time are investigated. The purity and the yield of targeted products obtained from optimized process are about 98% and 100%, respectively. The compact design of G1 reactor can be installed in normal fume hood of chemical synthesis lab, and deliver about 30 t/y HATP product capability. More importantly, it is a green chemistry process and can achieve "zero effluent" objectives. Source

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