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Wang J.,Kunming University of Science and Technology | Wang J.,University Paul Sabatier | Wang J.,CNRS Institute of Pharmacology and Structural Biology | Zhou R.-G.,Kunming Pharmaceutical Corporation | And 2 more authors.
Research on Chemical Intermediates

Abstract The title compound (5), a key intermediate for preparing Coenzyme Q analogues, was prepared in a good yield by a reaction sequence starting from the 2, 3, 4, 5-Tetramethoxytoluene (1) via Blanc Reaction, Kornblum oxidation, and 30 % H2O2 oxidation. © 2014 Springer Science+Business Media Dordrecht. Source

Dai J.-N.,Kunming Medical University | Zong Y.,Kunming Medical University | Zhong L.-M.,Kunming Medical University | Li Y.-M.,Kunming Medical University | And 6 more authors.

Background: Microglial activation plays an important role in neurodegenerative diseases by producing several proinflammatory enzymes and proinflammatory cytokines. The phenolic glucoside gastrodin, a main constituent of a Chinese herbal medicine, has been known to display anti-inflammatory properties. The current study investigates the potential mechanisms whereby gastrodin affects the expression of potentially pro-inflammatory proteins by cultured murine microglial BV-2 cells stimulated with lipopolysaccharide (LPS). Methodology/Principal Findings: BV-2 cells were pretreated with gastrodin (30, 40, and 60 μM) for 1 h and then stimulated with LPS (1 μg/ml) for another 4 h. The effects on proinflammatory enzymes, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and proinflammatory cytokines, tumor necrosis factor-α (TNF-α), and interleukin-1β (IL-1β), are analysed by double-immunofluorescence labeling and RT-PCR assay. To reveal the mechanisms of action of gastrodin we investigated the involvement of mitogen-activated protein kinases (MAPKs) cascades and their downstream transcription factors, nuclear factor-κB (NF-κB) and cyclic AMP-responsive element (CRE)-binding protein (CREB). Gastrodin significantly reduced the LPS-induced protein and mRNA expression levels of iNOS, COX-2, TNF-α, IL-1β and NF-κB. LPS (1 μg/ml, 30 min)-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERK1/2), c-Jun N-terminal protein kinase (JNK) and p38 mitogen-activated protein kinase (p38 MAPK) and this was inhibited by pretreatment of BV-2 cells with different concentrations of gastrodin (30, 40, and 60 μM). In addition, gastrodin blocked LPS-induced phosphorylation of inhibitor κB-α (IκB-α) (and hence the activation of NF-κB) and of CREB, respectively. Conclusion and Implications: This study indicates that gastrodin significantly attenuate levels of neurotoxic proinflammatory mediators and proinflammatory cytokines by inhibition of the NF-κB signaling pathway and phosphorylation of MAPKs in LPS-stimulated microglial cells. Arising from the above, we suggest that gastrodin has a potential as an anti-inflammatory drug candidate in neurodegenerative diseases. © 2011 Dai et al. Source

Xi L.,Yunnan University | Xi L.,Kunming Pharmaceutical Corporation | Wu D.,Yunnan University | Zhu H.-Y.,Yunnan University | And 3 more authors.
Current Organic Synthesis

N-Methyl-D-aspartic acid (NMDA) has significant potential as a drug to treat diabetes, Parkinson’s and Alzheimer’s disease. Consequently, many efforts have been made for synthesis of NMDA, but there exist some flaws yet. In this paper, we report an improved method for Large-Scale Synthesis of optically pure NMDA by Eschweiler–Clarke reaction and deprotection of benzyl by ACE-Cl reagent. The synthesis has been achieved in five steps with an overall yield of 70% and an enantiomeric excess over 99.5%, in particularly, the method avoided the use of toxic methylation reagent. This method can be scaled up to kilogram quantities, providing a solid basis for its further bioactivity studies and drug development. © 2015 Bentham Science Publishers. Source

Zeng X.-S.,Kunming University of Science and Technology | Zhou X.-S.,Kunming University of Science and Technology | Luo F.-C.,Kunming University of Science and Technology | Jia J.-J.,Kunming University of Science and Technology | And 4 more authors.
Canadian Journal of Physiology and Pharmacology

Panax notoginseng, a traditional Chinese medicine, has been used for thousands of years to treat ischemic patients. More than 20 saponin components have been isolated from P. notoginseng root and identified chemically. However, these different chemical components have different roles. In this study we compared the neuroprotective mechanisms of ginsenosides Rg1, Rb1, Rg1/Rb1, and panax notoginsenoside (PNS) against injuries caused by cerebral ischemia-reperfusion (I/R). Our results show that all of these treatments significantly reduced infarction volume and alleviated neurological deficits caused by cerebral I/R. The increase in malondialdehyde (MDA) concentration was inhibited by these treatments in the hippocampus. The decreased expressions of thioredoxin-1 (Trx-1), copper-zinc superoxide dismutase (SOD-1), protein kinase B (PKB/Akt), and nuclear factorkappa B (NF-κB) caused by cerebral I/R were restored by these treatments. The expression of heat shock protein 70 (HSP70) was enhanced in the middle cerebral artery occlusion (MCAO) group, as well as in all of the treatment groups. These results suggest that Rg1 and Rb1 have similar roles in protecting the brain from ischemic damage; however, neither Rg1/Rb1 nor PNS have synergistic effects, thus either Rg1 or the Rb1 monomer should be considered as a pharmacological neuroprotective strategy for use in the case of ischemic stroke. Source

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