To Speed up the Development and Industrialization of Natural Drugs in China

1.The Current Situation Facing China's accession to the WTO,our pharmaceutical industries must prepare to meet extremely strong competition,because 97% of the synthetic medicines and antibiotics marketed in the country are copies of foreign products.

Antiviral Drugs(Synthetic Small Molecule Inhibitors and Nature Drugs)Against EV71 in Enteroviruses:Advances and Perspectives

Background:Enterovirus 71(EV71)is a major virus that causes hand-foot-mouth disease.In cases of infants and young children,EV71 infection has been associated with severe neurological disease and potentially fatal systemic complications.The sporadic outbreak worldwide is increasingly prevalent in the Asia-Pacific region,where it has become a major public health concern.Objective:No specific antiviral drugs are currently approved for the treatment of EV71 infection.The purpose of this study is to comprehensively review the research progress of anti-EV71 drugs(synthetic small molecule inhibitors and nature drugs)in the past twenty years,and further to promote the research and development of antiviral drugs against enterovirus infection.Methods:This study reviewed the drugs on anti EV71 in the past decades.The literature search in PubMed database was conducted for original studies and review articles on drugs against enterovirus 71.Related articles published in English were selected for study and discussion.Results:As reviewed in this paper,bioactive molecules include receptor analogues,protease inhibitors,natural drugs derived from traditional chinese medicine or natural medicine.These bioactive molecules have shown significant effectiveness in inhibiting the entry and replication of EV71 in vitro and in vivo experiments.Conclusion:This review demonstrated that the entry receptor of EV71 into host cells has been studied,and receptor drugs against enterovirus have been made some progress,but most receptor analogues have not been reported.Further research is needed in this area in the future.On the other hand,the protease inhibitors have always been a major aspect of anti-enterovirus research and can be developed as antiviral agents for clinical application.In terms of natural drugs,many monomers derived from traditional chinese medicine or natural medicine have good antiviral activity and little toxic and side effects on host cells,but in view of their multi-target properties,the mechanism of drug action needs to be further studied.

Dual ligands relay-promoted transformation of unstrained ketones to polyfluoroarenes and nitriles

C-C bond activation has emerged as a powerful tool for the construction of complex molecules.Herein,we report a dual ligands relay-promoted transformation of unstrained aryl,alkenyl and alkynyl ketones to the corresponding polyfluoroarenes and nitriles via C-C(=O)bond cleavage and subsequent decarboxylative arylation process.Various polyfluoroarene and nitrile products are obtained in one pot under cyanide-free conditions.The protocol features high atom economy,broad functional group tolerance and excellent heterocyclic compatibility.The late-stage functionalization of the drug and natural product demonstrated the synthetic utility of our protocol.Furthermore,the decisive role of the dual ligands was clarified and the mechanistic rationale including theβ-C elimination as the rate-limiting step was supported by detailed density functional theory(DFT)studies.

Study on the Complex Prescription Compatibility Law of the Cold and Hot Nature of Mahuang Decoction(麻黄汤) and Its Categorized Formulae Based on the Cold-Hot Pad Differentiating Assay

Objective：To explore the complex prescription compatibility law of the cold and hot nature of Mahuang Decoction（麻黄汤,MHD） and Maxing Shigan Decoction（麻杏石甘汤,MXSGD）,both categorized formulas but with different hot/cold natures.Methods：Oxygen consumption of mice was determined among three groups：MHD,MXSGD and the control;a cold-hot pad differentiating assay was used to observe the variability of temperature tropism among the groups of mice which was treated with MHD,MXSGD,and their compositions. Meanwhile,the total anti-oxidant capability（T-AOC） activity were detected.Results：After administration of MHD, the mice showed increased oxygen consumption（P0.01）.Compared with MHD group,the remaining rate of MXSGD mice on the hot pad was found to be significantly increased with the cold-hot pad differentiating assay （P0.05）.There was no significant difference（P0.05） among the remaining rates of MXSGD,MXSGD with high dose Gypsum Fibrosum（MXHGF） group,and MXSGD with low dose Gypsum Fibrosum（MXLGF） group mice.Compared with the MHD group,T-AOC activity of the mice in the Consensus Compositons group was significantly decreased（P=0.0494）.Compared with the MXSGD group,T-AOC activity of Gypsum Fibrosum （GF） group was increased significantly（P=0.0013）.Conclusions：The differences in cold and hot nature could be represented objectively between MHD with a hot nature and MXSGD with a cold nature.The reason may be the Gypsum Fibrosum which decreased the efficacy of the consensus compositions.However,increasing or decreasing the dose of Gypsum Fibrosum will not change the cold and hot nature of MXSGD.