2.Development of pharmacology promotes new drug research and development
Chinese Journal of Pharmacology and Toxicology 2016;30(12):1243-1249
Pharmacology is a bridge discipline between medicine and pharmacy,betmeen basic medicine and clinical medicine,between life sciences and chemistry as well as material science. Phar?macology is closely related to many subjects,and is an indispensable subject in medical sciences. It plays an important role in the development of medical sciences. The main tasks of pharmacology development involve rational drug use,new drug research and development,and promotion of medical sciences and life sciences. During the whole process of new drug development,the development of pharmacolo?gy has played a positive role. As such,new drug research and development depends on the develop?ment of pharmacology. Pharmacology plays an important role in the development of new drugs and is involved in the whole process of research and development. Thus,it is a support subject for new drug development. Strengthening pharmacological research and improving the overall level of pharmacologi?cal in China are of great significance for promoting new drug research and development and ensuring ra?tional drug use.
3.Network pharmacology: new guidelines for drug discovery.
Acta Pharmaceutica Sinica 2010;45(12):1472-7
The development of new drug is not only the main driving force for the development of pharmaceutical industry, but also plays a very important role in the social development. However, with the increasing demands, new drug development is facing great difficulties in recent years. The hypothesis of highly selective single-target is meeting the challenges because of its limitations. Network pharmacology has been one of the new strategies for new drug discovery based on single-target drug research in recent years. This paper focused on the basis of network pharmacology and its research progress, discussed its development direction and application prospects, and analyzed its limitations and problems as well. The application of network pharmacology in new drug development is discussed by comparing its guidelines with those of traditional Chinese medicine theory and Effective Components Group hypothesis of Chinese medicines.
4.Water soluble active ingredients of Danshen--review on the Salvianolic acids
Basic & Clinical Medicine 2000;20(5):394-398
Danshen-Radix Salviae Miltiorrhizae,is one of the common traditional Chinese medicines,which has been used clinically in the treatment of cardiovascular diseases more than 20 centuries.The active ingredients of Danshen has been researched 5 decades by the modern methods.Many researchers investigated the pharmacological effects of water soluble ingredients of Danshen-salvianolic acids in vivo and in vitro.The results demonstrated that salvianolic acids have different pharmacological effects such as potent antioxidative effects,scavenging free radicals,protect neural cells against injuries caused by anoxia, etc.In present paper,the pharmacological effects of salvianolic acids and the mechanisms of their actions are reviewed based on the research results obtained in our laboratory and other authors.
5.Progress in the study of Apelin-APJ system
Chinese Pharmacological Bulletin 2003;0(08):-
The family of apelin peptides is derived from a single gene and activates the 7-transmembrane G-protein-coupled receptor,namely APJ.Apelins have been shown to be involved in the regulation of cardiovascular functions,fluid homeostasis,central nervous system functions,insulin sensitivity,food and water intake.The properties of this system may make it a novel drug target of therapeutic applications in the cardiovascular diseases such as hypertension and heart failure,and related diseases like obesity.
6.Screening of small molecules inducing PC12 cell differentiation
Chinese Pharmacological Bulletin 1987;0(02):-
Aim To search for small molecule NGF mimetic s using a primary screening model.Methods Both rapid quantitati ve bioassay for NGF(-like) activity by measurement of neurite extension in NGF -induced PC12 cells and a following MTT technique to monitor cells alive were u sed.Results More than 1 600 compounds were tested using the se methods and several effective samples with lower cytotoxicity were found. One of them, the compound B,was in good dose-and time-effect relationship. Conclusion All above studies provide a useful model and chemical info rmation for further screen of neurotrophic mimetics and neural cell tumor induce rs.
7.Protein kinases and neurodegenerative diseases
Chinese Journal of Pharmacology and Toxicology 2014;(5):748-757
Neurodegenerative diseases are complex nervous system disorders as a result of myelin damage,synapses loss and/ or neuron loss. The pathogenesis of these diseases is still not completely clear. Protein kinases play an important role in both normal nerve cells and neurodegenerative disorders. lnhibitors of protein kinases can effectively regulate the physiological function of nerve cells and prevent the development and progression of the disease. This article reviews protein kinases and their inhibitors involved in Alzheimer disease,Parkinson disease,Huntington disease and other neurodegenerative diseases.
8.Thioredoxin-interacting protein: a new potential target for diabetes and related vascular complications therapy.
Acta Pharmaceutica Sinica 2015;50(12):1559-64
Thioredoxin-interacting protein (TXNIP), also known as vitamin D3-up-regulated protein (VDUP1), is an endogenous inhibitor of thioredoxin (Trx), which regulates the cellular reduction-oxidation (redox) state. TXNIP regulates cellular survival, apoptosis and inflammation induced by glucotoxicity, heat shock and mechanical pressure. The above functions of TXNIP are regulated by carbohydrate response element binding protein (ChREBP) and AMP-dependent protein kinase (AMPK). In recent years, numerous studies showed that TXNIP is involved in diabetes and diabetic complications. On the one hand, TXNIP functions in diabetes by increasing insulin resistance and hepatic gluconeogenesis. TXNIP expression is induced by high glucose, which is implicated in pancreatic beta cell glucotoxicity and endothelial cells dysfunction. TXNIP may contribute to the development and progression of diabetes and its vascular complications. TXNIP may be a new target for diabetes and its vascular complications therapy.
9.Progress in the study of phosphodiesterase-7 as a new target for anti-inflammatory and immune drug
Chinese Pharmacological Bulletin 1987;0(01):-
Phosphodiesterases(PDEs) is the only protein enzyme family,which catalyze the hydrolysis of cyclic nucleotide second messages(cAMP and cGMP).PDEs regulate many physiologic and pathologic processes.Recent advance showed that PDE7 hydrolyze cAMP exclusively and is divided into PDE7A and PDE7B. PDE7 mainly express in immune and inflammatory cells.The selective inhibition of this family generates profound,functional effects and PDE7 has been used as a therapeutic target for diseases related with inflammation,such as chronic obstructive pulmonary disease(COPD),rheumatoid arthritis and Alzheimers disease(AD).
10.Pain of high-throughput screening--pan assay interference compounds.
Acta Pharmaceutica Sinica 2015;50(8):925-30
High-throughput screening is a regular approach available for identitying new lead compounds for the growing validated drug targets in drug screening. However, it has also introduced a large number of peculiar molecules which interfere drug screening. Pan assay interference compounds (PAINS) interfere with the progress of drug screening in various ways, such as interfering with a biochemical assay, modifying the protein, aggregate-based inhibitors and so on. So it is of vital significance to remove them. This paper has consulted the concept, category of PAINS and reviewed the way of PAINS interfering and the countermeasures to cope with them to direct the approach of high through screening and improve the hits percent.