Vsg-22, a new anti-inflammatory drug based on structure, was discovered by Shanghai Pharmaceutical Research Institute

The structure based anti-inflammatory candidate drug vsg-22 glucocorticoid receptor (GR) is a hot target for the development of anti-inflammatory drugs Up to now, glucocorticoids developed with the target have been widely used in the market as the most effective anti-inflammatory drugs Because of the prevalence of inflammation, this kind of anti-inflammatory drugs occupy a large proportion in the drug market For example, the global sales of asthma drugs exceed 20 billion US dollars, ranking the second in the sales of commonly used drugs However, a large number of clinical experiments show that glucocorticoids have very large side effects Even if they are used in a regulated standard dose for a long time, they will still lead to obesity, diabetes, osteoporosis, skin atrophy and other side effects The most typical example is dexamethasone (DEX) DEX can effectively inhibit SARS inflammation induced by SARS coronavirus, but it has caused many sequelae of necrosis of femoral head These side effects greatly limit the use of glucocorticoids Therefore, the development of a new anti-inflammatory drug with high efficiency, novel mechanism and low toxicity has become one of the key issues in the field of medicine and pharmacy Based on this, Xu Huaqiang research group, Jiang Hualiang research group and Van Andel Research Institute of Shanghai Pharmaceutical Research Institute of Chinese Academy of Sciences further designed and synthesized a series of new hydrocortisone derivatives with obvious targeting characteristics In vitro evaluation showed that compound vsg-22 has potential anti-inflammatory ability (its activity is higher than two orders of magnitude of anti-inflammatory drug DEX on the market today) At the same time, it was found that its esterase metabolite vsg-24 lost its anti-inflammatory activity These results show that vsg-22 has the potential to be a new effective and safe antiasthmatic drug, which is worthy of further development The above research has applied for U.S patent The research results were published online in the form of full text in the latest issue of cell research journal (2014, DOI: 10.1038 / cr.2014.52.) on April 25 Among them, researcher Xu Huaqiang from Shanghai Pharmaceutical Institute, Dr Yi Wei and Dr Yuanzheng he from Van Andel Institute in the United States are co authors of the paper As soon as the paper was published, it was highly praised by experts in this field, and also tracked and reported by many professional websites The above research work was supported by the "thousand talents plan" of the Chinese Organization Department, the Chinese Academy of Sciences, the National Natural Science Foundation of China, the China Postdoctoral Science Foundation, the Van Andel Institute of the United States and Amway China