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您的检索式：作者名="Ruolin Shi"
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| 1 | Structure-guided discovery of potent and oral soluble epoxide hydrolase inhibitors for the treatment of neuropathic pain显示文摘Soluble epoxide hydrolase(sEH) is related to arachidonic acid cascade and is over-expressed in a variety of diseases, making sEH an attractive target for the treatment of pain as well as inflammatory-related diseases. A new series of memantyl urea derivatives as potent sEH inhibitors was obtained using our previous reported compound 4 as lead compound. A preferential modification of piperidinyl to 3-carbamoyl piperidinyl was identified for this series via structure-based rational drug design. Compound A20 exhibited moderate percentage plasma protein binding(88.6%) and better metabolic stability in vitro. After oral administration, the bioavailability of A20 was 28.6%. Acute toxicity test showed that A20 was well tolerated and there was no adverse event encountered at dose of 6.0 g/kg. Inhibitor A20 also displayed robust analgesic effect in vivo and dose-dependently attenuated neuropathic pain in rat model induced by spared nerve injury, which was better than gabapentin and sEH inhibitor(±)-EC-5026. In one word, the oral administration of A20 significantly alleviated pain and improved the health status of the rats, demonstrating that A20 was a promising candidate to be further evaluated for the treatment of neuropathic pain. | Fangyu Du Ruolin Cao Lu Chen Jianwen Sun Yajie Shi Yang Fu Bruce D.Hammock Zhonghui Zheng Zhongbo Liu Guoliang Chen | 2022 | Acta Pharmaceutica Sinica B2022，12，3： | 0 |
| 2 | Biomimetic extracellular vesicles for the tumor targeted treatment显示文摘Extracellular vesicles(EVs)are nanoscale substances produced by most cells,which were not fully understood in the early years.However,with the development of advanced techniques,researchers have discovered that EVs play an essential role in information exchange and signal transduction between cells.Nowadays,EVs are being used,modified,and developed as a natural drug carrier in various medical fields because of their high biocompatibility and natural affinity with the source body.Many studies have shown that multiple sources of EVs have been modified and utilized in cancer therapy to improve patients’treatment windows and effectively prolong patient survival.In this paper,we review the advances in the treatment of cancer based on EVs.We summarize the types of EVs loading therapy,the modes of drug loading and the latest therapeutic applications of multiple modes combined with EVs in cancer treatment.We conclude with a discussion of the current status,challenges,and prospects of EVs as a tool for tumor therapy. | Ruolin Shi An Zhan Xinze Li Bin Kong Gaofeng Liang | 2023 | Engineered Regeneration2023，4，4： | 0 |
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