Chen, Liu Zeng; Zhang, Xing Xing; Liu, Ming Ming; Wu, Jing; Ma, Duo; Diao, Liang Zhuo; Li, Qingshan; Huang, Yan Shuang; Zhang, Rui; Ruan, Ban Feng; Liu, Xin Hua published the artcile< Discovery of Novel Pterostilbene-Based Derivatives as Potent and Orally Active NLRP3 Inflammasome Inhibitors with Inflammatory Activity for Colitis>, Quality Control of 3959-07-7, the main research area is pterostilbene NLRP3 inflammasome inhibitor colitis.
Studies have shown that the abnormal activation of the NLRP3 inflammasome is involved in a variety of inflammatory-based diseases. In this study, a high content screening model targeting the activation of inflammasome was first established and pterostilbene was discovered as the active scaffold. Based on this finding, total of 50 pterostilbene derivatives were then designed and synthesized. Among them, compound 47 was found to be the best one for inhibiting cell pyroptosis [inhibitory rate (IR) = 73.09% at 10μM], showing low toxicity and high efficiency [against interleukin-1β (IL-1β): half-maximal inhibitory concentration (IC50) = 0.56μM]. Further studies showed that compound 47 affected the assembly of the NLRP3 inflammasomes by targeting NLRP3. The in vivo biol. activity showed that this compound significantly alleviated dextran sodium sulfate (DSS)-induced colitis in mice. In general, our study provided a novel lead compound directly targeting the NLRP3 protein, which is worthy of further research and structural optimization.
Journal of Medicinal Chemistry published new progress about Apoptosis-regulating proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (ASC, expression not affected by inhibitor, and inhibition of ASC oligomerization). 3959-07-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H8BrN, Quality Control of 3959-07-7.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary