摘要
@#Abstract: Bruton’s tyrosine kinase (BTK), a cytoplasmic tyrosine kinase, plays a central role in the activation of B cells and granulocytes, operating downstream of B cell and Fcγ receptors, and is considered an attractive target for treating autoimmune diseases. Preclinical investigations have demonstrated that inhibition of BTK activity holds promise as a potential therapeutic strategy for inflammatory immune responses such as autoimmune diseases and allergies. This review provides an overview of the mechanisms by which BTK contributes to immune-related diseases and summarizes current research on the development of BTK inhibitors for treating these conditions, aiming to offer novel insights into non-oncology applications for BTK inhibitors.
摘要
@#Abstract: In the present study, the compound XL-12 from our previous work was utilized as a lead compound. Through the optimization of the terminal phenyl ring, 12 target compounds were designed and synthesized. The structures of all target compounds were confirmed by 1H NMR, 13C NMR, and H RMS. In vitro enzyme activity assay showed that most compounds demonstrated significant inhibitory activity toward Bruton’s tyrosine kinase (BTK) and Janus kinase 3 (JAK3). Among them, compound I-3 exhibited moderate cell proliferation inhibitory activity toward Daudi cells and BaF3-JAK3 cells. In the evaluation of anti-inflammatory activity in vitro, compound I-3 could effectively inhibit the production of inflammatory factors IL-6; besides, it exhibited superior anti-inflammatory activity compared to ibrutinib in xylene-induced ear swelling model in mice.
摘要
Objective To investigate effect of trepibutone tablet combined with ursodeoxycholic acid in treatment of patients with gallstone. Methods 200 cases with gallstone were diagnosed and randomly divided into observation group and control group from February 2013 to February 2014.100 cases in control group were given ursodeoxycholic acid treatment 50 mg/(kg? d),two times per day for six month.On the basis of control group observation group were treated with trepibutone one tablet per day,three times per day,4 weeks for 1 course, 2 weeks of treatment interval between 4 courses, totally for four courses.After treatment, patients were followed up and recorded gallbladder wall thickness, gallbladder functional status. Results After 6 months of treatment in patients with gallbladder wall thickness of observation group ( 2.77 ±0.38 ) mm was superior to control group (3.24 ±0.36)mm(P<0.05).After 6 months of treatment in patients with gallbladder function score of observation group (58.75 ±4.79) was better than control group (53.11 ±5.02) ( P<0.05).Recurrence rate of observation group was 9% better than that of control group 18%(χ2 =3.468,P<0.05)after treatment for 6 months.Conclusion Effect of trepibutone tablet combined with ursodeoxycholic acid in treatment of patients with gallstone is well.There is no obvious side effects during the treatment.