1.Clinical obstration on promoting the first stage of the multigravidae by using of 654-2
Chinese Journal of Primary Medicine and Pharmacy 2006;0(06):-
Objective To explore the clinical effect by using of 654-2 to multigravidae.Methods Among 60 multigravidaes deliverying,30 were treated with 654-2 and oxytocin,the other 30 multigravidaes were treated with oxytocin only for control.The time of dilatation of the cervix,the rate of fetal distress and neonatal asphyxia,the rate of operative delivery and postpartum hemorrhage were observed.Results The time of dilatation of the cervix and the rate of operative delivery were shorter than the control.It was significantly different between the two groups(P0.05).Conclusion 654-2 can promote the first stage of the multigravidae.It can reduce the rate of operative delivery.It is safety by using of 654-2 to short the first stage to multigravidae.
2.Effect of Serum Containing Rhizoma Chuanxiong on Proliferation and Differentiation of Mouse Embryonic Stem Cells
Deju JIANG ; Yi LUO ; Qian BAO ; Quan XIA
Journal of Guangzhou University of Traditional Chinese Medicine 2017;34(3):401-404
Objective To observe the influence of serum containing Rhizoma Chuanxiong on the proliferation and differentiation of mouse embryos stem cells(ESCs).Methods Mouse ESCs were co-cultured with serum containing Rhizoma Chuanxiong.The proliferation of ESCs was detected by CCK-8 method.The expression level of specific gene beta-myosin heavy chain (β-MHC) in cardiac myoblasts was detected by reverse transcription-polymerase chain reaction (RT-PCR).Results Compared with the blank rat serum group and the blank fetal bovine serum group,the differences of activities of ESCs in serum containing Rhizoma Chuanxiong group were in significant(P >0.05) and the expression level of specific gene β-MHC in cardiac myoblasts was increased (P < 0.05).Conclusion Serum containing Rhizoma Chuanxiong can promote the differentiation of ESCs into cardiac myoblasts.
3.Structural optimization and biological evaluation of 1,5-disubstituted pyrazole-3-carboxamines as potent inhibitors of human 5-lipoxygenase.
Yu ZHOU ; Jun LIU ; Mingyue ZHENG ; Shuli ZHENG ; Chunyi JIANG ; Xiaomei ZHOU ; Dong ZHANG ; Jihui ZHAO ; Deju YE ; Mingfang ZHENG ; Hualiang JIANG ; Dongxiang LIU ; Jian CHENG ; Hong LIU
Acta Pharmaceutica Sinica B 2016;6(1):32-45
Human 5-lipoxygenase (5-LOX) is a well-validated drug target and its inhibitors are potential drugs for treating leukotriene-related disorders. Our previous work on structural optimization of the hit compound 2 from our in-house collection identified two lead compounds, 3a and 3b, exhibiting a potent inhibitory profile against 5-LOX with IC50 values less than 1 µmol/L in cell-based assays. Here, we further optimized these compounds to prepare a class of novel pyrazole derivatives by opening the fused-ring system. Several new compounds exhibited more potent inhibitory activity than the lead compounds against 5-LOX. In particular, compound 4e not only suppressed lipopolysaccharide-induced inflammation in brain inflammatory cells and protected neurons from oxidative toxicity, but also significantly decreased infarct damage in a mouse model of cerebral ischemia. Molecular docking analysis further confirmed the consistency of our theoretical results and experimental data. In conclusion, the excellent in vitro and in vivo inhibitory activities of these compounds against 5-LOX suggested that these novel chemical structures have a promising therapeutic potential to treat leukotriene-related disorders.