The apical sodium-dependent bile acid transporter(ASBT) is the main transporter to promote re-absorption of bile acids from the intestinal tract into the enterohepatic circulation.Inhibition of ASBT could increase the...The apical sodium-dependent bile acid transporter(ASBT) is the main transporter to promote re-absorption of bile acids from the intestinal tract into the enterohepatic circulation.Inhibition of ASBT could increase the excretion of bile acids,thus increasing bile acid synthesis and consequently cholesterol consumption.Therefore,ASBT is an attractive target for developing new cholesterol-lowering drugs.In this report,a series of 1-(2,4-bifluorophenyl)-7-dialkylamino-1,8-naphthyridine-3-carboxamides were designed as inhibitors of ASBT.Most of them demonstrated potency against ASBT transport of bile acids.In particular,compound 4a_1 was found to have the best activity,resulting in 80.1%inhibition of ASBT at10μmol/L.展开更多
Objective: To study the enhancement of the immune functions and autologous tumor killing (ATK) activity by kappa selenocarrageenan (KSC) in mice bearing sarcoma 180. Methods: To measure the effects of KSC and/or Cy...Objective: To study the enhancement of the immune functions and autologous tumor killing (ATK) activity by kappa selenocarrageenan (KSC) in mice bearing sarcoma 180. Methods: To measure the effects of KSC and/or Cyclophosphamide (Cy) on natural killer (NK) activity, lymphokine activated killer (LAK) activity, the produc tion of interleukin 2 (IL 2), ATK activity and the growth of sarcoma 180 (S 180 ). Results: KSC promoted NK activity, LAK activity and ATK activity in vivo , increased IL 2 production at 40 mg/kg/d×9d. It also enhanced the antitumor action of Cy (20 mg/kg/d×9d) and offset the inhibition of Cy on immunocopetent cells. The ATK activity in splenocytes of S 180 bearing mice could be induced and increased by recombinant interleukin 2 (rIL 2) in vitro . Conclusion: KSC has an up regulating effect on the immune functions and ATK activity in tumor bearing mice. It can be used as a biological response modifier (BRM) in cancer biotherapy.展开更多
3,5,6,8-Tetrahydro-4H-thiopyrano[4＇,3＇：4,5]thieno[2,3-d]pyrimidin-4-ones（7） were synthesized via the base catalytic reactions of amines or phenols with carbodiimides（5）, which were obtained from the aza-Wittig ...3,5,6,8-Tetrahydro-4H-thiopyrano[4＇,3＇：4,5]thieno[2,3-d]pyrimidin-4-ones（7） were synthesized via the base catalytic reactions of amines or phenols with carbodiimides（5）, which were obtained from the aza-Wittig reac tions of iminophosphoranes（4） with aromatic isocyanates.展开更多
基金supported by the National Natural Science Foundation of China(Nos.81473098 and 81473099)Hebei Provincial Key Research Project of Medical Science(Nos.ZD20140027 and 20150588)
文摘The apical sodium-dependent bile acid transporter(ASBT) is the main transporter to promote re-absorption of bile acids from the intestinal tract into the enterohepatic circulation.Inhibition of ASBT could increase the excretion of bile acids,thus increasing bile acid synthesis and consequently cholesterol consumption.Therefore,ASBT is an attractive target for developing new cholesterol-lowering drugs.In this report,a series of 1-(2,4-bifluorophenyl)-7-dialkylamino-1,8-naphthyridine-3-carboxamides were designed as inhibitors of ASBT.Most of them demonstrated potency against ASBT transport of bile acids.In particular,compound 4a_1 was found to have the best activity,resulting in 80.1%inhibition of ASBT at10μmol/L.
文摘Objective: To study the enhancement of the immune functions and autologous tumor killing (ATK) activity by kappa selenocarrageenan (KSC) in mice bearing sarcoma 180. Methods: To measure the effects of KSC and/or Cyclophosphamide (Cy) on natural killer (NK) activity, lymphokine activated killer (LAK) activity, the produc tion of interleukin 2 (IL 2), ATK activity and the growth of sarcoma 180 (S 180 ). Results: KSC promoted NK activity, LAK activity and ATK activity in vivo , increased IL 2 production at 40 mg/kg/d×9d. It also enhanced the antitumor action of Cy (20 mg/kg/d×9d) and offset the inhibition of Cy on immunocopetent cells. The ATK activity in splenocytes of S 180 bearing mice could be induced and increased by recombinant interleukin 2 (rIL 2) in vitro . Conclusion: KSC has an up regulating effect on the immune functions and ATK activity in tumor bearing mice. It can be used as a biological response modifier (BRM) in cancer biotherapy.
基金Supported by the National Natural Science Foundation of China(No.20772041)the Key Project of Chinese Ministry of Education(No.107082)
文摘3,5,6,8-Tetrahydro-4H-thiopyrano[4＇,3＇：4,5]thieno[2,3-d]pyrimidin-4-ones（7） were synthesized via the base catalytic reactions of amines or phenols with carbodiimides（5）, which were obtained from the aza-Wittig reac tions of iminophosphoranes（4） with aromatic isocyanates.
