生物活性

• 描述Sulfasalazine is a potent and specific inhibitor of NF-kappaB activation. Treatment of SW620 colon cells with sulfasalazine inhibited TNFalpha-, LPS-, or phorbol ester- induced NF-kappaB activation. NF-kappaB-dependent transcription was inhibited by sulfasalazine at micro- to millimolar concentrations. TNFalpha-induced nuclear translocation of NF-kappaB was prevented by sulfasalazine through inhibition of IkappaBalpha degradation^[3]. Sulfasalazine is a direct inhibitor of IKK-alpha and -beta by antagonizing adenosine triphosphate binding. The suppression of NF-kappaB activation by inhibition of the IKKs contributes to the well-known anti-inflammatory and immunosuppressive effects of sulfasalazine^[4]. Sulfasalazine can inhibit NF-κB and reduce lipopolysaccharide-induced cytokine concentrations in fetal membrane explants and reduce the rate of Escherichia coli-induced preterm labour in mice^[5]. Sulfasalazine induces cell death via apoptosis in HBx-expressing liver cells, as evidenced by characteristic changes in nuclear morphology, cleavage of poly (ADP-ribose) polymerase (PARP), caspase-3 and caspase-9, and activation of caspase-3^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02930343	Rheumatoid Arthritis	Phase 4	Recruiting	August 2018	India ... more >> Department of Clinical Immunology , Jawaharlal Institute of Post graduate Medical Educationa and Research Recruiting Pondicherry, India, 605006 Contact: Dr. Vir Singh Negi, DM    0413-2297358    vsnegi22@yahoo.co.in    Contact: Dr. Pooja Belani, MD    8940482248    drpoojabelani@gmail.com Collapse <<
  NCT02590562	-	-	Completed	-	China ... more >> Peking University First Hospital Beijing, China, 100034 Beijing Jishutan Hospital; Rheumatology & Immunology Beijing, China, 100035 Peking University People's Hospital Beijing, China, 100044 Peking University Third Hospital Beijing, China, 100083 China-Janpan Friendship Hospital of Jilin University Changchun, China, 130031 West China Hospital, Sichuan University Chengdu, China, 610041 Sichuan Provincial People's Hospital Chengdu, China, 610072 The First Affiliated Hospital, Sun Yat-sen University Guangzhou, China, 510080 The First Affiliated Hospital of Guangzhou University of Chinese Medicine Guangzhou, China, 510405 Nanfang Hospital, Southern Medical University Guangzhou, China, 510515 Guanghua Hospital of Integrated Traditional Chinese and Western Medicine ( Guanghua Hospital) Shanghai, China, 200052 The Second Hospital of Shanxi Medical University Taiyuan, China, 030001 Tianjin Medical University General Hospital Tianjin (天津), China, 300052 First Affiliated Hospital of Medical College of Xi'an Jiaotong University Xi'an, China, 710061 Xinjiang Uygur Autonomous Region People Hospital Ürümqi, China, 830001 Collapse <<
  NCT02590562	-	-	Completed	-	-

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• 参考文献

• [1] Liptay S, Bachem M, et al. Inhibition of nuclear factor kappa B and induction of apoptosis in T-lymphocytes by sulfasalazine. Br J Pharmacol. 1999 Dec;128(7):1361-9.

  [2] Gadangi P, Longaker M, et al. The anti-inflammatory mechanism of sulfasalazine is related to adenosine release at inflamed sites. J Immunol. 1996 Mar 1;156(5):1937-41.

  [3] Wahl C, Liptay S, Adler G, Schmid RM. Sulfasalazine: a potent and specific inhibitor of nuclear factor kappa B. J Clin Invest. 1998 Mar 1;101(5):1163-74

  [4] Weber CK, Liptay S, Wirth T, Adler G, Schmid RM. Suppression of NF-kappaB activity by sulfasalazine is mediated by direct inhibition of IkappaB kinases alpha and beta. Gastroenterology. 2000 Nov;119(5):1209-18

  [5] Sykes L, Thomson KR, Boyce EJ, Lee YS, Rasheed ZB, MacIntyre DA, Teoh TG, Bennett PR. Sulfasalazine augments a pro-inflammatory response in interleukin-1β-stimulated amniocytes and myocytes. Immunology. 2015 Dec;146(4):630-44

  [6] Lee YM, Kang M, Hwang JM, Lee S, Cho H, Kim YS. Sulfasalazine induces apoptosis of HBx-expressing cells in an NF-kappaB-independent manner. Virus Genes. 2010 Feb;40(1):37-43

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