生物活性

• 描述Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory and antiproliferative effects. Triptolide induces apoptosis in cultured and primary Chronic Lymphocytic Leukemia (CLL) B-cells. Treatment of CD19+ B cells with Triptolide, induces a dose-dependent increase in apoptosis in cultured and primary CLL cells. Consistent with the inhibition of heat-shock induced HSP transcription, treatment with Triptolide attenuates heat-shock induced expression of HSPs^[3]. Triptolide induced apoptosis in a subgroup of acute lymphoblastic leukemia (ALL) cells overexpressing the MDM2 oncoprotein by inhibiting MDM2 expression^[4]. Triptolide could protect differentiated PC12 cells against Aβ25-35-induced cytotoxicity and attenuate Aβ25-35-induced differentiated PC12 cell apoptosis. Triptolide could also suppress the level of autophagy^[5].
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  A549 cells	-	Cytotoxic assay	-	Cytotoxicity against human A549 cells, IC50=0.019 μM	21470864
  human 786-O cells	-	Cytotoxic assay	72 h	Cytotoxicity against human 786-O cells after 72 hrs by MTT assay, IC50=0.022 μM	19637874
  human A549 cells	-	Function assay	-	Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay, IC50=0.014 μM	23895492

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• 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
  NCT03117920	Pancreatic Cancer	Phase 2	Recruiting	February 15, 2019	United States, Arizona ... more >> HonorHealth Research Institute Recruiting Scottsdale, Arizona, United States, 85258 Contact: Joyce Schaffer    480-323-1339    clinicaltrials@honorhealth.com    Principal Investigator: Erkut Borazanci          United States, California Moores UC San Diego Cancer Center Recruiting La Jolla, California, United States, 92037 Contact: Michelle Mendoza    858-822-6937    mgm018@ucsd.edu    Principal Investigator: Hitendra Patel, MD          United States, Pennsylvania University of Pennsylvania Not yet recruiting Philadelphia, Pennsylvania, United States, 19104 Contact: Peter O'Dwyer    215-360-0716       Principal Investigator: Peter O'Dwyer          United Kingdom Barts Health NHS Trust Not yet recruiting London, United Kingdom, E1 1BB Contact: David Propper          Principal Investigator: David Propper Collapse <<
  NCT03129139	Advanced Cancer ... more >> Gastric Cancer Breast Cancer Pancreatic Cancer Prostate Cancer Metastatic Colo-rectal Cancer Solid Tumor Solid Carcinoma Solid Carcinoma of Stomach Cancer of Stomach Collapse <<	Phase 1	Recruiting	December 1, 2019	United States, Arizona ... more >> Mayo Clinic Arizona Recruiting Phoenix, Arizona, United States, 85054 Contact: Clinical Trial Referral Office , MD    855-776-0015       Principal Investigator: Ramesh Ramanathan, MD          HonorHealth Research Institute Recruiting Scottsdale, Arizona, United States, 85258 Contact: Joyce Schaffer, MSN,RN,AOCNS    480-323-1339    Joyce.schaffer@honorhealth.com    Principal Investigator: Erkut Borazanci, MD, MS          United States, California Cedars-Sinai Medical Center Recruiting Los Angeles, California, United States, 90048 Contact: Jaime Richardson, RN    310-423-2133    cancer.trial.info@cshs.org    Principal Investigator: Monica Mita, MD          United States, Florida Mayo Clinic Recruiting Jacksonville, Florida, United States, 32224 Contact: Clinical Trial Referral Office    855-776-0015       Principal Investigator: Kabir Mody, MD          United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Clinical Trial Referral Office    855-776-0015       Principal Investigator: Ciara O'Sullivan, M.B., B.Ch Collapse <<
  NCT02044952	Inflammatory Bowel Diseases ... more >> Crohn's Disease Gastrointestinal Diseases Digestive System Diseases Intestinal Diseases Collapse <<	Phase 2 Phase 3	Unknown	July 2016	China, Jiangsu ... more >> General Surgery Institute, Jinling Hospital Recruiting Nanjing, Jiangsu, China, 210000 Contact: wei ming zhu, PhD,MD    +86-25-80860137    dr_zhuweiming@126.com Collapse <<

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• 参考文献

• [1] Yang S, Chen J, et al. Triptolide inhibits the growth and metastasis of solid tumors. Mol Cancer Ther. 2003 Jan;2(1):65-72.

  [2] Qiu D, Zhao G, et al. Immunosuppressant PG490 (triptolide) inhibits T-cell interleukin-2 expression at the level of purine-box/nuclear factor of activated T-cells and NF-kappaB transcriptional activation. J Biol Chem. 1999 May 7;274(19):13443-50.

  [3] Ganguly S, Home T, Yacoub A, et al. Targeting HSF1 disrupts HSP90 chaperone function in chronic lymphocytic leukemia. Oncotarget.2015;6(31):31767-31779

  [4] Huang M, Zhang H, Liu T, Tian D, Gu L, Zhou M. Triptolide inhibits MDM2 and induces apoptosis in acute lymphoblastic leukemia cells through a p53-independent pathway. Mol Cancer Ther. 2013;12(2):184-194

  [5] Xu P, Li Z, Wang H, Zhang X, Yang Z. Triptolide Inhibited Cytotoxicity of Differentiated PC12 Cells Induced by Amyloid-Beta₂₅₋₃₅ via the Autophagy Pathway. PLoS One. 2015;10(11):e0142719.

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