生物活性

• 描述Carmustine is an antitumor chemotherapeutic agent, which works by akylating DNA and RNA. NAT (N-acetyltransferase) activity in glial tumor cell cytosols and intact tumor cells were decreased by carmustine in a dose-dependent manner. Carmustine (8, 80, and 800 µM) decreases N-acetyltransferase (NAT) activities for 2-aminofluorene (AF) and p-aminobenzoic acid (PABA) in rat glial tumor cytosol and intact cells. In rat glial tumor cells, the DNA-AF adduct increases, and carmustine decreases the formation of DNA-AF adduct^[3]. Preincubation of cells with the glutathione reductase inhibitor, carmustine, led to elevated basal [Ca2+]i, yet the cells remained responsive to bradykinin^[4]. Carmustine (≥25 µM) stimulates eryptosis at least partially by increasing cytosolic Ca²⁺ activity^[5]. Carmustine (BCNU; 25 mg/kg, i.p.) causes higher levels of the rhe ratio of liver weight to body weight and plasma conjugated bilirubin, and lower biliary flow, oxidised glutation levels (GSSG) and reduced glutation (GSH)/GSSG values compared with control rats^[6].
• 临床研究

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  NCT03072771	Diffuse Large B Cell Lymphoma	Phase 1	Recruiting	September 30, 2021	United States, Missouri ... more >> Washington University School of Medicine Recruiting Saint Louis, Missouri, United States, 63110 Contact: Armin Ghobadi, M.D.    314-747-2743    arminghobadi@wustl.edu    Principal Investigator: Armin Ghobadi, M.D. Collapse <<
  NCT02504359	Plasma Cell Leukemia ... more >> Recurrent Plasma Cell Myeloma Collapse <<	Phase 1	Recruiting	July 1, 2021	United States, North Carolina ... more >> Duke University Medical Center Recruiting Durham, North Carolina, United States, 27710 Contact: Cristina Gasparetto    919-668-1017    cristina.gasparetto@duke.edu    Principal Investigator: Cristina Gasparetto          United States, Oregon OHSU Knight Cancer Institute Recruiting Portland, Oregon, United States, 97239 Contact: Emma C. Scott    503-494-2398    scottem@ohsu.edu    Principal Investigator: Emma C. Scott Collapse <<

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• 参考文献

• [1] Doishita S, Shimono T, et al. In vitro Study of Serial Changes to Carmustine Wafers (Gliadel) with MR Imaging and Computed Tomography. Magn Reson Med Sci. 2017 Sep 4.

  [2] Lin SH, Kleinberg LR. Carmustine wafers: localized delivery of chemotherapeutic agents in CNS malignancies. Expert Rev Anticancer Ther. 2008 Mar;8(3):343-59.

  [3] Hung CF. Effects of carmustine and lomustine on arylamine N-acetyltransferase activity and 2-aminofluorene-DNA adducts in rat glial tumor cells. Neurochem Res. 2000 Jun;25(6):845-51

  [4] Elliott SJ, Schilling WP. Carmustine augments the effects of tert-butyl hydroperoxide on calcium signaling in cultured pulmonary artery endothelial cells. J Biol Chem. 1990 Jan 5;265(1):103-7

  [5] Jilani K, Lang F. Carmustine-induced phosphatidylserine translocation in the erythrocyte membrane. Toxins (Basel). 2013 Apr 19;5(4):703-16

  [6] Demir A, Özütemiz O, Yildiz C, Yüce G, Tekeşin O, Ilter T. The effect of trimetazidine on intrahepatic cholestasis caused by carmustine in rats. Hepatol Res. 2001 May 1;20(1):133-143

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