Gliotoxin-13C13

Gliotoxin-13C13 is intended for use as an internal standard for the quantification of gliotoxin (Item No. 11433) by GC- or LC-MS. Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi with diverse biological activities.1,2,3,4,5,6,7,8 It inhibits 20S proteasomal chymotrypsin activity (IC50 = 10 μM), blocking the degradation of IκBα and preventing the activation of NF-κB.2,3 Gliotoxin induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutrophils.4,5 It suppresses viral infection by Nipah and Hendra virus in HEK293T cells (IC50s = 149 and 579 nM, respectively).6 Under reducing conditions, gliotoxin inhibits leukotriene A4 hydrolase (LTA4H; Item No. 10007817) epoxide hydrolase activity, but not aminopeptidase activity, and leukotriene B4 (LTB4; Item No. 20110) synthesis in neutrophils and monocytes.7 In vivo, gliotoxin (5 mg/kg) reduces LTB4 plasma levels and blocks peritoneal neutrophil infiltration in a mouse model of peritonitis induced by zymosan A (Item No. 21175). It also inhibits geranylgeranyltransferase I and farnesyltransferase (IC50s = 17 and 80 μM, respectively).8WARNING This product is not for human or veterinary use.

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[2] M KROLL. The secondary fungal metabolite gliotoxin targets proteolytic activities of the proteasome.[J]. Chemistry & biology, 1999, 6 10: 689-698. DOI: 10.1016/s1074-5521(00)80016-2
[3] H L PAHL. The immunosuppressive fungal metabolite gliotoxin specifically inhibits transcription factor NF-kappaB.[J]. Journal of Experimental Medicine, 1996, 183 4: 1829-1840. DOI: 10.1084/jem.183.4.1829
[4] KRISTIN ANSELMI. Gliotoxin causes apoptosis and necrosis of rat Kupffer cells in vitro and in vivo in the absence of oxidative stress: Exacerbation by caspase and serine protease inhibition[J]. Journal of Hepatology, 2007, 47 1: Pages 103-113. DOI: 10.1016/j.jhep.2007.02.024
[5] ENRICO ORCIUOLO. Effects of Aspergillus fumigatus gliotoxin and methylprednisolone on human neutrophils: implications for the pathogenesis of invasive aspergillosis[J]. Journal of Leukocyte Biology, 2007, 82 4: 839-848. DOI: 10.1189/jlb.0207090
[6] MOHAMAD ALJOFAN. Antiviral activity of gliotoxin, gentian violet and brilliant green against Nipah and Hendra virus in vitro.[J]. Virology Journal, 2009: 187. DOI: 10.1186/1743-422x-6-187
[7] STEFANIE KÖNIG . Gliotoxin from Aspergillus fumigatus Abrogates Leukotriene B4 Formation through Inhibition of Leukotriene A4 Hydrolase[J]. Cell Chemical Biology, 2019, 26 4: Pages 524-534.e5. DOI: 10.1016/j.chembiol.2019.01.001
[8] D M VIGUSHIN. Gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with antitumor activity against breast cancer in vivo.[J]. Medical Oncology, 2004, 21 1: 21-30. DOI: 10.1385/mo:21:1:21