胶质毒素是由曲霉属和其他具有不同生物活性的真菌的致病菌株产生的免疫抑制真菌毒素。[1]，[2]，[3]，[4]，[5]，[6]，[7]，[8]它抑制20S蛋白酶体糜蛋白酶活性(IC50 = 10微米)，阻断IκBα的降解，阻止NF-κB的激活[2]，[3]胶质毒素诱导单核细胞和树突细胞凋亡，减少中性粒细胞的吞噬作用。[4]，[5]它抑制HEK293T细胞中尼帕病毒和亨德拉病毒的病毒感染(IC50s分别为149和579 nM)。[6]在还原条件下，胶质毒素抑制白细胞三烯A4水解酶环氧化物水解酶活性，但不抑制氨肽酶活性和白细胞三烯B4在中性粒细胞和单核细胞中的合成。[7]在体内，在酵母多糖a诱导的腹膜炎小鼠模型中，胶质毒素(5 mg/kg)降低LTB4血浆水平并阻断腹膜中性粒细胞浸润。它还抑制牻牛儿牻牛儿基转移酶I和法呢基转移酶(IC50s分别为17和80微米)。[8]

产品性质：

Cas No.:67-99-2

别名:胶霉毒素,Aspergillin

化学名: (3R,5aS,6S,10aR)-6-hydroxy-3-(hydroxymethyl)-2-methyl-2,3,5a,6-tetrahydro-1H-3,10a-epidithiopyrazino[1,2-a]indole-1,4(10H)-dione

Canonical SMILES O[C@H]1C=CC=C2[C@@H]1N(C([C@@]3(N4C)CO)=O)[C@@](C4=O)(SS3)C2

分子式:C13H14N2O4S2

分子量:326.38

溶解度:5mg/mL in DMSO, or in DMF

储存条件:Store at -20°C, protect from light

注意事项：

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References:

[1]. Kwon-Chung, K.J., and Sugui, J.A. What do we know about the role of gliotoxin in the pathobiology of Aspergillus fumigatus? Med. Mycol. 47(Suppl 1), S97-S103 (2009).

[2]. Kroll, M., Arenzana-Seisdedos, F., Bachelerie, F., et al. The secondary fungal metabolite gliotoxin targets proteolytic activities of the proteasome. Chem. Biol. 6(10), 689-698 (1999).

[3]. Pahl, H.L., Krauss, B., Schulze-Osthoff, K., et al. The immunosuppressive fungal metabolite gliotoxin specifically inhibits transcription factor NF-κB. J. Exp. Med. 183(4), 1829-1840 (1996).

[4]. Anselmi, K., Stolz, D.B., Nalesnik, M., et al. 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. Hepatol. 47(1), 103-113 (2007).

[5]. Orciuolo, E., Stanzani, M., Canestraro, M., et al. Effects of Aspergillus fumigatus gliotoxin and methylprednisolone on human neutrophils: Implications for the pathogenesis of invasive aspergillosis. J. Leukoc. Biol. 82(4), 839-848 (2007).

[6]. Aljofan, M., Sganga, M.L., Lo, M.K., et al. Antiviral activity of gliotoxin, gentian violet and brilliant green against Nipah and Hendra virus in vitro. Virol. J. 6:187, (2009).

[7]. König, Pace, S., Pein, H., et al. Gliotoxin from Aspergillus fumigatus abrogates leukotriene B4 formation through inhibition of leukotriene A4 hydrolase. Cell. Chem. Biol. 26(4), 524-534 (2019).

[8]. Vigushin, D.M., Mirsaidi, N., Brooke, G., et al. Gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with antitumor activity against breast cancer in vivo. Med. Oncol. 21(1), 21-30 (2004).