膠質(zhì)毒素是由曲霉屬和其他具有不同生物活性的真菌的致病菌株產(chǎn)生的免疫抑制真菌毒素。[1]，[2]，[3]，[4]，[5]，[6]，[7]，[8]它抑制20S蛋白酶體糜蛋白酶活性(IC50 = 10微米)，阻斷IκBα的降解，阻止NF-κB的激活[2]，[3]膠質(zhì)毒素誘導單核細胞和樹突細胞凋亡，減少中性粒細胞的吞噬作用。[4]，[5]它抑制HEK293T細胞中尼帕病毒和亨德拉病毒的病毒感染(IC50s分別為149和579 nM)。[6]在還原條件下，膠質(zhì)毒素抑制白細胞三烯A4水解酶環(huán)氧化物水解酶活性，但不抑制氨肽酶活性和白細胞三烯B4在中性粒細胞和單核細胞中的合成。[7]在體內(nèi)，在酵母多糖a誘導的腹膜炎小鼠模型中，膠質(zhì)毒素(5 mg/kg)降低LTB4血漿水平并阻斷腹膜中性粒細胞浸潤。它還抑制牻牛兒牻牛兒基轉(zhuǎn)移酶I和法呢基轉(zhuǎn)移酶(IC50s分別為17和80微米)。[8]

產(chǎn)品性質(zhì)：

Cas No.:67-99-2

別名:膠霉毒素,Aspergillin

化學名: (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

儲存條件:Store at -20°C, protect from light

注意事項：

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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]. K?nig, 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).