Gachet C, Ennamany R, Kretz O, Ohlmann P, Krause C, Creppy E E, Dirheimer G, Cazenave J P
INSERM U.311, Centre Régional de Transfusion Sanguine, Strasbourg, France.
Hum Exp Toxicol. 1996 Jan;15(1):26-9. doi: 10.1177/096032719601500105.
Bolesatine is a toxic glycoprotein isolated from the mushroom Boletus satanas Lenz, which has been shown to inhibit protein synthesis in cell-free systems and cell culture. It is toxic to rodents, the LD50% 24 h being 1 mg kg-1 (i.p.) and 0.15 mg kg-1 (i.v.) in the rat in which it induces hepatic blood stasis. Bolesatine possesses lectinic properties with in particular a sugar binding site for D-galactose and mitogenic activity toward lymphocytes. Tested for cell agglutination on red blood cells and platelets, bolesatine agglutinates both human and rat platelets from threshold concentrations of 30 and 300 nM respectively. EDTA and PGI2 (aggregation inhibitors) do not decrease the agglutination induced by bolesatine, indicating that the process does not involve platelet activation. In contrast, fibrinogen decreases platelet agglutination induced by bolesatine, most likely by masking the binding sites on platelets or by interacting with the toxin. Bolesatine agglutinates all red blood cells without any blood group specificity in the concentration range of 20 to 40 nM. This haemagglutination cannot be prevented by sugars, including D-galactose at a concentration of 0.5 M.
博来他汀是一种从毒红菇中分离出的有毒糖蛋白，已证实在无细胞系统和细胞培养中可抑制蛋白质合成。它对啮齿动物有毒，在大鼠中其24小时半数致死剂量（LD50%）腹腔注射为1毫克/千克，静脉注射为0.15毫克/千克，可导致肝淤血。博来他汀具有凝集素特性，尤其具有与D-半乳糖结合的糖结合位点以及对淋巴细胞的促有丝分裂活性。在对红细胞和血小板进行细胞凝集测试时，博来他汀分别从30和300纳摩尔的阈值浓度开始凝集人和大鼠的血小板。乙二胺四乙酸（EDTA）和前列环素（PGI2，聚集抑制剂）不会降低博来他汀诱导的凝集，表明该过程不涉及血小板活化。相反，纤维蛋白原可降低博来他汀诱导的血小板凝集，很可能是通过掩盖血小板上的结合位点或与毒素相互作用来实现的。在20至40纳摩尔的浓度范围内，博来他汀可凝集所有红细胞，且无血型特异性。这种血细胞凝集不能被糖类阻止，包括浓度为0.5摩尔的D-半乳糖。
