Selenke W M, Leung G W, Townley R G
J Allergy Clin Immunol. 1980 Jun;65(6):454-64. doi: 10.1016/0091-6749(80)90239-0.
Certain macrolide antibiotics, such as troleandomycin (TAO), oleandomycin, and erythromycin estolate (Ilosone), can lower the maintenance dose of glucocorticoids required by severely asthmatic patients. These effects were postulated to be caused by an as yet undefined steroid-sparing effect. In this study, TAO in combination with methylprednisolone, when compared with methylprednisolone alone, was demonstrated to significantly increase liver glycogen deposition in adrenalectomized mice, intact mice, and adrenalectomized rats; protect histamine-sensitized mice following beta adrenergic blockade or adrenalectomy; further decrease the steroid-lowered glucose tolerance of mice and significantly increase the plasma corticosteroid levels in rats. TAO alone did not have these effects. TAO plus betamethasone, and erythromycin estolate plus methylprednisolone also increased liver glycogen deposition. However, TAO did not appear to potentiate the effects of hydrocortisone. Erythromycin stearate and to a lesser degree erythromycin ethylsuccinate when combined with methylprednisolone also decreased histamine lethality in mice. Leucomycin and tetracycline did not enhance the effects of methylprednisolone. TAO, alone or with methylprednisolone, did not alter serum glutamic oxaloacetic transaminase (SGOT) levels in rats. Thus, TAO and some other macrolides did not exert their effects on corticosteroids as antimicrobial agents, adrenocorticotropic hormone (ACTH)--like compounds, or quasisteroids, but as steroid-sparing agents by some undefined mechanism.
某些大环内酯类抗生素，如三乙酰竹桃霉素（TAO）、竹桃霉素和无味红霉素（依托红霉素），可降低重症哮喘患者所需的糖皮质激素维持剂量。这些作用被推测是由一种尚未明确的激素节省效应引起的。在本研究中，与单独使用甲基强的松龙相比，TAO联合甲基强的松龙被证明能显著增加去肾上腺小鼠、完整小鼠和去肾上腺大鼠的肝糖原沉积；在β肾上腺素能阻断或去肾上腺后保护组胺致敏小鼠；进一步降低小鼠因激素导致的葡萄糖耐量降低，并显著提高大鼠血浆皮质类固醇水平。单独使用TAO没有这些作用。TAO加倍他米松以及无味红霉素加甲基强的松龙也增加了肝糖原沉积。然而，TAO似乎没有增强氢化可的松的作用。硬脂酸红霉素以及程度较轻的琥乙红霉素与甲基强的松龙联合使用时，也降低了小鼠组胺致死率。柱晶白霉素和四环素没有增强甲基强的松龙的作用。单独使用TAO或与甲基强的松龙联合使用，均未改变大鼠血清谷氨酸草酰乙酸转氨酶（SGOT）水平。因此，TAO和其他一些大环内酯类抗生素并非作为抗菌剂、促肾上腺皮质激素（ACTH）样化合物或类甾体发挥对皮质类固醇的作用，而是通过某种未明确的机制作为激素节省剂发挥作用。
