Kurbanov O G, Kasumov Kh M
Antibiot Khimioter. 2004;49(3):40-6.
The review is concerned with the outlooks for the use of levorin, a membrane active and channel forming polyene antibiotic, and its alkyl derivatives in muscle activity. In complex with cholesterol and ergosterol, the aromatic heptaene antibiotic levorin forms structural ionic channels of the molecular size in the lipid and cell membranes. Levorin increases the membrane permeability for monosucrose and other neutral molecules as follows: H2O > urea > acetamide > glycerine > ribose > arabinose > glucose > saccharose. As a channel forming compound, levorin is able to induce in the cell membranes of the muscle fibres formation of additional channels permeable for the cations and to increase the flow of the energy dependent substrates to the cells and the outburst of the metabolites from them during intensive muscle activity. Levorin several times decreases the surface tension of aqueous solutions. In some models of experimental animals levorin promoted an increase of the blood fluidity and accelerated the blood stream in the blood vessels both in rest and in muscle activity. Physical load in a high power zone increases the intensity of lipid peroxidation that results in fatigue and lower physical efficiency. Possible prevention of an increase of the rate of free radical reactions by levorin and its alkyl derivatives providing higher antioxidant protection is discussed.
本综述关注的是左菌素（一种具有膜活性且能形成通道的多烯抗生素）及其烷基衍生物在肌肉活动中的应用前景。芳香族七烯抗生素左菌素与胆固醇和麦角固醇结合后，会在脂质膜和细胞膜中形成分子大小的结构离子通道。左菌素会按以下顺序增加单糖及其他中性分子的膜通透性：水＞尿素＞乙酰胺＞甘油＞核糖＞阿拉伯糖＞葡萄糖＞蔗糖。作为一种能形成通道的化合物，左菌素能够在肌肉纤维的细胞膜中诱导形成额外的阳离子可通透通道，并在剧烈肌肉活动期间增加能量依赖型底物向细胞的流动以及代谢产物从细胞中的释放。左菌素能使水溶液的表面张力降低数倍。在一些实验动物模型中，左菌素在休息和肌肉活动状态下均能促进血液流动性增加并加速血管中的血流。高功率区域的体力负荷会增加脂质过氧化的强度，从而导致疲劳和体能下降。本文讨论了左菌素及其烷基衍生物通过提供更高的抗氧化保护来防止自由基反应速率增加的可能性。
