Complexation and ionophoric properties of taxol and colchicine: complex formation and transport of sodium, potassium, magnesium and calcium ions across a liquid membrane.

M Blaghen, N Lahlou, F Z Dzairi, A Moutaouakkil, M Talbi
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引用次数: 2

Abstract

We report the activities of taxol (an anticancer drug) and colchicine, which are inhibitors of microtubule organization, on the complexation and transport of Na+, K+, Mg2+ and Ca2+ ions across a liquid membrane, using a spectrophotometric procedure. Taxol, a diterpenoid compound, that has been demonstrated to possess a potent antitumour activity, is shown to extract Na+, K+, Mg2+ and Ca2+ ions from the aqueous solution to the organic phase with preference for Ca2+ ions. A kinetic study of the transport and complexation of Na+, K+, Mg2+ and Ca2+ ions through a liquid membrane revealed that the K+ ion is more rapidly transported and the Ca2+ ion is more rapidly complexed than other ions. However, colchicine, another alkaloid compound, extracted and transported only the divalent ions tested, Mg2+ and Ca2+. In both complexation and transport, the flux of the ions increases with the concentration of taxol or colchicine. Complexation and ionophoric properties of taxol and colchicine sheds new lights on therapeutic properties of these drugs. The treatment of disease states by the administration of these drugs to alter membrane permeability will prove to be a valuable therapeutic concept.

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紫杉醇和秋水仙碱的络合和离子亲和性:钠、钾、镁和钙离子在液体膜上的络合形成和运输。
我们报告了紫杉醇(一种抗癌药物)和秋水仙碱的活性,这是微管组织的抑制剂,对络合和运输的Na+, K+, Mg2+和Ca2+离子通过液膜,使用分光光度法程序。紫杉醇是一种二萜类化合物,已被证明具有有效的抗肿瘤活性,可以从水溶液中提取Na+, K+, Mg2+和Ca2+离子到有机相,并优先提取Ca2+离子。对Na+、K+、Mg2+和Ca2+离子在液膜中的转运和络合动力学研究表明,K+离子比其他离子转运更快,Ca2+离子比其他离子络合更快。然而,秋水仙碱,另一种生物碱化合物,只提取和运输二价离子,Mg2+和Ca2+。在络合和转运过程中,离子通量随紫杉醇或秋水仙碱浓度的增加而增加。紫杉醇和秋水仙碱的络合性和离子亲和性为研究这些药物的治疗特性提供了新的思路。通过给予这些药物来改变膜的通透性来治疗疾病状态将被证明是一个有价值的治疗概念。
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Erratum: Alfonso D, Johnson HA, Colman-Saizarbitoria T, Presley CP, McCabe GP, McLaughlin JL (1996): SARs of annonaceous acetogenins in rat liver mitochondria. Nat Toxins 4:181-188. Advances in detection methods for fungal and algal toxins. HPLC/MS analysis of fusarium mycotoxins, fumonisins and deoxynivalenol. Neuronal binding of tetanus toxin compared to its ganglioside binding fragment (H(c)). A new type sandwich immunoassay for microcystin: production of monoclonal antibodies specific to the immune complex formed by microcystin and an anti-microcystin monoclonal antibody.
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