Boskey A L, Goldberg M R, Posner A S
Calcif Tissue Int. 1979 Mar 13;27(1):83-8. doi: 10.1007/BF02441165.
The diphosphonates disodium ethane-1-hydroxy-1, 1-diphosphonate (EHDP) and disodium dichloromethylene diphosphonate (Cl2MDP) prevent hydroxyapatite (HA) formation in metastable calcium phosphate solutions, induced by calcium-phospholipid-phosphate complexes and by the acidic phospholipids phosphatidyl serine and phosphatidyl inositol. The diphosphonates appear to act not only as HA crystal poisons but also as surfactants which probably change the nature of the lipid micelle and the charge and conformational properties of the lipid molecules. The surfactants sodium dodecyl sulfate (SDS) and Non-Idet P-40 (NP-40), like the diphosphonates, prevent HA formation by the acidic phospholipids and complexed lipids, but do not act as HA surface poisons. The lipid surfactant lyso-phosphatidyl serine did not induce HA formation from solution. The relevance of the ability of the diphosphonates to act as lipid surfactants to the in vivo use of these agents is discussed.
二膦酸盐乙烷-1-羟基-1,1-二膦酸二钠(EHDP)和二氯亚甲基二膦酸二钠(Cl2MDP)可防止在由钙-磷脂-磷酸盐复合物以及酸性磷脂磷脂酰丝氨酸和磷脂酰肌醇诱导形成的亚稳磷酸钙溶液中形成羟基磷灰石(HA)。二膦酸盐似乎不仅作为HA晶体毒物起作用,还作为表面活性剂,可能改变脂质微团的性质以及脂质分子的电荷和构象性质。表面活性剂十二烷基硫酸钠(SDS)和非离子去污剂P-40(NP-40)与二膦酸盐一样,可防止酸性磷脂和复合脂质形成HA,但不作为HA表面毒物起作用。脂质表面活性剂溶血磷脂酰丝氨酸不会从溶液中诱导形成HA。讨论了二膦酸盐作为脂质表面活性剂的能力与这些药物在体内使用的相关性。