Meunier M T, Villie F, Bastide P
Laboratoire de Pharmacologie et de Pharmacie Clinique, Faculté de Pharmacie, Clermont-Ferrant, France.
J Pharm Belg. 1994 Nov-Dec;49(6):453-61.
Cupressus sempervirens L. proanthocyanidolic (O.P.C.) oligomers inhibited the esterolytic activity of pancreatic elastase with a Cl50 of 0.0075 mg/ml when a sap substrate suc(Al)3NA was used in a Tris-HCl 0.05 M buffer with a pH of 7.5. Inhibition was slightly lower when the ionic strength of the buffer was increased. Elastolytic activity was inhibited using an elastinorcein substrate with a Cl50 of 0.05 mg/ml, whatever the pH or the ionic strength of the buffer. The oligomers bound with the elastase to form a precipitant complex where a 2 mg/ml concentration of oligomers precipitated the elastase at 1 mg/ml. Insoluble elastin fixed few 150 micrograms oligomers for 1 mg of elastin but the latter was partly protected by the subsequent action of the elastase. Soluble elastin fixed a greater number of oligomers but it was the peptids of elastin enzyme hydrolysis which fixed the largest amount: around 1500 micrograms per mg. The oligomers-elastin complex seems to be more stable than that of oligomers-elastase which regains part of its esterase activity. The elastic fibers seem to be protected by the O.P.C.
意大利柏木原花青素（O.P.C.）低聚物在0.05M Tris-HCl缓冲液（pH 7.5）中使用底物suc(Al)3NA时，对胰腺弹性蛋白酶的酯解活性具有抑制作用，其半数抑制浓度（Cl50）为0.0075mg/ml。当缓冲液的离子强度增加时，抑制作用略有降低。无论缓冲液的pH值或离子强度如何，使用弹性蛋白orcein底物时弹性蛋白酶活性均受到抑制，Cl50为0.05mg/ml。低聚物与弹性蛋白酶结合形成沉淀复合物，其中2mg/ml浓度的低聚物可使1mg/ml的弹性蛋白酶沉淀。不溶性弹性蛋白每毫克弹性蛋白固定少量150微克低聚物，但弹性蛋白酶的后续作用可对其提供部分保护。可溶性弹性蛋白固定的低聚物数量更多，但弹性蛋白酶解产生的肽段固定的低聚物数量最多：每毫克约1500微克。低聚物-弹性蛋白复合物似乎比低聚物-弹性蛋白酶复合物更稳定，后者可恢复部分酯酶活性。弹性纤维似乎受到原花青素的保护。
