Sarosiek J, Bilski J, Tsukada H, Slomiany A, Slomiany B L
Department of Medicine, New York Medical College, Valhalla.
Digestion. 1987;37(4):238-46. doi: 10.1159/000199507.
The effect of a new antiulcer drug, solon (sofalcone), on gastric mucus viscosity, permeability to hydrogen ion and degradation by pepsin was investigated using an in vitro system. Preincubation of the isolated gastric mucus with solon produced a marked enhancement in mucus viscosity. This enhancement was concentration dependent and at 2.2 X 10(-1) M solon reached a value of 230%. Permeability measurements showed that 2.2 X 10(-2) M solon increased the retardation ability of mucus to hydrogen ion by 32%, while 43% increase was obtained with 2.2 X 10(-1) M solon. The drug had no effect on the viscosity and hydrogen ion retardation capacity of albumin. The results of peptic activity assay indicated that solon had an inhibitory effect on the rate of mucus and albumin proteolysis. The rate of inhibition of peptic activity was proportional to the solon concentration up to 1.0 X 10(-5) M, at which concentration the proteolysis of mucus was inhibited by 60% and that of albumin by 45%. The results obtained here under in vitro conditions suggest that solon, by inhibiting peptic erosion of the mucus layer, increasing its viscosity and enhancing the ability to impede the hydrogen ion penetration, strengthens the gastric mucosal integrity and thus could aid in ulcer healing.
使用体外系统研究了一种新型抗溃疡药物索隆（索法酮）对胃黏液黏度、氢离子通透性及胃蛋白酶降解作用的影响。将分离出的胃黏液与索隆预孵育后，黏液黏度显著增加。这种增加呈浓度依赖性，在2.2×10⁻¹ M索隆时达到230%的值。通透性测量表明，2.2×10⁻² M索隆使黏液对氢离子的阻滞能力提高了32%，而2.2×10⁻¹ M索隆则使该能力提高了43%。该药物对白蛋白的黏度和氢离子阻滞能力无影响。胃蛋白酶活性测定结果表明，索隆对黏液和白蛋白的蛋白水解速率有抑制作用。在浓度高达1.0×10⁻⁵ M时，胃蛋白酶活性的抑制速率与索隆浓度成正比，在此浓度下，黏液的蛋白水解被抑制60%，白蛋白的蛋白水解被抑制45%。在体外条件下获得的结果表明，索隆通过抑制胃蛋白酶对黏液层的侵蚀、增加其黏度并增强其阻止氢离子渗透的能力，加强了胃黏膜的完整性，从而有助于溃疡愈合。
