Takeda Seiichi, Toda Takao, Nakamura Kazuki
Research and Development Center, Fuso Pharmaceutical Industries Ltd, Osaka, Japan
Research and Development Center, Fuso Pharmaceutical Industries Ltd, Osaka, Japan.
In Vivo. 2019 Jan-Feb;33(1):53-55. doi: 10.21873/invivo.11438.
BACKGROUND/AIM: We investigated the inhibitory action of medium molecular weight heparinyl phenylalanine (MHF) on type I hypersensitivity in comparison with medium molecular weight heparinyl arginine (MHR).
MHF and MHR were synthesized from heparin (HE) to decrease the side-effect of HE based on its anticoagulant action and used in this study.
MHF demonstrated a significant inhibitory action on 48-h homologous passive cutaneous anaphylaxis in rats. Although MHF did not affect the death of mice injected with a lethal dose of histamine, it significantly prolonged the survival time of mice administered a lethal dose of compound 48/80. On the other hand, MHR did not inhibit type I hypersensitivity.
The inhibitory action of MHF on the type I allergic reaction was due to a reduction or delay in histamine release from mast cells. MHF may be a potent anti-allergic agent.
背景/目的:我们研究了中分子量肝素苯丙氨酸(MHF)与中分子量肝素精氨酸(MHR)相比对I型超敏反应的抑制作用。
基于肝素(HE)的抗凝作用,从肝素合成了MHF和MHR以降低HE的副作用,并用于本研究。
MHF对大鼠48小时同源被动皮肤过敏反应表现出显著的抑制作用。虽然MHF不影响注射致死剂量组胺的小鼠的死亡,但它显著延长了给予致死剂量化合物48/80的小鼠的存活时间。另一方面,MHR不抑制I型超敏反应。
MHF对I型过敏反应的抑制作用是由于肥大细胞组胺释放减少或延迟。MHF可能是一种有效的抗过敏剂。