YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Protein Fraction Extracted from the Earthworm Lumbricus rubellus Activates Proteinase Activated Receptor-2 and is Effective on Hemokinesis

적토룡 추출 단백분획의 프로테나제 유도 수용체-2의 활성화 및 형행개선 효과

  • Lee, Chul-Kyu (Central Research Institute, Shin Poong Pharm. Co. Ltd.) ;
  • Shin, Jang-Sik (Central Research Institute, Shin Poong Pharm. Co. Ltd.) ;
  • Choi, Young-Keun (Central Research Institute, Shin Poong Pharm. Co. Ltd.) ;
  • Lim, Chae-Kon (Central Research Institute, Shin Poong Pharm. Co. Ltd.) ;
  • Cho, Il-Hwan (Central Research Institute, Shin Poong Pharm. Co. Ltd.) ;
  • Kim, Chul (Central Research Institute, Shin Poong Pharm. Co. Ltd.)
  • 이철규 (신풍제약(주) 중앙연구소) ;
  • 신장식 (신풍제약(주) 중앙연구소) ;
  • 최영근 (신풍제약(주) 중앙연구소) ;
  • 임채곤 (신풍제약(주) 중앙연구소) ;
  • 조일환 (신풍제약(주) 중앙연구소) ;
  • 김철 (신풍제약(주) 중앙연구소)
  • Published : 1997.04.01
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Abstract

The proteinase-activated receptor (PAR-2) belongs to the family of seven transmembrane region receptors, like the thrombin receptor, it is activated by specific proteolytic clea vage of its extracellular amino terminus and a synthetic peptide (SLIGRL). The earthworm protein fraction (EPF) extracted from Lumbricus rubellus elicted dose- and endothelium-dependent relaxations in phenylephrine-contracted rat thoracic aorta, whereas heat inactivated EPF (0.5 ${\mu}g$ /ml) had no effect. In the presence of the nitric oxide synthase inhibitor NG-methyl-L-arginine (1.8 micro M), EPF (0.5 ${\mu}g$ /ml)-induced relaxations were partially inhibited. Furthermore, EPF (0.5 ${\mu}g$ /ml) dramatically caused relaxation of thrombin-desenstized rat thoracic aorta. These results indicate that EPF activates PAR-2 in vascular endothelial cell. Intravenous injection of EPF (20 mg/kg, bolus) into anesthetized rats produced a marked depressor response. EPF (0 ~ 80 ${\mu}g$ /ml, gradient) was very effective on increasing of perfusion volume in rabbit ear vessel preparations. These results imply the usefulness of EPF as a vascular smooth muscle relaxant and indicate that the activation of PAR-2 may be a mechanism of EPF on hemokinetic improvement.

Keywords

References

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