Screening of Inflammatory Phospholipase $A_2$ Inhibitors from Natural Products

천연물로부터 염증성 포스포리파제 $A_2$ 저해제 검색

  • Published : 1997.10.01

Abstract

High levels of extracellular phospholipase $A_2$ (Plase $A_2$) associated with inflammatory process in man and animal models have been extensively reported elsew here. Thus, a logical approach to the treatment of inflammatory diseases should involve the inhibitors of Plase $A_2$. To develop new Plase $A_2$ inhibitors from natural products, two hundred crude drugs were screened using group II PLA$A_2$ inhibitory activity. Among them, methanol extract of 5 medicinal plants such as, Raphani Semen, Moutan cortex radicis, Arecae semen, Caryophylli Cortex and Betulae Cortex inhibited more than 90% of PLase $A_2$ activity at a concentration 2.5${\mu}g/ml$. Then, 10 methanol extracts sample were transferred into organic solvents, PLase $A_2$ inhibitory effects were found mainly in CHCl3 and EtoAc fractions.

Keywords

References

  1. v.56 Effect of ketotifen upon responses to platelet activating factor: A basic for asthma prophylaxis. Annals of Allergy. Morley, J.;Page, C. P.;Mazzoni, L.;Sanjar, S.
  2. Biochem. Biophys. Res. Commun. v.126 Structural identification of platelet activating factor in psoriatic scale. Mallet, A. I.;Cunningham, F. M.
  3. Biochem. Biophys. Res. Commun. v.127 Platelet activating factor(PAF) involvement in endotoxininduced hypotension in rats. Studies with PAF-receptors antagonist Kadsurenone. Doebber, T. W.;Wu, M.S.;Robbins, J.C.;Choy, B. M.;Chang, M. N.;Shen, T. Y.
  4. Throm. Res. v.25 Biosynthesis of platelet activating factor(PAF-acether). Involvement of phospholipase $A_2$ in the formation of PAF-acether and lyso-PAF-acether from rabbit platelet. Benveniste, J.;Chignard, M.;Le Couedic, J. P.;Vargaftig, B. B.
  5. Lab. Invest. v.55 Biology of diseases. Role of secretory phospholipase $A_2$ in the pathobiology of diseases. Vadas, P.;Pruzanski, P.
  6. J. Biochem. v.100 Extracellular phospholipase $A_2$ activity in peritoneal cavity of casein-treated rats. Chang, H. W.;Kudo, I.;Hara, S.;Inoue, K.
  7. J. Biochem. v.105 Hara, S.;Kudo, I.;Chang, H. W.;Inoue, K.;Purification and characterization of extracellular phospholipase $A_2$ from human synivial fluid in rheumatoid arthrits
  8. Life Sci. v.49 Detection and characterization of extracellular phospholipase $A_2$ in pleural effusion of patients with trberculosis. Baek, S. H.;Takayama, K.;Kudo, I.;Inoue, K.;Chang, H. W.
  9. Br. J. Dermatol. v.112 Characterization and activity of phospholipase $A_2$ in normal human epidermis and in lesion-free epidermis of patients with psoriasis or eczema. Forster, S.;Ilderton, E.;Norris, J. F. B.;Yardley, H. J.
  10. FEBS Lett. v.261 Group Ⅱ phospholipase $A_2$ mRNA synthesis is stimulated by two distinct mechanisms in rat smooth muscle cells. Nakano, T.;Ohara, O.;Teroka, H.;Arita, H.
  11. Biochem. Biophys. Res. Commun. v.174 Interleukin-1β, tumor necrosis factor and forskolin stimulate the synthesis of group Ⅱ phospholipase $A_2$ in rat mesangial cells. Schalkwijk, C.;Pfeilschifter, J.;Marki, F.;Van den Bosch, H.
  12. Int. Archa Allergy Appl. Immun. v.76 Inhibition of neutrophil phospholipase $A_2$ by ρ-bromophenacylbromide, nordihydroguaiaretic acid, 5, 8, 11, 14-eicosa-tetrayenoic acid and quercetin. Lanni, C.;Becker, E. L.
  13. Biochem. Pharmacol. v.39 Inactivation of human synovial fluid phospholipase A2 by the marine natural product. Manolide. Jacobson, P. B.;Marshall, L. A.;Sung, A.;Jacobs, R. S.
  14. Drug of the future v.15 no.2 Anti-inflammatory phospholipase $A_2$ inhibitors. Wilkerson, W. W.
  15. Agents and Actions. v.17 The inhibitory profiles of hog pancreatic and human rheumatoid synovial phospholipase $A_2$. Nixon, J. S.;Wilkinson, S. E.;Davis, P.;Bloxham, D. P.
  16. Toxicol. Appl. Pharmacol. v.90 Dantrolene and mepacrine antagonize the hemolysis of human red blood cell by halothane and bee venom phospholipass $A_2$. Fletcher, J.;Kistler, P.;Rosenberg, H.;Michaux, K.
  17. biotechnology v.5 Regulation of eicosanoid production: Role of phospholipase and inhibitors. Dennis, E. A.
  18. J. Immunol. v.151 Triggering of degranulation in mast cells by exogenous type Ⅱ phospholipase $A_2$. Murakami, M.;Hara, N.;Kudo, I.;Inoue, K.
  19. J. Biochem. v.100 Effect of serine phospholipid structure on the enhancement of concanavaline A induced degranulation in rat mast cell Horigome, K.;tamori-Natori, Y.;Inoue, K.;Nojima, S.
  20. J. Biochem. v.99 Properities of acid phospholipase in lysosome and extracellular medium of Tetrahymena pyriformis. Arai, H.;Inoue, K.;Nishikawa, K.;Banno, Y.;Nojima, S.
  21. Biochem. Biophys. Res. Commun. v.205 Inactivation of phospholipase $A_2$ by naturally occuring biflavonoid, ochnaflavone. chang, H. W.;Baek, S. H.;Chung, K. W.;Son, K. H.;Kim, H. P.;Kang, S. S.