Chapter 20. Complement Inhibitors

作者: Richard A. Patrick , Robert E. Johnson

DOI: 10.1016/S0065-7743(08)60381-4

关键词: Flufenamic acidComplement inhibitorBiochemistryAromatic amino acidsLeupeptinClassical complement pathwayProtease inhibitor (biology)HistamineIn vitroChemistry

摘要: Publisher Summary It is generally accepted that the treatment of certain diseases may be effected through control complement consumption by interrupting generation or action cellular stimuli attending inflammatory processes. Such include chemoattractants for polymorphonuclear leukocytes, inducements noncytotoxic enzyme secretion, histamine releasing agents, and permeability factors. Three fenamic acids, flufenamic, mefanamic, niflumic, block classical pathway activity. Flufenamic acid was most active this group, showing significant inhibition at 0.05 mM with human complement. Aromatic amino acids represent another class compounds alter activity more than a single reaction step. possessing phenolic hydroxyl group were shown to especially in inhibiting C4 sites (IIc). Certain peptides have been interfere function. Leupeptin (acetyl-leucyl-leucyl–arginal), protease inhibitor derived from actinomycete fermentation, an effective inhibitor. In vitro (50%) 0.5 mM. Polynucleotides, polyanionic substances, phenols, amines, other groups also come under discussion on inhibitors. The inorganics shows zinc cation reported reversibly inhibit whole 0.025 0.50 utilization every component except C5 C9 inhibited (12%-55%) 0.025-0.50

参考文章(70)
H Mineda, A Takada, Y Takada, Y Arimoto, Inhibition of the classical and alternative pathways by amino acids and their derivatives. Immunology. ,vol. 34, pp. 509- 515 ,(1978)
J. S. C. Fong, R. A. Good, Suramin--a potent reversible and competitive inhibitor of complement systems. Clinical and Experimental Immunology. ,vol. 10, pp. 127- ,(1972)
N Tamura, A S Baba, Influence of aromatic compounds on the interaction of activated C4 with EAC1. Immunology. ,vol. 32, pp. 251- ,(1977)
N. L. Gottlieb, R. M. Stroud, Patricia I. Arnold, K. Sakai, D. R. Schultz, J. E. Volanakis, Inactivation of C1 in rheumatoid synovial fluid, purified C1 and C1 esterase, by gold compounds Clinical and Experimental Immunology. ,vol. 17, pp. 395- 406 ,(1974)
Syed Shafi Asghar, K.W. Pondman, R.H. Cormane, Inhibition of C1r̄, C1s̄ and generation of C1s̄ by amidino compounds Biochimica et Biophysica Acta. ,vol. 317, pp. 539- 548 ,(1973) , 10.1016/0005-2795(73)90247-X
Taroh Kinoshita, Taketoshi Izawa, Kyongsu Hong, Wasei Miyazaki, Kozo Inoue, An Anticomplementary Agent, K-76 Monocarboxylic Acid: Its Site and Mechanism of Inhibition of the Complement Activation Cascade Journal of Immunology. ,vol. 122, pp. 2418- 2423 ,(1979)
Thomas W. Harrity, Marvin B. Goldlust, Anti-complement effects of two anti-inflammatory agents: Niflumic and flufenamic acids Biochemical Pharmacology. ,vol. 23, pp. 3107- 3120 ,(1974) , 10.1016/0006-2952(74)90596-6
Daniel Rosenblum, Donald Chatman, Stanley Yachnin, Biologic Properties of Polynucleotides: V. Studies on the Inhibition of the First Component of Complement by Polyinosinic Acid: the Interaction with C′1q Journal of Immunology. ,vol. 93, pp. 540- 548 ,(1964)