Molecular and Cellular Biochemistry

, Volume 124, Issue 2, pp 107–114 | Cite as

Inhibition of monoamine oxidase-A of rat brain by pyrethroids — anin vitro kinetic study

  • Gazula Valeswara Rao
  • K. S. Jagannatha Rao


Anin vitro kinetic study on inhibition of the monoamine oxidase-A (MAO-A) of the rat brain by two pyrethroids, namely permethrin (PM) and cypermethrin (CPM), has shown that PM and CPM competitively inhibit MAO-A by altering both the Michaelis-Menten constant (Km) and the maximum velocity (Vmax). Inhibitor constant values (Ki) indicated that CPM was a more effective inhibitor of MAO-A than PM. Both PM and CPM caused maximum inhibition of MAO-A at neutral pH. CPM significantly elevated the activation energy values of MAO-A as compared to those of PM.

Key words

permethrin cypermethrin monoamine oxidase-A 



Manoamine Oxidase






Toxicity Test Value


Inhibitor Concentration that causes 50 percent inhibition


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  1. 1.
    Fu RC, Xian-Fang Liu, Shiuan Chen: Inhibition of monoamine oxidase by 7-chloro-4-nitrobenzofurazan. J Neurochem 55:813–818, 1990Google Scholar
  2. 2.
    Johnston JP: Some observations upon a new inhibitor of monoamine oxidase in brain tissue. Biochem Pharmacol 17:1285–1297, 1968Google Scholar
  3. 3.
    Houslay MD, Tipton KF, Youdim MBH: Multiple forms of monoamine oxidase: fact and artefact. Life Sci 19:467–478, 1976Google Scholar
  4. 4.
    Akhilender Naidu K: Inhibition of monoamine oxidase by the fungicide metalaxyl. Journal of Toxicology and Environmental Health 27:395–398, 1989Google Scholar
  5. 5.
    Leung TKC, Lai JCK, Lim L: The regional distribution of monoamine oxidase activities towards different substrates: Effects in rat brain of chronic administration of manganese chloride and of ageing. J Neurochem 36:2037–2043, 1981Google Scholar
  6. 6.
    Knoll J: (−) Deprenyl — the MAO inhibitor without the cheese effect. Trends in Neurosciences 2:111–113, 1979Google Scholar
  7. 7.
    Kadir HA, Knowles CO: Inhibition of rat brain monoamine oxidase by insecticides. Gen Pharmacol 12:239–247, 1981Google Scholar
  8. 8.
    Elliot M (1977a): ‘Synthetic pyrethroids’, in Synthetic Pyrethroids (Elliot M ed.), American Chemical Society, Washington, DC. pp 1–28Google Scholar
  9. 9.
    Wouters W, Bercken JVD: Action of pyrethroids. Gen Pharmacol 9:387–398, 1978Google Scholar
  10. 10.
    Ghiasuddin SM, Soderlund DM: ‘Pyrethroid insecticides: Potent, stereospecific enhancers of mouse brain sodium channel activation’. Pestic Biochem Physiol 24:200–206, 1985Google Scholar
  11. 11.
    Eldefrawi ME, Abbassy MA, Eldefrawi AT: Effects of environmental toxicants on nicotinic acetylcholine receptors: action of pyrethroids. In: T. Narahashi (Ed.), Cellular and Molecular Neurotoxicology, Raven, New York, 1984, pp 177–189Google Scholar
  12. 12.
    Yoshii M, Tsunoo A, Narahashi T: Effects of pyrethroids and veratridine on two types of Ca channels in neuroblastoma cells. Soc Neurosci Absr 11:518, 1985Google Scholar
  13. 13.
    Casida JE, Gammon DW, Glickman AH, Lawrence LJ: Mechanisms of selective action of pyrethroid insecticides. Annu Rev Pharmacol Toxicol 23:413–438, 1983Google Scholar
  14. 14.
    Clark JM, Matsumura F: Two different types of inhibitory effects of pyrethroids on nerve Ca− and Ca+−Mg ATPase activity in the squid,Loligo Paelei, Pestic Biochem Physiol 18:180–190, 1982Google Scholar
  15. 15.
    Cole LM, Casida JE: Pyrethroid toxicology in the frog. Pestic Biochem Physiol 20:217–224, 1983Google Scholar
  16. 16.
    White INH, Verschoyle RD, Moradian MH, Barnes JM: The relationship between brain levels of cismethrin and bioresmethrin in female rats and neurotoxic effects. Pestic Biochem Physiol 6:491–500, 1976Google Scholar
  17. 17.
    Leibowitz MD, Schwarz JR, Holan G, Hille B: Electro-physiological comparison of insecticide and alkaloid agonists of Na channels. J Gen Physiol 90:75–93, 1987Google Scholar
  18. 18.
    Vijverberg PMH, Bercken JVD: Neurotoxicological effects and the mode of action of pyrethroid insecticides. CRC Critical Reviews of Toxicology 21:105–126, 1990Google Scholar
  19. 19.
    Israel Silman: Molecular structure of acetylcholinesterase TIBS 1: 225–227, 1976Google Scholar
  20. 20.
    Krajl M: A rapid microfluorimetric determination of monoamine oxidase. Biochem Pharmacol 14:1683–1685, 1965Google Scholar
  21. 21.
    Lowry OH, Rosebrough NJ, Farr AL, Randall RJ: Protein measurement with the Folin-phenol reagent. J Biol Chem 193:265–275, 1951Google Scholar
  22. 22.
    Jagannatha Rao KS:In vitro enzymatic toxicity test model validity approach. In:in vitro toxicology-approaches to validation (A. M. Goldberg (ed), No. 5, Mary Ann Liebert Inc. Publishers, New York, 1987, pp 421–451Google Scholar
  23. 23.
    Lineweaver H, Burk D: The determination of enzyme dissociation constants. J Am Chem Soc 56:658–666, 1934Google Scholar
  24. 24.
    Dixon M, Webb EC: Enzymes, 2nd Edn (Longmans Green and Co, London), 1964, p 330Google Scholar
  25. 25.
    Lehninger AL: Principles of Biochemistry, CBS Publishers and Distributors (India), 1984, pp 207–244Google Scholar

Copyright information

© Kluwer Academic Publishers 1993

Authors and Affiliations

  • Gazula Valeswara Rao
    • 1
  • K. S. Jagannatha Rao
    • 1
  1. 1.Department of Nutrition and Food SafetyCentral Food Technological Research InstituteMysoreIndia

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