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INTERACTION OF SOME ORGANOPHOSPHORUS COMPOUNDS IN SUSCEPTIBLE AND RESISTANT HOUSEFLIES (MUSCA DOMESTICA L.) M. D. ABDALLAH inobou school IN08201,353 INTERACTION OF SOME ORGANOPHOSPHOROUS COMPOUNDS IN SUSCEPTIBLE AND RESISTANT HOUSEFLIES (MUSCA DOMESTICA L.) THESIS SUBMITTED IN PARTIAL FULFILMENT OF THE REQUIREMENTS FOR THE DEGREE OF DOCTOR OF AGRICULTURAL SCIENCES AT THE AGRICULTURAL UNIVERSITY OF WAGENINGEN, THE NETHERLANDS, ON FRIDAY OCTOBER 4TH 1963 AT 4 P.M. BY M. D. ABDALLAH B. Sc. Cairo University Ir. Wageningen University H. VEENMAN EN ZONEN N.V. - WAGENINGEN - 1963 THEOREMS I Although the hypothesis that the toxic effect of parathion is due to the production of the oxygen analogue paraoxon seems reasonable, it fails to ex­ plain many observations satisfactorily. II The presence of high levels of resistance as tested byinjection , comparable to those found by topical application, does not necessarily mean that the cuticlei sho t a site of resistance factors. HI A contradiction existsi n the conception ofa simultaneous positive action of the hormone ecdyson onth e processes ofmoultin g and of growth and develop­ ment of insect larvae. IV It is uncertain whether 2-methyl-4-bromopyrimidine is an intermediate in the reaction of 2,6-dibromopyridine with potassium amide in liquid ammonia to yield 2-methyl-4-aminopyrimidine. H. J. DEN HERTOG. Abstr. A, 19th Intern. Congr. Pure Appl. Chem. p. 279 (A 5 - 133, 1963). The 9-oxodec-2-enoic acid produced by the queens of honey bees is not necessary functioning per se, but may be transformed into a more volatile compound which subsequently exerts the effect. VI In searching for compounds with a therapeutic effect on plant viruses, it is necessary to study their action on the growth and development of the plant in addition to their inhibitory activity against virus multiplication. VII An administrative reform as planned aiming at the introduction of local government officials andtraine dpersonne lfo r thesocia lservice si nth eEgyptia n villages will be confronted with the problem of the creation of the basiccondi ­ tions for this change. VIII The successful introduction of the blue green algae in irrigated rice fields islimite d to a few countries. IX Both Dutch and Egyptian housewives should beenable d to bemor e engaged in professional or social activities. M. D. ABDALLAH Wageningen,oktobe r 1963 VOORWOORD Nu ik het grote genoegen smaak mijn vijf-jarig studieverblijf in Ncderland met de voltooiing van dit proefschrift af te sluiten, wil ik gaarne de gelegen- heid gebruiken om opdez cplaat s alien tebedanke n dieerto e hebben bijgedra- genda tdez ejare n bijmi ji ndankbar e herinncringzulle n voortleven. Veel ben ik verschuldigd aan mijn promotor, Prof. Dr. J. on WILDE, voor diens lciding, waardcvollc suggesties en stimulcrcndc kritick. Ecn woord van speciale waardering zij gcricht tot Prof. Dr. H.J . DF.N HER- TOO en Prof. Dr.A .J . P.OOR Tvoo r nun goedezorgen . Mijn dank gaat vcrdcr uit naar de wctcnschappclijkc staf van het Labora- torium voor Entomologic, in het bijzondcr naar Dr. D. STEGWEEdi evoortdu - rend van zijn bclangstclling inmij n ondcrzoek blijk gafe n mijsteed s met raad terzijde stond. Zonder zijn hulpe nsteu n zoudi tproefschrif t niet tot stand zijn gekomen. Wat hetpersonee l vanhe t Laboratorium betreft, wil ikhie r mijn erkcntelijk- heid met name nogbetuige n aan Mcjuflrouw F.T . MENSINK voor haar hulp bij de chemische analyses, aan Mejuffrouw F. J. E. VAN REMMEN en de Heer T. VAN DER LAAN voor hungoed e zorgen bijhe t kweken vand cproefdicre n en aan deHee r A. H, GERRITSEN voor zijn technische assistcntic. Dankbaar beni k ookvoo r desteu n die ikbi jd eaanvan gva nmij n studieva n het ..International Agricultural Centre" heb mogen ontvangen. Het ishee l moeilijk onder woorden tebrenge n watvoo r mijhe t contactme t de vele Wageningse vrienden betekend hecft. Velen van hen lecrde ik in dc ..International Club" kennen. Zonder henzo umij n geest zich nimmcr zo aan- zienlijk in verschillende richtingen hebben kunnen verruimen. Overdmk 648.7:595.772.4 MEDEDELINGEN VAN DE LANDBOTJWHOGESCHOOL TE WAGENINGEN, NEDERLAND 63 (11) 1-97 (1963) INTERACTION OF SOME ORGANOPHOSPHORUS COMPOUNDS IN SUSCEPTIBLE AND RESISTANT HOUSEFLIES (MUSCA DOMESTICA L.) (met een samenvatting in het Nederlands) by/door M.D .ABDALLA H Communication 94, Laboratory of Entomology, Agricultural University, Wageningen, Netherlands (Received/Ontvangen 9.7.'63) CONTENTS GENERAL INTRODUCTION 3 MATERIALS AND METHODS 5 A. Strains of houseflies 5 B. Rearing of houseflies 5 C. Organophosphorus compounds used 6 D. Testing method 6 E. Measurements of cholinesterase and aliesterase activity 7 CHAPTER I. THE EFFECTO F TOCP UPON THE TOXICITYO F PARATHIONAN D PARAOXON.. 7 1.1. Introduction and reviewo f literature 7 1.2. Results and discussion 8 1.3. The relative toxicity of parathion and analogues 15 CHAPTER II. THE SIGNIFICANCE OF THORAX CHOLINESTERASE IN ORGANOPHOSPHORUS POISONING; THESYNERGISTI CAN DANTAGONISTI CEFFECT SO FTOC P IN TERMSO F ChE AND AliE INHIBITION 18 II.1 . Introduction and review of literature 18 II.2. Results and discussion 20 11.2.1. The invivo effect of TOCP on ChE and AliE activities 20 11.2.2. ChE and AliE measurements after parathion and paraoxon poisoning... 20 11.2.3. The significance of housefly brain ChE inhibition after poisoning 25 11.2.4. The joint action of TOCP and organophosphorus insecticides 26 11.2.5. Injection experiments 31 11.2.6.Th e number of aliesterases in the susceptible flies. 37 CHAPTER III. THE RELATION BETWEEN PENETRATION THROUGH THE CUTICLE AND THE LATENT PERIODI N PARATHIONPOISONING ;MECHANISM S OF SYNERGISM 38 III.1 . Introduction and review of literature 38 III.2. Results and discussion 39 Meded. Landbouwhogeschool, Wageningen 63 (II), 1-97 (1963) 1 111.2.1. Toxicity data 39 111.2.2. ChE and AliE measurements 42 111.2.3. Injection experiments 44 111.2.4. The concept ofth e "holding capacity" 48 111.2.5. The "opportunity factor" concept 50 III.3. Mechanisms ofsynergis m 51 111.3.1. Inhibition of ChE 51 111.3.2. Inhibition ofdetoxicatio n mechanisms 51 111.3.3. Sites oflos s . 53 CHAPTER IV. EXPERIMENTS WITH A RESISTANT STRAIN 56 IV.l. Introduction 56 IV.2. Review ofliteratur e . 56 IV.3. Results and discussion 57 IV.3.1. Degree ofresistanc e 57 IV.3.2. Levels and relative susceptibilities ofCh E and AliE 57 IV.3.3. The effect ofTOC P 57 IV.3.4. The effect oftopicall y applied parathion and paraoxon 59 IV.3.5. The joint action ofTOC P and parathion orparaoxo n 61 IV.3.6. Resistance levels after injection 64 IV.3.7. Discussion 66 IV.3.7.1. Reduced penetration as a factor inresistanc e 66 IV.3.7.2. Methods ofstudyin g penetration 67 IV.3.7.3. The relation between the nature of the injection vehicle and the levelo f resistance 68 IV.3.7.4. The possible relation between the gut and resistance 69 CHAPTER V. THE in vitro INHIBITION OF ChE AND AliE ACTIVITY BY PARATHION AND PARA­ OXON IN SUSCEPTIBLE AND RESISTANT HOUSEFLIES 70 V.l. Introduction 70 V.2. Results and discussion 70 CHAPTER VI. PERTINENCE OF SOME OBSERVATIONS TO THE HYPOTHESIS OF THE ROLE OF THE OXYGEN ANALOGUE IN PARATHION POISONING 73 VI.l. Introduction 73 VI.2. Review of literature 73 VI.3. Discussion 74 VI.3.1. The LZ>60value s ofparathio n and paraoxon 74 VI.3.1.1. Stability tohydrolysi s 74 VI.3.1.2. Liposolubility '.'.'.'.'.'.'.'.'.'. 15 VI.3.2. Oxidation ofparathio n ininsec t tissues 78 VI.3.3. The slow toxic action ofparathio n 79 VI.3.4. The strong in vivo ChE inhibition produced by parathion ........ 80 GENERAL DISCUSSION 80 A. Antagonism gg B. Penetration and permeability 80 C. Enhanced rate of detoxication of organophosphorus insecticides as afacto r in resistance 03 SUMMARY 85 ACKNOWLEDGEMENTS g8 SAMENVATTING go REFERENCES Q1 Meded. Landbouwhogeschool, Wageningen 63 (11), 1-97 (1963) GENERAL INTRODUCTION The first demonstrations of the potency of organophosphorus compounds to inhibit mammalian cholinesterase (ChE), were apparently those of ADRIAN, FELDBERG and KILBY (1941), and DIXON, MACKWORTH and WEBB (1942). In insects, abundant evidence for the powerful inhibitory properties of the insecticidal organophosphorus compounds or their metabolites against ChE and Aliesterases (AliE) have been reported at a much later date (CHADWICK and HILL 1947; METCALF and MARCH 1949). Since the function of the latter esterases in the normal physiology of the organism is so far unknown, little can be said about the significance of their inhibition in relation to organophos­ phorus poisoning. The inhibition of ChE, on the other hand, has most dramatic physiological consequences. The reason why these compounds specifically inhibit cholinesterases and other hydrolytic enzymes has been explained by BARNES (1954). ChE hydrolyses these toxic phosphorus esters,jus t as it does with its natural substrate acetyl­ choline (ACh). After hydrolysis, however, the phosphate group remains com­ bined with the "esteratic site" of ChE, thus preventing the hydrolytic action of the enzyme upon its natural substrate. This process is called phosphorylation by analogy with acetylation by ACh. The affinity of the free enzyme for its natural substrate is greater than that for the toxic phosphorus ester. This property had led VAN ASPEREN (1957,1958)t o develop the "substrate protection technique" in determining the in vivo inhibition of ChE in intoxicated insects, by adding ACh to the homogenizing medium, and thus preventing the free inhibitor, if present, from coming into contact with the enzyme during and after homogenization. There is no doubt that a major biochemical lesion in insects exposed to lethal doses of organophosphorus compounds is the inhibition of ChE, leading to accumulation of ACh in conductive tissues, and subsequent malfunction of conductive processes (SMALLMAN and FISHER 1958; SMALLMAN 1956; COLHOUN 1959; METCALF 1959; WINTERINGHAM and LEWIS 1959).

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