Comparative evaluation of 7 helminth antigens in the enzyme-linked immunosorbent assay (E.L.I.S.A.).

112 sera from Europeans with parasitologically proven helminthiasis were tested in the enzyme-linked immunosorbent assay (E.L.I.S.A.) against 6 crude extracts of various helminths (2 of adult worms: Dipetalonema viteae, Fasciola hepatica; 3 of eggs: Ascaris suum, Toxocara canis, Schistosoma mansoni; and of Echinococcus granulosus scolices) and against bovine hydatid fluid. Each serum was tested simultaneously at a fixed dilution of 1:160 against all antigens. Extensive cross-reactions were observed, leading to the conclusion that non-purified helminth antigens, even in combination, are of limited value for reliable serodiagnosis in E.L.I.S.A.     

Antimicrobial activity of carbazole derivatives

Summary Glycozoline and girinimbine isomers (IV andVII) were synthesized and their activity against 2 bacterial strains, viz.E. coli andS. aureus, and 2 fungal strains, viz.C. albicans andA. niger were studied. The hydroxy synthons (III) were also tested. The authors are thankful to Dr B.N. Apte, Association of Microbiologists of India, Bombay Unit, for providing some of the organisms, to Prof. A.K. De, Indian Institute of Technology, for financial assistance, to Prof. G. D. Shah, Department of Chemistry, Indian Institute of Technology for guidance, encouragement and helpful discussions.     

Biological activity of enantiomerically pure forms of insect juvenile hormone I and III inBombyx mori

Summary Biological activity of enantiomerically pure juvenile hormones was assayed by topical application on allatectomizedBombyx fourth instar larvae. JHs tested were (10R)-JH I [methyl (2E,6E,10R,11S)-10,11-epoxy-3,11-dimethyl-7-ethyl-2,6-tridecadienoate], (10S)-JH I [methyl (2E, 6E, 10S, 11R)-10,11-epoxy-3,11-dimethyl-7-ethyl-2,6-tridecadienoate], (10R)-JH III [methyl (2E,6E,10R)-10,11-epoxy-3,7,11-trimethyl-2,6-dodecadienoate] and (10S)-JH III [methyl (2E,6E,10S)-10,11-epoxy-3,7,11-trimethyl-2,6-dodecadienoate]. Among these compounds, natural (10R)-JH I was most active and the dose needed to induce 50% larval molting was 0.04 g/larva; it was approximately 12,000 times more active than unnatural (10S)-JH I. Though natural (10R)-JH III showed slight biological activity, it was only one three-thousandth of that of (10R)-JH I. Unnatural (10S)-JH III exhibited no biological activity at the levels assayed.     

The infectivity of polyhedra of nuclear polyhedrosis virus (N.P.V.) after passage through gut of an insectpredator

Summary Polyhedral inclusion bodies (P.I.B.) of a nuclear polyhedrosis virus ofHeliothis punctigera (Lep.) were found in excreta ofNabis tasmanicus (Het.), a predator ofH. punctigera. An immunofluorescent counting method was used to estimate numbers of P.I.B. Bioassays demonstrated that no loss of infectivity occurred during passage through the gut.Acknowledgment. I am grateful for the comments and criticism offered by Dr D.E. Pinnock, I thank D.J. Cooper for preparation of materials for the immunofluorescent counting method and J. Hardy for supplying me with eggs ofH. punctigera; all of Department of Entomology, Waite Agricultural Research Institute, Glen Osmond, South Australia.     

New route for 1-substituted hydantoins

Zusammenfassung 1,3-unsubstituierte Hydantoine (I) werden in einem 3-Stufenprozess in 1-substituierte Abkömmlinge (IV) übergeführt: Blockierung der Stellung 3 durch Aminomethylierung, gefolgt von N₁-Alkylierung mit anschliessender Entfernung der Schutzgruppe durch Hydrolyse.

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This paper represents Part V of the seriesSubstitution in the Hydantoin Ring; preceding Part,L. Trippetta, O. O. Orazi, andR. A. Corral, An. Asoc. quím. argent., in press.     

Muelleromyces,a new member of the sphaeriales (ascomycetes)

Zusammenfassung Ein auf Blättern vonEugenia jambolana Lam. in Indien Blattflecken verursachender Ascomycet gehört zu einer neuen Gattung,Muelleromyces Kamat undAnahosur; Typus istMuelleromyces indicus Kamat undAnahosur. Der Pilz hat dem Blattgewebe eingesenkte, einzelstehende und von einem mächtig entwickelten Klypeus überdeckte Perithecien, verschleimende Asci und ungleich zweizellige, hyaline Ascosporen; Paraphysen fehlen.

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The fungus is named after Dr.E. Müller of The Institute of Special Botany, Zürich (Switzerland), in recognition of his outstanding contributions to Fungi in general and Ascomycetes in particular. The material of this new fungus is deposited at M.A.C.S. Herb. Poona (India), C.M.I., Kew, Surrey (England) and Herb. Orientalis, New Delhi (India).     

Astragalin ausPodophyllum peltatum L. undP. emodi Wall.

Summary A yellow flavonoid pigment, which occurs as a companion of the lignan glycosides inPodophyllum peltatum L. andP. emodi Wall. has been identified as astragalin (=kaempferol-3-glucoside).

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18. Mitt. über mitoschemmende Naturstoffe. 17. Mitt.:E. Schreier, Helv. chim. Acta47, 1529 (1964).     

Development of DNA probes for cytotoxin and enterotoxin genes in enteric bacteria

Summary DNA probes to identify the genes encoding toxins in enteric bacteria have been developed. Use of these probes reduces the number of animals required for toxicity testing, as suspect bacteria can be directly tested for the presence of toxin. We have augmented the gene probes available by developing probes against theEscherichia coli enterotoxin LTII and shiga toxin fromShigella dysenteriae 1.The LTII gene fromE. coli 357900 was identified and characterised and a suitable internal probe was obtained. The LTII gene was found not to be common among enterobacteriae from various geographical locations. Isolates predominately of animal origin from Nigeria and Thailand hybridized with the probe.The shiga toxin gene was isolated fromS. dysenteriae 1 by a combination of in vivo and in vitro methods. An internal probe was identified and used against different serogroups ofShigella andE. coli isolated. The probe was found to hybridize withS. dysenteriae 1 isolates and also someS. flexneri andS. sonnei strains. Representatives were tested for toxin production and found to produce toxin at low levels.     

Reduction in bean common mosaic virus (BCMV) infectivity vis-a-vis crude leaf extract of some higher plants

Summary Crude leaf extracts of 17 plants were tested for their antiviral activity against BCMV. An extract ofAzadirachta indica A. Juss. was found to be most potent in reducing the infectivity of the virus.Authors are thankful to Dr R. D. Joshi for his valuable guidance and Prof. S. N. Mathur for providing lab facilities. Financial assistance by U. G. C. and C. S. I. R. is gratefully acknowledged.     

Experimental immunity against trypanosomiasis

Summary 9 groups of 6 female rats were used in an experiment using fraction 3 ofTrypanosoma rhodesiense. 500 g gave 100% immunoprotection and 1000 and 1500 g gave 66% immunoprotection when challenged with 5×10² T. brucei. 2 groups of 10 female rats were tested for a short period inoculation immune response. In this, 750 g of fraction 3 ofT. rhodesiense gave 70% immunoprotection when challenged withT. brucei.I thank the University of Zambia for support; Dr M. A. Q. Awan, Mazabuka, Zambia, forT. rhodesiense andT. brucei; Prof. J. W. Kibukamusoke, Dr O. Okong'o and Dr W. W. Anokbonggo for advice; Mr L. Nyaliti for technical help.     

über Peptidsynthesen,XLVI. Synthese kininliefernder Kininogensequenzen

Summary H-Met-Lys-bradykinin-Ser-Val-Gln-OH and H-Met-Lys-bradykinin- Ser-Val-Gin-Val-OH, sequences of bovine serum kininogen have been synthetized by different approaches. The natural and synthetic peptides were tested for their kinin liberating potency.

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XLV. Mitt.: E.Klieger, Justus Liebigs Ann. Chem.,724, 204 (1969).     

Antihypertensive agents III. Synthesis and antihypertensive activity of 3-[4-(p-fluoro-phenyl)-1,2,3,6-tetrahydro-1-pyridyl]-1-[1-(2-hydroxyethyl)-5-methyl-4-pyrazolyl]-1-propanone

Zusammenfassung 3-[4-(p-Fluorphenyl)-1,2,3,6-te-trahydro-1-pyridyl]-1-[1-(2-hydroxyaethyl)-5-methyl-4-pyrazolyl]-1-propanon (I, CIBA 4416/B-Go) senkt bei normotonischen und hypertonischen Tieren den Blutdruck. Die Drucksenkung kann hauptsächlich auf die periphere Vasodilatation sowie auf die Vasomotorenzentren bezogen werden. Ausserdem wirkt CIBA 4416/B-Go adrenolytisch.

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Previous paper:V. P. Arya, R. S. Grewal, C. L. Kaul, S. P. Ghate, D. V. Mehta andT. George, J. Pharm. Sci.58, 432 (1969).Contribution No. 243 from CIBA Research Centre.     

Alkaloid studies XXVI. The constitution of pyrifolidine

Zusammenfassung Die Struktur desAspidosperma-Alkaloids Pyrifolidin (I) wird durch Protonresonanz und durch Vergleich mit Aspidospermin und Aspidocarpin bewiesen. Dieses Alkaloid ist in seiner absoluten Konfiguration ein Antipode des Aspidospermins.

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Paper XXV,C. Djerassi, A. A. P. G. Archer, T. George, B. Gilbert, J. N. Shoolery, andL. F. Johnson, Exper.16, 532 (1960).

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Acknowledgement. Financial support has been provided by grant H-5048 of the National Heart Institute, National Institutes of Health (U.S. Public Health Service), and by the Conselho Nacional de Pesquisas (Brazil). The postdoctorate research fellowship ofB. Gilbert in Rio de Janeiro was financed from a grant of the Rockefeller Foundation in support of a collaborative research program between Stanford University and the Instituto de Quimica Agricola, Rio de Janeiro (Brazil).     

Kelletinin I and kelletinin A from the marine molluscBuccinulum corneum are inhibitors of eukaryotic DNA polymeraseα

Summary The inhibitory effect of esters of p-hydroxybenzoic acid (kelletinins I and A), extracted from the marine gastropodBuccinulum corneum, have been tested on eukaryotic and prokaryotic enzymes of DNA metabolism such as DNA polymerases and , DNA polymerase I, Exo III, pancreatic DNAse I, micrococcal DNAse andE. coli RNA polymerase. Kelletinin I and kelletinin A inhibit preferentially DNA polymerase. The inhibitory effect of kelletinin I involves the hydroxyl group of p-hydroxybenzoic acid.     

Antiparasitic agents. 4. Injectable phenylguanidine anthelmintics

Summary A series of phenylguanidine anthelminties has been discovered to be active by injection against nematode and trematode species.For the previous paper in this series, see R. D. Haugwitz, B. V. Maurer, G. A. Jacobs, V. L. Narayanan, L. R. Cruthers and J. Szanto, J. med. Chem.22, 1113 (1979).     

A comparison of cycloartenol and lanosterol biosynthesis and metabolism by the Oomycetes

Summary Representative members in each of the four orders of Oomycetes (Phytophthora cactorum, Peronosporales;Lagenidium callinectes, L. giganteum, Lagenidiales;Saprolegnia ferax, Saprolegniales;Apodachylella completa, Leptomitales) have been examined for their ability to synthesize and polycyclize squalene-oxide (SO) to a tetracyclic product and to differentiate between cycloartenol and lanosterol metabolism to sterols.P. cactorum andL. giganteum failed to synthesize or metabolize SO, cycloartenol or lanosterol. While the other three fungi synthesized sterols via SO and lanosterol, a minor metabolism of added cycloartenol to the 4,4-desmethyl-14-methylcyclosteroid dehydropollinastanol was observed.Acknowledgment.Saprolegnia ferax-ATCC 3605 (1),Lagenidium callinectes ATCC 24973 (2),Apodachlyella completa (3) were obtained from Dr J. Aronson, Arizona State Univ. (3),Lagenidium gigateum was obtained from a drainage ditch in California (4), andPhytophthora cactorum was obtained from the U.C. Berkeley Fungal Collection (5). The fungi were cultured as previously described: Cultures 1,2,3: Berg, L. B., Ph. D. dissertation, Univ. of MD., College Park (1983); culture 4: Kerwin, J.L., and Washino, R.K., Exp. Mycol.7 (1983) 109; culture 5: Nes, W.D., and Stafford, A.E., Lipids19 (1984) 544. Preliminary observations involving the labeled substrates were presented by Le, P.H., Nes, W.D., and Parish, E.J. J. Am. Oil Chem. Soc.62 (1985) 655(A). Please address all correspondence to W.D. Nes, Plant Physiology and Chemistry Research Unit, ARS-US Dept of Agriculture, Berkeley, CA 94710, USA.     

Volatile metabolites of aspergilli in relation to spore germination of some keratinophilic fungi

Summary The effect of volatile metabolites produced by 8 Aspergilli (i.e.,Aspergillus candidus, A. chevalieri, A. flavus, A. fumigatus, A. nidulans, A. niger, A. ochraceous andA. tamarii) on spore germination were tested againstAuxarthron conjugatum, Chrysosporium pannicola, Keratinomyces ajelloi andMicrosporum gypseum. The volatile metabolites inhibited the spore germination of all the test fungi.Acknowledgment. The authors thank Professor G.P. Mishra for the use of the facilities and S.K.D. acknowledges the fellowship award by I.C.M.R. New Delhi.     

Mass spectrometry in structural and stereochemical problems spegazzinine and spegazzinidine

Zusammenfassung Auf Grund von Protonresonanz und massenspektrometrischen Messungen werden die Strukturen III und VII für die Aspidosperma-Alkaloide Spegazzinidin und Spegazzinin vorgeschlagen.

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This paper represents part III. For preceding paper seeB. Gilbert, J. Ferreira, R. J. Owellen, C. E. Swanholm, H. Budzikiewicz, L. J. Durham, andC. Djerassi, Tetrahedron Letters,1962, 59.

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This paper represents Part VI in the La Plata seriesEstudios sobre Plantas; for paper V seeT. Nakano, C. Djerassi, R. A. Corral, andO. O. Orazi, J. org. Chem.26, 1184 (1961).     

Legionella pneumophila down-regulates MHC class I expression of human monocytic host cells and thereby inhibits T cell activation

Legionella (L.) pneumophila, the causative agent of Legionnaires disease, is an intracellular pathogen of alveolar macrophages that resides in a compartment displaying features of endoplasmatic reticulum (ER). In this study, we show that intracellular multiplication of L. pneumophila results in a remarkable decrease in MHC class I expression by the infected monocytes. During intracellular multiplication, L. pneumophila absorbs ER-resident chaperons such as calnexin and BiP, molecules that are required for the correct formation of the MHC class I complex. Due to reduced MHC class I expression, stimulation of allogeneic blood mononuclear cells was severely inhibited by infected host cells but cytotoxicity of autologous natural killer cells against Legionella-infected monocytes was not enhanced. Thus, reduced expression of MHC class I in infected monocytes may resemble a new immune escape mechanism induced by L. pneumophila.Received 22 November 2004; received after revision 27 December 2004; accepted 5 January 2005     

Alkaloids ofConoclinium coelestinum (L.) DC.,Eupatorium compositifolium walt., andE. altissimum L.: Isolation of crystalline intermedine fromC. coelestinum

Summary The isolation of crystalline intermedine fromConoclinium, coelestinum (L.) DC., notmixed with the diastereoisomeric congener base lycopsamine, is reported.E. compositifolium Walt. yielded the usual mixture of intermedine and lycopsamine; fromE. altissimum L. rinderine and 7-angelylheliotridine have been isolated.