A new view on an old drug: Pilocarpine

Zusammenfassung Pilocarpin ist ein geeignetes Beispiel einer parasympathischen Substanz mit dualistischer Wirkung. Auf Grund der Variationen in der Eigenaktivität (intrinsic activity) des Pilocarpins an verschiedenen Organen und Arten tritt entweder die parasympathomimetische oder die parasympatholytische Wirkung in den Vordergrund.     

A new compound effective against acute fascioliasis in sheep

Zusammenfassung 2-Acetoxy-4-chlor-3,5-dijodbenzanilid zeigte eine hohe Wirksamkeit gegen junge und gereifteF. hepatica andH. controtus in Schaften bei einer oralen Dosis von 25 und 40 mg/kg. Die gute Verträglichkeit der Verbindung in Schafen ergab sich aus Feldversuchen in Australien.     

Chemotaxis of human neutrophils against gravity: A new method

Summary A new method is described in which human neutrophils were made to migrate upward and against gravity. Thus, the possible effect of gravity on cell migration and consequent detachment of cell after migration have been eliminated.Supported in part by N.I.H. grants: No.HL19628-03, No. DE04898, No. CA24215 and No.RR05493).     

Arylpyridyl-thiosemicarbazones: A new class of anti-juvenile hormones active against Lepidoptera

Summary A new class of anti-juvenile hormone agents is described. Active anti-juvenile hormone compounds were either diazine thiosemicarbazones or aryl substituted pyridyl thiosemicarbazones, synthesized from substituted benzaldehydes. While many analogs in these classes showed feeding and growth inhibition in a variety of insects, a select group caused formation of precocious pupal characteristics inAgrotis ipsilon (black cutworm) andHeliothis virescens (tobacco budworm) and black cuticle and precocious pupae inManduca sexta (tobacco hornworm). They were active only by diet incorporation. The symptoms of precocious development could be reversed by co-administration of a juvenoid. One of the active compounds was shown to inhibit juvenile hormone biosynthesis in vitro by corpora allata of the cockroachDiploptera punctata. However, none of the compounds were active inhibitors of purified chicken liver prenyl transferase.     

o-N-diisopropylaminoethoxy-butyrophenone,a new local anaesthetic drug

Riassunto Da una serie di-fenossietilamine acilate è stata selezionata una nuova sostanza e cioè l'o-N-diisopropylaminoetossibutirrofenone, che possiede elevate proprietà anestetiche locali di superficie, per infiltrazione e tronculari. Si sono comparate le attività anestetiche e la tossicità del nuovo composto con quelle della cocaina e della procaina.     

A new group of rifamycin derivatives displaying activity against rifampicin-resistant mutants ofStaphylococcus aureus

Zusammenfassung Unter einer grossen Anzahl semi-synthetischer Rifamycinderivate wurde eine Gruppe strukturell verwandter Verbindungen gefunden, die neben ihrer hohen Wirksamkeit (MIC 0,002-0,01 g/ml) gegenüber rifampicinsensiblen, grampositiven Keimen in vitro auch eine gute Wirkung (MIC 1–10 (g/ml) gegenüber rifampicinresistenten, grampositiven Keimen aufweisen. Die Resistenzrate grampositiver rifampicinresistenter und -sensibler Keime ist bezüglich dieser Verbindungen mindestens 100mal kleiner als bei Rifampicin. Die Wirkung gegenüber resistenten Keimen scheint nicht auf einer Beeinflussung der DNA-abhängigen RNA-Polymerase zu beruhen. Eine Struktur-Wirkungs-Beziehung wird angegeben.     

A new agent for the treatment of liver fluke infection (Fascioliasis)

Zusammenfassung 3,5-Dijod-3-chlor-4-(p-chlorphenoxy) salicylanilid wird als ein neues Mittel gegen den Viehleberegel (Fasciola hepatica) beschrieben. In Schafen ergab eine Dosis von 5 mg/kg gegen geschlechtsreife Tiere und eine solche von 12,5 mg/kg gegen junge Leberegel eine hohe Wirksamkeit. Bei schwerem, akutem Leberegelbefall blieb sogar eine Dosis von 60 mg/kg ohne toxische Anzeichen. Ebenso wurde eine relativ hohe Wirksamkeit und eine gute Verträglichkeit bei der Behandlung von Leberegelinfektionen in Rindern festgestellt.     

Human specific immunoglobulin protects against infection with commonStaphylococcus in mice

Summary Mice infected with non-capsulatedStaphylococcus aureus strains highly resistant to methicillin survived after the administration of specific immunoglobulin extracted from pooled human sera by using homologous capsular type strains, but no protective effect was shown with a conventional immunoglobulin preparation and methicillin, even with high doses.     

Human specific immunoglobulin protects against infection with common Staphylococcus in mice

Mice infected with non-capsulated Staphylococcus aureus strains highly resistant to methicillin survived after the administration of specific immunoglobulin extracted from pooled human sera by using homologous capsular type strains, but no protective effect was shown with a conventional immunoglobulin preparation and methicillin, even with high doses.     

A new method of examining the stimulatory effect ofSerratia marcescens endotoxin on non-specific resistance to infection

Zusammenfassung In mit Endotoxin chronisch behandelten Ratten verändert sich die Vermehrungskurve desTrypanosoma equiperdum charakteristisch.     

Antiviral strategies against influenza virus: towards new therapeutic approaches

Influenza viruses are major human pathogens responsible for respiratory diseases affecting millions of people worldwide and characterized by high morbidity and significant mortality. Influenza infections can be controlled by vaccination and antiviral drugs. However, vaccines need annual updating and give limited protection. Only two classes of drugs are currently approved for the treatment of influenza: M2 ion channel blockers and neuraminidase inhibitors. However, they are often associated with limited efficacy and adverse side effects. In addition, the currently available drugs suffer from rapid and extensive emergence of drug resistance. All this highlights the urgent need for developing new antiviral strategies with novel mechanisms of action and with reduced drug resistance potential. Several new classes of antiviral agents targeting viral replication mechanisms or cellular proteins/processes are under development. This review gives an overview of novel strategies targeting the virus and/or the host cell for counteracting influenza virus infection.     

Administration of the antitumor drug mitoguazone protects normal thymocytes against spontaneous and etoposide-induced apoptosis

The suggestion has been made that polyamines may be involved in the control of cell death, since exceedingly high or low levels induce apoptosis in different cell systems. For a deeper insight into the relationship between apoptosis and polyamine metabolism, we investigated in vitro the effect on rat thymocytes of mitoguazone (MGBG, which inhibits S-adenosylmethionine decarboxylase, i.e. a key enzyme in the polyamine biosynthetic pathway). Thymocytes were selected as an especially suitable model system, since they undergo spontaneous apoptosis in vivo and can be easily induced to apoptose in vitro by etoposide, used here as an apoptogenic agent. MGBG protected thymocytes from both spontaneous and drug-induced apoptosis, and this protective effect was associated with a decrease in polyamine oxidase activity and total polyamine levels.Received 7 July 2004; received after revision 2 September 2004; accepted 9 September 2004     

Evaluation of oral vaccination against mouse-typhoid in a new animal model

Summary In a simple, new animal model the spread of mouse-typhoid within a mouse-colony was studied and oral vaccination against this disease was evaluated. Live vaccine was superior to inactivated vaccine.     

Cytoprotective effects of acidosis via heat shock protein HSP27 against the anticancer drug doxorubicin

Drug resistance continues to be a stumbling block in achieving better cure rates in several cancers. Doxorubicin is commonly used in treatment of a wide range of cancers. The aim of this study was to look into the mechanisms of how low ambient pH may contribute to down-regulation of apoptotic pathways in a gastric tumour cell line. Low pH culture conditions were found to dramatically prolong cell survival after doxorubicin treatment, an effect that was in part reversed by co-incubation with the specific p38 mitoge-activated protein kinase (MAP kinase) inhibitor SB203580, only mildly inhibited by blockade of the multi-drug resistance 1 (MDR1) transporter, but completely abolished by siRNA-mediated knockdown of the heat shock protein 27 (HSP27). In conclusion, acidic pH causes less accumulation of cytotoxic drug in the nucleus of adeno gastric carcinoma (AGS) cells and HSP27-dependent decrease in FasR-mediated gastric epithelial tumour cell apoptosis.     

A new guanidine alkaloid

Zusammenfassung Ein neues Alkaloid, Pterogynin, wurde aus der Rinde vonPterogyne nitens Tul. (Leguminosae) isoliert und seine Struktur bestimmt. Es handelt sich um das N,N-Di(isopenten-2-yl)-guanidin.

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Part XIV ofStudies on Plants; proceding part, R. A.Corral, O. O.Orazi and I. A.Benages, Tetrahedron Letters545 (1968).     

A new air sampler

Zusammenfassung Beschreibung eines verbesserten Luftprobensammlers zur Bestimmung von Keimzahlen in der Luft.