Potentiation of antifungal activity of sesquiterpene dialdehydes against Candida albicans and two other fungi.

The antifungal activity of two drimane sesquiterpene dialdehydes, polygodial (1) and warburganal (2), alone and in combination with several other substances, was examined against three fungi, Candida albicans, Saccharomyces cerevisiae and Pityrosporum ovale employing a broth dilution method. Anethole significantly synergized the activity of the two sesquiterpenoids against C. albicans and S. cerevisiae; however, it had only an additive effect against P. ovale. By contrast, two antioxidants, ascorbic acid (vitamin C) and BHA (butylated hydroxyanisole), noticeably enhanced the activity of the sesquiterpenoids against P. ovale, but had no effect against C. albicans and S. cerevisiae.     

Activation of stress signalling pathways enhances tolerance of fungi to chemical fungicides and antifungal proteins

Fungal disease is an increasing problem in both agriculture and human health. Treatment of human fungal disease involves the use of chemical fungicides, which generally target the integrity of the fungal plasma membrane or cell wall. Chemical fungicides used for the treatment of plant disease, have more diverse mechanisms of action including inhibition of sterol biosynthesis, microtubule assembly and the mitochondrial respiratory chain. However, these treatments have limitations, including toxicity and the emergence of resistance. This has led to increased interest in the use of antimicrobial peptides for the treatment of fungal disease in both plants and humans. Antimicrobial peptides are a diverse group of molecules with differing mechanisms of action, many of which remain poorly understood. Furthermore, it is becoming increasingly apparent that stress response pathways are involved in the tolerance of fungi to both chemical fungicides and antimicrobial peptides. These signalling pathways such as the cell wall integrity and high-osmolarity glycerol pathway are triggered by stimuli, such as cell wall instability, changes in osmolarity and production of reactive oxygen species. Here we review stress signalling induced by treatment of fungi with chemical fungicides and antifungal peptides. Study of these pathways gives insight into how these molecules exert their antifungal effect and also into the mechanisms used by fungi to tolerate sub-lethal treatment by these molecules. Inactivation of stress response pathways represents a potential method of increasing the efficacy of antifungal molecules.     

On the antitumour activity of some poducts of wood-decaying fungi

Zusammenfassung Die Versuchsergebnisse über die antitumoröse Aktivität einiger holzzerstörender Pilze (Lösung des roten Pigmentes nachSchánl ⁴) wurde beschrieben. Das Überleben von Mäusen mit implantiertem Ehrlich'schem Karzinom ist statistisch in der Gruppe der behandelten Tiere in 5% gesichert. Histologisch ist es bei länger behandelten und überlebenden Tieren zum Verschwinden des karzinomatösen Charakters gekommen, und an seiner Stelle bildete sich ein pleiomorföses Sarkom.     

A medium to demonstrate the ligninolytic activity of some fungi

Zusammenfassung Es wird hier eine neue Methode angeführt, um die holzauflösende Fähigkeit einiger Pilze zu bestimmen. Ein milchiges, homogenes Agarmedium wird hergestellt, indem man kugelgemahlenes Buchensägemehl als hauptsächliche Kohlenstoffquelle benutzt. Wenn man in dieses Medium bestimmte holzzerstörende Pilze einpflanzt, wird sowohl ihre holzspaltende als auch ihre zellulosezerstörende Wirkung dadurch gezeigt, dass das Medium unter dem Wurzelgeflecht sich aufklärt.     

ATPase activity of two rabbit laryngeal muscles

Zusammenfassung Die Myofibrillen- und Myosin-ATPase-Aktivität des schnellen «roten» M. thyroarytenoideus von Kaninchen ist höher als die ATPase-Aktivität des «weissen» M. extensor digitorum longus und wesentlich höher als die ATPase-Aktivität des «roten» M. soleus. Daraus folgt, dass in Abhängigkeit besonderer funktioneller Ansprüche auch rote Muskeln schnell sein können.     

Total synthesis of two cyclodecapeptides exerting polymyxin-like activity

Zusammenfassung Von den vier Cyclodekapeptiden, die als mögliche Strukturen für Polymyxin B₁ vorgeschlagen wurden, konnten nun auch die Ringstrukturen mit 7 Aminosäuren, nämlich 7 und 7 (vgl. Fig.), synthetisiert werden. Diese erwiesen sich im Gegensatz zu 8 und 8 als hochaktive antimikrobielle Wirkstoffe mit Wirkungsqualitäten der Polymyxine. Ob 7 oder 7 mit natürlichem Polymyxin B₁ identisch ist, wird durch weitere Versuche abgeklärt.     

Potentiation of histamine and inhibition of diamine oxidase by mescaline

Zusammenfassung Anhand zweier Versuchsanordnungen wird gezeigt, dass Meskalin Histaminwirkungen verstärken kann. Ausserdem vermag es die Histamin zerstörende Wirkung der Diaminooxydase zu hemmen (in 10^–5-molarer Konzentration).Es wird die Möglichkeit diskutiert, dass diese Eigenschaften mit der 4-Methoxyphenyl-äthylamin-Struktur des Meskalins in Zusammenhang stehen könnten.     

Potentiation of ethanol narcosis by dopamine- and l-DOPA-based isoquinolines.

The isoquinolines, salsolinol and 3-carboxysalsolinol, prolong ethanol-induced narcosis in mice. Pretreatment with carbidopa increases the effect of 3-carboxysalsolinol but not of salsolinol. These results suggest that ethanol sleeping-time potentiation by l-LOPA may involve a partial conversion to the isoquinoline in vivo. A central depressant action of salsolinol or the 3-carboxy analogue is suggested.     

Relevance of chlorine-substituent for the antifungal activity of syringomycin and syringotoxin,metabolites of the phytopathogenic bacteriumPseudomonas syringae pv.syringae

Structural analogues of syringomycin and syringotoxin were produced by fermentation, characterized by FAB-MS and amino acid analysis and compared to the parent compounds in the antibiosis test againstRhodotorula pilimanae. The C-terminal residue was shown to be important for the activity.     

Modification of clonazepam anticonvulsive activity by its association with other anti-epileptic drugs

Summary The modification of the anti-epileptic activity of clonazepam by other anticonvulsivants is studied. The results vary according to the drug and technique used. The usefulness of the 2 techniques employed is discussed.     

Inhibition of cyclic 3′, 5′-nucleotide phosphodiesterase activity by diuretics and other agents

Résumé Différent composés organo-mercuriels ainsi que l'acide éthacrinique inhibent les phosphodiestérases de l'AMP cyclique, du cur de cobaye, de buf et de rat, des plaquettes de rat et de l'homme ainsi que du cerveau de rat.     

In vitro effects of melanocytolytic agents and other compounds upon dominant human melanoma tyrosinase activity

Summary The activity of dominant human melanoma tyrosinase isozyme was greatly decreased by certain reducing agents. The number and geometry of phenolic groups as well as free-SH group appear important for enzymic inhibition.This investigation was supported by U.S. Public Health Service Research Grant No. CA-12731-02 and CA-15991-01 from National Cancer Institute.     

Potentiation of immunologic memory by Corynebacterium parvum and its mechanism]

Immune response to bovine serum albumin (BSA) at dose of 2,50 mg/kg which is rather a weak immunogen in Rabbits, when given intravenous was highly potentiated when the animals received a previous single intravenous infection of 2 mg/kg of C. parvum, followed by subsequent BSA anamnestic challenges for several months. Thus, the antibody amounts synthesized following the 1st anamnestic injection (3 weeks) were 0,260 mg/ml in the control versus, 0,800 mg/ml in the C. parvum pretreated groups; following the 2nd anamnestic challenge (12 weeks afterwards) 1 mg/ml in the control versus, 2,50 mg/ml in the treated groups following the 3rd anamnestic challenge (28 weeks afterwards) 1,3 mg/ml in the control versus 5 mg/ml in the C. parvum pretreated groups; following the 4th anamnestic challenge (52 weeks afterwards) 0,300 mg/ml in the control versus 0,800 mg/ml in the C. parvum treated groups. On the whole for the four first anamnestic challenges the differences at peak levels between the control and C. parvum treated groups were about to 4. Furthermore, the antibody molecules synthesized by the C. parvum treated animals were found to belong to IgG class. The results suggest that the immunological mechanisms mobilized are peculiar to C. parvum since they could not be reproduced either by BCG or by Freun'd adjuvant under similar conditions.     

In vitro effects of melanocytolytic agents and other compounds upon dominant human melanoma tyrosinase activity.

The activity of dominant human melanoma tyrosinase isozyme was greatly decreased by certain reducing agents. The number and geometry of phenolic groups as well as free--SH group appear important for enzymic inhibition.