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N Simonetti

Publications and source records attributed to N Simonetti.

At least 19 recordsLinked to original sources

Glucan synthesis and its inhibition by cilofungin in susceptible and resistant strains of Candida albicans.

The lipopeptide antimycotic agent, cilofungin, at a dose of 20 micrograms ml-1, inhibited beta 1-3 glucan synthesis in a drug-susceptible strain (3153; minimum inhibitory concentration (MIC) < 1 microgram ml-1) as well as in a drug-resistant strain of Candida albicans (CA-2, derived from 3153 by nitrosoguanidine mutagenesis; MIC > 50 micrograms ml-1). This was demonstrated for both whole cells under growing and non-growing conditions, and during protoplast regeneration. However, time-effect experiments, during growth of a CA-2 culture initially exposed to an inhibitory dose of cilofungin, showed that this strain was able to progressively regain both glucan synthesis and a growth rate comparable to that of cultures that had not been treated with the drug. This recovery was not attributable to cilofungin instability or degradation within the CA-2 culture. Our study suggests the existence of an as yet unknown drug-related and/or cell-related factor(s) modulating the inhibition of glucan synthesis, and then contributing to the actual inhibitory effects of cilofungin in C. albicans.

Antifungal Agents

Electrochemical Ag+ for preservative use.

In contact experiments with different experimental conditions, electrochemical Ag+ solutions exhibited better antimicrobial effectiveness against bacteria, a yeast species, and a mold than did analogous silver solutions from inorganic salts. The particular characteristics of electrochemical Ag+, such as the mode of action, effectiveness at low concentrations, and stability, indicate that Ag+ could be used effectively in preservatives.

Anti-Bacterial Agents

Antimicrobial contact activity of econazole sulfosalicylate.

The aim of this investigation was to compare the contact action of econazole sulfosalicylate (E-SSA) on mycetes (Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Trichophyton rubrum, T. cutaneum, Pityrosporum sp.), Gram-positive bacteria (Staphylococcus aureus, Streptococcus faecalis) and Gram-negative bacteria (Escherichia coli, Citrobacter freundii) with that exerted by econazole nitrate (E-NIT). The results show E-SSA activity greater than E-NIT (in particular against mycetes and Gram-negative bacteria). The E-SSA contact activity trials illustrated certain properties of this imidazole sulfosolicylate such as: absence of latency time, antimicrobial activity proportional to its concentration, when a high concentration is used, given the limiting influence of pH and ionic strength of the medium. The higher E-SSA contact activity, in relation to E-NIT, can be correlated to its greater lipophylia considering also the lipophylic properties of SSA and the scarce dissociation of E-SSA.

Aspergillus fumigatus

Increased in vitro sensitivity of Candida albicans to fluconazole.

Sodium dioctyl sulfosuccinate (SDSS), an anionic surfactant used at a non-antimicrobial concentration, increased the sensitivity of Candida albicans to fluconazole in complex media (such as Sabouraud). The conditions were assessed to determine the in vitro sensitivity to fluconazole. In this connection, the use of a liquid medium at a non-alkaline pH is important. The presence of SDSS in complex media does not seem to affect the neutralization of a particular substances but favours the activity of fluconazole.

Candida albicans

Researches on antibacterial and antifungal agents, XII: Analogues of bifonazole with two imidazole moieties and related azoles.

Analogues of bifonazole bearing two imidazole rings and other related azoles have been synthesized and tested as antifungal agents against Candida albicans and Candida spp.. Only a slight part of the antifungal power of the parent drug is retained by some derivatives as evinced by the comparison of new compounds with bifonazole, miconazole, and ketoconazole.

Antifungal Agents

Macrophage lysozyme stimulation by fructose-1-6-diphosphate.

FDP produces an increase of serum lysozyme concentration which may be related to stimulation of the phagocytic activity. Mice macrophages in vitro produce extracellular and intracellular LSZ (lysozyme) and FDP (fructose-1-6-diphosphate) increases this production. Also in vivo FDP stimulates the macrophages intracellular lysozyme production. The toxic activity in vitro and the protection in vivo against Staphylococcus pyogenes after FDP administration can also be related to macrophage stimulation.

Animals

Investigations of the activity by contact of miconazole sulfosalicylate.

The in-vitro antimicrobial activity of miconazole sulfosalicylate (M.SSA) has been investigated on mycetes (Candida albicans, Cryptococcus neoformans, Aspergillus niger, Trichophyton mentagrophytes), Gram-positive bacteria (Staphylococcus aureus, Streptococcus faecalis) and Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Serratia marcescens and Proteus vulgaris) in comparison with miconazole nitrate (M.NIT). The results showed M.SSA has a greater activity than M.NIT, particularly on mycetes and Gram-negative bacteria. The study of activity by contact with M.SSA showed some characteristics of this sulfosalicylate imidazole, such as the lack of a latency time, an antimicrobic action related directly to the concentration, the limited influence of pH and ionic strength of medium used. The greater activity by contact of M.SSA than M.NIT could be related to its higher lipophilia (due also to the lipophilic characteristics of SSA) and, therefore, to increased interaction with the cell membrane.

Candida albicans

In vitro antimicrobial activity of econazole and miconazole sulfosalicylate.

The in vitro activities of new sulfosalicylic salts of econazole (E.SSA) and miconazole (M.SSA) have been investigated in comparison with the respective nitrate (NIT) salts and sulfosalicylic acid (SSA) alone. The results reveal good antimicrobial activity of M.SSA and E.SSA against different strains of Candida, dermatophytes, moulds, Gram-positive bacteria and Trichomonas vaginalis. The MIC values demonstrate that M.SSA is more active than M.NIT on Candida and T. vaginalis. E.SSA was also more active than E.NIT on T.vaginalis. Both SSA and sodium sulfosalicylate (NaSSA) were practically without activity by themselves. Finally, the pH variations did not significantly modify the activity of the SSA salts, suggesting that their greater activity could be due to better lipophilic activity of these compounds with respect to the nitrate salts.

Animals

Researches on antibacterial and antifungal agents, X. Synthesis and antifungal activities of 1-(p-methyl-alpha-[4-(1H-pyrrol-1-yl)phenyl]benzyl)azoles and some related products.

The synthesis and antifungal activities against Candida albicans and Candida spp. of some pyrrole analogues of bifonazole are reported. 1-(p-Methyl-alpha-[4-(1H-pyrrol-1-yl)phenyl]benzyl)imidazole was found to be equipotent or sometimes superior to bifonazole and ketoconazole, and lightly inferior to miconazole. Substitution of the imidazole moiety with other azoles retained some activities. No activity was shown when the azole aromatic rings were replaced by the heteroalicyclic ones.

Antifungal Agents

Action of the ketoconazole-alkylaminoethylglycine combination on Candida albicans.

High concentrations of ketoconazole (Ktc) exhibit poor antimicrobial activity in microbicidal test. Alkylaminoethylglycine (AAEG), an amphoteric surface-active agent, employed in subinhibitory concentrations, can enhance the action of ketoconazole. The Ktc-AAEG combination causes a higher rate of potassium ion release compared to both drugs separately. The increased ketoconazole activity may be ascribed to the membrane damage indicated by increased permeability to potassium ions.

Candida albicans

Research on antibacterial and antifungal agents. XI. New antibacterial quinolones related to pirfloxacin.

The synthesis and antimicrobial activities against Gram-positive and Gram-negative bacteria of some 1-substituted quinolones related to pirfloxacin are reported. Compounds with a benzyl moiety at 1-position were generally found to be less active than the analogues bearing an unsaturated alkyl chain at the same position. Introduction of fluorine or chlorine in the benzyl moiety did not increase the antibacterial activity. All derivatives here reported were inferior to pirfloxacin as regards antibacterial power, but always superior in comparison with nalidixic acid and pipemidic acid against Gram-positive microorganisms.

Anti-Infective Agents

Glycogen medium, antitrichomonal drug activity in vaginal liquids.

The amount of glycogen in vaginal liquids decreases with Trichomonas vaginalis and this is connected with T. vaginalis activity in specimens. A glycogen-hydrolysed casein medium ("glycogen medium") added to vaginal liquid is a valid maintenance medium for T. vaginalis and therefore enables a direct test for antitrichomonas drugs to be performed.

Animals

"Mycelial vaginal test" and Candida susceptibility.

We have investigated the possibility of vaginal liquids affecting the transition from a yeast form (Y) to a mycelial one (M) in C. albicans and the possible relation to microbial flora, pH and glycogen. The C. albicans Y----M conversion, "mycelial vaginal test", in 250 specimens of vaginal liquid shows a 70% positivity rate against a test Candida strain. Results of the vaginal test are not related to bacteria, flora and pH, but to Candida infection and to glycogen concentration. Using a Y----M good-responder Candida strain in the vaginal test it is possible to have a global index of the factors affecting the Candida filamentation in the host. It can be advisable to utilize the vaginal test as a virulence test for Candida strains and as an indicative test of phenotypic drug resistance.

Candida albicans

[Substances with antibacterial and antifungal activity. VII. Synthesis and microbiologic activity of new derivatives of 1,5-diarylpyrrole].

The synthesis and antifungal activities of new 1,5-diarylpyrrole derivatives are reported. Antimicrobial data in comparison with pyrrolnitrin show that N-methylpiperazinylamides exhibit very poor activity against Candida albicans and Candida sp. while acid and ester derivatives are inactive. Vice-versa many acid or amide derivatives show interesting antibacterial activity. The results obtained are discussed on the basis of structure-activity relationships.

Anti-Bacterial Agents

Itraconazole: increased activity by chlorhexidine.

Chlorhexidine increases the activity of itraconazole against Candida isolates; itraconazole-chlorhexidine combinations show synergistic activity in culture media. The activity of itraconazole is discussed.

Animals

Itraconazole activity against fungal germination.

Itraconazole was found to be superior to ketoconazole in its antifungal activity in vitro against Hyphomycetes and Candida. In particular, complete inhibition of germination of Candida albicans and Aspergillus spp. by a lower dose of itraconazole can explain the better activity in vivo of this drug.

Antifungal Agents

[A substance with antibacterial and antifungal activity. IV. Synthesis and microbiological activity of new 1,5-diarylpyrrole derivatives].

The synthesis and antifungal activities of new 1,5-diarylpyrrole derivatives are reported. Antimicrobial data in comparison with pyrrolnitrin show that only carboxamide derivatives exhibit satisfactory antifungal activity. By contrast all tested compounds show very poor antibacterial activity. The displacement of NO2 group from para to meta or ortho position of the aryl at C5 of the pyrrole ring affects the antimicrobial activity.

Anti-Infective Agents