First report of chemical composition and cytotoxicity evaluation of Foraminispora rugosa basidiomata from Brazil.

BACKGROUND: Foraminispora rugosa is a species reported from Brazil, Venezuela, French Guiana, Costa Rica and Cuba. It is a basidiomycete in the Ganodermataceae family. In this study, both chemical composition and cytotoxicity of the ethanolic extract of F. rugosa were investigated for the first time. RESULTS: Phylogenetic analysis confirmed the identification of the specimens, and the results of cytotoxicity assays showed that at concentrations of 7.8-500.0 µg/mL the ethanolic extract displayed weak cytotoxicity against the tested cell lines. Five oxylipins were identified by ultra high performance liquid chromatography coupled with quadrupole time-of-flight and mass spectrometry (UHPLC-QTOF-MS). CONCLUSIONS: This study provides new insights into the current knowledge of bioactive compounds produced by macrofungi, and provides data for future biological assays with relative selectivity and safety.

2-Deoxy-d-Glucose and Its Analogs: From Diagnostic to Therapeutic Agents.

The ability of 2-deoxy-d-glucose (2-DG) to interfere with d-glucose metabolism demonstrates that nutrient and energy deprivation is an efficient tool to suppress cancer cell growth and survival. Acting as a d-glucose mimic, 2-DG inhibits glycolysis due to formation and intracellular accumulation of 2-deoxy-d-glucose-6-phosphate (2-DG6P), inhibiting the function of hexokinase and glucose-6-phosphate isomerase, and inducing cell death. In addition to glycolysis inhibition, other molecular processes are also affected by 2-DG. Attempts to improve 2-DG's drug-like properties, its role as a potential adjuvant for other chemotherapeutics, and novel 2-DG analogs as promising new anticancer agents are discussed in this review.

(-)-Linalool, a naturally occurring monoterpene compound, impairs memory acquisition in the object recognition task, inhibitory avoidance test and habituation to a novel environment in rats.

It is known that (-)-linalool is a competitive antagonist of NMDA receptors, which play a key role in the learning and memory processes; however, only a few studies have reported a possible interference of (-)-linalool in memory. The purpose of this study was to investigate the (-)-linalool effects on acquisition of short- and long-term memories through the objects recognition task, inhibitory avoidance test and habituation to a novel environment. Furthermore, the open field test was used to investigate the interference of (-)-linalool in motivation, locomotion and exploration by animals. Wistar male adult rats received an intraperitoneal injection (i.p.) of saline (NaCl 0.9%), tween 5% or (-)-linalool (50 or 100 mg/kg) before training in the tasks; MK-801 (0.1 mg/kg), a glutamate antagonist, was used as positive control. Short-term (STM) and long-term (LTM) memories were tested 1.5 and 24 h after training, respectively, in the inhibitory avoidance and recognition objects. The results suggested that (-)-linalool (as 50- and 100-mg/kg doses) impaired LTM acquisition, but not STM acquisition, in the object recognition task. In the inhibitory avoidance test, animals receiving linalool (both doses) showed impairment in acquisition of both memories measured. In the open field test, the animals that received (-)-linalool showed no significant difference in the crossings and latency to start the locomotion in any of the doses tested, although (-)-linalool 100 mg/kg reduced rearing behavior. When re-exposed to open field 24 h after training, the rats that received (-)-linalool 100mg/kg showed no habituation. Taken together, these data suggested that (-)-linalool was able to impair the acquisition of memory in rats, which can be associated to (-)-linalool antagonist capacity as regards NMDA glutamatergic receptors, since other glutamate antagonists also seem to affect memory.

Serum sensitivity of a Pseudomonas aeruginosa mucoid strain.

The susceptibility of Pseudomonas aeruginosa 144M (a mucoid strain isolated from the sputum of a cystic fibrosis patient) to the bactericidal activity of pooled fresh normal human serum (FHS) was examined. FHS at concentrations of greater than or equal to 2.5% was capable of killing greater than 95% of strain 144M. Strain 144M was killed by FHS in a dose-dependent manner. Although either immunoglobulin M (IgM) or IgG was bactericidal in the presence of complement, IgM was about 10 times as effective as IgG. However, optimal killing activity required both IgM and IgG and complement, activated by the classical pathway. A role for lysozyme in the killing of 144M was demonstrated only when low concentrations of FHS were used. In contrast to 144M, P. aeruginosa strains 144NM and 144M(SR) were totally resistant to FHS at all of the concentrations tested (up to 50%). Neither the FHS susceptibility of 144M nor the FHS resistance of 144NM or 144M(SR) was altered by choice of growth medium, growth phase, or temperature of growth. Results of absorption studies with whole organisms, isolated outer membrane preparations, or lipopolysaccharide (LPS) from each strain suggest that the antigen(s) which binds the bactericidal immunoglobulins is accessible on the surface of 144M but not on the surface of 144NM or 144M(SR), is insensitive to trypsin treatment, and is believed to be LPS. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis of the three LPS preparations demonstrated that 144M LPS contained primarily lipid-A-core polysaccharide components, whereas the LPS from 144NM and 144M(SR) were heterogeneous, with various degrees of O-side-chain substitution. These results suggest that at least one target for bactericidal antibody on the surface of 144M is contained in the rough LPS of this strain.

Development of an enzyme-linked immunosorbent assay for studying Pseudomonas aeruginosa cell surface antigens.

An enzyme-linked immunosorbent assay for the measurement of antibodies directed against Pseudomonas aeruginosa cell surface antigens was developed. Formalin-killed whole cells of P. aeruginosa, adsorbed to polystyrene acrylic copolymer cuvettes, were used as immobilized antigens. Antisera to P. aeruginosa mucoid strain 144M and to its spontaneous nonmucoid derivative, 144NM, were raised in rabbits by immunization with Formalin-killed bacteria. By using this enzyme-linked immunosorbent assay, anti-144M serum was found to have a ca. 10-fold-higher antibody titer to 144M than did anti-144NM serum, suggesting that 144M may have either immunogenic determinants not present on 144NM or perhaps simply more antigenic determinants. In contrast, anti-144M and anti-144NM immune sera were found to have nearly identical antibody titers to 144NM, suggesting that these strains share many determinants. Anti-P. aeruginosa immune serum was found to contain Pseudomonas-specific antibodies as well as antibodies which cross-reacted with other gram-negative bacteria. Finally, absorption studies demonstrated that this assay can detect both LPS and non-LPS surface-exposed antigenic determinants. Thus, this whole bacterial cell enzyme-linked immunosorbent assay should prove useful in monitoring patient sera and secretions for potentially protective immunoglobulins directed at P. aeruginosa cell surface antigens.