Plants as sources of new antimicrobials and resistance-modifying agents

Covering: up to November 2011Infections caused by multidrug-resistant bacteria are an increasing problem due to the emergence and propagation of microbial drug resistance and the lack of development of new antimicrobials. Traditional methods of antibiotic discovery have failed to keep pace with the evolution of resistance. Therefore, new strategies to control bacterial infections are highly desirable. Plant secondary metabolites (phytochemicals) have already demonstrated their potential as antibacterials when used alone and as synergists or potentiators of other antibacterial agents. The use of phytochemical products and plant extracts as resistance-modifying agents (RMAs) represents an increasingly active research topic. Phytochemicals frequently act through different mechanisms than conventional antibiotics and could, therefore be of use in the treatment of resistant bacteria. The therapeutic utility of these products, however, remains to be clinically proven. The aim of this article is to review the advances in in vitro and in vivo studies on the potential chemotherapeutic value of phytochemical products and plant extracts as RMAs to restore the efficacy of antibiotics against resistant pathogenic bacteria. The mode of action of RMAs on the potentiation of antibiotics is also described.     

Physicochemical characteristics of protein-NP bioconjugates: the role of particle curvature and solution conditions on human serum albumin conformation and fibrillogenesis inhibition

Gold nanoparticles (Au NPs) from 5 to 100 nm in size synthesized with HAuCl(4) and sodium citrate were complexed with the plasma protein human serum albumin (HSA). Size, surface charge, and surface plasmon bands of the Au NPs are largely modified by the formation of a protein corona via electrostatic interactions and hydrogen bonding as revealed by thermodynamic data. Negative values of the entropy of binding suggested a restriction in the biomolecule mobility upon adsorption. The structure of the adsorbed protein molecules is slightly affected by the interaction with the metal surface, but this effect is enhanced as the NP curvature decreases. Also, it is observed that the protein molecules adsorbed onto the NP surface are more resistant to complete thermal denaturation than free protein ones as deduced from the increases in the melting temperature of the adsorbed protein. Differences in the conformations of the adsorbed protein molecules onto small (<40 nm) and large NPs were observed on the basis of ζ-potential data and FTIR spectroscopy, also suggesting a better resistance of adsorbed protein molecules to thermal denaturing conditions. We think this enhanced protein stability is responsible for a reduced formation of HSA amyloid-like fibrils in the presence of small Au NPs under HSA fibrillation conditions.     

Spectral and Photophysical Properties of α-carboline (1-Azacarbazole) in Aqueous Solutions

The absorption and fluorescence spectra of α-carboline, 9H-pyrido[2,3-b]indole, AC, in organic aprotic solvents containing different water proportions and in acid/base aqueous solutions inside and outside the pH range have been examined. In the organic aprotic solvents, the addition of increasing concentrations of water sequentially quenches and shifts to the red the fluorescence spectra of AC. These spectral changes have been rationalized assuming the formation, at the lower water concentrations, of a discrete ground state non-cyclic weakly fluorescent AC hydrate emitting at 376 nm that, upon increasing the water concentrations, evolves to a higher order AC poly hydrate emitting at 397 nm. The changes of the AC absorption spectra in aqueous acid/basic solutions indicate the existence of three ground state prototropic species; the pyridinic protonated cation, C (pK_a?=?4.10?±?0.05), the neutral, N (pK_a?=?14.5?±?0.2), and the pyrrolic deprotonated anion, A. Conversely, the changes of the AC fluorescence spectra in these media indicate the existence of four excited state species emitting at 376 nm, 397 nm, 460 nm and 465 nm. Since the emissions at 376 nm and 397 nm satisfactorily match those of the hydrates observed in the organic-water mixtures, they were consistently assigned to two differently hydrated ground state N species. The remaining emissions at 460 nm and 465 nm have been assigned without ambiguity, on the basis of their excitation spectra, to the C and A species, respectively. The excited-state pK_as of the prototropic species of AC have been estimated by using the Förster-Weller cycle.     

Optimal Estimate of a Pure Qubit State from Uhlmann–Josza Fidelity

In the framework of collective measurements, efforts have been made to reconstruct one-qubit states. Such schemes find an obstacle in the no-cloning theorem, which prevents full reconstruction of a quantum state. Quantum Mechanics thus restricts us to obtaining estimates of the reconstruction of a pure qubit. We discuss the optimal estimate on the basis of the Uhlmann–Josza fidelity, respecting the limitations imposed by the no-cloning theorem. We derive a realistic optimal expression for the average fidelity. Our formalism also introduces an optimization parameter L. Values close to zero imply full reconstruction of the qubit (i.?e., the classical limit), while larger L’s represent good quantum optimization of the qubit estimate. The parameter L is interpreted as the degree of quantumness of the average fidelity associated with the reconstruction.     

Trapping and injecting single domain walls in magnetic wire by local fields

A single domain wall (DW) moves at linearly increasing velocity under an increasing homogeneous drive magnetic field. Present experiments show that the DW is braked and finally trapped at a given position when an additional antiparallel local magnetic field is applied. That position and its velocity are further controlled by suitable tuning of the local field. In turn, the parallel local field of small amplitude does not significantly affect the effective wall speed at long distance, although it generates tail-to-tail and head-to-head pairs of walls moving along opposite directions when that field is strong enough.     

Scattering forces and electromagnetic momentum density in crossed circularly polarized standing waves

We analyze the forces on a small dipolar particle and the electromagnetic momentum density in a configuration consisting in two perpendicular circularly polarized stationary waves. The field distribution shows regions in which the electric and magnetic fields are parallel corresponding to a null Poynting vector. Although the average value of the momentum density, proportional to the Poynting vector, is zero in these regions, there are scattering forces acting on small particles due to light's spin force. The total scattering force suggests a new definition of the average value of the momentum density for free propagating electromagnetic fields.     

Comparative study of the in vitro bioactivities of Bupleurum rigidum and B. fruticescens

Decoctions of the aerial parts of either Bupleurum rigidum or B. fruticescens are equally used in certain parts of Spain for the treatment of topical and musculoskeletal inflammations. In the present paper, their phytochemical profile and pharmacological value has been compared. After chromatographic and spectral analyses we could establish the presence of rutin and absence of chlorogenic acid in B. fruticescens, whilst the contrary applies to B. rigidum, providing a means to chemically differentiate extracts and dry materials from the two species. Their free radical scavenging and antiperoxidative activities were similar, with B. fruticescens being more active overall. The infusions of both Bupleurum species also showed similar anti-inflammatory activity when tested by NF-kappaB assay (40% and 42% at 60 microg x mL(-1)), as well as in a hexosaminidase exocytosis assay (30% at 50 microg x mL(-1)). Antimigratory effects on rat melanoma B16F10 showed significant activity for both infusions, with B. rigidum twice as potent as B. fruticescens, the activity of the latter not being fully explained by its content of rutin. Taking all these results together, we can conclude that, in the selected experimental models, there exist an in vitro bioequivalence of the infusions from both species, which is in agreement with the majority of ethnopharmacological reports.     

Structural study of six cycloalkylammonium cinnamate salt structures featuring one‐dimensional columns and two‐dimensional hydrogen‐bonded networks

Six ammonium carboxylate salts, namely cyclopentylammonium cinnamate, C₅H₁₂N⁺·C₉H₇O₂⁻, (I), cyclohexylammonium cinnamate, C₆H₁₄N⁺·C₉H₇O₂⁻, (II), cycloheptylammonium cinnamate form I, C₇H₁₆N⁺·C₉H₇O₂⁻, (IIIa), and form II, (IIIb), cyclooctylammonium cinnamate, C₈H₁₈N⁺·C₉H₇O₂⁻, (IV), and cyclododecylammonium cinnamate, C₁₂H₂₆N⁺·C₉H₇O₂⁻, (V), are reported. Salts (II)–(V) all have a 1:1 ratio of cation to anion and feature three N⁺—H...O⁻ hydrogen bonds forming one‐dimensional hydrogen‐bonded columns consisting of repeating R₄³(10) rings, while salt (I) has a two‐dimensional network made up of alternating R₄⁴(12) and R⁶₈(20) rings. Salt (III) consists of two polymorphic forms, viz. form I having Z′ = 1 and form II with Z′ = 2. The latter polymorph has disorder of the cycloheptane rings in the two cations, as well as whole‐molecule disorder of one of the cinnamate anions. A similar, but ordered, Z′ = 2 structure is seen in salt (IV).     

Helical self‐assembly of 2‐(1,4,7,10‐tetraazacyclododecan‐1‐yl)cyclohexan‐1‐ol (cycyclen)

The title macrocyclic amino alcohol compound, C₁₄H₃₀N₄O, is investigated as a solid‐state synthon for the design of a self‐assembled tubular structure. It crystallizes in a helical column constructed by stereospecific O—H...N and N—H...N interactions. The hydrogen‐bonding interactions, dependent upon macrocyclic ring helicity and molecular conformation, link R,R and S,S enantiomers in a head‐to‐tail fashion, forming a continuous hydrophilic inner core.     

Frequent hypercyclicity,chaos, and unconditional Schauder decompositions

We prove that if X is any complex separable infinite-dimensional Banach space with an unconditional Schauder decomposition, X supports an operator T which is chaotic and frequently hypercyclic. In contrast with the complex case, we observe that there are real Banach spaces with an unconditional basis which support no chaotic operator.