Preclinical pharmacokinetics comparison between resveratrol 2-hydroxypropyl-β-cyclodextrin complex and resveratrol suspension after oral administration

Trans-Resveratrol (RV) is a natural polyphenol characterized by interesting pleiotropic potentials and health benefits, but its administration is hampered by a unsatisfactory pharmacokinetics. Various approaches have been identified to circumvent it: among them, 2-hydroxypropyl-β-cyclodextrins (HPβCD) are valuable strategy. Here, we compare the employment of HPβCD based formulation with a resveratrol nanosupension (obtained by diluting a RV ethanol solution with PBS, added of 0.05 % hydroxyethylcellulose) to improve RV bioavailability after oral administration to mice. The inclusion of RV in HPβCD was confirmed by differential scanning calorimetry, Fourier transformed infrared spectroscopy, and phase solubility study. The two formulations were orally administered to BALB-c mice. RV concentrations in plasma and tissues were detected at different time (0–120 min) by HPLC method. HPβCD complexation mediate a approximately fourfold increment in plasma RV C_max and  approximately twofold augment of RV AUC_0-120 in comparison with RV nanosuspension. Similar increased concentrations were observed in heart, liver, kidney and gut. In particular, HPβCD mediated a 5.5-folds increase of resveratrol concentration in the intestine, in comparison to the nanosuspension. In conclusion, based on our results, HPβCD complexation is a promising approach to increase the oral bioavailability of RV. Moreover, the achievement of high concentrations in gut suggested a potential employment of oral RV-HPβCD as anti-inflammatory/chemopreventive agent in this tissue.     

Enhanced resolution of Mentha piperita volatile fraction using a novel medium‐polarity ionic liquid gas chromatography stationary phase

The evaluation of a novel medium‐polarity ionic‐liquid‐based gas chromatography column, SLB‐IL60, towards the analysis of a complex essential oil, namely, a peppermint essential oil sample, is reported. The SLB‐IL60 30 m column was subjected to bleeding measurements, by means of conventional gas chromatography with mass spectrometry. The SLB‐IL60 column was then evaluated in the analysis of pure standard compounds, chosen as typical constituents of peppermint essential oil. Resolution and peak symmetry (expressed as tailing factors at 10% of peak height) were measured and the results were compared to those obtained on the most widely used columns in such an application, namely a medium‐polarity [100% poly(ethyleneglycol)] stationary phase, and an apolar 5% diphenyl/95% dimethyl siloxane. The final part of the evaluation was dedicated to the gas chromatography with mass spectrometry analysis of a peppermint essential oil sample and again the data were compared to those obtained on the 100% poly(ethyleneglycol) and the 5% diphenyl/95% dimethyl siloxane phase. Linear retention indices were determined for all the identified components on the ionic liquid capillary.     

Iron Oxide Nanoparticles Labeled with an Excited‐State Intramolecular Proton Transfer Dye

Excited‐state intramolecular proton transfer (ESIPT) is a particularly well known reaction that has been very little studied in magnetic environments. In this work, we report on the photophysical behavior of a known ESIPT dye of the benzothiazole class, when in solution with uncoated superparamagnetic iron oxide nanoparticles, and when grafted to silica‐coated iron oxide nanoparticles. Uncoated iron oxide nanoparticles promoted the fluorescence quenching of the ESIPT dye, resulting from collisions during the lifetime of the excited state. The assembly of iron oxide nanoparticles with a shell of silica provided recovery of the ESIPT emission, due to the isolation promoted by the silica shell. The silica network gives protection against the fluorescence quenching of the dye, allowing the nanoparticles to act as a bimodal (optical and magnetic) imaging contrast agent with a large Stokes shift.     

Faithful tropicalisation and torus actions

For any affine variety equipped with coordinates, there is a surjective, continuous map from its Berkovich space to its tropicalisation. Exploiting torus actions, we develop techniques for finding an explicit, continuous section of this map. In particular, we prove that such a section exists for linear spaces, Grassmannians of planes (reproving a result due to Cueto, Häbich, and Werner), matrix varieties defined by the vanishing of 3 × 3-minors, and for the hypersurface defined by Cayley’s hyperdeterminant.     

Highly symmetric hypertopes

We study incidence geometries that are thin and residually connected. These geometries generalise abstract polytopes. In this generalised setting, guided by the ideas from the polytope theory, we introduce the concept of chirality, a property of orderly asymmetry occurring frequently in nature as a natural phenomenon. The main result in this paper is that automorphism groups of regular and chiral thin residually connected geometries need to be C-groups in the regular case and \({C^+}\)-groups in the chiral case.     

Acetone powder from dormant seeds of Ricinus communis L

The influence of several factors on the hydrolytic activity of lipase, present in the acetone powder from dormant castor seeds (Ricinus communis) was evaluated. The enzyme showed a marked specificity for short-chain substrates. The best reaction conditions were an acid medium, Triton X-100 as the emulsifying agent and a temperature of 30 degrees C. The lipase activity of the acetone powder of different castor oil genotypes showed great variability and storage stability of up to 90%. The toxicology analysis of the acetone powder from genotype Nordestina BRS 149 showed a higher ricin (toxic component) content, a lower 2S albumin (allergenic compound) content, and similar allergenic potential compared with untreated seeds.     

A multifunctional nanoassembly of mesogen-bearing amphiphiles and porphyrins for the simultaneous photodelivery of nitric oxide and singlet oxygen

We report a molecular nanoassembly able to supply simultaneously, in the same region of space and under the exclusive control of visible light, nitric oxide and singlet oxygen, two species playing a key role in the therapy of cancer; the considerable fluorescence of this nanoaggregate and its reduced size (ca. 40 nm) represent additional advantages that make this photoactive vehicle an appealing candidate to be tested in biological systems.     

Surface-activated chemical ionization ion trap mass spectrometry for the analysis of cocaine and benzoylecgonine in hair after extraction and sample dilution

Surface-activated chemical ionization (SACI) was employed for the analysis of cocaine and its metabolite, benzoylecgonine, extracted from hair. Following decontamination and acid hydrolysis procedures on the hair sample, the sample solution was diluted (1:10) and directly analyzed by liquid chromatography/surface-activated chemical ionization multiple collisional stage single reaction monitoring mass spectrometry (LC/SACI-MS(3)-SRM) without solid-phase extraction (SPE) pre-purification and concentration procedures. To increase the selectivity of the method, MS(3) was chosen instead of the less selective MS/MS. This data was compared with that achieved using gas chromatography/mass spectrometry (GC/MS), the reference method used by the Italian Government Institute of Health protocol. The limits of detection (LODs) were 0.003 ng/(mg hair) for cocaine and 0.02 ng/(mg hair) for benzoylecgonine and the limits of quantitation (LOQs) were 0.01 ng/(mg hair) for cocaine and 0.04 ng/(mg hair) for benzoylecgonine. The squared correlation coefficient (R(2)) of the calibration curve was 0.9887-0.9980 for cocaine and 0.9987-0.9997 for benzoylecgonine. The percent accuracy error was 2-5% for both cocaine and benzoylecgonine using the LC/SACI-MS(3)-SRM approach, whereas it was higher for benzoylecgonine (20-25%) using the LC/SACI-MS/MS-SRM approach compared with the GC/MS data due to hair matrix contamination. In both cases, high precision was achieved (1-3% precision error), which confirmed the stability of the developed methods.     

Pharmacological and Therapeutic Potential of Myristicin: A Literature Review

Natural products have been used by humanity for many centuries to treat various illnesses and with the advancement of technology, it became possible to isolate the substances responsible for the beneficial effects of these products, as well as to understand their mechanisms. In this context, myristicin, a substance of natural origin, has shown several promising activities in a large number of in vitro and in vivo studies carried out. This molecule is found in plants such as nutmeg, parsley, carrots, peppers, and several species endemic to the Asian continent. The purpose of this review article is to discuss data published in the last 10 years at Pubmed, Lilacs and Scielo databases, reporting beneficial effects, toxicity and promising data of myristicin for its future use in medicine. From 94 articles found in the literature, 68 were included. Exclusion criteria took into account articles whose tested extracts did not have myristicin as one of the major compounds.     

The catalytic reduction of nitrobenzene at the [MoVIO2(O2CC(S)(C6H5)2)2]2− complex intercalated in a Zn(II)–Al(III) layered double hydroxide host: A kinetic model for the molybdenum–pterin binding site in nitrate reductase

The heterogeneous reduction of nitrobenzene by thiophenol catalyzed by the dianionic bis(2‐sulfanyl‐2,2‐diphenylethanoxycarbonyl) dioxomolybdate(VI) complex, [Mo^VIO₂(O₂CC(S)(C₆H₅)₂)₂]²⁻, intercalated into a Zn(II)–Al(III) layered double hydroxide host [Zn_3−xAl_x(OH)₆]^x+, has been investigated under anaerobic conditions. Aniline was found to be the only product formed through a reaction consuming six moles of thiophenol for each mol of aniline produced. The kinetics of the system have been analyzed in detail. In excess of thiophenol, all reactions follow first‐order kinetics (ln([PhNO₂]/[PhNO₂]₀) = −k_appt) with the apparent rate constant k_app being a complex function of both initial nitrobenzene and thiophenol concentrations, as well as linearly dependent on the amount of solid catalyst used. A mechanism for this catalytic reaction consistent with the kinetic experiments as well as the observed properties of the intercalated molybdenum complex has thiophenol inducing the initial coupled proton–electron transfer steps to form an intercalated Mo^IV species, which is oxidized back to the parent Mo^VI complex by nitrobenzene via a two‐electron oxygen atom transfer reaction that yields nitrosobenzene. This mechanism is widespread in enzymatic catalysis and in model chemical reactions. The intermediate nitrosobenzene thus formed is reduced directly by excess thiophenol to aniline. The values of rate coefficients indicate that reduction of nitrobenzene proceeds much faster than proton‐assisted oxidation of thiophenol. This may account for the observation that the presence of protonic amberlite IR‐120(H) increases considerably the rate of the overall reaction catalyzed. Activation parameters in excess of the protonic resin and PhSH were ΔH^≠ = 80 kJ mol⁻¹ and ΔS^≠ = −70 J mol⁻¹ K⁻¹. The large negative activation entropy is consistent with an associative transition state. The present system is characterized by a well‐defined catalytic cycle with multiple‐turnovers reductions of nitrobenzene to aniline without appreciable deactivation. © 2001 John Wiley & Sons, Inc. Int J Chem Kinet 33: 212–224, 2001