Preliminary study of the anticancer applications of mesoporous materials functionalized with the natural product betulinic acid

Dehydrated MCM-41 (S1) was functionalized under nitrogen with 3-chloropropyltriethoxysilane (CPTS) and 3-aminopropyltriethoxysilane (APTS) by grafting in toluene at 80 °C over 48 h to give the corresponding materials S2 and S3, respectively. Subsequently, S2 and S3 were suspended in methanol and reacted in a nitrogen atmosphere with betulinic acid (BA) for 48 h at 65 °C (in the presence of the triethylamine of S2) to give the BA-functionalized materials S4 and S5. All materials studied were characterized by powder X-ray diffraction, X-ray fluorescence, nitrogen gas sorption, multinuclear MAS NMR spectroscopy, thermogravimetry, UV spectroscopy, IR, SEM, and TEM. To study the release of BA, S4 and S5 were suspended in solutions simulating various body pH conditions (pH 7.4, 5.5, and 3.0). Results of the quantification of BA release by HPLC for S4 show a pH-dependent and very slow BA release following a logarithmic tendency, while S5 behaves differently, also pH-dependent but, in this case, fast release of BA which requires only days for total release of the therapeutic compound. In addition, the cytotoxic activity of all synthesized materials against various cancer cell lines was studied. The results show the absence of an antiproliferative effect on the surfaces without BA S1-S3, while an antiproliferative effect was observed with S4 and S5 and was attributed to the release of BA in the medium.     

Lipid peroxidative damage on Cisplatin exposure and alterations in antioxidant defense system in rat kidneys: a possible protective effect of selenium

Cisplatin (Cis-diamminedichloroplatinum II, CP) is an important chemotherapeutic agent, useful in the treatment of several cancers, but with several side effects such as nephrotoxicity. The present study investigated the possible protective effect of selenium (Se) against CP-induced oxidative stress in the rat kidneys. Male Wistar albino rats were injected with a single dose of cisplatin (7 mg CP/kg b.m., i.p.) and selenium (6 mg Se/kg b.m, as Na(2)SeO(3), i.p.), alone or in combination. The obtained results showed that CP increased lipid peroxidation (LPO) and decreased reduced glutathione (GSH) concentrations, suggesting the CP-induced oxidative stress, while Se treatment reversed this change to control values. Acute intoxication of rats with CP was followed by statistically significant decreased activity of antioxidant defense enzymes: superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GR) and glutathione-S-transferase (GST). Treatment with Se reversed CP-induced alterations of antioxidant defense enzyme activities and significantly prevented the CP-induced kidney damage.     

Antiproliferative and Proapoptotic Activities of Methanolic Extracts from Ligustrum vulgare L. as an Individual Treatment and in Combination with Palladium Complex

The aim of this study is to examine the growth inhibitory effects of methanolic leaf and fruit extracts of L. vulgare on HCT-116 cells over different time periods and their synergistic effect with a Pd(apox) complex. The antiproliferative activity of plant extracts alone or in combination with the Pd(apox) complex was determined using MTT cell viability assay, where the IC(50) value was used as a parameter of cytotoxicity. Results show that antiproliferative effects of L. vulgare extracts increase with extension of exposure time, with decreasing IC(50) values, except for 72 h where the IC(50) values for methanolic leaf extract were lower than for the fruit extract. The Pd(apox) complex alone had a weak antiproliferative effect, but combination with L. vulgare extracts caused stronger effects with lower IC(50) values than with L. vulgare extracts alone. The type of cell death was explored by fluorescence microscopy using the acridin orange/ethidium bromide method. Treatments with plant extracts caused typical apoptotic morphological changes in HCT-116 cells and co-treatments with Pd(apox) complex caused higher levels of apoptotic cells than treatment with plant extracts alone. The results indicate that L. vulgare is a considerable source of natural bioactive substances with antiproliferative activity on HCT-116 cells and which have a substantial synergistic effect with the Pd(apox) complex.     

A comparative study of photocatalytically active nanocrystalline tetragonal zyrcon-type and monoclinic scheelite-type bismuth vanadate

Monoclinic scheelite-type BiVO₄ is currently considered as one of the most promising non-titania photocatalysts, wheras tetragonal zircon-type BiVO₄ is still poorly understood. Herein, a new and simple synthetic approach was applied and nanostructured single-phase zircon-type BiVO₄ was successfully prepared by a controllable ethylene-glycol colloidal route. In addition, nanostructured monoclinic scheelite-type BiVO₄ powders were also fabricated through annealing of the as-prepared samples. A comparative study of the two BiVO₄ polymorphs was conducted and it turned out that the novel synthetic approach had a significant impact on porosity and photocatalytic performance of zircon-structured BiVO₄. All the prepared materials, as-prepared and annealed, were mesoporous, while measured values of specific surface area of some zircon-structured samples (～34?m²/g) were ～7 times higher than those reported thus far for this phase. Interestingly, for the first time, zircon-type BiVO₄, previously considered to be a poor photocatalyst, exhibited a better overall performance in degradation of methyl orange compared to monoclinic scheelite-type BiVO₄. Hence, it could be expected that the here-presented synthesis and observations will both arouse interest in scarcely studied tetragonal zircon-type BiVO₄ and facilitate as well as speed up further research of its properties.     

Thermal noise in aqueous quadrupole micro- and nano-traps

ABSTRACT: Recent simulations and experiments with aqueous quadrupole micro-traps have confirmed a possibility for control and localization of motion of a charged particle in a water environment, also predicting a possibility of further reduction of the trap size to tens of nano-meters for trapping charged bio-molecules and DNA segments. We study the random thermal noise due to Brownian motion in water which significantly influences the trapping of particles in an aqueous environment. We derive the exact, closed-form expressions for the thermal fluctuations of position and velocity of a trapped particle and thoroughly examine the properties of the rms for the fluctuations as functions of the system parameters and time. The instantaneous signal transferring mechanism between the velocity and position fluctuations could not be achieved in the previous phase-average approaches.     

The A9 Core Sequence from NRPS Adenylation Domain Is Relevant for Thioester Formation

The adenylation (A) domain in nonribosomal peptide synthetases catalyses a two-step reaction in which an amino acid is activated and then transferred to the neighbouring thiolation (T) domain. In this study, we investigated the role of the conserved A9 core sequence of the A-domain of tyrocidine synthetase 1, by analysis of single amino acid mutations in the A9 region. Mutation of an absolutely conserved proline (P490G) significantly reduced the conformational stability of the protein, as evidenced by increased susceptibility to proteolytic cleavage and denaturation. All mutant A-domains were capable of amino acid activation, but the activity in the overall reaction was reduced. Surprisingly, the S491R mutant (mutation at the first residue following the A9 motif) showed elevated overall activity compared to the wild-type protein. Our results suggest that the A9 core sequence plays a role in the second reaction step, in which it could serve as a "clip" for the proper positioning of residues important for the interaction with the T-domain, and/or stabilisation of the thioester-forming conformation.     

High value polyurethane resins from rubber seed oil

Rubber seed oil having high free fatty acid content and high unsaturation was used to obtain high quality polyurethane resins through epoxidation and ring opening with methanol and free fatty acids. Two polyols prepared with free fatty acids and without were cured with modified methylene diphenyl diisocyanate to obtain strong, high modulus glassy polyurethanes. The effect of structure on thermal and mechanical properties was analyzed. This showed that the polyol with free fatty acid utilized to obtain a branched structure gave superior crosslinking density and mechanical properties. © 2016 Society of Chemical Industry     

Influence of high power ultrasound on physical–chemical properties of polypropylene films aimed for food packaging: barrier and contact angle features

Investigation was focused on the impact of high power ultrasound (HPUS), also called thermosonication, on the oxygen permeation properties (permeability, solubility and diffusion coefficients) of barrier films aimed for food packaging. For this purpose, biaxially oriented polypropylene (BOPP) coated with acrylic/polyvinylidene chloride (BOPPAcPVDC) and biaxially oriented coextruded polypropylene (BOPPcoex) were used. The physical–chemical profile of the samples was determined using goniometry. There is a significant impact only of extreme HPUS conditions (the longest time and the highest amplitude) on the permeability, solubility and diffusion coefficients of oxygen through the BOPP films. The highest influence on the oxygen permeability in both investigated BOPP samples involved an HPUS with an amplitude of 100% during a 6 min treatment. However, BOPP samples showed different sensitivities at lower HPUS treatments. © 2017 Society of Chemical Industry