Antiproliferative activity of synthetic fatty acid amides from renewable resources

AbstractIn the work, the in vitro antiproliferative activity of a series of synthetic fatty acid amides were investigated in seven cancer cell lines. The study revealed that most of the compounds showed antiproliferative activity against tested tumor cell lines, mainly on human glioma cells (U251) and human ovarian cancer cells with a multiple drug-resistant phenotype (NCI-ADR/RES). In addition, the fatty methyl benzylamide derived from ricinoleic acid (with the fatty acid obtained from castor oil, a renewable resource) showed a high selectivity with potent growth inhibition and cell death for the glioma cell line—the most aggressive CNS cancer

Uncommon Trimethoxylated Flavonol Obtained from Rubus rosaefolius

This study shows the evaluation the antiproliferative effect of the extract, fractions, and uncommon compounds isolated from R. rosaefolius leaves. The compounds were identified by conventional spectroscopic methods such as NMR-H1 and C13 and identified as 5,7-dihydroxy-6,8,4′-trimethoxyflavonol (1), 5-hydroxy-3,6,7,8,4′-pentamethoxyflavone (2), and tormentic acid (3). Both hexane and dichloromethane fractions showed selectivity for multidrug-resistant ovary cancer cell line (NCI-ADR/RES) with total growth inhibition values of 11.1 and 12.6 μg/ml, respectively. Compound 1 also showed selective activity against the same cell line (18.8 μg/ml); however, it was especially effective against glioma cells (2.8 μg/ml), suggesting that this compound may be involved with the in vitro antiproliferative action

Pharmacological characterization of Solanum cernuum Vell.: 31-norcycloartanones with analgesic and anti-inflammatory properties

Cycloeucalenone (1) and 24-oxo-31-norcycloartanone (2) obtained from Solanum cernuum Vell. were assayed to explore their pharmacologic roles. Previous studies showed that (2) has selective activity against lung tumor cell line (NCIH460) which expresses high levels of COX-2, suggesting its role in inflammatory process, and also a link between chronic inflammation and cancer-associated process. Dichloromethane crude extract (DCE) significantly reduced writhing and stretching induced by 0.8 % acetic acid at a dose of 100, 300, and 600 mg/kg, po; oral administration of different doses of (1) and (2) also displayed significant analgesic and anti-inflammatory effects in the writhing acetic acid test (p < 0.0001). Selected oral doses of both compounds (100 and 50 mg/kg) were assayed in the carrageenan-induced paw edema model. Compound (2) showed significant activity during the early phase (1.5–6 h) and also in the late phase (48 h) (p < 0.01). The anti-nociceptive activity observed for the compounds (1) and (2) and DCE was found to be related to the inhibition of different mediators involved in inflammation and nociceptive process. Both compounds decreas COX-2 protein expression, although only compound (2) reached a significant response (p < 0.05 vs control). However, in vitro Sirtuin 1 activity and TNF-a production in THP-1 macrophages were not affected

Phenolic composition, antiproliferative and antiulcerogenic activities of a polyphenol‐rich purified extract from açai ( Euterpe oleracea ) fruits

The bioactivity and phytochemical composition of a partially purified extract of açai (PPEA), concentrated in phenolic compounds (PC) and without the presence of macronutrients, were investigated. The major PC quantified by UHPLC-DAD-LTQ-Orbitrap MS-MS/MS in the PPEA are anthocyanins. In vitro, PPEA showed a cytostatic effect on the K-562 lymphoid leukaemia at a concentration of 40 μg PC mL−1, with a GI50 equal to 1.08 μg PC mL−1. In vivo, the extract did not promote acute toxicity in mice in any of the doses tested. The extract displayed gastroprotective activity in rats treated orally with 16, 48 and 160 mg PC kg−1, with a significant decrease in the ulcerative lesion index, compared with the negative control. The lack of toxicity and the bioactivity of the PPEA show that this extract is beneficial to health and useful as a commercial food additive containing natural violet colourant, with pharmaceutical and functional potentials

Path integral Monte Carlo studies of the H5 +/D 5 + clusters using ab initio potential surfaces

We report here on classical and path integral Monte Carlo studies for the H5 + cluster and its deuterated counterpart, in order to investigate the floppy nature of its molecular structure due to anharmonic quantum effects. This method relies on the standard harmonic normal mode analysis and has been found to be effective for evaluating thermochemical/ ground-state properties of highly anharmonic systems. A full-dimensional recent analytical CCSD(T) potential surface and a novel realistic density functional theory (DFT) 'on the fly'-based potential scheme were employed. Thermal equilibrium energies for H5 + and D5 + are determined from the path integral Monte Carlo (PIMC) calculations. The H5 + and D5 + probability density distributions are also obtained from both classical Monte Carlo and fully converged PIMC calculations, and they show strong spatial delocalization with highly anharmonic character. It was found that, on average, H5 + and D5 + can be described as a proton shared between the two outer almost freely rotating H2/D2 molecules. The implementation of such a combined PIMC/DFT approach to study nuclear quantum fluctuation on the electronic properties of H5 + is discussed, and its extension to larger protonated hydrogen clusters is also proposed. © 2011 The Royal Swedish Academy of Sciences.Peer Reviewe