1.Fish oils against Burkholderia and Pseudomonas aeruginosa: in vitro efficacy and their therapeutic and prophylactic effects on infected Galleria mellonella larvae.
Mil-Homens D1, Ferreira-Dias S2, Fialho AM1,3. J Appl Microbiol. 2016 Mar 25. doi: 10.1111/jam.13145. [Epub ahead of print]
AIM: This study investigates the antimicrobial effects of fish oil-based formulas rich in omega-3 fatty acids (free fatty acids, ethyl esters or triacylglycerols), against cystic fibrosis (CF) pathogens (Burkholderia cenocepacia K56-2 and Pseudomonas aeruginosa PAO1), often resistant to multiple antibiotics.
2.Neuroprotective Properties of Compounds Extracted from Dianthus superbus L. against Glutamate-induced Cell Death in HT22 Cells.
Yun BR1, Yang HJ1, Weon JB1, Lee J1, Eom MR1, Ma CJ2. Pharmacogn Mag. 2016 Apr-Jun;12(46):109-13. doi: 10.4103/0973-1296.177905.
BACKGROUND: Dianthus superbus L. has been used in Chinese herbal medicine as a diuretic and anti-inflammatory agent.
3.Royal Jelly Constituents Increase the Expression of Extracellular Superoxide Dismutase through Histone Acetylation in Monocytic THP-1 Cells.
Makino J1, Ogasawara R1, Kamiya T1, Hara H1, Mitsugi Y1, Yamaguchi E1, Itoh A1, Adachi T1. J Nat Prod. 2016 Apr 6. [Epub ahead of print]
Extracellular superoxide dismutase (EC-SOD) is one of the main SOD isozymes and plays an important role in the prevention of cardiovascular diseases by accelerating the dismutation reaction of superoxide. Royal jelly includes 10-hydroxy-2-decenoic acid (10H2DA, 2), which regulates the expression of various types of genes in epigenetics through the effects of histone deacetylase (HDAC) antagonism. The expression of EC-SOD was previously reported to be regulated epigenetically through histone acetylation in THP-1 cells. Therefore, we herein evaluated the effects of the royal jelly constituents 10-hydroxydecanoic acid (10HDA, 1), sebacic acid (SA, 3), and 4-hydroperoxy-2-decenoic acid ethyl ester (4-HPO-DAEE, 4), which is a derivative of 2, on the expression of EC-SOD in THP-1 cells. The treatment with 1 mM 1, 2, or 3 or 100 μM 4 increased EC-SOD expression and histone H3 and H4 acetylation levels. Moreover, the enrichment of acetylated histone H4 was observed in the proximal promoter region of EC-SOD and was caused by the partial promotion of ERK phosphorylation (only 4) and inhibition of HDAC activities, but not by the expression of HDACs.
4.Synthesis of tetracyclic iminosugars fused benzo[e][1,3]thiazin-4-one and their HIV-RT inhibitory activity.
Yin Z1, Zhu M1, Wei S1, Shao J1, Hou Y1, Chen H2, Li X3. Bioorg Med Chem Lett. 2016 Apr 1;26(7):1738-41. doi: 10.1016/j.bmcl.2016.02.049. Epub 2016 Feb 18.
Several aza-C-pseudonucleosides bearing 1,3-benzothiazin-4-one (6 and 7) were prepared by the one-pot three-component condensation from the iminosugar aldehyde 3, amino acid ethyl/methyl ester hydrochlorides 4(a-c), and 2-mercaptobenzoic acid 5. After removal of Boc and the isopropylidene groups, the target novel tetracyclic iminosugars fused benzo[e][1,3]thiazin-4-one 1(a-c) and 2(a-b) were first afforded by the intramolecular cyclo-amidation reaction. Their structures were determined by their (1)H, (13)C NMR, and HRMS (ESI) spectra and X-ray. The tetracyclic iminosugars 1(a-c) and 2(a-b) were examined for their HIV reverse transcriptase (RT) inhibitory activities. The result showed that all compounds could effectively inhibit RT activity. Among them, compound 2a was the best one with the IC50 value of RT inhibitory activity of 0.82μM. Structure-activity relationship analysis suggested that 1'R configuration in the tetracyclic azasugars was of benefit to their anti-HIV RT activity.