Application of acetylcholinesterase (AChE) inhibitors is the primary treatment for Alzheimer’s disease. Alkaloids, such as physostigmine, galanthamine, and huperzine A, play an important role as AChE inhibitors. The aim of this work was to evaluate Himatanthus lancifolius (Muell. Arg.) Woodson, a Brazilian species of Apocynaceae, and its main indole alkaloid uleine, in order to identify new AChE inhibitors. The plant fluid extract, fractions, and uleine were tested for AChE inhibitory activity using Ellman’s colorimetric method for thin-layer chromatography (TLC), 96-well microplates, and also Marston’s TLC colorimetric method. Both TLC assays showed similar results. At 5 mg/mL, the fluid extract inhibited the AChE enzyme by (50.71 ± 8.2)%. The ethyl acetate fraction exhibited the highest level of AChE inhibition, followed by the dichloromethane fraction. The isolated alkaloid uleine displayed an IC50 value of 0.45 μM.

A chemical study of the EtOAc extract of Nemania bipapillata (AT-05), an endophytic fungus isolated from the marine red alga Asparagopsis taxiformis - Falkenbergia stage, led to the isolation of five new botryane sesquiterpenes, including the diastereomeric pair (+)-(2 R ,4 S ,5 R ,8 S )-( 1 ) and (+)-(2 R ,4 R ,5 R ,8 S )-4-deacetyl-5-hydroxy-botryenalol ( 2 ), (+)-(2 R ,4 S ,5 R ,8 R )-4-deacetyl-botryenalol ( 3 ), one pair of diastereomeric botryane nor sesquiterpenes bearing an unprecedented degraded carbon skeleton, (+)-(2 R ,4 R ,8 R )-( 4 ) and (+)-(2 R ,4 S ,8 S )-( 5 ), which were named nemenonediol A and nemenonediol B, respectively, in addition to the known 4β-acetoxy-9β,10β,15α-trihydroxyprobotrydial ( 6 ). Their structures were elucidated using 1D and 2D NMR, HRESIMS and comparison with literature data of similar known compounds. The absolute configurations of 2 , 3 and 4 were deduced by comparison of experimental and calculated electronic circular dichroism (ECD) spectra, while those of 1 and 5 were assigned from vibrational circular dichroism (VCD) data. Compound 4 weakly inhibited acetylcholinesterase, whereas compound 1 inhibited both acetylcholinesterase and butyrylcholinesterase. Compounds 1 , 3 , 5 and 6 were tested against two carcinoma cell lines (MCF-7 and HCT-116), but showed no significant citotoxicity at tested concentrations (IC 50 > 50 µM).

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Affinity-based chromatography assays encompass the use of solid supports containing immobilized biological targets to monitor binding events in the isolation , identification and/or characterization of bioactive compounds. This powerful bioanalytical technique allows the screening of potential binders through fast analyses that can be directly performed using isolated substances or complex matrices. An overview of the recent researches in frontal and zonal affinity-based chromatography screening assays, which has been used as a tool in the identification and characterization of new anti-cancer agents, is discussed. In addition, a critical evaluation of the recently emerged ligands fishing assays in complex mixtures is also discussed.

Plants with antioxidant properties are beneficial for preventing the ageing events evoked by UV light, and numerous products based on Camellila sinensis (green tea) are commercially available, many of which claiming to contain bioactive compounds that would prevent UV-induced skin damage. In this study, we tested the efficacy of five commercial green tea extracts used to enrich cosmetic formulations for protecting human and mouse fibroblasts against UV radiation effects and compared with a fluid one prepared according to the Brazilian Pharmacopoeia recommendations. Taking into consideration that the ageing process can be accelerated by solar radiation by excessive free radical generation, leading to depletion of skin antioxidant defences, and its collapse caused by disruption of the metalloproteinase metabolism, we have used their individual (-)-epigallocathechin-3-gallate (EGCG) content, the catalase and SOD status and the matrix-degrading metalloproteases (MMP)-1, MMP-9 and MMP-13 levels as comparative parameters. The EGCG content of the commercial products showed wide variability, ranging from undetectable levels to 58.65 ± 1.12 μg mL(-1) , in contrast with the fluid extract (87.82 ± 1.35 μg mL(-1) ). Moreover, only the pharmacopoeic extract was able to significantly reduce MMP degradation while enhancing the levels of SOD and catalase. These results indicate, for the first time, that the methodologies for preparing herbal mixtures can interfere significantly with compounds endowed with photoprotective effects, and the efficacy of products containing C. sinensis extracts thought to act against effects of solar radiation can be compromised.

Experiments were designed and performed in order to investigate whether or not the different cellular energy deposition patterns of photon radiation with different energies (29 kV, 220 kV X rays; Co-60, Cs-137-gamma-rays) and alpha-radiation from an Am-241 source differ in DNA damage induction capacity in human cells. For this purpose, the alkaline comet assay (single cell gel electrophoresis) was applied to measure the amount of DNA damage in relation to the dose received. The comet assay data for the parameters '% DNA in the tail' and 'tail moment' for human peripheral lymphocytes did not indicate any difference in the initial radiation damage produced by 29 kV X rays relative to the reference radiations, 220 kV X rays and the gamma rays, whether for the total mean dose range of 0-3 Gy nor in the low-dose range. In contrast, when the 'tail length' data were analysed saturation of the fitted dose response curve appeared for X rays at about 1.5 Gy but was not apparent for gamma rays up to 3 Gy. Preliminary data for alpha exposures of HSC45-M2 cells showed a significant increase in DNA damage only at high doses (>2 Gy Am-241), but the damage at 2 Gy exceeded the damage induced at 2 Gy by Cs-137-gamma-rays by a factor of 2.5. In contrast, other experiments involving different cell systems and DNA damage indicators such as chromosomal aberrations have detected a significant increase in DNA damage at much lower doses, that is at 0.02 Gy for Am-241 and depicte a higher biological effectiveness. These results indicate that differences in biological effects arise through downstream processing of complex DNA damage.