Heliotropium procubens Mill: Taxonomic Significance and Characterization of Phenolic Compounds via UHPLC-HRMS- In Vitro Antioxidant and Enzyme Inhibitory Activities.

The aim of the present study was the phytochemical analysis of the aerial parts of Heliotropium procumbens Mill., a herb from Boraginaceae plant family not previously studied. The methanol (ME) and aqueous extracts (WE) of the aerial parts were assayed for their total phenolic and flavonoid content and antioxidant properties, using free radical scavenging (DPPH, ABTS), reducing power (FRAP, CUPRAC), phosphomolybdenum and metal chelating assays. The extracts displayed considerable free radical scavenging activity against DPPH and ABTS radicals, with potential values of 46.88 and 68.31 mg TE/g extract for ME, and 93.43 and 131.48 mg TE/g extract for WE, respectively. Key clinical enzymes involved in neurodegenerative diseases AChE and BChE, diabetes (α-amylase and α-glucosidase) and skin whitening (tyrosinase) were also assayed. The phytochemical profile of the studied species was determined through UHPLC-HRMS, whereby 26 secondary metabolites were identified, three of which (luteolin-7-glucoside, lithospermic and rosmarinic acids) were isolated and structurally determined by NMR spectral means. H. procubens was found to harbor bioactive metabolites and could, hence, serve as a source of biological activities which could be further explored and exploited for potential applications.

Hypericum Essential Oils-Composition and Bioactivities: An Update (2012-2022).

Hypericum genus, considered to comprise over 500 species that exhibit cosmopolitan distribution, has attracted human interest since ancient times. The present review aims to provide and summarize the recent literature (2012-2022) on the essential oils of the title genus. Research articles were collected from various scientific databases such as PubMed, ScienceDirect, Reaxys, and Google Scholar. Scientific reports related to the chemical composition, as well as the in vitro and in vivo pharmacological activities, are presented, also including a brief outlook of the potential relationship between traditional uses and Hypericum essential oils bioactivity.

Nutri-epigenetics and synthetic analogs in cancer chemoprevention.

Nutri-epigenetics has lately emerged as a new field in cancer epigenetic research. Cancer represents a multistage and heterogeneous disease that is driven by progressive genetic and epigenetic abnormalities. Epigenetic activity is influenced by several exogenous and endogenous factors including, nutrition, environment, disease, ethnicity, life style, medication, toxins, physical activity, age, gender and family genetics. Epigenetic therapy including mainly natural phenolics is a new area for drug development in cancer prevention. The current generation of epigenetic synthetic analogs are primarily target to inhibit the activity and expression of methyltransferases and histone deacetylases. Epigenetic mechanisms underlying nutrition seem very important tools nowadays in further understanding human health in general. New targeted natural and synthetic agents, along with the application of modern genomic methods, could substantially offer more specific armamentarium towards the prevention and therapy of cancer. The present short review demonstrates a selection of natural and recent synthetic chemopreventing compounds, in relation to their epigenetic mechanisms and current/future uses/limitations in therapeutics.

Photocatalytic and photoelectrocatalytic degradation of the antibacterial agent ciprofloxacin.

Photocatalytic and photoelectrocatalytic degradation of the antibacterial fluoroquinolone drug, ciprofloxacin, has been studied in the presence of nanocrystalline titania films supported on glass slides or transparent electrodes. The degradation has been examined either in pure water or in the presence of NaOH or NaCl. Titania films can photocatalytically or photoelectrocatalytically degrade ciprofloxacin. In the presence of NaOH, the degradation rate was lower than in pure water and this is explained by the fact that at high pH values attraction of ciprofloxacin to the titania surface is discouraged. In the presence of NaCl, the degradation rate was the highest, thanks to Cl-based radicals which can be photocatalytically created by interacting with photogenerated holes. Application of a forward (anodic) bias increased the photodegradation rate in the presence of both electrolytes while a reverse (cathodic) bias decreased the photodegradation rate. Electrocatalytic effects, i.e. degradation of ciprofloxacin in the dark or in the absence of a photocatalyst under an applied bias of up to ±1.0 V vs. Ag/AgCl, were not detected in the case of NaOH and were of limited importance in the case of NaCl.

Antioxidant treatment strategies for hyperphenylalaninemia.

Hyperphenylalaninemia (HPA) leads to increased oxidative stress in patients with phenylketonuria (PKU) and in animal models of PKU. Early diagnosis and immediate adherence to a phenylalanine-restricted diet prevents HPA and, consequently, severe brain damage. However, treated adolescent and adult PKU patients have difficulties complying with the diet, leading to an oscillation of phenylalanine levels and associated oxidative stress. The brain is especially susceptible to reactive species, and oxidative stress might add to the impaired cognitive function found in these patients. The restricted PKU diet has a very limited nutrient content from natural foods and almost no animal protein, which reduces the intake of important compounds. These specific compounds can act as scavengers of reactive species and can be co-factors of antioxidant enzymes. Supplementation with nutrients, vitamins, and tetrahydropterin has given quite promising results in patients and animal models. Antioxidant supplementation has been studied in HPA, however there is no consensus about its always beneficial effects. In this way, regular exercise could be a beneficial addition on antioxidant status in PKU patients. A deeper understanding of PKU molecular biochemistry, and genetics, as well as the need for improved targeted treatment options, could lead to the development of new therapeutic strategies.

Acute myeloid leukaemia: recent data on prognostic gene mutations, in relation to stratified therapies for elderly patients.

TET2 protein is encoded by the gene TET2 which specifically catalyses the demethylation of 5-methylcytosine to cytosine. Mutations in TET2 have been identified in a number of haematological malignancies, including leukaemias and lymphomas. In acute myeloid leukaemia (AML), loss of TET2 function drives DNA methylation and gene silencing, contributing to disease pathogenesis and progression, making it an interesting target. Although such mutations are considered rare, there is an increasing body in the literature identifying them as unfavourable prognostic markers in AML. The hypomethylating agent nucleoside analogue 5-azacytidine is used in the treatment of AML and other haematological malignancies i.e. myelodysplastic syndrome (MDS). It functions by re-activating silenced genes is responsible for cytosine methylation, thereby driving differentiation and also promoting apoptosis of dysfunctional haematological cells. The present review article deals with the consequences of DNA methylation in relation to TET2 in AML, focusing on the potential prognostic effect of TET2 gene mutations, along with demethylating epigenetic strategies towards prediction of therapeutic response. The necessity for personalized therapeutic regimes, especially for older patients suffering from AML with mutated TET2 and/or other genetic alterations, along with its prognostication are also underlined.

Chemical constituents from Cordia alliodora and C. colloccoca (Boraginaceae) and their biological activities.

Two new natural products, 5-O-[ß-D-apiofuranosyl-(1→6)-ß-d-glucopyranosyl]-1-isoindolinone (1) as well as N-(2E)-3-[(2S,3R)-2-(4-hydroxy-3-methoxyphenyl)-3-(hydroxymethyl)-7-methoxy-2,3-dihydro-1-benzofuran-5-yl]acryloylglycine (2), along with four known compounds (3-6), were isolated from the methanolic extract of Cordia alliodora root bark. Furthermore, the methanolic extract of Cordia colloccoca leaves, afforded the known flavonoids afzelin (7) and quercitrin (8). The isolated secondary metabolites were assayed for their antimicrobial activities against a panel of 6g positive and negative bacteria and three human pathogenic fungi. Moreover, their antiproliferative effect was also evaluated in vitro against the human non-small-cell bronchopulmonary carcinoma line NSCLC-N6, the epidermoid lung cancer cell line A549 as well as the normal human skin fibroblast cell line (AG01523).

Photocatalytic and photoelectrocatalytic degradation of the drug omeprazole on nanocrystalline titania films in alkaline media: Effect of applied electrical bias on degradation and transformation products.

Photocatalytic and photoelectrocatalytic degradation of the drug omeprazole has been studied in the presence of nanocrystalline titania films supported on glass slides or transparent FTO electrodes in alkaline environment. Its photocatalytic degradation rate was assessed by its UV absorbance and by HPLC, while its transformation products were analyzed by HR-LC-MS. Based on UV absorbance, omeprazole can be photocatalytically degraded at an average rate of 6.7×10(-4)min(-1) under low intensity UVA irradiation of 1.5mWcm(-2) in the presence of a nanoparticulate titania film. This corresponds to degradation of 1.4mg of omeprazole per gram of the photocatalyst per liter of solution per hour. The photodegradation rate can be accelerated in a photoelectrochemical cell by applying a forward bias. In this case, the maximum rate reached under the present conditions was 11.6×10(-4)min(-1) by applying a forward bias of +0.6V vs. Ag/AgCl. Four major transformation products were successfully identified and their profiles were followed by HR-LC-MS. The major degradation path includes the scission of the sulfoxide bridge into the corresponding pyridine and benzimidazole ring derivates and this is accompanied by the release of sulfate anions in the reaction mixture.