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The use of diversified raw materials and various extractant types is justified because the varied chemical composition of extracts obtained via extraction determines their biological activity. Therefore, the objective of this study was (i) to characterize the chemical profile of two types of bearberry extracts (70% ethanolic and water) and (ii) to investigate the biological activity of the analyzed extracts through an assessment of their possible proapoptotic effects on glioma cell lines. The HPLC-UV analysis of individual compounds was performed for the determination of the phytochemical profile of the bearberry extracts, and their total phenolic content (TPC) and total flavonoid content (TFC) were determined spectrophotometrically. The induction of apoptosis, autophagy, and necrosis in anaplastic astrocytoma MOGGCCM and human glioblastoma LN229 cell lines were investigated. The results indicated that the ethanolic (Et) and aqueous (Aq) extracts had different chemical profiles. The TPC in the Et was ca. 60% higher than in the Aq. Similarly, the TFC and methylarbutin (mARB) concentrations were significantly higher in the Et. On the other hand, the concentration of hydroquinone (HQ) was ca. 70% and that of corilagin (COR) was ca. 100% higher in the Aq. In turn, the presence of ursolic acid (UA) and oleanolic acid (OA) was confirmed solely in the Et. In contrast to Aq, Et demonstrated high proapoptotic activity. At the concentration of 2 µL/mL, the level of apoptosis varied between 14.7% and 26% in the case of the MOGGCCM cells and between 12.3% and 33.3% in the case of the LN229 cell line. The knowledge and information obtained in this study indicate a need for further research on the anticancer effect of the studied bearberry phytochemicals on the MOGGCCM and LN229 cell lines and for the elucidation of their molecular anticancer mechanisms. [ABSTRACT FROM AUTHOR]

Arabinogalactan proteins (AGPs) are proteoglycans with an unusual molecular structure characterised by the presence of a protein part and carbohydrate chains. Their specific properties at different stages of the fruit ripening programme make AGPs unique markers of this process. An important function of AGPs is to co-form an amorphous extracellular matrix in the cell wall-plasma membrane continuum; thus, changes in the structure of these molecules can determine the presence and distribution of other components. The aim of the current work was to characterise the molecular structure and localisation of AGPs during the fruit ripening process in transgenic lines with silencing and overexpression of SlP4H3 genes (prolyl 4 hydroxylase 3). The objective was accomplished through comprehensive and comparative in situ and ex situ analyses of AGPs from the fruit of transgenic lines and wild-type plants at specific stages of ripening. The experiment showed that changes in prolyl 4 hydroxylases (P4H3) activity affected the content of AGPs and the progress in their modifications in the ongoing ripening process. The analysis of the transgenic lines confirmed the presence of AGPs with highmolecular weights (120-60 kDa) at all the examined stages, but a changed pattern of the molecular features of AGPswas found in the last ripening stages, compared to WT. In addition to the AGP molecular changes, morphological modifications of fruit tissue and alterations in the spatio-temporal pattern of AGP distribution at the subcellular level were detected in the transgenic lines with the progression of the ripening process. The work highlights the impact of AGPs and their alterations on the fruit cell wall and changes in AGPs associated with the progression of the ripening process. [ABSTRACT FROM AUTHOR]

Arnica montana L. is one of Europe's endemic endangered medicinal plants, with diverse biological activities commonly used in medicine, pharmacy, and cosmetics. Its flower heads are a rich source of raw material, with antibacterial, antifungal, antiseptic, anti-inflammatory, antiradical, antioxidant, and antitumor properties. The objective of the present study was (i) to characterize the chemical composition of flower heads of A. montana plants cultivated under nitrogen fertilization, (ii) to identify the impact of the nitrogen fertilization and extraction method (water, ethanol) on the antioxidant activity of extracts, and (iii) to determine the role of different nitrogen doses applied during plant cultivation and different extraction methods in the anticancer activity of the extracts through analysis of apoptosis and autophagy induction in HT29, HeLa, and SW620 cell lines. The present study shows that nitrogen is a crucial determinant of the chemical composition of arnica flower heads and the antioxidant and anticancer activity of the analyzed extracts. Nitrogen fertilization can modify the composition of pharmacologically active substances (sesquiterpene lactones, flavonoids, essential oil) in Arnicae flos. The content of sesquiterpene lactones, flavonoids, and essential oil increased with the increase in the nitrogen doses to 60 kg N ha−1 by 0.66%, 1.45%, and 0.27%, respectively. A further increase in the nitrogen dose resulted in a decrease in the content of the analyzed secondary metabolites. Varied levels of nitrogen application can be regarded as a relevant way to modify the chemical composition of arnica flower heads and to increase the anticancer activity, which was confirmed by the increase in the level of apoptosis with the increase in fertilization to a level of 60 kg N ha−1. The fertilization of arnica plants with low doses of nitrogen (30 and 60 kg N ha−1) significantly increased the LOX inhibition ability of the ethanol extracts. The present study is the first report on the anticancer activity of A. montana water extracts, with emphasis on the role of water as a solvent. In further studies of factors modifying the quality of Arnicae flos, attention should be paid to the simultaneous use of nitrogen and other microelements to achieve synergistic results and to the possibility of a more frequent use of water as a solvent in studies on the biological activity of A. montana extracts. [ABSTRACT FROM AUTHOR]

ABSTRACT A new procedure for the synthesis of optically active t-butylophenylphosphinothioic acid as an enantiomerically pure dextrorotatory enantiomer having the absolute configuration ( R), by a reaction of the racemate of secondary t-butylphenylphosphine oxide with elemental sulfur in the presence of a molar equivalent of the levorotatory enantiomer of enantiomerically pure ( S)-α-phenylethylamine, is reported. It is obvious that with the use of the dextrorotatory enantiomer of α-phenylethylamine, the levorotatory enantiomer of this thioacid will be isolated. [ABSTRACT FROM AUTHOR]

Attempts at functionalization of fullerene C60with stereogenicS-(t-butylphenyl) phosphinyl or (α-p-toluenesulfinyl)methyl substituents are presented. [ABSTRACT FROM AUTHOR]

Neoplasm diseases are one of the main causes of death in Poland and worldwide. Forming and progression of tumour are regulated by the number of factors, among which one of the most important are matrix metalloproteinases (MMPs), zinc-dependant proteases, responsible for remodeling of extracellular matrix (ECM). They may induce cancer progression directly by modifying the ECM, enabling cancer growth and migrating of cells released from tumour, as well as invading adjacent tissue and blood or lymphatic vessels. MMPs may also induce carcinogenesis in indirect way by modifying tumour microenvironment and secreting factors promoting or inhibiting particular processes. There is number of factors secreted by cancer cells, stromal components and ECM elements regulating activation and functionality of matrix metalloproteinases. Understanding the mechanisms and pathways underlying regulation and activation of MMPs is crucial for comprehension of carcinogenesis and metastasis, and may contribute to developing of new therapeutic strategies.