Bioactive constituents from Tinospora cordifolia (willd.): Isolation, synthesis and their immunomodulatory activity.

Traditional medicinal plants have been used for centuries for their immunomodulatory properties and therapeutic potentials. The present study aims to investigate the immunomodulatory constituents from traditional medicinal plant, Tinospora cordifolia (willd.). Our study resulted in the isolation of new compound, 27-hydroxy octacosyl ferulate (1) along with eleven known compounds (2-12). The structures of the isolated compounds were characterized by combination of NMR (1D and 2D) and Mass spectroscopic methods. The hemisynthesis of compound 12 (ferulic acid) yielded (12a-12d and 12e-12 m) derivatives. Further, the isolated compounds and synthesized derivatives were assessed for their immunomodulatory potentials by evaluating their cytotoxicity and pro-inflammatory effects against macrophage cells (IL-6) and DC activation markers (CD 11c and 86). The biological results indicated that crude extract displayed potent immunomodulatory activity while isolated compounds and synthetic analogues showed moderate activity. Among the tested compounds, new compound (1), quercetin (10) and derivatives 12b, 12c found to be non-cytotoxic and displayed immunomodulatory potentials. Therefore, these compounds can be studied for autoimmunity and other immune suppressing conditions.

Isolation and Biological Characterization of Homoisoflavanoids and the Alkylamide N-p-Coumaroyltyramine from Crinum biflorum Rottb., an Amaryllidaceae Species Collected in Senegal.

Crinum biflorum Rottb. (syn. Crinum distichum) is an Amaryllidaceae plant used in African traditional medicine but very few studies have been performed on this species from a chemical and applicative point of view. Bulbs of C. biflorum, collected in Senegal, were extracted with ethanol by Soxhlet and the corresponding organic extract was purified using chromatographic methods. The pure compounds were chemically characterized by spectroscopic techniques (1D and 2D 1H and 13C NMR, HR MS and ECD) and X-ray analysis. Four homoisoflavonoids (1-4) and one alkylamide (5) were isolated and characterized as 5,6,7-trimethoxy-3-(4-hydroxybenzyl)chroman-4-one (1), as 3-hydroxy-5,6,7-trimethoxy-3-(4-hydroxybenzyl)chroman-4-one (2), as 3-hydroxy-5,6,7-trimethoxy-3-(4-methoxybenzyl)chroman-4-one (3) and as 5,6,7-trimethoxy-3-(4-methoxybenzyl)chroman-4-one (4), and the alkylamide as (E)-N-(4-hydroxyphenethyl)-3-(4-hydroxyphenyl)acrylamide (5), commonly named N-p-coumaroyltyramine. The relative configuration of compound 1 was verified thanks to the X-ray analysis which also allowed us to confirm its racemic nature. The absolute configurations of compounds 2 and 3 were assigned by comparing their ECD spectra with those previously reported for urgineanins A and B. Flavanoids 1, 3 and 4 showed promising anticancer properties being cytotoxic at low micromolar concentrations towards HeLa and A431 human cancer cell lines. The N-p-coumaroyltyramine (5) was selectively toxic to A431 and HeLa cancer cells while it protected immortalized HaCaT cells against oxidative stress induced by hydrogen peroxide. Compounds 1-4 also inhibited acetylcholinesterase activity with compound 3 being the most potent. The anti-amylase and the strong anti-glucosidase activity of compound 5 were confirmed. Our results show that C. biflorum produces compounds of therapeutic interest with anti-diabetic, anti-tumoral and anti-acetylcholinesterase properties.

Air frying pretreatment and the recovery of lipophilic sinapates from the oil fraction of mustard samples.

Roasting of mustard seeds prior to oil extraction is a well-documented unit operation essential to produce canolol and other lipophilic sinapates. This study investigated the effectiveness of air frying as a seed roasting treatment operation for enhancing the recovery of lipophilic sinapates from various mustard samples and fractions/products. Air frying of seeds, powder, cake, bran, and flour from different mustard varieties was carried out at temperature-time combinations of 160, 170, and 180°C for 5, 10, 15, and 20 min, respectively. Oil was extracted using the Soxtec method. Lipophilic sinapates were extracted from the oil using equal volumes of hexane to methanol 70% (v/v) and quantified by high performance liquid chromatography-diode array detection (HPLC-DAD). The total phenolic content (TPC) and antioxidant activity of the oils were also evaluated. The results showed a time-temperature dependency for the recovery of major oil-soluble sinapates in all mustard samples and fractions. The optimum air frying condition 180°C for 15 min produced the maximum yield of canolol as well as other unidentified oil-soluble sinapates (retention time (RT)-7.7, RT-11.50, RT-14.95, and RT-16.24 min). The oil from lower grade yellow mustard seeds (LGYMS) roasted at 180°C for 20 mins specifically had the highest TPC (3402.22 ± 58.79 mg GAE/g oil), while LGYMS oils generally showed better antioxidant activities (2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric ion reducing antioxidant power (FRAP), and inhibition of linoleic acid oxidation) but were lower in metal ion chelating capacity. This information would be beneficial to the oil industry because air frying generated valuable canolol and other antioxidant lipophilic sinapates from mustard varieties and their fractions. PRACTICAL APPLICATION: A major limitation in the application of natural extracts in vegetable oils is the poor lipophilic nature of phenolic compounds. This study employed a new thermal treatment (air frying) in the recovery of canolol and other lipophilic antioxidants. Such treatments can enrich mustard-based ingredients with canolol and other lipophilic antioxidants for domestic and industrial applications.

Prenylated Coumaric Acids from Artemisia scoparia Beneficially Modulate Adipogenesis.

Two new diprenylated coumaric acid isomers (1a and 1b) and two known congeners, capillartemisin A (2) and B (3), were isolated from Artemisia scoparia as bioactive markers using bioactivity-guided HPLC fractionation. Their structures were determined by spectroscopic means, including 1D and 2D NMR methods and LC-MS, with their purity assessed by 1D 1H pure shift qNMR spectroscopic analysis. The bioactivity of compounds was evaluated by enhanced accumulation of lipids, as measured using Oil Red O staining, and by increased expression of several adipocyte marker genes, including adiponectin in 3T3-L1 adipocytes relative to untreated negative controls. Compared to the plant's 80% EtOH extract, these purified compounds showed significant but still weaker inhibition of TNFα-induced lipolysis in 3T3-L1 adipocytes. This suggests that additional bioactive substances are responsible for the multiple metabolically favorable effects on adipocytes observed with Artemisia scoparia extract.

Selective Extraction of Sinapic Acid Derivatives from Mustard Seed Meal by Acting on pH: Toward a High Antioxidant Activity Rich Extract.

The aim of this paper is to study the effect of the pH on the extraction of sinapic acid and its derivatives from mustard seed meal. Solutions of acidic pH (pH 2), basic pH (pH 12) and distilled water (uncontrolled pH ~ 4.5) were tested at different percentages of ethanol. The maximum extraction yield for sinapic acid (13.22 µmol/g of dry matter (DM)) was obtained with a buffered aqueous solution at pH 12. For ethyl sinapate, the maximum extraction yield reached 9.81 µmol/g DM with 70% ethanol/buffered aqueous solution at pH 12. The maximum extraction yield of sinapine (15.73 µmol/g DM) was achieved with 70% ethanol/buffered aqueous solution at pH 2. The antioxidant activity of each extract was assessed by DPPH assay; the results indicated that the extracts obtained at pH 12 and at low ethanol percentages (<50%) exhibit a higher antioxidant activity than extracts obtained at acidic conditions. Maximum antioxidant activity was reached at pH 12 with buffer solution (11.37 mg of Trolox Equivalent/g DM), which confirms that sinapic acid-rich fractions exhibit a higher antioxidant activity. Thus, to obtain rich antioxidant extracts, it is suggested to promote the presence of sinapic acid in the extracts.

Isolation and characterization of opuntiol from Opuntia Ficus indica (L. Mill) and its antiproliferative effect in KB oral carcinoma cells.

In this study, we isolated and characterized a novel bioactive flavonol from the cactus pad of Opuntia Ficus indica Indica (L. Mill) (OFI) by chromatography techniques. The isolated compound was characterized by FT-IR, 1H and 13C NMR spectroscopy. Single-crystal XRD results illustrate that the obtained flavonol was opuntiol (6-hydroxymethyl-4-methoxy-2H-pyran-2-one) and it was found to be near planar except for the H atoms of the methylene and methyl groups. The crystal packing was stabilized by C-H….O and O-H….O intermolecular hydrogen bonds. The isolated opuntiol significantly inhibited KB cells proliferation and its IC50 value was found to be 30 µM. Further, we noticed that opuntiol significantly induced ROS generation and subsequently altered MMP in KB cells. Western blot analysis and morphological observations by fluorescence microscope indicate the apoptotic inducing potential of opuntiol in KB cells.

Accessing p-Hydroxycinnamic Acids: Chemical Synthesis, Biomass Recovery, or Engineered Microbial Production?

p-Hydroxycinnamic acids (i. e., p-coumaric, ferulic, sinapic, and caffeic acids) are phenolic compounds involved in the biosynthesis pathway of lignin. These naturally occurring molecules not only exhibit numerous attractive properties, such as antioxidant, anti-UV, and anticancer activities, but they also have been used as building blocks for the synthesis of tailored monomers and functional additives for the food/feed, cosmetic, and plastics sectors. Despite their numerous high value-added applications, the sourcing of p-hydroxycinnamic acids is not ensured at the industrial scale except for ferulic acid, and their production cost remains too high for commodity applications. These compounds can be either chemically synthesized or extracted from lignocellulosic biomass, and recently their production through bioconversion emerged. Herein the different strategies described in the literature to produce these valuable molecules are discussed.

Gastric healing effect of p-coumaric acid isolated from Baccharis dracunculifolia DC on animal model.

The p-coumaric acid is a phenolic compound present in large quantities in the extract of Baccharis dracunculifolia DC, a Brazilian medicinal plant used to treat gastric ulcer. Given the necessity for finding new chemical components capable of accelerating gastric healing, in this study, the effects of the p-coumaric acid were evaluated in the acetic acid-induced ulcer model in rats, where histological, inflammatory, and oxidative parameters were analyzed. The healing property was also evaluated in the scratch assay on fibroblast cells (L929) and the cytotoxicity of p-coumaric acid was assessed in both L929 and human gastric adenocarcinoma (AGS) cells by MTT assay. The treatment with p-coumaric acid (10 mg/kg, p.o.) for 7 days, twice a day, decreased by 44.6% the acetic acid-induced gastric ulcer compared with the vehicle-treated group. The vehicle control-treated group showed a larger extension of the ulcer base and an extensive damage into the mucosa and submucosa layers, which were mitigated by the treatment with p-coumaric acid. This beneficial effect was also associated with increased levels of mucin and reduced glutathione, decreased amount of lipid hydroperoxides, and increased superoxide dismutase and catalase activities without interfering with the activity of myeloperoxidase in the gastric tissue. The compound promoted the restructuring of the cell monolayer in the scratch test and did not show toxicity in the L929 cell line, while reduced the viability of the AGS, a lineage of human gastric adenocarcinoma. Thus, p-coumaric acid may be considered a natural source for the treatment of gastric ulcers, by reinforcing protective factors of gastric mucosa and by accelerating gastric healing.

A new ent-abietane lactone from Glycosmis pentaphylla.

A new ent-abietane lactone, 3-oxojolkinolide A (1), together with 16 known compounds, helioscopinolide E (2), helioscopinolide A (3), 3-methyl-9H-carbazole (4), carbalexin (5), carbalexin B (6), glycaborinine (7), arborinine (8), 1H-indole-3-carbaldehyde (9), glycoamide A (10), glycoamide B (11), 2-(N-methyl-2-phenylacetamido)benzoic acid (12), 2-(methylamine)-methylbenzoate (13), fraxidin (14), scopoletin (15), (-)-syringaresinol (16) and ferulic acid (17) were isolated from Glycosmis pentaphylla. The structures of these compounds were elucidated using spectroscopic techniques such as NMR and MS. Among them, compounds 1-3, 9 and 12-17 were isolated from the genus Glycosmis for the first time.

Health Properties and Composition of Honeysuckle Berry Lonicera caerulea L. An Update on Recent Studies.

Lonicera caerulea L., also known as haskap or honeysuckle berry, is a fruit commonly planted in eastern Europe, Canada and Asia. The fruit was registered as a traditional food from a third country under European Union regulations only on December 2018. It is resistant to cold, pests, various soil acidities and diseases. However, its attractiveness is associated mostly with its health properties. The fruit shows anticancer, anti-inflammatory, and antioxidant activity-important factors in improving health. These features result from the diverse content of phytochemicals in honeysuckle berries with high concentrations of phytocompounds, mainly hydroxycinnamic acids, hydroxybenzoic acids, flavanols, flavones, isoflavones, flavonols, flavanones and anthocyanins but also iridoids, present in the fruit in exceptional amounts. The content and health properties of the fruit were identified to be dependent on cultivar, genotype and the place of harvesting. Great potential benefits of this nutritious food are its ability to minimize the negative effects of UV radiation, diabetes mellitus and neurodegenerative diseases, and to exert hepato- and cardioprotective activity.

Advances in combined enzymatic extraction of ferulic acid from wheat bran.

Wheat bran could be utilised as feedstock for innovative and sustainable biorefinery processes. Here, an enzymatic hydrolysis process for ferulic acid (FA) extraction was optimised step by step for total wheat bran (Tritello) and then also applied to the outer bran layer (Bran 1). Proteins, reducing sugars, total phenols and FA were quantified. The highest FA yields (0.82-1.05 g/kg bran) were obtained either by rehydrating the bran by autoclaving (Tritello) or by steam explosion (Bran 1) using a bran/water ratio of 1:20, followed by enzymatic pre-treatment with Alcalase and Termamyl, to remove protein and sugars, and a final enzymatic hydrolysis with Pentopan and feruloyl esterase to solubilise phenol. FA was recovered from the final digestate via solid phase extraction. A 40-fold scale-up was also performed and the release of compounds along all the process steps and at increasing incubation times was monitored. Results showed that FA was initially present at a minimum level while it was specifically released during the enzymatic treatment. In the final optimized process, the FA extraction yield was higher than that obtained with NaOH control hydrolysis while, in comparison with other FA enzymatic extraction methods, fewer process steps were required and no buffers, strong acid/alkali nor toxic compounds were used. Furthermore, the proposed process may be easily scaled-up, confirming the feasibility of wheat bran valorisation by biorefinery processes to obtain valuable compounds having several areas of potential industrial exploitation.

Purification of Polyphenols from Distiller's Grains by Macroporous Resin and Analysis of the Polyphenolic Components.

We aimed to purify polyphenols from distiller's grain extract using macroporous resins and to identify its polyphenolic components. The influence of operational parameters on purification efficiency was investigated. The polyphenolic composition was analyzed by ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) and then quantified by UPLC-MS using authenticated standards. The results showed that the optimal purifying conditions were D101 resin with a dosage of 3 g, four hours adsorption, three hours desorption time, and 60% ethanol as the eluent, producing the highest purification rate of 51%. The purified distiller's grain extract exhibited stronger antioxidant activity than the unpurified extracts, which was assessed using DPPH and ABTS methods (IC50 DPPH = 34.03 and 16.21 µg/mL, respectively; IC50 ABTS = 20.31 and 5.73 µg/mL, respectively). UPLC-MS results indicated that (-)-epicatechin is the major compound found in distiller's grain extract which was quantified as 562.7 µg/g extract, followed by ferulic acid (518.2 µg/g), p-hydroxybenzoic acid (417.7 µg/g), caffeic acid (217.1 µg/g), syringic acid (158.0 µg/g) and quercetin (147.8 µg/g). Two compounds, vanillic acid (66.5 µg/g) and gallic acid (41.4 µg/g), were found in lower concentrations. The findings of this study suggest that purification of polyphenolic compounds from distiller's grain by macroporous resins is feasible, providing a new and effective method for the secondary use of distiller's grain resources.

Influence of Temperature, Solvent and pH on the Selective Extraction of Phenolic Compounds from Tiger Nuts by-Products: Triple-TOF-LC-MS-MS Characterization.

The aim of this study was to assess the effect of temperature, solvent (hydroethanolic mixtures) and pH on the recovery of individual phenolic compounds from "horchata" by-products. These parameters were optimized by response surface methodology and triple-TOF-LC-MS-MS was selected as the analytical tool to identify and quantify the individual compounds. The optimum extraction conditions were 50% ethanol, 35 °C and pH 2.5, which resulted in values of 222.6 mg gallic acid equivalents (GAE)/100 g dry matter and 1948.1 µM trolox equivalent (TE)/g of dry matter for total phenolic content (TPC) and trolox equivalent antioxidant capacity (TEAC), respectively. The extraction of phenolic compounds by the conventional solvent method with agitation was influenced by temperature (p = 0.0073), and more strongly, by the content of ethanol in the extraction solution (p = 0.0007) while the pH did not show a great impact (p = 0.7961). On the other hand, the extraction of phenolic acids was affected by temperature (p = 0.0003) and by ethanol amount (p < 0.0001) but not by the pH values (p = 0.53). In addition, the percentage of ethanol influenced notably the extraction of both 4-vinylphenol (p = 0.0002) and the hydroxycinnamic acids (p = 0.0039). Finally, the main individual phenolic extracted with hydroethanolic mixtures was 4-vinylphenol (303.3 µg/kg DW) followed by spinacetin3-O-glucosyl-(1→6)-glucoside (86.2 µg/kg DW) and sinensetin (77.8 µg/kg DW).

Wheat phenolics suppress doxorubicin-induced cardiotoxicity via inhibition of oxidative stress, MAP kinase activation, NF-κB pathway, PI3K/Akt/mTOR impairment, and cardiac apoptosis.

The present investigation has been undertaken to reveal the protective mechanism of polyphenolics extract of whole wheat grains (WWGPE), ferulic acid and apigenin against doxorubicin (Dox)-induced cardio-toxicity. WWGPE, apigenin, and ferulic acid exhibited concentration dependent cyto-protective effect against Dox (1 µM) in rat cardiomyocytes. Dox treatment significantly (p < 0.01) induced oxidative stress in the myocardial cells via excessive ROS production, increase in iNOS expression, NADPH oxidase activation, Nrf-2/HO-1 impairment, and inactivation of cellular redox defense system. In addition, Dox significantly (p < 0.01) activated MAP kinases, NF-κB, and apoptosis in cardiac cells; while, significant (p < 0.01) impairment in PI3K/Akt/mTOR signaling was observed in Dox-treated myocardial cells. On the other hand, WWGPE, apigenin, and ferulic acid significantly (p < 0.05-0.01) attenuated Dox-induced redox stress and oxidative stress-mediated signal transduction in myocardial cells. WWGPE, apigenin, and ferulic acid treatment also could significantly (p < 0.05-0.01) reinstate Dox-mediated changes in blood parameters in rats. Histological assessments were in agreement with the biochemical findings. Results showed that, WWGPE exhibited better cardio-protective effect over ferulic acid and apigenin, which may be due to the synergy between the comprising compounds and better oral bioavailability of dietary antioxidant molecules from whole phenolic extract.

4-methoxycinnamyl p-coumarate isolated from Etlingera pavieana rhizomes inhibits inflammatory response via suppression of NF-κB, Akt and AP-1 signaling in LPS-stimulated RAW 264.7 macrophages.

BACKGROUND: 4-methoxycinnamyl p-coumarate (MCC) was isolated from rhizomes of Etlingera pavieana by bioactivity-guided isolation, however, the molecular mechanism underlying its anti-inflammatory activity remains inadequately understood. PURPOSE: In this study, we elucidated the suppressive effect of MCC on LPS-induced expression of inflammatory mediators and the molecular mechanisms responsible for anti-inflammatory activities in RAW 264.7 macrophages. METHODS: Cell viability of MCC-treated RAW 264.7 macrophage was measured by MTT assay. Anti-inflammatory activity was evaluated by measurement of NO, PGE2, and cytokine production in LPS-stimulated cells. qRT-PCR and Western blotting analysis were used to investigate mRNA and protein levels of inflammatory responsive genes. NF-κB activation and transactivation activity were determined by immunofluorescence and reporter gene assay, respectively. RESULTS: MCC considerably suppressed both the production of NO, PGE2, IL-1ß as well as TNF-α and their expression. MCC inactivated NF-κB by reducing phosphorylation of IκBα and inhibiting NF-κB p65 nuclear translocation. Also, MCC significantly inhibited NF-κB transactivation activity. However, the inhibitory effect of MCC was independent of the MAPK signaling pathway. Furthermore, MCC significantly decreased phosphorylation of Akt and c-Jun, a main component of AP-1. CONCLUSION: These findings suggest that the anti-inflammatory effect of MCC could be mediated by the inhibition of LPS-induced expression of inflammatory mediators by down-regulation of the NF-κB, Akt and AP-1 signaling pathways in murine macrophages.

Identification of Six Phytochemical Compounds from Asparagus officinalis L. Root Cultivars from New Zealand and China Using UAE-SPE-UPLC-MS/MS: Effects of Extracts on H2O2-Induced Oxidative Stress.

A simple, rapid, specific, and sensitive method was developed for the simultaneous identification and quantification of six major bioactive compounds, namely, caffeic acid, quercetin, apigenin, ferulic acid, baicalein, and kaempferol, from Asparagus officinalis roots (ARs) native to New Zealand (green and purple cultivars) and China (yellow, green, purple, and white cultivars) using ultrasound-assisted, solid-phase extraction (UASE-SPE) coupled with ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). The method was validated in terms of linearity, limit of detection (LOD), limit of quantification (LOQ), accuracy (expressed as recovery %), and precision (expressed as relative standard deviation (%RSD)). The retention times, ultraviolet visible (UV-vis) data, and mass spectral patterns of the detected peaks matched those of commercial standards, allowing characterization of the target compounds. The LODs and LOQs were 23 ng/mL and 70 ng/mL, 50 ng/mL and 150 ng/mL, 10 ng/mL and 30 ng/mL, 18 ng/mL and 54 ng/mL, 14.4 ng/mL and 43.6 ng/mL, and 7.5 ng/mL and 22.5 ng/mL for caffeic acid, quercetin, apigenin, ferulic acid, baicalein, and kaempferol, respectively, and the mean recovery rates were 85.8%, 73.0%, 90.2%, 80.6%, 76.7%, and 74.5% for the six compounds, respectively. The levels of the target compounds were significantly different (p < 0.05) among the six cultivars. The Chinese yellow AR had the highest levels of bioactive compounds: 6.0, 3.9, 0.4, 1.0, 0.86, and 0.8 mg/g for caffeic acid, quercetin, apigenin, ferulic acid, baicalein, and kaempferol, respectively. The AR extracts showed protective effects against oxidative stress in the HepG2 and L929 cell lines. The results indicate that AR extracts contain high flavonoid levels that provide protective functions against oxidative stress and support the potential commercial application of AR extracts.

Ferulic Acid Exerts Anti-apoptotic Effects against Ischemic Injury by Activating HSP70/Bcl-2- and HSP70/Autophagy-Mediated Signaling after Permanent Focal Cerebral Ischemia in Rats.

This study assessed the anti-apoptotic effects of the administration of ferulic acid (FrA) in rats 30 min before middle cerebral artery occlusion (MCAo) followed by 3 d of ischemia and the involvement of 70 kDa heat shock protein (HSP70)-mediated signaling in the penumbral cortex. Our results demonstrated that FrA pretreatment at doses of 80 mg/kg (FrA-80 mg) and 100 mg/kg (FrA-100 mg) effectively ameliorated neurological functions and reduced the numbers of cytochrome c-, cleaved caspase-3-, and terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL)-positive cells in the penumbral cortex 3 d after ischemia. Moreover, FrA-80 mg and FrA-100 mg pretreatment markedly upregulated cytosolic HSP70, Beclin-1, microtubule-associated protein 1 light chain 3 (LC3) A/B-II and autophagy-related protein 5 (Atg5) expression; cytosolic and mitochondrial X-linked inhibitor of apoptosis (XIAP) expression and the Bcl-2/Bax ratio. FrA pretreatment downregulated cytosolic cytochrome c, apoptosis-inducing factor (AIF), procathepsin B, and cathepsin B expression and mitochondrial and cytosolic second mitochondria-derived activator of caspase/direct inhibitor of apoptosis protein-binding protein with a low isoelectric point (Smac/DIABLO) expression in the penumbral cortex. Pretreatment with VER155008, a HSP70 family inhibitor, significantly inhibited the effects of FrA-100 mg on the expression of the aforementioned proteins expression in the penumbral cortex. FrA-80 mg and FrA-100 mg pretreatment exerts neuroprotective effects against caspase-dependent and -independent apoptosis through activating HSP70/Bcl-2- and HSP70/autophagy-induced signaling pathways. Furthermore, the HSP70/Bcl-2- and HSP70/autophagy-induced anti-apoptotic effects of FrA pretreatment can be attributed to the regulation of Bax/cytochrome c/Smac/DIABLO/XIAP/ caspase-3- (or Bax/AIF-) and Beclin-1/LC3A/B-II/Atg5-mediated signaling, respectively, in the penumbral cortex 3 d after permanent MCAo.

Phenolic Acids Derivatives - Biotechnological Methods of Synthesis and Bioactivity.

Phenolic acids are secondary plant metabolites belonging to polyphenol classes, widely spread throughout the plant kingdom. The name "phenolic acids", in general, describes phenols that possess one carboxylic acid functionality and they could be divided into three major subclasses: hydroxybenzoic, hydroxycinnamic and hydroxyphenylacetic acids. The great interest in phenolic acids is associated with their high potential for food preservation (antioxidant and antimicrobial activity) and, last but not least, high therapeutic potential. The aim of this review is to summarise the current knowledge concerning phenolic acids and the topics discussed include natural sources of phenolic acids, biosynthesis and metabolism, health benefits of phenolic acids (first of all the antioxidant activity of dietary phenolics and also anticarcinogenic and anti-inflammatory effect), their antimicrobial activity for selected groups of bacteria and fungi (yeasts) and structural modifications of the molecule especially those increasing lipophilicity and improving solubility in lipids. Recent advances in the methods of enzymatic synthesis of phenolic acid derivatives are described and some conclusions referring to Structure-Property-Activity Relationships of phenolic acids, particularly important from the point of view of their pharmaceutical and nutritional applications, are discussed.

Bioactivities of Phenolics by Focusing on Suppression of Chronic Diseases: A Review.

Phenolics, which are secondary metabolites of plants, exhibit remarkable bioactivities. In this contribution, we have focused on their protective effect against chronic diseases rather than their antioxidant activities, which have been widely discussed in the literature. A large body of epidemiological studies has proven the bioactivities of phenolics in both standard compounds and natural extracts: namely, anticancer, anti-inflammatory, and antibacterial activities as well as reducing diabetes, cardiovascular disease, and neurodegenerative disease. Phenolics also display anti-analgesic, anti-allergic, and anti-Alzheimer's properties. Thus, this review provides crucial information for better understanding the bioactivities of phenolics in foods and fills a gap in the existing collective and overall knowledge in the field.

Assessment of effects of phenolic fractions from leaves and petals of dandelion in selected components of hemostasis.

Aerial parts and roots of Taraxacum officinale (dandelion) have been found to be rich sources of polyphenols, including cinnamic acid derivatives, flavonoids and triterpenoids, which exert different biological activities, such as anti-inflammatory, anticancer and antimicrobial. Additionally, the whole plant is recognized as safe and well tolerated by humans, with no reported adverse effects. Nowadays, dandelion is a commonly available dietary supplement and a component of pharmaceutical preparations used for the treatment of bladder, liver, and spleen. Nevertheless, the effect of dandelion on blood platelets and plasma - components of hemostasis involved in the functioning of a cardiovascular system and linked with various cardiovascular diseases, has not been studied yet. Thus, the main objective of our in vitro experiments was to examine the anti-platelet and antioxidant properties of four standardized dandelion phenolic fractions, i.e. leaves 50% and 85% methanol fractions, and petals 50% and 85% methanol fractions, in blood platelets. Additionally, aforementioned plant preparations were investigated for hemostatic activity in plasma, using three selected hemostatic parameters: the activated partial thromboplastin time (APTT), prothrombin time (PT) and thrombin time (TT). None of the studied dandelion fractions, caused the damage of human blood platelets, at the whole tested range. The inhibition of lipid peroxidation in platelets treated with H2O2/Fe (the donor of OH) was observed for two fractions: leaves and petals 50% fractions, both at the dose 50 µg/mL. Analysis of the effect on the coagulation activity of human plasma demonstrated that three fractions: petals 50% fraction, and leaves and petals 85% fractions, significantly prolonged the thrombin time, at the whole tested range. On the contrary, none of the fractions changed the APTT and the PT. The obtained results demonstrate that dandelion preparations, based on aerial parts, especially rich in hydroxycinnamic acid derivatives (leaves and petals 50% fractions) are promising plant materials exerting both antioxidant and anticoagulant activities of the hemostatic system that is beneficial in the prevention and treatment of cardiovascular diseases.