47 research outputs found
Caffeic acid expands anti-tumor effect of metformin in human metastatic cervical carcinoma HTB-34 cells : implications of AMPK activation and impairment of fatty acids de novo biosynthesis
The efficacy of cancer treatments is often limited and associated with substantial toxicity. Appropriate combination of drug targeting specific mechanisms may regulate metabolism of tumor cells to reduce cancer cell growth and to improve survival. Therefore, we investigated the effects of anti-diabetic drug Metformin (Met) and a natural compound caffeic acid (trans-3,4-dihydroxycinnamic acid, CA) alone and in combination to treat an aggressive metastatic human cervical HTB-34 (ATCC CRL1550) cancer cell line. CA at concentration of 100 µM, unlike Met at 10 mM, activated 5'-adenosine monophosphate-activated protein kinase (AMPK). What is more, CA contributed to the fueling of mitochondrial tricarboxylic acids (TCA) cycle with pyruvate by increasing Pyruvate Dehydrogenase Complex (PDH) activity, while Met promoted glucose catabolism to lactate. Met downregulated expression of enzymes of fatty acid de novo synthesis, such as ATP Citrate Lyase (ACLY), Fatty Acid Synthase (FAS), Fatty Acyl-CoA Elongase 6 (ELOVL6), and Stearoyl-CoA Desaturase-1 (SCD1) in cancer cells. In conclusion, CA mediated reprogramming of glucose processing through TCA cycle via oxidative decarboxylation. The increased oxidative stress, as a result of CA treatment, sensitized cancer cells and, acting on cell biosynthesis and bioenergetics, made HTB-34 cells more susceptible to Met and successfully inhibited neoplastic cells. The combination of Metformin and caffeic acid to suppress cervical carcinoma cells by two independent mechanisms may provide a promising approach to cancer treatment
Zinc and propolis reduces cytotoxicity and proliferation in skin fibroblast cell culture : total polyphenol content and antioxidant capacity of propolis
It has been demonstrated that zinc exerts its beneficial influence on skin fibroblasts. Propolis, a complex mixture of plant-derived and bees’ products, was reported to stimulate cicatrization processes in skin and prevent infections. The aim of this study was to find out how zinc and propolis influence human skin fibroblasts in cell culture and to compare the effect of individual compounds to the effect of a mixture of zinc and propolis. In this study, zinc, as zinc aspartate, at a concentration of 16 μM, increased human fibroblasts proliferation in cell culture, whereas propolis at a concentration of 0.01 % (w/v) revealed antiproliferative and cytotoxic action followed by mild cell necrosis. In culture, zinc was effectively transported into fibroblasts, and propolis inhibited the amount of zinc incorporated into the cells. An addition of propolis to the medium caused a decrease in the Zn(II) amount incorporated into fibroblasts. The obtained results also indicate an appreciable antioxidant property of propolis and revealed its potential as a supplement when applied at doses lower than 0.01 % (w/v). In conclusion, the present study showed that zinc had a protective effect on human cultured fibroblasts’ viability, although propolis revealed its antiproliferative action and caused mild necrosis
Selenium supplementation of amaranth sprouts influences betacyanin content and improves anti-inflammatory properties via NFκB in murine RAW 264.7 macrophages
Abstract Sprouts contain potent compounds which while influencing crucial transduction pathways in cell reveal anti-inflammatory and anticancer activities. In this study, we report the biological activity for seeds and colourful sprouts of four types of edible amaranth, as amaranth has recently attracted interest due to its appreciable nutritional value. MTT assay conducted for the amaranth seeds and sprouts did not show any adverse effect on the viability of murine RAW 264.7 cells. As amaranth accumulates selenium, the sprouts were supple-mented with this trace element (10 mg/L; 15 mg/L Se as so-dium selenite) while growing. Selenium concentration in sprouts was observed to be significantly correlated with betacyanins content of the tested species. The amounts of Se and betacyanins in sprouts varied for various Amaranth spe-cies. In the present study, Amaranthus cruentus sprouts with the highest betacyanins (19.30 ± 0.57–28.85 ± 2.23 mg of amaranthin/100 g of fresh weight) and high total selenium (22.51 ± 1.57–1044.75 ± 73.08 μg/L in methanol extracts) content prevented NFκB translocation to the cell nucleus and subsequently exerted an anti-inflammatory effect by sig-nificant decreasing inflammatory interleukin 6 production (587.3 ± 34.2–710.0 ± 88.1 pg/mL) in the cell culture of acti-vated RAW 264.7 macrophages (vs LPS control 1520 ± 114 pg/mL)
Identification of lipid derivatives in Hep G2 cells
Metabolism of polyunsaturated fatty acids results in biosynthesis of mediators with different physiological effects. These metabolites include prostaglandins, prostacyclins, isoprostanes and others that are important signalling molecules and regulate a variety of physiological and pathophysiological processes including inflammation. Prostaglandins and isoprostanes are produced by either non-enzymatic lipid peroxidation or by enzyme-induced peroxidation (cyclooxygenases and lipoxygenases). They are used as biomarkers of oxidative stress. The aim of our study was to assess the effect of eicosapentaenoic acid (EPA) supplementation with added benzo(a)pyrene (BaP) on HepG2 cells by using a UHPLC/MS-TOF method. This rapid and simple method was developed for the identification, separation and quantification of 8-iPGF3α, PGF3α, 8-isoPGF2α and 5-iPF2α in cultured cells. The UHPLC/MS-TOF method was validated. The calculated limit of detection was in the range of 0.16-0.50 ng/mL, precision (% RSD): 1.2-2.1% and recoveries better than 88%. This method empowered qualitative and quantitative analysis of the selected individual prostaglandins derived from arachidonic acid and eicosapentaenoic acid from cell extracts
New organic-inorganic hybrid compounds based on sodium peroxidomolybdates (VI) and derivatives of pyridine acids : structure determination and catalytic properties
Two organic-inorganic hybrids based on sodium peroxidomolybdates(VI) and 3,5-dicarboxylic pyridine acid (Na-35dcpa) or N-oxide isonicotinic acid (Na-isoO) have been synthesized and characterized. All compounds contain inorganic parts: a pentagonal bipyramid with molybdenum center, and an organic part containing 3,5-dicarboxylic pyridine acid or N-oxide isonicotinic acid moieties. The type of organic part used in the synthesis influences the crystal structure of obtained compounds. This aspect can be interesting for crystal engineering. Crystal structures were determined using powder X-ray diffraction or single crystal diffraction for compounds Na-35dcpa and Na-isoO, respectively. Elemental analysis was used to check the purity of the obtained compounds, while X-ray Powder Diffraction (XRPD) vs. temp. was applied to verify their stability. Moreover, all the compounds were examined by Infrared (IR) spectroscopy. Their catalytic activity was tested in the Baeyer–Villiger (BV) oxidation of cyclohexanone to ε-caprolactone in the oxygen-aldehyde system. The highest catalytic activity in the BV oxidation was observed for Na-35dcpa. The compounds were also tested for biological activity on human normal cells (fibroblasts) and colon cancer cell lines (HT-29, LoVo, SW 620, HCT 116). All compounds were cytotoxic against tumor cells with metastatic characteristics, which makes them interesting and promising candidates for further investigations of specific anticancer mechanisms
Aryl-1,3,5-triazine ligands of histamine receptor attenuate inflammatory and nociceptive response to carrageen, zymosan and lipopolysaccharide
Objective and design Histamine receptor () offers a
great potential for new therapeutic strategies for the treatment
of inflammation-based diseases. The aim of this study
is to present the pharmacological profile of two recently
synthesized ligands of with particular reference to
their anti-inflammatory and analgesic activity.
Materials and subjects We used mice and rats in the
in vivo tests. We also used murine RAW 264.7 cells and
isolated guinea-pig ileum in in vitro test.
Treatments In the in vivo tests, animals were pre-treated
with the increasing doses of investigated compounds (12.5,
25 and 50 mg/kg) and reference compounds: JNJ7777120 (25 mg/kg), indomethacin (10 mg/kg). Macrophages were
pre-treated with two concentrations of tested compounds
100 and 10 M.
Methods We examined anti-inflammatory and analgesic
effects of the new antagonists in the in vivo models of
inflammation induced by carrageenan or zymosan. We
assessed the level of cAMP and release of cytokines, ROS
and NO in lipopolysaccharide (LPS)-stimulated RAW
264.7 macrophages. Moreover, we assessed the affinity of
the investigated compounds for histamine receptor in
functional studies. Results Both investigated compounds reduced paw edema,
mechanical and thermal hyperalgesia in the carrageenaninduced
acute inflammation. Moreover, administration of
the investigated compounds resulted in decreased granulocyte
influx and attenuated nociceptive reaction in the
zymosan-induced peritonitis model. In the same model of
inflammation, the investigated compounds reduced vascular
permeability; however, this effect was observed only
after the highest applied dose. Furthermore, the test compounds
had no impact on cell viability in the experiments
on RAW 264.7 macrophages. In these cells, stimulated
with LPS, the test compounds decreased reactive oxygen
species (ROS) production. They increased the cellular
concentration of cAMP and attenuated the production of
inflammatory cytokines such as and . All
results were comparable to those obtained for the reference
compound JNJ7777120 with the exception of the impact on
NO production. Nevertheless, this effect was similar to that
obtained for the other reference compound rolipram, which
is a phosphodiesterase 4 (PDE 4) inhibitor. Further
experiments revealed that both of the investigated compounds
possessed relatively low affinity for histamine H
receptor and do not inhibit the activity of the PDE 4B1
enzyme. In addition, all the effects of the investigated compounds in in vivo experiments were observed at doses
that did not cause neurologic deficits in rotarod test and did
not reduce spontaneous locomotor activity.
Conclusions Our results demonstrate the anti-inflammatory
and analgesic activity of the new aryl-1,3,5-triazine
derivatives, which are primarily -dependent
Influence of selenium supplementation on fatty acids profile and biological activity of four edible amaranth sprouts as new kind of functional food
Suitability assessment of amaranth sprouts as a new
functional food was carried out. The optimisation of sprouting
process and the influence of selenium supplementation, in
doses 10, 15, and 30 mg/l of selenium as sodium selenite, on
amaranth growth and fatty acid profile were examined.
Methods such as FRAP, DPPH, polyphenols content and
GPX activity were applied to characterize antioxidant poten-
tial of seeds and sprouts of four different edible amaranth
genera.
E. coli, S. aureus, C. albicans
were used to evaluate
amaranth sprouts antimicrobial properties. Interaction be-
tween amaranth sprouts and biological systems was assessed
by analysing antibacterial and antifungal properties with a disc diffusion test. The studies proved amaranth sprouts to be
potentially attractive as functional food. As confirmed by all
the data amaranth sprouts are suitable as a moderate selenium
accumulator and are rich in essential fatty acids, especially
linoleic and alpha-linolenic acids, which are precursors of
long chain polyunsaturated fatty acids. Thus, it opens dietary
opportunities for amaranth sprouts. They can also serve as a
moderate source of antioxidant compounds. Nevertheless, the
experiments revealed neither antibacterial, nor antifungal
properties of sprouts. In general, amaranth sprouts biological
activity under evaluation has failed to prove to be significantly
impacted by selenium fertilization
Animals in iodine deficiency or sulfadimethoxine models of thyroid damage are differently affected by the consumption of brassica sprouts
The study was primarily aimed at investigating the effect of brassica sprout consumption, namely rutabaga (Brassica napus L. var. napobrassica) sprouts (R) generally recognized as antithyroid agent due to its goitrogenic substance content, on hematological, biochemical, and immunological parameters in rats. Sprouts were tested alone and in a combination with other antithyroid factors, such as iodine deficiency (RDI) and sulfadimethoxine (RS). The expression of the heme oxygenase-1 (HO-1) gene
in the thyroid as a stress-inducible protein was determined. The thermographic analysis was also estimated. The intake of rutabaga sprouts by healthy rats did not reveal any significant, harmful effect on the thyroid function. Both body temperature and expression of HO-1 remained unchanged in response to the consumed sprouts. In animals with hypothyroidism, rutabaga sprouts enhanced the negative effect of iodine deficiency or sulfadimethoxine ingestion on the organism by increasing the WBC (RDI), TNF-α (RS), creatinine (RS), and triglyceride (RDI and RS) levels, as well as decreasing PLT (RS) level. Moreover, rutabaga sprout consumption by rats with iodine deficiency and sulfadimethoxine decreased their body temperature. Additionally, the concomitant administration of sprouts and iodine depletion significantly reduced the expression of HO-1 in the thyroid. The results may prove useful in confirming rutabaga sprout consumption to be safe, though the seeds of this vegetable provide a well-known antithyroid agent. Our results have shown that rutabaga sprout consumption may be also a factor that enhances the negative clinical features only when combined with iodine deficiency and sulfadimethoxine ingestion