scholarly journals Antiausterity Activity of Arctigenin Enantiomers: Importance of (2R,3R)-Absolute Configuration

2014 ◽  
Vol 9 (1) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Suresh Awale ◽  
Mamoru Kato ◽  
Dya Fita Dibwe ◽  
Feng Li ◽  
Chika Miyoshi ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Absolute Configuration ◽  
The Other ◽  
Dependent Manner ◽  
Meoh Extract ◽  
Concentration Dependent Manner ◽  
Akt Activation ◽  
Other Hand

From a MeOH extract of powdered roots of Wikstroema indica, six dibenzyl-γ-butyrolactone-type lignans with (2 S,3 S)-absolute configuration [(+)-arctigenin (1), (+)-matairesinol (2), (+)-trachelogenin (3), (+)-nortrachelogenin (4), (+)-hinokinin (5), and (+)-kusunokinin (6)] were isolated, whereas three dibenzyl-γ-butyrolactone-type lignans with (2 R,3 R)-absolute configuration [(-)-arctigenin (1), (-)-matairesinol (2), (-)-trachelogenin (3)] were isolated from Trachelospermum asiaticum. The in vitro preferential cytotoxic activity of the nine compounds was evaluated against human pancreatic PANC-1 cancer cells in nutrient-deprived medium (NDM), but none of the six lignans (1–6) with (2 S,3 S)-absolute configuration showed preferential cytotoxicity. On the other hand, three lignans (1*–3*) with (2 R,3 R)-absolute configuration exhibited preferential cytotoxicity in a concentration-dependent manner with PC50 values of 0.54, 6.82, and 5.85 μM, respectively. Furthermore, the effect of (-)- and (+)-arctigenin was evaluated against the activation of Akt, which is a key process in the tolerance to nutrition starvation. Interestingly, only (-)-arctigenin (1*) strongly suppressed the activation of Akt. These results indicate that the (2 R,3 R)-absolute configuration of (-)-enantiomers should be required for the preferential cytotoxicity through the inhibition of Akt activation.

scholarly journals Effect of Palmitic Acid on Exosome-Mediated Secretion and Invasive Motility in Prostate Cancer Cells

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2722
Author(s):  
Ivan V. Maly ◽  
Wilma A. Hofmann
Keyword(s):  
Prostate Cancer ◽  
Palmitic Acid ◽  
Cancer Cells ◽  
Dependent Manner ◽  
Prostate Cancer Cells ◽  
Concentration Dependent Manner ◽  
Fat Consumption ◽  
Progression Markers

High fat consumption can enhance metastasis and decrease survival in prostate cancer, but the picture remains incomplete on the epidemiological and cell-biological level, impeding progress toward individualized recommendations in the clinic. Recent work has highlighted the role of exosomes secreted by prostate cancer cells in the progression of the disease, particularly in metastatic invasion, and also the utility of targeting these extracellular vesicles for diagnostics, as carriers of disease progression markers. Here, we investigated the question of a potential impact of the chief nutritional saturated fatty acid on the exosome secretion. Palmitic acid decreased the secretion of exosomes in human prostate cancer cells in vitro in a concentration-dependent manner. At the same time, the content of some prospective metastatic markers in the secreted exosomal fraction was also reduced, as was the ability of the cells to invade across extracellular matrix barriers. While by themselves our in vitro results imply that on the cell level, palmitic acid may be beneficial vis-à-vis the course of the disease, they also suggest that, by virtue of the decreased biomarker secretion, palmitic acid has the potential to cause unjustified deprioritization of treatment in obese and lipidemic men.

scholarly journals Toxicological Effects of Traumatic Acid and Selected Herbicides on Human Breast Cancer Cells: In Vitro Cytotoxicity Assessment of Analyzed Compounds

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1710 ◽  
Author(s):  
Agata Jabłońska-Trypuć ◽  
Urszula Wydro ◽  
Elżbieta Wołejko ◽  
Andrzej Butarewicz
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Breast Cancer Cell Lines ◽  
Dependent Manner ◽  
Food Contaminants ◽  
Food Ingredient ◽  
Concentration Dependent Manner ◽  
Traumatic Acid

The main consequence of herbicides use is the presence of their residues in food of plant origin. A growing body of evidence indicates that herbicides cause detrimental effects upon human health while demonstrating a direct link of pesticides exposure with the occurrence of human chronic diseases, including cancer. There is a pressing need to develop our knowledge regarding interactions of food contaminants and food components both in vitro and in vivo. Pesticides are highly undesirable food contaminants, and traumatic acid (TA) is a very beneficial food ingredient, therefore we decided to study if TA may act as a compound that delays the stimulatory effect of pesticides on breast cancer cells. To analyze the potential effects that selected herbicides (MCPA, mesotrione, bifenox and dichlobenil) may have upon cancerous cells, we conducted studies of the cytotoxicity of physiological concentrations of four pesticides and the mix of TA with tested herbicides in three different breast cancer cell lines (MCF-7, ZR-75-1 and MDA-MB-231) and one normal healthy breast cell line MCF-12A. Based on the obtained results we conclude that TA in a concentration-dependent manner might influence selected effects of the studied herbicides for particular cancer cells lines.

scholarly journals Fangchinoline Induces Apoptosis, Autophagy and Energetic Impairment in Bladder Cancer

2017 ◽  
Vol 43 (3) ◽  
pp. 1003-1011 ◽  
Author(s):  
Bo Fan ◽  
Xiaoyu Zhang ◽  
Yongliang Ma ◽  
Aili Zhang
Keyword(s):  
Bladder Cancer ◽  
Cancer Cells ◽  
Potential Candidate ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Metabolic Substrates ◽  
Bladder Cancer Cells ◽  
Exogenous Addition ◽  
Induced Apoptosis

Background/Aims: Tetrandrine and Fangchinoline (Fcn) are two natural products that are found in Stephania tetrandra. Tetrandrine is a known anti-bladder cancer compound, but the effects of Fcn on bladder cancer have been previously unclear. In the present study, we focused on the anti-tumor effects of Fcn on bladder cancer. Methods and Results: We treated T24 and 5637 bladder cancer cell lines with Fcn in vitro. We observed that Fcn inhibited the viability of bladder cancer cells in a concentration-dependent manner. The expression of PCNA, a biomarker of proliferation, was down-regulated. Fcn treatment induced both apoptosis and autophagy in bladder cancer cells, as shown by the increased cleavage of caspase-3, an up-regulated LC3-II/LC3-I ratio and the down-regulated p62 level. Blocking autophagy with 3-MA (3-Methyladenine) enhanced Fcn-induced apoptosis, indicating that Fcn-induced autophagy was adaptive. Additionally, we observed that Fcn treatment inhibited mTOR and reduced the intracellular ATP levels. The exogenous addition of methyl pyruvate (MP) to compensate metabolic substrates alleviated Fcn-induced apoptosis and autophagy. Conclusions: Our data indicated that Fcn caused an impairment in energy generation, which led to apoptosis and adaptive autophagy in bladder cancer. These results demonstrated that Fcn may be a potential candidate for use in the prevention and treatment of bladder cancer.

Flow-induced Dilation of Rat Coronary Microvessels Is Attenuated by Isoflurane but Enhanced by Halothane 

1998 ◽  
Vol 89 (1) ◽  
pp. 132-142 ◽  
Author(s):  
Kyung W. Park ◽  
Hai B. Dai ◽  
Edward Lowenstein ◽  
Frank W. Sellke
Keyword(s):  
Minimum Alveolar Concentration ◽  
Detection System ◽  
Volatile Anesthetics ◽  
No Synthase ◽  
The Other ◽  
Dependent Manner ◽  
Cyclooxygenase Inhibitor ◽  
Concentration Dependent Manner ◽  
Synthase Inhibitor

Background Volatile anesthetics attenuate agonist-induced endothelium-dependent vasodilation of coronary arteries. This study considered the hypothesis that the anesthetics may also attenuate flow-induced endothelium-dependent vasodilation. Methods Rat subepicardial arteries of approximately 100 microm were monitored for diameter changes in vitro by a video detection system, with the midpoint luminal pressure held constant at 40 mmHg but the pressure gradient (and therefore flow) across each vessel increased from 0 to 80 mmHg, in the presence or absence of 1 or 2 minimum alveolar concentration (MAC) isoflurane or 1 or 2 MAC halothane, with or without 10 microM of the nitric oxide (NO) synthase inhibitor NG-nitro-L-arginine (L-NNA) or 10 microM of the cyclooxygenase inhibitor indomethacin. Results Flow-induced dilation was attenuated by L-NNA or indomethacin (p < 0.001 each). It was attenuated by isoflurane in a concentration-dependent manner (P < 0.001). Attenuation by 2 MAC isoflurane persisted even in the presence of L-NNA (P < 0.01) or indomethacin (P < 0.05). On the other hand, flow-induced dilation was enhanced by 2 MAC halothane (P < 0.05). Halothane at 1 MAC had no significant effect. Enhancement by 2 MAC halothane was evident in the presence of indomethacin (P < 0.05) but not L-NNA (P = 0.40). Conclusions In rat subepicardial arteries, flow-induced dilation is endothelium-dependent and mediated by both NO and a prostanoid. Isoflurane attenuates flow-induced dilation, possibly by decreasing synthesis, the action of NO and a prostanoid, or both, whereas halothane enhances it, possibly by increasing synthesis, the action of NO, or both.

scholarly journals Suppression of progesterone-enhanced hyperactivation in hamster spermatozoa by estrogen

Reproduction ◽  
2010 ◽  
Vol 140 (3) ◽  
pp. 453-464 ◽  
Author(s):  
Masakatsu Fujinoki
Keyword(s):  
Steroid Hormones ◽  
Sperm Head ◽  
The Other ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Other Hand ◽  
Sperm Proteins ◽  
17Β Estradiol

In this study, I examined whether sperm hyperactivation in hamster is regulated by steroid hormones such as estrogen (estradiol, E2) and progesterone. Although sperm hyperactivation was enhanced by progesterone, 17β-estradiol (17βE2) itself did not affect sperm hyperactivation. However, 17βE2 suppressed progesterone-enhanced hyperactivation in a concentration-dependent manner through non-genomic pathways when spermatozoa were exposed to 17βE2 at the same time or before exposure to progesterone. When spermatozoa were exposed to 17βE2 after exposure to progesterone, 17βE2 did not suppress progesterone-enhanced hyperactivation. Moreover, 17α-estradiol, an inactive isomer of E2, did not suppress progesterone-enhanced hyperactivation. Observations using a FITC-conjugated 17βE2 showed that it binds to the acrosome region of the sperm head. Binding of 17βE2 to spermatozoa was not inhibited by progesterone, although 17βE2 did not suppress progesterone-enhanced hyperactivation when spermatozoa were exposed to 17βE2 after exposure to progesterone. On the other hand, binding of progesterone to spermatozoa was also not inhibited by 17βE2 even if progesterone-enhanced hyperactivation was suppressed by 17βE2. Although tyrosine phosphorylations of sperm proteins were enhanced by progesterone, enhancement of tyrosine phosphorylations by progesterone was suppressed by 17βE2. Moreover, tyrosine phosphorylations were inhibited by 17βE2 when only 17βE2 was added to the medium. From these results, it is likely that 17βE2 competitively suppresses progesterone-enhanced hyperactivation through the inhibition of tyrosine phosphorylations via non-genomic pathways.

Serotonin relaxes porcine pial veins

1994 ◽  
Vol 266 (3) ◽  
pp. H1000-H1006 ◽  
Author(s):  
T. J. Lee ◽  
M. Ueno ◽  
N. Sunagane ◽  
M. H. Sun
Keyword(s):  
Muscle Tone ◽  
The Other ◽  
Receptor Subtypes ◽  
Dependent Manner ◽  
Pial Arteries ◽  
Concentration Dependent Manner ◽  
Vasoactive Substances ◽  
Other Hand ◽  
Mechanical Stretching ◽  
Or Applications

The effect of serotonin [5-hydroxytryptamine (5-HT)] on pial venous tone of the pig was examined using in vitro tissue bath techniques. Isolated pial venous rings exhibited spontaneous rhythmic contractions (SRC) on mechanical stretching and/or applications of several vasoactive substances, including norepinephrine. On the other hand, KCl induced sustained active muscle tone (SAT) without SRC. The SRC induced by mechanical stretching were not affected by tetrodotoxin, nitro-L-arginine, alpha- and beta-adrenergic, histaminergic, and muscarinic receptor antagonists, indicating that the SRC in porcine pial veins are of myogenic origin. The SRC induced by stretching or applications of vasoactive substances and SAT induced by KCl were inhibited by 5-HT in a concentration-dependent manner. The inhibition was prevented by methysergide and methiothepin but not by ketanserin, propranolol, 3 alpha-tropanyl-1H-indole-3-carboxylic acid ester, hemoglobin, or nitro-L-arginine. The SRC and SAT were inhibited by 5-carboxamidotryptamine (5-CT), 8-hydroxy-2-di-N-propylaminotetralin HBr (8-OHDPAT), 1-[3-(trifluoromethyl)phenyl]piperazine (TFMPP), and 5-methoxytryptamine (5-MT), but not by sumatriptan, alpha-methylserotonin, or 2-methylserotonin. On the other hand, 5-CT, 8-OHDPAT, TFMPP, 5-MT, and sumatriptan constricted the porcine pial arteries exclusively. In 15% of pial venous preparations examined, 5-HT at low concentrations induced ketanserin-sensitive constrictions. These results indicate that the porcine pial venous smooth muscle contains multiple subtypes of 5-HT receptors. The 5-HT inhibition of SRC and SAT is predominant and is mediated by 5-HT1-like receptors, which, however, do not seem to correspond to 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D, 5-HT1E, or 5-HT1F receptor subtypes.(ABSTRACT TRUNCATED AT 250 WORDS)

scholarly journals Phenolic Compounds from Hypericum Calycinum and Their Antioxidant Activity

2009 ◽  
Vol 4 (4) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Hasan Kırmızıbekmez ◽  
Carla Bassarello ◽  
Sonia Piacente ◽  
Engin Celep ◽  
İrem Atay ◽  
...  
Keyword(s):  
Spectroscopic Analysis ◽  
Radical Scavenging ◽  
2D Nmr ◽  
Free Radical Scavenging ◽  
Dependent Manner ◽  
Meoh Extract ◽  
Concentration Dependent Manner ◽  
Caffeoylquinic Acid ◽  
Free Radical Scavenging Activities

From the MeOH extract of Hypericum calycinum, two caffeoylquinic acid derivatives, butyl chlorogenate (1), and chlorogenic acid (2), seven flavonoids, quercetin (3), quercitrin (4), hyperoside (5), isoquercitrin (6), miquelianin (7), rutin (8) and I3, II8-biapigenin (9) and two flavanols, (+)-catechin (10) and (-)-epicatechin (11) were isolated. Identification of the isolates was carried out by spectroscopic analysis including 1D and 2D NMR experiments as well as mass spectrometry. Free radical scavenging activities of the isolated compounds were determined in in-vitro 1,1-diphenyl-2-picrylhydrazyl (DPPH) and nitric oxide (NO) scavenging models. The compounds showed strong DPPH and moderate NO scavenging activities in a concentration dependent manner. (+)-Catechin and (-)-epicatechin were found to be the most active compounds with IC50 values of 4.16 and 4.67 μM for DPPH and 190 and 170 μM for NO scavenging activities, respectively.

Antiproliferative activity of synthesized some new benzimidazole carboxamidines against MCF-7 breast carcinoma cells

2018 ◽  
Vol 73 (3-4) ◽  
pp. 137-145 ◽  
Author(s):  
Cigdem Karaaslan ◽  
Filiz Bakar ◽  
Hakan Goker
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Benzimidazole Derivatives ◽  
Dependent Manner ◽  
Base Pairs ◽  
Mcf 7

AbstractBreast cancer is the most endemic cause of cancer among women in both developed and developing countries. Benzimidazole derivatives exemplify one of the chemical classes that show strong cytotoxic activity especially against breast cancer cells (MCF-7). Aromatic amidine derivatives are known as a group of DNA interactive compounds that bind minor groove of the genome, especially A-T base pairs, and show significant in vitro and in vivo toxicity toward cancer cells. In light of these studies, some new mono/dicationic amidino benzimidazole derivatives were synthesized and evaluated for cytotoxic activity on cultured MCF-7 breast cancer cells. Some of these compounds have strongly inhibited MCF-7 cell viability in a dose-dependent manner compared with clinically used reference compounds, imatinib mesylate and docetaxel. Among them, 4-[(5(6)-bromo-1H-benzimidazole-2-yl)amino]benzene-1-carboxamidine (30) showed the best inhibitory activity with IC50value of 4.6 nM.

scholarly journals A chalcone inhibits the growth and metastasis of KYSE-4 esophageal cancer cells

2020 ◽  
Vol 48 (6) ◽  
pp. 030006052092883
Author(s):  
Jie Chen ◽  
Chun-Yan Kang ◽  
Zhao-Xia Niu ◽  
Hui-Cong Zhou ◽  
Hong-Mei Yang
Keyword(s):  
Esophageal Cancer ◽  
Cell Growth ◽  
Cancer Cells ◽  
Migration And Invasion ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Anticancer Effects ◽  
Esophageal Cancer Cells

Objective To investigate the in vitro and in vivo anticancer effects of a chalcone against KYSE-4 esophageal cancer cells. Methods A chalcone was synthesized via the molecular hybridization strategy based on the anticancer activity of chalcone and dithiocarbamate scaffolds. The anticancer effects of different concentrations of the chalcone derivative were compared in esophageal cancer cells. Results This chalcone displayed strong inhibitory effects on esophageal cancer cell growth with an IC50 of 1.06 μM in KYSE-4 cells. Analysis of the mechanism revealed that the derivative obviously inhibited KYSE-4 cell growth, migration, and invasion in a concentration-dependent manner. Furthermore, the compound regulated migration-related biomarkers (E-cadherin, N-cadherin, and Slug) and inhibited the Wnt/β-catenin pathway. According to western blotting, this chalcone suppressed the expression of proline-rich protein 11 (PRR11) in a concentration- and time-dependent manner. Conclusions This chalcone might be a leading candidate for suppressing the growth and metastasis of esophageal cancer by downregulating PRR11 expression and inhibiting Wnt/β-catenin signaling.

scholarly journals Antioxidant and Prooxidant Effects of Metal Dafonates on the NADPH-Dependent Lipid Peroxidation in the Murine Hepatic Microsomal System

1999 ◽  
Vol 6 (3) ◽  
pp. 169-175 ◽  
Author(s):  
M. Gupta ◽  
R. K. Kale ◽  
P. P. Kulkarni ◽  
S. B. Padhye
Keyword(s):  
Lipid Peroxidation ◽  
Metal Ions ◽  
The Other ◽  
Inhibition Constant ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Other Hand ◽  
Significant Reversal

Dafone inhibits the lipid peroxidation significantly in a concentration dependent manner. The inhibition was found to be an uncompetitive type with the inhibition constant (Ki) of 62.5 μM On the other hand complexation with metal ions results in a significant reversal from antioxidant to pro-oxidant properties for the resulting complexes which are cationic and with associated halometallate anions. The nature of the potentiation in case of the ferric compound was of competitive type with activation constant (Ka) having the value 32.5 μM . The neutral copper-dafonate complex, however, inhibits lipid peroxidation with increase in concentration.

Sign in / Sign up

Export Citation Format

Share Document