scholarly journals Mechanism of the toxicity of the artificial ribonucleases for the different human cancer cell lines

2010 ◽  
Vol 56 (2) ◽  
pp. 230-243
Author(s):  
E.B. Logashenko ◽  
I.L. Kuznetsova ◽  
E.I. Ryabchikova ◽  
V.V. Vlassov ◽  
M.A. Zenkova
Keyword(s):  
Human Cancer ◽  
Dependent Manner ◽  
Artificial Ribonucleases ◽  
Short Term ◽  
Concentration Dependent Manner ◽  
Induce Cell Death ◽  
Human Cancer Cell Lines ◽  
Short Term Exposure ◽  
Effective Penetration ◽  
Macromolecular Organization

The ability of artificial ribonucleases to cause in the concentration-dependent manner death of cancer cells has been studied. The cytotoxic activity of artificial ribonucleases is observed at rather low concentration of these compounds (10-5 М). Analysis of the mechanism of artificial ribonucleases citotoxicity revealed that compounds under the study exhibit membranotropic activity in addition to ribonucleases activity found earlier. This activity is responsible for effective penetration of these compounds inside cells. The results obtained show that artificial ribonucleases induce cell death via damage of cells membrane, detachment of plasmalemma and derangement its macromolecular organization. In the case of short-term exposure of cells to the compounds, cells, even with damaged membrane, survive.

scholarly journals Jaceosidin Induces Apoptosis in Human Ovary Cancer Cells through Mitochondrial Pathway

2008 ◽  
Vol 2008 ◽  
pp. 1-6 ◽  
Author(s):  
Wen Lv ◽  
Xia Sheng ◽  
Ting Chen ◽  
Qiang Xu ◽  
Xing Xie
Keyword(s):  
Caspase 3 ◽  
Human Cancer ◽  
Flow Cytometric Analysis ◽  
Mitochondrial Pathway ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Human Cancer Cell Lines ◽  
Flow Cytometric ◽  
Dependent Inhibition ◽  
Pc3 Cells

We examined the antiproliferation effect of Jaceosidin (4′, 5, 7-trihydroxy-3′, 6-dimethoxyflavone) isolated from the herb ofArtemisia vestitaWall on several human cancer cell lines. Jaceosidin significantly reduced the proliferation of CAOV-3, SKOV-3, HeLa, and PC3 cells in a concentration-dependent manner. A time-dependent inhibition was also observed in CAOV-3 cells by Jaceosidin. By flow cytometric analysis, we found that Jaceosidin treatment resulted in an increased apoptosis in CAOV-3 cells. The cells treated with Jaceosidin exhibited a decreased mitochondrial membrane potential. Jaceosidin also increased the level of cleaved caspase-9 and induced the cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP), while caspase-3 inhibitor Z-DEVD-FMK significantly reversed the proapoptotic effect of Jaceosidin in CAOV-3 cells. Moreover, Jaceosidin elevated the level of cytochromecin cytosol. These findings suggest that the anticancer effect of Jaceosidin may be contributed by an induction of apoptosis involving cytochromecrelease from mitochondria to cytosol.

scholarly journals Semi-Synthesis and In Vitro Anti-Cancer Evaluation of Magnolol Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4302
Author(s):  
Xiao-Long Sun ◽  
Mei-Lin Zhu ◽  
Yi-Qun Dai ◽  
Hong-Mei Li ◽  
Bo-Han Li ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Biological Activities ◽  
Migration And Invasion ◽  
Dependent Manner ◽  
Anticancer Activities ◽  
Antitumor Effects ◽  
Concentration Dependent Manner ◽  
Human Cancer Cell Lines

Magnolol (MAG), a biphenolic neolignan, has various biological activities including antitumor effects. In this study, 15 MAG derivatives were semi-synthesized and evaluated for their in vitro anticancer activities. From these derivatives, compound 6a exhibited the best cytotoxic activity against four human cancer cell lines, with IC50 values ranging from 20.43 to 28.27 μM. Wound-healing and transwell assays showed that compound 6a significantly inhibited the migration and invasion of MDA-MB-231 cells. In addition, Western blotting experiments, performed using various concentrations of 6a, demonstrated that it downregulates the expression of HIF-1α, MMP-2, and MMP-9 in a concentration-dependent manner. Overall, these results suggest that substituting a benzyl group having F atoms substituted at the C2 position on MAG is a viable strategy for the structural optimization of MAG derivatives as anticancer agents.

Presynaptic Group II mGluR Inhibition of Short-Term Depression in the Medial Perforant Path of the Dentate Gyrus In Vitro

2001 ◽  
Vol 85 (6) ◽  
pp. 2509-2515 ◽  
Author(s):  
John Kilbride ◽  
Anthony M. Rush ◽  
Michael J. Rowan ◽  
Roger Anwyl
Keyword(s):  
Dentate Gyrus ◽  
Metabotropic Glutamate Receptors ◽  
State Level ◽  
Perforant Path ◽  
Dependent Manner ◽  
Short Term ◽  
Concentration Dependent Manner ◽  
Postsynaptic Response ◽  
Group Ii

Inhibition of short-term plasticity by activation of presynaptic group II metabotropic glutamate receptors (group II mGluR) was investigated in the medial perforant path of the dentate gyrus in the hippocampus in vitro. Brief trains of stimulation (10 stimuli at 1–200 Hz) evoked short-term depression of field excitatory postsynaptic potentials (EPSPs). The steady-state level of depression, measured after 10 stimuli, was frequency dependent, increasing between 1 and 200 Hz. Activation of group II mGluR by the selective agonist LY354740 did not alter short-term depression evoked by frequencies up to 10 Hz, but did inhibit short-term depression evoked at higher frequencies in a frequency- and concentration-dependent manner. The time-averaged postsynaptic response (EPSP per unit time) was found to increase linearly with frequency up to ∼20 Hz. At higher frequencies, the response plateaued, thereby becoming independent of frequency. Frequencies above this were differentiated only during the transient postsynaptic response that accompanies changes in firing rates. Activation of presynaptically located group II mGluR increased the frequency at which the EPSP per unit time plateaued up to 30–50 Hz.

Structure Activity Relationships of Antiproliferative Rocaglamide Derivatives from Aglaia Species (Meliaceae)

1999 ◽  
Vol 54 (1-2) ◽  
pp. 55-60 ◽  
Author(s):  
Frank I. Bohnenstengel ◽  
Klaus G. Steube ◽  
Corinna Meyer ◽  
Bambang W. Nugroho ◽  
Pham D. Hung ◽  
...  
Keyword(s):  
Cell Lines ◽  
Potential Role ◽  
Human Cancer ◽  
Experimental Medicine ◽  
Dependent Manner ◽  
Pyran Ring ◽  
Human Cancer Cell Lines ◽  
Structure Activity ◽  
High Doses

Eleven rocaglamide derivatives (cyclopentatetrahydrobenzofurans) and one structurally related aglain congener all isolated from different Aglaia species (Meliaceae) were tested for growth inhibiting properties using the human cancer cell lines MONO-MAC-6 and MEL-JUSO. Proliferation of both cell lines was efficiently inhibited in a dose and compound dependent manner. Applying a MTT-Assay, the IC50 of the most active compound didesmethyl-rocaglamide (1) was observed at 0.002 and 0.006 μg/ml (0.004 and 0.013 μM) depending on the cell line investigated. Bulky aminoacyl substituents at C-2, acetylation of the OH substituent at C-1 or insertion of a OH or OMe substituent at C-3 ’of the rocaglamide skeleton all diminished the activity of the compounds investigated. The aglain derivative 12 was inactive up to a concentration of 3 μg/ml (4.6 μᴍ) . This loss of activity is assumed to be mainly due to the presence of a pyran ring in the aglains vs. a furan ring as found in rocaglamide derivatives. Rocaglamide derivatives may act primarily by inhibition of cell proliferation as evidenced by the absence of a significant cytotoxic effect in long-term cultures of MONO-MAC-6 cells treated with high doses of didesmethylrocaglamide. Our data suggest that rocaglamide derivatives could exert a potential role in the treatment of malignant diseases and are worth to be investigated in further studies of experimental medicine and pharmacology

scholarly journals Synthesis and In Vitro Photocytotoxicity of 9-/13-Lipophilic Substituted Berberine Derivatives as Potential Anticancer Agents

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 677 ◽  
Author(s):  
Hong-Jhih Lin ◽  
Jinn-Hsuan Ho ◽  
Li-Chen Tsai ◽  
Fang-Yu Yang ◽  
Ling-Ling Yang ◽  
...  
Keyword(s):  
Liver Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Hepg2 Cells ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Dependent Manner ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Berberine Derivatives

The objective of this study was to synthesize the 9-/13-position substituted berberine derivatives and evaluate their cytotoxic and photocytotoxic effects against three human cancer cell lines. Among all the synthesized compounds, 9-O-dodecyl- (5e), 13-dodecyl- (6e), and 13-O-dodecyl-berberine (7e) exhibited stronger growth inhibition against three human cancer cell lines, (HepG2, HT-29 and BFTC905), in comparison with structurally related berberine (1). These three compounds also showed the photocytotoxicity in human cancer cells in a concentration-dependent and light dose-dependent manner. Through flow cytometry analysis, we found out a lipophilic group at the 9-/13-position of berberine may have facilitated its penetration into test cells and hence enhanced its photocytotoxicity on the human liver cancer cell HepG2. Further, in cell cycle analysis, 5e, 6e, and 7e induced HepG2 cells to arrest at the S phase and caused apoptosis upon irradiation. In addition, photodynamic treatment of berberine derivatives 5e, 6e, and 7e again showed a significant photocytotoxic effects on HepG2 cells, induced remarkable cell apoptosis, greatly increased intracellular ROS level, and the loss of mitochondrial membrane potential. These results over and again confirmed that berberine derivatives 5e, 6e, and 7e greatly enhanced photocytotoxicity. Taken together, the test data led us to conclude that berberine derivatives with a dodecyl group at the 9-/13-position could be great candidates for the anti-liver cancer medicines developments.

scholarly journals Fusarubin and Anhydrofusarubin Isolated from A Cladosporium Species Inhibit Cell Growth in Human Cancer Cell Lines

Toxins ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 503 ◽  
Author(s):  
Sabrina Adorisio ◽  
Alessandra Fierabracci ◽  
Isabella Muscari ◽  
Anna Liberati ◽  
Lorenza Cannarile ◽  
...  
Keyword(s):  
Cell Growth ◽  
Cell Lines ◽  
Cell Cycle Progression ◽  
Fas Ligand ◽  
Human Cancer ◽  
Dependent Manner ◽  
Food Contaminants ◽  
Human Cancer Cell Lines ◽  
Hematological Cancers ◽  
The Impact

Cladosporium species are endophytic fungi that grow on organic matter and are considered food contaminants. The anti-microbial and anti-tumor naphthoquinones fusarubin (FUS) and anhydrofusarubin (AFU) were isolated using column chromatography from a Cladosporium species residing inside Rauwolfia leaves. The impact of FUS and AFU on cell growth was assessed in acute myeloid leukemia (OCI-AML3) and other hematologic tumor cell lines (HL-60, U937, and Jurkat). Treatment with FUS or AFU reduced the number of OCI-AML3 cells as evaluated by a hemocytometer. Flow cytometry analyses showed that this effect was accompanied by diverse impairments in cell cycle progression. Specifically, FUS (20 or 10 μg/mL significantly decreased the percentage of cells in S phase and increased the percentage of cells in G2/M phase, whereas AFU increased the percentage of cells in G0/G1 phase (50 and 25 μg/mL) and decreased the percentage of cells in S (50 μg/mL) and G2/M (50 and 25 μg/mL) phases. Both substances significantly increased apoptosis at higher concentrations. The effects of FUS were more potent than those of AFU, with FUS up-regulating p21 expression in a p53-dependent manner, as detected by Western blot analyses, likely the consequence of decreased ERK phosphorylation and increased p38 expression (both of which increase p21 stability). FUS also decreased Akt phosphorylation and resulted in increased Fas ligand production and caspase-8/3-dependent apoptosis. These results suggest that FUS and AFU inhibit proliferation and increase apoptosis in cell lines derived from hematological cancers.

scholarly journals Design and Synthesis of C-19 Isosteviol Derivatives as Potent and Highly Selective Antiproliferative Agents

Molecules ◽  
2018 ◽  
Vol 24 (1) ◽  
pp. 121 ◽  
Author(s):  
Tian Luan ◽  
Li-Hua Cao ◽  
Hao Deng ◽  
Qing-Kun Shen ◽  
Yu-Shun Tian ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Human Cancer ◽  
Parent Compound ◽  
Cyclin A ◽  
Cyclin B1 ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Cyclin E1 ◽  
Hct 116

Six series of novel isosteviol derivatives; modified in the C-19 position; were synthesized; and their antiproliferative activity was evaluated against three human cancer cell lines (HCT-116; BEL-7402; HepG2) and the human L02 normal cell line in vitro. Most of the derivatives tested here exhibited improved antiproliferative activity with high selectivity when compared with the parent compound isosteviol and the positive control drug 5-fluorouracil. Among these derivatives; compound 5d exhibited the most potent antiproliferative activity and commendable selectivity between cancer and normal cells. In addition; compound 5d inhibited the colony formation of HCT-116 cells in a concentration-dependent manner. Further studies revealed that compound 5d arrested the HCT-116 cell cycle in the S phase; and western blot analysis demonstrated the mechanism may be correlated with a change in the expression of cyclin A; cyclin B1; and cyclin E1. Furthermore; the results of a docking study that involved placing compound 5d into the CDK2/cyclin A binding site revealed that its mode of action was possibly as a CDK2/cyclin A inhibitor.

Sevoflurane Blocks Cholinergic Synaptic Transmission Postsynaptically but Does Not Affect Short-term Potentiation

2005 ◽  
Vol 102 (5) ◽  
pp. 920-928 ◽  
Author(s):  
Hiroaki Naruo ◽  
Shin Onizuka ◽  
David Prince ◽  
Mayumi Takasaki ◽  
Naweed I. Syed
Keyword(s):  
Synaptic Plasticity ◽  
Synaptic Transmission ◽  
Fluorescent Imaging ◽  
Posttetanic Potentiation ◽  
Dependent Manner ◽  
General Anesthetics ◽  
Short Term ◽  
Concentration Dependent Manner ◽  
Cholinergic Synaptic Transmission ◽  
Term Potentiation

Background As compared with their effects on both inhibitory and excitatory synapses, little is known about the mechanisms by which general anesthetics affect synaptic plasticity that forms the basis for learning and memory at the cellular level. To test whether clinically relevant concentrations of sevoflurane affect short-term potentiation involving cholinergic synaptic transmission, the soma-soma synapses between identified, postsynaptic neurons were used. Methods Uniquely identifiable neurons visceral dorsal 4 (presynaptic) and left pedal dorsal 1 (postsynaptic) of the mollusk Lymnaea stagnalis were isolated from the intact ganglion and paired overnight in a soma-soma configuration. Simultaneous intracellular recordings coupled with fluorescent imaging of the FM1-43 dye were made in either the absence or the presence of sevoflurane. Results Cholinergic synapses, similar to those observed in vivo, developed between the neurons, and the synaptic transmission exhibited classic short-term, posttetanic potentiation. Action potential-induced (visceral dorsal 4), 1:1 excitatory postsynaptic potentials were reversibly and significantly suppressed by sevoflurane in a concentration-dependent manner. Fluorescent imaging with the dye FM1-43 revealed that sevoflurane did not affect presynaptic exocytosis or endocytosis; instead, postsynaptic nicotinic acetylcholine receptors were blocked in a concentration-dependent manner. To test the hypothesis that sevoflurane affects short-term potentiation, a posttetanic potentiation paradigm was used, and synaptic transmission was examined in either the presence or the absence of sevoflurane. Although 1.5% sevoflurane significantly reduced synaptic transmission between the paired cells, it did not affect the formation or retention of posttetanic potentiation at this synapse. Conclusions This study demonstrates that sevoflurane blocks cholinergic synaptic transmission postsynaptically but does not affect short-term synaptic plasticity at the visceral dorsal 4-left pedal dorsal 1 synapse.

scholarly journals Lipophilised resveratrol affects the generation of reactive nitrogen species in murine macrophages and cell viability of human cancer cell lines

2019 ◽  
Vol 7 ◽  
Author(s):  
Won Young Oh ◽  
Yi-Shiou Chiou ◽  
Min-Hsiung Pan ◽  
Fereidoon Shahidi
Keyword(s):  
Cell Viability ◽  
Cell Lines ◽  
Human Cancer ◽  
Raw 264.7 Cells ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Nitrite Production ◽  
Anti Inflammatory ◽  
Ht 29

Resveratrol was esterified with selected fatty acids to improve its lipophilicity and potential application in food and biological systems. In this study, resveratrol and monoesters of resveratryl propionate (RC3:0) and resveratryl docosahexaenate (RDHA) were examined for their effects on anti-inflammatory and anti-proliferative activity in vitro.  All test compounds showed a decreased nitrite production in murine RAW 264.7 cells in a concentration dependent manner. Resveratrol, RC3:0, and RDHA were evaluated for their effects on cell viability using liver cancer (HepG2), colon cancer (HT-29, A431), breast cancer (MCF7), and gastric cancer (AGS) cell lines. All test compounds showed decreased cell viability of HepG2, A431, MCF7, HT-29, and AGS in a concentration-dependent manner. The results suggest that resveratrol esters may serve as potential anti-inflammatory and anti-proliferative agents.

Recovery of Acid Production in Streptococcus mutans Biofilms after Short-Term Fluoride Treatment

2016 ◽  
Vol 50 (4) ◽  
pp. 363-371 ◽  
Author(s):  
Minh-Huy Dang ◽  
Ji-Eun Jung ◽  
Dae-Woo Lee ◽  
Kwang-Yeob Song ◽  
Jae-Gyu Jeon
Keyword(s):  
Treatment Period ◽  
Streptococcus Mutans ◽  
Acid Production ◽  
Fluoride Concentration ◽  
Dependent Manner ◽  
Short Term ◽  
Concentration Dependent Manner ◽  
Fluoride Treatment ◽  
Linear Pattern ◽  
Hygiene Measures

Fluoride is commonly used as an ingredient of topical oral hygiene measures. Despite the anti-acidogenic activities of fluoride against cariogenic biofilms, the recovery of the biofilms from fluoride damage is unclear. Herein, we investigated the recovery of acid production in Streptococcus mutans biofilms after short-term or during periodic 1-min fluoride treatments. For this study, 46-hour-old S. mutans biofilms were treated with fluoride (0-2,000 ppm F-) for 1-8 min and then incubated in saliva for 0-100 min. The 74-hour-old biofilms were also periodically treated with the fluoride concentration during biofilm formation (1 min/treatment). Changes in acidogenicity and viability were determined via pH drop and colony-forming unit assays, respectively. In this study, acid production after a 1-min fluoride treatment was recovered as saliva incubation time increased, which followed a linear pattern of concentration dependence (R = 0.99, R2 = 0.98). The recovery pattern was in a biphasic pattern, with an initial rapid rate followed by a second slow recovery. Furthermore, recovery from fluoride damage was retarded in a concentration-dependent manner as treatment time increased. In periodic 1-min fluoride treatments, acid production in the biofilms was not diminished during the non-fluoride treatment period; however, it was reduced in a concentration-dependent manner during the fluoride treatment period. The viability of the biofilm cells did not change, even at high fluoride concentrations. Collectively, our results suggest that brief fluoride treatment does not sustain anti-acidogenic activity against S. mutans in biofilms since the damage is recoverable with time.

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