scholarly journals Quercetin, a Flavonol, Promotes Disassembly of Microtubules in Prostate Cancer Cells: Possible Mechanism of its Antitumor Activity.

1998 ◽  
Vol 31 (5) ◽  
pp. 435-445 ◽  
Author(s):  
Tetsuo Takagi ◽  
Susumu Takekoshi ◽  
Takeshi Okabe ◽  
Hidetaka Nagata ◽  
Takao Honma ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Antitumor Activity ◽  
Cancer Cells ◽  
Prostate Cancer Cells

scholarly journals Antitumor activity and downregulation of pro-angiogenic molecules in human prostate cancer cells by a novel thiazolidione compound

The Prostate ◽  
2006 ◽  
Vol 66 (4) ◽  
pp. 430-438 ◽  
Author(s):  
Fuminori Teraishi ◽  
Shuhong Wu ◽  
Satoshi Inoue ◽  
Lidong Zhang ◽  
John J. Davis ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Antitumor Activity ◽  
Cancer Cells ◽  
Human Prostate ◽  
Human Prostate Cancer ◽  
Prostate Cancer Cells

scholarly journals Retigeric Acid B Exhibits Antitumor Activity through Suppression of Nuclear Factor-κB Signaling in Prostate Cancer Cells in Vitro and in Vivo

PLoS ONE ◽  
2012 ◽  
Vol 7 (5) ◽  
pp. e38000 ◽  
Author(s):  
Yong-Qing Liu ◽  
Xiao-Yan Hu ◽  
Tao Lu ◽  
Yan-Na Cheng ◽  
Charles Y. F. Young ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Antitumor Activity ◽  
Cancer Cells ◽  
Nuclear Factor Κb ◽  
Nuclear Factor ◽  
Prostate Cancer Cells

scholarly journals Synthesis and anticancer activity of 1-(41-isopropylphenyl)-4-(42-chlorophenyl)5,6,7,8-tetrahydro-2,4а-diazacyclopenta[cd]azulene-2-carboxylic acid arylamides against PC-3 prostate cancer cells

2019 ◽  
Vol 13 (5) ◽  
pp. 331-337
Author(s):  
S. A. Demchenko ◽  
Yu. A. Fedchenkova ◽  
T. А. Bukhtiarova ◽  
L. S. Bobkova ◽  
V. V. Sukhoveev ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Carboxylic Acid ◽  
Antitumor Activity ◽  
Cancer Cells ◽  
Quaternary Salt ◽  
In Vitro Test ◽  
Prostate Cancer Cells ◽  
Naoh Solution ◽  
Acid Arylamides

Pharmacotherapy of prostate cancer is an important part in combating oncologic diseases. This is very relevant, because prostate cancer is a cause of 10 % of deaths from all cancerous diseases in males. The aim of the study – to synthesize novel derivatives of 1-(41-isopropylphenyl)-4-(42-chlorophenyl)5,6,7,8-tetrahydro-2,4а-diazacyclopenta[cd]azulene-2-carboxylic acid arylamides and to evaluate their antitumor activity against PC-3 prostate cancer cells. By reaction of equimolar amounts of 2-methoxy-3,4,5,6-tetrahydro-7H-azepine with a-amino-4-chloroacetophenone chlorohydrate, 3-(4-chlorophenyl)-6,7,8,9- tetrahydro-5Н-imidazo[1,2-a]azepine was synthesized. By alkylation of a-bromo-4-іsopropylacetophenone in ethylacetate and following treatment of the obtained intermediary quaternary salt with excess of 5 % NaOH solution,1-(41-isopropylphenyl)-4-(42chlorophenyl)-5,6,7,8-tetrahydro-2,4а-diazacyclopenta[cd] azulene was synthesized. By boiling it with equimolar amounts of correspondding arylisocyanates in dried benzol, an array of 1-(41-iso propylphenyl)-4(42-chlorophenyl)-5,6,7,8-tetrahydro-2,4а-diazacyclopenta[cd]azulene-2-carboxylic acid arylamides were synthesized. Structure and purity of all compounds obtained were confirmed by data of MR1Н spectroscopy. Lipophilicity (LogP) of compounds 6 and 8 a-i was calculated with the ACD LogP program. Antitumor activity of 1-(41-isopropylphenyl)-4-(42-chlorophenyl)-5,6,7,8-tetrahydro-2,4а-diazacyclopenta[cd]azulene-2-carboxylic acid (3-methylphenyl) and (3-methoxyphenyl)-amides was evaluated at in vitro test on prostate cancer PC-3 cell lines. It is indicated, that at concentration of 10–5 M these compounds exceed 5-fluorouracil as comparison drug in inhibiting PC-3 prostate cancer cells growth by 52.32 % and 3.93 % correspondingly. The data obtained substantiate feasibility of further studies of 1-(41-isopro pylphenyl)-4-(42-chlorophenyl)-5,6,7,8-tetrahydro-2,4а-diazacyclopenta[cd] azulene-2-carboxylic acid arylamides as new, potential antitumor medicines for prostate cancer treatment.

scholarly journals Lx2-32c, a novel semi-synthetic taxane, exerts antitumor activity against prostate cancer cells in vitro and in vivo

2017 ◽  
Vol 7 (1) ◽  
pp. 52-58 ◽  
Author(s):  
Guangyao Lv ◽  
Dengjun Sun ◽  
Jingwen Zhang ◽  
Xiaoxia Xie ◽  
Xiaoqiong Wu ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Antitumor Activity ◽  
Cancer Cells ◽  
Prostate Cancer Cells

scholarly journals Antitumor Activity of Hyaluronic Acid Synthesis Inhibitor 4-Methylumbelliferone in Prostate Cancer Cells

2010 ◽  
Vol 70 (7) ◽  
pp. 2613-2623 ◽  
Author(s):  
Vinata B. Lokeshwar ◽  
Luis E. Lopez ◽  
Daniel Munoz ◽  
Andrew Chi ◽  
Samir P. Shirodkar ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Hyaluronic Acid ◽  
Antitumor Activity ◽  
Cancer Cells ◽  
Acid Synthesis ◽  
Prostate Cancer Cells ◽  
Synthesis Inhibitor

scholarly journals Inhibition of Hypoxia Inducible Factor Alpha and Astrocyte-Elevated Gene-1 Mediates Cryptotanshinone Exerted Antitumor Activity in Hypoxic PC-3 Cells

2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Hyo-Jeong Lee ◽  
Deok-Beom Jung ◽  
Eun Jung Sohn ◽  
Hanna Hyun Kim ◽  
Moon Nyeo Park ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Antitumor Activity ◽  
Cancer Cells ◽  
Untreated Control ◽  
Hypoxia Inducible Factor ◽  
Treated Group ◽  
Tube Formation ◽  
Cellular Level ◽  
Prostate Cancer Cells ◽  
Ki 67

Although cryptotanshinone (CT) was known to exert antitumor activity in several cancers, its molecular mechanism under hypoxia still remains unclear. Here, the roles of AEG-1 and HIF-1αin CT-induced antitumor activity were investigated in hypoxic PC-3 cells. CT exerted cytotoxicity against prostate cancer cells and suppressed HIF-1αaccumulation and AEG-1 expression in hypoxic PC-3 cells. Also, AEG-1 was overexpressed in prostate cancer cells. Interestingly, HIF-1αsiRNA transfection enhanced the cleavages of caspase-9,3, and PAPR and decreased expression of Bcl-2 and AEG1 induced by CT in hypoxic PC-3 cells. Of note, DMOG enhanced the stability of AEG-1 and HIF-1αduring hypoxia. Additionally, CT significantly reduced cellular level of VEGF in PC-3 cells and disturbed tube formation of HUVECs. Consistently, ChIP assay revealed that CT inhibited the binding of HIF-1αto VEGF promoter. Furthermore, CT at 10 mg/kg suppressed the growth of PC-3 cells in BALB/c athymic nude mice by 46.4% compared to untreated control. Consistently, immunohistochemistry revealed decreased expression of Ki-67, CD34, VEGF, carbonic anhydrase IX, and AEG-1 indices in CT-treated group compared to untreated control. Overall, our findings suggest that CT exerts antitumor activity via inhibition of HIF-1α, AEG1, and VEGF as a potent chemotherapeutic agent.

scholarly journals Study of antitumor activity of synthetic peptide ryqlhpyr on the prostate cancer cells

2019 ◽  
Vol 18 (2) ◽  
pp. 40-50
Author(s):  
N. P. Akentieva ◽  
S. S. Shushanov
Keyword(s):  
Prostate Cancer ◽  
Antitumor Activity ◽  
Cancer Cells ◽  
Tumor Cells ◽  
Synthetic Peptide ◽  
Caspase 3 ◽  
Therapeutic Potential ◽  
Prostate Cancer Cells ◽  
Embryonic Fibroblasts ◽  
Targeting Peptide

Introduction . The RHAMM (hyaluronan mediated mobility receptor) is overexpressed in many types of human cancer and increased synthesis of the RHAMM usually correlates with a poor prognostic factor. In this paper, we synthesized the peptide-RYQLHPYR modulating the activity of the RHAMM and examined the therapeutic potential of this RHAMM-targeting peptide as an antitumor agent.Objective . Study the effect of the synthetic peptide RYQLHPYR on viability, apoptosis, necrosis, caspase-3 / 7 activity, and invasion of prostate cancer cells.Materials and methods . The peptide RYQLHPYR was prepared by solid phase synthesis. Human prostate cancer cells (PC3 m-LN4), murine embryonic fibroblasts and murine embryonic fibroblasts (RHAMM- / -). To quantify the effect of the peptide on apoptosis and cell necrosis, ELISAPLUS was used. The activity of caspase-3 / 7 was determined by the colorimetric method. Evaluation of the anti-metastatic effect of the peptide in vitro was evaluated by invasion of cells by quantitative analysis of the area of degradation of fluorescent gelatin.Results . It was found that the peptide RYQLHPYR inhibited the growth of tumor cells PC3 m-LN4 at a concentration of 10 μg / ml (2 × 10–7 M) after 24 h by ~80 %. It was shown that the peptide stimulated the level of apoptosis in cancer cells, approximately 10-fold. It was found that the peptide increased the necrotic death of tumor cells by 2.5 times. During the research it was revealed that the peptide increased the caspase-3 / 7 activity in tumor cells by 2 times. At the same time, it was shown that RHAMM-targeting peptide had no significant effect on apoptosis and necrosis of normal cells (fibroblasts) and fibroblasts (RHAMM- / -). It was found that the peptide inhibited invasion of tumor cells by ~99.86 % at a concentration of 10 μg / ml (2 × 10–7 M).Conclusions . The obtained results indicate that the peptide RYQLHPYR has antitumor activity and, therefore, has a therapeutic potential for the treatment of prostate cancer. 

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