scholarly journals Studies of in vitro anti-prostate cancer potential of newer 1,2,4-triazolo-1,3,4-thiadiazines with different heteroaromatics

2015 ◽  
Vol 10 (2) ◽  
pp. 308 ◽  
Author(s):  
Mao-Chuan Fan ◽  
Guang-Ye Han ◽  
Xin-Jun Zhang ◽  
Hui-Fang Xi
Keyword(s):  
Prostate Cancer ◽  
Nmr Spectroscopy ◽  
Cell Lines ◽  
Prostate Cancer Cell ◽  
Cytotoxic Agents ◽  
Prostate Cancer Cell Lines ◽  
H Nmr ◽  
Ft Ir ◽  
C Nmr

<p>This study was aimed to evaluate anticancer potential of newer synthesize 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines and its derivatives. All newly furnished scaffolds were subjected to screening for their in vitro anticancer potential against DU-145 and PC-3 prostate cancer cell lines using SRB and MMT bioassays. The structures of final compounds were confirmed with the aid of FT-IR, <sup>1</sup>H NMR, <sup>13</sup>C NMR spectroscopy and CHN analysis. Bioassay studies suggested that all thiadiazines were promising cytotoxic agents with % cytotoxicity ranging from 44.39-71.24%, whereas potent GI<sub>50</sub> level in the range 11.96-32.51 µg/mL and results were comparable to the potencies of control drugs adriamycin and doxorubicin. Variation of heterocyclic pharmacophores along with the C-5 position of 1,2,4-triazole in terms of quinoline, quinazoline, coumarin and pyridine lead to the different SAR predictions in which quinoline and benzimidazole moieties found most promising.</p><p> </p>

scholarly journals Some Wild Edible Mushroom Anticancer Activity Against Prostate Cell Lines

Proceedings ◽  
2019 ◽  
Vol 40 (1) ◽  
pp. 40
Author(s):  
Hatice Bekci ◽  
Mustafa Cam ◽  
Ahmet Cumaoglu
Keyword(s):  
Prostate Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Prostate Cancer Cell ◽  
Cancer Cell Lines ◽  
Anticancer Activities ◽  
Prostate Cancer Cell Lines ◽  
Prostate Cell

Prostate cancer is one of the cause of mortality and morbidity in men. High nutritional quality mushrooms have been consumed as food for a long time and Thanks to their bioactive components, they can be used in many fields such as pharmaceuticals, cosmetic products, dietary supplements and functional food production. The purpose of the research was to evaluate these derivatives against in vitro to obtain novel specific and effective anticancer agents against prostate cancer. In the study, Amanita caesarea, Sparassis crispa, Lepista nuda, Auricularia auricula, Tricholoma terreum and Lentinus tigrinus fungi were used. Anticancer activities of the compounds were evaluated in vitro by using MTT method against PC-3 and DU-143 (androgen-independent human prostate cancer cell lines) prostate cancer cell lines. Cisplatin was used as the positive sensitivity reference standard. The most effective among these fungus species biological activity against PC3 cancer cell line (IC50 = 327.34 µM), against DU-145 (IC50 = 459.19 µM).

scholarly journals Assessment of In Vitro Bioactivities of Polysaccharides Isolated from Hericium Novae-Zealandiae

Antioxidants ◽  
2019 ◽  
Vol 8 (7) ◽  
pp. 211 ◽  
Author(s):  
Zhixia (Grace) Chen ◽  
Karen Suzanne Bishop ◽  
Hartono Tanambell ◽  
Peter Buchanan ◽  
Siew Young Quek
Keyword(s):  
Prostate Cancer ◽  
New Zealand ◽  
Cell Lines ◽  
Cancer Cell ◽  
Proliferative Activity ◽  
Prostate Cancer Cell ◽  
Cancer Cell Lines ◽  
Water Soluble ◽  
Prostate Cancer Cell Lines

The objective of this study was to investigate the potential effect of the polysaccharides isolated from Hericium novae-zealandiae, a native New Zealand fungus, on the in vitro proliferation of prostate cancer cell lines, gene expression, acetylcholinesterase (AChE) activity, and oxidation. One water-soluble and two alkali-soluble polysaccharide fractions were isolated from H. novae-zealandiae. The proliferation of the prostate cancer cell lines DU145, LNCaP, and PC3 was evaluated following treatment with these polysaccharide fractions. It was found that the polysaccharides possess anti-proliferative activity on LNCaP and PC3 cells, with a 50% growth inhibition (IC50) value as low as 0.61 mg/mL in LNCaP. Subsequently, it was determined through via RT-qPCR assay that apoptosis was one of the possible mechanisms responsible for the anti-proliferative activity in LNCaP. This was supported by the up-regulation of CASP3, CASP8, and CASP9. An alternative, discovered in PC3, was revealed to be anti-inflammation, which was hinted at by the down-regulation of IL6 and up-regulation of IL24. The polysaccharides also exhibited antioxidant and weak AChE inhibitory activities. This is the first report on the potential health benefits of polysaccharides prepared from the New Zealand fungus, H. novae-zealandiae.

In vitro efficacy of MAGMAS inhibition in prostate cancer.

2014 ◽  
Vol 32 (4_suppl) ◽  
pp. 281-281
Author(s):  
Benjamin C. Powers ◽  
Bhaskar Das ◽  
Boumediene Bouzahzah ◽  
Peter J. Van Veldhuizen ◽  
Emma Borrego-Diaz Reyes
Keyword(s):  
Prostate Cancer ◽  
Cell Proliferation ◽  
Cell Lines ◽  
Cancer Cell ◽  
Prostate Cancer Cell ◽  
Cancer Cell Lines ◽  
Prostate Cancer Cell Lines ◽  
Gm Csf ◽  
Androgen Independent

281 Background: Prostate cancer is the second most common cancer worldwide in males. The initial treatment in advanced cases is medical or surgical castration. The outlook declines when prostate cancer advances independently, despite the aforementioned castration. Within the last ten years, a handful of new agents have proven effective in this castration-resistant phase, but finding more effective, novel ways of treating advanced prostate cancer is warranted. MAGMAS (mitochondria-associated, granulocyte-macrophage colony stimulating factor (GM-CSF) signaling molecule) is a protein ubiquitously expressed in eukaryotic cells that plays a key role in embryonal development in a variety of species. Overexpression of MAGMAS has anti-apoptotic effects, as GM-CSF is a growth factor essential for survival, proliferation and differentiation of cells. MAGMAS and GM-CSF receptor levels have been shown to be overexpressed in prostate cancer, but do not correlate with pathological grade or clinical stage. The purpose of our study was to evaluate the efficacy of a MAGMAS inhibitor, synthesized by Dr Bhaskar Das, in androgen-dependent and androgen-independent prostate cancer cell lines, as well as in a normal prostate cell line as another control. Methods: The different cell lines were treated with MAGMAS inhibitor at various concentrations in vitro. For analysis, we used MTT Cell Proliferation assay at 24 and 48 hours, per manufacturer’s protocol. We tested MAGMAS inhibitor effect on apoptosis/necrosis, cell migration and microtubule destabilization as well. Results: After prostate cancer cell lines were treated with MAGMAS inhibitor in vitro, cell proliferation and migration decreased, apoptosis and necrosis were induced, and microtubules were destabilized, all showing more impressive results in the androgen-independent cells. MAGMAS inhibition did not affect cell proliferation in the normal prostate cells. Conclusions: In vitro studies show MAGMAS inhibition proves efficacious in both androgen-dependent and androgen-independent prostate cancer cell lines. This will be evaluated further in a xenograft mouse model.

250: In Vitro Cytotoxic Effects of Imatinib in Combination with Anticancer Drugs in Human Prostate Cancer Cell Lines

2005 ◽  
Vol 173 (4S) ◽  
pp. 68-69
Author(s):  
Hubert Kübler ◽  
Heiner van Randenborgh ◽  
Uwe Treiber ◽  
Sebastian Wutzler ◽  
Antonie Lehmer ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cell Lines ◽  
Anticancer Drugs ◽  
Cancer Cell ◽  
Prostate Cancer Cell ◽  
Human Prostate Cancer ◽  
Human Prostate Cancer Cell ◽  
Cytotoxic Effects ◽  
Prostate Cancer Cell Lines

Prostate cancer inhibitory activity of a novel dual inhibitor, EL102, in combination with docetaxel, and its effects on MDR1-mediated drug resistance in vitro.

2012 ◽  
Vol 30 (15_suppl) ◽  
pp. e15126-e15126
Author(s):  
Sharon A. Glynn ◽  
Aidan Toner ◽  
Joe Lewis ◽  
Frank Sullivan ◽  
Laura Breen ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Drug Resistance ◽  
Mouse Models ◽  
Cell Lines ◽  
Cancer Cell ◽  
Prostate Cancer Cell ◽  
Drug Resistant ◽  
Prostate Cancer Cell Lines ◽  
Androgen Independent

e15126 Background: EL102 is a dual-action drug promoting apoptosis and inhibiting angiogenesis. It exerts its action though the inhibition of Hif1a induced hypoxic signalling and induction of the Caspase 3/7 apoptotic cascade. The drug has equal activity in normoxia and hypoxia indicating it may be equally active in these different tumor compartments. We tested its ability to circumvent chemotherapeutic drug resistance. Methods: We assessed the ability of EL102 to inhibit prostate cancer cell proliferation and motility in vitro, calculating IC50s for CWR22, 22Rv2, PC3 and DU145 prostate cancer cell lines, comparing sensitivity between androgen dependent, androgen independent and metastatic prostate cancer. Additionally we assessed the activity of EL102 in combination with docetaxel in vitro and in murine CWR22 xenografts. The ability to overcome MDR1 and BCRP mediated drug resistance was also tested using DLKP drug resistant variants which exhibit 200 fold resistance to doxorubicin, docetaxel, paclitaxel and vincristine. Results: We found that prostate cancer cell lines are sensitive to EL102 with IC50s in the region of 10-50nM. Of particular interest was the identical sensitivity of the androgen independent 22Rv1 and its androgen dependent parent CWR22, suggesting ability to overcome hormone refractory prostate cancer. Additionally we demonstrate dose response for inhibition of cell motility in metastatic DU145. In CWR22 murine mouse models treatment with EL102 resulted in decreased tumor volume compared to control. A docetaxel and EL102 combination arm demonstrated the greater inhibition of tumor growth than EL102 or docetaxel alone. The lung cancer cell line DLKP, its drug resistant variants DLKPA (MDR1 overexpressing) and DLKPMitox (BCRP overexpressing) were equally sensitive to EL102 indicating that EL102 is not a substrate for MDR1 or BCRP. Conclusions: EL102 is a potential therapeutic for the treatment of prostate cancer, in particular in combination with docetaxel, and exhbibits the potential to overcome drug resistane. Future studies will include the efficacy of this drug in prostate cancer metastatic mouse models.

scholarly journals Imaging ToF-SIMS and synchrotron-based FT-IR microspectroscopic studies of prostate cancer cell lines

2004 ◽  
Vol 231-232 ◽  
pp. 452-456 ◽  
Author(s):  
E. Gazi ◽  
N.P. Lockyer ◽  
J.C. Vickerman ◽  
P. Gardner ◽  
J. Dwyer ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Prostate Cancer Cell ◽  
Cancer Cell Lines ◽  
Prostate Cancer Cell Lines ◽  
Tof Sims ◽  
Ft Ir
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