• Asian Pacific Journal of Cancer Prevention
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• v.14 no.9
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• pp.5421-5425
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• 2013

Background: To assess the antioxidant effects of gamma-oryzanol on human prostate cancer cells. Materials and Methods: Cytotoxic activity of gamma-oryzanol on human DU145 and PC3 prostate cancer cells was determined by proliferation assay using 3-(4, 5-dimethylthiazol, 2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) reagent. mRNA levels of genes involved in the intracellular antioxidant system, superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPX) and glutathione reductase (GSR) were determined by reverse transcription-polymerase chain reaction (RT-PCR). Cancer cell lysates were used to measure lipid peroxidation using thiobarbituric acid reactive substance (TBARS). Glutathione contents of the cell lysates were estimated by the reaction between sulfhydryl group of 5, 5'-dithio (bis) nitrobenzoic acid (DTNB) to produce a yellow-color of 5-thio-2-nitrobenzoic acid using colorimetric assay. Catalase activity was also analysed by examining peroxidative function. Protein concentration was estimated by Bradford's assay. Results: All concentrations of gamma-oryzanol, 0.1-2.0mg/ml, significantly inhibited cell growth in a dose- and time-dependent fashion in both prostate cancer cell lines, DU145 and PC3. Gene expression of catalase in DU145 and PC3 exposed to gamma-orizanol at 0.5mg/ml for 14 days was down regulated, while mRNA of GPX was also down regulated in PC3. The MDA and glutathione levels including catalase activity in the cell lysates of DU145 and PC3 treated with gamma-oryzanol 0.1 and 0.5mg/ml were generally decreased. Conclusions: This study highlighted effects of gamma-oryzanol via the down-regulation of antioxidant genes, catalase and GPX, not cytotoxic roles. This might be interesting for adjuvant chemotherapy to make prostate cancer cells more sensitive to free radicals. It might be useful for the reduction of cytotoxic agents and cancer chemoprevention.

• The Korean Journal of Physiology and Pharmacology
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• v.17 no.6
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• pp.517-523
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• 2013

Naphthyridine compounds are important, because they exhibit various biological activities including anticancer, antimicrobial, and anti-inflammatory activity. Some naphthyridines have antimitotic effects or demonstrate anticancer activity by inhibiting topoisomerase II. These compounds have been investigated as potential anticancer agents, and several compounds are now part of clinical trials. A series of naphthyridine derivatives were evaluated for their in vitro cytotoxic activities against human cervical cancer (HeLa), leukemia (HL-60), and prostate cancer (PC-3) cell lines using an MTT assay. Some compounds (14, 15, and 16) were more potent than colchicine against all three human cancer cell lines and compound (16) demonstrated potency with $IC_{50}$ values of 0.7, 0.1, and $5.1{\mu}M$, respectively. Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were used for quantitative structure-activity relationship (QSAR) molecular modeling of these compounds. We obtained accurate and predictive three-dimensional QSAR (3D-QSAR) models as indicated by the high PLS parameters of the HeLa ($q^2$, 0.857; $r^2$, 0.984; $r^2\;_{pred}$, 0.966), HL-60 ($q^2$, 0.777; $q^2$, 0.937; $r^2\;_{pred}$, 0.913), and PC-3 ($q^2$, 0.702; $q^2$, 0.983; $r^2\;_{pred}$, 0.974) cell lines. The 3D-QSAR contour maps suggested that the C-1 NH and C-4 carbonyl group of the naphthyridine ring and the C-2 naphthyl ring were important for cytotoxicity in all three human cancer cell lines.

• Journal of the Korean Chemical Society
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• v.63 no.2
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• pp.85-93
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• 2019

A panel of chalcone-sulphonamide hybrids has been designed by tethering appropriate sulphonamide scaffold with substituted chalcones as a multi-target drug for anticancer screening. Chalcones were prepared by Claisen-Schmidt condensation reaction of a substituted aldehyde with para aminoacetophenone. All the synthesized compounds were evaluated against selected five cancer cell lines, MCF-7 (Breast cancer), DU-145 (Human prostate Carcinoma), HCT-15 (Colon cancer), NCIH-522 (stage 2, adenocarcinoma; non-small cell lung cancer) and HT-3 (Human cervical cancer). Most of the synthesized chalcone-sulphonamide hybrids showed amended cytotoxic activity against various cancer cell lines which may be attributed to the linkage of sulphonamide with chalcone skeleton. The synthesized compounds were characterized by FT-IR, $^1H$ NMR, $^{13}C$ NMR and HR-LCMS and spectral study assert the structures of synthesized sulphonamide-chalcone hybrids.

• Journal of Physiology & Pathology in Korean Medicine
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• v.17 no.5
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• pp.1309-1314
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• 2003

We examined the effects of Oak Smoke Flavoring (OSF, Holyessing) on the cell proliferation of DU145 and PC3 human prostate carcinoma cell line. OSF treatment resulted in a concentration-dependent inhibition of the cell viability in both DU145 and PC3 cell lines. The anti-proliferative effects by OSF treatment in DU145 and PC3 cells were associated with morphological changes such as membrane shrinking and cell rounding up. DNA flow cytometric histograms showed that population of S phase of the cell cycle was increased by OSF treatment in a dose-dependent manner. Western blot analysis revealed that cyclin B1 and cdc2 proteins were reduced by OSF treatment in DU145 cells, whereas cyclin A was markedly inhibited in PC3 cells. Furthermore, we observed an increase of Cdk inhibitor p16 and p27 protein, and an inhibition of phosphorylation of pRB by OSF treatment in a dose-dependent manner. The present results indicated that OSF-induced inhibition of human prostate carcinoma cell proliferation is associated with the blockage of S phase progression.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.17
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• pp.7641-7651
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• 2015

It has been shown previously that nutritional supplements rich in polyphenolic compounds play a significant role in prostate cancer chemoprevention. Propolis is a natural, resinous hive product that has several pharmacological activities including antimicrobial, antioxidant, anti-inflammatory, and antitumoral activities. The aim of this study was to compare the cytotoxic, antioxidant and antitumoral activities of an ethanolic extract of Egyptian propolis (EEP) in vitro with an established chemotherapeutic drug such as doxorubicin (DOX), and the effects of their combination against the PC3 human prostate cancer cell line. Cellular viability and $IC_{50}$ levels with EEP, DOX and their (v/v) combination were detected by sulphorhodamine-B (SRB) assay after incubation of PC3 cells for 72h with different doses (0, 0.01, 0.1, 1, 10 and $100{\mu}g/ml$). Two selected doses of $IC_{50}$ and $IC_{25}$ were applied to cells for 24h for antitumor evaluation assay of treatment compounds. EEP and its (v/v) combination with DOX showed significant antitumor potential besides high antioxidant properties of superoxide dismutase (SOD), total antioxidant capacity (TAC), catalase (CAT), nitric oxide (NO) and reduced glutathione (GSH) levels when compared with the control untreated cells. DNA fragmentation assay and semi quantitative RT-PCR analyses for p53 and Bax genes showed that EEP activated cellular apoptosis and increased the mRNA expression levels more than other treatment. In conclusion, EEP alone or in combination with DOX at both doses used here showed greater antioxidant, antiproliferative and apoptotic effects against the PC3 cell lines as compared to treatment with DOX alone. Therefore, EEP could be considered as a promising candidate for prostate cancer chemotherapy.

• Journal of the Korean Society of Radiology
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• v.14 no.6
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• pp.755-762
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• 2020

This study is desinged to examine the effects of Taheebo(Tabebuia avellanedae) extract on the prostate of male rats as a natural radiation protection agent. Taheebo extract is well known to inhibit cell growth for the cell lines of breast and prostate cancer. In this study, the X-ray 7 Gy was irradiated in the prostate of male rat to identify radiation protection effects by Taheebo Extracts, 1, 7, and 21 Days later, hematological changes, external toxicity assessments(LDH), antioxidant enzyme(SOD) activity changes and tissue change were observed. IR+TH group showed greater lymphocyte levels than the irradiation group, which is believed to affect the hematopoietic immune system's resilience. As a results of the external toxicity assessment, Taheebo extract's toxicity is maximum 18.128±5.16%, minimum 13.6945±4.43%. Taheebo is considered to be of little toxicity. The composition of prostate cell nuclei and cytoplasm in Control and TH group was honogeneous, whereas the cell nucleus cohesion in the prostate in irradiation group and inflammatory reactions in cytoplasm were shown. IR+TH group showed less inflammatory reactions of cytoplasm in the prostate than in the radiation irradiation group, but showed a cohesive phenomenon of cell nuclei. It is judged that Taheebo extract has radiation protection against prostate cells.

• Asian Pacific Journal of Cancer Prevention
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• v.17 no.4
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• pp.1739-1744
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• 2016

We report herein an in vitro anticancer evaluation of a series of seven curcumin analogues (3a-g). The National Cancer Institute (NCI US) Protocol was followed and all the compounds were evaluated for their anticancer activity on nine different panels (leukemia, non small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer) represented by 60 NCI human cancer cell lines. All the compounds showed significant anticancer activity in one dose assay (drug concentration $10{\mu}M$) and hence were evaluated further in five dose assays (0.01, 0.1, 1, 10 and $100{\mu}M$) and three dose related parameters $GI_{50}$, TGI and $LC_{50}$ were calculated for each (3a-g) in micro molar drug concentrations (${\mu}M$). The compound 3d (NSC 757927) showed maximum mean percent growth inhibition (PGI) of 112.2%, while compound 3g (NSC 763374) showed less mean PGI of 40.1% in the one dose assay. The maximum anticancer activity was observed with the SR (leukemia) cell line with a $GI_{50}$ of $0.03{\mu}M$. The calculated average sensitivity of all cell lines of a particular subpanel toward the test agent showed that all the curcumin analogues showed maximum activity on leukemia cell lines with $GI_{50}$ values between 0.23 and $2.67{\mu}M$.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.3
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• pp.1031-1038
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• 2012

Background: Turmeric ($Curcuma$ $longa$) has been shown to possess anti-inflammatory, antioxidant and antitumor properties. However, despite the progress in research with $C.$ $longa$, there is still a big lacuna in the information on the active principles and their molecular targets. More particularly very little is known about the role of cell cycle genes $p57^{kip2}$ and Rad9 during chemoprevention by turmeric and its derivatives especially in prostate cancer cell lines. Methods: Accordingly, in this study, we have examined the antitumor effect of several extracts of $C.$ $longa$ rhizomes by successive fractionation in clonogenic assays using highly metastatic PC-3M prostate cancer cell line. Results: A mixture of isopropyl alcohol: acetone: water: chloroform: and methanol extract of $C.$ $longa$ showed significant bioactivity. Further partition of this extract showed that bioactivity resides in the dichloromethane soluble fraction. Column chromatography of this fraction showed presence of biological activity only in ethyl acetate eluted fraction. HPLC, UV-Vis and Mass spectra studies showed presence three curcuminoids in this fraction besides few unidentified components. Conclusions: From these observations it was concluded that the ethyl acetate fraction showed not only inhibition of colony forming ability of PC-3M cells but also up-regulated cell cycle genes $p57^{kip2}$ and Rad9 and further reduced the migration and invasive ability of prostate cancer cells.

• Proceedings of the Zoological Society Korea Conference
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• 1997.10b
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• pp.205.2-205
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• 1997

No Abstract, See Full Text

• Journal of Life Science
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• v.21 no.11
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• pp.1573-1578
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• 2011

Milk thistle (silybum marianum) is a famous dietary supplement widely used in the United States and Europe. Silbinin is a major biologically active compound of milk thistle and has strong antioxidant and radical scavenger activities. Anticancer activities, as well as chemopreventive effects on various cancer cell lines, including prostate, lung, colon, skin, and bladder, have also been reported in silbinin. In the present study, we investigated the anticancer effects of silibinin and apoptosis through cell cycle arrest on prostate cancer cell PC-3. We performed cell viability by MTT assay and western blotting to confirm cell cycle check point proteins such as cyclin A/D1/E and cyclin-dependent kinase (CDK) 2/4/6. To quantify silibinin-induced apoptotic cell death of PC-3, Annexin V and PI double staining was performed by flow cytometry, by which its cell distribution was determined. As a result, silibinin inhibited the cell growth of PC-3 cells in a time- and dose-dependent manner, and its treatment resulted in cell cycle arrest at the G1 phase. Also the level of cell cycle check point proteins (cyclin, CDK) was decreased by silibinin in a dose-dependent manner. Taken together, we suggest that apoptosis of prostate cancer cell line PC-3 induced by silibinin is associated with cell cycle arrest through decrease of cell cycle check point proteins, caspase-3 activation and poly (ADP-ribose) polymerase (PARP) cleavage.