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Anticancer Properties (anticancer + property)
Selected AbstractsAmido-Functionalised Prodigiosenes: Synthesis and Anticancer PropertiesCHEMMEDCHEM, Issue 5 2009Abstract Prodigiosin: Amido-functionalised prodigiosin-derived compounds were synthesised via a robust and efficient synthetic route. These compounds were then evaluated against 60 human cell lines consisting of nine diverse tumour cell types and their anticancer activities were assessed. [source] Photocarcinogenesis of topical tazarotene and isotretinoin alone and in combination with valproic acid in hairless miceEXPERIMENTAL DERMATOLOGY, Issue 11 2008Catharina M. Lerche Abstract:, Retinoids and the histone deacetylase inhibitor valproic acid have shown anticancer properties, but the photocarcinogenic or photoprotective effect is unclear. Therefore, we investigated whether a topical formulation of valproic acid is photocarcinogenic or photoprotective in hairless female C3.Cg/TifBomTac immunocompetent mice exposed to simulated solar radiation (SSR) and whether valproic acid changes the effect of the retinoids: tazarotene and isotretinoin. The products were applied on the dorsal skin of 400 mice (five times weekly) followed by SSR (three times weekly) 3,4 h after the application. This was performed during 12 months or until death. Tumors appeared sooner in groups treated with tazarotene and isotretinoin compared with that of the group treated with valproic acid and the control group. The present study shows that valproic acid alone is not photocarcinogenic or photoprotective in hairless mice. When valproic acid is combined with tazarotene or isotretinoin, it does not change their photocarcinogenicity significantly. [source] PPAR, and PP2A are involved in the proapoptotic effect of conjugated linoleic acid on human hepatoma cell line SK-HEP-1INTERNATIONAL JOURNAL OF CANCER, Issue 11 2007Giuliana Muzio Abstract Conjugated linoleic acid (CLA), found in dairy products, in beef and lamb has been demonstrated to possess anticancer properties protecting several tissues from developing cancer. Moreover, it has been shown to modulate apoptosis in several cancer cell lines. The aim of this study was to investigate which signaling transduction pathways were modulated in CLA-induced apoptosis in human hepatoma SK-HEP-1 cells. The cells exposed to CLA were evaluated for PPAR,, PP2A, pro-apoptotic proteins Bak, Bad and caspases, and anti-apoptotic proteins Bcl-2 and Bcl-XL. Cells were also treated with okadaic acid, a PP2A inhibitor, or with Wy-14643, a specific PPAR, agonist. The CLA-induced apoptosis was concomitant to the increase of percentage of cells in the S phase, PPAR,, PP2A and pro-apoptotic proteins; simultaneously, antiapoptotic proteins decreased. Inhibition of PP2A prevented apoptosis, and PPAR, agonist showed similar effect as CLA. The increased PP2A could be responsible for the dephosphorylation of Bcl-2 and Bad, permitting apoptotic activity of Bax and Bad. The increase of caspase 8 and 9 suggested that both the intrinsic and extrinsic apoptotic pathways were induced. PP2A was probably increased by PPAR,, since putative PPRE sequences were found in genes encoding its subunits. In conclusion, CLA induces apoptosis in human hepatoma SK-HEP-1 cells, by increasing PPAR,, PP2A and pro-apoptotic proteins. © 2007 Wiley-Liss, Inc. [source] Modulatory potential of ellagic acid, a natural plant polyphenol on altered lipid profile and lipid peroxidation status during alcohol-induced toxicity: A pathohistological studyJOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY, Issue 2 2008Nagarajan Devipriya Abstract Polyphenol-rich dietary foodstuffs, consumed as an integral part of vegetables, fruits, and beverages have attracted attention due to their antioxidant and anticancer properties. Ellagic acid (EA), a polyphenolic compound widely distributed in fruits and nuts, has been reported to scavenge free radicals and inhibit lipid peroxidation. Chronic consumption of alcohol potentially results in serious illness including hepatitis, fatty liver, hypertriglyceridemia, and cirrhosis. A little is known about the influence of EA on alcohol toxicity in vivo. Accordingly, in the present study, we have evaluated the protective effects of EA on lipid peroxidation and lipid levels during alcohol-induced toxicity in experimental rats. Forty female albino Wistar rats, which were weighing between 150,170 g were used for the study. The toxicity was induced by administration of 20% alcohol orally (7.9 g/kg body wt.) for 45 days. Rats were treated with EA at three different doses (30, 60, and 90 mg/kg body wt.) via intragastric intubations together with alcohol. At the end of experimental duration, liver marker enzymes (i.e., aspartate transaminase, alanine transaminase), lipid peroxidative indices (i.e., thiobarbituriacid reactive substances and hydroperoxides) in plasma, and lipid levels (i.e., cholesterol, free fatty acids, triglycerides and phospholipids) in tissues were analyzed to evaluate the antiperoxidative and antilipidemic effects of EA. Liver marker enzymes, lipid peroxidative indices, and lipid levels, i.e., cholesterol, triglycerides and free fatty acids, were significantly increased whereas phospholipid levels were significantly decreased in the alcohol-administered group. EA treatment resulted in positive modulation of marker enzymes, peroxidative indices, and lipid levels. EA at the dose of 60 mg/kg body wt. was found to be more effective when compared to the other two doses. Histological changes observed were also inconsistent with the biochemical parameters. Our study suggests that EA exerts beneficial effects at the dosage of 60 mg/kg body wt. against alcohol-induced damage, and it can be used as a potential drug for the treatment of alcohol-abuse ailments in the near future. © 2008 Wiley Periodicals, Inc. J Biochem Mol Toxicol 22:101,112, 2008; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/jbt.20226 [source] Anti-aging properties of resveratrol: review and report of a potent new antioxidant skin care formulationJOURNAL OF COSMETIC DERMATOLOGY, Issue 1 2008Richard A Baxter MD Summary Resveratrol, an antioxidant polyphenol from red wine, has been the subject of intense interest in recent years due to a range of unique anti-aging properties. These include cardiovascular benefits via increased nitric oxide production, down-regulation of vasoactive peptides, lowered levels of oxidized low-density lipoprotein, and cyclooxygenase inhibition; possible benefits on Alzheimer's disease by breakdown of beta-amyloid and direct effects on neural tissues; phytohormonal actions; anticancer properties via modulation of signal transduction, which translates into anti-initiation, antipromotion, and antiprogression effects; antimicrobial effects; and sirtuin activation, which is believed to be involved in the caloric restriction-longevity effect. Here we report a resveratrol-based skin care formulation, with 17 times greater antioxidant activity than idebenone. The role of resveratrol in prevention of photoaging is reviewed and compared with other antioxidants used in skin care products. [source] Sodium selenate fertilisation increases selenium accumulation and decreases glucosinolate concentration in rapid-cycling Brassica oleraceaJOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE, Issue 9 2001Craig S Charron Abstract Glucosinolates (GSs) are S-containing compounds found in Brassica species and whose degradation products may provide protection against cancer. Sulphoraphane, a product of 4-methylsulphinylbutyl GS degradation, is a particularly potent inhibitor of anticarcinogenic detoxification enzymes. Selenium also has anticancer properties, and consumption of plants containing Se may be an effective way to increase dietary Se. Since plant uptake of Se and S is competitive, GS synthesis may be affected by Se fertilisation. The objective of this study was to determine how Se fertilisation of rapid-cycling B oleracea would affect Se and GS concentrations. Plants were grown in hydroponic solutions containing 0.0, 1.0, 2.0, 3.0, 6.0, 7.2 or 9.0,mg,l,1 Na2SeO4. Mineral and glucosinolate concentrations were measured in shoots harvested just before anthesis. Total GSs decreased from 5.84,µmol,g,1 (0.0,mg,l,1 Na2SeO4) to 1.90,µmol,g,1 (9.0,mg,l,1Na2SeO4). Levels of 4-methylsulphinylbutyl GS decreased 90% when Na2SeO4 fertilisation was increased from 0 to 1,mg,l,1, and remained low at higher Na2SeO4 concentrations. Shoot Se concentration was undetectable at 0.0,mg,l,1 Na2SeO4 and increased significantly with Na2SeO4 fertilisation. Although B oleracea may not simultaneously deliver high levels of dietary 4-methylsulphinylbutyl GS and Se, levels of other GSs with anticarcinogenic benefits may be beneficial even with Se fertilisation. © 2001 Society of Chemical Industry [source] Complete and unambiguous assignments of 1H and 13C chemical shifts of new arylamino derivatives of ortho -naphthofuranquinonesMAGNETIC RESONANCE IN CHEMISTRY, Issue 12 2008Eufrānio N. da Silva Jśnior Abstract Six new nor-,-lapachones have been synthesized from reaction of 3-bromo-nor-,-lapachone with arylamines. These derivatives have potent anticancer properties against several cell lines. Here, we report complete unambiguous assignments of 1H and 13C chemical shifts of the new compounds. The assignments were made using a combination of one- and two-dimensional NMR techniques (1H, 13C, 1H1H COSY, 1H13C HSQC, and 1H13C HMBC). Copyright © 2008 John Wiley & Sons, Ltd. [source] Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infectionMEDICINAL RESEARCH REVIEWS, Issue 1 2004Robert H. Cichewicz Abstract 3,-Hydroxy-lup-20(29)-en-28-oic acid (betulinic acid) is a pentacyclic lupane-type triterpene that is widely distributed throughout the plant kingdom. A variety of biological activities have been ascribed to betulinic acid including anti-inflammatory and in vitro antimalarial effects. However, betulinic acid is most highly regarded for its anti-HIV-1 activity and specific cytotoxicity against a variety of tumor cell lines. Interest in developing even more potent anti-HIV agents based on betulinic acid has led to the discovery of a host of highly active derivatives exhibiting greater potencies and better therapeutic indices than some current clinical anti-HIV agents. While its mechanism of action has not been fully determined, it has been shown that some betulinic acid analogs disrupt viral fusion to the cell in a post-binding step through interaction with the viral glycoprotein gp41 whereas others disrupt assembly and budding of the HIV-1 virus. With regard to its anticancer properties, betulinic acid was previously reported to exhibit selective cytotoxicity against several melanoma-derived cell lines. However, more recent work has demonstrated that betulinic acid is cytotoxic against other non-melanoma (neuroectodermal and malignant brain tumor) human tumor varieties. Betulinic acid appears to function by means of inducing apoptosis in cells irrespective of their p53 status. Because of its selective cytotoxicity against tumor cells and favorable therapeutic index, even at doses up to 500 mg/kg body weight, betulinic acid is a very promising new chemotherapeutic agent for the treatment of HIV infection and cancer. © 2003 Wiley Periodicals, Inc. Med Res Rev, 24, No. 1, 90,114, 2004 [source] Platinum-based anticancer agents: Innovative design strategies and biological perspectivesMEDICINAL RESEARCH REVIEWS, Issue 5 2003Yee-Ping Ho Abstract The impact of cisplatin on cancer chemotherapy cannot be denied. Over the past 20 years, much effort has been dedicated to discover new platinum-based anticancer agents that are superior to cisplatin or its analogue, carboplatin. Most structural modifications are based on changing one or both of the ligand types coordinated to platinum. Altering the leaving group can influence tissue and intracellular distribution of the drug, whereas the carrier ligand usually determines the structure of adducts formed with DNA. DNA,Pt adducts produced by cisplatin and many of its classical analogues are almost identical, and would explain their similar patterns of tumor sensitivity and susceptibility to resistance. Recently some highly innovative design strategies have emerged, aimed at overcoming platinum resistance and/or to introduce novel mechanisms of antitumor action. Platinum compounds bearing the 1,2-diaminocyclohexane carrier ligand; and those of multinuclear Pt complexes giving rise to radically different DNA,Pt adducts, have resulted in novel anticancer agents capable of circumventing cisplatin resistance. Other strategies have focused on integrating biologically active ligands with platinum moieties intended to selectively localizing the anticancer properties. With the rapid advance in molecular biology, combined with innovation, it is possible new Pt-based anticancer agents will materialize in the near future. © 2003 Wiley Periodicals, Inc. Med Res Rev, 23, No. 5, 633,655, 2003 [source] Antiproliferative activity of Hungarian Asteraceae species against human cancer cell lines.PHYTOTHERAPY RESEARCH, Issue 12 2007Part I Abstract Aqueous and organic extracts of 25 selected species from four tribes of Hungarian Asteraceae were screened in vitro for antiproliferative activity against HeLa (cervix epithelial adenocarcinoma), A431 (skin epidermoid carcinoma) and MCF7 (breast epithelial adenocarcinoma) cells, using the MTT assay. Twenty five of the 228 tested extracts from different parts of the species of Astereae (6), Inuleae (3), Heliantheae (5) and Anthemideae (11) demonstrated a substantial antiproliferative effect (at least 50% inhibition of cell proliferation) at 10 µg/mL against one or more of the cell lines. Complete dose-response curves were generated and IC50 values were calculated for these active extracts, and their direct cytotoxic effects were determined. In summary, 11 of the tested 25 plants were found to be active and 4 of them (Anthemis ruthenica, Erigeron canadensis, Erigeron annuus and Inula ensifolia) had not been studied previously for either active compounds or anticancer properties. Copyright © 2007 John Wiley & Sons, Ltd. [source] Effect of selenium on N-nitrosodiethylamine-induced multistage hepatocarcinogenesis with reference to lipid peroxidation and enzymic antioxidantsCELL BIOCHEMISTRY AND FUNCTION, Issue 1 2001C. Thirunavukkarasu Abstract We have studied the relationship between antioxidant and anticancer properties of selenium (Se) in multistage hepatocarcinogenesis induced by N-nitrosodiethylamine (DEN). In this study we have observed an increased level of lipid peroxide (LPO) products and decreased antioxidant enzyme activities (superoxide dismutase and catalase) in hepatoma and surrounding liver tissues of cancer-bearing animals. Selenium (Se) was supplemented either before initiation or during initiation and selection/promotion phases of hepatocarcinogenesis and was found to be effective in altering hepatic lipid peroxidation and antioxidant enzyme activities to a statistically significant level measured either in the hepatoma or in the surrounding liver tissues. These alterations inclined towards normal in a time-dependent manner on selenium supplementation. Furthermore, increased levels of lipid peroxidation and decreased levels of antioxidants (superoxide dismutase and catalase) were also observed in distant organs of cancer-bearing rats other than the tumour-bearing site. These alterations are brought back to normal levels upon Se treatment. Our results confirm the fact that Se is particularly protective in limiting the action of DEN by its antioxidant property. Copyright © 2001 John Wiley & Sons, Ltd. [source] Induction of cytotoxicity in human lung adenocarcinoma cells by 6- O -carboxypropyl-,-tocotrienol, a redox-silent derivative of ,-tocotrienolINTERNATIONAL JOURNAL OF CANCER, Issue 5 2005Yoshihisa Yano Abstract Tocotrienols are one of the most potent anticancer agents of all natural compounds and the anticancer property may be related to the inactivation of Ras family molecules. The anticancer potential of tocotrienols, however, is weakened due to its short elimination half life in vivo. To overcome the disadvantage and reinforce the anticancer activity in tocotrienols, we synthesized a redox-silent analogue of ,-tocotrienol (T3), 6- O -carboxypropyl-,-tocotrienol (T3E). We estimated the possibility of T3E as a new anticancer agent against lung adenocarcinoma showing poor prognosis based on the mutation of ras gene. T3E showed cytotoxicity against A549 cells, a human lung adenocarcinoma cell line with a ras gene mutation, in a dose-dependent manner (0,40 ,M), whereas T3 and a redox-silent analogue of ,-tocopherol (T), 6- O -carboxypropyl-,-tocopherol (TE), showed much less cytotoxicity in cells within 40 ,M. T3E cytotoxicity was based on the accumulation of cells in the G1-phase of the cell-cycle and the subsequent induction of apoptosis. Similar to this event, 24-hr treatment of A549 cells with 40 ,M T3E caused the inhibition of Ras farnesylation, and a marked decrease in the levels of cyclin D required for G1/S progression in the cell-cycle and Bcl-xL, a key anti-apoptotic molecule. Moreover, the T3E-dependent inhibition of RhoA geranyl-geranylation is an inducing factor for the occurrence of apoptosis in A549 cells. Our results suggest that T3E suppresses Ras and RhoA prenylation, leading to negative growth control against A549 cells. In conclusion, a redox-silent analogue of T3, T3E may be a new candidate as an anticancer agent against lung adenocarcinoma showing poor prognosis based on the mutation of ras genes. © 2005 Wiley-Liss, Inc. [source] Resveratrol attenuates 1,2-dimethylhydrazine (DMH) induced glycoconjugate abnormalities during various stages of colon carcinogenesisPHYTOTHERAPY RESEARCH, Issue 8 2009Murugan Sengottuvelan Abstract Although a myriad of health promoting effects has been attributed to resveratrol (Res) (3,5,4,-trihydroxy- trans -stilbene), a phytoalexin, the most interesting is its anticancer property. The aim of this work was to elucidate the effectiveness of Res against cellular transformation (glycoconjugate alterations) initiated by 1,2-dimethylhydrazine (DMH), a colon specific carcinogen. Group 1 were control rats, group 2 were control rats that received Res (8 mg/kg body weight orally every day), rats in groups 3,6 were treated weekly with DMH (20 mg/kg body weight, subcutaneously × 15 times). In addition, groups 4,6 received Res (as in group 2) in three dietary regimens: initiation (I), post-initiation (PI) and entire period (EP). At the end of the 30 week experimental period in DMH alone exposed rats, altered levels of glycoconjugates (total hexoses, fucose, hexosamine and sialic acid) were observed in liver, intestine and colon tissues. Of the three dietary regimens of Res, the entire period supplementation significantly (p < 0.01) modulated the levels of glycoconjugates and reduced the incidence of adenoma and adenocarcinoma. These findings suggest that Res may extend its chemopreventive effect by restoring the alteration in glycoconjugates that are thought to be involved in the colonic malignant transformation process in this experimental model. Copyright © 2009 John Wiley & Sons, Ltd. [source] | |||||||||||||