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Lars Porskjaer Christensen - One of the best experts on this subject based on the ideXlab platform.
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dietary Polyacetylenes falcarinol and falcarindiol isolated from carrots prevents the formation of neoplastic lesions in the colon of azoxymethane induced rats
2017Co-Authors: Lars Porskjaer Christensen, Rime Bahij Elhouri, Morten Kobaeklarsen, Issam Alnajami, Xavier Frette, Gunnar BaatrupAbstract:Falcarinol (FaOH) and falcarindiol (FaDOH) are found in many food plants of the Apiaceae family. Carrots are a major dietary source of these Polyacetylenes. Feeding azoxymethane (AOM)-induced rats with carrots and purified FaOH have previously been shown to inhibit neoplastic transformations in the colon. FaOH and FaDOH have also shown to have a synergistic effect in vitro, resulting in a significant increased cytotoxic activity. Based on these findings the antineoplastic effect of FaOH and FaDOH (purity > 99%) was investigated in the AOM-induced rat model. Twenty rats received rat diet containing 7 μg FaOH per g feed and 7 μg FaDOH per g feed and 20 rats were controls receiving only rat diet. Then carcinogenesis was induced in all 40 rats with the carcinogen AOM. All animals received the designated diet for 2 weeks before AOM induction and continued on the designated diet throughout the experiment. Rats were euthanized 18 weeks after the first AOM injection and macroscopic polyp/cancers were measured, harvested and stained for histology. The difference in sizes of aberrant crypt foci (ACF) were analysed in a Wilcoxon rank sum test, in which the median number of small ACF was 218 in controls and 145 in polyacetylene treated rats (P < 0.001). Fifteen control rats and 8 treated rats had macroscopic tumors (P = 0.027). The number of tumors larger than 3 mm were 6 and 1 in control and treated rats, respectively (P = 0.032). In conclusion dietary supplements with FaOH and FaDOH reduced the number of neoplastic lesions as well as the growth rate of the polyps suggesting a preventive effect of FaOH and FaDOH on the development of colorectal cancer.
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Polyacetylenes from carrots daucus carota improve glucose uptake in vitro in adipocytes and myotubes
2015Co-Authors: Rime Bahij Elhouri, Dorota Kotowska, Kathrine Bisgaard Christensen, Sumangala Bhattacharya, Niels Oksbjerg, Gerhard Wolber, Karsten Kristiansen, Lars Porskjaer ChristensenAbstract:A dichloromethane (DCM) extract of carrot roots was found to stimulate insulin-dependent glucose uptake (GU) in adipocytes in a dose dependent manner. Bioassay-guided fractionation of the DCM extract resulted in the isolation of the Polyacetylenes falcarinol and falcarindiol. Both Polyacetylenes were able to significantly stimulate basal and/or insulin-dependent GU in 3T3-L1 adipocytes and porcine myotube cell cultures in a dose-dependent manner. Falcarindiol increased peroxisome proliferator-activated receptor (PPAR)γ-mediated transactivation significantly at concentrations of 3, 10 and 30 μM, while PPARγ-mediated transactivation by falcarinol was only observed at 10 μM. Docking studies accordingly indicated that falcarindiol binds to the ligand binding domain of PPARγ with higher affinity than falcarinol and that both Polyacetylenes exhibit characteristics of PPARγ partial agonists. Falcarinol was shown to inhibit adipocyte differentiation as evident by gene expression studies and Oil Red O staining, whereas falcarindiol did not inhibit adipocyte differentiation, which indicates that these Polyacetylenes have distinct modes of action. The results of the present study suggest that falcarinol and falcarindiol may represent scaffolds for novel partial PPARγ agonists with possible antidiabetic properties.
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aliphatic c 17 Polyacetylenes of the falcarinol type as potential health promoting compounds in food plants of the apiaceae family
2011Co-Authors: Lars Porskjaer ChristensenAbstract:: Many epidemiological studies have provided evidence that a high intake of fruits and vegetables is associated with a reduced risk for the development of cancer and cardiovascular diseases. Fruits and vegetables are known to contain health promoting components such as vitamins, minerals, antioxidants and dietary fibers, however, it is unclear which of these are responsible for the health promoting properties of fruits and vegetables. Aliphatic C(17)-Polyacetylenes of the falcarinol type, which occur in common food plants of the Apiaceae family such as carrot, celeriac, parsnip and parsley, have demonstrated interesting bioactivities including antibacterial, antimycobacterial, and antifungal activity as well as anti-inflammatory, anti-platelet-aggregatory, neuritogenic and serotonergic effects. In addition, the cytotoxicity of falcarinol type Polyacetylenes towards human cancer cells, bioavailability, and their potential anticancer effect in vivo indicates that these compounds may contribute to the health effects of certain vegetables and hence could be important nutraceuticals. The bioactivity of falcarinol type Polyacetylenes occurring in food plants of the Apiaceae family, their possible mode of action and possible health promoting effects are discussed in this review as well as the effect of storage, processing and other factors that can influence the content of these compounds in particular root vegetables and products. Moreover, recent patents on bioactivity of falcarinol type Polyacetylenes and inventions making use of this knowledge are presented and discussed.
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differential effects of falcarinol and related aliphatic c17 Polyacetylenes on intestinal cell proliferation
2009Co-Authors: Stig Purup, Eric Larsen, Lars Porskjaer ChristensenAbstract:Quantitative major Polyacetylenes of carrots (falcarinol and falcarindiol) and American ginseng roots (falcarinol and panaxydol) were isolated and tested in human intestinal epithelial cells of normal (FHs 74 Int.) and cancer (Caco-2) origin. A hormesis effect was seen for all isolated Polyacetylenes when added to Caco-2 cells in concentrations ranging from 1 ng/mL to 20 μg/mL. The relative inhibitory potency was falcarinol > panaxydol > falcarindiol. No hormesis effect was observed when adding the Polyacetylenes to FHs 74 Int. cells. Instead, an inhibitory growth response was observed above 1 μg/mL. The relative inhibitory potency was panaxydol > falcarinol > falcarindiol. Maximal inhibition at 20 μg/mL corresponded to approximately 95% and 80% inhibition of cell proliferation in normal and cancer cells, respectively. Combinations of falcarinol and falcarindiol added to normal and cancer cells showed a synergistic response for the inhibition of cell growth. Furthermore, the oxidized form of falcarinol, falcarinon, showed a significantly less growth inhibitory effect in intestinal cells of both normal and cancer origin; hence, a hydroxyl group at C-3 may be important for activity of falcarinol-type Polyacetylenes. Extracts of carrots, containing different amounts of falcarinol, falcarindiol, and falcarindiol 3-acetate had significant inhibitory effects on both normal and cancer cell proliferation. In cancer cells, the extract containing the highest concentration of falcarinol tended to have the highest growth inhibitory effect, in accordance with a higher potency of falcarinol than falcarindiol. The present study demonstrates that aliphatic C17-Polyacetylenes are potential anticancer principles of carrots and related vegetables and that synergistic interaction between bioactive Polyacetylenes may be important for their bioactivity.
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simultaneous determination of ginsenosides and Polyacetylenes in american ginseng root panax quinquefolium l by high performance liquid chromatography
2006Co-Authors: Lars Porskjaer Christensen, Martin Jensen, Ulla KidmoseAbstract:A method for simultaneous determination of ginsenosides and Polyacetylenes in Panax quinquefolium L. (American ginseng) roots was developed. The ginsenosides Rb1, Rb2, Rc, Rd, Re, Rg1, Ro, malonyl-Rb1, malonyl-Rc, and malonyl-Rd and the Polyacetylenes falcarinol and panaxydol were extracted from fresh ginseng roots in a sequential extraction process with 100% methanol followed by 80% aqueous methanol and quantified simultaneously in extracts by high-performance liquid chromatography using diode array detection. Separations were achieved with a phosphate buffer−acetonitrile gradient system using an RP-C18 column. Except for Rd, the present extraction method resulted in similar or significantly higher concentrations of both ginsenosides and Polyacetylenes in comparison to commonly used extraction methods for these compounds. The contents of Polyacetylenes and ginsenosides were determined in the root hairs, lateral roots, and main roots of 6 year old ginseng plants. The total mean concentrations of ginsenosi...
Jess D Reed - One of the best experts on this subject based on the ideXlab platform.
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purple carrot daucus carota l Polyacetylenes decrease lipopolysaccharide induced expression of inflammatory proteins in macrophage and endothelial cells
2008Co-Authors: Brandon T Metzger, David M. Barnes, Jess D ReedAbstract:Carrots (Daucus carota L.) contain phytochemicals including carotenoids, phenolics, Polyacetylenes, isocoumarins, and sesquiterpenes. Purple carrots also contain anthocyanins. The anti-inflammatory activity of extracts and phytochemicals from purple carrots was investigated by determining attenuation of the response to lipopolysaccharide (LPS). A bioactive chromatographic fraction (Sephadex LH-20) reduced LPS inflammatory response. There was a dose-dependent reduction in nitric oxide production and mRNA of pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) and iNOS in macrophage cells. Protein secretions of IL-6 and TNF-α were reduced 77 and 66% in porcine aortic endothelial cells treated with 6.6 and 13.3 µg/mL of the LH-20 fraction, respectively. Preparative liquid chromatography resulted in a bioactive subfraction enriched in the polyacetylene compounds falcarindiol, falcarindiol 3-acetate, and falcarinol. The Polyacetylenes were isolated and reduced nitric oxide production in macrophage cells by as much ...
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Purple carrot (Daucus carota L.) Polyacetylenes decrease lipopolysaccharide-induced expression of inflammatory proteins in macrophage and endothelial cells.
2008Co-Authors: Brandon T Metzger, David M. Barnes, Jess D ReedAbstract:Carrots ( Daucus carota L.) contain phytochemicals including carotenoids, phenolics, Polyacetylenes, isocoumarins, and sesquiterpenes. Purple carrots also contain anthocyanins. The anti-inflammatory activity of extracts and phytochemicals from purple carrots was investigated by determining attenuation of the response to lipopolysaccharide (LPS). A bioactive chromatographic fraction (Sephadex LH-20) reduced LPS inflammatory response. There was a dose-dependent reduction in nitric oxide production and mRNA of pro-inflammatory cytokines (IL-6, IL-1beta, TNF-alpha) and iNOS in macrophage cells. Protein secretions of IL-6 and TNF-alpha were reduced 77 and 66% in porcine aortic endothelial cells treated with 6.6 and 13.3 microg/mL of the LH-20 fraction, respectively. Preparative liquid chromatography resulted in a bioactive subfraction enriched in the polyacetylene compounds falcarindiol, falcarindiol 3-acetate, and falcarinol. The Polyacetylenes were isolated and reduced nitric oxide production in macrophage cells by as much as 65% without cytotoxicity. These results suggest that Polyacetylenes, not anthocyanins, in purple carrots are responsible for anti-inflammatory bioactivity.
Mutsumasa Kyotani - One of the best experts on this subject based on the ideXlab platform.
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synthesis of helical polyacetylene in chiral nematic liquid crystals using crown ether type binaphthyl derivatives as chiral dopants
2005Co-Authors: Kazuo Akagi, Taizou Mori, G Piao, Mutsumasa KyotaniAbstract:A series of crown ether type binaphthyl derivatives (CEBDs) were synthesized and used as chiral dopants to induce chiral nematic (N*) liquid crystals (LCs). The twisting powers of the CEBDs for phenylcyclohexane (PCH)-derived nematic LCs were evaluated. It was found that the twisting powers of the CEBDs increased with decreasing ring size of the crown ether. Helical Polyacetylenes were synthesized in the N*-LCs induced by the CEBDs. The relationship between the morphology of the helical polyacetylene and the helical structure of the N*-LC was investigated. The result showed that the interdistance between the fibril bundles of the helical polyacetylene was equal to a half-helical pitch of the N*-LC and the screw direction of the polyacetylene fibrils was opposite to that of the N*-LC.
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synthesis of helical polyacetylene in chiral nematic liquid crystals using crown ether type binaphthyl derivatives as chiral dopants
2005Co-Authors: Kazuo Akagi, Taizou Mori, G Piao, Mutsumasa KyotaniAbstract:A series of crown ether type binaphthyl derivatives (CEBDs) were synthesized and used as chiral dopants to induce chiral nematic (N*) liquid crystals (LCs). The twisting powers of the CEBDs for phenylcyclohexane (PCH)-derived nematic LCs were evaluated. It was found that the twisting powers of the CEBDs increased with decreasing ring size of the crown ether. Helical Polyacetylenes were synthesized in the N*-LCs induced by the CEBDs. The relationship between the morphology of the helical polyacetylene and the helical structure of the N*-LC was investigated. The result showed that the interdistance between the fibril bundles of the helical polyacetylene was equal to a half-helical pitch of the N*-LC and the screw direction of the polyacetylene fibrils was opposite to that of the N*-LC.
Brandon T Metzger - One of the best experts on this subject based on the ideXlab platform.
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purple carrot daucus carota l Polyacetylenes decrease lipopolysaccharide induced expression of inflammatory proteins in macrophage and endothelial cells
2008Co-Authors: Brandon T Metzger, David M. Barnes, Jess D ReedAbstract:Carrots (Daucus carota L.) contain phytochemicals including carotenoids, phenolics, Polyacetylenes, isocoumarins, and sesquiterpenes. Purple carrots also contain anthocyanins. The anti-inflammatory activity of extracts and phytochemicals from purple carrots was investigated by determining attenuation of the response to lipopolysaccharide (LPS). A bioactive chromatographic fraction (Sephadex LH-20) reduced LPS inflammatory response. There was a dose-dependent reduction in nitric oxide production and mRNA of pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) and iNOS in macrophage cells. Protein secretions of IL-6 and TNF-α were reduced 77 and 66% in porcine aortic endothelial cells treated with 6.6 and 13.3 µg/mL of the LH-20 fraction, respectively. Preparative liquid chromatography resulted in a bioactive subfraction enriched in the polyacetylene compounds falcarindiol, falcarindiol 3-acetate, and falcarinol. The Polyacetylenes were isolated and reduced nitric oxide production in macrophage cells by as much ...
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Purple carrot (Daucus carota L.) Polyacetylenes decrease lipopolysaccharide-induced expression of inflammatory proteins in macrophage and endothelial cells.
2008Co-Authors: Brandon T Metzger, David M. Barnes, Jess D ReedAbstract:Carrots ( Daucus carota L.) contain phytochemicals including carotenoids, phenolics, Polyacetylenes, isocoumarins, and sesquiterpenes. Purple carrots also contain anthocyanins. The anti-inflammatory activity of extracts and phytochemicals from purple carrots was investigated by determining attenuation of the response to lipopolysaccharide (LPS). A bioactive chromatographic fraction (Sephadex LH-20) reduced LPS inflammatory response. There was a dose-dependent reduction in nitric oxide production and mRNA of pro-inflammatory cytokines (IL-6, IL-1beta, TNF-alpha) and iNOS in macrophage cells. Protein secretions of IL-6 and TNF-alpha were reduced 77 and 66% in porcine aortic endothelial cells treated with 6.6 and 13.3 microg/mL of the LH-20 fraction, respectively. Preparative liquid chromatography resulted in a bioactive subfraction enriched in the polyacetylene compounds falcarindiol, falcarindiol 3-acetate, and falcarinol. The Polyacetylenes were isolated and reduced nitric oxide production in macrophage cells by as much as 65% without cytotoxicity. These results suggest that Polyacetylenes, not anthocyanins, in purple carrots are responsible for anti-inflammatory bioactivity.
Garth Loren Warnock - One of the best experts on this subject based on the ideXlab platform.
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devil s club falcarinol type Polyacetylenes inhibit pancreatic cancer cell proliferation
2019Co-Authors: Susan S C Cheung, Djamel Khelifi, Richard W Smith, David Hasman, Garth Loren WarnockAbstract:AbstractNatural falcarinol-type (FC-type) Polyacetylenes are known to show anticancer activities. We studied the bioactivity of synthetic FC, 1,2-dihydrofalcarinol (FCH) and 3-acetoxyfalcarinol (FCA) and compared them with the natural bioactive polyacetylene [9,17-octadecadiene-12,14-diyne-1,11,16-triol,1-acetate] (DCA) isolated from Devil’s club (DC) Oplopanax horridus. Antiproliferation activity of these Polyacetylenes, along with DC inner stem bark 70% ethanol and water extracts, was tested on human pancreatic ductal adenocarcinoma cell lines PANC-1 and BxPC-3. Chemically synthesized FC and FCA showed consistent IC50 (50% inhibition concentration) and higher potency than DCA. FC and DCA’s mechanism of action investigated by antibody array on apoptosis-associated genes, and cellular features confirmed by microscopy demonstrated that both compounds modulated genes related to pro-apoptosis, antiapoptosis, apoptosis, cell cycle, stress related, and death receptors. FC-type Polyacetylenes with a terminal do...
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devil s club falcarinol type Polyacetylenes inhibit pancreatic cancer cell proliferation
2019Co-Authors: Susan S C Cheung, Djamel Khelifi, Richard W Smith, David Hasman, Joseph Tai, Garth Loren WarnockAbstract:Natural falcarinol-type (FC-type) Polyacetylenes are known to show anticancer activities. We studied the bioactivity of synthetic FC, 1,2-dihydrofalcarinol (FCH) and 3-acetoxyfalcarinol (FCA) and compared them with the natural bioactive polyacetylene [9,17-octadecadiene-12,14-diyne-1,11,16-triol,1-acetate] (DCA) isolated from Devil's club (DC) Oplopanax horridus. Antiproliferation activity of these Polyacetylenes, along with DC inner stem bark 70% ethanol and water extracts, was tested on human pancreatic ductal adenocarcinoma cell lines PANC-1 and BxPC-3. Chemically synthesized FC and FCA showed consistent IC50 (50% inhibition concentration) and higher potency than DCA. FC and DCA's mechanism of action investigated by antibody array on apoptosis-associated genes, and cellular features confirmed by microscopy demonstrated that both compounds modulated genes related to pro-apoptosis, antiapoptosis, apoptosis, cell cycle, stress related, and death receptors. FC-type Polyacetylenes with a terminal double bond (FC, FCA, and DCA) are potent inhibitors of pancreatic cancer cell proliferation compared to FCH with a terminal single bond. Liquid chromatography mass spectrometry confirmed the presence of FC and FCH in the inner stem bark of DC. For potential applications of FC-type Polyacetylenes as anticancer agents, preparing them by chemical synthesis may provide an advantage over the labor intensive extraction process from raw plant material.
