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Ken Yasukawa - One of the best experts on this subject based on the ideXlab platform.
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Inhibitory effect of the flowers of artichoke cynara cardunculus on tpa induced inflammation and tumor promotion in two stage carcinogenesis in mouse skin
Journal of Natural Medicines, 2010Co-Authors: Ken Yasukawa, Hideki Matsubara, Yuri SanoAbstract:The methanol extract of the flowers of artichoke (Cynara cardunculus) exhibited remarkable antitumor activity in an in vivo two-stage carcinogenesis test in mice, using 7,12-dimethylbenz[a]anthracene as an initiator and 12-O-tetradecanoylphorbol-13-acetate (TPA) as a promoter. From the active fraction of the methanol extract, four triterpene alcohols and their corresponding acetates were isolated and identified. These compounds were evaluated for their Inhibitory effects on TPA-induced inflammation (1 μg/ear) in mice and showed marked anti-inflammatory effects, with a 50% Inhibitory Dose of 0.50–0.91 μmol/ear.
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anti tumor promoters phenolics and triterpenoid from hippophae rhamnoides
Fitoterapia, 2009Co-Authors: Ken Yasukawa, Susumu Kitanaka, Kenji Kawata, Kumiko GotoAbstract:Abstract A 70% ethanol extract of the branches of Hippophae rhamnoides exhibited remarkable antitumor activity in an in vivo two-stage carcinogenesis test in mice using 7,12-dimethylbenz[ a ]anthracene as an initiator and 12- O -tetradecanoylphorbol-13-acetate (TPA) as a promoter. From the active fraction of the 70% ethanol extract, three phenolic compounds, (+)-catechin (1), (+)-gallocatechin (2), and (−)-epigallocatechin (3) and a tritepenoid, ursolic acid (4) were isolated and identified. These compounds were evaluated for their Inhibitory effects on TPA-induced inflammation (1 µg/ear) in mice. Within the tested compounds, 3 and 4 showed marked anti-inflammatory effects, with a 50% Inhibitory Dose of 1.7 and 0.2 μmol/ear.
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Inhibitory effect of the rhizomes of Alpinia officinarum on TPA-induced inflammation and tumor promotion in two-stage carcinogenesis in mouse skin
Journal of Natural Medicines, 2008Co-Authors: Ken Yasukawa, Yi Sun, Susumu Kitanaka, Motofumi Miura, Naoyuki Tomizawa, Shigeyasu MotohashiAbstract:The methanol extract of galangal (the rhizomes of Alpinia officinarum L.) exhibited remarkable antitumor-promoting activity on an in vivo two-stage carcinogenesis test of mice using 7,12-dimethylbenz[ a ]anthracene as an initiator and 12- O -tetradecanoylphorbol-13-acetate (TPA) as a promoter. Seven diarylheptanoids ( 1 – 7 ) were isolated and identified from the active fraction of the methanol extracts of the galangal. These compounds, 1 – 7 , were evaluated for their Inhibitory effects on TPA-induced inflammation (1 μg/ear) in mice. These compounds ( 1–7 ) tested showed marked anti-inflammatory effects, with a 50% Inhibitory Dose of 0.8–2.7 μmol/ear.
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acerogenin m a cyclic diarylheptanoid and other phenolic compounds from acer nikoense and their anti inflammatory and anti tumor promoting effects
Chemical & Pharmaceutical Bulletin, 2006Co-Authors: Toshihiro Akihisa, Ken Yasukawa, Yosuke Taguchi, Hiroyuki Akazawa, Takashi Suzuki, Yumiko KimuraAbstract:A new cyclic diarylheptanoid, acerogenin M (1), has been isolated along with nine known diarylheptanoids, 2—10, and two known phenolic compounds, 11 and 12, from a MeOH extract of the stem bark of Acer nikoense MAXIM. (Aceraceae). The structure of 1 was determined on the basis of a spectroscopic method. Upon evaluation of the Inhibitory effects on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 μg/ear) in mice of nine of the compounds (2—6, 8, 10—12), six (2, 4—6, 8, 10) showed a marked anti-inflammatory effect with a 50% Inhibitory Dose (ID50) of 0.26—0.81 mg per ear. In addition, upon an evaluation against the Epstein–Barr virus early antigen (EBV-EA) activation induced by TPA for all of the compounds, all exhibited moderate Inhibitory effects against EBV-EA induction (IC50 values of 356—534 mol ratio/32 pmol TPA).
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Anti-inflammatory activities of the triterpene acids from the resin of Boswellia carteri
Journal of ethnopharmacology, 2006Co-Authors: Norihiro Banno, Yumiko Kimura, Toshihiro Akihisa, Ken Yasukawa, Harukuni Tokuda, Keiichi Tabata, Yuji Nakamura, Reiko Nishimura, Takashi SuzukiAbstract:Boswellic acids are the main well-known active components of the resin of Boswellia carteri (Burseraceae) and these are still dealing with the ethnomedicinal use for the treatment of rheumatoid arthritis and other inflammatory diseases. Although several studies have already been reported on the pharmacological properties, especially on the anti-inflammatory activity, of Boswellia carteri resin and boswellic acids, the ethnomedicinal importance of Boswellia carteri and its components, boswellic acids, prompted us to undertake detailed investigation on the constituents of the resin and their anti-inflammatory activity. Fifteen triterpene acids, viz., seven of the beta-boswellic acids (ursane-type) (1-7), two of the alpha-boswellic acids (oleanane-type) (8, 9), two of the lupeolic acids (lupane-type) (10, 11), and four of the tirucallane-type (12-14, 16), along with two cembrane-type diterpenes (17, 18), were isolated and identified from the methanol extract of the resin of Boswellia carteri. Upon evaluation of 17 compounds, 1-14 and 16-18, and compound 15, semi-synthesized from 14 by acetylation, for their Inhibitory activity against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 microg/ear) in mice, all of the compounds, except for 18, exhibited marked anti-inflammatory activity with a 50% Inhibitory Dose (ID(50)) of 0.05-0.49 mg/ear.
Toshihiro Akihisa - One of the best experts on this subject based on the ideXlab platform.
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acerogenin m a cyclic diarylheptanoid and other phenolic compounds from acer nikoense and their anti inflammatory and anti tumor promoting effects
Chemical & Pharmaceutical Bulletin, 2006Co-Authors: Toshihiro Akihisa, Ken Yasukawa, Yosuke Taguchi, Hiroyuki Akazawa, Takashi Suzuki, Yumiko KimuraAbstract:A new cyclic diarylheptanoid, acerogenin M (1), has been isolated along with nine known diarylheptanoids, 2—10, and two known phenolic compounds, 11 and 12, from a MeOH extract of the stem bark of Acer nikoense MAXIM. (Aceraceae). The structure of 1 was determined on the basis of a spectroscopic method. Upon evaluation of the Inhibitory effects on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 μg/ear) in mice of nine of the compounds (2—6, 8, 10—12), six (2, 4—6, 8, 10) showed a marked anti-inflammatory effect with a 50% Inhibitory Dose (ID50) of 0.26—0.81 mg per ear. In addition, upon an evaluation against the Epstein–Barr virus early antigen (EBV-EA) activation induced by TPA for all of the compounds, all exhibited moderate Inhibitory effects against EBV-EA induction (IC50 values of 356—534 mol ratio/32 pmol TPA).
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Anti-inflammatory activities of the triterpene acids from the resin of Boswellia carteri
Journal of ethnopharmacology, 2006Co-Authors: Norihiro Banno, Yumiko Kimura, Toshihiro Akihisa, Ken Yasukawa, Harukuni Tokuda, Keiichi Tabata, Yuji Nakamura, Reiko Nishimura, Takashi SuzukiAbstract:Boswellic acids are the main well-known active components of the resin of Boswellia carteri (Burseraceae) and these are still dealing with the ethnomedicinal use for the treatment of rheumatoid arthritis and other inflammatory diseases. Although several studies have already been reported on the pharmacological properties, especially on the anti-inflammatory activity, of Boswellia carteri resin and boswellic acids, the ethnomedicinal importance of Boswellia carteri and its components, boswellic acids, prompted us to undertake detailed investigation on the constituents of the resin and their anti-inflammatory activity. Fifteen triterpene acids, viz., seven of the beta-boswellic acids (ursane-type) (1-7), two of the alpha-boswellic acids (oleanane-type) (8, 9), two of the lupeolic acids (lupane-type) (10, 11), and four of the tirucallane-type (12-14, 16), along with two cembrane-type diterpenes (17, 18), were isolated and identified from the methanol extract of the resin of Boswellia carteri. Upon evaluation of 17 compounds, 1-14 and 16-18, and compound 15, semi-synthesized from 14 by acetylation, for their Inhibitory activity against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 microg/ear) in mice, all of the compounds, except for 18, exhibited marked anti-inflammatory activity with a 50% Inhibitory Dose (ID(50)) of 0.05-0.49 mg/ear.
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anti inflammatory and antitumor promoting effects of the triterpene acids from the leaves of eriobotrya japonica
Biological & Pharmaceutical Bulletin, 2005Co-Authors: Norihiro Banno, Yumiko Kimura, Motohiko Ukiya, Toshihiro Akihisa, Ken Yasukawa, Yosuke Taguchi, Hiroyuki Akazawa, Takashi SuzukiAbstract:Sixteen triterpene acids, viz., five of the oleanane-type (1-5), nine of the ursane-type (6-14), and two of the lupane-type (15, 16), were isolated and identified from the ethyl acetate-soluble fraction of the methanol extract of the leaves of loquat, Eriobotrya japonica LINDL. (Rosaceae). Twelve of these compounds, 1-4, 6, 8-13, and 15, were evaluated for their Inhibitory effects on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 microg/ear) in mice. All the compounds tested showed a marked anti-inflammatory effect, with a 50% Inhibitory Dose (ID50) of 0.03-0.43 mg per ear. In addition, an evaluation against the Epstein-Barr virus early antigen (EBV-EA) activation induced by TPA for all of the compounds, 12 and 13 showed potent Inhibitory effects on EBV-EA induction. Furthermore, euscaphic acid (12) exhibited marked antitumor-promoting activity in an in vivo two-stage carcinogenesis test of mouse tumor by using 7,12-dimethylbenz[a]anthracene (DMBA) as an initiator and TPA as a promoter.
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triterpene acids from the leaves of perilla frutescens and their anti inflammatory and antitumor promoting effects
Bioscience Biotechnology and Biochemistry, 2004Co-Authors: Norihiro Banno, Yumiko Kimura, Motohiko Ukiya, Toshihiro Akihisa, Ken Yasukawa, Harukuni Tokuda, Hiroshi Higashihara, Kenji Watanabe, Junichi Hasegawa, Hoyoku NishinoAbstract:Nine triterpene acids, viz., six of the ursane type, ursolic acid (1), corosolic acid (2), 3-epicorosolic acid (3), pomolic acid (4), tormentic acid (5) and hyptadienic acid (6), and three of the oleanane type, oleanolic acid (7), augustic acid (8) and 3-epimaslinic acid (9), among which 1 constituted the most predominant triterpene acid, were isolated and identified from ethanol extracts of the leaves of red perilla [Perilla frutescens (L.) Britton var. acuta Kudo] and green perilla [P. frutescens (L.) Britton var. acuta Kudo forma viridis Makino]. These eight compounds, 1, 2, 4–9, were evaluated for their Inhibitory effects on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 μg/ear) in mice. All the compounds tested showed a marked anti-inflammatory effect, with a 50% Inhibitory Dose (ID50) of 0.09–0.3 mg per ear. In addition, an evaluation against the Epstein-Barr virus early antigen (EBV-EA) activation induced by TPA showed five compounds, 1–3, 5 and 9, with a potent Inhibitory effec...
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constituents of compositae plants 2 triterpene diols triols and their 3 o fatty acid esters from edible chrysanthemum flower extract and their anti inflammatory effects
Journal of Agricultural and Food Chemistry, 2001Co-Authors: Motohiko Ukiya, Yumiko Kimura, Tamotsu Nikaido, Kazuo Koike, Toshihiro Akihisa, Ken Yasukawa, Yoshimasa Kasahara, Michio TakidoAbstract:The n-hexane soluble and the nonsaponifiable lipid fractions of the edible flower extract of chrysanthemum (Chrysanthemum morifolium) were investigated for triterpene diol and triol constituents. These triterpenes occur as the 3-O-fatty acid esters in the n-hexane soluble fraction from which 26 new and 6 known fatty acid esters were isolated and characterized. From the nonsaponifiable lipid fraction, 24 triterpene diols and triols were isolated, of which 3 were new compounds: (24S)-25-methoxycycloartane-3beta,24-diol (11), (24S)-25-methoxycycloartane-3beta,24,28-triol (22), and 22alpha-methoxyfaradiol (23). Faradiol (9) and heliantriol C (19), present in the nonsaponifiable lipid fraction and as the 3-O-palmitoyl esters in the n-hexane soluble fraction, were the most predominant triterpene diol and triol constituents. Fourteen triterpene diols and triols and 9 fatty acid esters were evaluated with respect to their anti-inflammatory activity against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in mice. All of the triterpenes examined showed marked Inhibitory activity, with a 50% Inhibitory Dose (ID50) of 0.03-1.0 mg/ear, which was more inhibitive than quercetin (ID50 = 1.6 mg/ear), a known inhibitor of TPA-induced inflammation in mice.
Juliet Carmichael - One of the best experts on this subject based on the ideXlab platform.
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phase ii trial of the oral parp inhibitor olaparib in brca deficient advanced breast cancer
Journal of Clinical Oncology, 2009Co-Authors: Andrew Tutt, Jeffrey N Weitzel, M E Robson, Judy E Garber, M W Audeh, M Friedlander, Juliet CarmichaelAbstract:CRA501 Background: Olaparib (AZD2281; KU-0059436) is a novel, orally active PARP inhibitor that induces synthetic lethality in homozygous BRCA-deficient cells. A phase I trial identified 400 mg bd as the maximum tolerated Dose (MTD) with an initial signal of efficacy in BRCA-deficient ovarian cancers (ASCO 2008; abst 5510). The primary aim of this study was to test the efficacy of olaparib in confirmed BRCA1/BRCA2 carriers with advanced refractory breast cancer. The secondary aim was to assess safety and tolerability in this population. Methods: In an international, multicenter, proof-of-concept, single-arm, phase II study, two sequential patient (pt) cohorts received continuous oral olaparib in 28-day cycles initially at the MTD, 400 mg bd (27 pts), and subsequently at 100 mg bd, a previously identified PARP Inhibitory Dose (27 pts). Eligibility criteria included confirmed BRCA1/BRCA2 mutation and recurrent, measurable chemotherapy-refractory breast cancer. The primary efficacy endpoint was best objectiv...
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phase ii trial of the oral parp inhibitor olaparib azd2281 in brca deficient advanced ovarian cancer
Journal of Clinical Oncology, 2009Co-Authors: M W Audeh, Clare L. Scott, M Friedlander, Richard T Penson, B Powell, Katherine M Bellmcguinn, Juliet CarmichaelAbstract:5500 Background: Olaparib (AZD2281; KU-0059436) is a novel, orally active PARP inhibitor that induces synthetic lethality in homozygous BRCA-deficient cells. A phase I trial identified 400 mg bd as the maximum tolerated Dose (MTD) with an initial signal of efficacy in BRCA-deficient cancers (ASCO 2008; abst 5510). The primary aim of this study was to test the efficacy of olaparib in confirmed BRCA1/BRCA2 carriers with advanced chemotherapy-refractory ovarian cancer. The secondary aim was to assess the safety and tolerability profile in ovarian cancer patients with BRCA1/2 deficiency. Methods: In an international, multicenter, proof-of-concept, single-arm, phase II study, two patient (pt) sequential cohorts received continuous oral olaparib in 28-day cycles, initially at the MTD, 400 mg bd (33 pts), and subsequently at 100 mg bd (24 pts), a previously shown clinically active and PARP Inhibitory Dose. Eligibility criteria included confirmed genetic BRCA1/2 mutation and recurrent, measurable, incurable disea...
J P Ganley - One of the best experts on this subject based on the ideXlab platform.
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inhibition of the enteroviruses that cause acute hemorrhagic conjunctivitis ahc by benzimidazoles enviroxime ly 122772 and enviradone ly 127123
Antiviral Research, 1995Co-Authors: Marlyn P Langford, W A Ball, J P GanleyAbstract:Enviradone (EvirD, (E)-1-[(1-methylethyl) sulfonyl]-6-(1-phenyl-1-propenyl)-1 H- benzimidazole-2-amine) and Enviroxime (EvirX, 2-amino-1-(isopropyl-sulfonyl)-6-benzimidazole phenyl ketone oxime) inhibited enterovirus 70 (EV70) and coxsackievirus A24 variant (CA24v) infection of conjunctival and laryngeal cells. On average, the continuous presence of 1-3 micrograms of EvirD or EvirX/ml in cell cultures acutely infected with EV70 or CA24v inhibited virus production (> 2 log10 reduction) and 100% of the viral cytopathogenic effect (CPE). The 50% CPE Inhibitory Dose (ID50) for EvirD and EvirX against 11 EV70 and 15 CA24v isolates ranged from 0.01 to 0.3 microgram and 0.01-0.65 microgram/ml, respectively. The mean ID50 for EvirD and EvirX against the 26 AHC viruses was 0.17 +/- 0.12 microgram and 0.13 +/- 0.14 microgram/ml, respectively. Pretreatment for 15 min with 3 micrograms EvirX/ml or for 1-2 h with 3 micrograms EvirD/ml protected conjunctival cells against viral CPE. The cells were resistant to infection for 1-2 h at 33 and 37 degrees C after removal of EvirD and EvirX. The addition of 10 micrograms EvirD/ml up to 6 h or 10 micrograms EvirX/ml 1-2 h after low multiplicity infection inhibited viral CPE. Ten-fold less EvirD inhibited EV70 when added to glioma cells 2 h before infection than when added 2 h after infection. Our results indicate that EvirX and EvirD inhibit AHC viruses in vitro at concentrations that are not cytotoxic and suggest that EvirX or EvirD may be prove useful against AHC.
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inhibition of the enteroviruses that cause acute hemorrhagic conjunctivitis ahc by benzimidazoles enviroxime ly 122772 and enviradone ly 127123
Antiviral Research, 1995Co-Authors: Marlyn P Langford, W A Ball, J P GanleyAbstract:Abstract Enviradone (EvirD, (E)-1-[(1-methylethyl) sulfonyl]-6-(1-phenyl-1-propenyl)-1H-benzimidazole-2-amine) and Enviroxime (EvirX, 2-amino-1-(isopropyl-sulfonyl)-6-benzimidazole phenyl ketone oxime) inhibited enterovirus 70 (EV70) and coxsackievirus A24 variant (CA24v) infection of conjunctival and laryngeal cells. On average, the continuous presence of 1–3 μg of EvirD or EvirX/ml in cell cultures acutely infected with EV70 or CA24v inhibited virus production (> 2 log10 reduction) and 100% of the viral cytopathogenic effect (CPE). The 50% CPE Inhibitory Dose (ID50) for EvirD and EvirX against 11 EV70 and 15 CA24v isolates ranged from 0.01 to 0.3 μg and 0.01–0.65 μg/ml, respectively. The mean ID50 for EvirD and EvirX against the 26 AHC viruses was 0.17 ± 0.12 μg and 0.13 ± 0.14 μg/ml, respectively. Pretreatment for 15 min with 3 μg EvirX/ml or for 1–2 h with 3 μg EvirD/ml protected conjunctival cells against viral CPE. The cells were resistant to infection for 1–2 h at 33 and 37°C after removal of EvirD and EvirX. The addition of 10 μg EvirD/ml up to 6 h or 10 μg EvirX/ml 1–2 h after low multiplicity infection inhibited viral CPE. Ten-fold less EvirD inhibited EV70 when added to glioma cells 2 h before infection than when added 2 h after infection. Our results indicate that EvirX and EvirD inhibit AHC viruses in vitro at concentrations that are not cytotoxic and suggest that EvirX or EvirD may be prove useful against AHC.
Toshitake Tamura - One of the best experts on this subject based on the ideXlab platform.
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Triterpene alcohols from the flowers of Compositae and their anti-inflammatory effects
Phytochemistry, 1996Co-Authors: Toshihiro Akihisa, Ken Yasukawa, Sakae Yamanouchi, Michio Takido, Hirotoshi Oinuma, Yoshimasa Kasahara, Kunio Kumaki, Toshitake TamuraAbstract:Eleven tabular and nine ligulate flowers from 15 species of Compositae plants were investigated for their triterpene alcohol constituents. This led to the isolation and identification of 11 triterpene alcohols as follows: heliaol, taraxasterol, psi-taraxasterol, alpha-amyrin, beta-amyrin, lupeol, taraxerol, cycloartenol, 24-methyl-enecycloartanol, tirucalla-7,24-dienol and dammaradienol. The tabular flowers of Calendula officinalis, Carthamus tinctorius, Cosmos bipinnatus, Chrysanthemum morifolium, Helianthus annuus and Matricaria matricarioides showed a characteristic feature by containing helianol as the most predominant component (29-86%) in the triterpene alcohol fractions. The triterpene alcohols from Compositae flowers were evaluated with respect to their anti-inflammatory activity against 12-O-tetradecanoylphorbol-13-acetate-induced inflammation (1 microgram per ear) in mice. All of these showed marked Inhibitory activity, and their 50% Inhibitory Dose was 0.1-0.8 mg per ear.
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some lupane type triterpenes inhibit tumor promotion by 12 o tetradecanoylphorbol 13 acetate in two stage carcinogenesis in mouse skin
Phytomedicine, 1995Co-Authors: Ken Yasukawa, Toshihiro Akihisa, Sakae Yamanouchi, Michio Takido, Toshitake TamuraAbstract:Summary We have found that several lupane-type triterpenes, including lupeol, its acetate, betulin and betulinic acid, inhibit 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation, and that betulinic acid inhibits tumor promotion in two-stage carcinogenesis in mice. Among seven lupane-type triterpenes assayed, these compounds inhibited the inflammatory activity induced by TPA in mice. The 50 % Inhibitory Dose of these compounds for TPA-induced inflammation was 0.4–4.0 μmol. Furthermore, topical application of lupeol, lupeol 3-acetate and betulin markedly suppressed the tumor-promoting effect of TPA (1 μg/mouse) in mouse skin initiated with 7,12-dimethyl-benz[a]anthracene (50 μg/mouse), at a grade corresponding to that of betulinic acid.