著者

金城 順英 土橋 良太

出版者

公益財団法人 日本ビフィズス菌センター

雑誌

腸内細菌学雑誌 (ISSN:13430882)

巻号頁・発行日

vol.26, no.4, pp.223-233, 2012 (Released:2012-12-28)

参考文献数

34

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大豆はイソフラボンとサポニンなどのフィトケミカルを豊富に含むことでも有名であり,そのうちイソフラボンはエストロゲン様作用を示すことが知られている.また食用豆類の伝承的薬効としてサポニンによる利尿作用なども知られている.一方,葛花はマメ科クズの花部を用いる生薬で肝保護作用を示すが,その活性本体はイソフラボンとサポニンであり,構造的に大豆成分と酷似している.構造上の微妙な相違点が,どのように生物活性に影響を与えるのか,腸内細菌叢による代謝反応が活性化に必要ではないかと推論し,ヒト由来の腸内細菌を用い実験を企図した.その結果,以下の知見が得られた.【1】肝保護作用において,a)サポニンではよりシンプルな構造が寄与し(C-24 methyl基),葛花サポニンの方が大豆サポニンより若干強い作用を示す.b)イソフラボンでは葛花イソフラボンのみ肝保護作用を示す.【2】女性ホルモン様作用は,大豆イソフラボンのよりシンプルな構造が顕著に寄与し,大豆イソフラボンのみに認められ,葛花イソフラボンには全く認められない.【3】腎保護(抗補体)作用において,大豆サポニンの腸内細菌および肝臓で代謝されたsoyasapogenol B monoglucuronideが葛花サポニンの代謝物に比べ強い活性を示す.【4】これらの活性発現において,腸内細菌による影響(代謝活性化)が非常に大きい.

著者

新甫 勇次郎 山崎 律 中島 嘉次郎 伊東 宏 竹下 尚 金城 順英 野原 稔弘

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.110, no.8, pp.604-611, 1990-08-25

被引用文献数

14

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The present study was designed to examine the effects of methanolic extract (PE-ME), isoflavonoid fraction (PF-IF), triterpenoid saponin fraction (PF-SP) and N-acyl-N_1-glucosyl-tryptophan (PF-P) isolated from puerariae flos on alcohol-induced unusual metabolism (as for glucose (BG), triglyceride (TG), and urea nitrogen (BUN) level in blood) and experimental liver injury (model : CCl_4-and high fatty food induced) in mice. These alcohol-induced increasing responses were inhibited by the extracted and refined substances from puerariae flos. In short, PF-ME (4500 mg/kg) and PF-P (400 mg/kg) inhibited an increase in BG level induced by alcohol, whereas PF-IF (1000 mg/kg) and PF-SP (1000 mg/kg) did not. Similary, PF-ME and PF-SP inhibited an increase in TG induced by alcohol, whereas PF-IF did not. In addition, PF-IF and PF-SP inhibited increasing BUN level. Still more, PF-IF and PF-SP significantly inhibited an increase in gulutamate oxalacetate transaminase or gulutamate pyruvate transaminase level induced by high-fatty food and CCl_4 in control animals. Especially PF-IF (250 mg/kg) administration showed a remarkable effect (inhibition : 76.3%) in control animals. These results suggested that puerariae flos or its combination drugs may be a useful drug as a traditional medicinal system for counteraction to drinking.

著者

新甫 勇次郎 山崎 律 中島 嘉次郎 伊東 宏 竹下 尚 金城 順英 野原 稔弘

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.109, no.6, pp.424-431, 1989-06-25

被引用文献数

12

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In the general rule, Puerariae Flos or it's combination drugs are used in traditional medicinal system for counteraction to drinking among Japanese and Chinese therapy. One of such drugs is Kakkakaiseito. Here we report the results of investigation on some pharmacological actions including alcoholic metabolism. The experiments were carried out to confirm its actual effect on alcohol, acetaldehyde and ketone body metabolism in the blood and the alteration of behaviour pattern of mice. Drugs used in this study were methanolic extract (PF-ME), isoflavonoid fraction (PF-IF) and triterpenoid saponin fraction (PF-SP) isolated from Puerariae Flos. Each drug was orally administrated to mice. These results were shown as follows : the concentrations of blood alcohol and acetaldehyde decreased more after the treatment with PF-IF (800 mg/kg) than those of the control group. This fact was evidenced remarkable effects with area under the blood concentration-time curve, mean residence time, and variance residence time and values on the moment analysis. However, a reduction effect was not recognized by the treatment with PF-SP (1000 mg/kg). Moreover, PF-ME and PF-IF suppressed the increment of spontaneous movement induced by alcohol administration, whereas PF-SP did not prevent the decrease in the increment caused by alcohol administration. These results support the basis that Puerariae Flos or its combination drugs is used in a traditional medicinal system for counteraction to drinking. However, further investigation is necessary.

著者

矢原 正治 金城 順英 下川 隆志 野原 稔弘 山原 條二 千坂 武司

出版者

天然有機化合物討論会

雑誌

天然有機化合物討論会講演要旨集

巻号頁・発行日

no.27, pp.726-733, 1985-09-07

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We have examined the constituents of three crude drugs showing an antihypercholesteremic activity. 1) Daemonorops draco --- D-7 was obtained as an active substance. It was further separated into two compounds (D-7-I,II) being the isomers each other and their substances were deduced to be the deoxy-proanthocyanidins by the spectral data. 2) Caesalpinia sappan --- Total nineteen compounds relating to brazilin were isolated and the chemical structures of fourteen compounds among them were discussed by the spectroscopic means. SO-k, g,e were the 3-benzyl-chroman-4-one derivatives; SO-i,b,c were shown to be the first examples of the 3-benzyl-chroman-4-ol derivatives and assumed to be the key-intermediates on the biogenetic route of brazilin; All of SO-j,p,SLC-b,c,d presented new novel framework-models among the naturally occurring compounds. SO-j was suggested to be produced from SO-i,b,c by oxidative coupling, SO-p was presumed to be derived from brazilin by oxidative fission. SLC-b,c,d were considered to be originated from brazilin. SLC-b was effective for antihypercholesteremia. 3) Dalbergia odorifera --- Five aromatic compounds, DO-I-V, were isolated from the active fraction and their structures were revealed to be the unique bi-isoflavanoids by the various spectral data.

著者

新甫 勇次郎 山崎 律 中島 嘉次郎 伊東 宏 竹下 尚 金城 順英 野原 稔弘

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.110, no.8, pp.604-611, 1990-08-25 (Released:2008-05-30)

参考文献数

33

被引用文献数

8 19

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The present study was designed to examine the effects of methanolic extract (PE-ME), isoflavonoid fraction (PF-IF), triterpenoid saponin fraction (PF-SP) and N-acyl-N1-glucosyl-tryptophan (PF-P) isolated from puerariae flos on alcohol-induced unusual metabolism (as for glucose (BG), triglyceride (TG), and urea nitrogen (BUN) level in blood) and experimental liver injury (model : CCl4-and high fatty food induced) in mice. These alcohol-induced increasing responses were inhibited by the extracted and refined substances from puerariae flos. In short, PF-ME (4500 mg/kg) and PF-P (400 mg/kg) inhibited an increase in BG level induced by alcohol, whereas PF-IF (1000 mg/kg) and PF-SP (1000 mg/kg) did not. Similary, PF-ME and PF-SP inhibited an increase in TG induced by alcohol, whereas PF-IF did not. In addition, PF-IF and PF-SP inhibited increasing BUN level. Still more, PF-IF and PF-SP significantly inhibited an increase in gulutamate oxalacetate transaminase or gulutamate pyruvate transaminase level induced by high-fatty food and CCl4 in control animals. Especially PF-IF (250 mg/kg) administration showed a remarkable effect (inhibition : 76.3%) in control animals. These results suggested that puerariae flos or its combination drugs may be a useful drug as a traditional medicinal system for counteraction to drinking.

著者

新甫 勇次郎 山崎 律 中島 嘉次郎 伊東 宏 竹下 尚 金城 順英 野原 稔弘

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.109, no.6, pp.424-431, 1989-06-25 (Released:2008-05-30)

参考文献数

26

被引用文献数

7 31

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In the general rule, Puerariae Flos or it's combination drugs are used in traditional medicinal system for counteraction to drinking among Japanese and Chinese therapy. One of such drugs is Kakkakaiseito. Here we report the results of investigation on some pharmacological actions including alcoholic metabolism. The experiments were carried out to confirm its actual effect on alcohol, acetaldehyde and ketone body metabolism in the blood and the alteration of behaviour pattern of mice. Drugs used in this study were methanolic extract (PF-ME), isoflavonoid fraction (PF-IF) and triterpenoid saponin fraction (PF-SP) isolated from Puerariae Flos. Each drug was orally administrated to mice. These results were shown as follows : the concentrations of blood alcohol and acetaldehyde decreased more after the treatment with PF-IF (800 mg/kg) than those of the control group. This fact was evidenced remarkable effects with area under the blood concentration-time curve, mean residence time, and variance residence time and values on the moment analysis. However, a reduction effect was not recognized by the treatment with PF-SP (1000 mg/kg). Moreover, PF-ME and PF-IF suppressed the increment of spontaneous movement induced by alcohol administration, whereas PF-SP did not prevent the decrease in the increment caused by alcohol administration. These results support the basis that Puerariae Flos or its combination drugs is used in a traditional medicinal system for counteraction to drinking. However, further investigation is necessary.

著者

野原 稔弘 池田 剛 桜田 忍 金城 順英

出版者

熊本大学

雑誌

基盤研究(B)

巻号頁・発行日

1999

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Incarvillateine (INCA)に関するこれまでの構造活性相関試験より、鎮痛活性発現に必要な基本骨格が明らかとなった。本結果を礎に、芳香環部あるいはアルカロイド部を多彩に変換することに依り、さらに強力な活性物質に導くことができるものと予想される。特にアルカロイド部分単独で強力な活性を有する化合物を本構造に導入することで、さらに活性を増強させることも可能であると考えられる。鎮痛作用発現のために重要な因子の中で、INCAの前駆体と考えられるモノマーのIncarvine Cが殆ど活性を示さなかったことより、特に二量体構造が、その強力な鎮痛活性発現に対して重要な役割を担っていることが示唆された。そこで、INCAと同様の立体構造を有するα型ジフェニルシクロブタンジカルボン酸:α-truxillic acid (TA)、および4,4'-dihydroxy-α-truxillic acid (DHTA)の二種を合成して鎮痛活性を検討した結果、腹腔内投与において、これら両者がホルマリンテストの第二相目の炎症性の疼痛行動を強力に抑制することが明らかとなった。特にDHTAはINCA以上の鎮痛活性を示し、NSAIDsの一般的な投与方法である経口投与においても、市販薬として繁用査されるロキソニンとほぼ同等の鎮痛抗炎症活性を示した。さらに、尿酸結晶を用いたラットの痛風モデルにおける痛みに対しても強力な鎮痛効果を示した。また、DHTAの大量経口投与時における潰瘍の発生は全く認められなかった。さらに多種のTAおよびその誘導体を合成し、鎮痛効果の比較および検討を行なった結果、同二相目における疼痛行動の抑制効果は、シクロブタン環の存在、α型の立体構造、シクロブタン環の遊離カルボン酸の存在、ならびに芳香環上の置換基の種類が重要な因子であることが判明した。