JP4633399B2 - グルコシルトランスフェラーゼ阻害剤 - Google Patents
グルコシルトランスフェラーゼ阻害剤 Download PDFInfo
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- JP4633399B2 JP4633399B2 JP2004230609A JP2004230609A JP4633399B2 JP 4633399 B2 JP4633399 B2 JP 4633399B2 JP 2004230609 A JP2004230609 A JP 2004230609A JP 2004230609 A JP2004230609 A JP 2004230609A JP 4633399 B2 JP4633399 B2 JP 4633399B2
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- extract
- junsai
- glucosyltransferase
- lotus
- added
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- 230000000052 comparative effect Effects 0.000 description 1
- 229920002770 condensed tannin Polymers 0.000 description 1
- 210000003298 dental enamel Anatomy 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 238000000502 dialysis Methods 0.000 description 1
- 230000029087 digestion Effects 0.000 description 1
- 229940101029 dipotassium glycyrrhizinate Drugs 0.000 description 1
- POLCUAVZOMRGSN-UHFFFAOYSA-N dipropyl ether Chemical compound CCCOCCC POLCUAVZOMRGSN-UHFFFAOYSA-N 0.000 description 1
- 230000035622 drinking Effects 0.000 description 1
- 229960002852 ellagic acid Drugs 0.000 description 1
- 235000004132 ellagic acid Nutrition 0.000 description 1
- 235000019414 erythritol Nutrition 0.000 description 1
- 229940009714 erythritol Drugs 0.000 description 1
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 150000002170 ethers Chemical class 0.000 description 1
- 229940072117 fennel extract Drugs 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000000174 gluconic acid Substances 0.000 description 1
- 235000012208 gluconic acid Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 239000003292 glue Substances 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 229940091561 guaiac Drugs 0.000 description 1
- 229920000588 gutta-percha Polymers 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 230000023597 hemostasis Effects 0.000 description 1
- FUZZWVXGSFPDMH-UHFFFAOYSA-N hexanoic acid Chemical compound CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 description 1
- 239000008123 high-intensity sweetener Substances 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 150000002576 ketones Chemical class 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 235000019421 lipase Nutrition 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 235000013372 meat Nutrition 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- FAARLWTXUUQFSN-UHFFFAOYSA-N methylellagic acid Natural products O1C(=O)C2=CC(O)=C(O)C3=C2C2=C1C(OC)=C(O)C=C2C(=O)O3 FAARLWTXUUQFSN-UHFFFAOYSA-N 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 239000012046 mixed solvent Substances 0.000 description 1
- 235000001968 nicotinic acid Nutrition 0.000 description 1
- 239000011664 nicotinic acid Substances 0.000 description 1
- 229960003512 nicotinic acid Drugs 0.000 description 1
- 235000013615 non-nutritive sweetener Nutrition 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 229920001778 nylon Polymers 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 238000005325 percolation Methods 0.000 description 1
- 239000008055 phosphate buffer solution Substances 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 235000019423 pullulan Nutrition 0.000 description 1
- HELXLJCILKEWJH-NCGAPWICSA-N rebaudioside A Chemical compound O([C@H]1[C@H](O)[C@@H](CO)O[C@H]([C@@H]1O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O HELXLJCILKEWJH-NCGAPWICSA-N 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- 229940112950 sage extract Drugs 0.000 description 1
- 235000020752 sage extract Nutrition 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 230000002000 scavenging effect Effects 0.000 description 1
- 239000004208 shellac Substances 0.000 description 1
- 235000013874 shellac Nutrition 0.000 description 1
- ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 description 1
- 229940113147 shellac Drugs 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- KSAVQLQVUXSOCR-UHFFFAOYSA-M sodium lauroyl sarcosinate Chemical compound [Na+].CCCCCCCCCCCC(=O)N(C)CC([O-])=O KSAVQLQVUXSOCR-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 235000019408 sucralose Nutrition 0.000 description 1
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 238000009210 therapy by ultrasound Methods 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 235000015961 tonic Nutrition 0.000 description 1
- 230000001256 tonic effect Effects 0.000 description 1
- 229960000716 tonics Drugs 0.000 description 1
- 108010021724 tonin Proteins 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- 239000000052 vinegar Substances 0.000 description 1
- 235000021419 vinegar Nutrition 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 239000005019 zein Substances 0.000 description 1
- 229940093612 zein Drugs 0.000 description 1
Landscapes
- Cosmetics (AREA)
- Medicines Containing Plant Substances (AREA)
- Confectionery (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
Description
<処方> 配合量(%)
1.リン酸水素カルシウム 42.0
2.ラウリル硫酸ナトリウム 1.2
3.グリセリン 18.0
4.カラギーナン 0.9
5.サッカリンナトリウム 1.0
6.グルコン酸クロルヘキシジン 0.1
7.香料 0.1
8.パラオキシ安息香酸エチル 0.1
9.実施例2のハスの雄しべ抽出液 2.0
10.水 残部
合計 100.0
<製法>
成分3〜10をよく混合した後、成分1及び2を加えて練和し、脱泡後チューブに充填して練歯磨を得た。
<処方> 配合量(%)
1.炭酸カルシウム 42.0
2.ラウリル硫酸ナトリウム 1.2
3.グリセリン 18.0
4.カラギーナン 0.9
5.サッカリンナトリウム 1.0
6.塩化セチルピリジニウム 0.05
7.香料 0.1
8.パラオキシ安息香酸エチル 0.1
9.実施例6のジュンサイ抽出液 2.0
10.水 残部
合計 100.0
<製法>
成分3〜10をよく混合した後、成分1及び2を加えて練和し、脱泡後チューブに充填して練歯磨を得た。
<処方> 配合量(%)
1.ハイドロキシアパタイト 42.0
2.ラウリル硫酸ナトリウム 1.0
3.グリセリン 18.0
4.カルボキシメチルセルロース 1.5
5.サッカリンナトリウム 0.5
6.イソプロピルメチルフェノール 0.1
7.香料 0.1
8.パラオキシ安息香酸エチル 0.1
9.実施例10のラフマ抽出液 4.0
10.水 残部
合計 100.0
<製法>
成分3〜10をよく混合した後、成分1及び2を加えて練和し、脱泡後チューブに充填して練歯磨を得た。
<処方> 配合量(%)
1.エタノール 20.0
2.グリセリン 10.0
3.塩化セチルピリジニウム 0.05
4.サッカリンナトリウム 0.1
5.香料 0.1
6.ポリオキシエチレン硬化ヒマシ油 1.5
7.パラオキシ安息香酸メチル 0.1
8.実施例4のハスの雄しべ抽出物 1.0
9.水 残部
合計 100.0
<製法>
成分9に成分2〜8を溶解した後、成分1加えて洗口液を得た。
<処方> 配合量(%)
1.エタノール 10.0
2.グリセリン 15.0
3.イソプロピルメチルフェノール 0.1
4.サッカリンナトリウム 0.1
5.香料 0.1
6.ポリオキシエチレン硬化ヒマシ油 1.5
7.パラオキシ安息香酸メチル 0.1
8.実施例8のジュンサイ抽出物 2.0
9.水 残部
合計 100.0
<製法>
成分9に成分2〜8を溶解した後、成分1加えて洗口液を得た。
<処方> 配合量(%)
1.エタノール 10.0
2.ソルビトール 10.0
3.トリクロサン 0.02
4.サッカリンナトリウム 0.1
5.香料 0.1
6.ポリオキシエチレン硬化ヒマシ油 1.5
7.グリチルリチン酸ジカリウム 0.1
8.パラオキシ安息香酸メチル 0.1
9.実施例12のラフマ抽出物 1.0
10.水 残部
合計 100.0
<製法>
成分10に成分2〜9を溶解した後、成分1加えて洗口液を得た。
<処方> 配合量(%)
1.実施例3のハスの雄しべ抽出物 5.0
2.マルチトール 47.0
3.キシリトール 44.0
4.香料 1.0
5.ショ糖脂肪酸エステル 3.0
合計 100.0
<製法>
成分1〜4を混合し、流動層造粒装置で造粒する。得られた顆粒に成分5を加えて打錠し、1錠1000mgのトローチを得た。
<処方> 配合量(%)
1.実施例5のジュンサイ抽出物 4.0
2.還元麦芽糖水飴 95.0
3.香料 1.0
合計 100.0
<製法>
成分1、2を水に溶解させて145℃で煮詰めた後、90〜100℃に冷却して成分3を混合し、冷却固化させてキャンディーを得た。
<処方> 配合量(%)
1.ガムベース 30.0
2.マルチトール 48.0
3.キシリトール 20.0
4.実施例11のラフマ抽出物 1.0
5.香料 1.0
合計 100.0
<製法>
加温した成分1に、成分2及び3を加えて練和する。更に成分4及び5を加えてよく練和した後、圧延してシート状にし、切断してチューインガムを得た。
ストレプトコッカス・ミュータンスJCM5705株を、ブレインハート・インフュージョン培地500mLに接種し、37℃で24時間培養した。培養液を14,000rpmで20分間遠心分離し、上澄液に硫酸アンモニウムを飽和(50%)させて沈殿を生じさせた。再度14,000rpmで20分間遠心分離し、得られた沈殿物をpH6.5の50mMリン酸緩衝液15mLに溶解し、同緩衝液を用いて十分に透析を行った。透析内液を0.45μmのメンブランフィルターでろ過し、ストレプトコッカス・ミュータンスが産生するグルコシルトランスフェラーゼ粗酵素液とした。
実施例1、実施例3、実施例4、実施例5、実施例7、実施例8、実施例9、実施例11、及び実施例12の抽出物についてグルコシルトランスフェラーゼの活性阻害を測定した。pH6.5の50mMリン酸緩衝液で調整した2%ショ糖溶液1.0mL、1%アジ化ナトリウム溶液0.1mL及び試料溶液0.8mL、並びに前述のグルコシルトランスフェラーゼ粗酵素液0.1mLを試験管に入れて混合し、試料とした。尚、それぞれの抽出物の濃度は、抽出物の乾燥物として1μg/mL〜250μg/mLの間で各種調製した。試料の入った試験管を30°に傾けて37℃で15時間静置した後、反応液を穏やかに除き、生成した水不溶性のグルカンを精製水で3回洗浄した。当該グルカンに精製水1mLを加えて超音波処理で均一に分散し、波長550nmにおける吸光度を測定した。又、抽出物の溶液の代わりに、pH6.5の50mMリン酸緩衝液を用いて同様に処理し、コントロールとした。得られた吸光度と下記の式から、グルコシルトランスフェラーゼの活性の阻害率を算出し、阻害率が50%となる抽出物の濃度を求めてIC50とした。比較例として、公知のグルコシルトランスフェラーゼ阻害剤である茶ポリフェノールのIC50を、市販製剤のテアフラン(登録商標)90Sを用い、同様の方法で求めた。以上の試験により得られたIC50を、表1に示す。
阻害率(%)=(1−試料溶液の吸光度/コントロール溶液の吸光度)×100
ウサギの前歯を1M水酸化ナトリウム溶液中で超音波処理し、肉片等を完全に除去してデシケーター中で1晩放置後、重量を測定して以下の試験に使用した。ブレインハート・インフュージョン培地に各抽出物が0.1%及びショ糖が5%となるように溶解して試験培地とし、バイアル瓶に入れ、準備したウサギの前歯をナイロン糸で瓶内に吊るして密封し、121℃で15分加熱した。これにストレプトコッカス・ミュータンスJCM5705株を接種し、試験培地を24時間毎に交換しながら37℃で96時間培養した。ウサギの前歯をバイアル瓶から取り出し、精製水中で超音波処理して付着物を回収し、精製水除去後の残渣をデシケーター中で一晩放置後、重量を測定して付着歯垢重量とした。コントロールは、各抽出物を精製水に置換したものを用いた。歯垢抑制率は、コントロールと各抽出物の試験における付着歯垢重量、コントロールと各抽出物の試験に用いたウサギの前歯の重量、及び下記の式より算出した。結果を表2に示す。
歯垢形成抑制率(%)=〔A−(B×C/D)〕/A×100
A:コントロールの試験における付着歯垢重量
B:各抽出物の試験における付着歯垢重量
C:コントロールの試験に用いたウサギの前歯の重量
D:各抽出物の試験に用いたウサギの前歯の重量
前述の歯垢形成抑制試験のウサギの前歯について、試験後の損傷面積及び試験前後の歯表面の光沢の変化を実体顕微鏡で観察した。結果を表3及び表4に示す。
Claims (3)
- ハスの雄しべ抽出物、ジュンサイ抽出物、及びラフマ抽出物よりなる群から選択される少なくとも1種の抽出物を有効成分として含有することを特徴とするグルコシルトランスフェラーゼ阻害剤。
- ハスの雄しべ抽出物及び/又はジュンサイ抽出物を有効成分として含有することを特徴とする歯垢形成抑制剤。
- ハスの雄しべ抽出物及び/又はジュンサイ抽出物を有効成分として含有することを特徴とする抗う蝕剤。
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JPH1053512A (ja) * | 1996-08-09 | 1998-02-24 | Kanebo Ltd | 口腔用組成物 |
JP2005035908A (ja) * | 2003-07-18 | 2005-02-10 | Nonogawa Shoji Kk | 抗歯周病剤 |
JP2005035907A (ja) * | 2003-07-18 | 2005-02-10 | Nonogawa Shoji Kk | 抗歯周病剤 |
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JPH1053512A (ja) * | 1996-08-09 | 1998-02-24 | Kanebo Ltd | 口腔用組成物 |
JP2005035908A (ja) * | 2003-07-18 | 2005-02-10 | Nonogawa Shoji Kk | 抗歯周病剤 |
JP2005035907A (ja) * | 2003-07-18 | 2005-02-10 | Nonogawa Shoji Kk | 抗歯周病剤 |
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