TWI337066B - Dietary supplement - Google Patents
Dietary supplement Download PDFInfo
- Publication number
- TWI337066B TWI337066B TW092129007A TW92129007A TWI337066B TW I337066 B TWI337066 B TW I337066B TW 092129007 A TW092129007 A TW 092129007A TW 92129007 A TW92129007 A TW 92129007A TW I337066 B TWI337066 B TW I337066B
- Authority
- TW
- Taiwan
- Prior art keywords
- composition
- vitamin
- quercetin
- juice
- aforementioned
- Prior art date
Links
- 235000015872 dietary supplement Nutrition 0.000 title claims description 5
- 239000000203 mixture Substances 0.000 claims abstract description 61
- REFJWTPEDVJJIY-UHFFFAOYSA-N Quercetin Chemical compound C=1C(O)=CC(O)=C(C(C=2O)=O)C=1OC=2C1=CC=C(O)C(O)=C1 REFJWTPEDVJJIY-UHFFFAOYSA-N 0.000 claims abstract description 38
- ZVOLCUVKHLEPEV-UHFFFAOYSA-N Quercetagetin Natural products C1=C(O)C(O)=CC=C1C1=C(O)C(=O)C2=C(O)C(O)=C(O)C=C2O1 ZVOLCUVKHLEPEV-UHFFFAOYSA-N 0.000 claims abstract description 23
- HWTZYBCRDDUBJY-UHFFFAOYSA-N Rhynchosin Natural products C1=C(O)C(O)=CC=C1C1=C(O)C(=O)C2=CC(O)=C(O)C=C2O1 HWTZYBCRDDUBJY-UHFFFAOYSA-N 0.000 claims abstract description 23
- MWDZOUNAPSSOEL-UHFFFAOYSA-N kaempferol Natural products OC1=C(C(=O)c2cc(O)cc(O)c2O1)c3ccc(O)cc3 MWDZOUNAPSSOEL-UHFFFAOYSA-N 0.000 claims abstract description 23
- 235000005875 quercetin Nutrition 0.000 claims abstract description 23
- 229960001285 quercetin Drugs 0.000 claims abstract description 23
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims abstract description 19
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 claims abstract description 18
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims abstract description 16
- PFTAWBLQPZVEMU-ZFWWWQNUSA-N (+)-epicatechin Natural products C1([C@@H]2OC3=CC(O)=CC(O)=C3C[C@@H]2O)=CC=C(O)C(O)=C1 PFTAWBLQPZVEMU-ZFWWWQNUSA-N 0.000 claims abstract description 11
- PFTAWBLQPZVEMU-UKRRQHHQSA-N (-)-epicatechin Chemical compound C1([C@H]2OC3=CC(O)=CC(O)=C3C[C@H]2O)=CC=C(O)C(O)=C1 PFTAWBLQPZVEMU-UKRRQHHQSA-N 0.000 claims abstract description 11
- LPTRNLNOHUVQMS-UHFFFAOYSA-N epicatechin Natural products Cc1cc(O)cc2OC(C(O)Cc12)c1ccc(O)c(O)c1 LPTRNLNOHUVQMS-UHFFFAOYSA-N 0.000 claims abstract description 11
- 235000012734 epicatechin Nutrition 0.000 claims abstract description 11
- AUNGANRZJHBGPY-UHFFFAOYSA-N D-Lyxoflavin Natural products OCC(O)C(O)C(O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-UHFFFAOYSA-N 0.000 claims abstract description 9
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 claims abstract description 9
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims abstract description 9
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 claims abstract description 9
- 229930003471 Vitamin B2 Natural products 0.000 claims abstract description 9
- 229930003537 Vitamin B3 Natural products 0.000 claims abstract description 9
- 229930003268 Vitamin C Natural products 0.000 claims abstract description 9
- 229960003512 nicotinic acid Drugs 0.000 claims abstract description 9
- DFPAKSUCGFBDDF-UHFFFAOYSA-N nicotinic acid amide Natural products NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims abstract description 9
- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 claims abstract description 9
- 229960002477 riboflavin Drugs 0.000 claims abstract description 9
- 235000019164 vitamin B2 Nutrition 0.000 claims abstract description 9
- 239000011716 vitamin B2 Substances 0.000 claims abstract description 9
- 235000019160 vitamin B3 Nutrition 0.000 claims abstract description 9
- 239000011708 vitamin B3 Substances 0.000 claims abstract description 9
- 235000019158 vitamin B6 Nutrition 0.000 claims abstract description 9
- 239000011726 vitamin B6 Substances 0.000 claims abstract description 9
- 235000019154 vitamin C Nutrition 0.000 claims abstract description 9
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- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 claims abstract description 8
- 229930003779 Vitamin B12 Natural products 0.000 claims abstract description 8
- 229960001948 caffeine Drugs 0.000 claims abstract description 8
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 claims abstract description 8
- FDJOLVPMNUYSCM-WZHZPDAFSA-L cobalt(3+);[(2r,3s,4r,5s)-5-(5,6-dimethylbenzimidazol-1-yl)-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl] [(2r)-1-[3-[(1r,2r,3r,4z,7s,9z,12s,13s,14z,17s,18s,19r)-2,13,18-tris(2-amino-2-oxoethyl)-7,12,17-tris(3-amino-3-oxopropyl)-3,5,8,8,13,15,18,19-octamethyl-2 Chemical compound [Co+3].N#[C-].N([C@@H]([C@]1(C)[N-]\C([C@H]([C@@]1(CC(N)=O)C)CCC(N)=O)=C(\C)/C1=N/C([C@H]([C@@]1(CC(N)=O)C)CCC(N)=O)=C\C1=N\C([C@H](C1(C)C)CCC(N)=O)=C/1C)[C@@H]2CC(N)=O)=C\1[C@]2(C)CCC(=O)NC[C@@H](C)OP([O-])(=O)O[C@H]1[C@@H](O)[C@@H](N2C3=CC(C)=C(C)C=C3N=C2)O[C@@H]1CO FDJOLVPMNUYSCM-WZHZPDAFSA-L 0.000 claims abstract description 8
- DPJRMOMPQZCRJU-UHFFFAOYSA-M thiamine hydrochloride Chemical compound Cl.[Cl-].CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N DPJRMOMPQZCRJU-UHFFFAOYSA-M 0.000 claims abstract description 8
- 235000019163 vitamin B12 Nutrition 0.000 claims abstract description 8
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- 229940030275 epigallocatechin gallate Drugs 0.000 claims abstract description 6
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 14
- 244000269722 Thea sinensis Species 0.000 claims description 13
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 claims description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 10
- 229930003427 Vitamin E Natural products 0.000 claims description 7
- 235000016213 coffee Nutrition 0.000 claims description 7
- 235000013353 coffee beverage Nutrition 0.000 claims description 7
- 235000011389 fruit/vegetable juice Nutrition 0.000 claims description 7
- 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 claims description 7
- 235000019165 vitamin E Nutrition 0.000 claims description 7
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- 235000015895 biscuits Nutrition 0.000 claims description 6
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- Organic Insulating Materials (AREA)
Description
1337066 $ 玫、發明說明: - 【發明所屬之技術領域】 . 本發明係關於一種抗氧化之組成物。 【先前技術】 部分天然抗氧•化物,如植物類黃酮素(flavonoid),能抑制自 由基所引起的急性或慢性疾病;並且,某些天然抗氧化物在與生 物相關氧化物如氫氧自由基、過氧化物、氧硫化物(oxysulfurs)、 二氧化硫及二氧化乳化反應時存在增效作用(synergy)。例如,研 究已指出維他命C及酚醛(phenolic)抗氧化物的協同抗氧化能力。 【發明内容】 本發明係根據一項超出預期的發現,槲皮素(quercetin),一 種抗氧化物’及多種其他天然產物具有增進健康的功效。 本發明係提供一種組成物,包含下列成份:維他命B1、維他 命B2、維他命B3、維他命B6、維他命B12、維他命C、咖啡因、 槲皮素(quercetin)、表沒食子兒茶素酸酯(epigall〇catechin gallate)、表兒茶素(epicatechin)、兒茶素沒食子酸酯(epicatechin gallate)、表沒食子兒茶素(epigaii〇catechin)及茶多盼(polyphenon E)。 前述組成物係可包含其他成分,如維他命E、輔酶 QlO(CoQ-lO)、黃豆類黃綱素(SOy isoflavones)、牛石黃酸(taurine)、 甜菜果膠纖維(sugar beet pectin fiber)或銀杏萃取物(ginko biloba extract)。前述組成物並可進一步視需要添加糖精以提高甜度,前 述糖精例如山梨醇(sorbitol)、麥芽糖醇(mahit〇l) '蔗糖、高乳糖 玉米糖漿或其他相似糖精。前述組成物也可包含胺基酸、礦物 質、增味劑或增色劑。綠茶的樹葉已知包含表沒食子兒茶素酸酯 (epigallocatechin gallate)、表兒茶素(epicatechin)、兒茶素沒食子 酸酯(epicatechin gallate)、表沒食子兒茶素(epigaii〇catechin)及茶 5 1337066 多酿'(polyphenonE),因此前述五種成份適合由綠茶萃取物提供。 本發明之組成物係可為乾燥型態(如粉末或藥片)或水溶液型 態(如飲料或糖漿),其可為飲食補充劑或藥劑,亦可為飲料或食 品,例如:茶(如茶飲料或茶包成份)、汽水、果汁(如水果萃取物 或果汁飲料)、牛奶、咖°非、餅乾、麥片、巧克力及點心棒。本發 明之組成物在任何前述形式下皆可用於治療關節炎、腫瘤、性障 礙、慢性便秘、腸發炎等疾病;改善注意力或心情;及降低膽固 醇或血壓。本發明之另一目的係使用本發明之組成物作為活性藥 劑及製造藥劑的成份之一,用於治療前述疾病。 本發明之詳細實施例係依循前述之目的詳述於實施方式 中,其他本發明之特徵、目的及優點係說明於實施方式及申請專 利範圍中。 【實施方式】 本發明組成物包含維他命B1、維他命B2、維他命B3、維他 命B6、維他命B 12、維他命C、咖0非因、槲皮素(quercetin)、表 沒食子兒茶素酸酿(epigallocatechin gallate)、表兒茶素 (epicatechin)、兒茶素沒食子酸醋(epicatechin gallate)、表沒食子 兒茶素(epigallocatechin)及茶多酌'(ροΐγρίιεηοη E)。綠茶萃取物適 合用於提供表沒食子兒茶素酸酯(epigallocatechin gallate)、表兒 茶素(epicatechin)、兒茶素沒食子酸酯(epicatechin gallate)、表沒 食子兒茶素(epigallocatechin)及茶多盼(polyphenon E)。 前述組成物之示範性組成成份含量係為:0.1-50mg維他命 Bl、0.1-150mg 維他命 B2、0.1-2000mg 維他命 B3、0.1-200mg 維 他命 B6,5-150"g 維他命 B12、50-2000mg 維他命 C、50-15 OOmg 咖0非因、20-2000mg樹皮素(quercetin)、10-500mg表沒食子兒茶 素酸自旨(epigallocatechin gallate)、10-500mg 表兒茶素 (epicatechin)、10-500mg 兒茶素沒食子酸酷(epicatechin gallate)、 1337066 % 10-500mgm子兒茶素(epigal丨〇加心丨啦i〇5_g茶多紛 (polyphenonE) ’其中前述組成成份係可溶解或分散於il水溶液 中。前述組成成份之含量係、可為與前述含量相同之相對比率。前 述名3樹皮素係扎樹皮素配糖甘基(quercet丨及树皮素 •f亍生物例如,樹皮素-3-0-葡萄糖甘(qUercetin_3_〇_giuc〇sjde)、 槲皮素-5-0-葡萄糖甘(quercetin_5_〇_gluc〇side)、槲皮素_7_〇-葡萄 糖甘(quercetin-7-〇-glucoside)、槲皮素-9-0-葡萄糖甘 (quercetin-9-O-glucoside)、槲皮素-3-0-芸香甘 (quercetin-3-O-rutinoside)、槲皮素 _3_0_[α_ i 李糖 —2)_α_ 鼠李 糖-(1 — 6)]-β-蘭萄糖甘(qUercetin_3_〇_[a_rhamnoSy|_(i — 2)-ot-rhamnosyl-(l -> 6)]-p-glucoside)、槲皮素-3-0-半乳糖甘 (quercetin-3-O-galactoside)、槲皮素-7-0-半乳糖甘 (quercetin-7-O-galactoside)、槲皮素-3-0-鼠李糖甘 (quercetin-3-O-rhamnoside)及槲皮素-7-0-鼠李糖甘 (quercetin-7-O-rhamnoside)。在消化後,槲皮素衍生物會轉化為 槲皮素配糖甘基,一可被身體吸收的活性型態。前述之槲皮素含 量係指槲皮素配糖甘基或槲皮素衍生物中槲皮素部分。例如:每 日使用的組成物係可為1L水溶液,該水溶液中包含1 〇〇〇mg槲皮 素、30mg維他命Bl、85mg維他命B2、lg維他命B3、lOOmg 維他命B6,120" g維他命B12、1200mg維他命C、1000IU維他 命E、lOOOmg咖啡因及包含120mg表沒食子兒茶素酸酯、MOmg 表兒茶素、360mg兒茶素沒食子酸酯、360mg表沒食子兒茶素及 120mg茶多盼(polyphenonE)的綠茶萃取物。 前述組成物也可包含一種或多種其他活性組成成份,如維他 命E、輔酶Q10、黃豆類黃酮素、牛磺酸、甜菜果膠纖維及銀杏 萃取物。這些組成成份的示範性含量為:3-1000 IU維他命E ' 10-400mg輔酶Q10、20-600mg黃豆類黃酮素、10-1000mg牛磺 1337066 酸' l-15g甜采果膠纖維及5〇_5〇〇mg銀杏萃取物(乾重)。前述組 成物並可進一步視需要藉由添加糖精來提高甜度,添加糖精例如 . 為山梨醇、麥芽糖醇、氫化葡萄糖漿、氫化澱粉水解物、高乳糖 .j 玉米糖水嚴糖、甜菜糖、果膠及薦糖素(sucralose)。 。 • 前述組成物的一個例子係為粉末形式,該粉末狀之組成物適 合用於製備飲料,如茶或果汁。前述粉末組成物亦可用於製備軟 膏、凝膠、膠囊或藥片。乳糖及玉米澱粉一般在膠囊中作為稀釋 物或在藥片中作為載體;一般可加入潤滑劑,如硬脂酸鎂 (magnesium stearate),以形成藥片。 本發明之組成物係可為飲食補充劑或藥劑。作為飲食補充劑 時,該組成物包含額外的營養物,如礦物質或氨基酸。前述組^ 物亦可為飲料或食品,如茶、汽水、果汁、牛奶、咖啡、餅乾、 麥片、巧克力及點心棒。 本發明之組成物在任何前述形式下皆可用於治療疾病或失 調症狀,如關節炎、腫瘤、性障礙、慢性便秘、腸發炎等疾病; 並改善注意力或心情;及降低膽固醇或血壓。名詞,,腫瘤”係指良 性腫瘤及惡性腫瘤(白血癌。、結腸癌、腎臟癌、肝癌、乳癌^ 癌)。名詞”治療,’、”改善”及,,降低”係㈣一具有一種或兩種之前 述疾病或失調症狀之對象,或具有—種或多種前述疾病之徵候或 傾向之對象服用-有效量之本發明組成物,其目的在治療減 輕、減緩、醫治或改善-種❹種之前述疾病或失調症狀或前 述疾病或失調症狀之徵候或傾向。名詞,’服用,,包含以口服或非口 服方式提供本發明之組成物給一對象,該組成物可為任何適合之 形式,如食品、飲料、藥片、膠囊、懸浮液及溶液。名詞,,非口服” 係指皮下、皮膚、靜脈、肌肉、關節、動脈、滑液、胸骨、囊内、 椎管内、或顧.内注射,及不同的注入方法。名詞,,有效量,,係指組 成物之劑量能充分提供治療療效,如降低膽固醇量或血壓。體内 1337066 及體外研究可用於推論決定最佳服用路徑及劑量。 下列實施例係僅用於進一步瞭解本發明,並非用於限制本發 明之揭露範圍。任何熟悉本技術領域之人士係可依本說明書揭露 之内谷,不需進一步闡述’進一步利用本發明使其發揮最大效 用。本說明書中引述之所有文獻係藉由參考全文方式併入本說明 書中。 配方l(formulation 1)之製備係描述如下。室溫下,在30mL 的純水中加入維他命B1 (8mg)、維他命B2(21.1mg)、維他命 B3(248mg)、維他命 B6(24.8mg)、維他命 B12(20.4mg)、維他命 C(74.4mg)、維他命Ε(3 7·2 IU)、咖啡因(99.2mg)、槲皮素糖甘基 (248mg)、及包含表沒食子兒茶素酸酯(8〇mg)、表兒茶素(80mg) ' 兒茶素沒食子酸酯(80mg)、表沒食子兒茶素(80mg)及茶多酚 (polyphenon E)(80mg)的綠茶萃取物。所有組成成份係可自 Spectrum Laboratory Products, Inc., Gardena, CA ; sigma, St.Louis, MO ;及Aldrich,Milwaukee,WI.獲得。前述混合物係由食物混拌機 劇烈攪拌,然後以純水稀釋至150mL。 在一實驗中,雄性 Spregue-dawley 鼠(150-180 克,Charles River Lab,boston, ΜΑ)放在頂端有渡網的籠子並可自由取用食物 和水,並養在一控制溫度的正壓房間内,在試驗期間内並控制曝 光週期。腸發炎疾病(如Crohn’s疾病)、結腸炎(結腸成長造成的 發炎)之動物模型,係藉由在結腸内灌入溶於0.5ml體積比30% 乙醇之25mg附著素(hapten)反應劑及2,4-二硝基苯磺酸 (2,4-dinitrobenzenesulfonic acid,TCI,Japan)引發。每一隻小鼠 先以metafane麻木,接著,以PE 50插管將DNBS/乙醇注入結腸 内距離肛門8公分處,然後透過插管緩慢注入2ml空氣以確保溶 液留在結腸中,之後將小鼠維持直立位置30秒後放回鼠籠中。 以相同的方法,空白對照組小鼠注入0.5m卜30%乙醇。請參閱 1337066
Hogaboam,etal,Eur.J· Pharmacol.(1996)309:26卜269。配方 1 及槲 皮素配糖甘基溶液(包含最終濃度為1%之甲基纖維素(MC))分別 • 以一天一次的口服方式餵給小鼠,持續7天。每日每公斤體重的 • 劑量包含3.125 mg至25 mg的槲皮素配糖甘基。每24小時監測 • 小鼠的體重。七天後,犧牲小鼠並取出結腸秤重。在取出每一條 結腸前’記錄結腸與其他器官在打開的腹腔中是否存在沾黏情 形’然後計算出每隻動物的結腸-體重比率,載體控制組 (vehicle-control)相對於空白對照組(biank_c〇ntr〇i)的淨增加比率 係作為與治療組比較的基準值。配方丨與槲皮素糖甘基兩者在劑 里25mg/kg下此抑制結腸成長,但在3.125mg/kg的劑量下無法抑 制結腸成長。然而,在6.25 mg/kg和12.5 mg/kg的劑量下,配方 1抑制結腸成長效果遠比槲皮素配糖甘基有效。 在另一貫驗中,以懸浮土壤製備1 〇mg/ml之細菌懸浮液,在 不元全弗氏佐劑(incomplete Freund’s adjuvant)中加熱殺死結核桿 菌H37Ra。在雌性Lewis小鼠藉由皮膚注入〇.lml前述懸浮液至 尾巴底部以誘發佐劑誘發關節炎(AA)。在誘發後,以口服方式給 予該小鼠配方1或槲皮素配糖甘基溶液(1%MC) ,每天一次持續 12天,每曰劑量25mg/kg槲皮素配甘糖基。在關節炎發展關鍵期 間(從發k後10曰至25曰),多發性關節炎的發展病程每日用肉 眼觀察監測並指定一關節炎指數給每一隻動物。多發性關節炎的 強度依下列方法評定:(a)根據關節的紅斑、腫脹及畸形給予每隻 腳爪〇-3的等級評定,如〇表示沒有合紅斑或腫脹;如果在至= 一關節上可觀察到腫脹則給予〇.5 ;丨表示輕微的腫脹及紅斑;2 表不腳踝及腕骨都有腫脹及紅斑;3表示關節僵硬及骨頭畸形。 (b)評定其他身體部分等級:〇 5表示耳朵呈紅色,另一個則〇 5 表不耳朵有硬塊;1表示鼻子結缔組織腫脹;及丨表示尾巴硬塊 或扭結。參考 Schorle_er eta丨,Drugs ExpU CM ^ Ι337Ό66 (1991)17 : 471-483。與使用槲皮素配糖甘基治療的小鼠相較,以 配方1治療的小鼠在1 8天時顯示出較顯著的關節炎症狀改善效 果。 在另一實驗,雌性 BD2Fl(C57BL/6xDBA/2Fl)小鼠自 Charles River Lab獲得,小鼠可自由取用食物及水。從腹膜内接種50,000 p388白血病細胞至剛好滿7週的雌性BD2F1小鼠,作為癌症動 物模型。組成物1或槲皮素配糖基溶液(1 % M C)以口服方式讓小鼠 每曰服用一次持續14天,每曰劑量12.5 mg/kg槲皮素配糖基。 所有對照組小鼠(非治療組小鼠)在21天左右時因腹水而死亡。抗 癌能力係藉由比較治療組與對照組的平均存活時間來決定。參考 Yoshimatsu etal.,cancer Res. (1997) 57 : 3208-3213。與樹皮素配 糖基治療的小鼠相較,以配方1治療的小鼠顯示出較長的平均存 活時間。 磷酸二酯酵素-5(PDE-5)是一種參與性功能的酵素。在更進一 步的實驗中,PDE-5活性之決定係使用經部分修改之本技術領域 人士 所認同的方法。參考 Thompson et al,, Method Enzymol. (1974)38:205-212。純化PDE-5活性係藉由與PH 7.5混合物反應 量測’該混合物包含 8μΜ cGMP(64pCi/mI [3H]-cGMP)、40mM MOPS、0.5mM EGTA、15mM 醋酸鎂、0_15mg/ml BSA 及存在 ΙμΜ 至100//M不同濃度的配方1、槲皮素配糖基溶液及3_異丁基q 曱基貫°票吟(IBMX ’ 一種常見的PDE-5抑制劑)溶液(1 % mc)。該 反應在37°C反應60分鐘,然後加熱至70°C維持2分鐘以終止反 應。之後’標記之酵素反應產物[3H]-GMP在〇. 1單位的核甘酸酵 素(nucleotidase)存在下,降解成[3H]-鳥嘌呤及磷酸。最後,未降 解的[3H]-GMP吸附於陰離子交換樹脂,表層的[3H]_鳥嗓吟以液 體閃爍計數器(liquid scintillation counter)計算其放射性。社果顯 示配方1抑制PDE-5活性之能力表現出劑量依賴性,其IC5〇遠 1337066 低於槲皮素配糖基和ΙΒΜχ。 人體研究亦引導出本發明之其他兩種配方’即配方2和3 ° 配方2之製備方法如下。室溫下’在200mL的純水中加入維他命 Bl(30mg)、維他命 B2(85mg)、維他命 B3(lg)、維他命 B6(100mg)、 維他命 B12(120pg)、維他命 C(1200mg)、維他命 E(1000 IU)、咖 啡因(lOOOmg)、槲皮素糖甘基(l〇〇〇mg)、及一包含表沒食子兒茶 素酸酯(120mg)、表兒茶素(140mg)、兒茶素沒食子酸酯(360mg)、 表沒食子兒茶素(360mg)及茶多g分(p〇丨yphenon E)(120mg)的綠茶 萃取物’前述混合物係由食物混拌機劇烈攪拌,然後以純水稀釋 至1L。配方3之製備方法如下:室溫下,在2〇〇mL的純水中加 入維他命 Bl(3.75mg)、維他命 B2(4.25mg)、維他命 B3(50mg)、 維他命B6(5mg)、維他命B12(lVg)、维他命c(15〇mg)、維他命 E(7.5IU)'咖啡因(200mg)、槲皮素糖甘基(5〇mg)、及包含表沒食 子兒余素酸S旨(30mg)、表兒茶素(35mg)、兒茶素沒食子酸酯 (9〇mg)、表,又艮子兒佘素(9〇mg)及茶多酚(p〇lyphen〇n E)(3〇mg) 的綠茶萃取物’前述混合物以純水和柳燈汁稀釋至1L,最後溶液 中包含10%重量百分比的柳橙汁。
在-研究試射,4位錄和4位女性具有高膽固醇和高血 查的文測對象以配方2治療,每位受測對象每日飲帛i槪配方 2j2〇fl. oz·,或591mL)持續1〇日。然後,其中 對象和3位女性對象)繼續每日飲用 另丨又、J 另-半則停止此種食物療法5天再相^的配方持續20曰。 配方持續2〇日。結果顯示所有受用2瓶相同 善現象,膽固醇和血壓也下降至正常範圍和心情都有改 沒有觀察_著的體重減輕,兩個群 X測對象身上並 究期間感到口渴。 有—位受測對象在研 在另一研究試驗中 兩位男性受測對“兩位女性受測對象 12 Ι337Ώ66 持續1個月每日飲用2瓶配方2(20fl. oz.每瓶)。結果顯示所有受 測對象的心情和性慾皆有改善,他們的體重減輕範圍在1〇_25磅 (肢重的2-6%) ’在研究測試結束後,大部分受測對象心情愉快。 在另一研究測試中,一位男性和三位女性有嚴重便秘的受測 對象以配方3治療。每位受測對象持續丨週每日飲用ι_3瓶配方 3(2〇fl. oz.每瓶)。每位受測對象的便秘程度都減輕了。 在另一研究測試中,一位患有克隆式症(Cr〇hn,s disease)並有 *胃痛和《症狀的男性受測對象使用配方3治療。所有的症狀顯 著減輕並且其效果在研究測試結束後仍維持至少1週。 其他實施態樣 所有本說明書所揭露之特徵皆可以任冑形式與直他方法人 併使用。本說明書中所揭露之特徵可以具有相同、相等或相似目° 的的特徵所取代。因此’除了明確強調的部分之外,所有本說明 書中揭露的特徵僅為幕多相等或相似特徵中的—個實施例。 人士可所揭露的内容,任何—位熟習本技術領域的 確目㈣本㈣之重要特色,在不賴本發明之 =了,係可對本發明做不同的改變與修飾使其符 =目的與情況。因此,其料絲樣亦Μ在下” 13
Claims (1)
- 拾、申請專利範圍: L 一種作為飲食補充劑的組成物,其係包含: 0.1-50毫克的維他命B1 ; 0.1-15〇毫克的維他命B2 ; 0.1-2000毫克的維他命B3 ; 0.1-200毫克的維他命B6 ; 5-150微克的維他命B12 ; 50-2000毫克的維他命C ; 50-15〇〇毫克的咖啡因; 20-2000 毫克的樹皮素(quercetin); 10-500毫克的表沒食子兒茶素酸酯(epigallocatechin gallate); 10-500毫克的表兒茶素(epicatechin); 10-500毫克的兒茶素沒食子酸酯(epicatechin gallate); 10-500毫克的表沒食子兒茶素(epigall〇Catechin);及 10-500 毫克的茶多 g分(p〇iyphenon E); 其中,前述組成成份之含量係可為與前述含量相同之相對 比率。 2. 如申請專利範圍第1項所述之組成物,係進一步包含3-1000 國際單位(IU)的維他命E。 3. 如申請專利範圍第1項所述之組成物,其係進一步包含輔酶 Q10、黃豆類黃酮素、牛磺酸、甜菜果膠纖維或銀杏萃取物。 4. 如申請專利範圍第2項所述之組成物,係進一步包含輔酶 、黃豆類黃酮素、牛磺酸、甜菜果膠纖維或銀杏萃取物。 5. 如申請專利範圍第1項所述之組成物,其中前述組成物係為乾 燥形式。 G 6. 如申請專利範圍第2項所述之組成物,其中前述組成物係為乾 燥形式。 7‘ 專利範圍第3項所述之組成物,其中前述組成物係為乾 8.專利範圍第4項所述之組成物,其中前述組成物係為乾 9· ^申請專利範㈣丨項所述之組成物,其中前述組成物 10 Γ由ΐ水、果汁、牛奶、咖啡、餅乾、麥片、巧克力或點心棒。 .二申凊專利範圍帛2項所述之組成物,其中前述組成物係為 余、4水、果汁、牛奶、咖啡、餅乾、麥片、巧克力或點心棒: =申請專利範圍帛3項所述之組成物,其中前述紅成物^為 余、汽水、果汁、牛奶、咖啡、餅乾、麥片、巧克力或點心棒’’’’。 12·=申請專利範圍帛4項所述之組成物,其中前述組成物^為 余、弋水、果汁、牛奶、咖啡、餅乾、麥片、巧克力或點心棒 13.如申請專利範圍第丨項所述之組成物,其中前述組成物包含— 水溶液。 S — 15
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- 2003-10-23 JP JP2004547143A patent/JP2006503896A/ja active Pending
-
2006
- 2006-06-14 HK HK06106781A patent/HK1086725A1/xx not_active IP Right Cessation
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2011
- 2011-03-09 JP JP2011052092A patent/JP2011157366A/ja active Pending
Also Published As
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CA2503363A1 (en) | 2004-05-06 |
JP2011157366A (ja) | 2011-08-18 |
AU2003282829B2 (en) | 2010-07-22 |
NZ540165A (en) | 2008-10-31 |
EP1562447B1 (en) | 2008-12-10 |
DE60325265D1 (de) | 2009-01-22 |
PT1562447E (pt) | 2009-03-17 |
EP1562447A4 (en) | 2006-04-12 |
EP1562449A4 (en) | 2008-02-20 |
TW200412863A (en) | 2004-08-01 |
DK1562449T3 (da) | 2011-06-06 |
EP1562449B1 (en) | 2011-03-09 |
AU2003282829A1 (en) | 2004-05-13 |
TWI383753B (zh) | 2013-02-01 |
ES2322577T3 (es) | 2009-06-23 |
TW200409601A (en) | 2004-06-16 |
JP2006503896A (ja) | 2006-02-02 |
DK1562447T3 (da) | 2009-04-06 |
CA2503373A1 (en) | 2004-05-06 |
KR20050088994A (ko) | 2005-09-07 |
KR101186898B1 (ko) | 2012-10-02 |
EP1562447A1 (en) | 2005-08-17 |
CA2503373C (en) | 2013-01-15 |
ATE500747T1 (de) | 2011-03-15 |
EP1562449A1 (en) | 2005-08-17 |
HK1086725A1 (en) | 2006-09-29 |
DE60336336D1 (de) | 2011-04-21 |
ATE416629T1 (de) | 2008-12-15 |
KR20050103268A (ko) | 2005-10-28 |
JP2006507283A (ja) | 2006-03-02 |
PT1562449E (pt) | 2011-06-16 |
CA2503363C (en) | 2012-01-17 |
AU2003284919A1 (en) | 2004-05-13 |
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