TW200403986A - A composition including isoflavones refined from plant - Google Patents

A composition including isoflavones refined from plant Download PDF

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TW200403986A
TW200403986A TW92132089A TW92132089A TW200403986A TW 200403986 A TW200403986 A TW 200403986A TW 92132089 A TW92132089 A TW 92132089A TW 92132089 A TW92132089 A TW 92132089A TW 200403986 A TW200403986 A TW 200403986A
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TWI260205B (en
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Mark Empie
Eric Gugger
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Archer Daniels Midland Co
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Abstract

A composition is prepared by extracting phytochemicals from plant matter. This composition is enriched preferably in isoflavones, lignans, saponins, catechins and phenolic acids. Soy is the preferred source of these chemicals; however, other plants may also be used, such as red clover, kudzu, flax, and cocoa. The composition is a dietary supplement for treatment of various cancers, pre-and post-menstrual syndromes, and various other disorders.

Description

200403986 五、發明說明(1) 此一正式申請乃取代1997年(民國八十六年)十月二曰 第6 0 / 0 6 0,5 4 9號之臨時性申請。 本發明係有關於植物萃取物,尤其關於植物化學物 質,包括:植物皂素配質、植物皂素、兒茶酸、木素糖、 酚酸與異黃酮;尤其是萃取自大豆、亞麻、茶、可可等類 植物;以及利用此類組合物作為營養補充品或食物添加濟 之方法。200403986 V. Description of Invention (1) This formal application replaces the provisional application No. 60/0 6 0, 5 4 9 of October 1997 (Republic of China). The invention relates to plant extracts, in particular to phytochemicals, including: phytosaponin, phytosaponin, catechin, lignose, phenolic acid and isoflavones; especially extracted from soybean, flax, tea , Cocoa and other plants; and methods for using such compositions as nutritional supplements or food supplements.

眾人皆知植物物質含有數類低分子量之有機化合物, 其在各類動物中具生物活性。傳統上,此類化合物被認為 不具養分,但近來科學證據顯示這些物質在健康維護上, 在化學預防上及在減輕與性賀爾蒙循環有關之一些情狀或 疾病包括睡眠失調及陰道乾躁症上可扮演重要之角色。 一般飲食中之食用植物或作為草藥療法/補充的物質品 皆可能含結構相關的化合物。與其他植物相比較,這些相 關物質往往在量質與分布上均較特殊。此類具生物活性之 化合物最有名為類黃酮、異黃酮、植物皂素、木素糖、生 物鹼、兒茶酸與酚酸。It is well known that plant matter contains several types of low molecular weight organic compounds that are biologically active in all types of animals. Traditionally, such compounds have been considered non-nutritional, but recent scientific evidence indicates that these substances are used for health maintenance, chemoprevention, and alleviation of some conditions or diseases related to the sex hormone cycle including sleep disorders and vaginal dryness Can play an important role. Edible plants in the general diet or substances used as herbal remedies / supplements may contain structurally related compounds. Compared with other plants, these related substances are often special in terms of quality and distribution. These biologically active compounds are best known as flavonoids, isoflavones, phytosaponins, xylose, alkaloids, catechins and phenolic acids.

流行病學研究與疾病有關之飲食發現若干飲食中所含 之成份,可以降低人類感染某些疾病之風險。東方人食用 大豆可以降低罹患乳癌、列腺癌、結腸癌及冠狀心臟病; 而芬蘭人罹患列腺癌比例也已下降。研究者目前正針對飲 食中特定組合物進行研究,以了解上述流行病學觀察結 果。 在飲食中食用之各種植物,有數種是含有豐富之植物Epidemiological studies of disease-related diets have identified certain dietary ingredients that can reduce the risk of human infection with certain diseases. Orientals eating soy can reduce breast cancer, prostate cancer, colon cancer, and coronary heart disease; Finns also have a lower incidence of prostate cancer. Researchers are currently investigating specific compositions in food to understand the epidemiological observations. A variety of plants eaten in the diet, several are rich in plants

第6頁 200403986 五、發明說明(2) 化=物。大旦製品含有高量之異黃酮及植 ^食用穀物,如:大麥,psyllium、稻^息素。非精製 3木素糖。可可含兒茶酸及酚酸。某此二亞廚「燕麥則Page 6 200403986 V. Description of the invention (2) Chemical = thing. Da Dan products contain high amounts of isoflavones and plant food grains, such as: barley, psyllium, and rice. Unrefined 3 xylose. Cocoa contains catechin and phenolic acids. So these two Asian chefs

I :化學分子之來源,如:葛類植物之c亦為此 糖與異黃酮。木素糖與異黃酮可作為 二目宿中含木素 1。茶類植物亦含有豐富的植物化學物:J激素的物 酸。 3 包括兒茶酸及酚 單獨使用異黃g同可治療或預防乳 與結腸痔戋作為嫌別… :应、Μ腺癌、皮膚癌 勝尼A作為機制抑制物。單獨使 預防盥芦M tH扣~ ^共育_也可降低或I: The source of chemical molecules, such as c of kudzu plants, sugars and isoflavones. Lignose and isoflavones can be used as lignin in binocular. Tea plants are also rich in phytochemicals: J hormones and acids. 3 Includes catechin and phenol. The use of isoflavone g alone can treat or prevent milk and colon hemorrhoids as a suspect ...: Ying, M adenocarcinoma, skin cancer, Sini A as a mechanism inhibitor. Separate use of preventive toilet M tH buckle ~ ^ co-cultivation _ can also reduce or

防與彳τ經期開始及期間有關的各類徵候 J ^ 發熱(hot Hashes)及骨質疏鬆症。里、廿群,匕括陣發Prevention of various symptoms related to the beginning and duration of the 彳 τ menstrual period J ^ hot Hashes and osteoporosis. Li, 廿 群, dagger burst

Si括心Ϊ病之特定心臟病血管應用上,降低膽固醇-月曰,里,調整血管生成,及其他血管上的效果。甚至於, -汽S同單獨使用連帶能減少頭痛、癡呆症、發炎及齡酒 症’同時也能增強免疫性。Si encompasses heart disease in specific vascular applications, which lowers cholesterol-month, month, month, and month, regulates angiogenesis, and other blood vessel effects. Furthermore, the use of -S together with S-S alone can reduce headache, dementia, inflammation, and aging alcohol 'while also enhancing immunity.

單獨使用木素糖也能預防或治療乳癌、列腺癌及結腸 癌,同時也能減少陣發性發熱,預防骨質疏鬆症及顯示有 抗過濾性病毒能力,木素糖也能抵抗細胞有絲分裂及具殺 菌功效,一種植物木素糖叫鄰苯二酚-二氫癒創木酸曾被食 品工業當作抗氧化劑使用。 單獨使用植物皂素能預防或治療皮膚癌,結腸癌,減 少血中膽固醇,及能增強免疫性及具抗病毒活性。植物皂 素同時顯示具抗氧化劑效果及可當作自由基清道夫。 驗酸已顯示具抗氧化活性。Lignin alone can also prevent or treat breast cancer, prostate cancer, and colon cancer. It can also reduce paroxysmal fever, prevent osteoporosis, and show resistance to filter viruses. Lignin can also resist cell mitosis and With bactericidal effect, a plant xylose called catechol-dihydroguaiaretic acid has been used as an antioxidant by the food industry. Phytosaponin alone can prevent or treat skin cancer, colon cancer, reduce blood cholesterol, and enhance immunity and antiviral activity. Phytosaponins also show antioxidant effects and can act as free radical scavengers. Acid tests have shown antioxidant activity.

第7頁 200403986 I五、發明說明(3) -Page 7 200403986 I. Explanation of the Invention (3)-

I | 食用高大豆含量之人’可減少許多上述各類徵候群。^ 此顯示食用如發現於大豆中含一定比例之植物化學物丨 合物之飲食可能導致附加的或協力效用。然而,高大豆含 I 量飲食對西方消費者有些不良作用,如:胃腸氣脹、不良丨 味覺及遲疑,而改變其生活型態將大豆納入飲食中,即使I 為了這些益處。 目前所知,屬異環狀酚類異黃酮包括:大豆類化合物 5,7,4-三羥基異黃酮(2611丨51:丨11)、黃豆贰((1&1(12111)、 甘氨酸素(glycitein)、雞豆黃素A (biochanin Α)、牛 尿紛(equol)、芒柄花黃素(formononetin)、去甲安哥 拉紫檀素(o-desmethylangolensin)與自然衍生物。當這 些化合物被食用時,這些化合物以及糖贷其配基或去甲基 糖苷配基化合物,如5,7,4 -三羥基異黃酮(或染料木配 質),與黃豆甘原,皆具類似活性。而其有時被稱為植物 雌激素。 木素糖定義為含2, 3 -二芊基丁烷構造之化合物。其包· 括:羅漢松脂素(m a t a i r e s i η ο 1 )、閉異落葉松脂素 (secoisolariciresinol )、落葉松脂素 (lariciresinol)、異落葉松脂素 (isolariciresinol )、去甲二氫愈創木酸 (nordihydroguaiaretic acid)-松脂醇 (pinoresinol)、橄欖樹脂素(〇iivn)與其他可能是腸i 内酯及腸二醇之前趨物與變異物,其_包括雙糠苷。 紛酸包括對-氫苯酸(p-hydrobenzoic acid)、原兒I | People who eat high soy content ’can reduce many of these types of symptoms. ^ This shows that eating a diet containing a certain proportion of phytochemicals 丨 compounds found in soybeans may lead to additional or synergistic effects. However, high-soy diets have some adverse effects on Western consumers, such as gastrointestinal flatulence, bad taste, and hesitation, and they have changed their lifestyles to include soy in their diets, even if they are for these benefits. Currently known, isoflavones which are isocyclic phenols include: soybean compounds 5,7,4-trihydroxy isoflavones (2611 丨 51: 丨 11), soy bean syrup ((1 & 1 (12111), glycin glycitein, biochanin A, equiol, formononetin, o-desmethylangolensin and natural derivatives. When these compounds are consumed These compounds, as well as sugar aglycones or demethyl aglycone compounds, such as 5,7,4-trihydroxy isoflavones (or genistein), have similar activity to soy glycogen. And they have It is called phytoestrogens. Xylose is defined as a compound containing 2, 3 -difluorenyl butane structure. It includes: mathansi (matairesi η ο 1), secoisolariciresinol , Lariciresinol, isolariciresinol, nordihydroguaiaretic acid-pinoresinol, olivn and other possible enteric lactones And intestinal glycol precursors and mutations ., _ Which comprises a double-furoic acid glycosides include Fun - hydrogen benzoic acid (p-hydrobenzoic acid), the original child

第8頁 200403986 五、發明說明(4) .Page 8 200403986 V. Description of Invention (4).

茶酸(protocatechuic acid)及香草酸(vanillic acid)。其他紛酸尚有綠原酸(chlorogenic acid)、咖 啡酸(caffeic acid)、阿魏酸(ferulic acid)、沒食 子酸(gallic acid)、芬子酸(sinapic acid) 、丁香酸 (syringic acid )、香豆酸(coumar i c ac i d )、肉桂酸 (cinnamic acid)、龍膽酸(gen t i s i c acid)、水楊酸 (salicylic acid)、羥苯甲酸(hydroxy benzoic acid)、羥苯乙酸(hydroxy phenyl acetic acids)及其 衍生物。酚酸類物質尚應涵蓋來自天然蔬果中之各種同分 異構物及衍生物。 兒茶酸或黃烷醇包括··表沒食子兒茶酸 (epigallocatechin)、兒茶酸(catechin)、表兒茶酸 (epicatechin)與沒食子兒茶酸(gallocatechin)。Protocatechuic acid and vanillic acid. Other acids are chlorogenic acid, caffeic acid, ferulic acid, gallic acid, sinapic acid, syringic acid ), Coumar ic ac id, cinnamic acid, gen tisic acid, salicylic acid, hydroxy benzoic acid, hydroxybenzoic acid phenyl acetic acids) and its derivatives. Phenolic acids should also cover various isomers and derivatives from natural fruits and vegetables. Catechin or flavanols include: epigallocatechin, catechin, epicatechin, and gallocatechin.

皂化物為含2 7個碳(C - 2 7 )之類固醇,其支鏈經代謝 產生螺旋縮酮。自然生成之皂化物為植物皂素,其為類固 醇或三萜為主體之3-0 -葡萄糖苷。毛地黃中之毛地黃皂甘 為植物皂素。植物皂素包括:皂甘配基之糖苷如三類祐或 類固醇;及醣類如葡萄糖、阿拉伯糖、半乳糖、葡萄醛 酸。典型之豆科植物皂素為:異白!菌(Glycyrrhiza glabra)之干草皂甘(甘草次酸(giyCyrrhetinic acid) +葡萄駿酸(glucuronic acid)),大豆中之大豆皂素以 及苜蓿(Medicago sativa)中之苜蓿植物皂素 (alfalfasaponin)。植物皂素尚含已被認定三萜類酚之 丨化學實體,如:蕃茄素(tom atine)、大豆皂甘配基酚 200403986 五、發明說明(5) ^ A,B,C,D,E及F ( soyasapogeno 1 s A,B,C,D,E and F),人Saponification is a steroid containing 27 carbons (C-2 7), and its branched chain is metabolized to produce a spiral ketal. The naturally occurring saponin is phytosaponin, which is a 3-0-glucoside with steroids or triterpenes as the main component. Digitalis saponin in foxglove is plant saponin. Phytosaponins include: saponin glycosides such as three types of steroids or steroids; and sugars such as glucose, arabinose, galactose, and uronic acid. The typical leguminous saponin is: Isobaric! Glycyrrhiza glabra, hay soap glycyrrhizin (giyCyrrhetinic acid + glucuronic acid), soy saponin in soybean, and alfalfa phytosaponin (alfalfasaponin) in Medica sativa. Phytosaponins still contain chemical entities that have been identified as triterpenoids, such as: tom atine, soybean saponin phenol 200302986 V. Description of the invention (5) ^ A, B, C, D, E And F (soyasapogeno 1 s A, B, C, D, E and F), people

I * I 丨蔘皂甘部分 3與 4 (ginsengoside fraction 3 and 4),苜 丨蓿内酸(medicagenic acid)、常春配基 I ( hederagenin)、干草息甘(glycyrrhi z i nI * I 丨 sensengoside fractions 3 and 4, alfalfa 丨 Medicagenic acid, hederagenin I, glycyrrhi z i n

I digitonin)、毛地黃皂甘(quillaj a saponin)、皂樹酸 (lucernic acid)、紫苜稽酸(zahnic acid)。植物中 所含之上述各種化合物之自然改變物亦包括於此認定。 所需之改良組合物,其成分大體包括異黃酮、木素 糖、皂化物、植物皂素、及/或酚酸,其將產生較服用單一 物質更佳之效果。此外,需要較天然成分濃度富含更高之鲁 有效植物化學物質之組合物。此允許個人方便食用這類植 物化學物作為營養補充劑或食物添加劑。 本發明之目的在於提供一般大眾一個方便方式異黃 酮、木素糖、植物皂素、兒茶酸、及/或酚酸,作為營養補 充攝取劑或傳統食物成分。 本發明之另一目的為提供最佳之植物化學物萃取組合 物予消費者,遞送足夠的濃度以易於服用如:丸狀、片 狀、膠囊狀、液體或為食物之成分。 本發明之再另一目的為將植物化學萃取物製備成可局 部使用之乳霜或乳液。在此形式,異黃酮、木素糖、植物鲁 皂素、兒茶酸及/或酚酸懸浮於一適當液體或凝膠體中以提 供一安定之乳霜或乳液以供使用。 I 本發明之又另一目的為提供一萃取物濃度,其化學組|I digitonin), quillaj a saponin, lucernic acid, zahnic acid. Natural modifications of the above-mentioned compounds contained in plants are also included herein. The required improved composition, which generally includes isoflavones, xylose, saponification, phytosaponin, and / or phenolic acids, will produce a better effect than taking a single substance. In addition, there is a need for a composition that is richer in effective phytochemicals than natural ingredient concentrations. This allows individuals to easily consume such plant chemicals as a nutritional supplement or food additive. The object of the present invention is to provide a convenient way for the general public to provide isoflavones, xylose, phytosaponins, catechins, and / or phenolic acids as nutritional supplements or traditional food ingredients. Another object of the present invention is to provide the optimal phytochemical extract composition to consumers, and deliver sufficient concentration for easy taking such as: pills, tablets, capsules, liquids or food ingredients. Yet another object of the present invention is to prepare a phytochemical extract as a cream or lotion for local use. In this form, isoflavones, xylose, phytolusin, catechin and / or phenolic acid are suspended in a suitable liquid or gel to provide a stable cream or lotion for use. I Yet another object of the present invention is to provide an extract concentration, its chemical group |

i成與自然植物所發現之化學物質極為相近。 IIt is very similar to the chemicals found in natural plants. I

第10頁 200403986 五、發明說明(6) 秉持上述發明構想,異黃酮、木素糖、植物皂素、兒 茶酸及/或酚酸均自適當植物中萃取出,以提供一較天然物 質濃度更高之組成物,且其中一種或多種生物活性物質較 天然物質高出五倍。 本萃取物可單獨使用或與一種或多種其他植物萃取物 合併使用以產生最佳組合。此外,本萃取組合物可與一種 或多種營養劑組合,如··維他命、礦物質、氨基酸等,以 提供一最佳化營養補充劑可促成所欲之健康效果。Page 10 200303986 V. Description of the invention (6) In keeping with the above-mentioned invention concept, isoflavones, xylose, phytosaponin, catechin and / or phenolic acids are all extracted from appropriate plants to provide a more natural substance concentration Higher composition, and one or more of the biologically active substances are five times higher than natural substances. This extract can be used alone or in combination with one or more other plant extracts to produce the optimal combination. In addition, the extract composition can be combined with one or more nutritional agents, such as vitamins, minerals, amino acids, etc., to provide an optimized nutritional supplement that can promote desired health effects.

以上所有之成分皆可與必要之接合劑、賦形劑、防腐 劑、色素以及其他工業上常用物質,以生產適當之藥片、 膠囊、藥丸、液體、乳霜、粉末或食物成分。 這些植物化學物可以補充劑及食物成分工業之所熟知 方法包裝供給。這些物質主要在提供健康及福祉。All of the above ingredients can be combined with the necessary binders, excipients, preservatives, pigments and other substances commonly used in the industry to produce appropriate tablets, capsules, pills, liquids, creams, powders or food ingredients. These phytochemicals can be packaged and supplied in a manner well known in the supplement and food ingredient industries. These substances are primarily intended to provide health and well-being.

本改良組合物可經由含高量異黃酮、木素糖及其他植 物化學物如去脂大豆片、大豆糖蜜、大豆乳漿、紅苜罃、 苜蓿、亞麻、可可、茶或葛根分餾取得。這些均可單獨分 德或與其他已知含高量異黃酮、木素糖、植物皂素、兒茶 酸與酚酸之植物一起分餾。分餾結果從來源物質中移除大 量之水、碳水化合物、蛋白質與脂肪。此分餾方法較佳為 揭露在同時審理中之美國專利第5, 702, 752號或美國專利第 4,428,876號,或乙酸乙S旨或η -丁 S?·之萃取法。美國專利第 5, 702, 752號讓渡於本發明之受讓人。 可單獨或合併應用之其他萃取方法包括溶解度差異 法、蒸德法、溶劑萃取法、吸附法、分子量差異過慮法及The improved composition can be obtained by fractional distillation containing high amounts of isoflavones, xylose and other phytochemicals such as defatted soybean flakes, soybean molasses, soybean milk, red clover, alfalfa, flax, cocoa, tea, or pueraria. These can be fractionated separately or fractionated with other plants known to be high in isoflavones, xylose, phytosaponins, catechins and phenolic acids. Fractionation results remove large amounts of water, carbohydrates, proteins, and fats from the source material. This fractionation method is preferably an extraction method disclosed in U.S. Patent No. 5,702,752 or U.S. Patent No. 4,428,876, or ethyl acetate or η-butyl S? U.S. Patent No. 5,702,752 is assigned to the assignee of the present invention. Other extraction methods that can be used individually or in combination include the solubility difference method, steam distillation method, solvent extraction method, adsorption method, molecular weight difference method, and

第11頁 200403986 I五、發明說明(7) 沉澱法。 較佳之組合物為已知之商業化產品之改良品,主要是 其每克所含植物化學物之量與影響生理功能之不同植物化 學物質的量。 這些天然物質乃長期被食用,且尤其有關於對健康助 益之攝取物質,其提供了傳染病學上的證據。此外,其它 好處得自於物理性質已改進之相關植物化學物,而此類植 物化學物乃源自其原始食物來源。 所得之組合物較佳者為包括5-95%之異黃3同、0-70%Page 11 200403986 I. Explanation of the invention (7) Precipitation method. The preferred composition is an improvement on a known commercial product, mainly the amount of phytochemicals per gram and the amount of different plant chemical substances that affect physiological functions. These natural substances have been eaten for a long time, and in particular they are related to the intake of health benefits, which provide infectious disease evidence. In addition, other benefits are derived from related phytochemicals whose physical properties have been improved, and such phytochemicals are derived from their original food source. The obtained composition preferably includes 5-95% of iso-yellow, 3%, 0-70%

木素糖、2 - 7 0 %的皂化物及植物皂素。另一較佳形式為萃 取自大豆。另一較佳形式為該組合物包括(植物皂素+皂化 物)對異黃酮之比為1 : 1 0 0到1 0 0 : 1之間,其中異黃酮主 要5, 7, 4 -三羥基異黃酮之天然衍生物與/或其前趨物雞豆黃 素A及黃豆苷原與/或其前趨物芒柄花黃素所組成,而 5,7,4 -三羥基異黃酮衍生物對黃豆甘原衍生物之比在1 0 0 ·· 1到1 : 1 0 0之間。較佳地,異黃酮主要為糖基衍生物。Lignin, 2-70% saponin and phytosaponin. Another preferred form is from soybeans. Another preferred form is that the composition includes a ratio of (phytosaponin + saponification) to isoflavones between 1: 100 and 100: 1, wherein the isoflavones are mainly 5, 7, 4-trihydroxy Isoflavone natural derivatives and / or its progenitors chitosan A and daidzein and / or its precursors formononetin, and 5,7,4-trihydroxy isoflavone The ratio to the soybean bean glycogen derivative is between 1 0 0 · · 1 to 1: 1 0 0. Preferably, the isoflavones are mainly glycosyl derivatives.

此組合物之比率可很容易的經由改變植物來源或結合 萃取植物來源而有所變動。故進一步研究顯示不同植物化 學之結合對某些健康狀況更為有效,而此特定之組合物亦 將有所改變。 目前已知異黃嗣、木素糖與植物皂素對治療或預防各 類癌症極有助益,其中包括乳癌、列腺癌、皮膚癌與結腸 丨癌。 ! 一般確信此改良組合物可以化學預防之方式提供極大The ratio of this composition can be easily changed by changing the plant source or combining extracted plant sources. Therefore, further research shows that the combination of different phytochemicals is more effective for certain health conditions, and this particular composition will also change. Isoflavone, xylose and phytosaponin are known to be extremely helpful in the treatment or prevention of various types of cancer, including breast cancer, prostate cancer, skin cancer and colon cancer. ! It is generally believed that this improved composition can provide great benefits in a chemopreventive manner

第12頁 200403986 I五、發明說明(8) ^ 助益。而最近之實驗亦證實此一信念。 _ 範例一 進行一系列之初步動物實驗以了解食用大豆製品對皮 下植入LNCaP之SCI D雄鼠生長之影響。高異黃酮含量之大豆 蛋白分離物(SPI) (2毫克異黃酮/公克SPI)由美國密蘇 里州之國際蛋白技術公司(Protein Technology International)提供。一種大立植物化學萃取物為含有 28.5%之大豆異黃酮及不同量之其它大豆植物化合物之大 豆植物化學濃縮物(SPC),由美國伊利諾州之Archer Daniels Midland公司提供。這些物質用於製備六組實驗食 物。表一顯示食物的成分。 8週大的S C I D雄鼠,在其腹側以皮下植入方式注入 2 X1 0 6取自寄主之LNC aP細胞,隨機將雄鼠分成六組(n = 1 ^ 並各配予一組實驗食物,測定食物攝取量、體重與腫瘤 積。實驗結束時,收集血液樣本,分離出血清進行p $八-析。腫瘤組織之一部分以福馬林固定,並以石蠟包壇、〃刀 成4 m ra以對〉周亡細胞(a ρ ο p t 〇 t i c c e 1 1 )作原位、纟且織化、刀 定並進行血管生成與繁殖之免疫組織化學分析。敌 學蜊 /、部八 則製備成細胞溶解液以進行西方轉印法決定凋亡相 刀 產物。 基因 表一整理出大豆製品對食物攝取、體重、異黃 與腫瘤之影響。大豆製品對食物攝取或體重並無_荽攝玉 變。與絡蛋白質银食之控制組相比,給予處理sp厂改 (20〇/〇 ) 、SPC ( 1· 〇% )及 SPI 和 spc ( h 〇0/〇 )之白Page 12 200403986 I V. Description of the invention (8) ^ Assistance. And recent experiments have confirmed this belief. _ Example 1 A series of preliminary animal experiments were performed to understand the effects of edible soy products on the growth of SCI D male rats implanted subcutaneously with LNCaP. High Isoflavone Content Soy Protein Isolate (SPI) (2 mg isoflavone / g SPI) was provided by Protein Technology International, Missouri, USA. A Dahli phytochemical extract is a soybean phytochemical concentrate (SPC) containing 28.5% soy isoflavones and various amounts of other soybean plant compounds, and is provided by Archer Daniels Midland Company of Illinois, USA. These materials were used to prepare six groups of experimental foods. Table 1 shows the composition of the food. Male 8-week-old SCID rats were injected subcutaneously with 2 X 1 0 6 LNC aP cells taken from the host, and the male rats were randomly divided into six groups (n = 1 ^ and each was given a set of experimental food) At the end of the experiment, blood samples were collected, and serum was isolated for p-eight analysis. One part of the tumor tissue was fixed with formalin, and paraffin coated altar and trowel were used to form 4 m ra Immunohistochemical analysis of> Zhou Zhou cells (a ρ ο pt 〇ticce 1 1) in situ, sacrifice and weaving, knife set and angiogenesis and reproduction. Enemy clams, and Buba were prepared into cells The solution was used for western transfer to determine the apoptotic phase-knife product. Gene Table 1 sorted out the effects of soybean products on food intake, body weight, yellowing, and tumors. Soy products did not affect food intake or body weight. Compared with the control group of protein protein and silver food, the treatments were treated with sp factory modification (200 / 〇), SPC (1.0%), and SPI and spc (h 〇0 / 〇).

第13頁 200403986 I五、發明說明(9) " --~ 丨量分別減少 12% 、28% (ρ<〇·04)及 4〇% (p<〇 〇〇5)。分 丨析結果顯示蛋白質來源對腫瘤生長無顯著影響,線性回歸-I分析顯示腫瘤量與飲食中異黃酮量成反比(腫瘤量(立方 丨公分)--〇·〇〇〇8 + 2·121χ異黃自同(毫克),r2 = q 76,p <0· 03 ) 〇 表三則顯示s p c控制在1 · 〇 %飲食對細胞凋亡程序、增 瘦、血官新生之影響。其顯示大豆植物化學物之食品添加 劑可以促進癌細胞〉周亡和抑制腫瘤細胞之增殖來抑制在活 體内生長之LNCaP腫瘤。其對腫瘤血管新生之抑制效果並不 明顯,可能是因為樣品數太小(n = 2 )。 試管實驗顯示5,7,4 -三羥基異黃酮與大豆植物化學濃 縮物可抑制LNCaP細胞分泌PSA至介質中。以25及50mm之 5,7,4 -三羥基異黃酮處理時,P S A之濃度可分別減少6 8 °/。與 74% ;而以25及50mm之大豆植物化學濃縮物處理時,PSA可 分別降低31%及42% 。Page 13 200403986 I V. Description of the invention (9) "-~ The amount of reduction is 12%, 28% (ρ < 0.04) and 40% (p < 〇〇〇05). The analysis results showed that the protein source had no significant effect on tumor growth. Linear regression-I analysis showed that the amount of tumor was inversely proportional to the amount of isoflavones in the diet (tumor volume (cubic 丨 cm)-〇〇〇〇〇 + 2.121χ Isoflavones (mg), r2 = q 76, p < 0.03) 〇 Table 3 shows the effect of spc control at 1.0% diet on apoptosis, weight loss, and blood regeneration. It shows that food additives of soybean phytochemicals can promote cancer cell death and inhibit tumor cell proliferation to inhibit LNCaP tumors growing in vivo. Its inhibitory effect on tumor angiogenesis is not obvious, probably because the number of samples is too small (n = 2). Test tube experiments have shown that 5,7,4-trihydroxy isoflavones and soybean phytochemical concentrates can inhibit PSA secretion by LNCaP cells into the medium. When treated with 5,7,4-trihydroxy isoflavones at 25 and 50 mm, the P S A concentration can be reduced by 6 8 ° /. And 74%; and when treated with 25 and 50mm soybean phytochemical concentrates, PSA can be reduced by 31% and 42%, respectively.

第14頁 200403986 三、發明說明no ) 表一 實驗食物成份(:公克) 配万1 酪蛋白質 配万2 SPI 配方3 酪蛋白質 /LSPC 配万4 SPI/LSPC 配方5 酪蛋白質 /HSPC 配万6 SPI/HSPC SPI 0 200 0 200 0 200 酪蛋白質 200 0 200 0 200 0 DL-申硫胺酸 〇 3 3 3 η 3 玉米澱粉 150 150 150 150 150 150 蔗糖 500 500 500 500 500 500 纖維素,BW200 50 50 50 50 50 50 玉米油 50 50 50 50 50 50 礦物質混合物, S10001 35 35 35 35 35 35 維他命混合物, V10001 10 10 10 10 10 10 二酒石酸膽鹼 2 2 2 2 2 2 大豆植物化合物 0 0 2 2 10 10 總計(公克) 1000 1000 1002 1002 1010 1010 (異黃酮,毫克/公 斤食物) 0 245 341 586 705 950Page 14 200303986 III. Description of the invention no) Table 1. Experimental food ingredients (: grams) with 1 casein with 2 SPI formula 3 casein / LSPC with 4 SPI / LSPC formula 5 casein / HSPC with 6 SPI / HSPC SPI 0 200 0 200 0 200 200 Casein 200 0 200 0 200 0 0 DL-Synthetic acid 03 3 3 η 3 Corn starch 150 150 150 150 150 150 Sucrose 500 500 500 500 500 500 Cellulose, BW200 50 50 50 50 50 50 Corn oil 50 50 50 50 50 50 50 Mineral mixture, S10001 35 35 35 35 35 35 Vitamin mixture, V10001 10 10 10 10 10 10 Choline ditartrate 2 2 2 2 2 2 Soy plant compounds 0 0 2 2 10 10 Total (g) 1000 1000 1002 1002 1010 1010 (Isoflavones, mg / kg food) 0 245 341 586 705 950

1 ·· Dr.E.A.Ulman Research Diets, Inc·自 AIN 公式微幅 修改1 ·· Dr.E.A.Ulman Research Diets, Inc · Slightly modified from AIN formula

第15頁 200403986 五、發明說明(11) 表二 最終體重、總食物攝取量、總異黃酮攝取量及腫 瘤體積 ΤΓΠ 體重 食物攝取量 公克/公尺 總異黃酮量 腫瘤體積 (立方公分) 酪蛋白質 22.4土0.5丨 46.6士3.‘ 0.00士0.00 2.32±0.3Γ SPI 23.1士0·7 46.2土2.8 17.(30土 6.37 2.06^0.32 酪蛋白質 /LSPC 21.牡0.7 41.2土3.4 14.03 土 14 1·88土0.35 SPI/LSPC 22.6士0.6 50.1Μ.7 29.36士2.76 1.66士0.29‘ 酪蛋白質 /HSPC 22_2士0.7 44.8土6.1 76·38土10.40 1.6牡0.22‘ SPI/HSPC 22.0土0.6 47.5 土 1.7 92.53土3.22 1.39土0.30“Page 15 200303986 V. Description of the invention (11) Table 2 Final weight, total food intake, total isoflavone intake and tumor volume ΤΓΠ weight food intake g / m total isoflavone volume tumor volume (cm3) casein 22.4 soil 0.5 丨 46.6 ± 3. '0.00 ± 0.00 2.32 ± 0.3Γ SPI 23.1 ± 0 · 7 46.2 ± 2.8 1.7 (30 ± 6.37 2.06 ^ 0.32 casein / LSPC 21.U 0.7 41.2 ± 3.4 14.03 ± 14 1 · 88 soil 0.35 SPI / LSPC 22.6 people 0.6 50.1M.7 29.36 people 2.76 1.66 people 0.29 'casein / HSPC 22_2 people 0.7 44.8 people 6.1 76 · 38 people 10.40 1.6 0.22' SPI / HSPC 22.0 people 0.6 47.5 people 1.7 92.53 people 3.22 1.39 dirt 0.30 "

丨2:數值為平均值I標準差-代表對於食物攝取或體重並無 I顯著影響。 丨3 :與控制組比較,SPI/LSPC、酪蛋白質/ HSPC及SPI/HSPC |顯著具有較小腫瘤體積(*:Ρ<0·04;**: PC0.005) 丨表三對眉亡指標(人1,%1^心1)、繁殖指標(?1,%?€以丨 2: The value is the average I standard deviation-it means that there is no significant effect on food intake or body weight.丨 3: Compared with the control group, SPI / LSPC, casein / HSPC and SPI / HSPC | Significantly smaller tumor volume (*: P < 0 · 04; **: PC0.005) 丨 Table 3 pairs of eyebrow death indicators (Person 1,% 1 ^ heart 1), reproduction index (? 1,%?)

處理 AI (% TUNEL) PI (% PCNA ) 微血管密度 控制組(n=2) 6.07土0.88 60.1士1.1 12.5 士 3.8 酪蛋白質 /HSPC(n=2) 10.75士0.54 51.7士1.3 9.7 土〇·7 P値 <0.02 <0.01 >0.05Treatment AI (% TUNEL) PI (% PCNA) Microvessel density control group (n = 2) 6.07 ± 0.88 60.1 ± 1.1 12.5 ± 3.8 Casein / HSPC (n = 2) 10.75 ± 0.54 51.7 ± 1.3 9.7 ± 0.7 P値 < 0.02 < 0.01 > 0.05

落16 I 200403986 五、發明說明(12) . 數值以平均值±標準差 總而言之,初步結果顯示大豆製品可抑制SC I D雄鼠中_ LNCaP腫瘤之皮下生長,可能是因為誘引細胞凋亡程序,同 時抑制血管新生與增殖。 異黃酮或木素糖可減輕停經期有關的徵候群,如陣發 性發熱與骨質疏鬆症,同時減輕月經期間引起之症狀。而 其進一步推論是由於雌性激素的活性。故此文中所描述之 改良組合物應對這些症狀之減輕更為有效。 又,異黃酮對心臟血管相關症狀亦有正面影響,如心 臟疾病、膽固醇(植物皂素亦對膽固醇有正面影響)、血 管新生與其他血管症狀。相信改良之組合物可同迄今所知 方法一樣減少心臟血管疾病但花費卻較低。 如前所述,已知異黃酮、木素糖與植物皂素個別對神 經及免疫症狀均有正面影響,相信改良之組合物將會減輕 神經和免疫症狀,與迄今所知方法應有相同功效,但花費 卻較低。此外,可期待此文中描述之組合產生協助作用。 口服或注射或非口服方式服用改良之組合物,例如皮 下注射、靜脈内注射、肌肉注射、腹膜内注射,或以鼻内 滴入或以喷霧方式喷至黏膜組織,或以軟膏或乳霜方式塗 抹於皮膚。 可以固態或液態方式之任何適合媒介服用改良之組合 |物,如錠劑、膠囊、粉末、軟膠、液體、懸浮液、乳化 丨劑、軟膏或乳液方式攝取。該改良組合物亦可以食物添加 I濟或補充劑方式服用之。16 I 200403986 V. Explanation of the invention (12). The values are the average value ± the standard deviation. In summary, the preliminary results show that soybean products can inhibit the subcutaneous growth of _ LNCaP tumors in SC ID male rats, possibly because of the induction of apoptosis procedures, and Inhibits angiogenesis and proliferation. Isoflavones or xylose can reduce symptoms associated with menopause, such as paroxysmal fever and osteoporosis, and alleviate symptoms during menstruation. And its further inference is due to the activity of estrogen. Therefore, the improved compositions described herein are more effective in reducing these symptoms. In addition, isoflavones also have positive effects on cardiovascular-related symptoms, such as heart disease, cholesterol (phytosaponin also has a positive effect on cholesterol), angiogenesis, and other vascular symptoms. It is believed that the improved composition will reduce cardiovascular disease as well as the methods known so far but at a lower cost. As mentioned previously, it is known that isoflavones, xylose and phytosaponins each have positive effects on neurological and immune symptoms. It is believed that the improved composition will reduce neurological and immune symptoms and have the same effect as the methods known so far. , But the cost is lower. In addition, the combination described in this article can be expected to assist. Take the modified composition orally or by injection or parenterally, such as subcutaneously, intravenously, intramuscularly, intraperitoneally, or intranasally or sprayed into the mucosal tissue, or as an ointment or cream Apply to skin. Modified compositions can be taken in any suitable vehicle in solid or liquid form, such as lozenges, capsules, powders, soft gels, liquids, suspensions, emulsifiers, ointments or emulsions. The improved composition can also be taken as a food supplement or supplement.

第17頁 200403986 丨五、發明說明(13) - | 改良組合物之服用量隨個體、服用方式及欲得成效而 |定。一般有效劑量為10-2000毫克/劑。 I範例二藥片製造 ! 本專利所提供之組合物可用於製備成藥片狀或其他服 用型式。範例二提供一膠囊製備之實例。具活性之成分濃 度愈高則其愈容易形成片狀或乳膠狀。此一性質可將其他 營養劑加入其中。一實例是製備一植物化學物片劑其含有 鈣與維他命E,作為維護骨骼健康並/或減少停經後之症狀 如陣發性發熱。在此實施例之實例中,製備了含有1 2 5毫克 異黃酮濃縮物(5 0毫克異黃酮化合物)之6 0 0毫克乾狀壓縮 片劑。而在此片劑中即含鈣與鎂。 乾狀壓縮片劑之生產首先將下列成分置於1 2 0夸脫之哈 伯(Η 〇 b a r t )混合器中擾拌··四公斤之改良組合物 (3 9· 83%異黃酮)、1· 91公斤之山梨醇、0· 0 9 5公斤之硬酯 酸鎂、13. 1 1公斤磷酸二鈣。攪拌完成後即以史脫克BB2簡 易壓縮機在1噸壓力下將之壓縮成片狀,每片重量為600毫 克並含1 2 5 . 5 3毫克之改良組合物,故含5 0毫克之總異黃 酮。 或者,一種植物化學濃縮物可以單一服用方式提供 之,如:皮膚乳液或添加於傳統食物之食物成分,劑量為 1 0到2 0 0 0毫克/劑,此目的在於促進健康與福祉。益處包括 癌症預防、雌激素與性賀爾蒙相關疾病、抑制腦下垂體-甲 狀腺-生殖腺軸、減低酒精依賴、調節心臟血管、免疫與神 經系統、抗濾過性病源體效用及止痛效用。Page 17 200403986 丨 V. Description of the Invention (13)-| The dosage of the improved composition depends on the individual, the way of taking and the desired effect. A generally effective dose is 10-2000 mg / dose. I Example 2 Tablet Manufacturing! The composition provided by this patent can be used to prepare tablets or other servings. Example 2 provides an example of capsule preparation. The higher the active ingredient concentration, the easier it is to form a sheet or latex. This property allows other nutrients to be added to it. One example is the preparation of a phytochemical tablet containing calcium and vitamin E as a means of maintaining bone health and / or reducing symptoms such as paroxysmal fever after menopause. In the example of this embodiment, a 600 mg dry compressed tablet containing 125 mg of isoflavone concentrate (50 mg of isoflavone compound) was prepared. This tablet contains calcium and magnesium. The production of dry compressed tablets first put the following ingredients in a 120-quart Hubble (Η 〇bart) mixer and stir. · 4 kg of the improved composition (39.83% isoflavones), 1 91 kg of sorbitol, 0.95 kg of magnesium stearate, 13.1 kg of dicalcium phosphate. After the stirring is completed, it is compressed into a sheet by a Stryker BB2 simple compressor at a pressure of 1 ton. Each tablet weighs 600 mg and contains 125.53 mg of the improved composition, so it contains 50 mg of Total isoflavones. Alternatively, a phytochemical concentrate can be provided in a single dose, such as a skin lotion or a food ingredient added to traditional foods at a dose of 10 to 2000 mg / dose for the purpose of promoting health and well-being. Benefits include cancer prevention, estrogen and sex hormone-related diseases, suppression of the pituitary-thyroid-gonadal axis, reduction of alcohol dependence, regulation of the cardiovascular system, immune and nervous system, anti-filter pathogenic effects and analgesic effects.

第18頁 200403986 五、發明說明(14) » 範例三 | 兩片式動物性膠囊之製備方法為將0.106公克之改良組 i合物(44.35%異黃酮)灌入0狀空膠囊之一半,並以另一 |半之膠囊蓋緊,其可提供47.2毫克之總異黃酮。P.18 200303986 V. Explanation of the invention (14) »Example three | Two-piece animal capsules are prepared by filling 0.106 g of the modified compound (44.35% isoflavone) into one half of the 0-shaped empty capsule, and Cap tightly with the other half of the capsule, which provides 47.2 mg of total isoflavones.

I 範例四 表四列出植物化學物製品之不同來源之比較。其顯示 本發明異黃酮濃縮物之組合物之植物化學較一般自然蔬果 中含量高出甚多。明顯地,糖苷類異黃酮葡萄糖與植物皂 素含量較食物來源高出一百倍以上,而較可自然濃縮此類 植物化學物質之植物幼芽高出二十倍以上。本發明之’異黃 酮濃縮物’與其他濃縮物相比較,顯示異黃酮為後者產物之 優勢成分,其會減少其他有益於健康之植物化學物。此 外,其他產品之萃取技術利用改變其成份(尤其是異黃酮) 之技術,故其並非與自然蔬果中物質完全相同(美國專利 編號 3, 637, 562) 一種改良組合物與其他先前敘述之組合物相比較,結 果顯示於表四。I Example 4 Table 4 shows a comparison of different sources of phytochemicals. It shows that the phytochemistry of the composition of the isoflavone concentrate of the present invention is much higher than that of ordinary natural fruits and vegetables. Obviously, the content of glucoside isoflavones glucose and phytosaponin is more than 100 times higher than that of food sources, and more than 20 times higher than that of young shoots of plants that can naturally concentrate such phytochemicals. Compared with other concentrates, the 'isoflavone concentrate' of the present invention shows that isoflavones are the dominant component of the latter product, which will reduce other health-friendly phytochemicals. In addition, the extraction technology of other products uses technology that changes its composition (especially isoflavones), so it is not exactly the same as that in natural fruits and vegetables (US Patent No. 3,637, 562). An improved composition combined with other previously described combinations The results are shown in Table IV.

第19頁 200403986 五、發明說明(15) 表四本發明之比較產品 產品樣本 異黃酮糖 類產品 (毫克/克) 異黃酮配 悬產品(晕 克/克) 5,7,4-三 羥基異黃 -酮/黃豆甘 原比 1木素糖(毫 :克/克) 植物皂素 (毫克/克) 酚酸(毫 克/克) 改良組合物 401.1 3.37 1.06 至 1 0.2 460.7 25.47 大豆 1.748-2.77 6a 2.776、0.07 5 1.59-2.7 NA 0.9-3.2° 大豆麵粉(去 脂) 1.969a 0.045a 3.58 0.0013 2.870c 大豆芽 24.32d 0.85d NA 16.7-1.985 ΝΑ 專利產物ε (PTD ΝΑ 2.5-6.5c 0.5-3.5 NA NA ΝΑ 專利產物f (PTI) ΝΑ 5.M4.7f 0.433-3.48 NA NA ΝΑ 專利產物2 (ΡΤΙ) ΝΑ 1.7-3.52 0.66-2.86 NA NA ΝΑ ΡΤΙ 產物h ΝΑ 970 12.8 NA NA ΝΑ ΡΤΙ 產物h ΝΑ 640 2.0 NA NA ΝΑ 大豆蜜糖(乾 式) 27.6 0.1 1.37 NA NA 5.788 Novogen : 0.0 550 1-1.7 tol NA NA ΝΑPage 19, 200403986 V. Description of the invention (15) Table 4 Comparative product samples of the present invention Product samples isoflavone sugar products (mg / g) Isoflavone suspension products (halo g / g) 5,7,4-trihydroxy isoflavone -Keto / soybean glycogen ratio 1 xylose (milli: g / g) Phytosaponin (mg / g) Phenolic acid (mg / g) Improved composition 401.1 3.37 1.06 to 1 0.2 460.7 25.47 Soy 1.748-2.77 6a 2.776 0.07 5 1.59-2.7 NA 0.9-3.2 ° Soy flour (non-fat) 1.969a 0.045a 3.58 0.0013 2.870c Soy sprout 24.32d 0.85d NA 16.7-1.985 ΝΑ Patented product ε (PTD ΝΑ 2.5-6.5c 0.5-3.5 NA NA ΝΑ patented product f (PTI) NA 5.M4.7f 0.433-3.48 NA NA ΝA patented product 2 (PTI) NA 1.7-3.52 0.66-2.86 NA NA ΝΑ ΡΙΙ h h ΝΑ 970 12.8 NA NA ΝΑ ΡΙΙ h h ΝΑ 640 2.0 NA NA ΝΑ Soy molasses (dry) 27.6 0.1 1.37 NA NA 5.788 Novogen: 0.0 550 1-1.7 tol NA NA ΝΑ

a ·· W a n g Η ·和 M u r p h y P . A.,農業食物化學期刊, 1 9 9 4, 4 2, 1 6 6 6 - 1 6 7 3,a ·· W a n g Η · and Mu r p h y P. A., Journal of Agricultural Food Chemistry, 1 9 9 4, 4 2, 1 6 6 6-1 6 7 3,

第20頁 200403986 五、發明說明(16) _ b: Anderson R.L·和 Wolf W.J·,營養期刊,125:581S-588S, 1995 ' c: Seo A·和Morr C.V·,農業食物化學期刊,1 984, 32, 530-533. d: Soy LifeTM宣傳文獻 e: WO 95/10530, PCT/US94/10697 e: WO 95/10512, PCT/US94/10699 e: WO 95/10529, PCT/US94/10696 h: NCI文獻 i : Novogen宣傳文獻 範例五 該改良組合物包含糠苷形式之異黃酮,較先前描述之 含糖每配基類之組合物在體溫下之溶解度為高。 用量瓶製備5,7,4 -三羥基異黃酮(genistein)、染料木甘 (genistin)、黃豆武原(daidzein) ' 黃豆武(diadzin)與異 黃酮濃縮物。將樣品置於3 7 °C之水浴中1 7小時,既而以〇, 2 微米針筒式過濾器快速過濾以去除粒狀物。濾液則以高效 能液相層析法(HPLC )分析異黃酮濃度。結果列於表五。Page 20 200403986 V. Description of the invention (16) _ b: Anderson RL · and Wolf WJ ·, Journal of Nutrition, 125: 581S-588S, 1995 'c: Seo A · and Morr CV ·, Journal of Agricultural Food Chemistry, 1 984 , 32, 530-533. D: Soy LifeTM promotional literature e: WO 95/10530, PCT / US94 / 10697 e: WO 95/10512, PCT / US94 / 10699 e: WO 95/10529, PCT / US94 / 10696 h : NCI document i: Novogen propaganda document Example 5 This improved composition contains isoflavones in the form of furoside, which has a higher solubility at body temperature than the sugar-containing per-lipid composition described previously. A 5,7,4-trihydroxy isoflavone (genistein), genistin, daidzein (diadzin) and isoflavone concentrate were prepared from a measuring bottle. The sample was placed in a water bath at 37 ° C for 17 hours, and then quickly filtered with a 0.2 micron syringe filter to remove particulate matter. The filtrate was analyzed for isoflavone concentration by high performance liquid chromatography (HPLC). The results are shown in Table 5.

第21頁 200403986 五、發明說明(17) 表五:異黃酮糖苷類與糖苷配基類溶解度之比較 異黃酮樣品 5,7,4-三羥基異 黃酮 (ppm) 染料木武(ρρπ0 黃豆貳原 (ppm) 黃豆貳 (ppm) 5,7,4-三羥基異 黃酮 7.42 染料木貳 33.89 黃豆Λ原 3.64 黃豆甙 48.51 異黃酮濃縮物 0.492 30.075 0.672 37.69 糖苷類形式之黃豆甙與染料木贰,在37°C下之濃度較 相對之糖苷配基類形式至少分別高出4. 57與13. 32倍。 |Page 21 200303986 V. Description of the invention (17) Table 5: Comparison of solubility of isoflavone glycosides and aglycones. Isoflavone samples 5,7,4-trihydroxy isoflavones (ppm) Genistein (ρρπ0 Soya Bean Primitive) (ppm) Soy Bean (ppm) 5,7,4-trihydroxy isoflavone 7.42 Genistein 33.89 Soybean Λ original 3.64 Daidzein 48.51 Isoflavone concentrate 0.492 30.075 0.672 37.69 Glycosides and daidzein, in The concentration at 37 ° C is at least 4.57 and 13.32 times higher than the relative aglycone form, respectively. |

i Ii I

對異黃酮之改變為去除異黃酮週邊之碳水化合物。此 I 1 iThe change to isoflavones is to remove carbohydrates around the isoflavones. This I 1 i

丨一改變使異黃酮較不易溶於水。維護自然改變,糖基作 IA change made the isoflavones less soluble in water. Maintain natural change, sugar base as I

; I 丨用,可促進溶解度。此一事實顯現於表五中溶解度之比 丨 j t 丨較。與相對之非糖苷類形式比較,染料木貳異黃酮之溶解丨 ; ! 丨度高出4. 6倍,而黃豆甙異黃酮高出13. 3倍。高溶解度使腸i 丨道生物有較佳生物利用性。糖基作用並不會抑制其在腸道丨 |之吸收,因為腸中細菌可在吸收前將糖苷形式轉變為糖苷 :配基類形式。 範例六 < 木素糖可以下列方法自亞麻中萃取。 9 78克之脫脂亞麻肉(F1)以2000克85 %之乙醇在40 °C 下萃取1 0分鐘,形成泥狀物。泥狀物經過濾後,以6 0 0 0克 酒精重複萃取兩次。; I 丨 use, can promote solubility. This fact is shown in Table 5 for the solubility ratio 丨 j t 丨 comparison. Compared with the relative non-glycoside form, the dissolution of genistein isoflavones is 4.6 times higher, while daidzein isoflavones are 13.3 times higher. The high solubility makes the intestinal organisms have better bioavailability. Glycosylation does not inhibit its absorption in the intestine, because bacteria in the intestine can convert the glycosidic form to the glycosidic: aglycone form before absorption. Example 6 < Xylose can be extracted from flax by the following methods. 9 78 g of defatted flax meat (F1) was extracted with 2000 g of 85% ethanol at 40 ° C for 10 minutes to form a mud. After filtering the mud, it was repeatedly extracted twice with 60,000 g of alcohol.

第22頁 200403986 五、發明說明(18) ^ 酒精部分在7 0 3C真空狀態下揮發,形成1 1 8 6克之液態 物。此一液態物與1 0 0 0克之水相混合。 上述混合物以5 0 0 0分子量分離膜超過慮之,形成7 6 7克 之濾液以及1 2 8 3克之濾渣。 濾產部分經冷束乾燥後,形成2 7 · 8 4克之樣品(F 2 )。 7 6 7克之濾液部分則在5 0 °C下以每分鐘1 0毫升之速度注 入至3 5毫升之X A D - 4樹脂管柱中。出流液收集並乾燥,形成 1 4. 8克樣品(F3 ) 。XAD-4為一種吸收性樹酯商標名,購自Page 22 200403986 V. Description of the invention (18) ^ The alcohol part is volatilized in a vacuum state of 70 3C to form 1 186 g of liquid substance. This liquid was mixed with 1,000 grams of water. The above-mentioned mixture has a molecular weight separation membrane of 50000, and a filtrate of 767 g and a filter residue of 123 g are formed. After the filtered part was dried by cold beam, a sample of 2 7 · 84 g (F 2) was formed. The 7 6 g portion of the filtrate was poured into a 35 mL X A D-4 resin column at 50 ° C at a rate of 10 mL per minute. The effluent was collected and dried to form 14.8 grams of sample (F3). XAD-4 is a brand name of absorbent resin, purchased from

Rohm & Haas 〇 管柱以四倍的體積(1 4 0毫升)之7 0 %乙醇在5 0 °C下沖 洗。洗出液在7 0 °C真空狀態下揮發乾燥,形成1. 7 9克樣品 (F4 )。針對四個部分進行木素糖含量分析並以閉異落葉 松脂素(secoisolariciresinol)重量計算濃度。如表六所 示,此一萃取方法可提高木素糖之濃度。 表六:木素糖濃度(以閉異落葉松脂素計算) 部分 F1 F2 F3 F4 閉異落葉松脂素濃度 (毫克/克) 2.3 1.9 4.8 13.4 酚酸 雖然本發明已發表較佳實施例以便於協助對本發明之 φ 了解,但本發明亦可在不背離發明原則下,有各種不同實 施例。故本發明在不背離所附申請專利範圍之發明原則 下,應涵蓋所有可能之實施例、改良及與實施例相當之範 例。 200403986 圖式簡單說明The Rohm & Haas 〇 column was rinsed with 70% ethanol in four volumes (140 ml) at 50 ° C. The eluate was evaporated to dryness under vacuum at 70 ° C to form 1.79 grams of sample (F4). The lignin content analysis was performed for four parts and the concentration was calculated based on the weight of secoisolariciresinol. As shown in Table 6, this extraction method can increase the concentration of xylose. Table 6: Lignin Concentrations (Calculated with L-Isolanin) Partial F1 F2 F3 F4 Iso-Larisin Concentrations (mg / g) 2.3 1.9 4.8 13.4 Phenolic acid Although the present invention has published preferred embodiments to assist Know the φ of the present invention, but the present invention can also have various embodiments without departing from the principles of the invention. Therefore, the present invention should cover all possible embodiments, improvements, and examples equivalent to the embodiments without departing from the invention principles of the scope of the attached patent application. 200403986 Schematic description

Claims (1)

200403986 六、申請專利範圍 · 1. 一種提供飲食補充品的方法,可被用來預防或改善選自 由乳癌、皮膚癌及腸癌所構成之族中的疾病,該方法包括 提供一植物萃取組合物並有助人體健康之步驟,該組合物 包含至少兩種以上提煉之植物化學物質餾分物,其選自由 異黃酮、木素糖、植物皂素、兒茶酸與酚酸所構成之族。 2 .如申請專利範圍第1項之方法,其中該方法可被用作治療 乳癌。 3. 如申請專利範圍第1項之方法,其中該方法可被用作治療 皮膚癌。200403986 6. Scope of patent application 1. A method for providing dietary supplements, which can be used to prevent or ameliorate diseases selected from the group consisting of breast cancer, skin cancer, and intestinal cancer. The method includes providing a plant extract composition It also helps human health. The composition contains at least two or more refined phytochemical distillates selected from the group consisting of isoflavones, xylose, phytosaponins, catechins, and phenolic acids. 2. The method according to item 1 of the scope of patent application, wherein the method can be used to treat breast cancer. 3. The method according to the scope of patent application, wherein the method can be used to treat skin cancer. 4. 如申請專利範圍第1項之方法,其中該方法可被用作治療 腸癌。 5. —種提供飲食補充品的方法,可被用來預防或改善選自 由尿道癌、膀胱癌及列腺癌所構成之族中的疾病,該方法 包括提供一植物萃取組合物並有助人體健康之步驟,該組 合物包含至少兩種以上提煉之植物化學物質餾分物,其選 自由異黃酮、木素糖、植物皂素、兒茶酸與酚酸所構成之 族0 6. 如申請專利範圍第5項之方法,其中該方法可被用作治療 尿道癌。 I I 7. 如申請專利範圍第5項之方法,其中該方法可被用作治療· 膀胱癌。 8. 如申請專利範圍第5項之方法,其中該方法可被用作治療 列腺癌。 9. 一種提供飲食補充品的方法,可被用來預防或改善選自4. The method according to item 1 of the patent application scope, wherein the method can be used to treat bowel cancer. 5. A method of providing dietary supplements, which can be used to prevent or ameliorate diseases selected from the group consisting of urinary tract cancer, bladder cancer and prostate cancer, the method comprising providing a plant extract composition and helping the human body In the step of health, the composition includes at least two or more refined phytochemical distillates selected from the group consisting of isoflavones, xylose, phytosaponins, catechins and phenolic acids. The method of item 5, wherein the method can be used for treating urethral cancer. I I 7. The method according to item 5 of the patent application, wherein the method can be used for the treatment of bladder cancer. 8. The method of claim 5 in the scope of patent application, wherein the method can be used to treat prostate cancer. 9. A method of providing dietary supplements that can be used to prevent or improve 第25頁 200403986 六、申請專利範圍 由偏頭痛及癡呆症所構成之族中的失調疾病,該方法包括 提供一植物萃取組合物並有助人體健康之步驟,該組合物 包含至少兩種以上提煉之植物化學物質餾分物,其選自由 異黃酮、木素糖、植物皂素、兒茶酸與酚酸所構成之族。 1 〇.如申請專利範圍第9項之方法,其中該方法可被用作治 療偏頭痛。 11 ·如申請專利範圍第9項之方法,其中該方法可被用作治 療癡呆症。Page 25, 200403986 6. Patent application: Disorder disorders in the family consisting of migraine and dementia. The method includes the steps of providing a plant extract composition and helping human health. The composition contains at least two types of extraction. The phytochemical distillate is selected from the group consisting of isoflavones, xylose, phytosaponins, catechins and phenolic acids. 10. The method according to item 9 of the scope of patent application, wherein the method can be used for treating migraine. 11-The method according to item 9 of the patent application, wherein the method can be used to treat dementia. 1 2 · —種提供飲食補充品的方法,可被用來預防或改善酗酒 疾病,該方法包括提供一植物萃取組合物並有助人體健康 之步驟,該組合物包含至少兩種以上提煉之植物化學物質 餾分物,其選自由異黃酮、木素糖、植物皂素、兒茶酸與 紛酸所構成之族。 1 3. —種提供飲食補充品的方法,可被用來預防或降低血液 中膽固醇、減低冠狀心臟病危險或調節血液脂肪狀況,該 方法包括提供一植物萃取組合物並有助人體健康之步驟, 該組合物包含至少兩種以上提煉之植物化學物質餾分物, 其選自由異黃酮、木素糖、植物皂素、兒茶酸與酚酸所構 成之族。 1 4 ·如申請專利範圍第1 3項之方法,其中該方法可被用作降鲁 低血液中膽固醇。 1 5.如申請專利範圍第1 3項之方法,其中該方法可被用作減 i低冠狀心臟病危險。 | 1 6.如申請專利範圍第1 3項之方法,其中該方法可被用作調1 2 · A method for providing a dietary supplement, which can be used to prevent or improve alcoholism, the method comprises the steps of providing a plant extract composition and helping human health, the composition comprising at least two kinds of refined plants A distillate of a chemical substance, which is selected from the group consisting of isoflavones, xylose, phytosaponins, catechins and phenols. 1 3. A method of providing dietary supplements, which can be used to prevent or reduce cholesterol in the blood, reduce the risk of coronary heart disease, or regulate blood fat, the method includes the steps of providing a plant extract composition and helping human health The composition contains at least two or more refined phytochemical distillates selected from the group consisting of isoflavones, xylose, phytosaponins, catechins and phenolic acids. 14 · The method according to item 13 of the scope of patent application, wherein the method can be used to reduce cholesterol in the blood. 15. The method according to item 13 of the scope of patent application, wherein the method can be used to reduce the risk of coronary heart disease. 1 6. The method according to item 13 of the patent application scope, wherein the method can be used as a debugger 第26頁 200403986 I六、申請專利範圍 - 節血液脂肪狀況。 17. —種提供飲食補充品的方法,可被用來降低或預防陣發 性發熱、骨質疏鬆症、睡眠失調、陰道乾燥症或經前症 候,該方法包括提供一植物萃取組合物並有助人體健康之 步驟,該組合物包含至少兩種以上提煉之植物化學物質餾 分物,其選自由異黃酮、木素糖、植物皂素、兒茶酸與酚 酸所構成之族。 1 8.如申請專利範圍第1 7項之方法,其中該方法可被用作預 防或治療紅潮。 1 9.如申請專利範圍第1 8項之方法,其中該方法可被用作預 防或治療骨質疏鬆症。 2 〇.如申請專利範圍第1 8項之方法,其中該方法可被用作預 防或治療經前症候。 21.如申請專利範圍第18項之方法,其中該方法可被用作預 防或治療睡眠失調。 2 2.如申請專利範圍第1 8項之方法,其中該方法可被用作預 防或治療陰道乾燥症。Page 26 200403986 I Sixth, the scope of patent application-blood fat status. 17. A method of providing a dietary supplement that can be used to reduce or prevent paroxysmal fever, osteoporosis, sleep disorders, vaginal dryness or premenstrual symptoms, the method comprising providing a plant extract composition and helping For human health, the composition includes at least two or more refined phytochemical distillates selected from the group consisting of isoflavones, xylose, phytosaponin, catechin, and phenolic acid. 18. The method according to item 17 of the scope of patent application, wherein the method can be used to prevent or treat red tide. 19. The method according to item 18 of the scope of patent application, wherein the method can be used to prevent or treat osteoporosis. 20. The method according to item 18 of the scope of patent application, wherein the method can be used for preventing or treating premenstrual symptoms. 21. The method of claim 18, wherein the method can be used to prevent or treat sleep disorders. 2 2. The method of claim 18 in the scope of patent application, wherein the method can be used to prevent or treat vaginal xerostomia. 第27頁 200403986 六、指定代表圖Page 27 200403986 VI. Designated Representative Map
TW92132089A 1997-10-02 1999-01-14 A composition including isoflavones refined from plant TWI260205B (en)

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