JP2007051120A - Method of manufacturing mulberry branch and stem extract - Google Patents

Method of manufacturing mulberry branch and stem extract Download PDF

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Publication number
JP2007051120A
JP2007051120A JP2005269101A JP2005269101A JP2007051120A JP 2007051120 A JP2007051120 A JP 2007051120A JP 2005269101 A JP2005269101 A JP 2005269101A JP 2005269101 A JP2005269101 A JP 2005269101A JP 2007051120 A JP2007051120 A JP 2007051120A
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extract
mulberry
deoxynojirimycin
polyphenols
blood glucose
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Chukei Nomura
忠敬 野村
Takashi Ninagawa
隆 蜷川
Kazuaki Sugiura
和明 杉浦
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SILK KOGEI KK
Kyoto City
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SILK KOGEI KK
Kyoto City
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Abstract

<P>PROBLEM TO BE SOLVED: To provide a mulberry branch and stem extract enhanced in blood sugar suppresive effect by synergetic effect of an activity inhibition of an α-glucosidase by a 1-deoxynojirimycine and an activity inhibition of an α-amylase by polyphenols. <P>SOLUTION: By squeezing mulverry chips which have been conventionally diposed of by a compressor, the mulberry branch and stem extract containing the 1-deoxynojirimycine and polyphenols in a high concentration and having the high blood sugar suppressing effect, is extracted. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

発明の詳細な説明Detailed Description of the Invention

日常の食生活で多く摂取する糖類によって発症する糖尿病はじめ多くの生活習慣病を予防する目的としてこれまで廃棄物として焼却処分されていた桑条チップ抽出エキスに血糖値上昇抑制作用を見出した技術。A technology that has been found to have an inhibitory effect on the increase in blood sugar level of mulberry chip extract, which has been incinerated as waste for the purpose of preventing diabetes and other lifestyle-related diseases caused by saccharides ingested in daily diets.

近年の日本人に見られる生活習慣病は欧米化の食生活によるものとされているが、日常の食生活が大きく反映し、米や穀物の摂取による糖類の過剰に起因している可能性が高い。特に糖尿病は食生活の改善が最大の予防治療の手段とされ低カロリーの食事、運動療法、薬物療法など専門機関で指導実施されている。The lifestyle-related diseases seen in Japanese people in recent years have been attributed to the Western diet, but the daily diet is largely reflected and may be due to excess sugar due to ingestion of rice and grains. high. Diabetes mellitus, in particular, is the most preventive and therapeutic means of improving dietary habits, and is being guided by specialized institutions such as low-calorie diets, exercise therapy, and drug therapy.

このところ糖類の吸収を抑制または糖類の分解代謝を調節する薬剤の開発が進みα−グルコシダーゼ阻害剤として「アカルボーズ」「ベイズイン」等が上市され今では糖尿病、肥満の治療予防薬として主流を占めている感がある。「桑白皮」として糖尿病や高血圧などの生薬として用いられ、その作用の多くは血糖値上昇抑制作用に関するものであった。その後現代にいたって、血糖値上昇抑制作用の機序が1−デオキシノジリマイシンによるα−グルコシダーゼ阻害作用(YOSIKUNI,Y.,Agric.Biol.Chem.52,pp ,1988)に基づくことが明らかにされた。近年、桑葉に関して熱抽出エキスにα−アミラーゼ阻害作用、マルターゼ、スクラーゼ阻害作用が見出され、その作用物質が1−デオキシノジリマイシン以外の成分であることが示唆されている。1−デオキシノジリマイシンは桑以外では中南米産のザコビニア属の植物と放線菌の培養液にしか見出されていない。したがって、桑には他の植物に見られない特異的な血糖値上昇抑制物質が存在していることは明らかである。Recently, the development of drugs that suppress the absorption of saccharides or regulate the degradation metabolism of saccharides has progressed, and “Acarbose”, “Baisein”, etc. have been put on the market as α-glucosidase inhibitors, and now they are mainly used as therapeutic and preventive agents for diabetes and obesity. There is a feeling. It was used as a herbal medicine for diabetes and hypertension as “mulberry skin”, and many of its actions were related to the inhibitory action on the increase in blood glucose level. Since then, it has been clarified that the mechanism of the inhibitory action on the increase in blood glucose level is based on the α-glucosidase inhibitory action by 1-deoxynojirimycin (YOSIKUNI, Y., Agric. Biol. Chem. 52, pp, 1988). It was done. In recent years, α-amylase inhibitory action, maltase, sucrase inhibitory action has been found in heat-extracted extracts with respect to mulberry leaves, and it has been suggested that the active substance is a component other than 1-deoxynojirimycin. 1-deoxynojirimycin is found only in the culture solution of plants of the genus Zacobinia from Latin America and actinomycetes except for mulberry. Therefore, it is clear that mulberry has a specific inhibitor of blood sugar level elevation that is not found in other plants.

発明しようとする課題Problems to be invented

本発明の課題は、桑条抽出エキスにも従来報告されている桑白皮や桑葉同様の血糖値上昇抑制物質が存在することを本発明で明らかにし、桑条抽出エキスが糖尿病患者はもとより血糖値の上昇が懸念される二次性糖尿病が予知される人への改善と発症の予防に大変有用性のある機能性健康食品として発展する可能性がある。The object of the present invention is to clarify in the present invention that a mulberry bark extract has the same blood glucose level inhibitory substances as mulberry bark and mulberry leaves that have been reported in the past. There is a possibility that it will develop as a functional health food that is very useful for the improvement and prevention of the onset of secondary diabetes, for which an increase in blood glucose level is a concern.

春に桑株から生じた桑条を2−6ヶ月後に伐採し、1週間から12ヶ月間乾燥したもの20キログラムを約0.5〜5センチメートルのチップ状に破砕した。これを水に浸漬した後、圧縮機で絞り10リットルの抽出エキスを得た。浸漬圧縮して得られたエキス10リットルを85℃以下の温浴中で連続濃縮し、濃縮エキス500ミリリットルを得た。
1−デオキシノジリマイシンの定量法
Mulberry strips produced from mulberry strains in the spring were harvested 2-6 months later, and 20 kilograms dried for 1 to 12 months were crushed into chips of about 0.5 to 5 centimeters. After this was immersed in water, an extract of 10 liters was obtained by squeezing with a compressor. 10 liters of extract obtained by immersion compression was continuously concentrated in a hot bath at 85 ° C. or less to obtain 500 ml of concentrated extract.
Determination method of 1-deoxynojirimycin

浸漬圧縮エキスおよび濃縮エキスを0.5ミリリットルを正確にキャップ付ネジ口試験管にとり、30mMホウ酸緩衝液2.4ml、4−Fluro−7−nitrobenzofurazan5.0ミリグラムをエタノール1ミリリットルに溶解した溶液100マイクロリットルを正確に加えて混合する。混合溶液を60℃40分間加温後、直ちに冷却し、1N塩酸2ミリリットルを正確に加えた。この混合液20マイクロリットルをHPLCで分析した。分析にはxxxx社製のHPLCシステム(モデルLC−10A)を用い、カラムはODSカラム(YMC−pack DOS−A A−302)を、移動層はA液;0.05%リン酸、B液;メタノール:5%リン酸(99:1)を用い、0分(A100%)−45分(95%、B5%)のグラジエント系(流速1ミリリットl/分、温度40℃)により分析し、Ex470nm、Em530nmで蛍光強度を測定し求めた。
総ポリフェノールの定量法
A solution obtained by accurately taking 0.5 ml of the soaked compressed extract and concentrated extract in a capped screw-cap test tube and dissolving 2.4 ml of 30 mM borate buffer and 5.0 mg of 4-Fluoro-7-nitrobenzofurazane in 1 ml of ethanol 100 Add exactly microliters and mix. The mixed solution was heated at 60 ° C. for 40 minutes and then immediately cooled, and 2 ml of 1N hydrochloric acid was accurately added. 20 microliters of this mixture was analyzed by HPLC. For analysis, an HPLC system (model LC-10A) manufactured by xxx was used, the column was an ODS column (YMC-pack DOS-A A-302), the moving bed was liquid A; 0.05% phosphoric acid, liquid B Analyzed with methanol: 5% phosphoric acid (99: 1) with a 0 minute (A100%)-45 minute (95%, B5%) gradient system (flow rate 1 milliliter l / min, temperature 40 ° C.); The fluorescence intensity was measured and obtained at Ex 470 nm and Em 530 nm.
Quantitative determination of total polyphenols

総ポリフェノールの定量はフェノール発色試験錠(和光純薬工業株式会社)を用い比色法で行った。試験溶液10ミリリットリにフェノール発色試験錠1錠を加え室温で20分間放置後、510nmにおける吸光度を測定しコーヒー酸量として算出した。The total polyphenol was quantified by a colorimetric method using a phenol coloring test tablet (Wako Pure Chemical Industries, Ltd.). One phenol coloring test tablet was added to 10 milliliters of the test solution and allowed to stand at room temperature for 20 minutes, and then the absorbance at 510 nm was measured and calculated as the amount of caffeic acid.

桑幹浸漬抽出エキスおよび濃縮エキスの1−デオキシノジリマイシンおよび総ポリフェノールの含有量

Figure 2007051120
阿武らによって報告されている(日本食品保蔵科学会雑誌VOL.30 No.5,2004)桑葉エキス中に含まれる1−デオキシノジリマイシンの含有量に比べ、桑条浸漬抽出エキス中の1−デオキシノジリマイシン含有量の方が勝る結果が得られた。また、総ポリフェノール含量も桑葉エキスの報告内容を上回る成績が得られた。この成績は、桑葉エキスを凌駕する血糖値上昇抑制効果が桑条浸漬抽出エキスにあることを示唆している。Content of 1-deoxynojirimycin and total polyphenols in mulberry trunk soaked extract and concentrated extract
Figure 2007051120
Compared with the content of 1-deoxynojirimycin contained in the mulberry leaf extract reported by Abu et al. (Japan Food Preservation Science Society magazine VOL.30 No. 5, 2004), A better result was obtained with a deoxynojirimycin content. In addition, the total polyphenol content exceeded the reported content of mulberry leaf extract. These results suggest that the extract extracted from mulberry leaves has the effect of suppressing the increase in blood glucose level that exceeds that of mulberry leaves extract.

桑条浸漬エキスおよび過熱濃縮エキスの経口投与による血糖上昇抑抑制作用
実験前日一晩絶食された7週令のWister系雄性ラツトを用い、澱粉及びショ糖を含む人工飼料投与前に桑条浸漬抽出エキスおよび加熱濃縮エキスを経口投与し、経時的に各群5匹の血糖値をグルコースオキシダーゼ法にて測定し平均値から上昇抑制率を算出し、エキス非投与群と比較した。血糖値の変化率(%)は下式より求めた。
血糖値の変化率(%)
=検体投与後の血糖値(mg/dl)/検体投与前の血糖値(mg/dl)x100

Figure 2007051120
投与10分後から血糖値が100%以上上昇した無処置対象群に対して、桑条浸漬エキス群および濃縮エキス群では共々血糖値はほとんど上昇せず100分後まで検体投与前の血糖値とほぼ同じ値で推移した。以上の結果は1−デオキシノジリマイシンによるグルコシダーゼの阻害のみならず、ポリフェノール類によるアミラーゼの阻害が起こったことを示している。Inhibition of blood glucose elevation by oral administration of mulberry strip soaked extract and superheated concentrated extract Using 7-week-old Wister male rat fasted overnight the day before the experiment, before mulberry strip soak extraction before administration of artificial feed containing starch and sucrose The extract and the heat-concentrated extract were orally administered, and the blood glucose level of each group of 5 mice was measured over time by the glucose oxidase method, and the increase inhibition rate was calculated from the average value, and compared with the extract non-administered group. The change rate (%) of the blood glucose level was obtained from the following formula.
Change rate of blood glucose level (%)
= Blood glucose level after sample administration (mg / dl) / blood glucose level before sample administration (mg / dl) x 100
Figure 2007051120
In contrast to the untreated subject group, whose blood glucose level increased by 100% or more from 10 minutes after administration, the blood glucose level hardly increased in the mulberry strip soaked extract group and the concentrated extract group. It remained almost the same value. The above results indicate that not only the inhibition of glucosidase by 1-deoxynojirimycin but also the inhibition of amylase by polyphenols.

発明の効果The invention's effect

桑条抽出エキスに含まれる1−デオキシノジリマイシンやポリフェノールは水溶性であることから有効成分の濃度調整が容易であり飲料水は基より日常の菓子類に至るまで使用が可能である。即ち食品、食品添加物、化粧品、医薬等の分野での血糖値上昇抑制剤、また、桑条エキスのポリフェノール成分は、桑葉抽出エキスに含まれるクロロゲン酸、コーヒー酸、アストラガリンなどと同様の物質群からなると考えられ、これらの物質はアミラーゼ阻害作用を有することが報告されている。特にクロロゲン酸は、葉のエキス中で含量が多くα−アミラーゼ阻害活性に関与していることが認められている。桑条エキスにも含量が多いことが予測されるクロロゲン酸は、肝臓における過剰な糖新生の抑制に関与するグルコース−6−フォスファターゼ阻害作用やインスリン分泌促進作用を示すとの報告があり、抗糖尿病作用以外の肝障害予防作用、老化防止などの発展的な作用が期待できる。Since 1-deoxynojirimycin and polyphenol contained in the mulberry extract extract are water-soluble, it is easy to adjust the concentration of the active ingredient, and the drinking water can be used from the base to the daily confectionery. That is, the blood sugar level increase inhibitor in the fields of food, food additives, cosmetics, medicine, etc., and the polyphenol component of mulberry extract is the same as chlorogenic acid, caffeic acid, astragalin, etc. contained in mulberry leaf extract. It is considered that the substance consists of a group of substances, and these substances have been reported to have an amylase inhibitory action. In particular, chlorogenic acid is found to have a high content in leaf extracts and to be involved in α-amylase inhibitory activity. Chlorogenic acid, which is predicted to have a high content in mulberry strip extract, has been reported to exhibit glucose-6-phosphatase inhibitory action and insulin secretion promoting action involved in the suppression of excessive gluconeogenesis in the liver. In addition to the effects, it can be expected to develop effects such as preventing liver damage and preventing aging.

Claims (2)

活性物質1−デオキシノジリマイシンおよびポリフェノール類を含有する桑株から生じた桑条(桑枝)を伐採後天日乾燥せしめた桑条チップを水に浸漬して得られる浸漬抽出エキスおよび85℃以下の温浴によって得られた加熱濃縮エキス。Active substance 1-deoxynojirimycin and mulberry extract (mulberry branch) produced from a mulberry strain containing polyphenols, and a soaked extract obtained by immersing mulberry chips that have been dried in the sun after being cut in water, Heated concentrated extract obtained by warm bath. 乾燥桑条の浸漬抽出エキス25ml/kgおよび加熱濃縮エキス0.5ml/kg投与群のラットは澱粉及びショ糖を含む飼料群の血糖値上昇を100分後まで抑制した成績から、桑条浸漬抽出エキスは1−デオキシノジリマイシンによるグルコシダーゼ阻害とポリフェノール類によるアミラーゼ阻害により小腸でのグルコース吸収を抑制する特異的な相乗効果が発揮される請求項1に記載の1−デオキシノジリマイシンおよびポリフェノール類を含有するエキス。From the results in which the rats in the group administered with 25 ml / kg of the dried mulberry soak extract and 0.5 ml / kg of the heat-concentrated extract suppressed the increase in blood glucose level of the feed group containing starch and sucrose until 100 minutes later, The extract contains 1-deoxynojirimycin and polyphenols according to claim 1, wherein a specific synergistic effect of suppressing glucose absorption in the small intestine is exhibited by inhibition of glucosidase by 1-deoxynojirimycin and amylase inhibition by polyphenols. To extract.
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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010536804A (en) * 2006-08-21 2010-12-02 中国医学科学院薬物研究所 Use of an effective fraction of alkaloids derived from mulberry branches to prepare hypoglycemic agents
JP2013216712A (en) * 2013-08-02 2013-10-24 Inst Of Materia Medica Chinese Academy Of Medical Sciences Use of effective fraction of alkaloid originating from mulberry branch for preparing hypoglycemic medicine
JP2015168657A (en) * 2014-03-07 2015-09-28 国立大学法人岩手大学 hair modifier
JP2016011305A (en) * 2015-09-24 2016-01-21 中国医学科学院薬物研究所 Use of effective fraction of alkaloid originating from mulberry branch for preparing hypoglycemic medicine

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010536804A (en) * 2006-08-21 2010-12-02 中国医学科学院薬物研究所 Use of an effective fraction of alkaloids derived from mulberry branches to prepare hypoglycemic agents
JP2013216712A (en) * 2013-08-02 2013-10-24 Inst Of Materia Medica Chinese Academy Of Medical Sciences Use of effective fraction of alkaloid originating from mulberry branch for preparing hypoglycemic medicine
JP2015168657A (en) * 2014-03-07 2015-09-28 国立大学法人岩手大学 hair modifier
JP2016011305A (en) * 2015-09-24 2016-01-21 中国医学科学院薬物研究所 Use of effective fraction of alkaloid originating from mulberry branch for preparing hypoglycemic medicine

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