JP2007145724A - Endurance improver - Google Patents

Endurance improver Download PDF

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JP2007145724A
JP2007145724A JP2005338405A JP2005338405A JP2007145724A JP 2007145724 A JP2007145724 A JP 2007145724A JP 2005338405 A JP2005338405 A JP 2005338405A JP 2005338405 A JP2005338405 A JP 2005338405A JP 2007145724 A JP2007145724 A JP 2007145724A
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endurance
fatigue
nootkaton
food
foods
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JP4719556B2 (en
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Yoshihiko Minegishi
慶彦 峯岸
Takatoshi Murase
孝利 村瀬
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Kao Corp
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Kao Corp
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Priority to US11/480,504 priority patent/US20070054965A1/en
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Priority to US13/008,086 priority patent/US8829057B2/en
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Abstract

<P>PROBLEM TO BE SOLVED: To provide a highly safe and easily available endurance improver and anti-fatigue agent having rich history of use in foods and even excellent processability. <P>SOLUTION: The endurance improver and anti-fatigue agent comprise nootkatone as an active ingredient. A food and drink, etc., having endurance improving effects and anti-fatigue effects on sports and broadly-defined exercises including activities of daily life and labors are provided by using a highly safe natural product material having the rich history of use in foods. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

本発明は、運動及び日常の動作及び労働を含む広義の運動に対する持久力向上剤、抗疲労剤に関する。   The present invention relates to an endurance improver and an anti-fatigue agent for exercise in a broad sense including exercise and daily activities and labor.

持久力は、競技的な運動のみでなく、労働をはじめとし、歩く、立つ等の日常のすべての動作についても必要不可欠なものである。つまり日常生活を有意義に、健康的に過ごすためには持久力は極めて重要であるといえる。しかし、近年では、高齢社会の進展や交通手段の発達や情報・通信技術の発展に伴い、運動不足による持久力の低下が問題となっている。また、今後高齢化社会の到来と共に、運動機能の低下は一層大きな問題になると考えられる。持久力を向上させるには、運動をすることが適切であるといえるが、忙しさのため十分な運動をする時間がとれないことや、身体の事情により、運動がしたくてもできないといった人達が多いのが現状である。   Endurance is indispensable not only for competitive exercises but also for daily activities such as labor, walking, standing and so on. In other words, endurance is extremely important for a meaningful and healthy life. However, in recent years, with the progress of an aging society, the development of transportation means and the development of information / communication technology, a decrease in endurance due to lack of exercise has become a problem. In addition, with the arrival of an aging society in the future, the decline in motor function will be a bigger problem. It can be said that exercise is appropriate to improve endurance, but people who cannot do enough exercise due to their busyness or who cannot exercise due to physical circumstances There are many current situations.

これらの問題を解決する一つの手段として、持久力向上や抗疲労作用を有する食品成分を日常的に摂取することが考えられる。例えば、本発明者らは、カテキンを摂取することによる持久力向上効果を見出した(特許文献1)。その他の持久力向上効果を有する成分として報告されている例は、サンザシ抽出物(特許文献2)や霊芝成分(特許文献3)、プロアントシアニジン及びリコペン(特許文献4)等が挙げられる。また、抗疲労作用を有する成分の例としては、コエンザイムQ10、カルニチン配合物(特許文献5)やグルタミンペプチド(特許文献6)等が挙げられる。   As one means for solving these problems, it is conceivable to ingest food components having endurance improvement and anti-fatigue action on a daily basis. For example, the present inventors have found an endurance improvement effect by ingesting catechin (Patent Document 1). Examples of other reported components having endurance enhancing effects include hawthorn extract (Patent Document 2), ganoderma component (Patent Document 3), proanthocyanidins and lycopene (Patent Document 4). Examples of the component having anti-fatigue action include coenzyme Q10, a carnitine compound (Patent Document 5), a glutamine peptide (Patent Document 6), and the like.

ヌートカトンは、4,4a,5,6,7,8−ヘキサヒドロ−6−イソプロペニル−4,4a−ジメチル−2(3H)−ナフタレノンなるセスキテルペンケトンであり、グレープフルーツ果皮等に存在し、グレープフルーツの特徴的な香味を有するため香料としては非常に注目されている物質であるが(非特許文献1)、これまでその生理作用についてはほとんど報告されていない。また、グレープフルーツに関しては、グレープフルーツオイル(精油)を含有する香料組成物が、交感神経系を活性化することにより、抗肥満作用を示すこと(特許文献7)、グレープフルーツオイルを含有する皮膚外用剤(特許文献8)が報告されている。しかし、ヌートカトンが持久力をはじめとする運動能力、疲労に対して与える影響については、これまで全く知られていない。   Nootkaton is a sesquiterpene ketone, 4,4a, 5,6,7,8-hexahydro-6-isopropenyl-4,4a-dimethyl-2 (3H) -naphthalenone, present in grapefruit peels, Although it has a characteristic flavor, it is a substance that has attracted a great deal of attention as a fragrance (Non-patent Document 1), but its physiological action has hardly been reported so far. As for grapefruit, a perfume composition containing grapefruit oil (essential oil) exhibits an anti-obesity action by activating the sympathetic nervous system (Patent Document 7), and a skin external preparation containing grapefruit oil (Patent Document 7) Patent Document 8) has been reported. However, the effects of Noot Katon on endurance, athletic performance, and fatigue have never been known.

特開2005−89384号公報JP 2005-89384 A 特開平8−47381号公報JP-A-8-47381 特開平5−123135号公報JP-A-5-123135 特開2005−334022号公報Japanese Patent Laying-Open No. 2005-334022 特開2005−97161号公報JP-A-2005-97161 特開2005−97162号公報JP-A-2005-97162 特開2002−193824号公報JP 2002-193824 A 特開2005−47935号公報JP-A-2005-47935 荒井綜一編、「最新 香料の事典」、第1版、朝倉書店、2000年5月10日、p.112、p.254Arai Junichi, “Latest Perfume Encyclopedia”, 1st edition, Asakura Shoten, May 10, 2000, p.112, p.254

本発明は、食経験が豊富であり安全性が高く、入手が容易で加工性にも優れた持久力向上剤、抗疲労剤及びそれを含有する飲食品を提供することに関する。   The present invention relates to providing endurance improvers, anti-fatigue agents, and foods and drinks containing them, which have abundant food experience, are highly safe, are easily available, and are excellent in processability.

本発明者らは、持久力向上において有効な成分の探索を行った結果、食経験が豊富で安全性が高い天然物素材の中から、グレープフルーツ果皮等に存在し、グレープフルーツの特徴的な香気成分であるヌートカトンに持久力向上効果があり、持久力向上剤、抗疲労剤として有用であることを見出した。   As a result of searching for an effective component in improving endurance, the present inventors have found that it is present in grapefruit peels, etc. from among natural products with abundant food experience and high safety, and a characteristic aroma component of grapefruit It was found that Nootkaton, which has the effect of improving endurance, is useful as an endurance improver and anti-fatigue agent.

すなわち本発明は、ヌートカトンを有効成分とする持久力向上剤、及び抗疲労剤を提供するものである。   That is, the present invention provides an endurance improver and an anti-fatigue agent containing nootkatone as an active ingredient.

また、本発明はヌートカトンを含有し、持久力向上効果を有することを特徴とし、持久力向上のために用いるものである旨の表示を付した飲料又は食品、及びヌートカトンを含有し、抗疲労効果を有することを特徴とし、抗疲労のために用いるものである旨の表示を付した飲料又は食品を提供するものである。   Further, the present invention is characterized in that it contains nootkaton and has an effect of improving endurance, and contains beverages or foods labeled as being used for improving endurance, and nootkaton, and has an anti-fatigue effect. It is characterized by having a drink, or a food with an indication that it is used for anti-fatigue.

本発明によれば、食経験が豊富で安全性が高い天然物素材を用いた、運動及び日常の動作及び労働を含む広義の運動に対する持久力向上、抗疲労効果を有する飲食品等が提供される。   ADVANTAGE OF THE INVENTION According to this invention, the foodstuffs etc. which have the endurance improvement with respect to the exercise in a broad sense including exercise and daily operation | movement and labor using the natural product material with rich food experience and high safety, an anti-fatigue effect, etc. are provided. The

本発明において、ヌートカトンとは、4,4a,5,6,7,8−ヘキサヒドロ−6−イソプロペニル−4,4a−ジメチル−2(3H)−ナフタレノンなるセスキテルペンケトンをいう。当該ヌートカトンには、8種類の光学異性体が存在する。本発明においては、それら異性体を単独又は混同して用いることができるが、次の構造式(I)で表される(+)−ヌートカトンを用いるのが好ましい。   In the present invention, nootkatone refers to a sesquiterpene ketone of 4,4a, 5,6,7,8-hexahydro-6-isopropenyl-4,4a-dimethyl-2 (3H) -naphthalenone. There are eight types of optical isomers in the Nootkaton. In the present invention, these isomers can be used alone or confused, but (+)-Nootkatone represented by the following structural formula (I) is preferably used.

本発明で用いるヌートカトンは、公知の有機化学的合成、微生物を用いた合成等により製造することができ、例えば、特開2004−123561公報、特開2003−250591公報、特表平11−501052公報に記載の方法により得ることができる。   Nootkatone used in the present invention can be produced by known organic chemical synthesis, synthesis using microorganisms, and the like. For example, JP 2004-123561 A, JP 2003-250591, JP 11-501052 A. It can obtain by the method of description.

また、本発明で用いるヌートカトンは、ヌートカトンを含有する天然物から公知の方法により抽出することにより得ることもできる。ここで、抽出は、例えば、水、熱水、アルコール水、有機溶剤等を用いて行う抽出操作と高速液体クロマトグラフやカラムクロマトグラフ等による精製操作や蒸留操作を適宜組み合わせて行う方法により行うことができる。ヌートカトンを含有する天然物としては、例えばグレープフルーツが挙げられる。グレープフルーツから抽出する場合、その原料としては例えば、グレープフルーツ果実、グレープフルーツ果皮、グレープフルーツオイル、グレープフルーツ濃縮果汁、グレープフルーツ果汁搾汁後の残渣等を用いることができる。   Moreover, the nootkaton used by this invention can also be obtained by extracting by a well-known method from the natural product containing a nootkaton. Here, the extraction is performed by a method in which, for example, an extraction operation performed using water, hot water, alcohol water, an organic solvent, or the like is combined with a purification operation or a distillation operation using a high performance liquid chromatograph or a column chromatograph as appropriate. Can do. Examples of natural products containing nootkaton include grapefruit. When extracting from grapefruit, the raw material can be, for example, grapefruit fruit, grapefruit peel, grapefruit oil, grapefruit concentrated fruit juice, residues after squeezing grapefruit juice, and the like.

上記合成や抽出により得られるヌートカトンは、単数又は複数工程の精製等により夾雑物が除かれた高純度のものを用いることが好ましいが、本発明の効果を奏する限り粗精製物であってもよい。また、ヌートカトンを比較的多く含有することが知られる、グレープフルーツ精油を用いることも出来る。   The nootkatone obtained by the above synthesis or extraction is preferably a high purity product from which impurities are removed by single or multiple step purification, but may be a crude product as long as the effects of the present invention are exhibited. . Grapefruit essential oil, which is known to contain a relatively large amount of nootkaton, can also be used.

本発明の持久力向上剤は、ヒト及び動物に投与することができる他、各種飲食品、医薬品、ペットフード等に配合して摂取することができる。食品としては、持久力向上及び疲労の予防、改善等の生理機能をコンセプトとし、その旨を表示した機能性飲食品、病者用飲食品、特定保健用食品に応用できる。飲料の形態は特に限定されないが、例えば、果汁飲料、炭酸飲料、茶系飲料、乳飲料、アルコール飲料、清涼飲料等、あらゆる飲料に配合可能である。また、ゼリー状食品や各種スナック類、焼き菓子、ケーキ類、チョコレート、ガム、飴、スープ類等、あらゆる食品形態で配合し、持久力向上食品、抗疲労食品として用いることが可能である。医薬品として使用する場合は、例えば、錠剤、顆粒剤等の経口用固形製剤や、内服液剤、シロップ剤等の経口用液体製剤とすることができる。   The endurance improver of the present invention can be administered to humans and animals, and can be ingested by being mixed with various foods, medicines, pet foods and the like. The food is based on the concept of physiological functions such as improving endurance and preventing or improving fatigue, and can be applied to functional foods, foods for the sick, and foods for specified health use. Although the form of a drink is not specifically limited, For example, it can mix | blend with all drinks, such as a fruit juice drink, a carbonated drink, a tea-type drink, a milk drink, an alcoholic drink, a soft drink. Moreover, it can mix | blend with all food forms, such as jelly-like foodstuffs, various snacks, baked confectionery, cakes, chocolate, gum, candy, and soups, and it can be used as an endurance food and anti-fatigue food. When used as a pharmaceutical, for example, oral solid preparations such as tablets and granules, and oral liquid preparations such as oral liquids and syrups can be used.

尚、経口用固形製剤を調製する場合には、本発明のヌートカトンに賦形剤、必要に応じて結合剤、崩壊剤、滑沢剤、着色剤、矯味剤、矯臭剤等を加えた後、常法により錠剤、被覆錠剤、顆粒剤、散剤、カプセル剤等を製造することができる。また、経口用液体製剤を調製する場合は、矯味剤、緩衝剤、安定化剤、矯味剤等を加えて常法により内服液剤、シロップ剤、エリキシル剤等を製造することができる。   When preparing an oral solid preparation, after adding an excipient, if necessary, a binder, a disintegrant, a lubricant, a colorant, a corrigent, a corrigent, etc. to the nootkaton of the present invention, Tablets, coated tablets, granules, powders, capsules and the like can be produced by conventional methods. Moreover, when preparing a liquid preparation for oral use, a liquid preparation, a syrup, an elixir, etc. can be manufactured by a conventional method by adding a corrigent, a buffer, a stabilizer, a corrigent and the like.

これらのものに対するヌートカトンの配合量は、その使用形態により異なるが、飲食品やペットフード等の形態では、通常0.0002〜5質量%、更に0.001〜3質量%、特に0.02〜2質量%とするのが好ましい。医薬品、例えば錠剤、顆粒剤、カプセル剤等の経口用固形製剤、内服液剤、シロップ剤等の経口用液体製剤等として用いる場合には、通常0.01〜95質量%、更に0.1〜95質量%、特に2〜80質量%とするのが好ましい。   Although the compounding quantity of Nootkaton with respect to these things changes with the usage forms, in forms, such as food-drinks and pet food, it is 0.0002-5 mass% normally, Furthermore, 0.001-3 mass%, Especially 0.02- It is preferable to set it as 2 mass%. When used as pharmaceutical preparations such as oral solid preparations such as tablets, granules and capsules, oral liquid preparations such as oral liquids and syrups, etc., usually 0.01 to 95% by mass, and further 0.1 to 95%. It is preferable to set it as the mass%, especially 2-80 mass%.

本発明の持久力向上剤の投与量(有効摂取量)は、一日あたり1〜1000mg/60kg体重とするのが好ましく、特に2〜700mg/60kg体重、さらに5〜500mg/60kg体重とするのが好ましい。   The dosage (effective intake) of the endurance improving agent of the present invention is preferably 1 to 1000 mg / 60 kg body weight per day, particularly 2 to 700 mg / 60 kg body weight, more preferably 5 to 500 mg / 60 kg body weight. Is preferred.

以下に、本発明の代表的実施例を示す。
実施例1 ヌートカトンの持久力向上・抗疲労効果に対する評価
ヌートカトンの持久力向上・抗疲労効果に対する評価を下記の通り行った。尚、ヌートカトンはAvocado社製の物を用いた。
The following are representative examples of the present invention.
Example 1 Evaluation of Nootkaton for Endurance Improvement / Anti-fatigue Effect Evaluation of nootkaton for endurance improvement / anti-fatigue effect was performed as follows. In addition, the thing made from Avocado company was used for Nootkaton.

流水プールにおけるマウス限界遊泳時間測定法(参考文献:Am J Physiol Regul Integr Comp Physiol,Vol.288,R708-R715,2005)により、持久力向上・抗疲労効果の評価を行った。実験用プールは、透明なアクリル製のプール(長さ90×幅45×深さ45cm)に38cmの深さまで水を満たし、ヒーターで34℃に維持した状態で使用した。水流はポンプ(C−P60H、日立製)を用いて作り出し、流速はWater flowmeter(東京フローメータ研究所)をポンプに連結させ、バルブの開閉により調節した。また、流速は流速計(SV−101−25S、三光精密工業)で確認を行った。   Endurance improvement and anti-fatigue effects were evaluated by a method for measuring the limit swimming time of mice in a running water pool (reference: Am J Physiol Regul Integr Comp Physiol, Vol. 288, R708-R715, 2005). The experimental pool was used with a transparent acrylic pool (length 90 × width 45 × depth 45 cm) filled with water to a depth of 38 cm and maintained at 34 ° C. with a heater. The water flow was created using a pump (C-P60H, manufactured by Hitachi), and the flow rate was adjusted by connecting a water flow meter (Tokyo Flow Meter Laboratory) to the pump and opening and closing the valve. Moreover, the flow velocity was confirmed with a velocimeter (SV-101-25S, Sanko Precision Industry).

実験動物には5週齢のBalb/c系雄性マウス(チャールスリバー)を用い、一定の飼育環境下(23±2℃、明期:午前7時から午後7時)で1週間予備飼育をし、馴化を行った。その後1週間は、遊泳運動に慣れさせるためのトレーニングを週3回行った(初日に流速5L/分で30分、3日目、5日目に6L/分で30分の遊泳運動を行った)。次の1週間に、各個体を2時間絶食させた状態で、流速7L/分における限界遊泳時間(呼吸のため水面に顔を出せなくなった状態で救出した時点を限界遊泳時間とした)を2回測定した。限界遊泳時間に群間差が出ないように1群8匹で試験食群と対照食群の2群に群分けを行った。表1に示す配合組成で調製した食餌を用いて10週間飼育を行った。この間、限界遊泳時間測定(7L/分)とトレーニング(6L/分、30分)を週1回ずつ行った。飼育10週目におけるマウスの限界遊泳時間を表2に示した。   As experimental animals, 5-week-old Balb / c male mice (Charles River) were used and pre-bred for 1 week in a constant breeding environment (23 ± 2 ° C, light period: 7am to 7pm). Acclimated. After that, for one week, training was performed three times a week to get used to swimming exercise (30 minutes of swimming exercise was performed on the first day for 30 minutes at a flow rate of 5 L / min, 3 days on the third day, and 6 L / min for 30 minutes on the third day). ). In the next week, with each individual fasted for 2 hours, limit swimming time at a flow rate of 7 L / min (the limit swimming time was defined as the time when rescued in a state where the face could not be exposed due to breathing). Measured once. The group was divided into two groups, the test food group and the control food group, with 8 animals per group so that there was no difference between the groups in the limit swimming time. Using the diet prepared with the composition shown in Table 1, the animals were reared for 10 weeks. During this time, limit swimming time measurement (7 L / min) and training (6 L / min, 30 minutes) were performed once a week. Table 2 shows the limit swimming time of mice at the 10th week of breeding.

表2から、ヌートカトンを含有する試験食を摂取したマウスでは、対照食群と比較して10週間飼育後の限界遊泳時間が有意に延長しており、ヌートカトンは持久力向上効果、抗疲労効果を有することがわかる。   From Table 2, the mice that took the test meal containing nootkaton had significantly increased marginal swimming time after 10 weeks of breeding compared to the control diet group, and nootkaton has the effect of improving endurance and anti-fatigue. You can see that

実施例2 製剤例
(1)持久力向上・抗疲労用飲料
下記組成物を混合し、果汁飲料を製造した。
Example 2 Formulation Example (1) Better Endurance / Anti-fatigue Beverage The following composition was mixed to produce a fruit juice drink.

(2)持久力向上・抗疲労用カプセル剤
カプセル化剤中に下記組成物(300mg)を封入した。
(2) Endurance improvement / anti-fatigue capsule The following composition (300 mg) was encapsulated in an encapsulating agent.

(3)持久力向上・抗疲労用錠剤
下記組成物(1錠=250mg)を打錠し、錠剤を製造した。
(3) Endurance improvement / anti-fatigue tablet The following composition (1 tablet = 250 mg) was tableted to produce a tablet.

(4)持久力向上・抗疲労用顆粒剤
下記組成物(1袋=500mg)を混合し顆粒剤を製造した。
(4) Endurance improvement / anti-fatigue granule The following composition (1 bag = 500 mg) was mixed to produce a granule.

(5)持久力向上、抗疲労用食品
下記組成物(1錠=1000mg)を打錠し、チュアブルタイプのタブレット食品を製造した。
(5) Food for improving endurance and anti-fatigue The following composition (1 tablet = 1000 mg) was tableted to produce a chewable tablet food.

(6)持久力向上・抗疲労飲料
下記組成物を混合し、持久力向上・抗疲労飲料を製造した。
(6) Endurance improvement / anti-fatigue drink The following composition was mixed to produce an endurance improvement / anti-fatigue drink.

(7)持久力向上・抗疲労用カプセル剤
カプセル化剤中に下記組成物(300mg)を封入した。
(7) Capsule for improving endurance and anti-fatigue The following composition (300 mg) was encapsulated in a capsule agent.

Claims (4)

ヌートカトンを有効成分とする持久力向上剤。   An endurance improver containing nootkaton as an active ingredient. ヌートカトンを有効成分とする抗疲労剤。   Anti-fatigue agent containing nootkaton as an active ingredient. ヌートカトンを含有し、持久力向上効果を有することを特徴とし、持久力向上のために用いるものである旨の表示を付した飲料又は食品。   A beverage or food containing nout katon, characterized by having an effect of improving endurance, and having an indication that it is used for improving endurance. ヌートカトンを含有し、抗疲労効果を有することを特徴とし、抗疲労のために用いるものである旨の表示を付した飲料又は食品。   Beverages or foods that contain nootkaton and have an anti-fatigue effect, and are labeled as being used for anti-fatigue.
JP2005338405A 2005-09-05 2005-11-24 Endurance improver Expired - Fee Related JP4719556B2 (en)

Priority Applications (3)

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JP2005338405A JP4719556B2 (en) 2005-11-24 2005-11-24 Endurance improver
US11/480,504 US20070054965A1 (en) 2005-09-05 2006-07-05 AMPK activating agent
US13/008,086 US8829057B2 (en) 2005-09-05 2011-01-18 AMPK activating agent

Applications Claiming Priority (1)

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JP2005338405A JP4719556B2 (en) 2005-11-24 2005-11-24 Endurance improver

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JP2007145724A true JP2007145724A (en) 2007-06-14
JP4719556B2 JP4719556B2 (en) 2011-07-06

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010280598A (en) * 2009-06-03 2010-12-16 Kao Corp Lkb1 activator

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005137204A (en) * 2003-11-04 2005-06-02 Yutaka Miyauchi Liquid drink

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005137204A (en) * 2003-11-04 2005-06-02 Yutaka Miyauchi Liquid drink

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010280598A (en) * 2009-06-03 2010-12-16 Kao Corp Lkb1 activator

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