JP2004149494A - Capsinoid-containing composition - Google Patents
Capsinoid-containing composition Download PDFInfo
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- JP2004149494A JP2004149494A JP2002319341A JP2002319341A JP2004149494A JP 2004149494 A JP2004149494 A JP 2004149494A JP 2002319341 A JP2002319341 A JP 2002319341A JP 2002319341 A JP2002319341 A JP 2002319341A JP 2004149494 A JP2004149494 A JP 2004149494A
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Abstract
Description
【0001】
【発明の属する技術分野】
本発明は、血圧上昇または脈拍増加を回避すべき者に対して安全にカプサイシノイドの生理活性による効果を発揮させるための、カプシノイドを有効成分とする組成物に関する。
【0002】
【従来の技術】
トウガラシ(Capsicum属)の果実は、食品、香辛料および医薬品原料として広く利用されている。その辛味成分は、カプサイシン、ジヒドロカプサイシンなど12種類以上の同族体からなる一群の物質であり、カプサイシノイドと総称される。これまでに、カプサイシノイドは様々な生理活性、例えば、アドレナリンの分泌促進に基づくエネルギー代謝の亢進によって肥満抑制をもたらす等の作用を有していることが知られている(例えば、非特許文献1または2参照)しかし、カプサイシノイドは同時に血圧上昇作用および脈拍増加作用も有しており、血圧の上昇または脈拍の増加を回避しなければならない者、典型的には高血圧症や動脈硬化症に代表される心臓血管系の疾患ならびに腎疾患を有する患者あるいは、かかる疾患に罹患している可能性の高い者は、カプサイシノイドの有利な生理活性を有効に利用できないでいた。
【0003】
【非特許文献1】バック(Buck SH)ら著、ファーマコロジカル レビュー(Pharmacol.Rev.)、発行国:アメリカ合衆国、発行所:American Society for Pharmacology and Experimental Therapeutics,Danvers,Mass.、1986年、38巻、p.179−226。
【非特許文献2】岩井和夫、渡辺達夫編、「トウガラシ 辛味の科学」、幸書房、2000年1月、p.148−227。
【0004】
【発明が解決しようとする課題】
本発明は、カプサイシノイドに認められる有利な生理活性を享受しつつ、同時にカプサイシノイドの持つ血圧上昇または脈拍増加という危険性を有しない、新たな経口組成物(食品および医薬を含む)を提供することを目的とする。
【0005】
【課題を解決するための手段】
本発明者らは、カプシノイドと称されるカプサイシノイド類似物質が、カプサイシノイドに認められる有利な生理活性を有しつつ、同時にカプサイシノイドの持つ血圧上昇または脈拍増加という特徴を有しない化合物であることを見出し、本発明を完成した。
【0006】
すなわち、本発明はカプシノイドを含む血圧上昇または脈拍増加を回避すべき者のための経口組成物である。
【0007】
カプシノイドとは、バニリルアルコールに脂肪酸がエステル結合した化合物の総称であり、バニリルアミンに脂肪酸が酸アミド結合したカプサイシノイドとは構造を異にする化合物群である(Kobata K et al.J.Agricultural and Food Chemistry 1998,46,1695−1697)。特に、カプシノイドは、タイ国で食用に栽培されているトウガラシ辛味品種「CH−19辛」(京都府立大学農学部野菜園芸学研究室導入番号)の自殖後代から京都大学実験圃場にて選抜固定された無辛味品種「CH−19甘」(品種登録番号第10375号)に確認される。この品種は、通常のカプサイシノイドを殆ど含まず、下式で表されるカプシノイドを多量に含んでいる(矢澤ら、園芸学会雑誌、58巻、601−607頁、1989年)。
【0008】
【化2】
【0009】
この化合物は、カプサイシノイドと同様のエネルギー代謝促進作用および肥満抑制作用、免疫賦活作用などの他、鎮痛作用、持久力向上作用、抗掻痒作用、血糖値抑制作用などを有することが知られている(特許第3345744号公報、特開2001−26538号公報参照)。しかし、この化合物は、体内に接種された場合でも、血圧の上昇も脈拍の増加ももたらさないことがヒトによる臨床試験において明らかとなった。
【0010】
従って、かかるカプシノイドを血圧上昇または脈拍増加を回避すべき者に接種させれば、血圧の上昇または脈拍の増加というリスクを伴うことなく、カプサイシノイドと同様の上記有用性、代表的にはエネルギー代謝促進効果などを享受することができる。特に、血圧上昇または脈拍増加を回避すべき疾患に罹患している者の多くは、運動療法を受けることができない状況にあることがしばしばであり、エネルギー代謝促進効果を安全に得られるという本発明のもつ意義は大きいものとなる。
【0011】
本発明が好適に利用され得る疾患としては、高血圧症、肥満症、糖尿病、不整脈、うっ血性心不全、肝硬変肝疾患、腎疾患、甲状腺機能亢進症、副腎皮質疾患、副腎髄質疾患、またはこれらに起因する合併症などが挙げられる。これらは、その原因や詳細な症状によりさらに細分化され得るが、いずれの場合においても、血圧の上昇あるいは脈拍の増加がその疾患において好ましくない生理現象である限り、本発明の好適な対象となる。特に、肥満はそれ自体が疾患と認識されるよりは、むしろ種々の疾患を誘発する原因とも言えるものであり、またいわゆる現代人にあっては深刻な問題となっていることから、本発明のもたらす意義は極めて重要である。なお、本発明は、医師による診断の結果として上記各種の疾患に罹患していると判断された者のみならず、自覚症状的にかかる疾患に罹患している可能性が高いと認められる者の他、自発的に血圧上昇または脈拍増加を回避しようとする者に対しても、安全に使用することのできる組成物である。
【0012】
さらに、本発明におけるカプシノイドは、カプサイシノイドと異なり辛味を有していないために、子供から老人に至るまで、また性差の区別や辛味への嗜好の有無に関係なく、有効量を確実に摂取することができる点でも有利な素材である。
【0013】
【発明の実施の形態】
本発明において使用されるカプシノイドは、辛味成分であるカプサイシノイドを殆ど含まないトウガラシ無辛味品種から調製することができる。特に本発明において好ましいカプシノイド化合物は、トウガラシ品種「CH−19甘」(品種登録番号第10375号)の青果から、特開2002−226445号公報に開示された方法に従って抽出し、利用することができる。また、本発明は、このカプシノイドを、収穫したトウガラシの青果をそのままの形態としても、乾燥、粉砕等の適当な加工を施した形態としても実施することができる。また、食事の際にトウガラシあるいはその加工食品として摂取してもよく、乾燥粉末をカプセルに封入または適切な賦形剤と混合して打錠して、これらを固形健康食品あるいは医薬品として服用してもよい。また、本発明におけるカプシノイドあるいは該成分を含む適当な形態の原料を水などの適当な溶媒に溶解または懸濁させて、液剤として服用してもよい。この場合において、本発明の組成物を調製する際に使用される各種賦形剤、生理活性有効成分、その他の成分は、本発明の効果を打ち消す作用を有するものを除く他は特に制限なく使用することができる。
【0014】
本発明において使用するカプシノイドを含む種々の形態の組成物を調製する方法においても格別の制限はなく、特開2002−114676号、特開2001−158738号、特開2001−26538号などで開示される方法ならびに形態を採用することができる。
【0015】
このようにして、本発明のカプシノイドを含有する調理品あるいはトウガラシ品種「CH−19甘」の乾燥粉末や抽出物を利用した食品用または医薬用経口組成物を容易に調製することができ、これらを摂取することによりカプシノイドの作用に基づくエネルギー代謝の活性化作用、肥満抑制作用、持続運動における持久力増進等の各種生理活性作用を発揮させることができる。
【0016】
使用量としては、一日当たり、カプシノイドとして0.001〜6mg/kg体重、好ましくは0.01〜0.6mg/kg体重が服用量の目安である。
【0017】
【実施例】
次に、実施例を挙げて本発明をさらに具体的に説明するが、実施例は本発明を何等限定するものではない。
【0018】
実施例
22−26才の健康な男女9名を被験者とし、ヘルシンキ宣言によるガイドラインに基づいて実験内容を十分に説明したあと、被験者全員から実験の同意書を得た。同一の被験者に対し、体重1kg当たり0.1gの「CH−19甘(無辛味品種のトウガラシ)」、「Cayenne Long Slim(辛味品種のトウガラシ)」および対照の「California Wander(無辛味品種のピーマン)」の3種類をそれぞれ別々の日に食べさせて、これらの果実の摂食が心拍数と血圧に及ぼす影響を調べた。これらの果実は、収穫後数時間以内に−20℃に凍結保存し、実験の直前に流水により解凍して被験者に食べさせた。
【0019】
日内変動の影響を避けるため、実験は毎回16:00に開始し、測定開始の3時間前から摂食、摂水を禁止した。1セットの測定時間は8分間とし、この時間内に心拍数と血圧の両者を測定した。測定は合計9セット連続して行った。各セット8分の測定時間のうち、最初の5分間は心拍数を測定し、残りの3分間は休憩とした。血圧は、この3分間の休憩時間内(9回)と測定開始直前の合計10回測定した。最初の2セットは各果実を摂食する前の安静状態における測定とし、2セット後の休憩中(血圧測定後)に果実を摂食した。
【0020】
CH−19甘摂取群、Cayenne Long Slim摂取群およびCalifornia Wander摂取群の群間について、測定時間ごとに心拍数と最高血圧の有意差検定をDunnett法により多重比較した。果実を摂食する前の各人の安静状態における測定値2回分の平均値をゼロとして、各時点の増減値を表示した。
【0021】
心拍数については、Cayenne Long Slim摂取群は摂取後8〜16分後に対照のCalifornia Wander摂取群との間に有意差が認められた。これに対して、CH−19甘摂取群は対照のCalifornia
Wander摂取群との間に有意差が認められなかった(図1)。
【0022】
また、最高血圧についても心拍数の場合と同様に、Cayenne LongSlim摂取群は摂取後8〜56分後に対照のCalifornia Wander摂取群との間に有意差が認められたが、CH−19甘摂取群は対照のCalifornia Wander摂取群との間に有意差が認められなかった(図2)。
【0023】
【発明の効果】
本発明の組成物は心拍数上昇作用および血圧上昇作用を有さないため、高血圧症や動脈硬化症患者などの、血圧上昇または脈拍増加を回避しなければならない者であっても安心して摂取し、カプサイシノイドと同等の効果を享受することができる。
【図面の簡単な説明】
【図1】図1は、本発明の組成物を摂取したときの心拍数変化を示す。
【図2】図2は、本発明の組成物を摂取したときの血圧変化を示す。[0001]
TECHNICAL FIELD OF THE INVENTION
The present invention relates to a composition containing capsinoid as an active ingredient for safely exerting the effect of capsaicinoid's physiological activity on those who should avoid an increase in blood pressure or pulse.
[0002]
[Prior art]
Capsicum fruit is widely used as a food, spice and pharmaceutical ingredient. The pungent component is a group of substances composed of 12 or more homologs such as capsaicin and dihydrocapsaicin, and is generally called capsaicinoid. To date, capsaicinoids are known to have various physiological activities, for example, an effect of causing obesity suppression by enhancing energy metabolism based on promotion of adrenaline secretion (for example,
[0003]
[Non-Patent Document 1] Pharmacologic Review (Pharmacol. Rev.), published by the United States, published by the American Society for Pharmacology and Experimental Therapeutics, Danvers. 1986, 38, p. 179-226.
[Non-Patent Document 2] Kazuo Iwai and Tatsuo Watanabe, eds., "The Science of Hot Pepper", Koshobo, January 2000, p. 148-227.
[0004]
[Problems to be solved by the invention]
The present invention provides a novel oral composition (including food and medicine) that enjoys the advantageous physiological activity of capsaicinoid and does not have the risk of increasing blood pressure or increasing the pulse of capsaicinoid. Aim.
[0005]
[Means for Solving the Problems]
The present inventors have found that a capsaicinoid-like substance called capsinoid is a compound having the advantageous physiological activity observed in capsaicinoids, but at the same time not having the characteristics of increasing blood pressure or increasing the pulse rate of capsaicinoids, The present invention has been completed.
[0006]
That is, the present invention is an oral composition containing capsinoids for those who should avoid increasing blood pressure or increasing pulse.
[0007]
Capsinoids are a general term for compounds in which a fatty acid is ester-bonded to vanillyl alcohol, and a group of compounds having a different structure from capsaicinoids in which a fatty acid is acid-amide bonded to vanillylamine (Kobata K et al. J. Agricultural and Food). Chemistry 1998, 46, 1695-1697). In particular, capsinoids are selected and fixed in the experimental field of Kyoto University from the self-progeny of the pepper spicy variety “CH-19 hot” (introduced in the Kyoto Prefectural University Faculty of Agriculture, Vegetable Horticultural Laboratory) cultivated in Thailand for food. It is identified as a non-spicy variety “CH-19 sweet” (various registration number 10375). This variety hardly contains ordinary capsaicinoids and contains a large amount of capsinoids represented by the following formula (Yazawa et al., Journal of Horticultural Society, Vol. 58, pp. 601-607, 1989).
[0008]
Embedded image
[0009]
This compound is known to have an energy metabolism-promoting action, an obesity-suppressing action, an immunostimulatory action, and the like, as well as an analgesic action, an endurance-improving action, an antipruritic action, a blood sugar level-suppressing action, and the like (the same as capsaicinoid) See Japanese Patent No. 3345744 and JP-A-2001-26538). However, it has been shown in human clinical trials that this compound, even when inoculated in the body, does not cause an increase in blood pressure or pulse.
[0010]
Therefore, if such a capsinoid is inoculated to a person who should avoid an increase in blood pressure or pulse, the same usefulness as capsaicinoid, typically energy promotion, without the risk of an increase in blood pressure or pulse. The effect can be enjoyed. In particular, many of those suffering from diseases in which an increase in blood pressure or pulse should be avoided are often unable to receive exercise therapy, and the present invention provides a safe energy metabolism promoting effect. Has a great significance.
[0011]
The diseases to which the present invention can be preferably used include hypertension, obesity, diabetes, arrhythmia, congestive heart failure, liver cirrhosis, renal disease, hyperthyroidism, adrenal cortical disease, adrenal medulla disease, or caused by these. Complications. These can be further subdivided according to the cause or detailed symptom, but in any case, as long as an increase in blood pressure or an increase in pulse is an unfavorable physiological phenomenon in the disease, it is a suitable object of the present invention. . In particular, obesity is a cause of various diseases rather than being recognized as a disease itself, and is a serious problem for so-called modern people. The significance of bringing is extremely important. In addition, the present invention is not only for those who are determined to be suffering from the above-mentioned various diseases as a result of diagnosis by a doctor, but also for those who are highly likely to suffer from such a disease subjectively. In addition, it is a composition that can be used safely even for those who voluntarily try to avoid an increase in blood pressure or pulse.
[0012]
Furthermore, since the capsinoids of the present invention do not have pungency unlike capsaicinoids, it is necessary to ensure that an effective amount is taken from children to the elderly, regardless of gender differences and preference for pungency. It is also an advantageous material in that it can be used.
[0013]
BEST MODE FOR CARRYING OUT THE INVENTION
The capsinoid used in the present invention can be prepared from a pepper-free pungent variety that hardly contains capsaicinoid as a pungent component. Particularly preferred capsinoid compounds in the present invention can be extracted from fruits and vegetables of pepper variety "CH-19 sweet" (variety registration number: 10375) according to the method disclosed in JP-A-2002-226445 and used. . In addition, the present invention can be carried out in the form of the capsinoid in the form of harvested pepper fruits and vegetables as it is, or in a form subjected to appropriate processing such as drying and pulverization. Also, it may be ingested as a pepper or its processed food at the time of meal, and the dry powder is encapsulated or mixed with an appropriate excipient and tableted, and these are taken as a solid health food or pharmaceutical. Is also good. In addition, the capsinoid or the raw material in an appropriate form containing the component according to the present invention may be dissolved or suspended in an appropriate solvent such as water and taken as a liquid. In this case, various excipients, physiologically active ingredients, and other components used in preparing the composition of the present invention are used without any particular limitation except for those having an effect of negating the effects of the present invention. can do.
[0014]
The method for preparing various forms of compositions containing capsinoids used in the present invention is not particularly limited, and is disclosed in JP-A-2002-114676, JP-A-2001-158738, JP-A-2001-26538 and the like. Methods and configurations can be employed.
[0015]
In this way, it is possible to easily prepare an oral composition for food or medicine using a dry powder or an extract of a cooked product or a pepper variety "CH-19 sweet" containing the capsinoid of the present invention. By ingesting it, various physiological activities such as activation of energy metabolism based on the action of capsinoids, obesity suppression, and endurance enhancement in continuous exercise can be exerted.
[0016]
As a dose, 0.001 to 6 mg / kg body weight, preferably 0.01 to 0.6 mg / kg body weight as a capsinoid per day is a standard of the dose.
[0017]
【Example】
Next, the present invention will be described more specifically with reference to examples. However, the examples do not limit the present invention in any way.
[0018]
Example 22 Nine healthy males and females aged 26 to 26 were given subjects, and the contents of the experiment were sufficiently explained based on the guidelines according to the Declaration of Helsinki. For the same subject, 0.1 g / kg body weight of "CH-19 sweet (capsicum of a non-pungent variety)", "Cayenne Long Slim" (capsicum of a pungent variety) and control "California Wander (pepper of a non-pungent variety) )) Were fed on different days, and the effect of eating these fruits on heart rate and blood pressure was examined. These fruits were cryopreserved at −20 ° C. within a few hours after harvest, thawed with running water immediately before the experiment, and fed to the subjects.
[0019]
In order to avoid the influence of circadian fluctuation, the experiment was started at 16:00 every time, and eating and drinking were prohibited 3 hours before the start of the measurement. The measurement time of one set was 8 minutes, and both the heart rate and the blood pressure were measured during this time. The measurement was performed continuously for a total of 9 sets. Heart rate was measured for the first 5 minutes of each set of 8 minutes, and rest was taken for the remaining 3 minutes. The blood pressure was measured 10 times in total during the 3-minute rest period (9 times) and immediately before the start of measurement. The first two sets were measured in a resting state before eating each fruit, and the fruits were eaten during a break after the two sets (after blood pressure measurement).
[0020]
For the CH-19 sweet intake group, the Cayenne Long Slim intake group and the California Wander intake group, a significant difference test between heart rate and systolic blood pressure was multiple-compared by the Dunnett method at each measurement time. Before and after eating the fruit, the average value of two measured values in the resting state of each person was set to zero, and the increase / decrease value at each time point was displayed.
[0021]
Regarding the heart rate, a significant difference was observed between the group taking the Cayenne Long Slim and the group taking the
No significant difference was observed between the group and the Wander intake group (FIG. 1).
[0022]
Also, as in the case of heart rate, a significant difference was observed between the Cayenne LongSlim group and the control
[0023]
【The invention's effect】
Since the composition of the present invention does not have a heart rate increasing effect and a blood pressure increasing effect, it can be safely taken even by those who need to avoid an increase in blood pressure or pulse, such as patients with hypertension or arteriosclerosis. Thus, the same effect as that of capsaicinoid can be enjoyed.
[Brief description of the drawings]
FIG. 1 shows the change in heart rate when the composition of the present invention is ingested.
FIG. 2 shows the change in blood pressure when the composition of the present invention was ingested.
Claims (9)
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WO2011096413A1 (en) | 2010-02-03 | 2011-08-11 | 花王株式会社 | Agent for improving motility function |
WO2011096414A1 (en) | 2010-02-03 | 2011-08-11 | 花王株式会社 | Mitochondrial function improver |
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