JPH04210645A - Antiulcer agent - Google Patents
Antiulcer agentInfo
- Publication number
- JPH04210645A JPH04210645A JP2409692A JP40969290A JPH04210645A JP H04210645 A JPH04210645 A JP H04210645A JP 2409692 A JP2409692 A JP 2409692A JP 40969290 A JP40969290 A JP 40969290A JP H04210645 A JPH04210645 A JP H04210645A
- Authority
- JP
- Japan
- Prior art keywords
- ulcer
- rice
- extract
- product
- present
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000003699 antiulcer agent Substances 0.000 title claims abstract description 20
- 235000007164 Oryza sativa Nutrition 0.000 claims abstract description 32
- 235000009566 rice Nutrition 0.000 claims abstract description 32
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 22
- 239000003960 organic solvent Substances 0.000 claims abstract description 12
- 240000007594 Oryza sativa Species 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 abstract description 32
- 231100000397 ulcer Toxicity 0.000 abstract description 32
- 241000209094 Oryza Species 0.000 abstract description 31
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract description 21
- 230000000694 effects Effects 0.000 abstract description 20
- 208000000718 duodenal ulcer Diseases 0.000 abstract description 10
- 206010042220 Stress ulcer Diseases 0.000 abstract description 9
- 210000002784 stomach Anatomy 0.000 abstract description 9
- 230000003449 preventive effect Effects 0.000 abstract description 7
- 239000003795 chemical substances by application Substances 0.000 abstract description 5
- 238000001914 filtration Methods 0.000 abstract description 2
- 238000000227 grinding Methods 0.000 abstract description 2
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- 238000010298 pulverizing process Methods 0.000 abstract 1
- 238000000605 extraction Methods 0.000 description 20
- 241000699670 Mus sp. Species 0.000 description 11
- 239000003814 drug Substances 0.000 description 11
- 241000700159 Rattus Species 0.000 description 10
- 238000007654 immersion Methods 0.000 description 10
- 238000000034 method Methods 0.000 description 10
- 238000007920 subcutaneous administration Methods 0.000 description 10
- 241000699666 Mus <mouse, genus> Species 0.000 description 9
- 239000004480 active ingredient Substances 0.000 description 9
- 229940079593 drug Drugs 0.000 description 9
- 239000002504 physiological saline solution Substances 0.000 description 9
- 230000000767 anti-ulcer Effects 0.000 description 6
- 238000003809 water extraction Methods 0.000 description 6
- 235000013305 food Nutrition 0.000 description 5
- 239000000243 solution Substances 0.000 description 5
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 4
- 229920002472 Starch Polymers 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- 230000002496 gastric effect Effects 0.000 description 4
- 210000001156 gastric mucosa Anatomy 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 235000019698 starch Nutrition 0.000 description 4
- 239000008107 starch Substances 0.000 description 4
- 239000004382 Amylase Substances 0.000 description 3
- 102000013142 Amylases Human genes 0.000 description 3
- 108010065511 Amylases Proteins 0.000 description 3
- 239000003513 alkali Substances 0.000 description 3
- 235000019418 amylase Nutrition 0.000 description 3
- 238000009835 boiling Methods 0.000 description 3
- 238000011160 research Methods 0.000 description 3
- 238000000638 solvent extraction Methods 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 241000196324 Embryophyta Species 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 230000002354 daily effect Effects 0.000 description 2
- 210000004051 gastric juice Anatomy 0.000 description 2
- 230000000762 glandular Effects 0.000 description 2
- 230000035876 healing Effects 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 229940043274 prophylactic drug Drugs 0.000 description 2
- 235000020083 shōchū Nutrition 0.000 description 2
- 235000021419 vinegar Nutrition 0.000 description 2
- 239000000052 vinegar Substances 0.000 description 2
- HMUNWXXNJPVALC-UHFFFAOYSA-N 1-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]-2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)C(CN1CC2=C(CC1)NN=N2)=O HMUNWXXNJPVALC-UHFFFAOYSA-N 0.000 description 1
- 208000030453 Drug-Related Side Effects and Adverse reaction Diseases 0.000 description 1
- YBHQCJILTOVLHD-YVMONPNESA-N Mirin Chemical compound S1C(N)=NC(=O)\C1=C\C1=CC=C(O)C=C1 YBHQCJILTOVLHD-YVMONPNESA-N 0.000 description 1
- 101100489867 Mus musculus Got2 gene Proteins 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 208000007107 Stomach Ulcer Diseases 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 235000021329 brown rice Nutrition 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000027119 gastric acid secretion Effects 0.000 description 1
- 238000007429 general method Methods 0.000 description 1
- 210000004013 groin Anatomy 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 239000005457 ice water Substances 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 229930014626 natural product Natural products 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 235000011837 pasties Nutrition 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 235000019992 sake Nutrition 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000017423 tissue regeneration Effects 0.000 description 1
- 210000002417 xiphoid bone Anatomy 0.000 description 1
Landscapes
- Cereal-Derived Products (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
Description
［０００１１ [00011
【産業上の利用分野］本発明は、米からの水抽出物また
は有機溶媒抽出物をそのまま、あるいはこれを含有した
ものを用いることにより、経口投与においても、皮下矧
与においても潰瘍を予防および治癒する効果をもつ抗潰
瘍剤に関するものである。
［０００２］
【従来の技術】従来、米は主食以外に、清酒、焼酎、封
酒、みりん、酢、麹などとして用途開発され、古くから
生活に欠かせないものとなっている。この他には、美容
的用途として糠袋が知られている。これは、米を単なる
主食であるとみるか、またはせいぜい澱粉源としてしか
みていなかったということによるものであると思われる
。また、糠袋にしても、皮膚に良いとされ、慣例的にそ
のまま使用されていたのみであり、有効成分という概念
もなければ、抽出という考え方も全くなかったのである
。
［０００３］一方、現在は日常生活においてストレス時
代といわれ、生活環境の目まぐるしい変化、対人関係の
複雑化により、ストレスを受けることが多くなってきて
いる。また、従来、自然に存在しなかったものを数多く
摂取する機会も多くなってきた。
［０００４］そこで、これらの要因により、胃潰瘍、十
二指腸潰瘍などに悩まされている人が多くなり、現在で
はさまざまな抗潰瘍剤が開発利用されている。現在使用
されている抗潰瘍剤をみると、大別して胃液の消化力抑
制剤、胃液分泌抑制剤、粘膜保護組織修復剤などがあり
、経口投与または皮下投与されている。しかし、これら
のいずれの製剤も、単離された薬剤または合成された薬
剤であり、それぞれに副作用があり、使用対象および使
用量についての制限が厳しくなっており、有効で、しか
も、安全な抗潰瘍剤は開発利用されていない。
［０００５］このため、これらの抗潰瘍剤は、安全性の
点から常用できないので、予防とか、再発防止には利用
できていない。一方、潰瘍の予防薬としては、整腸剤と
か、胃酸の分泌抑制効果を持つ薬剤を用いているだけで
あり、これらも予防薬とはいえない。
［０００６］[Industrial Application Field] The present invention uses a water extract or an organic solvent extract from rice as it is or a product containing the same to prevent and prevent ulcers both by oral administration and by subcutaneous administration. This invention relates to an anti-ulcer agent that has a healing effect. [0002] Conventionally, in addition to being a staple food, rice has been developed for uses such as sake, shochu, hofushu, mirin, vinegar, and koji, and has been an indispensable part of daily life since ancient times. In addition to this, bran bags are also known for their cosmetic uses. This seems to be due to the fact that rice was viewed simply as a staple food, or at best as a source of starch. Furthermore, even when it was made into a rice bran bag, it was said to be good for the skin and was just used as is, and there was no concept of it being an active ingredient, nor was there any concept of extraction. [0003] On the other hand, we are currently living in an age of stress in our daily lives, and people are increasingly experiencing stress due to rapid changes in their living environment and the increasing complexity of interpersonal relationships. In addition, there are now many opportunities to ingest many things that have not traditionally existed naturally. [0004] Due to these factors, many people are suffering from gastric ulcers, duodenal ulcers, etc., and various anti-ulcer agents have now been developed and utilized. Anti-ulcer agents currently in use can be broadly classified into gastric juice digestive power suppressants, gastric juice secretion suppressants, and mucosal protective tissue repair agents, which are administered orally or subcutaneously. However, all of these preparations are isolated or synthesized drugs, each with their own side effects, and there are strict restrictions on who can use them and how much they can be used. Ulcer agents have not been developed or utilized. [0005] For this reason, these anti-ulcer agents cannot be used regularly from the viewpoint of safety, and therefore cannot be used for prevention or prevention of recurrence. On the other hand, as prophylactic drugs for ulcers, only intestinal regulating agents and drugs that have the effect of suppressing gastric acid secretion are used, and these cannot be called preventive drugs either. [0006]
【発明が解決しようとする課題】現在、薬剤の人体に対
する副作用が問題となっており、天然物で全く副作用が
なく、シかも、予防薬、再発防止薬として常用しても十
分に安全である抗潰瘍効果を持つ薬剤が要求されている
。本発明は、抗潰瘍効果に優れ、安全で安価であり、し
かも、予防薬、再発防止薬として常用しても、全く安全
な米からの天然抗潰瘍剤を提供することを目的とするも
のである。
［０００７］[Problem to be solved by the invention] Currently, the side effects of drugs on the human body are a problem, and it is a natural product that has no side effects at all and is sufficiently safe to be used regularly as a preventive drug or a drug to prevent recurrence. There is a need for drugs with anti-ulcer effects. The object of the present invention is to provide a natural anti-ulcer agent derived from rice that has excellent anti-ulcer effects, is safe and inexpensive, and is completely safe even when used regularly as a prophylactic drug or anti-recurrence drug. be. [0007]
【課題を解決するための手段】本発明者らは、動植物合
印すの観点から、主食である米を中心に種々の植物成分
の研究を進めてきた。その過程で、米には今まで予測で
きなかった数多くの可能性、効果があることが判明して
きた。そこで、主食として用いられ安全性が最も高いこ
とが実証されている米をテーマとしてとりあげ、米の総
合利用研究を行ってきた。そのうちの一つのテーマとし
て、米からの抗潰瘍剤について鋭意研究を本ねできた。
その過程で、米の抽出物をそのまま、あるいはこれを含
有するものを経口および皮下投与したところ、どちらの
場合も非常に顕著な抗潰瘍作用があることが判明し、本
発明を完成するに至った。
［０００８］すなわち、本発明は、米からの水抽出物ま
たは有機溶媒抽出物をそのまま、あるいはこれを含有し
てなることを特徴とする抗潰瘍剤であって、米を水抽出
（酸、アルカリ抽出も含む）またはアルコールなどの有
機溶媒で抽出することにより、簡単安価に、しかも、全
く安全に上記の効果を顕す非常に優れた抗潰瘍剤が得ら
れるのである。
［０００９１抽出を行う場合、まず、米を粉砕または粉
体化すると表面積が大きくなるため、きわめて抽出効率
が良好となる。この方法は１．粉砕機または精米機等を
用い、一般的な方法によればよい。粉砕しなくてもよい
が、この場合には、未組織の分解および抽出に長時間を
要する。
［００１０１水抽出に当たっては、米をそのまま、好ま
しくは粉砕または粉体化したものに加水する。米は玄米
でも白米でもよい。加水量については、米に対して２〜
５倍量で効率よく抽出されるが、収率、作業性、最終使
用目的等に応じて適宜選定すればよい。この後、加温し
てゆき、沸騰状態になった時点で抽出を完了する。
［００１１１抽出を完了した後、使用目的により、圧搾
、濾過を行えば、清澄な抽出エキスが得られる。なお、
最初から熱水を加えて抽出を行ってもよい。
［００１２］水抽出の際の抽出温度は、抽出液中の有効
成分が解明されていないが、この未知の有効成分が熱に
安定であることは確認できたので、高温が効率的である
。低温でも長時間おけば、充分に抽出を行うことができ
る。ただし、４０℃以下の低温の場合は、ｐＨを酸性あ
るいはアルカリ性にするか、防腐剤を加えることが必要
である。抽出時間は、沸騰抽出の場合には数分でよいが
、それ以下の中温の場合には数時間から一昼夜が必要で
ある。低温の場合は、米の粉砕状態にもよるが、数日〜
１ケ月必要である。ただし、この場合にも、なるべく最
後には加熱するのがより効果的である。
［００１３］水抽出の場合に最も問題になるのは、糊化
現象である。糊状になれば、抽出効率が悪くなるのみで
なく、実作業においては困難を極める。これを防ぐため
には、アミラーゼを加えて反応させるか、塩酸などで酸
性にして澱粉を分解すればよく、この方法を用いること
により、充分に解決でき、実用上も全く問題がない。
［００１４］抽出液中の有効成分は、酸、アルカリに安
定であるためか、酸抽出あるいはアルカリ抽出を行うの
も有効である。また、水抽出の場合、酸、アルカリで前
処理するか、米の組織に働く酵素（例えば、アミラーゼ
）を反応させて前処理を行い、抽出する方法が効果的で
ある。これは、前処理により、有効成分がより抽出され
やすくなるためであると思われる。
［００１５］さらに、有機溶媒抽出でも、本効果を持っ
たエキスが抽出されることが判明した。このことは、有
効成分の解明を進める上で、また、有効成分をコンクに
抽出したり、水に溶けないものとの配合という利用用途
の上できわめて有効である。この場合、なるべく微粉砕
または粉体化することが好ましい。また、ここで用いる
有機溶媒は、アルコールのような人体に投与しても安全
なものを使用することが望ましい。
［００１６］なお、本発明品の米からの抽出には、以上
のように有機溶媒抽出または水抽出し、その抽出物中の
有効成分をさらに溶媒抽出すると、より有効である。し
かし、これは、濃縮状態が得られたためと思われ、澱粉
などの不用なものを除いたり、濃縮することにより、同
等の効果が得られる。
［００１７］米は主食として毎日食べており、あまりに
も身近すぎて、このような抗潰瘍剤として使用するとい
う概念すらなく、思いもよらないことであった。また、
食べる以外には清酒、焼酎、酢などに用いられてきたが
、米の抽出という考え方も方法も取られていない。これ
は、抽出しようとすると米の特性として糊状になり、Ｃ
従来の考え方では非常に困難であったことにもよるもの
と思われる。そのため、本発明においては、有機溶媒抽
出、酸、アルカリ抽出などを用い、また、水抽出の場合
、アミラーゼなどを作用させ、抽出を容易にすることに
より、目的を達成することができるようにしたのである
。
［００１８］このようにして十分抽出操作を行って初め
て、非常に優れた抗潰瘍剤としての有効成分を抽出する
ことができるのである。
［００１９］この本発明品の抗潰瘍剤としての効果をみ
るために、まず、拘束水浸ストレス潰瘍に対する本発明
品の経口投与においての効果を調べた。その方法は、渡
辺らの方法に準じて行った。すなわち、８週齢のｄｄＹ
系雄性マウスを２４時間絶食後、実施例１により得た本
発明品を０． ３ｍｌ／マウス経口投与し、３０分後に
ストレスゲージに入れ、１５℃の水中に剣状突起まで浸
し、拘束水浸ストレスを負荷した。５時間後に頚椎脱臼
して層殺し、胃を摘出した。その後、１％ホルマリン溶
液１、 ５ｍｌを胃内に注入し、さらに、同液中に浸す
ことにより胃組織を軽く固定し、２４時間そのまま放置
した。
その後、大変に添って切開し、腺胃部に発生した損傷の
長さ（ｍｍ）を測定し、−匹当たりのその総和を潰瘍係
数として表した。また、コントロールとしては、ストレ
スゲージに入れる３０分前に同量の生理食塩水を経口投
与したものを用いた。マウスは各々１５匹ずつで行った
。
その結果を示すと[Means for Solving the Problems] The present inventors have been conducting research on various plant ingredients, centering on rice, which is a staple food, from the viewpoint of animal and plant identification. In the process, it has become clear that rice has many possibilities and effects that were previously unforeseen. Therefore, we have been conducting research on the comprehensive use of rice, which is used as a staple food and has been proven to be the safest. As one of these themes, I was able to conduct intensive research on anti-ulcer agents derived from rice. During this process, when we administered the rice extract directly or contained it orally and subcutaneously, we discovered that it had a very pronounced anti-ulcer effect in both cases, which led us to complete the present invention. Ta. [0008] That is, the present invention is an anti-ulcer agent characterized by containing a water extract or an organic solvent extract from rice as is or containing the water extract or organic solvent extract from rice. By extracting with an organic solvent such as alcohol (including extraction) or using an organic solvent such as alcohol, an excellent anti-ulcer agent that exhibits the above-mentioned effects can be obtained easily, inexpensively, and completely safely. [00091 When performing extraction, first of all, if the rice is crushed or powdered, the surface area becomes larger, so the extraction efficiency becomes extremely good. This method is 1. It may be carried out by a general method using a crusher, a rice mill, or the like. Grinding may not be necessary, but in this case it takes a long time to break down and extract the unstructured material. [00101 In water extraction, water is added to the rice as it is, preferably to the crushed or powdered rice. The rice may be brown rice or white rice. Regarding the amount of water added, 2~
Although 5 times the amount can be extracted efficiently, the amount may be appropriately selected depending on the yield, workability, final use purpose, etc. After this, the mixture is heated and the extraction is completed when it reaches a boiling state. [00111] After completing the extraction, a clear extracted extract can be obtained by squeezing or filtering depending on the purpose of use. In addition,
Extraction may be performed by adding hot water from the beginning. [0012] Regarding the extraction temperature during water extraction, although the active ingredients in the extract have not been elucidated, it has been confirmed that this unknown active ingredient is stable to heat, so a high temperature is efficient. Even at low temperatures, if left for a long time, sufficient extraction can be achieved. However, in the case of low temperatures below 40°C, it is necessary to make the pH acidic or alkaline, or to add a preservative. The extraction time may be several minutes in the case of boiling extraction, but in the case of lower temperature extraction, several hours to a day and night are required. If the temperature is low, it will last for several days, depending on how the rice is ground.
One month is required. However, even in this case, it is more effective to heat the mixture at the end if possible. [0013] The most problematic issue in water extraction is the gelatinization phenomenon. If it becomes pasty, not only will the extraction efficiency deteriorate, but it will also be extremely difficult in actual work. In order to prevent this, it is sufficient to add amylase to the reaction or to acidify the starch with hydrochloric acid to decompose the starch. By using this method, the problem can be solved satisfactorily and there is no practical problem at all. [0014] Perhaps because the active ingredients in the extract are stable to acids and alkalis, it is also effective to perform acid extraction or alkali extraction. In addition, in the case of water extraction, it is effective to perform pretreatment with an acid or alkali, or to react with an enzyme (for example, amylase) that acts on the rice tissue, followed by extraction. This seems to be because the pretreatment makes it easier to extract the active ingredient. [0015] Furthermore, it has been found that an extract having this effect can also be extracted by organic solvent extraction. This is extremely effective in further elucidating the active ingredients, and in applications such as extracting the active ingredients into concrete or blending them with substances that are insoluble in water. In this case, it is preferable to pulverize or powder it as much as possible. Further, as the organic solvent used here, it is desirable to use one that is safe even when administered to the human body, such as alcohol. [0016] In order to extract the product of the present invention from rice, it is more effective to perform organic solvent extraction or water extraction as described above, and then further solvent extract the active ingredients in the extract. However, this is probably due to the fact that a concentrated state was obtained, and the same effect can be obtained by removing unnecessary substances such as starch or by concentrating it. [0017] Rice is eaten every day as a staple food and is so familiar to us that there was no concept of using it as such an anti-ulcer agent, and it was completely unexpected. Also,
In addition to eating, it has been used to make sake, shochu, vinegar, etc., but the concept and method of extracting rice has not been used. When you try to extract this, it becomes sticky due to the characteristics of rice, and C
This is probably due to the fact that it was extremely difficult to do so using conventional thinking. Therefore, in the present invention, the purpose can be achieved by using organic solvent extraction, acid, alkali extraction, etc., and in the case of water extraction, by applying amylase etc. to facilitate extraction. It is. [0018] Only by performing the extraction operation sufficiently in this manner can it be possible to extract the active ingredient as an extremely excellent anti-ulcer agent. [0019] In order to examine the effect of the present invention product as an anti-ulcer agent, first, the effect of oral administration of the present invention product on restrained water immersion stress ulcers was investigated. The method was carried out according to the method of Watanabe et al. That is, 8 week old ddY
After fasting male mice for 24 hours, the product of the present invention obtained in Example 1 was added to 0. 3 ml/mouse was orally administered, and 30 minutes later, the mouse was placed in a stress gauge and immersed up to the xiphoid process in water at 15°C to apply restraint water immersion stress. Five hours later, the cervical vertebrae were dislocated and the stomach was removed. Thereafter, 1.5 ml of a 1% formalin solution was injected into the stomach, and the gastric tissue was lightly fixed by immersing it in the same solution and left as it was for 24 hours. Thereafter, an incision was made along the groin, and the length (mm) of the damage caused in the glandular stomach was measured, and the sum total per animal was expressed as the ulcer index. As a control, the same amount of physiological saline was orally administered 30 minutes before being placed in the stress gauge. Fifteen mice were used for each test. Showing the results
【表１】のとおりである。 ［００２０１It is as shown in [Table 1]. [00201
【表１］ 本発明品の経口投与における拘束水浸ストレ
ス潰瘍マウスに対する有効性
投与量ムｌ／マウス）
検体数
潰瘍係数の平均
生理食塩水
０．３
６５．４
本発明品
０．３
２９．１
［００２１］
【表１】のように、コントロールとして生理食塩水を投
与したマウスにおける潰瘍係数の平均が６５．４である
のに対して、本発明品を投与したマウスにおける潰瘍係
数の平均は２９．１となり、明らかに本発明品は、経口
投与することにより拘束水浸ストレス潰瘍に対する抗潰
瘍剤として有効であることが判明した。この結果、本発
品は、胃腸粘膜から直接に作用して抗潰瘍剤として有効
な効果を示すことが判明した。
［００２２］次に、拘束水浸ストレス潰瘍に対する本発
明品の皮下投与においての効果を調べた。その方法は、
経口投与の場合と同様に、渡辺らの方法に準じて行った
。実施例１により得た本発明品を０． ３ｍｌ／マウス
皮下投与したもの、および生理食塩水を０． ３ｍｌ／
マウス皮下投与したちの各々１５匹について、３０分放
置後、ストレスゲージに入れ、拘束水浸ストレスを負荷
し、本発明品を皮下投与することによる拘束水浸ストレ
ス潰瘍に対する有効性を５べた。その結果を示すと[Table 1] Effectiveness of oral administration of the product of the present invention on restrained water immersion stress ulcer mice (dose ml/mouse) Number of samples Average ulcer coefficient of physiological saline 0.3 65.4 Product of the present invention 0.3 29. 1 [0021] As shown in [Table 1], the average ulcer index in mice administered with physiological saline as a control was 65.4, whereas the average ulcer index in mice administered with the product of the present invention was 65.4. 29.1, clearly demonstrating that the product of the present invention is effective as an anti-ulcer agent for restrained water immersion stress ulcers when administered orally. As a result, it was found that the product of the present invention acts directly on the gastrointestinal mucosa and exhibits an effective effect as an anti-ulcer agent. [0022] Next, the effect of subcutaneous administration of the product of the present invention on restraint water immersion stress ulcers was investigated. The method is
As in the case of oral administration, it was performed according to the method of Watanabe et al. The product of the present invention obtained in Example 1 was 0. 3 ml/mouse subcutaneously administered, and 0.0 ml/mouse of physiological saline. 3ml/
After being left for 30 minutes, each of the 15 mice administered subcutaneously was placed in a stress gauge and subjected to restraint water immersion stress to evaluate the effectiveness of subcutaneously administering the product of the present invention against restraint water immersion stress ulcers. Showing the results
【表
２】のとおりである５
［００２３］As shown in [Table 2]5 [0023]
【表２】 本発明品の皮下投与におけ令、拘束水浸スト
レス潰瘍マウスに対する有効性
投与量（ｍｌ／マウス）
検体数
潰瘍係数の平均
生理食塩水
０．３
４３．０
本発明品
０．３
２２．７
［００２４］[Table 2] Effective dose (ml/mouse) of subcutaneous administration of the product of the present invention for age-restricted water immersion stress ulcerated mice (ml/mouse) Number of samples Average ulcer coefficient of saline 0.3 43.0 Product of the present invention 0. 3 22.7 [0024]
【表２】のように、生理食塩水を０． ３ｍｌ／マウス
皮下投与したものにおける１５匹の潰瘍係数の平均は４
３゜Ｏ１本発明品を０． ３ｍｌ／マウス皮下投与した
ものにおけるマウス１５匹の潰瘍係数の平均は２２．７
であり、本発明品を皮下投与することにより抗潰瘍剤と
して有効であることが明らかになった。
［００２５］このように皮下投与することにより、本発
明品が抗潰瘍剤として有効な抗潰瘍性を示したことは、
本発明品が胃粘膜に直接的に効果を有するだけではなく
、血液を通して根本的に防ぐという効果をも合わせ持っ
ているということがいえる。
［００２６１以上の結果より、本発明品は、ストレス性
の潰瘍に対して、経口投与においても、皮下投与におい
ても有効であるということが判明した。
［００２７１次に、胃粘膜に直接作用しておこる潰瘍の
一つであるエタノール性の潰瘍に対する本発明品の抗潰
瘍剤としての有効性を経口投与において調べた。ストレ
ス潰瘍に対して、本発明品が経口投与においても、皮下
投与においても有効であることが判明しているので、こ
こでは経口投与の場合のみ行った。エタノール潰瘍はＲ
Ｏｂｅｒｔらの方法に準じて行った。すなわち、８週齢
のＷｉＳｔａｒ／ＳＴ系雄性ラットを２４時間絶食、１
６時間絶氷水後実施例２によって得られた本発明品５ｇ
を生理食塩水１０ｍ１に溶かしたものを１． ０ｍｌ／
ラット経口投与し、その３０分後、１００％エタノール
を１． ０ｍｌ／ラット経口投与し、その３０分後、頚
椎脱臼して層殺し、胃を摘出した。その後、１％ホルマ
リン溶液１０ｍ１を胃内に注入し、さらに、同液中に浸
し、胃組織を軽く固定し、マウスの場合と同様に腺胃部
に発生した潰瘍の総和を潰瘍係数として測定した。また
、この場合も、コントロールとして生理食塩水を経口投
与したものを用いた。
ここでラットは各々１５匹で行った。その結果を示すと
As shown in [Table 2], 0.0% physiological saline was added. The average ulcer index of 15 mice after subcutaneous administration of 3 ml/mouse was 4.
3゜O1 The product of the present invention at 0. The average ulcer index of 15 mice after subcutaneous administration of 3 ml/mouse was 22.7.
It was revealed that subcutaneous administration of the product of the present invention is effective as an anti-ulcer agent. [0025] The fact that the product of the present invention showed effective anti-ulcer properties as an anti-ulcer agent by subcutaneous administration as described above
It can be said that the product of the present invention not only has a direct effect on the gastric mucosa, but also has the effect of fundamentally preventing gastric mucosa through blood. [00261 From the above results, it was found that the product of the present invention is effective against stress-induced ulcers both when administered orally and when administered subcutaneously. [00271]Next, the effectiveness of the product of the present invention as an anti-ulcer agent against ethanol-induced ulcers, which is one type of ulcer caused by direct action on the gastric mucosa, was investigated by oral administration. Since the product of the present invention has been found to be effective against stress ulcers both by oral administration and by subcutaneous administration, only oral administration was conducted here. Ethanol ulcer is R
It was carried out according to the method of Obert et al. Specifically, 8-week-old WiStar/ST male rats were fasted for 24 hours,
5 g of the product of the present invention obtained in Example 2 after 6 hours of ice water
1. Dissolved in 10ml of physiological saline. 0ml/
Rats were orally administered, and 30 minutes later, 100% ethanol was administered once. 0 ml/rat was orally administered, and 30 minutes later, the cervical vertebrae were dislocated, the layers were removed, and the stomach was removed. Thereafter, 10 ml of 1% formalin solution was injected into the stomach, and the stomach tissue was lightly fixed by immersion in the same solution, and the sum of ulcers generated in the glandular stomach was measured as the ulcer index, as in the case of mice. . Also in this case, as a control, physiological saline was orally administered. Here, 15 rats were used for each experiment. Showing the results
【表３］のとおりである。
［００２８］
【表３】 本発明品の経口投与におけるエタノール潰瘍
ラットマウスに対する抗潰瘍性
検体数
潰瘍係数の平均
投与量−１７ラツト）
生理食塩水
１．０
４８．１
本発明品溶液
１．０
１９．１
［００２９］It is as shown in [Table 3]. [0028] [Table 3] Anti-ulcer properties of oral administration of the product of the present invention to rat mice with ethanol ulcers Average dose of the number of specimens and ulcer coefficient - 17 rats) Physiological saline 1.0 48.1 Solution of the present invention 1.0 19.1 [0029]
【表３】のように、コントロールとして生理食塩水を１
、 ０ｍｌ／ラット経口投与したラットにおける潰瘍係
数の平均は４８．１であるのに対して、本発明品１．
０ｐａｌ／ラツトを経口投与したラットにおける潰瘍係
数の平均は１９，１であり、本発明品は、胃粘膜に直接
作用しておこるエタノール潰瘍に対しても有効な抗潰瘍
剤であることが判明した。
［００３０１これらの結果より、本発明品は、有効では
あるが、胃腸に傷害を与えるような医薬品と併用するこ
とにより、それらの薬剤からの胃腸保護剤としても有効
である。
［００３１１なお、米糠の不鹸化物中に含まれていると
されるオリザノールは、実施例１〜３により得られた本
発明品中には、高速液体クロマトグラフによる分析結果
において、いずれも含まれていなかった。
［００３２１以上のとおり、本発明品が経口投与および
皮下投与において、間接的潰瘍の代表としての拘束水浸
ストレス潰瘍に対して有効であること、および直接的潰
瘍の代表としてのエタノール潰瘍に対して有効であると
いう結果より、本発明品が潰瘍全般に有効であり、治療
薬としても、予防薬としても有効であり、経口および皮
下投与においても巾広く利用できることが判明した。
［００３３］As shown in [Table 3], physiological saline was added as a control.
The average ulcer index in rats to which 0 ml/rat was orally administered was 48.1, whereas the inventive product 1.
The average ulcer index in rats to which 0pal/rat was orally administered was 19.1, indicating that the product of the present invention is an effective anti-ulcer agent even for ethanol ulcers caused by direct action on the gastric mucosa. . [00301] From these results, the product of the present invention is effective, but when used in combination with drugs that cause gastrointestinal damage, it is also effective as a gastrointestinal protectant from those drugs. [00311 It should be noted that oryzanol, which is said to be contained in the unsaponifiables of rice bran, was not found in any of the products of the present invention obtained in Examples 1 to 3 in the analysis results by high performance liquid chromatography. It wasn't. [00321 As described above, the product of the present invention is effective against restraint water immersion stress ulcers, which are representative of indirect ulcers, and ethanol ulcers, which are representative of direct ulcers, when administered orally and subcutaneously. The results show that the product of the present invention is effective against ulcers in general, is effective both as a therapeutic agent and a preventive agent, and can be widely used for oral and subcutaneous administration. [0033]
【発明の効果】本発明品は、間接的な潰瘍（ストレス潰
瘍）および胃に直接作用する潰瘍（エタノール潰瘍）い
ずれにも顕著な効果を示す。しかも、経口投与において
も、皮下投与においても多大の効果があることは、実用
上内服用にも注射用にもどちらにも利用できるものであ
り、巾広い用途が見込まれる。このように顕著な抗潰瘍
作用を持つものが、２０００年来安全性が実証されてい
る米から簡単安価に得られたことは画期的なことである
。
［００３４］これにより、治癒効果だけでなく、常用し
ても−切問題がないことから、潰瘍の予防効果を合わゼ
もち、予防医学の面でも非常に優れた事績になるととも
に、潰瘍をわずらった人の再発防止という観点からも、
これらの人々にとって大きい福音となるものである。
［００３５］Effects of the Invention The product of the present invention shows remarkable effects on both indirect ulcers (stress ulcers) and ulcers that directly affect the stomach (ethanol ulcers). Furthermore, the fact that it is highly effective both in oral administration and subcutaneous administration means that it can be practically used for both oral administration and injection, and is expected to have a wide range of uses. It is epoch-making that a substance with such remarkable anti-ulcer effects could be easily and inexpensively obtained from rice, whose safety has been proven for 2000 years. [0034] As a result, it not only has a healing effect but also has an ulcer preventive effect even when used regularly, and is an excellent achievement in terms of preventive medicine. From the perspective of preventing recurrence for those who have experienced it,
This is great news for these people. [0035]
【実施例】実施例１
白米１５ｋｇをよく粉砕し、これに６０℃の温水４５１
と液化酵素５０ｇを加え、よく攪拌した。その後、徐々
に温度を上げてゆき、５分間煮沸抽出した後、３０℃ま
で冷却した。その後、しぼり機でしぼり、圧搾液４１１
を得た。
［００３６］実施例２
実施例１により得た圧搾液８００ｍ１を冷凍乾燥し、１
１１．７５ｇの冷凍乾燥品を得た。
［００３７］実施例３
白米１ｋｇをよく粉砕し、９５％アルコール３１を添加
し、よく攪拌して放置した。４日後、しぼり機でしぼり
、圧搾液２．５１と残渣１． ２ｋｇを得た。この圧搾
液に５００ｍ１加水し、ロータリーエバポレーターによ
りアルコールを完全に除去し、本発明品５０ｍ１を得た
。[Example] Example 1 Thoroughly crush 15 kg of polished rice and add 45 kg of warm water at 60°C.
and 50 g of liquefied enzyme were added and stirred well. Thereafter, the temperature was gradually raised, and after boiling and extraction for 5 minutes, the mixture was cooled to 30°C. After that, squeeze it with a squeezing machine and press liquid 411
I got it. [0036] Example 2 800 ml of the squeezed liquid obtained in Example 1 was freeze-dried, and 1
11.75 g of freeze-dried product was obtained. [0037] Example 3 1 kg of polished rice was thoroughly ground, 95% alcohol 31 was added thereto, and the mixture was stirred well and left to stand. After 4 days, it was squeezed using a squeezing machine, and the squeezed liquid was 2.51 g and the residue was 1.5 g. I got 2 kg. 500 ml of water was added to this squeezed liquid, and alcohol was completely removed using a rotary evaporator to obtain 50 ml of a product of the present invention.
Claims (1)
そのまま、あるいはこれを含有してなることを特徴とす
る抗潰瘍剤。Claims: 1. An anti-ulcer agent comprising a water extract or an organic solvent extract from rice as is or containing the same.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP40969290A JP3550403B2 (en) | 1990-12-11 | 1990-12-11 | Anti-ulcer agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP40969290A JP3550403B2 (en) | 1990-12-11 | 1990-12-11 | Anti-ulcer agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH04210645A true JPH04210645A (en) | 1992-07-31 |
| JP3550403B2 JP3550403B2 (en) | 2004-08-04 |
Family
ID=18518995
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP40969290A Expired - Lifetime JP3550403B2 (en) | 1990-12-11 | 1990-12-11 | Anti-ulcer agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3550403B2 (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0616810A1 (en) * | 1993-02-19 | 1994-09-28 | SOKEN Co., Ltd. | Anti-cancer agent |
| EP0620007A1 (en) * | 1993-02-16 | 1994-10-19 | SOKEN Co., Ltd. | Anti-ulcer agent |
| US5728384A (en) * | 1993-02-16 | 1998-03-17 | Soken Co., Ltd. | Antiulcer agent |
| KR20010104425A (en) * | 2000-04-27 | 2001-11-26 | 안봉환 | Composition with anti-ulcer activity comprising extracts of glutinous rice and raw ginseng |
| WO2008117996A1 (en) * | 2007-03-27 | 2008-10-02 | Dasan M & F, Inc. | Anti-peptic ulcer composition in the form of clear liquid comprising glutinous rice extract and tea extract |
| JP2011516467A (en) * | 2008-04-02 | 2011-05-26 | ダサン エムアンドエフ，アイエヌシー． | Anti-peptic ulcer composition containing rice prolamin |
-
1990
- 1990-12-11 JP JP40969290A patent/JP3550403B2/en not_active Expired - Lifetime
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0620007A1 (en) * | 1993-02-16 | 1994-10-19 | SOKEN Co., Ltd. | Anti-ulcer agent |
| US5728384A (en) * | 1993-02-16 | 1998-03-17 | Soken Co., Ltd. | Antiulcer agent |
| EP0616810A1 (en) * | 1993-02-19 | 1994-09-28 | SOKEN Co., Ltd. | Anti-cancer agent |
| KR20010104425A (en) * | 2000-04-27 | 2001-11-26 | 안봉환 | Composition with anti-ulcer activity comprising extracts of glutinous rice and raw ginseng |
| WO2008117996A1 (en) * | 2007-03-27 | 2008-10-02 | Dasan M & F, Inc. | Anti-peptic ulcer composition in the form of clear liquid comprising glutinous rice extract and tea extract |
| JP2011516467A (en) * | 2008-04-02 | 2011-05-26 | ダサン エムアンドエフ，アイエヌシー． | Anti-peptic ulcer composition containing rice prolamin |
Also Published As
| Publication number | Publication date |
|---|---|
| JP3550403B2 (en) | 2004-08-04 |
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