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JP2521196B2 - Colorectal cancer preventive composition - Google Patents

Colorectal cancer preventive composition

Info

Publication number
JP2521196B2
JP2521196B2 JP3108977A JP10897791A JP2521196B2 JP 2521196 B2 JP2521196 B2 JP 2521196B2 JP 3108977 A JP3108977 A JP 3108977A JP 10897791 A JP10897791 A JP 10897791A JP 2521196 B2 JP2521196 B2 JP 2521196B2
Authority
JP
Japan
Prior art keywords
polyphenols
colorectal cancer
composition
cancer
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.)
Expired - Lifetime
Application number
JP3108977A
Other languages
Japanese (ja)
Other versions
JPH04264027A (en
Inventor
宣行 萩原
雅也 立石
重光 赤地
武▲祚▼ 金
哲郎 山根
俊雄 高橋
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Taiyo Kagaku KK
Original Assignee
Taiyo Kagaku KK
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Filing date
Publication date
Application filed by Taiyo Kagaku KK filed Critical Taiyo Kagaku KK
Priority to JP3108977A priority Critical patent/JP2521196B2/en
Publication of JPH04264027A publication Critical patent/JPH04264027A/en
Application granted granted Critical
Publication of JP2521196B2 publication Critical patent/JP2521196B2/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Description

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

【産業上の利用分野】本発明は大腸癌予防用組成物に関
する。
TECHNICAL FIELD The present invention relates to a composition for preventing colorectal cancer.

【0004】[0004]

【従来の技術】近年、食生活の欧米化に伴い大腸癌の罹
患率が急増しており、近い将来その死亡率は胃癌を抜い
て1位を占めることが予測されている。従って、日常の
食生活において、大腸癌の予防に有効な食品の摂取を励
行することは、将来的に国民の癌死亡率を低下させるた
めに効果的な方法である。今日、大腸癌の予防に有効な
食品成分として食物繊維が挙げられているが、これの過
剰摂取は腹部の充満感や下痢を伴う等少なからず問題が
ある。
2. Description of the Related Art In recent years, the morbidity of colorectal cancer has been rapidly increasing with the westernization of eating habits, and it is predicted that the mortality rate in the near future will surpass gastric cancer and occupy the first place. Therefore, encouraging the intake of foods that are effective in preventing colorectal cancer in daily diet is an effective method for reducing the cancer mortality rate of the people in the future. Today, dietary fiber is mentioned as a food ingredient effective in preventing colorectal cancer, but excessive intake of this is not without problems, such as abdominal fullness and diarrhea.

【0005】又、茶のポリフェノール類は、動物実験に
おいて経口投与により乳腺(原ら、第43回日本癌学会
総会記事,1984年,280頁)、食道・前胃(小国
ら、日本農芸化学会誌,1990年,288頁)、十二
指腸[藤田ら、ジャパニーズジャーナルオブキャンサー
リサーチ(Japanese journal ofc
ancer research),第80巻,503〜
505頁]の発癌抑制や、20−メチルコラントレン誘
発肉腫の増殖抑制(特開昭60−190719、原ら,
日本栄養・食糧学会誌,第42巻,39〜45頁)等、
ある種の癌に予防効果を有することが最近の研究から示
唆されている。しかし、十二指腸癌以外の前記試験例に
おける投与量は、ヒトに換算すると約10g/60kg
/日以上の摂取量となり、茶のポリフェノール類が有す
る渋みを考慮にいれると、このような多量のポリフェノ
ール類を日常の生活に取り入れることは極めて困難であ
る。更に、十二指腸癌はヒトではほとんど発生しない等
の理由で、茶のポリフェノール類を癌予防の目的に利用
した例は今だ知られていない。
Tea polyphenols are orally administered to mammary glands (Hara et al., 43rd Annual Meeting of the Japanese Cancer Society, 1984, 280 pages), esophagus and forestomach (Oguni et al., Journal of the Japan Society for Agricultural Chemistry) in animal experiments. , 1990, p. 288), Duodenum [Fujita et al., Japanese Journal of Cancer Research.
ancer research), Volume 80, 503-
505] and carcinogenesis inhibition of 20-methylcholanthrene-induced sarcoma (Japanese Patent Application Laid-Open No. 60-190719, Hara et al.
Journal of Japan Society of Nutrition and Food Science, Vol. 42, 39-45), etc.
Recent studies suggest that it has a preventive effect on certain cancers. However, the dose in the above test cases other than duodenal cancer is about 10 g / 60 kg when converted to human.
The intake is more than 1 day / day, and taking into consideration the astringency of tea polyphenols, it is extremely difficult to incorporate such a large amount of polyphenols into daily life. Furthermore, because of the fact that duodenal cancer rarely occurs in humans, there are still no known examples of utilizing tea polyphenols for the purpose of cancer prevention.

【0006】[0006]

【発明が解決しようとする課題】本発明の目的は上記の
実状に鑑み、安全かつ低濃度で優れた大腸癌予防効果を
有し、日常の食生活に適宜取り入れて無理なく摂取でき
る大腸癌予防用組成物を提供することにある。
In view of the above situation, the object of the present invention is to prevent colon cancer which has a safe and low concentration and an excellent effect of preventing colorectal cancer, and which can be appropriately incorporated into daily eating habits without difficulty. The present invention provides a composition for use.

【0007】[0007]

【課題を解決するための手段】本発明者らは、前記課題
を解決するため鋭意研究を重ねた結果、茶(Camel
lia sinensis,〈L.〉O.Kuntz
e)に含まれるポリフェノール類が、意外にも低濃度で
大腸癌の予防に有効であることを見い出し、本物質を有
効成分とする安全性の高い、優れた大腸癌予防用組成物
を得ることに成功した。本発明のポリフェノール類は、
表1に示した6種類の主要な化合物よりなる。
[Means for Solving the Problems] As a result of intensive studies to solve the above problems, the present inventors have found that
lia sinensis, <L. > O. Kuntz
It was found that the polyphenols contained in e) are surprisingly effective in preventing colorectal cancer at low concentrations, and a highly safe and excellent composition for preventing colorectal cancer containing this substance as an active ingredient is obtained. succeeded in. The polyphenols of the present invention are
It consists of the six main compounds shown in Table 1.

【0008】[0008]

【表1】 [Table 1]

【0009】本発明に用いられるポリフェノール類の典
型的調製法は、本発明者等が先に出願した特許(特開昭
64−90124)に詳細に例示される。このようなポ
リフェノール類は、我々が日常飲用に供している茶の成
分として多量に含まれていることから、安全であること
は歴史的に証明されている。参考として、後述する実施
例1の方法により調製したポリフェノール類の急性毒性
試験の結果を以下に記載する。 ddy マウス雄 LD50>3000mg/kg(経口) ddy マウス雌 LD50>3000mg/kg(経口) 尚、LD50値はリッチフィールド−ウィルコクソン法
により算出した。
A typical method for preparing the polyphenols used in the present invention is illustrated in detail in the patent filed by the present inventors (Japanese Patent Laid-Open No. 64-90124). Such polyphenols are historically proven to be safe because they are contained in large amounts as ingredients of teas that we drink daily. As a reference, the results of the acute toxicity test of the polyphenols prepared by the method of Example 1 described later are described below. ddy mouse male LD 50 > 3000 mg / kg (oral) ddy mouse female LD 50 > 3000 mg / kg (oral) The LD 50 value was calculated by the Richfield-Wilcoxon method.

【0010】〈使用形態〉 本発明のポリフェノール類を有効成分として含有する大
腸癌予防用組成物は、種々の菓子類、飲料を含む食品の
形態とすることが好ましい。これらの食品を製造するの
に用いられる成分としては、使用目的、使用形態等に応
じて種々の食品素材、食品添加物が用いられる。例え
ば、着色料、甘味料、酵素、増粘安定剤、ガムベース、
被膜剤、苦味料、酸化防止剤、調味料、強化剤、製造用
剤、保存料、着香料、酸味料、油脂、結着剤、香辛料、
乳製品、穀物、精製タンパク、微生物製剤、栄養強化剤
等が適宜配合される。本発明の有効成分であるポリフェ
ノール類は、体重60kgのヒト成人に300〜600
mg/日の投与量で大腸癌予防効果を発揮する。従っ
て、1日当りの食事量と最終製品の仕上り(外観、味)
を考慮すると、本発明の大腸癌予防用組成物中のポリフ
ェノール類含有率は0.05〜0.7%が適当であり、
より好ましくは0.3〜0.5%である。0.05%未
満の場合は、本発明の大腸癌予防用組成物の多量摂取を
要し、一方、0.7%を超える場合は、最終製品の外観
と味が著しく損なわれ、本発明の「日常の食生活におい
て無理なく摂取できる」という目的を達成することは難
しくなる。又、本発明の大腸癌予防用組成物の摂取間隔
については、各人の体重に応じて算定した1日の必要量
を毎日摂取することが好ましい。
<Form of Use> The composition for preventing colorectal cancer containing the polyphenols of the present invention as an active ingredient is preferably in the form of food including various confectioneries and beverages. As a component used for producing these foods, various food materials and food additives are used depending on the purpose of use, usage form and the like. For example, colorants, sweeteners, enzymes, thickening stabilizers, gum bases,
Coating agent, bittering agent, antioxidant, seasoning, strengthening agent, manufacturing agent, preservative, flavoring agent, acidulant, oil and fat, binder, spice,
Dairy products, grains, purified proteins, microbial preparations, nutritional enhancers, etc. are appropriately mixed. The polyphenols, which are the active ingredients of the present invention, are 300 to 600 for a human adult weighing 60 kg.
It exerts a colon cancer preventive effect at a dose of mg / day. Therefore, the amount of food per day and the finish of the final product (appearance, taste)
Considering the above, the content of polyphenols in the composition for preventing colorectal cancer of the present invention is suitably 0.05 to 0.7%,
It is more preferably 0.3 to 0.5%. If it is less than 0.05%, a large amount of the composition for preventing colorectal cancer of the present invention is required, while if it exceeds 0.7%, the appearance and taste of the final product are significantly impaired. It will be difficult to achieve the purpose of "it can be taken without difficulty in the daily diet". Regarding the interval of ingestion of the composition for preventing colorectal cancer of the present invention, it is preferable to ingest the daily required amount calculated according to the weight of each person every day.

【0011】[0011]

【作用】本発明の有効成分であるポリフェノール類の作
用を、以下に試験例を挙げて詳細に説明する。 試験例1. Fisher系ラット(雄,8週齢)をオリエンタル酵
母(株)社製MF固型飼料及び水道水で飼育し、第1週
から10週までアゾキシメタン(シグマ社)を週1回、
7.4mg/kg皮下投与し、イニシエーションを行っ
た。これらのラットを3群に分け、各々対照群(26
匹)、試験群(26匹)、比較群(26匹)とした。対
照群は引き続き水道水で、試験群は実施例1のポリフェ
ノール類を0.01%含む水道水で、比較群は茶の熱水
抽出物を0.01%含む水道水で11週から26週目ま
で飼育した。又、アゾキシメタン無処理であることを除
き、上記3群と同じ条件にて飼育した群(10匹×3)
も設定した。26週後剖検し、大腸癌を検索した。腫瘍
発生率及びラット1匹当りの腫瘍数の検定には、それぞ
れスチューデントのt−検定、χ−検定を用いた。そ
の結果を表2に示す。
The action of the polyphenols which are the active ingredients of the present invention will be described in detail below with reference to test examples. Test Example 1. Fisher rats (male, 8 weeks old) were bred with MF solid feed and tap water manufactured by Oriental Yeast Co., Ltd., and azoxymethane (Sigma) once a week from week 1 to week 10.
7.4 mg / kg was subcutaneously administered to initiate the treatment. These rats were divided into 3 groups, each of which had a control group (26
Animals), a test group (26 animals), and a comparison group (26 animals). The control group was continuously tap water, the test group was tap water containing 0.01% of the polyphenols of Example 1, and the comparison group was tap water containing 0.01% hot water extract of tea for 11 to 26 weeks. It was raised to the eyes. In addition, except that it was not treated with azoxymethane, the group was raised under the same conditions as the above 3 groups (10 animals x 3)
Also set. After 26 weeks, autopsy was performed and colon cancer was searched. Student's t-test and χ 2 -test were used to test the tumor incidence and the number of tumors per rat, respectively. The results are shown in Table 2.

【0012】[0012]

【表2】 [Table 2]

【0013】尚、アゾキシメタン無処理の3群には腫瘍
発生はなかった。
No tumors developed in the 3 groups that were not treated with azoxymethane.

【0014】[0014]

【試験例2】Fisher系ラット(雄、8週齢)をオ
リエンタル酵母(株)社製MF粉末飼料及び水道水で飼
育し、第1週から10週までアゾキシメタン(シグマ
社)を週1回、7.4mg/kg皮下投与し、イニシエ
ーションを行った。これらのラットを3群に分け、各々
対照群(30匹)、試験群(30匹)、比較群(30
匹)とした。対照群は引続きMF粉末飼料で、試験群は
実施例1のポリフェノール類を0.015%含むMF粉
末飼料で、比較群は市販の抹茶を0.015%含むMF
粉末飼料で11週から26週目まで飼育した。又、アゾ
キシメタン無処理であることを除き、上記3群と同じ条
件にて飼育した群(10匹×3)も設定した。26週後
剖検し、大腸癌を検索した。腫瘍発生率及びラット1匹
当りの腫瘍数の検定には、それぞれスチューデントのt
−検定、χ−検定を用いた。その結果を表3に示す。
[Test Example 2] Fisher rats (male, 8 weeks old) were bred with Oriental Yeast Co., Ltd. MF powder feed and tap water, and azoxymethane (Sigma) once a week from week 1 to week 10. 7.4 mg / kg was subcutaneously administered to initiate the treatment. These rats were divided into 3 groups, each of which was a control group (30 animals), a test group (30 animals), and a comparison group (30 animals).
). The control group continued to be MF powder feed, the test group was MF powder feed containing 0.015% of the polyphenols of Example 1, and the comparison group was MF powder containing 0.015% of commercially available matcha.
The animals were fed with powdered feed from the 11th week to the 26th week. In addition, a group (10 animals × 3) raised under the same conditions as those of the above-mentioned three groups was also set except that it was not treated with azoxymethane. After 26 weeks, autopsy was performed and colon cancer was searched. Tumor incidence and number of tumors per rat were tested by Student's t
- test, χ 2 - using the test. Table 3 shows the results.

【0015】[0015]

【表3】 [Table 3]

【0016】尚、アゾキシメタン無処理の3群には腫瘍
発生はなかった。
No tumor was found in the three groups that had not been treated with azoxymethane.

【0017】前記試験例1、2から明らかなごとく、本
発明の有効成分であるポリフェノール類は飲水或いは食
餌中0.01〜0.015%の濃度で大腸癌を有意に抑
制することができる。この有効量を体重60kgのヒト
成人に換算すると約300〜600mg/日となり、日
常の食生活において本発明の大腸癌予防用組成物を無理
なく摂取することができる。
As is clear from Test Examples 1 and 2, polyphenols, which are the active ingredients of the present invention, can significantly suppress colon cancer at a concentration of 0.01 to 0.015% in drinking water or diet. This effective amount is about 300 to 600 mg / day when converted into a human adult with a body weight of 60 kg, and the composition for preventing colorectal cancer of the present invention can be reasonably taken in daily diet.

【0018】[0018]

【実施例】実施例1. 市販の緑茶300gに水を約3l加え時々撹拌し、75
℃で1時間抽出した。抽出液をろ過して水層を得、酢酸
エチル3lを加えて激しく撹拌後、一晩放置した。酢酸
エチル層を減圧乾固後、シリカゲルカラムクロマトグラ
フィー(8cm×70cm,1.5kg)に付し、2
0:1、次いで10:1(V/V)のクロロホルム−メ
タノールの溶媒にて順次溶出した。10:1(V/V)
のクロロホルム−メタノール溶出液を減圧乾固後、純度
93%のポリフェノール類を20g得た。尚、ポリフェ
ノール類の含量は、公定タンニン分析法をもって表し
た。
EXAMPLES Example 1. Add about 3 liters of water to 300 g of commercially available green tea, stir occasionally, and
Extracted at C for 1 hour. The extract was filtered to obtain an aqueous layer, 3 l of ethyl acetate was added, and the mixture was vigorously stirred and left overnight. The ethyl acetate layer was evaporated to dryness under reduced pressure and subjected to silica gel column chromatography (8 cm × 70 cm, 1.5 kg).
Elution was performed sequentially with a solvent of 0: 1 and then 10: 1 (V / V) of chloroform-methanol. 10: 1 (V / V)
The chloroform-methanol eluate of was dried under reduced pressure to obtain 20 g of polyphenols having a purity of 93%. The content of polyphenols was expressed by the official tannin analysis method.

【0019】実施例2.コーヒー乳飲料 脱脂乳860mlを35℃に加温後、砂糖39.9g、
コーヒーシロップ97g、カラメル2g、香料1g、実
施例1のポリフェノール類4gを撹拌しながら順次加
え、ポリフェノール類を0.4%含むコーヒー乳飲料を
作製した。実施例3.クッキーバター120gをクリー
ミングし、砂糖119g及び実施例1のポリフェノール
類2.4gを加えて十分クリーミングする。これに全卵
50gを加えてさらにクリーミングし、予め混合してお
いた小麦粉302g、重曹1.35g、クエン酸0.6
8gを加え、軽く混合して生地とする。生地を絞り袋に
入れて成形、160℃、12分間焙焼しポリフェノール
類を0.4%含むクッキーを作成した。
Example 2. Coffee milk drink After heating 860 ml of skim milk to 35 ° C., 39.9 g of sugar,
97 g of coffee syrup, 2 g of caramel, 1 g of flavor, and 4 g of the polyphenols of Example 1 were sequentially added with stirring to prepare a coffee milk beverage containing 0.4% of polyphenols. Example 3. 120 g of cookie butter is creamed, 119 g of sugar and 2.4 g of the polyphenols of Example 1 are added and sufficiently creamed. To this, 50 g of whole eggs was added and further creamed, and 302 g of flour mixed in advance, 1.35 g of baking soda and 0.6 of citric acid were mixed.
Add 8g and mix gently to make dough. The dough was put in a squeezing bag, molded, and baked at 160 ° C. for 12 minutes to prepare a cookie containing 0.4% of polyphenols.

【0020】[0020]

【発明の効果】前記試験例から明らかなごとく、本発明
の大腸癌予防用組成物は優れた効果を有している。又、
原料として用いる茶は古来から飲用として供されてお
り、かつ前記急性毒性試験例から明らかなごとく、安全
性が高いので、日常の食生活に本発明の大腸癌予防用組
成物を適宜取り入れて長期摂取しても何ら問題はない。
更に、茶は入手が容易で実用上も適切な原料であり、
又、本発明の有効成分であるポリフェノール類を得る方
法が極めて簡単で大量に操作できる方法であることか
ら、本発明は効果の高い大腸癌予防用組成物を大量かつ
安価に供給することが可能である。従って、国民の健康
増進に貢献することは勿論、産業的にも極めて有用であ
る。
As is clear from the above test examples, the composition for preventing colorectal cancer of the present invention has excellent effects. or,
Tea used as a raw material has been served as a drink since ancient times, and as is clear from the acute toxicity test example, it is highly safe, and therefore, the composition for preventing colon cancer of the present invention is appropriately incorporated into daily diet for a long period of time. There is no problem even if ingested.
Furthermore, tea is an easily available and practically suitable raw material,
Further, since the method for obtaining the polyphenols, which is the active ingredient of the present invention, is a very simple and large-scale operation method, the present invention can supply a highly effective composition for preventing colon cancer at a large amount and at a low cost. Is. Therefore, it is very useful industrially as well as contributing to the health promotion of the people.

───────────────────────────────────────────────────── フロントページの続き (72)発明者 高橋 俊雄 京都市左京区修学院桧峠町6−5 審査官 星野 紹英 (56)参考文献 特開 昭60−190719(JP,A) 特開 昭56−16412(JP,A) ZHONGGUO YIXUE KE XUEYUAN XUEBAO(中国医 学科学院学報)11〜4!(1989)P. 259−264(CHEMICAL ABST RACTS 112 (1990)要約番号: 132044) JPN.J. CANCER RE S.,80〜6!(1989)P.503−505 ─────────────────────────────────────────────────── ─── Continuation of front page (72) Inventor Toshio Takahashi 6-5 Shugakuin, Sakyo Ward, Kyoto City Examiner Shoei Hoshino (56) References JP-A-60-190719 (JP, A) JP-A-56- 16412 (JP, A) ZHONGGUO YIXUE KE XUEYUAN XUEBAO (Chinese Academy of Medical Sciences) 11-4! (1989) P. 259-264 (CHEMICAL ABST RACTS 112 (1990) Abstract No .: 132044) JPN. J. CANCER RE S. , 80-6! (1989) P. 503-505

Claims (2)

(57)【特許請求の範囲】(57) [Claims] 【請求項1】 式(1)及び/又は式(2)で表される
ポリフェノール類を有効成分として含有することを特徴
とする大腸癌予防用組成物。 【0001】 【化1】 【0002】(式中、Rは水素原子又はヒドロキシル
基を示し、Rは水素原子又は3,4,5−トリヒドロ
キシベンゾイル基を示す。)
1. A composition for preventing colon cancer, which comprises a polyphenol represented by the formula (1) and / or the formula (2) as an active ingredient. ## STR1 ## (In the formula, R 1 represents a hydrogen atom or a hydroxyl group, and R 2 represents a hydrogen atom or a 3,4,5-trihydroxybenzoyl group.)
【請求項2】 有効成分の含有率が0.05〜0.7%
である請求項1の大腸癌予防用組成物。 【0003】
2. The content rate of the active ingredient is 0.05 to 0.7%.
The composition for preventing colorectal cancer according to claim 1. [0003]
JP3108977A 1991-02-16 1991-02-16 Colorectal cancer preventive composition Expired - Lifetime JP2521196B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP3108977A JP2521196B2 (en) 1991-02-16 1991-02-16 Colorectal cancer preventive composition

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP3108977A JP2521196B2 (en) 1991-02-16 1991-02-16 Colorectal cancer preventive composition

Publications (2)

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JPH04264027A JPH04264027A (en) 1992-09-18
JP2521196B2 true JP2521196B2 (en) 1996-07-31

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Country Link
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997041137A1 (en) * 1996-04-17 1997-11-06 Unifob Use of anthocyanidin and anthocyanidin derivatives
EP0938897A1 (en) * 1997-12-26 1999-09-01 Japanese Foundation For Cancer Research Telomerase inhibitor
GB0615781D0 (en) * 2006-08-09 2006-09-20 Coressence Ltd Prebiotic composition
CN102526170B (en) * 2011-12-31 2015-04-29 许学志 Catechu extract composition for resisting tubercle bacillus, preparation method of catechu extract composition, pharmaceutical preparation containing catechu extract composition, and application of catechu extract composition
EP3074028B1 (en) * 2013-11-27 2022-04-06 Research Foundation Of The City University Of New York Activity enhancing curcumin compositions and methods of use
CN108653209A (en) * 2018-06-05 2018-10-16 西南大学 A kind of new type natural Tea Flower derives the preparation and its application of lipid nanometer vesica
CN115887443A (en) * 2023-02-27 2023-04-04 深圳市第二人民医院(深圳市转化医学研究院) Application of epigallocatechin in preparation of medicine for treating colorectal cancer

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JPN.J.CANCERRES.,80〜6!(1989)P.503−505
ZHONGGUOYIXUEKEXUEYUANXUEBAO(中国医学科学院学報)11〜4!(1989)P.259−264(CHEMICALABSTRACTS112(1990)要約番号:132044)

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