JPH0761930A - Inhibitor of cancer metastasis - Google Patents
Inhibitor of cancer metastasisInfo
- Publication number
- JPH0761930A JPH0761930A JP23247793A JP23247793A JPH0761930A JP H0761930 A JPH0761930 A JP H0761930A JP 23247793 A JP23247793 A JP 23247793A JP 23247793 A JP23247793 A JP 23247793A JP H0761930 A JPH0761930 A JP H0761930A
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- cancer metastasis
- inhibitor
- cells
- metastasis
- 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.)
- Pending
Links
Landscapes
- Other In-Based Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【０００１】[0001]
【産業上の利用分野】本発明は、ガン転移抑制剤に関す
る。TECHNICAL FIELD The present invention relates to a cancer metastasis inhibitor.
【０００２】[0002]
【従来の技術】近年、ガンの治療法は急速な進歩をとげ
てきた。特に、外科的な手術または放射線療法によっ
て、原発ガンの除去に対する成功率が大幅に向上してい
る。ところが原発ガンの除去が完全になされても、ガン
の転移によって死に至る場合が少なくなく、最近、ガン
の転移阻害がガン治療上克服すべき重要な問題であると
の認識がたかまっている。2. Description of the Related Art In recent years, cancer treatment methods have made rapid progress. In particular, surgical procedures or radiation therapy have significantly increased the success rate for removal of the primary cancer. However, even if the primary cancer is completely removed, it often happens that the cancer metastasizes to death, and recently, it has been recognized that inhibition of cancer metastasis is an important problem to be overcome in cancer treatment.
【０００３】しかしながら、外科的手術や放射線療法で
は手法的に限界があり、ガンの転移を有効に阻害するこ
とができない。又、抗ガン剤を用いる化学療法はガン細
胞に直接作用を及ぼすものであるが、この際、宿主の正
常細胞に対しても有害な副作用を及ぼすものが多く、ガ
ンの転移に対しても必ずしも有効といえない状況にあ
る。However, surgical operation and radiation therapy have a limit in terms of technique, and cancer metastasis cannot be effectively inhibited. Further, chemotherapy using an anti-cancer agent has a direct effect on cancer cells, but in this case, many of them also have harmful side effects on normal cells of the host and are not always effective against cancer metastasis. The situation is not effective.
【０００４】ガン転移の機構に関しては、多くの研究が
為され、転移の抑制に関する物質の検索は広くなされて
きた。ガン細胞は原発巣より遊離した後、血管中に侵入
し、そしてガン細胞は血管壁の血管内皮細胞層にもぐり
こみ細胞外基質成分と接着した後、分解酵素により細胞
外基質を破壊する。このようにしてガン細胞は他の臓器
に侵入し、そこで新たな転移巣を形成すると考えられて
いる（Ｌ．Ａ．Ｌｉｏｔｔａ ｅｔ ａｌ．，Ｌａｂ．
Ｉｎｖｅｓｔ．，４９，６３６（１９８３））。ガン転
移抑制剤の開発の為には、上で示す各ステップのいずれ
かを抑制するものが開発されればよいと考えられる。例
えば細胞外基質と細胞の結合を効率よく阻害するもの、
血管内皮細胞層への浸潤を抑制する物質、分解酵素を阻
害する物質等が上げられる。また、その中でも副作用の
弱い物質が望ましい。Much research has been conducted on the mechanism of cancer metastasis, and the search for substances relating to the inhibition of metastasis has been extensively conducted. After the cancer cells are released from the primary focus, they invade the blood vessels, and the cancer cells dig into the vascular endothelial cell layer of the blood vessel wall and adhere to the extracellular matrix component, and then the extracellular matrix is destroyed by the degrading enzyme. In this way, cancer cells are thought to invade other organs and form new metastatic foci there (LA Liotta et al., Lab.
Invest. , 49 , 636 (1983)). In order to develop a cancer metastasis inhibitor, it is considered that it is sufficient to develop an agent that suppresses any one of the above steps. For example, those that efficiently inhibit the binding between extracellular matrix and cells,
Examples include substances that suppress invasion into the vascular endothelial cell layer, substances that inhibit degrading enzymes, and the like. Among them, substances with weak side effects are desirable.
【０００５】一方、カルバマゼピン化合物は、抗てんか
ん剤および鎮痛剤等の治療薬として知られている。しか
し、これらの化合物にガンの転移を抑制する作用がある
ことは知られていなかった。On the other hand, carbamazepine compounds are known as therapeutic agents such as antiepileptic agents and analgesics. However, it has not been known that these compounds have an action of suppressing cancer metastasis.
【０００６】[0006]
【発明が解決しようとする課題】本発明者らは、新たな
ガン転移抑制活性を有する化合物を見いだすべく鋭意検
討した結果、カルバマゼピン化合物に高いガン転移抑制
活性を見いだし、本発明を完成するに至った。DISCLOSURE OF THE INVENTION The present inventors have conducted extensive studies to find a compound having a new cancer metastasis inhibitory activity, and as a result, found a high cancer metastasis inhibitory activity in a carbamazepine compound, and completed the present invention. It was
【０００７】[0007]
【問題を解決するための手段】かくして本発明によれ
ば、５Ｈ−ジベンズ［ｂ，ｆ］アゼピン−５−カルボキ
サミド（以下「化合物１」という）、または１０,１１
−ジヒドロ−５Ｈ−ジベンズ［ｂ，ｆ］アゼピン−５−
カルボキサミド（以下「化合物２」という）を有効成分
とするガン転移抑制剤が提供される。Thus, according to the present invention, 5H-dibenz [b, f] azepine-5-carboxamide (hereinafter referred to as "compound 1"), or 10,11
-Dihydro-5H-dibenz [b, f] azepine-5-
A cancer metastasis inhibitor comprising a carboxamide (hereinafter referred to as "compound 2") as an active ingredient is provided.
【０００８】本発明の薬剤の有効成分である化合物１お
よび化合物２は、市販された公知の化合物である。Compounds 1 and 2 which are the active ingredients of the drug of the present invention are known commercially available compounds.
【０００９】本発明の転移抑制剤は、経口的または非経
口的に投与することが出来る。投与量は、患者の年齢、
健康状態、体重、投与形態などにより異なるが、一般的
な一日の投与量は、通常１〜５００ｍｇ／ｋｇであり、
一回あるいはそれ以上投与される。The metastasis suppressor of the present invention can be administered orally or parenterally. The dose depends on the age of the patient,
Generally, the daily dose is 1 to 500 mg / kg, although it varies depending on the health condition, body weight, administration form, etc.
It is administered once or more.
【００１０】用いられる投与形態は、錠剤、カプセル
剤、散剤、顆粒剤、シロップ剤、注射剤、坐剤、点滴
剤、各種軟膏剤などである。製剤化のために、有効成分
と反応しない適当な賦形剤、滑沢剤、保存剤、希釈剤な
どを加えてもよい。このような添加剤の具体的な例とし
ては、デンプン、マンニット、結晶セルロース、カルボ
キシメチルセルロース、カルボキシメチルセルロース
ナトリウム、アラビヤゴム、植物油、ポリエチレングリ
コール、ゼラチン、乳糖、アミロース、ステアリン酸、
マグネシウム、タルク、ケイ酸、パラフィン、香料油、
脂肪酸モノグリセライドおよびジグリセライド、水、エ
タノール、生理食塩水、グルコース溶液、輸液剤などが
挙げられる。The dosage forms used are tablets, capsules, powders, granules, syrups, injections, suppositories, drops, various ointments and the like. For formulation, suitable excipients, lubricants, preservatives, diluents and the like which do not react with the active ingredient may be added. Specific examples of such additives include starch, mannitol, crystalline cellulose, carboxymethyl cellulose, carboxymethyl cellulose.
Sodium, arabic gum, vegetable oil, polyethylene glycol, gelatin, lactose, amylose, stearic acid,
Magnesium, talc, silicic acid, paraffin, fragrance oil,
Examples thereof include fatty acid monoglyceride and diglyceride, water, ethanol, physiological saline, glucose solution, infusion solution and the like.
【００１１】[0011]
【実施例】本発明のガン転移抑制剤について以下実施例
を挙げて具体的に説明するが、本発明はこれら実施例に
限られるものではない。EXAMPLES The cancer metastasis inhibitor of the present invention will be specifically described with reference to the following examples, but the present invention is not limited to these examples.
【００１２】試験例 転移抑制効果の確認 腹水肝ガン細胞ＡＨ−１３０細胞の浸潤に及ぼす化合物
評価方法は、明渡らの方法（Ｃａｎｃｅｒ Ｒｅｓ．，
４６，２４１６（１９８６））に従って行った。即ち、
ラット腸間膜中皮細胞を初代培養し、７日後にコンフレ
ントになった中皮細胞培養層に、腹水肝ガン高浸潤細胞
株を添加した。その２４時間後に、中皮細胞層の下に浸
潤した腹水肝ガン細胞の数を計測して、各化合物添加群
と対照（無添加）群との比較により下式の浸潤抑制率を
算出した。浸潤抑制率（％）は、（（対照群の浸潤細胞
数−化合物添加群の浸潤細胞数）／ （対照群の浸潤細
胞数））×１００の計算式により算出した。その結果を
表１に示す。Test Example Confirmation of Metastasis Inhibitory Effect The compound evaluation method on the invasion of ascites hepatoma cells AH-130 cells was evaluated by the method of Cancer Research, Cancer Res.
46 , 2416 (1986)). That is,
Rat mesenteric mesothelial cells were primary-cultured, and the ascites hepatoma highly infiltrating cell line was added to the mesothelial cell culture layer that became confluent after 7 days. Twenty-four hours later, the number of ascites hepatoma cells infiltrating under the mesothelial cell layer was counted, and the invasion inhibition rate of the following formula was calculated by comparing each compound-added group with the control (no addition) group. The invasion inhibition rate (%) was calculated by a calculation formula of ((number of infiltrating cells in control group-infiltrating cell number in compound-added group) / (number of infiltrating cells in control group)) x 100. The results are shown in Table 1.
【００１３】[0013]
【表１】 [Table 1]
Claims (1)
−カルボキサミド、または、１０,１１−ジヒドロ−５
Ｈ−ジベンズ［ｂ，ｆ］アゼピン−５−カルボキサミド
を有効成分とするガン転移抑制剤。1. 5H-dibenz [b, f] azepine-5
-Carboxamide, or 10,11-dihydro-5
A cancer metastasis inhibitor containing H-dibenz [b, f] azepine-5-carboxamide as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP23247793A JPH0761930A (en) | 1993-08-25 | 1993-08-25 | Inhibitor of cancer metastasis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP23247793A JPH0761930A (en) | 1993-08-25 | 1993-08-25 | Inhibitor of cancer metastasis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH0761930A true JPH0761930A (en) | 1995-03-07 |
Family
ID=16939921
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP23247793A Pending JPH0761930A (en) | 1993-08-25 | 1993-08-25 | Inhibitor of cancer metastasis |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0761930A (en) |
-
1993
- 1993-08-25 JP JP23247793A patent/JPH0761930A/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Tessitore et al. | Pharmacological interference with tissue hypercatabolism in tumour-bearing rats | |
| EP1315505B1 (en) | Pharmaceutical compositions for headache, migraine, nausea and emesis | |
| RAGAN et al. | The treatment of gold dermatitides: Use of BAL (2, 3-dimercaptopropanol) | |
| EP3860601A1 (en) | Compositions for reducing serum uric acid | |
| DE69333362T2 (en) | USE OF ANGIOTENSINE ANTAGONISTS (AT1) TO REDUCE DISEASE AND DEATH RISK TO MYOCARDINE FARCT | |
| RU2423692C2 (en) | Substances for pancreatitis prevention and treatment | |
| EP2026806A2 (en) | Use of vx-702 for treating rheumatoid arthritis | |
| KR100207356B1 (en) | Cancerous metastasis inhibitor | |
| US6583127B1 (en) | Use of etherlysophospholipids as antiinflammatory agents | |
| KR900006993B1 (en) | Dl-5-(2-benzyl-3,4-dihydro-2h-benzo pyrano-6-yl)methyl thiazolidine-2,4-dione as an antiatherosclerosis agent | |
| JPH0761930A (en) | Inhibitor of cancer metastasis | |
| WO1991019488A1 (en) | REDUCTION OF CARDIOVASCULAR VESSEL OCCLUSIONS WITH ASCORBATE AND LIPOPROTEIN (a) BINDING INHIBITORS | |
| CN113712960A (en) | Application of R-ketorolac in prevention and treatment of aortic dissection and aortic aneurysm | |
| McMahon et al. | Lack of disulfiram-like reactions with ceftizoxime | |
| Roba et al. | Antagonism by suloctidil of arterial thrombus formation in rats | |
| US7179838B2 (en) | Coumarin analog compounds for safer anticoagulant treatment | |
| GB2105192A (en) | Composition for use in treating atherosclerosis | |
| EP1699452A2 (en) | Use of statins for the treatment of metabolic syndrome | |
| Yong et al. | Synergism in pharmacokinetics of retagliptin and metformin observed during clinical trials of their combination therapy | |
| Borreli et al. | The co-operative action of hyaluronidase and urokinase on the isoproterenol-induced myocardial infarction in rats | |
| EP0075845A1 (en) | Uric acid-lowering composition, method and use | |
| AU748754B2 (en) | Treatment of hepatic cirrhosis | |
| CA2108065A1 (en) | Antiarteriosclerosis agent and antihyperlipoproteinemics | |
| KR100356899B1 (en) | Preventives and remedies for ulcerous colitis and/or crohn's disease | |
| EP0163258A2 (en) | New use of dihydroergotamine |