JPH04108736A - Virus-genomic inactivating-carcinogenic promotion inhibitor - Google Patents
Virus-genomic inactivating-carcinogenic promotion inhibitorInfo
- Publication number
- JPH04108736A JPH04108736A JP2224012A JP22401290A JPH04108736A JP H04108736 A JPH04108736 A JP H04108736A JP 2224012 A JP2224012 A JP 2224012A JP 22401290 A JP22401290 A JP 22401290A JP H04108736 A JPH04108736 A JP H04108736A
- Authority
- JP
- Japan
- Prior art keywords
- virus
- magnolol
- extract
- genomic
- active ingredient
- 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
- 239000003112 inhibitor Substances 0.000 title claims abstract description 7
- VVOAZFWZEDHOOU-UHFFFAOYSA-N magnolol Chemical compound OC1=CC=C(CC=C)C=C1C1=CC(CC=C)=CC=C1O VVOAZFWZEDHOOU-UHFFFAOYSA-N 0.000 claims abstract description 30
- 241000700605 Viruses Species 0.000 claims abstract description 12
- 239000000284 extract Substances 0.000 claims abstract description 12
- 239000004480 active ingredient Substances 0.000 claims abstract description 8
- 230000000711 cancerogenic effect Effects 0.000 claims description 5
- 231100000315 carcinogenic Toxicity 0.000 claims description 5
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 230000000415 inactivating effect Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 abstract description 3
- 241000124008 Mammalia Species 0.000 abstract description 2
- 239000000401 methanolic extract Substances 0.000 abstract description 2
- 239000003960 organic solvent Substances 0.000 abstract description 2
- 238000001256 steam distillation Methods 0.000 abstract description 2
- 238000013268 sustained release Methods 0.000 abstract description 2
- 239000012730 sustained-release form Substances 0.000 abstract description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 2
- 241001673966 Magnolia officinalis Species 0.000 abstract 3
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 239000003443 antiviral agent Substances 0.000 abstract 1
- 208000005623 Carcinogenesis Diseases 0.000 description 6
- 230000036952 cancer formation Effects 0.000 description 5
- 231100000504 carcinogenesis Toxicity 0.000 description 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 201000011510 cancer Diseases 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- ARSRBNBHOADGJU-UHFFFAOYSA-N 7,12-dimethyltetraphene Chemical compound C1=CC2=CC=CC=C2C2=C1C(C)=C(C=CC=C1)C1=C2C ARSRBNBHOADGJU-UHFFFAOYSA-N 0.000 description 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 2
- 241000699666 Mus <mouse, genus> Species 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 230000004913 activation Effects 0.000 description 2
- 230000003217 anti-cancerogenic effect Effects 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- XVOKPNRYHDZDMX-UHFFFAOYSA-N 1-(4-ethyl-2-bicyclo[2.2.1]heptanyl)cyclohexan-1-ol Chemical compound C1C(CC)(C2)CCC1C2C1(O)CCCCC1 XVOKPNRYHDZDMX-UHFFFAOYSA-N 0.000 description 1
- VFZRZRDOXPRTSC-UHFFFAOYSA-N DMBA Natural products COC1=CC(OC)=CC(C=O)=C1 VFZRZRDOXPRTSC-UHFFFAOYSA-N 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 241000701044 Human gammaherpesvirus 4 Species 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 230000000840 anti-viral effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 210000004748 cultured cell Anatomy 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 241000411851 herbal medicine Species 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000003999 initiator Substances 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 231100000590 oncogenic Toxicity 0.000 description 1
- 230000002246 oncogenic effect Effects 0.000 description 1
- PHEDXBVPIONUQT-RGYGYFBISA-N phorbol 13-acetate 12-myristate Chemical compound C([C@]1(O)C(=O)C(C)=C[C@H]1[C@@]1(O)[C@H](C)[C@H]2OC(=O)CCCCCCCCCCCCC)C(CO)=C[C@H]1[C@H]1[C@]2(OC(C)=O)C1(C)C PHEDXBVPIONUQT-RGYGYFBISA-N 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
Landscapes
- Medicines Containing Plant Substances (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【発明の詳細な説明】
〔産業上の利用分野〕
この発明は、ウィルス・ゲノム不活化−発癌プロモーシ
ョン阻害剤に関するものである。このような薬剤は発癌
プロモーター阻害剤として、癌の予防治療およびウィル
ス病の治療に有用である。DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention relates to a virus genome inactivation-carcinogenesis promotion inhibitor. Such drugs are useful as oncogenic promoter inhibitors in the preventive treatment of cancer and the treatment of viral diseases.
〔従来の技術および発明が解決しようとする課題〕発癌
には刺激または炎症としての研究が必然的に伴うもので
あるという考えに基づいて、マウスにおいて発癌二段階
実験が行なわれた。それ以来、発癌機構において長期間
の作用を要する二段階目のプロモーション（促進作用）
が重要な過程として取り上げられ、現在、その研究が幅
広く進められている。ヒトの生活の関与する物質中には
、さまざまな発癌プロモーターが存在するとともに、さ
まざまな抗発癌プロモーター物質も存在し、これらの物
質はヒトの発癌に関連する重要な要因となっている。[Prior Art and Problems to be Solved by the Invention] Based on the idea that carcinogenesis necessarily involves the study of stimulation or inflammation, a two-step carcinogenesis experiment was conducted in mice. Since then, the second stage of promotion, which requires a long-term action in the carcinogenic mechanism, has been
has been recognized as an important process, and a wide range of research is currently underway. Among the substances involved in human life, there are various carcinogenic promoters as well as various anti-carcinogenic promoter substances, and these substances are important factors related to human carcinogenesis.
抗発癌プロモーターとしては、生薬中に活性成分の存在
がみとめられることが次第に明らかになってきているが
、まだその有効性を分析した例は少なく、その解析およ
びそれに基づく新たな薬剤の開発が望まれている。Although it is gradually becoming clear that active ingredients exist in crude drugs as anti-carcinogenic promoters, there are still few cases in which their effectiveness has been analyzed, and it is desirable to analyze them and develop new drugs based on them. It is rare.
本発明者等は、発癌プロモーターがウィルス活性化剤と
重なるところから、アフリカに多発するパーキット（Ｂ
ｕｒｋｉｔｔ）・リンパ腫由来のエプスタイン・バー
ル・ウィルス（Ｅｐｓｔｅｉｎ Ｂａｒｒ ｖｉｒｕｓ
。The present inventors discovered that Perkitt (B
urkitt) and Epstein Barr virus derived from lymphoma.
.
以下ＥＢウィルスと略称）を含むが、ＥＢウィルス非産
生のリンパ芽球様培養細胞であるラジ（Ｒａｊｉ）細胞
にプロモーターとしてテトラデカノイルホルボールアセ
テート（以下、ＴＰＡと略称）を作用させることにより
ＥＢウィルスを活性化する系を用いて、薬用植物中に含
まれるＥＢウィルス活性化抑制物質を検索したところ、
厚朴の抽出物およびマグノロールがＴＰＡによるＥＢウ
ィルス活性化を顕著に抑制することを見出だした。EB virus (hereinafter abbreviated as EB virus), but by acting on Raji cells, which are lymphoblastoid cultured cells that do not produce EB virus, with tetradecanoylphorbol acetate (hereinafter abbreviated as TPA) as a promoter. Using a system that activates viruses, we searched for substances that inhibit EB virus activation contained in medicinal plants.
It has been found that extracts of Namibaku and Magnolol significantly inhibit TPA-induced EB virus activation.
また、マウスの系を用いて、発癌二段階実験を行ったと
ころ、厚朴の抽出物およびマグノロールが悪性腫瘍に対
して抑制効果のあることを見出だした。すなわち、発癌
二段階実験のイニシエーター（初発因子）として、ジメ
チルベンズアントラセン（以下、ＤＭＢＡと略称）を用
い、プロモーター（促進因子）として、ＴＰＡを使用し
て、ＴＰＡ処理する前の段階で上記の成分を用いたとこ
ろ、ＴＰＡによるマウス皮膚での悪性腫瘍の形成を顕著
に抑制することを見出した。In addition, when conducting a two-step carcinogenesis experiment using a mouse system, it was found that extracts of Koboku and magnolol had an inhibitory effect on malignant tumors. That is, dimethylbenzanthracene (hereinafter abbreviated as DMBA) was used as an initiator (initiating factor) in a two-step carcinogenic experiment, TPA was used as a promoter (promoting factor), and the above-mentioned When the ingredients were used, it was found that the formation of malignant tumors in mouse skin caused by TPA was significantly suppressed.
本発明は、厚朴の抽出物またはマグノロールを有効成分
とするウィルス・ゲノム不活化剤を提供するものである
。The present invention provides a virus/genome inactivating agent containing an extract or magnolol as an active ingredient.
また本発明は、厚朴の抽出物またはマグノロールを有効
成分とする発癌プロモーノヨン阻害剤を提供するもので
ある。The present invention also provides an inhibitor of carcinogenic promoters, which contains an extract or magnolol as an active ingredient.
厚朴（Ｍａｇｎｏｌ ｉａ Ｂ ａｒｋ）として取引さ
れているものは、主としてホウツキ（Ｍａｇｎｏｌｉａ
ｏｂｏｖａｔａ、和厚朴）、カラホウ（Ｍａｇｎｏｌ
ｉａ ｏｆＴｉｃｉｎａｌｉｓ、唐厚朴）およびその変
種（Ｍ、ｏｌＴｉｃｉｎａｌｉｓ ｖａｒ、ｂｉｌｏｂ
ａ１同上）の幹皮を乾燥した生薬である。これらは、−
成分としてマグノロールを含有する。What is traded as Magnolia Bark is mainly Magnolia Bark.
obovata, Wakoboku), Karahou (Magnol)
ia ofTicinalis var, bilob) and its varieties (M, olTicinalis var, bilob
It is a herbal medicine made by drying the stem bark of A. a1 (same as above). These are −
Contains magnolol as an ingredient.
この発明にいう「抽出物」は、マグノロールを含有する
限り任意の方法による抽出物であり得るが、これは、水
、親水性有機溶媒（メタノール、エタノール、アセトン
等）またはこれらの混合物による抽出エキスおよび水蒸
気蒸留による留出物が含まれる。好ましいのはメタノー
ル抽出物である。The "extract" referred to in this invention may be an extract obtained by any method as long as it contains magnolol, but this may include extraction with water, a hydrophilic organic solvent (methanol, ethanol, acetone, etc.), or a mixture thereof. Includes extracts and distillates from steam distillation. Preferred is a methanol extract.
マグノロールは、厚朴に含有され、後記の式に示した構
造を有する公知の化合物で、文献〔薬学雑誌９３＠４２
２頁（１９７３年）〕に記載されている。含有率は、唐
厚朴の方が和厚朴より高い。Magnolol is a well-known compound that is contained in Atsugaku and has the structure shown in the formula below.
2 (1973)]. The content is higher in Tokoboku than in Wakoboku.
ｉｐ １０２″
分子式： Ｃ＋ ＊ Ｈｌ＊ Ｏｔ
ＭＳ ｍ／ｅ：２６６（Ｍ＝）
ＵＶ（ＥｔＯＨ）：λ２９４．３２３ｎｔａＮＭＲ（Ｃ
ＤＣＩｓ）：δ３．４．５．１，６．Ｌ６．０．６．８
−７．３ｐｐｍ
ウィルス・ゲノム不活化、発癌プロモーション阻害およ
びそれらに基づく抗癌、抗ウィルス作用を目的とする上
記、厚朴の抽出物およびマグノロールの投与量は、勿論
投与の目的、患者の年齢、状態、症状の重さ等によって
異なるが、一般に目的とする作用を発揮するに十分な有
効成分の濃度をもたらす量であり、これは通常マグノロ
ールとしてｌＯ〜１０００μｇ／ｍＩ２である。哺乳動
物に投与する場合、通常マグノロールとして２０〜５０
０Ｑｎを１日２〜４回の分割投与または持効性製剤とし
て投与する。なお、上記化合物をマウスに投与した場合
顕著な毒性が見られなかった。ip 102″ Molecular formula: C+ * Hl * Ot MS m/e: 266 (M=) UV (EtOH): λ294.323ntaNMR (C
DCIs): δ3.4.5.1,6. L6.0.6.8
-7.3ppm The dosage of the above-mentioned Koboku extract and magnolol, which aims to inactivate the virus genome, inhibit carcinogenesis promotion, and have anticancer and antiviral effects based on these, is of course determined by the purpose of administration and the age of the patient. Although it varies depending on the condition, severity of symptoms, etc., it is generally the amount that provides a sufficient concentration of the active ingredient to exert the desired effect, and this is usually 10 to 1000 μg/mI2 for magnolol. When administered to mammals, the dosage is usually 20 to 50% as magnolol.
Administer 0Qn in divided doses 2 to 4 times per day or as a sustained release formulation. Note that no significant toxicity was observed when the above compound was administered to mice.
Claims (2)
るウィルス・ゲノム不活化剤。(1) A virus/genome inactivating agent containing Koboku extract or Magnolol as an active ingredient.
る発癌プロモーション阻害剤。(2) A carcinogenic promotion inhibitor containing an extract or magnolol as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2224012A JPH04108736A (en) | 1990-08-24 | 1990-08-24 | Virus-genomic inactivating-carcinogenic promotion inhibitor |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2224012A JPH04108736A (en) | 1990-08-24 | 1990-08-24 | Virus-genomic inactivating-carcinogenic promotion inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH04108736A true JPH04108736A (en) | 1992-04-09 |
Family
ID=16807206
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2224012A Pending JPH04108736A (en) | 1990-08-24 | 1990-08-24 | Virus-genomic inactivating-carcinogenic promotion inhibitor |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH04108736A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6582735B2 (en) * | 2000-12-15 | 2003-06-24 | Npi, Llc. | Compositions and methods of use for extracts of magnoliaceae plants |
| JP2008542192A (en) * | 2005-02-23 | 2008-11-27 | アービサー ジャック エル． | Honokiol derivatives for the treatment of proliferation disorders |
| DE102009048044A1 (en) * | 2009-10-02 | 2011-04-21 | Beiersdorf Ag | Use of magnolol or honokiol as antibacterial, antimycotic, antiparasitic or antiviral agents |
| CN110227050A (en) * | 2019-07-26 | 2019-09-13 | 嘉兴言肌草生物技术有限公司 | A kind of anti-aging maintenance sustained release Essence and the anti-aging Face-protecting mask using its preparation |
-
1990
- 1990-08-24 JP JP2224012A patent/JPH04108736A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6582735B2 (en) * | 2000-12-15 | 2003-06-24 | Npi, Llc. | Compositions and methods of use for extracts of magnoliaceae plants |
| US6814987B2 (en) | 2000-12-15 | 2004-11-09 | Npi, Llc. | Compositions and methods of use for extracts of magnoliaceae plants |
| JP2008542192A (en) * | 2005-02-23 | 2008-11-27 | アービサー ジャック エル． | Honokiol derivatives for the treatment of proliferation disorders |
| DE102009048044A1 (en) * | 2009-10-02 | 2011-04-21 | Beiersdorf Ag | Use of magnolol or honokiol as antibacterial, antimycotic, antiparasitic or antiviral agents |
| CN110227050A (en) * | 2019-07-26 | 2019-09-13 | 嘉兴言肌草生物技术有限公司 | A kind of anti-aging maintenance sustained release Essence and the anti-aging Face-protecting mask using its preparation |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Liczbiński et al. | Molecular mechanism of curcumin action in signaling pathways: Review of the latest research | |
| Rauf et al. | Honokiol: A review of its pharmacological potential and therapeutic insights | |
| Zhang et al. | Nicotine in inflammatory diseases: anti-inflammatory and pro-inflammatory effects | |
| Nishino et al. | Antitumor-promoting activity of garlic extracts | |
| US7410656B2 (en) | Anti-cancer compounds | |
| Xiao et al. | Indigo naturalis suppresses colonic oxidative stress and Th1/Th17 responses of DSS‐induced colitis in mice | |
| JPH02111725A (en) | Drug composition | |
| Ijaz et al. | Rosmarinic acid and its derivatives: Current insights on anticancer potential and other biomedical applications | |
| Li et al. | Wound-healing activity of Zanthoxylum bungeanum maxim seed oil on experimentally burned rats | |
| Zhao et al. | Hybrid molecules based on caffeic acid as potential therapeutics: A focused review | |
| EP3391893B1 (en) | Pharmaceutical composition for treating leukemia and preparation method thereof | |
| AU2006279332B2 (en) | Anti-inflammatory activity of phenethylisothiocyanate (PEITC) and the Barbarea verna seed preparation containing this compound | |
| Lin et al. | Nuclear factor erythroid 2-related factor 2 (Nrf2) as a potential therapeutic target for vitiligo | |
| Dong et al. | Salvianolic acid B ameliorates CNS autoimmunity by suppressing Th1 responses | |
| Devarajan et al. | Pharmacotherapeutic values of berberine: A Chinese herbal medicine for the human cancer management | |
| JPH04108736A (en) | Virus-genomic inactivating-carcinogenic promotion inhibitor | |
| US20100197780A1 (en) | Compounds extracted from palm oil mill effluent for the treatment of cancer, compositions thereof and methods therewith | |
| US20040156799A1 (en) | Cancer treatment method and compositions | |
| Sekhar et al. | A review on anticancer potential of natural drugs: hispolon and limonene | |
| CN114452297A (en) | Medicinal preparation for treating dermatitis and preparation method thereof | |
| EP1392266A2 (en) | Cancer treatment method and compositions comprising compounds of the ginger family | |
| CN111358806A (en) | Anti-ovarian cancer pharmaceutical composition with synergistic effect and application thereof | |
| KR102653057B1 (en) | Immuno Anticancer Composition Containing Rhus Veniciflua Strokes Extract And Cytokine Induced Killer Cells | |
| Yang et al. | A new method for purifying Brazilin from lignum sappan–Cytotoxic and anti-proliferative effects in cell lines and improved survival in mice bearing urinary bladder carcinoma | |
| Grunberg et al. | Anti-mycobacterial properties of a new derivative of Isoniazid |