JPH03227925A - Antiviral agent against aids-causative virus - Google Patents
Antiviral agent against aids-causative virusInfo
- Publication number
- JPH03227925A JPH03227925A JP2079090A JP2079090A JPH03227925A JP H03227925 A JPH03227925 A JP H03227925A JP 2079090 A JP2079090 A JP 2079090A JP 2079090 A JP2079090 A JP 2079090A JP H03227925 A JPH03227925 A JP H03227925A
- Authority
- JP
- Japan
- Prior art keywords
- aids
- effective
- antiviral agent
- virus
- causative virus
- 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
- 241000700605 Viruses Species 0.000 title claims abstract description 15
- 239000003443 antiviral agent Substances 0.000 title claims abstract description 10
- 208000030507 AIDS Diseases 0.000 claims abstract description 21
- MOFVSTNWEDAEEK-UHFFFAOYSA-M indocyanine green Chemical compound [Na+].[O-]S(=O)(=O)CCCCN1C2=CC=C3C=CC=CC3=C2C(C)(C)C1=CC=CC=CC=CC1=[N+](CCCCS([O-])(=O)=O)C2=CC=C(C=CC=C3)C3=C2C1(C)C MOFVSTNWEDAEEK-UHFFFAOYSA-M 0.000 claims abstract description 5
- 229960004657 indocyanine green Drugs 0.000 claims abstract description 5
- 239000004480 active ingredient Substances 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 5
- 102100034343 Integrase Human genes 0.000 abstract description 4
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 abstract description 4
- 230000000840 anti-viral effect Effects 0.000 abstract description 2
- 239000008280 blood Substances 0.000 abstract description 2
- 210000004369 blood Anatomy 0.000 abstract description 2
- 230000037396 body weight Effects 0.000 abstract description 2
- 239000002775 capsule Substances 0.000 abstract description 2
- 238000002347 injection Methods 0.000 abstract description 2
- 239000007924 injection Substances 0.000 abstract description 2
- 230000007246 mechanism Effects 0.000 abstract description 2
- 206010001513 AIDS related complex Diseases 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 241000725303 Human immunodeficiency virus Species 0.000 abstract 2
- 231100000053 low toxicity Toxicity 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 description 4
- HBOMLICNUCNMMY-XLPZGREQSA-N zidovudine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](N=[N+]=[N-])C1 HBOMLICNUCNMMY-XLPZGREQSA-N 0.000 description 3
- 229960002555 zidovudine Drugs 0.000 description 3
- 238000000034 method Methods 0.000 description 2
- -1 nasal preparations Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- FIAFUQMPZJWCLV-UHFFFAOYSA-N suramin Chemical compound OS(=O)(=O)C1=CC(S(O)(=O)=O)=C2C(NC(=O)C3=CC=C(C(=C3)NC(=O)C=3C=C(NC(=O)NC=4C=C(C=CC=4)C(=O)NC=4C(=CC=C(C=4)C(=O)NC=4C5=C(C=C(C=C5C(=CC=4)S(O)(=O)=O)S(O)(=O)=O)S(O)(=O)=O)C)C=CC=3)C)=CC=C(S(O)(=O)=O)C2=C1 FIAFUQMPZJWCLV-UHFFFAOYSA-N 0.000 description 2
- 229960005314 suramin Drugs 0.000 description 2
- 208000011580 syndromic disease Diseases 0.000 description 2
- 241001430294 unidentified retrovirus Species 0.000 description 2
- 206010001985 Amoebic colitis Diseases 0.000 description 1
- 201000002909 Aspergillosis Diseases 0.000 description 1
- 208000036641 Aspergillus infections Diseases 0.000 description 1
- 108020004414 DNA Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 208000007766 Kaposi sarcoma Diseases 0.000 description 1
- 208000001388 Opportunistic Infections Diseases 0.000 description 1
- 206010035664 Pneumonia Diseases 0.000 description 1
- MKUXAQIIEYXACX-UHFFFAOYSA-N aciclovir Chemical compound N1C(N)=NC(=O)C2=C1N(COCCO)C=N2 MKUXAQIIEYXACX-UHFFFAOYSA-N 0.000 description 1
- 229960004150 aciclovir Drugs 0.000 description 1
- 230000036436 anti-hiv Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 241001493065 dsRNA viruses Species 0.000 description 1
- 210000000987 immune system Anatomy 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 210000003127 knee Anatomy 0.000 description 1
- 231100001231 less toxic Toxicity 0.000 description 1
- 229940037525 nasal preparations Drugs 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 230000010076 replication Effects 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 230000007442 viral DNA synthesis Effects 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
［産業上の利用分野コ
本発明は、現在までに有用性の高い治療法が知られてい
ないエイズの原因ウィルスに対して有効な抗ウィルス剤
に関する。DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to an antiviral agent effective against the virus that causes AIDS, for which no highly useful treatment is known to date.
［従来の技術］
抗ウィルス作用を有するウィルス剤は、アラ・ニー（Ａ
ｒａ−Ａ）、アシクロビール（Ａｃｙｃｌｏｖｉｒ）な
どのようにウィルスのＤＮＡ合成阻害作用を持つもの、
レトロウィルスなどの逆転写酵素の阻害作用を持ツスラ
ミン（Ｓｕｒａｍｉｎ）、リバビリン（Ｒｉｂａｖｉｒ
ｉｎ）、ニーφゼットφティー（ＡＺＴ、Ａｚｉｄｏｔ
ｈｙｍｉｄｉｎｅ）などが知られている。[Prior Art] Viral agents with antiviral effects include Ara Ni (A
ra-A), acyclovir, etc., which have an inhibitory effect on viral DNA synthesis,
Suramin and Ribavir have inhibitory effects on reverse transcriptase of retroviruses, etc.
in), Knee φ Z φ Tee (AZT, Azidot
hymidine) etc. are known.
エイズ［Ａ Ｉ Ｄ Ｓ （Ａｃｑｕｉｒｅｄ Ｉｍ
ｍｕｎｅ Ｄｅｆｉｃｉｅｎｃｙ Ｓｙｎｄｒｏｍｅ
：後天性免疫不全症候群）〕原因ウィルスは、ＲＮＡか
らＤＮＡへの転写を逆転酵素で行なうＲＮＡウィルスで
あるレトロウィルスであって、ＨＴ Ｌ Ｖ −ｍ （
Ｈｕｍａｎ Ｔ ｅｅｌ Ｉ Ｌｙｍｐｈｏｔｒ。Acquired Im
mune Deficiency Syndrome
: Acquired Immune Deficiency Syndrome)] The causative virus is a retrovirus, which is an RNA virus that uses reverse enzyme to transcribe RNA to DNA.
Human T eel I Lymphotr.
ｐｈｉｃ Ｖｉｒｕｓ） Ｎ ＬＡＶ （Ｌｙｍｐｈａ
ｄｅｎｏｐａｔｈｙ−ａｓｓｏｃｉａｔｅｄ Ｖｉｒｕ
ｓ）またはＨＩ Ｖ （ｌｌｕｍａｎ Ｉｍｍｕｎｏｄ
ｅｆｉｃｉｅｎｃｙ ｖｉｒｕｓ）と呼ばれる。phic Virus) N LAV (Lympha)
denopathy-associated Viru
s) or HIV (lluman immunod
efficiency virus).
エイズ原因ウィルスの感染後、Ａ Ｃ（Ａｓｙｍｐｔｏ
ｍａｔｉｃ Ｃａｒｒｉｅｒ）からＡ ＲＣ（ＡＩＤＳ
Ｒｅ１ａｔｅｄ Ｃｏｍｐｌｅｘ）を経てエイズとな
ることが知られている。これにより、生体の免疫機能が
低下し、カポジ肉腫、カリニ肺炎、カンシタ感染、アス
ペルギルス感染、アメーバ大腸炎などの日和見感染を生
じるもので、現在までにＡＺＴがＨＩＶの増殖を抑える
薬剤として知られているに過ぎない。After infection with the AIDS-causing virus, AC (Asympto
matic carrier) to ARC (AIDS
It is known that AIDS develops through AIDS. As a result, the immune system of the body is weakened, leading to opportunistic infections such as Kaposi's sarcoma, carinii pneumonia, Cancissa infection, Aspergillus infection, and amoebic colitis.To date, AZT is known as a drug that suppresses the proliferation of HIV. It's just that.
［発明が解決しようとする課題］
抗ウィルス剤として逆転写酵素の阻害物質として作用す
るものは、正常な細胞群に対する毒性が強く、投与によ
る延命作用とともに生体への副作用が強い。[Problems to be Solved by the Invention] Antiviral agents that act as inhibitors of reverse transcriptase are highly toxic to normal cell groups, and their administration not only prolongs life but also has strong side effects on living organisms.
本発明は、毒性の少ない逆転写酵素の阻害作用およびそ
の他のメカニズムを持つ物質により、エイズ原因ウィル
スの細胞への感染を抑制し、および／またはＡＲＣへの
進展、さらにはエイズへの到達を阻害するのに有効であ
り、ひいてはエイズの治療に有用な抗ウィルス剤を提供
することを目的とするものである。The present invention suppresses the infection of cells by the AIDS-causing virus and/or inhibits the progression to ARC and furthermore, the arrival of AIDS, using a substance that has a less toxic reverse transcriptase inhibitory effect and other mechanisms. The purpose of the present invention is to provide an antiviral agent that is effective for the treatment of AIDS.
［課題を解決するための手段］
本発明は、インドシアニングリーンを有効成分とするエ
イズ原因ウィルスに対する抗ウィルス剤である。[Means for Solving the Problems] The present invention is an antiviral agent against the AIDS-causing virus, which contains indocyanine green as an active ingredient.
本発明に用いられるインドシアニングリーンは、トリカ
ルボシアニン系の色素であって、下記の化学構造を有す
るものである。Indocyanine green used in the present invention is a tricarbocyanine dye and has the following chemical structure.
作用がみられたことよりヒト血中でも同程度で有効と考
えられ、体重６０ｋｇ当たり２ｍｇ〜１ｇの投与で効果
が期待できる。Since the effect was observed, it is considered to be effective at the same level in human blood, and an effect can be expected with administration of 2 mg to 1 g per 60 kg of body weight.
本発明の抗ウィルス剤は安定化剤などを含んでもよ（、
剤型としては、注射剤、カプセル剤、経鼻剤、座薬、経
口薬、軟膏剤など、種々の形態のものが用いられる。The antiviral agent of the present invention may contain a stabilizer, etc.
Various dosage forms are used, such as injections, capsules, nasal preparations, suppositories, oral preparations, and ointments.
［実 験 例］
ポウエルズ（Ｐａｕｗｅｌｓ、 Ｉ？、）らの方法［Ｐ
ａｕｗｅｌｓ。[Experimental example] Pauwels et al.'s method [P
auwels.
Ｒ，ｅｔ ａｌ、、 Ｊ、 Ｖｉｒｏｌ、 Ｍｅ
ｔｈｏｄ、 １Ｂ、 Ｈｌ−１８５（１９８７）〕
に従い、ａｎｔｉ −ＨＩ Ｖアッセイを行なった。R, et al., J. Virol, Me.
thod, 1B, Hl-185 (1987)]
Anti-HIV assay was performed according to the method.
ＭＴ−４細胞（培養開始細胞数Ｉ Ｘ １０４／ｗｅｌ
ｌ）に、エイズ原因ウィルスとしてＨＴＬＶ−ＩＩＩＢ
（２００ＣＣＩ Ｄ ５０／ ｗｅｌ Ｉ）を感染させ
、３７℃、４日間培養し、エイズ原因ウィルスの複製の
抑制効果を測定した。MT-4 cells (culture starting cell number I x 104/well
l), HTLV-IIIB as the AIDS-causing virus
(200CCI D 50/well I), cultured at 37°C for 4 days, and the inhibitory effect on the replication of the AIDS-causing virus was measured.
コントロールとしてスラミンを用いた。結果を表−１に
示す。Suramin was used as a control. The results are shown in Table-1.
［発明の効果］
本発明の抗ウィルス剤は、エイズ原因ウィルスの細胞へ
の感染およびＡＲＣへの進展の抑制、さらにエイズの治
療に有効である。[Effects of the Invention] The antiviral agent of the present invention is effective in suppressing infection of cells by the AIDS-causing virus and progression to ARC, and is effective in treating AIDS.
Claims (1)
原因ウィルスに対する抗ウィルス剤。(1) An antiviral agent against the AIDS-causing virus containing indocyanine green as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2079090A JPH03227925A (en) | 1990-01-30 | 1990-01-30 | Antiviral agent against aids-causative virus |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2079090A JPH03227925A (en) | 1990-01-30 | 1990-01-30 | Antiviral agent against aids-causative virus |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH03227925A true JPH03227925A (en) | 1991-10-08 |
Family
ID=12036881
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2079090A Pending JPH03227925A (en) | 1990-01-30 | 1990-01-30 | Antiviral agent against aids-causative virus |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH03227925A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000186040A (en) * | 1998-12-21 | 2000-07-04 | Hayashibara Biochem Lab Inc | Antiinfectant against hiv |
| EP1155694A4 (en) * | 1998-12-24 | 2004-06-02 | Hayashibara Biochem Lab | Anti-hiv infection agents and method for treating hiv infection |
-
1990
- 1990-01-30 JP JP2079090A patent/JPH03227925A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000186040A (en) * | 1998-12-21 | 2000-07-04 | Hayashibara Biochem Lab Inc | Antiinfectant against hiv |
| EP1155694A4 (en) * | 1998-12-24 | 2004-06-02 | Hayashibara Biochem Lab | Anti-hiv infection agents and method for treating hiv infection |
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