JPH01313433A - Anti-hiv agent - Google Patents

Anti-hiv agent

Info

Publication number
JPH01313433A
JPH01313433A JP14544088A JP14544088A JPH01313433A JP H01313433 A JPH01313433 A JP H01313433A JP 14544088 A JP14544088 A JP 14544088A JP 14544088 A JP14544088 A JP 14544088A JP H01313433 A JPH01313433 A JP H01313433A
Authority
JP
Japan
Prior art keywords
hiv
agent
fucoidan
active ingredient
administration
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
Application number
JP14544088A
Other languages
Japanese (ja)
Inventor
Kourou Hoshino
洪郎 星野
Yasuo Suzuki
康夫 鈴木
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.)
NIPPON KOUTAI KENKYUSHO KK
Original Assignee
NIPPON KOUTAI KENKYUSHO KK
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by NIPPON KOUTAI KENKYUSHO KK filed Critical NIPPON KOUTAI KENKYUSHO KK
Priority to JP14544088A priority Critical patent/JPH01313433A/en
Publication of JPH01313433A publication Critical patent/JPH01313433A/en
Pending legal-status Critical Current

Links

Landscapes

  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

PURPOSE:To obtain an anti-human immunodeficiency virus(HIV) agent, containing fucoidan as an active ingredient, effective in preventing infection of HIV, prevention of onset and treatment of AIDS and related syndromes thereof and suitably usable for administration for a long period. CONSTITUTION:An anti-HIV agent containing fucoidan which is a polysaccharide extracted from Fucus vesiculosus that is one species of brown algae and containing much fucose containing sulfuric acid in the molecule as an active ingredient. The dose of the above-mentioned anti-HIV agent for an adult is preferably 0.1-10g in the case of oral administration and 0.1-1g in the case of parenteral administration.

Description

【発明の詳細な説明】 〔産業上の利用分野〕 本発明は、ヒト免疫不全症ウィルス(以下1”’ HI
V Jと略称する)に関し、更に詳細には、特定の糖脂
質を有効成分とする新しい抗f(IV剤に関する。
[Detailed Description of the Invention] [Industrial Application Field] The present invention relates to human immunodeficiency virus (hereinafter referred to as 1"' HI
In particular, the present invention relates to a new anti-f (IV agent) containing a specific glycolipid as an active ingredient.

〔従来の技術及びその課題〕[Conventional technology and its problems]

後天性免疫不全症候群(Acquired Immun
eDeficiency Syndrom ; A11
)S〕は、 )Iff[Human Imynunod
eficiency Virus ; Nature。
Acquired Immune Deficiency Syndrome
eDeficiency Syndrome; A11
)S] is )Iff[Human Imynunod
efficiency Virus; Nature.

き起される重篤な5P!、役不全症でアリ、その死亡率
が非常に高いことから、かかるHIV感染及びAI D
Sに対する対策は大きな社会的課題とさえなっている。
A serious 5P awakening! , HIV infection and AIDs, as the mortality rate is very high.
Countermeasures against S have even become a major social issue.

現在臨床的に効果があると認められている抗I(IV剤
としては、逆転写酵素の阻害作用を有するアシドチミジ
ン(AZT )が知られているが、その臨床的効果は、
尚不十分で6J)、更にこれによる副作用、例えば骨髄
(造血組織)の障害や頭痛、けいれん等の神経症状等の
副作用が強いという問題を抱えている。殊にHIVは、
その遺伝子がプロウィルスとなって感染した細胞の染色
体に潜シ込み遺伝病のような状態になっていることから
必然的に薬剤の長期投与が要求されておfi、AZTの
有するかかる’rare用は、これを抗HIV剤として
用いる場合の大きな障害となっている。
Acidothymidine (AZT), which has an inhibitory effect on reverse transcriptase, is known as an anti-I (IV drug) that is currently recognized to be clinically effective.
However, it is still insufficient (6J), and there is a further problem in that it causes strong side effects such as damage to the bone marrow (hematopoietic tissue) and neurological symptoms such as headaches and convulsions. In particular, HIV
Since the gene becomes a provirus and infiltrates the chromosomes of infected cells, causing a condition similar to a genetic disease, long-term administration of the drug is inevitably required. This is a major obstacle in using it as an anti-HIV agent.

また、)IIV感染者が、AIDSを発症するまでには
、通常極めて長い臨床的潜伏期がありその為、感染予防
対策をたてることが非常に困難とされている。
Furthermore, there is usually an extremely long clinical incubation period before a person infected with )IIV develops AIDS, which makes it extremely difficult to take measures to prevent infection.

かかる現状からMIV感染及びAI DSに対して奏効
する新しい医薬製剤の開発が斯界で待ち望まれている。
Under these circumstances, the development of new pharmaceutical preparations that are effective against MIV infection and AIDS is eagerly awaited.

〔課題を解決するための手段〕[Means to solve the problem]

本発明者は、1(IVに対して作用を有する化合物につ
いて鋭意研究金おこなった結果、フコイダンが抗1−I
IV剤として有効であることを見出し、本発明全完成し
た。
As a result of intensive research into compounds that have an effect on 1-IV, the present inventor discovered that fucoidan has an anti-1-I effect.
It was found to be effective as an IV agent, and the present invention was completed.

すなわち本発明は、フコイダンを有効成分として含有す
る抗1(IV剤を提供するものである。
That is, the present invention provides an IV agent containing fucoidan as an active ingredient.

本発明の有効成分であるフコイダン (Fucoidan又はFucoidin )は、褐4
類の一種であるフッカ ベシクロサス(FucusVe
siculoaus )から抽出され、分子内に鉱酸を
含有するフコースを多く宮む?リサツヵライドであり、
現在、L−7コースの原料として主に用いられているも
のである。
Fucoidan or Fucoidin, which is the active ingredient of the present invention, is brown 4
Fucus Vesiculosus
siculoas) and contains a lot of fucose, which contains mineral acids in the molecule? It is Risatsuka Ride,
Currently, it is mainly used as a raw material for L-7 course.

フコイダンはすでに市販されている安全性の高い化合物
であり(例えばシグマカタログ番号1” 5631 )
 、本発明においてはこの市販品を用いることができる
Fucoidan is a highly safe compound that is already commercially available (e.g. Sigma catalog number 1” 5631).
This commercially available product can be used in the present invention.

本発明の抗f(IV剤は、上記フコイダンを必、須成分
とし、通常その薬理有効量と共に適当な医薬#!剤担体
を配合することにより調製され゛る。
The anti-f(IV) agent of the present invention contains the above-mentioned fucoidan as an essential ingredient, and is usually prepared by blending a pharmacologically effective amount thereof with a suitable pharmaceutical agent carrier.

製剤担体としては、使用形態に応じた製剤をgIl製す
るのに通常慣用される元項剤、増量剤、保湿剤、崩壊剤
、表面活性剤等の賦形剤ないし希釈剤等のいずれもが使
用できる。製剤組成物の形態はこれが上記有効成分を効
果的に含有する状態であれば籍に限定はなく、例えば、
錠剤、粉剤、顆粒剤、丸剤等の固剤や通常液剤、懸濁剤
、乳剤等の液剤であることができる。またこれを使用前
に適当な担体の添加によって液状となし得る乾燥品とす
ることもできる。上記製剤組成物には、必要に応じて通
常の各種添加剤、例えば溶解補助剤、緩衝剤、無痛化剤
、保存剤、着色剤等を添加することもでき、更に他の医
薬品を組み合せ配合することもできる。
As a pharmaceutical carrier, any of excipients or diluents such as excipients, bulking agents, humectants, disintegrants, surfactants, etc., which are commonly used to prepare pharmaceutical preparations according to the usage form, can be used. Can be used. The form of the pharmaceutical composition is not limited as long as it effectively contains the above-mentioned active ingredient; for example,
They can be solid preparations such as tablets, powders, granules, and pills, and liquid preparations such as liquid preparations, suspensions, and emulsions. It can also be made into a dry product that can be made into a liquid by adding a suitable carrier before use. Various conventional additives such as solubilizing agents, buffering agents, soothing agents, preservatives, coloring agents, etc. may be added to the above pharmaceutical composition as necessary, and other pharmaceuticals may also be combined. You can also do that.

本発明の抗1(IV剤は、該製剤組成物の形態に応じた
適当な投与経路で投与される。投与方法も特に限定はな
く、内用、外用及び注射によることができる。注射剤は
、例えば静脈内、筋肉内、皮下、皮内、腹腔内等に投与
し得、外用剤には、全開等も包含される。
The anti-1 (IV agent) of the present invention is administered by an appropriate administration route depending on the form of the pharmaceutical composition.The administration method is also not particularly limited, and can be administered internally, externally, or by injection. For example, it can be administered intravenously, intramuscularly, subcutaneously, intradermally, intraperitoneally, etc., and external preparations also include fully administered.

本発明抗HIV剤の投与量は、その製剤形態、投与方法
、使用目的及びこれを通用される患者の年齢、体重、病
状等に応じて適宜設定され、一定ではないが一般には製
剤中に含有される有効成分の量が一成人当シ、経口投与
の場合0.12〜101程度、非経口投与の場合0.1
2〜12程度とすることが好ましく、製剤中の有効成分
量は、この投与量に従って適宜設定される。なお、投与
は必要に応じて1日数回に分けて行うことも可能である
The dosage of the anti-HIV agent of the present invention is determined appropriately depending on its formulation form, administration method, purpose of use, and the age, weight, medical condition, etc. of the patient to whom it is administered, and although it is not fixed, it is generally contained in the formulation. The amount of active ingredient administered per person is approximately 0.12 to 101 for oral administration, and 0.1 for parenteral administration.
It is preferable to set it as about 2-12, and the amount of active ingredients in a formulation is suitably set according to this dosage. Note that the administration can be divided into several times a day if necessary.

〔発明の効果〕〔Effect of the invention〕

本発明の抗HIV剤は、 )IIV感染の予防及びAI
 DS並びにその関連症候群圧の発症予防韮びに治療に
有効でめ9、またその有効成分であるフコイダンの細胞
毒性が低いことから、長期の投与にも好適に使用し得る
ものである。
The anti-HIV agent of the present invention has the following features: ) Prevention of IIV infection and AI
It is effective in preventing and treating the onset of DS and related syndrome pressure9, and its active ingredient, fucoidan, has low cytotoxicity, so it can be suitably used for long-term administration.

従って、本発明の抗1(IV剤は健常人のかかるHIV
感架の予防、無症候感染者(キャリア)の発症予防なら
びに治療及び発症したAIDSならびに戚患者の治療に
極めて有用である。
Therefore, the anti-1 (IV agent) of the present invention is effective against such HIV in healthy people.
It is extremely useful for preventing infection, preventing and treating asymptomatic carriers, and treating AIDS patients and their relatives who have developed AIDS.

〔実施例〕〔Example〕

以下、本発明抗HIV剤及びその効果をよシー層間らか
にするため、実施例を挙けて更に本発明を説明するが、
本発明はこれら実施例に限定されるものではない。なお
以下実施例におけるフコイダンは、シグヤ社のもの(カ
タログ番号F5631)を用いた。
Hereinafter, the present invention will be further explained with reference to examples in order to clearly demonstrate the anti-HIV agent of the present invention and its effects.
The present invention is not limited to these examples. Note that the fucoidan used in the following examples was manufactured by Shiguya Co., Ltd. (catalog number F5631).

実施例ル シチンーコレステロールーフコイダンからなるす?ソー
ム分散液(フコイダン懸濁g)を調製した〔保田立二9
等、免疫実験操作法ix 、p 2989−2994 
(1980)J。即ち、5mM卵黄レシチン、10mM
コレステロール、1 lnMホスファチシン酸及び1〜
tooay/−7jイダンを有機溶媒(クロロホルム:
メタノール=2 : 11 V/V)中に容積比が順次
2:1:1:1となるように混合した。有機溶媒を留去
後、緩衝液(リン酸緩衝生理食塩液−PBS )を加え
、ミキサー(Vortex m1xer )で攪拌して
、l−中にフコイダンを1■含有する分散g剤を調製し
た。
Example: Consisting of lucitin-cholesterol-fucoidan? A soma dispersion (fucoidan suspension g) was prepared [Tatsuji Yasuda 9
et al., Immunology Experimental Procedures ix, p. 2989-2994.
(1980)J. i.e. 5mM egg yolk lecithin, 10mM
Cholesterol, 1 lnM phosphatic acid and 1 to
tooay/-7j idan in an organic solvent (chloroform:
The mixture was sequentially mixed in methanol (2:11 V/V) at a volume ratio of 2:1:1:1. After distilling off the organic solvent, a buffer solution (phosphate buffered saline-PBS) was added and stirred with a mixer (Vortex m1xer) to prepare a dispersion g agent containing 1 part of fucoidan in 1 volume.

実施例2  薬理試験: (1)抗HIV活性 抗)IIV活性を下記の方法により試験した。Example 2 Pharmacological test: (1) Anti-HIV activity Anti)IIV activity was tested by the following method.

即ちs  5 X 103pfu/ff17!のfiI
V 50 ttlと種々濃度のフコイダン懸濁液(PB
S ) 200μgとを混合して、37℃下に30分間
インキュベートした。このウィルス混合g250μEを
s  2 X 10’ Ce1ls/d培地(RPMI
−1640+10%FCS )に調製したMT −4細
胞(m1yoshi 、 1.等、 Gann Mon
ogr、、 28 。
That is, s 5 X 103 pfu/ff17! fiI of
V 50 ttl and various concentrations of fucoidan suspension (PB
S) was mixed with 200 μg and incubated at 37° C. for 30 minutes. 250 μE of this virus mixture was added to s 2 × 10' Ce1ls/d medium (RPMI
-1640+10%FCS) prepared into MT-4 cells (Mlyoshi, 1. et al., Gann Mon.
ogr,, 28.

p219−228(1982)]の0.25−に加えて
4日間培養後、ウィルスの感染状況を間接螢光抗体法(
Harada S、等、 5cience 。
p219-228 (1982)], and after culturing for 4 days, the virus infection status was determined by indirect fluorescent antibody method (
Harada S, et al. 5science.

229 、p563−566 (1985);Take
uchi、 Y1等Jpn、 J、 Cancer R
es、 (Gann) 。
229, p563-566 (1985); Take
uchi, Y1 etc. Jpn, J, Cancer R
es, (Gann).

78、pH−15(1987)  〕によシ調ぺた。ウ
ィルス感染細胞()IIV抗原陽性細胞)の6分率←)
を算出した結果を下記第1表に示す。
78, pH-15 (1987)] Yoshicho Peta. 6% of virus-infected cells () IIV antigen-positive cells ←)
The results of the calculation are shown in Table 1 below.

第1表 上記結果よシ、本発明抗HIV剤は、有効にHIVウィ
ルス感染を防止することがわかる。
The above results in Table 1 show that the anti-HIV agent of the present invention effectively prevents HIV virus infection.

(2)  細胞毒性 フコイダンの細胞毒性を上記(1)に準じて試験した。(2) Cytotoxicity The cytotoxicity of fucoidan was tested according to (1) above.

即ち、lXl0’細胞/−に調製したMT−4,lfi
胞を種々濃度のフコイダンの存在下に、4日間培養後そ
の細胞数をカウントし、細胞毒性を評価した。結果を下
記第2表に示す。
That is, MT-4, lfi prepared in lXl0' cells/-
The cells were cultured for 4 days in the presence of various concentrations of fucoidan, and the number of cells was counted to evaluate cytotoxicity. The results are shown in Table 2 below.

@2表 上記結果よシ、フコイダンには著名な細胞毒性がないこ
とが明らかである。
From the above results in Table 2, it is clear that fucoidan has no significant cytotoxicity.

以上 出願人 株式会社日本抗体研死所 代理人 弁理士 有 賀 三 幸that's all Applicant: Japan Antibody Research Institute, Inc. Agent: Patent attorney Miyuki Yuga

Claims (1)

【特許請求の範囲】[Claims] 1、フコイダンを有効成分として含有することを特徴と
する抗HIV剤。
1. An anti-HIV agent characterized by containing fucoidan as an active ingredient.
JP14544088A 1988-06-13 1988-06-13 Anti-hiv agent Pending JPH01313433A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP14544088A JPH01313433A (en) 1988-06-13 1988-06-13 Anti-hiv agent

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP14544088A JPH01313433A (en) 1988-06-13 1988-06-13 Anti-hiv agent

Publications (1)

Publication Number Publication Date
JPH01313433A true JPH01313433A (en) 1989-12-18

Family

ID=15385290

Family Applications (1)

Application Number Title Priority Date Filing Date
JP14544088A Pending JPH01313433A (en) 1988-06-13 1988-06-13 Anti-hiv agent

Country Status (1)

Country Link
JP (1) JPH01313433A (en)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990009181A1 (en) * 1989-02-10 1990-08-23 Taiho Pharmaceutical Co., Ltd. Anti-hiv drug
WO1997047208A1 (en) * 1996-06-12 1997-12-18 Takara Shuzo Co., Ltd. Foods or drinks
US6812220B2 (en) 2001-08-29 2004-11-02 University Of British Columbia Pharmaceutical compositions and methods relating to fucans
WO2010086746A2 (en) 2009-01-28 2010-08-05 Life Science Nutrition As Compositions and methods of treating viral infections
WO2019074387A2 (en) 2017-10-12 2019-04-18 Bojan Pavlovic F-fucoidan, desulfated f-fucoidan, and its processed derivatives in terms of desulfated oligo-fucose as inhibitors of gastrointestinal infection

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990009181A1 (en) * 1989-02-10 1990-08-23 Taiho Pharmaceutical Co., Ltd. Anti-hiv drug
WO1997047208A1 (en) * 1996-06-12 1997-12-18 Takara Shuzo Co., Ltd. Foods or drinks
US6812220B2 (en) 2001-08-29 2004-11-02 University Of British Columbia Pharmaceutical compositions and methods relating to fucans
US7163930B2 (en) 2001-08-29 2007-01-16 The University Of British Columbia Pharmaceutical compositions and methods relating to fucans
WO2010086746A2 (en) 2009-01-28 2010-08-05 Life Science Nutrition As Compositions and methods of treating viral infections
US8697670B2 (en) 2009-01-28 2014-04-15 Life Science Nutrition As Compositions and methods of treating viral infections
US9789142B2 (en) 2009-01-28 2017-10-17 Life Science Nutrition As Method of increasing lean body mass
WO2019074387A2 (en) 2017-10-12 2019-04-18 Bojan Pavlovic F-fucoidan, desulfated f-fucoidan, and its processed derivatives in terms of desulfated oligo-fucose as inhibitors of gastrointestinal infection

Similar Documents

Publication Publication Date Title
US20090142427A1 (en) Composition and its Therapeutic Use
AU2007203159B2 (en) Compositions for therapeutic use comprising a vitamin, a metal salt and insulin or a growth hormone
JPH06505231A (en) Use of quinones in the treatment of cancer or AIDS
KR960000432B1 (en) Pharmaceutical composition
AU662883B2 (en) Use of trinitrobenzenes or carminic acid in the treatment of cancer or viral diseases
DE60032915T2 (en) GALLIUM COMPLEXES OF 3-HYDROXY-4-PYRONES FOR THE TREATMENT OF INFECTIONS CAUSED BY INTRA-CELLULAR PROCYNOTES, DNA AND RETRO VIRUSES
JPH01313433A (en) Anti-hiv agent
PL185678B1 (en) Novel applications of lysozime dimers
JPH05504774A (en) Use of metalloporphyrins to enhance AIDS treatment
JP3631245B2 (en) Use of hymenoptera venom for the manufacture of a medicament for the treatment of DNA virus infection
KR100302994B1 (en) New application as a medicament for multipotent Parapox immunogenic factors from attenuated non-immunogenic Foxvirus or Parapoxvirus
EP2722053B1 (en) Antibacterial agent for treating infectious diseases of bacterial origin
US5059592A (en) Composition for prevention and (or) treatment of AIDS
JP2589120B2 (en) Anti-HIV agent
JPH02191225A (en) Antiviral agent
JP2848634B2 (en) Drugs with immunosuppressive action
AU2003234637B2 (en) Methods and compositions for inhibiting HIV replication
CH694687A5 (en) Drugs to treat viral infections from Vernonia Oligocephalus.
US5229368A (en) Composition for prevention and (or) treatment of Aids
WO1991016916A1 (en) Antineoplastic agent
Osváth et al. Herpes Encephalitis
HRP920891A2 (en) Quinone preparation
JPH01172321A (en) Antiviral agent containing 6-0-substituted-d-gluco-delta-lactam
JP2013018729A (en) Potency enhancing oral preparation for therapeutic agent for alzheimer disease
WO1997000685A1 (en) Use of substituted pentose or hexose derivates in the treatment of aids and aids related neoplastic disorders