JPS63253026A - Aids virus multiplication inhibitor - Google Patents
Aids virus multiplication inhibitorInfo
- Publication number
- JPS63253026A JPS63253026A JP8717887A JP8717887A JPS63253026A JP S63253026 A JPS63253026 A JP S63253026A JP 8717887 A JP8717887 A JP 8717887A JP 8717887 A JP8717887 A JP 8717887A JP S63253026 A JPS63253026 A JP S63253026A
- Authority
- JP
- Japan
- Prior art keywords
- dextran sulfate
- case
- aids virus
- hiv
- addition salt
- 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 abstract description 10
- 239000003112 inhibitor Substances 0.000 title abstract description 4
- 229960000633 dextran sulfate Drugs 0.000 claims abstract description 13
- 239000004480 active ingredient Substances 0.000 claims abstract description 4
- 150000003839 salts Chemical class 0.000 claims abstract description 4
- 239000003513 alkali Substances 0.000 claims abstract 3
- 239000000126 substance Substances 0.000 claims abstract 3
- 241000725303 Human immunodeficiency virus Species 0.000 claims description 17
- 239000003966 growth inhibitor Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 abstract description 9
- 239000003814 drug Substances 0.000 abstract description 5
- 239000000243 solution Substances 0.000 abstract description 5
- 229940079593 drug Drugs 0.000 abstract description 4
- 238000000034 method Methods 0.000 abstract description 4
- 238000007911 parenteral administration Methods 0.000 abstract description 4
- 231100000053 low toxicity Toxicity 0.000 abstract description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 abstract description 2
- 239000002775 capsule Substances 0.000 abstract description 2
- 239000008298 dragée Substances 0.000 abstract description 2
- 239000008103 glucose Substances 0.000 abstract description 2
- 239000008187 granular material Substances 0.000 abstract description 2
- 238000002347 injection Methods 0.000 abstract description 2
- 239000007924 injection Substances 0.000 abstract description 2
- 239000000843 powder Substances 0.000 abstract description 2
- 239000002904 solvent Substances 0.000 abstract description 2
- 239000007940 sugar coated tablet Substances 0.000 abstract description 2
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 239000008354 sodium chloride injection Substances 0.000 abstract 1
- 210000004027 cell Anatomy 0.000 description 20
- 229920003045 dextran sodium sulfate Polymers 0.000 description 8
- 238000002474 experimental method Methods 0.000 description 7
- 230000035755 proliferation Effects 0.000 description 6
- 208000030507 AIDS Diseases 0.000 description 4
- 230000007850 degeneration Effects 0.000 description 4
- 239000000427 antigen Substances 0.000 description 3
- 102000036639 antigens Human genes 0.000 description 3
- 108091007433 antigens Proteins 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- 241000699666 Mus <mouse, genus> Species 0.000 description 2
- 241000283973 Oryctolagus cuniculus Species 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- BLFLLBZGZJTVJG-UHFFFAOYSA-N benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 description 2
- 230000007717 exclusion Effects 0.000 description 2
- 231100000957 no side effect Toxicity 0.000 description 2
- 241001430294 unidentified retrovirus Species 0.000 description 2
- 230000005727 virus proliferation Effects 0.000 description 2
- UJQBOUAGWGVOTI-XSSZXYGBSA-N 1-[(2r,4s,5r)-4-azido-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@](O)(N=[N+]=[N-])C1 UJQBOUAGWGVOTI-XSSZXYGBSA-N 0.000 description 1
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 1
- 229920000936 Agarose Polymers 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- 241000233866 Fungi Species 0.000 description 1
- 239000004378 Glycyrrhizin Substances 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 206010020565 Hyperaemia Diseases 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 206010061598 Immunodeficiency Diseases 0.000 description 1
- 208000029462 Immunodeficiency disease Diseases 0.000 description 1
- 102100034343 Integrase Human genes 0.000 description 1
- 102000015696 Interleukins Human genes 0.000 description 1
- 108010063738 Interleukins Proteins 0.000 description 1
- 208000007766 Kaposi sarcoma Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 208000001388 Opportunistic Infections Diseases 0.000 description 1
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 description 1
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 231100000215 acute (single dose) toxicity testing Toxicity 0.000 description 1
- 238000011047 acute toxicity test Methods 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000036436 anti-hiv Effects 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- VFBJEDFCUUCMBQ-UHFFFAOYSA-O azanium;sodium;antimony(3+);oxygen(2-);tungsten Chemical compound [NH4+].[O-2].[Na+].[Sb+3].[W] VFBJEDFCUUCMBQ-UHFFFAOYSA-O 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 235000010216 calcium carbonate Nutrition 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 210000001728 clone cell Anatomy 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000000120 cytopathologic effect Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 238000011257 definitive treatment Methods 0.000 description 1
- 238000004925 denaturation Methods 0.000 description 1
- 230000036425 denaturation Effects 0.000 description 1
- 230000010460 detection of virus Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000001605 fetal effect Effects 0.000 description 1
- LPLVUJXQOOQHMX-UHFFFAOYSA-N glycyrrhetinic acid glycoside Natural products C1CC(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2=O)C(O)=O)C)(C)CC2)(C)C2C(C)(C)C1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O LPLVUJXQOOQHMX-UHFFFAOYSA-N 0.000 description 1
- 229960004949 glycyrrhizic acid Drugs 0.000 description 1
- UYRUBYNTXSDKQT-UHFFFAOYSA-N glycyrrhizic acid Natural products CC1(C)C(CCC2(C)C1CCC3(C)C2C(=O)C=C4C5CC(C)(CCC5(C)CCC34C)C(=O)O)OC6OC(C(O)C(O)C6OC7OC(O)C(O)C(O)C7C(=O)O)C(=O)O UYRUBYNTXSDKQT-UHFFFAOYSA-N 0.000 description 1
- 235000019410 glycyrrhizin Nutrition 0.000 description 1
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 description 1
- 159000000011 group IA salts Chemical class 0.000 description 1
- 210000002443 helper t lymphocyte Anatomy 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 230000007813 immunodeficiency Effects 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000000391 magnesium silicate Substances 0.000 description 1
- 235000019792 magnesium silicate Nutrition 0.000 description 1
- 229910052919 magnesium silicate Inorganic materials 0.000 description 1
- ZADYMNAVLSWLEQ-UHFFFAOYSA-N magnesium;oxygen(2-);silicon(4+) Chemical compound [O-2].[O-2].[O-2].[Mg+2].[Si+4] ZADYMNAVLSWLEQ-UHFFFAOYSA-N 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 230000010076 replication Effects 0.000 description 1
- 210000003296 saliva Anatomy 0.000 description 1
- 210000000582 semen Anatomy 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 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 1
- 229960005314 suramin Drugs 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
（産業上の利用分計）
本発明は、デキストラン硫酸を有効成分として含有する
エイズ・ウィルス増殖抑制剤に関するものである。DETAILED DESCRIPTION OF THE INVENTION (Industrial Application) The present invention relates to an AIDS virus growth inhibitor containing dextran sulfate as an active ingredient.
（従来技術及び問題点）
後天性免疫不全症候群（ＡＩＤＳ、 エイズ）は、１９
８２年に米国で発見された疾患である。その原因はウィ
ルスによるものであり、このライ・ルスは発見者等によ
り、Ｌｙｍｐｈｏａｄｅｎａｐｔｈｙ ａｓｓｏｃｉａ
ｔｅｄ ｖｉｒｕｓ（ＬＡＹ）、またはＨｕｍａｎ Ｔ
ｌｙｍｐｈｏｔｒｏｐｉｅ ｒｅｔｒｏ ｖｉｒｕｓｔ
ｙｐｅ ＩＩＩ （ＨＴＬＶ−ＩＩ ）と命名きれた。(Prior art and problems) Acquired immunodeficiency syndrome (AIDS) is 19
This disease was discovered in the United States in 1982. The cause is due to a virus, and the discoverer and others believe that Lymphoidea is caused by a virus.
ted virus (LAY), or Human T
lymphotropie retro virust
ype III (HTLV-II).
しかし現在では一般に、Ｈｕｍａｎ Ｉｍｍｕｎｏｄｅ
ｆｉｃｉｅｎｃｙ ｖｉｒｕｓ（ＨＩＶ）と表現されて
いる。これはヒトレトロウィルス、に属し、このウィル
スによりリンパ球のヘルパーＴ細胞が破壊され、その結
果、細胞性免疫不全となり、原虫、真菌、ウィルス、細
菌などによる日和見感染、カポシ肉腫などが発生する死
亡率の高い重篤な疾患である。このＨＩＶはエイズ患者
の血液及び精液や唾液中に存在し、輸血その他の原因に
よって感染する。However, currently, Human Immunode
ficiency virus (HIV). This virus belongs to the human retrovirus, and this virus destroys lymphoid helper T cells, resulting in cellular immunodeficiency, leading to opportunistic infections caused by protozoa, fungi, viruses, bacteria, etc., and death due to Kaposi's sarcoma, etc. It is a serious disease with a high incidence. This HIV exists in the blood, semen, and saliva of AIDS patients, and is transmitted through blood transfusions and other causes.
この疾患に対する治療剤は従来からいくつか報告きれて
いる。それらの多くは、ＨＩＶ中に含まれているレトロ
ウィルスの複製に重要な役割をもつ逆転写酵素活性を抑
制する作用を持つもので、例えば３゛−アジド−デオキ
シチミジン、２゛、３′−ジブオキシシチジン、スラミ
ン、又はＨＰＡ−２３などがあるが、これらは副作用が
強い欠点があり、また工業的な製造が不可能である。Several therapeutic agents for this disease have been reported so far. Many of them have the effect of suppressing reverse transcriptase activity, which plays an important role in the replication of retroviruses contained in HIV, such as 3'-azido-deoxythymidine, 2', 3'- There are dibuoxycytidine, suramin, HPA-23, etc., but these have the disadvantage of strong side effects and are impossible to produce industrially.
これに加え、インターロイキンπ等が免疫欠損に対する
免疫促進剤として使用されている。In addition, interleukin π and the like are used as immune promoters for immune deficiencies.
最近、副作用のないグリチルリチンが注目されているが
、現状では決定的な治療法は無く、言らに多くの有用な
治療薬め開亮が急務である。Recently, glycyrrhizin, which has no side effects, has been attracting attention, but there is currently no definitive treatment, and there is an urgent need for the development of many useful therapeutic drugs.
本発明者等は、種々の薬剤を検索中、従来から高詣血症
剤として用いられているデキストラン硫酸がＨＩＶ（７
７増殖を有効に抑制する作用があることを発見し、本発
明を完成するに至ったものである。While searching for various drugs, the present inventors found that dextran sulfate, which has traditionally been used as a hyperemia drug, was found to be effective against HIV (7
The inventors discovered that the present invention has the effect of effectively suppressing the proliferation of 7.
（発明の構成）
本発明に係るエイズ・ウィルス増殖抑制剤は、次式で表
わされるデキストラン硫酸を有効成分とする。(Structure of the Invention) The AIDS virus proliferation inhibitor according to the present invention contains dextran sulfate represented by the following formula as an active ingredient.
上記デキストラン硫酸は顕著なエイズ・ウィルス増殖抑
制作用を示し、エイズ・ウィルス増殖抑制剤として用い
ることができる。またデキストラン硫酸は低毒性で、か
、つ副作用がない利点があり、通常は、その製剤上許容
される塩、即ちデキストラン硫酸のアルカリ塩、例えば
デキストラン硫酸ナトリウム塩の形でエイズ患者に投与
することが可能である。The above-mentioned dextran sulfate exhibits a remarkable effect of inhibiting the proliferation of AIDS virus and can be used as an AIDS virus proliferation inhibitor. In addition, dextran sulfate has the advantage of low toxicity and no side effects, and is usually administered to AIDS patients in the form of a pharmaceutically acceptable salt, that is, an alkaline salt of dextran sulfate, such as dextran sulfate sodium salt. is possible.
投与する方法としては経口、或いは非経口のいずれをも
選択でき、また投与量は患者の年齢、症状等により異な
るが、一般には、経口投与では成人−日当り４５０〜９
００ ｍｇの範囲で用いることにより、所期の効果が期
待できる。Either oral or parenteral administration can be selected, and the dosage varies depending on the patient's age, symptoms, etc., but in general, oral administration is 450 to 90 mg/day for adults.
By using within the range of 0.00 mg, the desired effect can be expected.
剤形は、製剤上許容される無害の一種或いは数種の賦形
剤、例えば炭酸水素ナトリウ゛ム、塩化ナトリウム、乳
糖、バレイショデンブン、アルギン酸ナトリウム、ケイ
酸マグネシウム、炭酸カルシウム、ヒドロキシプロピル
セルロース等を配剤し、常法により散剤、顆粒剤、糖衣
錠、及びカプセル剤等とすることができる。The dosage form contains one or more pharmaceutically acceptable harmless excipients, such as sodium bicarbonate, sodium chloride, lactose, potato starch, sodium alginate, magnesium silicate, calcium carbonate, hydroxypropyl cellulose, etc. However, it can be made into powders, granules, sugar-coated tablets, capsules, etc. by conventional methods.
非経口の場合の投与量は、一般には、成人−日当り３０
０ ｍｇの範囲で用いられる。注射剤の場合の溶媒は、
例えば生理食塩液、或いは５％ブドウ糖液が適当である
。For parenteral administration, the dosage is generally 30 mg/day for adults.
Used in the range of 0 mg. The solvent for injections is
For example, physiological saline or 5% glucose solution is suitable.
以下にデキストラン硫酸のエイズ・ウィルス増殖抑制作
用についての実験例を掲げるが、これらの実験によりデ
キストラン硫酸がエイズ・ウィルス（ＨＩＶ）の増殖を
強く抑制し、かつ感染細胞の変性抑制効果のあることが
明らかになった。Examples of experiments on the inhibitory effect of dextran sulfate on the proliferation of AIDS virus are listed below, and these experiments demonstrate that dextran sulfate strongly inhibits the proliferation of AIDS virus (HIV) and has the effect of suppressing the degeneration of infected cells. It was revealed.
［実験例］
（材料）
（１）細胞とウィルス
感染細胞はＭｏ１ｔ−４ｃｌｏｎｅ Ｎｏ、８を用いた
。ウィルスはＭｏ１ｔ−４／ＨＩＶ産生株より得たも・
のを使用した。[Experimental Example] (Materials) (1) Molt-4 clone No. 8 was used as cells and virus-infected cells. The virus was obtained from the Molt-4/HIV producing strain.
I used the.
（り被験薬は、デキストラン硫酸ナトリウム（和光純薬
−５ｉｇｍａ社製）を用いた。(The test drug used was dextran sodium sulfate (Wako Pure Chemical-5Igma).
［Ｉ］感染細胞の変性抑制実験
本実験は、デキストラン硫酸の、Ｍｏ１ｔ−４ａｌｏｎ
ｅＮＯ１８細胞に対するＨＩＶの感染細胞変性の抑制効
果に関するものであり、アガロースなしの培養条件にお
いて実施した。[I] Experiment for suppressing degeneration of infected cells This experiment was conducted using dextran sulfate, Molt-4alon.
This study relates to the inhibitory effect of HIV-infected cell degeneration on eNO18 cells, and was conducted under culture conditions without agarose.
３Ｘ１０’個のＭｏ１ｔ−４ａｌｏｎｅ Ｎｏ、８細胞
に、６Ｘ１０”ＰＦＵのＨＩＶを感染きせ、種々の濃度
のデキストラン硫酸ナトリウム水溶液を加えて、４日間
、抗生物質と１０％胎児ウシ血漬を含むＲＰＭ１１６４
０培養液で培養した。3 x 10' Molt-4alone No. 8 cells were infected with 6 x 10'' PFU of HIV and treated with RPM1164 containing antibiotics and 10% fetal bovine blood for 4 days by adding various concentrations of dextran sodium sulfate aqueous solution.
0 culture solution.
その後、上記培養液を攪拌して半量ずつに分割し、一方
に培養液に混和した種々の濃度のデキストラン硫酸ナト
リウム水溶液を加え、きらに３日間培養した。また他方
の半量をトリバンブルー排除法で生細胞数を計測した。Thereafter, the above-mentioned culture solution was stirred and divided into halves, and to one half was added dextran sodium sulfate aqueous solutions of various concentrations mixed with the culture solution, and the kira was cultured for 3 days. In addition, the number of living cells in the other half was counted using the Trivan blue exclusion method.
対照として、非感染細胞にも同様の実験を行なった。As a control, similar experiments were performed on uninfected cells.
トリバンブルー排除法により、７日間の培養において、
デキストラン硫酸ナトリウム０．７５から４、０００μ
ｇ／ｍ ｆｆｉの用量で抑制がみられた。その結果を図
に示す。In 7 days of culture by Trivan blue exclusion method,
Dextran sulfate sodium 0.75 to 4,000μ
Suppression was seen at doses of g/m ffi. The results are shown in the figure.
図は、ＨＩＶ非感染細胞、及びＨＩＶ感染細胞の増殖に
対し、デキストラン硫酸ナトリウムの及ぼす影響を表わ
す。図中、夫々、口はＨＩＶ非感染細胞、羽はＨＩＶ感
染細胞を示す。ＨＩＶ感染細胞は、０．７５〜４、 ｏ
ｏｏＩ１ｇ／ｍ ｆｆの量のデキストラン硫酸ナトリウ
ムにより変性が抑制きれて活性化し、増殖するのがわか
る。The figure depicts the effect of dextran sodium sulfate on the proliferation of HIV-uninfected cells and HIV-infected cells. In the figure, the mouth represents an HIV-uninfected cell, and the wing represents an HIV-infected cell. HIV-infected cells are 0.75-4, o
It can be seen that dextran sodium sulfate in an amount of ooI1g/mff suppresses denaturation, activates the cells, and causes proliferation.
一方、非感染細胞に対するデキストラン硫酸ナトリウム
の細胞変性効果は、そのＩＤ５０が４ ＋ｎｇ／ｍ １
以上であった。On the other hand, the cytopathic effect of dextran sodium sulfate on uninfected cells is that its ID50 is 4 + ng/m 1
That was it.
［１ｒ］ウイルス抗原の検出
感染細胞について、抗ＨＩＶ抗体陽性血清を使用した間
接螢光抗体法を行なった。デキストラン硫、酸ナトリウ
ムは、１２．５〜４０００ Ｉｔ ｇ／ｍ ｌ （７）
濃度範囲においてＨＩＶ抗原陽性細胞の出現を２％以下
に抑制した。これより低い濃度では、次第・に陽性細胞
の割合が増加した。[1r] Detection of virus antigen Indirect fluorescent antibody method using anti-HIV antibody positive serum was performed on infected cells. Dextran sulfate, acid sodium is 12.5-4000 It g/ml (7)
The appearance of HIV antigen-positive cells was suppressed to 2% or less over a range of concentrations. At lower concentrations, the percentage of positive cells gradually increased.
その結果を図に示す。折れ線（□）は、各種の濃度にお
けるＨＩＶ陽性細胞の割合を％で示す。The results are shown in the figure. The broken line (□) indicates the percentage of HIV-positive cells at various concentrations.
（急性毒性試験）
デキストラン硫酸ナトリウムについてのＩＤ５０は以下
の通りであり、低毒性である。(Acute toxicity test) The ID50 of dextran sodium sulfate is as follows, indicating low toxicity.
（１）経口投与
マウス・・・・・・・・・２１０００ ｍｇ／ｋｇ（２
）非経口投与（静注）
マウス・・・・・・・・、８１１５８００ ｍｇ／ｋｇ
マウス・・・・・・・・ＭＬ７０００ ｍｇ／ｋｇウサ
ギ・・・・・・・・雄２０５００ ｍｇ／ｋｇウサギ・
・・・・・・・雌１９０００ ｍｇ／ｋｇ(1) Orally administered mice...21000 mg/kg (2
) Parenteral administration (intravenous injection) Mouse..., 8115800 mg/kg
Mouse...ML7000 mg/kg Rabbit...Male 20500 mg/kg Rabbit
...Female 19000 mg/kg
図面は、実験例におけるＭｏ１ｔ−４ｃｌｏｎｅ細胞に
対する変性抑制効果の実験、及びウィルス抗原の検出実
験の結果を示す図である。The drawings are diagrams showing the results of an experiment for suppressing degeneration of Molt-4 clone cells and an experiment for detecting a virus antigen in an experimental example.
Claims (1)
るアルカリ付加塩を有効成分として含有するエイズ・ウ
ィルス増殖抑制剤。[Claims] An AIDS virus growth inhibitor containing dextran sulfate represented by the formula: ▲Mathical formula, chemical formula, table, etc.▼ and a pharmaceutically acceptable alkali addition salt thereof as active ingredients.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP8717887A JPS63253026A (en) | 1987-04-10 | 1987-04-10 | Aids virus multiplication inhibitor |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP8717887A JPS63253026A (en) | 1987-04-10 | 1987-04-10 | Aids virus multiplication inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS63253026A true JPS63253026A (en) | 1988-10-20 |
Family
ID=13907734
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP8717887A Pending JPS63253026A (en) | 1987-04-10 | 1987-04-10 | Aids virus multiplication inhibitor |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS63253026A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1990009181A1 (en) * | 1989-02-10 | 1990-08-23 | Taiho Pharmaceutical Co., Ltd. | Anti-hiv drug |
| JP2002512180A (en) * | 1998-04-21 | 2002-04-23 | インフェクティオ ルシェルシェ インコーポレイティド | Formulation for prevention or treatment of diseases affecting mucous membrane or skin, or for prevention of pregnancy, and applicator for reaching topical formulation into mucosal cavity |
-
1987
- 1987-04-10 JP JP8717887A patent/JPS63253026A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1990009181A1 (en) * | 1989-02-10 | 1990-08-23 | Taiho Pharmaceutical Co., Ltd. | Anti-hiv drug |
| JP2002512180A (en) * | 1998-04-21 | 2002-04-23 | インフェクティオ ルシェルシェ インコーポレイティド | Formulation for prevention or treatment of diseases affecting mucous membrane or skin, or for prevention of pregnancy, and applicator for reaching topical formulation into mucosal cavity |
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