ANTHRAQUINONES AS A NEW CLASS OF ANTIVIRAL AGENTS AGAINST HUMAN-IMMUNODEFICIENCY-VIRUS

被引：141

作者：

SCHINAZI, RF

CHU, CK

BABU, JR

OSWALD, BJ

SAALMANN, V

CANNON, DL

ERIKSSON, BFH

NASR, M

机构：

[1] VET AFFAIRS MED CTR,ATLANTA,GA

[2] EMORY UNIV,SCH MED,DEPT PEDIAT,BIOCHEM PHARMACOL LAB,ATLANTA,GA 30322

[3] UNIV GEORGIA,COLL PHARM,DEPT MED CHEM & PHARMACOGNOSY,ATHENS,GA 30602

[4] NIAID,AIDS PROGRAM,BETHESDA,MD 20205

来源：

ANTIVIRAL RESEARCH | 1990年 / 13卷 / 05期

关键词：

Anthraquinone; Anti-HIV-1; activity; Hypericin; Reverse transcriptase;

D O I：

10.1016/0166-3542(90)90071-E

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Various anthraquinones substituted with hydroxyl, amino, halogen, carboxylic acid, substituted aromatic group, and sulfonate were tested to determine their activity against human immunodeficiency virus type 1 (HIV-1) in primary human lymphocytes. Among the compounds tested, polyphenolic and/or polysulfonate substituted anthraquinones were found to possess the most potent antiviral activity. Hypericin, an anthraquinone dimer previously shown to have activity against nonhuman retroviruses also exhibited anti-HIV-1 activity in lymphocytes. Some of the active anthraquinones inhibited HIV-1 reverse transcriptase. However, this enzyme inhibition was selective only for 1,2,5,8-tetrahydroanthraquinone and hypericin. Hypericin interacts nonspecifically with protein suggesting that this effect may dictate its inhibitory activity against the viral reverse transcriptase. © 1990.

引用

收藏

页码：265 / 272

页数：8

相关论文

共 29 条

[1] POTENT AND SELECTIVE ANTI-HTLV-III/LAV ACTIVITY OF 2',3'-DIDEOXYCYTIDINENE, THE 2',3'-UNSATURATED DERIVATIVE OF 2',3'-DIDEOXYCYTIDINE [J].

BALZARINI, J ;

PAUWELS, R ;

HERDEWIJN, P ;

DECLERCQ, E ;

COONEY, DA ;

KANG, GJ ;

DALAL, M ;

JOHNS, DG ;

BRODER, S .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1986, 140 (02) :735-742

[2]

BALZARINI J, 1987, MOL PHARMACOL, V32, P162

[3] STRUCTURE ACTIVITY RELATIONSHIPS OF PYRIMIDINE NUCLEOSIDES AS ANTIVIRAL AGENTS FOR HUMAN IMMUNODEFICIENCY VIRUS TYPE-1 IN PERIPHERAL-BLOOD MONONUCLEAR-CELLS [J].

CHU, CK ;

SCHINAZI, RF ;

AHN, MK ;

ULLAS, GV ;

GU, ZP .

JOURNAL OF MEDICINAL CHEMISTRY, 1989, 32 (03) :612-617

[4] COMPARATIVE ACTIVITY OF 2',3'-SATURATED AND UNSATURATED PYRIMIDINE AND PURINE NUCLEOSIDES AGAINST HUMAN IMMUNODEFICIENCY VIRUS TYPE-1 IN PERIPHERAL-BLOOD MONONUCLEAR-CELLS [J].

CHU, CK ;

SCHINAZI, RF ;

ARNOLD, BH ;

CANNON, DL ;

DOBOSZEWSKI, B ;

BHADTI, VB ;

GU, ZP .

BIOCHEMICAL PHARMACOLOGY, 1988, 37 (19) :3543-3548

[5] BROAD-SPECTRUM ANTIRETROVIRAL ACTIVITY OF 2',3'-DIDEOXYNUCLEOSIDES [J].

DAHLBERG, JE ;

MITSUYA, H ;

BLAM, SB ;

BRODER, S ;

AARONSON, SA .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1987, 84 (08) :2469-2473

[6]

DHANANJAYA KVR, 1987, INDIAN J BIOCHEM BIO, V24, P265

[7] PYROPHOSPHATE ANALOGS AS INHIBITORS OF HERPES-SIMPLEX VIRUS TYPE-1 DNA-POLYMERASE [J].

ERIKSSON, B ;

LARSSON, A ;

HELGSTRAND, E ;

JOHANSSON, NG ;

OBERG, B .

BIOCHIMICA ET BIOPHYSICA ACTA, 1980, 607 (01) :53-64

[8]

ERIKSSON BFH, 1989, ANTIMICROB AGENTS CH, V33, P633

[9] THE EFFICACY OF AZIDOTHYMIDINE (AZT) IN THE TREATMENT OF PATIENTS WITH AIDS AND AIDS-RELATED COMPLEX - A DOUBLE-BLIND, PLACEBO-CONTROLLED TRIAL [J].

FISCHL, MA ;

RICHMAN, DD ;

GRIECO, MH ;

GOTTLIEB, MS ;

VOLBERDING, PA ;

LASKIN, OL ;

LEEDOM, JM ;

GROOPMAN, JE ;

MILDVAN, D ;

SCHOOLEY, RT ;

JACKSON, GG ;

DURACK, DT ;

KING, D .

NEW ENGLAND JOURNAL OF MEDICINE, 1987, 317 (04) :185-191

[10] PHOSPHORYLATION OF 3'-AZIDO-3'-DEOXYTHYMIDINE AND SELECTIVE INTERACTION OF THE 5'-TRIPHOSPHATE WITH HUMAN-IMMUNODEFICIENCY-VIRUS REVERSE-TRANSCRIPTASE [J].

FURMAN, PA ;

FYFE, JA ;

STCLAIR, MH ;

WEINHOLD, K ;

RIDEOUT, JL ;

FREEMAN, GA ;

LEHRMAN, SN ;

BOLOGNESI, DP ;

BRODER, S ;

MITSUYA, H ;

BARRY, DW .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1986, 83 (21) :8333-8337