Anti-picornavirus activity of synthetic flavon-3-yl esters

被引:17
作者
Conti, C
Mastromarino, P
Sgro, R
Desideri, N
机构
[1] Univ La Sapienza, Dept Pharmaceut Studies, I-00185 Rome, Italy
[2] Univ La Sapienza, Sch Med, Inst Microbiol, I-00185 Rome, Italy
关键词
anti-rhinovirus activity; anti-poliovirus activity; flavonoids;
D O I
10.1177/095632029800900607
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The in vitro antiviral activity against picornaviruses (rhinovirus serotype 1B and 14, and poliovirus type 2) of new synthetic 3-hydroxyflavones, 3-acetoxyflavones, and substituted cinnamic and benzoic acid flavon-3-yl esters was evaluated. The maximum non-toxic concentration of compounds was determined in a human cell line (HeLa) suitable for the replication of the three viruses. Their antiviral potency was measured by a plaque reduction assay. Generally, rhinoviruses exhibited a higher sensitivity to the new flavonoids than poliovirus. Flavones, with sterically small substituents in position 3, showed good activity against both rhinoviruses tested. However, the introduction of bulky substituents in the same position resulted in analogues with a higher toxicity and often with a lower efficacy.
引用
收藏
页码:511 / 515
页数:5
相关论文
共 24 条
[1]   A COMPARATIVE TEST OF 15 COMPOUNDS AGAINST ALL KNOWN HUMAN RHINOVIRUS SEROTYPES AS A BASIS FOR A MORE RATIONAL SCREENING-PROGRAM [J].
ANDRIES, K ;
DEWINDT, B ;
SNOEKS, J ;
WILLEBRORDS, R ;
STOKBROEKX, R ;
LEWI, PJ .
ANTIVIRAL RESEARCH, 1991, 16 (03) :213-225
[2]   2 GROUPS OF RHINOVIRUSES REVEALED BY A PANEL OF ANTIVIRAL COMPOUNDS PRESENT SEQUENCE DIVERGENCE AND DIFFERENTIAL PATHOGENICITY [J].
ANDRIES, K ;
DEWINDT, B ;
SNOEKS, J ;
WOUTERS, L ;
MOEREELS, H ;
LEWI, PJ ;
JANSSEN, PAJ .
JOURNAL OF VIROLOGY, 1990, 64 (03) :1117-1123
[3]   4',6-DICHLOROFLAVAN (BW683C), A NEW ANTI-RHINOVIRUS COMPOUND [J].
BAUER, DJ ;
SELWAY, JWT ;
BATCHELOR, JF ;
TISDALE, M ;
CALDWELL, IC ;
YOUNG, DAB .
NATURE, 1981, 292 (5821) :369-370
[4]   SYNTHESIS AND ANTIRHINOVIRUS ACTIVITY OF HALOGEN-SUBSTITUTED ISOFLAVENES AND ISOFLAVANS [J].
BURALI, C ;
DESIDERI, N ;
STEIN, ML ;
CONTI, C ;
ORSI, N .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1987, 22 (02) :119-123
[5]   3-METHYLQUERCETIN IS A POTENT AND SELECTIVE INHIBITOR OF POLIOVIRUS RNA-SYNTHESIS [J].
CASTRILLO, JL ;
VANDENBERGHE, D ;
CARRASCO, L .
VIROLOGY, 1986, 152 (01) :219-227
[6]   MECHANISM OF ACTION OF THE ANTIRHINOVIRUS FLAVANOID 4', 6-DICYANOFLAVAN [J].
CONTI, C ;
TOMAO, P ;
GENOVESE, D ;
DESIDERI, N ;
STEIN, ML ;
ORSI, N .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1992, 36 (01) :95-99
[7]   EFFECT OF ISOFLAVANS AND ISOFLAVENES ON RHINOVIRUS-1B AND ITS REPLICATION IN HELA-CELLS [J].
CONTI, C ;
ORSI, N ;
STEIN, ML .
ANTIVIRAL RESEARCH, 1988, 10 (1-3) :117-127
[8]   ACTIVITIES AND MECHANISMS OF ACTION OF HALOGEN-SUBSTITUTED FLAVANOIDS AGAINST POLIOVIRUS TYPE-2 INFECTION INVITRO [J].
CONTI, C ;
GENOVESE, D ;
SANTORO, R ;
STEIN, ML ;
ORSI, N ;
FIORE, L .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1990, 34 (03) :460-466
[9]   SYNTHESIS AND ANTIRHINOVIRUS ACTIVITY OF CYANO AND AMIDINO SUBSTITUTED FLAVANOIDS [J].
CONTI, C ;
DESIDERI, N ;
ORSI, N ;
SESTILI, I ;
STEIN, ML .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1990, 25 (09) :725-730
[10]   4'-HYDROXY-3-METHOXYFLAVONES WITH POTENT ANTIPICORNAVIRUS ACTIVITY [J].
DEMEYER, N ;
HAEMERS, A ;
MISHRA, L ;
PANDEY, HK ;
PIETERS, LAC ;
VANDENBERGHE, DA ;
VLIETINCK, AJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (02) :736-746