Neyts Johan, De Clercq Erik
Rega Institute for Medical Research, Minderbroedersstraat 10, 3000 Leuven, Belgium.
Antiviral Res. 2003 Jan;57(1-2):25-33. doi: 10.1016/s0166-3542(02)00197-3.
The era of antiviral chemotherapy started more than 50 years with the findings by Domagk and his colleagues that thiosemicarbazones showed activity against vaccinia virus. One of the derivatives, methisazone, was even investigated in the prophylaxis of smallpox. With the successful implementation of the smallpox vaccine, the use of methisazone was not further pursued. Should there be a threat of smallpox or other poxvirus infections, that could not be immediately controlled by vaccination, a therapeutic intervention could be envisaged based on several therapeutic strategies targeted at such cellular enzymes as IMP dehydrogenase, SAH hydrolase, OMP decarboxylase and CTP synthetase, as well as viral enzymes such as the DNA polymerase. Most advanced as a therapeutic or early prophylactic modality to tackle poxvirus infection is cidofovir, which was found active (i) in vitro against all poxviruses studied so far; (ii) in vivo, against vaccinia and cowpox virus infections in experimental animal models; as well as (iii) some human poxvirus infections, such as molluscum contagiosum. In case of an inadvertent poxvirus epidemic, antiviral therapy (i.e. with cidofovir) will offer the possibility to provide short-term prophylaxis, or therapy. Cidofovir should also allow to treat severe complications of vaccination as may happen in for example immunosuppressed patients.
抗病毒化疗时代始于50多年前,当时多马克及其同事发现硫代氨基脲对痘苗病毒有活性。其中一种衍生物甲吲噻腙甚至被用于天花的预防研究。随着天花疫苗的成功推广,甲吲噻腙的使用未再继续。如果出现天花或其他痘病毒感染的威胁,而疫苗接种又无法立即控制,那么可以设想基于针对IMP脱氢酶、SAH水解酶、OMP脱羧酶和CTP合成酶等细胞酶以及DNA聚合酶等病毒酶的几种治疗策略进行治疗干预。作为治疗或早期预防痘病毒感染的最先进药物是西多福韦,它被发现:(i)在体外对迄今为止研究的所有痘病毒均有活性;(ii)在体内,对实验动物模型中的痘苗病毒和牛痘病毒感染有效;以及(iii)对一些人类痘病毒感染,如传染性软疣有效。万一发生意外的痘病毒流行,抗病毒治疗(即使用西多福韦)将提供短期预防或治疗的可能性。西多福韦还应能够治疗例如免疫抑制患者可能发生的严重疫苗接种并发症。