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单剂量给予9-(2-膦酰甲氧基乙基)腺嘌呤(PMEA)和9-(2-膦酰甲氧基乙基)-2,6-二氨基嘌呤(PMEDAP)用于体内预防逆转录病毒感染。

Single-dose administration of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) and 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) in the prophylaxis of retrovirus infection in vivo.

作者信息

Naesens L, Balzarini J, De Clercq E

机构信息

Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.

出版信息

Antiviral Res. 1991 Jul;16(1):53-64. doi: 10.1016/0166-3542(91)90058-y.

Abstract

9-(2-Phosphonylmethoxyethyl)adenine (PMEA) and 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) are selectively inhibitory to human immunodeficiency virus and other retroviruses. We have now investigated the effects of different PMEA and PMEDAP treatment schedules in newborn mice infected with Moloney murine sarcoma virus (MSV). Administration of a single dose of PMEA or PMEDAP on the day of MSV inoculation conferred a greater protective effect against MSV-induced tumor formation than when this dose was divided over two, four or seven injections per week. Also, the therapeutic index of PMEA and PMEDAP was increased if administered as a single dose. Furthermore, PMEA and PMEDAP afforded a marked antiviral protection if administered within one day before MSV infection. Thus, single doses of PMEA or PMEDAP, when administered shortly before or after MSV infection, appear to be effective in preventing the manifestations of the retroviral disease.

摘要

9-(2-膦酰甲氧基乙基)腺嘌呤(PMEA)和9-(2-膦酰甲氧基乙基)-2,6-二氨基嘌呤(PMEDAP)对人类免疫缺陷病毒和其他逆转录病毒具有选择性抑制作用。我们现在研究了不同的PMEA和PMEDAP治疗方案对感染莫洛尼氏鼠肉瘤病毒(MSV)的新生小鼠的影响。在接种MSV当天给予单剂量的PMEA或PMEDAP,比将该剂量每周分为两次、四次或七次注射时,对MSV诱导的肿瘤形成具有更大的保护作用。此外,如果单剂量给药,PMEA和PMEDAP的治疗指数会增加。此外,如果在MSV感染前一天内给药,PMEA和PMEDAP能提供显著的抗病毒保护。因此,在MSV感染前不久或之后给予单剂量的PMEA或PMEDAP,似乎能有效预防逆转录病毒疾病的表现。

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