Artemisinin and the antimalarial endoperoxides: from herbal remedy to targeted chemotherapy.
نویسندگان
چکیده
Artemisinin and its derivatives are endoperoxide-containing compounds which represent a promising new class of antimalarial drugs. In the presence of intraparasitic iron, these drugs are converted into free radicals and other electrophilic intermediates which then alkylate specific malaria target proteins. Combinations of available derivatives and other antimalarial agents show promise both as first-line agents and in the treatment of severe disease.
منابع مشابه
Artemisinin and a series of novel endoperoxide antimalarials exert early effects on digestive vacuole morphology.
Artermisinin and its derivatives are now the mainstays of antimalarial treatment; however, their mechanism of action is only poorly understood. We report on the synthesis of a novel series of epoxy-endoperoxides that can be prepared in high yields from simple starting materials. Endoperoxides that are disubstituted with alkyl or benzyl side chains show efficient inhibition of the growth of both...
متن کاملAntimalarial activities of Breynia Nivosa
Background & Aim: Antiplasmodial activity of leaf extract of Breynia nivosa was evaluated to ascertain the folkloric claim of its antimalarial activity. Experimental: The crude leaf extract (75 – 225 mg/kg), of Breynia nivosa was investigated for antiplasmodial activity against chloroquine sensitive Plasmodium berghei infections in mice. The antiplasmodial activity d...
متن کاملComparative ex vivo activity of novel endoperoxides in multidrug-resistant plasmodium falciparum and P. vivax.
The declining efficacy of artemisinin derivatives against Plasmodium falciparum highlights the urgent need to identify alternative highly potent compounds for the treatment of malaria. In Papua Indonesia, where multidrug resistance has been documented against both P. falciparum and P. vivax malaria, comparative ex vivo antimalarial activity against Plasmodium isolates was assessed for the artem...
متن کاملAntimalarial activities of Breynia Nivosa
Background & Aim: Antiplasmodial activity of leaf extract of Breynia nivosa was evaluated to ascertain the folkloric claim of its antimalarial activity. Experimental: The crude leaf extract (75 – 225 mg/kg), of Breynia nivosa was investigated for antiplasmodial activity against chloroquine sensitive Plasmodium berghei infections in mice. The antiplasmodial activity d...
متن کاملAntimalarial efficacy and drug interactions of the novel semi-synthetic endoperoxide artemisone in vitro and in vivo.
OBJECTIVES The in vitro and in vivo efficacy and drug-drug interactions of the novel semi-synthetic endoperoxide artemisone with standard antimalarials were investigated in order to provide the basis for the selection of the best partner drug. METHODS Antimalarial activity and drug interactions were evaluated in vitro against Plasmodium falciparum by the incorporation of [(3)H]hypoxanthine. I...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Microbiological reviews
دوره 60 2 شماره
صفحات -
تاریخ انتشار 1996