Trioxaquine PA1259 alkylates heme in the blood-feeding parasite Schistosoma mansoni.

نویسندگان

  • Vincent Pradines
  • Julien Portela
  • Jérôme Boissier
  • Frédéric Coslédan
  • Bernard Meunier
  • Anne Robert
چکیده

Trioxaquine PA1259 is an efficient drug on larval- and adult-stage schistosomes, able to alkylate heme inside worms treated with it, leading to the formation of covalent heme-drug adducts. Such a mechanism, similar to one reported for other trioxaquines in Plasmodium, indicates that heme may be a common target of these trioxane-based drugs in different blood-feeding parasites.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

The antimalarial trioxaquine DU1301 alkylates heme in malaria-infected mice.

The in vivo alkylation of heme by the antimalarial trioxaquine DU1301 afforded covalent heme-drug adducts that were detected in the spleens of Plasmodium sp.-infected mice. This result indicates that the alkylation capacities of trioxaquines in mammals infected with Plasmodium strains are similar to that of artemisinin, a natural antimalarial trioxane-containing drug.

متن کامل

Arylmethylamino steroids as antiparasitic agents

In search of antiparasitic agents, we here identify arylmethylamino steroids as potent compounds and characterize more than 60 derivatives. The lead compound 1o is fast acting and highly active against intraerythrocytic stages of chloroquine-sensitive and resistant Plasmodium falciparum parasites (IC50 1-5 nM) as well as against gametocytes. In P. berghei-infected mice, oral administration of 1...

متن کامل

Inhibition of heme aggregation by chloroquine reduces Schistosoma mansoni infection.

Adult Schistosoma mansoni digest large amounts of host hemoglobin and release potentially toxic heme inside their guts. We have previously demonstrated that free heme in S. mansoni is detoxified through aggregation, forming hemozoin (Hz). Possible mechanisms of heme aggregation and the effects of chloroquine (CLQ) on formation of Hz and on the viability of this parasite have now been investigat...

متن کامل

Kicking in the Guts: Schistosoma mansoni Digestive Tract Proteins are Potential Candidates for Vaccine Development

Schistosomiasis is a debilitating disease that represents a major health problem in at least 74 tropical and subtropical countries. Current disease control strategies consist mainly of chemotherapy, which cannot prevent recurrent re-infection of people living in endemic area. In the last decades, many researchers made a remarkable effort in the search for an effective vaccine to provide long-te...

متن کامل

Antioxidant effects of gold nanoparticles on Schistosoma mansoni induced granuloma, in vitro

Objective(s): Schistosomiasis and hepatitis C virus [HCV] co-infection is common among the Egyptian population. Co-infected patients have higher rate of chronic hepatitis, cirrhosis and hepatocellular carcinoma. The aim of the present study was to investigate the potential role of gold nanoparticles on granuloma in vitro. Materials and Methods: In the current study, granulocytes were isolated f...

متن کامل

ذخیره 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 نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Antimicrobial agents and chemotherapy

دوره 55 5  شماره 

صفحات  -

تاریخ انتشار 2011