Infectious diseases, the leading cause of premature deaths in the world, are killing almost 50.000 people every day.1 Despite the existence of a wide variety of antibacterial agents, the treatment of infectious diseases is a frequent problem in modern-day-medicine due to a significant increase of bacterial resistance to several antibiotics.2 One way to prevent antibiotic resistance is using new compounds that a...
Malaria a serious parasitic disease, spread by mosquitoes from Anopheles species, is still the most devastating in the world. It has been estimated that in the last 20 years mortality from malaria has doubled (it is currently 3 millions deaths annually), and a major factor responsible for this increase is the resistance of malaria parasites to antimalarial drugs.1 Consequently, there is an urgent need to discov...
Infectious diseases caused by bacteria, fungi, viruses and parasites are a major threat to public health, despite great progress in therapy. The impact of infectious diseases is especially important in developing countries, where drugs are limited and the emergence of widespread drug resistance is a reality.1 Malaria is a major parasitic disease in the tropical and subtropical regions of the world. It is respon...
We have isolated three -carboline indole alkaloids (1-3) from the MeOH extract of the leaves of Tabernaemontana elegans. The chemical structures of these novel entities were established by means of spectroscopic techniques including 2D NMR spectroscopic experiments. The new skeletal features of compounds 1 and 2 were the presence of a two-carbon unit, attached to a structurally related -carboline skeleton, re...
The overexpression of P- glycoprotein (P-gp) is one of the mechanisms of multidrug resistance (MDR), responsible for the failure of cancer treatment. One strategy to restore the effectiveness of the anti-cancer drugs is to co-administer compounds that are not toxic themselves, but inhibit these efflux pumps. These compounds have been called MDR inhibitors, MDR modulators, MDR reversal agents or chemosensitizers...
All living cells contain genes encoding multidrug transporters and some of them play an important role in conferring drug resistance in mammalian cancer cells and in microbial pathogens such as Staphylococcus aureus, Enterococcus faecalis, Candida albicans, Plasmodium falciparum, and Leishmania donovani. The over-expression of P- glycoprotein (P-gp) is one of the principal mechanisms of multidrug resistance (MD...
Resistance of cancer cells to multiple classes of structurally and mechanistically unrelated antitumor drugs can be defined as multidrug resistance (MDR), and it is one of the major causes of chemotherapy failure. The most significant mechanism of MDR, referred as typical or classical, results from altered cell membrane transport due to overexpression of transporter proteins that act as efflux pumps, such as P-...
Malaria,caused by protozoan parasites of the genus Plasmodium,is a devastating infectious disease in developing countries.One of the biggest problems that have hindered the control of malaria is the emergence and spread of drug resistant Plasmodium strains, particularly Plasmodium falciparum. In order to overcome this problem,new therapeutic agents based on new mechanisms of action or with new structures are ur...