Abstract
In our continuing work looking for new anti-infective lead compounds from Brazilian biomes, the two known piperidine alkaloids ( - )-cassine and ( - )-spectaline were isolated from the flowers of Senna spectabilis (syn. Cassia spectabilis). Their structures were elucidated using a combination of spectroscopic and spectrometric data analysis. Further, these compounds were acetylated yielding the derivatives ( - )-3-O-acetylcassine and ( - )-3-O-acetylspectaline. All compounds were screened against P. falciparum-infected red blood cells (RBC) in culture, aiming to identify antimalarial prototypes. Among all compounds screened, the first two alkaloids (IC50 1.82 µM and IC50 2.76 µM) were more effective than the derivatives (IC50 24.47 µM and IC50 25.14 µM) in comparison to the standard compound chloroquine (IC50 0.30 µM). These data show that piperidine alkaloids constitute a class of natural products that feature a broad spectrum of biological activities, and are, therefore, important templates for drug design, including antimalarial.
Highlights
Malaria, a life-threatening disease caused by Plasmodium parasites, infects and destroys red blood cells, leading to fever, severe anemia, and cerebral malaria and if untreated may cause death
In our continuing work looking for new anti-infective lead compounds from Brazilian biomes, the two known piperidine alkaloids (–)-cassine and (–)-spectaline were isolated from the flowers of Senna spectabilis
Malaria accounts for ca. 250 million clinical cases and nearly 1 million deaths each year, the great majority of which occur in children younger than 5 years of age and in young, pregnant women, which are more frequently attacked because of the lower immunological protection.[1]
Summary
A life-threatening disease caused by Plasmodium parasites, infects and destroys red blood cells, leading to fever, severe anemia, and cerebral malaria and if untreated may cause death. In our continuing work looking for new anti-infective lead compounds from Brazilian biomes, the two known piperidine alkaloids (–)-cassine and (–)-spectaline were isolated from the flowers of Senna spectabilis
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