Abstract
Based on ethnobotanical studies, the Aspidosperma excelsum was selected due to its highest claim of popular use for malaria and febrile diseases treatments. This species is rich in secondary metabolites as alkaloids and therefore, the aim of this study was to evaluate the pharmacokinetic, toxicological and biological activity of alkaloids isolated from Aspidosperma excelsum by in silico studies. All substances already isolated from this species were submitted to predictive studies of biological, toxicological and pharmacokinetic activities. Predictive studies of biological activities did not attribute the antimalarial activity to pure substances. However, other activities were found, such as: action on central nervous system and antineoplastic activity. In pharmacokinetic terms, many substances showed an inhibitory action on cytochrome P450 (CYP) and many adverse reactions, highlighting actions on the CNS. Also, several alkaloids, being nitrogenous substances, presented mutagenic or genotoxic activities. Thus, it is demonstrated the species potential for biological activities not yet studied, as well as the importance of investigating its pharmacokinetic and toxicological properties, justifying the accomplishment of the present study.
Highlights
The use of plants for medicinal purposes - treatment, cure and prevention of diseases is one of the oldest forms of human medicinal practice (Veiga-Jr & Pinto, 2005)
When we chemically evaluate the cimetidine, which inhibits several cytochrome P450 (CYP)-450 enzymes, we realize it has 4 hydrogen acceptor groups, which are capable of making hydrogen bonds with protonated enzyme residues, it has 3 donor groups of hydrogen
The species belonging to the genus Aspidosperma have been widely submitted to assays for evaluating their antimalarial activity in vitro (Dolabela, et al, 2015; Chierito, et al, 2014; Meneguetti, et al, 2014; Paula, et al, 2014; Coutinho, et al, 2013; Dolabela, et al, 2012; Andrade-Neto, et al, 2007) and in vivo (Chierito, et al, 2014; Coutinho, et al, 2013; Silva, et al, 2012)
Summary
The use of plants for medicinal purposes - treatment, cure and prevention of diseases is one of the oldest forms of human medicinal practice (Veiga-Jr & Pinto, 2005). The use of plants, for medicinal purposes in Brazil, started with the indigenous people, who had knowledge about Brazilian flora. The shamans were responsible for improving their use and passing on knowledge to new generations (Martins, et al, 2000; Sousa, 1971). The use of medicinal plants to treat diseases in Brazil is ingrained to European, African and native cultures, resulting in a multicultural production, which for a long time was the main form of cure used by the rural population. The use of medicinal plants to treat diseases in Brazil is ingrained to European, African and native cultures, resulting in a multicultural production, which for a long time was the main form of cure used by the rural population. (Coelho, 1989)
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