STUDIES BASED ON NEGLECTED DISEASES - EVALUATION OF TERPENE ACTIVITY AS A POSSIBLE ANTIPARASITARY AGENT: A PHARMACOLOGICAL OVERVIEW
Jose Isaque Do Nascimento Mangueira1, Wesley Natanael da Silva Lacerda1 Helen Raynara Dantas1, Kailane Lourenço Araújo1, Luís Felipe Alves Dionísio1, José Elizandro Batista de Oliveira1, Kaline de Araújo Medeiros1
1 Department of Pharmacy, State University of Paraíba, Campina Grande, PB Email:jose.isaque@aluno.uepb.edu.br
Among neglected diseases, those of parasitic etiology stand out as a threat to the health and well-being of millions of individuals, especially in developing nations. In this context, a promising strategy to address this challenge is the exploration of natural products, which are rich in phytochemical compounds, especially terpenoids, effective substances in the fight against helminths and protozoa. Thus, the aim of this study is to conduct a literature review of research on the antiparasitic activity of terpenoids targeted for the treatment of helminthiases. To this end, a retrospective study of the literature was conducted, using the PubMed, CAPES Periodicals Portal, and Web of Science databases, employing descriptors indexed in DeCS: "Terpene and Antiparasitic," "Terpene and Antiparasitic Agents," and "Terpene and Parasitoses," cross-referenced using the boolean operator "And." The search was restricted to articles published in English from 2018 to 2023, resulting in the identification of 255 articles, of which 26 met the inclusion and exclusion criteria and were therefore selected to be part of the study.Among the phytoconstituents present in natural products, such as extracts and essential oils, triterpenes, sesquiterpenes, monoterpenes, and diterpenes stand out. The most significant compounds among them include thymol, eugenol, carvacrol, 12-hydroxy-11,14-diceto-6,8,12-abietatrien-19,20-olide (HABTO), and 5-epi-icetexone (ICTX). In this regard, in vitro and in vivo studies have shown promising pharmacological activities for these compounds, particularly against the genera Leishmania spp. in amastigote forms (using essential oil rich in monoterpenes extracted from Citrus limon leaves), Trypanosoma cruzi in trypomastigote forms (by using ?-caryophyllene, a sesquiterpene found in essential oil), Plasmodium spp, and in helminths. The anti-helminthic mechanism of action of these compounds involves rapid paralysis of the worms, accompanied by inhibition of egg hatching, thus enhancing the anti-helminthic effect.Therefore, the results of this study demonstrated the relevance of this class of agents. Through in silico screening, the best interaction between protein targets and ligands was analyzed, such as sesquiterpenoids, which are more active against Leishmania spp. and Trypanosoma cruzi, and thymol, which is more effective against Cryptosporidium parvum. Thus, they can be explored as potential promising agents in the creation of therapeutic formulations. To achieve this, it is essential to explore variables such as the compatibility of these agents with pharmaceutical excipients, stability, toxicity, and in vitro and in vivo pharmacological action, with the aim of developing medications that combine efficacy, safety, and quality, making them more advantageous than conventional therapies.
Keywords: Phytopharmaceuticals.Terpenes. Antihelmintics.
Support: CAPES.
Area: Natural Products.
Comissão Organizadora
Francisco Mendonça Junior
Pascal Marchand
Teresinha Gonçalves da Silva
Isabelle Orliac-Garnier
Gerd Bruno da Rocha
Comissão Científica
Ricardo Olimpio de Moura