Gibbilimbol analogues as antiparasitic agents—Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum

Varela, Marina T.; Dias, Roberto Z.; Martins, Ligia F.; Ferreira, Daiane Dias; Tempone, André G.; Ueno, Anderson K.; Lago, João Henrique G.; Fernandes, João Paulo S.

doi:10.1016/j.bmcl.2016.01.040

Cited by 21 publications

(13 citation statements)

References 20 publications

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“…Promising antiplasmodial activity was reported for extracts from P. capense [268], P. cumanense [170] and P. nigrum [272], with IC 50 values of 2 µg/mL, 7 μg/mL and 12.5 μg/mL, respectively. In contrast, antitrypanosomal and antileishmanial potentialities were prominent in the EO from P. aduncum [45] with IC 50 values of 2.8 μg/mL, 12.1 μg/mL and 9 μg/mL in cell-derived and metacyclic trypomastigotes, as well as intracellular amastigotes, and P. malacophyllum with 17 μg/mL against trypomastigotes [273] of T. cruzi ; while oil from P. demeraranum with IC 50 value of 15 µg/mL [93] and P. hispidum with 4.7 µg/mL value [274] against Leishmania amazonensis .…”

Section: Antiparasitic Activities Of Piper Speciesmentioning

confidence: 99%

Piper Species: A Comprehensive Review on Their Phytochemistry, Biological Activities and Applications

et al. 2019

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Piper species are aromatic plants used as spices in the kitchen, but their secondary metabolites have also shown biological effects on human health. These plants are rich in essential oils, which can be found in their fruits, seeds, leaves, branches, roots and stems. Some Piper species have simple chemical profiles, while others, such as Piper nigrum, Piper betle, and Piper auritum, contain very diverse suites of secondary metabolites. In traditional medicine, Piper species have been used worldwide to treat several diseases such as urological problems, skin, liver and stomach ailments, for wound healing, and as antipyretic and anti-inflammatory agents. In addition, Piper species could be used as natural antioxidants and antimicrobial agents in food preservation. The phytochemicals and essential oils of Piper species have shown strong antioxidant activity, in comparison with synthetic antioxidants, and demonstrated antibacterial and antifungal activities against human pathogens. Moreover, Piper species possess therapeutic and preventive potential against several chronic disorders. Among the functional properties of Piper plants/extracts/active components the antiproliferative, anti-inflammatory, and neuropharmacological activities of the extracts and extract-derived bioactive constituents are thought to be key effects for the protection against chronic conditions, based on preclinical in vitro and in vivo studies, besides clinical studies. Habitats and cultivation of Piper species are also covered in this review. In this current work, available literature of chemical constituents of the essential oils Piper plants, their use in traditional medicine, their applications as a food preservative, their antiparasitic activities and other important biological activities are reviewed.

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Section: Antiparasitic Activities Of Piper Speciesmentioning

confidence: 99%

Piper Species: A Comprehensive Review on Their Phytochemistry, Biological Activities and Applications

et al. 2019

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“…These results encouraged researchers to prepare several quite simple synthetic analogues. Among these, the compound n -octyl-4-hydrozybenzylamine (LINS03003) ( 31 ) was the most potent, with IC 50 values of 5.5 μ M against amastigote forms of T. cruzi , with a higher activity than that of the natural prototype (Figure 11) [70].…”

Section: Introductionmentioning

confidence: 99%

Active Essential Oils and Their Components in Use against Neglected Diseases and Arboviruses

Luna

Scotti

et al. 2019

Oxidative Medicine and Cellular Longevity

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The termneglected diseasesrefers to a group of infections caused by various classes of pathogens, including protozoa, viruses, bacteria, and helminths, most often affecting impoverished populations without adequate sanitation living in close contact with infectious vectors and domestic animals. The fact that these diseases were historically not considered priorities for pharmaceutical companies made the available treatments options obsolete, precarious, outdated, and in some cases nonexistent. The use of plants for medicinal, religious, and cosmetic purposes has a history dating back to the emergence of humanity. One of the principal fractions of chemical substances found in plants are essential oils (EOs). EOs consist of a mixture of volatile and hydrophobic secondary metabolites with marked odors, composed primarily of terpenes and phenylpropanoids. They have great commercial value and were widely used in traditional medicine, by phytotherapy practitioners, and in public health services for the treatment of several conditions, including neglected diseases. In addition to the recognized cytoprotective and antioxidative activities of many of these compounds, larvicidal, insecticidal, and antiparasitic activities have been associated with the induction of oxidative stress in parasites, increasing levels of nitric oxide in the infected host, reducing parasite resistance to reactive oxygen species, and increasing lipid peroxidation, ultimately leading to serious damage to cell membranes. The hydrophobicity of these compounds also allows them to cross the membranes of parasites as well as the blood-brain barrier, collaborating in combat at the second stage of several of these infections. Based on these considerations, the aim of this review was to present an update of the potential of EOs, their fractions, and their chemical constituents, against some neglected diseases, including American and African trypanosomiasis, leishmaniasis, and arboviruses, specially dengue.

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“…Em alguns dos trabalhos avaliados, foram utilizados óleos essenciais provenientes das plantas (ALOUI et al, 2016;ANDRADE et al, 2016;CARVALHO et al, 2017;de MELO et al, 2013;DEZAKI et al, 2016;ESSID et al, 2015;MACHADO et al, 2012;MONZOTE, PASTOR, SCULL;GILLE, 2014;MONZOTE et al, 2014;MUKHERJEE et al, 2016;RODRIGUES et al, 2015;RODRIGUES et al, 2013;VARELA et al, 2016). Os componentes dos óleos essenciais possuem caráter lipofílico e dessa maneira, conseguem atravessar a membrana plasmática, interferindo na composição desta.…”

Section: Discussionunclassified

“…Já em outros trabalhos (DEZAKI et al, 2016;RO-DRIGUES et al, 2013;VARELA et al, 2016), o mecanismo de ação do produto vegetal tem como alvo de ação a membrana plasmática, aumentando a sua permeabilidade ou despolarizando-a, e fazendo com que a célula sofra lise.…”

Section: Discussionunclassified

Leishmaniose E Plantas Medicinais: Uma Revisão

Hellmann¹,

Marchesan²,

Velasquez³

2018

Arq. Ciênc. Saúde Unipar

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A leishmaniose, segundo a Organização Mundial de Saúde, é uma das mais negligenciadas doenças tropicais re-emergentes, sendo reportada em várias partes do globo. Diante das dificuldades encontradas com as drogas disponíveis no mercado atualmente, como a elevada toxicidade e, em alguns casos, resistência por parte do parasito, inúmeras pesquisas tem sido realizadas com o objetivo de encontrar novas alternativas para o tratamento da leishmaniose. Nesse contexto, chama-se a atenção para o foco em compostos oriundos de plantas, as quais podem apresentar moléculas que tragam bons resultados no futuro. O objetivo de presente trabalho foi o de realizar uma revisão bibliográfica sobre produtos naturais utilizados em pesquisas com Leishmania como potenciais agentes utilizados como forma de tratamento contra o referido parasita. Foram analisados artigos científicos publicados nos últimos 5 anos nas bases eletrônicas de dados indexados na base de dados da LILACS, PubMed e ScienceDirect, utilizando os descritores em português “plantas medicinais”, “leishmania” e seus correspondentes em Inglês. Selecionaram-se 61 artigos de estudos científicos, oriundos de 17 países, a maioria realizada no Brasil e Índia. Com base nos mecanismos de ação propostos pelos autores dos trabalhos realizados com amastigotos de Leishmania, grande parte está associada com estresse oxidativo na célula e com alterações no ambiente do macrófago, criando espécies reativas que funcionam como microbicidas. É possível que um composto ativo de uma planta tenha mais de um alvo na célula, sendo capaz de interferir de diferentes maneiras, dependendo do tipo celular e dos alvos disponíveis. As vantagens da utilização da fitoterapia incluem o baixo custo, baixa incidência de efeitos colaterais e sua efetividade. Além disso, é importante que sejam consideradas as espécies vegetais disponíveis no local, visando à diminuição nos custos do fitoterápico.

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Gibbilimbol analogues as antiparasitic agents—Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum

Cited by 21 publications

References 20 publications

Piper Species: A Comprehensive Review on Their Phytochemistry, Biological Activities and Applications

Piper Species: A Comprehensive Review on Their Phytochemistry, Biological Activities and Applications

Active Essential Oils and Their Components in Use against Neglected Diseases and Arboviruses

Leishmaniose E Plantas Medicinais: Uma Revisão

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