Current Approaches to Discover Marine Antileishmanial Natural Products

Tempone, André G.; Oliveira, Camila Martins de; Berlinck, Roberto G. S.

doi:10.1055/s-0030-1250663

Cited by 98 publications

(74 citation statements)

References 97 publications

(152 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…In addition to the more "genomic" types of publications, the potential for secondary metabolites to provide new treatments for parasitic diseases have also been discussed. An example would be the 2011 paper 96 discussing the potential of marine-sourced antileishmanial compounds, and work reported from Finland where novel agents against both leishmania and Chagas disease have been derived from simple diterpenes that are known from plant and marine sources, the abietane amides with "compound 10" (33) in the paper by Pittimaa et al, 97 giving the best bioactivities against these two parasites.…”

Section: Potential Areas For Future Consideration From a Biodiversitymentioning

confidence: 99%

The Influence of Brazilian Biodiversity on Searching for Human Use Pharmaceuticals

Newman¹

2016

J. Braz. Chem. Soc.

View full text Add to dashboard Cite

This relatively short review will cover the history of some potential drug entities whose beginnings were from Brazilian flora and fauna that led to scientific findings many years later that could not even have been thought of at the time of their initial discovery. The first two are the discoveries of the effects of peptidic toxins from the highly poisonous snake Bothrops jararaca upon the control of bradykinins that led to the angiotensin converting enzyme inhibitors, and the identification of pederin from the blister beetle Paederus species that 50 plus years later led to brand new discoveries as the source of many marine sponge metabolites. All occurred well before the Convention on Biological Diversity (CBD), in 1992. Then come discussions on lapachol and its congeners and then the potential for the investigation of microbes that are associated with insects, plants and marine invertebrates and their control of the syntheses of novel metabolites with pharmaceutical potential. The review finishes with comments on the biodiversity programs that São Paulo State has put in place and how they are materially aiding in investigations of Brazilian flora and fauna but under conditions that are CBD-compliant.

show abstract

Section: Potential Areas For Future Consideration From a Biodiversitymentioning

confidence: 99%

The Influence of Brazilian Biodiversity on Searching for Human Use Pharmaceuticals

Newman¹

2016

J. Braz. Chem. Soc.

View full text Add to dashboard Cite

show abstract

“…The leishmaniasis treatment includes pentavalent antimonials (Pentostam® and Glucantime®), the polyene antibiotic amphotericin B (including the lipid preparation Ambisome®) and pentamidine. However, such drugs are costly, show undesirable side effects and resistant strains have emerged (Croft and Olliaro 2011;Tempone et al 2011) which reinforces the need for novel therapeutic agents.…”

Section: Introductionmentioning

confidence: 99%

Oleanonic acid from Lippia lupulina (Verbenaceae) shows strong in vitro antileishmanial and antitrypanosomal activity

et al. 2016

View full text Add to dashboard Cite

Leishmaniasis and Chagas disease affect millions of people in tropical and subtropical regions. Drugs used currently to treat such diseases often present undesirable side effects and low efficiency. The aim of this work was to identify extracts and isolated compounds from the genus Lippia with leishmanicidal and trypanocidal activity. , respectively). The triterpenoid oleanonic acid showed the strongest activity against these protozoans (IC 50 of 18.5 and 29.9 µM, respectively). Our results indicate that Lippia plants and their derivatives deserve further investigation in the search for new antiprotozoal drugs, particularly for the treatment of leishmaniasis and Chagas disease. KEYWORDS: Leishmanicidal, trypanocidal, triterpenoids, flavonoids, T. cruzi Ácido oleanônico isolado de Lippia lupulina (Verbenaceae) apresenta potentes atividades leishmanicida e tripanocida Leishmaniose e doença de Chagas afetam milhões de pessoas em regiões tropicais e subtropicais. As drogas atualmente usadas para tratar estas doenças frequentemente apresentam efeitos colaterais indesejáveis e baixa eficiência. Este trabalho teve como objetivo encontrar extratos, frações e compostos isolados de espécies do gênero Lippia com atividades leishmanicida e tripanocida. Quinze extratos de diferentes partes de plantas do gênero Lippia, com composições químicas parcialmente conhecidas, quatro frações de partição, seis substâncias e uma mistura de quatro flavanonas interconversíveis isolados de Lippia salviaefolia e Lippia lupulina foram testados, in vitro, frente a formas epimastigotas de Trypanosoma cruzi e promastigotas de Leishmania amazonensis. O extrato etanólico das raízes de L. lupulina apresentou atividade potente contra T. cruzi e L. amazonensis (IC 50 de 20,0 e 54,5 µg mL -1 , respectivamente), enquanto que o ácido oleanônico mostrou as atividades mais fortes contra estes protozoários, com IC 50 de 18,5 e 29,9 µM, respectivamente. Estes resultados indicam que espécies do gênero Lippia e seus derivados merecem investigações adicionais na busca por novas terapias antiprotozoárias, especialmente para o tratamento de leishmaniose e doença de Chagas.

show abstract

“…Current chemotherapeutic agents for the treatment of all clinical manifestations of leishmaniasis are pentavalent antimonials compounds (e.g., sodium stibogluconate and meglumine antimoniate) and amphotericin B, which unfortunately are considerably toxic (Croft and Olliaro 2011, Tempone et al 2011, Singh and Sundar 2012. Furthermore, these drugs exhibit several limitations, including high cost and the need for daily parenteral administration (Singh and Sundar 2012).…”

Section: Introductionmentioning

confidence: 99%

Antileishmanial activity of some Brazilian plants, with particular reference to Casearia sylvestris

Antinarelli

Pinto

Scio

et al. 2015

An. Acad. Bras. Ciênc.

View full text Add to dashboard Cite

Leishmaniasis is a complex of diseases caused by Leishmania protozoa which treatment is restricted to a limited number of drugs that exhibit high toxicity, collateral effects and are often costly. There are a variety of tropical plants distributed in Brazil, and for many poor people the therapy for several diseases is based mainly on the use of traditional herbal remedies. In this work, the cytotoxic activity of 17 plant methanol extracts was evaluated on several Leishmania species and murine macrophages. Among them, the extract of Casearia sylvestris, Piptocarpha macropoda, Trembleya parviflora, Samanea tubulosa and Plectranthus neochilus showed a promissing leishmanicidal activity, exhibiting IC 50 values below of 20 µg/mL against at least one species of Leishmania. Casearia sylvestris showed the most expressive activity against all promastigote forms of Leishmania species (IC 50 values of 5.4 µg/mL, 5.0 µg/mL, 8.5 µg/mL and 7.7 µg/ mL for L. amazonensis, L. braziliensis, L. chagasi and L. major, respectively), being more effective than the reference drug miltefosine. In spite of the cytotoxic effect on macrophages (CC 50 value of 5.2 µg/mL), C. sylvestris exhibited a strong inhibition against intracellular amastigotes of L. braziliensis (IC 50 value of 1.3 µg/ mL). Further studies, including bio-guided fractionation will be conducted to identify the active compounds.

show abstract

Current Approaches to Discover Marine Antileishmanial Natural Products

Cited by 98 publications

References 97 publications

The Influence of Brazilian Biodiversity on Searching for Human Use Pharmaceuticals

The Influence of Brazilian Biodiversity on Searching for Human Use Pharmaceuticals

Oleanonic acid from Lippia lupulina (Verbenaceae) shows strong in vitro antileishmanial and antitrypanosomal activity

Antileishmanial activity of some Brazilian plants, with particular reference to Casearia sylvestris

Contact Info

Product

Resources

About