Abstract
Natural marine products have shown an interesting array of diverse and novel chemical structures with potent biological activities. Our study reports the antiproliferative assays of crude extracts, fraction and pure compound (4R,9S,14S)-4α-acetoxy-9β,14α-dihydroxydolast-1(15),7-diene (1) obtained from brown alga Canistrocarpus cervicornis showing the antileishmanial activity. We showed that 1 had a dose-dependent activity during 72 h of treatment, exhibiting IC50 of 2.0 μg/mL, 12.0 μg/mL, and 4.0 μg/mL for promastigote, axenic amastigote and intracellular amastigote forms of Leishmania amazonensis, respectively. A cytotoxicity assay showed that the action of the isolated compound 1 was 93.0 times less toxic to the macrophage than to the protozoan. Additionally, compound 1 induced ultrastructural changes, including extensive mitochondrial damage; decrease in Rh123 fluorescence, suggesting interference with the mitochondrial membrane potential; and lipid peroxidation in parasite cells. The use of 1 from C. cervicornis against L. amazonensis parasites might be of great interest as a future alternative to the development of new antileishmanial drugs.
Highlights
Human leishmaniasis is an endemic parasitic disease which represents a major health problem in the tropical and subtropical regions of the world
Marine brown algae of the family Dictyotaceae are rich sources of monocyclic, bicyclic, and tryciclic diterpenes as major secondary metabolites [18,22,23,24,25,26]. This seaweed has a wide distribution along the Brazilian coast [25]. This traditional medicine still plays an important role in primary health care [27]
Plant-derived drugs remain an important resource, especially in developing countries, in combating diseases [6]. This is true for marine natural products, which show an interesting array of diverse and novel chemical structures with potent biological activities [28]
Summary
Human leishmaniasis is an endemic parasitic disease which represents a major health problem in the tropical and subtropical regions of the world. Pentavalent antimonials have been used for leishmaniasis treatment for more than 50 years They cause serious side effects, such as cardiac and renal toxicity, as well as continuing to require long-term treatment. Other alternative drugs to antimonials in unresponsive cases are: Pentamidine and amphotericin B These drugs cause toxic effects [5,6]. Brown algae produce a range of these compounds that have a wide variety of ecological functions such as defense against herbivores [8], fouling [9,10] and pathogenic microbes [11] They display a wide spectrum of pharmacological properties, such as antiviral [12], antiprotozoa [13,14], antibacterial [15], antioxidant [16] and anticoagulant [17]. In this study the leishmanicidal activity of crude extracts, fraction, and a 4-acetoxy-dolastane diterpene (1) obtained from C. cervicornis were first measured in laboratory assays against the Leishmania amazonensis
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