Abstract
BackgroundPanama has an extensive mangrove area and it is one of the countries with the highest biodiversity in America. Mangroves are widely used in traditional medicine, nevertheless, there are very few studies that validates their medicinal properties in America. Given the urgent need for therapeutic options to treat several diseases of public health importance, mangrove ecosystem could be an interesting source of new bioactive molecules. This study was designed to evaluate the potential of Pelliciera rhizophorae as a source of bioactive compounds.ResultsThe present investigation was undertaken to explore the possible antiparasitic potential and α-glucosidase inhibition by compounds derived from the Panamanian mangrove Pelliciera rhizophorae. Bioassay-guided fractionation of the crude extract led to the isolation of ten chemical compounds: α-amyrine (1), β-amyrine (2), ursolic acid (3), oleanolic acid (4), betulinic acid (5), brugierol (6) iso-brugierol (7), kaempferol (8), quercetin (9), and quercetrin (10). The structures of these compounds were established by spectroscopic analyses including APCI-HR-MS and NMR. Compounds 4 (IC50 = 5.3 µM), 8 (IC50 = 22.9 µM) and 10 (IC50 = 3.4 µM) showed selective antiparasitic activity against Leishmania donovani, while compounds 1 (IC50 = 19.0 µM) and 5 (IC50 = 18.0 µM) exhibited selectivity against Tripanosoma cruzi and Plasmodium falciparum, respectively. Moreover, compounds 1–5 inhibited α-glucosidase enzyme in a concentration-dependent manner with IC50 values of 1.45, 0.02, 1.08, 0.98 and 2.37 µM, respectively. Their inhibitory activity was higher than that of antidiabetic drug acarbose (IC50 217.7 µM), used as a positive control. Kinetic analysis established that the five compounds acted as competitive inhibitors. Docking analysis predicted that all triterpenes bind at the same site that acarbose in the human intestinal α-glucosidase (PDB: 3TOP).ConclusionsThree groups of compounds were isolated in this study (triterpenes, flavonols and dithiolanes). Triterpenes and flavones showed activity in at least one bioassay (antiparasitic or α-glucosidase). In addition, only the pentacyclic triterpenes exhibited a competitive type of inhibition against α-glucosidase.
Highlights
Panama has an extensive mangrove area and it is one of the countries with the highest biodiversity in America
All fractions were submitted for bioactivity testing, resulting in fractions IX (70 % growth inhibition (GI) against T. cruzi), FXIII (83 % GI against L. donovani and 69 % GI against P. falciparum), FXXVIII (80 % GI against L. donovani, 73 % GI against P. falciparum and 67 % GI against T. cruzi), and FXXXIII (75 % GI against L. donovani) having antiparasitic properties and fractions IX (86 %), FXIII (93 %), and FXXXIII (84 %) showed inhibition of α-glucosidase activity at a concentrations of 10 μg/mL for parasites and 6.25 μg/mL for α-glucosidase
In summary, ten compounds were isolated from the endemic mangrove P. rhizophorae
Summary
High levels of poverty results in malnutrition, overcrowding, bad sanitation and polluted water These conditions lead to a fertile environment for parasitic diseases and diabetes. According to World Health Organization (WHO) forecasts, DM will be the 7th leading cause of death in 2030, and its prevalence has shown to be higher in low and middle-income countries. This disease is known for allowing high sugar levels in human blood, either because insulin production is inadequate or because the body’s cells do not respond properly to insulin, or both. There is an urgent need to search for novel drugs from several sources, including natural products, to fight global health problems posed by parasitic infections and DM
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