Publications by authors named "Gabriela S Ramos"
In vitro and in vivo antileishmanial activity of β-acetyl-digitoxin, a cardenolide of Digitalis lanata potentially useful to treat visceral leishmaniasis.
Parasite
April 2021
Article Synopsis
- - Current treatments for visceral leishmaniasis have issues like side effects, high costs, and emerging drug resistance, creating a need for new low-cost antileishmanial agents.
- - The study identifies β-acetyl-digitoxin (b-AD), a compound from Digitalis lanata, showing strong antileishmanial activity both in vitro and in vivo, effectively reducing parasite load in infected mice and enhancing anti-parasite immune responses.
- - b-AD delivered in polymeric micelles (b-AD/Mic) showed higher efficacy than other treatments, including the standard drug miltefosine, with low toxicity observed, suggesting it could be a promising option for treating visceral leishmaniasis.
Digitoxigenin presents an effective and selective antileishmanial action against Leishmania infantum and is a potential therapeutic agent for visceral leishmaniasis.
Parasitol Res
January 2021
Article Synopsis
- Treatment for visceral leishmaniasis (VL) faces challenges such as drug toxicity, high costs, and parasite resistance, prompting interest in drug repositioning, particularly with cardenolides like digitoxigenin (DIGI) from Digitalis lanata.
- The study revealed that DIGI showed significant anti-leishmanial activity with a selectivity index (SI) superior to the standard drug amphotericin B, impacting mitochondrial function and triggering oxidative stress in Leishmania infantum parasites.
- When DIGI was combined with Pluronic® F127-based micelles for treatment in mice, it resulted in greater reductions in parasite load and improved immune responses compared to both miltefosine and DIGI alone, suggesting
Human herpesviruses are among the most prevalent pathogens worldwide and have become an important public health issue. Recurrent infections and the emergence of resistant viral strains reinforce the need of searching new drugs to treat herpes virus infections. Cardiac glycosides are used clinically to treat cardiovascular disturbances, such as congestive heart failure and atrial arrhythmias.
View Article and Find Full Text PDFCardiac glycosides (CGs) are natural compounds traditionally used for the treatment of heart disorders, and recently new therapeutic possibilities were proposed. Their antitumor reports and clinical trials have notably enhanced, including those targeted for lung cancer, the most lethal type that lacks of new treatment agents, instigating the research of these molecules. The CGs studied here, named C10 {3β-[(N-(2-hydroxyethyl)aminoacetyl]amino-3-deoxydigitoxigenin} and C18 (3β-(aminoacetyl)amino-3-deoxydigitoxigenin), are semisynthetic derivatives prepared from digitoxigenin scaffold.
View Article and Find Full Text PDFIn recent years, new therapeutic possibilities were proposed for cardiac glycosides traditionally used to treat heart diseases, such as anticancer and antiviral activities. In this sense, this work aimed to synthesize the readily accessible 3β-azido-3-deoxydigitoxigenin (5) from digitoxigenin (1). Two new series of compounds were obtained from derivative (5): (i) O-glycosyl trizols through click chemistry with propargyl glycosides; and (ii) compounds substituted in the alpha carbonyl position with different residues linked via an amino-group.
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