Development and characterization of liposomal formulations containing sesquiterpene lactones for the treatment of chronic gout.

Gout and hyperuricemia are characterized by high uric acid levels, and their treatment involves medications that have adverse effects. In this study, we evaluated oral liposomal formulations with eremantholide C and goyazensolide as a novel approach to reduce the toxicity associated with these substances while maintaining their anti-hyperuricemic activity. We characterized the formulations and evaluated them based on encapsulation efficiency and stability over 12 months and under simulated physiological environments.

Chemical Analysis of Ethanolic Extract and Its Effects on Hyperuricaemia.

In vivo assays and chemical analyses were performed on the ethanolic extract from leaves of . UHPLC-ESI-QTOF analysis confirmed the presence of glucosinolates and flavonol glucosides. The major flavonoid of the ethanolic extract, kaempferol-3,4'-di--β-glucoside, was isolated, a HPLC-DAD method developed and validated to quantify its content in the extract.

Metabolic Profile Changes in Mangalarga Marchador Horses Subjected to A Hypercaloric Diet Evaluated by Proton NMR Spectroscopy.

The incidence of equine metabolic syndrome, a condition that results in endocrinopathic laminitis, is increasing worldwide. Although it is well known that the development of this syndrome depends on imbalances in energy metabolism and genetic traits, its pathophysiology remains unclear. Hydrogen nuclear magnetic resonance (H NMR) is a powerful tool used to compare metabolic profiles and to discriminate metabolites in living beings.

A Comprehensive View on (-)-7-Oxo-ent-kaur-16-en-19-oic Acid, the Major Constituent of Xylopia sericea Leaves Extract: Complete NMR Assignments, X-Ray Crystallographic Structure, in Vitro Antimalarial Activity and Cytotoxicity.

Bioguided fractionation of Xylopia sericea antiplasmodial dichloromethane leaves extract led to the isolation of (-)-7-oxo-ent-kaur-16-en-19-oic acid (C H O ) that was identified by a combination of 1D and 2D NMR experiments (COSY, HMBC, HSQC, HSQC-TOCSY, HSQC-NOESY and NOESY) and by X-ray crystallography. A feature to be pointed out is its (4R) configuration that was inferred from the NOE experiments (HSQC-NOESY and NOESY) and X-ray crystallography. In vitro evaluation of this rare diterpene acid against the chloroquine-resistant strain Plasmodium falciparum W2 by the PfLDH method showed it disclosed a low antiplasmodial activity and was not cytotoxic to HepG2 cells (CC 862.

Potential anti-herpes and cytotoxic action of novel semisynthetic digitoxigenin-derivatives.

In 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.

Esterification of trans-aconitic acid improves its anti-inflammatory activity in LPS-induced acute arthritis.

trans-Aconitic acid (TAA) is an abundant constituent in the leaves of Echinodorus grandiflorus, a medicinal plant used to treat rheumatoid arthritis in Brazil. Esterification was explored as a strategy to increase lipophilicity and biopharmaceutical properties of TAA, a highly polar tricarboxylic acid. We herein report the synthesis of TAA esters via Fischer esterification with ethanol, n-butanol and n-octanol.

Development of a bone-targeted pH-sensitive liposomal formulation containing doxorubicin: physicochemical characterization, cytotoxicity, and biodistribution evaluation in a mouse model of bone metastasis.

Background: Despite recent advances in cancer therapy, the treatment of bone tumors remains a major challenge. A possible underlying hypothesis, limitation, and unmet need may be the inability of therapeutics to penetrate into dense bone mineral, which can lead to poor efficacy and high toxicity, due to drug uptake in healthy organs. The development of nanostructured formulations with high affinity for bone could be an interesting approach to overcome these challenges.

Nematicidal activity of Annona crassiflora leaf extract on Caenorhabditis elegans.

Background: The aim of this work was to investigate the potential nematicidal activity of Annona crassiflora leaf extract against Caenorhabditis elegans.

Methods: The hydroalcoholic leaf extract and its fractions (dichloromethane, ethyl acetate, methanol and water) were submitted to mobility assay against the roundworm Caenorhabditis elegans. GC-MS and NMR analysis were performed in order to identify metabolites.

The first report on flavonoid isolation from Annona crassiflora Mart.

Annona crassiflora, a native tree from Brazilian Cerrado, is reported to possess several ethnomedical uses. Here, we report the isolation and unambiguous characterisation of the flavonoids quercetin-3-O-β-D-glucopyranosil(1 → 6)-O-α-L-arabinoside (1), known as peltatoside, kaempferol-3-O-β-D-galactopyranoside (2), quercetin-3-O-β-D-galactopyranoside (3), quercetin-3-O-β-L-arabinopiranoside (4) and the ( - )-epicatechin (5) from the hydroalcoholic portion of the leaf ethanolic extract. Their structures were elucidated by using 1D and 2D NMR, ESI-MS, UV/Vis spectroscopy, optical rotation analysis and literature data comparison.

Strychnos pseudoquina and Its Purified Compounds Present an Effective In Vitro Antileishmanial Activity.

The development of new and cost-effective alternative therapeutic strategies to treat leishmaniasis has become a high priority. In the present study, the antileishmanial activity of Strychnos pseudoquina St. Hil.

Bioguided isolation of myricetin-3-O-β-galactopyranoside with antinociceptive activity from the aerial part of Davilla elliptica St.-Hil.

Ethnopharmacological Relevance: Davilla elliptica St.-Hil. (Dilleniaceae) is a medicinal plant traditionally used in Brazil to treat inflammatory processes, to relieve pain, as diuretic, gastro- and hepatoprotective agents.

Biotransformation of 21-O-acetyl-deoxycorticosterone by cell suspension cultures of Digitalis lanata (strain W.1.4).

Cell cultures of Digitalis species are known to accept exogenous substrates for biotransformation reactions. We here report the biotransformation of 21-O-acetyl-deoxycorticosterone (1) by cell suspension cultures of Digitalis lanata strain W.1.

Chemical composition and vasodilatation induced by Cuphea carthagenensis preparations.

The aerial parts of Cuphea carthagenensis (Jacq.) J.F.

Pharmacological basis for use of Lychnophora trichocarpha in gouty arthritis: anti-hyperuricemic and anti-inflammatory effects of its extract, fraction and constituents.

Ethnopharmacological Relevance: The ethanolic extract of Lychnophora trichocarpha Spreng. is used in Brazilian folk medicine to treat bruise, pain and inflammatory diseases.

Aim Of The Study: The present study aimed at investigating whether ethanolic extract of L.

Antimicrobial, antiviral and cytotoxic activity of extracts and constituents from Polygonum spectabile Mart.

Polygonum spectabile is used in Brazil for treatment of several infection diseases. Extracts and constituents isolated from this species were evaluated for cytotoxicity and effects on 15 bacterias and yeasts as well on 4 viruses strains (HHV-1, VACV-WR, EMCV, DEN-2). Less polar extracts were effective against Staphylococcus aureus, Bacillus subtillis, Micrococcus luteus, M.

Dihydroisocoumarin from Xyris pterygoblephara active against dermatophyte fungi.

The ethanol extract from Xyris pteygoblephara aerial parts was evaluated against five microorganism strains, by the microdilution and agar diffusion methods. Extract fractionation led to the isolation of three compounds, whose structures were assigned by spectrometric data (1D and 2D NMR, IR, MS and UV) as (3R,4R)-(-)-6-methoxy-3,4-dihydro-3-n-pentil-4-acethoxy-1H-2-benzopyran-1-one (1), moronic acid and quercetin. The absolute configuration of 1 was defined by circular dichroism spectroscopy and comparison with data reported for other dihydroisocoumarins.

Antifungal constituents of Clytostoma ramentaceum and Mansoa hirsuta.

Ethanol extracts of Clytostoma ramentaceum Bur. & K. Schum and Mansoa hirsuta DC.

NMR characterization of new 10-membered-ring macrolactones and dihydrobenzophenazine-5-one, oxidized derivatives of benzo[a]phenazines.

Peroxidation of the phenazine of beta-lapachone using m-ClC6H4CO3H-CH2Cl2 furnished a macrolactone with a rigid 10-membered ring, and the corresponding N-oxide, along with a dihydrobenzophenazine-5-one. All of the new compounds were fully characterized by spectroscopic methods, with the unambiguous assignment of the hydrogens and carbon NMR signals for the N-oxide, with the aid of 2-D NMR, mainly COSY, HMQC, HSQC and HMBC. For the other two compounds some signals could not be assigned owing to their own intrinsic features.

Antimicrobial activity and constituents of Coccoloba acrostichoides.

The ethanol extract and fractions from Coccoloba acrostichoides aerial parts were assayed for in vitro antimicrobial activity. The extract was active against the assayed bacteria while most of the fractions also inhibited fungal growth, especially the n-hexane and EtOAc fractions. The isolated beta-sitosterol and betulin were tested, being the last one active against Fusarium oxysporum.

Diterpenes from Alomia myriadenia (Asteraceae) with cytotoxic and trypanocidal activity.

Further investigation of the aerial parts of Alomia myriadenia revealed an halimane diterpene identified as ent-8S,12S-epoxy-7R,16-dihydroxyhalima-5(10),13-dien-15,16-olide along with the known ent-16-hydroxylabda-7,13-dien-15,16-olide, ent-12R-hydroxylabda-7,13-dien-15,16-olide, 6,7-methylenedioxycoumarin (ayapin), and kaempferol-7-methylether (rhamnocitrin). Evaluated in a panel of human cancer cell lines, the 16-hydroxylabade diterpene was the most active, showing an ED(50) value of 0.3 mug/ml against Lu1 (human lung cancer) cells.

In vitro evaluation of the activity of aromatic nitrocompounds against Trypanosoma cruzi.

Fourteen compounds were evaluated for their activity against Trypanosoma cruzi blood stream forms at the concentration of 500 g/ml. Six compounds were active and re-tested at lower concentrations.