Anti-Acanthamoeba castellanii activity of alkaloid-enriched extracts and lycorine from the Amaryllidaceae species

Abstract Free-living amoebae of the genus Acanthamoeba are the causative agents of granulomatous encephalitis and keratitis, severe human infections. Bioactive compounds from plants are recognized as an alternative source for the development of new drugs. The Amaryllidaceae is a botanical family able to synthesize a very specific and consistent group of biologically active isoquinoline-like alkaloids. The alkaloidal fractions from the Brazilian species Hippeastrum canastrense, H. diniz-cruziae, H. puniceum, and Crinum x amabile, along with the alkaloid lycorine, were investigated against Acanthamoeba castellanii. The in vitro assays were performed with distinct concentrations of lycorine and alkaloidal fractions, while the cell viability was evaluated by the MTT method upon MDCK cells. Chlorhexidine 0.02% was used as the positive control. The effect of alkaloid fractions was concentration dependent, and 2000 µg mL-1 of H. canastrense and H. diniz-cruziae provided a 100% inhibition. At concentrations of 250, 500, and 1000 µg mL-1, the H. diniz-cruziae alkaloidal fraction showed the lowest cytotoxic effect (5%-7%) and remarkable anti-amoebic activity, demonstrating values of IC50 285.61 µg mL-1, low cytotoxicity (5%-7%), and selectivity index (7.0). Taken together, the results are indicative of the great potential that the alkaloids from H. diniz-cruziae have as new candidates for anti-amoebicidal compounds

Chemical evaluation and anticholinesterase activity of Hippeastrum puniceum (Lam. ) Kuntz bulbs (Amaryllidaceae)

Hippeastrum puniceum is a species that belongs to the Amaryllidaceae family. A particular characteristic of this family is the consistent and very specific presence of isoquinoline alkaloids, which have demonstrated a wide range of biological activities such as antioxidant, antiviral, antifungal, antiparasitic, and acetylcholinesterase inhibitory activity, among others. In the present work, fifteen alkaloids were identified from the bulbs of Hippeastrum puniceum (Lam.) Kuntz using a GC-MS approach. The alkaloids 9-O-demethyllycoramine, 9-demethyl-2α-hydroxyhomolycorine, lycorine and tazettine were isolated through chromatographic techniques. The typical Amaryllidaceae alkaloids lycorine and tazettine, along with the crude and ethyl acetate extract from bulbs of the species were evaluated for their inhibitory potential on α-amylase, α-glucosidase, tyrosinase and acetylcholinesterase activity. Although no significant inhibition activity was observed against α-amylase, α-glucosidase and tyrosinase from the tested samples, the crude and ethyl acetate extracts showed remarkable acetylcholinesterase inhibitory activity. The biological activity results that correlated to the alkaloid chemical profile by GC-MS are discussed herein. Therefore, this study contributed to the knowledge of the chemical and biological properties of Hippeastrum puniceum (Lam.) and can subsidize future studies of this species

New lycosinine derivative from Hippeastrum breviflorum

AbstractA new lycosinine derivative, 9-O-demethyllycosinine B, was isolated from the native Brazilian Hippeastrum breviflorumHerb., Amaryllidaceae, along with the well-known alkaloids lycosinine B and lycorine. The structure of the new compound was established by physical and spectroscopic methods. 9-O-demethyllycosinine B is the third lycosinine variant identified in the Amaryllidaceae family.

Caracterización fitoquímica de una fracción de biflavonoides de Garcinia madruno: Su inhibición de la oxidación de LDL humana y su mecanismo de estabilización de especies radicalarias / Phytochemycal characterization of a biflavonoid fraction from Garcinia madruno: Inhibition of human LDL oxidation and its free radical scavenging mechanism

A una fracción biflavonoide (FB) caracterizada fitoquímicamente de Garcinia madruno (Clusiaceae),se le evalúa su potencial inhibitorio de la oxidación de LDL y su capacidad estabilizadora de especies radicalarias, correlacionando dichas actividades con su contenido en biflavonoides. Los biflavonoides morelloflavona, volkensiflavona y amentoflavona se identifican a partir de la FB. El extracto que contiene la FB (extracto AcOEt) se determina como el principal factor involucrado en la actividad estabilizadora de radicales libres de esta especie vegetal, obteniendo la actividad estabilizadora del radical DPPH• a una concentración de 4,50 μg/mL. La peroxidación inducida con CuSO4 de las lipoproteínas de baja densidad, se reduce significativamente en presencia de FB (CE50 = 11,85 μg/mL). El biflavonoide morelloflavona se determina como el principal responsable de la protección ejercida por la FB frente a la actividad estabilizadora de radicales libres y la peroxidación lipídica, aunque posiblemente existan procesos de sinergismo. Estas propiedades sugieren que la FB de G. madruno es un excelente candidato para ser utilizado como antioxidante.