ABSTRACT
Background: Plants are an important option in the treatment of malaria, especially in endemic regions, and are a less expensive and more accessible alternative with a lower risk of toxicity. Colombia has a great diversity of plants, and evaluation of natural extracts could result in the discovery of new compounds for the development of antimalarial drugs. The purpose of this work was to evaluate the in vitro antiplasmodial activity and the cytotoxicity of plant extracts from the Colombian North Coast against Plasmodium falciparum. Materials and Methods: The antiplasmodial activity of 12 plant species from the Colombian North Coast that are used in traditional medicine was evaluated through in vitro cultures of P. falciparum, and the cytotoxicity of extracts of these species to human cells was determined. Plant extracts with high antiplasmodial activity were subjected to preliminary phytochemical screening. Results: Extracts from five plants had promising antiplasmodial activity. Specifically, Bursera simaruba (Burseraceae) (bark), Guazuma ulmifolia Lam. (Malvaceae) (whole plant), Murraya exotica L. (Rutaceae) (leaves), Hippomane mancinella L. (Euphorbiaceae) (seeds), and Capparis odoratissima Jacq. (Capparaceae) (leaves). Extracts presented 50% inhibitory concentration values between 1 and 9 µg/ml. Compared to no extract, these active plant extracts did not show cytotoxic effects on mononuclear cells or hemolytic activity in healthy human erythrocytes. Conclusions: The results obtained from this in vitro study of antiplasmodial activity suggest that active plant extracts from the Colombian North Coast are promising for future bioassay-guided fractionation to allow the isolation of active compounds and to elucidate their mechanism of action against Plasmodium spp.
ABSTRACT
The use of natural products by communities from the Colombian Caribbean region to treat health issues, together with biodiversity and geographical features, constitute a great scenery to develop new therapies based on ethnopharmacological heritage. Here, we investigated the anti-inflammatory potential of 10 commonly used plants in Colombian folk medicine, evaluating their effect on nitric oxide (NO) production by LPS-stimulated RAW 264.7 macrophages. The most active plant was evaluated in vivo using 12-O-tetradecanoyl-phorbol-13-acetate (TPA)-induced mouse ear edema, along with its effect on the production of pro-inflammatory mediators in vitro. The extract of Physalis angulata L. calyces showed the highest activity. This extract was fractionated and its dichloromethane fraction (DF) was the most active in vitro, inhibiting the production of NO, prostaglandin E2 (PGE2), interleukin (IL)-1ß, IL-6, tumor necrosis factor (TNF)-α and monocyte chemotactic protein (MCP)-1 (CCL2). In vivo, DF showed a significant inhibition of ear edema and myeloperoxidase (MPO) activity, with evident reduction of the leukocyte infiltration into tissue. Our results support the ethnopharmacological use of the selected plants in folk medicine. P. angulata dichloromethane fraction represents a promising source of pharmacological compounds with great potential therapeutic use to treat inflammatory illness.
ABSTRACT
El exoesqueleto de camarón desechado por la industria puede ser aprovechado para la obtención de quitina y quitosano con la utilización de reactivos comerciales de muy bajo costo. El quitosano es un biopolímero que tiene diversos usos, entre ellos, la remoción de metales pesados a partir de aguas residuales. En este estudio se utilizó quitosano para la remoción de cromo hexavalente a partir de muestras de aguas residuales del proceso de galvanizado (cromado) de una industria de Cartagena. La remoción de cromo se realizó por un proceso discontinuo, a un pH óptimo encontrado en este estudio de 2.0 y una temperatura de 26 °C. La cinética de adsorción fue estudiada mediante el uso de la isoterma de Langmuir, siendo la capacidad máxima de adsorción (Qmax) de 200 mg/g. La remoción de cromo hexavalente a partir de las muestras de aguas residuales fue del 99.98 %.
The exoskeleton of shrimp discarded by the industry, can be used for the production of chitin and chitosan with the use of very low cost commercial reagents. Chitosan is a biopolymer that has many uses, including heavy metals removal from wastewater. In this study, chitosan was used to remove hexavalent chromium from wastewater samples from the galvanizing process (chrome) of an industry in the city of Cartagena. The chromium removal was performed by a batch process at an optimum pH found in this study of 2.0 and a temperature of 26 °C. The adsorption kinetics was studied by using the Langmuir isotherm, being the maximum adsorption capacity (Qmax.) of 200 mg/g. The removal of hexavalent chromium from wastewater samples was 99.98 %.
O exoesqueleto de camarão desperdiçado pela indústria pode ser aproveitado para a obtenção de quitina e quitosana usando reagentes comerciais de baixo custo. A quitosana é um biopolimero que tem diversos usos como a remoção de metais pesados de aguas residuais. Neste estudo se usou quitosana para a remoção de cromo hexavalente de amostras de aguas residuais do processo de galvanizado (cromado) de uma indústria da cidade de Cartagena (Colômbia). A remoção do cromo se realizou através de um processo continuo em um pH de 2.0 como condição ótima encontrada durante a realização deste estudo e uma temperatura de 26 °C. A cinética de adsorção foi estudada através do uso da isoterma de Langmuir, sendo a capacidade máxima de adsorção (Qmax) de 200 mg/g. A remoção de cromo hexavalente a partir das amostras residuais foi de 99.98 %.
ABSTRACT
Cytotoxicity-based, bioassay-guided fractionation of the chloroform-soluble extracts of both the roots and leaves of Picramnia latifolia led to the isolation of two new anthrone C-glycosides, picramniosides G (1) and H (2), two new oxanthrone C-glycosides, mayosides D (3) and E (4), and a new benzanthrone natural product, 6,8-dihydroxy-10-methyl-7H-benz[de]anthracen-7-one (5), together with 10 known compounds, 6,8-dihydroxy-4-methyl-7H-benz[de]anthracen-7-one (6), nataloe-emodin (7), chrysophanein, chrysophanol, 1,5-dihydroxy-7-methoxy-3-methylanthraquinone, pulmatin, 7-hydroxycoumarin, 7-hydroxy-6-methoxycoumarin, beta-sitosterol, and beta-sitosterol glucoside. The structures of 1-5 were established by spectroscopic methods, including 1D and 2D NMR, HRMS, and CD data interpretation. The cytotoxic activity of all isolates was evaluated in a small panel of human cancer cell lines. Compound 7 exhibited significant in vitro cytotoxic activity in the tested cell lines, but no significant activity was observed with an in vivo hollow fiber model at doses of 6.25, 12.5, 25, and 50 mg/kg/injection.
Subject(s)
Anthracenes/isolation & purification , Antineoplastic Agents, Phytogenic/isolation & purification , Glycosides/isolation & purification , Plants, Medicinal/chemistry , Anthracenes/chemistry , Anthracenes/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/pharmacology , Drug Screening Assays, Antitumor , Glycosides/chemistry , Glycosides/pharmacology , Humans , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Peru , Plant Leaves/chemistry , Stereoisomerism , Tumor Cells, CulturedABSTRACT
Bioassay-guided fractionation of the chloroform-soluble extract of the leaves of Vitex negundo led to the isolation of the known flavone vitexicarpin (1), which exhibited broad cytotoxicity in a human cancer cell line panel. In an attempt to increase the cytotoxic potency of 1, a series of acylation reactions was performed on this compound to obtain its methylated (2), acetylated (3), and six new acylated (4-9) derivatives. Compound 9, the previously unreported 5,3'-dihexanoyloxy-3,6,7,4'-tetramethoxyflavone, showed comparative cytotoxic potency to compound 1 and was selected for further evaluation. However, this compound was found to be inactive when evaluated in the in vivo hollow fiber assay with Lu1, KB, and LNCaP cells at the highest dose (40 mg/kg/body weight) tested, and in the in vivo P-388 leukemia model (135 mg/kg), using the ip administration route.