Hepatodamianol as hepatoprotective constituent of Turnera diffusa.

It is well known that liver diseases are a major health problem and that there is a lack of hepatoprotective agents. Turnera diffusa (damiana) is a plant with a widespread distribution in México, which has many traditional uses, including the treatment of hepatic illnesses. Based on the bioassay-guided fractionation of a methanolic extract obtained from the aerial part of T. diffusa, we purified and identified a compound called hepatodamianol (1). This C-glycoside exhibited a four times greater hepatoprotective effect than the widely used hepatoprotective agent silibinin against carbon tetrachloride damage in an in vitro model using HepG2 cells. Hepatodamianol produced no cytotoxic effects and it exhibited a high antioxidant capacity. Therefore, hepatodamianol is a good candidate compound for testing as a hepatoprotective agent in a preclinical trial.

Turnera diffusa extract attenuates profibrotic, extracellular matrix and mitochondrial markers in activated human hepatic stellate cells (HSC).

INTRODUCTION AND OBJECTIVES: Hepatic fibrosis is characterized by the accumulation of extracellular matrix which includes the accumulation of α-smooth muscle actin (α-SMA), collagen type I (COL1α1), as well as remodeling induced by metalloproteinases and tissue inhibitor of metalloproteinase (TIMPs), where hepatic stellate cells (HSCs) play a central role. In addition, the transcription factor SNAI1 (which participates in epithelial-mesenchymal transition, EMT) and mitofusin 2 (MFN2, a mitochondrial marker) plays an important role in chronic liver disease. Turnera diffusa (TD), a Mexican endemic plant, has been shown to possess antioxidant and hepatoprotective activity in vitro. We treated human HSC (LX2 cells) with a methanolic extract of Turnera diffusa (METD) to evaluate the mechanism involved in its hepatoprotective effect measured as fibrosis modulation, EMT, and mitochondrial markers. MATERIALS AND METHODS: HSC LX-2 cells were treated with METD (100 and 200ng/mL) alone or combined with TGF-ß (10ng/mL) at different time points (24, 48, and 72h). α-SMA, COL1α1, MMP2, TIMP1, SNAI1, and MFN2 mRNAs and protein levels were determined by real-time quantitative PCR and Western Blot analysis. RESULTS: We found that METD decreases COL1α1-mRNA, α-SMA, and TIMP1 protein expression in LX2 cells treated with and TGF-ß. This treatment also decreases MFN2 and TIMP1 protein expression and induces overexpression of MMP2-mRNA. CONCLUSIONS: Our results suggest that a methanolic extract of Turnera diffusa is associated with an antifibrotic effect by decreasing profibrotic and mitochondrial markers together with the possible induction of apoptosis through SNAI1 expression in activated HSC cells.

Acute Hypoglycemic and Antidiabetic Effect of Teuhetenone A Isolated from Turnera diffusa.

Diabetes mellitus is a chronic degenerative disease that causes long-term complications and represents a serious public health problem. Turnera diffusa (damiana) is a shrub that grows throughout Mexico and is traditionally used for many illnesses including diabetes. Although a large number of plant metabolites are known, there are no reports indicating which of these are responsible for this activity, and this identification was the objective of the present work. Through bioassay-guided fractionation of a methanolic extract obtained from the aerial part of T. diffusa, teuhetenone A was isolated and identified as the main metabolite responsible for the plant's hypoglycemic activity. Alpha-glucosidase inhibitory activity and cytotoxicity of this metabolite were determined. Hypoglycemic and antidiabetic activities were evaluated in a murine model of diabetes in vivo, by monitoring glucose levels for six hours and comparing them with levels after administering various controls. Teuhetenone A was not cytotoxic at the tested concentrations, and did not show inhibitory activity in the glucosidase test, and the in vivo assays showed a gradual reduction in glucose levels in normoglycemic and diabetic mice. Considering these results, we suggest that teuhetenone A has potential as an antidiabetic compound, which could be further submitted to preclinical assays.

Actividad antimicrobiana y toxicidad frente a Artemia salina del extracto diclorometánico de raíces de Morinda royoc L / Antimicrobial action and toxicity against Artemia salina of the dichlormethane extract from Morinda royoc L roots

Introducción: las plantas son una fuente de diversidad natural por la gran variedad de compuestos que sintetizan. Particularmente las antraquinonas resultan un importante grupo de metabolitos secundarios con actividad antimicrobiana y antioxidante. Objetivos: evaluar la actividad antimicrobiana del extracto diclorometánico de raíces de Morinda royoc L, así como su toxicidad contra Artemia salina. Métodos: la actividad antimicrobiana se determinó utilizando el método de microdilución en placa de 96 pozos. Se evaluó la actividad del extracto frente a 7 aislados clínicos de Candida spp. y frente a las bacterias Staphylococcus aureus resistente a meticilina, Staphylococcus aureus ATCC 12598, Enterococus faecales, Escherichia coli, Acinetobacter baumanii, Pseudomonas aeruginosa y Klebsiella pneumoniae. La toxicidad del extracto se evaluó mediante el ensayo de letalidad con A salina. Resultados: el extracto crudo fue activo frente a todas las especies de Candida evaluadas. La concentración mínima inhibitoria más baja fue 1,95 µg/mL. El extracto mostró fuerte actividad inhibitoria contra S. aureus, E faecales, y E coli. El valor más bajo de concentración mínima inhibitoria obtenido fue 31,25 µg/mL. El extracto presentó una toxicidad moderada hacia A salina. Conclusiones: los resultados obtenidos demuestran el potencial del extracto diclorometánico de raíces de M. royoc L en el tratamiento de infecciones causadas por bacterias y hongos

Introduction: plants are a source of natural diversity because of the great variety of compounds that they synthesize. Anthraquinones in particular are an important group of secondary metabolites characterized by their antimicrobial and antioxidant action. Objectives: to evaluate the antimicrobial action of dichloromethane extract from Morinda royoc L roots as well as its toxicity against Artemia salina. Methods: the antimicrobial action was determined by using the brooth microdilution in 96-well plate. The extract action against 7 Candida spp clinical isolates and against bacteria such as methicillin-resistant Staphylococcus aureus, Staphylococcus aureus ATCC 12598, Enterococus faecales, Escherichia coli, Acinetobacter baumanii, Pseudomonas aeruginosa and Klebsiella pneumoniae was evaluated. The extract toxicity was measured using brine shrimp (Artemia salina) lethality test. Results: the crude extract proved to be active against all the tested Candida species. The lowest minimal inhibitory concentration was 1,95 µg/mL. The extract showed strong inhibitory action against S aureus, E. faecales, and E coli. The lowest minimal inhibitory concentration was 31.25 µg/mL. The extract presented moderate toxicity against A salina. Conclusions: the results showed the potentialities of dichloromethane extract from M. royoc L. roots for the treatment of bacterial and fungal infections

Actividad antimicrobiana y toxicidad frente a Artemia salina del extracto diclorometánico de raíces de Morinda royoc L / Antimicrobial action and toxicity against Artemia salina of the dichlormethane extract from Morinda royoc L roots

Introducción: las plantas son una fuente de diversidad natural por la gran variedad de compuestos que sintetizan. Particularmente las antraquinonas resultan un importante grupo de metabolitos secundarios con actividad antimicrobiana y antioxidante. Objetivos: evaluar la actividad antimicrobiana del extracto diclorometánico de raíces de Morinda royoc L, así como su toxicidad contra Artemia salina. Métodos: la actividad antimicrobiana se determinó utilizando el método de microdilución en placa de 96 pozos. Se evaluó la actividad del extracto frente a 7 aislados clínicos de Candida spp. y frente a las bacterias Staphylococcus aureus resistente a meticilina, Staphylococcus aureus ATCC 12598, Enterococus faecales, Escherichia coli, Acinetobacter baumanii, Pseudomonas aeruginosa y Klebsiella pneumoniae. La toxicidad del extracto se evaluó mediante el ensayo de letalidad con A salina. Resultados: el extracto crudo fue activo frente a todas las especies de Candida evaluadas. La concentración mínima inhibitoria más baja fue 1,95 µg/mL. El extracto mostró fuerte actividad inhibitoria contra S. aureus, E faecales, y E coli. El valor más bajo de concentración mínima inhibitoria obtenido fue 31,25 µg/mL. El extracto presentó una toxicidad moderada hacia A salina. Conclusiones: los resultados obtenidos demuestran el potencial del extracto diclorometánico de raíces de M. royoc L en el tratamiento de infecciones causadas por bacterias y hongos(AU)

Introduction: plants are a source of natural diversity because of the great variety of compounds that they synthesize. Anthraquinones in particular are an important group of secondary metabolites characterized by their antimicrobial and antioxidant action. Objectives: to evaluate the antimicrobial action of dichloromethane extract from Morinda royoc L roots as well as its toxicity against Artemia salina. Methods: the antimicrobial action was determined by using the brooth microdilution in 96-well plate. The extract action against 7 Candida spp clinical isolates and against bacteria such as methicillin-resistant Staphylococcus aureus, Staphylococcus aureus ATCC 12598, Enterococus faecales, Escherichia coli, Acinetobacter baumanii, Pseudomonas aeruginosa and Klebsiella pneumoniae was evaluated. The extract toxicity was measured using brine shrimp (Artemia salina) lethality test. Results: the crude extract proved to be active against all the tested Candida species. The lowest minimal inhibitory concentration was 1,95 µg/mL. The extract showed strong inhibitory action against S aureus, E. faecales, and E coli. The lowest minimal inhibitory concentration was 31.25 µg/mL. The extract presented moderate toxicity against A salina. Conclusions: the results showed the potentialities of dichloromethane extract from M. royoc L. roots for the treatment of bacterial and fungal infections(AU)

Antimicrobial activity of the dichloromethane extract from in vitro cultured roots of Morinda royoc and its main constituents.

The dichloromethane extract and seven anthraquinones isolated from in vitro cultured roots of Morinda royoc L. were tested for their antimicrobial activity against seven yeast and seven bacterial strains. The extract showed a minimum inhibitory concentration (MIC) value of 15.6 microg/m against all species of Candida tested; except C. glabrata (MIC 1.95 microg/mL), and it inhibited the growth of oxacillin-resistant Staphylococcus aureus (MIC 31.2 microg/mL). Only morindone showed activity against all yeast strains (MIC 1.9 microg/mL), and against oxacillin-resistant Staphylococcus aureus (MIC 15 microg/mL).

Antimicrobial activity of coupled hydroxyanthracenones isolated from plants of the genus Karwinskia.

The in vitro activity of some isolated hydroxyanthracenones belonging to the genus Karwinskia against four bacteria, six filamentous fungi and four yeast are reported. These hydroxyanthracenones were found to possess antimicrobial activity, particularly against Streptococcus pyogenes, Candida albicans, C. boidinii, C. glabrata and Cryptococcus neoformans; minimal inhibitory concentrations range between 16 and 2 microg/ml.