Desarrollo de un medicamento herbolario con actividad hepatoprotectora a partir de Turnera diffusa.

Propósito y Método del Estudio: El propósito del presente trabao fue desarrollar un medicamento herbolario con actividad hepatoprotectora a partir ce Turnera dirlusa estandarizado y con criterios de control de calidad. Se reaizaron 10 colectas de T diffusa, se estableció y estandarizó el proceso de obtención/purficecičn del medicamento. Se cuantficó el hepatodamianol los flavoinoides totales los solventes residuales asi como las actividades antioxdantes y hepatcprotectora in vitro. Se identificaron los principales componentes por HPLCMS con el fin de abtener las condiciones minimas que de cumpir el medicamento . Por medio de anáisis quimométrico, se selecciond la colecta que tuviera mayor simlitud con el resto y se realiaó la actividad hepetoprolectora in vivo. Como parte del desarrolo del medicament también se establidad en condiciones aceleradas. Contribuciones y Conclusiones: En los últmos años los medicamentos herbolarios con actividad base a plantas no nativas de México Con este trabajo se para el desarrollo de un medicamento herbolano con los suficientes de caidad para poder ser empleado como conocimiento seria el primer medicamento diffusa. Se de identificación del hepatodamiandl en muestras de T comprobar que presenta actividad hepatoprotectora in vvo hepatoprotectora aprobados por COFEPRIS son en as bases hepetoprotector en nuestro realizado a partir de T odos cromatográficos y espectroscopicos para la ditusa y se pudo comprobar que presenta actividad hepatoprotectora in vivo

Models of hepatoprotective activity assessment

Liver diseases are a major health problem worldwide, making it necessary to develop new molecules that help counteract or prevent such diseases. On account of this fact, investigations aiming to obtain natural and/or synthetic compounds possessing hepatoprotective activity have been undertaken. The development of new drugs consists of a variety of steps, ranging from the discovery of the pharmacological effects in cellular and animal models, to finally demonstrate their efficacy and safety in humans. Different models for assessment of the hepatoprotective activity in vitro, ex vivo and in vivo can be found in medical literature. The purpose of this review is to show the features, main advantages and disadvantages of each of the models, the hepatotoxic agents most commonly used (CCl4, acetaminophen, ethanol, dgalactosamine, t-BuOOH, thioacetamide) as well as the biochemical parameters useful to assess liver damage in the different models

Two Ways to Achieve the Same Goal—Two Validated Quantitative NMR Strategies for a Low-Abundance Natural Product in Standardized Extracts: The Case of Hepatodamianol in Turnera diffusa

The quantification of low-abundance secondary metabolites in plant extracts is an analytical problem that can be addressed by different analytical platforms, the most common being those based on chromatographic methods coupled to a high-sensitivity detection system. However, in recent years nuclear magnetic resonance (NMR) has become an analytical tool of primary choice for this type of problem because of its reliability, inherent simplicity in sample preparation, reduced analysis time, and low solvent consumption. The versatility of strategies based on quantitative NMR (qNMR), such as internal and external standards and electronic references, among others, and the need to develop validated analytical methods make it essential to compare procedures that must rigorously satisfy the analytical well-established acceptance criteria for method validation. In this work, two qNMR methods were developed for the quantification of hepatodamianol, a bioactive component of T. diffusa. The first method was based on a conventional external standard calibration, and the second one was based on the pulse length-based concentration determination (PULCON) method using the ERETIC2 module as a quantitation tool available in TopSpin software. The results show that both procedures allow the content of the analyte of interest in a complex matrix to be determined in a satisfactory way, under strict analytical criteria. In addition, ERETIC2 offers additional advantages such as a reduction in experimental time, reagent consumption, and waste generated

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 200 ng/mL) alone or combined with TGF-β (10 ng/mL) at different time points (24, 48, and 72 h). 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-β. 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