Determination of Flavonolignan Compositional Ratios in Silybum marianum (Milk Thistle) Extracts Using High-Performance Liquid Chromatography.

Milk thistle is one of the most popular ingredients in the liver protection products market. Silymarin is the main component of milk thistle and contains multiple isomers. There have been few studies focusing on the compositional ratios of silymarin isomers. In this study, we developed an HPLC method for the separation and quantification of silymarin isomers, thereby elucidating their compositional ratios. Through the analysis of more than 40 milk thistle extract products on the market, we found that the ratios, specifically Ratio 1 (the silybin B content to the silybin A content, SBNB/SBNA) and Ratio 2 (the sum of the contents of silybin B and isosilybin B to the sum of the contents of silybin A and isosilybin A, (SBNB + IBNB)/(SBNA + IBNA)), are highly consistent across milk thistle extracts, averaging approximately 1.58 and 1.28, respectively. Furthermore, such ratios were verified in milk thistle seed samples. This study introduces significant findings concerning the stable ratios among silymarin isomers in milk thistle extracts and seeds, thereby offering an innovative approach for quality assurance of milk thistle extracts.

Chemical Standardization of Milk Thistle (Silybum marianum L.) Extract Using UHPLC-MS/MS and the Method of Standard Addition.

Extracts prepared from the seeds of the medicinal plant milk thistle [Silybum marianum (L.) Gaertn. (Asteraceae)] are widely used as dietary supplements due to anti-inflammatory, antitumor, and hepatoprotective effects. Called silymarin, the main components of lipophilic extracts of milk thistle seeds are flavonoids and flavonolignans including silybin A, silybin B, isosilybin A, isosilybin B, silydianin, silychristin, taxifolin, and 2,3-dehydrosilybins. The aim of this study was to develop a method based on UHPLC-MS/MS for the chemical authentication and standardization of milk thistle silymarin. Validation included the method of standard addition to account for the lack of a blank matrix. Potential matrix effects were investigated by analyzing silymarin standards dissolved only in the initial UHPLC mobile phase. Measurements of six flavonolignans and taxifolin in the milk thistle extract using UHPLC-MS/MS with standard addition or external standard calibration produced similar results for all analytes except silydianin and 2,3-dehydrosilybin B, which showed significant peak enhancement during negative ion electrospray due to botanical matrix effects. The UHPLC-MS/MS-based method of standard addition requires <10 min per injection and is suitable for the standardization of silymarin from milk thistle in support of preclinical and clinical studies of safety and efficacy.

Bioavailability augmentation of silymarin using natural bioenhancers: An in vivo pharmacokinetic study

Abstract Pharmacokinetic studies were carried out in male and female rats to quantify silymarin as silybin (A+B) after the oral administration of various silymarin formulations combined with three bioenhancers, namely, lysergol, piperine, and fulvic acid, and compared with plain silymarin formulation (control). A non-compartmental analysis, model independent analysis, was utilized, and various pharmacokinetic parameters (C max, T max, and AUC 0-t) were calculated individually for each treatment group, and the values were expressed as mean ± SEM (n = 6). Plasma samples obtained from the rats were analyzed for the concentration of silymarin through a validated RP-HPLC method and on the basis of data generated from the pharmacokinetic studies. Results indicated that the bioenhancers augmented pharmacokinetic parameters and bioavailability increased 2.4-14.5-fold in all the formulations compared with the control. The current work envisages the development of an industrially viable product that can be further subjected to clinical trials and scientifically supports the development of silymarin as a contemporary therapeutic agent with enhanced bioavailability and medicinal values.

Silimarina / Silymarin

Introduction: Silymarin is a plant known for decades and with varied medicinal properties targeted to the liver.Objective: To investigate evidence of the use of silymarin in alcoholic liver disease and on hepatitis B and C.Methods: Review of the literature through electronic search, including studies of good methodological quality assessing the effects of silymarin on liver.Results: A systematic review of 13 studies and only 3 of them with good methodological quality showed unsatisfactory results in chronic liver diseases most common evolutionary disease as alcoholic and viral hepatitis B and C. Were demonstrated statistically significant changes in the decrease of transaminases and gamma-GT (gamma-glutamyl transpeptidase) in alcoholic liver disease, but did not change the mortality and other clinical and biochemical parameters in both alcoholic liver disease and in liver viral.Conclusion: Experimental studies have shown beneficial effects of silymarin in the liver by various drugs. However, there is insufficient evidence of its efficacy and safety in the treatment of chronic alcoholic liver disease and viral in its outcome greater mortality.

Introdução: A silimarina é uma planta conhecida há décadas e com propriedades medicinais variadas direcionadas para o fígado.Objetivo: Verificar evidências do uso da silimarina na doença alcóolica do fígado e nas hepatites B e C.Métodos: Revisão sistematizada da literatura por meio de busca eletrônica, incluindo estudos com boa qualidade metodológica que avaliem os efeitos da silimarina em hepatopatias.Resultados: Uma revisão sistemática com 13 estudos e somente 3 deles com boa qualidade metodológica mostraram resultados não satisfatórios nas hepatopatias crônicas evolutivas mais comuns como por doença alcóolica e hepatites virais B e C. Foram demonstradas alterações estatisticamente significantes na diminuição das transaminases e gama-GT (gama-glutamil transpeptidase) na doença hepática alcoólica, porém, sem alterar a mortalidade e outros parâmetros clínicos e bioquímicos tanto na hepatopatia alcoólica como nas hepatopatias virais.Conclusão: Estudos experimentais mostraram efeitos benéficos da silimarina nas hepatopatias por diversas drogas. No entanto, não há evidências suficientes de sua eficácia e segurança no tratamento de hepatopatias crônicas alcoólicas e virais no seu desfecho maior, a mortalidade.