Pancreatic lipase (PNLIP, EC 3.1.1.3) plays a pivotal role in the digestion of dietary lipids, a metabolic pathway directly related to obesity. One of the effective strategies in obesity treatment is the inhibition of PNLIP, which is possible to be achieved by specific phenolic compounds occurring in high abundance in some plants. In this study, a multidisciplinary approach is presented investigating the PNLIP inhibitory effect of 33 plants belonging in the Asteraceae botanical family. In the first stage of the study, a rapid and cost-efficient PNLIP assay in a 96-microwell plate format was developed and important parameters were optimized, e.g., the enzyme substrate. Upon PNLIP assay optimization, aqueous and dichloromethane Asteraceae plant extracts were tested and a cut-off inhibition level was set to further analyze only the samples with a significant inhibitory effect (inhibitory rate > 40%), using an ultra-high-performance liquid chromatography hybrid quadrupole time-of-flight mass spectrometry (UHPLC-q-TOF-MS) method. Specifically, a metabolomic suspect screening was performed and 69 phenolic compounds were tentatively identified, including phenolic acids, flavonoids, flavonoid-3-O-glycosides, and flavonoid-7-O-glycosides, amongst others. In the case of aqueous extracts, phytochemicals known for inducing PNLIP inhibitory effect, e.g., compounds containing galloyl molecules or caffeoylquinic acids, were monitored in Chrysanthemum morifolium, Grindella camporum and Hieracium pilosella extracts. All in all, the presented approach combines in vitro bioactivity measurements to high-end metabolomics to identify phenolic compounds with potential medicinal and/or dietary applications.

• Klíčová slova
• bioprospecting, enzyme assay, in vitro testing, metabolomics, obesity, phytochemicals, polyphenols, suspect screening, ultra-high-performance liquid chromatography hybrid quadrupole time-of-flight mass spectrometry,
• MeSH
• Asteraceae * chemie   MeSH
• chromatografie kapalinová MeSH
• fenoly analýza   MeSH
• flavonoidy chemie   MeSH
• fytonutrienty analýza   MeSH
• glykosidy MeSH
• hmotnostní spektrometrie MeSH
• lipasa MeSH
• lipidy MeSH
• methylenchlorid MeSH
• obezita MeSH
• rostlinné extrakty chemie   farmakologie   MeSH
• vysokoúčinná kapalinová chromatografie metody   MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• fenoly MeSH
• flavonoidy MeSH
• fytonutrienty MeSH
• glykosidy MeSH
• lipasa MeSH
• lipidy MeSH
• methylenchlorid MeSH
• rostlinné extrakty MeSH

Milk thistle seeds contain a mixture of flavonoids known as silymarin, which consists of silybin, isosilybin, silychristine, and silydianin. Until now, there has been no evidence of monitoring the digestibility of silymarin complex in horses. The aim of the research was to evaluate the digestibility of silymarin complex and the effect of nutrient digestibility in horses. Different daily feed doses (FD) of milk thistle expeller (0 g, 100 g, 200 g, 400 g, 700 g) were administered to five mares kept under the same conditions and at the same feed rations. Digestibility of silymarin complex was monitored by HPLC-UV. Digestible energy (DE), crude protein, crude fat, crude fiber, nitrogen-free extract (NFE), crude ash, calcium (Ca), and phosphorus (P) were determined according ISO/IEC 17025:2017. The biochemical profile of blood plasma (total protein, albumin, alanine transaminase (ALT), aspartate transaminase (AST), alkaline phosphatase (ALP), gamma-glutamyl transferase (GGT), bilirubin, total cholesterol, HDL cholesterol, LDL cholesterol, triacyl glyceride (TAG), non-esterified fatty acid (NEFA), creatine kinase (CK), creatinine, urea, glutathione peroxidase (GSH-Px), total antioxidant status (TAS), glucose, calcium, and inorganic phosphate) was investigated. Moreover, the flavonolignans of the silymarin complex in plasma were detected. Statistically significant differences (p ≤ 0.05) were found between daily doses of milk thistle expellers in digestibilities. Our findings showed the digestibility of flavonolignans increased with the daily dose and then stagnated with the dose of milk thistle seed cakes at 700 g/day.

• Klíčová slova
• blood, horse nutrition, plasma, silybin, silychristin, silydianin, silymarin,
• Publikační typ
• časopisecké články MeSH

The consumption of herbal-based supplements, which are believed to have beneficial effects on human health with no side effects, has become popular around the world and this trend is still increasing. Silybum marianum (L.) Gaertn, commonly known as milk thistle (MT), is the most commonly studied herb associated with the treatment of liver diseases. The hepatoprotective effects of active substances in silymarin, with silybin being the main compound, have been demonstrated in many studies. However, MT can be affected by toxigenic micro-fungi and contaminated by mycotoxins with adverse effects. The beneficial effect of silymarin can thus be reduced or totally antagonized by mycotoxins. MT has proven to be affected by micro-fungi of the Fusarium and Alternaria genera, in particular, and their mycotoxins. Alternariol-methyl-ether (AME), alternariol (AOH), beauvericin (BEA), deoxynivalenol (DON), enniatin A (ENNA), enniatin A1 (ENNA1), enniatin B (ENNB), enniatin B1 (ENNB1), HT-2 toxin (HT-2), T-2 toxin (T-2), tentoxin (TEN), and zearalenone (ZEA) seem to be most significant in MT-based dietary supplements. This review focuses on summarizing cases of mycotoxins in MT to emphasize the need for strict monitoring and regulation, as mycotoxins in relation with MT-based dietary supplements are not covered by European Union legislation.

• Klíčová slova
• food supplements, liver diseases, milk thistle, mycotoxins, silymarin,
• MeSH
• Evropská unie MeSH
• lidé MeSH
• mykotoxiny škodlivé účinky   analýza   MeSH
• ostropestřec mariánský škodlivé účinky   MeSH
• potravní doplňky škodlivé účinky   analýza   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• přehledy MeSH
• Názvy látek
• mykotoxiny MeSH

Silymarin is a well-known standardized extract from the seeds of milk thistle (Silybum marianum L., Asteraceae) with a pleiotropic effect on human health, including skin anticancer potential. Detailed characterization of flavonolignans properties affecting interactions with human skin was of interest. The partition coefficients log Pow of main constitutive flavonolignans, taxifolin and their respective dehydro derivatives were determined by a High Performance Liquid Chromatography (HPLC) method and by mathematical (in silico) approaches in n-octanol/water and model lipid membranes. These parameters were compared with human skin intake ex vivo. The experimental log Pow values for individual diastereomers were estimated for the first time. The replacement of n-octanol with model lipid membranes in the theoretical lipophilicity estimation improved the prediction strength. During transdermal transport, all the studied compounds permeated the human skin ex vivo; none of them reached the acceptor liquid. Both experimental/theoretical tools allowed the studied polyphenols to be divided into two groups: low (taxifolin, silychristin, silydianin) vs. high (silybin, dehydrosilybin, isosilybin) lipophilicity and skin intake. In silico predictions can be usefully applied for estimating general lipophilicity trends, such as skin penetration or accumulation predictions. However, the theoretical models cannot yet provide the dermal delivery differences of compounds with very similar physico-chemical properties; e.g., between diastereomers.

• Klíčová slova
• Silybum marianum, experimental and computational hydrophobicity, flavonoids, flavonolignans, skin intake, theoretical lipid membrane models,
• MeSH
• hydrofobní a hydrofilní interakce MeSH
• lékové transportní systémy * MeSH
• lidé MeSH
• ostropestřec mariánský chemie   MeSH
• permeabilita MeSH
• polyfenoly aplikace a dávkování   chemie   farmakologie   MeSH
• škára účinky léků   MeSH
• termodynamika MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• polyfenoly MeSH