Silymarin
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Silymarin, standardizovaný extrakt z plodu Silybum marianum, je osvědčeným přírodním doplňkem stravy, jenž je využívaný k podpoře léčby řady patologických stavů organismu. Metformin podávaný se silymarinem může zmírnit rozvoj jaterní steatózy, zejména v prediabetickém stavu. Fenofibrát v kombinaci se silymarinem může snížit lipoperoxidaci a expresi CYP2E1 (a tím i produkci ROS), což přispívá ke snížení rizika rozvoje komplikací steatózy v játrech. Mechanismus jeho hypolipidemického působení nespočívá v aktivaci PPARα receptorů (jak je tomu například u fibrátů), ale pravděpodobně ve snížení absorpce cholesterolu ze střeva (což působí i jeho polymerní frakce) nebo zvýšené expresi cytochromů P450 zapojených do metabolismu a vylučování cholesterolu. Upregulace transportních proteinů ABCG5 a ABCG8 silymarinem a n-3 PUFA snižuje hladinu triglyceridů a celkového cholesterolu, což může působit preventivně v rozvoji metabolických poruch vyvolaných hypertriglyceridemií. Uvedené závěry in vivo studií ukazují pozitivní působení silymarinu (ať už jeho komponent, nebo celku) na organismus v rámci prevence nebo podpůrné léčby řady onemocnění včetně metabolického syndromu.
Silymarin, a standardized extract from the Silybum marianum fruit, is a proven natural food supplement that is used to support the treatment of a number of pathological conditions of the organism. Metformin administered with silymarin may reduce the development of hepatic steatosis, especially in the prediabetic state. Fenofibrate in combination with silymarin can reduce lipoperoxidation and CYP2E1 expression (and thus ROS production) which contributes to reducing the risk of developing complications of steatosis in the liver. Mechanism of its hypolipidemic effect does not work via activation of PPARα receptors (as it does in the case of fibrates), but probably in the reduction of cholesterol absorption from the intestine (which is also the effect of its polymer fraction) or in the increased expression of cytochromes P450 involved in the metabolism and excretion of cholesterol. Upregulation of transport proteins ABCG5 and ABCG8 by silymarin and n-3 PUFA reduces the level of triglycerides and total cholesterol, which can act preventively in the development of metabolic disorders caused by hypertriglyceridemia. The stated conclusions of in vivo studies show a positive effect of silymarin (whether its component or whole) on the organism in the prevention or supportive treatment of a number of diseases, including metabolic syndrome.
- MeSH
- lidé MeSH
- nemoci jater farmakoterapie MeSH
- rostlinné extrakty terapeutické užití MeSH
- silibinin farmakologie terapeutické užití MeSH
- silymarin * analýza farmakologie terapeutické užití MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- přehledy MeSH
Díky novým poznatkům narůstá zájem o rostlinné extrakty i v průmyslově vyspělých zemích, jejich klasifikace je však problematická. Je nutné jasně stanovit hranici mezi lékem, s definovaným obsahem individuální účinné látky, a potravním doplňkem, který je volně v prodeji. Extrakt zesemen S. marianum (ESM) vykazuje biologické účinky odpovídající potravním doplňkům, proto je logičtější řadit ESM do této skupiny a sledovat farmakologické účinky u jeho chemicky definovaných složek.
Thanks to the new knowledge, there is an increase of interest in plant extracts in the developed countries, but their classification is, however, problematic. It is necessary to clearly define the borderline between a drug or a defined content of an individual active principle, and a nutritional supplement, which is freely on sale. The extract from the seeds of S. marianum of (ESM) shows biological effects corresponding to nutritional supplements, and it is therefore more logical to class ESM with this group and to investigate the pharmacological effects in its chemically defined components.
Prezentovaná studie měla za cíl porovnat obsah silybinu ve vybraných potravních doplňcích obsahujících silymarin dostupných v České republice. Stanovení silybinu bylo provedeno pomocí HPLC/UV. Naše výsledky ukazují, že většina potravních doplňků obsahuje silybin v referenčním rozmezí 20–40 %. Výrobky NaturProdukt® Silymarin forte s obsahem 40 % silybinu (80,00 ± 0,50 mg) a Nefdesanté® Silymarin ostropestřec s obsahem 33 % silybinu (81,58 ± 0,14 mg) patří mezi výrobky s vysokým obsahem této přírodní látky. Na druhou stranu nejméně silybinu bylo naměřeno u přípravku WALMARK® Ostropestřec mariánský (< 20 %). Výsledky naznačují, že většina z testovaných potravních doplňků je kvalitní a obsahuje deklarované množství obsahových látek.
The aim of this study was to determine the amount of silybin in selected nutraceuticals containing silymarin available in the Czech Republic. The determination of silybin was performed using HPLC/UV. Results show that almost all of the tested nutraceuticals contain the sufficient amount of silybin (range 20–40 %). NaturProdukt® Silymarin forte contained 40 % of silybin (80.00 ± 0.50 mg) and Nefdesanté® Silymarin ostropestřec contained 33 % of silybin (81.58 ± 0.14 mg). Both can be included among the products with high silybin content. On the other hand, the lowest amount of silybin was measured in WALMARK® Ostropestřec mariánský (< 20 %). Our results suggest that almost all of the tested products are of high quality and contain the declared amount of constituents.
- MeSH
- hodnocení léčiv MeSH
- lidé MeSH
- ostropestřec mariánský * MeSH
- potravní doplňky MeSH
- silibinin MeSH
- silymarin MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- srovnávací studie MeSH
Silymarin, a standardised extract of Silybum marianum (milk thistle), comprises mainly of silybin, with dehydrosilybin (DHSB), quercetin, taxifolin, silychristin and a number of other compounds which are known to possess a range of salutary effects. Indeed, there is evidence for their role in reducing tumour growth, preventing liver toxicity, and protecting a number of organs against ischemic damage. The hepatoprotective effects of silymarin, especially in preventing Amanita and alcohol intoxication induced damage to the liver, are a well established fact. Likewise, there is weighty evidence that silymarin possesses antimicrobial and anticancer activities. Additionally, it has emerged that in animal models, silymarin can protect the heart, brain, liver and kidneys against ischemia reperfusion injury, probably by preconditioning. The mechanisms of preconditioning are, in general, well studied, especially in the heart. On the other hand, the mechanism by which silymarin protects the heart from ischemia remains largely unexplored. This review, therefore, focuses on evaluating existing studies on silymarin induced cardioprotection in the context of the established mechanisms of preconditioning.
Silymarin is known for its hepatoprotective effects. Although there is solid evidence for its protective effects against Amanita phalloides intoxication, only inconclusive data are available for alcoholic liver damage. Since silymarin flavonolignans have metal-chelating activity, we hypothesized that silymarin may influence alcoholic liver damage by inhibiting zinc-containing alcohol dehydrogenase (ADH). Therefore, we tested the zinc-chelating activity of pure silymarin flavonolignans and their effect on yeast and equine ADH. The most active compounds were also tested on bovine glutamate dehydrogenase, an enzyme blocked by zinc ions. Of the six flavonolignans tested, only 2,3-dehydroderivatives (2,3-dehydrosilybin and 2,3-dehydrosilychristin) significantly chelated zinc ions. Their effect on yeast ADH was modest but stronger than that of the clinically used ADH inhibitor fomepizole. In contrast, fomepizole strongly blocked mammalian (equine) ADH. 2,3-Dehydrosilybin at low micromolar concentrations also partially inhibited this enzyme. These results were confirmed by in silico docking of active dehydroflavonolignans with equine ADH. Glutamate dehydrogenase activity was decreased by zinc ions in a concentration-dependent manner, and this inhibition was abolished by a standard zinc chelating agent. In contrast, 2,3-dehydroflavonolignans blocked the enzyme both in the absence and presence of zinc ions. Therefore, 2,3-dehydrosilybin might have a biologically relevant inhibitory effect on ADH and glutamate dehydrogenase.
- MeSH
- alkoholdehydrogenasa antagonisté a inhibitory MeSH
- chelátory farmakologie MeSH
- flavonolignany farmakologie MeSH
- glutamátdehydrogenasa antagonisté a inhibitory MeSH
- koně MeSH
- kvasinky účinky léků MeSH
- silibinin farmakologie MeSH
- silymarin farmakologie MeSH
- zinek izolace a purifikace metabolismus MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
Silybum marianum (L.) is a medicinal plant traditionally used in treatment of liver disorders. In last decades, silymarin (SM), a standardized extract from S. marianum seeds has been studied for its dermatological application, namely for UVB-protective properties. However, information on SM and its polyphenols effect on activity of enzymes participating in the (photo)aging process is limited. Therefore, evaluation of SM and its flavonolignans potential to inhibit collagenase, elastase, and hyaluronidase in tube tests was the goal of this study. The antioxidant and UV screening properties of SM and its flavonolignans silybin, isosilybin, silydianin, silychristin and 2,3-dehydrosilybin (DHSB) were also evaluated by a DPPH assay and spectrophotometrical measurement. DHSB showed the highest ability to scavenge DPPH radical and also revealed the highest UVA protection factor (PF-UVA) that corresponds with its absorption spectrum. SM and studied flavonolignans were found to exhibit anti-collagenase and anti-elastase activity. The most potent flavonolignan was DHSB. None of studied flavonolignans or SM showed anti-hyaluronidase activity. Our results suggest that SM and its flavonolignans may be useful agents for skin protection against the harmful effects of full-spectrum solar radiation including slowing down skin (photo)aging.
- MeSH
- antioxidancia chemie izolace a purifikace MeSH
- flavonolignany chemie izolace a purifikace MeSH
- kůže účinky léků patologie účinky záření MeSH
- lidé MeSH
- ostropestřec mariánský chemie MeSH
- rostlinné extrakty chemie MeSH
- semena rostlinná chemie MeSH
- silymarin chemie izolace a purifikace MeSH
- ultrafialové záření škodlivé účinky MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
