Antioxidant and antiviral activities of silybin fatty acid conjugates

Gažák, Radek; Purchartová, Kateřina; Marhol, Petr; Zivná, Lucie; Sedmera, Petr; Valentová, Kateřina; Kato, Nobuo; Matsumura, Hiroyo; Kaihatsu, Kunihiro; Křen, Vladimı́r

doi:10.1016/j.ejmech.2009.11.056

Cited by 56 publications

(41 citation statements)

References 43 publications

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“…The lower activity of SLP might relate to interactions between the different substances in the compound evaluated (Medix). The antioxidative activities of SLB and SLM that we observed are in agreement with previous research, which has reported strong DPPH free radical-scavenging activity for these compounds [35, 36]. …”

Section: Discussionsupporting

confidence: 93%

In vitro assessment of hepatoprotective agents against damage induced by acetaminophen and CCl4

Torres-González

Minsky

Espinosa

et al. 2017

BMC Complement Altern Med

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BackgroundIn vitro bioassays are important in the evaluation of plants with possible hepatoprotective effects. The aims of this study were to evaluate the pretreatment of HepG2 cells with hepatoprotective agents against the damage induced by carbon tetrachloride (CCl4) and paracetamol (APAP).MethodsAntioxidative activity was measured using an assay to measure 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging. The in vitro hepatotoxicity of CCl4 and APAP, and the cytotoxic and hepatoprotective properties of silymarin (SLM), silybinin (SLB), and silyphos (SLP) were evaluated by measuring cell viability; activities of aspartate aminotransferase (AST), alanine aminotransferase (ALT), and lactate dehydrogenase (LDH); total antioxidant capacity (TAOxC); and reduced glutathione (GSH), superoxide dismutase (SOD), and lipid peroxidation (malondialdehyde (MDA) levels).ResultsOnly SLB and SLM showed strong antioxidative activity in the DPPH assay (39.71 ± 0.85 μg/mL and 14.14 ± 0.65 μg/mL, respectively). CCl4 induced time- and concentration-dependent changes. CCl4 had significant effects on cell viability, enzyme activities, lipid peroxidation, TAOxC, and SOD and GSH levels. These differences remained significant up to an exposure time of 3 h. APAP induced a variety of dose- and time-dependent responses up to 72 h of exposure. SLM, SLB, and SLP were not cytotoxic. Only SLB at a concentration of 100 μg/mL or 150 μg/mL significantly decreased the enzyme activities and MDA level, and prevented depletion of total antioxidants compared with CCl4.ConclusionsCCl4 was more consistent than APAP in inducing cell injury. Only SLB provided hepatoprotection. AST, LDH, and MDA levels were good markers of liver damage.

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Section: Discussionsupporting

confidence: 93%

In vitro assessment of hepatoprotective agents against damage induced by acetaminophen and CCl4

Torres-González

Minsky

Espinosa

et al. 2017

BMC Complement Altern Med

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“…We have shown that co-adminstration of silymarin (100 mg/kg) to Mn exposed rats led to a reduction of reactive oxygen species. Its neuroprotective properties exhibited various pathways of action: (1) Inhibition of lipid peroxidation and membrane stabilization (2) a decreased glutathione depletion (3) an ability to scavenge and quench reactive oxygen species based on the strong antioxidant capacity of the flavonoids and (iiii) a direct modulation of antioxidant enzymes synthesis [42][43][44].…”

Section: Discussionmentioning

confidence: 99%

Improvement of Cerebellum Redox States and Cholinergic Functions Contribute to the Beneficial Effects of Silymarin Against Manganese-Induced Neurotoxicity

et al. 2011

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Manganese (Mn) is a potent neurotoxin involved in the initiation and progression of various cognitive disorders. Oxidative stress is reported as one of accepted mechanisms of Mn toxicity. The present study was designed to explore the effects of silymarin, a natural antioxidant, in attenuating the toxicity induced by Mn in rat cerebellum. In this investigation, rats were treated orally with MnCl₂ (20 mg/ml) for 30 days, subsets of these animals were treated intraperitoneally daily with silymarin (100 mg/kg) along with respective controls. Mn exposure caused a marked oxidative stress in cerebellum as indicated by a significant decrease in the activities of enzymatic antioxidants like superoxide dismutase, catalase and glutathione peroxidase and in the levels of non-enzymatic antioxidants like reduced glutathione (GSH), total thiols and vitamin C. Conversely an increase was obtained in lipid and protein markers such as thiobarbituric reactive acid substances, lipid hydroperoxide and protein carbonyl products contents. A significant increase in acetylcholinesterase and a decrease in Na⁺/K⁺-ATPase activities were also shown, with a substantial rise in the expression of acetylcholinesterase and inducible nitric oxide synthase (iNOS), and nitric oxide levels. The potential effect of SIL to prevent Mn induced neurotoxicity was also reflected by histopathological observations. Rats exposed to Mn showed a reduced number and morphological alterations of cerebellar Purkinje cells. These phenomenons were completely reversed by SIL co-treatment. We concluded that silymarin may protect against Mn-induced oxidative stress in cerebellum by inhibiting both lipid and protein oxidation and by activating acetylcholinesterase and inducible nitric oxide synthase (iNOS) gene expression.

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“…SIL is also efficacious in preventing hepatic lipid peroxidation and ischemia (Lettéron et al 1990; Raza et al 2011). Recently, SIL derivatives have gained attention because of their chemoprotective and anticancer activities (Singh and Agarwal 2004;Gazák et al 2010;Gándara et al 2014).…”

Section: Introductionmentioning

confidence: 98%

Preparation and performance evaluation of emulsomes as a drug delivery system for silybin

Zhou

Chen

2015

Arch. Pharm. Res.

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We developed silybin (SIL) emulsomes and evaluated their physicochemical properties and the in vivo pharmacokinetics of SIL delivered by emulsomes in rats. SIL emulsomes were prepared using the thin film dispersion method. SIL emulsomes were evaluated for their entrapment efficiency, particle size, zeta potential, morphology, in vitro release, and in vivo drug delivery in rats. The entrapment efficiency was above 80 %. The average particle size and zeta potential were 364.1 ± 20 nm and -34 ± 8 mV, respectively. Morphological analysis revealed that the SIL emulsomes were spherical in shape. Compared to an SIL solution, emulsomes produced sustained release of SIL for up to 48 h after an initial burst release in vitro. The pharmacokinetics of SIL emulsomes in rats were evaluated after intravenous injection, and the results were compared with those obtained for the control SIL solution. Following SIL delivery by emulsomes, the area under the curve was 2.2-fold higher and the mean residence time was 2.5-fold higher than the corresponding values recorded using SIL solution. Hence, emulsomes might represent a promising system for improving the bioavailability of lipophilic drugs. Moreover, emulsomes produce sustained drug release, which is advantageous in the clinical setting.

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Antioxidant and antiviral activities of silybin fatty acid conjugates

Cited by 56 publications

References 43 publications

In vitro assessment of hepatoprotective agents against damage induced by acetaminophen and CCl4

In vitro assessment of hepatoprotective agents against damage induced by acetaminophen and CCl4

Improvement of Cerebellum Redox States and Cholinergic Functions Contribute to the Beneficial Effects of Silymarin Against Manganese-Induced Neurotoxicity

Preparation and performance evaluation of emulsomes as a drug delivery system for silybin

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