• Biomolecules & Therapeutics
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• 제21권4호
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• pp.264-269
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• 2013

Silymarin has been introduced fairly recently as a hepatoprotective agent. But its mechanisms of action still have not been well established. The aim of this study was to make alcoholic fatty liver model of rats in a short time and investigate silymarin's protective effects and possible mechanisms on alcoholic fatty liver for rats. The model of rat's alcoholic fatty liver was induced by intragastric infusion of ethanol and high-fat diet for six weeks. Histopathological changes were assessed by hematoxylin and eosin staining (HE). The activities of alanine transarninase (ALT) and aspartate aminotransferase (AST), the levels of total bilirubin (TBIL), total cholesterol (TC) and triglyceride (TG) in serum were detected with routine laboratory methods using an autoanalyzer. The activities of superoxide dismutase (SOD) and glutathione peroxidase (GPx) and the level of malondialdehyde (MDA) in liver homogenates were measured by spectrophotometry. The TG content in liver tissue was determined by spectrophotometry. The expression of nuclear factor-${\kappa}B$ (NF-${\kappa}B$), intercellular adhesion molecule-1 (ICAM-1) and interleukin-6 (IL-6) in the liver were analyzed by immunohistochemistry. Silymarin effectively protected liver from alcohol-induced injury as evidenced by improving histological damage situation, reducing ALT and AST activities and TBIL level in serum, increasing SOD and GPx activities and decreasing MDA content in liver homogenates and reducing TG content in liver tissue. Additionally, silymarin markedly downregulated the expression of NF-${\kappa}B$ p65, ICAM-1 and IL-6 in liver tissue. In conclusion, Silymarin could protect against the liver injury caused by ethanol administration. The effect may be related to alleviating lipid peroxidation and inhibiting the expression of NF-${\kappa}B$.

• Journal of Applied Biological Chemistry
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• 제65권3호
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• pp.221-230
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• 2022

본 연구는 실리마린의 항산화 및 항염증 활성을 알아보고자 하였다. 항산화 활성은 2,2-diphenyl-1-picrylhydrazyl (DPPH)와 2,2'-azino-bis (3-ethylbenzothiazoline5 6-sulfonic acid) (ABTS) 라디칼에 대한 소거능을 측정하여 확인하였다. 실리마린은 1 mg/mL의 농도에서 DPPH 라디칼을 71%, ABTS 라디칼을 78% 소거하여 우수한 항산화 효과를 나타냈다. 실리마린은 DNA의 산화적 손상을 효과적으로 억제하였고 사람 혈청 단백질과 Cu,Zn-SOD의 산화적 변형을 억제하였다. 또한 실리마린은 H₂O₂와 LPS에 의한 세포사멸, ROS 생성 및 DNA fragmentation을 억제하였다. 본 연구 결과들을 통해 실리마린은 효과적인 천연 항산화 및 항염증 소재로 적용될 수 있음을 제시하였다.

• Journal of Pharmaceutical Investigation
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• 제25권1호
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• pp.37-46
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• 1995

The experiment was designed to investigate the sustained release dosage form of silymarin (SL) from chitosan (CS) carrier. Solid dispersed system was prepared by mixing the drug with chitosan. This solid dispersed system was cross-linked by glutaraldehyde, formaldehyde, acetaldehyde and butylaldehyde, respectively. The dissolution rates of these preparations were compared with each other in vitro. The silymarin was mired with anionic alginate gel and bead was prepared by dropping this mixture to cationic chitosan solution including calcium chloride. Chitosan encapsulated alginate bead after drying in the oven was investigated for the dissolution rate. The dissolution rate of SL-CS mixture was delayed with increase in the amounts of CS and the concentration of aldehyde. The effect on the delay of dissolution rate was in the increasing order of formaldehyde, glutaraldehyde, acetaldehyde, butylaldehyde. The dissolution rate of chitosan encapsulated alginate bead was parallel with the concentration of chitosan in diluted hydrochloric acid solution and delayed with increase in the concentration of chitosan in phosphate buffer solution.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-1
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• pp.56-56
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• 2003

Carduus marianus extract (formally called silymarin) have been used mainly as a medicament for hepatobiliary diseases. The major component of silymarin is silybin, which constitutes between 50 and 70% of the drug and is the major active component. Many experiments show the efficacy of silybin parenterally administerated. But, its bioavailability is low after oral administration due to its low solubility in water. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.296.2-296.2
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• 2003

Carduus marianus extract (formally called silymarin) have been used mainly as a medicament for hepatobiliary diseases. The major component of silymarin is silybin, which constitutes between 50 and 70％ of the drug and is the major active component. Many experiments show the efficacy of silybin parenterally administerated. But, its bioavalability is low after oral administration due to its low solubility in water. (omitted)

• 생약학회지
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• 제29권2호
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• pp.146-148
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• 1998

The increased AST and ALT activities of rat serum disturbed by $CCl_4-intoxication$ intoxication were significantly inhibited by silymarin and biphenyl dimethylene dicarboxylate at the oral doses of 150 and 5 mg/kg, respectively. The combined administration of the drugs showed remarkable inhibition of the enzyme activities. This fact may suggest that the two drugs have potentiative action in this experiment.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2001년도 International Symposium on Dietary and Medicinal Antimutgens and Anticarcinogens
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• pp.130-130
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• 2001

Silymarin, a polyphenolic flavonoid antiodant, has been shown to have anti-inflammatory, hepatoprotective, and anticarcinogenic effects. In the present study, we report the inhibitory effect of silymarin on nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) mRNA expression in macrophages. In vivo administration of silymarin attenuated NO production of peritoneal macrophages in lipopolysaccharide (LPS)-treated mice.(omitted)

• 약학회지
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• 제54권2호
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• pp.97-101
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• 2010

Recently, it was found that the formation of reactive metabolites by cytochrome P450s as well as the depletion of glutathione would play important roles in hepatotoxicity induced by 1-bromopropane. In the present study, possible roles of anti-oxidants in 1-bromopropane-induced hepatotoxicity were investigated in male ICR mice. The hepatotoxicity induced by 1-bromopropane was significantly protected by the co-treatment with either N-acetyl cysteine or silymarin. 1-Bromopropane-induced decrease in hepatic glutathione level was significantly protected by the pretreatment with N-acetyl cysteine. Taken together, the present results indicated that the reduction of hepatic glutathione level caused by 1-bromopropane treatment might be associated in 1-bromopropane-induced hepatotoxicity in mice.

• 대한한방내과학회지
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• 제44권3호
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• pp.402-417
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• 2023

Objective: Liver fibrosis is a highly conserved wound-healing response and the final common pathway of chronic inflammatory injury. This study aimed to evaluate the potential anti-fibrotic effect of the combination of Rhei Radix et Rhizoma water extract (RW) and silymarin in a thioacetamide (TAA)-induced liver fibrosis model. Methods: The liver fibrosis mouse model was established through the intraperitoneal injection of TAA (1 week 100 mg/kg, 2-3 weeks 200 mg/kg, 4-8 weeks 400 mg/kg) three times per week for eight weeks. Animal experiments were conducted in five groups; Normal, Control (TAA-induced liver fibrosis mice), Sily (silymarin 50 mg/kg), RSL (RW 50 mg/kg+silymarin 50 mg/kg), and RSH (RW 100 mg/kg+silymarin 50 mg/kg). Biochemical analyses were measured in serum, including aspartate aminotransferase (AST), alanine aminotransferase (ALT), malondialdehyde (MDA), and ammonia levels. Liver inflammatory cytokines and fibrous biomarkers were measured by Western blot analysis, and liver histopathology was evaluated through tissue staining. Results: A significant decrease in the liver function markers AST and ALT and a reduction in ammonia and total bilirubin were observed in the group treated with RSL and RSH. Measurement of reactive oxygen species and MDA revealed a significant decrease in the RSL and RSH administration group compared to the TAA induction group. The expression of extracellular matrix-related proteins, such as transforming growth factor β1, α-smooth muscle actin, and collagen type I alpha 1, was likewise significantly decreased. All drug-administered groups had increased matrix metalloproteinase-9 but a decreasing tissue inhibitor of matrix metalloproteinase-1. RSL and RSH exerted a significant upregulation of NADPH oxidase 2, p22^phox, and p47^phox, which are oxidative stress-related factors. Furthermore, pro-inflammatory proteins such as cyclooxygenase 2 and interleukin-1β were markedly suppressed through the inhibition of nuclear factor kappa B activation. Conclusions: The administration of RW and silymarin suppressed the NADPH oxidase factor protein level and showed a tendency to reduce inflammation-related enzymes. These results suggest that the combined administration of RW and silymarin improves acute liver injury induced by TAA.

• 한국식품영양과학회지
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• 제38권9호
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• pp.1153-1160
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• 2009

Monascus purpureus KCCM 12002 홍국균으로 발효시킨 홍국발효홍삼 분말을 식이 중에 1% 수준으로 첨가하여 4주간 흰쥐에 급여한 후 혈청 임상생화학적 특성과 조직 내항산화 활성 및 간 조직에 미치는 영향을 검토하였다. 체중증가량, 식이섭취량 및 음료섭취량은 각 실험 군 간에 유의적인 차이는 없었다. 간 조직 총 중량 및 상대 중량은 다른 실험 군에 비해 홍국발효홍삼 분말 투여 군에서만 유의적으로 증가하였다. 간 손상 임상지표인 AST 및 $\gamma$-GTP 활성은 대조군에 비해 홍국발효홍삼 분말 투여 군에서 현저하게 저하하였으나, ALT 활성에는 영향을 미치지 못하였다. 혈중 총 지질 및 중성지질 농도는 대조군에 비해 silymarin 투여 군에서 유의적으로 감소하였고, 홍삼 분말 투여 군에서는 감소경향을 보인 반면 홍국발효홍삼 분말 투여 군에서는 유의적인 증가를 나타내었다. 혈청 총 콜레스테롤 농도는 대조군에 비해 silymarin, 홍삼 분말 및 홍국발효홍삼 분말 투여 군들에서 모두 저하경향을 보였다. 혈중 HDL-콜레스테롤 농도는 대조군에 비해 홍국발효홍삼 분말 투여 군에서만 유의적으로 증가하였다. 따라서 총 콜레스테롤 농도에 대한 HDL-콜레스테롤 농도의 비로 나타내는 동맥경화지수(AI)는 대조군에 비해 Silymarin 및 홍삼 분말 투여 군에서 유의적으로 감소하였고, 홍국발효홍삼 분말 투여 군에서도 현저하게 감소하였다. 간 조직의 과산화지질(TBARS)을 측정한 결과, 대조군에 비해 홍국발효홍삼 분말 투여 군에서는 유의적으로 감소하였으나, silymarin 및 홍삼 분말 투여 군에서는 감소경향을 보였다. 특히 홍국발효홍삼은 간 조직내에서 높은 과산화지질 억제작용을 나타내어 조직 내 항산화 물질로 잘 알려진 glutathione 농도는 대조군에 비해 silymarin 및 홍국발효홍삼 분말 투여 군에서 유의적으로 증가하였으며, 홍삼 분말 투여 군에서만 증가경향을 보였다. 간 조직의 조직학적 검사를 실시한 결과 대조군에서는 혈관을 중심으로 간 소엽 구조가 잘 유지되었으며, 간세포들은 풍부한 호산성 세포질과 둥근 핵을 가지고 있었고 간세포판은 대부분 한 층으로 잘 유지되어 있었으며, silymarin, 홍삼 분말 및 홍국발효홍삼 분말 투여 군에서도 대조군과 같은 현상을 보였다. 이상의 실험결과 홍국발효홍삼은 항동맥경화 작용뿐만 아니라 간 조직 내 항산화물질 증가에 의한 산화스트레스를 경감시킴으로써 향후 간 독성 개선 효능을 가지는 건강기능식품 개발의 기초 소재로 활용될 가능성이 높은 것으로 판단되어진다.