• Archives of Pharmacal Research
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• 제27권9호
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• pp.947-953
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• 2004

The antioxidative and hepatoprotective potentials of two anthraquinones, alaternin (2-hydroxy-emodin) and emodin, to scavenge and/or inhibit hydroxyl radicals generated by the Fenton reaction and to protect tacrine-induced cytotoxicity in human liver derived HepG2 cells were evaluated, respectively. The inhibitory activity on hydroxyl radical generated in a cell-free chemical system (FeSO$_4$/$H_2O$$_2$) was investigated by a fluorescence spectrophotometer using a highly fluorescent probe, 2$^1$,7$^1$-dichlorofluorescein. The hydroxyl radical scavenging activity was determined by electron spin resonance spectroscopy using 5,5-dimethy-1-pyrroline-N-oxide as hydroxyl radicals trapping agents. Tacrine-induced HepG2 cell toxicity was determined by a 3-［4,5-dimethylthiazole-2yl］-2,5-diphenyltertrazolium bromide assay. Although the scavenging activity of alaternin on hydroxyl radical was similar to that of emodin in dose-dependent pat-terns, the inhibitory activity exhibited by the former on hydroxyl radical generation was stron-ger than that of the latter, with $IC_{50}$/ values of 3.05$\pm$0.26 $\mu$M and 13.29$\pm$3.20 $\mu$M, respectively. In addition, the two anthraquinones, alaternin and emodin showed their hepatoprotective activ-ities on tacrine-induced cytotoxicity, and the EC$_{50}$ values were 4.02 11M and 2.37 $\mu$M, respec-tively. Silymarin, an antihepatotoxic agent used as a positive control exhibited the EC$_{50}$ value of 2.00 $\mu$M. These results demonstrated that both alaternin and emodin had the simultaneous antioxidant and hepatoprotective activities.ies.

• Archives of Pharmacal Research
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• 제24권2호
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• pp.114-118
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• 2001

The present study was undertaken to investigate whether or not the hepatoprotective activity of acetylbergenin was superior to bergenin in carbon tetrachloride ($CCl_4$)-intoxicated rat. Acetylbergenin was synthesized by acetylating bergenin, which was isolated from Mallotus japonicus. The hepatoprotective effects of acetylbergenin were examined against $CCl_4$-induced liver damage in rats by means of serum and liver biochemical Indices. Acetylbergenin was administered orally once daily for 7 successive days, then a 0.5 ${m/kg}$ mixture of $CCl_4$in olive oil (1:1) was intraperitoneally injected at 12 h and 36 h after the final administration of acetylbergenin. Pretreatment with acetylbergenin reduced the elevated serum enzymatic activities of alanine/aspartate aminotransferase, sorbitol dehydrogenase and $\gamma$-glutamyltransferase in a dose dependent fashion. Acetylbergenin also prevented the elevation of hepatic malondialdehyde formation and depletion of glutathione content dose dependently in $CCl_4$-intoxicates rats. In addition, the decreased activities of glutathione S-transferase and glutathione reductase were restored to almost normal levels. The results of this study strongly suggest that acetylbergenin n has potent hepatoprotective activity against $CCl_4$-induced hepatic damage in rats by glutathione-mediated detoxification as well as having free radical scavenging activity. In addition, acetylbergenin doses of 50 ${mg/kg}$showed almost the same levels of hepatoprotection activity as 100 ${mg/kg}$ of bergenin, indicating that lipophilic acetylbergenin is more active against the antihepatotoxic effects of $CCl_4$ than those of the much less lipophilic bergenin.

• Biomolecules & Therapeutics
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• 제5권2호
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• pp.194-201
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• 1997

The hepatoprotective activity of six extracts (BE, EE, HH, PS-1, PS-2, KP) from Artimisia iwayomogi was investigated against experimentally produced hepatic damages. Silymarin, DDB and UDCA were used as reference compounds. Treatment with PS-1 extract reduced hepatic demages induced by $CCl_4$, acetaminophen and ANIT but it did not alter ethionine-induced hepatotoxicity In addition, PS-1 extract showed a protective effect against chronic $CCl_4$-induced hepatotoxicity as well as liver regeneration. PS-2 and KP extracts exhibited significant antihepatotoxic effects on D-galactosamine-induced hepatitis. Treatment with EE extract inhibited ethionine-induced fatty liver. These data indicate that the PS-1 extract is the roost hepato-protective constituent and rationalize the traditional use of this plant in hepatobiliary disorders.

• Natural Product Sciences
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• 제10권4호
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• pp.182-189
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• 2004

To find the action mechanism of the MeOH extract (LFS) of Ligularia fischeri var. spiciformis herbs (Compositae) and its active component, 3,4-dicaffeoylquinic acid (DCQA) on antihepatotoxicity, the effect was investigated on hepatic lipid perxodation and drug-metabolizing enzyme activities in acetaminophen-treated rat. Pretreatment with 250 mg/kg LFS (p.o.) and 10 mg/kg DCQA (p.o.) significantly decreased hepatic lipid peroxidation caused by acetaminophen injection. Further, LFS and DCQA inhibited hepatic microsomal enzyme activation such as hepatic P-450 cytochrome $b_5$, aniline hydroxylase and aminopyrine N-demethylase, suggesting that the two substances might effectively prevent the metabolic activation or scavenge electrophilic intermediates capable of causing hepatotoxicity. Both LFS and DCQA increased hepatic glutathione content and glutathione reductase activity, indicating that both resultantly prevented hepatotoxicity via antioxidative mechanism. Therefore, it was found that LFS had antihepatotoxicity based on the antioxidative action of DCQA.

• 생약학회지
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• 제18권4호
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• pp.254-264
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• 1987

This study was attempted to investigate the effect of Ganoderma lucidum (Young-Jii) extract on the activities of GPT GOT Al. P LDH and the level of total bilirubin and total cholesterol in serum of $CCl_4$-intoxicated rats, and on the level of total lipids triglyceride phospholipids and total cholesterol in the serum of experimentally induced hyperlipemic rats, and on the effect of body and liver weight in rats. The results were shown as follows; In $CCl_4$-intoxicated rats, the extract showed a significant decrease in the activities of GPT and Al.P, a slight decrease in the activity of GOT and LDH; The level of total bilirubin was slightly affected, but significantly decreased at a dose as high as 500 mg/kg; the level of total cholesterol was increased dose dependently. In hyperlipemic rats, the extract caused a significant decrease in the level of total lipids and triglyceride and the rate of decrease was more pronounced with repeated treatments for 10 days; the level of phospholipids and total cholesterol were slightly decreased with repeated treatment of the extract at a dose of 300 mg/kg for 10 days; A significant body weight gain was shown with the treatment of the extract.

• Toxicological Research
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• 제28권3호
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• pp.165-172
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• 2012

Raphanus sativus (Cruciferaceae), commonly known as radish is widely available throughout the world. From antiquity it has been used in folk medicine as a natural drug against many toxicants. The present study was designed to evaluate the hepatoprotective activity of radish (Raphanus sativus) enzyme extract (REE) in vitro and in vivo test. The $IC_{50}$ values of REE in human liver derived HepG2 cells was over 5,000 ${\mu}g/ml$ in tested maximum concentration. The effect of REE to protect tacrine-induced cytotoxicity in HepG2 cells was evaluated by MTT assay. REE showed their hepatoprotective activities on tacrine-induced cytotoxicity and the $EC_{50}$ value was 1,250 ${\mu}g/ml$. Silymarin, an antihepatotoxic agent used as a positive control exhibited 59.7% hepatoprotective activity at 100 ${\mu}g/ml$. Moreover, we tested the effect of REE on carbon tetrachloride ($CCl_4$)-induced liver toxicity in rats. REE at dose of 50 and 100 mg/kg and silymarin at dose of 50 mg/kg were orally administered to $CCl_4$-treated rats. The results showed that REE and silymarin significantly reduced the elevated levels of serum enzyme markers induced by $CCl_4$. The biochemical data were supported by evaluation with liver histopathology. These findings suggest that REE, can significantly diminish hepatic damage by toxic agent such as tacrine or $CCl_4$.

• 한국식품영양과학회지
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• 제40권1호
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• pp.78-83
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• 2011

최근 국내의 건강기능성 추출물을 이용한 차 음료 시장이 확대되고 있고, 국화, 산수유 및 오미자는 이들의 높은 생리 활성과 기호도로 인하여 그 활용도가 더욱 높을 것으로 기대된다. 현재까지 국화, 산수유 및 오미자의 개별적인 생리활성 연구는 활발히 이루어지고 있는 반면, 이들을 혼합하여 제조한 차류의 효능에 대한 연구는 아직 보고되지 않고 있는 실정이다. 따라서 본 연구에서는 $CCl_4$ 처리에 의해 손상된 간세포에 대한 국화차 조성물의 간 기능 보호효과와 인체백혈구에서 $H_2O_2$로 유도된 산화적 DNA 손상에 대한 국화차 조성물의 항유전독성 효과를 검증하고자 하였다. $CCl_4$로 유도된 간세포 독성에 대해 국화차 조성물 I형, II형은 유의적인 간세포 보호효과를 나타내었으며, 국화차 조성물 III형은 $CCl_4$처리군보다 약간 높은 세포생존율을 보였으나 유의적이지는 않았다. $CCl_4$를 처리에 의해 증가한 간세포 배지 내 AST 및 ALT 활성은 국화차 조성물에 의해 배지 내 효소활성을 감소시킴으로 간세포 보호효과가 있는 것으로 사료되며, 그 효과는 AST 효소활성에 더 큰 영향을 미치는 것으로 나타났다. 특히 국화차 조성물 I형의 0.01 mg/mL 농도에서 가장 높은 AST 및 ALT 유리 억제능을 나타내었다. 이 결과로 국화추출물의 $CCl_4$ 유도에 의해 AST>ALT 순으로 유리가 증가되는 것으로 여겨진다. 국화차 조성물 I형의 $1\sim50{\mu}g$/mL, 국화차 조성물 II의 $50{\mu}g$/mL 및 국화차 조성물 III 의 $1\sim50{\mu}g$/mL 농도 범위에서 산화적 스트레스로 유도된 인체 백혈구 DNA 손상에 대한 보호효과를 나타내었다. 이러한 결과를 통하여 국화차 조성물의 간세포 손상보호효과와 산화적 스트레스에 대한 인체 백혈구 DNA 손상 보호능을 검증할 수 있었다.

• 생약학회지
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• 제26권4호
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• pp.390-410
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• 1995

This study was attempted to investigate the effects of Composite Preparation (Samulchungkan-Tang) extract (SCTE), Scutellarias Radix extract (SRE), Artemisiae iwayomogii Herba extract (AIHE), Artemisia capillaris Flos extract (ACFE), Paeaniae Radix extract (PRE) and Gardeniae Fructus extract (GFE) on the activities of GOT, GPT, ALP and LDH, and Content of total cholesterol in serum of $CCl_4$ and ${_D}-galactosamime$ intoxicated rats, and bile flow in rats. 1) In $CCl_4-intoxicated$ rats-The activities of S-GOT and S-GPT which were elevated by $CCl_4$ were significantly decreased in dose of SCTE 450 mg/kg, ACFE 600 mg/kg and GFE 300 mg/kg, respectively as compared to $CCl_4$ intoxicated rats. ALP activity increased by $CC1_4-treatment$ was markedly decreased in dose of SCTE 450 mg and 600 mg/kg, SRE 400 mg/kg, AIHE 400 mg/kg, ACFE 600 mg/kg and PRE 300 mg/kg, and LDH activity in SCTE 450 mg and 600 mg/kg, ACFE 600 mg/kg and GFE 300 mg/kg, respectively compared to $CCl_4$ treated rates. ACFE 400 mg/kg and PRE 300 mg/kg decreased the content of total cholesterol increased by $CCl_4$, the liver weight in all sample administered groups was decreased significantly as compared to $CCl_4$ treated groups. 2) In ${_D}-galactosamine$ intoxicated rats-Sample of SCTE 450 mg and 600 mg/kg, SRE 400 mg/kg, AIHF 400 mg and 600 mg/kg, ACFE 600 mg/kg, PRE 300 mg/kg and GFE 300 mg and 500 mg/kg decreased the activities of S-GPT, ALP and LDH which was increased by ${_D}-galactosamine$ intoxication, compared to ${_D}-galactosamine$ intoxicated groups. In S-GOT activity elevated by ${_D}-galactosamine$ was significantly decreased by SCTE 450 mg/kg, ACFE 600mg/kg, AIHE 600 mg/kg, PRE 300 mg/kg, GFE 300 mg and 500 mg/kg. However, SCTE 600 mg/kg, SRE 400 mg/kg, and AIHE 400 mg/kg were not effected significantly. 3) In bile secretion-SCTE 450 mg and 600 mg/kg, ACFE 600 mg/kg and GFE 500mg/kg increased significantly the amount of bile secretion as compared to normal groups, but AIHE 400 mg/kg, SRE 400 mg/kg, and PRE 300 mg/kg did not effected significantiy.

• 한국식품영양과학회지
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• 제22권4호
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• pp.412-417
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• 1993

녹각이 동양의학에서 보혈강장제라는 사실에 근거하여 생체내 물질대사에 중요한 역할을 하는 간장의 장해시 효소활성 변동에 미치는 녹각의 효능을 구명할 목적의 일환으로 간독성 물질인 benzo(a)pyrene으로 간장해를 유도한 후 각각의 녹각추출물을 급여함으로써 간해독 과정에 관여하는 효소의 활성을 생화학적 측면에서 비교하였다. 각각의 녹각추출물 급여로 인한 체중증가량, 식이섭취량 및 식이효율은 녹각추출물 군간의 유의성은 나타나지 않았으나, Control군에 비하여 유의적인 증가를 보였고 B(a)P 투여군에서도 Cont-B군에 비하여 녹각추출물 급여군에서 유의적인 증가를 나타내었다. 체중 100g당 장기무게는 간장의 경우 benzo (a)pyrene 투여로 증가하는 경향을 보였으나 비장과 신장 및 심장에는 별다른 차이가 없었다. 녹각추출물 급여로 4주간 사육한 흰쥐에서 간해독계 효소중 cytochrome P-450의 함량은 Control 군에 비하여 ben-zo(a)pyrene 투여로 유의적인 감소를 보였으며, 녹각추출물과 benzo(a)pyrene을 병행 투여한 실험군 중 Water-B군이 정상군에 가깝게 증가되었다. 간조직 중의 glutathione함량은 Water군과 Neutral군에서 증가를 보였으나 benzo(a)pyrene 투여로 감소하였다. 또한 간조직 중의 glutathione peroxidase 활성은 녹각추출물 급여에 따른 영향은 없었으며, benzo(a)pyrene 투여로 감소된 활성이 water-B군에서 정상군에 가까운 증가를 나타내었다. 간조직 중의 과산화지질 함량은 Water-B군에서 그 감소 정도가 가장 현저하였다. 이상의 결과를 종합해 볼 때 녹각추출물 중의 water-ext.와 neutral-ext.에 함유되어 있는 유효성분이 간장의 해독기구 효소활성을 유도하고, benzo(a)pyrene의 대사를 촉진시키므로 간손상을 억제할 수 있을 것으로 생각된다.