• Archives of Pharmacal Research
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• 제28권1호
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• pp.44-48
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• 2005

Phytochemical investigation of the MeOH extract of the root barks of Cudrania tricuspidata Bureau (Moraceae), as guided by hepatoprotective activity in vitro, furnished four isoprenylated xanthones, cudratricusxanthone A (1), cudraxanthone L (2), cudratricusxanthone E (3), and macluraxanthone B (4). All of these compounds showed the significant hepatoprotective effect on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells. Compounds 1, 2, and 4 also exhibited the significant hepatoprotective effect on nitrofurantoin-induced cytotoxicity in human liver-derived Hep G2 cells.

• 한국약용작물학회지
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• 제27권3호
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• pp.208-217
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• 2019

Background: In the present study, we identified two cytotoxic compounds from the root of Rumex crispus L. using a bioassay-based method. Methods and Results: Compared with the other fractions, the diethyl ether ($Et_2O$) fraction of R. crispus root extract exhibited the strongest of 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging effect [scavenging concentration 50% $(SC_{50})=63.8{\pm}1.47{\mu}g/m{\ell}$], nitric oxide (NO) production inhibitory effect on the mouse macrophage cell line RAW264.7 [inhibitory concentration 50% $(IC_{50})=60.9{\pm}7.52{\mu}g/m{\ell}$] and cytotoxicity effect on the human hepatoma cell line, HepG2 [lethal concentration 50% $(LC_{50})=115.4{\pm}1.86{\mu}g/m{\ell}$]. According to the bioassay-based method, two cytotoxic compounds were purified from the $Et_2O$ fraction by using column chromatography and preparative high performance liquid chromatography (prep-HPLC). These two compounds were identified as parietin and chrysophanol by using nuclear magnetic resonance (NMR) and liquid chromatography quadruple time of flight mass spectrometry (LC-QTOF-MS). In addition, both parietin and chrysophanol exhibited a cytotoxicity effect on HepG2 cells, their $LC_{50}$ values were $169.1{\pm}17.67{\mu}M$ and $111.5{\pm}6.62{\mu}M$, respectively. Conclusions: Parietin and chrysophanol isolated from the $Et_2O$ fraction of the R. crispus root extract showed cytotoxicity in HepG2 cell.

• Mycobiology
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• 제29권3호
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• pp.170-172
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• 2001

The methanolic extract of fruiting body of Paecilomyces tenuipes DGUM 32001 showed significant cytotoxicity against human cancer cells: HepG2 and MCF-7. The methanolic extract was further fractionated with organic solvents such as chloroform and ethyl acetate in that order. Among the fractions tested, the ethyl acetate fraction showed the highest cytotoxicity against the carcinoma tested. The $IC_{50}$ values of ethyl acetate fraction against HepG and MCF-7 were 40 and 9.6 ${\mu}g/ml$, respectively.

• 한국식품과학회지
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• 제46권3호
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• pp.384-389
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• 2014

본 연구에서는 인간 간암세포주 HepG2세포에서 $H_2O_2$로 인해 유도된 산화적 스트레스에 대한 방사선 돌연변이 블랙베리 ${\gamma}$-B201 추출물의 세포보호 효능에 대하여 알아보고자 하였다. ${\gamma}$-B201 추출물 처리 시 $H_2O_2$로 처리된 HepG2 세포에서 ROS 생성이 억제되었으며, 세포 생존율을 증가시키고 LDH의 방출을 억제함을 확인하였다. Comet assay를 통해 DNA 손상 정도를 분석한 결과, $H_2O_2$로 인해 유도된 산화적 스트레스에 의한 DNA 손상은 ${\gamma}$-B201 추출물의 처리에 의해 감소하였다. 또한, HepG2 세포에 $H_2O_2$ 처리에 의해 저하된 항산화 효소인 SOD와 CAT의 활성을 ${\gamma}$-B201 추출물에 의해 증가시킴으로써 $H_2O_2$로 인해 유도된 산화적 스트레스로부터 HepG2 간세포를 보호하는 것으로 판단되며, ${\gamma}$-B201 추출물이 간 손상 보호 및 간 기능 개선 효과를 갖는 기능성 소재로서 활용될 수 있는 것으로 사료된다.

• Biomolecules & Therapeutics
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• 제13권2호
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• pp.113-117
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• 2005

Organosulfur compounds have been shown to exert an anti-cancer activity. In an attempt to develop novel chemopreventive and anti-cancer agents for liver cancer, we synthesized allylthiopyridazine derivatives. We have previously shown that allylthiopyridazine derivatives exert inhibitory effects on proliferation, invasion and migration of SK-Hep-1 hepatocarcinoma cells in vitro. The in vivo anti-tumor effect of 3-methvl-6-allylthiopy-ridazine, named as K6, was also reported. In this study, we further investigated the preclinical anti-cancer efficacy of K6 for hepatocarcinoma using nude mice xenografted with Hep-G2 hepatocellular carcinoma cells. K6(20-100 mg/kg, orally administered everyday for 30 days) markedly decreased the tumor volume of Hep-G2 cell-transplanted nude mice as evidenced by ultrasonographic and plethysmogranhic analyses. The inhibitory effect on tumor volume was lower than that exerted by doxorubicin (2 mg/kg), intravenously injected) which was used as a positive control. This study shows that K6 efficiently suppresses xenograft tumor growth, revealing K6 as apotential anti-cancer agent for suppressing in vivo progression of liver cancer. Given that hepatocarcinoma is among the most prevalent and lethal malignancies and there is no effective treatment to date, our study may contribute to the potential drug development for liver cancer.

• 동의생리병리학회지
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• 제24권2호
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• pp.284-289
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• 2010

The purpose of this study is to investigate the effect of water extract from Artemisiae Argi Folium Fermented with Sacchromyces cerevisiae (AFS) on viability of human hepatocyte HepG2 cells treated with hepatotoxicants such as EtOH, gallic acid, nicotine, acetaminophen, acetaldehyde, and lipopolysaccharide. AFS (0~400 ug/mL) was treated with EtOH, gallic acid, nicotine, acetaminophen, acetaldehyde, and lipopolysaccharide. And the viability of HepG2 cells was measured by MTT assay. AFS showed to increase significantly viabilities of HepG2 cells compared with hepatotoxicants (EtOH, gallic acid, nicotine, acetaminophen, and lipopolysaccharide) only (p<0.05). AFS could be supposed to have the hepatoprotective effect against hepatotoxicants such as gallic acid, EtOH, nicotine, acetaminophen, and lipopolysaccharide.

• Archives of Pharmacal Research
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• 제28권10호
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• pp.1183-1189
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• 2005

Although plant-derived phenolic acids have been reported to have anti-cancer activity, the exact mechanism is not completely understood. In this study, we investigated the role for reactive oxygen species (ROS) as a mediator of the apoptosis induced by caffeic acid (CA) and ferulic acid (FA), common phenolic acids in plants in HepG2 human hepatoma cells. CA and FA reduced cell viability, and induced apoptotic cell death in a dose-dependent manner. In addition, they evoked a dose-related elevation of intracellular ROS. Treatment with various inhibitors of NADPH oxidase (diphenylene iodonium, apocynin, neopterine) significantly blunted both the generation of ROS and the induction of apoptosis induced CA and FA. These results suggest that ROS generated through activation of NADPH oxidase may play an essential role in the apoptosis induced by CA and FA in HepG2 cells. These results further suggest that CA and FA may be valuable for the therapeutic management of human hepatomas.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2003년도 추계학술대회
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• pp.146-146
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• 2003

20-O-(${\beta}$-D-Glucopyranosyl)-20(S)-protopanaxadiol (IH901), an intestinal bacterial metabolite of ginseng saponins formed from ginsenosides Rb1, Rb2 and Rc, is suggested to be a potential chemopreventive agent. Here we show that IH901 induces apoptosis in human hepatoblastoma HepG2 cells.(omitted)

• 한국식품영양학회지
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• 제27권6호
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• pp.1090-1095
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• 2014

Anthocyanins, a class of flavonoids, are natural water-soluble pigments, which are mainly found in vegetables and fruits. Anthocyanins have attractive pharmacological activities, such as anti-oxidant, anti-inflammatory, anti-cancer, and anti-diabetic. The purpose of this study was to investigate the protective effects of anthocyanins-rich fraction (ANF) from Korean purple sweet potato variety, "Shinjami", against hydrogen peroxide ($H_2O_2$)-induced oxidative stress. In our results, pre-treatment of HepG2 cells with ANF ($10{\mu}g/mL$) significantly prevented cell death and maintained cell integrity, following exposure to 0.9 mM hydrogen peroxide. The $H_2O_2$-dependent production of intracellular ROS was also significantly decreased by pre-treatment with ANF (6 h, $10{\mu}g/mL$). In addition, ANF increased the mRNA levels of antioxidant enzymes, catalase and glutathione level in $H_2O_2$-treated HepG2 cells. These results indicated that ANF protected HepG2 cells against $H_2O_2$-induced oxidative stress by inducing protective system.

• Preventive Nutrition and Food Science
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• 제9권2호
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• pp.150-155
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• 2004

The free radical scavenging activities and the protective effects of Rhus javanica extracts against oxidative damage induced by reactive oxygen species (ROS) were investigated. n-Hexane, ethyl acetate and water fractions were prepared from a methanol extract. DPPH radical, superoxide anion and hydroxyl radical scavenging activities were estimated. Intracellular ROS formation was quantified using fluorescent probes, 2', 7'-dichlorofluorescin diacetate (DCFH-DA) for hydroxyl radical and dihydroethidium (DHE) for superoxide anion. The oxidative DNA damage was investigated by the comet assay in HepG$_2$ cells exposed either to $H_2O$$_2$ or to menadione. The highest $IC_{50}$/ values for DPPH radical scavenging activity was found in the ethyl acetate fraction with a value of 5.38 $\mu\textrm{g}$/mL. Cells pretreated with $\geq$ 1 $\mu\textrm{g}$/mL of the ethyl acetate extract had significantly increased cell viability compared to control cells, which were not pretreated with the extract. Intracellular ROS formation and DNA damage in HepG$_2$ cells, which were pretreated with the various concentrations of Rhus javanica ethyl acetate extract and then incubated either with $H_2O$$_2$ or with menadione, reduced in a dose-dependent manner. These findings suggest that Rhus javanica might have biologically active components which have strong protective effects against ROS induced oxidative damages to the biomolecules, such as cell membranes and DNA.