• Parasites, Hosts and Diseases
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• v.54 no.4
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• pp.415-421
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• 2016

The drug-resistance of malaria parasites is the main problem in the disease control. The huge Brazilian biodiversity promotes the search for new compounds, where the animal kingdom is proving to be a promising source of bioactive compounds. The main objective of this study was to evaluate the antiplasmodial and cytotoxic activity of the compounds obtained from the toad venoms of Brazilian Amazon. Toad venoms were collected from the secretion of Rhinella marina and Rhaebo guttatus in Mato Grosso State, Brazil. The powder was extracted at room temperature, yielding 2 extracts (RG and RM) and a substance ('1') identified as a bufadienolide, named telocinobufagin. Growth inhibition, intraerythrocytic development, and parasite morphology were evaluated in culture by microscopic observations of Giemsa-stained thin blood films. Cytotoxicity was determined against HepG2 and BGM cells by MTT and neutral red assays. The 2 extracts and the pure substance ('1') tested were active against chloroquine-resistant Plasmodium falciparum strain, demonstrating lower $IC_{50}$ values. In cytotoxic tests, the 2 extracts and substance '1' showed pronounced lethal effects on chloroquine-resistant P. faciparum strain and low cytotoxic effect, highlighting toad parotoid gland secretions as a promising source of novel lead antiplasmodial compounds.

• Molecular & Cellular Toxicology
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• v.5 no.4
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• pp.310-316
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• 2009

Some environmental chemicals have been shown to cause liver-toxicity as the result of bioaccumulation. Particularly, fungicides have been shown to cause varying degrees of hepatictoxicity and to disrupt steroid hormone homeostasis in in vivo models. The principal objective of this study was to evaluate the liver-toxic responses of environmental chemicals-in this case selected fungicides and parasiticides-in order to determine whether or not this agent differentially affected its toxicogenomic activities in hepatic tumor cell lines. To determine the gene expression profiles of 3 fungicides (triadimefon, myclobutanil, vinclozolin) and 1 parasiticide (dibutyl phthalate), we utilized a modified HazChem human array V2. Additionally, in order to observe the differential alterations in its time-dependent activities, we conducted two time (3 hr, 48 hr) exposures to the respective IC20 values of four chemicals. As a result, we analyzed the expression profiles of a total of 1638 genes, and we identified 70 positive significant genes and 144 negative significant genes using four fungicidic and parasiticidic chemicals, using SAM (Significant Analysis of Microarray) methods (q-value<0.5%). These genes were analyzed and identified as being related to apoptosis, stress responses, germ cell development, cofactor metabolism, and lipid metabolism in GO functions and pathways. Additionally, we found 120 genes among those time-dependently differentially expressed genes, using 1-way ANOVA (P-value<0.05). These genes were related to protein metabolism, stress responses, and positive regulation of apoptosis. These data support the conclusion that the four tested chemicals have common toxicogenomic effects and evidence respectively differential expression profiles according to exposure time.

• The Korean Journal of Food And Nutrition
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• v.22 no.3
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• pp.456-462
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• 2009

Adlay, barley and rice bran were extracted using various concentrations of methanol(10% and 80%) and chloroform : methanol(2 : 1) to examine the biological activities of these raw grains. Extraction with 80% methanol resulted in high Vitamin C Equivalent Antioxidant Capacity(VCEAC), in the order of barley > rice bran > adlay, as determined by DPPH and ABTS assays. In addition, the extracts of adlay and rice bran showed high cellular antioxidant activity in HepG2 cells possibly due to the presence of polyphenol glycosides in these grains. We examined the expression of glucose/fatty acid metabolizing genes in differentiated 3T3-L1 adipocyte cells. Glut1 was downregulated after treatment with rice bran and no changes in the expression of Glut4 was observed. In contrast, genes involved in fatty acid metabolism, CD36 and aP2, were upregulated. Since these physiological changes were matched with peroxisome proliferator activating receptor $\gamma$(PPAR $\gamma$) agonism, we suggest that the extracts from adlay, barley and rice bran may play preventive roles against aging and diabetes via antioxidant activity and increased uptake of fatty acids by adipocytes.

• The Korean Journal of Food And Nutrition
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• v.30 no.3
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• pp.454-463
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• 2017

Ganoderma lucidum has been traditionally used as a medicine for treatment of bronchitis, arthritis, and high blood pressure, and it has been reported to display many biological activities including anticancer and immune activities. Since mushroom mycelium is known to have excellent biological activities together with mushroom fruiting body, studies on biological activities of mushroom mycelium have been actively conducted. Thus, the present study compared the biological activities before and after the cultivation of Ganoderma lucidum mycelium on Atractylodes rhizoma. When the radical scavenging activity was assessed by the DPPH assay, ARGL (ethanol extract of Atractylodes rhizoma mycelium fermented with Ganoderma lucidum) showed radical scavenging activity of 5.58~82.56% at concentrations of $10{\sim}500{\mu}g/assay$, while AR (ethanol extract of Atractylodes rhizoma) showed radical scavenging activity of 5.27~72.08% at the same concentrations. When measured by using the ABTS assay, ARGL showed higher radical scavenging activity than AR, which was consistent with the result obtained by the DPPH assay. In the MTT assay, the cytotoxicity of ARGL against all cell lines was higher than that of AR. In particular, the cytotoxicities of AR and ARGL against Hep3B at a concentration of $400{\mu}g/assay$ were 71.81% and 86.40%, respectively. In addition, the result obtained by the SRB assay was consistent with the result obtained by the MTT assay. According to the results mentioned above, there is a high probability that medicinal herb cultures using mycelium can be used as sources of functional foods since the cytotoxicities against cancer cells and antioxidant activities increased when the mycelium was fermented with Atractylodes rhizoma.

• Bulletin of the Korean Chemical Society
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• v.35 no.8
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• pp.2335-2341
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• 2014

Chemical investigation on the methanol extract of the starfish Ctenodiscus crispatus resulted in the isolation of five steroids, (22E,$24{\zeta}$)-26,27-bisnor-24-methyl-$5{\alpha}$-cholest-22-en-$3{\beta}$,5,$6{\beta}$,$15{\alpha}$,25-pentol 25-O-sulfate (1), (22E,24R,25R)-24-methyl-$5{\alpha}$-cholest-22-en-$3{\beta}$,5,$6{\beta}$,$15{\alpha}$,25,26-hexol 26-O-sulfate (2), (28R)-24-ethyl-$5{\alpha}$-cholesta-$3{\beta}$,5,$6{\beta}$,8,$15{\alpha}$,28,29-heptaol-24-sulfate (3), (25S)-$5{\alpha}$-cholestane-$3{\beta}$,5,$6{\beta}$,$15{\alpha}$,$16{\beta}$,26-hexaol (4), and ${\Delta}7$-sitosterol (5). Their structures were identified by extensive spectroscopic analyses, including 1D, 2D NMR and MS and chemical methods. Compound 4 showed cytotoxicity against human hepatoma HepG2 and glioblastoma U87MG cells via inhibition of cell growth and induction of apoptosis. Induction of apoptosis by 4 was demonstrated by cell death, DNA fragmentation, increased Bax/Bcl-2 protein ratio and the activation of caspase-3, caspase-9 and poly (ADP-ribose) polymerase (PARP).

• Archives of Pharmacal Research
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• v.25 no.3
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• pp.293-299
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• 2002

Cytotoxic and antimutagenic effects of a novel cis-$\varepsilon$-viniferin and five known stilbenes, transresveratrol, trans-$\varepsilon$-viniferin, gnetin H, suffruticosols A and B, isolated from the seeds of Paeonia lactiflora Pall. (Paeoniaceae) were determined against five different cancer cell lines, and mutagenicity of N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) in Salmonella typhimurium TA100, respectively. Six stilbenes showed cytotoxic activity in a dose-dependent manner, and especially did potent cytotoxic activity against C6 (mouse glioma) cancer cell with $IC_{50}$ values ranging from 8.2 to $20.5{\;}{\mu\textrm{g}}/ml$. trans-Resveratrol showed significant cytotoxic activity against HepG2 (liver hepatoma) and HT-29 (colon) human cancer cell lines with $IC_{50}$ values of 11.8 and 25.2 g/ml, respectively. In contrast, trans-$\varepsilon$-viniferin and cis--viniferin, and gnetin H exhibited marked cytotoxic activity against Hela (cervicse) and MCF-7 (breast) human cancer cell lines with $IC_{50}$ values of 20.4, 21.5, and $12.9{\;}{\mu\textrm{g}}/ml$, respectively. However, suffruticosol A and B had less cytotoxic effect against all cancer cells except C6. Meanwhile, six stilbenes exerted antimutagenic activity in a dose-dependent fashion. Of them, trans-resveratrol exhibited the strongest antimutagenic effect against MNNG with $IC_{50}$ value of $27.0{\;}{\mu\textrm{g}}/plate$, while other five resveratrol oligomers also did moderate antimutagenic activity with $IC_{50}$ values ranging from 31.7 to $35.2{\;}{\mu\textrm{g}}/plate$.

• Journal of Ginseng Research
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• v.42 no.1
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• pp.16-20
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• 2018

Background: The Panax ginseng plant is used as an herbal medicine. Phytosterols of P. ginseng have inhibitory effects on inflammation-related factors in HepG2 cells. Methods: Phytosterols (e.g., stigmasterol and ${\beta}$-sitosterol) in the roots of P. ginseng grown under various conditions were analyzed using high-performance liquid chromatography. The P. ginseng roots analyzed in this study were collected from three cultivation areas in Korea (i.e., Geumsan, Yeongju, and Jinan) and differed by cultivation year (i.e., 4 years, 5 years, and 6 years) and production process (i.e., straight ginseng, red ginseng, and white ginseng). Results: The concentrations of stigmasterol and ${\beta}$-sitosterol in P. ginseng roots were 2.22-23.04 mg/g and 7.35-59.09 mg/g, respectively. The highest concentrations of stigmasterol and ${\beta}$-sitosterol were in the roots of 6-year-old P. ginseng cultivated in Jinan (82.14 mg/g and 53.23 mg/g, respectively). Conclusion: Six-year-old white ginseng and white ginseng cultivated in Jinan containing stigmasterol and b-sitosterol are potentially a new source of income in agriculture.

• Journal of Plant Biology
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• v.38 no.2
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• pp.173-180
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• 1995

We investigated levels and distribution of genetic variation in Korean populations of Calystegia soldanella and C. japonica, clonally reproducing herbaceous perennials. Calystegia soldanella is one ofecologically important beach plants growing only on sand and beach dunes in Europe, East Asia, the Pacific Islands, and the west coast of North America. In contrast, C. japonica usually grows on small mounds of paddy fields, roadsides, and waste places with patchy distribution. Starch gel electrophoresis was conducted on leaves collected from 13 populations of C. soldanella and eight populations of C. japonica. The levels of genetic variation of the two species are very comparable; means of expected heterozygosity (Hep) were 0.100 and 0.099 for C. soldanella and C. japonica, respectively. These values were also very similar to those for species with similar life-history and ecological traits. However, the proportion of total genetic diversity partitioned among populations (GST) of C. soldanella (0.146) was considerably lower than that of C. japonica (0.383). In addition, means of Nei's genetic identity (Ⅰ) for C. soldanella and C. japonica were 0.985 and 0.900, respectively, which supports a restricted gene flow resulting from obligate clonal reproduction of C. japonica. Significant differences in allele frequency were detected among populations at eight and nine of nine polymorphic loci for C. soldanella and C. japonica (P<0.01), respecitvely. Considering the ecological importance of C. soldanella, the isolated beach populations coupled with present destruction of natural habitats of the species may result in erosion of genetic diversity in the near future. In this respect, conservation efforts should be focused on those populations that currently maintain the most genetic diversity such as those populations in the eastern and southeastern Korean Peninsula and Hamduck Beach, Cheju Island.

• Journal of Physiology & Pathology in Korean Medicine
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• v.31 no.3
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• pp.159-166
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• 2017

Through this study, the authors investigated the anti-steatosis effects of the Amomum cardamomum ethyl acetate fraction in free fatty acids (FFAs)-induced human hepatocellular carcinoma HepG2 cells. The ethyl acetate fraction of Amomum cardamomum (ACEA) was extracted with 70% ethanol and then the extract was evaporated using a rotary evaporator prior to sequential fractionation. Human hepatocellular carcinoma were treated with different concentrations of ACEA in the presence and absence of FFAs. To demonstrate the reactive oxygen species (ROS) scavenging activity, DCFDA level was analyzed by using in vitro assay system. Cell viability, lipid accumulation, intracellular triglycerides, malondialdehyde (MDA), liver steatosis related signaling molecules and inflammatory cytokines such as interleukin (IL)-6, 8, tumor necrosis factor-alpha ($TNF-{\alpha}$) were also investigated. As results, ACEA inhibited the FFAs-induced ROS, lipid accumulation, intracellular triglycerides, and MDA in a dose dependent manner. Treatment of human hepatocellular cells with ACEA induced the phosphorylation of 5' adenosine monophosphate-activated protein kinase (AMPK) and carnitine palmitoyltransferase I (CPT1) expression using western blot analysis. ACEA also potently suppressed the FFAs-induced inflammatory cytokines including IL-6, IL-8 and $TNF-{\alpha}$. These results suggest that the ethyl acetate fraction of Amomum cardamoum extract own inhibitory effects of liver steatosis by inhibiting ROS, lipid accumulation, intracellular triglycerides, MDA through AMPK signaling and anti-inflammatory actions.

• The Korean Journal of Food And Nutrition
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• v.26 no.4
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• pp.609-614
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• 2013

This study was carried out in order to investigate the functional properties of methanol extracts from two parts (root and fruit) of Xanthium strumarium by means of measuring the contents of total polyphenols and flavonoid as well as determining $ABTS{\cdot}^+$, DPPH radical scavenging activity, hydroxyl radical scavenging activity (OH${\cdot}$) and anticancer activity. The examination of physiologically active substances in the two parts revealed that the Xanthium strumarium fruit had high total polyphenol, flavonoid contents, $ABTS{\cdot}^+$ DPPH and hydroxyl radical scavenging activity. The Xanthium strumarium fruit has higher activities of anticancer activities on prostate cell lines compared to other cancer cell lines.