• Archives of Pharmacal Research
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• v.26 no.8
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• pp.585-590
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• 2003

Activity-guided fractionation of the EtOAc-soluble extract of the whole plants of Sida acuta using a bioassay based on the induction of quinone reductase (OR) in cultured Hepa 1c1c7 mouse hepatoma cells, led to the isolation of ten active compounds of previously known structure, quindolinone (1), cryptolepinone (2), 11-methoxyquindoline (3), N-trans-feruloyltyramine (4), vomifoliol (5), loliolide (6), 4-ketopinoresinol (7), scopoletin (8), evofolin-A (9), and evofolin-B (10), along with five inactive compounds of known structure, ferulic acid, sinapic acid, syringic acid, ($\pm$)-syringaresinol, and vanillic acid. These isolates were identified by physical and spectral data measurement. A new derivative of quindolinone, 5,10-dimethylquindolin-11-one (1a) was synthesized and characterized spectroscopically. Of the active substances, compounds 1-3 and 1a exhibited the most potent QR activity, with observed CD (concentration required to double induction) values ranging from 0.01 to 0.12 $\mu$ g/mL. Six compounds were then evaluated in a mouse mammary organ culture assay, with cryptolepinone (2), N-trans-feruloyltyramine (4), and 5,10-dimethylquindolin-11-one (1a) found to exhibit 83.3, 75.0, and 66.7% inhibition of 7,12-dimethylbenz[a]anthracene-induced preneoplastic lesions, respectively, at a dose of 10 $\mu\textrm{g}$/mL.

• Journal of Life Science
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• v.21 no.6
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• pp.775-782
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• 2011

In this study, the antioxidant activity of methanol extracts and fractions from papaya seed were investigated in vitro. Total polyphenol contents of methanol extracts and fractions from papaya seed varied from 17.74 to 125.99 ${\mu}g/mg$ and total flavonoid contents varied from 1.60 to 32.69 ${\mu}g/mg$. Contents of polyphenol and flavonoid in ethyl acetate (EtOAc) fraction was found to be extremely high (compared with the other fractions examined). Radical-scavenging activities of methanol extracts and fractions were examined using ${\alpha}$,${\alpha}$-diphenyl-${\beta}$-picrylhydrazyl (DPPH) radicals, 2,2'-azino-bis (3-ethyl-benzthiazoline-6-sulfonic acid) (ABTS) and hydrogen peroxide assay. As a result, ethyl acetate fraction of papaya seed showed the highest radical-scavenging activity in various antioxidant systems. The EtOAc fraction from papaya seed induced QR activity in concentrations of 12.5 to 50 ${\mu}g/ml$ with a maximum of a 3.3-fold induction at 50 ${\mu}g/ml$ of fraction. Therefore, the most effective QR inducer among these fractions can be said to reside in the EtOAc fraction, indicating that strong constituents responsible for QR induction potency in the papaya seed extract are largely contained in the EtOAc fraction.

• Journal of Physiology & Pathology in Korean Medicine
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• v.20 no.4
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• pp.951-956
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• 2006

The purpose of this study is to prepare black ginseng and evaluate its antitumor activity. In order to achieve such aim, 5 year fresh ginsenges were steamed at 95'E for 3 hr in pottery apparatus and dried at $60^{\circ}C$ for 12-36 hr. This process was repeated again nine times in same condition. Among the ginseng saponins in black ginseng, the amount of Ginsenoside $Rg_3$ was examined by HPLC. 10.05 mE of Ginsenoside $Rg_3$ was obtained from 1 g of dried black ginseng prepared. The extract of black ginseng exhibited stronger cytotoxic activity against MCF-1, HT-1080 and Hepa 1C1C7 tumor cell lines in vitro than the extract of red ginseng. Also, the extract of black ginseng exhibited stronger antitumor activity(33%) in BDFl mice bearing Lewis lung carcinoma cells(LLC) than the extract of red ginseng(23%). From these results, it was concluded that Black ginseng had antitumor activity suggesting its application for the prevention and treatment of cancer.

• Journal of the Korean Society of Food Science and Nutrition
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• v.26 no.2
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• pp.186-192
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• 1997

Increased activities of phase 2 enzymes including quinone reductase(QR) have been reported to be associated with protection of animals from neoplastic, mutagenic, and other toxic effects of many carcinogens. In previous study, we found that methanol extract of roasted and defatted perilla meal induced the activity of quinone reductase, an anticarcinogenic marker enzyme, in murine hepalc1c7 cells. Current study showed that unroasted perilla had a limited QR-inducing activity, suggesting that roasting cause the generation of active component(s). Thus we hypothesized that QR inducer in perilla might be covalently linked to sugar moiety and released during roasting process. Methanol extract of defatted raw perilla was subject to acid treatment in order to hydrolyze the potential sugar moiety. Prolonged hydrolysis of methanol extract of defatted raw perilla at $98{\sim}100^{\circ}C$ increased the ability to induce cytosolic QR activity of hepalclc7 cells. Furthermore roasting at 180 and $200^{\circ}C$ resulted in significant induction of QR activity. The result strongly support the idea that QR inducer(s) is present in bound form in raw perilla and released during roasting. Cellular QR activity was induced proportionately with the increase of concentration of methanol extract of roasted perilla. The induction of QR by defatted perilla was also examined in the cytosols of liver, small intestine, stomach, lung and kidney of male ICR mice. Induction patterns showed specificity with respect to target tissue and roasting of perilla. Unroasted perilla meal (defatted) significantly induced QR in liver and lung, while roasted perilla meal induced QR in liver and stomach. The observation that raw perilla showed similar QR induction patterns to roasted perilla is consistent with our proposal that QR inducer(s) is present in bound form and released by physical and chemical treatments as digestive or microbial enzymes could release the inducers from inactive glycoside forms in gastrointestinal tract of mice. In conclusion, perilla could exert protective effect against chemically induced carcinogenesis by inducing phase 2 enzymes in biological systems regardless of chemical and physical process such as roasting.