• YAKHAK HOEJI
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• v.42 no.2
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• pp.144-148
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• 1998

One hundred and seventeen crude drugs were screened for DNA-binding activity in vitro. The DNA-methyl green assay is a useful biochemical screen for the detection or development of biologically active compounds which bind to DNA. This assay is based upon the fact that free methyl green undergoes rapid spontaneous molecular rearrangement to its colorless carbinol base so that the liberation of the dye from DNA by displacement can be followed spectrophotometrically as a decrease in absorbance at 65Onm. Seven methanolic extracts of crude drugs including Cinnamomi Cortex spissus, Coicis Semen, Coptidis Rhizoma, Perillae Semen, Plantaginis Semen, Polygalae Radix and Zanthoxyli Fructus showed less than 2,000${\mu}$g/ml as their $IC_{50}$ values. The active principles of Plantaginis Semen and Zanthoxyli Fructus were transferred into organic solvents, which showed the $IC_{50}$ values with 588 and 574${\mu}$g/ml, respectively. These fractions have been selected for isolation of biologically active constituents.

• Archives of Pharmacal Research
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• v.20 no.2
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• pp.155-157
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• 1997

An attempt to estabilish the relationship between anti-cell adhesive action of phenylacetylshikonin analogues and their cytotoxicity against A549 cells was done. In the one hour incubation with A549 cells,${\alpha}$-methoxyphenylacetyl-(9), ${\alpha}$-acetoxyphenylacetyl-(13), 3,4-methylenedioxyphenylacetyl-(15) and 4-(N,N-dimethylamino)-phenylacetylshikonin (17) analogues showed a high anti-cell adhesive activity $(IC_100; value, 4-8{\mu}g/ml)$, while halophenylacetyl- and dimethoxy- or trimethoxyphenylacetyl analogues expressed no activity at $40{\mu}g/ml$, indicating that the presence of a bulky group at $ C^I-{\alpha}$ and a polar group at C-4 of phenylacetyl moiety may be important. A similar structure activity relationship exists for the 48 hr cytotoxocity $(ED_{50})$ of phenylacetylshikonin analogues in A 549 cells, but not in either K562 or L1210 cells. Furthermore, the difference between $IC_{100}$ values for anti-cell adhesive activity and$ED_{50}$ values for cytotoxicity of potent compound in A549 cells was not so great (1.5 to 3 times). Based on these observations, it is proposed that the anti-cell adhesive action of phenylacetylshikonins might be responsible for their cytotoxicity in A549 cells.

• BMB Reports
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• v.35 no.2
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• pp.239-243
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• 2002

Angiotensin I that converts the enzyme (ACE) inhibitory peptide, Gly-Pro-Leu, previously purified and identified from the Alaskan pollack skin gelatin hydrolysate, were synthesized. In addition, the peptides Gly-Leu-Pro, Leu-Gly-Pro, Leu-Pro-Gly, Pro-Gly-Leu, Pro-Leu-Gly, Gly-Pro, and Pro-Leu, which consisted of glycine, proline, and leucine, were synthesized by the solid-phase method. The $IC_{50}$ values of each tripeptide - namely Leu-Gly-Pro, Gly-Leu-Pro, Gly-Pro-Leu, Pro-Leu-Gly, Leu-Pro-Gly, and Pro-Gly-Leu - were 0.72, 1.62, 2.65, 4.74, 5.73, and $13.93{\mu}M$, respectively. The ACE inhibitory activity of these tripeptides was higher than that of dipeptides, such as Gly-Pro and Pro-Leu with $IC_{50}$ values of 252.6 and $337.3\;{\mu}M$, respectively. Among the tripeptides, Leu-Gly-Pro and Gly-Leu-Pro had higher inhibitory activity than Gly-Pro-Leu that was isolated from the Alaskan pollack skin gelatin hydrolysate. Among the different types of tripeptides that were examined, the highest ACE inhibitory activity was observed for Leu-Gly-Pro. It had the leucine residue at the N-terminal and proline residue at the C-terminal.

• YAKHAK HOEJI
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• v.52 no.6
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• pp.441-445
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• 2008

To investigate effect of caffeic acid on the intracellular reactive oxygen species production, we used DHE for intracellular superoxide anion production, DCF for intracellular ${H_2}{O_2}$ production and DHR for intracellular hydroperoxide production in Raw 264.7 cells. DPPH assay showed that antioxidant activity of caffeic acid with 39.5 ${\mu}M$ of ${IC}_{50}$ values was similar to that of ascorbic acid with 41.3 ${\mu}M$ of ${IC}_{50}$ values. Caffeic acid dose-dependently inhibited silica-induced ${H_2}{O_2}$ and hydroperoxide production but did not affect superoxide anion production in Raw 264.7 cells, which suggest that antioxidant effect of caffeic acid acts on the post-step of superoxide anion. On the other hand, caffeic acid showed a potent antioxidant effect in $lCuSO_4$-induced lipid peroxidation. Furthermore, plasma superoxide dismutase activity (3.43${\pm}$0.23 U/ml) in 10 mg/kg caffeic acid-fed mice was significantly higher than that (2.32${\pm}$0.24 U/ml) of control. From the above results, it is referred that caffeic acid appears to have potent anti-oxidant activity in both cell system and in vivo system.

• Bulletin of the Korean Chemical Society
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• v.33 no.12
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• pp.4074-4078
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• 2012

The first step in the common pathway for the biosynthesis of branched chain amino acids is catalyzed by acetohydroxyacid synthase (AHAS). The AHAS is found in plants, fungi and bacteria. With an aim to identify new anti-tuberculosis drugs that inhibit branched chain amino acid biosynthesis, we screened a chemical library against Mycobacterium tuberculosis AHAS. The screening identified four compounds, AVS 2087, AVS 2093, AVS 2236, and AVS 2387 with $IC_{50}$ values of 0.28, 0.21, 3.88, and $0.25{\mu}M$, respectively. Moreover, these four compounds also showed strong inhibition against reconstituted AHAS with $IC_{50}$ values of 0.37, 0.26, 1.0, and $1.18{\mu}M$, respectively. The basic scaffold of the AVS group consists of 1-pyrimidin-2-yl-1H-[1,2,4]-triazole-3-sulfonamide. The most active compound, AVS 2387, showed the lowest total interaction energy -8.75 Kcal/mol and illustrates its binding mode by hydrogen bonding with $H_{\varepsilon}$ of Gln517 with the distance of $2.24{\AA}$.

• The Korean Journal of Food And Nutrition
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• v.34 no.5
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• pp.553-559
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• 2021

The aim of study to investigate the phytochemicals and biological activities the bark of Betula schmidtii. The studies consisted of the solvent extraction, followed by the isolation of phenolic components 1~3 from ethyl acetate-soluble fraction of Betula schmidtii Bark. Their chemical structures were identified as arbutin (1), ρ-coumaric acid (2) and ferulic acid (3) using Ultraviolet-Visible (UV-Vis) Spectrophotometer, Electrospray Ionization Mass Spectrometry (ESI-MS) (negative ion mode), ¹H-Nuclear Magnetic Resonance (NMR), ¹³C-NMR, ¹H-¹H Correlation Spectroscopy (COSY) and ¹H-¹³C Hetero Nuclear Multiple Quantum Correlation (HMQC) spectral data. Compounds 1~3 shows the anti-oxidant effect with IC₅₀ values of 29.74±1.52, 21.32±1.07 and 34.41±1.24 in 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity, respectively. Also, compounds 1~3 exhibited mushroom tyrosinase inhibitory activity with IC₅₀ values of 31.14±1.07, 42.54±1.46 and 69.22±1.43 µM, respectively.

• Natural Product Sciences
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• v.25 no.2
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• pp.122-129
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• 2019

The roots of Phlomis umbrosa (Turcz.) (Phlomidis Radix) have been traditionally used to treat cold, reduce swelling and staunch bleeding. Four iridoids (1 - 3 and 5) and six phenylethanoid derivatives (4, and 6 - 10) were isolated from the roots of P. umbrosa. A simple, sensitive, and reliable analytical HPLC/PDA method was developed, validated, and applied to determine 10 marker compounds in Phlomidis Radix. Furthermore, the isolates were evaluated for cytotoxic and anti-oxidant activities as well as DPPH-HPLC method. Among them, compounds 4 and 6 - 9 displayed potent anti-oxidant capacities using DPPH assay with $IC_{50}$ values of $27.7{\pm}2.4$, $10.2{\pm}1.1$, $18.0{\pm}0.8$, $19.1{\pm}0.3$, and $19.9{\pm}0.6{\mu}M$, and compounds 6, 8, and 9 displayed significant cytotoxic activity against HL-60 with $IC_{50}$ values of $35.4{\pm}3.1$, $18.6{\pm}2.0$, and $42.9{\pm}3.0{\mu}M$, respectively.

• Journal of the Korean Society of Food Culture
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• v.25 no.6
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• pp.832-838
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• 2010

In this study, the quality characteristics of jelly with black garlic (0, 10, 20, and 30%) were evaluated. The pH of jelly with black garlic decreased according to the amount of black garlic added. The sugar content of the jelly increased significantly with added black garlic. Lightness, redness, and yellowness decreased with increasing black garlic content. Moreover, the textural properties, which included hardness, springiness, cohesiveness, gumminess, and chewiness decreased in jelly that contained black garlic compared to the controls. Additionally, the antioxidant activity of jelly that contained black garlic increased in a concentration dependent manner. The $IC_{50}$ values of the DPPH radical scavenging activity for jelly that contained 10, 20 and 30% black garlic were 132.47, 50.97, 40.06, and 30.41 mg/mL, respectively. The $IC_{50}$ values of the hydroxyl radical scavenging activity of jelly decreased as the black garlic concentration increased. Finally, sensory results showed that the scores of over-all preference and buying intention for jelly with 20% black garlic were the highest.

• Journal of Mushroom
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• v.12 no.4
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• pp.304-310
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• 2014

The use of mushrooms has immense potential in many diverse applications. Until now, more than 3,000 species are consumed around the world, and more than 100 have shown promising clinical activity against cancer and other chronic diseases. Sparassis latifolia (formerly S. crispa) is an edible mushroom that harbors ${\beta}$-glucan reported to possess immunostimulatory and anticancer properties. However there have been no reports on the anticancer activity of hydrophobic fractions of S. latifolia. In this study, the anticancer activities of S. latifolia extract and hydrophobic fractions were investigated using AGS (stomach cancer), A529 (lung cancer), and HepG2 (liver cancer) cell lines. In cytotoxicity results of A529 cells, fractions of A2, A3, A4, A6, A7, A8, A9, and A10 in all 12 fractions show low $IC_{50}$ values. For HepG2 cells, A7 fraction results in the lowest $IC_{50}$ value while A7, A8, and A11 fractions show low $IC_{50}$ values in AGS cells. S. latifolia extract lead to low cell viability in cancer cells, compared to positive control of paclitaxel. A compound with molecular weight of 181 were detected using HPLC-MS but not identified yet. As a result, the hydrophobic fractions of S. latifolia EtOH extract would be a possible candidate as natural anticancer agents in the future.

• Journal of Life Science
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• v.34 no.6
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• pp.365-376
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• 2024

The present study assessed the cytotoxic effects on cell growth and senescence in human cancer (A-549, AGS, HCT-116, MDA-MB-231, and U 87-MG) and normal (MRC-5 and mesenchymal stem cells) cell lines treated with efavirenz (EFA), an inhibitor of non-nucleoside reverse transcriptase (RTase). Following EFA treatment, the half-maximal inhibitory concentration (IC₅₀) values were approximately 15 µM, and the IC₅₀ value was significantly (p<0.05) lower in the cancer cell lines, compared to normal cell lines. After determining the IC₅₀ values against EFA, each cell line was treated with 15 µM EFA for up to one week. Significant (p<0.05) decreases in endogenous RTase and telomerase activity were observed in the cancer cell lines. RTase and telomerase activity were absent or detected at very low levels in both EFA-untreated and treated MRC-5 and MSC normal cells. The cell doubling time (CDT) was also significantly (p<0.05) prolonged by the decreased cell growth rate in the EFA-treated cancer cell lines compared to the untreated cell lines. Furthermore, EFA-treated cancer cells displayed a high number of cells with a high intensity of senescence-associated ß-galactosidase activity (SA-ß-gal activity), compared to the untreated cells. The present study showed that inhibition of RTase activity induces cellular senescence and arrests cell growth in human cancer cell lines; however, normal cell lines showed greater tolerance against EFA. RTase treatment could offer optional chemotherapy for cancer treatment in human cancer cell lines with high RTase activity.