• Proceedings of the Korean Society of Applied Pharmacology
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• 2003.11a
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• pp.85-85
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• 2003

This study has been undertaken to increase availability of native camellia in Jeonnam as a medicinal resource and to isolate the effective components from them. Multidrug resistance(MDR) by tumor cells is a major obstacle to successful cancer chemotherapy. We report that the crude extracts of camellia flowers, leaves has a chemosensitizing effect that can reverse Pgp-mediated MDR by increasing the intracellular accumulation of drugs. The cytotoxic and chemosensitizing effects of MeOH extract from 12 spp. citrus fruits on the AML-2/D100 were determined using MTT assay. Chemosensitizing effects was screened in the presence of vincristine, a good substrate of Pgp. IC$\sub$50/ for extracts in AML-2/WT was found to be 65∼350$\mu\textrm{g}$/$m\ell$ whereas the range of its mean IC$\sub$50/ value in Pgp-overexpressing cells (AML-2/Dl00) in the presence of vincristine was 90∼400$\mu\textrm{g}$/$m\ell$. Of the extracts tested, mature leaf extract displayed the most potent chemosensitizing effect［IC$\sub$50/;100 $\mu\textrm{g}$/$m\ell$, CR;1.06, RF;2.97 in the presence of VCR］. This indicates that the toxicity (IC$\sub$50/;288.89$\mu\textrm{g}$/$m\ell$) of mature leaf extract is minimal at concentrations required for a complete reversal of the drug resistance. Also, this result indicates that crude extracts of camellia mature leaves would contain some principles which have chemosensitizing activity.

• Korean Journal of Pharmacognosy
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• v.31 no.2
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• pp.252-255
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• 2000

In order to screen new radical scavenging principle which is expected to be antiaging drug lead, we have investigated 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity of the marine microalgae, greenalgae(10 speices), diatom (10 speices) and blue-green algae (10 speices). The significant activities$(IC_{50}:\;<100\;{mu}g/ml)$ were observed in 4 species of green algae (MA002, 006, 009, 010), 1 species of diatom (MA015) and 5 species of blue-green algae (MA017, 018, 019, 024, 025). Within the scope of family tested, MA009 $(IC_{50}:\;=78\;{mu}g/ml)$, MA015 $(IC_{50}:\;=38\;{mu}g/ml)$ and MA019 $(IC_{50}:\;=41\;{mu}g/ml)$ displayed the most significant activity. Among the marine microalgae tested at family level, cyanophycean blue-green algae was shown to be the most active family on screening of new bioactive compounds.

• Natural Product Sciences
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• v.19 no.4
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• pp.366-371
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• 2013

Seventeen compounds (1 - 17), ${\beta}$-sitosterone (1), lupenone (2), arborinone (3), ${\beta}$-sitosterol (4), lupeol (5), epi-lupeol (6), taraxerol (7), betulinic acid (8), 24R-methyllophenol (9), germanicol (10), hexatriacontane (11), nonacosan-1-ol (12), benzoic acid (13), tetradecyl(E)-ferulate (14), di(2-ethylhexyl) phthalate (15), trilinolein (16) and monopalmitin (17), were isolated from the methylene chloride-soluble fraction of the cork of Euonymus alatus Sieb. The structures of these compounds were elucidated on the basis of spectroscopic evidence. Compounds 6, 11, 13 and 14 were isolated for the first time from this plant. Compound 4 showed moderate cytotoxic activity with an $IC_{50}$ value of 6.22 ${\mu}M$ in HL-60 cell line. Compound 9 exhibited moderate cytotoxic activity with $IC_{50}$ values of 63.31, 15.45, 15.14 and 21.72 ${\mu}M$ in four kinds of human cancer cell lines, Jurkat T, HeLa, HL-60 and MCF-7, respectively. Compound 17 showed moderate cytotoxic activity with an $IC_{50}$ value of 70.71 ${\mu}M$ in Jurkat T cell line. In addition, compounds 2, 3, 14 and 16 exhibited weak antioxidant activity with $IC_{50}$ values of 151.76, 170.79, 137.46 and 139.37 ${\mu}M$, respectively.

• Korean Journal of Plant Resources
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• v.30 no.5
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• pp.535-541
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• 2017

In this study, methanol (CAMe) and ethanol (CAEt) extract of Theobroma cacao L. were tested to see possibility as natural functional cosmetic agent. Cacao extract and cacao extract loaded gel were evaluated for various properties such as antioxidant, antimicrobial, cell viability, anti-inflammatory. Inhibition of nitric oxide production in lipopolysaccaride (LPS) stimulated raw 264.7cells, at concentration of $0.125{\sim}1{\mu}g/ml$ a dose-dependent manner. Gel formulation (3% extract) were stable for 60day in both extract. In conclusion, gel containing extract of Theobroma cacao L. indicated strong possibility for functional cosmetic ingredient.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.13
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• pp.5371-5376
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• 2015

Berberine (B1), isolated from stems of Coscinium fenestratum (Goetgh.) Colebr, was used as a principle structure to synthesize three phenolic derivatives: berberrubine (B2) with a single phenolic group, berberrubine chloride (B3) as a chloride counter ion derivative, and 2,3,9,10-tetra-hydroxyberberine chloride (B4) with four phenolic groups, to investigate their direct and indirect antioxidant activities. For DPPH assay, compounds B4, B3, and B2 showed good direct antioxidant activity ($IC_{50}$ values=$10.7{\pm}1.76$, $55.2{\pm}2.24$, and $87.4{\pm}6.65{\mu}M$, respectively) whereas the $IC_{50}$ value of berberine was higher than $500{\mu}M$. Moreover, compound B4 exhibited a better DPPH scavenging activity than BHT as a standard antioxidant ($IC_{50}=72.7{\pm}7.22{\mu}M$) due to the ortho position of hydroxyl groups and its capacity to undergo intramolecular hydrogen bonding. For cytotoxicity assay against human fibrosarcoma cells (HT1080) using MTT reagent, the sequence of $IC_{50}$ value at 7-day treatment stated that B1 < B4 < B2 ($0.44{\pm}0.03$, $2.88{\pm}0.23$, and $6.05{\pm}0.64{\mu}M$, respectively). Berberine derivatives, B2 and B4, showed approximately the same level of CAT expression and significant up-regulation of SOD expression in a dose-dependent manner compared to berberine treatment for 7-day exposure using reverse transcription-polymerase chain reaction (RT-PCR) assays. Our findings show a better direct-antioxidant activity of the derivatives containing phenolic groups than berberine in a cell-free system. For cell-based system, berberine was able to exert better cytotoxic activity than its derivatives. Berberine derivatives containing a single and four phenolic groups showed improved up-regulation of SOD gene expression. Cytotoxic action might not be the main effect of berberine derivatives. Other pharmacological targets of these derivatives should be further investigated to confirm the medical benefit of phenolic groups introduced into the berberine molecule.

• The Journal of Korean Medicine
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• v.30 no.4
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• pp.1-12
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• 2009

Objectives: This study was to investigate the anti-oxidation and anti-cancer activity of Chaga mushroom extract. Extraction condition optimization and beta-glucan analysis and anti-cancer activity tests were also done. Methods: Optimum extraction conditions for Chaga mushroom extract were at a temperature of $90^{\circ}C$ and 2hrs with 10 times of water. Extraction yield and economics were best under these conditions. Results: Anti-oxidation activity was the highest with the fraction of 100,000 MWCO and $IC_{50}$ value was $13{\mu}g/ml$ and this value was comparable to that of vitamin E, alpha-tocopherol. Among the fractions from various organic solvents, ethyl acetate fraction showed the highest anti-oxidation activity with $IC_{50}$ value of $7{\mu}g/ml$. For anti-cancer activity, chloroform fraction showed little anti-cancer activity and ethyl acetate fraction showed the best anti-cancer activity with $IC_{50}$ $1.5{\mu}g/ml$ for stomach cancer cells. Anti-cancer activities for different molecular weight fractions were the best in the fraction of molecular weight less than 100,000Da, and $IC_{50}$ values for stomach cancer cells and liver cancer cells were 1.7 and $1.4{\mu}g/ml$, respectively. Conclusions: From these results, we can conclude that the extract of Chaga mushroom could be a good source for functional food and natural anti-cancer medicine.

• Journal of the Korean Society of Food Science and Nutrition
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• v.32 no.7
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• pp.1120-1125
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• 2003

Bioactive properties of low molecular weight peptides purified from anchovy sauce fermented in underground at 15$\pm$3$^{\circ}C$ for 1, 3, and 5 years, respectively, were investigated. The fermented anchovy sauce for 1 year showed 3 peaks on gel permeation chromatography pattern, while 3 and 5 year fermented anchovy sauce showed 4 and 5 peaks, respectively. The longer fermentation period, the lower molecular weight of peptides on gel permeation chromatography pattern. Antioxidative, antitumor, and ACE inhibitory activities of low molecular weight peptides increased as fermentation period increased. Antioxidative and antitumor activities of peptide peak 3 purified from 3 year fermented anchovy sauce were the highest with 34 and 44 $\mu\textrm{g}$/mL of $IC_{50}$/ values, respectively, while ACE inhibitory activity ($IC_{50}$/, 32 $\mu\textrm{g}$/mL) of peak 3 purified from 1 year fermented was the highest.

• Korean Journal of Food Science and Technology
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• v.36 no.6
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• pp.974-978
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• 2004

Brown-alga-derived natural agent NX42, mainly composed of algal polysaccharides and phlorotannins, showed mild but dose-dependent inhibition of acetylcholinesterase with $IC_{50}=600-700\;{\mu}g/mL$. Phlorotannin-rich fraction of NX42 showed substantial increase of the activity by more than one order of magnitude ($IC_{50}=54\;{\mu}g/mL$) and significant protection of SK-N-SH cells from oxidative stress by $H_2O_2$. Learning trials of mice for 5 consecutive days revealed electric-shock treatment during learning period significantly retarded learning process, whereas NX42-treated mice showed significant resistance against leaning deficiency possibly mainly due to anticholinesterase and neuroprotective activities of phlorotannin.

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
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• v.26 no.1
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• pp.53-58
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• 2000

Treatment of oral cancers with chemotherapeutic agents are evaluated as an effective method for remission to reduce cancer proliferation nowadays. But, minimization of side-effects such as bone marrow suppression, gastrointestinal toxicity and renal damage is another problem to be solved. Thus, a possible approach to develop a clinically applicable chemotherapeutic agents is to screen anticancer activity among traditional medicinal plants which have been used for thousands of years with very low side-effects in orient. In this study we focused on screening anti-oral cancer activities among 14 traditional medicinal plant extracts that revealed anticancer activities on other solid tumors. The results were as follow : 1. Methanol extract of Lepidium apetalum showed the highest anti-oral cancer activity against A253 cells. At concentration of $4{\mu}g/ml$, the cell viability was 48% under our experimental condition. $IC_{50}$ value obtained was $4{\mu}g/ml$. 2. Methanol extract of Coptis japonica and Solanum nigrum were effective on KB cells. Cell viability observed were 62% and 67% at concentration of $4{\mu}g/ml$, and $IC_{50}$ values were $12{\mu}g/ml$ and $10{\mu}g/ml$ respectively. 3. When the methanol extract of Lonicera caerule was combined with $2{\mu}g/ml$ of cisplatin, the anticancer activity was synergistically increased. One hundred ${\mu}g/ml$ of Lonicera caerule showed 92%(alone) or 59%(combined with cisplatin) cell viabilities. $IC_{50}$ value of Lonicera caerule extract against KB cells was reduced from $301{\mu}g/ml$ to $126{\mu}g/ml$ when combined with $2{\mu}g/ml$ of cisplatin. 4. Medicinal plant extracts effective on both A253 and KB cells were Coptis japonica, Lepidium apetalum, Solanum nigrum, Caesalpiniae Lignum, Curcuma aromatica.

• Archives of Pharmacal Research
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• v.28 no.5
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• pp.534-540
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• 2005

Activity-guided fractionation of the CH$_2Cl_2$-soluble fraction of the roots of Sophora flavescens furnished five 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scaveng ers: trans-hexadecyl ferulic acid (1) cis-octadecyl ferulic acid (2), trans-hexadecyl sinapic acid (3), (-)-4-hydroxy-3-methoxy-(6aR,11aR)-8, 9-methylenedioxypterocarpan (4) and desmethylanhydroicaritin (8), along with nine known inactive compounds: (-)-maackiain (5), xanthohumol (6), formononetin (7), (2S)-2'-methoxykurarinone (9), (2S)-3${\beta}$,7,4'-trihydroxy-5-methoxy-8-(${\gamma},{\gamma}$- imethylallyl )-flavanone (10), (2S)-7,4'-dihydroxy-5-methoxy-8- (${\gamma},{\gamma}$-dimethylallyl ) -flavanone (11), umbelliferone (12), kuraridin (13), and trifolirhizin (14). Compounds 1-4 and 8 exhibited DPPH free radical scavenging effects at IC$_{50}$ values of 33.01 ${\pm}$ 0.20, 57.06 ${\pm}$ 0.16, 39.84 ${\pm}$ 0.36, 35.83 ${\pm}$ 0.47, and 18.11 ${\pm}$ 0.04${\mu}$M, respectively. L-Ascorbic acid, when used as a positive control, exhibited an IC$_{50}$ value of 7.39 ${\pm}$ 0.01 ${\mu}$M. Compounds 1-4 and 8 also appeared to exert significant scavenging effects on authentic ONOO-, with IC$_{50}$ values of 5.76 ${\pm}$ 1.19, 15.06 ${\pm}$ 1.64, 8.17 ${\pm}$ 4.97, 1.95 ${\pm}$ 0.29 and 4.06 ${\pm}$ 2.41 ${\mu}$M, respectively. Penicillamine (IC$_{50}$= 2.36 ${\pm}$ 0.79${\mu}$M) was used as a positive control. In addition, compounds 2,4,6,8, and 10 were isolated from this plant for the first time.