• Title/Summary/Keyword: $IC_{50}$ values

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Effects of Methyl Gallate on Arachidonic Acid Metabolizing Enzymes: Cyclooxygenase-2 and 5-Lipoxygenase in Mouse Bone Marrow-Derived Mast Cells

  • Kim, Se-Jong;Jin, Mei-Hua;Lee, Eun-Kyung;Moon, Tae-Chul;Quan, Zhe-Jiu;Yang, Ju-Hye;Son, Kun-Ho;Kim, Kil-Ung;Son, Jong-Kun;Chang, Hyeun-Wook
    • Archives of Pharmacal Research
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    • v.29 no.10
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    • pp.874-878
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    • 2006
  • Methyl gallate (MG) is a medicinal herbal product that is isolated from Paeonia lactiflora that inhibits cyclooxygenase-2 (COX-2) dependent phases of prostaglandin $D_2\;(PGD_2)$ generation in bone marrow-derived mast cells (BMMC) in a concentration-dependent manner with an $IC_{50}$ values of $17.0\;{\mu}M$. This compound also found inhibited the COX-2-dependent conversion of the exogenous arachidonic acid to $PGD_2$ in a dose-dependent manner with an $IC_{50}$ values of $190\;{\mu}M$, using a COX enzyme assay kit. However, at concentrations up to $80\;{\mu}M$, MG did not inhibit COX-2 protein expression in BMMC, indicating that MG inhibits COX-2 activity directly. Furthermore, MG consistently inhibited the production of leukotriene $C_4\;(LTC_4)$ in a dose dependent manner, with an $IC_{50}$ value of $5.3\;{\mu}M$. These results demonstrate that MG has a dual cyclooxygenase-2/5-lipoxygenase inhibitory activity, which might provide the basis for novel anti-inflammatory drugs.

Evaluation of Abelmoschus Esculentus Seed for Antioxidant and Phytochemical Analysis Using In vitro Assays

  • Rahman, Md. Saifur;Yoo, Jin Cheol
    • Journal of Integrative Natural Science
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    • v.7 no.4
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    • pp.260-265
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    • 2014
  • The aim of this study was to assess the in vitro potential of methanolic seed extract of Abelmoschus esculentus as a natural antioxidant. The DPPH activity of the Ethyl acetate soluble fraction (10, 20, 40, 80, and $160{\mu}g/mL$) was increased in a dose dependent manner, which was found in the range of 18.97-90.47% as compared to ascorbic acid 26.44-93.71%. The $IC_{50}$ values of Ethyl acetate soluble fraction (EAES) and ascorbicacid in DPPH radical scavenging assay were obtained to be 28.12 and $18.43{\mu}g/mL$, respectively. Measurement of polyphenol content of the EAES of A. esculentus seed was achieved using Folin-Ciocalteau reagent containing 53.80 mg/g of total phenolic content, which was found signicantly higher when compared to reference standard gallic acid. Similarly total flavonoids and proabthocyanidis of EAES and chloroform soluble fraction (CAES) were found significantly 147 mg/g and 14.24 mg/g respectively when both compared to reference standard quercetin. EAES exhibited high significant lipid peroxidation inhibition effects in a dose-dependent manner, with $IC_{50}$ values of $38.08{\mu}g/mL$, whereas, standard quercetin, with $IC_{50}$ value of $36.67{\mu}g/mL$. All extract/fractions showed dose dependent reducing power ability and these differences were statistically significant (p<0.001). The results obtained in this study clearly indicate that A. esculentus seed has a signicant potential to use as a natural antioxidant agent.

Antineoplastic Effect of Low Molecular Weight Chitooligosaccharide on Various Tumor Cell Lines (저분자량 키토산 올리고당의 항종양성)

  • Park, Heon-Kuk
    • The Korean Journal of Food And Nutrition
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    • v.22 no.2
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    • pp.308-312
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    • 2009
  • In this study, the effects of low molecular weight chitooligosaccharides were assessed. Low molecular weight chitooligosaccharide evidenced no cytotoxicity in in vitro trials with the normal cell line, Vero E6(Africa green monkey kidney cell). The $IC_{50}$ of low molecular weight chitooligosaccharide was $923.20{\mu}g/m{\ell}$. Low molecular weight chitooligosaccharide exhibited in vitro antineoplastic activity in five human tumor(lung carcinoma, bladder carcinoma, colon carcinoma, stomach carcinoma, breast carcinoma) cell lines. The $IC_{50}$ values of low molecular weight chitooligosaccharide on A549, J82, SNU-C4, SNU-1 and ZR75-1 were $477.42{\mu}g/m{\ell}$, $480.40{\mu}g/m{\ell}$, $436.84{\mu}g/m{\ell}$, $373.55{\mu}g/m{\ell}$, and $539.95{\mu}g/m{\ell}$, respectively.

In Vitro Antineoplastic Effects of Chitosan Hydrolysates on Various Tumor Cell Lines (키토산 가수분해물의 In Vitro 항종양성)

  • Park, Heon-Kuk
    • The Korean Journal of Food And Nutrition
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    • v.22 no.4
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    • pp.639-643
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    • 2009
  • In this study, the antineoplastic effects of chitosan hydrolysates were assessed. The chitosan hydrolysates showed no cytotoxicity in in vitro trials using the normal cell line, Vero E6(Africa green monkey kidney cells). The $IC_{50}$ value of the chitosan hydrolysates on Vero E6 was 1,107.95 ${\mu}g/m{\ell}$. The hydrolysates exhibited in vitro antineoplastic activity in five human tumor (lung carcinoma, bladder carcinoma, colon carcinoma, stomach carcinoma, breast carcinoma) cell lines. The $IC_{50}$ values of the hydrolysates on A549, J82, SNU-C4, SNU-1, and ZR75-1 cells were 421.06, 417.99, 445.54, 380.65 and 460.49 ${\mu}g/m{\ell}$, respectively.

Antioxidant Effect of Berberine and its Phenolic Derivatives Against Human Fibrosarcoma Cells

  • Pongkittiphan, Veerachai;Chavasiri, Warinthorn;Supabphol, Roongtawan
    • 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.

Studies on the Anti-cancer Activity of Chaga Mushroom Extract (차가버섯 추출물의 항암활성에 관한 연구)

  • Moon, Byung-Hyuk;Lee, Won-Chul
    • 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.

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Biofunctionality of Peptides Purified from Naturally Fermented Anchovy Sauce (천연 숙성 멸치액젓 Peptide의 생리활성)

  • 박종혁;김상무
    • 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.

STUDIES ON ANTI-ORAL CANCER ACTIVITIES OF MEDICINAL PLANT EXTRACTS (구강암에 대한 약용식물 추출물의 항암효과에 관한 연구)

  • Lee, Young-Hoon;Kim, Yeo-Gab;Kim, Jung-Hee
    • 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.

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Quality Characteristics of Yanggeng Prepared with Different Concentrations of Mulberry Fruit Syrup (오디시럽을 이용한 오디양갱 제조 및 품질특성)

  • Kim, Ae-Jung
    • Journal of the East Asian Society of Dietary Life
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    • v.22 no.1
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    • pp.62-67
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    • 2012
  • In this research, mulberry fruit was processed into mulberry fruit syrup (MFS) using sugar and then used as stabilizer for anthocyanine pigment in yanggeng. MFS was added to the yanggeng in order to make mixture ratio of 0%, 5%, 10%, 15% and 20%. The resulting sensory and physicochemical aspects, as compared between the various MFS ratio were investigated. The yanggeng L and b values decreased with increasing ratio of MFS. With addition of MFS the sensory evaluation results for, taste, color, flavor, texture and overall acceptability improved. The yanggeng prepared using MFS found to possess more effective antioxidants behavior as observed by in vitro evaluating 1,1-diphenyl-2-picrylhydrazyl(DPPH) radical scavenging and superoxide radical activities. The $IC_{50}$ of the antioxidant was found to be proportional to the mulberry fruit syrup concentration in the yanggeng.

Property Comparison of Polyclonal Anti-Soy Protein Antibodies Produced for ELISA (효소면역측정법을 위한 다클론 항대두단백 항체의 생산 및 특성비교)

  • Shon, Dong-Hwa;Kim, Hyun-Jung;Yun, Sung-Seob
    • Korean Journal of Food Science and Technology
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    • v.32 no.6
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    • pp.1221-1226
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    • 2000
  • Specific antibodies were produced to develope the enzyme-linked immunosorbent assay for analysis of soy proteins and the properties of the antibodies were compared. Isolate soy protein(ISP), and ISP heated with SDS and urea (ISP(SU)), acidic subunits(AS) of 11S globulin were immunized to produce polyclonal antibodies. By using competitive indirect ELISA(ciELISA), the reactivities of the antibodies toward soy proteins treated with different methods were investigated and shown as $IC_{50}$. $IC_{50}'s$ of anti-ISP antibodies to ISP, ISP(SU), ISP treated with 2-ME(ISP(ME)), and crude 11S were 20, 30, 36, and $1000\;{\mu}g/mL$, respectively. And the values of anti-ISP(SU) antibodies to the same antigens were 100, 5, 4, and $220\;{\mu}g/mL$ and those of anti-AS antibodies were 20, 2, 2.5, and $200\;{\mu}g/mL$, respectively. Therefore, anti-AS antibodies showed the highest reactivities toward soy proteins among the produced antibodies as determined by ciELISA.

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