• Title/Summary/Keyword: $IC_50$

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Antimicrobial and Antioxidative Effects of Isoflavonoids on Skin Microbial Inflammation Pathogens (Isoflavonoid의 피부염증균에 대한 항균 및 항산화효과)

  • Shin, Jung-Mi;Yu, Hung-Won;Lee, Hyun-Ok;Lee, Mi-Hee;Baek, Seung-Hwa
    • YAKHAK HOEJI
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    • v.50 no.1
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    • pp.15-20
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    • 2006
  • Puerarin and daidzin have been isolated from Puerariae thunbergiana Benth. Structures were determined by spectroscopic methods. Compounds showed weak antimicrobial activity against S. mutans, S. epidermidis, S. aureus, and C. albicans (MIC, $800{\mu}g/ml$). However, these compounds were not antioxidative. Puerariae thunbergiana Benth. extracts against microorganisms were evaluated in terms of the minimum inhibitory concentrations (MIC). In general, C. albicans was stronger antimicrobial activity than the other microorganisms. The antioxidative activity of was observed in the etyl acetate extract ($IC_{50},\;119.87{\pm}0.16\;{\mu}g/ml$). The DPPH radical scavenging effect ($IC_{50},\;1,673.3{\pm}0.54\;{\mu}M$) of the puerarin was comparable with that of synthetic antioxidant, BHA $(IC_{50},\;88.39{\pm}1.1){\times}10^{3}{\mu}M$. These results suggest that puerarin and daidzin have a potential antimicrobial activity.

Screening of Herbal Medicines from China and Vietnam with Inhibitory Activity on Advanced Glycation End Products (AGEs) Formation (IV) (중국, 베트남산 약용식물의 최종당화산물 생성저해활성 검색 (IV))

  • Kim, Jong-Min;Kim, Young-Sook;Kim, Joo-Hwan;Yoo, Jeong-Lim;Kim, Jin-Sook
    • Korean Journal of Pharmacognosy
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    • v.40 no.4
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    • pp.388-393
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    • 2009
  • Advanced glycation end products (AGEs) have been implicated in the development of diabetic complications. The AGEs inhibitors or cross-link breakers attenuate various functional and structural manifestations of diabetic complications. In this study, 64 herbal medicines from China and Vietnam have been investigated with an in vitro evaluation system using AGEs inhibitory activity. Of these, eight herbal medicines ($IC_{50}$<50 ${\mu}g$/ml) were found to have strong AGEs inhibitory activity compared with aminoguanidine (14 days, $IC_{50}$=75.98 ${\mu}g$/ml; 28 days, $IC_{50}$=88.27 ${\mu}g$/ml). Particularly, four herbal medicines, Buddleja officinalis (whole plant), Syzygium cuminii (leaf), Eugenia caryophyllate (seed), and Paeonia suffruticosa (root) showed more potent inhibitory activity (approximately 5-6 fold) than the positive control aminoguanidine.

Characterization of Dye Decolorization in Cell-Free Culture Broth of Trametes versicolor CBR43

  • Ryu, Hyun;Ryu, Hee Wook;Cho, Kyung-Suk
    • Journal of Microbiology and Biotechnology
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    • v.27 no.1
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    • pp.155-160
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    • 2017
  • The dye decolorization rate in a cell-free culture broth of the white-rot fungus Trametes versicolor CBR43 was studied, including the effects of inhibitors of NaCl, Zn(II), and Cd(II) on dye decolorization activity. The maximum rates of dye decolorization in cell-free culture broth were 1,410, 44.7, 41.2, and $0.19{\mu}mol{\cdot}l^{-1}{\cdot}min^{-1}$ for Acid Blue 62, Acid Black 175, Reactive Blue 4, and Acid Red 114, respectively. The inhibition effects of NaCl, Zn(II), and Cd(II) on dye decolorization were quantitatively compared using the half maximal inhibition concentration ($IC_{50}$), which indicates the concentration of an inhibitor required for 50% inhibition. Based on $IC_{50}$ values, dye decolorization in the cell-free culture broth of CBR43 was most potently inhibited by Cd(II), whereas the inhibitory effect of NaCl was relatively low. The dye decolorization rates and $IC_{50}$ data can be used in the design and development of a dye-wastewater treatment process using T. versicolor CBR43 and its operating factors.

Pharmacological Effects of Asaronaldehyde Isolated from Acorus gramineus Rhizome

  • Kim, Hyo-Gyung;Jeon, Ju-Hyun;Kim, Moo-Key;Lee, Hoi-Seon
    • Food Science and Biotechnology
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    • v.14 no.5
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    • pp.685-688
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    • 2005
  • Antibacterial and antiplatelet activities of Acorus gramineus rhizome-derived asaronaldehyde and asaron were analyzed using platelet aggregometer and six human intestinal bacteria. Active constituent of A. gramineus rhizome was isolated and characterized as asaronaldehyde by spectral analyses. At 2 and 1 mg/disk, asaronaldehyde exhibited strong inhibition of Clostridium perfringens and C. difficile without adverse effects on growth of beneficial bacteria such as Bifidobacterium bifidum, Lactobacillus acidophilus, and L. casei. Asaron also revealed moderate growth inhibition against C. perfringens and C. difficile at 2 mg/disk, no growth-inhibiting activity was observed on B. bifidum, L. acidophilus, L. casei, and E. coli. At 50% inhibitory concentration ($IC_{50}$) value, asaronaldehyde was effective in inhibiting platelet aggregation induced by collagen ($IC_{50}$, $27.6\;{\mu}M$) and arachidonic acid ($IC_{50}$, $53.7\;{\mu}M$). These results suggest asaronaldehyde may be useful as lead compound for inhibiting platelet aggregation induced by collagen and arachidonic acid.

Anticoagulant Properties of the Active Compound Derived from Cinnamomum cassia Bark

  • Lee, Hoi-Seon
    • Food Science and Biotechnology
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    • v.16 no.2
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    • pp.218-222
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    • 2007
  • The anticoagulant properties of Cinnamomum cassia bark-derived materials were evaluated against platelet aggregation induced by arachidonic acid (AA), collagen, platelet activating factor (PAF), or thrombin, and these effects were then compared to those of three commercially available compounds (cinnamic acid, cinnamyl alcohol, and aspirin). The active constituent obtained from C. cassia barks was isolated by silica gel column chromatography and high pressure liquid chromatography (HPLC), and was characterized as trans-cinnamaldehyde by MS, $^1H-NMR$, $^{13}C-NMR$, and IR spectroscopy. With regard to 50% inhibitory concentration ($IC_{50}$) values, cinnamaldehyde was found to effectively inhibit platelet aggregation induced by AA ($IC_{50},\;43.2\;{\mu}M$) and collagen ($IC_{50},\;3.1\;{\mu}M$). By way of comparison, cinnamaldehyde proved to be a significantly more potent platelet inhibitor against platelet aggregation induced by collagen than aspirin. The effect exerted by cinnamaldehyde against platelet aggregation induced by AA was 1.2 times less than that of aspirin. These results indicate that cinnamaldehyde may prove useful as a lead compound for the inhibition of platelet aggregation induced by AA and collagen.

Lipoxygenase Inhibitory and Antioxidant Activities of Isolated Compounds from Moutan Cortex

  • Ha, Do-Thi;Trung, Trinh-Nam;Thuan, Nguyen-Duy;Yim, Nam-Hui;Min, Byung-Sun;Bae, Ki-Hwan
    • Natural Product Sciences
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    • v.16 no.2
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    • pp.68-74
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    • 2010
  • Phytochemical investigation on the ethyl acetate and n-butanol fractions of Moutan Cortex resulted in the isolation and characterization of a new monoterpene glycoside (3) and twenty known monoterpene glycosides (1, 2, 4-21). The structure of 3 was determined by spectroscopic data interpretation and physico-chemical properties. Compounds 1 and 8 presented a remarkable inhibitory activity against lipoxygenase-1 (LOX-1) with $IC_{50}$ values of 45.2 and $37.5\;{\mu}M$, respectively. Compounds 9, 10, 13, 18, 19, and 21 showed significant 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging effect with $IC_{50}$ values of 9.8, 25.5, 6.4, 15.2, 18.7, and $23.7\;{\mu}M$, respectively. Benzoylpaeoniflorin (8), which exhibited the highest inhibitory effect with an $IC_{50}$ value of $37.5{\pm}0.7{\mu}M$, was further analyzed the inhibition kinetics by Lineweaver-Burk plots. Results indicated that 8 is a non-competitive inhibitor, and the kinetic parameter values were estimated to be ($31.04\;{\mu}M$, Ki), ($0.29\;{\mu}M/min$, $V_m$), and ($48.50\;{\mu}M$, $K_m$).

Screening of Korean Herbal Medicines with Inhibitory Activity on Advanced Glycation End Products Formation (IX) (한국약용식물의 최종당화산물 생성저해활성 검색 (IX))

  • Lee, Yun Mi;Kim, Young Sook;Kim, Joo Hwan;Kim, Jin Sook
    • Korean Journal of Pharmacognosy
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    • v.44 no.3
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    • pp.298-304
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    • 2013
  • In this study, 64 Korean herbal medicines have been investigated with an in vitro evaluation systems using glycation end products (AGEs) formation inhibitory activity. Of these, 30 herbal medicines ($IC_{50}&lt;50{\mu}g/ml$) were found to have significant AGEs formation inhibitory activity. Of these, four herbal medicines ($IC_{50}&lt;5{\mu}g/ml$) were found to have significant AGEs formation inhibitory activity. Particularly, Cornus controversa (branches and leaves), Acer ginnala (stems and leaves), Platycarya strobilacea (flowers) and Picrasma quassioides (stems), showed more potent inhibitory activity (approximately 17-27 fold) than the positive control aminoguanidine ($IC_{50}=77.04{\mu}g/ml$).

Suppression of MCF-7 Human Breast Cancer Cell Proliferation by Globefish Takifugu obscurus Homogenate (복어(Takifugu obscurus) 균질액에 의한 MCF-7 인간 유방암세포 성장 억제 효과)

  • Kim, Junghoon;Kim, Jungho
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.53 no.6
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    • pp.878-885
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    • 2020
  • Previously, we reported that globefish Takifugu obscurus homogenate suppresses the growth of human colorectal cancer cells. To extend the applications of globefish homogenate, we investigated its cytotoxic effects on human breast cancer cells. To assess the effects of globefish homogenate on growth of MCF (Michigan Cancer Foundation)-7 human breast cancer cells, cell proliferation and colony formation assays were performed using the cell counting and Crystal Violet staining methods. The 50% inhibitory concentration (IC50) of globefish homogenate on MCF-7 cell proliferation was calculated from the sigmoidal dose-response curve. The colony formation assay demonstrated that MCF-7 cells treated with globefish homogenate formed up to 80% fewer colonies than control MCF-7 cells. Treatment with globefish homogenate markedly suppressed the growth of MCF-7 cells in a dose-dependent manner. The sensitivity of the cells to globefish homogenate was determined by calculating the IC50; in this case, the IC50 was 210 ㎍/mL. Furthermore, significant downregulation of Cyclin D1 expression, along with phospho-Akt and total Akt levels, was observed in MCF-7 cells treated with globefish homogenate. This study demonstrates that treatment with globefish homogenate inhibits the proliferation of MCF-7 human breast cancer cells by downregulating the expression of phosphor-Akt, total Akt, and Cyclin D1 proteins.

Enterocarpam-III Induces Human Liver and Breast Cancer Cell Apoptosis via Mitochondrial and Caspase-9 Activation

  • Banjerdpongchai, Ratana;Wudtiwai, Benjawan;Pompimon, Wilart
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.5
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    • pp.1833-1837
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    • 2015
  • An aristolactam-type alkaloid, isolated from Orophea enterocarpa, is enterocarpam-III (10-amino-2,3,4,6-tetramethoxyphenanthrene-1-carboxylic acid lactam). It is cytotoxic to various human and murine cancer cell lines; however, the molecular mechanisms remain unclear. The aims of this study were to investigate cytotoxic effects on and mechanism (s) of human cancer cell death in human hepatocellular carcinoma HepG2 and human invasive breast cancer MDA-MB-231 cells compared to normal murine fibroblast NIH3T3 cells. Cell viability was determined by MTT assay to determine $IC_{10}$, $IC_{20}$ and $IC_{50}$ levels, reactive oxygen species (ROS) production with 2',7'-dichlorohydrofluorescein diacetate and the caspase-3, -8 and -9 activities using specific chromogenic (p-nitroaniline) tetrapeptide substrates, viz., DEVD-NA, IETD-NA and LEHD-NA and employing a microplate reader. Mitochondrial transmembrane potential (MTP) was measured by staining with 3, 3'-dihexyloxacarbocyanine iodide ($DiOC_6$) and using flow cytometry. The compound was cytotoxic to HepG2 and MDA-MB-231 cells with the $IC_{50}$ levels of $26.0{\pm}4.45$ and $51.3{\pm}2.05{\mu}M$, respectively. For murine normal fibroblast NIH3T3 cells, the $IC_{50}$ concentration was $81.3{\pm}10.1{\mu}M$. ROS production was reduced in a dose-response manner in HepG2 cells. The caspase-9 and -3 activities increased in a concentration-dependent manner, whereas caspase-8 activity did not alter, indicating the intrinsic pathway activation. Enterocarpam-III decreased the mitochondrial transmembrane potential (MTP) dose-dependently in HepG2 cells, suggesting that the compound induced HepG2 cell apoptosis via the mitochondrial pathway. In conclusion, enterocarpam-III inhibited HepG2 and MDA-MB-231 cell proliferation and induced human HepG2 cells to undergo apoptosis via the intrinsic (mitochondrial) pathway and induction of caspase-9 activity.

Antioidants of Theae Folium and Moutan Cortex (녹차와 목단피의 항산화 성분)

  • Boo, Yong-Chool;Jeon, Che-Ok
    • Applied Biological Chemistry
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    • v.36 no.5
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    • pp.326-331
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    • 1993
  • Three antioxidants were isolated: (-)-epigallocatechin and (-)-epigallo catechin gallate from Theae Folium generally called green tea, and gallic acid from Moutan Cortex. They inhibited $Fe^{3+}-ADP/ascorbate-induced$ lipid peroxidation in rat liver microsomal fraction, showing $IC_{50}$, the concentration of antioxidants which is required to inhibit 50% of the peroxidation for microsomal membranes at 1 mg protein/ml, to be $0.2\;{\mu}g/ml$, $0.4\;{\mu}g/ml$ and $2.5\;{\mu}g/ml$, respectively.

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