• Title/Summary/Keyword: Organic IC

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Study on antioxidative, antidiabetic and antiobesity activity of solvent fractions of smilax china L. leaf extract (청미래덩굴잎 추출물 용매분획의 항산화, 항당뇨 및 항비만 활성연구)

  • Kang, Yun Hwan;Lee, Young-Sil;Kim, Kyoung Kon;Kim, Dae Jung;Kim, Tae Woo;Choe, Myeon
    • Journal of Nutrition and Health
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    • v.46 no.5
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    • pp.401-409
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    • 2013
  • Smilax china L., a native plant found in Asian countries, has several medicinal properties including antioxidant, anti-inflammatory, and anti-cancer effects. Although the root of the plant is commonly used as traditional herbal medicine in Korea and China, the medicinal properties of the leaves have not gained the same attention. In this study, we analyzed the antioxidant activity, ${\alpha}$-glucosidase inhibitory effect and lipid accumulation inhibition effect of Smilax china L. leaf water extract (SCLE) and its solvent fractions. SCLE was fractionated by using a series of organic solvents, including ethylacetate (EA) and n-butanol (BuOH). The EA fraction had the highest total polyphenol content ($440.20{\pm}12.67$ mg GAE/g) and total flavonoid content ($215.14{\pm}24.83$ mg QE/g). The radical scavenging activity $IC_{50}$ values of the EA fraction for 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azino-bis-(3-ethylbenzthiazoline)-6-sulfonic acid (ABTS) were 0.022 mg/mL and 0.13 mg/mL, respectively. Further, SOD-like activity and reducing power values of the EA fraction were higher than those of the other fractions. However, both the ${\alpha}$-glucosidase and lipid accumulation inhibition assays showed that the BuOH fraction ($83.35{\pm}4.18%$ at 1 mg/mL) and water extract ($11.27{\pm}2.67%$) were more effective than the EA fraction ($64.13{\pm}6.35%$, and $45.66{\pm}7.20%$). These results provide new insights into the potential anti-diabetic and anti-obesity effects of Smilax china L. leaf.

Aburatubolactam C, a Novel Apoptosis-inducing Substance Produced by Marine Streptomyces sp. SCRC A-20

  • Bae, Myung-Ae;Yamada, Kaoru;Uemura, Daisuke;Seu, Jung-Hwan;Kim, Young-Ho
    • Journal of Microbiology and Biotechnology
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    • v.8 no.5
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    • pp.455-460
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    • 1998
  • In the course of screening for new antitumor substances, a novel cytotoxic agent inducing apoptotic cell death was isolated from the culture broth of marine bacterial strain SCRC A-20. Strain SCRC A-20 was separated from a mollusk and was chemotaxonomically identified as a Streptomyces sp. The cytotoxic substance was purified by organic solvent extraction followed by silica gel column chromatography and preparative TLC. HRFAB-MS determined its molecular formula to be $C_{30}H_{40}N_2O_5$ (MW 508). The 1D and 2D NMR spectral data demonstrated that the substance has a novel lactam structure of a 20-membered macrocycle coupled with a unique acyl tetramine and bicyclo[3.3.0] octane, which includes three methyl groups, six olefinic protons, five carbonyl groups, a conjugated diene and a dienone. The substance, named aburatubolactam C, appeared to be cytotoxic for various continuously proliferating tumor cells of human and murine origins. The $IC_{50}$ values determined by MIT assay were in the range of 0.3 to $5.8\mug/ml$. When Jurkat T cells were treated with $3\mug/ml$. of aburatubolactam C, the apoptotic DNA fragmentation was detectable within 3 h, indicating that the cytotoxic effect of aburatubolactam C on tumor cells is attributable to the induced apoptosis.

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Simplified the Screening and In Vitro Appraisal of Antioxidant, Cytotoxic, Thrombolytic, Antimicrobial and Membrane Stabilizing Activities of Lablab Purpures at a Time

  • Rahman, M. Saifur;Uddin, M. Gias;Alam, M. Badrul;Yoo, Jin Cheol
    • Journal of Integrative Natural Science
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    • v.7 no.3
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    • pp.173-182
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    • 2014
  • To simplify the different biological investigation of the methanolic extract and solvent-solvent partitioning of Lablab purpures (L. purpures) bark. In-vitro anti-oxidant study was determined using total DPPH radical scavenging assay. In vitro antimicrobial study was measured by observing zone of inhibition. The cytotoxic activity was studied using brine shrimp lethality bioassay and thrombolytic activity by clot disruption method. The antioxidant potential was evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and Folin-Ciocalteau reagents using butylated hydroxytolune (BHT) and ascorbic acid as standards. The Aqueous soluble fraction revealed the highest free radical scavenging activity ($IC_{50}=48.76{\mu}g/mL$). The antimicrobial screening of the bark of L. purpures exhibited mild to moderate activity in test microorganisms. The CSF showed the maximum relative percentage inhibition against Salmonella parathyphi (34.2%) for bacteria and C. albicans (28.8%) for fungi whereas, lowest relative percentage inhibition against Sarcina lutea (22.0%) for bacteria and Aspergillus niger (24.4%) for fungi. In the brine shrimp lethality bioassay, The $LC_{50}$ values of Carbon tetrachloride and N-Hexane soluble fraction were found $92.18{\mu}g/mL$, and $68.95{\mu}g/mL$ respectively while the $LC_{50}$ values of standard Vincristine sulphate was $1.37{\mu}g/mL$. The methanolic extract and its organic soluble fractions of Lablab purpureus at concentration 2.0 mg/mL, significantly protected the lysis of erythrocyte membrane induced by hypotonic solution and heat as compared to the standard, acetyl salicylic acid (0.10 mg/mL). The MSF and AQSF produced 61.48 % and 53.75% inhibition of hemolysis of RBC caused by hypotonic solution respectively, whereas acetyl salicylic acid (0.10 mg/mL) showed 76.42%. Ethanol extract of L. purpures and all of its different partitions exhibited moderate thrombolytic activity of 37.25%-2.40%. Very good preliminary screening and simplified experiments were able to show the different biological activity of methanolic extract and its soluble fractions of L. purpures at a time.

Portable Amperometric Perchlorate Selective Sensors with Microhole Array-water/organic Gel Interfaces

  • Lee, Sang Hyuk;Kim, Hyungi;Girault, Hubert H.;Lee, Hye Jin
    • Bulletin of the Korean Chemical Society
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    • v.34 no.9
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    • pp.2577-2582
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    • 2013
  • A novel stick-shaped portable sensing device featuring a microhole array interface between the polyvinylchloride-2-nitrophenyloctylether (PVC-NPOE) gel and water phase was developed for in-situ sensing of perchlorate ions in real water samples. Perchlorate sensitive sensing responses were obtained based on measuring the current changes with respect to the assisted transfer reaction of perchlorate ions by a perchlorate selective ligand namely, bis(dibenzoylmethanato)Ni(II) (Ni(DBM)2) across the polarized microhole array interface. Cyclic voltammetry was used to characterize the assisted transfer reaction of perchlorate ions by the $Ni(DBM)_2$ ligand when using the portable sensing device. The current response for the transfer of perchlorate anions by $Ni(DBM)_2$ across the micro-water/gel interface linearly increased as a function of the perchlorate ion concentration. The technique of differential pulse stripping voltammetry was also utilized to improve the sensitivity of the perchlorate anion detection down to 10 ppb. This was acquired by preconcentrating perchlorate anions in the gel layer by means of holding the ion transfer potential at 0 mV (vs. Ag/AgCl) for 30 s followed by stripping the complexed perchlorate ion with the ligand. The effect of various potential interfering anions on the perchlorate sensor was also investigated and showed an excellent selectivity over $Br^-$, $NO_2{^-}$, $NO_3{^-}$, $CO{_3}^{2^-}$, $CH_3COO^-$ and $SO{_4}^{2^-}$ ions. As a final demonstration, some regional water samples from the Sincheon river in Daegu city were analyzed and the data was verified with that of ion chromatography (IC) analysis from one of the Korean-certified water quality evaluation centers.

Structure and Isolation of Antioxidative Substance Derived from Phaeodactylum tricornutum (Phaeodactylum tricornutum으로부터 항산화성 물질의 분리 및 구조)

  • KIM Se-Kwon;BYUN Hee-Guk;BAEK Ho-Chul;PARK Pyo-Jam;KANG Ok-Ju;KIM Jong-Bae
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.34 no.5
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    • pp.556-562
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    • 2001
  • The antioxidative activity of marine microalgae, Phaeodactylum tricornutum (P. tricornutum) of Bacillariophyceae, was determined by measuring radical scavenging effect on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. The chloroform fraction of P. tricornutum showed strong antioxidative activity, The potential antioxidative activity of factions extracted with mixture solution of organic solvents was detected in dichloromethane : methanol (2 : 1) fraction, This fraction was further purified by preparative thin layer chromatography (PTLC) and repeated reverse-phase HPLC. On the basis of chemical and spectoscopic evidence from results obtained by UV, FT-IR, EIMS and NMR, the compound purified from P. tricornutum was identified as zeaxanthin.

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Antitumor Activity of Paecilomyces japonica is Mediated by Apoptotic Cell Death

  • Park, Youn-Hee;Moon, Eun-Kyung;Shin, Yong-Kyu;Bae, Myung-Ae;Kim, Jong-Guk;Kim, Young-Ho
    • Journal of Microbiology and Biotechnology
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    • v.10 no.1
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    • pp.16-20
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    • 2000
  • The aqueous extract from the cultural mycelium of Paecilomyces japonica showed cytotoxicity against several tumor cells including Jurkat, U937, HL-60, HepG2, BW5147.G.1.4, and NIH3T3. When the aqueous extract was fractionated by sequential organic solvent extractions using n-hexane and ethyl acetate, the ethyl acetate fraction appeared to contain the most cytotoxic activity, and the $IC_{50}$ values for various tumor cells were in the range from 1.5 to $10.0{\;}\mu\textrm{g}/ml$. To elucidate the cellular mechanism underlying the induced cytotoxicity, the apoptotic DNA fragmentation along with the cell cycle proression was examined in Jurkat T cells following the ethyl acetate fraction treatment. In the presence of $2.5{\;}\mu\textrm{g}/ml$ of the ethyl acetate fraction, apoptotic DNA fragmentation of the cells was detected within 1 h and increased upto 24 h in a time-dependent manner. Under the same conditions, a sub-G1 peak was detectable by flow cytometry. These results indicate that the cytotoxic effect of P. japonica on tumor cells is attributable to the induced apoptosis.

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New Triterpenoids from the Fruits of Schisandra wilsoniana and Their Biological Activities

  • Gao, Xue-Mei;Li, Yun-Qi;Shu, Li-Dan;Shen, Yan-Qiong;Yang, Li-Ying;Yang, Liu-Meng;Zheng, Yong-Tang;Sun, Han-Dong;Xiao, Wei-Lie;Hu, Qiu-Fen
    • Bulletin of the Korean Chemical Society
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    • v.34 no.3
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    • pp.827-830
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    • 2013
  • Investigation of an organic extract of the fruits Schisandra wilsoniana led to the isolation of two new highly oxygenated nortriterpenoids, named schilancidilactones V-W (1-2). Their structures were elucidated by spectroscopic evidence. Compounds 1-2 feature a double bond between C-7 and C-8 compared with related known nortriterpenoids isolated from the genus Schisandra. Compounds 1 and 2 were tested for their anti-HIV-1 activities and cytotoxicity. The results revealed that compounds 1 and 2 showed moderate anti-HIV-1 activities with $EC_{50}$ 3.05 and 2.87 ${\mu}g/mL$, respectively, and compound 1 showed high cytotoxicity against KB and MDA-MB-231 cell with $IC_{50}$ values of 3.18 and 5.22 ${\mu}M$, respectively.

Transport of choline and its relationship to transport of cationic drugs in immortalized rat brain capillary endothelial cell line

  • Park, Hong-Mi;Lee, Kyeong-Eun;Lee, Na-Young;Kang, Young-Sook
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2003.11a
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    • pp.106-106
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    • 2003
  • Choline serves critical roles in the CNS both as a precursor of neurotransmitter and as an essential component of membrane phospholipids. The long-term maintenance of brain choline concentration is dependent on choline transport across the blood-brain barrier (BBB), And, we examined to elucidate the characteristics of transport of choline across the BBB using conditionally immortalized rat brain capillary endothelial cell line (TR-BBB) in vitro. The [$^3$H]choline in TR - BBB was increased by time dependently, but independent on Na$\^$+/, and the transport process is saturable with Michaelis-Menten constrant, Km of about 26 ${\mu}$M. The uptake of [$^3$H]choline is susceptible for inhibition by various organic cationic compounds including hemicholinium-3, tetraethylammonium chloride (TEA) and $\ell$-carnitine. Also, we investigated the relationship of transport of choline and cationic drugs. The uptake of [$^3$H]choline is inhibited by antioxidant, a-phenyl-n-tert-butyl nitrone (PBN) with IC$\sub$50/ of 1.2 mM. and by Alzheimer's disease therapeutics, such as acetyl $\ell$-carnitine, tacrine and donepezil. Also, choline uptake presented competitive inhibition with PBN, donepezil and acetyl $\ell$-carnitine in Lineweaver-Burk plot. In conclusion, TR-BBB cells express a saturable transport system for uptake of choline, and several cationic drugs may be transported into the brain by BBB choline transporter.

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Screening of Biological Activity of Solvent Extract from Styela clava Tunic for Fishery Waste Recycling (수산폐기물 재활용을 위한 미더덕껍질 용매 추출물의 생리활성 탐색)

  • Lee, Sang-Mee;Kang, Eun-Jin;Go, Tae-Hun;Jeong, Seong-Yun;Park, Geun-Tae;Lee, Hee-Sup;Hwang, Dae-Youn;Jung, Young-Jin;Son, Hong-Joo
    • Journal of Environmental Science International
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    • v.23 no.1
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    • pp.89-96
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    • 2014
  • Styela clava tunic is generated in large amounts as a waste from S. clava processing plants and causes environmental problem. Although biological activities of S. clava were reported by many investigators, study on S. clava tunic was little. In this study, therefore, tyrosinase inhibition and antioxidative activities of extracts from S. clava tunic using different solvent were investigated for recycling of the fishery waste. Among extraction methods tested, autoclaved extraction (25.7%) and hot water extraction (18.2%) appeared to be effective for extraction. The highest total phenolic content was 46.6 mg/g in autoclaved extract while the highest flavonoid content was 23.0 mg/g in chloroform extract. All extracts possessed tyrosinase inhibition activity and the inhibition activity was concentration-dependent. Inhibition concentration ($IC_{50}$) against tyrosinase activity was $0.36{\times}10^4$ mg/ml in ethanol extract, $0.11{\times}10^3$ mg/ml in acetone extract and 0.27 mg/ml in n-butanol extract. Among extracts tested, hot water and autoclaved extracts displayed higher antioxidative activity than organic solvent extracts. Therefore, our data suggest that extract from S. clava tunic may potential candidate for cosmetic product with whitening effect and medicine for diseases caused by various oxidative stresses.

Bioassay-Guided Isolation and Identification of Compounds from Arecae Pericarpium with Anti-inflammatory, Anti-oxidative, and Melanogenesis Inhibition Activities

  • Indriana, Amelia;Lee, Kyoung Jin;Kim, Yeong Shik
    • Natural Product Sciences
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    • v.22 no.3
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    • pp.193-200
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    • 2016
  • This study describes the anti-inflammatory, anti-oxidant, and melanogenesis inhibition activities of methanol extract and various organic solvent fractions of Arecae Pericarpium. We examined the inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, 1,1-diphenyl-2-picrylhydrazine (DPPH) scavenging activity, mushroom tyrosinase inhibition activity and melanin contents. The study showed that, among all tested fractions, methylene chloride fraction showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells ($IC_{50}$ value $8.89{\mu}g/mL$) and DPPH radical scavenging activity ($EC_{50}$ value $21.39{\mu}g/mL$). Methylene chloride and ethyl acetate fractions similarly inhibited mushroom tyrosinase activity. Methanol extract exhibited strongest reduction of melanin content in B16F10 melanoma cells. Based on the bioactivity assay results, methylene chloride and ethyl acetate fractions were further separated. Eight phenolic compounds were isolated, which are dimeric syringol (1), catechol (2), 4-hydroxybenzaldehyde (3), vanillin (4), 4-hydroxyacetophenone (5), apocynin (6), protocatechuic acid (7) and 4-hydroxybenzoic acid (8). Among the isolated compounds tested, catechol showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells. Catechol also showed the concentration-dependent NF-${\kappa}B$ inhibition activity. Arecae Pericarpium might have potentials to be developed as anti-inflammatory agent or dermatological product for skin-whitening agent.