• 제목/요약/키워드: $IC_{50}$ values

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백련(白蓮) 잎의 영양 성분 및 항산화 활성 (Nutritional Composition and Antioxidant Activity of the White Lotus (Nelumbo nucifera Gaertn) Leaf)

  • 김금숙;신미경;김현영
    • 동아시아식생활학회지
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    • 제18권4호
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    • pp.499-506
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    • 2008
  • The nutritional composition of the white lotus(Nelumbo nucifera Gaertn) leaf are moisture($1.87{\pm}0.06%$), crude ash($9.57{\pm}0.07%$), crude protein($15.53{\pm}0.4%$) and crude lipid($2.42{\pm}0.1%$) per 100g. The highest mineral content was K and Ca. The principal free sugars in the white lotus leaf was sucrose, fructose and glucose. The total phenolics compounds evidenced maximal levels of $8,842.73{\pm}20.57\;g/100g$. DPPH and hydroxyl radical of scavenging ability of each sample tended to increase with increasing degrees of the sample concentration. The $IC_{50}$ values of the ethanol extract, n-hexane, chloroform, ethylacetate, butanol and water fraction from the white lotus leaf to DPPH radicals were 5.65, 8.5, 8.27, 2.03, 2.3 and $13.7\;{\mu}g/mL$ respectively. The $IC_{50}$ values of the hydroxyl radical scavenging ability of the ethanol extract, ethylacetate, butanol and water fraction were 390, 574, 327 and $378\;{\mu}g/mL$ respectively.

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Design, Synthesis and In Vitro Cytotoxic Activity Evaluation of New Mannich Bases

  • Bui, Trung Hieu;Le, Thi Thuy;Vu, Thu Thuy;Hoang, Xuan Tien;Luu, Van Chinh;Vu, Dinh Hoang;Tran, Khac Vu
    • Bulletin of the Korean Chemical Society
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    • 제33권5호
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    • pp.1586-1592
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    • 2012
  • A series of Novel Mannich bases has been synthesized and evaluated $in$ $vitro$ cytotoxic activity against the human hepatocellular carcinoma (HepG2), human lung carcinoma (SK-LU-1), and human breast cancer (MCF-7). Compound $\mathbf{9f}$ was found to be most potent against three cell lines with $IC_{50}$ values of 1.57, 1.16 and 1.21 ${\mu}g$/mL, respectively. In addition, compounds $\mathbf{9g}$, $\mathbf{10f}$ exhibited very significant activity against MCF-7 cell line with $IC_{50}$ values of 2.0 ${\mu}g$/mL.

Inhibitory Effects of Quinoline Isolated from Ruta chalepensis and Its Structurally Related Derivatives against α-Amylase or α-Glucosidase

  • Park, Jun-Hwan;Lee, Hoi-Seon
    • Journal of Applied Biological Chemistry
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    • 제58권1호
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    • pp.5-8
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    • 2015
  • This study was to isolate an active component of the chloroform fraction from the methanol extract of Ruta chalepensis leaves and to measure inhibitory effects against ${\alpha}$-glucosidase or ${\alpha}$-amylase. The inhibitory compound of R. chalepensis leaves was isolated using chromatographic methods and identified as quinoline. Quinoline and its structurally related derivatives were tested for their inhibitory activities by evaluating the $IC_{50}$ values against ${\alpha}$-amylase or ${\alpha}$-glucosidase and were compared with that of acarbose. Based on the $IC_{50}$ values, quinazoline exhibited the greatest inhibitory activity ($20.5{\mu}g/mL$), followed by acarbose ($66.5{\mu}g/mL$), and quinoline ($80.3{\mu}g/mL$) against ${\alpha}$-glucosidase. In case of ${\alpha}$-amylase, quinazoline had potent inhibitory activity, followed by quinoline ($179.5{\mu}g/mL$) and acarbose ($180.6{\mu}g/mL$). These results indicate that R. chalepensis extract, quinoline, and quinazoline could be useful for inhibiting ${\alpha}$-glucosidase or ${\alpha}$-amylase.

Evaluation on the P-Glycoprotein Inhibitory Activity of Indonesian Medicinal Plants

  • Go, Eun-Jung;Kim, Hyang-Rim;Chung, Soo-Yeon;Jeong, Yeon-Hee;Kim, Na-Hyung;Han, Ah-Reum;Seo, Eun-Kyoung;Lee, Hwa-Jeong
    • Natural Product Sciences
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    • 제10권2호
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    • pp.85-88
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    • 2004
  • One hundred Indonesian plant extracts were screened to investigate their effects on the P-glycoprotein (P-gp) activity in human uterine sarcoma cells, MES-SA/DX5, for the first time. Among others, four samples, Alpinia galanga (BuOH ext.), Sindora sumatrana $(CHCl_3\;ext.)$, Strychnos ligustrina $(CHCl_3\;ext.)$, and Zingiber cassumunar Roxb (hexane ext.), exhibited the most potent inhibition on the P-gp activity. They increased cytotoxic activity of daunomycin up to $IC_{50}$ values of less than $1.41\;{\mu}M$, which is a value with a positive control, verapamil. Other 25 samples showed significant P-gp inhibitory activity with $IC_{50}$ values between 1.4 and $4.0\;{\mu}M$. These prospective samples will be subjected to further laboratory phytochemical investigation to find active principles.

치자추출물의 Monoamine Oxidase 저해활성 (Inhibitory Activity of the Fruit Extract of Gardenia jasminoides on Monoamine Oxidase)

  • 박태규;황금희
    • 생약학회지
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    • 제38권2호통권149호
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    • pp.108-112
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    • 2007
  • We examined the inhibitory activities against monoamine oxidase (MAO) of Gardenia jasminoides in vitro and in vivo methods. Methanolic extract and ethylacetate fraction of Gardenia jasminoides fruit showed a significant inhibitory activity on MAO-A and MAO-B in vitro. The IC$_{50}$ values of each fraction on MAO-A and MAO-B are as fo11owed; total methanol extracts 1.23 and 1.34 mg/ml, EtOAc fraction 0.72 and 0.77 mg/ml. Water-soluble fraction also showed IC$_{50}$ values of 0.81 mg/ml on MAO-B. MAO-A activity was increased by the oral administration of ethanolic extract of G. jasminoides, while MAO-B activity was decreased. The concentration of serotonin of brain tissue administrated of ethanolic extract of G. jasminoides is slightly increased in rat. This tendency is not different from the activity of deprenyl which is a well known MAO inhibitor was used as a positive control. Consequently, we suggest that G. jasminoides may have the effects on the inhibitory activity against MAO This activity of G. jasminoides is considerable for development of functional materials for treatment and control of depression, dementia, Parkinson' disease, stress and promoting exercise, etc.

Cytotoxic Triterpenoids from the Fruiting Bodies of Ganoderma lucidum

  • Tung, Nguyen The;Trang, Tran Thi Thu;Cuong, To Dao;Thu, Nguyen Van;Woo, Mi Hee;Min, Byung Sun
    • Natural Product Sciences
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    • 제20권1호
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    • pp.7-12
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    • 2014
  • Twelve triterpenoids (1 - 12) were isolated from $CHCl_3$-soluble fraction of fruiting bodies of Ganoderma lucidum. Extensive spectroscopic and chemical studies established the structures of these compounds as butyl lucidenate P (1), butyl lucidenate $E_2$ (2), butyl lucidenate $D_2$ (3), butyl lucidenate Q (4), ganoderiol F (5), methyl ganoderate H (6), methyl ganoderate J (7), lucidumol B (8), ganodermanondiol (9), methyl lucidenate N (10), methyl lucidenate A (11) and butyl lucidenate N (12). All of the compounds were examined for their cytotoxic activity against HL-60, HeLa, and MCF-7 cancer cell lines. Among them, compounds 4 and 8 showed cytotoxic activity with $IC_{50}$ values of 6.6 and 1.6 ${\mu}M$ against HL-60, respectively. In addition, compound 8 also showed cytotoxic activity with $IC_{50}$ values of 2.0 ${\mu}M$ against HeLa cancer cell line, other compounds were moderate or inactive.

차전자의 항암활성성분 (Anticancer Compounds of Plantago asiatica L.)

  • 문형인;지옥표
    • 한국약용작물학회지
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    • 제7권2호
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    • pp.143-146
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    • 1999
  • 차전자의 메탄올추출물을 헥산, 클로로포름, 에틸아세테이트, 부탄올로 계통분획하여, 활성을 검정하고, 그 중 활성분획인 헥산과 에틸아세테이트 분획을 크로마토그라피하여 4종의 화합물을 분리하였으며, 각종 기기분석과 이화학적 분석을 통하여 ${\beta}-sitosterol(C1)$, $cholest-5-en-3{\beta}-ol(C2)$, rutin(C3), $coumarin-7-O-{\beta}-glucopyranoside(C4)$임을 확인 하였으며, 4종의 화합물 중 $cholest-5-en-3{\beta}-ol$, rutin(C3)이 주요 항암 성분 이었다.

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New Production of 5-Bromotoluhydroquinone and 4-O-Methyltoluhydroquinone from the Marine-Derived Fungus Dothideomycete sp.

  • Leutou, Alain S.;Yun, Keum-Ja;Choi, Hong-Dae;Kang, Jung-Sook;Son, Byeng-Wha
    • Journal of Microbiology and Biotechnology
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    • 제22권1호
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    • pp.80-83
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    • 2012
  • The addition of NaBr to the fermentation medium of a marine isolate of the fungus Dothideomycete sp. resulted in induced production of two toluhydroquinone derivatives, 5-bromotoluhydroquinone (1) and 4-O-methyltoluhydroquinone (2), and two known compounds, toluhydroquinone (3) and gentisyl alcohol (4). The structures of 1 and 2 were assigned through the spectroscopic data analyses. Compounds 1-4 showed a potent antibacterial activity against the methicillin-resistant and multidrug-resistant Staphylococcus aureus (MRSA and MDRSA) with MIC (minimum inhibitory concentration) values of 6.2, 12.5, 6.2, and 12.5 ${\mu}g/ml$, respectively. Compounds 1-4 also exhibited a moderate radical scavenging activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH) with $IC_{50}$ values of 11.0, 17.0, 12.0, and 7.0 ${\mu}M$, respectively, which were more active than the positive control, L-ascorbic acid ($IC_{50}$, 20.0 ${\mu}M$).

Anti-inflammatory Compounds from the Leaves of Ailanthus altissima Meihua JIN

  • Jin, Me-Ihua;Bae, Ki-Hwan;Chang, Hyeun-Wook;Son, Jong-Keun
    • Biomolecules & Therapeutics
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    • 제17권1호
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    • pp.86-91
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    • 2009
  • In our ongoing search for biological components from the Korea endemic plants, the MeOH extract of Ailanthus altissima leaves (Simaroubaceae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity by assessing their effects on the production of prostaglandin $D_2$ ($PGD_2$) and leukotriene $C_4$ ($LTC_4$) in mouse bone marrow-derived mast cells (BMMCs). In further study, eight compounds, squalene (1), ${\beta}$-sitosterol (2), scopoletin (3), quercetin (4), luteolin (5), astragalin (6), scopolin (7), and daucosterol (8) were isolated, the chemical structures were elucidated on the basis of physicochemical and spectroscopic data and by comparison with those of published literatures. Among the compounds, 2, 4, and 5 strongly inhibited both the COX-2-dependent PGD2 generation with $IC_{50}$ values of 2.6, 7.3 and 2.5 ${\mu}M$, respectively and the generation of $LTC_4$ in the 5-LOX dependent phase with $IC_{50}$ values of 2.0, 5.1 and 1.8 ${\mu}M$, respectively, which suggest that the anti-inflammatory activity of A. altissima might occur in part via the inhibition of both $PGD_2$ and $LTC_4$ generation by 2, 4 and 5.

Flavonols from Houttuynia cordata with Protein Glycation and Aldose Reductase Inhibitory Activity

  • Jang, Dae-Sik;Kim, Jong-Min;Lee, Yun-Mi;Yoo, Jeong-Lim;Kim, Young-Sook;Kim, Joo-Hwan;Kim, Jin-Sook
    • Natural Product Sciences
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    • 제12권4호
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    • pp.210-213
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    • 2006
  • A 4,5-dioxoaporphine type alkaloid, cepharadione B (1), a phenolic acid, protocatechuic acid (2), and flavonols, quercetin (3), afzelin (4), and quercitrin (5), were isolated from the EtOAc-soluble extract of the whole plants of Houttuynia cordata. All the isolates (1-5) were subjected to in vitro bioassays to evaluate advanced glycation end products (AGEs) formation and rat lens aldose reductase (RLAR) inhibitory activity. The three flavonols 3-5 exhibited a significant inhibitory activity on AGEs formation with $IC_{50}$ values of 66.9, 58.9, and $32.3{\mu}M$, respectively. While the two flavonol rhamnosides 4 and 5 showed a remarkable inhibitory activity against RLAR with $IC_{50}$ values of 0.81 and $0.16{\mu}M$, respectively.