• Title/Summary/Keyword: IC values

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Inhibition Effect of ACE (Angiotensin Converting Enzyme) and Kinetics of Aloe Acethylmannan (알로에 아세칠만난의 ACE (Angiotensin Converting Enzyme) 저해효과 및 동력학적 분석)

  • Ryu, Il-Whan;Shin, Yong-Seo
    • Korean Journal of Food Science and Technology
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    • v.29 no.6
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    • pp.1269-1274
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    • 1997
  • This study was researched to purify and characterize variety bioactive material acethylmannan from Aloe vera. Purified acethylmannan was mannose (67%), acetyl group (23%) and the rest glucose, galactose that consisting of long chain polydispered ${\beta}-1,4$ linked mannan polymers. The sugar and acetyl group in molecular were linked molar ration one third. $IC_{50}$ value (i.e that concentration which exhibits 50% more enzyme inhibition than control) on angiotensin converting enzyme were 0.58 mM. This compound were found to be a competitive inhibition of Angiotensin Converting Enzyme with apparent Ki values of 0.068 mM.

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Cardiotoxicity assessment of 31 herbal formulae by activity of hERG potassium channel in HEK 293 cells (hERG 칼륨채널 활성도 변화에 따른 31종 한약처방의 심장독성 평가)

  • Ha, Hyekyung;Jin, Seong Eun;Lee, Sion;Kim, Dong-Hyun;Seo, Chang-Seob;Shin, Hyeun-kyoo
    • The Journal of Korean Medicine
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    • v.43 no.1
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    • pp.33-41
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    • 2022
  • Objectives: Drug-induced blockade of the human ether-à-go-go related gene (hERG) potassium ion channel causes acquired long QT syndrome, which is known to cause cardiac arrhythmias and be fatal. To establish safety evidence of herbal formulae, we evaluated the effects of 31 herbal formulae on hERG channel activity. Methods: The current through hERG channel was measured by changing the membrane voltage before and after treatment with 31 herbal formulae in HEK 293 cell overexpressing hERG channel using a whole-cell patch clamp system. The current-voltage curves and the activity curves were fitted, and the hERG activity and 50% inhibitory concentration (IC50) according to each herbal formula were calculated. Results: Chokyungjongok-tang, Oncheong-eum, and Cheongsangbangpung-tang strongly inhibited the hERG activity, with IC50 values of 67.67, 141.2, and 296.3 ㎍/mL, respectively. Yeonkyopaedok-san, Eunkyo-san, Ukgan-san gajinphibanha, Daegunjoong-tang (except Oryzae gluten), Insamyangyoung-tang, Banhahubak-tang, SokyungHwalhyul-tang, Jodeung-san, Hyeonggaeyeongyo-tang, and Bangkeehwangkee-tang weakly inhibited hERG activity, with IC50 values ranging from 400 to 1000 ㎍/mL. The other 18 herbal formulae showed very weak hERG activity inhibition of less than 50% at the highest concentration (1000 ㎍/mL). Conclusion: This study provided safety information on cardiotoxicity by cardiac arrhythmia risk assessment of herbal formulae, and is expected to be a reference data for predicting the safety and risk of herbal formulae.

In vitro anti-cancer activity of hydrophobic fractions of Sparassis latifolia extract using AGS, A529, and HepG2 cell lines (꽃송이버섯(Sparassis latifolia) 추출물 소수성 분획의 항암 활성)

  • Choi, Moon-Hee;Han, Hyo-Kyung;Lee, Yong-Jo;Jo, Han-Gyo;Shin, Hyun-Jae
    • Journal of Mushroom
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    • v.12 no.4
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    • pp.304-310
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    • 2014
  • The use of mushrooms has immense potential in many diverse applications. Until now, more than 3,000 species are consumed around the world, and more than 100 have shown promising clinical activity against cancer and other chronic diseases. Sparassis latifolia (formerly S. crispa) is an edible mushroom that harbors ${\beta}$-glucan reported to possess immunostimulatory and anticancer properties. However there have been no reports on the anticancer activity of hydrophobic fractions of S. latifolia. In this study, the anticancer activities of S. latifolia extract and hydrophobic fractions were investigated using AGS (stomach cancer), A529 (lung cancer), and HepG2 (liver cancer) cell lines. In cytotoxicity results of A529 cells, fractions of A2, A3, A4, A6, A7, A8, A9, and A10 in all 12 fractions show low $IC_{50}$ values. For HepG2 cells, A7 fraction results in the lowest $IC_{50}$ value while A7, A8, and A11 fractions show low $IC_{50}$ values in AGS cells. S. latifolia extract lead to low cell viability in cancer cells, compared to positive control of paclitaxel. A compound with molecular weight of 181 were detected using HPLC-MS but not identified yet. As a result, the hydrophobic fractions of S. latifolia EtOH extract would be a possible candidate as natural anticancer agents in the future.

Arrest of Cell Growth by Inhibition of Endogenous Reverse Transcription Activity in Cancer and Somatic Cell Lines (사람의 암세포주 및 정상세포주에서 역전사 효소의 억제에 의한 세포 성장의 제한)

  • Mi-Jeong Kim;Sung-Ho Lee;Jong-Kuen Park;Byeong-Gyun Jeon
    • Journal of Life Science
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    • v.34 no.6
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    • pp.365-376
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    • 2024
  • The present study assessed the cytotoxic effects on cell growth and senescence in human cancer (A-549, AGS, HCT-116, MDA-MB-231, and U 87-MG) and normal (MRC-5 and mesenchymal stem cells) cell lines treated with efavirenz (EFA), an inhibitor of non-nucleoside reverse transcriptase (RTase). Following EFA treatment, the half-maximal inhibitory concentration (IC50) values were approximately 15 µM, and the IC50 value was significantly (p<0.05) lower in the cancer cell lines, compared to normal cell lines. After determining the IC50 values against EFA, each cell line was treated with 15 µM EFA for up to one week. Significant (p<0.05) decreases in endogenous RTase and telomerase activity were observed in the cancer cell lines. RTase and telomerase activity were absent or detected at very low levels in both EFA-untreated and treated MRC-5 and MSC normal cells. The cell doubling time (CDT) was also significantly (p<0.05) prolonged by the decreased cell growth rate in the EFA-treated cancer cell lines compared to the untreated cell lines. Furthermore, EFA-treated cancer cells displayed a high number of cells with a high intensity of senescence-associated ß-galactosidase activity (SA-ß-gal activity), compared to the untreated cells. The present study showed that inhibition of RTase activity induces cellular senescence and arrests cell growth in human cancer cell lines; however, normal cell lines showed greater tolerance against EFA. RTase treatment could offer optional chemotherapy for cancer treatment in human cancer cell lines with high RTase activity.

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

  • Kim, Kum-Suk;Shin, Mee-Kyung;Kim, Hyun-Young
    • Journal of the East Asian Society of Dietary Life
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    • v.18 no.4
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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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    • v.33 no.5
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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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    • v.58 no.1
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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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    • v.10 no.2
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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.

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

  • Park, Tae-Kyu;Hwang, Keum-Hee
    • Korean Journal of Pharmacognosy
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    • v.38 no.2 s.149
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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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    • v.20 no.1
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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.