• 제목/요약/키워드: Inhibitory concentration($IC_{50}$/)

검색결과 441건 처리시간 0.024초

넓패(Ishige foliacea) 추출물의 생리활성 탐색 (In Vitro Screening of the Physiological Activities of lshige foliacea Extracts)

  • 김지윤;박다빈;김민겸;박선주;김용태
    • 한국수산과학회지
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    • 제57권3호
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    • pp.209-215
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    • 2024
  • Ishige foliacea belongs to class Phaeophyceae and family Ishigeaceae. This study investigated the physiological activities of the Korean marine algae I. foliacea. Its solvent extracts were prepared with 70% ethanol, 80% methanol, and distilled water. The ethanol and methanol extracts had higher α-glucosidase (half-maximal inhibitory concentration, IC50: 0.67-0.73 mg/mL), xanthine oxidase (IC50: 0.25-0.28 mg/mL), and angiotensin-converting enzyme (IC50: 25.29-38.28 ㎍/mL) inhibitory activities than those of the water extract. The ethanol and methanol extracts possessed high acetylcholinesterase inhibitory activity (IC50: 0.78c0.97 mg/mL). Conversely, the water extract exhibited the highest β-secretase inhibitory activity (IC50: 0.48 mg/mL). These results indicate that I. foliacea may be useful as a functional substance in food and pharmaceuticals with anti-diabetic, anti-gout, anti-hypertension, and anti-dementia properties.

Discovery of Epinastine-NSAID Hybrids as Potential Anti-inflammatory Agents: Synthesis and In Vitro Nitric Oxide Production Inhibitory Activity Study

  • Woo, Hyeong Ryeol;Damodar, Kongara;Lee, Yeontaek;Lim, Soon-sung;Jeon, Sung Ho;Lee, Jeong Tae
    • 대한화학회지
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    • 제64권2호
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    • pp.79-83
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    • 2020
  • A novel pharmacophore with epinastine (1) and NSAID moieties (2-5) was designed by molecular hybridization approach. The hybrid compounds 6-9 were synthesized by EDCI/HOBt or HATU-mediated coupling of 1 with salicylic acid (2), mefenamic acid (3), indomethacin (4) and naproxen (5), respectively, and were assessed for their inhibitory effect against NO production in LPS-induced RAW-264.7 macrophages in vitro. The Hybrids were found to exhibit significant NO production inhibitory effects with half-maximal inhibitory concentration (IC50) values ranging in between 15.96 ± 1.32 and 36.68 ± 2.53 μM and were non-cytotoxic to macrophages. Comparing the inhibition concentration (IC50), cytotoxicity concentration (CC50) and in vitro efficacy index (iEI), 6 (IC50 = 17.97 ± 1.92 μM; iEI = 11.13) and 9 (IC50 = 15.96 ± 1.32 μM; iEI = 12.53) were better suited than other hybrids as well as their parent compound. Our findings signify that hybrids 6 and 9 may serve as platforms for continued investigations for the development of more efficient anti-inflammatory agents.

Antimicrobial, Antioxidative, Elastase and Tyrosinase Inhibitory Effect of Supercritical and Hydrothermal Asparagopsis Armata Extract

  • Lee, Kwang Won;Heo, Soo Hyeon;Lee, Jinseo;Park, Su In;Kim, Miok;Shin, Moon Sam
    • International Journal of Advanced Culture Technology
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    • 제8권3호
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    • pp.231-240
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    • 2020
  • In this paper, we present to evaluate physiological activity of Asparagopsis armata extraction. After extraction with Asparagopsis armata using hydrothermal and supercritical carbon dioxide, various physiological activities were examined. The total concentration of polyphenol compounds was determined to be 18.85 mg/g of hydrothermal Asparagopsis armata extraction and 14.74 mg/g of supercritical Asparagopsis armata extraction. In DPPH radical scavenging assay, ascorbic acid was used as positive antioxidant control. In ABTS radical scavenging assay, ascorbic acid was used as positive antioxidant control. The percentage of inhibition and IC50 were measured. The IC50 of Asparagopsis armata extraction is 261.44ppm and the IC50 of supercritical Asparagopsis armata extraction is 153.98 ppm. The elastase inhibitory assay showed concentration dependence and the IC50 of hydrothermal Asparagopsis armata extraction is 3387 ppm and the IC50 of supercritical Asparagopsis armata extraction is higher than 2500 ppm. In mushroom tyrosinase inhibition experiments, tyrosinase inhibition's IC50 of supercritical Asparagopsis armata extraction was 248.06. In the SOD-like experiments, the concentration-dependent results were showed and IC50 of hydrothermal Asparagopsis armata extraction is 845.29 ppm. In the antimicrobial experiments, maximum clear zones of supercritical Asparagopsis armata extraction represented 23.00 mm in Propionibacterium acnes. In the other hand, in experiments with the same conditions, hydrothermal Asparagopsis armata extraction had no effect in all strains.

Anticoagulant Properties of Compounds Derived from Fennel (Foeniculum vulgare Gaertner) Fruits

  • Lee, Hoi-Seon
    • Food Science and Biotechnology
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    • 제15권5호
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    • pp.763-767
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    • 2006
  • The anticoagulant properties of compounds derived from fennel (Foeniculum vulgare Gaertner) fruits were evaluated using a platelet aggregometer and compared with aspirin. The active constituents of fennel fruits were isolated and identified as (+)-fenchone and extragole by various spectral analysis techniques. With regard to the 50% inhibitory concentration ($IC_{50}$), (+)-fenchone effectively inhibited platelet aggregation induced by treatment with collagen ($IC_{50}$, $3.9\;{\mu}M$) and arachidonic acid (AA) ($IC_{50}$, $27.1\;{\mu}M$), and estragole inhibited collagen-induced platelet aggregation ($IC_{50}$, $4.7\;{\mu}M$). By way of comparison, (+)-fenchone and estragole proved to be significantly more potent than aspirin at inhibiting platelet aggregation induced by collagen. The inhibitory activity of (+)-fenchone toward platelet aggregation induced by AA was 1.3 times stronger than that of aspirin. These results indicate that (+)- fenchone and estragole may be useful as lead compounds for inhibiting platelet aggregation induced by arachidonic acid and collagen.

Antioxidant and Antidiabetic Activities of Eucommia ulmoides Bark

  • Qu, Guan-Zheng;Heo, Seong-Il;Wang, Myeong-Hyeon
    • Journal of Applied Biological Chemistry
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    • 제49권3호
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    • pp.82-85
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    • 2006
  • Eucommia ulmoides bark extracts by cold water, boiling water, 100% EtOH, 70% EtOH, 100% MeOH, 70% MeOH and $CHCl_3$ were assayed for their medicinal effects. The antioxidant activity of the extracts ranged from $IC_{50}$ 125.2 to $IC_{50}\;872.7{\mu}g/ml$ in the 1,1-diphenyl-2-picrylhydrazyl (DDPH) free radical-scavenging assay, and cold water extracts had the highest antioxidant activity. $CHCl_3$ extracts had the highest inhibitory effect on angiotensin I-converting enzyme (ACE) giving inhibition of up to 56.4% at a concentration of 1 mg/ml. Extracts in 100% EtOH had the greatest inhibitory effect on $\acute{a}-amylase$ activity ($IC_{50}=174.6{\mu}g/ml$), and 70% MeOH extracts had the greatest inhibitory effect on ${\alpha}-glucosidase$ activity ($IC_{50}=14.0{\mu}g/ml$). Taken together, these results provided the in vitro evidence on the ACE, amylase and glucosidase inhibitory actions of E. ulmoides bark that form the pharmacological basis for its antihypertensive and antidiabetic action.

새삼 (Cuscuta japonica Choisy) 및 실새삼 (C. australis R.Be) 추출물의 Mushroom Tyrosinase 활성 억제 효과 (Inhibitory Effects of Cuscuta japonica Extract and C. australis Extract on Mushroom Tyrosinase Activity)

  • 이승자;배정미;석귀덕
    • 생약학회지
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    • 제35권4호통권139호
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    • pp.380-383
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    • 2004
  • The purpose of this study was to evaluate mushroom Tyrosinase inhibitory activity of Cuscuta japonica Choisy and C. australis R.Be. The experimental materials were expressed juice from their stems and flowers, both water and ethanol extracts, their seeds, and two kinds of commercially available cosmetic packing Wontosa and Bupjetosa (made from seeds of C. japonica). The 50% inhibitory concentration $(IC_{50})$ of C. Japonica juice was 5.4 mg/ml. However, C. australis juice showed negligible mushroom tyrosinase inhibitory activity. The $IC_{50}$ of water extracted C. japonica seed was $54.0\;{\mu}g/ml$, water extracted product of Wontosa $50.0\;{\mu}g/ml$ and Bupjetosa $40\;{\mu}g/ml$. The $IC_{50}$ of ethanol extracted C. japonica seed was $10\;{\mu}g/ml$, Wontosa $10\;{\mu}g/ml$ and Bupjetosa $20\;{\mu}g/ml$.

인체 폐암 세포주에 대한 무의 에탄올 추출물의 세포독성 (Cytotoxicity of Ethanol Extract of Raphanuse Sativus on a Human Lung Cancer Cell Line)

  • 임효빈;이건순;채희정
    • 한국식품영양과학회지
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    • 제33권2호
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    • pp.287-290
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    • 2004
  • 무의 에탄올추출물을 이용하여 폐암에 대한 세포독성을 조사하였다. 청운 무를 무줄기와 무뿌리로 나누어 수세, 정선, 탈수한 후 에탄올과 물(5 : 5, v/v)의 흔합용매로 추출하고 폐암 세포주 A-549를 사용하여 MTT(3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide)법을 사용하여 항암 활성을 분석하였다. 각 well의 570 nm에서의 흡광도를 측정하고 대조군의 흡광도에 대한 백분율을 산출하였다. 실험 결과 무줄기 추출물과 무뿌리 추출물은 모두 A-549에 대한 세포 독성을 가지고 있었다. 무줄기 추출물의 $IC_{50}$/(50% inhibitory concentration)은 0.015%이었고 무뿌리 추출물의 $IC_{50}$/은 0.03%이었다. 동일 농도(0.01%)에서 무줄기 추출물이 무뿌리 추출물보다 A-549에 대한 항암활성이 더 뛰어났다.

Potential Role of $Ca^{++}$ on the Differentiation of Erythroid Progenitor Cells

  • Cho, In-Koo;Huh, In-Hoe;Lee, Sang-Jun;Kim, Dong-Seop;Ann, Hyung-Soo
    • Archives of Pharmacal Research
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    • 제18권2호
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    • pp.105-112
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    • 1995
  • In ordedr to gain insight into the mechanisms byl which erythropoietin promotes erythropoiesis, effects of various inhibitors on the erythropoietin-propmoted differentiation of erythroid progenitor cells and on the erythroid progenitor cells and on the erythropoietin-promoted $Ca^{++}$ uptake in the progenitor cells were determined, and the relationship between the inhibitory activity of each inhibitor cells were determined, and he relationship between the inhibitory activity of each inhibitor toward the differentiation and channel blocker (varapamil), a $Ca^{++}$ chelator (EDTA) and a protein kinase C inhibitor (stauroporine). All of these agents inhibited both the erythropoietin-mediated differentiation of the erythroid progenitor cells, as determined by the incroporation of $^{59}Fe$ into heme, and $Ca^{++}$ uptake in a concentrtion dependent manner. In the cases of varapamil and EDTA, the half-miximal inhibitory concentration $(IC_{50})$ values for differentiation of the progenitor cells may be theconsequence of the inhibition of the $Ca^{++}$ uptake in a concentration dependent manner. In the cases of varapamil and EDTA, the half-miximal inhibitory concentration dependent manner. In the cases of verapamil and EDTA, the half-miximal inhibitory concentration $(IC_{50})$ values for differentiation of the progenitor cells may be the consequence of the inhibition of the $Ca^{++}$ uptake by the inhibitor. On the other hand, in the cases of genistein and stauroporine, the $IC_{50}$ values for inhibition of differentitation were significantly different from that for inhibition of $Ca^{++}$uptake. These results suggest that the mechanism of inhibition of differentiation by these two inhibitors in complex. However, taken all together, the above results support the proposition that $Ca^{++}$ uptake may play a role in the erythropoietin-mediated differentiation of erythoid progenitor cells.

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클로렐라 가수분해물의 생리활성 분석 (Biological Efficacy Assay of Chlorella hydrolysate)

  • 강민숙;채희정
    • 한국산학기술학회논문지
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    • 제4권4호
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    • pp.366-371
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    • 2003
  • 클로렐라 추출물을 trypsin으로 가수분해하여 얻은 가수분해물을 이용하여 항균, 미백과 항암 활성을 분석하였다. Tyrosinase inhibition assay를 이용하여 미백활성을 측정한 결과 클로렐라 가수분해물의 효소활성에 대한 IC/sub 50/(50% inhibitory concentration)은 12%로 나타났다. In vitro에서 인체 폐암세포인 A-549에 대한 클로렐라 가수분해물의 항암 활성을 분석한 결과 클로렐라 가수분해물 0.15%에서 88.2%의 높은 암세포 억제율을 보였다.

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EFFICACY EVALUATION OF THE WHITENING COSMETICS USING IN VITRO TYROSINASE INHIBITION ASSAY

  • Lee, J. P.;Kim, Y. O.;J. Y. Jang;K. H. Son;S. J. Yang;Lee, K. S.;Kim, W. H.;J. T. Hong;Park, S. S.
    • 대한화장품학회:학술대회논문집
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    • 대한화장품학회 2003년도 IFSCC Conference Proceeding Book II
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    • pp.479-479
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    • 2003
  • We investigated the tyrosinase inhibitory effect using whitening materials such as arbutin, ethyl ascorbyl ether, glabridin, kojic acid, magnesium ascorbyl phosphate and ascorbic acid. Tyrosinase inhibition rate were determined varying the enzyme concentration, reaction time, reaction temperature and pH. The optimal conditions to measure the inhibitory efficacy were as follows. : enzyme concentration 1,500 or 2,000IU/mL, reaction time 15min(for the enzyme concentration 1,500 IU/mL) and l0min(for the enzyme concentration 2,000IU/mL), reation temperature 42$^{\circ}C$, pH 6.5. Under these conditions $IC_{50}$/ of arbutin, ethyl ascorbyl ether, glabridin, kojic acid, magnesium ascorbyl phosphate and ascorbic acid were calculated. In the case of magnesium ascorbyl phosphate, the inhibitory effect of tyrosinase was very low and the $IC_{50}$/ of magnesium ascorbyl phosphate could not be calculated. Other five materials showed good inhibitory effect of tyrosinase and can be used for the whitening materials.

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