• Title/Summary/Keyword: $IC_{50}values$

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Effect of Ainsliaea acerifolia Extract on Anti-acetylcholinesterase and Peroxynitrite Scavenging and Analysis of Caffeoylquinic Acids (단풍취 추출물의 Acetylcholinesterase 저해 및 Peroxynitrite 소거에 대한 활성과 Caffeoylquinic Acid 성분의 분석)

  • Nugroho, Agung;Choi, Jae Sue;Song, Byong-Min;Park, Hee-Juhn
    • Korean Journal of Plant Resources
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    • v.32 no.4
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    • pp.270-274
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    • 2019
  • Anti-acetylcholinesterase (anti-AChE) activity and peroxynitrite scavenging activity of Ainsliaea acerifolia (Compositae) were studied to find its anti-Alzheimer's activity. The $IC_{50}$ was $73.4{\mu}g/mL$ in AChE assay and $8.60{\mu}g/mL$ in peroxynitrite assay. Caffeoylquinic acids that have been reported to have anti-Alzheimer's activity were analyzed in the leaf- and stem extract by HPLC. Caffeoylquinic acids occupied 25.1% of the leaf extract which was higher than 8.1% of the stem extract. Particularly, the content of 3,5-dicaffeoylquinic acid (145.6 mg/g) was highest of the tested caffeoylquinic acids. In addition, the $IC_{50}$ values of 3,5-dicaffeoylquinic acid were shown to be $3.79{\mu}g/mL$ in peroxynitrite assay and $69.19{\mu}g/mL$ in anti-AChE assay.

In vitro antioxidant activity of black tea (Camellia sinensis L.) residue extract (홍차박 추출물의 in vitro 항산화 활성)

  • Kim, Dong Chung
    • Journal of Applied Biological Chemistry
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    • v.62 no.3
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    • pp.281-286
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    • 2019
  • A black tea (Camellia sinensis L.) residue extract (BTRE) was prepared by 30% ethanol extraction to evaluate its in vitro antioxidant activity. The yield and polyphenol content of BTRE were $22.4{\pm}1.18%$ and $23.2{\pm}1.02{\mu}g$ gallic acid equivalents/mg-extract, respectively. Antioxidant activity of BTRE proportionally increased as BTRE concentration increased. $IC_{50}$ values of BTRE for cation radical, free radical and nitrite scavenging were 141.8, 108.1, and $397.2{\mu}g/mL$, respectively. Also $IC_{50}$ value of BTRE for ferric reducing anti-oxidant power was $97.8{\mu}g/mL$. BTRE effectively inhibited linoleic acid peroxidation. These results imply that BTRE possessed potent antioxidant activity, thus being utilized as a physiologically active material.

Anti-inflammatory Effects in LPS-treated RAW 264.7 Cells and the Influences on Drug Metabolizing Enzyme Activities by the Traditional Herbal Formulas, Yongdamsagan-Tang and Paljung-san

  • Ha, Hyekyung;Jin, Seong Eun;Seo, Chang-Seob;Shin, Hyeun-kyoo
    • The Journal of Korean Medicine
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    • v.42 no.4
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    • pp.10-24
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    • 2021
  • Objectives: Yongdamsagan-tang (YST) and Paljung-san (PJS) in traditional medicine and finasteride in modern medicine are used to treat benign prostatic hyperplasia (BPH). In recent, the use of combination herbal remedies with conventional drugs has been increasing. Therefore, we investigated the anti-inflammatory effects of these drugs to treat BPH and the influence of herbal formulas on finasteride metabolism. Methods: The inhibitory effects of the herbal formulas and finasteride on the production of inflammatory mediators and cytokines were determined in lipopolysaccharide (LPS)-treated RAW 264.7 cells. Additionally, the influence of herbal formulas on activities of human drug metabolizing enzymes (DMEs) was assessed using human microsomal enzymes. Results: We observed that YST, PJS and finasteride inhibited the production of nitric oxide (NO), prostaglandin E2 (PGE2) and interleukin-6 (IL-6) in RAW 264.7 cells. The half maximal inhibitory concentration (IC50) of YST on PGE2 production was calculated to be below 25 ㎍/mL. YST inhibited the activity of uridine diphosphate-glucuronosyltransterase (UGT) 1A4 with an IC50 value of 49.35 ㎍/mL. The activities of cytochrome P450 (CYP) 1A2, CYP2B6, CYP2C19, CYP3A4, and UGT1A1 were inhibited by PJS (IC50 < 100 ㎍/mL, each). Although PJS and YST inhibited the activities of CYP3A4 and UGT1A4, respectively, these formulas may not influence the metabolism of finasteride because the IC50 values of herbal formulas on DMEs are too high to affect metabolism. Conclusions: Our results suggest that the combination of finasteride and YST or PJS might not influence their drug metabolism and that the drugs may have synergistic effects against BPH.

Quantifying the Interactive Inhibitory Effect of Heavy Metals on the Growth and Phosphorus Removal of Pseudomonas taeanensis

  • Yoo, Jin;Kim, Deok-Hyun;Oh, Eun-Ji;Chung, Keun-Yook
    • Korean Journal of Soil Science and Fertilizer
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    • v.51 no.1
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    • pp.35-49
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    • 2018
  • This study was initiated to quantitatively evaluate the effects of five heavy metals (Cd, Cu, Zn, Pb, and Ni) on growth and P removal efficiencies of Pseudomonastaeanensis, known as the phosphorus accumulating microorganism. The heavy metals were added individually and with the binary mixture to the batch culturing system of Pseudomonastaeanensis. $IC_{50}$ and $EC_{50}$ were used to quantitatively evaluate their effects on the growth and phosphorus removal efficiency of Pseudomonas taeanensis in those treatments. Additionally, additive index value method was used to evaluate the interactive effects of heavy metals for Pseudomonas taeanensis in this study. As those heavy metals were singly added to Pseudomonastaeanensis, the greatest inhibitory effect on its growth and P removal efficiency was observed in Cd, whereas, the smallest effect was found in Ni. As the concentrations of all heavy metals added were gradually increased, its growth and P removal efficiency was correspondingly decreased. Specifically, $IC_{50}$ of Pseudomonas taeanensis for Cd, Cu, Zn, Pb, and Ni were $0.44mg\;L^{-1}$, $5.12mg\;L^{-1}$, $7.46mg\;L^{-1}$, $8.37mg\;L^{-1}$ and $14.56mg\;L^{-1}$, respectively. The P removal efficiency of Pseudomonas taeanensis was 81.1%. $EC_{50}$ values of Pseudomonas taeanensis for Cd, Cu, Zn, Pb, and Ni were $0.44mg\;L^{-1}$, $4.08mg\;L^{-1}$, $7.17mg\;L^{-1}$, $8.90mg\;L^{-1}$ and $11.26mg\;L^{-1}$, respectively. In the binary treatments of heavy metals, the lowest $IC_{50}$ and $EC_{50}$ were found in the Cd + Cu treatment, whereas, the highest $IC_{50}$ and $EC_{50}$ were found in the Zn + Pb and Pb + Ni treatments, respectively. Most of the interactive effects for the binary mixture treatments of heavy metals were antagonistic. Based on the results obtained from this study, it appears that they could provide the basic information about the toxic effects of the respective individual and binary treatments of heavy metals on the growth and P removal efficiency of other phosphorus accumulating organisms.

Anticoagulation and Anticancer Constituents from Eugenia caryophyllata Thunb

  • Han, Kyung-Min;Kim, Dong-Hyun;Ahn, Eun-Mi;Lee, Youn-Hyung;Chung, In-Sik;Kim, Dae-Keun;Kwon, Byoung-Mog;Kim, Sung-Hoon;Baek, Nam-In
    • Korean Journal of Medicinal Crop Science
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    • v.15 no.2
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    • pp.82-88
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    • 2007
  • From the EtOAc fraction of Eugenia caryophyllata, four compounds were isolated through activity-guided silica gel column chromatography, From the result of spectroscopic data including NMR, MS and IR, the chemical structures of the compounds were determined as 1-allyl-4-hydroxy-3-methoxybezene acetate (eugenol acetate, 1), 1-allyl-4-hydroxy-3-methoxybezene (eugenol, 2), $3{\beta}-hydroxyolean-12-en-28-oic$ acid (oleanolic acid, 3) and $2{\alpha}$, $3{\beta}-dihydroxyolean-12-en-28-oic$ acid (maslinic acid, 4). Compounds 3 and 4 were isolated for the first time from this plant. Also, compounds 1, 2 and 3 exhibited relatively high platelet aggregation inhibitory activity with the $IC_{50}$ values of 0.24, 0.09 and 0.07 mM, respectively. Compound 2 significantly prolonged activated partial thromboplastin time (aPTT) with the value of $124{\pm}11.2$ seconds as compared to the control with the value of $37.5{\pm}2.2$ seconds at the concentration of 50 ${\mu}g/ml$. Compounds 1 and 3 revealed inhibitory activity on farnesyl protein transferase (FPTase) with the $IC_{50}$ values of 0.49 and 0.24 mM and compounds 1 and 2 highly inhibited the growth of rat-H-ras cells with the $Gl_{50}$ values of 6.63 and 5.70 ${\mu}M$, respectively.

Antimalarial Activity and Phytochemical Profile of Ethanolic and Aqueous Extracts of Bidara Laut (Strychnos ligustrina Blum) Wood

  • MANURUNG, Harisyah;SARI, Rita Kartika;SYAFII, Wasrin;CAHYANINGSIH, Umi;EKASARI, Wiwied
    • Journal of the Korean Wood Science and Technology
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    • v.47 no.5
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    • pp.587-596
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    • 2019
  • This study aimed to determine the antimalarial effect of the Strychnos ligustrina (SLW) wood extracts and to analyze its phytochemicals. The SLW powder samples were macerated with 100% ethanol (E100), 75% ethanol (E75), 50% ethanol (E50), 25% ethanol (E25), and aqueous (A100). The extracts were analyzed by LCMS/MS, and its in-vitro antimalarial activity was tested with Plasmodium falciparum. The results showed that the extract yields of E100, E75, E50, E25, and A100 were 4.3, 5.2, 5.3, 4.7, and 3.6%, respectively. The antimalarial activities of the A100, E25, E50, and E75 extracts were classified as active with $IC_{50}$ values of 38.6, 42.6, 42.9, and $43.7{\mu}g/mL$, respectively. But, the antimalarial activity of the E100 extract was classified as slightly active with $IC_{50}$ values of $87.4{\mu}g/mL$. The dominant compounds contained in the extracts of A100, E25, E50, E75, and E100 was the alkaloid compound, namely brucine with relative concentrations of 24.96, 24.55, 21.33, 11.79, and 11.62%, respectively.

Antiplatelet and Antithrombotic Activities of Lindera obtusiloba Extract in vitro and in vivo

  • Lee, Jung-Ok;Kim, Chul-Young;Lee, Seung-Woo;Oak, Min-Ho
    • Biomolecules & Therapeutics
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    • v.18 no.2
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    • pp.205-210
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    • 2010
  • Several studies have shown that plant-derived polyphenols reduce cardiovascular accidents in high-risk patients and the inhibition of platelet function may be responsible for part of this benefit. Lindera obtusiloba is widely used in traditional herbal medicine for the treatment of cardiovascular and inflammatory diseases. Therefore, the antiplatelet and antithrombotic activities of Lindera obtusiloba Extracts (LOE) on in vitro platelet aggregation, radical scavenging activity and in vivo murine pulmonary thrombosis were examined. LOE was able to directly scavenge the stable DPPH radical in a concentration-dependent manner and its $IC_{50}$ value was 3.9 ${\pm}$ 0.1 ${\mu}g$/ml. LOE significantly inhibited collagen- and ADP-induced platelet aggregation in a concentration-dependent manner and its $IC_{50}$ value is 0.9 ${\pm}$ 0.1 mg/ml and 0.4 ${\pm}$ 0.1 mg/ml respectively. The inhibitory effect of LOE was comparable to aspirin ($IC_{50}$ values were 1.0 ${\pm}$ 0.5 and 1.0 ${\pm}$ 0.7 mg/ml, respectively). Furthermore, oral administration of LOE suppressed the death of mice with pulmonary thrombosis induced by intravenous injection of collagen plus epinephrine. Taken together, our results suggest LOE may be a promising candidate for antithrombotic agent, and the antithrombotic effect of LOE may be due to, at least in part, antiplatelet activity.

Investigation of Antioxidant, Hypoglycemic and Anti-Obesity Effects of Euphorbia Resinifera L.

  • Benrahou, Kaoutar;El Guourrami, Otman;Mrabti, Hanae Naceiri;Cherrah, Yahia;My El Abbes, Faouzi
    • Journal of Pharmacopuncture
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    • v.25 no.3
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    • pp.242-249
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    • 2022
  • Objectives: The aim of this work is to evaluate the in vitro antioxidant, hypoglycemic, and antiobesity effects of Euphorbia resinifera extracts and investigate the phenolic constituents and the toxicity of these extracts. Methods: Phytochemical screening was performed to detect polyphenols and flavonoids. Antioxidant activity was evaluated by four methods (DPPH, ABTS, H2O2, and xanthine oxidase inhibition). The hypoglycemic effect was determined by the inhibition of α-amylase and α-glucosidase enzymes in vitro and via a starch tolerance study in normal rats. The antiobesity effect was estimated by in vitro inhibition of lipase. Results: Phytochemical screening revealed that the ethanolic extract was rich in polyphenols (99 ± 0.56 mg GEA/g extract) and tannins (55.22 ± 0.17 mg RE/g extract). Moreover, this extract showed higher antioxidant activity in different tests: the DPPH assay (IC50 = 53.81 ± 1.83 ㎍/mL), ABTS assay (111.4 ± 2.64 mg TE/g extract), H2O2 (IC50 = 98.15 ± 0.68 ㎍/mL), and xanthine oxidase (IC50 = 10.26 ± 0.6 ㎍/mL). With respect to hypoglycemic effect, the aqueous and ethanolic extracts showed IC50 values of 119.7 ± 2.15 ㎍/mL and 102 ± 3.63 ㎍/mL for α-amylase and 121.4 ± 1.88 and 56.6 ± 1.12 ㎍/mL for α-glucosidase, respectively, and the extracts lowered blood glucose levels in normal starch-loaded rats. Additionally, lipase inhibition was observed with aqueous (IC50 = 25.3 ± 1.53 ㎍/mL) and ethanolic (IC50 = 13.7 ± 3.03 ㎍/mL) extracts. Conclusion: These findings show the antioxidant, hypoglycemic, and hyperlipidemic effects of E. resinifera extracts, which should be investigated further to validate their medicinal uses and their pharmaceutical applications.

α-Glucosidase Inhibition Activity of the Extracts of Katsura Tree (Cercidiphyllum japonicum Sieb. Et Zucc) Leaves

  • Lee, Tae-Seong;Ryu, Wang-Gyun;Bae, Young-Soo
    • Journal of the Korean Wood Science and Technology
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    • v.43 no.2
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    • pp.238-247
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    • 2015
  • Katsura tree (Cercidiphyllum japonicum Sieb. Et Zucc) leaves were collected, air-dried and extracted with 70% aqueous acetone, then concentrated and sequentially fractionated using n-hexane, $CH_2Cl_2$, EtOAc, and $H_2O$ to be freeze dried for antioxidant and ${\alpha}$-glucosidase inhibition activity tests. The antioxidant activity of the extracts was evaluated using DPPH (1,1-diphenyl 2-picrylhydrazyl) free radical scavenging assay. The test concentrations were adjusted to 500, 250, 125, 62.5, 31.25, 15.62, 7.81, 3.9, 1.95 and 0.97 ppm. The $H_2O$ and EtOAc fractions showed higher activities compared with the control, ${\alpha}$-tocopherol, at all concentrations. The crude fraction also gave better activity at the concentrations lower than 62.5 ppm. However, the nonpolar n-hexane and $CH_2Cl_2$ fractions gave prominently lower activities compared with the control at all concentrations. The $IC_{50}$ values of the crude, EtOAc, and $H_2O$ fractions exhibited 11.78, 4.29 and $9.80{\mu}g/m{\ell}$, respectively, compared with $12.08{\mu}g/m{\ell}$ of the control. But the n-hexane and $CH_2Cl_2$ fractions indicated 300 and $91.85{\mu}g/m{\ell}$ of $IC_{50}$, respectively. ${\alpha}$-Glucosidase inhibition activity was evaluated at the concentrations of 50, 25, 12.5, 6.3, 3.1, 1.6 and 0.8 ppm. The inhibition activities were increased according to as the increase of sample concentrations. However, the nonpolar n-hexane and $CH_2Cl_2$ fractions indicated very low inhibition activities compared with acarbose, a positive control. The EtOAc fraction showed very good capability as almost 100% compared with the control at the higher concentrations than 12.5 ppm and the crude fraction also indicated good potential as 95% and 100% at 25 and 50 ppm, respectively. The $H_2O$ fraction gave good inhibition value as 90% at 50 ppm although the value was lower than the control. These results showed that the polar fractions had better ${\alpha}$-glucosidase inhibition activities. The $IC_{50}$ values of the nonpolar fractions, n-hexane and $CH_2Cl_2$, showed very lower values as 468 and $103.6{\mu}g/m{\ell}$, respectively, than the control. ${\alpha}$-Glucosidase Inhibition Activity of the Extracts of Katsura Tree (Cercidiphyllum japonicum Sieb. Et Zucc) Leaves However, the polar fractions, crude, EtOAc and $H_2O$, showed 7.1, 3.7 and $13{\mu}g/m{\ell}$, respectively, indicating that these fractions can be used as natural bioresources for treating diabetes mellitus. Also ${\alpha}$-glucosidase inhibition activity had a positive correlation with antioxidant activity of the extracts.

Antioxidant activities of hot water extract of Syneilesis palmata root and aerial part (우산나물 뿌리와 지상부 열수 추출물의 항산화 활성)

  • Lee, Yang-Suk;Kim, Nam-Woo
    • Food Science and Preservation
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    • v.21 no.1
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    • pp.9-16
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    • 2014
  • This study was performed in order to investigate the antioxidant properties of hot water extract from the root and aerial part of the Syneilesis palmata in respect to its potential use as food, cosmetics material, or medicinal resource. The results showed that the S. palmata root hot water extract (RHW) possessed a higher content of total flavonoid compounds (4.58 mg/g) and total polyphenol compounds (59.11 mg/g). The SOD-like activities of the RHW and APHW were 23.74% and 21.61%, respectively, at a concentration $2,000{\mu}g/mL$. In the nitrite scavenging ability of a $2,000{\mu}g/mL$ concentration, the RHW showed 63.06% (pH 1.2) and 47.16% (pH 3.0). The $IC_{50}$ values of the nitrite scavenging abilities were $99.93{\mu}g/mL$ (ascorbic acid), $1,150.85{\mu}g/mL$ (RHW), and $1,610.25{\mu}g/mL$ (APHW). The $IC_{50}$ values of DPPH free radical scavenging abilities were $99.87{\mu}g/mL$ (RHW) and $118.29{\mu}g/mL$ (APHW). The inhibition values ($IC_{50}$) of xanthine oxidase were $139.62{\mu}g/mL$ (RHW) and $111.11{\mu}g/mL$ (APHW). In all of the experiments, the S. palmata root hot water extracts have higher activities than the aerial hot water extract, except for the xanthine oxidase inhibitory activity. These results suggest that the S. palmata is a potentially useful antioxidant source for the development of functional nutraceuticals, cosmetics and medicine.