• Title/Summary/Keyword: IC values

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Antioxidant Activity of Brown Seaweed, Ecklonia maxima, Collected from South Africa (남아프리카공화국 갈조류 Ecklonia maxima 줄기의 항산화 활성 평가)

  • Choi, Ye-Ji;Kim, Hyun-Soo;Je, Jun-Geon;Wang, Lei;Jeon, You-Jin
    • Journal of Marine Bioscience and Biotechnology
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    • v.11 no.1
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    • pp.29-35
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    • 2019
  • In the present study, the alcoholic and enzymatic extracts of Ecklonia maxima were prepared and their antioxidant activities were evaluated via the free radical scavenging activities. The lyophilized seaweed powder was extracted by 70% ethanol and the resultant extract was obtained, named as the alcoholic extract of E. maxima stem (EMSE) obtained. The residue after EMSE preparation was continuously by Celluclast-assistant extraction and then the obtained enzymatic extract was identified as polysaccharides-rich extract of E. maxima stem (EMSP). The results indicated that the extraction yields of EMSE and EMSP were 2.18% and 5.43%, respectively. In addition, the free radical scavenging activities of EMSE and EMSP were determined using an electron spin resonance (ESR) spectrometer. EMSE containing 5.36% of polyphenol and 1.56% of polysaccharide scavenged DPPH and alkyl radicals at the $IC_{50}$ values of 0.48 and 0.63 mg/mL, respectively. EMSP containing 0.33% of polyphenol and 41.58% of polysaccharide showed at the $IC_{50}$ values of 0.33 and 0.55 mg/mL, respectively. These results demonstrate that EMSP containing a high amount of polysaccharides possesses a strong free radical scavenging activity which might be a potential ingredient in pharmacological and cosmeceutical industries.

Characterization of Natural Compounds as Inhibitors of NS1 Endonuclease from Canine Parvovirus Type 2

  • So-Hyung Kwak;Hayeong Kim;Hyeli Yun;Juho Lim;Dong-Hyun Kang;Doman Kim
    • Journal of Microbiology and Biotechnology
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    • v.33 no.6
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    • pp.788-796
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    • 2023
  • Canine parvovirus type 2 (CPV-2) has high morbidity and mortality rates in canines. Nonstructural protein 1 (NS1) of CPV-2 has endonuclease activity, initiates viral DNA replication, and is highly conserved. Thus, it is a promising target for antiviral inhibitor development. We overexpressed a 41.9 kDa active recombinant endonuclease in Escherichia coli and designed a nicking assay using carboxyfluorescein and quencher-linked ssDNA as substrates. The optimal temperature and pH of the endonuclease were 37℃ and pH 7, respectively. Curcumin, bisdemethoxycurcumin, demethoxycurcumin, linoleic acid, tannic acid, and α-tocopherol inhibited CPV-2 NS1 endonuclease with IC50 values of 0.29 to 8.03 µM. The extracted turmeric, yerba mate, and sesame cake suppressed CPV-2 NS1 endonuclease with IC50 values of 1.48, 7.09, and 52.67 ㎍/ml, respectively. The binding affinity between curcumin, the strongest inhibitor, and CPV-2 NS1 endonuclease by molecular docking was -6.4 kcal/mol. Curcumin inhibited CPV-2 NS1 endonuclease via numerous hydrophobic interactions and two hydrogen bonds with Lys97 and Pro111 in the allosteric site. These results suggest that adding curcuminoids, linoleic acid, tannic acid, α-tocopherol, extracted turmeric, sesame cake, and yerba to the diet could prevent CPV-2 infection.

Biochemical and structural comparisons of non-nucleoside reverse transcriptase inhibitors against feline and human immunodeficiency viruses

  • Siriluk Rattanabunyong ;Khuanjarat Choengpanya;Chonticha Suwattanasophon ;Duangnapa Kiriwan ;Peter Wolschann ;Thomanai Lamtha ;Abdul Rajjak Shaikh ;Jatuporn Rattanasrisomporn;Kiattawee Choowongkomon
    • Journal of Veterinary Science
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    • v.24 no.5
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    • pp.67.1-67.15
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    • 2023
  • Background: Feline immunodeficiency virus (FIV) causes an acquired immunodeficiency-like syndrome in cats. FIV is latent. No effective treatment has been developed for treatment the infected cats. The first and second generations non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV treatment, nevirapine (NVP) and efavirenz (EFV), and rilpivirine (RPV), were used to investigate the potential of NNRTIs for treatment of FIV infection. Objective: This study aims to use experimental and in silico approaches to investigate the potential of NNRTIs, NVP, EFV, and RPV, for inhibition of FIV reverse transcriptase (FIV-RT). Methods: The FIV-RT and human immunodeficiency virus reverse transcriptase (HIV-RT) were expressed and purified using chromatography approaches. The purified proteins were used to determine the IC50 values with NVP, EFV, and RPV. Surface plasmon resonance (SPR) analysis was used to calculate the binding affinities of NNRTIs to HIV-RT and FIV-RT. The molecular docking and molecular dynamic simulations were used to demonstrate the mechanism of FIV-RT and HIV-RT with first and second generation NNRTI complexes. Results: The IC50 values of NNRTIs NVP, EFV, and RPV against FIV-RT were in comparable ranges to HIV-RT. The SPR analysis showed that NVP, EFV, and RPV could bind to both enzymes. Computational calculation also supports that these NNRTIs can bind with both FIV-RT and HIV-RT. Conclusions: Our results suggest the first and second generation NNRTIs (NVP, EFV, and RPV) could inhibit both FIV-RT and HIV-RT.

Chemical composition, antioxidant and antifungal activities of rhizome essential oil of Kaempferia parviflora Wall. ex Baker grown in Vietnam

  • Dang-Minh-Chanh Nguyen;Thi-Hoan Luong;Tien-Chung Nghiem;Woo-Jin Jung
    • Journal of Applied Biological Chemistry
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    • v.66
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    • pp.15-22
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    • 2023
  • The aim of the present study was to evaluate the chemical composition and antioxidative activity of rhizome essential oil of Kaempferia parviflora Wall. ex Baker. The essential oil extracted by hydrodistillation was chemically profiled by GC/MS analysis. The antioxidative activity was determined and evaluated spectroscopically by the 2,2-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging assays. According to the results, the major essential oil components were camphene (18.03%), β-pinene (14.25%), a-pinene (12.38%), endo-borneol (10.23%), β-copaene (8.38%), and linalool (8.20%). K. parviflora rhizome oil possessed antioxidant potential, exhibiting DPPH and ABTS radical scavenging activities as high as 80.90 and 94.04%, respectively, at a concentration of 10 mg/mL. The corresponding IC50 values were 0.451±0.051 and 0.527±0.022 mg/mL, respectively (IC50 values for ascorbic acid, as the standard, were 0.209±0.016 and 0.245±0.022 mg/mL, respectively). The mycelium of F. oxysporum was distorted and collapsed when treated with 0.5 mg/mL of the EO of K. parviflora rhizome for 3 days treatment, which may provide an important information for exploring the metabolism of the fungicide K. parviflora rhizome and its derived compounds against F. oxysporum. This study provides the chemical properties of the essential oil of K. parviflora rhizome grown in Vietnam and their potential antioxidant and antifungal activities.

Identification and Antioxidative Effects of Phenolic Compounds from Chinese Soybean (Heinong 48) (중국산 대두 (Heinong 48)의 페놀성 화합물 검출 및 항산화 효과)

  • Jeon, Ki-Suk;Xu, Yun-Long;Park, Shin-In
    • Culinary science and hospitality research
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    • v.21 no.3
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    • pp.259-269
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    • 2015
  • This study was performed to investigate the phenolic compounds content and antioxidative activity of methanol extract from Chinese soybean. The content of total phenolics and total flavonoids of Chinese soybean Heinong 48) extract were $9.91{\pm}0.57GAE\;mg/g$ and $4.15{\pm}0.39QE\;mg/g$, respectively. The antioxidative activities of Chinese soybean extract were significantly increased in a dose dependent manner on 1,1-diphenyl-2-picrylhydrazyl(DPPH) radical scavenging and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)(ABTS) radical scavenging($IC_{50}$ values were $2.04{\pm}0.16$ and $3.31{\pm}0.31mg/mL$, respectively). These results suggest that Chinese soybean may have great potential as a natural antioxidant source with health benefits.

Secondary Metabolites with Anti-complementary Activity from the Stem Barks of Juglans mandshurica Maxim

  • Li, Zi-Jiang;Chen, Shilin;Yang, Xiang-Hao;Wang, Rui;Min, Hee-Jeong;Wu, Lei;Si, Chuan-Ling;Bae, Young-Soo
    • Journal of the Korean Wood Science and Technology
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    • v.46 no.2
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    • pp.118-124
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    • 2018
  • Juglans mandshurica is a fast growing hard species, which is a tree in family of Juglandaceae and has a wide distribution in China, Korea and eastern Russia. Plant materials from J. mandshurica have extensively been used in folk medicines to prevent or cure gastric, esophageal, lung and cardiac cancer. As one chain of our searching for anticomplementary agents from natural sources, two epimeric ellagitannins, [2,3-O-4,4',5,5',6,6',-hexahydroxydiphenoyl (HHDP))-(${\alpha},{\beta}$)-D-glucose] (I) and pedunculagin (II) were purified from 70% acetone extracts of the stem barks of J. mandshurica by Thin Layer Chromatography and Sephadex LH-20 column chromatography approaches. The chemical structures of the isolated compounds were characterized by MS, NMR, and a careful comparation with published literatures. The epimeric ellagitannins I and II exhibited inhibitory properties against a classical pathway of complementary system with 50 % inhibitory concentrations ($IC_{50}$) values of 65.3 and $47.7{\mu}M$, respectively, comparing with riliroside ($IC_{50}=104{\mu}M$) and rosmarinic acid ($IC_{50}=182{\mu}M$), which were used as positive controls. Thus, the work indicated both the two secondary metabolites possess excellent inhibitory activity and might be developed as potential anticomplementary chemicals.

Low Density Lipoprotein-oxidation Inhibitory Phytochemicals from the Fruits of Rhus parviflora

  • Shrestha, Sabina;Park, Ji-Hae;Cho, Jin-Gyeong;Lee, Dae-Young;Kang, Ji-Hyun;Li, Hua;Jeong, Tae-Sook;Kim Cho, Somi;Lee, Dong-Sun;Baek, Nam-In
    • Journal of Applied Biological Chemistry
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    • v.58 no.2
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    • pp.109-112
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    • 2015
  • Fruits of Rhus parviflora were extracted with 80% aqueous methanol (MeOH), and the concentrated extract was partitioned using ethyl acetate (EtOAc), n-butanol (n-BuOH), and $H_2O$, successively. Purification of EtOAc fraction led to isolation of fifteen polyphenols of which structures were identified by spectroscopic methods including 2D-NMR. Most compounds apart from compound 10 inhibited low density lipoproteinoxidation within $IC_{50}$ value of $10{\mu}M$. Among compounds, taxifolin (2), quercetin 3-O-${\alpha}$-L-rhamnopyranoside (13), agathisflavone (5) sulfuretin (4), and aureusidin (3) showed $IC_{50}$ values 0.9, 0.8, 5.8, 2.9, and $2.4{\mu}M$ which were of highly significant in comparison positive control butylated hydroxytoluene with $IC_{50}$ value of $2.1{\mu}M$. The results indicate fruits of R. parviflora as a source of antihypercholesterolemic compounds.

Anti-Proliferation Effects of Benzimidazole Derivatives on HCT-116 Colon Cancer and MCF-7 Breast Cancer Cell Lines

  • Al-Douh, Mohammed Hadi;Sahib, Hayder B.;Osman, Hasnah;Hamid, Shafida Abd;Salhimi, Salizawati M.
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.8
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    • pp.4075-4079
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    • 2012
  • Benzimidazoles 1-4 were obtained using modified synthesis methods and studied for their ability to inhibit cell proliferation of colon cancer cell HCT-116 and breast cancer cell MCF-7 using MTT assays. In the HCT-116 cell line, benzimidazole 2 was found to have an $IC_{50}$ value of $16.2{\pm}3.85{\mu}g/mL$ and benzimidazole 1 a value of $28.5{\pm}2.91{\mu}g/mL$, while that for benzimidazole 4 was $24.08{\pm}0.31{\mu}g/mL$. In the MCF-7 cell line, benzimidazole 4 had an $IC_{50}$ value of $8.86{\pm}1.10{\mu}g/mL$, benzimidazole 2 a value of $30.29{\pm}6.39{\mu}g/mL$, and benzimidazole 1 a value of $31.2{\pm}4.49{\mu}g/mL$. Benzimidazole 3 exerted no cytotoxity in either of the cell lines, with $IC_{50}$ values $>50{\mu}g/mL$. The results suggest that benzimidazoles derivatives may have chemotherapeutic potential for treatment of both colon and breast cancers.

Field Validation of a Sampling and Analytical Method Developed for Preventing Airborne Hexavalent Chromium Collected on PVC Filter from Reduction (PVC 여과지에서의 환원 방지를 위해 개발된 공기중 6가 크롬 측정방법의 현장 평가)

  • 신용철;백남원
    • Journal of Environmental Health Sciences
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    • v.28 no.2
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    • pp.109-116
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    • 2002
  • The purpose of this study was to evaluate a new sampling and analytical method for the determination of airborne hexavalent chromium, Cr(Ⅵ), in a field plating operation. The procedures of this new method (Shin & Paik's Method) are as the following: Airborne hexavalent chromium is collected on polyvinyl chloride (PVC) filter according to the National Institute iota Occupational Safety and Health (NIOSH) Method 7600, and the filler sample is placed in a screw-capped vial and soaked with 2% NaOH/3% Na₂CO₃ solution immediately after sampling. The Cr(Ⅵ) sample is analyzed by ion chromatography/visible spectrophotometry (IC/VS) according to the U.S. Environmental Protection Agency (EPA) Method 218.6. The airborne Cr(Ⅵ) concentrations measured by this method were compared with those determined by three reference methods: One (NIOSH/EPA Method) consisted of sampling airborne Cr(Ⅵ) on PVC filters and storing the sample filters in strew-capped vials according to the NIOSH method, and analyzing Cr(Ⅵ) in samples using IC/VS according to the EPA method. The second method (Impinger Method/NaHCO₃) consisted of absorbing airborne Cr(Ⅵ) into 0.02 M NaHCO₃ solution in midget impinger, and analyzing the Cr(Ⅵ) in samples using IC/VS. The third method was the OSHA Method ID-215. Using these four different methods, lour replicates of air samples were collected at an electroplating process and analyzed simultaneously. Two-way ANOVA and paired t-test were used to test difference among values determined by the methods. There was no significant difference and a strong correlation (r²:0.99) between Cr(Ⅵ) concentrations measured by the Shin & Paik's Method and an impinger method (p>0.05). However, Cr(Ⅵ) concentrations determined by Shin & Paik's Method were significant1y different from those by the NIOSH/EPA Method (p<0.05) or the OSHA method (p<0.05). The Cr(Ⅵ) concentrations of Shin & Paik's Method were significantly higher than those of the NIOSH/EPA Method or the OSHA method. This result indicated that the Shin & Paik's Method may prevent Cr(Ⅵ) losses caused by reduction and give more reliable results of airborne Cr(Ⅵ) concentrations in work environments.

Investigation of Antitumor Effects of Sorafenib and Lapatinib Alone and in Combination on MCF-7 Breast Cancer Cells

  • Kacan, Turgut;Altun, Ahmet;Altun, Gulsah Gultekin;Kacan, Selen Baloglu;Sarac, Bulent;Seker, Mehmet Metin;Bahceci, Aykut;Babacan, Nalan
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.7
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    • pp.3185-3189
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    • 2014
  • Background: Breast cancer evolution and tumor progression are controlled by complex interactions between steroid receptors and growth factor receptor signaling. Aberrant growth factor receptor signaling can augment or suppress estrogen receptor function in hormone-dependent breast cancer cells. Thus, we aimed to investigate antitumor effects of sorafenib and lapatinib alone and in combination on MCF-7 breast cancer cells. Materials and Methods: Cytotoxicity of the sorafenib and lapatinib was tested in MCF-7 cells by XTT assays. 50, 25, 12.5 and $6.25{\mu}M$ concentrations of sorafenib and 200, 100, 50 and $25{\mu}M$ concentrations of lapatinib were administered alone and in combination. Results were evaluated as absorbance at 450nM and $IC_{50}$ values are calculated according to the absorbance data Results: Both sorafenib and lapatinib showed concentration dependent cytotoxic effects on MCF-7 cells. Sorafenib exerted cytotoxic effects with an $IC_{50}$ value of $32.0{\mu}M$; in contrast with lapatinib the $IC_{50}$ was $136.6{\mu}M$. When sorafenib and lapatinib combined, lapatinib increased cytotoxic effects of sorafenib at its ineffective concentrations. Also at the concentrations where both drugs had cytotoxic effects, combination show strong anticancer effects and killed approximately 70 percent of breast cancer cells. Conclusions: Combinations of tyrosine kinase inhibitors and cytotoxic agents or molecular targeted therapy has been successful for many types of cancer. The present study shows that both sorafenib and lapatinib alone are effective in the treatment of breast cancer. Also a combination of these two agents may be a promising therapeutic option in treatment of breast cancer.