• Title/Summary/Keyword: inhibitory index

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Effects of Korean and Chinese Crataegi Fructrus on the Antioxidant Activity and Antiproliferation of Cancer Cells (한국산과 중국산 산사의 항산화 활성 및 암세포 증식 억제효과)

  • Park, Yonghyun;Lee, Hyun-Joo;Lee, Jae-Joon
    • The Korean Journal of Community Living Science
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    • v.26 no.1
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    • pp.103-113
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    • 2015
  • This study examines the effects of Korean Crataegi fructrus(KCF) and Chinese Crataegi fructrus(CCF) on the antioxidative activity and antiproliferation of human cancer cells(HCT-116 human colon, Hep G2 human liver, and A549 human lung cancer cells). The total polyphenol and flavonoid contents, and antioxidative index of the Crataegi fructrus ethanol extracts were significantly higher in KCF than in CCF. The DPPH radical-scavenging activity of the KCF ethanol extract was 82.26%(1000 ppm), and that of the CCF ethanol extract was 77.64%. Antiproliferation effects of 80% ethanol extracts of KCF and CCF on human cancer cells(HCT-116, Hep G2 and A549) increased in a dose-dependent manner. Inhibitory effects of KFC on HCT-116 and A549 cells were greater than those of CCF. The results suggest that ethanol extracts of Crataegi fructrus have antioxidative and hyperplasia inhibition effects on human cancer cells.

Administration of Aqueous Extract of Schizandra chinensis Fruit Inhibits the Experimental Colitis in Mice

  • Kang, Chon-Sik;Tae, Jin;Ham, Seong-Ho;Kim, Dae-Ki;Lee, Young-Mi;Lee, Kang-Soo;Yun, Yong-Gab
    • Natural Product Sciences
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    • v.13 no.1
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    • pp.78-84
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    • 2007
  • Schizandra chinensis fruits (SC) have been used as a traditional Oriental medicine for treatments of many stress-induced diseases. In the present study, we investigated the protective effect of SC aqueous extract(SC-Ex) in the inflammatory diseases of intestine using a mouse model of ulcerative colitis. An experimental colitis was induced by daily treatment with 5% dextran sulfate sodium (DSS). SC-Ex was orally administered from day 2 of DSS treatment in a dose-dependent manner. Administration of SC-Ex reduced significantly clinic signs of DSS-induced colitis, including body weight loss, shorten colon length, increased disease activity index, and histological colon injury. Moreover, SC-Ex suppressed significantly not only the activities of myeloperoxidase (MPO) and chymase, but also the expressions of $TNF-{\acute{a}}$ and COX-2 in DSS-treated colon tissues. Inhibitory effect of SC-Ex was effective at a dose over 20 mg/kg. Our results indicate that SC-Ex may possess therapeutic effect on the development of DSS-induced colitis.

Luteolin and Chicoric Acid, Two Major Constituents of Dandelion Leaf, Inhibit Nitric Oxide and Lipid Peroxide Formation in Lipopolysaccharide-Stimulated RAW 264.7 Cells

  • Park, Chung-Mu;Park, Ji-Young;Song, Young-Sun
    • Preventive Nutrition and Food Science
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    • v.15 no.2
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    • pp.92-97
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    • 2010
  • Luteolin and chicoric acid are the most abundant phytochemicals in dandelion (Taraxacum officinale) leaf. In this study, four kinds of extraction methods [hot water, ambient temperature (AT) water, ethanol, and methanol] were applied to analyze the contents of both phytochemicals and verify their anti-inflammatory and antioxidative activities. The methanol extract showed the most potent nitric oxide (NO) inhibitory effect. The luteolin and chicoric acid concentrations were 3.42 and $12.86\;{\mu}g/g$ dandelion leaf in the methanol extract. The NO-suppressive effect of luteolin and chicoric acid was identified in a dose-dependent manner with $IC_{50}$ values of $21.2\;{\mu}M$ and $283.6\;{\mu}M$, respectively, in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells without cytotoxicity. Malondialdehyde (MDA) concentration, as an index for free radical injury on cell membrane, was also dose-dependently inhibited by the two compounds. The suppressive effect was further examined using mRNA and protein expression levels, which were attributable to the inhibition of inducible nitric oxide synthase (iNOS). These results suggest that two phytochemicals in dandelion leaf, luteolin and chicoric acid, may play an important role in the amelioration of LPS-induced oxidative stress and inflammation.

Effects of Lepidii Semen on Acute Edematous Lung Injury Induced by Skin Burn

  • Myoung-Je Cho;Hyun Gug Cho
    • Biomedical Science Letters
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    • v.9 no.1
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    • pp.37-42
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    • 2003
  • The present study was conducted to determine whether administration of heat extract of Lepidii Semen has an inhibitory effect on neutrophil-derived oxidative injury following dermal scald burn in rats. Acute lung injury was induced by scald burn (15% of TBSA) in rats. To identify acute edematous lung injury, protein concentrations and numbers of polymorphonuclear leukocytes were measured in bronchoalveolar lavage (BAL) at 5 h after skin burn. In addition, the level of lung KC (neutrophil chemoattractant cytokine) and activity of lung myeloperoxidase (MPO) were measured, and histopathological changes were observed as well. Lung weight and concentration of BAL protein, the index of lung injury, were clearly increased at 5 h postburn compared with those of sham-operated group. Administration of heat extract of Lepidii Semen after scald burn inhibited the production of KC in lung tissue and decreased the activity of lung MPO related to infiltration of neutrophils. In histopathological changes in lung tissue, infiltration of inflammatory cells and pulmonary edema induced by skin burn were decreased by administration of heat extract of Lepidii Semen after scald burn. These results suggest that Lepidii Semen may be an effective medical stuff for acute lung injury induced by skin burn.

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Improvement of Rheological and Functional Properties of Salmon FPC by Enzymatic Partial Hydrolysis 2. Rheological and functional properties of salmon FPC hydrolysates

  • LEE Jong-Ho;LEE Keun-Tai;PARK Seong-Min;PARK Chan-kyu
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.30 no.6
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    • pp.956-963
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    • 1997
  • To enhance application of FPC in food industry, salmon FPC hydrolysates were produced and their functional properties were investigated. Hydrolysates of salmon FPC showed high solubilities ranged from approximately $80\~95\%$. Emulsifying activity index (EAI) values of hydrolysates were higher than that of egg white, however sugar ester showed the highest EAI value of 32.5. Though sugar ester had the best emulsifying stability value $({\Delta}EAI)$ of 9.65, hydrolysates showed better ${\Delta}EAI$ value than that of egg white. Foam Activity of hydrolysates was predominantly better than those of controls and also foam stability value showed similiar trend. Osmolality of hydrolysates was increased with the increase of degree of hydrolysis (DH) and concentration of protein, but it showed very lower osmolality than that of NaCl. Flow property of hydrolysates showed different upward-downward curves, and hysteresis loop increased with the increase of DH. ACE inhibitory activity showed similiar value ranged from $21.1\~24\%$ at all DH values.

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Antibacterial Effect of Amentoflavone and Its Synergistic Effect with Antibiotics

  • Hwang, Ji Hong;Choi, Hyemin;Woo, Eun-Rhan;Lee, Dong Gun
    • Journal of Microbiology and Biotechnology
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    • v.23 no.7
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    • pp.953-958
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    • 2013
  • Selaginella tamariscina is a traditional herb used in medicine. Phytochemical amentoflavone, a biflavonoid class of flavonoids, was isolated from the plant of Selaginella tamariscina. In this study, the antibacterial effects and combination effects of amentoflavone and conventional antibiotics such as ampicillin, cefotaxime, and chloramphenicol were investigated. These results showed that amentoflavone had a considerable antibacterial effect and synergistic interaction with antibiotics against various bacterial strains (fractional inhibitory concentration index ${\leq}$ 0.5), except for Streptococcus mutans. To study the mechanism(s) involved in the synergistic activities between amentoflavone and antibiotics, we detected hydroxyl radical formation using 3'-(p-hydroxyphenyl) fluorescein and measured the $NAD^+/NADH$ ratio by $NAD^+$ cycling assay. The results indicated that the formation of hydroxyl radical would be a cause of the synergistic effect and that this oxidative stress originated from a transient NADH depletion. This study suggests that amentoflavone synergizes with antibiotics and has potential as a therapeutic agent for antimicrobial chemotherapy.

Comparative Molecular Similarity Index Analysis on 2-(indol-5-yl)thiazolederivatives as Xanthine Oxidase(XO)inhibitors

  • Nagarajan, Santhosh Kumar;Madhavan, Thirumurthy
    • Journal of Integrative Natural Science
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    • v.9 no.3
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    • pp.190-198
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    • 2016
  • Xanthine Oxidase is an enzyme, which oxidizes hypoxanthine to xanthine, and xanthine to uric acid. It is widely distributed throughout various organsincluding the liver, gut, lung, kidney, heart, brain and plasma. It is involved in gout pathogenesis. In this study, we have performed Comparative Molecular Field Analysis (CoMSIA) on a series of 2-(indol-5-yl) thiazole derivatives as xanthine oxidase (XO) inhibitors to identify the structural variations with their inhibitory activities. Ligand based CoMSIA models were generated based on atom-by-atom matching alignment. In atom-by-atom matching, the bioactive conformation of highly active molecule 11 was generated using systematic search. Compounds were aligned using the bioactive conformation and it is used for model generation. Different CoMSIA models were generated using different alignments and the best model yielded across-validated $q^2$ of 0.698 with five components and non-cross-validated correlation coefficient ($r^2$) of 0.992 with Fisher value as 236.431, and an estimated standard error of 0.068. The predictive ability of the best CoMSIA models was found to be $r{^2}_{pred}$ 0.653. The study revealed the important structural features required for the biological activity of the inhibitors and could provide useful for the designing of novel and potent drugs for the inhibition of Xanthine oxidase.

In Vivo Screening Method for the Anti-AIDS Drugs in the BALB/c Mice Inoculated by Anemia Strain of Friend Virus (Friend Anemia Virus에 감염된 BALB/c 생쥐를 이용한 항AIDS약물의 생체내 약효검색)

  • 안형수;염윤기;장영수
    • YAKHAK HOEJI
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    • v.39 no.6
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    • pp.622-630
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    • 1995
  • Inoculation of Friend anemia virus, which was a Kind of retro virus such as HIV, results splenomegaly, anemia, the increase of WBC counts and reverse transcriptase activity in serum. These results were due to the inhibition of the differentiation of erythroid progenitor cell by the FVA at the spleen. Using these as index of antiviral effects, we pursued the establishment of in vivo screening method for the new anti-ADS drugs. Among zidovudine, didanosine and zalcitabine, which were already approved as anti-AIDS drugs, treatment of zidovudine for 18 days in BALB/c mice inoculated with Friend anemia virus resulted the most potent inhibitory effects on the splenomegaly, the increase of WBC counts and reverse transcriptase activity, but did not recovered the anemia due to the tomcity of zidovudhie itself on the bone marrow. The antiviral effects of zidovudine was reduced in case of zidovudine treatment 7 days after Friend anemia virus inoculation. These results suggested that the sooner treatment of zidovudine would be better improved when the virus was inoculated. Human recombinant interferon itself .alpha. did not showed the antiviral activity against Friend anemia virus and did not also affected the antiviral activity of zidovudine. These results suggested that Friend anemia virus would be used as a tool in vivo screening method for the Lobster of reverse transcriptase.

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Physiological Effects and Utilization of Corbicula elatior Products -Effect of Cockle Extracts on Carcinogen-induced Cytotoxicity and Immune REsponse RElated to Its Antitumor Activity- (재첩가공품의 생리학적 특성과 이용 -재첩추출물의 항암효과와 면역활성증강 효과-)

  • 서재수;최명원;전순실;장명웅
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.29 no.2
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    • pp.235-240
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    • 2000
  • Inhibitory effects of cockle extracts on carcinogen-induced cytotoxicity in C3H/10T1/2 cells were studied. Soup (62$\mu\textrm{g}$/mL), solubility (28$\mu\textrm{g}$/mL) and liposolubility (9 $\mu\textrm{g}$/mL) of the cockle inhibited 3-methyl-cholanthrene(MCA)-induced cytotoxicity in C3H/10T1/2 cells by 53 and 94%, respectively. These results suggest that the extracts cockle might have anticarcinogen-induced cytotoxicity of C3H/10T1/2 cells. The effects of cockle extracts on the immune response related to its antitumor activity in vitro and in vivo were investigated. The cockle extracts showed a direct cytotoxic effect on sarcoma-180 cells, tumor cells in vitro. Soup (0.49 mg/mL), solubility (0.11 mg/mL) and liposolubiliy (0.05 mg/mL) of the cockle markedly decreased the total numbers of sarcoma-180 cells, but not their viability. The phagocytic acitivity of peritoneal macrophage of mice was significantly augmented by these extracts of the cockle compared with that of control in vivo. These extracts also raised the phagocuytic index, indicating that the number of phagocytize dmicrobes per macrophage increased. Thus, cockle extracts might show a antitumor activity by enhancing the phagocytic cell activities.

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Sclerotiorin: a Novel Azaphilone with Demonstrated Membrane Targeting and DNA Binding Activity against Methicillin-Resistant Staphylococcus aureus

  • Dasagrandhi, Chakradhar;Pandith, Anup;Imran, Khalid
    • Microbiology and Biotechnology Letters
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    • v.48 no.4
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    • pp.429-438
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    • 2020
  • The emergence of multi-drug resistant, pathogenic methicillin-resistant Staphylococcus aureus (MRSA) is a threat to global health and has created a need for novel functional therapeutic agents. In this study, we evaluated the underlying mechanisms of the anti-MRSA effect of an azaphilone pigment, sclerotiorin (SCL) from Penicillium sclerotiorum. The antimicrobial activity of SCL was evaluated using agar disc diffusion, broth microdilution, time-kill assays and biophysical studies. SCL exhibits selective activity against Gram positive bacteria including MRSA (range, MIC = 128-1028 ㎍/ml) and exhibited rapid bactericidal action against MRSA with a > 4 log reduction in colony forming units within three hours of administration. Biophysical studies, using fluorescent probes and laser or electron microscopy, demonstrated a SCL dose-dependent alternation in membrane potential (62.6 ± 5.0.4% inhibition) and integrity (> 95 ± 2.3%), and the release of UV260 absorbing materials within 60 min (up to 3.2 fold increase, p < 0.01) of exposure. Further, SCL localized to the cytoplasm and hydrolyzed plasmid DNA. While in vitro checkerboard studies revealed that SCL potentiated the antimicrobial activity of topical antimicrobials such as polymixin, neomycin, and bacitracin (Fractional Inhibitory Concentration Index range, 0.26-0.37). Taken together these results suggest that SCL targets the membrane and DNA of MRSA to facilitate its anti-MRSA antimicrobial effect.