• Title/Summary/Keyword: inhibitory index

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Comparison of Ingredient and Efficacy of Galgeun-tang (Gegen-tang) Mix Extract Powder and Decoction (갈근탕 혼합단미엑스제 및 전탕액의 성분 및 생리활성 비교 연구)

  • Kim, Jung Ok;Kim, Se Jin;Kim, Jong Beom;Nam, Won Hee;Lee, Ji Beom;Lee, Hwa Dong
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.33 no.1
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    • pp.39-47
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    • 2019
  • Galgeun-tang (GGT) is a traditional herbal medicine generally used to treat cold, fever, headache, migraine and convulsion. To investigate the difference of ingredient and efficacy of GGT according to production method, mix extract powder and decoction, the quantities of index components, antioxidant and anti-inflammatory effects of two kinds of GGT formulation were compared. The contents of ten index components were simultaneously analyzed with HPLC. A HPLC method was developed and validated for the simultaneous determination. The GGT mix extract powder contained higher puerarin and daidzin content than the decoction, while the GGT decoction contained higher cinnamic acid and glycyrrhizic acid content than the mix extract powder. But ingredient of GGT mix extract powder and decoction was statistically very similar (r=0.8335). GGT decoction showed higher antioxidant effect than GGT mix extract powder, but the difference was low. The patterns of productions for NO, iNOS, COX-2, TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 were decreased along the increasing dose of GGT formulation in LPS-induced RAW 264.7 macrophages. The inhibitory effects on NO, iNOS, COX-2, IL-$1{\beta}$ and IL-6 in Raw 264.7 cell were very similar to each other. The results obtained in this study could be used as fundamental data for verifying the equivalence and effectiveness of the herbal medicines.

Inhibitory Effects of Eel (Anguilla japonica) Extracted Carnosine on Protein Glycation (뱀장어(Anguilla japonica)로부터 추출된 Carnosine의 단백질당화 억제효과)

  • Song, Ho-Su;Lee, Keun-Tai;Park, Seong-Min;Kang, Ok-Ju
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.42 no.2
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    • pp.104-108
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    • 2009
  • Glycation and oxidation induce formation of carbonyl (CO) groups in proteins, which can be used to develop an index of cellular aging. Methyl glyoxal (MG) and hypochlorite anions are deleterious products of oxygen free-radical reaction. The effects of eel carnosine on protein modification mediated by MG and hypochlorite were studied. MG and hypochlorite induced formation of carbonyl groups with high molecular weight and cross-linked forms of ovalbumin. The presence of eel carnosine effectively inhibited these modifications in a concentration-dependent manner. Imidazole ring in eel carnosine might have a primary role in inhibition of protein glycation. Our data suggests that the eel carnosine may be useful as a "natural" anti-glycating agents.

Antioxidative Activity and Irritation Response of Lespedeza bicolor

  • Lee Yang-Suk;Chang Zhiqiang;Park Seung-Chun;Rim Nac-Ryong;Kim Nam-Woo
    • Toxicological Research
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    • v.21 no.2
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    • pp.115-119
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    • 2005
  • In the present study, we evaluated the free radical scavenging and xanthine oxidase inhibitory activities exhibited by extracts obtained from the dried stems (and leaves) of Lespedeza bicolor We also assessed its potential irritation activities with regard to cosmetic use. When the DPPH radical scavenging activities of L. bicolor were assessed at six different concentrations (0, 50, 100, 250, 500 and 1000 ${\mu}g/ml$), the concentration of L. bicolor required to inhibit DPPH radical formation by $50\%$ was found to be $164.90{\mu}g/ml$. The effects of L. bicolor on the inhibition of xanthine oxidase were determined at seven different concentrations. The $50\%$ effective concentration was found to be $282.75{\mu}g/ml$. In the skin irritation test, all animals survived for the duration of the study, and all exhibited normal gains in body weight. The control sites exhibited no response to the control procedures. No edema, erythema, or eschar formation was observed in any of the tested rabbits. In the ocular irritation study, all of the rabbit eyes remained normal. In summary, L. bicolor extracts were considered to be non-irritating to the skin and eye.

Antioxidative Activity and Anti-inflammatory Effects on the Murine Macrophages of Methanol Extracts of Amphibians

  • Kim, Sang-Bum;Chang, Min-Ho;Han, Sang-Hyun;Oh, Hong-Shik
    • Korean Journal of Environmental Biology
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    • v.30 no.3
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    • pp.157-163
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    • 2012
  • Oxidative stress has been reported to be one of causes of neuritis. This study examined antioxidative activities of methanol extracts of six amphibian species known to be medicinal animals (Rana catesbeiana, R. coreana, R. rugosa, R. dybowskii, R. nigromaculata, and Hyla japonica) and investigated their effects of inhibiting nitric oxide (NO) production and cytotoxicity on the murine macrophage RAW264.7 cells. As inflammation is closely associated with reactive oxygen species, assays on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, xanthine oxidase inhibitory activity, superoxide anion radical scavenging activity and NO scavenging activity of the extracts of the six species were performed to investigate their antioxidative activity. The results obtained were as follows; All extracts showed antioxidative activity, and the activity of R. dybowskii was the highest in comparison among those. Anti-inflammatory effects of the extracts were also examined, the five extracts except that of R. rugosa did not show cytotoxicity for RAW264.7 cells at the maximal concentration ($1,000{\mu}g\;mL^{-1}$). Selectivity index, meaning NO scavenging activity compared to cytotoxicity, showed the highest level in the extract of R. dybowskii. These results will be very useful basic data for future studies on prevention and treatment of human diseases to understand the biological roles of amphibian extracts throughout the antioxidative or anti-inflammatory pathways.

Evaluation of Cigarette Quality by Use of ??1-Protease Inhibitor (단백질 분해효소억제제를 이용한 담배의 품질평가)

  • 손형옥;임흥빈;이영구;이동욱;김용태
    • Journal of the Korean Society of Tobacco Science
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    • v.13 no.2
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    • pp.27-33
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    • 1991
  • Current studies indicated that emphysema in smokers might be due, in part, to the local suppression of G, -protease inhibitor(u, -Pl) in lung by reactive oxygen species in cigarette smoke or smoke-activated lung neutrophiles. In the present works, we examined the possibility that a measure which inactivated $\alpha$l-Pl by cigarette smoke could be an alternative method to evaluate the cigarette quality, In order to determine the inactivation of $\alpha$1, -Pl, trypsin inhibitory capacity(TIC) was assayed. A rapid loss of $\alpha$1, -Pl activity occurred when $\alpha$1-Pl solutions was exposed the gas phase or total particulate matter(TPM) obtained from various brands. The inactivation of $\alpha$1-Pl by gas phase was dependent upon the number of puffs and the age of the smoke. However, that by TPM was rather decreased since 2 puffs and also showed no more change over 24hrs after exposing. Inactivation of $\alpha$1-Pl determined by our suggested method(5 puffs, 24hours of aging after exposing) using various commercial cigarettes exhibited that high tar brands has inactivated it more strongly than low tar cigarettes. But the ability of some brands to inactivate $\alpha$1-Pl does not correlate with the content of tar or nicotine. These results so여esc that the degree of $\alpha$1-Pl inactivation by cigarette smoke may be a useful index for the evaluation of cigarette quality and that it should be also contribute to the manufacture of less hazardous cigarettes.

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Pharmacodynamics of florfenicol alone and in combination with amoxicillin or cefuroxime against pathogenic bacteria of fish origin (Florfenicol-amoxicillin 혹은 florfenicol-cefuroxime 병용투여시 어류 병원성 세균에 대한 약역학)

  • Lee, Eun-Mi;Choi, Myung-Jin;Lee, Seung-Jin;Park, Seung-Chun
    • Korean Journal of Veterinary Research
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    • v.50 no.4
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    • pp.279-284
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    • 2010
  • Combination therapy of antibiotics is leading to improved efficacy or safety profiles with decrease emergence of bacterial resistance. Because of this benefit, many of antibacterial combinations have been used in veterinary practice for the past few decades. The purpose of this study was to examine the in vitro activity of an amoxicillin alone and in combination with other antibiotics against pathogenic bacteria of fish origin. Based on the fractional inhibitory concentration (FIC) index (FIC $$\leq_-$$ 0.5), a synergistic interaction was shown in combination of florfenicol with amoxicillin or cefuroxime. The combination of florfenicol and amoxillin showed higher antibacterial activity than that of florfenicol and cefuroxime. Ratio of amoxicillin and florfenicol in combination was 1 : 1, which showed the antibacterial activity against bacterial isolates of fish as compared with other ratios. A synergetic effect of the combination (amoxicillin and florfenicol) was further confirmed in the time-kill curve study. The study showed a better in vitro antibacterial activity of a 1 : 1 combination of amoxicillin and florfenicol than the individual antibacterial against bacterial isolates of fish. In conclusion, the combination of florfenicol and amoxicillin may serve as a potential antibacterial therapy in fishes infected pathogenic bacteria.

Chitosan-Based Film of Tyrothricin for Enhanced Antimicrobial Activity against Common Skin Pathogens Including Staphylococcus aureus

  • Han, Sang Duk;Sung, Hyun Jung;Lee, Ga Hyeon;Jun, Joon-Ho;Son, Miwon;Kang, Myung Joo
    • Journal of Microbiology and Biotechnology
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    • v.26 no.5
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    • pp.953-958
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    • 2016
  • Chitosan-based film-forming gel is regarded as a promising vehicle for topical delivery of antimicrobial agents to skin wounds, since it protects from microbial infection and the cationic polymer itself possesses antibacterial activity. In this study, possible synergistic interaction against common skin pathogens between the cationic polymer and tyrothricin (TRC), a cyclic polypeptide antibiotic, was investigated, by determining the concentration to inhibit 90% of bacterial isolates (MIC). The addition of the polysaccharide to TRC dramatically reduced the MIC values of TRC by 1/33 and 1/4 against both methicillin-resistant and methicillin-susceptible Staphylococcus aureus, respectively. The synergism of TRC and chitosan combination against both strains was demonstrated by the checkerboard method, with a fractional inhibitory concentration index below 0.5. Moreover, co-treatment of TRC and chitosan exhibited antibacterial activity against Pseudomonas aeruginosa, due to the antibacterial activity of chitosan, whereas TRC itself did not inhibit the gram-negative bacterial growth. These findings suggested that the use of chitosan-based film for topical delivery of TRC could be an alternative to improve TRC antimicrobial activity against strains that are abundant in skin wounds.

Evaluation of Ciclopirox as a Virulence-modifying Agent Against Multidrug Resistant Pseudomonas aeruginosa Clinical Isolates from Egypt

  • Zakaria, Azza S.;Edward, Eva A.;Mohamed, Nelly M.
    • Microbiology and Biotechnology Letters
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    • v.47 no.4
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    • pp.651-661
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    • 2019
  • Targeting the pathogen viability using drugs is associated with development of drug resistance due to selective pressure. Hence, there is an increased interest in developing agents that target bacterial virulence. In this study, the inhibitory effect of ciclopirox, an antifungal agent with iron chelation potential, on the microbial virulence factors was evaluated in 26 clinical MDR Pseudomonas aeruginosa isolates collected from Alexandria Main University Hospital, a tertiary hospital in Egypt. Treatment with 9 ㎍/ml ciclopirox inhibited the hemolytic activity in 70% isolates, reduced pyocyanin production, decreased protease secretion in 46% isolates, lowered twitching and swarming motility, and decreased biofilm formation by 1.5- to 4.5-fold. The quantitative real-time PCR analysis revealed that treatment with ciclopirox downregulated the expression levels of alkaline protease (aprA) and pyocyanin (phzA1). Ciclopirox is used to treat hematological malignancies and the systemic administration of ciclopirox is reported to have adequate oral absorption with a satisfactory drug safety profile. It is important to calculate the appropriate clinical dose and therapeutic index to reposition ciclopirox from a topical antifungal agent to a promising virulence-modifying agent agent against P. aeruginosa, a problematic Gram-negative pathogen.

An in silico Appraisal to Identify High Affinity Anti-Apoptotic Synthetic Tetrapeptide Inhibitors Targeting the Mammalian Caspase 3 Enzyme

  • Kelotra, Seema;Jain, Meeta;Kelotra, Ankit;Jain, Ish;Bandaru, Srinivas;Nayarisseri, Anuraj;Bidwai, Anil
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.23
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    • pp.10137-10142
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    • 2015
  • Apoptosis is a general phenomenon of all multicellular organisms and caspases form a group of important proteins central to suicide of cells. Pathologies like cancer, Myocardial infarction, Stroke, Sepsis, Alzheimer's, Psoriasis, Parkinson and Huntington diseases are often associated with change in caspase 3 mediated apoptosis and therefore, caspases may serve as potential inhibitory targets for drug development. In the present study, two series of synthetic acetylated tetrapeptides containing aldehyde and fluromethyl keto groups respectively at the C terminus were proposed. All these compounds were evaluated for binding affinity against caspase 3 structure. In series 1 compound Ac-DEHD-CHO demonstrated appreciable and high binding affinity (Rerank Score: -138.899) against caspase 3. While in series 2 it was Ac-WEVD-FMK which showed higher binding affinity (Rerank Score: -139.317). Further these two compounds met ADMET properties and demonstrated to be non-toxic.

Alleviative Effects of Jujube Water Extract on the Inflammation and Barrier Damage in Hairless Mice Skin (Hairless 마우스에서 대추 열수추출물의 피부내 염증 및 장벽 손상 완화 효과)

  • Choi, So-Young;Kim, Young-Chul
    • Environmental Analysis Health and Toxicology
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    • v.24 no.4
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    • pp.351-357
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    • 2009
  • To investigate the alleviative effects of jujube water extract (JWE) on the inflammation and skin barrier damage, both the irradiation of UVB and the application of squalene monohydroperoxide (Sq-OOH) were applied to the back skin of experimental animals for 4 weeks. And at the same time experimental materials were applied topically. Six weeks female SKH-1 hairless mice were divided into five groups (five animals for each group) including normal (N; saline), control (C; UVB+Sq-OOH+saline), vehicle control (VC; UVB+Sq-OOH+vehicle), positive control (PC; UVB+Sq-OOH+0.01% retinoic acid) and experimental (E; UVB+Sq-OOH+JWE) groups. The skin erythema index in the E group was significantly low compared to the C group (p<0.05). Lipid (p<0.05) and water (p<0.01) capacities in the E group were significantly high compared to the C group. In comparison with the C group, E group showed a relatively well preserved lipid lamellae in the epidermis and a relatively much less infiltration of mast cells in the dermis or hypodermis. As for the both absolute and relative weights of the spleen, PC group were significantly higher than the other groups. These results suggest that JWE have a considerably inhibitory effect on the inflammation and the skin barrier damage induced by UVB irradiation and Sq-OOH application.