• Title/Summary/Keyword: medicinal reaction

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Silencing MR-1 attenuates atherosclerosis in ApoE-/- mice induced by angiotensin II through FAK-Akt -mTOR-NF-kappaB signaling pathway

  • Chen, Yixi;Cao, Jianping;Zhao, Qihui;Luo, Haiyong;Wang, Yiguang;Dai, Wenjian
    • The Korean Journal of Physiology and Pharmacology
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    • v.22 no.2
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    • pp.127-134
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    • 2018
  • Myofibrillogenesis regulator-1 (MR-1) is a novel protein involved in cellular proliferation, migration, inflammatory reaction and signal transduction. However, little information is available on the relationship between MR-1 expression and the progression of atherosclerosis. Here we report atheroprotective effects of silencing MR-1 in a model of Ang II-accelerated atherosclerosis, characterized by suppression focal adhesion kinase (FAK) and nuclear factor kappaB ($NF-{\kappa}B$) signaling pathway, and atherosclerotic lesion macrophage content. In this model, administration of the siRNA-MR-1 substantially attenuated Ang II-accelerated atherosclerosis with stabilization of atherosclerotic plaques and inhibited FAK, Akt, mammalian target of rapamycin (mTOR) and NF-kB activation, which was associated with suppression of inflammatory factor and atherogenic gene expression in the artery. In vitro studies demonstrated similar changes in Ang II-treated vascular smooth muscle cells (VSMCs) and macrophages: siRNA-MR-1 inhibited the expression levels of proinflammatory factor. These studies uncover crucial proinflammatory mechanisms of Ang II and highlight actions of silencing MR-1 to inhibit Ang II signaling, which is atheroprotective.

Immunomodulating Activity of Fungal ${\beta}-Glucan$ through Dectin-1 and Toll-like Receptor on Murine Macrophage

  • Kim, Ha-Won
    • 한국약용작물학회:학술대회논문집
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    • 2006.11a
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    • pp.103-115
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    • 2006
  • [ ${\beta}-Glucan$ ] is a glucose polymer that has linkage of ${\beta}-(1,3)$, -(1,4) and -(1,6). As exclusively found in fungal and bacterial cell wall, not in animal, ${\beta}-glucans$ are recognized by innate immune system. Dendritic cells (DC) or macrophages possesses pattern recognition molecule (PRM) for binding ${\beta}-glucans$ as pathogen-associated molecular pattern (PAMP). Recently ${\beta}-glucans$ receptor was cloned from DC and named as dectin-l which belongs to type II C-type lectin family. Human dectin-l is consisted of 7 exons and 6 introns. The polypeptide of dectin-l has 247 amino acids and has cytoplasmic, transmembrane, stalk and carbohydrate recognition domains. Dectin-l could recognize variety of beta-l,3 and/or beta-l,6 glucan linkages, but not alpha-glucans. In our macrophage cell line culture system, dectin-l mRNA was detected in RA W264.7 cells by reverse transcription-polymerase chain reaction (RT-PCR). Dectin-l was also detected in the murine organs of spleen, thymus, lung and intestines. Treatment of RA W264.7 cells with ${\beta}-glucans$ of Ganoderma lucidum (GLG) resulted in increased expression of IL-6 and $TNF-{\alpha}$ in the presence of LPS. However, GLG alone did not increase IL-6 nor $TNF-{\alpha}$ These results suggest that receptor dectin-l cooperate with CD14 to activate signal transduction that is very critical in immunoresponse.

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Synthesis of New 2-Thiouracil-5-Sulfonamide Derivatives with Biological Activity

  • Fathalla, O.A.;Zaghary, W.A.;Radwan, H.H.;Awad, S.M.;Mohamed, M.S.
    • Archives of Pharmacal Research
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    • v.25 no.3
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    • pp.258-269
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    • 2002
  • 2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.

Antioxidative Flavonoids from Leaves of Carthamus tinctorius

  • Lee, Jun-Young;Chang, Eun-Ju;Kim, Hyo-Jin;Park, Jun-Hong;Choi, Sang-Won
    • Archives of Pharmacal Research
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    • v.25 no.3
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    • pp.313-319
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    • 2002
  • A total of eight flavonoids (1-8), including a novel $quercetin-7-o-(6"-o-acetyl)-{\beta}-D-glucopyranoside$ (6) and seven known flavonoids, luteolin (1), quercetin (2), luteolin $7-o-{\beta}-D-glucopyranoside$ (3), $luteolin-7-o-(6"-Ο-acetyl)-{\beta}-D-glucopyranoside$ (4) quercetin $7-o-{\beta}-D-glucopyranoside$ (5), acacetin 7-o-{\beta}-D-glucuronide (7) and apigenin-6-C-{\beta}-D-glucopyrano $syl-8-C-{\beta}-D-glucopyranoside$ (8), have been isolated from the leaves of the safflower (Carthamus tinctorius L.) and identified on the basis of spectroscopic and chemical studies. The antioxidative activity of these flavonoids was evaluated against 2-deoxyribose degradation and rat liver microsomal lipid peroxidation induced by hydroxyl radicals generated via a Fenton-type reaction. Among these flavonoids, luteolin-acetyl-glucoside (4) and quercetin-acetyl-glucoside (6) showed potent antioxidative activities against 2-deoxyribose degradation and lipid peroxidation in rat liver microsomes. Luteolin (1), quercetin (2), and their corresponding glycosides (3 & 5) also exhibited strong antioxidative activity, while acacetin glucuronide (7) and apigenin-6,8-di-C-glucoside (8) were relatively less active.

Apoptosis and Anti-proliferaction by Saussurea lappa and Pharbitis nil in AGS Human Gastric Cancer Cell Line

  • Ko Seong-Gyu;Oh Hee-Rah;Lee Sun-Dong;Hwang Gwi-Seo
    • The Journal of Internal Korean Medicine
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    • v.24 no.1
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    • pp.134-143
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    • 2003
  • Objectives : We performed this study to understand the molecular basis of the antitumor effect of Saussurea lappa, Pharbitis nil, Plantago asiatica and Taraxacum mongolicum, which have been used for cancer treatment in Korean traditional medicine. Design: We analyzed, the effect of these medicinal herbs on proliferation and apoptosis of tumor cells and its association with gene expression, We performed semi-quantitative reverse transcription-polymerase chain reaction(RT-PCR) analysis of cell cycle- and apoptosis-related genes using a gastric cancer cell line AGS. Results : Cell counting assay and $[^3H]thymidine$ uptake analysis showed that Saussurea lappa and Pharbitis nil strongly inhibit cell proliferation of AGS in a dose-dependent manner. Interestingly, gene espression assay revealed that mRNA espression levels of c-Jun, c-Fos, c-Myc, and Cyclin D1 were markedly decreased by Saussurea lappa and Pharbitis nil. Furthermore, Saussurea lappa was identified to activate expression of the p53 tumor suppressor and its downstream effector $p21^{Wafl}$, which leads to $G_1$ cell cycle arrest and apoptosis. These observations suggest that the anticancer effect of Saussurea lappa and Pharbitis nil might be associated with their regulatory capability of tumor-related gene expression.

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Three Intraspecific groups in Korean Isolates of Phytophthora drechsleri Based on PCR-RFLP of Ribosomal DNA (Ribosomal DNA의 PCR-RFLP에 의한 국내산 Phytophthora drechsleri의 3가지 종내그룹)

  • 홍승범;지형진;이승임;고승주;류진창;김인수
    • Korean Journal Plant Pathology
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    • v.14 no.5
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    • pp.519-525
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    • 1998
  • Intraspecific genetic diversity of Korean isolates of Phytophthora drechsleri was investigated based on PCR-RFLP of rDNA along with closely related species in the genus; P. cryptogea, P. melonis, P. erythroseptica, P. cinnamomi, P. cambivora and P. cactorum. Gene regions of nuclear small subunit and internal transcribed spacer (ITS) in rDNA were amplified with polymerase chain reaction and digested with 9 restriction enzymes. Phytophthora species was readily differentiated from each other based on the digestion patterns, however, P. cryptogea was not separable from some isolates of P. drechsleri. Twenty one isolates of P. drechsleri originated from 15 host plants were divided into three distinct groups designated as PdG1, PdG2 and PdG3, respectively. Four isolates in PdG1 were originated from green vegetables and tomato and nine isolates in PdG2 were mainly isolated from medicinal plants. The two groups showed 95.3% homology and four isolates of P. cyptogea came under the groups. However, Eight isolates in PdG3 collected from cucurbits were clearly differentiated from those of PdG1 and PdG2 by 66.5% homology, but completely matched with a Taiwan isolate of P. melonis. Results indicated that three distinct groups exist in Korean isolates of P. drechleri and each group has host preference. In addition, reclassification of the cucurbits isolates are reserved because of their distinct genetic characters from other intraspecific groups in P. drechsleri.

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Characterization of ginseng extracts

  • Woo, Lin-Keun;Han, Byung-Hoon;Baik, Duck-Woo;Park, Dae-Sic
    • YAKHAK HOEJI
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    • v.17 no.3
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    • pp.129-136
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    • 1973
  • In order to establish the chemical standards for the quality control of ginsentgextract, an approach for the assay of sapogenin contents in the part of main roots and fibrous side roots was performed by combination of preparative thin layer chromotographic procedure and vanillin-$H_{2}SO_{4}$ color reaction. The contents of dammarane aglycones as funcction of dammarane glycosides in 80%-EtOH extracts were analyzed by the method from the main roots and fibrous side roots of Korean ginseng grown for 4-6 years. The differences by their grown ages in the contents of dammarane glycosides, in the ratio of panaxadiol to panaxatriol contents, and in the mounts of 80% EtOH extract were not significant in the parts of main roots and fibrous side roots of Korean gingeng. Differences due to the part for medicinal uses were highly significant in all parameters mentioned, showing following results ; in the main roots ; 80% EtOH extract, 12.7-15.7 % : the ratio of aglycone composition, 0.955-1.012 : dammarane glycoside (as diglucoside bases), 1.537-1.863 ; in fibrous isde roots ; 80% EtOH extract, 26.0-26.02% : dammarane glycoside, 4.767-5.641 : the ratio, 1.456-1.50.

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Social Relief Scheme for Serious Adverse Drug Reactions - Lessons from other countries for Korea (외국의 의약품 부작용 피해구제제도 현황과 국내 실시 방안)

  • Park, Sylvia;Chae, Su-Mi
    • Korean Journal of Clinical Pharmacy
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    • v.18 no.1
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    • pp.18-27
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    • 2008
  • This study investigated social relief schemes for serious adverse drug reactions in foreign countries and deduced lessons and implications for Korea to implement the scheme. A social relief scheme for serious adverse drug reactions provides reliefs for diseases and such health effects as disabilities or deaths that were caused by adverse reactions to pharmaceuticals prescribed at hospitals and clinics as well as those purchased at pharmacies notwithstanding their proper use. The US and the UK do not have specific relief schemes for adverse drug reactions but apply rules of strict liability or negligence. New Zealand and Nordic countries provide no-fault compensation schemes for health effects or injuries caused by medical treatments or medicinal products. Japan and Taiwan have operated the schemes since 1980 and 2000, respectively. In designing the scheme in Korea, we suggested that cases eligible for relief be confined to serious adverse reactions such as death or disability and then extended to diseases. It is desirable to encourage the reporting system of adverse drug reactions and quality use of medicines for the relief scheme to work efficiently.

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Anti-inflammatory Properties of Meso-dihydroguaiaretic Acid in Lipopolysaccharide-induced Macrophage

  • Kim, Yong-Jae;Kang, Yeo-Jin;Kim, Tack-Joong
    • Biomedical Science Letters
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    • v.16 no.2
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    • pp.91-95
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    • 2010
  • Meso-dihydroguaiaretic acid (MDGA) is a medicinal herbal product isolated from the bark of Machilus thunbergii Sieb. et Zucc. (Lauraceae). It exhibits a neuroprotective effect and also exerts cytotoxicity to certain cancer cells. In the present study, we investigated whether or not MDGA inhibits inflammatory reaction through the inhibition of nitric oxide (NO) generation. The results showed that MDGA (5~$25 {\mu}M$) inhibited 100 ng/ml lipopolysaccharide (LPS)- induced NO generation in macrophage Raw 264.7 cells in a concentration-dependent manner. We also measured the cytotoxic effects of MDGA on Raw 264.7 cells and found no evidence of cytotoxicity. The inhibition of NO generation by MDGA was consistent with the inhibitory effect on the expression of inducible nitric oxide synthase (iNOS). In addition, MDGA inhibited the LPS-induced gene expression of $interleukin-1{\beta}$ $(IL-1{\beta})$ as well as tumor necrosis $factor-{\alpha}$ $(TNF-{\alpha})$. The present results may provide that MDGA has anti-inflammatory properties through inhibition of the toll-like receptors (TLRs) pathway, and suggest that MDGA can be used as an anti-inflammatory agent.

Impact of Amino-Acid Coating on the Synthesis and Characteristics of Iron-Oxide Nanoparticles (IONs)

  • Ebrahiminezhad, Alireza;Ghasemi, Younes;Rasoul-Amini, Sara;Barar, Jaleh;Davaran, Soodabeh
    • Bulletin of the Korean Chemical Society
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    • v.33 no.12
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    • pp.3957-3962
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    • 2012
  • Iron-oxide nanoparticles (IONs) with biocompatible coatings are the only nanostructural materials which have been approved by the FDA for clinical use. Common biocompatible coatings such as hydrocarbons, polymers, and silica have profound influences on critical characteristics of IONs. Recently, amino acids were introduced as a novel biocompatible coating. In the present study, the effects of amino acids on IONs synthesis and characteristics have been evaluated. Magnetite nanoparticles with L-arginine and L-lysine coatings were synthesised by a coprecipitation reaction in aqueous solvent and their characteristics were compared with naked magnetite nanoparticles. The results showed that amino acids can be a perfect coating for IONs and would increase particle stability without any significant effects on the critical properties of nanoparticles such as particle size and magnetization saturation value.