• Title/Summary/Keyword: Aminoguanidine

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Screening of Korean Herbal Medicines with Inhibitory Activity on Advanced Glycation End Products (AGEs) Formation (II) (한국약용식물의 최종당화산물 생성저해활성 검색 (II))

  • Lee, Yun-Mi;Kim, Young-Sook;Kim, Jong-Min;Jang, Dae-Sik;Kim, Joo-Hwan;Yoo, Jeong-Lim;Kim, Jin-Sook
    • Korean Journal of Pharmacognosy
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    • v.39 no.3
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    • pp.223-227
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    • 2008
  • Advanced glycation end products (AGEs) contribute to the progression of micro and macrovsacular complication of diabetes and therefore present a promising target for therapeutic agents. In this study, 40 Korean herbal medicines have been investigated with an in vitro evaluation system using AGEs inhibitory activity. Of these, 21 herbal medicines $(IC_{50}<50{\mu}g/ml)$ exhibited an inhibitory activity against AGEs formation compared with anminoguanidine $(IC_{50}=72.12{\mu}g/ml)$. Particularly, 7 herbal medicines, Actinidia arguta (root and stem), Crataegus pinnatifida (twig), Camellia japonica (whole), Kalopanax pictus (bark), Lagerstroemia indica (leaf-stem), Reynoutria sachalinensis (root) showed more potent inhibitory activity (approximately 3-10 fold) than the positive control aminoguanidine.

Screening of Herbal Medicines from China with Inhibitory Activity on Advanced Glycation End Products (AGEs) Formation (V) (중국산 약용식물의 최종당화산물 생성저해활성 검색 (V))

  • Kim, Young-Sook;Choi, Sung-Hoon;Kim, Joo-Hwan;Kim, Jin-Sook
    • Korean Journal of Pharmacognosy
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    • v.42 no.1
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    • pp.46-53
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    • 2011
  • Advanced glycation end products (AGEs) have been postulated to play a central role in the development of diabetic complications. A variety of different agents that inhibit AGEs have been under investigation. In this study, 66 herbal medicines from China have been investigated with an in vitro evaluation system using AGEs formation inhibitory activity. Of these, 31 herbal medicines ($IC_{50}$ < $50\;{\mu}g/ml$) were found to have significant AGEs formation inhibitory activity. Particularly, 5 herbal medicines, Camptotheca acuminata (branches and leaves), Quercus franchetii (branches), Camellia pitardii (leaves, branches, and fruits), Antidesma bunius (whole plants), and Loranthus parasiticus (whole plants) showed more potent inhibitory activity (approximately 6-20 fold) than the positive control aminoguanidine ($IC_{50}=52.96\;{\mu}g/ml$).

Screening of Korean Herbal Medicines with Inhibitory Activity on Advanced Glycation End Products Formation (VII) (한국약용식물의 최종당화산물 생성저해활성 검색(VII))

  • Choi, So-Jin;Kim, Young Sook;Song, Yoo Jin;Lee, Yun Mi;Kim, Joo Hwan;Kim, Jin Sook
    • Korean Journal of Pharmacognosy
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    • v.43 no.4
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    • pp.345-351
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    • 2012
  • In this study, 49 Korean herbal medicines have been investigated with an in vitro evaluation system using glycation end products (AGEs) formation inhibitory activity. Of these, 18 herbal medicines ($IC_{50}$ < $50{\mu}g/ml$) were found to have significant AGEs formation inhibitory activity. Of these, five herbal medicines ($IC_{50}$ < $50{\mu}g/ml$) were found to have significant AGEs formation inhibitory activity. Particularly, Mallotus japonicus (twigs and leaves), Rhus javanica (twigs and leaves), Boehmeria nivea (whole plants), Quercus acuta (stems), and Eurya japonica (stems) showed more potent inhibitory activity (approximately 9-37 fold) than the positive control aminoguanidine ($IC_{50}=76.47{\mu}g/ml$).

Phenolic Compounds from the Leaves of Homonoia riparia and their Inhibitory Effects on Advanced Glycation End Product Formation

  • Lee, Ik-Soo;Jung, Seung-Hyun;Kim, Chan-Sik;Kim, Jin Sook
    • Natural Product Sciences
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    • v.23 no.4
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    • pp.274-280
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    • 2017
  • In a search for novel treatments for diabetic complications from natural resources, we found that the ethyl acetate-soluble fraction from the 80% ethanol extract of the leaves of Homonoia riparia has a considerable inhibitory effect on advanced glycation end product (AGE) formation. Bioassay-guided isolation of this fraction resulted in identification of 15 phenolic compounds (1 - 15). These compounds were evaluated in vitro for inhibitory activity against the formation of AGE. The majority of tested compounds, excluding ethyl gallate (15), markedly inhibited AGE formation, with $IC_{50}$ values of $2.2-89.9{\mu}M$, compared with that of the positive control, aminoguanidine ($IC_{50}=962.3{\mu}M$). In addition, the effects of active isolates on the dilation of hyaloid-retinal vessels induced by high glucose (HG) in larval zebrafish was investigated; (-)-epigallocatechin-3-O-gallate (6), corilagin (7), and desmanthine-2 (11) significantly decreased HG-induced dilation of hyaloid-retinal vessels compared with the HG-treated control group.

Effects of Lipopolysaccharide-Induced Heme Oxygenase and Carbon Monoxide Production on the Aortic Contractility (Lipopolysaccharide에 의한 Heme Oxygenase Induction과 Carbon Monoxide생성이 혈관수축력에 미치는 영향)

  • 장우성;손의동;이석용
    • YAKHAK HOEJI
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    • v.45 no.1
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    • pp.78-84
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    • 2001
  • Heme oxygenase is a rate-limiting enzyme in heme catabolism that cleaves heme to form biliverdin, iron, and carbon monoxide. Heme oxygenase-1 is expressed in many types of cells and tissues and is highly induced in response to oxidative stress. Carbon monoxide, one of the products of heme oxygenase, can stimulate soluble guanylate cyclase and dilate the vascular smooth muscle. So, the induction of heme oxygenase by lipopolysaccharide (LPS)-induced oxydative stress and the effect of the resultant carbon monoxide on aortic contractility were examined in this study. Zinc protoporphyrine IX (ZnPP), a inhibitor of heme oxygenase, elicited weak contraction of thoracic aortic ring, and this effect was more potent in aorta of LPS-treated rats than control and was blocked by methylene blue. The hyperreactivity to ZnPP in LPS-treated group was blocked by co-treatment with aminoguanidine. In the aortic ring of LPS-treated rats, ZnPP didn't change the vasoreactivity to phenylephrine or acetylcholine. ZnPP elicited hyper-tensive effect in concious rats, and pretreatment with LPS did not affect this effect. Prazosin significantly diminished the hypertensive effect of ZnPP. These results indicate that LPS induced heme oxygenase in aotra, and the resultant carbon monoxide diminished the aortic reactivity to vasoconstrictor.

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Constituents of the Roots of Pueraria Iobata Inhibit Formation of Advanced Glycation End Products (AGEs)

  • Kim, Jong-Min;Lee, Yun-Mi;Lee, Ga-Young;Jang, Dae-Sik;Bae, Ki-Hwan;Kim, Jin-Sook
    • Archives of Pharmacal Research
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    • v.29 no.10
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    • pp.821-825
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    • 2006
  • Two isoflavone C-glucosides, puerarin (1) and PG-3 (2), a but-2-enolide, $({\pm})-puerol$ B (3), two isoflavone O-glucosides, daidzin (4) and genistin (5), and three pterocarpans, (-)-medicarpin (6), (-)-glycinol (7) and (-)-tuberosin (8), were isolated from a MeOH extract of the roots of Pueraria Iobata, using an in vitro bioassay based on the inhibition of the formation of advanced glycation end products (AGEs) to monitor chromatographic fractionation. The structures of 1-8 were determined by spectroscopic data interpretation, particularly by 1D- and 2D-NMR studies, and by comparison of these data with values in the literature. All of the isolates (1-8) were evaluated for their inhibitory activity on AGEs formation in vitro. Of these, puerarin (1), PG-3 (2), and $({\pm})-puerol$ B (3) exhibited more potent inhibitory activity than the positive control aminoguanidine.

Nitric oxide induced by Indian ginseng root extract inhibits Infectious Bursal Disease virus in chicken embryo fibroblasts in vitro

  • Ganguly, Bhaskar;Umapathi, Vijaypillai;Rastogi, Sunil Kumar
    • Journal of Animal Science and Technology
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    • v.60 no.1
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    • pp.2.1-2.5
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    • 2018
  • Infectious Bursal Disease is a severe viral disease of chicken responsible for serious economic losses to poultry farmers. The causative agent, Infectious Bursal Disease virus, is inhibited by nitric oxide. Root extract of the Indian ginseng, Withania somnifera, inhibits Infectious Bursal Disease virus in vitro. Also, Withania somnifera root extract is known to induce nitric oxide production in vitro. Therefore, the present study was undertaken to determine if the inhibitory activity of Withania somnifera against Infectious Bursal Disease virus was based on the production of nitric oxide. We show that besides other mechanisms, the inhibition of Infectious Bursal Disease virus by Withania somnifera involves the production of nitric oxide. Our results also highlight the paradoxical role of nitric oxide in the pathogenesis of Infectious Bursal Disease.

Effect of Immunosuppressants on Lipopolysaccharide-Induced Changes of Nitric Oxide Synthase Activity in Liver and Brain of Mice (면역억제제가 Lipopolysaccharide에 의한 생쥐의 간 및 뇌조직의 Nitric Oxide Synthase 활성도의 변화에 미치는 영향)

  • Min, Byung-Woo;Han, Hyng-Soo;Park, Jung-Sook;Kim, Choong-Young
    • The Korean Journal of Pharmacology
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    • v.31 no.2
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    • pp.233-239
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    • 1995
  • To verify the effect of immunosuppressants on the endotoxin-induced increase in iNOS activity, the action of immunosuppressants, dexamethasone (1.5 mg/kg), azathioprine (5 mg/kg/day) and cyclosporine (10 mg/kg), were evaluated in mice pretreated with LPS. The intraperitoneal injection of lipopolysaccharide (10 mg/kg) increased the nitric oxide synthase (NOS) activity in the brain and liver to maximum at 1 and 3 hours, respectively. The increase in NOS activity was blocked by the treatment with NOS inhibitor, LNAME(300 mg/kg) and aminoguanidine(100 mg/kg); a protein inhibitor, cycloheximide (10 mg/kg); and a transcription inhibitor of inducible NOS(iNOS), dexamethasone(1.5 mg/kg). Immunosuppressants, azathioprine (5 mg/kg) and cyclosporine (10 mg/kg), effectively blocked the increase in NOS activity. These results suggest that iNOS expression plays an important role in LPS-induced the increase in NOS activity and that immunosuppressants can be used as candidate for therapeutic agents in endotoxemia.

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Effects of Oxidative Stress on the Expression of Aldose Reductase in Vascular Smooth Muscle Cells

  • Kim, Hyo-Jung;Chang, Ki-Churl;Seo, Han-Geuk
    • The Korean Journal of Physiology and Pharmacology
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    • v.5 no.3
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    • pp.271-278
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    • 2001
  • Oxidative stress and methylglyoxal (MG), a reactive dicarbonyl metabolites produced by enzymatic and non-enzymatic reaction of normal metabolism, induced aldose reductase (AR) expression in rat aortic smooth muscle cells (SMC). AR expression was induced in a time-dependent manner and reached at a maximum of 4.5-fold in 12 h of MG treatment. This effect of MG was completely abolished by cyclohemide and actinomycin D treatment suggesting AR was synthesized by de novo pathway. Pretreatment of the SMC with N-acetyl-L-cysteine significantly down-regulated the MG-induced AR mRNA. Furthermore, DL-Buthionine-(S,R)-sulfoximine, a reagent which depletes intracellular glutathione levels, increased the levels of MG-induced AR mRNA. These results indicated that MG induces AR mRNA by increasing the intracellular peroxide levels. Aminoguanidine, a scanvenger of dicarbonyl, significantly down-regulated the MG-induced AR mRNA. In addition, the inhibition of AR activities with statil, an AR inhibitor, enhanced the cytotoxic effect of MG on SMC under normal glucose, suggesting a protective role of AR against MG-induced cell damages. These results imply that the induction of AR by MG may contribute to an important cellular detoxification of reactive aldehyde compounds generated under oxidative stress in extrahepatic tissues.

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Screening of Korean Herbal Medicines with Inhibitory Activity on Advanced Glycation End Products Formation (IX) (한국약용식물의 최종당화산물 생성저해활성 검색 (IX))

  • Lee, Yun Mi;Kim, Young Sook;Kim, Joo Hwan;Kim, Jin Sook
    • Korean Journal of Pharmacognosy
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    • v.44 no.3
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    • pp.298-304
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    • 2013
  • In this study, 64 Korean herbal medicines have been investigated with an in vitro evaluation systems using glycation end products (AGEs) formation inhibitory activity. Of these, 30 herbal medicines ($IC_{50}&lt;50{\mu}g/ml$) were found to have significant AGEs formation inhibitory activity. Of these, four herbal medicines ($IC_{50}&lt;5{\mu}g/ml$) were found to have significant AGEs formation inhibitory activity. Particularly, Cornus controversa (branches and leaves), Acer ginnala (stems and leaves), Platycarya strobilacea (flowers) and Picrasma quassioides (stems), showed more potent inhibitory activity (approximately 17-27 fold) than the positive control aminoguanidine ($IC_{50}=77.04{\mu}g/ml$).