• Title/Summary/Keyword: pharmaceutical effects

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Anti-stress effects of Urosodeoxycholic acid on the restraint stress in rat

  • Cho, Tai-Soon;Lee, Sun-Mee;Yeom, Je-Ho;Yu, Eun-Joo;Lim, Seung-Wook;Kim, Young-Man;Yu, Young-Hyo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.195-195
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    • 1996
  • 우루소데옥시콜린산을 1% CMC에 현탁하여 25mg/kg 의 농도로 각각 1, 3, 6, 10일간 1일 3회씩 투여한 후. 고정틀에 묶어 고정시키고 4시간 동안 스트레스를 가하였다. 스트레스 부과후 복부를 개복하여 혈액을 채취하고 스트레스지표인 ALP, AST, ALT, LDH를 측정하였다. 한편 일부 혈액은 백혈구, 림프구수를 측정하기 위해 이용되었다. 부신 및 비장을 적출하여 무게를 측정하고 부신은 분쇄하여 아스코르빈산 함량을 정량하였다. 스트레스 부과시간에 따른 백혈구, 림프구수의 변화실험은 별도로 시행하였다.

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Potent inhibition of Lipopolysaccharide-Inducible Nitric Oxide Synthase Expression by Dibenzylbutyrolactone Lignans through Inhibition of I-kB Phosphorylation and of p65 Nuclear Translocation in Macrophages

  • Cho, Min-Kyung;Park, Jung-Won;Jang, Young-Pyo;Kim, Young-Choong;Kim, Sang-Geon
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.05a
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    • pp.139-139
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    • 2001
  • Arctigenin and demethyltraxillagenin, dibenzylbutyrolactone lignans, are phenylpropanoid plant metabolites with antioxidative and anti-inflammatory activities. The effects of arctigenin and demethyltraxillagenin on the nuclear factor-kB (NF-kB)-mediated inducible nitric oxide synthase (iNOS) gene expression were studied in Raw264.7 cells.(omitted)

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Inhibitory effects of new quinone compounds on eNOS activity in rat aorta and nNOS activity in rat brain

  • Yoo, So-Yeon;Seo, Ji-Hui;Ryu, Chung-Kyu;Kim, Hwa-Jung
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.248.3-249
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    • 2002
  • Nitric oxide (NO) has been shown to play an important role in the regulation of vascular tone. platelet function. neurotransmission. and immune function. NO is synthesized from the L-arginine by NO synthase (NOS). Three distinct isoforms of NOS have been identified: calcium/calmodulin-dependent endothelial (eNOS) and neuronal (nNOS) isoforms which are constitutive and produce small quantities of NO, and an inducible isoform (iNOS) which is markedly induced in response to lipopolysaccharide (LPS) or inflammatory cytokines. (omitted)

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Synthesis and Biological Properties of New 5-Cyano-1,1-disubstituted Phthalans for the Treatment of Premature Ejaculation

  • Kim, Dong-Sung;Kang, Kyung-Koo;Lee, Kyung-Seok;Ahn, Byoung-Ok;Yoo, Moo-Hi;Yoon, Seung-Soo
    • Bulletin of the Korean Chemical Society
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    • v.29 no.10
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    • pp.1946-1950
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    • 2008
  • The synthesis of new 5-cyano-1,1-disubstituted phthalans having aromatic and aminoalkyl groups at C-1 position of phthalan ring and their biological evaluation are described. Most compounds exhibited comparable ejaculation-retarding effects to citalopram. Of these compounds, 3a, e showed excellent efficacy in delaying ejaculation.

Eudesmin Inhibits Tumor Necrosis Factor-$\alpha$ Production and T cell Proliferation

  • Cho, Jae-Youl;Yoo, Eun-Sook;Baik, Kyoung-Up;Park, Myung-Hwan
    • Archives of Pharmacal Research
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    • v.22 no.4
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    • pp.348-353
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    • 1999
  • Possible antiinflammatory effect of eudesmin were examined by assessing the effects on tumor necrosis factor (TNF)-$\alpha$ production and lymphocyte proliferation as well as cytotoxicity against murine and human macrophages. the compound significantly inhibited TNF-$\alpha$, production by lipopolysaccaride (LPS)-stimulated murine macrophage RAW264.7 without displaying cytotoxicity suggesting that eudesmin may inhibit TNF-$\alpha$ production without any interference of normal cell function. It also significantly attenuated T cell proliferation stimulated by concanavalin A (Con A) in a dose-dependent manner.

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The Screening of Hepatic Functional Improvement. Liver Protection and Antifibrotic Effect from Dried Extracts of Concha Cipangopaludinae

  • Kim, Hee-Seok;Bae, Heung-Mo;Kim, Eun-Sook;Kim, Jin-Sook;Kim, Ki-Young
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.286.2-286.2
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    • 2002
  • Oxidative stress and its consequent lipid peroxidation exert harmful effects, which have been currently involved in the generation of carbon tetrachloride(CC14)-induced fibrosis(cirrhosis). In this study, it was investigated whether dried extract of 田螺(Concha Cipangopaludinae: CC) is liver functional improvement, antioxidative and antifibrotic effect under the liver fibrotic(cirrhotic) condition by CC14 administration. The female Sprague-Dawley rats were divided into 3 groups(Normal, AC, AC-CC), and were observed for 3 weeks. (omitted)

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The Preventive Effects of Paeoniae Radix Extract against LPS-induced Acute Hepatotoxicity (LPS로 유도된 급성 간독성에 대한 백작약 추출물의 보호 효과)

  • Kim, In-Deok;Kwon, Ryun-Hee;Heo, Ye-Young;Lee, Dong-Geun;Lee, Jae-Hwa;Lee, Sang-Hyeon;Ha, Jong-Myung;Ha, Bae-Jin
    • Journal of Food Hygiene and Safety
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    • v.23 no.3
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    • pp.222-226
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    • 2008
  • The purpose of this study was to investigate the preventive effects of Paeoniae Radix Extract(PRE) against the acute hepatotoxicity-inducing lipopolysaccharide(LPS) in the liver. PRE of 100 mg/kg concentration was intraperitoneally administered into rats at dose of 1.5 ml/kg for 20 days. On day 21, 5 mg/kg of LPS dissolved in saline was injected 4 hours before anesthetization. We examined the levels of glutamate oxaloacetate transaminase(GOT), glutamate pyruvate transaminase(GPT), lactate dehydrogenase(LDH) in serum of rats, superoxide dismutase(SOD) in mitochondrial fractions, and malondialdehyde(MDA), catalase(CAT), glutathione peroxidase(GPx) in liver homogenates. LPS-treatment markedly increased the levels of GOT, GPT, LDH and MDA, and significantly decreased those of SOD, CAT and GPx. But PRE-pretreatment decreased the levels of GOT, GPT, LDH and MDA, by 59.7%, 43.6%, 59.6% and 63.5%, respectively and increased those of SOD, CAT and GPx, by 85.5%, 57.8% and 62.9%, respectively. These results showed that the PRE had the preventive effects against the acute hepatotoxicity-inducing LPS in the liver.

Anti-Oxidative Effects of Rubus coreanum Miquel Extract on Hepatic Injury Induced by Lipopolysaccharide (복분자 추출물이 Lipopolysaccharide로 유도된 간 손상에 대한 항산화 효과)

  • Kim, In-Deok;Kang, Kum-Suk;Kwon, Ryun-Hee;Ha, Bae-Jin
    • Toxicological Research
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    • v.23 no.4
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    • pp.347-352
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    • 2007
  • The protective effects of Rubus coreanum Miquel (RCM) extract against LPS-induced hepatotoxicity were studied in rats. Squrague-Dawley rats were intraperitoneally administered the RCM at 100 mg/kg per day for three weeks. Then single dose of LPS (5 mg/kg) was injected into rats. Four hours later, they were anesthesized with ether and dissected. We examined the levels of glutamate oxaloacetate transaminase (AST), glutamate pyruvate transaminase (ALT), alkaline phosphatase (ALP) and lactate dehydrogenase (LDH) in sera, superoxide dismutase (SOD) in mitochondrial fraction and catalase (CAT), glutathione peroxidase (GPx) in liver homogenate. LPS-treatment markedly increased the levels of AST, ALT, ALP, LDH and significantly decreased those of SOD, CAT and GPx. But RCM-pretreatment decreased the levels of AST, ALT, ALP and LDH by 57.9%, 37.4%, 62% and 69% respectively and increased those of SOD, CAT and GPx by 82.9%, 64.2% and 96.7% respectively. Subsequently, the protective effects of RCM was evaluated through histopathological examination of liver tissue. The LPS treatment increased the state of necrosis and cirrhosis surrounding the central veins (CV) and sinusoid, but RCM-treatment decreased the state of necrosis and cirrhosis in the liver tissue. These results demonstrated that protective effects of RCM against LPS-induced hepatotoxicity.

Inhibitory Effects of Phylligenin on the Proliferation of Cultured Rat Neural Progenitor Cells

  • Lee, Sung-Hoon;Go, Hyo-Sang;Choi, Chang-Soon;Cheong, Jae-Hoon;Han, Sun-Young;Bae, Ki-Hwan;Ko, Kwang-Ho;Park, Seung-Hwa
    • Biomolecules & Therapeutics
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    • v.18 no.1
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    • pp.48-55
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    • 2010
  • Neural progenitor cells (NPCs) differentiate into astrocytes, neurons and oligodendrocytes, which is controlled by various factors in brain. Recent evidences suggest that small molecules modulating the proliferation and differentiation of NPCs may have therapeutic value as well as the potential use as chemical probes. Phylligenin is a lignan with anti-inflammatory activity that is isolated from the fruits of Forsythia koreana. We investigated effects of phylligenin on proliferation and differentiation of NPCs. Treatment of phylligenin decreased the number of proliferating NPCs in culture without effects on the differentiation and survival of neural cells such as neurons and astrocytes. To examine the mechanism of the decreased NPCs number, we performed cell cycle analysis. Proliferation of NPCs was decreased via G1-S transition block by phylligenin treatment, and it was mediated by the increase of p21 level. However, phylligenin did not induce apoptosis of NPCs as determined by TUNEL assay and PARP cleavage. We also found that viability of glioma cell lines such as C6 and U87MG glioma cells, but not that of primary neuron and astrocyte, was inhibited by phylligenin. These results suggest that phylligenin selectively inhibits proliferation of rapidly growing cells such as neural stem cells and glioma cells. Given that the possible role of brain tumor stem cells in the pathology of brain cancers, the inhibitory effects of phylligenin might be useful in the development of new therapeutic agents against brain cancers.

Comparison of electrophysiological effects of calcium channel blockers on cardiac repolarization

  • Lee, Hyang-Ae;Hyun, Sung-Ae;Park, Sung-Gurl;Kim, Ki-Suk;Kim, Sung Joon
    • The Korean Journal of Physiology and Pharmacology
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    • v.20 no.1
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    • pp.119-127
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    • 2016
  • Dihydropyridine (DHP) calcium channel blockers (CCBs) have been widely used to treat of several cardiovascular diseases. An excessive shortening of action potential duration (APD) due to the reduction of $Ca^{2+}$ channel current ($I_{Ca}$) might increase the risk of arrhythmia. In this study we investigated the electrophysiological effects of nicardipine (NIC), isradipine (ISR), and amlodipine (AML) on the cardiac APD in rabbit Purkinje fibers, voltage-gated $K^+$ channel currents ($I_{Kr}$, $I_{Ks}$) and voltage-gated $Na^+$ channel current ($I_{Na}$). The concentration-dependent inhibition of $Ca^{2+}$ channel currents ($I_{Ca}$) was examined in rat cardiomyocytes; these CCBs have similar potency on $I_{Ca}$ channel blocking with $IC_{50}$ (the half-maximum inhibiting concentration) values of 0.142, 0.229, and 0.227 nM on NIC, ISR, and AML, respectively. However, ISR shortened both $APD_{50}$ and $APD_{90}$ already at $1{\mu}M$ whereas NIC and AML shortened $APD_{50}$ but not $APD_{90}$ up to $30{\mu}M$. According to ion channel studies, NIC and AML concentration-dependently inhibited $I_{Kr}$ and $I_{Ks}$ while ISR had only partial inhibitory effects (<50% at $30{\mu}M$). Inhibition of $I_{Na}$ was similarly observed in the three CCBs. Since the $I_{Kr}$ and $I_{Ks}$ mainly contribute to cardiac repolarization, their inhibition by NIC and AML could compensate for the AP shortening effects due to the block of $I_{Ca}$.