• Title/Summary/Keyword: Pharmaceutical compound

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Effect of Ephedrae Herba on Immunomodulatory Activity in Lipopolysaccharide-Exposed Rats and Raw 264.7 Cells (마황이 LPS투여 흰쥐의 면역조절능에 미치는 영향)

  • Lee, Eun
    • Korean Journal of Plant Resources
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    • v.22 no.5
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    • pp.431-437
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    • 2009
  • To investigate the anti-inflammatory effect of Ephedrae Herba in vivo and in vitro acute inflammation was induced by lipopolysaccharide (LPS) shock in rats fed Ephedrae Herba extracts and inflammatory cytokine concentrations were examined. In addition, the effect of Ephedrae Herba extracts on the production of inflammatory cytokines was examined in LPS-stimulated Raw 264.7 cells. In an in vivo experiment, plasma interleukin-$1{\beta}$ (IL-$1{\beta}$), interleukin-6 (IL-6), interleukin-10 (IL-10) and tumor necrosis factor-$\alpha$ (TNF-$\alpha$) concentrations were increased at 2 h and reached to maximal levels at 5 h after LPS treatment in all groups. Compared with control group, plasma IL-$1{\beta}$, IL-6, and TNF-$\alpha$ levels were lowered at 5 h after LPS treatment, but plasma IL-10 level was higher in at 2 and 5 h after LPS treatment in Ephedrae Herba extract group. In an in vitro experiment using Raw 264.7 macrophages, IL-$1{\beta}$, IL-6 and TNF-$\alpha$ concentrations in the Ephedrae Herba extract group were lower than those in control group. Compared with control group, IL-10 concentration appeared to be higher in the Ephedrae Herba extract group, but this trend was not significant. In conclusion, these results suggested that functional compound (s) in Ephedrae Herba extract may play a role in alleviating inflammatory response.

Differential Effect of Bovine Serum Albumin on Ginsenoside Metabolite-Induced Inhibition of ${\alpha}3{\beta}4$ Nicotinic Acetylcholine Receptor Expressed in Xenopus Oocytes

  • Lee, Jun-Ho;Jeong, Sang-Min;Lee, Byung-Hwan;Kim, Dong-Hyun;Kim, Jong-Hoon;Kim, Jai-Il;Lee, Sang-Mok;Nah, Seung-Yeol
    • Archives of Pharmacal Research
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    • v.26 no.10
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    • pp.868-873
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    • 2003
  • Ginsenosides, major active ingredients of Panax ginseng, that exhibit various pharmacological and physiological actions are transformed into compound K (CK) or M4 by intestinal microorganisms. CK is a metabolite derived from protopanaxadiol (PD) ginsenosides, whereas M4 is a metabolite derived from protopanaxatriol (PT) ginsenosides. Recent reports shows that ginsenosides might playa role as pro-drugs for these metabolites. In present study, we investigated the effect of bovine serum albumin (BSA), which is one of major binding proteins on various neurotransmitters, hormones, and other pharmacological agents, on ginsenoside $Rg_{2-}$, CK-, or M4-induced regulation of $\alpha3\beta4$ nicotinic acetylcholine (ACh) receptor channel activity expressed in Xenopus oocytes. In the absence of BSA, treatment of ACh elicited inward peak current ($I_{Ach}$) in oocytes expressing $\alpha3\beta4$ nicotinic ACh receptor. Co-treatment of ginsenoside $Rg_2$, CK, or M4 with ACh inhibited IAch in oocytes expressing $\alpha3\beta4$ nicotinic ACh receptor with reversible and dose-dependent manner. In the presence of 1% BSA, treatment of ACh still elicited $I_{Ach}$ in oocytes expressing $\alpha3\beta4$ nicotinic ACh receptor and co-treatment of ginsenoside $Rg_2$ or M4 but not CK with ACh inhibited $I_{Ach}$ in oocytes expressing $\alpha3\beta4$ nicotinic ACh receptor with reversible and dose-dependent manner. These results show that BSA interferes the action of CK rather than M4 on the inhibitory effect of $I_{Ach}$ in oocytes expressing $\alpha3\beta4$ nicotinic ACh receptor and further suggest that BSA exhibits a differential interaction on ginsenoside metabolites.

Highly sensitive and selective detection of cyanide in aqueous solutions using a surface acoustic wave chemical sensor (표면음향파 화학센서를 이용한 수용액 중 시안화이온의 선택적인 고감도 검출)

  • Lee, Soo Suk
    • The Journal of the Acoustical Society of Korea
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    • v.35 no.6
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    • pp.473-479
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    • 2016
  • We report a highly selective and sensitive 200 MHz Surface Acoustic Wave (SAW) sensor that can detect cyanide ion in aqueous solution using surface immobilized thioester molecules in combination with gold nanoparticles (AuNPs). To construct the sensor device, a monolayer of thioester compound was immobilized on the SAW sensor surface. At the sensor surface, hydrolysis of thioester group by nucleophilic addition of cyanide occurred and the resulting free thiol unit bound to AuNP to form thiol-AuNP conjugate. For the signal enhancement, gold staining signal amplification process was introduced subsequently with gold (III) chloride trihydrate and reducing agent, hydroxylamine hydrochloride. The SAW sensor showed a detection ability of $17.7{\mu}M$ for cyanide in aqueous solution and demonstrated a saturation behavior between the frequency shift and the concentration of cyanide ion. On the other hand, our SAW sensor had no activities for other anions such as fluoride ion, acetate ion and sulfate ion, moreover, no significant interference observed by other anions. Finally, all the experiments were carried out in-house developed sensor and fluidics modules to obtain highly reproducible results.

Inflammation inhibitory effect of water extract from pumpkin's tendril (호박 덩굴손 물 추출물의 염증제어 활성)

  • Jeong, Ha-Na;Choi, Ju-Hee;Lee, Ha-Nul;Lee, So-Hyeon;Cho, Soon-Chang;Park, Jong-Hwan;Kim, Young-Min
    • Food Science and Preservation
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    • v.24 no.8
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    • pp.1122-1128
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    • 2017
  • Pumpkin has long been used as traditional health materials in oriental medicine, pharmacy, medicine, and food industries in many countries. In this study, the water extract and two active components from tendril of young C. moschata Duch. were investigated on inflammation inhibitory activity. The water extract of young C. moschata Duch. showed high cell viability over 95% and it decreased the production of interlukin 6 (IL-6) and tumor necrosis factor (TNF-${\alpha}$) in the capacity of mouse bone marrow-derived macrophages (BMDM) upon lipopolysaccharide (LPS) stimulation. Also, isolated fraction (B4) suppressed the secretion of IL-6 and TNF-${\alpha}$. Among the domestically cultivated pumpkins, B4 fraction contained in the tendril part of them and it comprised of the order of tendril from Cucurbita pepo var. cylindrica, old of C. moschata Duch., and young of C. moschata Duch. These results suggest that water extracts of C. moschata Duch. and purified active compound, rutin, show anti-inflammation activity by suppression of the secretion of IL-6 and TNF-${\alpha}$. It can be applicable as pharmaceutical materials.

Comparison of Ginseng Saponin, Fatty Acid, Polysaccharide, Phenolic Compound and Organic Acid of Ginseng Hairy Roots and Callus (인삼모상근과 캘루스의 사포닌, 지방산, 산성다당체, 페놀성 물질 및 유기산의 함량비교)

  • Lee Jun-Won;Kim Jin-Ju;Yang Deok-Chun
    • Korean Journal of Plant Resources
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    • v.18 no.2
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    • pp.207-215
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    • 2005
  • Korean ginseng(Panax ginseng C.A. Meyer) roots have long been known as the best medicinal plant and its pharmaceutical bio-activities have been proven by scientific analyses of their components - ginsenosides, acidic polysaccharides, phenolic compounds, fatty acids and organic acids etc. Ginseng hairy roots and callus have been cultured in vitro for stable supply of ginseng material. In this study, the amount of ginsenosides, fatty acids, acidic polysaccharides, phenolic compounds and organic acids in ginseng hairy roots and callus were compared. Higher amount of ginsenoside was found in ginseng hairy roots than ginseng callus. Higher amount of saturated fatty acid (palmitic acid) was found in callus and higher amount of unsaturated fatty acid (linoleic acid) was found in hairy roots. Acidic polysaccharide and phenolic compounds were contained by the same amount in both hairy roots and callus. Organic acids were found more in hairy roots.

Pharmacokinetic Study of CKD-602, A New Camptothecin Derivative: Distribution, Metabolism and Excretion (신규 캄토테신계 항암제 CKD-602의 약물동태: 분포, 대사 및 배설)

  • Lee, Ju-Mong;Lee, Jun-Hee;Kim, Joon-Kyum;Shin, Hee-Jong;Lee, Hyung-Ki;Lee, Sang-Joon;Hong, Chung-Il
    • YAKHAK HOEJI
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    • v.42 no.4
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    • pp.437-446
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    • 1998
  • The distribution, metabolism and excretion of CKD-602{20(S)-7-[2-(N-Isopropylamino)ethyl]camptothecin HCI), a new camptothecin derivative, were investigated in rats after a sing le administration of CKD-602. 1. The tissue levels of CKD-602 given to mice by the intravenous route at a dose of 20mg/kg were the highest in intestine, followed in descending order by kidney, liver, stomach,lung, heart, spleen and plasma. The concentrations of CKD-602 after 24hrs decreased to less than 2% of the peak level in most tissues except the skin. The urinary and fecal excretion of CKD-602 were 47.6% and 44.4% of the administered dose, respectively, with 0.7% remaining in the rinse. 2. After administration of CKD-602 at 10mg/kg in rats, metabolism of this compound was examined in plasma, urine, and feces. The plasma samples were collected for 24hr, urinary and fecal samples for 72hr. While any peak of CKD-602 in HPLC chromatograms was not detected from plasma and urine it was detected in feces (peaks, 9.8 min). However, additional peak area was about 0.5% of the peak area of parent CKD-602. Therefore, CKD-602 may be eliminated with the parent form and rarely metabolized in the body. 4. After I.v. administration of CKD-602 at 10mg/kg in rats, urinary and fecal excretions were examined for 72hrs post dose period. 87% of total urinary excretion of CKD-602 was excreted within 8hr after administration, 53%, and 32% of total fecal excreted amounts were determined in 0-24 hr and 24-48hr periods, respectively. The total excretion amounts of CKD-602 into urine and feces were 94% of the administered dose.

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The Effect of Linarin on LPS-Induced Cytokine Production and Nitric Oxide Inhibition in Murine Macrophages Cell Line RAW264.7

  • Kim, Kyung-Jae;Han, Shin-Ha;Sung, Ki-Hyun;Yim, Dong-Sool;Lee, Sook-Kyeon;Lee, Chong-Kil;Ha, Nam-Ju
    • Archives of Pharmacal Research
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    • v.25 no.2
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    • pp.170-177
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    • 2002
  • The herb, Chrysanthemum zawadskii var, latilobum commonly known as Gu-Jul-Cho in Korea, used in traditional medicine to treat pneumonia, bronchitis, cough, common cold, pharyngitis, bladder-related disorders, gastroenteric disorders, and hypertension. Linarin is the main active compound and the biological mechanisms of its activity are unclear. It is believed that effects of this herb may be exerted through the pluripotent effectors of linarin due to its ability to treat a variety of afflictions. In this study, the effects of linarin on the mouse macrophages cell line, RAW 264.7, were investigated. It was found that linarin could activate macrophages by producing cytokines. Monocytes and tissue macrophages produce at least two groups of protein mediators of inflammation, interleukin 1 (IL-1 ) and the tumor necrosis factor (TNF). Recent studies have shown that TNF and IL-1 modulate the inflammatory function of endothelial cells, leukocytes, and fibroblasts. $TNF-{\alpha}$ production by macrophages treated with linarin occured in a dose dependent manner However, IL-1 production was largely unaffected by this natural product. This study demonstrated the ability of linarin to activate macrophages both directly and indirectly. Linarin also affect both cytosine production and nitric oxide inhibition, in addition to the expression of some surface molecules. Nitric oxide (NO), derived from L-argin-ine, is produced by two forms(constitutive and inducible) of nitric oxide synthase (NOS). The NO produced in large amounts by inducible NOS is known to be responsible for the vasodilation and hypotension observed in septic shock. Linarin was found to inhibit NO production in the LPS-activated RAW 264.7 cells. Linarin may be a useful candidate as a new drug for treating endotoxemia and the inflammation accompanied by NO overproduction. The linarin-treated total Iymphocytes exhibited cytotoxicity in a dose dependent manner between $20{\;}{\mu}g/ml{\;}and{\;}40{\;}{\mu}g/ml$. These results suggest that linarin may function through macrophage activation.

Artemisolide from Artemisia asiatica: Nuclear $Factor-{\kappa}B\;(NF-{\kappa}B)$ Inhibitor Suppressing Prostaglandin $E_2$ and Nitric Oxide Production in Macrophages

  • Reddy, Alavala Matta;Lee, Jun-Young;Seo, Jee-Hee;Kim, Byung-Hak;Chung, Eun-Yong;Ryu, Shi-Yong;Kim, Young-Sup;Lee, Chong-Kil;Min, Kyung-Rak;Kim, Young-Soo
    • Archives of Pharmacal Research
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    • v.29 no.7
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    • pp.591-597
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    • 2006
  • Aerial parts of Artemisia asiatica (Compositae) have been traditionally used as an oriental medicine for the treatment of inflammatory and ulcerogenic diseases. In the present study, artemisolide was isolated as a nuclear factor $(NF)-{\kappa}B$ inhibitor from A. asiatica by activity-guided fractionation. Artemisolide inhibited $NF-{\kappa}B$ transcriptional activity in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 with an $IC_{50}$ value of $5.8\;{\mu}M$. The compound was also effective in blocking $NF-{\kappa}B$ transcriptional activities elicited by the expression vector encoding the $NF-{\kappa}B$ p65 or p50 subunits bypassing the inhibitory kB degradation signaling $NF-{\kappa}B$ activation. The macrophages markedly increased their $PGE_2$ and NO production upon exposure to LPS alone. Artemisolide inhibited LPS-induced $PGE_2$ and NO production with $IC_{50}$ values of $8.7\;{\mu}M$ and $6.4\;{\mu}M$, respectively, but also suppressed LPS-induced synthesis of cyclooxygenase (COX)-2 or inducible NO synthase (iNOS). Taken together, artemisolide is a $NF-{\kappa}B$ inhibitor that attenuates LPS-induced production of $PGE_2$ or NO via down-regulation of COX-2 or iNOS expression in macrophages RAW 264.7. Therefore, artemisolide could represent and provide the anti-inflammatory principle associated with the traditional medicine, A. asiatica.

Proliferative Effects of Flavan-3-ols and Propelargonidins from Rhizomes of Drynaria fortunei on MCF-7 and Osteoblastic Cells

  • Chang, Eun-Ju;Lee, Won-Jung;Cho, Sung-Hee;Choi, Sang-Won
    • Archives of Pharmacal Research
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    • v.26 no.8
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    • pp.620-630
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    • 2003
  • The proliferative effects of thirty Oriental medicinal herbs on MCF-7 (estrogen-sensitive breast cancer cell line) and ROS 17/2.8 osteoblast-like cells were determined using the MTT assay. Methanol extracts from several herbs was found to show proliferative activity on the above two cell lines in the range of 5 to 100 $\mu$g/mL. Among these active herbs, the methanol extract from the rhizomes of Drynaria fortunei showed the most potent proliferative activity, and the cell proliferations were significantly increase by 136 and 158% in the MCF-7 and ROS 17/2.8 cells, respectively, when treated with 100 $\mu$ g/mL. Through a bioassay-guided separation, eight flavonoids, including four new flavan-3-ols and two propelargonidins, together with the known (-)-epiafzelechin and naringin, were isolated. Their chemical structures were characterized as (-)-epiafzelechin (1), (-)-epiafzelechin-3-O-$\beta$-D-allopyranoside (2), (-)-epiafzelechin-3-O-(6"-O-acetyl)-$\beta$-D-allopyranoside (3), 4$\beta$-carboxymethyl-(-)-epiafzelechin methyl ester (4), 4$\beta$-car-boxymethyl-(-)-epiafzelechin sodium salt (5), naringin (6), (-)-epiafzelechin-(4$\beta$\rightarrow8)-4$\beta$-car-boxymethylepiafzelechin methyl ester (7) and (-)-epiafzelechin-($4\beta\rightarrow8, 2\beta\rightarrowΟ\rightarrow7)-epiafzelechin-(4\beta\righarrow8)-epiafzelechin (8) by extensive 1D and 2D NMR spectroscopy. Most of these flavonoids, in the range of $10^{-15}∼10^{-6}$ M, accelerated the proliferation of MCF-7 cell, with compounds 7 and 8, in the range of $10^{-15}∼10^{-12}$ M, showing especially potent proliferation effects. Meanwhile, seven flavonoids, with the exception of compound 4, stimulated the proliferation of ROS 17/2.8 cells in the range of $10^{-15}∼10^{-6}$ M, with compounds 5-8 especially accelerating the proliferation, in dose-dependent manners ($10^{-15}∼10^{-9}$ M), and their proliferative effect was much stronger than that of $E_2$ and genistein. These results suggest that propelargonidin dimers and trimers isolated from the rhizomes of Drynaria fortunei may be useful as potential phytoestrogens, which play important physiological roles in the prevention of postmenopausal osteoporosis.

Decomposition of Sulfamethoxazole by Catalytic Wet Peroxide Oxidation (촉매습식과산화(CWPO)를 이용한 설파메톡사졸의 분해)

  • Kim, Dul Sun;Lee, Dong-Keun;Kim, Jin Sol
    • Clean Technology
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    • v.24 no.4
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    • pp.293-300
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    • 2018
  • Sulfamethoxazole (SMX) is sulfaamide-based synthetic antibiotics, which are widely prescribed pharmaceutical compound to treat bacterial infections in both human and animals. Most of them are not completely decomposed as refractory substances. The environmental impact of pharmaceuticals as emerging contaminants has generated severe concerns. In this study, catalytic wet peroxide oxidation (CWPO) of SMX was carried out with $Cu/Al_2O_3$ catalyst and investigated the optimum reaction conditions of temperature, dosage of catalyst and concentration of $H_2O_2$ to completely decompose the SMX. It was observed that SMX was completely decomposed within 20 min using 0.79 mM $H_2O_2$ and 6 g $Cu/Al_2O_3$ catalyst at 1 atm and $40^{\circ}C$, but SMX was not fully mineralized and converted to intermediates as hydroylated-SMX, sulfanilic acid, 4-aminobenzenesulfinic acid and nitrobenzene. After that these are completely mineralized through organic acid. We proposed the decomposition reaction path ways of SMX by analyzing the behavior of these intermediates. To investigate the durability of heterogeneous catalyst, decomposition of SMX was observed by continuously recycling catalysts. When the heterogeneous catalyst of 10 wt% $Cu/Al_2O_3$ was continuously reused 5 times, decomposition of SMX was a little lowered, but the activity of catalyst was overall very stable.