• Korean Journal of Plant Resources
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• v.19 no.6
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• pp.660-664
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• 2006

The aerial part of Siegesbeckia pubescens (Compositae) has been used to treat rheumatoid arthritis and hypertension in the Oriental medicine. This crude drug has been used without process (SP-0) or with three times-process of steaming and drying (SP-3) or the nine times of that process (SP-9). To search for the antinociceptive anti-inflammatory components from this crude drug, activity-directed fractionation was performed on this crude drug. Since the $CHCl_3$ extract was shown to have a more potent effect than other extracts, it was subjected to silica gel & ODS column chromatography to yield two diterpene compounds (1). Compound 1 was structurally identified as ent-16 (H, 17-hydroxykauran-19-oic acid, which were tentatively named siegeskaurolic acid A. A main diterpene, siegeskaurolic acid A was tested for the antiiflammatory antinociceptive effects using both hot plate- and writhing anti-nociceptive assays and carrageenan-induced anti-inflammatory assays in mice and rats. Pretreatment with siegeskaurolic acid A (20 and 30mg/kg) significantly reduced the stretching episodes, action time of mice and carrageenan-induced edema. These results support that siegeskaurolic acid is a main diterpene responsible for antinociceptive and antiiflammatory action of S. pubescens. In addition, the assays on SP-0, SP-3 and SP-9 produced the experimental results that SP-9 had more significant effects than other two crude drugs. These results suggest that the processing on the original plant may lead to the higher pharmacological effect.

• YAKHAK HOEJI
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• v.45 no.6
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• pp.634-640
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• 2001

Ibuprofen is one of the nonsteroidal anti-inflammatory drugs (NSAID) and has shown antiinflammatory; antipyretic, and analgesic activity in both animals and humans. But it causes gastric mucosal abnormalities including edema, erythema, and submucosal petechial hemorrhages and erosin in human. In addition, based on the pharmaceutical point of view the compression and dissolution ability of ibuprofen is known as poor. Therefore we studied to develop novel formulation containing water-insoluble drug, ibuprofen, using microemulsion consisting of surfactant, oil phase, and water phase was prepared for the purpose of increasing its bioavilability The physicochemical properties such as particle size, dissolution rate, solubility of ibuprofen in the system were determined. After oral administration of ibuprofen containing the microemulsion system, to Sprague-Dawley rats, pharmacokinetic parameters were also obtained. For the formulation in the study, oleic acid, linoleic acid, and several kinds of glycerides and triglycerides were used as an oil phase with several surfactants. Diethylene glycol monoethyl ether (Transcuto $l^{ }$) or saturated polyglycolized glycerides (Labrafil $^{ }$)as surfactant was used, the domain of microemulsion was wide. The diameter of o/w microemulsion was ranged from 90 to 220 nm. Microemulsion, prepared with unsatulated polyglycolized glycerides (Labrafil $^{ }$) and the 2 : 1 molar mixture of diethylene glycol monoethyl ether (Transcuto $l^{ }$)/polyoxyethylene(4) lauryl ether (Bri $j^{ }$ 30) , is expected to be promising system that increased the bioavilability of ibuprofen.ibuprofen.

• YAKHAK HOEJI
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• v.46 no.5
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• pp.343-347
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• 2002

In the present study, effects of essential oils isolated from various plants have been evaluated on lipopolysaccharide (LPS)-induced release of nitric oxide (NO), prostaglandin E$_2$(PGE$_2$) and tumor necrosis factor-a (TNF-$\alpha$) by the macrophage RAW 264.7 cells. Among the tested essential oils, essential oil of Ligularia fischeri var. spiciformis (LF-oil) significantly inhibited the LPS-induced generation of NO, PGE$_2$ and TNF-$\alpha$ in Raw 264.7 cells. Consistent with these observations, the expression of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 enzyme was inhibited by LF-oil in a concentration-dependent manner. Thus, this study suggests that inhibition of release of iNOS, COX-2 expression, and TNF-$\alpha$ by the essential oil of Ligularia fischer may be one of the mechanisms responsible for the anti-inflammatory effects of this medicinal plant.

• Journal of Ginseng Research
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• v.31 no.3
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• pp.127-136
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• 2007

Ginseng, the root of Panax species, is a well-known herbal medicine. It has been used as traditional medicine in Korea, China and Japan for thousands of years and now is a popular and worldwide natural medicine. The active principles of ginseng are ginsenosides which are also called ginseng saponins. Traditionally ginseng has been used primarily as a tonic to invigorate weak body functions and help the restoration of homeostasis. Current in vivo and in vitro studies demonstrate its beneficial effects in a wide range of pathological conditions such as cardiovascular diseases, cancer, immune deficiency and hepatotoxicity. Moreover, recent research indicates that some of ginseng's active ingredients exert beneficial actions on aging and neurodegenerative disorders such as Parkinson´s disease. Essentially, antioxidant, antiinflammatory, anti-apoptotic and immunostimulant activities are mostly underlying the postulated ginseng-mediated protective mechanisms. Next to animal studies, data from neural cell cultures contribute to the understanding of these mechanisms which involve decreasing nitric oxide, scavenging of free radicals and counteracting excitotoxicity. This paper focuses on own and other neuroprotective data on ginseng for dopaminergic neurons and intends to show aspects where neuroprotection e.g. by ginsenosides, additionally or preceding standard Parkinson therapy, could come about as a valuable contribution to slow neurodegenerative processes.

• Proceedings of the Plant Resources Society of Korea Conference
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• 1999.10a
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• pp.58-64
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• 1999

As indicated by Chinese letters "사혁" (sha-ji) is the ripe fruit of Seabuckthron (Hippophae rhamnoides Linneus) Family Flaeagnaceae is one of ancient natural medicine used by the Tibetan and Mongolian nationallites with ancient methods to treat desease, It is an effectiv Traditional Tibetan medicine. Bud only now are they beginning to be understood in the world of modern medicine. Hippophae was written in the book of Traditional Tibetan Medicine - "Somalaza" (8th century), "Sibuyidian" (1840) and "Jingzhubencao" (Qing Dynasty). The "Sibuyidien" was trnslated in to the Russian and published at 1903 in the Russian. Then the Russian bigan to study on Hippophae and they have achieved great successes. The Chinese scientists began to study on the chemical constituent and medical action with modern technique at 1952. With more than 40 years painstaking eport they have conceived and used a wide variety of experimental screening systems, achieved successes. Finally the)1 with one's own tests has keen verified that the crude drug being various kind of bioactive substance could Inhibits tumor, increase immunity, wipe out free radical, prevent disease of cardiovascular system, have anti-radiation, anti-inflammeutory effects. At 1977 the Hippophae rhamnoides was written in Chinase Pharmacopoeia.e rhamnoides was written in Chinase Pharmacopoeia.

• Bulletin of the Korean Chemical Society
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• v.28 no.4
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• pp.561-566
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• 2007

Adenosine kinase (AK) is a ubiquitous intracellular enzyme, which catalyzes the phosphorylation of adenosine (ADO) to adenosine monophosphate (AMP). AK inhibitors have therapeutic potential as analgesic and antiinflammatory agents. A chemical feature based pharmacophore model has been generated from known AK inhibitors (26 training set compounds) by HypoGen module implemented in CATALYST software. The top ranked hypothesis (Hypo1) contained four features of two hydrogen-bond acceptors (HBA) and two hydrophobic aromatics (Z). Hypo1 was validated by 124 test set molecules with a correlation coefficient of 0.905 between experimental and estimated activity. It was also validated by CatScramble method. Thus, the Hypo1 was exploited for searching new lead compounds over 238,819 chemical compounds in NCI database and then the selected compounds were screened based on restriction estimated activity and Lipinski's rules to evaluate their drug-like properties. Finally we could obtain 72 new lead candidates and the two best compound structures from them were posted.

• Journal of Pharmaceutical Investigation
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• v.26 no.1
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• pp.55-59
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• 1996

The crystal structure of diflunisal, 2',4'-difluoro-4-hydroxy-3-biphenyl-carboxylic acid, was determined by single crystal X-ray diffraction technique. The compound was recrystallized from a mixture of acetone and water in monoclinic, space group C2/c, with $a\;=\;34.666(6),\;b\;=\;3.743(1),\;c\;=\;20.737(4)\;{\AA},\;{\beta}=\;110.57(2)^{\circ}$, and Z = 8. The calculated density is $1.324\;g/cm^3$. The structure was solved by the direct method and refined by full matrix least-squares procedure to the final R value of 0.045 for 1299 observed reflections. It was found that the molecules in the crystal are partially disordered, that is, the two equivalent conformers $(180^{\circ}$ rotated ones through C(1)-C(7)) are packed alternatively without regular symmetry or sequence. The two phenyl rings of the biphenyl group is tilted to each other by the dihedral angle of $43.3^{\circ}$. The carboxyl group at the salicylic moiety is just coplanar to the phenyl ring, and the planarity of this salicylic moiety is stabilized by an intramolecular hydrogen bond of O(3)-H(O3) O(2). The molecules are dimerized through the intermolecular hydrogen bonds at the carboxyl group in the crystal.

• Archives of Pharmacal Research
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• v.27 no.6
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• pp.628-632
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• 2004

The chloroform and the ethyl acetate fractions from the roots of Acanthopanax chiisanensis exhibited a significant inhibition of prostaglandin E$_2$ (PGE$_2$）production in rat peritoneal macrophages stimulated by the protein kinase C activator, 12-O-tetradecanoylphorbol 13-acetate （TPA）. Hyperin was isolated as an active principle from the ethyl acetate fraction. It sup-pressed not only $PGE_2$ production but also nitric oxide （NO） production in vitro in a concentration dependent manner. their $IC_{50}$, being 24.3 and $32.9{\;}{\mu}M$, respectively. Hyperin also caused a significant inhibition of increase in acetic acid-induced vascular permeability in mice in vivo.

• YAKHAK HOEJI
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• v.42 no.2
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• pp.214-219
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• 1998

Tissue distributions and association of cyclooxygenase-2 (COX-2) with inflammatory have led us to search for COX-2 selective inhibitors from natural products. Conceptually, COX- 2 selective inhibitors should be expected to retain anti-inflammatory efficacy by inhibition of PGs production while reducing or eliminating the gastric, renal and hemostatic side effects commonly associated with NSAIDs use. Thus, a logical approach to the treatment of inflammatory diseases should involve the inhibitors of COX-2. To develop new COX-2 inhibitors from natural products, two hundred crude drugs were screened by inhibiting PGD2 generation in bone marrow derived mast cells (BMMC). Among them, 6 methanol extracts of crude drugs such as, Bletillae rhizoma, Aconiti kgreani rhizoma, Belamcandae rhizoma, Nelumbinis semen, Gleniae radix, Aurantii immatri pericarpium inhibited more than 85% of BMMC COX-2 activity at a concentration 2.5${\mu}$g/ml.

• Journal of the East Asian Society of Dietary Life
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• v.22 no.6
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• pp.772-781
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• 2012

This study was conducted to examine the development of a new anti-inflammatory substance with potent anti-inflammatory activities that was derived from the Platycodi Radix butanol fraction. To accomplish this, the chemical structures and anti-inflammatory activities of the components were elucidated. Upon column chromatography of the tertiary subfraction, fractions 8-4-1 and 8-4-2 were identified as platycodin D and D3, respectively, following recrystallization, based on melting point (MP), infrared (IR), and positive fast atom bombardment (FAB)-mass and nuclear magnetic resonance (NMR) spectral data. Platycodin D and D3 exhibited strong anti-inflammatory activities in rats when administerd at oral doses of 12 mg/kg and 36 mg/kg, p.o., respectively. Platycodin D and D3 induced inhibitory effects on capillary vascular permeability in rats at oral doses of 16 mg/kg and 24 mg/kg, p.o., respectively, and potent inhibition of leukocyte emigration in a carboxymethyl cellulose (CMC)-pouch when administered at doses of 3 mg/rat and 7 mg/rat, s.c., respectively. These results verified the high antiinflammatory potency of the platycodin D and D3 components in Platycodi Radix.