• Journal of Physiology & Pathology in Korean Medicine
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• v.30 no.4
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• pp.229-235
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• 2016

Sasa borealis has long been used in folk remedies and traditional Korean medicine for analgesic, sedative and anticarcinogenic purposes. To excavate novel natural compounds for treating obesity, we separated leaf and stem and fractionated. We screened phenolic contents, anti-oxidative and anti-inflammatory properties with the fractions. Dichloromethane (DCM) and ethyl acetate (EA) fraction from both leaf and stem exhibited high anti-oxidative properties demonstrated by DPPH, ABTS assay in accordance with their phenolic contents. In addition, DCM and EA fraction from leaf inhibited nitric oxide (NO) production as well as inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in Raw 264.7 cell. Finally, DCM and EA fraction from both leaf and stem significantly inhibited 3T3-L1 preadipocyte differentiation and decreased intracellular lipid level. These results suggest that DCM and EA fraction from Sasa borealis may contain therapeutic agent for obesity by attenuating inflammation and oxidative stress.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.234-234
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• 1996

DA-5018은 여러 opiate수용체 실험에서 morphine 또는 naloxone 보다 10-100배 정도 낮은 친화력을 나타내었다. 기니픽 회장표본과 랫드 수정관표본의 전기자극 실험에서는 DA-5018의 의해 유도된 수축반응이 naloxone의 영향을 받지 앉았고, 랫드에서의 진통효과도 naloxone 전처치에 의해 차단되지 않았으므로, DA-5018은 opiate 수용체를 경유하지 앉는 것으로 생각된다. 또한, OA-5018 120$\mu$M에서 cyclooxygenase 생성을 50% 증가시켰고 mM 농도에서 5-lipooxygenase 합성을 약간 억제하였으므로, NSAID계 유사약물이 아님을 확인하였다. DA-5018은 기니픽 기관 표본에 대해 capsaicin과 동일하게 수축반응을 나타내었고, 이것은 capsazepine 전처리에 의해 억제되었다. 척수에서의 substance P 유리활성은 capsaicin보다 약 9배 강한 것으로 나타났다. 또한 랫드에 DA-5018 진통유효용량인 1mg/kg을 피하주사한 후 분리한 척수에서 capsaicin에 의한 substance P의 유리활성은 15분 후에 감소하였고 120분 후에는 회복되었다. 따라서 OA-5018의 진통작용에도 substance P의 고갈이 관여하는 것으로 생각된다. 이상의 결과로부터, DA-5018의 진통작용은 capsaicin수용체를 매개하는 것으로 사료된다.

• The Journal of Korean Medicine
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• v.24 no.4
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• pp.34-42
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• 2003

This study was designed to investigate the modulation of the Corydalis tuber on glycine-activated ion current in rat periaqueductal gray (PAG) neurons. Aqueous extract from Corydalis tuber has been widely used for pain control such as dysmenorrhea, irregular menstruation or amenorrhea with abdominal cramping, neuralgia, headache and gastrointestinal spasm. The PAG region of the brain is known to be involved heavily with nociception. Modulation of the Corydalis tuber on glycine-induced ion current in rat periaqueductal gray (PAG) neurons was studied by a nystatin-perforated patch-clamp technique. High concentrations of Corydalis tuber elicited ion current, which was suppressed by strychnine application. Low concentrations of Corydalis tuber reduced glycine-induced ion currents in the PAG neurons. Inhibitory action of Corydalis tuber on glycine-activated ion current was reduced by treatment with naltrexone, a non- selective opioid antagonist. Application of N-methylmalemide (NEM), a sulfhydryl alkylating agent, also reduced the inhibitory action of Corydalis tuber on glycine-activated ion current in the PAG neurons. These results suggest that the inhibitory effect of Corydalis tuber on glycine-activated ion current in the PAG neurons is one of the analgesic mechanisms of the Corydalis tuber, which may activate descending pain control system in PAG neurons.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.191-192
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• 2002

Since capsaicin was found as an excellent vanilloid receptor agonist, considerable efforts toward the development of a novel analgesic have been continued. However, the small therapeutic window between these effects and the excitatory side effects, such as hypothermia, bronchoconstriction, increased GI mobility, and hypertension, precluded the development of capsaicin as a systemic agent. (omitted)

• Natural Product Sciences
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• v.18 no.4
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• pp.215-220
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• 2012

The stem of Lindera obtusiloba (Lauraceae), has been widely used as a traditional medicine for the treatment of abdominal pain, bruise and hepatocirrhosis. In the present study, antinociceptive and sedative properties of the methanol extract of L. obtusiloba (MLO) were evaluated. MLO demonstrated strong and dose-dependent antinociceptive activities on various experimental pain models including thermal nociception and chemical nociception, compared to tramadol and indomethacin, reference drugs. In combination test using naloxone, the diminished analgesic activity of MLO was observed, indicating the relation with opioid receptor. Moreover, MLO also decreases pentobarbital-induced sleep latency and increases sleeping time suggesting its hypnotic and sedative action. The present results indicate that MLO could be used as valuable antinociceptive and sedative agent for the treatment of various diseases.

• Korean Journal of Pharmacognosy
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• v.31 no.3
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• pp.340-344
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• 2000

Lonicerae Flos, the flower of Lonicera japonica Thunb., has been used as a diuretic, stomachic, antipyretic, analgesic and anti-inflammatory agent in Korea. In order to evaluate the quality of Lonicerae Flos, the method of isolation and quantitative determination of luteolin $7-O-{\beta}-D-glucoside$ as a reference standard compound has been developed. Different specimens of Lonicerae Flos were collected from twenty Korean markets and were analyzed with HPLC using the mobile phase of MeOH-4.5% acetic acid solution (16.5:83.5). The average content of luteolin $7-O-{\beta}-D-glucoside$ from Lonicerae Flos in Korean markets was $0.43{\pm}0.34%$.

• Toxicological Research
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• v.31 no.2
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• pp.165-172
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• 2015

Cornus officinalis is widely distributed in Korea, and its fruit has been used to make as herbal drug for traditional medicine in Korea, Japan, and China because of its tonic, analgesic, and diuretic properties. However, the effects of C. officinalis methanol extract (COME) on melanogenesis remain poorly understood. We evaluated the melanogenic capability of COME in melan-a cells, which are immortalized mouse melanocytes. COME increased melanin synthesis in a dose-dependent manner. Treatment with $12.5{\mu}g/mL$ of COME significantly increased melanin content by 36.1% (p < 0.001) to a level even higher than that (31.6%) of 3-isobutyl-1-methyl-xanthine, a well-known pigmentation agent. COME also upregulated tyrosinase activity and its messenger RNA and protein expression. In addition, COME upregulated the expression of tyrosinase-related proteins 1 and 2 and microphthalmia-associated transcription factor-M messenger RNA expression. These results imply that COME may be appropriate for development as a natural product to treat hair graying.

• Biomolecules & Therapeutics
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• v.9 no.4
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• pp.298-306
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• 2001

To develop a novel transdermal delivery system of loxoprofen (LP), a potent antiinflammatory and analgesic agent, the effects of vehicle composition and drug loading dose on the skin permeation property were investigated. And in vivo skin absorption property studied by analysing the $C_{max}$ and AUC was investigated after applying the developed plaster systems on rabbit back skin. Addition of isopropyl myristate (IPM) and IPM-diethylene glycol monoethyl ether (DGME) cosolvent in the plaster showed higher permeation rates than those from propylene glycol laurate-DGME cosolvent systems. As the concentration of LP in the plaster increased from 0.56 mg/$\textrm{cm}^2$ to 1.19 mg/$\textrm{cm}^2$, the drug release and skin permeation rates increased linearly. At loading dose of 1.19 mg/$\textrm{cm}^2$, the flux reached 35.6 $\mu$g/$\textrm{cm}^2$/hr. New LP plasters showed a good adhesive property onto skin, and showed no crystal formation. The AU $C_{0-24hr}$ and $C_{max}$ after dermal application of LP plaster (60 mg/70 $\textrm{cm}^2$) were found to be 6951$\pm$230 ng.hr/ml and 400$\pm$44 ng/ml, respectively. And the plasma concentration maintained above 300 ng/ml up to 24 hr period. In the carrageenan-induced rat paw edema test, LP plaster showed similar inhibition rate with marketed ketoprofen (Ketoto $p^{R}$) plaster.aster.r.

• The Korean Journal of Physiology and Pharmacology
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• v.19 no.5
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• pp.413-420
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• 2015

Dexmedetomidine is a sedative and analgesic agent that exerts its effects by selectively agonizing ${\alpha}2$ adrenoceptor. Histamine is a pathophysiological amine that activates G protein-coupled receptors, to induce $Ca^{2+}$ release and subsequent mediate or progress inflammation. Dexmedetomidine has been reported to exert inhibitory effect on inflammation both in vitro and in vivo studies. However, it is unclear that dexmedetomidine modulates histamine-induced signaling and pro-inflammatory cytokine expression. This study was carried out to assess how dexmedetomidine modulates histamine-induced $Ca^{2+}$ signaling and regulates the expression of pro-inflammatory cytokine genes encoding interleukin (IL)-6 and -8. To elucidate the regulatory role of dexmedetomidine on histamine signaling, HeLa cells and human salivary gland cells which are endogenously expressed histamine 1 receptor were used. Dexmedetomidine itself did not trigger $Ca^{2+}$ peak or increase in the presence or absence of external $Ca^{2+}$. When cells were stimulated with histamine after pretreatment with various concentrations of dexmedetomidine, we observed inhibited histamine-induced $[Ca^{2+}]_i$ signal in both cell types. Histamine stimulated IL-6 mRNA expression not IL-8 mRNA within 2 hrs, however this effect was attenuated by dexmedetomidine. Collectively, these findings suggest that dexmedetomidine modulates histamine-induced $Ca^{2+}$ signaling and IL-6 expression and will be useful for understanding the antagonistic properties of dexmedetomidine on histamine-induced signaling beyond its sedative effect.

• YAKHAK HOEJI
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• v.47 no.5
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• pp.300-306
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• 2003

Rhizoma of Smilax china has been used as anti-inflammatory and analgesic, antiedemic agent in Korean folk medicine. In order to investigate the efficacy of anti-oxidative activity, the activity-guided fractionation and the isolation were performed. Each fractions ($H_2O$ fraction, 20％, 40％, 60％, 100％ MeOH fractions and CHCl$_3$ fraction) was examined antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging potential. It was revealed that 40％, 20％ MeOH fractions and $H_2O$ fractions have significant anti-oxidative activity. From 40％ and 20％ MeOH fractions two flavonoid glycosides and one procyanidin were isolated and elucidated apigenin-7-Ο-$\alpha$-L-rhamnopyranosyl(1\longrightarrow2)-$\beta$-D-glucopyranoside, apigenin-7-Ο-$\alpha$-L-rhamnopyranosyl(1\longrightarrow6)-$\beta$-D-glucopyranoside and catechin(4$\alpha$\longrightarrow6)epicatechin through their physicochemical data and IR, FAB-MS, $^{13}$ C-NMR, and $^1$H-NMR analysis with authentics, respectively. The isolated compounds were examined by DPPH method. Apigenin-7-Ο-$\alpha$-L-rhamnopyranosyl(1\longrightarrow2)-$\beta$-D-glucopyranoside and catechin (4$\alpha$\longrightarrow6) epicatechin showed powerful radical scavenging activities on DPPH radical among three compounds.