• The Korean Journal of Pharmacology
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• v.10 no.2
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• pp.43-54
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• 1974

The cactus family Cactaceae, numbering about 1,500 species, is a fleshy-stemmed perennial plant which is principally distributed in the south and north America. On the other hand, the cactus plant is presumed to be introduced into Korea in 1912-1945, thereafter it has been cultivated merely in favor of ornamentation with the exception of being occasionally used as medication among laymen. Opuntia elata which belongs to Opuntia genus, the Cactaceae family is one of the cacti being cultivated a great deal in Korea. Cho et. al. reported in 1974 that Opuntia dilenii manifested the cardiac inhibitory effect and oxytocic effect, and its mechanism might be partially due to the direct action. Besides this, there are few reports on the pharmacological research concerning Opuntia genus to be demonstrated in Korea. However, some other cacti have the remarkable pharmacological effects; the active ingredients, mescaline, anhalamine, anhalanine, etc. from Peyote cactus (Lophophora williamsii) belonging to Lophophora genus have the psychotomimetic and sympathomimetic effects, and the cardioactive glycosides from Cactus Grandifolius (Selenicereus grandiflorus) belonging to Cereus genus have the cardioactive and diuretic effects. The authors hereby inquired into this study to find out the propriety of the pharmacological properties of the ethanol extract of Opuntia elata (EX) on the heart, blood pressure, respiration, intestine and uterus in the experimental animals. The results of the experiment were as follows: 1. Administration of EX manifested the cardiac inhibitory effect caused by the negative inotropic action in the isolated heart of frog, and the pretreatment of atropine did not affect the inhibitory effect produced by EX. 2. Administration of EX manifested the transient hypotensive effect in the intact rabbit, and the pretreatment of atropine did not affect the hypotensive effect produced by EX. 3. Administration of the small dose of EX manifested no significant effect, but moderate dose or more the stimulating effect, and the large dose the asphyxia on the respiratory motility in the intact rabbit. 4. Administration of EX manifested the sustained augmentation of contractility in the excised duodenum of rabbit, and the pretreatment of atropine did not affect the stimulating effect produced by EX. 5. Administration of EX manifested the sustained augmentation of contractility in the excised pregnant uterus of rabbit, and the pretreatment of atropine and oxytocin did not affect the oxytocic effect produced by EX, but that of barium chloride more or less stimulated the oxytocic effect produced by EX.

• The Korean Journal of Physiology and Pharmacology
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• v.20 no.3
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• pp.269-277
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• 2016

Ellagic acid (EA), an antioxidant polyphenolic constituent of plant origin, has been reported to possess diverse pharmacological properties, including anti-inflammatory, anti-tumor and immunomodulatory activities. This work aimed to clarify the skin anti-photoaging properties of EA in human dermal fibroblasts. The skin anti-photoaging activity was evaluated by analyzing the reactive oxygen species (ROS), matrix metalloproteinase-2 (MMP-2), total glutathione (GSH) and superoxide dismutase (SOD) activity levels as well as cell viability in dermal fibroblasts under UV-B irradiation. When fibroblasts were exposed to EA prior to UV-B irradiation, EA suppressed UV-B-induced ROS and proMMP-2 elevation. However, EA restored total GSH and SOD activity levels diminished in fibroblasts under UV-B irradiation. EA had an up-regulating activity on the UV-B-reduced Nrf2 levels in fibroblasts. EA, at the concentrations used, was unable to interfere with cell viabilities in both non-irradiated and irradiated fibroblasts. In human dermal fibroblasts, EA plays a defensive role against UV-B-induced oxidative stress possibly through an Nrf2-dependent pathway, indicating that this compound has potential skin antiphotoaging properties.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.1
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• pp.218-223
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• 2005

According to the Chinese and Korean medicinal and herbal literature, SSG(Silsosangami) is effective for the treatment of inflammation, hyperlipemia and arteriosclerosis. The pharmacological action of SSG has been limitedly studied in regard to ischemic infarction. This herbal medicine has been shown to express diverse activities such as immunomodulating, anti-infarction, anti-allergic and anti-inflammatory effects. Antisclerotic effects of SSG in experimentally induced atherosclerosis in rabbits have also been reported. However, pharmacological mechanisms of SSG on lipid metabolism and atherosclerosis formation are poorly understood. The present paper reports the effect of extracts obtained from SSG on endotoxin-induced experimental DIC in rats. Also, these were tested for their effect on endotoxin-induced blood platelet aggregation, thrombin-induced conversion of fibrinogen and fibrinolysis in vitro experiments with aspirin as a positive agent. The anti-thrombic properties of SSG were also investigated by means of analytical parameters of bood composition. The extracts of SSG and its seven herbs, except Cnidii Rhizoma and Carthami Flos, inhibited the endotoxin-induced DIC and thrombosis in rats. Also the extract inhibited the endotoxin-induced decrease in blood platelets and fibrinogen, and endotoxin-induced increase in fibrin degradation products (FDP) on disseminated intravascular coagulation in normal rats.

• Biomolecules & Therapeutics
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• v.11 no.1
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• pp.41-50
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• 2003

General pharmacological properties of DA-8159, a new pyrazolopyrimidinone derivative were examined in laboratory animals to investigate its safety profile. The oral administration of DA-8159 (1, 5 or 30 mg/kg) in mice and rats had no effect on general behaviors and central nervous system of the animals in test systems, such as hexobarbital-induced sleeping time, motor coordination, normal body temperature, writhing syndromes induced by 0.75% acetic acid solution, chemo-shock produced by pentetrazole solution and rotar rod test. Anesthetized cats treated intravenously with DA-8159 (0.1, 0.3, 1, 3 or 10 mg/kg) showed transient and mild decrease in blood pressure. However, heart rate, respiration rate and tidal volume were not changed by intravenous DA-8159. In the isolated organs including ileum, heart (sinus rate of atria and contractility of papillary muscle), trachea of guinea pigs and phrenic nerve of rats, DA-8159 ($10^{-8}$ ∼$10^{-5}$ mg/L) did not elicit any effect or inhibitory action on the chemically or electrically stimulated contraction. DA-8159 did not influence gastric secretion, pH and total acid output in rats and intestinal propulsion in mice. The administration of DA-8159 in rats had no effect on the platelet aggregation induced by ADP in rabbit plasma, urinary volume and electrolyte ion ($Na^{+}$, $K^{+}$, $Cl^{-}$) excretion in rats. Prothrombin time (PT) of the rats showed a mild but significant increase after administration of DA-8159. Activated partial thromboplastin time (APTT), however, was not affected by DA-8159. These results indicate that DA-8159 does not exert any of serious pharmacological effects.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.21
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• pp.9049-9058
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• 2014

Casticin (3', 5-dihydroxy-3, 4', 6, 7-tetramethoxyflavone) is an active compound isolated from roots, stems, leaves, fruits and seeds of a variety of plants. It is well known for its pharmacological properties and has been utilized as an anti-hyperprolactinemia, anti-tumor, anti-inflammatory, neuroprotetective, analgesic and immunomodulatory agent. Recently, the anticancer activity of casticin has been extensively investigated. The resulkts showed that it exerts protective potential by targeting apoptosis, considered important for cancer therapies. In this article, our aim was to review the pharmacological and therapeutic applications of casticin with specific emphasis on its anticancer functions and related molecular mechanisms. Chemotherapeutic effects are dependent on multiple molecular pathways, which may provide a new perspective of casticin as a candidate anti-neoplastic drug. This review suggests that additional studies and preclinical trials are required to determine specific intracellular sites of action and derivative targets in order to fully understand the mechanisms of its antitumor activity and validate this compound as a medicinal agent for the prevention and treatment of various cancers.

• YAKHAK HOEJI
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• v.34 no.2
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• pp.126-132
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• 1990

To enhance the activity of ibuprofen, amides of ibuprofen, 1-piperazinyl-2-(4-isobutylphenyl)propionamide(Ibu-P.A.) and 1-(4-methylpiperazinyl)-2-(4-isobutylphenyl)propionamide (Ibu-M.P.), were synthesized and the pharmaceutical properties and the pharmacological activities of the amides were studied. The lipid:water partition coefficients and pKa values were examined in vitro, and the antiinflammatory effect, analgesic effects, acute toxicity, and intestinal absorption were studied for the amides and compared with ibuprofen in vivo. The results are summarized as belows; 1) The lipid:water partition coefficients of Ibu-M.P. were higher than those of ibuprofen. 2) The calculated pKa values of ibuprofen and Ibu-M.P. were 5.49 and 8.66, respectively. 3) The antiinflammatory effects of ibuprofen, Ibu-P.A., and Ibu-M.P. were same intensity, but the duration of the effects of Ibu-P.A. and Ibu-M.P. were longer than that of ibuprofen. 4) The analgesic effect of Ibu-M.P. was more potent than those of ibuprofen and Ibu-P.A. in the acetic acid-induced writhing test. 5) The $LD_{50}$ was 495 mg/kg for ibuprofen, 187 mg/kg for Ibu-M.P., and over 1250 mg/kg for Ibu-P.A.. 6) The absorption rate constants(k) and half-life($t_{1/2}$) were 0.74($hr^{-1}$) and 0.94(hr) for ibuprofen, and 0.72 ($hr^{-1}$) and 0.96 (hr) respectively for Ibu-M.P..

• Biomolecules & Therapeutics
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• v.10 no.1
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• pp.19-24
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• 2002

The effects of a newly synthesized $H^+/K^+$ ATPase inhibitor,1-(2-methyl-4-methoxypheny)-4-[(3-hy-droxypropyl)amino] -6-methyl-2,3-dihydropyrrolo (3,2-c) quinoline (DBM-819) , on the central nervous system, isolated smooth muscle, cardiovascular and digestive systems and renal function were investigated in various experimental animals. Oral administration of DBM-819 had no effect on the central nervous system except body temperature of mice slightly decreased at doses of 15 and 50 mg／kg. DBM-819 produced a moderate analgesic effect in acetic acid-induced writhing test in mice at 50 mg／kg (p.o.). In conscious rats, DBM-819 (15 and 50 mg／kg, p.o.) showed a slight increase in blood pressure and a small decrease in heart rate. DBM-819 had an significant effect on agonist-induced contraction of guinea pig ileum at $1.5{\times}10^{-5}g/ml.$ No significant effect of DBM-819 (5 and 15 mg／kg, i.p) on urinary volume or urinary excretion of $Na^+,\;K^+$ and Cl- was observed in rats. DBM-819 had no significant effect on intestinal transport of a semisolid meal in mice at 15 and 50 mg／kg (p.o.). These findings suggest that DBM-819 exerts no significant pharmacological effects on the central nervous system and renal function at 15 mg／kg (p.o.), but produces some effects on the smooth muscle and circulatory system.

• The Korean Journal of Pharmacology
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• v.32 no.2
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• pp.283-292
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• 1996

The spinal dorsal horn is the area where primary afferent fibers terminate and cutaneous sensory information is processed. A number of putative neurotransmitter substances, including excitatory and inhibitory amino acids and peptides, are present in this region. In this study, single neurons of the spinal dorsal horn were acutely isolated and the properties of whole cell current and responses to excitatory and inhibitory neurotransmitters were studied by patch clamp technique. Transverse slice ($(300{\mu}m$) of lumbar spinal cords from young rats$(7{\sim}14\;days)$ were sequentially treated with two pretenses(pronase 0.75 mg/ml and thermolysin 0.75 mg/ml), then single neurons were mechanically dissociated. These neurons showed near-intact morphology such as multipolar, ellipsoidal and bipolar, and pyramidal cells and we recorded the typical whole cell currents of $K^+$, $Ca^{2+}$ and ligand-operated channels from these neurons. Glutamate $(30{\mu}M)$ and N-methyl-D-aspartate(NMDA, $30{\mu}M)$ induced inward currents of $117{\pm}12.4$ pA(n=5) and $49{\pm}6.9$ pA(n=3), respectively. Glycine $(1{\mu}M)$ potentiated glutamate-induced currents $4{\sim}5$ times and NMDA-induced currents $8{\sim}10$ times. In addition, glycine $(30{\mu}M)$ induced Inward current ($31{\pm}6.1$ nA, n=2), which was rapidly desensitized after the peak to a new steady-state level. However, the inward currents induced by ${\gamma}-amino$ butyric acid(GABA, $1{\mu}M$) decreased continuously after the peak($226{\pm}41.6$ pA, n=3) under the similar experimental condition. The ionic currents and pharmacological responses of isolated neurons in this work were similar to those observed in vivo or in vitro spinal cord slice, indicating that acutely isolated neurons could be effectively used for further pharmacological studies.

• Herbal Formula Science
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• v.22 no.2
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• pp.25-34
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• 2014

Objectives : Excessive nutrition intake and lack of physical activity induce obesity through accumulation of fat in human body. The obesity have been categorized as a disease and known to cause several chronic diseases and cancers. In Japan, Bangpungtongsung-san has been applied as one of the therapies of the obesity and it's pharmacological uses have been studied for a long time. The purpose of this study is reviewing researches of Bangpungtongsung-san related to the obesity. Methods : By searching with the keyword of "Bangpungtongsung-san" or related words such as "Bofutsushosan" and 'TJ-62" from PubMed and off-line libraries, many reports were gathered and reviewed from the perspective of the obesity. Results and Conclusions : It has become evident by reviewing the reports that Bangpungtongsung-san is useful as a therapy of the obesity though some case reports showed side effects. Also, the mechanisms of Bangpungtongsung-san on obesity were reviewed and suggested.

• The Korea Journal of Herbology
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• v.35 no.5
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• pp.13-21
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• 2020

Objective : The genus Glycyrrhiza has been used in food and traditional herbal medicine. Many experimental studies reported that Glycyrrhiza species possess several pharmacological properties. Glycyrrhiza new varieties WONGAM and SINWONGAM have been developed by Korea Rural Development Administration doing research for registration on Ministry of Food and Drug Safety. During the evaluations about pharmacological effect of Glycyrrhiza new varieties WONGAM and SINWONGAM, we focused the anti-allergic effect in this study. Methods : We investigated the anti-allergic effect of WONGAM and SINWONGAM compared with Glycyrrhiza uralensis Fischer and G. glabra L. using anti-dinitrophenyl-immunoglobulin E (IgE)/human serum albumin-stimulated RBL-2H3 cells, phorbol 12-myristate 13-acetate plus calcium ionophore A23187-stimulated HMC-1 cells and compound 48/80-induced anaphylaxis mice model. We analyzed the effect on the expression of various cytokines, and IgE from mast cells and the underlying molecular mechanisms of WONGAM and SINWONGAM in presented models. Results : WONGAM and SINWONGAM showed the inhibitory effect on the histamine release from rat peritoneal mast cells or human mast cells without cytotoxicity. WONGAM and SINWONGAM blocked anaphylactic shock and decreased the IgE production. Furthermore, WONGAM and SINWONGAM inhibited the productions of TNF-α and IL-6 in compound 48/80-induced anaphylaxis mice model. Conclusion : These results indicated that WONGAM and SINWONGAM would have protect effect on allergic responses through the inhibition of allergic mediators and pro-inflammatory cytokines. This study may facilitate the development on Glycyrrhiza new varieties for allergy.