• Animal cells and systems
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• 제16권5호
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• pp.366-375
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• 2012

Gallotannin (GT) is derived from plant poly phenol and is associated with biological actions in a wide range of cells. In this study, we evaluated the effect of GTon apoptosis and cyclooxygenase-2 (COX-2) expression and attempted to shed light on the mechanism of action in A549 human lung carcinoma cells. We found that GT dramatically induced apoptosis as demonstrated by expression of p53 and active caspase-3 via western blot analysis and fragmented DNA as detected by DNA fragmentation and DAPI staining. We also observed that GT significantly causes COX-2 expression in a dose-dependent manner determined by western blot analysis. Phosphorylation of Akt and p38 was considerably increased by GT in A549 human lung carcinoma cells. Inhibition of Akt and p38kinase with LY294002 or SB203580 suppressed GT-induced apoptosis and COX-2 expression. Furthermore, we have shown that prevention of COX-2 with NS398 or indomethacin does not any effects on apoptosis induced by GT. Taken together, our present results suggest that GT regulates apoptosis and COX-2 expression through Akt and p38kinase pathway in A549, human lung carcinoma cells.

• Archives of Pharmacal Research
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• 제21권3호
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• pp.241-247
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• 1998

This study was designed to determine biochemical and pharmacological properties of a newly synthesized benzimidazole derivative, 2-amino-4, 5-dihydropyrido [1, 2-a] thiazolo [5, 4-g] benzimidazole (YJA20379-5) in vitro and in vivo. In the leaky membrane vesicles of pig gastric mucosa, YJA20379-5 inhibited the $K^+$-stimulated $H^+$, $K^+$-ATPase activity in a concentration- and time-dependent manner, with $IC_{50}$ values being $43{\mu}\textrm{M}$ and $43{\mu}\textrm{M}$ at pH 6.4 and 7.4, respectively. YJA20379-5, given intraduodenally, had a potent inhibitory effect on the gastric acid secretion in pylorus-ligated rats. The $ED_{50}$ value for acid secretion was 15.4 mg/kg. YJA20379-5, administered orally, also suppressed gastric damages induced by water-immersion stress, indomethacin and ethanol, and duodenal damage induced by mepirizole in rats; the $ED_{50}$ values were 17.6, 4.7, 3.0 and 18.7 mg/kg, respectively. Furthermore, repeated oral administration of YJA20379-5 accelerated the spontaneous healing of acetic acid-induced gastric ulcers in rats. It is concluded that the a-ntisecretory activity of YJA20379-5 appears to be associated with inhibition of $H^+$, $K^+$-ATPase, while its antigastric and antiduodenal lesion activities are primarily related to the antisecretory effect.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1993년도 학술대회지
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• pp.40-48
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• 1993

Intravenous administration of saponin extracted from the root of Panax ginseng lowered the blood pressure dose-dependently (10-200 mg/kg, B.W) in anesthetized rats. Therefore, experiments were designed to study the hypothesis that the lowering of blood pressure is associated with the release of endothelium-derived relaxing factor and the accumulation of guanosine 3, 5-cyclic monophosphate (cGMP). Rings of thoracic aorta with and without endothelium were suspended for the measurement of isometric tension in organ chamber and the tissue content of cGMP was measured by radioimmunoassay. All experiments were performed in the presence of $indomethacin(10^{-5}M).$ Ginseng saponin $(10^{-5}-3{\times}10^{-6}g/ml)$ relaxed contractions induced by phenylephrine $10^{-6}M)$ in the aorta with endothelium but not in that without endothelium. Treatment of aortic rings with $N^G$ monomethyl-L-arginine (L-NMMA, $10^{-4}M$ for 30 min), a competitive inhibitor of nitric oxide synthase, and methylene blue $(MB,\;3{\times}10^{-7}M$ for 30 min). an inhibitor of soluble guanylate cyclase, diminished the relaxation induced by Ginseng saponin. Ginseng saponin $10^{-4}g/ml$ for 2 min) increased the accumulation of cGMP in rings with endothelium. L-NMMA and MB inhibited the accumulation of cGMP induced by Ginseng saponin. These data suggest that vascular relaxations induced by Ginseng saponin are mediated by release of endothelium-derived relaxing factor and the accumulation of cGMP. The effect of Ginseng saponin on endothelial function in hypercholesterolemic rabbits was examined. In hypercholesterolemic rabbits fed with $2\%$ cholesterol for 8 weeks, relaxation of aortic rings to acetylcholine was impaired. The impaired relaxations of aortic rings in hypercholesterolemic rabbits were improved by dietary supplementation of Ginseng saponin, probably because of an improved release of endothelium - derived relaxing factor.

• 동의생리병리학회지
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• 제17권5호
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• pp.1194-1201
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• 2003

Jaeumgenby-tang(JGT) have been used in oriental medicine for many centries as a therapeutic agent of vertigo caused by deficiency of qi(氣) and blood(血). Effect of Aurantii Fructus(AF) take off the phlegm by promoting the circulation of qi, Gastrodae Rhizoma(GR) has effects treating for headarch, vertigo by calming the liver and suppressing hyperactivity of the liver-yang (陽). I investigated whether injection of JGT adding AFㆍGR extract(JTG) affects cerebral hemodynamics [regional cerebral blood f1ow(rCBF), pial arterial diameter(PAD) in cerebral ischemia rats by MCA occlusion method, and I designed to make manifest whether JTG is mediated by adrenergic β-receptor, cyclooxygenase or guanylate cyclase. The changes of rCBF was determinated by laser-doppler flowmetry(LDF), and the changes of PAD was determinated by video microscope and width analyzer. The results were as follows in cerebral ischemic rats; The changes of rCBF and PAD were increased stabilizly by treatment with JTG(10 ㎎/kg, i.v.) during the period of cerebral reperfusion, and pretreatment with propranolol and indomethacin were increased JTG induced increase of rCBF and PAD during the period of cerebral reperfusion. Pretreatment methylene blue was decreased JTG induced increase of rCBF and PAD during the period of cerebral reperfusion. In conclusion, JTG causes a diverse response of rCBF and PAD, and action of JTG is mediated by adrenergic β-receptor and cyclooxygenase. I suggest that JTG has an anti-ischemic effect through the improvement of crebral hemodynamics.

• 대한한의학회지
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• 제17권2호
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• pp.296-302
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• 1996

Pericarpium Citri Nobilis Viride, a traditional herb medicine, has been used in Korea and China for many centuries as a treatment for respiratory disease. The purpose of the present study was to determine the effect of Pericarpium Citri Nobilis Viride on histamine-induced tracheal smooth muscle contraction in rats. Guinea pigs(500g , female) were killed by $CO_2$ exposure and a segment (8-10mm) of the thoracic trachea from each guinea pig was cut into equal segments and mounted 'in pairs' in a tissue bath. Contractile force was measured with force displacement transducers under 0.5g loading tension. The dose of histamine which evoked 50% of maximal response $(ED_{50})$ was obtained from cumulative dose response curves for histamine $(10^{-7}-10^{-4}M)$. Contractions evoked by histamine ($ED_{50}$) were inhibited significantly by Pericarpium Citri Nobilis Viride. The mean percent inhibition was 53.7% (P<0.05) after 1.5mg／ml Pericarpium Citri Nobilis Viride, and 87.7% (P<0.01) after 5.0mg／ml Pericarpium Citri Nobilis Viride. Propranolol $(10^{-7}M)$ slightly but significantly attenuated the inhibitory effects of Pericarpium Citri Nobilis Viride. Following treatment with propranolol the mean present inhibition caused by 1.5 and 5.0mg／ml Pericarpium Citri Nobilis Viride. Indomethacin and methylene blue $(10^{-7}M)$ did not significantly alter the inhibitory effect of Pericarpium Citri Nobilis Viride These results indicate that Pericarpium Citri Nobilis Viride can relax histamine-induced contraction of guinea pig tracheal smooth muscle, and that this inhibition involves in part symphathetic nerve system.

• Journal of Acupuncture Research
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• 제25권6호
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• pp.1-12
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• 2008

Objectives : Joongjeo($TE_3$) Supplementation Aekmoon($TE_2$) Draining is a method belongs to Ohaeng-acupuncture, using directional supplementation and draining. Methods : This study was designed to investigate the effects of $TE_3$ supplementation $TE_2$ draining on changes in cerebral blood flow(rCBF) and mean arterial blood pressure(MABP) in normal rats. For these reasons, the present author investigated rCBF and MABP using laser doppler flowmeter in normal rats. In addtion, the present author also investigated action mechanisms of $TE_3$ supplementation $TE_3$ draining on changes in rCBF and MABP too. Results : In this results, $TE_3$ supplementation $TE_2$ draining elevated rCBF in time-dependent manner, but MABP levels decresed by $TE_3$ supplementation $TE_2$ draining. Pre-treatment with indomethacin (IDM), an inhibitor of cyclooxygenase, inhibited increase of rCBF effectively. But pre-treatment with methylene blue(MTB), an inhibitor of guanylate cyclase, decreased rCBF levels. In addition, pre-treatment with IDM also decreased MABP levels, but pre-treatement with MTB increased MABP levels. Conclusions : In conclusion, these results suggest that $TE_3$ supplementation $TE_2$ draining is effective to treat patient with disease related to cerebral ischemia, because $TE_3$ supplementation $TE_2$ draining can increase rCBF. In addition, the mechanisms are thought to be related to guanylate cyclase pathways.

• 대한본초학회지
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• 제23권4호
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• pp.71-79
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• 2008

Objectives: SimJeok-Hwan(CP, Cardiotonic Pills) was made to treat patients with coronary arteriosclerosis, angina pectoris and hyperlipidemia. This study was designed to investigate the effects of CP on Proliferation rates neuroglia cells and protective effect of CP against oxidative stress, and also investigate the effects on regional Cerebral Blood Flow(rCBF) in normal rats. Methods: In this experiment, effects of CP on proliferation rates of neuroglia cells were measured using modified MTT methods. Oxidative stress was induced by treatment with 200 mM of hydrogen peroxide for 2 hr. rCBF and MABP were measured using Laser doppler flowmeter. Results: Treatment with CP elevated proliferation rates in C6 cells. In addition, CP protected cell death of C6 cells induced by oxidative stress. In results, rCBF was elevated by treatment with CP in normal rats. But, Mean Arterial Blood Pressure(MABP) did not affected by CP. In addition, the elevation of rCBF was blacked by pre-treatment with 1 mg/kg of indomethacin effectively. On the other hand, pre-treatment with 0.01 mg/kg of methylene blue did not affect rCBF level in normal rats. Conclusions: In conclusion, these results suggest that CP can act as anti-oxidant to protect neuroglia cells and also suggest that CP can elevate rCBF, which are involved in cyclooxygenase pathway.

• 대한본초학회지
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• 제35권6호
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• pp.55-68
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• 2020

Objectives : We observed the possibilities that blue honeysuckle has favorable analgesic or refinement effects on the Primary dysmenorrhea (PD) in rats. Methods : Estradiol benzoate and oxytocin were used to induce the PD rat model. And Blue honeysuckle concentration lyophilized powders (BH) 500, 250 and 125 mg/kg and 500 mg/kg of Lonicerae Flos aqueous extract lyophilized powders (LF) were orally administered, once a day for 10 days at 30 min after each estradiol benzoate treatment. Then the changes on the body weights and gains during experimental periods, abdominal writhing response for analgesic activities, uterine weights, uterus lipid peroxidation, antioxidant defense system - glutathione contents, superoxide dismutase and catalase activities, NF-κB and COX-2 mRNA expressions were monitored with uterus histopathology including immunohistochemistry for tumor necrosis factor (TNF)-α and inducible nitric oxide synthase (iNOS).. Results : Inflammatory and oxidative stress mediated PD signs were favorably and dose-dependently inhibited by 10 days continuous oral administration of three different dosages of BH - 500, 250 and 125 mg/kg as comparable to those of indomethacin(IND) 5 mg/kg treated rats in BH 500 mg/kg administered PD rats, and similar to those of LF 500 mg/kg in BH 125 mg/kg, at least in a condition of the present PD rat model. Conclusions : The results suggest that BH has favorable analgesic and refinement activities on the estradiol benzoate and oxytocin treatment-induced PD signs through anti-inflammatory and antioxidative potentials.

• 대한한의학방제학회지
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• 제17권2호
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• pp.175-186
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• 2009

The vasorelaxant effect of an extract of Lophatherum gracile Brongn (ELB) and its possible action mechanism were ascertained in aortic tissues isolated from rats. ELB relaxed endothelium-intact thoracic aorta in a dose-dependent manner. However, the induced vascular relaxation was abolished by removal in endothelium of the thoracic aorta. Pretreatment of endothelium-intact vascular tissues with $N^G$-nitro-L-arginine methyl ester (L-NAME) or 1H-[1,2,4]-oxadiazole-[4,3-$\alpha$]-quinoxalin-1-one (ODQ) significantly inhibited vascular relaxation induced by ELB. Moreover, ELB significantly increased cGMP production in aortic tissues, which was blocked by pretreatment with L-NAME or ODQ. The vasorelaxant effect of ELB was attenuated by tetraethylammonium (TEA), and glibenclamide. ELB-induced vasorelaxation was not blocked by atropine, propranolol, indomethacin, verapamil, and diltiazem. Taken together, the present study demonstrates that ELB dilates vascular smooth muscle via an endothelium-dependent NO-cGMP signaling pathway, which may be at least in part related with the function of $K^+$ channels.

• Clinical and Experimental Pediatrics
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• 제60권6호
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• pp.175-180
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• 2017

Purpose: Plasma level of B-type natriuretic peptide (BNP), an emerging, sensitive, and specific biomarker of hemodynamically significant patent ductus arteriosus (PDA), rapidly decreases in infants receiving cyclooxygenase inhibitors for ductal closure. We investigated the usefulness of serial BNP measurement as a guide for individual identification of early constrictive responses to ibuprofen in preterm infants with symptomatic PDA (sPDA). Methods: Before March 2010, the standard course of pharmacological treatment was initiated with indomethacin (or ibuprofen) and routinely followed by 2 additional doses at intervals of 24 hours. After April 2010, individualized pharmacological treatment was used, starting with the first dose of ibuprofen and withholding additional ibuprofen doses if the BNP concentration was <600 pg/mL and clinical symptoms of PDA improved. Results: The BNP-guided group received significantly fewer doses of ibuprofen than the standard group did during the first course of treatment and the entire study period. The need for further doses of cyclooxygenase inhibitors and for surgical ligation was not significantly different between the 2 groups. No significant differences were seen in clinical outcomes and/or complications related to sPDA and/or pharmacological treatment. Conclusion: Individualized BNP-guided pharmacological treatment may be used clinically to avoid unnecessary doses of cyclooxygenase inhibitors without increasing the ductal closure failure and the short-term morbidity related to sPDA.