• Archives of Pharmacal Research
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• v.2 no.2
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• pp.121-125
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• 1979

Piperine showed a central nervous system depressant activity which was characterized by the antagonistic effect against chemoshock seizure as well as potent muscular incoordination in mice.

• Proceedings of the Korean Society of Plant Pathology Conference
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• 1999.10a
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• pp.66.2-66
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• 1999

• Archives of Pharmacal Research
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• v.23 no.4
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• pp.324-328
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• 2000

Three dimensional QSAR studies for antihistamine and antibradykinin effects of new piperazine derivatives were conducted using the comparative molecular field analysis. Electrostatic and steric factors, but not hydrophobic factor, of the synthesized compounds were correlated with the antagonistic effect.

• Korean Journal of Pharmacognosy
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• v.17 no.3
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• pp.215-222
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• 1986

Although the 'Insamyangwee-tang' has been widely used in clinical purposes in the oriental medicine, its clinical efficacy is only documentated for the cases of gastritis, gastric ulcer and enteritis, but the experimental study on these has not been undertaken. So, to investigate the clinical efficacy of 'Insamyangwee-tang' comparing with animal experiments, This study was carried out. The results showed that relaxing action was shown on the isolated ileum in mice and that strong antagonistic actions were seen on $BaCl_2$, acetylcholine and histamine induced contraction of the ileum in mice, rats, rabbits and guinea-pigs that the relaxing effect of the intestinal smooth muscle was recognized. Inhibitory effects on transport rate in the small intestine of mice. Strong antagonistic actions were seen on acetylcholine induced contraction of duodenum in rats and remarkably inhibiting actions were seen of duodenum in rats. Inhibitory action on the secretion of gastric juice and pepsin, anti-ulceration effect was recognized.

• YAKHAK HOEJI
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• v.33 no.3
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• pp.167-174
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• 1989

KR-1008 and KR-30006 are 1,4-dihydropyridine derivatives, new vasodilatory calcium antagonists from KRICT. Calcium antagonistic properties of the compounds were studied in the isolated heart (Langendorff preparation), pulmonary artery (vasodilation), and in the papillary muscle (negative inotropic effect) of the guinea pig. Antihypertensive effect were also investigated after i.v. or oral administration in the SHR (spontaneously hypertensive rat). They produced a sigificant inhibition of Ca-induced contraction in the guinea pig pulmonary artery at the concentrations of above $10^{-8}M$. The negative inotropic effect of the electrically stimulated papillary muscle appeared from the concentration of $10^{-6}M$, which is about hundred times higer than the concentration of vasodilation effect. Left ventricular pressure also decreased from the concentration of $3\;{\times}\;10^{-6}M$ in KR-1008 and KR-3006 in the Langendorff heart preparations. Coronary flow rate increased from $10^{-6}M$ in KR-1008 and nicardipine and appeared no change in KR-30006. The antihypertensive effect of KR-1008 (EC 20: $2.9\;{\mu}g/kg$) was potent more than nicardipine (EC 20: $3.4\;{\mu}g/kg$) and than Kr-30006 (EC 20: $6.8\;{\mu}g/kg$) was, after i.v. bolus injection in the anesthetized SHR. The antihypertensive effect in the conscious SHR appeared 30 minutes after oral administration of 10 mg/kg and persisted 4 hrs in KR-1008 and 12 hrs in KR-30006. Heart rate tended to increase for 0.5-1 hr after oral administration of the test compounds.

• Korean Journal of Environmental Agriculture
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• v.35 no.4
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• pp.241-246
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• 2016

BACKGROUND: Recently, the widespread distribution of pesticides in the hive has been of concern about pesticide exposure on honeybee (Apis mellifera L.) health. Larval toxicity was adapted to assess the synergistic and antagonistic interaction of cumulative mortality to the honeybee larvae of the four most common pesticides detected in pollen. METHODS AND RESULTS: Acetamiprid($3.0{\mu}l/L$), chlorothalonil ($803.0{\mu}l/L$), coumaphos ($128.0{\mu}l/L$), and tau-fluvalinate ($123.0{\mu}l/L$) were tested in combination; binary, ternary and four component mixture. Larvae were exposed to four pesticides mixed in diet at the average levels detected in pollen. As a result, synthetic toxicity was observed in the binary mixture of acetamiprid with coumaphos. The binary and ternary component mixtures of tested pesticides have mostly demonstrated additive effect in larval bees. The significant antagonistic effects were found in four parings of mixtures including chlorothalonil added to acetamiprid/tau-fluvalinate or acetamiprid/coumaphos/tau-fluvalinate, and tau-fluvalinate added to acetamiprid/chlorothalonil or acetamiprid/coumaphos/chlorothalonil. CONCLUSION: Interactions between combinations of four pesticides showed mostly additive or antagonistic effects in larval bees. Therefore, predicting the larval mortality of pesticides mixtures on the basis of the results of single pesticide may actually overestimate the risk. We suggest that pesticide mixture in pollen be evaluated by adding their toxicity together for complete data on interactions.

• Korean Journal of Weed Science
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• v.18 no.2
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• pp.161-170
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• 1998

Antagonistic mode of action of fenoxaprop-P-ethyl [ethyl(R)2-4-{(6-chloro-2-benzoxazolyloxy) phenoxy}propionate] with bentazon was investigated with respect to absorption, translocation, metabolism, and change in target site response of fenoxaprop-P-ethyl using four-leaf stage of rice(Oryza sativa L.) and barnyardgrass [Echinochloa eras-galli (L.) P. Beauv.]. Shoots of rice and barnyardgrass was more sensitive to fenoxaprop-P-ethyl than the roots. More than 90% of fenoxaprop-P-ethyl was absorbed within 6 hours after treatment and 30% of the absorbed was acropetally and basipetally translocated at 24 hours after treatment. Fenoxaprop-P-ethyl was rapidly transformed to its acid form, fenoxaprop(2-[4-(6-chloro-2-benzoxazolyloxy)phenoxy]propionic acid), which was subsequently metabolized to polar conjugates. However, changes in absorption, translocation, and metabolism of fenoxaprop-P-ethyl by bentazon treatment were not found in both species. Background activity of acetyl-CoA carboxylase(ACCase) in rice and barnyardgrass was 26.5 and 23.2nmol/min/mg, respectively. Concentration required to inhibit fifty percent enzyme activity$(I_{50})$ in vitro was 6.5~7.4${\mu}M$ of fenoxaprop-P-ethyl and more than 500${\mu}M$ of bentazon. There were no significant differences in $I_{50}$ value between two treatments of fenoxaprop-P-ethyl alone and its bentazon mixture. However, bentazon reduced ACCase activity in vivo and inhibited electron transport in chloroplast thylakoid. Based on the results obtained, it is concluded that the antagonistic effect of bentazon occurs due not to direct effect on target site of fenoxaprop-P-ethyl, but to indirect involvement in reducing herbicidal activity of fenoxaprop-P-ethyl through physiological disturbances caused by bentazone at whole chloroplast level.

• Journal of Ginseng Research
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• v.11 no.2
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• pp.123-129
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• 1987

Antagonisms of the analgesic effect of morphine in mice by ginsenoside Rbl, Rb2, Rgl and Re were investigated in these experiments. These ginsenosides antagonized the analgesic effect induced by morphine in mice and the administration of 2,4-dihy-droxyphenylalanine or 5-hydroxytryptophan reduced the antagonisms of morphine analgesia by the ginsenosides. Possible mechanisms involved in the antagonistic actions of the ginsenosides on morphine analgesia were described.

• The Korean Journal of Mycology
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• v.44 no.1
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• pp.36-47
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• 2016

This study was conducted to evaluate five different strains of rhizobacterial isolates viz. PA1, PA2, PA4, PA5 and PA12 for biological control against Colletotrichum acutatum, C. coccodes, C. gloeosporioides, C. dematium, Botrytis cinerea, Rhizoctonia solani, Sclerotinia minor and Fusarium sp. In vitro inhibition assay was performed on three different growth mediums, potato dextrose agar (PDA), tryptic soy agar (TSA), and PDA-TSA (1:1 v/v) for the selection of potential antagonistic isolates. According to the result, isolate PA2 showed the highest inhibitory effect with 65.5% against C. coccodes on PDA and with 96.5% against S. minor on TSA. However, the same isolate showed the highest inhibition with 58.5% against C. acutatum on PDA-TSA. In addition, an in vivo experiment was performed to evaluate these bacterial isolates for biological control against fungal pathogens. Plants treated with bacteria were analyzed with phytopathogens and plants inoculated with phytopathogens were treated with isolates to determine the biological control effect against fungi. According to the result, all five isolates tested showed inhibitory effects against phytopathogens at various levels. Mode of action of these rhizobacterial isolates was evaluated with siderophore production, protease assay, chitinase assay and phosphate solubilizing assay. Bacterial isolates were identified by 16S rDNA sequencing, which showed that isolates PA1 and PA2 belong to Bacillus subtilis, whereas, PA4, PA5, and PA12 were identified as Bacilus altitudinis, Paenibacillus polymyxa and Bacillus amyloliquefaciens, respectively. Results of the current study suggest that rhizobacterial isolates can be used for the plant growth promoting rhizobacteria (PGPR) effect as well as for biological control of various phytopathogens.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.10
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• pp.4369-4376
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• 2015

Background: To investigate in-vitro antagonistic effect of low-dose liquiritigenin on gemcitabine-induced capillary leak syndrome (CLS) in pancreatic adenocarcinoma via inhibiting reactive oxygen species (ROS)-mediated signalling pathways. Materials and Methods: Human pancreatic adenocarcinoma Panc-1 cells and human umbilical vein endothelial cells (HUVECs) were pre-treated using low-dose liquiritigenin for 24 h, then added into gemcitabine and incubated for 48 h. Cell viability, apoptosis rate and ROS levels of Panc-1 cells and HUVECs were respectively detected through methylthiazolyldiphenyl-tetrazoliumbromide (MTT) and flow cytometry. For HUVECs, transendothelial electrical resistance (TEER) and transcellular and paracellular leak were measured using transwell assays, then poly (ADP-ribose) polymerase 1 (PARP-1) and metal matrix proteinase-9 (MMP9) activity were assayed via kits, mRNA expressions of p53 and Rac-1 were determined through quantitative polymerase chain reaction (qPCR); The expressions of intercellular adhesion molecule 1 (ICAM-1), vascular cell adhesion molecule-1 (VCAM-1) and PARP-1 were measured via western blotting. Results: Low-dose liquiritigenin exerted no effect on gemcitabine-induced changes of cell viability, apoptosis rate and ROS levels in Panc-1 cells, but for HUVECs, liquiritigenin ($3{\mu}M$) could remarkably elevate gemcitabine-induced decrease of cell viability, transepithelial electrical resistance (TEER), pro-MMP9 level and expression of ICAM-1 and VCAM-1 (p<0.01). Meanwhile, it could also significantly decrease gemcitabine-induced increase of transcellular and paracellular leak, ROS level, PARP-1 activity, Act-MMP9 level, mRNA expressions of p53 and Rac-1, expression of PARP-1 and apoptosis rate (p<0.01). Conclusions: Low-dose liquiritigenin exerts an antagonistic effect on gemcitabine-induced leak across HUVECs via inhibiting ROS-mediated signalling pathways, but without affecting gemcitabine-induced Panc-1 cell apoptosis. Therefore, low-dose liquiritigenin might be beneficial to prevent the occurrence of gemcitabine-induced CLS in pancreatic adenocarcinoma.