• Korean Journal of Clinical Laboratory Science
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• v.51 no.2
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• pp.235-244
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• 2019

This study examined the neurotoxicity of aluminum sulfate (AS), an environmental pollutant, and the protective effect of Phrymaleptostachya var. asiatica HARA (PLVAH) extract on the neurotoxicity induced by AS in the cultured C6 glioma cells. For this study, the cell viability and antioxidative effects, such as electron donating (ED) activity, lipid peroxidation (LP) activity, and superoxide anion-radical (SAR) scavenging activity, were analyzed. AS decreased the cell viability significantly in a dose-dependent manner and the $XTT_{50}$ value was measured at $120.0{\mu}M$ of AS. The neurotoxicity of AS was determined to be mid-toxic by Borenfreund and Puerner's toxic criteria. In addition, the catalase (CAT), antioxidant enzyme remarkably increased the cell viability injured by AS-induced neurotoxicity in these cultures. Regarding the protective effect of the PLVAH extract on AS-induced neurotoxicity, PLVAH extract significantly increased the ED ability, and the inhibitory ability of the LP and SAR scavenging ability. These findings suggest that oxidative stress is involved in the cytotoxicity of AS, and the PLVAH extract effectively protected against AS-induced neurotoxicity by its antioxidative effects. Natural resources, such as the PLVAH extract may be a putative therapeutic agent for the treatment of the toxicity induced by heavy metallic compounds, such as AS correlated with the oxidative stress.

• Bulletin of the Korean Chemical Society
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• v.26 no.11
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• pp.1757-1760
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• 2005

A series of 6-alkyloxyl-3,4-dihydro-2(1H)-quinoliones (5a-5n) were synthesized through nitration, reduction, diazotization, hydrolysis and alkylation from 3,4-dihydro-2(1H)-quinolione. Their structures were characterized by IR, $^1H$-NMR and MS. The anticonvulsant activity was evaluated by the Maximal electroshock test (MES) and the subcutaneous pentylenetetrazole (Metrazole) test (sc-Met). The neurotoxicity was measured by the Rotarod test (Tox). The result showed that 6-hexyloxy-3,4-dihydro-2 (1H)-quinolinone (5c) was potent in anti-MES and anti-scMet test with $ED_{50}$ of 24.0 mg/kg and 21.2 mg/kg, respectively, albeit its $TD_{50}$ (67.6 mg/kg) revealed the high neurotoxicity. 6-Benzyloxy-3,4-dihydro-2(1H)-quinolinone (5f) was less effective against MES induced seizure with $ED_{50}$ of 29.6 mg/kg, but no neurotoxicity was observed even under 300 mg/kg. Its Protective index (PI) was greater than 10 preferable to Phenytoin, Carbamazepin, Phenobarbital and Valproate.

• Analytical Science and Technology
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• v.14 no.2
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• pp.191-195
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• 2001

Cucurbitacin D and F, the protostane type triterpenoid of S. sorbifolia, were isolated with chromatograpic method and used as the standard substances for quantitative analysis. The compounds were identified with $^1H$-NMR, FAB-MS and UV spectrophotometer. They were separated on YMC-Pack ODS-AQ(303)[$250{\times}4.6mm$ I.D., $S-5{\mu}m$, 120A] column by HPLC. Cucurbitacin F was detected at 10.73mg/kg in cortex of S. sorbifolia, but cucurbitacin D was not. The compounds were shown to exihibit significant cytotoxicity($ED_{50}$<$0.1{\mu}g/mL$) against several tumor cell lines and acute toxicity(cucurbitacin D: 4.7mg/kg/day, cucurbitacin F: 2.5mg/kg/day) against BDF-1 mouse.

• The Journal of Internal Korean Medicine
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• v.17 no.1
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• pp.210-217
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• 1996

Farfarae Flos, 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 Farfarae Flos on histamine-induced tracheal smooth muscle contraction in rats. Guinea pigs(500g, female) were killed by CO2 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 (ED50) was obtained from cumulative dose response curves for histamine (10-7-10-4M). Contractions evoked by histamine(ED50) were inhibited significantly by Farfarae Flos. The mean percent inhibition was 8.7% after 1.5mg/ml Farfarae Flos, and 33.5% (p<0.05) after 5.0mg/ml Farfarae Flos. Propranolol (10-7M) slightly but significantly attenuated the inhibitory effects of Farfarae Flos. Following treatment with propranolol, the mean percent inhibition caused by 5.0mg/ml Farfarae Flos. Indomethacin and methylene blue (10-7M) did not significantly alter the inhibitory effect of Farfarae Flos. These results indicate that Farfarae Flos can relax histamine-induced contraction of guinea pig tracheal smooth muscle, and that this inhibition involves, in part, symphathetic nerve system.

• Journal of Physiology & Pathology in Korean Medicine
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• v.16 no.2
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• pp.322-326
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• 2002

Artemisia iwayomogi has been used in Korea for many centuries as a treatment for anemia. The effect of Artemisia iwayomogi on tracheal smooth muscle is not known. The purpose of the present study is to determine the effect of Artemisia iwayomogi on histamine induced tracheal smooth muscle contraction in guinea pigs. Guinea pigs(500g, male) were killed by CO₂ exposure and a segment (8-10mm) of the thoracic trachea from each rat and 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 (His) which evoked 50% of maximal response (ED/sub 50/) was obtained from cumulative dose response curves for histamine (10/sup -7/～10/sup -4/M). Contractions evoked by His (ED/sub 50/) were inhibited significantly by Artemisia iwayomogi. In guinea pig tracheal smooth muscle, the mean percent inhibition of histamine induced contraction was 31.9% (p<0.05) after 100㎕/㎖ Artemisia iwayomogi. L-NNA slightly but significantly attenuated the inhibitory effects of Artemisia iwayomogi. Following treatment with L-NNA, the mean percent inhibition caused by 100㎕/㎖ Artemisia iwayomogi fell to 44.6% in guinea pig induced by histamine contraction. Propranolol, indomethacin and methylene blue did not significantly alter the inhibitory effect of Artemisia iwayomogi. These results indicate that Artemisia iwayomogi can relax histamine induced contraction of guinea pig, and that this inhibition related to nitric oxide formation.

• The Korean Journal of Pain
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• v.18 no.2
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• pp.118-123
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• 2005

Background: A nerve ligation injury may produce a tactile allodynia. The effects of intrathecally delivered lamotrigine on allodynia induced due to fifth and sixth lumbar spinal nerves ligation in rats, using lumbar intrathecal catheters were examined. Methods: Sprague-Dawley rats (body weight 160-180 g) were prepared by tightly ligating the fifth and sixth left lumbar spinal nerves, with the implantation of a chronic intrathecal catheter for drug administration. Mechanical allodynia and allodynic threshold were measured using von Frey filaments and the updown method, respectively. After the baseline hind paw withdrawal thresholds had been obtained, lamotrigine (10, 30, 100 and $300{\mu}g$) was administered intrathecally. Thereafter, the dose-response curves and 50% effective dose ($ED_{50}$) were obtained. Motor dysfunction was assessed by observing the righting/stepping reflex responses and abnormal weight bearing. Results: Intrathecal administration of lamotrigine produced a dose-dependent antiallodynic action ($ED_{50}=61.7{\mu}g$). Mild motor weakness was observed with $300{\mu}g$ lamotrigine, but no severe motor impairment was found. Conclusions: It is suggested that intrathecal lamotrigine could produce moderate antagonism of mechanical allodynia at the spinal level in a rat neuropathic pain model with minimal motor weakness.

• Archives of Pharmacal Research
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• v.21 no.3
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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.

• The Journal of Korean Medicine
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• v.17 no.2 s.32
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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.

• Herbal Formula Science
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• v.10 no.2
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• pp.143-158
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• 2002

The purpose of the present study is to determine the effect of Jakyakgamchotang on histamine or acetylcholine induced tracheal smooth muscle contraction in rats and guinea pigs. Guinea pig(500g, male) and Sprague Dawley rats(250g, male) were killed by $CO_2$ exposure and a segment (4-5mm) of the thoracic trachea from each rat and 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(His) which evoked 50% of maximal response($ED_{50}$) was obtained from cumulative dose response curves for histamine($10^{-7}{\sim}10^{-4}M$). Contractions evoked by His($ED_{50}$) were inhibited significantly by Jakyakgamchotang. In guinea pig tracheal smooth muscle, the mean percent inhibition of histamine induced contraction was 90.8% (p〈0.001) after $100{\mu}l/ml$ Jakyakgamchotang. In rat tracheal smooth muscle, the mean percent inhibition of acetylcholine induced contraction was 22.1% (p〈0.05) after $100{\mu}l/ml$ Jakyakgamchotang. Propranolol indomethacin and methylene blue($10^{-7}M$) slightly but significantly attenuated the inhibitory effects of Jakyakgamchotang. These results indicate that Jakyakgamchotang can relax histamine or acetylcholine induced contraction of guinea pig and rat tracheal smooth muscle.

• The Korean Journal of Pain
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• v.25 no.1
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• pp.1-6
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• 2012

Background: Curcumin has been reported to have anti-inflammatory, antioxidant, antiviral, antifungal, antitumor, and antinociceptive activity when administered systemically. We investigated the analgesic efficacy of intrathecal curcumin in a rat model of inflammatory pain. Methods: Male Sprague Dawley rats were prepared for intrathecal catheterization. Pain was evoked by injection of formalin solution (5%, $50{\mu}l$) into the hind paw. Curcumin doses of 62.5, 125, 250, and $500{\mu}g$were delivered through an intrathecal catheter to examine the flinching responses. The $ED_{50}$ values (half-maximal effective dose) with 95% confidence intervals of curcumin for both phases of the formalin test were calculated from the dose-response lines fitted by least-squares linear regression on a log scale. Results: In rats with intrathecal administration of curcumin, the flinching responses were significantly decreased in both phases. The slope of the regression line was significantly different from zero only in phase 2, and the $ED_{50}$ value (95% confidence interval) of curcumin was $511.4{\mu}g$ (23.5-1126.5). There was no apparent abnormal behavior following the administration of curcumin. Conclusions: Intrathecal administration of curcumin decreased inflammatory pain in rats, and further investigation to elucidate the precise mechanism of spinal action of curcumin is warranted.