• Journal of Pharmaceutical Investigation
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• 제16권2호
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• pp.43-54
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• 1986

To increase the bioavailability of clonixin, clonixin argininate was prepared and compared with clonixin by determining solubility, pKa, lipid-water partition coefficient, dissolution rate and in vivo tests. The results are summerized as followings; 1) The solubility of clonixin argininate was increased by 20 times in water, about 1.2 times in pH 1.2 and pH 8.0 buffer solution, and about 1.8 times in pH 6.8 buffer solution compared with that of clonixin. 2) pKa values of clonixin, clonixin lysinate and clonixin argininate were 6.32, 7.20 and 7.45, respectively. 3) The lipid-water partition coefficient of clonixin argininate was increased more than that of the clonixin in n-hexane, carbon tetrachloride, chloroform, methylene chloride, and n-butanol, but the partition coefficient of clonixin was increased more than that of clonixin argininate in benzene/pH 1.2 buffer solution, ether/pH 8.0 buffer solution, and 3-methylbutyl acetate/pH 1.2, pH 8.0 buffer solution. 4) The time required to dissolve 60% $(T_{60%},\;min.)$ of clonixin argininate was about 1.5 min. in water and pH 1.2 buffer solution, and about 5 min. in pH 6.8 buffer solution. $T_{60%}$ of clonixin lysinate was about 1.5 min. in water, about 1.8 min. in pH 6.8 buffer solution, and about 8 min. in pH 1.2 buffer solution. But $T_{60%}$ of clonixin was about 96 min. in pH 6.8 buffer solution, over 2 hours in water and pH 1.2 buffer solution. 5) Anti-inflammatory effect of clonixin argininate was increased more than that of clonixin over 6 hours, and that of clonixin lysinate was followed by lapse of time. 6) Analgesic effect of clonixin argininate was increased by 1.5 times more than that of clonixin and the effect of clonixin argininate was nearly identical with that of clonixin lysinate. 7) The absorption rates (Ka) of clonixin, clonixin lysinate and clonixin argininate were $0.169\;hr^{-1},\;0.652\;hr^{-1}$ and $0.723\;hr^{-1}$ in situ, respectively.

• The Korean Journal of Physiology and Pharmacology
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• 제24권5호
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• pp.373-384
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• 2020

Paeonol, quercetin, β-sitosterol, and gallic acid extracted from Moutan Cortex had been reported to possess anti-oxidative, anti-inflammatory, and anti-tumor activities. This work aimed to illustrate the potential anti-oxidative mechanism of monomers in human liver hepatocellular carcinoma (HepG2) cells-induced by hydrogen peroxide (H₂O₂) and to evaluate whether the hepatoprotective effect of monomers was independence or synergy in mice stimulated by carbon tetrachloride (CCl₄). Monomers protected against oxidative stress in HepG2 cells in a dose-response manner by inhibiting the generation of reactive oxygen species, increasing total antioxidant capacity, catalase and superoxide dismutase (SOD) activities, and activating the antioxidative pathway of nuclear factor E2-related factor 2/Kelch-like ECH-associated protein 1 (Nrf2/Keap1) signaling pathway. We found that the in vitro antioxidant capacities of paeonol and quercetin were better than those of β-sitosterol and gallic acid. Furthermore, paeonol apparently diminished the levels of alanine transaminase and aspartate aminotransferase, augmented the contents of glutathione and SOD, promoted the expressions of Nrf2 and heme oxygenase-1 proteins in mice stimulated by CCl₄. In HepG2 cells, paeonol, quercetin, β-sitosterol, and gallic acid play a defensive role against H₂O₂-induced oxidative stress through activating Nrf2/Keap1 pathway, indicating that these monomers have anti-oxidative properties. Totally, paeonol and quercetin exerted anti-oxidative and hepatoprotective effects, which is independent rather than synergy.

• 생명과학회지
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• 제23권11호
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• pp.1381-1387
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• 2013

국내에서 식품으로 사용되고 있는 국화과 식물인 곤달비(Ligularia stenocephala) 잎과 뿌리의 생물활성을 과학적으로 검증하기 위하여 각 추출물에 대하여 항산화 활성 및 세포독성을 in vitro에서, 간보호 효과, 알코올 해독작용 및 기억증진 효능 등을 in vivo에서 평가하였으며 잎의 독특한 향기성분을 GC-MS로 분석하였다. 지질과산화 억제효과는 잎(20.4% 억제율)이 뿌리 보다 좋았으며, 유해 라디칼의 일종인 superoxide anion은 뿌리에서 생성 억제효과가 더 좋았고, DPPH 소거활성은 잎과 뿌리 모두 77~79%로 매우 뛰어났다. 사염화탄소로 유발된 급성 간독성 개선효과를 AST와 ALT 효소활성도를 지표로 확인한 결과, 잎의 ALT 억제활성이 대조군에 비해 약 78% 정도 감소하였으며 알코올을 투여한 mouse의 혈중 알코올 농도는 잎추출물 투여시 약 60% 가량 유의성 있게 감소되어 효과를 인정할 수 있었다. 세포독성은 뿌리에서 비교적 강하게 나타났는데, 흑색종의 경우, $IC_{50}=40.14mg/ml$이었으며, 잎의 세포독성은 비교적 약하였다. 기억증진 효과를 동물모델을 이용한 수동회피시험법으로 평가한 결과, 잎과 뿌리 모두 scopolamine에 의해 유도된 기억력 감소를 80% 이상 향상시킨 것으로 조사되었다. 곤달비 잎의 n-헥산 추출물을 GC-MS로 분석한 결과, 독특한 향기는 주로 terpene 화합물에서 유래되는 것으로 추정되었다.

• Nutrition Research and Practice
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• 제7권4호
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• pp.273-280
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• 2013

Bamboo salt, a Korean folk medicine, is prepared with solar salt (sea salt) and baked several times at high temperatures in a bamboo case. In this study, we compared the preventive effects of bamboo salt and purified and solar salts on hepatic damage induced by carbon tetrachloride in Sprague-Dawley rats. Compared with purified and solar salts, bamboo salts prevented hepatic damage in rats, as evidenced by significantly reduced serum levels of aspartate aminotransferase, alanine aminotransferase, and lactate dehydrogenase (P < 0.05). Bamboo salt (baked $9{\times}$) triggered the greatest reduction in these enzyme levels. In addition, it also reduced the levels of the proinflammatory cytokines interleukin (IL)-6, interferon (IFN)-${\gamma}$, and tumor necrosis factor (TNF)-${\alpha}$. Histopathological sections of liver tissue demonstrated the protective effect of bamboo salt, whereas sections from animals treated with the other salt groups showed a greater degree of necrosis. We also performed reverse transcription-polymerase chain reaction and western blot analyses of the inflammation-related genes iNOS, COX-2, TNF-${\alpha}$, and IL-$1{\beta}$ in rat liver tissues. Bamboo salt induced a significant decrease (~80%) in mRNA and protein expression levels of COX-2, iNOS, TNF-${\alpha}$, and IL-$1{\beta}$, compared with the other salts. Thus, we found that baked bamboo salt preparations could prevent $CCl_4$-induced hepatic damage in vivo.

• 한국응용과학기술학회지
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• 제27권3호
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• pp.290-299
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• 2010

The bioactive effects of ethanol extracts from fly maggot (ME) on reduction of plasma lipids levels in rats fed high-fat diets (Expt. Ⅰ), and on liver function recovery of hepatotoxicity rats by intraperitoneal injection of carbon tetrachloride ($CCl_4$) or by orally administration of alcohol (Expt. II) were investigated. In expt. I, twenty seven, male rat SDS(sprague dawley strain) were randomly assigned to three treated groups, including normal control group, HF (group with high fat diets which have no extracts) and HFE (HF plus orally administered doses of ME extract at 5.0 mg/100g of body weight). In expt. II, forty five, male rats (SDS) were randomly assigned to each of the five groups: T1 (control), T2 (intraperitoneal injection of $CCl_4$), T3 (intraperitoneal injection of $CCl_4$ after orally administered with ME), T4 (orally administered with combination of ME and alcohol), T5 (orally administration of ME after orally administered with alcohol). There were significant decreases in plasma (TAG), (TC), (LDL-C) in the HFE group with orally administered doses of ME at 5.0 mg/100g of body weight, respectively, however, the (HDL-C) were significantly increased in HFE group as compared to HF group with high fat diets which have no extracts (p<0.05). The levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), ${\gamma}$-glutamyl transferse(${\gamma}$-GTP) and bilirubin were highest in T2 or T3, and high in order T4 or T5, and lowest in T1 except for bilirubin which has same with T4, T5 (p<0.05). The high recovery of liver damage by $CCl_4$ from the light microscopic appearance was observed in rats (T3) with extracts, and also high in T4 than T5 by orally administrated with alcohol. In conclusion, the ethanol extracts from fly maggot may have a bioactive effects to prevent for human lipids disorder and alcoholic disease.

• 방사선산업학회지
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• 제7권1호
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• pp.81-85
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• 2013

This study was conducted to investigate the effect of fermented blackberry drinks (BD) on carbon tetrachloride ($CCl_4$)-induced liver injury in rats. Male Sprague-Dawley rats were randomly divided into four groups with 6 rats per group: control, $CCl_4$, $CCl_4$ plus BD $3ml\;kg^{-1}$, and $CCl_4$ plus BD $6ml\;kg^{-1}$. We found that the levels of serum aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were significantly increased and the activity of antioxidant enzyme glutathione peroxidase (GPx) in the liver was decreased in rats treated with $CCl_4$ alone when compared with the control group. However, the administration of BD attenuated the levels of serum AST and ALT in $CCl_4$-treated rats. Moreover, the administration of BD significantly increased the activity of GPx in $CCl_4$-treated rat livers. Taken together, these results suggest that BD could protect the liver from $CCl_4$-induced hepatic damage.

• 약학회지
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• 제50권6호
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• pp.358-366
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• 2006

The aim of this study was to investigate the protective effects of glycynhizin, active glycosides of Glycyrrhizae Radix, and baicalin, bioactive flavonoid isolated from Scutellariae Radix, on hepatocyte injury induced by carbon tetrachloride(CCl$_4$, 10 mM), tert-butyl hydroperoxide (TBH, 0.5 mM), and D-galactosamine (GaIN, 30 mM). Primary cultures of rat hepatocyte (18 hr cultured) were treated with CCl$_4$, TBH, or GaIN and various concentrations (0.1, 1, 10, and 100 ${\mu}$M) of glycyrrhizin or baicalin. Activity was accessed by determining the release of lactate dehydrogenase (LDH) and aminotransferses. CCl$_4$ significantly increased the levels of LDH, alanine aminotransferase (ALT), and aspartate aminotransferase(AST) and these increases were prevented by baicalin concentrations of 0.1,1, and 100 ${\mu}$M. The increases in ALT and AST levels were reduced by glycyrrhizin concentration of 100 ${\mu}$M. The level of LDH was markedly increased by TBH, and this increase was reduced by both glycyrrhizin and baicalin. ALT and AST levels were increased by TBH, which were prevented by glycynhizin and bacalin, respectively: GaIN markedly increased the levels of LDH, ALT and AST These increases was significantly reduced by both glycyrrhizin and baicalin. These results suggest that glycynhizin and baicalin possess the hepatoprotective activity.

• 대한약침학회지
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• 제22권1호
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• pp.41-48
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• 2019

Objective: The aim of the study was to evaluate the hepatoprotective activity of the bark extract (Ethanol: Water) in the ratio of (3:1) of Rhizophora mucronata (BERM) by intoxicating the $HepG_2$ cell lines with different toxicants viz, $CCL_4$, Ethanol and Paracetamol with different concentrations of the extract were used. The $HepG_2$ cell lines were subjected to MTT Assay for studying the cytotoxicity. Methods: $HepG_2$ cells were plated using 96 well plate in 10% bovine serum, exposed to different toxicants viz, 2% $CCl_4$, 60% Ethanol and 14 mM Paracetamol respectively. The various test concentrations (18.85, 37.5, 75, 150 and $300{\mu}g/ml$) of bark extract of Rhizophora mucronata was added and incubated for 24 hours. Medium was removed after incubation period and 0.5 mg/ml MTT(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) was added and again incubated for 4 hours at 37oC. Then MTT was removed the crystals was dissolved in DMSO and absorbance was measured at 570 nm. Results: The result showed that dose dependent increase in percentage of viability at the doses of 18.85, 37.5, 75, 150, $300{\mu}g/ml$. Te results for the $CCl_4$ intoxicated, at $300{\mu}g/ml$ of the concentration of the extract, the % of viable cells was found out to be 99.6%, for Ethanol intoxicated, 97.67%, and Paracetamol induced, 75.37%, IC50 was $21.53{\mu}g/ml$, $12.61{\mu}g/ml$ and $21.42{\mu}g/ml$ respectively. Conclusion: Thus, we conclude that, the extract possesses defensive effect against different toxicants and can be used as an alternate drug for hepatotoxicity.

• Safety and Health at Work
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• 제10권3호
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• pp.355-361
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• 2019

Background: Painters in the automotive sector are routinely exposed to volatile organic solvents, and the levels vary depending on the occupational health and safety controls enforced at the companies. This study investigates the levels of exposure to organic vapors and the existence of controls in the formal economy sector in southern Colombia. Methods: This is an exploratory study of an observational and descriptive character. An analysis of solvents is conducted via the personal sampling of painters and the analysis of samples using the National Institute for Occupational Safety and Health 1501 method. The amount of solvents analyzed varied according to the budget allocated by the companies. The person in charge of the occupational safety and health management system was interviewed to learn about the exposure controls implemented at the companies. Results: A medium exposure risk for toluene was found in one company. Another presented medium risk for carbon tetrachloride, xylene, ethylbenzene, and n-butanol. The others showed low risk of exposure and that the controls implemented were not sufficient or efficient. Conclusion: These results shed light on the working conditions of these tradespeople. The permissible limits established by Colombian regulations for the evaluated chemical contaminants were not exceeded. However, there were contaminants that exceeded the limits of action. The analysis of findings made it possible to propose improvements in occupational safety and health management systems to allow the optimization of working conditions for painters, prevent the occurrence of occupational diseases, and reduce costs to the country's health system.

• Journal of Electrochemical Science and Technology
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• 제13권4호
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• pp.453-461
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• 2022

A chemically sintered and binder-free paste of TiO₂ nanoparticles (NPs) was prepared using a binary-liquid mixture of 1-octanol and CCl₄. The 1:1 (v/v) complex of CCl₄ and 1-octanol easily interacted chemically with the TiO₂ NPs and induced the formation of a highly viscous paste. The as-prepared binary-liquid paste (P_BL)-based TiO₂ film exhibited the complete removal of the binary-liquid and residuals with the subsequent low-temperature sintering (~150℃) and UV-O₃ treatment. This facilitated the fabrication of TiO₂ photoanodes for flexible dye-sensitized solar cells (f-DSSCs). For comparison purposes, pure 1-octanol-based TiO₂ paste (P_O) with moderate viscosity was prepared. The P_BL-based TiO₂ film exhibited strong adhesion and high mechanical stability with the conducting oxide coated glass and plastic substrates compared to the P_O-based film. The corresponding low-temperature sintered P_BL-based f-DSSC showed a power conversion efficiency (PCE) of 3.5%, while it was 2.0% for P_O-based f-DSSC. The P_BL-based low- and high-temperature (500℃) sintered glass-based rigid DSSCs exhibited the PCE of 6.0 and 6.3%, respectively, while this value was 7.1% for a 500℃ sintered rigid DSSC based on a commercial (or conventional) paste.