• Title/Summary/Keyword: 타크린

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Hepatoprotective Effects of Various Enzyme Hydrolysates from Oysters on Tacrine-Induced Toxicity in Human Hepatoma Cells (타크린으로 유발한 간세포 독성에 대한 효소별 굴 가수분해물의 보호 효과)

  • Park, Hye-Jin;Do, Hyung-Joo;Kim, Ok-Ju;Kim, Andre;Ha, Jong-Myung
    • Journal of Life Science
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    • v.22 no.1
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    • pp.117-125
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    • 2012
  • This study investigated the potential hepatoprotective benefits of Crassostrea gigas oyster hydrolysates. Oysters are known to have many biofunctional properties. In particular, oyster enzymatic hydrolysates produce substances with beneficial functions. The potential hepatoprotective effects of C. gigas hydrolysates against damage induced by tacrine were evaluated in vitro in HepG2 cells. Peptides were generated from C. gigas by enzymatic hydrolysis with Neutrase, Flavourzyme, or Protamex enzyme preparations. Tacrine treatment induced considerable cell damage in HepG2 cells, as shown by significant leakage of glutamic oxaloacetic transaminase (GOT) and lactate dehydrogenase (LDH). Cells treated with C. gigas hydrolysates showed an increased resistance to oxidative challenge compared to control cells, as revealed by higher cell survival against tacrine-induced hepatotoxicity. In addition, treatment with C. gigas hydrolysates reduced the leakage of GOT and LDH. These findings indicate that enzyme hydrolysates derived from C. gigas may be of benefit for developing hepatoprotective foods and drugs.

Hepatoprotective Constituents of Saururus chinensis Roots Against Tacrine-induced Cytotoxicity in Human Liver-derived Hep G2 Cells (삼백초근의 타크린으로 유발한 간 세포독성 보호 성분)

  • Jeong, Gil-Saeng;Li, Bin;Lee, Dong-Sung;Kwon, Ji-Wung;Lee, Hye-Suk;Kwon, Tae-Oh;Kim, Youn-Chul
    • Korean Journal of Pharmacognosy
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    • v.38 no.2 s.149
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    • pp.176-180
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    • 2007
  • Five liglans, sauchinone (1), di-0-methyltetrahydrofuriguaiacin B (2), manassantin A (3), manassantin B (4) and saucerneol B (5), have been isolated from the MeOH extract of Saururus chinesis roots. The evaluation for protective effect of compounds 1-5 against tacrine-induced cytotoxicity in human liver-derived Hep G2 cells was conducted. Compounds 1,2, and 5 showed significant protective effects with the EC$_{50}$ values of74.2${\pm}$0.9, 111.3${\pm}$0.8,64.3${\pm}$0.8 ${\mu}$M, respectively. Silybin, one of the well-known hepatoprotective agents, used as a positive control, and also showed protective effect with an EC$_{50}$ value of 86.2${\pm}$0.5 ${\mu}$M.

Hepatoprotective compounds of Cassiae Semen on tacrine-induced cytotoxicity in Hep G2 cells (결명자의 타크린으로 유발한 간 세포독성 보호 성분)

  • Byun, Erisa;Jeong, Gil-Saeng;An, Ren-Bo;Li, Bin;Lee, Dong-Sung;Ko, Eun-Kyung;Yoon, Kwon-Ha;Kim, Youn-Chul
    • Korean Journal of Pharmacognosy
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    • v.38 no.4
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    • pp.400-402
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    • 2007
  • Tacrine is an acetylcholinesterase inhibitor that is approved for the treatment of Alzheimer's disease. However, tacrine treatment for Alzheimer's disease results in reversible hepatotoxicity in 30-50% of patients, which seriously limits its clinical use. Accordingly, the identification of constituents in natural products that have protective effects on tacrine-induced hepatotoxicity would be valuable. In the present study, an immortalized human hepatoma cell line, HepG2 was employed to screen for agents that protect against tacrine-induced hepatotoxicity. The bioassay-guided fractionation of water extract of Cassiae Semen furnished two anthraquinones, aurantio-obtusin (1) and obtusifolin (2). Compounds 1 and 2 showed hepatoprotective effects with the protection ratio values of 55.3 +/- 0.5% and 41.2 +/- 0.8% at $160{\mu}M$, respectively.

Percutaneous Absorption Characteristics of Tacrine in Alzheimer-type Dementia Treatment (Alzheimer형 치매치료제인 Tacrine의 경피 투과 특성 연구)

  • Lee, Han-Seob
    • Journal of the Korean Applied Science and Technology
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    • v.29 no.4
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    • pp.552-560
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    • 2012
  • Drug delivery technologies are patent protected formulation technologies that modify drug release profile, absorption, distribution, and elimination for the benefit of improving product efficacy and safety, as well as patient convenience and compliance. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stop if the drug dosage lead to side effect. Polysaccharide, such as karaya gum and locust bean gum(LBG)/water-soluble chitosan oligomer(WSCO) were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, tacrine contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in tacrine such as lipophilic drug in vitro. We used glycerin, PEG 400, and PEG 800 as enhancers. Therefore, transdermal absorption of tacrine could be improved by changing vehicle composition or by using penetration enhancers. Especially it would be anticipated that the high permeation efficacy could be obtained by using vehicle that has enhancing effect for itself and by adding enhancers to it.

Hepatoprotective Effects of Plants Extracts from Baekdu Mountain on Tacrine-induced Cytotoxicity in HepG2 Cells (타크린으로 유발한 간 세포 독성에 대한 백두산 식물 추출물의 보호 효과)

  • Lee, Dong-Sung;Jeong, Gil-Saeng;An, Ren-Bo;Li, Bin;Byun, E-Ri-Sa;Yoon, Kwon-Ha;Kim, Youn-Chul
    • Korean Journal of Pharmacognosy
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    • v.39 no.1
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    • pp.68-73
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    • 2008
  • The present study represents the screening of the protective effects of herbal methanolic extracts from Baekdu mountain against tacrine-induced cytotoxicity in HepG2 cells. Tacrine is an acetylcholinesterase inhibitor, and used for the treatment of Alzheimer's disease. However, administration of tacrine for the treatment of Alzheimer's disease results in a reversible hepatotoxicity in 30-50% of patients, consequently limiting clinical use. Therefore, studies for natural products with protective effect on the tacrine-induced hepatotoxicity would be valuable as providing potential therapeutic use. 109 plant sources were collected in Baekdu mountain, and extracted with methanol. These extracts had been screened the protective effects against tacrine-induced cytotoxicity in HepG2 cells at the 100 and 300 ${\mu}g/ml$. Of these, ten methanolic extracts, roots of Ampelosis japonica, aerial parts of Berberis amurensis, aerial parts of Sedum aizoon, aerial parts of Lespedeza tomentosa, aerial parts of Lespedeza juncea, aerial parts of Hypenricum ascyron, stem barks of Syringa reticulata, fruits of Gleditsia japonica, aerial parts of Chamaenerion angustifolium, branches of Ginkgo biloba, showed significant protective effects against tacrine-induced cytotoxicity in HepG2 cells.

Radical Scavenging Activities of Phellinus pini (상황버섯(Phellinus pini)의 라디칼 소거작용)

  • Nam, Byung-Hyouk;Jo, Wol-Soon;Cui, Yong;Choi, Yoo-Jin;Lee, Jae-Dong;Jeong, Min-Ho
    • Journal of Life Science
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    • v.20 no.3
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    • pp.326-335
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    • 2010
  • The concentration of phenolics in Phellinus pini (CY001) extracts, expressed as mg of GAEs per g of P. pini fractions, and the EtOAc fraction (436.5 mg GAEs/g) of P. pini had a higher phenolic content than other fractions. Several biochemical assays were used to screen antioxidant properties such as reducing power, 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity, NBT/XO superoxide system and inhibition of DCF/AAPH peroxyl radicals. Among the six mushroom extracts, the EtOAc fraction from P. pini (CY001) showed the most potent DPPH radical, superoxide radical, and peroxyl radical scavenging activities, with $IC_{50}$ values of $11.49\;{\mu}g/ml$, $8.32\;{\mu}g/ml$, and $1.91\;{\mu}g/ml$, respectively. The EtOAc fraction of P. pini (CY001) significantly inhibited enzymatic lipid peroxidation and effectively attenuated LPS-induced NO production of RAW 264.7 cells without cytotoxicity. We also found that the EtOAc fraction had a significant hepato-protectant effect on tacrine-induced cytotoxicity in HepG2 cells. These findings suggest that P. pini (CY001) may have potential as a natural antioxidant, which contains compound(s) with radical scavenging activity.

Anti-inflammatory Efficacy and Liver Protective Activity of Pine Pollen according to Probe Sonicator Ultrasonic Disintegration Extraction Method (송화분의 초음파 파쇄 추출 방법에 따른 항염증 효능 및 간 보호 활성)

  • Kim, Ok Ju;Woo, Young Min;Jo, Eun Sol;Jo, Min Young;Li, Chun-Ri;Lee, Young-Ho;Ahn, Mee Young;Lee, Sang-Hyeon;Ha, Jong Myung;Kim, Andre
    • Applied Chemistry for Engineering
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    • v.30 no.5
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    • pp.569-579
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    • 2019
  • In this study, the effect anti-oxidant, anti-inflammatory, and liver protective activity was investigated via quick ultrasonic disintegration of pine pollen using a probe sonicator (PS) followed by the extraction with water, 70% ethanol, and 100% ethanol. The anti-inflammatory effect was studied by measuring the production of nitric oxide (NO) and cytokine in RAW264.7 cells induced with lipopolysaccharides (LPS). The cell toxicity was also checked with an 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and the experiment was conducted using non-toxic $100{\mu}g/mL$. The NO inhibition rate was highest in the 70% ethanol PS group at $85.99{\pm}0.12%$. Also an excellent efficiency was obtained from the results of interlukin-1 beta ($IL-1{\beta}$) and tumor necrosis factor alpha ($TNF-{\alpha}$), which is related to inflammation-related cytokine, with the respective inhibition rates of 63 and 22%. To examine liver protective activity, HepG2 cells were treated with Taclin, and the generation of glutamic oxaloacetic transaminase (GOT) and lactate dehydrogenase (LDH) was measured in the culture solution. From GOT and LDH generation results, the inhibition rates in the 70% ethanol PS group were 28% and 13%, respectively, which was higher compared to that of using negative control group. Our results suggest that pine pollen extracted in 70% ethanol using PS may be used to develop food products that have anti-aging, anti-inflammatory, and liver protective effects.