• Title/Summary/Keyword: Lipoxygenase inhibitor

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The Contents of Antinutritional Factors and Lipoxygenase Activity of the Recommended Soybean Varieties in Korea (장려품종 콩의 영양저해 인자 및 리폭시게나아제 특성)

  • Kim, Dong-Man;Baek, Hyung-Hee;Kim, Kil-Hwan
    • Korean Journal of Food Science and Technology
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    • v.22 no.4
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    • pp.393-397
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    • 1990
  • The contents of the several antinutritional factors and lipoxygenase activity of 19 soybean varieties recommended for cultivation in Korea were analyzed. The ranges of raffinose and stachyose contents, which are the flatulence factors, were $0.74{\sim}1.58%\;d.b.\;and\;3.34{\sim}5.30%d.b.$, respectively and the total amount of these sugars was high in the varieties of Hill, Baekun and Jangbaek. The contents of trypsin inhibitor and phytate phosphorus in the soybean varieties ranged from 21.2 to 37.0 TI/g, d.b. and from 337 to 605mg%, d.b. respectively. The lipoxygenase activity of $163.6{\sim}403.5unit$ was shown in the 19 soybean varieties, and Padal, Jangbaek and S-133 were the varieties with the higest activity.

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lntracellular $Ca^{2+}$ Mediates Lipoxygenase-induced Proliferation of U-373 MG Human Astrocytoma Cells

  • Kim, Jung-Ae;Chung, Young-Ja;Lee, Yong-Soo
    • Archives of Pharmacal Research
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    • v.21 no.6
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    • pp.664-670
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    • 1998
  • The role of intracellular $Ca^{2+}$, in the regulation of tumor cell proliferation by products of arachidonic acid (AA) metabolism was investigated using U-373 MG human as trocytoma cells. Treatment with nordihydroguaiaretic acid (NDGA), a lipoxygenase (LOX) inhibitor, or caffeic acid (CA), a specific 5-LOX inhibitor, suppressed proliferation of the tumor cells in a dose-dependent manner. However, indomethacin (indo), a cyclooxygenase (COX) inhibitor, did not significantly alter proliferation of the tumor cells. At anti-proliferative concentrations, NDGA and CA significantly inhibited intracellular $Ca^{2+}$ release induced by carbachol, a known intracelluar $Ca^{2+}$ agonist in the tumor cells. Exogenous administration of leukotriene $B_4(LTB_4)$, an AA metabolite of LOX pathway, enhanced proliferation of the tumor cells in a concentration-dependent fashion. In addition, $LTB_4$, induced intracelluar $Ca^{2+}$ release. Intracellular $Ca^{2+}$-inhibitors, such as an intracellular $Ca^{2+}$ chelator (BAPTA) and intracellular $Ca^{2+}$-release inhibitors (dantrolene and TMB-8), significantly blocked the LTB4-induced enhancement of cell proliferation and intracellular $Ca^{2+}$ release. These results suggest that LOX activity may be critical for cell proliferation of the human astrocytoma cells and that intracelluar $Ca^{2+}$ may play a major role in the mechanism of action of LOX.

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Structure-Activity Relationship. A Theoretical Study of Catechol Derivatives as 5-Lipoxygenase Inhibitor (구조-활성 상관관계. 5-Lipoxygenase의 저해제인 Catechol류에 관한 이론적 연구)

  • Park, Seongsik;Kim, Sang-Yun;Chung, Duk-Young;Yoh, Soo-Dong
    • Journal of the Korean Chemical Society
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    • v.39 no.9
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    • pp.741-748
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    • 1995
  • Various catechol derivatives inhibiting 5-lipoxygenase were studied with theoretical calculations and QSAR study. It was hypothesized that receptor site model could accept the active site of the catechol derivatives. The molecular length, molecular surface area, C5 net charge, HOMO/LUMO energy, van der Waals surface area and volume were used as variables to find the relationships between activity and physicochemical parameters.

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Effect of Inhibitor on Lipoxygenase Inactivation in Soybean Homogenates (대두 현탁액의 Lipoxygenase의 활성저해 인자들의 영향)

  • Im, Hyo-Sig;Cho, Young-Hun;Rhee, Chong-Ouk
    • Korean Journal of Food Science and Technology
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    • v.27 no.1
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    • pp.19-24
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    • 1995
  • The effect of several inhibitors such as ascorbic acid on the lipoxygenase in soybeans known to catalyze reaction resulting in racid off-flavors was examined in the soybean homogenates by the oxygen electrode method. Among 8 compounds added at homogenizing process, 10 mM ascorbic acid inhibited lipoxygenase-1 and lipoxygenase-2/3 activities to 41.7 and 49.8%, respectively. Inactivation of lipoxygenase-2/3 was highly accelerated by homogenization for 15 min at room temperature, so the activity was inhibited 70.8% comparing with the homogenization of 3 min. When soybean homogenates with 10 mM ascorbic acid was stored at $25^{\circ}C$ for 72 hrs, lipoxygenase-2/3 activities lowered to 52.8% whereas L-1 activities lowered to 15.8%. Since it is reported that lipoxygenase-2 is responsible for the off-flavor of soybean products, the inhibitory effect of ascorbic acid among several inhibitors investigated might be useful in soybean processing.

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Physicochemical Characteristics and Antioxidant Activity of Kanjang made from Soybean Cultivars Lacking Lipoxygenase and Kunitz Trypsin Inhibitor Protein (Lipoxygenase와 Kunitz Trypsin Inhibitor 단백질 결핍콩으로 제조한 간장의 이화학적 특성 및 항산화 활성)

  • Hwang, Cho-Rong;Lee, Soo-Jung;Kang, Jae-Ran;Kwon, Min-Hye;Kwon, Hyo-Jin;Chung, Jong-Il;Sung, Nak-Ju
    • Journal of agriculture & life science
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    • v.46 no.5
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    • pp.111-125
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    • 2012
  • In order to evaluate suitability by processing for non-GM soybean cultivars such as Gaechuck#2, Jinyangkong and CJ#1 lacking lipoxygenase (LOX) and kunitz trypsin inhibitor (KTI) protein, physicochemical characteristics and antioxidant activity of Kanjang made from above soybean were compared to Kanjang made from a conventional cultivar (Taekwangkong). Proximate compositions of soybeans were similar for the 4 kinds cultivars. Total phenol and flavonoid contents were significantly higher in cultivars lacking LOX and KTI protein than the Taekwangkong. In Kanjang, contents of total and reducing sugar were higher in Taekwangkong Kanjang than Kanjang from made cultivars lacking LOX and KTI protein. Contents of total and amino type nitrogen were the highest in the Jinyangkong Kanjang. Mineral contents were higher in the Jinyangkong and CJ#1 Kanjangs, amino acid contents were higher in the Kanjang made from 3 cultivars lacking LOX and KTI protein than the Taekwangkong. Taste of the Jinyangkong Kanjang with higher sweety and savory was also found to be superior to that of others in overall acceptability evaluation. Total phenol and flavonoid contents in Kanjang were significantly higher in the Kanjang made from cultivars lacking LOX and KTI protein than the Taekwangkong. Radical scavenging activity of Kanjang was increased in the total phenol contents dependent on. Reducing power by ferric-reducing antioxidant potential (FRAP) was significantly higher the Kanjang made from Gaechuck#2 and CJ#1 than the Taekwangkong. $Fe^{2+}$ chelating activity was higher in Taekwangkong Kanjang than the other cultivars, but its activity was similar to Jinyangkong Kanjang. Therefore, higher nutritional composition, total phenol and flavonoids contents and antioxidant activity in the Kanjang made from soybean cultivars lacking LOX and KTI protein might be provide better benefit for manufacture of another their products.

Lipoxygenase Inhibition and Antioxidative Activity of Flavonoids from Paeonia moutan Seeds

  • Kim, Hyo-Jin;Chung, Shin-Kyo;Park, Sang-won
    • Preventive Nutrition and Food Science
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    • v.3 no.4
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    • pp.315-319
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    • 1998
  • Previously, the methanolic extract of Paeonia moutan seeds was found to potently inhibit soybean lipoxy-genase (SLO). Hence to isolate SLO inhibitor, the defattd methaniolic extract of the seeds was consecutively partitioned wiht ether, ethyl acetate,n-butanol ,adn water. The ether souble fraction showing strong inhibitory activity against SLO was further fractionated into a strongly acidic, a weakly acidic, and a neutral fractions. The strongly acidic components of the ether extract were successively subjected to chromatography on a silica gel, Sephadex LH-20, and preparative HPLC. Four phenolic compounds were isolated , and twio of them showing a strong SLO inhibition activity were identified as luteolin (IC50=2.32$\mu\textrm{g}$/ml) and 5,6,4'-trihydroxy-7,3'- dimethoxylflavone (IC50=0.31$\mu\textrm{g}$/ml) by UV, IR, 1H-& 13C-NMR, and MS spectroscopy. In addition, two flavonoids showed significantly antioxidative activity as strong as that of of $\alpha$-tocopherol (p<0.05) in the autoxidation system of linoleic acid. These results suggest that luteolin and 5,6,4'-trihydroxy-7,3'-dimethoxy-flavone may be used as a potential source of anti-inflammatory agents with antioxidative activity.

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Lipoxygenase Inhibitory Activity of Korean Indigenous Mushroom Extracts and Isolation of an Active Compound from Phellinus baumii

  • Lee, Seung Woong;Song, Ja-Gyeong;Hwang, Byung Soon;Kim, Dae-Won;Lee, Yoon-Ju;Woo, E-Eum;Kim, Ji-Yul;Lee, In-Kyoung;Yun, Bong-Sik
    • Mycobiology
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    • v.42 no.2
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    • pp.185-188
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    • 2014
  • We investigated a total of 335 samples of Korean native mushroom extracts as part of our lipoxygenase (LOX) inhibitor screening program. Among the mushroom-methanolic extracts we investigated, 35 exhibited an inhibitory activity greater than 30% against LOX at a concentration of 100 ${\mu}g/mL$. Especially, Collybia maculata, Tylopilus neofelleus, Strobilomyces confusus, Phellinus gilvus, P. linteus, P. baumii, and Inonotus mikadoi exhibited relatively potent LOX inhibitory activities of 73.3%, 51.6%, 52.4%, 66.7%, 59.5%, 100.0%, and 85.2%, respectively. Bioassay-guided fractionation led to the isolation of inoscavin A from the methanolic extract of P. baumii, which showed the most potent activity and was identified by spectroscopic methods. Specifically, inoscavin A exhibited potent LOX inhibitory activity with an $IC_{50}$ value of $6.8{\mu}M$.

The Activity of 5-Lipoxygenase and the Inhibitor of Leukotriene $B_4$ Biosynthesis (5-Lipoxygenase의 활성과 Leukotriene $B_4$ 생합성 억제물질)

  • Min, Kyung-Rak;Shin, Jong-Man;Chang, Yun-Sook;Kim, Young-Soo
    • YAKHAK HOEJI
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    • v.33 no.6
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    • pp.319-323
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    • 1989
  • Polymorphonuclear leukocyte (PMNL) was obtained from peritoneal cavity in rat treated with casein. Effects of divalent cations and drugs on leukotriene $B_4(LTB_4)$ formation from arachidonic acid in the PMNL were determined by HPLC assay. 5-Lipoxygenase, a key enzyme for $LTB_4$ formation from arachidonic acid, exhibited $V_{max}$ at $1\;{\times}\;10^{-5}M$, and $K_m$ at $9.89\;{\times}\;10^{-5}M$ of arachidonic acid. Optimal $Ca^{++}$ concentration for the enzyme activity was $1\;{\times}\;10^{-5}M$ but $Zn^{++}$ did not show any significant effects on the $LTB_4$ formation. Indomethacin and caffeic acid exhibited inhibitory effects on the $LTB_4$ formation at $1\;{\times}\;10^{-5}M$ and $4\;{\times}\;10^{-5}M$, respectively. However, 6-aminohexanoic acid did not show any significant effects on the $LTB_4$ formation.

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Phenidone, a dual inhibitor of cyclooxygenase and lipoxygenase, inhibits carbon tetrachloride-induced acute liver injury in rats

  • Choi, Hyuop;Joeng, Donghwan;Jung, Bae-Dong;Shin, Taekyun;Wie, Myung-Bok
    • Korean Journal of Veterinary Research
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    • v.50 no.2
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    • pp.145-149
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    • 2010
  • This study was carried out to find whether phenidone (1-phenyl-3-pyrazolidinone), a cyclooxygenase as well as a lipoxygenase inhibitor, exhibits the preventive effect on carbon tetrachloride $(CCl_{4})-induced$ acute liver injury in rats. Rats were pretreated with phenidone at a dose of 50 or 200 mg/kg (p.o.) once daily for 3 consecutive days before $CCl_{4}$ administration. Serum aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were measured. Malondialdehyde (MDA) production was determined as an index of lipid peroxidation in the liver and serum. The histopathological changes in the liver were also examined in each group. The reduction in body weights was significantly inhibited in the phenidone-treated group than in the $CCl_{4}$ control group. Significant increase in the relative liver weights of the phenidone-treated groups was observed compared with either the vehicle or $CCl_{4}$ groups. Elevation of serum AST and ALT activities occurred after $CCl_{4}$ treatment was significantly attenuated by the pretreatment with phenidone. The elevation of MDA levels in liver and serum were completely inhibited in phenidone-treated groups. The protective effects on phenidone-treated groups were confirmed histopathologically. These results suggest that phenidone may be a useful protector through modulation of hepatic inflammation in $(CCl_{4})-induced$ acute liver injury.