• Journal of Life Science
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• v.25 no.12
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• pp.1370-1376
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• 2015

The 1, 1- diphenyl 2-picrylhyorazyl (DPPH) is a well-known radical and a trap (scavenger) for other radicals. Hyaluronidase (HAase) is an enzyme that depolymerizes the polysaccharide hyaluronic acid (HA) in the extracellular matrix of connective tissue. Lipoxygenase (LOX) enzyme was reported to convert the arachidonic, linoleic and other polyunsaturated fatty acid into biologically active metabolites involved in the inflammatory and immune responses. The purpose of the present study is to evaluate plant extracts as sources of natural antioxidants and to examine whether Achyranthes japonica having significant DPPH, HAase and LOX inhibitory activity. The inhibitory effect of HAase by A. japonica was assayed using a Morgan microplate assay. The antioxidant activity of the A. japonica extracts was measured on the basis of the scavenging activity of the stable 1, 1- diphenyl 2-picrylhyorazyl (DPPH) free radical. DPPH scavenging activity of matured roots of A. japonica was evaluated at 4.0 mg/ml was 87.8% and that of young roots was 86.2% at same concentration. The roots of A. japonica showed maximum inhibition of HAase activity (IC₅₀ = 27.7 μg/ml). The highest LOX inhibition was recorded in the root extract among three vegetative parts. Inhibition of HAase activity of roots may contribute towards the development of herbal medicines. Although percent inhibition of lipoxygenase by Achyranthes japonica for all young and matured groups for leaves, stems, and roots at different concentrations, there were not show a statistically significant difference (p<0.05).

• Journal of the Korean Chemical Society
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• v.37 no.1
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• pp.68-75
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• 1993

Various biological activities (enzyme inhibitory potency, lipoxygenase inhibition, tadpole narcosis, vapor toxicity and heat of vaporization) of molecules are correlated with molecular descriptors. The molecular descriptors used in this works are molecular connectivity index, Wiener distance index and ad hoc descriptor, which can encode information about branching, size, cyclization, unsaturation, hetero atom content and polarizability. It is found that calculated values from multiple regression equations are in a good agreement with experimental data on five biological activities of alcohol, ester and ketone compounds.

• Korean Journal of Food Science and Technology
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• v.34 no.2
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• pp.157-163
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• 2002

An investigation was carried out to study the characteristics of lipoxygenase in dioctyl sulfosuccinate (aerosol-OT, AOT)/isooctane revered micelles of microaqueous system containing infinitesimal water. ${\alpha}-Linoleic$ acid as a substrate could be analyzed by the colorimetric methodology using 5%(w/v) cupric acetate-pyridine solution and the activity of lipoxygenase was able to be assayed by the degree of ${\alpha}-linoleic$ acid consumption per minute. Optimal pH, temperature, and R-value ([water]/[AOT]) were determined as the value of 5.0, $25^{\circ}C$, and 10.0, respectively. Kinetic analysis of the enzyme reaction under the optimal conditions showed that the values of $K_m$ and $V_{max}$ were 0.31 mM of ${\alpha}-linoleic$ acid and $384.16{\mu}mol$ of ${\alpha}-linoleic$ acid decomposed/min, respectively. The results indicate the reaction to be lipoxygenase-catalyzed oxidation of ${\alpha}-linoleic$ acid in AOT/isooctane reversed micellar system. The inhibitory effect of natural antioxidants on lipoxygenase showed little inhibitory effect of L-ascrobic acid while ${\alpha}-tocopherol$ showed 72% of inhibitory effect.

• Preventive Nutrition and Food Science
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• v.3 no.3
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• pp.216-220
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• 1998

Lipoxygenase inhibitory acitivity of the methanolic extract of 60 different kinds of plant seeds was determined by a spectrophotometric method using a soybean lipoxigenase(SLO) and linolenic acid. Among the extracts examined, the methanolic extract of nutmeg(Myristical fragrans)seed showed the most potent SLO inhibitory activity. To isolate SLO inhibitor, hence, the defatted methanol extract was further partitioned with ether, ehtylacetate , and n-butanol , stepwise. The ether souble fraction was successively chromatographed on silica gel, Sephadex LH-20 and preparative TLC. Three phenolic compounds were isolated , and one of them showing a strong SLO inhibition activity was identified as a 2,6-dihydroxy-9-(3', 4', -dihydroxyphenyl)nonylphenone (IC50a=0.39$\mu\textrm{g}$/ml) by 1H-& 13C0NMR, IR, and MS spectroscopy.

• Journal of Korean Neurosurgical Society
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• v.29 no.1
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• pp.28-34
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• 2000

Object : To verify the effect of the lipoxygenase inhibitor and cycloxygenase inhibitor on meningioma cell proliferation. Method : Using two meningioma cell lines, cell proliferation was determined at 96 hrs after adding inhibitor (AA861, Nordihydroguaiaretic acid(NDGA), Indomethacin, acetyl-11-keto-beta-boswellic acid(AKBA) into medium by methyl tetrazolium salt/phenazine methosulfate(MTS/PMS) non-radioactive cell proliferation assay. We checked optical density with 490nm wavelength UV and this value was used as a proliferative index. The percent of inhibition was also calculated from this value. Conclusion : Indomethacin and NDGA showed no effect on meningioma proliferation. AA861 also showed no significant inhibitory effect, but AKBA demonstrated a significant inhibitory effect on meningioma cell proliferation.

• Journal of Life Science
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• v.26 no.9
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• pp.1022-1026
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• 2016

In this study the hot water extract was prepared from Hydrocotyle sibthorpioides (Araliaceae) leaves and stems to study antioxidant activities and lipoxygenase inhibition. The extract showed the protective hydroxyl radical (-OH) which can damage virtually all types of macromolecules: carbohydrates, nucleic acids (mutations), lipids (lipid peroxidation), and amino acids. Hydroxyl radical scavenging activity of H. sibthorpioides was 78.6%. The extract showed strong activity against 1, 1- diphenyl 2-picrylhyorazyl (DPPH) which is a well-known radical and a trap (scavenger) for other radicals. DPPH scavenging activity of leaves of H. sibthorpioides was evaluated at 8.0 mg/ml was 86.0%. Lipoxygenases (LOXs) constitute a heterogeneous family of lipid peroxidizing enzymes capable of oxygenating polyunsaturated fatty acids to their corresponding hydroperoxy derivatives. The inhibitory effect of 15-LOX by H. sibthorpioides was assayed using a Morgan microplate assay. The extract of H. sibthorpioides was 55.5% inhibitory effects on the inhibition of LOX at 8.0 mg/ml. The IC₅₀ values for OH activity, DPPH activity, and LOX inhibition from leaves 5.23 mg/ml, 6.44 mg/ml, and 3.71 mg/ml, respectively. Antioxidative activity assay showed that the water extracts from leaf and stem had a strong reducing power. These results show that H. sibthorpioides has some phytochemical constituents which may be active against the free radicals (OH and DPPH) and lipoxygenase enzyme.

• Biomolecules & Therapeutics
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• v.5 no.1
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• pp.87-93
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• 1997

DA-5018, a new capsaicin derivative, showed potent analgesic effect comparable to that of morphine in various experimental acute pain models. in this study, whether the analgesic mechanism of DA-5018 is related to opiate receptors or prostanoids was investigated. The affinity of DA-5018 for opiate receptor was determined by receptor binding assay. The Ki values of DA-5018 for nonspecific and specific $\mu$, $textsc{k}$, $\delta$-opiate receptor was 299$\pm$8.88, 735$\pm$215, 2930$\pm$ 163, 1550$\pm$813 nM, respectively and DA-5018 exhibited lower affinity than morphine. DA-5018 (10-"~3$\times$10-′M) inhibited electrically-evoked contractions of the guinea ply ileum and rat vas deferens, and these inhibition was not antagonized by naloxone(10 nM), an opiate receptor antagonist. Antagonism of analgesic effect of 7A-5018 by naloxone was examined by tail pinch test. Analgesic action of DA-5018(0.1 ~2 mg/kg, 5.c.) was not antagonized by naloxone(1 mg/rg, i.p.). These results indicate that pharmacological action of DA-5018 is not related with opiate receptor. Cyclooxygenase and 5-lipoxygenase activities in rat peritoneal neutrophil treated with A23187 and arachidonic acid were measured by radioimmunoassay. DA-5018 stimulated the cyclooxygenase activity and the concentration show-ing the two fold increase of activity was 124$\mu$M. DA-5018 slightly inhibited 5-lipoxygenase activity and these results together indicate that analgesic action of 3A-5018 is not mediated through inhibition of cyclooxy genase or lipoxygenase. These results suggest that the analgesic effect of DA-5018 is not due to blocking opiate receptor or to inhibiting the synthesis of prostanoids in the arachidonic acid metabolism pathway.

• 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.

• Proceedings of the Korean Society of Life Science Conference
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• 2007.10a
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• pp.76.2-76.2
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• 2007

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• Journal of the Korean Society of Food Science and Nutrition
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• v.35 no.1
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• pp.21-27
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• 2006

Effects of root, stem and leaf extracts of Zanthoxylum piperitum on the inhibition of lipid peroxidation in the hepatic microsome of rat, DPPH radical scavenging activity, soybean lipoxygenase activity and activated partial thromboplastin times (APTT) were examined in vitro. The highest inhibition of hepatic microsomal lipid peroxidation was observed by ethyl acetate fraction of the root and stem extracts. The high inhibition of lipid peroxidation was observed in the leaf, the root and the stem in order. The DPPH radical scavenging activity of ethyl acetate fraction was higher than that of n-butanol fraction and it was similar to the root and the steam extract. It was similar to the inhibition of hepatic microsomal lipid peroxidation. The DPPH radical scavenging activity was the highest in 0.50 mg/mL of ethyl acetate fraction, and it was 4.4-fold higher than that of a-tocopherol, as an antioxidant standard. The DPPH radical scavenging activity was dependent on the extract concentration in the range of $0.12\~5.00$ mg/mL. The soybean lipoxygenase activity of ethyl acetate fraction was higher than that of n-butanol fraction and it was similar to the root and the stem extracts. The soybean lipoxygenase activity was the highest in 0.50 mg/mL of ethyl acetate fraction. The soybean lipoxygenase activity was dependent on the extract concentration in the range of $0.12\~5.00$ mg/mL. The leaf extract showed the highest antithrombogenic effect followed by the stem and then the root extract. The activated partial thromboplastin times were dependent on the extract concentration in the range of $0.10\~2.00$ mg/mL.