• Proceedings of the Korean Society of Postharvest Science and Technology of Agricultural Products Conference
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• 2003.04a
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• pp.111.2-112
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• 2003

A total of 20 extracts derived from different plant family commonly used in Indonesian traditional inflammation medicine were screened for their inhibitory effect on soybean lipoxygenase (SBL) and hyaluronidase (HAse) activity. Three methanol extracts, the bark of Cinnamomum burmanni (CB), the leaves of Piper betel (PB), and fruit of Barringtonia acutangula (BA) were found to have high inhibitory effects, whereas the methanol extract of the leaves of Mimusops elengi (ME) have medium inhibitory effect. The IC50 of CB, PB, BA and ME were found to be 21.7, 16.9, 39.1 and 62.8 g/$m\ell$, respectively. Among the tested extracts, only CB inhibited HAse (IC50 = 27g/$m\ell$). CB was successively fractionated with n-hexane, ethyl acetate, butanol and water. The EtOAc fraction having the strongest activity was fractionated and some compounds were isolated and purified by a preparative HPLC(Develosil ODS-HG-5 column). Coumarin and 2-hydroxy cinnamaldehyde. were identified through the analyses of UV-Vis absorption 1H-NMR, 13C-NMR and FAB+-MS spectra.

• Archives of Pharmacal Research
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• v.25 no.3
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• pp.329-335
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• 2002

Previously, several prenylated flavonoids having a C-8 lavandulyl moiety were found to inhibit cyclooxygenase-1 (COX-1) as well as 5-lipoxygenase (5-LOX), and sophoraflavanone G was the most potent inhibitor against these eicosanoid generating enzymes among 19 prenylated flavonoids tested. In this investigation, effects of sophoraflavanone G on COX-2 induction from RAW 264.7 cells and in vivo inflammatory response were studied. Sophoraflavanone G inhibited prostaglandin $E_2{\;}(PGE_2)$ production from lipopolysaccharide (LPS)-treated RAW cells by COX-2 down-regulation at 1-50 uM. Other prenylated flavonoids including kuraridin and sanggenon D also down-regulated COX-2 induction at 10-25 uM, while kurarinone and echinoisoflavanone did not. In addition, sophoraflavanone G showed in vivo anti-inflammatory activity against mouse croton oil-induced ear edema and rat carrageenan paw edema via oral (2-250 mg/kg) or topical administration (10-250 ug/ear). Although the potencies of inhibition were far less than that of a reference drug, prednisolone, this compound showed higher anti-inflammatory activity when applied topically, suggesting a potential use for several eicosanoidrelated skin inflammation such as atopic dermatitis.

• Natural Product Sciences
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• v.16 no.2
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• pp.68-74
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• 2010

Phytochemical investigation on the ethyl acetate and n-butanol fractions of Moutan Cortex resulted in the isolation and characterization of a new monoterpene glycoside (3) and twenty known monoterpene glycosides (1, 2, 4-21). The structure of 3 was determined by spectroscopic data interpretation and physico-chemical properties. Compounds 1 and 8 presented a remarkable inhibitory activity against lipoxygenase-1 (LOX-1) with $IC_{50}$ values of 45.2 and $37.5\;{\mu}M$, respectively. Compounds 9, 10, 13, 18, 19, and 21 showed significant 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging effect with $IC_{50}$ values of 9.8, 25.5, 6.4, 15.2, 18.7, and $23.7\;{\mu}M$, respectively. Benzoylpaeoniflorin (8), which exhibited the highest inhibitory effect with an $IC_{50}$ value of $37.5{\pm}0.7{\mu}M$, was further analyzed the inhibition kinetics by Lineweaver-Burk plots. Results indicated that 8 is a non-competitive inhibitor, and the kinetic parameter values were estimated to be ($31.04\;{\mu}M$, Ki), ($0.29\;{\mu}M/min$, $V_m$), and ($48.50\;{\mu}M$, $K_m$).

• IMMUNE NETWORK
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• v.9 no.3
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• pp.106-113
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• 2009

Background: We previously demonstrated remarkable differences in the expression of IL-8/CXCL8 in aortic tissues and vascular smooth muscle cells (VSMC) from spontaneously hypertensive rats (SHR) compared to VSMC from normotensive Wistar-Kyoto rats (WKY). In the present study, we investigated the direct effect of IL-8/CXCL8 on expression of 12-lipoxygenase (LO), a hypertensive modulator, in SHR VSMC. Methods: Cultured aortic VSMC from SHR and WKY were used. Expression of 12-LO mRNA was determined by real-time polymerase chain reaction. Phosphorlyation of ERK1/2 and production of 12-LO and angiotensin II subtype 1 ($AT_1$) receptor were assessed by Western blots. IL-8/CXCL8-stimulated DNA synthesis was determined by measuring incorporation of [$^3H$]-thymidine. And effect of IL-8/CXCL8 on vascular tone was determined by phenylephrine-induced contraction of thoracic aortic rings. Results: Treatment with IL-8/CXCL8 greatly increased 12-LO mRNA expression and protein production compared to treatment with angiotensin II. IL-8/CXCL8 also increased the expression of the $AT_1$ receptor. The increase in 12-LO induced by IL-8/CXCL8 was inhibited by treatment with an $AT_1$ receptor antagonist. The induction of 12-LO mRNA production and the proliferation of SHR VSMC by IL-8/CXCL8 was mediated by the ERK pathway. The proliferation of SHR VSMC and the vascular contraction in the thoracic aortic ring, both of which were induced by IL-8/CXCL8, were inhibited by baicalein, a 12-LO inhibitor. Conclusion: These results suggest that the potential role of IL-8/CXCL8 in hypertensive processes is likely mediated through the 12-LO pathway.

• Korean journal of applied entomology
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• v.51 no.4
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• pp.349-356
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• 2012

Eicosanoid mediates various cellular immune responses in insects. This study aimed to discover its novel action on the modulation of hemocyte populations in response to an immune challenge. Upon bacterial challenge, the last instar larvae of the beet armyworm, Spodoptera exigua, increased their total hemocyte density in 2 h, and then decreased it to a basal hemocyte density level. This rapid increase in total hemocyte density was explained by an increase of plasmatocyte and spherulocyte densities. When larvae were treated with dexamethasone (a specific phospholipase $A_2$ ($PLA_2$) inhibitor), they did not show any increase in hemocyte density in response to bacterial challenge. However, the addition of arachidonic acid (a catalytic product of $PLA_2$) to larvae treated with dexamethasone recovered the up-regulation of hemocyte density in response to bacterial infection. Among eicosanoid, cyclooxygenase (COX), but not lipoxygenase (LOX), products seemed to mediate the increase of hemocyte density in response to bacterial infection because naproxene (a COX inhibitor) inhibited the hemocyte density increase, though esculetin (a LOX inhibitor) did not. Prostaglandin $E_2$, a COX product, significantly increased the hemocyte density even without bacterial infection. These results suggest that eicosaniod mediates a rapid increase in total hemocyte density in response to immune challenge.

• YAKHAK HOEJI
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• v.33 no.1
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• pp.1-9
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• 1989

We have recently reported that $Mg^{++}-deficiency$ showed endothelium dependent relaxation in isolated canine coronary arteries precontracted with $PGF_{2{\alpha}}$. To differentiate the release of EDRF or $PGI_2$ from the endothelium cells as the cause of vasorelaxation by $Mg^{++}-deficiency$, effects of several inhibitors of arachidonic acid metabolism on the relaxation by $Mg^{++}-deficiency$ were evaluated and also compared with that of acetylcholine. Ibuprofen and tranylcypromine ($10{\mu}M$), an inhibitor of cyclo-oxygenase and $PGI_2$ synthetase, respectively, did not effect on $Mg^{++}-free$ induced vasorelaxation. Pretreatment of quinacrine ($10{\mu}M$), an inhibitor of phospholipase $A_2$ and also $Ca^{++}$ uptake, blocked vasorelaxation by $Mg^{++}-free$. But trifluoperazine ($10{\mu}M$), which is about as potent as quinacrine in the inhibition of $Ca^{++}$ uptake, did not effect on $Mg^{++}-deficiency$ induced vasorelaxation. NDGA ($10{\mu}M$), an inhibitor of lipoxygenase, completely restored $Mg^{++}-free$ induced vasorelaxation, even though pretreatment of that was not blocked which might be due to the characteristics of vasorelaxation of NDGA itself. Pretreatment of methylene blue ($10{\mu}M$), which is known as a inhibitor of EDRF through the blocking effect of guanylate cyclase, completely blocked vasorelaxation by $Mg^{++}-free$ as well as acetylcholine ($0.1{\mu}M$). Acetylcholine-induced dose response curve was also antagonized by pretreatment of quinacrine ($10{\mu}M$), but not by ibuprofen, tranylcypromine and NDGA. These results appear to suggest that $Mg^{++}-free$ induced vasorelaxation was mediated by the release of EDRF through the activation of phospholipase $A_2$ and noncyclo-oxygenase on arachidonate metabolism.

• KOREAN JOURNAL OF CROP SCIENCE
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• v.49 no.spc1
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• pp.169-175
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• 2004

동의보감에 수재되어 있는 약쑥은 식용뿐만이 아니고 한방에서는 출혈 및 지혈약으로 자궁출혈, 임신중의 출혈, 코피지혈 등에 효과가 크다고 알려져 왔다. 또한 부인병과 건위, 설사치료와 항암활성, HeLa cell에 대한 억제작용도 보고되어 있다. MeOH엑스가 HCl-EtOH유발법, $1\%$ 암모니아 수용액 유발법, HCl-aspirin 유발법등에 의하여 유발된 위 손상에 대하여 강한 억제 작용을 나타내고 있는데 이는 flavonoid의 일종인 eupatilin으로 확인된 바 있다. 이 물질이 5-lipoxygenase inhibitor ($ID_{50}=14{\times}16^{-6}M$) 작용과 prosta glandin synthase의 활성을 약간 억제한다고 보고되었다. 약쑥의 eupatilin과 jaceosidin을 분리하여 그 화학구조를 구명하였다. 이를 지표물질로 하여 HPLC 분석조건과 HPLC용 검체의 조제, 표준검량선을 작성하였다. 강화사자발쑥 100 g의 잎에는 eupatilin은 240 mg, jaceosidin은 10 mg함유되어 있고 싸주아리쑥에는 eupatilin은 330 mg, jaceosidin은 123 mg 함유되어 있음이 확인되었다.

• KOREAN JOURNAL OF CROP SCIENCE
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• v.68 no.3
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• pp.114-120
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• 2023

Soybean is the one of the most important crops for providing quality vegetable protein to umans and livestock. Soybean cultivars with a brown seed coat have a wide range of antioxidant benefits because of the flavonoid components. However, they also contain lectin, 7S α′ subunit, lipoxygenase, and Kunitz trypsin inhibitor (KTI) proteins that can be allergenic and digestive inhibitors and reduce processing aptitude. Genetic removal of these four proteins is necessary in soybean breeding. Therefore, this study was conducted to select a new line with brown seed coat, green cotyledon, and tetra-null genotype (lecgy1lox1lox2lox3ti) for lectin, 7S α′ subunit, lipoxygenase, and KTI proteins in the mature seed. Five germplasms were used to create breeding population. From a total of 58 F₂ plants, F₂ plants with lele genotype were selected using a DNA marker, and F₃ seeds with a brown seed coat, green cotyledon, and the absence of 7S α′ subunit protein were selected. Three lines (S1, S2, and S3) were developed. Genetic absence of lectin, 7S α′ subunit, lipoxygenase, and KTI proteins was confirmed in F₆ seeds of the three lines, which had a brown seed coat, green cotyledons, and a white hilum. The 100 seed weights of the three lines were 26.4-30.9 g, which were lower than 36 g of the check cultivar - 'Chungja#3'. The new S2 line with 30.9 g hundred seed weight can be used as a parent to improve colored soybean cultivars without antinutritional factors such as lectin, 7S α′ subunit, lipoxygenase, and KTI proteins.

• The Korean Journal of Physiology and Pharmacology
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• v.19 no.3
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• pp.263-268
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• 2015

5-Lipoxygenase (5-LO) plays a pivotal role in the progression of atherosclerosis. Therefore, this study investigated the molecular mechanisms involved in 5-LO expression on monocytes induced by LPS. Stimulation of THP-1 monocytes with LPS ($0{\sim}3{\mu}g/ml$) increased 5-LO promoter activity and 5-LO protein expression in a concentration-dependent manner. LPS-induced 5-LO expression was blocked by pharmacological inhibition of the Akt pathway, but not by inhibitors of MAPK pathways including the ERK, JNK, and p38 MAPK pathways. In line with these results, LPS increased the phosphorylation of Akt, suggesting a role for the Akt pathway in LPS-induced 5-LO expression. In a promoter activity assay conducted to identify transcription factors, both Sp1 and NF-${\kappa}B$ were found to play central roles in 5-LO expression in LPS-treated monocytes. The LPS-enhanced activities of Sp1 and NF-${\kappa}B$ were attenuated by an Akt inhibitor. Moreover, the LPS-enhanced phosphorylation of Akt was significantly attenuated in cells pretreated with an anti-TLR4 antibody. Taken together, 5-LO expression in LPS-stimulated monocytes is regulated at the transcriptional level via TLR4/Akt-mediated activations of Sp1 and NF-${\kappa}B$ pathways in monocytes.

• Korean Journal of Food Science and Technology
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• v.15 no.2
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• pp.101-107
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• 1983

The four varieties of Korean soybeans were allowed to undergo natural fermentation for seven days at ambient temperature. The average pH of the product was 3.93 and titratable acidity was 1.94%. For all varieties of soybeans the content of riboflavin increased from 98 to $309.4{\mu}g/100g$ dry-matter, relative nutritive value from 78.66 to 94.59% and available lysine from 6.56 to 7.38 mg/gN, respectively. During fermentation, the activities of protease and lipase increased, while lipoxygenase and trypsin inhibitor activity decreased markedly. The capacity of water sorption of fermented soybean flour was increased with progress of proteolysis during fermentation. The cookie and noodle prepared with 20:80 mixture of fermented soybean flour and wheat flour were in the 'like' category, but it was desirable to neutralize the sour taste produced by fermentation. Among five kinds of products prepared from the fermented soybean flour pan cake was liked most by rural consumers.