• Nutritional Sciences
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• v.5 no.4
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• pp.184-189
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• 2002

The effects of dietary Int levels on lipid metabolism under fixed P/S (1.3) and n-6/n-3 (5.1) fatty acid ratios were examined in rats using palm oil, soybean oil and perilla oil. These ratios correspond to the recommended composition of dietary fat for humans. The range of dietary fat levels was 5-20% by weight (11.8-39.3% of total energy). The levels of dietary fat did not influence the concentrations of serum and liver cholesterol, whereas the level of triglycerides was gradually elevated with increasing levels of dietary fat, especially in the liver. The fatty acid composition of tissue phosphatidylcholine seemed to vary with the different levels of fat. The ratio of linoleic acid to arachidonic acid was increased more significantly in the heart than in the liver. In adipose tissue total lipids, the percentages of saturated and monounsaturated fatty acids decreased, whereas the percentage of polyunsaturated fatty acid increased, with increasing dietary Int levels. In addition, though the level of aortic prostacyclin was not uniformly affected by increasing dietary fat levels, thromboxane A2 production by platelets tended to increase with higher levels of dietary fat, suggesting an increased risk of thrombosis in this situation. Thus, even though dietary fat may have desirable compositions of fatty acids, these excessive consumption can produce unfavorable metabolic responses.

• Journal of Nutrition and Health
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• v.24 no.2
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• pp.97-103
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• 1991

The increase in alcohol consumption level has been noticed in Korea recently. Alcohol appreciably inhibits cell mediated immunity and this may contribute to the high prevalence of serious infection such as pulmonary tuberculosis among alcoholic subjects. The present study was undertaken to examine the effect of ethanol on the cyclooxygenase metabolites of human monocyte in vitro. Monocytes were activated with 800 units of gamma interferon(IFN-${\gamma}$) for 3 days following apply of Ficool-hypaque density gradient and gelatin coated flasks for separation of monocytes. Ethanol with addition of 100mM, 300mM and 600 mM for 30 minutes to 106 monocytes with/without previous IFN-${\gamma}$ treatment caused a dose dependent decrease in the production of thromboxane B2, 6-keto-PGE1$\alpha$ and PGE2 by radioimmunoassay at 6 hours after ethanol treatment. Quite different from the findings after 6 hours there was dose dependent increase in three prostaglandins without IFN-${\gamma}$ treatment after 24 hours of incubation. With previous treatment of IFN-${\gamma}$ reduced productions of three prostaglandins at 24 hours than control is spite of ethanol stimjulation. These findings show that IFN-${\gamma}$ can inhibit alcohol induced derangement of arachidonic acid metabolism of monocytes.

• 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.

• Journal of Physiology & Pathology in Korean Medicine
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• v.27 no.2
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• pp.212-224
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• 2013

This study intends to clarify how Sayeok-tang(here in after reffered to SYT) affect C57BL/10 mice whose osteoarthritis was induced by papain. Osteoarthritis was induced by injecting papain in the knee joint of 3 groups(n=6) of mice. Normal group was non-treatment group and was not injected papain, whereas control mice were orally administered with $200{\mu}{\ell}$ of physiological saline. Positive comparison group was medicated with 100 mg/kg of Joins$^{(R)}$ mixed with $200{\mu}{\ell}$ of physiological saline. Experimental group was medicated with 400 mg/kg of SYT mixed with $200{\mu}{\ell}$ of physiological saline. Both Positive and experimental comparison groups were orally medicated once per day for 4 weeks. After the experiment, the functions of liver and kidney, inflammation cytokine values within serum, degree of revelation for inflammation cytokine genes, immune cells within blood, metabolism of arachidonic acid and amount of cartilage were measured and histopathological changes in the knee joint structures were observed. As results, SYT had no significant effect on the liver and kidney functions. Interleukin-$1{\beta}$(IL-$1{\beta}$), interleukin-6(IL-6), monocyte chemo attractant protein-1(MCP-1) and tumor necrosis factor-${\alpha}$(TNF-${\alpha}$) were significantly decreased. Inflammation cytokines in joints were all significantly decreased. Prostaglandin $E_2(PGE_2)$, thromboxane $B_2(TXB_2)$ were significantly decreased. Destruction of cartilage on micro computed tomography(CT)-arthrography was meaningfully decreased. In terms of histopathology, infiltration of inflammation, proliferation of synovial membrane, subsidence of cartilage and bone due to penetration of excessive formation of synovial cell and destruction of cartilage were small. Based on all results mentioned above, Sayeok-tang(SYT) is believed to be meaningful for suppressing the progress of osteoarthritis and its treatments because of its anti-inflammatory effects and alleviation of pain with histopathological effective efficacy.

• Mass Spectrometry Letters
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• v.11 no.4
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• pp.113-117
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• 2020

Cytochrome P450 2J2 (CYP2J2) is a member of the cytochrome P450 superfamily, and is known to be arachidonic acid epoxygenase that mediates the formation of four bioactive regioisomers of epoxyeicosatrienoic acids (EETs). CYP2J2 is also involved in the metabolism of drugs such as albendazole, astemizole, danazol, ebastine, and terfenadine. CYP2J2 is highly expressed in the heart and cancer tissues. In this study, the inhibitory potential of ten natural products against CYP2J2 activity was evaluated using human liver microsomes and tandem mass spectrometry. Among them, bilobetin, which is a kind of biflavonoid, exhibits a strong inhibitory effect against the CYP2J2-mediated astemizole O-demethylation (IC50 = 0.73 μM) and terfenadine hydroxylation (IC50 = 0.89 μM). This result suggests that bilobetin can be used as strong CYP2J2 inhibitor in drug metabolism study.

• 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.

• Journal of Nutrition and Health
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• v.30 no.4
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• pp.415-424
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• 1997

Serum lipid levels and fatty acid composition of serum phospholipids(PL) were investigated in 24 healthy male subjects who consumed either corn oil(CO) rich In linoleic acid(LA), perilla oil(PO) rich in $\alpha$-linolenic acid($\alpha$-LNA), or canola oil acid(OA) as a major fat source fir 5 weeks. The PO and the CNO groups showed significant(P <0.05) increases in serum high density lipoprotein-cholesterol(HDL-C) levels and in ratios of HDL- C/total cholesterol(TC) compared with initial values measured at the beginning of the study. Significantly(p <0.05) increased concentrations of serum triglycerides(TG) ware observed after 5 weeks of the CO based diet compared with both its intial value and the concentration observed after 5 weeks with the PO-based diet. fatty acid composition of serum PL reflected changes in dietary fatty acid composition and metabolism. Compared with the initial levels, significandy increased contents of eicosapentaenoic acid(EPA) and docosahexaenoic acid(DHA) were observed in serum PL of the PO group and significantly increased contents of $\alpha$-LNA and EPA were observed in the CNO group. Arachidonic acid(AA) content of serum PL did not change in the CO group during the study period, although, the increase in LA was significant(P <0.05). Compared with the CO-based diet, both the PO and the CNO-based diets seem to have beneficial effects on atherosclerosis by influencing the serum lipid profile and fatty acid composition of serum PL.

• Advances in Traditional Medicine
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• v.9 no.1
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• pp.74-82
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• 2009

Pharmacological investigations were carried out with aqueous methanolic extract (AME) of Swietenia mahagoni (L.) Jacq. (Meliaceae) leaves. Acute toxicity studies revealed that the $LD_{50}$ dose of AME was 600 mg/kg, i.p. AME was found to possess significant anti-inflammatory activity in acute, sub-chronic and chronic models of inflammation. AME selectively inhibited cyclooxygenase (COX)-2 activity, which is involved in arachidonic acid metabolism and biosynthesis of prostaglandins under inflammatory conditions. Treatment with AME significantly enhanced total peritoneal cell count and the number of macrophages in normal mice, which revealed that AME may also alter the immune response along with its anti-inflammatory effect. The saponins or the alkaloids present in AME may be responsible for the anti-inflammatory activity.

• Proceedings of the PSK Conference
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• 2003.10a
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• pp.66-69
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• 2003

Mast cell playa crucial role in allergic and inflammatory disease through the exocytosis of preformed granule-associated mediators, such as histamine, serotonin, proteases and the generation of newly synthesized lipid mediators such as, leucotrien (LT) $C_4$ and prostaglandin (PG) $D_2$ in response to crosslinking of high affinity for IgE (Fc$\gamma$RI). New eicosanoids are synthesized by the oxidative metabolism of arachidonic acid, which is generally esterified sn-2 position of the major classes of glycerophospholipids. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.105.2-105.2
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• 2003

Recently, several reports suggest that ceramide formation has been implicated in the apoptosis signaling in response to chemotherapeutic agents. In this study, to enhance paclitaxel-mediated cytotoxicity and endogenous ceramide levels, we blocked ceramide metabolism using an inhibitor of glucosylceramide synthase, l-phenyl-2- dacanoylamino-3-morpholino-l-propanol(PDMP) and SM synthase, D609. Exposure of human breast cancer cells to paclitaxel accumulated de novo ceramide synthesis by enhancement of SPT activity 1.2-fold, whereas ceramide synthase activity was not altered. (omitted)