• Natural Product Sciences
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• v.25 no.1
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• pp.64-71
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• 2019

The present study was conducted to investigate anti-nociceptive and anti-inflammatory effects of the leaves of Ilex latifolia Thunb (I. latifolia) in in vivo and in vitro. Writhing responses induced by acetic acid and formalin- and thermal stimuli (tail flick and hot plate tests)-induced pain responses for nociception were evaluated in mice. I. latifolia (50 - 200 mg/kg, p.o.) and ibuprofen (100 mg/kg, p.o.), a positive non-steroidal anti-inflammatory drug (NSAID), inhibited the acetic acid-induced writhing response and the second phase response (peripheral inflammatory response) in the formalin test, but did not protect against thermal nociception and the first phase response (central response) in the formalin test. These results show that I. latifolia has a significant anti-nociceptive effect that appears to be peripheral, but not central. Additionally, I. latifolia (50 and $100{\mu}g/mL$) and 3,5-di-caffeoyl quinic acid methyl ester ($5{\mu}M$) isolated from I. latifolia as an active compound significantly inhibited LPS-induced NO production and mRNA expression of the pro-inflammatory mediators, iNOS and COX-2, and the pro-inflammatory cytokines, IL-6 and $IL-1{\beta}$, in RAW 264.7 macrophages. These results suggest that I. latifolia can produce antinociceptive effects peripherally, but not centrally, via anti-inflammatory activity and supports a possible use of I. latifolia to treat pain and inflammation.

• Archives of Pharmacal Research
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• v.24 no.1
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• pp.51-54
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• 2001

Three varieties of methyl citrate and 1 -methyl malate were isolated from the fruits of Opuntia ficus-indica var. saboten Makino through in vitro bioassay-guided isolation for the inhibition on monoamine oxidase(MAO). The $IC_50$ values for MAO-B of 1-monomethyl citrate, 1,3-dimethy citrate, trimethyl citrate and 1-methyl malate were 0.19, 0.23, 0.61 and 0.25 mM, respectively. However, on MAO-A, their inhibitions showed only marginal activity.

• KSBB Journal
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• v.13 no.6
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• pp.706-717
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• 1998

Enzymatic synthesis of fructose-based sugar fatty acid esters, such as methyl fructoside oleic acid mono and diester, was investigated using methyl fructoside as a sugar starting material. For the production of methyl fructoside fatty acid monoester by solvent process, 2-methyl 2-propanol was found to be a god reaction medium resulting a higher yield and productivity due to its high sugar solubility. The yield and productivity of methyl fructoside oleic acid monoester were 70% and 12.6g/L-hr, respectively, when molar ratio of methyl fructoside, initial concentration of methyl fructoside, enzyme(Novozym 435) content, and reaction temperature were 3:1, 200g/L, 1%(w/v), and $60^{\circ}C$, respectively. Methyl fructoside oleic acid diester was prepared by lipase-catalyzed diacylation of methyl fructoside and oleic acid in the solvent-free process. Maximum yield of 98% and productivity of 140g/L-hr were achieved when molar ratio(methyl fructoside and oleic acid) of 1:2 enzyme content of 10%(w/v) and reaction temperature of $70^{\circ}C$ were applied for the operating conditions under a reduced pressure of 20∼200 mmHg.

• Natural Product Sciences
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• v.5 no.2
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• pp.80-84
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• 1999

Peroxynitrite is a cytotoxic intermediate produced by the reaction between the superoxide anion radical and nitric oxide. Flavonoids (afzelin, quercitrin and quercetin 3-O-sambubioside), and chlorogenic acid and its methyl ester obtained from leaves of loquat (Eriobotrya japonica) have recently been shown to scavenge 1,1-diphenyl-2-picrylhydrazyl radical and to inhibit lipid peroxidation in mouse liver homogenate. The aim of this study is to investigate the inhibitory effects of the above components on peroxynitrite produced stimulated by 3-morpholinosydnonimine (SIN-1) to produce superoxide anion radical and nitric oxide at the same time. In addition, the present study tests whether or not the components directly scavenge peroxynitrite itself. The results showed that the components with the aromatic ortho-dihydroxyl groups (catechol) were more potent inhibitors of peroxynitrite formation by SIN-1. In particular, the methyl ester form of chlorogenic acid showed the most potent inhibition. At $5\;{\mu}M$ concentration, the order of minimizing peroxynitrite formation were : methyl chlorogenic acid > quercitrin > quercetin 3-O-sambubioside > chlorogenic acid > afzelin. Authentic peroxynitrite was directly scavenged by the components in a manner similar to peroxynitrite formation by SIN-1. In particular, when compared with penicillamine as a positive control, methyl chlorogenate was as effective in inhibiting peroxynitrite formation and approximately 2 times more effective in scavenging an authentic peroxynitrite. These results demonstrate therefore, that components extracted from the leaves of Eriobotrya japonica effectively scavenged peroxynitrite.

• The Korean Journal of Pharmacology
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• v.32 no.3
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• pp.389-397
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• 1996

Gatric mucosa is exposed to toxic, reactive oxygen species generated within the lumen. Nitric oxide protected acetaminophen-induced hepatotoxicity by maintaining glutathione homeostasis. The present study examined the role of nitric oxide in mediating hydrogen peroxide - induced damage to gastric cells. Hydrogen peroxide was generated by glucose oxidase acting on ${\beta}-D-glucose$. L-arginine, $N^G-nitro-L-arginine$ methyl ester, or $N^G-nitro-L-arginine$ were treated to the cells with glucose/glucose oxidase. Lipid peroxidation and nitrite release and cellular content of glutathione were determined. As a result, dose - dependent increase in lipid peroxide production as well as dose - dependent decrease in nitrite release and cellular glutathione content were observed in glucose/glucose oxidase - treated cells. Pretreatment of L-arginine, a substrate for nitric oxide synthase, prevented the increase of lipid peroxide production and the reduction of nitrite release as well as glutathione content. Inhibitors of nitric oxide synthase such as $N^G-nitro-L-arginine$ methyl ester and $N^G-nitro-L-arginine$ did not protect hydrogen peroxide - induced cell damage. In conclusion, nitric oxide protects gestric cells from hydrogen peroxide possibly by inhibiting lipid peroxidation and by preserving cellular glutathione stores.

• YAKHAK HOEJI
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• v.48 no.6
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• pp.328-334
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• 2004

Cervical cancer is one of the leading causes of female death. Viral oncoproteins E6 and E7 are selectively retained and expressed in carcinoma cells infected with HPV (Human pa pilloma virus) type 16 and cooperated in immotalization and transformation of primary keratinocyte. E6 and E7 oncoproteins interfere the functions of tumor suppressor proteins p53 and retinoblasoma protein (pRb), respectively. Among a lots of natural products, Mentha arvensis Linne var.piperascens have inhibitory effects on bindings between E6 oncoprotein and tumor suppressor p53, E3 ubiqutin- protein ligase (E6AP). HPV oncoprotein inhibitors from Mentha piperita L. were isolated by solvent partition and column chromatography (Silica gel, RP-18) and inhibitory compounds were finally purified by HPLC using an ELISA screening system based on binding between E6 and E6AP. The aim of this study is to identify the structure of inhibitory compounds and to investigate whether these compounds have inhibitory effects on functions of E6 oncoprotein. We investigated whether caffeic acid methyl ester (CAM) extracted from Mentha piperita L. could inhibit the function of E6 oncoprotein. CAM inhibited the in vitro binding of E6 and E6AP which are essential for the binding and degradation of the tumor suppressor p53 and also inhibited the proliferation of human cervical cancer cell lines (SiHa and CaSKi) in a dose response manner. These results suggest that CAM inhibited the function of E6 oncoprotein, suggesting that it can be used as a potential drug for the treatment of cervical cancers infected with HPV.

• Analytical Science and Technology
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• v.13 no.4
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• pp.466-473
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• 2000

The complex formation constants (${\beta}_{MLn}$) of potassium and various sodium-selective neutral carriers in solvent polymeric membranes have been determined using solvent polymeric membrane-based optodes and ion-selective electrodes (ISEs). Two different types of PVC-based membranes containing the H^+selective chromoionophore (ETH 5294) with and without a sodium ionophore (4-tert-bntylcalix[4]arenetetraacetic acid tetraethyl ester, ETH 2120, bis[(12-crown-4)methyl] dodecylmethylmalonate or monensin methyl ester) were prepared and their optical responses to either the changes in alkali metal cation (e.g., sodium and potassium) concentrations at a fixed pH (0.05 M Tris-HCl, pH 7.2) or varying pH at a fixed alkali metal cation concentration (0.1 M) were measured. The same type of membranes were also mounted in conventional electrode body and their potentiometric responses to varying pH at a fixed alkali metal cation concentration (0.1 M) were measured. The complex formation constants of the ligand could be calculated from the calibration plots of the relative absorbance vs. the activity ratios of cation and proton ($a_{M^+}/a_{H^+}$) and of the emf vs. pH. It was confirmed that the ratio values of the complex formation constants for the primary and interfering ions are closely related to the experimental selectivity coefficients of ISEs.

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.723-728
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• 1998

The chemical behaviours of 4-methyl-2-oxo-2H-benzopyran-7-yl oxoacetyl hydrazine (2) towards some different reagents such as anhydride compounds, aromatic aldehydes, carb on disulphide, and nitrous acid yielded the corresponding pathalazine derivatives (3, 4, 5), hydrazone derivative (6), 1,3,4-oxadiazole derivative (7, 8, 9) and acid azide (10) respectively. Treatmen of 10 with absolute alcohols, amines and ethyl amino acid ester gave the corresponding carbamate derivative (11), substituted urea derivative (12) and ethyl substituted alkyl acetate (13) respectively. The biological activity of some synthesized compounds was evaluated.

• Archives of Pharmacal Research
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• v.27 no.2
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• pp.173-176
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• 2004

Three phenolic compounds, rosmarinic acid (1), methyl rosmarinate (2), ethyl rosmarinate (3), and two flavonoids, luteolin (4), luteolin-7-O-$\beta$-D-glucuronide methyl ester (5) were isolated from the aerial part of Lycopus lucidus (Labiatae). Their structures were determined by chemical and spectral analysis. Compounds 1-5 exhibited potent antioxidative activity on the NBT superoxide scavenging assay. The $IC_{50}$ values for compounds 1-5 were 2.59, 1.42, 0.78, 2.83, and 3.05 $\mu\textrm{g}$/mL respectively. In addition, five compounds were isolated from this plant for the first time.

• YAKHAK HOEJI
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• v.28 no.1
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• pp.25-27
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• 1984

Some $\betha$-lactam antibiotics-penicillins and cephalosporins-were determined by gas chromatography (GC) with flame photometric detector (FPD) which was selective and sensitive to sulfur-containing compounds. Methyl ester derivatives of carboxyl group in $\betha$-lactam antibiotics were prepared using 0.5Mmethyl iodide in methylene chloride and were taken for gas chromatography with 0.9% or 0.6% QF-1 on Chromosorb WAW-DMCS. We have found that it is possible to determine methyl esters of $\betha$-lactam antibiotics by GC/FPD.