• Korean Journal of Plant Resources
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• v.19 no.6
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• pp.660-664
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• 2006

The aerial part of Siegesbeckia pubescens (Compositae) has been used to treat rheumatoid arthritis and hypertension in the Oriental medicine. This crude drug has been used without process (SP-0) or with three times-process of steaming and drying (SP-3) or the nine times of that process (SP-9). To search for the antinociceptive anti-inflammatory components from this crude drug, activity-directed fractionation was performed on this crude drug. Since the $CHCl_3$ extract was shown to have a more potent effect than other extracts, it was subjected to silica gel & ODS column chromatography to yield two diterpene compounds (1). Compound 1 was structurally identified as ent-16 (H, 17-hydroxykauran-19-oic acid, which were tentatively named siegeskaurolic acid A. A main diterpene, siegeskaurolic acid A was tested for the antiiflammatory antinociceptive effects using both hot plate- and writhing anti-nociceptive assays and carrageenan-induced anti-inflammatory assays in mice and rats. Pretreatment with siegeskaurolic acid A (20 and 30mg/kg) significantly reduced the stretching episodes, action time of mice and carrageenan-induced edema. These results support that siegeskaurolic acid is a main diterpene responsible for antinociceptive and antiiflammatory action of S. pubescens. In addition, the assays on SP-0, SP-3 and SP-9 produced the experimental results that SP-9 had more significant effects than other two crude drugs. These results suggest that the processing on the original plant may lead to the higher pharmacological effect.

• Korean Journal of Pharmacognosy
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• v.17 no.2
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• pp.178-183
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• 1986

It was our working hypothesis that introduction of 11-keto groups to 12-oleanene/ursene series of triterpenoids should endow them with corticoid-like activities, since pharmacological actions of glycyrrhetinic acid (GA) are known to be caused by inhibition on $corticoid-{\delta}^4-reductase$. 11-Keto-triterpenoids derived artificially in these studies, such as 11, 19-diketo-18, 19-secoursolic acid methyl ester(I), $11-keto-{\beta}-boswellic$ acid derivatives (IIa-IIc), 11-Keto-presenegenin dimethyl ester (III), II-keto-oleanolic acid derivatives (IVa-IVd) and 11-keto-hederagenin (V) possess the fundamental functions of ${\alpha},\;{\beta}-unsaturated$ ketone on C-11 and hydroxyl group on C-3, as like GA (VI). Additionally, they involve the carboxyl groups on rings A (II, III), D (I, III, IV, V) and E (VI), and the hydroxyl groups on rings A (III, V) and C (III). All the compounds competitively inhibited $corticoid-5{\beta}-reductase$, and the highest inhibitory potency appeared in I. All of them except $3,\;11-diketo-{\beta}-boswellic$ acid methyl ester (IIc) were more effective about five times to twice than GA. On carrageenin-induced edema test, compounds I and IVa-IVd showed anti-inflammatory activities, but III enhanced rather edema. Structure-activity relations were found in the aspects of hydrophilicity of ring A and hydrophobicity of rings C/D. The more they were hydrophilic in ring A and hydrophobic in rings C/D, the more they inhibited the enzyme. And the more they were hydrophobic in rings C/D, the more they exhibited antiiflammatory activities. However, the increased hydrophilicity in ring A resulted in increasing edema, probably due to a nonspecific inhibition on $aldosterone-5{\beta}-reductase$.

• Korean Journal of Pharmacognosy
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• v.28 no.4
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• pp.185-191
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• 1997

Cyperus rotundus L. (Cyperaceae) has been used as an analgesic and antiiflammatory agent and in the treatment of menstrual disorder in folk remedies. Cyperi Rhizomata, processed and unprocessed, were extracted with methanol and fractionated with petroleum ether, chloroform. Butanol, water. The effect of unprocessed Cyperi Rhizoma and processed Cyperi Rhizoma on $CCl_4$ induced lipid peroxidation and hepatotoxity have been tested in rats. BuOH. Water fractions of unprocessed Cyperi Rhizome enhanced the inhibition of antilipid peroxidative effects in liver lipid. In chemical parameters obtained from serum analysis. Butanol fraction of unprocessed Cyperi Rhizoma showed significant decrease in hepatotoxicity. In result, unprocessed Cyperi rhizoma has significant antilipid peroxidative effect and hepatoprotective activity.

• Journal of Food Hygiene and Safety
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• v.8 no.3
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• pp.157-161
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• 1993

In order to get infonnations on the development of alcohol induced cardiovascular disorders, primary cultured vascular smooth muscle cells (PVSMC) were treated with acetaldehyde, one of the most reactive metabolites of ethanol. Acetaldehyde caused the striking release of lactate dehydrogenase (LDH) from PVSMC and it stimulated the prostaglandin synthesis in the same system. But it didn't induce cyclooxygenase activity. lipoxygenase inhibitors-propyl gallate and nordihydroguaiaretic acid could reverse the effect of acetaldehyde, but dexamethasone, a phospholipase $A_2\;(PIA_2)$ inhibitor and cyclooxygenase inhibitors except indomethacin could not protect the cells from acetaldehyde toxicity. These results indicate that enhanced prostaglandin synthesis by acetaldehyde is not a direct cause of cell death, but secondary effect due to the activation of PIAl and also, the roles of the lipoxygenase metabolites and/or $PIA_2$ activity itself might be more important in the cytotoxicity of acetaldehyde.