• 생약학회지
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• 제34권1호통권132호
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• pp.25-27
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• 2003

In order to clarify the anti-thrombosis activity of rhubarb, we investigated the effect of stilbene derivatives from rhizomes of Rheum undulatun on cyclooxygenase activity. Stilbene derivatives (desoxyrhapontigenin, rhapontigenin, piceatannol) exhibited the inhibitory effects on COX-1, and desoxyrhapontigenin showed inhibitory effect on COX-2. These inhibitory effect may partially contributed to anti-thrombosis activity of rhubarb.

• Archives of Pharmacal Research
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• 제22권1호
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• pp.18-24
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• 1999

Various flavonoid derivatives were previously reported to possess the inhibitory activity on cyclooxygenase/lipoxygenase. And these properties of flavonoids might contribute to their anti-inflammatory activity in vivo. In this study, several polyhydroxylated/methoxylated flavonoid derivatives such as oroxylin A. wogonin, skullcapflavone II, tectorigenin and iristectorigenin A were isolated from the medicinal plants. these compounds were evaluated fro their inhibitory effects on cyclooxygenase/lipoxygenase from the homogenate of human platelets in vitro. It was found that isoflavones including daidzein and tectorigenin possessed the inhibitory activity on cycloooxygenase, although the potency of inhibition was far less than that of indomethacin. In addition, oroxylin A, baicalein and wogonin inhibited 12-lipoxygenase activity without affecting cyclooxygenase, which suggested that 5,6,7- or 5,7,8-trisubstitutions of A-ring of flavone gave favorable results. The IC50 values of oroxylin A and NDGA against 12-lipoxygenase were found to be 100 and 1.5 uM, respectively.

• 약학회지
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• 제44권3호
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• pp.272-278
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• 2000

The antiinflammatory mechanism of NSAIDs is attributed to the reduction of prostaglandin synthesis by the direct inhibition of cyclooxygenase. Inhibition of prostaglandin production in organs such as stomach and kidney can result in gastric lesions, nephrotoxicity and increased bleeding. In this study, newly designed COX-2 inhibitors, synthesized 1,2-benzothiazine derivatives, were screened in vitro for selectivity of COX-1 and COX-2 inhibition properties. Lead compounds in the structure-activity relationship were studied to synthesize new highly selective COX-2 inhibitors.13 determine inhibitory effect of COX-2, synthesized 1,2-benzothiazine derivatives were screened with accumulation of prostaglandin by lipopolysaccharide (LPS) in aspirin-treated macrophages and murine macropharge cell. Some of synthesized 1,2-benzothiazine derivatives were shown to be effective as selective COX-2 inhibitory activity. Others exhibited a preferential inhibition of COX-2, although some COX-1 inhibitory activity was still present. As a conclusion, simple monomer derivatives were more active than dimer derivatives. Substitution of halogen (Br, C1) on the benzothiazine nucleus slightly enhanced inhibition activity.

• Natural Product Sciences
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• 제2권1호
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• pp.56-74
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• 1996

Prostaglandin $H_2$ synthase is the pharmacological target site of nonsteroidal antiinflammatory drugs. Inhibitory effects on cyclooxygenase activity of the synthase by extracts prepared from herbal medicines and wild plants in Korea have been estimated. Sixteen species out of 612 species exhibited more than 50% of inhibition on the enzyme activity. The active extracts prepared from Carex humilis, Celastrus orbiculatus, Eugenia caryophyllata, Gleditsia japonica var. koraiensis, Glycyrrhiza grabra, Glycyrrhiza uralensis, Gyrophora exculenta, Lespedeza maximowiczii, Morus alba, Persicaria conspicua, Prunus salicina, pterocarya stenoptera, Rheum undulatum, Vitis amurensis, and Vitis coignetiae have been sequentially washed with methylene chloride, ethyl acetate, n-butanol. Among the solvent fractions of the active herbal extracts, ethyl acetate fraction of Carex humilis exhibited the highest inhibitory effect on the cyclooxygenase activity of prostaglandin $H_2$ synthase.

• Archives of Pharmacal Research
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• 제21권4호
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• pp.406-410
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• 1998

Biflavonoid is one of unique classes of naturally-occurring bioflavonoids. Certain biflavonoids including amentoflavone were previously reported to have inhibitory effect on the group 11 phospholipase $A_2$ activity. Amentoflavone was also found to inhibit cyclooxygenase from guinea-pig epidermis without affecting lipoxygenase. In this study, anti-inflammatory and analgesic activities of amentoflavone were evaluated. When amentoflavone was administered intraperitoneally, it showed a potent anti-inflammatory activity as determined by amelioration of croton-oil induced mouse ear edema. It also showed a potent anti-inflammatory activity in the rat carrageenan paw edema model ($ED_{50}$=42 mg/kg) compared to the activity of prednisolone (35 mg/kg) and indomethacin (10 mg/kg). However, amentoflavone did not show a significant inhibitory activity against rat adjuvant-induced arthritis, a chronic inflammatory model. In addition, amentoflavone was found to possess a potent analgesic activity in the acetic acid writhing test ($ED_{50}$=9.6 mg/kg) compared to the activity of indomethacin (3.8 mg/kg). These results suggest that amentoflavone may be a potential lead for a new type of anti-inflammatory agents having dual inhibitory activity of group 11 phospholipase $A_2$ and cyclooxygenase.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.216.1-216.1
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• 2003

P. ginseng C.A. Meyer is one of the most widely used herbal medicine in Asia. It has been used for the treatment of many disorders. Its major constituent is known to be ginsenosides, and there are many documents about bioactivities of ginsenosides such as anti-oxidant, anti-tumorigenic, anti-fatigue, and anti-inflammatory activities. Some of these activities are supposed to have some correlation with inhibitory action of cyclooxygenase (COX). Ginsenosides from P. ginseng and sapogenins were evaluated for their inhibitory effects against both cyclooxygenase-1 and -2 (COX-1 and -2). Inhibitory activity was evaluated by measuring prostaglandin E$_2$ (PGE$_2$) production from arachidonic acid with an ELISA reader. (omitted)

• 한국약용작물학회지
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• 제13권2호
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• pp.75-79
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• 2005

Five coumarins, psoralen (1), scopoletin (2), isoimperatorin (4), (+)-marmesin (5) and xanthotoxin (6), three chromones, cimifugin (3), hamaudol (7) and sec-O-glucosylhamaudol (10), one sterol, daucosterol (8) and one aliphatic alcohol, galactitol (9) were isolated from the root of Peucedanum japonicum. Their chemical structures were identified by the physicochemical and spectroscopic data by comparing literature values. Among them, compounds 9 and 10 were isolated for the first time from this plant. The anti-inflammatory effects of isolated compounds were examined on cyclooxygenase (COX), compounds 1, 2 and 7 showed inhibitory activity on COX-1 with $IC_{50}$ values of 0.88, 0.27 and 0.30 mM, respectively. In the test for COX-2 activity, only compound 7 showed significant inhibitory activity with the $IC_{50}$ value of 0.57 mM. The other compounds exhibited weak inhibitory or no inhibitory activity.

• Natural Product Sciences
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• 제18권1호
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• pp.22-25
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• 2012

Five triterpenoids, epifriedelanol (1), friedelin (2), lupeol (3), ${\beta}$-sitosterol (4), daucosterol (5), and one phenyl propanoids ester, trans-docosanoyl ferulate (6) were isolated from the whole parts of Portulaca oleracea. They were determined using a combination of spectroscopic analyses ($^1H-$, $^{13}C$-NMR, and MS data) and evaluated for their cyclooxygenase inhibitory activity. Compound 6 exhibited inhibitory effect with $IC_{50}$ values of $40.2{\mu}M$ and 1.6 mM on COX-1 and COX-2 activities, respectively.

• 동의생리병리학회지
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• 제19권5호
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• pp.1419-1426
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• 2005

This study was carried out to investigate the effects of herbal extracts on the skin inflammatory reactions which use the makeup preparations. In experiment 1, among the herbal ingredients of herbal extracts, ethanol extracts and 1,3-BG(Butylene Glycol) extracts of Galla Rhois showed potent radical scavenging activity, more than 91% at all concentrations, tested by DPPH (1,1-diphenyl-2-picryl-hyrazyl) method. In experiment 2, ethanol extracts of Chrysanthemi Flos, Gardenias Flos, Galla Rhois showed potent inhibitory activity of the lipopolysaccharide-induced nitric oxide(NO) production, more than 87% at $10{\mu}g/m{\ell}$, by the macrophage RAW 246.7 cells. And 1,3-BG extracts of Taraxaci Herbs, Corm Fructus, Galla Rhois showed potent inhibitory activity of nitric oxide production, more than 89% at $10{\mu}g/m{\ell}$. In experiment 3, ethanol extracts of Chrysanthemi Flos, Gardeniae Flos, Galla Rhois showed potent inhibitory effects of cyclooxygenase-II activity, more than 78% at $10{\mu}g/m{\ell}$, by using ELISA kit. And 1,3-BG extracts of Galla Rhois, Carthami Flos, Chrysanthemi Flos, Taraxaci Herba, Corm Fructus showed potent inhibitory effects of cyclooxygenase-II(COX-II) activity, more than 80% at $10{\mu}g/m{\ell}$. Therefore, 1 expect that herbal extracts, especially Galla Rhois may be used as a drug for treatment on skin inflammation and a material of the makeup preparations.

• Archives of Pharmacal Research
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• 제26권10호
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• pp.832-839
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• 2003

Activated macrophages express inducible isoforms of nitric oxide synthase (iNOS) and cyclooxygenase (COX-2), and produce excessive amounts of nitric oxide (NO) and prostaglandin E$_2$ (PGE$_2$), which play key roles in the processes of inflammation and carcinogenesis. The root of Paeonia lactiflora Pall., and the root cortex of Paeonia suffruticosa Andr., are important Chinese crude drugs used in many traditional prescriptions. 1,2,3,4,6-penta-O-galloyl-$\beta$-D-glucose (PGG) is a major bioactive constituent of both crude drugs. PGG has been shown to possess potent anti-oxidant, anti-mutagenic, anti-proliferative and anti-invasive effects. In this study, we examined the inhibitory effects of 1,2,3,4,6-penta-O-galloyl-$\beta$-D-glucose (PGG) isolated from the root of Paeonia lactiflora Pall. on the COX-2 and iNOS activity in LPS-activated Raw 264.7 cells, COX-1 in HEL cells. To investigate the structure-activity relationships of gallate and gallic acid for the inhibition of iNOS and COX-2 activity, we also examined (-)-epigallocatechin gallate (EGCG), gallic acid, and gallacetophenone. The results of the present study indicated that PGG, EGCG, and gallacetophenone treatment except gallic acid significantly inhibited LPS-induced NO production in LPS-activated macrophages. All of the four compounds significantly inhibited COX-2 activity in LPS-activated macrophages. Among the four compounds examined, PGG revealed the most potent in both iNOS ($IC_{50}$ = 18 $\mu\textrm{g}/mL$) and COX-2 inhibitory activity (PGE$_2$: $IC_{50}$ = 8 $\mu\textrm{g}/mL$ and PGD$_2$: $IC_{50}$ = 12 $\mu\textrm{g}/mL$), respectively. Although further studies are needed to elucidate the molecular mechanisms and structure-activity relationship by which PGG exerts its inhibitory actions, our results suggest that PGG might be a candidate for developing anti-inflammatory and cancer chemopreventive agents.