• Biomolecules & Therapeutics
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• v.13 no.3
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• pp.185-189
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• 2005

We isolated a coumarin compound, isoimperatorin ($C_{16}H_{14}O_4$ mw: 270) from Angelica koreana through silica gel column chromatography, and characterized it by NMR. Here, for the first time we observed that isoimperatorin (25, 50 and 100 ${\mu}M$) treatment for 24-72h inhibited growth and induced death in human prostate carcinoma DU145 cells. Further, in mechanistic investigation, isoimperatorin-induced cell growth inhibition was associated with a strong increase in G1 arrest in cell cycle progression, which started at 24h of the treatment. These findings suggest a novel anticancer efficacy of isoimperatorin mediated via induction of G1 arrest against hormone refractory human prostate carcinoma DU145 cells.

• YAKHAK HOEJI
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• v.14 no.1_2
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• pp.21-27
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• 1970

Isoimperatorin and Oxypeucedanin isolated from root of Angelica Koreana Max. (Umbelliferae) that is used as "Kang-Whal" a botanical drug, in Korea, Show following general pharmacologic activities. The treatment with Oxypeucedanin on the exercised duodenum of the rabbit increased the motility of it while isoimperatorin shows little effects. But on the exercised heart of the frogs, both components depressed its contractility. Whereas Oxypeucedanin depressed both blood pressure of the carotied artery and respiration of the rabbit, Isoimperatorin tends to increase blood pressure, respiration and the tonus of the muscle of the earth worm. Oxypeucedanin did not affect the tonus of the muscles of the earth worm, but depressed the uterus contraction of the rabbit, which was, on the contrary, increased by Isoimperatorin.

• Korean Journal of Crystallography
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• v.8 no.2
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• pp.138-143
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• 1997

The crystal structure of isoimperatorin, f-[(3-methyl-2-butenyl)oxy]-7H-furo[3,2-g][1] benzopyran-7-one, has been determined from single crystal x-ray diffraction study; C16H14O4, Monoclinic, P21/c, a=8.865(1) Å, b=9.331(1) Å, c=16.156(1) Å, β=98.12(1)', V=1322.9(2) Å3, T=293(2)K, z=4, Cu Kα(λ=1.5418 Å). The structure was solved by direct method and refined by full-matrix least squares to a final R=5.72% for 1922 unique observed Fo>4o(F0) reflections and 182 parameters.

• Biomolecules & Therapeutics
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• v.14 no.4
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• pp.202-206
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• 2006

Angelicae Dahiricae Radix has been used for controlling inflammatory respiratory diseases in oriental medicine and their components, phellopterin, isoimperatorin and byakangelicol were reported to have various biological effects. In this study, we investigated whether phellopterin, isoimperatorin and byakangelicol affect adenosine triphosphate(ATP)-induced mucin secretion from cultured airway epithelial cells. Confluent primary hamster tracheal surface epithelial(HTSE) cells were metabolically radiolabeled using $^3H$-glucosamine for 24 h and chased for 30 min in the presence of varying concentrations of each agent to assess the effects on $^3H$-mucin secretion. The results were as follows: 1) phellopterin significantly inhibited ATP-induced mucin secretion; 2) However, isoimperatorin and byakangelicol did not affect ATP-induced mucin secretion, significantly. This result suggests that phellopterin can regulate 'mucin secretion induced by ATP'-a phenomenon simulating mucus overproduction from inflamed airway epithelial cells-by directly acting on airway mucin-secreting cells. Therefore, phellopterin should further be investigated for the possible use as mucoregulators in the treatment of inflammatory airway diseases.

• YAKHAK HOEJI
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• v.42 no.2
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• pp.125-131
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• 1998

The total ethanol extract of Angelica koreana radix (UmbeUiferae) showed potent inhibitory effect on tumor necrosis factors (TNF-${\alpha}$) production from LPS-stimulated RAW 264.7 cells in screening studies on 118 Korean medicinal plants. The activity-guided fractionation of the total ethanol extract resulted in the isolation of 4 compounds, including active substances. The chemical structures of the compounds isolated were established by chemical and spectrometric analyses as imperatorin, isoimperatorin, osthol and oxypeucedanin. Among them, osthol, oxypeucedariin and isoimperatorin showed significant inhibitory activities on TNF-${\alpha}$ production as 54.3${\pm}$2.1%, 33.6${\pm}$1.0% and 17.7${\pm}$3.0%, respectively, at 12.5${\mu}$g/ml.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.856-859
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• 2002

In the course of finding Korean natural products for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the roots of Angelica dahurica showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of three furanocoumarins, isoimperatorin (1), imperatorin (2) and oxypeucedanin (3), as active principles. These compounds inhibited AChE activity in a dosedependent manner, and the $IC_{50}$ values of compounds 1-3 were 74.6, 63.7 and 89.1 uM, respectively.

• Journal of Pharmaceutical Investigation
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• v.9 no.4
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• pp.8-12
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• 1979

A study on the effects of the root components of Angelica koreana Max. on voluntary activity in mice has confirmed that: 1. MeOH soluble Ex., MeOH insoluble Ex., oxypucedanine and isoimperatorin were antagonized against the voluntary activity in mice pretreated with a dose of C.N.B. 30mg/kg. 2. MeOH insoluble Ex. showed higher depressant effect than MeOH soluble Ex.. 3. the depressant activity of oxypucedanine was significantly more effective than that of isoimperatorin.

• Korean Journal of Pharmacognosy
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• v.21 no.1
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• pp.74-82
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• 1990

The effects of naturally occurring furanocoumarins on cytochrome P-450 have been investigated in rat liver microsomes. Incubation of microsomes with an NADPH-generating system and four furanocoumarins such as imperatorin, isoimperatorin, phellopterin and byakangelicin at $37^{\circ}$ in vitro resulted in a significant destruction of cytochrome P-450. A single treatment(50 mg/kg, i.p.) of rats with each furanocoumarin caused a rapid loss of cytochrome P-450 accompanied by the loss of heme from the microsomes but not by the loss of cytochrome $b_5$. It is suggested that cytochrome P-450 is specifically destroyed by furanocoumarins in a metabolic process involving destruction of its heme group and as a consequence, hepatic enzyme activities are depressed markedly.

• Korean Journal of Pharmacognosy
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• v.22 no.3
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• pp.156-161
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• 1991

Four furocoumarins and two dihydrofuranocoumarin glycosides have been isolated from the benzene-soluble and butanol-soluble portions of the roots of Ostericum koreanum Kitagawa, respectively. Four furocoumarins have been determined as imperatorin, isoimperatorin, oxypeucedanin and oxypeucedanin hydrate, and two dihydrofuranocoumarin glycosides determined as marmesinin and $4'-O-{\beta}-D-glucopyranosyl-3'-hydroxymarmesin$ on the basis of spectral data and physico-chemical evidence.

• Archives of Pharmacal Research
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• v.23 no.5
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• pp.467-470
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• 2000

Five furanocoumarins including a new one were isolated from the root of Angelica dahurica by repeated silica gel column chromatography. Their chemical structures were determined to be isoimperatorin (1), oxypeucedanin hydrate-3"-butyl ether (2), imperatorin (3), knidilin (4), and oxypeucedanin hydrate (5). This represents the first study in which the compound 2 has been isolated and identified, The long-range coupling ($^{5}J$) in the $^1H$-NMR spectrum observed in the linear furanocoumarin skeleton was also investigated in detail.