• Korean Journal of Pharmacognosy
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• v.41 no.3
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• pp.185-189
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• 2010

In this study, we analyzed and quantified the amounts of bioactive phenolic constituents, xanthotoxin (1), oxypeucedanin (2), and imperatorin (3) in each part of the root of Angelica dahurica by HPLC, which validated by ICH guide lines comparing the linearity, intra day precision, inter-day precision. As a result, the amount of imperatorin 2.96% in the rootlet was two fold higher than that of the main root 1.32%. On the other hand, the amounts of xanthotoxin and oxypeucedanin in the rootlet showed similar to those of main root. In addition, the cortex of root is more plentiful of three consitituents (0.66%, 0.53%, and 1.85%) than those of xylem (0.29%, 0.05%, and 0.07%). These results show that the rootlet and cortex contain a large amount of bioactive phenolic constituent including xanthotoxin, oxypeucedanin, and imperatorin than other parts of the root.

• The Korean Journal of Pesticide Science
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• v.5 no.3
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• pp.26-35
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• 2001

In order to search potent antifungal substances from domestic plants, 40 plants cultivated in Korea were collected. After extracting with methanol (MeOH) and concentrating to dryness, the MeOH extracts were screened for in vivo antifungal activity against six plant diseases at a concentration of $2000{\mu}g/mL$. Fourteen extracts showed disease-controlling activity more than 90% against at least one of the 6 plant diseases tested; eight, seven, and three extracts controlled more than 90% the development of rice blast, tomato late blight, and wheat leaf rust, respectively. However, none of the extracts exhibited in vivo antifungal activity more than 90% against rice sheath blight, tomato gray mold, and barley powdery mildew. From the MeOH extracts of Angelica gigas and A. dahurica showing potent controlling activity against rice blast, 1 and 2 antifungal substances, respectively, were isolated by solvent partitioning and column chromatography. The three compounds were identified to be coumarins, namely, decursin, imperatorin, and isoimperatorin, by mass spectrometry and NMR spectroscopy. They were examined for in vitro and in vivo antifungal activities together with umbelliferone (7-bydroxycournarin) and scopoletin (6-methoxy-7-hydroxycoumarin) containing a free hydroxyl group at position 7 to investigate the structure-activity relationship. In vitro, most of 50% growth inhibitory concentrations ($IC_{50}$) were over $200{\mu}g/mL$, indicating that they have relatively weak antifungal activity. The antifungal activity of decursin and scopoletin, containing cyclic alkoxy groups instead of free hydroxyl group at position 7, was stronger than umbelliferone and scopoletin. Especially, decursin and imperatorin showed potent antifungal activities against Pythium ultimum and Magnaporthe grisea, respectively, with $IC_{50}$ values less than $25{\mu}g/mL$. In vivo, decursin and imperatorin showed potent antifungal activity against rice blast, whereas other coumarins hardly controlled the development of 6 plant diseases tested. These results suggest that the antifungal activity of 7-hydroxycoumarin derivative is substantially increased when the hydroxyl group at position 7 is protected by a stable cyclic alkoxy grouping.

• 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.

• Herbal Formula Science
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• v.10 no.1
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• pp.143-155
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• 2002

In the hope of identifying anti-leukemic agents from traditional herbal medicines. this study was designed to investigate the anti-leukemic effects of the herbal medicine Jipaesan, which is composed of Angelica Dahurica and Fritillariae Verticillata. in acute promyeloid leukemia HL-60 cells. Jipaesan showed anti-proliferative effect through the induction of differentiation and apoptosis in HL -60 cells. Verticinone as a major differentiating agent and imperatorin as major apoptosis-inducing agent were isolated from the water extracts of F. Verticillata and A. Dahurica, respectively. Combined treatment of HL-60 cells with two major compounds showed synergy in the induction of differentiation. Since the induction of differentiation and/or apoptosis has therapeutic values in curing acute leukemic diseases. Jipaesan could be useful as an anti-leukemic agent.

• 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.

• YAKHAK HOEJI
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• v.12 no.3_4
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• pp.59-64
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• 1968

Silica gel column chromatography of the ether extract of the root of Angelica Koreana $M_{AXIMOWICZ}$ (Umbelliferae) gave five kinds of crystalline products of coumarin. The following kinds of furocoumarins were identified by UV, IR, NMR spectra and physico-chemical tests. iso-imperatorin m.p. 108-$109^{\circ}$ $C_{16}H_{14}O_{4}$ oxypeucedanin m.p. 142-$143^{\circ}$ $C_{16}H_{14}O_{5}$ prangolarine m.p. 104-$105^{\circ}$ $C_{16}H_{14}O_{5}$ imperatorin m.p. 100-$101^{\circ}$ $C_{16}H_{14}O_{4}$ These analyses also showed that white needles m.p. 129-$130^{\circ}$ were likely to be a furocoumarin. Besides, the methanol extract of the root was found to contain sucrose.

• 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.

• Plant Resources
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• v.3 no.2
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• pp.123-130
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• 2000

The medicinal constituents contained in Korean and Chinese Angelicae dahuricae Radix were compared by confirming their qualities. From the extracts of Angelicae dahuricae Radix, oxypeucedanin, imperatorin, and alloisoimperatorin etc. furanocoumarin derivatives were identified by GC/MS analysis. Through GC/FID analysis, the furanocoumarin derivatives content of Baizi cultivated in Korea was more than that cultivated in China, except for one cultivated at Ankuk province, and so confirmed to possess, on the whole, good quality medicinal constituents by content, as compared with the ones cultivated in China.

• The Korean Journal of Physiology and Pharmacology
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• v.26 no.3
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• pp.145-155
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• 2022

Multidrug resistance of tumors has been a severe obstacle to the success of cancer chemotherapy. The study wants to investigate the reversal effects of imperatorin (IMP) on doxorubicin (DOX) resistance in K562/DOX leukemia cells, A2780/Taxol cells and in NOD/SCID mice, to explore the possible molecular mechanisms. K562/DOX and A2780/Taxol cells were treated with various concentrations of DOX and Taol with or without different concentrations of IMP, respectively. K562/DOX xenograft model was used to assess anti-tumor effect of IMP combined with DOX. MTT assay, Rhodamine 123 efflux assay, RT-PCR, and Western blot analysis were determined in vivo and in vitro. Results showed that IMP significantly enhanced the cytotoxicity of DOX and Taxol toward corresponding resistance cells. In vivo results illustrated both the tumor volume and tumor weight were significantly decreased after 2-week treatment with IMP combined with DOX compared to the DOX alone group. Western blotting and RT-PCR analyses indicated that IMP downregulated the expression of P-gp in K562/DOX xenograft tumors in NOD/SCID mice. We also evaluated glycolysis and glutamine metabolism in K562/DOX cells by measuring glucose consumption and lactate production. The results revealed that IMP could significantly reduce the glucose consumption and lactate production of K562/DOX cells. Furthermore, IMP could also remarkably repress the glutamine consumption, α-KG and ATP production of K562/DOX cells. Thus, IMP may sensitize K562/DOX cells to DOX and enhance the antitumor effect of DOX in K562/DOX xenograft tumors in NOD/SCID mice. IMP may be an adjuvant therapy to mitigate the multidrug resistance in leukemia chemotherapy.