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AIM: To investigate the effect of oxypeucedanin (OPD) on doxorubicin resistance in human breast cancer MCF-7/DOX cells and its possible mechanism. METHODS: MCF-7/DOX cells were cultured in vitro, MTT assay was used to detect the effect of OPD on the survival of MCF-7/DOX cells, and the effect of OPD combined with different concentrations of doxorubicin on the proliferation of MCF-7/DOX cells were investigated. The effect of OPD combined with doxorubicin on the expression of genes including MDR1, MRP1, AGPAT2, CHKA, CEPT1, DGKA, PCYT1A, PLA2G15 in MCF-7/DOX cells was measured by qRT-PCR. The effect of OPD combined with doxorubicin on the protein expression of MDR1, MRP1, CHKA and CCTα in MCF-7/DOX cells was determined by Western blot. RESULTS: The IC
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Objective: To analyze the quality of Angelicae Dahuricae Radix (ADR) from national drug evaluation sampling, continuously improve and revise the standard determination method, and ensure the safety of public drug use, six index components of ADR medicinal material and decoction pieces were determined by combining HPLC fingerprint chromatography and quantitative analysis of multi-components by single marker (QAMS). Methods: The determination and exploratory study were carried out according to the National Standard. The establishment of steamed Angelicae dahurica HPLC fingerprint, method for multiple assessment of six index components to conduct a methodological survey determination of multi-index component content of 20 batches of Angelicae dahurica tablets, the final determination of the quality of Angelicae dahurica. Result:s A total of 239 batches of ADR were received from 189 enterprises, in which 225 batches were qualified and 14 batches were unqualified. The qualified rate was 94%. A method that determined content of six kinds of coumarin in ADR decoction pieces using imperatorin as control was established, which could solve the problem of difficulty in obtaining control and consuming long determination time. It would better indicate the drug quality. Conclusio:n The method we had established could be used in qualitative and quantitative analysis of oxypeucedanin hydrate, byakangelicin, oxypeucedanin, berapten, imperatorin and isoimperatorin in ADR decoction pieces. Through this random inspection, it is found that there were still some quality problems in ADR decoction pieces. The quality supervision of traditional Chinese medicine should be strengthened further.
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Objective:To establish an HPLC gradient elution method for the determination of isoalantolactone,alantolactone,xan-thotoxol,oxypeucedanin,imperatorin and osthole in Kangfu ointment simultaneously. Methods:Isoalantolactone,alantolactone,xan-thotoxol,oxypeucedanin,imperatorin and osthole were determined by HPLC with a chromatographic column of Agilent TC-C18(250 mm ×4.6 mm,5 μm),the mobile phase was methanol-0.1% formic acid solution with gradient elution at a flow rate of 0.9 ml·min-1. The detection wavelengths were 220 nm and 300 nm. The column temperature was 35℃. Results: The linear range of isoalantolac-tone,alantolactone,xanthotoxol,oxypeucedanin,imperatorin and osthole was 6.16-123.20 μg·ml-1,3.78-75.60 μg·ml-1,1.87-37.40 μg·ml-1,4.06-81.20 μg·ml-1,9.27-185.40 μg·ml-1and 13.89-277.80 μg·ml-1,respectively. The correlation coef-ficient was 0.999 4,0.999 8,0.999 6,0.999 5,0.999 9 and 0.999 7, respectively. The average recovery was 98.04% (RSD=1.06%),97.10%(RSD = 1.53%), 96.73% (RSD = 0.90%), 98.92% (RSD = 1.36%), 99.12% (RSD = 0.83%) and 100.27%(RSD=0.58%),respectively. Conclusion:The method is simple and accurate,which can be used to improve the quality standard for Kangfu ointment.
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The study was aimed to establish a liquid chromatography-tandem mass spectrometric method for the determination of the docetaxel concentration in rat plasma, and study the effect of coumarin constituents (imperatorin, isoimperatorin and oxypeucedanin) in Angelica dahurica on pharmacokinetics of docetaxel.Plasma was precipitated with acetonitrile and determined by LC-MS method with Paclitaxel as an internal standard. The specificity, linearity, range, accuracy, precision and stability of the method were suitable for the determination of docetaxel in plasma.Six sprague-dawley rats in each group received intragastric administration of docetaxel (50 mg•kg⁻¹), oxypeucedanin (8 mg•kg⁻¹) combined with docetaxel (50 mg•kg⁻¹), imperatorin (15 mg•kg⁻¹) combined with docetaxel (50 mg•kg⁻¹), and isoimperatorin(15 mg•kg⁻¹) combined with docetaxel (50 mg•kg⁻¹).Their drug plasma concentration was determined by LC-MS with Paclitaxel as an internal standard to draw plasma concentration-time curve, and the phamacokinetic parameters were calculated by DAS 2.0. The results showed that the phamacokinetic parameters of docetaxel all had notable changes when combined with imperatorin, isoimperatorin, and oxypeucedanin, respectively. The phamacokinetic parameters AUC and Cmax were significantly increased, indicating that coumarin constituents in Angelica dahurica could promote the oral bioavailability of docetaxel, and their effects were in the following order: oxypeucedanin> isoimperatorin> imperatorin.
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Objective: To study the chemical constituents of ethyl acetate soluble parts in 70% ethanol aqueous extract from the roots of Angelica dahurica var. formosana. Methods: The compounds were separated and purified by repeated column chromatography on silica gel and HPLC, and their structures were determined by spectroscopic data analyses of MS and NMR. Results: Forty-two compounds were obtained and identified as imperatorin (1), phellopterin (2), bergaptol (3), heraclenol (4), falcarindiol (5), isoimperatorin (6), byakangelicin (7), psoralen (8), bergapten (9), isogosferol (10), japoangelol A (11), atractylenolactam (12), columbianadin (13), 5-hydroxy-8-methoxypsoralen (14), (8E)-1,8-heptadecadiene-4,6-diyne-3,10-diol (15), pabulenol (16), byakangelicin ethoxide (17), isobyakangelicol (18), umbelliferone (19), xanthotoxol (20), osthole (21), alloimperatorin (22), 5-(2- acetoxy-3-hydroxy-3-methylbutoxy) psoralen (23), oxypeucedanin hydrate (24), oxypeucedanin ethanolate (25), alloisoimperatorin (26), pabularinone (27), oxyalloimperatorin (28), isooxypeucedanin (29), adenine (30), trans-ferulic acid (31), vanillic acid (32), 2-ethoxy-2-(4-hydroxyphenyl)-ethanol (33), suberosin (34), isopimpinellin (35), xanthotoxin (36), ulopterol (37), 2,4- dihydroxybenzoic acid methylate (38), scoparone (39), swietenol (40), marmesin (41), and 5-hydroxymethylfurfural (42), respectively. Conclusion: Except for the compounds 1, 3, 6, 7, 10, 13, 14, 16, 21, 24, and 26, other compounds were isolated from the roots of A. dahurica var. formosana for the first time.
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Objective: To study the effects of coumarins in Angelicae Dahuricae Radix (imperatorin, isoimperatorin, bergapten, and oxypeucedanin) on the activities of adenosine triphosphate (ATPase) in P-glycoprotein (P-gp) in vitro and to investigate the P-gp mediated meschanism in transport of drug. Methods: The ATPase activity assay was used to identify whether the coumarins in Angelicae Dahuricae Radix were P-gp substrates or not. Results: The average fluorescent values (ΔRLUTC) of imperation and oxypeucedanin at each concentration were greater than average basic fluorescence value (ΔRLUbasal). The average fluorescent values (ΔRLUTC) in medium and low concentration of isoimperatorin and bergapten groups were lower than average basic fluorescence value (ΔRLUbasal). Conclusion: Imperation and oxypeucedanun are non-concentration dependent P-gp ATP inhibitors. Isoimperatorin and bergamot lactones could inhibit the ATPase activity at low concentration and have the inhibitory effect on P-gp. At high concentration, the activity of ATPase can be induced so as to induce P-gp.
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To determine the contents of oxypeucedanin, oxypeucedanin hydrate, byakangelicol and byak-angelicin both before and after Angelicae Dahuricae Radix was stewed with yellow rice wine by high-performance liquid chromatography, and study the mutual transformation mechanisms of oxypeucedanin into oxypeucedanin hydrate, as well as byakangelicol into byak-angelicin. The research results indicated that the contents of oxypeucedanin and byakangelicol were decreased, but the contents of oxypeucedanin hydrate and byak-angelicin were increased after Angelicae Dahuricae Radix was processed with yellow rice wine. The contents' changes of these chemical compounds were due to the ring opening reaction of epoxy compounds, such as oxypeucedanin and byakangelicol under the weak acidity and heating conditions of yellow rice wine. This research could provide a scientific basis for the processing mechanism of Angelicae Dahuricae Radix with yellow rice wine stewing.
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Objective: To investigate the influence of furan coumarins from Angelicae Dahuricae Radix on intestinal absorption of puerarin, paeoniflorin, and vincristine, and to explore the influence law of furan coumarins on the intestinal absorption of the drugs with different structures. Methods: The apparent permeability coefficient (Papp) of drugs across the Caco-2 cell monolayers as evaluated index and Caco-2 cell model was used to study the absorption effects of furan coumarins (imperatorin, isoimperatorin, bergapten, and oxypeucedanin) on the transport of puerarin, paeoniflorin, and vincristine across Caco-2 cell monolayers. Results: There are different effects of the four coumarins on puerarin, paeoniflorin, and vincristine. For imperatorin, isoimperatorin, and oxypeucedanin could improve the transport of puerarin on Caco-2 cell significantly (P < 0.05, 0.01), while bergapten has no effect on the transport of puerarin across Caco-2 cell monolayers. For imperatorin and bergapten have no effect on the transport of paeoniflorin: However isoimperatorin and oxypeucedanin could significantly inhibit the transport of paeoniflorin across Caco-2 cell monolayers (P < 0.05, 0.01). Iperatorin, isoimperatorin, and oxypeucedanin could improve the transport of vincristine across Caco-2 cell monolayers significantly (P < 0.05, 0.01), but bergapten could significantly restrain the transport of vincristine across Caco-2 cell monolayers (P < 0.05). Conclusion: Different furan coumarins have different effects on the intestinal transport of the same medicine. Although the structures all are the furan type, the influence shows the opposite effect on drug transport. The same furan coumarin combined with different drugs have the different influences on the intestinal transport of compatibility drugs.