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Objective Based on the theory of"lung governs the skin and hair"in"Yellow Emperor's Inner Classic",this paper analyzes the medication rules of whitening and freckle-removing.The aim of this study is to provide reference for the clinical practice of traditional Chinese medicine(TCM)theory and the medication in TCM cosmetics.Methods"Chinese Medical Classics"was used to search the records of whitening and freckle-related drugs.The frequency,nature,flavor,meridian tropism and compatibility laws of TCM for whitening and freckle-removal were analyzed by statistics and association rules.The network pharmacology research was used to analyze the whitening and freckle-removing effects and mechanisms of high-frequency drugs.Then,the potential active ingredients were analyzed.The whitening and anti-freckle effect was verified through cytotoxicity experiments and melanin content detection.Results A total of 171 external prescriptions were selected in eligible articles,including 261 Chinese medicinals,most of which were pungent and belong to the lung meridian.The most frequently used Chinese medicinals was"Erbai Yixin"(EBYX,Angelicae Dahuricae Radix,Typhonii Rhizoma,Asari Radix et Rhizoma).Network pharmacological analysis showed that the core targets of EBYX for whitening and removing freckles are TP53,EGFR,ALB,etc.,which are mainly involved in oxygen perception and response,skin immune regulation,skin cell growth,differentiation,stress,inflammatory response,and other biological processes.Based on the results of molecular docking,biological analysis proved that the active ingredients of EBYX are chrysophanol,gallic acid and caffeic acid,which have inhibitory effects on the proliferation of melanoma cells and melanin production.Conclusion Most of the ancient prescriptions for whitening and removing freckles are pungent and belong to the lung meridian,which embodies the theory of"lung governs the skin and hair".The high-frequency drug EBYX may play a role by regulating skin redox,immunity and inflammation.The active ingredients of EBYX have an inhibitory effect on melanin formation.This study enriches the scientific connotation of TCM whitening and freckle-removing prescriptions based on the theory of"lung governs the skin and hair",realizes interdisciplinary integration and provides support for the modernization of TCM.
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Objective:To investigate the factors affecting the quality of post-harvest Angelicae Dahuricae Radix （Baizhi） and to provide the corresponding suggestions according to these factors. Method:A series of factors affecting the quality of Baizhi were analyzed comprehensively by visiting several origins， medicinal material markets， pharmacies， supermarkets and storehouses combined with plenty of literature reports. Result:The rot of Baizhi was the most common phenomenon after harvest， and mildew， discoloration and moth could occur during the processes of processing， storage and packaging. So the quality of Baizhi should be controlled strictly through the whole process. The roots of Baizhi should be harvested on sunny days to avoid mining damage and dried as soon as possible to prevent rotting. The drying methods included both traditional lime burial and modern ways such as sulfur fumigation， saline dehydration， sun drying method， and oven drying method. However， the water content should be strictly controlled. Furthermore， the storehouses should be disinfected firstly. The temperature and humidity of the storehouses should be controlled strictly. Some suitable ways could be adopted to prevent moth and discoloration during storage， which included airtight fumigation of aluminum phosphide， cold storage， air conditioning maintenance， antagonism storage with other Chinese medicinal materials， dry ice storage at room temperature， etc. Large quantities of Baizhi were generally packaged in woven bags. Otherwise， kraft paper bags， polyvinyl chloride plastic bags， glass bottles， aluminum foil composite film bags， and other packaging materials had been adopted for the retail. However， the packaging specification should be selected according to the situation. Conclusion:The quality of Baizhi can be directly affected by harvesting， drying， processing， storage and packaging. Scientific and reasonable methods should be adopted to ensure the quality of Baizhi.
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To study the changes in the pharmacokinetic behavior of four coumarins (bergapten, oxypeucedanin, imperatorin and isoimperatorin) in rats before and after combinating Angelicae Dahuricae Radix with Chuanxiong Rhizoma. The plasma concentrations of the drugs were determined by ultra performance liquid chromatography-fluorescence detection (UPLC-FLD) for dose response and time dependent curves. The pharmacokinetic parameters were calculated by DAS 3.2.8, and SPSS 20.0 was used to analyze the differences of main pharmacokinetic parameters between the two groups. The result showed: comparing with Angelicae Dahuricae Radix group, the area under drug time curve (AUC0-24 h) of bergapten, oxypeucedanin and imperatorin increased by 177.2%, 97.14% and 54.43% respectively, AUC0-∞ increased by 282.3%, 104.2%, and 75.40% respectively, and clearance rate (CLZ/F) decreased by 68.26%, 51.08% and 43.98% respectively; the peak drug concentration (Cmax) of four coumarins was significantly increased; the distribution volume (VZ/F) of bergapten was significantly decreased. These data indicated that Chuanxiong Rhizoma can promote the absorption of coumarins in Angelicae Dahuricae Radix, slow down the elimination of coumarins, and increase their bioavailability in vivo. The animal experiment scheme in this study has been approved by the Experimental Animal Ethics Committee of Beijing University of Chinese Medicine (approval number: BUCM-4-2020083105-3072).
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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 observe the preventive effects of combined application of total coumarin and essential oil of Angelicae Dahuricae Radix on the migraine rats induced by nitroglycerin, and to explore their mechanisms. Methods: A total of 56 Wistar rats were randomly divided into normal control group (saline 0. 1 mL · 10 g 1), migraine model group (saline 0. 1 mL · 10 g 1), total coumarin of Angelicae Dahuricae Radix group (100 mg · kg-1), essential oil of Angelicae Dahuricae Radix group (100 mg · kg-1), and low dose (25 mg · kg-1), middle dose (50 mg · kg-1) and high dose (100 mg · kg-1) of total coumarin and essential oil composition of Angelicae Dahuricae Radix groups (composition groups) (n=8). After continuously intragastric adminstration for 7 d, the rats were injected subcutaneously with nitroglycerin (10 mg · kg-1) for establishing the migraine models. The behavior of the rats were observed, the levels of nitric oxide (NO) in serum and brain tissue of rats, the levels of calcitonin gene related peptide (CGRP) and endothelin (ET) in plasma of the rats in various groups were detected. Results: Compared with normal control group, the frequencies of head shaking, the face shoting times of posterior legs and the scratching times of anterior limbs of the rats in migraine model group were increased (P<0. 05 or P<0. 01), and the levels of NO in serum and brain tissue of the rats were increased (P< 0. 01). Compared with migraine model group, the frequencies of head shaking, the face shoting times of posterior legs and scratching times of anterior limbs of the rats in total coumarin group, essential oil group, and composition groups were decreased (P<0. 05 or P<0. 01), and the levels of NO in serum and brain tissue of the rats were decreased (P<0. 05 or P<0. 01). Compared with migraine model group, the levels of CGRP and ET in plasma of the rats in essential oil group, total coumarin group and middle and high doses of composition groups were decreased (P<0. 05). Conclusion: The composition of two active ingredients of Angelicae Dahuricae Radix, total coumarin and essential oil, has preventive effects in the migraine rats induced by nitroglycerin, and their mechanisms may be related to regulation of the levels and function of vasoactive substances.
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Objective To prepare the reservoir patch of coumarins in Angelicae Dahuricae Radix and investigate its release and transdermal absorption characteristics in vitro. The efficient enhancers were chosen to improve the drug’s permeation rate. Methods The reservoir patch was prepared using hydroxypropyl methylcellulose (HPMC) as medium and ethylene vinyl acetate (EVA) membrane to control the release of drug. The Franz diffusion cells were used and HPLC was used to determine imperatorin content and permeation rate. The content of imperatorin was determined by HPMC. The effect of the gel consumption, the content of coumarins and penetration enhancer on the transdermal flux were investigated by selecting porcine skin as model. The release of the selected patch in vitro was investigated. Results 1% HPMC, 1% coumarins in Angelicae Dahuricae Radix, 1% Isopropyl Myristate (IPM) and 3% Azone were the best permeation of the patch. The permeation rate reached 0.713 μg/(cm2•h). The release mechanisms of the patch in vitro coincided with zero-order kinetic. Conclusion The reservoir patch of coumarins in Angelicae Dahuricae Radix had high transdermal rate and complete in vitro release. It was indicated that the patch could be expected to be an effective transdermal drug delivery system.
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Objective To investigate the effect of compatibility on brain tissue distribution in rat of corydaline, tetrahydropalmatine, protopine, imperatorin and isoimperatorin in Corydalis Rhizoma and Angelicae Dahuricae Radix, and to provide further experimental evidence for confirming the Q-marker of Yuanhu Zhitong Prescription. Methods After oral administration of Corydalis Rhizoma, Angelicae Dahuricae Radix, and Yuanhu Zhitong Prescription extracts respectively, the concentration of five compounds in brain tissue samples at different time points was determined by UPLC-MS/MS, and the effect of compatibility on brain tissue distribution was further evaluated by kinetic parameters. Results Compared with single-herb group, AUC and Cmax of corydaline, tetrahydropalmatine and protopine in Yuanhu Zhitong Prescription group were increased significantly, and MRT of imperatorin and isoimperatorin were prolonged at the same time. Conclusion Corydalis Rhizoma and Angelicae Dahuricae Radix exist synergistic effect, the compatibility of these two herbs promote brain tissue distribution of corydaline, tetrahydropalmatine, protopine, imperatorin and isoimperatorin, which can be used as Q-marker of Yuanhu Zhitong Prescription.
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AIM To investigate the effects of aqueous extraction at normal temperature,40 ℃,and water boiling on total coumarins extract of Angelicae dahuricae Radix.METHODS For the extracts Ⅰ-Ⅳ obtained by ethanol reflux extraction and three aqueous extraction preprocessing methods,respectively,UV and HPLC were adopted in the content determination of total coumarins and imperatorin,then the powder properties and dissolution rates were compared.RESULTS The contents of total coumarins in four extracts were 3.98％,6.03％,6.81％ and 4.46％,while those of imperatorin were 0.633％,0.540％,0.465％ and 0.155％,respectively.The angles of repose were 48.455°,42.587°,42.689° and 42.024° with the bulk densities of 0.214,0.324,0.316 and 0.354 g/cm3,respectively.Within 100 min,extract Ⅰ demonstrated higher moisture adsorption rate and equilibrium moisture absorption content than the other three extracts.The accumulative dissolution rates of various extracts were much higher than that of medicinal material fine powder within 120 min.CONCLUSION All the three aqueous extraction preprocessing methods can obviously improve the powder properties of total coumarins extract of A.dahuricae Radix and increase the dissolution rate of medicinal material fine powder.
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Objective To establish the HPLC fingerprint of Liujing Toutong Tablets (LTT) and multi-wavelength method for determination of the contents of 3’-hydroxy puerarin, puerarin, daidzin, nuezhenide, and daidzein, so as to provide a reference for the quality control. Methods Using the method of HPLC, the fingerprint chromatography of high polarity and low polarity were established, with a mobile phase of acetonitrile-0.1% phosphoric acid and Diamonsil C18 column (250 mm × 4.6 mm, 5 μm). Furtherly, the Diamonsil C18 column was used with a mobile phase of acetonitrile-0.1% acetic acid gradient elution to determine the five contents. Results The fingerprint chromatography of high and low polarities with 11 batches of LTT were established, and the similarities of 11 batches were all over 0.90. The low polarity fingerprint chromatography included 16 mutual peaks, 12 of which belonged to herbs: No. 11, 12, 13 belonged to Angelicae Dahuricae Radix, No. 1, 2, 3, 7 belonged to Puerariae Lobatae Radix, No. 8 belonged to Ligustri Lucidi Fructus, No. 5, 6 belonged to Chuanxiong Rhizoma, No. 15 belonged to Ligustici Rhizoma et Radix and No. 4 belonged to Chuanxiong Rhizoma and Ligustici Rhizoma et Radix. Seven peaks including puerarin (No. 1), 3’-methoxy puerarin (No. 2), daidzin (No. 3), ferulic acid (No. 4), daidzein (No. 7), imperatorin (No. 11), and isoimperatorin (No. 13) were verified by standard compounds. The high polarity fingerprint chromatography included 10 mutual peaks, among them No. 2-9 belonged to Puerariae Lobatae Radix, No. 1, 10 belonged to Ligustri Lucidi Fructus. Five peaks including 3’-hydoxypuerarin (No. 2), puerarin (No. 3), 3’-methoxypuerarin (No. 4), daidzin (No. 7) and specnuezhenide (No. 10) were verified by standard compounds. The five active components were well separated and showed good lineaeity, such as 3’-hydroxy puerarin 71.60-716.00 ng (r = 0.999 1), puerarin 407.78-4 077.80 ng (r = 0.999 4), daidzin 90.72-907.20 ng (r = 0.999 9), nuezhenide 95.80-958.00 ng (r = 0.999 1), daidzein 21.98-219.80 ng (r = 0.999 9). The average recoveries and corresponding RSD values were 101.1% (1.38%), 97.8% (0.72%), 99.1% (0.75%), 97.8% (2.75%), and 98.7% (0.70%). The contents of 3’-hydoxypuerarin, puerarin, daidzin, specnuezhenide and daidzein in the 10 batches of sample were 3.08-3.84 mg/mL, 17.71-21.24 mg/mL, 3.51-4.71 mg/mL, 1.40-5.69 mg/mL, and 0.66-0.86 mg/mL, respectively. Conclusion The HPLC fingerprint combined with multi index determination method can reflect the intrinsic quality of LTT, which is stability, accurate, and reproducible, providing a scientific reference for quality control.
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Objective: To explore the compatibility rationality of Yuanhu Zhitong Dropping Pills (YZDP) for the treatment of primary dysmenorrhea. Methods: The potential targets and pathways of tetrahydropalmatine, palmatine, glaucine, protopine, imperatorin, and isoimperatorin, selected as the representative compounds of alkaloid and coumarin from Corydalis Rhizoma and Angelicae Dahuricae Radix, were predicted by the methods of network pharmacology. The results were verified by docking and the mechanism and compatibility regularity of YZDP were analyzed by integrating all the data. Results: The in silico prediction results showed that the six compounds of YZDP affected 19 related pathways through 23 target proteins. The pathways were involved in central analgesia, hormonal regulation, spasmolysis, vasodilatation, inflammation, and immunoregulation. The alkaloid and coumarin showed common targets and pathways but also had their own emphasis. The pathways were connected by the common targets, showing the synergistic effect of different compounds by acting on multi-targets and multi-pathways. Conclusion: Corydalis Rhizoma acts as monarch drug, showing the effect of analgesia, regulating qi, and activating blood by acting on thromboxane receptors, angiotensin receptors, and targets related with central analgesia and spasmolysis. Angelicae Dahuricae Radix, showing the effect of regulating qi, and activating blood by regulating the pathways of spasm, inflammation, and so on, acts as ministerial drug to assist monarch drug to enhance treatment which reflected the compatibility rationality of Corydalis Rhizoma and Angelicae dahuricae Radix.
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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 establish an HPLC characteristic spectrum of raw herbs-decoction pieces-extract-dispensing granules of Angelicae Dahuricae Radix (ADR) and evaluate the correlation among them. Methods: Gradient elution was performed with mobile phase of acetonitrile-water, detection wavelength of 320 nm, flow rate of 1.0 mL/min, and column temperature of 25℃, by setting the characteristic spectrum as control and evaluating the correlation of raw herbs-decoction pieces-extract-dispensing granules. Results: There were 10 common characteristic peaks in all characteristic spectra of 10 batches of raw herbs, decoction pieces, extract, and dispensing granules of ADR, presenting a good correlation. Conclusion: This study established an HPLC characteristic spectrum and reflected the whole picture of multi-component of raw herbs, decoction pieces, extract, and dispensing granules of ADR provides the reference for quality control of dispensing granules of ADR.
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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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Objective To evaluate the quality coherence of commercial Angelicae Dahuricae Radix (Baizhi) decoction pieces. Methods The samples of 12 batches of commercial decoction pieces, 1 batch of sulphur fumigated Baizhi, and 1 batch of naturally dried Baizhi were collected. HPLC method was used to determine the fingerprints and the contents of imperatorin and isoimperatorin by C18 column (4.6 mm×250 mm, 5 μm) with a gradient mobile phase of acetonitrile-water solution system at the flow rate of 1.0 mL/min. The column temperature was set at 35 ℃, and the max plot of detection wavelength was in 210-800 nm. Similarity calculation was used to analyze the data. Results The HPLC fingerprint analysis method was established with 12 common peaks. The similarities of 12 batches of commercial decoction pieces of Baizhi were 0.840-0.973. Their similarities compared with the sulphur fumigated Baizhi were 0.672-0.908. Compared with naturally dried Baizhi, the similarities of fingerprint were 0.536-0.684. The contents of imperatorin and isoimperatorin in 12 batches of commercial decoction pieces were 0.035%-0.140% and 0.028%-0.069%, respectively. Conclusion The quality of Baizhi decoction pieces was consistent. It can be speculated that Baizhi decoction pieces were processed with sulphur fumigation.
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Objective: To establish the ultra-fast liquid chromatographic (UFLC) fingerprint of Huoxiang Zhengqi Dripping Pill (HZDP) for evaluating the quality of the preparation. Methods: The UFLC separation was achieved on an Waters Acquity UPLC BEH C18 column (100 mm × 2.1 mm, 1.7 μm) with acetonitrile (A)-0.2% formic acid solution (B) as mobile phase at the flow rate of 0.4 mL/min by gradient elution of 0-6 min, 10% →15% A, 6-9 min, 15% →20% A, 9-14 min, 20% →30% A, 14-19 min, 30% → 50% A, 19-21 min, 50% →65% A, 21-26 min, 65% →75% A, 26-28 min, 75% A, 28-30 min, 75% →10% A, 30-32 min, 10% A. The column temperature was 30 ℃. The UV detection wavelength was 300 nm. The similarity of 11 batches of HZDP was analyzed with similarity evaluation system for chromatographic fingerprint of tradition Chinese medicine (Version 2004 A). Results: Fingerprints of 11 batches of HZDP were established and 18 common peaks were identified, 13 of which belonged to herbs and were identified by the reference substance and UFLC-IT-TOF/MS. Among them, five common peaks (peaks 6, 7, 9, 10, and 12) came from Angelicae Dahuricae Radix, three common peaks (peaks 4, 5, and 8) came from Citri Reticulatae Pericarpium, four common peaks (peak 1, 2, 11, and13) came from Magnoliae Officmalis Cortex, and one common peak (peak 17) came from Atractlodis Rhizoma. Conclusion: The method is rapid, accurate, reliable, and reproducible. The established fingerprint could provide the references for the study of substance basis and quality control of HZDP.
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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.
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Objective To study whether sulphur fumigation can cause changes to the content of imperatorin in Angelicae Dahuricae Radix (Baizhi).Methods The fresh samples of Angelicae Dahuricae Radix were collected from some cultivation bases. Half of each batch root was fumigated with sulfur according to the conventional method, and another half was cut into slices and dried naturally (i.e. without sulfur fumigation). The content of imperatorin was determined by HPLC on C18 column (4.6 mm×250 mm, 5μm) with a gradient mobile phase of acetonitrile-water solution system at the follow rate of 1.0 mL/min, 35℃ of the column temperature, and the max plot in 210-800 nm of the detective wavelength.ResultsTotally 29 batches of fresh roots ofAngelica dahurica were collected. The average contents of imperatorin were 0.202% in the Angelicae Dahuricae Radix with sulfur fumigation and 0.120% in the Angelicae Dahuricae Radix without sulfur fumigation. Compared with the corresponding samples without sulfur fumigation, the content of imperatorin in every Angelicae Dahuricae Radix with sulfur fumigation decreased by 6.77%-77.56% with an average decrease of 39.86%.Conclusion The content of imperatorin decreased significantly in every batch of Angelicae Dahuricae Radix with sulphur fumigation. It shows that the sulphur fumigation method was not suitable for producing and processing Angelicae Dahuricae Radix from fresh roots ofA. dahurica.
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Objective: To prepare and optimize the formulation of intranasal thermo-sensitive gel of Zhi Xiong San and to evaluate its in vitro release mechanism and nasal mucosa permeability. Methods: The formulations of poloxamer thermo-sensitive gel were optimized by a central composite design-response surface method and its in vitro release mechanism and nasal mucosa permeability were evaluated by Franz diffusion chambers. Results: The optimal formulation was Poloxamer 407 (P407) 20% and Poloxamer 188 (P188) 6.5%. Imperatorin was released from the thermo-sensitive gels approximately with a zero-order mechanism, while ferulic acid with a Higuchi model. The formulation demonstrated the enhancement of nasal mucosa permeability. Conclusion: The optimal formulation provides a basis for the development of new administration routes and dosage forms of Zhi Xiong San.
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Objective: To study the chemical constituents of Huoxiang Zhengqi Liquid. Methods: Silica gel column chromatography, preparative thin-layer chromatography, and recrystallization were used to isolate the chemical constituents from chloroform extract. And the structures of compounds were identified by spectral analysis and physicochemical properties. Results: Fifteen compounds were obtained and identified as liquiritin (1), liquiritigenin (2), isoliquiritigenin (3), formononetin (4), oxypeucedanin hydrate (5), byakangelicin (6), hesperidin (7), 5, 7, 8, 3′, 4′- pentamethoxyflavone (8), 5, 6, 7, 3′, 4′-pentamethoxyflavone (9), 5, 7, 8, 4′-tetramethoxyflavone (10), nobiletin (11), 3, 5, 6, 7, 8, 3′, 4′-heptamethoxyflavone (12), tangeretin (13), honokiol (14), and magnolol (15). Conclusion: All the compounds are isolated from Huoxiang Zhengqi Liquid for the first time. Compounds 1-4 may come from Glycyrrhizae Radix et Rhizoma; compounds 5 and 6 from Angelicae Dahuricae Radix; compounds 7-13 from Citri Reticulatae Pericarpium; and compounds 14 and 15 from Magnoliae Officinalis Cortex.
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Objective: To study the enzymatic reaction kinetics of dl- tetrahydropalmatine (TET) in total alkaloid (TA) of Corydali Rhizoma in rat liver microsomes and to investigate the compatible effects of the effective components such as coumarin (Cou) and volatile oil (VO) in Angelicae Dahuricae Radix with TA in Corydali Rhizoma on enzymatic reaction kinetics of TET. Methods: Rat liver microsomes were prepared by ultracentrifugation and the TET concentration in incubation medium was determined by HPLC. Comparative study on the enzymatic reaction kinetics of TET in each group of TA, TA-Cou, TA-VO, and TA-Cou-VO to deduce the michaelis constant (Km) and maximum reaction rate (Vmax) of TET in each group and calculate the clearance rate (CLint) of TET in each group. Results: The Km, V max, and CLint in TA group were 0.12 μmol/ (L·min·mg), 5.40 μmol/L, and 0.022 L/(min·mg), respectively; In TA-Cou group they were 0.27 μmol/(L·min·mg), 40.18 μmol/L, and 0.006 L/(min·mg), respectively; In TA-VO group they were 0.57 μmol/(L·min·mg), 22.60 μmol/L, and 0.025 L/(min·mg), respectively; In TA-Cou-VO they were 0.84 μmol/(L·min·mg), 23.25 μmol/L, and 0.036 L/(min·mg), respectively. Conclusion: The effective components of TA in Corydali Rhizoma with Cou and VO in Angelicae Dahuricae Radix could decrease CLint of TET in TA of liver.