ABSTRACT
Phenylalaninammo-nialyase (PAL) is a key enzyme in the synthesis of methyl benzoate - a plant aroma compound. In order to understand the function of this enzyme in the formation of fragrance in the scented Rhododendron species-Rhododendron fortunei, we cloned a gene encoding this enzyme and subsequently examined the gene expression patterns and the profile of enzyme activity during development in various tissues. The full length of RhPAL gene was cloned by reverse transcription-PCR (RT-PCR) and rapid amplification of cDNA ends (RACE) techniques. The expression levels of RhPAL gene were measured by real-time quantitative reverse transcription PCR (qRT-PCR) and the amount of phenylalanine and cinnamic acid were assayed with LC-MS. The results showed that the ORF sequence of RhPAL gene amplified from the cDNA templates of flower buds had 2 145 bp, encoding 715 amino acids, and shared 90% homology to the PAL amino acid sequences from other species. qRT-PCR analysis showed that the expression of RhPAL in petals during flowering kept in rising even until the flowers wilted. The expression of RhPAL in pistil was much higher than that in stamen, while the expression in the younger leaves was higher than in old leaves. However, the expression level was relatively lower in petal and stamen compared to that in leaves. We also measured the PAL activity by Enzyme-linked immuno sorbent assay in the petals of flowers at different flowering stages. The results showed that PAL activity reached the highest at the bud stage and then decreased gradually to the lowest when the flowers wilted, which followed a similar trend in the emission of the flower fragrance. The phenylalanine and cinnamic acid contents measured by LC-MS were highly correlated to the expression level of RhPAL in various tissues and at different flowering stages, implying that RhPAL plays an important role in the formation of the flower fragrance. This work may facilitate the breeding and improvement of new fragrant Rhododendron cultivars.
Subject(s)
Amino Acid Sequence , Cloning, Molecular , DNA, Complementary , Flowers/genetics , Rhododendron/geneticsABSTRACT
Objective:To develop the UPLC-MS/MS method for the determination of amygdalin, cinnamic acid, rhein, emodin and glycyrrhizic acid in Taohe-Chengqi Decoction simutaneously. Methods:The separation was performed on Supelco Discovery C18, and isocratic elution was carried out with mobile phase consisting of acetonitrile - 4 mmol/L ammonium formate. The mass spectrometer was operated in the positive and negative ionization electrospray (ESI) mode using multiple monitoring (MRM) to analize of five ingredients. The precursor to product ion transitions monitored for amygdalin, cinnamic acid, rhein, emodin and glycyrrhizic acid were m/z 458.2→296.0, 146.8→103.1, 283.7→239.9, 269.7→226.1 and 821.4→350.9, respectively. Results:Amygdalin, cinnamic acid, rhein, emodin and glycyrrhizic acid were analyzed, the linear ranges were 0.001 6-0.102 4, 0.001 6-0.102 4, 0.001 6-0.102 4, 0.000 8-0.051 2 and 0.000 4-0.256 0 ng, respectively. The r were 0.998 7, 0.999 1, 0.999 5, 0.998 9 and 0.998 6, respectively. The recovery of five analytes ranges from 97.33% to 105.33% and the Relative Standard Deviations were all below 2.69%. Conclusion:This UPLC-MS/MS method is exclusive, rapid and sensitivewhich could be applied for the determination of amygdalin, cinnamic acid, rhein, emodin and glycyrrhizic acid in Taohe-Chengqi Decoction.
ABSTRACT
Objective: To establish an HPLC fingerprint analysis method of Zhishi Xiebai Guizhi Decoction (ZXGD) and the content determination method of 10 index components of the decoction, and carry out the relevant evaluation and analysis. Methods: HPLC method was used to establish the fingerprint analysis method of ZXGD and then similarity evaluation was carried out. Ten index components of the decoction were determined, the influence of the change of compatibility of medicinal materials on the content of index components was analyzed. Cluster analysis and other chemometrics methods were used to analyze the relevant data and evaluate the impact and value of quality control related indicators of ZXGD. Results: The similarity of 10 batches of samples ranged from 0.376 to 0.990, and that of five batches was more than 0.9, which indicated that the similarity of 10 batches of samples was quite different. In 10 batches of samples, S1, S2, S3, S5, S6, S8 and S10 were in one group, S4 and S9 were in one group, S7 was in one group. In this study, 30 characteristic peaks were calibrated, and principal components 1-6 was the main factor affecting the quality evaluation of medicinal materials. Among the 30 characteristic peaks, peak 21 (neohesperidin), 26, 29 (honokiol), 3, 23, 17, 30 (magnolol), 5, 24 (coumarin), 28, and 7 were the key components. The results showed that except quercetin, the other nine components had good linear relationship, precision, stability and repeatability in the range of mass concentration. Different compatibilities could increase or inhibit the dissolution of related components in medicinal materials. Conclusion: The HPLC method can be used for the simultaneous determination of ten chemical components in ZXGD. The method is efficient, accurate and reproducible, and can be used for the quality control and evaluation of ZXGD.
ABSTRACT
Objective: To analyze and predict the Q-marker of Cinnamomi Ramulus in Danggui Sini Decoction based on fingerprint and network pharmacology. Methods: The fingerprints of Cinnamomi Ramulus Decoction and Danggui Sini Decoction were established, and analyzed by using the similarity evaluation system software for chromatographic fingerprint of traditional Chinese medicine (2012 edition); The network pharmacology was used to screen and analyze the function target and pathway of related components of Cinnamomi Ramulus, and the "component-target-pathway" network was constructed to predict the potential Q-marker of Cinnamomi Ramulus in Danggui Sini Decoction. Results: The fingerprints of 15 batches of Cinnamomi Ramulus Decotion and 15 batches of Danggui Sini Decoction were established. The similarity of fingerprints was more than 0.96, and seven common components were identified, including protocatechuic acid, coumarin, cinnamic acid, cinnamaldehyde, cinnamyl alcohol, 2-methoxy cinnamic acid, and 2-methoxy cinnamaldehyde. A total of five active components, seven core target sites and 15 key pathways of Cinnamomi Ramulus were screened out through network pharmacology system, and based on the "Five Principles" of quality markers, 2-methoxy cinnamaldehyde, cinnamaldehyde, and cinnamic acid were predicted as potential quality markers. Conclusion: In this study, the quality markers of Cinnamomi Ramulus in Danggui Sini Decoction are analyzed by fingerprint and network pharmacology, which provides a basis for comprehensive control of the quality of Danggui Sini Decoction, reference for further study on the mechanism of Danggui Sini Decoction, and demonstration for the correlation study of quality markers of compound and single medicine in the classic prescription.
ABSTRACT
Objective: To study the effect of compatibility on pharmacokinetics of the main components of Guizhi Zhumian prescription (GZP) based on the concept of Q-marker and to provide evidences for the determination of the Q-markers of this prescription. Methods: UPLC-MS/MS method was established for the study of the pharmacokinetics behaviors of seven main components, including cinnamic acid, 4-methoxycinnamic acid, coumarin, gardenoside, genipin, geniposidic acid, and chlorogenic acid, before and after the compatibility of GZP in plasma of cynomolgus monkeys. Results: Compared with the pharmacokinetics parameters of Cinnamomum cassia and Gardenia jasminoides, the AUC and Cmax of cinnamic acid, coumarin, geniposidic acid, and chlorogenic acid in GZP were increased obviously; The t1/2 of cinnamic acid, 4-methoxycinnamic acid, and coumarin were decreased; And the tmax of 4-methoxycinnamic acid, and geniposide were prolonged. Conclusion: Compatibility of GZP could significantly change the in vivo exposure status of the main components, and the seven main compounds were determined to be the Q-markers of GZP.
ABSTRACT
Objective::To establish a rapid evaluation method for Cinnamomi Cortex decoction pieces by near infrared spectroscopy. Method::The contents of coumarin, cinnamalol, cinnamic acid and cinnamaldehyde in 86 batches of Cinnamomi Cortex of different origins were determined by HPLC. And the NIR spectra of different batches of Cinnamomi Cortex were also collected. With NIR spectrum as independent variable and coumarin, cinnamalol, cinnamic acid and cinnamaldehyde as dependent variables, a quantitative analysis model of four components in cinnamon was established by partial least squares method. Result::The correlation coefficients (r) of coumarin, cinnamic alcohol, cinnamic acid and cinnamaldehyde near infrared quantitative analysis models were 0.952 8, 0.977 7, 0.961 9, 0.992 2, root mean square error of cross(RMSEC) were 0.012 2, 0.006 1, 0.004 3, 0.82 g·g-1, root mean square errorof cross-validation(RMSECV) were 0.015 8, 0.011 2, 0.002 0, 1.481 1 g·g-1, and root mean square error of prediction(RMSEP) were 0.017 8, 0.010 3, 0.010 3, 0.005 5, 1.63 g·g-1. Conclusion::The established NIR quantitative analysis model of four active ingredients in Cinnamomi Cortex slices has a good accuracy, and provides a basis for rapid evaluation of the quality of Cinnamomi Cortex slices.
ABSTRACT
Objective To develop a high-performance liquid chromatography-diode array detector (HPLC-DAD) method for determination of cinnamic acid in the decoction of cinnamon, and investigate the effect of different storage temperature and time for the stability of cinnamic acid. Methods An HPLC- DAD method was established. Separation was performed on an Agilent Zorbax C18 column (4.6 mm×250 mm, 5 μm) with 0.1% formic-acetonitrile acid water solution (60:40) as the mobile phase by isocratic elution. The flow rate was 1.0 ml/min, the temperature of column was 25 ℃, the injection volume was 5 μl, the detective UV wave length was 275 nm. The decoction were stored under refrigerated temperature (4 ℃) ambient temperature (25 ℃) and high temperature (40 ℃). The cinnamic acid was detected after 0, 1, 3, 7, 14, 21, 30 d. Results Cinnamic acid was successfully separated by this method, with good linear relationship between 10.21-204.20 μg/ml. The precision, repeatability, stability and recovery were good. Compared with the zero day, the content of cinnamic acid in the decoction of cinnamon decreased significantly (P<0.01) after 21 days and 30 days of ambient temperature storage and after 14 days, 21 days and 30 days of high temperature storage, but no significant change was found in the other groups (P>0.05). Conclusion This HPLC-DAD method had good stability and repeatability. Cinnamic acid was stable in the decoction of cinnamon for 30 days under refrigerated temperature.
ABSTRACT
Objective: To establish a quantitative analysis of multi-components by single marker(QAMS)method for the simultaneous determination of jaceosidin, eupatilin, limoni, evodiamine, rutaecarpine, cinnamyl alcohol, cinnamic acid and cinnamal-dehyde in Changwei San. Methods: The Waters Symmetry C18 column(250 mm×4.6 mm, 5 μm)was used for the separation, and the mobile phase was the acetonitrile(A)and 0.1% phosphoric acid(B)solution in a gradient elution at a flow rate of 1.0 ml/min. The detection wavelengths were set at 345 nm for jaceosidin and eupatilin, 215 nm for limoni, evodiamine and rutaecarpine, and 275 nm for cinnamyl alcohol, cinnamic acid and cinnamaldehyde. With evodiamine as an internal reference standard, the relative correction factors for the other 7 components were established and their contents were calculated with the relative correction factors to achieve the QAMS, and then the differences between the calculated values by QAMS and measured values by the external standard method(ESM) were compared to validate the accuracy and feasibility of the QAMS method. Results: Jaceosidin, eupatilin, limoni, evodiamine, rutaecarpine, cinnamyl alcohol, cinnamic acid and cinnamaldehyde showed good linear relationships within the ranges of 0.98-19.60, 2.67-53.40, 4.06-81.20, 1.98-39.60, 2.69-53.80, 0.56-11.20, 1.49-29.80, and 8.77-175.40 μg/ml(r≥0.9992), whose average recoveries(RSD) were 98.77%(0.96%), 99.38%(1.01%), 100.02%(0.83%), 97.80%(1.40%), 98.91%(1.18%), 96.99% (1.13%), 98.09%(1. 24%)and 99.10%(0.67%), respectively. No significant difference was observed between the calculated values by QAMS and the measured values by ESM. Conclusion: The established QAMS method is simple and accurate, which might be used to evaluate the quality of Changwei San.
ABSTRACT
Objective: To synthesize sophocarpine-cinnamic acid ester derivatives and evaluate the in vitro antitumor activities of the derivatives. Methods: Taking sophocarpine as the starting material, the target compounds were synthesized by oxidation, esterification, N-alkylation, reduction, condensation, hydrolysis, and salification. Their antitumor activities in vitro were evaluated for HeLa, HepG2 and A-549 by MTT assay. Results: Eleven sophocarpine-cinnamic acid ester derivatives were synthesized and the structures were characterized by 1H-NMR, 13C-NMR and HRMS. MTT assay showed that some derivatives exhibited good antitumor activities. Compound 5g showed good antitumor activity against three human tumor cell lines, which was better than that of the positive control drug, cisplatin. Conclusion: Some derivatives showed promising antitumor activities and compound 5g was worth further studying.
ABSTRACT
Objective In order to provide a scientific basis for the grade quality standard criterion of Scrophulariae Radix, a HPLC-DAD method was established to acquire fingerprint and detect the content of multiple components. Methods The chromatographic separate was achieved on Elipse XDB-C18 (250 mm × 4.6 mm, 5 μm) column, with the temperature of 25 ℃, using acetonitrile (A)-0.03% phosphoric acid water (B) as the mobile phase gradient elution, a flow rate of 1.0 mL/min, and the detection wavelength was set at 207 nm for fingerprint, 210 nm for Harpagide, 280 nm for harpagoside, and 264 nm for cinnamic acid. The injection volume was 10 μL. The fingerprints of different grades of Scrophulariae Radix from 30 batches were evaluated with a chromatographic fingerprint similarity evaluation system (version 2012), and the content of harpagide, harpagoside, and cinnamic acid was also determined at the same time. Results There were seven common peaks in the fingerprints, the RSD values of relative retention time were lower than 2.0% and those of relative peak area were quite different, which indicated that the main chemical compounds can exist stably in Scrophulariae Radix with different content. Compared with control, the results of fingerprintsimilarity were presented as follows: 5% under 0.7, 12.5% arranged 0.7 to 0.8, 40% between 0.8 and 0.9, and another 42.5% exceed 0.9, demonstrated that there was qualitative difference in various batches of Scrophulariae Radix. Also, the quantitative analysis of multi-index showed the differences in three main compounds, the content respectively was 0.18%—2.89% in harpagide, 0.01%—0.35% in harpagoside, and 0.01%—0.24% in cinnamic acid. Conclusion Suggestions were provided in the formulation of new grade quality standard, such as adding the fingerprints and multi-index detection of main chemical components based on the original criterion of classification.
ABSTRACT
Objective: To study the chemical constituents from Litchi Semen. Methods: Different column chromatographic techniques were used to separate and purify the chemical constituents and their structures were elucidated by spectral analysis. Results: A total of 15 compounds were isolated and identified as 5-p-trans-coumaroylquinic acid (1), 3-O-trans- coumaroylquinic acid (2), phlorizin (3), naringin (4), rutin (5), naringenin-7-O-rutinoside (6), kaempferol 3-O-(6-O-caffeoyl)-β-D- glucopyranosyl-(1→2)-α-L-rhamnopyranosyl-7-O-α-L-rhamnopyranoside (7), proanthocyanidin A-2 (8), p-hydroxybenzoic acid (9), protocatechuic aldehyde (10), p-hydroxybenzaldehyde (11), protocatechuic acid (12), Z-p-hydroxy-cinnamic acid (13), E-p-hydroxy-cinnamic acid (14), and 3,6-dihydroxy-5,11-epoxy-7Z-megastigmaen-9-one (15). Conclusion: Compounds 1, 2, 7, 13-15 are isolated from the genus Litchi for the first time, and they are also isolated from this plant for the first time.
ABSTRACT
Objective: In this study, a two-classification model based on the idea of “ingredient-efficacy” was established for the quality classification of Cinnamomum cassia with considerations to quality control components and biological activities. Methods: A method to determine quality control components was proposed by UPLC. The in vitro anti-oxidant activity of C. cassia was reflected by DPPH and hydroxyl radical scavenging experiment. The quality control index and anti-oxidant index were correlated by a Logistic algorithm. Finally, a binary logistic regression model for classification of C. cassia was established. Results: UPLC fingerprints of 20 samples of C. cassia were established, and their anti-oxidant activities were determined. Four quality control components (coumarin, cinnamyl alcohol, cinnamic acid, and cinnamaldehyde) were screened out by principal component analysis, and their methodological validation was carried out. According to the regression equation, 20 batches of C. cassia were divided into four grades: excellent, good, medium, and poor. Conclusion: The binary logistic regression model can describe the mapping relationship between the grade of C. cassia. It can better express the classification standard for the prepared C. cassia. This study provides a new idea for quality evaluation of C. cassia.
ABSTRACT
OBJECTIVE： To establish a method for simultaneous determination of gallic acid， cinnamic acid and catechin in 3 processed products of Rheum officinale. METHODS： RP-HPLC method was established. The determination was performed on Thermo ScientificTM Hypersil GOLD Dim column with mobile phase consisted of methanol-0.1％ phosphoric acid solution （gradient elution） at the flow rate of 1.0 mL/min. The detection wavelength was set at 278 nm， and the column temperature was 30 ℃. The sample size was 10 μL. RESULTS： The linear range of gallic acid， cinnamic acid and catechin were 0.126 2-1.262 0 μg（r＝0.999 9）， 0.036 2-0.362 0 μg（r＝0.999 9） and 0.177 9-1.779 4 μg（r＝0.999 8）， respectively. Quantitative limits were 25.4， 28.2， 62.5 ng， and detection limits were 6.2， 3.6， 11.8 ng， respectively. RSDs of precision， stability， repeatability and durability tests were all less than 3％. The recoveries ranged from 94.64％-102.71％（RSD＝2.74％， n＝9）， 95.35％-102.49％（RSD＝2.44％， n＝9）， 93.56％-103.66％（RSD＝3.27％， n＝9）. The determination results showed that the contents of gallic acid and cinnamic acid in prepared R. officinale were higher， and the order of both were prepared R. officinale＞steamed R. officinale＞raw R. officinale. The content of catechin in raw R. officinale was higher， and the order of it was raw R. officinale＞ steamed R. officinale＞prepared R. officinale. CONCLUSIONS： The method is sensitive， reliable and reproducible. It can be used to determine the contents of gallic acid， cinnamic acid and catechins in 3 processed products of R. officinale simultaneously.
ABSTRACT
The chemical constituents from methanol extract of Dichroa hirsuta were separated by silica gel and Sephadex LH-20 column chromatography,high pressure preparative liquid chromatography( HPLC) and recrystallization. Their structures were elucidated by NMR and MS. Nine compounds were obtained and their structures were identified as 3β,21α-O-diacetyl-lup-9( 11)-en-7β-ol( 1),( Z)-methyl p-hydroxycinnamate( 2),cis-p-coumaric acid ethyl ester( 3),( E)-methyl p-hydroxycinnamate( 4),trans-p-coumaric acid ethyl ester( 5),4( 3 H)-quinazolinone( 6),7-hydroxycoumarin( 7),hydrangenol( 8) and thunberginol C( 9). Compound 1 is a new lupane-type triterpenoid,and compounds 1-5,8-9 were firstly isolated from this plant. Dual reporter assay results showed that compounds 2-5 could activate the Nrf2-ARE signaling pathway.
Subject(s)
Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Hydrangea , Chemistry , Phytochemicals , Pharmacology , Triterpenes , PharmacologyABSTRACT
Abstract INTRODUCTION Leishmaniasis, Chagas disease, and malaria cause morbidity globally. The drugs currently used for treatment have limitations. Activity of cinnamic acid analogs against Leishmania spp., Trypanosoma cruzi, and Plasmodium falciparum was evaluated in the interest of identifying new antiprotozoal compounds. METHODS In vitro effects of analogs against L. braziliensis, L. infantum chagasi, T. cruzi, and P. falciparum, and hemolytic and cytotoxic activities on NCTC 929 were determined. RESULTS Three analogs showed leishmanicidal and tripanocidal activity. No antiplasmodial, hemolytic, or cytotoxic activity was observed. CONCLUSIONS Antiprotozoal activity of analogs against L. infantum braziliensis, L. infantum chagasi, and T. cruzi was demonstrated.
Subject(s)
Plasmodium falciparum/drug effects , Trypanosoma cruzi/drug effects , Cinnamates/pharmacology , Leishmania/drug effects , Antiprotozoal Agents/pharmacology , Cinnamates/chemistry , Parasitic Sensitivity Tests , Antiprotozoal Agents/chemistryABSTRACT
In order to investigate the effect of various production processes on the quality of Safflower Injection, the biological activities of the intermediates were evaluated by measuring activated partial thromboplastin time (APTT) and adenosine diphosphate (ADP) induced platelet aggregation in vitro. Intermediates were produced by key processes, such as extraction, concentration, twice alcohol precipitation, water sedimentation and two sterilizations during the production of Safflower Injection. The content of main chemical components in intermediates was determined by HPLC. The results showed that with the advance of the preparation process of Safflower Injection, the inhibition of ADP-induced platelet aggregation rate of each intermediate decreased gradually, and the trend of extending APTT activity decreased first and then increased. Meanwhile, the content of hydroxy safflor yellow A (HSYA) was gradually lowered, the content of p-hydroxy-cinnamic acid was increased, and new chemical component p-hydroxybenzaldehyde was produced. In conclusion, sterilization played a key role in the biological activity and HSYA content of Safflower injection.
Subject(s)
Carthamus tinctorius , Chalcone , Chromatography, High Pressure Liquid , Partial Thromboplastin Time , Platelet AggregationABSTRACT
Objective To establish a quantitative analysis of multi-components with a single-marker (QAMS) method for the simultaneous determination of oxypaeoniflorin, albiflorin, paeoniflorin, benzoylpaeoniflorin, cinnamic acid, cinnamaldehyde, saikosaponin a, and saikosaponin d in Guishao Zhenxian Tablets (GZT). Methods The separation was performed on a Thermo ODS C18 column (250 mm × 4.6 mm, 5 μm), with the mobile phase consisting of acetonitrile-0.1% phosphate acid solution for gradient elution. The column temperature was 25 ℃, and flow rate was 1.1 mL/min. Using paeoniflorin as internal reference substance, the relative correlation factors of oxypaeoniflorin, albiflorin, benzoylpaeoniflorin, cinnamic acid, cinnamaldehyde, saikosaponin a, and saikosaponin d were calculated and established by HPLC. The results were compared with those obtained by the external standard method to verify the rationality, feasibility, and repeatability of QAMS method. Results Oxypaeoniflorin, albiflorin, paeoniflorin, benzoylpaeoniflorin, cinnamic acid, cinnamaldehyde, saikosaponin a, and saikosaponin d had good relations within the ranges of 2.63-65.75 μg/mL (r = 0.999 7), 9.67-241.75 μg/mL (r = 0.999 8), 13.59-339.75 μg/mL (r = 0.999 5), 1.79-44.75 μg/mL (r = 0.999 4), 2.45-61.25 μg/mL (r = 0.999 1), 7.98-199.50 μg/mL (r = 0.999 7), 2.79-69.75 μg/mL (r = 0.999 3), and 2.51-62.75 μg/mL ( r= 0.999 5), respectively. The recovery rates were 98.64%, 99.33%, 100.02%, 97.42%, 96.95%, 98.75%, 98.21%, and 97.81%, RSDs were 0.89%, 1.19%, 1.00%, 1.33%, 1.51%, 0.99%, 1.43%, and 0.80%, respectively. The relative correlation factors values of oxypaeoniflorin, albiflorin, benzoylpaeoniflorin, cinnamic acid, cinnamaldehyde, saikosaponin a, and saikosaponin d to paeoniflorin were 0.520 9, 1.086 9, 0.476 8, 0.626 1, 0.802 1, 0.713 8, and 0.367 0, respectively. There were no significant difference in assay results between QAMS and the external standard method. Conclusion The QAMS method is feasible and credible, and could be used to determine oxypaeoniflorin, albiflorin, paeoniflorin, benzoylpaeoniflorin, cinnamic acid, cinnamaldehyde, saikosaponin a, and saikosaponin d in Guishao Zhenxian Tablets for the quality control.
ABSTRACT
Objective To establish a measurement method for the content of five compounds (acteoside, harpagide, harpagoside, angoroside-C, and cinnamic acid) in Scrophularia Radix quantitative analysis multi-components by single-marker (QAMS), and verify the accuracy and feasibility of QAMS in the quality control. Methods Taking harpagide as internal standard substance, the relative correlation factor (RCF) of acteoside, cinnamic acid, harpagoside, and angoroside C was established. And the content of each component in Scrophularia Radix was determined by the above-mentioned RCF. In order to prove the scientificity and feasibility of this method, the results were compared with the external standard method. Results The relative correction factors of acteoside, cinnamic acid, harpagoside, and angoroside-C were 0.068 (RSD = 0.53%), 0.060 (RSD = 0.81%), 0.142 (RSD = 1.17%), 0.197 (RSD = 1.82%). No significant differences were found among the quantitative results of four components in 25 batches of Scrophularia Radix determined by the two methods. Conclusion It is feasible and accurate to evaluate the quality of Scrophularia Radix by QAMS.
ABSTRACT
AIM To prepare Guizhi Fuling transdermal patch.METHODS With kinds of pressure-sensitive adhesive and penetration enhancer,kind and consumption of solvent,drug loading as influencing factors,appearance,formability and viscidity of patch,extract dispersion as evaluation indices,single factor test was applied to optimizing the preparation.And subsequent in vitro transdermal absorption test was performed to investigate the steady-state permeation rates of paeoniflorin,cinnamic acid and paeonol onto rat skins.RESULTS The optimal conditions were determined to be Duro-Tak 87-2677 polyacrylate pressure-sensitive adhesive (matrix),1 ∶ 0.5 for ratio of extract to propanediol (solvent),3％ azone as a penetration enhancer,and 20％ for drug loading,the obtained transdermal patch demonstrated both ideal initial adhesion force and holding adhesion force.These three constituents' average transdermal rates were 34.32,1.684,72.90 μg/(cm2 · h) with the average release rates of 26.81,1.523,111.8 μg/(cm2 · h),respectively,whose in vitro transdermal permeation curves conformed to Higuchi equation.CONCLUSION Guizhi Fuling transdermal patch processed with simple and stable preparation technique exhibits good in vitro transdermal permeation performance.
ABSTRACT
AIM To establish an HPLC method for the simultaneous content determination of six constituents in Xuanmai Ganju Granules (Scrophulariae Radix,Ophiopogonis Radix,Glycyrrhizae Radix et Rhizoma,Platycodonis Radix).METHODS The analysis of 80％ methanol extract of this drug was performed on a 35 ℃ thermostatic ZORBAX SB-C18 column (4.6 mm × 250 mm,5 μm),with the mobile phase comprising of acetonitrile0.1％ phosphoric acid flowing at 1.0 mL/min in a gradient elution manner,and the detection wavelengths were set at 210,250,278 nm.RESULTS Harpagide,liquiritin apioside,liquiritin,harpagoside,cinnamic acid and glycyrrhizic acid showed good linear relationships within the ranges of 2.177-43.539 μg/mL(r =0.999 6),1.713-34.261 μg/mL (r =0.999 5),1.946-38.916 μg/mL(r =0.999 6),2.070-41.395 μg/mL(r =0.999 7),2.06-41.2 pg/mL (r =0.999 6) and 3.623-72.454 μg/mL (r =0.999 6),whose average recoveries (RS-Ds) were96.08％ (2.1％),95.55％ (2.5％),95.04％ (2.6％),94.86％ (2.7％),95.70％ (1.9％) and 95.47％ (1.9％),respectively.CONCLUSION This simple and accurate method can be used for the quality control of Xuanmai Ganju Granules.