Determination of eight active components of Bufei Huoxue Capsules in rat plasma and their pharmacokinetics by UHPLC-MS/MS / 中国中药杂志

An ultra-high performance liquid chromatography-tandem mass spectrometry(UHPLC-MS/MS) method was established to investigate the pharmacokinetic behaviors of psoralenoside, isopsoralenoside, calycosin-7-glucoside, ononin, psoralen, isopsoralen, methylnissolin, and neobavaisoflavone in rat plasma after oral administration of Bufei Huoxue Capsules. After SD rats were administered with Bufei Huoxue Capsules suspension by gavage, blood samples were collected from the inner canthus at different time points. After protein precipitation, plasma samples were separated on ACQUITY UPLC BEH C_(18) column(2.1 mm×100 mm, 1.7 μm). The mobile phase consisted of acetonitrile(A) and water(B) containing 0.1% formic acid in gradient elution. The positive and negative ions were measured simultaneously in the multi-reaction monitoring(MRM) mode. The pharmacokinetic parameters were calculated and fitted by DAS 3.2.8. Psoralenoside, isopsoralenoside, calycosin-7-glucoside, ononin, psoralen, isopsoralen, methylnissolin, and neobavaisoflavone were detected in the rat plasma after drug administration, with AUC_(0-t) of(3 357±1 348),(3 555±1 696),(3.03±0.88),(2.21±0.33),(1 787±522),(2 295±539),(5.69±1.41) and(3.40±0.75) μg·L~(-1)·h, and T_(max) of(1.56±0.62),(1.40±0.70),(0.21±0.05),(0.25±0.12),(0.26±0.11),(0.34±0.29),(0.74±0.59), and 0.25 h. The method is proved specific and repeatable and is suitable for the determination of psoralenoside, isopsoralenoside, calycosin-7-glucoside, ononin, pso-ralen, isopsoralen, methylnissolin, and neobavaisoflavone in the rat plasma, which can be applied to pharmacokinetic study.

Mechanism of Olibanum-Myrrha in treatment of rheumatoid arthritis based on network pharmacology and molecular docking / 中国中药杂志

In this paper, network pharmacology method and molecular docking technique were used to investigate the target genes of Olibanum and Myrrha compatibility and the possible mechanism of action in the treatment of rheumatoid arthritis(RA). Our team obtained the main active components of Olibanum-Myrrha based on literatures study, relevant traditional Chinese medicine systematic pharmacological databases and literature retrieval, and made target prediction of the active components through SwissTargetPrediction database. At the same time, RA-related targets were collected through DrugBank, GeneCards and Therapeutic Target Database(TDD) databases; and VENNY 2.1 was use to collect intersection targets to map common targets of drug and disease of Venn diagram online. The team used STRING database to construct PPI protein interaction network diagram, and screen out core targets according to the size of the interaction, and Cytoscape 3.6.0 software was used to construct network models of "traditional Chinese medicine-component-target" "traditional Chinese medicine-component-target-disease" and core target interaction network model. The intersection target was analyzed by using DAVID 6.8 online database for GO function analysis and KEGG pathway enrichment analysis, and Pathon was used to visualization. AutoDock Vina and Pymol were used to connect the core active components with the core targets. Sixteen active components of Olibanum-Myrrha pairs were found and collected in the laboratory, and 320 relevant potential targets, 468 RA-related targets and 62 intersection targets were obtained through the Venn diagram. It mainly acted on multiple targets, such as IL6, TNF, IL1 B and MAPK1, involving TNF signaling pathway and Toll-like receptor signaling pathway in RA treatment. Finally, in this study, possible targets and signaling pathways of Olibanum-Myrrha compatibility therapy for RA were discussed, and molecular docking between core targets and core active components was conducted, which could provide scientific basis for the study on the mechanism of Olibanum-Myrrha compatibility.

[Identification of metabolites of Zhali Nusi Prescription in rat plasma, bile, urine and feces after oral administration].

This study was designed to determine the metabolites of Zhali Nusi Prescription(ZLNSP) in rats. The ultra-high performance liquid chromatography-LTQ Orbitrap mass spectrometric(UHPLC-LTQ-Orbitrap-MS) and mass defect filter techniques were applied to analyze the metabolites of ZLNSP in rat plasma, bile, urine and feces. The biological samples were analyzed by ACQUITY UPLC BEH T_3 column(2.1 mm×100 mm,1.7 µm), with 0.1% formic acid water(A)-acetonitrile(B) as mobile phase, and the biological samples were analyzed in negative ion mode by electrospray ionization mass spectrometry(ESI-MS). An analytical method for biological samples of rats was established, and 8 prototype components and 36 metabolites were identified. The results showed that the metabolic pathways of the main components of ZLNSP in rats included methylation, glucuronidation, sulfation and so on. It provi-ded information for the therapeutic effect of ZLNSP in vivo.

Research thoughts and methods on grading identification and transmission change law of traditional Chinese medicine(TCM) Q-marker / 中国中药杂志

The quality marker( Q-maker) of traditional Chinese medicine( TCM) has been the core concept of TCM quality evaluation and control in recent years. Based on the knowledge and long-term practice of the researches on TCM quality,we put forward that " Taking the effectiveness as the core,the measurability and peculiarity as necessary conditions,and considering compatibility for TCM formulae,TCM Q-makers are selected and confirmed,and then the transmission and traceability should be investigated as its functional attributes". Selecting the commonly used representative TCM as the research object,based on the score of TCM effectiveness,measurability and peculiarity,a layered three-dimensional integrated technology was adopted for the quantitative evaluation and grading identification of the Q-markers for TCM. And after Q-markers for TCM are selected and confirmed,the transmission variation of the Q-markers is studied in the whole process from the formation of TCM to its function representation. Based on TCM chemical and biological characteristics as well as effectiveness,and integrating multidisciplinary techniques and methods,researches on innovative methods for system identification and confirmation of the TCM Q-makers are developed emphatically to form representative and exemplary extensive application,which will provide significant theoretical and methodological support for effectively improving the quality control level of TCM.

Modern research approaches and strategies for compatibility effects and efficacy components of herbal pairs / 药学学报

The herb pair is the simple and exquisite experience summary accumulated by generations of traditional Chinese medicine (TCM) experts in the process of long-term herbal prescription for curing diseases. Although it is only a combination of two herbs, it is cleverly matched and properly proportioned, which can well interpret TCM characteristics of "great combination and artful application". Moreover, the herb pair is an intermediate point between single herb and several TCM formulae, which implicates certain regularity and some connotation of many TCM formulae for diagnosis and treatment based on an overall analysis of the illness and the patient's condition. Our team has long been focusing on the complexity of drug interactions and the diversity of TCM components to carry out systematic research on herb pair by using modern scientific and technological knowledge and approaches. As results, a series of modern research approaches and strategies formed for the compatibility effect and bio-active components of the herb pair. By representing the principles and application characteristics of these approaches, this paper provides important support for elucidating scientific connotation of compatibility regularity of herb pairs and application of formulae optimization, as well as explorative ideas and approaches for modern research on other herb pairs.

Characterization of molecular signature of the roots of Paeonia lactiflora during growth / 中国天然药物

The roots of Paeoniae lactiflora Pall. are widely consumed as crude drugs in Asian countries due to their remarkable beneficial health effects. The present research was undertaken to illuminate the dynamic changes in metabolites and enzymes and facilitate selection of the harvesting time when the herb can provide optimum health benefits. P. lactiflora roots were analyzed at 12 stages of growth for monoterpenoid glycosides, phenols, nucleosides, nucleobases, amino acids, and polysaccharides by high-performance liquid chromatography with photodiode array detector, ultra-high pressure liquid chromatography coupled with tandem mass spectrometry, and UV spectrophotometry. The enzyme activities of plant β-glucosidases and esterases were determined by UV methods. The total content of monoterpenoid glycosides and phenols peaked in December. For nucleosides and nucleobases, the highest content appeared in April. The maximum phasic accumulation of the total amino acids took place in March, and the content of total polysaccharides reached a peak value in September. December, April, and March were selected as the appropriate harvesting times for producing natural medicinal or health food products. Plant β-glucosidases and esterases showed the highest activity in December and May, respectively. When the activity of β-glucosidase increased, esterase activity decreased, while the contents of oxypaeoniflora and paeoniflorin increased. When esterase activity increased, the contents of benzoylpaeoniflorin, paeoniflorin, and gallic acid decreased. In conclusion, the results from the present study would be useful in determination of the suitable time for harvesting P. lactiflora roots for medicinal purposes.

Analysis and identification of water soluble components of water buffalo horn / 药学学报

This study is to analyze and identify the water soluble components of water buffalo horn (Bubali Cornu, WBH), and also establish a method for investigating these components. Shotgun proteomic analysis identified proteins in WBH aqueous extraction: keratin, collagen, desmoglein, etc. Ultrafiltration and LC-MS/MS were used to separate and identify the peptides in WBH aqueous extract, as a result, identified peptides were mainly derived from nonspecific degradation products of keratin and collagen, which including C-terminal peptides and non C-terminal peptides. Hypoxanthine, uridine, guanosine, and adenosine were identified by comparing with the standards. The strategy in present study could be used in analyzing water soluble components of animal horn derived TCM. It provides a reference for investigation of the material basis of animal horn derived TCM.

Study on incompatibility of traditional Chinese medicines / 中国中药杂志

The incompatibility of traditional Chinese medicines is related to the clinical medication safety, so has attracted wide attentions from the public. With the deepening of studies on the incompatibility of traditional Chinese medicines represented by 18 incompatible herbs, the incompatibility of theory traditional Chinese medicines has raised to new heights. From the origin of incompatibility theory of traditional Chinese medicines, relationship of herbs, harms of incompatible herbs and principle of prevention to toxic effects of specific incompatible medicines, the innovation and development of the traditional Chinese medicine incompatibility theory was explored. Structurally, the incompatibility of traditional Chinese medicines refers to the opposition of two herbs based on seven emotions and clinical experience. The combination of incompatible herbs may lead to human harms, especially latent harm and inefficacy of intervention medicines. The avoidance of the combination of incompatible herbs and the consideration of both symptoms and drug efficacy are the basic method to prevent adverse reactions. The recent studies have revealed five characteristics of incompatible herbs. Toxicity potentiation, toxication, efficacy reduction and inefficacy are the four manifestations of the incompatible relations. The material changes can reflect the effects of toxicity potentiation and toxication of opposite herbs. The accumulation of toxicity and metabolic changes are the basis for latent harms. The antagonistic effect of main efficacies and the coexistence of positive and negative effects are the distinctive part of the incompatibility. The connotation of incompatible herbs plays an important role in the innovation of the traditional Chinese medicine incompatibility theory.

Study on material base of Carthamus tinctorius with antioxidant effect based on selective knock-out / 中国中药杂志

<p><b>OBJECTIVE</b>To establish a method for studying efficacious materials of traditional Chinese medicines from an overall perspective.</p><p><b>METHOD</b>Carthamus tinctorius was taken the example. Its major components were depleted by preparing liquid chromatography. Afterwards, the samples with major components depleted were evaluated for their antioxidant effect, so as to compare and analyze the major efficacious materials of C. tinctorius with antioxidant activity and the contributions.</p><p><b>RESULT</b>Seven major components were depleted from C. tinctorius samples, and six of them were identified with MS data and control comparison. After all of the samples including depleted materials are compared and evaluated for their antioxidant effect, the findings showed that hydroxysafflor yellow A, anhydrosafflor yellow B and 6-hydroxykaempferol-3, 6-di-O-glucoside-7-O-glucuronide were the major efficacious materials.</p><p><b>CONCLUSION</b>This study explored a novel and effective method for studying efficacious materials of traditional Chinese medicines. Through this method, we could explain the direct and indirect contributions of different components to the efficacy of traditional Chinese medicines, and make the efficacious material expression of traditional Chinese medicines clearer.</p>

Comparative analysis of the promoting blood effects of the combination of different proportions of danggui and honghua by the principal component analysis and multi-attribute comprehensive index methods / 药学学报

The combination of Danggui and Honghua (GH) is a popular herb pair commonly used in clinic for the treatment of blood stasis syndrome in China. To evaluate the activating blood circulation and dissipating blood stasis effects of the combination of different proportions of Danggui and Honghua on acute blood stasis rats, and optimize the proportion of GH to have the best activating blood circulation and dissipating blood stasis effect. Acute blood stasis rat model was induced by subcutaneous injection of adrenaline and ice water bath. The blood stasis rats were administrated intragastrically with GH (1 : 0, 4 : 1, 2 : 1, 3 : 2, 1 : 1, 2 : 3, 1: 2, 1 : 4 and 0 : 1) extracts. The whole blood viscosity (WBV), plasma viscosity (PV), and high shear whole blood relative index (HSWBRI), low shear whole blood relative index (LSWBRI), and erythrocyte aggregation index (EAI) were tested to observe the effects of GH on hemorheology of blood stasis rats. And the maximum aggregation induced by adenosine diphosphate (ADP) was tested to observe the effect of GH on platelet aggregation index of blood stasis rats. In addition, the prothrombin time (PT), thrombin time (TT), activated partial thromboplastin time (APTT) and plasma fibrinogen (FIB) were tested to observe the effects of GH on blood coagulation function of blood stasis rats. Then principal component analysis and multi-attribute comprehensive index methods were both used to comprehensively evaluate the total activating blood circulation and dissipating blood stasis effects of GH. The results showed that the hemorheological indexes and coagulation parameters of model group both had significant differences with normal group. Compared with model group, GH (1 : 0, 4 : 1, 2: 1, 3 : 2, 1 : 1, 2 : 3, 1 : 2, 1 : 4 and 0 : 1) could improve all the blood hemorheology indexes and regulate part indexes of blood coagulation function and platelet aggregation in acute blood stasis rats. Based on principal component analysis and multi-attribute comprehensive index methods, GH 1 : 1 and GH 3 : 2 both had the best effect of blood circulation and dissipating blood stasis, and the effect of GH 1 : 1 was slightly better than GH 3 : 2. These results suggest that GH could obviously ameliorate the abnormality of hemorheology and blood coagulation function in acute blood stasis rats. The optimized proportion of GH was consistent with regulations of medicine usage that GH 1 : 1 had the highest frequency used in traditional Chinese formulae. It could provide scientific basis for more effective application of the compatibility between Danggui and Honghua in modern clinic medicine.

Quercetin-3-O-β-D-glucopyranosyl-(4→1)-α-L-rhamnoside metabolites in the rat using UPLC-Q-TOF/MS / 中国天然药物

Ultraperformance liquid chromatography/quadrupole-time-of-flight mass spectrometry (UPLC-Q-TOF/MS) and the Metabolynx™ software, combined with mass defect filtering, were applied to identity the metabolites of quercetin-3-O-β-D-gluco-pyranosyl-(4→1)-α-L-rhamnoside (QGR) in rats after intravenous administration. MS(E) was used for simultaneous acquisition of precursor ion information and fragment ion data at high and low collision energy in one analytical run, which facilitated the rapid structural characterization of eight metabolites in rat plasma, urine and bile. The results indicated that methylation and glucuronidation were the major metabolic pathways of QGR in vivo. The present study provided important information about the metabolism of QGR which will be useful for fully understanding the mechanism of action of this compound. Furthermore, this work demonstrated the potential of the UPLC-Q-TOF/MS approach using Metabolynx for rapid and automated research of the metabolites of natural products.

Metabolomic study of the action mechanism of nourishing blood effect of fo-shou-san on blood deficiency mice / 药学学报

The metabolic effect of Fo-Shou-San on blood deficiency mice was studied by using metabolomic method. UPLC-QTOF/MS was used to analyze the plasma metabolome in blood deficiency mice. MS data were processed by MarkerLynx software. With multivariate statistical analysis of plasma metabolite profiles, a clear separation among control, blood deficiency model, and Fo-Shou-San groups was achieved. Potential biomarkers were selected according to the parameters of variable importance in the projection (VIP) and identified according to MS information and database retrieval. The metabolic network of blood deficiency was predicted via MetPA database. Twenty-two potential biomarkers were identified and used to explain the thiamine metabolism, arachidonic acid metabolism, sphingolipid metabolism, glyoxylate and dicarboxylate metabolism, histidine metabolism, nicotinate and nicotinamide metabolism, cysteine and methionine metabolism, tryptophan metabolism, starch and sucrose metabolism, tyrosine metabolism and citrate cycle (TCA cycle). Those metabolic pathways were disturbed in blood deficiency mice, but which could be regulated nearly to normal state after Fo-Shou-San administration. In this study, the metabolomics of blood deficiency mice and the action mechanism of nourishing blood effect of Fo-Shou-San were evaluated. The physiological and metabolic state of the organism could be represented comprehensively by using metabolomics. And metabolomics can be used to evaluate the pharmacodynamics and related mechanisms of Chinese medicine and formulae.

Study on antioxidant interaction of different preparations and proportions of Danggui-Chuanxiong drug pair / 中国中药杂志

<p><b>OBJECTIVE</b>To observe the in vitro antioxidant interaction of different preparations and proportions of Danggui-Chuanxiong drug pair in the DPPH free radical scavenging rate with the response surface methodology.</p><p><b>METHOD</b>The 2,2-diphenyl-1-picryl-hydrazyl (DPPH) free radical scavenging rate method was adopted for determining the antioxidant activity of extracts from Danggui-Chuanxiong with 10 proportions and three extraction processes. The response surface methodology was used to determine the parameters of the dose-effect curve and establish a three-dimensional response surface model. The three-dimensional response surface graph was constructed with Matlab software.</p><p><b>RESULT</b>All of the 30 samples with different proportions and preparations had antioxidant effect in scavenging free radicals and a remarkable dose-effect relationship. Their water extracts had a narrow synergistic range, with only spot distribution. Their antagonist ranges were districted in six bands of various widths. The synergistic ranges of ethanol extracts were districted in small bands, with the antagonist ranges scattered in points. The synergistic ranges of their water-alcohol extracts were distributed in three bands, with their antagonist ranges scattered in points. In short, the water-alcohol extracts showed a wider synergistic range than ethanol extracts, followed by water-extracts. All of the three extraction processes showed no obvious synergistic and antagonist effects.</p><p><b>CONCLUSION</b>The quantitative study on the interaction of traditional Chinese medicines with different compatibilities with the response surface methodology provides reference of thoughts and methods for relevant studies.</p>

Change in dissolution of chemical components of frankincense-myrrh before and after their compatibility and effect on no release of LPS-induced macrophage cells / 中国中药杂志

<p><b>OBJECTIVE</b>To analyze the difference of chemical compounds of frankincense-myrrh before and after their compatibility, and evaluate the effect of differentiated compounds on NO generated by LPS-induced peritoneal macrophage cells in rats, in order to discuss synergetic material basis of frankincense-myrrh compatibility from the prospective of change in chemical constituents.</p><p><b>METHOD</b>UPLC-Q-TOF-MS/MS combined technology was used to analyze the chemical components of frankincense-myrrh before and after their compatibility. MarkerLynx 4. 1 statistical software was used to analyze differentiated compounds before and after their compatibility.</p><p><b>RESULT</b>The results of PCA showed that there were significant differences in the combined extracts of frankincense-myrrh and the chromatogram of their combined liquid, suggesting significant differences in their chemical compounds before and after their compatibility; after their compatibility, the dissolution of pentacyclic triterpenoid (alpha-boswellic acid, beta-boswellic acid) and tetracyclic triterpenoid (elemonic acid, 3-acetoxy-16-hydroxy-dammar-24-ene, 3-hydroxytirucalla-8,24-dien-21-oic acid or 3-hydroxytirucalla-7,24-dien-21-oic acid) increased notably, while the dissolution of both yclic sesquiterpenes and macrocyclic diterpenoids decreased. According to the evaluation on in vitro activity, 2-methoxy-8, 12-epoxy-germa-1 (10), 7, 11-triene-6-ketone, 2-methoxy-5-acetoxyl-furan-germa-1 (10)-alkene-6-ketone and 3-carbonyl Euphorbia kansui-8, 24-diene-21-carboxylic acid notably inhibited NO generated by LPS-induced peritoneal macrophage cells in rats.</p><p><b>CONCLUSION</b>These findings provide scientific basis and reference for studies on anti-inflammatory material basis of frankincense-myrrh compatibility.</p>

Evaluate activating blood circulation and dissipating blood stasis effect mechanism of foshousan on acute blood stasis rats on basis of metabolomic approach / 中国中药杂志

Ice water bath and subcutaneous injection of adrenaline were used to establish the acute blood stasis model of rats. Ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS) was used to study the urine metabolic changes of acute blood stasis rats. Potential biomarkers were selected by variable importance projection, and identified on basis of MS information and databases. The metabolic pathways were predicted via MetPA database. To study the effect of Foshousan on endogenous metabolites of acute blood stasis model rats, find potential biomarkers, and explore the effect mechanism of Foshousan on activating blood circulation and dissipating blood stasis. Eleven potential biomarkers were identified with multivariate statistical analysis of urine metabolite profiles, and which also were used to explain the phenylalanine metabolism, tryptophan metabolism and sphingolipid metabolism. Those disturbed metabolic pathways in acute blood stasis rats could be regulated closely to normal state after Foshousan administration. Metabolomics has a bright prospect in the efficacy evaluation and effect mechanism elucidation of the traditional Chinese medicines.

Research on nourishing and tonifying blood effects of the herb pair consisting of Angelica sinensis and Ligusticum chuanxiong on the basis of drug interaction / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To study the pharmacodynamic interaction of nourishing and tonifying blood effects of the herb pair consisting of Angelica sinensis and Ligusticum chuanxiong by response surface method.</p><p><b>METHODS</b>The blood deficiency rat model was induced by injecting N-acetylphenylhydrazine and cyclophosphamide. The effects of Angelica sinensis and Ligusticum chuanxiong in different proportions (0:1, 1:5, 2:5, 2:3, 1:1, 3:2, 5:2, 5:1, and 1:0) and at different concentrations on the peripheral blood index and the organ indices were observed. Then all indices were integrated to the total nourishing effect value by comprehensive index method. The interaction was analyzed by response surface method. The model parameters were estimated with nonlinear regression. The three-dimensional response surfaces were constructed with Matlab Software.</p><p><b>RESULTS</b>In the response surface, most compatibility of Angelica sinensis and Ligusticum chuanxiong showed synergistic action, some showed addition action, and few of them showed obvious antagonist action. The proportion of Angelica sinensis and Ligusticum chuanxiong from 4:1 to 2:1 and the dose of Angelica sinensis and Ligusticum chuanxiong from low to high showed addition action, while the other proportions showed obvious addition action at low dose and synergistic action at high dose.</p><p><b>CONCLUSIONS</b>The research results could provide scientific evidence for reasonable application of Angelica sinensis and Ligusticum chuanxiong in clinics of Chinese medicine. The quantitative analysis on drug interactions of herbal compatibility by response surface method could provide reference for relative studies.</p>

Study on Chinese medicine pairs (V)--Their modern research strategies and approaches / 中国中药杂志

Along with progress of modern science and technology, human is utilizing natural resources and their inherent law more effectively and more efficiently according to their own purposes. Chinese medicine pair (CMP) is relatively fixed combination of two TCMs which was proven to be effective in clinical application. CMP has its inner specification, and it is an intermediate point between single herb and many TCM formulae. With the aid of modern science and technology, and by means of choosing appropriate strategies and approaches, the compatibility rules of CMP might be revealed, which will be significant to develop the compatibility theory of TCM formulae and create modern TCM new drugs.

Research on Chinese medicine pairs (II)--Their data mining / 中国中药杂志

Data mining technology has become a powerful tool in traditional Chinese medicine (TCM) research. In this paper, based on the principle and basic requirements of data mining, the mining methods and procedures were described. And then the application of data mining technology in Chinese medicine pair research was classified and summarized, such as the compatibility characters, characteristic pairs, dosage-effect relationship and property compatibility, which provide the direction and data base for modern research of Chinese medicine pair.

In vitro transdermal delivery of the active fraction of xiangfusiwu decoction based on principal component analysis / 药学学报

The objective of the present study was to establish a method based on principal component analysis (PCA) for the study of transdermal delivery of multiple components in Chinese medicine, and to choose the best penetration enhancers for the active fraction of Xiangfusiwu decoction (BW) with this method. Improved Franz diffusion cells with isolated rat abdomen skins were carried out to experiment on the transdermal delivery of six active components, including ferulic acid, paeoniflorin, albiflorin, protopine, tetrahydropalmatine and tetrahydrocolumbamine. The concentrations of these components were determined by LC-MS/MS, then the total factor scores of the concentrations at different times were calculated using PCA and were employed instead of the concentrations to compute the cumulative amounts and steady fluxes, the latter of which were considered as the indexes for optimizing penetration enhancers. The results showed that compared to the control group, the steady fluxes of the other groups increased significantly and furthermore, 4% azone with 1% propylene glycol manifested the best effect. The six components could penetrate through skin well under the action of penetration enhancers. The method established in this study has been proved to be suitable for the study of transdermal delivery of multiple components, and it provided a scientific basis for preparation research of Xiangfusiwu decoction and moreover, it could be a reference for Chinese medicine research.

Evaluation study on integration effect of taohong siwu tang in treating primary dysmenorrhea / 中国中药杂志

<p><b>OBJECTIVE</b>To evaluate the effect of Taohong Siwu Tang and its fractions on hotplate-induced pain in mice, acetic acid-induced writhing response, dysmenorrheal model and isolated uterine contraction in vitro in mice, and discuss material basis of effect sites.</p><p><b>METHOD</b>The samples of fractions were prepared by macroporous adsorptive resins (TH-1-TH-15). In the whole animal experiment, the hotplate-induced pain mice model was established to observe the effect of the samples on pain threshold in mice; the acetic acid-induced writhing response mice model was built to observe the effect of the samples on the writhing response in mice; the mice dysmenorrheal model was established to observe the effect of the samples on the writhing response, and calcium ion (Ca2+) and nitric oxide (NO) levels in uterine tissue of mice. In the isolated uterus contraction experiment, the oxytocin-induced isolated uterus contraction mice model was established to observe the effect of the samples on the isolated uterus contraction index. HPLC-DAD method was adopted for the content determination of effect sites.</p><p><b>RESULT</b>According to the evaluation of the integration geological effect, beside TH-2 and TH-4, other three active fractions (TH-9, TH-10 and TH-11) extracted from Taohong Siwu Tang are the main effect sites. Their chemical components were analyzed and identified as monoterpene glycosides, phthalides, organic acids, etc.</p><p><b>CONCLUSION</b>The effect sites of Taohong Siwu Tang on dysmenorrhea are TH-9, TH-10 and TH-11, which are 30% - 50% active fractions obtained from water-soluble small-molecular fractions by gradient elution using ethanol through macroporous absorption resin. Compared with TH-10 and TH-11, TH-9 shows stronger effect, which may be related to the type and content of chemical components it contains.</p>