Variation and interaction mechanism between active components in Rheum officinale and rhizosphere soil microorganisms under drought stress / 中国中药杂志

To explore the changes and the reaction mechanisms between soil microecological environment and the content of secon-dary metabolites of plants under water deficit, this study carried out a pot experiment on the 3-leaf stage seedlings of Rheum officinale to analyze their response mechanism under different drought gradients(normal water supply, mild, moderate, and severe drought). The results indicated that the content of flavonoids, phenols, terpenoids, and alkaloids in the root of R. officinale varied greatly under drought stresses. Under mild drought stress, the content of substances mentioned above was comparatively high, and the content of rutin, emodin, gallic acid, and(+)-catechin hydrate in the root significantly increased. The content of rutin, emodin, and gallic acid under severe drought stress was significantly lower than that under normal water supply. The number of species, Shannon diversity index, richness index, and Simpson index of bacteria in the rhizosphere soil were significantly higher than those in blank soil, and the number of microbial species and richness index decreased significantly with the aggravation of drought stresses. In the context of water deficit, Cyanophyta, Firmicutes, Actinobacteria, Chloroflexi, Gemmatimonadetes, Streptomyces, and Actinomyces were the dominant bacteria in the rhizosphere of R. officinale. The relative content of rutin and emodin in the root of R. officinale was positively correlated with the relative abundance of Cyanophyta and Firmicutes, and the relative content of(+)-catechin hydrate and(-)-epicatechin gallate was positively correlated with the relative abundance of Bacteroidetes and Firmicutes. In conclusion, appropriate drought stress can increase the content of secondary metabolites of R. officinale from physiological induction and the increase in the association with beneficial microbe.

Determination of 10 mycotoxins in Hippophae Fructus medicinal and edible products by ultra-performance liquid chromatography- tandem mass spectrometry / 中国中药杂志

An analytical method for 10 mycotoxins in Hippophae Fructus medicinal and edible products was established in this study, and the contamination of their mycotoxins was analyzed. First of all, the mixed reference solution of ten mycotoxins such as aflatoxin, ochratoxin, zearalenone, and dexoynivalenol was selected as the control, and the Hippophae Fructus medicinal and edible products were prepared. Secondly, based on the ultra-performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) technology, 10 mycotoxins in Hippophae Fructus medicinal and edible products were quantitatively investigated and their content was determined. Finally, the contamination of mycotoxins was analyzed and evaluated. The optimal analysis conditions were determined, and the methodological inspection results showed that the 10 mycotoxins established a good linear relationship(r>0.99). The method had good repeatability, test sample specificity, stability, and instrument precision. The average recovery rates of 10 mycotoxins in Hippophae Fructus medicinal products, edible solids, and edible liquids were 90.31%-109.4%, 87.86%-107.8%, and 85.61%-109.1%, respectively. Relative standard deviation(RSD) values were 0.22%-10%, 0.75%-13%, and 0.84%-8.5%, repsectively. Based on UPLC-MS/MS technology, the simultaneous determination method for the limits of 10 mycotoxins established in this study has fast detection speed, less matrix interference, high sensitivity, and accurate results, which is suitable for the limit examination of 10 mycoto-xins in Hippophae Fructus medicinal and edible products.

Mangiferin inhibited neuroinflammation through regulating microglial polarization and suppressing NF-κB, NLRP3 pathway / 中国天然药物

Inflammation plays important roles in the progress of neurodegenerative diseases, such as Parkinson's disease and Alzheimer's disease. Microglia is responsible for the homeostasis of the central nervous system (CNS), and involved in the neuroinflammation. Therefore, it could be potential in treatment of neurodegenerative diseases to suppress the microglia-mediated neuroinflammation. Mangiferin, a major glucoside of xanthone in Anemarrhena Rhizome, has anti-inflammatory, anti-diabetes, and anti-oxidative properties. However, the effect of mangiferin on the inflammatary responses of microglia cells are still poorly understand. In this study, we investigated the mechanism by which mangiferin inhibited inflammation in LPS-induced BV

Pre-formulation physicochemical properties of component-based Chinese medicine of Qinqi Fengshi Fang / 中国中药杂志

Pre-formulation physicochemical properties of the component-based Chinese medicine of Qinqi Fengshi Fang were investigated to provide a research basis for the design of the dosage form for component-based Chinese medicine of Qinqi Fengshi Fang. The macroporous resin adsorption and refining technology was used to prepare the total glycosides extract of Gentianae Macrophyllae Radix, Panacis Majoris Rhizome and Corni Fructus respectively in the prescription of Qinqi Fengshi Fang. Their physicochemical properties were investigated, including solubility, wettability, hygroscopicity, equilibrium solubility, oil-water partition coefficient, and stability. The results showed that the total glycosides of Gentianae Macrophyllae Radix, Panacis Majoris Rhizome and Corni Fructus all had good solubility and wettability. The solubility index of each total glycoside component was greater than 85%, and the water absorption index was greater than 50%. In the range of pH 2.0-7.4, the equilibrium solubility of three kinds of total glycosides all increased with the increase of pH, showing a consistent change trend of solubility. The hydrophilicity was also suitable and similar. Overall, three kinds of total glycosides showed good stability, but strong hygroscopicity. The degree of hygroscopicity was as follows: total glycosides of Gen-tianae Macrophyllae Radix > total glycosides of Corni Fructus > total glycosides of Panacis Majoris Rhizome. Therefore, the hygroscopi-city needed to be considered in the preparation of the component-based Chinese medicine of Qinqi Fengshi Fang. The excipients and packaging materials can be properly selected to reduce the hygroscopicity of the preparation. This study provides a reference for the dosage form design of the component-based Chinese medicine of Qinqi Fengshi Fang.

Responses of seed germination of Astragalus membranaceus to light and temperature conditions accompanied with drought and salt stresses / 中国中药杂志

We studied the seed germination of Astragalus membranaceus under PEG and Na Cl osmotic stress gradients( 0,-0. 1,-0. 3,-0. 5,-0. 7 MPa) respectively applied with light( continuous light,light 12 h/dark 12 h circulation and continuous dark) and temperature( constant 15 ℃,15 ℃ 12 h/30 ℃ 12 h circulation and constant 30 ℃) treatments. The results showed as following: ① Under the light and temperature interactive treatments,total germination percentage( TGP) was restrained by high temperature and continuous light also decreased TGP under high temperature. Mean germination time( MGT) was not changed by light mode. Root development was enhanced by dark and low temperature. Shoot development was enhanced by light and high temperature. Hypocotyl length was enhanced by dark and high temperature. ② Under the light and temperature interactive treatments combined respectively with PEG and NaCl stress conditions,although the inhibitions of seed germination and growth were gradually strengthened with the increases of osmotic stresses,slight osmotic stress can promote seed germination. Under the same osmotic potential,the effects of PEG on TGPs and MGTs were stronger than that of NaCl. As the temperature increase,the seeds may change from photo-neutrality to photo-phobia. Decreased TGP under drought and continuous light interactive treatment is an adaptation strategy to avoiding drought. Hypocotyl growth accelerated under continuous dark treatment is an ecological trait which could increase dry matter input in stem and height for more light. Seed development under high concentration of NaCl treatment is better than that of PEG treatment due to low water potential caused by Na~+,which can enter into seed coat and promote water absorption.

Preparation and quality standard of standard decoction of Scrophulariae Radix pieces / 中国中药杂志

The standard decoction of Chinese herbal decoction pieces is a standard reference substance to measure whether different dosage forms of Chinese medicine are basically consistent with those of clinical decoction,and provides new ideas and methods for effectively solving the problems of uneven quality in Chinese medicine dispensing granules. In this study,a systematic method for evaluating the quality of Scrophulariae Radix decoction was established from the perspective of " standard decoction",providing reference for the quality control of the Scrophulariae Radix dispensing granules. 15 batches of Scrophulariae Radix decoction pieces from different origins were collected,and 15 batches of standard decoctions were prepared according to the standardized process with water as solvent.Harpagide and harpagoside were used as quantitative detection indicators to determine the content,calculate the transfer rates and determine the extraction rate. The high performance liquid chromatography( HPLC) was used to establish a standard decoction fingerprint analysis method. The results showed that the transfer rates of harpagide and harpagoside in 15 batches of Scrophulariae Radix pieces standard decoction were( 70. 84±13. 39) % and( 48. 56±6. 40) % respectively; the extraction rate was( 57. 47±5. 89) %. Nine peaks were identified in the HPLC fingerprint,and the similarity was higher than 0. 97 between the fingerprints of 15 batches of standard decoction and the control fingerprint. In this study,the preparation process of standard decoction of Scrophulariae Radix pieces conformed to the traditional decoction preparation method. The sources of the samples were representative,and the established fingerprint method was stable and feasible,which can provide reference for the preparation and quality control of Scrophulariae Radix dispensing granules.

Quantitative determination of nine furanocoumarins for quality evaluation of Angelica dahurica from different habitats / 中国中药杂志

A UPLC method has been developed for simultaneous determination of nine furanocoumarins of Angelica dahurics,and was used for quality evaluation of A. dahurica from different habitats. ACQUITY UPLC BEH C18 chromatographic column was employed,the separation was performed with the mobile phase consisting of acetonitrile and water,and the detection wavelength was set at254 nm. This method was used to simultaneously determine the content of xanthotoxol,oxypeucedaninhydrate,byak-angelicin,psoralen,xanthotoxin,bergapten,oxypeucedanin,imperatorin and isoimperatorin in A. dahurica from different habitats. Then,the further quality assessment of the drug was carried out by similarity evaluation,cluster analysis( CA),principal component analysis( PCA),and orthogonal partial least squares discriminant analysis( OPLS-DA). The content order of measured furanocoumarins from high to low was: oxypeucedanin>imperatorin>isoimperatorin>oxypeucedaninhydrate>bergapten>byak-angelicin>xanthotoxin>xanthotoxol>psoralen,with the mean content 2. 844,1. 277,0. 649 2,0. 216 2,0. 129 8,0. 062 68,0. 052 68,0. 019 30,0. 018 19 mg·g-1,respectively. There were difference between the batches of the drug,and the quality was influenced by smouldering sulphur based on the results of chemical pattern recognition and content determination. Finally,six active ingredients were recognized as the quality makers using OPLS-DA method. The validated UPLC fingerprint combined with chemical pattern recognition method can be used in the quality control and evaluation of A. dahurica.

Programmed cell death induced by drought stress in sprout tumble of Pinellia ternata / 中国中药杂志

To further study the mechanism of sprout tumble caused by drought,drought stress was simulating with 30% PEG 6000,physiological,and then the morphological changes of Pinellia ternata cells at different treatment time were detected. The results indicated that,along with the period of drought stress continued,the contents of chlorophyll and water potential were decreased,relative electrical conductivity,contents of soluble sugar and MDA increased. Sprout tumble of P. ternata first occurred on the fourth day during drought stress,large scale of sprout tumble appeared on the eighth day with about 73% of tumble rate. The nuclei exposed to drought stress for 2 days were flattened,lobed,invalidated or irregular in shape and significant showed the apoptotic morphological characteristics. Adenylate transferase( ANT) gene expressions were inhibited by drought,with the rapid increase of Caspase-3 enzyme activity,the cell death rate increased. All this proves that the essence of sprout tumble caused by drought is programmed cell death,which may be a self dormancy protection mechanism of P. ternata against adverse environment.

Influence of ceftriaxone on pharmacokinetics, anticoagulation andantithrombotic effects of phenolic acids from Danhong injection in rats / 药学学报

Danhong injection (DHI) and ceftriaxone sodium were used in combination based on their experimental uses in clinic. This study was designed to investigate the impact of ceftriaxone on pharmacokinetics and pharmacodynamics of the phenolic acids from DHI. After administration of DHI for 7 d, ceftriaxone (CFTX) was combined with DHI for the next 7 d in adult male Sprague-Dawley (SD) rats. All the drugs were administered through caudal vein. UHPLC-TQ-MS was applied in determining the plasma concentration of p-coumaric acid (p-CA), salvianolic acid D (SaD), rosmarinic acid (RA) and salvianolic acid B (SaB). The pharmacokinetic parameters of the combination group or the Danhong injection alone group were calculated by statistical moment method, Cmax and the average of the area under the curve AUC0-t using 90% confidence interval of the bioequivalence and bioavailability degree module in DAS 3.2.8 statistic software. The results showed that Cmax of p-CA, SaD, RA and SaB were unqualified within 90% confidence intervals for bioequivalence statistics. And the results showed that AUC0-t of SaD, RA and SaB within 90% confidence intervals for bioequivalence statistics were unqualified. There were no significant difference in the tmax (P>0.05). The results of anticoagulation in vivo showed that the international normalized ratio (INR), prothrombin time (PT), thrombin time (TT) and activated partial thromboplastin time (APTT) were significantly increased when combined with CFTX (P<0.05 or P<0.01). The results in antithrombotic effects revealed that the thromboxane B2 (TXB2) level in serum was significantly decreased (P<0.01) in the combination group compared with Danhong injection alone. However, there was no significant difference in antiplatelet effects. These results suggest that CFTX may enhance the anticoagulation and antithrombotic effects of DHI through altering pharmacokinetics and pharmacodynamics in SD rats.

Effects of shading on key enzyme genesexpression and accumulation of saponins in Panax japonicus var. major / 中国中药杂志

To explore the effects of shading and the expression of key enzyme genes on the synthesis and accumulation of Panax japonicus var. major saponins, different shading treatments (0%, 30%,50%) of potted P. japonicus var. major were used as test materials, the expression of three key enzyme genes(CAS,DS,-AS) of leaves and rhizomes in different growth periods of P. japonicus var. major was determined by real-time quantitative PCR, the content of total saponins was determined by ultraviolet spectrophotometry. The results indicated that, in flowering stage, CAS,DS,-AS were highly expressed in the aerial parts of P. japonicus var. major, 30% shading treatment significantly inhibited the expression of CAS in leaves and promoted the expression of DS and -AS in stems, leaves and flowers, it was speculated that the main part of saponin synthesis was leaf in this stage. Both the expression levels of DS and -AS and changes in the content of total saponins in leaves showed a tendency of low-high-low throughout the growth cycle, correlation coefficient analysis showed that there was a positive correlation between them. Compared with control, the expression levels of DS and -AS and the content of total saponins were greatly enhanced under shading treatment, 30% shading treatment significantly promoted the accumulation of total saponins. Therefore, it is suggested that 30% shading treatment should be applied to the artificial cultivation of P. japonicus var. major, which is beneficial to the accumulation and quality improvement of saponins.

Preliminary study on RC membrane permeability and mechanism of seven traditional Chinese medicine alkaloids such as berberine / 中国中药杂志

In order to analyze the law of membrane permeation of different alkaloids, seven traditional Chinese medicine alkaloids with different parent nucleus and substituent structures, including berberine, palmatine, sinomenine, matrine, oxymatrine, sophoridine, and tetrandrine, were prepared into the simulated solution with same molar concentration, and the membrane penetrating experiments with membrane RC1K and membrane RC5K were carried out. The dynamic transmittance, the total transmittance and the total adsorption rate of each substance were measured, and the scanning electron microscopy (SEM) images of the membrane surface before and after the membrane experiment were considered to predict and analyze the reason of differences in dynamic transmittance of different alkaloids. The results showed that there were significant differences in the dynamic transmittance of the chemical constituents of different alkaloids during penetrating the two membranes. The contamination degree on the surface of the membrane material was also different. The transmittance of the same compound through the RC5K membrane was larger than that through RC1K membrane. Within a certain range, the smaller the pore size of the membrane, the better the selective screening effect on the chemical constituents of traditional Chinese medicine. All the membrane surfaces were less polluted. The difference in transmittance between different substances on the same membrane showed a positive correlation with the difference in structural complexity, providing an experimental basis for the surface modification design in contamination control of membrane materials. In the design of membrane modified material, the surface properties of the membrane can be improved by grafting different polar groups, thereby changing the adsorption characteristics of the membrane surface. The pore size was designed accordingly to achieve the high transmittance and low pollution of the corresponding compounds.

Chemical constituents from roots of Pieris formosa and their bioactivity / 中国中药杂志

By the means of chromatographic methods and spectroscopic evidences, 7 diterpenoids were isolated and identified from the roots of Pieris formosa. These known compounds are elucidated as secorhodomollolide C(1), pierisoid B (2), secorhodomollolide B (3), secorhodomollolide A (4), pierisformotoxin G (5), pierisformotoxin B (6) and pierisformotoxin A (7). Compounds 3, 4 were obtained from this plant for the first time. The analgesic activities of compounds 1-7 were evaluated using an acetic acidinduced writhing test in mice. Compounds 3, 4, 6, and 7 exhibited significant analgesic activity at 5 mg·kg;⁻ (ip) compared to vehicle-injected mice (<0.05). The writhe inhibition rates of compounds 3, 4, 6 and 7 at 5 mg·kg⁻¹ (ip) were 41.3%, 39.4%, 38.6% and 37.5%, respectively.

Study on essential oil separation from Forsythia suspensa oil-bearing water body based on vapor permeation membrane separation technology / 中国中药杂志

To investigate the feasibility of vapor permeation membrane technology in separating essential oil from oil-water extract by taking the Forsythia suspensa as an example. The polydimethylsiloxane/polyvinylidene fluoride (PDMS/PVDF) composite flat membrane and a polyvinylidene fluoride (PVDF) flat membrane was collected as the membrane material respectively. Two kinds of membrane osmotic liquids were collected by self-made vapor permeation device. The yield of essential oil separated and enriched from two kinds of membrane materials was calculated, and the microscopic changes of membrane materials were analyzed and compared. Meanwhile, gas chromatography-mass spectrometry (GC-MS) was used to compare and analyze the differences in chemical compositions of essential oil between traditional steam distillation, PVDF membrane enriched method and PDMS/PVDF membrane enriched method. The results showed that the yield of essential oil enriched by PVDF membrane was significantly higher than that of PDMS/PVDF membrane, and the GC-MS spectrum showed that the content of main compositions was higher than that of PDMS/PVDF membrane; The GC-MS spectra showed that the components of essential oil enriched by PVDF membrane were basically the same as those obtained by traditional steam distillation. The above results showed that vapor permeation membrane separation technology shall be feasible for the separation of Forsythia essential oil-bearing water body, and PVDF membrane was more suitable for separation and enrichment of Forsythia essential oil than PDMS/PVDF membrane.

Flavor and meridian tropism classification analysis of Callianthemum taipaicum / 中国中药杂志

To explore the flavor and meridian tropism classification of Callianthemum taipaicum by principal components analysis(PCA) and partial least square analysis(PLS). Meanwhile,to establish a high performance liquid chromatography-tandem mass spectrometry(HPLC-ESI-MS) method for the simultaneous determination of 55 active components from 13 kinds of Ranunculaceae of Chinese traditional herbs. Samples were separated on HPLC system by Agilent 5 TC-C₁₈（2）（4.6 mm×250 mm，5 μm）column and eluted with acetonitrile and 0.1% formic acid at the flow rate of 0.6 mL·min⁻¹. The data were performed by HPLC-ESI-MS with multiple reaction monitoring（MRM）scanning mode under positive and negative ion modes and quantified by external standards. The data from 13 Ranunculaceae herbs were analyzed by the PLS-tree and cooman's prediction of PCA and PLS to evaluate the similarities and differences of C. taipaicum in flavor and meridian tropism. The results showed that calibration curves of 55 components all showed good linearity, >0.99,with good precision, repeatability and stability. After compared to other 12 herbs,PCA and PLS results revealed that the C. taipaicum belonged to lung and bladder meridians while its flavor attributive to pungent,warm in nature. In conclusion,the analysis approach of chemometric calculation combined with multi-components quantification is suitable for the classification of meridian tropism and flavor of Chinese traditional medicine,which can be used for alternative research of rare herbs.

Analysis and evaluation of eight active ingredients in Lilium lancifolium from different regions / 中国中药杂志

This study established a rapid UPLC-TQ-MS/MS method for determination of eight active ingredients in Lilium lancifolium. The contents range of regaloside E, F, C and B are as follows: 0.604 0×10⁻¹-18.62×10⁻¹, 0.680 0×10⁻²-44.75×10⁻², 0.700 0×10⁻³-29.65×10⁻¹, 0.170 0×10⁻¹-4.724 mg•g⁻¹; the contents of chlorogenic acid, caffeic acid, protocatechualdehyde and ferulic acid, within the range of 6.827×10⁻³-16.07×10⁻³, 0.011 1×10⁻³-79.71×10⁻³, 0.593 7×10⁻³-2.962×10⁻³, 2.606×10⁻²-45.89×10⁻² mg•g⁻¹, respectively. According to PCA (principal components analysis) plotting, 35 batches can be divided into two categories, namely Anhui Huoshan and Hunan Longshan. The main different elements between these two categories are caffeic acid and ferulic acid according to the VIP (variable importance in the projection) points figure. Based on comprehensive principal component values, there are eight batches of L. lancifolium from Huoshan among the comprehensive ranking of ten. The UPLC-TQ-MS method for simultaneous analysis of eight active ingredients is accurate, efficient and convenient. This result can provide scientific basis for quality control of L. lancifolium.

Preparation and evaluation of dioscin nanostructured lipid carriers / 中国中药杂志

In this report, a heat and high-pressure homogenization method was used to prepare dioscin nanostructured lipid carriers, and the formulation of dioscin nanostructured lipid carriers was optimized by central composite design-response surface methodology. In vitro evaluation data showed that the preparation of dioscin nanostructured lipid carriers under optimal process by central composite design-response surface methodology had a spherical shape and homogeneous size distribution, with a particle size of (90.9±0.6) nm, a polydispersity index of (0.253±0.07), Zeta potential of (-45.7±0.5) mV, encapsulation efficiency of (90.2±0.5)%, and the drug loading of (23.30±0.10)%. These results clearly indicate that the preparation of dioscin nanostructured lipid carriers made with the heat and high-pressure homogenization method have very good physical and chemical properties, suitable for therapeutic applications.

Adsorption characteristics of proteins on membrane surface and effect of protein solution environment on permeation behavior of berberine / 中国中药杂志

In order to explore the adsorption characteristics of proteins on the membrane surface and the effect of protein solution environment on the permeation behavior of berberine, berberine and proteins were used as the research object to prepare simulated solution. Low field NMR, static adsorption experiment and membrane separation experiment were used to study the interaction between the proteins and ceramic membrane or between the proteins and berberine. The static adsorption capacity of proteins, membrane relative flux, rejection rate of proteins, transmittance rate of berberine and the adsorption rate of proteins and berberine were used as the evaluation index. Meanwhile, the membrane resistance distribution, the particle size distribution and the scanning electron microscope (SEM) were determined to investigate the adsorption characteristics of proteins on ceramic membrane and the effect on membrane separation process of berberine. The results showed that the ceramic membrane could adsorb the proteins and the adsorption model was consistent with Langmuir adsorption model. In simulating the membrane separation process, proteins were the main factor to cause membrane fouling. However, when the concentration of proteins was 1 g•L⁻¹, the proteins had no significant effect on membrane separation process of berberine.

Rationality analysis of clinical application of Danhong injection in affiliated hospital of Nanjing university of Chinese medicine from 2013 to 2014 / 中国中药杂志

It is necessary to investigate the influence of the rationality of clinical drug use on the benefit and risk factors of traditional Chinese medicine injections. The retrospective survey was based on the medical records and information of 4 950 patients who used Danhong injection in the HIS database of the first affiliated hospital of Nanjing University of Chinese Medicine from 2013 to 2014. The basic statistical methods and associated rules analysis were utilized to analyze the HIS information of these patients, including the basic information, the diagnosis, the department, the dosage, the usage of medication, the drug combination and the adverse reactions. And the rationality analysis of the clinical application of Danhong injection was carried out to investigate relevant factors of the adverse reactions. The results showed that most cases came from the department of cardiology (51.95%) and encephalopathy center (20.67%). In the statistical period, the patients aged above 40 years old accounted for 96.65%. And the two western medicine diagnosis items with the highest confidence level were coronary heart disease and angina pectoris (97.15%), while the three items were coronary heart disease, angina pectoris and hypertension (97.02%). The irrational indications were mainly hypertension (12.93%) and diabetes (4.55%). All of them were diagnosed as blood stasis syndrome by the traditional Chinese medicine. About 98.93% of the single dosage was within the range stipulated on package insert, the duration mainly ranged between 1 and 21 days, and 97.64% of the menstrua contained 0.9% NS and 5% GS. According to the medication records,99.26% were the use of combined drugs, with 8.41 drugs on average. Antiplatelet drugs (72.04%) were the most frequently combined with western medicine, followed by the cholesterol-regulating drugs (64.86%) and the cerebrovascular drugs (60.26%). When used in the combination with antibiotics for the infection, cephalosporin antibiotics were the most frequently applied (8.81%). When used with traditional Chinese medicines, traditional Chinese medicines for activating blood circulation and removing blood stasis or monomer traditional Chinese medicine injections (28.93%) were the dominance, in which Gastrodin injection was the most frequently applied (16.23%). And 12 cases of adverse reactions were reported, with the ADR rate of 0.24%. The indications, solvent compatibility and irrational drug combination may be the potential risk factors for ADRs induced by Danhong injection. Further experiments are required to evaluate the benefits and risks in these three aspects.

Stability of cantharidin and cantharidic acid in Mylabris aqueous solution / 中国中药杂志

To investigate the stability and the conversion rules of cantharidin and cantharidic acid contained in the Mylabris aqueous solution under different conditions. The contents of cantharidin and cantharidic acid under different conditions (pH, temperature and light) were determined by HPLC-TQ-MS. The results showed that the content of cantharidin was gradually decreased with the rising of pH value, while on the contrary, the content of cantharidic acid was increased gradually; after Mylabris aqueous solution with different pH values were placed at 25, 40 ℃ and 25 ℃ respectively for lighting for 90 days, the samples were collected for analysis. The results showed the contents of cantharidin and cantharidic acid were changed greatly in the first 10 days, mainly including the decrease of cantharidic acid and increase of cantharidin when the solution was acidic, and the increase of cantharidic acid and decrease of cantharidin when the solution was alkaline. After that, the contents of the above two components basically remained stable. This study revealed that pH was the main factor to affect the contents of cantharidin and cantharidic acid, and they could be converted into each other with the changes of pH value. High temperature and light can accelerate the speed of achieving such balance. The study can provide certain reference for the quality control of the medicines using the Mylabris as raw material.

Synthesis of new 4-anilinoquinazoline analogues and evaluation of their EGFR inhibitor activity / 药学学报

Thirteen of 4-anilinoquinazoline derivatives with imine groups at position 6 of quinazoline ring were synthesized and their antitumor activities were evaluated by MTT assay and Western blotting analysis. Among these compounds, 13a-131 were reported first time. The MTT assay was carried out on three human cancer cell lines (A549, HepG2 and SMMC7721) with EGFR highly expressed. Among the tested compounds, 13i and 13j exhibited notable inhibition potency and their IC50 values on three cell lines were equivalent to or less than those of gefitinib. Compound 14, without imine group substituted, displayed excellent inhibitor potency only on A549 cell line. Compounds 14 and 13j were chosen to perform Western blotting analysis on A549. The results showed that both of the compounds could inhibit the expression level of phosphorylated EGFR remarkably. It was concluded that the inhibitor potency of compound 14 was almost equivalent to that of gefitinib and the inhibitor potency of 13j was better than that of gefitinib.