Qualitative and quantitative study of constituents in Lysionoti Herba based on UHPLC-Q-Exactive Orbitrap HRMS and HPLC-UV / 中国中药杂志

Ultra-high performance liquid chromatography-quadrupole-Exactive Orbitrap high resolution mass spectrometry(UHPLC-Q-Exactive Orbitrap HRMS) was employed to systematically analyze the chemical constituents in Lysionoti Herba, and high perfor-mance liquid chromatography-ultraviolet(HPLC-UV) to determine the content of main compounds. A Synergi~(TM) Hydro-RP 100 Å colu-mn(2 mm×100 mm, 2.5 μm) was used for gradient elution with acetonitrile-0.1% aqueous formic acid as the mobile phase at a flow rate of 0.2 mL·min~(-1) and a column temperature of 40 ℃. MS and MS/MS were conducted with electrospray ionization(ESI) in both positive and negative modes. The chemical components in Lysionoti Herba were identified by comparison with the retention time and mass spectra of reference compounds and the relevant mass spectral data reported in MS databases and relevant literature. Furthermore, the content of five constituents(neochlorogenic acid, chlorogenic acid, forsythoside B, acteoside, and nevadensin) in different Lysiono-ti Herba samples was simultaneously determined by HPLC-UV at the wavelength of 330 nm. A total of 84 compounds were identified in Lysionoti Herba, including 27 flavonoids, 20 phenylethanoid glycosides, 5 amino acids, 18 organic acids, 1 alkaloid, 6 nucleosides, and 7 others. The content of neochlorogenic acid, chlorogenic acid, forsythoside B, acteoside, and nevadensin showed good linear relationship(r>0.999) with the peak area within certain concentration ranges, which were 3.22-102.90, 12.84-410.82, 31.63-1 012.01, 25.00-800.11, and 4.08-130.51 μg·mL~(-1), respectively. The instrument precision, method repeatability, and solution stability all met requirement, and the average recovery rate was 97.31%-100.2%, with RSD ranging from 0.95% to 2.4%. The content of the five components varied among different Lysionoti Herba samples collected from different regions of Guizhou, and the average content of forsythoside B was the highest. The established qualitative method can rapidly and efficiently identify the chemical components of Lysionoti Herba, and the developed HPLC-UV method can simultaneously determine the content of five components in a simple, ra-pid, and accurate manner, providing a scientific basis for the quality evaluation of Lysionoti Herba.

Acupoint selection for cancer pain: based on current evidence and Delphi method / 中国针灸

Based on literature research and Delphi expert consensus method, the important acupoints for cancer pain was summarized to provide evidence basis for the formulation of

Complete plastid genomes of Bupleurum chinense DC. and B. boissieuanum H. Wolff, with comparative and phylogenetic analyses of medicinal Bupleurum species / 药学学报

italic>Bupleurum L. (Apiaceae) is an economically important genus, in which many species are of medicinal value. In this study, the complete plastid genomes (plastomes) of B. chinense DC. and B. boissieuanum H. Wolff were sequenced and their characteristics were investigated. Comparative and phylogenetic analyses were conducted with other published Bupleurum plastomes. The complete plastomes of B. chinense and B. boissieuanum were 155 458 and 155 800 bp in length, and both exhibited the typical quadripartite circular structure consisting of a large single copy region (LSC, 85 343 and 85 804 bp), a small single copy region (SSC, 17 495 and 17 410 bp), and a pair of inverted repeat regions (IRa/b, 26 310 and 26 293 bp), respectively. A total of 129 genes, including 84 protein-coding genes, 37 transfer RNA (tRNA) genes, and eight ribosomal RNA (rRNA) genes were identified from each of the two plastomes. Repeat sequences detected were similar in types and distribution patterns, but the numbers were slightly different. Comparative analyses revealed that the Bupleurum plastomes were highly conserved in length, structure, the guanine and cytosine (GC) content, and gene content and order, both intraspecifically and interspecifically, and no obvious expansion or contraction of the inverted repeat regions occurred. Sequence variation was lower within the same species than among different species, noncoding sequences (including intergenic regions and introns) showed a higher divergence than the protein-coding sequences, and sequences in the LSC and SSC regions were more divergent than those in the IR regions. In addition, 11 sequences with higher nucleotide diversity among species were detected in the LSC and SSC regions. All studied Bupleurum species were inferred forming a monophyletic group with a 100% bootstrap value. Bupleurum chinense and B. boissieuanum were phylogenetically closest to B. commelynoideum and B. falcatum, separately, with all three B. chinense accessions clustered into a distinct clade. These results provide genetic information for further species identification, phylogenetic resolution, and will assist in exploration and utilization of medicinal Bupleurum species.

Mechanism of Liangfu Dropping Pills in treatment of gastrointestinal diseases based on plasma pharmacochemistry and network pharmacology / 中国中药杂志

To study the active chemical components and mechanism of Liangfu Dropping Pills in treatment of gastrointestinal diseases. The UHPLC-Q-TOF-MS method was employed to analyze the components of Liangfu Dropping Pills in plasma. The protein targets of the absorbed compounds were predicted in the TCMSP database and the SwissTargetPrediction database. The targets associated with gastrointestinal diseases were collected from OMIM, CTD, GeneCards, and DrugBank. The common target genes between components and diseases were screened out for the building of protein-protein interaction(PPI) network in the STRING database. Metascape was used to carry out gene ontology(GO) and Kyoto encyclopedia of genes and genomes(KEGG) pathway enrichment analysis. Cytoscape was employed to construct the PPI network diagram and absorbed component-target network diagram. The molecular docking between the components absorbed in blood and potential key targets was performed by AutoDock vina 4.2.6 to screen and verify the main active components and targets. Twelve chemcial components were identified in Liangfu Dropping Pills, in which four components were absorbed in blood, including galangin, rhamnocitrin, galangin 3-methyl ether, and α-cyperone. These components acted on 189 common targets which were mainly involved in the cell responses to nitrogen compounds, organic cyclic compounds, and hormones, and enriched in the PI3 K-Akt signaling pathway, Foxo signaling pathway, and IL-17 signaling pathway. Molecular docking results showed that the four components had strong affinity with core targets. The material basis of Liangfu Dropping Pills treating gastrointestinal diseases may be galangin, rhamnocitrin, galangin 3-methyl ether, and α-cyperone. This study provides a theoretical basis for further development and application of Liangfu Dripping Pills.

Application of ultrasonic visualization technology in the treatment of war trauma / 第二军医大学学报

In modern war, the advancement of military technology and weapons results in the gathering of severe casualties and increases the difficulty in field rescue, which brings great challenges for medical staff to complete the assessment, classification and rescue tasks in a short time. Ultrasonic examination can easily and quickly screen and diagnose the wounded in battlefield environment or field hospital, and improve the efficiency of classification and treatment. Ultrasonic visualization technology can improve the screening and diagnosis efficiency of war trauma patients with chest, abdomen, craniocerebral and skeletal soft tissue injuries. It also provides convenience for emergency treatment of war trauma patients and improves the emergency treatment effects. This paper reviews the application of ultrasonic visualization technology in the evaluation and emergency treatment of war trauma patients.

Identification of Bupleurum Seeds by ITS2 Genetic Barcoding and Seed Morphology / 中国实验方剂学杂志

Objective:To accurately identify Bupleurum seeds by traditional morphological identification method combined with DNA barcoding technique. Method:A total of 41 seed samples on the market were collected and 75 ribosomal DNA internal transcribed spacer 2 (ITS2) sequences of 15 varieties were downloaded from the GenBank database as experimental materials. The seeds were measured and observed by stereomicroscope and vernier caliper, and their 1 000-grain weights were calculated. Genomic DNA was extracted from the seeds and used as a template, and ITS2 sequences were amplified using polymerase chain reaction (PCR) and bidirectional sequencing. Species identification was conducted based on BLAST method, neighbor-joining (NJ) phylogenetic tree method, Kimura two-parameter model (K2P) genetic distance method, and secondary structure of ITS2 sequence. Result:There were slight differences in the length, width, cross-section, and 1 000-grain weight among Bupleurum seeds from different origins. The ITS2 sequences of B. chinense seeds had 2 intraspecific variable sites and 3 haplotypes, the maximum intraspecific genetic distance (0.009) was far smaller than the minimum interspecific genetic distance (0.032). B. chinense and B. scorzonerifolium in the NJ phylogenetic tree were clustered into independent branches with good monophyletic property. The secondary structure of ITS2 sequences could make up for the shortcomings of NJ tree in identifying variants. The collected 41 seeds included 30 B. chinense seeds, 3 B. scorzonerifolium seeds, 5 B. falcatum seeds, 2 B. marginatum var. stenophyllum seeds, and 1 B. smithii var. parvifolium seeds. Conclusion:The B. chinense seeds on the market have problems of diverse sources and chaotic origins. Based on the combination of ITS2 gentic barcoding and seed morphological identification, the Bupleurum seeds can be accurately identified, which provides scientific bases for establishing the quality standard of Bupleurum seeds, standardizing the cultivation of B. chinense, and solving the quality problems of B. chinense from the source, and provides a reference for the accurate identification of other medicinal plant seeds or seed medicinal materials.

Effect of Arisaema Rhizoma and Pinelliae Pedatisectae Rhizoma on Water Metabolism and Hemorheology in Rats / 中国实验方剂学杂志

Objective:To discuss the effect of Arisaema Rhizoma and Pinelliae Pedatisectae Rhizoma on water metabolism and hemorheolog in rats. Method:A total of 50 healthy SD rats were randomly divided into 5 groups, namely normal group, high-dose Arisaema Rhizoma group (1.2 g·kg·d-1), low-dose Arisaema Rhizoma group (1.2 g·kg·d-1), high-dose Pinelliae Pedatisectae Rhizoma group (1.2 g·kg·d-1) and low dose Pinelliae Pedatisectae Rhizoma group (0.3 g·kg·d-1), with 10 rats in each group. The effects of Arisaema Rhizoma and Pinelliae Pedatisectae Rhizoma on water metabolism and hemorheology were compared, with the micturition index, fecal volume, fecal water content, pathological morphology of submandibular gland, aquaporin (AQP2) content in kidney, adenosine cyclic 3′,5′-(hydrogen phosphate)/current good manufacture practices (cAMP/cGMP) and Na+-K+-ATP enzyme content in serum as the evaluation indexes of water metabolism, and the whole blood viscosity (WBV) and erythrocyte aggregation index (RE) as the evaluation indexes of hemorheolog. Result:Compared with normal group, the fecal volume, fecal water content and AQP2 expression decreased significantly， acinus of submandibular gland were atrophied， micturition index, cAMP/cGMP and Na+-K+-ATP enzyme content in serum were increased significantly， WBV and RE were increased significantly in high-dose Arisaema Rhizoma and Pinelliae Pedatisectae Rhizoma groups（P<0.05）, but with no significant difference between them. Conclusion:High-dose Arisaema Rhizoma and Pinelliae Pedatisectae Rhizoma groups had significant effects on water metabolism and hemorheology in rats, suggesting that attention shall be given to the safety of Arisaema Rhizoma and Pinelliae Pedatisectae Rhizoma. And this study provides a theoretical basis for the rational use of the two traditional Chinese medicines in clinic.

Advances in Bioculture Technology of Bupleuri Radix and Biosynthesis Pathways of Saikosaponins / 中国实验方剂学杂志

Synthetic biology is an emerging discipline that analyzes the biosynthesis pathways of active constituents in traditional Chinese medicine and explores genes involved in biosynthesis. Bupleuri Radix is one of the most commonly used Chinese medicinal materials with remarkable medicinal value, its index component is saikosaponins, which has significant anti-inflammatory, anti-viral and anti-tumor activities. However, the current wild resources of Bupleuri Radix have been destroyed, and there were some problems in the process of artificial cultivation. The application of biological culture technology and synthetic biology can expand the sources of saikosaponins and protect resources of Bupleuri Radix. The culture conditions of different plants can be followed without a fixed pattern, and the biosynthetic pathways of different medicinal active ingredients are also inconsistent. At present, there is no review report on the culture technology of Bupleuri Radix and the research on the biosynthesis pathway of saikosaponins. This paper introduces the research progress of biological culture techniques, such as callus culture, adventitious root culture, hairy root culture and suspension cell culture used in synthetic biology, and the biosynthesis pathway of saikosaponins and its key enzyme functional genes. It is suggested to optimize the biological culture technology of Bupleuri Radix by referring to the tissue culture technology of other traditional root medicinal materials, so as to provide a reference for the in-depth study on the biosynthesis pathway and metabolic regulation of saikosaponins.

Effect of Compound Longmaining on TLR4/MyD88/NF-κB p65 Signaling Pathway in Rats with Acute Myocardial Infarction / 中国实验方剂学杂志

Objective: To investigate the protective effect of compound Longmaining isoprenaline hydrochloride-induced myocardial infarction model and its effect on Toll-like receptor 4(TLR4)/myeloid differentiation factor 88(MyD88)/nuclear transcription factor-kappa B (NF-κB) signaling pathway.Method: Forty-eight male SD rats were randomly divided into 6 groups:normal group,model group,compound salvia miltiorrhiza drop pill group (0.072 9 g·kg-1),and low,medium and high-dose compound Longmaining decoction groups (0.36,0.71,1.43 g·kg-1).The acute myocardial infarction model was induced through subcutaneous injection with isoproterenol.The pathological changes of myocardial tissue were examined by hematoxylin-eosin (HE) staining.The levels of interleukin-1β(IL-1β),interleukin-6(IL-6),tumor necrosis factor-α(TNF-α),monocyte chemotaxis protein-1(MCP-1) and nitrogen (NO) in serum were measured by enzyme linked immunosorbent assay (ELISA).The expression levels of inhibitors of NF-κB kinase subunit-β(IKKβ),NF-κB inhibitor α(IκBα),TLR4,MyD88 and NF-κB p65 were measured by immunohistochemical staining and Western blot.Result: Compared with normal group,the myocardial injury in model group was obvious.The levels of IL-1β,IL-6,TNF-α,MCP-1 and NO in serum increased significantly (PκBα decreased significantly (Pβ,TLR4,MyD88 and NF-κB p65 increased significantly in myocardial tissue (Pβ,IL-6,TNF-α,MCP-1 and NO levels in the serum (PκBα(Pβ,TLR4,MyD88 and NF-κB p65(PConclusion: Compound Longmaining plays a protective effect on acute myocardial infarction by regulatingthe expressions of TLR4/MyD88/NF-κB p65 signaling pathway and relevant inflammatory factors.

Comparison of different methods for drug delivery via the lumbar spinal subarachnoid space in rats / 南方医科大学学报

OBJECTIVE@#To compare 3 commonly used methods for drug delivery via the lumbar spinal subarachnoid space in rats.@*METHODS@#We compared the effects of 3 methods for drug delivery via the lumbar spinal subarachnoid space in Sprague Dawley rats, namely acute needle puncture, chronic catheterization via laminectomy, and non-laminectomized catheterization. Body weight changes of the rats were measured, and their general and neurological conditions were assessed after the surgeries. The motor function of the rats was examined using rota rod test both before and after the surgeries. Nociceptive tests were performed to assess nociception of the rats. HE staining was used to examine local inflammation caused by the surgeries in the lumbar spinal cord tissue, and lidocaine paralysis detection and toluidine blue dye assay were used to confirm the precision of drug delivery using the 3 methods.@*RESULTS@#Both needle puncture and catheterization via laminectomy resulted in a relatively low success rate of surgery and caused neurological abnormalities, severe motor dysfunction, hyperalgesia, allodynia and local inflammation. Catheterization without laminectomy had the highest success rate of surgery, and induced only mild agitation, slight cerebral spinal fluid leakage, mild sensory and motor abnormalities, and minimum pathology in the lumbar spinal cord. Catheterization without laminectomy produced less detectable effects on the behaviors in the rats and was well tolerated compared to the other two methods with also higher precision of drug delivery.@*CONCLUSIONS@#Catheterization without laminectomy is a safe, accurate and effective approach to lumbar drug delivery in rats.

Pleural amoebic empyema: a case report / 中国血吸虫病防治杂志

In this paper, a case of pleural amoebic empyema and its diagnosis and treatment were reported.

Metabolic Characteristics of Leucocyte-deplated and Suspended RBC Produced by Using Lipid Whole Blood During Routine Storage / 中国实验血液学杂志

<p><b>OBJECTIVE</b>To investigate the differences of metabolic pathways of leucocyte-deplated RBCs prepared by using lipid whole blood and nomal blood during routine storage so as to provide some reference for clinical blood use.</p><p><b>METHODS</b>Twenty U whole blood from 20 donors, including 10 U lipid blood and 10 U normal whole blood, were selected for preparing leukodepleted red blood cells, red blood cells were taken from storage bags on day 0, 14 and 35, respectively. Metabolites in the red blood cells were analyzed, red blood cell metabolic extracts were detected by UPLC-MS/MS. The metabolite data of RBC from 2 groups were analyzed by SIMCA-P 13.0 software using OPLS-DA and by SPSS 19.0 using Mann-Whitney U test. Difference of metabolic pathways was described according to different metabolites.</p><p><b>RESULTS</b>The glucose, adenine, pyruvic acid, GSH, GSSG and niacinamide levels on day 0 in lipid RBCs were higher than those in the control group(P<0.05). The glucose, pyruvic acid and GSH levels on day 14 in lipid RBCs were lower than those in the control group (P<0.05), and the levels of adenine, GSSG and niacinamide were higher than that in the control group (P<0.05). The glucose level on day 0 was lower than that in the control group (P<0.05), and the levels of adenine and niacinamide were higher than those in the control group (P<0.05). but the pyruvic acid, GSH and GSSG levels were not significantly different between 2 groups (P>0.05).</p><p><b>CONCLUSION</b>Compared with the normal red blood cells, the energy metabolism pathway decreases in lipid red blood cells within the storage period and pentose phosphate pathway increases.</p>

Pleural amoebic empyema: a case report / 中国血吸虫病防治杂志

In this paper, a case of pleural amoebic empyema and its diagnosis and treatment were reported.

Micro RNA differential expression in primary retroperitoneal liposarcoma / 中国现代普通外科进展

Objective:To explore the miRNA (micro RNA)differential expression profile between primary retroperitoneal liposarcoma tissues and normal fat tissues,and to provide the evidence that miRNA were involved in the molecular pathways of primary retroperitoneal liposarcoma tissues' occurrence.Methods:Collecting retroperitoneal liposarcoma tissues and normal fat tissues from 4 patients after radical surgery of retroperitoneal lipsarcoma.Using microarray analysis.The tissues' miRNA hybridizated with human's LC Sciences microRNA Microarray-Single (miRBase 21.0) expression profile gene chips,and got the date.Analyzing the differential expressing of the siginal date by LOWESS.Results:Total 38 differential expressed miRNA were found (P＜0.05),including 23 over-expression and 15 low-expression miRNAs.10 of them(38 differential miRNAs) was significant deviation (P＜0.01),including 4 over-expression and 6 low-expression.Date analysis revealed that some miRNAs were associated some different tumors,Conclusion:The number of over-expression were more than the low-expression in primary retroperitoneal liposarcoma compared with the normol fat tissue,which indicate that the genes expression are less abundant in primary retroperitoneal li-posarcoma;some of the miRNAs might involved in the molecular pa-thways of primary retroperitoneal liposarcoma tissues' occurrence and recurrence,they might become the target point of the targetedtherapy of the primary retroperitoneal liposarcoma,some of the over-expressed miRNAs can become new biomarkers in the following diagnosis of the primary retroperitoneal liposarcoma.

Individual strategy of retroperitoneoscopic nephrectomy for benign non-functioning kidneys (84 cases) / 中国内镜杂志

Objective To explore the technique and clinical efficacy of retroperitoneoscopic nephrectomy (RN) at different anatomical plane for benign non-functioning kidneys. Method We retrospectively reviewed the clinical data of 84 patients who underwent RN for benign non-functioning kidneys from February 2010 to November 2016. Various anatomical plane was performed for differing etiology, image and plane, included radical nephrectomy (A group, n = 35), simple nephrectomy (B group, n = 27) and subcapsular nephrectomy (C group, n = 22). Clinical data and preoperative information was collected and analyzed. Result Nephrectomy was performed successfully in 84 patients. There are significantly longer mean operative time and more estimated blood loss in the C group than that in A group and B group (P < 0.05), however, postoperative hospital stay, complications and recovery time were significantly less in the three groups. There was longer mean operative time and more estimated blood in specific and nonspecific infection group compared with the other two groups (P < 0.05). Conclusion Retroperitoneoscopic nephrectomy, although challenging, is safe, reliable, and successful for treatment of benign non-functioning kidneys.Anatomical plane of avascular zone should be offered as the choice of modality to all patients with benign non-functioning kidney.

Analysis of influencing factors of lymph node metastasis in patients with central and peripheral types of squamous cell lung cancer / 天津医药

Objective To analyze the factors related to the metastasis of lung squamous cell carcinoma in patients with central and peripheral types of lung squamous carcinoma, and provide evidence-based basis for preoperative preparation, intraoperative lymph node treatment choice and postoperative treatment. Methods Clinical data of 142 patients with lung squamous carcinoma who performed operation in Tianjin Medical University Cancer Institute and Hospital from January 2014 to December 2015 were retrospectively analyzed. There were 83 cases of central lung squamous cell carcinoma and 59 cases of peripheral lung squamous carcinoma in these 142 patients. Single factor and multiple factor Logistic regression analysis were used to analyze the clinical data in patients with different type groups, including gender, age, smoking history and smoking index, preoperative CYFRA21-1 level, preoperative predictive lymph nodes metastasis, tumor diameter, tumor type (keratotic and non-keratotic), pleura invasion, tumor embolism and postoperative lymph node metastasis. Results There were 47 cases with lymph node metastasis in 147 patients, including 31 cases of central type metastasis, and 16 cases of peripheral type metastasis. Single factor analysis showed that gender, smoking history, smoking index, preoperative lymph node metastasis assessment, tumor diameter, and non-keratotic type were related to the metastasis of central type of lung squamous cell carcinoma. Pleural invasion and non-keratotic type were associated with peripheral type of pulmonary squamous cell carcinoma. Multivariate Logistic regression analysis showed that more smoking, large tumor diameter and non-keratotic type were independent risk factors for lymph node metastasis of central type of lung squamous cell carcinoma. The non-keratotic type was an independent risk factor for lymph node metastasis of peripheral pulmonary squamous carcinoma. Conclusion Non-keratotic type of squamous cell carcinoma is related to lymph node metastasis especially N1 lymph node metastasis. It is suggested that such patients should be actively treated and colsely followed up after the operation. Patients with more smoking may be more likely to have N2 lymph node metastasis.

Sinonasal mammary analogue secretory carcinoma: a clinicopathological analysis of 2 cases / 临床与实验病理学杂志

Purpose To investigate the clinicopathological features of sinonasal primary secretory carcinoma (SC) and its diagnosis, differential diagnosis. Methods Two cases of sin-nasal SC were analyzed by light microscopy with immunohisto-chemical staining (EnVision) for CK, vimentin, S-100 protein, SOX10, PAS, DPAS, Mamaglobin, Calponin, DOG1, p63 and molecular detection of ETV6 gene break. Results Morphologically, SC revealed varying proportions of solid, tubular, acinar, microcystic, tubular growth patterns. All SC cases were cytological low grade with uniform cells, small-to medium-sizes nuclei, occasional small nucleoli, and abundant pink, bubbly cytoplasm. Mitotic figures were rarely encountered. Tumor cells secreted eosinophilic, colloid-like secretions that were PAS positive. There were no DPAS positive zymogen granules in cyto-plasm. This tumor cells were CK, vimentin, S-100, SOX10, PAS positive and Mamaglobin, Calponin and p63 negative. The ETV6 gene rearrangement was confirmed in all cases by fluorescence in situ hybridization (FISH). After excision, all two patients were survival without tumor recurrence for 41 months and53 months. Conclusion Sinonasal primary SC is a low grade malignant tumor. The histological features of SC are overlap with other salivary gland tumors. Immunohistochemical analysis and FISH are useful for the diagnosis and differential diagnosis.

Bioassay-guided isolation of saikosaponins with agonistic activity on 5-hydroxytryptamine 2C receptor from Bupleurum chinense and their potential use for the treatment of obesity / 中国天然药物

5-Hydroxytryptamine 2C (5-HT) receptor is one of the major targets of anti-obesity agents, due to its role in regulation of appetite. In the present study, the 70% EtOH extract of the roots of Bupleurum chinense was revealed to have agonistic activity on 5-HT receptor, and the subsequent bioassay-guided isolation led to identification of several saikosaponins as the active constituents with 5-HT receptor agonistic activity in vitro and anti-obesity activity in vivo. The new compound, 22-oxosaikosaponin d (1), was determined by extensive spectroscopic analyses (HR-ESI-MS, IR, and 1D and 2D NMR). The primary structure-activity relationship study suggested that the intramolecular ether bond between C-13 and C-28 and the number of sugars at C-3 position were closely related to the 5-HT receptor agonistic activity. Saikosaponin a (3), the main saponin in B. chinense, showed obviously agonistic activity on 5-HT receptor with an EC value of 21.08 ± 0.33 μmol·Lin vitro and could reduce food intake by 39.1% and 69.2%, and weight gain by 13.6% and 16.4%, respectively, at 3.0 and 6.0 mg·kgin vivo. This investigation provided valuable information for the potential use of B. chinense as anti-obesity agent.

Effect of compound Longmaining decoction with different combinations on intestinal absorption of puerarin / 中国中药杂志

To study the effects of compound Longmaining(FFLMN) with different combinations on the intestinal absorption of puerarin. The rat single pass intestinal perfusion model was adopted, and the concentration of puerarin in intestinal samples was determined by HPLC. The effects of different combination groups on the absorption of puerarin in duodenum, jejunum, ileum and colon were investigated. The combined drugs were GG(Puerariae Lobatae Radix), GG-CSL (Puerariae Lobatae Radix compared with Dioscoreae Nipponicae Rhizoma), GG-CX(Puerariae Lobatae Radix compared with Chuanxiong Rhizoma) and FFLMN (compound Longmaining). We found that the absorption rate constant(Ka) and the apparent coefficient(Papp) of puerarin had no significant difference between GG-CSL and FFLMN groups, but significantly higher in GG and GG-CX groups(P<0.05) in the duodenum and ileum. In jejunum and colon, Ka and Papp of puerarin showed significant differences between GG and other groups(P<0.05). At the same time, FFLMN also had significant differences with GG-CSL and GG-CX groups(P<0.05). The results showed that in the whole intestine of rats, FFLMN could significantly promote the absorption of puerarin. In the duodenum and ileum, Dioscoreae Nipponicae Rhizoma played a significant role in promoting absorption of puerarin. In jejunum and colon, Dioscoreae Nipponicae Rhizoma and Chuanxiong Rhizoma have a synergistic effect in promoting absorption of puerarin.

Effect of puerarin in Longmaining formula on pharmacokinetics-pharmacodynamics correlation in rats with myocardial ischemia / 中国中药杂志

To study the pharmacokinetics of puerarin in compound Longmaining(FFLMN) in normal rats and myocardial ischemia rats, and investigate its correlation with anti-myocardial ischemia effect of FFLMN. Models of myocardial ischemia rats were produced by subcutaneous injection of isoproterenol(ISO), then FFLMN extract solution was administered by gavage. Orbital sinus blood sampling was collected at different time points after gavage. HPLC-UV method was applied to determine the concentration of puerarin in plasma, and compare the difference in pharmacokinetics between normal rats and model rats after application of same dose of FFLMN. Meanwhile, microplate reader was used to determine IL-6 and SOD activities in plasma of different time points, and draw dose-effect curve. The results indicated that the pharmacokinetics of puerarin conformed to the two-compartment model in both normal group and myocardial ischemia model group. In the comparison of main pharmacokinetic parameters between two groups: AUC0-∞=(11.451±3.228) mg•h•L⁻¹,AUC0-t=(14.047±3.765) mg•h•L⁻¹, Cmax=(5.623±1.40) mg•L⁻¹ in normal group; AUC0-∞=(68.849±50.396 9) mg•h•L⁻¹, AUC0-t= (58.312±45.802) mg•h•L⁻¹,Cmax=(18.456±7.517) mg•L⁻¹ in treatment group. The SOD level was significantly increased and IL-6 concentration was significantly decreased in plasma, indicating that as compared with the normal group, puerarin in FFLMN had a higher plasma concentration, slower elimination rate and higher bioavailability. Therefore, puerarin concentration in plasma has correlation with the anti-myocardial ischemia effect of FFLMN, which could increase SOD level and inhibit the release of IL-6.