Structure-activity relationship of Lycium barbarum polysaccharides / 中国中药杂志

As a traditional Chinese herb and functional food, the fruits of Lycium barbarum has been widely used for thousands of years in China. L. barbarum polysaccharides(LBPs) are predominant active components, which have immunomodulatory, antioxidant, hypoglycemic, neuroprotective, anti-tumor, and prebiotic activities. The molecular weight, monosaccharide composition, glycosidic bond, branching degree, protein content, chemical modification, and spatial structure of LBPs are closely related to their biological activity. Based on the previous studies of this research team, this paper systematically combed and integrated the research progress of structure, function, and structure-activity relationship of LBPs. At the same time, some problems restricting the clarification of the structure-activity relationship of LBPs were considered and prospected, hoping to provide references for the high value utilization of LBPs and in-depth exploration of their health value.

Effect of modified Chufeng Yisun Decoction on ocular surface inflammation after pterygium surgery / 国际眼科杂志(Guoji Yanke Zazhi)

AIM: To investigate the effect of modified Chufeng Yisun Decoction on ocular surface inflammation after pterygium surgery.METHODS: A total of 60 patients(60 eyes)with primary pterygium who underwent pterygium surgery were randomly divided into control group and study group, with 30 cases(30 eyes)in each group. In the control group, patients were treated with pranoprofen eye drops, tobramycin dexamethasone eye drops, and deproteinized calf blood extract eye gel after the surgery. In the study group, patients were treated by oral modified Chufeng Yisun Decoction in addition to the treatments in the control group. The changes of ocular irritation symptoms, ocular inflammatory signs, tear interleukin 6(IL-6)levels, and tear ferning test(TFT)of patients in the two groups were assessed.RESULTS: The visual analogue scale(VAS)in patients of both groups was significantly lower at 2d and 1wk after the surgery than that at 1d after the surgery(all P<0.01), and the VAS of the study group was significantly better than that of the control group at 2d and 1wk after surgery(P<0.01). The ocular signs integrals(OSI)and TFT results of both groups at 1wk were significantly lower than those at 1d after the surgery(all P<0.01), and the OSI and TFT were also lower in the study group than in the control group at 1wk after the surgery(all P<0.01). In addition, the concentration of tear IL-6 in both groups was significantly lower at 1wk after the surgery than 1d after the surgery(all P<0.01), and it was also significantly lower in the study group than in the control group at 1wk after the surgery(P<0.05).CONCLUSION: The combination of Chufeng Yisun Decoction and conventional treatment of western has a better effect on controlling ocular surface inflammation after pterygium surgery.

Analysis on incidence trend of liver cancer in China, 2005-2016 / 中华流行病学杂志

Objective: To understand the incidence trend of liver cancer in China from 2005 to 2016, and explore the correlation between the incidence trend of liver cancer and the incidence trend of hepatitis B. Methods: The incidence data of liver cancer in China from 2005 to 2016 were collected from the Annual Report of Cancer Registry in China. The incidence data of hepatitis B were collected from China Public Health Science Data Center. World standardized incidence rate (WSR) was calculated according to the World Segi's population. Joinpoint regression model was used to analyze the trend of WSR of liver cancer [measured by average annual percentage change (AAPC)]. The age-period-cohort model was fitted to analyze the age, period and cohort effects in people aged 20- years and above. Pearson correlation coefficient was used to explore the correlation between the incidence of liver cancer and the incidence of hepatitis B. Results: The crude incidence of liver cancer in China showed a trend of first increase before 2009 and then relatively stable. The world standardized morbidity rate of liver cancer in China decreased from 19.11 per 100 000 in 2005 to 17.74 per 100 000 in 2016 (AAPC=-0.5%, 95%CI: -1.3%-0.3%, P=0.240). The incidence of liver cancer in male decreased significantly (AAPC=-1.0%, 95%CI: -1.5%--0.5%, P=0.001). The incidence of liver cancer in women increased from 2005 to 2010 [annual percentage change (APC)=1.7%, 95%CI: -0.1%-3.4%, P=0.059] but showed a significant decrease trend from 2010 to 2016 (APC=-1.6%, 95%CI: -2.3%--1.0%, P=0.001). From 2005 to 2016, the incidence of liver cancer showed a decreasing trend in urban areas (AAPC=-0.3%, 95%CI: -0.8%-0.3%, P=0.316) and rural areas (AAPC=-3.9%, 95%CI: -4.4%--3.3%, P<0.001). Risk for liver cancer increased with age, while the period effect showed a trend of first increase then decrease and cohort effect showed a decrease trend. The morbidity rates of both hepatitis B and liver cancer showed decrease trends from 2009 to 2016, and there was a significant correlation (r=0.71, 95%CI: 0.01-0.94, P=0.048). Conclusions: From 2005 to 2016, the morbidity rate of liver cancer in China showed a decrease trend, and there were significant gender and urban-rural area specific differences. Age effect had a great impact on the risk for liver cancer. With the progress of population aging in China, liver cancer is still a public health problem, to which close attention needs to be paid.

Chemical Compositions and Anti-tumor Effect of Tetrastigma hemsleyanum： A Review / 中国实验方剂学杂志

Due to the infinite proliferation， strong migration and loss of contact inhibition of tumor cells， tumor has become the most intractable diseases to be cured in the world. At present， the main treatments of tumor diseases are surgical resection， radiotherapy， chemotherapy， targeted-therapy and immunotherapy. Although these measures can inhibit or kill the tumor to a certain extent， they still cannot avoid adverse reactions and drug resistance. After thousands of years of clinical practice， traditional Chinese medicine （TCM） has the characteristics of good curative effect， few adverse reactions and significantly improving the quality of life in patients， which provides new ideas for the prevention and treatment of tumors. As an endemic and rare plant in China， Tetrastigma hemsleyanum has been listed in the 2015 edition of Zhejiang Provincial Processing Specification of TCM with the effects of heat-clearing and detoxification， detumescence and analgesia， dissipating phlegm and resolving masses. It has been reported that the chemical constituents of T. hemsleyanum are mainly flavonoids， polysaccharides， phenolic acids， terpenoids， steroids， volatile oils， alkaloids and so on. It can exert a broad spectrum of anti-tumor effects through various ways such as inhibiting proliferation， migration and invasion of tumor cells， inducing apoptosis of tumor cells， inhibiting angiogenesis of tumor cells， reversing multidrug resistance of tumor cells and regulating body autoimmunity. On the basis of reviewing relevant literature at home and abroad， this paper intends to systematically sort out the chemical and anti-tumor research of T. hemsleyanum， and in order to provide a new idea for its synergistic anti-tumor effect of multi-component， multi-pathway and multi-target， and finally provide theoretical basis for the research and development and clinical application of new anti-tumor drugs of T. hemsleyanum.

Two cardenolide glycosides from the seed fairs of Asclepias curassavica and their cytotoxic activities / 中国天然药物

Two cardenolide glycosides, corotoxigenin 3-O-[β-D-glucopyranosyl-(1→4)-6-deoxy-β-D-glucopyranoside] (1) and coroglaucigenin 3-O-[β-D-glucopyranosyl-(1→4)-6-deoxy-β-D-glucopyranoside] (2), were isolated from the seed fairs of Asclepias curassavica. The structures of 1-2 were determined based on the combination of the analysis of their MS, NMR spectroscopic data and acid hydrolysis. The inhibitory effects of compounds 1 and 2 on human colorectal carcinoma cells (HCT116), non-small cell lung carcinoma cells (A549) and hepatic cancer cells (SMMC-7721) were evaluated. The results showed that both compounds 1 and 2 significantly inhibited the viability, proliferation, and migration of A549, HCT116 and SMMC-7721 cells, suggesting that compounds 1 and 2 can be applied in the treatment of lung, colon and liver cancers in clinical practice. This study may not only provide a scientific basis for clarifying the active ingredients in A. curassavica, but also help to understand its antitumor activity, which can promote the application of A. curassavica in clinical treatment of various cancers.

New tirucallane-type triterpenoids from the resin of Boswellia carteriiand their NO inhibitory activities / 中国天然药物

Six new tirucallane-type triterpenoids (1-6), along with ten known triterpenoids, were isolated from methylene chloride extract of the resin of Boswellia carterii Birdw. By the application of the comprehensive spectroscopic data, the structures of the compounds were clarified. The experimental electronic circular dichroism spectra were compared with those calculated, which allowed to assign the absolute configurations. Compounds 5 and 6 possesed a 2, 3-seco tirucallane-type triterpenoid skeleton, which were first reported. Their inhibitory activity against NO formation in LPS-activated BV-2 cells were evaluated. Compound 9 showed appreciable inhibitory effect, with an IC

Synergistic effect on biosynthesis of Panax notoginseng saponins by overexpressing a transcription factor PnbHLH and RNA interference of cycloartenol synthase gene / 中国中药杂志

This study cloned the transcription factor gene PnbHLH which held an open reading frame of 966 bp encoding 321 amino acids. This study constructed the overexpression vector of transcription factor PnbHLH of Panax notoginseng. The combination of PnbHLH overexpression and RNAi of the key enzyme gene PnCAS involved in the phytosterol biosynthesis was achieved in P. notoginseng cells, thus exploring the biosynthetic regulation of P. notoginseng saponins(PNS) by the synergistic effect of PnbHLH overexpression and PnCAS RNAi. The results showed that the PnbHLH transcription factor interacted with the promoters of key enzyme genes PnDS, PnSS and PnSE in the biosynthetic pathway of PNS, and then regulated the expression levels of key enzyme genes and affected the biosynthesis of saponins indirectly. Further study indicated that the synergistic effect of PnbHLH overexpression and PnCAS RNAi was a more effective approach to regulate the biosynthesis of saponins. Compared with the wild type and PnCAS RNAi cells of P. notoginseng, the contents of total saponins and monomeric saponins(Rd, Rb_1, Re, Rg_1 and R_1) were increased to some extent in the cell lines of PnbHLH overexpression and PnCAS RNAi. This indicated that the two ways of forward regulation and reverse regulation of saponin biosynthesis showed superposition effect. This study explored a more rational and efficient regulation strategy of PNS biosynthesis based on the advantages of multi-point regulation of transcription factors as well as the down-regulation of by-product synthesis of saponins.

Chemical Constituents of Pericarps of Zanthoxylum bungeanum / 中国实验方剂学杂志

<b>Objective::To study the chemical constituents of pericarps of <italic>Zanthoxylum bungeanum</italic>. <b>Method::The dried pericarps of <italic>Z</italic>. <italic>bungeanum</italic> were smashed, and then extracted and concentrated in 95%ethanol to obtain the total extract. The total extract was loaded on a silica gel CC, eluted with different polar solvents in sequence, and then concentrated to obtain corresponding parts. The methylene chloride fraction and the <italic>n</italic>-butanol fraction were separated and purified by silica gel column chromatography, Sephadex LH-20 gel column chromatography, ODS column chromatography, semi-preparative HPLC, etc. And their structures were identified based on physicochemical properties and various spectroscopic methods. <b>Result::Fourteen compounds were isolated from the dichloromethane fraction and the n-butanol fraction of the <italic>Z</italic>. <italic>bungeanum</italic> and identified as(1<italic>S</italic>, 3<italic>S</italic>)-1-methyl-1, 2, 3, 4-tetrahydro-<italic>β</italic>-carboline-3-carboxylic acid(<bold>1</bold>), (3<italic>S</italic>)-1, 2, 3, 4-tetrahydro-<italic>β</italic>-carboline-3-carboxylic acid(<bold>2</bold>), apigenin-7, 4′-dimethyl ether(<bold>3</bold>), genkwanin(<bold>4</bold>), lcariside F₂(<bold>5</bold>), breyniaionoside A(<bold>6</bold>), 3-methoxyphenethyl alcohol-4-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-glucopynanoside(<bold>7</bold>), 1-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-glucopyranosyloxy-3-methoxy-5-hydroxybenzene(<bold>8</bold>), orcinol-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-glucopyranoside(<bold>9</bold>), syringin(<bold>10</bold>), 4-[(3<italic>S</italic>)-3-hydroxybutyl]-2-methoxyphenyl-<italic>β</italic>-<italic>D</italic>-glucopyranoside(<bold>11</bold>), (+ )-lyoniresinol-3a-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-glucopyranoside(<bold>12</bold>), 2-methylpropanyl-6-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-apiofuranosyl-<italic>β</italic>-<italic>D</italic>-glucopyranoside(<bold>13</bold>)and(<italic>E</italic>)-6-hydroxy-2, 6-dimethylocta-2, 7-dienoic acid(<bold>14</bold>). <b>Conclusion::All compounds were isolated from <italic>Z</italic>. <italic>bungeanum</italic> for the first time, and compounds <bold>1-4, 12</bold> and <bold>14</bold> were isolated from this genus for the first time.

Research Progress in Population Pharmacokinetics of Multiple Target Tyrosine Kinase Inhibitors in the Treatment of Malignant Tumors / 中国药学杂志

Multiple target tyrosine kinase inhibitors are commonly used in clinical as anti-tumor drugs, which can promote tumor cell apoptosis by inhibiting cell signal transduction, with high selectivity and few side effects. At present, it is widely used in the treatment of non-small cell lung cancer, metastatic renal cancer, thyroid cancer and hematological malignancies. However, the clinical efficacy and pharmacokinetic characteristics of these drugs are affected by many factors, and there are great individual differences. In recent years, the study of population pharmacokinetics is emerging and is widely used in the study of many drugs. In this paper, the pharmacokinetic characteristics and influencing factors of axitinib, imatinib, erlotinib and sunitinib in cancer patients and healthy people were summarized through the retrieval of relevant literature, and then the progress of pharmacokinetic research of tyrosine kinase inhibitors(TKIs) was reviewed. The pharmacokinetic characteristics in different tumor types were analyzed and the related covariates were summarized. The results showed that demographic factors, gene polymorphism, blood biochemical indexes, combined use of drugs and liver and kidney function were important factors affecting metabolism in vivo. Factors such as experimental design and model construction may be the important reasons for the differences in research results. The purpose of this study is to provide a reference for making a reasonable and safe drug therapy plan.

Current situation on the global distribution of hepatitis B virus subtypes / 中华疾病控制杂志

Hepatitis B virus (HBV) infection is an important global public health concern and a major cause of chronic hepatitis, cirrhosis and liver cancer. Many studies have shown that different genotypes and subtypes have significant differences in pathogenicity, thus affecting the disease progression and prognosis of infected individuals. So far, a total of 10 HBV genotypes and more than 40 subtypes have been reported across the world, and these subtypes have shown distinct distribution characteristics. In the present review, we systematically summarized the current situation on the global distribution of HBV genotypes.

Effects of hypothermia on the repolarization duration of ventricular myocytes in rats and its mechanism / 中国应用生理学杂志

To observe the effects of hypothermia on the repolarization duration and the expression of Kir2.1 protein of ventricular myocytes in isolated rat heart and explore the role of Kir2.1 protein. Eighteen healthy adult male Sprague-Dawley rats were randomly divided into three groups (n=6 per group): Control group (C group), 35℃ group (H group), 32℃ group (H group). Langendorff isolated heart models were established. After 15 min 37℃ K-H fluid banlanced perfusion, C group continued to perfuse the K-H solution at 37℃ for 30 minutes, H group continued to perfuse the K-H solution at 35℃ for 30 minutes, H group continued to perfuse the K-H solution at 32℃ for 30 minutes. At 15 min of balanced perfusion (T), and 30 min of continuous perfusion (T), the heart rate,and the MAP in the three layers of the left ventricular anterior wall were recorded, the action potential duration at 50% repolarization (MAPD), the action potential duration at 90% repolarization (MAPD) and transmural dispersion of repolarization(TDR) were calculated. At the same time, the occurrence of arrhythmia was recorded. The expression of Kir2.1 protein was measured by Western blot. The average optical density (AOD) and the distribution of Kir2.1 protein were measured by immunohistochemistry in the ventricular tissue measured by electrophysiology. Compared with T, the heart rate was decreased, MAPD and MAPD were prolonged significantly (P＜0.05), and TDR was increased significantly (P＜0.05) in H group, H group at T. Compared with C group, the HR was decreased, the MAPD was prolonged significantly (P＜0.05), TDR was increased significantly (P＜0.05),the expression and the AOD of Kir2.1 protein were decreased significantly (P＜0.05) in Hgroup, Hgroup at T. Compared with H group, the heart rate of H group was decreased significantly (P＜0.05), MAPD and MAPD were prolonged significantly (P＜0.05), and TDR was increased significantly (P＜0.05) at T. The distribution of Kir2.1 protein in group C was normal, while the distribution of Kir2.1 in H group and H group was disordered. Hypothermia prolonged the ventricular duration of repolarization and increased the dispersion of repolarization. The mechanism is related to the down-regulation the expression of Kir2.1 protein and the disorder of the distribution of Kir2.1 protein.

Recent progress of robots in stomatology / 华西口腔医学杂志

With the development of industrial robot technology, robotics has entered the medical field, and the research and development of new robots for many medical applications have become a significant research direction in global robotics. Robots are widely used in various aspects of dentistry, such as prosthodontics, orthodontics, implants, endodontics, and oral surgery. This article mainly introduces the application of robots in stomatology from the above five aspects.

Efficacy and safety of early initiation of sacubitril-valsartan therapy in patients with acute decompensated heart failure / 中华心血管病杂志

Objective: To assess the efficacy and safety of the initiation of sacubitril-valsartan （ARNI） therapy, as compared with ACEI therapy, after hemodynamic stabilization among patients hospitalized for acute decompensated heart failure （ADHF）. Methods: A total of 199 hospitalized patients for ADHF in our department from January 2017 to June 2019 were included in this retrospective analysis. According to the medication early after hemodynamic stabilization, patients were divided into ARNI group (n=92) and ACEI group (n=107). Among the included patients, 61 patients with newly diagnosed heart failure at the time of admission were also divided into ARNI group (n=30) and ACEI group (n=31) according to the applied medication. Clinical baseline data and follow-up results of enrolled patients were collected through the electronic medical records at admission, outpatient and telephone follow-up. The primary effectiveness observation index was left ventricular ejection fraction (LVEF) and left ventricular end diastolic dimension (LVEDD) measured by echocardiography; the secondary observation index was death from any causes and hospitalization for heart failure. Safety outcomes were the incidences of symptomatic hypotension, worsening renal function, hyperkalemia, and angioedema. Results: The clinical baseline characteristics were similar between ARNI group and ACEI group（all P>0.05）. The duration of follow up was (15.2±6.5) months in all patients enrolled, (12.3±5.0) months in ARNI group, and (18.2±6.5) months in ACEI group. At the end of follow-up, prevalence of an absolute LVEF increase of more than 5% was 48.9% (45/92) in ANRI group and 25.2% (27/107) in ACEI group (P=0.001). Percent of LVEF increase to more than 50% was 17.4% (16/92) in ANRI group and 3.7% (4/107) in ACEI group (P=0.001). Percent of patients with more than 10 mm LVEDD reduction was 14.1% (13/92) in ANRI group and 3.7% (4/107) in ACEI group (P=0.009). All-cause mortality rate was 5.7% (5/88) in ARNI group and 15.3% (13/85) in ACEI group (P=0.038). Rate of re-hospitalization due to heart failure was 50% (46/92) in ARNI group and 71% (76/107) in ACEI group（P=0.002）.The rates of symptomatic hypotension, worsening renal function, hyperkalemia, and angioedema were similar between ARNI group and ACEI group (all P>0.05). In patients with first diagnosed heart failure，percent of LVEF increase to more than 50% was 30% (9/30) in ANRI group and 6.5% (2/31) in ACEI group (P=0.017). Percent of more than 10 mm LVEDD reduction was 26.7%(8/30) in ANRI group and 3.2%(1/31) in ACEI group (P=0.012). Percent of an absolute LVEF increase of more than 5% was 53.3% (16/30) in ANRI group and 51.6% (16/31) in ACEI group (P=0.893). Re-hospitalization due to heart failure was 23.3% (7/30） in ARNI group and 73.3% (11/31) in ACEI group（P<0.01）. Rate of all-cause death tended to be lower in patients receiving ARNI (3.4% (1/29)) as compared to patients receiving ACEI (13.0% (3/23), P=0.197）. Conclusions: Among patients with heart failure with reduced ejection fraction hospitalized for ADHF, the initiation of ARNI therapy after hemodynamic stabilization is associated with a more significant improvement of cardiac remodeling and pump function than ACEI therapy and satisfactory safety. In ADHF patients with first diagnosed heart failure, initiation of ARNI therapy after hemodynamic stabilization can more effectively improve cardiac remodeling and pump function than treatment with ACEI.

Challenges and countermeasures of schistosomiasis control in Hunan Province in the new era / 中国血吸虫病防治杂志

This paper describes the current epidemic characteristics and endemic status of schistosomiasis, analyzes the main challenges of schistosomiasis control and proposes the emphasis and interventions for future schistosomiasis control activities in Hunan Province, so as to provide insights into the elimination of schistosomiasis in Hunan Province.

Implications, spiritual characteristics and practical significance of Chinese schistosomiasis control culture / 中国血吸虫病防治杂志

The culture of schistosomiasis control is specific in the history of Chinese culture. Broadly speaking, the culture of schistosomiasis control is a summary of specific social mood, social consciousness and material culture created by Chinese populations during the progress of schistosomiasis control since the founding of the People’s Republic of China. Narrowly speaking, the culture of schistosomiasis control is the spiritual culture that is jointly created and nurtured by schistosomiasis control workers since the founding of the People’s Republic of China. The spiritual features of Chinese schistosomiasis control culture are characterized by the patriotism and care about the people, the matter-to-fact attitude, the pioneering and enterprising spirit, and the spirit of sacrifice and dedication. The ultimate goal of the research on the culture of schistosomiasis control is to facilitate the achievement of the strategic goal of Healthy China 2030 as scheduled, accelerate the progress towards elimination of schistosomiasis, and to promote the sustainable development of schistosomiasis control in China.

3, 4-seco-Labdane diterpenoids from the leaves of Callicarpa nudiflora with anti-inflammatory effects / 中国天然药物

Four new 3, 4-seco-labdane diterpenoids, nudiflopenes J-M, were isolated from the leaves of Callicarpa nudiflora along with six known compounds. The structures of these diterpenoids were determined by comprehensive spectroscopic analysis. All the isolated compounds were evaluated for their inhibitory effects on NO production in LPS-stimulated RPMs and RAW264.7 cells. The results suggest that nudiflopenes J-M and other four known compounds showed significant inhibitory effects against NO production comparable to the positive control dexamethasone.

Genotypic and Phenotypic Analysis of αβ-Thalassemia in Children / 中国实验血液学杂志

OBJECTIVE@#To analyze the genotype and hematological characteristics of children with αβ-thalassemia in Shenzhen area of China.@*METHODS@#The erythrocyte parameters and hemoglobin components of the children were determined by blood routine examination and capillary electrophoresis (CE). Reverse dot blot (RDB) -polymerase chain reaction (PCR) was used to determine gene mutations in α- and β-thalassemia children. The Gap-PCR was used to determine the gene deletion of α-thalassemia children，while specimens suspected HKαα were determined with nested PCR.@*RESULTS@#Total of 29 complex genotypes were detected from 74 cases of αβ-thalassemia, among which 1 case was determined as β-thalassemia with αααanti4.2/αα and 5 cases were double heterozygous β-thalassemia combining α-thalassemia with intermediate phenotype. 1 case of β-28/βcap+40-43 double heterozygotes combined with --/αα and the other 62 cases were characterized by light β-thalassemia, 2 cases ofβCAP+40-43/βN with --/αα showed light α-thalassemia.@*CONCLUSION@#The genotypes of αβ-thalassemia in Shenzhen area of China are complex and diverse. The common complex genotypes are similar to those of simple β-thalassemia. If the genotype and phenotype are not consistent, the existence of rare genotype should be considered.

Pharmacokinetic Features of Reactive Sulfide in Plasma of Rats After Oral Administration of Cinnabaris by Using HPLC Coupled with Pre-column Derivatization / 中国中医药信息杂志

Objective To study the pharmacokinetic features of reactive sulfide in rats after oral administration of Cinnabaris. Methods An HPLC coupled with precolumn derivatization method was developed for the pharmacokinetic features study on reactive sulfide in rats after oral administration of Cinnabaris. Results Good linearity (r>0.99) was found for reactive sulfide in plasma in the concentration range of 0.25–15 μmol/L (r>0.99). The LOQ and LOD of the method were 0.1 μmol/L and 0.02 μmol/L, respectively. The intra- and inter-day precision was less than 4.4% and 3.5% respectively, and the accuracy was -9.9%–6.0%. The average recovery rate was 74.9%. 0.6 g/kg Cinnabaris was given the rats for gavage, and the time-course pharmacokinetics parameters were as follows:Cmax(1.33±0.13) μmol/L, tmax(150±34) min, t1/2(323±62) min, AUC0-∞ (5743±297) ng/mL?h. Conclusion A sensitive, robust and accurate precolumn derivatization-HPLC method for the determination of plasma reactive sulfide is developed and validated. The method is successfully applied in the pharmacokinetic features study on reactive sulfide in plasma of rats after administration of Cinnabaris.

Simultaneous determination of flavonol glycoside and its major metabolites by LC-MS/MS in rat plasma / 药学学报

Flavonol glycoside is in clinical trials for treatment of hyperlipidemia. An accurate and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of flavonol glycoside (M0), aglycone (M1) and glucuronide conjugate (M2) in rat plasma. d6-Flavonol glycoside was used as internal standard (IS). After extraction from the plasma by protein precipitation, the analytes and internal standard were separated on a XDB C18 column (50 mm×4.6 mm, 1.8 μm) using a gradient elution procedure. The mobile phase consisted of methanol and water (0.2% formic acid) at a flow rate of 0.6 mL·min−1. The total run time was 4.5 min. Positive electrospray ionization was performed using multiple reaction monitoring (MRM) with transitions of m/z 461.3 → m/z 299.1 for M0, m/z 299.1 → m/z 283.1 for M1, m/z 475.0 → m/z 299.1 for M2, and m/z 467.3 → m/z 305.1 for d6-flavonol glycoside. The method was validated and successfully applied to the pharmacokinetics study of flavonol glycoside in SD rats which were given flavonol glycoside (30 mg·kg−1) by gavage. The Cmaxof M0 is (341 ±106) ng·mL−1 and AUC0−t is (1 960 ±725) h·ng·mL−1, while the Cmaxof M2 is (1 720 ±843) ng·mL−1and AUC0−t is (8 510 ±2 920) h·ng·mL−1. The results suggest that flavonol glycoside existed mainly in the form of M0 and M2 in rats. After flavonol glycoside being hydrolyzed by the intestinal flora, it was absorbed in the form of aglycone and further metabo­lized to M2 after the first-pass effect. In this paper, the main metabolites of flavonol glycoside in rat plasma were determined for the first time, which provided a basis for the design of clinical pharmacokinetic experiment.

Functional analysis of a chitinase gene PnCHI1 from Panax notoginseng / 中国中药杂志

Chitinases, a glycosidase enzyme that hydrolyzes chitin to N-acetylglucosamine, are widely found in plant cells, and they are an important part of plant antifungal defense system. The function of a Panax notoginseng chitinase gene PnCHI1 was characterized in this paper. Expression vector of PnCHI1 was constructed and transiently expressed in onion epidermal cells, and laser scanning confocal microscopy demonstrated that PnCHI1 was localized in the cell wall. Prokaryotic expression vector of PnCHI1 was also constructed, and recombinant protein of PnCHI1 was induced and purified. In vitro antibacterial assay showed that recombinant PnCHI1 protein had strong inhibitory activity on the mycelium growth of Fusarium solani, F. oxysporum and F. verticillioide. The function of PnCHI1 was further verified by reverse genetics. PnCHI1 expression vector was transferred into tobacco by Agrobacterium tumefaciens and expression of PnCHI1 was confirmed by qRT-PCR. It was found by leaf inoculation experiment that resistance of transgenic tobacco to F. solani was significantly increased. It is conclnded that: PnCHI1 is a chitinase localized in the cell wall, which inhibits several fungi which cause the root rot disease of P. notoginseng. Overexpression of this chitinase gene in tobacco greatly increased resistance to F. solani. PnCHI1 may be an important resistance gene in P. notoginseng that participates in the defense against root rot disease.