Preparation and polarization activity research of astragalus polysaccharide-superparamagnetic iron oxide nanocomposite / 药学学报

Size and surface modification are the two key factors affecting the effect of macrophages polarization induced by superparamagnetic iron oxide nanoparticles (SPIONs). The smaller the particle size, the better the polarization effect of SPIONs. Besides, the reasonable SPIONs surface modification method can also be used to enhance the polarization effect. In this study, SPIONs was prepared by solvothermal method and optimized by Box-Benhnken center combination design and response surface method. Furthermore, astragalus polysaccharide-superparamagnetic iron oxide nanocomplex (APS-SPIONs) was successfully constructed by EDC/NHS esterification method. The structure of APS-SPIONs was confirmed by dynamic light scatter and infrared spectrometer, and the contents of iron and polysaccharide were characterized by spectrophotometry. The effect of APS-SPIONs on inducing mouse macrophages RAW264.7 polarization was investigated by flow cytometry. The RAW264.7 macrophages-HepG2 human hepatoma cancer cells Transwell co-culture system was established to investigate APS-SPIONs improve anti-tumor function of macrophages in vitro, and the proliferation activity of APS-SPIONs on RAW264.7 detected by cell counting kit-8 (CCK-8) method. The results showed that the average particle size and zeta potential of APS-SPIONs were (82.93 ± 1.47) nm and (-24.00 ± 0.47) mV. Polysaccharide and Fe content were 8.69% and 7.04%, respectively. APS-SPIONs effectively induced the polarization of RAW264.7 into M1 type in vitro, improving the anti-tumor ability of macrophages in a co-culture system, without effecting the proliferation of macrophages. Our study provides a drug development strategy and preliminary research results to educate macrophages and reshape the tumor immune microenvironment to achieve tumor-killing effects.

Factors affecting osteoporosis among physical examination populations aged over 35 years in urban areas of Hangzhou City / 预防医学

Objective@#To investigate the development of osteoporosis (OS) and its influencing factors among physical examination populations aged over 35 years in urban areas of Hangzhou City, so as to provide insights into OP prevention.@*Methods@#Subjects aged over 35 years that underwent physical examinations in Wenhui Street Community Health Service Center of Gongshu District, Hanghzhou City during the period between April and July, 2022 were enrolled. Subjects' demographic characteristics and physical examination data were collected, and the bone mineral density and serum vitamin D levels were measured. The factors affecting the development of OP were identified using a logistic regression model.@*Results@#A total of 1 561 subjects were recruited, including 616 males (39.46%) with a median (interquartile range) age of 62 (18) years, and 945 females (60.54%) with a median (interquartile range) age of 62 (19) years. The prevalence of OP was 43.69% among the study subjects. Multivariable logistic regression analysis identified women (OR=1.367, 95%CI: 1.105-2.979) and increased age (OR=1.057, 95%CI: 1.044-1.069) as risk factors for OP and elevated serum 25-hydroxy-vitamin D levels as a protective factor for OP (OR=0.969, 95%CI: 0.954-0.985).@*Conclusions@#The prevalence of OP was 43.69% among physical examination populations aged over 35 years in urban areas of Hangzhou City, and gender, age and serum 25-hydroxy-vitamin D were factors affecting the development of OP.

Therapeutic Effect of Canagliflozin on Nephrotic Syndrome and Its Ultrasonic Evaluation / 中山大学学报(医学科学版)

ObjectiveTo investigate the therapeutic effect of antidiabetic drug canagliflozin （CGLZ） on adriamycin-induced nephrotic syndrome （NS） in rats， and the evaluation of contrast-enhanced ultrasound （CEUS） combined with color Doppler flow imaging （CDFI） during the treatment. MethodsA total of 56 male SD rats were randomly divided into normal group （NG）， model group （MG）， prednisone （PAT） group （PG）， low-dose single CGLZ group （LSCG）， high-dose single CGLZ group （HSCG）， low-dose CGLZ + PAT group （LUCG） and high-dose CGLZ + PAT group （HUCG）， with 8 rats in each group. The NS model in rats was induced by injecting adriamycin twice into the tail vein， and then the NS rats were treated by intragastric administration daily for 6 weeks with reference of PAT. Twenty-four hour urine total protein （24 h-UTP） was assessed one day before the start of oral administration and at the end of 2， 4 and 6 weeks after oral administration， respectively. CDFI and CEUS were performed on the right renal artery at the end of 6 weeks after oral administration， and the blood of abdominal aorta was taken for serological test the next day. ResultsCompared with those detection index of NG rats， the 24-hour UTP of MG rats increased （P＜0.01）， the serum ALB decreased and TG， TC， LDL increased （P＜0.01）， and CDFI shows that RRCT was thinner （P＜0.01） and the renal artery blood flow indicators RA-PI， RA-RI， RA-S/D all increased （P＜0.05）， and CEUS image shows that the TIC curve parameters TTP， AT， AUC all increased and DPI decrease in MG rats （P＜0.01）. After drug treatment， compared with those detection index of MG rats， 24 h-UTP decrease in LSCG after 2 weeks （P＜0.01）， and decrease significantly in all drug groups after 6 weeks （P＜0.01）； the serological test results show that the serum ALB in all CGLZ groups increased （P＜0.05）， TG decrease in LSCG （P＜0.01）， TC and LDL also decrease in LUCG after 6 weeks （P＜0.05）； CDFI shows that the RRCT thinning degree in all CGLZ is reduced （P＜0.01）， and the RA-PI in LSCG， RA-RI in PG， and RA-S/D in PG， LSCG， HSCG and LUCG rats all decreased （P＜0.05）； CEUS shows that the TTP， AT and AUC of renal TIC curve in drug treatment groups all decreased （P＜0.01）， and the DPI in PG， HSCG， LUCG and HUCG rats increased （P＜0.01）. ConclusionsCGLZ has the effect of treating NS， and the small dose is the best. CEUS combined with CDFI can be used to evaluate the renal morphology and hemodynamic changes of NS model rats before and after drug treatment， which is helpful to guide clinical application.

Clinical characteristics and guideline compliance analysis of chronic obstructive pulmonary disease patients with initial triple therapy in real-life world / 中国医师杂志

Objective:To observe the clinical characteristics and guideline compliance of chronic obstructive pulmonary disease (COPD) patients with initial triple therapy in real-life world.Methods:This study is a cross-sectional study. The subjects of the study were COPD patients admitted to 13 hospitals in Hunan Province and Guangxi Zhuang Autonomous Region from December 2016 to December 2021. The initial treatment was triple inhaled drugs. The data collected included gender, age, diagnosis, body mass index (BMI), history of acute exacerbation (AE) in the past year, pulmonary function, COPD Assessment Test (CAT) score, modified British Medical Research Council Dyspnea Questionnaire (mMRC), inhaled drugs and other indicators. The characteristics and differences of COPD patients before and after 2020 were analyzed.Results:7 184 patients with COPD were enrolled in this study, including 2 409 COPD patients treated with initial triple therapy, accounting for 33.5%(2 409/7 184). Taking January 1st, 2020 as the cut-off point, 1 825 COPD patients (75.8%) received initial treatment with triple inhaled drugs before 2020 and 584 patients (24.2%) after 2020 were included in this study. Compared with COPD patients before 2020, the COPD patients after 2020 had higher FEV 1% [(40.9±15.5 )% vs (39.3±15.5)%, P=0.040], lower CAT [(15.8±6.5)point vs (17.5±6.2)point, P<0.001], less AE in the past year [1(0, 2)times vs 1(0, 2)times, P=0.001] and higher rate of non-AE [255(43.7%) vs 581(37.1%), P=0.006]. In addition, before 2020, patients with COPD were mainly treated with open triple drugs (1 825/1 825, 100%); after 2020, 306 patients (52.4%) received open triple inhaled drugs, and 278 patients (47.6%) received closed triple inhaled drugs. Conclusions:In real-life world, most of patients with COPD treated with triple therapy have severe lung function, obvious symptoms and high risk of acute exacerbation. The real-world prescribing of triple therapy in patients with COPD does not always reflect recommendations in guidelines and strategies, and overtreatment is common. After 2020, prescribing triple therapy for COPD patients is more positive and worse consistency with guideline.

Status and compliance with the guideline of inhaled corticosteroids use in patients with chronic obstructive pulmonary disease / 中国医师杂志

Objective:To understand the use of inhaled corticosteroids (ICS) in patients with chronic obstructive pulmonary disease (COPD) in the real world and analyze its compliance with the guidelines.Methods:This study is a multicenter, cross-sectional study. 1 051 COPD patients who were treated in the Second Xiangya Hospital of Central South University, the First Affiliated Hospital of Shaoyang College and Zhuzhou Central Hospital from January 2020 to March 2022 were collected. The general information, drug use, types of exposure risk factors, acute exacerbation (AE) in the past year, the scores of the modified British Medical Research Council Dyspnea Questionnaire (mMRC), COPD Assessment Test (CAT), pulmonary function, blood routine of patients were collected. The status of ICS use in COPD patients, the clinical characteristics and guideline compliance of non-ICS users and ICS users were analyzed.Results:Among 1 051 patients with COPD, ICS was used in 490 cases (46.6%) and was not used in 561 cases (53.4%). ICS use was associated with relapse, frequent AE, severe AE, Global Initiative for Chronic Obstructive Pulmonary Disease (GOLD) grade 2 or above, GOLD D group, mMRC score, bronchial asthma, and blood eosinophils (EOS) (all P<0.05). Among 1 051 patients, 583(55.5%) were newly treated, 222(38.1%) were newly treated with ICS, and 361(61.9%) were not treated with ICS. ICS use in newly treated patients was associated with frequent AE, severe AE in the past year, GOLD grade 2 to 3, GOLD B and D group, mMRC score, bronchial asthma, and blood EOS (all P<0.05). Conclusions:Nearly half of patients with COPD are treated with ICS, and patients with ICS use had a higher risk of AE, more severe symptoms, higher blood EOS, and higher rates of asthma. However, there still exists the phenomenon of overuse of ICS.

Analysis of treatment for 360 critically ill pregnant and parturient women in intensive care unit / 中华危重病急救医学

Objective:To analyze the clinical characteristics and outcomes of critically ill pregnant and parturient women in intensive care unit (ICU), and to provide clinical experience for the subspecialty construction of critical obstetrics.Methods:The clinical data of critically ill pregnant and parturient women admitted to the department of critical care medicine, the Second Affiliated Hospital of Kunming Medical University from January 2011 to December 2019 were collected. The main reasons for maternal transfer to ICU, the causes of maternal death, and organ support measures, etc. were summarized.Results:A total of 39 567 critically ill pregnant and parturient women were admitted to the department of obstetrics in our hospital, and 360 were transferred to ICU, with an average ICU transfer rate of 0.91%. Since 2016, the number of obstetric admissions, the number of ICU transfers and the ICU transfer rate had increased significantly. The average age of severe maternals admitted to ICU was (30.9±5.7) years old. The average acute physiology and chronic health evaluation Ⅱ(APACHEⅡ) score was 7 (4, 10). The average length of ICU stay was 1 (1, 2) day. The average ventilator duration was 9.0 (3.0, 17.5) hours. The main delivery mode of pregnant women in ICU was cesarean section (84.72%). Forty-eight patients (13.33%) underwent hysterectomy, of which 42 (87.5%) due to postpartum hemorrhage. The top 3 causes of ICU admission were severe postpartum hemorrhage [36.94% (133/360)], hypertensive disorders of pregnancy [21.67% (78/360)], pregnancy with cardiac disease [15.00% (54/360)]. The leading cause of postpartum hemorrhage in women transferred to ICU was placental abnormality [63.98% (103/161)], followed by uterine atony [28.57% (46/161)]. The average blood loss was (4 019±2 327) mL within 24 hours after delivery, and the number of women who underwent hysterectomy due to postpartum hemorrhage decreased year by year. During the study period, there were 2 maternal deaths, which were indirect obstetric deaths, 3 cases were discharged against-advice (expected death), including 1 indirect death and 2 direct obstetric death; the mortality in ICU was 1.39% (5/360).Conclusions:The most common reasons for pregnant and parturient women to be admitted to ICU were severe postpartum hemorrhage and hypertensive disorders of pregnancy. The leading cause of postpartum hemorrhage was placental problem. Indirect obstetric deaths exceeded direct obstetric deaths, mainly due to pregnancy complicated with cardiac disease and severe pneumonia. ICU has become an important battlefield for rescuing critically ill maternal and an important guarantee for reducing the maternal mortality.

Expression and promoter methylation status of leucine rich repeat containing 55 in pancreatic carcinoma tissue and the clinical value / 中华胰腺病杂志

Objective:To detect the mRNA expression and methylation status of leucine rich repeat containing 55(LRRC55) gene in pancreatic carcinoma tissues, and discuss the clinical value.Methods:Resected pancreatic ductal adenocarcinoma and normal adjacent specimens from 37 patients admitted in General Surgery of First Affiliated Hospital of Naval Medical University were collected from May 2019 to May 2021. Another two normal pancreas specimens and two blood samples from healthy adults were also collected. All patients′ age, gender, tumor location, tumor size, tumor differentiation, TNM staging, lymphatic metastasis, CEA and CA19-9 level were recorded. Bisulfite treatment of genomic DNA and sequencing analysis was used to study methylation patterns in CpG islands of the promoter for LRRC55 gene in fresh tissues from 2 pancreatic adenocarcinoma and adjacent tissues, 2 normal pancreatic tissues, 2 pancreatic cancer cell lines (PaTu8988 and ASPC1). LRRC55 mRNA in 35 pancreatic adenocarcinoma and adjacent tissues was detected by real-time quantitative PCR and the correlations with clinical parameters were analyzed.Results:CpG islands of LRRC55 in pancreatic adenocarcinoma tissues and pancreatic cancer cell lines was highly methylated and the mean methylation rate was 53% and 71%, respectively; while LRRC55 gene in pancreatic adjacent tissues and normal pancreatic tissues was lowly methylated, and the mean methylation rate was 8% and 11%. The relative expression in the pancreatic adenocarcinoma tissues and the paired adjacent normal tissues was 0.21 (0.02, 1.00 ) and 0.98 (0.33, 3.66 ), respectively; the former was significantly lower than the later and the difference was statistically significant ( P=0.003). Correlation analysis showed that LRRC55 mRNA expression level was related to tumor differentiation and CEA, but not correlated with patients′ age, gender, tumor location and size, CA19-9 level, lymphatic metastasis and TNM staging. Conclusions:Pancreatic cancer tissue and cell lines had abnormal methylation of LRRC55 gene; LRRC55 gene hypermethylation was related with its lower mRNA expression level in pancreatic cancer, which was correlated with the tumor differentiation and CEA level. LRRC55 may be a potential suppressor gene for pancreatic cancer.

Construction and clinical effects of endocrinology nursing subspecialty group / 中国实用护理杂志

Objective:To construct endocrinology nursing subspecialty model and explore its clinical effect.Methods:In December 2018, the organization structure of endocrinology nursing subspecialty was constructed in the Drum Tower Hospital Affiliated of Nanjing University Medical School and applied in clinic. In this model, the data of 2018 were taken as the data before application and the data of 2020 were taken as the data after application. The comprehensive ability of nurses, nurse satisfaction, related nursing workload and scientific research ability of nurses were compared before and after the application of the model.Results:After the application of subspecialty nursing mode, nurses′ comprehensive ability score was (92.00 ± 2.36) points. Compared with (84.25 ± 3.24) points before implementation, the difference was statistically significant ( t=-9.46, P<0.01); nurses′ satisfaction evaluations including specialty development (7.92 ± 1.41), self-quality improvement (8.00 ± 1.69), work pressure (6.42 ± 2.67), salary and welfare (3.96 ± 0.85), compared with (5.79 ± 2.31), (6.17 ± 2.82), (8.33 ± 1.50), (2.88 ± 1.59) before implementation, the difference was statistically significant ( t values were -3.86--2.73, all P<0.05). The annual workload of related nursing increased and the scientific research ability of nurses was improved. Conclusions:The application of endocrinology nursing subspecialty mode is beneficial to improve nurses′ comprehensive ability of clinical work, improve the level of specialized nursing, improve the quality of nursing service and promote the improvement of economic benefits, which is worthy of clinical promotion.

Observation of binocular visual quality after single-focal and multifocal intraocular lens with different types of implantation / 国际眼科杂志(Guoji Yanke Zazhi)

AIM: The clinical outcomes of unilateral single-focal intraocular len(SIOL), contralateral implanted multifocal IOL(MIOL)and the SIOL was implanted in binoculus were compared.METHODS: There were 60 cases with 120 eyes age-related cataract patients in January 2019 to January 2021 underwent phacoemulsification and IOL implantation in Chengdu Aier Eye Hospital. The SIOL has been implanted in the dominant eyes, all patients were divided into three groups according to the types of IOL implanted in the contralateral non-dominant eyes, among them, there were 36 eyes of 18 cases in group A with non-dominant eyes implanted MIOL(SBL-3); 38 eyes of 19 cases in group B were implanted MIOL(SN6AD1)in non-dominant eyes. SIOL was implanted in all 46 eyes of 23 cases of control group. After operation at 3mo,the results of binocular vision and visual quality of the three groups were evaluated and compared.RESULTS: After operationat 3mo, there was no difference in the uncorrected distance vision and corrected distance vision, uncorrected medium vision and corrected near vision among the three groups(P<0.05).The uncorrected near visual acuity and corrected intermediate visual acuity of both eyes in groups A and B were significantly improved in both groups compared with the control group(P<0.05). The scores of Catquest 9SF-CN scale showed that the quality of life of patients in group A and group B(11.11±1.323, 11.89±1.883 scores)was better than that in the control group(14.65±1.722 scores, both P<0.05). The rate of lens removal in group A, B and control group were 88.9%, 84.2% and 39.1%, respectively, and the rate of lens removal in group A was significantly higher than that in the control group(P<0.0167).CONCLUSION: Dominant eye implantation of SIOL in patients with cataract and contralateral non-dominant eye implantation of MIOL(SBL-3/SN6AD1)can obtain better full-range visual acuity than binoculus, less postoperative adverse visual symptoms, and higher patient disengagement rate and satisfaction.

Efficacy and safety of dupilumab in the treatment of 21 cases of bullous pemphigoid: a retrospective study / 中华皮肤科杂志

Objective:To retrospectively analyze the efficacy and safety of dupilumab in the treatment of bullous pemphigoid (BP) .Methods:Clinical data were collected from BP patients who received injections of dupilumab at an initial dose of 600 mg followed by an every-2-week regimen at a dose of 300 mg (the frequency of injections could be increased if necessary) in Department of Dermatology, Peking University First Hospital from October 2020 to October 2021, and their clinical manifestations and changes in laboratory indices were analyzed.Results:A total of 21 BP patients treated with dupilumab were included in this study. Nineteen (90.5%) patients achieved complete or marked disease control after 2-week treatment with dupilumab; 12 patients were followed up for 16 weeks, and all maintained complete disease control at 16 weeks. All patients had a bullous pemphigoid disease area index (BPDAI) score of 122.5 ± 51.1 points at baseline, which decreased to 30.6 ± 27.4 points after 2-week treatment with dupilumab ( t = 8.53, P < 0.001) , and continued to decrease to 12.7 ± 9.1 points after 4-week treatment ( t = 9.73, P < 0.001) . Pruritus was markedly relieved in all the 21 patients within 4-week treatment with dupilumab. Among 10 patients with elevated eosinophil counts at baseline, the eosinophil counts markedly decreased in 9 after treatment. The serum IgE level was elevated in 7 patients at baseline, which markedly decreased in 6 after treatment. Viral conjunctivitis occurred in 1 (4.8%) patient, and no adverse reactions were observed in other patients. Conclusion:Dupilumab is effective in the control of BP and relief of pruritus, with a favorable safety profile.

Clinical efficacy of mucopolysaccharide polysulfate cream in combination with sertaconazole nitrate cream in the treatment of scaly hyperkeratotic tinea pedis / 中华皮肤科杂志

Objective:To investigate clinical efficacy of mucopolysaccharide polysulfate cream combined with sertaconazole nitrate cream in the treatment of scaly hyperkeratotic tinea pedis.Methods:From March 2019 to January 2020, 100 patients with scaly hyperkeratotic tinea pedis were enrolled into this study, and randomly and equally divided into 2 groups by using a random number table: control group treated with topical sertaconazole nitrate cream alone at a dose of 0.5-1 g twice a day; combined group treated with topical mucopolysaccharide polysulfate cream at a dose of 0.5-1 g followed by topical sertaconazole nitrate cream at a dose of 0.5-1 g 30 minutes later, which were performed twice a day. The treatment lasted 4 weeks. The time to clinical symptom relief, efficacy and incidence of adverse reactions were compared between the two groups. Dermatology life quality index (DLQI) was assessed at 0, 2 and 4 weeks after the start of treatment. Two-independent-sample t test, repeated measures analysis of variance and chi-square test were used for statistical analysis. Results:After treatment, the time to pruritus relief and that to desquamation improvement were 6.05 ± 1.98 and 12.03 ± 3.92 days respectively in the combined group, which were significantly shorter than those in the control group (8.39 ± 2.11, 15.11 ± 4.05 days, t = 5.72, 3.86, respectively, both P < 0.001) . During the 4 weeks of treatment, DLQI scores gradually decreased in both the 2 groups (all P < 0.001) , which were significantly lower in the combined group than in the control group at weeks 2 and 4 (both P < 0.001) . After 4-week treatment, the total response rate was 98% (49/50) in the combined group, significantly higher than that in the control group (82%, 41/50; χ2= 7.11, P= 0.007) . There was no significant difference in the incidence of adverse reactions between the two groups ( P > 0.05) . Conclusion:Mucopolysaccharide polysulfate cream can improve the efficacy of sertaconazole nitrate cream in the treatment of scaly hyperkeratotic tinea pedis.

Active Constituents and Mechanism of Epimedii Folium Against Liver Cancer： A Review / 中国实验方剂学杂志

Liver cancer is a worldwide malignant tumor with an increasing incidence by years. At present， it is facing the predicament of poor prognosis and lack of effective therapeutic drugs. Epimedii Folium is a well-known traditional Chinese medicine with a long history， and exiting clinical and pharmacological studies show that it can be used in clinical treatment of liver cancer. According to reports， Epimedii Folium polysaccharides （EPS）， C-8-isopentenyl substituted flavonoids and their glycosides （icaritin， icariin， baohuoside Ⅰ， epimedin C） have good anti-liver cancer activity. They are the main active ingredients of Epimedii Folium against liver cancer. The data which comes from in vitro and in vivo studies suggests flavonoids in Epimedii Folium demonstrate anti-liver cancer activity through various mechanisms， including inhibiting hepatoma cells proliferation， promoting hepatoma cells apoptosis， improving tumor immunosuppression microenvironment， inhibiting hepatoma cells immune escape， invasion and migration， reversing hepatoma cells resistance， suppressing hepatocellular carcinoma initiation cells and regulating the immunity of the body. While EPS play an anti-hepatocellular carcinoma role mainly through the regulation of immunity. Epimedii Folium exerts good anti-liver cancer effects with multiple components， multiple targets， and multiple pathways， which makes it a valuable anti-liver cancer drug. However， the comprehensive analysis of related aspects is still lacking. Therefore， this study briefly reviewed the anti-hepatocellular carcinoma active ingredients of Epimedii Folium and their mechanisms. In addition， in the process of literature review， it was found that the anti-liver cancer studies of Epimedii Folium mainly focused on a few components and the studies elucidating the active constituents and mechanism of Epimedii Folium against liver cancer on the whole level were insufficient. Based on these questions， the study also proposed corresponding suggestion to provide reference for the further study of substance basis， clinical application and rational development of Epimedii Folium against liver cancer.

Research Progress on Compatibility Mechanism of Coptidis Rhizoma-Euodiae Fructus： A Review / 中国实验方剂学杂志

Herb pair， a common form of compounding in Chinese medicinal prescriptions， reflects the experience of pharmacists in clinical medication in the past. It is characterized by simple composition while has the basic characteristics of Chinese medicine compounding. The combination of two medicinal herbs can enhance effect or reduce toxicity. Coptidis Rhizoma （CR） has the effects of clearing heat， drying dampness， purging fire， and removing toxin. Euodiae Fructus （EF） is acrid， bitter， and hot-natured， which can not only warm the Yang Qi in spleen and stomach to dissipate cold and relieve pain， but also descend stomach Qi and prevent vomiting. Furthermore， it can warm the liver and kidney. CR and EF form a typical cold-heat herb pair， which oppose and yet also complement each other. Specifically， their cold and heat natures interact with each other to clear liver fire， harmonize stomach for descending adverse Qi， relieve depression， and dissipate mass. CR clears the intestine and stops dysentery， while EF warms the middle and promotes the circulation of Qi. The combination of them can thus clear heat， dry dampness， and relieve pain. Modern pharmacological studies have demonstrated that CR-EF has not only significant efficacy against digestive system diseases but also good anti-cancer， anti-inflammatory， anti-ulcer， and lipid-lowering activities. Therefore， the article summarized the effect enhancement and toxicity reduction of the herb pair at the levels of cellular molecule， isolated organ， and whole animal， and clarified the mechanism of its pharmacological action. It will provide a theoretical basis for further development and clinical use of the herb pair.

Baicalein Mediated FAK Protein Regulates PI3K/Akt Signaling Pathway to Inhibit Proliferation and Migration of Gastric Cancer HGC-27 Cells / 中国实验方剂学杂志

ObjectiveTo study the possible molecular mechanism of baicalein （BAI）-mediated focal adhesion kinase （FAK） in the regulation of phosphatidylinositol 3-kinase/protein kinase B （PI3K/Akt） signaling pathway to inhibit the proliferation and migration of gastric cancer HGC-27 cells. MethodThe gastric epithelial GES-1 cells and gastric cancer HGC-27 cells were respectively treated with BAI （0， 5， 15， 25， and 50 μmol·L-1） for 48 h， and then methyl thiazolyl tetrazolium （MTT） assay was adopted to detect effect of BAI on cell proliferation. Western blot （WB） was employed to detect the expression of FAK and the proteins related to epithelial-mesenchymal transition （EMT） and PI3K signaling pathway after intervention with different concentrations of BAI. The HGC-27 cells stably overexpressing FAK were constructed with lentivirus-mediated transfection technique， and the transfection of FAK was detected through WB and green fluorescent protein （GFP）. The cells were divided into empty vector （NC） group， BAI group， FAK overexpression group， and BAI-treated FAK overexpression group， and cell proliferation activity was detected by MTT assay. The colony formation and cell migration were observed via colony formation assay and Transwell migration assay， respectively. The expression of proteins involved in EMT and PI3K signaling pathways were detected by Western blot. ResultCompared with the NC group， BAI （15， 25 and 50 μmol·L-1） inhibited the proliferation of HGC-27 cells in a dose-dependent manner （P<0.05， P<0.01） while did not affect that of GES-1 cells. BAI （5， 15 and 25 μmol·L-1） down-regulated the expression level of p-FAK （P<0.05， P<0.01）. Compared with NC group， FAK overexpression group showed up-regulated expression level of FAK in HGC-27 cells. The HGC-27 cells in both NC group and FAK overexpression group had green fluorescence. Compared with NC group， BAI inhibited the growth， colony formation， and migration， while FAK overexpression promoted those of HGC-27 cells. The treatment of FAK overexpression group with BAI inhibited the enhancement of cell proliferation and migration （P<0.05）. WB showed that compared with NC group， BAI （15， 25 μmol·L-1） significantly up-regulated the expression of E-cadherin protein and down-regulated that of Vimentin， Snail， p-PI3K， and p-Akt protein in HGC-27 cells （P<0.05， P<0.01）. Compared with NC group， FAK overexpression group showed down-regulated expression of E-cadherin， up-regulated expression of p-FAK， Vimentin， and Snail， and increased ratios of p-FAK/FAK， p-PI3K/PI3K and p-Akt/Akt （P<0.05）. This phenomenon would be reversed after BAI treatment. ConclusionBAI can affect the proliferation and migration of gastric cancer HGC-27 cells by mediating FAK to regulate PI3K/Akt signaling pathway.

Modern research thoughts and methods on bio-active components of TCM formulae / 中国天然药物

TCM formulae are the important guidances for clinical application of traditional Chinese medicines, which follow the principles of diagnosis and treatment in TCM. Elucidating the bio-active components of TCM formulae is the key to the modernization and internationalization of traditional Chinese medicines. With the rapid development of modern instruments and technology, many new theories, methods and strategies are emerging, which upgrade the research of TCM formulae into a higher level. Only when the medicinal efficacy, bio-active components, function mechanism of TCM formulae are understood, we can guarantee TCM safety and quality control. In this paper, we summarized the latest modern research thoughts and methods on bio-active components of TCM formulae including formula decomposition study, serum pharmacology and serum pharmacochemistry, association analysis, biochromatography, network pharmacology, metabolomics and proteomics, so as to provide reference for the research and development of TCM in the future.

Research on Q-markers of Polygoni Perfoliati Herba based on analytic hierarchy process-entropy weight method and fingerprints / 中国中药杂志

The potential quality markers(Q-markers) of Polygoni Perfoliati Herba were studied based on analytic hierarchy process(AHP)-entropy weight method(EWM), network pharmacology, and spectrum-effect relationship analysis. The AHP-EWM was used for quantitative identification of the Q-markers. To be specific, AHP was applied for the weight analysis of the validity, testability, and specificity of the first-level indexes, and EWM for the analysis of the second-level indexes supported by literature and experimental data. Based on literature and network pharmacology, the validity analysis was to study the component-target-disease-efficacy network, and select the components with the strongest correlation with the efficacy of clearing heat and removing toxin, diuresis and alleviating edema, and relieving cough. For the testability analysis, the high performance liquid chromatography(HPLC) and literature research were used to determine the 10 components in Polygoni Perfoliati Herba, and the fingerprints of Polygoni Perfoliati Herba were established at the same time. The specificity analysis was based on the statistics of the number of plants in which the components existed. Thereby, the 11 compounds: quercetin, oleanolic acid, ellagic acid, gallic acid, kaempferol, rutin, esculetin, quercetin-3-O-glucuronide, ursolic acid, protocatechuic acid, and ferulic acid, were identified as potential Q-markers. The 11 compounds were identified to have high anti-inflammatory activity, indicating that the 11 Q-markers may be the functional material basis. The result in this study is expected to serve as a reference for the quality control of Polygoni Perfoliati Herba.

Acetylation of Rehmannia glutinosa polysaccharides and antioxidant activity of acetylated derivatives / 中国中药杂志

This study aims to acetylate Rehmannia glutinosa polysaccharides by acetic anhydride method, optimize process parameters and evaluate their antioxidant activity. With the degree of substitution(D_s) as a criterion, the effects of reaction time, acetic anhydride-to-polysaccharides ratio and temperature were investigated. Process parameters were optimized by single-factor experiment and response surface methodology. The infrared spectroscopy(IR) and scanning electron microscopy(SEM) proved the successful acetylation and were employed to preliminarily analyze the structural characteristics of acetylated derivatives. The results showed that the D_s was 0.327 under the optimal technological conditions, including m(acetic anhydride):m(R. glutinosa polysaccharides)=2.70, reaction time 3.0 h and temperature 48 ℃. Further, the antioxidant properties of acetylated derivatives were investigated in vitro and acetylation was found effective to improve the antioxidant activity of R. glutinosa polysaccharides. This study provides a reference for the further development and application of R. glutinosa polysaccharides.

Discovery and confirmation of protein action site AK1 of ginsenosides in brain based on DARTS technology / 中国中药杂志

This study aims to explore the targets of ginsenosides in brain based on drug affinity responsive target stability(DARTS) technology. Specifically, DARTS technology was combined with label-free liquid chromatography tandem mass spectrometry(LC-MS) to screen out the proteins in the brain that might interact with ginsenosides. Based on the screening results, adenylate kinase 1(AK1) was selected for further confirmation. First, the His-AK1 fusion protein was yielded successively through the construction of recombinant prokaryotic expression vector, expression of target protein, and purification of the fusion protein. Biolayer interferometry(BLI) was employed to detect the direct interaction of Rg_1, Re, Rb_1, Rd, Rh_2, F1, Rh_1, compound K(CK), 25-OH-PPD, protopanaxa-diol(PPD), and protopanaxatriol(PPT) with AK1, thereby screening the ginsenoside monomer or sapogenin that had strong direct interaction with the suspected target protein AK1. Then, the BLI was used to further determine the kinetic parameters for the binding of PPD(strongest interaction with AK1) to His-AK1 fusion protein. Finally, molecular docking technology was applied to analyze the binding properties between the two. With DARTS and LC-MS, multiple differential proteins were screened out, and AK1 was selected based on previous research for target verification. Fusion protein His-AK1 was obtained by prokaryotic expression, and the response(nm) of Re, Rg_1, Rd, Rb_1, Rh_1, Rh_2, F1, PPT, PPD, 25-OH-PPD, and CK with His-AK1 was respectively 0.003 1, 0.001 9, 0.042 8, 0.022 2, 0.013 4, 0.037 3, 0.013 9, 0.030 7, 0.140 2, 0.016 0, and 0.040 8. The K_(on), K_(off), and K_D values of PPD and His-AK1 were determined by the BLI as 1.22×10~2 mol~(-1)·L·s~(-1), 1.04×10~(-2) s~(-1), 8.52×10~(-5) mol·L~(-1). According to the molecular docking result, PPD bound to AK1 with the absolute value of the docking score of 3.438, and hydrogen bonds mainly formed between the two. Thus, AK1 is one of the protein action sites of ginsenosides in the brain. The direct interaction between ginsenoside metabolite PPD and AK1 is the strongest.

Active constituents of Urtica fissa in inhibition of benign prostatic hyperplasia / 中国中药杂志

The present study investigated the material basis of Urtica fissa for the inhibition of benign prostatic hyperplasia(BPH). The active fractions were screened, and the extracts of dichloromethane and ethyl acetate exhibited significantly inhibitory activities against 5α-reductase in vitro and BPH in model rats. The chemical constituents in the active fractions were systematically investigated, and 28 compounds were obtained, which were identified as lobechine methyl ester(1), dibutyl-O-phthalate(2), 1-monolinolein(3), epipinoresinol(4), 5-hydroxy-3,4-dimethyl-5-pentanyl-2(5H)-furanone(5), E-7,9-diene-11-methenyl palmitic acid(6), evofolin B(7), ficusal(8), threo-2,3-bis-(4-hydroxy-3-methoxyphenyl)-3-ethoxypropan-1-ol(9), α-viniferin(10),(9R,7E)-9-hydroxy-5,7-mengatigmadien-4-one-9-O-β-D-glucopyranoside(11), indole-3-carboxaldehyde(12), p-hydroxy ethyl cinnamate(13), benzyl alcohol-O-β-D-glucoside(14), L-methionine(15), 4-methoxyaniline(16), 6-aminopurine(17), 8'-acetyl oilvil(18), 4-methoxyl-8'-acetyl oilvil(19), vanillic acid(20), β-hydroxypropiovanillone(21), 7-hydroxy-6-methoxycoumarin(22), p-hydroxybenzaldehyde(23), pinoresinol(24), erythro-1,2-bis-(4-hydroxy-3-methoxyphenyl)-1,3-propanediol(25), urticol(26), urticol-7-O-β-D-glucopyranoside(27), and lobechine(28). Compounds 1-17 were isolated from U. fissa for the first time. Meanwhile, compound 1 was a new natural product. Compounds 10, 11, 19, 21, and 27 exhibited significant inhibitory effects on 5α-reductase.

Draft Genome Assembly and Annotation for Cutaneotrichosporon dermatis NICC30027, an Oleaginous Yeast Capable of Simultaneous Glucose and Xylose Assimilation

The identification of oleaginous yeast species capable of simultaneously utilizing xylose and glucose as substrates to generate value-added biological products is an area of key economic interest. We have previously demonstrated that the Cutaneotrichosporon dermatisNICC30027 yeast strain is capable of simultaneously assimilating both xylose and glucose, resulting in considerable lipid accumulation. However, as no high-quality genome sequencing data or associated annotations for this strain are available at present, it remains challenging to study the metabolic mechanisms underlying this phenotype. Herein, we report a 39,305,439 bp draft genome assembly for C. dermatis NICC30027 comprised of 37 scaffolds, with 60.15% GC content. Within this genome, we identified 524 tRNAs, 142 sRNAs, 53 miRNAs, 28 snRNAs, and eight rRNA clusters. Moreover, repeat sequences totaling 1,032,129 bp in length were identified (2.63% of the genome), as were 14,238 unigenes that were 1,789.35 bp in length on average (64.82% of the genome). The NCBI non-redundant protein sequences (NR) database was employed to successfully annotate 11,795 of these unigenes, while 3,621 and 11,902 were annotated with the Swiss-Prot and TrEMBL databases, respectively. Unigenes were additionally subjected to pathway enrichment analyses using the Gene Ontology (GO), Kyoto Encyclopedia of Genes and Genomes (KEGG), Cluster of Orthologous Groups of proteins (COG), Clusters of orthologous groups for eukaryotic complete genomes (KOG), and Non-supervised Orthologous Groups (eggNOG) databases.Together, these results provide a foundation for future studies aimed at clarifying the mechanistic basis for the ability of C. dermatis NICC30027 to simultaneously utilize glucose and xylose to synthesize lipids.