Design, synthesis, antibacterial and antitumor activities of novel pyrazolo3,4-bpyridine-4-one-5-carboxylic acid derivatives / 药学学报

To discover new structural hits, based on the important role of pyrazole ring and fragment of pyridinone carboxylic acid in drug design, novel title pyrazolo[3,4-b]pyridine-4-one-5-carboxylic acid derivatives (10a-10p) were designed and synthesized, the structures were confirmed by spectral data and elemental analyses. The antibacterial and antitumor activities were evaluated by the measured minimum inhibitory concentration (MIC) values against the tested four strains and half inhibitory concentration (IC50) values against the tested four cancer cells, respectively. The results displayed markedly poor antibacterial activity and observably potent antitumor activity. In particularly, the title difluorophenyl (10d, 10e, 10f), pyridyl (10j), ethyl (10k) and cycloproyl (10l) compounds exhibited comparable activity against Capan-1 and A549 cells to that of the comparison doxorubicin. Thus, pyrazolo[3,4-b]pyridine-4-one-5-carboxylic acid derivatives as promising antitumor hits need to be developed.

Effect of peripheral cannulation for cardiopulmonary bypass in patients with congenital heart disease undergoing reoperation: A retrospective cohort study / 中国胸心血管外科临床杂志

@#Objective    To evaluate the safety and efficacy of peripheral cannulation for cardiopulmonary bypass (CPB) in patients with reoperation of congenital heart disease. Methods    The perioperative data of patients with congenital heart disease who underwent reoperation in Fuwai Hospital from 2019 to 2020 were retrospectively collected. They were divided into two groups according to the cannulation methods: a central group and a peripheral group. The prognosis of the patients was analyzed. Results     A total of 80 patients were collected, including 43 patients in the central group, and 37 pateints in the peripheral group. In the central group, the median age was 18 (14, 32) years, and 21 patients were male. The median age of the peripheral group was 16 (10, 27 ) years, and 18 patients were male. The CPB time in the peripheral group was 201 (164, 230) min, which was longer than that in the central group [143 (97, 188 ) min, P<0.001]. The lactate after CPB in the peripheral group was statistically higher than that in the central group [2 (1, 2 ) mmol/L vs. 1 (1, 1) mmol/L, P=0.002]. The dosage of albumin use during CPB in the peripheral group was statistically higher than that in the central group [10 (0, 20) g vs. 0 (0, 0) g, P=0.004]. There was no statistical difference in the postoperative dosage of red blood cells use [0 (0, 2) U vs. 0 (0, 0) U, P=0.117], mechanical ventilation time [14 (11, 19) h vs. 13 (10, 15) h, P=0.296], ICU stay time [43 (23, 80) h vs. 40 (20, 67) h, P=0.237] or postoperative hospital stay time [10 (7, 12) d vs. 8 (7, 10) d, P=778] between the two groups. Conclusion    It’s safe and efficient to establish CPB through peripheral cannulation in patients with complex congenital heart disease undergoing reoperation.

Role of suPAR in the Pathogenesis of Podocyte Injury of Primary Focal Segmental Glomerulosclerosis / 中山大学学报(医学科学版)

ObjectiveThis study aims to investigate the role of suPAR in the pathogenesis of podocyte injury in FSGS. Methods① The sera of primary FSGS patients （17 cases） were collected. Healthy volunteers （10 cases） and patients with other types of primary nephrotic syndrome （10 cases） were set as normal and disease controls. SuPAR levels were detected by ELISA； ② Podocytes were stimulated by suPAR in vitro， and cells were collected to analyze apoptosis by flow cytometry and for RNAseq analysis； ③ Differentially expressed genes （DEGs） were screened from RNAseq data. Both up-regulated and down-regulated genes were analyzed by KEGG and GO enrichment analysis. Heat map was used to show expression of genes related to podocyte focal adhesion， slit diaphragm and actin dynamics and endocytosis. Differentially expressed genes were verified by qPCR. Results① The level of suPAR in FSGS patients was significantly increased， and that in other nephrotic syndrome（NS） patients was also significantly increased； ② suPAR stimulation significantly altered the transcriptome pattern of human podocytes. A total of 272 up-regulated genes and 288 down-regulated genes were screened； ③ KEGG and GO enrichment analysis of up-regulated and down-regulated genes showed that Focal adhesion and DNA replication and DNA repair related pathways were significantly down-regulated； ④ suPAR did not increase podocyte apoptosis. ConclusionThe level of suPAR is significantly increased in patients with primary FSGS. SuPAR may promote podocyte injury by interfering with genomic homeostasis and disrupting focal adhesion， slit diaphragm， actin dynamics and endocytosis-related functional molecules of podocytes.

Research advances on antitumor mechanism of NK cells and its application in cancer targeted therapy / 药学学报

Natural killer (NK) cells, as an essential part of innate immunity, can directly identify and kill tumor cells after being activated by the synergistic action of surface inhibitory receptors and activated receptors. It can secrete cytokines to recruit dendritic cells (DCs), induce DCs maturation and enhance adaptive immune response. It can target cancer stem cells (CSCs) and circulating tumor cells (CTCs) to inhibit cancer metastasis. NK cells have a unique inflammatory tendency, which can respond to cytokines and chemokines released from tumor sites and migrate to tumor sites, making them occupy an important advantage in cancer targeted therapy. The research on cancer targeted therapy of NK cells as drug delivery carriers, NK cell membrane-coated biomimetic nanoparticles, and NK cell extracellular vesicles (NKEVs) has attracted more and more attention. The article will focus on the mechanism of NK cells inhibiting cancer, and summarize the research progress of cancer targeted therapy of NK cells.

Comparison of IgG Antibody Levels in Mice Immunized with SARS-CoV-2 RBD Proteins Produced from Two Expression Systems / 中国生物化学与分子生物学报

The COVID-19 pandemic is still spreading around the world,posing a severe challenge to public health security and economic development in China and beyond. The pivotal process of SARS-COV-2 invasion is that the receptor binding domain (RBD) of Coronavirus spike protein binds with the angioten-sin converting enzyme 2 (ACE2) receptor on host cells. Therefore, RBD is closely related to our major anti-epidemic strategies such as rapid pathogen detection and development of vaccines and antiviral drugs. In this study, we aim to compare the anti-RBD IgG by immunizing mice with the recombinant RBDs of novel Coronavirus spike protein, and evaluate the antibody titers and duration elicited by RBD produced from different host cells and used in different doses, which can be used for vaccine evaluation, drug development, and pathogen detection. SDS-PAGE and mass spectrometry analysis showed that the molecular weight of bRBD (produced by insect cells) and hRBD (produced by mammalian cells) were slightly different, which are mainly caused by different glycosylation modification. Flow cytometry revealed that the binding rates of bRBD and hRBD to HEK293-ACE2-overexpressing cells were 88. 5% and 92. 7%, respectively, indicating that both antigens have favorable bioactivity. Balb/ c mice are immunized intramuscularly with 10 μg and 20 μg per mouse of RBD proteins, which were mixed with Quick Antibody adjuvant previously, and blood samples collected from the tail at 2, 4, 6, 8, 12 and 24 weeks after the primary immunization. Enzyme-linked immunosorbent assay (ELISA) showed that both RBD immunization with 10 μg or 20 μg could induce a rapid immune response to produce IgG antibodies. The antibody titers reached the peak at 4-6 weeks post first immunization, and persisted over a long time up to 6 months. No significant difference was observed in the induced antibody titers by bRBD and hRBD as well as their different doses. Virus Neutralization Assays showed that specific antibodies induced by RBD-immunized mice could inhibit the infection of ACE2-positive cells by SARS-CoV-2 pseudovirus. These results suggest that both RBD proteins through commendable adjuvant inoculation can rapidly induce an effective humoral immune response and generate specific neutralizing antibodies. It is expected to be helpful for rapid preparation of antibodies against the future various RBD mutants during the pandemic.

Long Time Efficacy and Safety of Microvascular Decompression Combined with Internal Neurolysis for Recurrent Trigeminal Neuralgia

Objective@#: To explore the clinical efficacy and safety of microvascular decompression (MVD) combined with internal neurolysis (IN) in the treatment of recurrent trigeminal neuralgia (TN) after MVD. @*Methods@#: Sixty-four patients with recurrent TN admitted to the hospital from January 2014 to December 2017 were divided into two groups according to the surgical method. Twenty-nine patients, admitted from January 2014 to December 2015, were treated with MVD alone, whereas 35 admitted from January 2016 to December 2017 were treated with MVD+IN. The postoperative efficacy, complications, and pain recurrence rate of the two groups were analyzed. @*Results@#: The efficacy of the MVD+IN and MVD groups were 88.6% and 86.2%, and the cure rates were 77.1% and 65.5% respectively. There was no statistically significant difference between the two groups (p>0.05). The cure rate (83.3%) of patients in the MVD+IN group, who were only found thickened arachnoid adhesions during the operation that could not be fully released, was significantly higher than that of the MVD group (30.0%) (p0.05). For patients whose arachnoid adhesions were completely released, there had no significant difference (p>0.05) in the efficacy (87% vs. 94.7%) and recurrence rate (5.0% vs. 11.1%). The incidence of postoperative facial numbness (88.6%) in the MVD+IN group was higher than that in the MVD group (10.3%) (p0.05). In the 18–36 months follow-up, the recurrence rate of patients in the MVD+IN group (9.7%) and in the MVD group (16%) were not statistically different (p>0.05). @*Conclusion@#: A retrospective comparison of patients with recurrent TN showed that both MVD and MVD combined with IN can effectively treat recurrent TN. Compared with MVD alone, MVD combined with IN can effectively improve the pain cure rate of patients with recurrent TN who have only severe arachnoid adhesions. The combination does not increase the incidence of long-term facial numbness and other complications.

Meta-analysis of long-term efficacy of vitrectomy combined with anti-VEGF in the treatment of proliferative diabetic retinopathy / 国际眼科杂志(Guoji Yanke Zazhi)

@#AIM: To explore the long-term efficacy of vitrectomy combined with or without anti-VEGF in the treatment of proliferative diabetic retinopathy(PDR).<p>METHODS: Randomized controlled trials(RCTs)comparing the efficacy of vitrectomy combined with or without anti-VEGF therapy for PDR were retrieved from databases including PUBMED, EMBASE, Cochrane Central Register of Controlled Trials(CENTRAL)and Web of Science. The retrieval time was from the establishment of the databases to July 2020. According to the inclusion and exclusion criteria, the literature was selected, then data extraction and quality evaluation was completed. Primary evaluation measures included postoperative incidence of retinal detachment, central retinal thickness(CRT), and best corrected visual acuity(BCVA). <p>RESULTS: In this article, 11 randomized controlled studies(880 eyes)were included. Meta-analysis results showed that the incidence of retinal detachment after vitrectomy was significantly lower in PDR patients who received anti-VEGF injection before vitrectomy than in patients who did not receive anti-VEGF injection \〖Risk ratio(<i>RR</i>)=0.39, 95% Confidence interval(<i>CI</i>)0.22 to 0.71, <i>P</i>=0.002\〗. There were significant differences in the incidence of retinal detachment after vitrectomy between the anti-VEGF group and the non-VEFG group in both Asian and non-Asian populations(Asian:<i> RR</i>=0.20, 95%<i>CI</i> 0.05 to 0.87, <i>P</i>=0.03; Non-Asian:<i> RR</i>=0.46, 95%<i>CI</i> 0.24 to 0.89, <i>P</i>=0.02). The central retinal thickness of PDR patients who received preoperative anti-VEGF therapy was significantly lower than that of patients who did not receive anti-VEGF therapy 3 and 6mo after PPV(<i>MD</i>=-78.49, 95%<i>CI</i> -94.81 to -62.17, <i>P</i><0.00001. <i>MD</i>= -39.62, 95%<i>CI</i> -48.44 to -30.80, <i>P</i><0.00001). The BCVA at 6mo after PPV in PDR patients with preoperative anti-VEGF treatment was better than that in patients without preoperative anti-VEGF treatment(<i>MD</i>=-0.16, 95%<i>CI</i> -0.21 to -0.10, <i>P</i><0.00001).<p>CONCLUSION: Anti-VEGF injection before PPV can effectively reduce the incidence of retinal detachment, alleviate postoperative macular edema, reduce the central retinal thickness, and improve BCVA in PDR patients.

Preparation of personalized traditional Chinese medicine condensed water pill without excipients based on correlation between concentrate viscosity and molding quality / 中国中药杂志

To explore the correlation between concentrate viscosity and molding quality of personalized traditional Chinese medicine(TCM) condensed water pill, this study established a concentrate viscosity characterization method with rotational rheometry. Seven model prescriptions were respectively concentrated to different degrees and the viscosity of each concentrate was determined. The pre-sence of 'viscosity jump' in the middle stage of 'flag hanging' of all the model prescriptions implied that there might be an ideal viscosity range in the preparation of condensed water pill. The further study of 22 model prescriptions demonstrated that the optimum viscosity range of concentrate was 5-15 Pa·s(25 ℃) for approximately 82% of the prescriptions. About 18% of the prescriptions had a wide range, which might be caused by the high proportions of mineral and crustacean drugs in the crushing part and sugar and fibrous drugs in the decocting part. This study clarified the optimum viscosity range for concentrates of personalized TCM condensed water pills and achieved a preparation technology without any excipient, laying a foundation for the on-line control of the preparation.

Cognition on diagnosis and treatments of bronchiectasis among respiratory specialists / 中华健康管理学杂志

Objective:To investigate the cognition of the diagnosis and management of bronchiectasis among respiratory specialists.Methods:Between May and June 2020, a questionnaire survey based on expert consensus and guidelines was conducted among respiratory specialists from 50 hospitals from Sichuan and Yunnan provinces. Total 691 questionnaires were distributed and 641 were received. 601 valid questionnaires were chosen for further analysis with an effective recovery rate of 87.0%. The respondents were required to finish the e-questionnaires independently in terms of cognition of diagnosing, severity assessment, treatments and Chinese medicines of bronchiectasis. The responses were collected online and the cognitive levels were evaluated by calculating the correct rates of corresponding questions.Results:540 (89.9%) of the respondents agreed that high-resolution computed tomography (HRCT) was the gold standard for diagnosing of bronchiectasis, but 318 (52.9%) had an incomplete understanding of common radiographic manifestations of bronchiectasis, and different cognitive degrees of common radiographic manifestations of bronchiectasis existed among respondents with different qualifications or working in different levels of hospitals ( P<0.05). Only 118 (19.6%) of the respondents were familiar with severity assessments of bronchiectasis, but 65 (55.1%) of the 118 respondents said they won′t apply these severity assessments to patient during their clinical works. For the treatment of patients with stable bronchiectasis, airway clearance techniques were most recommended by specialists surveyed [410 (68.2%)], among which, postural drainage was the most known method [559 (93.0%)]. For patients undergoing an acute exacerbation, most respondents recommended antibiotics [600 (99.8%)] as the primary treatment, and examinations such as sputum culture [544 (90.5%)], inflammatory markers [523 (87.0%)] should be performed as well. 504 (83.9%) thought that pseudomonas aeruginosa was the most common conditioned pathogen for bronchiectasis. For patients with frequent exacerbations (≥3 per year), 385 (64.1%) of the respondents supported the therapeutic effect of long-term antibiotics, however, among the 385 respondents supporting long-term antibiotics, only [113 (29.4%)] were willing to recommend long-term antibiotic treatment actively during their clinical practice. Besides, 304 (50.6%) respondents held a positive attitude to the clinical effect of traditional Chinese medicine therapies. Among 304 respondents holds the point of supporting, only 86 (28.3%) were willing to recommend traditional Chinese medicine to patients actively, differences about the attitude and clinical behaviors were found between respondents working in different levels of hospitals ( P<0.05). Conclusions:Respiratory specialists′ cognition on diagnosis and treatments of bronchiectasis remains inadequate, and cognitive levels differ among respondents working in different levels of hospitals. There is a gap between respondents′ cognition and clinical practice. Further education and trainings are necessary for improving respiratory specialists′ knowledge for timely diagnosis and standard treatment of bronchiectasis.

Effect and Mechanism of Modified Banxia Xiexintang on Depression During Perimenopause / 中国实验方剂学杂志

Objective::To observe the effect of modified Banxia Xiexintang on depression during perimenopause, in order to study itseffecton 5-hydroxytryptamine (5-HT) and proinflammatory factors. Method::One hundred and thirty-nine patients were randomly divided into control group (69 cases) and observation group (70 cases) by random number table.Patients in control group got tibolone tablets, 2.5 mg/time, 1 time/day, and paroxetine hydrochloride tablets, 20 mg/time, 1 time/day.In addition to the therapy in control group, patients in observation group were added with modified Banxia Xiexintang, 1 dose/day.The course of treatment was 8 weeks.And before and after treatment, Hamilton depression scale for-17 items (HAMD-17), Zung's self-rating depression scale (SDS), hamilton anxiety scale (HAMA), improvement Kupperman(KI), liver depression and spleen deficiency syndrome, menopause-specific quality of life questionnaire (MENQOL) and treatment emergent symptom scale (TESS) were scored, and levels of 5-HT, rain-derived neurotrophic factor (BDNF), interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) were detected. Result::After treatment, scores of HAMD-17 and SDS in observation group were lower than those in control group (P<0.01). And the effect on trea depression in observation group was better than that in control group (Z=2.074, P<0.05). The degree of depression in observation group was ligher than that in control group (Z=2.157, P<0.05). And scores of HAMA, KI and liver depression and spleen deficiency syndrome were lower than those in control group (P<0.01). The severity of perimenopausal syndrome was ligher than that in control group (Z=2.046, P<0.05). And scores of vasomotor symptoms and psychological symptoms of MENQOL scale and the total scores were lower than those in control group (P<0.05). Levels of 5-HT and BDNF were higher than those in control group (P<0.01), while levels of IL-1β, TNF-α and TESS were lower than those in control group (P<0.01). Conclusion::In addition to theroutine western medicine, modified Banxia Xiexintang can alleviate the severity of depression, release the symptoms of depression, anxiety and perimenopausal syudrome(PMS), improve the quality of life, inhibit pro-inflammatory factors, and enhance the expressions of 5-HT and BDNF, with no adverse event.

Clinical Research on Treatment of Acute Cerebral Infarction with ‘Sanjiao Regular Sequence Therapy’ / 中国实验方剂学杂志

Objective:To evaluate the clinical efficacy of Sanjiao Cidi therapy on acute cerebral infarction and its effect on levels of S100-β protein （S100-β）， tumor necrosis factor-α （TNF-α）， hypersensitive C-reactive protein （hs-CRP） and neuropeptide （NPY）. Method:One hundred and eighty patients were randomly divided into control group （90 cases） and observation group （90 cases） by random number table. Patients in control group got aspirin enteric-coated tablets， 100 mg/time， 1 time/day， edaravone injection （injected within 30 minutes） for 14 days， 30 mg/time， 2 times/day， simvastatin tablets， 20 mg/time， 1 time/day. In addition to the basic therapy of meloxicam tablets， patients in observation group were also treated with Sanjiao Cidi therapy. In the first step， patients got Guizhi therapy to dredge Zhongjiao and Shangjiao， 1 dose/day， for 8 days. In the second step， patients got Sini therapy to dredge Zhongjiao and Xiajiao， 1 dose/day， for 10 days. In the third step， patients got Tianjing Gubentherapy， 1 dose/day， for 10 days. The course of treatment was 4 weeks. Before the treatment， and at the first， second， third and fourth weeks after treatment， National Institutes of Health Stroke Scale （NIHSS） was scored. And before and after treatment， function scale of fuglmeyer （FMA）， ability of daily life activities （ADL）， mini-mental state examination （MMSE） and main symptoms of traditional Chinese medicine were scored. Comprehensive assessment of patient report outcome （PRO） was made. And levels of S100-β， hs-CRP， TNF-α and NPY were detected. And the incidence rate of pulmonary infection， urinary infection， skeletal myalgia， shoulder hand syndrome and shoulder subluxation of patients were recorded during hospitalization. Result:The clinical efficacy in observation group was better than that in control group （Z=2.141， P<0.05）. Scores of NIHSS in observation group were lower than those in control group at the first， second， third and fourth weeks after treatment （P<0.01）. Scores of upper limb， legs and the total scores from FMA were higher than those in control group （P<0.01）. Scores of the main symptoms of traditional Chinese medicine， symptoms， psychological and social scores， total scores of PRO， S100-β， hs-CRP， TNF-α and NPY were lower than those in the observation group （P<0.01）. And scores of ADL and MMSE were higher than those in control group （P<0.01）. Total incidence of complications in observation group was 27.27%（21/77）， which was lower than 46.15%（36/78） in control group （χ2=5.941， P<0.05）. Conclusion:In addition to conventional western medicine treatment， Sanjiao Cidi therapy can treat the patients with acute cerebral infarction， alleviate the degree of neurological deficit， improve the cognitive function， motor function of limbs and the ability of daily life， reduce the main symptoms of traditional Chinese medicine， the incidence of complications and the inflammatory response， protect the nerve cells， with a better clinical efficacy and comprehensive effect in patients than pure Western medicine.

Effects of substrate on growth and lipid accumulation of Tribonema sp. FACHB-1786 / 生物工程学报

Filamentous microalga Tribonema sp. has the advantages of highly resistance to zooplankton-predation, easy harvesting, and high cellular lipid content, in particular large amounts of palmitoleic acid (PA) and eicosapentaenoic acid (EPA). Therefore, Tribonema sp. is considered as a promising biomass feedstock to produce biodiesel and high-value products. In this work, we studied the effect of different concentrations of nitrogen (NaNO₃: 255-3 060 mg/L), phosphorus (K₂HPO₄: 4-240 mg/L), iron ((NH₄)₃FeC₁₂H₁₀O₁₄: 0.6-12 mg/L) and magnesium (MgSO₄: 7.5-450 mg/L) on the biomass, lipid content, and fatty acid composition of Tribonema sp. FACHB-1786, aiming at enhancing cell lipid productivity. The growth of Tribonema sp. had a positive correlation with the concentration of magnesium, and the maximum biomass of Tribonema sp. (under the condition of 450 mg/L MgSO₄) was 8.09 g/L, much greater than those reported in previous studies using the same and other Tribonema species under autotrophic conditions. Different nitrogen concentrations exerted no significant effect on algal growth (P > 0.05), but a higher nitrogen concentration resulted in a greater amount of lipid in the cells. The maximum volumetric productivities of total lipids (319. 6 mg/(L·d)), palmitoleic acid (135.7 mg/(L·d)), and eicosapentaenoic acid (24.2 mg/(L·d)) of Tribonema sp. were obtained when the concentrations of NaNO₃, K₂HPO₄, (NH₄)₃FeC₁₂H₁₀O₁₄, and MgSO₄ were 765 mg/L, 80 mg/L, 6 mg/L, and 75 mg/L, respectively. This study will provide a reference for substrate optimization for Tribonema sp. growth and lipid production.

Inhibition of chemotherapy-related breast tumor EMT by application of redox-sensitive siRNA delivery system CSO-ss-SA/siRNA along with doxorubicin treatment / 浙江大学学报（英文版）（B辑：生物医学和生物技术）

Metastasis is one of the main reasons causing death in cancer patients. It was reported that chemotherapy might induce metastasis. In order to uncover the mechanism of chemotherapy-induced metastasis and find solutions to inhibit treatment-induced metastasis, the relationship between epithelial-mesenchymal transition (EMT) and doxorubicin (DOX) treatment was investigated and a redox-sensitive small interfering RNA (siRNA) delivery system was designed. DOX-related reactive oxygen species (ROS) were found to be responsible for the invasiveness of tumor cells in vitro, causing enhanced EMT and cytoskeleton reconstruction regulated by Ras-related C3 botulinum toxin substrate 1 (RAC1). In order to decrease RAC1, a redox-sensitive glycolipid drug delivery system (chitosan-ss-stearylamine conjugate (CSO-ss-SA)) was designed to carry siRNA, forming a gene delivery system (CSO-ss-SA/siRNA) downregulating RAC1. CSO-ss-SA/siRNA exhibited an enhanced redox sensitivity compared to nonresponsive complexes in 10 mmol/L glutathione (GSH) and showed a significant safety. CSO-ss-SA/siRNA could effectively transmit siRNA into tumor cells, reducing the expression of RAC1 protein by 38.2% and decreasing the number of tumor-induced invasion cells by 42.5%. When combined with DOX, CSO-ss-SA/siRNA remarkably inhibited the chemotherapy-induced EMT in vivo and enhanced therapeutic efficiency. The present study indicates that RAC1 protein is a key regulator of chemotherapy-induced EMT and CSO-ss-SA/siRNA silencing RAC1 could efficiently decrease the tumor metastasis risk after chemotherapy.

Sugarcane stem nodes based on the maximum value points of the vertical projection function / Identificação de nós de tronco de cana-de-açúcar com base nos pontos de valor extremos da função de projeção vertical

ABSTRACT: In order to solve the problem that the stem nodes are difficult to identify in the process of sugarcane seed automatic cutting, a method of identifying the stem nodes of sugarcane based on the extreme points of vertical projection function is proposed in this paper. Firstly, in order to reduce the influence of light on image processing, the RGB color image is converted to HSI color image, and the S component image of the HSI color space is extracted as a research object. Then, the S component image is binarized by the Otsu method, the hole of the binary image is filled by morphology closing algorithm, and the sugarcane and the background are initially separated by the horizontal projection map of the binary image. Finally, the position of sugarcane stem is preliminarily determined by continuously taking the derivative of the vertical projection function of the binary image, and the sum of the local pixel value of the suspicious pixel column is compared to further determine the sugarcane stem node. The experimental results showed that the recognition rate of single stem node is 100%, and the standard deviation is less than 1.1 mm. The accuracy of simultaneous identification of double stem nodes is 98%, and the standard deviation is less than 1.7 mm. The accuracy of simultaneous identification of the three stem nodes is 95%, and the standard deviation is less than 2.2 mm. Compared with the other methods introduced in this paper, the proposed method has higher recognition and accuracy.

RESUMO: Para resolver o problema que os nós do caule são difíceis de identificar no processo de corte automático de sementes de cana-de-açúcar, é proposto, neste artigo, um método para identificar os nós do colmo da cana-de-açúcar com base nos pontos extremos da função de projeção vertical. Em primeiro lugar, a fim de reduzir a influência da luz no processamento da imagem, a imagem de cor RGB foi convertida em imagem de cor HSI, e a imagem de componente S do espaço de cores HSI é extraída como um objeto de pesquisa. Em seguida, o método Otsu foi usado para binarizar o mapa do componente S, e a operação morfológica fechada foi usada para preencher os espaços da imagem binária, e a projeção horizontal da imagem binária foi usada para separar a cana de açúcar do fundo. Finalmente, a posição do caule de cana-de-açúcar foi preliminarmente determinada através da tomada contínua do derivado da função de projeção vertical da imagem binária, e a soma do valor pixel local da coluna de pixel suspeito foi comparada para determinar ainda mais o nódulo da cana-de-açúcar. Os resultados experimentais mostram que a taxa de reconhecimento do nó de haste única foi de 100%, o desvio padrão foi inferior a 1.1 mm. A precisão da identificação simultânea de nós de haste dupla foi de 98%, o desvio padrão foi menor que 1.7 mm. A precisão da identificação simultânea dos três nós de haste é de 95%, o desvio padrão foi inferior a 2.2 mm. Comparado com os outros métodos introduzidos neste artigo, o método proposto possui maior reconhecimento e precisão.

Extraction of navigation line based on improved grayscale factor in corn field / Obtenção de linhas de tráfego em lavoura de milho baseada no fator de escala de cinza melhorado

ABSTRACT: Focusing on the problem that corn plant in different growth periods is grayed out by known methods, the gray scale difference of different part is large or the soil discrimination degree is not high, the navigation path is low in accuracy and speed. This paper proposed a new method for extracting cornfield navigation baselines, which is used to control walking of agricultural robots. Design method included image segmentation, navigation point extraction, and navigation path fitting. Image segmentation is based on a new grayscale factor combined with median filtering, OSTU method and morphological operations to achieve the separation of crops and soil. The extraction of the navigation point is based on the binary image vertical projection map to obtain the region of interest, and the navigation point coordinates are determined by calculating the relative center point of the white pixel points of the sampling line in the region of interest. The Hough transform is used to fit the navigation point obtained by the vertical projection map to determine the navigation path, and then the control parameters are obtained. The gray scale factor that is improved in this paper combined with the vertical projection map can extract the target ridge with an accuracy rate of 92%, and the accuracy of extracting the navigation line is more than 90%. When conducting navigation tracking experiments in corn field, the maximum error is 5cm.

RESUMO: Depois de usar o método conhecido como escala de cinza para plantas de milho, a diferença de escala de cinza entre diferentes partes da planta é grande ou a diferenciação do solo não é alta, a precisão do trajeto de navegação é baixa e a velocidade é lenta. Neste trabalho foi proposto um novo método de extração da linha de referência de navegação para campos de milho, que é usado para controlar a caminhada de robôs agrícolas. Os métodos de projeto incluem: segmentação de imagem, extração de ponto de navegação e encaixe de linha de navegação. A segmentação por imagem é baseada na separação de culturas e solos com base no novo fator de escala de cinza combinado com a filtragem mediana, método de Otsu e operação morfológica. A extração de pontos de navegação é baseada em um mapa de projeção vertical de imagem de dois valores para obter a área de interesse, e as coordenadas do ponto de navegação são determinadas por cálculo do ponto central relativo no pixel branco da linha amostral na área de interesse. O fator de escala de cinza melhorado nesta pesquisa irá extrair o centro da entre linha de plantio alvo com uma taxa de precisão de 92%. A precisão de extração da linha de navegação é mais de 90%. O erro máximo foi de 5cm quando o experimento de rastreamento de navegação em tempo foi é realizado em campos de milho.

Clinical observation on the inflammatory indexes in septic gastrointestinal dysfunction treated with acupuncture at Jiaji (EX-B 2) / 中国针灸

OBJECTIVE@#To evaluate the effect on the inflammatory indexes of septic gastrointestinal dysfunction treated with acupuncture at Jiaji (EX-B 2).@*METHODS@#A total of 118 patients of septic gastrointestinal dysfunction were randomized into an observation group and a control group, 59 cases in each one. In the control group, mosapride citrate was prescribed for oral administration, 5 mg each time, 3 times a day, bifidobacterium triple viable capsules, 420 mg each time, twice a day, intravenous drip with omeprazole, 40 mg, twice a day. Additionally, the antibiotics and the symptomatic treatment were selected rationally for maintaining the functions of the important organs, e.g. heart, lung, brain and kidney, and water-electrolyte balance. In the observation group, on the routine management as the control group, acupuncture at Jiaji (EX-B 2, T-T) was added, the needles were retained for 30 min in each treatment, once a day, 10 days as one course and 1 course was required. Separately, on the 1st, 3rd, 6th and 10th days of treatment, the white blood cell (WBC) count, the levels of hypersensitive C-reactive protein (hs-CRP) and procalcitonin (PCT) were observed, the enteral nutrition feeding dose and gastrointestinal dysfunction score before and after treatment as well as the clinical effect were assessed in the two groups.@*RESULTS@#The differences were not significant in the indexes mentioned above on 1st and 3rd days of treatment between the two groups (>0.05). On the 6th and 10th days of treatment, regarding the gastrointestinal dysfunction score and inflammatory indexes count, the results in the observation group were lower than the control group (all <0.05), and feeding dose in the observation group was higher than the control group (<0.05). After treatment, the gastrointestinal dysfunction scores and inflammatory indexes count were all reduced and feeding dose was increased as compared with those before treatment in the patients of the two groups (all <0.05). After treatment, the total effective rate was 91.5% (54/59) in the observation group, higher than 76.3% (45/59) in the control group (<0.05).@*CONCLUSION@#Acupuncture at Jiaji (EX-B 2) points achieves the satisfactory effect on septic gastrointestinal dysfunction and reduces the inflammatory indexes count.

Synthesis and antitumor activity of fluoroquinolone C-3 arylidene thiazolone derivatives from ciprofloxacin / 药学学报

To expand an efficient strategy for the conversion of antibacterial activity of fluoroquinolones into an antitumor activity, sixteen new compounds, 1-cyclopropyl-6- fluoro-7-(4-methyl-piperazin-1-yl)-3-(5-arylidene-thiazol-4(5H)-one-2-yl)-quinolon-4(1H)-ones (7a-7p), were designed and synthesized with a thiazolone ring and an arylidene moiety as an isostere and modified group, respectively, from ciprofloxacin. Their structures were characterized by elemental analysis and spectral data. The in vitro antitumor activity of the synthesized compounds were measured using Hep-3B, Capan-1 and HL60 cell lines and were found to be more potent than ciprofloxacin. Meanwhile, the SAR revealed that the halogenated phenyl compounds such as fluorophenyl (7h, 7i), chlorophenyl (7j, 7k) or bromophenyl compounds (7l, 7m), and aromatic heterocyclic substitution such as furyl (6n) or pyridyl compounds (6o, 6p) displayed better activity than the control compounds, especially the IC50 values of pyridyl compounds 6o and 6p against Capan-1 cell growth was comparable to doxorubicin. Thus, an arylidene-modified thiazolone scaffold as the replacement of the C-3 carboxylic acid group appears to be an alternative route for an improved antitumor activity of fluoroquinolones.

Development status and research strategy of traditional Chinese medicine temporary prescription preparation technology / 中国中药杂志

Temporary prescription preparation is the preparation processed into different dosage forms by relevant pharmacist according to the temporary preparation requirement and the personalized prescription made by the doctor in accordance with the syndrome differentiation and drug performance.It is an important part in personalized pharmaceutical services.Rational design of process route,production equipment and quality control method for the temporary prescription preparation,and establishment of technology research strategy and mode in accordance with the characteristics of traditional Chinese medicine temporary prescription preparations play an important role in promoting the development of the temporary prescription preparations.To promote the normalization,standardization and intelligent development of temporary prescription preparations,we would comprehensively summarize the significance,policy,technology characteristics,technology research status quo and existing problems in this paper,and put forward the research direction of temporary prescription preparation technology based on the physical properties of raw materials,equipment research strategy,and intelligent manufacturing technology.Thus it will push the inheritance and innovation of temporary prescription preparation.

Retinol dehydrogenase 10 promotes metastasis of glioma cells via the transforming growth factor-β/SMAD signaling pathway / 中华医学杂志(英文版)

BACKGROUND@#Glioma is the most common primary malignant tumor in the central nervous system. Because of the resistance of glioma to chemoradiotherapy and its aggressive growth, the survival rate of patients with glioma has not improved. This study aimed to disclose the effect of retinol dehydrogenase 10 (RDH10) on the migration and invasion of glioma cells, and to explore the potential mechanism.@*METHODS@#Reverse transcription-polymerase chain reaction (RT-PCR) was used to determine the expression levels of RDH10 in healthy glial cells and glioma cells. Human glioma cell strains, U87 and U251, were infected with negative control or RDH10-interfering lentiviruses. RT-PCR and Western blotting were performed to determine the knockdown efficiency. Scratch and transwell assays were used to assess cell migration and invasion after RDH10 knockdown. Finally, changes in transforming growth factor-β (TGF-β)/SMAD signaling pathway-related expression were examined by Western blotting. Differences between groups were analyzed by one-way analysis of variance.@*RESULTS@#RDH10 was highly expressed in glioma cells. Compared with the control group, RDH10 knockdown significantly reduced RDH10 messenger RNA and protein expression levels in U87 and U251 glioma cells (U87: 1.00 ± 0.08 vs. 0.22 ± 0.02, t = 16.55, P < 0.001; U251: 1.00 ± 0.17 vs. 0.39 ± 0.01, t = 6.30, P < 0.001). The scratch assay indicated that compared with the control group, RDH10 knockdown significantly inhibited the migration of glioma cells (U87: 1.00% ± 0.04% vs. 2.00% ± 0.25%, t = 6.08, P < 0.01; U251: 1.00% ± 0.11% vs. 2.48% ± 0.31%, t = 5.79, P < 0.01). Furthermore, RDH10 knockdown significantly inhibited the invasive capacity of glioma cells (U87: 97.30 ± 7.01 vs. 13.70 ± 0.58, t = 20.36, P < 0.001; U251: 96.20 ± 7.10 vs. 18.30 ± 2.08, t = 18.51, P < 0.001). Finally, Western blotting demonstrated that compared with the control group, downregulation of RDH10 significantly inhibited TGF-β expression, phosphorylated SMAD2, and phosphorylated SMAD3 (TGF-β: 1.00 ± 0.10 vs. 0.53 ± 0.06, t = 7.05, P < 0.01; phosphorylated SMAD2: 1.00 ± 0.20 vs. 0.42 ± 0.17, t = 4.01, P < 0.01; phosphorylated SMAD3: 1.00 ± 0.18 vs. 0.41 ± 0.12, t = 4.12, P < 0.01).@*CONCLUSION@#RDH10 knockdown might inhibit metastasis of glioma cells via the TGF-β/SMAD signaling pathway.

SeqSQC: A Bioconductor Package for Evaluating the Sample Quality of Next-generation Sequencing Data / 基因组蛋白质组与生物信息学报·英文版

As next-generation sequencing (NGS) technology has become widely used to identify genetic causal variants for various diseases and traits, a number of packages for checking NGS data quality have sprung up in public domains. In addition to the quality of sequencing data, sample quality issues, such as gender mismatch, abnormal inbreeding coefficient, cryptic relatedness, and population outliers, can also have fundamental impact on downstream analysis. However, there is a lack of tools specialized in identifying problematic samples from NGS data, often due to the limitation of sample size and variant counts. We developed SeqSQC, a Bioconductor package, to automate and accelerate sample cleaning in NGS data of any scale. SeqSQC is designed for efficient data storage and access, and equipped with interactive plots for intuitive data visualization to expedite the identification of problematic samples. SeqSQC is available at http://bioconductor.org/packages/SeqSQC.