ABSTRACT
In recent years, some large public hospitals in China had successively opened scientific research outpatients to provide consulting services for clinical research, but there were generally problems such as insufficient audience and single role of expert teams. In July 2021, Shanghai Clinical Research Center established a multidisciplinary scientific research outpatient for the entire clinical research cycle, providing medical staffs with such services as clinical research design and project application, paper revision and achievement transformation. It also provided clerkship for medical students on campus to cultivate their standardized clinical research thinking. As of July 2022, the outpatient had provided research consulting services 16 times, teaching 8 class hours to medical students, and collaborated to solve multi-dimensional clinical research practical problems throughout the entire cycle, such as clinical trial design, project application, and paper publication. Good results had been achieved by this outpatient to provide reference for promoting the development of scientific research outpatients in China and improving the clinical research level of hospitals.
ABSTRACT
Objective To explore the potential mechanism of Erchen decoction in the treatment of obese polycystic ovary syndrome and obese infertility, in order to provide theoretical basis for “treating different diseases with same method”. Methods The active ingredients and targets of Erchen decoction were obtained from TCMSP database, and the targets of obese polycystic ovary syndromes and obese infertility were obtained from GeneCard database. Active ingredient-target network was constructed by Cytoscape 3.7.1, and protein-protein interaction network and core target were obtained from STRING. GO and KEGG enrichment analysis were performed by Cytoscape 3.7.1 and online software. Results 125 ingredients and 218 targets of Erchen decoction were obtained. There were 2 783 target genes for obese infertility and 2 962 target genes for obese polycystic ovary syndrome. Erchen decoction has a total of 117 target genes in the treatment of obese infertility and obese polycystic ovary syndromes, which proves the principle of “treating different diseases with same method”. Potential active ingredients include quercetin, kaempferol, naringin, baicalin and formononetin. PPI showed that STAT3, JUN, AKT1, MAPK3, MAPK1, MAPK14, IL-6 and FOS were the core targets of “treating different diseases with same method”. Molecular docking results showed that quercetin, kaempferol, etc. had good binding ability with JUN. GO and KEGG enrichment analysis showed that AGE-RAGE signaling pathway, IL-17 signaling pathway and endocrine resistance might be the key pathways for the “treating different diseases with same method” of Erchen decoction. Conclusion Erchen decoction treating "different diseases with same method" involves same targets and same pathways, which can provide reference for future experimental research.
ABSTRACT
Baicalein (BE) is an active ingredient derived from the root of Scutellaria baicalensis Georgi. It is a polyhydroxyflavonoid in structure and has many biological activities. Among them, the antitumor effects of baicalein have received widespread attention. It exerts anti-tumor effects by inducing tumor cell apoptosis and invasion, inhibiting tumor angiogenesis, and eliminating free radicals. This article reviews the most recent research works of baicalein in its anti-tumor effects and mechanisms. It is aimed to provide a theoretical basis for the search and development of potential new anti-tumor drugs.
ABSTRACT
Objective To investigate the main chemical constituents of the low polarity extracts from pinusmassoniana Lamb. leaves and their synergetic activity with fluconazole against fluconazole-resistant Candida albicans. Methods The pinusmassoniana leaves were extracted with 80% ethanol, and then the extracts were extracted by petroleum ether to obtain the low polarity extracts. The chemical components were detected by GC-MS and elucidated by the comparison with the standard mass spectral data. The relative contents in percentage were calculated using the area normalization method. The minimal inhibitory concentrations (MIC80) of fluconazole-resistant Candida albicans strains by the low polarity extracts in combination with fluconazole were determined by checkerboard microdilution assay. Results 30 components were detected from the low polarity extracts, and 17 components were identified. The minimum inhibitory concentration (MIC80) of the 80% ethanol extracts, the low polarity extracts and the petroleum ether extracts from the pinusmassoniana leaves combined with fluconazole against fluconazole-resistant Candida albicans were 7.81 μg/ml, 31.25 μg/ml and >250 μg/ml, respectively. Conclusion The 80% ethanol extracts of pinusmassoniana leaves and its low polarity extracts have synergistic activity combined with fluconazole onfluconazole-resistant Candida albicans. The diterpenoids (53.99%) may be the effective components of the low polarity extracts.
ABSTRACT
Herba Monochasmae savatii, whole plant of the Monochasma savatier Franch. or Monochasma sheareri Franch. ex Maxim., scrophulariaceae, was first found in "Zhiwu Mingshi Tukao". It has the effects of clearing heat and detoxicating, dispelling wind and relieving pain, cooling the blood and stopping bleeding, etc. This review used Monochasma savatier Franch. or Monochasma sheareri Franch. ex Maxim. as the subject term to search CNKI, PubMed and SciFinder, and reviewed the classification of medicinal material, medicinal standards, chemical components, biological activities and pharmacological effects of Herba Monochasmae savatii in recent years to provide a basis for the research, development and clinical rational application.
ABSTRACT
Objective To explore the potential mechanism of Jiangzhihugan capsule (JZHG) for fatty liver (FL), and to provide a theoretical guideline for the clinical application of JZHG. Methods TCMSP and TCMID databases were used to search for the active components and targets of JZHG. GeneCards and OMIM database were used to search the FL related targets. The intersection method was used to identify the common targets of JZHG and FL. Cytoscape software was applied for the construction of active compounds-targets network map. Protein-protein interaction network was constructed by STRING software. Gene ontology functional enrichment analysis and KEGG pathway enrichment analysis were conducted with Bioconductor database and R software. Results 46 potential active components were screened out from JZHG. 7406 targets were retrieved through GeneCard and OMIM database. 118 genes were obtained from the intersection of component-target and disease-target. These genes were mainly involved with the response to oxidative stress, apoptosis, inflammatory response, hormone resistance and other biological processes. The mechanism was related to PI3K-Akt signaling pathway, human cytomegalovirus infection, microRNAs in cancer, etc. Conclusion The mechanism of active ingredients for FL in JZHG may be due to improving lipid metabolism and reducing liver fat accumulation through anti-oxidative stress and anti-inflammatory effects.
ABSTRACT
Objective To explore the potential mechanism of Qingkailing (QKL) on influenza, and to provide a theoretical basis for the clinical application of QKL. Methods TCMSP, TCMID, and PubChem databases were used to search for the active ingredients and action targets of QKL. GeneCards database was used to search for the targets of influenza. The intersection method was used to obtain the targets related to the therapeutic effects of QKL. Cytoscape software was applied for the construction of active compounds-targets network map. Protein-protein interaction network was constructed by STRING database. Gene ontology functional enrichment analysis and KEGG pathway enrichment analysis were conducted by Bioconductor database and R software. Auto Dock Tools were used for molecular docking. Results Total 90 potential active components were identified from QKL with the corresponding 225 targets. PPI network analysis showed that there were 34 key targets intervening influenza by QKL. GO and KEGG showed that the mechanism of QKL intervention on influenza was related to anti-inflammatory and antiviral. The results of molecular docking showed that cholic acid, hyodeoxycholic acid and baicalin had affinity with RELA and JUN. Conclusion The active ingredients of QKL target on JUN, RELA, MAPK1, IL6 and AKT1 to regulate multiple signal pathways, and play an intervention role in influenza.
ABSTRACT
Hepatitis C virus (HCV) is an important factor leading to chronic hepatitis, cirrhosis and hepatocellular carcinoma. Currently, there is no vaccine available to prevent HCV infection. This article reviews the natural products with anti-HCV activity discovered from plants in recent years, and classifies and summarizes them according to their mechanism of action, in order to provide a basis for discovering anti-HCV drugs from natural products.
ABSTRACT
Objective To design, synthesize and measure antifungal activities of galloyl piperazine derivatives. Methods Trimethoxyl gallic acid was used as starting material, reacted with piperazine in the presence of PyBOP/DIEA to afford the intermediates. The target compounds were obtained through the reaction with corresponding acids after deprotection gave. The antifungal activities of the target compounds were evaluated by FLC-resistant Candida albican isolated according to the CLSI recommended method. Results 11 target compounds were synthesized and six of them showed more potent antifungal activities than gallic acid. Conclusion Galloyl piperazine derivatives could enhance antifungal activities. Galloyl moiety was an important pharmacophore, which could improve antifungal activities with the introduction of cinnamic acid and 2,3-dichlorobenzoic acid.
ABSTRACT
Objective To investigate the structure and optical activity of flavonoid derivative:2-(3,4-dimethoxyphenyl)-4-oxo-4 H-chromen-3-yl acetate(4).Methods The absolute configuration was obtained by X-ray single crystal diffraction.The optical rotation of the compound was determined by the SGW ?R-1 automatic polarimeter.Results X-ray single crystal diffrac-tion showed that compound 4 belongs to the orthorhombic space group P212121with a=7.763(2)?A,b=13.930(4)?A and c=14.906(4),α= β= γ=90.00°,V =1611.91(8)?A3,Z=8.There is no hydrogen bonding between the molecules in this crystal state.The molecules maintain their stable arrangement in space by van der Waals forces.It can be seen from the single-crystal data that there is a 33.9(2)° torsion of the dimethoxy-substituted benzene ring in the compound 4 with respect to the 4 H-chromene skeleton,suggesting that there may exist optical activity.Further experimental results of the optical rotation proved that the compound has a L-rotatory,specific rotation[α]19.1D = -5.077°.Conclusion The results of the single crystal indicated that the benzene ring substituted with dimethoxy group in compound 4 has a 33.9(2)° torsion relative to the 4 H-chromene skeleton,which results in chirality and optical activity.This is the first report that non-flavonoid-glycoside has optical activity.
ABSTRACT
Objective To design and synthesize schisandrone derivatives for the therapy of disease like AD,and to meas-ure their anti-oxidation activity.Methods Ten compounds were synthesized,and seven of them were first reported.The influ-ence all the compounds on SOD from the mouse serum were measured to evaluate anti-oxidation activity.Structure-activity rela-tionship(SARs)were also discussed.Results Compounds 2,3,5 and 8 could increase the activity of SOD in mouse serum.Fur-thermore,Compounds 2,3 and 5 showed better activities than schisandrone.Conclusion Synthesized schisandrone derivatives showed anti-oxidation activity.The SARs demonstrated the carbonyl of C-1 position and the methyls of C-2 and 3 had no influ-ences to the anti-oxidant activity.
ABSTRACT
Objective A series of 4 substituted salidroside derivatives were designed and synthesized .Their anti-fatigue effects were investigated .Methods With five-acetyl glucose and different 4-substituted benzyl tyrosols as the starting materi-als ,salidroside derivatives were synthesized through glycosidation and deacetylation reactions .The exercise exhaustive mice model was used to study the anti-fatigue effects of those synthesized derivatives by comparing the loading swimming time of mice .Results 10 novel salidroside derivatives were synthesized .The loading swimming tests showed that the swimming time of the mice in the positive group (salidroside) and 3a-1 group (phenethyl-β-D-glucoside) was longer than that in the control group with statistically significant difference(P<0 .05) .The swimming times for other groups were similar to control group with no statistically significant difference .Conclusion This synthetic method for salidroside derivatives was convenient and feasible for large production .The 4-hydroxyl groups on the benzene ring of salidroside and its derivatives may be the active site responsible for their anti-fatigue activity .
ABSTRACT
Objective:To analyze the curative effects of laparoscopic radical prostatectomy for the prostate cancer and the its effect on the level serum hormones levels.Methods:86 patients with prostate cancer were selected and divided into the control group and the observation group with 43 cases in each group according to the draw method.The control group was treated by open radical prostatectomy,while the observation group was treated by laparoscopic radical prostatectomy.The operation indicators,serum follicle stimulating hormone (FSH),luteinizing hormone (LH),dihydrotestosterone (DHT),free testosterone (FT),total testosterone (T),prostate specific antigen (T-PSA,F-PSA) levels,CD3+,CD4+,CD8+,CD4+/CD8+ before and after the surgery as well as the occurrence of postoperative complications were compared between two groups.Results:The operation time of observation group was significantly longer than that of the control group,and the blood loss,bowel function recovery time,hospital stay,pain scores of observation group was significantly lower or shorter than those of the control group (P＜0.05).No significant difference was found in the serum FSH,LH,DHT,FT,T,T-PSA,F-PSA levels before and after the surgery between two group(P＞0.05).The CD3+,CD4+,CD4+/CD8+ of observation group was significantly higher than those of the control group (P＜0.05),the CD8+ of observation group was lower than that of the control group(P＜ 0.05).The incidence rate of postoperative complication in the observation group was significantly lower than that of the control group (P＜0.05).Conclusion:Laparoscopic radical prostatectomy could play a similar effect with the open surgery on the tumor control,it could improve the level of serum testosterone,immune function with high safety.
ABSTRACT
Objective To optimize novel triazole antifungal compounds synthesis of key intermediates.Methods The or-thogonal experimental design is used,emphasizing on four factors including the reaction temperature,the weight ratio of mate-rial,reaction time and solvent on the yield.Results The effect of reaction temperature on the reaction yield is the most signifi-cant,followed by reaction time ;the weight ratio of material and solvent on the yield impact is not obvious.Conclusion The new technology has several advantages and yields up to about 50%,less reactive impurities,easy post processing.
ABSTRACT
Oridonin is an en-kaurene diterpenoids compound which was found to have effect on tumor in vitro.But the clinical application has been limited because of poor water solubility,low bioavailability and oral absorption.Many scholars conducted a large number of structure modification researches of oridonin to search for new diterpenes with higher bio-activities and better bio-availabilities,and to develop new antitumor drugs.In this paper,studies on this aspect of oridonin were re-viewed.
ABSTRACT
Fluconazole,the third generation of triazole-antifungal drug,becomes the first choice in the treatment of fun-gal infection due to its broad antifungal spectrum,good water solubility and low toxicity.With an increasingly drug-resistant strain,developing new fluconazole derivatives is becoming an attractive topic.This review mainly indicates that people can get new fluconazole derivatives used by clinic through structural modification of fluconazole,which will give clues for advanced re-search.
ABSTRACT
Objective:To synthesize disubstituted pyridine and I-substituted propynyl carbamates and study their antimicrobial activities, searching for more potent and less toxic antimicrobial agents.Methods: The title compounds were synthesized through the process of electrophilic and nucleophilic substitution. Antimicrobial test in vitro was determined with 13 kinds of common mildews and bacteria(Aspergullus niger, aspergillus flavus, Aspergillus versicolor,Trichoderma viride, Paecilomium varioti Bainier, Chaetomium globsum, Penicillium citrinum, Cladochytrium clodospoium, Escherichia colo, Staphylococcus aureus, Pseudomonas fluorescens Bacillus fluorescens, and Bacillus megatherium). The chemical structures of all compounds were determined by IR, 1 HNMR and elementary analysis.Results: Seven disubstituted pyridine and I-substituted propynyl carbamates obtained were firstly reported. All compounds showed antimicrobial activity, especially compound 3e, who had more potent activity compared with the that of 3-iodo-2-propynyl-butyl- carbamate (IPBC). MIC of the compound 3e was between 2?10 -6 g/ml to 30?10 -6 g/ml . Conclusion: Compound 3e has the best antimicrobial activity and should be futher studied.
ABSTRACT
Objective:To investigate the chemical constituents in the roots of Angelica dahurica var.formosana.Methods: The dried rhizomes of Angelica dahurica var.formosana were chopped and extracted with 80% EtOH for 3 times under reflux.The EtOH extract was isolated by chromatography on silica gel using a gradient solvent system(PE:EtOAc & CHCl_3MeOH) and Sephadex LH-20.The structures of the contents were elucidated by nuclear magnetic resonance and MS spectral analysis.Results: Seventeen compounds were identified,namely,isoimperatorin(1),imperatorin(2),bergapten(3),alloimperatorin(4),xanthotoxol(5),cnidilin(6),byakangelicin(7),bergaptol(8),byakangelicol(9),pabulenol(10),oxypeucedanin hydrate(11),desmodimine(12),palmitic acid(13),stiamasterol(14),?-sitosterol(15),?-daucosterin(16),and sucrose(17).Conclusion: Compounds 8 and 12 have been isolated from Angelica dahurica var.formosana for the first time.Compound 12 has been firstly isolated from Umbelifera plants.All the courmarin compounds belong to linear 6,7-furanocourmarins.