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1.
J Am Chem Soc ; 146(8): 5316-5323, 2024 Feb 28.
Article in English | MEDLINE | ID: mdl-38364304

ABSTRACT

Efficient synthesis of enantioenriched amines is of great importance due to their significant synthetic and biological applications. Photoredox-mediated asymmetric α-amino C(sp3)-H functionalization offers an atom-economical and sustainable approach to access chiral amines. However, the development of analogous reactions is in its early stages, generally affording chiral amines with a single stereocenter. Herein, we present a novel synergistic triple-catalysis approach for the asymmetric α-C-H addition of readily available N-sulfonyl amines to aldehydes under mild conditions. This method allows for the efficient synthesis of a diverse array of valuable ß-amino alcohols bearing vicinal stereocenters. Unlike previous reports, our protocol employs a radical approach using earth-abundant Cr catalysis. Quinuclidine plays a dual role by facilitating highly selective hydrogen-atom transfer to generate α-amino radicals and promoting the dissociation of the Cr-O bond, which is crucial for the overall catalytic cycle as evidenced by control, NMR, and DFT experiments. Preliminary mechanistic studies, including radical trapping, nonlinear effect, Stern-Volmer plot, kinetic isotope effect, and Hammett plot, offer valuable insights into the reaction pathway.

2.
Angew Chem Int Ed Engl ; 61(10): e202117114, 2022 03 01.
Article in English | MEDLINE | ID: mdl-35029018

ABSTRACT

α-Allenol is a versatile synthon in organic synthesis. The catalytic asymmetric synthesis of α-allenols from readily available starting materials remains a prominent challenge, especially when simultaneous control over axial and central chirality is required. Herein, we describe the Cr-catalyzed enantioconvergent allenylation of aldehydes with racemic propargyl halides to rapidly access a wide range of chiral α-allenols with adjacent axial and central chiralities. This method features excellent regio-, diastereo- and enantioselectivity control with broad substrate scope, and provides facile access to all four stereoisomers when allied with a Mitsunobu reaction. Preliminary mechanistic studies support radical-based reaction pathways. The synthetic utility is demonstrated by the application in late-stage functionalization and the formal total synthesis of (+)-varitriol.

3.
Zhongguo Dang Dai Er Ke Za Zhi ; 23(5): 513-518, 2021 May.
Article in Zh | MEDLINE | ID: mdl-34020743

ABSTRACT

OBJECTIVE: To study the change and significance of serum pentraxin-3 (PTX-3) and syndecan-4 in children with chronic heart failure (CHF). METHODS: A total of 40 children with CHF who were admitted to the Department of Pediatrics of the First Affiliated Hospital of Zhengzhou University were enrolled as the heart failure group, and 30 children who underwent physical examination in the outpatient service during the same period of time were enrolled as the control group. The serum levels of PTX-3, syndecan-4, and N-terminal pro-brain natriuretic peptide (NT-proBNP) were compared between the two groups. RESULTS: The children with CHF had significant reductions in the serum levels of PTX-3, syndecan-4, and NT-proBNP after treatment. The levels of these markers in children with CHF were significantly higher than the control group before and after treatment (P < 0.05). The CHF children with grade II/III/IV cardiac function had significantly higher serum levels of PTX-3 and syndecan-4 than the control group (P < 0.05). The levels of PTX-3 and syndecan-4 were related to the severity of cardiac function. Compared with the grade II cardiac function group, the grade IV cardiac function group had significant increases in the serum levels of PTX-3 and syndecan-4 (P < 0.05). The serum level of PTX-3 was positively correlated with that of syndecan-4 in children with CHF (rs=0.999, P < 0.05); the serum level of PTX-3 was positively correlated with NT-proBNP, left ventricular mass index (LVMI), and cardiac function grade (rs=0.726, 0.736, and 0.934 respectively, P < 0.05) and was negatively correlated with left ventricular ejection fraction (LVEF) and left ventricular fractional shortening (LVFS) (rs=-0.852 and -0.767 respectively, P < 0.05); the serum level of syndecan-4 was positively correlated with NT-proBNP, LVMI, and cardiac function grade (rs=0.733, 0.743, and 0.934 respectively, P < 0.05) and was negatively correlated with LVEF and LVFS (rs=-0.856 and -0.771 respectively, P < 0.05). CONCLUSIONS: Serum PTX-3 and syndecan-4 may be involved in the development and progression of ventricular remodeling in children with CHF and may be used as markers for the diagnosis, cardiac function grading, and treatment outcome evaluation of children with heart failure.


Subject(s)
Heart Failure , Syndecan-4 , Biomarkers , C-Reactive Protein , Child , Chronic Disease , Humans , Natriuretic Peptide, Brain , Peptide Fragments , Serum Amyloid P-Component , Stroke Volume , Ventricular Function, Left
4.
Zhongguo Dang Dai Er Ke Za Zhi ; 23(1): 84-90, 2021 Jan.
Article in Zh | MEDLINE | ID: mdl-33476543

ABSTRACT

This article summarizes and analyzes the clinical features and gene mutation characteristics of children with noncompaction of the ventricular myocardium (NVM). For the 6 children with NVM (4 boys and 2 girls), the age of onset ranged from 3 months to 12 years. Of the 6 children, 5 had arrhythmia, 3 had cardiac insufficiency, 1 had poor mental state, and 1 had chest distress and sighing. NVM-related gene mutations were detected in 4 children, among whom 2 had MYH7 gene mutation, 1 had PRDM16 gene mutation, and 1 had mutations in the ACTN2 and TNNT2 genes. Four children had improvement in cardiac function. The two children with no significant improvement in cardiac function had a younger age of onset, a greater reduction in systolic function on echocardiography, and greater increases in myocardial enzyme and N-terminal pro-brain natriuretic peptide. It is concluded that for children with the initial symptoms of chest distress, sighing, arrhythmia, enlarged heart shadow, and increased myocardial enzyme, echocardiography and cardiac magnetic resonance are recommended for the diagnosis of NVM. NVM can have various genetic mutations.


Subject(s)
Cardiomyopathies , Heart Ventricles , Child , Child, Preschool , Echocardiography , Female , Heart Ventricles/diagnostic imaging , Humans , Infant , Male , Mutation , Myocardium
5.
Zhongguo Dang Dai Er Ke Za Zhi ; 21(4): 332-336, 2019 Apr.
Article in Zh | MEDLINE | ID: mdl-31014424

ABSTRACT

OBJECTIVE: To study the association of exposure to polycyclic aromatic hydrocarbons (PAH) during pregnancy and autism spectrum disorder (ASD)-related behaviors in toddlers. METHODS: A total of 348 toddlers who had accepted the measurement of PAH-DNA adduct in umbilical cord blood and evaluation of behavior problems at the age of 36 months were enrolled in this birth cohort study. Child Behavior Checklist (CBCL) and Autism Behavior Checklist (ABC) were used to evaluate behavior problems at the age of 36 months. The correlation of the concentration of PAH-DNA adduct in umbilical cord blood with CBCL and ABC scores at the age of 36 months were analyzed. RESULTS: The detection rate of PAH-DNA adduct in umbilical cord blood was 52.3%, and the median concentration was 0.68 ng/mL. The median total scores of CBCL and ABC scales were 23 and 8 respectively. In children aged 36 months, the concentration of PAH-DNA adduct was positively correlated with the score of social withdrawal in the CBCL scale (rs=0.205, P<0.05), the total score of the ABC scale (rs=0.412, P<0.05), and the self-care score of the ABC scale (rs=0.355, P<0.05). The concentration of PAH-DNA adduct was closely associated with the total score of the ABC scale in children aged 36 months (ß=0.122, P<0.05). CONCLUSIONS: PAH exposure during pregnancy may be a risk factor for ASD-related behaviors in toddlers. Effective reduction of PAH exposure during pregnancy and detection of PAH-DNA adduct in neonatal umbilical cord blood are of vital importance for early prevention, screening and intervention of ASD.


Subject(s)
Autism Spectrum Disorder , Polycyclic Aromatic Hydrocarbons/adverse effects , Prenatal Exposure Delayed Effects , Autism Spectrum Disorder/chemically induced , Child Behavior , Child, Preschool , Cohort Studies , Female , Fetal Blood , Humans , Pregnancy , Prenatal Exposure Delayed Effects/chemically induced
6.
Yi Chuan ; 38(2): 144-54, 2016 02.
Article in Zh | MEDLINE | ID: mdl-26907778

ABSTRACT

Recent years have witnessed the rapid development of the clustered regularly interspaced short palindromic repeats/CRISPR-associated protein(CRISPR/Cas9)system. In order to realize gene knockout with high efficiency and specificity in zebrafish, several labs have synthesized distinct Cas9 cDNA sequences which were cloned into different vectors. In this study, we chose two commonly used zebrafish-codon-optimized Cas9 coding sequences (zCas9_bz, zCas9_wc) from two different labs, and utilized them to knockout seven genes in zebrafish embryos, including the exogenous egfp and six endogenous genes (chd, hbegfa, th, eef1a1b, tyr and tcf7l1a). We compared the knockout efficiencies resulting from the two zCas9 coding sequences, by direct sequencing of PCR products, colony sequencing and phenotypic analysis. The results showed that the knockout efficiency of zCas9_wc was higher than that of zCas9_bz in all conditions.


Subject(s)
CRISPR-Cas Systems , Codon/genetics , Embryo, Nonmammalian/metabolism , Zebrafish Proteins/genetics , Zebrafish/genetics , Amino Acid Sequence , Animals , Animals, Genetically Modified , Base Sequence , Embryo, Nonmammalian/embryology , Female , Gene Expression Regulation, Developmental , Green Fluorescent Proteins/genetics , Green Fluorescent Proteins/metabolism , Male , Molecular Sequence Data , RNA, Messenger/genetics , RNA, Messenger/metabolism , Sequence Homology, Amino Acid , Time Factors , Zebrafish/embryology , Zebrafish Proteins/metabolism
7.
Zhongguo Zhong Yao Za Zhi ; 41(16): 2998-3001, 2016 Aug.
Article in Zh | MEDLINE | ID: mdl-28920338

ABSTRACT

The endophytic fungi HL-Y-3, which was isolated from the healthy leaves of Coptis chinensis, produced berberine when grown in the PDA culture medium. The presence of berberine was confirmed by the chromatographic and spectroscopic analyses. The yield of berberine was recorded as 9.313 µg•g⁻¹ by HPLC. The strain HL-Y-3 was identified as Alternaria sp.by morphological observation and 5.8S rDNA-ITS sequence analysis.The separation and purification of constituents were performed by PTLC. The mass spectrometry (MS) of the analyte was shown to be identical with authentic berberine.Further analysis with nuclear magnetic resonance (NMR) spectroscopy to showed that the chemical structure of the fungal berberine was identical with authentic berberine. The research provided new resources for the utilization of berberine.


Subject(s)
Alternaria/chemistry , Berberine/isolation & purification , Coptis/microbiology , Chromatography, High Pressure Liquid , Endophytes/chemistry , Plant Leaves/microbiology
8.
Bioorg Med Chem ; 22(12): 3146-58, 2014 Jun 15.
Article in English | MEDLINE | ID: mdl-24794743

ABSTRACT

HIV integrase (IN) is an essential enzyme for the viral replication. Currently, three IN inhibitors have been approved for treating HIV-1 infection. All three drugs selectively inhibit the strand transfer reaction by chelating a divalent metal ion in the enzyme active site. Flavonoids are a well-known class of natural products endowed with versatile biological activities. Their ß-ketoenol or catechol structures can serve as a metal chelation motif and be exploited for the design of novel IN inhibitors. Using the metal chelation as a common pharmacophore, we introduced appropriate hydrophobic moieties into the flavonol core to design natural product-based novel IN inhibitors. We developed selective and efficient syntheses to generate a series of mono 3/5/7/3'/4'-substituted flavonoid derivatives. Most of these new compounds showed excellent HIV-1 IN inhibitory activity in enzyme-based assays and protected against HIV-1 infection in cell-based assays. The 7-morpholino substituted 7c showed effective antiviral activity (EC50=0.826 µg/mL) and high therapeutic index (TI>242). More significantly, these hydroxyflavones block the IN-LEDGF/p75 interaction with low- to sub-micromolar IC50 values and represent a novel scaffold to design new generation of drugs simultaneously targeting the catalytic site as well as protein-protein interaction domains.


Subject(s)
Adaptor Proteins, Signal Transducing/metabolism , Antiviral Agents/pharmacology , Chromones/pharmacology , Drug Design , Drug Discovery , Flavonoids/chemistry , HIV Integrase Inhibitors/pharmacology , HIV Integrase/chemistry , Morpholines/pharmacology , Oncogene Proteins v-fos/metabolism , Transcription Factors/metabolism , Antiviral Agents/chemical synthesis , Catalytic Domain , Chromones/chemical synthesis , HIV Integrase/metabolism , HIV Integrase Inhibitors/chemical synthesis , HIV-1/drug effects , Humans , Molecular Structure , Morpholines/chemical synthesis , Structure-Activity Relationship
9.
Int J Gynecol Cancer ; 24(3): 534-40, 2014 Mar.
Article in English | MEDLINE | ID: mdl-24557437

ABSTRACT

OBJECTIVE: AT-rich interactive domain 1A (ARID1A) is a tumor suppressor gene that encodes the BAF250a protein. Recent studies have shown the loss of ARID1A expression in several types of tumors. We aimed to investigate the clinical and pathologic role of BAF250a in endometrial carcinoma. METHODS: We examined the expression of BAF250a and its correlation with the expression of p53, estrogen receptor, progesterone receptor, glucocorticoid receptor, hypoxiainduciblefactor-1α, and vascular endothelial growth factor in normal and various malignant endometrial tissues. RESULTS: The expression of BAF250 was significantly down-regulated in endometrial carcinoma when compared with normal endometrial tissues. The loss of BAF250a expression was found in 25% of endometrial carcinoma samples but not in normal endometrial tissues, complex endometrial hyperplasia, and atypical endometrial hyperplasia samples. Subtypes of endometrial carcinoma, especially uterine endometrioid carcinoma and uterine clear cell carcinoma, had higher frequency of loss of BAF250a expression. In addition, the expression of BAF250a was positively correlated with estrogen receptor and negatively correlated with p53 in poorly differentiated endometrial adenocarcinoma. Moreover, the expression of BAF250a was significantly associated with the differentiation status of endometrial carcinoma but not associated with clinical stage, the depth of myometrial invasion, lymph node metastasis, and overall survival of patients with endometrial carcinoma. CONCLUSIONS: Our data showed that loss of BAF250a is frequently found in high-grade endometrioid and clear cell carcinomas but not in other types of endometrial carcinoma. The loss of BAF250a expression does not have prognostic value for endometrial carcinoma.


Subject(s)
Biomarkers, Tumor/metabolism , Carcinoma/pathology , Endometrial Neoplasms/pathology , Endometrium/pathology , Nuclear Proteins/metabolism , Transcription Factors/metabolism , Carcinoma/genetics , Carcinoma/metabolism , DNA-Binding Proteins , Endometrial Neoplasms/genetics , Endometrial Neoplasms/metabolism , Endometrium/metabolism , Female , Humans , Middle Aged , Prognosis
10.
Taiwan J Obstet Gynecol ; 63(2): 154-160, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38485307

ABSTRACT

The relationship between CD276 and malignancies of the female reproductive system has previously been controversial. The purpose of this study was to evaluate the predictive value of CD276 expression in clinicopathological features and prognosis of female reproductive system malignant tumors through meta-analysis. PubMed, Embase, Cochrane Library, Web of Science, CNKI and Wanfang databases were searched for studies published up to December 2022 on the role of CD276 expression in the clinicopathological features and prognosis of female reproductive system malignancies. STATA 14.0 was used for meta-analysis. A total of 10 studies were included, involving 840 patients with malignant tumors of the female reproductive system. The results showed that in terms of clinicopathological features: CD276 expression was closely related to lymph node status [OR = 2.33, 95 %CI = 1.32-4.11, P = 0.003], tumor differentiation [OR = 2.15, 95 %CI = 1.27-3.63, P = 0.004], and FIGO stage [OR = 2.58, 95 %CI = 1.44-4.61, P = 0.001] of reproductive system malignant tumors. In terms of prognosis: CD276 expression is strongly associated with shorter OS in patients with female reproductive system malignancies [HR = 3.33, 95 % CI = 1.36-8.15, P = 0.01]. CD276 may be a new target for immunotherapy and a biomarker for predicting poor prognosis of female reproductive system malignancies.


Subject(s)
Genital Neoplasms, Female , Neoplasms , Humans , Female , Prognosis , Biomarkers, Tumor/metabolism , Databases, Factual , Genitalia, Female/metabolism , Genitalia, Female/pathology , B7 Antigens
11.
Planta Med ; 79(9): 744-52, 2013 Jun.
Article in English | MEDLINE | ID: mdl-23700113

ABSTRACT

The traditional Chinese medicinal herb Danshen (Salvia miltiorrhiza), first recorded in the "Shen Nong's Herbal Classic", has long been used to treat cardiovascular conditions, although the mechanism(s) underlying its effects remain unclear. Here, an iron dextran injection (50 mg · kg⁻¹ per day) was delivered intraperitoneally to establish a mouse model for investigating the ameliorative effects of Danshen injection (low dose at 3 g · kg⁻¹ per day or high dose at 6 g · kg⁻¹ per day) on iron overload-induced cardiac damage. The iron-chelating agent deferoxamine (100 mg · kg⁻¹ per day) was administered as a positive control. The main constituents of Danshen injection, salvianic acid A (danshensu), protocatechuic aldehyde, and salvianolic acid B, were quantified at concentrations of 2.15, 0.44, and 1.01 mg · mL⁻¹, respectively, using HPLC with UV detection. Danshen injection significantly lowered cardiac iron deposition and the concentration of the lipid oxidation product malondialdehyde, as well as improved cardiac superoxide dismutase and glutathione peroxidase levels in iron-overloaded mice. Serum levels of creatine kinase, creatine kinase isoenzyme, and lactate dehydrogenase in the iron-overloaded mice were significantly elevated (up to ~ 160 %), whereas their activities were downregulated by Danshen injection by 25 ~ 35 % at the high dose and by ~ 20 % at the low dose. Morphological changes of cardiac tissue analyzed by hematoxylin and eosin staining indicated that lesions induced by iron overload could be ameliorated by Danshen injection dose-dependently. Altogether, these results illustrated that the protective effects of Danshen injection were at least in part due to decreased iron deposition and inhibition of lipid peroxidation.


Subject(s)
Drugs, Chinese Herbal/pharmacology , Heart/drug effects , Iron Overload/drug therapy , Iron Overload/physiopathology , Phenanthrolines/pharmacology , Salvia miltiorrhiza/chemistry , Animals , Benzaldehydes/analysis , Benzaldehydes/pharmacology , Benzofurans/analysis , Benzofurans/pharmacology , Catechols/analysis , Catechols/pharmacology , Chromatography, High Pressure Liquid , Creatine Kinase/blood , Disease Models, Animal , Dose-Response Relationship, Drug , Drugs, Chinese Herbal/chemistry , Glutathione Peroxidase/metabolism , Injections, Intraperitoneal , L-Lactate Dehydrogenase/blood , Lactates/analysis , Lactates/pharmacology , Male , Medicine, Chinese Traditional/methods , Mice , Myocardium/enzymology , Myocardium/pathology , Phenanthrolines/chemistry , Superoxide Dismutase/metabolism
12.
World J Clin Cases ; 11(29): 7221-7226, 2023 Oct 16.
Article in English | MEDLINE | ID: mdl-37946777

ABSTRACT

BACKGROUND: Ectopic pancreas may be unfamiliar to many people because it is rare and difficult to diagnose. However, this disease is highly susceptible to misdiagnosis and missed diagnosis. In this article, we report two cases of pancreatic heterotopia in the gastric sinus and small intestine, respectively, both of which were confirmed by histopathological examination. CASE SUMMARY: The first patient was a 43-year-old female which reported abdominal distension for 2 mo. The second was a 67-year-old female who experienced intermittent epigastric discomfort for 15 d. In both cases, there was no confirmed preoperative examination, and the postoperative pathology indicated the presence of ectopic pancreas. CONCLUSION: The diagnosis of ectopic pancreas is difficult, and is often prone to misdiagnosis and the possibility of being overlooked. Various laboratory tests and imaging tests should be carefully evaluated before surgery to achieve early detection, early diagnosis and early treatment.

13.
Nat Commun ; 13(1): 5036, 2022 08 26.
Article in English | MEDLINE | ID: mdl-36028488

ABSTRACT

The merger of photoredox and transition-metal catalysis has evolved as a robust platform in organic synthesis over the past decade. The stereoselective 1,4-functionalization of 1,3-enynes, a prevalent synthon in synthetic chemistry, could afford valuable chiral allene derivatives. However, tremendous efforts have been focused on the ionic reaction pathway. The radical-involved asymmetric 1,4-functionalization of 1,3-enynes remains a prominent challenge. Herein, we describe the asymmetric three-component 1,4-dialkylation of 1,3-enynes via dual photoredox and chromium catalysis to provide chiral allenols. This method features readily available starting materials, broad substrate scope, good functional group compatibility, high regioselectivity, and simultaneous control of axial and central chiralities. Mechanistic studies suggest that this reaction proceeds through a radical-involved redox-neutral pathway.


Subject(s)
Chromium , Catalysis , Chemistry Techniques, Synthetic , Oxidation-Reduction
14.
Bioorg Med Chem ; 19(16): 4935-52, 2011 Aug 15.
Article in English | MEDLINE | ID: mdl-21778063

ABSTRACT

HIV-1 integrase (IN) is a validated therapeutic target for antiviral drug design. However, the emergence of viral strains resistant to clinically studied IN inhibitors demands the discovery of novel inhibitors that are structurally as well mechanistically different. Herein, we describe the design and discovery of novel IN inhibitors targeting the catalytic domain as well as its interaction with LEDGF/p75, which is essential for the HIV-1 integration as an IN cofactor. By merging the pharmacophores of salicylate and catechol, the 2,3-dihydroxybenzamide (5a) was identified as a new scaffold to inhibit the strand transfer reaction efficiently. Further structural modifications on the 2,3-dihydroxybenzamide scaffold revealed that the heteroaromatic functionality attached on the carboxamide portion and the piperidin-1-ylsulfonyl substituted at the phenyl ring are beneficial for the activity, resulting in a low micromolar IN inhibitor (5p, IC(50)=5 µM) with more than 40-fold selectivity for the strand transfer over the 3'-processing reaction. More significantly, this active scaffold remarkably inhibited the interaction between IN and LEDGF/p75 cofactor. The prototype example, N-(cyclohexylmethyl)-2,3-dihydroxy-5-(piperidin-1-ylsulfonyl) benzamide (5u) inhibited the IN-LEDGF/p75 interaction with an IC(50) value of 8 µM. Using molecular modeling, the mechanism of action was hypothesized to involve the chelation of the divalent metal ions inside the IN active site. Furthermore, the inhibitor of IN-LEDGF/p75 interaction was properly bound to the LEDGF/p75 binding site on IN. This work provides a new and efficient approach to evolve novel HIV-1 IN inhibitors from rational integration and optimization of previously reported inhibitors.


Subject(s)
Adaptor Proteins, Signal Transducing/antagonists & inhibitors , Catalytic Domain/drug effects , Catechols/chemical synthesis , HIV Integrase Inhibitors/chemical synthesis , HIV-1/drug effects , Receptor, Nerve Growth Factor/antagonists & inhibitors , Salicylates/chemical synthesis , Transcription Factors/antagonists & inhibitors , Adaptor Proteins, Signal Transducing/analysis , Adaptor Proteins, Signal Transducing/drug effects , Adaptor Proteins, Signal Transducing/metabolism , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Catalytic Domain/genetics , Catechols/chemistry , Cell Line, Tumor , Drug Design , Drug Resistance, Multiple, Viral , Drug Screening Assays, Antitumor , HIV Integrase Inhibitors/chemistry , HIV Integrase Inhibitors/pharmacology , HIV-1/genetics , Humans , Metals/chemistry , Models, Molecular , Molecular Structure , Molecular Targeted Therapy , Receptor, Nerve Growth Factor/analysis , Receptor, Nerve Growth Factor/drug effects , Receptor, Nerve Growth Factor/metabolism , Salicylates/chemistry , Transcription Factors/analysis , Transcription Factors/drug effects , Transcription Factors/metabolism
15.
Zhongguo Zhong Xi Yi Jie He Za Zhi ; 31(8): 1132-4, 2011 Aug.
Article in Zh | MEDLINE | ID: mdl-21910351

ABSTRACT

The integrative medicine concepts were analyzed from a brand-new view angle of lab diagnostics. The microcosmic, objective, early diagnostic, dynamic, and multi-point features of lab diagnostics can be integrated respectively with the macroscopic concept, experience, prevention ahead of disease attack, constant changing concept, and the wholism in Chinese medicine. The concept of integrative medicine in the lab diagnostics is of far-reaching significance in the clinics, research, and teaching of Chinese medicine, as well as the discipline construction of integrative medicine diagnostics. In addition, the complementarity and compatibility of Chinese medicine and lab diagnostics are studied.


Subject(s)
Integrative Medicine , Laboratories , Medicine, Chinese Traditional/methods
16.
Ying Yong Sheng Tai Xue Bao ; 32(12): 4263-4271, 2021 Dec.
Article in Zh | MEDLINE | ID: mdl-34951267

ABSTRACT

The community characteristics of soil nematodes are an important basis for evaluating and indicating soil health. In this study, cotton fields with different continuous monocropping years (5, 10, 15, 20, and 25 years) were selected. High-throughput sequencing technology was used to explore the responses of soil properties and nematode communities to long-term continuous monocropping in cotton fields. The results showed that after 10-15 years, soil pH and soil conductivity increased significantly, and the contents of soil organic carbon, total nitrogen, available phosphorus (AP), available potassium, nitrate and soil microbial biomass carbon (MBC) decreased significantly. A total of 25 genera, 18 families, 7 orders and 3 classes of soil nematodes were identified. Among them, Helicotylenchus was the dominant genus. Parasitic nematodes were the dominant trophic groups, showing a trend of first decreasing and then increasing. Compared with other continuous monocropping years, plant parasitic nematodes increased by 9.1%-208.6% and Helicotylenchus increased by 392.0% under continuous monocropping for 25 years. With the increases of continuous monocropping duration, plant parasitic nematodes such as Tylenchorhynchus, Ditylenchus, Discopersicus, Mesocriconema, and Criconemoides were detected. After continuous monocropping for 15 years, soil nematode richness index and maturity index of free-living nematodes (MI) decreased significantly, PPI/MI increased significantly, and diversity index (Shannon) and Wasilewska index were the lowest. Soil AP and MBC were the main environmental factors affecting the changes of soil nematode communities. Our results suggested that, after 10-15 years continuous monocropping, soil nutrients were unbalanced, the diversity of soil nematodes was reduced, the stability of soil food network was deteriorated, and the parasitic nematodes were increased, which resulted in continuous monocropping obstacles in cotton.


Subject(s)
Nematoda , Soil , Animals , Carbon , China , Humans , Soil Microbiology
17.
Eur J Med Chem ; 217: 113359, 2021 May 05.
Article in English | MEDLINE | ID: mdl-33725632

ABSTRACT

A series of highly active CF3-containing 3'-(nitroisoxazole)spiro[pyrrolidin-3,2'-oxindoles] were synthesized and found to be novel glutathione peroxidase 4 (GPX4)/mouse double minute 2 (MDM2) dual inhibitors. Bioactive spirooxindole and isoxazole skeletons were combined, and the resulting compounds exhibited strong activities against both targets. In particular, compound 3d displayed excellent activity in the suppression of MDM2-mediated degradation of p53, as well as levels of GPX4, in MCF-7 breast cancer cells. Moreover, 3d also exhibited inhibitory effects on MDM2 and GPX4 in MCF-7 xenograft model to trigger ferroptotic and apoptotic cell death in in vivo experiments, which was consistent with the results of in vitro experiments.


Subject(s)
Antineoplastic Agents/pharmacology , Drug Design , Isoxazoles/pharmacology , Nitro Compounds/pharmacology , Phospholipid Hydroperoxide Glutathione Peroxidase/antagonists & inhibitors , Proto-Oncogene Proteins c-mdm2/antagonists & inhibitors , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Female , Humans , Isoxazoles/chemical synthesis , Isoxazoles/chemistry , MCF-7 Cells , Mammary Neoplasms, Experimental/drug therapy , Mammary Neoplasms, Experimental/metabolism , Mammary Neoplasms, Experimental/pathology , Mice , Molecular Structure , Nitro Compounds/chemical synthesis , Nitro Compounds/chemistry , Oxindoles/chemistry , Oxindoles/pharmacology , Phospholipid Hydroperoxide Glutathione Peroxidase/metabolism , Proto-Oncogene Proteins c-mdm2/metabolism , Pyrrolidines/chemistry , Pyrrolidines/pharmacology , Spiro Compounds/chemistry , Spiro Compounds/pharmacology , Structure-Activity Relationship
18.
J Tradit Chin Med ; 30(1): 9-12, 2010 Mar.
Article in English | MEDLINE | ID: mdl-20397453

ABSTRACT

OBJECTIVE: To observe the effects of acupuncture at different times on plasma thromboxane (TXB2) and prostaglandin 6-Keto-PGF1a (6-K-P) in patients with ischemic cerebrovascular disease. METHODS: Totally 90 patients were randomly divided into a group acupunctured at 7-9 am, a group acupunctured at 3-5 pm and a drug control group, with 30 cases in each group. The contents of plasma TXB2 and 6-K-P from venous blood before treatment were compared with those 15 days after treatment. RESULTS: The plasma TXB2 levels of the two acupuncture groups were obviously lower than those before treatment (P < 0.05, P < 0.01), but the 6-K-P levels of both the acupuncture groups were remarkably higher than those before treatment (P < 0.05, P < 0.01). and the TXB2 level in the 3-5 pm acupuncture group was obviously lower than that in the 7-9 am acupuncture group (P < 0.05), and the 6-K-P level of the former was obviously higher than that of the latter (P < 0.05). CONCLUSION: Acupuncture can promote functional recovery in patients with ischemic cerebrovascular disease and enhance their survival quality.


Subject(s)
Acupuncture Therapy , Brain Ischemia/therapy , Prostaglandins/blood , Thromboxanes/blood , Acupuncture Points , Adult , Aged , Aged, 80 and over , Brain Ischemia/blood , Female , Humans , Male , Middle Aged , Young Adult
19.
Zhonghua Zhong Liu Za Zhi ; 31(7): 505-9, 2009 Jul.
Article in Zh | MEDLINE | ID: mdl-19950697

ABSTRACT

OBJECTIVE: To examine the in vivo anti-metastatic effect of enhanced expression of CD40L cDNA in murine ovarian cancer OVHM cells (CD40L-OVHM) injected into the spleen on liver metastasis in mice. METHODS: OVHM cells were inoculated into the spleen of 6 to 8 week-old female B6C3F1 (C57BL/6N x C3H/He) mice. The established liver metastasis was identified by histopathology (HE staining). OVHM cells, DNA-pMKITneo-OVHM cells or CD40L-OVHM cells were inoculated into the spleen of female B6C3F1 mice and the expressions of CD11c in splenic cells were detected by flow cytometry. The specific cytotoxicity of splenic cells was detected by MTT assay, and the serum cytokines of IFN-gamma, TNF-alpha, IL-12, IL-4 and IL-10 of the mice were measured by enzyme linked immunoabsorbent assay. The liver metastases and the survival time of the mice were also recorded. RESULTS: The mouse models with liver metastasis by injecting tumor cells into the spleen of mice were established. The expression of CD11c and the specific killing rate in CD40L-OVHM cells group was significantly higher than that in the OVHM cells group and DNA-pMKITneo-OVHM cells group. The expressions of IFN-gamma, TNF-alpha and IL-12 in the CD40L-OVHM cells group were much more increased than OVHM cells group and DNA-pMKITneo-OVHM cells group, but the expressions of IL-4 and IL-10 in the CD40L-OVHM cells group were decreased significantly (p < 0.05). The average weights of livers and spleens of mice in CD40L-OVHM cells group were significantly lower than those of DNA-pMKITneo-OVHM cells group and OVHM cells group. The survival time of mice in CD40L-OVHM cells group was also significantly longer than that in the OVHM cells group and DNA-pMKITneo-OVHM cells group (P < 0.05). CONCLUSION: The data directly demonstrate that the expression of CD40L in ovarian cancer cells (CD40L-OVHM) can enhance the proliferation and differentiation of dendritic cells in the spleen and induce specific cytotoxic effect of T cells in the spleen, and may regulate the immune function of peripheral blood cells and the immune balance between Th1 cells and Th2 cells, which maybe the possible mechanism induced by CD40L in mice inhibiting the development of liver metastasis.


Subject(s)
CD11c Antigen/metabolism , CD40 Ligand/metabolism , Liver Neoplasms/secondary , Ovarian Neoplasms/metabolism , Animals , CD40 Ligand/genetics , Cell Differentiation , Cell Line, Tumor , Cell Proliferation , DNA, Complementary/genetics , Dendritic Cells/cytology , Female , Interferon-gamma/metabolism , Interleukin-10/metabolism , Interleukin-12/metabolism , Interleukin-4/metabolism , Liver Neoplasms/pathology , Mice , Mice, Inbred C3H , Mice, Inbred C57BL , Neoplasm Transplantation , Ovarian Neoplasms/pathology , Spleen/metabolism , T-Lymphocytes, Cytotoxic/immunology , Tumor Necrosis Factor-alpha/metabolism
20.
Ying Yong Sheng Tai Xue Bao ; 30(4): 1218-1226, 2019 Apr.
Article in Zh | MEDLINE | ID: mdl-30994282

ABSTRACT

A long-term field experiment was conducted to investigate the effects of continuous cotton production years (0 as control, 5, 10, 15 and 20 years) and straw return on soil organic carbon (SOC) structure and stability by using Fourier transform infrared spectroscopy (FTIR) in Manas River valley of Xinjiang. The results showed that the relative peak intensity of polysaccharide and aromatics decreased with increasing continuous cropping years, whereas the aliphatic and alcoholic phenols relative peak intensity and the CH/C=C increased. The content of soil particulate organic carbon (POC) increased significantly in the 5-yr of cotton production farmland and then decreased with the increases of continuous cropping years. POC content was 5.11 times higher in 5-yr than that of the control. The content of mineral-bound organic carbon (MOC) was the highest in 10-yr farmland, being 1.84 times higher than that of the control. The highest value of the ratio of POC and MOC content (ω(POC)/ω(MOC)) was observed in 5-yr farmland. Together, long-term continuous cotton production with straw return led to SOC structure aliphatic and soil mineral binding increased the protection of organic matter, thus increasing the stability of soil organic matter.


Subject(s)
Agriculture/methods , Carbon , Fertilizers , Gossypium/growth & development , Minerals , Soil , Spectroscopy, Fourier Transform Infrared
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