Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 54
Filtrar
1.
Nat Commun ; 15(1): 1182, 2024 Feb 21.
Artículo en Inglés | MEDLINE | ID: mdl-38383554

RESUMEN

High reproductive compatibility between crops and their wild relatives can provide benefits for crop breeding but also poses risks for agricultural weed evolution. Weedy rice is a feral relative of rice that infests paddies and causes severe crop losses worldwide. In regions of tropical Asia where the wild progenitor of rice occurs, weedy rice could be influenced by hybridization with the wild species. Genomic analysis of this phenomenon has been very limited. Here we use whole genome sequence analyses of 217 wild, weedy and cultivated rice samples to show that wild rice hybridization has contributed substantially to the evolution of Southeast Asian weedy rice, with some strains acquiring weed-adaptive traits through introgression from the wild progenitor. Our study highlights how adaptive introgression from wild species can contribute to agricultural weed evolution, and it provides a case study of parallel evolution of weediness in independently-evolved strains of a weedy crop relative.


Asunto(s)
Variación Genética , Oryza , Evolución Molecular , Porosidad , Fitomejoramiento , Asia Sudoriental , Malezas/genética , Oryza/genética
2.
J Clin Nurs ; 33(2): 740-751, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-37888145

RESUMEN

AIMS AND OBJECTIVES: This study aimed to describe the knowledge, attitudes and practices (KAP) of nurses in implementing advance directives (ADs) for older patients and analyze the influencing factors before the establishment of the first advance directives act in China. DESIGN: Multicenter cross-sectional survey. The standards for reporting the STROBE checklist are used. METHODS: This cross-sectional study developed a self-designed structured questionnaire to assess nurses' knowledge, attitudes and practices about ADs. Nurses were recruited by stratified random sampling through the Nursing Departments of 12 hospitals in southwest China and were asked to fill out the questionnaire face to face about knowledge, attitudes and practices. Data were analyzed following descriptive statistics, rank-sum test and multiple linear regression. RESULTS: This study included 950 nurses. The study found that nurses were extremely supportive of ADs. Unmarried nurses had better knowledge of ADs than married ones. Nevertheless, there was a discrepancy between the participants' knowledge, attitude and practice. The participants' practice was lower (4.3%) compared with their attitude (81.9%) and knowledge (42.2%). Knowledge on, attitudes towards and standardized procedures for ADs in the workplace affected nursing practice. CONCLUSIONS: The study recommends that courses on ADs and appropriate support from medical institutions should be provided to nurses to increase their knowledge and confidence in implementing ADs. Healthcare professionals should be sufficiently equipped to implement ADs and handle their execution appropriately to provide adequate end-of-life care corresponding to patients' wishes. RELEVANCE TO CLINICAL PRACTICE: The study results inform rich insights as it discusses the numerous interrelating factors influencing these three fundamental aspects that affect the success of any AD policy by surveying the knowledge, attitudes and practices of clinical nurses. Furthermore, our results hint at distinct areas of improvement in the nursing practice to facilitate the wider implementation and acceptance of ADs in China. PATIENT OR PUBLIC CONTRIBUTION: This study involved no patient.


Asunto(s)
Conocimientos, Actitudes y Práctica en Salud , Enfermeras y Enfermeros , Humanos , Estudios Transversales , Competencia Clínica , Directivas Anticipadas , Encuestas y Cuestionarios , Actitud del Personal de Salud
3.
Biomed Pharmacother ; 164: 114902, 2023 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-37209628

RESUMEN

BACKGROUND: Intestinal mucositis (IM) is characterized by damage to the intestinal mucosa resulting from inhibition of epithelial cell division and loss of renewal capacity following anticancer chemotherapy and radiotherapy. Cytarabine (Ara-C), the main chemotherapy drug for the treatment of leukemia and lymphoma, is a frequent cause of IM. Guiqi Baizhu prescription (GQBZP) is a traditional Chinese medicine with anti-cancer and anti-inflammatory effects. PURPOSE: To determine if GQBZP can ameliorate Ara-C induced IM and identify and characterize the pharmacologic and pharmacodynamic mechanisms. STUDY DESIGN AND METHODS: IM was induced in mice with Ara-C and concurrently treated with orally administered GQBZP. Body weight and food intake was monitored, with HE staining to calculate ileal histomorphometric scoring and villus length/crypt depth. Immunoblotting was used to detect intestinal tissue inflammatory factors. M1 macrophages (M1) were labeled with CD86 by flow cytometry and iNOS + F4/80 by immunofluorescence. Virtual screening was used to find potentially active compounds in GQBZP that targeted JAK2. In vitro, RAW264.7 cells were skewed to M1 macrophage polarization by lipopolysaccharide (LPS) and interferon-γ (INF-γ) and treated orally with GQBZP or potential active compounds. M1 was labeled with CD86 by flow cytometry and iNOS by immunofluorescence. ELISA was used to detect inflammatory factor expression. Active compounds against JAK2, p-JAK2, STAT1 and p-STAT1 were identified by western blotting and HCS fluorescence. Molecular dynamics simulations and pharmacokinetic predictions were carried out on representative active compounds. RESULTS: Experimental results with mice in vivo suggest that GQBZP significantly attenuated Ara-C-induced ileal damage and release of pro-inflammatory factors by inhibiting macrophage polarization to M1. Molecular docking was used to identify potentially active compounds in GQBZP that targeted JAK2, a key factor in macrophage polarization to M1. By examining the main components of each herb and applying Lipinski's rules, ten potentially active compounds were identified. In vitro experimental results suggested that all 10 compounds of GQBZP targeted JAK2 and could inhibit M1 polarization in RAW264.7 cells treated with LPS and INF-γ. Among them, acridine and senkyunolide A down-regulated the expression of JAK2 and STAT1. MD simulations revealed that acridine and senkyunolide A were stable in the active site of JAK2 and exhibited good interactions with the surrounding amino acids. CONCLUSIONS: GQBZP can ameliorate Ara-C-induced IM by reducing macrophage polarization to M1, and acridine and senkyunolide A are representative active compounds in GQBZP that target JAK2 to inhibit M1 polarization. Targeting JAK2 to regulate M1 polarization may be a valuable therapeutic strategy for IM.


Asunto(s)
Mucositis , Ratones , Animales , Mucositis/patología , Citarabina/farmacología , Lipopolisacáridos/farmacología , Lipopolisacáridos/metabolismo , Simulación del Acoplamiento Molecular , Macrófagos/metabolismo , Interferón gamma/metabolismo
4.
Phytomedicine ; 114: 154744, 2023 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-36934667

RESUMEN

BACKGROUND: Acute lung injury (ALI) has the attribution of excessive inflammation of the lung. Jinzhen oral liquid (JO), a famous Chinese recipe used to treat ALI, has a favorable therapeutic effect on ALI. However, its anti-inflammatory mechanism has not been extensively studied. PURPOSE: This study was to elucidate the effects of JO on lipopolysaccharide (LPS)-induced ALI and its molecular mechanism. METHODS: An ALI model was established by intratracheal instillation of LPS (2 mg/50 µl). The open field experiment was carried out to explore the spontaneous movement and exploratory behavior of ALI mice. Cytokines levels concentrations (IL-6, IL-10 and TNF-α) were determined by enzyme-linked immunosorbent assay (ELISA). Network pharmacology was used to predict the mechanism of JO against ALI. Immunofluorescence, co-immunoprecipitation, fluorescence resonance energy transfer (FRET), Western blot and RT-PCR were used to verify the molecular mechanisms of JO. RESULTS: The in vivo results suggested that JO (1, 2, 4 g/kg) dose-dependently improved the exercise performance of mice and reduced the lung W/D weight ratio as well as the production of IL-6 and TNF-α, but increased the release of IL-10 in the ALI group. The network pharmacological analysis demonstrated that the Toll-like receptor (TLR) pathway might be the fundamental action mechanisms of JO against ALI. Immunofluorescence staining and co-immunoprecipitation analysis showed that JO decreased the expression levels of TLR4 and MyD88 and reduced their interaction in the lung tissue of ALI mice. Meanwhile, JO decreased nuclear translocation and phosphorylation of NF-κB P65. The results from cellular experiments were in line with those in vivo. The FRET experiment also confirmed that JO disturbed the interaction of TLR4 and MyD88. Subsequently, we also found that the six indicative components of JO have the similar therapeutic effect as JO. CONCLUSIONS: In summary, we suggested that JO suppressed the TLR4/MyD88/NF-κB signaling pathway, thus inhibiting LPS-induced ALI in vitro and in vivo. The clarified mechanism provided an important theoretical basis and a novel treatment strategy for the ALI treatment of JO.


Asunto(s)
Lesión Pulmonar Aguda , FN-kappa B , Humanos , FN-kappa B/metabolismo , Lipopolisacáridos/efectos adversos , Factor 88 de Diferenciación Mieloide/metabolismo , Interleucina-10/metabolismo , Receptor Toll-Like 4/metabolismo , Interleucina-6/metabolismo , Factor de Necrosis Tumoral alfa/metabolismo , Lesión Pulmonar Aguda/tratamiento farmacológico , Pulmón/metabolismo
5.
Chem Biodivers ; 20(4): e202300067, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-36810976

RESUMEN

In this phytochemical investigation, two pairs of new phenylethanoid derivative enantiomers (1a/1b and 2a/2b), a new phenylethanoid derivative 3b, and seven known compounds (3a, 4-9) were isolated from the leaves of Picrasma quassioides. Spectroscopic techniques were used for the elucidation of their chemical structures, and the absolute configurations were determined by a comparison between the experimental and calculated ECD data, as well as the application of Snatzke's method. Compounds (1a/1b-3a/3b) were measured for their production of NO levels in LPS-induced BV-2 microglial cells. The results showed that all compounds exhibited potential inhibitory effects, and compound 1a showed stronger activity than the positive control.


Asunto(s)
Antiinflamatorios , Microglía , Alcohol Feniletílico , Antiinflamatorios/química , Antiinflamatorios/farmacología , Estructura Molecular , Análisis Espectral , Estereoisomerismo , Alcohol Feniletílico/análogos & derivados
6.
Phytomedicine ; 109: 154605, 2023 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-36610133

RESUMEN

BACKGROUND: Intestinal mucositis (IM) is one of the common side effects of chemotherapy with Cytarabine (Ara-C) and contributes to the major dose-limiting factor of chemotherapy, while the effective drug for IM is little. Astragalus, one of the main active components extrated from the roots of Astragalus membranaceus (AS-IV), is a common Chinese herbal medicine used in gastrointestinal diseases. However, the effect and mechanism of AS-IV on IM is unclear. Accumulating evidence suggests that M1 macrophages play a pivotal role in IM progression. PURPOSE: The purpose of the study was to explore the protection of AS-IV and its potential molecular mechanism on intestinal mucositis injury induced by Ara-C. METHOD: The protective effect of AS-IV was investigated in LPS-induced macrophages and Ara-C-induced intestinal mucositis mouse model. H&E, immunofluorescence and western blotting were used to evaluate the damage in different doses of Ara-C. Silencing AKT targeted by siRNA was performed to explore the potential mechanisms regulating macrophage polarization effect of Ara-C, which was investigated by CCK-8, immunofluorescence and western blotting. Flow cytometry, immunofluorescence and Western blotting were used to detect macrophage surface marker proteins and inflammatory genes to explore the potential molecular mechanism of AS-IV regulating macrophage polarization. RESULTS: The Cytarabine intervention at dose of 100mg/kg significantly induced IM in mice, with the ileum the most obvious site of injury, accompanied by decreased intestinal barrier, intestinal macrophage polarization to M1 and inflammation response. The administration of AS-IV improved weight loss, food intake, ileal morphological damage, intestinal barrier destruction and inflammatory factor release in mice induced by Ara-c, and also suppressed macrophage polarization to M1, regulating in phenotypic changes in macrophages. In vitro, the expression of M1 macrophage surface marker protein was markedly decreased in LPS-induced macrophages after silencing AKT. Similarly, the western blotting of intestinal tissues and molecular docking indicated that the key mechanisms of AS-IV were remodel AKT signaling, and finally regulating M1 macrophages and decrease inflammation response. CONCLUSION: Our study highlights that AS-IV exerts protective effect in Ara-C-induced IM through inhibit polarization to M1 macrophages based on AKT, and AS-IV may serve as a novel AKT inhibitor to counteract the intestinal adverse effects of chemotherapeutic agents.


Asunto(s)
Citarabina , Mucositis , Proteínas Proto-Oncogénicas c-akt , Animales , Ratones , Citarabina/efectos adversos , Inflamación/tratamiento farmacológico , Lipopolisacáridos , Macrófagos , Proteínas de la Membrana/metabolismo , Simulación del Acoplamiento Molecular , Mucositis/inducido químicamente , Mucositis/tratamiento farmacológico , Mucositis/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo
7.
J Clin Virol ; 158: 105354, 2023 01.
Artículo en Inglés | MEDLINE | ID: mdl-36525852

RESUMEN

BACKGROUND: Respiratory syncytial virus (RSV) is one of the main pathogens that causes acute lower respiratory tract infection (ARTI) in infants. During the Coronavirus Disease 2019 (COVID-19) pandemic, although strict interventions have been implemented, RSV infection has not decreased. OBJECTIVES: To study the epidemiological and genetic characteristics of RSV circulating in Hangzhou after the peak of COVID-19. METHODS: A total of 1225 nasopharyngeal swabs were collected from outpatients with ARTIs from July 2021 to January 2022 in The Children's Hospital, Zhejiang University School of Medicine. RESULTS: A total of 267 (21.79%) of the 1225 samples were RSV positive. There was no gender bias. However, an obvious age preference for infection was observed, and children aged 3-6 years were more susceptible, which was very different from previous RSV pandemic seasons. Phylogenetic analysis of 115 sequenced RSV isolates showed that all the RSV-A viruses belong to the ON1 subtype, which could be clustered into three clusters. While all the RSV-B viruses belong to BA9. Further analysis of the mutations highlights the fixation of ten mutations, which should be given extra attention regarding their biological properties. CONCLUSION: The incidence of RSV infection in preschool children reported in this study is high. Phylogenetic analysis showed that the subtype A ON1 genotype was the dominant strain in Hangzhou from July 2021 to January 2022.


Asunto(s)
COVID-19 , Infecciones por Virus Sincitial Respiratorio , Virus Sincitial Respiratorio Humano , Infecciones del Sistema Respiratorio , Lactante , Preescolar , Humanos , Infecciones por Virus Sincitial Respiratorio/epidemiología , Filogenia , COVID-19/epidemiología , Genotipo
8.
Front Pharmacol ; 13: 993498, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36506533

RESUMEN

Osteoarthritis (OA) is a multifactorial and chronic degenerative joint disease. Due to the adverse effects of currently used drugs, a safer and more effective therapy for treating OA is needed. Peroxisome proliferator-activated receptor-γ (PPARγ) is a key protein protecting cartilage. DNMT1-mediated hypermethylation of PPARγ promoter leads to its suppression. Therefore, DNMT1 might be an effective target for exerting cartilage protective effects by regulating the epigenetic expression of PPARγ. Dabushen decoction (DD) is a representative prescription of Dunhuang ancient medical prescription, which has a potential therapeutic effect on OA. So far, the research of the efficacy and material basis of DD in the treatment of OA remains unclear. In this study, Micro-CT, HE staining, S-O staining, and immunohistochemistry analysis were used to demonstrate that DD increased the expression of PPARγ and collagen synthesis in an OA rat model. Next, the structure of DNMT1 was used to screen the active constituents of DD by molecular docking method for treatment OA. Seven potential active constituents, including isoliquiritigenin, emodin, taxifolin, catalpol, alisol A, zingerone, and schisandrin C were hited. The protective effect of the potential active constituents to chondrocytes were evaluated by protein capillary electrophoresis, immunofluorescence assays, and ex vivo culture of rat knee cartilage. The five constituents, such as alisol A, emodin, taxifolin, isoliquiritigenin, and schisandrin C could promote the expression of PPARγ and ameliorate IL-1ß-induced downregulation of collagen II and the production of MMP-13. Alisol A and Emodin could effectively mitigate cartilage damage. At last, molecular dynamics simulations with MM-GBSA method was applied to investigate the interaction pattern of the active constituents and DNMT1 complexes. The five constituents, such as alisol A, emodin, taxifolin, isoliquiritigenin, and schisandrin C achieved a stable binding pattern with DNMT1, in which alisol A has a relatively high binding free energy. In conclusion, this study elucidates that the active constituents of DD (alisol A, emodin, taxifolin, isoliquiritigenin, and schisandrin C) could ameliorate osteoarthritis via PPARγ preservation by targeting DNMT1.These findings facilitated clinical use of DD and provided a valuable strategy for developing natural epigenetic modulators from Chinese herbal formula.

9.
Zhongguo Shi Yan Xue Ye Xue Za Zhi ; 30(5): 1376-1383, 2022 Oct.
Artículo en Chino | MEDLINE | ID: mdl-36208238

RESUMEN

OBJECTIVE: To establish an optimized model of bone marrow suppression induced by cytarabine (Ara-C) in C57BL/6 mice and preliminarily explore the mechanism of myelosuppression based on the cycle and apoptosis of BMNC. METHODS: C57BL/6 mice were intraperitoneally injected with Ara-C 50, 100 and 200 mg/kg for 7 days, respectively. The survival rate and body weight of C57BL/6 mice were monitored. The number of peripheral blood cells and bone marrow nucleated cells (BMNC) was detected, and the morphology of bone marrow, thymus and spleen were measured on the 7th, 14th and 21st day of the experiment. The cycle and apoptosis of BMNC were also detected by flow cytometry. RESULTS: Ara-C 200 mg/kg caused 46.7% mortality in mice, and other doses had no significant effect on mortality. All doses of Ara-C induced bone marrow suppression in mice, as shown by a decrease in the number of peripheral blood cells (WBC, Neu, RBC, PLT) and BMNC (P<0.05), decrease in bone marrow hyperplasia, accompanied by immunosuppression and compensatory hematopoiesis of the spleen, and the above manifestations and duration were dose-dependent. Among them, the myelosuppression caused by Ara-C 50 mg/kg recovered quickly, and caused by Ara-C 200 mg/kg was too severe. The result of flow cytometry showed that Ara-C could cause S and G2/m arrest and increased apoptosis in BMNC. CONCLUSION: Ara-C can induce myelosuppression in mice with a dose-dependent severity and duration, and the model of myelosuppression with Ara-C 100 mg/kg is more optimized. The mechanism is related to the inhibition of BMNC proliferation and the promotion of apoptosis.


Asunto(s)
Enfermedades de la Médula Ósea , Citarabina , Animales , Células de la Médula Ósea , Citarabina/efectos adversos , Modelos Animales de Enfermedad , Ratones , Ratones Endogámicos C57BL
10.
Phytochemistry ; 201: 113275, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-35718134

RESUMEN

Five undescribed sesquiterpenoids stellerasespenes A‒E and four reported congeners were isolated from the roots of Stellera chamaejasme. The structures were elucidated by comprehensive spectroscopic analyses together with X-ray single crystal diffraction and theoretical calculations. The structure of holosericin B was revised. All the isolated compounds were evaluated for NO production in murine microglial BV2 cells induced by LPS. Stellerasespene A showed better inhibitory activity than the positive control minocycline, inhibiting NO production and overexpression of pro-inflammatory cytokine IL-1ß in LPS-activated BV2 cells.


Asunto(s)
Sesquiterpenos , Thymelaeaceae , Animales , Lipopolisacáridos/farmacología , Ratones , Estructura Molecular , Raíces de Plantas/química , Sesquiterpenos/química , Thymelaeaceae/química
12.
Zhongguo Zhong Yao Za Zhi ; 47(7): 1942-1954, 2022 Apr.
Artículo en Chino | MEDLINE | ID: mdl-35534265

RESUMEN

Angelicae Sinensis Radix excels in activating blood, but the scientific mechanism has not been systematically analyzed, thus limiting the development of the medicinal. This study employed the computer-aided drug design methods, such as structural similarity-based target reverse prediction, complex network analysis, molecular docking, binding free energy calculation, cluster analysis, and ADMET(absorption, distribution, metabolism, excretion, toxicity) calculation, and enzyme activity assay in vitro, to explore the components and mechanism of Angelicae Sinensis Radix in activating blood. Target reverse prediction and complex network analysis yielded 40 potential anticoagulant targets of the medicinal. Gene Ontology(GO) term enrichment and Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway enrichment analysis indicated that the targets mainly acted on the complement and coagulation cascade signaling pathway to exert the anticoagulant function. Among them, the key enzymes thrombin(THR) and coagulation factor Xa(FXa) in coagulation cascade and thrombosis were the drug targets for thromboembolic diseases. At the same time, molecular docking and cluster analysis showed that the medicinal had high selectivity for FXa. According to binding free energy score, 8 potential active components were selected for enzyme activity assay in vitro. The results demonstrated that 8 components inhibited THR and FXa, and the inhibition was stronger on FXa than on THR. The pharmacophore model of 8 active compounds was constructed, which suggested that the components had the common pharmacophore AAHH. The ADMET calculation result indicated that they had good pharmacokinetic properties and were safe. Based on target reverse prediction, complex network analysis, molecular docking and binding free energy calculation, anticoagulant activity in vitro, spatial binding conformation of molecules and targets, pharmacophore model construction, and ADMET calculation, this study preliminarily clarified the material basis and molecular mechanism of Angelicae Sinensis Radix in activating blood from the perspective of big data, and calculated the pharmacology and toxicology parameters of the active components. Our study, for the first time, revealed that the medicinal had obvious selectivity and pertinence for different coagulation proteins, reflecting the unique effect of different Chinese medicinals and the biological basis. Therefore, this study can provide clues for precision application of Angelicae Sinensis Radix and the development of the blood-activating components with modern technology.


Asunto(s)
Medicamentos Herbarios Chinos , Anticoagulantes/farmacología , Coagulación Sanguínea , Diseño de Fármacos , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Simulación del Acoplamiento Molecular
13.
Eur J Pharmacol ; 925: 174989, 2022 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-35490722

RESUMEN

Scabertopin (SCP), an abundant germacrane-type sesquiterpene lactone (SLC) isolated from Elephantopus scaber, was selected as a reference compound for modification and evaluation as anticancer agents for non-small cell lung cancer (NSCLC) treatment. All derivatives (SCP-1-SCP-13) except for SCP-3 showed potential inhibitory effect (IC50 5.2-9.7 µM) against A549 cells. The most promising compound SCP-7 also showed good cytotoxic activity against another two NSCLC cell lines (H1299 and H460), with IC50 value of 4.4 and 8.9 µM, respectively. Furthermore, SCP-7 could induce apoptotic cell death that was associated with the increased reactive oxygen species (ROS) generation, the loss of mitochondrial membrane potential, Bcl-2 family proteins modulation, caspases-3 and PARP cleavage. In addition, SCP-7 also inhibited cell growth by increasing Bax expression and reducing the Ki-67 positive cells in vivo, but there were no obvious toxic and side effects on internal organs. Mechanistically, PharmMapper, molecular docking and Western blot analysis revealed that SCP-7 might interact with the epidermal growth factor receptor (EGFR) and inhibit its expression in lung cancer cells. Together, above results suggest further effective application of SCP-7 as a potential anti-tumor agent in the treatment of NSCLC.


Asunto(s)
Antineoplásicos , Carcinoma de Pulmón de Células no Pequeñas , Neoplasias Pulmonares , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico , Apoptosis , Carcinoma de Pulmón de Células no Pequeñas/tratamiento farmacológico , Carcinoma de Pulmón de Células no Pequeñas/patología , Línea Celular Tumoral , Humanos , Lactonas/farmacología , Lactonas/uso terapéutico , Neoplasias Pulmonares/patología , Simulación del Acoplamiento Molecular , Fitoquímicos/farmacología , Especies Reactivas de Oxígeno/metabolismo , Sesquiterpenos de Germacrano/farmacología , Sesquiterpenos de Germacrano/uso terapéutico
14.
Pest Manag Sci ; 78(5): 2011-2021, 2022 May.
Artículo en Inglés | MEDLINE | ID: mdl-35118797

RESUMEN

BACKGROUND: Insect pests seriously decrease the yield and quality of agricultural crops. Resistance to commonly used insecticides is increasingly undermining their effectiveness, and therefore the development of agents with novel modes of action is desirable. Isoxazolines are a new class of insecticides that act on γ-aminobutyric acid (GABA) gated chloride channels. In this work, we used the highly active 4-triazolyphenyl isoxazoline DP-9 as a parent structure to design and synthesize a series of quaternary ammonium salt (QAS) derivatives, and we systematically evaluated their insecticidal and antifungal activities. RESULTS: Many of the synthesized QASs exhibit insecticidal activities equivalent to or higher than that of DP-9. In particular, compounds I-31 (93%, 0.00005 mg/L) and I-34 (80%, 0.00001 mg/L) showed insecticidal activities against diamondback moth larvae that were 2-10 times higher than those of fluralaner (70%, 0.0001 mg/L) and DP-9 (80%, 0.0001 mg/L), in addition to showing excellent activities against oriental armyworm, fall armyworm, cotton bollworm, corn borer, and mosquito larvae. Furthermore, all of the synthesized compounds also showed broad-spectrum fungicidal activities. CONCLUSION: The insecticidal activities of QAS derivatives of DP-9 were the same as or better than the activity of DP-9. Compounds I-31 and I-34 showed better insecticidal activities against diamondback moth larvae than fluralaner and DP-9, and thus are promising new candidates for insecticide research.


Asunto(s)
Compuestos de Amonio , Insecticidas , Mariposas Nocturnas , Animales , Diseño de Fármacos , Insecticidas/química , Larva , Estructura Molecular , Relación Estructura-Actividad
15.
J Nat Prod ; 85(2): 352-364, 2022 02 25.
Artículo en Inglés | MEDLINE | ID: mdl-35090346

RESUMEN

Two series of germacrane-type sesquiterpene lactones were produced by semisynthetic modulation of scaberol C, which was prepared by a standard chemical transformation from an Elephantopus scaber extract. Their inhibition activities against non-small-cell lung cancer cells were screened, and preliminary structure-activity relationships were also established. Among them, monomeric analog 1u and dimeric analog 3d exhibited superior anti-non-small-cell lung cancer cytotoxic potencies with IC50 values of 4.3 and 0.7 µM against A549 cells, respectively, and were more active than cisplatin and the standard sesquiterpene lactones, parthenolide and scabertopin. Further studies revealed that compounds 1u and 3d cause G2/M phase arrest and induce apoptosis through the activation of mitochondrial pathways in A549 cells. Collectively, the results obtained suggest that compounds 1u and 3d are promising anti-non-small-cell lung cancer lead compounds.


Asunto(s)
Antineoplásicos Fitogénicos , Asteraceae , Carcinoma de Pulmón de Células no Pequeñas , Neoplasias Pulmonares , Sesquiterpenos , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Asteraceae/química , Carcinoma de Pulmón de Células no Pequeñas/tratamiento farmacológico , Humanos , Lactonas/química , Lactonas/farmacología , Neoplasias Pulmonares/tratamiento farmacológico , Fitoquímicos , Sesquiterpenos/química , Sesquiterpenos/farmacología , Sesquiterpenos de Germacrano/farmacología
16.
J Int Med Res ; 49(12): 3000605211066303, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-34939882

RESUMEN

OBJECTIVE: This study was performed to compare the effectiveness and safety of vesselplasty versus vertebroplasty in the treatment of osteoporotic compression fractures with posterior wall rupture. METHODS: Patients who underwent treatment of a single osteoporotic vertebral compression fracture with posterior wall rupture from January 2016 to February 2020 were retrospectively reviewed. They were divided into a vesselplasty group (n = 17) and a vertebroplasty group (n = 43). Pain relief, radiographic outcomes, and bone cement leakage were compared between the two groups. RESULTS: There were no significant differences in the operation time, postoperative pain relief, vertebral compression recovery, or local Cobb angle improvement between the two groups. However, the overall bone cement leakage rate (29.4% vs. 67.4%) and spinal canal leakage rate (0.0% vs. 30.2%) were significantly lower in the vesselplasty group than vertebroplasty group. CONCLUSIONS: Vesselplasty offers similar pain relief and vertebral compression recovery but lower spinal canal leakage compared with vertebroplasty. Vesselplasty is thus a better option than vertebroplasty for patients with osteoporotic compression fractures with posterior wall rupture.


Asunto(s)
Fracturas por Compresión , Cifoplastia , Fracturas Osteoporóticas , Fracturas de la Columna Vertebral , Vertebroplastia , Cementos para Huesos/uso terapéutico , Fracturas por Compresión/diagnóstico por imagen , Fracturas por Compresión/cirugía , Humanos , Fracturas Osteoporóticas/complicaciones , Fracturas Osteoporóticas/diagnóstico por imagen , Fracturas Osteoporóticas/cirugía , Estudios Retrospectivos , Fracturas de la Columna Vertebral/diagnóstico por imagen , Fracturas de la Columna Vertebral/cirugía , Resultado del Tratamiento
17.
Zhen Ci Yan Jiu ; 46(5): 421-5, 2021 May 25.
Artículo en Chino | MEDLINE | ID: mdl-34085467

RESUMEN

OBJECTIVE: To evaluate the effect of electroacupuncture(EA) combined with acupoint catgut embedding the-rapy for postoperative pain after fistulotomy. METHODS: A total of 138 patients were randomly assigned into EA, acupoint catgut embedding and combination groups, with 46 patients in each group. The interventions were performed 30 min before surgery in all the three groups. The acupoints were Changqiang(GV1) and Chengshan(BL57). The visual analogue scale (VAS) score and limb activity score of the three groups at 6, 12, 24, 48 and 72 h after surgery, as well as maximum VAS score within 24 h(T24max VAS) of 1-3 d and total amounts of oral analgesic within 72 h after surgery were observed and recorded. RESULTS: The VAS score and limb activity score from the 6, 12 and 24 h after surgery, and T24max VAS score on the 1st day of the EA group were lower than those of the acupoint embedding group (P<0.05). While the VAS pain score and limb activity score at the 48 h and 72 h after surgery, and T24max VAS score at the 2nd to 3rd day, and total dose of oral analgesic within 72 h in the acupoint embedding group were lower than those of the EA group (P<0.05). The combination group was superior to the EA and acupoint embedding groups in terms of VAS score and limb activity score at different postoperative time, T24max VAS score at 1-3 d after surgery, and the total amounts of analgesic used within 72 h (P<0.05). CONCLUSION: EA combined with acupoint catgut embedding is more effective than simple EA or acupoint catgut embedding for postoperative pain after fistulotomy, with significant curative effect and no adverse reactions.


Asunto(s)
Puntos de Acupuntura , Electroacupuntura , Catgut , Extremidades , Humanos , Dolor Postoperatorio/etiología , Dolor Postoperatorio/terapia
18.
FEMS Microbiol Lett ; 368(6)2021 04 22.
Artículo en Inglés | MEDLINE | ID: mdl-33693611

RESUMEN

Russula griseocarnosa is one of the uncultivable important mycorrhizal edible fungi. Currently, there is a limited insight into the dynamic composition of the microbial communities associated with Russula. Here, the microbiota in the root and mycorrhizosphere from Russula-Fagaceae nature areas of Fujian province were identified by Illumina MiSeq high-throughput sequencing. First, we compared three types of fungal communities associated with Russula-Fagaceae root mycelia-running stage (stage-1), Russula sporocarping stage-2 (stage-2) and Russula-free Fagaceae root (stage-3). Fungal diversity negatively correlated with Russula. Russula, Tomentella and Lactarius were core EcM in Fagaceae roots. A total of eight genera, including Boletus, are likely a positive indicator of Russula sporocarp production in Russula-Fagaceae roots, while Tomentella and Elaphomyces for Russula symbiosis. Secondly, analysis of fungal and bacterial communities within rhizosphere soils from the three stages revealed six genera, including Dacryobolus and Acidocella, as possible indicator species associated with sporocarping in Russula. Elaphomyces, Tomentella, Sorangium, Acidicaldus, Acidobacterium and Haliangium occurred more frequently in the Russula rhizosphere. Furthermore, operational taxonomic unit (OTU) network analysis showed a positive correlation between Russula,Tomentella, Elaphomyces and Sorangium. Overall, our results revealed a relationship between micro-community and Russula, which may provide a new strategy for improving Russula symbiosis and sporocarp production.


Asunto(s)
Basidiomycota , Biodiversidad , Microbiota , Micorrizas , Simbiosis , Bacterias/clasificación , Bacterias/genética , China , Hongos/clasificación , Hongos/genética , Secuenciación de Nucleótidos de Alto Rendimiento , Microbiota/fisiología , Micorrizas/clasificación , Micorrizas/genética , Raíces de Plantas/microbiología , Microbiología del Suelo
19.
Chemistry ; 27(13): 4302-4306, 2021 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-33453077

RESUMEN

The catalytic enantioselective diorganozinc additions to cyclic diketones including pyrazolin-4,5-diones and isatins have been developed. In the presence of morpholine-containing chiral amino alcohol ligand, the corresponding chiral cyclic tertiary alcohols were produced in good to excellent yields (up to 97 %) and enantioselectivities (up to 95 % ee). The notable feature of this protocol includes its mild reaction conditions, Lewis acid additives free and broad functional group tolerance.

20.
Nat Prod Res ; 35(20): 3370-3375, 2021 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-31841031

RESUMEN

Two new cephalochromin derivatives, prenylcephalochromin A (1), prenylcephalochromin B (2), along with cephalochromin (3) were isolated from the Alternaria sp. ZG22 obtained from a Dasymaschalon rostratum collected from the Hainan. The structures of two new compounds were elucidated by comprehensive spectroscopic methods. Compounds 1-3 showed α-glucosidase inhibitory activity.


Asunto(s)
Alternaria , Annonaceae , Cefalosporinas , Estructura Molecular
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA
...