RESUMO
DNA damage is a key factor affecting gametogenesis and embryo development. The integrity and stability of DNA are fundamental to a woman's successful conception, embryonic development, pregnancy and the production of healthy offspring. Aging, reactive oxygen species, radiation therapy, and chemotherapy often induce oocyte DNA damage, diminished ovarian reserve, and infertility in women. With the increase of infertility population, there is an increasing need to study the relationship between infertility related diseases and DNA damage and repair. Researchers have tried various methods to reduce DNA damage in oocytes and enhance their DNA repair capabilities in an attempt to protect oocytes. In this review, we summarize recent advances in the DNA damage response mechanisms in infertility diseases such as PCOS, endometriosis, diminished ovarian reserve and hydrosalpinx, which has important implications for fertility preservation.
Assuntos
Dano ao DNA , Reparo do DNA , Infertilidade Feminina , Feminino , Humanos , Infertilidade Feminina/genética , Infertilidade Feminina/terapia , Oócitos , Síndrome do Ovário Policístico/genética , Endometriose/genética , Reserva Ovariana/fisiologia , Preservação da Fertilidade/métodosRESUMO
There is no doubt that derivation of intermediates from natural product is a very efficient way to develop new environmentally friendly pesticide. We synthesis a succession of compounds esterified with pregn-5-ene-3ß,17α,20(S)-triol to evaluate its insecticidal and bacteriostatic activity. Otherwise, their structure-activity relationships (SAR) are also discussed. As a result, compounds 7g, 7h, 7j, 7l and 7o exhibit more obvious insecticidal activity against 3rd Mythimna separata Walker (LC50 = 0.60, 0.68, 0.79, 0.85 and 0.78 mg/mL, respectively) than periplocoside F (PSF). Meanwhile, compounds 7g, 7h and 7i perform well inhibitory activity against Pseudomas syringae pv. actinidiae (Psa) in vitro (minimum inhibitory concentration (MIC) values: 0.10-0.25 mg/mL, minimum bactericidal concentration (MBC) values: 0.15-0.35 mg/mL). And SAR analysis indicates that the replacement and position of fluorine atom on benzoyl are highly vital to biological activity.
Assuntos
Produtos Biológicos , Inseticidas , Ésteres , Flúor , Testes de Sensibilidade MicrobianaRESUMO
Reflective phenomena often occur in the detecting process of pointer meters by inspection robots in complex environments, which can cause the failure of pointer meter readings. In this paper, an improved k-means clustering method for adaptive detection of pointer meter reflective areas and a robot pose control strategy to remove reflective areas are proposed based on deep learning. It mainly includes three steps: (1) YOLOv5s (You Only Look Once v5-small) deep learning network is used for real-time detection of pointer meters. The detected reflective pointer meters are preprocessed by using a perspective transformation. Then, the detection results and deep learning algorithm are combined with the perspective transformation. (2) Based on YUV (luminance-bandwidth-chrominance) color spatial information of collected pointer meter images, the fitting curve of the brightness component histogram and its peak and valley information is obtained. Then, the k-means algorithm is improved based on this information to adaptively determine its optimal clustering number and its initial clustering center. In addition, the reflection detection of pointer meter images is carried out based on the improved k-means clustering algorithm. (3) The robot pose control strategy, including its moving direction and distance, can be determined to eliminate the reflective areas. Finally, an inspection robot detection platform is built for experimental study on the performance of the proposed detection method. Experimental results show that the proposed method not only has good detection accuracy that achieves 0.809 but also has the shortest detection time, which is only 0.6392 s compared with other methods available in the literature. The main contribution of this paper is to provide a theoretical and technical reference to avoid circumferential reflection for inspection robots. It can adaptively and accurately detect reflective areas of pointer meters and can quickly remove them by controlling the movement of inspection robots. The proposed detection method has the potential application to realize real-time reflection detection and recognition of pointer meters for inspection robots in complex environments.
RESUMO
Steroids modification for improving their biological activities is one of the most efficient and fruitful methods to develop novel medicines. Steroids with aza-heterocycles attaching to the C-17 owing various biological activities have received great attentions and some of the compounds are developed successfully as drugs. In this review, the research of the syntheses and biological activities of steroids bearing various aza-heterocycles published in the last 8 years is assembled, and some important structure-activity relationships (SARs) of active compounds are presented. According to the analysis of the literatures and our experiences in this field, the potential of aza-heterocyclic steroids as medicinal drugs is proposed.
Assuntos
Compostos Heterocíclicos , Esteroides Heterocíclicos , Compostos Heterocíclicos/farmacologia , Esteroides/farmacologia , Relação Estrutura-AtividadeRESUMO
BACKGROUND: Congenital anomalies (CAs) are the leading causes for children's disabilities and mortalities worldwide. The associations between air pollution and CAs are not fully characterized in fetuses born by in vitro fertilization (IVF) who are at high risk of congenital anomalies. METHODS: We conducted a cross-sectional study including 16,971 IVF cycles from three hospitals in Hebei Province, China, 2014-2019. Air quality data was obtained from 149 air monitoring stations. Individual average daily concentrations of PM2.5, PM10, NO2, SO2, CO, and O3 were estimated by spatiotemporal kriging method. Exposure windows were divided into 5: preantral follicle period, antral follicle period, germinal period, embryonic period and early fetal period. Logistic generalized estimating equations were used to estimate the associations between air pollutants and overall or organ-system specific congenital anomalies. Negative control exposure method was used to detect and reduce bias of estimation. RESULTS: We found increasing levels of PM2.5 and PM10 were associated with higher risk of overall congenital anomalies during early fetal period, equating gestation 10-12 weeks (OR: 1.05, 95% CI: 1.02-1.09, p = 0.013 for a 10 µg/m3 increase of PM2.5; OR: 1.03, 95% CI: 1.01-1.06, p = 0.021 for a 10 µg/m3 increase of PM10). Cleft lip and cleft palate were associated with PM10 in germinal period and early fetal period. The CAs of eye, ear, face and neck were related to CO in preantral follicle stage. We did not find an association between chromosome abnormalities and air pollution exposure. CONCLUSIONS: We concluded that ambient air pollution was a risk factor for congenital anomalies in the fetuses conceived through IVF, especially exposure in early fetal period.
Assuntos
Poluentes Atmosféricos , Poluição do Ar , Poluentes Atmosféricos/análise , Poluentes Atmosféricos/toxicidade , Poluição do Ar/análise , Poluição do Ar/estatística & dados numéricos , Criança , China/epidemiologia , Estudos Transversais , Feminino , Fertilização in vitro , Humanos , Material Particulado/análise , Material Particulado/toxicidade , Parto , GravidezRESUMO
UNLABELLED: Classical swine fever virus (CSFV), a member of the genus Pestivirus within the family Flaviviridae, is a small, enveloped, positive-strand RNA virus. Due to its economic importance to the pig industry, the biology and pathogenesis of CSFV have been investigated extensively. However, the mechanisms of CSFV entry into cells are not well characterized. In this study, we used systematic approaches to dissect CSFV cell entry. We first observed that CSFV infection was inhibited by chloroquine and NH4Cl, suggesting that viral entry required a low-pH environment. By using the specific inhibitor dynasore, or by expressing the dominant negative (DN) K44A mutant, we verified that dynamin is required for CSFV entry. CSFV particles were observed to colocalize with clathrin at 5 min postinternalization, and CSFV infection was significantly reduced by chlorpromazine treatment, overexpression of a dominant negative form of the EPS15 protein, or knockdown of the clathrin heavy chain by RNA interference. These results suggested that CSFV entry depends on clathrin. Additionally, we found that endocytosis of CSFV was dependent on membrane cholesterol, while neither the overexpression of a dominant negative caveolin mutant nor the knockdown of caveolin had an effect. These results further suggested that CSFV entry required cholesterol and not caveolae. Importantly, the effect of DN mutants of three Rab proteins that regulate endosomal traffic on CSFV infection was examined. Expression of DN Rab5 and Rab7 mutants, but not the DN Rab11 mutant, significantly inhibited CSFV replication. These results were confirmed by silencing of Rab5 and Rab7. Confocal microscopy showed that virus particles colocalized with Rab5 or Rab7 during the early phase of infection within 45 min after virus entry. These results indicated that after internalization, CSFV moved to early and late endosomes before releasing its RNA. Taken together, our findings demonstrate for the first time that CSFV enters cells through the endocytic pathway, providing new insights into the life cycle of pestiviruses. IMPORTANCE: Bovine viral diarrhea virus (BVDV), a single-stranded, positive-sense pestivirus within the family Flaviviridae, is internalized by clathrin-dependent receptor-mediated endocytosis. However, the detailed mechanism of cell entry is unknown for other pestiviruses, such as classical swine fever (CSF) virus (CSFV). CSFV is the etiological agent of CSF, a highly contagious disease of swine that causes numerous deaths in pigs and enormous economic losses in China. Understanding the entry pathway of CSFV will not only advance our knowledge of CSFV infection and pathogenesis but also provide novel drug targets for antiviral intervention. Based on this objective, we used systematic approaches to dissect the pathway of entry of CSFV into PK-15 cells. This is the first report to show that the entry of CSFV into PK-15 cells requires a low-pH environment and involves dynamin- and cholesterol-dependent, clathrin-mediated endocytosis that requires Rab5 and Rab7.
Assuntos
Colesterol/metabolismo , Vírus da Febre Suína Clássica/fisiologia , Clatrina/metabolismo , Dinaminas/metabolismo , Internalização do Vírus , Proteínas rab de Ligação ao GTP/metabolismo , Proteínas rab5 de Ligação ao GTP/metabolismo , Animais , Linhagem Celular , Endocitose , Células Epiteliais/virologia , Concentração de Íons de Hidrogênio , Suínos , proteínas de unión al GTP Rab7RESUMO
A facile one-pot two-enzyme chemoenzymatic approach has been established for the gram (Neu4,5Ac2α3Lac, 1.33 g) and preparative scale (Neu4,5Ac2α3LNnT) synthesis of monotreme milk oligosaccharides. Other O-acetyl-5-N-acetylneuraminic acid (Neu4,5Ac2)- or 4-O-acetyl-5-N-glycolylneuraminic acid (Neu4Ac5Gc) -containing α2-3-sialosides have also been synthesized in the preparative scale. Used as an effective probe, Neu4,5Ac2α3GalßpNP was found to be a suitable substrate by human influenza A viruses but not bacterial sialidases.
Assuntos
Leite/química , N-Acilneuraminato Citidililtransferase/metabolismo , Oligossacarídeos/biossíntese , Ácidos Siálicos/biossíntese , Sialiltransferases/metabolismo , Animais , Leite/metabolismo , Conformação Molecular , Oligossacarídeos/química , Ácidos Siálicos/químicaRESUMO
BACKGROUND: Classical swine fever (CSF) caused by CSF virus (CSFV) is highly contagious andcauses significant economic losses in the pig industry throughout the world. Previously we demonstrated that porcine Mx1 (poMx1), when fused to HIV Tat protein transduction domain (PTD), inhibits CSFV propagation in PK-15 cells, but it is unknown whether PTD-poMx1 exhibits antiviral activity in other porcine lines and it is efficacious for controlling CSFV infection in pigs in China. METHODS: Two porcine cell lines, ST and 3D4/21, were used to investigate in vitro antiviral activity of PTD-poMx1 against CSFV using confocal microscopy, western blot, flow cytometry, and real-time RT-PCR. Furthermore, in vivo antiviral activity of PTD-poMx1 was assessed by means of rectal temperature, clinical score, pathological lesion, white blood cell count, viral load, etc. RESULTS: PTD-poMx1 entered both cell lines within 3 h and maintained for 16 h, but did not affect CSFV binding and uptake. Viral titers and qRT-PCR data showed that PTD-poMx1 inhibited CSFV replication in both cell lines, showing significant antiviral activity after infection. Injection of PTD-poMx1 into CSFV-challenged pigs attenuated CSFV symptoms and viremia in dose-dependent manner but did not completely block virus replication within 14 days post challenge, suggesting that PTD-poMx1 confers partial protection against a lethal challenge. CONCLUSION: We demonstrated the anti-CSFV activity of PTD-poMx1 in vitro and in vivo. The results have shown that treatment with PTD-poMx1 alleviated symptoms and viral load in infected pigs. The results support our previous in vitro studies and suggest that PTD-poMx1 could be promising in reducing the clinical signs caused by CSFV.
Assuntos
Vírus da Febre Suína Clássica/imunologia , Peste Suína Clássica/prevenção & controle , Vacinas Virais/uso terapêutico , Produtos do Gene tat do Vírus da Imunodeficiência Humana/genética , Animais , Western Blotting , Linhagem Celular , Vírus da Febre Suína Clássica/genética , Ensaio de Imunoadsorção Enzimática/veterinária , Citometria de Fluxo/veterinária , Técnicas In Vitro , Microscopia Confocal/veterinária , Reação em Cadeia da Polimerase em Tempo Real/veterinária , Suínos , Transdução Genética/métodos , Transdução Genética/veterinária , Vacinas Sintéticas/genética , Vacinas Sintéticas/uso terapêutico , Vacinas Virais/genética , Viremia/veterináriaRESUMO
Sixty 2-aryl-4,5-dihydrothiazoles were designed and synthesized in yields ranging from 64% to 89% from cysteine and substituted-benzonitriles via a novel metal- and catalyst-free method. The structures of the title compounds were confirmed mainly by NMR spectral data analysis. Antibacterial activity assays showed that the compounds (S)-2-(2'-hydroxyphenyl)-4-hydroxy-methyl- 4,5-dihydrothiazole (7h) and (R)-2-(2'-hydroxyphenyl)-4-hydroxymethyl-4,5-dihydro-thiazole (7h') exhibited significant inhibition against Ralstonia solanacearum, Pseudomonas syringae pv. actinidiae, Bacillus subtilis and Bacillus cereus, with minimum inhibitory concentrations (MICs) ranging from 3.91 to 31.24 µg·mL(-1). The effect of substituents showed that not only electron-withdrawing groups, but also electron-donating groups could abolish the antibacterial activities unless a 2'-hydroxy group was introduced on the 2-aryl substituent of the 4,5-dihydrothiazole analogues. The results of scanning electron microscope (SEM) and fatty acid exposure experiments indicated that these antibacterial compounds influence fatty acid synthesis in the tested bacteria.
Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Desenho de Fármacos , Tiazóis/química , Tiazóis/farmacologia , Antibacterianos/síntese química , Bactérias/efeitos dos fármacos , Bactérias/ultraestrutura , Técnicas de Química Sintética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Tiazóis/síntese químicaRESUMO
OBJECTIVE: To investigate the steroidal glycoside constituents of Solanum cumingii. METHODS: The compounds were isolated by silica gel, Sephadex LH-20, RP-C18 column and Pre-HPLC chromatography. Their structures were identified by ESI-MS and NMR. RESULTS: Six known compounds including torvoside K (1), torvoside J (2), torvoside L (3), khasianine (4), aculeatiside A (5) and solamargine (6) were isolated from Solanum cumingii. CONCLUSION: All compounds are isolated from Solanum cumingii for the first time.
Assuntos
Glicosídeos/química , Solanum/química , Cromatografia Líquida de Alta Pressão , Espectroscopia de Ressonância Magnética , Fitosteróis , Alcaloides de Solanáceas , EspirostanosRESUMO
Periplocoside NW (PSNW) with pregnane glycoside skeleton is a novel insecticidal compound isolated from the root bark of Periploca sepium Bunge. This compound has a potent stomach poisoning activity against several insect pests. In this study, we observed the intoxication symptoms, investigated the histopathological effects and carried out immuno-electron microscopic localization of PSNW on the midgut epithelium of oriental armyworm Mythimna separata Walker larvae for better understanding its action mechanism against insects. Ultrastructural observations showed that cell damages caused by PSNW in the midgut of M. separata larvae are related to the degeneration of brush border microvilli. The dissolution of cytoskeletal structures in the interior and on the surface of microvilli was responsible for the decrease in size and eventual disappearance of microvilli when bubbles of cytoplasmic substances protrude into the midgut lumen of M. separata, thus resulting in cell death. The immuno-electron microscopic localization research showed that gold particle appeared on the microvilli layer of the midgut of M. separate larvae firstly. The density of gold particle gradually added with the time, and finally microvilli layer was destructed severely. Meantime, the gold particles were also presented to the intracellular organelle membrane and the organelles also were destructed. Therefore, we proposed that this membrane system on insect midgut epithelium cells is the initial acting site of PSNW against insects.
Assuntos
Glicosídeos/toxicidade , Inseticidas/toxicidade , Mariposas/efeitos dos fármacos , Periploca/química , Extratos Vegetais/toxicidade , Pregnanos/toxicidade , Animais , Sistema Digestório/química , Sistema Digestório/efeitos dos fármacos , Sistema Digestório/ultraestrutura , Epitélio/química , Epitélio/efeitos dos fármacos , Epitélio/ultraestrutura , Histologia , Larva/química , Larva/efeitos dos fármacos , Larva/ultraestrutura , Microscopia Imunoeletrônica , Microvilosidades/química , Microvilosidades/efeitos dos fármacos , Microvilosidades/ultraestrutura , Mariposas/química , Mariposas/ultraestruturaRESUMO
BACKGROUND: To compare the expression levels of long non-coding RNA (lncRNA) and messenger RNA (mRNA) in pre-receptive endometrium between patients with Polycystic Ovary Syndrome (PCOS)and normal ovulation undergoing in vitro fertilization-embryo transfer (IVF-ET). METHODS: Endometrial tissues were collected with endometrial vacuum curette in pre-receptive phase (3 days after oocytes retrieval) from PCOS and control groups. LncRNAs and mRNAs of endometrium were identified via RNA sequencing and alignments. A subset of 9 differentially expressed lncRNAs and 11 mRNAs were validated by quantitative reverse transcription polymerase chain reaction(qRT-PCR)in 22 PCOS patients and 18 ovulation patients. The function of mRNAs with differential expression patterns were explored using Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG). RESULTS: We found out 687 up-regulated and 680 down-regulated mRNAs, as well as 345 up-regulated and 63 down-regulated lncRNAs in the PCOS patients in contrast to normal ovulation patients. qRT-PCR was used to detect the expression of 11 mRNAs, and validated that the expression of these 6 mRNAs CXCR4, RABL6, OPN3, SYBU, IDH1, NOP10 were significantly elevated among PCOS patients, and the expression of ZEB1 was significantly decreased. qRT-PCR was performed to detect the expression of 9 lncRNAs, and validated that the expression of these 7 lncRNAs IDH1-AS1, PCAT14, FTX, DANCR, PRKCQ-AS1, SNHG8, TPT1-AS1 were significantly enhanced among PCOS patients. Bioinformatics analysis showed that differentially expressed genes (DEGs) involved KEGG pathway were tyrosine metabolism, PI3K-Akt pathway, metabolic pathway, Jak-STAT pathway, pyruvate metabolism, protein processing in endoplasmic reticulum, oxidative phosphorylation and proteasome. The up-regulation of GO classification was involved in ATP metabolic process, oxidative phosphorylation, RNA catabolic process, and down-regulation of GO classification was response to corticosteroid, steroid hormone, and T cell activation. CONCLUSION: Our results determined the characteristics and expression profile of endometrial lncRNAs and mRNAs in PCOS patients in pre-receptive phase, which is the day 3 after oocytes retrival. The possible pathways and related genes of endometrial receptivity disorders were found, and those lncRNAs may be developed as a predictive biomarker of endometrium in pre-receptive phase.
Assuntos
Síndrome do Ovário Policístico , RNA Longo não Codificante , Humanos , Feminino , RNA Mensageiro/metabolismo , RNA Longo não Codificante/metabolismo , Síndrome do Ovário Policístico/genética , Janus Quinases/genética , Janus Quinases/metabolismo , Fosfatidilinositol 3-Quinases/genética , Transdução de Sinais , Fatores de Transcrição STAT/genética , Fatores de Transcrição STAT/metabolismo , Perfilação da Expressão Gênica , Transferência Embrionária , Endométrio/metabolismo , Fertilização in vitro , Redes Reguladoras de Genes , Opsinas de Bastonetes/genética , Opsinas de Bastonetes/metabolismoRESUMO
To maintain the health of aquaculture fish, it is critical to understand the composition of microorganisms in aquaculture water and sediment and the factors affecting them. This study examined the water and sediment microbiota compositions of four different types of ponds in South China that were used to culture grass carp (Ctenopharyngodon idella) of different sizes through high-throughput sequencing of the 16S rRNA gene, and analyzed their correlations with environmental factors. The results showed that ponds with cultured grass carp of different sizes exhibited significant differences in terms of water physicochemical properties and composition of water and sediment microbiota. Furthermore, the exchange of microorganisms between water and sediment microbiota was lowest in ponds with the smallest grass carp and highest in ponds with the largest grass carp. All detected environmental factors except water temperature were significantly correlated with the water microbiota, and all detected environmental factors in the sediment were correlated with sediment microbiota. Moreover, Aeromonas hydrophila and Vibrio were significantly increased in the water microbiota, especially in ponds with small juvenile grass carp, implying an increased risk of A. hydrophila and Vibrio infections in these environments. Our results provide useful information for the management of grass carp aquaculture ponds.
Assuntos
Carpas , Microbiota , Animais , Lagoas , RNA Ribossômico 16S/genética , China , Microbiota/genética , ÁguaRESUMO
The larvicidal activity of crude petroleum ether, ethyl acetate, and methanol extracts of the whole plants of Phryma leptostachya L. was assayed for its toxicity against the early fourth instar larvae of Culex pipiens pallens. The larval mortality was observed after 24 h of exposure. Among three solvent extracts from Phyrma leptostachya L., the petroleum ether extract exhibited the best larvicidal activity. The corresponding LC50 values of petroleum ether, ethyl acetate, and methanol extracts were 3.23, 5.23, and 61.86 ppm against the early fourth instar larvae of Culex pipiens pallens. The petroleum ether extract was successively subjected to column chromatography and preparative high performance liquid chromatography, and yielded the three lignans, phrymarolin-I, haedoxane A, and haedoxane E, which were isolated and identified as new mosquito larvicidal compounds. Phrymarolin-I, haedoxane A, and haedoxane E showed high larvicidal activity, for which the lethal doses LC50 were estimated at 1.21, 0.025, and 0.15 ppm against the early fourth instar larvae of Culex pipiens pallens, respectively. The structures were elucidated by analyses of IR, UV, MS, and NMR spectral data. This is the first report on the mosquito larvicidal activity of the three compounds, phrymarolin-I, haedoxane A, and haedoxane E from Phyrma leptostachya L.
Assuntos
Benzodioxóis/análise , Benzodioxóis/farmacologia , Culex/efeitos dos fármacos , Inseticidas , Larva/efeitos dos fármacos , Lignanas/análise , Lignanas/farmacologia , Magnoliopsida/química , Extratos Vegetais/farmacologia , Animais , Culex/crescimento & desenvolvimento , Extratos Vegetais/químicaRESUMO
BACKGROUND: High-dose chemotherapy combined with autologous stem cell rescue (HDCT + ASCR) has been used to treat newly diagnosed medulloblastoma, but there was no high-level evidence to support its efficacy. METHODS: Databases were retrieved, and patients were divided into 2 groups: group A was radiotherapy combined with HCDT + ASCR, and group B was classical radiotherapy and chemotherapy. The clinical benefit rate, progression-free survival (PFS), overall survival (OS) and toxicities data were extracted. RESULTS: 22 clinical trials met the inclusion criteria, 416 in group A and 2331 in group B. There was no difference in CBR between 2 groups (80.0% vs 71.5%, P.262). The 3-year PFS (3-y PFS) of group A was significantly better than group B (79.0% vs 69.5%, P = .004). The analysis found that there was no difference between the 2 groups of the standard risk group or the high-risk group. In the standard risk group, the 5-y PFS of group A was significantly better than group B (83.6% vs75.6%, P = .004). Comparison of 3-y OS and 5-y OS between 2 groups of all MB patients showed no difference (P = .086; P = .507), stratified analysis was the same result. The gastrointestinal toxicity in group A was significantly higher than that in group B (P = .016), and the level 3/4 ototoxicity in high-risk group A was higher than that in group B (P = .001). CONCLUSIONS: HDCT + ASCR can prolong 3-year PFS significantly, and prolong 5-y PFS significantly in the standard risk group, but increase gastrointestinal toxicity significantly for newly diagnosed medulloblastoma.
Assuntos
Neoplasias Cerebelares , Meduloblastoma , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico , Neoplasias Cerebelares/tratamento farmacológico , Humanos , Meduloblastoma/tratamento farmacológico , Células-Tronco , Transplante AutólogoRESUMO
A series of steroidal piperidone derivatives were synthesized, and their agricultural activities were evaluated against Myzus persicae, Aphis citricola, Brevicoryne brassicae Linn., and Bemisia tabaci (Gennadius). Most of the tested compounds exhibited potent insecticidal activity against these four pests. Compound I-9 displayed the highest activity against M. persicae, A. citricola, and Brevicoryne brassicae, with LC50 values of 11.3, 10.4, and 8.68 µg/mL, respectively. The mode of action test indicated that these derivatives had superior contact and systemic insecticidal activity against M. persicae. In addition, we initially explored whether the foregut and midgut might be the action sites of the target derivatives against M. persicae. Furthermore, a field trial showed that the control of compound I-9 was similar to that of acetamiprid against M. persicae, at a dose of 50 µg/mL; the control rates were 97.8 and 99.2% after 14 and 21 days, respectively. The structure-activity relationship of these analogues provided some important insights for the discovery and development of new insecticides to solve the current pesticide resistance crisis.
Assuntos
Afídeos , Inseticidas , Piperidonas , Animais , Inseticidas/farmacologia , Relação Estrutura-AtividadeRESUMO
Objective: To evaluate the pregnancy outcomes of progestin-primed ovarian stimulation (PPOS) protocol for patients with endometrioma underwent in vitro fertilization/intra-cytoplasmic sperm injection embryo transfer (IVF/ICSI-ET). Design: Observational retrospective cohort study. Setting: University affiliated reproductive center. Study Participants: 605 infertile patients with endometrioma underwent IVF/ICSI-ET from January 2016 to March 2021 were included in this study. Methods: Multivariable logistic regression analyses were conducted to determine the independent effect of controlled ovarian stimulation (COS) protocols on reproductive outcomes of first embryo transfer (ET) cycles. The live birth was primary outcome, the implantation rate, biochemical pregnancy, clinical pregnancy and ongoing pregnancy were secondary outcomes. Results: Compared to PPOS protocol, the probability of implantation showed no significant difference with ultra-long gonadotrophin-releasing hormone agonist (GnRHa) protocol and gonadotrophin-releasing hormone antagonist (GnRHant) protocol (OR 1.7, 95% CI 0.9-3.1, OR 1.2, 95% CI 0.7-2.1, respectively). The PPOS protocol was correlated with a significantly lower biochemical pregnancy and clinical pregnancy than ultra-long GnRHa protocol in the multivariable logistic regression analysis (OR 2.3, 95% CI 1.1-4.9, OR 2.4, 95% CI 1.1-5.3, respectively). However, there was no significant difference in terms of biochemical pregnancy, clinical pregnancy and ongoing pregnancy between PPOS and GnRHant protocol (OR 1.4, 95% CI 0.7-2.7, OR 1.3, 95% CI 0.7-2.4, OR 1.1, 95% CI 0.6-2.3, respectively). In addition, compared to PPOS protocol, ultra-long GnRHa protocol and GnRHant protocol demonstrated no statistical difference in ongoing pregnancy (OR 2.0, 95% CI 0.9-4.5, OR 2.1, 95% CI 0.6-2.3, respectively). Notably, the ultra-long GnRHa protocol was associated with a significant higher probability of live birth than PPOS protocol both in crude analysis and multivariable logistic regression analysis (OR 2.6, 95% CI 1.3-5.1, OR 2.5, 95% CI 1.1-5.7, respectively). Nevertheless, no statistical difference was found in live birth between PPOS and GnRHant protocol either in crude analysis and multivariable logistic regression analysis (OR1.2, 95% CI 0.6-2.3, OR 1.2, 95% CI 0.6-2.5, respectively). Conclusions: Based on the reproductive outcomes of the first ET cycles in patients with endometrioma, PPOS protocol may associated with inferior reproductive outcomes in terms of biochemical pregnancy, clinical pregnancy and live birth than ultra-long GnRHa protocol. However, there was no significant difference in implantation rate, clinical pregnancy, ongoing pregnancy and live birth between PPOS and GnRHant protocol.
Assuntos
Endometriose , Progestinas , Endometriose/tratamento farmacológico , Feminino , Fertilização in vitro/métodos , Antagonistas de Hormônios , Humanos , Estudos Observacionais como Assunto , Indução da Ovulação/métodos , Gravidez , Estudos RetrospectivosRESUMO
Objective: The aim of this study is to investigate the optimal estradiol (E2) level on the day of gonadotropin-releasing hormone antagonist (GnRH-ant) initiation to maximize the clinical pregnancy rate (CPR) after fresh embryo transfer among patients with simple tubal factor infertility. Methods: A retrospective cohort study was conducted in the Reproductive Medicine Center, the Second Hospital of Hebei Medical University. A total of 1,493 IVF-ET cycles of patients diagnosed with single tubal factor infertility from August 2016 to August 2021 were included and equally allocated into five distinct groups according to the quintile serum E2 levels on the day of GnRH-ant initiation. The five groups had similar baseline data except for antral follicle count. Results: The serum E 2 level on GnRH-ant initiation day was determined as an independent predictor of clinical pregnancy after adjusting for confounding factors such as age, infertility duration, body mass index, cycle number, antral follicle count, and the number of transferred embryos. Through smooth curve fitting, we found that, with the increase of serum E2 levels on the day of GnRH-ant initiation, CPR showed a trend of slight increase and then slight decrease. The maximal CPR was achieved when the serum E2 level on GnRH-ant initiation day was 498 pg/ml. When E2 was less than 498 pg/ml, the odds ratio (OR) of clinical pregnancy was 1.05 (95% CI: 1.00, 1.11, P = 0.0583). When E2 was greater than 498 pg/ml, the OR of clinical pregnancy was 0.97 (95% CI: 0.95, 0.98, P = 0.0003). Furthermore, CPR remained high when E2 was 436.8-658.6 pg/ml but declined significantly by more than 40% when E2 was ≥ 894.4 pg/ml (P < 0.05). Conclusions: The serum E2 level should be considered as an adjuvant parameter for GnRH-ant initiation. The best E2 value was 498 pg/ml, and GnRH-ant administration could be recommended to initiate when serum E2 was 436.8-658.6 pg/ml. If GnRH-ant was initiated when serum E2 was above 894.4 pg/ml, then the CPR after fresh embryo transfer may decline dramatically, and thus, cancellation of fresh embryo transfer and earlier initiation of GnRH-ant in future cycles should be considered.
Assuntos
Fertilização in vitro , Infertilidade , Estradiol , Feminino , Hormônio Liberador de Gonadotropina , Antagonistas de Hormônios/uso terapêutico , Humanos , Gravidez , Estudos RetrospectivosRESUMO
The ultrastructural effects of ingested Celangulin V (CA-V), an insecticidal component extracted from the root bark of Chinese bittersweet (Celastrus angulatus Maxim), on the midgut epithelial cells of the oriental armyworm larva (Mythimna separata Walker) were studied. Transmission electron microscopy showed that CA-V could induce a severe, time-dependent cytotoxicity of the midgut epithelial cells, which had large cytoplasmic spaces, disrupted microvilli and swollen mitochondria. The cisternae of the rough endoplasmic reticulum were excessively dilated, vesiculated and then fragmented. The nuclei were pycnotic and contained one or two divided nucleoli and agglomerated chromatin. Numerous lysosome-like vacuoles and secretion granules were observed. Finally, the CA-V resulted in cell death by necrosis with plasma membrane lysis and the cytoplasm content leakage into the migdut lumen.
Assuntos
Trato Gastrointestinal/efeitos dos fármacos , Haptenos/toxicidade , Inseticidas/toxicidade , Mariposas/efeitos dos fármacos , Extratos Vegetais/toxicidade , Animais , Retículo Endoplasmático/efeitos dos fármacos , Retículo Endoplasmático/ultraestrutura , Células Epiteliais/efeitos dos fármacos , Células Epiteliais/ultraestrutura , Trato Gastrointestinal/ultraestrutura , Microscopia Eletrônica de Transmissão , Microvilosidades/efeitos dos fármacos , Microvilosidades/ultraestrutura , Mariposas/ultraestruturaRESUMO
The title mol-ecule, C(17)H(20)O(3)S, displays a U-shaped structure; the two benzene rings are nearly parallel and partially overlapped to each other, the dihedral angle and centroid-to-centroid distance being 15.0â (2)° and 3.723â (2)â Å. In the crystal, weak inter-molecular C-Hâ¯O hydrogen bonds link the mol-ecules, forming supra-molecular chains running along the a axis.