RESUMEN

We report herein a dynamic facet-selective capping (dFSC) strategy for α-calcium sulfate hemihydrate crystal growth from dihydrate gypsum in the presence of a catechol-derived PEI capping agent (DPA-PEI) with inspiration by the biomineralization process of mussel. The crystal shape is controllable and varies from long and pyramid-tipped prisms to thin hexagonal plate. The highly uniform truncated crystals have extremely high compression and bending strengths after hydration molding.

RESUMEN

Auxins as an important class of phytohormones play essential roles in plant life cycle; therefore, developing compounds with auxin-like properties for plant growth regulation and weed control applications is of great significance. Herein, we reported the design, synthesis, and herbicidal activity evaluation of a series of novel indole-3-carboxylic acid derivatives as auxin receptor protein TIR1 antagonists. Petri dish herbicidal activity assay demonstrated that most of the as-synthesized target compounds exhibited good-to-excellent inhibition effects (60-97% inhibitory rates) on roots and shoots of both dicotyledonous rape (B. napus) and monocotyledonous barnyard grass (E. crus-galli). The inhibition rates of compounds 10d and 10h reached up to 96% and 95% for the root of rape (B. napus) at 100 mg/L, and they also maintained 92% and 93% inhibition rates even if at 10 mg/L, respectively. Molecular docking revealed that the interactions between these synthesized target compounds and TIR1 protein include tight π-π stacking, hydrogen bond, and hydrophobic interactions. This work expands the range of auxin chemistry for the development of new auxin mimic herbicides.

RESUMEN

Objective To investigate the short- and long-term therapeutic efficacies of intravenous trans- plantation of bone marrow stem cells (MSCs) in rats with experimental myocardial infarction by meta- analysis. Methods Randomized controlled trials were systematically searched from PubMed, Science Citation Index (SCI), Chinese journal full-text database (CJFD) up to December 2014. While the experimental groups (MSCs groups) were injected MSCs intravenously, the control groups were injected Delubecco's minimum essential medium (DMEM) or phosphate buffered saline (PBS). Subgroup analysis for each outcome measure was performed for the observing time point after the transplantation of MSCs. Weighted mean differences (WMD) and 95% confidence intervals (CI) were calculated for outcome parameters including ejection fraction (EF) and fractional shortening (FS), which were measured by echocardiogram after intravenous injection and analyzed by RevMan 5.2 and STATA 12.0. Results Data from 9 studies (190 rats) were included in the meta-analysis. As compared to the control groups, the cardiac function of the experimental groups were not improved at day 7 (EF: WMD=0.08, 95%CI -1.32 to 1.16, P>0.01; FS: WMD=-0.12, 95%CI -0.90 to 0.65, P>0.01) until at day 14 after MSCs' transplantation (EF: WMD=10.79, 95%CI 9.16 to 12.42, P<0.01; FS: WMD=11.34, 95%CI 10.44 to 12.23, P<0.01), and it lasted 4 weeks or more after transplantation of MSCs (EF: WMD=13.94, 95%CI 12.24 to 15.64, P<0.01; FS: WMD=9.64, 95%CI 7.98 to 11.31, P<0.01). Conclusion The therapeutic efficacies of MSCs in rats with myocardid infarction become increasing apparent as time advances since 2 weeks after injection.

Asunto(s)

Corazón/fisiopatología , Trasplante de Células Madre Hematopoyéticas , Infarto del Miocardio/fisiopatología , Animales , Sesgo de Publicación , Ratas , Volumen Sistólico

RESUMEN

The chemoselective transformation of diarylethanones via either aerobic oxidative cleavage to give arylmethanoic acids or tandem aerobic oxidation/benzilic acid rearrangement/decarboxylation to give diarylmethanones has been developed. The transformation is controllable and applicable to a broad spectrum of substrates and affords the desired products in good to excellent yields. Mechanistic insights with control reactions, (1)H NMR tracking, and single-crystal X-ray diffraction reveal a complex mechanistic network in which two common intermediates, α-ketohydroperoxide and diarylethanedione, and three plausible pathways are proposed and verified. These pathways are interlinked and can be switched reasonably by changing the reaction conditions. This method enables scalable synthesis and access to a number of valuable compounds, including vitamin B3, diphenic acid, and the nonsteroidal anti-inflammatory drug ketoprofen. The present protocol represents a step forward in exploiting complex mechanistic networks to control reaction pathways, achieving divergent syntheses from the same class of starting materials.

RESUMEN

BACKGROUND: This study observes changes in levels of seminal nitric oxide (NO), nitric oxide synthase (NOS), macrophage migration inhibitory factor (MIF), sperm DNA integrity, chromatin condensation and Caspase-3in adult healthy men after scrotal heat stress (SHS). METHODS: Exposure of the scrotum of 25 healthy male volunteers locally at 40-43°C SHS belt warming 40 min each day for successive 2 d per week. The course of SHS was continuously 3 months. Routine semen analysis, hypo-osmotic swelling (HOS) test, Aniline blue (AB) staining, HOS/AB and terminal deoxynucleotidyl transferase-mediated d UDP nick-end labeling (TUNEL) were carried out before, during and after SHS. Seminal NO and NOS contents were determined by nitrate reduction method. The activated Caspase-3 levels of spermatozoa and MIF in seminal plasma were measured by the enzyme-linked immunosorbent assay (ELISA) method. Statistical significance between mean values was determined using statistical ANOVA tests. RESULTS: The mean parameters of sperm concentration, motile and progressive motile sperm and normal morphological sperm were significantly decreased in groups during SHS 1, 2 and 3 months compared with those in groups of pre-SHS (P<0.001). Statistically significant differences of sperm DNA fragmentation, normal sperm membrane, and Caspase-3 activity as well as the level of NO, NOS and MIF in semen were observed between the groups before SHS and after SHS 3 months and the groups during SHS 1, 2 and 3 months (P<0.001). After three months of the SHS, various parameters recovered to the level before SHS. WBC in semen showed a positively significant correlation with the levels of NO, NOS, MIF and Caspase-3 activity. The percentage of abnormal sperm by using the test of HOS showed a positively significant correlation with that of HOS/AB. CONCLUSIONS: The continuously constant SHS can impact the semen quality and sperm DNA and chromatin, which may be contributed to the high level of NO, NOS, MIF and Caspase-3 by SHS.

Asunto(s)

Caspasa 3/metabolismo , Trastornos de Estrés por Calor/genética , Trastornos de Estrés por Calor/metabolismo , Factores Inhibidores de la Migración de Macrófagos/metabolismo , Óxido Nítrico Sintasa/metabolismo , Semen/metabolismo , Espermatozoides/metabolismo , Adulto , Fragmentación del ADN , Voluntarios Sanos , Calor , Humanos , Masculino , Óxido Nítrico , Análisis de Semen , Recuento de Espermatozoides , Motilidad Espermática

RESUMEN

The aim of the study was to investigate the anti-apoptotic potency of TNFR:Fc gene in ischemia/reperfusion-induced myocardial cell injury and hypoxia/reoxygenation-induced H9c2 rat cardiomyocytes injury. Rats were randomly divided into the following groups (n=8): (1) sham operation group; (2) ischemia-reperfusion (I/R) rats treated with rAAV-EGFP; (3) I/R rats treated with rAAV-TNFR:Fc group. rAAV-EGFP or rAAV-TNFR:Fc was injected intra-myocardial at four sites on the anterior and posterior walls of left ventricle immediately after the construction of I/R-induced AMI model in rats. The effects of TNFR:Fc on apoptosis and cardiacfunction were observed after 72 h of coronary reperfusion. In the in vitro study, apoptosis was analyzed in H9c2 rat cardiomyocytes treated either with nomoxia alone, or hypoxia/reoxygenation in the presence of rAAV-GFP or rAAV-TNFR:Fc. We found that (1) TNFR:Fc gene improved cardiac function (EF, LVESP, LVEDP and dp/dt max) post I/R-induced AMI; (2) TNFR:Fc gene inhibited I/R-induced apoptosis and attenuated the level of TNF-α in serum and cardiac tissue; (3) TNFR:Fc gene prevented apoptosis in hypoxia/reoxygenation-induced H9c2 rat cardiomyocytes associated with inhibition of caspase-3 activation and normalization of ratio of the Bcl-2/Bax. We concluded that TNFR:Fc gene transfection has anti-apoptotic potency in ischemia/reperfusion-induced myocardial cell injury.

Asunto(s)

Apoptosis/genética , Daño por Reperfusión Miocárdica/genética , Miocitos Cardíacos , Receptores Fc/genética , Receptores del Factor de Necrosis Tumoral/genética , Animales , Apoptosis/efectos de los fármacos , Masculino , Daño por Reperfusión Miocárdica/patología , Daño por Reperfusión Miocárdica/prevención & control , Miocitos Cardíacos/efectos de los fármacos , Miocitos Cardíacos/patología , Ratas , Ratas Sprague-Dawley , Receptores Fc/administración & dosificación , Receptores del Factor de Necrosis Tumoral/administración & dosificación

RESUMEN

BACKGROUND: Studies of functional modules in a Protein-Protein Interaction (PPI) network contribute greatly to the understanding of biological mechanisms. With the development of computing science, computational approaches have played an important role in detecting functional modules. RESULTS: We present a new approach using multi-agent evolution for detection of functional modules in PPI networks. The proposed approach consists of two stages: the solution construction for agents in a population and the evolutionary process of computational agents in a lattice environment, where each agent corresponds to a candidate solution to the detection problem of functional modules in a PPI network. First, the approach utilizes a connection-based encoding scheme to model an agent, and employs a random-walk behavior merged topological characteristics with functional information to construct a solution. Next, it applies several evolutionary operators, i.e., competition, crossover, and mutation, to realize information exchange among agents as well as solution evolution. Systematic experiments have been conducted on three benchmark testing sets of yeast networks. Experimental results show that the approach is more effective compared to several other existing algorithms. CONCLUSIONS: The algorithm has the characteristics of outstanding recall, F-measure, sensitivity and accuracy while keeping other competitive performances, so it can be applied to the biological study which requires high accuracy.

Asunto(s)

Algoritmos , Biología Computacional/métodos , Evolución Molecular , Mapeo de Interacción de Proteínas/métodos , Proteínas Fúngicas/metabolismo , Humanos , Levaduras/metabolismo

RESUMEN

It has been reported that insulin-like growth factor 1 (IGF-1) promoted migration of endothelial cells and cardiac resident progenitor cells. In the previous study, we found the time-dependent and dose-dependent effects of IGF-1 treatment on the CXCR4 expression in MSCs in vitro, but it is still not clear whether IGF-1 pretreatment of MSCs may play anti-apoptotic and anti-inflammation role in myocardial infarction. In this study, we demonstrated that IGF-1-treated MSCs' transplantation attenuate cardiac dysfunction, increase the survival of engrafted cells in the ischemic heart, decrease myocardium cells apoptosis, and inhibit protein production and gene expression of inflammation cytokines tumor necrosis factor alpha (TNF-α), interleukin (IL)-1ß, and IL-6. IGF-1 pretreatment of MSCs may play anti-apoptotic and anti-inflammation roles in post-myocardial infarction.

Asunto(s)

Factor I del Crecimiento Similar a la Insulina/farmacología , Trasplante de Células Madre Mesenquimatosas/métodos , Células Madre Mesenquimatosas/metabolismo , Infarto del Miocardio/metabolismo , Infarto del Miocardio/terapia , Animales , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/fisiología , Inflamación/metabolismo , Inflamación/patología , Inflamación/terapia , Masculino , Células Madre Mesenquimatosas/efectos de los fármacos , Infarto del Miocardio/patología , Ratas , Ratas Sprague-Dawley

RESUMEN

A one-pot palladium-catalyzed synthesis of symmetrical and unsymmetrical diarylmethanones using acetophenone and aryl bromides as raw materials has been developed. In this reaction, acetophenone acts as a latent carbonyl donor and two pathways of palladium-catalyzed sequential coupling and aerobic oxidation are identified. The reaction is applicable to a spectrum of substrates and delivers the products in moderate to good yields. This method can be used for the synthesis of ketoprofen, a nonsteroidal anti-inflammatory drug, in a two-step procedure and 45% overall yield.

Asunto(s)

Acetofenonas/química , Hidrocarburos Bromados/química , Cetonas/síntesis química , Compuestos Organometálicos/química , Paladio/química , Catálisis , Cetonas/química , Estructura Molecular , Oxidación-Reducción

RESUMEN

BACKGROUND: Depot medroxyprogesterone acetate (DMPA) as a hormonal contraceptive is highly effective and widely used, but it may reduce bone mineral density (BMD) and increase the risk of osteoporosis. We compared BMD between users of intramuscular DMPA and nonhormonal subjects. METHODS: The study included 102 women aged between 16 and 18 years using DMPA for 24 months and 97 women aged between 16 and 18 years using nonhormonal contraception as nonusers control group. BMD of the lumbar spine and femoral neck was measured every 12 months for 24 months using dual-energy X-ray absorptiometry, comparing mean BMD changes in DMPA users and nonusers. RESULTS: There were no significant differences between groups at baseline in age, gynecologic age, body mass index (BMI), lumbar spine BMD and femoral neck BMD, etc. At 24 months of DMPA treatment, the mean percentage change from baseline in lumbar spine and femoral neck BMD values had decreased by 1.88% and 2.32%, respectively. The mean lumbar spine and femoral neck BMD in DMPA group at 24 months were not significantly different compared to baseline (P = 0.212 and P = 0.106, respectively). In comparison, in nonhormonal control group, there was a trend toward increasing BMD. At 24 months of observation, the mean percentage change from baseline in lumbar spine and femoral neck BMD had increased by 2.08% and 1.46%, respectively. There were no significant difference compared to baseline (P = 0.160 and P = 0.288, respectively). Mean BMD at the spine and femoral neck did not differ significantly between DMPA users and nonusers over 12-month, but the BMD values at both anatomical sites were significantly lower in DMPA users compared with nonusers after 24-month treatment (P = 0.009 and P = 0.009, respectively). CONCLUSION: The evidence of our study suggested that the use of DMPA for short-term (≤12-month) has no significant effects on BMD at spine and femoral neck, but long-term exposure to DMPA may prevent the bone mass accrual in adolescents.

Asunto(s)

Densidad Ósea/efectos de los fármacos , Anticonceptivos Femeninos/farmacología , Acetato de Medroxiprogesterona/farmacología , Adolescente , Femenino , Humanos

RESUMEN

OBJECTIVE: To perform a systematic review and meta-analysis of the predictive abilities of CHADS2 and CHA2DS2-VASc in stroke and thromboembolism risk stratification of atrial fibrillation (AF) patients. METHODS: We searched PubMed and EMBASE for English-language literature on comparisons of the diagnostic performance between CHADS2 and CHA2DS2-VASc in predicting stroke, or systemic embolism, in AF. We then assessed the quality of the included studies and pooled the C-statistics and 95% confidence intervals (95% CI). RESULTS: Eight studies were included. It was unsuitable to perform a direct meta-analysis because of high heterogeneity. When analyzed as a continuous variable, the C-statistic ranged from 0.60 to 0.80 (median 0.683) for CHADS2 and 0.64-0.79 (median 0.673) for CHA2DS2-VASc. When analyzed as a continuous variable in anticoagulation patients, the subgroup analysis showed that the pooled C-statistic (95% CI) was 0.660 (0.655-0.665) for CHADS2 and 0.667 (0.651-0.683) for CHA2DS2-VASc (no significant difference). For non-anticoagulation patients, the pooled C-statistic (95% CI) was 0.685 (0.666-0.705) for CHADS2 and 0.675 (0.656-0.694) for CHA2DS2-VASc (no significant difference). The average ratio of endpoint events in the low-risk group of CHA2DS2-VASc was less than CHADS2 (0.41% vs. 0.94%, P < 0.05). The average proportion of the moderate-risk group of CHA2DS2-VASc was lower than CHADS2 (11.12% vs. 30.75%, P < 0.05). CONCLUSIONS: The C-statistic suggests a similar clinical utility of the CHADS2 and CHA2DS2-VASc scores in predicting stroke and thromboembolism, but CHA2DS2- VASc has the important advantage of identifying extremely low-risk patients with atrial fibrillation, as well as classifying a lower proportion of patients as moderate risk.

RESUMEN

BACKGROUND: The aim of this study was to explore a new three-dimensional, reticular intrauterine device (3-DRIUD) composed of nitinol and silicone rubber and to observe the contraceptive effect of the device in rats. STUDY DESIGN: Two contraceptive experiments were performed. In the first, female rats underwent bilateral placement of a 20.0-35.0-mm 3-DRUID (experimental group, n=30) via an abdominal incision or a sham operation with no IUD (control group, n=30). Two weeks after the operation was performed, the rats from either group were caged together with male rats. The contraceptive effects of the 3-DRIUD were observed at 1 to 3 months postoperation, after which the 3-DRIUDs were removed. One month after this second operation, the rats from the two groups were again coupled with fertile male rats. In a second experiment, female rats underwent bilateral placement of a 10.0-mm 3-DRUID (n=5) via an abdominal incision or a two-dimensional IUD (2-DIUD, n=20) and mated 1 month after surgery. The single-pipeline IUD was placed in 10 rats, while the enfolded-pipeline IUD was placed in 10 different rats. RESULTS: In the first experiment, none of the females in the experimental 3-DRIUD group became pregnant (0/30, 0%) after 3 months, compared to 28/30 (93.3%, p<.0001) rats in the control group. After the 3-DRIUDs were removed from the experimental group after 3 months, 27/30 (90%) became pregnant, compared with 29/30 (97%, p>.05). The litter size (mean±SD) did not differ between groups (10.9±1.5 3-DRUID, 11.2±1.1 control, p>.05). In the second experiment, five rats had a 10.0-mm 3-DRUID (which was one third the length of one uterine horn) inserted into the bilateral uterine horns, and three of the five rats became pregnant. All 20 rats were pregnant 1 month after the insertion of the 2-DIUD. Thus, the contraceptive rate for the 2-DIUD group was 0. CONCLUSIONS: The primary contraceptive mechanism effect of the new 3-DRIUD in rodents appears to be a result of occupying physical space in the uterus.

Asunto(s)

Dispositivos Intrauterinos , Aleaciones , Animales , Fenómenos Químicos , Femenino , Infertilidad Femenina/prevención & control , Expulsión de Dispositivo Intrauterino , Dispositivos Intrauterinos/efectos adversos , Tamaño de la Camada , Ensayo de Materiales , Níquel , Embarazo , Ratas , Ratas Wistar , Elastómeros de Silicona , Titanio , Perforación Uterina/prevención & control

RESUMEN

The aim of this study was to explore sperm chromosomal aneuploidy and DNA integrity in infertile patients with spinal cord injury (SCI). Semen samples were collected from 12 infertile men with SCI by percutaneous vasal sperm aspiration (PVSA) and from 14 male SCI patients by penile vibratory stimulation (PVS). These semen samples as well as samples from 16 donors were analyzed using the hypo-osmotic swelling (HOS) test, the sperm chromatin dispersion test, terminal deoxynucleotidyl transferase-mediated terminal uridine nick-end labeling assay, and multicolor fluorescence in situ hybridization with probes specific for the chromosomes 13, 18, 21, X, and Y. There were significant differences in the percentages of motile sperm, normal morphologic sperm, normal HOS/eosin staining, and sperm DNA fragmentation between the infertile men with SCI and the control group (P < .05 and P < .01). The sperm forward motility was significantly greater in the PVSA group than in the PVS group (P < .01). The number of round cells per milliliter of semen obtained from the 14 SCI patients by PVS was between 1 million and 12 million. The rate of sperm DNA fragmentation, as identified by the sperm chromatin dispersion test, was higher in the PVS group than in the PVSA group (P < .05). The aneuploidy rates for the SCI patients were 1.5- to 1.6-fold higher for chromosomes 13, 18, and 21, and were 2.3- to 2.4-fold higher for chromosomes X and Y than for patients in the control group (P < .001). These results suggest that for men with SCI, the semen quality is poorer, the prevalence of abnormal HOS/eosin staining is greater, and sperm DNA fragmentation and sperm chromosomal aneuploidies are seen at a higher rate compared with healthy, fertile, and normospermic men.

Asunto(s)

Infertilidad Masculina/etiología , Pene/inervación , Análisis de Semen , Recuperación de la Esperma , Espermatozoides/patología , Traumatismos de la Médula Espinal/complicaciones , Adulto , Aneuploidia , Estudios de Casos y Controles , Forma de la Célula , Distribución de Chi-Cuadrado , Cromosomas Humanos Par 13 , Cromosomas Humanos Par 18 , Cromosomas Humanos Par 21 , Cromosomas Humanos X , Cromosomas Humanos Y , Fragmentación del ADN , Humanos , Hibridación Fluorescente in Situ , Etiquetado Corte-Fin in Situ , Infertilidad Masculina/genética , Infertilidad Masculina/patología , Infertilidad Masculina/fisiopatología , Masculino , Motilidad Espermática , Traumatismos de la Médula Espinal/genética , Traumatismos de la Médula Espinal/patología , Traumatismos de la Médula Espinal/fisiopatología , Succión , Vibración

RESUMEN

PURPOSE: To explore sperm chromosomal aneuploidy, sperm membrane and DNA integrity in infertile patients with anejaculation. METHODS: Semen samples were collected from 18 infertile men with spinal cord injury (SCI) by penile vibratory stimulation (PVS) and from 14 psychogenic anejaculation (PA) patients by percutaneous vasal sperm aspiration (PVSA). These semen samples as well as samples from 16 donors were analyzed using the hypo-osmotic swelling (HOS) test, the sperm chromatin dispersion (SCD) test and multi-color fluorescence in situ hybridization (FISH) with probes specific for chromosomes 13, 18, 21, X and Y. RESULTS: There were significant differences in the percentages of motile sperm, normal morphologic sperm and sperm DNA fragmentation between the infertile men with SCI and the control group (P < 0.05 and P < 0.01). The sperm motility was significantly greater in the PA-PVSA group than in the SCI-PVS group (P < 0.01). The number of round cells per mL of semen obtained from the 18 SCI patients by PVS was between 1 and 8 million. The rate of sperm DNA fragmentation in the SCI-PVS group was higher than that of the PA-PVSA group (P < 0.05). The aneuploidy rates for the SCI patients were 2.4-fold higher for chromosomes 13, 18 and 21 and 2.2-fold higher for chromosomes X and Y than for patients in the control group (P < 0.0001). CONCLUSIONS: The semen quality is poorer, sperm DNA fragmentation and sperm chromosomal aneuploidies are seen at a higher rate for SCI patients compared to healthy, fertile and normospermic men. Whether the difference in yield is due to increased scrotal temperature, genitourinary infection, or other reasons requires further study.

Asunto(s)

Aneuploidia , Infertilidad Masculina/genética , Motilidad Espermática , Espermatozoides/citología , Cromosomas Humanos/genética , Fragmentación del ADN , Humanos , Hibridación Fluorescente in Situ , Infertilidad Masculina/etiología , Masculino , Traumatismos de la Médula Espinal/complicaciones

RESUMEN

OBJECTIVE: To explore the mechanism of spermicidal effect of crude extract and platycodin-D from Platycodon grandiflorum (PG) root in vitro. METHODS: Between February 2006 and December 2009, 38 fertile and healthy adult males were selected as donors. PG root was extracted and platycodin-D purified. Grouping was as follows: crude extract from PG root, platycodin-D, nonoxynol-9 (N-9, as a reference standard) and semen-added physiological saline (as control). Spermicidal experiments were carried out in vitro (Sander-Cramer test). The hypo-osmotic swelling (HOS) test and modified Eosin-Giemsa (EG) staining were used to detect the integrity of sperm membrane. Four types of sperm morphology were divided through HOS-EG test: Type A: spermatozoa with swelling in tails and head white staining HOS(+)-EG(-) (membrane intact); Type B: spermatozoa with no swelling in tails (membrane-damaged) and head white staining HOS(-)-EG(-); Type C: spermatozoa with tail swelling and head red HOS(+)-EG(+); Type D: spermatozoa with no swelling in tails and head red HOS(-)-EG(+). Sperm chromatin dispersion (SCD) test was performed to determine the integrity of sperm DNA. RESULTS: The crude extract from PG root could immobilize and kill 100% spermatozoa within 20 s in vitro at the concentrations of 50.0 g/L and 20.0 g/L (v:v = 1:1 in semen). When the semen sample was exposed to the concentrations of 2.0 g/L and 1.0 g/L of platycodin-D, all spermatozoa were immobilized within 20 s. In the control group, the mean percentage of Types A, B, C and D was (69.0 ± 8.3)%, (3.4 ± 0.5)%, (10.2 ± 1.7)% and (17.4 ± 2.1)% respectively. In the groups of platycodin-D and N-9 solution, the rate of Types A and B was 0. The rate of Types C [(65.3 ± 3.8)%] and D [(34.7 ± 7.1)%] significantly increased versus control in the platycodin-D group (P < 0.01). Sperm DNA fragmentation had no change upon an exposure to the extract from PG root, platycodin-D and N-9 solution. And the sperm revival test showed none of the spermatozoa recovered their motility. CONCLUSION: The extract and platycodin-D from PG root have a quick sperm-killing effect in a short time in vitro by disrupting the integrity of sperm membrane (main head).

Asunto(s)

Extractos Vegetales/farmacología , Platycodon/química , Saponinas/farmacología , Espermicidas/farmacología , Espermatozoides/efectos de los fármacos , Triterpenos/farmacología , Adulto , Membrana Celular/efectos de los fármacos , Humanos , Masculino

RESUMEN

OBJECTIVE: To compare the effects of sperm chromatin dispersion (SCD) test and TdT-mediated dUTP nick end labeling (TUNEL) assay in assessing the DNA fragmentation in human sperm. METHODS: Motile sperms were isolated from the semen samples obtained from 20 healthy fertile men and 32 clinically infertile patients by swim-up technique, and underwent SCD and TUNEL to analyze the DNA fragmentation. RESULTS: The rate of sperm with DNA damage of the infertile patients was 12.8% +/- 5.8% tested by SCD, significantly higher than that of the healthy fertile men (7.6% +/- 3.3%, t = 3.576, P = 0.001), and the rate of sperm with DNA damage of the infertile patients was 11.1% +/- 5.1% tested by TUNEL assay, significantly higher than that of the healthy fertile men (6.8% +/- 2.8%, t = 3.467, P = 0.001). The proportion of sperm cell with abnormal DNA integrity measured by SCD test was correlated strongly with that determined by TUNEL for the infertile men (r = 0.841, P = 0.000) and for the fertile men too (r = 0.823, P = 0.000). The rate of sperm with DNA damage measured by SCD were not significantly different from those of TUNEL-positive sperm in fertile men (t = 1.996, P = 0.060). The rate of sperm with DNA damage measured by SCD was significantly higher than that measured by TUNEL among infertile patients (t = 3.023, P = 0.005). CONCLUSION: The presence of sperm DNA damage may lead to male infertility. SCD is simpler, cheaper and more reliable than TUNEL in testing the sperm DNA damage.

Asunto(s)

Daño del ADN , ADN/genética , Infertilidad Masculina/diagnóstico , Infertilidad Masculina/genética , Espermatozoides/química , Adulto , Estudios de Casos y Controles , Fragmentación del ADN , Humanos , Infertilidad Masculina/metabolismo , Masculino , Motilidad Espermática

RESUMEN

A series of novel 4-(4-(5-methyl-3-arylisoxazol-4-yl)thiazol-2-yl)piperidyl carboxamides and thiocarboxamides were synthesized as potential lead compounds of inhibitors targeting D1 protease in plants. These compounds were designed on the basis of a D1 protease inhibitor hit structure identified by homology modeling and virtual screening. The syntheses of these compounds were accomplished via a four-step procedure including the isoxazole ring formation, alpha-bromination of acetyl group, thiazole ring formation, and carboxamide/thiocarboxamide attachment. The in vivo herbicidal activity tests show that most compounds possess moderate to good herbicidal activities. The enzyme activity of one compound against the native spinach D1 protease exhibits a competitive inhibition. The results suggest that these compounds are indeed potential inhibitors for targeting D1 protease in plants.

Asunto(s)

Herbicidas/síntesis química , Piperidinas/síntesis química , Proteínas de Plantas/antagonistas & inhibidores , Inhibidores de Proteasas/síntesis química , Unión Competitiva , Simulación por Computador , Herbicidas/farmacología , Isoxazoles , Modelos Moleculares , Piperidinas/farmacología , Inhibidores de Proteasas/farmacología , Spinacia oleracea/enzimología , Tiazoles

RESUMEN

In the title molecule, C(26)H(24)N(4)O(2)S, the dihedral angle between the isoxazole ring and the adjoining benzene ring is 21.4 (5)°, and between the isoxazole ring and the thia-zole ring is 14.3 (4)°. The piperidine ring is in a chair conformation. In the crystal structure, mol-ecules are linked by inter-molecular N-H⋯O and weak C-H⋯O hydrogen bonds into one-dimensional chains along [001].