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1.
Org Lett ; 2021 Apr 12.
Artigo em Inglês | MEDLINE | ID: mdl-33844550

RESUMO

N-Heterocyclic carbene-catalyzed asymmetric construction of cyclopentenones using enals and α-diketones is achieved, furnishing a series of highly functionalized cyclopentenones in a highly diastereo- and enantioselective manner. The protocol tolerates substrates with both aromatic and aliphatic groups, and further transformations of the products delivered a range of value-added molecules.

2.
Ophthalmol Glaucoma ; 2021 Apr 05.
Artigo em Inglês | MEDLINE | ID: mdl-33831643

RESUMO

OBJECTIVE: Understanding trends and patterns in the use of minimally invasive glaucoma surgery (MIGS) and patient profiles undergoing each procedure is important given their relative expense and unknown long-term safety and effectiveness. DESIGN: Retrospective analysis SUBJECTS: MIGS and standard glaucoma surgeries recorded in the American Academy of Ophthalmology (AAO) Intelligent Research in Sight (IRIS®) Registry. METHODS: We used the data from IRIS® Registry between 2013-2018 (inclusive) to measure annual number of MIGS and standard surgical techniques (trabeculectomy or glaucoma drainage device (GDD)) performed in the US, stratified by demographic characteristics. Secondary analyses of concurrent surgeries and of subsequent surgeries for MIGS and standard surgical technique were also conducted. MAIN OUTCOME MEASURES: Trends and sociodemographic characteristics of MIGS usage in the US. RESULTS: 203,332 eyes and 232,537 unique procedures had associated, documented International Statistical Classification of Diseases and Related Health Problems (ICD) 9/10 codes for glaucoma and were included in final analyses. Among eyes with documented glaucoma diagnoses, there was a substantial increase in annual MIGS procedures over the study period (from 7,586 in 2013 to 39,677), and a smaller decrease in standard glaucoma procedures (from 16,215 to 13,701). The proportion of iStent procedures almost tripled during the study period (from 14% to 40%), and by 2017 accounted for almost half (43.7%) of all glaucoma surgeries in the US. 21,025 (10.3%) of all eyes received multiple procedures; 7,638 (36.3%) on the same day and 13,387 (63.7%) on subsequent days. ECP and iStent were the most common concurrent procedures (55.4% of all concurrent procedures). Trabeculectomy and GDD were most commonly followed by another standard glaucoma surgery, but when followed by sequential MIGS, ECP and goniotomy were the most common procedures performed (33.0%, 21.9%, respectively). CONCLUSIONS: There was a significant increase in MIGS use over the recent six-year period despite limited evidence of their long-term safety or effectiveness, highlighting the need for trials comparing safety and outcomes of novel MIGS vs traditional surgical treatments for glaucoma.

3.
Plant Dis ; 2021 Apr 14.
Artigo em Inglês | MEDLINE | ID: mdl-33851863

RESUMO

Bletilla striata (Thunb.) Rchb. f. (Orchidaceae), a perennial plant, is a traditional Chinese herb (known as baiji) used to treat hemorrhage, scalding injuries, gastric ulcers, pulmonary diseases, and inflammation (Zu et al. 2019). In May 2019, foliar blight symptoms were observed on approximately 25% of B. striata (cv. Guiji No.1) plants in three plantations (∼4.5 hectares in total) in Ziyuan County, Guangxi Province, China. Initial symptoms were light brown, irregular, water-soaked spots on the plant leaves. Several spots often merged, forming large, irregular, lesions that extended onto the stem after a week and led to leaf abscission, and even plant death. To determine the causal agent, 5-mm squares cut from the margin of 6 infected leaves were surface disinfected in 1% sodium hypochlorite solution for 2 min, rinsed three times with sterile distilled water, plated on potato dextrose agar (PDA), and incubated at 28°C (12-h light-dark cycle) for 3 days. The emerging hyphal tip of a single mycelium was transferred to PDA to obtain pure cultures of the isolates. Twenty isolates were obtained, and 10 isolates (50%) were initially white before turning light brown (∼4 days). Septate hyphae were 4.29 to 10.75 µm (average 6.42 µm) in diameter and branched at right angles with a constriction at the origin of the branch point. Staining with 1% safranin O and 3% KOH solution (Bandoni 1979) revealed multinucleated cells (3 to 9 nuclei per cell, n = 142). This morphology was typical of Rhizoctonia solani Kühn (Meyer et al. 1990). For species confirmation by molecular identification, three isolates (BJ101.6, BJ101.11, and BJ102.2) were cultured on PDA for 4 days, then DNA was extracted from the mycelium using the CTAB method (Guo et al. 2000), and the ribosomal ITS1-5.8S-ITS2 region was amplified by PCR using the universal fungal primers ITS1 and ITS4 (White et al. 1990). Internal transcribed spacer (ITS) sequences of strains BJ101.6, BJ101.11, and BJ102 (deposited in GenBank under accession nos MT406271, MT892815, and MT892814, respectively) had over 99% similarity with those of R. solani AG-2-2 IIIB in GenBank (accession nos JX913810 and AB054858) (Carling et al. 2002; Hong et al. 2012). Phylogenetic analysis using ITS sequences showed that the isolates clustered monophyletically with strains of R. solani AG-2-2 IIIB. The AG of the isolates was confirmed by their ability to grow well on PDA at 35°C, which separates AG-2-2 IIIB from AG-2-2 IV (Inokuti et al. 2019). Based on morphological characteristics and nucleotide sequence analysis, the isolates were identified as R. solani AG-2-2 IIIB. Pathogenicity was tested using 1.5-year-old B. striata (cv. Guiji No.1) plants grown in a perlite and peat moss mixture (1:3) in 7-cm pots. Healthy leaves on plants were inoculated with an aqueous suspension (approximately 1 × 105 hyphal fragments/mL, 100 µL) prepared from cultures of strains BJ101.6, BJ101.11, and BJ102.2, each isolate was inoculated onto three plants; three other plants with sterile water served as controls. All plants were enclosed in transparent plastic bags and incubated in a greenhouse at 28°C for 14 days (12-h photoperiod). Three days post-inoculation, leaves exposed to the mycelial fragments had symptoms similar to those originally observed in the field. No symptoms were detected on control plants. Experiments were replicated three times with similar results. To fulfill Koch's postulates, R. solani AG-2-2 IIIB was re-isolated on PDA from symptomatic leaves and confirmed by sequencing, whereas no fungus was isolated from the control plants. To our knowledge, this is the first report of R. solani AG-2-2 IIIB causing foliar blight on B. striata in China, and these findings will be useful for further control strategies and research.

4.
Artigo em Inglês | MEDLINE | ID: mdl-33852177

RESUMO

Electrocatalytic reduction of carbon dioxide (CO2) into value-added products (e.g., ethylene) is a promising approach for greenhouse gas mitigation, but many details of electrocatalytic CO2 reduction reactions (CO2RR) remain elusive. Raman spectroscopy is suitable for in situ characterization of CO2RR mechanisms, but the low signal intensity and resulting poor time resolution (often up to minutes) hampers the application of conventional Raman spectroscopy for the study of the dynamic CO2 reduction reaction, which requires sub-second time resolution. By using Time-Resolved Surface Enhanced Raman Spectroscopy (TR-SERS) we were able to successfully monitor CO2RR over Cu surfaces with sub-second time resolution. Anodic treatment at 1.55 V vs. the reversible hydrogen electrode (RHE) and subsequent surface oxide reduction (below -0.4 V vs. RHE) induced roughening of the Cu electrode surface, which resulted in hot-spots for TR-SERS, enhanced time resolution (down to ~ 0.7 s) and improved CO2RR efficiency (i.e., four-fold increase in ethylene faradaic efficiency). With TR-SERS, the initial formation of hot-spots for SERS and CO2RR was followed (<7 s), after which a stable copper surface surrounded by increased local alkalinity was formed. Our measurements revealed that a highly dynamic CO intermediate, with a characteristic vibration below 2060 cm-1, is related to C-C coupling and ethylene production (-0.9 V vs. RHE), whereas lower cathodic bias (-0.7 V vs. RHE) resulted in gaseous CO production from isolated and static CO surface species with a distinct vibration at 2092 cm-1. Our results provide valuable time-resolved insights into the dynamic nature of the electrode surface and adsorbed intermediates during CO2 electrochemical reduction on copper and showcase the potential of TR-SERS in copper-based electrocatalysis to follow reaction dynamics.

5.
Org Lett ; 2021 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-33793241

RESUMO

The geminal difluorocyclobutane core is a valuable structural element in medicinal chemistry. Strategies for gem-difluorocyclobutanes, especially the 2-substituted cases, are limiting and often suffer from harsh reaction conditions. Reported herein is a migratory gem-difluorination of aryl-substituted methylenecycloproanes (MCPs) for the synthesis of 2-arylsubstituted gem-difluorocyclobutanes. Commercially available Selectfluor (F-TEDA-BF4) and Py·HF were used as the fluorine sources. The protocol proceeds via a Wagner-Meerwein rearrangement with mild reaction conditions, good functional group tolerance, and moderate to good yields. The product could be readily transformed to gem-difluorocyclobutane-containing carboxylic acid, amine, and alcohol, all of which are useful building blocks for biologically active molecule synthesis.

6.
J Org Chem ; 2021 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-33787277

RESUMO

Application of a hypervalent fluoroiodane for the regiodivergent synthesis of dihydroxazines and fluorinated oxazepanes from allylaminoethanol was investigated. The reaction was carried out under mild conditions and gave the products in moderate to good yields. The selectivity of this transformation is controlled by the substituents of the allylaminoethanol.

7.
Biosci Rep ; 41(4)2021 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-33739370

RESUMO

BACKGROUND: Coronary artery disease (CAD) is a chronic inflammatory disease caused by development of atherosclerosis (AS), which is the leading cause of mortality and disability. Our study aimed to identify the differentially expressed genes (DEGs) in CD14+ monocytes from CAD patients compared with those from non-CAD controls, which might pave the way to diagnosis and treatment for CAD. METHODS: The RNA-sequencing (RNA-seq) was performed by BGISEQ-500, followed by analyzing with R package to screening DEGs. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analyses were performed by R package. In addition, we validated the results of RNA-seq using real-time quantitative polymerase chain reaction (RT-qPCR). Furthermore, we explored the function of selected ten genes in LDL-treated CD14+ monocytes by RT-qPCR. RESULTS: a total of 2897 DEGs were identified, including 753 up- and 2144 down-regulated genes in CD14+ monocytes from CAD patients. These DEGs were mainly enriched in plasma membrane and cell periphery of cell component, immune system process of biological process, NF-κB signaling pathway, cell adhesion molecules signaling pathway and cytokine-cytokine receptor interaction signaling pathway. In LDL-treated CD14+ monocytes, the mRNA expression of pyruvate dehydrogenase kinase 4 (PDK4) was significantly up-regulated. CONCLUSION: In the present study, we suggested that PDK4 might play a role in progression of CAD. The study will provide some pieces of evidence to investigate the role and mechanism of key genes in the pathogenesis of CAD.

8.
Clin Gerontol ; : 1-14, 2021 Mar 27.
Artigo em Inglês | MEDLINE | ID: mdl-33775222

RESUMO

OBJECTIVES: This study examined the mediating effect of life satisfaction and the moderating effect of the availability of community recreational facilities (CRF) in the association between loneliness and depression in rural older adults and urban older adults, respectively. METHODS: Quantitative data collected from 7547 Chinese older adults were analyzed using the SPSS macro PROCESS to test a moderated mediation model with life satisfaction as the mediator and CRF availability and residency type (rural vs. urban) as moderators. RESULTS: Loneliness negatively predicted life satisfaction, life satisfaction negatively predicted depression, and loneliness positively predicted depression. The interaction of loneliness and CRF availability had a significant effect on depression for urban older adults but not for rural older adults. The direct impact of loneliness on depression differed significantly between rural and urban older adults. CONCLUSIONS: Life satisfaction mediated the association between loneliness and depression in both rural and urban older adults; CRF availability unexpectedly boosted the effect of loneliness on depression in urban older adults but not in rural older adults. Given the same level of loneliness, urban older adults were more likely to be depressed than rural older adults. CLINICAL IMPLICATIONS: Psychogeriatric practitioners may embed life satisfaction into intervention programs to minimize depression among older adults. Public administrators should examine the utilization of public facilities to avoid wasted resources and counterproductive effects on older adults. Lonely urban older adults deserve special attention.

9.
PLoS One ; 16(3): e0245677, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33725016

RESUMO

Musk is a secretion of the forest musk deer (Moschus berezovskii). Normal musk is a brown solid secretion with a light fragrance. In this study, abnormal types of musk, namely, white and black musks, were discovered during the musk collection process. Researchers have long been concerned with the components of musk. Herein, GC-MS, headspace solid-phase microextraction (HS-SPME), and nonmetric multidimensional scaling (NMDS) were used to analyze the nonpolar organic components, volatile organic components, and sample similarities among different musks, respectively. Abundant steroid hormones and proteins were also found in the musk. The steroid hormone concentrations were detected using a radioimmunoassay (RIA). Proteins in the samples were hydrolyzed and the amino acids concentrations were detected. The steroid hormone and amino acid concentrations in white musk were significantly lower than in normal and black musks (p<0.05). The components were subjected to NMDS analysis to understand the differences in components among different types of musk, with the results suggesting that white musk was different from normal and black musks.

10.
J Org Chem ; 2021 Mar 10.
Artigo em Inglês | MEDLINE | ID: mdl-33719444

RESUMO

The mechanism of N-heterocyclic carbene-catalyzed umpolung of ß,γ-unsaturated α-diketone was studied using both density functional theory (DFT) calculations and experimental methods. In contrast to the originally proposed mechanism, the calculations revealed a more complicated process involving both nucleophilic O-acylated homoenolate and electrophilic α,ß-unsaturated acyl azolium intermediates. The experimental studies confirmed the existence of the aforementioned two key intermediates. A revised mechanism has been proposed to demonstrate the detailed mechanistic insights into the product formation.

11.
World J Gastroenterol ; 27(11): 1055-1063, 2021 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-33776372

RESUMO

BACKGROUND: Constipation is one of the most important nonmotor symptoms in Parkinson's disease (PD) patients, and constipation of different severities is closely related to the pathogenesis of PD. PD with constipation (PDC) is considered a unique type of constipation, but its mechanism of formation and factors affecting its severity have been less reported. Understanding the gastrointestinal motility characteristics and constipation classification of PDC patients is essential to guide the treatment of PDC. In this study, the colonic transit test and high-resolution anorectal manometry were used to identify the intestinal motility of PDC to provide a basis for the treatment of PDC. AIM: To investigate the clinical classification of PDC, to clarify its characteristics of colonic motility and rectal anal canal pressure, and to provide a basis for further research on the pathogenesis of PDC. METHODS: Twenty PDC patients and 20 patients with functional constipation (FC) who were treated at Xuanwu Hospital of Capital Medical University from August 6, 2018 to December 2, 2019 were included. A colonic transit test and high-resolution anorectal manometry were performed to compare the differences in colonic transit time, rectal anal canal pressure, and constipation classification between the two groups. RESULTS: There were no statistically significant differences in sex, age, body mass index, or duration of constipation between the two groups. It was found that more patients in the PDC group exhibited difficulty in defecating than in the FC group, and the difference was statistically significant. The rectal resting pressure, anal sphincter resting pressure, intrarectal pressure, and anal relaxation rate in the PDC group were significantly lower than those in the FC group. The proportion of paradoxical contractions in the PDC group was significantly higher than that in the FC group. There was a statistically significant difference in the type composition ratio of defecatory disorders between the two groups (P < 0.05). The left colonic transit time, rectosigmoid colonic transit time (RSCTT), and total colonic transit time were prolonged in PDC and FC patients compared to normal values. The patients with FC had a significantly longer right colonic transit time and a significantly shorter RSCTT than patients with PDC (P < 0.05). Mixed constipation predominated in PDC patients and FC patients, and no significant difference was observed. CONCLUSION: Patients with PDC and FC have severe functional dysmotility of the colon and rectum, but there are certain differences in segmental colonic transit time and rectal anal canal pressure between the two groups.

12.
Front Immunol ; 12: 625783, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33717139

RESUMO

Although cancers arise from genetic mutations enabling cells to proliferate uncontrollably, they cannot thrive without failure of the anticancer immunity due in a large part to the tumor environment's influence on effector and regulatory T cells. The field of immune checkpoint inhibitor (ICI) therapy for cancer was born out of the fact that tumor environments paralyze the immune cells that are supposed to clear them by activating the immune checkpoint molecules such as PD-1. While various subsets of effector T cells work collaboratively to eliminate cancers, Tregs enriched in the tumor environment can suppress not only the native anticancer immunity but also diminish the efficacy of ICI therapies. Because of their essential role in suppressing autoimmunity, various attempts to specifically deplete tumor-associated Tregs are currently underway to boost the efficacy of ICI therapies without causing systemic autoimmune responses. A better understanding the roles of Tregs in the anti-cancer immunity and ICI therapies should provide more specific targets to deplete intratumoral Tregs. Here, we review the current understanding on how Tregs inhibit the anti-cancer immunity and ICI therapies as well as the advances in the targeted depletion of intratumoral Tregs.

13.
Biomed Res Int ; 2021: 6666453, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33688501

RESUMO

Background: A prediction model can be developed to predict the risk of cancer-related cognitive impairment in colorectal cancer patients after chemotherapy. Methods: A regression analysis was performed on 386 colorectal cancer patients who had undergone chemotherapy. Three prediction models (random forest, logistic regression, and support vector machine models) were constructed using collected clinical and pathological data of the patients. Calibration and ROC curves and C-indexes were used to evaluate the selected models. A decision curve analysis (DCA) was used to determine the clinical utility of the line graph. Results: Three prediction models including a random forest, a logistic regression, and a support vector machine were constructed. The logistic regression model had the strongest predictive power with an area under the curve (AUC) of 0.799. Age, BMI, colostomy, complications, CRA, depression, diabetes, QLQ-C30 score, exercise, hypercholesterolemia, diet, marital status, education level, and pathological stage were included in the nomogram. The C-index (0.826) and calibration curve showed that the nomogram had good predictive ability and the DCA curves indicated that the model had strong clinical utility. Conclusions: A prediction model with good predictive ability and practical clinical value can be developed for predicting the risk of cognitive impairment in colorectal cancer after chemotherapy.

15.
J Neurosci Res ; 99(5): 1308-1324, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33634546

RESUMO

Neurodegenerative diseases (NDs) are incurable and can develop progressively debilitating disorders, including dementia and ataxias. Alzheimer's disease and Parkinson's disease are the most common NDs that mainly affect the elderly people. There is an urgent need to develop new diagnostic tools so that patients can be accurately stratified at an early stage. As a common post-translational modification, protein glycosylation plays a key role in physiological and pathological processes. The abnormal changes in glycosylation are associated with the altered biological pathways in NDs. The pathogenesis-related proteins, like amyloid-ß and microtubule-associated protein tau, have altered glycosylation. Importantly, specific glycosylation changes in cerebrospinal fluid, blood and urine are valuable for revealing neurodegeneration in the early stages. This review describes the emerging biomarkers based on glycoproteomics in NDs, highlighting the potential applications of glycoprotein biomarkers in the early detection of diseases, monitoring of the disease progression, and measurement of the therapeutic responses. The mass spectrometry-based strategies for characterizing glycoprotein biomarkers are also introduced.

17.
Org Lett ; 23(4): 1504-1509, 2021 Feb 19.
Artigo em Inglês | MEDLINE | ID: mdl-33534595

RESUMO

A unique deoxygenative cyclodimerization of alkynyl 1,2-diketones facilitated by Ti(OiPr)4 is achieved, affording a series of highly functionalized furan products. An unusual C-C bond and C═O bond cleavage of the substrates is observed, and Ti(OiPr)4 plays triplicate roles in the reaction. Furthermore, the products show uncommon fluorescent emission in the solid state, indicating the potential practical applications of this work.

18.
J Physiol Sci ; 71(1): 6, 2021 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-33546583

RESUMO

Our previous research has shown that galanin plays an antinociceptive effect via binding to galanin receptors (GalRs) in nucleus accumbens (NAc). This study focused on the involvement of GalR2 in galanin-induced antinociceptive effect in NAc of neuropathic pain rats. The chronic constriction injury of sciatic nerve (CCI) was used to mimic neuropathic pain model. The hind paw withdrawal latency (HWL) to thermal stimulation and hind paw withdrawal threshold (HWT) to mechanical stimulation were measured as the indicators of pain threshold. The results showed that 14 and 28 days after CCI, the expression of GalR2 was up-regulated in bilateral NAc of rats, and intra-NAc injection of GalR2 antagonist M871 reversed galanin-induced increases in HWL and HWT of CCI rats. Furthermore, intra-NAc injection of GalR2 agonist M1145 induced increases in HWL and HWT at day 14 and day 28 after CCI, which could also be reversed by M871. Finally, we found that M1145-induced antinociceptive effect in NAc of CCI rats was stronger than that in intact rats. These results imply that the GalR2 is activated in the NAc from day 14 to day 28 after CCI and GalR2 is involved in the galanin-induced antinociceptive effect in NAc of CCI rats.

19.
J Cell Physiol ; 2021 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-33554336

RESUMO

Breast cancer, a common malignancy for women, preferentially metastasizes to bone and obesity elevates the chance of its progression. While mechanical loading can suppress obesity and tumor-driven osteolysis, its effect on bone-metastasized obese mice has not been investigated. Here, we hypothesized that mechanical loading can lessen obesity-associated bone degradation in tumor-invaded bone by regulating the fate of bone marrow-derived cells. In this study, the effects of mechanical loading in obese mice were evaluated through X-ray imaging, histology, cytology, and molecular analyses. Tumor inoculation to the tibia elevated body fat composition, osteolytic lesions, and tibia destruction, and these pathologic changes were stimulated by the high-fat diet (HFD). However, mechanical loading markedly reduced these changes. It suppressed osteoclastogenesis by downregulating receptor activator of nuclear factor Kappa-B ligand and cathepsin K and promoted osteogenesis, which was associated with the upregulation of OPG and downregulation of C/enhancer-binding protein alpha and proliferator-activated receptor gamma for adipogenic differentiation. Furthermore, it decreased the levels of tumorigenic genes such as Rac1, MMP9, and interleukin 1ß. In summary, this study demonstrates that although a HFD aggravates bone metastases associated with breast cancer, mechanical loading significantly protected tumor-invaded bone by regulating the fate of bone marrow-derived cells. The current study suggests that mechanical loading can provide a noninvasive, palliative option for alleviating breast cancer-associated bone metastasis, in particular for obese patients.

20.
Invest New Drugs ; 2021 Jan 09.
Artigo em Inglês | MEDLINE | ID: mdl-33420642

RESUMO

Purpose To assess the pharmacokinetic (PK) effect of proton pump inhibitors on the novel poly(adenosine diphosphate-ribose) polymerase (PARP) inhibitor fluzoparib, and observe the safety of its co-administration with omeprazole. Patients and methods Sixteen male healthy volunteers (HVs) were enrolled in a single-center, single-arm, open-label, fixed-sequence study. HVs took fluzoparib (100 mg, p.o.) after meal consumption on day-1, took omeprazole 40 mg (p.o.) under a fasting condition from day-5 to day-9, and took fluzoparib (100 mg, p.o.) after meal consumption on day-9. Blood samples were collected at predetermined timepoints for PK analyses. Safety was assessed via clinical laboratory tests. The study was registered with the Clinical Trials Registry on 30 September 2019 (NCT04108676). Results The peak plasma concentrations (Cmax) after fluzoparib administration was 2395.17 ± 418.27 ng/mL, the area under the curve (AUC) within 72 h (AUC0 - 72 h) was 26669.09 ± 7320.12 h·ng/mL, and AUC0-∞ was 26897.44 ± 7573.61 h·ng/mL. The Cmax after co-administration of fluzoparib and omeprazole was 2489.43 ± 423.72 ng·mL, AUC0 - 72 h was 30300.49 ± 8350.08 h·ng/mL, and AUC0-∞ was 30678.74 ± 8595.55 h·ng/mL. The geometric mean ratio of Cmax, AUC0 - 72 h and AUC0-∞ was 104.0% (90%CI: 94.8-114.0%), 113.6% (104.2-123.9%) and 104.1% (104.5-124.6%). The number of HVs with adverse reactions was identical (eight) for administration of fluzoparib and co-administration of fluzoparib and omeprazole. Conclusions The proton pump inhibitor omeprazole did not have a significant influence on the PK behavior of fluzoparib, and its safety profile was good upon co-administration with omeprazole. (NCT04108676, 30 September 2019).

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