Enhanced physical performance, attention, and mood states after a nap opportunity following a sleep restriction night in female athletes: A randomized controlled trial

Article

Author: Ammar, Achraf ; BenSalem, Sahar ; Souissi, Nizar ; Boukhris, Omar ; Trabelsi, Khaled ; M Glenn, Jorden ; Chtourou, Hamdi ; Jahrami, Haithem ; Salem, Atef

This study examined the effects of two nap durations (40 minutes (N40) and 90 minutes (N90)) on physical performance, sleepiness, attention, mood states (Profile of Mood States, POMS), perceived exertion (RPE), pain perception (PP), recovery (PRS), and delayed onset muscle soreness (DOMS) in well-trained women. Fourteen female boxers underwent the digit cancellation test, POMS, and the 5-meter shuttle run test (5mSRT) under no-nap (N0), N40, and N90 conditions after either normal sleep (NSN) or sleep restriction (SRN). RPE and PP were assessed immediately post-5mSRT, while PRS and DOMS were recorded at 5 min and 24 h post-5mSRT. Total distance (TD) and higher distance (HD) were better in N40 and N90 after NSN compared to SRN (p < 0.05). Fatigue index (FI) was lower in N40 and N90 than in N0, and lower in N90 than N40 (p < 0.05). PRS improved and RPE, DOMS, and PP decreased significantly after N40 and N90 compared to N0, with N90 showing greater benefits (p < 0.05). Total POMS scores were better after N40 and N90 than N0, with N90 outperforming N40 (p < 0.05). Overall, N90 provided greater benefits than N40 in enhancing physical performance, attention, recovery, and mood, while reducing exertion, pain, and soreness after both NSN and SRN.

01 May 2024·Bioorganic & Medicinal Chemistry

Discovery of novel pyridone-benzamide derivatives possessing a 1-methyl-2-benzimidazolinone moiety as potent EZH2 inhibitors for the treatment of B-cell lymphomas

Article

Author: Wu, Di ; Gong, Ping ; Zeng, Xiaoyi ; Zhao, Yuanhao ; Qin, Mingze

Enhancer of zeste homolog 2 (EZH2) is a promising therapeutic target for diffuse large B-cell lymphoma. In this study, based on the binding model of 1 (tazemetostat) with polycomb repressive complex 2 (PRC2), we designed and synthesized a series of tazemetostat analogs bearing a 1-methyl-2-benzimidazolinone moiety to improve the inhibitory activity of EZH2 wild-type (WT) and Y641 mutants and enhance metabolic stability. After the assessment of the structure-activity relationship at enzymatic and cellular levels, compound N40 was identified. Biochemical assays showed that compound N40 (IC₅₀ = 0.32 nM) exhibited superior inhibitory activity against EZH2 WT, compared with 1 (IC₅₀ = 1.20 nM), and high potency against EZH2 Y641 mutants (EZH2 Y641F, IC₅₀ = 0.03 nM; EZH2 Y641N, IC₅₀ = 0.08 nM), which were approximately 10-fold more active than those of 1 (EZH2 Y641F, IC₅₀ = 0.37 nM; EZH2 Y641N, IC₅₀ = 0.85 nM). Furthermore, compound N40 (IC₅₀ = 3.52 ± 1.23 nM) effectively inhibited the proliferation of Karpas-422 cells and was more potent than 1 (IC₅₀ = 35.01 ± 1.28 nM). Further cellular experiments showed that N40 arrested Karpas-422 cells in the G1 phase and induced apoptosis in a dose-dependent manner. Moreover, N40 inhibited the trimethylation of lysine 27 on histone H3 (H3K27Me3) in Karpas-422 cells bearing the EZH2 Y641N mutant. Additionally, N40 (T_1/2 = 177.69 min) showed improved metabolic stability in human liver microsomes compared with 1 (T_1/2 = 7.97 min). Our findings suggest N40 as a promising EZH2 inhibitor; further investigation remains warranted to confirm our findings and further develop N40.

04 Apr 2022·Evidence-Based Complementary and Alternative MedicineQ4 · MEDICINE

Naringenin Improves Ovalbumin-Induced Allergic Asthma in Rats through Antioxidant and Anti-Inflammatory Effects

Q4 · MEDICINE

ArticleOA

Author: Fakhri, Sajad ; Jasemi, Seyed Vahid ; Khazaei, Hosna ; Mohammadi-Noori, Ehsan ; Farzaei, Mohammad Hosein

Asthma is a chronic disease with eosinophilic inflammation and oxidative damages leading to airway obstruction. Naringenin is a phytochemical possessing strong antioxidant and anti-inflammatory activities against chronic destructive conditions. The current study is devoted to evaluating naringenin’s effects on the attenuation of inflammation and oxidative stress in lung tissue in a rat model of ovalbumin-induced asthma. Male Wistar rats were allocated to five groups of six: normal control (NC, receiving 1 ml/day of normal saline, orally), asthmatic (AS, receiving ovalbumin (1 mg/mL), and alum (1 mg/mL in saline) on days 0 and 14. Then, on days 21, 22, and 23, they were sensitized with the inhalation of ovalbumin), AS treated with dexamethasone (AS, 1 mg/kg/day, orally) [AS + D1], AS treated with naringenin (20 mg/kg/day, orally) [AS + N20], and AS treated with naringenin (40 mg/kg/day, orally) [AS + N40]. All the groups received associated drugs/agents for 28 days. Finally, bronchoalveolar lavage fluid (BALF) and lung tissue samples were taken off from the animals. The eosinophil count in BALF and malondialdehyde (MDA), glutathione (GSH), interleukin-13 and -4 (IL-13 and IL-4) levels were measured. Besides, the expression of urocortin (UCN) and surfactant protein-D (SP-D) were evaluated in the lung tissue using immunohistochemistry (IHC) and western blotting methods, respectively. Hematoxylin and eosin (H&E) staining were utilized to conduct histopathological analysis. Naringenin treatment significantly reduced MDA, remarkably increased GSH, and meaningfully reduced IL-4 and IL-13 levels in lung tissue. The count of eosinophils in the BALF of AS + N20 and AS + N40 was significantly reduced in comparison with the AS group. The UCN and SP-D protein levels were significantly decreased in the AS + N20 and AS + N40 groups compared to the AS group, using the IHC and western blot methods, respectively. Histopathological analysis data also confirm the results. Naringenin improves the symptoms of allergic asthma through antioxidant and anti-inflammatory effects.

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Indication	Highest Phase	Country/Location	Organization	Date
Diffuse Large B-Cell Lymphoma	Preclinical	China	Shenyang Pharmaceutical University	14 Apr 2024

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