Globunoids A-D, undescribed bichalconoid and biflavanoids with α-glucosidase and α-amylase inhibitory activities from Knema globularia stems.

A bichalconoid, globunoid A (1) and three biflavanones, globunoids B-D (2-4), previously undescribed, were isolated from the stems of Knema globularia, along with fourteen known analogues 5-18. The chemical structures of 1-4 were elucidated by the comprehensive spectroscopic analysis including UV, IR, HRESIMS, and NMR; the absolute configurations were determined based on their NOESY data, DP4+ statistical analysis, and ECD calculation. Up to now, compounds 2 and 3 represent the first 3,3″-linked biflavanone structures. Among the isolated compounds, 2, 3, and 2,3-dihydrocalodenin B (6) potently inhibited α-glucosidase and α-amylase activities, with IC50 values in the range 1.1-7.5 µM. Furthermore, the most active compound 6 was found to be a non-competitive inhibitor against these two enzymes.

Identification and α-glucosidase inhibitory activity evaluation of two new coumarins derived from Mansonia gagei J. R. Drumm.

Five coumarins were isolated from the heartwood of Mansonia gagei, which included two newly discovered compounds, namely 11-hydroxypopulene E (1) and mansorin D (2), along with three previously identified compounds. The structures were determined through the utilisation of comprehensive spectroscopic data, ECD calculations, and a thorough comparison with existing literature data. The α-glucosidase inhibitory activities of all isolated compounds were assessed in yeast. Out of the compounds tested, compound 2 exhibited the most significant activity, displaying a percentage inhibition of 34.33% at a concentration of 200 µM.

External Focus Affects Drop Jump Performance: Focusing on Different Aims and Words of Instruction.

Attentional focus strategies eliciting external focus of attention effectively enhance drop jump (DJ) performance, however, their effects vary depending on the words used for the instructions. We aimed to examine the effects of different words on DJ performance using instructions eliciting external focus to minimize contact time (CT) or maximize jump height (JH). Twenty collegiate athletes performed DJs from a 30-cm platform after receiving one of the four instructions: two instructions (COND 1 and 2) about minimizing CT, and two instructions (COND 3 and 4) about maximizing JH. The reactive strength index (RSI), CT, JH, relative peak vertical ground reaction force (vGRF), and leg stiffness (kvert) were compared between conditions using repeated-measures analysis of variance. There was no significant main effect of conditions on the RSI, relative peak vGRF, and kvert (p > 0.05). CT was significantly shorter under CONDs 1 and 2 than COND 3 (p < 0.05); JH was significantly higher under COND 3 than CONDs 1 and 2 (p < 0.05), and under COND 4 than COND 1 (p < 0.05). When using attentional focus strategies in DJ, it is necessary to use different words and purposes according to the players' tasks.

α-Glucosidase inhibition of sesquiterpenoids from the heartwood of Mansonia gagei.

Nine undescribed sesquiterpenoids, along with ten known compounds, were isolated from the ethyl acetate extract of Mansonia gagei heartwood. Their structures were determined by spectroscopic data analysis (FTIR, 1D, 2D NMR, and HRESIMS), and their absolute configurations were established by ECD calculation. The isolated compounds were evaluated for their inhibitory effect against α-glucosidase from yeast. The results showed that mansonone U, mansonialactam, heliclactone and mansonone S exhibited exceptionally potent activities when compared to the positive control, acarbose, with IC50 values of 12.38 ± 0.71, 0.20 ± 0.05, 13.12 ± 2.85, and 12.05 ± 1.91 µM, respectively. Among them, mansonialactam possessed the most potent inhibitory activity against yeast α-glucosidase, and it showed an uncompetitive inhibition mode.

Age-related differences in kinetics during double- and single-leg jumps in boys.

BACKGROUND: Plyometric training, such as single-leg jumps, may be one of the most effective ways to improve a child's jumping and sprinting ability. However, few studies on age-related changes in single-legged jumping ability seem to exist. Therefore, the aim of this study was to examine age-related changes in double- and single-leg jump performance. METHODS: A total of 143 untrained boys aged 7-15 years performed double-leg counter-movement jump (CMJ) and rebound jump (RJ) and single-leg CMJ (SCMJ) and RJ (SRJ). Jump height (JH), peak vertical ground reaction force (PvGRF), and relative vertical ground reaction force (RvGRF) during CMJ and SCMJ, and RJ-Index, JH, ground contact time (CT), PvGRF, and RvGRF during RJ and SRJ were recorded, and one-way analysis of variance was used to examine differences between age group. RESULTS: JH, PvGRF, and RvGRF of CMJ and SCMJ increased with age with a similar trend (P<0.001). RJ-Index, JH, and PvGRF of RJ and SRJ also increased with age (P<0.001). CT of RJ did not change with age, but SRJ became longer with age (P<0.001). The RvGRF of RJ increased with age (P<0.001), but the RvGRF of SRJ did not change. CONCLUSIONS: These results suggest that age-related changes in CMJ among boys aged 7-15 years have similar trends for double- and single-leg jumps. However, age-related changes of RJ differed between double- and single-leg jumps, suggesting that differences in adaptation of relative force exertion may occur.

Effect of Neutral, Internal, and External Focus on Drop Jump Performance: Is Drop Jump Performance Affected by Plyometric Training Experience?

ABSTRACT: Furuhashi, Y, Hioki, Y, Yoshimoto, S, and Hayashi, R. The effect of neutral, internal, and external focus on drop jump performance: is drop jump performance affected by plyometric training experience? J Strength Cond XX(X): 000-000, 2021-Providing an external focus of attention through verbal instructions can improve the drop jump (DJ) performance, which differs based on the skill level of athletes. The purpose of this study was to assess the effect of change of focus of attention on the performance of DJs in experienced and inexperienced athletes. Thirty-eight male collegiate athletes divided into the experienced group (E group: age, 21.5 ± 1.4 years; height, 173.4 ± 5.7 cm; and body mass, 65.7 ± 6.2 kg) and the inexperienced group (I group: age, 21.9 ± 1.5 years; height, 172.8 ± 5.1 cm; and body mass, 68.7 ± 5.5 kg) performed 2 trials of DJs after listening to instructions designed to evoke a neutral, internal, or external focus of attention. Contact time (CT), jump height (JH), reactive strength index (RSI), and leg-spring stiffness (k vert ) were recorded during DJ and compared between the 2 groups using a repeated-measures analysis of variance. In the E group, the neutral condition was associated with a significantly higher RSI, JH, and k vert than the internal and external conditions ( p < 0.05). In the I group, the external condition was associated with significantly higher RSI and k vert and shorter CT than other conditions ( p < 0.05). Therefore, this suggests that attentional focus strategies need to be selected depending on DJ experience: A neutral focus may be preferable for athletes experienced in DJs, whereas an external focus may be more suitable for athletes with lesser DJ experience.

Garcinoic Acids and a Benzophenone Derivative from the Seeds of Garcinia kola and Their Antibacterial Activities against Oral Bacterial Pathogenic Organisms.

In this study, three new garcinoic acid dimers, δ,δ-bigarcinoic acid (1), δ,δ-bi-O-garcinoic acid (2), and γ,δ-bi-O-garcinoic acid (3), and a new benzophenone derivative, (8E)-4-geranyl-3,5-dihydroxybenzophenone (4), as well as seven known compounds (5-11) were isolated from the seeds of Garcinia kola. The structures of the new compounds were elucidated using MALDI-TOF-MS and spectroscopic data, including 1D and 2D NMR and electronic circular dichroism spectra. All of the isolated compounds were evaluated for their antimicrobial activity against two oral pathogens, Porphyromonas gingivalis and Streptococcus sobrinus. Among them, 4 and δ-garcinoic acid (6) exhibited antimicrobial activity against both of these microorganisms (MICs of 31.3-62.5 µM for P. gingivalis and 15.6-31.3 µM for S. sobrinus). These results indicate that some chemical constituents in G. kola seeds have potential application in the prevention of oral diseases.

Apolipoprotein E binds to and reduces serum levels of DNA-mimicking, pyrrolated proteins.

Lysine N-pyrrolation, converting lysine residues to Nϵ-pyrrole-l-lysine, is a recently discovered post-translational modification. This naturally occurring reaction confers electrochemical properties onto proteins that potentially produce an electrical mimic to DNA and result in specificity toward DNA-binding molecules such as anti-DNA autoantibodies. The discovery of this unique covalent protein modification provides a rationale for establishing the molecular mechanism and broad functional significance of the formation and regulation of Nϵ-pyrrole-l-lysine-containing proteins. In this study, we used microbeads coupled to pyrrolated or nonpyrrolated protein to screen for binding activities of human serum-resident nonimmunoglobin proteins to the pyrrolated proteins. This screen identified apolipoprotein E (apoE) as a protein that innately binds the DNA-mimicking proteins in serum. Using an array of biochemical assays, we observed that the pyrrolated proteins bind to the N-terminal domain of apoE and that oligomeric apoE binds these proteins better than does monomeric apoE. Employing surface plasmon resonance and confocal microscopy, we further observed that apoE deficiency leads to significant accumulation of pyrrolated serum albumin and is associated with an enhanced immune response. These results, along with the observation that apoE facilitates the binding of pyrrolated proteins to cells, suggest that apoE may contribute to the clearance of pyrrolated serum proteins. Our findings uncover apoE as a binding target of pyrrolated proteins, providing a key link connecting covalent protein modification, lipoprotein metabolism, and innate immunity.

Lysine pyrrolation is a naturally-occurring covalent modification involved in the production of DNA mimic proteins.

Covalent modification of proteins exerts significant effects on their chemical properties and has important functional and regulatory consequences. We now report the identification and verification of an electrically-active form of modified proteins recognized by a group of small molecules commonly used to interact with DNA. This previously unreported property of proteins was initially discovered when the γ-ketoaldehydes were identified as a source of the proteins stained by the DNA intercalators. Using 1,4-butanedial, the simplest γ-ketoaldehyde, we characterized the structural and chemical criteria governing the recognition of the modified proteins by the DNA intercalators and identified N(ε)-pyrrolelysine as a key adduct. Unexpectedly, the pyrrolation conferred an electronegativity and electronic properties on the proteins that potentially constitute an electrical mimic to the DNA. In addition, we found that the pyrrolated proteins indeed triggered an autoimmune response and that the production of specific antibodies against the pyrrolated proteins was accelerated in human systemic lupus erythematosus. These findings and the apparent high abundance of N(ε)-pyrrolelysine in vivo suggest that protein pyrrolation could be an endogenous source of DNA mimic proteins, providing a possible link connecting protein turnover and immune disorders.