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Lorenza Marinaccio Azzurra Stefanucci Giuseppe Scioli Alice Della Valle Gokhan Zengin Angelo Cichelli Adriano Mollica 《International journal of molecular sciences》2022,23(6)
Elastases are a broad group of enzymes involved in the lysis of elastin, the main component of elastic fibres. They are produced and released in the human body, mainly by neutrophils and the pancreas. The imbalance between elastase activity and its endogenous inhibitors can cause different illnesses due to their excessive activity. The main aim of this review is to provide an overview of the latest advancements on the identification, structures and mechanisms of action of peptide human neutrophil elastase inhibitors isolated from natural sources, such as plants, animals, fungi, bacteria and sponges. The discovery of new elastase inhibitors could have a great impact on the pharmaceutical development of novel drugs through the optimization of the natural lead compounds. Bacteria produce mainly cyclic peptides, while animals provide for long and linear amino acid sequences. Despite their diverse natural sources, these elastase inhibitors show remarkable IC50 values in a range from nM to μM values, thus representing an interesting starting point for the further development of potent bioactive compounds on human elastase enzymes. 相似文献
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Previous research on perceiving spatial layout has found that people often exhibit normative biases in their perception of the environment. For instance, slant is typically overestimated and distance is usually underestimated. Surprisingly, however, the perception of height has rarely been studied. The present experiments examined the perception of height when viewed from the top (e.g., looking down) or from the bottom (e.g., looking up). Multiple measures were adapted from previous studies of horizontal extents to assess the perception of height. Across all of the measures, a large, consistent bias was found: Vertical distances were greatly overestimated, especially from the top. Secondary findings suggest that the overestimation of distance and size that occurs when looking down from a high place correlates with reports of trait- and state-level fear of heights, suggesting that height overestimation may be due, in part, to fear. (PsycINFO Database Record (c) 2010 APA, all rights reserved) 相似文献
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Linkenauger Sally A.; Witt Jessica K.; Stefanucci Jeanine K.; Bakdash Jonathan Z.; Proffitt Dennis R. 《Canadian Metallurgical Quarterly》2009,35(6):1649
Previous research has suggested that perceived distances are scaled by the action capabilities of the body. The present studies showed that when “reachability” is constrained due to a difficult grasp required to pick up an object, perceived distance to the object increases. Participants estimated the distances to tools with handle orientations that made them either easy or difficult to grasp with their dominant and nondominant hands. Right-handed participants perceived tools that were more difficult to grasp to be farther away than tools that were easier to grasp. However, perceived distance did not differ in left-handed participants. These studies suggest that, when reaching toward a target, the distance to that target is scaled in terms of how far one can effectively reach, given the type of reaching posture that is executed. Furthermore, this effect is modulated by handedness. (PsycINFO Database Record (c) 2010 APA, all rights reserved) 相似文献
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Kouadio Ibrahime Sinan Ouattara Katinan Etienne Azzurra Stefanucci Adriano Mollica Mohamad Fawzi Mahomoodally Sharmeen Jugreet Gabriele Rocchetti Luigi Lucini Abdurrahman Aktumsek Domenico Montesano Gunes Ak Gokhan Zengin 《Flavour and Fragrance Journal》2021,36(1):148-158
Several studies demonstrated the wide pharmacological properties of extracts and essential oils (EOs) prepared from Euphorbia species. In the present study, the chemical composition and biological activities of EOs from three different Euphorbia species were evaluated using in vitro methods. A total of 29, 33 and 42 constituents were identified in the EOs of E hirta, E convolvuloides and E heterophylla, respectively. The EOs exhibited in vitro radical scavenging potential in the ABTS assay (2.89‐21.50 mg/g). Additionally, an inhibitory effect on acetylcholinesterase (4.23‐5.12 mg/g) was detected. Besides, remarkable tyrosinase inhibition was reported by the EOs (95.24‐113.74 mg/g). Molecular docking was also performed to elucidate the binding interactions between selected EO components and enzymes. Phytol and geranyl‐(E)‐acetone had a good binding with tyrosinase in the molecular docking. This study highlighted the promising pharmacological profiles of these EOs as natural sources of antioxidants as well as cholinesterase and tyrosinase inhibitors that could be further explored in the management of human ailments in food and pharmaceutical industries. 相似文献
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Teachman Bethany A.; Stefanucci Jeanine K.; Clerkin Elise M.; Cody Meghan W.; Proffitt Dennis R. 《Canadian Metallurgical Quarterly》2008,8(2):296
Emotion and psychopathology researchers have described the fear response as consisting of four main components--subjective affect, physiology, cognition, and behavior. The current study provides evidence for an additional component in the domain of height fear (perception) and shows that it is distinct from measures of cognitive processing. Individuals High (N = 35) and Low (N = 36) in acrophobic symptoms looked over a two-story balcony ledge and estimated its vertical extent using a direct height estimation task (visual matching), and an indirect task (size estimation); the latter task seems to exhibit little influence from cognitive factors. In addition, implicit and explicit measures of cognitive processing were obtained. Results indicated that, as expected, the High Fear group showed greater relative, implicit height fear associations and explicit threat cognitions. Of primary interest, the High (compared to Low) Fear group estimated the vertical extent to be higher, and judged target sizes to be greater, even when controlling for the cognitive bias measures. These results suggest that emotional factors such as fear are related to perception. (PsycINFO Database Record (c) 2010 APA, all rights reserved) 相似文献
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Traditionally, perception was considered to be an encapsulated process that was unaffected by top-down processes like affect. Recent work in vision draws this framework into question by showing that changes in the affective state of the perceiver can impact many different aspects of visual perception. Here, we extend the relationship between affect and perception into another perceptual modality: audition. Participants were induced into a negative or neutral mood by writing about a frightening or neutral experience in their past. They then listened to a series of short, neutral tones (320 and 640 ms) and rated the loudness and duration of the tones. Participants in a negative mood rated the tones as significantly louder, but not longer, than participants in a neutral mood, suggesting that the difference between the groups was perceptual rather than just a response bias. This research shows for the first time that the role of affect in perceptual processes may be more pervasive than previously considered. (PsycINFO Database Record (c) 2011 APA, all rights reserved) 相似文献
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In a series of experiments, it was found that emotional arousal can influence height perception. In Experiment 1, participants viewed either arousing or nonarousing images before estimating the height of a 2-story balcony and the size of a target on the ground below the balcony. People who viewed arousing images overestimated height and target size more than did those who viewed nonarousing images. However, in Experiment 2, estimates of horizontal distances were not influenced by emotional arousal. In Experiment 3, both valence and arousal cues were manipulated, and it was found that arousal, but not valence, moderated height perception. In Experiment 4, participants either up-regulated or down-regulated their emotional experience while viewing emotionally arousing images, and a control group simply viewed the arousing images. Those participants who up-regulated their emotional experience overestimated height more than did the control or down-regulated participants. In sum, emotional arousal influences estimates of height, and this influence can be moderated by emotion regulation strategies. (PsycINFO Database Record (c) 2010 APA, all rights reserved) 相似文献
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Stefanucci A Pinnen F Feliciani F Cacciatore I Lucente G Mollica A 《International journal of molecular sciences》2011,12(5):2853-2890
A successful design of peptidomimetics must come to terms with χ-space control. The incorporation of χ-space constrained amino acids into bioactive peptides renders the χ(1) and χ(2) torsional angles of pharmacophore amino acids critical for activity and selectivity as with other relevant structural features of the template. This review describes histidine analogues characterized by replacement of native α and/or β-hydrogen atoms with alkyl substituents as well as analogues with α, β-didehydro unsaturation or C(α)-C(β) cyclopropane insertion (ACC derivatives). Attention is also dedicated to the relevant field of β-aminoacid chemistry by describing the synthesis of β(2)- and β(3)-models (β-hHis). Structural modifications leading to cyclic imino derivatives such as spinacine, aza-histidine and analogues with shortening or elongation of the native side chain (nor-histidine and homo-histidine, respectively) are also described. Examples of the use of the described analogues to replace native histidine in bioactive peptides are also given. 相似文献
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