Flat foot pain is a common complaint that requires therapeutic intervention. Currently, myofascial release techniques are often used in the therapy of musculoskeletal disorders. A group of 60 people ...suffering from flat feet with associated pain. Patients were assigned to four groups (15 people each): MF-myofascial release, E-the exercise program, MFE-myofascial release and the exercise program, C-no intervention. The rehabilitation program lasted 4 weeks. The NRS scale was used to examine pain intensity and FreeMed ground reaction force platform was used to examine selected static and dynamic foot indicators. Statistically significant pain reduction was obtained in all research. A static test of foot load distribution produced statistically significant changes only for selected indicators. In the dynamic test, statistically significant changes were observed for selected indicators, only in the groups subjected to therapeutic intervention. Most such changes were observed in the MF group. In the dynamic test which assessed the support phase of the foot, statistically significant changes were observed only for selected subphases. Most such changes were observed in the MFE group. Both exercise and exercise combined with myofascial release techniques, and especially myofascial release techniques alone, significantly reduce pain in a flat foot. This study shows a limited influence of both exercises and myofascial release techniques on selected static and dynamic indicators of a flat foot.
Introduction The foot is an important element of the human motor system. It is a single mechanism of propulsion and amortisation. Sports people, football players in particular, are especially prone ...to limb loading. In this discipline, the first contact with the sport as well as training begin at a very young age. In order to prevent traumas and injuries among young players, it is important to assess their foot arch. Material and methods A group of 30 players aged 13-18 who played football at the Progres Sports Academy in Cracow and at the lower- and upper-secondary schools in Cracow under the patronage of Marcin Gortat were tested. The tests involved the podoscopic evaluation of both feet, the test of both feet on a tensometric mat and a survey. To assess the longitudinal foot arch, Clarke’s angle was applied in the authors’ own tests. The transverse arch was evaluated using the Wejsflog index. Results For the overwhelming majority of the persons tested, the most common type of longitudinal arch was flat foot. Only a scant minority had a tendency towards hollow foot. The most common injuries among the examined footballers included muscle pulling and tearing as well as sprains and overloading. Most players suffered injuries of thigh muscles, knee joints, tarsal joints and feet. Conclusions It was confirmed that there was a significant correlation between the intensity of training and the frequency of injuries.
Currently, low back pain is a major health social and economic problem. The aim of this study was assessment of low back pain and habits of movement in individuals leading a sedentary lifestyle, due ...to the nature of their work. The study was conducted from November 2010 to February 2011. Research material consisted of two groups of people: 57 office workers (including 40 women and 17 men) and 43 bus drivers and taxi drivers (men only). In the first group age ranged from 21 to 60 years, and the second between 21 and 63 years. Research tool was the author’s own questionnaire consists of four parts. The first and second part contained questions about personal data and information about the job. In the third part respondents were asked about any pain in the lower spine, while in the fourth part we asked about movement of habits, knowledge of prevention and ways of spending free time. The results indicate frequent occurrence of low back pain among drivers (62,8%). This problem also often applies to people with high abnormal BMI (25 and above). More irregularities in posture appeared in the group of office workers than among drivers.
In order to find new hypotensive drugs possessing higher activity and better selectivity, a new series of fifteen 5,5-dimethylhydantoin derivatives (1–15) was designed. Three-step syntheses, ...consisting of N-alkylations using standard procedures as well as microwaves, were carried out. Crystal structures were determined for compounds 7–9. All of the synthesized 5,5-dimethylhydantoins were tested for their affinity to α1-adrenergic receptors (α1-AR) using both in vitro and in silico methods. Most of them displayed higher affinity (Ki < 127.9 nM) to α1-adrenoceptor than urapidil in radioligand binding assay. Docking to two subtypes of adrenergic receptors, α1A and α1B, was conducted. Selected compounds were tested for their activity towards two α1-AR subtypes. All of them showed intrinsic antagonistic activity. Moreover, for two compounds (1 and 5), which possess o-methoxyphenylpiperazine fragments, strong activity (IC50 < 100 nM) was observed. Some representatives (3 and 5), which contain alkyl linker, proved selectivity towards α1A-AR, while two compounds with 2-hydroxypropyl linker (11 and 13) to α1B-AR. Finally, hypotensive activity was examined in rats. The most active compound (5) proved not only a lower effective dose than urapidil but also a stronger effect than prazosin.
In the search for an effective strategy to overcome antimicrobial resistance, a series of new morpholine-containing 5-arylideneimidazolones differing within either the amine moiety or at position ...five of imidazolones was explored as potential antibiotic adjuvants against Gram-positive and Gram-negative bacteria. Compounds (
-
) were tested for oxacillin adjuvant properties in the Methicillin-susceptible
(MSSA) strain ATCC 25923 and Methicillin-resistant
MRSA 19449. Compounds
-
were tested additionally in combination with various antibiotics. Molecular modelling was performed to assess potential mechanism of action. Microdilution and real-time efflux (RTE) assays were carried out in strains of
to determine the potential of compounds
-
to block the multidrug efflux pump AcrAB-TolC. Drug-like properties were determined experimentally. Two compounds (
,
) containing non-condensed aromatic rings, significantly reduced oxacillin MICs in MRSA 19449, while
additionally enhanced the effectiveness of ampicillin. Results of molecular modelling confirmed the interaction with the allosteric site of PBP2a as a probable MDR-reversing mechanism. In RTE, the compounds inhibited AcrAB-TolC even to 90% (
). The 4-phenylbenzylidene derivative (
) demonstrated significant MDR-reversal "dual action" for
-lactam antibiotics in MRSA and inhibited AcrAB-TolC in
.
displayed also satisfied solubility and safety towards CYP3A4 in vitro.
In order to find new hypotensive drugs possessing higher activity and better selectivity, a new series of fifteen 5,5-dimethylhydantoin derivatives (1–15) was designed. Three-step syntheses, ...consisting of N-alkylations using standard procedures as well as microwaves, were carried out. Crystal structures were determined for compounds 7–9. All of the synthesized 5,5-dimethylhydantoins were tested for their affinity to αsub.1-adrenergic receptors (αsub.1-AR) using both in vitro and in silico methods. Most of them displayed higher affinity (Ki < 127.9 nM) to αsub.1-adrenoceptor than urapidil in radioligand binding assay. Docking to two subtypes of adrenergic receptors, αsub.1A and αsub.1B, was conducted. Selected compounds were tested for their activity towards two αsub.1-AR subtypes. All of them showed intrinsic antagonistic activity. Moreover, for two compounds (1 and 5), which possess o-methoxyphenylpiperazine fragments, strong activity (ICsub.50 < 100 nM) was observed. Some representatives (3 and 5), which contain alkyl linker, proved selectivity towards αsub.1A-AR, while two compounds with 2-hydroxypropyl linker (11 and 13) to αsub.1B-AR. Finally, hypotensive activity was examined in rats. The most active compound (5) proved not only a lower effective dose than urapidil but also a stronger effect than prazosin.
Searching for new chemosensitizers of bacterial multidrug resistance (MDR), chemical modifications of (Z)-5-(4-chlorobenzylidene)-2-(4-methylpiperazin-1-yl)-3H-imidazol-4(5H)-one (
) were performed. ...New compounds (
⁻
), with fused aromatic rings at position 5, were designed and synthesized. Crystallographic X-ray analysis proved that the final compounds (
⁻
) were substituted with tertiary amine-propyl moiety at position 3 and primary amine group at 2 due to intramolecular Dimroth rearrangement. New compounds were evaluated on their antibiotic adjuvant properties in either Gram-positive or Gram-negative bacteria. Efflux pump inhibitor (EPI) properties towards the AcrAB-TolC pump in
(EA289) were investigated in the real-time efflux (RTE) assay. Docking and molecular dynamics were applied to estimate an interaction of compounds
⁻
with penicillin binding protein (PBP2a). In vitro ADME-Tox properties were evaluated for compound
. Most of the tested compounds reduced significantly (4-32-fold) oxacillin MIC in highly resistant MRSA HEMSA 5 strain. The anthracene-morpholine derivative (
) was the most potent (32-fold reduction). The tested compounds displayed significant EPI properties during RTE assay (37⁻97%). The naphthyl-methylpiperazine derivative
showed the most potent "dual action" of both oxacillin adjuvant (MRSA) and EPI (
). Molecular modeling results suggested the allosteric mechanism of action of the imidazolones, which improved binding of oxacillin in the PBP2a active site in MRSA.
In this study, a search for new therapeutic agents that may improve the antibacterial activity of conventional antibiotics and help to successfully overcome methicillin-resistant Staphylococcus ...aureus (MRSA) infections has been conducted. The purpose of this work was to extend the scope of our preliminary studies and to evaluate the adjuvant potency of new derivatives in a set of S. aureus clinical isolates. The study confirmed the high efficacy of piperazine derivatives of 5-arylideneimidazol-4-one (7–9) tested previously, and it enabled the authors to identify even more efficient modulators of bacterial resistance among new analogs. The greatest capacity to enhance oxacillin activity was determined for 1-benzhydrylpiperazine 5-spirofluorenehydantoin derivative (13) which, at concentrations as low as 0.0625 mM, restores the effectiveness of β-lactam antibiotics against MRSA strains. In silico studies showed that the probable mechanism of action of 13 is related to the binding of the molecule with the allosteric site of PBP2a. Interestingly, thiazole derivatives tested were shown to act as both oxacillin and erythromycin conjugators in S. aureus isolates, suggesting a complex mode of action (i.e., influence on the Msr(A) efflux pump). This high enhancer activity indicates the high potential of imidazolones to become commercially available antibiotic adjuvants.
In this study, a search for new therapeutic agents that may improve the antibacterial activity of conventional antibiotics and help to successfully overcome methicillin-resistant Staphylococcus ...aureus (MRSA) infections has been conducted. The purpose of this work was to extend the scope of our preliminary studies and to evaluate the adjuvant potency of new derivatives in a set of S. aureus clinical isolates. The study confirmed the high efficacy of piperazine derivatives of 5-arylideneimidazol-4-one (7–9) tested previously, and it enabled the authors to identify even more efficient modulators of bacterial resistance among new analogs. The greatest capacity to enhance oxacillin activity was determined for 1-benzhydrylpiperazine 5-spirofluorenehydantoin derivative (13) which, at concentrations as low as 0.0625 mM, restores the effectiveness of β-lactam antibiotics against MRSA strains. In silico studies showed that the probable mechanism of action of 13 is related to the binding of the molecule with the allosteric site of PBP2a. Interestingly, thiazole derivatives tested were shown to act as both oxacillin and erythromycin conjugators in S. aureus isolates, suggesting a complex mode of action (i.e., influence on the Msr(A) efflux pump). This high enhancer activity indicates the high potential of imidazolones to become commercially available antibiotic adjuvants.
In order to find new hypotensive drugs possessing higher activity and better selectivity, a new series of fifteen 5,5-dimethylhydantoin derivatives (
-
) was designed. Three-step syntheses, ...consisting of N-alkylations using standard procedures as well as microwaves, were carried out. Crystal structures were determined for compounds
-
. All of the synthesized 5,5-dimethylhydantoins were tested for their affinity to α
-adrenergic receptors (α
-AR) using both in vitro and in silico methods. Most of them displayed higher affinity (Ki < 127.9 nM) to α
-adrenoceptor than urapidil in radioligand binding assay. Docking to two subtypes of adrenergic receptors, α
and α
, was conducted. Selected compounds were tested for their activity towards two α
-AR subtypes. All of them showed intrinsic antagonistic activity. Moreover, for two compounds (
and
), which possess o-methoxyphenylpiperazine fragments, strong activity (IC
< 100 nM) was observed. Some representatives (
and
), which contain alkyl linker, proved selectivity towards α
-AR, while two compounds with 2-hydroxypropyl linker (
and
) to α
-AR. Finally, hypotensive activity was examined in rats. The most active compound (
) proved not only a lower effective dose than urapidil but also a stronger effect than prazosin.
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