Antiproliferative and Cytotoxic Properties of Propynoyl Betulin Derivatives against Human Ovarian Cancer Cells: In Vitro Studies.

Due to the incidence of ovarian cancer (OC) and the limitations of available therapeutic strategies, it is necessary to search for novel therapeutic solutions. The aim of this study was to evaluate the cytotoxic effect of betulin 1 and its propynoyl derivatives 2-6 against ovarian cancer cells (SK-OV-3, OVCAR-3) and normal myofibroblasts (18Co). Paclitaxel was used as the reference compound. The propynoyl derivatives 2-6 exhibited stronger antiproliferative and cytotoxic activities compared to betulin 1. In both ovarian cancer cell lines, the most potent compound was 28-propynoylbetulin 2. In the case of compound 2, the calculated IC50 values were 0.2 µM for the SK-OV-3 cells and 0.19 µM for the OVCAR-3 cells. Under the same culture conditions, the calculated IC50 values for compound 6 were 0.26 µM and 0.59 µM, respectively. It was observed that cells treated with compounds 2 and 6 caused a decrease in the potential of the mitochondrial membrane and a significant change in cell morphology. Betulin 1, a diol from the group of pentacyclic triterpenes, has a confirmed wide spectrum of biological effects, including a significant anticancer effect. It is characterized by low bioavailability, which can be improved by introducing changes to its structure. The results showed that chemical modifications of betulin 1 only at position C-28 with the propynoyl group (compound 2) and additionally at position C-3 with the phosphate group (compound 3) or at C-29 with the phosphonate group (compound 6) allowed us to obtain compounds with greater cytotoxic activity than their parent compounds, which could be used to develop novel therapeutic systems effective in the treatment of ovarian cancer.

Temporal and Spatial Characteristics of Pacing Strategy in Elite Women's 400 Meters Hurdles Athletes.

The main objective of the study was to assess the pacing strategy of running 400 m hurdles of the world-level female athletes over the past 40 years based on the functional asymmetry -temporal and spatial characteristics. The data were collected from 1983 to 2019 using the review of scientific literature. Over the 35 years of the study, 37 top-level competitions with 283 finalists-competitors were included. The analysis of the 400 m hurdle covered mainly spatial and temporal factors of the run, related to those technical skills, the level of motor skills, and somatic structure. In addition to the basic statistics, the ANOVA analysis of variance, regression analysis, Pearson correlation, the principal component analysis (PCA), and Kaiser's criterion was used for the multivariate analysis. The final result in the 400 mH run is determined not by the simple sum of the individual temporal and/or spatial characteristics of the run (the number of steps, the type of attacking leg, but their interaction in the area of functional asymmetry. The decisive factor in the 400 mH run strategy is the second curve, where the emphasis is on the optimal setting of the stride pattern in the context of minimizing the loss of running speed. Additionally, the application of multidimensional statistical methods is a valuable tool that allows to significantly deepen the interpretation of the obtained results, and thus optimize a strategy for a 400 mH run.

Uncommon Bone Injuries in Soccer Players.

Soccer is the most common team sport in the world. A significant number of players are associated with a large number of injuries. Injuries occur in a variety of contexts regardless of the age or performance level of players. The vast majority of injuries involve soft tissues. Bone injuries are less common, but usually result in long-term exclusion from the game. Three different types of fractures related to soccer are classified as acute types, stress fractures and avulsion. This manuscript outlines the diagnostic procedures and treatments for stress fractures, avulsion fractures and bone cyst. The common feature of the described injuries includes frequent difficulties associated with the correct diagnosis and treatment direction. In therapeutic treatment, the doctor and the patient often have to choose between conservative treatment and surgical treatment, which in many cases is not simple. We suggest that in the event of injuries to soccer players, surgical treatment should be used, shortening the time to return to full sports activity. A very important element of the therapeutic process is proper rehabilitation, which should be individually tailored to the patient in order to optimize the treatment process. Some of the rehabilitation protocols should be permanently incorporated into the warm-up protocols for training. Such a procedure has a preventive effect.

Analysis of intercondylar notch size and shape in patients with cyclops syndrome after anterior cruciate ligament reconstruction.

BACKGROUND: Cyclops lesion is the second most common cause of extension loss after anterior cruciate ligament reconstruction. This study focused on the correlation between the anatomy of the intercondylar notch and the incidence of cyclops lesion. To determine whether the size and shape of the intercondylar notch are related to cyclops lesion formation following anterior cruciate ligament reconstruction according to magnetic resonance imaging (MRI) findings. METHODS: One hundred twenty-five (125) patients were retrospectively evaluated. The notch width index (NWI) and notch shape index (NSI) were measured based on coronal and axial MRI sections in patients diagnosed with cyclops syndrome (n = 25), diagnosed with complete anterior cruciate ligament (ACL) tears (n = 50), and without cyclops lesions or ACL ruptures (n = 50). RESULTS: Imaging analysis results showed that the cyclops and ACL groups had lower mean NWI and NSI values than the control group. Significant between-group differences were found in NSI (p = 0.0140) based on coronal cross-sections and in NWI (p = 0.0026) and NSI (p < 0.0001) based on axial sections. CONCLUSIONS: The geometry of the intercondylar notch was found to be associated with the risk of cyclops lesion formation and ACL rupture.

The Fifth Metatarsal Bone Fracture in Athletes - Modalities of Treatment Related to Agility in Soccer Players.

The 5th metatarsal fracture is a common foot fracture which could exclude a player from competition for several months and significantly affect his or her career. This manuscript presents the treatment and rehabilitation of professional soccer players who had acute fractures of the 5th metatarsal bone and a cannulated screw fixation. The main purpose of the analysis was to determine the minimum time necessary for a permanent return to the sport after a 5th metatarsal fracture among professional soccer players. We followed the surgical and rehabilitation path of 21 professional soccer players from the Polish League (Ist and IInd divisions) who suffered from the 5th metatarsal bone fracture. All players underwent standard percutaneous internal fixation with the use of cannulated screws. The total inability to play lasted for 9.2 (± 1.86) weeks among players treated only surgically (n = 10), 17.5 (± 2.5) weeks in the conservative and later surgery group, excluding players with nonunion (n = 6), and 24.5 (± 10.5) weeks for nonunion and switch treatment (n = 4) players. Prompt fracture stabilization surgery is recommended for athletes, enabling the implementation of an aggressive rehabilitation protocol as soon as possible. Early limb loading after surgery (from week 2) does not delay fracture healing or hinder the bone union, thus rehabilitation plays a crucial role in shortening the time of RTP (return to play) and is obligatory for each athlete who undergoes surgical treatment.

Nanoformulations for Delivery of Pentacyclic Triterpenoids in Anticancer Therapies.

The search for safe and effective anticancer therapies is one of the major challenges of the 21st century. The ineffective treatment of cancers, classified as civilization diseases, contributes to a decreased quality of life, health loss, and premature mortality in oncological patients. Many natural phytochemicals have anticancer potential. Pentacyclic triterpenoids, characterized by six- and five-membered ring structures, are one of the largest class of natural metabolites sourced from the plant kingdom. Among the known natural triterpenoids, we can distinguish lupane-, oleanane-, and ursane-types. Pentacyclic triterpenoids are known to have many biological activities, e.g., anti-inflammatory, antibacterial, hepatoprotective, immunomodulatory, antioxidant, and anticancer properties. Unfortunately, they are also characterized by poor water solubility and, hence, low bioavailability. These pharmacological properties may be improved by both introducing some modifications to their native structures and developing novel delivery systems based on the latest nanotechnological achievements. The development of nanocarrier-delivery systems is aimed at increasing the transport capacity of bioactive compounds by enhancing their solubility, bioavailability, stability in vivo and ensuring tumor-targeting while their toxicity and risk of side effects are significantly reduced. Nanocarriers may vary in sizes, constituents, shapes, and surface properties, all of which affect the ultimate efficacy and safety of a given anticancer therapy, as presented in this review. The presented results demonstrate the high antitumor potential of systems for delivery of pentacyclic triterpenoids.