Cytotoxic effects of extracts obtained from plants of the Oleaceae family: bio-guided isolation and molecular docking of new secoiridoids from Jasminum humile

ContextTraditionally, Oleaceae plants are used to treat many diseases, such as rheumatism, hypercholesterolaemia, or ulcers.ObjectivesTo investigate the cytotoxic potential of Jasminum humile L., Jasminum grandiflorum L., and Olea europaea L. (Oleaceae) extracts against selected human cancer cells lines, followed by a phytochemical investigation of the most potent one.Materials and methodsThe 95% ethanol extracts of aerial parts of three oleaceous plants were examined for their cytotoxicity against HepG-2, MCF-7, and THP-1 cell lines using MTT assay and doxorubicin (positive control). J. humile was bio-selected and submitted to bio-guided fractionation. Chromatographic workup of ethyl acetate and n-butanol fractions afforded two new compounds; 1-methoxyjasmigenin (1) and 1-methyl-9-aldojasmigenin (2), along with five known ones (3–7). Structures were unambiguously elucidated using 1D/2D NMR and ESI-HRMS. Isolated compounds were assessed for their anti-proliferative potential, and both selectivity index and statistical significance were determined. Molecular docking was conducted against the Mcl-1 receptor using (AZD5991) as a standard.ResultsJasmoside (5) was the most potent anticancer compound showing IC₅₀ values of 66.47, 41.32, and 27.59 µg/mL against HepG-2, MCF-7, and THP-1 cell lines, respectively. Moreover, isojasminin (4) exhibited IC₅₀ values of 33.49, 43.12, and 51.07 µg/mL against the same cell lines, respectively. Interestingly, 5 exhibited the highest selectivity index towards MCF-7 and THP-1, even greater than doxorubicin. Molecular docking results were in full agreement with the MTT assay and the proposed SAR.ConclusionIn this study, two new compounds were purified. The biological activity highlighted jasmoside (5) as a lead anticancer drug for further future investigation.     

Consensus guidelines on pediatric acute rheumatic fever and rheumatic heart disease

JUSTIFICATION: Acute rheumatic fever and rheumatic chronic valvular heart disease is an important preventable cause of morbidity and mortality in suburban and rural India. Its diagnosis is based on clinical criteria. These criteria need verification and revision in the Indian context. Furthermore, there are glaring differences in management protocols available in literature. These facts prompted Indian Academy of Pediatrics to review the management of rheumatic fever. PROCESS: Management of Rheumatic fever was reviewed and recommendation was formulated at national consultative meeting on 20th May 2007 at New Delhi. OBJECTIVES: To formulate uniform guidelines on management of acute rheumatic fever and rheumatic heart disease in the Indian context. Guidelines were formulated for the management of streptococcal pharyngitis, acute rheumatic fever and its cardiac complication as well as secondary prophylaxis for recurrent episodes. RECOMMENDATIONS: (1) Streptococcal eradication with appropriate antibiotics (Benzathine penicillin single dose or penicillin V oral or azithromycin). (2) Diagnosis of rheumatic fever based on Jones criteria. (3) Control inflammatory process with aspirin with or without steroids (total duration of treatment of 12 weeks). (4) Treatment of chorea according to severity (therapy to continue for 2-3 weeks after clinical improvement). (5) Protocol for managing cardiac complication like valvular heart disease, congestive heart failure and atrial fibrillation. (6) Secondary prophylaxis with benzathine penicillin and management of anaphylaxis.     

Introduction of cadmium chloride additive to improve the performance and stability of perovskite solar cells

With the increase in the importance of using green energy sources to meet the world''s energy demands, attempts have been made to push perovskite solar cell technology toward industrialization all around the world. Improving the properties of perovskite materials as the heart of PSCs is one of the methods to fabricate favorable photovoltaic (PV) solar cells based on perovskites. Here, cadmium chloride (CdCl₂) was used as an additive source for the perovskite precursor to improve its PV properties. Results indicated CdCl₂ improves the perovskite growth and tailors its crystalline properties, suggesting boosted charge transport processes in the bulk and interfaces of the perovskite layer with electron–hole transport layers. Overall, by incorporation of 1.0% into the MAPbI₃ layer, a maximum power conversion efficiency of 15.28% was recorded for perovskite-based solar cells, higher than the 12.17% for the control devices. The developed method not only improved the PV performance of devices but also boosted the stability behavior of solar cells due to the passivated domain boundaries and enhanced hydrophobicity in the CdCl₂-based devices.

With the increase in the importance of using green energy sources to meet the world''s energy demands, attempts have been made to push perovskite solar cell technology toward industrialization all around the world.     

Effect of Zr and Ti Addition and Aging Treatment on the Microstructure and Tensile Properties of Al-2%Cu-Based Alloys

The present work investigated the effect of aging treatment on the microstructure and tensile properties of an Al-2%Cu base alloy containing various additions of Zr and other alloying elements. Aging was carried out at temperatures of 180–300 °C for different aging times at each temperature. The tensile properties indicated that Zr additions improved the strength of the base alloy, especially at high Zr levels at 180 °C. At the 220 °C aging temperature, however, while Zr addition did not have a beneficial effect on the alloy strength, the ductility was found to improve. Zr-Ti combined additions had a significant effect on the microstructure of the base alloy, as the morphology of the α-Al grains transformed into a non-dendritic morphology, and the grain size decreased sharply. These effects were at their maximum at 180 °C and 0.5 wt% Zr addition. Moreover, the Zr-containing alloys aged at higher temperatures, such as 220 °C and 240 °C, maintained a noticeably higher level of strength over the base alloy aged at the same temperatures. Quality index charts based on the tensile test data also reflected an improvement in alloy quality and strength with Zr-Ti combined additions.     

Influence of Cross-Section Shape and FRP Reinforcement Layout on Shear Capacity of Strengthened RC Beams

The evaluation of the shear capacity of an FRP-strengthened reinforced-concrete beam is challenging due to the complex interaction between different contributions provided by the concrete, steel stirrup and FRP reinforcement. The shape of the beam and the FRP inclination can have paramount importance that is not often recognized by the models that are suggested by codes. The interaction among different resisting mechanisms has a significant effect on the shear capacity of beams, since it can cause a reduction in the efficiency of some resisting mechanisms. A comparative study of the performance in the shear resistance assessment provided by three models with six different effectiveness factors (R) is performed, considering different cross-section shapes, FRP wrapping schemes, inclination and anchorage systems. The results revealed that the cross-section shape, the FRP inclination and the efficiency of the FRP anchorages have a significant effect on the shear strength of beams. The analysis results show that the three models are able to provide an accurate average estimation of shear strength (but with a coefficient of variation up to 0.35) when FRP reinforcement orthogonal to the beam axis is considered, while a significant underestimation (up to 19%) affected the results for inclined FRP reinforcement. Moreover, all the models underestimated the resistance of beams with a T section.     

Evaluating the Effect of Tideglusib-Loaded Bioactive Glass Nanoparticles as a Potential Dentine Regenerative Material

Dental pulp treatment is the least intrusive procedure currently available for preserving the vitality of the pulp. Several studies are underway to improve the bioactivity of pulp capping materials. Tideglusib isa potent anti-inflammatory, antioxidant, and a regenerative drug developed against Alzheimer’s disease and has been shown to be effective in the treatment of dental cavities. However, its bioactive properties encapsulated within the nanoparticles as a component of pulp capping material are largely unknown. In this study, tideglusib-loaded bioactive glass nanoparticles were synthesized (tideglusib-BgNPs) and mixed at various concentrations into the calcium silicate cement to testits physiomechanical and bioactivitiescompared with biodentine (control). The calcium silicate cement with 10wgt% tideglusib-BgNPs showed comparable physiomechanical properties to that of biodentine. Additionally, the assessment of cytotoxicity and bioactivity (cell proliferation, wound healing, and cell migration assays) showed increased bioactivity in terms of better wound healing, increased proliferation, and better migration of human dental pulp stem cells than biodentine. These findings suggest new opportunities to use tideglusib-BgNPs in pulp therapy.     

Mechanical pulmonic valve thrombosis: expanding role of cardiac CT and multimodality imaging

We report a case of a 44-year-old man with a clinical history of Tetralogy of Fallot status post staged surgical correction with mechanical pulmonic valve replacement who presented with progressive exertional dyspnea in the setting of non-compliance with anticoagulation. In the context of this suggestive clinical presentation, the diagnosis of mechanical pulmonic valve thrombosis (MPVT) was made possible via multimodality imaging, including transthoracic echocardiogram and cardiac computed tomography angiography. Due to the uncommon nature of the condition, the patient was treated with systemic thrombolysis and anticoagulation using evidence-based guidelines, largely extrapolated from left-sided mechanical valve thrombosis. Our case underscores the importance of anticoagulation in MPVT and recognizing the features of MPVT on clinical history, physical examination, and multimodality imaging. It is essential to understand the pivotal role of multimodality imaging in the assessment of MPVT and realize the limitations of available data regarding the management of MPVT in the current era.     

Isolation,characterisation and complement fixation activity of acidic polysaccharides from Argemone mexicana used as antimalarials in Mali

ContextGlobal studies on Argemone mexicana L. (Papaveraceae) traditionally used against malaria in Mali are limited to its low-mass compounds activities, and little information on its bioactive polysaccharides is available.ObjectiveThis study determines the structure and the immunomodulatory activity of polysaccharides from aerial parts of A. mexicana.Materials and methodsAcidic polysaccharides from this plant material named HMAmA1 and HMAmA2 were isolated from water extracts. Their monosaccharide composition was determined by gas chromatography. Glycosidic linkages were determined using GC-MS. NMR was also applied. The polymers were tested for effects on the human complement system in vitro at different doses.ResultsThe monosaccharide composition showed that the two polysaccharides contained in different amounts the following monomers: arabinose, rhamnose, galactose, and galacturonic acid. Overall structural analysis showed the presence of a low ratio of 1,2-linked rhamnose compared to 1,4-linked galacturonic acid with arabinogalactans substituted on position 4 of rhamnose. NMR data showed the presence of galacturonans alternated by rhamnogalacturonans bearing arabinose and galactose units. α-Linkages were found for l-arabinose, l-rhamnose and d-galacturonic acid, while β-linkages were found for d-galactose. The two polysaccharides exhibited strong complement fixation activities, with HMAmA1 being the highest potent fraction. ICH₅₀ value of HMAmA1 was 5 µg/mL, compared to the control BPII being 15.9 µg/mL.Discussion and conclusionsPolysaccharides form A. mexicana presented a complement fixation effect. The complement system is an important part of the immune defense, and compounds acting on the cascade are of interest. Therefore, these polymers may be useful as immunodulatory agents.     

Inhibitory potential of nitrogen,oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase

Heterocycles are the key structures in organic chemistry owing to their immense applications in the biological, chemical, and pharmaceutical fields. Heterocyclic compounds perform various noteworthy functions in nature, medication, innovation etc. Most frequently, pure nitrogen heterocycles or various positional combinations of nitrogen, oxygen, and sulfur atoms in five or six-membered rings can be found. Inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes is a popular strategy for the management of numerous mental diseases. In this context, cholinesterase inhibitors are utilized to relieve the symptoms of neurological illnesses like dementia and Alzheimer''s disease (AD). The present review focuses on various heterocyclic scaffolds and their role in designing and developing new potential AChE and BChE inhibitors to treat AD. Moreover, a detailed structure–activity relationship (SAR) has been established for the future discovery of novel drugs for the treatment of AD. Most of the heterocyclic motifs have been used in the design of new potent cholinesterase inhibitors. In this regard, this review is an endeavor to summarize the biological and chemical studies over the past decade (2010–2022) describing the pursuit of new N, O and S containing heterocycles which can offer a rich supply of promising AChE and BChE inhibitory activities.

The present review focuses on various heterocyclic scaffolds and their role in designing and developing new potential AChE and BChE inhibitors to treat AD.     

Nutritional Assessment and Interventions in Elective Hip and Knee Arthroplasty: a Detailed Review and Guide to Management

Purpose of Review8.5 to 50% of total joint arthroplasty (TJA) patients are reported to have preoperative malnutrition. The narrative review identifies the relationship between preoperative malnutrition for TJA patients and postoperative outcomes as well as the use of perioperative nutritional intervention to improve postoperative complications.Recent FindingsBiochemical/laboratory, anthropometric, and clinical measures have been widely used to identify preoperative nutritional deficiency. Specifically, serum albumin is the most prevalent used marker in TJA because it has been proven to be correlated with protein-energy malnutrition due to the surgical stress response. However, there remains a sustained incidence of preoperative malnutrition in total knee arthroplasty (TKA) and total hip arthroplasty (THA) patients due to a lack of agreement among the available nutritional screening tools and utilization of isolated laboratory, anthropometric, and clinical variables. Previous investigations have also suggested preoperative malnutrition to be a prognostic indicator of complications in general, cardiac, vascular, and orthopaedic surgery specialties.SummarySerum albumin, prealbumin, transferrin, and total lymphocyte count (TLC) can be used to identify at-risk patients. It is important to employ these markers in the preoperative setting because malnourished TKA and THA patients have shown to have worse postoperative outcomes including prolonged length, increased reoperation rates, increased infection rates, and increased mortality rates. Although benefits from high-protein and high-anti-inflammatory diets have been exhibited, additional research is needed to confirm the use of perioperative nutritional intervention as an appropriate treatment for preoperative TJA patients.