Search

Context: Medicinal plants are considered the bases for chemical compounds that could be used therapeutically. Euphorbia paralias belongs to the family Euphorbiaceae. Some species of this family have demonstrated anticancer and antioxidant activities. However, the chemical compounds responsible for the anticancer and antioxidant activities of E. paralias have not been extensively studied. Aims: To identify chemical compounds of E. paralias that possess anticancer and antioxidant properties. Methods: Liquid chromatography/mass spectrometry (LC/MS) was employed to characterise the chemical compounds E. paralias methanolic extract. Using the MTT assay, anticancer activity was investigated. DPPH, ABTS, and FRAP tests were applied to assess the antioxidant action. Results: Several polyphenolic compounds, including phenolic acids, flavonoids, flavanols, fatty acids, terpenoids, and sterols, were identified in the extract. These compounds possess various biological activities. The cancer cell lines most affected by the E. paralias extract were PANC-1 with an IC50 of 60.1 ± 10.1 µg /mL, DLD-1 with an IC50 of 64.3 ± 17.5 µg/mL, and A549 with IC50 of 71.9 ± 9.8 µg/mL. The values of IC50 for the MCF-7 and U87 cancer cell lines were 74.6 ± 15.6 µg/mL and 121.3 ± 17.2 µg/mL, respectively. The cell line of normal HDF had an IC50 of 128.9 ± 11.7 µg/mL. ABTS and DPPH showed that the methanol extract scavenged the free radicals by 89.57% and 92.65%, respectively, compared to ascorbic acid and Trolox positive controls. The FRAP test showed that 1 mg of methanol extract was equivalent to 387.41 μM of Trolox. Conclusions: E. paralias contained various phytochemicals that may have anticancer and antioxidant activities. E. paralias may possess anticancer activity against pancreatic, colon and lung cancers, and it may also have antioxidant activity. Future research is recommended to investigate the isolated phytochemicals from E. paralias.

Relationship between excited state dynamics and nonlinear optical (NLO) parameters is very unique. Herein, three different polyoxometalates (POMs) namely WD-POM (Wells-Dawson POM) based porphyrin hybrids WDPOM3PyP, Trans-2WDPOM2PyP, and 3WDPOMPyP (having one, two, and three WD-POM respectively), and their porphyrin precursors with (Trishydroxyl amino methane) namely Tris3PyP, Trans-2Tris2PyP, and 3TrisPyP respectively have been used for the study. Fluorescence decay and Z-scan studies by using nanosecond (ns) time span conveys the corresponding lifespan for each excited state, along with the NLO analysis respectively. The calculated lifetime data were found in the range of 3WDPOMPyP (τ 1  = 5.65 ns), Trans-2WDPOM2PyP (τ 1  = 2.21 ns), and WDPOM3PyP (τ 1  = 1.96 ns). Third order NLO measurements represented that WDPOM3PyP showed better NLO response (χ 3  = 2.26 × 10 -10 esu and β = 1.54 × 10 -5 esu) as compared to Trans-2WDPOM2PyP (χ 3  = 1.73 × 10 -10 esu and β = 1.53 × 10 -5 esu), and 3WDPOMPyP (χ 3  = 1.55 × 10 -10 esu and β = 0.65 × 10 -5 esu) obtained at wavelength of 532 nm. Electrochemical studies have shown that the minor energy differences between the singlet and triplet excited states are responsible for intercrossing system (ISC) that helps in the transfer of electrons from porphyrin moiety to WD-POM. By absorbing a photon, the excited species were produced causing an initial charge transfer. This charge transfer state undergoes an electron transfer decaying to the lowest triplet state, and singlet state causing an increase in NLO. The obtained results indicated potential uses in photonic and all-optical switching devices., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier B.V. All rights reserved.)

Diabetes mellitus type 2 (T2DM) can be managed by targeting dipeptidyl peptidase-4 (DPP-4), an enzyme that breaks down and deactivates peptides such as GIP and GLP-1. In this context, a new series of 2-(2-substituted hydrazineyl)thiazole derivatives 4, 5, 6, 8, 10, and 11 conjugated with the 2-hydroxy-5-(pyrrolidin-1-ylsulfonyl)benzylidene fragment were designed and synthesized. The virtual screening of the designed derivatives inside DPP-4 demonstrated good to moderate activity, with binding affinity ranging from -6.86 to -5.36 kcal/mol compared to Sitagliptin (S=-5.58 kcal/mol). These results encourage us to evaluate DPP-4 using in-vitro fluorescence-based assay. The in-vitro results exhibited inhibitory percentage (IP) values ranging from 40.66 to 75.62 % in comparison to Sitagliptin (IP=63.14 %) at 100 µM. Subsequently, the IC 50 values were determined, and the 5-aryl thiazole derivatives 10 and 11 revealed strong potent IC 50 values 2.75 ± 0.27 and 2.51 ± 0.27 µM, respectively, compared to Sitagliptin (3.32 ± 0.22 µM). The SAR study exhibited the importance of the substituents on the thiazole scaffold, especially with the hydrophobic fragment at C5 of the thiazole, which has a role in the activity. Compounds 10 and 11 were further assessed toward α-glucosidase and α-amylase enzymes and give promising results. Compound 10 showed good activity against α-glucosidase with IC 50 value of 3.02 ± 0.23 µM compared to Acarbose 3.05 ± 0.22 µM and (11 = 3.34 ± 0.10 µM). On the other hand, for α-amylase, compound 11 was found to be most effective with IC 50 value of 2.91 ± 0.23 µM compared to compound 10 = 3.30 ± 0.16 µM and Acarbose (2.99 ± 0.21 µM) indicating that these derivatives could reduce glucose by more than one target. The most active derivatives 10 and 11 attracted great interest as candidates for oral bioavailability and safe toxicity profiles compared to positive controls. The in-silico docking simulation was performed to understand the binding interactions inside the DPP-4, α-glucosidase, and α-amylase pockets, and it was found to be promising antidiabetic agents through a number of interactions., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Inc. All rights reserved.)

Uncontrolled diabetes can lead to hyperglycemia, which causes neuropathy, heart attacks, retinopathy, and nervous system damage over time, therefore, controlling hyperglycemia using potential drug target inhibitors is a promising strategy. This work focused on synthesizing new derivatives via the diazo group, using a hybridization strategy involving two approved drugs, paracetamol and several sulfonamides. The newly designed diazo-paracetamols 5-12 were fully characterized and then screened for in vitro α-amylase and α-glucosidase activities and exhibited inhibitory percentages (IP) = 92.5-96.5 % and 91.0-95.7 % compared to Acarbose IP = 96.5 and 95.8 %, respectively at 100 μg/mL. The IC 50 values of the synthesized derivatives were evaluated against α-amylase and α-glucosidase enzymes, and the results demonstrated moderate to potent activity. Among the tested diazo-paracetamols, compound 11 was found to have the highest potency activity against α-amylase with IC 50 value of 0.98 ± 0.015 μM compared to Acarbose IC 50  = 0.43 ± 0.009 μM, followed by compound 10 (IC 50  = 1.55 ± 0.022 μM) and compound 9 (IC 50  = 1.59 ± 0.023 μM). On the other hand, for α-glucosidase, compound 10 with pyrimidine moiety demonstrated the highest inhibitory activity with IC 50  = 1.39 ± 0.021 μM relative to Acarbose IC 50  = 1.24 ± 0.029 μM and the order of the most active derivatives was 10 > 9 (IC 50  = 2.95 ± 0.046 μM) > 11 (IC 50  = 5.13 ± 0.082 μM). SAR analysis confirmed that the presence of 4,5-dimethyl-isoxazole or pyrimidine nucleus attached to the sulfonyl group is important for activity. Finally, the docking simulation was achieved to determine the mode of binding interactions for the most active derivatives in the enzyme's active site., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Masson SAS. All rights reserved.)

Although the Caesarean section (CS) is considered a harmless surgery, it has various complications. Women scheduled for elective CSs often have high levels of anxiety due to a lack of knowledge. The aim of this quantitative quasi-experimental study was to determine the relationship between preoperative educational sessions and anxiety levels among women undergoing CSs. The study was conducted at the antenatal unit in the King Faisal Medical Complex (KFMC) in Taif, Saudi Arabia, using a structured interview questionnaire, the State-Trait Anxiety Inventory (STAI), and satisfaction interviews. A total of 50 pregnant women participated in this study, who were divided into two groups: 25 participants in the intervention group and 25 in the control group. Most participants (92%) in the intervention group had low anxiety levels following educational sessions, and 96% of the participants were very satisfied with the preoperative information they had been given. Women in the control group (again, 92%) had high anxiety levels, and there was a significant difference in the anxiety levels of the intervention and control groups ( p ≤ 0.5) after the educational sessions. Providing proper preoperative education about CSs can reduce preoperative anxiety, improve patient outcomes, and enhance patients' involvement in their care and decision-making.