Phenolic Profile, Bioactivities and In Silico Analysis of the Trunk Bark of Acacia Cyanophylla Lindl.

In the current investigation, total phenolics and flavonoids of the methanolic extract obtained from the trunk bark of Acacia cyanophylla Lindl. were quantified by LC-HRMS technique. DPPH and ABTS reagents were employed to assay the antioxidant potential. The anti-tyrosinase and anti-α-amylase potentials were also assayed. The findings revealed that thirteen polyphenolic compounds were detected in the methanolic extract with trans-taxifolin (23.2 g/kg), as the major constituent. A. cyanophylla extract displayed a higher activity with DPPH test (IC50=10.14±1.00 µg/mL) than with ABTS (IC50=15.27±2.09 µg/mL). The same extract also exhibited interesting α-amylase inhibitory action (IC50 value of 4.00±0.17 µg/mL). Moreover, methanolic trunk bark extract exerted strong anti-tyrosinase capacity with an IC50 of 5.12±0.41 µg/mL in comparison to kojic acid (IC50=10.22±0.85 µg/mL) used as positive control. The antioxidant, anti-tyrosinase and anti-α-amylase potentials of the methanolic extract of A. cyanophylla trunk bark were reinforced by in silico molecular docking analyses, which confirmed the results of the in vitro tests.

Biological Activities of Novel Oleanolic Acid Derivatives from Bioconversion and Semi-Synthesis.

Oleanolic acid (OA) is a vegetable chemical that is present naturally in a number of edible and medicinal botanicals. It has been extensively studied by medicinal chemists and scientific researchers due to its biological activity against a wide range of diseases. A significant number of researchers have synthesized a variety of analogues of OA by modifying its structure with the intention of creating more potent biological agents and improving its pharmaceutical properties. In recent years, chemical and enzymatic techniques have been employed extensively to investigate and modify the chemical structure of OA. This review presents recent advancements in medical chemistry for the structural modification of OA, with a special focus on the biotransformation, semi-synthesis and relationship between the modified structures and their biopharmaceutical properties.

Simultaneous Exposure to Noise and Toluene Induces Oxidative and Inflammatory Damage in the Heart of Wistar Rats: Therapeutic Potential of Olea europaea L. Leaf Extract.

Workers in occupational settings often face simultaneous exposure to multiple risk factors, including noise and chemicals. This study aimed to investigate the effects of combined exposure to noise and toluene on the cardiac health of rats, with a focus on assessing the potential mitigating effects of Olea europaea L. (OLE) leaf extract (40 mg/kg/day). The evaluation involved scrutinizing biochemical and hematological markers, quantifying oxidative stress levels, determining proinflammatory cytokines in the serum, and conducting an in silico Docking studies. Forty-two male Wistar rats were divided into eight groups-(n = 6/group):-Control-group-(C),-OLE-group-(Rats administered OLE), NT-group (rats co-exposed to noise and toluene), NT-4 group-(rats co-exposed to noise and toluene four weeks after the exposure period), NT + OLE1-group (rats co-exposed to noise and toluene treated with OLE for one week), NT + OLE2-group-(rats co-exposed to noise and toluene treated with OLE for two weeks), NT + OLE3-group-(rats co-exposed to noise and toluene treated with OLE for three weeks), and NT + OLE4-group (rats co-exposed to noise and toluene treated with OLE for four weeks). The results revealed that combined exposure to noise and toluene led to oxidative damage and increased serum levels of proinflammatory cytokines. However, OLE treatment attenuated these effects by reducing lipid peroxidation and enhancing catalase and superoxide dismutase activities. Additionally, OLE treatment significantly decreased proinflammatory cytokine levels compared to the noise and toluene co-exposed group. The study highlighted the potential of OLE to attenuate the adverse effects of combined exposure to noise and toluene, attributed to its anti-inflammatory and antioxidant properties.

Phytochemical profiling, antioxidant, and tyrosinase inhibitory potential of the Acacia cyclops trunk bark: in vitro combined with in silico approach.

The aim of this study was to analyze the phytochemical profile of Acacia cyclops trunk bark ethyl acetate extract using LC-tandem mass spectrometry for the first time, along with evaluating its antioxidant and anti-tyrosinase properties. Consequently, we determined the total phenolic and flavonoid contents of the extract under investigation and identified and quantified 19 compounds, including phenolic acids and flavonoids. In addition to assessing their antioxidant potential against DPPH (2,2-diphenyl-1-picrylhydrazyl) and ABTS (2,2'-azino-bis-[3-ethylbenzothiazoline-6-sulfonic] acid) assays, in vitro and in silico studies were conducted to evaluate the tyrosinase inhibitory properties of the A. cyclops extract. The ethyl acetate trunk bark extract exhibited a substantial total phenolic content and demonstrated significant antioxidant activity in terms of free radical scavenging, as well as notable tyrosinase inhibitory action (half-maximal inhibitory concentration [IC50] = 14.08 ± 1.10 µg/mL). The substantial anti-tyrosinase activity of the examined extract was revealed through molecular docking analysis and druglikeness prediction of the main selected compounds. The findings suggest that A. cyclops extract holds promise as a potential treatment for skin hyperpigmentation disorders.

Olea europaea L. leaf extract mitigates pulmonary inflammation and tissue destruction in Wistar rats induced by concurrent exposure to noise and toluene.

This study aimed to investigate the effects of combined exposure to noise (85 dB(A)) and inhaled Toluene (300 ± 10 ppm) on rat lung health. It also aimed to assess the potential therapeutic effects of Olea europaea L. leaves extract (OLE) (40 mg/kg/day) using biochemical, histopathological, and immunohistochemical (IHC) analyses, as well as determination of pro-inflammatory cytokines (TNF-α and IL-1ß), and in silico Docking studies. The experiment involved forty-two male Wistar rats divided into seven groups, each exposed to a 6-week/6-hour/day regimen of noise and Toluene. The groups included a control group, rats co-exposed to noise and Toluene, and rats co-exposed to noise and Toluene treated with OLE for different durations. The results indicated that noise and Toluene exposure led to structural damage in lung tissue, oxidative harm, and increased levels of pro-inflammatory cytokines (TNF-α and IL-1ß). However, the administration of OLE extract demonstrated positive effects in mitigating these adverse outcomes. OLE treatment reduced lipid peroxidation and enhanced the activities of catalase and superoxide dismutase, indicating its anti-oxidant properties. Furthermore, OLE significantly decreased the levels of pro-inflammatory cytokines compared to the groups exposed to noise and Toluene without OLE treatment. Moreover, the in silico investigation substantiated a robust affinity between COX-2 and OLE components, affirming the anti-inflammatory activity. Overall, our findings suggest that OLE possesses anti-inflammatory and anti-oxidative properties that mitigate the adverse effects of concurrent exposure to noise and Toluene.

Ozone therapy (O2-O3) alleviates the progression of early intervertebral disc degeneration via the inhibition of oxidative stress and the interception of the PI3K/Akt/NF-κB signaling pathway.

Intervertebral disc degeneration (IDD) stands for the most frequent cause of low back pain. Finding a cure for this disease is an important challenge as current conservative treatments and surgical interventions fail to bring a solution to this disease. Ozone therapy (O2-O3) has yielded outstanding outcomes in intervertebral disc pathology. The ozone's efficacy in the treatment of IDD remains unconfirmed. This study aimed to assess the effectiveness of intradiscal ozone injection on IDD induced in a rat. Effects of ozone therapy on the viability of nucleus pulposus cells were evaluated by CCK-8 assays. Macrophage immunoreactivity was detected by immunohistochemical, the expression of collagen type II was evaluated by western blot, and measurement of oxidative stress parameters was realized. Molecular docking studies were carried out in order to predict the interaction formed between O3 and the target enzymes, on the one hand, O3 with PI3K and, on the other hand, O3 with COX-2. IRM, X-ray, hematoxylin-eosin, and bleu alcian staining were realized to assess the therapeutic impacts of ozone in the puncture-induced rat model of IDD. In vivo, O3 ameliorated the IDD in the early stage of this disease. It was also displayed in molecular docking that O3 might bind to PI3K to suppress the PI3K/Akt/NF-κB signaling pathway. This study's results show that the O3 should be administered at the low grade of IDD and at an early stage because it cannot restore the advanced inflammatory alteration of the IVD. Our results corroborated also that O3 inhibits the progression of IDD via the PI3K/Akt/NF-κB signaling pathway, which supports O3 as an effective therapeutic option for treating IDD.

Semi-synthesis, α-amylase inhibition, and kinetic and molecular docking studies of arylidene-based sesquiterpene coumarins isolated from Ferula tunetana Pomel ex Batt.

Despite all the significant progresses made to enhance the efficacy of the existing bank of drugs used to manage and cure type II diabetes mellitus, there is still a need to search and develop novel bioactive compounds with superior efficacy and minimal adverse effects. This study describes the valorization of the natural bioactive sesquiterpene coumarin via the semi-synthesis of new analogs and the study of their α-amylase inhibition activity. The sesquiterpene coumarin named coladonin (1) was quantitatively isolated from the chloroform extract of endemic Ferula tunetana roots. Subsequently, the oxidation of 1via the Jones oxidation reaction, used as a key reaction, afforded precursor 2. The condensation of oxidized coladonin (2) with various aryl aldehydes provided a series of new arylidene-based sesquiterpene coumarin derivatives (3a-m), which were characterized by NMR and ESI-HRMS experiments. All derivatives evaluated in vitro for their α-amylase inhibitory potential showed interesting α-amylase inhibition with IC50 values ranging from 7.24 to 28.98 µM. Notably, compounds 3k and 3m exhibited lower IC50 values (7.24 µM and 8.38 µM, respectively) compared to the standard (acarbose: IC50 = 9.83 µM). In addition, the structure-activity relationship (SAR) for all the compounds was studied. The most active compounds were found to be mixed-type inhibitors, which was revealed by kinetic studies. Furthermore, molecular in silico docking studies were established for all synthesized analogs with the binding site for the α-amylase enzyme.