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This study focused on the isolation of actinobacteria capable of producing extracellular keratinase from keratin-rich residues, which led to the selection of an actinobacterial strain referenced as Streptomyces strain DZ 06 (ES41). The Plackett–Burman screening plan was used for the statistical optimization of the enzymatic production medium, leading to the identification of five key parameters that achieved a maximum activity of 180.1 U/mL. Further refinement using response surface methodology (RSM) with a Box–Behnken design enhanced enzyme production to approximately 458 U/mL. Model validation, based on the statistical predictions, demonstrated that optimal keratinase activity of 489.24 U/mL could be attained with 6.13 g/L of chicken feather meal, a pH of 6.25, incubation at 40.65 °C for 4.11 days, and an inoculum size of 3.98 × 107 spores/mL. The optimized culture conditions yielded a 21.67-fold increase in keratinase compared with the initial non-optimized standard conditions. The results show that this bacterium is an excellent candidate for industrial applications when optimal conditions are used to minimize the overall costs of the enzyme production process. [ABSTRACT FROM AUTHOR]

The convenient synthesis of dihydroberberine by the reduction of berberine is described as an experiment for an upper-division undergraduate organic chemistry laboratory course. Students obtained up to 74% yield of the desired pure product without the use of chromatographic techniques. The antimicrobial activities of both compounds against "Staphylococcus aureus" and "Candida albicans" were then assessed and compared in an upper-division undergraduate microbiology laboratory course. The students verified that berberine shows higher antimicrobial activity than its derivative dihydroberberine, demonstrating that small changes in a chemical structure can result in great biological differences.

Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA) are classified as high-risk infections that can lead to death, particularly among older individuals. Nowadays, plant nanoparticles such as glycyrrhizic acid are recognized as efficient bactericides against a wide range of bacterial strains. Recently, scientists have shown interest in plant extract nanoparticles, derived from natural sources, which can be synthesized into nanomaterials. Interestingly, glycyrrhizic acid is rich in antioxidants as well as antibacterial agents, and it exhibits no adverse effects on normal cells. In this study, glycyrrhizic acid nanoparticles (GA-NPs) were synthesized using the hydrothermal method and characterized through physicochemical techniques such as UV–visible spectrometry, DLS, zeta potential, and TEM. The antimicrobial activity of GA-NPs was investigated through various methods, including MIC assays, anti-biofilm activity assays, ATPase activity assays, and kill-time assays. The expression levels of mecA, mecR1, blaR1, and blaZ genes were measured by quantitative RT-qPCR. Additionally, the presence of the penicillin-binding protein 2a (PBP2a) protein of S. aureus and MRSA was evaluated by a Western blot assay. The results emphasized the fabrication of GA nanoparticles in spherical shapes with a diameter in the range of 40–50 nm. The data show that GA nanoparticles exhibit great bactericidal effectiveness against S. aureus and MRSA. The treatment with GA-NPs remarkably reduces the expression levels of the mecA, mecR1, blaR1, and blaZ genes. PBP2a expression in MRSA was significantly reduced after treatment with GA-NPs. Overall, this study demonstrates that glycyrrhizic acid nanoparticles have potent antibacterial activity, particularly against MRSA. This research elucidates the inhibition mechanism of glycyrrhizic acid, which involves the suppressing of PBP2a expression. This work emphasizes the importance of utilizing plant nanoparticles as effective antimicrobial agents against a broad spectrum of bacteria. [ABSTRACT FROM AUTHOR]

The diterpene 7α-acetoxy-6β-hydroxyroyleanone isolated from Plectranthus grandidentatus demonstrates promising antibacterial, anti-inflammatory and anticancer properties. However, its bioactivity may be enhanced via strategic structural modifications of such natural products through semisynthesis. The anticancer potential of 7α-acetoxy-6β-hydroxyroyleanone and five derivatives was analyzed in silico via the prediction of chemicals absorption, distribution, metabolism, excretion, and toxicity (ADMET), quantum mechanical calculations, molecular docking and molecular dynamic simulation. The protein targets included regulators of apoptosis and cell proliferation. Additionally, network pharmacology was used to identify potential targets and signaling pathways. Derivatives 7α-acetoxy-6β-hydroxy-12-O-(2-fluoryl)royleanone and 7α-acetoxy-6β-(4-fluoro)benzoxy-12-O-(4-fluoro)benzoylroyleanone achieved high predicted binding affinities towards their respective protein panels, with stable molecular dynamics trajectories. Both compounds demonstrated favorable ADMET parameters and toxicity profiles. Their stability and reactivity were confirmed via geometry optimization. Network analysis revealed their involvement in cancer-related pathways. Our findings justify the inclusion of 7α-acetoxy-6β-hydroxy-12-O-(2-fluoryl)royleanone and 7α-acetoxy-6β-(4-fluoro)benzoxy-12-O-(4-fluoro)benzoylroyleanone in in vitro analyses as prospective anticancer agents. Our binding mode analysis and stability simulations indicate their potential as selective inhibitors. The data will guide studies into their structure optimization, enhancing efficacy and drug-likeness. [ABSTRACT FROM AUTHOR]

Aim: suppression of methylation inhibitors (epigenetic genes) in hepatocarcinogenesis induced by diethylnitrosamine using glycyrrhetinic acid. Method: In the current work, we investigated the effect of sole GA combined with different agents such as doxorubicin (DOX) or probiotic bacteria (Lactobacillus rhamanosus) against hepatocarcinogenesis induced by diethylnitrosamine to improve efficiency. The genomic DNA was isolated from rats' liver tissues to evaluate either methylation-sensitive or methylationdependent resection enzymes. The methylation activity of the targeting genes DLC-1, TET-1, NF-kB, and STAT-3 was examined using specific primers and cleaved DNA products. Furthermore, flow cytometry was used to determine the protein expression profiles of DLC-1 and TET-1 in treated rats' liver tissue. Results: Our results demonstrated the activity of GA to reduce the methylation activity in TET-1 and DLC-1 by 33.6% and 78%, respectively. As compared with the positive control. Furthermore, the association of GA with DOX avoided the methylation activity by 88% and 91% for TET-1 and DLC-1, respectively, as compared with the positive control. Similarly, the combined use of GA with probiotics suppressed the methylation activity in the TET-1 and DLC-1 genes by 75% and 81% for TET-1 and DLC-1, respectively. Also, GA and its combination with bacteria attenuated the adverse effect in hepatocarcinogenesis rats by altering potential methylomic genes such as NF-kb and STAT3 genes by 76% and 83%, respectively. Conclusion: GA has an ameliorative effect against methylation inhibitors in hepatocellular carcinoma (HCC) by decreasing the methylation activity genes. [ABSTRACT FROM AUTHOR]

Simple Summary: Euphorbiaceae is a large family of flowering plants that includes a wide spectrum of useful plants, from edible plants to toxic and medicinal plants. They are cosmopolitan plants that have very different shapes, from little herbaceous plants to big trees and cactus-like forms. This review article focuses on the potential anticancer activity of extracts, isolated compounds, and nanoparticles generated from the plants of the Euphobiaceae family based on in vitro and in vivo experiments. Possible mechanisms of action are also discussed. The number of cancer cases will reach 24 million in 2040, according to the International Agency for Research on Cancer. Current treatments for cancer are not effective and selective for most patients; for this reason, new anticancer drugs need to be developed and researched enough. There are potentially useful drugs for cancer isolated from plants that are being used in the clinic. Available information about phytochemistry, traditional uses, in vitro and in vivo experiments with plants, and pure compounds isolated from the Euphorbiaceae family indicates that this family of plants has the potential to develop anticancer drugs. This review examines selected species from the Euphorbiaceae family and their bioactive compounds that could have potential against different types of cancer cells. It reviews the activity of crude extracts, isolated compounds, and nanoparticles and the potential underlying mechanisms of action. [ABSTRACT FROM AUTHOR]

ABSTRACT Background: Abietane diterpenes have attracted much attention because they display a wide range of biological activities, including antitumor activities. These compounds are the most diverse of the diterpenoids isolated [...]

This document is an editorial published in Frontiers in Pharmacology titled "Women in experimental pharmacology and drug discovery 2023." The editorial highlights the achievements of women scientists in the field of pharmacology and drug discovery, showcasing their diverse and impactful research endeavors. It also discusses the importance of promoting gender equality in science and encouraging girls and women to pursue careers in STEM fields. The editorial features several key studies conducted by women scientists, covering topics such as hepatoprotective potential, sustainable ingredients, antioxidative components, and the role of certain molecules in disease treatment. The document emphasizes the need to support and celebrate the work of women scientists to foster a more inclusive and innovative scientific community. [Extracted from the article]