In silico approaches for developing sesquiterpene derivatives as antagonists of human nicotinic acetylcholine receptors (nAChRs) for nicotine addiction treatment.

Cinnamomum, a genus within the Lauraceae family, has gained global recognition due to its wide-ranging utility. Extensive research has been dedicated to exploring its phytochemical composition and pharmacological effects. Notably, the uniqueness of Cinnamomum lies in its terpenoid content, characterized by distinctive structures and significant biological implications.

Secondary metabolites of Alternaria alternate appraisal of their SARS-CoV-2 inhibitory and anti-inflammatory potentials.

This study identifies the secondary metabolites from Alternaria alternate and evaluates their ACE-2: Spike RBD (SARS-CoV-2) inhibitory activity confirmed via immunoblotting in human lung microvascular endothelial cells. In addition, their in vitro anti-inflammatory potential was assessed using a cell-based assay in LPS-treated RAW 264.7 macrophage cells.

The Cyclin-Dependent Kinase 8 Inhibitor E966-0530-45418 Attenuates Pulmonary Fibrosis and .

Pulmonary fibrosis (PF) is a high-mortality lung disease with limited treatment options, highlighting the need for new therapies. Cyclin-dependent kinase 8 (CDK8) is a promising target due to its role in regulating transcription via the TGF-β/Smad pathway, though CDK8 inhibitors have not been thoroughly studied for PF. This study aims to evaluate the potential of E966-0530-45418, a novel CDK8 inhibitor, in mitigating PF progression and explores its underlying mechanisms.

Antibiotic candidates for Gram-positive bacterial infections induce multidrug resistance.

Several antibiotic candidates are in development against Gram-positive bacterial pathogens, but their long-term utility is unclear. To investigate this issue, we studied the laboratory evolution of resistance to antibiotics that have not yet reached the market. We found that, with the exception of compound SCH79797, antibiotic resistance generally readily evolves in .

New Hydrogenated Phenanthrene Glycosides from the Edible Vegetable W.T.Wang with DPP-IV Inhibitory and Hepatoprotective Activity.

Based on molecular networking-guided isolation, 15 previously undescribed hydrogenated phenanthrene glycosides, including eight hexahydro-phenanthrenone glycosides, four tetrahydro-phenanthrenone glycosides, one dihydro-phenanthrenol glycoside, two dimers, and two known dihydrophenanthrene glycosides, were isolated from W.T.Wang, a popular regional edible vegetable at the northwest region of Vietnam.

Herbal nanoemulsions in cosmetic science: A comprehensive review of design, preparation, formulation, and characterization.

The rapid development of delivery systems for cosmetics has revealed two critical challenges in the field: enhancing the solubility of active ingredients and ensuring the stability of natural materials used in cosmetics. Nanoemulsion technology has emerged as an indispensable solution for addressing these challenges, not only enhancing the stability of cosmetics but also improving the solubility of pharmaceuticals and active ingredients with poor solubility. Nanoemulsion formulations have reinforced stability and amended the bioavailability of hydrophobic drugs.

Antioxidant, anti-acetylcholinesterase, and anti-amyloid-β peptide aggregations of hispolon and its analogs in vitro and improved learning and memory functions in scopolamine-induced ICR mice.

Background: Hispolon, one of bioactive phenolic compounds from a medicinal mushroom of sang-huang (Phellinus linteus) has been reported to exhibit anticancer and anti-inflammatory activities. The Alzheimer's disease (AD) is ranked one of the top ten leading causes of death worldwide. Little is known about the effects of hispolon on delaying AD progression.

Chemical characterization, neuroprotective effect, and evaluation of the petroleum ether extract of three palm tree species against glutamate-induced excitotoxicity in rats.

The burden of neurological disorders is growing substantially with limited therapeutic options, urging the consideration and assessment of alternative strategies. In this regard, we aimed to elucidate the phytochemical profile of the petroleum ether extract (PEE) of three palm tree species: Burret, H. Wendl.

Modulation of Multispecific Transporters by Extract and Its Major Phytoconstituents.

One of the major risks associated with the concomitant use of herbal products and therapeutic drugs is herb-drug interactions (HDIs). The most common mechanism leading to HDIs is the inhibition and/or induction of transport proteins and drug-metabolizing enzymes by herbal ingredients, causing changes in the pharmacokinetic disposition of the victim drug. The present study aimed to determine the potential interactions of (UT) (cat's claw), a popular herb due to its supposed health benefits.

Polyphenolic Compounds Activate SERCA1a and Attenuate Methylglyoxal- and Palmitate-Induced Impairment in Pancreatic INS-1E Beta Cells.

Sarco/endoplasmic reticulum Ca-ATPase (SERCA) is an important regulatory protein responsible for maintaining calcium homeostasis within cells. Impairment of SERCA associated with activity/expression decrease has been implicated in multiple chronic conditions, including cardiovascular diseases, diabetes, cancer, neurodegenerative diseases, and skeletal muscle pathologies. Natural polyphenols have been recognized to interact with several target proteins involving SERCA.

Aglaia elliptifolia Leaf Extract Inhibits Autophagy-Related 4B Protease and Suppresses Malignancies of Colorectal Cancer Cells.

Autophagy is a self-eating pathway for maintaining normal cellular physiology, while dysregulation of autophagy is associated with cancer progression. Autophagy-related 4B gene (ATG4B) is a cysteine protease to regulate autophagosome formation and is positively correlated with poor prognosis of colorectal cancer (CRC) patients. An increasing number of reports have implied that ATG4B might be an attractive drug target for CRC.

Phytosesquiterpene lactones deregulate mitochondrial activity and phenotypes associated with triple-negative breast cancer metastasis.

Background: Triple-negative breast cancer (TNBC) recurrence and metastasis are the major causes of failure in TNBC therapy. The difficulties in treating TNBCs may be because of increased cancer cell plasticity that involves the fine-tuning of cellular redox homeostasis, mitochondrial bioenergetics, metabolic characteristics, and the development of cancer stem cells (CSCs).

Purpose: To investigate the effects and the underlying mechanisms of the phytosesquiterpene lactone deoxyelephantopin (DET) and its semi-synthesized derivative (DETD-35) in suppressing different phenotypic TNBC cell populations that contribute to tumor metastasis.

Selenocompounds as Potent Efflux Pump Inhibitors on Gram-positive Bacteria.

In recent years, selenocompounds have gained increasing attention as potential anticancer and antibacterial agents. Several selenoderivatives have been confirmed to act as MDR efflux pump inhibitors, based on their in vitro results against the bacterial AcrAB-TolC system and the cancer MDR efflux pump P-glycoprotein. Efflux pumps can contribute directly or indirectly to the virulence of bacteria, as they can reduce the intracellular concentration of antibacterial substances by expelling them out of the cell.

The functional role of N-link glycosylation in a novel cellobiohydrolase II (LsCel6A) from a white-rot fungus Lentinus sp. WR2.

White-rot fungi produce a wide spectrum of lignocellulose-degradation enzymes, which can be used in bioenergy, bioremediation, and other industrial applications. This study identified a cellobiohydrolase II (Cel6A, GH6 cellobiohydrolase, EC 3.2.

Consumption of carotenoid-rich (Gac) aril improves glycemic control in type 2 diabetic mice partially through taste receptor type 1 mediated glucagon-like peptide 1 secretion.

Incretin-based therapies are widely used to improve glycemic control and β cell dysfunction in the treatment of type 2 diabetes. (Gac fruit), a nutritious melon cultivated in many regions, has underexplored health benefits, particular its edible aril. This study comprehensively investigates the stimulatory effect of Gac aril on glucagon-like peptide 1 (GLP-1) secretion, identifies the responsible active constituents, and explores the underlying mechanisms related to its anti-diabetic effects.

Tumor Antigen-Tethered Spiked Virus-Like- Poly(Lactic-Co-Glycolic Acid)-Nanoparticle Vaccine Enhances Antitumor Ability Through Th9 Promotion in Mice.

Purpose: Immunotherapy emerges as a promising frontier in cancer therapy and prevention. This study investigates the capacity of tumor-antigenic nanoparticles, specifically ovalbumin-tethered spiked virus-like poly(lactic-co-glycolic acid) nanoparticles (OVA-sVLNP), to effectively elicit humoral and cellular immune responses against tumors.

Methods: OVA-sVLNP were synthesized through thiol-maleimide crosslinking using a single emulsion method.

Correction: Agbadua et al. Oxidized Resveratrol Metabolites as Potent Antioxidants and Xanthine Oxidase Inhibitors. 2022, , 1832.

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Exploring the Link between Xerostomia and Oral Health in Mental Illness: Insights from Autism Spectrum Disorder, Depression, Bipolar Disorder, and Schizophrenia.

Background: The relationship between mental disorders and oral health is complex, involving behavioral, biological, and psychosocial factors. This review aims to investigate the impact of mental disorders, including autism spectrum disorder (ASD), depression, bipolar disorder, and schizophrenia, on oral health outcomes.

Methods: A comprehensive review of existing literature was conducted to analyze the oral health outcomes associated with each mental disorder.

Spatheliachromen mitigates methylglyoxal-induced myotube atrophy by activating Nrf2, inhibiting ubiquitin-mediated protein degradation, and restoring mitochondrial function.

Background: Methylglyoxal (MGO) is a potent precursor of glycative stress that leads to oxidative stress and muscle atrophy in diabetes. Spatheliachromen (FPATM-20), derived from Ficus pumila var. awkeotsang, exhibited potential antioxidant activity.

Combined HDAC8 and checkpoint kinase inhibition induces tumor-selective synthetic lethality in preclinical models.

The elevated level of replication stress is an intrinsic characteristic of cancer cells. Targeting the mechanisms that maintain genome stability to further increase replication stress and thus induce severe genome instability has become a promising approach for cancer treatment. Here, we identify histone deacetylase 8 (HDAC8) as a drug target whose inactivation synergized with the inhibition of checkpoint kinases to elicit substantial replication stress and compromise genome integrity selectively in cancer cells.

Semisynthetic Ecdysteroid Cinnamate Esters and -Butyl Oxime Ether Derivatives with Trypanocidal Activity.

The parasite is the causative agent of Chagas disease, a neglected tropical disease that affects the lives of millions of indigenous people in Latin America. As medications to treat Chagas disease are limited to the application of benznidazole and nifurtimox, which are not ideal treatments for the chronic stage of the disease, the search for new antichagasic drug candidates is an important need. Ecdysone has previously been shown to interfere with the life cycle of .

Phytochemical and pharmacological investigation of the non-volatile compounds of Lepidium cartilagineum (J. C. Mayer) Thell. and determination of the essential oil composition of its flowers and fruits.

Eighteen compounds, among them phenylpropanoids (1-2), neolignans (3-9), a megastigmane (10), a phenyl glucoside (11), flavonoids (12-14), and N-containing compounds (15-18) were isolated from the methanolic extract of the whole plant of L. cartilagineum. The structures of the compounds were determined by NMR and MS measurements.

Synthesis and biological evaluation of -phenyl phenylhydroxamic acids containing phenothiazine with improved selectivity for class IIa histone deacetylases.

Class IIa histone deacetylases (HDACs) have been linked to tumorigenesis in various cancers. Previously, we designed phenylhydroxamic acid as a potent class IIa HDAC inhibitor. However, it also unselectively inhibited class I and class IIb HDACs.

Dynamic changes in the metabolome and microbiome during Citrus depressa Hayata liquid fermentation.

Citri Reticulatae Pericarpium (CRP) is a common traditional Chinese herbal medicine, valued for its multi-bioactivity. However, its processing time, environment, and microorganisms all affect its quality and bioactivity. To address this, the study replaced solid-state fermentation with liquid fermentation using microorganisms and isolated Bacillus amyloliquefaciens, respectively.