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Neuroprotective effect of Urolithin A via downregulating VDAC1-mediated autophagy in Alzheimer's disease.

BACKGROUND: Amyloid β (Aβ) accumulation in the brains of patients with Alzheimer's disease (AD) contributes to cognitive impairment and neuronal damage. Urolithin A (UA), a gut microbiota-derived metabolite of ellagic acid, has been reported to cross the blood-brain barrier to exert anti-inflammatory and anti-oxidation effects in the brain. However, the molecular mechanisms of UA in AD were still unclear. This study aims to explore the neuroprotective effect and mechanism of UA on APP/PS1 mice and Aβ1-42-injured N2a and PC12 cells. METHODS: In this study, Morris water maze was used to detect

Dietary supplementation of pterostilbene, a major component in small berries, prevents alcohol-induced liver injury associated with lipid accumulation and inflammation.

Pterostilbene (PTE), a natural stilbene found in small berries, exhibits multiple pharmacological activities, particularly antioxidant and anti-inflammatory activities. This study explores the dietary supplementation of PTE to ameliorate acute and chronic alcohol-associated liver disease (ALD). C57BL/6 mice were administrated with PTE and subjected to acute or chronic alcohol stimulation. They were intragastrically administered with alcohol (5 g kg-1, 3 times per 24 h) to induce acute alcohol liver injury or fed a Lieber-DeCarli liquid diet containing 5% ethanol for 4 weeks and a single binge

Phytochemical Profiling, In Vitro and In Silico Anti-Microbial and Anti-Cancer Activity Evaluations and Staph GyraseB and h-TOP-IIβ Receptor-Docking Studies of Major Constituents of Zygophyllum coccineum L. Aqueous-Ethanolic Extract and Its Subsequent Fractions: An Approach to Validate Traditional Phytomedicinal Knowledge.

Zygophyllum coccineum, an edible halophytic plant, is part of the traditional medicine chest in the Mediterranean region for symptomatic relief of diabetes, hypertension, wound healing, burns, infections, and rheumatoid arthritis pain. The current study aimed to characterize Z. coccineum phytoconstituents, and the evaluations of the anti-microbial-biofilm, and anti-cancers bioactivities of the plant's mother liquor, i.e., aqueous-ethanolic extract, and its subsequent fractions. The in silico receptors interaction feasibility of Z. coccineum major constituents with Staph GyraseB, and human topo

Resveratrol and clinical trials: the crossroad from in vitro studies to human evidence.

Resveratrol (3,5,4'-trihydroxy-trans-stilbene) is a non-flavonoid polyphenol that may be present in a limited number of foodstuffs such as grapes and red wine. Resveratrol has been reported to exert a plethora of health benefits through many different mechanisms of action. This versatility and presence in the human diet have drawn the worldwide attention of many research groups over the past twenty years, which has resulted in a huge output of in vitro and animal (preclinical) studies. In line with this expectation, many resveratrol- based nutraceuticals are consumed all over the world with qu

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… Amongst stilbenes, trans -resveratrol (3,5,4’-trihydroxy- trans -stilbene; RES) is the most relevant compound due to its well-known bioactivity. However, its presence in the human diet is limited to a few foodstuffs including grapes, red wine, peanuts and some types of berries. … Authors conclude that RES metabolism by human gut microbiota shows pronounced interindividual differences, which should be taken into account during the investigation of health-related effects of this stilbene. …

Suppression of N-nitrosomethylbenzylamine (NMBA)-induced esophageal tumorigenesis in F344 rats by resveratrol.

Resveratrol (3,5,4'-trihydroxy-trans-stilbene) is a natural product occurring in grapes and various other plants with medicinal properties associated with reduced cardiovascular disease and reduced cancer risk. To evaluate the possibility and potential mechanism(s) of which resveratrol inhibits N-nitrosomethylbenzylamine (NMBA)-induced rat esophageal tumorigenesis, 96 F344 male rats were divided into 10 groups and resveratrol (1 and 2 mg/kg) was administered orally or intraperitoneally (i.p.). In the groups in which resveratrol was administered at 2 mg/kg (orally, for 16 weeks), 1 and 2 mg/kg

Inhibition and stimulation of K+ transport across the frog erythrocyte membrane by furosemide, DIOA, DIDS and quinine.

Frog erythrocytes were incubated in iso- or hypotonic media containing 10 mmol/l Rb+ and 0.1 mmol/l ouabain and both Rb+ uptake and K+ loss were measured simultaneously. Rb+ uptake by frog red cells in iso- and hypotonic media was reduced by 30-60% in the presence of 0.01-0.1 mmol/l [(dihydroindenyl)oxy] alkanoic acid (DIOA) or 0.5-1.0 mmol/l furosemide. Furosemide inhibited K+ loss from frog erythrocytes incubated in hypotonic media but did not affect it in isotonic media. DIOA at a concentration of 0.05 mmol/l inhibited of K+ loss from frog erythrocytes in both iso- and hypotonic media. At t

Recent discovery of tyrosinase inhibitors in traditional Chinese medicines and screening methods.

ETHNOPHARMACOLOGICAL RELEVANCE: Tyrosinase, the key rate-limiting enzyme for melanogenesis, is one of the main targets for skin senescence a … inly belonging to flavonoids, lignans, terpenoids, Diels-Alder adducts, simple phenylpropanoids and stilbenes, from 61 kinds of TCMs have been reported to possess tyrosinase inhibitory activity, among which flavonoids are mainly focused on. Furthermore, on the basis of bioactive detection strategies, the screening methods for tyrosinase inhibitors have been …

Novel benzofuran/pterostilbene hybrids trigger programmed cell death and impair migration in CRC cells.

Colorectal cancer (CRC) remains one of the most prevalent and lethal malignancies worldwide, highlighting the urgent need for developing effective treatments. Molecular hybridization is a promising strategy for identifying new bioactive compounds. This study focused on designing and synthesizing a novel series of benzofuran-pterostilbene hybrid molecules. These compounds were successfully obtained, and their structures were elucidated by spectroscopic analysis. In addition, the activity of the hybrids was evaluated against colorectal adenocarcinoma cells. After the treatments, hybrids 6d and 6

Dual inhibition of ERα/NF-κB pathways coupled with sonodynamic therapy via a multifunctional AIEgen.

Here we report TBEP, a trifunctional sonosensitizer integrating aggregation-induced emission characteristics for ultrasound-triggered reactive oxygen species generation, estradiol-mediated ERα targeting, and pterostilbene-derived inflamation inhibition. This modular platform synergizes spatially precise SDT with tumor microenvironment modulation, offering a promising strategy for breast cancer therapy.

Mechanisms of resveratrol in cartilage injury repair and protection: A review.

Cartilage injury is a central pathological feature of degenerative joint diseases such as osteoarthritis. Due to its avascular, aneural, and low-cell-density nature, cartilage has a very limited capacity for self-repair. Consequently, identifying agents capable of delaying cartilage degeneration and promoting repair remains a major research focus. Resveratrol, a natural polyphenol, has garnered significant attention for its potent antioxidant, anti-inflammatory, and cytoprotective properties. Based on recent research advances, this narrative review summarizes the multifaceted protective roles

Resveratrol attenuates moxifloxacin-induced oxidative damage in the liver, kidneys, brain, and serum of Wistar rats.

ObjectiveMoxifloxacin, a widely used fluoroquinolone, has been associated with oxidative stress and tissue injury. Resveratrol may attenuate oxidative damage. This study investigated the effects of resveratrol co-administration on oxidative and apoptotic biomarkers in rats exposed to moxifloxacin.MethodsTwenty-four male Wistar albino rats were randomly assigned to three groups (n = 8 per group): (a) control; (b) moxifloxacin; and (c) moxifloxacin + resveratrol groups. Moxifloxacin was administered intraperitoneally at 50 mg/kg/day during the final 7 days of a 28-day experimental period, wherea

Pterostilbene synergizes with colistin against multidrug-resistant bacteria via iron chelation and membrane disruption, and promotes gut health restoration in weaned piglets.

The emergence of polymyxin-resistant Gram-negative pathogens has severely compromised colistin (COL) efficacy in veterinary therapy, posing critical challenges to animal health and food safety. Here, we show that pterostilbene (PTE), a dietary phenolic compound abundant in blueberries and grapes, effectively restores and enhances the antibacterial activity of COL. PTE acts synergistically with COL against multidrug-resistant strains, eliminates metabolically dormant persister cells and suppresses biofilm formation. Mechanistically, PTE chelates ferrous iron to deplete intracellular iron pools,

Effect of Topical Application of Resveratrol Loaded Chitosan Nanoparticles on Chemically Induced Epithelial Dysplasia in Hamster Pouch.

OBJECTIVES: This research aimed to investigate the topical effect of Resveratrol (RV) loaded on chitosan nanoparticles (CS-NP) on chemically induced epithelial dysplasia in the hamster buccal pouch. MATERIAL AND METHODS: 35 Syrian hamsters were used in this study; they were divided into 4 groups. Group A (n = 5) was the negative control group. 7,12-dimethylbenzo anthracene (DMBA) was applied topically for 6 weeks to induce oral epithelial dysplasia in the remaining 30 animals, then they were divided into group B (n = 10) as the positive control group, group C (n = 10) animals received CS-NP (

Resveratrol attenuates the CoCl2-induced hypoxia damage by regulation of lysine β-hydroxybutyrylation in PC12 cells.

BACKGROUND: Stroke is a cerebrovascular disease that is the main cause of death and disability worldwide. Hypoxia is a major factor that causes neuronal damage and even cellular death. However, the mechanism and therapeutic drugs for hypoxia are not completely understood. METHODS: In this study, PC12 cells (a rat adrenal pheochromocytoma cell line) were exposed to Cobalt chloride (CoCl2) to induce hypoxia. Using this cell model, the impacts of hypoxia on cell viability, proliferation, reactive oxygen species (ROS), and the levels of lysine β-hydroxybutyrylation (Kbhb) and the inflammatory sig

An update on topical therapies for psoriasis.

PURPOSE OF REVIEW: Topical therapies are a mainstay of treatment for mild psoriasis and may be a useful adjunct in treatment of moderate-to-severe psoriasis. This review summarizes recent advances in topical therapies for psoriasis and currently available treatments. RECENT FINDINGS: Topical aryl hydrocarbon receptor modulators (tapinarof) and topical phosphodiesterase-4 inhibitors (roflumilast) have been proven effective in randomized controlled trials for psoriasis. Although topical JAK inhibitors have also been studied, none are currently licensed for treatment of psoriasis. Topical cortic

Towards multicenter β-amyloid PET imaging in mouse models: A triple scanner head-to-head comparison.

AIM: β-amyloid (Aβ) small animal PET facilitates quantification of fibrillar amyloidosis in Alzheimer's disease (AD) mouse models. Thus, the methodology is receiving growing interest as a monitoring tool in preclinical drug trials. In this regard, harmonization of data from different scanners at multiple sites would allow the establishment large collaborative cohorts and may facilitate efficacy comparison of different treatments. Therefore, we objected to determine the level of agreement of Aβ-PET quantification by a head-to-head comparison of three different state-of-the-art small animal PET

Combretastatin A-4 based compounds as potential anticancer agents: A review.

The current review discusses the importance of combretastatin A-4 (CA-4) as a lead compound of microtubule targeting agents. CA-4 holds a unique place among naturally occurring compounds having cytotoxic activity. In this review an overall picture of design strategies, structure-activity relationship, synthesis, cytotoxic activity, and binding interactions of promising CA-4 analogues, are discussed and arranged chronologically from 2016 to early 2023. Also, this review emphasizes their biological activity as anticancer agents, within an overview of clinical application limitation and suggested

Design and characterization of a binary CT complex of imidazole-oxyresveratrol: exploring its pharmacological and computational aspects.

A new binary charge transfer (CT) complex between imidazole (IMZ) and oxyresveratrol (OXA) was synthesized and characterized experimentally and theoretically. The experimental work was carried out in solution and solid state in selected solvents such as chloroform (CHL), methanol (Me-OH), ethanol (Et-OH), and acetonitrile (AN). The newly synthesized CT complex (D1) has been characterized by various techniques such as UV-visible spectroscopy, FTIR, 1H-NMR, and powder-XRD. The 1:1 composition of D1 is confirmed by Jobs' method of continuous variation and spectrophotometric (at λmax 554 nm) metho

Study methodology and insights from the palovarotene clinical development program in fibrodysplasia ossificans progressiva.

BACKGROUND: The design of clinical trials in rare diseases is often complicated by a lack of real-world translational knowledge. Fibrodysplasia ossificans progressiva (FOP) is an ultra-rare genetic disorder characterized by skeletal malformations and progressive heterotopic ossification (HO). Palovarotene is a selective retinoic acid receptor gamma agonist. Here, we describe the methodology of three studies in the palovarotene clinical development program in FOP and discuss insights that could inform future research, including endpoint suitability and the impact of trial design. METHODS: PVO-

Fast and Accurate Amyloid Brain PET Quantification Without MRI Using Deep Neural Networks.

This paper proposes a novel method for automatic quantification of amyloid PET using deep learning-based spatial normalization (SN) of PET images, which does not require MRI or CT images of the same patient. The accuracy of the method was evaluated for 3 different amyloid PET radiotracers compared with MRI-parcellation-based PET quantification using FreeSurfer. Methods: A deep neural network model used for the SN of amyloid PET images was trained using 994 multicenter amyloid PET images (367 18F-flutemetamol and 627 18F-florbetaben) and the corresponding 3-dimensional MR images of subjects who