Exploring Phage Peptide Scaffolds: Tyrosinase-Mediated Cyclization for Selective Generation of Bioactive Cyclic Peptides.

Phage display is an ideal platform for selecting peptide hits and offers a diverse array of cyclic binders with high affinity. While many recently developed phage display platforms incorporate chemical strategies, the vast majority of these are detrimental to the phage life cycle due to cross-reactivity with the capsid protein. In contrast, enzyme catalysis, which combines high efficiency and biocompatibility, offers a promising approach for phage-based cyclic peptide display.

UPLC-Q-TOF-MS/MS driven quality characterization of market-dominant Huajiao cultivars: Varietal heterogeneity of amide compounds and drying process response pattern.

As a cornerstone of Chinese culinary and medicinal heritage, Huajiao owes its multifaceted bioactivities predominantly to amide compounds. However, the intricate interplay between cultivar-specific amide profiles and processing-induced metabolic shifts remains poorly characterized. This study employed UPLC-Q-TOF-MS/MS-based untargeted metabolomics to systematically and initially characterize the amide metabolomes of seven market-dominant Huajiao cultivars and evaluate the effects of three drying-methods on amide retention.

Ganoderma calidophilum-derived highly oxygenated lanostane triterpenoids: Multitarget neuroprotection through AMPK/mTOR/SIRT1 axis modulation and gut-brain axis crosstalk.

Ganoderma calidophilum, a medicinal fungus with dual-purpose applications, has garnered significant attention due to its diverse pharmacological activities. This study explores the neuroprotective potential of its highly oxygenated lanostane triterpenoids. Sixteen triterpenoids, including eleven previously undescribed compounds, were isolated and structurally characterized.

Polyene Cyclization/Mannich Cascade for Streamlined Construction of the A/E/F Tricyclic System of Diterpenoid Alkaloids.

The A/E/F tricyclic system characteristic of C-, C-, and denudatine-type C-diterpenoid alkaloids was constructed via a strategically designed polyene cyclization/Mannich cascade. The configurational inversion of the phenyl group at C7 successfully proceeded through a radical cascade process involving sequential 1,5-HAT and intermolecular HAT, ultimately establishing the desired tricyclic system with an β-oriented phenyl group.

Diverse abietane diterpenoids as multifunctional antimicrobial effects from Salvia castanea.

Background: Phytopathogenic fungal diseases significantly impact the quality of vegetables and fruits in agriculture. Salvia castanea, a Tibetan medicinal plant, possessed anti-inflammatory, antitumor, and antimicrobial activities. Therefore, we investigated the antimicrobial ingredients from this plant and clarified their protective and curative in plants in detail.

Total Synthesis of (+)-Ansatrienol K.

The first total synthesis of ansatrienol K, a novel trienomycin congener featuring a diene moiety within its 19-membered macrolactam ring, is reported. Key steps include two sequential palladium-catalyzed cross-coupling reactions for constructing the trisubstituted benzene ring and two distinct strategies for assembling the C6-C18 fragment. A Co(CO)-catalyzed carbonylative epoxide ring-opening provided the diene fragment, while late-stage Stewart-Grubbs catalyst-mediated diene-ene ring-closing metathesis (RCM) enabled efficient macrocyclization.

The diphenylpyrimidine derivative as a novel HDAC6 inhibitor alleviates atopic dermatitis through anti-inflammatory effects facilitated via TLR4/MAPK, STAT3 and NF-κB pathways.

Atopic dermatitis (AD) is a systemic immune disease that primarily affects infants and children, characterized by recurring severe pruritus and chronic eczema. Studies have demonstrated that histone deacetylase 6 inhibitors (HDAC6is) can exhibit anti-inflammatory activities by regulating the acetylation level of target proteins. Building on these findings, our research focused on a synthetic diphenylpyrimidine derivative, specifically 15b, which we identified as a potent HDAC6i and an effective anti-inflammatory agent.

Exploring the molecular tapestry of secondary metabolites: chemical structures, activities, and biosynthesis.

mushrooms are esteemed as a rare and highly valuable resource for both culinary and medicinal purposes. Ancient medical classics have documented their beneficial effects on conditions such as indigestion, loss of appetite, and neurological disorders. Modern phytochemical research into their secondary metabolites has led to the discovery of numerous bioactive compounds with significant biological activities.

Hypertums A-J, bioactive polycyclic polyprenylated acylphloroglucinols with diverse skeletons from Hypericum perforatum L. (St. John's wort).

Ten previously undescribed polycyclic polyprenylated acylphloroglucinols (PPAPs), hypertums A-J (1-10), together with eighteen known analogues (11-28), belonging to five subclasses of PPAPs, were isolated from the aerial parts of Hypericum perforatum L. (St. John's wort).

Cytochalasins and orsellinic acid derivatives with cytotoxicity from the soil-derived fungus Trichocladium asperum.

Four undescribed cytochalasins (1-4), three undescribed orsellinic acid derivatives (5-7) and two known metabolites including methyl lecanorate (8) and methyl orsellinate (9) were isolated from the solid-state cultivation of a soil-derived fungus Trichocladium asperum SQ2-3 collected in Qinghai-Tibet Plateau. Their structures were elucidated by analysis of NMR (1D and 2D) and mass spectrometry data. The absolute configurations of 1-7 were assigned by a combination of the modified Mosher's method, microscale derivatization and Mo(OAc)-induced circular dichroism experiment.

Naphthoquinone Derivatives from the Endophytic Fungus Induce Pancreatic Cancer Cells Apoptosis via Targeting EGFR-Mediated PI3K/Akt Pathway.

Seven new polyketide compounds, four naphthoquinone derivatives, neofusarubins A-D (, , , and ) and three graminin-like compounds, fusofuranones A-C (-), together with 14 known naphthoquinone derivatives, were isolated from the solid fermentation of , an endophytic fungus obtained from medicinal plant as tea, . The structures of new compounds were elucidated based on chemical evidence and spectral data analysis (1D and 2D-NMR, HR-ESI-MS, ECD, SC-XRD). Among the isolated compounds tested, 2-acetonyl-3-methyl-5-hydroxy-7-methoxy-naphthazarin () exhibited the most potent inhibitory activity against pancreatic cancer in PANC-1, MiaPaCa-2, and BxPC-3 cells.

Chemical structures, biological activities, and biosynthetic analysis of secondary metabolites of the Diatrypaceae family: A comprehensive review.

The family Diatrypaceae is a less well-known group within the order Xylariales (Ascomycota). Initially, the focus on its metabolites was related to the pathogenicity of one of its members, . To date, a total of 254 natural products have been identified from Diatrypaceae strains.

Evaluation of Phenazine Derivatives from the Lichen-Associated as Potent Antineuroinflammatory Agents In Vitro and In Vivo.

Eighteen nitrogen-containing compounds (-) were isolated from cultures of the lichen-associated collected from the Qinghai-Tibet Plateau, including seven phenazine derivatives with three new ones, named subphenazines A-C (-), two new furan pyrrolidones (-), and nine known alkaloids. The structures were elucidated by spectroscopic data analysis, and absolute configurations were determined by single-crystal X-ray diffraction and ECD calculations. The phenazine-type derivatives, in particular compound , exhibited significantly better antineuroinflammatory activity than other isolated compounds (-).

Ganoderic Acid A Mitigates Inflammatory Bowel Disease through Modulation of AhR Activity by Microbial Tryptophan Metabolism.

Inflammatory bowel disease (IBD), including Crohn's disease and ulcerative colitis, is a complex gastrointestinal condition influenced by genetic, microbial, and environmental factors, among which the gut microbiota plays a crucial role and has emerged as a potential therapeutic target. Ganoderic acid A (GAA), which is a lanostane triterpenoid compound derived from edible mushroom , has demonstrated the ability to modulate gut dysbiosis. Thus, we investigated the impact of GAA on IBD using a dextran sodium sulfate (DSS)-induced colitis mouse model.

A new neuroprotective candidate TJ1 targeting amyloidogenesis in 5xFAD Alzheimer's disease mice.

As one of the main pathmechanisms of Alzheimer's disease (AD), amyloid-β (Aβ) is widely considered to be the prime target for the development of AD therapy. Recently, imidazolylacetophenone oxime ethers or esters (IOEs) have shown neuroprotective effects against neuronal cells damage, suggesting their potential use in the prevention and treatment of AD. Thirty IOEs compounds from our lab in-house library were constructed and screened for the inhibitory effects on Aβ-induced cytotoxicity.

Mechanistic Insights from the Crystal Structure and Computational Analysis of the Radical SAM Deaminase DesII.

Radical S-adenosyl-L-methionine (SAM) enzymes couple the reductive cleavage of SAM to radical-mediated transformations that have proven to be quite broad in scope. DesII is one such enzyme from the biosynthetic pathway of TDP-desosamine where it catalyzes a radical-mediated deamination. Previous studies have suggested that this reaction proceeds via direct elimination of ammonia from an α-hydroxyalkyl radical or its conjugate base (i.

Three New Ionone Glycosides from Maxim.

Six ionone glycosides (- and -), including three new ones, named capitsesqsides A-C (-), together with an eudesmane sesquiterpenoid glycoside () and three known triterpenoid saponins (-) were isolated from . The structures of these compounds were determined by extensive spectroscopic techniques (MS, UV, 1D-NMR, and 2D-NMR) and comparison with data reported in the literature. The absolute configurations were determined by comparison of the experimental and theoretically calculated ECD curves and LC-MS analyses after acid hydrolysis and derivatization.

Synthesis and Antifungal Activities of Novel Griseofulvin Derivatives as Potential Anti-Phytopathogenic Fungi Agents.

The extensive and repeated application of chemical fungicides results in the rapid development of fungicide resistance. Novel antifungal pesticides are urgently required. Natural products have been considered precious sources of pesticides.

Chemical Structures, Biological Activities, and Biosynthetic Analysis of Secondary Metabolites from Mushrooms: A Review.

mushrooms are an important genus in the Agaricaceae family, belonging to the order Agaricales of the class Basidiomycota. Among them, is a common mushroom for mass consumption, which is not only nutritious but also possesses significant medicinal properties such as anticancer, antibacterial, antioxidant, and immunomodulatory properties. The rare edible mushroom, , contains unique agaricol compounds with significant anticancer activity against liver cancer.

Inubritantrimers A-D: Trimerized Sesquiterpenoid [4 + 2] Adducts Featuring a Distinctive Spiro-Polycyclic Scaffold from .

Inubritantrimer A (), a trace trimerized sesquiterpenoid [4 + 2] adduct featuring an unusual - type spiro-polycyclic scaffold, together with three new - [4 + 2] adducts, inubritantrimers B-D (-), were discovered from the flowers of . Their structures were elucidated using 1D/2D NMR, X-ray diffraction, and ECD approaches. is characterized as a novel - trimer, synthesized biogenetically from three sesquiterpenoid monomers, featuring a unique linkage of C-11/C-1', C-13/C-3' and C-13'/C-3″, C-11'/C-1″ through a two-step [4 + 2] cycloaddition process.

Natural and engineered xylosyl products from microbial source.

Glycosylation is a prevalent post-modification found in natural products and has a significant impact on the structural diversity and activity variation of natural products. Glucosylation is the most common type of glycosylation, whereas xylosylation is relatively rare. Despite their unique chemical structures and beneficial activities, xylosylated natural products from microorganisms have received little attention.

Discovery from Hypericum elatoides and synthesis of hyperelanitriles as α-aminopropionitrile-containing polycyclic polyprenylated acylphloroglucinols.

The search for lead compounds with anti-neuroinflammatory activity from structurally 'optimized' natural products is a crucial and promising strategy in the quest to discover safe and efficacious agents for treating neurodegenerative diseases. A phytochemical investigation on the aerial portions of Hypericum elatoides led to the isolation of five nitrogenous polycyclic polyprenylated acylphloroglucinols (PPAPs), hyperelanitriles A-D (1-4) and hyperelamine A (5). Their structures were determined by spectroscopic analysis, ECD and NMR calculations, and X-ray crystallography.

Design and Synthesis of a Water-Based Nanodelivery Pesticide System for Improved Efficacy and Safety.

Developing an environmentally friendly and safe nanodelivery system is crucial to improve the efficacy of pesticides and minimize environmental and health risks. However, preparing a completely water-based nanopesticide without using harmful solvents is a technical challenge. In this study, a water-based nanodelivery pesticide system was constructed to improve the efficacy and safety of Emamectin Benzoate (EB).