The usnic acid derivative peziculone targets cell walls of Gram-positive bacteria revealed by high-throughput CRISPRi-seq analysis.

Usnic acid, a representative dibenzofuran metabolite, is known to have antimicrobial properties. However, despite considerable interest as an antimicrobial agent, the mechanism by which usnic acid and its derivatives exert their action is not fully characterized. This article describes the synthesis of peziculone, a 5:1 equilibrium mixture of two inseparable usnic acid derivatives: peziculone A and peziculone B.

Construction of model animals to explore intestinal microbiome for detection of breast cancer.

Breast cancer ranks first among female cancers and has become a major public health problem in the current society. More studies indicated that these cancers are related to the change in the gut microbiome that can cause metabolic and immune system disorders in the body. However, there are few studies on the changes in gut microbiome caused by the onset of breast cancer, and the relationship between breast cancer and gut microbiome needs to be further clarified.

The Effect of Cyclosporin A on and the Possible Mechanisms Involved.

is one of the major pathogenic fungi causing postharvest grape decay. The development of antifungal agents is beneficial to reduce the loss of grapes during storage. The aim of this study was to investigate the antifungal mechanism of cyclosporin A (CsA).

Antifungal Mechanism of MTE-1, a Novel Oligosaccharide Ester, against .

is a pathogenic fungus that causes false smut disease in rice during the flowering stage through stamen filaments. Currently, there is a need to develop safe and effective antifungal agents for the control of this disease. In our preliminary experiments, we found that MTE-1, a new trisaccharide ester, exhibits significant inhibitory activity against .

Acuminatums E and F, two new cyclic lipopeptides from HU0053 and their antifungal activity.

Two new cyclic lipopeptides, acuminatums E () and F (), together with four known cyclic lipopeptides, acuminatums A-D (-) were isolated from the corn culture of endophytic HU0053. Their structures were elucidated by spectroscopic and advanced Marfey's amino acid analysis. All compounds were found to exhibit antifungal activities against .

A Combined Analysis of Transcriptome and Proteome Reveals the Inhibitory Mechanism of a Novel Oligosaccharide Ester against .

Blue mold caused by is one of the most serious postharvest diseases of citrus fruit. The aim of this study was to investigate the inhibitory effect of a novel oligosaccharide ester, 6---L-mannopyranosyl-3--(2-methylbutanoyl)-4--(8-methyldecanoyl)-2--(4-methyl-hexanoyl) trehalose (MTE-1), against . Scanning electron microscopy (SEM) and transmission electron microscopy (TEM), along with transcriptome and proteome analysis also, were conducted to illuminate the underlying mechanism.

Genomic landscape of a relict fir-associated fungus reveals rapid convergent adaptation towards endophytism.

Comparative and pan-genomic analyses of the endophytic fungus Pezicula neosporulosa (Helotiales, Ascomycota) from needles of the relict fir, Abies beshanzuensis, showed expansions of carbohydrate metabolism and secondary metabolite biosynthetic genes characteristic for unrelated plant-beneficial helotialean, such as dark septate endophytes and ericoid mycorrhizal fungi. The current species within the relatively young Pliocene genus Pezicula are predominantly saprotrophic, while P. neosporulosa lacks such features.

Radicicol, a Novel Lead Compound against the Migratory-Stage Schistosomula of .

Schistosomiasis poses a serious threat to human health and remains a major tropical and parasitic disease in more than 70 countries. Praziquantel (PZQ) has been the primary treatment for schistosomiasis for nearly 4 decades. However, its efficacy against migratory-stage schistosomula is limited.

Dihydrochalcones from the leaves of .

Three new phlorizin derivatives, 6"--vanilloylphlorizin (), 6"--(4-hydroxybenzoyl)phlorizin (), 6"--feruloylphlorizin (), along with four known dihydrochalcones, phlorizin (), 3-hydroxyphlorizin, trilobatin, and 6"--acetylphlorizin were isolated from the leaves of . Their structures were established by analysis of extensive spectroscopic data. The new compounds were shown to be non-cytotoxic when tested against A549, HeLa, HepG2, and MCF-7 cell lines.

Bioactive Polyhydroxanthones from .

Eight new polyhydroxanthones, penicixanthones A-H (-), including four monomers (-) and four dimers (-), were isolated from solid cultures of SC0070. Their structures were elucidated by extensive spectroscopic analysis, X-ray single-crystal diffraction, and theoretical computations of ECD spectra. Penicixanthone B () has a hexahydroxanthone structure featuring an unusual oxygen bridge between C-6 and C-8a.

Streptovertimycins A-H, new fasamycin-type antibiotics produced by a soil-derived Streptomyces morookaense strain.

Eight new fasamycin-type polyketides, streptovertimycins A-H (1-8), were isolated from soil-derived Streptomyces morookaense SC1169 cultivated on wheat grains. Their structures were established by extensive spectroscopic analysis and theoretical computations of ECD spectra. Compounds 1-8 have a fasamycin-type pentacyclic structure featuring a 15-O-methyl group.

Colletotryptins A-F, new dimeric tryptophol derivatives from the endophytic fungus Colletotrichum sp. SC1355.

Seven new dimeric tryptophol-related alkaloids (1-4, 5a, 5b, and 6) were isolated from solid cultures of the endophytic fungus Colletotrichum sp. SC1355. The structures and absolute configurations of these compounds were determined by NMR spectroscopic analyses in combination with quantum chemical calculations of NMR (GIAO) shifts and ECD spectra.

Dinghupeptins A-D, Chymotrypsin Inhibitory Cyclodepsipeptides Produced by a Soil-Derived Streptomyces.

Four new cyclodepsipeptides, dinghupeptins A-D (1-4), possessing a rare N-(2-hydroxylethyl)glutamine moiety, were isolated from cultures of the soil-derived Streptomyces sp. SC0581. Their structures were elucidated by spectroscopic and advanced Marfey's amino acid analysis, and their 3D structures were established by theoretical conformational analysis.

Acremotins A-D, peptaibiotics produced by the soil-derived fungus Acremonium persicinum SC0105.

Four new peptaibiotics, acremotins A-D (1-4) featuring three α,α-dialkylated amino acid-imino acid motifs and an unreduced C-terminal residue, along with the known peptaibiotic XR586 (5) were isolated from the solid cultures of the soil-derived fungus Acremonium persicinum SC0105. Their primary structures were characterized by detailed analysis of the HRESIMS/MS fragmentation pattern combined with comprehensive interpretation of the 1D and 2D NMR spectroscopic data. The absolute configurations of amino acid residues were determined by the advanced Marfey's method.

A novel icariin type flavonoid from .

A novel icariin type flavonoid glycoside with a malonaldehydic acid intramolecular ester and two known flavonoid glycosides were isolated from . Their structures were elucidated on the basis of spectroscopic analysis and comparison of their data to the values reported in the literatures. The anti-inflammatory activities of these compounds icariin 3'''--malonaldehydic acid intramolecular 1'''', 2''' ester (1), icariin (2) and epimedin C (3) were tested.

Antifungal and Cytotoxic β-Resorcylic Acid Lactones from a Paecilomyces Species.

Eight new β-resorcylic acid lactones (RALs), including the hypothemycin-type compounds paecilomycins N-P (1-3) and the radicicol-type metabolites dechloropochonin I (4), monocillins VI (5) and VII (6), 4'-hydroxymonocillin IV (7), and 4'-methoxymonocillin IV (8), along with nine known RALs (9-17), were isolated from the cultures of Paecilomyces sp. SC0924. Compounds 1 and 2 feature a novel 6/11/5 ring system, and 3 is the first 5'-keto RAL.

Anti-inflammatory neolignans from Epimedium pseudowushanese.

One new 8-O-4' neolignan has been isolated from Epimedium pseudowushanese B. L. Guo, together with nine other known neolignans.

Bioactive Pentacyclic Triterpenoids from the Leaves of Cleistocalyx operculatus.

Thirteen new pentacyclic triterpenoids, cleistocalyxic acids A-K (1, 2, 4, 5, and 7-13) and cleistocalyxolides A (3) and B (6), and 15 known analogues (14-28), based on taraxastane, oleanane, ursane, multiflorane, and lupane skeletons, were isolated from the leaves of Cleistocalyx operculatus. The structures of 1-13 were elucidated by analysis of their spectroscopic data and ECD/TDDFT computations. Cleistocalyxolide A (3), presumed to be derived from the known taraxastane-type compound 14, has a rare rearranged triterpenoid backbone.

Novel synthesized 2, 4-DAPG analogues: antifungal activity, mechanism and toxicology.

2, 4-Diacetylphloroglucinol (2,4-DAPG), a natural phenolic compound, has been investigated in light of its biological activities against plant pathogens. To improve its potential application, fourteen 2,4-DAPG analogous were synthesized through the Friedel-Crafts reaction using acyl chlorides and phloroglucinol. Of the 2,4-DAPG derivatives, MP4 exhibited much higher antifungal activity against Penicillium digitatum and P.

Bisacremines E-G, Three Polycyclic Dimeric Acremines Produced by Acremonium persicinum SC0105.

Three dimeric acremines, bisacremines E-G (1-3), with an unusual carbon skeleton were isolated from cultures of the soil-derived fungus Acremonium persicinum SC0105. Their structures were elucidated by spectroscopic analysis, X-ray diffraction, and ECD/TDDFT computations. Compound 3 exhibited inhibitory effects on the production of TNF-α, IL-6, and NO in LPS-stimulated macrophages.

Bisacremines A-D, Dimeric Acremines Produced by a Soil-Derived Acremonium persicinum Strain.

Four dimeric acremines, bisacremines A-D (1-4), with a novel carbon skeleton and a new monomer, acremine T (5), were obtained from cultures of the soil-derived fungus Acremonium persicinum SC0105. Their structures were characterized by analysis of spectroscopic data, ECD/TDDFT computations, and X-ray diffraction. Compounds 1 and 2 exhibited weak cytotoxicity against HeLa cells, and 2 also showed modest activity against A549 and HepG2 cells.

Bioactive Polycyclic Tetramate Macrolactams from Lysobacter enzymogenes and Their Absolute Configurations by Theoretical ECD Calculations.

Two new polycyclic tetramate macrolactams, lysobacteramides A (1) and B (2), together with HSAF (heat-stable antifungal factor, 3), 3-dehydroxy HSAF (4), and alteramide A (5) were isolated from a culture of Lysobacter enzymogenes C3 in nutrient yeast glycerol medium. Their structures were determined by MS and extensive NMR analysis. The absolute configurations of 1-5 were assigned by theoretical calculations of their ECD spectra.

Penicillitone, a potent in vitro anti-inflammatory and cytotoxic rearranged sterol with an unusual tetracycle core produced by Penicillium purpurogenum.

A rearranged sterol with an unusual tetracycle core skeleton, penicillitone (1), and a new sterol, penicillisterol (2), were obtained from the culture of the fungus Penicillium purpurogenum SC0070. Their structures were characterized by spectroscopic analysis, DFT/TDDFT compuations, and X-ray diffraction. Compound 1 demonstrated potent inhibitory effects on tumor cell growth and key pro-inflammatory cytokine production in macrophages.

Anti-inflammatory cyclopeptides from exocarps of sugar-apples.

Two new cyclic peptides, fanlizhicyclopeptide A, cyclo(Pro(1)-Pro(2)-Tyr(3)-Leu(4)-Pro(5)-Gly(6)-Val(7)) (1), and fanlizhicyclopeptide B, cyclo(Pro(1)-Ile(2)-Tyr(3)-Ala(4)-Gly(5)) (2), were isolated along with six known kaurane diterpenoids and a known clovane sesquiterpene from the exocarps of sugar-apples, the fruit of Annona squamosa. Their structures were elucidated by ESI MS/MS experiments, 1D and 2D NMR data and chemical degradation. In the anti-inflammatory assay, both 1 and 2 showed in vitro inhibitory effects on the production of pro-inflammatory cytokines, TNF-α and IL-6, in LPS-stimulated RAW 264.