Fungi have been recognised as a prolific source of structurally unique secondary metabolites with promising pharmacological properties. This review comprehensively summarises the chemical architectures, bioactivities, and research strategies for new fungal-derived natural products, focusing on representative studies published in 2024. A total of 907 novel fungal-derived compounds are systematically cataloged (isomers are also contained in the total count), including 284 polyketides, 362 terpenoids, 28 steroids, 108 alkaloids, 75 peptides, and 50 glycosides, while highlighting cutting-edge methodologies such as metabolomics-guided discovery platforms and biosynthetic pathway engineering. By establishing connections between chemical novelty and therapeutic value, this review not only provides strategic guidance for fungal chemical diversity exploration but also illuminates their transformative potential in overcoming drug discovery bottlenecks.

Three new racemic bianthrones, including two pairs of (±)-penithrones A (1) and B (2), and a chlorinated derivative (±)-penithrone C (3), along with their biogenetic precursors (4–6) were discovered from the culture extract of the mangrove-derived fungus Penicillium hispanicum LA032 using HSQC-based DeepSAT. The structural elucidation of these new compounds was achieved through comprehensive integration of NMR spectroscopy, high-resolution mass spectrometry (HRESIMS), and NMR calculations with CP3 analysis. Compounds 1 and 2 exhibited significant cytotoxic activity against HeLa, HCT116, and MCF-7 cancer cell lines, with IC₅₀ values ranging from 5.09 ± 0.65 to 9.47 ± 0.22 μmol/L. In addition, network pharmacology analysis and molecular docking studies revealed Mitogen-Activated Protein Kinase 10 (MAPK10) as a potential target of 1 for its anticancer effect.

Two new pairs of chlorinated orsellinic aldehyde enantiomers acresorcinols A and B (1a/1b and 2a/2b), and three orsellinic aldehydes, acresorcinols C−E (3−5) were discovered from the extract of the deep-sea-derived fungus Acremonium sclerotigenum LW14. Their structures, including absolute configurations, were experimentally elucidated by spectroscopic analysis, NMR calculations with DP4+ probability analysis, and ECD calculations. Compounds 1 and 2 exemplify the first reported chlorinated orsellinic aldehydes, characterised by a distinctive 6/5−5 tricyclic core structure with a bridged framework. Acresorcinol C (3) was a rare carbon-bridged resorcinol dimer via a methylene bridge. The bioassay results showed that all compounds exhibited antifungal activities against Cryptococcus gattii 3271G1 at 32 μg/mL. Compounds 1−3 showed antifungal effects against C. gattii 3271G1, displaying MIC values of 8, 16, and 16 µg/mL, respectively.

Fungi have been identified as a prolific source of structurally unique secondary metabolites, many of which display promising biological and pharmacological properties. This review provides an overview of the structures of new natural products derived from fungi and their biological activities along with the research strategies, which focuses on literature published in the representative journals in 2023. In this review, a total of 553 natural products including 219 polyketides, 145 terpenoids, 35 steroids, 106 alkaloids, and 48 peptides are presented. By summarising the latest findings, this review aims to provide a guide and inspire further innovation in the fields of the discovery of fungal natural products and pharmaceutical development.

The plant endophytes, Pestalotiopsis spp., are prolific producers of bioactive secondary metabolites. Chemical studies on the fungus, Pestalotiopsis fici, have provided over 70 new natural products from different biosynthetic routes. Some metabolites have shown biological activities, including cytotoxic, antimicrobial and anti-HIV effects. This review covers the structure, bioactivities and putative biosynthetic pathways of selected metabolites published by us over the past three years.