A semi-rationally engineered P450 disrupts the native radical transfer pathway to achieve highly selective B-ring C7β functionalization of pentacyclic triterpenoids. The installed C7β-OH handle supports chemoenzymatic synthesis of previously inaccessible B-ring-modified PT derivatives with potent antitumor activity, demonstrating the utility of enzyme engineering for the late-stage diversification of complex natural products. ABSTRACT Pentacyclic triterpenoids (PTs) feature a steroid-like privi…

Ganoderma adspersum is a white-rot wood-degrading basidiomycete of ecological, biotechnological and medicinal interest. In addition to its role in lignin degradation, it produces bioactive metabolites...

Almond hulls are a rich source of triterpenoids (betulinic, urosolic, and oleanolic acids), flavonols, phenolics, catechins, and other polyphenolic compounds, some of which have antibacterial and anti...

Targeting retinoic acid-related orphan receptor γ (RORγ) with inverse agonists presents a promising therapeutic strategy for treating autoimmune diseases, including psoriasis, rheumatoid arthritis, an

Ganoderic acids (GAs) are high-value lanostane-type triterpenoids derived from Ganoderma lucidum (G. lucidum) with broad applications in functional foods and nutraceuticals, yet their low natural abundance limits industrial production. In this study, an integrated life-cycle multiomics analysis combining metabolomics, transcriptomics, and proteomics was conducted across six developmental stages in four G. lucidum strains to elucidate regulatory mechanisms governing GA biosynthesis. Weighted gene coexpression network analysis identified candidate cytochrome P450 enzymes and transcription factors associated with GA accumulation. A Zn2Cys6-type transcription factor, Zn2Cys6_61, was identified as a central regulator and functionally validated through overexpression and RNA interference. Genetic manipulation of Zn2Cys6_61 expression significantly altered GA levels, with overexpression markedly enhancing GA accumulation. Further analysis demonstrated that Zn2Cys6_61 directly binds to and activates the promoter of squalene synthase, a key enzyme in triterpenoid backbone biosynthesis. Together, these findings identify Zn2Cys6_61 as an effective engineering target and provide a transcription factor-based strategy for improving GA production in medicinal mushrooms.

Four new dichapetalin hybrid triterpenoids, namely phyllanfranchins A–D (1–4), were obtained from the aerial part of Phyllanthus franchetianus H. L'ev…

IntroductionCucurbitacin, a class of triterpenoid compounds isolated from Pedicellus Melo, possesses various biological activities and is the primary active ...

Guided by the MS/MS metabolome-based molecular networking, 50 compounds, including 18 new triterpenoid metabolites (ganoleucocontins A–R, 1–18), were obtained from Ganoderma leucocontextum. The chemical structures of these novel metabolites were determined based on comprehensive spectroscopic methods and chemical derivation. Compounds 12–15, 17, and 18 represent a new class of triterpenoid dimers linked by 3-hydroxy-3-methylglutaryl (HMG), which were reported for the first time. The cytotoxicity was assessed in Huh7 cells, revealing IC50 values of 24.39–47.29 μM for new compounds 10, 13, 15, 16, and 18. Further studies on the anticancer properties demonstrated that compounds 10 and 15 inhibited tumor cell growth by promoting apoptosis and disrupting the cell cycle. Meanwhile, the mass spectrometry imaging experiments showed that triterpenoids were predominantly distributed at the edge of the upper shell layer in both the cap and stipe, supporting the peels of G. leucocontexum as a main distribution of Ganoderma triterpenoids.

Isolation of the effective anti-inflammatory fraction of Salvia rosmarinus (rosemary) was guided by its anti-inflammatory activity in lipopolysaccharide-stimulated RAW264.7 cells, as an in vitro inflammation model, and its chemical components were systematically characterized by UPLC-Orbitrap MS/MS coupled with GNPS. Eighty-three triterpenoids were identified, among which 51 were separated and elucidated, including 10 new compounds and six triterpenoids that exhibited significant anti-inflammatory activity. The mass spectrometry fragmentation pathways of the five types of compounds were analyzed and their anti-inflammatory structure–activity relationship of the separated compounds was explored. The results indicate that the anti-inflammatory activity of rosemary is not mainly exerted by a few main components, such as ursolic acid and oleanolic acid, as previously reported, but is the result of the synergistic effect of many triterpenoids. The findings of the study provide a scientific basis for the development of rosemary anti-inflammatory functional foods.

The simultaneous determination of pentacyclic triterpenoids, which are secondary metabolites in plants, is difficult because of the similarity in stru…

Abstract. Centella asiatica is renowned for its medicinal properties, particularly due to its triterpenoid saponins, such as asiaticoside and madecassoside

Calendula, a plant used in traditional medicine for centuries, helps reduce inflammation. Here the authors identify natural compounds that are key to its anti-inflammatory activity, revealing how…

Abstract. Cyclic terpenoids are a class of lipid compounds containing immense structural and functional diversity, with many cyclic triterpenoids acting as