Steroids, peniciversiols and aspergilosidols from endophytic fungus Aspergillus sp. TZS-Y4.

Endophytic fungi have emerged as a crucial resource for medicinal drug development. The genus Aspergillus, in particular, has yielded diverse bioactive secondary metabolites. In this study, we isolated nine steroids, five peniciversiols, and two aspergilosidols from the endophytic fungus Aspergillus sp.

Six new prenylated flavonoids from Dodonaea viscosa with anti-Zika virus activity.

Six new prenylated flavonoids, named visconaeas A-F (1-6), and eleven known isopentenyl flavonoids (7-17) were isolated from Dodonaea viscosa (L.) Jacq. The structures of the separated compounds were determined through comprehensive spectral analysis and quantum chemical calculations.

Two new oleanane triterpenes from .

Two new triterpenes mayteneri A (), mayteneri B (), and seven known compounds () were isolated from stems of Loes. The chemical structures of compounds and were established by 1D, 2D NMR, HRESIMS analysis, and calculating electronic circular dichroism (ECD). The structures of known compounds - were determined by comparison of their spectral with those reported.

Three new lanostane triterpenoids and two new amides from sp. with NLRP3 inflammasome inhibitory activity.

Three new lanostane triterpenoids () along with two new amides fatty compounds () were isolated from the ethyl acetate extract of a culture of the endophytic fungus gx-2. Their structures were identified by 1D and 2D NMR spectral data and HRESIMS. Compounds were evaluated for their anti-inflammatory and tyrosinase inhibition activities.

Nudifloids A-N, structurally diverse 3,4-seco-labdane diterpenoids from Callicarpa nudiflora with inflammatory inhibitory activity.

Fourteen undescribed seco-type diterpenoids, named nudifloids A-N, together with ten known analogs, were isolated from the leaves of Callicarpa nudiflora. Nudifloids A-N had a characteristic 3,4-seco-labdane-type diterpenoid skeleton, whereas nudifloids A-C and K-N were 3,4-seco-norditerpenoids. Nudifloid A was the first example of a 3,4-seco-12,13,14,15,16-quartnor-labdane diterpenoid, with a seven-membered lactone ring formed through esterification between C-3 and C-11.

Chemical constituents from the twigs and leaves of .

Two new compounds, including a norsesquiterpenoid, annuionone H (), and a quassinoid, picraqualide G (), along with eleven known compounds (), were isolated from the twigs and leaves of . Comprehensive spectroscopic analyses and NMR calculation with DP4+ analysis were used to identify their structures. Moreover, of all these compounds, compound showed a week inhibition rate in the anti-inflammatory screening results against mouse macrophage J774A.

Two new compounds from .

Two new compounds verboncin A () and verboncin B () and 14 known compounds ( and ) were isolated from , and these 14 compounds were first obtained from this plant. Their chemical structures were established by one and two-dimensional NMR and HRESIMS analysis and the results were compared with literature values. The absolute configuration of was determined by calculating electronic circular dichroism (ECD).

The discovery of potentially active diterpenoids to inhibit the pyroptosis from Callicarpa arborea.

Pyroptosis is a programmed-inflammatory cell death, which leads to release of inflammatory cellular contents and formation of inflammation. Uncontrollable pyroptosis can result in serious immune diseases, such as cytokine release syndrome (CRS), sepsis, disseminated intravascular coagulation (DIC), and acute organ damage, including acute respiratory distress syndrome (ARDS) and acute kidney injury (AKI). Members of the Callicarpa genus are significant raw materials for traditional Chinese medicine, widely used for analgesia, hemostasis, and anti-inflammation.

Design, synthesis and anti-breast cancer evaluation of biaryl pyridine analogues as potent RSK inhibitors.

In order to discover and develop the new RSK kinase inhibitor, 50 pyridyl biaryl derivatives were designed and synthesized with LJH685 as the lead compound and their anti-tumor ability was tested. The results showed that the ability of 7d compound to inhibit the phosphorylation of YB-1 was comparable to that of LJH685. Among them, after preliminary screening, compound 7d showed good activity in inhibiting cell proliferation.

Spiroarborin, an -Clerodane Homodimer from as an Inhibitor of the Eleven-Nineteen Leukemia (ENL) Protein by Targeting the YEATS Domain.

A spiro -clerodane homodimer with a rare 6/6/6/6/6-fused pentacyclic scaffold, spiroarborin (), together with four new monomeric analogues (-), were isolated from . Their structures were elucidated by comprehensive spectroscopic data analysis, quantum-chemical calculations, and X-ray diffraction. A plausible biosynthetic pathway of was proposed, and a biomimetic synthesis of its derivative was accomplished.

Optimized Expression of Recombinant Human NIMA-related Kinase 7 (NEK7) with A Higher Purity in Escherichia coli.

Background: NIMA (never in mitosis, gene A) serine/threonine kinase 7 (NEK7) is a regulator of mitosis spindle in mammals and is considered as a drug target of inflammasome related inflammatory diseases. However, most commercially available or reported recombinant NEK7 proteins are either inactive or have low purity. These shortcomings limit the pharmacological studies and development of NEK7 inhibitors.