Discovery of non-retinoid compounds that suppress the pathogenic effects of misfolded rhodopsin in a mouse model of retinitis pigmentosa.

Pathogenic mutations that cause rhodopsin misfolding lead to a spectrum of currently untreatable blinding diseases collectively termed retinitis pigmentosa. Small molecules to correct rhodopsin misfolding are therefore urgently needed. In this study, we utilized virtual screening to search for drug-like molecules that bind to the orthosteric site of rod opsin and improve its folding and trafficking.

Drug Leads from Endophytic Fungi: Lessons Learned via Scaled Production.

Recently, the isolation and elucidation of a series of polyhydroxyanthraquinones were reported from an organic extract of a solid phase culture of an endophytic fungus, (strain G85). One of these compounds, -hydroxyemodin (1: ), showed promising quorum-sensing inhibition against clinical isolates of methicillin-resistant (MRSA) in both and models. The initial supply of 1: was 19 mg, and this amount needed to be scaled by a factor of 30 to 50 times, in order to generate material for further studies.

Delitpyrones: α-Pyrone Derivatives from a Freshwater Delitschia sp.

In research focused on the discovery of new chemical diversity from freshwater fungi, a peak library was built and evaluated against a prostate cancer cell line, E006AA-hT, which was derived from an African American, as this population is disproportionately affected by prostate cancer. The chemical study of the bioactive sample accessioned as G858 ( sp.) led to the isolation of eight new -pyrone derivatives (1:  - 7: , and 11: ), as well as the new 3,4-7-ethyl-4,8-dihydroxy-3,6-dimethoxy-3,4-dihydronaphthalen-1()-one (15: ).

Prealamethicin F50 and related peptaibols from : Validation of their authenticity via chemical analysis.

In the field of natural products chemistry, a common question pertains to the authenticity of an isolated compound, i.e. are the interesting side chains biosynthesized naturally or an artefact of the isolation/purification processes? The droplet-liquid microjunction-surface sampling probe (droplet-LMJ-SSP) coupled to a hyphenated system (UPLC-UV-HRESIMS) empowers the analysis of natural product sources , providing data on the biosynthetic timing and spatial distribution of secondary metabolites.