Setosphlides A-D, New Isocoumarin Derivatives from the Entomogenous Fungus Setosphaeria rostrate LGWB-10

Investigation of the entomogenous fungus Setosphaeria rostrate LGWB-10 from Harmonia axyridis led to the isolation of four new isocoumarin derivatives,setosphlides A-D(1-4),and four known analogues(5-8).Their planar structures and the relative configurations were elucidated by comprehensive spectroscopic methods.The absolute configurations of isocoumarin nucleus for 1-4 were elucidated by their ECD spectra.The C-10 relative configurations for the pair of C-10 epimers(1 and 2)were established by comparing the magnitude of the computed 13C NMR chemical shifts(Δδcalcd.)with the experimental 13C NMR values(Δδexp.)for the epimers.All of the isolated compounds(1-8)were evaluated for their cytotoxicities against four human tumor cell lines MCF-7,MGC-803,HeLa,and Huh-7.

Study on Biotransformation of Natural Anti-tumor Drug Podophyllotoxin

[Objective] This study aimed to select stains for transforming podophyllotoxin, to isolate the transformation product and to identify the structure. [ Method~ Structure of podophyllotoxin was modified with microbial batch transformation method. Podophyllotoxin and its transformation products were detected by using TLC and HPLC methods to select strains with ability to transform podophyllotoxin. Scale-up fermentation of one podophyllotoxin-transforming strain was carried out and the fermented material was extracted with EtoAc, isolated with conventional silica gel column chromatography, structure of the transformation product was identified by using classic spectroscopy technology. [ Result ] Based on researches of pedophyllotoxin transformation, seven strains with ability to transform po- dophyllotoxin were selected, including BS. Str-1, BS. Str-2, BS. Str-3, BS. Str-7, BS. Str-18, BS. Str-21 and BS. Str-29. By scale up fermentation, the only trans- formation product of BS. Str-21 strain was extracted and isolated, which was identified as picropodophyllotoxin. [ Conclusion] This study demonstrates that podo- phyllotoxin derivatives can be obtained by biotransformation methods, which lays the foundation for acquisition of natural drugs with high anti-tumor activity.

Selective recognition of HIV RNA by dinuclear metallic ligands

We describe the development of dinuclear metallic ligands to target specific HIV RNA structures. Two series of dipyridinyl-N bridged dinuclear metal complexes were synthesized in moderate to good yields and their binding activities toward TAR and RRE RNA were studied both experimentally and theoretically. The docking calculation elucidated some structure features in dimetallic complexes that can affect TAR RNA-binding properties.