New cytotoxic indole derivatives with anti-FADU potential produced by the endophytic fungus Penicillium oxalicum 2021CDF-3 through the OSMAC strategy.

Fungi possess well-developed secondary metabolism pathways that are worthy of in-depth exploration. The One Strain Many Compounds (OSMAC) strategy is a useful method for exploring chemically diverse secondary metabolites. In this study, continued chemical investigations of the marine red algae-derived endophytic fungus Penicillium oxalicum 2021CDF-3 cultured in PDB media yielded six structurally diverse indole derivatives, including two new prenylated indole alkaloids asperinamide B (1) and peniochroloid B (5), as well as four related derivatives (compounds 2-4 and 6). The chemical structures of these compounds, including the absolute configurations of 1 and 5, were determined by extensive analyses of HRESIMS, 1D and 2D NMR spectroscopic data, and TDDFT-ECD calculations. Compound 1 was found to possess an unusual 3-pyrrolidone dimethylbenzopyran fused to the bicyclo[2.2.2]diazaoctane moiety, which was rare in previously reported prenylated indole alkaloids. In vitro cytotoxic experiments against four human tumor cell lines (HeLa, HepG2, FADU, and A549) indicated that 1 strongly inhibited the FADU cell line, with an IC50 value of 0.43 ± 0.03 µM. This study suggested that the new prenylated indole alkaloid 1 is a potential lead compound for anti-FADU drugs.

Realization of monolayer ZrTe5 topological insulators with wide band gaps.

Two-dimensional topological insulators hosting the quantum spin Hall effect have application potential in dissipationless electronics. To observe the quantum spin Hall effect at elevated temperatures, a wide band gap is indispensable to efficiently suppress bulk conduction. Yet, most candidate materials exhibit narrow or even negative band gaps. Here, via elegant control of van der Waals epitaxy, we have successfully grown monolayer ZrTe5 on a bilayer graphene/SiC substrate. The epitaxial ZrTe5 monolayer crystalizes in two allotrope isomers with different intralayer alignments of ZrTe3 prisms. Our scanning tunneling microscopy/spectroscopy characterization unveils an intrinsic full band gap as large as 254 meV and one-dimensional edge states localized along the periphery of the ZrTe5 monolayer. First-principles calculations further confirm that the large band gap originates from strong spin-orbit coupling, and the edge states are topologically nontrivial. These findings thus provide a highly desirable material platform for the exploration of the high-temperature quantum spin Hall effect.

Genome-wide identification of cyclophilin genes in Gossypium hirsutum and functional characterization of a CYP with antifungal activity against Verticillium dahliae.

BACKGROUND: Cyclophilins (CYPs), belonging to the peptidyl prolyl cis/trans isomerase (PPIase) superfamily, play important roles during plant responses to biotic and abiotic stresses. RESULTS: Here, a total of 79 CYPs were identified in the genome of Gossypium hirsutum. Of which, 65 GhCYPs only contained one cyclophilin type PPIase domain, others 14 GhCYPs contain additional domains. A number of cis-acting elements related to phytohormone signaling were predicated in the upstream of GhCYPs ORF. The expression analysis revealed that GhCYPs were induced in response to cold, hot, salt, PEG and Verticillium dahliae infection. In addition, the functional importance of GhCYP-3 in Verticillium wilt resistance was also presented in this study. GhCYP-3 showed both cytoplasmic and nuclear localization. Overexpression of GhCYP-3 in Arabidopsis significantly improved Verticillium wilt resistance of the plants. Recombinant GhCYP-3 displayed PPIase activity and evident inhibitory effects on V. dahliae in vitro. Moreover, the extracts from GhCYP-3 transgenic Arabidopsis displayed significantly inhibit activity to conidia germinating and hyphal growth of V. dahliae. CONCLUSIONS: Our study identified the family members of cotton CYP genes using bioinformatics tools. Differential expression patterns of GhCYPs under various abiotic stress and V. dahliae infection conditions provide a comprehensive understanding of the biological functions of candidate genes. Moreover, GhCYP-3 involved in the resistance of cotton to V. dahliae infection presumably through antifungal activity.

Overexpression of 3-deoxy-7-phosphoheptulonate synthase gene from Gossypium hirsutum enhances Arabidopsis resistance to Verticillium wilt.

KEY MESSAGE: Expression of DHS1 in cotton is induced upon infection by Verticillium dahliae , and overexpression of GhDHS1 endows transgenic Arabidopsis plants excellent Verticillium resistance. Verticillium wilt is caused by a soil-borne fungus Verticillium dahliae. Resistance in most cotton cultivars is either scarce or unavailable, making Verticillium wilt a major obstacle in cotton production. Here, we identified a 3-deoxy-7-phosphoheptulonate synthase (DHS, EC 4.1.2.15) gene from Gossypium hirsutum, named GhDHS1. Its 1620 bp open reading frame encodes a putative 59.4 kDa protein. Phylogenetic analysis indicated that GhDHS1 is clustered in a clade with potato and tomato DHSs that can be induced by wounding and elicitors, respectively. Expression analysis demonstrated that GhDHS1 is constitutively expressed in cotton roots and stems, but transcripts are rare or non-existent in the leaves. Subcellular localization showed that GhDHS1 occurs in the plastids. When plants of three cultivars were inoculated with V. dahliae, DHS1 expression was more significantly up-regulated in the roots of resistant G. barbadense cv. Pima90-53 and G. hirsutum cv. Jimian20 than in the susceptible G. hirsutum cv. Han208. This suggested that DHS1 is involved in the cotton resistance to Verticillium wilt. Furthermore, GhDHS1 overexpressing transgenic lines of Arabidopsis were developed via Agrobacterium tumefaciens-mediated transformation. Compared with the untransformed WT (wild type), these transgenic plants showed excellent Verticillium wilt resistance with a significantly lower disease index. The overexpressing transgenic lines also had significantly longer primary roots and greatly increased xylem areas under V. dahliae infection. Overall, our results indicate that GhDHS1 performs a role in the cotton resistance to V. dahliae and would be potential to breeding cottons of Verticillium wilt resistance.