Jianbing Tan

Koninginins X-Z (1–3), three novel polyketides, were isolated from the solid fermentation of the endophytic fungus Trichoderma koningiopsis SC-5. Their structures, including the absolute configurations, were comprehensively characterized by a combination of NMR spectroscopic methods, HRESIMS, ¹³C NMR, DFT GIAO ¹³C NMR, and electronic circular dichroism calculations as well as single crystal X-ray diffraction. In addition, all the compounds were evaluated for antifungal activity against Candida albicans.

Five new furofurans lignans, Brasesquilignan A–E (1–5), were isolated from the aqueous ethanol extract of Selaginella braunii Baker. Their structures were elucidated by extensive analysis of NMR and HRESIMS data. Their absolute configurations were determined by CD spectra, enzymatic hydrolysis, and GCMS analysis. Furthermore, all compounds were evaluated for anti-proliferative activities against various human cancer cellsin vitro. Compounds 2 and 3 exhibited weak inhibitorypotency against five human cancer cells.

Two new phthalide derivatives, rhytidhylides A (1) and B (2), together with ten known compounds (3–12) were isolated from cultures of Rhytidhysteron sp. BZM-9, an endophyte isolated from the leaves of Leptospermum brachyandrum. Their structures were identified by an extensive analysis of NMR, HRESIMS, ECD, and through comparison with data reported in the literature. In addition, the cytotoxic activities against two human hepatoma cell lines (HepG2 and SMMC7721) and antibacterial activities against MRSA and E. coli were evaluated.

Four new biflavonoids (1–4) were isolated from Selaginella doederleinii together with a known biflavonoid derivative (5). Their structures contained a rare linker of individual flavones to each other by direct C-3-O-C-4′′′ bonds, and were elucidated by extensive spectroscopic data, including HRESIMS, NMR and ECD data. All isolates significantly inhibited the proliferation of NSCLC cells (IC₅₀ = 2.3–8.4 μM) with low toxicity to non-cancer MRC-5 cells, superior to the clinically used drug DDP. Furthermore, the most active compound 3 suppressed XIAP and survivin expression, promoted upregulation of caspase-3/cleaved-caspase-3, as well as induced cell apoptosis and cycle arrest in A549 cells. Together, our findings suggest that 3 may be worth studying further for intervention of NSCLC.

Nowadays, many commercial drugs have poor solubility and bioavailability. Cocrystals are formulated to modulate active pharmaceutical ingredients’ properties with improved solubility, dissolution, and bioavailability compared to their pristine individual components in the pharmaceutical industry. Nano-cocrystals, crystals in the nano range, can further enhance these properties because of not only the cocrystal structure, but also the large surface to volume ratio of nanocrystals. Even though there are many studies on cocrystals, the research of pharmaceutical nano-cocrystals is still in the initial stage. Thus, it is necessary to conduct a systematic study on pharmaceutical nano-cocrystals. In this review, the possible preparation approaches of nano-cocrystals have been reported. To have a comprehensive understanding of nano-cocrystals, some analytical techniques and characterizations will be discussed in detail. In addition, the feasible therapeutic application of nano-cocrystals will be presented. This work is expected to provide guidance to develop new nano-cocrystals with commercial value in the pharmaceutical industry.