Kaempferol (kae) and its glycosides are widely distributed in nature and show multiple bioactivities, yet few reports have compared them. In this paper, we report the antitumor, antioxidant and anti-inflammatory activity differences of kae, kae-7-O-glucoside (kae-7-O-glu), kae-3-O-rhamnoside (kae-3-O-rha) and kae-3-O-rutinoside (kae-3-O-rut). Kae showed the highest antiproliferation effect on the human hepatoma cell line HepG2, mouse colon cancer cell line CT26 and mouse melanoma cell line B16F1. Kae also significantly inhibited AKT phosphorylation and cleaved caspase-9, caspase-7, caspase-3 and PARP in HepG2 cells. A kae-induced increase in DPPH and ABTS radical scavenging activity, inhibition of concanavalin A (Con A)-induced activation of T cell proliferation and NO or ROS production in LPS-induced RAW 264.7 macrophage cells were also seen. Kae glycosides were used to produce kae via environment-friendly enzymatic hydrolysis. Kae-7-O-glu and kae-3-O-rut were hydrolyzed to kae by β-glucosidase and/or α-L-rhamnosidase. This paper demonstrates the application of enzymatic catalysis to obtain highly biologically active kae. This work provides a novel and efficient preparation of high-value flavone-related products.

The green and efficient extraction of bioactive compounds from plant biomass is an important area of interest in the pharmaceutical industries. Hydrophilic deep eutectic solvents (DESs) have been considered as green alternatives to conventional solvents for bioactive compound extraction. In this study, we aimed to provide a practical example demonstrating the tunability of hydrophobic DESs as designer solvents to efficiently extract bioactive compounds from plant biomass. Artemisinin, known as the only drug effective in the treatment of malaria, was chosen for extraction from Artemisia annua leaves. A hydrophobic DES named N81Cl-NBA that was tailor-made from methyl trioctyl ammonium chloride and 1-butanol at a molar ratio of 1:4 showed the highest extraction yield. With N81Cl-NBA-based ultrasound-assisted extraction (UAE), the main factors affecting the extraction yield were statistically optimized using a central composite design combined with a response surface methodology. The optimal conditions were obtained as follows: solvent/solid ratio 17.5:1, ultrasonic power 180 W, temperature 45 °C, particle size 80 mesh, and extraction time 70 min. Under these conditions, an extraction yield of 7.9936 ± 0.0364 mg/g was obtained, which was distinctly higher than that obtained using the conventional organic solvent petroleum ether. Moreover, the recovery of the target artemisinin from the N81Cl-NBA extraction solution was achieved by AB-8 macroporous resin with a recovery yield of 85.65%. N81Cl-NBA could be reused at least two times without a significant decrease in extraction yield. This study suggests that not only hydrophilic DESs but also hydrophobic DESs are truly designer solvents that can be used as green and safe extraction solvents for pharmaceutical applications.

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As one of the most ancient tree species, the codon usage pattern analysis of Ginkgo biloba is a useful way to understand its evolutionary and genetic mechanisms. Several studies have been conducted on angiosperms, but seldom on gymnosperms. Based on RNA-Seq data of the G. biloba transcriptome, amount to 17,579 unigenes longer than 300 bp were selected and analyzed from 68,547 candidates. The codon usage pattern tended towards more frequently use of A/U-ending codons, which showed an obvious gradient progressing from gymnosperms to dicots to monocots. Meanwhile, analysis of high/low-expression unigenes revealed that high-expression unigenes tended to use G/C-ending codons together with more codon usage bias. Variation of unigenes with different functions suggested that unigenes involving in environment adaptation use G/C-ending codons more frequently with more usage bias, and these results were consistent with the conclusion that the formation of G. biloba codon usage bias was dominated by natural selection.