Daphne genkwa (D. genkwa) is the dried flower buds of a Chinese medicinal plant with multiple biological activities. Response surface methodology (RSM) combined with artificial neural network (ANN) techniques were utilized to optimize ultrasound-assisted extraction conditions for D. genkwa. Antioxidant activity and anti-inflammatory and analgesic properties of total flavonoids from D. genkwa (TFDG) were assessed. Optimal conditions involving ultrasonic power of 225 W, 30 min extraction time, 30 mL/g liquid-solid ratio, 60 °C extraction temperature, and 70% ethanol concentration yielded a maximum total flavonoids content (TFC) of 5.41 mg/g. After microporous resin purification, four specific flavonoids in D. genkwa were identified and quantified using high-performance liquid chromatography (HPLC). The TFDG demonstrated potent antioxidant activity, with a 94% rate of scavenging the 2, 2-diphenyl-1-picrylhydrazyl (DPPH). Furthermore, TFDG exhibited pain-alleviating properties in hot plate and acetic acid-induced writhing tests and noteworthy inhibitory effects on xylene-induced ear swelling in mice. The total flavonoids extracted by ultrasound had excellent biological activity. This establishes a foundation for further investigation into the potential medical value of D. genkwa.

Cyanidin-3-O-galactoside and cyanidin-3-O-arabinoside (purity >98%) were isolated from black chokeberry by preparative high-performance liquid chromatography, and an animal experiment was conducted to investigate the pharmacokinetics of two anthocyanin monomers after intravenous administration. The results showed that cyanidin-3-O-galactoside has preferable druggability than cyanidin-3-O-arabinoside in pharmacokinetic area. [GRAPHICS]

1. This study aimed to assess the effects of total flavonoid extracts (TFDG) and the monomers of Daphne genkwa on the CYP2C8 activity in vitro and in vivo. 2. The 50% inhibitory concentration (IC₅₀) values were used to determine the inhibitory effect of TFDG and its four monomers for the CYP2C8 activity by recombinant human CYP2C8 (RHCYP2C8) yeast microsome system in vitro, and the volume per dose index (VDI) was predicted the potential inhibition in vivo. The effects of multiple-dose administration of TFDG on the pharmacokinetic parameters of rosiglitazone in rats were evaluated. 3. The IC₅₀ values of apigenin, luteolin, hydroxy-genkwanin, genkwanin, and TFDG were 7.27μmol/L, 11.9μmol/L, 28.1μmol/L, 127μmol/L, and 13.4μg/mL, respectively. The VDI values of apigenin and TFDG were 2.15L and 6.60L. In vivo study, compared with the control group, the elimination phase half-life and mean residence time in the TFDG treatment group were significantly increased by 96.9% and 106.8% (p < 0.05), respectively. 4. Apigenin showed a moderate inhibitory effect on the CYP2C8 activity in vitro, while the other three monomers were weak inhibitors. TFDG had a strong inhibitory effect on CYP2C8 in vitro and in vivo, and also inhibited the metabolism of rosiglitazone in rats.