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DHDK is a novel diaryl heptanone analog isolated from mistletoe. (1 E, 4 E) 1,7‐bis (4‐hydroxyphenyl) hept‐1,4‐diene‐3‐one (DHDK) exhibits good antitumor activity and excellent stability, but it doesn't have good solubility or bioavailability. In order to improve this deficiency, the structure was modified and five new DHDK derivatives were successfully synthesized. The in vitro cytotoxic activity of DHDK derivatives against four cancer cell lines was determined by Cell Counting Kit‐8 (CCK‐8) assay. The results show that DHDK derivatives exhibit excellent potential, especially for human multiple myeloma cells (KMS‐11) and triple‐negative breast cancer cell line (MDA‐MB 231). The equilibrium solubility and oil‐water partition coefficient of DHDK derivatives were better improved by structural modification. [ABSTRACT FROM AUTHOR]

Tilianin (Til), a flavonoid glycoside, is well-known for its therapeutic promise in treating inflammatory disorders. Its poor water solubility and permeability limit its clinical applicability. In order to overcome these restrictions, an antisolvent precipitation and ultrasonication technique was used to prepare amorphous tilianin nanocrystals (Til NCs). We have adjusted the organic solvents, oil-to-water ratio, stabilizer composition, and ultrasonic power and time by combining single-factor and central composite design (CCD) methodologies. The features of Til NCs were characterized using powder X-ray diffraction (PXRD), scanning calorimetry (DSC), and transmission electron microscopy (TEM). Specifically, the optimized Til NCs were needle-like with a particle size ranging from 90 to 130 nm. PVA (0.3%, w/v) and TPGS (0.08%, w/v) stabilized them well. For at least two months, these Til NCs stayed amorphous and showed an impressive stability at 4 °C and 25 °C. Remarkably, Til NCs dissolved almost 20 times faster in simulated intestinal fluid (SIF) than they did in crude Til. In RAW264.7 cells, Til NCs also showed a better cellular absorption as well as safety and protective qualities. Til NCs were shown to drastically lower reactive oxygen species (ROS), TNF-α, IL-1β, and IL-6 in anti-inflammatory experiments, while increasing IL-10 levels and encouraging M1 macrophages to adopt the anti-inflammatory M2 phenotype. Our results highlight the potential of amorphous Til NCs as a viable approach to improve Til's anti-inflammatory effectiveness, solubility, and dissolving rate. [ABSTRACT FROM AUTHOR]