Discovery of 4'-trifluoromethylchalcones as novel, potent and selective hCYP1B1 inhibitors without concomitant AhR activation.

Human cytochrome P450 1B1 (hCYP1B1), an extrahepatic cytochrome P450 enzyme over-expressed in various tumors, has been validated as a promising target for preventing and treating cancers. Herein, two series of chalcone derivatives were synthesized to discover potent hCYP1B1 inhibitors without AhR agonist effect. Structure-activity relationship (SAR) studies demonstrated that 4'-trifluoromethyl on the B-ring strongly enhanced the anti-hCYP1B1 effects, identifying A9 as a promising lead compound.

Tongxie-Yaofang formula regulated macrophage polarization to ameliorate DSS-induced colitis via NF-κB/NLRP3 signaling pathway.

Background: Macrophages infiltration and activation play multiple roles in maintaining intestinal homeostasis and participate in the occurrence and development of UC. Thus, the restoration of immune balance can be achieved by targeting macrophage polarization. Previous studies have reported that TXYF could effectively ameliorate DSS-induced colitis.

Cucurbitacin B controls M2 macrophage polarization to suppresses metastasis via targeting JAK-2/STAT3 signalling pathway in colorectal cancer.

Ethnopharmacological Relevance: Cucurbitacin B (CuB), extracted from muskmelon pedicel, is a widely available triterpenoid molecule that exerts influence on various biological activities. Modern pharmacological studies have found that cucurbitacin B has many kinds of pharmacological anti-tumor and anti-metastasis functions.

Aim Of The Study: To explore the mechanism of anti-tumor and anti-metastasis effect of cucurbitacin B.

[Study on determination of anthraquinones in dachengqi tang residues of Magnolia officinalis and Citrus aurantium removed in decoction process].

Objective: The traditional decoction method of Dachengqi Tang is that "First boiling Magnolia officinalis and Citrus aurantium with a pipeful of water, taking out five litres from the decoction, removing residues, adding rheum officinale, boiling again, taking out two litres from it, removing residues, adding mirabilite, boiling it with low fire". According to it, residues of M. officinalis and C.

[Advances in studies compatibility applied toattenuation and synergy of Tripterygium wilfordii].

Review the research and development status that Chinese medicine are compatible with Tripterygium wilfordii for attenuation and synergy for recent year. From modern medicine view and Chinese medicine dialectical perspective explain the mechanisms and methods of compatibility applied to attenuation and synergy of T. wilfordii.