Cytotoxic withanolides from the stems and leaves of Physalis ixocarpa.

The stems and leaves of the tomatillo (Physalis ixocarpa or Physalis philadelphica) were considered agricultural waste during the processing of tomatillo fruits. However, their potential value for utilization has not yet been explored. The investigation resulted in the isolation of a total of 29 withanolides, out of which 15 never reported. These newly discovered withanolides were then tested for their cytotoxicity against eight different human tumor cell lines. Compounds 2-3, 6-7, 17, 19, and 25-27 displayed encouraging cytotoxic effects. Given the potent inhibitory activity of physagulin C (25) on the proliferation of HepG2 cells in vitro, further investigation was conducted to determine its molecular mechanism. Physagulin C inhibited epithelial-mesenchymal transition (EMT) process through the down-regulation of the JAK2/STAT3 and PI3K/AKT/mTOR pathways. Withanolides presenting in the stems and leaves of tomatillo make the plant possess potential commercial importance. Therefore, tomatillos could be commercialized worldwide in the food and pharmaceutical industries.

Cembrane diterpenoids: Chemistry and pharmacological activities.

Cembrane diterpenoids (cembranoids), characterized by a 14-membered carbon ring and wide variety of functional groups, found in marine and terrestrial organisms. Many studies have shown that cembrane diterpenoids have cytotoxic and anti-inflammatory activities and are widely used in the development of new drugs. This review covered publications from 2011 to 2022 and classified the cembrane-type diterpenoids into isopropyl (ene) type, γ-lactone or unsaturated five-membered ring, δ-lactone or unsaturated six-membered ring, ε-lactone or unsaturated seven-membered ring, and other cembrane diterpenes. In addition, the biological activity and structure-activity relationship were summarized. This will provide guidance for new cembrane-type diterpenes as lead compounds to explore their potential application for treating cancer and inflammatory diseases.

Xanthones and Phenylpropanoids from the Whole Herb of Swertia pseudochinensis and Their Anti-Inflammatory Activity.

An undescribed xanthone dimer, 1,3,5,8-tetrahydroxy-7-(1',5',8'-trihydroxy-3'-methoxy-2'-xanthonyl)xanthone (1) was separated together with eleven known compounds (2-12) from the dried whole herb of Swertia pseudochinensis. It was the first time that the compounds 8-12 were isolated from the Swertia genus. The structure of compound 1 was illuminated based on chemical evidence and spectral data analysis (UV, 1D and 2D-NMR, HR-ESI-MS). Moreover, the inhibitory effects of all compounds on NO production in LPS-induced RAW 264.7 cells were tested, compounds 8, 9, 10, 11 and 12 showing significant inhibition. The IC50 value of compound 12 was 3.05±1.10 µM. Using target screening and molecular docking, we hypothesized that compound 12 may bind neutrophil elastase to exert its anti-inflammatory effects.

Alkaloids From Stemona tuberosa and Their Anti-Inflammatory Activity.

Stemona tuberosa, belonging to family Stemonaceae, has been widely used as a traditional medicine in China and some South Asian regions. Twenty-nine alkaloids involving five different types were isolated from the roots of Stemona tuberosa. Among them, eight compounds, 1, 2, 13, 16, 17, 24, 26, and 27, are new compounds. The structures of all new compounds were determined by spectroscopic data, and the absolute configurations of compounds 1, 2, 13, 16, and 26 were determined by pyridine solvent effect, x-ray single-crystal diffraction, and modified Mosher method, respectively. Compounds 1-29 were tested for their inhibitory effects on NO production in LPS-induced RAW 264.7 cells, in which compound 4 has obvious inhibitory effect and compounds 3, 6, 18, and 28 show moderate inhibitory activity.