Two new xanthones, cowaxanthones G (1) and H (2), and 23 known analogues were isolated from an acetone extract of the leaves of Garcinia cowa. The isolated compounds were evaluated for cytotoxicity against three cancer cell lines and immortalized HL7702 normal liver cells, whereby compounds 1, 5, 8, and 15–17 exhibited significant cytotoxicity. Cell cycle analysis using flow cytometry showed that 5 induced cell cycle arrest at the S phase in a dose-dependent manner, 1 and 16 at the G2/M phase, and 17 at the G1 phase, while 16 and 17 induced apoptosis. Moreover, autophagy analysis by GFP-LC3 puncta formation and western blotting suggested that 17 induced autophagy. Taken together, our results suggest that these xanthones possess anticancer activities targeting cell cycle, apoptosis, and autophagy signaling pathways.

Gardeniae fructus (GF), the fruit from Gardenia jasminoides Ellis, is a traditional Chinese medicine used for the treatment of nonalcoholic fatty liver disease (NAFLD) in the clinic. To explore the hepatoprotective mechanism of GF for the treatment of NAFLD, we proposed a novel strategy that integrated in vivo efficacy evaluation, network pharmacology analysis, molecular docking, and experimental validation. A NAFLD animal model induced by high fat diet (HFD) feed was established, then orally administrated with or without GF. The results showed that GF significantly decreased the levels of serum total cholesterol (TC), lipoprotein cholesterol, triglyceride (TG), alanine aminotransferase, aspartate aminotransferase, lactate dehydrogenase, free fatty acids, glucose, and insulin and the levels of liver TG, TC, and malondialdehyde compared with the nontreated HFD group. Network pharmacology studies showed that quercetin, oleanolic acid, kaempferol, and geniposide were the main biocompounds in GF that targeted the PPARα and PPARγ genes through regulating the PPAR and AMPK signal pathways to protect against NAFLD. The interactions between bioactive compounds and their corresponding target proteins were analyzed by molecular docking and subsequently confirmed using the qRT-PCR assay. Collectively, GF was a therapeutic drug for the treatment of NAFLD.

Background: Ovarian cancer (OC) is a serious public health concern in the world. It is important to develop novel drugs to inhibit OC. Purpose: This study investigated the isolation, elucidation, efficiency, molecular docking, and pharmaceutical mechanisms of xanthones isolated from Garcinia nujiangensis. Methods: Xanthones were isolated, and purified by different chromatography, including silica gel, reversed-phase silica gel (ODS-C₁₈), and semipreparative HPLC, then identified by analysis of their spectral data. Three xanthones were estimated for their efficiency on the human OC cells HEY and ES-2. 2 was found to be the most potent cytotoxic xanthones of those tested. Further, its mechanisms of action were explored by molecular docking, cell apoptosis, and Western blotting analysis. Results: Bioassay-guided fractionation of the fruits of Garcinia nujiangensis led to the separation of a new xanthone named nujiangexanthone G ( 1) and two known xanthones. Among these, isojacareubin ( 2) exhibited the most potent cytotoxic compound against the HEY and ES-2 cell lines. The analysis of Western blot suggested that 2 inhibited OC via regulating the PARP, PI3K/AKT/mTOR, and ERK/MAPK signal pathways in the HEY cell lines. Conclusion: In conclusion, isojacareubin ( 2) might be a potential drug for the treatment of OC.