Gambogic acid enhances proteasome inhibitor-induced anticancer activity

Sulindac enhances the proteasome inhibitor bortezomib-mediated oxidative stress and anticancer activity.

PURPOSE The nonsteroidal antiinflammatory drug sulindac is a promising chemopreventive agent against colon cancer. Here, we address whether sulindac enhances the anticancer effects of the proteasome inhibitor bortezomib (PS-341) in colon cancer cells. EXPERIMENTAL DESIGN The synergistic effects of sulindac with bortezomib were evaluated by cell death, colony formation assay, DNA fragmentation...

Gambogic acid is a tissue-specific proteasome inhibitor in vitro and in vivo.

Gambogic acid (GA) is a natural compound derived from Chinese herbs that has been approved by the Chinese Food and Drug Administration for clinical trials in cancer patients; however, its molecular targets have not been thoroughly studied. Here, we report that GA inhibits tumor proteasome activity, with potency comparable to bortezomib but much less toxicity. First, GA acts as a prodrug and onl...

Keywords: Gambogic acid, anticancer, ER stress, Apoptosis, HeLa cells

Subcellular localization and activity of gambogic acid.

The natural product gambogic acid (GA) has shown significant potential as an anticancer agent as it is able to induce apoptosis in multiple tumor cell lines, including multidrug-resistant cell lines, as well as displaying antitumor activity in animal models. Despite the fact that GA has entered phase I clinical trials, the primary cellular target and mode of action of this compound remain uncle...

Dihydromyricetin prevents cardiotoxicity and enhances anticancer activity induced by adriamycin

Adriamycin, a widely used anthracycline antibiotic in multiple chemotherapy regimens, has been challenged by the cardiotoxicity leading to fatal congestive heart failure in the worst condition. The present study demonstrated that Dihydromyricetin, a natural product extracted from ampelopsis grossedentat, exerted cardioprotective effect against the injury in Adriamycin-administrated ICR mice. Di...