Tailored Beta-Lapachone Nanomedicines for Cancer-Specific Therapy.

Nanotechnology shows the power to improve efficacy and reduce the adverse effects of anticancer agents. As a quinone-containing compound, beta-lapachone (LAP) is widely employed for targeted anticancer therapy under hypoxia. The principal mechanism of LAP-mediated cytotoxicity is believed due to the continuous generation of reactive oxygen species with the aid of NAD(P)H: quinone oxidoreductase 1 (NQO1). The cancer selectivity of LAP relies on the difference between NQO1 expression in tumors and that in healthy organs. Despite this, the clinical translation of LAP faces the problem of narrow therapeutic window that is challenging for dose regimen design. Herein, the multifaceted anticancer mechanism of LAP is briefly introduced, the advance of nanocarriers for LAP delivery is reviewed, and the combinational delivery approaches to enhance LAP potency in recent years are summarized. The mechanisms by which nanosystems boost LAP efficacy, including tumor targeting, cellular uptake enhancement, controlled cargo release, enhanced Fenton or Fenton-like reaction, and multidrug synergism, are also presented. The problems of LAP anticancer nanomedicines and the prospective solutions are discussed. The current review may help to unlock the potential of cancer-specific LAP therapy and speed up its clinical translation.

Brevianthrones, bianthrones from a Chinese isolate of the endophytic fungus Colletotrichum brevisporum.

Seven undescribed bianthrones, the brevianthrones, together with two known anthraquinones, were isolated from the plant-derived fungus Colletotrichum brevisporum, obtained from the plant Piper sarmentosum Roxb., collected in Guangxi, China. This is the first report of the isolation of bianthrones from the Colletotrichum genus. The structures of the compounds were elucidated by a combination of NMR and MS spectroscopic analysis, while the absolute configurations were determined by X-ray crystallography and by simulation of ECD spectra.