Phyllanthusmin and acutissimalignan A compound derivatives for anticancer and immunostimulation

A group of potential antitumor arylnapthalene lactone derivatives, which may be developed as novel anticancer and immunostimulant agents.

The Need

Natural products and semi-synthetic derivatives derived from them have been used for anticancer drugs or drug leads for many years. However, side-effects such as myelosuppression and secondary leukemia have been reported. Furthermore, these natural products can be difficult to use for targeting specific cancers and water solubility is not optimal. Naturally occurring arylnapthalene lignan lactones show cytotoxicity towards cancer cell lines in vitro and in vivo, but there is still a need for new compositions for cancer treatment and immunostimulation.

The Technology

Researchers at The Ohio State University have generated a group of potential antitumor compositions from the isolation and characterization of new arylnaphthalene lignan glycosides from Phyllanthusmin and acutissimalignan A compounds. These pharmaceutical compounds can be used to prevent, treat, or ameliorate cancer and stimulate the immune system. They can be prepared in a variety of ways and can be delivered with a carrier, topically through ointments or sprays, or in liquid for oral administration. The compositions may be used for treating cancer in humans or animals or as immunostimulants. Some of these compounds are topoisomerase II inhibitors, while others can activate caspase-3.

Commercial Applications

  • Combination therapy for immune-related malignancies
  • Antiviral agent dual treatments
  • Antibody-drug conjugates
  • Prodrugs
  • Targeted tumor prophylatic and therapeutic treatments
  • Cancer treatment
    • Brain cancer
    • Bladder Cancer
    • Cervical Cancer
    • Ovarian Cancer
    • Epstein-Barr Virus


  • May prove useful for the treatment of cancer types for which presently there is no known treatment
  • Potentially less toxic effects
  • Enhanced activity and water solubility
  • PK studies completed for some compounds
  • Potent in xenograft murine model of ovarian cancer


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