Cardiac Glycoside Constituents of Streblus asper with Potential Antineoplastic Activity

  • J Nat Prod. 2017 Mar 24;80(3):648-658. doi: 10.1021/acs.jnatprod.6b00924.
Yulin Ren ,  Wei-Lun Chen  1 ,  Daniel D Lantvit  1 ,  Ellen J Sass ,  Pratik Shriwas ,  Tran Ngoc Ninh  2 ,  Hee-Byung Chai ,  Xiaoli Zhang ,  Djaja D Soejarto  1  3 ,  Xiaozhuo Chen ,  David M Lucas ,  Steven M Swanson  1  4 ,  Joanna E Burdette  1 ,  A Douglas Kinghorn
Affiliations
  • 1. Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago , Chicago, Illinois 60612, United States.
  • 2. Institute of Ecology and Biological Resources, Vietnam Academy of Science and Technology , Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam.
  • 3. Science and Education, Field Museum of Natural History , Chicago, Illinois 60605, United States.
  • 4. School of Pharmacy, University of Wisconsin-Madison , Madison, Wisconsin 53705, United States.
PMID: 27983842 DOI: 10.1021/acs.jnatprod.6b00924
Abstract

Three new (1-3) and two known (4 and 5) cytotoxic cardiac glycosides were isolated and characterized from a medicinal plant, Streblus asper Lour. (Moraceae), collected in Vietnam, with six new analogues and one known derivative (5a-g) synthesized from (+)-strebloside (5). A preliminary structure-activity relationship study indicated that the C-10 formyl and C-5 and C-14 hydroxy groups and C-3 sugar unit play important roles in the mediation of the cytotoxicity of (+)-strebloside (5) against HT-29 human colon Cancer cells. When evaluated in NCr nu/nu mice implanted intraperitoneally with hollow fibers facilitated with either MDA-MB-231 human breast or OVCAR3 human ovarian Cancer cells, (+)-strebloside (5) showed significant cell growth inhibitory activity in both cases, in the dose range 5-30 mg/kg.