2. Academic Validation
  3. Antiproliferative steroidal glycosides from rhizomes of Polygonatum sibiricum

Antiproliferative steroidal glycosides from rhizomes of Polygonatum sibiricum

  • Phytochemistry. 2019 Aug;164:172-183. doi: 10.1016/j.phytochem.2019.05.013.
Di Zhou 1,  Xuezheng Li 2,  Wenhui Chang 1,  Yueqing Han 1,  Bo Liu 1,  Gang Chen 3,  Ning Li 4
Affiliations

Affiliations

  • 1 School of Traditional Chinese Materia Medica; Liaoning Province Key Laboratory of Computational Chemistry-Based Natural Antitumor Drug Research & Development, Shenyang Pharmaceutical University, Shenyang, 110016, PR China.
  • 2 Department of Pharmacy, Yanbian University Hospital, Yanji 133000, PR China.
  • 3 School of Traditional Chinese Materia Medica; Liaoning Province Key Laboratory of Computational Chemistry-Based Natural Antitumor Drug Research & Development, Shenyang Pharmaceutical University, Shenyang, 110016, PR China. Electronic address: chengang1152001@163.com.
  • 4 School of Traditional Chinese Materia Medica; Liaoning Province Key Laboratory of Computational Chemistry-Based Natural Antitumor Drug Research & Development, Shenyang Pharmaceutical University, Shenyang, 110016, PR China. Electronic address: liningsypharm@163.com.
PMID: 31158602 DOI: 10.1016/j.phytochem.2019.05.013
Abstract

Screening assays showed that total glycoside-rich fraction (TG) of rhizomes of Polygonatum sibiricum unveiled remarkable anti-proliferative activities against three Cancer cell lines (A549, HepG2, and Caco2). Activity-guided isolation of TG afforded seven undescribed steroidal glycosides (polygonosides 1-7), along with 24 known glycosides. Their structures were established by 1D and 2D NMR spectroscopic analyses, high-resolution mass spectrometry, and chemical evidence. The isolated steroidal glycosides were tested for their antiproliferative activities against A549, HepG2, and Caco2 cells. Compounds 8, 10, 11, and 16 possessed stronger Anticancer activities against A549 cells than the positive control Bay (25.8 μM), with IC50 values ranging from 5.8 to 24.2 μM. Compound 10 reduced the expression of Blc-2 and pro-caspase3 and increased the production of Bax as determined by western blotting. Molecular docking experiment suggested that 10 bound stably to the BH3-binding groove of the Bcl-2 protein by hydrogen bond interactions. These compounds could be candidates for Anticancer agents with cytotoxic activity.

Keywords

Cancer cell lines; Cytotoxicity; Molecular docking; Polygonatum sibiricum F.Delaroche (Asparagaceae); Steroidal glycosides.

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