A new bufadienolide with cytotoxic activity from the Chinese traditional drug Ch'an Su

Chin J Nat Med. 2014 Aug;12(8):623-7. doi: 10.1016/S1875-5364(14)60095-9.

Abstract

Aim: To study the bufadienolides in the Chinese traditional drug "Ch'an Su" and their cytotoxic activity.

Method: Various chromatographic techniques were used to isolate the constituents, and their structures were elucidated through physical and spectroscopic data.

Results: Twenty compounds were isolated, and eighteen were evaluated in vitro for their cytotoxic activity against A-549 and K-562 cells.

Conclusion: Compound 1 (bufalin 3β-acrylic ester) was a new bufadienolide and exhibited the most potent activity against the two tumor cell lines with IC50 values of 7.16 and 6.83 nmol · L(-1). The relationships between structure and activity are discussed.

Keywords: Bufalin 3β-acrylic ester; Cytotoxicity; New bufadienolide; “Ch'an Su”.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amphibian Venoms / chemistry
  • Amphibian Venoms / pharmacology
  • Amphibian Venoms / therapeutic use*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / isolation & purification
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Biological Products / chemistry
  • Biological Products / pharmacology
  • Biological Products / therapeutic use*
  • Bufanolides / chemistry
  • Bufanolides / isolation & purification
  • Bufanolides / pharmacology
  • Bufanolides / therapeutic use*
  • Humans
  • Inhibitory Concentration 50
  • K562 Cells
  • Medicine, Chinese Traditional
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Structure-Activity Relationship

Substances

  • Amphibian Venoms
  • Antineoplastic Agents
  • Biological Products
  • Bufanolides
  • bufalin 3beta-acrylic ester
  • chan su