Novel galactonic acid-binding hexameric lectin from Hibiscus mutabilis seeds with antiproliferative and potent HIV-1 reverse transcriptase inhibitory activities

Acta Biochim Pol. 2009;56(4):649-54. Epub 2009 Dec 4.

Abstract

A hexameric 150-kDa lectin was isolated from dried Hibiscus mutabilis seeds using a chromatographic protocol that involved ion exchange chromatography on SP-Sepharose, and gel filtration on Superdex 75 and Superdex 200. The lectin was not adsorbed on SP-Sepharose and was eluted from the Superdex 75 column in the void volume. It was eluted in the first peak from Superdex 200. It was strongly adsorbed on DEAE-cellulose and Q-Sepharose and could not be easily desorbed. The hemagglutinating activity of the lectin, which was stable at pH 4-7 and up to 50 degrees C, could be inhibited by 25 mM galactonic acid. This is the first report of a galactonic acid-binding lectin. It potently inhibited HIV-1 reverse transcriptase with an IC(50) of 0.2 microM. It exhibited weak antiproliferative activity towards both hepatoma HepG2 cells (40% inhibition) and breast cancer MCF-7 cells (50% inhibition) at 100 microM concentration of the lectin. It did not inhibit mycelial growth of a number of fungi tested.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Cell Line, Tumor
  • Chromatography, Gel
  • Chromatography, Ion Exchange
  • HIV Reverse Transcriptase / antagonists & inhibitors*
  • Hemagglutination / drug effects
  • Hep G2 Cells
  • Hibiscus / chemistry*
  • Humans
  • Inhibitory Concentration 50
  • Plant Lectins / chemistry
  • Plant Lectins / isolation & purification*
  • Plant Lectins / pharmacology
  • Protein Binding
  • Protein Multimerization
  • Rats
  • Reverse Transcriptase Inhibitors / pharmacology
  • Seeds / chemistry
  • Sugar Acids / chemistry

Substances

  • Antineoplastic Agents, Phytogenic
  • Plant Lectins
  • Reverse Transcriptase Inhibitors
  • Sugar Acids
  • galactonic acid
  • reverse transcriptase, Human immunodeficiency virus 1
  • HIV Reverse Transcriptase