Justicidin B and related lignans from two South African Monsonia species with potent activity against HeLa cervical cancer cells

Nasir Tajuddeen, Séverin Muyisa, Juthamart Maneenet, Hung Hong Nguyen, Dashnie Naidoo-Maharaj, Vinesh Maharaj, Suresh Awale*, Gerhard Bringmann

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

Cervical cancer is a deadly malignancy, one of the most common for women, evidencing the need for effective new chemotherapeutic agents to treat the disease. Lignans are widely occurring natural products with important pharmacological effects, including anticancer activities. Five arylnaphthalene lignans, isolated from Monsonia angustifolia and M. glauca (Geraniaceae), were investigated for their cytotoxicity against HeLa human cervical cancer cells. The best activity (IC50 1.2 μM) was exerted by justicidin B (4). The presence of additional methoxy groups in the “northern part” of the arylnaphthalene scaffold, at C-6 and/or C-7, lowered the cytotoxicity. Even more significantly, a free hydroxy group at C-7, leads to a drastic decrease in potency, by two orders of magnitude. Live-cell imaging experiments revealed that 4 induces changes in cancer cells morphology, effecting their elongation and eventual death. Justicidin B (4) inhibited formation of HeLa cell colonies in a dose-dependent manner. Mechanistic investigations showed that 4 modulates the expression of key proteins involved in apoptosis, suggesting that it induces cell death through several mechanisms.

Original languageEnglish
Pages (from-to)234-238
Number of pages5
JournalPhytochemistry Letters
Volume60
DOIs
StatePublished - 2024/04

Keywords

  • Anticancer
  • Cervical cancer HeLa cells
  • Justicidins
  • Lignans
  • Monsonia angustifolia
  • Monsonia glauca

ASJC Scopus subject areas

  • Biotechnology
  • Biochemistry
  • Agronomy and Crop Science
  • Plant Science

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