New sesquiterpenes from Asteriscus graveolens

Area of Science:

• Phytochemistry
• Pharmacology
• Natural Products Chemistry

Background:

• Asteriscus graveolens (Forsk) Less. is a Saharan medicinal plant from the Asteraceae family.
• This plant is traditionally recognized for its therapeutic properties.
• Investigating its chemical constituents and biological activities is crucial for potential pharmaceutical applications.

Purpose of the Study:

• To isolate and characterize novel and known compounds from Asteriscus graveolens.
• To evaluate the cytotoxic effects of extracts and isolated compounds on human colon cancer cell lines.
• To assess the selectivity of these compounds by testing against normal human dermal fibroblasts.

Main Methods:

• Isolation of compounds using polar extraction techniques.
• Structure elucidation through 1D-2D NMR and high-resolution mass spectrometry.
• In vitro cytotoxic assays on Human Colon Carcinoma (HCT116) and Human Colorectal Adenocarcinoma (DLD1) cells, and Primary Human Dermal Fibroblast (HDFa).

Main Results:

• A new acyclic sesquiterpene and two new sesquiterpene germacranolide lactone derivatives were identified, along with eight known compounds.
• Asteriscus graveolens extracts and compounds demonstrated significant, dose-dependent inhibition of HCT116 and DLD1 cell growth (IC50 range: 32.6–728.1 µg/mL).
• No cytotoxic effects were observed on normal HDFa cells at tested concentrations, indicating potential selectivity.

Conclusions:

• Asteriscus graveolens is a rich source of bioactive sesquiterpenes with promising anti-cancer properties.
• The isolated compounds exhibit selective cytotoxicity against colon cancer cells, warranting further investigation for therapeutic development.
• This study validates the traditional use of Asteriscus graveolens and highlights its potential in cancer treatment.