Bioactive compounds from the fern Lepisorus contortus

Area of Science:

• Phytochemistry
• Pharmacology
• Natural Products Chemistry

Background:

• The fern Lepisorus contortus (Christ) Ching is a source of diverse phytochemicals.
• Phenylethanoid glycosides have not been previously reported in the Polypodiaceae family.
• Natural products are increasingly explored for cancer chemopreventive properties.

Purpose of the Study:

• To isolate and characterize phytochemicals from Lepisorus contortus.
• To evaluate the cancer chemopreventive potential of isolated compounds.
• To investigate the inhibitory effects on specific molecular targets related to cancer development.

Main Methods:

• Phytochemical investigation involving isolation and structure elucidation of compounds.
• In vitro assays to assess inhibition of tumor necrosis factor alpha (TNF-α)-induced NF-κB activity.
• Enzyme inhibition assays for aromatase, quinone reductase 2 (QR-2), and COX-1/-2.

Main Results:

• Five new phenylethanoid glycosides and one new flavonoid glycoside were isolated, along with 14 known compounds.
• Quercetin-3-O-β-d-glucoside (15) inhibited QR2 (IC50 = 3.84 µM) and NF-κB (IC50 = 33.6 µM).
• Compounds 1, 2, 4, and 6 exhibited aromatase inhibitory activity (IC50 values ranging from 26.8 to 35.3 µM).

Conclusions:

• Lepisorus contortus is a source of novel phenylethanoid glycosides with potential chemopreventive activities.
• Kaempferol/quercetin glycosides are confirmed as active inhibitors of QR2.
• The study highlights the potential of Lepisorus contortus constituents in cancer chemoprevention strategies.