Bioactive 2-arylbenzofuran and chalcone derivatives from Morus mesozygia Stapf

Area of Science:

• Natural Product Chemistry
• Pharmacology
• Medicinal Chemistry

Background:

• Morus mesozygia is a plant species known for its traditional medicinal uses.
• Secondary metabolites from plants are a rich source of novel therapeutic agents.
• Understanding the chemical constituents and bioactivities of Morus mesozygia can lead to new drug discoveries.

Purpose of the Study:

• To isolate and identify secondary metabolites from the stem bark of Morus mesozygia.
• To evaluate the cytotoxic, anti-inflammatory, antibacterial, antitumor, and antiviral activities of the isolated compounds.
• To identify potential lead compounds for therapeutic development.

Main Methods:

• Phytochemical investigation using NMR and mass spectrometry for structure elucidation.
• In vitro assays for cytotoxicity (CC₅₀), anti-inflammatory activity (TNF-α, NF-κB, NO inhibition), antibacterial activity (MIC), antitumor activity (IC₅₀), and antiviral activity (CPE-based and plaque reduction assays).

Main Results:

• Fourteen known secondary metabolites were isolated and identified.
• Moracin D (7) exhibited potent anti-inflammatory activity against NF-κB release.
• 3β-Acetoxy-urs-12-en-11-one (12) showed potent antibacterial activity against Bacillus subtilis and Micrococcus luteus.
• Moracin M (6) displayed significant antitumor activity against SK-MEL-28 human melanoma cells.
• Isobavachalcone (9) demonstrated activity against Human Rhinovirus 2 (HRV-2).

Conclusions:

• Moracin D (7), isobavachalcone (9), and 3β-acetoxy-urs-12-en-11-one (12) are promising lead compounds for developing anti-inflammatory, antiviral, and antibacterial agents, respectively.
• The study highlights the therapeutic potential of secondary metabolites from Morus mesozygia.
• Further research is warranted to explore the full therapeutic applications of these compounds.