Discovery and development of anticancer agents from plants

Area of Science:

• Natural Product Chemistry
• Drug Discovery
• Pharmacology

Background:

• The search for novel anticancer agents is ongoing, with natural products representing a rich source of bioactive compounds.
• Traditional screening methods can be inefficient; novel assays are needed to accelerate the discovery of potent anticancer drugs.

Purpose of the Study:

• To develop and apply a novel in vitro assay for the discovery of anticancer agents from a large collection of plant extracts.
• To identify and isolate specific anticancer compounds from promising plant sources.

Main Methods:

• An in vitro assay was employed to screen aqueous and organic extracts from 1847 plant species.
• Active extracts were fractionated using the assay to guide the isolation of bioactive compounds.
• Compounds were categorized based on their activity and selectivity (inactive, equally active, equally active and potent, solid tumor selective, human selective).

Main Results:

• 62% of extracts were inactive, while 36% showed equal activity.
• A small percentage exhibited selective activity: 1.4% solid tumor selective and 0.8% human selective.
• Fractionation of Psorothamnus emoryi yielded dalrubone and 5-methoxydalrubone (solid tumor selective).
• Calocedrus decurrens yielded deoxypodophyllotoxin (equally active and potent).
• Linanthus floribundus yielded strophanthidin (human selective).

Conclusions:

• The developed in vitro assay is effective for discovering novel anticancer agents from plant-derived extracts.
• The assay facilitated the identification of specific anticancer compounds with potential therapeutic applications.
• This approach highlights the value of natural products in anticancer drug discovery.