Bioactive agents from natural sources: trends in discovery and application

Area of Science:

• Natural Product Chemistry
• Drug Discovery and Development
• Medicinal Chemistry

Background:

• Approximately 30% of global drug sales originate from natural products, highlighting their therapeutic importance.
• Low-molecular mass natural compounds offer superior compliance and bioavailability compared to recombinant proteins and peptides.
• Despite historical success, natural product research faces challenges in isolating active compounds and elucidating structures, leading to reduced attention in drug discovery.

Purpose of the Study:

• To address the need for new strategies in natural product chemistry to generate diverse compound libraries.
• To enable natural products to compete with combinatorial chemistry in high-throughput screening (HTS).
• To accelerate drug discovery and development by improving lead finding and target elucidation.

Main Methods:

• Review of the role of natural products in drug discovery.
• Discussion of challenges in natural product isolation and structural elucidation.
• Exploration of advancements in molecular biology, cell biology, and genetic engineering for target identification.

Main Results:

• High-throughput screening (HTS) has revolutionized industrial drug discovery, enabling the testing of vast compound libraries.
• Genomic advancements provide a larger pool of potential drug targets.
• There is a growing demand for novel concepts to generate large, structurally diverse compound collections.

Conclusions:

• Natural products possess significant therapeutic potential, but innovative approaches are required to overcome current limitations in their utilization.
• Developing new strategies in natural product chemistry is crucial for sustained contributions to drug discovery.
• Integrating natural product-derived compounds into HTS pipelines is essential for future therapeutic advancements.