Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2022 Jan 6;27(2):349.
doi: 10.3390/molecules27020349.

Modern Approaches in the Discovery and Development of Plant-Based Natural Products and Their Analogues as Potential Therapeutic Agents

Asim Najmi  1 , Sadique A Javed  1 , Mohammed Al Bratty  1 , Hassan A Alhazmi  1   2
Affiliations
Review

Modern Approaches in the Discovery and Development of Plant-Based Natural Products and Their Analogues as Potential Therapeutic Agents

Asim Najmi et al. Molecules. .

Abstract

Natural products represents an important source of new lead compounds in drug discovery research. Several drugs currently used as therapeutic agents have been developed from natural sources; plant sources are specifically important. In the past few decades, pharmaceutical companies demonstrated insignificant attention towards natural product drug discovery, mainly due to its intrinsic complexity. Recently, technological advancements greatly helped to address the challenges and resulted in the revived scientific interest in drug discovery from natural sources. This review provides a comprehensive overview of various approaches used in the selection, authentication, extraction/isolation, biological screening, and analogue development through the application of modern drug-development principles of plant-based natural products. Main focus is given to the bioactivity-guided fractionation approach along with associated challenges and major advancements. A brief outline of historical development in natural product drug discovery and a snapshot of the prominent natural drugs developed in the last few decades are also presented. The researcher's opinions indicated that an integrated interdisciplinary approach utilizing technological advances is necessary for the successful development of natural products. These involve the application of efficient selection method, well-designed extraction/isolation procedure, advanced structure elucidation techniques, and bioassays with a high-throughput capacity to establish druggability and patentability of phyto-compounds. A number of modern approaches including molecular modeling, virtual screening, natural product library, and database mining are being used for improving natural product drug discovery research. Renewed scientific interest and recent research trends in natural product drug discovery clearly indicated that natural products will play important role in the future development of new therapeutic drugs and it is also anticipated that efficient application of new approaches will further improve the drug discovery campaign.

Keywords: bioactivity-guided; drug discovery; ethnopharmacological; extraction; isolation; plant-based natural products.

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
The major processes involved in the discovery and development of natural products from botanical sources.
Figure 2
Figure 2
An outline of parallel approach for biological activity guided fractionation of plant extracts.
Figure 3
Figure 3
An outline of sequential approach for biological activity guided fractionation of plant extract.
Figure 4
Figure 4
An outline for structural elucidation of new phytochemicals.
Figure 5
Figure 5
The overall approaches in modern drug discovery and development process from botanical sources.
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

References

    1. Newman D.J., Cragg G.M., Snader K.M. The influence of natural products upon drug discovery. Nat. Prod. Rep. 2000;17:215–234. - PubMed
    1. Newman D.J., Cragg G.M., Snader K.M. Natural products as sources of new drugs over the period 1981–2002. J. Nat. Prod. 2003;66:1022–1037. doi: 10.1021/np030096l. - DOI - PubMed
    1. Koehn F.E., Carter G.T. The evolving role of natural products in drug discovery. Nat. Rev. Drug Discov. 2005;4:206–220. doi: 10.1038/nrd1657. - DOI - PubMed
    1. Balunas M.J., Kinghorn A.D. Drug discovery from medicinal plants. Life Sci. 2005;78:431–441. doi: 10.1016/j.lfs.2005.09.012. - DOI - PubMed
    1. Drahl C., Cravatt B.F., Sorensen E.J. Protein-reactive natural products. Angew. Chem. Int. Ed. Engl. 2005;44:5788–5809. doi: 10.1002/anie.200500900. - DOI - PubMed

Substances

LinkOut - more resources