The screening toolbox of bioactive substances from natural products: A review

• Published in: Fitoterapia Vol. 82; no. 8; pp. 1141 - 1151
• Main Authors: Wang, Bochu, Deng, Jia, Gao, Yimeng, Zhu, Liancan, He, Rui, Xu, Yingqian
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 01.12.2011; Elsevier
• Subjects: Active components; animal models; Animals; binding properties; bioactive properties; Biological and medical sciences; Biological Products - therapeutic use; Drug Evaluation, Preclinical - methods; drugs; General pharmacology; Humans; Lead screening; Medical sciences; Models, Animal; Models, Theoretical; Natural products; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Phytotherapy; plant extracts; Plant Extracts - therapeutic use; researchers; screening; Screening models; Lead screening; Active components; Screening models; Natural products; Performance evaluation; Drug; Animal model; Methodology; Pharmacognosy; Natural product; Review; Natural compound; Experimental study; Heavy metal; Medicinal plant; Screening; Plant origin; Lead; Technique
• ISSN: 0367-326X; 1873-6971
• DOI: 10.1016/j.fitote.2011.08.007

Hunting lead compounds from natural products plays a vital role in finding successful drug candidates. The efficiency of screening campaigns is mainly determined by the validity of selected screening models. To screen desired lead compounds, researchers have developed a plethora of experimental screening models. However, the considerable diversity of screening models from animal models, tissue models, to cell models and so on, may cause some trouble in choosing the suitable one. This review provides a toolbox of experimental screening models that have been used to discover new drug candidates from natural products. Two screening indexes are designed for different research directions in this screening toolbox. Index I is proposed from the direction of screening different objective substance populations, including plant extracts, active fractions and pure compounds; index Π is according to screening different drug properties, including pharmacological properties, pharmacokinetic properties and affinity binding properties. We hope that the abbreviated bibliographies will help readers to quickly retrieve useful information by two screening indexes and provide certain reference value for choosing more appropriate screening models. Finally, we discuss ways of improving model systems, as well as future directions. [Display omitted]