Abstract
Based on a meta-analysis of data mined from almost 2000 publications on bioactive natural products (NPs) from >80 000 pages of 13 different journals published in 1998–1999, 2004–2005, and 2009–2010, the aim of this systematic review is to provide both a survey of the status quo and a perspective for analytical methodology used for isolation and purity assessment of bioactive NPs. The study provides numerical measures of the common means of sourcing NPs, the chromatographic methodology employed for NP purification, and the role of spectroscopy and purity assessment in NP characterization. A link is proposed between the observed use of various analytical methodologies, the challenges posed by the complexity of metabolomes, and the inescapable residual complexity of purified NPs and their biological assessment. The data provide inspiration for the development of innovative methods for NP analysis as a means of advancing the role of naturally occurring compounds as a viable source of biologically active agents with relevance for human health and global benefit.
Highlights
The diversity of the purification methods was assessed and encoded into binary format as a byte integer, consisting of the following five bits: 0 = undefined or literature reference only; 2° = precipitation or crystallization; = paper or thin-layer chromatography (TLC), including centrifugal TLC; = column liquid chromatography (LC), vacuum LC, and low-pressure LC, and the value 21 was added to encode repetition in the entire scheme; 23 = medium-pressure and high-pressure LC (MLPC, HPLC), and the value 21 was added to encode repetition in the entire scheme; 24 =
At least three additional dimensions of complexity affect the interpretation of research data on bioactive natural products (NPs) and will be addressed in the following: (i) the role and relationship of in vivo vs in vitro bioassays used to assess bioactivity in the NP purification and characterization workflow (Figure 1); (ii) the depth and diversity of the purification workflow; and (iii) the role of purity and residual complexity (RC)
Potential further dimensions to consider relate to the connectivity between single chemical entity (SCE), RC, and bioassay (Figure 2), i.e., the specificity, both qualitative and quantitative, of the bioassay
Summary
A series of excellent articles, coauthored by G. J. Newman, and colleagues,[1−5] has documented the invaluable role of NPs in drug discovery. Underlying evidence came from an extensive meta-analysis of the primary literature of all drugs, in or completing FDA-approved studies within a set time frame and classifying them according to their origin as NPs, inspired by NPs, analogues of these two classes, or from non-NP sources
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