Natural Products as a Source for Novel Antibiotics

Abstract

Natural products have historically been of crucial importance in the identification and development of antibacterial agents. Interest in these systems has waned in recent years, but the rapid emergence of resistant bacterial strains has forced their re-evaluation as a route to identify novel chemical skeletons with antibacterial activity for elaboration in drug development. This overview examines the current situation, highlights new natural product systems which have been found, together with re-examination of some old ones, and new technologies for their identification. While natural products certainly have the potential to re-emerge as a key start-point in antibacterial drug discovery, reports of new or reinvestigated structures need to be supported with sufficient quality chemical (solubility, stability), biochemical (including toxicity in particular, along with target information) and microbiological [minimum inhibitory concentration (MIC) and resistance frequency] validation data to assist in the identification of promising hit structures and to avoid wasted effort from trawling over already cultivated territory. This is particularly important in a resource-limited research environment.

Centaurea rupestris L.: Cytogenetics, Essential Oil Chemistry and Biological Activity

“…This forced reevaluation of natural products as a source of novel chemical skeletons with antibacterial activity for elaboration in drug development. [2] In this study, we aim to investigate the antimicrobial activity of Centaurea rupestris L. essential oil (EO) targeting the nosocomial pathogens included in the notorious multidrug resistant 'ESKAPE' group (Enterococcus spp., Staphylococcus aureus, Klebsiella spp., Acinetobacter baumannii, Pseudomonas aeruginosa and Enterobacter spp.) that effectively evade the therapeutic effects of antibacterial drugs.…”

Quantitative NMR Studies of Multiple Compound Mixtures

“…Natural products have a close relation with our everyday life and play an important role in modern life science [113] and are extensively applied for drug discovery [114,115], food [116], and cosmetic development [117]. In traditional natural products research, several restrictive factors may slow down the discovery and identification of new single chemical entities (SCEs), such as time consuming and cumbersome separation, purification and structural elucidation steps, redundant work such as identifying already known compounds, limited detection sensitivity, lacking systematic registration of origin organisms and derived compounds.…”

Antimicrobial activity of stigmasterol from the stem bark of <i>Neocarya macrophylla</i>

“…In the last few decades, the interest of the industry in natural products has dwindled; however, in recent times, the need to tackle multidrug resistance and other emerging health problems has fuelled the rebirth of natural product drug discovery. In this regard, natural products may continue to play a vital role in antimicrobial drug discovery; therefore, there is an urgent need for novel natural product scaffolds with superior properties (Chen et al 2016;Moloney 2016). Nature's biodiversity represents a huge reservoir of bioactive chemical diversity and has been central in the identification and development of therapeutic agents (Siddiqui et al 2013); hence, drug discovery approaches exploiting nature's chemical diversity may uncover novel natural products with desired bioactivity (Pawar 2014).…”