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Nature has produced a rich diversity of structurally complex compounds or secondary metabolites with a wide variety of biological activities.Natural products have long been exploited for therapeutic purposes in traditional medicines around the world.Recently, it was reported almost half of the 1562 new approved drugs introduced between 1981 and 2014 are natural products or derived from natural products or biological1.Therefore, the identification of active components from natural products can provide potential therapeutics in drug discovery.A limitation, however, lies in the complexity of natural products including the dynamic range of the secondary metabolites.Traditional bioassay-guided fractionation approaches, the most commonly used approach, involve repeated fractionation and biological activity screening before obtaining single bioactive compounds.While successful, this technique is labor intensive and time consuming.As a result, in the last 20-30 years, several methods have been developed to increase the throughput or decrease the complexity for the isolation of active components from natural products.In this special column, prominent scientists were invited to publish their most recent advances in the development of natural products screening technologies.