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Natural products have a long history of use as folk medicines in several systems of traditional medicine. Extensive evidence from modern pharmacological studies has confirmed traditional applications, and unveiled the vast potential of naturally occurring compounds, particularly plant-derived phytochemicals, in the management of chronic human diseases. The past decade has witnessed a surge of findings from randomized controlled trials testifying the safety and efficacy of natural products as adjuncts or alternatives to standard-of-care medications for several illnesses. Biomolecular studies have unveiled hundreds of cellular and molecular targets for phytochemicals including key transcription factors, receptors, enzymes, hormones, neurotransmitters, cytokines, lipids, and non-coding RNAs.