Herbal Medicine of the 21st Century: A Focus on the Chemistry, Pharmacokinetics and Toxicity of Five Widely Advocated Phytotherapies

Curr Top Med Chem. 2019;19(29):2718-2738. doi: 10.2174/1568026619666191112121330.

Abstract

Widely advocated for their health benefits worldwide, herbal medicines (HMs) have evolved into a billion dollar generating industry. Much is known regarding their wellness inducing properties, prophylactic and therapeutic benefits for the relief of both minor to chronic ailment conditions given their long-standing use among various cultures worldwide. On the other hand, their equally meaningful chemistry, pharmacokinetic profile in humans, interaction and toxicity profile have been poorly researched and documented. Consequently, this review is an attempt to highlight the health benefits, pharmacokinetics, interaction, and toxicity profile of five globally famous HMs. A systematic literature search was conducted by browsing major scientific databases such as Bentham Science, SciFinder, ScienceDirect, PubMed, Google Scholar and EBSCO to include 196 articles. In general, ginsenosides, glycyrrhizin and curcumin demonstrate low bioavailability when orally administered. Ginkgo biloba L. induces both CYP3A4 and CYP2C9 and alters the AUC and Cmax of conventional medications including midazolam, tolbutamide, lopinavir and nifedipine. Ginsenosides Re stimulates CYP2C9, decreasing the anticoagulant activity of warfarin. Camellia sinensis (L.) Kuntze increases the bioavailability of buspirone and is rich in vitamin K thereby inhibiting the activity of anticoagulant agents. Glycyrrhiza glabra L. displaces serum bound cardiovascular drugs such as diltiazem, nifedipine and verapamil. Herbal medicine can directly affect hepatocytes leading to hepatoxicity based on both intrinsic and extrinsic factors. The potentiation of the activity of concurrently administered conventional agents is potentially lethal especially if the drugs bear dangerous side effects and have a low therapeutic window.

Keywords: Herb-drug interactions; Metabolism; Narrow therapeutic window; Pharmacokinetics; Phytoconstituents; Toxicity..

Publication types

  • Historical Article
  • Review

MeSH terms

  • Area Under Curve
  • Biological Availability
  • Cytochrome P-450 CYP2C9 / biosynthesis
  • Cytochrome P-450 CYP3A / biosynthesis
  • Enzyme Induction
  • Herbal Medicine*
  • History, 21st Century
  • Humans
  • Phytochemicals / pharmacokinetics*
  • Phytochemicals / toxicity*
  • Phytotherapy*

Substances

  • Phytochemicals
  • Cytochrome P-450 CYP2C9
  • Cytochrome P-450 CYP3A