Bioavailability and Pharmaco-therapeutic Potential of Luteolin in Overcoming Alzheimer's Disease

CNS Neurol Disord Drug Targets. 2019;18(5):352-365. doi: 10.2174/1871527318666190319141835.

Abstract

Luteolin is a naturally occurring, yellow crystalline flavonoid found in numerous dietary supplements we frequently have in our meals. Studies in the last 2 decades have revealed its therapeutic potential to reduce the Alzheimer's disease (AD) symptoms in various in vitro and in vivo models. The anti-Alzheimer's potential of luteolin is attributed to its ability to suppress Aβ as well as tau aggregation or promote their disaggregation, down-regulate the expression of COX-2, NOS, MMP-9, TNF-α, interleukins and chemokines, reduce oxidative stress by scavenging ROS, modulate the activities of transcription factors CREB, cJun, Nrf-1, NF-κB, p38, p53, AP-1 and β-catenine and inhibiting the activities of various protein kinases. In several systems, luteolin has been described as a potent antioxidant and anti-inflammatory agent. In addition, we have also discussed about the bio-availability of the luteolin in the plasma. After being metabolized luteolin persists in plasma as glucuronides and sulphate-conjugates. Human clinical trials indicated no dose limiting toxicity when administered at a dose of 100 mg/day. Improvements in the formulations and drug delivery systems may further enhance the bioavailability and potency of luteolin. The current review describes in detail the data supporting these studies.

Keywords: Alzheimer's disease; Luteolin; ROS; bioavailability; oxidative stress; pharmaco-therapeutic..

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Alzheimer Disease / drug therapy*
  • Animals
  • Biological Availability
  • Humans
  • Luteolin / pharmacokinetics*
  • Luteolin / pharmacology
  • Luteolin / therapeutic use*
  • Neuroprotective Agents / pharmacokinetics
  • Neuroprotective Agents / pharmacology
  • Neuroprotective Agents / therapeutic use

Substances

  • Neuroprotective Agents
  • Luteolin