Pharmacological Activity, Pharmacokinetics, and Clinical Research Progress of Puerarin

Abstract

As a kind of medicine and food homologous plant, kudzu root (Pueraria lobata (Willd.) Ohwi) is called an "official medicine" in Chinese folk medicine. Puerarin is the main active component extracted from kudzu root, and its structural formula is 8-β-D-grapes pyranose-4, 7-dihydroxy isoflavone, with a white needle crystal; it is slightly soluble in water, and its aqueous solution is colorless or light yellow. Puerarin is a natural antioxidant with high health value and has a series of biological activities such as antioxidation, anti-inflammation, anti-tumor effects, immunity improvement, and cardio-cerebrovascular and nerve cell protection. In particular, for the past few years, it has also been extensively used in clinical study. This review focuses on the antioxidant activity of puerarin, the therapy of diverse types of inflammatory diseases, various new drug delivery systems of puerarin, the "structure-activity relationship" of puerarin and its derivatives, and pharmacokinetic and clinical studies, which can provide a new perspective for the puerarin-related drug research and development, clinical application, and further development and utilization.

Keywords: anti-inflammation; antioxidation; clinical studies; new drug delivery systems; pharmacokinetic; pharmacological activities; puerarin.

Figure 1

Partial mechanism of puerarin alleviating oxidative stress [9,11,12,13].

Figure 2

Mechanism of puerarin in improving ALI inflammation caused by gunpowder smog [45].

Figure 3

Mechanism of puerarin inhibiting the expression of pro-inflammatory cytokine IL-6 [64].

Figure 4

The mechanism of puerarin preventing cardiac fibrosis [99].

Figure 5

The mechanism of puerarin on immune cells.

Figure 6

Chemical structures of a series of puerarin derivatives [137,138,139,140,141,142,143].