Advances for pharmacological activities of Polygonum cuspidatum - A review

Abstract

Context: Polygonum cuspidatum Sieb. et Zucc (Polygonaceae), the root of which is included in the Chinese Pharmcopoeia under the name 'Huzhang', has a long history as a medicinal plant and vegetable. Polygonum cuspidatum has been used in traditional Chinese medicine for the treatment of inflammation, hyperlipemia, etc.

Objective: This article reviews the pharmacological action and the clinical applications of Polygonum cuspidatum and its extracts, whether in vivo or in vitro. We also summarized the main phytochemical constituents and pharmacokinetics of Polygonum cuspidatum and its extracts.

Methods: The data were retrieved from major medical databases, such as CNKI, PubMed, and SinoMed, from 2014 to 2022. Polygonum cuspidatum, pharmacology, toxicity, clinical application, and pharmacokinetics were used as keywords.

Results: The rhizomes, leaves, and flowers of Polygonum cuspidatum have different phytochemical constituents. The plant contains flavonoids, anthraquinones, and stilbenes. Polygonum cuspidatum and the extracts have anti-inflammatory, antioxidation, anticancer, heart protection, and other pharmacological effects. It is used in the clinics to treat dizziness, headaches, traumatic injuries, and water and fire burns.

Conclusions: Polygonum cuspidatum has the potential to treat many diseases, such as arthritis, ulcerative colitis, asthma, and cardiac hypertrophy. It has a broad range of medicinal applications, but mainly focused on root medication; its aerial parts should receive more attention. Pharmacokinetics also need to be further investigated.

Keywords: Chinese herb; Huzhang; anti-inflammatory; anticancer; heart protection; pharmacokinetics.

Figure 1.

The main mechanism of anti-inflammatory effect of Polygonum cuspidatum. (a) In Raw 264.7 cells, the extract of Polygonum cuspidatum can decrease the expression of MCP-1, miR155 and the pathway of NF-κB/JNK/STAT directly, and also suppress the expression of IL-1β, IL-6 and NO, as well increase the expression of SOCS1. (b) The extract of Polygonum cuspidatum can also treat arthritis in different pathways. It can increase the expression of PPAR-γ, and then the IL-17 as well as p65 are inhibited. In addition, whether the NLRP3/ASC/Caspase-1 or the Wnt/β-catenin pathway can be activated by this plant, their downstream factors, such as IL-1β, TNF-α, HIF-1α, iNOS and NO are induced.

Figure 2.

The main mechanism of the antioxidant effect of Polygonum cuspidatum Sieb. et Zucc. The component of this plant can inhibit the expression of p38 MAPK and Keap1, then Nrf2 is upregulated, which will activate the ARE gene, further induce the expression of ROS, MDA, CAT and TGF-β1.