Abstract

Astragali radix (AR) is one of the most widely used traditional Chinese herbal medicines. Modern pharmacological studies and clinical practices indicate that AR possesses various biological functions, including potent immunomodulation, antioxidant, anti-inflammation and antitumor activities. To date, more than 200 chemical constituents have been isolated and identified from AR. Among them, isoflavonoids, saponins and polysaccharides are the three main types of beneficial compounds responsible for its pharmacological activities and therapeutic efficacy. After ingestion of AR, the metabolism and biotransformation of the bioactive compounds were extensive in vivo. The isoflavonoids and saponins and their metabolites are the major type of constituents absorbed in plasma. The bioavailability barrier (BB), which is mainly composed of efflux transporters and conjugating enzymes, is expected to have a significant impact on the bioavailability of AR. This review summarizes studies on the phytochemistry, pharmacology and pharmacokinetics on AR. Additionally, the use of AR as a personalized medicine based on the BB is also discussed, which may provide beneficial information to achieve a better and more accurate therapeutic response of AR in clinical practice.

Highlights

  • Astragali radix (AR), well-known as Huangqi in China, is one of the most popular herbal medicines that has been widely applied for over 2000 years in Chinese clinics

  • It was found that Astragalus polysaccharides (APS) could up-regulate the expression of galectin-1 in muscle of streptozotocin-induced Type 1 diabetes mellitus (T1DM) mice, resulting in the apoptosis of CD8 + T cells, which may be an important mechanism by which APS protects β cells of the pancreatic islets from apoptosis induced by CD8 + T cells in T1DM in vivo [89] (Figure 2 2 )

  • The results showed that three of the isoflavonoids, formononetin, ononin and calycosin could prevent the decrease in activity of antioxidant enzymes superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) and the depletion of GSH in glutamate-damaged PC12 cells, indicating that these compounds could protect PC12 cells from oxidative stress induced by glutamate

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Summary

Introduction

Astragali radix (AR), well-known as Huangqi in China, is one of the most popular herbal medicines that has been widely applied for over 2000 years in Chinese clinics. Because of the extensive use of AR in clinical practice and its effective pharmacological functions, a large number of studies on the pharmacokinetic characteristics of AR and its bioactive compounds have been performed [20,21,22]. These studies clearly provide an insight into the pharmacokinetic process of the bioactive compounds in AR in vivo, which may help provide beneficial information for the safe and effective application of AR. The use of AR as a personalized medicine based on the BB is discussed

Chemical Composition
Astragalus Triterpene Saponins
Astragalus Flavonoids
Other Constituents
Pharmacological Activities
Effects of AR and Its Main Components on Cardiovascular Diseases
Effects of AR and its Main Components on Diabetes Mellitus
Effects of AR and Its Main Components on T2DM
Effects of AR and Its Main Components on Cancer
Effects of AR and Its Main Components on Nervous System Diseases
Other Pharmacological Activities
Pharmacokinetic Studies on AR Extracts
Formononetin
Ononin
AR as Personalized Medicine
Findings
Conclusions and Future Prospects
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