4.6 Review

Atractylenolides (I, II, and III): a review of their pharmacology and pharmacokinetics

Journal

ARCHIVES OF PHARMACAL RESEARCH
Volume 44, Issue 7, Pages 633-654

Publisher

PHARMACEUTICAL SOC KOREA
DOI: 10.1007/s12272-021-01342-6

Keywords

Atractylenolides; Pharmacology; Pharmacokinetics; Safety

Funding

  1. Department of Science and Technology of Sichuan Province [2020095, 2019YFS0113]

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Atractylenolides derived from Atractylodes macrocephala Koidz have shown various pharmacological activities such as anti-cancer, anti-inflammatory, and neuroprotective effects. Further clinical studies are recommended to explore their therapeutic effects and potential side effects when combined with other drugs.
Atractylodes macrocephala Koidz is a widely used as a traditional Chinese medicine. Atractylenolides (-I, -II, and -III) are a class of lactone compounds derived from Atractylodes macrocephala Koidz. Research into atractylenolides over the past two decades has shown that atractylenolides have anti-cancer, anti-inflammatory, anti-platelet, anti-osteoporosis, and antibacterial activity; protect the nervous system; and regulate blood glucose and lipids. Because of structural differences, both atractylenolide-I and atractylenolide-II have remarkable anti-cancer activities, and atractylenolide-I and atractylenolide-III have remarkable anti-inflammatory and neuroprotective activities. We therefore recommend further clinical research on the anti-cancer, anti-inflammatory and neuroprotective effects of atractylenolides, determine their therapeutic effects, alone or in combination. To investigate their ability to regulate blood glucose and lipid, as well as their anti-platelet, anti-osteoporosis, and antibacterial activities, both in vitro and in vivo studies are necessary. Atractylenolides are rapidly absorbed but slowly metabolized; thus, solubilization studies may not be necessary. However, due to the inhibitory effects of atractylenolides on metabolic enzymes, it is necessary to pay attention to the possible side effects of combining atractylenolides with other drugs, in clinical application. In short, atractylenolides have considerable medicinal value and warrant further study.

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