Chemical Constitution, Pharmacological Effects and the Underlying Mechanism of Atractylenolides: A Review

Abstract

Atractylenolides, comprising atractylenolide I, II, and III, represent the principal bioactive constituents of Atractylodes macrocephala, a traditional Chinese medicine. These compounds exhibit a diverse array of pharmacological properties, including anti-inflammatory, anti-cancer, and organ-protective effects, underscoring their potential for future research and development. Recent investigations have demonstrated that the anti-cancer activity of the three atractylenolides can be attributed to their influence on the JAK2/STAT3 signaling pathway. Additionally, the TLR4/NF-κB, PI3K/Akt, and MAPK signaling pathways primarily mediate the anti-inflammatory effects of these compounds. Atractylenolides can protect multiple organs by modulating oxidative stress, attenuating the inflammatory response, activating anti-apoptotic signaling pathways, and inhibiting cell apoptosis. These protective effects extend to the heart, liver, lung, kidney, stomach, intestine, and nervous system. Consequently, atractylenolides may emerge as clinically relevant multi-organ protective agents in the future. Notably, the pharmacological activities of the three atractylenolides differ. Atractylenolide I and III demonstrate potent anti-inflammatory and organ-protective properties, whereas the effects of atractylenolide II are infrequently reported. This review systematically examines the literature on atractylenolides published in recent years, with a primary emphasis on their pharmacological properties, in order to inform future development and application efforts.

Role of traditional Chinese medicine in age-related macular degeneration: exploring the gut microbiota’s influence

“…Atractylodes macrocephala , commonly referred to as “Yuzhu,” “Xizhu,” or “Wuzhu,” functions as the desiccated rhizome of A. macrocephala within the Asteraceae family. Atractylodes macrocephala contains sesquiterpenes, lactones, polysaccharides, flavonoids, and other chemical components that have antioxidant, anti-apoptosis, and anti-inflammatory effects, improve gastrointestinal function and immunity, and lowers blood lipids ( Xie et al, 2023 ). In a study involving a macular edema formula containing A. macrocephala , the total volume of the macular center area in diameter of the patients was significantly reduced, and the visual acuity and visual field were significantly improved ( Zhu et al, 2016 ).…”

Phytochemistry and Pharmacology of Sesquiterpenoids from Atractylodes DC. Genus Rhizomes

“…Zhang et al [44] identified atramacronoids A-C (18)(19)(20) from the rhizomes of A. macrocephala using spectroscopic data analysis, chemical calculations, and X-ray diffraction, which were found to contain an unusual 6/6/5/5/6 skeleton furnished by an unexpected C-8-C-16 linkage. Subsequently, twenty undescribed eudesmane-type sesquiterpenes named atramacronoids D-W (21)(22)(23)(24)(25)(26)(27)(28)(29)(30)(31)(32)(33)(34)(35)(36)(37)(38)(39)(40) were identified in the rhizomes of A. macrocephala using extensive spectroscopic data analysis, Snatzke's rule, ECD calculations, and X-ray crystallographic analysis [45,46]. A chemical investigation of the ethanol extract of A. lancea resulted in the isolation of nine eudesmanetype sesquiterpenoids (41)(42)(43)(44)(45)(46)(47)(48)(49), and their structures were elucidated using spectroscopic techniques and HRESIMS [47].…”

“…[ 13 , 14 , 15 ]. According to the diverse skeletal structures of sesquiterpenes in Atractylodes DC., they can be divided into the following five categories: eudesmane-type (such as β -eudesmol, atractylon), guaiane-type (such as atractylmacrol A, atrchiterpene D), spirovetivane-type (such as hinesol, hinesolone), isopterocarpolone-type (such as 14-hydroxy-isopterocarpolone, Atractyloside I), and eremophilane-type [ 10 , 16 , 17 , 18 , 19 , 20 , 21 ]. β -eudesmol, atractylon, and hinesol are usually used as chemical markers for evaluating the quality of Atractylodes DC.…”