Alpinetin: A Review of Its Pharmacology and Pharmacokinetics

Abstract

Flavonoids isolated from medicinal herbs have been utilized as valuable health-care agents due to their virous biological applications. Alpinetin is a natural flavonoid that emerges in many widely used medicinal plants, and has been frequently applied in Chinese patent drugs. Accumulated evidence has demonstrated that alpinetin possesses a broad range of pharmacological activities such as antitumor, antiinflammation, hepatoprotective, cardiovascular protective, lung protective, antibacterial, antiviral, neuroprotective, and other properties through regulating multiple signaling pathways with low systemic toxicity. However, pharmacokinetic studies have documented that alpinetin may have poor oral bioavailability correlated to its extensive glucuronidation. Currently, the reported pharmacological properties and pharmacokinetics profiles of alpinetin are rare to be scientifically reviewed. In this article, we aimed to highlight the mechanisms of action of alpinetin in various diseases to strongly support its curative potentials for prospective clinical applications. We also summarized the pharmacokinetics properties and proposed some viable strategies to convey an appreciable reference for future advances of alpinetin in drug development.

UHPLC-Q-Orbitrap-MS-Based Metabolomics Reveals Chemical Variations of Two Types of Rhizomes of Polygonatum sibiricum

“…This natural flavonoid has also been reported to exist in Polygonatum ferruginea [ 38 ]. Alpinetin is one of the major active compounds of Chinese patent drugs such as Jianweizhitong tablet, Fufangcaodoukou tincture, Baikoutiaozhong pill, and Xingqiwenzhong granule [ 39 ]. Recently, Zhao et al [ 39 ] systematically reviewed the pharmacological activities of alpinetin, including the counteraction against cardiovascular disease, inflammatory diseases, carcinoma, bacterial and virus infection, and neuro-disorders.…”

“…Alpinetin is one of the major active compounds of Chinese patent drugs such as Jianweizhitong tablet, Fufangcaodoukou tincture, Baikoutiaozhong pill, and Xingqiwenzhong granule [ 39 ]. Recently, Zhao et al [ 39 ] systematically reviewed the pharmacological activities of alpinetin, including the counteraction against cardiovascular disease, inflammatory diseases, carcinoma, bacterial and virus infection, and neuro-disorders. Regarding grandisin, it is a tetrahydrofuran neolignan, isolated from Piper solmsianum [ 40 ], and Virola surinamensis [ 41 ], with the pharmacological activities of antinociception and anti-inflammation [ 41 ].…”

Dual effects of cardamonin/alpinetin and their acrolein adducts on scavenging acrolein and the anti-bacterial activity from Alpinia katsumadai Hayata as a spice in roasted meat

“…Previous studies have shown that CAR and ALP have antibacterial activity, 22,33 and we wondered about the antibacterial activity of CAR/ALP after trapping ACR. Therefore, we investigated the antibacterial activity of the adducts.…”

Traditional Chinese Medicine Regulates Th17/Treg Balance in Treating Inflammatory Bowel Disease

“…Simultaneous activation of AhR transcription factors, by upregulating cytochromeP4501A1 levels, increases Foxp3 expression, causes Treg cells differentiation, and comprehensively regulates 17/Treg balance through these two pathways [53][54][55]. Alpinetin is a flavonoid isolated from Alpinia officinarum Hance, which has hepatoprotective, cardiovascular, antibacterial, antiviral, and neuroprotective effects and is widely used in medicine [56,57]. Studies have confirmed that Alpinetin promotes Treg cells differentiation and restores 17/Treg balance by activating AhR, promoting miR-302 expression, while downregulating DNA methyltransferase-1 expression, reducing Foxp3 promoter region methylation levels, promoting cAMP-response element binding protein binding to Foxp3 promoter region, and upregulating Foxp3 expression, further improving intestinal mucosal pathological outcomes in colitic mice, including alleviating surface epithelial damage and significantly reducing crypt number and inflammatory cell infiltration [58].…”