Pharmacokinetic, Metabolism, and Metabolomic Strategies Provide Deep Insight Into the Underlying Mechanism of Ginkgo biloba Flavonoids in the Treatment of Cardiovascular Disease

Abstract

Ginkgo biloba, known as the “living fossil,” has a long history of being used as botanical drug for treating cardiovascular diseases and the content of flavonoids as high as 24%. More than 110 different kinds of flavonoids and their derivatives have been separated from G. biloba, including flavones, flavonols, biflavonoids, catechins, and their glycosides, etc., all of which display the ability to dilate blood vessels, regulate blood lipids, and antagonize platelet activating factor, and protect against ischemic damage. At present, many types of preparations based on G. biloba extract or the bioactive flavonoids of it have been developed, which are mostly used for the treatment of cardiovascular diseases. We herein review recent progress in understanding the metabolic regulatory processes and gene regulation of cellular metabolism in cardiovascular diseases of G. biloba flavonoids. First, we present the cardioprotective flavonoids of G. biloba and their possible pharmacological mechanism. Then, it is the pharmacokinetic and liver and gut microbial metabolism pathways that enable the flavonoids to reach the target organ to exert effect that is analyzed. In the end, we review the possible endogenous pathways toward restoring lipid metabolism and energy metabolism as well as detail novel metabolomic methods for probing the cardioprotective effect of flavonoids of G. biloba.

Uncovering the pharmacology of Ginkgo biloba folium in the cell-type-specific targets of Parkinson’s disease

“…G. biloba , a medicinal plant belonging to the Ginkgoaceae family, is considered the oldest tree alive in the world ( Chen et al, 2021 ). GBE has been used for medical purposes for centuries in various diseases, typically for cardiovascular conditions ( Li et al, 2018b ; Zhan et al, 2021 ; Tao et al, 2022 ). Commercialized GBE, EGB 761 ® , has a recognized neuroprotective role for cognitive impairment like Alzheimer’s disease (AD) ( Liu et al, 2019 ; Verma et al, 2020 ; Abdelmeguid et al, 2021 ; Ge et al, 2021 ; Zhao et al, 2021 ).…”

Flavonols and Flavones as Potential anti-Inflammatory, Antioxidant, and Antibacterial Compounds

“…Only aglycones forms were considered able to pass the gut wall, and no enzymes that can split these predominantly β -glycosidic bonds are secreted into the gut or present in the intestinal wall [ 84 ]. Unlike terpenes with high bioavailability, flavonoids can have low bioavailability due to the extensive first-pass effect and glucuronidation [ 85 ]. However, research on the mechanisms for aglycone transfer across the gut wall is lacking.…”

Effect of Ginkgo biloba extract on pharmacology and pharmacokinetics of atorvastatin in rats with hyperlipidaemia

“…[18][19][20] More than 110 different kinds of flavonoids and their derivatives have been isolated from ginkgo leaves, 21 all of which display the ability to dilate blood vessels, 22 regulate blood lipids, antagonize platelet activating factor, and protect against ischaemic damage. 23 At present, many types of preparations based on GBE or its bioactive flavonoids have been developed, and they are mostly used for the treatment of cardiovascular diseases.…”