Proceedings of Chemistry, Pharmacology, Pharmacokinetics and Synthesis of Biflavonoids

Abstract

Biflavonoids, composed of two monoflavonoid residues, occur naturally in angiosperms, bryophytes, ferns, and gymnosperms. More than 592 biflavonoids have been structurally elucidated, and they can be classified into two groups of C-C and C-linear fragments-C, based on whether the linker between the two residues contains an atom. As the linker can be established on two arbitrary rings from different residues, the C-C type contains various subtypes, as does the C-linear fragment-C type. Biflavonoids have a wide range of pharmacological activities, including anti-inflammatory, antioxidant, antibacterial, antiviral, antidiabetic, antitumor, and cytotoxic properties, and they can be applied in Alzheimer’s disease and Parkinson’s disease. This review mainly summarizes the distribution and chemistry of biflavonoids; additionally, their bioactivities, pharmacokinetics, and synthesis are discussed.

Biflavonoids: Important Contributions to the Health Benefits of Ginkgo (Ginkgo biloba L.)

“…The first biflavonoid, ginkgentin, was isolated from ginkgo in 1929. as a yellow pigment [ 37 ] and since then, numerous biflavonoid compounds have been isolated from various plants. He et al [ 19 ] reported that more than 592 biflavonoids have been structurally elucidated, but the actual number is probably even higher. In ginkgo, 13 different biflavonoids have been described so far [ 18 ].…”

“…Biflavonoids are dimers of flavone–flavone, flavone–flavonone, flavonone–flavonone subunits, and in rare cases, dimers of chalcones and isoflavones. As summarized by He et al [ 19 ], a total of 592 biflavonoids are widely distributed in angiosperms, ferns, gymnosperms, and bryophytes, with most of them found in angiosperms. The vast majority of biflavonoids are from Clusiaceae, Thymelaeaceae, Ochnaceae, and Selaginellaceae, which account for about 50% of biflavonoids in all families [ 19 ].…”

“…As summarized by He et al [ 19 ], a total of 592 biflavonoids are widely distributed in angiosperms, ferns, gymnosperms, and bryophytes, with most of them found in angiosperms. The vast majority of biflavonoids are from Clusiaceae, Thymelaeaceae, Ochnaceae, and Selaginellaceae, which account for about 50% of biflavonoids in all families [ 19 ]. Their presence is frequently reported in plants used in traditional and modern medicine, indicating their potential health benefits.…”

“…Their presence is frequently reported in plants used in traditional and modern medicine, indicating their potential health benefits. Therefore, it is not surprising that biflavonoids have become the focus of scientific attention in recent years due to their pharmacological activities, including anti-inflammatory, antioxidant, antibacterial, antiviral, antidiabetic, antitumor, and cytotoxic properties, and may be used to treat Alzheimer’s and Parkinson’s disease [ 19 ]. To date, 13 different biflavonoids have been reported, of which ginkgetin, isoginkgetin, amentoflavone, bilobetin and sciadopitysin are the predominant biflavonoids [ 18 ].…”

Garcinia Biflavonoid 1 Improves Lipid Metabolism in HepG2 Cells via Regulating PPARα

“…Garcinia biflavonoid 1 (GB1, chemical structure as showed in Figure 1 F), the main active chemical composition of Garcinia kola , was reported to be capable of regulating glucose and lipid metabolism, inhibiting inflammation, and protecting the liver [ 10 , 11 , 12 , 13 , 14 ]. An animal experiment also identified the potential role of GB1 in the treatment of NAFLD, as it could decrease the blood glucose level induced by STZ in rabbits and was protective of the liver [ 15 ].…”