Theaflavin 3,3'-digallate

Theaflavin-3,3'-digallate (TFDG) is a major polyphenol found in black tea with diverse biological activities.^1,2,3 It has antioxidant activity, inhibiting the formation of superoxide radicals, singlet oxygen, hydrogen peroxide, and hydroxyl radicals in vitro (IC₅₀s = 26.7, 0.83, 0.39, and 25.07 µmol/L, respectively).¹ It also reduces hydroxyl radical-induced damage to plasmid DNA. TFDG (12.5-50 µM) prevents LPS-induced release of TNF-α, IL-1β, and IL-6, expression of JNK and p38, and nuclear translocation of NF-κB in RAW 264.7 cells.² In vivo, TFDG reduces serum levels of TNF-α, IL-1β, and IL-6 and decreases pulmonary edema, pulmonary congestion, and thickening of the alveolar wall in a mouse model of LPS-induced acute lung injury. It also inhibits osteoclast formation, polarization, and osteoclastic bone resorption in vitro and reduces titanium particle-induced bone erosion and the number of mature osteoclasts in mice in a dose-dependent manner.³

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1. Wu, Y.-y., Li, W., Xu, Y., et al. Evaluation of the antioxidant effects of four main theaflavin derivatives through chemiluminescence and DNA damage analyses. J. Zhejiang. Univ. Sci. B. 12(9), 744-751 (2011).

2. Wu, Y., Jin, F., Wang, Y., et al. In vitro and in vivo anti-inflammatory effects of theaflavin-3,3'-digallate on lipopolysaccharide-induced inflammation. Eur. J. Pharmacol. 794(5), 52-60 (2017).

3. Hu, X., Ping, Z., Gan, M., et al. Theaflavin-3,3'-digallate represses osteoclastogenesis and prevents wear debris-induced osteolysis via suppression of ERK pathway. Acta. Biomater. 48(15), 479-488 (2017).