To evaluate the antiviral activity of theaflavins against HSV-1, results showed that TF3 at 50 μM and above inhibited >99% of HSV-1 viral particle production.
Antiviral Res. 2015 Jun;118:56-67
Vero cells
75 µM
1 hour
To evaluate the antiviral activity of theaflavins against HSV-1, results showed that TF3 at 50 μM and above inhibited >99% of HSV-1 viral particle production.
Antiviral Res. 2015 Jun;118:56-67
CV-1 cells
250-500 µM
1 hour
Assess the inactivation effect of TF-3 on HSV-1 clinical isolates. Results indicated that some HSV-1 clinical isolates required higher concentrations of TF-3 (250-500 μM) to achieve comparable inactivation to HSV-2.
Evaluate the efficacy of TF-3 combined with lactic acid (LA) in inactivating HSV-1 and HSV-2 at various pH levels. Results showed that TF-3 combined with LA almost completely inactivated clinical isolates of HSV-2 and HSV-1 at pH 4.5 to 5.7.
Theaflavin-3,3'-digallate (TF-3) reduced the impact of methylmercury by maintaining the adipocytes morphology and secretion patterns of adiponectin, resistin and 4-hydroxynonenal. TF-3 showed dose-dependent effects in counteracting methylmercury-induced oxidative stress and inflammation.
Int J Mol Sci. 2019 Jun 5;20(11):2755
H9c2 cells
1-10 µM
24 hours
Prevention of angiotensin II-induced pathological cardiac hypertrophy via inhibition of the CaN-NFAT signaling pathway
Nutrients. 2022 Mar 26;14(7):1391
Peritoneal macrophages
40 µM
24 hours
To evaluate the inhibitory effect of TFDG on NO production in LPS-activated macrophages. Results showed that TFDG downregulated NO production in a concentration-dependent manner, with maximal effect at 40 μM and no cytotoxicity observed.
Br J Pharmacol. 2006 Sep;149(1):121-31
Human ovarian carcinoma cells OVCAR-3
10-20 µM
24 hours
TF3 significantly reduced the viability of OVCAR-3 cells and induced apoptosis and G0/G1 cell cycle arrest.
Molecules. 2019 Feb 14;24(4):673
Demineralized dentin collagen
12.5, 25, 50, 100 mg/mL
30 and 60 seconds
TF3/ethanol solution could effectively crosslink demineralized dentin collagen and improve its resistance to collagenase digestion and biomechanical properties (p<0.05), showing concentration and time dependence. The effect of 25 and 50 mg/ml TF3/ethanol solution was similar to that of 5% GA, whereas the 100 mg/mL TF3/ethanol solution exhibited better performance (p<0.05).
Front Bioeng Biotechnol. 2024 May 15;12:1401032
Rat aortic rings
0.02–2 µM
30 minutes
To investigate the vasorelaxation induced by theaflavin-3,3'-digallate and its mechanism, it was found that it mediates NO-dependent vasodilation through the production of hydrogen peroxide (H2O2).
Antioxidants (Basel). 2020 May 7;9(5):390
Rat aortic endothelial cells (RAECs)
0.5 μg/mL
30 minutes
TF3 suppressed Hcy-induced ER stress markers (e.g., phosphorylated eIF2α, ATF3, and cleaved ATF6) and reduced ROS production.
Sci Rep. 2015 May 15;5:10340
Rat aortic smooth muscle cells (RASMCs)
1, 10, 20 µM
48 hours
To evaluate the effect of TF3 on PDGF-BB-induced migration in RASMCs. Wound healing and Transwell assays showed that TF3 inhibited PDGF-BB-induced migration in a concentration-dependent manner.
Front Pharmacol. 2022 Jul 12;13:861319
Rat aortic smooth muscle cells (RASMCs)
1, 10, 20 µM
48 hours
To evaluate the effect of TF3 on PDGF-BB-induced proliferation in RASMCs. EdU and CCK-8 assays showed that TF3 inhibited PDGF-BB-induced proliferation in a concentration-dependent manner.
Front Pharmacol. 2022 Jul 12;13:861319
Rat aortic smooth muscle cells (RASMCs)
1, 10, 20 µM
48 hours
To evaluate the effect of TF3 on PDGF-BB-induced phenotypic switching in RASMCs. Results showed that TF3 reversed the PDGF-BB-induced decrease in contractile proteins (MYH11, α-SMA, and SM22) in a concentration-dependent manner.
Front Pharmacol. 2022 Jul 12;13:861319
Purified F1-ATPase
0.7 µM
5 minutes
To evaluate the inhibitory effect of Theaflavin 3,3'-digallate on purified F1-ATPase, results showed an IC50 value of 0.7 μM and an inhibition rate of 90%.
J Nutr Biochem. 2012 Aug;23(8):953-60
E. coli membrane vesicles
10-20 µM
5 minutes
To evaluate the inhibitory effect of Theaflavin 3,3'-digallate on ATP hydrolysis, results showed an IC50 value of 10 μM and an inhibition rate of 90%.
J Nutr Biochem. 2012 Aug;23(8):953-60
MC3T3-E1 cells
0.1 µM and 1 µM
7 days
TFDG promotes the formation of osteoblasts and enhances their mineralization ability in inflammatory environment
Front Pharmacol. 2021 Mar 23;12:648969
Theaflavin 3,3'-digallate/茶黄素-3,3'-双没食子酸 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Zebrafish (Danio rerio)
Alloxan-induced diabetic model
Water solution treatment
0.5-20 μg/mL
24 hours
To evaluate the hypoglycemic effect and mechanism of TF3 in diabetic zebrafish, results showed that TF3 could significantly reduce blood glucose levels by down-regulating PEPCK and up-regulating GCK expression, and promote β cells regeneration at low concentrations.
Nutrients. 2021 Dec 7;13(12):4379
C57BL/6 mice
Ovariectomy-induced osteoporosis model
Injection
1 mg/kg and 10 mg/kg
Every 2 days for 5 weeks
TFDG significantly increased bone mass in ovariectomized mice, reduced the release of proinflammatory cytokines, and increased the expression of osteogenic markers
Front Pharmacol. 2021 Mar 23;12:648969
DBA/1 mice
Collagen-induced arthritis (CIA) model
Intraperitoneal injection
1 mg/kg or 10 mg/kg
6 days a week for 8 weeks
To investigate the effect of TFDG on CIA mice. Results showed that TFDG ameliorated joint destruction, reduced inflammatory cytokines, and promoted M2 macrophage polarization.
J Inflamm Res. 2023 Jan 10;16:109-126
C57BL/6J female mice
Ovariectomy (OVX)-induced osteoporosis model
Intraperitoneal injection
1 mg/kg, 10 mg/kg
Three times per week for 3 months
To evaluate the effect of TF3 on OVX-induced bone loss. Results showed that TF3 significantly attenuated OVX-induced bone loss and osteoclastogenesis in a dose-dependent manner.
Front Pharmacol. 2020 Jun 29;11:803
C57BL/6 mice
Carotid artery ligation model
Intraperitoneal injection
10 mg/kg
Injected one day before surgery and repeated every other day for 14 or 28 days
To evaluate the effect of TF3 on carotid artery ligation-induced neointimal hyperplasia. Results showed that TF3 significantly reduced the intima-to-media ratio (I/M ratio) and increased lumen diameter and area.
Front Pharmacol. 2022 Jul 12;13:861319
Chicken embryos
Chick chorioallantoic membrane (CAM) model
Implanted onto the CAM
25 µM
Single administration, lasting for 5 days
To evaluate the inhibitory effect of TF3 on tumor angiogenesis in vivo, results showed that TF3 significantly reduced blood vessel density.
Int J Oncol. 2016 Jan;48(1):281-92
Mice
Leptin-deficient obese (ob/ob) mice
Intraperitoneal injection
5 mg/kg, 10 mg/kg, 20 mg/kg
Once daily for 4 weeks
TF3 treatment prevented body weight and waistline gain, reduced lipid accumulation, and alleviated liver function injury, as well as decreased serum lipid levels and TG levels in livers.
Front Pharmacol. 2022 Aug 29;13:925264
BALB/c mice
TNBS-induced colitis model
Oral gavage
5 mg/kg/day
Once daily for 18 days
To evaluate the protective effect of TFDG on TNBS-induced colitis. Results showed that TFDG significantly improved macroscopic and microscopic damage scores, reduced neutrophil infiltration, decreased mRNA and protein levels of proinflammatory cytokines (TNF-α, IL-12, IFN-γ) and iNOS, and preserved IκBα by inhibiting IKK activity and nuclear translocation of NF-κB.
Br J Pharmacol. 2006 Sep;149(1):121-31
BALB/c mice
S aureus pneumonia model
Hypodermic injection
50 mg/kg TFDG, 15 mg/kg cephalothin
Every 12 hours for 72 hours
Evaluate the protective effect of TFDG combined with cephalothin against S aureus pneumonia in mice, showing that the combination significantly reduced mortality and alleviated lung pathological changes.
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