Theaflavin (TF) is a suitable natural inhibitor against influenza A (H1N1) neuraminidase. Theaflavin, found in green tea, is observed to inhibit H1N1 NA proteins strongly supported by lowest docking energy. Theaflavin is a plant product traditionally used for treatment of influenza infection. Theaflavin derivatives have shown pronounced antiviral activity[3]. Theaflavin was strong inhibitors of OATP (Organic anion-transporting polypeptide) 2B1-mediated E3S uptake. Theaflavin showed a significantly higher uptake into the OATP2B1-expressing HEK293 cells than the control cells. The concentration dependence of the uptake of theaflavin was determined over a range of concentrations (0.5-100 μM) and the kinetic parameters (Km and Vmax) of theaflavin uptake were found to be 5.12 ± 0.67 μM and 41.6 ± 1.3 pmol/mg protein/min, respectively[4]. TF improved survival of irradiated wild-type mice and ameliorated TBI-induced (total body irradiation) hematopoietic injury by attenuating myelosuppression and myeloid skewing, increasing HSC (hematopoietic stem cell) frequency, and promoting reconstitution of irradiated HSCs. Furthermore, TF inhibited TBI-induced HSC senescence[5].
Theaflavin/茶黄素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
BMDMs
50, 100, 200 µM
1 hour
Theaflavin dose-dependently inhibited NLRP3 inflammasome activation induced by ATP or nigericin, as evidenced by reduced release of caspase-1p10 and mature IL-1β.
Acta Pharmacol Sin. 2023 Oct;44(10):2019-2036.
J774A.1 cells
50, 100, 200 µM
1 hour
Theaflavin dose-dependently inhibited NLRP3 inflammasome activation induced by ATP or nigericin, as evidenced by reduced release of caspase-1p10 and mature IL-1β.
Acta Pharmacol Sin. 2023 Oct;44(10):2019-2036.
3T3-L1 adipocytes
100 µM
10 days
To evaluate the effects of theaflavin-3,3'-digallate on methylmercury-exposed 3T3-L1 adipocytes. Results showed that 100 µM TF-3 partially restored adipocyte morphology and adipokine secretion patterns.
Int J Mol Sci. 2019 Jun 5;20(11):2755
3T3-L1 adipocytes
50 µM
10 days
To evaluate the effects of theaflavin-3,3'-digallate on methylmercury-exposed 3T3-L1 adipocytes. Results showed that 50 µM TF-3 partially restored adipocyte morphology and adipokine secretion patterns.
Int J Mol Sci. 2019 Jun 5;20(11):2755
3T3-L1 adipocytes
25 µM
10 days
To evaluate the effects of theaflavin-3,3'-digallate on methylmercury-exposed 3T3-L1 adipocytes. Results showed that 25 µM TF-3 significantly restored adipocyte morphology and adipokine secretion patterns.
Int J Mol Sci. 2019 Jun 5;20(11):2755
3T3-L1 adipocytes
12.5 µM
10 days
To evaluate the effects of theaflavin-3,3'-digallate on methylmercury-exposed 3T3-L1 adipocytes. Results showed that 12.5 µM TF-3 partially restored adipocyte morphology and adipokine secretion patterns.
Int J Mol Sci. 2019 Jun 5;20(11):2755
3T3-L1 adipocytes
6.25 µM
10 days
To evaluate the effects of theaflavin-3,3'-digallate on methylmercury-exposed 3T3-L1 adipocytes. Results showed that 6.25 µM TF-3 significantly improved adipocyte morphology and adipokine secretion patterns.
Int J Mol Sci. 2019 Jun 5;20(11):2755
3T3-L1 adipocytes
3.14 µM
10 days
To evaluate the effects of theaflavin-3,3'-digallate on methylmercury-exposed 3T3-L1 adipocytes. Results showed that 3.14 µM TF-3 partially restored the morphological changes and adipokine secretion patterns induced by methylmercury.
Int J Mol Sci. 2019 Jun 5;20(11):2755
HK-2 cells
20 and 50 μg/ml
2 hours pretreatment followed by 24 hours
To evaluate the protective effect of theaflavin on COM-induced oxidative stress injury in renal tubular epithelial cells. Results showed that theaflavin significantly enhanced SOD activity, reduced LDH, MDA, and H2O2 levels, decreased intracellular ROS generation, and upregulated SIRT1 expression.
Int J Biol Sci. 2021 Mar 2;17(4):1050-1060
Human subcutaneous fat cells (hSCF)
0.5 to 2 μg/mL (TF and TFDG)
21 days
To assess the effects of theaflavin on adipocyte differentiation. Results showed that theaflavin (TF) increased intracellular lipid droplet formation at concentrations ranging from 0.5 to 2 μg/mL, while theaflavin-3,3'-digallate (TFDG) inhibited lipid droplet formation.
Int J Mol Sci. 2019 Apr 25;20(8):2034
Human subcutaneous fat cells (hSCF)
1 to 5 μg/mL
24 and 72 hours
To evaluate the effects of theaflavin on cell proliferation and viability. Results showed that theaflavin increased cell proliferation after 24 h, and no cytotoxicity was observed after 72 h, with a slight increase in cell viability in some cases.
Int J Mol Sci. 2019 Apr 25;20(8):2034
A875 melanoma cells
240 µg/ml (464.7 µM)
24 hours
To evaluate the effect of theaflavin on another melanoma cell line. Results showed that theaflavin significantly inhibited the viability of A875 cells.
Front Pharmacol. 2020 Aug 31;11:1317
HFF-1 skin fibroblasts
240 µg/ml (464.7 µM)
24 hours
To evaluate the effect of theaflavin on normal cells. Results showed that theaflavin had little effect on the viability of HFF-1 cells.
Front Pharmacol. 2020 Aug 31;11:1317
Human umbilical vein endothelial cells (HUVECs)
0, 25, 50 µM
24 hours
To evaluate the protective effect of Theaflavin on TBHP-induced oxidative stress. Results showed that Theaflavin alleviated apoptosis and cell dysfunction and activated the PI3K/AKT/Nrf2 signaling pathway.
Front Bioeng Biotechnol. 2022 Mar 2;10:830574
A375 human melanoma cells
50-400 µg/ml (96.8-744.4 µM)
24, 48, 72 hours
To evaluate the anti-proliferative and pro-apoptotic effects of theaflavin on melanoma cells. Results showed that theaflavin significantly inhibited the proliferation of A375 cells in a concentration-dependent manner, with IC50 values of 218.9 µg/ml (423.8 µM) at 24 hours and 84.9 µg/ml (164.4 µM) at 72 hours.
Front Pharmacol. 2020 Aug 31;11:1317
Porcine nasopharyngeal epithelial cell Nptr
256 µg/mL (1/2 MIC)
30 minutes
Evaluate the effect of theaflavin on the adhesion ability of Streptococcus suis SC19, results showed significantly reduced adhesion
Int J Mol Sci. 2023 Apr 18;24(8):7442
Porcine nasopharyngeal epithelial cell Nptr
128 µg/mL (1/4 MIC)
30 minutes
Evaluate the effect of theaflavin on the adhesion ability of Streptococcus suis SC19, results showed reduced adhesion
Int J Mol Sci. 2023 Apr 18;24(8):7442
Porcine nasopharyngeal epithelial cell Nptr
512 µg/mL
30 minutes
Evaluate the cytotoxicity of theaflavin on Nptr cells, results showed no cytotoxicity
Int J Mol Sci. 2023 Apr 18;24(8):7442
Drosophila intestinal cells
1 mg/mL and 2.5 mg/mL
Continuous feeding
Theaflavins extend Drosophila lifespan and increase climbing ability
iScience. 2021 Feb 6;24(3):102150
Theaflavin/茶黄素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Larval zebra fishes
A375 xenograft model
Dissolved in culture medium
0.22, 0.67, 2.0 mg/ml (0.4, 1.3, 3.9 µM)
24 hours
To evaluate the inhibitory effect of theaflavin on melanoma growth in vivo. Results showed that theaflavin significantly inhibited A375 tumor growth in larval zebra fishes, with an inhibitory rate of 46.4% at 2.0 mg/ml (3.9 μM), outperforming cisplatin.
Front Pharmacol. 2020 Aug 31;11:1317
Drosophila melanogaster
W1118 Drosophila
Dietary supplementation
1 mg/mL and 2.5 mg/mL
Continuous feeding
Theaflavins extend Drosophila lifespan and increase climbing ability
iScience. 2021 Feb 6;24(3):102150
Male albino Wistar rats
High fat diet and streptozotocin-induced diabetic rat model
Oral
100 mg/kg b.w/day
Once daily for 30 days
To evaluate the effect of theaflavin on the activities of key enzymes of carbohydrate metabolism in high fat diet and streptozotocin-induced diabetic rats. The results showed that theaflavin significantly ameliorated plasma glucose, insulin levels, HOMA-IR index, HbA1c, and glycogen content in liver and muscle. Additionally, theaflavin reduced lipid peroxidation markers (TBARS and hydroperoxides) and enhanced the activities of antioxidant enzymes.
Redox Rep. 2019 Dec;24(1):41-50
Sprague-Dawley rats
Full-thickness skin wound model
Oral
20 mg/kg
Once daily until the end of the experiment
To evaluate the promoting effect of Theaflavin on wound healing. Results showed that Theaflavin enhanced vascularization in regenerated tissues and accelerated wound healing.
Front Bioeng Biotechnol. 2022 Mar 2;10:830574
C57BL/6J male mice
CaOx nephrocalcinosis mouse model
Gavage
20, 50, and 100 mg/kg
Once daily for 14 days
To evaluate the protective effect of theaflavin on CaOx-induced kidney oxidative stress injury and crystal deposition. Results showed that theaflavin significantly reduced crystal deposition, alleviated tissue damage and apoptosis, and improved oxidative stress status.
Int J Biol Sci. 2021 Mar 2;17(4):1050-1060
C57BL/6J mice
MSU-induced peritonitis model
Oral
250 mg/kg
Once daily for three consecutive days
Theaflavin significantly attenuated MSU-induced peritonitis in mice, as shown by reduced levels of IL-1β and IL-6 in peritoneal lavage fluids and decreased neutrophil infiltration.
Acta Pharmacol Sin. 2023 Oct;44(10):2019-2036.
Sprague-Dawley rats
Middle cerebral artery occlusion (MCAO) model
Intravenous injection
5, 10, and 20 mg/kg
Single administration, lasting 24 hours
Theaflavin significantly protected neurons from cerebral ischemia-reperfusion injury by limiting leukocyte infiltration and expression of ICAM-1, and suppressing upregulation of inflammatory-related prooxidative enzymes (iNOS and COX-2) in ischemic brain via, at least in part, reducing the phosphorylation of STAT-1.
Mediators Inflamm. 2006;2006(5):30490
Kun-Ming mice
Streptococcus suis SC19 infection model
Intragastrically
50 mg/kg
Single administration, observed for 7 days post-infection
Evaluate the protective effect of theaflavin on infected mice, results showed survival rate increased to 40% and clinical symptoms were alleviated
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