[Retracted] Theaflavin Chemistry and Its Health Benefits

Table 2

The pharmacological activities of theaflavin and its derivatives.

Theaflavins	In vitro/in vivo model	Results	Refs
TF3	Human ovarian cancer cells (A2780/CP70 and OVCAR3 cells)	Decreasing cell viability and upregulating the protein expression of caspase-3 and -7 in the cells	[12]
TF3 and (PGG)	LNCaP prostate cancer cells	Reduced androgen-responsive LNCaP prostate cancer cell growth, suppressed expression of the AR	[13]
TF3	Human ovarian cancer cells (OVCAR-3)	Activate extrinsic apoptosis in OVCAR-3 cells by inducing G0/G1 cell cycle arrest	[16]
TF-3	Human oral squamous carcinoma HSC-2 cells and normal GN46 fibroblasts	Induction of apoptotic cell death by elevated activity of caspase-3	[18]
TF3 and cisplatin	Human ovarian cancer cells (A2780/CP70 and OVCAR3 cells)	Combined treatment showed a synergistic cytotoxicity	[19]
TF3	Cisplatin-resistant ovarian cancer A2780/CP70 cells	G2 cell cycle arrest	[20]
Theaflavins (TF-1, TF-2, TF-3)	HepG2 cells, cell culture, and high-fat dietMale Wistar rats	Reduced lipid accumulation, suppressed fatty acid synthesis, and stimulated fatty acid oxidation	[34]
Theaflavins, EGCG	JB6 mouse epidermal cell line	Both inhibited UVB-induced AP-1 activation. Inhibitory effects of theaflavins were stronger than those of EGCG	[38]
TF-3	α Melanocyte-stimulating hormone (αMSH)-induced melanogenesis in mouse B16 melanoma cells	Showed inhibitory effect on melanogenesis due to suppression of tyrosinase protein and mRNA levels	[39]
Cofermented green tea with a high level of TFs	Human subcutaneous fat cells (hSCFs)	Promoted differentiation of hSCFs	[41]
Theaflavin	Mouse fatty liver model	Decreased liver steatosis, oxidative stress, inflammation, and hepatocyte apoptosis	[53]
TF3	HepG2 cells and HEK 293T cells	Reduced lipid droplet accumulation in hepatocytes, inhibited the activation of plasma kallikrein, and stimulate AMPK	[57]
TF1, TF2A, TF2B and TF3	Cell model of PC12 cells	Prevent oxidative stress by suppressing oxidant enzyme activity and downregulated the expression of caspase-3	[68]
TFs	Human neuroblastoma SH-SY5Y cells	Prevented 6-hydroxydopamine-induced loss of cell viability, condensed nuclear morphology, and apoptosis	[69]
TFs	MPTP/p induced neurodegenaration in C57BL/6 mice	Attenuates apoptosis and neurodegeneration	[70]
TFs	Influenza virus in vitro	Inhibitory effects against influenza virus	[71]
TF-2	Human colon cancer cells	Induced the upregulation of P53 and BAXand suppressed the COX-2 gene expression and also downregulated TNF-α, iNOS, ICAM-1, and NFκB	[72]
Theaflavin	Cerebral I/R injury in rats	Inhibited leukocyte infiltration and expression of ICAM-1, COX-2, and iNOS. Suppressing upregulation of iNOS and COX-2	[74]
TF3	Male C57BL/6 mice, bone marrow-derived macrophages and RAW264.7 murine acrophages	Inhibited osteolysis and prevented bone destruction. Suppressed osteoclast formation, polarization and osteoclastic bone resorption	[85]
TF3	Acute lung injury (ALI) in a mouse model. RAW 264.7 macrophages	Suppressed the phosphorylation of c-Jun N-terminal kinase and p38 MAPK,TNF-α, IL-1, and IL-6	[86]
TF1, TF2A, TF2B and TF3	Herpes simplex virus type 1 infected Vero and A549 cells	TF3 showed most strong anti-HSV-1 effect in both Vero and A549 cells	[133]
Theaflavin	C57/BL6 J model of I/R injury, hypoxia/reoxygenation (H/R) model of TCMK-1 cells	Inhibited I/R- and H/R-induced renal injury and cell apoptosis	[144]
Theaflavins and thearubigins	Arginine induced renal alfunction in rats	Significant reduction in lipid profile, glucose content, renal function tests and TBARS with enhancement in insulin, HDL, and hematological parameters	[149]
Catechins, theaflavins	C3(1) SV40 T,t antigen transgenic mouse model	The size of the largest tumor per mouse was decreased. Increased levels of cleaved caspase-3 in tumor tissue and increased apoptosis.	[150]
Mixture of TF3, TF2A, TF2B thearubigin, and EGCG	Lipopolysaccharide-activated murine macrophages, RAW 264.7 cells	TF3 exerted strong inhibiting effect on NO generation than EGCG	[151]