Health Benefits
1. Skin cancer
In the investigation of the tumor-inhibiting property of black tea polyphenol, theaflavin, found that The treatment of theaflavin downregulated the gelatinolytic activity, mRNA and protein expression of MMP-2. It reduced the mRNA and protein expression of membrane type-1 MMP (MT1-MMP) and induced mRNA and protein expression of tissue inhibitor of MMP-2 (TIMP-2), suggesting theaflavin's inhibitory effect on MMP-2 activation. Theaflavin reduced the binding of A375 cell to ECM ligands demonstrating that theaflavin treatment hinders cell-ECM adhesion, cell motility, and integrin-mediated MMP-2 activation, according to "Black tea polyphenol (theaflavin) downregulates MMP-2 in human melanoma cell line A375 by involving multiple regulatory molecules" by Sil H, Sen T, Moulik S, Chatterjee A.(1)
2. Anti cancers
In the review of anti-tumor p53 functions by dietary plant polyphenols particularly black tea and its active component theaflavins, by dietary plant polyphenols particularly black tea and its active component theaflavins has gained immense recognition from the point of view of both efficacy and safety, indicated that the review discusses about the possible role of theaflavin-p53 cross talk in targeting CSCs. Such attempts to target the complexities of p53 functions during neogenesis will be of immense help in developing a "new" strategy for successful cancer prevention and therapy by theaflavins, according to "Operation 'p53 Hunt' to combat cancer: Theaflavins in action" by Mohanty S, Adhikary A, Chakrabarty S, Sa G, Das T.(2)
3. Anti-oxidant, anti-inflammatory, and anti-apoptotic activities
In the investigation of the role of theaflavin, a polyphenol substance extracted from black tea, in attenuating acute I/R injury in a fatty liver model, found that theaflavin significantly diminished the ROS production of steatotic hepatocytes and TNF-α production by LPS-stimulated RAW264.7 cells and concluded that theaflavin has protective effects against I/R injury in fatty livers by anti-oxidant, anti-inflammatory, and anti-apoptotic mechanisms, according to "Theaflavin attenuates ischemia-reperfusion injury in a mouse fatty liver model" by
Luo XY, Takahara T, Hou J, Kawai K, Sugiyama T, Tsukada K, Takemoto M, Takeuchi M, Zhong L, Li XK.(3)
4. HIV-1 infection
In the investigation of the mechanism by which TFmix inhibits HIV-1 infection was investigated using time-of-addition, found that TFmix is an economic natural product preparation containing high content of theaflavins with potent anti-HIV-1 activity by targeting the viral entry step through the disruption of gp41 6-HB core structure. It has a potential to be developed as a safe and affordable topical microbicide for preventing sexual transmission of HIV, according to "A natural theaflavins preparation inhibits HIV-1 infection by targeting the entry step: Potential applications for preventing HIV-1 infection" by Yang J, Li L, Tan S, Jin H, Qiu J, Mao Q, Li R, Xia C, Jiang ZH, Jiang S, Liu S.(4)
5. Cholesterol
In the investigation of 240 men and women 18 years or older on a low-fat diet with mild to moderate hypercholesterolemia were randomly assigned to receive a daily capsule containing theaflavin-enriched green tea extract (375 mg) or placebo for 12 weeks, found that after 12 weeks, the mean ± SEM changes from baseline in total cholesterol, LDL-C, HDL-C, and triglyceride levels were -11.3% ± 0.9% (P = .01), -16.4% ± 1.1% (P = .01), 2.3% ± 2.1% (P = .27), and 2.6% ± 3.5% (P = .47), respectively, in the tea extract group. The mean levels of total cholesterol, LDL-C, HDL-C, and triglycerides did not change significantly in the placebo group. No significant adverse events were observed, according to "Cholesterol-Lowering Effect of a Theaflavin-Enriched Green Tea Extract" by David J. Maron, MD; Guo Ping Lu, MD; Nai Sheng Cai, MD; Zong Gui Wu, MD; Yue Hua Li, MD; Hui Chen, MD; Jian Qiu Zhu, MD; Xue Juan Jin, MS; Bert C. Wouters, MA; Jian Zhao, PhD.(5)
6. Parkinson's disease
In the assessment of the effect of theaflavin against MPTP/p induced neurodegenaration in C57BL/6 mice, found that theaflavin attenuates MPTP/p induced apoptosis and neurodegeneration as evidenced by increased expression of nigral tyrosine hydroxylase (TH), dopamine transporter (DAT) and reduced apoptotic markers such as caspase-3, 8, 9 accompanied by normalized behavioral characterization. This may be due to anti oxidative and anti apoptotic activity, according to "Theaflavin, a black tea polyphenol, protects nigral dopaminergic neurons against chronic MPTP/probenecid induced Parkinson's disease" by Anandhan A, Tamilselvam K, Radhiga T, Rao S, Essa MM, Manivasagam T.(6)
7. Antioxidant effects
In the investigation of four main TF derivatives (theaflavin (TF(1)), theaflavin-3-gallate (TF(2)A), theaflavin-3'-gallate (TF(2)B), and theaflavin-3,3'-digallate (TF(3))) in scavenging reactive oxygen species (ROS) in vitro, their properties of inhibiting superoxide, singlet oxygen, hydrogen peroxide, and the hydroxyl radical, and their effects on hydroxyl radical-induced DNA oxidative damage, found that compared with (-)-epigallocatechin gallate (EGCG), TF derivatives were good antioxidants for scavenging ROS and preventing the hydroxyl radical-induced DNA damage in vitro. TF(3) was the most positive in scavenging hydrogen peroxide and hydroxyl radical, and TF(1) suppressed superoxide. Positive antioxidant capacities of TF(2)B on singlet oxygen, hydrogen peroxide, hydroxyl radical, and the hydroxyl radical-induced DNA damage in vitro were found, according to "Evaluation of the antioxidant effects of four main theaflavin derivatives through chemiluminescence and DNA damage analyses" by Wu YY, Li W, Xu Y, Jin EH, Tu YY.(7)
8. Antibacterial effects
in the evaluation of the antibacterial effects of various concentrations of theaflavin as well as combinations of theaflavin and epicatechin, using the disk diffusion assay, found that strong antibacterial activity of theaflavin against eight clinical isolates of S. maltophilia and A. baumannii. Significant synergy (P≤0.05) was also observed between theaflavin and epicatechin against all isolates, according to "Antibacterial effects of theaflavin and synergy with epicatechin against clinical isolates of Acinetobacter baumannii and Stenotrophomonas maltophilia" by Betts JW, Kelly SM, Haswell SJ.(8)
9. Gastric ulcer healing
In the investigation of black tea (BT) and its constituent theaflavins (TFs) during their healing action against indomethacin-induced stomach ulceration in mice, found that Treatment with BT (40 mg/kg) and TF (1 mg/kg) for 3 days reversed these parameters and provided excellent (78-81%) ulcer healing. However, alterations of NOS expressions and levels of selectins and CAMs were only partially responsible for the excellent healing capacity (∼80%) of omeprazole (3 mg/kg × 3 days), according to "Black tea and theaflavins suppress various inflammatory modulators and i-NOS mediated nitric oxide synthesis during gastric ulcer healing" by Adhikary B, Yadav SK, Chand S, Bandyopadhyay SK, Chattopadhyay S.(9)
10. Cardio-protective activities
In the analyzing the protective effect of theaflavin (TF1) and its underlying mechanism,
found that (1) compared with the control group, TF1 (10, 20, 40 μmol/l) displayed a better recovery of cardiac function after ischemia/reperfusion in a concentration-dependent manner. At 60 min of reperfusion, LVDP, ± LVdP/dt (max) and CF in the TF1 group were much higher than those in the control group, whereas left ventricular end-diastolic pressure (LVEDP) in the TF1 group was lower than that in the control group (P < 0.01). (2) Pretreatment with glibenclamide (10 μmol/l), a K(ATP) antagonist, completely abolished the cardioprotective effects of TF1 (20 μmol/l). Also, most of the effects of TF1 (20 μmol/l) on cardiac function after 60 min of reperfusion were reversed by 5-HD (100 μmol/l), a selective mitochondria K(ATP) antagonist. (3) Atractyloside (20 μmol/l), a mitochondrial permeability transition pore (mPTP) opener, administered at the beginning of 15 min of reperfusion completely abolished the cardioprotection of TF1 (20 μmol/l), according to "ATP-dependent potassium channels and mitochondrial permeability transition pores play roles in the cardioprotection of theaflavin in young rat" by Ma H, Huang X, Li Q, Guan Y, Yuan F, Zhang Y.(10)
11. Cervical cancer
In the study of antiproliferative activity of theaflavins in cervical carcinoma HeLa cells and their effects on cellular microtubules and purified goat brain tubulin, found that in vitro, polymerization of purified tubulin into microtubules was also inhibited by theaflavins with an IC(50) value of 78 ± 2.43 μg/mL (P < 0.01). Thus, disruption of cellular microtubule network of HeLa cells through microtubule depolymerization may be one of the possible mechanisms of antiproliferative activity of theaflavins, according to " Theaflavins depolymerize microtubule network through tubulin binding and cause apoptosis of cervical carcinoma HeLa cells" by Chakrabarty S, Das A, Bhattacharya A, Chakrabarti G.(11)
12. Allergic effects
In the determination of the preventive effects of black tea theaflavins, theaflavin-3-gallate (3-TF) and theaflavin-3,3'-digallate (TFDG), on oxazolone-induced type IV allergy in male ICR mice, found that the anti-allergic mechanisms of action of theaflavins involve inhibition of the fluctuations of cytokines and maintenance of antioxidant status in allergic mice, according to "Preventive effects of black tea theaflavins against mouse type IV allergy" by Yoshino K, Yamazaki K, Sano M.(12)
13. Alzheimer's disease and obesity
In the investigation of the effect of Theaflavin and the symptoms of Alzheimer's disease and reduce the body weight of obese individuals, found that Clearly TH(2) inhibits PAI-1 and might play a role in slowing down the progression of Alzheimer's disease or obesity by a PAI-1-dependent pathway. While the clinical value of TH(2) has not been proven, long-term prospective studies assessing its efficacy are warranted due to the benign nature of the substance, according to "Theaflavin digallate inactivates plasminogen activator inhibitor: could tea help in Alzheimer's disease and obesity?" by Skrzypczak-Jankun E, Jankun J.(13)
14. Etc.
4. HIV-1 infection
In the investigation of the mechanism by which TFmix inhibits HIV-1 infection was investigated using time-of-addition, found that TFmix is an economic natural product preparation containing high content of theaflavins with potent anti-HIV-1 activity by targeting the viral entry step through the disruption of gp41 6-HB core structure. It has a potential to be developed as a safe and affordable topical microbicide for preventing sexual transmission of HIV, according to "A natural theaflavins preparation inhibits HIV-1 infection by targeting the entry step: Potential applications for preventing HIV-1 infection" by Yang J, Li L, Tan S, Jin H, Qiu J, Mao Q, Li R, Xia C, Jiang ZH, Jiang S, Liu S.(4)
5. Cholesterol
In the investigation of 240 men and women 18 years or older on a low-fat diet with mild to moderate hypercholesterolemia were randomly assigned to receive a daily capsule containing theaflavin-enriched green tea extract (375 mg) or placebo for 12 weeks, found that after 12 weeks, the mean ± SEM changes from baseline in total cholesterol, LDL-C, HDL-C, and triglyceride levels were -11.3% ± 0.9% (P = .01), -16.4% ± 1.1% (P = .01), 2.3% ± 2.1% (P = .27), and 2.6% ± 3.5% (P = .47), respectively, in the tea extract group. The mean levels of total cholesterol, LDL-C, HDL-C, and triglycerides did not change significantly in the placebo group. No significant adverse events were observed, according to "Cholesterol-Lowering Effect of a Theaflavin-Enriched Green Tea Extract" by David J. Maron, MD; Guo Ping Lu, MD; Nai Sheng Cai, MD; Zong Gui Wu, MD; Yue Hua Li, MD; Hui Chen, MD; Jian Qiu Zhu, MD; Xue Juan Jin, MS; Bert C. Wouters, MA; Jian Zhao, PhD.(5)
6. Parkinson's disease
In the assessment of the effect of theaflavin against MPTP/p induced neurodegenaration in C57BL/6 mice, found that theaflavin attenuates MPTP/p induced apoptosis and neurodegeneration as evidenced by increased expression of nigral tyrosine hydroxylase (TH), dopamine transporter (DAT) and reduced apoptotic markers such as caspase-3, 8, 9 accompanied by normalized behavioral characterization. This may be due to anti oxidative and anti apoptotic activity, according to "Theaflavin, a black tea polyphenol, protects nigral dopaminergic neurons against chronic MPTP/probenecid induced Parkinson's disease" by Anandhan A, Tamilselvam K, Radhiga T, Rao S, Essa MM, Manivasagam T.(6)
7. Antioxidant effects
In the investigation of four main TF derivatives (theaflavin (TF(1)), theaflavin-3-gallate (TF(2)A), theaflavin-3'-gallate (TF(2)B), and theaflavin-3,3'-digallate (TF(3))) in scavenging reactive oxygen species (ROS) in vitro, their properties of inhibiting superoxide, singlet oxygen, hydrogen peroxide, and the hydroxyl radical, and their effects on hydroxyl radical-induced DNA oxidative damage, found that compared with (-)-epigallocatechin gallate (EGCG), TF derivatives were good antioxidants for scavenging ROS and preventing the hydroxyl radical-induced DNA damage in vitro. TF(3) was the most positive in scavenging hydrogen peroxide and hydroxyl radical, and TF(1) suppressed superoxide. Positive antioxidant capacities of TF(2)B on singlet oxygen, hydrogen peroxide, hydroxyl radical, and the hydroxyl radical-induced DNA damage in vitro were found, according to "Evaluation of the antioxidant effects of four main theaflavin derivatives through chemiluminescence and DNA damage analyses" by Wu YY, Li W, Xu Y, Jin EH, Tu YY.(7)
8. Antibacterial effects
in the evaluation of the antibacterial effects of various concentrations of theaflavin as well as combinations of theaflavin and epicatechin, using the disk diffusion assay, found that strong antibacterial activity of theaflavin against eight clinical isolates of S. maltophilia and A. baumannii. Significant synergy (P≤0.05) was also observed between theaflavin and epicatechin against all isolates, according to "Antibacterial effects of theaflavin and synergy with epicatechin against clinical isolates of Acinetobacter baumannii and Stenotrophomonas maltophilia" by Betts JW, Kelly SM, Haswell SJ.(8)
9. Gastric ulcer healing
In the investigation of black tea (BT) and its constituent theaflavins (TFs) during their healing action against indomethacin-induced stomach ulceration in mice, found that Treatment with BT (40 mg/kg) and TF (1 mg/kg) for 3 days reversed these parameters and provided excellent (78-81%) ulcer healing. However, alterations of NOS expressions and levels of selectins and CAMs were only partially responsible for the excellent healing capacity (∼80%) of omeprazole (3 mg/kg × 3 days), according to "Black tea and theaflavins suppress various inflammatory modulators and i-NOS mediated nitric oxide synthesis during gastric ulcer healing" by Adhikary B, Yadav SK, Chand S, Bandyopadhyay SK, Chattopadhyay S.(9)
10. Cardio-protective activities
In the analyzing the protective effect of theaflavin (TF1) and its underlying mechanism,
found that (1) compared with the control group, TF1 (10, 20, 40 μmol/l) displayed a better recovery of cardiac function after ischemia/reperfusion in a concentration-dependent manner. At 60 min of reperfusion, LVDP, ± LVdP/dt (max) and CF in the TF1 group were much higher than those in the control group, whereas left ventricular end-diastolic pressure (LVEDP) in the TF1 group was lower than that in the control group (P < 0.01). (2) Pretreatment with glibenclamide (10 μmol/l), a K(ATP) antagonist, completely abolished the cardioprotective effects of TF1 (20 μmol/l). Also, most of the effects of TF1 (20 μmol/l) on cardiac function after 60 min of reperfusion were reversed by 5-HD (100 μmol/l), a selective mitochondria K(ATP) antagonist. (3) Atractyloside (20 μmol/l), a mitochondrial permeability transition pore (mPTP) opener, administered at the beginning of 15 min of reperfusion completely abolished the cardioprotection of TF1 (20 μmol/l), according to "ATP-dependent potassium channels and mitochondrial permeability transition pores play roles in the cardioprotection of theaflavin in young rat" by Ma H, Huang X, Li Q, Guan Y, Yuan F, Zhang Y.(10)
11. Cervical cancer
In the study of antiproliferative activity of theaflavins in cervical carcinoma HeLa cells and their effects on cellular microtubules and purified goat brain tubulin, found that in vitro, polymerization of purified tubulin into microtubules was also inhibited by theaflavins with an IC(50) value of 78 ± 2.43 μg/mL (P < 0.01). Thus, disruption of cellular microtubule network of HeLa cells through microtubule depolymerization may be one of the possible mechanisms of antiproliferative activity of theaflavins, according to " Theaflavins depolymerize microtubule network through tubulin binding and cause apoptosis of cervical carcinoma HeLa cells" by Chakrabarty S, Das A, Bhattacharya A, Chakrabarti G.(11)
12. Allergic effects
In the determination of the preventive effects of black tea theaflavins, theaflavin-3-gallate (3-TF) and theaflavin-3,3'-digallate (TFDG), on oxazolone-induced type IV allergy in male ICR mice, found that the anti-allergic mechanisms of action of theaflavins involve inhibition of the fluctuations of cytokines and maintenance of antioxidant status in allergic mice, according to "Preventive effects of black tea theaflavins against mouse type IV allergy" by Yoshino K, Yamazaki K, Sano M.(12)
13. Alzheimer's disease and obesity
In the investigation of the effect of Theaflavin and the symptoms of Alzheimer's disease and reduce the body weight of obese individuals, found that Clearly TH(2) inhibits PAI-1 and might play a role in slowing down the progression of Alzheimer's disease or obesity by a PAI-1-dependent pathway. While the clinical value of TH(2) has not been proven, long-term prospective studies assessing its efficacy are warranted due to the benign nature of the substance, according to "Theaflavin digallate inactivates plasminogen activator inhibitor: could tea help in Alzheimer's disease and obesity?" by Skrzypczak-Jankun E, Jankun J.(13)
14. Etc.
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Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/20528747
(2) http://www.ncbi.nlm.nih.gov/pubmed/22202062
(3) http://www.ncbi.nlm.nih.gov/pubmed/22155236
(4) http://www.ncbi.nlm.nih.gov/pubmed/22155187
(5) http://archinte.ama-assn.org/cgi/content/abstract/163/12/1448
(6) http://www.ncbi.nlm.nih.gov/pubmed/22138428
(7) http://www.ncbi.nlm.nih.gov/pubmed/21887850
(8) http://www.ncbi.nlm.nih.gov/pubmed/21885260
(9) http://www.ncbi.nlm.nih.gov/pubmed/21545263
(10) http://www.ncbi.nlm.nih.gov/pubmed/21503789
(11) http://www.ncbi.nlm.nih.gov/pubmed/21323312
(12) http://www.ncbi.nlm.nih.gov/pubmed/20597096
(13) http://www.ncbi.nlm.nih.gov/pubmed/20514421
Theaflavin is an antioxidant polyphenol which is formed from the condensation of flavan-3-ols in tea leaves during the enzymatic oxidation (fermentation) of black tea. Theaflavin
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