Table 1.
Summary of studies on bioactivities of theacrine.
| Bioactivity | Assay employed or models | Dose or concentration tested | Results | Ref.* |
|---|---|---|---|---|
| Antioxidant | DPPH and FRAP assay | Water soluble Kucha tea extract (TE) 0.2–1.0 mg/mL | The TEAC in scavenging DPPH radicals was 436.78 ± 12.44 mg/mL and IC50 was 0.79 ± 0.022 mg/mL; TEAC in scavenging RFAP radicals was 493.67 ± 8.02 mg/mL. | (14) |
| Antioxidant | ORAC, CAA, chick embryo | 50 pM, 50 nM, 50 μM | Compared to AAPH, theacrine significantly increased ORAC and chick embryo vessel density, decreased MDA level. | (18) |
| Antioxidant | Mouse intervertebral disc degeneration model | Orally 10 mg/kg | Theacrine stimulated the expression of collagen II, SIRT3, FOXO3a, and SOD2. | (19) |
| Antioxidant | Estrogen-deficient Mouse | 20 mg/kg via gavage | Theacrine activated SIRT3 and repress myocardial fibrosis and apoptosis after myocardial infarction in ovariectomized mice, resulting in improvement of the cardiac function of ovariectomized mice with myocardial infarction. | (20) |
| Antioxidant | Mouse | Orally 10, 20, 30 mg/kg | Theacrine decreased activities of plasma ALT, AST and levels of MDA, but increased activity of SOD and level of ORAC. | (21) |
| Anti-inflammation | Mouse | Orally 8–32 mg/kg | Theacrine significantly inhibited the ear edema induced by xylene and hind paw edema induced by λ-carrageenan. | (22) |
| Anti-inflammation | Mouse | Orally 10–30 mg/kg | Theacrine reduced hepatic mRNA levels of inflammatory mediators (IL-6, IL-1 β, TNF α, and IFN γ), decreased the levels of plasma ALT and AST, and reversed the histologic damages. | (21) |
| Anti-inflammation | FIA-induced SD rats (n = 8) | Orally 12.5–25.0 mg/kg | Theacrine attenuated rheumatoid arthritis via the suppression of IL-6 and the activation of TGF-β by the TGF-β/SMAD pathway. | (23) |
| Locomotor activation and reducing fatigue | Long Evans rats (n = 8) | 24 or 48 mg/kg, i.p. | Pre-treatment with theacrine significantly attenuated the motor depression induced by the adenosine receptor agonists which is mediated by both the adenosinergic and dopaminergic systems. | (24) |
| Improving cognitive performance | Clinic test on Human (n = 12) | Orally 65–300 mg theacrine and 25–650 mg caffeine daily | Administration of the theacrine and caffeine improved mood, energy, focus, concentration, cognitive function, or sexual desire, reduced anxiety or fatigue. | (25, 26) |
| Improving cognitive performance | Clinic test on Human (n = 19) | Orally PWS containing 10–15 mg theacrine for 1 week | Theacrine significantly improved Stroop word testing and Stroop color testing results. | (27) |
| Improving cognitive performance | 6-OHDA-treated rats and MPTP-treated mice and zebrafish | Theacrine 10–20 mg/kg, i.p. | Theacrine relieved PD by retrieving the apoptosis of dopaminergic neurons and activating SIRT3. | (28) |
| Improving cognitive performance | Male kunming mice/Morris water maze test | Orally 5–15 mg/kg, | Theacrine significantly reversed learning and memory impairment caused by central fatigue by normalizing glucose metabolism, restoring 5-HT level and inhibiting phosphodiesterase in the restraint-stressed mice brain. | (17) |
| Improving cognitive performance | Male and female soccer players (n = 24) | Orally 275 mg placebo (PL), 275 mg Teacrine (TCr), 275 mg caffeine (Caf), or a combination of 125 mg TCr and 150 mg Caff (TCr + Caf) 30 min prior to exercise. | Compared to PL, 275 mg of Caf or a combination of Caf + TCr produced modest cognitive benefits, particularly following the first half of the simulated soccer match. | (16) |
| Hypnotic and antidepressant effects | Mice (n = 20) | Orally 10 and 30 mg/kg | Theacrine prolonged remarkably pentobarbital-induced sleeping time at both doses (p < 0.01). | (29) |
| Hypnotic and antidepressant effects | Male NIH mice (n = 10) | 3, 10, 30 mg/kg, i.g. | Theacrine showed antidepressant effects on mice, including shortening the immobility time in the tail suspension test (P < 0.05), enhancing the rotatory locomotor activities during forced swimming test (P < 0.05), increasing the mortality induced by yohimbine and the head-twitching number induced by 5-HTP (p < 0.01). | (30) |
| Hypnotic and antidepressant effects | Male ICR mice and male Sprague Dawley rats (n = 5) | 3, 10, 30 mg/kg, i.g. | Theacrine significantly enhanced pentobarbital-induced sleep in mice by shortening wake time and increasing NREMS time, but it had no effect on REMS. Theacrine significantly reversed the decrease in sleeping time in mice pretreated with the adenosine A1 receptor antagonist DPCPX. | (31) |
| Ameliorating lipid metabolism | In vitro: 3T3-L cells; in vivo: kunming mice (n-8) | In vitro: 2, 0.5, 0.125, 0.03125 m mol/L; in vivo: orally 0, 20, 40 mg/kg | In vitro, theacrine up-regulated expression of genes encoding SIRT3, LCAD, FABP4 and LPL genes. In vivo, theacrine (10 mg/kg) up-regulated SIRT3 gene expression in liver, but 40 mg/kg of theacrine showed inhibition on SIRT3. | (32) |
| Ameliorating lipid metabolism | 3T3-L cells | 50–200 μg/Ml C. kucha extract | Kucha extract significantly suppressed lipid droplet and TG accumulation and inhibited the expression of genes FAS, FAT, SCD-1, LPL, SREBP-1c and ACC in 3T3-L1 cells in dose dependent manner. | (33) |
| Ameliorating lipid metabolism | In vivo: C57BIM 6J mice (n-8); in vitro: HepG cells | Theacrine 10, 20 mg/kg for in vivo and 2 m mol/L for in vitro. | Theacrine significantly decreased hepatic TG content (p < 0.01) and ameliorated hepatic steatosis in mice. | (34) |
| Ameliorating lipid metabolism, anti-inflammation | C57BL/6 mice | Theacrine 10, 20 mg/kg | Theacrine inhibited hepatic steatosis and liver inflammation, improved energy expenditure and ameliorated acylcarnitine metabolism disorder in HFD-fed mice through SIRT3/LCAD signaling pathway. | (35) |
| Inhibiting cancer cell metastasis | MDA-MB-231 cells | Theacrine 10–100 μM | Theacrine suppressed TGF-β-induced progression and metastasis of TNBC through inhibiting EMT. | (36) |
| Anti-virus | MDCK cells | 50 or 100 μM | Theacrine at 50 μM significantly inhibited the expression of influenza virus A NS1 protein at 12 hpi; theacrine at 100 μM significantly reduced the yield of viral progenies. | (37) |
| No effect | Men (n = 10) and women (n-10) | Orally TheaTrimTM containing 150 mg theacrine | Theacrine did not result in a statistically significant improvement in cognitive performance, but might favorably impact multiple subjective feelings related to energy and mood. | (38) |
| No effect | Resistance-trained men (n = 12) | Theacrine 300 mg, caffeine 300 mg, or theacrine 150 mg + caffeine 150 mg (combination) | Neither theacrine, caffeine or their combination improved muscular strength, power, or endurance performance in resistance-trained men. | (39) |
*
Ref., Reference.