TML-6

TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein and β-amyloid (Aβ) . TML-6 can upregulate Apo E, suppress NF-κB and mTOR , and increase the activity of the anti-oxidative Nrf2 gene. TML-6 has the potential for Alzheimer’s disease (AD) research In Vitro TML-6 (0.65-5.24 µg/mL; for 24 h) reduces the protein expression levels of APP and phospho-NF-κB, and induces the protein expression level of ApoE. TML-6 inhibits the mTOR signaling pathway through the suppression of phospho-mTOR. TML-6 (0.31, 0.63, 2.5, 5, 10, 20 μM; 24 h) reveals no cytotoxicity in Huh-7 cells at concentrations below 5 μM and has an IC 50 of 4.19 µg/mL (8 μM). TML-6 (1.05, 2.09, 3.14, 4.19 μg/mL; 24 h) reduces the production of Aβ40 and Aβ42 between 1.05, 2.09 and 3.14 μg/mL (equal to 2, 4 and 6 μM) in a dose-dependent manner in N2a/APPswe cell. TML-6 can exhibit transcriptional activation of the Nrf2 gene in a dose-dependent manner, with the highest activity at a concentration of 1.32 µg/mL. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Huh-7 cells Concentration: 0.65, 1.31, 1.96, 2.61, 3.93, 5.24 µg/mL Incubation Time: For 24 hours Result: Reduced the amyloid precursor protein (APP) protein expression level by 60% and decreased the level of phosphorylated NF-κB by about 50% at a dose of 1.96 µg/mL after 24 h treatment. Induced the protein expression level of ApoE by approximately 44% at a dose of 2.62 µg/mL. In Vivo TML-6 (diet; 150 mg/kg/day; for four months) treatment results in significant improvement in learning, suppression of the microglial activation marker Iba-1, and reduction in Aβ in the brain . TML-6 (oral; 150 mg/kg) has a T 1/2 of 1.27 hours, a C max of 35.9 ng/mL and an AUC of 177 ng•hr/mL . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Six-month-old 3xTg (mutations: APP KM670/671NL , MAPT P301L and PSEN1 M146V ) AD transgenic mice Dosage: 150 mg/kg Administration: Diet; daily; for four months Result: Improved the learning behaviors, significantly suppressed the Aβ levels and Iba-1 expression in the brain of 3xTg AD transgenic mice. Animal Model: SD rats Dosage: 150 mg/kg (Pharmacokinetic Analysis) Administration: Oral Result: Had a T 1/2 of 1.27 hours, a C max of 35.9 ng/mL and an AUC of 177 ng•hr/mL. Form:Solid IC50& Target:NF-κB mTOR

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