TML-6 是一种口服有效的姜黄素衍生物，抑制 β-淀粉样前体蛋白和 β-淀粉样蛋白 (Aβ) 的合成。TML-6 上调 Apo E，抑制NF-κB和mTOR，并增加抗氧化Nrf2基因的活性。TML-6 具有用于阿尔茨海默氏病 (AD) 研究的潜力。
| 生物活性 | TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein andβ-amyloid (Aβ). TML-6 can upregulate Apo E, suppressNF-κBandmTOR, and increase the activity of the anti-oxidativeNrf2gene. TML-6 has the potential for Alzheimer’s disease (AD) research[1]. |
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体外研究
(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[1].
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 IC50of 4.19 μg/mL (8 μM)[1].
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[1].
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[1].
Western Blot Analysis[1] | Cell 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. |
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体内研究
(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[1].
TML-6 (oral; 150 mg/kg) has a T1/2of 1.27 hours, a Cmaxof 35.9 ng/mL and an AUC of 177 ngohr/mL[1].
| Animal Model: | Six-month-old 3xTg (mutations: APPKM670/671NL, MAPTP301Land PSEN1M146V) AD transgenic mice[1] | | 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[1] | | Dosage: | 150 mg/kg (Pharmacokinetic Analysis) | | Administration: | Oral | | Result: | Had a T1/2of 1.27 hours, a Cmaxof 35.9 ng/mL and an AUC of 177 ngohr/mL. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 120 mg/mL(229.17 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9098 mL | 9.5489 mL | 19.0978 mL | | 5 mM | 0.3820 mL | 1.9098 mL | 3.8196 mL | | 10 mM | 0.1910 mL | 0.9549 mL | 1.9098 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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