姜酮酚 T7113

Product Introduction
Bioactivity


英文名: Paradol

描述: Paradol ([6]-Gingerone) 是一种姜科植物中发现的酚类天然产物，具有抗癌、抗炎、抗氧化和神经保护作用。在小鼠皮肤癌变中，可结合到环氧合酶(COX-2) 活性位点。

动物实验: MOG35-55 was emulsified in an equal amount of CFA.?Mice were anesthetized with isoflurane and 200 μg of emulsion MOG35-55 in CFA was injected subcutaneously at the start day of immunization (day 1). In addition, 400 ng of Bordetella pertussis toxin (PTX) per mouse was injected intraperitoneally on the start day of MOG immunization and 2 days later.?Mice were weighed and monitored daily for clinical symptoms of EAE as follows: 0, no clinical signs of EAE;?0.5, some lack of tone, however, some strength at the base of tail;?1.0, total loss of tail tonicity and flaccid tail;?2.0, hind limb weakness;?2.5, incomplete paralysis of one or both hind limbs;?3.0, total paralysis of one or both hind limbs;?4.0, hind and fore limbs paralysis;?5.0, death from disease.?For drug administration, symptomatic EAE mice were divided into three groups;?(1) the vehicle-treated EAE group, (2) the 6-shogaol-treated EAE group, and (3) the 6-paradol-treated EAE group.?Vehicle (10% Tween 80), 6-shogaol (5 mg/kg), or 6-paradol (5 mg/kg) was orally administered daily into symptomatic EAE mice from day 29 to day 42 (for 13 days) post immunization[1].

体内活性: EAE-symptomatic mice were treated with 6-shogaol or 6-paradaol (5 mg/kg, p.o.) once daily for 14 days (between days 29 and 42 after immunization).?Both 6-shogaol and 6-paradol significantly improved EAE-relevant symptoms from the fourth day after drug administration (between days 32 and 42) except days 36 and 37 in the 6-paradol-treated EAE group compared to the vehicle-treated EAE group (Fig. 1A, Supplementary Table 1). The effectiveness of 6-shogaol and 6-paradol was also clearly shown from cumulative clinical scores from days 30 to 43.?Administration of 6-paradol or 6-shogaol significantly reduced the cumulative clinical score (6-shogaol, 25.25%;?6-paradol, 25.75%) compared to the vehicle-treated EAE group.?6-shogaol and its metabolite, 6-paradaol, exert neuroprotective effects against EAE.?Moreover, these molecules are therapeutically effective for EAE[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (179.6 mM)


关键字: Inhibitor | inhibit | COX | [6]-Paradol | Paradol | Cyclooxygenase

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