Goodenowe Dayan B, Haroon Jonathan, Kling Mitchel A, Zielinski Margaret, Mahdavi Kennedy, Habelhah Barshen, Shtilkind Leah, Jordan Sheldon
Prodrome Services USA LLC, Temecula, CA, United States.
The Regenesis Project, Santa Monica, CA, United States.
Front Cell Dev Biol. 2022 Jul 6;10:864842. doi: 10.3389/fcell.2022.864842. eCollection 2022.
Plasmalogens are a specific type of glycerophospholipid found in especially high levels in neuronal membranes. Decreased blood and brain levels of docosahexaenoic acid (DHA) containing plasmalogens are associated with decreased cognition and neuromuscular function in humans. Administration of 1-O-alkyl-2-acylglycerol (AAG) plasmalogen precursors containing DHA at the sn-2 position dose-dependently increase blood DHA plasmalogens and are neuroprotective in animal models of neurodegeneration at doses between 10 and 50 mg/kg. We conducted an investigational clinical trial in 22 cognitively impaired persons to evaluate the effects of an escalating oral dosing regimen of DHA-AAG from 900 to 3,600 mg/day over a 4-month period on blood serum plasmalogen and non-plasmalogen phospholipids and oxidative stress biomarkers. Safety, tolerability and therapeutic effects on cognition and mobility were also evaluated. DHA plasmalogen levels increased with increasing dose and remained significantly elevated at all treatment doses and durations. DHA plasmalogen levels were positively associated with catalase activity and negatively associated with malondialdehyde (MDA) levels. DHA-AAG supplementation normalized catalase activity in persons with low baseline catalase activity, normalized MDA levels in persons with high baseline MDA levels, and normalized superoxide dismutase activity in persons with high baseline SOD activity. Cognition improved in nine participants, was unchanged in nine, and declined in four. Mobility improved in twelve, was unchanged in five and declined in four participants. Changes in cognition and mobility were statistically significant versus a random outcome. Baseline DHA-plasmalogen levels were not predictive of clinical response. DHA-AAG was well tolerated at all dosages and no adverse reactions were observed.
缩醛磷脂是一种特殊类型的甘油磷脂,在神经元膜中的含量尤其高。血液和大脑中含二十二碳六烯酸(DHA)的缩醛磷脂水平降低与人类认知能力和神经肌肉功能下降有关。在sn-2位含DHA的1-O-烷基-2-酰基甘油(AAG)缩醛磷脂前体,以10至50mg/kg的剂量给药可剂量依赖性地增加血液中DHA缩醛磷脂含量,并且在神经退行性疾病动物模型中具有神经保护作用。我们对22名认知障碍者进行了一项研究性临床试验,以评估在4个月内将DHA-AAG口服剂量从900mg/天逐步增加至3600mg/天,对血清缩醛磷脂和非缩醛磷脂以及氧化应激生物标志物的影响。还评估了其对认知和活动能力的安全性、耐受性及治疗效果。DHA缩醛磷脂水平随剂量增加而升高,在所有治疗剂量和疗程中均显著升高。DHA缩醛磷脂水平与过氧化氢酶活性呈正相关,与丙二醛(MDA)水平呈负相关。补充DHA-AAG可使基线过氧化氢酶活性低的人过氧化氢酶活性恢复正常,使基线MDA水平高的人MDA水平恢复正常,使基线超氧化物歧化酶活性高的人超氧化物歧化酶活性恢复正常。9名参与者的认知能力有所改善,9名未变,4名下降。12名参与者的活动能力有所改善,5名未变,4名下降。与随机结果相比,认知和活动能力的变化具有统计学意义。基线DHA-缩醛磷脂水平不能预测临床反应。DHA-AAG在所有剂量下耐受性良好,未观察到不良反应。