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酒石酸左旋肉碱和多颗粒形式肌酸单水合物对成肌细胞肌肉蛋白合成的影响及其在人和啮齿动物中的生物利用度。

Effects of Low Doses of L-Carnitine Tartrate and Lipid Multi-Particulate Formulated Creatine Monohydrate on Muscle Protein Synthesis in Myoblasts and Bioavailability in Humans and Rodents.

机构信息

Nutrition, Exercise Physiology, and Sarcopenia Laboratory, Jean Mayer USDA Human Nutrition Research Center, Aging Tufts University, Boston, MA 02111, USA.

Biodynamics and Human Performance Center, Georgia Southern University, Armsrong Campus, Savannah, GA 31419, USA.

出版信息

Nutrients. 2021 Nov 9;13(11):3985. doi: 10.3390/nu13113985.

Abstract

The primary objective of this study was to investigate the potential synergy between low doses of L-carnitine tartrate and creatine monohydrate to induce muscle protein synthesis and anabolic pathway activation in primary human myoblasts. In addition, the effects of Lipid multi-particulates (LMP) formulation on creatine stability and bioavailability were assessed in rodents and healthy human subjects. When used individually, L-carnitine tartrate at 50 µM and creatine monohydrate at 0.5 µM did not affect myoblast protein synthesis and signaling. However, when combined, they led to a significant increase in protein synthesis. Increased AKT and RPS6 phosphorylation were observed with 50 µM L-carnitine tartrate 5 µM creatine in combination in primary human myoblasts. When Wistar rats were administered creatine with LMP formulation at either 21 or 51 mg/kg, bioavailability was increased by 27% based on the increase in the area under the curve (AUC) at a 51 mg/kg dose compared to without LMP formulation. Tmax and Cmax were unchanged. Finally, in human subjects, a combination of LMP formulated L-carnitine at 500 mg (from L-carnitine tartrate) with LMP formulated creatine at 100, 200, or 500 mg revealed a significant and dose-dependent increase in plasma creatine concentrations. Serum total L-carnitine levels rose in a similar manner in the three combinations. These results suggest that a combination of low doses of L-carnitine tartrate and creatine monohydrate may lead to a significant and synergistic enhancement of muscle protein synthesis and activation of anabolic signaling. In addition, the LMP formulation of creatine improved its bioavailability. L-carnitine at 500 mg and LMP-formulated creatine at 200 or 500 mg may be useful for future clinical trials to evaluate the effects on muscle protein synthesis.

摘要

本研究的主要目的是探讨低剂量酒石酸左旋肉碱和一水肌酸联合使用对原代人肌母细胞诱导肌肉蛋白质合成和合成代谢途径激活的潜在协同作用。此外,还评估了脂质多颗粒(LMP)配方对肌酸稳定性和生物利用度的影响,分别在啮齿动物和健康人体受试者中进行。当单独使用时,50µM 的酒石酸左旋肉碱和 0.5µM 的一水肌酸对肌母细胞蛋白质合成和信号无影响。然而,当联合使用时,它们导致蛋白质合成显著增加。在原代人肌母细胞中,当 50µM 酒石酸左旋肉碱与 5µM 一水肌酸联合使用时,观察到 AKT 和 RPS6 磷酸化增加。当 Wistar 大鼠以 21 或 51mg/kg 的剂量给予肌酸与 LMP 配方时,与不使用 LMP 配方相比,在 51mg/kg 剂量下,AUC 的增加使生物利用度提高了 27%。Tmax 和 Cmax 未改变。最后,在人体受试者中,LMP 配方的左旋肉碱 500mg(来自酒石酸左旋肉碱)与 LMP 配方的肌酸 100、200 或 500mg 的组合显示出血浆肌酸浓度的显著且剂量依赖性增加。三种组合中血清总左旋肉碱水平以相似的方式升高。这些结果表明,低剂量酒石酸左旋肉碱和一水肌酸的组合可能导致肌肉蛋白质合成的显著协同增强和合成代谢信号的激活。此外,肌酸的 LMP 配方提高了其生物利用度。500mg 的左旋肉碱和 200 或 500mg 的 LMP 配方肌酸可能对未来的临床试验有用,以评估其对肌肉蛋白质合成的影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/98ac/8625796/09d348ef1121/nutrients-13-03985-g001.jpg

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