Kim Go Woon, Chung Sung Hyun
Department of Pharmacology, College of Pharmacy, Kyung Hee University, Seoul 02447, Korea.
Korean J Physiol Pharmacol. 2021 Jul 1;25(4):333-339. doi: 10.4196/kjpp.2021.25.4.333.
Injection lipolysis or mesotherapy gained popularity for local fat dissolve as an alternative to surgical liposuction. Phosphatidylcholine (PPC) and aminophylline (AMPL) are commonly used compounds for mesotherapy, but their efficacy and safety as lipolytic agents have been controversial. Glycerophosphocholine (GPC) is a choline precursor structurally similar to PPC, and thus introduced in aesthetics as an alternative for PPC. This study aimed to evaluate the effects of GPC on adipocytes differentiation and lipolysis and compared those effects with PPC and AMPL using and models. Adipogenesis in 3T3-L1 was measured by Oil Red O staining. Lipolysis was assessed by measuring the amount of glycerol released in the culture media. To evaluate the lipolytic activity of GPC on a physiological condition, GPC was subcutaneously injected to one side of inguinal fat pads for 3 days. Lipolytic activity of GPC was assessed by hematoxylin and eosin staining in adipose tissue. GPC significantly suppressed adipocyte differentiation of 3T3-L1 in a concentration-dependent manner (22.3% inhibition at 4 mM of GPC compared to control). Moreover, when lipolysis was assessed by glycerol release in 3T3-L1 adipocytes, 6 mM of GPC stimulated glycerol release by two-fold over control. Subcutaneous injection of GPC into the inguinal fat pad of mice significantly reduced the mass of fat pad and the size of adipocytes of injected site, and these effects of GPC were more prominent over PPC and AMPL. Taken together, these results suggest that GPC is the potential therapeutic agent as a local fat reducer.
注射溶脂或美塑疗法作为手术抽脂的替代方法，因可局部溶解脂肪而受到欢迎。磷脂酰胆碱（PPC）和氨茶碱（AMPL）是美塑疗法常用的化合物，但它们作为溶脂剂的疗效和安全性一直存在争议。甘油磷酸胆碱（GPC）是一种结构与PPC相似的胆碱前体，因此作为PPC的替代品被引入美容领域。本研究旨在评估GPC对脂肪细胞分化和脂肪分解的影响，并使用3T3-L1和小鼠模型将这些影响与PPC和AMPL进行比较。通过油红O染色测量3T3-L1中的脂肪生成。通过测量培养基中释放的甘油量来评估脂肪分解。为了评估GPC在生理条件下的溶脂活性，将GPC皮下注射到腹股沟脂肪垫的一侧，持续3天。通过苏木精和伊红染色评估脂肪组织中GPC的溶脂活性。GPC以浓度依赖性方式显著抑制3T3-L1的脂肪细胞分化（与对照组相比，4 mM GPC时抑制率为22.3%）。此外，当通过3T3-L1脂肪细胞中的甘油释放评估脂肪分解时，6 mM GPC刺激甘油释放量比对照组增加了两倍。将GPC皮下注射到小鼠腹股沟脂肪垫中可显著降低脂肪垫质量和注射部位脂肪细胞的大小，并且GPC的这些作用比PPC和AMPL更显著。综上所述，这些结果表明GPC作为局部减脂剂具有潜在的治疗作用。
