The Korean Journal of Physiology and Pharmacology

The Korean Society of Pharmacology (대한약리학회)
권호 표지
DOI QR코드

DOI QR Code

The beneficial effect of glycerophosphocholine to local fat accumulation: a comparative study with phosphatidylcholine and aminophylline

  • Kim, Go Woon (Department of Pharmacology, College of Pharmacy, Kyung Hee University) ;
  • Chung, Sung Hyun (Department of Pharmacology, College of Pharmacy, Kyung Hee University)
  • Received : 2020.12.11
  • Accepted : 2021.05.06
  • Published : 2021.07.01
Download PDF
⟨ Previous Next ⟩

Abstract

Injection lipolysis or mesotherapy gained popularity for local fat dissolve as an alternative to surgical liposuction. Phosphatidylcholine (PPC) and aminophyl-line (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 in vitro and in vivo 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.

Keywords

Acknowledgement

We thank to Beauvous Co. for providing Alfocholine Inj., Lipobean i.v., Aminophylline Injection Huons and valuable information related to this study.

References

  1. Couillard C, Gagnon J, Bergeron J, Leon AS, Rao DC, Skinner JS, Wilmore JH, Despres JP, Bouchard C. Contribution of body fatness and adipose tissue distribution to the age variation in plasma steroid hormone concentrations in men: the HERITAGE Family Study. J Clin Endocrinol Metab. 2000;85:1026-1031. https://doi.org/10.1210/jcem.85.3.6427
  2. O'Brien KS, Latner JD, Ebneter D, Hunter JA. Obesity discrimination: the role of physical appearance, personal ideology, and anti-fat prejudice. Int J Obes (Lond). 2013;37:455-460. https://doi.org/10.1038/ijo.2012.52
  3. Alizadeh Z, Halabchi F, Mazaheri R, Abolhasani M, Tabesh M. Review of the mechanisms and effects of noninvasive body contouring devices on cellulite and subcutaneous fat. Int J Endocrinol Metab. 2016;14:e36727. https://doi.org/10.5812/ijem.36727
  4. Hasengschwandtner F. Injection lipolysis for effective reduction of localized fat in place of minor surgical lipoplasty. Aesthet Surg J. 2006;26:125-130. https://doi.org/10.1016/j.asj.2006.01.008
  5. Zeisel SH. Choline: critical role during fetal development and dietary requirements in adults. Annu Rev Nutr. 2006;26:229-250. https://doi.org/10.1146/annurev.nutr.26.061505.111156
  6. Nair AB, Jacob S. A simple practice guide for dose conversion between animals and human. J Basic Clin Pharm. 2016;7:27-31. https://doi.org/10.4103/0976-0105.177703
  7. Jung GS. Effectiveness of local fat-dissolving solution injection. Aesthet Surg J. 2019;39:NP156-NP158. https://doi.org/10.1093/asj/sjz034
  8. Galarraga M, Campion J, Munoz-Barrutia A, Boque N, Moreno H, Martinez JA, Milagro F, Ortiz-de-Solorzano C. Adiposoft: automated software for the analysis of white adipose tissue cellularity in histological sections. J Lipid Res. 2012;53:2791-2796. https://doi.org/10.1194/jlr.D023788
  9. Izu H, Okuda M, Shibata S, Fujii T, Matsubara K. Anti-diabetic effect of S-adenosylmethionine and α-glycerophosphocholine in KKAy mice. Biosci Biotechnol Biochem. 2019;83:747-750. https://doi.org/10.1080/09168451.2018.1559721
  10. Zeisel SH, Blusztajn JK. Choline and human nutrition. Annu Rev Nutr. 1994;14:269-296. https://doi.org/10.1146/annurev.nu.14.070194.001413
  11. Biswas S, Giri S. Importance of choline as essential nutrient and its role in prevention of various toxicities. Prague Med Rep. 2015;116:5-15. https://doi.org/10.14712/23362936.2015.40
  12. Kawamura T, Okubo T, Sato K, Fujita S, Goto K, Hamaoka T, Iemitsu M. Glycerophosphocholine enhances growth hormone secretion and fat oxidation in young adults. Nutrition. 2012;28:1122-1126. https://doi.org/10.1016/j.nut.2012.02.011
  13. Zimmermann R, Strauss JG, Haemmerle G, Schoiswohl G, BirnerGruenberger R, Riederer M, Lass A, Neuberger G, Eisenhaber F, Hermetter A, Zechner R. Fat mobilization in adipose tissue is promoted by adipose triglyceride lipase. Science. 2004;306:1383-1386. https://doi.org/10.1126/science.1100747
  14. Zhu J, Wu Y, Tang Q, Leng Y, Cai W. The effects of choline on hepatic lipid metabolism, mitochondrial function and antioxidative status in human hepatic C3A cells exposed to excessive energy substrates. Nutrients. 2014;6:2552-2571. https://doi.org/10.3390/nu6072552
  15. Narukawa M, Kamiyoshihara A, Izu H, Fujii T, Matsubara K, Misaka T. Efficacy of long-term feeding of α-Glycerophosphocholine for aging-related phenomena in old mice. Gerontology. 2020;66:275-285. https://doi.org/10.1159/000504962
  16. Noh Y, Heo CY. The effect of phosphatidylcholine and deoxycholate compound injections to the localized adipose tissue: an experimental study with a murine model. Arch Plast Surg. 2012;39:452-456. https://doi.org/10.5999/aps.2012.39.5.452
  17. Rose PT, Morgan M. Histological changes associated with mesotherapy for fat dissolution. J Cosmet Laser Ther. 2005;7:17-19. https://doi.org/10.1080/14764170510037743
  18. Schuller-Petrovic S, Wolkart G, Hofler G, Neuhold N, Freisinger F, Brunner F. Tissue-toxic effects of phosphatidylcholine/deoxycholate after subcutaneous injection for fat dissolution in rats and a human volunteer. Dermatol Surg. 2008;34:529-542; discussion 542-543. https://doi.org/10.1097/00042728-200804000-00011
  19. Ristow M, Muller-Wieland D, Pfeiffer A, Krone W, Kahn CR. Obesity associated with a mutation in a genetic regulator of adipocyte differentiation. N Engl J Med. 1998;339:953-959. https://doi.org/10.1056/NEJM199810013391403
  20. Sorisky A, Magun R, Gagnon AM. Adipose cell apoptosis: death in the energy depot. Int J Obes Relat Metab Disord. 2000;24 Suppl 4:S3-S7. https://doi.org/10.1038/sj.ijo.0801491
  21. Jung TW, Park T, Park J, Kim U, Je HD, Kim HD, Cho SW, Abd El-Aty AM, Song JH, Kim HC, Shin YK, Jeong JH. Phosphatidylcho-line causes adipocyte-specific lipolysis and apoptosis in adipose and muscle tissues. PLoS One. 2019;14:e0214760. https://doi.org/10.1371/journal.pone.0214760
  22. Li H, Lee JH, Kim SY, Yun HY, Baek KJ, Kwon NS, Yoon Y, Jeong JH, Kim DS. Phosphatidylcholine induces apoptosis of 3T3-L1 adipocytes. J Biomed Sci. 2011;18:91. https://doi.org/10.1186/1423-0127-18-91
  23. Won TJ, Nam Y, Lee HS, Chung S, Lee JH, Chung YH, Park ES, Hwang KW, Jeong JH. Injection of phosphatidylcholine and deoxycholic acid regulates gene expression of lipolysis-related factors, proinflammatory cytokines, and hormones on mouse fat tissue. Food Chem Toxicol. 2013;60:263-268. https://doi.org/10.1016/j.fct.2013.07.057
  24. Kim HK, Kim YW, Kim HJ. The evaluation of the effect of aminophylline injection to subcutaneous fat reduction. J Korean Soc Aesthet Plast Surg. 2003;9:17-21.
  25. Park SH, Kim DW, Lee MA, Yoo SC, Rhee SC, Koo SH, Seol GH, Cho EY. Effectiveness of mesotherapy on body contouring. Plast Reconstr Surg. 2008;121:179e-185e. https://doi.org/10.1097/01.prs.0000304611.71480.0a