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Int J Med Sci 2020; 17(7):903-911. doi:10.7150/ijms.44188 This issue Cite

Research Paper

Tranexamic Acid Inhibits Angiogenesis and Melanogenesis in Vitro by Targeting VEGF Receptors

Jian-Wei Zhu1, Ya-Jie Ni1, Xiao-Yun Tong1, Xia Guo1, Xiao-Ping Wu1, Zhong-Fa Lu2✉

1. Department of Dermatology, Zhejiang Hospital, No. 12, Lingyin Rd., Hangzhou, 310013, Zhejiang Province, China.
2. Department of Dermatology, Second Affiliated Hospital, Zhejiang University School of Medicine, No. 88, Jiefang Rd., Hangzhou, 310009, Zhejiang Province, China.

✉ Corresponding author: Zhong-Fa Lu, E-mail: lzfskinedu.cn

Citation:
Zhu JW, Ni YJ, Tong XY, Guo X, Wu XP, Lu ZF. Tranexamic Acid Inhibits Angiogenesis and Melanogenesis in Vitro by Targeting VEGF Receptors. Int J Med Sci 2020; 17(7):903-911. doi:10.7150/ijms.44188. https://www.medsci.org/v17p0903.htm
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Abstract

Melasma is a common but complex skin condition concerning cosmetic problems. Tranexamic acid (TA) has been proved to be effective in treatment of melasma with still unclear mechanisms. Here, we show that VEGF165 enhanced the expression of VEGF receptors (VEGFRs, including VEGFR-1, VEGFR-2 and NRP-1) in human umbilical vein endothelial cells (HUVECs), which was attenuated by TA. VEGF165 also promoted tyrosine phosphorylation of VEGFR-1 and VEGFR-2 in HUVECs, which was again abolished by TA. TA further showed similar effects to neutralization of VEGFR-1 and VEGFR-2 in inhibiting cell proliferation, migration, invasion and tube formation of HUVECs induced by VEGF165, suggesting that TA could inhibit angiogenesis by targeting VEGFRs in HUVECs. In addition, VEGF165 enhanced the expression of VEGFRs and promoted tyrosine phosphorylation of VEGFR-1 and VEGFR-2 in normal human melanocytes, which were also attenuated by TA. Furthermore, TA showed similar effects to neutralization of VEGFR-1 and VEGFR-2 in inhibiting tyrosinase activity, melanin production and even melanogenic proteins induced by VEGF165, suggesting that TA could reduce melanogenesis via inhibiting activation of VEGFRs and subsequent expression of melanogenic proteins in melanocytes. Taken together, we demonstrate that TA can inhibit angiogenesis and melanogenesis in vitro at least in part by targeting VEGFRs, which may offer a new understanding of the pathogenesis of melasma as well as the molecular mechanism for TA in treatment of the disease.

Keywords: tranexamic acid, VEGF receptors, human umbilical vein endothelial cells, angiogenesis, melanocytes, melanogenesis

Citation styles

APA
Zhu, J.W., Ni, Y.J., Tong, X.Y., Guo, X., Wu, X.P., Lu, Z.F. (2020). Tranexamic Acid Inhibits Angiogenesis and Melanogenesis in Vitro by Targeting VEGF Receptors. International Journal of Medical Sciences, 17(7), 903-911. https://doi.org/10.7150/ijms.44188.

ACS
Zhu, J.W.; Ni, Y.J.; Tong, X.Y.; Guo, X.; Wu, X.P.; Lu, Z.F. Tranexamic Acid Inhibits Angiogenesis and Melanogenesis in Vitro by Targeting VEGF Receptors. Int. J. Med. Sci. 2020, 17 (7), 903-911. DOI: 10.7150/ijms.44188.

NLM
Zhu JW, Ni YJ, Tong XY, Guo X, Wu XP, Lu ZF. Tranexamic Acid Inhibits Angiogenesis and Melanogenesis in Vitro by Targeting VEGF Receptors. Int J Med Sci 2020; 17(7):903-911. doi:10.7150/ijms.44188. https://www.medsci.org/v17p0903.htm

CSE
Zhu JW, Ni YJ, Tong XY, Guo X, Wu XP, Lu ZF. 2020. Tranexamic Acid Inhibits Angiogenesis and Melanogenesis in Vitro by Targeting VEGF Receptors. Int J Med Sci. 17(7):903-911.

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