The First Human Clinical Trial on the Skin Depigmentation Efficacy of Glycinamide Hydrochloride

A previous study identified certain low molecular anti-melanogenic peptides that share a common sequence with α-melanocyte stimulating hormone (MSH) and end with a glycinamide moiety. Glycinamide itself also showed anti-melanogenic activity in cell-based assays, but neither glycine nor acetyl glycin...

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Main Authors: Yong Chool Boo, Da Jung Jo, Chang Min Oh, Shin Young Lee, Young Mi Kim
Format: Article
Language:English
Published: MDPI AG 2020-07-01
Series:Biomedicines
Subjects:
Online Access:https://www.mdpi.com/2227-9059/8/8/257
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author Yong Chool Boo
Da Jung Jo
Chang Min Oh
Shin Young Lee
Young Mi Kim
author_facet Yong Chool Boo
Da Jung Jo
Chang Min Oh
Shin Young Lee
Young Mi Kim
author_sort Yong Chool Boo
collection DOAJ
description A previous study identified certain low molecular anti-melanogenic peptides that share a common sequence with α-melanocyte stimulating hormone (MSH) and end with a glycinamide moiety. Glycinamide itself also showed anti-melanogenic activity in cell-based assays, but neither glycine nor acetyl glycinamide were active, which indicated a special structure and activity relationship. The aim of this study was to examine the skin depigmentation efficacy of glycinamide hydrochloride in human subjects. The primary skin irritation potential of glycinamide hydrochloride was evaluated by patch testing in 30 human subjects. The skin depigmentation efficacy of glycinamide hydrochloride was evaluated in a double-blinded clinical test in 21 human subjects. The test product and a control product were applied to designated sites on the right or left side of the face twice daily for eight weeks. Skin color parameters, i.e., the melanin index, the L* value (representing skin lightness), a* value (redness), and b* value (yellowness) were measured using instruments. The individual topology angle (ITA<sup>o</sup>, representing skin color) was calculated from L* and b values. The degree of skin pigmentation was visually assessed by two testers. The primary skin irritation test showed that a solution containing glycinamide hydrochloride up to 10% did not induce any adverse skin responses. In the efficacy test, the test product significantly reduced the melanin index, and increased L* value and ITA<sup>o</sup> after two weeks of application relative to the baseline value at the start of the test. It also significantly lowered the degree of pigmentation after 6 weeks of application, relative to the baseline value. Differences in the melanin index, L* value, ITA<sup>o</sup> and the degree of pigmentation between the test and control groups became statistically significant after six weeks or eight weeks of application. No signs of skin irritation were observed during the efficacy test. The present study suggests that glycinamide hydrochloride has great potential to be used in the control of skin hyperpigmentation.
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spelling doaj.art-14a20838b3ef4f1b8f0d2bf94eb602112023-11-20T08:35:24ZengMDPI AGBiomedicines2227-90592020-07-018825710.3390/biomedicines8080257The First Human Clinical Trial on the Skin Depigmentation Efficacy of Glycinamide HydrochlorideYong Chool Boo0Da Jung Jo1Chang Min Oh2Shin Young Lee3Young Mi Kim4Department of Molecular Medicine, School of Medicine, Kyungpook National University, Daegu 41944, KoreaDermapro Skin Research Center, Dermapro Ltd., Seoul 06684, KoreaDepartment of Molecular Medicine, School of Medicine, Kyungpook National University, Daegu 41944, KoreaRuby Crown Co., Ltd., Suite 505, Korea Mediventure Center, 76 Dongnae-ro, Dong-gu, Daegu 41061, KoreaRuby Crown Co., Ltd., Suite 505, Korea Mediventure Center, 76 Dongnae-ro, Dong-gu, Daegu 41061, KoreaA previous study identified certain low molecular anti-melanogenic peptides that share a common sequence with α-melanocyte stimulating hormone (MSH) and end with a glycinamide moiety. Glycinamide itself also showed anti-melanogenic activity in cell-based assays, but neither glycine nor acetyl glycinamide were active, which indicated a special structure and activity relationship. The aim of this study was to examine the skin depigmentation efficacy of glycinamide hydrochloride in human subjects. The primary skin irritation potential of glycinamide hydrochloride was evaluated by patch testing in 30 human subjects. The skin depigmentation efficacy of glycinamide hydrochloride was evaluated in a double-blinded clinical test in 21 human subjects. The test product and a control product were applied to designated sites on the right or left side of the face twice daily for eight weeks. Skin color parameters, i.e., the melanin index, the L* value (representing skin lightness), a* value (redness), and b* value (yellowness) were measured using instruments. The individual topology angle (ITA<sup>o</sup>, representing skin color) was calculated from L* and b values. The degree of skin pigmentation was visually assessed by two testers. The primary skin irritation test showed that a solution containing glycinamide hydrochloride up to 10% did not induce any adverse skin responses. In the efficacy test, the test product significantly reduced the melanin index, and increased L* value and ITA<sup>o</sup> after two weeks of application relative to the baseline value at the start of the test. It also significantly lowered the degree of pigmentation after 6 weeks of application, relative to the baseline value. Differences in the melanin index, L* value, ITA<sup>o</sup> and the degree of pigmentation between the test and control groups became statistically significant after six weeks or eight weeks of application. No signs of skin irritation were observed during the efficacy test. The present study suggests that glycinamide hydrochloride has great potential to be used in the control of skin hyperpigmentation.https://www.mdpi.com/2227-9059/8/8/257melaninglycinamide hydrochloridedepigmentingpigmentationskin lighteningwhitening
spellingShingle Yong Chool Boo
Da Jung Jo
Chang Min Oh
Shin Young Lee
Young Mi Kim
The First Human Clinical Trial on the Skin Depigmentation Efficacy of Glycinamide Hydrochloride
Biomedicines
melanin
glycinamide hydrochloride
depigmenting
pigmentation
skin lightening
whitening
title The First Human Clinical Trial on the Skin Depigmentation Efficacy of Glycinamide Hydrochloride
title_full The First Human Clinical Trial on the Skin Depigmentation Efficacy of Glycinamide Hydrochloride
title_fullStr The First Human Clinical Trial on the Skin Depigmentation Efficacy of Glycinamide Hydrochloride
title_full_unstemmed The First Human Clinical Trial on the Skin Depigmentation Efficacy of Glycinamide Hydrochloride
title_short The First Human Clinical Trial on the Skin Depigmentation Efficacy of Glycinamide Hydrochloride
title_sort first human clinical trial on the skin depigmentation efficacy of glycinamide hydrochloride
topic melanin
glycinamide hydrochloride
depigmenting
pigmentation
skin lightening
whitening
url https://www.mdpi.com/2227-9059/8/8/257
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