Pharmacology of RALGA, a Mixture of Retinaldehyde and Glycolic Acid

Tran, Christian; Kasraee, Behrooz; Grand, Denise; Carraux, Pierre; Didierjean, Liliane; Sorg, Olivier; Saurat, Jean‐Hilaire

doi:10.1159/000082542

Cited by 24 publications

(16 citation statements)

References 59 publications

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“…Second, glycolic acid, the other component of RALGA, is a peeling compound and is known to have a skin-depigmenting property in humans [15]. We have demonstrated that the presence of glycolic acid (6.4%) in a formulation containing 0.1% RAL significantly increases the bioavailability of RAL in the mouse skin [17]. Therefore, apart from its own depigmenting ability, glycolic acid could enhance the effect of RAL.…”

Section: Discussionmentioning

confidence: 99%

The Depigmenting Effect of RALGA in C57BL/6 Mice

et al. 2005

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Background: It has been known for a long time that the topical use of retinoic acid (RA) produces mild depigmentation of human skin. However, RA has two major disadvantages for its utilisation as a topical depigmenting compound. First, RA can act as an irritant and can produce considerable erythema and exfoliation of skin. Second, RA has a relatively weak depigmenting ability compared to other known depigmenting chemicals. Objective: In this study, we show that RALGA, a combination of the less irritant retinoid retinaldehyde (RAL; 0.1%) and glycolic acid (6.4%), has a higher skin-depigmenting potential than RA 0.05% in the tail skin of C57BL/6 mice. This effect was observed in reducing the number of functioning melanocytes and/or in inhibiting their ability to synthesise melanin. In addition, the visually recognisable depigmenting effect of RALGA was evident earlier than that of RA, i.e. only after 1 week of application. RALGA may therefore serve as a depigmenting product for the treatment of skin hyperpigmentary disorders. Postacne hyperpigmented lesions represent a very common pigmentary problem among acne patients. RALGA may thus act as an anti-acne product, due to the presence of RAL – an RA precursor – which could simultaneously remove the postacne hyperpigmented lesions in such patients.

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Section: Discussionmentioning

confidence: 99%

The Depigmenting Effect of RALGA in C57BL/6 Mice

et al. 2005

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“…Topical RA and its 13-cis isomer (isotretinoin) are used as anti-acne therapeutic agents, whereas RAL is used in cosmetic formulations to slow down skin ageing or to lighten skin pigmentation [19][20][21]. On the other hand, most, if not all, depigmenting agents target tyrosinase, the enzyme that catalyzes the rate-limiting step of melanogenesis [22].…”

Section: Discussionmentioning

confidence: 99%

In Vitro Assessment of the Tolerance Profile, the Metabolism and the Potential Depigmenting Activity of New Retinoid Derivatives

Sorg¹,

Kasraee²,

Saurat³

2014

TODDISJ

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Abstract:Background: In spite of the numerous depigmenting agents available, there is an inverse relationship between safety and efficiency. Natural retinoids exert depigmenting activities in vivo, but have a narrow therapeutic window. There is thus a need for a new class of depigmenting agents that would be both safe and useful.Objective: The aim of the study was to analyse the potential interest of new retinoid derivatives as topical depigmenting agents. Methods:The tolerance profile of the new retinoids was analysed in murine BDVII keratinocytes and murine B16 melanocytes using the MTT assay. The uptake and the metabolism of the retinoids were analysed in keratinocytes and melanocytes by HPLC/UV. The cellular content of melanin was determined in melanocytes using a photometric assay.Results: Methyl-and t-butyl-4-oxoretinoate, arbutin retinoate and retinoic acid were shown to have the best depigmenting potential according to the ratio between the IC 50 for MTT assay and that for melanin content. Retinaldehyde, 4-hydroxyretinaldehyde and methyl-4-hydroxyretinoate have a good depigmenting potential too, although the therapeutic window is narrower due to a higher toxicity.Conclusion: 4-Oxoesters of retinoic acid, arbutin retinoate and 4-hydroxyretinaldehyde derivatives offer a new family of depigmenting agents acting via a different pathway than tyrosinase inhibitors.

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“…The enzyme activity of RALDH was assayed as described by Tran et al [34] , using a nonradioactive substrate for the enzyme. Thus, endogenous cytosol RA was subtracted from the cytosolic RA yield obtained after incubation with the enzyme substrates.…”

Section: Assay For the Enzyme Activity Of Raldhmentioning

confidence: 99%

Regulation of IgA Class Switch Recombination in Immunoglobulin A Nephropathy: Retinoic Acid Signaling and BATF

Peng²,

Chen³

et al. 2016

Am J Nephrol

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Background: Immunoglobulin (Ig) A nephropathy (IgAN) is the ﬁnding of immune deposits predominantly containing polymeric IgA in the glomerular mesangium on renal biopsy. Increasing evidence suggested that retinoic acid (RA) signaling selectively induces IgA isotype switching and basic leucine zipper transcription factor, ATF-like (BATF) controls the global regulators of class switch recombination (CSR) in lymphocytes. Great effort has been paid to identify whether impaired immune regulation along the ‘mucosa-bone marrow (BM) axis' play an important role in the pathogenesis of IgAN. Methods: The aim of the study was to investigate the expression of all-trans-RA (ATRA) and BATF, and to identify their impact on IgA CSR in IgAN patients and rat animal models. Blood samples and tonsillar tissue specimens were obtained from 22 patients with IgAN and 24 patients with chronic tonsillitis as control. Results: Immunohistochemical, RT-PCR and western blotting examination revealed that RA signaling and BATF productions are activated in IgAN patients compared with controls. Lipopolysaccharide and α-hemolytic streptococcus stimulation upregulated RA receptor (RAR) and BATF expression, promote IgA CSR and ATRA productions in tonsil mononuclear cells. RAR alpha (RARα) or BATF siRNA decreases IgA expression. We also built IgAN rat models and found that RARα, BATF and activation-induced cytidine deaminase were upregulated in the peripheral blood, spleen and BM. With ATRA (500 μg/kg body weight) treatment for 8 weeks, IgA deposition on glomeruli and mesangial cells proliferation increased. It also revealed that ATRA activated BATF and IgA CSR in vivo. Conclusion: These data point toward the role of RA signaling together with BATF in IgA CSR of IgAN, and the data also support the notion that mucosal immunization with neoantigen results in impaired mucosal and systemic IgA responses.

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Pharmacology of RALGA, a Mixture of Retinaldehyde and Glycolic Acid

Cited by 24 publications

References 59 publications

The Depigmenting Effect of RALGA in C57BL/6 Mice

The Depigmenting Effect of RALGA in C57BL/6 Mice

In Vitro Assessment of the Tolerance Profile, the Metabolism and the Potential Depigmenting Activity of New Retinoid Derivatives

Regulation of IgA Class Switch Recombination in Immunoglobulin A Nephropathy: Retinoic Acid Signaling and BATF

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