ANTI-AGEING


Novel third-generation vitamin A derivative


June Li - Aneco ABSTRACT


Vitamin A compounds have many physiological effects in the human body, some of which are recognized as anti- ageing active substances in the cosmetics industry. In view of the disadvantages of the first generation vitamin A (retinoic acid) and the second generation vitamin A (retinol and its esters, etc.) in cosmetic applications, such as poor stability, poor safety (irritant, phototoxic), long conversion pathway, weak efficacy etc., Aneco has developed the third generation vitamin A - hydroxybenzophenone retinate (HPR), which has excellent stability, higher safety, and more significant efficacy. As a new generation of vitamin A derivatives, HPR has great market prospects in the cosmetics industry.


Retinoids include compounds structurally related to vitamin A and compounds with vitamin A bioactivity, of which more than 4,000 are known today. Commonly, such as β-carotene (found in


various vegetables and fruits such as carrots, β-carotene enters the human body, each β-carotene molecule can be converted into two molecules of Vitamin A, which is then bound to retinol-binding proteins for plasma transport and cellular uptake.1 That is why β-carotene is called pro-vitamin


A), retinol (narrowly defined as vitamin A, mainly found in the liver, blood and retina of animals, is the form of vitamin A often referred to as vitamin A, and is the earliest vitamin A to be discovered), retinoic acid (abbreviated as RA), and so on (Figures 1, 2 and 3).


Retinoic acid RA is an active metabolite of the vitamin A class that plays an important role in the regulation of cell aggregation, differentiation, apoptosis,


proliferation, and inflammatory responses, and is highly therapeutic for skin problems, which was the first topical application of a retinoid approved by the FDA for the treatment of acne.2 RA can be called the first generation of vitamin A.


RA includes various forms such as ATRA (all-


trans retinoic acid), 9-cis-RA, 13-cis-RA, etc., and it is mainly ATRA that exerts endogenous active effects. According to the literature, the mechanism of action of RA is mainly manifested by the receptor-mediated trans-activation or transcriptional repression of RARs and RXRs.3,4,5 Trans-activation is accomplished in five


steps including ligand binding, formation of dimers (RAR/RXR), interaction with DNA, recruitment of coactivators and RNA elongation. Different RAs have different receptor binding properties. Intranuclear binding of RAR by all-trans


retinoic acid (ATRA) leads to the formation of an activated heterodimeric complex (RAR/RXR), which stimulates transcription of the target


gene by binding to the promoter region of the vitamin A response element. The interaction between the vitamin


A receptor and the nuclear transcription factor activator protein-1 (AP-1) results in the formation of a protein complex that represses the transcription of the target gene (Figure 4).6 However, RA is banned in cosmetics in most


countries (including China). Later on, people introduced the second generation of vitamin A for cosmetic use through the research of vitamin A, including retinol, retinol esters (retinyl palmitate, retinyl propionate, etc.), as shown in Table 1. For retinol to function, it is converted to RA


and related compounds through a two-step oxidation process. First, retinol is oxidized to retinaldehyde by retinol dehydrogenase (EC.1.1.1.105) or other alcohol dehydrogenases. Retinaldehyde is subsequently oxidized to


RA and others by retinaldehyde dehydrogenase (EC.1.2.1.36).7


Cellular retinoic acid-binding protein I (CRBP-I, see Figure 4) acts as a O OH OH


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Figure 1: β-carotene www.personalcaremagazine.com


Figure 2: Retinol (vitamin A)


Figure 3: Retinoic acid (RA) November 2024 PERSONAL CARE


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