Modulation of skin androgenesis and sebum production by a dermocosmetic formulation

Crocco, Elisete Isabel; Bonifácio, Evellin Barbosa; Facchini, G; Silva, Gustavo Henrique da; Silva, Michelle Sabrina da; Pinheiro, Ana Lucia Tabarini Alves; Avelar, Paula Voltarelli Franco; Eberlin, Samara

doi:10.1111/jocd.13503

Cited by 8 publications

(9 citation statements)

References 27 publications

(41 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Interestingly, unlike another FGFR inhibitor, AZD4547, HA-P5 did not trigger the elevation of AKR1C3. AKR1C3 encodes a pivotal enzyme that catalyzes testosterone [ 62 , 85 ], which is one of the major culprits driving the formation and development of acne lesions [ 86 , 87 ]. AZD4547 treatment, on the one hand, decreased FGFRs and AR signalling; however, on the other hand, it increased the formation of androgen, demonstrating the role of fence-sitters in acne therapy.…”

Section: Discussionmentioning

confidence: 99%

Hyaluronic acid-FGF2-derived peptide bioconjugates for suppression of FGFR2 and AR simultaneously as an acne antagonist

Zhang

Cao

et al. 2023

J Nanobiotechnol

View full text Add to dashboard Cite

Acne is a chronic skin condition that has serious consequences for mental and social well-being because it frequently occurs on the face. Several acne treatment approaches have commonly been used but have been hampered by side effects or weak activity. Thus, the investigation of the safety and efficacy of anti-acne compounds is of considerable medical importance. Herein, an endogenous peptide (P5) derived from fibroblast growth factors 2 (FGF2) was conjugated to the polysaccharide hyaluronic acid (HA) to generate the bioconjugate nanoparticle HA-P5, which suppresses fibroblast growth factor receptors (FGFRs) to significantly rehabilitate acne lesions and reduce sebum accumulation in vivo and in vitro. Moreover, our results show that HA-P5 inhibits both fibroblast growth factor receptor 2 (FGFR2) and androgen receptor (AR) signalling in SZ95 cells, reverses the acne-prone transcriptome, and decreases sebum secretion. Furthermore, the cosuppression mechanism revealed that HA-P5 blocks FGFR2 activation, as well as the YTH N6-methyladenosine RNA binding protein F3 (YTHDF3) downstream molecules, including an N6-methyladenosine (m6A) reader that facilitates AR translation. More importantly, a significant difference between HA-P5 and the commercial FGFR inhibitor AZD4547 is that HA-P5 does not trigger the overexpression of aldo-keto reductase family 1 member C3 (AKR1C3), which blocks acne treatment by catalyzing the synthesis of testosterone. Overall, we demonstrate that a polysaccharide-conjugated and naturally derived oligopeptide HA-P5 can alleviate acne and act as an optimal FGFR2 inhibitor and reveal that YTHDF3 plays a crucial role in signalling between FGFR2 and AR. Graphical Abstract

show abstract

Section: Discussionmentioning

confidence: 99%

Hyaluronic acid-FGF2-derived peptide bioconjugates for suppression of FGFR2 and AR simultaneously as an acne antagonist

Zhang

Cao

et al. 2023

J Nanobiotechnol

View full text Add to dashboard Cite

show abstract

“…Testosterone is altered to the most active form of androgen, DHT, by the 5-alpha reductase enzyme [ 44 ]. Higher concentrations of the 5-alpha reductase enzyme in sebaceous glands are associated with acne-prone skin [ 45 ]. SRD5A1 , expressed as 5-alpha reductase enzyme type 1, can be found in sweat glands, hair follicles, skin, and especially in facial sebaceous glands [ 46 , 47 ].…”

Section: Resultsmentioning

confidence: 99%

In Vitro and In Vivo Regulation of SRD5A mRNA Expression of Supercritical Carbon Dioxide Extract from Asparagus racemosus Willd. Root as Anti-Sebum and Pore-Minimizing Active Ingredients

et al. 2022

View full text Add to dashboard Cite

Oily skin from overactive sebaceous glands affects self-confidence and personality. There is report of an association between steroid 5-alpha reductase gene (SRD5A) expression and facial sebum production. There is no study of the effect of Asparagus racemosus Willd. root extract on the regulation of SRD5A mRNA expression and anti-sebum efficacy. This study extracted A. racemosus using the supercritical carbon dioxide fluid technique with ethanol and investigated its biological compounds and activities. The A. racemosus root extract had a high content of polyphenolic compounds, including quercetin, naringenin, and p-coumaric acid, and DPPH scavenging activity comparable to that of the standard L-ascorbic acid. A. racemosus root extract showed not only a significant reduction in SRD5A1 and SRD5A2 mRNA expression by about 45.45% and 90.86%, respectively, but also a reduction in the in vivo anti-sebum efficacy in male volunteers, with significantly superior percentage changes in facial sebum production and a reduction in the percentages of pore area after 15 and 30 days of treatment. It can be concluded that A. racemosus root extract with a high content of polyphenol compounds, great antioxidant effects, promising downregulation of SRD5A1 and SRD5A2, and predominant facial sebum reduction and pore-minimizing efficacy could be a candidate for an anti-sebum and pore-minimizing active ingredient to serve in functional cosmetic applications.

show abstract

“…In this study, we focus on the use of botanical compounds for the treatment of oily skin, especially for the improvement of large pores [14]. It is documented that Lotus corniculatus extracts and their active components have therapeutic properties, such as anti-inflammatory effects [15,16], anti-proliferative activities [17], and antioxidant effects [18].…”

Section: Discussionmentioning

confidence: 99%

“…Dihydrotestosterone (DHT) is converted intracellularly from testosterone by the 5α-reductase enzyme and influences sebocyte proliferation, differentiation and regulation of lipid synthesis by binding to the androgen receptor on sebocytes [11][12][13]. Patients with acne have higher testosterone levels and higher DHT production rates in the skin [14].…”

Section: Introductionmentioning

confidence: 99%

Inhibition of lipogenesis and sebum secretion for Lotus corniculatus seed extract in vitro and in vivo

Cheng

Guo

2022

Intern J of Cosmetic Sci

View full text Add to dashboard Cite

Background: Botanical ingredients are widely used in hair-and skin-care products. However, few studies have investigated the effectiveness of botanical products on counteracting sebum synthesis and secretion.Objective: To investigate the composition of Lotus corniculatus seed extract (LC) and its potential inhibition of lipogenesis in SZ95 sebocytes and oily human skin. Methods:The active components of LC solutions were identified by highperformance liquid chromatography (HPLC) and nuclear magnetic resonance (NMR). The in vitro effects of LC were evaluated using SZ95 cells treated with linoleic acid (LA) and dihydrotestosterone (DHT) and incubated with LCs for 24 h and 72 h. Lipogenesis was assessed by Oil Red O and Nile Red staining of the cells. In vivo effects were assessed on 30 subjects with oily skin who were enrolled in a randomized, blank-controlled trial and were treated with LC solution for 6 h and 4 weeks. The skin sebum contents and area on the forehead and cheeks were evaluated using a Sebumeter SM815 and Sebfix sebutape with Visioscan VC98. In addition, VISIA was used to collect half-face photos for analysis. Results:A novel active molecule, 5′-o-rhamnosyl uridine, was identified in LC.LC exhibited a dose-dependent inhibitory effect on LA and DHT-induced lipid synthesis. When 5% LC was applied for 3 h, the skin sebum contents and area were significantly reduced compared with the vehicle control, with an obvious reduction after 6 h. Continued use of the serum containing 5% LC for 4 weeks resulted in a significant reduction in the skin sebum contents and area. No adverse reactions were reported during the study.Conclusions: Topical application of LC resulted in an immediate and longlasting reduction of the sebum contents and area of oily human skin by reducing sebaceous lipogenesis through the LA and DHT pathways. This indicates the potential of LC as a new biological treatment for oily skin.

show abstract

Modulation of skin androgenesis and sebum production by a dermocosmetic formulation

Cited by 8 publications

References 27 publications

Hyaluronic acid-FGF2-derived peptide bioconjugates for suppression of FGFR2 and AR simultaneously as an acne antagonist

Hyaluronic acid-FGF2-derived peptide bioconjugates for suppression of FGFR2 and AR simultaneously as an acne antagonist

In Vitro and In Vivo Regulation of SRD5A mRNA Expression of Supercritical Carbon Dioxide Extract from Asparagus racemosus Willd. Root as Anti-Sebum and Pore-Minimizing Active Ingredients

Inhibition of lipogenesis and sebum secretion for Lotus corniculatus seed extract in vitro and in vivo

Contact Info

Product

Resources

About