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1.
J Cutan Med Surg ; 27(5): 472-475, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37571839

RESUMO

BACKGROUND: Acne vulgaris is a worldwide dermatological condition that has a complex pathophysiology in which androgens play an important role. Flutamide is a first-generation non-steroidal antiandrogen that can be used for acne treatment. AIM: To evaluate the potential therapeutic efficacy and safety of topical flutamide in the treatment of acne vulgaris. METHODS: A andomized controlled study included two equal groups, each had 27 patients, with a total of 54 patients with mild to moderate acne vulgaris having inflammatory (papules and pustules) and non-inflammatory (comedones) lesions. For eight weeks, Group (A) received 1% Flutamide topical gel on the face twice daily, whereas Group (B) served as the control group. RESULT: After 8 weeks of topical Flutamide 1% gel application twice daily, there was a significant reduction in papules count, and a highly significant reduction in pustules number from baseline. LIMITATIONS: We recommend that topical Flutamide 1% gel be tried on a larger number of patients with acne vulgaris, for longer therapeutic duration and follow up periods after treatment. CONCLUSION: Patients with acne vulgaris may find topical Flutamide 1% gel to be a viable, efficient, and safe solution with few adverse effects.


Assuntos
Acne Vulgar , Exantema , Humanos , Flutamida/uso terapêutico , Acne Vulgar/tratamento farmacológico , Acne Vulgar/patologia , Géis/uso terapêutico , Resultado do Tratamento
2.
Molecules ; 27(14)2022 Jul 08.
Artigo em Inglês | MEDLINE | ID: mdl-35889274

RESUMO

Kaempferia parviflora (Black ginger) is used widely in medical fields as an anti-microorganism and anti-inflammation. In this study, the aim was to evaluate the in vitro and in vivo anti-acne efficacy of black ginger extract. The results indicate that the methanol and ethanol extracts showed the highest total phenolic contents, without a significant difference, whereas the n-hexane extract showed the highest total flavonoid content. Nine flavones were detected using UPLC-QTOF-MS, and the ethyl acetate extract showed the highest amount of 5,7-dimethoxyflavone (DMF) according to HPLC. Antibacterial activity against Staphylococcus aureus, S. epidermidis, and Cutibacterium acnes was observed. All the extracts showed antimicrobial activity against C. acnes, revealing MICs in the range of 0.015 to 0.030 mg/mL, whereas the ethyl acetate extract inhibited the growth of S. epidermidis with a MIC of 3.84 mg/mL. In addition, the ethyl acetate extract showed the highest activity regarding nitric oxide inhibition (IC50 = 12.59 ± 0.35 µg/mL). The ethyl acetate extract was shown to be safe regarding cell viability at 0.1 mg/mL. The anti-acne efficacy was evaluated on volunteers. The volunteers were treated in two groups: one administered a 0.02% ethyl acetate extract gel-cream (n = 9) and one administered a placebo (n = 9) for 6 weeks. The group treated with the gel-cream containing the extract showed 36.52 and 52.20% decreases in acne severity index (ASI) after 4 and 6 weeks, respectively, and 18.19 and 18.54% decreases in erythema, respectively. The results suggest that K. parviflora could be a potent active ingredient in anti-inflammatory and anti-acne products.


Assuntos
Acne Vulgar , Zingiberaceae , Acne Vulgar/tratamento farmacológico , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Humanos , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Propionibacterium acnes , Rizoma , Staphylococcus epidermidis
3.
Molecules ; 27(9)2022 May 02.
Artigo em Inglês | MEDLINE | ID: mdl-35566257

RESUMO

This study aimed to evaluate the phenolic profile and biological activity of the extracts from the leaves and fruits of Cotoneaster nebrodensis and Cotoneaster roseus. Considering that miscellaneous species of Cotoneaster are thought to be healing in traditional Asian medicine, we assumed that this uninvestigated species may reveal significant therapeutic properties. Here, we report the simultaneous assessment of chemical composition as well as biological activities (antioxidant, anti-inflammatory, antibacterial, and cytotoxic properties) of tested species. Complementary LC-MS analysis revealed that polyphenols (especially flavonoids and proanthocyanidins) are the overriding phytochemicals with the greatest significance in tested biological activities. In vitro chemical tests considering biological activities revealed that obtained results showed different values depending on concentration, extraction solvent as well as phenolic content. Biological assays demonstrated that the investigated extracts possessed antibacterial properties and were not cytotoxic toward normal skin fibroblasts. Given the obtained results, we concluded that knowledge of the chemical composition and biological activities of investigated species are important to achieve a better understanding of the utilization of these plants in traditional medicine and be useful for further research in their application to treat various diseases, such as skin disorders.


Assuntos
Acne Vulgar , Rosaceae , Acne Vulgar/tratamento farmacológico , Antibacterianos/uso terapêutico , Antioxidantes/química , Frutas/química , Fenóis/análise , Fenóis/farmacologia , Extratos Vegetais/química , Folhas de Planta/química , Rosaceae/química
4.
Ann Pharm Fr ; 80(2): 157-168, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34029557

RESUMO

OBJECTIVES: The chief objective of the present research was to reduce local side effects by reducing the dose, controlling the release, and improving the stability by developing and optimizing tretinoin (TRT)-loaded topical emulgel formulation. METHODS: TRT emulgel (TE) was prepared and optimized at varying ratios of excipients and using 32 optimal response surface design (ORSD). The TRT emulgel was optimized based on TRT content and in vitro release profile of TRT from formulated emulgel batches. The optimized TRT was characterized for physical properties, pH, viscosity, spreadability, extrudability, photomicroscopy, in vitro anti-acne, in vivo skin irritation, in vivo anti-inflammatory activity, and stability study. RESULTS: The FTIR and DSC analysis revealed the compatibility between TRT and formulation excipients of emulgel. The batch F5 of emulgel formulation displayed maximum drug content (98.69±1.26%), and controlled TRT release (78.27±0.69%). Thus, batch F5 was selected as an optimized batch for further characterization. The photomicroscopic analysis of optimized TE exhibited the presence of spherical globules. The pH and viscosity of optimized TE were found to be 6.20±0.12 and 3240cP respectively. Besides, the optimized TE showed good spreadability and extrudability. The in vitro anti-acne activity against Propionibacterium acne (P. acne) of optimized TE (diameter of zone of inhibition 34.54±0.26mm) was found to be the comparatively same as that of marketed Sotret® gel (diameter of zone of inhibition 36.13±0.43mm). Moreover, no sign of irritation was observed in rats treated with optimized TE indicating the safety of TE. Furthermore, the optimized TE displayed significant (p<0.01) in vivo anti-inflammatory activity when compared to marketed gel. Besides, optimized TE was found to be stable when stored in cool conditions for three months. CONCLUSION: Thus, the emulgel could be a promising approach for the topical delivery of TRT with improved performance and reduced side effects.


Assuntos
Excipientes , Tretinoína , Animais , Emulsões , Excipientes/química , Géis , Tamanho da Partícula , Ratos , Tretinoína/farmacologia
5.
Molecules ; 25(9)2020 May 05.
Artigo em Inglês | MEDLINE | ID: mdl-32380665

RESUMO

Quercus mongolica (QM)-a member of the Fagaceae family-has been used as traditional medicine in Korea, China and Mongolia as a treatment for inflammation of oral, genital or anal mucosa and for external inflammation of skin. To treat acne vulgaris (AV), we evaluated the inhibition of inflammatory cytokines (IL-6 and IL-8) of QM leaf extract (QML) and its main compound, pedunculagin (PD) in vitro and 5α-reductase inhibitory activity by western blotting. As results, QML and PD showed potent NO production inhibitory activity compared with the positive control (PC), NG-monomethyl-L-arginine (L-NMMA). QML and PD was also showed the decreases of IL-6 and IL-8 compared with the PC, EGCG and exhibited potent 5α-reductase type 1 inhibitory activities compared with the PC, dutasteride.


Assuntos
Inibidores de 5-alfa Redutase/farmacologia , Anti-Inflamatórios/farmacologia , Quercus/química , Taninos/farmacologia , Acne Vulgar/tratamento farmacológico , Linhagem Celular , Colestenona 5 alfa-Redutase/metabolismo , Regulação para Baixo , Humanos , Interleucina-6/metabolismo , Interleucina-8/metabolismo , Lipopolissacarídeos/efeitos adversos , Medicina Tradicional , Óxido Nítrico/metabolismo , Extratos Vegetais/farmacologia , Folhas de Planta/química , ômega-N-Metilarginina/metabolismo
6.
Molecules ; 25(15)2020 Jul 25.
Artigo em Inglês | MEDLINE | ID: mdl-32722482

RESUMO

One new dibenzocycloheptene, validinol (1), and one butanolide firstly isolated from the natural source, validinolide (2), together with 17 known compounds were isolated from the stem of Cinnamomum validinerve. Among the isolates, lincomolide A (3), secosubamolide (7), and cinnamtannin B1 (19) exhibited potent inhibition on both superoxide anion generation (IC50 values of 2.98 ± 0.3 µM, 4.37 ± 0.38 µM, and 2.20 ± 0.3 µM, respectively) and elastase release (IC50 values of 3.96 ± 0.31 µM, 3.04 ± 0.23 µM, and 4.64 ± 0.71 µM, respectively) by human neutrophils. In addition, isophilippinolide A (6), secosubamolide (7), and cinnamtannin B1 (19) showed bacteriostatic effects against Propionibacterium acnes in in vitro study, with minimal inhibitory concentration (MIC) values at 16 µg/mL, 16 µg/mL, and 500 µg/mL, respectively. Further investigations using the in vivo ear P. acnes infection model showed that the intraperitoneal administration of the major component cinnamtannin B1 (19) reduced immune cell infiltration and pro-inflammatory cytokines TNF-α and IL-6 at the infection sites. The results demonstrated the potential of cinnamtannin B1 (19) for acne therapy. In summary, these results demonstrated the anti-inflammatory potentials of Formosan C. validinerve during bacterial infections.


Assuntos
Acne Vulgar/tratamento farmacológico , Cinnamomum/química , Inflamação/tratamento farmacológico , Extratos Vegetais/farmacologia , Acne Vulgar/microbiologia , Acne Vulgar/patologia , Antibacterianos/química , Antibacterianos/farmacologia , Humanos , Inflamação/metabolismo , Inflamação/microbiologia , Inflamação/patologia , Testes de Sensibilidade Microbiana , Monócitos/efeitos dos fármacos , Monócitos/microbiologia , Extratos Vegetais/química , Caules de Planta/química , Propionibacterium acnes/efeitos dos fármacos , Propionibacterium acnes/patogenicidade
7.
Molecules ; 25(19)2020 Oct 06.
Artigo em Inglês | MEDLINE | ID: mdl-33036279

RESUMO

Acne is a common skin condition observed in adolescents. Nutmeg (Myristica fragrans Houtt) (MF) is a well-known traditional Chinese medicine; its major toxic components, safrole and myristicin, are rich in essential oils. Essential oils of MF (MFO) were extracted by hydrodistillation; the residue was extracted using 50% methanol (MFE-M). The minimum inhibitory concentration (MIC) of MFE-M against Cutibacterium acnes and Staphylococcus aureus was 0.64 mg. Four compounds were obtained from MFE-M: myristicin (1), (+)-erythro-Δ8'-7S,8R- dihydroxy-3,3,5'-trimethoxy-8-O-4'-neolignan (2), (+)-erythro-Δ8'-7-hydroxy-3,4,3',5'-tetramethoxy 8-O-4-neolignan (3), and erythro-Δ8'-7-acetoxy-3,4,3',5'-tetramethoxy-8-O-4'-neolignan (4). Compound 2 exerted the strongest antimicrobial activity, with MICs of 6.25 and 3.12 µg/mL against C. acnes and S. aureus, respectively. Moreover, 2 inhibited NO, PGE2, iNOS, and COX-2 levels in RAW 264.7 cells induced by LPS or heat-killed C. acnes; NO production at 50% inhibitory concentrations (IC50) was 11.07 and 11.53 µg/mL, respectively. Myristicin and safrole content was higher in MFO than in MFE-M. MFO and MFE-M caused no skin irritation after a single topical application in Wistar rats. MFE-M, with low safrole and myristicin content, did not cause skin irritation and exhibited an anti-acne effect; moreover, 2 was identified as the active substance. Therefore, MFE-M could be employed to develop anti-acne compounds for use in cosmetics.


Assuntos
Anti-Inflamatórios/farmacologia , Lignanas/química , Myristica/química , Derivados de Alilbenzenos/farmacologia , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Anti-Inflamatórios/química , Dioxolanos/farmacologia , Feminino , Propionibacteriaceae/efeitos dos fármacos , Ratos , Ratos Wistar , Safrol/farmacologia , Pele/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos
8.
BMC Complement Altern Med ; 19(1): 323, 2019 Nov 21.
Artigo em Inglês | MEDLINE | ID: mdl-31752827

RESUMO

BACKGROUND: Carpinus tschonoskii (CT) has been previously studied for various activities in the improvement of skin diseases. In the present study, we examined the in vitro anti-acne vulgaris (AV) effect of CT leaves (CTL) and tellimagrandin I (TI), one of the main ellagitannins from CT, including skin barrier improvement and 5α-reductase inhibitory activity. METHODS: To test the anti-AV activities of CTL and TI, firstly, anti-oxidative and anti-inflammatory activities including DPPH radical scavenging activity, nitric oxide (NO) inhibitory activity, and cytokines [interleukin (IL)-6 and IL-8] were tested. Skin barrier improvement experiments were tested using developing cornified envelope (CE) formation, and filaggrin mRNA expression level was determined by RT-PCR. The 5α-reductase inhibitory activity was determined by measuring the testosterone levels in rat liver microsomes. RESULTS: CTL and TI showed potent anti-oxidative activity and anti-inflammatory activities. Especially, the cytokine production inhibitory activities of TI were found to be similar to the positive control, epigallocatechin gallate (EGCG). CTL and TI enhanced the CE formation and filaggrin mRNA expression levels and showed potent activities compared to that in the positive control, 1.5 mM Ca2+. In additionally, CTL and TI showed 5α-reductase inhibitory activities in a dose-dependent manner. CONCLUSION: The results showed that CTL and TI inhibit AV endogenous factors such as 5α-reductase and inflammatory cytokines and affect exogenous factors such as developing skin barrier function (CE and filaggrin levels). Therefore, CTL and TI may be plant-derived agent, promising in the treatment of acne vulgaris.


Assuntos
Inibidores de 5-alfa Redutase/farmacologia , Betulaceae , Ácido Gálico/análogos & derivados , Glucosídeos/farmacologia , Extratos Vegetais/farmacologia , Acne Vulgar , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Citocinas/metabolismo , Proteínas Filagrinas , Ácido Gálico/farmacologia , Humanos , Camundongos , Extratos Vegetais/química , Folhas de Planta/química , Células RAW 264.7
9.
Phytother Res ; 33(3): 584-590, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30506753

RESUMO

Acne is a chronic inflammatory disease of the skin that occurs when bacteria abnormally grow in hair follicles. The most common treatment is antibiotics, but they are limited due to antibiotic resistance. The purpose of this study was to identify the active ingredients of the antimicrobial effects of red ginseng (Panax ginseng C.A. Meyer), compare it to existing antibacterial substances, and determine its potential efficacy as a natural drug product. The hydrophobic fraction in red ginseng ethanol extract (RGEF) showed the same or better antimicrobial activity against Propionibacterium acnes than benzoyl peroxide or azelaic acid. In addition, the antimicrobial component derived from red ginseng selectively showed a high antimicrobial effect on P. acnes. Nuclear magnetic resonance spectroscopic analysis showed that the active antimicrobial substance in this fraction was panaxynol and panaxydol. Twenty subjects who had acne symptoms were treated with cream containing 3 mg/g of RGEF for 4 weeks. It was found that oxidized sebum contents and redness of the skin were reduced, and symptoms of the early to middle stage of acne were effectively improved. This study showed that red ginseng extract containing panaxynol and panaxydol can effectively control the symptoms of acne.


Assuntos
Acne Vulgar/tratamento farmacológico , Antibacterianos/farmacologia , Panax/química , Extratos Vegetais/farmacologia , Adulto , Antibacterianos/isolamento & purificação , Fracionamento Químico , Cromatografia Líquida de Alta Pressão , Cosméticos , Di-Inos/isolamento & purificação , Di-Inos/farmacologia , Álcoois Graxos/isolamento & purificação , Álcoois Graxos/farmacologia , Feminino , Humanos , Interações Hidrofóbicas e Hidrofílicas , Masculino , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Pele/efeitos dos fármacos , Creme para a Pele/química , Adulto Jovem
10.
Molecules ; 23(2)2018 Feb 13.
Artigo em Inglês | MEDLINE | ID: mdl-29438284

RESUMO

Azelaic acid (AzA) and its derivatives have been known to be effective in the treatment of acne and various cutaneous hyperpigmentary disorders. The esterification of azelaic acid with lauryl alcohol (LA) to produce dilaurylazelate using immobilized lipase B from Candida antarctica (Novozym 435) is reported. Response surface methodology was selected to optimize the reaction conditions. A well-fitting quadratic polynomial regression model for the acid conversion was established with regards to several parameters, including reaction time and temperature, enzyme amount, and substrate molar ratios. The regression equation obtained by the central composite design of RSM predicted that the optimal reaction conditions included a reaction time of 360 min, 0.14 g of enzyme, a reaction temperature of 46 °C, and a molar ratio of substrates of 1:4.1. The results from the model were in good agreement with the experimental data and were within the experimental range (R² of 0.9732).The inhibition zone can be seen at dilaurylazelate ester with diameter 9.0±0.1 mm activities against Staphylococcus epidermidis S273. The normal fibroblasts cell line (3T3) was used to assess the cytotoxicity activity of AzA and AzA derivative, which is dilaurylazelate ester. The comparison of the IC50 (50% inhibition of cell viability) value for AzA and AzA derivative was demonstrated. The IC50 value for AzA was 85.28 µg/mL, whereas the IC50 value for AzA derivative was more than 100 µg/mL. The 3T3 cell was still able to survive without any sign of toxicity from the AzA derivative; thus, it was proven to be non-toxic in this MTT assay when compared with AzA.


Assuntos
Ácidos Dicarboxílicos/química , Dodecanol/química , Enzimas Imobilizadas/química , Ésteres/química , Proteínas Fúngicas/química , Lipase/química , Animais , Biocatálise , Sobrevivência Celular/efeitos dos fármacos , Ácidos Dicarboxílicos/farmacologia , Ésteres/farmacologia , Análise Fatorial , Cinética , Camundongos , Testes de Sensibilidade Microbiana , Modelos Estatísticos , Células NIH 3T3 , Staphylococcus epidermidis/efeitos dos fármacos , Staphylococcus epidermidis/crescimento & desenvolvimento
11.
Int J Mol Sci ; 18(5)2017 May 11.
Artigo em Inglês | MEDLINE | ID: mdl-28492484

RESUMO

The leaves of loquat (Eriobotrya japonica) possess high medicinal value and have been used as traditional medicines. However, there are no evidence-based studies on the skin-care effects of E. japonica leaves. To explore new biological activities of E. japonica leaves against skin disorder and to gain a better understanding of the chemical components associated with bioactivities, we evaluated 18 triterpenoids from E. japonica leaves on anti-melanogenesis, anti-acne, anti-allergy and anti-aging activities. Our results revealed that eight compounds showed anti-melanogenesis activity, of which ursolic acid (1) and maslinic acid (7) were the most potent with the similar selective index to that of arbutin. Structure-activity relationship and possible mechanism of active compounds were proposed. Twelve compounds exhibited anti-acne effect; ursolic acid (1), maslinic acid (7), corosolic acid (8) and euscaphic acid (12) showed highest activities against P. acnes. Four compounds displayed anti-allergy and anti-inflammatory activity; 3-epicorosolic acid (9) and euscaphic acid (12) showed marked activity against ß-hexosaminidase release. Finally, ursolic acid (1), pomolic acid (10), colosolic acid (8) and its methylated derivative (6) exhibited the highest anti-aging activity by stimulating collagen and hyaluronic acid (HA) production. Our findings provide valuable evidence that E. japonica leaves have potential applications as ingredients of function foods or cosmetics for health benefits and a number of triterpenoids may play an important role in these bioactivities.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Eriobotrya/química , Dermatopatias/tratamento farmacológico , Dermatopatias/prevenção & controle , Triterpenos/uso terapêutico , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Colágeno/efeitos dos fármacos , Relação Dose-Resposta a Droga , Humanos , Ácido Hialurônico/biossíntese , Concentração Inibidora 50 , Melaninas/biossíntese , Camundongos , Extratos Vegetais/química , Folhas de Planta/química , Envelhecimento da Pele/efeitos dos fármacos , Triterpenos/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologia , beta-N-Acetil-Hexosaminidases/efeitos dos fármacos
12.
Exp Dermatol ; 23(4): 290-3, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24690039

RESUMO

For decades, retinoic acid (RA) is known as the most potent therapeutic option in the therapy of acne and altered homeostasis of endogenous retinoids has been discussed in the context of acne pathogenesis. Besides retinoids, antibiotics such as tetracyclines or erythromycin are well established in acne pharmacotherapy. Accumulating evidence points towards common molecular pathways being targeted by both RA and anti-acne antibiotics; however, a precise 'common denominator' connecting these chemically diverse anti-acne agents has not yet been identified. Interestingly, tetracyclines are associated with the occurrence of pseudotumor cerebri, a rare neurological side effect otherwise associated with retinoid intoxication or RA exposure. This association at the clinical level suggests an interaction between tetracyclines and endogenous RA signalling. As erythromycin does not cross the blood brain barrier, CNS side effects are not to be expected, yet not precluding a possible local interaction of erythromycin with endogenous RA metabolism in the skin. We hypothesize tetracyclines and erythromycin to locally inhibit endogenous RA metabolism in the skin and thus mimic therapeutic action of RA. This readily testable hypothesis suggests inhibition of endogenous RA metabolism and amplification of endogenous RA signalling as a mechanism underlying the biochemical actions of antibiotics in acne therapy. Elucidation of such interactions may ultimately enhance our understanding of acne therapy and pathogenesis and may yield a sound, scientific basis for hypothesis-driven development of novel therapeutic compounds.


Assuntos
Acne Vulgar/tratamento farmacológico , Eritromicina/farmacologia , Tetraciclinas/farmacologia , Tretinoína/metabolismo , Acne Vulgar/metabolismo , Sistema Enzimático do Citocromo P-450/metabolismo , Eritromicina/uso terapêutico , Humanos , Tetraciclinas/uso terapêutico
13.
J Steroid Biochem Mol Biol ; 237: 106427, 2024 03.
Artigo em Inglês | MEDLINE | ID: mdl-38008365

RESUMO

Ecdysteroids, a class of naturally isolated polyhydroxylated sterols, stands at a very good place in the pharmaceutical industry from their medicinal point of views like anti-inflammatory, neuroprotective, anti-microbial, anti-diabetic, antioxidant, and anti-tumor effects. Due to their excellent antioxidant and anti-microbial potential, ecdysteroids have extensive use in skin products, especially derma creams. To monitor the best anti-acne phytoecdysteroids, here made use of different computational approaches, by using the rapid, easy, cost-effective and high throughput method to screen and identify ecdysteroids as androgen receptor inhibitors. 3D-QSAR study was carried out on a dataset of ecdysteroids by using comparative molecular field analysis (CoMFA) to determine the factors responsible for the activity of compounds. Statistically a cross-validated (q2) 0.1457 and regression coefficient (r2) 0.9713 indicated the best model. Contour map results showed the influence of steric effect to enhance activity. A molecular docking analysis was done to further find out the binding sites and their anti-acne potential against three crystal structured macromolecules (PDB ID: 2REQ, 2BAC, 4EM0). Docking results were further evaluated by prime MM-GBSA analysis and findings confirmed the accuracy. Toxicity by ADMET assessment was carried out and M2 was found as lead druglike with best anti-acne activity against Propionium acnes GehA lipase bacteria after passing all filters. This research study is novel because it is representing first effort to explore ecdysteroids class for their high therapeutic output as androgen receptor inhibitor by using computational tools and expectedly led to novel scaffold for androgen receptor inhibitor. This is a novel and new approach to investigate the ecdysteroids for first time for their practical applications.


Assuntos
Relação Quantitativa Estrutura-Atividade , Receptores Androgênicos , Simulação de Acoplamento Molecular , Ecdisteroides , Antioxidantes
14.
Z Naturforsch C J Biosci ; 79(3-4): 47-60, 2024 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-38549398

RESUMO

Garcinia mangostana fruits are used traditionally for inflammatory skin conditions, including acne. In this study, an in silico approach was employed to predict the interactions of G. mangostana xanthones and benzophenones with three proteins involved in the pathogenicity of acne, namely the human JNK1, Cutibacterium acnes KAS III and exo-ß-1,4-mannosidase. Molecular docking analysis was performed using Autodock Vina. The highest docking scores and size-independent ligand efficiency values towards JNK1, C. acnes KAS III and exo-ß-1,4-mannosidase were obtained for garcinoxanthone T, gentisein/2,4,6,3',5'-pentahydroxybenzophenone and mangostanaxanthone VI, respectively. To the best of our knowledge, this is the first report of the potential of xanthones and benzophenones to interact with C. acnes KAS III. Molecular dynamics simulations using GROMACS indicated that the JNK1-garcinoxanthone T complex had the highest stability of all ligand-protein complexes, with a high number of hydrogen bonds predicted to form between this ligand and its target. Petra/Osiris/Molinspiration (POM) analysis was also conducted to determine pharmacophore sites and predict the molecular properties of ligands influencing ADMET. All ligands, except for mangostanaxanthone VI, showed good membrane permeability. Garcinoxanthone T, gentisein and 2,4,6,3',5'-pentahydroxybenzophenone were identified as the most promising compounds to explore further, including in experimental studies, for their anti-acne potential.


Assuntos
Acne Vulgar , Benzofenonas , Garcinia mangostana , Simulação de Acoplamento Molecular , Xantonas , Xantonas/química , Xantonas/farmacologia , Benzofenonas/química , Benzofenonas/farmacologia , Garcinia mangostana/química , Humanos , Acne Vulgar/tratamento farmacológico , Acne Vulgar/microbiologia , Simulação de Dinâmica Molecular , Proteína Quinase 8 Ativada por Mitógeno/metabolismo , Proteína Quinase 8 Ativada por Mitógeno/química , Simulação por Computador , Ligação de Hidrogênio
15.
Int J Pharm ; 654: 123980, 2024 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-38460769

RESUMO

Solid lipid microparticles (SLMs) represent a promising approach for drug delivery in anti-acne applications. In this study, asiatic acid-loaded SLMs (AASLMs) were prepared by melt emulsification method in conjunction with freeze-drying. Comprehensive evaluations comprised particle size, %entrapment efficiency (%EE), %labeled amount (%LA), surface morphology, stability, %release, %skin permeation, and anti-acne activity. The AASLMs exhibited an average particle size ranging from 7.46 to 38.86 µm, with %EE and %LA falling within the range of 31.56 to 100.00 and 90.43 to 95.38, respectively. The AASLMs demonstrated a spherical shape under scanning electron microscopy, and maintained stability over a 3-month period. Notably, formulations with 10 % and 15 % cetyl alcohol stabilized with poloxamer-188 (specifically F6 and F12) displayed a minimum inhibitory concentration (MIC) value of 75 mg/ml against Cutibacterium acnes. Furthermore, F12 exhibited a higher %release and %skin permeation compared to F6 over 24 h. In a single-blind clinical trial involving fifteen participants with mild-to-moderate acne, F12 showcased its potential not only in reducing porphyrin intensity and enhancing skin barriers but also in significantly improving skin hydration and brightness. However, further investigations with larger subject cohorts encompassing diverse age groups and genders are necessary to thoroughly establish the performance of the developed AASLMs.


Assuntos
Acne Vulgar , Sistemas de Liberação de Medicamentos , Triterpenos Pentacíclicos , Feminino , Humanos , Masculino , Acne Vulgar/tratamento farmacológico , Portadores de Fármacos , Sistemas de Liberação de Medicamentos/métodos , Lipídeos , Tamanho da Partícula , Método Simples-Cego
16.
J Cosmet Dermatol ; 23(6): 2156-2169, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38406887

RESUMO

BACKGROUND: Acne is a common skin issue that typically occurs during adolescence. It causes long-lasting redness and swelling in the skin. An alternative approach to treating acne could involve using a cosmetic facial mask containing herbal ingredients such as Curcumin and Rosa Damascena extract for its antibacterial properties. AIMS: This study aims to create and try out a peel-off mask gel made from Curcumin and R. Damascena extract. This gel is intended to have the ability to kill bacteria such as Staphylococcus aureus, Escherichia coli, and Propionibacterium acnes and remove dead cells from the skin surface. METHODS: The peel-off mask was made using polyvinyl alcohol (PVA) in 8% and 10% as solidifier. The evaluation of peel-off masks comprises the examination of physiochemical and mechanical aspects. Furthermore, their longevity, effectiveness, and antibacterial properties are also considered. RESULTS: The white color, pleasant smell, and soft texture were the defining features of the peel-off gel mask. The changes in PVA affect the pH level, thickness, and how quickly the peel-off mask dries. The stability test found that the peel-off mask had no significant physical changes when exposed to freezing and thawing. However, there were some differences in color and separation when using the real-time method. A prepared peel-off mask containing 10% PVA and curcumin works best against P. acne. The amount of PVA in the formula affected the physical and chemical qualities, but it did not impact on the antibacterial abilities of the peel-off mask gel. The best formula that gives the best results uses 10% PVA + curcumin. CONCLUSIONS: Using the Curcumin and R. Damascena extract in the creation of the peel-off mask gel ensures its efficacy and safety for skin application.


Assuntos
Acne Vulgar , Antibacterianos , Antioxidantes , Curcumina , Extratos Vegetais , Rosa , Staphylococcus aureus , Curcumina/farmacologia , Curcumina/administração & dosagem , Extratos Vegetais/farmacologia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Rosa/química , Humanos , Antibacterianos/farmacologia , Antibacterianos/administração & dosagem , Antioxidantes/farmacologia , Antioxidantes/administração & dosagem , Acne Vulgar/tratamento farmacológico , Acne Vulgar/microbiologia , Staphylococcus aureus/efeitos dos fármacos , Propionibacterium acnes/efeitos dos fármacos , Álcool de Polivinil/química , Escherichia coli/efeitos dos fármacos , Creme para a Pele/administração & dosagem , Pele/efeitos dos fármacos , Pele/microbiologia , Testes de Sensibilidade Microbiana
17.
Fitoterapia ; 164: 105375, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36511341

RESUMO

We collected stingless bee propolis Tetragonula biroi in order to find materials for medicine and cosmetics applications from tropical rainforest resources. Even though this bee has some biological functions including a cancer cell line, hair growth promotion, asthma remedy, α-glucosidase enzyme inhibition, and antiviral action, the investigation on anti-acne has not been reported yet. This study was to focus on propolis Tetragonula biroi extracts and leads us to isolate active compounds for antioxidant, anti-inflammatory, and anti-acne. We used methanol to obtain the extract from this propolis and assayed it with antioxidants, anti-inflammation, and anti-acne. The extract showed strong activity in antioxidants by DPPH radical scavenging activity (82.31% in 6.25 µg/ml). Via a column chromatography and Reveleris PREP purification system, we isolated 3'-O-methyldiplacone, nymphaeol A, and 5,7,3',4'-tetrahydroxy-6-geranyl flavonol. These compounds showed potential biological activity with IC50 for antioxidant 6.33, 15.49, 17.32 µM; and antiinflammatory 121.54, 121.20, 117.31 µM. The isolated compounds showed anti-acne properties with properties 0.00, 14.11, and 13.78 mm for the inhibition zone (at a concentration of 1 µg/well), respectively. The results indicated that the propolis extract of Tetragonula biroi has the potential to be developed as a cosmetic agent; however, further work needs to be done to clarify its application.


Assuntos
Própole , Animais , Própole/química , Antioxidantes/farmacologia , Antioxidantes/química , Estrutura Molecular , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Flavonóis
18.
Artigo em Inglês | MEDLINE | ID: mdl-37403398

RESUMO

Ongoing development in cosmetics is increasingly making use of probiotics, which are defined as "live microorganisms with health-enhancing properties mediated through ingestion or topical application to the host". The observation that several bacterial strains augment normal processes of healthy tissue maintenance, particularly for the skin, has opened up new avenues for the use of bacterial strains in cosmetics. A principal feature of such "cosmeceuticals" is an application of increasing insight into the biochemical nature of the skin's normal microbial flora, also called its microbiome. The opportunity of manipulating the skin microbiome to address various skin disorders has revealed novel routes for treatment. The skin microbiome manipulation approaches to address various skin disorders include skin microbiome transplantation, skin bacteriotherapy, and prebiotic stimulation. Research in this field has revealed that medical outcome-targeted manipulation of skin microbiome bacterial strain makeup may significantly increase skin health and appearance. Commercial availability of probiotic skincare products is rapidly expanding worldwide due to satisfactory laboratory results and public perception of probiotics as being intrinsically more wholesome than other bioactive substances, such as synthetics. Major outcomes of probiotic use include a significant reduction in skin wrinkling, acne and other conditions adversely affecting skin appearance and healthy function. Moreover, probiotics may additionally promote normal skin hydration, resulting in a vibrant and lustrous appearance. Nevertheless, significant technical challenges remain for the full optimization of probiotics in cosmetic products. This article summarizes the evolving nature of this field and explores current probiotic research initiatives, along with regulatory aspects and significant challenges in the manufacturing of cosmetics in the context of market expansion for these products.

19.
Res Pharm Sci ; 17(5): 457-467, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36386483

RESUMO

Background and purpose: Garcinia mangostana, simply known as mangosteen, has long been used by Thai traditional medicine because of its reported antibacterial and anti-inflammatory activities for the treatment of skin infections. In this study, mangosteen pericarps were developed into a hydrogel patch to eradicate acne-inducing bacteria. Experimental procedure: The G. mangostana extract was investigated for bactericidal activity. A hydrogel patch containing the extract was examined for mechanical properties, antibacterial activity, in vitro release, skin permeation, and a phase I clinical study of skin irritation and allergic testing by a closed patch test. Finding/Results: The G. mangostana hydrogel patch made from carrageenan and locust bean gum powders was yellow in color, smooth, durable, and flexible. This G. mangostana hydrogel patch was effective against Cutibacterium acnes, Staphylococcus epidermidis, and Staphylococcus aureus. The active ingredient, α-mangostin, was released and permeated from the G. mangostana hydrogel patch within the first 30 min at 33.16 ± 0.81% and 32.96± 0.97%, respectively. The G. mangostana hydrogel patch showed no irritation in 30 healthy volunteers. However, two volunteers had delayed allergic contact dermatitis to 0.5% (w/w) G. mangostana hydrogel patch. Conclusion and implication: This hydrogel patch containing G. mangostana ethanolic extract is not recommended for patients who have any reaction to mangosteen but has utility as an anti-acne facial mask.

20.
J Cosmet Dermatol ; 21(2): 501-505, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33825313

RESUMO

Shikimic acid (SA) has been mainly used in the pharmaceutical industry for production of drugs, however, recently it has also appeared in the world of cosmetics. So far, there have not been many publications on cosmetics containing SA or research studies on the compound, especially those that would involve testing cosmetic products on subjects. The main source of SA is star anise. The recommended concentration of SA in cosmetic preparations ranges between 1 and 5%. The pH of a 5% solution of SA in water is 3. SA at a concentration of 5% has a similar exfoliative effect to that of 50% glycolic acid. It shows antiviral, exfoliating, deodorizing, anti-acne, anti-dandruff, whitening and moisturizing activity. It also regulates the amount of secreted sebum, moreover, it has antibacterial, anti-inflammatory, hair-growth stimulating, anti-aging effect and antifungal properties.


Assuntos
Acne Vulgar , Cosméticos , Acne Vulgar/tratamento farmacológico , Anti-Inflamatórios/uso terapêutico , Cosméticos/uso terapêutico , Humanos , Sebo , Ácido Chiquímico/uso terapêutico
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