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1.
Skin Pharmacol Physiol ; 36(5): 235-248, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38008088

RESUMO

BACKGROUND: Curcumin is a polyphenolic compound present in turmeric (Curcuma longa). Curcumin, turmeric powder, and extracts are widely used in traditional Indian medicine and are active ingredients of dietary supplements and cosmeceutical products. The pharmacological properties of curcumin/turmeric as well as the studies performed in vitro, in animal models, and in volunteers have been the objects of a vast literature. Most of the clinical studies report on the effects of curcumin/turmeric administered orally, while only a few describe its topical applications. SUMMARY: This review focuses on clinical studies in which curcumin/turmeric was applied topically to treat various skin conditions based on its antioxidant, anti-inflammatory, and antimicrobial properties. KEY MESSAGES: The clinical studies employing curcumin/turmeric as the only active ingredient allow us to appreciate its therapeutic potential without confounding contributions coming from additional pharmacologically active substances present in the same formulation. Curcumin/turmeric was regarded as an attractive alternative to conventional drugs, such as corticosteroids and antibiotics, thanks to its characteristics of a safe and well-tolerated natural substance.


Assuntos
Curcumina , Dermatopatias , Animais , Humanos , Curcumina/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia
2.
Molecules ; 26(21)2021 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-34771020

RESUMO

Human skin is colonized by diverse commensal microbes, making up the skin microbiota (SM), contributing to skin integrity and homeostasis. Many of the beneficial effects aroused by the SM are exerted by microbial metabolites such as short-chain fatty acids (SCFAs), including butyric acid. The SCFAs can be used in cosmetic formulations against skin diseases to protect SM by preserving and/or restoring their natural balance. Unpleasant sensorial properties and unfavorable physico-chemical properties of butyrate strongly limit its cosmetic use. In contrast, some butyrate derivatives, including phenylalanine butyramide (C13H18N2O2, FBA), a solid form of butyric acid, are odorless while retaining the pharmacokinetic properties and safety profile of butyric acid. This study assessed the FBA's permeation across the skin and its soothing and anti-reddening potential to estimate its cosmetic application. The dosage method used to estimate FBA's levels was validated to be sure of analytical results. The FBA diffusion tests were estimated in vitro using a Franz-type vertical diffusion cell. The soothing action was evaluated in vivo by Colorimeter CL400, measuring the erythema index. The results suggest that the FBA represents an innovative way to exploit the benefits of butyric acid in the cosmetic fields since it cannot reach the bloodstream, is odorless, and has a significative soothing action (decrease the erythema index -15.7% after 30', and -17.8% after 60').


Assuntos
Amidas/farmacologia , Cosméticos/farmacologia , Fenilalanina/farmacologia , Substâncias Protetoras/farmacologia , Pele/efeitos dos fármacos , Amidas/química , Cosméticos/química , Humanos , Estrutura Molecular , Fenilalanina/química , Substâncias Protetoras/química , Pele/metabolismo
3.
Phytother Res ; 35(1): 530-540, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32816329

RESUMO

Facial pore enlargement is considered a significant esthetic and health concern in skincare cosmetics. The pores fulfill the critical function of keeping the skin surface hydrated and protected against microbial infections. The hyperseborrhea, the stress factors, and the hormonal triggers can cause pore size enlargement, causing higher susceptibility of the skin to microbe aggressions and inflammatory reactions. Thus, reducing excessive sebum production and keeping functional pores are two of the most requested activities in skincare cosmetics. A Cirsium eriophorum cell culture extract was investigated for its role in sebum regulation, stratum corneum desquamation, and anti-inflammation. The extract was able to regulate essential markers associated with sebum secretion and pore enlargements, such as the enzyme 5α-reductase, which plays a central role in sebum production, and the trypsin-like serine protease Kallikrein 5, which promotes skin exfoliation and antimicrobial response. Moreover, the extract showed a sebum-normalizing and pore refining activity in individuals having seborrheic or acne-prone skins, suggesting a role of the C. eriophorum extract in rebalancing altered skin conditions responsible for pore enlargement.


Assuntos
Anti-Inflamatórios/farmacologia , Cirsium/química , Extratos Vegetais/farmacologia , Sebo/metabolismo , Pele/efeitos dos fármacos , Acne Vulgar , Adulto , Técnicas de Cultura de Células , Cosméticos , Face , Feminino , Fibroblastos/efeitos dos fármacos , Células HaCaT , Humanos , Inflamação , Masculino , Pele/metabolismo , Fenômenos Fisiológicos da Pele , Adulto Jovem
4.
Artigo em Inglês | MEDLINE | ID: mdl-26302898

RESUMO

The synthesis and antihypertensive activity of a group of imidazo[1,2-a]pyridine is described. New synthesized compound have been tested both in vivo and in vitro as antagonists on Angiotensin AT1 receptor, and compared to Losartan, used as reference drug. Binding assay an Angiotensin AT1 receptor were carried on as well. Compounds 6b and 6g showed a potent antihypertensive activity and an high affinity on AT1 receptor.


Assuntos
Antagonistas de Receptores de Angiotensina/síntese química , Anti-Hipertensivos/síntese química , Antagonistas de Receptores de Angiotensina/uso terapêutico , Anti-Hipertensivos/uso terapêutico , Humanos , Modelos Moleculares
5.
J Pharm Sci ; 98(7): 2364-76, 2009 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-18973192

RESUMO

The aim of this work was to synthesize new pro-vitamins of alpha-tocopherol (VE) able to release another moiety such as an amino acid, in order to obtain a combined antioxidant and moisturizing effect upon topical application. The new derivatives were characterized and tested for sensitivity to chemical and enzymatic hydrolysis. Lipophilicity was estimated using Log capacity factor and skin retention was determined in vitro, using rabbit ear skin as barrier. Five molecules were synthesized using L-proline, L-serine, L-tyrosine, L-asparagine, and L-citrulline as amino acidic moiety. All pro-vitamins showed similar or lower lipophilicity than alpha-tocopheryl acetate (VEAc), taken as reference, and similar stability in aqueous solutions. All pro-vitamins showed to be sensitive to enzymatic hydrolysis. None of the pro-vitamins crossed the skin in significant amounts, whereas they accumulated into the skin, in both the dermis and the epidermis. They are more hydrophilic and more water-soluble than the currently used acetate.


Assuntos
Aminoácidos/síntese química , Pele/metabolismo , Vitamina E/síntese química , Vitamina E/metabolismo , alfa-Tocoferol/síntese química , alfa-Tocoferol/metabolismo , Aminoácidos/química , Animais , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/metabolismo , Esterases/metabolismo , Hidrólise , Lipídeos/química , Fígado/enzimologia , Coelhos , Absorção Cutânea , Solubilidade , Suínos , Vitamina E/análogos & derivados , Vitamina E/química , alfa-Tocoferol/análogos & derivados , alfa-Tocoferol/química
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