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1.
J Pharmacopuncture ; 15(2): 20-3, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-25780638

RESUMO

Panax ginseng is a well-known herbal medicine in traditional Asian medicine, and wild ginseng is widely accepted to be more active than cultivated ginseng in chemoprevention. However, little has actually been reported on the difference between wild ginseng and cultivated ginseng. Thus, to identify and analyze those differences, we used suppressive subtraction hybridization (SSH) sequences with microarrays, realtime polymerase chain reaction (PCR), and reverse transcription PCRs (RT-PCRs). One of the clones isolated in this research was the chloroplast rpoC1 gene, a ß subunit of RNA polymerase. Real-time RT-PCR results showed that the expression of the rpoC1 gene was significantly upregulated in wild ginseng as compared to cultivated ginseng, so, we conclude that the rpoC1 gene may be one of the important markers of wild ginseng.

2.
Int J Pharm ; 419(1-2): 154-60, 2011 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-21839822

RESUMO

Various amide prodrugs of salicylic acid were synthesised, and their physicochemical properties including lipophilicity, chemical stability and enzymatic hydrolysis were investigated. In vivo skin permeation and accumulation profiles were also evaluated using a combination of common permeation enhancing techniques such as the use of a supersaturated solution of permeants in an enhancer vehicle, a lipophilic receptor solution, removal of the stratum corneum and delipidisation of skin. Their capacity factor values were proportional to the degree of carbon-carbon saturation in the side chain. All these amides were highly stable in acetonitrile and glycerine. Amide prodrugs were converted to salicylic acid both in hairless mouse liver and skin homogenates. N-dodecyl salicylamide (C12SM) showed the lowest permeation of salicylic acid in skin compared to the other prodrugs, probably due to its low aqueous solubility. It had a high affinity for the stratum corneum and its accumulation was restricted to only the uppermost layer of skin. Thus, this amide prodrug could be a safer topical sunscreen agent with minimum potential for systemic absorption.


Assuntos
Salicilatos/farmacocinética , Absorção Cutânea , Protetores Solares/farmacocinética , Administração Cutânea , Amidas/síntese química , Amidas/química , Amidas/farmacocinética , Animais , Estabilidade de Medicamentos , Técnicas In Vitro , Fígado/metabolismo , Camundongos , Camundongos Pelados , Permeabilidade , Pró-Fármacos , Salicilatos/síntese química , Salicilatos/química , Pele/metabolismo , Solubilidade , Protetores Solares/síntese química , Protetores Solares/química
3.
Drug Dev Ind Pharm ; 37(7): 841-8, 2011 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-21244220

RESUMO

The purpose of this study was to investigate the physicochemical properties and in vitro evaluation of fatty ester prodrugs of salicylic acid for ultraviolet (UV) protection. The physicochemical properties such as lipophilicity, chemical stability and enzymatic hydrolysis were investigated with the following fatty ester prodrugs of salicylic acid: octanoyl (C8SA), nonanoyl (C9SA), decanoyl (C10SA), lauroyl (C12SA), myristoyl (C14SA) and palmitoyl oxysalicylate (C16SA). Furthermore, their skin permeation and accumulation were evaluated using a combination of common permeation enhancing techniques such as the use of a lipophilic receptor solution, removal of stratum corneum and delipidization of skin. Their k' values were proportional to the degree of carbon-carbon saturation in the side chain. All these fatty esters were highly stable in 2-propanol, acetonitrile and glycerin, but unstable in methanol and ethanol. They were relatively unstable in liver and skin homogenates. In particular, C16SA was mostly hydrolyzed to its parent compound in hairless mouse liver and skin homogenates, suggesting that it might be converted to salicylic acid after its topical administration. In the skin permeation and accumulation study, C16SA showed the poorest permeation in all skins, suggesting that it could not be permeated in the skin. Furthermore, C14SA and C16SA were less accumulated in delipidized skin compared with normal skin or stripped skin, suggesting that these esters had relatively strong affinities for lipids compared with the other prodrugs in the skin. C16SA showed significantly higher dermal accumulation in all skins compared with its parent salicylic acid. Thus, the palmitoyl oxysalicylate (C16SA) might be a potential candidate for UV protection due to its absence of skin permeation, smaller uptake in the lipid phase and relatively lower skin accumulation.


Assuntos
Pró-Fármacos/química , Pró-Fármacos/farmacologia , Salicilatos/química , Salicilatos/farmacologia , Protetores Solares/química , Protetores Solares/farmacologia , Animais , Avaliação Pré-Clínica de Medicamentos , Estabilidade de Medicamentos , Ácidos Graxos/química , Ácidos Graxos/farmacocinética , Ácidos Graxos/farmacologia , Técnicas In Vitro , Camundongos , Camundongos Pelados , Pró-Fármacos/farmacocinética , Salicilatos/farmacocinética , Pele/efeitos dos fármacos , Pele/metabolismo , Pele/efeitos da radiação , Absorção Cutânea , Protetores Solares/farmacocinética , Raios Ultravioleta/efeitos adversos
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