Abstract:
BACKGROUND:Hydroquinone (HQ) and salicylic acid (SA) are drugs for treating melasma through the mechanisms of tyrosinase inhibition and chemical peeling, respectively. Their high frequency of causing skin irritation has led to limited use of both drugs. OBJECTIVES:We designed the new conjugates obtained by joining HQ and SA by the co-drug concept for evaluating cutaneous absorption capability. METHODS:Monoester (4-hydroxyphenyl 2-hydroxybenzoate, HPH) and diester (1,4-phenylene bis(2-hydroxybenzoate), PBH) forms of the conjugates were synthesized and physicochemically characterized. The enzymatic hydrolysis to the parent drugs was examined. Both an equimolar dose and a saturated solubility were utilized as the applied dose for testing cutaneous absorption via pig and nude mouse skins. RESULTS:The conjugates had higher lipophilicity, less aqueous solubility, and a lower melting point/crystallinity than the parent drugs. Both conjugates showed a quick conversion into the parent drugs in esterases and skin homogenates, with PBH showing the greater hydrolysis. The hydrolysis level in skin after topical application was less as compared to that in esterases and homogenates. The tyrosinase inhibition (%) and molecular docking demonstrated that the conjugates possessed skin-lightening capability (3% for HPH and 7% for PBH) although this activity was lower than that of HQ (23%). The conjugates showed an increased skin deposition compared to the respective parent drugs. Total absorption of HPH and PBH led to a 13- and 19-fold enhancement in cutaneous retention compared to HQ alone. A similar increment of skin deposition was shown for the conjugates when compared to SA. Contrary to skin reservoir retention, transdermal transport across the skin was decreased by the conjugates, especially for PBH. This indicates the maximization of cutaneous targeting by the conjugates. CONCLUSIONS:Topically applied HPH and PBH can be the new candidates for treating melasma due to efficient skin absorption and acceptable skin tolerance.
journal_name
J Dermatol Scijournal_title
Journal of dermatological scienceauthors
Hsieh PW,Aljuffali IA,Fang CL,Chang SH,Fang JYdoi
10.1016/j.jdermsci.2014.08.013subject
Has Abstractpub_date
2014-11-01 00:00:00pages
120-31issue
2eissn
0923-1811issn
1873-569Xpii
S0923-1811(14)00212-6journal_volume
76pub_type
杂志文章abstract:BACKGROUND:Merkel cell carcinoma (MCC) is a neuroendocrine cancer of the skin postulated to originate through Merkel cell polyomavirus (MCPyV) oncogenesis and/or by mutations in molecules implicated in the regulation of cell growth and survival. Despite the fact that MCPvV is detected more broadly within the population...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/j.jdermsci.2015.04.002
更新日期:2015-07-01 00:00:00
abstract::In order to investigate the mode of action of testosterone (T) on human hair follicles we studied the metabolism of T and localization of androgen receptors in outer root sheath cells (ORSC) and dermal papilla cells (DPC) from different body sites. T was principally metabolized to androstenedione (delta 4) even in bea...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/0923-1811(94)90040-x
更新日期:1994-07-01 00:00:00
abstract::Large numbers of pigmented melanocytes are located in human hair follicles, predominantly around the dermal papillae, and the number of melanocytes and the melanogenic activity of the hair follicles are closely related to the hair cycle. We found that cultured human dermal papilla cells secreted a melanocyte chemoattr...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/s0923-1811(01)00145-1
更新日期:2002-01-01 00:00:00
abstract::Annexins (AX) or lipocortins are a family of calcium and phospholipid binding proteins that have been implicated to play a role in the regulation of inflammation and cellular differentiation. To investigate a potential role of AX in skin disorders we studied the distribution of six different AX in normal human skin (N...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/0923-1811(93)90043-o
更新日期:1993-12-01 00:00:00
abstract::Survival and extracellular matrix gene expression were studied by viable cell count assay and Northern transfer analysis to compare the sensitivity of normal skin and keloid fibroblasts towards x-irradiation. As the dosage of radiation increased, the numbers of viable cells in irradiated groups were remarkably decreas...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/0923-1811(94)90318-2
更新日期:1994-08-01 00:00:00
abstract::Considerable evidence suggests that factor XIIIa, a blood coagulation factor, also functions in tissue repair, and specifically in the dynamic process of fibroplasia. On the other hand, the dynamic process of tissue expansion would require a loosening of the dermis, the opposite of fibroplasia. We examined the effects...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/0923-1811(91)90044-x
更新日期:1991-01-01 00:00:00
abstract::In order to know the possible effects of gastrin releasing peptide (GRP) on nevus cells and melanocytes, we studied the effect of GRP on the proliferation of cultured human nevus cells and normal melanocytes. MTS assay showed that GRP stimulated the growth of viable melanocytes at 1000 ng/ml. GRP also stimulated the g...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/s0923-1811(97)00079-0
更新日期:1998-06-01 00:00:00
abstract:BACKGROUND:In vivo application of confocal Raman spectroscopy (CRS) allows non-invasive depth measurement of the skin. Thereby obtained knowledge of the skin composition is essential to reliably assess the actual skin state. Besides other components, the skin cholesterol concentration is of interest; however, little is...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/j.jdermsci.2017.08.002
更新日期:2017-12-01 00:00:00
abstract::p53, A tumor suppressor gene, has been documented as the most frequently mutated gene in human cancers including non-melanoma skin tumors. It has been controversial whether the p53 gene mutation plays a major role for melanoma genesis. To examine the role of p53 in human malignant melanoma carcinogenesis, we performed...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/0923-1811(95)00465-3
更新日期:1996-06-01 00:00:00
abstract:BACKGROUND:Currently available topical treatments for actinic keratosis (AK) are associated with substantial side-effects. OBJECTIVES:To evaluate the efficacy and safety of topical SR-T100 gel in treating AK. METHODS:A multicenter, randomized, double-blinded phase III trial was conducted. Patients with at least two c...
journal_title:Journal of dermatological science
pub_type: 杂志文章,多中心研究,随机对照试验
doi:10.1016/j.jdermsci.2018.02.015
更新日期:2018-06-01 00:00:00
abstract:BACKGROUND:Pseudoxanthoma elasticum (PXE) is an autosomal recessive metabolic disorder with ectopic mineralization in the skin, eyes and cardiovascular system. PXE is caused by mutations in ABCC6. OBJECTIVE:To examine 54 unrelated South African PXE patients for ABCC6 PXE causing mutations. METHODS:Patients were scree...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/j.jdermsci.2009.02.008
更新日期:2009-06-01 00:00:00
abstract:BACKGROUND:Sarcoidosis is a systemic granulomatous disease characterized by the combination of Th1 and Th17 responses. Recently, several arguments have suggested a potential involvement of B cells as well as T cells in the pathogenesis of sarcoidosis. Follicular helper CD4+ T (TFH) cells are specialized in interacting ...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/j.jdermsci.2020.02.002
更新日期:2020-03-01 00:00:00
abstract::Hair follicles reconstitute themselves though the hair cycle, suggesting the presence of intrinsic stem cells. In contrast to the previous belief that stem cells reside in the bulbar region of hair follicles, stem cells were detected in the bulge area, a contiguous part of outer root sheath, that provides the insertio...
journal_title:Journal of dermatological science
pub_type: 杂志文章,评审
doi:10.1016/j.jdermsci.2006.12.002
更新日期:2007-05-01 00:00:00
abstract::A simple method is described for the procurement of human blood eosinophil phenotypes by combining an anti-CD16 monoclonal antibody, immunobeads, and a non-toxic and non-ionic density gradient medium, Nycodenz. The purification depends on the removal of mononuclear cells using a 1.076/1.102 g/ml Nycodenz density gradi...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/0923-1811(95)00394-8
更新日期:1995-09-01 00:00:00
abstract::Quinolone antibacterial agents, known to elicit photosensitive dermatitis as an adverse effect, have both phototoxicity and photoallergenicity. The latter potency is mainly derived from their photohaptenic moiety; quinolones covalently bind to protein and cells upon exposure to ultraviolet A (UVA) light. Our previous ...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/s0923-1811(99)00011-0
更新日期:1999-09-01 00:00:00
abstract::Systemic sclerosis (SSc) is a connective tissue disease with unknown etiology characterized by excessive deposition of collagen in the skin as well as various internal organs. One of the characteristic histological features is the presence of infiltrating mononuclear cells in the dermis in its early stage. As well as ...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/s0923-1811(00)00169-9
更新日期:2001-06-01 00:00:00
abstract::A cell line, designated ISOS-1, was established from a tumor formed by transplantation of a human angiosarcoma into mice with severe combined immunodeficiency (SCID). The cells showed endothelial properties, based on the uptake of Dil-Ac-LDL and binding of UEA-I/GSA-I lectins, but were negative for CD11b and Pan Cytok...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/s0923-1811(97)00032-7
更新日期:1998-01-01 00:00:00
abstract::Propionibacterium acnes (P. acnes) causes an inflammatory acne that is characterized by massive neutrophilic infiltration. IL-8 is thought to play an important role in the pathophysiology of P. acnes, although the mechanisms by which P. acnes up-regulates the release of IL-8, a neutrophilic chemokine, from target cell...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/s0923-1811(02)00013-0
更新日期:2002-08-01 00:00:00
abstract:BACKGROUND:Tyrosinase, the rate-limiting enzyme required for melanin production, has been targeted to develop active brightening/lightening materials for skin products. Unexpected depigmentation of the skin characterized with the diverse symptoms was reported in some subjects who used a tyrosinase-competitive inhibitin...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/j.jdermsci.2014.07.001
更新日期:2014-10-01 00:00:00
abstract:BACKGROUND:While immunologic events elicited by acute barrier disruption or UVB irradiation have been studied in detail, the biological sequel of multiple insults to the skin is not well understood. OBJECTIVE:Since the skin would receive a variety of simultaneous stimuli in daily life, we tested the effects of sequent...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/s0923-1811(03)00177-4
更新日期:2003-12-01 00:00:00
abstract:BACKGROUND:The tetracycline (Tet) responsive system is a valuable tool that is routinely used in a wide variety of mammalian cells for regulatable expression of gene products. However, technical difficulties such as harsh selection conditions and extensive screening processes to identify suitably responsive clones limi...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/j.jdermsci.2007.09.003
更新日期:2008-01-01 00:00:00
abstract::Stem cells are fascinating because of their potential in regenerative medicine. Stem cell homeostasis has been thought to be mainly regulated by signals from their adjacent micro-environment named the "stem cell niche". However, recent studies reveal that there can be multiple layers of environmental controls. Here we...
journal_title:Journal of dermatological science
pub_type: 杂志文章,评审
doi:10.1016/j.jdermsci.2012.02.007
更新日期:2012-04-01 00:00:00
abstract:BACKGROUND:Carbonylated proteins (CPs) are generated by the reaction of basic amino acid residues in proteins with aldehyde compounds produced during lipid peroxidation. CPs in the stratum corneum (SC) impact skin conditions such as skin moisture functions including water content and transepidermal water loss (TEWL). I...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/j.jdermsci.2016.09.016
更新日期:2016-12-01 00:00:00
abstract::Hamster flank organs are useful for studying androgen-dependent growth of hair follicles and sebaceous glands. A cDNA clone (FAR-17a) was isolated from the hamster flank organ, whose expression was highly sensitive to androgen. The mRNA level of this gene was reduced after castration but reappeared after testosterone ...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/s0923-1811(97)00597-5
更新日期:1997-05-01 00:00:00
abstract:BACKGROUND AND OBJECTIVE:Staphylococcus epidermidis is an autologous bacterium that is beneficial to skin health. Our goal was to develop a novel, personalized basic cosmetic that exploits this characteristic. METHODS:We conducted a double-blinded, randomized clinical trial on augmentation with S. epidermidis as a pil...
journal_title:Journal of dermatological science
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/j.jdermsci.2015.05.001
更新日期:2015-08-01 00:00:00
abstract:BACKGROUND:Several inhibitor of apoptosis proteins (IAPs) are cleaved during apoptosis. Studies of the melanoma-associated IAP (ML-IAP) Livin, using recombinant molecules, have implicated both caspases 3/7 and the serine protease Omi/HtrA2 in its proteolytic cleavage. OBJECTIVE:To characterize the apoptotic cleavage o...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/j.jdermsci.2006.05.007
更新日期:2006-09-01 00:00:00
abstract:BACKGROUND:Psoriasis is a chronic inflammatory disease characterized by demarcated, raised, and scaling skin lesions. It often serves as a model for immune-mediated disorders. Gene expression profiling of affected skin has allowed insights into psoriasis pathogenesis. However, the mechanisms leading to specific mRNA ex...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/j.jdermsci.2019.11.003
更新日期:2020-01-01 00:00:00
abstract::We have previously reported that two species of pro alpha 1(IV) collagen chains, disulfided (500 kDa) and non-disulfided (180 kDa), were produced by B16 melanoma cells (J Biochem (1994) 116; 1039-1043). The mechanism by which the non-disulfided pro alpha 1(IV) chain is produced was studied. No significant difference i...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/0923-1811(95)00486-6
更新日期:1996-10-01 00:00:00
abstract::Epithelial-mesenchymal transition (EMT) plays important roles not only in the morphogenesis but also in wound repair, tissue fibrosis and cancer progression. Recently, regulatory mechanism of this process has been elaborately elucidated. EMT can be a new therapeutic target for treating skin ulcer, fibrosing alopecia, ...
journal_title:Journal of dermatological science
pub_type: 杂志文章,评审
doi:10.1016/j.jdermsci.2010.11.015
更新日期:2011-01-01 00:00:00
abstract:BACKGROUND:Zinc deficiency is believed to be a predisposing factor for the development and intractable healing of pressure ulcers (PUs); however, the mechanisms of this association have not been elucidated. OBJECTIVE:Objective was to elucidate the mechanisms of the formation of severe and prolonged PUs under the zinc ...
journal_title:Journal of dermatological science
pub_type: 杂志文章
doi:10.1016/j.jdermsci.2019.07.004
更新日期:2019-08-01 00:00:00