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文献分享系列(一)

广东省化妆品学会 2018-12-05 14:35:42



01

Skin whitening agents: medicinal chemistry perspective of tyrosinase inhibitors

从药理化学角度分析皮肤美白成分酪氨酸酶抑制因子的机理研究


ABSTRACT

Melanogenesis is a process to synthesize melanin, which is a primary responsible for the pigmentation of human skin, eye and hair. Although numerous enzymatic catalyzed and chemical reactions are involved in melanogenesis process, the enzymes such as tyrosinase and tyrosinase-related protein-1 (TRP-1) and TRP-2 played a major role in melanin synthesis. Specifically, tyrosinase is a key enzyme, which catalyzes a rate- limiting step of the melanin synthesis, and the downregulation of tyrosinase is the most prominent approach for the development of melanogenesis inhibitors. Therefore, numerous inhibitors that target tyrosinase have been developed in recent years. The review focuses on the recent discovery of tyrosinase inhibitors that are directly involved in the inhibition of tyrosinase catalytic activity and functionality from all sources, including laboratory synthetic methods, natural products, virtual screening and structure-based molecular docking studies.

摘要:黑色素原的生成是一个黑色素合成的过程,其主要负责人体皮肤、眼睛、头发的色素生成。虽然黑素原生成过程中涉及大量的酶和化学反应物,但是像酪氨酸酶和酪氨酸蛋白酶1(TRP-1)和酪氨酸蛋白酶2(TRP-2)在黑色素形成中扮演主要的角色。特别是,酪氨酸酶作为黑色素合成中的限速酶,是一种关键酶。降低酪氨酸酶是抑制黑素原生成的重要手段。因此,近些年有大量的用于抑制酪氨酸酶的抑制因子被发现。这篇文章主要通过实验室方法、天然产物、虚拟筛选以及基于分子结构的研究等方式,探讨酪氨酸抑制剂在酪氨酸酶酶促反应及功能性。


02

Overview of skin whitening agents with an insight into the illegal cosmetic market in Europe

洞察欧洲不合法化妆品市场中美白成分的概述


ABSTRACT

Lightening skin tone is an ancient and well-documented practice, and remains common practice among many cultures. Whitening agents such as corticosteroids, tretinoin and hydroquinone are medically applied to effectively lighten the skin tone of hyperpigmented lesions. However, when these agents are used cosmetically, they are associated with a variety of side-effect. Alternative agents, such as arbutin and its derivatives kojic acid and nicotinamide have been subsequently developed for cosmetic purposes. Unfortunately, some cosmetics contain whitening agents that are banned for use in cosmetic products. This article provides an overview of the mode of action and potential side-effects of cosmetic legal and illegal whitening agents, and the pattern of use of these types of products. Finally, an EU analysis of the health prob- lems due to the presence of illegal products on the market is summarized.

摘要美白皮肤历来被大量历史文献记载,并且在不同的文化中都非常盛行。美白成份如皮质甾类、维生素A、氢醌能有效的应用于美白肌肤。但是,当这类的成分用于化妆品中,他们也伴随着各种副作用。各种成分如熊果苷和其派生物曲酸和烟酰酸也陆续被用于化妆品中。不幸的是某些含有美白成分的化妆品含中有违禁物。本文主要讨论美白作用机理、化妆品中具有潜在副作用的合法和不合法美白成分及这类成分的使用情况。最后的总结是关于欧盟对市场中不合法化妆品对人体健康影响的分析报告。


03

Hexamidine salts – applications in skin health and personal care products

己脒定盐类在皮肤健康和个人护理品中的应用


ABSTRACT

Hexamidine (HEX) has been used as a preservative in topical prepa- rations since the 1950s. A number of studies also indicate that the molecule plays a beneficial role in skin homoeostasis. In this review, we describe the physicochemical properties of hexamidine diisethionate (HEX D) and the corresponding hydrochloride salt (HEX H). The biocidal and protease inhibition properties of HEX are outlined as well as the effects of HEX on lipid processing enzymes, corneocyte maturity, stratum corneum thickness and transepider- mal water loss (TEWL). Skin permeation properties of HEX D and HEX H are summarized, and formulation approaches for effective dermal targeting of HEX are discussed.

摘要:己脒定从1950开始就一直当防腐剂使用。许多研究表明己脒定在皮肤平衡方面也有重要的作用。这篇文章主要讨论己脒定二盐 (HEX D)和己脒定二盐酸盐(HEX H)的物理化学性质。己脒定抑制微生物和蛋白酶方面特性以及对油脂加工酶、角质细胞成熟度、角质层厚度、经皮失水值(TEWL)的作用效果 。总而言之:HEX系列对真皮的渗透吸收和皮肤的屏障功能有作用。

文中主要从:HEX D和HEX H的物理化学特性分析两者的区别;己脒定作为抗微生物制剂的应用;酶抑制剂; 与皮肤的生理学信息;


04

Polar extracts from the berry-like fruits of Hypericum androsaemum L. as a promising ingredient in skin care formulations

金丝桃属植物的果实中提取极性溶剂提取物用于皮肤护理产品


ABSTRACT

Ethnopharmacological relevance: The top flowering aerial parts of the Hypericum species are traditionally used to prepare ointments to heal cuts and burns. Sometimes even the fruits are used for these purposes. Hypericum androsaemum L., commonly known as tutsan or shrubby St. John's Wort, is a Mediterranean medicinal plant which has been traditionally used to prepare an ointment for treating cuts and wounds.

Aim of the study: To evaluate the extracts obtained from H. androsaemum red berries as functional ingredients for skin care formulations.Materials and methods: The methanolic extract was obtained by Soxhlet extraction while the aqueous extract was prepared by decoction; their composition was determined by HPLC analysis. Their biological activities were measured in terms of proliferation and migration of human fibroblasts, inhibition of collagenase activity, and immunomodulatory effects on human peripheral blood mononuclear cells (PBMCs). In addition, we evaluated their photostability by UV spectroscopy and their protective effects against APPH-induced hemolysis in red blood cells (RBC).

Results: The polar extracts contained significant amounts of shikimic (108,143.7–115,901.3 mg/kg) and chlorogenic acids (45,781.1–57,002.7 mg/kg). The main components of these extracts made an important contribution to a significant increase in human fibroblast migration. Both extracts were also active as collagenase inhibitors, with the aqueous one showing a greater inhibitory capacity (IC50 value of 88.1 μg/ mL), similar to that of chlorogenic acid. The kinetic parameters determined for the enzymatic reaction revealed for both aqueous extract and chlorogenic acid an uncompetitive mechanism of inhibition. The methanolic extract showed important effects on PBMCs by modulating IL-6. Both extracts proved to be photostable in the UVA/B range and protected RBC against peroxidation at low concentrations.

Conclusions: H. androsaemum red berries were proven to contain phytochemicals that improve skin regeneration, hence potentially employable in skin care formulations.

相关信息:金丝桃属的花蕊和果实可用于制作治愈刀伤烧伤的软膏。

实验材料和方法:用索式提取法得到甲醇提取物和水浸提法得到水溶性提取物,通过HPLC分析各组成成分。通过组织扩散和人体成纤维细胞合成、胶原酶活性抑制功能、对人体血红单核细胞的免疫调节等方面的测试了解其生物活性。另外,也通过UV测试评估其耐光性和对降低红细胞中血红素溶解的作用。

结果:甲醇提取物包含重要的莽草酸(108.1-115.9g/kg)和绿原酸(45.781-57.0g/kg)。这些提取物的成份对人体成纤维细胞的增加有重要的作用,而且这两类提取物具有胶原酶抑制作用的功能。水提取物具有更好的抑制能力(IC5088.1μg /ml),类似于绿原酸。其酶反应动力学参数表明水溶性提取物和绿原酸是非竞争性抑制机制。甲醇提取物通过调节IL-6,对人体外周血单核细胞有重要影响。实验证明这两种提取物都具有一定的UVA/UVB耐光性,并且在低浓度下能防止氧化,保护红细胞。

结论:金丝桃属含有植物素能帮助皮肤再生,具有应用于皮肤护理产品的潜力。


05

Introduction to skin aging

皮肤老化的介绍


ABSTRACT 

Cutaneous science has seen considerable development in the last 25 years, in part due to the Omics revolution, and the appreciation that this organ is hardwired into the body’s key neuro-immuno-endocrine axes. Moreover, there is greater appreciation of how stratification of skin disorders will permit more targeted and more effective treatments. Against this has been how the remarkable extension in the average human life-span, though in the West at least, this parallels worrying increases in lifestyle-associated conditions like diabetes, skin cancer etc. These demographic trends bring greater urgency to finding clinical solutions for numerous age-related deficits in skin function caused by extrinsic and intrinsic factors. Mechanisms for aging skin include the actions of reactive oxygen species (ROS), mtDNA mutations, and telomere shortening, as well as hormonal changes.

We have also significantly improved our understanding of how to harness the skin’s considerable regenerative capacity e.g., via its remarkable investment of stem cell subpopulations. In this way we hope to develop new strategies to selectively target the skin’s capacity to undergo optimal wound repair and regeneration. Here, the unsung hero of the skin regenerative power may be the humble hair follicle, replete with its compliment of epithelial, mesenchymal, neural and other stem cells. This review introduces the topic of human skin aging, with a focus on how maintenance of function in this complex multi-cell type organ is key for retaining quality of life into old age.

摘要:由于组织时代的兴起,皮肤科学的发展已经有近25年的历史,人体器官的发展与人体关键的神经-免疫-内分泌系统息息相关。而且,皮肤紊乱需要更具针对性更有效的治疗方式。至少在西方国家,如何提升人的平均寿命和解决糖尿病、皮肤癌等一样重要。大量统计数据显示,对内外因素导致的与老化相关方面的皮肤功能缺陷,急需找到关键的解决办法。皮肤老化的机理包括:活性氧活跃度、mtDNA(线粒体脱氧核糖核酸) 突变、端粒变短、荷尔蒙变化等有关。

我们对如何利用皮肤的再生能力的理解有了显著性提高,比如皮肤干细胞的发现。通过皮肤干细胞的应用,能够做到有选择性的修复皮肤损伤和皮肤再生。皮肤的再生能力可能与上皮组织中布满毛囊、间质干细胞、神经细胞和其他干细胞有关。这个综述主要是讨论人体皮肤老化,研究人体衰老过程中复杂的多细胞形器官如何保持其功能特性。


06

3-(3,4,5-Trimethoxybenzylidene)-2,4-pentanedione: Design of a novel photostabilizer with in vivo SPF boosting properties and its use in developing broad-spectrum sunscreen formulations

3-3,4,5-三甲氧基苯亚基)-2,4-戊二酮—一款用于提升防晒性能的新型光稳定性原料及在广谱防晒配方中的应用


OBJECTIVE: The study concerned the synthesis of a novel photo- stabilizer based on benzylidenepentanedione chemistry and the evaluation of its potential in developing a broad-spectrum sun- screen formulation containing avobenzone.

METHODS: 3-(3,4,5-Trimethoxybenzylidene)-2-4-pentanedione (TMBP) was synthesized through a condensation reaction and incorporated into a sunscreen formulation containing, inter alia, avobenzone. The SPF, critical wavelength and in vitro photostability of the product were measured. The photostability was compared with that afforded by current avobenzone photostabilizers, namely octocrylene, ethylhexylmethoxycrylene and diethylhexylsyringylidenemalonate. The photostability of TMBP either alone or in the presence of avobenzone in a methanolic solution was also evaluated by UV spectrophotometric and HPLC analyses. The optical prop- erties of TMBP were estimated experimentally and supported by time- dependent density functional theory (TD-DFT) calculations.

RESULTS: The ability of TMBP to stabilize avobenzone under ultravi- olet (UV) light exposure was shown both in formulated products and in solution. A comparative stability study incorporating various com- binations of avobenzone, TMBP (vs. three commercial photostabiliz- ers) and UVB sunscreens clearly showed TMBP to be a very effective stabilizer. The photostabilizing effect of TMBP arises from triplet-state energy transfer from avobenzone to TMBP and through light-induced reactions that preserve the main chromophores. Interestingly, a 50% in vivo SPF boosting was observed when TMBP was used with organic and inorganic sunscreens when alone it has no contribution to SPF. TMBP-containing sunscreen formulations clearly showed a critical wavelength of well over 370 nm and can thus be categorized as broad-spectrum sunscreens.

CONCLUSION: We were able to design a very effective photostabi- lizer, trimethoxybenzylidene pentanedione (INCI name), based on benzylidenepentanedione chemistry. TMBP is very efficient in stabiliz- ing avobenzone in formulated products and boosts in vivo SPF by >50% for organic and inorganic sunscreens, and the formulations have critical wavelengths of> 370 nm. These efficacious properties make it a promising additive for inclusion in broad-spectrum photo- protective products.

目的:基于苯亚基戊二酮的一款新型光稳定性的合成及评估在含有阿伏苯宗的防晒产品配方中的潜力。

方法: 3-(3,4,5-三甲氧基苯亚基)-2,4-戊二酮(TMBP)是通过合成方法而得到,可在防晒产品中与阿伏苯宗复配。与阿伏苯宗等对比,通过测定波长和体外光稳定性,UV和HPLC分析,TMBP的光学特性,含时密度泛函理论计算其稳定性。

结果:在UV光照射下,TMBP的稳定性在配方产品及溶液中都能表现出来。一个阿伏苯宗和TMBP的稳定性实验表明,TMBP具有更好的UVB防晒功能。有趣的是:在单独使用有机或是无机防晒产品时可能没有作用,但是加入TMBP可以提升50%的防晒效果。并且TMBP能够在大于370nm下有很好的防晒作用,能够作为广谱防晒产品有效添加成分。


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