Evaluation of the UVB‐screening capacity and restorative effects exerted by farnesol gel on UVB‐caused sunburn

Farnesol, a natural 15‐carbon organic compound, has various microbiological and cellular activities. It has been found to exert apoptosis‐inducing effects against carcinoma cells as well as antiallergic and anti‐inflammatory effects in vivo. In the current study, a series of formulations composed of various concentrations of hydroxypropyl methylcellulose (HPMC) with the addition of hyaluronan (HA) and xanthan gum (XG) was designed to evaluate the UVB‐screening and H₂O₂‐eliminating effects of farnesol in normal fibroblasts. Farnesol at 0.005, 0.0075, and 0.01% exhibited significant capacity for H₂O₂ scavenging; at 0.0025%, it showed insignificant effects. Under 120‐min UVB exposure, screening with plural gel composed of 0.0025% farnesol, 0.5% HA, and 0.5% XG containing 1.5% or 2% HPMC retained normal fibroblast viability. After 60‐min exposure to UVB, screening with plural gel composed of farnesol, HA, XG, and 0.5%, 1.0%, 1.5%, or 2% HPMC decreased the ratio of the G1 phase and increased ratio of the S phase in comparison with the accumulated cell cycle of the normal fibroblasts without screening. The gel with 2% HPMC displayed the strongest cell cycle‐reversal ability. In vivo histopathological results showed that the prepared plural gels with 0.5% or 2% HPMC and farnesol, HA, and XG had greater antiphotoaging and reparative effects against UVB‐induced changes and damage in the skin. In conclusion, the current in vitro and in vivo results demonstrated that the prepared plural composed of 0.0025% farnesol, 0.5% HA, 0.5% XG, and 2% HPMC possessed the greatest UVB‐screening capacity and the strongest restorative effects on UVB‐induced sunburned skin.     

密度感应分子对白色念珠菌生物被膜形成作用的研究

目的:白色念珠菌生物被膜形成受密度感应分子调控,法尼醇和酪醇是白色念珠菌产生的两种密度感应分子?本研究探讨不同生物被膜时相,密度感应分子对白色念珠菌形态及生物被膜形成的作用?方法:体外构建白色念珠菌生物被膜?研究分为法尼醇处理组?酪醇处理组?法尼醇和酪醇联合处理组?对照组?首先采用XTT检测不同生物被膜时相酪醇和法尼醇对白色念珠菌细胞活力的作用?扫描电子显微镜(scanning electron microscopy,SEM)观察酪醇和法尼醇对白色念珠菌生物被膜的作用?同时采用气相色谱-质谱联用(gas chromatography-mass spectrometry,GC/MS)检测白色念珠菌生物被膜法尼醇的产生,高效液相色谱(high press liquid chromograph,HPLC)检测白色念珠菌生物被膜酪醇的产生?结果:XTT结果显示,与对照组比较,酪醇可促进6 h白色念珠菌生物膜活力(P < 0.05),法尼醇抑制早期(3 h和6 h)生物被膜活力(P < 0.05),联合作用组抑制6 h生物被膜活力(P < 0.001)?扫描电镜观察发现,酪醇促进3 h和6 h白色念珠菌细胞的出芽,法尼醇抑制3 h和6 h菌丝形成,两者联合作用以后者对菌丝形成的抑制作用为主?GC/MS及 HPLC结果表明在早期(3 h和6 h)生物被膜,2种密度感应分子产生少且无明显升高趋势(P > 0.05);随着生物被膜成熟(24 h及36 h),酪醇产生明显增多(P < 0.05),法尼醇产生也明显增多(P < 0.05)?24 h生物被膜产生酪醇最多,36 h 生物被膜产生法尼醇最多?结论:酪醇可以促进白色念珠菌出芽和菌丝伸长,促进早期生物被膜形成?法尼醇抑制出芽和菌丝形成,抑制早期生物被膜形成?两者联合作用以法尼醇对菌丝形成的抑制作用为主?     

Patch testing with a new fragrance mix - reactivity to the individual constituents and chemical detection in relevant cosmetic products

A new fragrance mix (FM II), with 6 frequently used chemicals not present in the currently used fragrance mix (FM I), was evaluated in 6 dermatological centres in Europe, as previously reported. In this publication, test results with the individual constituents and after repeated open application test (ROAT) of FM II are described. Furthermore, cosmetic products which had caused a contact dermatitis in patients were analysed for the presence of the individual constituents. In 1701 patients, the individual constituents of the medium (14%) and the highest (28%) concentration of FM II were simultaneously applied with the new mix at 3 concentrations (break‐down testing for the lowest concentration of FM II (2.8%) was performed only if the mix was positive). ROAT was performed with the concentration of the FM II which had produced a positive or doubtful (+ or ?+) patch test reaction. Patients' products were analysed for the 6 target compounds by gas chromatography‐mass spectrometry (GC‐MS). Results: 50 patients (2.9%) showed a positive reaction to 14% FM II and 70 patients (4.1%) to 28% FM II. 24/50 (48%) produced a positive reaction to 1 or more of the individual constituents of 14% FM II and 38/70 (54.3%) to 28% FM II, respectively. If doubtful reactions to individual constituents are included, the break‐down testing was positive in 74% and 70%, respectively. Patients with a positive reaction to 14% FM II showed a higher rate of reactions to the individual constituent of the 28% FM II: 36/50 (72%). Positive reactions to individual constituents in patients negative to FM II were exceedingly rare. If doubtful reactions are regarded as negative, the sensitivity, specificity, positive predictive value and negative predictive value for the medium concentration of FM II towards at least 1 individual constituent was 92.3% (exact 95% confidence interval 74.9–99.1%), 98.4% (97.7–99.0%), 48% (33.7–62.6%) and 99.9% (99.6–"100.0%), respectively. For the high concentration, the figures were very similar. The frequency of positive reactions to the individual constituents in descending order was the same for both FM II concentrations: hydroxyisohexyl 3‐cyclohexene carboxaldehyde (Lyral^®) > citral > farnesol > citronellol > α‐hexyl‐cinnamic aldehyde (AHCA). No unequivocally positive reaction to coumarin was observed. Lyral^® was the dominant individual constituent, with positive reactions in 36% of patients reacting to 14% FM II and 37.1% to 28% FM II. 5/11 patients developed a positive ROAT after a median of 7 days (range 2–10). The 5 patients with a doubtful or negative reaction to 28% FM II were all ROAT negative except 1. There were 7 patients with a certain fragrance history and a positive reaction to either 28% or 14% FM II but a negative reaction to FM I. Analysis with GC‐MS in a total of 24 products obtained from 12 patients showed at least 1–5 individual constituents per product: Lyral^® (79.2%), citronellol (87.5%), AHCA (58.3%), citral (50%) and coumarin (50%). The patients were patch test positive to Lyral^®, citral and AHCA. In conclusion, patients with a certain fragrance history and a negative reaction to FM I can be identified by FM II. Testing with individual constituents is positive in about 50% of cases reacting to either 14% or 28% FM II.     

Miconazole,a pharmacological barrier to skin fungal infections

Introduction: Miconazole (MCZ) is a time-honored antifungal of the imidazole class. MCZ exerts a multipronged effect on fungi. It inhibits the cytochrome P450 complex, including the 14α-demethylase enzyme required for ergosterol biosynthesis, in fungal cell membranes. In addition, intracellular accumulation of toxic methylated sterols occurs and the synthesis of triglycerides and phospholipids is altered. Disturbances in oxidative and peroxidative enzyme activities lead to an intracellular toxic concentration of hydrogen peroxide. As a result, intracellular organelle destruction then leads to cell necrosis. Farnesol synthesis stimulated in Candida spp. prevents the yeast-to-mycelium formation. MCZ is further active against Gram-positive bacteria.

Areas covered: This review aims at revisiting the MCZ antifungal activity in dermatomycoses.

Expert opinion: MCZ's wide spectrum of activity appears noteworthy. The full pharmacological profile of MCZ indicates its fungistatic profile through its effect on ergosterol biosynthesis. In addition, it exhibits a fungicidal effect against a number of fungal species, due to hydrogen peroxide accumulation. MCZ is characterized by high safety, efficacy and versatility, and a unique, multifaceted nature of activity in the treatment of dermatomycoses.     

Evaluation of tyrosol and farnesol as inducer in pigment production by Monascus purpureus ATCC16365

This study focused on investigating the effect of exogenously applied two quorum sensing molecules (tyrosol and farnesol) on the synthesis of bioactive metabolites (pigments, lactic acid, ethanol, and citric acid) in Monascus purpureus ATCC16365. None of the tested concentrations (62.5, 125, 250, and 500 µl/L) of farnesol affected the synthesis of metabolites as well as cell growth. As with farnesol application, none of the tested concentrations (3.45, 6.9, 13.8, and 27.6 mg/L) of tyrosol caused a significant change in the synthesis of lactic acid and citric acid as well as cell growth. Conversely, all of the tested concentrations of tyrosol increased pigment synthesis but reduced ethanol synthesis, compared with the control. Maximum increases (3.16-, 2.68-, and 2.87-fold increase, respectively) in yellow, orange, and red pigment production were achieved, especially when 6.9-mg/L tyrosol was added to the culture on day 3. On the contrary, 6.9-mg/L tyrosol reduced the content of citrinin by approximately 51.5%. This is the first report on the effect of tyrosol and farnesol on the synthesis of Monascus metabolites. Due to potential properties, such as low price, nonhuman toxicity, promotion of pigment synthesis, and reduction in citrinin synthesis, tyrosol can be used as a novel inducer in the fermentative production of Monascus pigments.     

胆汁酸代谢与2型糖尿病的研究进展

胆汁酸（bile acids, BA）在肝脏中合成,是胆固醇的代谢产物。进食时,BA随胆汁进入肠道,其中95%的胆盐可被肠道（主要在回肠）重吸收入肝,以保持胆盐池的稳定。BA作为一种代谢调节因子,能够激活多种核受体和膜受体介导的信号通路,参与多种代谢调节过程,不仅可以促进食物中脂类的消化吸收,还参与糖脂及能量的代谢,同时BA谱又是代谢稳态的关键调节剂。BA代谢和信号转导的改变与肥胖和2型糖尿病（type 2 diabetes mellitus, T2DM）相关。BA螯合剂治疗的T2DM患者或进行减肥手术的病态肥胖患者,其血糖水平的显著改善均与BA谱和信号转导的变化有关。本文就BA的代谢调节通路与T2DM相关性进行综述。     

法呢醇对长角血蜱若虫蜕皮及存活的影响

在长角血蜱若虫饱血后不同的发育阶段点滴不同剂量的法呢醇，发现在饱血当天、１０天，２０μｇ／蜱的剂量明显地延长了若虫的蜕皮前期；饱血后５、１２天，则无此效应。在这三个时期，大剂量（如２０，５０μｇ／蜱）均能引起较高的死亡率（蜕皮前死亡）。推测长角血蜱若虫有内源的、结构类似昆虫保幼激素的物质参与其蜕皮的激素调控。