[Contamination Characteristics and Source Apportionment of Potentially Toxic Elements in Soil around the Coal-fired Power Plant Using APCS-MLR and PMF Models].

To investigate the characteristics and sources of potentially toxic elemental contamination in soils around the coal-fired power plant, we selected the soil around the Jingyuan power plant as the object of investigation. Thirty-six and 27 soil samples collected from the urban and farmland areas were analyzed for PTEs (As, Cd, Cr, Cu, Hg, Ni, Pb, and Zn), respectively. We employed the geoaccumulation index, single-factor pollution index, and improved Nemerow integrated pollution index to evaluate the contamination characteristics of PTEs, and combined correlation analysis with absolute principal component scores-multiple linear regression (APCS-MLR) and positive matrix factorization (PMF) receptor models were used to quantitatively analyze the pollution sources of PTEs. The results revealed that all the average concentrations of other soil metals around Jingyuan power plant exceeded their corresponding background values of Gansu Province, except for As, in agricultural soil, and Hg exhibited significant spatial non-homogeneity, and thus it was visibly affected by anthropogenic activities. The values of the single-factor pollution and geoaccumulation indices indicated that the soils of both sites were mainly contaminated with Cd, Cr, Ni, and Pb, and Hg contamination was reflected in wide areas for both sites. Additionally, the results of the improved Nemerow index demonstrated that the investigated soil was between moderately contaminated and heavily contaminated. Further, the comprehensive pollution degree of urban soil was higher than that of agricultural soil. Moreover, source apportionment revealed that PTEs in urban soil were derived from mixed sources of traffic activities and coal combustion, mixed sources of traffic activities and industrial and mining activities, and atmospheric deposition from industrial activities, with contribution rates of APCS-MLR of 35.2%, 25.1%, and 23.4%, respectively. The PMF contribution rates were 40.2%, 12.4%, and 47.7%, respectively. PTEs in agricultural soil were from one mixture source of industrial, mining, agricultural, and traffic sources, and the other mixed source was of traffic activities and coal combustion, with a APCS-MLR contribution rate of 40.3% and 35.9% and a contribution rate of PMF of 36.2% and 18.0%, respectively. In addition, another mixed source of agricultural activities and coal combustion was obtained using the PMF model, with a contribution rate of 48.5%.

[Spatial Distribution Characteristics and Source Analysis of Heavy Metals in Urban River Surface Sediments from the Lanzhou Reach of the Yellow River].

In order to investigate the contamination characteristics and potential sources of heavy metals from the urban river surface sediments in the Yellow River Basin, we selected the Lanzhou reach of the Yellow River as the object of investigation. A total of 46 surface sediment samples were collected along the Lanzhou reach of the Yellow River, and the contents of eight heavy metals, Cr, Ni, Cu, Zn, As, Cd, Hg, and Pb, were determined by using inductively coupled plasma mass spectrometry and an atomic fluorescence spectrometer. Contamination indexes including single factor pollution index (Pi) and geo-accumulation index (Igeo), together with the sediment pollution index (SPI), were used to assess heavy metal pollution characteristics and ecological risk levels in the urban river surface sediments of the Lanzhou reach of the Yellow River. Pearson's correlation analysis (CA), positive matrix factorization (PMF), and principal component analysis/absolute principal component score (PCA/APCS) were jointly employed to quantitatively analyze pollution sources of heavy metals. The results showed that the mean concentrations of the majority of heavy metals exceeded their corresponding background values of Gansu Province and Lanzhou City with the exception of As, and the spatial distribution of high concentrations of heavy metals was mainly concentrated in the corner of the river. Based on the single factor pollution and geo-accumulation indexes of the eight heavy metals, in the Lanzhou reach of the Yellow River, Cr was the dominant pollution element in the urban river surface sediments, followed by Cd and Ni. Additionally, the SPI values for the eight heavy metals in the surface sediments ranged from 0.48 to 8.56, presenting natural to low ecological risk level. Furthermore, source apportionment revealed that a mixture source of industrial and agricultural activities (77.6%) was the largest contributor of Cr, Ni, Zn, As, Cd, and Pb in the urban river surface sediments, followed by natural sources (11.4%) and a mixed source of industrial and traffic activities (11%).

[Evaluation on application of 3D printing digital positioning guide in root canal retreatment].

PURPOSE: To explore the application of 3D printing digital positioning guide in root canal retreatment. METHODS: Eighty-two isolated teeth collected in Chifeng College Affiliated Hospital from January 2018 to December 2021 were selected, and divided into experimental group and control group by random number table method, with 41 teeth in each group. Both groups were given root canal retreatment. The control group underwent traditional pulpotomy, while the experimental group underwent precise pulpotomy under 3D printing digital positioning guide. The damage of the coronal prosthesis caused by pulpotomy was compared between the two groups, the time of pulpotomy was recorded, removal of root canal fillings in the two groups was counted, fracture resistance of the tooth tissue in the two groups was compared, and the incidence of complications in the two groups was recorded. SPSS 18.0 software package was used for statistical analysis of the data. RESULTS: The ratio of pulp opening area to total dental and maxillofacial area in the experimental group was significantly lower than that in the control group (P＜0.05). The pulp opening time in the experimental group was lower than that in the control group(P＜0.05), and the root canal preparation time in the experimental group was significantly higher than that in the control group(P＜0.05). There was no significant difference in the total time between pulp opening and root canal preparation between the two groups(P＞0.05). The removal rate of root canal filling in the experimental group was higher than that in the control group (P＜0.05). The failure load value of the experimental group was significantly higher than that of the control group (P＜0.05). There was no significant difference in the incidence of total complications between the two groups (P＞0.05). CONCLUSIONS: Application of 3D-printed digital positioning guides in root canal retreatment can achieve precise and minimally invasive pulp opening, reduce damage to coronal restorations, preserve more dental tissue, and improve the removal efficiency of root canal fillings and the fracture resistance of dental tissue, as well as performance, safety and reliability.

Conceptual radar trap model realized via polarization conversion metasurface.

General metasurfaces (MSs) can realize low observability of radar by manipulating the polarization mode and transmission direction of the electromagnetic (EM) waves. Here, we propose the radar trap model to realize EM wave imprisonment. This three-layer model is composed of the transmission polarization converter, the connected dielectric substrate and the reflection polarization converter. Using Jones calculation as a guide, we optimized the geometric parameters of the upper and lower layers to realize specific polarization conversion functions. The middle layer is regarded as the support and matching layer. On this basis, the combined radar trap model can realize the imprisonment of EM waves between upper and lower layers, which is attributed to the cooperative effect of asymmetric transmission and polarization conversion. We further verified the feasibility and correctness of our investigations through two kinds of model designs based on linear and circular polarization conversion mechanisms. Good agreements are observed between simulation and experiment. Even though the design presents a narrow operating bandwidth, it still provides novel ideas for developing radar stealth technology.

Potential protective effect of hesperidin on hypoxia/reoxygenation-induced hepatocyte injury.

Hesperidin (HDN) has been reported to have hydrogen radical- and hydrogen peroxide-removal activities and to serve an antioxidant role in biological systems. However, whether HDN protects hepatocytes (HCs) against hypoxia/reoxygenation (H/R)-induced injury remains unknown. The present study aimed to explore the role of HDN in H/R-induced injury. HCs were isolated and cultured under H/R conditions with or without HDN treatment. HC damage was markedly induced under H/R, as indicated by cell viability, supernatant lactate dehydrogenase levels and alanine aminotransferase levels; however, HDN treatment significantly reversed HC injury. Oxidative stress markers (malondialdehyde, superoxide dismutase, glutathioneand reactive oxygen species) were increased markedly during H/R in HCs; however, this effect was significantly attenuated after exposure to HDN. Compared with those of the control group, the mRNA expression levels of IL-6 and TNF-α in HCs and the concentrations of IL-6 and TNF-α in the supernatants increased significantly following H/R, and HDN significantly ameliorated these effects. Western blotting demonstrated that microtubule-associated protein 1 light chain 3α (MAP1LC3A, also known as LC3) and Beclin-1 protein expression levels increased, while sequestosome 1 levels decreased during H/R following exposure to HDN. The number of GFP-LC3 puncta in HCs following exposure to HDN was increased compared with that observed in HCs without HDN exposure under the H/R conditions after bafilomycin A1 treatment. In summary, the present study demonstrated that HDN attenuated HC oxidative stress and inflammatory responses while enhancing autophagy during H/R. HDN may have a potential protective effect on HCs during H/R-induced injury.

Disulfide-Reduction-Triggered Spontaneous Photoblinking Cy5 Probe for Nanoscopic Imaging of Mitochondrial Dynamics in Live Cells.

Mitochondria are highly dynamic organelles with interconnected tubule structures that are sensitive to environmental stress and light illumination. Super-resolution optical imaging of mitochondrial dynamics is of significance for understanding such biological events. Direct stochastic optical reconstruction microscopy has the advantages of a high spatial resolution, low phototoxicity in live-cell imaging, and the capacity to incorporate smart fluorescent probes. However, dSTORM imaging in live cells is challenging because of the requirement for an imaging buffer and a low temporal resolution. In this work, we achieved dSTORM imaging of mitochondrial dynamics in live cells with a disulfide-substituted Cy5 probe without using any toxic imaging buffer. Under the illumination of very low laser power, the probe exhibited spontaneous photoblinking triggered by disulfide-bond reduction in mitochondria of live cells. The obtained thiol attacked nearby carbon to form a six-membered ring and the reversible opening/closing of the ring produced spontaneous photoblinking behavior. With this new STORM strategy, we achieved observation of mitochondrial dynamics for more than 3 min, which provides a promising tool for further studies of mitochondria with an ultrafine structure.

IL-17 is a potential biomarker for predicting the severity and outcomes of pulmonary contusion in trauma patients.

Pulmonary contusion (PC) is very common in blunt chest trauma, and always results in negative pulmonary outcomes, such as pneumonia, acute respiratory distress syndrome (ARDS), respiratory failure or even death. However, there are no effective biomarkers which can be used to predict the outcomes in these patients. The present study aimed to determine the value of interleukin (IL)-17 and IL-22 in predicting the severity and outcomes of PC in trauma patients. All trauma patients admitted to The First Affiliated Hospital of Guangxi Medical University between January 2015 and December 2017, were studied. Patients aged >14 years old with a diagnosis of PC upon their admission to the emergency department were included. Patients with PC were enrolled as the PC group, patients without PC were enrolled as the non-PC group, and healthy individuals were selected as the control group. Clinical information, including sociodemographic parameters, clinical data, biological findings and therapeutic interventions were recorded for all patients who were enrolled. Blood samples were collected and stored according to the established protocols. PC volume was measured by computed tomography and plasma cytokine levels were assayed by ELISA. A total of 151 patients with PC (PC group) and 159 patients without PC (non-PC group) were included in the present study. In addition, 50 healthy individuals were used as the control group. The primary cause of PC was motor vehicle crashes. PC patients had more rib fractures, but similar injury severity scores compared with other patients. More patients received Pleurocan drainage treatment and had pneumonia complications in the PC group compared with the other two groups. PC patients had a high incidence of ARDS and admission to the intensive care unit (ICU). PC patients also experienced longer periods on mechanical ventilation and had longer stays in the ICU and hospital. PC volume was effective in predicting the outcomes of PC patients. IL-22 levels were similar in the PC group and non-PC group. However, IL-17 could be used as a biomarker to predict the severity of PC, and was strongly associated with PC volume. IL-17 was significantly associated with pro-inflammatory complications in PC patients and could be used as a biomarker for predicting in-patient outcomes of patients with PC. In conclusion, IL-17 is a potential biomarker for predicting the severity and outcomes of PC in trauma patients.

Hesperidin ameliorates liver ischemia/reperfusion injury via activation of the Akt pathway.

Hesperidin (HDN) is a bioflavonoid that serves a role as an antioxidant in biological systems. However, although HDN has hydrogen radical­ and hydrogen peroxide­removal activities, the role of HDN in liver ischemia/reperfusion (I/R) injury remains unknown. This study aimed to determine the role of HDN in liver I/R injury. Male C57BL/6J wild­type (WT) mice were subjected to warm partial liver I/R injury. Liver damage was evaluated by measuring serum alanine aminotransferase (ALT) levels, cytokine production, oxidative stress indicators, tissue hematoxylin­eosin staining and cell death. The Akt signaling pathway was examined to elucidate the underlying mechanisms. HDN had no effect on ALT levels and tissue damage in WT mice without liver I/R injury. However, HDN significantly ameliorated liver I/R injury as measured by serum ALT levels and necrotic tissue areas. HDN decreased malondialdehyde content, but increased the levels of superoxide dismutase, catalase, glutathione peroxidase and glutathione. In addition, HDN significantly attenuated the mRNA expression levels of TNF­α, IL­6 and IL­1ß after liver I/R injury. Furthermore, HDN protected the liver against apoptosis in liver I/R injury by increasing the levels of Bcl­2 and decreasing the levels of cleaved­caspase 3. Mechanistically, the levels of phosphorylated Akt were elevated by HDN during liver I/R injury. In addition, HDN could induce Akt activation in hepatocytes in vitro. Most importantly, treatment with the Akt inhibitor LY294002 in WT mice blocked the hepatoprotective effects of HDN in liver I/R injury. In summary, the results of the present study suggested that HDN may protect against liver I/R injury through activating the Akt pathway by ameliorating liver oxidative stress, suppressing inflammation and preventing hepatocyte apoptosis. HDN may be a useful factor for liver injury protection and a potential therapeutic treatment for liver I/R injury in the future.

Image reconstruction with a deep convolutional neural network in high-density super-resolution microscopy.

An accurate and fast reconstruction algorithm is crucial for the improvement of temporal resolution in high-density super-resolution microscopy, particularly in view of the challenges associated with live-cell imaging. In this work, we design a deep network based on a convolutional neural network to take advantage of its enhanced ability in high-density molecule localization, and introduce a residual layer into the network to reduce noise. The proposed scheme also incorporates robustness against variations of both the full width at half maximum (FWHM) and the pixel size. We validate our algorithm on both simulated and experimental data by achieving performance improvement in terms of loss value and image quality, and demonstrate live-cell imaging with temporal resolution of 0.5 seconds by recovering mitochondria dynamics.

STORM imaging of mitochondrial dynamics using a vicinal-dithiol-proteins-targeted probe.

Stochastic optical reconstruction microscopy (STORM) is a promising method for the visualization of ultra-fine mitochondrial structures. However, this approach is limited to monitoring dynamic intracellular events owing to its low temporal resolution. We developed a new strategy to capture mitochondrial dynamics using a compressed sensing STORM algorithm following raw data pre-treatments by a noise-corrected principal component analysis and K-factor image factorization. Using STORM microscopy with a vicinal-dithiol-proteins targeting probe, visualizing mitochondrial dynamics was attainable with spatial and temporal resolutions of 45 nm and 0.8 s, notably, dynamic mitochondrial tubulation retraction of ~746 nm in 1.2 s was monitored. The labeled conjugate was observed as clusters (radii, ~90 nm) distributed on the outer mitochondrial membranes, not yet reported as far as we know. This strategy is promising for the quantitative analysis of intracellular behaviors below the optical diffraction limit.

ICT and AIE Characteristics Two Cyano-Functionalized Probes and Their Photophysical Properties, DFT Calculations, Cytotoxicity, and Cell Imaging Applications.

Two probes, AIE-1 and AIE-2, were synthesized to investigate the effect of substitutional functional group on aggregation (aggregation-caused quenching (ACQ) or aggregation-induced emission (AIE)) and intramolecular charge transfer (ICT) behavior as well as on the cell imaging aspect. The yellow-color non-substituted probe AIE-1 showed weak charge-transfer absorption and an emission band at 377 nm and 432 nm, whereas the yellowish-orange color substituted probe AIE-2 showed a strong charge-transfer absorption and an emission band at 424 nm and 477 nm in THF solvent. The UV-Vis studies of AIE-1 and AIE-2 in THF and THF with different water fractions showed huge absorption changes in AIE-2 with high water fractions due to its strong aggregation behavior, but no such noticeable absorption changes were observed for AIE-1. Interestingly, the fluorescence intensity of AIE-1 at 432 nm gradually decreased with increasing water fractions and became almost non-emissive at 90% water. However, the monomer-type emission of AIE-2 at 477 nm was shifted to 584 nm with a 6-fold increase in fluorescence intensity in THF-H2O (1:9, v/v) solvent mixtures due to the restriction of intramolecular rotation on aggregation in high water fractions. This result indicates that the probe AIE-1 shows ACQ and probe AIE-2 shows AIE behaviors in THF-H2O solvent mixtures. Furthermore, the emission spectra of AIE-1 and AIE-2 were carried out in different solvent and with different concentrations to see the solvent- or concentration-dependent aggregation behavior. Scanning electron microscope (SEM) and dynamic light scattering (DLS) experiments were also conducted to assess the morphology and particle size of two probes before and after aggregation. Both of the probes, AIE-1 and AIE-2, showed less toxicity on HeLa cells and were suitable for cell imaging studies. Density functional theory (DFT) calculation was also carried out to confirm the ICT process from an electron-rich indole moiety to an electron-deficient cyano-phenyl ring of AIE-1 or AIE-2.

Super-resolution imaging of the dynamic cleavage of intercellular tunneling nanotubes.

As a new method of cell-cell communication, tunneling nanotubes (TNTs) play important roles in cell-cell signaling and mass exchanges. However, a lack of powerful tools to visualize dynamic TNTs with high temporal/spatial resolution restricts the exploration of their formation and cleavage, hindering the complete understanding of its mechanism. Herein, we present the first example of using stochastic optical reconstruction microscopy (STORM) to observe the tube-like structures of TNTs linking live cells with an easily prepared fluorescent dye. Because of this new imaging microscopy, the cleavage process of TNTs was observed with a high spatial resolution.

How do new members affect the relationship between principal investigator's network position and academic output of granted funds?

The paper focuses on how to improve academic output of a granted fund when the adding of new members changes principal investigator's network position. This objective is refined by exploring how new members affect the relationship between principal investigator's network position and the academic output of granted funds, and whether this effect is similar in high-output and low-output collaboration networks. New members are divided into two groups, namely, international collaboration and inbound mobility. Using negative binomial regression on research funds supported by the National Natural Science Foundation of China, the results indicate that new members indeed have moderating effects on the relationship between principal investigator's network position and the academic output of granted funds. Moreover, we find that this moderating effect in high-output collaboration networks is larger than that in low-output collaboration networks. Our findings provide practical implications for the decision makers to design funding planning and for the principal investigators to improve academic output.

[Effect of individualized healing abutment on patients with posterior implant prosthesis and improvement of food impaction symptoms].

PURPOSE: To observe the effect of individualized healing abutment on patients with posterior dental implant prosthesis and its influence on implant stability and food impaction. METHODS: Eighty patients who received posterior dental implants in Jiangsu Stomatological Hospital from June 2013 to June 2018 were selected as the study subjects. According to the different healing abutment, they were divided into traditional operation group (40 cases) and experimental group (40 cases). Patients in the experimental group used personalized healing abutment on the basis of traditional dental implants. Differences in dental implant stability, food impaction score, masticatory efficiency and incidence of complications between the two groups after implant restoration were compared. SPSS 13.0 software package was used to analyze the data. RESULTS: At 1, 3 and 6 months after operation, the stability of implants in the experimental group was significantly higher than that in the control group (P<0.01); One, 3 and 6 months after operation, the food impaction score in the experimental group was significantly lower than that in the traditional operation group(P<0.01); There was no significant difference in masticatory ability between the two groups before operation; After treatment, the occlusive force and masticatory efficiency in the experimental group were significantly higher than those in the traditional operation group (P<0.05). The incidence of complications such as tooth loosening and periodontitis in the experimental group was significantly lower than in the traditional operation group (P<0.05). CONCLUSIONS: Individualized healing abutment has a good therapeutic effect on patients with posterior implant prosthesis, and can significantly improve the incidence of food impaction and complications with a good application value.

Support Vector Machine Classification of Nonmelanoma Skin Lesions Based on Fluorescence Lifetime Imaging Microscopy.

Early diagnosis of malignant skin lesions is critical for prompt treatment and a clinical prognosis of skin cancers. However, it is difficult to precisely evaluate the development stage of nonmelanoma skin cancers because they are derived from the same tissues as a result of the uncontrolled growth of abnormal squamous keratinocytes in the epidermis layer of the skin. In the present study, we developed a linear-kernel support vector machine (LSVM) model to distinguish basal cell carcinoma (BCC) from actinic keratosis (AK) and Bowen's disease (BD). The input parameters of the LSVM model consist of appropriate lifetime components and entropy values, which were extracted from two-photon fluorescence lifetime imaging of hematoxylin and eosin (H&E)-stained biopsy sections. Different features used as inputs for SVM training were compared and evaluated. In constructing the SVM models, features obtained from the lifetime (τ2) of the second component were found to be significantly more predictive than the average fluorescence lifetime (τm) in terms of diagnostic accuracy, sensitivity, and specificity. The above findings were confirmed on the basis of the receiver operating characteristic (ROC) curves of diagnostic models. Shannon entropy was added to the SVM models as an independent feature to further improve the diagnostic accuracy. Therefore, fluorescence lifetime analysis and entropy calculations can provide highly informative features for the accurate detection of skin neoplasm disorders. In summary, fluorescence lifetime imaging microscopy (FLIM) combined with the SVM classification exhibited great potential for developing an effective computer-aided diagnostic criterion and accurate cancer detection in dermatology.

Redefining the photo-stability of common fluorophores with triplet state quenchers: mechanistic insights and recent updates.

Light microscopy can offer certain advantages over electron microscopy in terms of acquiring detailed insights into the biological/intra-cellular milieu. In recent years, with the development of new fluorescence imaging technologies, it has become extremely important to assess the role of designing appropriate fluorophores in acquiring desired biological information without encountering any untoward hitches. Over the years, external fluorophores have been prevalently used in fluorescence microscopy and single-molecule fluorescence microscopy-based studies. Photostable fluorogenic probes with high extinction coefficients and quantum yields, exhibiting minimum autofluorescence and photobleaching properties, are preferred in single-molecule microscopy as they can tolerate long-term laser exposure. Therefore, the development of triplet state quenchers and/or any other suitable new strategy to ensure the photo-stability of the fluorophores during long-term live cell imaging exercises is highly anticipated. In this feature article, various strategies for stabilizing fluorophores, including the mechanisms of TSQ-induced stabilization, have been thoroughly reviewed considering contemporary literature reports and applications.

In Vitro and in Vivo Antitumor Effects of Plant-Derived Miliusanes and Their Induction of Cellular Senescence.

Our earliest phytochemical separation of Miliusa sinensis aided us in the isolation of a class of unique miliusanes, which were demonstrated as anticancer lead molecules. In the present study, we isolated 19 miliusanes (1-19), including 11 novel ones (5 and 10-19) from another Miliusa plant ( M. balansae), and synthesized additional derivatives to elucidate the structure-activity relationship of miliusanes. When extrapolated to various carcinoma xenograft mouse models, miliusol (1) and its derivatives 20, 26, and 27 (7.5-40 mg/kg) were demonstrated with tumor inhibitory efficacy comparable or even superior to the mainstay chemotherapeutics paclitaxel or fluorouracil. To gain a molecular insight into their anticancer mechanism, 1-3 (GI50 0.03-4.79) were administered to a wide spectrum of human cancer cell lines, including those with specific drug resistance. We further revealed that the antiproliferative properties of miliusanes in carcinoma cells were highly associated with the p21-dependent induction of cellular senescence.

Antimalarial Activity of Plant Metabolites.

Malaria, as a major global health problem, continues to affect a large number of people each year, especially those in developing countries. Effective drug discovery is still one of the main efforts to control malaria. As natural products are still considered as a key source for discovery and development of therapeutic agents, we have evaluated more than 2000 plant extracts against Plasmodium falciparum. As a result, we discovered dozens of plant leads that displayed antimalarial activity. Our phytochemical study of some of these plant extracts led to the identification of several potent antimalarial compounds. The prior comprehensive review article entitled “Antimalarial activity of plant metabolites” by Schwikkard and Van Heerden (2002) reported structures of plant-derived compounds with antiplasmodial activity and covered literature up to the year 2000. As a continuation of this effort, the present review covers the antimalarial compounds isolated from plants, including marine plants, reported in the literature from 2001 to the end of 2017. During the span of the last 17 years, 175 antiplasmodial compounds were discovered from plants. These active compounds are organized in our review article according to their plant families. In addition, we also include ethnobotanical information of the antimalarial plants discussed.

Design, synthesis and evaluation of novel dihydrostilbene derivatives as potential anti-melanogenic skin-protecting agents.

The stems of Dendrobium orchids (Orchidaceae), also known as Shi Hu, have been used for medicinal purposes for centuries in oriental countries. In fact, the health benefits of Shi Hu have been evidenced by its modern pharmacological actions on conquering oxidative stress in pathological conditions. From the extracts of two commonly used Dendrobium species, we obtained discernible amounts of stilbenoids, explicitly trans-resveratrol (1) and dihydro-resveratrol (2), which are prototypical antioxidants. When applied to cultured melanocytes, these stilbenoids, dihydro-resveratrol (2) in particular, significantly reduced melanin formation via inhibiting tyrosinase activity and expression of tyrosinase-related proteins. By utilizing dihydro-resveratrol (2) as the basic structural unit, we synthesized 11 novel dihydrostilbene derivatives (3-13) in good yields and purity, with manipulative steps. In addition to their anti-melanogenic activity, some of the novel derivatives are indeed potential antioxidants as they quenched intracellular oxidative radicals in a manner more efficient than Trolox, a water-soluble analogue of vitamin E, and thus premeditated beneficial to skin protection.

Dual roles of TPGS based microemulsion for tacrolimus: Enhancing the percutaneous delivery and anti-psoriatic efficacy.

In this study, we demonstrate for the first time the dual roles of Tocopheryl Polyethylene Glycol 1000 Succinate (TPGS) based microemulsion (ME) for tacrolimus (TAC) to enhance TAC percutaneous delivery and anti-psoriatic efficacy. The ME formulation was developed and optimized based on pseudo-ternary phase diagrams combined with in vitro permeation. The result of Fourier transform infrared spectroscopy (FTIR) demonstrated that TAC was completely solubilized in the TPGS-ME. In vitro permeation studies showed that TPGS-ME enhanced TAC permeation through and into the skin, and the enhanced deposition of TAC in the normal or psoriatic skin was further confirmed in vivo. The cellular uptake performed with HaCaT cells presented more pronounced uptake of TPGS-ME. Topical TAC-TPGS-ME treated imiquimod-induced psoriasis in mice more efficaciously than the commercial formulation of TAC (Protopic®), which is consistent with the enhanced TAC levels by TAC-TPGS-ME in the psoriatic skin. Haematoxylin and Eosin (HE) staining revealed that TAC-TPGS-ME significantly diminished the severity of the psoriasis-like skin inflammation. Moreover, TPGS-ME vehicle exhibited a moderate anti-inflammatory activity, which indicated that TPGS acted as a potential adjuvant in the TAC anti-psoriasis process, and the synergism was identified in anti-proliferation against HaCaT cells. The colloidal nano-carrier combined ME with TPGS is a potential approach for percutaneous delivery of TAC, which exploited both virtues of ME and TPGS to obtain the synergetic effects of enhanced permeability and anti-psoriatic efficacy.