Research Advances in Clinical Applications, Anticancer Mechanism, Total Chemical Synthesis, Semi-Synthesis and Biosynthesis of Paclitaxel.

Paclitaxel, a natural secondary metabolite isolated and purified from the bark of the Taxus tree, is considered one of the most successful natural anticancer drugs due to its low toxicity, high potency and broad-spectrum anticancer activity. Taxus trees are scarce and slow-growing, and with extremely low paclitaxel content, the contradiction between supply and demand in the market is becoming more and more intense. Therefore, researchers have tried to obtain paclitaxel by various methods such as chemical synthesis, artificial culture, microbial fermentation and tissue cell culture to meet the clinical demand for this drug. This paper provides a comprehensive overview of paclitaxel extraction, combination therapy, total synthesis, semi-synthesis and biosynthesis in recent years and provides an outlook, aiming to provide a theoretical basis and reference for further research on the production and application of paclitaxel in the future.

Fabricating Materials of Institute Lavoisier-53(Fe)/zeolite imidazolate framework-8 hybrid materials as high-efficiency and reproducible adsorbents for removing organic pollutants.

Environmental pollution by emerging contaminants has become an urgent problem. Herein, novel binary metal-organic framework hybrids were constructed from Materials of Institute Lavoisier-53(Fe) (MIL-53(Fe)) and zeolite imidazolate framework-8 (ZIF-8) for the first time. A battery of characterizations were employed to determine the MIL/ZIF hybrids' properties and morphology. Furthermore, the MIL/ZIF towards toxic antibiotics (tetracycline, ciprofloxacin and ofloxacin) were studied to explore their adsorption abilities. The present work disclosed that the obtained MIL-53(Fe)/ZIF-8 = 2:3 possessed an eminent specific surface area with an admirable removal efficiency of tetracycline (97.4%), ciprofloxacin (97.1%) and ofloxacin (92.4%), respectively. The tetracycline adsorption process conformed to the pseudo-second-order kinetic model and this process was more compatible with the Langmuir isotherm model with the highest adsorption capacity of 215.0 mg g-1. Moreover, the process of removing tetracycline was proved to be spontaneous and exothermic by the thermodynamic results. Furthermore, the MIL-53(Fe)/ZIF-8 = 2:3 towards tetracycline exhibited significant regeneration ability. The effects of pH, dosage, interfering ions and oscillation frequency on tetracycline adsorption capacity and removal efficiency were also investigated. The primary factors contributing to the decent adsorption ability between MIL-53(Fe)/ZIF-8 = 2:3 and tetracycline included electrostatic, π-π stacking, hydrogen bonding and weak coordination interactions. Additionally, we also investigated the adsorption ability in real wastewater. Thus, the proposed binary metal-organic framework hybrid materials can be deemed a promising adsorbent in wastewater purification.

Does low-intensity pulsed ultrasound accelerate phasic calcium phosphate ceramic-induced bone formation?

PURPOSE: Low-intensity pulsed ultrasound (LIPUS) has been used to stimulate the healing of the fresh fracture, delayed union, and non-union in both animal and clinical studies. Besides, biphasic calcium phosphate ceramic (BCP) is a promising biomaterial for bone repair as it shows favorable biocompatibility, osteoinduction, and osteoconduction. However, scarcity is known about the combined effect of LIPUS and BCP on bone formation. METHODS: The combined effect of LIPUS and BCP was studied in a beagle model. Twelve dogs were used. BCP granules without any additions were implanted into bilateral erector spinae muscles. One side is the BCP group, while the counterlateral side is LIPUS + BCP group. Histological and histomorphometric analyses, and quantitative real-time polymerase chain reaction were evaluated. RESULTS: Compared with BCP alone, the LIPUS + BCP showed no advantages in early bone formation. Furthermore, the Notch signaling pathway-related mRNA has no significant difference between the two groups. CONCLUSIONS: The preliminary results showed that the BCP, which has intrinsic osteoinduction nature, was an effective and promising material. However, LIPUS has no enhanced effect in BCP induced ectopic bone formation. Furthermore, LIPUS has no effect on the Notch signaling pathway. Whether costly LIPUS could be used in combination with BCP should be a rethink.

Current Perspectives on Paclitaxel: Focus on Its Production, Delivery and Combination Therapy.

Paclitaxel is an anticancer drug first isolated from the bark of the Pacific yew tree. It has been widely used for the treatment of ovarian, breast, uterine and other cancers because of its low toxicity, high efficiency and broad-spectrum anticancer activity, and it is considered to be one of the most successful natural anticancer drugs available. Paclitaxel is a microtubule-targeting drug whose main molecular mechanism is to disrupt microtubule dynamics and induce mitotic arrest and cell death. Despite the many clinical successes of paclitaxel, the extraction of natural paclitaxel from Taxus species has proven to be environmentally unsustainable and economically unviable. As a result, researchers are constantly working to find innovative ways to meet society's need for this drug. Currently, many methods, including artificial cultivation, microbial fermentation, chemical synthesis, and tissue and cell culture, have been explored and developed to obtain paclitaxel. In addition, the poor water solubility of paclitaxel has led to significant limitations in its clinical application. Conventional paclitaxel formulations use Cremophor EL and ethanol to dissolve paclitaxel, which can lead to serious side effects. In recent decades, a series of new nanotechnology-based paclitaxel dosage forms have been developed, including albumin-bound paclitaxel, polymeric micellar paclitaxel, polymer-paclitaxel couples, and liposome-encapsulated paclitaxel. These nanoformulations can significantly reduce the toxicity of paclitaxel and greatly improve its anti-tumor efficiency. This paper reviews the development of the production, dosage form and combination therapy of paclitaxel in recent years and presents an outlook, with the aim of providing a theoretical basis and reference for further research on the production and application of paclitaxel in the future.

Stereoscopic Differences in the Identification, Bioactivity, and Metabolism of C-20 and C-24 Epimeric Ginseng Saponins.

Ginseng, the roots and/or rhizomes of Panax spp.(Araliaceae), has been used as a popular herbal medicine in East Asia for at least two millennia. As a functional food and healthenhancing supplement, ginseng has been shown to have a wide range of pharmacological effects on cognition and blood circulation as well as antioxidant, antitumor, and anti-fatigue effects. The main active properties of ginseng are considered to be the triterpene saponins, often referred to as ginsenosides, which are the basis for their wide-ranging pharmacological effects. Four of these glycosides, including protopanaxadiol, protopanaxatriol, ocotillol, and oleanolic acid, are the most common saponins found in ginseng. Compared to other ginsenosides, the C-20 chimeric ginsenosides, including Rg3, Rh2, Rg2, Rh1, PF11, C-20, and C-24, as well as epimeric ocotillol-type saponins and their derivatives exhibit significant, steric differences in biological activity and metabolism. 20(R)-ginseng saponins, one class of important rare ginsenosides, have antitumor, antioxidative, antifatigue, neuroprotective and osteoclastogenesis inhibitory effects. However, 20(R)- ginsenosides are rare in natural products and are usually prepared from 20(S)-isomers through chemical differential isomerization and microbial transformation. The C20 configuration of 20(R)-ginseng saponins is usually determined by 13C NMR and X-ray single-crystal diffraction. There are regular differences in the chemical shift values of some of the carbons of the 20(S)- and 20(R)-epimers, including C-17, C-21, and C-22. Owing to their chemical structure and pharmacological and stereoselective properties, 20(R)-ginseng saponins have attracted a great deal of attention in recent years. Herein, the stereoscopic differences in the identification, bioactivity, and metabolism of C-20 and C-24 epimeric ginseng saponins are summarized.

Analysis of carbon emission drivers of secondary industries in Energy "Golden Triangle" area based on LMDI and two-dimensional decoupling model.

As an essential energy and chemical base in China, carbon reduction in the Energy "Golden Triangle" (EGT) area is significant. This paper used the logarithmic mean Divisia index (LMDI) method to analyze the drivers of carbon emissions from secondary industry energy consumption (CESEC) in EGT from 2005 to 2019 and then used the GM (1,1) method to simulate carbon emissions in 2030. Meanwhile, the decoupling relationship between carbon emissions and economic development was also analyzed using the two-dimensional decoupling model to test the effectiveness of carbon reduction by the region's government. This paper showed the following: (1) CESEC in the EGT area increased from 1.89×108t to 2.617×108 t; (2) the economic output effect is the main factor influencing carbon emissions in the EGT area, followed by population effect and energy structure effect, while energy intensity effect mitigates carbon emissions; and (3) CESEC will peak at 12.362×108t in 2030, leaving an arduous task on carbon reduction. The two-dimensional decoupling condition between carbon emissions and economic growth in the EGT area is low level-weak decoupling (WD-LE) for 2005-2019. The decoupling condition in Yulin and Ningdong is concentrated in low level-expansion connection (EC-LE) and low level-weak decoupling (WD-LE). Furthermore, Erdos reached high level-expansion negative decoupling (END-HE) condition during 2015-2019. Based on the above findings, a low-carbon development strategy for EGT should consider improving emission reduction technologies for high-carbon energy sources like coal, adjusting the energy consumption structure and seeking government policy support for carbon reduction.

Does low-intensity pulsed ultrasound accelerate phasic calcium phosphate ceramic-induced bone formation?

Purpose: Low-intensity pulsed ultrasound (LIPUS) has been used to stimulate the healing of the fresh fracture, delayed union, and non-union in both animal and clinical studies. Besides, biphasic calcium phosphate ceramic (BCP) is a promising biomaterial for bone repair as it shows favorable biocompatibility, osteoinduction, and osteoconduction. However, scarcity is known about the combined effect of LIPUS and BCP on bone formation. Methods: The combined effect of LIPUS and BCP was studied in a beagle model. Twelve dogs were used. BCP granules without any additions were implanted into bilateral erector spinae muscles. One side is the BCP group, while the counterlateral side is LIPUS + BCP group. Histological and histomorphometric analyses, and quantitative real-time polymerase chain reaction were evaluated. Results: Compared with BCP alone, the LIPUS + BCP showed no advantages in early bone formation. Furthermore, the Notch signaling pathway-related mRNA has no significant difference between the two groups. Conclusions: The preliminary results showed that the BCP, which has intrinsic osteoinduction nature, was an effective and promising material. However, LIPUS has no enhanced effect in BCP induced ectopic bone formation. Furthermore, LIPUS has no effect on the Notch signaling pathway. Whether costly LIPUS could be used in combination with BCP should be a rethink.

Porous Organic Cage-Embedded C10-Modified Silica as HPLC Stationary Phase and Its Multiple Separation Functions.

Reduced imine cage (RCC3) was covalently bonded to the surface of silica spheres, and then the secondary amine group of the molecular cage was embedded in non-polar C10 for modification to prepare a novel RCC3-C10@silica HPLC stationary phase with multiple separation functions. Through infrared spectroscopy, thermogravimetric analysis and nitrogen adsorption-desorption characterization, it was confirmed that RCC3-C10 was successfully bonded to the surface of silica spheres. The resolution of RCC3-C10@silica in reversed-phase separation mode is as high as 2.95, 3.73, 3.27 and 4.09 for p-phenethyl alcohol, 1-phenyl-2-propanol, p-methylphenethyl alcohol and 1-phenyl-1-propanol, indicating that the stationary phase has excellent chiral resolution performance. In reversed-phase and hydrophilic separation modes, RCC3-C10@silica realized the separation and analysis of a total of 70 compounds in 8 classes of Tanaka mixtures, alkylbenzene rings, polyphenyl rings, phenols, anilines, sulfonamides, nucleosides and flavonoids, and the analysis of a variety of chiral and achiral complex mixtures have been completed at the same time. Compared with the traditional C18 commercial column, RCC3-C10@silica exhibits better chromatographic separation selectivity, aromatic selectivity and polar selectivity. The multifunctional separation mechanism exhibited by the stationary phase originates from various synergistic effects such as hydrophobic interaction, π-π interaction, hydrogen bonding and steric interaction provided by RCC3 and C10 groups. This work provides flexible selectivity and application prospects for novel multi-separation functional chromatographic columns.

Sesame (Sesamum indicum L.): A Comprehensive Review of Nutritional Value, Phytochemical Composition, Health Benefits, Development of Food, and Industrial Applications.

Sesame (Sesamum indicum L.), of the Pedaliaceae family, is one of the first oil crops used in humans. It is widely grown and has a mellow flavor and high nutritional value, making it very popular in the diet. Sesame seeds are rich in protein and lipids and have many health benefits. A number of in vitro and in vivo studies and clinical trials have found sesame seeds to be rich in lignan-like active ingredients. They have antioxidant, cholesterol reduction, blood lipid regulation, liver and kidney protection, cardiovascular system protection, anti-inflammatory, anti-tumor, and other effects, which have great benefits to human health. In addition, the aqueous extract of sesame has been shown to be safe for animals. As an important medicinal and edible homologous food, sesame is used in various aspects of daily life such as food, feed, and cosmetics. The health food applications of sesame are increasing. This paper reviews the progress of research on the nutritional value, chemical composition, pharmacological effects, and processing uses of sesame to support the further development of more functionalities of sesame.

Fabrication of hydrangea-shaped Bi2WO6/ZIF-8 visible-light responsive photocatalysts for degradation of methylene blue.

In this paper, the hydrangea-shaped Bi2WO6/ZIF-8 (BWOZ) visible light photocatalysts have been prepared via a facile synthetic strategy for the first time. The constructed BWOZ composites were systematically studied by a series of characterization techniques. The SEM results manifested the octahedral ZIF-8 coated the flower-like Bi2WO6 uniformly and the composition of BWOZ composites had been confirmed by XPS measurement. And the photocatalytic activity was evaluated by eliminating methylene blue with the help of visible light. The results showed that 7%-BWOZ (7.0 wt% Bi2WO6) exhibited better photodegradation capability than pure Bi2WO6 and ZIF-8. Compared with Bi2WO6, the photocatalytic degradation of methylene blue by 7%-BWOZ could reach 85.7%. In addition, the pseudo-first-order kinetic constant of 7%-BWOZ was 23.00 and 1.61 times that of pristine Bi2WO6 and ZIF-8, respectively. The improved photocatalytic ability of BWOZ systems may be due to the construction of heterojunctions between Bi2WO6 and ZIF-8, which resulted in the rapid separation of photogenerated carriers. Additionally, the specific surface area of the formed BWOZ system was also improved in comparison with the flower-shaped Bi2WO6, and thus more active sites could be provided to contact with methylene blue molecules, thereby achieving better removal capacity. Moreover, trapping experiments and electron spin resonance results further illustrated that the coexistence of multiple free radicals realized efficient degradation of methylene blue. More importantly, the photocatalytic property of the 7%-BWOZ composite remained even after three cycles. Furthermore, a feasible photodegradation mechanism was also explored in depth.

Variations of root and canal morphology of mandibular second molars in Chinese individuals: a cone-beam computed tomography study.

BACKGROUND: The mandibular second molars demonstrate variations on root and canal morphology. The aim of this study was to investigate all the root canal morphology of mandibular second molars and analyze the morphological variations in patients by gender and age in a Chinese population use CBCT imaging. METHODS: Cone-beam computed tomographic images of 1200 bilateral mandibular second molars were obtained from 600 patients (300 females and 300 males) who required a preoperative assessment for implant surgery, surgical removal of impacted teeth, orthodontic treatment, surgery of maxillofacial tumour and cysts or LeFort I osteotomy. CBCT images were divided into 5 groups according to age: "15-24 years", "25-34 years", "35-44 years", "45-54 years" and "≥ 55 years"; and 2 groups by gender: "females" and "males". The following information were recorded: the number of roots and canals and their morphology, the frequency and configuration of C-shaped canals by gender, age and position (left and right). The chi-square test was used to analyse differences between groups. P value of < 0.05 was considered statistically significant. RESULTS: Of the 1200 teeth, 61% had two separate roots located mesiodistally, 35.6% had one C-shaped root. The 45.3% teeth had three canals in two-rooted mandibular second molars. The mesial root showed a Vertucci type II configuration in 28.9% cases followed by type IV(24.4%). While the distal root showed a significant higher prevalence of type I configuration in 95.6%. In the examined 1200 teeth, 430 teeth (35.8%) had C-shaped root canals. The prevalence of C-shaped root canal systems was significantly higher in females (42.5%) than in males (29.1%) (P = 0.000), and did not differ with age (P = 0.126). The 80.4% C-shaped canals were bilateral (P = 0.000) and did not differ with side (left and right) (P = 0.758). CONCLUSIONS: The most commonly observed root morphology for the mandibular second molars was 2 separate roots with three canals.The prevalence of C-shaped root canal is 35.8% and is more higher in females than in males.

Effect of extrusion-spheronization granulation and manganese loading on catalytic ozonation of petrochemical wastewater.

The petrochemical secondary effluent (PSE) is typical refractory wastewater derived from the petrochemical industries, which requires advanced treatment due to the strict environmental protection policies. Catalytic ozonation is one of the most widely used advanced oxidation technologies in wastewater treatment because of its high mineralization rate, in which the alumina-based catalyst usually plays an important role. Extrusion-spheronization is a promising technique for the preparation of alumina spheres because the synthesized alumina particles have high sphericity, high specific surface aera and narrow particle size distribution. In this paper, two kinds of alumina-based catalysts (catalyst A: manganese nitrate added after alumina granulation and catalyst B: manganese nitrate added into alumina powder before granulation) were prepared by the extrusion-spheronization method and used for PSE treatment by catalytic ozonation. The prepared alumina samples were characterized by Brunauer-Emmett-Teller (BET) method, X-ray photoelectron spectroscopy (XPS), X-ray diffraction (XRD) and scanning electron microscopy (SEM), while the wastewater samples were analyzed for Total organic carbon (TOC), UV254 and fluorescence spectroscopy. Results showed that manganese was uniformly distributed in both catalysts, and the specific surface area of two catalysts was 318.36 m2/g and 354.95 m2/g, respectively. Catalytic ozonation experiments were repeated nine times with each catalyst under the same conditions. The TOC removal rates for catalysts A and B in the first run were 48.88% and 49.06%, respectively, then it dropped to 28.05% for catalyst A but remained 47.81% for catalyst B after using for nine times. This implied that the long-term performance of catalyst B would be more stable than catalyst A. Similar result were found in three-dimensional fluorescence analysis. UV254 results indicated that the removal efficiency of aromatic and unsaturated substances by catalyst B was higher than catalyst A. A possible explanation is that the active component manganese oxide formed a catalyst skeleton in catalyst B, which makes it hard to dissolve. Effect of extrusion-spheronization granulation and manganese loading on advanced oxidant treatment of petrochemical wastewater.

LncRNA GACAT1 induces tongue squamous cell carcinoma migration and proliferation via miR-149.

Recent studies have observed that lncRNAs (long non-coding RNAs) are involved in the progression of various tumours including tongue squamous cell carcinoma (TSCC). Recently, a new lnRNA, GACAT1, has been firstly identified in gastric cancer. However, its potential role in TSCC remains unknown. In this reference, we observed that GACAT1 was overexpressed in TSCC samples and cell lines. Of 25 TSCC specimens, GACAT1 expression was overexpressed in 18 patients (18/25, 72%) compared to non-tumour specimens. Ectopic expression of GACAT1 induced cell growth and migration and promoted epithelial to mesenchymal transition in TSCC. In addition, ectopic expression of GACAT1 decreased miR-149 expression in SCC1 cell. We observed that miR-149 expression was down-regulated in TSCC cell lines. Moreover, we observed that GACAT1 expression was negatively correlated with miR-149 expression. GACAT1 overexpression induced TSCC cell growth and migration via regulating miR-149 expression. These data provided that GACAT1 played an oncogenic role in the progression of TSCC partly through modulating miR-149 expression.

lncRNA RPSAP52 induced the development of tongue squamous cell carcinomas via miR-423-5p/MYBL2.

Growing lncRNAs have been noted to involve in the initiation and development of several tumours including tongue squamous cell carcinomas (TSCCs). However, the biological role and mechanism of lncRNA RPSAP52 were not well-explained. We indicated that RPSAP52 was higher in TSCC samples compared with that in control samples. The higher expression of RPSAP52 was positively correlated with higher T stage and TNM stage. Ectopic expression of RPSAP52 induced TSCC cell growth and cycle and induced cytokine secretion including IFN-γ, IL-1ß and IL-6, IL-8, IL-10 and TGF-ß. We found that the overexpression of RPSAP52 suppressed miR-423-5p expression in SCC-4 cell. miR-423-5p was lower in TSCC samples compared with that in control samples, and miR-423-5p level was negatively correlated with higher T stage and TNM stage. Pearson's correlation indicated that miR-423-5p was negatively associated with that of RPSAP52 in TSCC tissues. Furthermore, MYBL2 was one direct gene of miR-423-5p and elevated expression of miR-423-5p suppressed MYBL2 expression and ectopic expression of RPSAP52 increased MYBL2 expression in SCC-4 cell. Finally, we illustrated that RPSAP52 overexpression promoted TSCC cell growth and cycle and induced cytokine secretion including IFN-γ, IL-1ß and IL-6, IL-8, IL-10 and TGF-ß via modulating MYBL2. These data provided new insight into RPSAP52, which may be one potential treatment target for TSCC.

LUCAT1 as an oncogene in tongue squamous cell carcinoma by targeting miR-375 expression.

Emerging studies suggested that lncRNAs play a crucial molecular role in cancer development and progression. LncRNA LUCAT1 has been proved as oncogenic molecular in lung cancer, glioma, osteosarcoma, renal carcinoma and oesophageal squamous cell carcinoma. However, its roles and function mechanisms in tongue squamous cell carcinoma (TSCC) are still unknown. We showed that the expression of LUCAT1 was up-regulated in the TSCC cells and tissues and the higher LUCAT1 expression was associated with the poor overall survival (OS). Knockdown expression of LUCAT1 suppressed TSCC cell proliferation, cycle and migration. In addition, we demonstrated that miR-375 overexpression inhibited the luciferase activity of LUCAT1 wild-type and knockdown LUCAT1 promoted the miR-375 expression in TSCC cell. Furthermore, we indicated that miR-375 expression was down-regulated in the TSCC cell lines and tissues and the lower expression of miR-375 was associated with poor OS. The expression of miR-375 was inversely correlated with LUCAT1 expression in the TSCC tissues. Knockdown LUCAT1 promoted TSCC cell proliferation, cell cycle and migration partly through regulating miR-375 expression. In summary, this study suggested the tumorigenic effect of lncRNA LUCAT1 in TSCC cells by targeting miR-375 expression.

Isolation and identification of alkaloids from Macleaya microcarpa by UHPLC-Q-TOF-MS and their cytotoxic activity in vitro, antiangiogenic activity in vivo.

BACKGROUND: Extensive bioactivities of alkaloids from the genus Macleaya (Macleaya cordata (Willd.) R. Br. and Macleaya microcarpa (Maxim.) Fedde) have been widely reported, as well as more and more concerned from the scientific communities. However, systematic research on the phytochemical information of M. microcarpa is incomplete. The aim of this study was to rapidly and conveniently qualitative analyze alkaloids from M. microcarpa by ultra-performance liquid chromatography/quadrupole-time-of-fight mass spectrometry (UHPLC-Q-TOF-MS) using accurate mass weight and characteristic fragment ions, furthermore separate and identify the main alkaloids, test antitumor activity in vitro and antiangiogenic activity in vivo. RESULTS: A total of 14 alkaloids from fruits of M. microcarpa were identified by UHPLC-Q-TOF-MS, including 5 protopines, 2 benzophenanthridines, 1 dimer, 1 dihydrobenzophenanthridines and 5 unknown structure compounds. Two major alkaloids were isolated by various column chromatographic methods. Their structures were determined by NMR data and related literatures. The two major alkaloids were evaluated for intro cytotoxic activities against HL-60, MCF-7, A-549, and in vivo antiangiogenic activity using transgenic zebrafish. CONCLUSIONS: Current qualitative method based on UHPLC-Q-TOF-MS technique provided a scientific basis for isolation, structural identification, and in vitro or in vivo pharmacological further study of alkaloids from M. microcarpa in the future.

Intermolecular Chirality Modulation of Binaphthalene-Bridged Bisporphyrins With Chiral Diamines.

A new pair of 2,2'-diamino-1,1'-binaphthyl linked porphyrin dimers, (R)-/(S)-H, were synthesized to study their supramolecular interactions with a pair of chiral diamines ((R)-/(S)-PPDA) by using UV-Vis absorption, fluorescence and NMR titrations. The spectroscopic titrations indicated that sandwich-type 1:1 complexes were formed at low guest concentration and then transformed to 1:2 open complexes at high guest concentration. The supramolecular interactions afforded sensitive circular dichroism responses, and the CD signs of the 1:1 complexes are decided by the stereostructure of chiral diamine guests. Moreover, due to the shortened linking units, (R)-/(S)-H show more sensitive and predicable CD response than the previously reported hosts (R)-/(S)-H1 and this can be reasonably explained by DFT molecular modeling. The present results suggest (R)-/(S)-H are promising for chiral optical sensing.

Optimization of Ultrasonic-Assisted Extraction and Purification of Zeaxanthin and Lutein in Corn Gluten Meal.

Zeaxanthin and lutein have a wide range of pharmacological applications. In this study, we conducted systematic experimental research to optimize antioxidant extraction based on detection, extraction, process amplification, and purification. An ultrasonic-assisted method was used to extract zeaxanthin and lutein with high efficiency from corn gluten meal. Firstly, the effects of solid-liquid ratio, extraction temperature, and ultrasonic extraction time on the extraction of zeaxanthin were investigated in single-factor experiments. The optimization extraction parameters of zeaxanthin and lutein with ethanol solvent were obtained using the response surface methodology (RSM) as follows: liquid-solid ratio of 7.9:1, extraction temperature of 56 °C, and extraction time of 45 min. The total content of zeaxanthin and lutein was 0.501%. The optimum extraction experimental parameters were verified by process amplification, and we confirmed that the parameters of the extraction process optimized using the RSM design are reliable and precise. Zeaxanthin and lutein from crude extract of corn gluten were separated and purified using silica gel column chromatography with the purity of zeaxanthin increasing from 0.28% to 31.5% (about 110 times) and lutein from 0.25% to 16.3% (about 65 times), which could be used for large-scale industrial production of carotenoids.

Long non-coding RNA CASC2 serves as a ceRNA of microRNA-21 to promote PDCD4 expression in oral squamous cell carcinoma.

Background: Oral squamous cell carcinoma (OSCC) is a common oral disease with high morbidity and mortality. Recently, long non-coding RNAs (lncRNAs) were identified as critical regulators in OSCC tumorigenesis. The present study aimed to work out the functions and the possible molecular mechanisms of lncRNA CASC2 in human OSCC. Methods: The expression levels of CASC2 in clinical OSCC tissue samples and cultured OSCC cell lines were detected by RT-qPCR analysis. MTT assay was performed to detect the proliferation ability of OSCC cells, whereas the apoptosis rate and cell cycle distribution of OSCC cells were determined by flow cytometric analysis. The expression levels of relevant proteins were detected by Western blot assay. Dual-luciferase reporter assay was performed to validate the predicted relationship between CASC2, miR-21 amd PDCD4. The role of CASC2 in OSCC tumorigenesis in vivo was evaluated using a nude mouse tumor model. Results: The results demonstrated that CASC2 was significantly downregulated in clinical OSCC tissue samples and cultured OSCC cell lines. Low CASC2 expression was closely correlated with adverse clinicopathological characteristics of OSCC patients. Functionally, overexpression of CASC2 remarkably inhibited cell proliferation partly through inducing cell cycle arrest and cell apoptosis. Furthermore, bioinformatics analysis and dual-luciferase reporter assay showed that CASC2 might act as a competing endogenous RNA of miR-21 to promote the expression of PDCD4. Rescue experiments also showed that miR-21 blocked the tumor-suppressive role that CASC2 exerted in OSCC cells. Finally, in vivo study indicated that overexpression of CASC2 restrained OSCC tumor growth in volume and weight. Conclusion: In conclusion, these findings indicate that CASC2/miR-21/PDCD4 axis might be a potential regulator of OSCC tumorigenesis, and shed new light on lncRNA-directed diagnostics and therapeutics in OSCC.

Wide pH range enantioseparation of cyclodextrin silica-based hybrid spheres for high performance liquid chromatography.

pH plays an important role in the enantiomeric separation process by changing the polarity of the mobile phase and the conformation and ionization state of the enantiomers. Herein, ß-cyclodextrin-silica hybrid spheres with n-propyl groups as hydrophobic linkers and ethyl-silica as a support were prepared using a one-pot approach, and then the hydroxyl group was further modified with 3,5-dimethylphenyl isocyanate. The new ß-cyclodextrin-silica hybrid chiral stationary phase (CD-HCSP) was prepared and characterized using techniques including scanning electron microscopy and transmission electron microscopy. The enantioseparation properties of CD-HCSP were evaluated with different solvents over a wide pH range (1-10) in reversed phase. 14 enantiomers were successfully resolved, and favorable chiral resolution and high stability was demonstrated for multiple types of enantiomer under different pH conditions. Compared with commercial columns, CD-HCSP showed better chiral resolution and, more importantly, could be used for chiral resolution over a wide pH range. This work combines the high pH tolerance of the hybrid material and excellent chiral recognition of cyclodextrin for enantioseparation of chiral drugs, which could lead to the development of a new type of chiral separation material.