LncRNA SLC7A11-AS1 promotes the progression of hepatocellular carcinoma by mediating KLF9 ubiquitination.

Hepatocellular carcinoma (HCC) is a malignant tumor, which seriously threatens the life of patients. LncRNA SLC7A11-AS1 was reported to be abnormally expressed in HCC. Here, the functions and relative molecular regulatory mechanism of SLC7A11-AS1 in HCC were investigated. Nude mice and HCC cells were used as the experimental subjects. Knockdown or overexpression of exogenous genes was conducted in HCC cells. RT-qPCR, IHC, and western blot were employed to evaluate the abundance of genes and proteins. The malignant behaviors were evaluated using CCK-8, clone formation, wound-healing, and Transwell. The locations of SLC7A11-AS1 and KLF9 in cells were determined by FISH and IF assays. The total m6A level was evaluated by dot-blot assay. m6A modification of SLC7A11-AS1 was detected using RNA MeRIP. The interactions among molecules were validated by RIP, ChIP, dual luciferase reporter assay, and co-IP. SLC7A11-AS1 was elevated apparently in HCC cells and HCC tissues from mice. SLC7A11-AS1 silencing could suppress HCC progression, which was validated in in vivo and in vitro experiments. Furthermore, METTL3 mediated m6A modification of SLC7A11-AS1 to elevate its expression. In addition, SLC7A11-AS1 downregulated KLF9 expression by affecting STUB1-mediated ubiquitination degradation and KLF9 enhanced PHLPP2 expression to inactivate the AKT pathway. Eventually, rescue experiments revealed that KLF9 knockdown abolished SLC7A11-AS1 silencing-mediated suppression of HCC progression in vivo and in vitro. Our results unveiled that m6A-modified SLC7A11-AS1 promoted HCC progression by regulating the STUB1/KLF9/PHLPP2/AKT axis, indicating that targeting SLC7A11-AS1 might alleviate HCC progression.

Visible-Light-Promoted Phosphorylation/Cyclization of 1-Acryloyl-2-cyanoindoles in Green Solvent.

A visible-light-induced persulfate-promoted cascade phosphorylation/cyclization reaction to access various phosphorylated pyrrolo[1,2-a]indolediones under mild conditions was developed. Notably, the transformation was carried out with diethyl carbonate/H2O as a green medium at room temperature. More impressively, traditional metal catalysts and photocatalysts could be effectively avoided. The reactions are simple to operate, easy to scale up, and have good functional group tolerance.

Phosphorus Radical-Initiated Cascade Reaction To Access 2-Phosphoryl-Substituted Quinoxalines.

An effective radical cascade cyclization strategy was developed, by which a wide range of 2-phosphoryl-substituted quinoxalines were prepared in one pot via reaction of ortho-diisocyanoarenes with diarylphosphine oxides in the presence of AgNO3 under mild reaction conditions.

[Ecology suitability regions and ecological characteristics of Panax notoginseng (Burk.) F.H. Chen based on maximum entropy model].

The ecology suitability and ecological characteristics of Panax notoginseng (Burk.) F. H. Chen were studied to provide a reference for its artificial introduction and cultivation. The maximum entropy model (MaxEnt) and geographic information system (GIS) were used to investigate the global ecology suitability regions for Panax notoginseng (Burk.) F. H. Chen based on its 67 distribution points collected from global biodiversity information facility (GBIF), Chinese virtual herbarium(CVH) and the related references. The results showed that the possible ecological suitable regions of Panax notoginseng (Burk.) F. H. Chen were located in Yunnan, Guangxi, Guangdong, Guizhou, Hainan, Sichuan, Fujian and Chongqing provinces. The areas with ecological similarity higher than 60% were about 89 571.3 square kilometers in total, mainly distributing in Yunnan and Guangxi provinces and small portion was located in Guangdong and Guizhou provinces. The areas with ecological similarity between 40% and 60% were about 155 172 square kilometers, mainly in Yunnan,Guangxi, Guangdong, Guizhou, Hainan, Sichuan provinces. The distribution areas were about 329 952.8 square kilometers with ecological similarity between 20% and 40%, mainly in Yunnan, Guangxi, Guangdong, Guizhou, Hainan, Sichuan, Fujian and Chongqing. The climate factors mainly affecting the distribution of Panax notoginseng (Burk.) F. H. Chen were precipitation of warmest quarter, SD of temperature seasonality, altitude, isothermality, coefficient of variation of precipitation seasonality, mean temperature of monthly, precipitation of driest month, reference bulk density of soil and soil texture.

[Spatial Distribution and Global Potential Suitability Regions of Artemisia annua].

OBJECTIVE: To study the spatial distribution and potential climatic suitability regions of Artemisia annua around the world. METHODS: The spatial distribution and climatic characteristics were researched by factor analysis based on Global Biodiversity Information Facility Database and World Climate Database. The global potential suitability regions of Artemisia annua were analyzed by ArcGIS. RESULTS: Artemisia annua distributed in three longitude zones, including 90. 55 °W - 77. 14 °W, 2. 03 °E - 11. 75 °E and 98. 27 °E - 111. 05 °E,which were respectively in North America, Europe and Asia. The latitude range was mainly 29. 15 °N - 51. 36 ° N. 80% of Artemisia annua were in the regions which elevation range was 22. 00 - 491. 00 m, annual precipitation was 492. 30 ~ 1 366. 70 mm, annual average temperature was from 8. 10 to 17. 27 °C. The potential suitability regions of Artemisia annua with 95% ~ 100% climate similarity were mainly in 30 °S and 30 °N regions, centered around the equator axis. Conclusion: Latitude is closely related to the distribution of Artemisia annua, the key affecting climatic factors are annual precipitation, the wettest season precipitation, the warmest season precipitation and the highest temperature in the warmest month, the average temperature of the warmest season, as well as the average temperature of the wettest season. The potential suitability regions of Artemnisia annua are in eastern North America, western Europe and eastern Asia.

Visible-light-induced photocatalyst-free cascade cyclization of 3-(2-(ethynyl)phenyl)quinazolinones to sulfonated quinolino[2,1-b]quinazolinones.

A visible-light-induced K2S2O8-promoted cascade sulfonation/cyclization reaction was established using 3-(2-(ethynyl)phenyl)quinazolinones as efficient substrates under mild conditions. A series of sulfonated quinolino[2,1-b]quinazolinones were successfully synthesized under transition-metal- and photocatalyst-free conditions. Notably, this strategy has the advantages of room temperature and simple operation, easy scale-up, and good functional group tolerance.

1-Acryloyl-2-cyanoindole: A Skeleton for Visible-Light-Induced Cascade Annulation.

1-Acryloyl-2-cyanoindoles were found to be novel and efficient skeletons in visible-light-induced persulfate-promoted cascade cyclization reactions. With this transition-metal-free photocatalytic procedure, various sulfonated/thiocyanated pyrrolo[1,2-a]indolediones were synthesized from 1-acryloyl-2-cyanoindoles with sulfonyl hydrazides/NH4SCN at room temperature under mild reaction conditions.

Visible-Light-Induced Cascade Cyclization of 3-(2-(Ethynyl)phenyl)quinazolinones to Phosphorylated Quinolino[2,1-b]quinazolinones.

3-(2-(Ethynyl)phenyl)quinazolinones were designed and synthesized as a class of novel and efficient skeletons for phosphorylation/cyclization reactions. Under visible light irradiation, a series of phosphorylated quinolino[2,1-b]quinazolinones (35 examples, up to 87% yield) were first synthesized from 3-(2-(ethynyl)phenyl)quinazolinones and diarylphosphine oxides by using 4CzIPN as a photocatalyst under mild conditions. This reaction was also applicable under sunlight irradiation. Moreover, the reaction efficiency could be significantly improved under continuous-flow conditions.

Acyl Radicals from α-Keto Acids: Metal-Free Visible-Light-Promoted Acylation of Heterocycles.

A general and metal-free visible-light-induced decarboxylative arylation procedure at room temperature was described for the construction of acylated heterocyclic derivatives, such as benzimidazo/indolo[2,1-a]isoquinolin-6(5H)-ones, aroylazaspiro[4.5]trienones, thioflavones, and so on. This practical arylation procedure was conducted by using 2,4,5,6-tetra(9H-carbazol-9-yl)isophthalonitrile (4CzIPN) as a photocatalyst under mild conditions, which avoided the use of an additional base, traditional heating, and metal reagents.

[Study on pharmacokinetics of phillyrin in Shuanghuanglian for injection].

OBJECTIVE: To study the plasma concentration and pharmacokinetics of phillyrin in Shuanghuanglian for injection in rats. METHODS: SD rats were given Shuanghuanglian for injection by iv, blood samples were collected at different time. The phillyrin concentration in plasma was determined by RP-HPLC. The parameters of pharmacokinetics were analyzed by program DAS 2.0. RESULTS: The main pharmacokinetics parameters of phillyrin in rats:t1/2 (alpha) (0.44 +/- 0.06) h, t1/2 (beta) (2.77 +/- 0.36) h, V1 (0.09 +/- 0.01) L/kg, CL (0.09 +/- 0.007) L/(h x kg), AUC0-1, (5.56 +/- 0.47 mg x h/L), AUC0-infinity (6.44 +/- 0.53) mg x h/L. CONCLUSION: Phillyrin has two compartment model in rats, the pharmacokinetics of phillyrin characteristic is a process of rapid dispatching and slow elimination in rats.

Arylaminomethyl Radical-Initiated Cascade Annulation Reaction of Quinoxalin-2(1H)-ones Catalyzed by Recyclable Photocatalyst Perovskite.

A feasible arylaminomethyl radical-triggered tandem annulation reaction has been developed toward a large variety of poly fused heterocycles, tetrahydroimidazo[1,5-a]quinoxalin-4(5H)-ones, by reacting diverse quinoxalin-2(1H)-ones with various N-arylglycines in green solvent (DMC) in the presence of CsPbBr3 under white-light irradiation conditions.

Visible-Light Induced Radical Perfluoroalkylation/Cyclization Strategy To Access 2-Perfluoroalkylbenzothiazoles/Benzoselenazoles by EDA Complex.

A novel and practical fluoroalkyl radical-initiated cascade reaction was developed to access diverse 2-fluoroalkylbenzothiazoles by reacting various fluoroalkyl radical sources, including perfluoroalkyl iodide (IC nF2 n+1, n = 3-8, 10), ICF(CF3)2, ICF2COOEt, ICF2CF2Cl, or ICF2CF2Br, tetramethylethane-1,2-diamine (TMEDA), and 2-isocyanoaryl thioethers in tetrahydrofuran under nitrogen atmosphere and blue-light irradiation conditions. Furthermore, this one-pot protocol could well be expanded to access various 2-fluoroalkylbenzoselenazoles starting from (2-isocyanophenyl)(methyl)selane, perfluoroalkyl iodides (IC nF2 n+1, n = 3-8) or ICF2COOEt and TMEDA.

Antiviral treatment of hepatitis B virus-transgenic mice by a marine organism, Styela plicata.

AIM: To evaluate the antiviral effect of the effective ingredient of Styela plicata in a murine model of hepatitis B virus carrier. METHODS: HBV-transgenic mice were divided into 3 groups (control group, lamivudine treatment group and the effective ingredient of Styela plicata treatment group) and assigned to receive normal diet, lamivudine or the effective ingredient of Styela plicata for consecutive weeks. Serum hepatitis B surface antigen was detected by enzyme-linked immunosorbent assay (ELISA) method. Serum HBV DNA was detected by real-time polymerase chain reaction (RT-PCR). Serum T helper (h) 1 cytokine interleukin (IL)-2 and Th2 cytokine IL-6 were detected by the quantitative sandwich enzyme immunoassay technique. Another group of HBV-transgenic mice was assigned to receive the effective ingredient of Styela plicata for consecutive weeks. The histology of liver tissue was evaluated before and after treatment. RESULTS: Twelve weeks after starting the therapy, serum hepatitis B surface antigen was significantly lowered in Styela plicata -treated mice and lamivudine-treated mice compared with the mice receiving normal diet (F(12wk) = 88.81, P(12wk) = 0.000<0.01). Serum HBV DNA was significantly lowered in Styela plicata -treated mice and lamivudine-treated mice compared with the mice receiving normal diet (F(12wk) = 20.71, P(12wk) = 0.000<0.01). However, like lamivudine, the effective ingredient of Styela plicata could not inhibit the replication of HBV completely. A rebound phenomenon of hepatitis B surface antigen and HBV DNA in sera could be found 4 wk after withdrawal of medication. Eight weeks after starting the therapy, serum levels before and after Styela plicata treatment of IL-2 were 2.41 +/- 0.38 and 10.56 +/- 0.78 ng/L, respectively (t(8wk) = -16.51, P(8wk) = 0.000<0.01). Compared with the serum levels of IL-2 in the normal diet-treated mice (2.48+/-0.17 ng/L; t(8wk) = 13.23, P(8wk) = 0.000<0.01). Serum levels before and after Styela plicata treatment of IL-6 were 63.62 +/- 6.31 and 54.52 +/- 6.22 ng/L, respectively, compared with the serum levels of IL-6 in the normal diet-treated mice (60.84 +/- 4.21 ng/L). Histological analysis of liver from Styela plicata-treated HBV-transgenic mice also showed catabatic status in inflammation and hepatitis B surface antigen. CONCLUSION: Styela plicata may be an effective antiviral medicine in treating chronic hepatitis B.

Chemometrics-based approach to feature selection of chromatographic profiles and its application to search active fraction of herbal medicine.

In our previous report (J Pharmaceut Biomed 56 (2011) 443-447), a support vector machine (SVM)-based pharmacodynamic model was established for predicting active fractions of herbal medicines (HMs), where information contents embedded in the chromatograms of the fractions were represented with the peak areas. However, in this representation the global characteristics of the chromatograms were completely missed, which is definitely contrary to the global and holistic views in theories of HMs and undoubtedly reduce the success rate of this model. To deal with the challenge, two chemometrics methods, that is, minimum redundancy maximum relevance (mRMR) and particle swarm optimizer (PSO), were applied in this article for feature selection of the whole chromatograms, and the PSO was also used to tune the SVM parameters. As a case, a sample HM, that is, Xiangdan injection, was investigated. The predictive accuracy was fully evaluated and compared with those by other popular and reported methods. Furthermore, the confirmation on the independent predicting set exhibited that the predicted bioactivities were well consistent with the experimental values. The important potential application of the present model is to be extended to help search active fractions of other HMs.