Palladium-Catalyzed Synthesis of Indanone via C-H Annulation Reaction of Aldehydes with Norbornenes.

A novel methodology for the synthesis of indanone derivates has been developed. The palladium-catalyzed annulation reaction of o-bromobenzaldehydes with norbornene derivatives is achieved through extremely concise reaction processes. The indanone skeleton was established directly via C-H activation of the aldehyde group under a mild reaction condition. This method is simple and practical, which simplified the traditional synthesis method for the rapid construction of indanone.

Palladium-Catalyzed Direct Esterification via C-H Bond Activation of Aldehydes.

A concise and highly efficient synthesis method of direct esterification of aldehydes via Pd-catalyzed C-H bond activation of aldehyde group has been developed. The strategy avoids the preoxidation step of aldehyde or use of condensing agents in ester synthesis, which is not only applicable to various alcohols but also suitable for the esterification of phenolics which are usually difficult to be esterified. The methodology has the significant advantages of broad substrate scope, mild reaction conditions, and nonrequirement of additional oxidants.

Three new diterpenoids from Euphorbia peplus.

Three new diterpenoids (1-3) (two abietane type diterpenoids and a paralianone type diterpenoid), together with four known compounds (4-7) were isolated from the whole plants of Euphorbia peplus. Their structures were elucidated through spectroscopic analysis and physicochemical characteristics. The cytotoxic activities of compounds 1-7 against five human tumour cell lines were evaluated, however, they were inactive at the concentration of 40 µM. The compound 3 enhanced lysosomal biogenesis with Lyso Tracker staining intensity of 132.6%.

Harpertrioate A, an A,B,D-seco-Limonoid with Promising Biological Activity against Alzheimer's Disease from Twigs of Harrisonia perforata (Blanco) Merr.

Harpertrioate A (1), an A,B,D-seco-limonoid with a rearranged ring B incorporating exocyclic C-30, was isolated from the EtOAc extract of Harrisonia perforata twigs. Its structure, including absolute configurations, was determined on the basis of spectroscopic data and X-ray crystallography. This compound exhibited biological activities against Alzheimer's disease by reducing Aß42 and Aß40 production and shifting APP processing toward nonamyloidogenic pathway. The effect of 1 on the Aß production was comparable to that of gemfibrozil.

Stemtuberolines A-G, new alkaloids from Stemona tuberosa and their anti-TMV activity.

Three new tuberostemoamide-type alkaloids, stemtuberolines A-C (1-3), four new stenine-type alkaloids, stemtuberolines D-G (4-7), together with five known Stemona alkaloids (8-12), were isolated from the roots of Stemona tuberosa. Their structures were elucidated on the basis of comprehensive spectroscopic data analysis. Stemtuberoline C (3) exhibited significant anti-TMV activity with an inhibition rate of 60.48% at the concentration of 50 µg/mL, while that of ningnamycin, the positive control, was 52.89%.

Acoapetaludines A-K, C20 and C19-diterpenoid alkaloids from the whole plants of Aconitum apetalum (Huth) B.Fedtsch.

A C20-diterpenoid alkaloid with an unprecedented carbon skeleton, acoapetaludine A, together with ten undescribed aconitine-type C19-diterpenoid alkaloids, acoapetaludines B-K, were isolated from the whole plants of Aconitum apetalum (Huth) B. Fedtsch. (Ranunculaceae). The structures were elucidated based on a comprehensive spectroscopic data analysis. The absolute configuration of acoapetaludine A was determined by quantum ECD calculation. Acoapetaludines D and E exhibited weak anti-Helicobacter pylori activity at a minimum inhibitory concentration (MIC) of 100 and 50 µg/mL, respectively.

Chemical composition and in vitro digestibility of corn stover during field exposure and their fermentation characteristics of silage prepared with microbial additives.

OBJECTIVE: To effectively use corn stover resources as animal feed, we explored the chemical composition and in vitro digestibility of corn stover during field exposure and the fermentation characteristics of silage prepared with lactic acid bacteria (LAB) and cellulase. METHODS: Corn ears including the cobs and shucks were harvested at the ripe stage. The corn stover was exposed in the field under natural weather conditions. Silages were prepared after 0, 2, 4, 7, 15, 30, and 60 d of exposure. Corn stover was chopped into approximately 1-2 cm lengths and then packed into 5 liter plastic silos. The ensiling density was 550.1±20.0 g/L of fresh matter, and the silos were kept at room temperature (10-25°C). Silage treatments were designed as follows: without additives (control), with LAB, with cellulase, and with LAB+cellulase. After 45 d of fermentation, the silos were opened for chemical composition, fermentation quality and in vitro digestion analyses. RESULTS: After harvest, corn stover contained 78.19% moisture, 9.01% crude protein (CP) and 64.54% neutral detergent fiber (NDF) on a dry matter (DM) basis. During field exposure, the DM, NDF, and acid detergent fiber (ADF) contents of corn stover increased, whereas the CP and water-soluble carbohydrate contents and in vitro digestibility of the DM and CP decreased (p<0.05). Compared to the control silage, cellulase-treated silage had lower (p<0.05) NDF and ADF contents. The pH values were lower in silage treated with LAB, cellulase, or LAB+cellulase, and lactic acid contents were higher (p<0.05) than those of the control. Silage treated with cellulase or LAB+cellulase improved (p<0.05) the in vitro DM digestibility (IVDMD) compared to that of the control or LAB-treated silage. CONCLUSION: Corn stover silage should be prepared using fresh materials since stover nutrients are lost during field exposure, and LAB and cellulase can improve silage fermentation and IVDMD.

Fine Mapping and Candidate Gene Prediction for White Immature Fruit Skin in Cucumber (Cucumis sativus L.).

In this study, a single recessive gene (designated w0) was identified to control the white immature fruit color. Genetic mapping with simple sequence repeats (SSR) markers located the w0 gene in the distal region of cucumber chromosome 3 (Chr.3). Fine mapping was then conducted using the method of draft genome scaffold-assisted chromosome walking with 7304 F2 individuals, which allowed for the assignment of the gene locus to a 100.3 kb genomic DNA region with two flanking markers, Q138 and Q193. Thirteen candidate genes were predicted in the 100.3 kb region. Quantitative real-time polymerase chain reaction (qRT-PCR) analysis showed that the expression of the Csa3G904140 gene, which encodes a two-component response regulator-like protein, was much higher in the immature fruit skin of the green parental line (Q1) than in the white parental line (H4). A coding sequence analysis suggested that a single-base insertion occurred at the ninth exon, resulting in a frameshift mutation in Csa3G904140 of H4, and the mutation was consistent with the phenotype in 17 green/white germplasms. Therefore, Csa3G904140 was taken as the likely candidate gene controlling the immature fruit color of cultivated cucumber. This study will contribute to the cloning of candidate genes and the development of white cucumber cultivars using marker-assisted breeding.

Seven new anthranilamide derivatives from Aconitum apetalum.

Seven new anthranilamide derivatives, acoapetalines A-G (1-7), including one new naturally occurring compound (7), together with six known ones (8-13) were isolated from the whole plants of Aconitum apetalum. Their structures were established on the basis of extensive spectroscopic analyses (IR, UV, HRESIMS, 1D and 2D NMR). All compounds were evaluated for their anti-tobacco mosaic virus (anti-TMV) activities. The results showed that compound 10 exhibited significant anti-TMV activity with an inhibition rate of 67.57% (100 µg/mL), which was higher than that of ningnamycin (52.89%).

Transcriptome Analysis Reveals Candidate Genes Associated with Leaf Etiolation of a Cytoplasmic Male Sterility Line in Chinese Cabbage (Brassica Rapa L. ssp. Pekinensis).

Cytoplasmic male sterility (CMS) is universally utilized in cruciferous vegetables. However, the Chinese cabbage hau CMS lines, obtained by interspecific hybridization and multiple backcrosses of the Brassica juncea (B. juncea) CMS line and Chinese cabbage, show obvious leaf etiolation, and the molecular mechanism of etiolation remains elusive. Here, the ultrastructural and phenotypic features of leaves from the Chinese cabbage CMS line 1409A and maintainer line 1409B are analyzed. The results show that chloroplasts of 1409A exhibit abnormal morphology and distribution. Next, RNA-sequencing (RNA-Seq) is used to identify 485 differentially expressed genes (DEGs) between 1409A and 1409B, and 189 up-regulated genes and 296 down-regulated genes are found. Genes that affect chloroplasts development, such as GLK1 and GLK2, and chlorophyll biosynthesis, such as PORB, are included in the down-regulated DEGs. Quantitative real-time PCR (qRT-PCR) analysis validate that the expression levels of these genes are significantly lower in 1409A than in 1409B. Taken together, these results demonstrate that leaf etiolation is markedly affected by chloroplast development and pigment biosynthesis. This study provides an effective foundation for research on the molecular mechanisms of leaf etiolation of the hau CMS line in Chinese cabbage (Brassica rapa L. ssp. pekinensis).

Mental health system in China: history, recent service reform and future challenges.

This paper summarizes the history of the development of Chinese mental health system; the current situation in the mental health field that China has to face in its effort to reform the system, including mental health burden, workforce and resources, as well as structural issues; the process of national mental health service reform, including how it was included into the national public health program, how it began as a training program and then became a treatment and intervention program, its unique training and capacity building model, and its outcomes and impacts; the barriers and challenges of the reform process; future suggestions for policy; and Chinese experiences as response to the international advocacy for the development of mental health.