Hyperelodiones A-C, monoterpenoid polyprenylated acylphoroglucinols from Hypericum elodeoides, induce cancer cells apoptosis by targeting RXRα.

Hyperelodiones A-C, three undescribed monoterpenoid polyprenylated acylphloroglucinols possessing 6/6/6 fused tricyclic core, were isolated from Hypericum elodeoides Choisy. Their gross structures were elucidated by HRESIMS and NMR data. The absolute configurations of hyperelodiones A-C were assigned by their calculated and compared electronic circular dichroism (ECD) spectra combined with their common biosynthetic origin. A fluorescence quenching assay suggested that hyperelodiones A-C could bind to RXRα-LBD, whereas hyperelodione C showed the strongest interaction with a KD of 12.81 μΜ. In addition, hyperelodiones A-C dose-dependently inhibited RXRα transactivation and the growth of HeLa and MCF-7 cells. Among them, hyperelodione C showed the most potent inhibitory activities and dose-dependent PARP cleavage. Molecular docking results suggested that hyperelodione C showed a different interaction mode compared with hyperelodione A and hyperelodione B. Thus, hyperelodione C can be considered as a promising lead compound for cancer therapy, which can bind to RXRα-LBD and induce HeLa and MCF-7 cell apoptosis

The observations on Polar Stratospheric Clouds at Zhongshan Station, Antarctica

A lidar system (694 nm) was used to measure the stratospheric aerosol layer at Zhongshan Station (69°22'S, 76°22'E) in 1993. A total of 53 sets of lidar data presented in this paper were obtained over a period of 224 days between March 27 and November 5, 1993. The average vertical profiles of stratospheric aerosol backscattering ratio and the integrated backscatter coefficient over the 12 km - 30 km altitude range were reversed from the return signal of lidar. The results of observations show that the stratospheric aerosol content more noticeable enhanced in 1993 than that in 1990 due to Mt. Pinatubo eruption in Philippines in June of 1991. Polar Stratospheric Clouds (PSCs) were observed from late May until early August. The vertical profiles of stratospheric aerosol backscattering ratio at Antarctica in 1993 show a clear double-layer structure. One layer is at an altitude of about 12 km, the other is at an altitude of about 25 km . The upper layer is varied with season

Dgcr8 deletion in the primitive heart uncovered novel microRNA regulating the balance of cardiac-vascular gene program

Abstract Primitive mammalian heart transforms from a single tube to a four-chambered muscular organ during a short developmental window. We found that knocking out global microRNA by deleting Dgcr8 microprocessor in Mesp1 cardiovascular progenitor cells lead to the formation of extremely dilated and enlarged heart due to defective cardiomyocyte (CM) differentiation. Transcriptome analysis revealed unusual upregulation of vascular gene expression in Dgcr8 cKO hearts. Single cell RNA sequencing study further confirmed the increase of angiogenesis genes in single Dgcr8 cKO CM. We also performed global microRNA profiling of E9.5 heart for the first time, and identified that miR-541 was transiently highly expressed in E9.5 hearts. Interestingly, introducing miR-541 back into microRNA-free CMs partially rescued their defects, downregulated angiogenesis genes and significantly upregulated cardiac genes. Moreover, miR-541 can target Ctgf and inhibit endothelial function. Our results suggest that microRNAs are required to suppress abnormal angiogenesis gene program to maintain CM differentiation

Potential allelopathic azaphilones produced by the endophytic <i>Chaetomium globosum</i> TY1 inhabited in <i>Ginkgo biloba</i> using the one strain−many compounds method

<p>On the basis of the one strain−many compounds strategy, seven azaphilones, including Chaetomugilin A (<b>1</b>), D (<b>2</b>), S (<b>3</b>), I (<b>4</b>), J (<b>5</b>), Q (<b>6</b>) and O (<b>7</b>), were isolated from the endophytic <i>Chaetomium globosum</i> TY1. Their structures were identified by NMR and HRESIMS spectrometry data. All azaphilones were evaluated for plant growth regulation using eight species of herbaceous plant seeds seedling growth bioassay, which showed the plant growth influence of the seedling. Among these compounds tested, Chaetomugilin O (<b>7</b>) with tetrahydrofuran exhibited higher response index and lower IC₅₀ values than positive control glyphosate, a broad-spectrum systemic herbicide. <b>1</b>–<b>3</b> also showed better or similar inhibit activity to glyphosate. The structure−allelopathic activity relationship analysis of these isolated azaphilones indicates that both tetrahydrofuran and tetrahydrofuran combine with lactones ring groups give potent inhibition of seedling growth. Chaetomugilin O and Chaetomugilin A, D, S could be used to develop natural eco-friendly herbicides.</p