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Overexpression or activation of Yes‐associated protein (YAP) is common in cancer cells. Thus, targeting YAP may be a strategy for cancer therapy. Licochalcone A (LicA) is a primary active compound of licorice root and is known to have medicinal effects, such as antioxidant, antibacterial, antiviral, and anticancer effects. However, the anticancer pharmacological mechanism of LicA has not been investigated in cholangiocarcinoma. In this study, we investigated the antiproliferative effect of LicA and the underlying molecular mechanism in HCCC‐9810 and RBE human cholangiocarcinoma cells. Our experiments indicated that LicA suppressed the growth of cholangiocarcinoma cells through inactivation of the Hippo pathway. Pescadillo ribosomal biogenesis factor 1 (PES1) was notably upregulated and related to carcinogenesis. We also found that LicA suppressed the expression and nuclear localization of PES1, which was associated with the inhibition of YAP expression and transcriptional activity. [ABSTRACT FROM AUTHOR]

Plant vacuolar Na+/H+ antiporter genes play significant roles in salt tolerance. However, the roles of the chrysanthemum vacuolar Na+/H+ antiporter genes in salt stress response remain obscure. In this study, we isolated and characterized a novel vacuolar Na+/H+ antiporter gene DgNHX1 from chrysanthemum. The DgNHX1 sequence contained 1920 bp with a complete open reading frame of 1533 bp encoding a putative protein of 510 amino acids with a predicted protein molecular weight of 56.3 kDa. DgNHX1 was predicted containing nine transmembrane domains. Its expression in the chrysanthemum was up-regulated by salt stress, but not by abscisic acid (ABA). To assess roles of DgNHX1 in plant salt stress responses, we performed gain-of-function experiment. The DgNHX1-overexpression tobacco plants showed significant salt tolerance than the wild type (WT). The transgenic lines exhibited more accumulation of Na+ and K+ under salt stress. These findings suggest that DgNHX1 plays a positive regulatory role in salt stress response. [ABSTRACT FROM AUTHOR]

Abstract  A Cys2/His2-type zinc finger protein gene, DgZFP, was isolated from chrysanthemum by rapid amplification of cDNA ends (RACE) approach. The DgZFP encodes a protein of 211 amino acids residues with a calculated molecular mass of 22.9 kDa and theoretical isoelectric point is 8.59. DgZFP contains two Cys2/His2-type zinc finger motifs, one nuclear localization domain, one Leu-rich domain, and one ethylene-responsive element-binding factor (ERF)-associated amphiphilic repression (EAR) domain. The transcript of DgZFP was enriched in flowers than in roots, stems, and leaves of the adult chrysanthemum plants. The gene expression was strongly induced by NaCl, drought and cold treatment, and weakly by ABA treatment in the seedlings. Subcellular localization revealed that DgZFP was localized preferentially distributed to nucleus. Overexpression of DgZFP improved salt tolerance and resulted in growth suppression in transgenic tobacco. We argued that DgZFP is a new member of the Cys2/His2-type zinc finger protein genes, and it maybe function as a regulator in response to salt stress in plants. [ABSTRACT FROM AUTHOR]

Cobalt-catalyzed enantioconvergent cross-coupling of C(sp 3 )-H bonds with in situ -generated sulfenate anions is achieved to access chiral sulfoxides, which are found in the structures of many biologically active agents. The more challenging aliphatic C-H bonds as well as sterically hindered substrates containing tertiary C-H bonds could also be tolerated well. Mechanistic studies indicate that the transformation could undergo a Co II S(O)R-mediated single-electron transfer with N -fluorocarboxamides, followed by a 1,5-hydrogen atom transfer and then a pivotal organocobalt(IV)-controlled enantioselective cross-coupling process. This novel asymmetric radical reaction for C-S bond construction could open a new door for the synthesis of sulfur-centered chiral compounds.

We herein report a copper-catalyzed formal [5 + 2] aza-annulation of N -fluorosulfonamides and 1,3-dienes/1,3-enynes for synthesis of structurally diverse alkene/alkyne-containing azepanes. The reaction features selective functionalization of distal unactivated C(sp 3 )-H bonds and a broad substrate scope, thus allowing the late-stage modification of pharmaceuticals and natural products. A radical mechanism involving 1,5-hydrogen atom transfer of N-radicals, facile coupling of alkyl radicals with 1,3-dienes/1,3-enynes, and the construction of azepane motifs via C-N bond formation is proposed.