Carboxylesterases play important roles in the metabolism of endogenous and foreign compounds, therefore, xenobiotic regulation carboxylesterase gene expression has both physiological pharmacological significance. We previously reported that liver microsomal esterase activity was significantly decreased rats treated with dexamethasone accompanied by a decrease immunoreactive proteins rat hydrolase A, B, C. The aim this study to determine whether suppressed these enzymes linked change mRNA...

Piscidin 1 (Pis-1) is a novel cytotoxic peptide with cationic α-helical structure that was isolated from the mast cells of hybrid striped bass [Silphaduang, U., and Noga, E. J. (2001) Nature 414, 268−269]. Pis-1 not selective for bacterial versus mammalian cells. In present study, to develop antibiotic peptides selectivity cells, we examined effect substituting two glycine residues, Gly8 Gly13, Ala or Pro on this peptide's biological activities. The cell decreased in following order: Gly→Pro...

Abstract The cell‐penetrating peptide Tat (48–60) (GRKKRRQRRRPPQ) derived from HIV‐1 protein showed potent antibacterial activity (MIC: 2–8 µ M ). To investigate the effect of dimerization analog, [Tat(W): GRKKRRQRRRPWQ‐NH 2 ], on antimicrobial and mechanism bactericidal action, its dimeric peptides, di‐Tat(W)‐C di‐Tat(W)‐K, were synthesized by a disulfide bond linkage lysine monomeric Tat(W), respectively. From viewpoint weight basis monomer concentration, these peptides displayed almost...

Pancreatic cancer remains one of the most difficult to treat human cancers despite recent advances in targeted therapy. Inhibition isoprenylcysteine carboxylmethyltransferase (ICMT), an enzyme that posttranslationally modifies a group proteins including several small GTPases, suppresses proliferation some cells. However, efficacy ICMT inhibition on pancreatic has not been evaluated. In this study, we have evaluated panel cell lines and identified those are sensitive inhibition. these cells,...

Background: Phenotypic traits are crucial for studying biological systems. Tree shrews widely used in environmental adaptation research due to their genetic diversity and phenotypic polymorphism. The measurement of its physical indicators skull provides a new perspective exploring the adaptive characteristics different tree shrew populations. Methods: To elucidate (Tupaia belangeri) relationship with factors, present study measured body shape 134 individuals across 12 regions. Result:...

Abstract Arenicin‐1 (AR‐1) is a novel antimicrobial peptide that was isolated from coelomocytes of the marine polychaeta lugworm Arenicola marina and shown to contain single disulfide bond between Cys3 Cys20, forming an 18‐residue ring [Ovchinnikova, T. V. et al., FEBS Lett 2004, 577, 209–214]. To determine role this bond, we synthesized AR‐1 (RWCVYAYVRVRGVLVRYRRCW) its linear derivative, arenicin‐1‐S (AR‐1‐S: RWSVYAYVRVRGVLVRYRRSW). Activity assays revealed AR‐1‐S somewhat less active...

The cell penetrating peptide, penetratin (RQIKIWFQNRRMKWKK‐NH 2 ) showed potent antimicrobial activity (MIC: 0.5–4 μ m without any cytotoxicity against mammalian cells. This study investigated the effect of linking together two peptide chains on and cytolytic activities plausible mode bactericidal action. Two‐stranded was prepared by a simultaneous solid‐phase synthesis strands single lysine residue attached to solid support. markedly increased human erythrocytes NIH‐3T3 mouse fibroblast...

Abstract Pep‐1‐K (PK) is a good cell‐selective antimicrobial peptide designed from cell‐penetrating Pep‐1. To develop novel short peptides with higher cell selectivity and shorter length compared PK, several PK analogs were by the deletion, addition and/or substitution of amino acids. Among these analogs, PK‐12‐KKP (KKPWWKPWWPKWKK) showing sequence structure homology Trp/Pro‐rich natural peptide, indolicidin (IN), displayed 20‐fold as to IN. Circular dichroism analysis revealed that adopts...

The process of autophagy is situated at the intersection multiple cell signaling pathways, including metabolism, growth, and death, hence subject to forms regulation. We previously reported that inhibition isoprenylcysteine carboxylmethyltransferase (Icmt), which catalyzes final step in post-translational prenylation so-called CAAX proteins, results induction enhances death some cancer cells. In this study, using siRNA-mediated knockdown a group small GTPases are predicted Icmt substrates,...

Metformin has been extensively studied for its impact on cancer cell metabolism and anticancer potential. Despite evidence of significant reduction in occurrence diabetic patients taking metformin, phase II trials the agent have disappointing, quite possibly because lack molecular mechanism-based patient stratification. In an effort to identify cancers that are responsive we discovered mitochondria respiratory capacity reserve, which vary widely among cells, correlate strongly metformin...

To investigate the effect of Pro --> peptoid residue substitution on cell selectivity and mechanism antibacterial action Pro-containing beta-turn antimicrobial peptides, we synthesized tritrpticin-amide (TP, VRRFPWWWPFLRR-NH(2)) its residue-substituted peptides in which two residues at positions 5 9 are replaced with Nleu (Leu residue), Nphe (Phe or Nlys (Lys residue). Peptides (TPf) (TPl) retained activity but had significantly higher toxicity to mammalian cells. In contrast, (TPk)...

Abstract Recently, we designed a novel cell‐selective antimicrobial peptide (TPk) with intracellular mode of action from Pro → Nlys (Lys peptoid residue) substitution in noncell‐selective cathelicidin‐derived Trp/Pro‐rich peptide, tritrpticin‐amide (TP; VRRFPWWWPFLRR‐NH 2 ) ( Biochemistry 2006; 45: 13007–13017). In this study, to elucidate the effect on therapeutic index and other peptides develop short high cell selectivity/therapeutic index, synthesized Nlys‐substituted peptides, TPk, STPk...

FoxO proteins are important regulators in cellular metabolism and recognized to be nodes multiple signaling pathways, most notably those involving PI3K/AKT mTOR. primarily function as transcription factors, but recent study suggests that cytosolic FoxO1 participates the regulation of autophagy. In current study, we find indeed stimulates autophagy cancer cell lines, it regulates not only basal also induced by rapamycin response nutrient deprivation. These findings illustrate importance...

Anoectochilus roxburghii (Wall.) Lindl. polysaccharides (ARPs) have been reported to exhibit multiple pharmacological activities including anti-inflammatory and anti-hyperglycemia. This study aims investigate the effect of ARPs on cognitive dysfunction induced by high fat diet (HFD).Six-week-old male mice were treated with dietary supplementation for 14 weeks. The function was determined assessing changes in spatial learning memory ability, neurotrophic factors hippocampus, inflammatory...

Emerging evidence suggests that butyrate, a short-chain fatty acid, may have beneficial effects on obesity and its associated metabolic comorbidities, but the related molecular mechanism is largely unknown. This study aims to investigate role of butyrate in diet-induced disorders relevant regulatory mechanisms. Here, dietary supplementation with Sodium (NaB) was carried out mice fed high-fat diet (HFD) or chow diet. At week 14, HFD displayed an obese phenotype down-regulated expression...

Veratrilla baillonii Franch is an important Chinese medicinal herb for treating liver-related diseases, which has been over-collected in the recent decades. However, effective conservation and related population genetic study hindered because of lack genome sequences markers natural population. We have conducted RNA-seq on V. baillonii. performed de novo assembly these data to characterize transcriptome, resulting 133,019 contigs with size >200 bp. These were annotated using NCBI...

The 16 EphA and EphB receptors represent the largest family of receptor tyrosine kinases, their interactions with 9 ephrin-A ephrin-B ligands initiate bidirectional signals controlling many physiological pathological processes. Most occur between ephrins same class, only EphA4 can bind all A B ephrins. To understand structural dynamic principles that enable Eph to utilize jellyroll β-sandwich fold ephrins, VAPB-MSP domain, peptides small molecules, we have used crystallography, NMR molecular...

An important objective of evolutionary biology has always been to grasp the and genetic processes that contribute speciation. The present work provides first detailed account physiological adaptation changing environmental temperatures as well reasons causing intraspecific divergence in

Pneumonia remains the leading cause of death among children aged 1-59 months. The early prediction poor outcomes (PO) is critical concern. This study aimed to explore risk factors relating PO in severe community-acquired pneumonia (SCAP) and build a PO-predictive nomogram model for with SCAP.We retrospectively identified 300 Chinese pediatric patients diagnosed SCAP who were hospitalized Affiliated Hospital Southwest Medical University from August 1, 2018, October 31, 2021. Children divided...

Morphological characteristics are closely related to habitat characteristics; differences drive morphological differentiation, resulting in intraspecific and interspecific differences. In the present study, it was shown that body mass length Eothenomys miletus from five regions: (Dali (DL), Jianchuan (JC), Lijiang (LJ), Xianggelila (XGLL) Deqin (DQ)) of Hengduan Mountain, showed differentiation bone indices. The sternum E. JC is smaller than XGLL, lumbar vertebrae XGLL DQ. other trunk bones...