Structure-Activity Relationship Study of Majusculamide D: Overcoming Metabolic Instability and Severe Toxicity with a Fluoro Analogue.

Majusculamide D, isolated from the marine cyanobacterium , is an anticancer lipopentapeptide consisting of fatty acid, tripeptide, and pyrrolyl proline moieties. In this work, by utilizing a convergent synthetic approach, late-stage modification, and bioisostere strategy, 26 majusculamide D analogues were synthesized, and two ( and ) demonstrated IC values < 1 nM against PANC-1 cancer cells. The results summarized a preliminary structure-activity relationship mainly at the C23, C4, C34, and C10 sites.

Vitexicarpin suppresses malignant progression of colorectal cancer through affecting c-Myc ubiquitination by targeting IMPDH2.

Background: Colorectal cancer (CRC) is the second most common cause of cancer-related mortality and is characterised by extensive invasive and metastatic potential. Previous studies have shown that vitexicarpin extracted from the fruits of Vitex rotundifolia can impede tumour progression. However, the molecular mechanisms involved in CRC treatment are still not fully established.

Anti-angiogenesis in colorectal cancer therapy.

The morbidity of colorectal cancer (CRC) has risen to third place among malignant tumors worldwide. In addition, CRC is a common cancer in China whose incidence increases annually. Angiogenesis plays an important role in the development of tumors because it can bring the nutrients that cancer cells need and take away metabolic waste.

Probe Synthesis Reveals Eukaryotic Translation Elongation Factor 1 Alpha 1 as the Anti-Pancreatic Cancer Target of BE-43547A.

The natural product, BE-43547A , decreases pancreatic cancer cell stemness. However, its anticancer molecular mechanisms have not been fully established. Based on structure-activity relationships of BE-43547A , we synthesized a probe and investigated its potential targets using an in situ click reaction.

Cooccurrence of pH-sensitive shifting blue and immobile green triple surface-state fluorescence in ultrasmall super body-centered cubic carbon quantum dots.

Carbon quantum dots are widely used in various fields owing to excellent optical properties and outstanding biocompatibility. We synthesize rare super body-centered cubic (C) structured carbon quantum dots by using cheap source materials and simple preparation method. They exhibit one shifting blue emission band and two close immobile green bands.

Resonant defect recombination-localized surface plasmon energy transfer and exciton dominated fluorescence in ZnO-Au-ZnO multi-interfaced heteronanocrystals.

The semiconductor-metal heteronanocrystals (HNCs) that possess a perfect epitaxial interface can accommodate novel and interesting physical phenomena owing to the strong interaction and coupling between the semiconductor excitons and metal plasmons at the interface. Here, we fabricate the pyramidal ZnO-Au HNCs and study their unique photophysical properties. Several Au nanospheres are perfectly epitaxially bound with a single ZnO NC owing to the small lattice mismatch between them and there are also ZnO-Au-ZnO sandwiched HNCs.

Influence of crystallization temperature on fluorescence of n-diamond quantum dots.

Nanodiamonds are popular biological labels because of their superior mechanical and optical properties. Their surfaces bridging the core and surrounding medium play a key role in determining their bio-linkage and photophysical properties. n-diamond is a mysterious carbon allotrope whose crystal structure remains debated.

ACT001, a novel PAI-1 inhibitor, exerts synergistic effects in combination with cisplatin by inhibiting PI3K/AKT pathway in glioma.

PAI-1 plays significant roles in cancer occurrence, relapse and multidrug resistance and is highly expressed in tumours. ACT001, which is currently in phase I clinical trials for the treatment of glioblastoma (GBM). However, the detailed molecular mechanism of ACT001 is still unclear.

Joint bioinformatics analysis of underlying potential functions of hsa-let-7b-5p and core genes in human glioma.

Background: Glioma accounts for a large proportion of cancer, and an effective treatment for this disease is still lacking because of the absence of specific driver molecules. Current challenges in the treatment of glioma are the accurate and timely diagnosis of brain glioma and targeted treatment plans. To investigate the diagnostic biomarkers and prospective role of miRNAs in the tumorigenesis and progression of glioma, we analyzed the expression of miRNAs and key genes in glioma based on The Cancer Genome Atlas database.

Pharmacokinetics, tissue distribution and excretion of ACT001 in Sprague-Dawley rats and metabolism of ACT001.

This study investigated pharmacokinetics, tissue distribution and excretion of ACT001 in Sprague-Dawley rats. Stability study and metabolism study of ACT001 are conducted. The absolute bioavailability of ACT001 is 50.

Online solid phase extraction and liquid chromatography-mass spectrometric determination of nucleoside drugs in plasma.

The bioanalysis and especially the sample preparation of nucleoside drugs in complex media, such as human plasma, has been challenging due to the high polarity and high solubility of these drugs in water. Online solid phase extraction (SPE) offers significant advantages, such as automation and timesaving. Thus, several types of SPE columns have been developed for compounds with different polarities.

Syntheses and Biological Evaluation of Costunolide, Parthenolide, and Their Fluorinated Analogues.

Inspired by the biosynthesis of sesquiterpene lactones (SLs), herein we report the asymmetric total synthesis of the germacrane ring (24). The synthetic strategy features a selective aldol reaction between β,γ-unsaturated chiral sulfonylamide 15a and aldehyde 13, as well as the intramolecular α-alkylation of sulfone 21 to construct a 10-membered carbocylic ring. The key intermediate 24 can be used to prepare the natural products costunolide and parthenolide (PTL), which are the key precursors for transformation into other SLs.

Preparation of an anhydrous reverse micelle delivery system to enhance oral bioavailability and anti-diabetic efficacy of berberine.

To enhance oral bioavailability and anti-diabetic efficacy of berberine (BER), an anhydrous reverse micelle (ARM) delivery system was prepared through lyophilization of water-in-oil (W/O) emulsions. Using soy phosphatidylcholine as emulsifiers, BER-containing W/O emulsions were prepared and then lyophilized to form dry products which, upon addition of oil, formed clear ARMs containing amorphous BER nanoparticles. BER-loaded ARMs or free BER solutions were administered to streptozocin-induced diabetic mice.