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Poor aqueous solubility and bioavailability limit the translation of new drug candidates into clinical applications. Nanocrystal formulations offer a promising approach for improving the dissolution rate and saturation solubility. These formulations are applicable for various routes of administration, with each presenting unique opportunities and challenges posed by the physiological barriers.

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Background: Oxidative stress is strongly linked to neurodegeneration through the activation of c-Abl kinase, which arrests α-synuclein proteolysis by interacting with parkin interacting substrate (PARIS) and aminoacyl tRNA synthetase complex-interacting multifunctional protein 2 (AIMP2). This activation, triggered by ataxia-telangiectasia mutated (ATM) kinase, leads to dopaminergic neuron loss and α-synuclein aggregation, a critical pathophysiological aspect of Parkinson's disease (PD). To halt PD progression, pharmacological inhibition of c-Abl kinase is essential.

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The surge in plastic production has spurred a global crisis as plastic pollution intensifies, with microplastics and nanoplastics emerging as notable environmental threats. Due to their miniature size, these particles are ubiquitous across ecosystems and pose severe hazards as they are ingested and bioaccumulate within organisms. Although global plastic production has reached an alarming 400.

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Macrocyclic Diterpenoids from Possessing Activity Towards Autophagic Flux.

Int J Mol Sci

December 2024

State Key Laboratory of Functions and Applications of Medicinal Plants & College of Pharmacy, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang 550014, China.

Euphjatrophanes H-L (-), four new jatrophane-type and one new lathyrane-type diterpenoid, were isolated from , along with eight known diterpenoids (-). Their structures were established on the basis of extensive spectroscopic analysis and X-ray crystallographic experiments. All compounds were subjected to bioactivity evaluation using flow cytometry in autophagic flux assays with HM mCherry-GFP-LC3 cells, the human microglia cells which stably expressed the tandem monomeric mCherry-GFP-tagged LC3.

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This study aimed to investigate β-Caryophyllene (BCA) pharmacokinetics as well as the potential antitumor activity and mechanism of action of BCA and eugenol (EU), alone or in combination, in U87 glioblastoma (GB) cells. The BCA pharmacokinetic was studied by evaluating its concentration profiles in rat blood and cerebrospinal fluid after oral and intravenous administration. EU and BCA antitumor mechanisms were assessed by comparing their effects in U87 GB cells and non-tumoral HMC3 cells.

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