The objective of this work was to investigate phytantriol-based liquid crystal (LC) gels including cubic (Q₂) and hexagonal (H₂) phase for ocular delivery of pilocarpine nitrate (PN) to treat glaucoma. The gels were produced by a vortex method and confirmed by crossed polarized light microscopy, small-angle X-ray scattering, and rheological measurements. Moreover, the release behaviors and permeation results of PN from the gels were estimated using in vitro studies. Finally, the anti-glaucoma effect of LC gels was evaluated by in vivo animal experiments. The inner structure of the gels was Pn3m-type Q₂ and H₂ phase, and both of them showed pseudoplastic fluid properties based on characterization techniques. In vitro release profiles suggested that PN could be sustainably released from LC gels within 48 h. Compared with eye drops, Q₂ and H₂ gel produces a 5.25-fold and 6.23-fold increase in the P_app value (p < .05), respectively, leading to a significant enhancement of corneal penetration. Furthermore, a good biocompatibility and longer residence time on precorneal for LC gels confirmed by in vivo animal experiment. Pharmacokinetic studies showed that LC gels could maintain PN concentration in aqueous humor for at least 12 h after administration and remarkably improve the bioavailability of drug. Additionally, in vivo pharmacodynamics studies indicated that LC gels had a more significant intraocular pressure-lowering and miotic effect compared to eye drops. These research findings hinted that LC gels would be a promising pharmaceutical strategy for ocular application to enhance the efficacy of anti-glaucoma.

01 Jun 2008·ApoptosisQ3 · BIOLOGY

A novel diquinolonium displays preclinical anti-cancer activity and induces caspase-independent cell death

Q3 · BIOLOGY

Article

Author: Tabitha Wood ; Robert A. Batey ; Rose Hurren ; Aaron D. Schimmer ; Reza Beheshti Zavareh ; Nazir Jamal ; Hans Messner ; Hong Chang ; Shadi Dalili ; David Rose

Quinolines are a class of chemical compounds with emerging anti-cancer properties. Here, we tested the activity of series of quinolines and quinoline-like molecules for anti-cancer activity and identified a novel diquinoline, 1-methyl-2-[3-(1-methyl-1,2-dihydroquinolin-2-yliden)prop-1-enyl]quinolinium iodide (Q(2)). Q(2 )induced cell death in leukemia, myeloma, and solid tumor cell lines with LD50s in the low to submicromolar range. Moreover, Q(2) induced cell death in primary acute myeloid leukemia (AML) cells preferentially over normal hematopoietic cells. In a mouse model of leukemia, Q(2) delayed tumor growth. Mechanistically, Q(2) induced cell death through caspase independent mechanisms. By electron microscopy, Q(2) increased cytoplasmic vacuolization and mitochondrial swelling. Potentially consistent with the induction of autophagic cell death, Q(2) treatment led to a punctate distribution of LC3 and increased MDC staining. Thus, Q(2) is a novel quinolinium with preclinical activity in malignancies such as leukemia and myeloma and warrants further investigation.

01 Apr 1950·Biochemical JournalQ3 · BIOLOGY

Some properties of specific cholinesterase with particular reference to the mechanism of inhibition by diethyl p-nitrophenyl thiophosphate (E 605) and analogues

Q3 · BIOLOGY

Article

Author: Aldridge, W. N.

Goat red cells were used as source of specific cholinesterase because the cells as well as serum of goat blood contain practically no pseudocholinesterase and the cholinesterase of goat red cells of the same animal seems to remain constant for months. p-Nitrophenyl diethyl thiophosphate (E 605), p-nitrophenyl diethyl phosphate (E 600), and diisopropyl fluophosphate (DFP) inhibit without any significant reversibility, while 8-quinolyl diethyl thiophosphate (Q₂) of N-mustard are partly reversible.The course of inhibition by E 605 or E 600 shows characteristics of a bimol. reaction while that of Q₂ of a monomol. reaction.Benzoylcholine is an inhibitor of specific cholinesterase.It was found that at a concentration of 1.0 × 10^-8 M E 600 a straight line is obtained and, since straight lines in a graph are obtained for bimol. reactions only when one of the reactants is in excess, it may be possible to put an upper limit on the molar concentration of enzyme.When the inhibitor is not more than 4 times the enzyme concentration the line will be curved, as can be shown by calculation, and since in a bimol. reaction there must be 1 mol. enzyme active center to 1 mol. inhibitor, the enzyme concentration can be estimated as not more than 2.5 × 10^-9 M.

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Indication	Highest Phase	Country/Location	Organization	Date
Prostatic Cancer	Preclinical	AU	UniQuest Pty Ltd.	28 Aug 2023

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