scholarly journals Protein ruthenation and DNA alkylation: chlorambucil-functionalized RAPTA complexes and their anticancer activity

2015 ◽  
Vol 44 (8) ◽  
pp. 3614-3623 ◽  
Author(s):  
Alexey A. Nazarov ◽  
Samuel M. Meier ◽  
Olivier Zava ◽  
Yulia N. Nosova ◽  
Elena R. Milaeva ◽  
...  

The conjugation of chlorambucil to the RAPTA scaffold results in an anticancer active agent capable of cross-linking DNA and proteins.

1946 ◽  
Vol 19 (4) ◽  
pp. 900-914 ◽  
Author(s):  
John Rehner ◽  
Paul J. Flory

Abstract Experiments have been carried out to determine the chemical reactions that occur when Butyl rubber is vulcanized by quinone dioxime or related compounds. Observations have been made of the reactions of these substances with simple olefins, and of the effect of oxidizing agents on the dioxime-type of vulcanization of Butyl in solution. The theory is proposed that, in the vulcanization of Butyl by quinone dioxime or its esters, in presence of oxidizing agents, the active agent is p-dinitrosobenzene formed by oxidation of the dioxime. Chemical reactions are suggested for the subsequent cross-linking or vulcanizing steps, and the results of confirmatory experiments are presented. p-Dinitrosobenzene and other polynitroso compounds are active vulcanizing agents for Butyl, natural rubber, Buna-S, Buna-N, and Neoprene, and do not require the addition of an oxidizing agent. It is suggested that vulcanization of natural rubber by polynitro compounds involves their reduction to corresponding nitroso compounds as the first step, and that the nitroso group adds to rubber to produce cross-linkages.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 451 ◽  
Author(s):  
Ang ◽  
Darwis ◽  
Por ◽  
Yam

Curcuminoids have been long proven to possess antioxidant, anti-inflammatory and antibacterial properties which are crucial in their role as a pharmacological active agent. However, its poor solubility, high oxidative degradation, light sensitivity and poor bioavailability have been huge hurdles that need to be overcome for it to be administered as an oral or even a topical medication. In this present study, a complex coacervation microencapsulation approach was used to encapsulate the curcuminoids using both gelatin B and chitosan (at the optimum ratio of 30:1% w/w) for a more efficient drug delivery system. Curcuminoids microcapsules (CPM) were developed to be spherical in shape, discrete and free flowing with a reduced color staining effect. The thick wall of the CPM contributes directly to its integrity and stability. Cross-linking increases the density of polymers’ wall network, hence, further increasing the decomposition temperature of curcuminoids microcapsules. Microencapsulation demonstrated an increment in curcuminoids solubility, while chemical cross-linking allowed for sustained release of the drug from the microcapsules by lowering the swelling rate of the available polymer networks. Thus, the microcapsules complied with the zero order release kinetics with super case-II transport mechanism. On the basis of all that was discussed above, it can be safely concluded that CPM should be incorporated in delivery system of curcuminoid, especially in its topical delivery for controlled drug release purposes, for not only a more efficient drug delivery system design but also a more efficacious optimization of the pharmacological benefits of curcuminoids.


2012 ◽  
Vol 19 (1) ◽  
pp. 383-390
Author(s):  
Dhurairajan Senthilnathan ◽  
Anbarasan Kalaiselvan ◽  
Ponnambalam Venuvanalingam

1998 ◽  
Vol 79 (2) ◽  
pp. 264-266 ◽  
Author(s):  
J A Hartley ◽  
C C O’Hare ◽  
J Baumgart
Keyword(s):  

2018 ◽  
Vol 54 (22) ◽  
pp. 2788-2791 ◽  
Author(s):  
Wen Zhou ◽  
Mohammad Almeqdadi ◽  
Michael E. Xifaras ◽  
Imogen A. Riddell ◽  
Ömer H. Yilmaz ◽  
...  

The trans-DDP based phenanthridine Pt(ii) complex displays significant antitumor properties, with a different spectrum of activity than that of classic bifunctional cross-linking agents like cisplatin.


Author(s):  
D. James Morré ◽  
Charles E. Bracker ◽  
William J. VanDerWoude

Calcium ions in the concentration range 5-100 mM inhibit auxin-induced cell elongation and wall extensibility of plant stems. Inhibition of wall extensibility requires that the tissue be living; growth inhibition cannot be explained on the basis of cross-linking of carboxyl groups of cell wall uronides by calcium ions. In this study, ultrastructural evidence was sought for an interaction of calcium ions with some component other than the wall at the cell surface of soybean (Glycine max (L.) Merr.) hypocotyls.


Author(s):  
Ann M. Thomas ◽  
Virginia Shemeley

Those samples which swell rapidly when exposed to water are, at best, difficult to section for transmission electron microscopy. Some materials literally burst out of the embedding block with the first pass by the knife, and even the most rapid cutting cycle produces sections of limited value. Many ion exchange resins swell in water; some undergo irreversible structural changes when dried. We developed our embedding procedure to handle this type of sample, but it should be applicable to many materials that present similar sectioning difficulties.The purpose of our embedding procedure is to build up a cross-linking network throughout the sample, while it is in a water swollen state. Our procedure was suggested to us by the work of Rosenberg, where he mentioned the formation of a tridimensional structure by the polymerization of the GMA biproduct, triglycol dimethacrylate.


Author(s):  
John H. Luft

With information processing devices such as radio telescopes, microscopes or hi-fi systems, the quality of the output often is limited by distortion or noise introduced at the input stage of the device. This analogy can be extended usefully to specimen preparation for the electron microscope; fixation, which initiates the processing sequence, is the single most important step and, unfortunately, is the least well understood. Although there is an abundance of fixation mixtures recommended in the light microscopy literature, osmium tetroxide and glutaraldehyde are favored for electron microscopy. These fixatives react vigorously with proteins at the molecular level. There is clear evidence for the cross-linking of proteins both by osmium tetroxide and glutaraldehyde and cross-linking may be a necessary if not sufficient condition to define fixatives as a class.


Author(s):  
S.K. Aggarwal ◽  
J.M. Fadool

Cisplatin (CDDP) a potent antitumor agent suffers from severe toxic side effects with nephrotoxicity being the major dose-limiting factor, The primary mechanism of its action has been proposed to be through its cross-linking DNA strands. It has also been shown to inactivate various transport enzymes and induce hypocalcemia and hypomagnesemia that may be the underlying cause for some of its toxicities. The present is an effort to study its influence on the parathyroid gland for any hormonal changes that control calcium levels in the body.Male Swiss Wistar rats (Crl: (WI) BR) weighing 200-300 g and of 60 days in age were injected (ip) with cisplatin (7mg/kg in normal saline). The controls received saline injections only. The animals were injected (iv) with calcium (0.5 ml of 10% calcium gluconate/day) and were killed by decapitation on day 1 through 5. Trunk blood was collected in heparinized tubes.


Author(s):  
Richard D. Powell ◽  
James F. Hainfeld ◽  
Carol M. R. Halsey ◽  
David L. Spector ◽  
Shelley Kaurin ◽  
...  

Two new types of covalently linked, site-specific immunoprobes have been prepared using metal cluster labels, and used to stain components of cells. Combined fluorescein and 1.4 nm “Nanogold” labels were prepared by using the fluorescein-conjugated tris (aryl) phosphine ligand and the amino-substituted ligand in the synthesis of the Nanogold cluster. This cluster label was activated by reaction with a 60-fold excess of (sulfo-Succinimidyl-4-N-maleiniido-cyclohexane-l-carboxylate (sulfo-SMCC) at pH 7.5, separated from excess cross-linking reagent by gel filtration, and mixed in ten-fold excess with Goat Fab’ fragments against mouse IgG (obtained by reduction of F(ab’)2 fragments with 50 mM mercaptoethylamine hydrochloride). Labeled Fab’ fragments were isolated by gel filtration HPLC (Superose-12, Pharmacia). A combined Nanogold and Texas Red label was also prepared, using a Nanogold cluster derivatized with both and its protected analog: the cluster was reacted with an eight-fold excess of Texas Red sulfonyl chloride at pH 9.0, separated from excess Texas Red by gel filtration, then deprotected with HC1 in methanol to yield the amino-substituted label.


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