Allogenic grafted tissues are subjected to biodegradation and replaced by the regenerate. To minimize the immune response and improve the rebuilding of tissues there was developed a technology to treat tissues with a cells elimination and dosed out extraction of proteoglycanes (Alloplant. With aim to clarify the role of macrophages in the tissues regeneration resulting implantation the biomaterials 112 rats were injected the allogenic and xenogenic (rabbit's) pulverized biomaterials in the form of suspension. Injections were performed subcutaneously into the animals' back by the base of the tail. The control group (14 rats) were injected a physiologic saline. Animals were killed by ether inhalation on day 2, 4, 7, 14, 30, 90 and 180 and tissue sections were studied by light and electron microscopy. The study showed the key role of the macrophages in resorption of the allogenic biomaterial and formation of the newly-formed tissue. Implantation of the biomaterial induced activity a great number of the mature macrophages, which completely lysed and resorbed the biomaterial particles. Expression TNFalpha was significantly higher whereas expression TGF-beta1 was significantly lower. With xenogenic biomaterial implantation there were less macrophages, their activity was restricted. Macrophages containing large vacuoles with an active endo- and exocytosis were revealed in the allogenic biomaterial implantation and were named 'matrix-forming macrophages'. We may suppose that these macrophages synthesize (or re-synthesize) proteoglycan component of the newly-formed collagen fibers. There was put forward a hypothesis about the two component mechanism of the collagen fibers formation.
The oxidation of N acetyl and N benzoylanabasine with the tert butyl hydroperoxide (TBHP)-МoCl 5 system or МCРBA proceeds selectively at the nitrogen atom of the pyridine ring. The oxidation of N methylanabasine under similar conditions gives a mixture of stereo isomeric N oxides at the piperidine nitrogen atom, their ratio depending on the reagent used. The oxidation of anabasine by TBHP-МoCl 5 or МCРBA is accompanied by dehydrogenation and results in anabaseine N oxide. The reactions of anabasine and anabaseine pyridine N oxides with acetic anhydride were investigated. The substituted 1H 3 pyridin 2 ones were prepared. 2 pyridone, N acetylpiperidyl 2 pyridone, anabasein 3 one.Anabasine, 3 (2 piperidyl)pyridine (1), is the princi pal alkaloid of the Anabasis aphylla L. plant. 1 Anabasine hydrochloride is used as a means for giving up smoking; 2 the mechanism of its action includes binding to nicotine sensitive receptors. The anabasine base exhibits clear cut physiological activity. The action of this alkaloid is due to affection of the H cholinoreactive structures of various parts of the nervous system and violation of the mem brane permeability of cells, which results in a faulty course of redox processes in the organism. 3 Anabasine is an initial base in the synthesis of revers ible and irreversible choline esterase inhibitors, 4 in par ticular, phosphamide, 5 carbamide derivatives, 6 and a number of pharmacologically valuable compounds ob tained by reactions at the piperidine ring nitrogen atom. 7,8 Anabasine derivatives containing bulky acyl and alkyl sub stituents at the piperidine ring nitrogen atom exert an antinicotinic action, 9 and its hydrogenated derivatives ex hibit analgesic activities. 10 Thus, targeted synthetic transformations of anabasine may produce effective analogues with other types of physi ological activities.This paper describes a study of the oxidation of ana basine (1) and its N acetyl (2), N benzoyl (3) and N methyl (4) derivatives on treatment with tert butyl hydroperoxide (TBHP) and МCРBA and some transfor mations of the N oxides thus formed. Results and DiscussionPreviously, 11 we demonstrated that anabasine oxida tion with hydrogen peroxide in acetic acid is accompa nied by cleavage of the piperidine ring. No N oxidation of anabasine or its derivatives 2-4 by other reagents has yet been carried out. We found that refluxing of anabasine (1) in the presence of the TBHP-MoCl 5 system in benzene with water removal gives crystalline anabaseine N oxide (5) in 54% yield (Scheme 1). Thus, the hydroperoxide serves as a dehydrogenating agent. The oxidation of N acetyl (2) or N benzoylanabasine (3) under the ac tion of TBHP-MoCl 5 affords individual N acetyl and N benzoylanabasine pyridine N oxides 6 and 7 in 79 and 89% yields, respectively. It should be emphasized that previously, this reagent has been successfully used for N oxidation of diverse pyridine derivatives. 12-14 The use of VO(acac) 2 as the catalyst proved inefficient. The at tempted N oxidation of anabasine derivatives 2 and ...
Aim. To evaluate morphological skin changes of the experimental animals after intradermal injection of collagenous medication. Methods. The histological and histochemical methods (staining with hematoxylin and eosin, by Van-Gieson, Mallory and Foot method) were used to study the skin of mature female rats in the area of intradermal injection of collagen preparation «Kollost» by using mesotherapy method in 2, 4, 21 and 37 days. Murine skin was compared between experimental and control groups, in which the rats had solution of dextrose (glucose) injected intradermally. Results. On days 2-4 after the injection, inflammatory reaction was weak in the form of cellular infiltration along the needle stick. Numerous macrophages resorbing fibrous elements of the medication were determined in the injection zone. On days 7-14 fibroblasts proliferation, occurrence of argyrophilic thin newly-formed collagenous fibres and significant content of glycosaminoglycanes in the granulation tissue were revealed. By the 21-st day of the experiment following the injection, the dermal plate of the skin had become more dense due to the formation of thicker collagenous bundles in regeneration zones. When impregnated by silver nitrate they became yellow-brown that was indicative of fibre maturity. On day 37, the collagen fibers of the injected preparation in the injection zone were not detected in free unsubstituted form. The skin had a typical structure. The signs of stimulation of regeneration processes were not revealed in the skin of rats from the control group following the glucose solution injection. Conclusion. The collagenous preparation did not cause any pronounced inflammatory processes in the skin following intradermal injection to mature female rats; the fibrous structures of «Kollost» are resorbed by macrophages and substituted by the collagenous fibres integrating into the tissues; the processes are accompanied by stimulation of proliferation of structural elements of the skin connective tissue.
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