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Biomedical subjects

J Grochowski

Publications and source records attributed to J Grochowski.

At least 19 recordsLinked to original sources

Effects of a carane derivative local anesthetic on a phospholipid bilayer studied by molecular dynamics simulation.

Molecular dynamics (MD) simulations of two hydrated palmitoyloleoylphosphatidylcholine (POPC) bilayers each containing eight carane derivative (KP-23) local anesthetic (LA) molecules in neutral (POPC-LA) or protonated (POPC-LAH) forms were carried out to investigate the effect of KP-23 and its protonation on the bilayer. 3-ns trajectories were used for analyses. A pure POPC bilayer was employed as a reference system. In both POPC-LA and POPC-LAH systems a few KP-23 molecules intercalated into the bilayer and moved near the bilayer/water interface. They were located on the hydrophobic core side of the interface in the POPC-LA bilayer, but on the water phase side in the POPC-LAH bilayer. The order of the POPC chains was higher in the POPC-LA bilayer than in the pure POPC bilayer and was lower in the POPC-LAH bilayer. Interactions between polar groups of KP-23 and POPC or water were responsible for a lower hydration of POPC headgroups in POPC bilayers containing KP-23 than in the pure POPC bilayer. KP-23 molecules were found to form aggregates both in POPC-LA and POPC-LAH bilayers. Due to higher amphiphilicity of LAH, the LAH aggregate was more micelle-like and larger than the LA one. The results demonstrate the rapid timescales of the initial processes that take place at and near the bilayer interface as well as details of the atomic level interactions between local anesthetic and the lipid matrix of a cell membrane.

Anesthetics, Local↗

New spirans containing a 1,5-benzodithiepine system, derived from methylbenzenes. Conformational transmission

[structure: see text] A synthesis of three new spirans, derived from methylbenzenes, containing the 1,5-benzodithiepine system is reported. X-ray structure proved the identity of model monospiran 9. In the solid and liquid state, the conformation of the seven-membered ring is chair, and the five-membered ring has the envelope conformation. The effect of conformational transmission in spirans 9 and 10 was observed. The synthesis of trispirans from hexamethylbenzene using the proposed scheme is also possible.

Journal Article↗

[Ethylene glycol poisoning as a cause of chronic renal failure].

We showed some observations two Dialysis Centres concerning acute ethylene glycol poisoning and four cases of chronic renal failure progress. Renal biopsy at one patient and our clinical observations indicate for possibility of chronic renal failure development in some pts. We discussed hypotension of CRF development at those pts.

Adult↗

[Glycol ethylene poisoning as a cause of chronic renal failure].

There were shown some observations from two Dialysis Centres concerning acute Ethylene Glycol poisoning and four cases of chronic renal failure progress. The renal biopsy made at one patient and our clinical observations indicate for possibility of chronic renal failure development in some pts. There were discussed hypothesis of CRF development at these pts.

Adult↗

Structural investigation of the new potent DNA alkylator spiro(2H-1,3,2-benzodiazaphosphole-2,2',lambda 5 [1,3,5,2,4,6] triazatriphosphorine),4',4',6',6'-tetrakis(1-aziridinyl)-1,3,4',4',6', 6',-hexahydro.

The molecular structure of spiro(2H-1,3,2-benzodiazaphosphole-2,2',lambda 5 [1,3,5,2,4,6] triazatriphosphorine), 4',4',6',6'-tetrakis(1-aziridinyl)-1,3,4',4',6',6'-hexahydro (CAS 133586-94-4), a recently synthesized potent cytostatic, was determined using X-ray diffraction method. The substance crystallizes in P2(1)2(1)2(1) orthorhombic space group. The unit cell contains 8 formal molecules coupled into 4 pseudo-centrosymmetric dimers by double intermolecular hydrogen bonds. The compound revealed, besides previously determined long-term chemical stability and good water solubility, also radiation stability. In spite of having less aziridinyl groups than 1,3,5,2,4,6-triazatriphosphorine,2,2,4,4,6,6-hexakis (1-aziridinyl)-2,2,4,4,6,6-hexahydro (N3P3Az3, Az = aziridinyl, CAS 52-46-0; Myko 63) the compound is twice more cytostatically active. Hypotheses attributing high cytostatic activity to the existence of conjugated pi-electron systems in the molecule and dimeric structures are discussed.

Alkylating Agents↗

Synthesis and CLOGP correlation of imidooxy anticonvulsants.

Continuing structure-activity studies on the anticonvulsant activity of analogs of N-(benzyloxy)-2-azaspiro[4.4]nonane-1,3-dione (2a), which displayed anti-electroshock seizure (MES) activity and a protective index (TD50/ED50) of > 4.5 are reported. An in-depth analysis of this moiety was studied employing the Topliss structure activity and the Craig plot analytical approaches as well as a semiempirical method. CLOG P analysis was also applied to this series after experimentally determining the NOR fragment. All compounds were minimized and these physicochemical parameters correlated to anticonvulsant activity. Several interesting substituted benzyloxy compounds emerged from this study: the 2',4'-dichloro (2b), 4'-(trifluoromethyl) (2c), 2'-bromo (2d), 3'-chloro (2o), 2'-chloro (2r), 2'-fluoro (2p), and 3'-fluoro (2w) analogs, all of which had comparable, or better activity than the parent unsubstituted analog (2a). X-ray crystal analysis of the active 2a versus inactive N-benzyl-2-azaspiro[4.4]nonane-1,3-dione (10) is discussed.

Animals↗

Molecular structure and antiaggregating activity of the potent local anaesthetic (-)-4-[2-hydroxy-3-(N-isopropylamino)-propoxyimino]-cis-carane .

The molecular structure of (-)-4-[-2-hydroxy-3-(N-isopropylamino)- propoxyimino]-cis-carane (C16H30O2N2.HCl), a recently synthesized potent local anaesthetic, including the absolute configuration at 4 chirality centres was determined using X-ray diffraction method. The substance crystallizes in diastereoisomeric form in lowest symmetry (triclinic P1 space group). Determined intermolecular close contacts between chlorine atoms and nitrogen and hydroxyl oxygen are the main determinants of crystal packing. In the crystalline state nitrogen of the isopropylamine group has quaternary coordination. The influence of the title compound on blood platelets aggregation induced by adenosine diphosphate was studied. The results of parallel tests conducted for lidocaine and bupivacaine show that the antiaggregating activity of the title compound is much stronger. This property could be attributed to the monoterpene part of its molecule, in analogy to the observed cyclic adenosine monophosphate inhibitory action of forskolin (diterpene).

Adenosine Diphosphate↗

[Parasitic uveitis in children].

Seven children with an atypical parasitic uveitis were treated in the Department of Ophthalmology in Bialystok in the period 1985-1989. Parasitic background had been discovered in all the children: toxocara in 3, lambliasis in 2 and nematodiasis also in 2. Specific treatment achieved an improvement of the visual acuity and the inflammatory process abated.

Antinematodal Agents↗

[Function of the visual system after orbital surgery. Late observations].

Forty six persons with an orbital tumor were operated in the period of 1980-1988. A control examination performed in 39 persons did not show in 38 any characteristics of recurrence of the tumor; the motility of the eye ball was normal. In 29 persons the visual acuity of the eye at the side of the operated tumor was over 5/6.

Adolescent↗

Immunological reactivity in children with Wilms' tumor.

Cellular immune reactivity was investigated in 49 newly diagnosed children with Wilms' tumor and compared to age-matched control. The level of total T (T4 degrees) and B lymphocytes was normal while the relative number of T lymphocytes with high affinity receptors for sheep erythrocytes (T29 degrees) was significantly decreased in the patients studied. The lymphocyte response to PHA in vitro was diminished but PHA-induced lymphokine production was not altered. The depression of T29 degrees level and lymphocyte reactivity to PHA was associated with high grade tumor rather than with the clinical stage. Lymphocytes of 42-47% patients reacted with autochthonous and allogeneic KCl tumor extracts in the migration inhibition test and the degree of reactivity was related to the histological differentiation of the tumor.

B-Lymphocytes↗

CNS malformations in the Kraków region. I. Birth prevalence and seasonal incidence during 1979-1981.

The birth prevalence of CNS malformations in the region of Krakow from 1979 to 1981 was determined to be 1.26/1000 from records of all live- and still-birth deliveries. The frequency of anencephaly was 0.23/1,000; spina bifida and encephalocele, 0.70/1000; isolated hydrocephaly, 0.26/1,000; and other CNS anomalies, 0.06/1,000. The observed rates are below the median European level. Female preponderance was found among the probands with anencephaly, encephalomeningocele, and myelomeningocele. Cytogenetic examination of 35 newborns with CNS malformations documented normal karyotypes in all neonates. The analysis of seasonal distribution of proband's birthdate and of date of mother's last menstrual period showed no significant seasonal trend.

Cross-Sectional Studies↗

Identification of atypical calcium oxalate crystalluria following ethylene glycol ingestion.

A case of ethylene glycol poisoning was associated with heavy crystalluria unidentifiable by light microscopy. Extensive analysis utilizing scanning electron microscopy, x-ray fluorescence, and diffraction method revealed that the sediment contained calcium oxalate monohydrate in one crystallographic phase. Newest diffraction data for identification of the various forms of calcium oxalate, along with the photographs of the crystals by light and electron microscopy, are included. Fifty cases of ethylene glycol poisoning were reviewed to ascertain the most common form of calcium oxalate crystalluria. The search revealed scanty morphologic data associated with the calcium oxalate crystalluria; however, numerous forms were reported. It is concluded that calcium oxalate crystalluria following ethylene glycol ingestion may assume many forms, which should be recognized to facilitate the rapid diagnosis of ethylene glycol ingestion.

Adult↗

Blood serum immunoreactive gastrin level in infants with hypertrophic pyloric stenosis.

Blood serum immunoreactive gastrin level (IRG) was measured in infants with hypertrophic pyloric stenosis before and after corrective surgery and in a control group children of corresponding age. No significant difference in IRG level was found between the stenotic infants and the control group. In the stenotic infants IRG values were higher at the seventh day after than before the operation and significantly higher in those infants in whom gain of body weight was noted during that time as compared with the infants without gain of weight. These observations remain in agreement with the view that the main role of gastrin in infants is trophic action on the mucosa of the upper gastrointestinal tract.

Body Weight↗