Synthesis,AM<Subscript>1</Subscript> calculation,and biological studies of thiopyran-4-one and their azine derivatives

Some novel N(1)-arylidene-N(2)-cis-2,6-diphenyltetrahydrothiopyran-4-one azine derivatives were synthesised and their antibacterial activity against Streptococcus faecalis, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus and antifungal activity against Candida-6, Candida-51, Aspergillus niger, and Aspergillus flavus were evaluated.     

Postpemphigus acanthomata: a sign of clinical activity?

Background Pemphigus is a group of vesiculobullous disorders in which the blisters usually heal with hyper- or hypopigmentation. The appearance of acanthomata at sites of previous blisters has been noted in some cases. Methods All cases of pemphigus admitted to the Madras Medical College hospitals during a 2-year period from March 1993 to March 1995 were taken into the study and screened for the presence of acanthomata. Results Fifty-two cases of pemphigus were identified, 47 of pemphigus vulgaris and five of pemphigus foliaceus; and of these 13 developed acanthomata when the blisters healed. Ten of these cases were of pemphigus vulgaris and three were of pemphigus foliaceus; biopsy of these lesions showed hyperkeratosis, acanthosis, papillomatosis, and intraepidermal clefting. Immunofluorescence carried out in two of these acanthomata also showed intercellular fluorescence. Conclusions The occurrence of acanthomata in healed lesions of pemphigus is not uncommon; because histopathologic and immunofluorescence evidence of disease activity is present, cases of this sort require careful follow-up.     

Crosslinked polyimide foams derived from poly(imidepropylene oxide) copolymers

A new route for the synthesis of high glass transition temperature, thermally stable polymer foams has been developed, using compositionally asymmetric microphase-separated block copolymers where the minor component (poly(propylene oxide)) is thermally labile and the major component (polyimide) is thermally stable. The minor component decomposes to low molecular weight species upon heating, and the decomposition products diffuse out of the film, leaving behind pores embedded in a matrix of the thermally stable component. In this study, the polyimide block was crosslinked with ethynyl functionalities to obtain a stable porous structure. The decomposition of the propylene oxide in the block copolymer was studied by thermogravimetric, dynamic mechanical and thermomechanical analyses. Mild conditions were required to avoid rapid depolymerization of the propylene oxide and plasticization of the polyimide matrix. The foams showed pore sizes with diameters up to a micrometer in size as well as the expected reduction in the mass density.     

Inhibition of interleukin-2 production by adherent cell factors from lepromatous leprosy patients.

Twenty-four hour supernatants (MoF) were obtained from monocyte rich 2 h adherent cells of 19 leprosy patients and four healthy contacts. MoF from borderline and lepromatous patients produced 52-61% inhibition of human interleukin-2 (IL-2) production by a PHA conditioned T cell line (Jurkat). Non-adherent cell supernatants and MoF from tuberculoid and healthy individuals had little effect on IL-2 production. The suppression effected by MoF was in the first 12 h of initiation of PHA stimulated Jurkat cell cultures. Suppressive MoF did not interfere with (1) IL-2 release, (2) IL-2 utilization by Con A-induced T cell blasts or (3) constitutive proliferation of Jurkat cells. Such MoF were released spontaneously from adherent cells of bacilliferous leprosy patients but required in vitro antigen triggering in long term treated lepromatous patients. It is possible that the unresponsiveness associated with lepromatous leprosy is related to the inhibition of IL-2 production by suppressive factors, thereby, preventing the further expansion of antigen reactive T cells.     

Hapten-specific responses to the phenyltrimethyl-amino hapten. I. Evidence for idiotype-anti-idiotype interactions in delayed-type hypersensitivity in mice

The delayed-type hypersensitivity (DTH) reaction to the phenyltrimethylamino (TMA) hapten in mice has been investigated. TMA-derivatized syngeneic spleen cells (TMA-SC) administered s.c. in several strains of mice consistently evoked DTH reactivity, as measured by footpad swelling after challenge with the diazonium salt of TMA. DTH could be induced by low levels of anti-idiotypic antisera (anti-Id) in lieu of antigen. The DTH reaction induced by either mode was hapten-specific, could be transferred into naive recipients by viable lymph node cells but not with serum from immune mice and was not influenced by cyclophoshamide pretreatment. Unlike TMA-SC which induced DTH in all of the strains of the mice tested, anti-Id induced DTH only in strains of the Igh-1e allotype. Positive DTH reactions were induced by anti-Id in the C57.Ige strain (H-2b, Igh-1e) but not in its allotype-congenic partner C57BL/6J (H-2b, Igh-1b). Interestingly this reaction could be suppressed if relatively high amounts of anti-Id were inoculated i.v. just prior to antigen challenge. In addition, the administration of anti-Id 1 h prior to antigen challenge in TMA-SC-sensitized mice significantly blocked the DTH reaction only in the Igh-1e strains. These results demonstrate that the induction and abrogation of TMA-specific DTH by anti-Id is linked to the IgCh locus.     

Cholecystokinin and neurotensin mRNAs are differentially expressed in subnuclei of the ventral tegmental area

Immunohistochemical studies of ventral tegmental area (VTA) neurons indicate that individual cells can contain dopamine as well as the neuropeptide neurotransmitters cholecystokinin (CCK) and neurotensin (NT). We have defined the distribution of the cells expressing the mRNAs encoding these two dopamine cotransmitter peptides in each of the subnuclei of the ventral tegmental area, and quantitated the extent of expression of each gene by using in situ hybridization methods. These studies reveal significant differences in the patterns of expression of each of these two genes within various subdivisions of the VTA. The rostral linear nucleus contained numerous CCK positive cells, some of which appeared to express preproCCK-mRNA at a very high level, but this nucleus contained relatively few NT-expressing cells. The parabrachialis pigmentosus contained numerous NT and CCK positive cells. The paranigralis and interfascicularis nuclei displayed positive CCK cells but with expression at only modest levels. NT cells were very few in these nuclei. The caudal linear nuclei contained the highest number of NT-expressing neurons and these cells expressed very high levels of NT mRNA. The selective distribution of these peptide genes within the VTA subnuclei may have specific consequences. Studies of the connectivity of neurons in the VTA show that the different subnuclei of this region project to several functionally and architectonically different regions of the cerebral cortex and subcortically to nuclei related to the limbic system. Results from our study show very prominent expression of CCK mRNAs in those subnuclei that project heavily to the prefrontal, other cortical areas, and the amygdaloid complex. The NT gene is expressed prominently in those subnuclei of VTA that project heavily to the entorhinal cortex and amygdaloid complex. These results provide support for a differential role for the NT-expressing neurons than that of CCK-expressing neurons of VTA in "reward" mechanisms and in drug-seeking and motivational behavior. These observations could be applied to create working hypotheses and experimental paradigms to test the differential functional activity of the subdivisions of VTA and their potential roles in the pathogenesis and treatment of drug-seeking behavior and other neuropsychiatric disorders.     

Osteocutaneous radial forearm free flaps. The necessity of internal fixation of the donor-site defect to prevent pathological fracture

BACKGROUND: Osteocutaneous radial forearm free flaps have fallen from favor due to pathological fractures of the radius. The purposes of this study were to propose a means to decrease the rate of pathological fracture by prophylactic fixation of the donor-site defect and to evaluate this technique biomechanically. METHODS: Two groups of ten matched pairs of fresh-frozen cadaveric radii were harvested. In Group 1, an eight-centimeter length of radius comprising 50 percent of the cross-sectional area of the bone was removed to simulate an osteocutaneous radial forearm donor-site defect. This defect was created in one member of each pair, with the other bone in the pair left intact. In Group 2, both members of the ten matched pairs of radii had identical defects created as previously described. However, one radius in each pair had a twelve-hole, 3.5-millimeter dynamic compression plate placed across the segmental defect. In each group, five matched pairs were tested to failure in torsion and five matched pairs were tested to failure in four-point bending. RESULTS: In Group 1, the intact radius was a mean of 5.7 times stronger in torsion and 4.2 times stronger in four-point bending than the radius with the segmental resection. In Group 2, the radius that was ostectomized and fixed with a plate was a mean of 4.0 times stronger in torsion and 2.7 times stronger in four-point bending than the ostectomized radius. CONCLUSIONS: Removal of an eight-centimeter segment from the radius dramatically decreased both torsion and bending strength. Application of a plate over the defect in the radius significantly restored the strength of the radius (p = 0.01).     

Anticancer activity of Sargassum wightii Greville on Dalton’s ascitic lymphoma简

AIM： Sargassum wightii Greville is a marine brown alga belonging to the Sargassaceae family which has about 200 species. The ethanolic extract of the whole dry plant powder contained numerous phytoconstituents, including flavonoids. The study was fo- cused on the anticancer activity ofSargassum wightii in mice. METHOD： The ethanolic extract ofSargassum wightii （EESW） at two dose levels was used to examine the anticancer activity in mice using DAL cell lines to induce cancer. The body weight, viable and non-viable tumor cell count, mean survival time, increase in life span, and hematological parameters were observed for anticancer activity of EESW. RESULTS： The intraperitoneal inoculation of DAL cells in mice significantly increased cancer cell count. The decrease in the cancer cell number observed in the EESW-treated group cancer animals indicates that the test drug has a significant inhibitory ef- fect on the tumor cell proliferation. Treatment with EESW also showed a significant decrease in tumor weight, and hence increased the lifespan of DAL-treated mice. In addition, EESW administration significantly restored the hematological parameters in DAL-treated mice. CONCLUSION： The present study results suggest that administration of extract offers enhanced antioxidant potential. Therefore it can be concluded from this study that EESW possesses anticancer activity.