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PubMed2001

The role of time as a quantifiable variable of toxicity and the experimental conditions when Haber's c x t product can be observed: implications for therapeutics.

One hundred years ago, Warren established for the first time a quantitative link between dose and time while studying the toxicity of sodium chloride in Daphnia magna (Straus). During this century, many toxicologists in different contexts returned to this idea, which has become known as Haber's Rule of inhalation toxicology. Most attempts to explore this relationship ended in frustration because of the observed deviations from it, which were unfortunately called exceptions. Thus, toxicologists concentrated on the quantitative relationship between dose and effect under mostly isotemporal conditions, while time was assigned such arbitrary, semiquantitative designations as acute, subacute, subchronic, and chronic. Time itself as a quantifiable variable of toxicity was seldom studied and when it was examined, it was often not done under isodosic (steady-state) conditions. A recent analysis of time as a variable of toxicity indicated the existence of at least three independent time scales (toxicokinetic, toxicodynamic, exposure frequency/duration) in toxicological studies, which interact with dose and effect to yield the enormous complexity known to every toxicologist. Based on prototypical examples when toxicokinetic (dioxins, chloroacetic acid), toxicodynamic (nitrosamines, soman, sarin, tabun), exposure frequency (methylene chloride), or other experimental design-related conditions (HgCl(2), CdCl(2)) represent the critical time scale, the general validity of the c x t = k concept will be discussed as a starting point for a theory of toxicology. As endpoints of toxicity, (delayed) acute toxicity, blood dyscrasias, and cancer will be used to illustrate the critical conditions needed to demonstrate the validity of this theory. The relevance of this theory to the pharmacologic action of chemicals and its implication for the therapeutic index are also discussed.

Acetates↗
PubMed2001

[Basophilic differentiation of leukemic cells in a patient with acute leukemia carrying minor bcr/abl chimeric mRNA].

A 77-year-old woman was referred to our hospital because of leukocytosis and leukoblastosis in September 1999. She was healthy except for hypertension, and no abnormal findings in the peripheral blood had been observed up to December 1998. Physical examination revealed neither hepatosplenomegaly nor superficial lymphadenopathy. A bone marrow film showed massive proliferation of blast cells (87.8%), some of which contained coarse basophilic granules (38.6%). The cells were negative for peroxidase and esterase (alpha-naphtyl butyrate and ASD-chloroacetate) staining, but the granules showed metachromasia upon toluidine blue staining. As immunophenotypic analysis of the cells showed double positive for CD13/CD19 but negativity for CD33, this case did not meet the diagnostic criteria for biphenotypic acute leukemia. Chromosome and gene analysis showed positivity for the Ph1 chromosome with minor bcr/abl chimeric mRNA. A homogenate of the peripheral mononuclear cells demonstrated a high concentration of histamine. Electron microscopy analysis confirmed that some of the blast cells contained dense granules, which closely resembled "immature basophil granules" morphologically. These results suggested that the blast cells showed basophilic differentiation. As the clinical course and peripheral blood findings were different from blastic crisis of chronic myelogenous leukemia (CML) and CML with minor bcr/abl chimeric mRNA, the present case was diagnosed as "multiphenotypic acute leukemia", a type of acute basophilic leukemia classified by Duchayne.

Aged↗
PubMedDate not supplied

Synthesis of some new quinoline derivatives: new routes to synthesize polysubstituted 2(1H)-quinolone derivatives.

Reaction of 4-hydroxyquinolines 1a,b or 1c,d with the ylidenenitriles 2b-g and 2h,c yielded pyranoquinolines 6 and 9, respectively. 4-Anilinoquinoline 10 reacted with 2a,e to give pyridoquinolines 12. Treating of 1a or 14 with SO2Cl2 gave 3-dichloroacetyl derivative 15. Compound 15 reacted with KCN/H2O and NaN3 to give furoquinoline 16 and the tetrazole 18, respectively. Reaction of 1a, b, f with a mixture of phenyl isothiocyanate and glycine gave pyranoquinoline 22. This compound reacted with chloroacetic acid to yield thiazolidinones 23. Pyranoquinolines 27 were synthesized either from the reaction of 1c,d with enamine 24 or reaction of 1e,f with hippuric acid. Condensation of 1c,d with the enamine 25 gave azlactone 28. The latter compound reacted with 4-aminoantipyrine and 2-aminopyridine to give the imidazole derivatives 30.

4-Quinolones↗
PubMed1979

Chronologic changes of activities of naphthol AS-D acetate esterase and other nonspecific esterases in the mononuclear phagocytes of tuberculous lesions.

Nonspecific esterases of mononuclear phagocytes (MNs) were studied histochemically in the developing and healing tuberculous lesions produced in rabbit skin by bacille Calmette Guérin (BCG). Nonspecific esterases were assayed with the following substrates: naphthol AS-D acetate (AS-D), naphthol AS-D chloroacetate (AS-D Chl), naphthol AS acetate (AS) and alpha-naphthyl acetate (alpha-N), beta-Galactosidase, a lysosomal enzyme of MNs, was also assayed as a marker of MN activation. The number of MNs hydrolyzing AS-D Chl, AS, and alpha-N increased for 2 to 4 weeks after infection. These chronologic changes were similar to that of beta-galactosidase. In contrast, MNs hydrolyzing AS-D appeared predominantly in the healing lesions five to six weeks after infection. These MNs had the morphologic features of balloon-like cells. They contained few lysosomes and gathered in clumps far from the caseous center. The activity of the AS-D esterase was almost completely inhibited by various trypsin inhibitors, but not by the serine esterase inhibitor of phenylmethylsulfonyl-fluoride. These results suggest that the AS-D esterase is a trypsin-like esterase which participates in the healing of tuberculous lesions.

Animals↗
PubMedDate not supplied

Synthesis and pharmacological activity of 1,4-benzodiazepine derivatives.

2-Aminobenzamides (3a-g) were prepared starting with isatoic anhydride. These compounds reacted with chloroacetic acid to give (4a-g), which were cyclized by dicyclohexylcorbodiimide to afford (5a-g). The preliminary pharmacological screening revealed that some of the new 2H-1,4-benzodiazepin-3,5(1H,4H)-dione derivatives (5) exhibited CNS-depressant and anticonvulsant activities.

Animals↗
PubMed2002

Extramedullary hematopoiesis in the uterine isthmus: a case report and review of the literature.

Extramedullary hematopoiesis (EH) is the ectopic production of myeloid, erythroid and megakaryocytic elements. In postfetal life it usually occurs in conditions with hyperactive, depleted or infiltrated marrow; it is extremely rare in the genital tract. We report a case of EH in the uterine isthmus (UI) which was found incidentally in a 40-year-old patient who presented with a right ovarian cyst and a history of a right modified radical mastectomy for infiltrating invasive lobular carcinoma one year earlier. The patient underwent total abdominal hysterectomy with bilateral salpingo-oophorectomy. Microscopic examination of UI revealed foci of hematopoiesis, consisting of white blood cell precursors confirmed by positive chloroacetate-esterase staining. Bone marrow biospy showed diffuse infiltration secondary to breast cancer. Further work-up, including a bone scan, showed multiple metastases suggesting that the high degree of bone marrow infiltration by neoplasmatic cells had stimulated the EH. In conclusion, the unusual finding of EH in UI heralded widespread infiltration of bone marrow.

Adult↗
PubMed2002

[Granulocytic sarcoma developing in lymph nodes].

A 77-year-old man was admitted to a hospital because of a left cervical tumor. He was initially diagnosed as having non-Hodgkin lymphoma, diffuse large cell type, Ann Arbor stage IV, and transferred to our hospital for chemotherapy. Flow cytometric analysis of the left axillary lymph node cells derived from a biopsy specimen showed that in addition to lymphoid surface markers (CD5, 7, 21), myeloid surface markers (CD11b, 33, 34) were also positive. The diagnosis of malignant lymphoma was therefore confirmed. The patient, was treated with THP-COP therapy, which proved very effective. Thereafter, a biopsy specimen was found to be positive for MT1 (CD43) staining but negative for myeloperoxidase and chloroacetate esterase staining on immunohistochemistry. Furthermore, no rearrangement of the IgH JH, TCR C beta 1 or TCR J gamma gene was detected by Southern blot analysis. On basis of these findings and the previous results of flow cytometry, we changed the diagnosis from malignant lymphoma to granulocytic sarcoma. THP-COP therapy was continued, and complete remission was achieved. Two months later, however, the patient developed acute myelocytic leukemia (AML M1) and received DCP therapy, but he died of pneumonia.

Aged↗
PubMedDate not supplied

Central nervous system activity of new pyrimidine-8-on[2,1-f]theophylline-9-alkylcarboxylic acids derivatives.

The appropriate esters 1-3 were synthesized by the alkylation of unsubstituted pyrimidin-8-on[2,1-f]theophylline I with ethyl-chloroacetate, ethyl-acrylate and ethyl-4-bromobutyrate. The acids 4-6 were obtained by hydrolysis of the esters 1-3, and transformed into Na salts 4a-6a. Amidation of the ester 1 with 25% ammonia and hydroxylamine led to amide 7 and N-hydroxyamide 8. The bromination of 1 gave 7-bromo intermediate 9 transformed to the 7-amino derivatives via nucleophilic substitution with phenylpiperazine for compound 10 and morpholine for compound 11. In the reaction of 9, 10 and 11 with sodium alcoholate, the corresponding Na salts 12a-14a were obtained. The pharmacological properties of the compounds were tested in CNS activity screening. It was found that all of the investigated compounds produced significant sedative effects in behavioral tests except weak activity of pyrimido[2,1-f]theophylline-9-sodium acetate 4a. The potent activity of pyrimido[2,1-f]theophylline-9-sodium butyrate 6a, pyrimido[2,1-f]theophylline-9-acetamide-7,7-N-phenylpiperazine-pyrimido[2,1-f]theophylline-9-sodium acetate 13a, and 7-N-morpholine-pyrimido[2,1-f]theophylline-9-sodium acetate 14a was observed. They inhibited spontaneous locomotor activity, potentiated sedation and prolonged duration of sleeping time after thiopental sodium administration. All compounds had no effects in the test of analgesia and they showed weak anti-convulsant properties. The results of this investigation may suggest hypnotic, sedative and/or tranquillizing properties of the tested compounds.

Animals↗
PubMed2002

Synthesis of some new bis-thiazoles as possible anticancer agents.

Several new 5-(2,3-dihydrothiazol-2-yledinyl)rhodanines 3a-c and 5-(4-oxothiazolidinon-2-ylidenyl)rhodanine 4 were synthesized through the reaction of 5-thiocarbamoyl rhodanines 2 with phenacyl bromides or chloroacetic acid, respectively. The synthesis of the arylidene derivatives 5a-c were also described. The 5-(4-amino-5-cyano-2,3-dihydrothiazol-2-yledinyl)rhodanines 10a, b were obtained through reaction of rhodanines 1a, b with thiazolium salt 9. All the prepared compounds were screened for their anticancer activity using the NCI in vitro anticancer screening program. Three compounds showed promising anticancer activity against particular human cell lines used in the assay.

Antineoplastic Agents↗
PubMed2003

Synthesis of some new pyrimidine and fused pyrimidine derivatives (Part 2).

6-Oxo-4(2-thienyl)-2-thioxo-1,3-dihydropyrimidine-5-carbonitrile (1) was synthesized and reacted with alkyl halides to give the S-alkyl compounds (2a,b), which reacted with phosphorous oxychloride to yield (3a,b). Reaction of 3a,b with phenyl-hydrazine, hydrazine hydrate, ammonia, acid hydrazides and thiourea leads to formation of the compounds (4a,b), the dihydrazino compound derivative (5), the amino compounds (7a,b), triazolopyrimidine derivatives (9a-d), and the mercapto compounds (10a,b), respectively. Treatment of (10a) with chloroacetone gave (11a), which condensed with benzaldehyde giving the tricyclic compound (12). Also (10b) reacted with ethyl chloroacetate followed by hydrolysis and cyclization yielded (14). Heating of (5) gave (6), which reacted with sodium nitrite and/or carbondisulphide and give (15) and (16), respectively.

Cyclization↗
PubMed2003

Pharmaco-economical analysis of the treatment with antibiotics in a surgery department.

6-Oxo-4(2-thienyl)-2-thioxo-1,3-dihydropyrimidine-5-carbonitrile (1) was synthesized and reacted with alkyl halides to give the S-alkyl compounds (2a,b), which reacted with phosphorous oxychloride to yield (3a,b). Reaction of 3a,b with phenyl-hydrazine, hydrazine hydrate, ammonia, acid hydrazides and thiourea leads to formation of the compounds (4a,b), the dihydrazino compound derivative (5), the amino compounds (7a,b), triazolopyrimidine derivatives (9a-d), and the mercapto compounds (10a,b), respectively. Treatment of (10a) with chloroacetone gave (11a), which condensed with benzaldehyde giving the tricyclic compound (12). Also (10b) reacted with ethyl chloroacetate followed by hydrolysis and cyclization yielded (14). Heating of (5) gave (6), which reacted with sodium nitrite and/or carbondisulphide and give (15) and (16), respectively.

Age Factors↗
PubMed1992

[Synthesis and radiosensitizing activity of benzimidazoles].

In search for effective radiosensitizer with low neurotoxicity, benzimidazole compounds were synthesized. Reaction of 2-nitrobenzimidazole with ethyl chloroformate yielded ethyl alpha-(2-nitrobenzimidazolyl-1)-formate(1) or ethyl alpha-(2-hydroxybenzimidazolyl-1)-formate(2), depending upon the solvents used. Reaction of 2-nitrobenzimidazole with 1,2-epoxy-3-chloropropane gave a cyclized compound which was confirmed to be benzimidazo(1,2b)-5'-chloromethyl-oxazolidine(3). In attempt to increase hydrophilicity, 1-substituted 2(3'-pyridyl)-5-nitrobenzimidazoles were prepared by reaction of 2-(3'-pyridyl)-5(6)-nitrobenzimidazole(4) with alkyl epoxides or ethyl chloroacetate. Some of the compounds synthesized were tested for radiosensitizing activity in Ehrlich ascites carcinoma-bearing mice. Preliminary results showed that some compounds have radiosensitizing activity. The radiosensitizing enhancement ratio (SER) of compounds 3, 5 and 6 were found to be 1.50, 1.52 and 1.65 respectively.

Animals↗
PubMed1992

[Cytochemical evaluation of blast cells in acute myeloblastic leukemia after induction of their maturation in liquid culture--diagnostic usefulness].

We have performed the cytochemical analysis (myeloperoxidase, ASD-chloroacetate and acid alpha-naphthylacetate esterases, Sudan black B) of blast cells from 25 acute leukemia patients, after 3, 5 and 7 days of liquid culture with conditioned medium from phytohemagglutinin stimulated leukocytes (PHA-LCM). In case of acute myeloid leukemia blast cells an increase of percentage of positive cells simultaneously with the enhancement of the cytochemical reactions was observed. This method may be useful for the precise diagnosis of poorly differentiated blasts with weak expression of cytochemical phenotype.

Adolescent↗
PubMed1992

Primary myelodysplastic syndromes: diagnostic and prognostic significance of immunohistochemical assessment of bone marrow biopsies.

Material from 63 cases with primary myelodysplastic syndromes (P-MDS) (French-American-British [FAB] types: refractory anemia [RA] = 21; RA with ring sideroblasts [RARS] = 8; RA with excess of blasts (RAEB) = 10; RAEB in transformation (RAEBt) = 6; chronic myelomonocytic leukemia [CMML] = 10 and unclassifiable = 8, ie, bone marrow aspiration was inadequate and stringent FAB criteria were not applicable) was analyzed for bone marrow histologic and immunohistochemical patterns. Standard Giemsa, hematoxylin and eosin (H&E) and reticulin stains were used for morphologic assessment. To identify the cell lineage precisely, chloroacetate esterase staining and an indirect immunoperoxidase technique using mouse monoclonal antibodies CD15, CD68, HLA-DR, and rabbit polyclonal CD3 and UEA-1 (lectin) was developed on formalin-fixed paraffin embedded bone marrow biopsies (BMB). The immunohistochemical assessment permitted accurate identification of dysplastic features such as mononuclear and binuclear megakaryocytes, Pelger-Huet neutrophils, and binuclear erythroblasts. Additional bone marrow histologic and immunohistochemical features observed were heterogeneity of immunohistochemical staining in various cell lineages, megakaryocytic emperipolesis, alteration of bone marrow microarchitecture, intravascular clusters of hematopoietic cells, and the types of benign lymphoid aggregates. The nature of abnormally localized immature precursors (ALIP) was discerned. Three types of clusters of immature cells were found that were difficult to distinguish on Giemsa and H&E morphology, these were erythroid aggregates (n = 18); megakaryocytic aggregates (n = 4), and immature granulocytic and monocytic aggregates (n = 32). The bone marrow histologic and immunohistologic patterns permitted the identification of four groups of clinical relevance: Group 1, cases with predominant erythroid hyperplasia and without ALIP (n = 15); group 2, cases with prominent myeloid hyperplasia and presence of ALIP (n = 32); group 3, cases with hypoplastic MDS (n = 10); and group 4, cases with hyperfibrotic MDS (n = 6). Statistical analysis showed a significant difference in survival and leukemic transformation between groups 1, 2, 3, and 4, with cases in group 2 showing the worst prognosis with early death due to increased propensity to leukemic transformation and cytopenia-related complications (P less than .0001). We conclude that immunohistochemistry is feasible on routinely processed BMB and the information obtained is of diagnostic and prognostic importance in P-MDS. The phenotype of ALIP varies with the morphologic and histologic subtypes of MDS and the term should be reserved for cases in whom the clusters in the intertrabecular region are of myeloid (granulocytic and monocytic) lineage on immunohistochemistry.

Aged↗
PubMed1992

[A case of systemic mastocytosis].

The authors describe a rare case of systemic mastocytosis without skin infiltration. The first symptom were episodes of flushing in the face and upper trunk. From the case-history it was assumed that the condition had a several year's benign course, the diagnosis was established in the stage of malignant acceleration of the disease from bone marrow biopsy and liver biopsy. Atypical mastocytes displayed metachromasia with toluidine blue and positive naphthol-AS-D chloroacetate esterase. Symptomatic treatment with sodium cromoglycate reduced temporarily the frequency of flushing episodes, but it was not possible to arrest the increase of the mastocyte mass by cytostatic treatment.

Bone Marrow↗
PubMed1992

[A case of monoblastic crisis of CML beginning with extramedullary tumor formation in a rib].

A patient with CML showed monoblastic crisis which started with extramedullary tumor formation in a rib before medullary involvement. She was diagnosed as having CML in 1984 at the age of 57. In February 1990, she was admitted to Furukawa City Hospital because of extramedullary blastic crisis beginning at the right 5th rib. At that time, the bone marrow revealed 4.6% blasts. On March 5, after one course of chemotherapy, she was transferred to our hospital for radiotherapy. Hematological findings were WBC 10,100/microliter with 10% blasts, Hb 10.9 g/dl, platelet 3.7 x 10(4)/microliters. Bone marrow aspiration was unsuccessful. The blasts in the peripheral blood were negative for peroxidase and chloroacetate esterase; but positive for naphtylbutyrate esterase. The leukemic cells were positive for CD13, CD33, and had phagocytic activity. Chromosomal analysis revealed 46XX with Ph1 chromosome and some additional anomalies. Southern blot analysis of tumor cells shows BCR rearrangement. These findings suggest that the blasts were immature monocytic cells, and we conclude that this is a rare case of extramedullary monoblastic crisis of CML.

Bone Neoplasms↗
PubMedDate not supplied

Presacral myelolipoma. Report of a case with fine needle aspiration cytology and immunohistochemical and histochemical studies.

The cytomorphologic features of a case of the rare presacral myelolipoma, diagnosed by computed tomography (CT)-guided percutaneous fine needle aspiration (FNA) biopsy, are presented. It occurred in a 40-year-old man on prolonged steroid therapy for bronchial asthma. On the air-dried, Diff-Quik-stained smear, hematopoietic cells of all lineages and fragments of collapsed stroma were seen in a background of fat droplets. Megakaryocytic, myelocytic and eosinophilic lineages were further demonstrated by Factor VIII immunostain, chloroacetate esterase and LUNA-E histochemical stain, respectively. The reticulum stain of the resected tumor demonstrated that the hematopoietic cells and fat were supported by numerous reticulum fibers of varying thickness; that accounted for the collapsed stroma in the aspirated material. Presacral myelolipoma, occurring predominantly in female adults and presenting secondarily as a space-occupying lesion, is best regarded as encapsulated, heterotopic bone marrow supported by a network of reticulum fibers; it has a characteristic image on CT scan and can be diagnosed by FNA.

Adult↗
PubMed1977

An enzyme histochemical study of non-Hodgkin's lymphoma and allied disease.

The enzyme activity for alpha-naphthyl-acetate esterase, naphthol-AS-acetate esterase, naphthol-AS-D-chloroacetate esterase, acid phosphatase, L(+)-tartrate-resistant acid phosphatase, adenosine triphosphatase, and 5'-nucleotidase was examined on the neoplastic cells of giant follicular lymphoblastoma, the so-called reticulum cell sarcoma and Sézary syndrome. The neoplastic cells of giant follicular lymphoblastoma showed distinct activity for adenosine triphosphatase and 5'-nucleotidase, and those of the so-called reticulum cell sarcoma had no characteristic nature of the reticulum cells or histiocytes enzyme histochemically. These findings suggest that these neoplastic cells may be derived from the B-cell system. In Sézary syndrome, acid phosphatase activity was localized in a small paranuclear area in Sézary cells, which were considered to have a T-cell nature. It is thought that these enzyme histochemical methods are easy and useful in differentiating the B- or T-cell nature and the classification of non-Hodgkin's lymphomas.

Acid Phosphatase↗