Gastroprotective Effect of Capparis spinosa on Indomethacin-induced Gastric Ulcer in Rats.

Peptic ulcer is an acid-induced lesion that is usually found in the stomach and duodenum. It is usually a case of imbalance between the acid (and other injurious factors) and the mucosal defense mechanisms. Indomethacin is one of the most ulcerogenic drugs that is prescribed over-the-counter for the management of musculoskeletal problems. Capparis spinosa is one of the most important species in the Capparidaceae family, which has a wide range of diversity. Caper (Capparis spinosa L.) is a common member of the genus Capparis (Capparidaceae family). The present study was designed to compare the effect of C. spinosa extract as a gastroprotective agent with indomethacin as an induction agent and ranitidine as a standard drug. To this aim, 40 adult male Wistar rats were randomly divided into 4 groups (n=10 each), including Control +: indomethacin-treated group, Control -: receiving physiological saline solution, C.S: C. spinosa-treated group; and ranitidine-treated group (50 mg/kg) as a standard agent for the treatment of the gastric ulcer. After the experimental period, all the animals were sacrificed by anesthesia overdose and their stomachs were removed. The gastroprotective effect of C. spinosa was investigated by studying prostaglandin E2 (PGE2), Gastrin, anti-tumor necrosis factor alpha (TNF-α), and Interleukin 1 beta (IL1-ß), along with histopathological examination. The results showed a significant increase in PGE2 levels in the ranitidine-treated group with a significant reduction in Gastrin, TNF-α, and IL1-ß. The recorded data obtained from the histopathological study showed a significant improvement in the treated group with the extract of C. spinosa. The study concluded that C. spinosa had gastroprotective properties possibly through enhancing PGE2 which was acting as anti-inflammatory inhibiting neutrophil infiltration.

Synthesis, antitumor, cytotoxic and antioxidant evaluation of some new pyrazolotriazines attached to antipyrine moiety.

Iminopropanehydrazonoyl cyanide 4 was achieved upon reaction of antipyrine diazonium salt 2 with 3-iminobutanenitrile (3) in EtOH/AcONa. 3-Aminopyrazole derivative 5 was obtained upon reaction of 4 with hydrazine hydrate. Diazodization of 5 afforded the diazonium salt 6 which coupled with active methylene compounds 7-10, 19, 20, 25, 29 and 32 in pyridine to give aryl hydrazone derivatives 11-14, 21, 22, 26, 30 and 33, respectively. Refluxing of compounds 11-14, 21, 22, 26 and 33 in acetic acid afforded the pyrazolotriazines 15-18, 23, 24, 28 and 35, respectively. The newly synthesized compounds were screened for their cytotoxic and antioxidant activities. The results showed clearly that compounds 4, 5, 13, 22, and 24 displayed promising in vitro anticancer activity against four different cell lines (HepG2, WI 38, VERO and MCF-7). Compounds 4 and 22 are the more potent antioxidant and anticancer agents. On the other hand, most of the compounds exhibited good cytotoxic activity toward (EAC).

Effect of surgery for cannula implantation into the hypothalamus on the behaviour and neural activity of broiler chicks.

1. The effects of a surgical operation, to implant a guide cannula in the chick hypothalamus for microdialysis, on behavioural responses and neural activity in broiler chicks are described. 2. General behavioural activities (feeding, preening, sitting, drinking, cage pecking and beak wiping), open field and locomotor activity tests were conducted to evaluate the effects related to surgery in the immediate 4 d following this procedure. Perfusion of Ringer solution with high K(+) after 4 d of guide cannula implantation was used to estimate the neural activity resulting from surgery through stimulation of monoamine release by in vivo brain dialysis. 3. The results of direct behavioral observations indicated that the stress provoked by surgical guide cannula insertion caused behavioural alterations that are particularly evident in the immediate days following this procedure. Open-field tests on day 4 after surgery showed that, compared to the intact control chickens, the treated chicks had a shorter latency to ambulate and defecate, with more vocalisation. Locomotor activity was less in the treated chicks than in the controls. 4. After 4 d of guide cannula implantation, the serotonin concentration started to increase 30 min after the onset of perfusing high-K(+) Ringer solution. It reached its highest value at one hour, suggesting that the 4 d after surgery is enough to alleviate some neurochemical dysfunction resulting from surgery. The results of behavioural observations, open-field and locomotor activity tests indicate that the surgical operation caused stress and fear in chicks which persisted up to 4 d.

Synthesis, antitumor evaluation, molecular modeling and quantitative structure-activity relationship (QSAR) of some novel arylazopyrazolodiazine and triazine analogs.

The synthesis, in vivo and in vitro antitumor evaluation, and QSAR studies of some novel pyrazole analogs against Ehrlich Ascites Carcinoma (EAC) cells were described. In vitro results revealed that compounds 10, 6 and 4 were the most potent analogs against EAC, respectively. Moreover, in vivo evaluation of compounds 6 and 10 proved their capability to normalize the blood picture in comparison to 5-FU, a well known anticancer drug. These novel pyrazole analogs were molecularly designed with the goal of having significant potent cytotoxic effect against EAC cells. To develop a QSAR model capable of identifying the key molecular descriptors associated with the biological activity of the novel pyrazole analogs and predicting the cytotoxic effect for other novel pyrazole analogs against EAC cells, different QSAR models, using different physicochemical and topological molecular descriptors, were developed. Different molecular descriptors were predicted solely from the chemical structures of 16 pyrazolo-diazine and triazine analogs following the prediction of the equilibrium molecular geometry of each analog at the DFT level using B88-LYP functional energy and double zeta valence polarized (DZVP) basis set. It was found that dipole moment, excitation energy, the energy value of LUMO, solvent accessible surface area, and heat of formation were the key molecular descriptors in descriping the cytotoxic effect of those compounds against EAC.

Prognostic value of p53 and MDM2 expression in bilharziasis-associated squamous cell carcinoma of the urinary bladder.

The aim of this study was to elucidate the associations between immunostaining for MDM2 and p53, their respective expression in squamous cell carcinoma of the urinary bladder, and the value of these variables for predicting treatment outcome after cystectomy. Inactivation of TP53 might play a role in the development and progression of bladder cancer. Complex formation with the MDM2 product is one mechanism that inactivates the p53 protein. Therefore, the MDM2 and the p53 protein were investigated to study potential interactions in bladder cancer. Fifty archival bladder tissue specimens were immunohistochemically stained using monoclonal antibodies against p53 and MDM2. Staining for p53 was observed in 48% of the specimens and staining for MDM2 in 20%. Univariate analysis demonstrated a significant correlation between p53 accumulation and survival (p = 0.0101), while the correlation between MDM2 and survival was not significant (p = 0.7183). The combined expression of MDM2 and p53 doest not add to the prognostic information provided by p53 alone.

Synthesis and reactions of some new substituted 6-imidazolyl-4-oxo-4H-1-benzopyran-3-carboxaldehyde and use of DNA in evaluation of their biological activity.

Vilsmeier-Haack reaction of imidazolyl acetophenone I gave 6-imidazolyl-4-oxo-4H-1-benzopyran-3-carboxaldehyde II. The compound II was reacted with primary amines (1:1 molar ratio) to form the corresponding n-aril (meteroaryl) imino derivatives IIIa-f. Treatment of aldehyde II with excess amines (1:2 molar ratio) gave the corresponding 2-arylamino-3-arylaminomethylenebenzopyran derivatives IVa-c. The n-aril (meteroaryl) imino derivatives IIIb,d,e,f were reacted with thioglycollic acid to give benzopyranothiazepinone derivatives VIa-d. When the aldehyde II was treated with secondary amines gave the corresponding trans-enaminoketones VIIIa-c. Trans-enaminoketones VIIIa-c were reacted with hydrazines and/or hydroxylamine hydrochloride to give pyrazolyl and/or isoxazolyl benzene IXa-c and X, respectively. The reaction of aldehyde II with hydrazines on cold gave the corresponding hydrazones XIIIa-d. However, the reaction of aldehyde II with hydrazines on refluxing gave the corresponding pyrazole derivatives 5 XIVa,b and XVa,b.. The structural formula of the new compounds were established by using different instrumental analyses. Some compounds in this study were biologically evaluated for their ability to bind to DNA.

Case report: endometrial cancer implanting in the laparotomy scar.

A 58-year-old woman underwent abdominal hysterectomy and bilateral salpingo-oophorectomy for stage Ib, grade 2 endometrial adenocarcinoma followed by external pelvic irradiation. Five years later she presented with a 7 cm solitary infraumbilical incisional tumor recurrence that was resected. Histology of the tumor implant was similar to that of the primary cancer. The patient was then started on progestin therapy with no evidence of recurrence for four years. To our knowledge this is the fourth reported case of endometrial cancer implanting in an abdominal scar.

Giant cervical polyp. A case report.

BACKGROUND: Very large cervical polyps are rarely reported. CASE: A giant cervical polyp, 17 x 10 x 5 cm, protruded through the vaginal introitus in a 27-year-old, sexually inactive woman. CONCLUSION: Although carcinomatous change occurs in 1.7% of cervical polyps, malignant degeneration did not occur in the six reported cases. Thus, biopsy of these tumors before excision may not be necessary.

Intrathoracic Kaposi's sarcoma. CT findings.

AIM: To describe the thin CT scans findings in AIDS patients with intrathoracic Kaposi's sarcoma (KS). MATERIAL AND METHODS: Fifty-three CT scans of patients with KS were retrospectively reviewed. The diagnosis of intrathoracic KS was established histologically (n = 17) or on the association of skin KS and the visualization of characteristic endobronchial lesions (n = 36). CT scans were performed with thin slices (2 mm) obtained at 10-mm intervals, and a 512 x 512 reconstruction matrix. No patients had Pneumocystis carinii pneumonia within the 3 months preceding the CT scan examination. RESULTS: Numerous nodules (n = 42), tumoral masses (n = 28), bronchovascular pathways thickening (n = 35), and pleural effusions (n = 28) were the most frequent patterns. Septal lines (n = 15), ground-glass opacities (n = 3), and mediastinal adenopathies (n = 8) were not frequent. CONCLUSION: Numerous nodules, tumoral masses, bronchovascular pathways thickening, and bilateral pleural effusions were the main signs of intrathoracic KS; their association (66%) is very characteristic. An opportunistic infection or mycobacteriosis must be sought if the thin CT scans reveal ground-glass opacities and/or mediastinal adenopathies.

Chromosome aberrations in cultured rat bone marrow cells treated with inorganic fluorides.

The genotoxic effects of inorganic fluorides were investigated by treating cultured rat bone marrow cells with varying concentrations (0.1-100 microM) of potassium fluoride (KF) and sodium fluoride (NaF) for different durations (12, 24 and 36 h) and measuring the incidence of cells with aberrations and number of breaks per cell. Both forms of fluoride were found to be weak mutagens relative to the positive control N-methyl-N-nitro-N-nitrosoguanidine (MNNG). A specificity of fluoride ion in inducing chromosome aberrations (CA) was indicated by the observation that both NaF and KF behaved almost equivalently in this study and at significantly higher variations from the results with potassium chloride (KCl) and sodium chloride (NaCl).

Prolonged intake of chlorambucil for ovarian cancer.

The use of alkylating agents has been reported to be a cause of secondary leukemia particularly in patients surviving for 2 years or more after treatment of ovarian carcinoma. The risk of developing leukemia is possibly related to the duration of treatment and the total dose of alkylating agents administered. We report a patient with epithelial ovarian carcinoma who received chlorambucil for 130 consecutive months with no clinical or laboratory evidence of leukemia.

Reproductive outcome following abdominal metroplasty.

OBJECTIVE: To evaluate pregnancy outcome following uterine unification procedures in patients with uterine anomalies. METHODS: A retrospective survey included all abdominal metroplasty procedures performed on 43 patients at the American University of Beirut Medical Center between January 1, 1974 and December 31, 1991. Age at metroplasty, type of anomaly and surgical procedures, as well as preoperative and postoperative reproductive performance were all recorded. RESULTS: Forty (93%) out of 43 patients who underwent metroplasty had postoperative live births compared with five (12%) prior to surgery. The fetal wastage rate dropped from 93% pre- to 16% postoperatively. All seven patients with a history of primary infertility conceived and had live births. CONCLUSION: Our data suggest a remarkable improvement following abdominal metroplasty in patients with both typical and uncharacteristic preoperative reproductive performance.

Chromosome aberrations in blood lymphocytes from petroleum refinery workers.

To evaluate the possible cytogenetic consequences of exposure of human populations to petrochemicals, the frequency of chromosomal aberrations was studied in blood lymphocytes obtained from 233 persons working at different locations in a large oil refinery (184 exposed and 49 worksite controls) and from 47 individuals who served as community controls. Chromosomal aberrations occurred with frequencies (mean +/- SEM) between 0.023 +/- 0.013 and 0.037 +/- 0.011 breaks per cell (1.56 +/- 0.87% to 2.66 +/- 0.54% aberrant cells) in the exposed groups. These values, with the exception of those observed in two workshops (crude oil unloading as well as petroleum tanker washing and lubrication), were significant compared to the presumably spontaneous (control) levels (0.015 +/- 0.004 to 0.021 +/- 0.007 breaks per cell and 1.17 +/- 0.29% to 1.46 +/- 0.40% aberrant cells). Cigarette-smoking was not associated with increased chromosomal aberrations in the exposed and in the control groups.

Case report and review of literature: leptomeningeal relapse in epithelial ovarian cancer.

The diagnosis of leptomeningeal relapse in a patient with epithelial ovarian cancer was confirmed by the presence of malignant ovarian cells in the cerebrospinal fluid. There was no clinical evidence of tumor spread elsewhere. Therapy, including intrathecal methotrexate and whole-brain irradiation led to transient clinical improvement. International literature review revealed only 13 other cases of leptomeningeal carcinomatosis in epithelial ovarian cancer; all died within 15 months following the diagnosis of leptomeningeal spread.