Molluscicidal and ovicidal activities of plant extracts of the Piperaceae on Biomphalaria glabrata (Say, 1818).

Schistosomiasis is a tropical disease caused by Schistosoma and occurs in 54 countries, mainly in South America, the Caribbean region, Africa and the eastern Mediterranean. Currently, 5 to 6 million Brazilian people are infected and 30,000 are under infection risk. Typical of poor regions, this disease is associated with the lack of basic sanitation and very frequently to the use of contaminated water in agriculture, housework and leisure. One of the most efficient methods of controlling the disease is application of molluscicides to eliminate or to reduce the population of the intermediate host snail Biomphalaria glabrata. Studies on molluscicidal activity of plant extracts have been stimulated by issues such as environmental preservation, high cost and recurrent resistance of snails to synthetic molluscicides. The aim of this study was to determine the molluscicide action of extracts from Piperaceae species on adult and embryonic stages of B. glabrata. Fifteen extracts from 13 Piperaceae species were obtained from stems, leaves and roots. Toxicity of extracts was evaluated against snails at two different concentrations (500 and 100 ppm) and those causing 100% mortality at 100 ppm concentration were selected to obtain the LC90 (lethal concentration of 90% mortality). Piper aduncum, P. crassinervium, P. cuyabanum, P. diospyrifolium and P. hostmannianum gave 100% mortality of adult snails at concentrations ranging from 10 to 60 ppm. These extracts were also assayed on embryonic stages of B. glabrata and those from P. cuyabanum and P. hostmannianum showed 100% ovicidal action at 20 ppm.

Molluscicidal and ovicidal activities ofplant extracts of the Piperaceae onBiomphalaria glabrata (Say, 1818)

Schistosomiasis is a tropical disease caused by Schistosoma and occurs in 54countries, mainly in South America, the Caribbean region, Africa and the easternMediterranean. Currently, 5 to 6 million Brazilian people are infected and 30,000are under infection risk. Typical of poor regions, this disease is associated withthe lack of basic sanitation and very frequently to the use of contaminated water in agriculture, housework and leisure. One of the most efficient methods of controlling the disease is application of molluscicides to eliminate or to reduce the population of the intermediate host snail Biomphalaria glabrata. Studies on molluscicidal activity of plant extracts have been stimulated by issues such as environmental preservation, high cost and recurrent resistance of snails tosynthetic molluscicides. The aim of this study was to determine the molluscicideaction of extracts from Piperaceae species on adult and embryonic stages ofB. glabrata. Fifteen extracts from 13 Piperaceae species were obtained from stems, leaves and roots. Toxicity of extracts was evaluated against snails at two different concentrations (500 and 100ppm) and those causing 100% mortality at 100ppm concentration were selected to obtain the LC90 (lethal concentration of 90% mortality). Piper aduncum, P. crassinervium, P. cuyabanum, P. diospyrifolium and P. hostmannianum gave 100% mortality of adult snails at concentrations ranging from 10 to 60 ppm. These extracts were also assayed on embryonic stages of B. glabrata and those from P. cuyabanum and P. hostmannianum showed 100%ovicidal action at 20ppm.

The inhibitory effects of TNP470 on tumour growth of head and neck carcinoma cell producing interleukin-8.

The anti-tumour effect of the angiogenic inhibitor TNP470, sigma-(chloro-acetyl-carbamoyl) fumagillol, a synthetic analogue of fumagillin, was studied in vitro and in vivo using KB cells, one of the human head and neck carcinoma cell lines that produce interleukin(IL)-8. In the in vitro study, the combination treatment of TNP470 and anti-IL-8 antibody significantly reduced the proliferation of KB cells. In the in vivo studies, TNP470 administration by any route (intratumoral: i.t., intraperitoneal: i.p., intravenous: i.v.) reduced the tumour volume significantly, compared to the control group. Among the groups administered TNP470, the anti-tumour effect was strongest in the it group. Furthermore, the concurrent treatment of anti-IL-8 antibody and TNP470 also maximally reduced the tumour volume. The combination therapy of TNP470 and anti-IL-8 antibody was very effective. These results suggest that combination therapy of TNP470 and anti-IL-8 antibody could be beneficial for solid tumours, such as head and neck cancer.

[Antitumor effect of the angiogenesis inhibitor, TNP470, on squamous cell carcinoma cells in head and neck cancer].

The antitumor effect of the angiogenesis inhibitor TNP470, O-(chloro-acetyl-carbamoyl) fumagillol, a synthetic analogue of fumagillin, was studied in vitro and in vivo on, cell line KB which produced interleukin (IL)-8. In vitro, TNP470 reduced the production of IL-8 from KB cells, the same as anti-IL-8 antibody (Ab.) The combination of anti-IL-8 Ab (10 micrograms/ml) and TNP470 (10 ng/ml) significantly inhibited the proliferation of KB cells, compared to no treatment (p < 0.05). Proliferation of KB cells was also significantly more suppressed by simultaneous treatment of cisplatin and TNP470 (1 mg/ml), than cisplatin alone. The in vivo antitumor effect of TNP470 was studied using anti-IL-8 Ab, anti-vascular endothel growth factor (VEGF) Ab, and TNP470, in administered by different routes, i.e., intratumoral (i.t.), intraperitoneal (i.p.), and intravenous. TNP470 (10 mg/ml) showed an antitumor effect, and intratumoral administration of TNP470 was the most effective route. Combined administration of anti-IL-8 Ab (i.p.) and TNP470 (i.t.) reduced tumor volume more than anti-IL-8 Ab alone did. These results suggest that the combination of TNP470, cisplatin, and anti-IL-8 Ab could be a beneficial treatment for solid tumors of the head and neck.

Relation between green tea consumption and the severity of coronary atherosclerosis among Japanese men and women.

PURPOSE: To examine the relation between green tea consumption and arteriographically determined coronary atherosclerosis. METHODS: Study subjects were 512 patients (302 men and 210 women) aged 30 years or older who underwent coronary arteriography for the first time at four hospitals in Fukuoka City or one hospital in an adjacent city between September 1996 and August 1997. Lifestyle characteristics including green tea consumption were ascertained before arteriography by a questionnaire supported with interview. RESULTS: 117 men (38.7%) and 50 women (23.8%) had significant stenosis of one or more coronary arteries. Green tea consumption tended to be inversely associated with coronary atherosclerosis in men, but not in women. An evident, protective association between green tea and coronary atherosclerosis was observed in a subgroup of 262 men excluding those under dietary or drug treatment for diabetes mellitus. In this subgroup, after adjustment for traditional coronary risk factors and coffee, odds ratios of significant stenosis for consumption of 2-3 cups and 4 or more cups per day were 0.5 (95% confidence interval 0.2-1.2) and 0.4 (0.2-0.9), respectively, as compared with a consumption of one cup per day or less. CONCLUSIONS: The results indicate that green tea may be protective against coronary atherosclerosis at least in men.

Importance of the G protein gamma subunit in activating G protein-coupled inward rectifier K(+) channels.

The G protein-coupled inward rectifier K(+) channel (GIRK) is activated by direct interaction with the heterotrimeric GTP-binding protein betagamma subunits (Gbetagamma). However, the precise role of Gbeta and Ggamma in GIRK activation remains to be elucidated. Using transient expression of GIRK1, GIRK2, Gbeta1, and Ggamma2 in human embryonic kidney 293 cells, we show that C-terminal mutants of Gbeta1, which do not bind to Ggamma2, are still able to associate with GIRK, but these mutants are unable to induce activation of GIRK channels. In contrast, other C-terminal mutants of Gbeta1 that bind to Ggamma2, are capable of activating the GIRK channel. These results suggest that Ggamma plays a more important role than that of an anchoring device for the Gbetagamma-induced GIRK activation.

Unsaturated fatty acid feeding prevents the development of acute hepatitis in Long-Evans cinnamon (LEC) rats.

To investigate the effects of dietary alpha-linolenic acid (18:3, n-3; alpha-LNA) and linoleic acid (18:2, n-6; LA) on the development of hereditary hepatitis, we compared incidences and grades of acute hepatitis between the Long-Evans cinnamon (LEC) rats fed with safflower oil-supplemented diet and perilla oil-supplemented diet. Both safflower and perilla oil supplemented diets reduced the incidence of hepatitis and significantly prolonged its onset as compared to the non-supplemented conventional diet. No significant difference was observed between safflower and perilla oil diets in the rats of incidence of hepatitis. At the age of 16 weeks, just before the onset of hepatitis, serum levels of transaminase (AST, ALT) and concentration of copper in rats fed with both test diets were significantly reduced as compared with that of rats fed alpha-linolenate and linoleate have an inhibitory effect on the development of hepatitis in LEC rats due to the prevention of serum copper elevation.

Cloning and characterization of a Drosophila melanogaster cDNA encoding a glutamate transporter.

A Drosophila cDNA encoding a glutamate transporter was cloned and examined. The predicted protein (479 amino acid residues) shows significant sequence identity with mammalian counterparts. The protein expressed in Xenopus oocytes had a glutamate transport activity. Northern blot analysis showed that the transcript increased in amount developmentally. This expression pattern is different from those of Drosophila glutamate receptors.

Synchronous multiple colorectal adenocarcinomas.

BACKGROUND: The object of the present work was to characterize clinical features and the quality of preoperative examinations in patients with synchronous colorectal carcinomas, and to compare the incidence of associated benign polyps with our findings in patients with a single malignant lesion. METHODS: A retrospective evaluation of 225 patients with primary colorectal carcinoma revealed 9 cases (4.0%) of synchronous colorectal carcinomas. RESULTS: The synchronous colorectal carcinomas were located in the same anatomical segment in 7 patients and were divided into different segments in 2 patients. The accuracy of preoperative diagnosis was 55.6% by endoscopy alone and 66.7% by double contrast barium enema (DCBE) alone, while the rate was 77.8% when colonoscopy and DCBE were combined. There was a higher incidence of associated benign polyps in the group with synchronous colorectal carcinomas (55.6%) versus 28.7% for a single carcinoma (P < 0.05). The main reason why multiple lesions could not be identified preoperatively was that the distal lesions prevented examination of the proximal lesions. CONCLUSIONS: At the time of surgical resection, it is important to ascertain preoperatively whether or not a second lesion exists. If synchronous polyps are present in patients with synchronous colorectal carcinomas, they should be ablated to reduce the risk of metachronous colorectal carcinoma.

[Comparison of analgesic effect of lidocaine tape versus eutectic mixture of lidocaine and tetracaine during infiltration of local anesthetics before epidural block].

We compared analgesic effects of a lidocaine tape (Penles) and the eutectic mixture of lidocaine and tetracaine (LT ointment) during local infiltration before epidural block. Ninety-six patients were randomly assigned to 3 groups. In groups 1 and 2, lidocaine tape was applied on the skin of the epidural puncture site 30-60 min before epidural block. In group 3, 1 g of LT ointment was applied on the same place 1-2 h before block. Additionally, patients in groups 2 and 3 were medicated intramuscularly with midazolam 5 mg. Although no significant difference in pain relief in 5 pin prick tests was observed among the three groups, there was a significantly greater decrease in the pain score during the infiltration of local anesthetics in groups 1 and 2, compared with group 3. There was no significant difference in the pain score between groups 1 and 2. We concluded that lidocaine tape is more useful than LT ointment in decreasing pain of local infiltration anesthesia, and midazolam did not exert any supplementary analgesic effect.

Combined drug therapy with diltiazem, dextran, and hydrocortisone (DDH therapy) for late cerebral vasospasm after aneurysmal subarachnoid hemorrhage: assessment of efficacy and safety in an open clinical study.

Late cerebral vasospasm after subarachnoid hemorrhage (SAH) is a disastrous phenomenon for the patients and a definite treatment has not been established. We studied 48 consecutive patients receiving high-dose diltiazem (5 micrograms/kg/min) injection combined with dextran and hydrocortisone to late cerebral vasospasm after aneurysmal subarachnoid hemorrhage (SAH). All but 2 patients underwent surgery within 72 hours after SAH. Diltiazem was continuously given via a central venous line for up to 2 weeks in conjunction with simple cisternal drainage. 5% of dextran solution (500 ml/day) was infused for 7-10 days. Hydrocortisone was given 1,600 mg on the first day, then the dose was gradually decreased over 14 days. Symptomatic vasospasm (SVS) occurred in 5 patients (10.4%), 4 patients recovered, but 1 had severe neurological deficit. A low density area on CT-scan was observed in 2 patients. Thirty patients (62.5%) had good recovery, 10 patients (20.8%) had moderate disability, 3 (6.3%) had severe disability and 3 (6.3%) had vegetative survival. Two patients died of the initial brain damage. There were no severely hypotensive side effects. However, 3 patients showed atrioventricular blockage on electrocardiogram. These side effects subsided after the dose of the drug was decreased or administration was stopped altogether. These findings show that high-dose calcium antagonist diltiazem therapy combined with dextran and hydrocortisone injection is safe and effective for prevention of late cerebral symptomatic vasospasm after SAH.

[A study of hemodynamic effects during dental treatment under local anesthesia. Observation of parasympathetic activity based on the index of R-R interval variation in ECG].

Observing hemodynamic changes occurring during dental treatment performed under local anesthesia is very important. Although many reports on such changes have been made on the basis of blood pressure and heart rate indexes, few have been made on the basis of parasympathetic activity. This is a report of a study on observations of parasympathetic activity on the basis of the index of R-R interval variation in ECG. A multipurpose monitoring system was used to observe and record hemodynamic changes in 52 patients undergoing dental treatment under local anesthesia. In addition, parasympathetic activity was observed on the basis of the index of the coefficient of variation of the R-R interval in ECG (CVR-R = SD/MEAN x 100%). To evaluate R-R interval variations in ECG during dental treatment clearly, comparisons were made between subjects to whom atropine sulfate was administered (prior to treatment) and subjects to whom no drug was administered. In instances of which the subject experiences no unpleasant symptom (for instance, the fainting) during dental treatment, comparative examinations of R-R interval variations in ECG were made at various points during the course of therapy. In instances of which the fainting was induced, examinations of these variations were made during, before, and after the occurrence of the fainting. Results and Conclusions 1. In measuring R-R interval variations in ECG, maintaining stable heart rates and respiratory frequency and depth made it possible to evaluate parasympathetic activity during dental treatment. 2. Consistently low CVR-R values after administration of atropine sulfate clearly showed that patients treated in this way were in a state of parasympathetic blockade. 3. Patients to whom atropine sulfate was administered demonstrated higher values for systolic and diastolic blood pressure and for heart rate than controls: and their posttreatment recovery was slower. 4. Increasing age produced a correlative decrease in CVR-R during both the pretreatment rest period and immediately before treatment. 5. Systolic and diastolic blood pressure and heart rate increased at local anesthesia and maintained such levels until the end of treatment in no fainting cases, however, CVR-R increased just before the end of treatment. This finding leads to the assumption that, as a result of intensified sympathetic activity at the initial stage and the maintenance of this condition, parasympathetic activity increases just before the end of therapy to keep hemodynamic activity in balance.(ABSTRACT TRUNCATED AT 400 WORDS)

Effects of Laurus nobilis (Lauraceae) on Biomphalaria glabrata (Say, 1818).

Experiments were carried out using aqueous extracts from leaves and flowers of Laurus nobilis on Biomphalaria glabrata. Treatments were performed on blastula stage (+/- 15 h after first cleavage) and on adult snails (11-18 mm). In both instances they were exposed for 24 h to different concentrations of the extracts on snails (200 to 2500 ppm) and embryos (20 to 300 ppm) at 25 +/- 1 degree C. The embryos were observed for a period of 20 days after treatment and the snails for 10 days. Results obtained with leaf aqueous extracts have shown a degree of toxicity on embryos starting at a concentration of 125 ppm, the flower extract being effective at 35 ppm. The malformation obtained with the different concentrations falls into the unespecific type category, however some cephalic and shell malformations were found in embryos treated with concentrations over 50 ppm (leaves) and 25 ppm (flowers). The LD90 on adult snails obtained by treatments with flower and leaf extract was observed at concentrations of 340 ppm and 1900 ppm respectively.