In vitro anti-leukemia, antioxidant, and anti-inflammatory properties of Lantana camara.

It has been demonstrated that Lantana camara possesses several therapeutic properties that can be used to treat various human diseases, including dermatological and gastrointestinal conditions, tetanus, malaria, and tumours. In this investigation, every collected part of L. camara was extracted with absolute methanol to examine its antioxidant capacity using the DPPH assay and its anti-leukemia activity on two AML cell lines, MOLM-13 and MV4-11. In addition, anti-inflammatory effectiveness was evaluated. The results show that extracts from various sections of L. camara have a significant ability to neutralize free radicals, as indicated by their EC50 values. Most of the extracts had values less than 100 µg/ml, with the flower extract having an even lower value of less than 50 µg/ml. Experiments on two AML cell lines showed that the anti-leukemia effects of the extracts were remarkable, with the most potent impact belonging to the root extract (IC50 was 9.78 ± 0.61 and 12.48 ± 1.69 for MOLM-13 and MV4-11 cell lines). The antitumor effect of the extracts was determined to be time- and dose-dependent and did not correlate with antioxidant capacity. Furthermore, when BJ cells were exposed to L. camara root and leaf extracts, their migratory potential was dramatically reduced compared to untreated cells. The extracts demonstrated potential anti-inflammatory capabilities by lowering NO production in LPS-induced BJ cells.

Relation of pharmacological and behavioral effects of a hallucinogenic amphetamine to distribution in cat brain.

The hallucinogen 2,5-dimethoxy,-4-methylamphetamine, also known as STP, accumulates in specfic areas of cat brains. The unchanged compound was detected in the brain for at least 6 hours, whereas its behavioral effects lasted for about 4 hourS. The coincidental pharmacological and behavioral effects of the compound apparently indicate a relation between the anatomical distribution and action.

Antifungal effect of gaseous nitric oxide on mycelium growth, sporulation and spore germination of the postharvest horticulture pathogens, Aspergillus niger, Monilinia fructicola and Penicillium italicum.

AIM: To evaluate the antifungal activity of nitric oxide (NO) against the growth of the postharvest horticulture pathogens Aspergillus niger, Monilinia fructicola and Penicillium italicum under in vitro conditions. METHODS AND RESULTS: Different volumes of NO gas were injected into the Petri dish headspace to obtain the desired concentrations of 50-500 microl l(-1). The growth of the fungi was measured for 8 days of incubation in air at 25 degrees C. All concentrations of NO were found to produce an antifungal effect on spore germination, sporulation and mycelial growth of the three fungi, with the most effective concentration for A. niger and P. italicum being 100 and 500 microl l(-1) for M. fructicola. CONCLUSIONS: Short-term exposure to a low concentration of NO gas was able to inhibit the subsequent growth of A. niger, M. fructicola and P. italicum. SIGNIFICANCE AND IMPACT OF THE STUDY: NO gas has potential use as a natural fungicide to inhibit microbial growth on postharvest fruit and vegetables.

Haloperidol. Plasma levels and prolactin response as predictors of clinical improvement in schizophrenia: chemical v radioreceptor plasma level assays.

The relationship between clinical response of schizophrenic patients to haloperidol and (1) blood levels of the medication, determined by both gas-liquid chromatography (GLC) and radioreceptor (RR) assays, or (2) prolactin response to the medication, was examined in an inpatient study using several fixed doses of haloperidol. Regression analysis disclosed a substantial curvilinear relationship between steady-state GLC-determined plasma haloperidol levels and decrease in Brief Psychiatric Rating Scale (BPRS) Psychosis factor scores; however, no substantial relationship was found between clinical response and RR plasma haloperidol levels or serum prolactin response to haloperidol. Our results suggest that steady-state plasma levels of haloperidol determined by the GLC chemical assay are a better predictor of decreases in BPRS Psychosis factor scores than RR assayed plasma haloperidol levels or prolactin response to haloperidol.

Effects of neuroleptics on platelet monoamine oxidase activity.

Platelet MAO activity in schizophrenics was significantly decreased, by about 15%, after 3 weeks of treatment with haloperidol. Treatment with thioridazine or butaperazine also tended to decrease platelet MAO activity. The neuroleptic-induced decrease began to appear within a few days of treatment and did not show tolerance over 1-2 months of treatment with haloperidol. Platelet MAO activity of schizophrenic patients measured during drug-free base-line was not significantly different from that of normal controls, but MAO activity of schizophrenics was significantly lower than normals after 3 weeks of treatment with neuroleptics. The extent of decrease in platelet MAO activity correlated negatively with base-line prolactin and its increase after 24 hr. With PEA as substrate, the decrease in activity correlated positively with steady state plasma haloperidol.

Anxiety and platelet MAO levels after relaxation training.

The authors measured platelet MAO activity with phenylethylamine and tryptamine substrates in a group of 20 subjects with chronic anxiety before and after they underwent relaxation training. Levels of anxiety were quantified using a self-rating scale. Posttreatment values for anxiety and enzyme activity were significantly lower than pretreatment values. Anxiety and enzyme activity levels were not significantly correlated at any stage of the study.

The effects of (-)-delta9-tetrahydrocannabinol on reserpine-induced hypothermia in rats.

1. An intravenous injection into rats of 1 mg/kg (-)-Delta(9)-tetrahydrocannabinol Delta(9)-THC) had no effect on rectal temperature and produced in the subcellular fractions of the brain a shift of 5-hydroxytryptamine (5-HT) from the particulate or ;bound' 5-HT to the supernatant or ;free' fraction, whereas the noradrenaline (NA) decreased in both fractions.2. Pretreatment of rats by an intravenous injection of 1 mg/kg Delta(9)-THC three times a week for four weeks, prevented the hypothermia and the reduction in brain 5-HT produced by an intraperitoneal injection of 15 mg/kg reserpine given 24 h after the last Delta(9)-THC injection.3. Pretreatment of rats by a single intravenous injection of 1 mg/kg Delta(9)-THC prevented the hypothermia and reduction in brain 5-HT produced by an intraperitoneal injection of reserpine given 1 h before. The reduction in brain NA was not prevented except at the 18 h time interval.4. An injection of 1 mg/kg Delta(9)-THC intravenously into rats 3 h after an intraperitoneal injection of reserpine accentuated the reserpine hypothermia as well as the reduction of 5-HT but not of NA in the brain.5. The reserpine hypothermia was not prevented by a single intravenous injection of 1 mg/kg Delta(9)-THC when cinanserin, a 5-HT inhibitor, was injected 30 min before the reserpine.

MAO, DBH and COMT: the effect of anxiety.

Anxiety, a common accompaniment of depression, can be a source of confusion in affective disorder research. The present study examined the effect of anxiety on platelet monoamine oxidase, RBC catechol-0-methyltransferase, and serum dopamine-beta-hydroxylase-enzymes frequently implicated in affective disorders. Levels of anxiety, plasma catecholamines and the enzymes mentioned above were quantified in groups of anxious subjects and mentally and physically healthy controls. Anxious subjects were found to have significantly higher levels of blood plasma catecholamines and platelet monoamine oxidase. significant positive correlations were demonstrated between plasma catecholamines and platelet monoamine oxidase, while significant inverse correlations were found between trait anxiety and COMT, norepinephrine and DBH, and COMT and DBH

The discriminative stimulus properties of 2,5-dimethoxy-4-methylamphetamine (DOM): differentiation from amphetamine.

Rats were trained in a two-lever operant procedure to discriminate either 1.0 mg/kg (+)amphetamine or 1.5 mg/kg DOM from saline. Rats trained to discriminate DOM from saline showed generalization with the DOM training condition when tested with mescaline or 2,5-dimethoxy-4-ethylamphetamine (DOET), but not when tested with (+)amphetamine or methylphenidate. Both isomers of DOM generalized with racemic training compound, the (-)isomer being more potent. The DOM stimulus was completely blocked by the serotonin (5-HT) antagonists cinanserin and methysergide, but not by the peripheral 5-HT antagonist xylamidine nor the dopamine antagonist haloperidol. Rats trained to discriminate (+)amphetamine from saline generalized with the amphetamine training condition when tested with methylphenidate but not when tested with mescaline, DOET, racemic DOM, or either isomer of DOM. The amphetamine stimulus was blocked by pretreatment with haloperidol but not by cinanserin, methysergide, or xylamidine. The results show that, despite their structural similarity, amphetamine and DOM induce pharmacologically distinct stimuli.

Ultrastructural localization of LH-RH-immunoreactive synapses in the hamster accessory olfactory bulb.

Electron microscopic immunocytochemistry was used to localize luteinizing hormone-releasing (LH-RH) immunoreactivity within the male golden hamster accessory olfactory bulb. Two LH-RH-immunoreactive fiber populations were identified in the accessory olfactory bulb. A superficial system of immunoreactive axons was localized to the vomeronasal nerve and glomerular layers, and a periventricular system appeared in granule cell and periventricular layers. LH-RH-immunoreactive varicosities were observed to contain large reactive vesicles (80-120 nm) as well as a variable degree of cytoplasmic reaction product. Additionally, small vesicles with unreactive lumens and mitochondria were often present. Intravaricose segments of immunoreactive fibers invariably displayed fewer reactive vesicles than did varicosities. Within both glomerular and periventricular layers, some LH-RH-immunoreactive varicosities were observed to form asymmetric contacts characterized by prominent postjunctional densities. In the glomerular layer, these junctions could be identified as synaptic by several features. The presence of LH-RH-immunoreactivity in presynaptic elements supports a neuromodulatory role for LH-RH. As the accessory olfactory system is critically involved in the initiation of mating behavior of the male golden hamster, LH-RH-immunoreactive synapses in the accessory olfactory bulb may function to regulate reproductive behavior.

Periaqueductal gray neurons response to microiontophoretically injected morphine in naive and morphine-dependent rats.

The attempt of this study was to investigate the direct effects of increasing doses of morphine on the neuronal activity of the periaqueductal gray in morphine-naive and morphine-dependent rats. The microiontophoresis technique was used for this purpose. The four different responses induced by morphine exhibited dose-related patterns. Naloxone antagonized these responses in about 40% of the cases. Differences were found in the sensitivity of the neurons of morphine between naive and morphine-dependent rats. The phenomena of acute tolerance, chronic tolerance and dependence have been found. The results of this study indicate the presence of different neural populations in the periaqueductal gray in relation to their response to morphine, supporting the notion that subpopulations of opiate receptors exist within this brain area.

Inhibition of brain choline acetyltransferase by tetraplatin.

Tetraplatin inhibited choline acetyltransferase (CAT) from rat and bovine brain with I50 values of 13.5 and 40 microM, respectively. At 0.5 mM concentration, tetraplatin exhibited inhibition of the rat brain enzyme by 89%, whereas cisplatin yielded only 18% inhibition. With bovine CAT, tetraplatin showed noncompetitive inhibition with the substrate choline, Km 337 microM, Ki 29 microM, Vmax 2.83 nmoles acetylcholine formed/min/mg protein, and competitive inhibition with the substrate acetyl-CoA, Km 21 microM, Ki 16 microM, Vmax 3.85 nmoles acetylcholine formed/min/mg protein.

Correlation between plasma cortisol and CSF catecholamines in endogenous depressed dexamethasone nonsuppressors.

Nineteen endogenous depressive in-patients (13 with major depression and 6 with bipolar disorder-depressed) and 10 other patients with dysthymic disorder serving as the control group were given the dexamethasone suppression test (DST, 1 mg/subject). The results showed that the DST sensitivity in endogenous depressives was 73.7% and the specificity was 90%. After the patients were treated daily for 6 weeks with 150-200 mg imipramine, 88.9% of those endogenous depressive patients who previously had a positive DST response exhibited a negative response. Moreover, a significantly negative correlation was found between the CSF norepinephrine level and the pre-dexamethasone 4 p.m. plasma cortisol level in those endogenous depressed patients who had a positive DST response. Pre-treatment data also showed that the 4 p.m. plasma cortisol had a significant negative correlation with CSF dopamine. These findings suggest that endogenous depression with positive DST could be related not only to a lower norepinephrine level, but also to a lower dopamine level.

The residual effect of chronic neuroleptic treatment on the neuroleptic binding assay in rats.

Chronic chlorpromazine administration to rats (25 mg/Kg/day) for 30 days followed by a washout period of 10 days resulted in an increase in both the measured maximum number of binding sites, Bmax, and the apparent dissociation constant, Kd, for the binding of 3H-spiroperidol to neural membranes of the brain. When membrane suspensions were progressively diluted before the binding assay, it was found that the apparent Bmax did not change with dilution, remaining higher in membranes of chlorpromazine-treated rats than in controls. The apparent increase in Kd, on the other hand, was found to be an artifact of the assay. Thus extrapolation of the measured or apparent Kd value to infinite dilution resulted in identical value for Kd regardless of the treatment.

Cholinesterase enzymes in the blood of patients with Alzheimer's disease.

Plasma pseudocholinesterase activity was about 100% higher in patients with Alzheimer's type dementia than in similar age controls. Red cell acetylcholinesterase activity tended to be lower in patients than controls. Administration of lecithin substantially increased plasma choline levels but did not alter activity of either of the cholinesterase enzymes.

Video compression of coronary angiograms based on discrete wavelet transform with block classification.

A new method of video compression for angiographic images has been developed to achieve high compression ratio (~20:1) while eliminating block artifacts which leads to loss of diagnostic accuracy. This method adopts motion picture experts group's (MPEGs) motion compensated prediction to takes advantage of frame to frame correlation. However, in contrast to MPEG, the error images arising from mismatches in the motion estimation are encoded by discrete wavelet transform (DWT) rather than block discrete cosine transform (DCT). Furthermore, the authors developed a classification scheme which label each block in an image as intra, error, or background type and encode it accordingly. This hybrid coding can significantly improve the compression efficiency in certain eases. This method can be generalized for any dynamic image sequences applications sensitive to block artifacts.

Various inputs modify caudate neuronal activity.

This study investigates the input of substantia nigra (SN), dorsal raphe (DR), and medial lemniscus (ML) on caudate nucleus (CN) neurons as well as a non-specific-polysynaptic input (acoustic AC). Ninety-one units demonstrating spontaneous activity were recorded extracellularly using anesthetized rats. SN, DR, ML, and AC stimulation altered the spontaneous discharges in 79%, 90%, 86%, and 85% of the CN neurons, respectively. Only ML stimulation elicited patterns of time-locked responses in 16% of the CN units. The CN neurons showed high convergence to the four types of stimulation. Based on these results, interconnections and interrelations between SN, DR, ML, and the CN are suggested.

Depression, antidepressants, and plasma DBH.

Plasma levels of dopamine-beta-hydroxylase (DBH) were determined in 16 unmedicated patients with major depressive episodes (nonpsychotic) and in an equal number of normal subjects, before and after 4 weeks of treatment with tricyclic antidepressants. Some eight patients were treated with amitriptyline, and the remainder received desipramine. The controls remained medication free during the entire experimental period. Degrees of depression were quantified before and after treatment with the Hamilton Rating Scale of Depression (HRSD). There were no significant differences between the depressed patients and the controls on levels of DBH. Similarly, there were no within-group, pre-posttreatment differences on the enzyme levels in either group. Pre- and posttreatment HRSD scores did not correlate with corresponding plasma DBH levels. Plasma levels of amitriptyline, nortriptyline (product of amitriptyline in the body), and desipramine at the end of 4 weeks of treatment also failed to correlate with the enzyme levels.

Catechol-O-methyltransferase and catecholamines in anxiety and relaxation.

Levels of anxiety, plasma epinephrine and norpinephrine, and red blood cell (RBC) catechol-O-methyltransferase (COMT) activity were measured before and after 4 weeks of relaxation training in a group of 15 drug-free, anxious subjects and at a similar interval in a group of 15 drug-free, healthy controls. The index group showed significant decreases in levels of anxiety and plasma epinephrine and norepinephrine after treatment. No changes were observed in the control values. RBC COMT did not show any significant differences in activity between the index and control groups and between the pre- and posttreatment values. Similarly, COMT activity levels failed to correlate with levels of anxiety and catecholamines before or after treatment. These findings indicate that anxiety is unlikely to have an effect on RBC COMT activity, whereas it has a direct effect on plasma catecholamines.

Prolactin response to single and multiple doses of haloperidol in schizophrenic patients.

Serum prolactin and blood levels of haloperidol were assessed in schizophrenic patients after single acute oral doses of haloperidol and during fixed dose treatment with this medication. Although significant intrapatient correlations between prolactin responses to different doses of haloperidol were found, no statistically significant interpatient relationship between haloperidol dose and prolactin response emerged. There were statistically significant relationships between steady-state plasma and red cell haloperidol levels (measured by radioreceptor or gas liquid chromatographic techniques) and serum prolactin response, but not between blood levels after the acute haloperidol dose and prolactin response.