Two new isoquinoline alkaloids from Corydalis hendersonii / 中国中药杂志

Corydalis hendersonii(CH) is a Tibetan folk medicine with the functions of clearing heat, detoxifying, cooling blood, checking diarrhea, and lowering blood pressure. It is often used to treat high altitude polycythemia, vasculitis, peptic ulcer, and diarrhea. Nine compounds were separated from the ethanol extract of CH by silica gel, ODS, Sephadex LH-20 chromatography and semi-preparative HPLC. Their structures were identified as hendersine H(1),hendersine I(2), dehydrocheilanthifoline(3), protopine(4), izmirine(5), 6,7-methylenedioxy-1(2H)-isoquinolinone(6), icariside D_2(7), ethyl 4-(β-D-glucopyranosyloxy)-3-methoxybenzoate(8), 3-hydroxy-4-methoxybenzoic acid(9), respectively, by the spectroscopic data analysis and comparison with those in the literature. Among them, compounds 1 and 2 are new isoquinoline alkaloids, and compounds 7-9 are reported the first time for Corydalis. The hypoglycemic model of H9c2 cardiomyocytes and the inflammatory model of H9c2 cardiomyocytes induced by conditional supernatant were employed to determine the activities of the above compounds. The results showed that 20 μmol·L~(-1) compound 1 had a protective effect on H9c2 cardiomyocytes and 10 μmol·L~(-1) compounds 4 and 5 inhibited H9c2 cardiomyocyte inflammation induced by conditional supernatant.

Advances in chemical constituents of isoquinoline alkaloids from Nelumbo nucifera and their smooth muscle relaxation effect / 中国中药杂志

Lotus( Nelumbo nucifera) is a traditional medicinal plant,and nowadays it is regarded both as medicine and food. It is widespread across China and rich in natural resources. Almost every part of N. nucifera could be used for medical or edible purpose,including seeds( Lianzi),black ripe fruits( Shilianzi),seed coats( Lianyi),green embryos of mature seed( Lianzixin),flowers( Lianhua),stamens( Lianxu),receptacles( Lianfang),leaves( Heye),leaf or flower stalks( Hegeng),leaf bases( Heyedi),rhizomes( Ou) and rhizome nodes( Oujie). Therefore,this plant is praised as a commercial crop with great economic values. Isoquinoline type alkaloids are the main chemical components of lotus. Smooth muscles usually exist in the digestive tract,respiratory tract and vascular,urinary,reproductive and other human systems. Dysfunction of smooth muscle contraction will induce many diseases including hypertension,asthma and gastrointestinal disorder,etc.,and most of current therapeutic strategies rely on relaxation of smooth muscle by drugs.Previous studies have shown that alkaloids of lotus have strong relaxation activity on smooth muscle. The present paper reviews phytochemistry and smooth muscle relaxation activity of 59 isoquinoline alkaloids from N. nucifera through accessing CNKI,PubMed and multiple databases for biomedical sciences.

Hemodynamic responses during and after multiple sets of stretching exercises performed with and without the Valsalva maneuver

OBJECTIVE: This study investigated the acute hemodynamic responses to multiple sets of passive stretching exercises performed with and without the Valsalva maneuver. METHODS: Fifteen healthy men aged 21 to 29 years with poor flexibility performed stretching protocols comprising 10 sets of maximal passive unilateral hip flexion, sustained for 30 seconds with equal intervals between sets. Protocols without and with the Valsalva maneuver were applied in a random counterbalanced order, separated by 48-hour intervals. Hemodynamic responses were measured by photoplethysmography pre-exercise, during the stretching sets, and post-exercise. RESULTS: The effects of stretching sets on systolic and diastolic blood pressure were cumulative until the fourth set in protocols performed with and without the Valsalva maneuver. The heart rate and rate pressure product increased in both protocols, but no additive effect was observed due to the number of sets. Hemodynamic responses were always higher when stretching was performed with the Valsalva maneuver, causing an additional elevation in the rate pressure product. CONCLUSIONS: Multiple sets of unilateral hip flexion stretching significantly increased blood pressure, heart rate, and rate pressure product values. A cumulative effect of the number of sets occurred only for systolic and diastolic blood pressure, at least in the initial sets of the stretching protocols. The performance of the Valsalva maneuver intensified all hemodynamic responses, which resulted in significant increases in cardiac work during stretching exercises. .

Minimal endoscopic changes in non-erosive reflux disease / Alterações endoscópicas mínimas na doença do refluxo não erosiva

BACKGROUND: Gastroesophageal reflux disease is an increasingly common condition worldwide causing a considerable economic impact. More than half the patients with clinical symptoms of reflux disease display no mucosal erosions on esophagogastroduodenoscopy, making it impossible to confirm the diagnosis without further investigations. AIM: To evaluate the correlation between minimal endoscopic changes on white-light esophagogastroduodenoscopy (carditis, mucosal thickening and invisibility of vessels) and histologic changes observed in distal esophageal biopsies in a sample of patients with symptoms suggestive of reflux disease, and to verify the specificity of these symptoms for non-erosive reflux disease. METHODS: Retrospective, cross-sectional study based on information retrieved from a digital database at a Brazilian hospital for the period March-October, 2012. The sample consisted of previously untreated, non-smoking subjects aged >18 years with symptoms suggestive of reflux disease but no esophageal erosions, submitted to esophagogastroduodenoscopy and distal esophageal biopsy. RESULTS: The final sample included 23 subjects. The most frequently observed change was invisibility of vessels (n=21; 91.3%), followed by mucosal thickening (n=15; 65.2%) and carditis (n=5; 21.7%). The correlation coefficient between each variable and the anatomopathological diagnosis was 0.386 for body mass index, 0.479 for mucosal thickening, -0.116 for invisibility of vessels, 0.306 for carditis and 0.462 for hiatal hernia. CONCLUSION: All patients displayed minimal endoscopic changes on esophagogastroduodenoscopy, but only mucosal thickening revealed a moderately significant correlation with severity of esophagitis, although increased body mass index values and the presence of hiatal hernia were also associated. .

RACIONAL: Doença do refluxo gastroesofágico é condição cada vez mais comum em todo o mundo causando impacto econômico considerável. Mais da metade dos pacientes com sintomas clínicos da doença não apresentam erosões endoscópicas da mucosa, o que torna impossível confirmar o diagnóstico sem outras investigações. OBJETIVO: Avaliar a correlação entre mudanças mínimas endoscópicas em endoscopia digestiva alta de luz branca (cardite, espessamento da mucosa e invisibilidade de vasos) e as alterações histológicas observadas em biópsias distais de uma amostra de pacientes com sintomas sugestivos de doença do refluxo, e para verificar a especificidade desses sintomas para a doença não-erosiva. MÉTODOS: Estudo retrospectivo, transversal, com base em informações obtidas a partir de uma base de dados digital em um hospital brasileiro no período de março/outubro de 2012. A amostra foi composta por indivíduos não tratados previamente, não fumantes, >18 anos, com sintomas sugestivos de doença do refluxo, mas sem erosões esofágicas submetidos à endoscopia digestiva alta e biópsia de esôfago distal. RESULTADOS: A amostra final incluiu 23 indivíduos. A alteração mais frequente foi invisibilidade dos vasos (n=21; 91,3%), seguido por espessamento de mucosa (n=15; 65,2%) e cardite (n=5; 21,7%). O coeficiente de correlação entre cada variável e o diagnóstico anatomopatológico foi 0,386 para o índice de massa corporal, 0,479 para espessamento de mucosa, -0,116 para a invisibilidade de vasos, 0,306 para carditis e 0,462 para hérnia hiatal. CONCLUSÃO: Todos os pacientes apresentaram alterações endoscópicas mínimas, mas apenas espessamento da mucosa revelou correlação moderadamente significativa com a gravidade da esofagite, apesar do aumento dos valores no índice de massa corporal e da presença de hérnia hiatal também estarem associados. .

Metoclopramida e ondansetrona alteram o bloqueio neuromuscular induzido por mivacurio? - um estudo randomizado / Do metoclopramide and ondansetrone alter mivacurium-induced neuromuscular blockade? - a randomised trial / La metoclopramida y la ondansetrona alteran el bloqueo neuromuscular inducido por mivacurio? - un estudio aleatorizado

Experiência: Objetivamos investigar os efeitos de metoclopramida e ondansetrona no bloqueio neuromuscular por mivacúrio. Métodos: Foram incluídos no estudo 75 pacientes ASA I-II, com idades entre 18 e 65 anos e agendados para cirurgia eletiva necessitando de intubação traqueal. Os pacientes receberam metoclopramida 10 mg, ondansetrona 4 mg ou salina normal 5 mL; grupo M, grupo O e grupo SN (n = 25) respectivamente. Antes da anestesia, os medicamentos em estudo foram administrados em um volume de 5 mL. O nível de colinesterase plasmática foram obtidos antes e 5 minutos depois da administração dos medicamentos em estudo e 5 minutos depois da administração de mivacúrio. Os tempos até o início e os níveis T25, T75, T25-75 e T90 foram comparados entre si, tendo sido investigadas as diferenças entre cada paciente. Depois de registrar T90, o estudo foi terminado, tendo início a cirurgia. Resultados: O tempo até o início foi significativamente mais breve no Grupo M versus os outros dois grupos. O tempo até o início no Grupo O foi significativamente mais breve versus grupo SN. No grupo M, T25, T75, T90 e os índices de recuperação foram significativamente maiores versus Grupo NS (p < 0,001). No Grupo O, T25 e T75 foram maiores versus Grupo NS (p < 0,01 e p < 0,05,respectivamente). No Grupo M, T75, T90 e índices de retorno da anestesia foram significativamente maiores versus Grupo O (p < 0,001, p < 0,01, p < 0,001, respectivamente). Nos Grupos M e O, os níveis plasmáticos de colinesterase diminuíram significativamente (p < 0,001). Depois da administração dos medicamentos em estudo e de mivacúrio. Houve também redução na colinesterase plasmática no Grupo NS 5 minutos após a administração de mivacúrio (p < 0,001). ...

Background: We aimed to investigate the effects of metoclopramide and ondansetrone on mivacurium neuromuscular blockade. Methods: Seventy five, ASA I-II patients, aged 18-65 and scheduled for elective surgery requiring tracheal intubation were included in the study. The patients received metoclopramide 10 mg, ondansetrone 4 mg or normal saline 5 mL; group M, group O, group NS (n = 25), respectively. Before anesthesia study drugs were administered in a volume of 5 mL. The level of plasma cholinesterase were obtained before and 5 minutes after the administration of study drugs and5 minutes after the administration of mivacurium. Onset time, T25, T75, T25-75, T90 levelswere compared with each other and differences between each patients were investigated. After recording T90, the study was terminated and surgery was started. Results: Onset time was significantly shorter in group M, than the other two groups. Onset time in group O was significantly shorter than in group NS. In Group M T25, T75, T90 and recovery indices were significantly greater than in Group NS (p < 0.001). In Group O T25, T75 were greater than Group NS (p < 0.01 and p < 0.05, respectively). In Group M T75, T90 and emergence indices were significantly higher than Group O (p < 0.001, p < 0.01, p < 0.001, respectively). In Groups M and O, plasma cholinesterase levels decreased significantly (p < 0.001) after administration of study drugs and mivacurium. Plasma cholinesterase also was reduced in Group NS 5 minutes after the administration of mivacurium (p < 0.001). Conclusion: Ondansetrone is believed to be more reliable agent than metoclopramide when used with mivacurium. .

prospective, randomized, double-blind, comparative study of the efficacy of intravenous ondansetron and palonosetron for prevention of postoperative nausea and vomiting

Palonosetron is a second generation 5-Hydroxytryptamine-3 receptor antagonist with longer half life and higher receptor binding affinity than Ondansetron. To assess the efficacy and safety profile of intravenous palonosetron compared to the ondansetron for prevention of post-operative nausea and vomiting [PONV] under general anesthesia. A prospective, randomized, placebo-controlled, double-blind study was conducted in 90 patients aged 20-60 years, undergoing major surgeries. Group I [n=30] received placebo injection; Group II [n=30] received inj. ondansetron 8 mg and Group III [n=30] received inj. palonosetron 0.075 mg IV. In the operating room, the study drugs were given IV in equal volume of 4ml, before inducing the patients. In postoperative period each patient was observed for retching, nausea and/or vomiting at 30 min; and then at 1, 2, 6, 12 and 24 hours. Any side effects intra-operatively and post-operatively were recorded. The number of patients, who remained vomiting free in the first 24 hours after surgery was 56.6%, 80% and 86% in the placebo, Ondansetron and Palonosetron groups respectively. The difference with placebo was highly significant for ondansetron [p < 0.05], and highly significant for palonosetron [p=0.009]. The difference in vomiting between Ondansetron and Palaonosetron was not significant but the incidence of nausea was significantly less common in the Palonosetron group than the Ondansetron group [16.7% vs. 43.4%, p=0.006]. We conclude that the second generation 5-HT3 antagonist, palonosetron is significantly more effective against PONV than ondansetron. It has a particularly more pronounced and prolonged effect on postoperative nausea

Circadian and pharmacological regulation of casein kinase I in the hamster suprachiasmatic nucleus.

In mammals, the mechanism for the generation of circadian rhythms and entrainment by light-dark (LD) cycles resides in the hypothalamic suprachiasmatic nuclei (SCN), and the principal signal that adjusts this biological clock with environmental timing is the light:dark cycle. Within the SCN, rhythms are generated by a complex of molecular feedback loops that regulate the transcription of clock genes, including per and cry. Posttranslational modification plays an essential role in the regulation of biological rhythms; in particular, clock gene phosphorylation by casein kinase I , both epsilon (CKIepsilon) and delta (CKIdelta), regulates key molecular mechanisms in the circadian clock. In this paper, we report for the first time that CKI activity undergoes a significant circadian rhythm in the SCN (peaking at circadian time 12, the start of the subjective night), and its pharmacological inhibition alters photic entrainment of the clock, indicating that CKI may be a key element in this pathway.

In vitro brain tyrosine hydroxylase activation in catfish Heteropneustes fossilis (Bloch): seasonal changes in involvement of cAMP-dependent protein kinase A and Ca2+ -dependent protein kinase C.

In the present in vitro study, the involvement of cAMP dependent-protein kinase A (PKA) and calcium-dependent protein kinase C (PKC) in the regulation of forebrain (telencephalon and hypothalamus) tyrosine hydroxylase (TH) activity was demonstrated during the reproductive seasons of the female catfish H. fossilis. In the concentration studies conducted in prespawning phase, cAMP (0.05 nM, 0.5 nM, 1 mM and 2.0 mM) or the phosphodiesterase inhibitor isobutylmethylxanthine (IBMX-0.5-2.0 mM) stimulated enzyme activity. Likewise, the incubation of the enzyme preparations with the cAMP dependent-protein kinase A inhibitor H-89 (1 and 10 microM) and PKC inhibitor calphostin C (cal C; 1 and 10 microM) inhibited enzyme activity in a concentration-dependent manner. In seasonal studies, the incubation of the enzyme preparations with cAMP (1 mM), IBMX (1 mM), H-89 (10 microM) and cal-C (10 microM) produced season-dependent effects on enzyme activity. The stimulatory effect of cAMP and IBMX and the inhibitory effect of H-89 and cal C were greater in the resting and spawning phases. The results suggest the involvement of both signal transduction pathways in TH activation vis-à-vis catecholaminergic activity with a more dominant role by the cAMP-PKA pathway.

Protein kinase C micron plays an essential role in hypertonicity-induced heat shock protein 70 expression

Heat shock protein 70 (HSP70), which evidences important functions as a molecular chaperone and anti-apoptotic molecule, is substantially induced in cells exposed to a variety of stresses, including hypertonic stress, heavy metals, heat shock, and oxidative stress, and prevents cellular damage under these conditions. However, the molecular mechanism underlying the induction of HSP70 in response to hypertonicity has been characterized to a far lesser extent. In this study, we have investigated the cellular signaling pathway of HSP70 induction under hypertonic conditions. Initially, we applied a variety of kinase inhibitors to NIH3T3 cells that had been exposed to hypertonicity. The induction of HSP70 was suppressed specifically by treatment with protein kinase C (PKC) inhibitors (Go6976 and GF109203X). As hypertonicity dramatically increased the phosphorylation of PKC micron, we then evaluated the role of PKC micron in hypertonicity-induced HSP70 expression and cell viability. The depletion of PKC micron with siRNA or the inhibition of PKC micron activity with inhibitors resulted in a reduction in HSP70 induction and cell viability. Tonicity-responsive enhancer binding protein (TonEBP), a transcription factor for hypertonicity-induced HSP70 expression, was translocated rapidly into the nucleus and was modified gradually in the nucleus under hypertonic conditions. When we administered treatment with PKC inhibitors, the mobility shift of TonEBP was affected in the nucleus. However, PKC micron evidenced no subcellular co-localization with TonEBP during hypertonic exposure. From our results, we have concluded that PKC micron performs a critical function in hypertonicity-induced HSP70 induction, and finally cellular protection, via the indirect regulation of TonEBP modification.

Genital Sensory Stimulation Shifts Estradiol Intraoviductal Signaling from Nongenomic to Genomic Pathways, Independently from Prolactin Surges

Estradiol (E2) accelerates oviductal egg transport through nongenomic pathways involving oviductal protein phosphorylation in non-mated rats, and through genomic pathways in mated rats. Here we investigated the ability of cervico-vaginal stimulation (CVS) to switch the mode of action of E2 in the absence of other male-associated components. Pro-estrous rats were subjected to CVS with a glass rod and 12 hours later were injected subcutaneously with E2 and intrabursally with the RNA synthesis inhibitor Actinomycin D or the protein phosphorylation inhibitor H-89. The number of eggs in the oviduct, assessed 24 h later, showed that Actinomycin D, but not H-89 blocked the E2-induced egg transport acceleration. This clearly indicates that CVS alone, without other mating-associated signals, is able to shift E2 signaling from nongenomic to genomic pathways. Since mating and CVS activate a neuroendocrine reflex that causes iterative prolactin (PRL) surges, the involvement of PRL pathway in this phenomenon was evaluated. Prolactin receptor mRNA and protein expression in the rat oviduct was demonstrated by RT-PCR and Western blot, but their levels were not different on day 2 of the cycle (C2) or pregnancy (P2). Activated ST AT 5a/b (phosphorylated) was detected by Western blot on P2 in the ovary, but not in the oviduct, showing that mating does not stimulate this PRL signalling pathway in the oviduct. Other rats subjected to CVS in the evening of pro-estrus were treated with bromoergocriptine to suppress PRL surges. In these rats, H-89 did not block the E2-induced acceleration of egg transport suggesting that PRL surges are not essential to shift E2 signaling pathways in the oviduct. We conclude that CVS is one of the components of mating that shifts E2 signaling in the oviduct from nongenomic to genomic pathways, and this effect is independent of PRL surges elicited by mating.

Protein kinase A mediates microglial activation induced by plasminogen and gangliosides

In the injured brain, microglia is known to be activated and produce proinflammatory mediators such as interleukin-1beta (IL-1beta), tumor necrosis factor-alpha (TNF-alpha) and inducible nitric oxide synthase (iNOS). We investigated the role of protein kinase A (PKA) in microglial activation by both plasminogen and gangliosides in rat primary microglia and in the BV2 immortalized murine microglial cell line. Both plasminogen and gangliosides induced IL-1beta, TNF-alpha and iNOS mRNA expression, and that this expression was inhibited by the addition of the PKA inhibitors, KT5720 and H89. Both plasminogen and gangliosides activated PKA and increased the DNA binding activity of the cAMP response element- binding protein (CREB). Furthermore, KT5720 and H89 reduced the DNA binding activities of CREB and NF-kappaB in plasminogen-treated cells. These results suggest that PKA plays an important role in plasminogen and gangliosides- induced microglial activation.

Inhibition of thymidylate synthase by pergularinine, tylophorinidine and deoxytubulosine.

The activity of thymidylate synthase (TS) purified in our laboratory from Lactobacillus leichmannii was inhibited by pergularinine (PGL) and tylophorinidine (TPD) and deoxytubulosine (DTB) isolated from the Indian medicinal plants Pergularia pallida and Alangium lamarckii respectively. Cytotoxicity studies showed that cell growth of L. leichmannii was inhibited (IC50 = 40-45 microM) by all the three alkaloids, the concentrations > 80-90 microM resulting in complete loss of the enzyme activity. Ki values of the enzyme calculated from Lineweaver-Burk and Dixon plots for PGL, TPD and DTB were 10 x 10(-6) M, 9 x 10(-6) M and 7 x 10(-6) M respectively. These are typed as 'non-competitive' inhibitors of TS. All the three alkaloids inhibited (IC50 = 50 microM) the elevated TS activity of leukocytes in cancer patients with clinically diagnosed chronic myelocytic leukemia (n = 10), acute lymphocytic leukemia (n = 8) and metastatic solid tumours (n = 3).

Alcaloides isoquinolínicos de la corteza y flores de Erythrina fusca Loureiro / Isoquinolinic alcaloids from the bark and flowers of the Erythrina fusca Loureiro

De la corteza y flores de Erythrina fusca Loureiro se aislaron los alcaloides isoquinolínicos (+) -epieritratidina y 8-(+)-oxoerisodina, los cuales fueron identificados con base en sus constantes espectroscópicas. Se determinó la actividad antimicrobiana de extractos crudos y fracciones frente a bacterias y hongos. Se evaluó la actividad farmacólogica de extractos crudos y fracciones frente a ratas tipo WISTAR

Neuromuscular and hemodynamic effects of mivacurium and succinylcholine in adult patients during nitrous oxide-propofol-fentanyl anesthesia

The neuromuscular and hem+odynamic effects of mivacurium 0.15 mg/kg and succinylcholine 1 mg/kg were compared in 26 adult patients (ASA I and II) during nitrous oxide-oxygen-propofol-fentanyl anesthesia. Neuromuscular block was monitored by recording the compound electromyogram of the hypothenar muscle resulting from supramaximal train-of-four stimuli applied to the ulnar nerve. Time to onset of over 95% block and duration to 25% recovery of control twitch after injection of mivacurium were significantly longer than for succinylcholine (201 +/- 37.6 vs 54 +/- 5.2 sec and 13.0 +/- 2.2 vs 8.4 +/- 2.1 min; mean +/- SD). Onset of mivacurium with priming technique was shortened (125 +/- 20.7 sec), but was also slower than that of succinylcholine. Although the recovery index during spontaneous recovery was significantly longer for mivacurium than for succinylcholine (6.9 +/- 1.3 vs 5.1 +/- 0.9 min), antagonism with neostigmine at 25% recovery of twitch height sufficiently facilitated the recovery index of mivacurium (4.5 +/- 1.0 min) to a level similar to that of succinylcholine with no statistical difference. The hemodynamic effects of mivacurium were few as compared to those of succinylcholine. In conclusion, mivacurium is considered to have additional advantages for short procedures when succinylcholine is undesirable.

Effects of central epinephrine synthesis inhibition on stress-induced prolactin secretion in male rats

1. The present study was designed to examine the role of central epinephrine pathways in the control of stress-induced prolactin secretion in male adulto Wistar rats. 2. Intracerebroventricular adminsitration of two epinephrine synthesis inhibitors, SKF64139 (5 and 10 µg/rat) and LY 134046 (10 and 20 µg/rat), 6 h before the onset of immobilization stress blocked prolactin secretion in a dose-dependent manner. Prolactin values before stress were about 4.0 ng/ml and increased to almost 50 ng/ml in the control group. SKF 64139 injection in the higher dose (10 µg/rat) induced a complete blockade of the stress-induced prolactin release, whereas partial blockade was observed after the higher dose (20 µg/rat) of LY 134046. 3.Salbutamol pretreatment (10 µg/rat) completely restored stress-induced prolactin secretion in animals receiving a central injection of both epinephrine synthesis inhibitors under the same conditions as described above. 4. It is suggested that epinephrine pathways in the brain play an important role in the control of prolactin release occuring during immobilization stress

Bloqueadores neuromusculares: novas opçöes clínicas / Neuromuscular blocking agents: new options

Säo apresentados dois novos bloqueadores neuromusculares, atracúrio e vecurônio, ambos do tipo näo-despolarizante. Praticamente desprovidas de efeitos cardiovasculares, estas drogas säo de eliminaçäo plasmática mais rápida que o pancurônio e podem ser empregadas em técnicas de infusäo contínua. Embora näo substituam completamente a succinilcolina, tendem a fazer diminuir a freqüência do seu uso para obtençäo de paralisia muscular para intubaçäo traqueal ou procedimentos de curta duraçäo

Estudio comparativo entre el atracurium y el pancuronio en niños anestesiados / Comparative study between atracurion and pancuroniun in chidren under anesthesia

Se realizó un estudio prospectivo en el cual se analizó comparativamente la conducta clínica de dos bloqueadores neuromusculares no depolarizantes (pancuronio y atracurium), en un grupo de 62 niños sometidos a cirugía programada, bajo anestesia analgésica a base de fentanyl. Se observó su influencia sobre la frecuencia cardiaca, tensión arterial y presión ocular, a una dosis de 80 mcgrs. de pancuronio y 600 mcgr. de atracurium, ambos por Kg. de peso. Se analizó el tiempo de latencia y de acción, así como la presencia de efectos indeseables. Las cifras basales de frecuencia cardiaca y tensión arterial con ambos relajantes musculares no sufrieron cambios con significación estadística en el periodo inductivo. Durante el transanestésico hubo decremento significativo de la frecuencia cardiaca y tensión arterial en el grupo al que se le administró atracurium, posiblemente debido a la influencia del fentanyl y al término del tiempo de acción del bloqueador neuromuscular. Se observó también que la presión ocular no sufrió cambios significativos en el grupo del pancuronio, sin embargo el grupo de atracurium incrementó discretamente la presión ocular

Alterations of the surface tegument of Opisthorchis viverrini exposed to praziquantel in vitro and in vivo.

The in vitro and in vivo effects of praziquantel on the ultrastructural surface of Opisthorchis viverrini were investigated using scanning electronmicroscopy. For the in vitro study, adult flukes were collected from experimentally infected hamsters, and were incubated for various time intervals at 37 degrees C in Earle's basal medium containing praziquantel at final concentrations of 0.01-100 micrograms/ml. For the in vivo study, flukes were collected from the biliary system of experimentally infected hamsters that had been treated 4 hours previously with 350 mg of praziquantel per kg body weight (mg/kg). Flukes were also obtained from the feces of a patient with opisthorchiasis who had been given praziquantel once at a dose of 40 mg/kg 4-6 hours previously and from the bile of a patient at the time of operation 24 hours after praziquantel treatment. Scanning electronmicroscopic analyses of the surface teguments of flukes exposed to praziquantel either in vitro or in vivo showed similar changes. Tegumental bubbles of different sizes appeared on the surface; they later ruptured and resulted in the formation of crater-like lesions. These lesions might be so extensive as to result in the peeling of the entire areas. On occasions, "micronodules" appeared later in these areas and those at the periphery of the lesions; these micronodules may represent an attempt by the worm to regenerate new tegument. The possibility that these ultrastructural changes may represent a generalized response of the tegumental surface to an obnoxious agent was discussed.