Clinical effect of pidotimod oral liquid as adjuvant therapy for infectious mononucleosis / 中国当代儿科杂志

<p><b>OBJECTIVE</b>To study the clinical effect of pidotimod oral liquid as adjuvant therapy for infectious mononucleosis and its effect on T lymphocyte subsets.</p><p><b>METHODS</b>A total of 76 children with infectious mononucleosis, who were admitted to the hospital between July 2016 and June 2017, were enrolled and randomly divided into two groups: conventional treatment and pidotimod treatment (n=38 each). The children in the conventional treatment group were given antiviral therapy with ganciclovir for injection and symptomatic treatment. Those in the pidotimod treatment group were given pidotimod oral liquid in addition to the treatment in the conventional treatment group. The course of treatment was two weeks for both groups. The two groups were compared in terms of the recovery of clinical indices and the changes in peripheral blood T lymphocyte subsets.</p><p><b>RESULTS</b>Compared with the conventional treatment group, the pidotimod treatment group had significantly shorter fever clearance time, time to the disappearance of isthmopyra, time to the relief of lymph node enlargement, time to the relief of hepatosplenomegaly, and length of hospital stay (P<0.05). After treatment, the pidotimod treatment group had significant reductions in the percentages of CD3 and CD8 T cells and had significantly lower percentages of CD3 and CD8 T cells than the conventional treatment group (P<0.001). The pidotimod treatment group had significant increases in the percentage of CD4 T cells and CD4/CD8 ratio after treatment, which was significantly higher than those in the conventional treatment group (P<0.001). The conventional treatment group had no significant changes in T lymphocyte subsets after treatment (P>0.05).</p><p><b>CONCLUSIONS</b>Pidotimod oral liquid has a good clinical effect as the adjuvant therapy for infectious mononucleosis and can improve cellular immune function, so it holds promise for clinical application.</p>

Pidolate de magnésium dans la prévention des AVC. A propos de 60 cas à l'Institut Cœur de Grâce en Côte d'Ivoire

L'hypertension artérielle (HTA) représente une cause fréquente de consultation dans les pays en voie de développement. Elle est pourvoyeuse de complications neurologiques de type encéphalopathie hypertensive et accident vasculaire cérébral ischémique transitoire (AIT).L'objectif de cette étude était de d'évaluer l'efficacité synergique de l'association Pidolate de Magnésium et traitement antihypertenseur chez les patients hypertendus suivis à l'institut cœur de grâce (ICG) à Cocody Danga.Patients et méthodes : Il s'agit d'une étude randomisée, prospective portant sur 60 patients hypertendus tirés au sort. Le premier groupe de patients concernait ceux qui avaient reçu du pidolate de magnésium en association à un traitement antihypertenseur, le second groupe servant de témoin n'avait reçu que le traitement antihypertenseur. Le test de Chi carré et le test de Fisher exact ont été appliqués. Le seuil de signification (p < 0.05) ; l'odds ratio, les valeurs de tendance centrale et l'écart-type ont été calculés. Le logiciel EPI-INFO a permis d'analyser les données.Résultats : Dans cette étude, il n'y a pas de différence significative au niveau du sexe (p = 0,398) entre les deux groupes de population. Globalement la moyenne d'âge était de 51,7 ans ± 11 (extrêmes 32 et 76 ans). Spécifiquement dans le groupe 1 avec la supplémentation magnésique, la moyenne d'âge était de 51,9 ans ± 11 (extrêmes 36 et 73 ans) et dans le groupe 2 sans magnésium la moyenne d'âge était de 51,5 ans ± 11 (extrêmes 32 et 76 ans). Il n'y avait pas de différence significative (p = 0,889). Les tranches d'âges étaient harmonieusement réparties (Chi2 = 0,309 et p = 0,856). La répartition des patients en fonction des étiologies était équitable entre les deux groupes (Test de Fischer exact p = 0,397) avec distribution harmonieuse des patients ayant présenté une encéphalopathie hypertensive (12 patients versus 14) et une HTA sévère (18 patients versus 16) et aucune différence significative n'a été observée entre les deux groupes (OR = 0,7619 ; IC 95% [0,2737­2,12] p = 0,39). Nous constatons dans cette étude que la supplémentation magnésique au traitement anti-hypertensif a eu un effet bénéfique, donc un rôle protecteur contre la survenue d'accident vasculaire cérébral ischémique. Le bénéfice cardiovasculaire s'est avéré supérieur à celui que l'on pouvait imputer à la baisse de la pression artérielle (Test de Fischer exact p = 0,000003).Conclusion : Ces résultats plaident fortement pour l'importance du pidolate de magnésium dans la prise en charge de l'hypertension artérielle

The modular nature of bradykinin-potentiating peptides isolated from snake venoms

Bradykinin-potentiating peptides (BPPs) are molecules discovered by Sergio Ferreira - who found them in the venom of Bothrops jararaca in the 1960s - that literally potentiate the action of bradykinin in vivo by, allegedly, inhibiting the angiotensin-converting enzymes. After administration, the global physiological effect of BPP is the decrease of the blood pressure. Due to this interesting effect, one of these peptides was used by David Cushman and Miguel Ondetti to develop a hypotensive drug, the widely known captopril, vastly employed on hypertension treatment. From that time on, many studies on BPPs have been conducted, basically describing new peptides and assaying their pharmacological effects, mostly in comparison to captopryl. After compiling most of these data, we are proposing that snake BPPs are 'modular' peptidic molecules, in which the combination of given amino acid 'blocks' results in the different existing peptides (BPPs), commonly found in snake venom. We have observed that there would be mandatory modules (present in all snake BPPs), such as the N-terminal pyroglutamic acid and C-terminal QIPP, and optionalmodules (amino acid blocks present in some of them), such as AP or WAQ. Scattered between these modules, there might be other amino acids that would 'complete' the peptide, without disrupting the signature of the classical BPP. This modular arrangement would represent an important evolutionary advantage in terms of biological diversity that might have its origins either at the genomic or at the post-translational modification levels. Regardless of the modules' origin, the increase in the diversity of peptides has definitely been essential for snakes' success on nature.(AU)

Prise en charge de la pré-éclampsie : le pidolate de magnésium injectable peut-il être une alternative au sulfate de magnésium dans les pays à ressources limitées ?

Introduction : La pré-éclampsie et ses complications représentent la deuxième cause de mortalité maternelle dans notre pays. L'administration de magnésium sulfate en IV est la référence du traitement médical, mais le pidolate de magnésium par voie IM peut être une alternative. Méthodes : Il s'agissait d'une étude prospective, comparative, randomisée en double aveugle, menée de janvier 2015 à décembre 2015 à la maternité du centre hospitalo-universitaire (CHU) de Cocody-Abidjan. Tous les cas de pré-éclampsie modérée, soit une pression artérielle systolique ≥ 140 mmHg et une pression artérielle diastolique ≥ 90 mmHg, associée à une protéinurie à 300 mg chez des gestantes porteuses d'une grossesse à 37 semaines d'aménorrhée (SA), ont été retenus (n = 136). Ces gestantes ont été réparties en deux groupes de 68 cas et ont été suivies régulièrement dans l'attente de la décision d'accouchement. Cette surveillance hospitalière comportait, outre un examen obstétrical et général complet, un contrôle horaire systématique de la pression artérielle (PA) et la recherche de la protéinurie aux bandelettes réactives jusqu'à l'accouchement. Le premier groupe de gestantes représentait les cas et a reçu un traitement au pidolate de magnésium injectable (Mag injectable 0,8%®) à raison de 244,2mg de magnésium par jour, réparti en 3 injections intramusculaires (IM) d'une ampoule de 10ml contenant 81,4mg de magnésium, chaque 8 heures. Aux gestantes du 2e groupe, qui représentaient le groupe témoin, il a été prescrit un traitement par le sulfate de magnésium injectable, selon le protocole de l'OMS, soit en traitement d'attaque : 14g en dose de charge répartie de la manière suivante : 10g en IM dont 5g dans chaque fesse et 4g en IV, puis en traitement d'entretien : 1g en IV après chaque 4h jusqu'à l'accouchement. Lorsque persistaient les signes de gravité, la césarienne ou le déclenchement artificiel du travail étaient immédiatement décidés. Ces gestantes ont, parallèlement, reçues un traitement antihypertenseur. L'analyse statistique a consisté en une comparaison de l'issue de la grossesse et la survenue de complications aiguës materno-fœtales de la pré-éclampsie. Le test du khi deux au seuil de signification fixé à 5% (p<0,05) et le t-Student ont été utilisés pour la comparaison des effectifs.Résultats : Nous n'avons pas observé de différence significative concernant l'apparition de complications maternelles (éclampsie, hématome rétro placentaire et HELLP syndrome), ou de complications fœtales (petit poids de naissance, mort fœtale in utero et mauvais score d'Apgar), entre les 2 groupes. Conclusion : Le pidolate de magnésium par voie IM est aussi efficace dans la prévention de la crise d'éclampsie que le magnésium sulfate. Il présente, en outre, l'avantage de sa meilleure disponibilité, d'une facilité d'emploi et d'un coût faible

Case report of acquired pyroglutamic acidemia in a pediatric patient

Pyroglutamic acid (also known as 5-oxoproline) is an organic acid intermediate of the gamma-glutamyl cycle. Accumulation of pyroglutamic acid is a rare cause of high anion gap metabolic acidosis. In the pediatric population, the congenital form of pyroglutamic acidemia has been extensively described. However, there are scarce reports of the acquired form of this condition in children. The urine test for organic acids confirms the diagnosis of pyroglutamic acidemia. We report the case of a 16-month-old girl who developed transient 5-oxoprolinemia associated with malnutrition and the use of acetaminophen and ampicillin for the treatment of acute otitis media and abdominal pain. The patient received 21-hour course of n-acetylcysteine with improvement of metabolic acidosis. This report highligts the need of considering pyroglutamic acidemia in the differencial diagnosis for high anion gap metabolic acidosis in pediatric patients with malnutrition and other risk factors...

Late Outcome of a Randomized Study on Oral Magnesium for Premature Complexes / Evolução Tardia de Estudo Randomizado com Uso de Magnésio Via Oral em Extrassístoles Sintomáticas

Background: Ventricular and supraventricular premature complexes (PC) are frequent and usually symptomatic. According to a previous study, magnesium pidolate (MgP) administration to symptomatic patients can improve the PC density and symptoms. Objective: To assess the late follow-up of that clinical intervention in patients treated with MgP or placebo. Methods: In the first phase of the study, 90 symptomatic and consecutive patients with PC were randomized (double-blind) to receive either MgP or placebo for 30 days. Monthly follow-up visits were conducted for 15 months to assess symptoms and control electrolytes. 24-hour Holter was performed twice, regardless of symptoms, or whenever symptoms were present. In the second phase of the study, relapsing patients, who had received MgP or placebo (crossing-over) in the first phase, were treated with MgP according to the same protocol. Results: Of the 45 patients initially treated with MgP, 17 (37.8%) relapsed during the 15-month follow-up, and the relapse time varied. Relapsing patients treated again had a statistically significant reduction in the PC density of 138.25/hour (p < 0.001). The crossing-over patients reduced it by 247/hour (p < 0.001). Patients who did not relapse, had a low PC frequency (3 PC/hour). Retreated patients had a 76.5% improvement in symptom, and crossing-over patients, 71.4%. Conclusion: Some patients on MgP had relapse of symptoms and PC, indicating that MgP is neither a definitive nor a curative treatment for late follow-up. However, improvement in the PC frequency and symptoms was observed in the second phase of treatment, similar to the response in the first phase of treatment. .

Fundamento: Extrassístoles (ES) ventriculares e supraventriculares são frequentes e muitas vezes sintomáticas. Segundo estudo prévio, a administração de pidolato de magnésio (PMg) a pacientes sintomáticos pode resultar na melhora da densidade das ES e dos sintomas relacionados. Objetivo: Avaliar os resultados dessa intervenção clínica inicial no seguimento tardio de pacientes recebendo PMg ou placebo. Métodos: Noventa pacientes com ES, sintomáticos e consecutivos foram randomizados (duplo-cego) para receber PMg ou placebo por 30 dias. Visitas mensais de seguimento (15 meses) foram realizadas para avaliar a sintomatologia e controlar eletrólitos. O Holter de 24 horas foi realizado sempre que sintomáticos, ou duas vezes, independentemente dos sintomas. Na segunda fase do estudo, os pacientes cujos sintomas recidivassem, seja do grupo PMg ou placebo (crossing over), receberam PMg seguindo-se o mesmo protocolo. Resultados: Dos 45 pacientes que receberam inicialmente o PMg, 17 (37,8%) apresentaram recidiva dos sintomas em tempo variável nos 15 meses. Os pacientes com recidiva e tratados uma segunda vez apresentaram redução estatisticamente significante na densidade de ES de 138,25/hora (p < 0,001). Os pacientes de crossing reduziram em 247/hora (p < 0,001). Nos pacientes que não apresentaram recidiva, a frequência de ES foi baixa (3 ES/hora). A melhora dos sintomas foi de 76,5% nos retratados e de 71,4% nos de crossing. Conclusão: Houve recorrência de sintomas e das ES em alguns pacientes que usaram PMg, deixando claro não ser essa uma forma de tratamento definitivo ou curativo no seguimento tardio. Contudo, houve também melhora na frequência de ES e de sintomas em uma segunda etapa de tratamento, semelhante à resposta na primeira etapa. .

Studies on chemical constituents from fruits of Morus alba L / 药学学报

Chemical investigation of fruits of Mours alba L. lead to the isolation of fifteen compounds by various chromatographies such as silica gel, Sephadex LH-20, RP-C18 column chromatography. Their structures were determined to be: 1-[5-(2-formlfuryl) methyl] dihydrogen 2-hydroxypropane-1, 2, 3-tricarboxylate 2, 3-diethyl ester (1), 1-[2-(furan-2-yl)-2-oxoethyl] pyrrolidin-2-one (2), divaricataester A (3), methyl 1-[2-(furan-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carboxylate (4), 1-[2-(furan-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carboxylic acid (5), L-pyroglutamic acid (6), L-pyroglutamic acid ethyl ester (7), 3-O-caffeoylquinic acid methyl ester (8), 3-O-caffeoylquinic acid ethyl ester (9), 5-O-caffeoylquinic acid methyl ester (10), 5-O-caffeoylquinic acid ethyl ester (11), 4-O-caffeoylquinic acid methyl ester (12), 4-O-caffeoylquinic acid methyl ester (13), 4-O-caffeoylquinic acid (14), 3-O-caffeoylquinic acid (15), respectively, based on the spectral analysis such as NMR, MS etc. Compounds 1-14 were isolated from this genus for the first time, among which 1 was a new compound.

Redução da densidade de extrassístoles e dos sintomas relacionados após administração de magnésio por via oral / Successful improvement of frequency and symptoms of premature complexes after oral magnesium administration

FUNDAMENTO: As extrassístoles ventriculares e supraventriculares (EV e ESSV) são frequentes e muitas vezes sintomáticas. O íon magnésio (Mg) desempenha um papel importante na fisiologia do potencial de ação transmembrana celular e do ritmo cardíaco. OBJETIVO: Avaliar se a administração do pidolato de magnésio (PMg) em pacientes com EV e ESSV tem desempenho superior ao uso do placebo (P) na melhora dos sintomas e densidade das extrassístoles (DES). MÉTODOS: Estudo duplo-cego, randomizado, com 60 pacientes sintomáticos consecutivos, com mais de 240/EV ou ESSV ao Holter de 24 horas e selecionados para receber P ou PMg. Para avaliar a melhora da sintomatologia, foi feito um questionário categórico e específico de sintomas relacionados às extrassístoles. Após o tratamento, foi considerada significante uma redução de mais de 70% na DES por hora. A dose do PMg foi de 3,0 g/dia por 30 dias, equivalente a 260 mg do elemento Mg. Nenhum paciente tinha cardiopatia estrutural ou insuficiência renal. RESULTADOS: Dos 60 pacientes estudados, 33 eram do sexo feminino (55%). A faixa etária variou de 16 a 70 anos. No grupo PMg, 76,6% dos pacientes tiveram redução maior que 70%, 10% deles maior que 50% e somente 13,4% tiveram redução menor que 50% na DES. No grupo P, 40% dos pacientes tiveram melhora de apenas 30% na frequência de extrassístoles (p < 0,001). A melhora dos sintomas foi alcançada em 93,3% dos pacientes do grupo PMg, comparada com somente 16,7% do grupo P (p < 0,001). CONCLUSÃO: A suplementação de Mg via oral reduziu a DES, resultando em melhora dos sintomas.

BACKGROUND: Premature ventricular and supraventricular complexes (PVC and PsVC) are frequent and often symptomatic. The magnesium (Mg) ion plays a role in the physiology of cell membranes and cardiac rhythm. OBJECTIVE:We evaluated whether the administration of Mg Pidolate (MgP) in patients with PVC and PsVC is superior to placebo (P) in improving symptoms and arrhythmia frequency. METHODS: Randomized double-blind study with 60 consecutive symptomatic patients with more than 240 PVC or PsVC on 24-hour Holter monitoring who were selected to receive placebo or MgP. To evaluate symptom improvement, a categorical and a specific questionnaire for symptoms related to PVC and PsVC was made. Improvement in premature complex density (PCD) per hour was considered significant if percentage reduction was >70% after treatment. The dose of MgP was 3.0 g/day for 30 days, equivalent to 260mg of Mg element. None of the patients had structural heart disease or renal failure. RESULTS: Of the 60 patients, 33 were female (55%). Ages ranged from 16 to 70 years old. In the MgP group, 76.6% of patients had a PCD reduction >70%, 10% of them >50% and only 13.4% <50%. In the P group, 40% showed slight improvement, <30%, in the premature complexes frequency (p < 0.001). Symptom improvement was achieved in 93.3% of patients in the MgP group, compared with only 16.7% in the P group (p < 0.001). CONCLUSION: Oral Mg supplementation decreases PCD, resulting in symptom improvement.

protective effects of N-acetl-cysteine, oxo-thiazolidine-carboxylate, acetaminophen and their combinations against sulfur mustard cytotoxicity on human skin fibroblast cell line [HF2FF]

Using human skin-fibroblast cell line HF2FF, the efficacy of some drugs was evaluated against sulfur mustard [SM] cytotoxicity. The drugs were the sulfhydryl containing molecule including Nacetylcysteine [NAC], 2-oxo-thiazolidine-4-carboxylate [OTC] and acetaminophen as glutathione [GSH] stimulator pathway. The protective effects of NAC [0.1 mM], OTC [1.8 mM], and acetaminophen [25 mM] alone or in combination with each other were evaluated on SM [180 micro M]-induced cytotoxicity. NAC and OTC were applied with SM simultaneously and acetaminophen 30 min before SM exposure, incubated for 1 h and then were rinsed and incubated with fresh medium. The efficacy was evaluated by determination of cells viability, intracellular GSH level and catalase activity 1 and 24 h post SM exposure or co-treatments. The cells viability was decreased 21.8% and 55.2%, respectively for 1 and 24 h post SM [1 h exposure] incubation. So, the 1-h SM exposure and 24-h treatment incubation were selected for evaluation. While, NAC alone treatment increased the cells viability [25%], GSH level [320%] and catalase activity [18%], the most effective combination was NAC plus OTC and acetaminophen which increased more significantly the cells viability [about 40%], GSH level [470%] and catalase activity [100%]. The most effective combination was NAC [0.1 mM] plus OTC [1.8 mM] and acetaminophen [25 mM] which should be used before or concomitant with SM exposure. These drugs may reduce SM toxicity possibly by increment of GSH level and catalase activity. This efficacy needs to be confirmed by in vivo study

Capsule metadoxine in the treatment of alcoholic liver disease: a randomized, double-blind, placebo-controlled, multicenter study / 中华肝脏病杂志

<p><b>OBJECTIVE</b>To evaluate the efficacy and safety of Capsule metadoxine in the treatment of alcoholic liver disease.</p><p><b>METHODS</b>A randomized double blind multicenter placebo-controlled clinical study was performed to evaluate the therapeutic effectiveness and safety of capsule metadoxine. Patients in metadoxine group received capsule metadoxine 500mg tid po. Patients in placebo group received placebo 2 pillows tid po. The treatment duration was 6 weeks. Patients were followed up 2 weeks after the treatment. Patients were visited once every 3 weeks during the treatment period. Clinical symptoms and liver function were evaluated in all the patients before treatment, at week 3, week 6 and 2 weeks after therapy. CT scan was done in some patients before treatment and at the end point of therapy.</p><p><b>RESULTS</b>254 patients were recruited in the study, 126 in metadoxine group and 128 in placebo group. Median ALT, AST, GGT level in metadoxine group were decreased from 80.0 U/L, 59.2 U/L, 123.0 U/L (before treatment) to 41.1 U/L, 36.0 U/L, 57.0 U/L (after 6 weeks therapy). The improvement in liver function was more significant in metadoxine group than in placebo group (P less than 0.05). For the patients who stopped drinking during the study, the total effective rate of improvement in liver function was 82.8% in metadoxine group, much higher than that in placebo group (55.7% , P=0.0000). For the patients who did not stop drinking during the study, the total effective rate of improvement in liver function was 65.4% in metadoxine group, which is not significantly higher than that in placebo group (44.8%, P=0.1767). The CT value ratio of liver to spleen was significantly improved in metadoxine group (P=0.0023), and there was no significant difference between the two groups (P=0.6293). The rate of adverse was 1.6% in both of groups.</p><p><b>CONCLUSION</b>Capsule metadoxine is an effective and safe treatment for alcoholic liver disease.</p>

An antioxidant modulates expression of receptor activator of NF-kappaB in asthma

Oxidative stress plays critical roles in airway inflammation that is usually accompanied by increased vascular permeability and plasma exudation. VEGF increases vascular permeability and leads to airway inflammation. In addition, VEGF has been shown to enhance receptor activator of NF-kappaB (RANK) expression in endothelial cells. An aim of the study was to determine the potential role of antioxidant in the regulation of RANK expression in murine model of asthma. We have used a C57BL/6 mouse model of allergic asthma to evaluate the effect of L-2-oxothiazolidine-4-carboxylic acid (OTC), a prodrug of cysteine, which acts as an antioxidant, and VEGF receptor inhibitor on RANK mRNA expression. The mice develop the following pathophysiological features of asthma in the lungs: increased expression of RANK mRNA, increased number of inflammatory cells of the airways, increased vascular permeability, and increased levels of VEGF. Administration of OTC and VEGF receptor inhibitor markedly reduced plasma extravasation and VEGF levels in allergen-induced asthmatic lungs. We also showed that the increased RANK mRNA expression at 72 h after ovalbumin inhalation were reduced by the administration of OTC or VEGF receptor inhibitor. The results indicate that OTC and VEGF receptor inhibitor which inhibit up-regulation of VEGF expression modulate RANK expression that may be in association with the regulation of vascular permeability, and suggest that VEGF may regulate the RANK expression. These findings provide a crucial molecular mechanism for the potential use of antioxidants to prevent and/or treat asthma and other airway inflammatory disorders.

Studies on chemical constituents in leaf of Isatis indigotica / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of the leaf of Isatis indigotica.</p><p><b>METHOD</b>Chromatography and spectral analysis were respectively used to isolate and identify the constituents.</p><p><b>RESULT</b>Three compounds were isolated from the ethanol extracts of theleaf of I. indigotica, and identified as indirubin, tryptanthrin and L-pyroglutamic acid.</p><p><b>CONCLUSION</b>L-pyroglutamic acid was isolated from the genus for the first time, and tryptanthrin was isolated from the leaf of this plant for the first time.</p>

Study on the mechanism of male reproductive toxicity of metadoxine in mice and rats / 中华预防医学杂志

<p><b>OBJECTIVE</b>To study the mechanism of male reproductive toxicity of metadoxine (MTDX) on mice and rats.</p><p><b>METHODS</b>Mouse multiple endpoints assay and Hershberger assay were employed to evaluate the potential estrogenic and/or antiandrogenic effects of MTDX. In mouse multiple endpoints assay, MTDX (0, 640, 1500 and 4000 mg/kg, respectively) were administered once daily p.o. for 5 days in sexually matured and ovariectomied female NIH mice. Five endpoints evaluated as markers of estrogenicity included the ratio of uterine weight to body weight, incidence and extent of uterine fluid imbibition (hydrometra), vaginal epithelial cornification during estrous cycle (estrinization) and thickness of uterine epithelial cell and stroma cell. In Hershberger assay, MTDX (0, 600 and 1500 mg/kg, respectively) was administered once daily p.o. for 10 days to castrated male SD rats with or without testosterone propionate (TP, 12.5 mg/kg, i.p. for 10 days) substitution. Relative weight of androgen dependent issues was measured.</p><p><b>RESULTS</b>In mouse multiple endpoints assay, ratio of uterine weight to body weight was 1.33, 1.38 and 1.31 x 10(-4) in MTDX 640, 1500 and 4000 mg/kg groups, respectively, without significant difference from that in control group (1.22 x 10(-4)). Thickness of uterine uterine epithelial cell (0.90 and 1.03 microm) and stroma cell (3.38 and 3.25 microm) in MTDX 1500 and 4000 mg/kg groups was not significantly different from the control group (0.85 microm and 2.77 microm, respectively). In Hershberger assay, relative weight of prostate plus seminal vesicle, levator ani muscle and bulbocavernous muscle was 1.13, 0.17 and 0.42, respectively, in the 1500 mg/kg group, significantly decreased as compared with those in the control group (1.46, 0.24 and 0.70, respectively) (P < 0.01). Relative weight of prostate plus seminal vesicle (1.29) in the MTDX 600 mg/kg group reduced slightly, with statistical significance (P < 0.05), as compared with that in the control group (1.46).</p><p><b>CONCLUSIONS</b>In the present study, MTDX did not exhibit any estrogenic effect in mice in vivo. However, it had antiandrogenic activity in castrated male SD rats, indicating that its antiandrogenic effect may be involved in it's male reproductive toxicity.</p>

Oleyl pyroglutamate for use as transdermal enhancer and its enhancing mechanism / 药学学报

<p><b>AIM</b>To test the enhancing activity and the mechanism of oleyl pyroglutamate used as transdermal enhancer.</p><p><b>METHODS</b>The penetration-enhancing effects of oleyl pyroglutamate, oleyl alcohol and oleic acid on the three drugs (caffeine, tinidazole and cortisone) were observed; the transdermal enhancing mechanism of oleyl pyroglutamate was studied with the attenuated total reflectance Fourier-transfer infrared spectroscopy(ATR-FTIR) of the human stratum corneum in vivo.</p><p><b>RESULTS</b>The penetration-enhancing ratio of the three drugs was 7.9 fold, 41.8 fold and 2.8 fold, respectively. The absorptions at 2,800-2,950 cm-1 and 1,642-1,646 cm-1 (amide-I) in the ATR-FTIR spectrum of the stratum were found to be shifted differently following removal of the stratum corneum which was treated with oleyl pyroglutamate.</p><p><b>CONCLUSION</b>Oleyl pyroglutamate showed better penetration-enhancing effect on the penetration of drugs. Its transdermal enhancing mechanism may be that oleyl pyroglutamate induced not only disordering of the stratum corneum lipid, but also change of the secondary structure of keratin.</p>

Reproductive toxicity of metadoxine in rats / 中华预防医学杂志

<p><b>OBJECTIVE</b>To study the reproductive toxicity of metadoxine.</p><p><b>METHODS</b>Male and female rats were given metadoxine before pregnancy and early gestation, i.e. to feed metadoxine to male rats for 60 days before copulation and continue feeding during copulation, and feed metadoxine to female rats for 14 days before copulation.</p><p><b>RESULTS</b>No significant toxic effect was observed in the 400 mg/kg group. A few rats showed paralysis of hind leg in the 800 mg/kg group. The dosage of 1 600 mg/kg caused significant paralysis of hind legs, emaciation, and reduced weight gain. In the 1600 mg/kg group, the mating rate of male rats was significantly affected (P < 0.01). In the 800 and 1 600 mg/kg group, fertility of male rats was markedly reduced (P < 0.01). In the 800 mg/kg group, the effect on sperm counts of epididymis of male rats was markedly reduced (P < 0.05). In the 1 600 mg/kg group, testicle weight and body weight ratio and sperm counts of epididymis rate were significantly (P < 0.001) reduced. In the 1 600 mg/kg group, the fertility rate of female rats was remarkably (P < 0.001) reduced. In the 800 mg/kg group, the weight gain of pregnant rats was significantly reduced (P < 0.001). In both the 800 and 1 600 mg/kg groups, the gestation rate was greatly reduced (P < 0.001). In the 800 mg/kg group, mortality rate before nidation (P < 0.001) and average live fetus number were significantly reduced (P < 0.05). In the 400 mg/kg group, the fetal weight was significantly reduced (P < 0.001). In the 800 mg/kg group, body length, tail length, body weight and sternum development of fetal rats were significantly affected (P < 0.001).</p><p><b>CONCLUSION</b>Under the presented experimental conditions, metadoxine has no teratogenic effects on SD rats and the no effect dose is 400 mg/kg. And the no effect dose for the developmental toxicity is less than 400 mg/kg.</p>

Advances in modulation of mammalian sperm function by fertilization promoting peptide / 中华医学遗传学杂志

Both fertilization promoting peptide and adenosine stimulate capacitation but inhibit spontaneous acrosome loss by modulation of the adenylyl cyclase (AC)/cAMP signal transduction pathway. This is a review aimed at analyzing the function of fertilization promoting peptide during this process. The possible molecular basis is also discussed.