Secretion of reproductive hormones and estrous cycle in rats interfered by combined exposure to beta-cypermethrin and emamectin benzoate / 环境与职业医学

Backgroud Beta-cypermethrin and emamectin benzoate are widely used for the prevention and control of pests in the greenhouse planting industry, and their combined exposure may increase the accumulation of beta-cypermethrin and emamectin benzoate in organisms and affect human health. Objective Based on the changes in reproductive hormone levels in the hypothalamic-pituitary-ovarian (HPO) axis, to investigate the effect of combined exposure to beta-cypermethrin and emamectin benzoate on the estrous cycle of female mice. Methods Twenty-four healthy adult SD rats were randomly divided into a blank control group, a beta-cypermethrin group (Beta-CYP, 53 mg·m−3), an emamectin benzoate group (EMB, 8 mg·m−3), and a beta-cypermethrin and emamectin benzoate combined exposure group (Beta-CYP+EMB, Beta-CYP 53 mg·m−3 + EMB 8 mg·m−3). Six rats in each group were exposed to the designed treatment protocol by aerosol inhalation 6 d a week for 13 weeks. The general condition of the rats was observed in real time during the treatment. From the 12th week of exposure, a 10-day reproductive tract smear was performed on the rats to observe the estrous cycle. The rats were neutralized on the second day after the end of the treatment protocol, and the ovarian tissues were stained with HE to observe histopathological changes. Serum levels of gonadotropin-releasing hormone (GnRH), follicle-stimulating hormone (FSH), luteinizing hormone (LH), and estradiol (E2) were measured by ELISA. Experimental results were expressed as mean ± standard deviation (\begin{document}$ \overline{x}\pm s $\end{document}). One-way ANOVA was used for comparison among groups, and LSD test for pairwise comparison between groups. The significance level was α=0.05. Results After four weeks of the treatment protocol, the rats in the Beta-CYP group and the Beta-CYP+EMB group continued to be hyperactive and irritable, while the EMB group showed symptoms of mental disorder, decreased activity, and slow response. On the 90th day of the treatment protocol, the body weight of rats in the control group increased to (314.51±2.44) g, and that in the Beta-CYP+EMB group only increased to (253.47±1.50) g. There was no abnormal cellular morphology in the control group; however, small deeply stained nuclei appeared in the Beta-CYP group, the EMB group, and the Beta-CYP+EMB group, and abnormal morphological development of keratinized epithelial cells in the Beta-CYP+EMB group was found. The estrous cycle of rats in the control group was (97.83±4.17) h, and compared with the control group, the estrous cycles of rats in the Beta-CYP group, the EMB group, and the Beta-CYP+EMB group were prolonged to (134.33±7.53) h, (126.50±5.28) h, and (156.00±6.66) h, respectively. The results of ANOVA showed that the numbers of leukocytes (527.17±15.83), keratinized epithelial cells (35.67±4.32), and non-keratinized epithelial cells (70.50±4.51) in the vaginal smears during diestrus in the Beta-CYP+EMB group were significantly lower than those in the control group (752.50±28.89, 50.50±2.74, 101.33±7.92) (P<0.001). The hormone levels of GnRH and FSH in the control group were (5.13±0.59) and (0.76±0.09) IU·L−1 respectively, while the levels in the Beta-CYP+EMB group were increased to (16.86±0.59) and (3.80±0.19) IU·L−1 respectively (P<0.05). The levels of LH and E2 in the control group were (12.93±0.81) IU·L−1 and (22.23±1.44) pmol·L−1 respectively, and the levels in the Beta-CYP+EMB group were decreased to (5.63±0.41) IU·L−1 and (10.45±0.78) pmol·L−1 respectively (P<0.05). Conclusion The combined exposure to beta-cypermethrin and emamectin benzoate may ultimately affect the estrous cycle of female rats by interfering with the secretion of reproductive hormones involved in the HPO axis.

Annona muricata Linn Stem Bark Protects against Uterine Proliferative Disorder Induced by Estradiol Benzoate in Female Rat

Aim: The opening of mitochondrial permeability transition (mPT) pore is an important event in the execution of mitochondrial-mediated apoptosis. Some bioactive compounds elicit their chemotherapeutic effects against tumor/cancer cells via the induction of mitochondrial-mediated apoptosis. Annona muricata, a medicinal plant, is folklorically used in the treatment of tumors and cancers. This study therefore aimed at investigating the effect of methanol stem bark extract of Annona muricata (MEAM) on apoptosis via mPT pore and estradiol benzoate (EB)-induced proliferative disorder using female Wistar rats. Methodology: Mitochondria were isolated using differential centrifugation. The mPT pore opening, cytochrome c release and mitochondrial ATPase activity were determined spectrophotometrically. The levels of estrogen (E2), luteinizing hormone (LH), follicle stimulating hormone (FSH), malondialdehyde (MDA) and activities of superoxide dismutase (SOD), glutathione peroxidase (GSH), were determined using ELISA technique. Histological and histochemical assessments of the uterine sections were carried out using standard methods. Phytochemical constituents of MEAM were determined using Gas Chromatography-Mass Spectroscopy (GC-MS). Results: The in vitro results showed a significant induction of mPT pore opening, release of cytochrome c and enhancement of mitochondrial ATPase (mATPase) activity in a concentration-dependent manner. However, oral administration of MEAM did not induce rat uterine mPT pore opening, neither any significant release of cytochrome c nor enhancement of mATPase activity at the dosages used. Interestingly, MEAM reversed the EB-induced increase in E2, LH and FSH. The MEAM also improved the antioxidant milleu by reducing MDA level and increasing the SOD and GSH-Px activities in the treatment groups. Administration of EB induced endometrial hyperplasia in the model group which was mitigated by MEAM in the treatment group. The GC-MS analysis of MEAM revealed the presence of some important phytochemicals that are pharmacological relevant in cancer treatment. Conclusions: This study suggests that the methanol stem bark extract of Annona muricata contains bioactive compounds that protect against EB-induced uterine proliferative disorder in female Wistar rats.

The gelling properties of Dillenia indica mucilage in benzyl benzoate emulgel formulations

Abstract The objective of the study was to evaluate the gelling properties of Dillenia indica mucilage in benzyl benzoate emulgel formulation. Mucilage was extracted from the fruits of Dillenia indica using established methods and characterized by rheology and swelling. Emulsion (F1) was prepared using the continental emulsification method. Gelling agents (2 %w /v) were prepared by dispersing in distilled water with constant stirring at a moderate speed using a magnetic stirrer. F1 was added to the gel (0-75 %w /w) to obtain emulgel formulations and evaluated using viscosity, globule size, pH, release profiles and kinetic modeling. Data were expressed as mean ± SD, and similarity factor (f2) was used to compare all formulations. Formulation viscosity was significantly higher with carbopol than with Dillenia; globule sizes increased with concentration of gelling agents, and pH reduced as the concentration of Dillenia increased. All formulations showed controlled release properties with t80 ranging between 114 and 660 min. The release was governed by Korsmeyer-Peppas model. Formulation F5 prepared with 50 % Dillenia showed highest similarity to F4 prepared with 75 %w /w carbopol. Dillenia indica demonstrated acceptable gelling properties comparable with that of carbopol and could be improved for use in emulgel formulations.

Formulation development and pharmacokinetic studies of long acting in situ depot injection of risperidone

Abstract Risperidone is an atypical antipsychotic drug widely prescribed all over the world due to its clinical advantages. The currently available long acting marketed depot formulation of risperidone is a microsphere based preparation using poly-[lactide-co-glycolide] (PLGA) as drug release barrier. It is however, a cold chain product due to thermal instability of PLGA at room temperature. After beginning the depot injection therapy it is administered every two weeks but associated with another drawback of about 3 weeks lag time due to which its tablets are also administered for three weeks so as to attain and maintain therapeutic drug concentration in the body. The present work attempts to develop a long acting depot delivery system of risperidone for once a month administration based on the combination of sucrose acetate isobutyrate and polycaprolactone dissolved in benzyl benzoate to provide an effective drug release barrier for one month without any lag time and which can be stored at room temperature precluding the requirement of cold supply chain. The developed depot formulation showed a sustained in vitro drug release profile with 88.95% cumulative drug release in 30 days with little burst release. The in vivo pharmacokinetic studies of the developed formulation conducted on rats showed attainment of mean peak plasma drug concentration of 459.7 ng/mL in 3 days with a mean residence time of 31.2 days, terminal half-life of 20.6 days, terminal elimination rate constant of 0.0336 per day, and a good in vitro- in vivo correlation.

Rapid Qualitative and Quantitative Analysis of Caffeine and Sodium Benzoate in Annaca by Infrared Spectroscopy / 法医学杂志

Objective To establish an infrared spectroscopic method for the rapid qualitative and quantitative analysis of caffeine and sodium benzoate in Annaka samples. Methods Qualitative and quantitative modeling samples were prepared by mixing high-purity caffeine and sodium benzoate. The characteristic absorption peaks of caffeine and sodium benzoate in Annaka samples were determined by analyzing the infrared spectra of the mixed samples. The quantitative model of infrared spectra was established by partial least squares （PLS）. Results By analyzing the infrared spectra of 17 mixed samples of caffeine and sodium benzoate （the purity of caffeine ranges from 10% to 80%）, the characteristic absorption peaks for caffeine were determined to be 1 698, 1 650, 1 237, 972, 743, and 609 cm-1. The characteristic absorption peaks for sodium benzoate were 1 596, 1 548, 1 406, 845, 708 and 679 cm-1. When the detection of all characteristic absorption peaks was the positive identification criteria, the positive detection rate of caffeine and sodium benzoate in 48 seized Annaka samples was 100%. The linear range of PLS quantitative model for caffeine was 10%-80%, the coefficient of determination （ R2） was 99.9%, the root mean square error of cross validation （RMSECV） was 0.68%, and the root mean square error of prediction （RMSEP） was 0.91%; the linear range of PLS quantitative model for sodium benzoate was 20%-90%, the R2 was 99.9%, the RMSECV was 0.91% and the RMSEP was 1.11%. The results of paired sample t test showed that the differences between the results of high performance liquid chromatography method and infrared spectroscopy method had no statistical significance. The established infrared quantitative method was used to analyze 48 seized Annaka samples, the purity of caffeine was 27.6%-63.1%, and that of sodium benzoate was 36.9%-72.3%. Conclusion The rapid qualitative and quantitative analysis of caffeine and sodium benzoate in Annaka samples by infrared spectroscopy method could improve identification efficiency and reduce determination cost.

Synthesis, Spectral Characterization And Biopotential Significance Of Co(Ii) And Ni(Ii) Complexes With Biologically Active Ligands

New Cobalt(II) and Nickel(II) metal complexes of 2-aminothiazole (ATZ) and benzoate ion (BEN) ligands were synthesized under microwave irradiation. The empirical formulae and the structure of the complexes have been deduced from CHN analysis, electrical conductance, magnetic moment, electronic (DRS method), Infra Red spectra, TGA analysis, cyclic voltammetry and powder-XRD techniques. The low electrical conductance values indicate that the complexes are non-electrolyte (1:0) type. The electronic spectra and the magnetic moment indicate the structures of the complexes are found to be octahedral geometry. Infra Red spectra illustrate that 2-aminothiazole and benzoate ion is bonded to the metal ion in a monodentate approach. The antifungal activities of ligands and their cobalt(II) and nickel(II) metal complexes were studied aligned with the few microorganisms by agar - well diffusion method at 100,200 and 400 conc. µg/ml concentration. The prepared cobalt(II) and nickel(II) metal complexes show prospective action against the tested fungi as compared to free 2-aminothiazole ligand. The free radical scavenging action of the prepared complexes and the ligand has been resolute by measuring their interface with the stable free radical DPPH. The complexes have larger antioxidant activity as compared to the free ligand. DNA-binding properties have been calculated by fluorescence-emissions method. The obtained results suggest that the complexes powerfully bind to DNA because of metal complexes are well-known to speed up the drug action and the capability of healing agent which can repeatedly be enhanced leading coordination with a metal ion.

A new monoterpene glycoside compound from roots of Paeonia lactiflora / 中草药

Objective: To study the constituents from the roots of Paeonia lactiflora. Methods: The chemical constituents were isolated by various chromatographic techniques and their structures were elucidated by physicochemical properties and NMR data. Results: Eleven compounds were obtained and characterized as (4S)-perillic acid 6-O-α-L-arabinopyranosyl-(1'→6'')- β-D-glucopyranosyl (1), 4,9-dihydroxy-8,10-dehydrothymol-1-O-β-D-glucoside (2), emodin-8-O-β-D-glucoside (3), resveratrol (4), β-D-glucopyranosyl benzoate (5), ilexperphenoside A (6), catechol (7), methyl gallate (8), ethyl gallate (9), 3-methoxygallic acid (10), 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranoside (11). Conclusion: Compound 1 is identified as a new compound, named perillic acid glycoside, compounds 2 and 5 are identified from the genus Paeonia for the first time.

Isolation and identification of unknown impurities of alogliptin benzoate / 中国药科大学学报

@#By silica gel column chromatography, solvent extraction and preparative high performance liquid chromatography (HPLC), four new related substance were isolated and purified from the mass production and preparation process of alogliptin benzoate. Then it was analyzed and confirmed by various spectrum identification methods such as nuclear magnetic resonance (NMR) spectroscopy, high-resolution mass spectrometry (HR-MS) and Fourier-transform infrared spectroscopy (FTIR) according to its physical and chemical properties. The chemical structures of the four related substances produced in each step of the synthesis process of alogliptin benzoate were determined, and they were named as impurities L, M, T, and V. These four related substances were new impurities which were found for the first time. The isolation and identification of these impurities are of great importance to the quality control of alogliptin benzoate, and the optimization of manufacturing process.

Different times to perform timed artificial insemination when using a P4/E2/eCG-based protocol in buffalo / Momentos diferentes para executar a inseminação artificial em tempo fixo utilizando o protocolo à base de P4/E2/eCG em búfalas

ABSTRACT: The aim of this study was to evaluate different times for timed artificial insemination (TAI) in buffalo submitted to a P4/E2/eCG-based protocol. In this study, 204 buffaloes were distributed into one of two groups (TAI56, n=103 and TAI64, n=101). At a random stage of the oestrous cycle (Day 0 = D0), in the morning (TAI56, a.m.) or afternoon (TAI64, p.m.), buffaloes received an intravaginal progesterone device (P4; 1.0 g) plus EB (2.0 mg i.m.). On D9 a.m. (TAI56) or p.m. (TAI64), the P4 was removed and buffaloes received PGF2a (0.53 mg i.m. sodium cloprostenol) and eCG (400 IU i.m.). On D10 a.m. (TAI56) or p.m. (TAI64), 24 h after P4 removal, buffaloes were treated with EB (1.0 mg i.m.). Buffaloes from TAI56 and TAI64 were inseminated 56 and 64 h after P4 removal (D11, p.m. and D12, a.m., respectively). Ultrasound examinations were performed on D0 to ascertain ovarian follicular status, at TAI to measure the diameter of the dominant follicle (DF) and D42 for pregnancy diagnosis. The statistical analysis was performed using the GLIMMIX procedure of SAS®. There was no difference between TAI56 and TAI64 for the diameter of the DF at TAI and the pregnancy per TAI. It was concluded that TAI 56 or 64 h after P4 removal did not affect fertility in buffaloes submitted to the induction of ovulation with EB. The present research supports that is possible to perform TAI at any time throughout the day in buffalo synchronized during the non-breeding season.

RESUMO: O objetivo deste estudo foi avaliar diferentes momentos para a realização da IATF em búfalas submetidas a um protocolo à base de P4/E2/eCG. Neste estudo, 204 búfalas foram distribuídas em um de dois grupos (IATF56, n=103 e IATF64, n=101). Em estágio aleatório do ciclo estral (Dia 0 = D0), pela manhã (IATF56, manhã) ou pela tarde (IATF64, tarde), as búfalas receberam um dispositivo intravaginal de progesterona (P4; 1,0 g) e BE (2,0 mg i.m.). No D9 pela manhã (IATF56) ou pela tarde (IATF64), a P4 foi removida e as búfalas receberam PGF2a (0,53 mg i.m. cloprostenol sódico) e eCG (400 UI i.m.). No D10 pela manhã (IATF56) ou pela tarde (IATF64), 24 h após a remoção da P4, as búfalas foram tratadas com BE (1,0 mg i.m.). As búfalas dos grupos IATF56 e IATF64 foram inseminadas 56 e 64 h após a remoção da P4 (D11, pela tarde e D12, pela manhã, respectivamente). Avaliações ultrassonográficas foram realizadas no D0 para verificar o status folicular ovariano, na IATF para medir o diâmetro do folículo dominante (FD) e no D42 para o diagnóstico de gestação. A análise estatística foi realizada utilizando o procedimento GLIMMIX do SAS®. Não houve diferença entre os grupos IATF56 e IATF64 no diâmetro do FD na IATF e na prenhez por IATF. Conclui-se que a IATF 56 ou 64 h após a remoção da P4 não afeta a fertilidade de búfalas submetidas à indução da ovulação com BE. A presente pesquisa evidencia que é possível realizar a IATF durante todo o dia em búfalas sincronizadas durante a estação reprodutiva desfavorável.

Comparative study of oral ivermectin, topical permethrin and benzyl benzoate in the treatment of scabies

Background: Efficacy of these modalities as shown by various investigations are inconsistent and ambiguous. Thus, evidence based effective treatment option is warranted. Aim of the study was to compare the efficacy of oral ivermectin, topical permethrin and benzyl benzoate in the treatment of uncomplicated scabies.Methods: Patients with confirmed diagnosis of scabies were included in this study. One hundred and ninety-five subjects were included in this investigation as per inclusion and exclusion criteria laid down. Equal numbers of patients were randomly allocated to one of the three treatment groups. Efficacy of three groups [oral ivermectin (Group A), topical permethrin (Group B) and benzyl benzoate (Group C)] of drugs was compared in terms of improvement in clinical grading of disease (%) and improvement in clinical grading of pruritus (%) during follow up visits.Results: Those subjects receiving topical permethrin, at 1st follow up 56.9% showed cure rate which increased to 89.2% at 2nd follow up with respect to clinical improvement in pruritus. Maximum relief in severity of pruritus at the end of 6th week was reported by 58(89.2%) patients receiving group B treatment modality followed by 52 patients (80%) in arm A. Regarding efficacy of three treatment groups in terms of improvement in severity of lesion at the end of 6 weeks, maximum number of patients 57(87.7%), receiving group B treatment reported improvement which is better than other two treatment groups.Conclusions: maximum number of patients receiving topical Permethrin treatment reported improvement better than other Oral Ivermectin therapy and topical benzyl benzoate. Oral ivermectin may serve a good alternative for managing scabies under certain conditions like poor compliance to topical scabicides.

Analytical Method Development And Its Validation For Estimation Of Chlorhexidine Gluconate

In the present work, Independent method was developed for estimation of Chlorhexidine Gluconate, Metronidazole benzoate,Lignocaine Hydrochloride, and Salicylic Acid in bulk and dosage form by UV-Visible Spectrophotometry. In this method the determination ofmaximum absorbance (λmax) of the drugs were found to be 259 nm, 285.8 nm, 263 nm and 304 nm. The validation parameters were studiedaccording to ICH guidelines. On the basis of % agreement criteria, therefore Average % agreement found to be 100.05 at 259 nm, 99.32 at285.8 nm, 100.001 at 304 nm and 99.70 at 263 nm. Specificity study shows the good agreement with results, indicating that excipients did notinterfere with the analyte. Repeatability study showed a % R.S.D of 0.2486 at 259 nm, 0.2605 at 285.8 nm, 0.403174 at 304 nm and 0.880817at 263 nm for Chlorhexidine Gluconate, Metronidazole benzoate, Lignocaine Hydrochloride, and Salicylic Acid. Thus it is concluded that theanalytical technique has a good repeatability precision as R.S.D are less than 5.3% (Specified) and less than 2% (desired). So it can be said thatthe proposed method is precise. Intraday study were showed a % R.S.D of 1.246918, 0.984763, 0.775939 and 1.022045 respectively forChlorhexidine Gluconate, Metronidazole benzoate, Lignocaine Hydrochloride, and Salicylic Acid. So it can be said that the proposed method isprecise. Interday study were showed a % R.S.D of 1.358486, 0.829325, 1.273356 and 0.968196 respectively for Chlorhexidine Gluconate,Metronidazole benzoate, Lignocaine Hydrochloride, and Salicylic Acid. So it can be said that the proposed method is precise. Limit of detectionwere found to be 0.097, 0.117, 0.010 and 0.074 g/ml at 259, 285.8, 304and 263 nm. Limit of quantification were found to be 0.29, 0.35, 0.030and 0.418 g/ml at 259, 285.5 304, and 263nm. The accuracy of the methods was proved by performing recovery studies in availableformulations. Since the % recovery 98.07 to 101.28 at 259 nm, 98.29 to 101.02 at 285.8 nm, 99.99 to 101.25 at 304nm and 99.10 to 101.78 at263nm are within the desirable confidence interval of 98-102%. So it can be said that the proposed method is accurate. The percent meanrecovery is 98.46, 101.42 (1:3), 98.20 and 99.78% of labeled amount, which is within specified limits of 98-102%. It can be said that proposedmethod can satisfactory be applied for analysis of Chlorhexidine Gluconate, Metronidazole benzoate, Lignocaine Hydrochloride, and SalicylicAcid in dosage form. The developed method is precise, accurate and do not suffer from any interference due to common excipients. It isevident from this study that the developed method is simple, sensitive, specific, precise and accurate and economic. Hence it can be employedfor routine analysis in quality control laboratories.

Volatile constituents of Atalantia roxburghiana Hook. f., Tetradium trichotorum Lour. and Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae) from Vietnam / Compuestos volátiles de Atalantia roxburghiana Hook. f., Tetradium trichotorum Lour. y Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae) provenientes de Vietnam

The chemical constituents of essential oils obtained by hydrodistillation of the leaves of Atalantia roxburghiana Hook. f. and Tetradium trichotomum Lour., as well as the leaves and fruits of Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae) are being reported. The essential oils were analysed by using gas chromatography (GC) and gas chromatography coupled with mass spectrometry (GC-MS). Sabinene (36.9%) was the most singly abundant compound in the leaf of A. roxburghiana. The major constituents present in the leaf oil of T. trichotorum were (E)-ß-ocimene (24.8%), α-pinene (10.4%), (Z)-ß-ocimene (9.4%) and ß-caryophyllene (8.0%). On the other hand, while α-pinene (17.5%), ß-caryophyllene (15.5%) and caryophyllene oxide (10.6%) occurred in higher proportion in the leaf of M. oligophlebia, the fruit oil was dominated by benzyl benzoate (16.8%), (E, E)-farnesol (8.3%) and ß-caryophyllene (6.0%).

Se muestran los constituyentes químicos de los aceites esenciales obtenidos, por hidrodestilación, de las hojas de Atalantia roxburghiana Hook. f. y de Tetradium trichotomum Lour., así como de las hojas y frutos de Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae). Los aceites esenciales fueron analizados por Cromatografía de Gases (CG) y por Cromatografía de Gases acoplada a Espectrometría de Masas (CG-EM). El compuesto más abundante en las hojas de A. roxburghiana es el sabineno (36.9%); mientras que los mayoritarios en el aceite de las hojas de T. trichotomum fueron (E)-ß-ocimeno (24.8%), α-pineno (10.4%), (Z)-ß-ocimeno (9.4%) y ß- cariofileno (8.0%). En las hojas de M. oligophlebia los compuestos más abundantes fueron α-pineno (17.5%), ß-cariofileno (15.5%) y óxido de cariofileno (10.6%); sin embargo, en el aceite obtenido del fruto fueron benzoato de bencilo (16.8%), (E, E)-farnesol (8.3%) y ß- cariofileno (6.0%).

Effects of denatonium benzoate on calcium binding protein S100A9 and mucus in the airways of asthmatic mice / 医学研究生学报

number of goblet cells, mucus secretion and mucin MUC5AC content in lung tissues. Results S100A9 in BALF of group B was (11.89±0.77) ng/mL, S100A9 integrated optical density (IOD) value in airway epithelial cells was 13.96±1.62, PAS stain area /epithelial cell area was (12.53±1.21)%, relative value of MUC5AC / NADPH was 173.91±4.29, all of the above were higher than those of group A [(6.19±0.61) ng/mL, 4.97±0.30, (1.94±0.18)%, 1];S100A9 levels, IOD of S100A9 in airway epithelial cells, PAS stain area / epithelial cell area (%), relative value of MUC5AC / NADPH in group C [(10.69±0.79) ng / ml, 11.80±0.72, (10.61±0.61)%, 94.65±1.59], group D[(9.49±0.99) ng/mL, 10.39±0.59, (8.63±0.62)%, 82.08±1.12], group E [(7.54± 0.42) ng/mL, 5.63±0.84, (4.59±0.87)%, 26.30±1.94] were lower than group B, which showed a dose-dependent reduction and the difference was statistically significant (P<0.05 or P<0.01). Conclusion DB downregulates the expression level of Ca2+-binding protein S100A9 and the mucus secretion amount of the airway goblet cells in rats.

Effect of denatonium benzoate on airway inflammation and remodeling in asthmatic mice / 重庆医学

Objective To evaluate the effect of denatonium benzoaten on α-smooth muscle actin (α-SMA),subepithelial collagen and airway inflammation in asthmu mice.Methods Forty-five BALB/c mice were divided into 3 groups,normal control group (A group),asthma model group (B group),asthma model+ denatonium benzoaten group(C group);α-SMA detected by using immunohistochemistry,lung sections were stained with Masson to detect subepithelial collagen,HE stain method was used to observe the airway inflammation the images were analyzed with semi-quantitative computer.Results The deposition of α-SMA、subepithelial collagen and inflammation degree in C group was significantly reduced compared with B group,the difference were statistically significant(P＜0.05).Conclusion Denatonium benzoaten can improve airway remodeling in asthmatic mice.

Development of fixed-time artificial insemination protocols for locally adapted Curraleiro Pé-Duro cows / Desenvolvimento de protocolos de inseminação artificial em tempo fixo em vacas da raça localmente adaptada Curraleiro Pé-Duro

Two experiments were conducted aiming to evaluate the effects of two ovulatory inducers (Exp.1) and equine chorionic gonadotropin (eCG; Exp.2) on follicular and luteal dynamics in a fixed-time AI (FTAI) protocol in locally adapted Curraleiro Pé-Duro cows. In Exp. 1 multiparous cows (n=12) received an intravaginal device containing 1g of progesterone (P4) for 8 days and 2mg of estradiol benzoate (EB) intramuscularly (IM) at device insertion (Day 0). At device removal (Day 8) 0.150mg of Sodium D-Cloprostenol was administered IM and the cows were randomly assigned to receive 1mg of EB (EB8) or 1mg of estradiol cypionate (EC8) IM, or to not receive any ovulatory inducer (Control). All the animals participated in all treatments (crossover). The interval from P4 removal to ovulation was shorter and less variable in the EB8 treatment group (P≤0.05). In Exp. 2 (crossover), multiparous cows (n=12) received the same hormonal treatment as the EB8 group in Exp.1. At device removal (Day 8) cows were randomly assigned to receive 300UI of eCG IM or to not receive eCG (Control). No difference was ascertained on follicular and luteal parameters in Exp. 2 (P>0.05). We concluded that EB can be used as the ovulatory inducer (Exp. 1) in a FTAI protocol in Curraleiro Pé-Duro cows. However, eCG (Exp. 2) was not able to stimulate follicular and luteal development. This result is probably due to the adaptive capacity of Curraleiro Pé-Duro cows that maintained a satisfactory body condition score even in dry and hot environments.(AU)

Foram realizados dois experimentos com o objetivo de avaliar o efeito de dois indutores da ovulação e da gonadotrofina coriônica equina (eCG) na dinâmica folicular e luteal, em um protocolo de inseminação artificial em tempo fixo (IATF) em vacas localmente adaptadas da raça Curraleiro Pé-Duro. No experimento 1, vacas pluríparas receberam um dispositivo intravaginal contendo 1g de progesterona (P4) durante oito dias e 2mg de benzoato de estradiol (BE) intramuscular (IM) no momento da inserção do dispositivo (dia zero). Na retirada do dispositivo (dia oito), as vacas receberam 0,150mg de D-cloprostenol sódico IM e foram separadas aleatoriamente para receber 1mg de BE IM (BE8) ou 1mg de cipionato de estradiol IM (CE8), ou nenhum indutor da ovulação (controle). Todos os animais participaram de todos os tratamentos (crossover). O intervalo entre a retirada da P4 e a ovulação foi menor e menos variável no tratamento BE8 (P≤0,05). O momento da ovulação foi mais precoce e mais concentrado nos animais do grupo BE 8. No experimento 2 (crossover), vacas pluríparas receberam o mesmo tratamento hormonal do grupo BE8 do experimento1. Na retirada do dispositivo (dia 8), as vacas foram separadas aleatoriamente para receberem 300UI de eCG IM, enquanto o controle não. Não houve diferença nos parâmetros foliculares e luteais avaliados no experimento 2 (P>0,05). Em conclusão, o BE pode ser utilizado como indutor da ovulação (experimento 1) em protocolos de IATF em vacas Curraleiras Pé-Duro. Entretanto, o eCG (experimento 2) não foi capaz de estimular o desenvolvimento folicular e luteal. Esse resultado é devido provavelmente à capacidade adaptativa das vacas Curraleiras Pé-Duro em manter uma condição corporal satisfatória mesmo em condições de clima seco e quente.(AU)

Antioxidant and Immunotropic Properties of some Lithium Salts.

Objective: The antioxidant activity and immuno-tropic effects of lithium glutamate, lithium salicylate, lithium benzoate and lithium lactate have been investigated in this work, as a base for new psychotropic medicines. Methods: The antioxidant properties were studied by the voltammetric method. Phagocytic activity of neutrophilic leucocytes and the reaction of blastic transformation of lymphocytes were used as test for assessments of influence of the lithium compounds on the immune cells of human blood. Results: It was revealed absence of toxic action on human blood cells for all tested substances. Lithium benzoate showed the most significant stimulating influence on lymphocytes. Glutamate and benzoate lithium expressed scavenging activity vs oxygen radicals. Salicylate and benzoate lithium revealed significant phagocytosis stimulation effects. Conclusion: Investigated lithium salts expressed antioxidant activity and immunotropic effects, all investigated substance are of interest in medical application for mental diseases and comorbid pathology treatment.

Simultaneous Determination of Six Active Constituents in Shexiang Baoxin Pills by GC-MS / 中国药师

Objective: To develop a GC-MS method for the simultaneous determination of six active constituents ( borneol, isoborneol, cinnamaldehyde, cinnamic acid, muscone and benzyl benzoate) in Shexiang Baoxin pills. Methods: A gas chromatogra-phy-mass spectrography (GC-MS) method was adopted using a DB-5 capillary column (30 m × 0. 25 mm,0. 1 μm). The column tem-perature was raised as the following program:the initial temperature was 70℃, maintained for 2 min, raised the temperature (5℃· min-1) to 150℃, maintained for 4 min and then raised the temperature (20℃·min-1) to 260℃, and maintained for 3 min. The range of mass-to-electric charge ratio was 10 to 425. Results:The calibration curves of borneol, isoborneol, cinnamaldehyde, cinnam-ic acid, muscone and benzyl benzoate were linear within the range of 0.022-22.000 μg·ml-1(r=0.999 6),0.024-24.000 μg· ml-1(r=0.999 6),0.028-28.000μg·ml-1(r=0.999 8),0.034-34.000μg·ml-1(r=0.999 6),0.040-40.000μg·ml-1(r=0.999 7) and 0.050-50. 000 μg·ml-1 (r =0.999 9), respectively. The average recovery was 97.20%, 97.40%, 97.53%, 99. 60%, 98. 78% and 98. 27% and RSD was 0. 89%, 1. 18%, 1. 52%, 1. 49%, 0. 79% and 1. 74%(n=6), respectively. Con-clusion:The method is accurate, suitable, convenient and reproducible, which can be used for the quality control of multi components in Shexiang Baoxin pills.

Determination and Comparison of the Content of Sodium Benzoate in Medicinal and Non-medicinal Grade by HPLC / 中国药房

OBJECTIVE:To establish a method to determine and compare the contents of sodium benzoate in medicinal(phar-maceutical excipients and active pharmaceutical ingredients) and non-medicinal (chemical reagents and food additives) grade. METHODS:HPLC was conducted for content determination,SPSS 18.0 software was adopted to compare the results. The column was Purospher STAR LP RP-18 endcapped with mobile phase of acetotrile-0.02% formic acid(adjusted pH to 4.0 with aqua ammo-nia)(30∶70,V/V)at a flow rate was 1.0 ml/min,the detection wavelength was 230 nm,column temperature was 35 ℃,and vol-ume injection was 20 μl. RESULTS:The linear range of sodium benzoate was 10.5-525.3 μg/ml(r=0.999 9);RSDs of precision, stability,reproducibility and durability tests were lower than 0.5%;recovery was 99.38%-101.26%(RSD=0.56%,n=9). The av-erage contents of sodium benzoate in medicinal and non-medicinal grade were between 99.400%-99.875%,but the average content of non-medicinal grade is lower than the medical grade. CONCLUSIONS:The method is accurate and simple with high specificity and good reproducibility,and can be used to determine and compare the content of sodium benzoate in medicinal and non-medici-nal grade.

Cytotoxic compounds from the leaves of Garcinia cowa Roxb.

The aims of this study was to isolate compounds from the leaves of methanol extract of Garcinia cowa and to evaluated their cytotoxic activity against breast (MCF-7) and lung (H-460) cell lines. The dichloromethane fraction was separated by successive silica gel column chromatography to give three compounds. Based on spectroscopic comparison with those of the literature these compounds were elucidated as methyl 2,4,6- trihydroxy-3-(3-methylbut-2-enyl)benzoate (1), garcinisidone-A (2) and methyl 4,6dihydroxy-2-(4-methoxy-5- (3-methylbut-2-enyl)-3,6-dioxocylohexa-1,4-dienyloxy)-3-(3-methylbut-2-enyl)benzoate (3). Compound 1, 2 and 3 had IC50 value of 21.0 ± 10.2 μM, 21.2 ±8.4 μM and 17.2 ± 6.2μM against MCF-7, while only compound (2) was found to be in active against H-460 with IC50 value of 18.1 ± 6.7 μM. Conclusion: The results indicate that G. cowa leaves could be important sources of natural cytotoxic compounds and only compound (2) had activity against H-460 cell lines.