Anticancer effect of Psidium guajava (Guava) leaf extracts against colorectal cancer through inhibition of angiogenesis

Objective: To evaluate the anti-angiogenic and anticancer activities of Psidium guajava leaf extracts against angiogenesis-dependent colorectal cancer. Methods: Three extracts were produced using distilled water, ethanol, and n-hexane as solvents. The extracts were physically characterised through gas chromatography-mass spectrometry, ultraviolet-visible spectroscopy, and Fourier transform infrared spectroscopy. Their antioxidant activity was evaluated using the 2,2-diphenyl-1-picrylhydrazyl, total phenolic content, and total flavonoid content assays. To assess their anti-angiogenic activity, cell viability and rat aortic ring assays were conducted, while cell migration, tube formation, colony formation, and VEGF ELISA assays were conducted to elucidate their effects on different aspects of angiogenesis. Molecular docking was used to assess the anti- angiogenic potential of some possible compounds in the extracts. Tumour spheroid assay was used to assess the extracts' potential as a treatment for colorectal cancer. Results: The ethanol extract showed the best antioxidant activity. The distilled water and ethanol extracts exhibited more inhibitory activity against EA.hy926 cell viability and aortic ring microvessel growth. In addition, the ethanol extract performed significantly better than the distilled water extract against cell migration and colony formation, and VEGF expression of the cells was suppressed by the ethanol extract. Both the distilled water and ethanol extracts showed significant inhibitory effect on EA.hy926 tube formation and tumour spheroids consisting of EA.hy926 and HCT116 cells. The ethanol extract contained β-caryophyllene and β-elemene by phytochemical analysis and subsequent docking studies, which may contribute to its anti-angiogenic activity. Conclusions: The ethanol extract of Psidium guajava has potential in the treatment of colorectal cancer through the inhibition of angiogenesis.

Angiosarcoma – a rare fatal cause of recurrent pericardial effusions

@#A 40-year-old man presented to the Hospital Sultanah Bahiyah, Alor Setar, Kedah, with constitutional and respiratory symptoms. Physical examination and echocardiogram demonstrated massive pericardial effusion. Patient required multiple attempts of pericardiocentesis due to recurrent pericardial effusion. Initial workup including pericardial fluids examination and computed tomography imaging did not reveal any apparent cause. Magnetic resonance imaging showed a suspicious mass infiltrating into the right atrium. Autoimmune screening was negative. Patient was subsequently treated as having tuberculous pericarditis. However, his disease progressed rapidly and he eventually passed away due to right atrial rupture. Postmortem revealed a ruptured right atrial tumour leading to massive haemothorax. Histopathological examination confirmed the diagnosis of primary pericardial angiosarcoma.

Comparison of Caesarean sections and instrumental deliveries at full cervical dilatation: a retrospective review

INTRODUCTION@#This study aimed to compare instrumental vaginal deliveries (IDs) and Caesarean sections (CSs) performed at full cervical dilatation, including factors influencing delivery and differences in maternal and neonatal outcomes.@*METHODS@#A retrospective review was conducted of patients who experienced a prolonged second stage of labour at Singapore General Hospital from 2010 to 2012. A comparison between CS and ID was made through analysis of maternal/neonatal characteristics and peripartum outcomes.@*RESULTS@#Of 253 patients who required intervention for a prolonged second stage of labour, 71 (28.1%) underwent CS and 182 (71.9%) underwent ID. 5 (2.0%) of the patients who underwent CS had failed ID. Of the maternal characteristics considered, ethnicity was significantly different. Induction of labour and intrapartum epidural did not influence delivery type. 70.4% of CSs occurred outside office hours, compared with 52.7% of IDs (p = 0.011). CS patients experienced a longer second stage of labour (p < 0.001). Babies born via CS were heavier (p < 0.001), while the ID group had a higher proportion of occipitoanterior presentations (p < 0.001). Estimated maternal blood loss was higher with CSs (p < 0.001), but neonatal outcomes were similar.@*CONCLUSION@#More than one in four parturients requiring intervention for a prolonged second stage of labour underwent emergency CS. Low failed instrumentation rates and larger babies in the CS group suggest accurate diagnoses of cephalopelvic disproportion. The higher incidence of CS after hours suggests trainee reluctance to attempt ID. There were no clinically significant differences in maternal and neonatal morbidity.

Clinical characteristics and therapeutic effect of drug-resistant tuberculosis in children / 中华儿科杂志

Objective@#To explore the clinical characteristics of drug-resistant tuberculosis (TB) in children and to study the effectiveness of second-line anti-TB therapy for children and to examine the incidence of adverse drug reactions.@*Method@#Retrospective research was conducted. The clinical records of children in West China Second Hospital diagnosed as drug-resistant TB from January 2010 to June 2014 were investigated.The clinical characteristics and risk factors were analyzed retrospectively. Treatment effect at discharge was examined as a short-term outcome indicator to evaluate the effectiveness of second-line anti-TB therapy and the incidence of adverse drug reactions. χ2 test was used.@*Result@#Forty-six patients were diagnosed as drug-resistant TB in 443 children infected with TB, with a 10.4% resistance rate. The 46 children included 26 male and 20 female patients, aged from one month and 28 days to 17 years and 5 months, with the average age (8.4±4.5) years, >7 to 14 years old patients as the biggest part(25 patients, 54.3%). Among the 46 children, 20 patients(43.5%)had close contact with TB patients, of whom 12 patients (60.0%) contacted with family members (including parents, brothers and sisters and grandparents living together) and 8 patients(40.0%) contacted with patients from outside family (such as relatives or neighbors). Moreover, 11 cases (23.9%) were under initial treatment and 35 cases (76.1%) were retreated.From 2010 to 2014, the number of cases of initial and retreated patients had no significant difference(0 and 1, 1 and 13, 4 and 7, 4 and 11, 2 and 3 cases, χ2=3.255, P=0.196). Among retreated patients, 31.4% (11/35) had irregular treatment before.Until discharge, the effective rate was 87.0% (40/46), while the incidence rate of adverse drug reaction was 10.9%(5/46).@*Conclusion@#The therapy for drug-resistant TB is effective and the incidence of adverse drug reaction is relatively low.

Differential radiologic characteristics of renal tumours on multiphasic computed tomography

<p><b>INTRODUCTION</b>This study analysed the tumour attenuation characteristics of different subtypes of renal cell carcinomas (RCCs), including clear cell RCC (ccRCC), papillary RCC (pRCC), mixed RCC, chromophobe RCC (chRCC) and oncocytoma.</p><p><b>METHODS</b>We randomly selected 100 RCC cases that underwent nephrectomy between 2004 and 2012 from a collaborative database. Of these cases, 36 were excluded due to the absence of available imaging. The remaining 64 cases comprised 35 ccRCCs, 11 pRCCs, eight chRCCs, seven mixed RCCs and three oncocytomas. The cases were classified as computed tomography (CT) kidney, CT urogram (with plain, nephrographic and pyelographic phases) or CT abdomen (with portovenous and delayed phases). A circular region of interest (ROI) ≥ 1 cmwas drawn and the same standard ROI size was used for each phase at the same site; three different circular ROIs were drawn per lesion per phase. Analysis of variance and t-test were used to examine differences in the radiological characteristics.</p><p><b>RESULTS</b>There was no statistical difference in the attenuation and degree of enhancement between mixed RCCs and ccRCCs. The attenuation and degree of enhancement of the oncocytomas were significantly higher than those of the other RCC subtypes.</p><p><b>CONCLUSION</b>While mixed RCCs did not have attenuation characteristics that differed significantly from those of ccRCCs, oncocytomas can be distinguished from ccRCCs, pRCCs, chRCCs and mixed RCCs by their high radiological density and enhancement. The ability to differentiate oncocytomas from these tumours potentially allows the preoperative selection of patients with small renal masses for conservative management.</p>

Decomposition and Reformulation of Banxia Baizhu Tianma Decoction: A Vasodilatory Approach / 中草药·英文版

Objective To decompose and reformulate Banxia Baizhu Tianma Decoction (BBT) in order to optimize its ratio for vasodilatory effect. The fingerprints of these six component herbs were also studied via Tri-step FTIR analysis. Methods The herbal components of BBT were extracted separately with different solvents, such as 95% ethanol, 50% ethanol, and distilled water. The vasodilatory effect of the extracts was studied using the in vitro pre-contracted aortic ring model. Among these extracts, the water extracts of Pinellia ternata [PT(W)] and Citri reticulatae [CR(W)], 50% ethanol extracts of Gastrodia elata [GE(50)] and Glycyrrhiza uralensis [GU(50)], and 95% ethanol extracts of Atractylodes macrocephala [AM(E)], and Poria cocos [PC(E)] were selected for the orthogonal stimulus-response compatibility group study due to their high effectiveness in vasodilation. Results The best combination ratio (G2) was GE(50), GU(50), AM(E), PC(E), CR(W), and PT(W) at EC0, EC5, EC5, EC5, EC5, and EC5, with EC50 of (0.06 ± 0.01) mg/mL. Comparison between the vasodilatory effects of extracts derived from G2 and BBT were also studied. From the results, the 50% ethanol extract following G2 ratio was found to be most potent extract with the highest vasodilatory effect compared with other extracts derived from G2 or BBT, with EC50 of (0.05 ± 0.005) mg/mL. Conclusion The optimum ratio and appropriate extraction method for the new BBT formulae are obtained. G2 is determined as the best formulae with the highest potency in producing the vasodilatory effect on isolated rat aortic rings. The results obtained suggest that 50% ethanol is found to be the best solvent to extract the vasoactive compounds of G2 in order to exhibit the highest efficacy of vasodilatory effect.

Influential factors for postpartum depression based on the structural equation model in Kaifu District in Changsha / 中南大学学报(医学版)

Objective:To investigate the current status of the postpartum depression in Kaifu District in Changsha,and to explore the influential factors for postpartum depression.Methods:We selected the mothers,who had a delivery and met the inclusion criteria in Changsha during 2015,as the participants and established a prospective birth cohort study.The social demographic characteristics and health-related information for the mothers and their families were collected by using self-made questionnaire.The mothers' depression symptoms after one month postpartum were assessed by the Edinburgh Postnatal Depression Scale.We used the structural equation model to analyze the influential factors for postpartum depression.Results:A total of 961 cases were investigated.82 of them whose scores of EPDS were ≥ 9 points,and the incidence of PPD was 8.2％.The results of structural equation model revealed the influential factors and their correlations with postpartum depression.It has been shown that maternal age,maternal education level,per capita income of family,intention of pregnancy,pregnancy-related complications,mode of conception,mode of delivery,feeding patterns,birth weight,baby gender,and infant illness could exert effects on postpartum depression.Conclusion:The incidence of postpartum depression in Kaifu District is at a low level and the structural equation model can be applied to analyze the influential factors and their relations with postpartum depression.

Compilation of a questionnaire on maternal and child health birth cohort study / 中南大学学报(医学版)

OBJECTIVE@#To compile a questionnaire on maternal and child health birth cohort study, to provide effective tools for exploring the effect of various exposure factors on pregnancy outcome and children's health, and to track children's growth and development dynamically.
@*METHODS@#The preliminary questionnaire on maternal and child health birth cohort study was designed after literature research, health information systems analysis and group discussion. The questionnaire was finalized after expert consultation and pre-survey.
@*RESULTS@#The formal questionnaire on maternal and child health birth cohort study was developed, including maternal health information and children's health information.
@*CONCLUSION@#The questionnaire can be used for collecting maternal health data and children's health data within 1 year old, and this work is useful for scholars in the study on birth cohort invovling the maternal and child health.

Influential factors for anemia in pregnancy based on a nested case-control study in Changsha / 中南大学学报(医学版)

OBJECTIVE@#To explore the prevalence of anemia during pregnancy and the influential factors in changsha city, and to provide scientific evidence for prevention and intervention of anemia during pregnancy. 
@*METHODS@#A cluster sampling of 713 mothers, who delivered baby between January 1, 2013 and December 31, 2013 in the three streets of kaifu district of Changsha, was selected to establish a retrospective cohort. The maternal health information during pregnancy was collected within 15 days after the delivery. The influential factors of anemia during pregnancy were analyzed by the method of retrospective nested case-control study and conditional logistic regression.
@*RESULTS@#The prevalence of anemia during pregnancy in Changsha was 9.96%. The multiple conditional logistic regression results show that high family income (OR=0.632, P=0.020), high education level (OR=0.276, P=0.033), folic acid supplement (OR =0.248, P=0.050), iron supplement (OR=0.272, P<0.001) and eating blood products (OR=0.588, P=0.044) were the beneficial factors for anemia during pregnancy, while multipara (OR=2.917, P=0.003), long duration of menstrual period before pregnancy (OR=1.335, P=0.041), living in new decoration housing (OR=3.690, P=0.045) and tea-drinking (OR=1.365, P=0.094) were the risk factors for anemia during pregnancy. 
@*CONCLUSION@#The prevalence of anemia during pregnancy in Changsha is below the average levels. The occurrence of anemia during pregnancy is closely related to the women's economic level and nutritional status. Women should strengthen maternal nutrition during pregnancy and bedroom environment monitor, drink little strong tea and improve the nutritional status of iron during pregnancy.

A new flavonoid with an aryl moiety from Selaginella uncinata / 中国中药杂志

The present study is to investigate the chemical constituents of the whole plants of Selaginella uncinata. A new flavonoid was isolated from the 75% ethanol extract of Selaginella uncinata by column chromatographies over macroporous resin, silica gel, Sephadex LH-20 and prep-HPLC. The structure was elucidated as 8-[4-(carboxyl)phenoxy]-5,4'-dihydroxy-7-methoxyflavanone (1) and named unciflacone G.

Impact of pre-pregnancy body mass index on baby's physical growth and nutritional status / 中南大学学报(医学版)

OBJECTIVE@#To explore the impact of pre-pregnancy body mass index on baby's physical growth and nutritional status.@*METHODS@#A total of 491 pairs of mother-infant were divided into 3 groups according to mother's pre-pregnancy body mass index (BMI): a pre-pregnancy low BMI group (BMI<18.5 kg/m², n=93), a pre-pregnancy normal BMI group (18.5 kg/m² ≤ BMI<24.0 kg/m², n=326), and a pre-pregnancy high BMI group (BMI ≥ 24.0 kg/m², n=72). Analysis of variance of repeated measurement data and the median percentage methods were used to compare the physical growth and nutritional status of babies in different groups.@*RESULTS@#Baby's weight in the high BMI group were higher than that in the normal BMI and the low BMI group (F=3.958, P=0.020). The incidence of malnutrition in the low BMI group showed a tendency to decline along with the months (χ²=5.611, P=0.018), the incidence of overweight and obesity in the high and the normal BMI groups displayed a tendency to decline along with the months (χ²=18.773, 53.248, all P<0.001). Baby in the low BMI group had higher incidence of malnutrition while baby in the high BMI group had higher incidence of overweight and obesity.@*CONCLUSION@#Pregnancy BMI was correlated with the growth of baby. Too high or too low prepregnancy BMI exerts harmful effect on baby's weight and nutritional status. Medical workers should strengthen the education on women's pre-pregnancy to remind them keeping BMI at normal level.

Effect of clopidogrel on plasma protein binding rate of ginsenosides: a liquid chromatography-mass spectrometry-based study / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the effect of clopidogrel on the binding rate of ginsenosides with rat serum proteins (RSA).</p><p><b>METHODS</b>Equilibrium dialysis and liquid chromatography-mass spectrometry were employed to quantify the concentration of ginsenoside Rg1 and Rb1. The protein-binding rates of Rg1 and Rb1 in the presence or absence of clopidogrel (1.0 mg/L) were determined. A molecular simulation model (consisting of homology modeling and molecular docking interaction) was used to reveal the target protein-compound interactions.</p><p><b>RESULTS</b>The binding rates of ginsenosides Rg1 (0.4, 1.0, and 2.0 mg/L) with RSA were (30.16∓2.82)%, (33.42∓4.21)%, and (34.61∓3.42)%, and those of and Rb1 were (50.13∓2.34)%, (51.23∓3.23)%, and (53.11∓3.26)%, respectively. In the presence of clopidogrel, the binding rates of Rg1 decreased to (22.13∓2.72)%, (21.42∓3.22)%, and (25.45∓3.52)%, and those of Rb1 to (40.13∓3.24)%, (41.25∓4.15)%, and (43.11∓3.31)%, receptively. The molecular docking suggested that these compounds competed to bind with RSA.</p><p><b>CONCLUSION</b>Clopidogrel can competitively bind to RSA with ginsenosides to lower the plasma protein binding rates of ginsenosides.</p>

Study of change in activity of hepatic drug metabolism enzymes in rat model of chronic unpredictable mild stress / 药学学报

This study aimed to explore the impact of depression caused by chronic unpredictable mild stress (CUMS) on in vivo activity of six kinds of CYP450 isoforms in rats. According to 'Katz' method, the model of CUMS was established. Tolbutamide, chlorzoxazone, theophylline, midazolam, omeprazole and dextromethorphan were chosen as probe substrates of CYP2C6, CYP2E1, CYP1A2, CYP3A2, CYP2D1 and CYP2D2 of rats. Plasma concentration of six kinds of CYP450 in control group and model group were determined by LC-MS/MS and computed pharmacokinetic parameters. Consequently, metabolism of theophylline and chlorzoxazone accelerated significantly (P < 0.01), but tolbutamide, dextromethorphan, omeprazole and midazolam had no significant difference. The present study proved that depression caused by CUMS had strong induction to CYP1A2 and medium induction to CYP2E1.

Flavonoids from Selaginella uncinata / 中国中药杂志

In the current study, nine flavonoids were isolated and purified from 75% ethanol extract of Selaginella uncinata (Desv.) Spring by column chromatographic techniques over macroporous resin, polyamide, silica gel, Sephadex LH-20 and pre-HPLC. On the basis of their physico-chemical properties and spectroscopic data analyses, these compounds were elucidated as cirsimarin (1), nepitrin (2), apigenin-6-C-α-L-arabinopyranosyl-8-C-β-D-glucopyranoside (3), apigenin-6-C-β-D-glucopyranosyl-8-C-α-L-arabinopyranoside (4), apigenin-7-O-β-D-glucopyranoside (5), 2,3-dihydroamentoflavone (6), 4'-O-methylamentoflavone (7), 2,3-dihydro-4'-O-methyl-amentoflavone (8), and 2,3,2",3"-tetrahydron-4'-O-methyl-robustaflavone (9). Compounds 1-5 belong to flavonoid glycosides and were isolated from the genus Selaginella for the first time.

Study on biomarker of Tripterygium wilfordii in treatment of rheumatoid arthritis based on PK/PD / 中国中药杂志

To observe the serum samples and the anti-inflammatory effect of Tripterygium wilfordii in treating RA by using the pharmacokinetic-pharmacodynamic model, make a correlation analysis on concentration-time and effect-time curves, and explore RORγt, IL-17, STAT3, IL-6 mRNA transcriptional levels in rats by PCR. Methotrexate, tripterine and high-dose T. wilfordii could down-regulate RORγt, IL-17, STAT3, IL-6 mRNA transcriptional levels in AA rat lymph nodes. The study on PK-PD model showed correlations between inflammatory factors and blood concentration of T. wilfordii. T. wilfordii and its main active constituent tripterine could show the inflammatory effect and treat RA by inhibiting IL-17 cytokine.

Epidemiological study on nasal carriage in hospitalized children infected with Staphylococcus aureus / 中国当代儿科杂志

<p><b>OBJECTIVE</b>To study the relationship between nasal carriage and Staphylococcus aureus (S. aureus) infection in hospitalized children.</p><p><b>METHODS</b>Fifty-six hospitalized children infected with S. aureus were recruited in this study. Nasal swabs were collected and cultured, and the nasal carriage rate of S. aureus was examined. PVL virulence gene and mecA resistance gene were both detected in clinical strains and nasal carriage strains by PCR.</p><p><b>RESULTS</b>Twenty-two (39%) of the 56 children had nasal carriage of S. aureus, and most of them (18 cases) were younger than one year. Among these 22 children, 11 (50%) had previous hospitalization over the past year. In the infected strains, the rate of methicillin-resistant S. aureus (MRSA) was 29% (16/56), while it was 32% (7/22) in carriage strains. The mecA positive results in clinical strains were consistent with the results in nasal carriage strains. Among 5 PVL-positive nasal carriage strains, 4 (90%) could be matched with their clinical strains, all of which were MRSA.</p><p><b>CONCLUSIONS</b>Nasal carriage is a potential risk factor for S. aureus infection. Nosocomial transmission may lead to nasal carriage, which can cause S. aureus infection. The isolation rate of MRSA is high in hospitalized children infected with S. aureus, which implies that more attention is needed for this situation. The isolates from noses may be clonally identical to the isolates from clinical secretions, and the homology between them needs to be confirmed by multi-locus sequence typing.</p>

Biotransformation and involved CYP450 isomers of bioactive xanthone HM-1 from Halenia elliptica, D. Don in rat liver microsomes / 中国药学杂志

OBJECTIVE: To study the biotransformation of bioactive xanthones 1-hydroxyl-2, 3, 5-trimethoxyxanthone (HM-1) from Halenia elliptica, D. Don and five mostly common CYP450 isoforms involved of the its metabolism in rat liver microsomes (RLMs).

Determination of plasma concentration of five phenolic acid by LC-MS/MS and study of pharmacokinetics in rats after Mailuoning injection / 中国中药杂志

To establish a LC-MS/MS method for quantification of chlorogenic acid, caffeic acid, 3,4-DCQA, ferulic acid and cinnamic acid in rats plasma and study its pharmacokinetics after administration of Mailuoning injection at a single dose to rats. Plasma samples were acidified with hydrochloric acid and extracted with ethyl acetate. The analytes were determined by LC-MS-MS using a ZOBAX SB C18 column with a mobile phase of methanol-water (containing 2 mmol x L(-1) ammonium acetic) (60:40)at a flow rate of 0.5 mL x min(-1) and detected using ESI with negative ionization mode. Ions monitored in the multiple reaction monitoring (MRM) mode were m/z 353.1/191.0 [M-H]- for chlorogenic acid, m/z 178.9/134.9 [M-H]- for caffeic acid, m/z 515.2/353.0 [M-H]-for 3,4-DCQA, m/z 193.0/133.9 [M-H]-for ferulic acid, m/z 146.9/102.9 [M-H]- for cinnamic acid and m/z 246.0/125.8 [M-H]- for tinidazole (IS). After administration of Mailuoning injection at a single dose to eight Sprague-Dawley rats, the concentrations of chlorogenic acid, caffeic acid, 3,4-DCQA, ferulic acid and cinnamic acid in plasma were determined by LC-MS/MS method. The main pharmacokinetics parameters of measured data were caluculated by using DASver 1.0 software. The linear concentration ranges of the calibration curves for chlorogenic acid, caffeic acid, 3,4-DCQA and cinnamic acid were 2.006-1,027 microg x L(-1) (r = 0.999 6), 1.953-1,000 microg x L(-1) (r = 0.999 7), 28.51-1.459 x 10(4) microg x L(-1) (r = 0.998 9), 1.836-940.0, g x L(-1) (r = 0.997 7) and 4.780-2,447 microg x L(-1) (r = 0.998 6) respectively. The inner and inter-days relative standard deviations were both less than 5.0%, indicating legitimate precise and accuracy to the requirement of biological sample analysis. For chlorogenic acid, the pharmacokinetic parameter t1/2, AUC0-t, and CL were (49.78 +/- 12.81) min, (123.55 +/- 14.82) mg x min x L(-1) and (0.004 3 +/- 0.000 5) L x min(-1), respectively. For caffeic acid, the pharmacokinetic parameter t1/2, AUC0-t, and CL were (36.65 +/- 10.59) min, (91.67 +/- 11.77) mg x min L(-1) and (0.005 7 +/- 0.000 7) L x min(-1), respectively. For 3,4-DCQA, the pharmacokinetic parameter t1/2, AUC0-t, and CL were (50.08 +/- 13.78) min, (278.34 +/- 31.82) mg x min x L-1 and (0.001 6 +/- 0.000 2) L x min(-1), respectively. For ferulic acid, the pharmacokinetic parameter t1/2, AUC0-t, and CL were (51.39 +/- 15.52) min, (34.72 +/- 4.67) mg x min x L(-1) and (0.000 4 +/- 0.0001) L x min(-1), respectively. For cinnamic acid, the pharmacokinetic parameter t1/2, AUCo-t, and CL were (74.42 +/- 18.32) min, (34.63 +/- 4.82) mg x min x L(-1) and (0.007 7 +/- 0.001 1) L x min-', respectively. The assay method is proved to be sensitive, accurate and convenient. It can be applied to the pharmacokinetic study of chlorogenic acid, caffeic acid, 3,4-DCQA, ferulic acid and cinnamic acid.

Study on determination of caffeic acid, chlorogenic acid in rat plasma and their pharmacokinetics with LC-MS/MS / 中国中药杂志

To establish a LC-MS/MS method to determine caffeic acid, chlorogenic acid in rat plasma and study their pharmacokinetics in rats. Six Sprague-Dawley rats were intravenously injected with 4 mL x kg(-1) of Dengzhanxixin injection, respectively. Their drug plasma concentration was determined by LC-MS/MS, with tinidazole as an internal standard. The pharmacokinetic parameters were calculated by DAS 1.0. The linear concentration ranges of caffeic acid, and chlorogenic acid were 2-128 microg x L(-1) (r = 0.998 1) and 3-384 microg x L(-1) (r = 0.998 7), respectively. The methodological test showed conformance to the requirements. The intraday and inter-day variable coefficients were both less than 10.0%, indicating that both of legitimate precise and accuracy were in conformity with the requirements of biological sample analysis. For caffeic acid, the pharmacokinetic parameter t1/2beta AUC0-t, and CL were (130.91 +/- 38.77) min, (4.89 +/- 0.96) mg x min x L(-1) and (0.12 +/- 0.02) L x min(-1) x kg(-1), respectively. For chlorogenic acid, the pharmacokinetic parameter t1/2beta , AUC0-t, and CL were (49.38 +/- 8.85) min, (9.54 +/- 0.95) mg x min x L(-1) and (0.09 +/- 0.003) L x min(-1) x kg(-1), respectively. The LC-MS/MS analysis method established in this study was proved to be so accurate and sensitive that it can be applied to the pharmacokinetic study of caffeic acid and chlorogenic acid.

Screening of differentially expressed microRNAs in borderline and malignant gastrointestinal stromal tumors / 中华病理学杂志

<p><b>OBJECTIVE</b>Gastrointestinal stromal tumors (GISTs) have a broad spectrum of biological behaviors ranging from benign, borderline and malignant. This study aimed to screen differentially expressed microRNAs (miRNAs) between malignant and borderline GISTs and to investigate the potential role of miRNAs in the malignant transformation of GISTs.</p><p><b>METHODS</b>Six GIST samples including borderline tumors (n = 3) and malignant tumors (n = 3) were collected based on the clinical and pathological characteristics. Total RNA was extracted, followed by miRNA microarray analysis to screen the differentially expressed miRNAs. The most significantly expressed 4 miRNAs were then chosen for further validation by real-time PCR in 22 additional GIST samples.</p><p><b>RESULTS</b>Direct comparison of malignant group versus borderline group revealed 14 significantly and differentially expressed miRNAs (P < 0.05, with a fold change of < 0.5 or > 2). Five miRNAs were up-regulated and nine were down-regulated in the malignant group. Four miRNAs (miR-221, miR-135b, miR-675(*) and miR-218) were most significantly and differentially expressed between the two groups. The differential expression of 2 miRNAs (miR-221 and miR-675(*)) were subsequently confirmed with good concordance by real-time PCR.</p><p><b>CONCLUSIONS</b>The differential miRNA expression profiles between two groups are revealed by miRNA microarray assay, and confirmed by real-time PCR. Among differentially expressed miRNAs, miR-221 and miR-675(*) might be related to the malignant transformation of GISTs, and have a potential value in predicting biological behavior of GISTs.</p>