Objective To extract and identify the chemical constituents in the leaf and stem of Ervatamia officinalis. Methods The solvent extraction approach and silica column chromatography were used to separate the chemical constituents, and their structures were identified by physicochemical properties and spectra analysis. Results Ten compounds were isolated and their structures were identified as α-amyrin(l),α-amyrin acetate(2),palmitic acid(3), tetratriacontanol(4),stigmasterol(5), (β-daucosterol(6), lupeol(7), calycosin(8), luteolin(9), and glaucocalyxin A(l0). Conclusion Compound l,3∼l0 have been isolated from this plant for the first time, and compound 7, 9 and 10 have been isolated from Ervatamia genus for the first time.

Objective To extract and identify the chemical constituents in the leaf and stem of Ervatamia officinalis. Methods The solvent extraction approach and silica column chromatography were used to separate the chemical constituents, and their structures were identified by physicochemical properties and spectra analysis. Results Ten compounds were isolated and their structures were identified as α-amyrin(l),α-amyrin acetate(2),palmitic acid(3), tetratriacontanol(4), stigmasterol(5), (β-daucosterol(6), lupeol(7), calycosin(8), luteolin(9), and glaucocalyxin A(10). Conclusion Compound l,3~l0 have been isolated from this plant for the first time, and compound 7, 9 and 10 have been isolated from Ervatamia genus for the first time.

0.05).Conclusions SNP of 2350G→A in ACE gene is associated with MI,AA genotype is probably a genetic marker of MI in Han nationality.

A phytochemical investigation on the aerial parts of a Tibetan medicine Meconopsis horridula, by solvent extraction, repeated chromatographies on silica gel, Sephadex LH-20, and preparative TLC techniques, led to the isolation of 9 compounds. By spectroscopic analysis and comparison of its 1H and 13C-NMR data with those in literatures, their structures were identified as oleracein E(1), N-( trans-p-coumaroyl) tyramine (2), chrysoeriol (3), apigenin (4), hydnocarpin (5), p-coumaric acid glucosyl ester (6), stigmast-5-ene-3beta-ylformate (7), 3beta-hydroxy-7alpha-ethoxy-24beta-ethylcholest-5-ene (8), and beta-sitosterol (9), respectively, among which compounds 6-8 were isolated from the genus for the first time,and 1,3 were isolated from the species for the first time. A MTT method was applied to evaluate the cytotoxic activity of compounds 14 against the human hepatocellular liver carcinoma cell line (HepG2), and compound 1 showed significant cytotoxicity against HepG2,with its inhibitory rate of 52.2% at 10 micromol x L(-1).
Medicine, Tibetan Traditional ; Molecular Structure ; Papaveraceae ; chemistry ; Plant Extracts ; chemistry ; Spectrometry, Mass, Electrospray Ionization

Poly(ADP-ribose) polymerase-1 (PARP-1) has emerged as a promising anticancer drug target due to its key role in the DNA repair process. It can polymerize ADP-ribose units on its substrate proteins which are involved in the regulation of DNA repair. In this work, a novel series of para-substituted 1-benzyl-quinazoline-2, 4 (1H, 3H)-diones was designed and synthesized, and the inhibitory activities against PARP-1 of compounds 7a-7e, 8a-8f, 9a-9c and 10a-10c were evaluated. Of all the tested compounds, nine compounds displayed inhibitory activities with IC50 values ranging from 4.6 to 39.2 micromol x L(-1). In order to predict the binding modes of the potent molecules, molecular docking was performed using CDOCKER algorithm, and that will facilitate to further develop more potent PARP-1 inhibitors with a quinazolinedione scaffold.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Drug Design ; Enzyme Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Molecular Docking Simulation ; Molecular Structure ; Poly (ADP-Ribose) Polymerase-1 ; Poly(ADP-ribose) Polymerases ; Quinazolinones ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship

Adolescent ; Adult ; Child ; Child, Preschool ; China ; epidemiology ; Hepatitis B ; epidemiology ; Humans ; Infant ; Middle Aged ; Risk Factors ; Seroepidemiologic Studies ; Young Adult

PARP [poly(ADP-ribose)polymerase] represents a novel potential target in cancer therapy. It is involved in a DNA repair process by catalyzing the transfer of ADP-ribose units from NAD to a number of its substrate proteins. In this work, a series of novel azaindole derivatives was designed and synthesized. Moreover, 16 target molecules were screened and 8 compounds displayed inhibitory activity against PARP-1. It has been demonstrated that these azaindoles bearing cycloamine substituents at 2-position were active to both PARP-1 and PARP-2.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Aza Compounds ; chemical synthesis ; chemistry ; pharmacology ; Indoles ; chemical synthesis ; chemistry ; pharmacology ; Poly (ADP-Ribose) Polymerase-1 ; Poly(ADP-ribose) Polymerases ; metabolism

Objective To compare adductor canal block(ACB)with topical anesthesia for postoperative analgesia in the patients undergoing arthroscopic knee surgery.Methods Sixty patients of both sexes,aged 18-64 yr,with body mass index of 18-30 kg/m2,of American Society of Anesthesiologists physical status ⅠorⅡ,scheduled for elective arthroscopic meniscectomy,were divided into 2 groups (n=30 each) using a random number table:ACB group and topical anesthesia group(TA group).In group ACB,0.2% ropivacaine 20 ml was injected into the adductor canal under the guidance of ultrasound at 30 min before operation to perform ACB.In group TA,0.25% ropivacaine 20 ml was injected into the articular cavity at 5 min before the end of operation.The development of effective analgesia (VAS scores ≤4)and weakened quadriceps femoris muscle strength(muscle strength 0-2 grade,post-operative muscle strength was assessed by using manual muscle testing),related complications(local anesthetic intoxication,bleeding at the puncture site and hematoma) and occurrence of postoperative nausea,vomiting and delayed emergence were recorded.Results Compared with group TA,the rate of effective analgesia within 12 h after surgery was significantly increased (P<0.01),and no significant change was found in the incidence of weakened quadriceps femoris muscle strength,nausea and vomiting in group ACB(P>0.05).Local anesthetic intoxication,bleeding at the puncture site,hematoma or delayed emergence was not observed in the two groups.Conclusion ACB produces better efficacy for postoperative analgesia than topical anesthesia in the patients undergoing arthroscopic knee surgery.

Objective To investigate the changes of serum cardiac troponin I(cTnI)and brain natriuretic peptide(BNP)in heart failure of children with pneumonia and their relationship with heart function.Methods Thirty healthy children aged from 5 months to 3 years old were randomly selected with 17 male and 13 female(healthy group).Thirty children with severe heart failure aged from 3 months to 2 years old were selected at the same time with 21 male and 9 female(heart failure group).Thirty children with ordinary pneumonia aged from 3 months to 3 years old were also sampled with 16 male and 14 female(ordinary pneumonia group).The peripheral bloods of 2-3 mL of all children were taken.The BNP level were measured by enzyme-linked immunosorbent assay and the cTnI level was determined by micro-particle enzyme immunoluminescent.Left ventricular ejection fraction(LVEF) and left ventricular fractional shor-tening(LVFS)were detected by echocardiography.SPSS 11.0 software was used to analyze the data.Results The levels of cTnI [(0.389?0.030) ?g/L] and BNP [(0.572?0.090) ?g/L] of heart failure group increased significantly compared with healthy and ordinary pneumonia group,while their LVEF and LVFS decreased significantly(Pa

Objective　To evaluate the role of transfected angiotensinⅡ(Ang Ⅱ) receptor AT1 anti-sense nucleotide (AT1A) in the expression of subtypes of AngⅡ receptor mRNA, synthesis of protein and nucleic acid in cardiomyocytes. Methods　AT1 cDNA sequence (476 bp) was cloned with RT-PCR and reversely inserted into PcDNA3.1 (5.4 kb) to construct an intact plasmid containing AT1A (PAT1A). The plasmid was then transfected into the cultured cardiomyocytes and identified with RT-PCR and Western blot. The synthesis of protein and nucleic acid identified by 3H-Leu and 3H-TdR incorporation, and expressions of AT1 and AT2 mRNA by RT-PCR, were compared between transfected and nontransfected cardiomyocytes after being stimulated with 10-7 mol/L AngⅡ for 24 h. Results　The plasmid PAT1A were successfully constructed. The AT1 mRNA and its protein were expressed significantly less in the transfected cardiomyocytes than in the control (P<0.01). In the transfected cardiomyocytes, AT1 mRNA expression was markedly decreased, but that of AT2 mRNA obviously increased (P<0.01) when compared with the nontransfected cardiomyocytes after stimulation for 24 h with AngⅡ 10-7 mol/L; no significant difference was found in 3H-Leu and 3H-TdR incorporation between them. Conclusion　After the cardiomyocytes was tranfected with AT1A, the expression of AT1 mRNA was markedly suppressed，while AT2 mRNA up-regulated at the same time. Our results indicate that AT1A blocking can not effectively interrupt the Ang Ⅱ-induced synthesis of the protein and nucleic acid in cardiomyocytes.