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1.
Zhonghua Wai Ke Za Zhi ; 59(12): 987-993, 2021 Dec 01.
Artigo em Zh | MEDLINE | ID: mdl-34839613

RESUMO

Objective: To investigate the long-term efficacy and safety of alternating double balloon occlusion combined with intra-aneurysm injection of human fibrin binder in the endovascular repair of ruptured abdominal aortic aneurysm (rAAA). Methods: The clinical data of 28 patients with rAAA admitted to Department of Vascular Surgery, the Fourth Affiliated Hospital of Guangxi Medical University from January 2015 to December 2019 were retrospectively analyzed. There were 23 males and 5 females, aged (62±5) years (range: 46 to 88 years).The maximum diameter of the tumors was (65.2±10.5) mm (range: 47.3 to 100.5 mm), all of which were subrenal rAAA. The intraoperative EVAR for abdominal aortic aneurysm was successfully performed under the emergency green channel procedure, and this surgery was assisted used the double balloon occlusion technique in aorta of inferior renal and superior renalcombined with intraoperative human fibrin binder injection technique. Observation indexes included: patients with preoperative preparation, operation time, hospitalization days, surgical treatment success rate and the incidence of postoperative complications, and aortic stent form during the follow-up period, the incidence of leakage, branch stents patency rate and infection rates. Results: The preoperative preparation time of 28 patients was (45.5±8.5) minutes (range:20 to 100 minutes). The operation time was (100.0±15.5) minutes (range:85 to 210 minutes), the ICU stay time was (7±2) days(range:1 to 17 days). The length of hospitalization was (13.5±2.5) days(range:5 to 43 days). The success rate of surgical treatment was 92.9% (26/28). Two patients died, 1 case died of postoperative multifocal lacunar cerebral infarction and massive gastrointestinal hemorrhage, and another elderly patient (84 years old) died of massive abdominal fluid due to preoperative abdominal aortic aneurysm rupture, postoperative complicated with significant abdominal compartment syndrome, and secondary multiple organ failure. Balloon occlusion of the upper renal aorta took (13±2)minutes (range:12 to 30 minutes). The intraoperative injection of fibrin adhesive was (14±2) ml(range:6 to 28 ml) in 22 cases. The incidence of major postoperative complications was 57.1% (16/28). Among the 26 patients who survived the surgery, 69.2% (18/26) completed the 3-year follow-up, and the follow-up time was (30±3) months(range:13 to 36 months). During the follow-up, the aortic stent was in good shape without obvious displacement. The incidence of leakage within 6 months after the operation was 10.7% (3/28), and there was no internal leakage in the patients who were followed up for 36 months after the operation. The patency rate of renal artery and iliac artery branch stents was 16/18. The incidence of stent infection was 7.7% (2/26), 1 case occurred at 1 month and another case at 6 months, respectively. All patients recovered after prolonged intensive anti-infection therapy. Conclusions: Under the standard emergency treatment process, the double balloon alternating occlusion technique combined with the intra-aneurysm injection of human fibrin adhesive technique can assist the successful completion of the endovascular repair of rAAA, effectively improve the success rate of treatment for patients, and reduce the incidence of postoperative leakage and serious complications. The mid-term and long-term results of EVAR for rAAA are good, safe and reliable.


Assuntos
Aneurisma da Aorta Abdominal , Oclusão com Balão , Implante de Prótese Vascular , Procedimentos Endovasculares , Idoso , Idoso de 80 Anos ou mais , Aneurisma da Aorta Abdominal/cirurgia , China , Feminino , Fibrina , Humanos , Masculino , Pessoa de Meia-Idade , Complicações Pós-Operatórias/terapia , Estudos Retrospectivos , Stents , Resultado do Tratamento
2.
Zhonghua Yi Xue Za Zhi ; 98(40): 3263-3267, 2018 Oct 30.
Artigo em Zh | MEDLINE | ID: mdl-30392293

RESUMO

Objective: To investigate whether the assisted reproductive techniques (ART) outcomes can be improved by using magnetic-activated cell sorting combined isolate density gradient centrifugation (MACS-DGC), and to compare the results with the conventional isolate density gradient centrifugation (DGC) method. Methods: In the period from January to December 2014, patients who attended the andrology laboratory for sperm DNA fragmentation analysis and underwent the in vitro fertilization and embryo transfer (IVF-ET) treatment were divided into 3 groups, and each group has two subgroups according to the way of fertilization : in vitro fertilization (IVF) as subgroup 1 and intracytoplasmic sperm injection (ICSI) as subgroup 2. Group A (A1, A2 ): DNA fragmentation index(DFI)≥20 and using MACs; Group B (B1, B2): DFI≥20 and using isolate method; Group C (C1, C2): DFI<20 and using isolate method. The fertilization rate, good-quality embryos, implantation rate, pregnancy rate and live-birth rate of each group were analyzed. Results: Similar results were obtained among groups for all the parameters compared: On IVF cycles no significant difference was observed in fertilization rate, percentage of good-quality embryos on day 3, implantation rate, positive beta-hCG tests, and live-birth rate among the three subgroups (A1 vs B1 vs C1). Between the subgroups of ICSI cycles (A2 vs B2 vs C2) the percentage of high-quality embryos, pregnancy rate, implantation rate and live-birth rate were all significantly higher in the MACS-DGC (A2) group compared to DGC alone (B2). Conclusion: Based on the results, MACS as a part of sperm preparation technique will not improve sperm fertilizing potential, embryos quality, implantation rate, pregnancy rate or live-birth rate of IVF, but it may help select the most fertile sperm and to improve clinical outcomes of ICSI.


Assuntos
Centrifugação com Gradiente de Concentração , Espermatozoides , Fragmentação do DNA , Feminino , Fertilização in vitro , Humanos , Masculino , Gravidez , Taxa de Gravidez , Técnicas de Reprodução Assistida , Injeções de Esperma Intracitoplásmicas
3.
Zhonghua Yi Xue Za Zhi ; 98(12): 930-934, 2018 Mar 27.
Artigo em Zh | MEDLINE | ID: mdl-29665668

RESUMO

Objective: To discuss the feasibility, effect and safety of lower abdominal aorta balloon occlusion technique by ultrasound guiding during caesarean section in patients with pernicious placenta previa. Methods: The clinical data of 40 patients with pernicious placenta previa complicated with placenta accreta from January 2015 to August 2017 in Liuzhou workers hospital were analyzed retrospectively. The study group included 20 cases, which were operated in the way of cesarean section combined lower abdominal aorta balloon occlusion technique by ultrasound guiding, while the control group also included 20 cases, which were operated in the way of the conventional cesarean section without balloon occlusion technique. The bleeding amount, blood transfusion volume, operative total time, hysterectomy and complications of the two groups were compared. Results: The bleeding amount and blood transfusion volume in study group were(850±100)ml and (400±50)ml, which were lower than that of the control group[(2 500±230)ml and (1 500±100)ml], the difference was statistically significant(t=35.624, 16.523, all P<0.05). In addition, the hysterectomy rate in study group was 5%, which was lower than that in the control group(30%), the difference was statistically significant(χ2=8.672, P<0.05). And the total time of operation was (2.0±0.5)h in the study group, which was shorter than that in the control group[(3.5±0.4)h]. The difference was statistically significant(t=11.362, P<0.05). No postoperative complications took place in the study group.The blood pressure, heart rate and blood oxygen fluctuated significantly, and the postoperative renal function was significantly reduced in the control group. Conclusions: The lower abdominal aorta balloon occlusion technique by ultrasound guiding during a caesarean section in patients with pernicious placenta previa can effectively control the bleeding during operation, and preserve reproductive function to the utmost degree.Therefore, the technique is safe, feasible, convenient and cheaper, and worthy of being widely applied in clinic.


Assuntos
Oclusão com Balão , Aorta Abdominal , Perda Sanguínea Cirúrgica , Cesárea , Feminino , Humanos , Histerectomia , Placenta Prévia , Hemorragia Pós-Parto , Gravidez , Estudos Retrospectivos
4.
Hum Reprod ; 26(7): 1860-7, 2011 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-21489975

RESUMO

BACKGROUND: The objective of this study was to explore the potential for vertical transmission of hepatitis B virus (HBV) from parents to offspring via human germ cells. METHODS: For study samples, 250 oocytes from hepatitis B surface antigen (HBsAg) seropositive women and 578 embryos from couples with at least one HBsAg seropositive partner were collected. HBV DNA in the nuclei of oocytes and embryos was detected by fluorescence in situ hybridization; HBsAg expression was analysed using immunofluorescence; and serum HBV DNA levels were measured by real-time PCR. The HBV infection duration of the women and the serum HBsAg status of their mothers were also examined. RESULTS: HBV DNA was present in 9.6% (24/250) of oocytes and 14.4% (83/578) of embryos. Rates of HBV DNA positive embryos were similar among couples in which the woman, man or both partners were HBsAg seropositive, 13.1% (57/436), 21.3% (16/75) and 14.9% (10/67), respectively. Rates of positivity in oocytes and embryos were significantly higher in a group with high serum levels HBV DNA than in a group with lower serum levels (P= 0.004 and P= 0.002, respectively). Higher rates of oocyte positivity were found for women whose mothers were HBV infected compared with those with uninfected mothers. Expression of HBsAg was observed in 8.7% (2/28) oocytes and 14.1% (10/71) embryos (P= 0.34). CONCLUSIONS: The presence of HBV DNA in human oocytes or embryos was related to the women's serum levels of HBV DNA and the infection status of their mothers. The HBV positive embryos were either maternally or paternally dependent. HBV infection may result in vertical transmission to the offspring via germ cells.


Assuntos
Embrião de Mamíferos/virologia , Hepatite B/transmissão , Transmissão Vertical de Doenças Infecciosas , Oócitos/virologia , DNA Viral/análise , Feminino , Hepatite B/imunologia , Antígenos de Superfície da Hepatite B/sangue , Vírus da Hepatite B/imunologia , Vírus da Hepatite B/isolamento & purificação , Humanos , Hibridização in Situ Fluorescente
6.
Artigo em Zh | MEDLINE | ID: mdl-29873216

RESUMO

Objective:To remove the immune function of children with obstructive sleep apnea hypopnea syndrome by resection of adenoids and tonsillar. Method: The fasting peripheral venous blood of children with OSAHS and healthy children were collected. The lymphocyte subsets, NK cells and immunoglobulin levels were compared between the two groups. The fasting blood samples of OSAHS children were collected again after 2d, 30d, 60d and 90d after operation. The changes of lymphocyte subsets, NK cells and immunoglobulin levels were observed after operation. Result: Before operation, at the 0.05 test level, it was not yet clear that the levels of IgG, IgM, IgA, NK, CD3+, CD4+ and CD8+ in OSAHS children were significantly different from those in the control group. The levels of IgA, CD3+ and CD4+ decreased significantly in children at 2d and OSAHS after operation, and IgG, IgM, IgA, NK, CD3+ and IgA continued to rise after 60d until ninetieth day after operation. Conclusion: There is no statistical disorder of immune level in children with OSAHS compared with healthy children. The implementation of adenoidectomy and tonsillectomy in children with OSAHS, the level of immunity in 90 days can be restored to the preoperative level.


Assuntos
Adenoidectomia , Antígenos CD/análise , Imunoglobulinas/análise , Apneia Obstrutiva do Sono/imunologia , Apneia Obstrutiva do Sono/cirurgia , Tonsilectomia , Tonsila Faríngea , Criança , Humanos , Tonsila Palatina
7.
Ultrason Sonochem ; 13(1): 28-31, 2006 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-16223683

RESUMO

Differential functionalization of the phenolic groups in genistein was carried out in excellent yields under ultrasonic irradiation. The isoflavone ring had proved to be unstable under stirring at 60 degrees C and phenyl benzyl ketone was unexpectedly isolated instead of the genistein derivative.


Assuntos
Genisteína/análogos & derivados , Genisteína/síntese química , Sonicação , Genisteína/isolamento & purificação , Genisteína/efeitos da radiação , Isomerismo
8.
Artigo em Zh | MEDLINE | ID: mdl-29798016

RESUMO

Objective:To observe the clinical effect of tympanostomy tube insertion with adenoidectomy for children with recurrent otitis media with effusion. Method:One hundred and twenty-six cases of children with recurrent otitis media were randomly divided into observation group and control group(63 in each group), subsequently compared the therapeutic effect of the two groups which observation group had tympanostomy tube insertion with adenoidectomy and the other group had only tympanostomy tube insertion. Result:In terms of the total effective rate,observation group and control group were 96.82% and 76.19% respectively, the difference had statistical significant(P<0.05);compared to control group, the recurrent rate of observation group after treatment was extremely lower, the same as middle ear cavity effusion time, which both had statistical significance (P<0.05); the complete healing time of two groups had no statistical significance(P>0.05). Conclusion:Tympanostomy tube insertion with adenoidectomy has significant treatment effect for children with recurrent otitis media with effusion, it could reduce the recurrent rate after surgery and shorten the time of middle ear cavity effusion.


Assuntos
Adenoidectomia , Ventilação da Orelha Média , Otite Média com Derrame/cirurgia , Criança , Pré-Escolar , Feminino , Humanos , Masculino , Otite Média/cirurgia , Recidiva
10.
Org Lett ; 1(1): 91-3, 1999 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-10822541

RESUMO

[formula: see text] The new crystalline phosphate reagent 3-(diethoxyphosphoryloxy)-1,2,3-benzotriazin-4(3H)-one (DEPBT) mediates amide bond formation with a remarkable resistance to racemization. Comparative racemization studies were carried out and DEPBT proved to be superior to typical phosphonium and uronium coupling reagents. DEPBT is easily prepared and is exceedingly stable with a shelf life of months at room temperature. The advantageous properties of DEPBT render it a useful and unique addition to the arsenal of coupling reagents.


Assuntos
Organofosfatos/química , Triazinas/química , Amidas/química , Estereoisomerismo
11.
FEMS Microbiol Lett ; 241(1): 67-72, 2004 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-15556711

RESUMO

Fractionation of the extract of Aspergillus niger. IFB-E003, an endophyte in Cyndon dactylon, gave four known compounds naphtho-gamma-pyrones rubrofusarin B, fonsecinone A, asperpyrone B and aurasperone A, which were further investigated biologically. Rubrofusarin B was shown to be cytotoxic to the colon cancer cell line SW1116 (IC50: 4.5 microgml-1), and aurasperone A inhibitory on XO (xanthine oxidase) (IC50: 10.9 micromoll-1). Moreover, the four naphtho-gamma-pyrones exhibited growth inhibitions against the five test microbes with MICs ranging in between 1.9 and 31.2 microgml(-1). The present recognition of rubrofusarin B and aurasperone A as strong co-inhibitors on XO, colon cancer cell and some microbial pathogens is of significance for the imperative discovery of new relevant therapeutic agents.


Assuntos
Anti-Infecciosos/farmacologia , Aspergillus niger/metabolismo , Inibidores Enzimáticos/farmacologia , Pironas/farmacologia , Xantina Oxidase/antagonistas & inibidores
12.
Steroids ; 58(1): 35-9, 1993 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-8430443

RESUMO

A series of amino acid and peptide derivatives of estradiol have been synthesized by coupling 17 beta-aminoestra-1,3,5(10)-trien-3-ol, 17-hydrazonoestra-1,3,5(10)-trien-3-ol with amino acids or peptides, using tetrahydrothiazole-2-thione, N-hydroxy-1,4-epoxycyclohex-5-ene-2,3-dicarbonylimide, benzotriazolyloxy-tris(dimethylamino)phosphonium hexafluorophosphate, and p-nitrophenol as reagents. N-protected peptidyl steroids were deprotected by traditional methods. The relative binding affinities of the deprotected derivatives to the estrogen receptor were determined by competitive radioligand binding assay.


Assuntos
Aminoácidos/síntese química , Estradiol/análogos & derivados , Peptídeos/síntese química , Receptores de Estrogênio/metabolismo , Aminoácidos/química , Aminoácidos/metabolismo , Animais , Ligação Competitiva , Estradiol/química , Estradiol/metabolismo , Feminino , Indicadores e Reagentes , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Peptídeos/química , Peptídeos/metabolismo , Ratos , Útero/metabolismo
13.
Scand J Work Environ Health ; 12(4 Spec No): 289-92, 1986 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-3490686

RESUMO

Vibration syndrome caused by hand-held vibrating tools in 14 locomotive and rolling stock plants in four regions of the People's Republic of China (south, north, middlewest, and northeast) and the influence of climatic factors on its prevalence rate were studied. For 1,028 male workers (705 riveters, 284 chippers, and 39 grinders), the prevalence rate of the syndrome was 13.4% and for a reference group of 256 workers it was 1.6%. The prevalence rate of white finger in the four regions differed and was higher in northeast and north China than in south and middlewest China. This finding suggests that cold climate and humidity may be causative factors of the vibration syndrome.


Assuntos
Clima , Dedos/irrigação sanguínea , Doenças Profissionais/epidemiologia , Ferrovias , Doença de Raynaud/epidemiologia , Vibração/efeitos adversos , Adolescente , Adulto , China , Estudos Transversais , Humanos , Masculino , Pessoa de Meia-Idade , Ocupações , Doença de Raynaud/etiologia , Síndrome
14.
Fa Yi Xue Za Zhi ; 17(4): 214-7, 2001 Nov.
Artigo em Zh | MEDLINE | ID: mdl-12533874

RESUMO

OBJECTIVE: To study the distribution and metabolism of methamphetamine in the hair of guinea pig. METHODS: Determination of methamphetamine and its metabolite amphetamine in hair was performed by GC/MS and GC/NPD. Concentration-time course of methamphetamine and amphetamine in hair of guinea were recorded. Relationship between hair color, administrated dose and drug concentration in hair were also discussed. RESULTS: The concentration of amphetamine is higher than the concentration of methamphetamine in the hair of guinea administrated a single dose or seven doses of methamphetamine. The concentration of methamphetamine and amphetamine were significantly related with administration dose and the incorporation rate into white and brown hair is much poorer than that of black hair. CONCLUSION: Administration methods, dose and the color of hair affect the concentration of methamphetamine and amphetamine.


Assuntos
Cabelo/metabolismo , Metanfetamina/metabolismo , Anfetamina/administração & dosagem , Anfetamina/metabolismo , Animais , Cobaias , Cor de Cabelo , Masculino , Metanfetamina/administração & dosagem
15.
Placenta ; 35(9): 691-5, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-25063251

RESUMO

OBJECTIVE: Several biomarkers, including maternal serum creatinine kinase and α-fetoprotein, have been described as potential tools for the diagnosis of placental abnormalities. This study aimed to determine whether maternal plasma mRNA levels of the ß subunit of human chorionic gonadotropin (ß-HCG) could predict placenta accreta prenatally. METHODS: Sixty-eight singleton pregnant women with prior cesarean deliveries (CDs) were classified into three groups: normal placentation (35 women, control group); placenta previa alone (21 women, placenta previa group); and both placenta previa and placenta accreta (12 women, placenta previa/accreta group). Maternal plasma concentrations of cell-free ß-HCG mRNA were measured by real-time reverse-transcription polymerase chain reaction and were expressed as multiples of the median (MoM). RESULTS: Cell-free ß-HCG mRNA concentrations (MoM, range) were significantly higher in women with placenta accreta (3.65, 2.78-7.19) than in women with placenta previa (0.94, 0.00-2.97) or normal placentation (1.00, 0.00-2.69) (Steel-Dwass test, P < 0.01 and P < 0.01, respectively). In the placenta previa/accreta group, the concentration of cell-free ß-HCG mRNA was significantly higher among women who underwent CDs with hysterectomy (4.41, 3.49-7.19) than among women whose CDs did not result in hysterectomy (3.20, 2.78-3.70) (Mann-Whitney U test, P = 0.012). DISCUSSION: An increased level of cell-free ß-HCG mRNA in the maternal plasma of women with placenta accreta may arise from direct uteroplacental transfer of cell-free placental mRNA molecules. CONCLUSIONS: The concentration of cell-free ß-HCG mRNA in maternal plasma may be applicable to the prenatal diagnosis of placenta accreta, especially to identify women with placenta accreta likely to require hysterectomy.


Assuntos
Gonadotropina Coriônica Humana Subunidade beta/metabolismo , Placenta Acreta/sangue , Placenta Prévia/sangue , Adulto , Biomarcadores/sangue , Estudos de Casos e Controles , Feminino , Humanos , Imageamento por Ressonância Magnética , Placenta/metabolismo , Placenta Acreta/diagnóstico por imagem , Placentação , Gravidez , RNA Mensageiro/sangue , Reação em Cadeia da Polimerase em Tempo Real , Ultrassonografia
18.
J Appl Microbiol ; 100(1): 195-202, 2006.
Artigo em Inglês | MEDLINE | ID: mdl-16405700

RESUMO

AIMS: Fungal infection is still a life-threatening risk for the immunocompromised population such as AIDS patients and those who receive treatments with immunosuppressors and/or frequent administrations of wide-spectrum antibiotics, which inevitably lead to the drug resistance and unbalanced microflora populations. The present work was accordingly performed to characterize more potent antifungal metabolites from various cultures of marine fungi residing in white croaker Argyrosomus argentatus. METHODS AND RESULTS: The three most common opportunistic human pathogens Candida albicans (CCCCM ID 00148), Aspergillus niger (CCCCM ACCC 30005) and Trichophyton rubrum (CCCCM ID 00001) were selected as test fungi. A total of 16 cultivable fungal strains were isolated from the variant tissues of Ar. argentatus collected from the Yellow Sea, followed by preliminary antifungal screenings of the EtOAc extracts of the corresponding cultures. As a result, the inhibition of the three target fungi, plus being allergic to isolators' skin, were discerned with the EtOAc extract of the fungus under the isolation number Z16 that was identified subsequently as Myrothecium sp. by a combination of morphological and 18S rDNA finger-typing characteristics. A follow-up bioassay fractionation of the EtOAc extract, in conjunction with spectral analyses [MS, (1)H-NMR, (13)C-NMR, distortionless enhancement by polarization transfer (DEPT), heteronuclear multiple quantum coherence (HMQC) and heteronuclear multiple bond resonance (HMBC)] wherever required, afforded eventually the characterization of a new acid (compound 1: 4,5-ditridecyl-octanedioic acid), three macrocyclic trichothecenes including roridin A (compound 2), verrucarin A (compound 3) and 8beta-acetoxy-roridin H (compound 4), (22E,24R)-cerevisterol (compound 5) and N-phenyl-beta-amino-naphthalene (compound 6). In vitro antifungal tests showed that the three trichothecenes were active against A. niger, T. rubrum and C. albicans with MICs of 31.25, 62.5 and 125 microg ml(-1) for compound 2, 250, 125 and 31.25 microg ml(-1) for compound 3 as well as 125, 62.5 and 125 microg ml(-1) for compound 4 respectively. The MICs of ketoconazole (co-assayed herewith as a positive reference) against A. niger, T. rubrum and C. albicans were 31.25, 250, 31.25 microg ml(-1) respectively. A preliminary structure-activity relationship of the antifungal trichothecenes was highlighted in brief. CONCLUSIONS: The present investigation demonstrated that marine fungus Myrothecium sp. Z16 associated with white croaker (Ar. argentatus), was an efficient producer of a new acid and antifungal trichothecenes, the latter presumably being also the allergic substances in the culture. SIGNIFICANCE AND IMPACT OF THE STUDY: The title marine fungus was investigated to be a resource of new aliphatic acid, and trichothecenes with potent antifungal and dermal toxic actions.


Assuntos
Antifúngicos/isolamento & purificação , Ascomicetos/metabolismo , Perciformes/microbiologia , Animais , Antifúngicos/farmacologia , Ascomicetos/crescimento & desenvolvimento , Aspergillus niger/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Meios de Cultura , DNA Ribossômico , Ácidos Dicarboxílicos/farmacologia , Micotoxinas/farmacologia , Naftalenos/farmacologia , Ressonância Magnética Nuclear Biomolecular/métodos , Fitosteróis/farmacologia , Relação Estrutura-Atividade , Trichophyton/efeitos dos fármacos , Tricotecenos/farmacologia
19.
J Pept Res ; 65(1): 143-8, 2005 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-15686545

RESUMO

In order to extend the use of proteases to organic synthesis and seek the rules of enzymatic reactions in organic media, we focused on unnatural substrates for proteases to form amide bonds. In this paper, the study of unnatural substrates containing D-amino acid residue, which act as acyl acceptors as well as acyl donors for proteases in organic media, is reported. Dermorphin is a heptapeptide (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH(2)) with potent analgesic activity. The N-terminal tetrapeptide is the minimum sequence that retains dermorphin activity, and is selected as the model compound in our study. Two dermorphin-(1-4) derivatives, Boc-Tyr-D-Ala-Phe-Gly-N(2)H(2)Ph and Boc-Tyr-D-Ala-Phe-Gly-NH(2), which contained a d-amino acid residue, were synthesized by proteases in organic media for the first time. The synthesis of these two dermorphin-(1-4) derivatives could be catalyzed by subtilisin with Boc-Tyr-D-Ala-OCH(2)CF(3) as an acyl donor substrate in AcOEt. The synthesis of dermorphin-(1-2) derivative Boc-Tyr-D-Ala-N(2)H(2)Ph was catalyzed by alpha-chymotrypsin in different organic solvents and D-Ala-N(2)H(2)Ph was used as an acyl acceptor substrate. Factors influencing the above enzymatic reactions were systematically studied.


Assuntos
Quimotripsina/metabolismo , Oligopeptídeos/química , Oligopeptídeos/metabolismo , Compostos Orgânicos/metabolismo , Solventes/metabolismo , Subtilisina/metabolismo , Catálise , Cromatografia Líquida de Alta Pressão , Estrutura Molecular , Peptídeos Opioides
20.
Planta Med ; 71(11): 1063-5, 2005 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-16320210

RESUMO

In addition to 7-methoxy-2-methyl-3,4,5-trihydroxyanthraquinone (1), physcion (2), macrosporin (3), deoxybostrycin (4), altersolanol B (5) and dactylariol (6), a new hexahydroanthraquinone named pleospdione (7) was isolated from the culture of Pleospora sp . IFB-E006, an endophytic fungus residing in the normal stem of Imperata cylindrical (Gramineae). Structure determination of pleospdione was accomplished using IR, HR-ESI-MS, 1D and 2D NMR spectral analysis. Compounds 4 - 6 exhibited significant cytotoxic activity against human colon cancer (SW1116) and leukemia (K562) cell lines while compounds 1, 2 and 7 were only weakly or moderately active.


Assuntos
Antraquinonas/química , Antraquinonas/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Ascomicetos/química , Poaceae/microbiologia , Antraquinonas/isolamento & purificação , Antineoplásicos/isolamento & purificação , Humanos , Células K562 , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular
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