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1.
Org Biomol Chem ; 19(35): 7690-7694, 2021 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-34524340

RESUMO

A bifunctional cinchona squaramide catalyzed enantioselective aza-Friedel-Crafts reaction between 2-naphthols and benzothiazolimines has been developed, and a series of chiral 2'-aminobenzothiazolomethyl naphthols with potential antiproliferative and anthelmintic activities have been successfully and effectively prepared in good to excellent yields (up to 98%) with excellent enantioselectivities (up to >99% ee) even in a scale-up preparation under mild conditions.

2.
Metab Eng ; 68: 86-93, 2021 Sep 21.
Artigo em Inglês | MEDLINE | ID: mdl-34555495

RESUMO

Coenzyme Q (CoQ) is vital for energy metabolism in living organisms. In humans, CoQ10 deficiency causes diseases and must be replenished via diet; however, CoQ content in plant foods is primarily low. Here, we report the breeding of high CoQ10 tomato lines by expressing four enzymes with a fruit-specific promoter, which modifies the chloroplast chorismate pathway, enhances cytosolic isoprenoid biosynthesis, and up-regulates the first two reactions in mitochondrion that construct the CoQ10 polyisoprenoid tail. We show that, while the level of the aromatic precursor could be markedly elevated, head group prenylation is the key to increasing the final CoQ10 yield. In the HUCD lines expressing all four transgenes, the highest CoQ10 content (0.15 mg/g dry weight) shows a seven-fold increase from the wild-type level and reaches an extraordinarily rich CoQ10 food grade. Overviewing the changes in other terpenoids by transcriptome and metabolic analyses reveals variable contents of carotenoids and α-tocopherol in the HUCD lines. In addition to the enigmatic relations among different terpenoid pathways, high CoQ10 plants maintaining substantial levels of either vitamin can be selected. Our investigation paves the way for the development of CoQ10-enriched crops as dietary supplements.

3.
Org Lett ; 23(6): 2227-2231, 2021 03 19.
Artigo em Inglês | MEDLINE | ID: mdl-33656901

RESUMO

A new and crucial synthon of 3-((diphenylmethylene)-amino)-oxindole was designed and synthesized, for which an organocatalytic and enantioselective Michael/cyclization reaction with a terminal vinyl ketone catalyzed by a cinchona base was disclosed. A wide variety (28 examples) of almost all new chiral spiro[oxindol-3,2'-pyrrols] were prepared in excellent yields (up to 99%) with excellent enantioselectivities (95-99% ee), of which a typical chiral spiro product was further reduced to chiral spiro[oxindole-3,2'-pyrrolidine].

4.
Org Biomol Chem ; 18(46): 9511-9515, 2020 Dec 07.
Artigo em Inglês | MEDLINE | ID: mdl-33185640

RESUMO

A new base promoted Michael-Michael domino cycloaddition between isoindigos and α-alkylidene succinimides has been developed for highly efficient and one-step convenient preparation of highly steric bispiroxindoles with two adjacent quaternary carbon centers and four consecutive cycles in excellent yields (up to 96%) and diastereoselectivities (up to >20 : 1) under mild conditions within a few minutes. A series of bisprooxindoles were obtained and the synthetic potential of the protocol was evaluated in a scale-up preparation.

5.
Chem Commun (Camb) ; 56(94): 14825-14828, 2020 Nov 26.
Artigo em Inglês | MEDLINE | ID: mdl-33155600

RESUMO

A cinchona alkaloid squaramide promoted enantioselective [4+2] cyclization between hydroxymaleimides and ortho-hydroxyphenyl p-QMs has been disclosed, and a wide range of chiral hemiketals containing chromane and succinimide frameworks with two adjacent quaternary stereogenic centers have been prepared for the first time with excellent results (up to 99% yield, up to 99 : 1 dr, up to >99% ee) under mild conditions.

6.
J Org Chem ; 85(14): 9290-9300, 2020 Jul 17.
Artigo em Inglês | MEDLINE | ID: mdl-32583669

RESUMO

A new enantioselective Michael addition between 3-(3-hydroxy-1H-pyrazol-1-yl)oxindole, a new synthon generated from isatin N,N'-cyclic azomethine imine 1,3-dipole, and ß-nitrostyrene has been disclosed. A series of chiral 3-(3-oxo-2,3-dihydro-1H-pyrazol-1-yl) disubstituted oxindoles were obtained in excellent results (up to 97% yield, up to 94% ee) with moderate to good diastereoselectivities (up to 4.3:1 dr).

7.
J Org Chem ; 85(5): 3921-3928, 2020 03 06.
Artigo em Inglês | MEDLINE | ID: mdl-31944112

RESUMO

An abnormal [3 + 2]-cycloaddition and highly effective and convenient one-step preparation of tetracyclic bispirooxindoles containing two all-carbon quaternary spirocenters from isatin N,N'-cyclic azomethine imine 1,3-dipole and 3-methyleneoxindole in the presence of catalytic organic base has been disclosed. A variety of bispirooxindoles bearing a dinitrogen heterocycle with four adjacent cycles have been obtained in excellent yields (up to 95%) and diastereoselectivities (>99:1) under mild conditions.

8.
Medicine (Baltimore) ; 98(35): e17002, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31464955

RESUMO

BACKGROUND: Chinese herbal medicine (CHM) has been shown to be effective in the treatment of stable chronic obstructive pulmonary disease (COPD) by published meta-analyses. However, disease outcomes were inconsistent and heterogeneity was observed attributed to placebo-controlled studies. We present a protocol for a systematic review aiming to evaluate the clinical efficacy and safety of CHM comparing to placebo in the treatment of stable COPD, to provide robust evidence for the use of CHM in COPD. METHODS: We will comprehensively search the following 9 databases from inception to March 2019: Web of Science, PubMed, EMBASE, Cochrane Central Register of Controlled Trials (CENTRAL), Chinese National Knowledge Infrastructure (CNKI), WANFANG Database, Chinese Scientific and Technological Periodical Database (VIP) and Chinese Biomedical Database (CBM), and the Cochrane Library database. All clinical randomized controlled trials comparing CHM to placebo for the treatment of stable COPD in English or Chinese will be included. The primary outcome will be quality of life, symptom score and exacerbation frequency, and the secondary outcomes include traditional Chinese medicine syndrome score and effective rate, lung function, 6-minute walk distance, and adverse events. Data extraction and quality assessment will be performed independently by 2 reviewers. Data synthesis and risk of bias will be assessed using the Review Manager software. This protocol will be conducted according to the Preferred Reporting Item for Systematic Review and Meta-analysis Protocols (PRISMA-P) guidance. RESULTS: This systematic review and meta-analysis will provide a high-quality comprehensive evaluation of the efficacy and safety based on current literature evidence of CHM intervention for stable COPD. CONCLUSION: The conclusion of this study will present the evidence of whether CHM is an effective and safe intervention for stable COPD patients.


Assuntos
Medicamentos de Ervas Chinesas/uso terapêutico , Medicamentos de Ervas Chinesas/efeitos adversos , Doença Pulmonar Obstrutiva Crônica/tratamento farmacológico , Qualidade de Vida , Ensaios Clínicos Controlados Aleatórios como Assunto , Projetos de Pesquisa , Testes de Função Respiratória , Teste de Caminhada
9.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao ; 41(2): 156-161, 2019 Apr 28.
Artigo em Chinês | MEDLINE | ID: mdl-31060668

RESUMO

Objective To explore the associations of non-alcoholic fatty liver disease(NAFLD)with the prevalence,severity,and prognosis of coronary heart disease(CHD). Methods A total of 512 hospitalized patients undergoing coronary angiography in our department from June 2013 to June 2015 were enrolled.Fatty liver was judged by ultrasound screening,and Gensini score was calculated according to the result of coronary angiography.Then the independent predictors of CHD were analyzed.The association between NAFLD and cardiovascular endpoints was analyzed during prospective follow-up among 276 CHD patients. Results The CHD prevalence was 76.8% in NAFLD group and 50.7% in non-NAFLD group(P=0.000),the number of target vessels was 2(1,3)and 1(1,3)(P=0.019),and the Gensini score was(29.02±27.62)and(24.04±20.18)(P=0.022),respectively.NAFLD was an independent predictor of CHD(OR=2.28,95%CI=1.54-3.56,P<0.001).The risk of cardiovascular endpoints was not significantly different between NAFLD group and non-NAFLD group(P>0.1).Cox regression analysis showed that NAFLD was not a predictor of cardiovascular endpoints in patients with CHD(HR=0.95,95%CI=0.62-1.58,P=0.691).Conclusion NAFLD is an independent predictor of CHD,and it is related to severity of coronary artery stenosis.However,it can not predict the clinical outcomes of patients with CHD.


Assuntos
Doença das Coronárias/complicações , Hepatopatia Gordurosa não Alcoólica/complicações , Angiografia Coronária , Humanos , Prevalência , Prognóstico , Estudos Prospectivos , Fatores de Risco
10.
Front Plant Sci ; 9: 1305, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30233632

RESUMO

Tyrosine serves as a precursor to several types of plant natural products of medicinal or nutritional interests. Hydroxyphenylpyruvate reductase (HPPR), which catalyzes the reduction of 4-hydroxyphenylpyruvic acid (pHPP) to 4-hydroxyphenyllactic acid (pHPL), has been shown to be the key enzyme in the biosynthesis of rosmarinic acid (RA) from tyrosine and, so far, HPPR activity has been reported only from the RA-accumulating plants. Here, we show that HPPR homologs are widely distributed in land plants. In Arabidopsis thaliana, which does not accumulate RA at detectable level, two homologs (HPPR2 and HPPR3) are functional in reducing pHPP. Phylogenetic analysis placed HPPR2 and HPPR3 in two separate groups within the HPPR clade, and HPPR2 and HPPR3 are distinct from HPR1, a peroxisomal hydroxypyruvate reductase (HPR). In vitro characterization of the recombinant proteins revealed that HPPR2 has both HPR and HPPR activities, whereas HPPR3 has a strong preference for pHPP, and both enzymes are localized in the cytosol. Arabidopsis mutants defective in either HPPR2 or HPPR3 contained lower amounts of pHPL and were impaired in conversion of tyrosine to pHPL. Furthermore, a loss-of-function mutation in tyrosine aminotransferase (TAT) also reduced the pHPL accumulation in plants. Our data demonstrate that in Arabidopsis HPPR2 and HPPR3, together with TAT1, constitute to a probably conserved biosynthetic pathway from tyrosine to pHPL, from which some specialized metabolites, such as RA, can be generated in specific groups of plants. Our finding may have broad implications for the origins of tyrosine-derived specialized metabolites in general.

11.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao ; 40(3): 338-343, 2018 Jun 28.
Artigo em Chinês | MEDLINE | ID: mdl-29978789

RESUMO

Objective To explore the relationship between serum uric acid (SUA) level and coronary heart disease(CHD) in male and female patients. Methods A total of 760 hospitalized patients undergoing coronary angiography in our department from June 2013 to June 2017 were enrolled. Gensini score was calculated according to the result of coronary angiography,and SUA was tested.Patients were divided according to SUA quartiles. The relationship between SUA level and the prevalence of CHD in male and female patients was analyzed. Results Among females,there was significant difference in SUA level between patients with and without CHD (t=4.415,P=0.000). Univariate logistic regression analysis showed that SUA level was independently associated with CHD (OR=1.32,95%CI:1.12-1.58,P=0.002). The prevalence of CHD was 31.2%,52.6%,47.4%,and 59.7%,respectively,in four quartile groups (χ2=13.652,P=0.003);in addition,female patients displayed significantly higher prevalence of CHD in the quartile 2 (P=0.007),3(P=0.038),and 4(P=0.000) groups than in quartile 1 group. Among female patients with CHD,there were significant differences in number of target vessels (Z=4.627,P=0.008),number of lesion vessels (χ2=18.522,P=0.005),and Gensini score (Z=3.683,P=0.029) in four groups. The Gensini scores of coronary artery were significantly higher in the quartile 4 group than in quartile 1 (P=0.012) and 2 (P=0.014) groups. Multiple linear regression analysis showed that there was a dose-response relationship between SUA level and Gensini score (B=1.105,SE=0.365,P=0.003). Among males,however,there was no significant difference in SUA level between patients with and without CHD(t=1.271,P=0.205). The prevalence of CHD in four quartile groups was 77.9%,69.0%,61.7%,and 79.6%,respectively,showing no significant difference(χ2=4.514,P=0.211). Conclusion sSUA is an independent risk fact for female CHD patients. High SUA level is correlated with severity of CHD only in women.


Assuntos
Doença das Coronárias/sangue , Ácido Úrico/sangue , Angiografia Coronária , Vasos Coronários/patologia , Feminino , Humanos , Masculino , Prevalência , Fatores de Risco
12.
Zhen Ci Yan Jiu ; 43(4): 269-73, 2018 Apr 25.
Artigo em Chinês | MEDLINE | ID: mdl-29888584

RESUMO

OBJECTIVE: To analyze studies published in journals included in PubMed in terms of randomized controlled trials (RCTs) examining the therapeutic effect of acupuncture for simple obesity, so as to provide a reference for subsequent RCT-related designs and results. METHODS: RCT literature about acupuncture treatment of simple obesity from the PubMed database and from 2000 to 2016 was retrieved by using keywords of "obesity" "fat" "acupuncture" "joint application of acupuncture and herbal medicine" or "auricular point" "electroacupuncture", "acupoint application", or "cupping", followed by screening, extraction and evaluation of the design methodology and outcomes using Consolidated Standards for Reporting of Trials (CONSORT) and Standards for Reporting Interventions in Controlled Trials of Acupuncture (STRICTA). RESULTS: Fourteen articles from six countries in Asia examining the therapeutic effect of acupuncture in the treatment of simple obesity mainly by using acupoints of the Stomach Meridian were included. Generally, acupuncture was found to be more effective than sham acupuncture. However, PubMed did not include any RCTs comparing acupuncture with western medicine for weight loss and many problems (as details of needling manipulation, etc.) remained in the the research reports available in the database. CONCLUSION: All the existing RCTs generally affirm the positive efficacy of acupuncture for simple obesity, but high-quality RCTs, particularly those comparing acupuncture with western medicines for weight loss are lacking.


Assuntos
Terapia por Acupuntura , Humanos , Obesidade/terapia , PubMed , Ensaios Clínicos Controlados Aleatórios como Assunto
13.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao ; 40(6): 765-768, 2018 Dec 20.
Artigo em Chinês | MEDLINE | ID: mdl-30606386

RESUMO

Objective To investigate the correlation between CYP2C19 gene polymorphism and elderly cerebral infarction.Methods Two polymorphisms including rs4244285 and rs4986893 of the CYP2C19 gene were detected by gene chip technology in 72 elderly patients with acute cerebral infarction (stroke group) and 77 otherwise healthy controls. The clinical data and the polymorphism distribution of CYP2C19 were compared,and the potential association between genetic polymorphism and cerebral infarction was analyzed by Logistic regression.Results The frequencies of rs4244285 GG (45.83% vs. 63.64%,Χ 2=4.766,P=0.029) and rs4244285 A allele (34.03% vs. 22.73%,Χ 2=4.695,P=0.030) were significantly higher in stroke group than in control group. There were no significant differences in the distribution of the alleles of rs4986893 or the rs4244285 GA and AA between these two groups (all P>0.05). After the conventional cerebrovascular risk factors including gender,age,body mass index,smoking,and total cholesterol were adjusted,Logistic regression analysis showed that rs4244285 A allele significantly increased the stroke risk [the additive model AA vs. GG:OR=2.564,95%CI=1.181-5.566,P=0.017;the dominant model AA/AG vs. GG:OR=2.763,95%CI=1.343-5.685,P=0.006].Conclusion CYP2C19 genetic polymorphism may be associated with the increased risk of cerebral infarction in the elderly,although future well-designed studies with larger sample sizes are warranted.


Assuntos
Infarto Cerebral/genética , Citocromo P-450 CYP2C19/genética , Idoso , Alelos , Isquemia Encefálica/genética , Estudos de Casos e Controles , Frequência do Gene , Predisposição Genética para Doença , Genótipo , Humanos , Polimorfismo de Nucleotídeo Único , Acidente Vascular Cerebral/genética
14.
Front Plant Sci ; 8: 627, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28487717

RESUMO

Salvia miltiorrhiza, a medicinal plant in China, has been used for thousands of years to treat coronary heart diseases. Although biosynthesis of tanshinones, a group of diterpenoids in S. miltiorrhiza, has been extensively investigated, to date we know little about the formation of monoterpenes and sesquiterpenes in this medicinal plant. Here, we report the characterization of three sesquiterpene synthases, named SmSTPS1, SmSTPS2, and SmSTPS3, which catalyzed the formation of a new compound, (-)-5-epieremophilene. Additionally, the (-)-5-epieremophilene biosynthesis activity of SmSTPS1 was confirmed by transient expression in Nicotiana benthamiana. Despite the similar enzyme activities of SmSTPS1, SmSTPS2, and SmSTPS3, the three (-)-5-epieremophilene synthase genes displayed different spatial expression patterns and responded differently to hormone treatments, implicating their specific roles in plant-environment interactions. Our results provide valuable data to understanding the biosynthesis and composition of terpenes in plant.

15.
J Zhejiang Univ Sci B ; 9(11): 857-62, 2008 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-18988304

RESUMO

OBJECTIVE: To assess the diagnostic efficiency of OMOM capsule endoscopy (CE) in a group of patients with different indications. METHODS: Data from 89 consecutive patients (49 males, 40 females) with suspected small bowel disease who underwent OMOM CE (Jinshan Science and Technology Company, Chongqing, China) examination were obtained by retrospective review. The patients' indications of the disease consisted of the following: obscure gastrointestinal bleeding (OGIB), abdominal pain or diarrhea, partial intestinal obstruction, suspected inflammatory bowel disease, tumor of unknown origin, hypoproteinemia, constipation, weight loss, and elevated tumor markers. RESULTS: CE failed in one patient. Visualization of the entire small bowel was achieved in 75.0%. Capsules were naturally excreted by all patients. The detection rate of abnormalities was 70.5% for patients with suspected small bowel disease, and the diagnostic yield for patients with OGIB was higher than that for patients with abdominal pain or diarrhea (85.7% vs 53.3%, P<0.005). Angiodysplasia was the most common small bowel finding. Active bleeding sites were noted in the small intestine in 11 cases. CONCLUSION: OMOM CE is a useful diagnostic tool for the diagnosis of variably suspected small bowel disease, whose diagnostic efficiency is similar to that of the Pillcam SB (small bowel) CE (Given Imaging, Yoqneam, Israel).


Assuntos
Endoscopia por Cápsula/métodos , Enteropatias/diagnóstico , Intestino Delgado/patologia , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Endoscopia por Cápsula/normas , Feminino , Humanos , Enteropatias/patologia , Masculino , Pessoa de Meia-Idade , Satisfação do Paciente , Estudos Retrospectivos , Adulto Jovem
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