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1.
Int J Biol Macromol ; 2020 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-32068062

RESUMO

The aim of this study was to evaluate the spatial structure and potential antifatigue activity of polysaccharide fractions which was extracted from Inonotus obliquus. The first polysaccharide fractions of Inonotus obliquus (PIO-1) were obtained after hot-water extraction and purification by DEAE cellulose-52 chromatography. Results of the forced swimming test showed that the doses (50 mg/kg) of PIO-1 could increase the climbing duration and swimming time as well as reduced the immobility time in the PIO treated mice. The fatigue related metabolic parameters showed that PIO-1 decreased the level of blood lactic acid (BLA), urea nitrogen (BUN) and lactic dehydrogenase (LDH). Additionally, PIO-1 significantly decreased the 5-HT concentrations in the mice brain. The results of monosaccharide analysis showed that the molar ratio of mannose, glucose, galactose, xylose and arabinose with the molar ratio of 1.0:1.9:3.5:18.5:5.7. The molecular morphology of the PIO-1 observed under atomic force microscopy (AFM). There were many spherical and heterogeneous clumps existed in the images. Therefore, current study indicated polysaccharide PIO-1 not only has great potential to postpone physical fatigue but also shown potential to improve mental fatigue.

2.
Acta Pharmacol Sin ; 2019 Nov 25.
Artigo em Inglês | MEDLINE | ID: mdl-31768045

RESUMO

Cadmium (Cd) is a nonessential heavy metal and a prevalent environmental toxin that has been shown to induce significant cardiomyocyte apoptosis in neonatal murine engineered cardiac tissues (ECTs). In contrast, zinc (Zn) is a potent metallothionein (MT) inducer, which plays an important role in protection against Cd toxicity. In this study, we investigated the protective effects of Zn against Cd toxicity in ECTs and explore the underlying mechanisms. ECTs were constructed from neonatal ventricular cells of wild-type (WT) mice and mice with global MT gene deletion (MT-KO). In WT-ECTs, Cd (5-20 µM) caused a dose-dependent toxicity that was detected within 8 h evidenced by suppressed beating, apoptosis, and LDH release; Zn (50-200 µM) dose-dependently induced MT expression in ECTs without causing ECT toxicity; co-treatment of ECT with Zn (50 µM) prevented Cd-induced toxicity. In MT-KO ECTs, Cd toxicity was enhanced; but unexpectedly, cotreatment with Zn provided partial protection against Cd toxicity. Furthermore, Cd, but not Zn, significantly activated Nrf2 and its downstream targets, including HO-1; inhibition of HO-1 by a specific HO-1 inhibitor, ZnPP (10 µM), significantly increased Cd-induced toxicity, but did not inhibit Zn protection against Cd injury, suggesting that Nrf2-mediated HO-1 activation was not required for Zn protective effect. Finally, the ability of Zn to reduce Cd uptake provided an additional MT-independent mechanism for reducing Cd toxicity. Thus, Zn exerts protective effects against Cd toxicity for murine ECTs that are partially MT-mediated. Further studies are required to translate these findings towards clinical trials.

3.
Clin Lab ; 65(11)2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-31710433

RESUMO

BACKGROUND: A noninvasive, fast, highly sensitive and simple test is needed for cancer screening in addition to the detection of biomarkers in blood. Recently, the patent (CN102565055A) for the Urinary Monohydroxyphenyl Metabolites Assay (UMM-A) was authorized, and the effectiveness of clinical application has yet to be studied further. METHODS: A retrospective study was conducted consisting of 432 cancer patients, 28 benign tumor patients, 117 non-cancerous diseases patients, and 120 healthy donors to analyze the levels of monohydroxyphenyl metabolites in the urine sample. A logistic regression model was used to study the possible confounding factors affecting the diagnostic performance and to test the probability of a case to be positive for UMM-A. RESULTS: Compared with healthy donors, non-cancerous disease, and benign tumor subjects, the positive rate and MM level of UMM-A in cancer patients have significantly increased. After the 246 retreated cancer patients were excluded, and 186 untreated cancer patients were included, with the same specificity to 77.0%, the sensitivity improved from 66.7 to 89.8%, the negative predictive value improved from 58.6 to 91.4%. CONCLUSIONS: The present study has provided important information on the diagnostic characteristics of UMM-A for untreated cancer and its potential application in cancer screening.

4.
J Zhejiang Univ Sci B ; 20(11): 928-932, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31595729

RESUMO

Hepatocellular carcinoma (HCC) is one of the most common types of liver cancer and is the second leading cause of cancer mortality with an estimated 745 500 deaths annually (Jemal et al., 2011). Although new therapeutic modalities including novel chemotherapeutic interventions and targeted therapy have been applied, the prognosis of HCC patients remains unsatisfactory due to the high incidence of intrahepatic and distal metastases (Siegel et al., 2018).

5.
Beilstein J Org Chem ; 15: 291-298, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30800179

RESUMO

Herein we report a novel palladium-catalyzed reaction that results in phenanthrene derivatives using aryl iodides, ortho-bromobenzoyl chlorides and norbornadiene in one pot. This dramatic transformation undergoes ortho-C-H activation, decarbonylation and subsequent a retro-Diels-Alder process. Pleasantly, this protocol has a wider substrate range, shorter reaction times and higher yields of products than previously reported methods.

6.
J Org Chem ; 84(5): 2721-2731, 2019 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-30695635

RESUMO

In this study, we performed a theoretical investigation of the intramolecular cyclization of bicyclic 2-allyl-2-methyl-2,3-dihydro-1 H-inden-1-iminyl radical 1 along with several iminyl model compounds. The results were used to comparatively evaluate the reaction mechanism suggested previously, in which the neophyl-like rearrangement was deemed to play a decisive role. The present computation and numerical simulation identify the experimentally observed endo product in the high-temperature cyclization of 1. The product results from a kinetically controlled endo cyclization-reduction pathway involving an initial reversible 5- exo ring-closure/ring-opening process, not via 5- exo cyclization/neophyl-like rearrangement/ endo-radical reduction pathway as proposed previously. Considering many available theoretical and experimental results, the neophyl-like rearrangement seems to play only a minor role in the intramolecular cyclization of N- and C-centered radicals. The structural effect of cyclized radical intermediates of bicyclic 1 leads to a lower thermodynamic reaction energy of exo cyclization than of endo cyclization, which together with the temperature effect should be responsible for the formation of the dominant endo product in the high-temperature region. Additionally, this investigation provided further insight into the cyclization of 1 and compounds structurally similar to 1; that is, control of endo- or exo-regioselective products is readily available by regulating the reaction temperature.

7.
Asia Pac J Clin Nutr ; 27(5): 1067-1076, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30272855

RESUMO

BACKGROUND AND OBJECTIVES: Obesity is linked to metabolic diseases characterized by insulin resistance, such as diabetes and cardiovascular disease. In this study, we investigated the metabolic disorders of uncomplicated obesity to identify early alterations in biological systems. METHODS AND STUDY DESIGN: Metabolic differences between overweight/obese (n=36) and normal-weight (n=35) young Chinese men without known metabolic disorders were assessed. Metabolic profiling of the serum and urine was performed using ultra-performance liquidchromatography quadrupole-time-of-flight mass spectrometry (UPLC-Q-TOF-MS). Partial least squares discriminant analysis (PLS-DA) was undertaken to reveal and classify the differences between the two groups. RESULTS: Compared to normal-weight men, obese men had higher levels of the serum metabolites phenylalanine, Phe-Phe, and L-tryptophan, whereas those of p-cresol sulfate and p-cresol were less in obesity. Urinary metabolites phenylacetamide, L-glutamine, phenylacetylglutamine, indoxyl sulfate, p-cresol, and p-cresol sulfate were greater in obese men. CONCLUSIONS: These findings indicate that disorders involving aromatic amino acids and the tricarboxylic acid cycle (TCA) have microbiomic involvement in the uncomplicated phase of obesity.


Assuntos
Metabolômica/métodos , Sobrepeso/sangue , Sobrepeso/urina , Adulto , Biomarcadores/sangue , Biomarcadores/urina , Cromatografia Líquida de Alta Pressão , Cresóis/sangue , Cresóis/urina , Análise Discriminante , Glutamina/análogos & derivados , Glutamina/urina , Humanos , Indicã/urina , Masculino , Espectrometria de Massas , Obesidade/sangue , Obesidade/urina , Fenilalanina/sangue , Triptofano/sangue , Adulto Jovem
8.
Chemistry ; 24(72): 19122-19135, 2018 Dec 20.
Artigo em Inglês | MEDLINE | ID: mdl-29984536

RESUMO

Alkenyl magnesium compounds have received much attention in synthetic organic chemistry because of their high reactivity. This review summarizes three types of alkenyl magnesium compounds which contain at least one [Mg-C=C] fragment, for example, (1) alkenyl Grignard reagents prepared by halogen-magnesium exchange reaction; (2) alkenyl magnesium carbenoids prepared by halogen-magnesium exchange reaction or sulfoxide-magnesium exchange reaction; (3) magnesacarbocycles containing at least one alkenyl magnesium bond prepared from Zr- or Ti-catalyzed cyclomagnesation or transmetalation, as well as their further reactions and applications.

9.
Aging (Albany NY) ; 10(6): 1424-1441, 2018 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-29969436

RESUMO

We tested the hypothesis that bevacizumab-induced hypertension may be a useful predictor for objective response rate, progression-free and overall survival in patients with metastatic colorectal cancer via a comprehensive meta-analysis. Search process, article selection and data extraction were independently performed by two investigators. Statistical analyses were conducted using the STATA/SE software. Fourteen independent studies and 2292 study subjects were synthesized. Overall relative risk of objective response rate for bevacizumab-induced hypertension was 2.03 (95% confidence interval [CI]: 1.18-3.48, p=0.01), with significant heterogeneity and publication bias, whereas unbiased estimate was nonsignificant after considering potentially missing studies. Overall hazard ratio for progression-free survival was 0.58 (95% CI: 0.43-0.77, p<0.001), with significant heterogeneity and publication bias, and unbiased estimate was significant (hazard ratio: 0.52, 95% CI: 0.41-0.66, p<0.001). Overall hazard ratio for overall survival was 0.51 (95% CI: 0.39-0.65, p<0.001), and this estimate was not likely confounded by heterogeneity or publication bias. Subgroup and meta-regression analyses suggested that hypertension grade of controls, sample size, age and gender were possible causes of heterogeneity. Taken together, our findings indicate that bevacizumab-induced hypertension can predict progress-free survival and overall survival in patients with metastatic colorectal cancer, whereas its prediction for objective response rate was nonsignificant.


Assuntos
Antineoplásicos Imunológicos/efeitos adversos , Bevacizumab/efeitos adversos , Neoplasias Colorretais/tratamento farmacológico , Hipertensão/induzido quimicamente , Neoplasias Colorretais/complicações , Humanos , Fatores de Risco
10.
Phys Chem Chem Phys ; 20(22): 15139-15148, 2018 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-29789848

RESUMO

In this study, the structures and field-emission properties of Li-decorated buckled α-borophene (BBP) were investigated by first-principles density functional theory at the PW91 level. Using the computed binding energies, Hirshfeld- and electrostatic potential-derived charges, induced dipole moments, densities of states, and ionization potentials, we evaluated the influence of an applied electric field on the structural stability, work function, and field-emission current of the Li-decorated BBP nanostructures. Furthermore, we also explored the quantitative dependence of the emission current on the electric field, Li concentration, and molecular orbitals. The computed results indicated that increasing the electric field and Li concentration has a considerably positive effect on the field-emission performance of the Li-decorated BBPs. Besides advantages including small work functions and low ionization potentials, most remarkably, the field-emission current can be as high as 48.81 µA in Li4/BBP (supercell with 36 atoms only) under a rather small applied electric field of 0.05 V Å-1, which rivals the highest value of the graphene-BN nanocomposite among all the theoretical nanostructures presented to date. Our results highly support the fact that Li-decorated BBPs can be appealing field-emission cathode materials with an extremely high emission current.

11.
Chemistry ; 24(13): 3186-3191, 2018 Mar 02.
Artigo em Inglês | MEDLINE | ID: mdl-29205548

RESUMO

A series of butadienyl organomagnesium complexes, including 1-Li-4-(MgR)-butadienes, 1,4-bis(MgR)-butadienes, and 1-Mg-4-(MgR)-butadiene were synthesized starting with 1,4-dilithio butadienes via the transmetalation reaction between alkenyllithium bond and alkenylmagnesium bond. Single-crystal X-ray structural analysis of these butadienyl organomagnesiates revealed unique bonding modes. Study on their structural transformation demonstrated that 1-Li-4-(MgR)-butadiene is the key intermediate in the reaction process leading to the formation of 1,4-bis(MgR)-butadiene and 1-Mg-4-(MgR)-butadiene.

12.
Eur J Nutr ; 57(5): 1957-1967, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28573457

RESUMO

PURPOSE: Mitochondrial dysfunction plays an important role in the development of obesity and obesity-associated metabolic diseases. METHODS: In this study, we dynamically observed the characteristics of mitochondrial damage in a rat model of diet-induced obesity (DIO). From the 2nd to the 10th week, animals were killed every 2 weeks and the heart, liver, kidney, and testicular tissues were harvested. Mitochondria were isolated and the activities of respiratory chain complexes I, II, III, and IV as well as the 8-Hydroxy-2-deoxy Guanosine content were determined. Reactive oxygen species and malondialdehyde were measured. RESULTS: Mitochondrial damages were observed in the heart and liver of DIO and DR rats, and the damages occurred later in DR group than that in DIO group. The mitochondrial membrane potential of heart and liver decreased in DIO and DR groups. The activity of the heart mitochondria complexes I, III, and IV (composing NADH oxidative respiratory) was higher in the early stage of DIO and lower in the end of week 10. The higher activity of the liver complexes I, III, and IV was found until the end of week 10 in DIO and DR groups, accompanied with enhanced oxidative stress. Besides, mitochondrial DNA damages were observed in all tissues. CONCLUSION: In DIO rats, the heart mitochondrial dysfunction occurred first and the liver presented the strongest compensatory ability against oxidative stress.


Assuntos
Dieta Hiperlipídica/efeitos adversos , Transporte de Elétrons/fisiologia , Obesidade/complicações , Estresse Oxidativo/fisiologia , Animais , Masculino , Malondialdeído/metabolismo , Mitocôndrias/metabolismo , Ratos , Ratos Wistar , Espécies Reativas de Oxigênio
13.
J Am Chem Soc ; 139(39): 13688-13691, 2017 10 04.
Artigo em Inglês | MEDLINE | ID: mdl-28933865

RESUMO

Reductive elimination of Cu(III) intermediates is often proposed as a key step in many copper-catalyzed or -mediated formation of C-C or C-heteroatom bonds. However, there still lacks concrete evidence on this key step, mainly because Cu(III) complexes are usually too unstable to be isolated and structurally characterized. In this work, novel organocopper(III) spiro complexes and their analogous organocopper(I) spiro complexes were synthesized and structurally characterized. Single-crystal X-ray structural analysis revealed that the spiro Cu(III) atom adopted a distorted square-planar geometry while its corresponding spiro Cu(I) atom was tetrahedrally coordinated. A redox transformation between these spiro Cu(I) and Cu(III) complexes was experimentally observed by reacting with reductants or oxidants, respectively. As concrete evidence, the organocopper(III) spiro compounds were found to form C-C bonds intramolecularly via reductive elimination.

14.
Oncotarget ; 8(63): 106661-106671, 2017 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-29290979

RESUMO

Both diabetes and angiotensin II (Ang II) excess trigger cardiac remodeling and dysfunction, and diabetic cardiomyopathy. We hypothesized that cardiac hypertrophy associated with the development of diabetic cardiomyopathy is worsened by increased Ang II. Male type 1 diabetic OVE26 and wild-type mice were given Ang II (sc., 1.15 mg/kg, twice a day) for 14 days. Diabetes-induced cardiac dysfunction and hypertrophy was exacerbated by Ang II treatment as determined by echocardiography, wheat germ agglutinin staining and atrial natriuretic peptide. Ang II treatment dramatically exacerbated diabetes-caused decreased LC3-II, a marker of autophagy, and increased p62, an indicator of cytosolic protein clearance. Ang II treatment also augmented diabetes-associated increased phosphorylated levels of c-Jun, JNK, mTOR, and miR-221, and decreased of p27 expression, a direct target of miR-221. Chromatin immunoprecipitation assay showed that Ang II elevated c-Jun binding to the promoter of miR-221 in diabetic mice. These results suggest that Ang II accelerates cardiac hypertrophy in the early stage of murine diabetes, probably through activation of the JKN/c-Jun/miR-221 axis and inhibition of downstream autophagy. Therefore, inhibition of Ang II or miR-221 in diabetic individuals may be a potential approach for delaying the onset and/or reducing the severity of diabetic cardiomyopathy.

15.
Org Lett ; 19(1): 298-300, 2017 01 06.
Artigo em Inglês | MEDLINE | ID: mdl-28029264

RESUMO

One novel hybrid peptide-polyketide, dahurelmusin A (1), was isolated from Elymus dahuricus infected by the Epichloë bromicola endophyte. Comprehensive spectroscopic analysis revealed that 1 is the first example of hybrid peptide-polyketide possessing an unprecedented 5-hydroxy-2,2,4,6-tetramethyl-3-oxooctanoic acid moiety. The single-crystal X-ray diffraction analyses allowed the absolute configuration assignment of this compound. Compound 1 also exhibited significant insecticidal activities against Rhopalosiphum padi and Brevicoryne brassicae with LC50 values of 0.092 and 0.251 mM, respectively.


Assuntos
Elymus/química , Endófitos/química , Epichloe/química , Peptídeos/química , Policetídeos/química , Animais , Afídeos , Caprilatos/química , Inseticidas/química , Inseticidas/isolamento & purificação , Estrutura Molecular , Peptídeos/isolamento & purificação , Policetídeos/isolamento & purificação
16.
J Phys Chem B ; 120(50): 12950-12958, 2016 12 22.
Artigo em Inglês | MEDLINE | ID: mdl-27957838

RESUMO

In this study, we employed the density functional method to simulate AIBN/HSnBu3-mediated radical cyclizations with different axially chiral conformers of N-(2-iodo-4,6-dimethylphenyl)-N,2-dimethyl-(2E)-butenamide as substrates. We constructed a reaction potential energy profile using the Gibbs free energies of the located stationary points. The thermodynamic and kinetic data of the profile were further used to evaluate the regioselectivity, stereoselectivity, and product distribution of the cyclizations. Additionally, we compared the present HSnBu3-mediated radical cyclization with the experimentally available Heck reaction and found that such a radical cyclization can convert (M,Z) and (P,Z) o-iodoanilide substrates to centrally chiral products with high chirality transfer. The goal of this study was to estimate the practicality of theoretically predicting the memory of chirality in such radical cyclizations. The present results can provide a strategy from a theoretical viewpoint for experimentally synthesizing highly stereoselective carbocyclic and heterocyclic compounds using radical cyclization methods.

17.
PeerJ ; 4: e2757, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27994971

RESUMO

Major research efforts have been devoted to the discovery and development of new chemical entities that could inhibit the protein-protein interaction between HIF-1α and the von Hippel-Lindau protein (pVHL), which serves as the substrate recognition subunit of an E3 ligase and is regarded as a crucial drug target in cancer, chronic anemia, and ischemia. Currently there is only one class of compounds available to interdict the HIF-1α/pVHL interaction, urging the need to discover chemical inhibitors with more diversified structures. We report here a strategy combining shape-based virtual screening and cascade docking to identify new chemical scaffolds for the designing of novel inhibitors. Based on this strategy, nine active hits have been identified and the most active hit, 9 (ZINC13466751), showed comparable activity to pVHL with an IC50 of 2.0 ± 0.14 µM, showing the great potential of utilizing these compounds for further optimization and serving as drug candidates for the inhibition of HIF-1α/von Hippel-Lindau interaction.

18.
Fitoterapia ; 113: 158-63, 2016 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27520493

RESUMO

Four novel lactams, colletotrilactam A-D (1-4), along with six known compounds (5-10) were isolated from the culture broth of Colletotrichum gloeosporioides GT-7, a fungal endophyte of Uncaria rhynchophylla. The structures of these compounds were elucidated by comprehensive NMR spectroscopy. Isolates were tested for monoamine oxidase (MAO) inhibitory activity and compound 9 showed potent MAO inhibitory activity with IC50 value of 8.93±0.34µg/mL, when the IC50 value of iproniazid as a standard was 1.80±0.5µg/mL.


Assuntos
Colletotrichum/química , Lactamas/química , Inibidores da Monoaminoxidase/química , Uncaria/microbiologia , Endófitos/química , Lactamas/isolamento & purificação , Estrutura Molecular , Monoaminoxidase/metabolismo , Inibidores da Monoaminoxidase/isolamento & purificação
19.
Adv Exp Med Biol ; 923: 283-289, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27526155

RESUMO

The aim of this study was to analyze the effects of exercise training on Bax and Bcl-2 protein content and sirtuin1 (SIRT1) mRNA expression levels to prevent sarcopenia in aging rats. Eight 18 months old male Sprague-Dawley rats were trained 5 days weekly for 8 weeks on a treadmill, and eight sedentary rats served as controls. Gastrocnemius muscles were dissected 2 days after the last training session. The mRNA content of PGC-1α, caspase-3, NRF1, TFAM, SOD2, and SIRT1 was estimated by RT-PCR with GAPDH used as an internal control. The protein expression of BAX and Bcl-2 was assessed by Western immunoblot. After training, significant (p < 0.05) increases were noted for the gastrocnemius muscle weights, the gastrocnemius mass/body mass ratio, the bcl-2/BAX ratio, the Bcl-2 protein and the SIRT1, PGC-1α, NRF1, TFAM, SOD2 mRNA content in the trained gastrocnemius, relative to the control samples. No difference was found in the BAX protein between control and trained muscles, whereas the caspase-3 mRNA content decreased by 50 %, in the gastrocnemius muscle of trained animals. Exercise training may inhibit age-induced myonuclear apoptosis by stimulating SIRT1/PGC-1α mRNA expression, thereby preventing sarcopenia in aging rat.


Assuntos
Envelhecimento/metabolismo , Músculo Esquelético/enzimologia , Coativador 1-alfa do Receptor gama Ativado por Proliferador de Peroxissomo/metabolismo , Esforço Físico , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Corrida , Sarcopenia/prevenção & controle , Sirtuína 1/metabolismo , Proteína X Associada a bcl-2/metabolismo , Fatores Etários , Envelhecimento/genética , Envelhecimento/patologia , Animais , Apoptose , Caspase 3/metabolismo , Masculino , Músculo Esquelético/patologia , Coativador 1-alfa do Receptor gama Ativado por Proliferador de Peroxissomo/genética , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Ratos Sprague-Dawley , Sarcopenia/enzimologia , Sarcopenia/genética , Sarcopenia/patologia , Transdução de Sinais , Sirtuína 1/genética , Fatores de Tempo
20.
Eur J Med Chem ; 121: 422-432, 2016 Oct 04.
Artigo em Inglês | MEDLINE | ID: mdl-27318119

RESUMO

In an effort to discover new molecules with good insecticidal activities, more than 40 new avermectin derivatives were synthesized and evaluated for their biological activities against three species of arachnids, insects and nematodes, namely, Tetranychus Cinnabarinus, Aphis craccivora and Bursaphelenchus xylophilus. All the tested compounds showed potent inhibitory activities against three insect species. Notably, the majority of compounds exhibited high selectivity against T. cinnabarinus, some of which were much better in comparison with avermectin. Especially compounds 9j (LC50: 0.005 µM) and 16d (LC50: 0.002 µM) were 2.5- and 4.7-fold more active than avermectin (LC50: 0.013 µM), respectively, against T. cinnabarinus. Moreover, compounds 9b, 9d-f, 9h, 9j, 9l, 9n, 9p, 9r, 9v and 17d showed superior activities with LC50 values of 2.959-5.013 µM compared to that of 1 (LC50: 6.746 µM) against B. xylophilus. Meanwhile, the insecticidal activities of compounds 9f, 9g, 9h, and 9m against A. craccivora were 7-8 times better than that of avermectin, with LC50 values of 7.744, 5.634, 6.809, 7.939 and 52.234 µM, respectively. Furthermore, QSAR analysis showed that the molecular shape, size, connectivity degree and electronic distribution of avermectin analogues had substantial effects on insecticidal potency. These preliminary results provided useful insight in guiding further modifications of avermectin in the development of potential new insecticides.


Assuntos
Antinematódeos/síntese química , Antinematódeos/farmacologia , Ivermectina/análogos & derivados , Relação Quantitativa Estrutura-Atividade , Animais , Antinematódeos/química , Técnicas de Química Sintética , Ivermectina/síntese química , Ivermectina/química , Ivermectina/farmacologia , Camundongos , Nematoides/efeitos dos fármacos , Relação Estrutura-Atividade
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