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1.
Org Lett ; 25(22): 4150-4155, 2023 Jun 09.
Artigo em Inglês | MEDLINE | ID: mdl-37252906

RESUMO

A convenient and efficient approach was developed to synthesize α-Kdo O-glycosides based on the Tf2O/(p-Tol)2SO preactivation strategy using peracetylated Kdo thioglycoside as a donor. Under the optimized reaction conditions, several O-glycoside products, including α-(2 → 1)-, α-(2 → 2)-, α-(2 → 3)-, and α-(2 → 6)-Kdo products, were stereoselectively synthesized in high yields. Remarkably, a series of aromatic α-Kdo O-glycosides were first and successfully constructed in high yields. An SN2-like mechanism was revealed by DFT calculations and experimental results.


Assuntos
Glicosídeos Cardíacos , Glicosídeos , Glicosilação , Açúcares Ácidos , Lipopolissacarídeos
2.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-908677

RESUMO

Objective:To study the effect of cyclin Y (CCNY) on the lesion degree of patients with liver cancer and its correlation with preoperative and postoperative liver injury.Methods:The clinical data of 60 patients with liver cancer (liver cancer group) and 69 patients with liver cirrhosis (liver cirrhosis group) in Hangzhou Hospital of Zhejiang Medical and Health Group from January 2015 to October 2017 were retrospectively analyzed. In liver cirrhosis group, Child-Pugh liver function grade A was in 33 cases (liver cirrhosis grade A group), grade B was in 21 cases (liver cirrhosis grade B group), grade C was in 15 cases (liver cirrhosis grade C group). The serum total bilirubin (TBIL), alanine aminotransferase (ALT), albumin, cholinesterase, γ-glutamyl transpeptidase (GGT) and total bile acid were detected by automatic biochemical analyzer. The serum CCNY was detected by WB method, and compared with 40 healthy subjects (healthy control group).Results:Compared with those in healthy control group, the albumin and cholinesterase in liver cirrhosis grade A, B and C groups were significantly decreased, the ALT, TBIL, GGT, total bile acid and CCNY were significantly increased, , and the changes were more obvious with the severity of liver disease, and there were statistical differences ( P<0.05). Pearson correlation analysis result showed that the CCNY was positive correlation with TBIL, ALT, total bile acid and GGT in patients with liver cancer ( r = 0.544, 0.612, 0.553 and 0.539; P<0.05), and CCNY was negative correlation with albumin and cholinesterase ( r = - 0.478 and - 0.620, P<0.05). In patients with liver cancer, before operation and 1, 2 and 7 d after operation, the CCNY was 3.01 ± 1.10, 7.24 ± 2.57, 6.29 ± 1.78 and 4.01 ± 1.52, ALT was (98.74 ± 16.79), (430.55 ± 197.62), (255.73 ± 26.77) and (121.89 ± 20.42) U/L, respectively; the CCNY and ALT 1 and 2 d after operation were significantly higher than those before operation, those 2 d after operation were significantly lower than those 1 d after operation, those 7 d after operation were significantly lower than those 2 d after operation, and there were statistical differences ( P<0.05); there were no statistical difference between 7 d after operation and before operation ( P>0.05). The expression of CCNY before operation and 1 d, 2 d, 7 d after operation was positive correlation with ALT in patients with liver cancer ( r = 0.669, 0.821, 0.663 and 0.642; P<0.01). Conclusions:The more severe the degree of liver lesions in patients with liver cancer, the higher the serum CCNY, and the higher the expression of CCNY, the more severe the degree of liver injury in patients with liver cancer due to surgery, which is positively correlated with liver injury indexes.

3.
Nat Prod Res ; 34(18): 2595-2601, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30623674

RESUMO

One new sesquiterpene (α-iso-cubebenol acetate, 8), together with 9 known compounds (1-7, 9, 10) were isolated from the stems of Schisandra chinensis (Turcz.) Baill. by repeated silica gel column chromatography. Based on the results of MS, NMR spectra and comparing with literature data, the six dibenzocyclooctadiene lignans were identified as schizandrin A to C (1-3), schizandrin (4), schisantherin A (5) and gomisin J (6), the two sesquiterpenes were identified as α-iso-cubebenol (7) and α-iso-cubebenol acetate (8), while the two triterpenic acids were identified as ganwuweizic acid (9) and kadsuric acid (10). The antifeedant activity of the 10 compounds against Tribolium castaneum adults was tested. Gomisin J (6) exhibited activity at 1500 ppm concentration with 40.3% antifeeding index percentages. As for the dibenzocyclooctene lignans (compounds 1-3, 6), the number of methylenedioxies and the position of hydroxyl groups were the main factors to affect their antifeedant activities.


Assuntos
Ciclo-Octanos/química , Comportamento Alimentar/efeitos dos fármacos , Lignanas/química , Caules de Planta/química , Schisandra/química , Tribolium , Animais , Ciclo-Octanos/análise , Ciclo-Octanos/isolamento & purificação , Dioxóis/isolamento & purificação , Lignanas/análise , Lignanas/isolamento & purificação , Compostos Policíclicos/isolamento & purificação , Sesquiterpenos/análise , Sesquiterpenos/isolamento & purificação , Relação Estrutura-Atividade , Tribolium/efeitos dos fármacos , Triterpenos/análise , Triterpenos/isolamento & purificação
4.
Ecotoxicol Environ Saf ; 190: 110106, 2020 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-31877546

RESUMO

In this work, the essential oil (EO) and supercritical CO2 fluid extract (SF extract) of four Valerianaceae plants (Valeriana officinalis L., Valeriana officinalis L. var. latifolia Miq., Valeriana jatamansi Jones and Nardostachys chinensis Bat.) were chemically characterized. GC-MS analysis identified 74 compounds, representing 35.2%-82.4% of the total EOs and SF extracts. The EO was dominated by low-molecular-weight components while the SF extract was rich in fatty acids. Bornyl acetate and camphene were the characteristic compounds in EO and SF extracts. The efficacy of six extracts against three stored-product insects was investigated. In contact assays, V. officinalis exhibited strongest toxicity to red flour beetle (LD50 = 10.0 µg/adult), and V. jatamansi EO was the most active one against the cigarette beetle (LD50 = 17.6 µg/adult), while V. officinalis var. latifolia EO showed outstanding efficacy against the booklouse (LD50 = 40.2 µg/cm2). Binary mixtures of two major compounds (camphene and bornyl acetate) were assessed for the contact toxicity to the red flour beetle. Additive effect existed in the natural proportion of V. officinalis, and synergism was observed in that of V. officinalis var. latifolia. This work confirmed the insecticidal efficacy of the species of the Valerianaceae family, and it would offer some information for the development of botanical insecticide.


Assuntos
Monoterpenos Bicíclicos/química , Canfanos/química , Repelentes de Insetos/toxicidade , Valerianaceae , Animais , Besouros , Cromatografia Gasosa-Espectrometria de Massas , Repelentes de Insetos/análise , Insetos , Inseticidas/análise , Óleos Voláteis/química
5.
Environ Sci Pollut Res Int ; 26(24): 24988-24997, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31240663

RESUMO

Essential oils (EOs) extracted from leaves (EL) and fruit pericarp (EFP) of Zanthoxylum planispinum var. dintanensis were analyzed for their chemical composition by GC-MS technique and evaluated for their fumigant, contact toxicity and repellency against three stored-product insects, namely Tribolium castaneum, Lasioderma serricorne, and Liposcelis bostrychophila adults. Results of GC-MS analysis manifested that EL and EFP of Z. planispinum var. dintanensis were mainly composed of oxygenated monoterpenes. Major components included linalool, sylvestrene and terpinen-4-ol. The obvious variation observed between two oil samples was that EL contained 2-dodecanone (11.52%) in addition to the above mentioned components, while this constituent was not detected in EFP. Bioassays of insecticidal and repellent activities were performed for EL, EFP as well as some of their individual compounds (linalool, terpinen-4-ol and 2-dodecanone). Testing results indicated that EL, EFP, linalool, terpinen-4-ol and 2-dodecanone exhibited potent insecticidal and repellent activities against the three target insects selected. Among the three individual compounds, 2-dodecanone was significantly toxic to T. castaneum (LD50 = 5.21 µg/adult), L. serricorne (LD50 = 2.54 µg/adult) and L. bostrychophila (LD50 = 23.41 µg/cm2) in contact assays and had beneficial repellent effects on L. serricorne at 2 and 4 h post-exposure. The anti-insect efficacy of Z. planispinum var. dintanensis EO suggests it has potential to be used as botanical insecticide or repellent to control pest damage in warehouses and grain stores.


Assuntos
Repelentes de Insetos/farmacologia , Inseticidas/análise , Monoterpenos/química , Óleos Voláteis/química , Terpenos/química , Zanthoxylum/química , Monoterpenos Acíclicos , Animais , Besouros/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Repelentes de Insetos/química , Inseticidas/química , Dose Letal Mediana , Monoterpenos/análise , Oxirredução , Tribolium/química
6.
Ecotoxicol Environ Saf ; 169: 807-813, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30597779

RESUMO

In this work, the essential oils (EO) were extracted from seven typical Chinese herbs, and their repellent and contact toxicities against Tribolium castaneum adults (red flour beetles) were evaluated. The experimental results showed that the above EOs presented the various levels of repellent and contact toxicities. The EOs extracted from A. lancea and A argyi of the Compositae (Asteraceae) family presented obvious repellent effects (Repellency Percentage > 90% at 3.15 nL/cm2 after 4 h exposure) and strong contact toxicity with LD50 values of 5.78 and 3.09 µg/adult respectively. Based on literature researches and screening results, the EO from A. lancea was analyzed by GC-MS and chosen for further identification of bioactive components. Altogether 59 chemical components were identified and 17 of them were recognized as sesquiterpene compounds, accounting for 57.8% of the total weight of the EO. From the identified sesquiterpenes, three individual compounds (ß-eudesmol, hinesol, valencene) were selected for the laboratory bioassays of the toxicity against red flour beetles. It was found that all the three compounds expressed some repellent effects. Although ß-eudesmol (31.2%) and hinesol (5.1%) were identified as main constituents and had been considered to be symbolic characteristics of high medicinal value, valencene (0.3%) showed strong repellent property which could be comparable to that of DEET (N, N­diethyl­3­methylbenzamide), a powerful commercial pesticides, and it had best toxicity with LD50 values of 3.25 (µg/adult) in the contact test. This work may provide toxicity evidence of seven common herbs against red flour beetles, add the information for the development and comprehensive utilization of A. lancea, and will contribute to the application of grain preservation.


Assuntos
Atractylodes/química , Medicamentos de Ervas Chinesas/química , Inseticidas , Tribolium , Animais , Cromatografia Gasosa-Espectrometria de Massas , Repelentes de Insetos/química , Repelentes de Insetos/isolamento & purificação , Inseticidas/química , Inseticidas/isolamento & purificação , Óleos Voláteis , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação
7.
J Oleo Sci ; 67(8): 1027-1034, 2018 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-30012895

RESUMO

The essential oils (EOs) extracted from Evodia lenticellata Huang and Evodia rutaecarpa (Juss.) Benth. leaves are screened to evaluate their contact toxicity and repellency towards Tribolium castaneum (Coleoptera: Tenebrionidae), Lasioderma serricorne (Coleoptera: Anobiidae) and Liposcelis bostrychophila (Psocoptera: Liposcelididae) adults. The EOs are obtained by hydrodistillation and analyzed by gas chromatography-mass spectrometry (GC-MS). The principal components in the E. lenticellata EO are identified to be caryophyllene oxide (28.5%), ß-caryophyllene (23.1%), ß-elemene (14.5%), and ß-cubebene (4.7%), while the main components of the E. rutaecarpa EO are α-pinene (39.4%), ß-elemene (13.5%), α-ocimene (7.6%), and α-selinene (4.0%). These two kinds of EOs and their individual compounds all showed different levels of contact toxicity and repellent activity against three stored-product insects.


Assuntos
Besouros/efeitos dos fármacos , Evodia/química , Repelentes de Insetos , Óleos Voláteis/química , Óleos Voláteis/toxicidade , Folhas de Planta/química , Tribolium/efeitos dos fármacos , Monoterpenos Acíclicos , Alcenos/análise , Alcenos/toxicidade , Animais , Monoterpenos Bicíclicos , Destilação/métodos , Cromatografia Gasosa-Espectrometria de Massas , Monoterpenos/análise , Monoterpenos/toxicidade , Óleos Voláteis/isolamento & purificação , Sesquiterpenos Policíclicos , Sesquiterpenos/análise , Sesquiterpenos/toxicidade
8.
Medicine (Baltimore) ; 97(28): e11285, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29995761

RESUMO

Acute nonspecific neck pain is one of the major public health problems lacking efficient treatments. The present study was designed to observe the analgesic effect of intracutaneous injection of local anesthestics and steroids on acute nonspecific neck pain.Thirty-six newly diagnosed with acute nonspecific neck pain patients were randomized to receive ibuprofen (IPB group) or intracutaneous injection of local anesthetics (lidocaine and bupivacaine) and steroid (methylprednisolone) (MLB group). The pain intensity was the primary outcome and evaluated with visual analog scale (VAS). Neck disability index (NDI) and patient global impression of changes (PGIC) were monitored for overall outcomes.Following treatments, patients from the 2 groups have decreased VAS scores and NDI when compared with their baseline level at 3 hours, day 1, and day 3 time points. Interestingly, the MLB group patients have lower VAS scores and NDI than IPB group. MLB patients also had a greater PGIC than IPB group.This study indicates that single intracutaneous injection of local anesthetics and steroids is sufficient to alleviate acute nonspecific neck pain.


Assuntos
Metilprednisolona/administração & dosagem , Cervicalgia , Adulto , Anestésicos Locais/administração & dosagem , Bupivacaína/administração & dosagem , Monitoramento de Medicamentos/métodos , Feminino , Glucocorticoides/administração & dosagem , Humanos , Injeções Intradérmicas , Lidocaína/administração & dosagem , Masculino , Pessoa de Meia-Idade , Cervicalgia/diagnóstico , Cervicalgia/fisiopatologia , Cervicalgia/terapia , Manejo da Dor/métodos , Medição da Dor/métodos , Resultado do Tratamento
9.
Ecotoxicol Environ Saf ; 160: 342-348, 2018 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-29857238

RESUMO

In this work, the essential oil (EO) was extracted from the fruits of Evodia lenticellata, and the fumigant toxicity, contact toxicity and repellency against three stored-product insect species were evaluated for the obtained EO and several of its chemical components. The target insects were the adults of Tribolium castaneum (Coleoptera: Tenebrionidae), Lasioderma serricorne (Coleoptera: Anobiidae) and Liposcelis bostrychophila (Psocoptera: Liposcelididae). The EO was obtained with hydrodistillation and its chemical components were analyzed with the gas chromatography-mass spectrometry (GC-MS). Twenty-seven compounds, accounting for 83.1% of the total amount of the oil, were identified from the EO sample. The main compounds included linalool (12.0%), ß-pinene (11.5%), 3-carene (9.6%), caryophyllene oxide (8.7%) and ß-caryophyllene (7.9%). Among them, the amounts of monoterpenes and sesquiterpenes were as high as 52.7% and 22.7% to the total amount of EO respectively. The results of bioactivity test showed that the EO and its testing compounds had interspecific toxicity and repellent activity. So that, it might be expected that the EO extracted from the fruits of E. lenticellata could be developed to a new type of eco-friendly natural insecticide or repellent for the control of stored-product insects.


Assuntos
Evodia , Repelentes de Insetos/toxicidade , Inseticidas/toxicidade , Monoterpenos/toxicidade , Neópteros/efeitos dos fármacos , Óleos Voláteis/toxicidade , Compostos Fitoquímicos/toxicidade , Animais , Frutas , Cromatografia Gasosa-Espectrometria de Massas , Repelentes de Insetos/análise , Repelentes de Insetos/farmacologia , Inseticidas/análise , Inseticidas/farmacologia , Monoterpenos/análise , Monoterpenos/farmacologia , Óleos Voláteis/análise , Óleos Voláteis/farmacologia , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia
10.
Environ Sci Pollut Res Int ; 25(22): 22236-22243, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29804253

RESUMO

The extract from Cinnamomum cassia Presl bark was obtained with supercritical CO2 fluid extraction (SFE). Chemical components of the SFE extract were characterized by GC-MS spectrometry. The repellency and contact toxicity of the SFE extract were evaluated against the adults of Tribolium castaneum and Lasioderma serricorne along with those of its two main compounds. The results of GC-MS analysis indicated that 33 volatile constituents were identified from the extract. The main components included trans-cinnamaldehyde (32.1%), 3,3-dimethylhexane (10.6%) and 2,4-di-tert-butylphenol (7.9%). Testing results showed that the SFE extract had potent contact toxicity against T. castaneum and L. serricorne with LD50 values of 3.96 and 23.89 µg/adult, respectively. LD50 values of trans-cinnamaldehyde against T. castaneum and L. serricorne were 5.78 and 3.24 µg/adult, respectively. Additionally, percentage repellency values of the SFE extract and trans-cinnamaldehyde against T. castaneum and L. serricorne were rather high (PR = 100% and PR > 90%, respectively) at 78.63 and 15.73 nL/cm2 at 2 h post-exposure. 2,4-Di-tert-butylphenol showed some repellency against both beetle species. Considering its insecticidal and repellent effects, the SFE extract from C. cassia bark might be used in integrated pest management programs for T. castaneum and L. serricorne.


Assuntos
Cinnamomum aromaticum/química , Repelentes de Insetos/análise , Inseticidas/análise , Tribolium , Animais , Dióxido de Carbono , Cromatografia com Fluido Supercrítico , Cromatografia Gasosa-Espectrometria de Massas , Casca de Planta/química , Extratos Vegetais/química
11.
Nat Prod Res ; 32(10): 1234-1238, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-28532258

RESUMO

The major chemical constituents of the essential oil extracted from Artemisia dubia wall. ex Bess. (Family: Asteraceae) were found as terpinolene (19.02%), limonene (17.40%), 2,5-etheno[4.2.2]propella-3,7,9-triene (11.29%), isoelemicin (11.05%) and p-cymene-8-ol (5.93%). Terpinolene and limonene were separated as main components from the essential oil. The essential oil showed fumigant toxicity against Tribolium castaneum and Liposcelis bostrychophila with LC50 values of 49.54 and 0.74 mg/L, respectively. The essential oil and isolated compounds of A. dubia showed repellency activities against both insects. Terpinolene and limonene showed the fumigant toxicity against T. castaneum. Terpinolene showed obvious fumigant toxicity against L. bostrychophila. The results indicated that the essential oil of A. dubia had potential to be developed into natural insecticides for controlling stored product pests.


Assuntos
Artemisia/química , Repelentes de Insetos/farmacologia , Óleos Voláteis/química , Ftirápteros/efeitos dos fármacos , Tribolium/efeitos dos fármacos , Animais , Monoterpenos Cicloexânicos , Cicloexenos/farmacologia , Armazenamento de Alimentos , Controle de Insetos/métodos , Repelentes de Insetos/química , Limoneno , Terpenos/farmacologia
12.
Pain Manag Nurs ; 19(2): 186-194, 2018 04.
Artigo em Inglês | MEDLINE | ID: mdl-29153295

RESUMO

The therapeutic effect of postherpetic neuralgia (PHN) is often disappointing and challenging. The role of intra-cutaneous injection of local anesthetic and steroids in preventing PHN remains unknown. The purpose of this study was to investigate the effect of a single intra-cutaneous injection of ropivacaine plus methylprednisolone on acute thoracic herpes zoster (HZ) pain intensity and duration, eruptive duration, and PHN incidence. A total of 97 patients with acute thoracic HZ diagnosed 1-7 days after the onset of the rash were randomly assigned to receive either 15 mL of 37.5 mg ropivacaine plus 40 mg methylprednisolone (active group, n = 49) or 15 mL of saline (placebo group, n = 48). Over 7 days, all patients received 800 mg of acyclovir 5 times daily and 150 mg pregabalin twice daily. Acetaminophen was used as a rescue analgesia when visual analog scale ≥4. Pain intensity was measured with visual analog scale and the amount of analgesic taken was evaluated at the initial visit and at weeks 1, 4, 12, and 24 after the intra-cutaneous injection. The time of complete resolution of pain, time of healing of skin eruption, and incidence of PHN were reported. The active group displayed a significantly shorter duration of pain (28.4 ±â€¯46.7 vs. 59.2 ±â€¯65.0, respectively; p = .009) and herpetic eruption (22.5 ±â€¯6.8 vs. 32.6 ±â€¯7.6, respectively; p < .001) than the placebo group. A significantly lower incidence of PHN was encountered in the active group after 4 weeks (16.3% vs. 47.9%, respectively; p = .001) and 12 weeks (10.2% vs. 29.2%, respectively; p = .019). Lower incidence of PHN was noticed in the active group after 24 weeks; however, this was not statistically significant (6.1% vs. 18.8%, respectively; p = .059). There was a significant reduction in the average and total doses of pregabalin and acetaminophen in the active group after the injection. No serious side effects were noticed during the study period. Early single intra-cutaneous injection, in combination with antiviral agents and optimal analgesics, in the course of acute thoracic HZ seems to be a simple, well-tolerated, and effective adjuvant treatment modality. It dramatically decreased pain intensity, shortened pain duration, reduced skin eruption, and reduced and may even prevent the development of PHN.


Assuntos
Analgésicos/farmacologia , Herpes Zoster/tratamento farmacológico , Neuralgia Pós-Herpética/tratamento farmacológico , Administração Cutânea , Idoso , Amidas/farmacologia , Amidas/uso terapêutico , Analgésicos/uso terapêutico , Feminino , Humanos , Masculino , Metilprednisolona/farmacologia , Metilprednisolona/uso terapêutico , Pessoa de Meia-Idade , Placebos/farmacologia , Placebos/uso terapêutico , Estudos Prospectivos , Ropivacaina , Esteroides/farmacologia , Esteroides/uso terapêutico , Tórax/anormalidades , Tórax/efeitos dos fármacos , Escala Visual Analógica
13.
Molecules ; 22(8)2017 Aug 20.
Artigo em Inglês | MEDLINE | ID: mdl-28825643

RESUMO

Sixteen compounds were isolated from the leaves and stems of Murrayatetramera Huang. Based on the NMR and MS spectral results, the structures were determined. It was confirmed that the isolated compounds included three new compounds (9, 10 and 13) and one new natural product (8), which were identified asmurratetra A (9), murratetra B (10), murratetra C (13) and [2-(7-methoxy-2-oxochromen-8-yl)-3-methylbut-2-enyl]3-methylbut-2-enoate (8), respectively. Meanwhile, the repellent activity against Tribolium castaneum was investigated for 13 of these isolated compounds. The results showed that the tested compounds had various levels of repellent activity against T. castaneum. Among them, compounds 1 (4(15)-eudesmene-1ß,6α-diol), 11 (isoferulic acid) and 16 (2,3-dihydroxypropyl hexadecanoate) showed fair repellent activity against T. castaneum. They might be considered as potential leading compounds for the development of natural repellents.


Assuntos
Repelentes de Insetos/química , Repelentes de Insetos/farmacologia , Murraya/química , Extratos Vegetais/química , Tribolium/efeitos dos fármacos , Animais , Espectroscopia de Ressonância Magnética , Estrutura Molecular
14.
Nat Prod Res ; 31(10): 1201-1204, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-27563800

RESUMO

A screening of Chinese medicinal herbs and wild plants for agrochemicals was carried out; the essential oil of Glycosmis lucida leaves was found to possess significant repellent activity against Tribolium castaneum and Liposcelis bostrychophila. It was found that the main components included elixene (19.81%), spathulenol (10.68%), anethole (12.05%), verbenone (10.32%) followed by ß-caryophyllene (6.87%). The essential oil, anethole and verbenone were strongly repellent against T. castaneum (96, 86 and 94%, respectively, at 15.73 nL cm-2) and L. bostrychophila (100, 68 and 72%, respectively, at 31.58 nL cm-2) after a 2h treatment. The results indicate that anethole and verbenone had the potential to be developed as natural repellents for control of stored product insects.


Assuntos
Repelentes de Insetos/farmacologia , Óleos Voláteis/farmacologia , Rutaceae/química , Derivados de Alilbenzenos , Animais , Anisóis/farmacologia , Óleos Voláteis/análise , Tribolium
15.
Nat Prod Res ; 31(7): 791-796, 2017 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-27739326

RESUMO

One sulphur-containing amide (N-[2-(4-Hydroxyphenyl)-ethyl]-3-methanesulfonyl-N-methyl-propionamide) which was isolated from Glycosmis lucida Wall ex Huang had a different NMR profile with this kind of compounds' normal case. Based on the information obtained by nuclear magnetic resonance pectroscopy (NMR) and mass spectrometry (MS), its configurations in solution were investigated. The results indicated that the compound would have two stable configurations in solution as the double bond switched between C-N and C-O in an appropriate rate. This phenomenon was clearly exposed by the one dimension selective NOE (1D-NOE) experiments. This conclusion would play an active role in the structure analysis work of this kind of compounds.


Assuntos
Rutaceae/química , Amidas/química , Espectroscopia de Ressonância Magnética/métodos , Espectrometria de Massas , Estrutura Molecular , Sulfonamidas/química , Enxofre/química
16.
Pain Med ; 18(8): 1566-1572, 2017 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-27492741

RESUMO

BACKGROUND: Treatment of established postherpetic neuralgia (PHN) is difficult and often disappointing. In this study, we assessed the efficacy of repetitive intracutaneous injections with local anesthetics and steroids in acute thoracic herpes zoster (HZ) pain, herpetic eruption, and incidence of PHN. METHODS: Ninety-three patients with acute thoracic HZ were randomly assigned to receive a standard treatment of antiviral medication with p.o. analgesics or the standard treatment with the addition of repetitive intracutaneous injections of a local anesthetic and steroid mixture. Patients were permitted to take tramadol when the visual analog scale (VAS) ≥ 4. Pain assessment using VAS was conducted at the initial visit, as well as 1, 2, 4, 12, and 24 weeks after the end of the treatments. RESULTS: In comparison with the standard treatment group, the VAS scores of the intracutaneous injection group were significantly lower during the study. The intracutaneous injection group also reported shorter duration of pain and skin eruption than the control group ( P = 0.005 vs P < 0.001, respectively). At 1 month post-therapy, 12.8% patients in the intracutaneous injection group reported zoster-associated pain, compared with 47.8% in the standard treatment group ( P < 0.001). At 3 and 6 months post-therapy, the incidence of PHN was still significantly lower in the intracutaneous injection group than the standard treatment group. EuroQol VAS scores were significantly higher in the intracutaneous injection group vs standard treatment group (P < 0.001). CONCLUSION: Repetitive intracutaneous injections with local anesthetics and steroids along with standard treatment significantly reduce the duration of pain and herpetic eruption and incidence of PHN.


Assuntos
Amidas/administração & dosagem , Anestésicos Locais/administração & dosagem , Herpes Zoster/tratamento farmacológico , Metilprednisolona/administração & dosagem , Neuralgia Pós-Herpética/prevenção & controle , Fármacos Neuroprotetores/administração & dosagem , Aciclovir/uso terapêutico , Idoso , Idoso de 80 Anos ou mais , Analgésicos Opioides/uso terapêutico , Antivirais/uso terapêutico , Feminino , Humanos , Incidência , Injeções Intradérmicas , Masculino , Pessoa de Meia-Idade , Neuralgia Pós-Herpética/epidemiologia , Medição da Dor , Ropivacaina , Tramadol/uso terapêutico
17.
National Journal of Andrology ; (12): 302-308, 2017.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-812769

RESUMO

Objective@#To explore the effect of the AXL expression on the chemosensitivity of prostate cancer PC-3 and DU145 cells to docetaxel and possible mechanisms.@*METHODS@#Using Western blot, we examined the expressions of the AXL protein, p-AXL and Gas6 in the docetaxel-resistant PC-3 (PC-3-DR) and DU145 (DU145-DR) cells stimulated with gradually increased concentrations of docetaxel. We transfected the PC-3 and DU145 cells with negative NC ShRNA and AXL-ShRNA, respectively, which were confirmed to be effective, detected the proliferation, apoptosis and cycle distribution of the cells by CCK8, MTT and flow cytometry after treated with the AXL-inhibitor MP470 and/or docetaxel, and determined the expression of the ABCB1 protein in the PC-3-DR and DU145-DR cells after intervention with the AXL-inhibitor R428 and/or docetaxel.@*RESULTS@#The expression of the AXL protein in the PC-3 and DU145 cells was significantly increased after docetaxel treatment (P <0.05). The expressions AXL and p-AXL were remarkably higher (P <0.05) while that of Gas6 markedly lower (P <0.05) in the PC-3 and DU145 than in the PC-3-DR and DU145-DR cells. The inhibitory effect of docetaxel on the proliferation and its enhancing effect on the apoptosis of the PC-3 and DU145 cells were significantly decreased at 48 hours after AXL transfection (P <0.05). MP470 obviously suppressed the growth and promoted the apoptosis of the PC-3-DR and DU145-DR cells, with a higher percentage of the cells in the G2/M phase when combined with docetaxel than used alone (P <0.05). R428 markedly reduced the expression of ABCB1 in the PC-3-DR and DU145-DR cells, even more significantly in combination with docetaxel than used alone (P <0.05).@*CONCLUSIONS@#The elevated expression of AXL enhances the docetaxel-resistance of PC-3 and DU145 prostate cancer cells and AXL intervention improves their chemosensitivity to docetaxel, which may be associated with the increased cell apoptosis in the G2/M phase and decreased expression of ABCB1.


Assuntos
Humanos , Masculino , Membro 1 da Subfamília B de Cassetes de Ligação de ATP , Metabolismo , Antineoplásicos , Farmacologia , Apoptose , Contagem de Células , Ciclo Celular , Linhagem Celular Tumoral , Proliferação de Células , Docetaxel , Resistencia a Medicamentos Antineoplásicos , Peptídeos e Proteínas de Sinalização Intercelular , Metabolismo , Neoplasias da Próstata , Tratamento Farmacológico , Metabolismo , Patologia , Proteínas Proto-Oncogênicas , Genética , Metabolismo , Pirimidinas , Farmacologia , RNA Interferente Pequeno , Receptores Proteína Tirosina Quinases , Genética , Metabolismo , Taxoides , Farmacologia
18.
J Oleo Sci ; 65(10): 871-879, 2016 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-27628733

RESUMO

Two essential oil samples were obtained from the pericarp of Zanthoxylum bungeanum with the methods of hydrodistillation (HD) and supercritical fluid CO2 extraction (SFE), their chemical components were identified, and their bioactivities against Lasioderma serricorne adults were evaluated. In the process of testing, the two samples showed significant bioactivities against Lasioderma serricorne adults. For an example, the SFE-sample expressed relatively stronger fumigant toxicity on Lasioderma serricorne adults (LC50 = 3.99 µg/mL air) than that of the HD-sample (LC50 = 12.54 µg/mL air). According to GC-MS analysis, the chemical components between two samples were different. The major chemical components for HD included linalool (25.99%), limonene (19.34%), linalyl anthranilate (12.22%), 4-terpinenol (10.49%), eucalyptol (6.53%) and α-terpineol (5.02%), while for SFE included nonanoic acid (21.43%), γ-terpinene (14.51%), eucalyptol (13.45%), α-terpineol (5.83%) and caryophyllene oxide (5.48%). The results showed that different chemical components result in different bioactivities. This work provides theoretical basis for traditional Chinese concept of antagonistic storage, and it also provides important information for the development and comprehensive utilization of Zanthoxylum bungeanum.


Assuntos
Besouros/efeitos dos fármacos , Repelentes de Insetos , Inseticidas , Óleos de Plantas , Zanthoxylum/química , Animais , Cromatografia com Fluido Supercrítico , Destilação , Ácidos Graxos/análise , Ácidos Graxos/isolamento & purificação , Cromatografia Gasosa-Espectrometria de Massas , Repelentes de Insetos/análise , Repelentes de Insetos/isolamento & purificação , Inseticidas/análise , Inseticidas/isolamento & purificação , Monoterpenos/análise , Monoterpenos/isolamento & purificação , Óleos de Plantas/análise , Óleos de Plantas/isolamento & purificação , Sesquiterpenos/análise , Sesquiterpenos/isolamento & purificação
20.
Chem Biodivers ; 13(8): 1053-7, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-27482698

RESUMO

The insecticidal activity and chemical constituents of the essential oil from Ajania fruticulosa were investigated. Twelve constituents representing 91.0% of the essential oil were identified, and the main constituents were 1,8-cineole (41.40%), (+)-camphor (32.10%), and myrtenol (8.15%). The essential oil exhibited contact toxicity against Tribolium castaneum and Liposcelis bostrychophila adults with LD50 values of 105.67 µg/adult and 89.85 µg/cm(2) , respectively. The essential oil also showed fumigant toxicity against two species of insect with LC50 values of 11.52 and 0.65 mg/l, respectively. 1,8-Cineole exhibited excellent fumigant toxicity (LC50  = 5.47 mg/l) against T. castaneum. (+)-Camphor showed obvious fumigant toxicity (LC50  = 0.43 mg/l) against L. bostrychophila. Myrtenol showed contact toxicity (LD50  = 29.40 µg/cm(2) ) and fumigant toxicity (LC50  = 0.50 mg/l) against L. bostrychophila. 1,8-Cineole and (+)-camphor showed strong insecticidal activity to some important insects, and they are main constituents of A. fruticulosa essential oil. The two compounds may be related to insecticidal activity of A. fruticulosa essential oil against T. castaneum and L. bostrychophila.


Assuntos
Asteraceae/química , Insetos/efeitos dos fármacos , Inseticidas/farmacologia , Óleos Voláteis/farmacologia , Animais , Relação Dose-Resposta a Droga , Inseticidas/síntese química , Inseticidas/química , Óleos Voláteis/síntese química , Óleos Voláteis/química
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