Research advance on structure and function of amides in Zanthoxylum plants / 中国中药杂志

Zanthoxylum belongs to the Rutaceae family, and there are 81 Zanthoxylum species and 36 varieties in China. Most of the Zanthoxylum plants are used as culinary spice. In recent years, scholars in China and abroad have carried out in-depth research on Zanthoxylum plants, and found that the peculiar numbing sensation of Zanthoxylum plants originates from amides. It is also determined that amides are an important material basis for exerting pharmacological effects, especially in anti-inflammatory analgesia, anesthesia and other aspects. In this paper, 123 amides in 26 Zanthoxylum plants and their pharmacological activity that have been reported were summarized, which provided scientific reference for the clinical application of Zanthoxylum plants and the research and development of new drugs, and also facilitated the sustainable development and utilization of Zanthoxylum plant resources.

Síntesis y actividad antifúngica in vitro frente a Fusarium oxysporum de amidas N-alquilsustituidas derivadas de 2-aminoácidos

Una serie de amidas N-alquilsustituidas 1-16 fueron sintetizadas a partir de malonato de dietilo y ésteres de alquilo derivados de los aminoácidos L-triptófano, L-alanina, L-fenilalanina y L-tirosina. Los métodos de síntesis empleados involucraron calentamiento por irradiación de microondas empleando tanto un ácido de Lewis (AlCl3) o 4-dimetilaminopiridina (DMAP) como catalizador y auxiliar nucleofílico, respectivamente. Los resultados sugieren que el uso de irradiación de microondas y de DMAP conlleva mejores rendimientos en un tiempo de reacción más corto. Para ilustrar las diferencias observadas, se presentan las propuestas mecanísticas de cada método de reacción para la formación de amidas N-alquilsustituidas. Finalmente, las amidas sintetizadas se evaluaron en condiciones in vitro frente a Fusarium oxysporum; mostraron actividad antifúngica a diferentes niveles (0,40 mM < IC50 < 29,1 mM), lo cual indicó que las variaciones de la actividad observada de este grupo de compuestos pueden deberse al efecto de la amida acíclica como bioisóstero no clásico de algunas fitoalexinas heterocíclicas.

N-alkyl substituted amides 1-16 were synthesized from diethyl malonate and alkyl esters derived from the amino acids L -tryptophan, L -alanine, L -phenylalanine, and L -tyrosine. In addition, a microwave-assisted protocol was employed using a Lewis acid (AlCl3) or dimethylaminopyridine (DMAP) as a catalyst and nucleophilic auxiliary, respectively, affording the desired compounds. The results suggest that DMAP-catalyzed reactions under microwave irradiation yield higher during short reaction times. Each reaction method's mechanistic proposals for forming N-alkyl-substituted amides are presented to illustrate the observed differences. The synthesized amides were evaluated under in vitro conditions against Fusarium oxysporum. The compounds exhibited antifungal activity at different levels (0.40 mM < IC50 < 29.1 mM). These results indicated that the observed activity variations of this compound group might be due to the effect of acyclic amide as a non-classical bioisostere of some heterocyclic phytoalexins.

Uma série de amidas N-alquil substituídas foram sintetizadas a partir de malonato de dietila e ésteres alquílicos derivados dos aminoácidos ʟ-triptofano, L -alanina, L-fenilalanina e L-tirosina. Os métodos de síntese empregados foram realizados usando aquecimento por irradiação de micro-ondas empregando um ácido de Lewis (AlCl3) ou dimetilaminopiridina (DMAP) como catalisador. Os resultados sugerem que a irradiação de micro-ondas usando DMAP leva a melhores rendimentos em um tempo de reação mais curto. Para ilustrar as diferenças observadas, são apresentadas as propostas mecanísticas de cada método de reação para a formação de amidas N-alquilsubstituídas. Finalmente, as amidas sintetizadas foram avaliadas in vitro contra Fusarium oxysporum, mostrando atividade antifúngica em diferentes níveis (0.40 mM < IC50 < 29.1 mM), o que indica que as variações observadas na atividade desse grupo de compostos podem ser devidas ao efeito de amida acíclica como um bioisóstero não clássico de algumas fitoalexinas heterocíclicas.

Atualização em reações de hipersensibilidade aos anestésicos locais / Update on local anesthetics hypersensitivity reactions

Os anestésicos locais são essenciais em diversos procedimentos médicos e odontológicos. Funcionam estabilizando as membranas neuronais e inibindo a transmissão de impulsos neurais, o que permite a realização desses procedimentos com mais segurança e sem dor. As reações adversas a drogas são definidas pela Organização Mundial da Saúde como todos os efeitos nocivos, não intencionais e indesejáveis de uma medicação, que ocorrem em doses usadas para prevenção, diagnóstico e tratamento. As reações de hipersensibilidade são reações adversas do tipo B, imprevisíveis, que clinicamente se assemelham a reações alérgicas e podem ou não envolver um mecanismo imune. As reações de hipersensibilidade verdadeiras aos anestésicos locais são raras, apesar de superestimadas. Nesta revisão destacamos a necessidade de uma avaliação completa dos pacientes com suspeita de reação alérgica aos anestésicos locais, incluindo a investigação de outros possíveis alérgenos que tenham sido utilizados no procedimento, como analgésicos, antibióticos e látex. A estratégia de investigação e seleção de pacientes para testes deve se basear na história clínica. Dessa forma, poderemos fornecer orientações mais assertivas e seguras aos pacientes.

Local anesthetics are essential in many medical and dental procedures. They work by stabilizing neuronal membranes and inhibiting the transmission of neural impulses, which allows these procedures to be performed more safely and without pain. Adverse drug reactions are defined by the World Health Organization as all harmful, unintended and undesirable effects of a medication, which occur at doses used for prevention, diagnosis and treatment. Hypersensitivity reactions are unpredictable type B adverse reactions that clinically resemble allergic reactions and may or may not involve an immune mechanism. True hypersensitivity reactions to local anesthetics are rare, although overestimated. In this review, we highlight the need for a thorough evaluation of patients with suspected allergic reaction to local anesthetics, including investigation of other possible allergens that may have been used in the procedure, such as analgesics, antibiotics and latex. The investigation strategy and patient selection for testing should be based on clinical history. In this way, we will be able to provide more assertive and safe guidelines to patients.

Comparison of efficacy of different volume of ropivacaine for subomohyiod anterior suprascapular nerve block in patients undergoing arthroscopic shoulder surgery with general anesthesia / 中华麻醉学杂志

Objective:To compare the efficacy of different volume of ropivacaine for subomohyiod anterior suprascapular nerve block (aSSNB) in the patients undergoing arthroscopic shoulder surgery with general anesthesia.Methods:One hundred and thirty-five patients of either sex, aged 18-64 yr, with body mass index of 18-30 kg/m 2, of American Society of Anesthesiologists Physical Status classification Ⅰ or Ⅱ, scheduled for elective arthroscopic shoulder surgery, were divided into 3 groups ( n=45 each) using a random number table method: 0.5% ropivacaine 5 ml group (L group), 10 ml group (M group), and 15 ml group (H group). Before induction, aSSNB was performed with 0.5% ropivacaine 5, 10 and 15 ml in L, M and H groups, respectively.Diaphragmatic excursion, occurrence and degree of diaphragmatic paralysis, decrease in SpO 2, dyspnea and Horner syndrome were recorded at 30 min after injection.The intraoperative consumption of remifentanil and cardiovascular events were recorded.The extubation time, length of post-anesthesia care unit stay, and duration of sensory block were recorded.Quality of Recovery-15 scale score and score for patient′s satisfaction with analgesia were recorded.The first pressing time of analgesic pump, effective pressing frequency of analgesic pump, requirement for rescue analgesia, nausea, vomiting and nerve block-related complications within 24 h after surgery were recorded. Results:Compared with group L, the incidence of diaphragmatic paralysis was significantly increased, the degree of diaphragmatic paralysis was aggravated, the first pressing time of analgesic pump and duration of sensory block were prolonged, the effective pressing times of analgesic pump was reduced, and the requirement for rescue analgesia was decreased in M and H groups, and the decrease in SpO 2 was significantly increased, and the introperative consumption of remifentanil was decreased in group H ( P<0.05). Compared with group M, the decrease in SpO 2 and incidence of diaphragmatic paralysis were significantly increased, the degree of diaphragmatic paralysis was aggravated, the first pressing time of analgesic pump and duration of sensory block were prolonged ( P<0.05), and no significant change was found in the introperative consumption of remifentanil, the effective pressing times of analgesic pump or requirement for rescue analgesia in group H ( P>0.05). There was no significant difference in the incidence of cardiovascular events, score for patient′s satisfaction with analgesia, incidence of dyspnea and extubation time, length of post-anesthesia care unit stay, Quality of Recovery-15 sacle score, and the incidence of nausea and vomiting among three groups ( P>0.05). There were no Horner syndrome and nerve block-related complications in the three groups. Conclusions:Subomohyoid aSSNB with 0.5% ropivacaine hydrochloride 10 ml provides optimal efficacy when used for subomohyiod anterior suprascapular nerve block in patients undergoing arthroscopic shoulder surgery with general anesthesia.

Optimization efficacy of nalbuphine mixed with ropivacaine for epidural labor analgesia in primiparas: comparison with sufentanil mixed with ropivacaine / 中华麻醉学杂志

Objective:To evaluate the optimization efficacy of ropivacaine mixed with nalbuphine for epidural labor analgesia through comparison with ropivacaine mixed with sufentanil in primiparas.Methods:Four hundred and forty primiparas with a singleton fetus in vertex presentation without abnormal fetus, aged 19-36 yr, at 37-42 weeks of gestation, who were suitable and volunteered to receive epidural labor analgesia, were selected and randomly divided into observation group (NR group, n=220) and conventional group (C group, n=220).Epidural labor analgesia solution contained nalbuphine 40 mg and ropivacaine 120 mg in 150 ml of normal saline in group NR.Epidural labor analgesia solution contained sufentanil 50 μg and ropivacaine 120 mg in 150 ml of normal saline in group C. The analgesia pump was set up to deliver a 5 ml bolus dose with a 20-min lockout interval, programmed intermittent bolus 10-15 ml/h and background infusion at 2 ml/h after an initial dose of 15 ml to maintain VAS score <3.The length of labor, adverse reactions during labor analgesia, neonatal Apgar score, parameters of umbilical artery blood gas analysis and neonatal behavioral neurological assessment score were recorded. Results:Compared with group C, the incidence of urinary retention, pruritus, nausea and vomiting and fever at birth was significantly decreased in group NR ( P<0.05).The duration of the first and second stages of labor, neonatal Apgar score, pH value of umbilical artery blood, lactate concentrations, and neonatal behavioral neurological assessment score were within the normal range in both groups, and there was no significant difference between the two groups ( P>0.05). Conclusions:Compared with conventional medication, nalbuphine mixed with ropivacaine has the same efficacy when used for epidural labor analgesia in primiparas, but it has a certain optimization efficacy in terms of safety.

Effect of dexmedetomidine on blood concentrations of ropivacaine during sciatic nerve block in rabbits / 中华麻醉学杂志

Objective:To evaluate the effect of dexmedetomidine on the blood concentrations of ropivacaine during sciatic nerve block in rabbits.Methods:Twelve New Zealand rabbits of both sexes, weighing 2-3 kg, were randomly divided into ropivacaine group (R group) and ropivacaine mixed with dexmedetomidine group (RD group). The right femoral vein was cannulated for blood sampling in both groups, 0.375% ropivacaine 3 ml was injected around the left sciatic nerve in group R, and 0.375% ropivacaine 3 ml containing 1.5 μg/kg dexmedetomidine was injected instead in group RD.Blood samples from the right femoral vein were collected before nerve block (T 0) and at 15, 30, 45, 60, 120 and 180 min after nerve block (T 1-6) for determination of plasma concentrations of ropivacaine using high-performance liquid chromatography after centrifugation, and concentration-time curves were plotted. Results:Compared with group R, the blood concentrations of ropivacaine were significantly decreased at T 1-3 ( P<0.05), no significant change was found in the blood concentrations of ropivacaine at T 4-6 ( P>0.05), the peak blood concentration of ropivacaine was significantly decreased ( P<0.01), and no significant change was found in the time to peak blood concentrations of ropivacaine or area under the concentration-time curves in group RD ( P>0.05). Conclusions:Dexmedetomidine can decrease the blood concentrations of ropivacaine during sciatic nerve block in rabbits.

Effect of butorphanol mixed with ropivacaine for erector spinae plane block on postoperative outcomes in patients undergoing thoracoscopic pulmonary lobectomy / 中华麻醉学杂志

Objective:To evaluate the effect of butorphanol mixed with ropivacaine for erector spinae plane block (ESPB) on postoperative outcomes in the patients undergoing thoracoscopic pulmonary lobectomy.Methods:Eighty patients of either sex, aged 35-64 yr, with body mass index of 19-30 kg/m 2, of American Society of Anesthesiologists physical status Ⅰ or Ⅱ, undergoing elective thoracoscopic pulmonary lobectomy, were divided into 2 groups ( n=40 each) using a computer-generated random number table method: butorphanol mixed with ropivacaine for ESPB group (group EB) and ropivacaine for ESPB group (group E). ESPB was performed under ultrasound guidance in both groups.A mixture of 0.1% butorphano 1 ml and 0.375% ropivacaine 20 ml was injected in EB group, and 0.375% ropivacaine 20 ml was injected in E group.The other anesthesia methods were the same in the two groups.And target-controlled infusion was stopped and PCIA was performed at the end of skin suture in the two groups.The intraoperative consumption of remifentanil, first time to press an analgesia pump, requirement for rescue analgesia within 24 h after surgery, and occurrence of ESPB-related complications were recorded.Quality of Recovery-40 (QoR-40) scores were recorded at 7 days after surgery.Before induction of anesthesia (T 1) and at 24 h after operation (T 2), the peripheral venous blood samples were collected for determination of plasma interleukin-6 (IL-6) and IL-10 concentrations, and bedside pulmonary function test was performed, and FEV 1/FVC was calculated. Results:Compared with group E, the QoR-40 scores were significantly increased at 7 days after operation, FEV 1/FVC was increased at T 2, the plasma concentrations of IL-10 were decreased at T 2, the plasma concentrations of IL-10 were increased at T 2, the intraoperative consumption of remifentanil was reduced, the first time to press an analgesia pump was prolonged, and the requirement for rescue analgesia within 24 h after surgery was decreased in group EB ( P<0.05). No ESPB-related complications were found in either group. Conclusion:Butorphanol mixed with ropivacaine for ESPB can improve postoperative outcomes in the patients undergoing thoracoscopic pulmonary lobectomy.

Median effective dose of 0.5% ropivacaine for ultrasound-guided femoral nerve block when combined with dexmedetomidine: dose based on per unit femoral nerve cross-sectional area / 中华麻醉学杂志

Objective:To determine the median effective dose (ED 50) of 0.5% ropivacaine when combined with dexmedetomidine based on femoral nerve cross-sectional area for ultrasound-guided femoral nerve block. Methods:American Society of Anesthesiologists physical statusⅠor Ⅱ patients of both sexes, aged 18-64 yr, with body mass index of 20-30 kg/m 2, scheduled for elective open reduction and internal fixation for patella fracture or removal of patella fracture by internal fixation, were randomly divided into dexmedetomidine and ropivacaine group (group DR) and ropivacaine group (group R). In group DR, 0.5% ropivacaine and 0.5 μg/kg dexmedetomidine were injected.In group R, 0.5% ropivacaine was injected.Ultrasonic localization of femoral nerve was performed for measurement of the femoral nerve cross-sectional area, and 0.5% ropivacaine was injected based on the area.ED 50 was determined by Dixon′ s up-and-down sequential method.The initial dose was 0.22 ml/mm 2, and the difference between the two successive doses was 0.02 ml/mm 2.The effective block was defined as complete loss of pain sensation in the areas of anterior skin of knee joint, skin on the inner side of the calf and dorsal medial skin of the foot and the degree of motor block was in stages 1-3 assessed using Brunnstrom motor function within 30 min after nerve block.Nerve block was considered ineffective if pain occurred in any nerve distribution area mentioned above.The study was terminated if 7 effective and ineffective alternating waves occurred.ED 50 and 95% confidence interval (CI) were calculated using Probit analysis. Results:In group R, 27 patients were enrolled in the study, and ED 50 (95%CI) of 0.5% ropivacaine for ultrasound-guided femoral nerve block was 0.106 (0.069-0.125) ml/mm 2.In group DR, 23 patients were enrolled in the study, and ED 50 (95% CI) of 0.5% ropivacaine for ultrasound-guided femoral nerve block was 0.038 (0.011-0.059) ml/mm 2.Compared with group R, ED 50 of 0.5% ropivacaine for femoral nerve block was significantly decreased in group R. Conclusion:When combined with dexmedetomidine 0.5 μg/kg, ED 50 of 0.5% ropivacaine based on femoral nerve cross-sectional area for ultrasound-guided femoral nerve block is 0.038 ml/mm 2.

Median effective dose of 0.5% ropivacaine for ultrasound-guided femoral nerve block: dose per unit femoral nerve cross-sectional area / 中华麻醉学杂志

Objective:To determine the median effective dose (ED 50) of 0.5% ropivacaine based on femoral nerve cross-sectional area for ultrasound-guided femoral nerve block. Methods:Patients of both sexes, aged 18-64 yr, of American Society of Anesthesiologists physical status I or Ⅱ, with body mass index of 20-30 kg/m 2, scheduled for elective open reduction and internal fixation for patella fracture or removal of patella fracture by internal fixation, were enrolled in this study.Ultrasonic localization of femoral nerve was performed for measurement of the femoral nerve cross-sectional area, and 0.5% ropivacaine was injected based on the area.ED 50 was determined by Dixon′s up-and-down sequential method.The initial dose was 0.22 ml/mm 2, and the difference between the two successive doses was 0.02 ml/mm 2.The effective block was defined as complete loss of pain sensation in the areas of anterior skin of knee joint, skin on the inner side of the calf and dorsal medial skin of the foot and the degree of motor block was in stages 1-3 assessed using Brunnstrom motor function within 30 min after nerve block.Nerve block was considered ineffective if pain occurred in any nerve distribution area mentioned above.The study was terminated if 7 effective and ineffective alternating waves occurred.ED 50 and 95% confidence interval (CI) were calculated using Probit analysis. Results:Twenty-seven patients were enrolled in the study with the femoral nerve cross-sectional area (75±5) mm 2.ED 50 (95%CI) of 0.5% ropivacaine for ultrasound-guided femoral nerve block was 0.106 (0.069-0.125) ml/mm 2. Conclusion:ED 50 of 0.5% ropivacaine based on femoral nerve cross-sectional area for ultrasound-guided femoral nerve block is 0.106 ml/mm 2.

Optimized strategy of anesthesia for thoracoscopic pulmonary surgery: erector spinae plane block with high volume of ropivacaine combined with general anesthesia / 中华麻醉学杂志

Objective:To evaluate the optimized efficacy of erector spinae plane block (ESPB) with high volume of ropivacaine combined with general anesthesia for patients undergoing thoracoscopic pulmonary surgery.Methods:Sixty American Society of Anesthesiologists physical status Ⅰ or Ⅱ patients of both sexes, aged 18-64 yr, with body mass index of 18-24 kg/m 2, scheduled for elective thoracoscopic pulmonary surgery, were divided into 2 groups ( n=30 each) using a random number table method: ESPB with high volume (40 ml) of 0.4% ropivacaine combined with general anesthesia group (E40 group) and ESPB with conventional volume (20 ml) of 0.4% ropivacaine combined with general anesthesia group (E20 group). Ultrasound-guided ESPB was performed on the operated side before general anesthesia induction in both groups.In E40 group, 0.4% ropivacaine 40 ml was injected.In E20 group, 0.4% ropivacaine 20 ml was injected.Total intravenous anesthesia was applied in both groups.Sufentanil was used for patient-controlled intravenous anesthesia (PCIA) after the end of operation.The PCIA pump was set up with a 2 ml bolus dose (0.04 μg/kg), a 10 min lockout interval and background infusion at a rate of 0.05 μg·kg -1·h -1.The analgesia lasted for 48 h after operation, and the numeric rating scale (NRS) score was maintained ≤ 3.When NRS score ≥ 4, morphine 5 mg was intravenously injected for rescue analgesia.The onset time of block, intraoperative consumption of propofol and remifentanil, time to first pressing the analgesia pump, the first requirement for morphine and the ratio of patients using morphine within 48 h after surgery were recorded.The cumulative consumption of requirement for opioids (effective pressing dose of analgesic pump+ consumption of requirement for morphine) within 12, 24, 36 and 48 h after surgery and satisfaction with analgesia were recorded.The extubation time, length of ICU stay, the first postoperative off-bed time, the chest tube removal time and duration of stay in hospital were recorded.The incidence of intraoperative adverse events (hypertension and hypotension) and postoperative adverse events (dizziness, nausea and vomiting) were recorded. Results:Compared with E20 group, the onset time of block was significantly shortened, the cumulative consumption of requirement for opioids within 24, 36 and 48 h after surgery was decreased, the ratio of paitents using morphine within 48 h after surgery was decreased, time to first pressing the analgesia pump and the first requirement for morphine were prolonged, satisfaction with analgesia score was increased, and the first postoperative off-bed time and the chest tube removal time were shortened in group E40 ( P<0.05). There was no significant difference in the incidence of adverse events between the 2 groups ( P>0.05). Conclusion:Compared with ESPB with the conventional volume of ropivacaine combined with general anesthesia, ESPB with the high volume of ropivacaine combined with general anesthesia can reduce the postoperative consumption of opioids, and prolong the duration of effective analgesia, which are helpful for postoperative rapid recovery without increasing the development of adverse events in patients undergoing thoracoscopic pulmonary surgery.

Identification of Chemical Constituents in Caulis of Erycibe schmidtii by UPLC-Q-Exactive Focus-MS/MS / 中国实验方剂学杂志

Objective:To rapidly recognize and identify the chemical constituents in caulis of Erycibe schmidtii by ultra-high performance liquid chromatography coupled with Q-Exactive Focus mass spectrometry (UPLC-Q-Exactive Focus-MS/MS). Method:Taking 80% methanol extract of E. schmidtii caulis as the test solution, the chemical constituents in caulis of E. schmidtii were analyzed and identified. Thermo Accucure aQ C18 column (2.1 mm×150 mm, 2.6 μm) was used for chromatographic separation with the mobile phase of methanol (A)-0.1% formic acid solution (B) for gradient elution (0-12 min, 5%-25%A; 12-20 min, 25%-30%A; 20-28 min, 30%-38%A; 28-40 min, 38%-42%A). Positive and negative ion monitoring modes and heated electrospray ion source (HESI) were used for mass spectrographic analysis. The scanning range was m/z 80-1 200. Result:A total of 42 chemical constituents from caulis of E. schmidtii were identified, including 12 coumarins, 14 chlorogenic acids, 1 tropane alkaloid, 1 amide and 14 esterified glycosides. Conclusion:Chemical constituents in caulis of E. schmidtii can be quickly and fully identified by UPLC-Q-Exactive Focus-MS/MS. Among them, 11 compounds are unambiguously identified by comparing with reference standards, 31 compounds are reported for the first time in this herb, 2 compounds are reported for the first time in Erycibe plants. This paper can provide the important basis for study on pharmacodynamic material base and substitute development of E. schmidtii caulis.

Efficacy of patient-controlled brachial plexus block with different concentrations of dexmedetomidine mixed with ropivacaine for analgesia after elbow joint surgery / 中华麻醉学杂志

Objective To evaluate the efficacy of patient-controlled brachial plexus block with different concentrations of dexmedetomidine mixed with ropivacaine for analgesia after elbow joint surgery.Methods One hundred patients of both sexes,aged 18-64 yr,weighing 45-75 kg,of American Society of Anesthesiologists physical status Ⅰ or Ⅱ,undergoing elbow joint surgedyy,were divided into 4 groups (n =25 each) using a random number table method:different concentrations of dexmedetomidine mixed with ropivacaine groups (DR1-3 groups) and ropivacaine group (group R).An analgesia pump was connected at the end of surgery and patient-controlled brachial plexus block was performed.The patient-controlled analgesia (PCA) solution contained 0.5 μg/ml dexmedetomidine and 0.2％ ropivacaine in group DR1,0.75 μg/ml dexmedetomidine and 0.2％ ropivacaine in group DR2,1 μg/ml dexmedetomidine and 0.2％ ropivacaine in group DR3 and 0.3％ ropivacaine in group R.All the drugs were diluted to 400 ml in normal saline in each group.The PCA pump was set up to deliver 3 ml bolus dose with a 20-min lockout interval and background infusion at 5 ml/h.Parecoxib 0.6 mg/kg was intravenously injected as a rescue analgesic.The visual analogue scale (VAS) scores at rest and during movement (voluntary and continuous passive movement) were recorded at the end of surgery and 12,24,36,48 and 72 h after surgery.The number of successfully delivered doses,the number of attempt and postoperative consumption of parecoxib were recorded.The elbow flexion angle during voluntary and continuous passive movement was recorded.The development of motor block and drug-related adverse reactions was also recorded.Results There was no significant difference in VAS scores at rest at each time point among the four groups (P＞0.05).Compared with group R,the VAS scores during movement,the number of attempts,the number of successfully delivered doses and parecoxib consumption were significantly increased in DR1 and DR2 groups,the elbow flexion angle during voluntary and continuous passive mnovement was significantly decreased in group DR1,the elbow flexion angle during continuous passive movement was significantly decreased in group DR2,and the elbow flexion angle during voluntary movement was significantly increased (P＜0.05),and no significant change was found in the other parameters in group DR3 (P＞0.05).Compared with group DR1,the VAS scores during movement were significantly decreased,the number of attempts,the number of successfully delivered doses and parecoxib consumption were decreased,and the elbow flexion angle during voluntary and continuous passive movement was increased in DR2 and DR3 groups (P＜0.05).Compared with group DR2,the VAS scores during movement were significantly decreased,the number of attempts,the number of successfully delivered doses and parecoxib consumption were decreased,and the elbow flexion angle during voluntary and continuous passive movement was increased in group DR3 (P＜0.05).No motor block was found in DR1,DR2,and DR3 groups,and the incidence of motor block was significantly higher in group R than in the other three groups (P＜0.05).The hemodynamics was stable and no drug-related adverse reactions were found in the perioperative period in the four groups.Conclusion Patient-controlled brachial plexus block with dexmedetomidine 1 μg/ml mixed with 0.2％ ropivacaine can provide satisfactory analgesia and is helpful in improving prognosis for the patients undergoing elbow joint surgery.

Dose-response relationship of ropivacaine for paravertebral nerve block in treating acute severe herpetic neuralgia / 中华麻醉学杂志

Objective To determine the dose-response relationship of ropivacaine for paravertebral nerve block in treating acute severe herpetic neuralgia.Methods One hundred patients with herpetic neuralgia,with the course of disease ≤ 1 month,of numeric rating scale score ≥ 7 points,scheduled for elective paravertebral nerve block with ropivacaine under ultrasound guidance,were divided into 5 groups n=20 each) using a random number table method:5 different concentrations of ropivacaine groups R1.5 groups).The herpes zoster-affected thoracic spinal nerves were identified,and the mixture 5 ml was injected into the paravertebral space corresponding to the spinal nerves.The mixture solution contained ropivacaine with the concentrations of 0.075 0％ (group R1),0.112 5％ (group R2),0.150 0％ (group R3),0.187 5％ (group R4) and 0.225 0％ (group R5),compound betamethasone 1 ml,and mecobalamin injection 1 ml diluted to 20 ml with normal saline.Effective block was defined as numeric rating scale score≤ 1 point at 10 min after paravertebral nerve block with ropivacaine.The median effective concentration (EC50),95％ effective concentration (EC9s) and 95％ confidence interval of ropivacaine for paravertebral nerve block in treating acute severe shingles neuralgia were calculated by Probit analysis.Results The EC50 and EC95 (95％ confidence interval) of ropivacaine for paravertebral nerve block in treating acute severe shingles neuralgia were 0.150 0％ (0.097 0％-0.216 0％) and 0.216 0％ (0.175 0％-0.541 0％),respectively.Conclusion The EC50and EC95 of ropivacaine for paravertebral nerve block in treating acute severe herpetic neuralgia are 0.150 0％ and 0.216 0％,respectively.

Optimum compatibility of nabupine mixed with ropivacaine for patient-controlled epidural analgesia after cesarean section / 中华麻醉学杂志

Objective To evaluate the optimum compatibility of nalbufine combined with ropivacaine for patient-controlled epidural analgesia (PCEA) after cesarean section.Methods A total of 100 parturients who were at full term with a singleton fetus,aged 24-35 yr,with body mass index of 29-33 kg/m2,of American society of Anesthesiologists physical status Ⅱ,scheduled for elective cesarean section under combined spinal-epidural anesthesia,were divided into 4 groups (n =25 each) using a random number table method:sufentanil 0.5 μg/ml plus 0.15％ ropivacaine group (SR group),nalbufine at final concentration of 0.2 mg/ml plus 0.15％ ropivacaine group (N1 R group),nalbufine at final concentration of 0.4 mg/ml plus 0.15％ ropivacaine group (N2R group) and nalbufine at final concentration of 0.4 mg/ml plus 0.1％ ropivacaine group (N3Rgroup).PCEA solution was prepared correspondingly after surgery,and all the drugs were diluted to 100 ml in normal saline in each group.The PCA pump was set up to deliver a 0.5 ml bolus dose with a 15-min lockout interval and background infusion at 2 ml/h.Visual analog scale scores of incisional pain and anduterine contraction pain were maintained＜4.Ramsay sedation scores were recorded at 8,12,24 and 48 h after surgery.The total pressing times of PCEA were recorded within 48 h after surgery.The development of adverse reactions such as nausea,vomiting,skin itching,numbness of lower extremity,urinary retention and respiratory depression was recorded in the analgesia period.Venous blood samples were collected before surgery and at 24 and 48 h after surgery for determination of plasma prolactin concentrations,and the time of colostrum was recorded.Neonatal nerve and adaptive capacity was assessed and scored.Results Compared with group SR,the total pressing times of PCEA were significantly reduced in N2R and N3R groups (P＜0.05),and no significant change was found in the total pressing times of PCEA in group N1R (P＞0.05).Compared with group N1R,the total pressing times of PCEA were significantly reduced in N2R and N3 R groups (P＜0.05).There was no significant difference in the total pressing times of PCEA between group N2R and group N3R (P＞0.05).The Ramsay sedation score was 2 in four groups.There was no significant difference in numbness of lower extremity,plasma prolactin concentrations or neonatal nerve and adaptive capacity scores among four groups (P＞0.05).Conclusion Nalbufine at final concentraction of 0.4 mg/ml mixed with 0.1％ ropivacaine is the optimum compatibility when used for PCEA after cesarean section.

Proteomic profile of Piper tuberculatum (Piperaceae) / Perfil proteômico e metabólico de Piper tuberculatum (Piperaceae)

Abstract Piper tuberculatum (Piperaceae) is a species that accumulates especially amides as secondary metabolites and several biological activities was previously reported. In this article, we report a proteomic study of P. tuberculatum. Bidimensional electrophoresis (2D SDS-PAGE) and mass spectrometry (ESI-Q-TOF) were used in this study. Over a hundred spots and various peptides were identified in this species and the putative functions of these peptides related to defense mechanism as biotic and abiotic stress were assigned. The information presented extend the range of molecular information of P. tuberculatum.

Resumo Piper tuberculatum (Piperaceae) é uma espécie que acumula especialmente amidas como metabólitos secundários e diversas atividades biológicas dessa espécie foram relatadas anteriormente. No presente artigo, relatamos um estudo proteômico dessa espécie. Eletroforese bidimensional (2D SDS-PAGE) e espectrometria de massas (ESI-Q-TOF) foram utilizadas nesse estudos. Mais de cem spots e vários peptídeos foram identificados nesta espécie e as funções putativas desses peptídeos relacionadas a mecanismo de defesa como estresse biótico e abiótico foram atribuídos. As informações apresentadas ampliam a gama de informações moleculares dessa espécie.

Efficacy of dental local anesthetics: A review

The objective of this review was to investigate the efficacy of dental local anesthetics, as it is well known among clinicians that local anesthesia may be challenging in some circumstances. Therefore, the focus of this review was on the efficacy of the products used in dental local anesthesia. In a Pubmed database literature search conducted, a total of 8646 articles were found to be related to dental local anesthetics. After having applied the inclusion criteria (human research, performed in the last 10 years, written in English language, and focus on dental local anesthetics) and having assessed the quality of the papers, 30 were deemed eligible for inclusion in this review. The conclusion of this review is that none of the dental local anesthetic amides provide 100% anesthesia. The problem appears to be more pronounced when mandibular teeth are attempted to be anaesthetized and especially if there is irreversible pulpitis involved. The authors conclude that this finding suggest exploration of more efficient techniques to administer dental local anesthesia, especially in the mandible, to establish a 100% efficacy, is needed.

Chemical constituents of amides from Zanthoxylum planispinum / 中草药

Objective: To study the chemical constituents of Zanthoxylum planispinum. Methods: The compounds were isolated and purified by repeated silica gel column chromatography, Sephadex LH-20 gel column chromatography, and preparative HPLC. Their chemical structures were identified on the basis of physico-chemical properties and spectral analysis. Results: Seven amides were isolated and elucidated as (2E, 7E, 9E)-N-isobutyl-6,11-dioxo-2,7,9-dodecatrienamide (1), armatamide (2), pellitorine (3), lanyuamide I (4), tetrahydro-bungeanool (5), hydroxy-γ-isosanshool (6), and dihydrobungeanool (7). Conclusion: Compound 1 is a new unsaturated alkylamide named planispinamide, and compounds 2-7 are obtained from this plant for the first time.

Efficacy of different doses of dexmedetomidine mixed with ropivacaine used for thoracic paraverte-bral nerve block combined with general anesthesia in patients undergoing radical resection of lung cancer / 中华麻醉学杂志

Objective To evaluate the efficacy of different doses of dexmedetomidine mixed with ropivacaine used for thoracic paravertebral nerve block (TPVB) combined with general anesthesia in the pa-tients undergoing radical resection of lung cancer. Methods One hundred patients of both sexes, aged 18-64 yr, with body mass index of 18-25 kg∕m2, of American Society of Anesthesiologists physical statusⅡorⅢ, scheduled for elective radical resection of lung cancer, were divided into 5 groups (n＝20 each) using a random number table method: general anesthesia group ( group G), TPVB with ropivacaine com-bined with general anesthesia group (group R), TPVB with 0. 5 μg∕kg dexmedetomidine mixed with ropiva- caine combined with general anesthesia group (group RD0. 5), TPVB with 1. 0 μg∕kg dexmedetomidine mixed with ropivacaine combined with general anesthesia group (group RD1. 0), and TPVB with 2. 0 μg∕kg dexmedetomidine mixed with ropivacaine combined with general anesthesia group ( group RD2. 0). Two-point TPVB was performed, and anesthetic 10 ml was injected into each puncture site. Zero point five per-cent ropivacaine was administered in group R. Dexmedetomidine 0. 5, 1. 0 and 2. 0 μg∕kg mixed with ropi-vacaine at the final concentration of 0. 5% were injected in group RD0. 5, group RD1. 0 and group RD2. 0, respectively. Anesthesia was maintained by intravenously infusing propofol and remifentanil and cisatracuri-um was intermittently injected to maintain muscle relaxation. The occurrence of intraoperative hypotension and bradycardia was recorded. The emergence time, extubation time, duration of postanesthesia care unit (PACU) stay and requirement for rescue analgesia during emergence from anesthesia were also recorded. Small marginal lung samples next to the tumor were harvested immediately after removing the tumor tissues. The expression of caspase-3 and Bcl-2 was determined by Western blot, the content of IL-1β in lung tissues was determined by enzyme-linked immunosorbent assay, the cell apoptosis was evaluated by TUNEL, and apoptosis index ( AI) was calculated. The injury to lung tissues was observed with a light microscope and scored. Results Compared with G and R groups, AI, IL-1β content and lung injury score were signifi-cantly decreased, the expression of caspase-3 was down-regulated, and the expression of Bcl-2 was up-regulated in the other three groups, the incidence of hypotension and bradycardia was significantly in-creased in group RD1. 0, the incidence of bradycardia was significantly decreased in group RD0. 5, and the incidence of hypotension and bradycardia was significantly increased, and the emergence time, extu-bation time and duration of PACU stay were prolonged in group RD2. 0 ( P＜0. 05). Compared with group RD0. 5, IL-1β content was significantly decreased, and the incidence of hypotension and bradycardia was increased in group RD1. 0, and IL-1β content was significantly decreased, the incidence of hypoten-sion and bradycardia was increased, and the emergence time, extubation time and duration of PACU stay were prolonged in group RD2. 0 ( P＜0. 05). Compared with group RD1. 0, the incidence of hypotension and bradycardia was significantly increased, and the emergence time, extubation time and duration of PACU stay were prolonged in group RD2. 0 ( P＜0. 05). There was no significant difference in the AI, expression of caspase-3 and Bcl-2, lung injury score, or requirement for rescue analgesia among RD0. 5, RD1. 0 and RD2. 0 groups ( P＞0. 05). Conclusion Dexmedetomidine 0. 5 μg∕kg mixed with ropiva-caine for TPVB combined with general anesthesia provides better efficacy in the patients undergoing radical resection of lung cancer.

Efficacy of dexmedetomidine mixed with ropivacaine for brachial plexus block in patients undergoing upper limb surgery: a meta-analysis / 中华麻醉学杂志

Objective To systematically review the efficacy of dexmedetomidine mixed with ropivacaine for brachial plexus block in the patients undergoing upper limb surgery.Methods Medline,PubMed,Embase,Web of Science,Weipu,Wanfang,Zhiwang databases were searched for randomized controlled trials involving the efficacy of dexmedetomidine mixed with ropivacaine for brachial plexus block in patients undergoing upper limb surgery from the date of database establishment up to July 2017,and the trials were published in Chinese or in English.Evaluation indexes included onset time and duration of sensory and motor blocks and analgesia time when used for brachial plexus block.Trials were selected and data were extracted independently by 2 investigators,and meta-analysis was conducted using the Cochrane Collaboration's RevMan 5.3 software.Results Twelve randomized controlled trials were included in our metaanalysis.Compared with control group,the onset time of sensory and motor blocks was significantly shortened,the duration of sensory and motor blocks was prolonged,and analgesia time when used for brachial plexus block was prolonged in dexmedetomidine group (P＜0.01).Conclusion Dexmedetomidine mixed with ropivacaine can be effectively used for brachial plexus block in the patients undergoing upper limb surgery.

Efficacy of transversus abdominis plane block with dexmedetomidine mixed with ropivacaine for postoperative analgesia in pediatric patients / 中华麻醉学杂志

Objective To evaluate the efficacy of transversus abdominis plane (TAP) block with dexmedetomidine mixed with ropivacaine for postoperative analgesia in pediatric patients.Methods Forty American Society of Anesthesiologists physical status Ⅰ or Ⅱ patients of both sexes,aged 1-4 yr,weighing 8-22 kg,scheduled for elective unilateral herniorrhaphy,were assigned into 2 groups (n=20 each) using a random number table method:ropivacaine group (group R) and dexmedetomidine mixed with ropivacaine group (group DR).TAP block was performed at the end of operation under ultrasound guidance,0.125％ ropivacaine 1 ml/kg was injected in group R and 0.075％ ropivacaine plus 1 μg/kg dexmedetomidine was injected in group DR.A dose of morphine 0.05 mg/kg was intravenously injected when Face Legs Activity Cry Consolability score ≥4.The duration of postoperative analgesia and consumption of morphine within 24 h after operation were recorded.The development of nausea and vomiting,bradycardia,hypotension,respiratory depression,over-sedation and TAP block-related complications (hematoma or infection at puncture site,peritoneal puncture,local anesthetic toxicity) within 24 h after operation were recorded.Results Compared with group R,the consumption of postoperative morphine within 24 h after operation was significantly reduced,and the duration of postoperative analgesia was prolonged in group DR (P ＜0.05).No hypotension,over-sedation or TAP block-related complications were found in two groups.There was no significant difference in the incidence of nausea and vomiting,respiratory depression or bradycardia after operation between two groups (P＞0.05).Conclusion Dexmedetomidine combined with ropivacaine provides better postoperative analgesic efficacy than ropivacaine alone when used for TAP block in pediatric patients.