Immediate analgesic effect of electroacupuncture combined with diclofenac sodium on acute gouty arthritis: a randomized controlled trial / 中国针灸

OBJECTIVE@#To observe the immediate analgesic effect of electroacupuncture (EA) combined with diclofenac sodium on acute gouty arthritis (AGA).@*METHODS@#A total of 90 patients with AGA were randomly divided into a low-dose medication (LM) group (30 cases, 1 case was eliminated, 1 case dropped off), a conventional medication (CM) group (30 cases, 1 case dropped off) and a combination of acupuncture and medication (AM) group (30 cases ). The LM group was given oral administration of 50 mg diclofenac sodium sustained-release capsule; the CM group was given oral administration of 100 mg diclofenac sodium sustained-release capsule; on the basis of the treatment of LM group, the AM group was treated with electroacupuncture at ashi points, Dadu (SP 2), Taichong (LR 3), Taibai (SP 3), Neiting (ST 44), Sanyinjiao (SP 6), Zusanli (ST 36) and Yinlingquan (SP 9) on the affected side, and Taichong (LR 3) and Zusanli (ST 36), Sanyinjiao (SP 6) and Yinlingquan (SP 9) were connected to electroacupuncture respectively, continuous wave, 2 Hz in frequency. The visual analogue scale (VAS) scores of pain before treatment and after 10 min, 2 h, 4 h and 6 h of treatment completion, joint tenderness and swelling scores before treatment and after 10 min and 6 h of treatment completion were compared, and the rate of diclofenac sodium addition within 24 h after treatment completion was recorded among the three groups.@*RESULTS@#After 10 min of treatment completion, the scores of VAS, joint tenderness and joint swelling in the AM group were lower than those before treatment (P<0.05), and the VAS score in the AM group was lower than that in the other two groups (P<0.05). After 2, 4 and 6 h of treatment completion, the VAS scores of the three groups were lower than those before treatment (P<0.05), and the scores in the AM group were lower than those in the LM group (P<0.05). After 6 h of treatment completion, the joint tenderness scores of the three groups and the joint swelling scores of the AM group and the CM group were lower than those before treatment (P<0.05), and the joint tenderness and swelling scores of the AM group were lower than those of the LM group (P<0.05). The rate of diclofenac sodium addition was 3.3 % (1/30) and 3.4 % (1/29) in the AM group and the CM group, respectively, which were lower than 17.9% (5/28) in the LM group (P<0.05).@*CONCLUSION@#Electroacupuncture combined with diclofenac sodium have a good immediate analgesic effect in the treatment of AGA, and have the advantages of small dosage of analgesic drugs and less adverse reactions.

Advances in medicinal research on tetrodotoxin / 药学实践杂志

Tetrodotoxin (TTX) is a neurotoxin found in puffer fish and other marine organisms. It has been used as an inhibitor of voltage-gated sodium channels (VGSCs), which could selectively bind to the α-subunit on the outer vestibule of VGSCs, preventing sodium ions from entering the channel, resulting in pharmacological activities. As a typical sodium channel blocker, TTX shows a significant analgesic effect. TTX could selectively block Na+ channels without affecting other ion channels, therefore it could reduce the probability of adverse reactions caused by commonly used antiarrhythmic drugs. In addition, TTX has a significant role in detoxification and prevention of renal failure, so TTX has great potential as a medicine. The structure and physicochemical properties, mechanism of action, pharmacological activities and preparations of tetrodotoxin have been reviewed in this paper, so as to provide a general support for the evaluation of its druggability and application in the field of pharmacy.

Efficacy and safety of ropivacaine combined with alfentanil for analgesia after knee arthroscopic surgery / 中国药房

OBJECTIVE To explore the efficacy and safety of intra-articular injection of ropivacaine combined with alfentanil for postoperative analgesia in patients who underwent knee arthroscopic surgery. METHODS A total of 60 patients who underwent knee arthroscopic surgery were collected from the Central Hospital of Enshi Tujia and Miao Autonomous Prefecture from March to September in 2022， and then divided into trial group and control group with random number table method， with 30 cases in each group. The control group received intra-articular injection of 0.25% ropivacaine 50 mg， and the trial group received intra-articular injection of 0.25% ropivacaine 50 mg+alfentanil 0.15 μg/kg.The first postoperative remedial analgesia time， the total amount of postoperative remedial drugs， numerical rating scale at rest （NRS-R） scores， numerical rating scale at movement （NRS-M） scores， heart rate， mean arterial blood pressure， and pulse oxygen saturation during exercise at different monitoring time points after surgery， the incidence of adverse drug reactions such as hypotension， respiratory depression， nausea， and vomiting after surgery were compared between 2 groups. RESULTS Compared with the control group， the first postoperative remedial analgesia time was significantly longer in the trial group， and the total amount of postoperative remedial drugs was significantly reduced （P＜0.001）. The trial group had lower NRS-R and NRS-M scores at each monitoring time point， with statistically significant differences （P＜0.001）， and there was an interactive effect between time and groups （P＜0.001）. The changes in heart rate， mean arterial blood pressure， and pulse oxygen saturation of patients in the trial group were relatively small， with no statistically significant differences （P＞0.05）， and there was no interactive effect between time and groups （P＞0.05）. There was no statistical significance in the incidence of adverse drug reactions between 2 groups， such as postoperative hypotension， respiratory depression， nausea， vomiting （P＞0.05）. CONCLUSIONS The intra- articular injection of ropivacaine combined with alfentanil shows good efficacy and safety for post-knee arthroscopic analgesia， and significantly prolongs the analgesic duration of ropivacaine.

Comparative study on analgesic effect of tetrodotoxin in four acute pain models / 药学实践杂志

Objective To evaluate the analgesic effect of tetrodotoxin (TTX) in four types of acute pain models and provide experimental support for its rational application. Methods Mice or rats were intramuscularly pretreated with morphine (1 mg/kg) or TTX (0, 0.5, 1, 2, 4 and 8 μg/kg) 40 min before acetic acid writhing test, formalin stimulation test, hot plate test or tail flick test. Pain response or pain threshold were recorded, and inhibition rate was calculated during the tests. The arachidonic acid of serum was determined by Elisa. Results Significant analgesic effects were observed with morphine in all four acute pain models. TTX dose-dependently reduced the number of writhing induced by acetic acid and inhibited the pain response induced by formalin during phase I and phase II, with the highest inhibition rate of more than 80.00% in two pain models. TTX showed analgesic effect in tail flick test and hot plate test, with the highest inhibition rate of 25.00% and 19.79%, respectively. Both acetic acid and formalin increased arachidonic acid in animal serum, but TTX had no significant inhibitory effect on the releasing of arachidonic acid. Conclusion TTX showed significant analgesic effect in the chemical stimulation pain models induced by acetic acid and formalin, but limited analgesic effect was observed on the physical stimulation pain model induced by heat (hot plate and hot water). TTX may produce analgesic effect by blocking the inflammatory mediators mediating pain response.

Quantitative Electrophysiological Evaluation of the Analgesic Efficacy of Two Lappaconitine Derivatives: A Window into Antinociceptive Drug Mechanisms / 神经科学通报·英文版

Quantitative evaluation of analgesic efficacy improves understanding of the antinociceptive mechanisms of new analgesics and provides important guidance for their development. Lappaconitine (LA), a potent analgesic drug extracted from the root of natural Aconitum species, has been clinically used for years because of its effective analgesic and non-addictive properties. However, being limited to ethological experiments, previous studies have mainly investigated the analgesic effect of LA at the behavioral level, and the associated antinociceptive mechanisms are still unclear. In this study, electrocorticogram (ECoG) technology was used to investigate the analgesic effects of two homologous derivatives of LA, Lappaconitine hydrobromide (LAH) and Lappaconitine trifluoroacetate (LAF), on Sprague-Dawley rats subjected to nociceptive laser stimuli, and to further explore their antinociceptive mechanisms. We found that both LAH and LAF were effective in reducing pain, as manifested in the remarkable reduction of nocifensive behaviors and laser-evoked potentials (LEPs) amplitudes (N2 and P2 waves, and gamma-band oscillations), and significantly prolonged latencies of the LEP-N2/P2. These changes in LEPs reflect the similar antinociceptive mechanism of LAF and LAH, i.e., inhibition of the fast signaling pathways. In addition, there were no changes in the auditory-evoked potential (AEP-N1 component) before and after LAF or LAH treatment, suggesting that neither drug had a central anesthetic effect. Importantly, compared with LAH, LAF was superior in its effects on the magnitudes of gamma-band oscillations and the resting-state spectra, which may be associated with their differences in the octanol/water partition coefficient, degree of dissociation, toxicity, and glycine receptor regulation. Altogether, jointly applying nociceptive laser stimuli and ECoG recordings in rats, we provide solid neural evidence for the analgesic efficacy and antinociceptive mechanisms of derivatives of LA.

Analgesic efficacy of dexmedetomidine combined with fentanyl citrate injection in patients undergoing laparoscopic appendectomy and its effects on inflammatory factor level / 中国基层医药

Objective:To investigate the analgesic efficacy of dexmedetomidine combined with fentanyl citrate injection in patients undergoing laparoscopic appendectomy and its effects on inflammatory factor level.Methods:200 patients with appendicitis who underwent laparoscopic appendectomy in Hangzhou Dajiangdong Hospital from April 2017 to March 2019 were included in this study. They were randomly assigned to receive postoperative anesthesia either with fentanyl citrate injection alone (control group, n = 100) or fentanyl citrate injection combined with dexmedetomidine (observation group, n = 100). At different time points after surgery, Visual Analogue Scale (VAS) score was compared between the two groups. Inflammatory factors C-reactive protein, interleukin-6, and tumor necrosis factor-α levels before and after surgery, and the incidence of adverse reactions were compared between the two groups. Results:At 6, 12, 24 and 48 hours after surgery, VAS score in the observation group was significantly lower than that in the control group ( t = 4.671, 9.594, 10.877 and 12.358, all P < 0.001). Before surgery, there were significant differences in C-reactive protein, interleukin-6, and tumor necrosis factor-α levels between the two groups ( t = 0.224, 0.188, 0.421, all P > 0.05). At 24 hours after surgery, C-reactive protein, interleukin-6, and tumor necrosis factor-α levels in each group were significantly increased compared with before surgery, and C-reactive protein, interleukin-6, and tumor necrosis factor-α levels in the observation group were significantly lower than those in the control group ( t = 2.496, 2.209, 3.165, all P < 0.05). There was no significant difference in the incidence of adverse reactions between the control and observation groups [8.00% (8/100) vs. 10.00% (10/100), χ2 = 0.244, P > 0.05]. Conclusion:Dexmedetomidine combined with fentanyl citrate injection exhibits good and anesthesic and analgesic effects during laparoscopic appendectomy, helps inhibit the expression of inflammatory factors, reduces the level of inflammatory factors, leads to less adverse reactions, and is highly safe.

Quantitative Electrophysiological Evaluation of the Analgesic Efficacy of Two Lappaconitine Derivatives: A Window into Antinociceptive Drug Mechanisms / 神经科学通报·英文版

Quantitative evaluation of analgesic efficacy improves understanding of the antinociceptive mechanisms of new analgesics and provides important guidance for their development. Lappaconitine (LA), a potent analgesic drug extracted from the root of natural Aconitum species, has been clinically used for years because of its effective analgesic and non-addictive properties. However, being limited to ethological experiments, previous studies have mainly investigated the analgesic effect of LA at the behavioral level, and the associated antinociceptive mechanisms are still unclear. In this study, electrocorticogram (ECoG) technology was used to investigate the analgesic effects of two homologous derivatives of LA, Lappaconitine hydrobromide (LAH) and Lappaconitine trifluoroacetate (LAF), on Sprague-Dawley rats subjected to nociceptive laser stimuli, and to further explore their antinociceptive mechanisms. We found that both LAH and LAF were effective in reducing pain, as manifested in the remarkable reduction of nocifensive behaviors and laser-evoked potentials (LEPs) amplitudes (N2 and P2 waves, and gamma-band oscillations), and significantly prolonged latencies of the LEP-N2/P2. These changes in LEPs reflect the similar antinociceptive mechanism of LAF and LAH, i.e., inhibition of the fast signaling pathways. In addition, there were no changes in the auditory-evoked potential (AEP-N1 component) before and after LAF or LAH treatment, suggesting that neither drug had a central anesthetic effect. Importantly, compared with LAH, LAF was superior in its effects on the magnitudes of gamma-band oscillations and the resting-state spectra, which may be associated with their differences in the octanol/water partition coefficient, degree of dissociation, toxicity, and glycine receptor regulation. Altogether, jointly applying nociceptive laser stimuli and ECoG recordings in rats, we provide solid neural evidence for the analgesic efficacy and antinociceptive mechanisms of derivatives of LA.

Analgesic and neuromotor effects of two extracts of Zanthoxylum rhoifolium (Rutaceae) in the Swiss albino mouse (Mus musculus) / Efectos analgésicos y neuromotores de dos extractos de Zanthoxylum rhoifolium (Rutaceae) en el ratón albino suizo (Mus musculus)

Background: Colombia has a high diversity of medicinal plants, including Tachuelo (Zanthoxylum rhoifolium), a tree belonging to the family Rutaceae, which has been attributed an analgesic use by communities of the Colombian southwest. Nevertheless, this species has been scarce studied in Colombia. The studies have been limited to the isolation of compounds with antifungal and insecticide activity, using the leaves, branches, and bark of the plant in aqueous, and organic extracts. Neither pharmacological tests have been carried out, nor the analgesic and neuromotor activity have been tested from preparations with this plant's fruits. Objectives: To evaluate the analgesic and neuromotor effect of the aqueous and hexane extract of the fruits of Z. rhoifolium.Methods: As there were no preliminary reports of this study, the first observation was made through Irwin's test. The formalin and the rotarod test were performed to determine the analgesic and motor coordination effects, respectively. Results: All the evaluated treatments demonstrated to generate analgesia, anesthesia, passivity, reduction in the alarm reaction, and have antinociceptive activity in the formalin test; while only the high dose of the nonpolar extract generated a deficit in the motor performance of the rodents in the rotarod test. Conclusions: the antinociceptive effect of the aqueous and hexane extracts of this species' fruits was demonstrated. The hexane extract generated a neuromotor effect, which validates the ethnobotanical reports on Z. rhoifolium fruits.

Antecedentes: Colombia tiene una alta diversidad de plantas medicinales, incluyendo al Ta chuelo (Zanthoxylum rhoifolium), un árbol de la familia Rutaceae al que se le ha atribuido un potencial analgésico debido al uso por parte de las comunidades del Suroccidente Colombiano. Sin embargo, esta especie ha sido poco estudiada en Colombia, limitándose al aislamiento de compuestos con actividad antifúngica e insecticida, empleando las hojas, ramas y corteza de la planta en extractos acuosos y orgánicos; sin embargo, no se han realizado ensayos farmacológicos ni se han probado la actividad analgésica y neuromotora a partir de preparaciones con los frutos de esta planta. Objetivos: Evaluar el efecto analgésico y neuromotor del extracto acuoso y en hexano de los frutos de Z. rhoifolium. Métodos: Al no haber reportes preliminares de este estudio, se realizó la primera observación mediante el test de Irwin. Para determinar el efecto analgésico y neuromotor se realizó el test de formalina y el test de rotarod, respectivamente. Resultados: Todos los tratamientos evaluados demostraron generar analgesia, anestesia, pasividad, reducción en la reacción de alarma, tener actividad antinociceptiva en el test de formalina, mientras que solo la dosis alta del extracto apolar generó un déficit en el rendimiento motor de los roedores en el test de rotarod. Conclusiones: Se demostró el efecto antinociceptivo del extracto acuoso y en hexano de los frutos de esta especie y el efecto neuromotor generado por el extracto en hexano, validando los reportes etnobotánicos sobre los frutos de Z. rhoifolium.

Efecto analgésico del bloqueo PENG (grupo de nervios pericapsulares) en pacientes con fractura de cadera / Analgesic effect of the PENG BLOCK (pericapsular nervous group) in patients with hip fracture

Ultrasound regional blockade emerged that blocks the branches of the femoral nerve, obturator and accessory obturator that innervate the anterior hip capsule, the PENG block (group of pericapsular nerves), which by its Recent description does not have enough evidence in medical practice. To verify the analgesic effect of the PENG block in patients with hip fracture and its analgesic permanence during the first 10 hours after the block in patients admitted with a diagnosis of hip fracture, at the General Interzonal Hospital of Acute "Dr Oscar E Alende "From Mar del Plata, Argentina, in the months of May to November 2019. A prospective descriptive observational study was carried out with a total of 53 patients, hospitalized patients with a diagnosis of hip fracture, with standardized intravenous analgesic scheme and who have not yet undergone hip surgery. Pain was evaluated with the EVA scale (visual analog scale) prior to the blockage, and then at 30 min and 10 hours after the blockade, 15 ml of 1% lidocaine and 15 ml of bupivacaine at 0 were used. 25%, convex or linear ultrasound probe according to patient weight and 100 mm needle. In order to reproduce and evaluate the pain, the patients had a 30º flexion of the hip. Prior to the blockade, 66% of the patients had severe pain and 34% moderate pain, none presented mild pain or absence, both at thirty minutes and ten hours after the blockade, no patient presented severe pain and all patients presented analgesia with a decrease in more than three points on the VAS scale, in some cases reaching a decrease of 10 points on that scale. The PENG block is a regional anesthesia technique that provides very good analgesia to patients with hip fractures, therefore, it is an excellent saving strategy for systemic analgesics. Knowing the analgesia provided by the blockade at 30 min and at 10 h, it could be performed both in the preoperative period for the transfer and mobilization of the patient, as well as in the postoperative period, which could save the use of opioids and decrease hospital stay.

INTRODUCCIÓN La fractura de cadera es una emergencia ortopédica común en ancianos asociada a gran morbimortalidad, una adecuada analgesia regional perioperatoria determina un ahorro en el uso de analgésicos sistémicos. Recientemente, en el año 2018, surgió un nuevo bloqueo regional ecoguiado muy prometedor que bloquea las ramas del nervio femoral, obturador y obturador accesorio que inervan la capsula anterior de la cadera, el bloqueo PENG (grupo de nervios pericapsulares), el cual por su reciente descripción no cuenta con la suficiente evidencia en la práctica médica. OBJETIVOS: Comprobar el efecto analgésico del bloqueo PENG en pacientes con fractura de cadera y su permanencia analgésica durante las 10 primeras horas posteriores al bloqueo en los pacientes internados con diagnóstico de fractura de cadera, en el Hospital Interzonal General de Agudos "Dr. Oscar E Alende" de Mar del Plata, Argentina, en los meses de mayo a noviembre del 2019. MATERIALES Y MÉTODOS: Se realizó un estudio observacional descriptivo prospectivo con un total de 53 pacientes, se incluyeron pacientes internados con diagnóstico de fractura de cadera, con esquema analgésico endovenoso estandarizado y que aún no hayan sido sometido a cirugía de cadera. Se evaluó el dolor con la escala EVA (escala análoga visual) previo al bloqueo, y luego a los 30 min y a las 10 Hs de haber realizado el bloqueo, para este se utilizaron 15 ml lidocaína 1% y 15 ml de bupivacaína al 0,25%, sonda ecográfica convexa o lineal según el peso del paciente y aguja 100 mm. Para reproducir y evaluar el dolor se les realizo a los pacientes una flexión de 30º de la cadera. RESULTADOS: Previo al bloqueo el 66% de los pacientes tuvieron dolor severo y 34% dolor moderado, ninguno presentaba dolor leve o ausencia del mismo, tanto a los treinta minutos como a las diez horas posteriores al bloqueo ningún paciente presento dolor severo y todos los pacientes presentaron analgesia con una disminución en más de tres puntos en la escala de EVA, llegando en algunos casos a una disminución de 10 puntos de dicha escala. CONCLUSIONES: El bloqueo PENG es una técnica de anestesia regional que brinda muy buena analgesia a los pacientes con fractura de cadera, por consiguiente, es una excelente estrategia ahorradora de analgésicos sistémicos. Conociendo la analgesia que brinda el bloqueo a los 30 min y a las 10 h de realizado, se podría realizar dicho bloqueo tanto en el preoperatorio para el traslado y movilización del paciente, como en el post-operatorio, lo que podría ahorrar el uso de opioides y disminuir la estancia hospitalaria.

Including preparation of cinnamon oil by vinyl pyrrolidone/vinyl acetate copolymer VA64-Soluplus spray-dried microspheres / 中草药

Objective: To investigate the applicability of the spray-dried microspheres of vinyl pyrrolidone/vinyl acetate copolymer VA64-Soluplus for inclusion of cinnamon oil (CO) and compare with traditional inclusion technology of β-cyclodextrin. Methods: HPLC was used to determine the encapsulation rate of inclusion complex. Transmission electron microscopy (TEM), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRD) were used to characterize the inclusion complex; The dissolution and stability of the inclusion complex was investigated by in vitro release test and accelerated stability test; The pharmacokinetic and analgesic efficacy tests were used to examine the bioavailability and efficacy of the inclusion complex. Results: The encapsulation rate of microsphere inclusion complex and β-cyclodextrin inclusion complex was (98.38 ± 0.30)% and (86.51 ± 0.52)%, respectively. Observation of the inclusion complex under TEM showed a uniform spherical-like structure with uniform dispersion; Observation under SEM showed that the inclusion complex was spherical with a concave surface; The endothermic peak of volatile oil of cinnamon in DSC and the diffraction peak in XRD disappeared. The cinnamon volatile oil was dispersed in theinclusion complex in the form of non-aggregation; The cumulative release rates of cinnamon volatile oil, microsphere inclusion complex and β-cyclodextrin inclusion complex in in vitro dissolution experiments were 97.05%, 93.36% and 80.26%, respectively; Accelerated stability test at 60 ℃ showed that the loss rate of volatile oil of microsphere inclusion complex was significantly lower than that of cinnamon volatile oil and β-cyclodextrin inclusion complex; Pharmacokinetics showed that the AUC0-∞ of cinnamon essential oil, microsphere inclusion complex and β-cyclodextrin inclusion complex were basically the same; Pharmacodynamics showed that the analgesic rates of cinnamon volatile oil in the three groups were 53.0%, 47.5% and 21.1%, respectively. Conclusion: The stability of cinnamon volatile oil was enhanced by the combination of spray-dried microspheres of vinyl pyrrolidone/vinyl acetate copolymer VA64-Soluplus. The in vitro release, bioavailability and analgesic efficacy of microsphere were basically consistent with the volatile oil of cinnamon volatile oil, and it was superior to the inclusion compound of β-cyclodextrin. The vinyl pyrrolidone/vinyl acetate copolymer VA64-Soluplus microsphere inclusion compound had better water solubility. This study provides a new method for the inclusion of volatile oil.

Research progress on biological activities and mechanism of betulinic acid and their derivatives / 中草药

Betulinic acid is a natural pentacyclic pentane triterpenoid, usually isolated from the bark of Betula platyphylla, or in the form of free glycosides and glycosyl derivatives in various plants. A variety of derivatives can be obtained by modifying its chemical structure. Betulinic acid and its derivatives have certain regulatory effects in anti-tumor, antiviral, anti-inflammatory, analgesic, inhibition of cerebral nerve and vascular injury, and treatment of other common diseases. The category, pharmacological activities and related mechanisms of betulinic acid and its derivatives are reviewed in this paper, in order to provide a theoretical reference for the future application.

Study on Analgesic Effect of 4 Sources of Curcumae Radix Decoction Pieces and Comparison of Curcuminol Content in Its Water Extracts / 中国药房

OBJECTIVE：To study the analgesic effects of 4 sources of Curcumae Radix decoction pieces （Curcuma wenyujin ， C. kwangsiensis ，C. phaeocaulis and C. longa ），and compare the contents of curcumenol in their water extracts. METHODS ： Using aspirin as positive control ，acetic acid writhing method was used to investigate the effects of 4 sources of Curcumae Radix decoction pieces water extract on writhing latency and times of writhing in mice. The moisture contents of 4 sources of Curcumae Radix decoction pieces （10 batches of each source ，the same below ）were determined according to the drying method in 2015 edition of Chinese Pharmacopoeia （part Ⅳ）. The yield of water extract in 4 sources of Curcumae Radix decoction pieces were investigated by hot dipping method ，the contents of curcumenol in water extract of 4 sources of Curcumae Radix decoction pieces were determined by HPLC ，and comparison was conducted. RESULTS ：Compared with model group ，aspirin and water extracts of 4 sources of Curcumae Radix decoction pieces could significantly prolong the writhing latency of model mice ，and the water extracts of C. wenyujin and C. phaeocaulis could significantly reduce the writhing times of model mice （P＜0.05 or P＜0.01）. For C. wenyujin ，C. kwangsiensis ，C. phaeocaulis and C. longa ，the contents of moisture were 7.39％-8.80％，7.88％-9.88％，7.66％- 10.5468/ogs.2019.62.6.382 9.86％ and 7.68％-10.20％；the average yield of water extract were 46.30％，60.40％，38.65％，42.99％；the average contents of curcumenol in water extract were 0.271，0.066，0.310，0.058 mg/g. Except for a few batches ，the higher the yield of water extract，the higher the content of curcuminol in the same source of Curcumae Radix decoction pieces. CONCLUSIONS ：Four sources of Curcumae Radix decoction pieces have analgesic effect. The contents of curcumenol in C. wenyujin and C. phaeocaulis were similar ，and the contents of curcumenol in C. kwangsiensis and C. longa about 1/5 of that in C. phaeocaulis and C. wenyujin .

Analgesic effects of aspirin combined with kv7 channel openers / 中国药理学通报

Aim To provide scientific evidence for clinical drug combination by exploring the analgesic effect of aspirin combined with Kv7 channel openers, retigabine and flupirtine. Methods The mice were randomly divided into control group, aspirin group, flupirtine group, retigabine group, aspirin + flupirtine group and aspirin + retigabine group. To assess the antinociceptive effects of each group, the acetic acid-induced abdominal constriction test and the hot-plate test were used. Results In the acetic acid-induced abdominal constriction test, compared to aspirin group, the amount of abdominal constriction in aspirin + flupirtine group was significantly reduced (P <0.01). The latent period of abdominal constriction in aspirin + retigabine group was significantly prolonged ( P < 0. 01) and the number of abdominal constriction was significantly reduced (P < 0. 01). In the hot-plate test, compared to aspirin group, the increment percentage of latent period in aspirin + flupirtine group and aspirin + retigabine group showed an increased trend. Among them, the increment percentage of latent period 30 and 60 minutes after injections in aspirin + retigabine group had a significant difference from that in aspirin group (P <0. 05). Conclusion Kv7 channel openers, retigabine and flupirtine, can enhance the analgesic effect of aspirin.

Analgesic effects of soluble epoxide hydrolase inhibitor in K/BxN serum transfer arthritis mouse model

BACKGROUND: Soluble epoxide hydrolase (sEH) is an enzyme that converts epoxyeicosatrienoic acid (EET) into the anti-inflammatory dihydroxyeicosatrienoic acids (DHET). Inhibition of sEH by the potent soluble epoxide hydrolase inhibitor (sEHI) decreases inflammation by increasing EET. The K/BxN serum transfer mouse model of arthritis displays an initial inflammation and an associated tactile allodynia that continues on following the resolution of inflammation. METHODS: We undertook the following studies: i) Using the K/BxN mouse model, we examined effects on allodynia during the early inflammatory phase of administration of sEHI 3 mg/kg and/or diclofenac (DFC) 10 mg/kg. ii) In the late inflammatory phase, we administered sEHI (3, 10, or 30 mg/kg); DFC 10 mg/kg; gabapentin 100 mg/kg. iii) Using the conditioned place preference (CPP) we examined the synergism between sEHI and DFC in the K/BxN mouse using the CPP paradigm. The drug was administered intraperitoneally and the allodynia was measured with the von Frey test. RESULTS: In the early phase, both sEHI and DFC displayed an antiallodynic action. In the late phase, sEHI, and gabapentin but not DFC were effective in reversing the allodynia. Comparable results were observed with the CPP. CONCLUSIONS: This study demonstrates that sEHI reduces mechanical allodynia in both the early and the late inflammatory K/BxN mouse model of arthritis. The sEHI target thus addresses the hyperalgesia arising from inflammation as well as the post-inflammatory phase that has been said to reflect neuropathic-like states, thus presenting alternatives to the limited efficacy of arthritis drugs in use.

Investigation of Analgesic Mechanisms of Bupleuri Radix with Network Pharmacology / 中国药学杂志

OBJECTIVE: To analyze the major analgesic mechanism and target of Bupleuri Radix with a network pharmacology method, clarify the difference targets between oral administration and injection administration, and validate the possible biological target for its quality evaluation. METHODS: The chemical components and potential targets of Bupleuri Radix were collected based on the database and literature searching and the analgesic associated targets were searched from Genecards database. All of the targets combined with interactional proteins from DIP database were used to construct a “compound-target-disease” network and the major analgesic mechanism of Bupleuri Radix were then predicted by the key function targets screened from it. RESULTS: According to the results of network analysis, 13 key targets were screened out, including trypsin-1, prothrombin, dipeptidyl peptidase 4, acetylcholinesterase, COX-2, androgen receptor, estrogen receptor, GABA receptor α1 and NOS-3, which might affect the process of cell proliferation, arginine catabolic process, platelet activation and so on. Trypsinogen-1, cyclooxygenase-2 and nitric oxide synthase-3 were the main targets for both of them, and could be used as the targets for biological evaluation of Bupleuri Radix. At the same time, there were some differences between oral administration and injection of Bupleuri Radix, the excessive effects of injection components on prothrombin may be associated with the adverse reactions of injection. Otherwise, inhibition of COX-2 enzyme activity by in vitro testing showed that Bupleuri Radix has good activity at the concentration of 3.125-50 μg•mL-1. CONCLUSION: Network pharmacology provides the potential to predict the analgesic mechanism and to establish new quality evaluation METHODS of Bupleuri Radix.

Research progress on pharmacological effect of Artemisiae Scopariae Herba / 中草药

The main chemical components of Artemisiae Scopariae Herba (ASH) include coumarins, flavonoids, organic acids, essential oils, and so on. Except for the traditional actions of clearing and draining dampness-heat, and disinhibiting gallbladder and anti-icteric, ASH has multiple pharmacological activities, such as antipyretic, analgesic, anti-inflammatory, antiviral, antitumor, hypotensive, hypolipidemic, anti-osteoporotic, neuroprotective, metabolic regulation effects, as well as prevention of Alzheimer’s disease, whose mechanism of actions are complex. This article reviews pharmacological actions and the corresponding mechanism of ASH, which can provide reference for the research, development and clinical application of ASH and its preparations.

Effect of scutellarein on acute pharyngitis in rats / 中国药科大学学报

@#In order to investigate the therapeutic effects of scutellarein on acute pharyngitis, 60 rats were randomly divided into five groups: blank group, model group, low-dose scutellarein group, high-dose scutellarein group and positive drug group. HE staining, blood-cell-analyzer, IL-6, IL-1β and TNF-α ELISA kit were used to study the effects of scutellarein on acute pharyngitis in pharyngeal tissue morphology, the counts of white blood cells and neutrophil and the serum concentrations of TNF-α, IL-1β and IL-6. Meanwhile, forty mice were randomly divided into four groups: blank group, low-dose scutellarein group, high-dose scutellarein group and positive drug group. Then, hot plate and writhing test of mice were carried out to study the analgesic effects of scutellarein. Results showed that, compared to the model group, scutellarein improved the physical status of acute pharyngitis rats, reduced the number of white blood cells significantly(P< 0. 05)and decreased the number of neutrophils and the levels of TNF-α, IL-1β and IL-6 in rats serum significantly(P< 0. 01). Meanwhile, scutellarein dramatically improved the pain threshold in hot plate test and decreased the number of writhing mice(P< 0. 01). It can be concluded that scutellarein can be used to treat acute pharyngitis with its anti-inflammatory and analgesic effect.

Research progress on chemical constituents and biological activities from Turpinia species / 中国中药杂志

Turpinia species have been used as local Chinese medicines. It has been widely concerned about their antibacterial and anti-inflammatory effects. Modern studies showed that the chemical constituents of Turpina species include flavonoids, triterpenoids, megastigans and phenoli acids. Its pharmacological research mainly focused on antibacterial, anti-inflammatory, antioxidant, analgesic, and immuneregulation effect. In this paper, the chemical compositions and pharmacological activities of Turpinia species were summarized, in order to provide scientific basis for the further development and utilization of Turpinia species.

Efficacy of local infiltration of ropivacaine combined with multimodal analgesia with parecoxib for perioperative analgesia in patients undergoing pancreaticoduodenectomy / 南方医科大学学报

OBJECTIVE@#To explore the effect of local infiltration of ropivacaine combined with multimodal analgesia with parecoxib for perioperative pain management in patients undergoing pancreaticoduodenectomy.@*METHODS@#This randomized controlled trial was conducted among 98 patients undergoing pancreaticoduodenectomy in the Department of Biliary Surgery of West China Hospital between March, 2017 and August, 2018. The patients were randomized to receive perioperative analgesia with local infiltration anesthesia with ropivacaine combined with multimodal analgesia with parecoxib (experimental group, =50) or postoperative analgesia with dizosin (control group, =48). The regimens for intraoperative anesthesia and postoperative pain relief were identical in the two groups. The differences in NRS pain score, use of pain relief agents, the incidences of adverse reactions to analgesia and wound infection, and the time to first ambulation and first flatus passage after the operation were compared between the two groups.@*RESULTS@#At 12, 24 h, 48 h, 72 h and 7 days after the operation, the patients in the experimental group had significantly lower NRS scores ( < 0.05) than those in the control group. The rate of use of rescue analgesics was significantly lower in the experimental group than in the control group (32% 66.67%, < 0.05); the rate of tramadol hydrochloride use was also significantly lower in the experimental group ( < 0.05). Compared with those in the control group, the patients in the experimental group showed a significantly lower total incidence of adverse reactions (22% 54.17%, < 0.05) as well as a lower incidence of nausea and vomiting ( < 0.05), an earlier time of first ambulation and first flatus passage after the operation ( < 0.05), and a shorter postoperative hospital stay ( < 0.05).@*CONCLUSIONS@#In patients undergoing pancreaticoduodenectomy, local infiltration of ropivacaine combined with multimodal analgesia with ropivacaine can effectively relieve perioperative pain, reduce the use of relief analgesics, lower the incidence of adverse reactions, and promote the recovery after the surgery.

Effect of cinobufagin on transient outward potassium current in dorsal root ganglion cells of rats with cancer-induced bone pain / 南方医科大学学报

OBJECTIVE@#To observe the effect of cinobufagin on transient outward potassium current () in rat dorsal root ganglion cells of cancer-induced bone pain (CIBP) and explore the possible analgesic mechanism of cinobufagin.@*METHODS@#Whole cell patch clamp technique was used to examine the effect of cionbufagin on in acutely isolated dorsal root ganglion (DRG) cells from normal SD rats and rats with bone cancer pain.@*RESULTS@#The DRG cells from rats with CIBP showed obviously decreased current density, an activation curve shift to the right, and an inactivation curve shift to the left. Cinobufagin treatment significantly increased the current density and reversed the changes in the activation and inactivation curves in the DRG cells.@*CONCLUSIONS@# current is decreased in DRG neurons from rats with CIBP. Cinobufagin can regulate the activation and inactivation of current in the DRG cells, which may be related to its analgesic mechanism.