OBJECTIVE: To investigate the effect of dexmedetomidine combined with pulmonary protective ventilation against lung injury in patients undergoing surgeries for esophageal cancer with one-lung ventilation (OLV). METHODS: Forty patients with undergoing surgery for esophageal cancer with OLV were randomly divided into pulmonary protective ventilation strategy group (F group) and dexmedetomidine combined with protective ventilation strategy group (DF group; =20). In F group, lung protective ventilation strategy during anesthesia was adopte, and in DF group, the patients received intravenous infusion of dexmedetomidine hydrochloride (0.3 μg · kg ·h) during the surgery starting at 10 min before anesthesia induction in addition to protective ventilation strategy. Brachial artery blood was sampled before ventilation (T), at 30 and 90 min after the start of OLV (T and T, respectively) and at the end of the surgery (T) for analysis of superoxide dismutase (SOD), malondialdehyde (MDA), tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), arterial oxygenation pressure (PaO), oxygenation index (OI) and lung compliance (CL). RESULTS: At the time points of T, T and T, SOD level was significantly higher and IL-6 level was significantly lower in the DF group than in F group ( < 0.05). The patients in DF group showed significantly higher PaO, OI and CL index than those in F group at all the 3 time points. CONCLUSIONS Dexmedetomidine combined with pulmonary protective ventilation strategy can reduce perioperative lung injury in patients undergoing surgery for esophageal cancer with OLV by suppressing inflammation and oxidative stress to improve lung function and reduce adverse effects of the surgery.
Analgesics, Non-Narcotic ; pharmacology ; therapeutic use ; Dexmedetomidine ; pharmacology ; therapeutic use ; Esophageal Neoplasms ; drug therapy ; surgery ; Humans ; Lung ; drug effects ; surgery ; One-Lung Ventilation ; Oxidative Stress ; drug effects ; Treatment Outcome

OBJECTIVE: To evaluate the effect of dexmedetomidine combined with ropivacaine on brachial plexus block in patients scheduled for elective shoulder arthroscopy. METHODS: Ninety patients with American Society of Anesthesiologists (ASA) I or II, scheduled for elective shoulder arthroscopy, were randomly divided into three groups. In group R (n=30), the patients were given 10 mL of 0.375% ropivacaine in branchial plexus block (interscalene approach guided by ultrasound), in group D1 (n=30), the patients were given 10 mL of 0.375% ropivacaine (interscalene approach guided by ultrasound) + dexmedetomidine 0.2 μg/(kg×h) (intravenous pump infusion), and in group D2 (n=30), the patients were given 10 mL of 0.375% ropivacaine (interscalene approach guided by ultrasound) + dexedetomidine 0.7 μg/(kg×h) (intravenous pump infusion). To evaluate the effect of brachial plexus block before general anesthesia. Group D1 and group D2 were given dexmedetomidine intravenously for 1.0 μg/kg during 10 min, then the drug was pumped by 0.2 μg/(kg×h) and 0.7 μg/(kg×h) respectively until 30 min before the operation finished. Changes in systolic blood pressure (SBP), diastolic blood pressure (DBP), heart rate (HR), and before anesthesia (T0), 10 min (T1), 30 min (T2) after giving dexmedetomidine, discontinue medication (T3), after operation (T4), and extubation (T5) were investigated. Motor and sensory block onset times, block durations, and duration of analgesia were recorded. The scores of pain after operation and the adverse effects of shiver, hypopiesia, drowsiness, and blood loss were recorded during operation. RESULTS: Compared with group R, the duration of analgesia and duration of sensory block in group D1 and group D2 were significant longer (P<0.01), there was no significant difference between groups D1 and D2 (P>0.05). Compared with group R, at each time point of T1-T5, the heart rate and systolic blood pressure in group D1 and group D2 were significantly decreased (P<0.01). Compared with D1 group, the incidence of hypotension and bradycardia in group D2 were significantly different (P<0.05). CONCLUSION Intravenous dexmedetomidine could prolong the duration of analgesia time and sensory block within the brachial plexus block, inhibiting the stress response during arthroscopic shoulder surgery. Compared with high-dose, low-dose can provide safer and better clinical effect and reduce the adverse effects of dexmedetomidine.
Analgesics, Non-Narcotic ; Anesthetics, Local/therapeutic use* ; Arthroscopy ; Brachial Plexus ; Brachial Plexus Block ; Dexmedetomidine/therapeutic use* ; Double-Blind Method ; Humans ; Hypnotics and Sedatives/pharmacology* ; Prospective Studies ; Ropivacaine/therapeutic use* ; Shoulder Joint/surgery*

To explore novel non-opioid analgesic agents, 16 compounds were synthesized and their structures were confirmed by 1H NMR and HR-MS. YX0611-1 was treated as the leading compound. The results of mice writhing model and hot plate model showed that compounds 2, 7, 8, 9, 11 and 15 had obvious analgesic activities in vivo. The test of affinity to mu, delta, kappa receptor displayed that active compounds didn't act on opioid receptor. The results of preliminary toxicity and pharmacokinetic tests showed that compound 7 had better safety and pharmacokinetic properties than that of YX0611-1, and it deserved further development.
Analgesics, Non-Narcotic ; chemical synthesis ; chemistry ; pharmacokinetics ; pharmacology ; toxicity ; Animals ; Female ; Male ; Mice ; Pain Measurement ; Piperazines ; chemical synthesis ; chemistry ; pharmacokinetics ; pharmacology ; toxicity ; Random Allocation ; Receptors, Opioid ; metabolism ; Structure-Activity Relationship

A series of aralkyl-ketone-4-piperidol derivatives were synthesized and tested for their analgesic activities. All of the novel 30 compounds were prepared from 4-piperidone and alpha-halo-aralkyl-ketone through five steps, including Boc protection, nucleophilic addition in presence of CeCl3/NaI catalyst, deprotection, condensation and salification. Their structures were confirmed by 1H NMR and HRMS. Preliminary in vivo pharmacological trials showed that most of the synthesized compounds revealed analgesic effects. Among the tested compounds, 8, 13 and 22 exhibited potent analgesic activities in both mice writhing and mice hot plate model. The three compounds have low affinity for mu, delta, kappa receptors, which is a chance to find a better precursor of non-opioid analgesic for further optimization.
Analgesics, Non-Narcotic ; chemical synthesis ; chemistry ; pharmacology ; Animals ; Mice ; Molecular Structure ; Pain Measurement ; Pain Threshold ; drug effects ; Piperidones ; chemical synthesis ; chemistry ; pharmacology ; Receptors, Opioid, delta ; metabolism ; Receptors, Opioid, kappa ; metabolism ; Receptors, Opioid, mu ; metabolism ; Structure-Activity Relationship

Aconitine ; analogs & derivatives ; pharmacology ; Analgesics, Non-Narcotic ; pharmacology ; Animals ; Female ; Intestine, Small ; physiology ; Male ; Mice ; Muscle Contraction ; drug effects ; Muscle, Smooth ; physiology ; Rabbits

The purpose of this study is to evaluate the interaction effects of In-Chen-How (Artemisia capillaries Thunb.) on the pharmacokinetics of acetaminophen and on liver microsomal cytochrome P450 enzyme activity in rats. The rats were divided into control group (n = 8) without In-Chen-How and the pretreated group (n = 8) administered with In-Chen-How (approximately 1.0 mL x kg(-1), according to weight) for 5 consecutive days. Rats in the control group received water simultaneously. Each rat was then given acetaminophen. The pharmacokinetic parameters of acetaminophen of the two groups were significantly different. In the In-Chen-How pretreated group, the maximum concentration of acetaminophen and the area under the plasma concentration-time curve were reduced about 58.4%, 56.7% and 55.4%. To further explain the results, liver microsomal suspensions were obtained from rats that were randomly divided into control and In-Chen-How pretreated group. The levels of CYP1A2 and CYP2E1 in hepatic microsomal protein from pretreated group were increased as compared to that from the control group. It indicated that In-Chen-How can stimulate the activity of CYP isozymes. The changes in the pharmacokinetics of acetaminophen resulting from the administration of In-Chen-How are related to an increase in metabolic activity of CYP1A2 and CYP2E1.
Acetaminophen ; administration & dosage ; blood ; pharmacokinetics ; Administration, Oral ; Analgesics, Non-Narcotic ; administration & dosage ; blood ; pharmacokinetics ; Animals ; Area Under Curve ; Artemisia ; chemistry ; Aryl Hydrocarbon Hydroxylases ; metabolism ; Cytochrome P-450 CYP1A2 ; metabolism ; Cytochrome P-450 CYP2E1 ; metabolism ; Drug Interactions ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Immunoblotting ; Male ; Metabolic Clearance Rate ; drug effects ; Microsomes, Liver ; drug effects ; enzymology ; Plants, Medicinal ; chemistry ; Random Allocation ; Rats ; Rats, Wistar

OBJECTIVETo investigate the regulatory effects of nerve growth factor (NGF) on basal and capsaicin-induced release of neuropeptide substance P (SP) in primary cultured embryonic rat dorsal root ganglion (DRG) neurons.

METHODSDRGs were dissected from 15-day-old embryonic Wistar rats. DRG neurons were dissociated and cultured, and then exposed to different concentrations of NGF (10 ng/mL, 30 ng/mL, or 100 ng/mL) for 72 h. The neurons cultured in media without NGF served as control. RT-PCR were used for detecting the mRNAs of SP and vanilloid receptor 1 (VR1) in the DRG neurons. The SP basal and capsaicin (100 nmol/L)-induced release in the culture were measured by radioimmunoassay (RIA).

RESULTSSP mRNA and VR1 mRNA expression increased in primary cultured DRG neurons in a dose-dependent manner of NGF. Both basal release and capsaicin-evoked release of SP increased in NGF-treated DRG neurons compared with in control group. The capsaicin-evoked release of SP also increased in a dose-dependent manner of NGF.

CONCLUSIONNGF may promote both basal release and capsaicin-evoked release of SP. NGF might increase the sensitivity of nociceptors by increasing the SP mRNA or VR1 mRNA.

Analgesics, Non-Narcotic ; pharmacology ; Animals ; Capsaicin ; pharmacology ; Cells, Cultured ; Dose-Response Relationship, Drug ; Embryo, Mammalian ; Ganglia, Spinal ; cytology ; Gene Expression Regulation ; drug effects ; Nerve Growth Factor ; pharmacology ; Neurons ; drug effects ; RNA, Messenger ; metabolism ; Radioimmunoassay ; methods ; Rats ; Rats, Wistar ; Substance P ; genetics ; metabolism

OBJECTIVETo investigate the changes of the activity of both protein kinase A and C and the mechanisms of antipyretic action of Guizhi decoction.

METHODThe fever responses were observed after combination injection of H-89 (a selective inhibitor of PKA) and calphostin C (a selective inhibitor of PKC), and oral pretreatment of Guizhi decoction in fever rats induced by an intra-cerebroventricular (icv) injection of an EP3 agonist, and both PKA and PKC activity in hypothalamus were measured in rats pretreated with Guizhi decoction and vehicle using isotopic tracing assay.

RESULTThe rise in rat body temperature was inhibited by H-89, Calphostin C, and Guizhi decoction, moreover, pretreatment with Guizhi decoction reduced PKA activity obviously. PKC activity in model rats exhibited a tendency to drop compared with that of control group, Oral administration of Guizhi decoction in large dose inhibited the response significantly, while the low dose of Guzhi decoction has no effect on PKC.

CONCLUSIONBoth PKA and PKC may participate in the mechanism of fever induction by EP3 agonist. The decrease of PKA and PKC may contribute to the antipyretic action of Guizhi decoction, some isoenzyme of PKC may play a role in the fever production.

Analgesics, Non-Narcotic ; pharmacology ; Animals ; Cinnamomum aromaticum ; chemistry ; Cyclic AMP-Dependent Protein Kinases ; metabolism ; Dinoprostone ; analogs & derivatives ; Dose-Response Relationship, Drug ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; pharmacology ; Fever ; chemically induced ; enzymology ; Hypothalamus ; enzymology ; Male ; Plants, Medicinal ; chemistry ; Protein Kinase C ; metabolism ; Random Allocation ; Rats ; Rats, Wistar ; Receptors, Prostaglandin E ; agonists ; Receptors, Prostaglandin E, EP3 Subtype

OBJECTIVETo study the analgesic, antipyretic and anti-inflammatory effect of Bailian Caogen granule.

METHODThe antipyretic effects of Bailian Caogen granule was evaluated in rabbit fever model induced by peptone. The analgesic effect of the drug was studied with pain model of mice induced by acetic acid and hot plate, The severity of oedema in inflamed animal was observed to study the anti-inflammatory effects of Bailian Caogen granule.

RESULTBailian Caogen granule could obviously inhibit the fever of rabbits. The number of writhing induced by acetic acid was reduced and the pain threshold of mice was increased by Bailian Caogen granule. Bailian Caogen granule also had anti-inflammatory activity against xylene-induced mouse ear swelling and carrageenin-induced rat paw edema.

CONCLUSIONBailian Caogen granule has significant analgesic, antipyretic and anti-inflammatory activities.

Acetic Acid ; Analgesics, Non-Narcotic ; pharmacology ; Animals ; Body Temperature ; drug effects ; Coptis ; chemistry ; Drug Combinations ; Drugs, Chinese Herbal ; pharmacology ; Edema ; pathology ; prevention & control ; Female ; Fever ; physiopathology ; prevention & control ; Glycyrrhiza uralensis ; chemistry ; Hot Temperature ; Hyperalgesia ; etiology ; physiopathology ; prevention & control ; Male ; Mice ; Pain ; chemically induced ; physiopathology ; prevention & control ; Pain Threshold ; drug effects ; Phellodendron ; chemistry ; Plants, Medicinal ; chemistry ; Pueraria ; chemistry ; Rabbits ; Random Allocation ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo clarify the resource of medicinal plants of genus Polygonum s. lat. distributed in Anhui Province.

METHODConducting field investigation and consulting related specimens and data.

RESULT AND CONCLUSIONThe distribution, growing environment and medicinal use of 32 taxa have been clarified. A scientific basis for further study for these medicinal plants has been provided.

Analgesics, Non-Narcotic ; pharmacology ; Antidiuretic Agents ; pharmacology ; China ; Conservation of Natural Resources ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Ecosystem ; Pharmacognosy ; Plants, Medicinal ; anatomy & histology ; chemistry ; classification ; Polygonum ; anatomy & histology ; chemistry ; classification