A number of herbs belonging to the genus Jatropha of Euphorbiaceae family are noted for their medicinal benefits. The genus Jatropha is one of the prospective biodiesel yielding crops. The plants which have been so far explored include J. curcas, J. gossypifolia, J. glandulifera, J. multifida and J. podagrica. Although, the plants of this genus are widely distributed, there is an exiguity of scientific literature proclaiming the medicinal benefits of the plants belonging to genus Jatropha. The present paper is a pragmatic approach to accrue the findings on this very significant genus.
Analgesics ; pharmacology ; therapeutic use ; Animals ; Anthelmintics ; pharmacology ; therapeutic use ; Anti-Inflammatory Agents ; pharmacology ; therapeutic use ; Anticonvulsants ; pharmacology ; therapeutic use ; Antidiarrheals ; pharmacology ; therapeutic use ; Antineoplastic Agents, Phytogenic ; pharmacology ; therapeutic use ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Humans ; Hypoglycemic Agents ; pharmacology ; therapeutic use ; Jatropha ; chemistry ; classification

OBJECTIVETo study the anti-inflammatory and analgesic activities of diethyl 1,3-dicyclohexyl-1,2,3,6-tetrahydropyrimidine-4,5-dicarboxylate (ZL-5010) in vivo and in vitro.

METHODSThe analgesic effect of ZL-5010 was evaluated by acetic acid-induced writhing response in mice, and the anti-inflammatory effects was assessed in mice with xylene-induced ear edema and in rats with carrageenan-induced paw edema. Mouse peritoneal exudate cells activated by bacterial lipopolysaccharides (LPS) were used to evaluate the anti-inflammatory effect of ZL-5010 in vitro. The levels of interleukin-1β (IL -1β) and tumor necrosis factor-α (TNF-α) in the cell culture supernatant were measured using enzyme-linked immunosorbent assay (ELISA).

RESULTSAt the doses of 0.25 and 0.5 mmol/kg, ZL-5010 administered by gavage once daily for 3 days significantly reduced acetic acid-induced writhing frequency and suppressed xylene-induced ear edema in mice, and alleviated paw edema induced by carrageenan in rats (P<0.05). The agent also inhibited the production of the pro-inflammatory cytokines IL-1β and TNF-α by LPS-induced mouse peritoneal exudate cells in vitro, with the statistically significant minimum effective concentrations of 10 and 20 µmol/L, respectively (P<0.05).

CONCLUSIONZL-5010 administered by gavage has anti-inflammatory and analgesic effects in mice and rats, and in mouse peritoneal exudate cell cultures, the agent also inhibits the production of the pro-inflammatory cytokines IL-1β and TNF-α.

Amino Acids, Diamino ; pharmacology ; therapeutic use ; Analgesics ; pharmacology ; therapeutic use ; Animals ; Anti-Inflammatory Agents ; pharmacology ; therapeutic use ; Cyclohexanes ; pharmacology ; therapeutic use ; Female ; Interleukin-1beta ; metabolism ; Male ; Mice ; Mice, Inbred Strains ; Pyrimidines ; pharmacology ; therapeutic use ; Rats ; Rats, Sprague-Dawley ; Tumor Necrosis Factor-alpha ; metabolism

The present study was designed to isolate and characterize the analgesic compounds of Artemisa sacrorum Ledeb. The EtOAc crude extracts from the aerial parts of Artemisa sacrorum Ledeb were separated by chromatography and the structures of new compounds were elucidated based on spectral analyses. Analgesic activities of the isolated compounds were assessed in rats with hot plate test and paw pressure assay. Two new flavone C-glycosides, named as Sacroroside A and B (Compounds 1 and 2) were isolated from the EtOAc crude extract of the aerial parts ofArtemisa sacrorum Ledeb. They showed significant analgesic effects. In conclusion, Compounds 1 and 2 are new natural products, which show significant analgesic effects in a dose-dependent manner.
Analgesics ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Animals ; Artemisia ; chemistry ; Disaccharides ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Flavanones ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Flavones ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Hot Temperature ; Male ; Molecular Structure ; Pain ; drug therapy ; Phytotherapy ; Plant Components, Aerial ; Plant Extracts ; chemistry ; pharmacology ; therapeutic use ; Pressure ; Rats, Wistar

We examined the possible anti-inflammatory mechanisms of gabapentin in the attenuation of neuropathic pain and the interaction between the anti-allodynic effects of gabapentin and interleukin-10 (IL-10) expression in a rat model of neuropathic pain. The anti-allodynic effect of intrathecal gabapentin was examined over a 7-day period. The anti-allodynic effects of IL-10 was measured, and the effects of anti-IL-10 antibody on the gabapentin were assessed. On day 7, the concentrations of pro-inflammatory cytokines and IL-10 were measured. Gabapentin produced an anti-allodynic effect over the 7-day period, reducing the expression of pro-inflammatory cytokines but increasing the expression of IL-10 (TNF-alpha, 316.0 +/- 69.7 pg/mL vs 88.8 +/- 24.4 pg/mL; IL-1beta, 1,212.9 +/- 104.5 vs 577.4 +/- 97.1 pg/mL; IL-6, 254.0 +/- 64.8 pg/mL vs 125.5 +/- 44.1 pg/mL; IL-10, 532.1 +/- 78.7 pg/mL vs 918.9 +/- 63.1 pg/mL). The suppressive effect of gabapentin on pro-inflammatory cytokine expression was partially blocked by the anti-IL-10 antibody. Expression of pro-inflammatory cytokines was significantly attenuated by daily injections of IL-10. The anti-allodynic effects of gabapentin may be caused by upregulation of IL-10 expression in the spinal cord, which leads to inhibition of the expression of pro-inflammatory cytokines in the spinal cords.
Amines/pharmacology/*therapeutic use ; Analgesics/pharmacology/*therapeutic use ; Animals ; Antibodies/immunology/pharmacology ; Behavior, Animal/drug effects ; Cyclohexanecarboxylic Acids/pharmacology/*therapeutic use ; Cytokines/*metabolism ; Disease Models, Animal ; Injections, Spinal ; Interleukin-10/genetics/immunology/*metabolism ; Male ; Neuralgia/*drug therapy/metabolism/pathology ; Rats ; Rats, Sprague-Dawley ; Recombinant Proteins/biosynthesis/genetics/pharmacology ; Spinal Cord/metabolism ; Up-Regulation ; gamma-Aminobutyric Acid/pharmacology/*therapeutic use

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*

OBJECTIVETo evaluate the analgesic, anti-inflammatory and antipyretic activity of methanolic Tecomaria capensis (T. capensis) leaves extract using different models in rats.

METHODSMethanolic T. capensis leaves extract (100, 300, 1000 and 2000 mg/kg body weight) was given to rats orally to observe acute toxicity, and observed for 14 days. Analgesic activity was evaluated using tail immersion and formalin induced paw licking models in rats. Anti-inflammatory activity was evaluated using carrageenan induced paw edema model in rats. Antipyretic activity was evaluated using brewer's yeast induced pyrexia model in rats. Methanolic T. capensis leaves extract were given at dose of 100, 200 and 500 mg/kg p.o.

RESULTSResults demonstrated that the no mortality was reported even after 14 days. This indicated that the methanol extract was safe up to a single dose of 2 000 mg/kg body weight. Methanolic T. capensis leaves extract (100, 200 and 500 mg/kg p.o.) significantly increased the latency period in the tail immersion test, reduced the licking time in both the neurogenic and inflammatory phases in the formalin test. Methanolic T. capensis leaves extract (100, 200 and 500 mg/kg p.o.) significantly prevented increase in volume of paw edema. Methanolic T. capensis leaves extract at the doses of (100, 200 and 500 mg/kg p.o.) significantly decreased the rectal temperature of the rats.

CONCLUSIONSThis study exhibites that methanolic T. capensis leaves extract possesses analgesic, anti-inflammatory and antipyretic activity which may be mediated by the central and peripheral mechanisms.

Analgesics ; chemistry ; pharmacology ; therapeutic use ; toxicity ; Animals ; Anti-Inflammatory Agents ; chemistry ; pharmacology ; therapeutic use ; toxicity ; Antipyretics ; chemistry ; pharmacology ; therapeutic use ; toxicity ; Behavior, Animal ; drug effects ; Bignoniaceae ; chemistry ; Disease Models, Animal ; Edema ; Female ; Fever ; Male ; Pain Management ; methods ; Pain Measurement ; Plant Extracts ; chemistry ; pharmacology ; therapeutic use ; toxicity ; Plant Leaves ; chemistry ; Rats

OBJECTIVETo study the analgesic effects and sites of oxymatrine-carbenoxolone sodium complex (OCSC).

METHODAdopting formalin test, warm water tail-flick test and intracerebroventricularly (icv) injection to observe the analgesic effects of OCSC in mice.

RESULTIntraperitoneally injecting (ip) OCSC (75, 150 mg x kg(-1)) remarkedly inhibited the pain of mice in the formalin test and prolonged latent phases of tail-shrinking of mice, icy OCSC (1.875, 3.75, 7.5 mg x kg(-1)) significantly prolonged latent phases of tail-shrinking of mice, it had dose-dependent effect with concentration.

CONCLUSIONThe result indicated that OCSC has obvious analgesic effects and its mechanism may be involved in central nervous system (CNS).

Alkaloids ; chemistry ; Analgesics ; administration & dosage ; chemistry ; pharmacology ; therapeutic use ; Animals ; Carbenoxolone ; administration & dosage ; chemistry ; pharmacology ; therapeutic use ; Dose-Response Relationship, Drug ; Female ; Male ; Mice ; Mice, Inbred ICR ; Pain ; drug therapy ; Quinolizines ; chemistry

OBJECTIVETo discuss the optimum extraction process of compound Nanxing pain-relieving cataplasm through orthogonal design and pharmacodynamic experiment

METHODThe orthogonal experiment method was adopted to optimize the ethanol extraction process with Angelica dahurica, Ligusticum chuanxiong and other herbs. The anti-inflammatory and analgesic effects of extracts from volatile oil in such herbs as syzygium aromaticum with different extraction processes were compared by tail pain tenderness test and food-pad swelling in mice, in order to optimize the extraction process of extracts from volatile oil in such herbs as syzygium aromaticum.

RESULTThe optimum extraction process of A. dahurica, L. chuanxiong and other herbs for compound Nanxing pain-relieving cataplasm were as follows: adding 8-fold amount of 70% alcohol, extracting for 2 times with 1.5 h each time. The 95% ethnol extracts of syzygium aromaticum and other herbs had more effect in the increasing the threshold of pain and the inhibition of toe swelling of mice than volatile oil obtained from steam distillation as well as volatile oil and water decoction obtained from steam distillation.

CONCLUSIONThe method is simple and reliable that it can provide technical reference for the development of modern preparations of compound Nanxing pain-relieving cataplasm.

Analgesics ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Animals ; Chemical Fractionation ; methods ; Chemistry, Pharmaceutical ; methods ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Ethanol ; chemistry ; Mice ; Oils, Volatile ; chemistry ; Pain ; drug therapy

OBJECTIVETo establish the processing method of fructus evodiae and its standard for quality control, toxicity aspects and pharmacodynamics were carried out at the same time.

METHODIn the studies of processing techniques, the optimized technical parameters were determined by the contents of evodiamine and evodine. And the acute toxicity and pharmacodynamics were studied by rats.

RESULTThe process was that the liquorice-processed fructus evodiae was wetted by liquorice decoction by sixth of raw fructus evodiae (V/W) and fried below 230 degrees C. The method of detecting the contents of evodiamine and evodine was that Alltima ODS C18 (4.6 mm x 250 mm, 5 microm); mobile phase acetonitrile-water-tetrahydrofuran-phosphoric acid (51:48: 1: 0.05); column temperature 25 degrees C; mobile rate 0.8 mL x min(-1); wave length 225 nm. The toxicity experimentation show that rats didnt show any notable changes after affused the raw material and the processed fructus evodiae's decotion 40 g x kg(-1) b. w. at one time seven days constantly. The analgesic effect was observed after 0.6 g (material) x kg(-1) (weight) b. w.

CONCLUSIONThe toxicity of the raw material and the processed one were low and the liquorice-processed fructus evodia analgesic effect was good.

Analgesics ; isolation & purification ; pharmacology ; therapeutic use ; toxicity ; Animals ; Chromatography ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; therapeutic use ; toxicity ; Female ; Glycyrrhiza ; chemistry ; Linear Models ; Male ; Mice ; Mice, Inbred ICR ; Pain ; drug therapy ; Reproducibility of Results ; Rutaceae ; chemistry ; Temperature

Pain is one of the common clinical symptom, previous studies have implicated sodium channels as a key constituent in pain signaling. Sodium channel blockers with efficient sodium channel blockade effect play an important role in analgesic treatment. However, most drugs used in clinic have many drawbacks and can not meet the demand of the clinical use. Therefore, for the development of new generation of sodium channel blockers, it is of great significance to find small molecule sodium channel blocking lead compounds with novel chemical scaffolds and new structures, sodium channel blocking activity and structure-activity relationship are discussed in detail, and current problems and trends in future research are also emphasized.
Analgesics ; chemistry ; pharmacology ; therapeutic use ; Animals ; Drug Design ; Humans ; Molecular Structure ; Neuralgia ; drug therapy ; Pain ; drug therapy ; Pain Measurement ; Sodium Channel Blockers ; chemistry ; pharmacology ; therapeutic use ; Sodium Channels ; drug effects ; Structure-Activity Relationship