This study investigated the chemical constituents of Rhododendri Mollis Flos. The n-butanol fraction of 95% ethanol extract of Rhododendri Mollis Flos was separated and purified using chromatographic techniques, including normal-phase silica gel, ODS, and Sephadex LH-20 column chromatography. The structures of the isolated compounds were identified by spectroscopic techniques. Seven compounds were isolated and identified as rhodomollein LXⅦ(1), rhodomollein X(2), nivalenol(3),(3S,6S)-cis-linalool-3,7-oxide-β-D-glucopyranoside(4), thymidine(5), cyclo(Ala-Tyr)(6), and(S)-5-hydroxypyrrolidin-2-one(7). Among them, compound 1 was identified as a new compound, and compound 3 was isolated from this plant for the first time. The analgesic activity of compound 1 was evaluated using the acetic acid-induced writhing test. At a dose of 5.0 mg·kg~(-1), compound 1 showed a 75.4% inhibition rate in the writhing test, indicating significant analgesic activity.
Drugs, Chinese Herbal/isolation & purification* ; Rhododendron/chemistry* ; Animals ; Flowers/chemistry* ; Mice ; Male ; Analgesics/isolation & purification* ; Molecular Structure

Two new sesquiterpenes, trivially named ricinusoids A (1) and ricinusoids B (2), were isolated from ethyl acetate fraction of Ricinus communis. The structures of new compounds were elucidated by detailed spectroscopic techniques, including 1D- and 2D-NMR, UV, IR spectroscopy, and mass spectrometry. The compounds (1-2) were also assessed for in-vivo sedative and analgesic like effects in open field and acetic acid induced writhing tests respectively at 5, 10, and 20 mg·kg i.p. Pretreatment of both test compounds caused significant (P ≤ 0.05) reduction in locomotive activity like sedative agents and abdominal constrictions like analgesics. Both compounds (1-2) possessed marked sedative and antinociceptive effects in animal models.
Analgesics ; administration & dosage ; chemistry ; isolation & purification ; Animals ; Humans ; Hypnotics and Sedatives ; administration & dosage ; chemistry ; isolation & purification ; Locomotion ; drug effects ; Male ; Mice ; Mice, Inbred BALB C ; Molecular Structure ; Pain ; drug therapy ; physiopathology ; Plant Extracts ; administration & dosage ; chemistry ; isolation & purification ; Plant Leaves ; chemistry ; Ricinus ; chemistry ; Sesquiterpenes ; administration & dosage ; chemistry ; isolation & purification

The present study was designed to search for compounds with analgesic activity from the Schizophyllum commune (SC), which is widely consumed as edible and medicinal mushroom world. Thin layer chromatography (TLC), tosilica gel column chromatography, sephadex LH 20, and reverse-phase high performance liquid chromatography (RP-HPLC) were used to isolate and purify compounds from SC. Structural analysis of the isolated compounds was based on nuclear magnetic resonance (NMR). The effects of these compounds on voltage-gated sodium (NaV) channels were evaluated using patch clamp. The analgesic activity of these compounds was tested in two types of mouse pain models induced by noxious chemicals. Five phenolic acids identified from SC extracts in the present study included vanillic acid, m-hydroxybenzoic acid, o-hydroxybenzeneacetic acid, 3-hydroxy-5-methybenzoic acid, and p-hydroxybenzoic acid. They inhibited the activity of both tetrodotoxin-resistant (TTX-r) and tetrodotoxin-sensitive (TTX-s) NaV channels. All the compounds showed low selectivity on NaV channel subtypes. After intraperitoneal injection, three compounds of these compounds exerted analgesic activity in mice. In conclusion, phenolic acids identified in SC demonstrated analgesic activity, facilitating the mechanistic studies of SC in the treatment of neurasthenia.
Analgesics ; administration & dosage ; chemistry ; isolation & purification ; Animals ; Humans ; Hydroxybenzoates ; administration & dosage ; chemistry ; isolation & purification ; Mice ; Neurasthenia ; drug therapy ; genetics ; metabolism ; Schizophyllum ; chemistry ; Voltage-Gated Sodium Channel Blockers ; administration & dosage ; chemistry ; isolation & purification ; Voltage-Gated Sodium Channels ; genetics ; 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

OBJECTIVETo investigate analgesic, antidiarrhoeal and cytotoxic activities of the ethanol extract of Passiflora foetida L. (Passifloraceae) by three experimental methods.

METHODSAnalgesic activity of the ethanol extract of Passiflora foetida L. (EEPF) acetic acid-induced writhing inhibition in mice. The method of castor oil-induced diarrhoea in mice was utilized to evaluate antidiarrhoeal activity. The cytotoxic activity of EEPF was explored with a brine shrimp lethality bioassay.

RESULTSThe extract showed 68.75% and 30.00% inhibition of writhe at the doses of 500 and 250 mg/kg body weight, respectively. The extract increased the mean latent period prior to diarrhoeal onset to about 1.55 h and 1.17 h, and decreased the mean number of stools to 4.4 and 5.6 at the doses of 500 and 250 mg/kg body weight. The extract also demonstrated cytotoxic activity in the brine shrimp lethality assay, and the median lethal concentration for brine shrimp nauplii was 80 μg/mL.

CONCLUSIONThe results suggest that the plant extract has analgesic and antidiarrhoeal activities, supporting its uses in traditional medicine. The results also demonstrate that the plant extract possesses cytotoxic activities.

Analgesics ; isolation & purification ; pharmacology ; Animals ; Antidiarrheals ; pharmacology ; Diarrhea ; chemically induced ; drug therapy ; Dose-Response Relationship, Drug ; Female ; Male ; Mice ; Pain ; drug therapy ; Passiflora ; chemistry ; Phytotherapy ; adverse effects ; methods ; Plant Extracts ; isolation & purification ; pharmacology ; toxicity

We investigated the anti-nociceptive effect of Excoecaria agallocha (E.agallocha) against chemically and thermally induced nociception, Albino mice received a dose of 10, 15, 20, or 25 mg/kg of alkaline chloroform fraction (Alk-CF) of E.agallocha by oral administration. Compared with controls, Alk-CF decreased the writhing numbers (P<0.01) in a dose dependent manner. Further we determined that, Alk-CF contained, a potent compared to control, also potent anti-nociceptive agent that acted via opioid receptors and using HPLC, identified this compound as Rutin. Docking simulation demonstrated that Rutin interacted strongly with cyclooxygenase, forming a number of specific hydrogen bonds. In conclusion we have identified peripheral and central anti-nociceptive activities of E.agallocha that involve opioid receptor, and in which the active compound is Rutin.
Analgesics ; isolation & purification ; therapeutic use ; Animals ; Drug Evaluation, Preclinical ; Euphorbiaceae ; chemistry ; Female ; Male ; Mice ; Pain ; drug therapy ; Phytotherapy ; Plant Extracts ; chemistry ; therapeutic use ; Rutin ; isolation & purification ; therapeutic use

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 investigate the chemical constituents from Lamiophlomis rotata and the bioactivities of 8-epideoxyloganic acid.

METHODThe constituents were isolated by using a combination of various chromatographic techniques including column chromatography over ployamide, silica gel and Sephadex LH-20. Structures of the isolates were identified by spectroscopic data analysis. Bioactivities were screened by using models in vivo.

RESULTFive constituents were isolated. 8-epideoxyloganic acid was isolated for the first time in L. rotata and also in lamioplomis genus. 8-epideoxyloganic acid could significantly inhibit aectic acid-induced twisting times and slower the time of homeostatsis, also inhibit xylene-induced ear edema in mice.

CONCLUSION8-epideoxyloganic acid possesses bioactivities of analgesia, homeostasis and anti-inflammatory.

Analgesics ; pharmacology ; Animals ; Anti-Inflammatory Agents ; pharmacology ; Female ; Lamiaceae ; chemistry ; Male ; Mice ; Pyrans ; isolation & purification ; pharmacology

The technology of liquid fermentation for producing the recombinant analgesic peptide BmK AngM1 from Buthus martensii Karsch in Pichia pastoris was studied by single-factor and orthogonal test. The results showed that the optimal culture conditions were as follows: 1.2% methanol, 0.6% casamino acids, initial pH 6.0, and three times of basal inoculation volume. Under the above culture conditions, the expression level of recombinant BmK AngM1 in Pichia pastoris was above 500 mg x L(-1), which was more than three times of the control. The study has laid a foundation for the large-scale preparation of BmK AngM1 to meet the needs of theoretical research of BmK AngM1 and development of new medicines.
Amino Acids ; pharmacology ; Analgesics ; isolation & purification ; metabolism ; Animals ; Fermentation ; Gene Expression ; Hydrogen-Ion Concentration ; Methanol ; pharmacology ; Peptides ; isolation & purification ; metabolism ; Pichia ; genetics ; metabolism ; Recombinant Proteins ; genetics ; metabolism ; Scorpion Venoms ; genetics ; isolation & purification ; metabolism ; Scorpions ; chemistry

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