ABSTRACT
A novel experimental model of free radical-induced emesis for screening anti-emetic compounds from natural sources was established. 2,2'-Azobis(2-amidinopropane) dihydrochloride (AAPH) dissolved in liposome induced emesis in young chickens, and the emesis was prevented by antioxidants including N-(2-mercaptopropionyl)-glycine (MPG), alpha-tocopherol, and L-ascorbic acid. Tropiseton, a serotonin receptor antagonist, also prevented emesis induced by AAPH. Known anti-emetic drugs and anti-emetic principles from natural sources also showed significant retching inhibition in the experiment using this system.
Subject(s)
Antiemetics/pharmacology , Antioxidants/pharmacology , Plants, Medicinal , Vomiting/prevention & control , Amidines , Animals , Antiemetics/isolation & purification , Chickens , Drug Evaluation, Preclinical/methods , Free Radicals , Liposomes , Male , Oxidants , Vomiting/chemically inducedABSTRACT
Bioassay-guided fractionation of anti-emetic extracts and constituents of 8 traditional Chinese herbal drugs was performed. Twenty extracts described in Table 1 showed anti-emetic activity on copper sulfate induced-emesis in young chicks. From the n-hexane extract of Pogostemon cablin, patchouli alcohol (1), pogostol (2), stigmast-4-en-3-one (3), retusin (4), and pachypodol (5) were tested and exhibited anti-emetic effects.
Subject(s)
Antiemetics/pharmacology , Drugs, Chinese Herbal/pharmacology , Animals , Chickens , Copper Sulfate/toxicity , MaleABSTRACT
The anticonvulsant effects of Shitei-To and its components on maximal electroshock seizures and chemical convulsions were examined. Shitei-To significantly prolonged the latency to bicuculline (2.0 mg/kg, s.c.)-induced clonic convulsions. Repeated treatment with Shitei-To also significantly prolonged the latency to strychnine (1.5 mg/kg, i.p.)- and pentylenetetrazol (90 mg/kg, i.p.)-induced clonic convulsions. On the other hand, Shitei-To had no effect on maximal electroshock seizures. Of the components of Shitei-To, Shitei had almost the same effect as Shitei-To against the clonic convulsions induced by the three chemical agents tested. These findings suggest that Shitei-To has anticonvulsant effects.
Subject(s)
Anticonvulsants/therapeutic use , Drugs, Chinese Herbal/therapeutic use , Seizures/drug therapy , Animals , Bicuculline , Convulsants , Electroshock , Male , Mice , Mice, Inbred Strains , Pentylenetetrazole , Seizures/chemically induced , StrychnineABSTRACT
Two novel diarylheptanoids named katsumadain A (1) and katsumadain B (2) were isolated from the seeds of Alpinia katsumadai, and their structures were determined by spectroscopic analysis. Both katsumadains A (1) and B (2) showed anti-emetic activities on copper sulfate-induced emesis in young chicks.
Subject(s)
Antiemetics/isolation & purification , Diarylheptanoids , Drugs, Chinese Herbal/isolation & purification , Pyrones/isolation & purification , Zingiberales/chemistry , Animals , Chickens , Models, Chemical , Seeds/chemistryABSTRACT
A crude globulin fraction was isolated from the tubers of Pinellia ternata (Thunb.) Breit. Tubers of P. ternata are one of the well known Chinese traditional medicines. It is used on account of its anti-emetic effect. 6KDP was separated by means of gel filtration and chromatography on CM-Toyopearl 650 M from the crude globulin fraction. 6KDP is a glycoprotein of M.W. 6 kDa. 6KDP has an anti-emetic activity and hemagglutination activity. Both activities dropped during heat treatment. For the purpose to evaluate the quality of the powdered tubers of P. ternata, the quantitative analysis by means of EIA was established. The contents of 6KDP varied from 5.75 to 8.30%. The assay demonstrated a low cross-reaction with the crude globulin fraction of Colocasia antiquorum, a member of the same family as P. ternata. 6KDP is one of major proteins in the tubers of P. ternata. Thus 6KDP is a marker for quantitative analysis of the tubers of P. ternata.
Subject(s)
Antiemetics/pharmacology , Plant Proteins/pharmacology , Plants, Medicinal/chemistry , Drugs, Chinese Herbal , Electrophoresis, Polyacrylamide Gel , Immunoenzyme Techniques , Medicine, Chinese Traditional , Plant Proteins/isolation & purificationABSTRACT
The structure of a new triterpene derivative isolated from Poria cocos was determined to be 3 beta-p-hydroxybenzoyldehydrotumulosic acid by spectral and chemical methods. 3 beta-p-hydroxybenzoyldehydrotumulosic acid showed marked inhibitory activity against 12-O-tetradecanoylphorbol-13-acetate (TPA)- and arachidonic acid (AA)-induced ear inflammation in mice. The 50% inhibitory doses of 3 beta-p-hydroxybenzoyldehydrotumulosic acid were 0.27 and 1.25 mg per ear on TPA- and AA-induced inflammation, respectively.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemistry , Plants, Medicinal , Triterpenes/chemistry , Animals , Anti-Inflammatory Agents, Non-Steroidal/isolation & purification , Arachidonic Acid , Female , Inflammation/chemically induced , Inflammation/drug therapy , Japan , Medicine, Chinese Traditional , Mice , Mice, Inbred ICR , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Tetradecanoylphorbol Acetate , Triterpenes/isolation & purification , Triterpenes/therapeutic useABSTRACT
Pachymic acid, 3-O-acetyl-16 alpha-hydroxytrametenolic acid, and poricoic acid B had been isolated from the sclerotium of Poria cocos Wolf. These compounds showed a strong inhibitory activity against 12-O-tetradecanoylphorbol-13-acetate-induced inflammation in mice. At 0.2 mumol/mouse, these compounds markedly inhibited the promoting effect of 12-O-tetradecanoylphorbol-13-acetate (1 microgram/mouse) on skin tumor formation following initiation with 7,12-dimethylbenz[a]anthracene (50 micrograms/mouse).
Subject(s)
Anticarcinogenic Agents/therapeutic use , Carcinogens , Plant Extracts/therapeutic use , Skin Neoplasms/chemically induced , Skin Neoplasms/prevention & control , Tetradecanoylphorbol Acetate , Triterpenes/therapeutic use , 9,10-Dimethyl-1,2-benzanthracene , Administration, Topical , Animals , Female , Mice , Mice, Inbred ICR , Time FactorsSubject(s)
Polychlorinated Biphenyls/poisoning , Animals , Blood/drug effects , Body Weight/drug effects , Liver/drug effects , Liver/pathology , Male , Microsomes, Liver/drug effects , Organ Size/drug effects , Pentobarbital/pharmacology , Polychlorinated Biphenyls/administration & dosage , Polychlorinated Biphenyls/metabolism , Rats , Sleep/drug effects , Tissue DistributionABSTRACT
Kanechlor (KC)-300, 400, 500, and 600 consisting of polychlorinated biphenyls (PCB) containing 43, 48, 55, and 61% chlorine respectively, were administered in a single dose of 100 mg/kg to mice and rats. The effect of PCB was investigated by determining pentobarbital sleeping time, liver microsomal hemoprotein contents, PCB level and gaschromatography (GC) pattern in tissue. Pentobarbital sleeping time was prolonged 2 to 4 times longer than that of control level after 3 to 4 hr of KC treatment in both ICR and ddN strain mice and KC-300 was the most effective. Forty-eight hr after treatment, however, this sleeping time was half that of the control. Sleeping time in ICR strain mice returned to control level 8 days after the treatment with KC-300 and KC-500, but the decrease in sleeping time continued in ddN mice. Conversely, the prolongation of sleeping time in rats was only 20% the control level at 3 hr after KC-300 treatment, but the shortening of sleeping time was more marked than in mice. Both the prolongation of sleeping time in mice treated with KC-300 and the shortening of sleeping time in rats treated wiht KC-500 were more rapidly effected when an oral dose rather than when a intraperitoneal one was given. Induction of liver microsomal cytochrome P-450 level was maximum in rats treated with KC-600 and increase of hemoprotein level and shortening of sleeping time were proportional to the chlorine content of PCB. The CO-difference spectrum of microsomes from rats treated with KC had an absorbance maximum at 448 nm. Direct relationship between storage of PCB in adipose tissue and the induced effect by KC has also been demonstrated in rats. PCB level in the liver of rats was higher for about 8 hr after KC-500 treatment given orally and was lower than the PCB level in adipose tissue after 8 hr. The GC-pattern of PCB stored in tissues was different from that of standard KC, indicating that all components were not metabolized at the same rate and that the components of the KC with the longer retention time were metabolized to a lesser degree than those with the shorter retention time.