摘要:

AbstractThe pharmacological effects of synthetic butylidenephthalide (Bdph), the most potent antispasmodic agent found in the neutral oil ofLigusticum wallichiiFranch., were examined in this study.In vivo, Bdph exerted a significant antihypertensive effect in anaesthetized renal hypertensive rats at a dose of 30 mg/kg (i.v. or i.p.), or 60 mg/kg (p.o.). Bdph antagonized noradrenaline (NA) induced increases in blood pressure in anaesthetized normotensive rats. In addition, Bdph prevented the pituitrin‐induced T‐wave lowering of the ECG in anaesthetized rats. It also dose‐dependently decreased coronary arterial pressure in dogs. It is concluded that Bdph dilates coronary vessels.In vitro, Bdph non‐competitively antagonized adrenaline‐induced contraction in isolated rabbit aortic strips. It also significantly antagonized the NA‐induced maximum decrease in perfusion rate of isolated rabbit ears. However, the vasodilator effect may cause a heat loss because Bdph significantly lowered the rectal temperature of rats at ambient temperature of 20°C, but not at 30°C. Bdph might be a useful coronary dilator and antihype

ISSN:0951-418X    

DOI:10.1002/ptr.2650080602

出版商:John Wiley&Sons, Ltd.    

年代:1994

数据来源: WILEY

摘要:

AbstractAn antitumour‐promoting activity in two‐stage carcinogenesis, is found in the methanol extract of the Carthami Flos (Carthamus tinctoriusL.; Compositae), which is a traditional Chinese medicine and natural pigment of rouge additivies in certain Asian countries. From these active fractions, δ5‐ and δ7‐sterol fractions were separated. The separation was examined for inhibitory activity against TPA‐induced inflammatory ear oedema in mice. Stigmasterol (71% in the mixture) was the most abundant of 14 sterols identified in the δ5‐sterol fraction. Schottenol (70% in the mixture) constituted the dominant sterol of the δ7‐sterol fraction. Furthermore, stigmasterol markedly inhibited tumour promotion in two‐stage carcino

ISSN:0951-418X    

DOI:10.1002/ptr.2650080603

出版商:John Wiley&Sons, Ltd.    

年代:1994

数据来源: WILEY

摘要:

AbstractAlpha‐terthienyl (αT), a thiophene compound isolated fromTagetes patula(Asteraceae), exhibits antifungal activity towards five strains of dermatophytes (Trichophyton mentagrophytes, T. rubrum, T. violaceum, Epidermophyton floccosum, Microsporum cookei). αT plus UVA irradiation for 90 min acted as a fungistatic at concentrations between 6 μM and 24 μM. Between 1 and 10 days after irradiation, the fungal growth was reduced or arrested with marked responses forT. mentagrophytes, T. rubrumandM. cookei. The ultrastructural events that occur inTrichophyton mentagrophytesafter treatment were studied by electron microscopy. In the dark, αT caused no important ultrastructural modifications within the hyphae. After UVA irradiation the photoactive compound caused damage to membranes of the nucleus, mitochondria and endoplasmic reticulum. Plasmolytic and autolytic changes resulted in plasma membrane breakage and in cell wall aberrations. UVA‐activated αT would appear to target protein‐rich membranes of the de

ISSN:0951-418X    

DOI:10.1002/ptr.2650080604

出版商:John Wiley&Sons, Ltd.    

年代:1994

数据来源: WILEY

摘要:

AbstractA polysaccharide active fraction (AF) obtained from a hot‐water extract ofSalviae miltiorrhizaeradix was found to reduce urinary protein excretion in rats with aminonucleoside‐induced experimental nephrosis. Its composition was determined as 20% neutral sugars and 80% uronic acids. Oral or intramuscular administration of AF to the rats with aminonucleoside‐induced nephrosis resulted in a significant decrease of urinary protein excretion and an improvement in the levels of serum albumin, cholesterol and lipid peroxide. Further, electron microscopical analysis revealed that the extent and the severity of lesions of the epithelial cells in glomerulus were significantly less in the rats treated wi

ISSN:0951-418X    

DOI:10.1002/ptr.2650080605

出版商:John Wiley&Sons, Ltd.    

年代:1994

数据来源: WILEY

摘要:

AbstractWe have investigated the effects of five phytochemicals on the microsomal‐dependent mutagenicity and metabolism of the tobacco‐specific nitrosamine, 4‐(methylnitrosamino)‐1‐(3‐pyridyl)‐1‐butanone (NNK). Two compounds, d‐limonene and silymarin, had no effect on NNK‐induced mutagenesis inSalmonella typhimuriumTA1535 over the concentration range of 0.1–0.4 μmol/plate. Diallyl sulphide was weakly antimutagenic at a concentration of 0.4 μmol/plate. Both capsaicin and tannic acid showed a dose‐dependent inhibition of mutagenesis in TA1535. Metabolism studies using [3H]NNK indicated that the effects of the phytochemicals on NNK‐induced mutagenesis did not always correlate with the effects on NNK metabolism. α‐Carbon hydroxylation reactions are considered the most significant pathways involved in the metabolic activation of NNK to mutagenic and carcinogenic species. D‐Limonene and silymarin (0,4 μmol) had the least inhibitory effect on the total α‐carbon hydroxylation reactions, 19% and 28%. Capsaicin and diallyl sulphide inhibited these pathways by 74% and 70%. Tannic acid, the most potent phytochemical tested in this study, inhibited total α

ISSN:0951-418X    

DOI:10.1002/ptr.2650080606

出版商:John Wiley&Sons, Ltd.    

年代:1994

数据来源: WILEY

摘要:

AbstractPunicalagain, an active principle isolated from the leaves ofLumnitzera racemosa(Combretaceae), reversed the fall in arterial blood pressure in conscious Wistar rats with orthostatic hypotension induced by injection of hexamethonium into animals subjected to 90° head‐up tilts for 60 s. Punicalagin was found to be less effective on prazosin‐induced orthostatic hypotension. Plasma norepinephrine (NE) was elevated by intravenous injection of punicalagin in a dose‐dependent manner from 0.5 to 15 mg/kg, both in normotensive rats and the orthostatic hypotensive animals. An increase of mean blood pressure was also found in rats that received the injection of punicalagin; this increase in blood pressure was totally abolished by prazosin. Failure of hexamethonium or pentolinium, antagonists of ganglionic nicotinic receptors, to influence the NE releasing action of punicalagin ruled out the participation of ganglionic stimulation. This NE‐releasing action of punicalagin was, however, totally blocked by the inhibitors of noradrenergic nerve terminals, guanethidine or bretylium. Also, the activity of punicalagin was not modified by adrenalectomy. Thus, a direct release of NE from the noradrenergic nerve terminals by punicalagin seems responsible for the reversal of orthostatic hyp

ISSN:0951-418X    

DOI:10.1002/ptr.2650080607

出版商:John Wiley&Sons, Ltd.    

年代:1994

数据来源: WILEY

摘要:

AbstractAdministration of olivacine, 1,5‐dimethyl‐6H‐pyrido[4,3‐b] carbazole to mice inoculated with 105, 103and 102leukaemic cells (L1210) produced significant survival in all treated groups which was not altered by association with the naturally occurring nucleoside deoxycytidine. Treatment with olivacine plus heterologous serum caused leucocytosis due to neutrophilia, lymphocytosis and monocytosis, as opposed to treatment with olivacine alone, which produced leucopenia due to neutropenia and lymphocy

ISSN:0951-418X    

DOI:10.1002/ptr.2650080608

出版商:John Wiley&Sons, Ltd.    

年代:1994

数据来源: WILEY

摘要:

AbstractFive extracts fromA. brasiliana, obtained through different procedures, showed anti‐HSV activity. The best activity was detected in a fraction (B) that was obtained from the crude cold aqueous extract on Sephadex G15. Fraction B showed low cellular toxicity and inhibition from 32.4% to 99.9% at concentrations from 6.2 to 50.0 μg/mL, exhibiting a therapeutic index of 32. Fractions obtained on Sephadex G100and reversed‐phase column also showed considerable inhibition. Fraction B did not show any virucidal activity, however, its inhibitory activity was revealed during the later stages of the virus replication cycle. This fraction showed activity on DNA synthesis of infected c

ISSN:0951-418X    

DOI:10.1002/ptr.2650080609

出版商:John Wiley&Sons, Ltd.    

年代:1994

数据来源: WILEY

摘要:

AbstractThere has recently been considerable interest concerning the biochemical and pharmacological mechanisms of action of resiniferatoxin (Rx). Rx is a daphnane diterpene ester, which is part of the phorbol ester family of diterpenes. We have synthesized3H‐Rx in a three‐step process from the parent alcohol, resiniferonol (Ro). The tritium label is incorporated into the resiniferonol nucleus at the C20position, before esterification of3H‐Ro to3H‐Rx. This compound will be of use in the elucidation of the binding characteristics of Rx to its biochemical receptor

ISSN:0951-418X    

DOI:10.1002/ptr.2650080610

出版商:John Wiley&Sons, Ltd.    

年代:1994

数据来源: WILEY

摘要:

AbstractSome organic solvent extracts of seeds and leaves fromAnnona squamosaexhibit insecticidal activity. They were studied for the management of human lice. However, toxicological data of these extracts have not yet been widely reported. In this experiment, the extracts of active compounds of leaves and seeds fromA. squamosain four organic solvents, i.e. petroleum ether, ether, chloroform and ethanol were tested for toxicity to the eyes and ear skin of rabbits, using 1:10 (w/v) dilutions of dried extracts in propylene glycol as test substances. The results revealed that some extracts caused conjunctival redness, chemosis, rugged cornea, skin erythema and oedema. The organic solvent extracts that produced adverse effects on rabbit eyes were in the following order of severity: ether>petroleum ether>chloroform>ethanol, and those on rabbit ear skin were petroleum ether>ether>chloroform>ethanol. Ethanol extracts of leaves and seeds seemed to produce mildest toxicity to rabbit eyes and no toxicity to rabbit ear skin.

ISSN:0951-418X    

DOI:10.1002/ptr.2650080611

出版商:John Wiley&Sons, Ltd.    

年代:1994

数据来源: WILEY