Effects of phytoestrogenic isoflavones from red clover (Trifolium pratense L.) on experimental osteoporosis.

The most common type of osteoporosis is bone loss associated with ovarian hormone deficiency at menopause. There is evidence that diets which contain high levels of phytoestrogenic isoflavones are associated with a low incidence of osteoporosis and menopausal symptoms. Plant extracts, which contain high levels of isoflavones, such as Red clover (Trifolium pratense L.), have been used to reduce menopausal symptoms. The objective of this study was to evaluate the preventive effects of Red clover total isoflavones on the progression of bone loss induced by estrogens deficiency (ovariectomy) in rats. Bilateral ovariectomy was performed on female Wistar rats. One week after the operation the rats were treated with an oral dose of 20 and 40 mg of total isoflavones daily for 14 weeks. The results from this study showed that the ovariectomy reduced bone mineral content, femoral weight, femoral density, mechanical strength of the tibia and increased the levels of bone specific alkaline phosphatase in the serum and the number of osteoclasts in the femur sections compared with sham operated controls. Treatment with isoflavones significantly increased bone mineral content, mechanical strength of the tibia, femoral weight, femoral density and prevented the rise of serum alkaline phosphatase levels. In addition, the treatment with isoflavones significantly reduced the number of osteoclasts compared with the ovariectomized control rats. These findings suggest that Red clover isoflavones are effective in reducing bone loss induced by ovariectomy, probably by reducing of the bone turnover via inhibition of bone resorption.

Cardiovascular effects of the aqueous extract of Gynostemma pentaphyllum Makino.

In the present study, the cardiovascular activity of the aqueous extract of Gynostemma pentaphyllum Makino leaves was investigated in the anaestetized guinea-pigs and has been compared with two of its isolated gypenosides (III, VIII) and with verapamil, a well-known Ca-antagonistic drug. The results obtained showed that the intravenous administration of the decoction of G. pentaphyllum (2.5, 5 and 10mg/kg) produced a protective effect against pitressin-induced coronaryspasm, arrhythmias and pressor response. Extract also increased the dose of ouabain required to cause ventricular tachyarrhythmias and lethality. Further extract reversed ouabain-induced persistent ventricular tachycardia and restored sinus rhythm in a dose-dependent manner. The results obtained have also shown that gypenosides III and VIII caused similar protective effects in both experimental models used; however, the duration of the action is lower than that of the extract containing corresponding quantities of gypenosides III and VIII.

Effects of Calotropis procera on oestrous cycle and on oestrogenic functionality in rats.

Effects of ethanolic and aqueous extracts of Calotropis procera (Ait.) R.Br. roots, have been studied on oestrous cycle and on some parameters of oestrogenic functionality in rats. Both extracts have been shown to interrupt the normal oestrous cycle in 60 and 80%, respectively, of rats treated. The rats exhibited prolonged dioestrous stage of the oestrous cycle with consequent temporary inhibition of ovulation. The contemporary administration of commercial oestro-progestinic preparation exhibited the same effects in 100% of rats treated. However, the extracts have not demonstrated to possess oestrogenic activity when tested in immature female bilaterally ovariectomized rats.

Central nervous system activity of terpenoids from marine sponge.

Some terpenoids extracted from marine sponge: triacetylated disidein, 2-tetraprenyl benzoquinol and 4 hydroxy-3-tetraprenylbenzoic acid 2-polyprenyl benzoquinols, avarol and furospongin-1 were tested by multidimensional Irwin screening and with some tests for analgesic and muscle relaxant activity. The three prenylhydroquinols derivatives and avarol show a good analgesic activity and low toxicity.

3,3'-Di[1,3-thiazolidine-4-one]system. IV. Synthesis and pharmacological properties of 3,3'(1,2-ethanediyl)bis [2-aryl-1,3-thiazolidine-4-one 1,1-dioxide] derivatives.

The 1,1' disulfones obtained by oxidation of the corresponding dl and meso 3,3'(1,2-ethanediyl)bis [2-aryl-4-thiazolidinone] compounds previously investigated, were evaluated as anti-histamine, anti-inflammatory, analgesic and anti-pyretic agents. All 2,2' fluorophenyl compounds were found to be significantly active in inhibiting carrageenin-induced edema, whereas only para-substituted derivatives were active on the histamine-induced bronchospasm in the guinea-pig. They also showed analgesic effects that reached and sometimes exceeded those of indomethacin and phenylbutazone used as reference drugs.

[Buflomedil and the speed of glycolysis. Note I]. / Buflomedil e velocità di glicolisi. Nota I.

An in vitro study was conducted into the speed of glycolysis is human erythrocytes. Incubation with Buflomedil does not change the speed of glycolysis.

[Changes in erythrocyte ATP after the oral administration of buflomedil hydrochloride]. / Modificazioni dell'ATP eritrocitario dopo somministrazione orale di buflomedil cloridrato.

Variations in erythrocyte ATP content were studied after the oral administration of 600 mg Buflomedil a day for seven days in ten vasculopathy patients. In all patients the drug increased erythrocyte ATP.

A drug used in traditional medicine: Harpagophytum procumbens DC. III. Effects on hyperkinetic ventricular arrhythmias by reperfusion.

In Langendorff preparations of rat heart, hyperkinetic ventricular arrhythmias (HVA) have been induced by an ischaemic perfusion (coronary flux 0.5 ml/min; pressure 8 mmHg) and following reperfusion at basal conditions (coronary flux 8 ml/min; pressure 50 mmHg). Crude methanolic extracts of Harpagophytum procumbens secondary roots and harpagoside showed a significant, dose-dependent, protective action toward HVA induced by reperfusion.

A drug used in traditional medicine: Harpagophytum procumbens DC. IV. Effects on some isolated muscle preparations.

Effects of the crude methanolic extract of Harpagophytum procumbens secondary roots and two of its active principles, harpagoside and harpagide, on some smooth muscle in vitro have been studied. The results obtained show how the action of H. procumbens is due to a complex interaction between the various active principles contained in the drug and suggest that they, especially harpagoside, interfere with the mechanisms that regulate the influx of calcium in the cells.

[3,3'-bi-1,3-thiazolidine]-4,4'-dione system. I. Synthesis, conformational analysis and pharmacological activities of 2,2'-diaryl derivatives.

The two configurational isomers, d1, and meso, of some 2,2'-diaryl-[3,3'-bi-1,3-thiazolidine]-4,4'-dione derivatives have been obtained and characterized. The 1H-N.M.R. spectra of both stereoisomers in DMSO-d6 solution are temperature-dependent and their dynamic behaviour has been related to the hindered rotation of the N--N bond. Evidence for an orthogonal disposition of the two heterocyclic rings, in the ground state, is presented. These new bicyclic compounds possess interesting antiinflammatory, analgesic and antipyretic activities as well as low acute toxicity and ulcerogenicity. The antiinflammatory effect, which in some compounds is higher than that of indomethacin and phenylbutazone, appears to be a function of the relative disposition of the substituents at position 2 and 2': generally the meso isomers are more active than the d1 ones. The lipophilicity of the tested compounds was determined by reversed-phase thin-layer chromatography.

Investigations on Dieffenbachia amoena Gentil. I: Endocrine effects and contraceptive activity.

Contraceptive activity and the correlated endocrine alterations of an aqueous extract of the leaves of Dieffenbachia amoena were investigated. In female Wistar rats the extract, given for 4 days during the estrous cycle, induced significant variations of luteinizing hormone (LH), follicle-stimulating hormone (FSH), prolactin (PRL) progesterone and 17 beta-estradiol levels. It also determined a reversible interruption of the estrous cycle with consequent temporary inhibition of ovulation.

N-trifluoroacetyl derivatives as pharmacological agents. III. Analgesic, antipyretic activities and physicochemical features of some antiinflammatory trifluoroacetanilides.

Further pharmacological (antipyretic and analgesic activities) and physicochemical (pka and relative lipophilicity) studies are reported on some trifluoroacetanilides which have preliminary revealed promising activities in the animal models of acute and chronic inflammation, in analogy with the known antiinflammatory trifluoromethanesulfonanilides.

A drug used in traditional medicine. Harpagophytum procumbens DC. I. Scanning electron microscope observations.

Histological characteristics, as observed by scanning electron microscope, of the secondary roots of Harpagophytum procumbens DC. (Pedaliaceae), a drug widely used in South African traditional medicine, specially by Bushmen, Hottentots and Bantu, are described in detail. It has been possible to reveal some morphological elements that, together with superficial granular material containing harpagoside and harpagide, allow drug identification.

A drug used in traditional medicine: Harpagophytum procumbens DC. II. Cardiovascular activity.

In conscious normotensive rats the dried crude methanolic extract of Harpagophytum procumbens secondary roots caused a significant dose-dependent reduction of arterial blood pressure. The decrease was significant only at higher doses given by gavage (dried extract = 400 mg/kg). At the same time a decrease of heart rate was observed. In the same experimental conditions, harpagoside presented an activity lower than doses of Harpagophytum procumbens extract containing corresponding quantities of harpagoside. In spontaneously beating Langendorff preparations of rabbit heart, the Harpagophytum procumbens methanolic extract caused a mild decrease in the heart rate with a concomitant mild positive inotropic effect at lower doses but a marked negative inotropic effect at higher doses. The coronary flow decreased at higher doses only. The negative chronotropic and positive inotropic effects of harpagoside were comparatively higher with respect to that of the extract, whereas harpagide had only a slight negative chronotropic effect and a considerable negative inotropic one. Both in experiments on intact rats and on isolated rabbit heart, the Harpagophytum procumbens extract also demonstrated a protective action with regard to arrhythmias induced by aconitine, and particularly to those provoked by calcium chloride and epinephrine--chloroform.

N-Trifluoroacetyl derivatives as pharmacological agents. II. Trifluoroacetanilides: synthesis and antiinflammatory activity.

The analogy with the anti-inflammatory trifluoromethane-sulfonanilides prompted us to the synthesis of a series of trifluoroacetanilides which were found to maintain the pharmacological properties of the analog sulfonanilides. Many of the obtained compounds inhibited either the carrageenin-induced rat paw edema and the adjuvant-induced arthritis; some showed better anti-inflammatory properties than indomethacin and phenylbutazone. Acute toxicity and ulcerogenic effects were significantly lower than those of reference drugs.