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PubMed1979

Haemodynamic and hormonal effects of short-term oestradiol treatment in postmenopausal women.

Haemodynamic changes during a 3-wk treatment with oestradiol valerianate (2 mg/day orally) were studied in 12 postmenopausal women by isotope 113Inm radiocardiography. Systolic blood pressure measured in the supine position decreased during oestradiol treatment by 3% (P less than 0.05) and the diastolic blood pressure decreased by 4% (P less than 0.01). The heart rate decreased by 15% (P less than 0.001). Blood volume increased during oestrogen treatment by 5% (P less than 0.05) whereas cardiac output decreased by 9% (P less than 0.05). Stroke volume increased by 13% (P less than 0.001) due to concomitant decrease in heart rate. Changes in plasma oestrone and oestradiol concentrations during oestradiol valerianate substitution showed a positive correlation with the changes of blood volume.

Adult↗
PubMed1979

Plants and hypotensive, antiatheromatous and coronarodilatating action.

However great the success in the therapy of hypertension, atherosclerosis and ischemic heart disease has been gained today by recent efficient drugs, the definite healing of patients is not yet attained. The late discovery of reserpine, such an efficient drug of plant origin against hypertension, convinced so far reluctant scientists to consider the chemical compounds of the plant world. With respect to this traditional medical knowledge, it seems necessary to define more accurately the specificity of these healings-sometimes recommended unspecifically for a whole branch of medicine. This experimental verification should not use inconsiderately the present-day classification of diseases; there should be an awareness that conventional experimental methods in pharmacology are often unsuitable for revealing the real biological activity of one or another medicinal plant. The interest in the millennial empirical field of health care is acknowledged by the World Health Organization which promotes research and development of traditional medicine, along with investigations into its psychosocial and ethnographic aspects. These studies cover a number of plants growing in Bulgaria that have a healing effect in hypertension, atherosclerosis and ischemic heart disease according to the data of traditional medicine. Using screening methods, extracts and chemically pure substances were investigated; extraction was done with solvents such as water, ether, chloroform, dichloretan, ethanol, methanol, and acetone. Most of the experiments were carried out on anesthetized cats, rabbits and dogs. The substances tested were applied mainly intravenously, and in some experiments orally. Chronic experiments were also carried out on wakeful dogs with induced hypertension, on animals fed on an atherogenic diet, and on animals with induced arrhythmia and coronary spasm. Data are presented of clinical examination of some plants or of active substances isolated from them. Major results of these studies are presented for the following plants: Garlic, Geranium; Hellebore; Mistletoe; Olive; Valerian; Hawthorn; Pseucedanum arenarium; Periwinkle; Fumitory. For another 50 plants growing in Bulgaria and in other countries the author presents his and other investigators' experimental and clinical data about hypotensive, antiatheromatous and coronarodilatating action.

Animals↗
PubMed1977

[Experimental studies of the effects of Seda-Kneipp on the sleep of sleep disturbed subjects; implications for the treatment of different sleep disturbances (author's transl)].

Seda-Kneipp a compound preparation of valerian and hops was given to sleep disturbed subjects during the second or third of three consecutive nights disturbed by heavy traffic noise. Prior drug administration reduced the noise induced disturbance of sleep stage patterns: slow-wave sleep and stage REM increased. It is recommended that the initial treatment of severe insomnia by "strong" sleeping pills should be followed by a period during which "weak" sleeping pills are given before the drug administration finally is discontinued.

Adult↗
PubMed1979

Thiaisoleucine and protein synthesis.

Thiaisoleucine is an isoleucine analogue having the gamma-methylene group of the valerianic carbon chain substituted by a sulphur atom. It has been demonstrated that thiaisoleucine is activated and transferred to tRNAIle by rat liver aminoacyl-tRNA synthetase and inhibits isoleucine incorporation into polypeptides in protein synthesizing systems from rat liver or rabbit reticulocytes, whereas it does not affect either leucine incorporation or ribosome run-off or polypeptide chain elongation rate. All tests were performed in comparison with O-methyl-threonine, an isoleucine analogue with the gamma-methylene group substituted by an oxygen atom. In all the reactions studied, both thiaisoleucine and O-methyl-threonine act as competitive inhibitors of isoleucine. With respect to O-methyl-threonine, thiaisoleucine shows higher activity as an isoleucine inhibitor.

Adenosine Triphosphate↗
PubMed1978

Estrogens delay the postpartum recovery of the LH-RH-induced gonadotropin release.

In 27 healthy postpartum women, who were neither lactating nor receiving any therapy, LH-RH stimulation tests (50 micrograms i.v.) were performed on days 7, 14, 21 and 28 of the puerperium. In a second group of 9 postpartum women an i.m. injection of 10 mg estradiol valerianate was administered within the 3rd postpartum day, and an LH-RH stimulation test was performed on days 14 and 21 of the puerperium. Blood was withdrawn at standard intervals and LH and FSH measured by radioimmunoassay. No significant FSH and LH response was found on day 7. On day 14 there was a significant release of FSH but no LH was released. On days 21 and 28 there was a significant release of FSH and LH but the magnitude of the FSH response was greater than that of the LH release. The administration of estrogens did inhibit the recovery of the pituitary from its refractoriness: on day 14 no release of LH and FSH was observed; on day 21, only a significant release of FSH could be detected in the second group of postpartum women. This emphasizes the major role played by steroids in the regulation of the hypothalamo-pituitary-gonadal function.

Estradiol↗
PubMed1977

[Estimation of the net energy using volatile acids produced in the process of in-vitro digestion with ruminal fluid].

47 types of green feeds and roughages were subjected to an in-vitro fermentation with dilute ruminal fluid. The volatile fatty acids produced in this process were determined quantitatively in accordance with the method of digestibility estimation proposed by Tilley and Terry (1963). An average of 5 Mol FFS (FFS=volatile fatty acids) was found per kg of dried feed, a value is also reported in the literature. The ratios of acetate to propionate to n-butyrate to iso-butyrate to n-valerianate were 64.2 : 25.4 : 6.6 : 0.8 : 1.5 : 1.5. In this ratio, propionic acid predominated so that acetic acid and n-butyric acid were misrepresented compared with the data of in-vivo measurements made for the corresponding foodstuffs. Consequently, it is only within certain limits that values of FFS concentrations obtained in vitro may be used for estimating net energy data, disregardful of the fact that the FFS are the main source of metabolizable energy in ruminants. The reliability index for an estimation of Starch Equivalents and NEFr based on the above-mentioned method was found to be considerable lower (0.71 and 0.80) than that based on in-vitro digestibility measurements (0.86).

Animal Feed↗
PubMed1977

Carbohydrate metabolism and hormonal replacement therapy: problems and clinical results.

Substitution treatment with a biphasic hormone combination (Cyclacur) was administered to twenty women in menopause. Nine of these had undergone hysterectomy and/or ovarectomy. The experimental cycle consisted of a daily dose of 2 mg estradiol valerianate as estrogen for 11 days, the identical dose of estrogen plus 0.5 mg dl-norgestrel as gestagen for 10 days, and a 7-day medication-free period. An initial placebo cycle was administered, followed by 7 experimental cycles and one final placebo cycle. Laboratory tests were carried out regularly. There were no significant changes during the investigation in serum lipids, blood sugar values, or serum enzyme tests used as parameters of hepatic function. Of the hematological parameters a moderate rise in hematocrit was observed. There was no change in serum protein-bound iodine.

Alkaline Phosphatase↗
PubMed1975

[Gynecological, hematological and metabolic studies during therapy with an estrogen-gestagen combination preparation].

Twenty women after menopause were submitted to substitution treatment with a biphasic hormone combination (Cyclacur¿). Nine of these had undergone hysterectomy + ovarectomy. Through 11 days each of the women was administered a daily dose of 2 mg estradiol-valerianate as estrogen. Subsequently, for another 10 days each was given the identical dose of estrogen plus 0.5 mg DL-norgestrel as gestagen. Upon this followed an intermission of 7 days without any medication. After 1 cycle of placebo, 7 cycles of medication were followed by 1 cycle of placebo again with regular controls. Climacteric signs and symptoms were eliminated entirely. In those women without hysterectomy withdrawal-menorrhagia occurred promptly 2--3 days after discontinuing medication. During the entire period of investigation there was no significant change in serum lipids, blood sugar values, or serum enzyme tests used as parameter of hepatic function. As far as hematology is concerned there was a moderate rise of hematocrit. No change of serum protein-bound iodine was observed.

Alanine Transaminase↗
PubMed1978

[Vertebrate hormones influence on the reproduction of Biomphalaria glabrata and on Schistosoma mansoni infection (author's transl)].

The influence of fifteen vertebrate hormones on the B. glabrata reproduction and on S. mansoni infection have been studied. Hecogenine and pregnadienolone significantly increased the snail's number of eggs; testosterone, diethylstilbestrol and estradiol valerianate decreased their number of eggs and the mesterolone and progesterone produced a slight decrease in the number of eggs. Crude hecogenine, pregnenolone, prednisone, estradiol, cholic acid, diosgenin, estrone and pregnadione have not shown any significant alteration on the snail reproduction. None of these hormones presented any influence upon the S. mansoni cycle in B. glabrata. Molluscicidal, oocidal and cercarcidal activities have been observed with diethylstilbestrol in concentrations below 10 ppm.

Animals↗
PubMed1977

[Comparison of vaginal cytologic effects and blood elimination curves of different oestrogen drugs (author's transl)].

With different oral oestrogens it was studied, if relations are existing between pharmacokinetic and vaginal effect. By means of Karyopycnotic Index and Dynamic Oestrogenicity Index the cytological effect was quantified from a single dose of oestradiol valerianate, mestranol, ethinyloestradiol and 3 depot oestrogens proved on postmenopause women and compared with adequate pharmacocinetical investigations. The courses of oestrogen levels did not correlate with indices. Both methods of investigation do not compensate, but complete one another. Depotoestrogens and short acting oestrogens are distinguishable with regard to proliferation maxium and steepness of index decline.

Delayed-Action Preparations↗
PubMed1976

[Additive treatment of metastasizing breast cancer with special reference to postmenopausal age (results of a randomized study)].

Two therapy groups were formed at random out of 82 patients with progressive carcinoma of the breast. One was treated with estrogens, namely 17-ethinyl 1,3,5-estratriene 3,17 diol (SH 8.1083). The second group was treated with depot preparations consisting of a combination of estrogens and gestagens; these patients received 90 mg estradiol valerianate and 300 mg 17-hydroxy-19-norprogesterone caproate (SH 8.0834) weekly. The estrogen therapy resulted in a remission rate of 48% (complete remission 21.1%, partial remission 26.9%). The remission rate of the combination treatment was 46.6% (complete remission 23.3%, partial remission 23.3%). There was no considerable difference between the remission rates produced by the two therapeutik methods. It is remarkable that much more osseous remissions were found under the combination therapy of estrogens and gestagens. There were no substantial differences between the remission rates of the soft-tissue metastases and the pleuropulmonary metastases. In the estrogen group the remissions took 7.7 months, whereas an average remission period of 8.3 months was observed in the estrogen-gestagen group.

Age Factors↗
PubMed1979

Mass spectrometry of valepotriates.

The mass spectrometry of eight valepotriates and their derivatives has been investigated. Mass spectral fragmentation schemes have been proposed as well as the use of this fragmentation for structural elucidation. Structures of two valepotriates, acevaltrate and homoacevaltrate, have been clarified.

Cyclopentanes↗
PubMed2025

The plastid genome of the critically endangered Valeriana trinervis (= Centranthus trinervis) and insights from comparison with other Valeriana plastomes (Caprifoliaceae).

The first complete plastid genome of the critically endangered species Valeriana trinervis was sequenced, assembled and compared with other published Valeriana plastomes. In this study, we assembled the plastid genome of the critically endangered, endemic species Valeriana trinervis (= Centranthus trinervis) and compare it with all published plastomes of Valeriana. We found not only differences in the inverted repeats boundaries, in the type and abundance of repeats, but also similarities in codon usage and microsatellite numbers. We detected non-canonical start codons in several genes and identified variation in several regions that could be useful for phylogenetic and phylogeographic studies. The phylogenetic tree inference based on both full plastomes and coding sequence data indicated that V. trinervis is sister to all Eurasian Valeriana accessions confirming the phylogenetic position recently investigated. This is the first plastome available for a species of the Mediterranean clade of Valeriana previously known as Centranthus, and it adds further data to understand the evolution and diversification of this systematically debated genus.

Genome, Plastid↗
PubMed1978

[High-performance liquid chromatographic separation and quantitative determination of valepotriates in valeriana drugs and preparations (author's transl)].

It is possible directly to separate and analyse, quantitatively and qualitatively, the valepotriates from Valeriana crude extracts or from commercial Valeriana preparations by high-performance liquid chromatography. The separations are achieved on 4 or 8 mm I.D. columns packed with silica gel (particle size 10 micron) with n-hexane-ethyl acetate mixtures as eluent. A refractive index detection system is necessary for determining all of the valepotriates. If the concentration differences between didrovaltratum and valtratum are very great, an ultraviolet (UV) detector must be used and the determination must be conducted in two steps. For valtratum drugs UV detection alone will suffice. As internal standards p-dimethylaminobenzaldehyde should be used for extracts and preparations from valtratum races, and benzaldehyde in the presence of didrovaltratum races. This determination is superior to the combined thin-layer chromatographic-hydroxamic acid method used hitherto with respect to time consumption, precision, and sensitivity.

Cyclopentanes↗