Effects of herbal preparation on libido and semen quality in boars.

The objective of this study was to investigate the effects of a preparation from herbal extracts (PHE) on libido and semen quality in breeding artificial insemination boars. Ten fertile boars were divided into control and experimental groups according to significant difference of libido. There were no differences in semen quality between groups. Animals were fed a commercial feeding mixture for boars. The feeding mixture for the experimental group was enriched with PHE, which was prepared from Eurycoma longifolia, Tribulus terrestris and Leuzea carthamoides. Duration of the experiment was 10 weeks. Samples of ejaculate were collected weekly. Libido was evaluated according to a scale of 0-5 points. Semen volume, sperm motility, percentage of viable spermatozoa, sperm concentration, morphologically abnormal spermatozoa, daily sperm production and sperm survival were assessed. Amounts of mineral components and free amino acids were analysed in seminal plasma. Significant differences were found in these parameters: libido (4.05 ± 0.22 vs 3.48 ± 0.78; p < 0.001), semen volume (331.75 ± 61.91 vs 263.13 ± 87.17 g; p < 0.001), sperm concentration (386.25 ± 107.95 vs 487.25 ± 165.50 × 10(3) /mm(3); p < 0.01), morphologically abnormal spermatozoa (15.94 ± 11.08 vs 20.88 ± 9.19%; p < 0.001) and Mg concentration (28.36 ± 11.59 vs 20.27 ± 13.93 mm; p < 0.05). The experimental group's libido was increased by 20% in comparison with the beginning of the experiment. Results of this study showed positive effect of PHE on libido and some parameters of boar semen quality.

DPPH Radical Scavenging Activity of Several Naturally Occurring Coumarins and Their Synthesized Analogs Measured by the SIA Method.

ABSTRACT Coumarins, naturally occurring compounds derived from benzopyran, have recently been studied extensively for their antioxidant properties. A lot of coumarins have been isolated and identified from natural sources and many others have been synthesized. It is also known that pharmacological and biochemical properties and thus also therapeutic application of simple coumarins depend upon the pattern of their substitution. As a part of studies of biological effects, four naturally occurring coumarins and 18 synthesized analogs of several compounds were assayed for 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) scavenging activity. For this purpose the highly reliable DPPH test modified to be performed by sequential injection analysis (SIA) system was used. This in our laboratory-developed method was originally proposed for antioxidant screening of large series of plant extracts. In this assay, the DPPH test using the SIA method was used for fast and sensitive evaluation of EC(50) of coumarins. The evaluation of EC(50) of a single compound takes only 15 to 30 min. The structure-activity relationships of tested compounds are also established. The results verified 7,8-dihydroxy-4-methylcoumarins as excellent DPPH radical scavengers. Obtained results correspond with those of other studies and suggest the SIA procedure as a suitable method for fast and sensitive antioxidant analysis of various types of compounds.

[Antioxidants, free radicals, mechanism of action and application in the therapy of the sulfur mustard caused injury]. / Antioxidanty, volné radikály, mechanizmus pusobení a vyuzití pri terapii yperitem navozených poskození.

Antioxidants perform an important role in the maintenance of the integrity of the living organisms. Recently, great attention has been given to antioxidants by a reason of their medical use. It is due to the association of many human diseases with oxidative stress. The present study briefly surveys the types of antioxidants, reactive oxygen and nitrogen species and describes the basic mechanisms of their activity. The application of antioxidants in the therapy of the injury caused by sulfur mustard, a vesicant type chemical warfare agent introduced in World War I, is also given.

Antifungal activity of a thiophene polyine from Leuzea carthamoides.

The thiophene polyine (E)-2-[5-(hept-5-en-1,3-diynyl)-thien-2-yl]-ethan-1,2-diol was isolated from an ethanolic extract of underground parts of Leuzea carthamoides. The thiophene polyine demonstrated significant antifungal activity against all tested species.

[Chalcones (1,3-diarylpropen-1-ones) and their analogs as potential therapeutic agents in cardiovascular system diseases]. / Chalkony(1,3-diarylpropen-1-ony) a jejich analogy jako potenciální terapeutika chorob kardiovaskulárního systému.

At the beginning of a new millennium, several important questions have come to the fore connected with the utilization of natural resources for the investigation of new medicaments (necessity of cooperation of both highly developed and developing countries in the protection of natural resources, necessity to justly evaluate and reward the contributions of the individual cultures in the case that a knowledge of traditional medicine was employed in the development of a new medicament, necessity to achieve the maximal chemical variety of real and virtual libraries of substances from which potential drugs are selected for screening tests). The research of chalcones and its analogues which are relatively easily available not only by isolation from natural material, but also by the methods of classical and combinatorial synthesis should not be substantially affected by the above-described changes. The present communication links up with previous papers (Opletalová, V., Sedivý, D.: Ces. slov. Farm. 48, 252 (1999); Opletalová, V.: Ces. slov. Farm. 49, 278 (2000); Opletalová, V. et al.: Folia Pharm. Univ. Carol. 25, 21 (2000)) and is devoted to the stabilizing action of chalcones on the vascular wall, vasodilating and anti-aggregating effects, and a favourable effect of their antioxidative activity on the functions of the cardiovascular system. The introduction also briefly discusses the nomenclature of this group of compounds.

[Phytotherapeutic aspects of diseases of the circulatory system. 8. Chinese magnolia (Schisandra chinensis (Turcz.) Baill.): production of the drugs and their evaluation, therapeutic and dietary preparations]. / Fytoterapeutické aspekty onemocnení obehového systému, 8. Magnolka cínská (Schisandra chinensis (TURCZ.) BAILL.): produkce drog a jejich hodnocení, lécivé a dietetické prípravky.

Extracts from the fruits (seeds) of Schisandra chinensis L. and pure isolated substances are one of the components of medicinal preparations designed for the treatment of cardiovascular diseases, liver diseases, diseases of the CNS related to the old age, as a supplement in the treatment of neoplasms, diabetes, etc. They are also used for the production of nutraceuticals (soft drinks and health foods), preparations for oral hygiene and for the care for the skin and hair. The review discusses complex analytical methods used for the determination of the content of substances and the phenomena of population ecology in relation with drug production.

[Phytotherapeutic aspects of diseases of the circulatory system. 7. Schisandra chinensis (Turcz.) Baill.): its composition and biological activity]. / Fytoterapeutické aspekty onemocnení obehového systému 7. Magnolka cínská (Schisandra chinensis (TURCZ.) BAILL.): Obsahové látky a jejich biologická aktivita.

Schisandra chinensis (TURCZ.) BAILL., originally a Japanese-Manchurian endemite, yields a vegetable drug (Schisandrae fructus) with a number of very utilizable therapeutic effects. The paper reports the results of phytochemical and pharmacological-toxicological studies approximately from the year 1990 carried out both with the drug and, in particular, the principal isolated lignans of the dibenzo[a,c]cyclooctadiene type. The results confirm the validity of the historical use of the drug, in particular as a hepatoprotective, adaptogenic, and antioxidative agent. It is obvious that a very positive therapeutic effect based on the use of a complex mixture of its principal constituents because their biological effects are complementary and potentiate each other. At the same time, some lignans (e.g. gomisin A, gomisin N) are interesting as new prospective medicines.

Simultaneous determination of quercetin, kaempferol and (E)-cinnamic acid in vegetative organs of Schisandra chinensis Baill. by HPLC.

A reversed-phase high-performance liquid chromatographic (RP-HPLC) separation method with UV spectrophotometric detection has been developed for the determination of major components in leaves and caulomas of Schisandra chinensis Baill. The flavonols (quercetin and kaempferol) and (E)-cinnamic acid were analysed after extraction with alcohol from the dry plant material. Identification was based on retention times and UV spectra by comparison with commercial standards. Quercetin, kaempferol and (E)-cinnamic acid were separated within 12 min using acetonitrile-aqueous 0.05% ortho-phosphoric acid (40:60 v/v) mobile phase. The method has been successfully applied for the quantitative analysis of all three major components in several samples from different harvests using propylparaben as the internal standard.

20-Hydroxyecdysone release from biodegradable devices: the effect of size and shape.

20-Hydroxyecdysone (20-OH) is a natural compound with many demonstrated effects on the physiological functions of vertebrates, particularly increased protein synthesis. Our study sought a suitable dosage form with continuous release of the drug lasting several weeks for implantation into agricultural animals. Biodegradable microparticles and implants of poly(L-lactic) and poly(DL-lactic) acids were prepared. Oligomers of these materials were synthesized, and a method of melting the binary mixture of the oligomer and 20-OH was employed. The particles were prepared simply by grinding the solidified block of the melt and sieving. Implants were prepared by extruding the melt into silicone tubes, removing the solidified content, and cutting into cylinders of 2 mm diameter and various lengths. A new method of preparation of hollow cylinders by aspirating air into silicone tubes filled with the melt was developed. The experiments demonstrated stability of 20-OH during heat treatment. Release of the active ingredient was tested in static in vitro conditions, analogous to those at the site of implantation, and prolonged drug release was obtained with both types of implant. The hollow implants gave release rates nearest to ideal zero-order kinetics and would appear most appropriate for testing in vivo.

Evidence for the anti-hyperlipidaemic activity of the edible fungus Pleurotus ostreatus.

The effects are described of adding either the dried fruiting bodies of the oyster fungus Pleurotus ostreatus, or an ethanolic extract of it, to the diet of normal Wistar male rats and a strain with hereditary hypercholesterolaemia. Addition of the dry oyster fungus to the diet significantly increased, by more than two-fold, the triacylglycerol (TAG) level in the plasma of both groups of rats compared with their respective controls. In contrast, the ethanolic extract did not significantly change TAG levels. Values for total cholesterol and its high- and low-density lipoprotein fractions in the plasma, as well as the calculated atherogenic index, did not show any significant change. Levels of liver cholesterol were significantly lowered by the dried oyster fungus in both hypercholesterolaemic and normal groups of rats, and by the ethanolic extract in normal rats. A significantly increased phospholipid-to-cholesterol ratio in the aortas of both groups of rats, after the administration of either dried oyster fungus or the ethanolic extract of it, suggests a favourable anti-atherogenic effect for both.

[Phytotherapeutic aspects of diseases of the circulatory system. 6. Leuzea carthamoides (WILLD.) DC: the status of research and possible use of the taxon]. / Fytoterapeutické aspekty onemocnení obehového systému. 6. Leuzea carthamoides (WILLD.) DC.: stav výzkumu a moznosti vyuzití taxonu.

Leuzea carthamoides (WILLD.) DC., Asteraceae, has become an important taxon usable in human practice and animal production in recent years. Originally an endemic plant of southern Siberia, now it is widely grown not only in the Union of Independent States, once the original region of introduction, but also in central and eastern Europe. The principal constituents of the whole plant are ecdysteroids (5 beta-cholest-6-on-7-ene derivatives) and flavonoids. In addition, the aerial part contains sesquiterpenic lactones of the guajanolide type, and the roots contain polyines (on the thiophene base). The present paper comprehensively discusses the occurrence, content and biological activity of these substances, the preparations manufactured from the plant, their use in therapeutic practice, food manufacture and animal production in the world and the Czech Republic. The plant has certainly become a taxon with prospects in the Czech Republic, particularly as the source of 20-hydroxyecdysone, which is getting into the limelight in the world.

[Phytotherapeutic aspects of diseases of the cardiovascular system. 5. Saponins and possibilities of their use in prevention and therapy]. / Fytoterapeutické aspekty onemocnení kardiovaskulárního systému. 5. Saponiny a moznosti jejich pouzití v prevenci a lécbe.

The summarizing paper deals with the structure and biological effects of saponins generally and in relation with the treatment and prevention of diseases of the heart and circulatory system. In this field, mainly the saponins from the plants of the genera Panax, Gynostemma or Bupleurum are of use. Also soya saponins and saponins of the genera Astragalus, Salvia, Boussigaultia and Litchi can be employed. Saponins exert a positive effect on the function of the heart direct, or they help treat related diseases. For instance, they inhibit the formation of lipid peroxides in the cardiac muscle or in the liver, they influence the function of enzymes contained in them, they decrease blood coagulation, cholesterol and sugar levels in blood, they stimulate the immunity system. They act either direct, blocking the transfer of Ca2+ ions or modulating the function of Na(+)-K(+)-ATPase, or they help resorb other active principles. It can be concluded that saponins are a prospective group of drugs of natural origin for the prevention and treatment of diseases of the heart and circulatory system.

[Phytotherapeutic aspects of diseases of the circulatory system. 4. Chitin and chitosan]. / Fytoterapeutické aspekty onemocnení obehového systému 4. Chitin a chitosan.

Chitin and chitosan are nitrogenous polysaccharides. The structure of the chitin molecule is similar to that of cellulose but it is composed of the units of 2-acetylamino-2-deoxy-D-glucopyranose bound (1 --> 4) by a glycosidic bond. In contrast to chitin, chitosan amino groups are not mostly acetylated. These polysaccharides occur particularly in the fungal kingdom, in invertebrate animals, in some brown algae, and very negligibly in higher plants. Great attention has been paid to chitin and chitosan in recent years. Of great interest are their antihypercholesterolemic and antihyperlipidemic activities which have been experimentally demonstrated. In practice there already exist some medicinal preparations and food products with medicinal and preventive properties against some risk factors of atherosclerosis. Also the anticoagulative and anti-aggregative effects of sulfated derivatives of chitosan are not negligible. The research in this field is, however, at the initial stage. Both polysaccharides have been introduced into pharmaceutical technology where they can be employed as very good drug vehicles. Promising results have been achieved in experiments with antineoplastics (5-fluorouracil and methotrexate), with nonsteroidal antiphlogistics (ibuprofen) and others. It is considered very advantageous that chitin and chitosan possess low toxicity, allergize only a little, and exert moderate immunostimulating effects. Both polysaccharides are metabolized by lysosome. Chitin is obtained from the cuticles of sea animals which are waste products from food industry. The technologies of obtaining chitin from lower fungi (e.g. the genus Aspergillus) have been worked out. Chitosan is obtained by deacetylation of chitin. Chitin and chitosan are polysaccharides with ever-extending use. Increasing attention is paid to them also due to the fact that they are contained in a large extent in food fungi, e.g. Pleurotus ostreatus.

[The basis and goals of the pharmacy profession--pharmacobotany and its contribution to the development of drugs]. / Východiska a cíle farmaceutických disciplín--farmakobotanika a její príspevek k vývoji léciv.

Pharmacy is one of very comprehensive and complex fields of human activity; the interrelationships of its individual principal disciplines did not always develop synergically in the course of time. At present, when the field commemorates important anniversaries and develops in the period of new social changes, it is necessary to contemplate the development of the individual fields and their balances in the principal entity for the pharmacist--the medicament. The historiography of the field unambiguously points at the cardinal position of classic pharmacognosy in this process, showing its development, separation of pharmacology, the relationship of pharmacognosy to pharmaceutical chemistry, the differences between the two disciplines and the origin of galenical pharmacy, or the not very fortunate concept of biopharmaceutics. This process takes place in the picture of the dialectical unity of the principal pharmaceutical categories: the drug--the pharmaceutical preparation--the medicament. The development of pharmacobotany as a practical complex discipline originated from pharmacognosy shows in a graphic way the development of the discipline "an sich" into the entity "für sich" and suggests the approach of the pharmacist to the phenomenon of the medicament from the historiographical viewpoint.

[CADISO (Cardiovascular Diseases and Stability of the Organism): 10 years of integrated research on natural substances at the Charles University Pharmacy School in Hradec Králové]. / CADISO: 10 let integrovaného výzkumu prírodních látek na Farmaceutické fakulte UK v Hradci Králové.

The research project CADISO (Cardiovascular Diseases and Stability of the Organism--Phytotherapeutical Possibilities) is an alliance board associating approximately 20 professional institutions, its centre and coordinating laboratory being the Department of Pharmaceutical Botany and Ecology, Faculty of Pharmacy, Charles University, Hradec Králové. It aims at the prevention (additives in food industry) and therapy of diseases of the circulatory apparatus using phytotherapeutic agents and substances isolated from higher plants and fungi. The project is divided into three systems of investigation: ADAPRETE, i.e. the substances increasing the nonspecific resistance of the organism (adaptogenes of plant origin, immunostimulants), DIACORD, dealing with the substances acting on the cardiovascular system in a mediated way, i.e. treating the diseases the eventual action of which alters the heart and vessels (antihypercholesterolemics, antihyperlipidemics, antidiabetics, anti-oxidants and quenchers of free radicals, hepatoprotectives, anti-aggregating agents), and CORCORAN studying the taxons and substances isolated from them which act directly on the circulatory system (cardiotonic, anti-arrhythmic and vasodilating agents). To achieve a real purpose of the project, the linking-up of the phytochemical, pharmacological-toxicological, pharmaceutical-technological fields, production of raw materials and legislation is ensured.

[Phytotherapeutic aspects of diseases of the circulatory system. III. Cardiotonic and cardiotoxic effects of hyrcanoside and deglucohyrcanoside isolated from Coronilla varia L]. / Fytoterapeutické aspekty onemocnení obehového systému. III. Kardiotonický a kardiotoxický úcinek hyrkanosidu a deglukohyrkanosidu izolovaných z Coronilla varia L.

The Cardiotonic and cardiotoxic effects of two cardiac glycosides-hyrcanoside and deglucohyrcanoside-isolated from the seeds of Coronilla varia L. were evaluated in the paper--in comparison with the effect and toxicity of digoxin and ouabain. Evaluation of the cardiotonic effect using the methods of heart "in situ" and the isolated heart (Langendorff) proved that deglucohyrcanoside is more effective than hyrcanoside and that its effect is equal to that of digoxin as well as ouabain. The efficacy of deglucohyrcanoside et least to that of digoxin, while the toxicity of the former is several times lower, makes the glycoside a potential candidate for therapeutic use.