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THE INTERACTION OF SOME STIMULANT AND DEPRESSANT DRUGS ON THE FROG HEART.

THE ACTIVITY OF FROG ISOLATED HEARTS WAS DEPRESSED BY ALTERING THE PERFUSING RINGER SOLUTION IN FIVE DIFFERENT WAYS: by reducing the calcium content, by increasing the potassium content, and by adding ether, thiopentone or acetylcholine. Depressed hearts were perfused with Ringer solution containing the following stimulant drugs: paullinia tannin, tannic acid, hydrogen peroxide, sodium oleate, sodium caprylate and ouabain. All these stimulant drugs had similar actions on hearts depressed by calcium lack, ether and thiopentone; hearts depressed by acetylcholine were, however, only weakly stimulated. Hearts depressed by potassium were readily stimulated by oleate, caprylate and paullinia tannin; ouabain and hydrogen peroxide had weak stimulant actions on hearts depressed by potassium, and tannic acid had a negative inotropic action. The differing actions on hearts depressed by potassium are probably related to differences in the degrees of fixation of the stimulant drugs. The mode of action of ouabain and the functional lesion in hearts depressed by narcotics are discussed.

Acetylcholine↗

Iron staining of the acquired enamel pellicle after exposure to tannic acid or chlorhexidine: preliminary report.

Extrinsic discoloration of teeth following a large consumption of tannin-containing beverages or a prolonged use of chlorhexidine mouthrinses is a well known observation. Tannins as well as chlorhexidine are denaturing agents. Based on preliminary studies revealing the presence of iron in chlorhexidine discolored pellicle material, the ability of iron to stain the integument after pretreatment with the two denaturants was studied in a human model. The denaturing effect of an acidic environment was also included. Enamel slabs fixed to acrylic appliances were carried in the oral cavity and alternately exposed to the test solutions in different sequences in vitro. Pretreatment with chlorhexidine or tannic acid led to marked discoloration upon iron application during 5-d tests, whereas the compounds individually had no such effect. A large content of the metal was found in the stained material. Stannous fluoride appeared to reduce the formation of the pigments, and strong oxidation completely bleached the established color. Possible mechanisms underlying the phenomena observed are discussed.

Chlorhexidine↗

Antitumor activities of ellagitannins against sarcoma-180 in mice.

Forty-five ellagitannins and related compounds were intraperitoneally injected into mice once, 4 d before intraperitoneal inoculation of S-180 cells, and their antitumor activities were evaluated. When an antitumor-active tannin was defined as one producing a 70% increase or more in the mean life span of mice or one regressor out of six mice, twenty-one ellagitannins were active. Among monomeric ellagitannins, tellimagrandin II was most active. Most of the oligomeric ellagitannins, consisting of tellimagrandins I and II as the monomer unit, had a significant antitumor activity. Macrocyclic ellagitannins were all active. Oenothein B, among them, had the most potent antitumor activity. In contrast, ellagitannins containing a casuarictin or potentillin moiety in their molecules, except for extensively oligomerized ones, showed very low or negligible activity. These results suggest that tannins need the ellagitannin monomer units, having galloyl groups at the O-2 and O-3 positions on the glucose core(s), such as tellimagrandins, in order to exhibit a strong antitumor activity.

Animals↗

New TNF-alpha releasing inhibitors, geraniin and corilagin, in leaves of Acer nikoense, Megusurino-ki.

The success of green tea as a cancer preventive is based on evidence that green tea contains tannins and antioxidants, does not show toxicity in humans and has long traditional use in Asia. In the light of this, herbal medicines are now also attracting attention as potential sources of cancer preventive agents. Using the inhibition of TNF-alpha release assay, we studied Acer nikoense (Megusurino-ki in Japanese), one of the herbal medicines. The inhibitory activity of TNF-alpha release was found in the leaf extract rather than the bark extract, and the main active constituents were identified as geraniin and corilagin, which are present in another Japanese traditional herb, Geranium thunbergii (Genno-shoko). The IC50 values of TNF-alpha release inhibition were 43 microM for geraniin and 76 microM for corilagin, whereas that for (-)-epigallocatechin gallate (EGCG) was 26 microM. Treatment with geraniin prior to application of okadaic acid, a tumor promoter on mouse skin initiated with 7,12-dimethylbenz(a)anthracene, reduced the percentage of tumor-bearing mice from 80.0 to 40.0% and the average numbers of tumor per mouse from 3.8 to 1.1 in week 20. Thus, geraniin has slightly weaker inhibitory activity than EGCG. Since geraniin and corilagin have been well investigated as representative tannins, we discuss here the new possibility of classical herbal medicine in the development of preventive agents for cancer and other life-style related diseases.

3T3 Cells↗

Effect of soaking, germination, cooking and fermentation on antinutritional factors in cowpeas.

The present work deals with the study of efficacy of some treatments, namely soaking (in water and bicarbonate solution), ordinary and pressure cooking, germination and fermentation in reducing or removal of antinutritional factors usually present in cowpeas (protease inhibitors, tannins, phytic acid and flatus-producing oligosaccharides (raffinose and stachyose). The results showed that long-time soaking (16 h) in bicarbonate solution caused remarkable reduction in the antinutritional factors. Pressure cooking was more effective than ordinary. Cooking pregerminated cowpeas was most effective. Fermentation completely removed trypsin inhibitor, oligosaccharides and reduced remarkably phytic acid. However, tannins noticeably increased.

Cooking↗

New perspectives on taste and primate evolution: the dichotomy in gustatory coding for perception of beneficent versus noxious substances as supported by correlations among human thresholds.

In various environments where primates are presently observed, as well as in forests and savannas which have been inhabited by australopithecines and early hominids, there are (or there have been presumably) categories of substances eliciting taste signals associated with stereotyped responses. Such is the case for various soluble sugars of fruits and nectars, attracting consumers, and for several plant compounds in which bitter or strongly astringent properties have a repulsive effect. The occurrence of such classes of tasty substances among natural products appears to be related to the evolutionary trends that shaped primate sensory perception (for detecting either beneficent or potentially noxious substances) in the context of a long history of coevolution between animals and plants. Here, we present original psychophysical data on humans (412 individuals aged 17-59 years) as an analogy with which to test recent evidence from electrophysiology in nonhuman primates (Hellekant et al. [1997] J. Neurophysiol. 77:978-993; Danilova et al. [1998] Ann. N.Y. Acad. Sci. 855:160-164) that taste fibers can be grouped into clusters of "best-responding fibers" with two more specific clusters, one for sugars and one for quinine and tannins. The collinearity found between human taste responses (recognition thresholds) for fructose and sucrose, as well as for quinine and tannins, is presented and discussed as another evidence of the two-direction evolutionary trend determining taste sensitivity. Salt perception appears to be totally independent of these trends. Accordingly, the appreciation of a salty taste seems to be a recent culturally learned response, and not a primary taste perception. The very existence of primary tastes is discussed in the context of evolutionary trends, past and present.

Adolescent↗

Fenton-type reactions and iron concentrations in the midgut fluids of tree-feeding caterpillars.

Peroxides are formed in the midgut fluids of caterpillars when ingested tannins and other phenolic compounds oxidize. If these peroxides broke down in the presence of redox-active metal ions, they would form damaging free radicals (Fenton-type reactions). Elemental iron is present in relatively large amounts in leaves and artificial diets, but little is known about its concentration and redox state in midgut fluids, or the extent of Fenton-type reactions in these conditions. This study compared the levels of hydroxyl radicals and iron in the midgut fluids of two species of caterpillars: Orgyia leucostigma, in which phenol oxidation is limited, and Malacosoma disstria, in which phenol oxidation is more extensive. We tested two hypotheses: (1) higher levels of hydroxyl radicals are formed in M. disstria (consistent with the higher concentrations of hydrogen peroxide in this species), and (2) lower concentrations of iron are present in O. leucostigma (providing greater protection of its midgut fluids from oxidative damage). Hydroxyl radical levels increased greatly in M. disstria, but not in O. leucostigma, when they consumed a tannin-containing diet, supporting the first hypothesis. Protein oxidation was also significantly increased in the midgut fluids of M. disstria that ingested tannic acid, consistent with hydroxyl radical damage. Contrary to the second hypothesis, similar concentrations of iron (70 microM) remained in solution or suspension in both species of caterpillars on an artificial diet. Over 90% of this iron appeared to be in the reduced (catalytically active) state in both species. We conclude that tree-feeding caterpillars protect their midgut fluids from oxidative damage caused by Fenton-type reactions by limiting the formation of peroxides, rather than by limiting the availability of reduced iron.

Analysis of Variance↗

Chemistry and function of vegetable polyphenols with high molecular weights.

Structure and function of polypehnols with high molecular weights (tannins) were briefly reviewed to better understand the significance of polyphenol-rich foods and beverages. In a survey of bioactive ellagiannins with a macrocyclic structure and/or a gluconic acid core, some new oligomeric ellagitannins (eucarpanins and elaeagnatins) have been found in species of Myrtaceae and Elaeagnaceae, and their structures were elucidated by spectroscopic and chemical methods. Cytotoxic activity against human oral tumor cell lines and antibacterial activity against Helicobacter pylori have been evaluated for the ellagitannins obtained from both plants, and related compounds. The macrocyclic dimers, oentothein B, camelliin B and woodfordin C showed a remarkable cytotoxicity against human oral squamous cell carcinoma, but not against normal cells. These active tannins induced apoptosis of tumor cells. A potent antibacterial activity against Helicobacter pylori was exhibited by monomeric ellagitannins such as tellimagrandin I and stricitinin.

Anti-Bacterial Agents↗

Chemical composition and antibacterial activities of lupin seeds extracts.

Determination of influence of lupin natural phenolic compounds on antibacterial properties of its seeds was carried out. Raw material were seeds of Lupinus albus, L. luteus, and L. angustifolius. The methods included the determination of the content of proteins, total phenolic compounds, free phenolic acids, and tannins as well as antibacterial properties with ethanol extracts. The content of total phenolic compounds was smaller in testas than in cotyledons and the highest levels are observed in bitter cultivars of Lupinus albus cv. Bac and L. angustifolius cv. Mirela. Lupin tannins mainly occurred in cotyledons of the white lupin, predominantly in the bitter cultivar Bac. Free phenolic acids were mainly found in testas. Only extracts from the testas displayed antibacterial properties, which excludes the possibility of alkaloid influence on the results. The results suggest that inhibition of test bacteria growth depended mainly upon the content of the total phenolic compounds.

Anti-Bacterial Agents↗

Tannic acid resistance in ruminal streptococcal isolates.

Tannin degrading isolates of Streptococcus spp. from rumen of non-adaptive cattle, when grown in BHI broth, were able to tolerate tannic acid upto a level of 50 g/l. An increase in lag period from 1.5 to 6 h was observed for the isolates in presence of increased concentration of tannic acid. In addition, the morphology of gram positive diplococci converted to an elongated chain of 40-50 cells with increasing tannic acid from 1 to 4%. Qualitatively, the tannase activity was found to be present in the isolates tested, indicating their potential of being a tannin degrader.

Animals↗

Characterisation of embalming materials of a mummy of the Ptolemaic era. Comparison with balms from mummies of different eras.

Gas chromatography-mass spectrometry has been used to determine the nature of organic materials used in mummification balms. A comparative analysis of samples taken from Egyptian mummies is developed. The results are given in two parts. First, it is shown that the chemical composition of the balm is practically independent of the part of the mummy from which it is taken. This study was done on a Ptolemaic mummy (circa 100 BC from the Guimet Museum in Lyon). Fats, beeswax, and diterpenic resins were the main components: they were found everywhere. Castor oil was also very often detected (in half of the samples). This particular fat is present in the balm inside the thorax but not in the skull. Moreover it is shown that a vegetable tannin was employed. Components indicative of vegetable tannin input (gallic acid and inositols) were found in seven samples out of eighteen, particularly close to the body and on the canopic pack of the heart. Secondly, some conclusions from a comparative study of the composition of balms from mummies of various social levels as well as of different Egyptian periods are reported. It is shown that beeswax was used as from very early times (XVIIIth dynasty). The mixture of beeswax, fats, and diterpenoid resins would appear to be more recent. The balms of three mummies dating from more recent Egyptian periods (XIXth to XXVth dynasty) were analysed. No evidence of a resin, gum-resin, or plant gum could be found. Some mummies would appear to have been embalmed with fats or beeswax. Finally, the entrails canopic pack said to belong to Ramses II undoubtedly shows an embalming process with a triterpenic resin of the mastic type. The adopted analytical methodology enabled us to achieve simultaneous detection of four components of the balm of the Ptolemaic mummy. Analysis of the other five mummies revealed far less complex chemical compositions for the balms. This may be an indication of different embalming processes, although we should bear in mind the question of organic matter preservation through the ages.

Castor Oil↗

Determining the binding affinities of phenolic compounds to proteins by quenching of the intrinsic tryptophan fluorescence.

The noncovalent binding of selected phenolic compounds (chlorogenic-, ferulic-, gallic acid, quercetin, rutin, and isoquercetin) to proteins (HSA, BSA, soy glycinin, and lysozyme) was studied by an indirect method applying the quenching of intrinsic tryptophan fluorescence. From the data obtained, the binding constants were calculated by nonlinear regression (one site binding; y = Bx/k + x). It has been reported that tannins inhibit human salivary amylase and that these complexes may reduce the development of cariogenic plaques. Further, amylase contains two tryptophan residues in its active site. Therefore, in a second part of the study involving 31 human subjects, evidence was sought for noncovalent interactions between the phenols of green tea and saliva proteins as measured by the fluorescence intensity. Amylase activity was determined before and after the addition of green tea to saliva of 31 subjects. Forty percent of the subjects showed an increase in amylase activity contrary to studies reporting only a decrease in activity. The interactions of tannin with amylase result in a decrease of its activity. It still remains to be elucidated why amylase does not react uniformly under conditions of applying green tea to saliva. Further, in terms of using phenols as caries inhibitors this finding should be of importance.

Amylases↗

Electron paramagnetic resonance studies of radical species of proanthocyanidins and gallate esters.

The polyphenols present in green tea or red wine comprise both regular flavon(ol)s and proanthocyanidins, i.e., derivatives of flavan-3-ols, whose distinct antioxidative potential is of great importance for explaining the beneficial effects of these nutrient beverages. Using EPR spectroscopy, we investigated radical structures obtained after oxidation of the parent compounds either by horseradish peroxidase/hydrogen peroxide or after autoxidation in moderately alkaline solutions. Both proanthocyanidins (monomers of condensed tannins, e.g., (+)-catechin, (-)-epicatechin, (-)-epicatechin gallate, (-)-epigallocatechin, (-)-epigallocatechin gallate, Pycnogenol) and gallate esters (hydrolyzable tannins, e.g., propylgallate, beta-glucogallin, pentagalloyl glucose and tannic acid) yielded predominantly semiquinone structures derived from the parent catechol or pyrogallol moieties. Evidence for a time-dependent oligomerization was obtained for (-)-epigallocatechin gallate, supporting our hypothesis that o-quinones formed from the initial semiquinone disproportionation are prone to nucleophilic addition reactions. Such phenolic coupling reactions would retain the numbers of reactive catechol/pyrogallol structures and thus the antioxidative potential. We therefore propose that proanthocyanidins are superior antioxidants as compared to flavon(ol)s proper, whose quinones are more likely to redox-cycle and act as prooxidants.

Anthocyanins↗

Histopathological effects of tannic acid on the midgut epithelium of some aquatic Diptera larvae.

The impact of tannins on larval Nematocera was investigated by an extensive survey of the relative toxicity of tannic acid in Diptera larvae representative of mosquito communities from alpine hydrosystems (Culicidae, Chaoboridae, Chironomidae, and Simuliidae) together with a nonindigenous vector competent Culicidae species. Bioassays indicate that exposure to tannic acid at concentrations from 0.25 to 4 mM is deleterious for Culex pipiens, Simulium variegatum, and Chironomus annularius, but not for Aedes, Anopheles, Culiseta, and Chaoborus species. Histopathological observations reveal that, among the target organs of tannic acid, mainly the midgut epithelium is affected by treatment. However, the extent of degeneration varies according to the taxon, the duration of the treatment, and the concentrations assayed. The vulnerability of epithelial cells differs among cell types, clear cells of the anterior midgut showing symptoms of intoxication before dark cells of the posterior midgut. The toxic effects of tannic acid are discussed, particularly in comparison to those of insecticidal bacteria, in order to evaluate the potential for use of tannins in the regulation of larval populations of dipteran pests.

Animals↗

The tonoplast, a specific marker of embryogenic microspores of Datura cultured in vitro.

Microspores of Datura metel L. have a thin tonoplast which, upon culture in vitro, develops a more or less uniform coating or deposit (as early as 12 h). This response was specific for embryogenic microspores, thereby making it possible to distinguish them from the nonembryogenic microspores. Cytochemical tests indicated the presence of tannins in this deposit which persists only until the early globular stage of embryogenesis. Thus tannin-coated tonoplasts can be used as a reliable and specific cytological marker for microspores following the embryogenic pathway in vitro.

Cells, Cultured↗

Physiochemical characteristics of flours of faba bean as influenced by processing methods.

Wet- and dry-processing with and without heating treatments were used to dehull faba beans for preparation of flours from the cotyledons. Flour qualities were assessed by levels of tannin and trypsin inhibitor and other measures of proximate composition. High roasting temperature and shorter process time that improved the recovered cotyledon yields were verified significant by path analysis methodologies. In turn, the higher cotyledon recoveries correlated with higher protein levels and inversely with the measured tannin levels. Ash reductions were correlated to the wet processing options in hull removal while reductions in the insoluble dietary fiber were notably influenced by level of heating temperatures applied. Trypsin inhibitor levels ranged from 42 to 56% of the original with reductions tied to applications of wet and/or heat processing in each case improved by increased durations and temperatures of treatments.

Chemical Phenomena↗

Production and chemical evaluation of some food condiments of Nigeria.

The study was aimed at investigating the nutrient and tannin composition of fermented legume seeds (oil bean, castor oil bean and African locust bean) used as food condiments in Nigeria. The legume seeds were purchased from local retailers, cleaned and subjected to varied fermentation periods. Standard assay techniques were adopted to analyze the parameters selected for use. The 4-day fermentation period caused the highest increases in protein and tannin and decreases in ash, lipids and non-protein nitrogen (NPN). The pulp of African locust bean had more protein an ash and the oil bean seeds less lipids and NPN. Fermentation times had varied effects on mineral levels. Fermentation for 4 d increased zinc, sodium and phosphorus except sodium for the African locust bean. The pulp had lower Zn and phosphorus than the seed. Fermentation for 4 d offers a greater advantage over other periods for production of nutritious and cheap food condiments in Nigeria.

Condiments↗

Common Indian spices: nutrient composition, consumption and contribution to dietary value.

Nutrient composition of eight commonly consumed spices of South India was analysed. Spices analysed were red chillies (Capsicum annum), black pepper (Piper nigrum), coriander seeds (Coriandrum sativum), cumin seeds (Cuminum cyminum), garlic (Allium sativum), asafoetida (Ferula foetida), dry ginger (Zingiber officinale) and ajowan (Carum copticum). The nutrients analysed were proximate principles, minerals, starch, sugars, dietary fibre components, tannins, phytic acid, enzyme inhibitors and amino acids. Dry ginger, ajowan and asafoetida had high calcium (1.0-1.5%) and iron (54-62 mg/100 g) levels. The tannin content of spices was also high (0.9-1.3% DM). Dietary fibre ranged from 14-53%. Spices had appreciable amounts of essential amino acids like lysine and threonine. A survey revealed the average per capita consumption of spices to be 9.54 g and at that level, the nutrient contribution from spices ranged from 1.2 to 7.9% of an average adult Indian male's requirement for different nutrients.

Amino Acids↗