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[The importance of concomitant compounds in plant extracts].

Plant extracts are multi-composed mixtures that can be subdivided into main active substances and concomitant compounds. Concomitant compounds are called co-effectors because they can change the physicochemical properties of the main active substances and therefore influence the biopharmaceutical parameters, e.g. solubility and bioavailability. The composition and the properties of plant extracts depend on a multitude of different factors such as quality and degree of reduction of the plant, and the process of extraction and drying. Concomitant compounds affect the physical and chemical stability of plant extracts. The hygroscopicity also depends on the composition of the concomitant compounds. It is an important property for the further processing of the plant extract to solid dosage form, e.g. tablets. Solubility and dissolution rate can be influenced by the concomitant compounds. Both properties are important for the absorption of the active substances though in many cases the responsible substances and mechanisms are still unknown. Solubilisation by surface-active agents, formation of soluble drug-concomitant compound-associates and solid dispersion, in which the drug is finely dispersed or X-ray amorphous, are often responsible for the increased solubility. Improved wettability in the presence of the concomitant compounds results in better dissolution. Supersaturated solutions of the active substances are stabilized for months by inhibition of crystallization. Numerous examples are known for influencing the absorption by natural concomitant compounds. The absorption is enhanced by the increased amount of dissolved drug or by the alteration of membrane permeability. Adsorption or complex formation with the concomitant compounds decrease the absorption rate, in some cases also the extent of absorption.

Animals↗

2,2-diphenyl-1-picrylhydrazyl (DPPH*) test demonstrates antiradical activity of Dorstenia psilurus and Dorstenia ciliata plant extracts.

Plants of the Dorstenia genus, used in traditional medicine and as food ingredient in Africa, are rich in polyphenolic compounds which can be involved in prevention of disease and food spoilage through their antioxidant activity. The antiradical activities of extracts of Dorstenia psilurus. D. ciliata and a phenolic compound (6-prenylapigenin) from D. ciliata were evaluated with the 2,2-diphenyl-1-picrylhydrazyl (DPPH*) test. D. psilurus chloroform and D. ciliata ethyl acetate extracts were shown to exhibit antiradical activities, with slow kinetic action. The efficient concentrations at different kinetic times "EC50,t" for the D. ciliata extract: 699, 479, 311 and 251 g/kg after 30, 60, 120 and 180 min, respectively, were always much lower than for the D. psilurus extract: 2341, 2312, 1672 and 1281 g/kg at the same times. The antiradical activity of 6-prenylapigenin was weak compared to the extracts. These results suggest the antioxidant activities of Dorstenia extracts and might help to understand their traditional use. We propose "EC50, t", calculated on the curves obtained with DPPH test, as a parameter to screen and compare antiradical activities of plant extracts with slow kinetic behaviour.

Antioxidants↗

Antiviral activity of some Nigerian medicinal plant extracts.

Plants from Northern Nigeria with a history of use in both human and veterinary traditional medicine have been investigated for their antiviral activity and their cytotoxicity determined. Extracts were tested against poliovirus, astrovirus, herpes simplex viruses and parvovirus, using the microtitre plate inhibition tests. Most of the extracts have activity against more than one virus at a dose rate of between 100 and 400 microg/100 microl.

Animals↗

Effect of plant extracts on physicochemical properties of chicken breast meat cooked using conventional electric oven or microwave.

This study evaluated effects of vacuum-infused fresh chicken breast meats with grape seed extracts, green tea extracts, or tertiary butyl hydroquinone on pH, texture, color, and thiobarbituric reactive substances after cooking using a microwave or conventional electric oven for 12 d storage at 5 degrees C. Thiobarbituric reactive substances values of uncooked (raw) chicken breast meats for 0 to 12 d of storage ranged from 1.12 to 3.5 mg of malonaldehyde/100 g of chicken. During 0 to 12 d of storage, thiobarbituric reactive substances values ranged from 2.50 to 7.80 and from 2.4 to 7.35 mg of malonaldehyde/100 g of chicken breast meat cooked by microwave and conventional electric oven, respectively. Meats cooked by microwave had higher redness and lower lightness values than those cooked by conventional electric oven. Also, meats cooked by microwave had higher maximum shear force, working of shear, hardness, springiness, cohesiveness, and chewiness values than meats cooked by conventional electric oven. Tertiary butyl hydroquinone was the most effective in raw and cooked meats in reducing lipid oxidation, followed by grape seed and green tea extracts. Plant extracts are effective in preventing undesirable changes in chemical properties in chicken breast meat caused by microwave and conventional electric oven cooking.

Animals↗

[Inhibitory effects of natural plant extracts on Verticillium albo-atrum].

This paper studied the inhibitory effects of 54 kinds of ethanol-extracted plant solutions on Verticillium albo-atrum. The results showed that 15 kinds of these extracts could inhibit the growth of verticillium albo-atrum mycelium, with an inhibitory rate more than 50%, among which, the inhibitory rate of Asarum sieboldii, Coptis chinensis, Magnolia officinalis, Acacia catechu, Sophora flavescens, Glycyrrhiza uralensis, Cnidium monnieri, Platycodon grandiflorum and Allium. cepa. extracts was higher than 65%, and that of Cnidium monnieri extract reached 86.84%. A total of 16 kinds of plant extracts decreased the spore germination of V. albo-atrum, with the inhibitory rate higher than 70%, and there were 7 kinds of plant extracts whose inhibitory rate reached 95%. Almost no spore bourgeon was found after treated with Asarum sieboldii, Coptis chinensis, and Magnolia officinalis extracts. The extract of Acacia catechu did not inhibit the growth of mycelium, but restrained the spore germination by 100%. Cnidium monnieri extract could strongly inhibit the growth of mycelium, but had a less effect on spore germination rate (only by 11.3%). The active substances found in natural plant extracts which had the inhibitory effects on pathogen brought us a new and promising method to deal with V. albo-atrum and other vegetable diseases.

Anti-Bacterial Agents↗

Treatment of trinitrotoluene by crude plant extracts.

Crude plant extract solutions (spinach and parrotfeather) were prepared and spiked with 2,4,6-trinitrotoluene (TNT) (20 mgl(-1)). 90-h TNT removal by these solutions was compared to controls. Spinach and parrotfeather extract solutions removed 99% and 50% of the initial TNT, respectively; TNT was not eliminated in the controls or in extract solutions where removal activity was deactivated by boiling. A first-order removal constant of 0.052 h(-1) was estimated for spinach extract solutions treating 20 mgl(-1) TNT concentrations, which compared favorably to intact plant removal. Concentration variation was described by Michaelis-Menton kinetics. Detectable TNT degradation products represented only a fraction of the total TNT transformed, and the transformation favored the formation of 4-aminodinitrotoluene. The results indicated that crude plant extracts transform TNT, without the presence of the live plant.

Biotransformation↗

Antiviral activity of south Brazilian medicinal plant extracts.

Brazilian plants are potential sources of useful edible and medicinal plants. Hydromethanolic extracts prepared from 54 medicinal plants used in folk medicine to treat infections were screened for antiviral properties against five different viruses (HSV-1, HSV-2, poliovirus type 2, adenovirus type 2 and VSV). Fifty-two percent of the plant extracts exhibited antiviral against one or more tested viruses. More specifically, 42.6% showed activity against HSV-1 (herpes simplex virus type 1), 42.6% against HSV-2 (herpes simplex virus type 2), 26% against poliovirus and 24% against VSV (vesicular stomatitis virus). None of the extracts was active against adenovirus. Trixis praestans (Vell.) Cabr. and Cunila spicata Benth. extracts were further characterized for antiviral activity.

Animals↗

A modified HET-CAM assay approach to the assessment of anti-irritant properties of plant extracts.

Hen's egg--chorioallantoic membranes were used to screen for and assess anti-irritant properties among aqueous extracts of plants (HET-CAM tests), in connection with searches for plant-derived substances with topical anti-irritant action. The main question to be answered was whether CAM-assay screening of plant extracts could provide a useful route to identifying promising anti-irritant extracts for follow-up clinical testing. To be useful, the method would have to flag materials with strong anti-irritant properties, and would have to avoid registering false negatives. The tests conducted provided positive indications. We measured the delays in onset of three manifestations of membrane irritation-vascular hemorrhaging, membrane lysis and membrane coagulation-observed with test substances relative to positive controls. Aqueous 15% lactic acid, a commonly used irritant in direct tests on human skin, was employed as the test irritant in this study. The ratio [irritation onset times after test substance pre-treatment]:[onset times without test substance pretreatment] was used to measure the anti-irritant power of test substances. A scoring notation was devised for this which treats the delay parameters as independent effects. Most tested plant extracts showed no significant irritant or anti-irritant effects. Among the apparently anti-irritant plant extracts (approx. 10% of all those tested), most showed their greatest effect against hemorrhaging. Lesser but still readily measurable effects against membrane lysis and coagulation were also observed in nearly all the apparently anti-irritant extracts. Two of the tested extracts proved to be membrane irritants. Some key CAM assay results were compared with results obtained in direct tests on human skin using the same test irritant (15% lactic acid). In these comparative tests on skin, an essentially similar pattern of efficacy was obtained, with the plant extract deemed best in the CAM screenings, outperforming the benchmark anti-irritant hydrocortisone. From these initial results it appears that physiological CAM assays may prove useful in screening natural materials for anti-irritant properties, as alternatives to mechanism-dependent biochemical assays, or expensive direct screening tests on human subjects. Further work remains to extend the CAM screening approach to irritants other than lactic acid, and to assess its quantitative powers of prediction of topical anti-irritancy.

Algorithms↗

Liquid chromatography combined with thermospray and continuous-flow fast atom bombardment mass spectrometry of glycosides in crude plant extracts.

In crude plant extracts, constituents of biological or pharmaceutical interest often exist in the form of glycosides. Off-line mass spectral investigations of these metabolites require soft ionisation techniques such as desorption chemical ionisation (DCI) or fast atom bombardment (FAB) if information on molecular mass or sugar sequence is desired. In LC-MS, glycosides can be ionised by using thermospray (TSP), continuous-flow fast atom bombardment (CF-FAB) or other interfaces. These techniques are thus potentially applicable to the on-line analysis of glycosides and can be applied to plant extract analysis. Thermospray (TSP) used with ammonium acetate as buffer provides mass spectra similar to those obtained with DCI-MS using NH3 and is potentially applicable to the on-line analysis of relatively small glycosides bearing no more than three sugar units. CF-FAB provides cleaner MS spectra than static FAB due to the lower concentration of the matrix used and can be applied to more polar compounds such as glycosides with a larger number of sugars. The use of a special setup involving post-column addition of the buffer or the matrix and splitting allows LC-UV, TSP LC-MS and CF-FAB LC-MS to be performed with the same standard HPLC conditions. Different crude plant extracts containing various types of glycosides with one to eight sugar units have been analysed by both TSP and CF-FAB. Cardenolides from Nerium odorum (Apocynaceae) and saponins from Swarzia madagascariensis (Leguminosae), Aster scaber and Aster tataricus (Asteraceae) have been studied by LC-MS. The combination of these two interfaces for the HPLC screening of crude plant extracts is discussed.

Cardenolides↗

Aflatoxin distribution in edible oil-extracting plants and in poultry feedmills.

The occurrence and distribution of aflatoxins B1, B2, G1 and G2 in the raw materials and products of three plants for extracting edible oils and in two poultry feedmills in which by-products of the oil extraction were used for feed formulation were investigated. While levels of aflatoxins were high in the products and by-products from the three extraction plants, the levels in the poultry feeds produced in the feedmills were found to be relatively low. The latter finding may reflect the proportion of pellets included in the feedstock formulation, while the climatic differences in the areas in which the extraction plants were situated were a possible factor in the differing levels of aflatoxin found in the samples from the three extraction plants.

Aflatoxins↗

Inhibition of low-density lipoprotein oxidation and up-regulation of low-density lipoprotein receptor in HepG2 cells by tropical plant extracts.

Twelve edible plant extracts rich in polyphenols were screened for their potential to inhibit oxidation of low-density lipoprotein (LDL) in vitro and to modulate LDL receptor (LDLr) activity in cultured HepG2 cells. The antioxidant activity (inhibition of LDL oxidation) was determined by measuring the formation of conjugated dienes (lag time) and thiobarbituric acid reagent substances (TBARS). Betel leaf (94%), cashew shoot (63%), Japanese mint (52%), semambu leaf (50%), palm frond (41%), sweet potato shoot, chilli fruit, papaya shoot, roselle calyx, and maman showed significantly increased lag time (>55 min, P < 0.05) and inhibition of TBARS formation (P < 0.05) compared to control. LDLr was significantly up-regulated (P < 0.05) by Japanese mint (67%), semambu (51%), cashew (50%), and noni (49%). Except for noni and betel leaf, most plant extracts studied demonstrated a positive association between antioxidant activity and the ability to up-regulate LDL receptor. Findings suggest that reported protective actions of plant polyphenols on lipoprotein metabolism might be exerted at different biochemical mechanisms.

Adult↗

Antihormonal effects of plant extracts: iodothyronine deiodinase of rat liver is inhibited by extracts and secondary metabolites of plants.

Aqueous extracts from plants such as Lycopus virginicus , Melissa officinalis ( Laminaceae ), and Lithospermum officinale ( Boraginaceae ), containing various antihormonal components, also inhibit both the extrathyroidal enzymic T4-5'-deiodination to T3 and the T4-5'-deiodination. The effects were dose dependent and ultimately complete using rat liver microsomes as a source of the enzyme in vitro. The "specific inhibitory activity" of extracts depends on the plant species used and the extraction procedure applied. It can be increased by either extraction of freeze dried aqueous extracts and decreased by oxidation with KMnO4. The active principle(s) exhibits chemical characteristics of phenols or phenolcarboxylic acids: rosmarinic acid, ellagic acid, and luteolin -7 beta-glucoside are active inhibitory components whilst other secondary plant metabolites consisting only of a single diphenolic ring e.g. cinnamic acid and derivatives are inactive. The inhibition of both iodothyronine-5'- and -5-deiodinase by this new class of iodine-free phenolic inhibitors--belonging to the cinnamic acid-flavonoid-type--supports the hypothesis that in rat liver only a single enzyme catalyses both deiodination pathways and might be of pharmacological interest for the treatment of hyperthyroidism.

Animals↗

The lipid lowering effect of an anti-diabetic plant extract.

An antidiabetic plant extract, in common use by Kuwaiti diabetics, was investigated for its hypolipidemic effect using both streptozotocin-induced diabetic and normal rats. The extract significantly decreased blood triglycerides under diabetic conditions only (p less than 0.01), while it decreased cholesterol in both normal (p less than 0.01) and diabetic rats (p less than 0.05). The hypolipidemia was accompanied by significant lowering of ketone bodies both in fasted normal and diabetic animals, in addition to decreasing free fatty acids in treated diabetic rats (p less than 0.005). Moreover, the extract prevented reduction in body weight observed in diabetic animals. In contrast to some other antidiabetic plant extracts, the present preparation seems to offer the additional benefit of lipid-lowering property.

3-Hydroxybutyric Acid↗