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Antimalarial activity of some Colombian medicinal plants.

Antimalarial activity of 10 vegetal extracts (9 ethanolic extracts and 1 crude alkaloid extract), obtained from eight species traditionally used in Colombia to treat malaria symptoms, was evaluated in culture using Plasmodium falciparum chloroquine resistant (FcB2) strain and in vivo on rodent malaria Plasmodium berghei. The activity on ferriprotoporphyrin biomineralization inhibition test (FBIT) was also assessed. Against Plasmodium falciparum, eight extracts displayed good activity Abuta grandifolia (Mart.) Sandwith (Menispermaceae) leaves, Acacia farnesiana (L.) Willd. (Mimosaceae) leaves, Acnistus arborescens (L.) Schltdl. (Solanaceae) aerial part, Croton leptostachyus Kunth (Euphorbiaceae) aerial part, Piper cumanense Kunth (Piperaceae) fruits and leaves, Piper holtonii C. DC. (Piperaceae) aerial part and Xylopia aromatica (Lam.) Mart. (Annonaceae) bark with IC(50) values ranging from <1 to 2.1 microg/ml, while in the in vivo model only Abuta grandifolia alkaloid crude extract exhibits activity, inhibiting 66% of the parasite growth at 250 mg/kg/day. In the FBIT model, five extracts were active (Abuta grandifolia, Croton leptostachyus, Piper cumanense fruit and leaves and Xylopia aromatica).

Animals↗

Evolution of Piperales--matK gene and trnK intron sequence data reveal lineage specific resolution contrast.

Piperales represent the largest basal angiosperm order with a nearly worldwide distribution. The order includes three species rich genera, Piper (ca. 2000 species), Peperomia (ca. 1500-1700 species), and Aristolochia s. l. (ca. 500 species). Sequences of the matK gene and the non-coding trnK group II intron are analysed for a dense set of 105 taxa representing all families (except Hydnoraceae) and all generic segregates (except Euglypha within Aristolochiaceae) of Piperales. A large number of highly informative indels are found in the Piperales trnK/matK dataset. Within a narrow region approximately 500 nt downstream in the matK coding region (CDS), a length variable simple sequence repeat (SSR) expansion segment occurs, in which insertions and deletions have led to short frame-shifts. These are corrected shortly afterwards, resulting in a maximum of six amino acids being affected. Furthermore, additional non-functional matK copies were found in Zippelia begoniifolia, which can easily be discriminated from the functional open reading frame (ORF). The trnK/matK sequence data fully resolve relationships within Peperomia, whereas they are not effective within Piper. The resolution contrast is correlated with the rate heterogeneity between those lineages. Parsimony, Bayesian and likelihood analyses result in virtually the same topology, and converge on the monophyly of Piperaceae and Saururaceae. Lactoris gains high support as sister to Aristolochiaceae subf. Aristolochioideae, but the different tree inference methods yield conflicting results with respect to the relationships of subfam. Asaroideae. In Piperaceae, a clade formed by the monotypic genus Zippelia and the small genus Manekia (=Sarcorhachis) is sister to the two large genera Piper and Peperomia.

Base Sequence↗

Jamu Gendong, a kind of traditional medicine in Indonesia: the microbial contamination of its raw materials and endproduct.

An examination on the microbiological quality of seven kinds of Jamu Gendong (JG) and their raw materials has been conducted according to the requirements of microbial contamination in traditional medicine, issued by the Department of Health of Indonesia in 1986. Samples of JG and their raw materials were taken from producers in three districts of Surabaya. The samples were subject to the following examinations: total plate count (TPC), MPN coliform, the enumeration of molds and yeasts, the presence or absence of Staphylococcus aureus, Salmonella and Vibrio. Each time the JG samples were taken from different producers together with their raw materials. The results of this investigation showed that most of the JG samples were heavily contaminated with bacteria, yeasts and molds. For bacteria, taken from the TPC results, their numbers were ranging from 7.7 x 10(2) microorganisms/ml to too many to count (TMTC). For yeasts and molds the numbers showed variations from 0 microorganisms/ml to TMTC. Contamination with Coliform in 1 ml of JG were ranged from 0 to > 2.4 x 10(6) microorganisms. In most of the samples pathogenic Staphylococci, Salmonella sp. and Vibrio sp. were not detected, so that a conclusion can be drawn that most of the contamination in JG are saprophytic, only a few pathogenic. The results also show that it is possible to have JG which fulfill the government's requirements. Similar results were obtained with the plant material constituents of JG such as rhizomes, leaves, herbs and fruits of Piper nigrum and Piper retrofractum, with the exception of Piper betle leaves and P. retrofractum fruits, both showing low contamination of Coliform bacteria. However, the fruits of Citrus aurantifolia and Morinda citrifolia were less contaminated, just like seeds of Oryza sativa, Parkia roxburghii, bulbs of Allium sativum and the pulp of Tamarindus indica. With these plant constituents of JG, it might be of interest to screen their antibacterial and antifungal activities.

Bacteria↗

Effect of an indigenous herbal compound preparation 'Trikatu' on the lipid profiles of atherogenic diet and standard diet fed Rattus norvegicus.

Combating heart disease is one of the challenging problems of biomedical science today. Towards this goal an indigenous preparation 'Trikatu' (a herbal combination containing Piper longum (fruit), Piper nigrum (fruit) and Zingiber officinale (rhizome) dry powder) was fed to normal and cholesterol fed male Rattus norvegicus to ascertain its efficacy as a hypolipidaemic agent. Its effects on body weight, blood and tissue (aortic, cardiac and hepatic) lipids--total, free and esterified cholesterol, low density lipoprotein(LDL) and high density lipoprotein(HDL) cholesterol, triglycerides and phospholipids--and the atherogenic index were measured. It was found that 'Trikatu' by virtue of its ability to reduce triglycerides and LDL cholesterol and to increase HDL cholesterol can reduce the risk of hyperlipidaemia and atherosclerosis. Hence 'Trikatu' can be used as a potent hypolipidaemic agent and it can reduce the atherosclerosis associated with a high fat diet.

Animals↗

Effect of piperine on the steady-state pharmacokinetics of phenytoin in patients with epilepsy.

Piperine, the active principle of Piper longum, Piper nigrum and Zingiber officinalis, has been reported to enhance the oral bioavailability of phenytoin in human volunteers. The objective of this study was to explore the effect of a single dose of piperine in patients with uncontrolled epilepsy on the steady-state pharmacokinetics of phenytoin. Two groups of 10 patients each receiving either a 150 mg or 200 mg twice daily dose of phenytoin were selected. Twelve hours after the night dose, venous blood samples were collected at 0, 0.5, 1, 2, 4, 6, 9, 12 h after administration of phenytoin. On the next study day, piperine 20 mg was administered along with phenytoin and samples were collected similarly. The mean plasma drug concentrations at different time points and the pharmacokinetic parameters before and after piperine administration were compared by Student's t-test. Piperine increased significantly the mean plasma concentration of phenytoin at most of the time points in both dose groups. There was a significant increase in AUC((0-12h)) (p < 0.01), C(max) (p < 0.001) and K(a) (p < 0.05) whereas the changes in K(el) and t(max) were not significant. The results showed that piperine enhanced the bioavailability of phenytoin significantly, possibly by increasing the absorption.

Adult↗

The in vitro anti-giardial activity of extracts from plants that are used for self-medication by AIDS patients in southern Thailand.

This study evaluated the anti-giardial activity of chloroform, methanol and water extracts of 12 medicinal plants (39 extracts), commonly used as self medication by AIDS patients in southern Thailand. The plant extracts and a standard drug, metronidazole, were incubated with 2x10(5) trophozoites of Giardia intestinalis per millilitre of growth medium in 96-well tissue culture plates under anaerobic conditions for 24 h. The cultures were examined with an inverted microscope and the minimum inhibitory concentration and the IC50 value for each extract was determined. The chloroform extracts from Alpinia galanga, Boesenbergia pandurata, Eclipta prostrata, Piper betle, Piper chaba, Zingiber zerumbet, and the methanol extracts from B. pandurata and E. prostrata were classified as "active", i.e. with an IC50 of <100 microg/ml, whereas the chloroform extract from Murraya paniculata was classified as being "moderately active". This study shows that extracts from some medicinal plants have potential for use as therapeutic agents against G. intestinalis infections.

Alpinia↗

Pharmacokinetic and pharmacodynamic studies on interaction of "Trikatu" with diclofenac sodium.

"Trikatu"-an Ayurvedic formulation comprising of a 1:1:1 ratio of dried fruits of Piper nigrum, Piper longum and dried rhizomes of Zingiber officinale is widely used to enhance the bioavailability of drugs, like vasicine, indomethacin, etc. The enhanced biological response might lead to alteration of therapeutic regimens of commonly prescribed drugs. The present work was aimed to study the effect of concomitant administration of Trikatu on the pharmacokinetics and pharmacodynamics of diclofenac sodium, a frequently prescribed non-steroidal anti-inflammatory drug, having a poor oral bioavailability (54 +/- 2%). The effect of Trikatu on the bioavailability profile of diclofenac sodium was studied in rabbits. It was observed that Trikatu significantly decreased the serum levels of diclofenac sodium. The pharmacodynamic study was carried out to evaluate the effect of Trikatu on the anti-inflammatory activity of diclofenac sodium using carragenin-induced rat paw edema model. It was observed that the mean percent edema inhibition shown by the combination of Trikatu and diclofenac was similar to that shown by Trikatu alone but significantly less than that shown by diclofenac alone. Thus, the experimental findings indicated that Trikatu pretreatment might decrease the bioavailability of certain drugs probably through a drug-herb interaction thereby adversely affecting the therapeutic efficacy of these drugs.

Administration, Oral↗

Advantages of soxflo extractions for phytochemical analysis and bioassay screening. 1. Terpenoids.

The Soxflo technique was evaluated for the rapid extraction of plant materials (<90 min) at room temperature. Qualitatively similar chromatograms were obtained by gas chromatography and thin layer chromatography (TLC) with Soxflo (SoF) and Soxhlet (SoL) extracts. Sequential solvent extractions by SoF gave slightly higher yields (132%) of five major sesquiterpenoids. TLC revealed that SoF extractions at room temperature were more selective as extracts contained compounds with a narrower range of R(f)() values. This means that the SoF technique offers the potential for one-step extractions and partial fractionation. This study also showed that there were large differences in the volatile composition of dried and fresh Piper fruits: dried fruits had predominantly sesquiterpenoids while fresh fruits had considerable quantities of both mono- and sesquiterpenoids. This is the first report of alpha-guaiene and alpha- and beta-selinene in Piper guineense fruits. It is suggested that the SoF technique can be useful for the screening of large numbers of plants for phytochemicals or for the preparation of plant extracts for subsequent bioassay studies.

Chromatography, Thin Layer↗

Antioxidant capacity of some herbs/spices from cameroon: a comparative study of two methods.

This study evaluates the antioxidant capacity of 14 herbs/spices from Cameroon. Freeze-dried samples extracted in methanol (free or unconjugated polyphenol) and in 1.2 M hydrochloric acid (HCl) in methanol (total antioxidant that is both unconjugated and conjugated) were analyzed using two different antioxidant assay methods [Folin-Ciocalteu reagent (Folin) and the ferric reducing antioxidant power (FRAP)]. The 1.2 M HCl in methanol extracts had significantly higher (P < 0.001) antioxidant capacities than the methanolic extract. Generally, the FRAP antioxidant values were significantly (P < 0.001) higher than the Folin antioxidant values. Although a significant correlation (P < 0.05) was obtained between the Folin phenol and the FRAP antioxidant, the trends of the antioxidant capacity of the samples were different for the Folin and FRAP methods. The leaves of the Piper species top the total antioxidant tables in both Folin and FRAP assay methods, respectively. Irvingia gabonensis tops the FRAP free antioxidant list, while Piper umbellatum leads the Folin free antioxidant followed by Thymus vulgaris. Thus, the antioxidant capacity of plant samples determined by different methods should be interpreted with caution. However, irrespective of the assay method used, the samples were rich in antioxidants.

Cameroon↗

Piperine modulates permeability characteristics of intestine by inducing alterations in membrane dynamics: influence on brush border membrane fluidity, ultrastructure and enzyme kinetics.

Piperine (1-Piperoyl piperidine) is a major alkaloid of Piper nigrum Linn. and Piper longum Linn. It is shown to possess bioavailability-enhancing activity with various structurally and therapeutically diverse drugs. The mechanism of enhancing the bioavailability, is, however, not understood. We hypothesize that piperine's bioavailability-enhancing property may be attributed to increased absorption, which may be due to alteration in membrane lipid dynamics and change in the conformation of enzymes in the intestine. Results of membrane fluidity studies using an apolar fluorescent probe, pyrene (which measures the fluid properties of hydrocarbon core), showed an increase in intestinal brush border membrane (BBM) fluidity. Piperine also stimulated Leucine amino peptidase and Glycyl-glycine dipeptidase activity, due to the alteration in enzyme kinetics. This suggests that piperine could modulate the membrane dynamics due to its apolar nature by interacting with surrounding lipids and hydrophobic portions in the protein vicinity, which may decrease the tendency of membrane lipids to act as stearic constrains to enzyme proteins and thus modify enzyme conformation. Ultra structural studies with piperine showed an increase in microvilli length with a prominent increase in free ribosomes and ribosomes on the endoplasmic reticulum in enterocytes, suggesting that synthesis or turnover of cytoskeletal components or membrane proteins may be involved in the observed effect. In conclusion, it is suggested that piperine may be inducing alterations in membrane dynamics and permeation characteristics, along with induction in the synthesis of proteins associated with cytoskeletal function, resulting in an increase in the small intestine absorptive surface, thus assisting efficient permeation through the epithelial barrier.

Alkaloids↗

Ingredients contribute to variation in production of reactive oxygen species by areca quid.

Areca quid (AQ) chewing has been implicated an independent risk factor for the development of oral cancer. Taiwanese areca quid (AQ) refers to a combination of areca nut (AN), lime, and inflorescence of Piper betle Linn. (IPB) or Piper betle leaf (PBL). Studies of AQ in other countries reported that AN extract combined with lime generates reactive oxygen species (ROS), such as hydroxyl radical (HO.), known to be a contributing factor in oral mucosa damage. To determine whether HO. is formed in the oral cavity during AQ chewing, the formation of meta-tyrosine (m-Tyr) and ortho-tyrosine (o-Tyr) from l-phenylalanine (Phe) was confirmed. It was demonstrated that combined aqueous extracts of AN, lime, metal ions (such as Cu2+ and Fe2+), and IPB or PBL produced HO.. Thus, the yield of HO. significantly increases when higher amounts of IPB or lime are added and also when Cu2+ and Fe2+ are increased. Further, the omission of any one of these ingredients significantly reduces the formation of HO.. Our results found that chewing AQ with IPB generated significantly higher HO. than chewing AQ with PBL, and may result in greater oxidative damage to the surrounding oral mucosa.

Adult↗

Biochemical properties of polysaccharides from black pepper.

The purified polysaccharides from Piper nigrum were prepared as follows: a hot water extract of pepper seeds was fractionated by ultrafiltration with a 5-kDa-membrane cartridge. A fraction with 5 kDa or bigger molecules was successively purified by open column chromatography on DEAE-Toyopearl 650C and Bio-gel P-60 with each active fraction, resulting in PN-Ib and PN-IIa, purified anti-complementary polysaccharides. None of the anti-complementary activity of any polysaccharide was changed by pronase digestion or polymyxin B treatment, but they were decreased by periodate oxidation. Analysis of component sugar and molecular mass determination of the anti-complementary polysaccharides indicated that PN-Ib with an average molecular mass of 21 kDa contained 88.5% glucose and other negligible minor monosaccharides, while PN-IIa showed a different monosaccharide composition, which contained a significant proportion of galactose, arabinose, galacturonic acid and rhamnose. The molar ratio of galactose and arabinose of PN-IIa (48 kDa) was 1.93:1. PN-1 did not react with beta-glucosyl Yariv reagent, however, PN-IIa did react, which indicated that PN-IIa might be an arabinogalactan. Based upon these results, the usefulness of purified anti-complementary polysaccharides from Piper nigrum is suggested as a supplement for immune enhancement.

Piper nigrum↗

Randomized controlled trial of modafinil for the treatment of fatigue in postpolio patients.

The purpose of this study was to test whether modafinil is effective in alleviating the symptoms of fatigue in postpolio patients, because it has been helpful for such symptoms in other neurologic disorders. Using a double-blind, randomized, placebo-controlled cross-over design, 14 postpolio patients with moderate to severe fatigue were assigned to receive modafinil or placebo first. Piper Fatigue Scale, Epworth Sleepiness Scale, digit span, and reaction time tests were done at baseline and then at weekly intervals. The Piper Fatigue Scale scores improved by 27 +/- 40% (mean +/- SD) following modafinil and by 43 +/- 36% following placebo. Scores for most of the other tests did not change during the study. Therefore, we conclude that modafinil was not effective in alleviating the symptoms of fatigue in postpolio patients.

Benzhydryl Compounds↗

Differential expression within a family of novel wound-induced genes in potato.

Wounding in higher plants leads to an increased synthesis of specific messenger RNAs. A cDNA clone complementary to a wound-induced message from potato tubers was used to isolate a lambda clone from a genomic library of Solanum tuberosum var. Maris Piper. DNA sequence analysis has shown that this single genomic clone contains two novel wound-induced genes, called win1 and win2, organised in close tandem array. The coding sequences of these two genes are highly homologous and are interrupted by a single intron. However, the sequences of the introns and flanking regions have diverged widely. Win1 and win2 encode cysteine-rich proteins of 200 and 211 amino-acids, respectively, which show striking homologies to several chitin-binding proteins. Southern analysis of genomic DNA has shown that win1 and win2 are members of a small multi-gene family which is estimated to have a minimum of five members per haploid genome of Maris Piper and appears to be conserved within the Solanaceae. We have shown by Northern analysis and S1 mapping that the two genes exhibit differential organ-specific expression after the wounding of a potato plant.

Amino Acid Sequence↗

Effect of muscle length on surface EMG wave forms in isometric contractions.

To elucidate the influence of muscle length on surface EMG wave form, comparisons were made of surface EMGs of the biceps and triceps brachii muscles during isometric contractions at different muscle lengths. Muscle lengths were altered by setting the elbow joint angle at several intervals between the limits of extension and flexion. The intensity of the isometric contractions was 25% of maximum voluntary contraction at the individual joint angles. Slowing was obvious in the EMG wave forms of biceps as muscle length increased. The so-called 'Piper rhythm' appeared when the muscle was more than moderately lengthened. The slowing trend with muscle lengthening, though less marked, was also seen in triceps. Zero-cross analysis revealed quasi-linear relationships between muscle length and slowing. Frequency analysis confirmed the development of 'Piper rhythm'. An attempt was made to interpret the slowing associated with muscle lengthening in terms of the propagation of myoelectric signals in muscle fibers. given the effect of muscle length on EMG wave forms, a careful control of joint angle may be required in assessing local making fatigue when using EMG spectral indices.

Adult↗

Cercaricidal activity of some essential oils of plants from Brazil.

Extended screening tests on the cercaricidal activity of various plants from northeast Brazil have shown that the extracts of the leaves and fruits of Piper marginatum, Protium heptaphyllum, and Capsicum annuum show a remarkable effect on the cercaria of Schistosoma mansoni. In the case of the oils of Piper marginatum and Capsicum annuum, 90--96% of the cercaria of Schistosoma mansoni were killed within 15 min. According to the NMR spectra, the active principles of the extracts seem to be water-soluble unsaturated compounds from the oils or their hydrolysis products. Natural substances provide an attractive alternative for preventive actions against schistosomiasis, as the perturbation of the ecological equilibrium of natural waters can be avoided in this manner.

Animals↗

Lipid composition of lesser known tropical seeds.

The lipid content and fatty acid profiles of four lesser known tropical seeds, Piper guineense, Chrysophyllum albidum, Garcinia kola and Dennettia tripetala, were determined. The total lipid content (g/kg dry weight) ranged between 31.8 and 68.9. The ranges of values for neutral lipids, triacylglycerol of neutral lipids, glycolipids and phospholipids were 17.3-58.0, 15.0-49.6, 3.0-7.2 and 3.7-11.2, respectively. The fatty acid profiles showed variation among different seeds. All the seeds contained substantial amounts of unsaturated fatty acids. Oleic and linoleic acids were the most abundant fatty acids. Dennettia tripetala and Piper guineense also contained moderate amounts of linolenic acid.

Africa↗

Field metabolic rates of phytophagous bats: do pollination strategies of plants make life of nectar-feeders spin faster?

Recently, it was argued that extrinsic factors, such as high foraging costs, lead to elevated field metabolic rates (FMR). We tested this suggestion by comparing the FMR of nectar-feeding and fruit-eating bats. We hypothesized that the foraging effort per energy reward is higher for nectar-feeding mammals than for fruit-eating mammals, since energy rewards at flowering plants are smaller than those at fruiting plants. Using the doubly labelled water method, we measured the FMR of nectar-feeding Glossophaga commissarisi and fruit-eating Carollia brevicauda, which coexisted in the same rainforest habitat and shared the same daytime roosts. Mass-specific FMR of G. commissarisi exceeded that of C. brevicauda by a factor of almost two: 5.3+/-0.6 kJ g(-1) day(-1) for G. commissarisi and 2.8+/-0.4 kJ g(-1) day(-1) for C. brevicauda. Since nectar-feeding bats imbibe nectar droplets of only 193 J energy content during each flower visit, a G. commissarisi bat has to perform several 100 flower visits per night to meet its energy requirement. The fruit-eating C. brevicauda, on the other hand, needs to harvest only 3-12 Piper infructescenses per night, as the energy reward per Piper equals ca. 6-30 kJ. We argue that the flowering and fruiting plants exert different selective forces on the foraging behaviour and energetics of pollinators and the seed dispersers, respectively. A comparison between nectar-feeding and non-nectar-feeding species in various vertebrate taxa demonstrates that pollinators have elevated FMRs.

Animals↗