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Kinase inhibitors from Polygonum cuspidatum.

Bioassay-directed fractionation of a medicinal plant, Polygonum cuspidatum (Polygonaceae), has led to the discovery of a hydroxystilbene, resveratrol [1], as an inhibitor of a protein-tyrosine kinase (p56lck) partially purified from bovine thymus. Both trans and cis isomers of resveratrol possess comparable protein-tyrosine kinase inhibitory activity. Comparison of the IC50 values of resveratrol for protein-tyrosine kinase inhibitory activity with those of piceid (resveratrol-O3-beta-glucoside) [2] and resveratrol-O4'-beta-glucoside [3] shows the requirement of free hydroxyl groups on both phenyl rings for the protein-tyrosine kinase inhibition. Protein kinase C inhibitory analysis suggests the requirements of two free hydroxyl groups on one phenyl ring only.

Animals↗

Vanicosides A and B, protein kinase C inhibitors from Polygonum pensylvanicum.

Two new protein kinase C inhibitory glycosides, vanicosides A [1] and B [2] were isolated from Polygonum pensylvanicum (Polygonaceae) by chromatographic techniques guided by bioassays for PKC inhibition. The structures of these glycosides were established primarily by analysis of 1H- and homonuclear correlated nmr and high-resolution fab mass spectra of 1 and 2 and the derived octaacetate, 3. Both glycosides were found to have p-coumaryl esters at the 1, 3, and 6 carbons of sucrose and a feruloyl ester at the 6' carbon. Vanicoside A [1] also had an acetate group at the 2' carbon.

Acetylation↗

Galloyl esters from rhubarb are potent inhibitors of squalene epoxidase, a key enzyme in cholesterol biosynthesis.

Galloyl glucoses and galloyl proanthocyanidins obtained from rhubarb (Rhei Rhizoma, Rheum palmatum L., Polygonaceae); e.g. 1,2,6-tri-O-galloyl-beta-D-glucose (IC50 = 0.63 microM), 1,6-di-O-galloyl-2-O-cinnamoyl-beta-D-glucose (IC50 = 0.58 microM), procyanidin B-2 3,3'-di-O-gallate (IC50 = 0.54 microM), and procyanidin B-5 3,3'-di-O-gallate (IC50 = 0.55 microM), were found to be potent inhibitors of rat squalene epoxidase (SE). The inhibition at submicromolar level was far more potent than that of chemically synthesized substrate analogs. It was demonstrated for the first time that the cholesterol-lowering effect of rhubarb may be attributed to the potent inhibition activities of SE, a rate-limiting enzyme of cholesterol biogenesis.

Animals↗

Molecular phylogeny and character evolution of carnivorous plant families in Caryophyllales--revisited.

Recent phylogenetic analyses based on single gene and combined data sets have substantially increased our knowledge of the phylogeny of Caryophyllales s.l., indicating that additional carnivorous families are related to this alliance. In earlier contributions towards a reassessment of inter- and infrafamilial relationships slowly evolving genes had been preferred for phylogenetic inference. The resulting tree topologies based on rbcL and 18S rDNA, however, were characterized by limited resolution, low internal support and topological incongruence. Therefore genomic regions evolving more rapidly have been used in subsequent studies. Comparative sequencing of the matK gene and the flanking trnK intron region as well as combined analyses based on plastid matK, atpB, rbcL, and nuclear 18S rDNA have effectively improved resolution and internal support. Tree topologies revealed Caryophyllales s.l. as monophyletic group and indicated a clear division into two sister clades, the "core" and the "non-core" Caryophyllales (with Rhabdodendraceae and Simmondsiaceae with unclear affinities). Contrary to the "core" group (with Asteropeiaceae and Physenaceae as successive sister groups), which corresponds largely to the previous circumscription of the order, the monophyly of "non-core" Caryophyllales comprising Polygonaceae, Plumbaginaceae, Frankeniaceae, and Tamaricaceae along with the carnivorous families Droseraceae, Nepenthaceae, Drosophyllaceae, Dioncophyllaceae, and Ancistrocladaceae are a recent discovery. Based on reliable tree topologies it is hypothesized that pitfall traps of Nepenthes and snap traps typical for Aldrovanda and Dionaea were derived from a common ancestor with adhesive flypaper traps. With exception of Triphyophyllum carnivory was secondarily lost in the remaining Dioncophyllaceae (Dioncophyllum, Habropetalum) and all taxa of Ancistrocladaceae.

Animals↗

Antiviral activity of Rwandan medicinal plants against human immunodeficiency virus type-1 (HIV-1).

Selected plants used in Rwandan traditional medicine for the treatment of infections and/or rheumatoid diseases were investigated for antiviral activity in vitro against human immunodeficiency virus type-1 (HIV-1). Of the 38 tested 80% ethanolic extracts, belonging to plants of 21 different families only the extracts from the leaves of Aspilia pluriseta (Asteraceae) and Rumex bequaertii (Polygonaceae) had interesting selectivity indices (SI = ratio of the 50% cytotoxic concentration to the 50% effective antiviral concentration) higher than 1. Further fractionation of the initially antivirally inactive ethanolic extract of Tithonia diversifolia, however, led to an aqueous fraction with a high anti-HIV-1 activity (SI > 461), indicating that the cytotoxicity of some plant components may mask the antiviral properties of the active plant substances in total plant extracts.

Anti-HIV Agents↗

Studies on the psychopharmacological activities of Rumex nepalensis Spreng. root extract in rats and mice.

The methanol extract of Rumex nepalensis Spreng. (Family - Polygonaceae) was assessed for different psychopharmacological activities in rats and mice by evaluation of general behaviour, exploratory behaviour, muscle relaxant activity and phenobarbitone sodium-induced sleeping time. The extract at doses 200 mg/kg and above exhibited a reduction in spontaneous activity (general behavioural profile), a decrease in exploratory behavioural pattern in the Y-maze and Head-dip tests, a reduction in muscle relaxant activity in rotarod, 30 degrees inclined screen and traction tests, and also potentiated phenobarbitone sodium-induced sleeping time.

Animals↗

Historical climate change and speciation: neotropical seasonally dry forest plants show patterns of both tertiary and quaternary diversification.

Historical climate changes have had a major effect on the distribution and evolution of plant species in the neotropics. What is more controversial is whether relatively recent Pleistocene climatic changes have driven speciation, or whether neotropical species diversity is more ancient. This question is addressed using evolutionary rate analysis of sequence data of nuclear ribosomal internal transcribed spacers in diverse taxa occupying neotropical seasonally dry forests, including Ruprechtia (Polygonaceae), robinioid legumes (Fabaceae), Chaetocalyx and Nissolia (Fabaceae), and Loxopterygium (Anacardiaceae). Species diversifications in these taxa occurred both during and before the Pleistocene in Central America, but were primarily pre-Pleistocene in South America. This indicates plausibility both for models that predict tropical species diversity to be recent and that invoke a role for Pleistocene climatic change, and those that consider it ancient and implicate geological factors such as the Andean orogeny and the closure of the Panama Isthmus. Cladistic vicariance analysis was attempted to identify common factors underlying evolution in these groups. In spite of the similar Mid-Miocene to Pliocene ages of the study taxa, and their high degree of endemism in the different fragments of South American dry forests, the analysis yielded equivocal, non-robust patterns of area relationships.

Base Sequence↗

A novel role of water-soluble chlorophyll proteins in the transitory storage of chorophyllide.

All chlorophyll (Chl)-binding proteins involved in photosynthesis of higher plants are hydrophobic membrane proteins integrated into the thylakoids. However, a different category of Chl-binding proteins, the so-called water-soluble Chl proteins (WSCPs), was found in members of the Brassicaceae, Polygonaceae, Chenopodiaceae, and Amaranthaceae families. WSCPs from different plant species bind Chl a and Chl b in different ratios. Some members of the WSCP family are induced after drought and heat stress as well as leaf detachment. It has been proposed that this group of proteins might have a physiological function in the Chl degradation pathway. We demonstrate here that a protein that shared sequence homology to WSCPs accumulated in etiolated barley (Hordeum vulgare) seedlings exposed to light for 2 h. The novel 22-kD protein was attached to the outer envelope of barley etiochloroplasts, and import of the 27-kD precursor was light dependent and induced after feeding the isolated plastids the tetrapyrrole precursor 5-aminolevulinic acid. HPLC analyses and spectroscopic pigment measurements of acetone-extracted pigments showed that the 22-kD protein is complexed with chlorophyllide. We propose a novel role of WSCPs as pigment carriers operating during light-induced chloroplast development.

Adaptation, Physiological↗

An insect countermeasure impacts plant physiology: midrib vein cutting, defoliation and leaf photosynthesis.

One type of specialised herbivory receiving little study even though its importance has frequently been mentioned is vein cutting. We examined how injury to a leaf's midrib vein impairs gas exchange, whether impairment occurs downstream or upstream from injury, duration of impairment, compared the severity of midrib injury with non-midrib defoliation, and modelled how these two leaf injuries affect whole-leaf photosynthesis. Leaf gas exchange response to midrib injury was measured in five Asclepiadaceae (milkweed), one Apocynaceae (dogbane), one Polygonaceae and one Fabaceae species, which have been observed or reported to have midrib vein cutting injury in their habitats. Midrib vein injury impaired several leaf gas exchange parameters, but only downstream (distal) from the injury location. The degree of gas exchange impairment from midrib injury was usually more severe than from manually imposed and actual insect defoliation (non-midrib), where partial recovery occurred after 28 d in one milkweed species. Non-midrib tissue defoliation reduced whole-leaf photosynthetic activity mostly by removing photosynthetically active tissue, while midrib injury was most severe as the injury location came closer to the petiole. Midrib vein cutting has been suggested to have evolved as a countermeasure to deactivate induced leaf latex or cardenolide defences of milkweeds and dogbanes, yet vein cutting effects on leaf physiology seem more severe than the non-midrib defoliation the defences evolved to deter.

Analysis of Variance↗

Allergenic pollens and pollinosis in Italy: recent advances.

The authors have mapped the occurrence of allergenic pollens throughout Italy and defined their most common clinical symptoms. To obtain an accurate aerobiological and clinical picture of such a geographically complex country as Italy, a detailed investigation was carried out involving 80 data-gathering stations and 40 clinical centers nationwide. Three main pollination periods can be distinguished: winter-pre-spring (January to March) for Betulaceae, Corylaceae, Cupressaceae, Salicaceae and Ulmaceae: spring-summer (April to June) for Gramineae, Urticaceae, Oleaceae, Plantago, Fagaceae, Pinaceae and Polygonaceae, and summer-autumn (August to September) for Urticaceae, Compositae and Chenopodiaceae. Examination of 49,660 patients affected by pollinosis (conjunctivitis, rhinitis, asthma, with positive skin tests or IgE-specific serum determination: RAST, ELISA) throughout Italy revealed sensitivity to Gramineae in 64.6%, to Parietaria in 36.7% to Olea in 15.8%, to Compositae in 13.2%, to Betulaceae-Corylaceae in 7% and to Fagaceae-Cupressaceae-Plantago in 4%-10%; marked regional variations were observed. The patients suffered from rhino-conjunctivitis (55.7%), rhino-conjunctivitis plus asthma (31.6%) and asthma (12.7%). In monosensitised individuals, Parietaria was seen to be the main cause of the asthmatic syndrome (though our preliminary data also implicate Olea) followed by Gramineae.

Air Pollution↗

Genetic diversity in populations of plants with different breeding and dispersal strategies in a free-flowing boreal river system.

We have studied the genetic diversity of three plant species: Angelica archangelica (Apiacieae), Bistorta vivipara (Polygonaceae) and Viscaria alpina (Caryophyllaceae) along the free-flowing Vindel River in northern Sweden. The plants differ in reproductive strategy. A archangelica and V. alpina are insect pollinated outbreeders while B. vivipara reproduces with apomixis through bulbils. The seeds of A. archangelica may float for over a year, while the propagules (seeds and bulbils, respectively) of V. alpina and B. vivipara float for less than two days. Genetic diversity was assessed using starch gel electrophoresis. The clonal diversity of B. vivipara measured by Simpson's index (D) ranged between 0.78 and 0.99. Only a few clones were shared between localities. The average percentages polymorphic loci and mean He based on polymorphic loci for V. alpina over all localities were 23.1 and 0.15, respectively. Wright's F-statistics showed a significant overall deficit of heterozygotes. The diversity of A. archangelica was found to increase downstream. Genetic diversity of each species is sufficiently high to be used in studies on hydrochory. Dispersal appears to be related to the floating ability of progagules.

Genes, Plant↗

Anthelmintic properties of Polygonum glabrum.

A pure anthelmintic substance (PGA) has been isolated from the methanol-aqueous extract of the leaf of Polygonum glabrum Willd., a semi-aquatic Sudanese species of the family Polygonaceae. The antiparasitic in-vitro activity of several fractions isolated from the plant, has been examined comparatively with that of PGA. PGA also showed molluscicidal activity against Biomphalaria glabrata and Limnea truncatula Müll. Structural determination of PGA was attempted following data analysis of UV, IR, 13C NMR, 1H NMR and MS spectra and suggests that PGA is a terpenoid.

Animals↗

Anti-inflammatory activity of Polygonum bistorta, Guaiacum officinale and Hamamelis virginiana in rats.

The aqueous ethanolic extracts of Polygonum bistorta L. Polygonaceae, Guaiacum officinale L. Zygophyllaceae and Hamamelis virginiana L. Hamamelidaceae were screened for anti-inflammatory activity. Administered (100 and 200 mg kg-1, p.o.) before the induction of carrageenan rat paw oedema, extracts of P. bistorta significantly suppressed both the maximal oedema response and the total oedema response (monitored as area under the time course curve). H. virginiana was inactive and G. officinale was only active at 200 mg kg-1. At 200 mg kg-1 administered before the induction of adjuvant arthritis, P. bistorta significantly inhibited both the acute and chronic phases of the adjuvant-induced rat paw swelling, while G. officinale and H. virginiana were only active against the chronic phase. Further studies on P. bistorta (100-800 mg kg-1) revealed a dose-dependent inhibition of the carrageenan-induced rat paw oedema over the dose range 100-400 mg kg-1, the E50 value being approximately 158.5 mg kg-1. The extract (200 mg kg-1), administered after the onset of the inflammatory responses reversed the course of both the carrageenan- and adjuvant-induced rat paw swelling. The results confirm that the extracts of P. bistorta, G. officinale and H. virginiana contain anti-inflammatory substances.

Animals↗

Ethnomedicine in Himalaya: a case study from Dolpa, Humla, Jumla and Mustang districts of Nepal.

Traditional plant use in Nepal has been documented for millennia. The importance of plants as medicine has not diminished in any way in recent times, and traditional medicines are still the most important health care source for the vast majority of the population. This paper examines the ethnobotany and traditional use of plants extracted from the vulnerable alpine zone in the Dolpa, Humla, Jumla and Mustang districts of Nepal. The results of this ethnobotanical study indicate that a very large number of plant species is used as traditional medicines. There were 107, 59, 44 and 166 species of ethnomedicinal importance in surveyed areas of Dolpa, Humla, Jumla and Mustang district respectively. Of these, 84 common species, used at least in two districts, were selected to enumerate their ethnomedicinal properties. The 84 species belonged to 75 genera and 39 families. The commonest species in this pharmacopoeia were: Allium wallichii, Cordyceps sinensis, Dactylorhiza hatagirea, and Rheum australe. A total of 21 species were most common in three districts and 59 in two districts. The genera Aconitum, Allium, Arisaema, Berberis, Corydalis, Gentiana, Hippophae, Juniperus and Rhododendron each possessed two species with ethnomedicinal use. Labiatae was the most medicinally important family with five species used, followed by Araceae, Compositae, Liliaceae, Polygonaceae, Ranunculaceae, Scrophulariaceae and Umbelliferae, each contributing four species.

Conservation of Natural Resources↗

Antimycobacterial agents from selected Mexican medicinal plants.

As part of the ICBG program Bioactive Agents from Dryland Biodiversity of Latin America, the present investigation was undertaken to explore the possible antimycobacterial potential of compounds derived from selected Mexican medicinal plants. Bioassay-guided fractionation of the crude extracts of Rumex hymenosepalus (Polygonaceae), Larrea divaricata (Zygophyllaceae), Phoradendron robinsonii (Loranthaceae) and Amphipteryngium adstringens (Julianiaceae) led to the isolation of several antimycobacterial compounds. Four stilbenoids, two flavan-3-ols and three anthraquinones were isolated from R. hymenosepalus. Two flavonols and nordihydroguaiaretic acid were obtained from L. divaricata. Sakuranetin was the antimycobacterial agent isolated from P. robinsonii. Two known triterpenoids and the novel natural product 3-dodecyl-1,8-dihydroxy-2-naphthoic acid were obtained from A. adstringens. In general, the isolates were identified by spectral means. The antimycobacterial activity of the secondary compounds isolated from the analysed species, as well as that of nine pure compounds previously isolated in our laboratories, was investigated; the MIC values ranged from 16 to 128 microg mL-1. Among the tested compounds, the glycolipids, sesquiterpenoids and triterpenoids showed the best antimycobacterial activity. The antimycobacterial property of the glycolipids is reported for the first time. Although the tested compounds showed moderate antimycobacterial activity, their presence in the analysed species provides the rationale for their traditional use in the treatment of tuberculosis.

Anti-Bacterial Agents↗

Ontogenesis of the attachment ability in the bug Coreus marginatus (Heteroptera, Insecta).

Each tarsus of Coreus marginatus L. (Coreidae) bears a pair of smooth flexible pulvilli adapted for attachment to relatively smooth surfaces, such as their host plant Rumex crispus L. (Polygonaceae). This account quantifies insect attachment abilities on smooth surfaces at various stages of ontogenesis. Friction (shear) force (FF) of adults and juvenile insects was measured by the use of a computer controlled centrifugal force tester equipped with a fibre optical sensor. Pad area, body size and body mass were determined individually for each experimental insect. Light microscopy revealed no difference in pulvilli area between different leg pairs. Pulvilli area demonstrated a stronger increase with increasing linear dimensions, as predicted by scaling laws. Since friction coefficient (relationship between FF and body weight) (FC) was always higher than 1, it was concluded that adhesion has strongly contributed to the measured friction. The frictional properties of pulvilli do not change during ontogenesis. Thus, only the growth of pulvilli and, therefore, the increased contact area, contribute to the increasing attachment ability in insects at later larval stages. Due to different scaling of the body mass and area of attachment organs, smaller insects attach relatively more strongly. Both FF and FC were higher in experiments in which higher angular acceleration (AC) was applied. Lateral tenacity determined individually for experimental insects and pooled for all animals and accelerations is 0.097 N m(-2). These data led us to suggest that viscosity of the pad secretion and/or visco-elastic properties of the foam-like material of pulvilli play an important role in the attachment ability of insects.

Animals↗

Metabolism of rhaponticin and chrysophanol 8-o-beta-D-glucopyranoside from the rhizome of rheum undulatum by human intestinal bacteria and their anti-allergic actions.

Rhaponticin and chrysophanol 8-o-beta-D-glucopyranoside isolated from the rhizomes of Rheum undulatum (Family Polygonaceae) are metabolized to rhapontigenin and chrysophanol, respectively, by human intestinal microflora. Most intestinal bacteria isolated from human feces catalyzed these metabolic pathways. Among rhaponticin and chrysophanol 8-o-beta-D-glucopyranoside and their metabolites, rhapontigenin had the most potent inhibitory activity on a hyaluronidase, a histamine release from mast cell and passive cutaneous anaphylaxis (PCA) PCA reaction. The inhibitory activity of rhapontigenin was more potent than that of disodium cromoglycate, one of the commercial anti-allergic drugs. These results suggest that rhaponticin in the rhizomes of R. undulatum is a prodrug that has an extensive anti-allergic property.

Animals↗

Antimutagenicity and cytotoxicity of the constituents from the aerial parts of Rumex acetosa.

Four anthraquinones isolated for the first time from the aerial parts of Rumex acetosa (Polygonaceae), a Korean and a Japanese medicinal plant, and two synthetic derivatives were examined for their cytotoxicities against five cultured human tumor cell lines, i.e. A549 (non-small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCY15 (colon), using the Sulfrhodamine-B method in vitro and antimutagenic activities by Ames test with Salmonella typhimurium TA98 and TA100 and SOS chromotest with E. coli PQ37. Among the tested compounds, emodin strongly inhibited the proliferation of each examined tumor cell line with IC50 values ranged from 2.94 to 3.64 microg/ml and showed potent antimutagenic activities with 71.5% and 53.3% at the concentration of 0.1 mg/plate against the mutagens, NPD and sodium azide, respectively. Its antigenotoxic activity was also very effective at the final concentration of 10 microg/reaction tube against the mutagens, MNNG and NQO by SOS chromotest, reducing the induction factors by 19.6% and 43.5%, respectively. The structure-activity correlation study suggests that an additional OH group at C-6 position in the anthraquinone nucleus may play an important role for their cytotoxicities and an introduction of OH- or OCH3 group at C-6 position is necessary for their antimutagenicities.

Animals↗