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1.
Six amide-esters and two sulphur-containing bisamides were isolated from the leaves, stem and root bark of Aglaia tenuicaulis together with two bisamides from the leaves of A. spectabilis. Their structures were elucidated by spectroscopic methods. The co-occurrence of amide-esters and bisamides suggests close biosynthetic connections replacing only one nitrogen atom of putrescine with oxygen. Putrescine appears to be the common building block linked to various acids from which the cinnamoyl moiety represents the prerequisite for an incorporation of bisamides into flavaglines. Corresponding amide-esters are apparently not incorporated, but closely related amide-alcohol derivatives were found as part of benzopyran and benzofuran flavaglines. The structure of a amide-alcohol is described, representing an artifact due to hydrolysis of an amide-ester during TLC purification. A hypothetical amide-amine building block is suggested to form the characteristic pyrimidinone structures only found in benzofuran flavaglines. Structural and biosynthetic connections between amide-esters, bisamides and flavaglines are discussed and the chemotaxonomic significance of accumulating specific derivatives within the genus Aglaia is highlighted.  相似文献   

2.
Magnesium (Mg2+) is essential for enzymatic activity, brain function and muscle contraction. Blood Mg2+ concentrations are tightly regulated between 0.7 and 1.1 mM by Mg2+ (re)absorption in kidney and intestine. The apical entry of Mg2+ in (re)absorbing epithelial cells is mediated by the transient receptor potential melastatin type 6 (TRPM6) ion channel. Here, flavaglines are described as a novel class of stimulatory compounds for TRPM6 activity. Flavaglines are a group of natural and synthetic compounds that target the ubiquitously expressed prohibitins and thereby affect cellular signaling. By whole-cell patch clamp analyses, it was demonstrated that nanomolar concentrations of flavaglines increases TRPM6 activity by ∼2 fold. The stimulatory effects were dependent on the presence of the alpha-kinase domain of TRPM6, but did not require its phosphotransferase activity. Interestingly, it was observed that two natural occurring TRPM6 mutants with impaired insulin-sensitivity, TRPM6-p.Val1393Ile and TRPM6-p.Lys1584Glu, are not sensitive to flavagline stimulation. In conclusion, we have identified flavaglines as potent activators of TRPM6 activity. Our results suggest that flavaglines stimulate TRPM6 via the insulin receptor signaling pathway.  相似文献   

3.
Insecticidal flavaglines and other compounds from Fijian Aglaia species   总被引:5,自引:0,他引:5  
Bioassays with lipophilic crude extracts of four Fijian Aglaia species against Spodoptera littoralis displayed strong insecticidal activity for A. basiphylla and A. gracilis, whereas A. archboldiana and A. vitiensis did not have any significant effects. The insect toxicity of A. basiphylla was caused by the well known benzofuran flavaglines rocaglamide, desmethylrocaglamide and aglafoline. In contrast, A. gracilis contained four related pyrimidinone derivatives in the root and stem bark, including two new congeners named marikarin and 3'-hydroxymarikarin. Moreover, two new putrescine bisamides, secoodorine and secopiriferine, a new benzopyran flavagline. desacetylaglain A. and a new norsesquiterpene were isolated from the leaves together with three known bisamides and 3-hydroxy-5,7,4'-trimethoxyflavone. The structures of the new compounds were elucidated by spectroscopic methods. Comparative feeding assays within the active pyrimidinone flavaglines showed that the free hydroxy group in aromatic ring A of marikarin diminishes insecticidal activity.  相似文献   

4.
Chikungunya virus (CHIKV) is a re‐emerging mosquito‐borne alphavirus that recently caused large epidemics in islands in, and countries around, the Indian Ocean. There is currently no specific drug for therapeutic treatment or for use as a prophylactic agent against infection and no commercially available vaccine. Prohibitin has been identified as a receptor protein used by chikungunya virus to enter mammalian cells. Recently, synthetic sulfonyl amidines and flavaglines (FLs), a class of naturally occurring plant compounds with potent anti‐cancer and cytoprotective and neuroprotective activities, have been shown to interact directly with prohibitin. This study therefore sought to determine whether three prohibitin ligands (sulfonyl amidine 1 m and the flavaglines FL3 and FL23) were able to inhibit CHIKV infection of mammalian Hek293T/17 cells. All three compounds inhibited infection and reduced virus production when cells were treated before infection but not when added after infection. Pretreatment of cells for only 15 minutes prior to infection followed by washing out of the compound resulted in significant inhibition of entry and virus production. These results suggest that further investigation of prohibitin ligands as potential Chikungunya virus entry inhibitors is warranted.  相似文献   

5.
6.
Flavaglines and triterpenoids from the leaves of Aglaia forbesii   总被引:1,自引:0,他引:1  
Three structurally complex flavaglines of the cyclopenta[bc]benzopyran type, named desacetylpyramidaglains A, C, D (1-3), and the triterpene 23, 24, 25-trihydroxycycloartan-3-one (4) were isolated from the leaves of Aglaia forbesii together with the two rare pregnane steroids 2beta,3beta-dihydroxy-5alpha-pregn-17(Z)-en-16-one and 2beta,3beta-dihydroxy-5alpha-pregn-17(E)-en-16-one, as well as the bisamide pyramidatine, the sesquiterpene spathulenol, and the widespread triterpenoids lupeol, lupenone, and a mixture of beta-sitosterol and stigmasterol. Their structures were elucidated by 1D and 2D NMR spectroscopy and mass spectrometry. Compounds 3, 4, 5, and 6 were tested for antituberculosis and antiviral activity.  相似文献   

7.
In an attempt to determine the relationships between the plant profiles (country of collection, taxonomy, plant part) and the compound classes isolated with cytotoxic activity against a panel of human tumor cell lines, the data compiled from a 15-year anticancer drug-discovery project were subjected to an analysis of variance (ANOVA). The results indicate significant trends in cytotoxic activity relative to collection location, taxonomy, plant part, and compound classes isolated. Plant collections were made in tropical forests in six countries, with collections from Ecuador resulting in higher activity than those from Indonesia and Peru. Interestingly, collections from Florida were not statistically different than those from the countries with higher biodiversity. One hundred and forty-five families were represented in the collections, with the Clusiaceae, Elaeocarpaceae, Meliaceae, and Rubiaceae having low ED50 (half maximal effective dose) values. Especially active genera included Aglaia, Casearia, Exostema, Mallotus, and Trichosanthes. Roots and below-ground plant materials were significantly more active than above-ground materials. Cucurbitacins, flavaglines, anthraquinones, fatty acids, tropane alkaloids, lignans, and sesquiterpenoids were significantly more active than xanthones and oligorhamnosides. The results from this study should serve as a guide for future plant collection endeavors for anticancer drug discovery.  相似文献   

8.

Aims

The clinical use of doxorubicin for the treatment of cancer is limited by its cardiotoxicity. Flavaglines are natural products that have both potent anticancer and cardioprotective properties. A synthetic analog of flavaglines, FL3, efficiently protects mice from the cardiotoxicity of doxorubicin. The mechanism underlying this cardioprotective effect has yet to be elucidated.

Methods and Results

Here, we show that FL3 binds to the scaffold proteins prohibitins (PHBs) and thus promotes their translocation to mitochondria in the H9c2 cardiomyocytes. FL3 induces heterodimerization of PHB1 with STAT3, thereby ensuring cardioprotection from doxorubicin toxicity. This interaction is associated with phosphorylation of STAT3. A JAK2 inhibitor, WP1066, suppresses both the phosphorylation of STAT3 and the protective effect of FL3 in cardiomyocytes. The involvement of PHBs in the FL3-mediated cardioprotection was confirmed by means of small interfering RNAs (siRNAs) targeting PHB1 and PHB2. The siRNA knockdown of PHBs inhibits both phosphorylation of STAT3 and the cardioprotective effect of FL3.

Conclusion

Activation of mitochondrial STAT3/PHB1 complex by PHB ligands may be a new strategy against doxorubicin-induced cardiotoxicity and possibly other cardiac problems.  相似文献   

9.
On the origin of the Hirudinea and the demise of the Oligochaeta   总被引:10,自引:0,他引:10  
The phylogenetic relationships of the Clitellata were investigated with a data set of published and new complete 18S rRNA gene sequences of 51 species representing 41 families. Sequences were aligned on the basis of a secondary structure model and analysed with maximum parsimony and maximum likelihood. In contrast to the latter method, parsimony did not recover the monophyly of Clitellata. However, a close scrutiny of the data suggested a spurious attraction between some polychaetes and clitellates. As a rule, molecular trees are closely aligned with morphology-based phylogenies. Acanthobdellida and Euhirudinea were reconciled in their traditional Hirudinea clade and were included in the Oligochaeta with the Branchiobdellida via the Lumbriculidae as a possible link between the two assemblages. While the 18S gene yielded a meaningful historical signal for determining relationships within clitellates, the exact position of Hirudinea and Branchiobdellida within oligochaetes remained unresolved. The lack of phylogenetic signal is interpreted as evidence for a rapid radiation of these taxa. The placement of Clitellata within the Polychaeta remained unresolved. The biological reality of polytomies within annelids is suggested and supports the hypothesis of an extremely ancient radiation of polychaetes and emergence of clitellates.  相似文献   

10.
Data on the ontogeny of the posterior haptor of monogeneans were obtained from more than 150 publications and summarised. These data were plotted into diagrams showing evolutionary capacity levels based on the theory of a progressive evolution of marginal hooks, anchors and other attachment components of the posterior haptor in the Monogenea (Malmberg, 1986). 5 + 5 unhinged marginal hooks are assumed to be the most primitive monogenean haptoral condition. Thus the diagrams were founded on a 5 + 5 unhinged marginal hook evolutionary capacity level, and the evolutionary capacity levels of anchors and other haptoral attachement components were arranged according to haptoral ontogenetical sequences. In the final plotting diagram data on hosts, type of spermatozoa, oncomiracidial ciliation, sensilla pattern and protonephridial systems were also included. In this way a number of correlations were revealed. Thus, for example, the number of 5 + 5 marginal hooks correlates with the most primitive monogenean type of spermatozoon and with few sensillae, many ciliated cells and a simple protonephridial system in the oncomiracidium. On the basis of the reviewed data it is concluded that the ancient monogeneans with 5 + 5 unhinged marginal hooks were divided into two main lines, one retaining unhinged marginal hooks and the other evolving hinged marginal hooks. Both main lines have recent representatives at different marginal hook evolutionary capacity levels, i.e. monogeneans retaining a haptor with only marginal hooks. For the main line with hinged marginal hooks the name Articulon-choinea n. subclass is proposed. Members with 8 + 8 hinged marginal hooks only are here called Proanchorea n. superord. Monogeneans with unhinged marginal hooks only are here called Ananchorea n. superord. and three new families are erected for its recent members: Anonchohapteridae n. fam., Acolpentronidae n. fam. and Anacanthoridae n. fam. (with 7 + 7, 8 + 8 and 9 + 9 unhinged marginal hooks, respectively). Except for the families of Articulonchoinea (e.g. Acanthocotylidae, Gyrodactylidae, Tetraonchoididae) Bychowsky's (1957) division of the Monogenea into the Oligonchoinea and Polyonchoinea fits the proposed scheme, i.e. monogeneans with unhinged marginal hooks form one old group, the Oligonchoinea, which have 5 + 5 unhinged marginal hooks, and the other group form the Polyonchoinea, which (with the exception of the Hexabothriidae) has a greater number (7 + 7, 8 + 8 or 9 + 9) of unhinged marginal hooks. It is proposed that both these names, Oligonchoinea (sensu mihi) and Polyonchoinea (sensu mihi), will be retained on one side and Articulonchoinea placed on the other side, which reflects the early monogenean evolution. Except for the members of Ananchorea [Polyonchoinea], all members of the Oligonchoinea and Polyonchoinea have anchors, which imply that they are further evolved, i.e. have passed the 5 + 5 marginal hook evolutionary capacity level (Malmberg, 1986). There are two main types of anchors in the Monogenea: haptoral anchors, with anlages appearing in the haptor, and peduncular anchors, with anlages in the peduncle. There are two types of haptoral anchors: peripheral haptoral anchors, ontogenetically the oldest, and central haptoral anchors. Peduncular anchors, in turn, are ontogenetically younger than peripheral haptoral anchors. There may be two pairs of peduncular anchors: medial peduncular anchors, ontogentically the oldest, and lateral peduncular anchors. Only peduncular (not haptoral) anchors have anchor bars. Monogeneans with haptoral anchors are here called Mediohaptanchorea n. superord. and Laterohaptanchorea n. superord. or haptanchoreans. All oligonchoineans and the oldest polyonchoineans are haptanchoreans. Certain members of Calceostomatidae [Polyonchoinea] are the only monogeneans with both (peripheral) haptoral and peduncular anchors (one pair). These monogeneans are here called Mixanchorea n. superord. Polyonchoineans with peduncular anchors and unhinged marginal hooks are here called the Pedunculanchorea n. superord. The most primitive pedunculanchoreans have only one pair of peduncular anchors with an anchor bar, while the most advanced have both medial and lateral peduncular anchors; each pair having an anchor bar. Certain families of the Articulonchoinea, the Anchorea n. superord., also have peduncular anchors (parallel evolution): only one family, the Sundanonchidae n. fam., has both medial and lateral peduncular anchors, each anchor pair with an anchor bar. Evolutionary lines from different monogenean evolutionary capacity levels are discussed and a new system of classification for the Monogenea is proposed.In agreeing to publish this article, I recognise that its contents are controversial and contrary to generally accepted views on monogenean systematics and evolution. I have anticipated a reaction to the article by inviting senior workers in the field to comment upon it: their views will be reported in a future issue of this journal. EditorIn agreeing to publish this article, I recognise that its contents are controversial and contrary to generally accepted views on monogenean systematics and evolution. I have anticipated a reaction to the article by inviting senior workers in the field to comment upon it: their views will be reported in a future issue of this journal. Editor  相似文献   

11.
Zhou SQ 《Hereditas》2003,138(1):65-72
The aneuploidy of Gossypium hirsutum L. (upland cotton) aneusomatics were obtained by induced parthenogenesis. These aneuploids could grow and set seeds normally. In the process of meiosis there appeared large quantities of heteromorphic pairs and multivalent chromosomes and many cases of cytomixis and multisperm fertilization occurred. The aneuploids produced offsprings through sexual propagation. We explored penetratingly the questions how and why these aneuploids could survive. Through this research, we found that the upland cotton possessed an immense latent capacity to adapt to adverse environments. More importantly, in the case of the upland cotton, we discovered that the genetic pattern of the polyploid differs in some respects from that of the diploid.  相似文献   

12.
Ectogenesis, or the use of an artificial womb to allow a foetus to develop, will likely become a reality within a few decades, and could significantly affect the abortion debate. We first examine the implications for Judith Jarvis Thomson’s violinist analogy, which argues for a woman’s right to withdraw life support from the foetus and so terminate her pregnancy, even if the foetus is granted full moral status. We show that on Thomson’s reasoning, there is no right to the death of the foetus, and abortion is not permissible if ectogenesis is available, provided it is safe and inexpensive. This raises the question of whether there are persuasive reasons for the right to the death of the foetus that could be exercised in the context of ectogenesis. Eric Mathison and Jeremy Davis have examined several arguments for this right, doubting that it exists, while Joona Räsänen has recently criticized their reasoning. We respond to Räsänen’s analysis, concluding that his arguments are unsuccessful, and that there is no right to the death of the foetus in these circumstances.  相似文献   

13.
Summary 1. The material for this study is drawn from two sources, (a) investigations of the fish fauna in the inner Oslofjord between 1897 and 1967, (b) fish landing statistics available since 1872 at the Oslo fish market.2. The investigations of the fish fauna reveal that 4 species of fish — 2 sharks and 2 arctic bullheads — have disappeared from the deep waters of the Oslofjord where they were known to exist in 1897. We assume that unfavourable conditions, great changes in temperature or lack of oxygen in the stagnant deep water to which these species belonged have been injurious to their propagation and survival.3. The annual fluctuations in the landed quantities of fish are great, but nevertheless there exists a marked decreasing trend since about 1930; total landings in recent years are less than 1/10 of what they were 30 or 40 years ago.4. The fluctuations in the landings of cod, herring and mackerel are studied in some detail. Three periods (of 20 to 22 years' duration) from 1872 to 1932 show increasing average landings of cod: 44, 57, and 74 tons respectively; in the period 1933 to 1955 landings decreased to an average of 16 tons per year. The effect of fluctuating year classes is discussed.5. The landings of herring and mackerel were very good between 1911 and 1919 or 1920 with a maximum of 1500 tons of herring and 800 tons of mackerel. In the following years there was a trend of decrease with a few years of moderately good landings. Mature mackerels are immigrating into the fjord for feeding and spawning, while mature herrings, to a major extent, are supposed to belong to a local stock. The highest landings of both species are due to extremely great catches of young fish, and the success of the fishery in any one year, therefore, dependent of a successful spawning and hatching one ort two years before.6. In conclusion, the attention is drawn to the fact that there are reasons to believe that the profuse growth of bacteria in the polluted waters seems to be injurious to the hatching of fish eggs and to the survival of fish larvae (Dannevig 1945,Oppenheimer 1955).
Veränderungen der Fischfauna und der Fischerei des Oslofjords seit der Jahrhundertwende
Kurzfassung Das Material zu dieser Untersuchung stammt aus zwei Quellen: (a) vier Untersuchungen über die Fischfauna des Oslofjords im Zeitraum zwischen 1897 und 1967, und (b) Statistiken für den Zeitraum von 1872 bis 1964 über die Fischmengen, die im inneren Oslofjord gefangen und an die Fischhalle in Oslo geliefert worden sind. Ein Vergleich der Resultate mit den vier Untersuchungen über die Fischfauna zeigt, daß vier Arten von Tiefwasserfischen aus dem inneren Oslofjord völlig verschwunden sind, nämlichEtmopterus spinax, Somniosus microcephalus, Artediellus uncinatus undIcelus bicornis, die beiden zuletzt genannten wahrscheinlich schon vor 1930. Eine Anzahl anderer Arten, die früher häufig waren, sind jetzt selten. Statistische Erhebungen über die im Oslofjord gefangenen Fische lassen erkennen, daß die Erträge seit den zwanziger und dreißiger Jahren stark zurückgegangen sind. Gleichzeitig hat die Zahl der Fischer abgenommen. Es wird die Schlußfolgerung gezogen, daß die Veränderungen des Oslofjords sich besonders in den letzten 30 Jahren für mehrere Fischarten als schädigend erwiesen haben. Diese Auffassung wird unterstützt durch die Untersuchungen vonDannevig (1945) undOppenheimer (1955), die gezeigt haben, daß die reiche Bakterienflora des Oslofjords für die Entwicklung der pelagischen Fischeier schädlich ist.
  相似文献   

14.
A G Zara?ski? 《Ontogenez》1991,22(4):365-374
Experiments were performed using X. laevis embryos during gastrulation and neurulation (stages 10, 11 1/2, 12 1/2, 13 1/2, 15 and 18). Part of presumptive epidermis and lateral plate mesoderm was removed, and embryos raised until stage 25. The size of axial structures (notochord, somite mesoderm, central nervous system) was determined using serial histological sections and compared with that of control embryos. In experimental embryos, the size of axial structures was decreased. Until a specific stage of development, close correlation was found between the volume of embryonic compartment corresponding to a particular, structure and the volume of presumptive epidermis and lateral plate mesoderm. This stage is individual for each axial organ: middle gastrula (stage 11 1/2) for notochord, late gastrula (stage 12 1/2) for somite mesoderm, and late neurula (stage 18) for central nervous system. This data suggest that differentiation pattern of ecto-mesodermal rudiment is subject to regulation during gastrulation-neurulation, and subdivision of ectoderm and mesoderm into axial and non-axial tissues is a self-organizing process.  相似文献   

15.
The figure of tetrahedron is formed in certain species of Plectus and in Tobrilus gracilis at the stage of 4 blastomeres rather than a rhombus which is formed in most highly organized nematodes. The analysis of the Nematoda's embryogenesis allows to conclude that tetrahedron, rhombus as well as some other figures play the role of preblastula sustaining the most expedient disposition of the first blastomers for transition to the formation of the blastula. With the increasing organization of nematodas the tetrahedron preblastula turns into a rhombic, linear-rhombic and at last in aphelenchoid-tylenchoid one. The character of the distribution of structural elements of organs and tissues of the definitive animal in the cytoplasm of the egg of Plectus and Tobrilus confirms the rightness of the division of the class of nematodas into subclasses Enoplia and Chromadoria rather than subclasses Adenophorea and Secernentea.  相似文献   

16.
On the basis of analysis of the results of author's studies and literature data, theoretical notions are developed, according to which spatial-temporal organization of cortical biopotentials is a result of activity of nonspecific different level systems subtly regulating current alertness in conformity with needs of the actual and forthcoming activities. In the hierarchy of regulating systems, in conditions of alertness, nonspecific thalamic and midbrain system is leading. Activity of these regulation levels provides in alertness for formation and destruction of functional neuronal ensembles which realize elementary informational transformations. The role is emphasized of asynchronous processes in the central nervous system activity.  相似文献   

17.
Actin microfilaments and microtubules are important cytoskeletal proteins that regulate endothelial repair through alterations in cell shape and through regulation of cell migration following wounding of the endothelium. Upstream pathways have been identified in the regulation of actin and microtubule organization, especially small GTPases. Recently, there have been numerous proteins suggested to be capable of regulating interaction between microtubules and microfilaments to mediate microtubule regulation of endothelial repair, an important process in limiting injury to the artery wall and in reducing the extent of arterial disease. If disrupted, a rapid repair mechanism is important in reestablishing the integrity of the endothelium in order to reestablish its function as a macromolecular barrier, a thromboresistant surface, and a biologically active tissue. Strategies to improve repair should alter the pathobiology of the atherosclerotic plaque and thus improve the prognosis of patients with atherosclerosis.  相似文献   

18.
The investigation has been performed on the cat by means of the retrograde axonal transport of horseradish peroxidase method and luminescent markers. To the putamen along its rostro-caudal length and to all the segments projection fibers get only from the neurons of the basal nucleus of the amygdaloid body, greater number of the neurons projecting to the antero-ventral parts of the putamen than to the posterior ones. The problem on likeness in organization of the projections of the amygdaloid body and the caudate nucleus is discussed.  相似文献   

19.
Nearly 50 years have elapsed since Hayflick challenged the dogma that individual human cells were immortal by demonstrating that after a predictable number of cellular divisions, normal human fibroblasts eventually entered a state of permanent growth arrest [Hayflick L: The limited in vitro lifetime of human diploid cell strains. Exp Cell Res 1965, 37:614-636.; Hayflick L, Moorhead PS: The serial cultivation of human diploid cell strains. Exp Cell Res 1961, 25:585-621]. This growth arrest, referred to as senescence, was hypothesized to function as a tumor suppressive mechanism, capable of limiting the replicative capacity of an incipient tumor cell. While originally met with skepticism, the existence of senescence and its importance as a tumor suppressive mechanism is now accepted. Here, we highlight this work and introduce studies that indicate that while senescent cells themselves cannot produce a neoplasia, they possess the ability to promote the growth of nearby preneoplastic cells and in this way may contribute to age-related increases in tumor incidences. This added level of complexity suggests that senescence functions as a biological 'double edged sword.'  相似文献   

20.
On the diversity of the Cladocera in the tropics   总被引:20,自引:13,他引:7  
The mythical concept of an impoverished tropical cladoceran fauna is refuted. On a planetary scale, around half of the cladoceran species presently known occur exclusively in the tropics-subtropics, often with considerable restriction to particular geographical subzones. On a regional (political) scale, the situation is often unclear because of the continued fragmentary nature of studies, and because political units are not a good basis for biogeographical comparisons. At the finest level of resolution (lake-perlake comparisons), there appears to be an upper limit of c. 50 cladoceran species per individual lake. No significant difference between lakes in the temperate zone and in the tropics could be established here. Daphnia is largely absent from the tropics, but is replaced by more Sidids, Moinids, and Bosminids, such that the average cladoceran community in the limnetic zone of a tropical lake is not characterized by less species but rather by lower population densities. This, in turn, is considered a consequence of higher prevalent predation levels in the tropics.  相似文献   

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