177 research outputs found
Unified Angular Momentum of Dyons
Unified quaternionic angular momentum for the fields of dyons and
gravito-dyons has been developed and the commutation relations for dynamical
variables are obtained in compact and consistent manner. Demonstrating the
quaternion forms of unified fields of dyons (electromagnetic fields) and
gravito-dyons (gravito-Heavisidian fields of linear gravity), corresponding
quantum equations are reformulated in compact, simpler and manifestly covariant
way
Alkaloids from Indian medicinal plants and their biosynthesis
The chemical, pharmacological and biosynthetic status of alkaloids from plants which either have a reputation in folklore medicine or the extracts of which have shown consistent biological activity in a broad biological screen has been reviewed
Natural Voltage‐Gated Sodium Channel Ligands: Biosynthesis and Biology
Natural product biosynthetic pathways are composed of enzymes that use powerful chemistry to assemble complex molecules. Small molecule neurotoxins are examples of natural products with intricate scaffolds which often have high affinities for their biological targets. The focus of this Minireview is small molecule neurotoxins targeting voltage‐gated sodium channels (VGSCs) and the state of knowledge on their associated biosynthetic pathways. There are three small molecule neurotoxin receptor sites on VGSCs associated with three different classes of molecules: guanidinium toxins, alkaloid toxins, and ladder polyethers. Each of these types of toxins have unique structural features which are assembled by biosynthetic enzymes and the extent of information known about these enzymes varies among each class. The biosynthetic enzymes involved in the formation of these toxins have the potential to become useful tools in the efficient synthesis of VGSC probes.Terrific toxins: Living organisms produce highly potent small molecule neurotoxins as forms of self‐defense. A subset of these toxins target voltage‐gated sodium channels, a potential target for non‐opioid pain management in humans. The biosynthetic pathways of these channel‐disrupting ligands are discussed in the context of biocatalytic applications.Peer Reviewedhttps://deepblue.lib.umich.edu/bitstream/2027.42/149247/1/cbic201800754.pdfhttps://deepblue.lib.umich.edu/bitstream/2027.42/149247/2/cbic201800754-sup-0001-misc_information.pdfhttps://deepblue.lib.umich.edu/bitstream/2027.42/149247/3/cbic201800754_am.pd
Acyclic pyrazolo[3,4-d]pyrimidine nucleoside as potential leishmaniostatic agent
A new synthesis of 6-amino-1-hydroxyethoxymethyl-4 (5H)-oxopyrazolo[3, 4]pyrimidine (4) has been mentioned. Compound 4 exhibited inhibition of amastigotes of Leishmania donovani to the extent of 89% at 30 μg/mL, whereas iso-guanine analogue 5 had the inhibition only to the extent of 52.8% at 100 μg/mL in vitro. In hamster model the maximum inhibitory response for compound 4 against amastigotes multiplication was observed to be 94% at 50 Mug/kg single dose for 5 consecutive days
Synthesis of stacked compounds based on pyrazolo[3,4-d]pyrimidines as new flexible models for studying intramolecular aromatic π-π interactions (APPI)
754-75
Synthesis and high resolution proton NMR studies on isomeric N-1-IN-2-,5,7-trisubstituted-4,6-dioxo-4,5,6,7-tetrahydropyrazolo[3,4-d]pyrimidinest
1228-123
Kramers nodal line in the charge density wave state of YTe and the influence of twin domains
Recent studies have focused on the relationship between charge density wave
(CDW) collective electronic ground states and nontrivial topological states.
Using angle-resolved photoemission and density functional theory, we establish
that YTe is a CDW-induced Kramers nodal line (KNL) metal, a newly proposed
topological state of matter. YTe is a non-magnetic quasi-2D chalcogenide
with a CDW wave vector () of 0.2907c. Scanning tunneling
microscopy and low energy electron diffraction revealed two orthogonal CDW
domains, each with a unidirectional CDW and similar YTe. The effective band
structure (EBS) computations, using DFT-calculated folded bands, show excellent
agreement with ARPES because a realistic x-ray crystal structure and twin
domains are considered in the calculations. The Fermi surface and ARPES
intensity plots show weak shadow bands displaced by from the main
bands. These are linked to CDW modulation, as the EBS calculation confirms.
Bilayer split main and shadow bands suggest the existence of crossings,
according to theory and experiment. DFT bands, including spin-orbit coupling,
indicate a nodal line along the line from multiple band crossings
perpendicular to the KNL. Additionally, doubly degenerate bands are only found
along the KNL at all energies, with some bands dispersing through the Fermi
level
The Biosynthesis of Artemisinin (Qinghaosu) and the Phytochemistry of Artemisia annua L. (Qinghao)
The Chinese medicinal plant Artemisia annua L. (Qinghao) is the only known source of the sesquiterpene artemisinin (Qinghaosu), which is used in the treatment of malaria. Artemisinin is a highly oxygenated sesquiterpene, containing a unique 1,2,4-trioxane ring structure, which is responsible for the antimalarial activity of this natural product. The phytochemistry of A. annua is dominated by both sesquiterpenoids and flavonoids, as is the case for many other plants in the Asteraceae family. However, A. annua is distinguished from the other members of the family both by the very large number of natural products which have been characterised to date (almost six hundred in total, including around fifty amorphane and cadinane sesquiterpenes), and by the highly oxygenated nature of many of the terpenoidal secondary metabolites. In addition, this species also contains an unusually large number of terpene allylic hydroperoxides and endoperoxides. This observation forms the basis of a proposal that the biogenesis of many of the highly oxygenated terpene metabolites from A. annua - including artemisinin itself may proceed by spontaneous oxidation reactions of terpene precursors, which involve these highly reactive allyllic hydroperoxides as intermediates. Although several studies of the biosynthesis of artemisinin have been reported in the literature from the 1980s and early 1990s, the collective results from these studies were rather confusing because they implied that an unfeasibly large number of different sesquiterpenes could all function as direct precursors to artemisinin (and some of the experiments also appeared to contradict one another). As a result, the complete biosynthetic pathway to artemisinin could not be stated conclusively at the time. Fortunately, studies which have been published in the last decade are now providing a clearer picture of the biosynthetic pathways in A. annua. By synthesising some of the sesquiterpene natural products which have been proposed as biogenetic precursors to artemisinin in such a way that they incorporate a stable isotopic label, and then feeding these precursors to intact A. annua plants, it has now been possible to demonstrate that dihydroartemisinic acid is a late-stage precursor to artemisinin and that the closely related secondary metabolite, artemisinic acid, is not (this approach differs from all the previous studies, which used radio-isotopically labelled precursors that were fed to a plant homogenate or a cell-free preparation). Quite remarkably, feeding experiments with labeled dihydroartemisinic acid and artemisinic acid have resulted in incorporation of label into roughly half of all the amorphane and cadinane sesquiterpenes which were already known from phytochemical studies of A. annua. These findings strongly support the hypothesis that many of the highly oxygenated sesquiterpenoids from this species arise by oxidation reactions involving allylic hydroperoxides, which seem to be such a defining feature of the chemistry of A. annua. In the particular case of artemisinin, these in vivo results are also supported by in vitro studies, demonstrating explicitly that the biosynthesis of artemisinin proceeds via the tertiary allylic hydroperoxide, which is derived from oxidation of dihydroartemisinic acid.
There is some evidence that the autoxidation of dihydroartemisinic acid to this tertiary allylic hydroperoxide is a non-enzymatic process within the plant, requiring only the presence of light; and, furthermore, that the series of spontaneous rearrangement reactions which then convert thi allylic hydroperoxide to the 1,2,4-trioxane ring of artemisinin are also non-enzymatic in nature
Leishmanicidal activity and cytotoxicity of compounds from two Annonacea species cultivated in Northeastern Brazil
Cytisus scoparius link - A natural antioxidant
BACKGROUND: Recent investigations have shown that the antioxidant properties of plants could be correlated with oxidative stress defense and different human diseases. In this respect flavonoids and other polyphenolic compounds have gained the greatest attention. The plant Cytisus scoparius contains the main constituent of flavone and flavonals. The present study was undertaken to evaluate the in vitro antioxidant activities of extract of aerial part of Cytisus scoparius. METHODS: The plant extract was tested for DPPH (1, 1-diphenyl, 2-picryl hydrazyl) radical scavenging, nitric oxide radical scavenging, superoxide anion radical scavenging, hydroxyl radical scavenging, antilipid peroxidation assay, reducing power and total phenol content. RESULTS: The extract exhibited scavenging potential with IC(50 )value of 1.5 μg/ml, 116.0 μg/ml and 4.7 μg/ml for DPPH, nitric oxide and superoxide anion radicals. The values were found to lesser than those of vitamin C, rutin, and curcumin, as standards. The extract showed 50% protection at the dose of 104.0 μg/ml in lipid peroxidation induced by Fe(2+)/ ascorbate system in rat liver microsomal preparation. There is decrease in hydroxyl radical generation with IC(50 )value of 27.0 μg/ml when compared with standard vitamin E. The reducing power of the extract depends on the amount of extract. A significant amount of polyphenols could be detected by the equivalent to 0.0589 μg of pyrocatechol from 1 mg of extract. CONCLUSION: The results obtained in the present study indicate that hydro alcoholic extract of aerial part of Cytisus scoparius is a potential source of natural antioxidants
- …
