scholarly journals Potential Anti-Acetylcholinesterase Activity of Cassia timorensis DC.

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4545
Author(s):  
Nurul Amira Nurul Azman ◽  
Maram B. Alhawarri ◽  
Mira Syahfriena Amir Rawa ◽  
Roza Dianita ◽  
Amirah Mohd Gazzali ◽  
...  

Seventeen methanol extracts from different plant parts of five different Cassia species, including C. timorensis, C. grandis, C. fistula, C. spectabilis, and C. alata were screened against acetylcholinesterase (AChE). C. timorensis extracts were found to exhibit the highest inhibition towards AChE whereby the leaf, stem, and flower methanol extracts showed 94–97% inhibition. As far as we are aware, C. timorensis is one of the least explored Cassia spp. for bioactivity. Further fractionation led to the identification of six compounds, isolated for the first time from C. timorensis: 3-methoxyquercetin (1), benzenepropanoic acid (2), 9,12,15-octadecatrienoic acid (3), β-sitosterol (4), stigmasterol (5), and 1-octadecanol (6). Compound 1 showed moderate inhibition towards AChE (IC50: 83.71 μM), while the other compounds exhibited poor to slightly moderate AChE inhibitory activity. Molecular docking revealed that the methoxy substitution of 1 formed a hydrogen bond with TYR121 at the peripheral anionic site (PAS) and the hydroxyl group at C5 formed a covalent hydrogen bond with ASP72. Additionally, the OH group at the C3′ position formed an interaction with the protein at the acyl pocket (PHE288). This possibly explains the activity of 1 in blocking the entry of acetylcholine (ACh, the neurotransmitter), thus impeding the hydrolysis of ACh.

1984 ◽  
Vol 49 (8) ◽  
pp. 1780-1787 ◽  
Author(s):  
Štefan Kučár ◽  
Juraj Zámocký ◽  
Juraj Zemek ◽  
Dušan Anderle ◽  
Mária Matulová

Partial hydrolysis of per-O-acetyl- and per-O-benzoyl derivatives of 1,6-anhydro-β-D-glucopyranose with methanolic hydrogen chloride and hydrazine hydrate was investigated. The acyl group at C(3) is of substantial influence on the course of hydrolysis. The esterified hydroxyl group at C(3) was found to be most stable on acid hydrolysis with methanolic hydrogen chloride when compared with that at C(2), or C(4); on the other hand, this ester group is the most labile upon hydrolysis with hydrazine hydrate. Selectivity of the respective ester groups towards hydrolysis made it possible to prepare all variations of acetyl and benzoyl derivatives of 1,6-anhydro-β-D-glucopyranose.


2020 ◽  
Author(s):  
Emine Salamci ◽  
Yunus Zozik

The efficient synthesis of two new stereoisomeric 3-aminocyclooctanetriols and new halocyclitol derivatives of them starting from cis,cis-1,3-cyclooctadiene are reported. Reduction of cyclooctene endoperoxide, obtained by photooxygenation of cis,cis-1,3-cyclooctadiene, with zinc yielded a cyclooctene diol followed by acetylation of the hydroxyl group, which gave dioldiacetate by OsO4/NMO oxidation. The cyclooctane dioldiacetate prepared was converted to the corresponding cyclic sulphate via the formation of a cyclic sulphite in the presence of catalytic RuO4. Reaction of this cyclic sulphate with a nucleophilic azide followed by the reduction of the azide group provided the target, 3-aminocyclooctanetriol. The second key compound, bromotriol, was prepared by epoxidation of the cyclooctene diol with m-chloroperbenzoic acid followed by hydrolysis with HBr(g) in methanol. Treatment of bromotriol with NaN3 and the reduction of the azide group yielded the other 3-aminocyclooctanetriol desired. Hydrolysis of the epoxides with HCl(g) in methanol gave stereospecifically new chlorocyclooctanetriols.


Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2594
Author(s):  
Maram B. Alhawarri ◽  
Roza Dianita ◽  
Khairul Niza Abd Razak ◽  
Suriani Mohamad ◽  
Toshihiko Nogawa ◽  
...  

Despite being widely used traditionally as a general tonic, especially in South East Asia, scientific research on Cassia timoriensis, remains scarce. In this study, the aim was to evaluate the in vitro activities for acetylcholinesterase (AChE) inhibitory potential, radical scavenging ability, and the anti-inflammatory properties of different extracts of C. timoriensis flowers using Ellman’s assay, a DPPH assay, and an albumin denaturation assay, respectively. With the exception of the acetylcholinesterase activity, to the best of our knowledge, these activities were reported for the first time for C. timoriensis flowers. The phytochemical analysis confirmed the existence of tannins, flavonoids, saponins, terpenoids, and steroids in the C. timoriensis flower extracts. The ethyl acetate extract possessed the highest phenolic and flavonoid contents (527.43 ± 5.83 mg GAE/g DW and 851.83 ± 10.08 mg QE/g DW, respectively) as compared to the other extracts. In addition, the ethyl acetate and methanol extracts exhibited the highest antioxidant (IC50 20.12 ± 0.12 and 34.48 ± 0.07 µg/mL, respectively), anti-inflammatory (92.50 ± 1.38 and 92.22 ± 1.09, respectively), and anti-AChE (IC50 6.91 ± 0.38 and 6.40 ± 0.27 µg/mL, respectively) activities. These results suggest that ethyl acetate and methanol extracts may contain bioactive compounds that can control neurodegenerative disorders, including Alzheimer’s disease, through high antioxidant, anti-inflammatory, and anti-AChE activities.


2012 ◽  
Vol 39 (2) ◽  
pp. 217-233 ◽  
Author(s):  
J. David Archibald

Studies of the origin and diversification of major groups of plants and animals are contentious topics in current evolutionary biology. This includes the study of the timing and relationships of the two major clades of extant mammals – marsupials and placentals. Molecular studies concerned with marsupial and placental origin and diversification can be at odds with the fossil record. Such studies are, however, not a recent phenomenon. Over 150 years ago Charles Darwin weighed two alternative views on the origin of marsupials and placentals. Less than a year after the publication of On the origin of species, Darwin outlined these in a letter to Charles Lyell dated 23 September 1860. The letter concluded with two competing phylogenetic diagrams. One showed marsupials as ancestral to both living marsupials and placentals, whereas the other showed a non-marsupial, non-placental as being ancestral to both living marsupials and placentals. These two diagrams are published here for the first time. These are the only such competing phylogenetic diagrams that Darwin is known to have produced. In addition to examining the question of mammalian origins in this letter and in other manuscript notes discussed here, Darwin confronted the broader issue as to whether major groups of animals had a single origin (monophyly) or were the result of “continuous creation” as advocated for some groups by Richard Owen. Charles Lyell had held similar views to those of Owen, but it is clear from correspondence with Darwin that he was beginning to accept the idea of monophyly of major groups.


2015 ◽  
Vol 12 (1) ◽  
pp. 3910-3918 ◽  
Author(s):  
Dr Remon M Zaki ◽  
Prof Adel M. Kamal El-Dean ◽  
Dr Nermin A Marzouk ◽  
Prof Jehan A Micky ◽  
Mrs Rasha H Ahmed

 Incorporating selenium metal bonded to the pyridine nucleus was achieved by the reaction of selenium metal with 2-chloropyridine carbonitrile 1 in the presence of sodium borohydride as reducing agent. The resulting non isolated selanyl sodium salt was subjected to react with various α-halogenated carbonyl compounds to afford the selenyl pyridine derivatives 3a-f  which compounds 3a-d underwent Thorpe-Ziegler cyclization to give 1-amino-2-substitutedselenolo[2,3-b]pyridine compounds 4a-d, while the other compounds 3e,f failed to be cyclized. Basic hydrolysis of amino selenolo[2,3-b]pyridine carboxylate 4a followed by decarboxylation furnished the corresponding amino selenolopyridine compound 6 which was used as a versatile precursor for synthesis of other heterocyclic compound 7-16. All the newly synthesized compounds were established by elemental and spectral analysis (IR, 1H NMR) in addition to mass spectra for some of them hoping these compounds afforded high biological activity.


2018 ◽  
Vol 52 (2) ◽  
pp. 455-462 ◽  
Author(s):  
G. Ya. Doroshina ◽  
I. A. Nikolajev

Sphagnum mires on the Greater Caucasus are rare, characterized by the presence of relict plant communities of glacial age and are in a stage of degradation. The study of Sphagnum of Chefandzar and Masota mires is carried out for the first time. Seven species of Sphagnum are recorded. Their distribution and frequency within the North Caucasus are analyzed. Sphagnum contortum, S. platyphyllum, S. russowii, S. squarrosum are recorded for the first time for the study area and for the flora of North Ossetia. The other mosses found in the study area are listed.


2018 ◽  
Author(s):  
Amir Forouharfar

The paper was shaped around the pivotal question: Is SE a sound and scientific field of research? The question has given a critical tone to the paper and has also helped to bring out some of the controversial debates in the realm of SE. The paper was organized under five main discussions to be able to provide a scientific answer to the research question: (1)<b> </b>is “social entrepreneurship” an oxymoron?, (2) the characteristics of SE knowledge, (3) sources of social entrepreneurship knowledge, (4) SE knowledge: structure and limitations and (5) contributing epistemology-making concepts for SE.<b> </b>Based on the sections,<b> </b>the study relied on the relevant philosophical schools of thought in <i>Epistemology </i>(e.g. <i>Empiricism</i>, <i>Rationalism</i>, <i>Skepticism</i>, <i>Internalism</i> vs. <i>Externalism</i>,<i> Essentialism, Social Constructivism</i>, <i>Social Epistemology, etc.</i>) to discuss these controversies around SE and proposes some solutions by reviewing SE literature. Also, to determine the governing linguistic discourse in the realm of SE, which was necessary for our discussion,<i> Corpus of Contemporary American English (COCA)</i> for the first time in SE studies was used. Further, through the study, SE buzzwords which constitute SE terminology were derived and introduced to help us narrowing down and converging the thoughts in this field and demarking the epistemological boundaries of SE. The originality of the paper on one hand lies in its pioneering discussions on SE epistemology and on the other hand in paving the way for a construction of sound epistemology for SE; therefore in many cases after preparing the philosophical ground for the discussions, it went beyond the prevalent SE literature through meta-analysis to discuss the cases which were raised. The results of the study verified previously claimed embryonic pre-paradigmatic phase in SE which was far from a sound and scientific knowledge, although the scholarly endeavors are the harbingers of such a possibility in the future which calls for further mature academic discussion and development of SE knowledge by the SE academia.


Author(s):  
Caroline Durand

Al-Qusayr is located 40 km south of modern al-Wajh, roughly 7 km from the eastern Red Sea shore. This site is known since the mid-19th century, when the explorer R. Burton described it for the first time, in particular the remains of a monumental building so-called al-Qasr. In March 2016, a new survey of the site was undertaken by the al-‘Ula–al-Wajh Survey Project. This survey focused not only on al-Qasr but also on the surrounding site corresponding to the ancient settlement. A surface collection of pottery sherds revealed a striking combination of Mediterranean and Egyptian imports on one hand, and of Nabataean productions on the other hand. This material is particularly homogeneous on the chronological point of view, suggesting a rather limited occupation period for the site. Attesting contacts between Mediterranean merchants, Roman Egypt and the Nabataean kingdom, these new data allow a complete reassessment of the importance of this locality in the Red Sea trade routes during antiquity.


2019 ◽  
Vol 23 (17) ◽  
pp. 1857-1866
Author(s):  
Munawar Hussain ◽  
Zaheer Ahmed ◽  
Shamsun N. Khan ◽  
Syed A. A. Shah ◽  
Rizwana Razi ◽  
...  

Three new 5-deoxyflavonoid and dihydroflavonoids 2, 3 and 4 have been isolated from the methanolic extract of Abutioln pakistanicum aerial parts, for which structures were elucidated explicitly by extensive MS- and NMR-experiments. In addition to these, 3,7,4′-trihydroxy-3′-methoxy flavonol (1) is reported for the first time from Abutioln pakistanicum. Compound 2 and 4 are p-coumaric acid esters while compounds 2–4 exhibited α-glucosidase inhibitory activity. Docking studies indicated that the ability of flavonoids 2, 3 and 4 to form multiple hydrogen bonds with catalytically important residues is decisive hence is responsible for the inhibition activity. The docking results signified the observed in-vitro activity quite well which is in accordance with previously obtained conclusion that phenol moiety and hydroxyl group are critical for the inhibition of α-glucosidase enzyme.


2016 ◽  
Vol 1 (1) ◽  
Author(s):  
D.G. Shah ◽  
D.N. Mehta ◽  
R.V. Gujar

Bryophytes are the second largest group of land plants and are also known as the amphibians of the plant kingdom. 67 species of bryophytes have been reported from select locations across the state of Gujrat. The status of family fissidentaceae which is a large moss family is being presented in this paper. Globally the family consists of 10 genera but only one genus, Fissidens Hedw. has been collected from Gujarat. Fissidens is characterized by a unique leaf structure and shows the presence of three distinct lamina, the dorsal, the ventral and the vaginant lamina. A total of 8 species of Fissidens have been reported from the state based on vegetative characters as no sporophyte stages were collected earlier. Species reported from the neighboring states also showed the absence of sporophytes. The identification of different species was difficult due to substantial overlap in vegetative characters. Hence a detailed study on the diversity of members of Fissidentaceae in Gujarat was carried out between November 2013 and February 2015. In present study 8 distinct species of Fissidens have been collected from different parts of the state. Three species Fissidens splachnobryoides Broth., Fissidens zollingerii Mont. and Fissidens curvato-involutus Dixon. have been identified while the other five are still to be identified. Fissidens zollingerii Mont. and Fissidens xiphoides M. Fleisch., which have been reported as distinct species are actually synonyms according to TROPICOS database. The presence of sexual reproductive structures and sporophytes for several Fissidens species are also being reported for the first time from the state.


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