Microwave Assisted Synthesis of BenzilideneBenzylamine and Its Acetylcholinesterase and Butyrylcholinesterase Activity

2020 ◽  
Vol 5 (2) ◽  
pp. 86-94
Author(s):  
Himayat Ullah ◽  
Khair Zaman ◽  
Muhammad Ismail
Keyword(s):  
Inhibitory Activity ◽  
Biological Activities ◽  
Microwave Assisted Synthesis ◽  
Pure Crystal ◽  
Azomethine Group ◽  
Wide Range ◽  
Standard Compound ◽  
Inhibitory Potential ◽  
Butyrylcholinesterase Activity

BenzilideneBenzylamine the derivative of Schiff bases contain azomethine group already used widely for industrial purposes and have wide range of biological activities. Benzilidene Benzylamine were synthesized by microwave irradiation reacting different aromatic and aniline purified pure crystal, 85% yield obtained reaction monitor by TLC. The Anticholinesterase activity utilized spectrophotometric Ellman assay for determination of butyrylcholinesterase and acetylcholinesterase. The synthesis compound 1 – 6 showed a wide range of inhibitory activity the compound 3((E)-N-(4-fluorobenzylidene)aniline) at 1000µg/mL, 71.62±0.74 percent inhibitory acetylcholinesterase potential while compound 6 ((E)-4 ((phenylimino)methyl) benzaldehyde) at 500 and 1000 µg/mL at IC50 show 71.68±0.22, 77.84±0.32 percent inhibitory potential comparatively greater than standard Galanthamine at 62.5µg/mL, 74.10±0.90 at IC50. The butyrylcholinesterase activity of compound 6 ((E)-4 ((phenylimino)methyl)benzaldehyde) at 1000 µg/mL, show 75.83±1.07 percent inhibitory potential which is similar to standard compound at 62.5µg/mL concentration of 75.45±0.90 percent butyrylcholinesterase inhibitory activity.

scholarly journals Microbiological and Antioxidant Activity of Phenolic Compounds in Olive Leaf Extract

Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 5946
Author(s):  
Dragana Borjan ◽  
Maja Leitgeb ◽  
Željko Knez ◽  
Maša Knez Hrnčič
Keyword(s):  
Phenolic Compounds ◽  
Leaf Extract ◽  
Biological Activities ◽  
Olive Leaf ◽  
Olive Leaves ◽  
Olive Leaf Extract ◽  
Antimicrobial Potential ◽  
Isolation And Characterization ◽  
Wide Range

According to many reports, phenolic compounds isolated from olive leaves have very good biological activities, especially antimicrobial. Presently, the resistance of microorganisms to antibiotics is greater than ever. Therefore, there are numerous recent papers about alternative solutions for inhibiting their influence on human health. Olive leaf is studied as an important source of antimicrobials with low cost and used in medicine. Numerous publications on involving green technologies for isolation of active compounds from olive leaves have appeared over the past few decades. The present review reports on current knowledge of the most isolated phenolic compounds from olive leaf extract as well as methods for their isolation and characterization. This paper uses recent research findings with a wide range of study models to describe the antimicrobial potential of phenolic compounds. It also describes the vast range of information about methods for determination of antimicrobial potential focusing on effects on different microbes. Additionally, it serves to highlight the role of olive leaf extract as an antioxidants and presents methods for determination of antioxidant potential. Furthermore, it provides an overview of presence of enzymes. The significance of olive leaves as industrial and agricultural waste is emphasized by means of explaining their availability, therapeutic and nutritional effects, and research conducted on this field.

scholarly journals Acetylcholine esterase inhibitory activity of green synthesized nanosilver by naphthopyrones isolated from marine-derived Aspergillus niger

PLoS ONE ◽  
2021 ◽  
Vol 16 (9) ◽  
pp. e0257071
Author(s):  
Ghada Mahmoud Abdelwahab ◽  
Amira Mira ◽  
Yuan-Bin Cheng ◽  
Tarek A. Abdelaziz ◽  
Mohamed Farid I. Lahloub ◽  
...  
Keyword(s):  
Aspergillus Niger ◽  
Inhibitory Activity ◽  
Active Sites ◽  
Biological Activities ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Acetylcholine Esterase ◽  
Protective Effects ◽  
Wide Range ◽  
First Time

Aspergillus niger metabolites exhibited a wide range of biological properties including antioxidant and neuro-protective effects and some physical properties as green synthesis of silver nanoparticles AgNP. The present study presents a novel evidence for the various biological activities of green synthesized AgNPs. For the first time, some isolated naphtho-γ-pyrones from marine-derived Aspergillus niger, flavasperone (1), rubrofusarin B (2), aurasperone A (3), fonsecinone A (4) in addition to one alkaloid aspernigrin A (7) were invistigated for their inhibitory activity of acetylcholine esterase AChE, a hallmark of Alzheimer’s disease (AD). The ability to synthesize AgNPs by compounds 3, 4 and 7 has been also tested for the first time. Green synthesized AgNPs were well-dispersed, and their size was ranging from 8–30 nm in diameter, their morphology was obviously spherical capped with the organic compounds. Further biological evaluation of their AChE inhibitory activity was compared to the parent compounds. AgNps dramatically increased the inhibitory activity of Compounds 4, 3 and 7 by 84, 16 and 13 fold, respectively to be more potent than galanthamine as a positive control with IC50 value of 1.43 compared to 0.089, 0.311 and 1.53 of AgNPs of Compounds 4, 3 and 7, respectively. Also compound 2 showed moderate inhibitory activity. This is could be probably explained by closer fitting to the active sites or the synergistic effect of the stabilized AgNPs by the organic compouds. These results, in addition to other intrinsic chemical and biological properties of naphtho-γ-pyrones, suggest that the latter could be further explored with a view towards other neuroprotective studies for alleviating AD.

Quantitative Determination of Quercitrin Levels in Rat Plasma Using UHPLC-MS/MS and its Application in a Pharmacokinetic Study after the Oral Administration of Polygoni Cuspidati Folium Capsules

2021 ◽  
Vol 22 ◽  
Author(s):  
Shi-tang Ma ◽  
Xin-yuan Zhang ◽  
Ning Zhang ◽  
Xiao-lin Bi ◽  
Cheng-Tao Feng
Keyword(s):  
Mass Spectrometry ◽  
Oral Administration ◽  
Quantitative Determination ◽  
Biological Activities ◽  
Rat Plasma ◽  
Negative Ion ◽  
Pharmacokinetic Parameters ◽  
Peripheral Tissues ◽  
Wide Range

Background: Quercitrin is widely found in herbal medicines, and it is particularly important in the design of new therapeutic agents. Because of its wide range of biological activities, methods for detecting quercitrin and its pharmacokinetics in biological samples must be investigated. Objective: To develop and validate a sensitive and reliable ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method for the quantitative determination of quercitrin levels in rat plasma and test its application in a pharmacokinetic investigation after the oral administration of Polygoni cuspidati folium capsules (HC). Methods: First, a rapid analytical method implementing UHPLC-MS/MS for the quantification of quercitrin levels in rat plasma was developed and validated. The analyte and internal standard (IS) tinidazole were extracted from rat plasma via protein precipitation with 800 μL of methanol and 50 μL of 1% formic acid solution. Chromatographic separation was performed using an Agilent ZORBAX C18 column within 4 min. Mass spectrometry was performed for quantification using a triple-quadrupole mass spectrometer employing electrospray ionization in the negative ion mode. The MRM transitions for quercitrin and IS were m/z 447.2→229.9 and m/z 246.0→125.8, respectively. The UHPLC-MS/MS method for the quantitative determination of quercitrin levels in rat plasma was then applied to investigate its pharmacokinetics after the oral administration of HC in rats. Results: The developed UHPLC-MS/MS method for detecting quercitrin in rat plasma was linear over the range of 0.1–160 ng/mL. The linear regression equation was Y = (0.7373 ± 0.0023)X − (0.0087 ± 0.0021) (r2 = 0.9978). The intra- and interday precision values were within 7.8%, and the recoveries of quercitrin and IS exceeding 67.3%. The UHPLC-MS/MS method was successfully applied to characterize the pharmacokinetic profile of quercitrin in eight rats after the oral administration of HC. The experimentally obtained values were fit to a one-compartment, first-order pharmacokinetic model, and they appeared to fit the concentration-time curve. Conclusion: Quercitrin was proven to be stable during sample storage, preparation, and analytical procedures. The pharmacokinetic parameters suggested that quercitrin may be present in the peripheral tissues of rats.

scholarly journals Alkaloid Profiling and Cholinesterase Inhibitory Potential of Crinum × amabile Donn. (Amaryllidaceae) Collected in Ecuador

Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2686
Author(s):  
Luciana R. Tallini ◽  
Angelo Carrasco ◽  
Karen Acosta León ◽  
Diego Vinueza ◽  
Jaume Bastida ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Biological Activities ◽  
New Drugs ◽  
Bioactive Molecules ◽  
Acetylcholinesterase Inhibition ◽  
Plant Family ◽  
Disease Symptoms ◽  
Amaryllidaceae Alkaloids ◽  
Inhibitory Potential

Natural products are one of the main sources for developing new drugs. The alkaloids obtained from the plant family Amaryllidaceae have interesting structures and biological activities, such as acetylcholinesterase inhibition potential, which is one of the mechanisms used for the palliative treatment of Alzheimer’s disease symptoms. Herein we report the alkaloidal profile of bulbs and leaves extracts of Crinum × amabile collected in Ecuador and their in vitro inhibitory activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. Using Gas Chromatography coupled to Mass Spectrometry (GC-MS), we identified 12 Amaryllidaceae alkaloids out of 19 compounds detected in this species. The extracts from bulbs and leaves showed great inhibitory activity against AChE and BuChE, highlighting the potential of Amaryllidaceae family in the search of bioactive molecules.

scholarly journals Phenolome of Asian Agrimony Tea (Agrimonia asiatica Juz., Rosaceae): LC-MS Profile, α-Glucosidase Inhibitory Potential and Stability

Foods ◽  
2020 ◽  
Vol 9 (10) ◽  
pp. 1348
Author(s):  
Nina I. Kashchenko ◽  
Daniil N. Olennikov
Keyword(s):  
Inhibitory Activity ◽  
High Performance ◽  
Phenolic Content ◽  
Mass Spectrometric ◽  
Wide Range ◽  
Functional Beverages ◽  
Reduce Blood Glucose ◽  
Photodiode Array ◽  
Inhibitory Potential ◽  
Tea Plants

Functional beverages constitute the rapidly increasing part of the functional food section and represent an area with a wide range of products including herbal-based beverages. We carried out screening investigations of the extracts of 85 Rosaceous tea plants. Among the extracts analyzed Agrimonia asiatica herb extract demonstrated the highest inhibitory activity against the enzyme α-glucosidase (20.29 µg/mL). As a result of chromato-mass-spectrometric profiling of A. asiatica herb with high-performance liquid chromatography with photodiode array and electrospray triple quadrupole mass-spectrometric detection (HPLC-PDA-ESI-tQ-MS) 60 compounds were identified, including catechins, ellagitannins, flavones, flavonols, gallotannins, hydroxycinnamates, procyanidins, most for the very first time. The analysis of the seasonal variation of metabolites in A. asiatica herb demonstrated that the phenolic content was highest in summer samples and lower in spring and autumn. HPLC activity-based profiling was utilized to identify compounds of A. asiatica herb with the maximal α-glucosidase inhibitory activity. The most pronounced inhibition of α-glucosidase was observed for agrimoniin, while less significant results of inhibition were revealed for ellagic acid and isoquercitrin. The evaluation of phenolic content in A. asiatica herbal teas with the subsequent determination of α-glucosidase inhibiting potential was discovered. Maximum inhibition of α-glucosidase was observed for hot infusion (75.33 µg/mL) and the minimum for 30 min decoction (159.14 µg/mL). Our study demonstrated that A. asiatica herbal tea is a prospective functional beverage in which dietary intake may help to reduce blood glucose.

scholarly journals Naturally Occurring Homoisoflavonoids: Phytochemistry, Biological Activities and Synthesis

2007 ◽  
Vol 2 (4) ◽  
pp. 1934578X0700200 ◽  
Author(s):  
Berhanu M. Abegaz ◽  
Joan Mutanyatta-Comar ◽  
Mathew Nindi
Keyword(s):  
Biological Activities ◽  
Optical Rotation ◽  
Biological Properties ◽  
Important Class ◽  
Melting Points ◽  
Naturally Occurring ◽  
Wide Range ◽  
Plant Families ◽  
Related Compounds

This review covers the phytochemical, biological properties, and synthesis of naturally occurring homoisoflavonoids. Homoisoflavonoids are a very important class of secondary metabolites whose numbers have grown from 20 in 1981 to 157 at the present time. They are found to occur in seven plant families. For the purpose of this review they are classified into five groups: 3-benzylchroman-4-ones, 3-benzylflavans, Δ3,9 and Δ2,3 3-benzylchroman-4-ones, benzocyclobutenes (scillascillins) and rearranged homoisoflavonoids (brazilin and related compounds). Biosynthetically, the 3-benzylchroman-4-ones and the 3-hydroxy-derivatives have been shown to arise from a chalcone precursor (sappanchalcone) and there is strong evidence that this isolable intermediate can be converted into the diverse structures such as the benzocyclobutenes (scillascillins) and the rearranged, brazilin-type compounds. Homoisoflavonoids possess a wide range of biological activities, including, antimicrobial, antimutagenic, anti-inflammatory, antidiabetic, etc, properties. The review also surveys the chemical synthesis of natural homoisoflavonoids. Analytical methods for the determination of these important metabolites are also reviewed. The last section is devoted to a brief review of the diagnostic NMR spectroscopic features of homoisoflavonoids. A comprehensive Table has also been compiled listing all known metabolites, their sources, melting points and optical rotation values (where available) and references.

scholarly journals Effect of Germination on Alfalfa and Buckwheat: Phytochemical Profiling by UHPLC-ESI-QTOF-MS/MS, Bioactive Compounds, and In-Vitro Studies of Their Diabetes and Obesity-Related Functions

Antioxidants ◽  
2021 ◽  
Vol 10 (10) ◽  
pp. 1613
Author(s):  
Simon-Okomo Aloo ◽  
Fred-Kwame Ofosu ◽  
Deog-Hwan Oh
Keyword(s):  
Inhibitory Activity ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Alfalfa Seed ◽  
Edible Seeds ◽  
Alfalfa Sprouts ◽  
Inhibitory Potential ◽  
Alfalfa Sprout

Germination can be used to enhance nutritional value and health functions of edible seeds. Sprouts are considered healthier than raw seeds because they are richer in the basic nutritional components (carbohydrates, protein, vitamins, and minerals) and also contain more bioactive components responsible for various biological activities. The effect of sprouting on the antioxidant, antidiabetic, antiobesity activities, and metabolite profiles of alfalfa and buckwheat seeds was investigated in this study. DPPH radical scavenging activity was highest in buckwheat sprouts followed by alfalfa sprout, buckwheat seed, and alfalfa seed, respectively. ABTS radical scavenging potential showed a similar trend as DPPH with buckwheat sprouts exerting the best scavenging capacity. Alfalfa sprout and buckwheat seed exhibited the highest percentage inhibitory activity of α-glucosidase (96.6 and 96.5%, respectively). Alfalfa sprouts demonstrated the strongest inhibitory activity against pancreatic lipase (57.12%) while alfalfa seed showed the highest advanced glycation end products (AGEs) formation inhibitory potential (28.7%). Moreover, thirty-three (33) metabolites were characterized in the seed and sprout samples. Sprouts demonstrated a higher level of metabolites compared to raw seeds. Hence, depending on the type of seed and the target activity, sprouting is a good technique to alter the secondary metabolites and functional properties of edible seeds.

Total synthesis of melleumins A and B and their analogs: Determination of stereochemistry and Wnt signal inhibitory activity

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
M Ishibashi ◽  
S Hanazawa ◽  
Y Uchino ◽  
X Li ◽  
MA Arai
Keyword(s):  
Total Synthesis ◽  
Inhibitory Activity ◽  
Wnt Signal

Pharmacologically potentials of different substituted coumarin derivatives

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Benzene Ring ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coumarin Derivatives ◽  
Wide Range ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
Coumarin Compounds

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.

DINAMIKA POLITIK PERSETUJUAN BERSAMA TENTANG PENETAPAN DESA ADAT DI KABUPATEN ROKAN HULU TAHUN 2014

2017 ◽  
Vol 15 (1) ◽  
pp. 21
Author(s):  
Haryo Suganda ◽  
Raja Muhammad Amin
Keyword(s):  
Regulatory Region ◽  
Field Research ◽  
Analysis Techniques ◽  
Political Dynamics ◽  
Political Interests ◽  
Wide Range ◽  
Information Method ◽  
Qualitative Descriptive ◽  
The Village

This study is motivated the identification of policies issued by the regional Governmentof Rokan Hulu in the form of Regulatory region number 1 by 2015 on the determination of thevillage and Indigenous Village. Political dynamics based on various interests against themanufacture of, and decision-making in the process of formation of the corresponding localregulations determination of Indigenous Villages in the Rokan Hulu is impacted to a verysignificantamount of changes from the initial draft of the number i.e. 21 (twenty one) the villagebecame Customary 89 (eighty-nine) the Indigenous Villages who have passed. Type of thisresearch is a qualitative descriptive data analysis techniques. The research aims to describe theState of the real situation in a systematic and accurate fact analysis unit or related research, aswell as observations of the field based on the data (information). Method of data collectionwas done with interviews, documentation, and observations through fieldwork (field research).The results of the research on the process of discussion of the draft local regulations andmutual agreement about Designation of Indigenous Villages in the Rokan Hulu is, showed thatthe political dynamics that occur due to the presence of various political interests, rejectionorally by Villagers who were judged to have met the requirements of Draft Regulations to beformulated and the area for the set to be Indigenous Villages, and also there is a desire fromsome villages in the yet to Draft local regulations in order to set the Indigenous village , there isa wide range of interests of these aspects influenced the agreement to assign the entire localVillage which is in the Rokan Hulu become Indigenous village, and the village of Transmigrationinto administrative Villages where the initiator of the changes in the number of IndigenousVillages in the Rokan Hulu it is the desire of the local Government of its own.

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