Synthesis and Biological Evaluation of Flavonoids as Antiacetyl- cholinesterase Agent

2014 ◽  
Vol 69 (1) ◽  
Author(s):  
Saleh Nazifi Ibrahim ◽  
Farediah Ahmad
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Microplate Assay ◽  
Synthetic Compounds ◽  
Ache Inhibitory Activity ◽  
Weak Activity ◽  
Layer Chromatography ◽  
Synthesis And Biological Evaluation

A series of chalcones, a flavone and one flavanone were synthesized and elucidated structurally by IR and 1H NMR spectroscopies. The synthetic compounds were then screened for acetylcholinesterase inhibitory activity using thin layer chromatography (TLC) and microplate assays. In the TLC assay, only 2′-hydroxy-4-methoxychalcone and 2′-hydroxy-4′-O-prenyl-2,6-dichlorochalcone were found to show moderate and weak activity respectively against acetylcholinesterase (AchE) at 0.1 mM concentration compared to the control galanthamine. 4′-Hydroxy-2,6-dichlorochalcone, 2′-hydroxy-4-nitrochalcone, 2′-hydroxy-4-(dimethyl)aminochalcone and 2′-hydroxy-4-methoxychalcone showed moderate AchE inhibitory activity with percentage inhibition of 54.24, 46.14 and 49.32 % respectively in the microplate assay.

Synthesis and Biological Evaluation of Acetylcholinesterase Inhibitor Macakurzin C and Its Derivatives

Synlett ◽  
2015 ◽  
Vol 26 (08) ◽  
pp. 1131-1134 ◽  
Author(s):  
Hyoungsu Kim ◽  
Seung-Hoon Baek ◽  
Hongjun Jang
Keyword(s):  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitor ◽  
Biological Evaluation ◽  
Hydroxyl Groups ◽  
Structural Requirements ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

The derivatives of macakurzin C containing a modified D ring and protected C(3)/C(5)-hydroxyl groups were synthesized and their in vitro AChE inhibitory activity and neurotoxicity were evaluated to identify the structural requirements for the activities. The results indicated that C(3)-benzyl-protected derivative has a more potent AChE inhibitory activity (IC50, 2.6 μM) and a less neurotoxicity (GI50, >100 μM) than synthetic macakurzin C (IC50, 9.1 μM; GI50, 16.6 μM).

scholarly journals PROLIFERATION INHIBITORY ACTIVITY OF THE ACTIVE FRACTION MARINE SPONGE Cinachyrella sp. AGAINST CELL LINE T47D

2015 ◽  
Vol 2 (1) ◽  
pp. 663
Author(s):  
Awik Puji Dyah Nurhayati ◽  
Rarastoeti Pratiwi ◽  
Subagus Wahyuono ◽  
Istriyati .
Keyword(s):  
Thin Layer ◽  
Ethyl Acetate ◽  
Thin Layer Chromatography ◽  
Cell Line ◽  
Inhibitory Activity ◽  
Doubling Time ◽  
Preparative Thin Layer Chromatography ◽  
Marine Sponges ◽  
Active Fraction ◽  
Layer Chromatography

<p>Marine sponges Cinachyrella sp. (Family:Tetillidae) in Kukup beach, Kemadang Village, Tanjungsari District, Gunung Kidul, DIY were producing diversity secondary metabolites such as polyketides, alkaloids, peptide and terpene. The purpose of this study was investigated proliferation inhibitory activity of active fraction Cinachyrella sp. against cell line T47D. Sponges samples were collected manually from rocky substrate at depth 0.5 m. The sponges was minced and extracted with 95% ethanol. The ethanol extract was partitioned sequentially with ethyl acetate. The extract ethyl acetate was fractionation with 4 organic solvent, in increasing order of polarity with vacuum liquid chromatography column (VLC) method. Doubling time method was applied to analyse the inhibition proliferative cell line T47D. Resulted showed ethyl acetate extract of Cinachyrella sp. were 12 fractions and all tested fraction obtained by thin layer chromatography (TLC). Fractions that have the same value Rf grouped together to obtain 6 fractions. The fraction number 5 exhibited proliferation inhibitory activity to cell line T47D. The Rf value of active fraction number 5 were 0.125; 0.25 and 0.437. The active fraction 5 than isolation by preparative thin-layer chromatography (PTLC) was 5 isolate fractions preparative. The isolate fractions preparative number 5 exhibited proliferation inhibitory activity against cell line T47D. Fraction which determined by cerium sulfate and results was expressed terpene and alkaloid. <br /><strong></strong></p><p><strong>Keywords</strong>: Cinachyrella sp., Doubling time method, proliferation inhibitory activity.</p>

scholarly journals Preliminary Assessment of the Antihypertensive and Antioxidative Activities of the Peptides from “Saba” Banana (Musa balbisiana Colla) Flesh

KIMIKA ◽  
2019 ◽  
Vol 30 (1) ◽  
pp. 31-39
Author(s):  
Eugene Clark L. Magpantay ◽  
Ana Teresa B. Sucgang ◽  
Mia Clare Marie B. Clemencia ◽  
Teofila D. C. Villar ◽  
Mary Ann O. Torio
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Inhibitory Activity ◽  
In Silico Analysis ◽  
Enzymatic Digestion ◽  
Ultra Performance Liquid Chromatography ◽  
Major Protein ◽  
Major Band ◽  
Lowry Assay ◽  
Layer Chromatography

The crude proteins were isolated using 0.125 M Tris-HCl with 50 mM NaCl at pH 7.4. The protein content of the crude extract was determined using the Lowry assay and was found to be 4.28 mg/mL.  The major band which corresponds to the major protein has an approximate molecular weight of 20 KDa. The isolated crude proteins were subjected to enzymatic digestion using pepsin, trypsin, chymotrypsin, and thermolysin for 3, 4, 12, and 24 hours. The 24-hour digest was found to have the highest percent anti-Angiotensin Converting Enzyme (ACE) activity (36.02%) while the 12-hour digest was found to have the highest anti-oxidative activity (33.14%) using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The 24-hour digest was subjected to Ultra-Performance Liquid Chromatography (UPLC) to determine the peptide fraction responsible for the ACE inhibitory activity. Three peptide fractions (PF1, PF2 and PF3) were chosen and PF2 exhibited the highest percent inhibitory activity (32.21) against ACE. PF2 was subjected to thin layer chromatography (TLC) and the possible identity is EK based on the Rf value traveled by glutamic acid (E) (0.43) and Lysine (K) (0.13). In silico analysis was done to correlate the results with the presence of putative peptides with antioxidative and antihypertensive activities. Results showed that antihypertensive peptides EK, GS, TY, FNE, FP, LKA, PT, PP, FAL and antioxidative peptides IR and VPW were found based on the sequence of the protein in “Saba” banana. The presence of the antihypertensive peptide EK was verified using thin layer chromatography (TLC).

scholarly journals Synthesis and Biological Evaluation of Coumarinyl Sydnone Derivatives

2011 ◽  
Vol 8 (1) ◽  
pp. 113-118 ◽  
Author(s):  
Keshav C. Patel ◽  
Himanshu D. Patel
Keyword(s):  
Antimicrobial Activity ◽  
Melting Point ◽  
Thin Layer ◽  
Biological Evaluation ◽  
Physical Methods ◽  
H Nmr ◽  
Antimicrobial Evaluation ◽  
Layer Chromatography ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

A novel series of compounds containing coumarinyl sydnone derivatives from 4-methyl-7-hydroxy-8-nitro coumarin were synthesized. The formed compounds have been evaluated by physical methods (melting point, thin layer chromatography, elemental analysis) and by spectral data (IR,1H-NMR &13C NMR). The antimicrobial evaluation of the compounds showed that some of them revealed promising antimicrobial activity.

Synthesis and Biological Evaluation of Benzothiazole-piperazinesulfonamide Conjugates and Their Antibacterial and Antiacetylcholinesterase Activity

2019 ◽  
Vol 16 (9) ◽  
pp. 723-734
Author(s):  
B. Ramalingeswara Rao ◽  
Mohana R. Katiki ◽  
Kommula Dileep ◽  
C. Ganesh Kumar ◽  
G. Narender Reddy ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Activity ◽  
Micrococcus Luteus ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Reference Drug ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation

Two series of N-2-benzothiazolyl-4-(arylsulfonyl)-1-piperazineacetamides/propanamides were synthesized from substituted 2-aminobenzothiazoles and were assayed for their in vitro antimicrobial activities against a panel of different pathogenic bacterial strains such as Micrococcus luteus, S. aureus, S. aureus MLS-16, B. subtilis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella planticola and Candida albicans. Among the synthesized compounds 5e,f,g and 6g,h,i showed promising antifungal activity against C. albicans as compared to the reference drug, miconazole. Further, compounds 6g,h,i showed broad spectrum antibacterial activity against all the tested bacterial strains, while the compounds 6a-f,j-m showed significant antibacterial activity against all the tested bacterial strains as compared to the reference drug, ciprofloxacin. In addition, the target compounds were evaluated for their acetylcholinesterase (AChE) inhibitory activity, and, among the tested, compounds 5j,k,l and 6i showed promising AChE inhibitory activity.

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