Unfolded and macrocyclic ammonium derivatives of diterpenoids steviol and isosteviol having choline moieties. Synthesis and inhibitory activities toward acetylcholine- and butyrylcholinesterases

MedChemComm ◽  
2012 ◽  
Vol 3 (11) ◽  
pp. 1449-1454 ◽  
Author(s):  
Mayya G. Korochkina ◽  
Alexandra D. Nikitashina ◽  
Ravil N. Khaybullin ◽  
Konstantin A. Petrov ◽  
Irina Yu. Strobykina ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Inhibitory Activities ◽  
Derivatives Of

Derivatives of isosteviol and steviol possessing choline moieties have been synthesized and assayed for AchE and BchE inhibitory activity.

scholarly journals α-Glucosidase and Pancreatic Lipase Inhibitory Activities of Diterpenes from Indian Mango Ginger (Curcuma amada Roxb.) and Its Derivatives

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4071 ◽  
Author(s):  
Yuri Yoshioka ◽  
Naori Yoshimura ◽  
Shinichi Matsumura ◽  
Hiroto Wada ◽  
Maya Hoshino ◽  
...  
Keyword(s):  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Parent Compound ◽  
Molecular Size ◽  
Porcine Pancreatic Lipase ◽  
Mango Ginger ◽  
Curcuma Amada ◽  
Structure Activity ◽  
Inhibitory Activities ◽  
Derivatives Of

Enzymatic inhibitions of crude extracts and their constituents from Zingiberaceae against both rat intestinal α-glucosidase and porcine pancreatic lipase were investigated. Structure–activity relationships using their derivatives were also investigated. The rhizomes extract of mango ginger, Curcuma amada showed remarkable inhibitory activity in the screening test. Two natural labdane diterpenes 1 and 2 and a drimane sesquiterpene 3 were major constituents isolated from this hexane extract. Among them, (E)-labda-8(17),12-diene-15,16-dial (1) was the most prominent compound and showed inhibitory activity against both α-glucosidase and lipase. Derivatives 4–10 from compound 1 were prepared and evaluated using inhibitory assays with these enzymes. The reduced derivative 4 maintained α-glucosidase inhibitory activity, but had decreased pancreatic lipase inhibitory activity compared with parent compound 1. Other tested derivatives of compound 1, including acetates 5–7 and oxidative derivatives 8–10, had very weak α-glucosidase inhibitory activity. Most of these compounds showed moderate pancreatic lipase inhibitory activity. However, only sesquiterpene albicanal (3) showed drastically decreased pancreatic lipase activity compared with 1. These findings suggested that molecular size was essential for enzymatic inhibitory activities of these compounds. These results demonstrated that mango ginger may be useful for the prevention of obesity and being overweight.

Bacteriocin-like Inhibitory Activity Associated with Beta-hemolytic Strains of Streptococcus salivarius

1987 ◽  
Vol 66 (8) ◽  
pp. 1321-1325 ◽  
Author(s):  
G.R. Tompkins ◽  
J.R. Tagg
Keyword(s):  
Inhibitory Activity ◽  
Plasmid Curing ◽  
Streptococcus Salivarius ◽  
Indicator Organisms ◽  
Beta Hemolytic Streptococcus ◽  
Distinctive Type ◽  
Complete Set ◽  
Inhibitory Activities ◽  
Inhibitory Agents ◽  
Derivatives Of

Seven beta-hemolytic Streptococcus salivarius isolates produced bacteriocin-like inhibitory activity in deferred antagonism tests using a set of nine indicator bacteria (I1-I 9). Five of these S. salivarius strains (KWF, TOVE-R, K17, K21, and K26) were inhibitory to indicators I2, I5, I6, and I7. Mutated non-hemolytic derivatives showed concomitant loss of inhibitory activity against I2, I5, and 16, but retained activity against I7. Inhibitory activity against I2, I5, and I6 was restored in beta-hemolytic revertants of such mutants. Strain 3638 was inhibitory to all of the indicator organisms except I3, and this pattern of inhibitory activity was retained by non-hemolytic derivatives. It appeared that strain 3638 produced an additional broadly-active inhibitory agent, since a mutant (strain 3638A), which was apparently defective in the production of this inhibitor, retained both the beta-hemolytic and I2-, I5-, 16-, and I7-inhibitory activities. Non-hemolytic derivatives of strain 3638A were inhibitory only to I7. Strain 3638, therefore, appeared to produce at least three inhibitory agents: one active only on I7; another acting on I 2, 15, and 16 (and associated with beta-hemolytic activity); and a third apparently active on all of the indicators other than I3. S. salivarius strain JH inhibited all nine indicator strains and possessed a beta-hemolytic character which differed from that of the other strains in being readily eliminated on treatment with the plasmid-curing agent novobiocin. Non-hemolytic derivatives of JH retained inhibitory activity against the complete set of indicators. The results of this study suggest that hemolysin production by some S. salivarius strains may be intimately associated with a distinctive type of bacteriocin-like activity.

scholarly journals SYNTHESIS OF ACETYL AND BENZOYL ESTERS OF XANTHORRHIZOL AND ITS OXIDATION PRODUCTS AND EVALUATION OF THEIR INHIBITORY ACTIVITY AGAINST NITRIC OXIDE PRODUCTION

2020 ◽  
pp. 135-138
Author(s):  
MAYA DAMAYANTI RAHAYU ◽  
SUSI KUSUMANINGRUM ◽  
HAYUN HAYUN
Keyword(s):  
Inhibitory Activity ◽  
Diclofenac Sodium ◽  
Positive Control ◽  
Oxidation Products ◽  
No Production ◽  
Raw 264.7 ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Reduced Toxicity ◽  
Derivatives Of

Objective: Xanthorrhizol is known to have anti-inflammatory activity. However, new xanthorrhizol derivatives with improved anti-inflammatoryactivity and reduced toxicity are needed.Methods: In this study, the derivatives of xanthorrhizol were synthesized and spectroscopically characterized, and their inhibitory activities againstnitric oxide (NO) production were evaluated in RAW 264.7 macrophage cells.Results: The first stage of synthesis produced compounds 2a and 2b in 58.49% and 63.26% yields, respectively. Compounds 2a and 2b were oxidizedusing potassium permanganate, giving compounds 3a and 3b in yields of 51.92% and 43.78%, respectively. Compounds 1, 2a, 3a, and 3b alongwith diclofenac sodium (the positive control) exhibited IC50 values for NO production of 31.82, 73.85, 354.05, 97.19, and 78.43 μM, respectively. Incontrast, compound 2b did not show any inhibitory activity. Based on cytotoxicity assay, compounds 1, 2a, 2b, 3a, 3b, and diclofenac sodium had LD50values of 30.97, 65.15, 31.15, 117.86, 53.40, and 51.67 μM, respectively. The NO inhibitory activities of compounds 2a, 3a, and 3b were lower than thatof xanthorrhizol (compound 1). However, cytotoxicity tests showed that compounds 2a, 3a, and 3b had reduced toxicities compared to xanthorrhizol.Conclusion: The modification of xanthorrhizol through esterification and oxidation produced derivative compounds with weaker anti-inflammatoryactivity but reduced cytotoxicity.

Synthesis and investigation of viral-inhibitory activity of nitrogen-containing derivatives of adamantane

1991 ◽  
Vol 25 (7) ◽  
pp. 485-488 ◽  
Author(s):  
Yu. N. Klimochkin ◽  
I. K. Moiseev ◽  
G. V. Vladyko ◽  
L. V. Korobchenko ◽  
E. I. Boreko
Keyword(s):  
Inhibitory Activity ◽  
Derivatives Of

scholarly journals Antioxidant and angiotensin I-converting enzyme inhibitory activities of Xuanwei ham before and after cooking and in vitro simulated gastrointestinal digestion

2018 ◽  
Vol 5 (7) ◽  
pp. 180276 ◽  
Author(s):  
Le Wang ◽  
Xiang Li ◽  
Yingnan Li ◽  
Wenying Liu ◽  
Xiaoyun Jia ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Scavenging Activity ◽  
Angiotensin I ◽  
Gastrointestinal Digestion ◽  
Ace Inhibitory Activity ◽  
Angiotensin I Converting Enzyme ◽  
Before And After ◽  
Inhibitory Activities ◽  
Ace Inhibitory ◽  
Significant Increment

Xuanwei ham is especially rich in a large amount of peptides and free amino acids under the action of protein degradation. Some of these peptides can potentially exert bioactivities of interest for human health. Traditionally, Xuanwei ham should undergo Chinese household cooking treatments before eating. However, it has not been known how its bioactivity changes after cooking and gastrointestinal digestion. Herein, Xuanwei ham is analysed before and after cooking, as well as gastrointestinal digestion being simulated so as to evaluate and compare its effect on antioxidant and angiotensin I-converting enzyme (ACE) inhibitory activities. The antioxidant activity is analysed using five different methods, and results demonstrate that cooking has some negative effects on antioxidative capacity when determined using different antioxidant methods except for a significant increment in 1,1'-diphenyl-2-picrylhydrazyl radical-scavenging activity, while ACE inhibitory activity increases significantly after cooking compared with control samples. After gastrointestinal digestion of samples, there is a significant increment of the antioxidant and ACE inhibitory activities in comparison with control and cooked samples. Particularly, after gastrointestinal digestion, free thiols content and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical-cation-scavenging activity of Xuanwei ham, respectively, increase about twice and fourfold, while ACE inhibitory activity increases about twice compared to cooked samples, reaching the value of 83.73%. Therefore, through cooking the antioxidant activity and ACE inhibitory activity of Xuanwei ham are not completely lost and a part of them is still maintained, while gastrointestinal digestion produces a significant enhancement in both bioactivities, highlighting a greater potential for a beneficial physiological effect on human health after eating it.

Synthesis and antibacterial evaluation of novel Schiff's base derivatives of nitroimidazole nuclei as potent E. coli FabH inhibitors

RSC Advances ◽  
2014 ◽  
Vol 4 (97) ◽  
pp. 54217-54225 ◽  
Author(s):  
Xin Zhang ◽  
Chetan B. Sangani ◽  
Li-Xin Jia ◽  
Pi-Xian Gong ◽  
Fang Wang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Schiff’S Base ◽  
E Coli ◽  
Derivatives Of ◽  
Antibacterial Evaluation ◽  
Potent Inhibitory Activity

Series of novel Schiff's base derivatives have been synthesized. Compound 10q showed the most potent inhibitory activity (IC50 = 2.6883 μM).

Derivatives of 3′-and 5′-Deoxyadenosine: Their Inhibitory Activity against DNA Viruses

Chemotherapy ◽  
1980 ◽  
Vol 26 (5) ◽  
pp. 316-322 ◽  
Author(s):  
Barbara Grytzmann ◽  
M. Morr ◽  
R. Wigand
Keyword(s):  
Inhibitory Activity ◽  
Dna Viruses ◽  
Derivatives Of

scholarly journals Synthesis and tyrosinase inhibitory activities of 4-oxobutanoate derivatives of carvacrol and thymol

2019 ◽  
Vol 29 (1) ◽  
pp. 56-58 ◽  
Author(s):  
Nicholas Brotzman ◽  
Yiming Xu ◽  
Allison Graybill ◽  
Alexander Cocolas ◽  
Andrew Ressler ◽  
...  
Keyword(s):  
Inhibitory Activities ◽  
Derivatives Of
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