Inhibition of flavonoids on acetylcholine esterase: binding and structure–activity relationship

2014 ◽  
Vol 5 (10) ◽  
pp. 2582-2589 ◽  
Author(s):  
Yixi Xie ◽  
Weijie Yang ◽  
Xiaoqing Chen ◽  
Jianbo Xiao
Keyword(s):  
Structure Activity Relationship ◽  
Acetylcholine Esterase ◽  
Activity Relationship ◽  
Hydroxyl Groups ◽  
Aromatic Rings ◽  
Structure Activity

Hydroxyl groups on the aromatic rings of flavonoids are favorable for inhibiting AChE, and the hydroxylation increases the affinities for AChE. However, methoxylation may decrease or increase the activities depending on the class of flavonoids.

scholarly journals Flavonoids from the Genus Euphorbia: Isolation, Structure, Pharmacological Activities and Structure–Activity Relationships

2021 ◽  
Vol 14 (5) ◽  
pp. 428
Author(s):  
Douglas Kemboi Magozwi ◽  
Mmabatho Dinala ◽  
Nthabiseng Mokwana ◽  
Xavier Siwe-Noundou ◽  
Rui W. M. Krause ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Structure Activity Relationship ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Skeletal Structure ◽  
Activity Relationship ◽  
Hydroxyl Groups ◽  
Structure Activity ◽  
Review Reports

Plants of the genus Euphorbia are widely distributed across temperate, tropical and subtropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohydrate attached at either C-3 or C-7, and were designated as d-glucose, l-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents.

scholarly journals Structure–activity relationship of surface hydroxyl groups during NO2 adsorption and transformation on TiO2 nanoparticles

2017 ◽  
Vol 4 (12) ◽  
pp. 2388-2394 ◽  
Author(s):  
Chang Liu ◽  
Qingxin Ma ◽  
Hong He ◽  
Guangzhi He ◽  
Jinzhu Ma ◽  
...  
Keyword(s):  
Tio2 Nanoparticles ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Hydroxyl Groups ◽  
Surface Hydroxyl ◽  
Surface Hydroxyl Groups ◽  
Structure Activity ◽  
No2 Adsorption ◽  
Relationship Of ◽  
Structure And Activity

The structure and activity of surface hydroxyl groups determined the performance of TiO2 during NO2 reaction.

Cytotoxic and antioxidant effects of methoxylated stilbene analogues on HepG2 hepatoma and Chang liver cells: Implications for structure activity relationship

2010 ◽  
Vol 30 (2) ◽  
pp. 138-144 ◽  
Author(s):  
AH Hasiah ◽  
AR Ghazali ◽  
JFF Weber ◽  
S. Velu ◽  
NF Thomas ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Structure Activity Relationship ◽  
Liver Cells ◽  
Activity Relationship ◽  
Hydroxyl Groups ◽  
Structure Activity ◽  
Total Antioxidant ◽  
Stilbene Analogues ◽  
Chang Liver

Stilbenes possess a variety of biological activities including chemopreventive activity. This study was conducted to evaluate the structural activity relationships of six methoxylated stilbene analogues with respect to their cytotoxic effects and antioxidant activities on HepG2 hepatoma and Chang liver cells. The cytotoxic and total antioxidant activities of six stilbene analogues were determined by MTT and Ferric Reducing Antioxidant Power (FRAP) assays, respectively. We found that the cis-methoxylated stilbene: (Z)-3,4,4'-trimethoxystilbene was the most potent and selective antiproliferative agent (IC50 89 µM) in HepG2 cells. For the total antioxidant activity, compounds possessing hydroxyl groups at the 4' position namely (E)-3-methoxy-4'-hydroxystilbene, (E)-3,5-dimethoxy-4'-hydroxystilbene (pterostilbene), (E)-4-methoxy-4'-hydroxystilbene showed the highest antioxidant activity. Structure activity relationship studies of these compounds demonstrated that the cytotoxic effect and antioxidant activities of the tested compounds in this study were structurally dependent.

Structure–activity relationship of Au/ZrO2 catalyst on formation of hydroxyl groups and its influence on CO oxidation

2013 ◽  
Vol 1 (19) ◽  
pp. 6051 ◽  
Author(s):  
Christopher J. Karwacki ◽  
P. Ganesh ◽  
Paul R. C. Kent ◽  
Wesley O. Gordon ◽  
Gregory W. Peterson ◽  
...  
Keyword(s):  
Co Oxidation ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Hydroxyl Groups ◽  
Structure Activity ◽  
Zro2 Catalyst ◽  
Relationship Of

scholarly journals Inhibition of Lipoxygenase and Peroxidase Reaction by Some Flavonols and Flavones: The Structure-Activity Relationship

2017 ◽  
Vol 12 (11) ◽  
pp. 1934578X1701201
Author(s):  
Zbigniew Sroka ◽  
Alina Sowa ◽  
Andrzej Dryś
Keyword(s):  
Correlation Coefficient ◽  
Antioxidant Properties ◽  
Structure Activity Relationship ◽  
Methoxyl Group ◽  
Activity Relationship ◽  
Hydroxyl Group ◽  
Hydroxyl Groups ◽  
Peroxidase Reaction ◽  
Structure Activity ◽  
Reducing Properties

Some flavonoids were investigated for their effects on lipoxygenase and peroxidase. The strongest inhibitor of lipoxygenase was kaempferol with one hydroxyl group situated at the 4’ position in the B ring, with activity of 21.2±2.03 calculated per μmole of compound. The weakest inhibition was observed for diosmetin with a hydroxyl group at the 3′ position and a methoxyl group at 4′ in the B ring, with activity of 1.17±0.77 per μmole. Peroxidase was most strongly inhibited by quercetin (22.7±0.05) with two hydroxyl groups in the B ring at 3′ and 4′. The weakest inhibitor of peroxidase was genkwanin (0±0.16) with one hydroxyl group at position 4′ in the B ring and methoxyl at position 7 in the A ring. The correlation coefficient between reduction of Fe3+ by flavonoids and inhibition of lipoxygenase by these compounds was 0.72 and the reduction of Fe3+ and inhibition of peroxidase was 0.24. The results show that inhibition of peroxidase is weakly associated with reducing properties of phenols and inhibition of lipoxygenase may be associated with antioxidant properties of flavonoids.

scholarly journals Recently isolated lycodine-type Lycopodium alkaloids and their total synthesis: a review

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Shriniwas P. Patil
Keyword(s):  
Total Synthesis ◽  
Structure Activity Relationship ◽  
Acetylcholine Esterase ◽  
Huperzine A ◽  
Activity Relationship ◽  
Main Body ◽  
Structural Requirement ◽  
Structure Activity ◽  
Lycopodium Alkaloids ◽  
Esterase Inhibitor

Abstract Background Since long back, several plants species belonging to family Lycopodiaceae or Huperziaceae are being traditionally used in treatment of diseases like Alzheimer’s disease and myasthenia gravis. In 1986, huperzine A, structurally lycodine type of alkaloid was isolated and established as potent acetylcholine esterase inhibitor. Hence, further, in pursuit of similar compounds, several hundreds of different types of lycopodium alkaloids have been isolated from different Lycopodiaceae or Huperziaceae plants species. Main body For few of these recently isolated alkaloids, the possible mechanisms of their biosynthesis have been proposed while few of them were tried for their laboratory total asymmetric synthesis. This review summarized lycodine-type Lycopodium alkaloids, whose isolation, biosynthesis, and total synthesis have been reported after 2000. It also includes structure–activity relationship. Short conclusion More than 40 lycodine-type alkaloids have been isolated and structurally elucidated since 2000. Their biosynthetic pathway suggested that they got biosynthesized from lysine, while structure–activity relationship established the structural requirement of lycodine-type alkaloids to possess potent acetylcholine esterase inhibitory activity.

Flavonoids inhibiting glycation of bovine serum albumin: affinity–activity relationship

2015 ◽  
Vol 69 (3) ◽  
Author(s):  
Quan Liu ◽  
Ting-Ting Chen ◽  
Hui Cao
Keyword(s):  
Bovine Serum Albumin ◽  
Serum Albumin ◽  
Bovine Serum ◽  
Structure Activity Relationship ◽  
Optimal Number ◽  
Protein Glycation ◽  
Activity Relationship ◽  
Hydroxyl Groups ◽  
Structure Activity

AbstractProtein glycation leads to the formation of advanced glycation end-products (AGEs), which contribute to the pathogenesis of diabetic complications. The structure-activity relationship of dietary flavonoids for inhibiting the glycation of bovine serum albumin (BSA) in vitro was subjected to a detailed investigation. The structure-activity relationship revealed that: 1) the hydroxylation on ring B of the flavones enhanced the inhibition and the hydroxyl groups at the C-5 and C-7 positions of flavones favoured the inhibition; 2) the optimal number of hydroxyl groups on ring B of the flavonols was one (at the C-3 position) and the methylation of flavonols weakened the inhibition; 3) the methoxylation at the C-6 position and methylation at C-4' position of genistein clearly enhanced the inhibition; 4) the hydroxyl groups at the C-5 and C-7 positions of flavanones were in favour of the inhibition; 5) the glycosylation of flavonoids significantly weakened the inhibition. Obvious linear affinity-activity relationships exist between the BSA-flavonoid interaction and flavonoids as BSA glycation inhibitors (R

scholarly journals Structure–Activity Relationship of Oligomeric Flavan-3-ols: Importance of the Upper-Unit B-ring Hydroxyl Groups in the Dimeric Structure for Strong Activities

Molecules ◽  
2015 ◽  
Vol 20 (10) ◽  
pp. 18870-18885 ◽  
Author(s):  
Yoshitomo Hamada ◽  
Syota Takano ◽  
Yoshihiro Ayano ◽  
Masahiro Tokunaga ◽  
Takahiro Koashi ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Hydroxyl Groups ◽  
Dimeric Structure ◽  
Structure Activity ◽  
Relationship Of
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