scholarly journals Inhibitory effects of caffeine analogues on neoplastic transformation: structure-activity relationship

2008 ◽  
Vol 29 (6) ◽  
pp. 1228-1234 ◽  
Author(s):  
E. A. Rogozin ◽  
K. W. Lee ◽  
N. J. Kang ◽  
H. Yu ◽  
M. Nomura ◽  
...  
Keyword(s):  
Neoplastic Transformation ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Inhibitory Effects ◽  
Structure Activity ◽  
Transformation Structure

scholarly journals The Inhibitory Effects of Plant Derivate Polyphenols on the Main Protease of SARS Coronavirus 2 and Their Structure–Activity Relationship

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1924
Author(s):  
Thi Thanh Hanh Nguyen ◽  
Jong-Hyun Jung ◽  
Min-Kyu Kim ◽  
Sangyong Lim ◽  
Jae-Myoung Choi ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Garlic Extract ◽  
Activity Relationship ◽  
Hydroxyl Group ◽  
Inhibitory Effects ◽  
Structure Activity ◽  
Main Protease ◽  
Ic50 Values ◽  
Km Value ◽  
Novel Coronavirus

The main protease (Mpro) is a major protease having an important role in viral replication of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the novel coronavirus that caused the pandemic of 2020. Here, active Mpro was obtained as a 34.5 kDa protein by overexpression in E. coli BL21 (DE3). The optimal pH and temperature of Mpro were 7.5 and 37 °C, respectively. Mpro displayed a Km value of 16 μM with Dabcyl-KTSAVLQ↓SGFRKME-Edans. Black garlic extract and 49 polyphenols were studied for their inhibitory effects on purified Mpro. The IC50 values were 137 μg/mL for black garlic extract and 9–197 μM for 15 polyphenols. The mixtures of tannic acid with puerarin, daidzein, and/or myricetin enhanced the inhibitory effects on Mpro. The structure–activity relationship of these polyphenols revealed that the hydroxyl group in C3′, C4′, C5′ in the B-ring, C3 in the C-ring, C7 in A-ring, the double bond between C2 and C3 in the C-ring, and glycosylation at C8 in the A-ring contributed to inhibitory effects of flavonoids on Mpro.

Structure-activity relationship of the inhibitory effects of flavonoids on nitric oxide production in RAW264.7 cells

2017 ◽  
Vol 25 (2) ◽  
pp. 779-788 ◽  
Author(s):  
Wen-Jun Jiang ◽  
Akihiro Daikonya ◽  
Mitsuyoshi Ohkawara ◽  
Takashi Nemoto ◽  
Ryusuke Noritake ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Raw264.7 Cells ◽  
Nitric Oxide Production ◽  
Inhibitory Effects ◽  
Oxide Production ◽  
Structure Activity ◽  
Relationship Of

Structure–activity relationship of human GLO I inhibitory natural flavonoids and their growth inhibitory effects

2008 ◽  
Vol 16 (7) ◽  
pp. 3969-3975 ◽  
Author(s):  
Ryoko Takasawa ◽  
Saki Takahashi ◽  
Kazunori Saeki ◽  
Satoshi Sunaga ◽  
Atsushi Yoshimori ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Inhibitory Effects ◽  
Structure Activity ◽  
Growth Inhibitory ◽  
Relationship Of
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