Non-Peptidic, Non-Prenylic Bisubstrate Farnesyltransferase Inhibitors. Effect of a Carboxyl Group at the Central Group on Farnesyltransferase Inhibitory Activity

2000 ◽  
Vol 6 (11) ◽  
pp. 507-512 ◽  
Author(s):  
M. Schlitzer ◽  
I. Sattler
2006 ◽  
Vol 1 (5) ◽  
pp. 1934578X0600100 ◽  
Author(s):  
Jie Liu ◽  
Kuniyoshi Shimizu ◽  
Ryuichiro Kondo

By means of 5α-reductase inhibitory activity-guided fractionation, a new lanostanoid, 15α-hydroxy-3-oxolanosta- 7, 9(11), 24(E)-trien-26-oic acid, named as ganoderic acid TR, was isolated from the ethanol extract of the fruiting bodies of Ganoderma lucidum (Fr.) Karst (Ganodermataceae). The compound showed potent inhibitory activity with an IC50 of 8.5 μM. Modified Mosher's method established the S-configuration of the secondary hydroxyl group at C-15. In addition, a carboxyl group on the side chain of ganoderic acid TR is essential to elicit the inhibitory activity because of the considerably lower activity of its methyl ester.


Author(s):  
Pınar Ercan ◽  
Sedef Nehir El

Abstract. The goals of this study were to determine and evaluate the bioaccessibility of total anthocyanin and procyanidin in apple (Amasya, Malus communis), red grape (Papazkarası, Vitis vinifera) and cinnamon (Cassia, Cinnamomum) using an in vitro static digestion system based on human gastrointestinal physiologically relevant conditions. Also, in vitro inhibitory effects of these foods on lipid (lipase) and carbohydrate digestive enzymes (α-amylase and α-glucosidase) were performed with before and after digested samples using acarbose and methylumbelliferyl oleate (4MUO) as the positive control. While the highest total anthocyanin content was found in red grape (164 ± 2.51 mg/100 g), the highest procyanidin content was found in cinnamon (6432 ± 177.31 mg/100 g) (p < 0.05). The anthocyanin bioaccessibilities were found as 10.2 ± 1%, 8.23 ± 0.64%, and 8.73 ± 0.70% in apple, red grape, and cinnamon, respectively. The procyanidin bioaccessibilities of apple, red grape, and cinnamon were found as 17.57 ± 0.71%, 14.08 ± 0.74% and 18.75 ± 1.49%, respectively. The analyzed apple, red grape and cinnamon showed the inhibitory activity against α-glucosidase (IC50 544 ± 21.94, 445 ± 15.67, 1592 ± 17.58 μg/mL, respectively), α-amylase (IC50 38.4 ± 7.26, 56.1 ± 3.60, 3.54 ± 0.86 μg/mL, respectively), and lipase (IC50 52.7 ± 2.05, 581 ± 54.14, 49.6 ± 2.72 μg/mL), respectively. According to our results apple, red grape and cinnamon have potential to inhibit of lipase, α-amylase and α-glucosidase digestive enzymes.


Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
M Ishibashi ◽  
S Hanazawa ◽  
Y Uchino ◽  
X Li ◽  
MA Arai

Planta Medica ◽  
2011 ◽  
Vol 77 (12) ◽  
Author(s):  
IJ Sousa ◽  
J Molnar ◽  
MU Ferreira ◽  
MX Fernandes

Sign in / Sign up

Export Citation Format

Share Document