scholarly journals Potent HAT Inhibitory Effect of Aqueous Extract from Roots of Platycodon grandiflorum on Androgen Receptor‐mediated Transcriptional Regulation

2007 ◽  
Vol 21 (6) ◽  
Author(s):  
HEEBUM KANG ◽  
Yoo‐Hyun Lee ◽  
Kyung Chul Choi ◽  
Hyo Kyoung Choi ◽  
Ho Geun Yoon
2019 ◽  
Vol 12 (2) ◽  
pp. 89
Author(s):  
Janeen H. Trembley ◽  
Betsy T. Kren ◽  
Md. J. Abedin ◽  
Daniel P. Shaughnessy ◽  
Yingming Li ◽  
...  

The prosurvival protein kinase CK2, androgen receptor (AR), and nuclear factor kappa B (NFκB) interact in the function of prostate cells, and there is evidence of crosstalk between these signals in the pathobiology of prostate cancer (PCa). As CK2 is elevated in PCa, and AR and NFκB are involved in the development and progression of prostate cancer, we investigated their interaction in benign and malignant prostate cells in the presence of altered CK2 expression. Our results show that elevation of CK2 levels caused increased levels of AR and NFκB p65 in prostate cells of different phenotypes. Analysis of TCGA PCa data indicated that AR and CK2α RNA expression are strongly correlated. Small molecule inhibition or molecular down-regulation of CK2 caused reduction in AR mRNA expression and protein levels in PCa cells and in orthotopic xenograft tumors by various pathways. Among these, regulation of AR protein stability plays a unifying role in CK2 maintenance of AR protein levels. Our results show induction of various endoplasmic reticulum stress signals after CK2 inhibition, which may play a role in the PCa cell death response. Of note, CK2 inhibition caused loss of cell viability in both parental and enzalutamide-resistant castrate-resistant PCa cells. The present work elucidates the specific link of CK2 to the pathogenesis of PCa in association with AR and NFκB expression; further, the observation that inhibition of CK2 can exert a growth inhibitory effect on therapy-resistant PCa cells emphasizes the potential utility of CK2 inhibition in patients who are on enzalutamide treatment for advanced cancer.


Author(s):  
Shah Asma Farooq ◽  
Randhir Singh

Abstract Introduction: Murraya koenigii (L.) and Ficus carica L. are traditionally used plants with significant medicinal and nutritional values. Aim and Objective: The present study was focused on the evaluation of hydro-alcoholic and aqueous extracts of M. koenigii (L.) leaves [MKHA (M. koenigii (L.) hydro-alcoholic extract) and MKAQ (M.koenigii (L.) aqueous extract)] and dried fruits of F. carica L. [FCHA (F. carica L. hydro-alcoholic extract) and FCAQ (F. carica L. aqueous extract)] in the attenuation of markers of microvascular complications associated with diabetes mellitus which can be further used to investigate the pharmacological activity of these plants in treatment of diabetes and its complications. Material and Method: The attenuating effect of the extracts was evaluated by calculating the ALR1 enzyme inhibition in a kidney of Wistar rat, anti-glycation activity in bovine serum albumin (BSA) and erythrocyte sorbitol accumulation inhibition in heparinized human blood. Results: A significant inhibitory effect (IC50 6.47μg/ml,7.26μg/ml,8.93 μg/ml and 9.66μg/ml) was observed with different concentrations of extracts (MKHA, MKAQ, FCHA and FCAQ) respectively, against ALR enzyme. After the 4th week of incubation, the inhibition of AGEs formation by MKHA, MKAQ, FCHA and FCAQ (500μg/ml) was found to be 82.58%, 78.58%, 74.39% and 69.56% respectively. MKHA, MKAQ, FCHA and FCAQ were found to exhibit significant inhibition against the accumulation of sorbitol in RBCs with IC50 188.88 μg/ml, 247.74μg/ml, 291.94μg/ml and 345.34μg/ml, respectively. Conclusion: The administration of different concentrations of MKHA, MKAQ, FCHA and FCAQ significantly attenuated ALR, AGEs and sorbitol accumulation; hence, it can provide a basis for identification and development of new inhibitors of these biomarkers.


1969 ◽  
Vol 73 (3) ◽  
pp. 337-346 ◽  
Author(s):  
J. P. Battle ◽  
W. J. Whittington

SummaryEvidence was obtained for the presence of germination inhibitors in the aqueous extract from sugar-beet clusters. A positive correlation was shown between the germination of cress seeds moistened with aqueous extracts from clusters of twenty sugarbeet plants and the germination characteristics of other clusters from the same plants. Inhibition was thus greater in extracts from clusters with poor rather than good germination, and also in extracts from immature clusters or those which had received overhead irrigation. The inhibitory effect was found to be located in the perianth and pericarp tissue rather than in the true seed.


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