2020
DOI: 10.3389/fphar.2020.00637
|View full text |Cite
|
Sign up to set email alerts
|

The Curcumin Derivative, H10, Suppresses Hormone-Dependent Prostate Cancer by Inhibiting 17β-Hydroxysteroid Dehydrogenase Type 3

Abstract: The 17b-hydroxysteroid dehydrogenase type 3 (17b-HSD3) enzyme is a potential therapeutic target for hormone-dependent prostate cancer, as it is the key enzyme in the last step of testosterone (T) biosynthesis. A curcumin analog, H10, was optimized for inhibiting T production in LC540 cells that stably overexpressed 17b-HSD3 enzyme (LC540 [17b-HSD3]) (P < 0.01), without affecting progesterone (P) synthesis. H10 downregulated the production of T in the microsomal fraction of rat testes containing the 17b-HSD3 en… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
2
1
1
1

Citation Types

1
5
0

Year Published

2022
2022
2025
2025

Publication Types

Select...
7
1

Relationship

0
8

Authors

Journals

citations
Cited by 9 publications
(6 citation statements)
references
References 24 publications
1
5
0
Order By: Relevance
“…The docking of the synthesized compounds were successfully correlated with the three dimensional crystallographic structures of the compound, specifically 1d, as observed against AChE and BuChE, given the in vitro results of 1d structure similarities with the calculated binding affinities of (−12.089 kcal/mol) and (−10.962 kcal/mol), respectively [25]. The compound 1d with chloride substituent on a phenyl ring showed higher enzyme inhibitory potential when compared to other analogs, which was parallel with the previous finding [26].…”
Section: Discussionsupporting
confidence: 84%
“…The docking of the synthesized compounds were successfully correlated with the three dimensional crystallographic structures of the compound, specifically 1d, as observed against AChE and BuChE, given the in vitro results of 1d structure similarities with the calculated binding affinities of (−12.089 kcal/mol) and (−10.962 kcal/mol), respectively [25]. The compound 1d with chloride substituent on a phenyl ring showed higher enzyme inhibitory potential when compared to other analogs, which was parallel with the previous finding [26].…”
Section: Discussionsupporting
confidence: 84%
“…The experimental group consisted of 132 mice, whereas the control group consisted of 131 mice, resulting in a total of 263 mice used in the study. Among the included studies, 13 originated in China ( Limin et al, 2007 ; Qi, 2009 ; ZHAO et al, 2010 ; LI et al, 2013 ; Zhang, 2013 ; Huang et al, 2015 ; QI et al, 2015 ; Yang et al, 2015 ; Ye, 2015 ; Roy et al, 2016 ; Zhao et al, 2018 ; MAO et al, 2019 ; Cheng et al, 2020 ). Additionally, three studies were conducted in the United States ( Dorai et al, 2001 ; Khor et al, 2006 ; Barve et al, 2008 ), while one study was conducted in Spain ( Fernández-Martínez et al, 2009 ).…”
Section: Resultsmentioning
confidence: 99%
“…Twelve studies ( Dorai et al, 2001 ; Higgins and Thompson, 2002 ; Khor et al, 2006 ; Limin et al, 2007 ; Fernández-Martínez et al, 2009 ; ZHAO et al, 2010 ; LI et al, 2013 ; Zhang, 2013 ; Hooijmans et al, 2014a ; Huang et al, 2015 ; Yang et al, 2015 ; Ye, 2015 ; Roy et al, 2016 ; Zhao et al, 2018 ; Cheng et al, 2020 ) included in the analysis provided data on the tumor volume. The findings revealed a noteworthy suppressive effect of curcumin on PCa tumor volume in mice compared to that in the control groups (SMD: 1.16, 95% CI: 0.52, 1.80, p < 0.001).…”
Section: Resultsmentioning
confidence: 99%
“…In addition, H10 was found to have weaker inhibitory activity towards liver CYP3A4, even after long-term administration [64]. H10 was also reported to inhibit the Adione-stimulated growth of prostate cancer cell xenografts established in nude mice [65].…”
Section: Pharmacokinetics Of Different Curcumin Dosage Preparationsmentioning
confidence: 97%