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

Cheng, Yueming; Yang, Yan; Wu, Yan-Guang; Wang, Wencheng; Xiao, Lichun; Zhang, Yifan; Tang, Justin; Huang, Yadong; Zhang, Shu; Xiang, Qi

doi:10.3389/fphar.2020.00637

Cited by 8 publications

(3 citation statements)

References 24 publications

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“…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%

Attenuation of Scopolamine-Induced Amnesia via Cholinergic Modulation in Mice by Synthetic Curcumin Analogs

et al. 2022

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Alzheimer’s disease is an emerging health disorder associated with cognitive decline and memory loss. In this study, six curcumin analogs (1a–1f) were synthesized and screened for in vitro cholinesterase inhibitory potential. On the basis of promising results, they were further investigated for in vivo analysis using elevated plus maze (EPM), Y-maze, and novel object recognition (NOR) behavioral models. The binding mode of the synthesized compounds with the active sites of cholinesterases, and the involvement of the cholinergic system in brain hippocampus was determined. The synthesized curcumin analog 1d (p < 0.001, n = 6), and 1c (p < 0.01, n = 6) showed promising results by decreasing retention time in EPM, significantly increasing % SAP in Y-maze, while significantly (p < 0.001) enhancing the % discrimination index (DI) and the time exploring the novel objects in NORT mice behavioral models. A molecular docking study using MOE software was used for validation of the inhibition of cholinesterase(s). It has been indicated from the current research work that the synthesized curcumin analogs enhanced memory functions in mice models and could be used as valuable therapeutic molecules against neurodegenerative disorders. To determine their exact mechanism of action, further studies are suggested.

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Section: Discussionsupporting

confidence: 84%

Attenuation of Scopolamine-Induced Amnesia via Cholinergic Modulation in Mice by Synthetic Curcumin Analogs

et al. 2022

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“…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%

Review of Curcumin and Its Different Formulations: Pharmacokinetics, Pharmacodynamics and Pharmacokinetic-Pharmacodynamic Interactions

Goswami¹,

Saxena²,

Yadav³

et al. 2022

OBM Integr Complement Med

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Curcumin, the yellow principle of the Indian Turmeric, ‘Haldi’ has recently attracted renewed interest in the field of experimental medicine with pleiotropic activity. This review has emphasized three pharmaceutical studies of interest: the pharmacokinetics, pharmacology, and pharmacodynamics of curcumin. In this review, we attempted to review the general pharmacokinetics profile, pharmacokinetic interactions, and pharmacokinetic-pharmacodynamic interactions of curcumin and its formulations. Different species of turmeric in India, as well as their cultivars, different forms of curcumin, and harvesting methods have also been discussed. Furthermore, pharmacokinetic studies of the interaction of curcumin and its different formulations with efflux transporters such as P-glycoprotein, ABC-transporter protein, multidrug-resistant protein, and cytochrome p450 metabolism enzymes have been broadly explained following data from preclinical and clinical trials reported in the literature. A few interesting chemical interactions between curcumin and its metabolites with the receptor have also been described. The pharmacological activities of curcumin and its related formulations and products have been reviewed in a few targeted disease pathologies of national concern, such as cancer, gastroduodenal disorder, immunodeficiency, liver disease, ophthalmology, diabetes and osteoarthritis among other metabolic diseases, and microbial and viral infections. The pharmacodynamics of curcumin, especially regarding the potassium/calcium ion channel pathway, apoptosis, calcium signaling pathway, endoplasmic reticulum stress, and other intracellular signaling pathways, have been documented. Lastly, the use of curcumin as a cosmetic and the value chain analysis of turmeric products, as well as curcumin, have also been placed appropriately. A total of 174 publications were reviewed and, overall, this review tried to cover various important therapeutic aspects of curcumin, which can generate new research interest in general.

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“…Even though findings are inconsistent, a relationship between sex hormones such as estrogen and testosterone and depression has been identified [ 180 , 181 ]. Curcumin can influence multiple pathways associated with estrogen receptor expression and signalling [ 182 , 183 ], and, in an animal study, ameliorated fluoxetine-induced reductions in testosterone [ 184 ] and influenced the activity of 17β-hydroxysteroid dehydrogenase, an enzyme involved in the biosynthesis of testosterone [ 185 ].…”

Section: Curcumin’s Potential Antidepressant Mechanisms Of Actionmentioning

confidence: 99%

Potential Role of Curcumin for the Treatment of Major Depressive Disorder

Lopresti

2022

CNS Drugs

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Curcumin is the major biologically active polyphenolic constituent in the turmeric plant (Curcuma longa) that has been shown to have antioxidant, anti-inflammatory, neuroprotective, anticancer, antimicrobial, and cardioprotective effects. Interest in curcumin as a treatment for mental health conditions has increased and there is an expanding body of preclinical and clinical research examining its antidepressant and anxiolytic effects. In this narrative review, human trials investigating the effects of curcumin for the treatment of depression or depressive symptoms are summarised. Using findings from in vitro, animal, and human trials, possible biological mechanisms associated with the antidepressant effects of curcumin are also explored. To increase the understanding of curcumin for the treatment of depression, directions for future research are proposed. Key PointsEvidence from animal and human trials confirms curcumin is a promising treatment for depression.Curcumin has multiple biological actions that may account for its antidepressant effects.More research is required to increase the understanding of the antidepressant effects of curcumin.

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

Cited by 8 publications

References 24 publications

Attenuation of Scopolamine-Induced Amnesia via Cholinergic Modulation in Mice by Synthetic Curcumin Analogs

Attenuation of Scopolamine-Induced Amnesia via Cholinergic Modulation in Mice by Synthetic Curcumin Analogs

Review of Curcumin and Its Different Formulations: Pharmacokinetics, Pharmacodynamics and Pharmacokinetic-Pharmacodynamic Interactions

Potential Role of Curcumin for the Treatment of Major Depressive Disorder

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