Quercetin Therapy for Selected Patients with PIM1 Kinase-Positive Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma: A Pilot Study

Baron, Beverly W.; Thirman, Michael J.; Giurcanu, Mihai; Baron, Joseph M.

doi:10.1159/000486361

Cited by 10 publications

(12 citation statements)

References 15 publications

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“…Merkel et al reported that PIM1 kinase had the potential as a target for cancer therapy [37]. Besides, many reports have shown that the activity of PIM1 could be inhibited by quercetin [38,39]. In our study, Figure 5 showed that the quercetin regulated the PIM1, which was involved in the breast cancer.…”

Section: Discussionsupporting

confidence: 58%

PIM1, CYP1B1, and HSPA2 Targeted by Quercetin Play Important Roles in Osteoarthritis Treatment by Achyranthes bidentata

Tian

Peng

et al. 2019

Evidence-Based Complementary and Alternative Medicine

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Aim. Achyranthes bidentata is one of the most commonly used Chinese herbal medicines (CHM) that is currently considered for the treatment of osteoarthritis. The purpose of this study was to reveal the mechanism of Achyranthes bidentata in osteoarthritis treatment based on the network pharmacology. Methods. The effective components of Achyranthes bidentata were firstly screened out from the TCMSP database with ADME property parameters. Then, osteoarthritis-related proteins targeted by the effective components were predicted based on the DrugBank and CTD databases. Subsequently, enrichment analysis and interaction network between targets of effective components and pathways were also studied. In addition, the differentially expressed genes (DEGs) of GSE55457 were used for validation of the osteoarthritis-related target proteins. Finally, the effective components–target molecular docking models were predicted. Results. A total of 10 effective components were identified, of which kaempferol and quercetin had 1 and 29 targets, respectively. There were 26 target proteins of quercetin related to the osteoarthritis. These targets were mainly enriched in mitochondrial ATP synthesis coupled proton transport, cellular response to estradiol stimulus, and nitric oxide biosynthetic process. In addition, there were three common proteins, PIM1, CYP1B1, and HSPA2 based on the DEGs of GSE55457, which were considered as the key targeted proteins of the quercetin. Conclusion. The docking of PIM1-quercetin, CYP1B1-quercetin, and HSPA2-quercetin may play important roles during the treatment of osteoarthritis by Achyranthes bidentata.

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Section: Discussionsupporting

confidence: 58%

PIM1, CYP1B1, and HSPA2 Targeted by Quercetin Play Important Roles in Osteoarthritis Treatment by Achyranthes bidentata

Tian

Peng

et al. 2019

Evidence-Based Complementary and Alternative Medicine

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“…34,35 Besides, quercetin owned the phytoestrogen-like activity, which is likely via the interaction with the estrogen receptor β. 36,37…”

Section: Resultsmentioning

confidence: 99%

“…34,35 Besides, quercetin owned the phytoestrogen-like activity, which is likely via the interaction with the estrogen receptor β. 36,37 We mapped the 143 predicted targets into the KEGG pathway database. Many targets are related to the metabolic pathways (43 targets), cancer pathways (23 targets), PI3K-Akt signaling pathway (21 targets), Ras signaling pathway (20 targets), and so on.…”

Section: Acs Omegamentioning

confidence: 99%

Large-Scale Target Identification of Herbal Medicine Using a Reverse Docking Approach

Zhang

Pan²,

et al. 2019

ACS Omega

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Herbal medicine has been used to countermine various diseases for centuries. However, most of the therapeutic targets underlying herbal therapy remain unclear, which largely slow down the novel drug discovery process from natural products. In this study, we developed a novel computational pipeline for assisting de novo identification of protein targets for herbal ingredients. The pipeline involves pharmacophore comparison and reverse ligand–protein docking simulation in a high throughput manner. We evaluated the pipeline using three traditional Chinese medicine ingredients such as acteoside, quercetin, and epigallocatechin gallate as examples. A majority of current known targets of these ingredients were successfully identified by the pipeline. Structural comparative analyses confirmed that the predicted ligand–target interactions used the same binding pockets and binding modes as those of known ligand–target interactions. Furthermore, we illustrated the mechanism of actions of the ingredients by constructing the pharmacological networks on the basis of the predicted target profiles. In summary, we proposed an efficient and economic option for large-scale target exploration in the herb study. This pipeline will be particularly valuable in aiding precise drug discovery and drug repurposing from natural products.

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“…Among these, its antileukemic effect has attracted increasing attention in recent years. In a pilot study, QUE demonstrated the potential of stabilizing the rising lymphocyte counts of patients with PIM1 kinase-positive chronic lymphocytic leukemia 2. The antileukemic action of QUE was also verified in a xenograft model of human leukemia HL60 cells 3.…”

Section: Introductionmentioning

confidence: 92%

<p>Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect</p>

Yin

Hou

Song

et al. 2019

IJN

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Background: Quercetin (QUE) shows a potential antileukemic activity, but possesses poor solubility and low bioavailability. Purpose: This article explored the bile salt transport pathway for oral deliver of QUE using cholate-modified polymer-lipid hybrid nanoparticles (cPLNs) aiming to enhance its antileukemic effect. Methods: QUE-loaded cPLNs (QUE-cPLNs) were developed through a nanoprecipitation technique and characterized by particle size, entrapment efficiency (EE), microscopic morphology and in vitro drug release. In vitro cellular uptake and cytotoxicity of QUE-cPLNs were examined on Caco-2 and P388 cells; in vivo pharmacokinetics and antileukemic effect were evaluated using Sprague Dawley rats and leukemic model mice, respectively. Results: The prepared QUE-cPLNs possessed a particle size of 110 nm around with an EE of 96.22%. QUE-cPLNs resulted in significantly enhanced bioavailability of QUE, up to 375.12% relative to the formulation of suspensions. In addition, QUE-cPLNs exhibited excellent cellular uptake and internalization capability compared to cholate-free QUE-PLNs. The in vitro cytotoxic and in vivo antileukemic effects of QUE-cPLNs were also signally superior to free QUE and QUE-PLNs. Conclusion: These findings indicate that cPLNs are a promising nanocarrier able to improve the oral bioavailability and therapeutic index of QUE.

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Quercetin Therapy for Selected Patients with PIM1 Kinase-Positive Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma: A Pilot Study

Cited by 10 publications

References 15 publications

PIM1, CYP1B1, and HSPA2 Targeted by Quercetin Play Important Roles in Osteoarthritis Treatment by Achyranthes bidentata

PIM1, CYP1B1, and HSPA2 Targeted by Quercetin Play Important Roles in Osteoarthritis Treatment by Achyranthes bidentata

Large-Scale Target Identification of Herbal Medicine Using a Reverse Docking Approach

<p>Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect</p>

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