Evidence map›Paper›PMID 32431503›Full record

ArticleInternational journal of nanomedicine2020

A Mansonone Derivative Coupled with Monoclonal Antibody 4D5-Modified Chitosan Inhibit AKR1C3 to Treat Castration-Resistant Prostate Cancer.

Meng Zhou, Xiaoyu Wang, Jie Xia, Yating Cheng, Lichun Xiao, Yu Bei, Jianzhong Tang, Yadong Huang, Qi Xiang, Shiliang Huang

Open access · goldAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in International journal of nanomedicine, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.4field-weighted citation impact, top 42% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

5 citing papers in PubMed, 8 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Article
  5. Dysregulated androgen synthesis and anti-androgen resistance in advanced prostate cancer.American journal of clinical and experimental urology · 2021
    Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 2 institutions in 1 country.

Meng Zhou *Institute of Biomedicine and Guangdong Provincial Key Laboratory of Bioengineering Medicine, Jinan University, Guangzhou 510632, People's Republic of China.
Xiaoyu Wang *Institute of Biomedicine and Guangdong Provincial Key Laboratory of Bioengineering Medicine, Jinan University, Guangzhou 510632, People's Republic of China.
Jie XiaSchool of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, People's Republic of China.ORCID 0000-0002-5005-3069
Yating ChengInstitute of Biomedicine and Guangdong Provincial Key Laboratory of Bioengineering Medicine, Jinan University, Guangzhou 510632, People's Republic of China.
Lichun XiaoInstitute of Biomedicine and Guangdong Provincial Key Laboratory of Bioengineering Medicine, Jinan University, Guangzhou 510632, People's Republic of China.
Yu BeiBiopharmaceutical R&D Center of Jinan University, Guangzhou 510630, People's Republic of China.
Jianzhong TangBiopharmaceutical R&D Center of Jinan University, Guangzhou 510630, People's Republic of China.
Yadong HuangInstitute of Biomedicine and Guangdong Provincial Key Laboratory of Bioengineering Medicine, Jinan University, Guangzhou 510632, People's Republic of China.ORCID 0000-0002-8879-3273
Qi XiangInstitute of Biomedicine and Guangdong Provincial Key Laboratory of Bioengineering Medicine, Jinan University, Guangzhou 510632, People's Republic of China.
Shiliang HuangSchool of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, People's Republic of China.
Jinan University · CNSun Yat-sen University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeAldo-ketoreductase (AKR) 1C3 is crucial for testosterone synthesis. Abnormally high expression/activity of AKR1C3 can promote castration-resistant prostate cancer (CRPC). A mansonone derivative and AKR1C3 inhibitor, 6e, was combined with 4D5 (extracellular fragment of the monoclonal antibody of human epidermal growth factor receptor-2)-modified chitosan to achieve a nanodrug-delivery system (CS-4D5/6e) to treat CRPC. MATERIALS AND

methodsMorphologies/properties of CS-4D5/6e were characterized by atomic force microscopy, zeta-potential analysis, and Fourier transform-infrared spectroscopy. CS-4D5/6e uptake was measured by immunofluorescence under confocal laser scanning microscopy. Testosterone in LNCaP cells overexpressing human AKR1C3 (LNCaP-AKR1C3) and cell lysates was measured to reflect AKR1C3 activity. Androgen receptor (AR) and prostate-specific antigen (PSA) expression was measured by Western blotting. CS-4D5/6e-based inhibition of AKR1C3 was evaluated in tumor-xenografted mice.

resultsCS-4D5/6e was oblate, with a particle size of 200-300 nm and thickness of 1-5 nm. Zeta potential was 1.39±0.248 mV. 6e content in CS-4D5/6e was 7.3±1.4% and was 18±3.6% for 4D5. 6e and CS-4D5/6e inhibited testosterone production significantly in a concentration-dependent manner in LNCaP-AKR1C3 cells, and a decrease in expression of AKR1C3, PSA, and AR was noted. Half-maximal inhibitory concentration of CS-4D5/6e on LNCaP-AKR1C3 cells was significantly lower than that in LNCaP cells (

conclusionWe demonstrated the antineoplastic activity of a potent AKR1C3 inhibitor (6e) and its nanodrug-delivery system (CS-4D5/6e). First, CS-4D5/6e targeted HER2-positive CRPC cells. Second, it transferred 6e (an AKR1C3 inhibitor) to achieve a reduction in intratumoral testosterone production. Compared with 6e, CS-4D5/6e showed lower systemic toxicity. CS-4D5/6e inhibited tumor growth effectively in mice implanted with tumor xenografts by downregulating testosterone production mediated by intratumoral AKR1C3. These results showed a promising strategy for treatment of the CRPC that develops invariably in prostate-cancer patients.

Indexed as

Aldo-Keto Reductase Family 1 Member C3AnimalsAntibodies, MonoclonalAntineoplastic AgentsCell Line, TumorChitosanDrug Delivery SystemsErb-b2 Receptor Tyrosine KinasesHumansMaleMice, Inbred BALB CMolecular Targeted TherapyNanostructuresNaphthoquinonesProstate-Specific AntigenProstatic Neoplasms, Castration-ResistantAKR1C3 protein, humanAldo-Keto Reductase Family 1 Member C3Antibodies, MonoclonalAntineoplastic AgentsAR protein, humanChitosanERBB2 protein, humanErb-b2 Receptor Tyrosine Kinasesmansonone FNaphthoquinonesProstate-Specific AntigenReceptors, AndrogenSesquiterpenesTestosteronecastration-resistant prostate cancerconjugate of HER2 monoclonal antibody extracellular fragment 4D5mansonone derivative

Identifiers

PMID32431503
PMCPMC7200237
OpenAlexW3023503912

What OpenQuestion holds

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LicenceCC BY-NC
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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.