Evidence map›Paper›PMID 38771401›Full record

ArticleNatural products and bioprospecting2024

Metabolism characterization and toxicity of N-hydap, a marine candidate drug for lung cancer therapy by LC-MS method.

Jindi Lu, Weimin Liang, Yiwei Hu, Xi Zhang, Ping Yu, Meiqun Cai, Danni Xie, Qiong Zhou, Xuefeng Zhou, Yonghong Liu and 3 more

Erratum issuedAbstract read
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In one paragraph

Article in Natural products and bioprospecting, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–field-weighted citation impact
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

2 citing papers in PubMed.

  1. Cytotoxic Cytochalasans from Sponge-DerivedMolecules (Basel, Switzerland) · 2025
    Article
  2. Article
4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

13 authors.

Jindi Lu *NMPA Key Laboratory for Research and Evaluation of Drug Metabolism, Guangdong Provincial Key Laboratory of New Drug Screening, Guangdong-Hong Kong-Macao Joint Laboratory for New Drug Screening, Southern Medical University Hospital of Integrated Traditional Chinese and Western Medicine, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China.
Weimin Liang *NMPA Key Laboratory for Research and Evaluation of Drug Metabolism, Guangdong Provincial Key Laboratory of New Drug Screening, Guangdong-Hong Kong-Macao Joint Laboratory for New Drug Screening, Southern Medical University Hospital of Integrated Traditional Chinese and Western Medicine, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China.
Yiwei HuCAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, 510301, China.
Xi ZhangNMPA Key Laboratory for Research and Evaluation of Drug Metabolism, Guangdong Provincial Key Laboratory of New Drug Screening, Guangdong-Hong Kong-Macao Joint Laboratory for New Drug Screening, Southern Medical University Hospital of Integrated Traditional Chinese and Western Medicine, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China.
Ping YuNMPA Key Laboratory for Research and Evaluation of Drug Metabolism, Guangdong Provincial Key Laboratory of New Drug Screening, Guangdong-Hong Kong-Macao Joint Laboratory for New Drug Screening, Southern Medical University Hospital of Integrated Traditional Chinese and Western Medicine, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China.
Meiqun CaiNMPA Key Laboratory for Research and Evaluation of Drug Metabolism, Guangdong Provincial Key Laboratory of New Drug Screening, Guangdong-Hong Kong-Macao Joint Laboratory for New Drug Screening, Southern Medical University Hospital of Integrated Traditional Chinese and Western Medicine, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China.
Danni XieNMPA Key Laboratory for Research and Evaluation of Drug Metabolism, Guangdong Provincial Key Laboratory of New Drug Screening, Guangdong-Hong Kong-Macao Joint Laboratory for New Drug Screening, Southern Medical University Hospital of Integrated Traditional Chinese and Western Medicine, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China.
Qiong ZhouNMPA Key Laboratory for Research and Evaluation of Drug Metabolism, Guangdong Provincial Key Laboratory of New Drug Screening, Guangdong-Hong Kong-Macao Joint Laboratory for New Drug Screening, Southern Medical University Hospital of Integrated Traditional Chinese and Western Medicine, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China.
Xuefeng ZhouCAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, 510301, China.
Yonghong LiuCAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, 510301, China.
Junfeng WangCAS Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, 510301, China. wangjunfeng@scsio.ac.cn.ORCID http://orcid.org/0000-0001-8914-5174
Jiayin GuoNMPA Key Laboratory for Research and Evaluation of Drug Metabolism, Guangdong Provincial Key Laboratory of New Drug Screening, Guangdong-Hong Kong-Macao Joint Laboratory for New Drug Screening, Southern Medical University Hospital of Integrated Traditional Chinese and Western Medicine, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China. g1227@smu.edu.cn.
Lan TangNMPA Key Laboratory for Research and Evaluation of Drug Metabolism, Guangdong Provincial Key Laboratory of New Drug Screening, Guangdong-Hong Kong-Macao Joint Laboratory for New Drug Screening, Southern Medical University Hospital of Integrated Traditional Chinese and Western Medicine, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China. tl405@smu.edu.cn.

Funding

National Natural Science Foundation of China 42376124National Natural Science Foundation of China 82274002
6 · The paper itself

Abstract

N-Hydroxyapiosporamide (N-hydap), a marine product derived from a sponge-associated fungus, has shown promising inhibitory effects on small cell lung cancer (SCLC). However, there is limited understanding of its metabolic pathways and characteristics. This study explored the in vitro metabolic profiles of N-hydap in human recombinant cytochrome P450s (CYPs) and UDP-glucuronosyltransferases (UGTs), as well as human/rat/mice microsomes, and also the pharmacokinetic properties by HPLC-MS/MS. Additionally, the cocktail probe method was used to investigate the potential to create drug-drug interactions (DDIs). N-Hydap was metabolically unstable in various microsomes after 1 h, with about 50% and 70% of it being eliminated by CYPs and UGTs, respectively. UGT1A3 was the main enzyme involved in glucuronidation (over 80%), making glucuronide the primary metabolite. Despite low bioavailability (0.024%), N-hydap exhibited a higher distribution in the lungs (26.26%), accounting for its efficacy against SCLC. Administering N-hydap to mice at normal doses via gavage did not result in significant toxicity. Furthermore, N-hydap was found to affect the catalytic activity of drug metabolic enzymes (DMEs), particularly increasing the activity of UGT1A3, suggesting potential for DDIs. Understanding the metabolic pathways and properties of N-hydap should improve our knowledge of its drug efficacy, toxicity, and potential for DDIs.

Indexed as

DDIsDMEsMetabolismN-HydapPharmacokineticsToxicity

Identifiers

PMID38771401
PMCPMC11109052

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