Toxicity, Pharmacokinetics, and Gut Microbiome of Oral Administration of Sesterterpene MHO7 Derived from a Marine Fungus.


Journal

Marine drugs
ISSN: 1660-3397
Titre abrégé: Mar Drugs
Pays: Switzerland
ID NLM: 101213729

Informations de publication

Date de publication:
26 Nov 2019
Historique:
received: 10 10 2019
revised: 25 11 2019
accepted: 25 11 2019
entrez: 30 11 2019
pubmed: 30 11 2019
medline: 28 5 2020
Statut: epublish

Résumé

Sesterterpene MHO7 derived from mangrove fungus is a novel estrogen receptor degrader for the treatment of breast cancer. To explore its safety and pharmacokinetics in vivo, Log P/D values, stability in simulated gastric/intestinal (SGF/SIF), toxicity, and pharmacokinetics studies were carried mainly by liquid chromatography technique coupled with tandem mass spectrometry (LC-MS/MS) method in mice, and the effect of MHO7 on mice gut microbiota at different time points was revealed by 16S rRNA sequencing. Log P/D values ranged 0.93-2.48, and the compound in SGF and SIF is stable under the concentration of 5 mM·L

Identifiants

pubmed: 31779201
pii: md17120667
doi: 10.3390/md17120667
pmc: PMC6950057
pii:
doi:

Substances chimiques

Sesterterpenes 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Subventions

Organisme : the National Key R&D Program of China
ID : No. 2018YFC0311005
Organisme : National Natural Science Foundation of China
ID : Grant No. 81741153

Déclaration de conflit d'intérêts

The authors declare no conflict of interest.

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Auteurs

Wei Tian (W)

Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Ministry of Education, and Wuhan University School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China.

Liang Yang (L)

Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Ministry of Education, and Wuhan University School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China.

Di Wu (D)

Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Ministry of Education, and Wuhan University School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China.

Zixin Deng (Z)

Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Ministry of Education, and Wuhan University School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China.

Kui Hong (K)

Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Ministry of Education, and Wuhan University School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China.

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Classifications MeSH