A Nitrobenzoyl Sesquiterpenoid Insulicolide A Prevents Osteoclast Formation Suppressing c-Fos-NFATc1 Signaling Pathway.

Front Pharmacol

Laboratory of Anti-inflammatory and Immunomodulatory Pharmacology, Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, China.

Published: January 2022

It is a viable strategy to inhibit osteoclast differentiation for the treatment of osteolytic diseases such as osteoporosis, rheumatoid arthritis and tumor bone metastases. Here we assessed the effects of insulicolide A, a natural nitrobenzoyl sesquiterpenoid derived from marine fungus, on receptor activator of nuclear factor-κB ligand (RANKL)-stimulated osteoclastogenesis and its protective effects on LPS-induced osteolysis mice model . The results demonstrated that insulicolide A inhibited osteoclastogenesis from 1 μM . Insulicolide A could prevent c-Fos and nuclear factor of activated T-cell cytoplasmic 1 (NFATc1) nuclear translocation and attenuate the expression levels of osteoclast-related genes and DC-STAMP during RANKL-stimulated osteoclastogenesis but have no effects on NF-κB and MAPKs. Insulicolide A can also protect the mice from LPS-induced osteolysis. Our research provides the first evidence that insulicolide A may inhibit osteoclastogenesis both and , and indicates that it may have potential for the treatment of osteoclast-related diseases.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8801808PMC
http://dx.doi.org/10.3389/fphar.2021.753240DOI Listing

Publication Analysis

Top Keywords

nitrobenzoyl sesquiterpenoid
8
rankl-stimulated osteoclastogenesis
8
lps-induced osteolysis
8
insulicolide
6
sesquiterpenoid insulicolide
4
insulicolide prevents
4
prevents osteoclast
4
osteoclast formation
4
formation suppressing
4
suppressing c-fos-nfatc1
4

Similar Publications

Marine fungi sp. is an important source of natural active lead compounds with biological and chemical diversity, of which sesquiterpenoids are an extremely important class of bioactive secondary metabolites. In this paper, we review the sources, chemical structures, bioactivity, biosynthesis, and druggability evaluation of sesquiterpenoids discovered from marine fungi sp.

View Article and Find Full Text PDF

The Secondary Metabolites and Biosynthetic Diversity From .

Front Chem

August 2022

Key Laboratory of Agro-Products Quality and Safety Control in Storage and Transport Process, Ministry of Agriculture and Rural Affairs, Institute of Food Science and Technology, Chinese Academy of Agricultural Sciences, Beijing, China.

, generally known as a food spoilage fungus, is the representative species in section . strains are widely distributed in nature, and usually isolated from cereal, coffee, fruit, and beverage. Increasing cases suggest acts as human and animal pathogens due to producing the mycotoxins.

View Article and Find Full Text PDF

Cytotoxic Nitrobenzoyl Sesquiterpenoids from an Antarctica Sponge-Derived .

J Nat Prod

April 2022

Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, People's Republic of China.

Pancreatic ductal adenocarcinoma (PDAC) is one of the most aggressive neoplastic diseases of the pancreas with fatal proliferation and metastasis and no medicine available for treatment. From an Antarctica sponge-derived fungus, HDN151418, four new nitrobenzoyl sesquiterpenoids, namely, insulicolides D-G (-), were isolated. Compounds and exhibited selective inhibition against human PDAC cell lines.

View Article and Find Full Text PDF

A Nitrobenzoyl Sesquiterpenoid Insulicolide A Prevents Osteoclast Formation Suppressing c-Fos-NFATc1 Signaling Pathway.

Front Pharmacol

January 2022

Laboratory of Anti-inflammatory and Immunomodulatory Pharmacology, Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, China.

It is a viable strategy to inhibit osteoclast differentiation for the treatment of osteolytic diseases such as osteoporosis, rheumatoid arthritis and tumor bone metastases. Here we assessed the effects of insulicolide A, a natural nitrobenzoyl sesquiterpenoid derived from marine fungus, on receptor activator of nuclear factor-κB ligand (RANKL)-stimulated osteoclastogenesis and its protective effects on LPS-induced osteolysis mice model . The results demonstrated that insulicolide A inhibited osteoclastogenesis from 1 μM .

View Article and Find Full Text PDF

Background And Purpose: Osteoclasts are unique cells to absorb bone. Targeting osteoclast differentiation is a therapeutic strategy for osteolytic diseases. Natural marine products have already become important sources of new drugs.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!