Abstract:
:β-Carbolines have been assessed for osteoclastogenesis. However, their effect on osteoblasts during estrogen deficiency is still unclear. Here, a series of novel piperazine and tetrazole tag β-carbolines have been synthesized and examined for osteoblast differentiation in vitro. In vitro data suggest that compound 8g is the most promising osteoblast differentiating agent that was evaluated for in vivo studies. Compound 8g promoted osteoblast mineralization, stimulated Runx2, BMP-2 and OCN expression levels, increased BrdU incorporation and inhibited generation of free radicals as well as nitric oxide. Since a piperazine group is involved in bone repair activity and β-carboline in IκB kinase (IKK) inhibition, compound 8g inhibited tumor necrosis factor α (TNFα) directed IκBα phosphorylation, preventing nuclear translocation of NF-κB thereby alleviating osteoblast apoptosis. In vivo studies show that compound 8g was able to restore estrogen deficiency-induced bone loss in ovariectomized rats without any toxicity, thus signifying its potential in bone-protection chemotherapy under postmenopausal conditions.
journal_name
Medchemcommjournal_title
MedChemCommauthors
Karvande A,Khan S,Khan I,Singh D,Khedgikar V,Kushwaha P,Ahmad N,Kothari P,Dhasmana A,Kant R,Trivedi R,Chauhan PMSdoi
10.1039/c8md00109jsubject
Has Abstractpub_date
2018-06-12 00:00:00pages
1213-1225issue
7eissn
2040-2503issn
2040-2511pii
c8md00109jjournal_volume
9pub_type
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