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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
Synthesis of diosgenin analogues as potential anti-inflammatory agents
Journal of Steroid Biochemistry and Molecular Biology, Volume 143, Year 2014
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Description
We herein report the synthesis of diosgenin analogues from commercially available diosgenin as the starting material. The structures of newly synthesised compounds were confirmed by 1H NMR, 13C NMR and mass spectrometry. All analogues were evaluated for in-vitro anti-inflammatory profile against LPS-induced inflammation in primary peritoneal macrophages isolated from mice by quantification of pro-inflammatory (TNF-α, IL-6 and IL-1β) cytokines in cell culture supernatant using the ELISA technique followed by in-vitro cytotoxicity study. Among the synthesised analogues, analogue 15 [(E) 26-(3′,4′,5′- trimethoxybenzylidene)-furost-5en-3β-acetate)] showed significant anti-inflammatory activity by inhibiting LPS-induced pro-inflammatory cytokines in a dose-dependent manner without any cytotoxicity. Efficacy and safety of analogue 15 were further validated in an in-vivo system using LPS-induced sepsis model and acute oral toxicity in mice. Oral administration of analogue 15 inhibited the pro-inflammatory cytokines in serum, attenuated the liver and lung injury and reduced the mortality rate in sepsis mice. Acute oral toxicity study showed that analogue 15 is non-toxic at higher dose in BALB/c mice. Molecular docking study revealed the strong binding affinity of diosgenin analogues to the active site of the pro-inflammatory proteins. These findings suggested that analogue 15 may be a useful therapeutic candidate for the treatment of inflammatory diseases. © 2014 Elsevier Ltd.
Authors & Co-Authors
Singh, Monika P.
India, Lucknow
Central Institute of Medicinal and Aromatic Plants India
Hamid, Abdulmumeen A.
India, Lucknow
Central Institute of Medicinal and Aromatic Plants India
Nigeria, Ilorin
University of Ilorin
Maurya, Anil K.
India, Lucknow
Central Institute of Medicinal and Aromatic Plants India
Prakash, Om
India, Lucknow
Central Institute of Medicinal and Aromatic Plants India
Khan, Feroz
India, Lucknow
Central Institute of Medicinal and Aromatic Plants India
Kumar, Anant
India, Lucknow
Central Institute of Medicinal and Aromatic Plants India
Aiyelaagbe, Olapeju O.
Nigeria, Ibadan
University of Ibadan
Negi, Arvind Singh
India, Lucknow
Central Institute of Medicinal and Aromatic Plants India
Bawankule, Dnyaneshwar Umrao
India, Lucknow
Central Institute of Medicinal and Aromatic Plants India
Statistics
Citations: 45
Authors: 9
Affiliations: 3
Identifiers
Doi:
10.1016/j.jsbmb.2014.04.006
Research Areas
Environmental
Health System And Policy
Violence And Injury