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Antidiabetic and cy...
Antidiabetic and cytotoxic polyhydroxylated oleanane and ursane type triterpenoids from Salvia grossheimii
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Zare, Somayeh (författare)
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Mirkhani, Hossein (författare)
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Firuzi, Omidreza (författare)
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Moheimanian, Niloofar (författare)
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Asadollahi, Mojtaba (författare)
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Pirhadi, Somayeh (författare)
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Chandran, Jima N. (författare)
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Schneider, Bernd (författare)
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Jassbi, Amir Reza (författare)
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- Elsevier BV, 2020
- 2020
- Engelska.
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Ingår i: Bioorganic chemistry. - : Elsevier BV. - 0045-2068. ; 104
- Relaterad länk:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
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- Two polyhydroxylated oleanane and seven ursane triterpenoids were isolated from aerial parts of Salvia grossheimii. The chemical structures of the undescribed triterpenoids (1–6) were characterized using 1 and 2 D NMR and ESI-MS spectral data as; 2α, 3β, 11α –trihydroxy-olean-12- ene (1), 2α, 3β, 11α-trihydroxy-olean-18-ene (2), 2α- acetoxy-urs-12-ene-3β, 11α, 20β-triol (3), 3-keto-urs-12-ene-1β, 11α, 20β -triol (4), 2α, 3β-diacetoxy-urs-12-ene-1β, 11α, 20β -triol (5), and 3β-acetoxy-urs-12-ene-1β, 11α, 20β –triol (6). All compounds were evaluated for the in vitro α-glucosidase inhibitory and cytotoxic activities against MCF-7 human cancer cell line. Compounds 1, 2, 4, and 6 showed in vitro α-glucosidase inhibitory activity with IC50 = 43.6–198.4 µM, which were more potent than the antidiabetic medicine, acarbose. The remaining compounds; 3, and 7–9 showed potent cytotoxic activity (IC50 = 6.2–31.9 µM) against the cancerous cell line, while the potent α-glucosidase inhibitors were inactive. Molecular docking analysis and kinetic studies were applied to investigate the structure activity relationships and mechanisms of the human and Saccharomyces cerevisiae α-glucosidase inhibitory of the purified compounds. Comparing the high cytotoxicity and α-glucosidase inhibitory of the oleanane and ursane type triterpenoids suggest them as potential lead compounds for further research in anticancer and antidiabetic research.
Ämnesord
- NATURVETENSKAP -- Biologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences (hsv//eng)
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