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Enhancement of antiproliferative activity by molecular simplification of catalpol |
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| Authors: | Celina García Leticia G León Carlos R Pungitore Carla Ríos-Luci Antonio H Daranas Juan C Montero Atanasio Pandiella Carlos E Tonn Víctor S Martín José M Padrón |
| Institution: | 1. Instituto Universitario de Bio-Orgánica ‘Antonio González’ (IUBO-AG), Universidad de La Laguna, C/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain;2. BioLab, Instituto Canario de Investigación del Cáncer (ICIC), C/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain;3. INTEQUI-CONICET, Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis, Chacabuco y Pedernera-5700-San Luis, Argentina;4. Departamento de Ingeniería Química y Tecnología Farmacéutica, Universidad de La Laguna, Avda. Astrofísico Francisco Sánchez s/n, 38206 La Laguna, Spain;5. Centro de Investigación del Cáncer, IBMCC/CSIC-Universidad de Salamanca, Campus Miguel de Unamuno. 37007 Salamanca, Spain |
| Abstract: | Two iridoid scaffolds were synthesized enantioselectively using as key step an l-proline-catalyzed α-formyl oxidation. The in vitro antiproliferative activities were evaluated against a representative panel of human solid tumor cell lines. Both iridoids induced considerably growth inhibition in the range 0.38–1.86 μM. Cell cycle studies for these compounds showed the induction of cell cycle arrest at the G1 phase. This result was consistent with a decrease in the expression of cyclin D1. Damaged cells underwent apoptosis as indicated by specific Annexin V staining. |
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