2. Academic Validation
  3. Cytotoxic diterpenes from roots of Crossopetalum gaumeri, a Celastraceae species from Yucatan Peninsula

Cytotoxic diterpenes from roots of Crossopetalum gaumeri, a Celastraceae species from Yucatan Peninsula

  • Bioorg Med Chem Lett. 2014 May 1;24(9):2105-9. doi: 10.1016/j.bmcl.2014.03.051.
Gumersindo Miron-Lopez 1,  Isabel L Bazzocchi 2,  Ignacio A Jimenez-Diaz 2,  Laila M Moujir 3,  Ramiro Quijano-Quiñones 1,  Leovigildo Quijano 4,  Gonzalo J Mena-Rejon 5
Affiliations

Affiliations

  • 1 Facultad de Química, Universidad Autónoma de Yucatán, C 41 No. 421, Col. Industrial, C.P. 97150 Mérida, Yucatán, Mexico.
  • 2 Instituto Universitario de Bio-Orgánica 'Antonio González', Universidad de La Laguna, Avda. Astrofísico Francisco Sánchez 2, 38206 Tenerife, Islas Canarias, Spain.
  • 3 Departamento de Microbiología y Biología Celular, Universidad de La Laguna, Avda. Astrofísico Francisco Sánchez 2, 38206 Tenerife, Islas Canarias, Spain.
  • 4 Instituto de Química, Universidad Nacional Autónoma de México, Circuito Exterior, Ciudad Universitaria, 04510 México, D.F., Mexico.
  • 5 Facultad de Química, Universidad Autónoma de Yucatán, C 41 No. 421, Col. Industrial, C.P. 97150 Mérida, Yucatán, Mexico. Electronic address: mrejon@uady.mx.
PMID: 24709561 DOI: 10.1016/j.bmcl.2014.03.051
Abstract

Four new diterpenes, crossogumerins A-D (1-4) along with six known ones (5-10) were isolated from the root bark of Crossopetalum gaumeri, an endemic medicinal plant from the Yucatan Peninsula. Their structures were elucidated on the basis of 1D and 2D NMR techniques, including HMQC, HMBC, and ROESY experiments. Compounds 1-5, 8-10 were evaluated for cytotoxicity against HeLa (carcinoma of the cervix) and Hep-2 (lung carcinoma) human tumor cells lines and against normal Vero cells (African green monkey kidney) in lag and log phase of growth. Podocarpane diterpenes, crossogumerin B (2) and nimbiol (10), exhibited the highest activity against HeLa cells (IC50 values of 3.1 and 8.1 μM, respectively), but also selectivity on Vero cells (SI 22.6 and 7.5, respectively). The preliminary SAR studies suggest that an epoxy moiety in ring B and a hydrogen bond-donor group strategically positioned in the diterpene core are important requirements for cytotoxicity and selectivity.

Keywords

Celastraceae; Crossopetalum; Cytotoxicity; Podocarpane; Yucatán.

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