Cytotoxic diterpenes from roots of Crossopetalum gaumeri,a Celastraceae species from Yucatan Peninsula |
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| Institution: | 1. Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, People''s Republic of China;2. State Key Laboratory of Phytochemistry and Plant Resourcese in West China, Kunming Institute of Botany, Chinese Academy of Science, Kunming 650204, People''s Republic of China;3. School of Pharmacy, Dali University, Dali 671003, People''s Republic of China;4. Central Hospital of Wuhan Affiliated to Tongji Medical College, Huazhong University of Science and Technologynd Technology, Wuhan 430000, People''s Republic of China |
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| 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. |
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| Keywords: | Podocarpane Yucatán Cytotoxicity Celastraceae |
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