Cytotoxic constituents from Hyptis Verticillata

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Abstract

A new cytotoxic (P-388 ED50 4 µg/ml) arylnaphthalene lignan has been isolated from the Mexican medicinal plant Hyptis verticillata (Lamiaceae) and characterized as 5-methoxydehydropodophyllotoxin [1]. Eight additional lignans were also obtained by bioactivitydirected fractionation using the brine shrimp lethality test. Of these, the dehydro-β-peltatin methyl ether 2 (P-388 ED501.8 µg/ml) is reported for the first time as a natural product isolate. The other bioactive compounds were identified as dehydropodophyllotoxin [3], deoxydehydropodophyllotoxin [4], (−)-yatein [5], 4′-demethyldeoxypodophyllotoxin [6], isodeoxypodophyllotoxin [7], deoxypicropodophyllin [8], and β-apopicropodophyllin [9]- Each of these compounds was evaluated against a panel of cell lines comprising a number of human cancer cell types [breast, colon, fibrosarcoma, lung, prostate, KB, and KB-VI (a multi-drug resistant cell line derived from KB)] and murine lymphocytic leukemia (P-388). Lignans 1–4 showed marginal cytotoxic activity against the human cell lines tested. In contrast, compounds 5–9 demonstrated a general nonspecific activity comparable to that of podophyllotoxin [12] (ED50 < 10−2 µg/ml). In addition, the antimitotic potential of these compounds was determined in the astrocytoma (ASK) assay. Finally, the plant was also shown to contain the fiavonoid sideritoflavone (KB ED501.6 µg/ml) and the known pentacyclic triterpenoids ursolic, maslinic, 2α-hydroxyursolic, and oleanolic acids. © 1993, American Chemical Society. All rights reserved.

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Novelo, M., Cruz, J. G., Hernández, L., Pereda-Miranda, R., Chai, H., Mar, W., & Pezzuto, J. M. (1993). Cytotoxic constituents from Hyptis Verticillata. Journal of Natural Products, 56(10), 1728–1736. https://doi.org/10.1021/np50100a011

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