[Reductive effect of the sesquiterpenic lactone "Helenalin " and its metallic derivatives in the formation of the estradiol receptor complex in breast tumor tissue].
Chemotherapy for systemic therapy in breast cancer has been widely used, and has been supported by many varied compounds with different origins and different compositions. Nevertheless, all of them produce several side adverse effects which must be taken into account. For this reason we must study new possibilities in which the administered drug acts selectively on the tumour cell without injuring healthy tissue. For studying its effect, a gamma lactone called "Helenaline" and its metalic derivates He-Co, He-Hg and He-Cu were studied, which chemical composition allows them to react with -SH residues present in the tumour cell receptors, which when interspaced by a previous reaction, could modify its structural composition and finally its affinity by the hormone. The inhibition effect for formation of estradiol-receptor complex in breast tumour tissue using Helenaline 12 n M and 126 n M was studied, obtaining 14% and 56% inhibition effect respectively. When He-Co, He-Hg and He-Cu effect was studied, this effect was raised obtaining 11%, 10.5% and 60% with 12 nM and 44.5%, 74.4% and 86% with 126 nM respectively.
Salazar Esquivel
E L
EL
Unidad de Investigación Médica en Biología de la Reproducción, Hospital de Gineco Obstetricia Luis Castelazo Ayala, IMSS, México, D.F.
Tellez
M C
MC
Calzada
L
L
D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000378:metabolism*; D018270:Carcinoma, Ductal, Breast / Q000378:metabolism*; D006801:Humans; D009942:Organometallic Compounds / Q000494:pharmacology*; D011959:Receptors, Estradiol / Q000187:drug effects*; D012717:Sesquiterpenes / Q000494:pharmacology*; D045789:Sesquiterpenes, Guaiane; D014407:Tumor Cells, Cultured
D000972:Antineoplastic Agents, Phytogenic; D009942:Organometallic Compounds; D011959:Receptors, Estradiol; D012717:Sesquiterpenes; D045789:Sesquiterpenes, Guaiane; C001329:helenalin
Efecto reductor de la lactona sesquiterpénica "Helenalina" y sus derivados metálicos en la formación del complejo estradiol receptor en tejido tumoral mamario.