Combined Action of Doxorubicin and Gestagens on Doxorubicin-Sensitive and Doxorubicin-Resistant MCF-7 Cells

Сергеев, П. В.; Semeikin, A. V.; Федотчева, Т. А.; Samoilikov, R V; Камерницкий, А. В.; Левина, И. С.; Rzheznikov, V. M.; Grinenko, G. S.; Korystov, Yu. N.; Ermakova, N V; Shaposhnikova, V. V.; Шимановский, Н. Л.

doi:10.1023/b:bebm.0000017093.04390.a3

Cited by 4 publications

(3 citation statements)

References 6 publications

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“…It has been demonstrated in our studies and those of foreign researchers that certain steroidal compounds, in particular, gestagens, can increase the cytostatic activity of doxorubicin, i.e., have a chemically sensitized activity on tumor cells [11,12]. In order to find chemically sensitizing activity of the investigated compounds, we studied their effect on the viability of MCF-7 tumor cells in combination with doxorubicin.…”

Section: Effect Of Hormonal Compounds In Combination With Doxorubicinmentioning

confidence: 92%

Comparative analysis of the effect of gestagens, antiestrogencytostatics, and androstenes on the viability of tumor and normal cells

et al. 2007

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The hormonal compound with the highest cytostatic activity against MCF-7 tumor cells (human breast cancer, BC) and the lowest activity against normal cells (rat skin fibroblasts) was sought among gestagens, androstenes, and antiestrogencytostatics. It was found that antiestrogencytostatics and androstenes had the highest cytostatic activity against tumor cells whereas gestagens and antiestrogencytostatics were least active against fibroblasts. Studies of the activity of the hormonal compounds in combination with doxorubicin on the viability of MCF-7 and rat skin fibroblasts found that all investigated compounds with the exception of dehydroepiandrosterone (DHEA) intensify the cytostatic activity of doxorubicin against tumor cells, the greatest effect seen for antiestrogencytostatics. A chemoprotective effect of androstenes on normal cells was noted.Treatment regimes for cancerous diseases have not yet been standarized despite the efforts of researchers and clinicians. This is apparently due to the fact that each tumor has its own receptor array and individual genetic profile and responds differently to one or another type of therapy. Agonists or antagonists of various steroidal receptors have turned out in several instances to be highly effective in treating hormone -dependent neoplasms. Depending on the age of the patient (reproductive or menopausal), various combinations of antiestrogens, progestins, and even androgens may be used in hormone therapy of human breast cancer (BC) [1]. Herein we report the screening of new synthetic gestagens, antiestrogencytostatics, and androstenes and the comparison of them with existing clinical drugs for tumor model and normal cells. The existing clinical drugs have several side effects and drawbacks (multidrug resistance and glucocorticoid, mineralocorticoid, and androgen side effects of hormone -therapy). Therefore, there is a continuous search for more effective and safer new compounds. Several new steroidal compounds have been synthesized. We studied the following of these: 1) 17a-Acetoxy-3b-butyloxy-6-methylpregna-4,6-dien-20-one (ABMP), a gestagen that does not have a D 4 -3-ketone and has a structure similar to progesterone but, in contrast with it, can be readily absorbed orally [2]. The reference drugs were progesterone (P) and medroxyprogesterone acetate (MPA).2) Po715 and Po716, antiestrogencytostatics that are estrogens having transformed C rings with substituents containing a bis-b-chloroethylamine moiety (Fig. 1) [3,4].We used 11a-derivatives of ethynylestradiol with the bis-b-chloroethylamine moiety bonded to the 3 -position.3) Dehydroepiandrosterone nitrate (DHEAN), androstendiol nitrate (AEDN), and androstendiol dinitrate (AEDDN), which are nitro derivatives of the endogenous androstenes dehydroepiandrosterone and androstendiol, respectively. The reference drugs were androstendiol (AED) and DHEA [5].

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Section: Effect Of Hormonal Compounds In Combination With Doxorubicinmentioning

confidence: 92%

Comparative analysis of the effect of gestagens, antiestrogencytostatics, and androstenes on the viability of tumor and normal cells

et al. 2007

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“…The animals were randomly distributed between seven groups (each containing 6 -10 rats), which received oil suspensions of various drugs per os over a period of eight days in the following daily doses: (1, 2) ABMP, 0.01 and 0.025 mg/kg; (3,4) levonorgestrel, 0.01 and 0.025 mg/kg; (5) MPA, 0.025 mg/kg; (6) AMP, 0.025 mg/kg; animals in the seventh (control) group received pure plant oil. Then, the animals were killed by decapitation under light ether narcosis, and the progesterone concentration in the blood serum was determined using the corresponding ELISA test kit (DSLabs, USA).…”

Section: Methodsmentioning

confidence: 99%

“…Previously, ABMP has been shown to have good prospects as an antitumor drug and an agent enhancing the antitumor action of cytostatics [4].…”

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confidence: 99%

Investigation of the Gestagen Activity of 17α-acetoxy-3β-butanoyloxy-6-methylpregna-4,6-dien-20-one

Сергеев¹,

Rzheznikov

Korkhov³

et al. 2005

Pharm Chem J

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The gestagen activity of a new synthetic progesterone derivative, 17a-acetoxy-3b-butanoiloxy-6-methylpregna-4,6-dien-20-one (ABMP) has been studied in rabbits (Clauberg -McPhail test) and in rats (test for the ABMP influence on the progesterone level in blood and on the endometrium morphology). The gestagen activity of ABMP is more pronounced than that of reference drugs (progesterone, levonorgestrel, acetomepregenol). ABMP transforms the endometrium of experimental animals from proliferative to secretory phase and reduces mitotic activity of endometrium in rats. ABMP reduces progesterone level in the rat blood to a lower degree than do the reference drugs. ABMP exhibits no anabolic and androgenic activity in the Hershberger test in rats. 3580091-150X/05/3907-0358

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Chemo-directed specific targeting of nanoparticle-doxorubicin complexes to tumor in animal model

Sreeja¹,

Nair²

2016

Journal of Drug Delivery Science and Technology

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Combined Action of Doxorubicin and Gestagens on Doxorubicin-Sensitive and Doxorubicin-Resistant MCF-7 Cells

Cited by 4 publications

References 6 publications

Comparative analysis of the effect of gestagens, antiestrogencytostatics, and androstenes on the viability of tumor and normal cells

Comparative analysis of the effect of gestagens, antiestrogencytostatics, and androstenes on the viability of tumor and normal cells

Investigation of the Gestagen Activity of 17α-acetoxy-3β-butanoyloxy-6-methylpregna-4,6-dien-20-one

Chemo-directed specific targeting of nanoparticle-doxorubicin complexes to tumor in animal model

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