Abstract
In this study, we first characterized the effect of natural brassinosteroids, 24-epibrassinolide (EBl) and 28-homocastasterone (HCS), and synthetic analogs, (22S,23S)-24-epibrassinolide and (22S,23S)-28-homocastastone, on the growth of the cancer cell line Hep G2 (hepatocellular carcinoma), as well as on the catalytic activity of cytochrome P450, which participates in the metabolism of most procarcinogens. All four compounds at high concentrations suppressed the proliferation of the test cell line. It is also interesting that at low concentrations, 24-EBl, (22S,23S)-24-EBl and (22S,23S)28-HCS activated significantly the Hep G2 cell growth. All studied brassinosteroids, except for 28-HCS, inhibited the activity of CYP1A1 and CYP1B1. The effect depended on the structure of the side chain and was more pronounced in the case of the SS orientation of the hydroxyl groups at the positions C22 and C23 ((22S,23S)-28-homocastasterone). The results of this work suggest that the studied brassinosteroids (especially (22S,23S)-28-homocastasterone) can be used to create effective drugs for tumor prevention and treatment.
Highlights
In this study, we first characterized the effect of natural brassinosteroids, 24-epibrassinolide (EBl) and 28-homocastasterone (HCS), and synthetic analogs, (22S,23S)-24-epibrassinolide and (22S,23S)-28-homocastastone, on the growth of the cancer cell line Hep G2, as well as on the catalytic activity of cytochrome P450, which participates in the metabolism of most procarcinogens
The results of this work suggest that the studied brassinosteroids (especially (22S,23S)-28-homocastasterone) can be used to create effective drugs for tumor prevention and treatment
В этом плане исследованные БС (в наибольшей степени (22S,23S)-28-ГКС (9)) могут стать основой для создания более эффективных препаратов для профилактики и лечения опухолевых заболеваний
Summary
ДЭ2 Суммарный продукт реакции B[a]P-7,8-диол (3) (субстрат) ДЭ2/продукт Продукт/субстрат. В [12; 13] на клетках линии MCF -7 б ы л а п о к а з а н а и н г и б и р у ю щ а я а к т и в н о с т ь в е щ е с т в р а с т и т ел ьн о го п р о и сх о ж д е н и я – ф л а воноидов, в частности кверцетина, кемпферола, мирицитина и апигенина в отношении CYP1A1 и CYP1B1, метаболизирующих Б[а]П (1). Все исследуемые в данной работе БС (за исключением 28-ГКС (8)) также ингибировали активность CYP1A1 и CYP1B1. В этом плане исследованные БС (в наибольшей степени (22S,23S)-28-ГКС (9)) могут стать основой для создания более эффективных препаратов для профилактики и лечения опухолевых заболеваний
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