Estrone-3-Glucuronide (E1G) ELISA Kit

Development of hybrid drug candidates is well known strategy for designing antitumor agents. Herein, a novel class of nitric oxide donating cucurbitacin inspired estrone analogs (NO-CIEAs) were designed and synthesized as multitarget agents. Synthesized analogs were initially evaluated for their anti-hepatocellular carcinoma activities. Among the tested analogs, NO-CIEAs 17 and 20a exhibited more potent activity against HepG2 cells (IC50 = 4.69 and 12.5 mu M, respectively) than the reference drug Erlotinib (IC50 = 25 mu M). Interestingly, NO-CIEA 17 exerted also a high potent activity against Erlotinib-resistant HepG2 cell line (HepG2-R) (IC50 = 8.21 mu M) giving insight about its importance in drug resistance therapy. Intracellular measurements of NO revealed that NO-CIEAs 17 and 20a showed a significant increase in NO production in tumor cells after 1 h of incubation comparable to the reference prodrug JS-K. Flow cytometric analysis showed that both NO-CIEAs 17 and 20a mainly arrested the HepG2 cells in the G0/G1 phase. Also, In-Cell Based ELISA screening showed that NO-CIEA 17 resulted in a potential inhibitory activity towards the EGFR and MAPK (25% and 29% inhibition compared to untreated control cells, respectively). This data suggests the binding ability of NO-CIEA 17 to the EGFR and ERK to be well correlated along with the docking and cellular studies. Also, treatment of HepG2-R cells with NO-CIEA 17 showed a potential reduction of MRP2 expression in a dose dependent manner providing a significant impact on the chemotherapeutic resistance. Overall, the current study provides a potential new approach for the discovery of a novel antitumor agent against HCC.

This paper explores the applicability of unmodified and chemically modified activated carbon cloths (ACCs) for the removal of estrone, 17 beta-estradiol, and 17 alpha-ethinylestradiol from water. In order to examine the influence of surface properties on hormone adsorption, chemical modification of ACCs with HNO3, HCl, or KOH was employed. Applied treatments increased the specific surface area and changed the content of oxygen functional groups. Increased content of acidic surface oxygen functionalities enhanced adsorption efficiency up to 30 % and had a more dominant influence on adsorption capacity than specific surface area. Adsorption of estrone, 17 beta-estradiol, and 17 alpha-ethinylestradiol followed pseudo-second-order kinetic model, while the equilibrium adsorption data fitted well with the Freundlich isotherm model. Calculated mean sorption energy values of 1.4475, 1.3387, and 1.0541 kJ/mol, for E1, E2, and EE2 respectively, indicated that removal of selected hormones was dominated by physisorption mechanism. Obtained Langmuir adsorption capacities, 12.34, 12.66, and 11.11 mg/g for estrone, 17 beta-estradiol, and 17 alpha-ethinylestradiol, respectively, as well as convenience of manipulation, recommend activated carbon cloth modified with HNO3 as an efficient adsorbent for removing estrogen hormones from the water.