The widespread accumulation of androgenic steroid endocrine disruptors in water and food has garnered increasing attention due to their significant risks to ecosystems and human health. These steroids, which cannot be completely eliminated, highlight the urgent need for advanced detection technologies. In this study, we present a novel emulsion-induced interface-anisotropic assembly strategy to synthesize bowl-like mesoporous polydopamine (PDA) particles, which exhibit high sensitivity in surface-enhanced Raman scattering (SERS) detection. In-situ reduction of chloroauric acid leads to the formation of Au nanoparticles (NPs) on the PDA surface, where synergistic Au-N interactions enhance the SERS performance. The distinctive bowl-like structure generates abundant "hot spots" on both sides, resulting in exceptional sensitivity. The low relative standard deviation (RSD) values (<11.7 %) across different PDA@Au NPs, along with real sample analyses (1.9-4.0 %), confirm the high reproducibility and uniformity of the SERS substrates, all achieved without the use of additional reducing agents. This cost-effective and straightforward method eliminates the need for complex surface treatments, making it particularly suitable for real-time detection of anabolic steroids across various matrices. These findings underscore the potential of bowl-like PDA materials for broader applications in clinical diagnostics, environmental monitoring, and sports doping control.

01 Mar 2025·Bioorganic Chemistry

Novel steroidal oximes as antiproliferative agents: Design, synthesis and biological activity evaluation

Article

Author: Botelho, Maria F ; Tavares-da-Silva, Elisiário J ; Alves, Raquel ; Abrantes, Ana M ; Gomes, Ana R ; Gonçalves, Ana C ; Roleira, Fernanda M F ; Pires, Ana S

Oximes have been the subject of extensive research given their interesting anticancer activity. Steroids are also important scaffolds in drug discovery, not only due to their ability to penetrate cell membranes and bind to the nuclear and membrane receptors but also due to their suitability for structural modifications, allowing their use as cytotoxic and cytostatic anticancer agents. Combining the oxime group with the steroidal skeleton can be a suitable strategy to create novel anticancer agents. In this study, we designed and synthesised several novel steroidal oximes (OX1, OX2, OX3, OX3.1, OX4, EP2OX, FormOX and ExeOX) and evaluated their anticancer activity in three of the most incident and deadliest types of cancer, prostate (PC3), lung (H1299) and triple-negative breast (HCC1806) cancers. Selectivity using a normal human cell line, MRC-5, and hemocompatibility were also assessed. EP2OX was the most active compound in the studied cancer cell lines (IC₅₀ values ranging from 1.13 to 3.70 µM) followed by OX1 (IC₅₀ values ranging from 18.69 to 29.95 µM). Further studies with EP2OX and OX1 showed that the first induced DNA damage by double-strand breaks triggered by ROS production, leading to apoptosis/necrosis (depending on the concentration), while the second induced cell death by apoptosis regardless of the concentration. Moreover, both compounds showed some selectivity towards cancer cells and proved to be non-haemolytic. Our results reinforce the importance of steroidal oximes in the oncology field, namely our novel compound EP2OX which might be the starting point for a potential drug candidate for treating these types of cancer.

01 Feb 2025·Drug Testing and Analysis

Development of 3β,4α‐dihydroxy‐5α‐androstan‐17‐one standard solution for doping analyses

Article

Author: Shimizu, Yoshitaka ; Ihara, Toshihide ; Numata, Masahiko ; Itoh, Nobuyasu ; Kuroe, Miho ; Saito, Naoki ; Yamazaki, Taichi

AbstractDoping analyses are essential for sporting events because some athletes might use prohibited substances to win games. To obtain reliable results from doping analyses, it is important to use both reliable standard solutions and validated analytical methods at accredited laboratories. Among the focused compounds related to prohibited substances listed by the World Anti‐Doping Agency, we developed a certified reference material (CRM) for 3β,4α‐dihydroxy‐5α‐androstan‐17‐one (DHAS), a metabolite of formestane that is used to conceal prohibited anabolic steroids, in methanol solution (NMIJ CRM 6212‐a). To develop a CRM traceable to the International System of Units (SI), we newly applied different analytical methods with an SI‐traceable internal standard for quantitative NMR (qNMR) instead of mass balance approach because this CRM solution was required to develop rapidly using a limited amount of high‐purity DHAS. One method was gravimetric blending using the purity of DHAS powder evaluated by both qNMR and a combination of qNMR and high‐performance liquid chromatography (HPLC), and the other was direct quantification of the DHAS mass fraction in the candidate solution CRM by both qNMR and qNMR/HPLC. Because the values obtained by gravimetric blending and direct quantification of the mass fraction were comparable, the arithmetic mean was applied to obtain the certified value. Considering homogeneity and stability according to ISO Guide 35: 2017, the certified values with expanded uncertainties (coverage factor k = 2, approximate 95% confidence interval) were (135.2 ± 9.5) μg/g for the mass fraction and (107.0 ± 7.5) μg/ml for the mass concentration.

100 Deals associated with Formestane

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KEGG	Wiki	ATC	Drug Bank
D07260	Formestane	L02BG02	DB08905

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Indication	Country/Location	Organization	Date
Neoplasms	China	Novartis Pharma Schweiz AG	20 Jul 2001

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