Steroids[JOURNAL]
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200 papers
In silico analysis of Moringaceae derived potential drug-like compounds against Newcastle disease virus.
Mustafa MH, Rehman FU, Ali M … +9 more , Javed M, Ahmad N, Shafique T, Zidan A, Bahadur A, Iqbal S, Mahmood S, Farouk AE, Jafri I
Steroids · 2025 Jul · PMID 40349813 · Publisher ↗
Newcastle disease virus (NDV) classified in the Avian avulavirus 1 [genus Orthoavulavirus, subfamily Avulavirinae, family Paramyxoviridae] constitutes a serious financial risk to the global poultry market. Available vacc...
Newcastle disease virus (NDV) classified in the Avian avulavirus 1 [genus Orthoavulavirus, subfamily Avulavirinae, family Paramyxoviridae] constitutes a serious financial risk to the global poultry market. Available vaccines do not show good results in catering to the virus. Currently there is no FDA-approved drug to treat the disease. Nucleoprotein (NP) is a structural protein playing that constitutes a serious financial risk to the global poultry market.a valuable role in the virus replication process and encapsidation. This study is an effort to screen phytochemicals, from the plant family Moringaceae, as potential inhibitors of the N protein. ADMET (adsorption, distribution, metabolism, excretion and toxicity) analysis was performed to screen potential phytochemicals with drug likeliness. Molecular Docking was performed for the binding affinities. Gas Chromatography-Mass Spectrometry (GC-MS) and Density Function Theory (DFT) were performed to evaluate the phytochemicals bioavailability and reactivity, respectively. The stability of protein-ligand complexes was examined by 50 ns MD simulations and MM/PBSA values were calculated. Out of 128 phytochemicals, 22 phytochemicals were selected following ADMET screening. Based on the binding energies and the number of H bonding the following 10 phytochemicals were suggested as potential inhibitors to N protein of NDV - cis-11,14-eicosadienoic acid methyl ester, aurantiamide acetate, α-tocopherol, 4,8,12,16-tetramethylheptadecan-4-olide, 3,7,11,15-tetramethyl-2-hexadecen-1-ol, β-amyrin, β-sitosterol-3-O-β-d-galactopyranoside, α-amyrin, pterygospermin and sitogluside. Furthermore, DFT results showed that the 4 pytochemicals - Cis-11,14-eicosadienoic acid methyl ester, aurantiamide acetate, α-tocopherol, and 3,7,11,15-tetramethyl-2-hexadecen-1-ol were most reactive and thus could be used as potential inhibitors of NDV N protein. Further studies are required to validate the selected four phytochemicals as drug candidates against NDV.
Palladium-catalyzed cross-coupling reactions of estrone.
Langer P
Steroids · 2025 Jul · PMID 40340002 · Publisher ↗
Palladium catalyzed cross-coupling reactions of estrone allow for the synthesis of a variety of substituted steroids which are not readily available by other methods. Products include various alkynylated and arylated est...
Palladium catalyzed cross-coupling reactions of estrone allow for the synthesis of a variety of substituted steroids which are not readily available by other methods. Products include various alkynylated and arylated estrones and 13α-estrones, 16-arylmethylidene-3-O-methylestrones and 16-alkynylmethylidene-3-O-methylestrones. Reactions usually proceed with excellent chemo- and regioselectivity and exhibit a broad functional group tolerance. In several cases, the estrone derivatives prepared proved to be active and selective inhibitors of alkaline phosphatases or exhibited considerable antiproliferative activities.
Steroid sulfatase and the transporter of sulfated steroids are upregulated in granulose cells from women of POSEIDON group 4 in controlled ovarian hyperstimulation for in vitro fertilization cycles.
Sequeira K, Henríquez S, Kohen P … +5 more , Fuentes A, Tapia-Pizarro A, Céspedes P, Godoy A, Devoto L
Steroids · 2025 Jul · PMID 40318834 · Publisher ↗
PURPOSE: The reduced circulating levels of dehydroepiandrosterone sulphate (DHEA-S) are associated with women with poor ovarian response, > 35 years old and low ovarian reserve (POSEIDON group 4, PG4) in cycles of contro...
PURPOSE: The reduced circulating levels of dehydroepiandrosterone sulphate (DHEA-S) are associated with women with poor ovarian response, > 35 years old and low ovarian reserve (POSEIDON group 4, PG4) in cycles of controlled ovarian hyperstimulation. In the ovary, the uptake of DHEA-S is facilitated by the transmembrane organic anion-transporting polypeptide, OATP2B1, whereas in the cytoplasm, the hydrolysis of the inactive precursor DHEA-S into the biologically active steroid DHEA is catalyzed by the steroid sulfatase enzyme (STS). The objective of the present study was to evaluate DHEA and DHEA-S in serum and follicular fluid as well as the expression levels for STS and OATP2B1 in granulosa cells from women in PG4 compared to a control group (control) of age matched women with normal ovarian reserve and response to controlled ovarian hyperstimulation. METHODS: Prospective study which included 23 women who underwent in vitro fertilization. We compared women in PG4 (n = 13) with a control (n = 8). Transcript levels and the cellular distribution of STS and OATP2B1 transporter were determined by qPCR and immunofluorescence respectively in granulosa cells collected at the time of oocyte pick-up. Gene expression was analyzed according to age, circulating AMH, antral follicle count (AFC) along with DHEA-S and DHEA in serum and follicular fluid. RESULTS: Serum and follicular fluid analysis showed that DHEA-S was significantly decreased in PG4 compared to control, whereas no differences in DHEA concentrations were observed. Women in PG4 had significantly higher expression of STS and OATP2B1 mRNA (n = 13, p < 0.05) compared with those of the control. CONCLUSION: Our results suggest that up-regulation of STS and OATP2B1 in granulosa cells from women in PG4 could be a compensatory mechanism to overcome the decreased circulating levels of DHEA-S possibly required as substrate for intraovarian production of DHEA.
Effect of dexamethasone on biological properties and metabolic adaptations of normal prostate epithelial cells under mild serum conditions.
Broszkiewicz W, Beda J, Domińska K
Steroids · 2025 Jul · PMID 40316041 · Publisher ↗
Limiting serum concentration in culture medium constitutes an environmental stress that disrupts cellular homeostasis and activates adaptive metabolism. This study aims to examine the impact of dexamethasone (DEX) on bio...
Limiting serum concentration in culture medium constitutes an environmental stress that disrupts cellular homeostasis and activates adaptive metabolism. This study aims to examine the impact of dexamethasone (DEX) on biological properties (e.g. viability, adhesion, migration) and glucose and lipid metabolism of prostate epithelial cells under stress conditions. The study used a non-tumorigenic human prostate cell line, PNT1A. In mild serum deprivation conditions, DEX, commonly used in the treatment of castration-resistant prostate cancer, also arrests normal prostate cells in the G0/G1 phase. Observed reduction in metabolic activity and limiting apoptosis of PNT1A cells as related to decreased expression of the NF-κB family and FOXO3 genes. Moreover, DEX modulated PNT1A migration by regulating cell plasticity thought capacity of adhesion to ECM proteins such as fibronectin and collagen I and IV. This was associated with changes in mRNA levels for the genes VIM, ZEB1 and ZEB2. Finally, it seems that dexamethasone helps PNT1A cells adapt to stress and enhance antioxidant defense, possibly by reprogramming lipid metabolism (e.g., LDLR, CPT1, MGLL), but not necessarily glucose metabolism.
Dehydroepiandrosterone sulphate (DHEAS) supplementation impacts adrenal cortex morphophysiology of aged female gerbils.
Bedolo CM, Cozim IC, Grigio V … +7 more , Bernussi GR, Silva SB, Guerra LHA, Campos SGP, Vilamaior PSL, Leonel ECR, Taboga SR
Steroids · 2025 Jun · PMID 40280348 · Publisher ↗
During the process of aging, it is common for women to take dehydroepiandrosterone sulphate (DHEAS) supplements to prevent adrenopause. However, the potential effects of this supplementation on the adrenal cortex have no...
During the process of aging, it is common for women to take dehydroepiandrosterone sulphate (DHEAS) supplements to prevent adrenopause. However, the potential effects of this supplementation on the adrenal cortex have not yet been fully elucidated. Therefore, the present study aimed to analyze the effects of DHEAS supplementation on the adrenal cortex of female Mongolian gerbils during the aging process. The experiment was conducted by dividing the aged female gerbils (18 months of age) into two groups (n = 5). The control group received no treatment, while the experimental group received 60 mg/kg of DHEAS for 5 weeks. The adrenal glands of both groups were then subjected to morphological, hormonal and immunohistochemistry analyses. The results showed that DHEAS supplementation led to a significant increase in the accumulation of lipofuscin granules in the adrenal cells. Furthermore, decreases in ERα and ERβ and the enzymes CYP17 and 17βHSD, and an increase in the 5α-reductase enzyme in the adrenal cortex were also observed. The results suggest that DHEAS supplementation has a negative feedback effect on the adrenal cortex, affecting its morphophysiology and, consequently, the gland's functionality. In addition, DHEAS supplementation does not reverse all aspects of the effects of aging on adrenal gland homeostasis.
Mendelian randomization studies of testosterone exposure: A systematic review.
Rhomberg-Kauert AM, Tulstrup M, Badsted C … +2 more , Horwitz H, Heerfordt IM
Steroids · 2025 Jun · PMID 40239830 · Publisher ↗
BACKGROUND: Testosterone impacts reproductive health, cardiovascular function, and metabolism. Considering the use of testosterone therapy and anabolic steroid misuse, understanding its health effects is important. While...
BACKGROUND: Testosterone impacts reproductive health, cardiovascular function, and metabolism. Considering the use of testosterone therapy and anabolic steroid misuse, understanding its health effects is important. While randomized clinical trials provide short-term insights, and observational studies struggle with confounding factors, Mendelian randomization offers an alternative by using genetic variations to explore causal relationships. METHOD: A systematic search was performed using MEDLINE to identify studies published from inception to October 2024. We included studies that conducted a Mendelian randomization analysis to evaluate associations between testosterone exposure and any health outcomes in males. RESULTS: Twenty-nine Mendelian randomization studies were included, examining a broad spectrum of health outcomes linked to testosterone exposure. Cardiovascular and metabolic health, alongside prostate cancer risk, were the most frequently studied areas. Most studies indicated that higher testosterone levels were associated with adverse cardiovascular outcomes, such as increased risks of thromboembolism, ischemic heart disease, and heart failure. Elevated levels of genetically predicted free testosterone consistently showed a correlation with increased prostate cancer risk. The relationship between testosterone and type 2 diabetes remained inconclusive. Neuropsychiatric and musculoskeletal outcomes received less attention, while dermatological, infectious, and respiratory health were minimally explored. CONCLUSION: This review provides information about the causal relationships between testosterone exposure and health outcomes, contributing to the ongoing discourse on testosterone-related health risks and benefits. The included studies exhibit great heterogeneity.
Synthesis, NMR and X-ray characterization of dibenzoannulated dimeric steroid spiroketals. Evaluation of cytotoxicity and anti-inflammatory activity.
Gutiérrez-Aguilar RU, Antolín-González JA, Campos-Xolalpa N … +4 more , Perez-Gutierrez S, Flores-Álamo M, Vazquez-Chavez J, Iglesias-Arteaga MA
Steroids · 2025 Jun · PMID 40233843 · Publisher ↗
Two dibenzoannulated dimeric steroid spiroketals were obtained from cholesterol and 1,4-phenylenedimethanol. The key step in synthetic protocol is a Pd-catalyzed double spiroketalization in an adduct obtained from the do...
Two dibenzoannulated dimeric steroid spiroketals were obtained from cholesterol and 1,4-phenylenedimethanol. The key step in synthetic protocol is a Pd-catalyzed double spiroketalization in an adduct obtained from the double Sonogashira coupling of the 5α and 5β diastereomers of 4,5-secocholestan-5-ol. A detailed NMR characterization supported by Single Crystal X-ray Diffraction studies corroborated the obtained structures. While no cytotoxic effect was observed, the obtained compounds produced a significant reduction in the production of nitric oxide in macrophages stimulated with Lipopolysaccharide (LPS), indicating a potential anti-inflammatory activity.
Evaluation of the diagnostic value of G protein-coupled estrogen receptor (GPER) in COVID-19 cases at Tokat Province.
Guzelgul F, Kurutas EB
Steroids · 2025 Jun · PMID 40222439 · Publisher ↗
OBJECTIVE: Factors affecting the clinical course of COVID-19, an infectious respiratory disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in humans, are still poorly understood. G protein-cou...
OBJECTIVE: Factors affecting the clinical course of COVID-19, an infectious respiratory disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in humans, are still poorly understood. G protein-coupled estrogen receptor (GPER) is a protein encoded by the GPER gene in humans. GPER is activated by binding to estradiol, a female sex hormone, leading to mediation of estradiol's rapid cellular effects. In this study, which was conducted for the first time, we aimed to investigate GPER levels and their diagnostic value in COVID-19 patients. METHODS: A total of 71 individuals [Female/Male (n = 36/35) range of ages 32 ∼ 62] were enrolled in this study and categorized into three groups: the patient group consisted of individuals diagnosed with COVID-19 and receiving supportive treatment in the intensive care unit (ICU), the mild group consisted of COVID-19 patients who received outpatient treatment, and the control group. Enzyme-linked immunosorbent assay (ELISA) was used to measure serum GPER levels. RESULTS: The general sex distribution of the patients was analyzed, revealing that 35(49.3 %) were male and 36(50.7 %) were female. GPER levels were significantly increased in severe COVID-19 females compared to control and mild course groups (p < 0.05). A GPER cut-off value of 2.95 ng/mL showed diagnostic accuracy in severe COVID-19 cases. CONCLUSION: This study, conducted for the first time, demonstrates that GPER levels are significantly associated with COVID-19 severity in female patients, suggesting that GPER may serve as a diagnostic marker for the progression of COVID-19.
From root to Recovery: The role of herbs in polycystic ovary syndrome management.
Zafar NU, Qureshi R, Siddiqa A … +8 more , Mustafa Naqvi SA, Waheed F, Mashwani ZU, Ali A, Hernández Ramírez KA, Medina-Pérez G, Pelaez-Acero A, Ahmad A
Steroids · 2025 Jun · PMID 40210106 · Publisher ↗
Polycystic ovarian syndrome (PCOS) is a prevalent complicated endocrine condition affecting women, caused by both hereditary and environmental factors. It often emerges during the reproductive years (15-35 years) and now...
Polycystic ovarian syndrome (PCOS) is a prevalent complicated endocrine condition affecting women, caused by both hereditary and environmental factors. It often emerges during the reproductive years (15-35 years) and now affects 1 out of 10 women worldwide. PCOS is distinguished by high androgen levels, particularly testosterone, as well as the appearance of many ovarian cysts (more than 10), which result in anovulation, infertility, and irregular menstrual periods. Furthermore, PCOS is associated with a variety of endocrine and metabolic abnormalities, including obesity, hirsutism, acne, diabetes, insulin resistance, and poor glucose tolerance. PCOS treatment includes allopathic, Ayurvedic, and natural therapies, as well as lifestyle changes. In comparison to allopathic treatments, herbal medicines are recognized for their cost-effectiveness, efficacy, and favourable role in PCOS management/treatment. This literature review briefly examines PCOS diagnosis, symptoms, hormonal imbalance, causes, related risk factors, and management, with a particular emphasis on the role of herbal remedies in PCOS treatment. This review highlights several medicinal plants with potential therapeutic benefits for various health conditions. These herbs have demonstrated efficacy in managing ailments such as hypothyroidism, hyperplasia, obesity, diabetes, menorrhagia, sleep disturbances, cardiovascular disorders, hyperlipidemia, hirsutism, infertility, and irregular menstrual cycles. The information was sourced from PubMed and multiple review articles. Various herbs, whether used individually, in combination, or as extracts, may help reduce risk factors associated with polycystic ovary syndrome (PCOS).
Genetic insights into vitamin D deficiency: a case-control study of GC and CYP24A1 gene polymorphism.
Usama, Khan A, Raza MK … +4 more , Abbas K, Mansour L, Ali A, Imran M
Steroids · 2025 Jun · PMID 40199414 · Publisher ↗
Despite the sunny climate, vitamin D deficiency is highly prevalent in several parts of the world. Several risk factors are associated with VD deficiency, including single nucleotide polymorphism and post-translational m...
Despite the sunny climate, vitamin D deficiency is highly prevalent in several parts of the world. Several risk factors are associated with VD deficiency, including single nucleotide polymorphism and post-translational modifications in its transport protein, known as vitamin D binding protein (DBP) or GC and CYP24A1, a protein associated with its degradation. Our study explores the impact of rs4588 and rs7041 in the GC gene, along with CYP24A1 rs4809960 and rs2585428, on serum vitamin D and the risk of vitamin D insufficiency. This study enrolled 114 healthy controls and 239 vitamin D-deficient subjects. SNPs were determined using polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP). The G/T genotype of D432E and the A/A genotype of T436K in the GC gene were observed to be risk factors for vitamin D deficiency. Overall, a significant (P < 0.05) association was observed between the D432E and T436K polymorphism and vitamin D deficiency. Polymorphic genotypes of CYP24A1 rs4809960 and rs2585428 polymorphisms were significantly associated with a higher risk of Vitamin D deficiency. D432E and T436K polymorphisms were associated with decreased vitamin D and increased PTH levels in vitamin D-deficient individuals. Similarly, both CYP24A1 polymorphisms were significantly associated with a higher risk of vitamin D deficiency. Also, a negative association was observed between sufficient serum levels of 25-hydroxyvitamin D and PTH levels.
Stress responses in blood donors: Oral fluid hormone dynamics and implications for donor support.
Alterio A, Feltracco M, Mazzi G … +3 more , Rosso B, Prosdocimi L, Gambaro A
Steroids · 2025 May · PMID 40158788 · Publisher ↗
Glucocorticoids (cortisol and cortisone) hormones are potential biomarkers for monitoring physiological stress in humans. These hormones are released into the bloodstream but are also detectable in other biological matri...
Glucocorticoids (cortisol and cortisone) hormones are potential biomarkers for monitoring physiological stress in humans. These hormones are released into the bloodstream but are also detectable in other biological matrixes such as oral fluid. Oral fluid hormone levels reflect those found in the blood, but oral fluid sampling is quicker and non-invasive, making it a viable alternative matrix for studying stress markers. This study investigates the stress response of blood donors at three different donation moments by analyzing cortisol and cortisone levels in oral fluid samples. To simultaneously detect these analytes, we developed and validated a new highly sensitive method using high-performance liquid chromatography coupled to a triple quadrupole mass spectrometer (HPLC-MS/MS). Glucocorticoid hormones were found in all samples with cortisone exhibiting higher concentrations than cortisol. Statistical results revealed a weakly negative trend over time for both analytes levels, indicating that the most crucial donation moment is upon donors' arrival. A notable distinction was found in the evolution of the glucocorticoid hormones in different locations, suggesting that different environmental factors influence stress level more than the act of donation itself.
Unleashing the pharmacological potential of taste receptors in reproductive processes beyond their gustatory role.
Magdy N, Abdelkader NF, Zaki HF … +1 more , Kamel AS
Steroids · 2025 May · PMID 40154931 · Publisher ↗
Traditionally, taste receptors (TRs) have been understood to reside within the taste buds on the tongue, serving as initiators for different taste perceptions. However, recent research has expanded our understanding, rev...
Traditionally, taste receptors (TRs) have been understood to reside within the taste buds on the tongue, serving as initiators for different taste perceptions. However, recent research has expanded our understanding, revealing that TRs are found throughout the body and perform a wide range of functions beyond taste perception as non-tasting functions. These receptors, along with their genetic variations, have been linked to various human health conditions. They are activated by an array of substances, including hormones, nutrients, and toxins, indicating their involvement in numerous biological processes. Specifically, in males, TRs are notably present in the testes and epididymis, where they contribute to the hormonal production, spermatogenesis, and sperm maturation. In females, these receptors are found in the ovaries, uterus, and myometrium, playing crucial roles in ovulation, menstrual cycle regulation, and embryo implantation. There are a lot of missed areas regarding TRs research that imposes to fulfill the gaps in the current understanding of their role in reproduction. This review aims to provide a comprehensive overview of the emerging roles of extraoral TRs in reproductive health, highlighting their physiological and pathophysiological significance in various reproductive processes. As well, grabbing the attention towards the release of new pharmacological interventions to manage conception and contraception in male and female was considered.
BSS-4, a diosgenin analogue, reduces carrageenan-induced paw inflammation in rat.
Casimiro-Rosas M, Parra I, Sandoval-Ramírez J … +4 more , Fernández Herrera MA, Tizabi Y, Martínez-García I, Mendieta L
Steroids · 2025 May · PMID 40122485 · Publisher ↗
Inflammation is an adaptive response that ensures the survival of the organism in the face of injuries or trauma primarily via the immune system. However, overactivation of this process can be detrimental to the point of...
Inflammation is an adaptive response that ensures the survival of the organism in the face of injuries or trauma primarily via the immune system. However, overactivation of this process can be detrimental to the point of fatality. To overcome this overactivation, immunosuppressant agents such as steroids and non-steroidal anti-inflammatory drugs (NSAIDs) are used. Given the limitations of these drugs, including their side effects, an urgent need for development of potent and safer anti-inflammatory drugs is evident. Diosgenin, a steroidal saponin (a glycoside found in plants) and its analog, BSS-4 are gaining ground in this respect. Our objective in this study was to determine the effectiveness of BSS-4 in an established model of inflammation and provide clues on its mechanism of action. Carrageenan (Carr)-induced paw edema was used to evaluate the effectiveness of two doses of BSS-4 (0.5 and 1 mg/kg administered intraperitoneally) in adult male Wistar rats. Plantar edema was induced by subcutaneous injection of 50 µL of carrageenan (1 %) into the plantar aponeurosis of the right paw. Inflammatory cytokine markers, tumor necrosis factor-alpha (TNF-α), and interleukin-1 beta (IL-1β) were quantified in this paw region using immunohistochemical assays. BSS-4 at 0.5 mg/kg dose, significantly reduced the paw edema up to three hours after administration. Concomitantly, TNF-α and IL-1β immunostaining were significantly reduced. BSS-4 also preserved the tissue architecture as assessed by hematoxylin and eosin (H&E) staining. These results indicate that BSS-4 can impart potent anti-inflammatory effects as well as reductions in TNF-α and IL-1β in an inflammatory rat model.
Microbial steroid biotransformation: Regio- and stereo selective 17β-reduction by Priestia aryabhattai.
Sudhakar Y, Manasa RK, Priyadarshini D … +3 more , Dalsaniya SC, Sheelu G, Kumaraguru T
Steroids · 2025 May · PMID 40120840 · Publisher ↗
The conversion of 17-oxosteroids to 17β-hydroxysteroids stands as a pivotal process in the synthesis of numerous steroidal drugs and intermediates. This study explored the potential of the strain Priestia aryabhattai (II...
The conversion of 17-oxosteroids to 17β-hydroxysteroids stands as a pivotal process in the synthesis of numerous steroidal drugs and intermediates. This study explored the potential of the strain Priestia aryabhattai (IICT-BC-1279) to catalyze the reduction of the C-17 carbonyl group in androst-4-ene-3,17-dione (AD), resulting in the exclusive production of testosterone (TS) through its 17β-hydroxysteroid dehydrogenase (17β-HSD) activity. Optimal conditions for this reduction were achieved at pH 7.0 and 25 °C, with supplementation of AD as an inducer (0.01 g/L), 1 % Tween 80 (w/v) and ethanol as co-solvent. Under these optimized parameters, 0.5 g/L AD was efficiently converted to TS as a sole product, achieving a yield of > 95 % and diastereomeric excess (d.e) of > 99 % within 48 h. The absence of by-products in this microbial 17β-reduction process simplifies product purification, highlighting the strain's potential as a valuable biocatalyst for this essential transformation. Additionally, the conversion of androsta-1,4-diene-3,17-dione (ADD) to (+)-Boldenone (BD) was studied to explore substrate scope.
Target-specific high-throughput screening of anti-inflammatory phytosteroids for autoimmune diseases: A molecular docking-dynamics simulation approach.
Sahoo A, Paidesetty SK, Panda M
Steroids · 2025 May · PMID 40120839 · Publisher ↗
Without proper pathophysiology and recommended therapy, synthetic steroids are widely used as a first-line option for the management of autoimmune diseases. However, their prolonged use often leads to severe side effects...
Without proper pathophysiology and recommended therapy, synthetic steroids are widely used as a first-line option for the management of autoimmune diseases. However, their prolonged use often leads to severe side effects such as osteoporosis, hypertension, cardiovascular, gastrointestinal complications, etc. To search for potential and safer therapeutic options, the present study aims to explore the potency and drug-ability profiles of anti-inflammatory phytosteroids (PSs). In a target-specific approach, we have selected three key molecular targets: glucocorticoid receptor/GR (PDB ID: 4P6W), cyclooxygenase-2/COX2 (PDB ID: 5F1A), and inducible nitric oxide synthase/iNOS (PDB ID: 4NOS) for a docking study of 167) selected PSs. The drug-chemistry profiles (physicochemical, toxicity, pharmacokinetic, drug-ability, etc.) of PSs were also assessed using various bioinformatics and chemoinformatics tools. The above assessment suggested that withaminilide B (PS46) is a lead candidate with higher drug-ability properties. Further, the drug stability and kinetic behaviour of the lead with the GR target 'GR-withaminilide B' in comparison with the control drug, 'GR-triamcinolone acetonide' docking complex, were studied through molecular dynamics (MD) simulation at 200 nanosecond with free energy calculation (MM/PBSA). Overall findings suggested that PSs exhibit distinct drug-ability profiles based on their functional attachments with a steroidal core moiety, where withaminilide B is a lead PSs among all to be used as alternative/ complementary candidates expected with limited adverse effects. Further experimentation is essential before mainstream application, but the study provided a platform to select drug-able candidates with a higher chance of experimental success and accelerate the drug discovery process within limited resources.
Isoxazolyl steroid blocks the Shh signaling pathway and the expression of MMP-2 and MMP-9 in cervical carcinoma cell lines.
Timoshenko O, Kugaevskaya E, Gureeva T … +7 more , Morozevich G, Lupatov A, Mekhtiev A, Rudovich A, Zhabinskii V, Khripach V, Lisitsa A
Steroids · 2025 May · PMID 40101884 · Publisher ↗
Cervical cancer is the fourth leading cause of cancer death among women worldwide. Matrix metalloproteinases MMP-2 and MMP-9 play a leading role in the processes of invasion and metastasis in cervical cancer. Research on...
Cervical cancer is the fourth leading cause of cancer death among women worldwide. Matrix metalloproteinases MMP-2 and MMP-9 play a leading role in the processes of invasion and metastasis in cervical cancer. Research on the development of MMP inhibitors not yielded the expected results due to their serious side effects. Study of signaling pathways involved in regulation of MMPs expression is of great importance for search of new classes of therapeutic drugs. Aberrant activation of the Sonic Hedgehog (Shh) signaling pathway is associated with increased MMPs in many types of human cancer. This study investigated the inhibitory action of 17β-((3-butylisoxazol-5-yl)methyl)-androst-5-en-3β-ol on the Shh signaling pathway key genes (Ptch, Smo, Gli) expression and MMP-2, MMP-9 genes expression in human cervical carcinoma cell lines (SiHa and CaSki) and keratinocytes (HaCaT). Cyclopamine was used for comparative analysis. Gene expression analysis was performed using real-time PCR; the effects on survival and cell cycle were studied using the MTT test and flow cytometry method. 17β-((3-butylisoxazol-5-yl)methyl)-androst-5-en-3β-ol had higher cytotoxicity and more effectively blocked the Shh signaling pathway genes and MMP-2 and MMP-9 genes compared to cyclopamine in all cell lines. The results obtained demonstrate potential of 17β-((3-butylisoxazol-5-yl)methyl)-androst-5-en-3β-ol as the anticancer drug that simultaneously block the Shh signaling pathway and MMP expression. We are confident that the search for substances capable of simultaneously affecting several key components involved in tumor progression is of great importance for the creation of next-generation therapeutic agents.
Stereo- and regioselectivity in nitrile oxide cycloaddition reactions to norethisterone acetate as dipolarophile.
Faita G, Mella M, Quadrelli P
Steroids · 2025 May · PMID 40097059 · Publisher ↗
Benzo- and anthracenenitrile oxides undergo 1,3-dipolar cycloaddition reactions with 17 α- acetate norethisterone affording the expected isoxazoline and isoxazoles derivatives in good yields and as single regioisomers. T...
Benzo- and anthracenenitrile oxides undergo 1,3-dipolar cycloaddition reactions with 17 α- acetate norethisterone affording the expected isoxazoline and isoxazoles derivatives in good yields and as single regioisomers. The structures of all the new compounds were elucidated on the basis of the corresponding analytical and spectroscopic data, which were presented and discussed. The stereo- and regiochemical outcome of the cycloadditions were also accounted on the basis of 1,3-dipolar cycloaddition theory and computational investigations. Electronic (Frontier Orbital theory) and steric effects are at work in orienting selectively the cycloaddition to specific regioisomeric steroids.
Evaluation of the short-term stability of 6α-chloro-testosterone, 6β-bromo-androstenedione and 6-oxo-androstenedione in dimethylsulfoxide and methanol using liquid and gas chromatography - mass spectrometry.
Martínez Brito D, Leogrande P, de la Torre X … +1 more , Botrè F
Steroids · 2025 May · PMID 40068705 · Publisher ↗
This work studied the short-term stability of 6α-chloro-testosterone (6-CT), 6β-bromo-androstenedione (6-BrAED) and 6-oxo-androstenedione (6-oxo-AED) in methanol (MeOH) and dimethylsulfoxide (DMSO) solutions by gas and l...
This work studied the short-term stability of 6α-chloro-testosterone (6-CT), 6β-bromo-androstenedione (6-BrAED) and 6-oxo-androstenedione (6-oxo-AED) in methanol (MeOH) and dimethylsulfoxide (DMSO) solutions by gas and liquid chromatography coupled to mass spectrometry. Solutions of 6-CT, 6-BrAED and 6-oxo-AED were prepared in MeOH and DMSO. They were stored at room temperature, +4°C and -20 °C. Measurements were made at 0, 7, 30, 60 and 90 days after solutions preparation, by liquid chromatography-tandem mass spectrometry and gas chromatography-high resolution mass spectrometry. Although the degradation of 6-CT and 6-BrAED was extensive, the most notable result was that the higher degradation occurred in DMSO instead of MeOH. The interaction of DMSO with halogenated species and secondary hydroxyl groups favored the degradation of these compounds by forming chemically related species. No degradation of 6-oxo-AED in either MeOH or DMSO was observed. Pronounced degradation of the 6-CT and 6-BrAED, during the derivatization reaction for the gas chromatography-mass spectrometry analysis was observed. Because of the acidic condition of the reaction and depending on the reactant, it was favored the loss of the halogen molecule or the dehydration reaction to form the unsaturated (Δ6) steroid derivative. Our finding suggests to take duly into account the possibility of degradation processes when performing quantitative determination of 6-CT, 6-BrAED and 6-oxo-AED by chromatographic-spectrometric techniques based on the use of reference solutions stored for sufficiently long times.
Antimicrobial diterpenoids from Rosmarinus officinalis.
Xu QJ, Liu JC, Xu J … +3 more , Wang X, Shang XY, Zi J
Steroids · 2025 May · PMID 40043926 · Publisher ↗
Three new diterpenoids, 12,16-epoxy-11-hydroxy-17(15 → 16)-abeo-abieta-8,11,13-trien-7-one (1), 7,12-dihydroxy abieta-6,8,10(5),11,13-quien-20-oic acid 1,20-lactone (2), labda-5(10),13(E)-dien-15-ol (11), one new natural...
Three new diterpenoids, 12,16-epoxy-11-hydroxy-17(15 → 16)-abeo-abieta-8,11,13-trien-7-one (1), 7,12-dihydroxy abieta-6,8,10(5),11,13-quien-20-oic acid 1,20-lactone (2), labda-5(10),13(E)-dien-15-ol (11), one new natural product (2E,6E)-3,7-dimethyl-9-[(1S,6R)-1,2,6-trimethylcyclohex-2-enyl]nona-2,6-dien-1-ol (16) and thirteen known compounds were isolated and elucidated from the excellent antimicrobial active fractions of Rosmarinus officinalis ethanol extract. The structures of the isolated compounds were determined by spectral data analysis and combined with literature reports. Among them, monocyclic diterpenoids (16 and 17) were discovered from rosemary for the first time. All isolated compounds were tested for antimicrobial activity against four strains (B. subtilis, S. aureus, P. aeruginosa, and Fusarium spp.), with six compounds showing very strong inhibitory activity against B. subtilis and four compounds showing strong inhibitory activity against P. aeruginosa.
17β-estradiol delays cardiac aging through suppressing the methylation of Beclin1 in a murine model.
Ye L, Wang R, Zhao J … +2 more , Chen J, Wang F
Steroids · 2025 Apr · PMID 40032072 · Publisher ↗
INTRODUCTION: Cardiac endogenous senescence will gradually change and aggravate with age. Recent research showed that 17β-estradiol (17β-E2), an estrogen with numerous biological activities including the prevention of va...
INTRODUCTION: Cardiac endogenous senescence will gradually change and aggravate with age. Recent research showed that 17β-estradiol (17β-E2), an estrogen with numerous biological activities including the prevention of vascular senescence. However, how 17β-E2 against cardiac aging is still unknown. This work addressed the underlying mechanism with regard to Beclin1 and autophagy activity to better understand the anti-senescent effect of 17β-E2 on a well-established animal model of cardiac aging. MATERIAL AND METHODS: In this study, an aging model in female mice was established using d-galactose and ovariectomy. Cardiac function was evaluated by echocardiography, RNA-seq was performed to analyze the gene expression profiles of myocardial tissues from 17β-E2 treated mice. Additionally,The levels of Beclin1, LC3, P62, and ATG5 in myocardial tissues were assessed using qPCR and Western blotting. Methylation levels of the Beclin1 promoter region in myocardial tissues were determined by MSP and BSP. RESULTS: The findings demonstrated that cardiac aging mice treated with 17β-E2 had improved heart function. 17β-E2 restored EF(increase 1.25-fold) and FS(increase 1.2-fold) to near-normal levels. By RNA-sequencing and Gene Set Enrichment Analysis (GSEA) analysis, the autophagy signaling pathway was further enriched in the myocardial tissue of cardiac aging mice treated with 17β-E2, and we also discovered that 17β-E2 suppress the methylation of Beclin1 promoter region, which mediate the activation of autophagy signal. CONCLUSIONS: Overall, our data showed that 17β-E2's anti-senescent effect on cardiac aging mice was mediated by the crucial suppression of methylation in the Beclin1 promoter area and subsequent activation of the autophagy signal, which may present a possible therapeutic approach to prevent cardiac aging.
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