Synthesis of hydroxytyrosol analogs with enhanced antioxidant and cytostatic properties against MG-63 human osteoblast-like cells and their potential implications for bone health.

Sixteen novel hydroxytyrosol (HT) analogs with substitutions at the C-1 position of the HT aliphatic side chain were synthesized and evaluated for their cytostatic activity against MG-63 human osteoblast-like cells and for their antioxidant properties. The results revealed that these analogs exhibited significantly higher inhibitory activity compared with HT, which served as the positive control. Among these, the cyclo-substituted compounds stood out as particularly potent, demonstrating strong radical scavenging abilities and notable cytostatic effects against MG-63 cells.

Ursolic Acid against Prostate and Urogenital Cancers: A Review of In Vitro and In Vivo Studies.

Prostate cancer is the second most diagnosed form of cancer in men worldwide and accounted for roughly 1.3 million cases and 359,000 deaths globally in 2018, despite all the available treatment strategies including surgery, radiotherapy, and chemotherapy. Finding novel approaches to prevent and treat prostate and other urogenital cancers effectively is of major importance.

Discovery of New 1,4,6-Trisubstituted-1-pyrazolo[3,4-]pyridines with Anti-Tumor Efficacy in Mouse Model of Breast Cancer.

Purine analogues are important therapeutic tools due to their affinity to enzymes or receptors that are involved in critical biological processes. In this study, new 1,4,6-trisubstituted pyrazolo[3,4-]pyridines were designed and synthesized, and their cytotoxic potential was been studied. The new derivatives were prepared through suitable arylhydrazines, and upon successive conversion first to aminopyrazoles, they were converted then to 1,6-disubstituted pyrazolo[3,4-]pyridine-4-ones; this served as the starting point for the synthesis of the target compounds.

Resveratrol against Cervical Cancer: Evidence from In Vitro and In Vivo Studies.

Cervical cancer affects many women worldwide, with more than 500,000 cases diagnosed and approximately 300,000 deaths each year. Resveratrol is a natural substance of the class of phytoalexins with a basic structure of stilbenes and has recently drawn scientific attention due to its anticancer properties. The purpose of this review is to examine the effectiveness of resveratrol against cervical cancer.

The T350G Variation of Human Papillomavirus 16 Gene Prevails in Oropharyngeal Cancer from a Small Cohort of Greek Patients.

Recent trends have shown a dramatic rise in the incidence of oropharyngeal squamous cell carcinoma strongly associated with high-risk human papillomavirus (HPV) of type 16. The genetic variability of HPV16 has been extensively studied in cervical cancer but there are very limited published data concerning the genetic variations of this HPV type in oropharyngeal cancer. In the present study, the genetic variations of HPV16 gene sequences originated from a small cohort of Greek patients diagnosed with oropharyngeal cancer were assessed.

Novel Substituted Purine Isosteres: Synthesis, Structure-Activity Relationships and Cytotoxic Activity Evaluation.

A number of pyrrolo[2,3-]pyridines, pyrrolo[3,2-]pyrimidines and pyrazolo[4,3-]pyrimidines were designed and synthesized as antiproliferative agents. The target compounds possessed selected substituents in analogous positions on the central scaffold that allowed the extraction of interesting SARs. The cytotoxic activity of the new derivatives was evaluated against prostatic (PC-3) and colon (HCT116) cell lines, and the most potent analogues showed IC values in the nM to low µM range, while they were found to be non-toxic against normal human fibroblasts (WI-38).

Pumpkin Seed Extracts Inhibit Proliferation and Induce Autophagy in PC-3 Androgen Insensitive Prostate Cancer Cells.

Pumpkin seed is a rich source of polyphenols and other bioactive compounds that may act as chemopreventive agents against cancer. In this study, five different extracts of pumpkin seeds were evaluated for their ability to affect proliferation and autophagy on PC-3 prostate cancer cells. All extracts (water [W], methanolic, acetone, ethylacetate, and polar lipid [PL]) inhibited cell proliferation in a dose-dependent manner.

Animal Coronaviruses Induced Apoptosis.

Apoptosis is a form of programmed death that has also been observed in cells infected by several viruses. It is considered one of the most critical innate immune mechanisms that limits pathogen proliferation and propagation before the initiation of the adaptive immune response. Recent studies investigating the cellular responses to SARS-CoV and SARS-CoV-2 infection have revealed that coronaviruses can alter cellular homeostasis and promote cell death, providing evidence that the modulation of apoptotic pathways is important for viral replication and propagation.

Fermentation of and mushrooms and their extracts by the gut microbiota of healthy and osteopenic women: potential prebiotic effect and impact of mushroom fermentation products on human osteoblasts.

Recent data have highlighted the role of the gut microbiota and its several metabolites in maintaining bone health. Thus, gut microbiota manipulation, e.g.

Assessment of the Nutraceutical Effects of Oleuropein and the Cytotoxic Effects of Adriamycin, When Administered Alone and in Combination, in MG-63 Human Osteosarcoma Cells.

Oleuropein (OLEU) is the most distinguished phenolic compound found in olive fruit and the leaves of L., with several pharmacological properties, including anti-cancer actions. Adriamycin (ADR) is an anthracycline widely used as a chemotherapeutic agent, although it presents significant side effects.

Silymarin Enriched Extract (Silybum marianum) Additive Effect on Doxorubicin-Mediated Cytotoxicity in PC-3 Prostate Cancer Cells.

Silymarin-enriched extract (SEE) is obtained from (Asteraceae). Doxorubicin (DXR) is a widely used chemotherapeutical yet with severe side effects. The goal of the present study was to assess the pharmacologic effect of SEE and its bioactive components silibinin and silychristine when administrated alone or in combination with DXR in the human prostate cancer cells (PC-3).

-Enhanced Extract and Adriamycin Antiproliferative Effect on PC-3 Prostate Cancer Cells.

Prostate cancer is the second most commonly diagnosed cancer in men worldwide, which is almost incurable, once it progresses into the metastatic stage. Adriamycin (ADR) is a known chemotherapeutic agent that causes severe side effects. In recent years, studies in natural plant products have revealed their anticancer activities.

Levosimendan prevents doxorubicin-induced cardiotoxicity in time- and dose-dependent manner: implications for inotropy.

Aims: Levosimendan (LEVO) a clinically-used inodilator, exerts multifaceted cardioprotective effects. Case-studies indicate protection against doxorubicin (DXR)-induced cardiotoxicity, but this effect remains obscure. We investigated the effect and mechanism of different regimens of levosimendan on sub-chronic and chronic doxorubicin cardiotoxicity.

Design and Synthesis of New Substituted Pyrazolopyridines with Potent Antiproliferative Activity.

Background: Purine isosteres are often endowed with interesting pharmacological properties, due to their involvement in cellular processes replacing the natural purines. Among these compounds, pyrazolopyridines are under active investigation for potential anticancer properties.

Objectives: Based on previously discovered substituted pyrazolopyridines with promising antiproliferative activity, we designed and synthesized new, suitably substituted analogues aiming to investigate their potential activity and contribute to SAR studies of this class of bioactive compounds.

Synthesis and antiproliferative activity of new pyrazolo[3,4-c]pyridines.

Background: Several pyrazolopyridines possess promising pharmacological activities, mainly attributed to their antagonistic nature towards the natural purines in many biological processes. Cytotoxicity and anticancer potential of this class of compounds is mainly related to induction of apoptotic cell death and inhibition of protein kinases.

Objectives: This prompted us to design, synthesize and study the antiproliferative activity of a number of new 3,7-disubstituted pyrazolo[3,4-c] pyridines.

Bioactive natural products against prostate cancer: mechanism of action and autophagic/apoptotic molecular pathways.

Prostate cancer is one of the leading causes of death worldwide for men. There is increasing evidence that diet and lifestyle play a crucial role in prostate cancer biology and tumorigenesis. Due to the fact that conventional chemotherapy is not adequately effective against prostate cancer and has severe side effects, numerous in vitro studies have been conducted in order to identify the potent cytotoxic or chemopreventive activity of naturally occurring compounds and their respective molecular mechanisms of action.

Clinical significance of nuclear factor (NF)-kappaB levels in urothelial carcinoma of the urinary bladder.

Nuclear factor (NF)-kappaB has been reported to be constitutively activated in various human neoplasms. However, its clinical significance in bladder urothelial carcinoma (UC) remains an unresolved issue. We conducted this study trying to elucidate the role of NFkappaB in bladder UC and its potential prognostic significance, by quantifying immunohistochemically the levels of p65/RelA expression in paraffin-embedded tissue from 116 patients.