There has been a long search for simple preparation of new cyclic analogues ionophore antibiotics. We report and general synthesis three derivatives polyether ionophore, monensin A (MON). The application the Huisgen 1,3-dipolar cycloaddition azides terminal alkynes to macrocyclization results in concise, synthetic route lacton or lactam only 4 steps. Additionally, macrolactamization by amidation reaction using HATU, commonly used conjugating agent, gives 72% yields utilizes neither high...

Consuming food that is rich in antioxidants reduces the risk of developing chronic diseases and oxidative stress. Fruits vegetables are an excellent source substances with antioxidant pro-health properties. Such raw materials, characterized by a high content polyphenolic compounds capacity, include pear fruits. In this study, concentrations bioactive compounds, as well antioxidant, anti-inflammatory, antiproliferative activity fruits five selected cultivars were determined compared. LC-MS...

Abstract Background Cancer-associated fibroblasts (CAFs) play an important role in the tumor microenvironment. Despite well-known vitro antitumoral effect of vitamin D 3 (VD ), its impact on breast CAFs is almost unknown. In this study, we analyzed ex vivo effects calcitriol isolated from cancer tissues. Methods were cultured with 1 and 10 nM their phenotype; gene expression, protein secretion assessed. Calcitriol-treated CAFs-conditioned media (CM) used to analyze migration expression MCF-7...

Abstract Our research found that vitamin D 3 (VD ) treatment increased lung metastasis in mice with 4T1 murine breast cancer (BC). This study aims to investigate the impact of VD on activation tumor-associated macrophages (TAMs) BC. Mice bearing 4T1, E0771, 67NR BC cells, and healthy mice, were fed diets varying contents (100—deficient, 1000—normal, 5000 IU/kg—elevated). Some 1000 100 IU/kg groups received calcitriol. We studied bone characterized TAMs marrow-derived (BMDMs). cells had...

Abstract Introduction Cancer is the main cause of mortality worldwide, and finding effective treatments with fewer side effects crucial. Medicinal plants offer significant potential in this area. They contain bioactive compounds that may have antitumor effects. The aim study to assess cytotoxicity various medicinal towards several cancer cell lines. Materials Methods Antiproliferative activity extracts from Crataegus monogyna , Rhamnus alaternus Lavandula dentata Aristolochia baetica Erica...

Low vitamin D status is considered as a risk factor for breast cancer and has prognostic significance. Furthermore, deficiency increases after adjuvant therapy, which alters bone metabolism increasing the of osteoporosis. It now postulated that supplementation in treatment delays recurrence thereby extending survival. We evaluated impact calcitriol its low-calcemic analogs, PRI‑2191 PRI‑2205, on tumor growth, angiogenesis, metastasis 4T1 mouse mammary gland cancer. Gene expression analysis...

Retinol-binding protein 4 (RBP4) is proposed as an adipokine that links obesity and cancer. We analyzed the role of RBP4 in metastasis breast cancer patients mice bearing metastatic 4T1 nonmetastatic 67NR mammary gland compared angiogenic potential these cells transduced with Rbp4 (4T1/RBP4 67NR/RBP4 cell lines). Higher plasma levels were observed tumors than healthy donors Increased plasma, tumor tissue, liver, abdominal fat. Moreover, blood vessel network was highly impaired to tumors....

5-Fluorouracil (5-FU) is an anticancer drug that most frequently used to treat colorectal cancer (CRC) patients, but unfortunately it shows limited efficacy. We recently demonstrated vitamin D analogs (VDAs), particularly tacalcitol (coded as PRI-2191), potentiate its activity in vivo mouse and human CRC model. The purpose of this study was explain the mechanism underlying enhancement 5-FU efficacy by PRI-2191 towards HT-29 cells. showed induces CDKN1A (gene encoding p21Waf1/Cip1) expression...

The active forms of vitamin D3 (calcitriol and tacalcitol) coupled to the D receptor (VDR) are known exhibit anti-cancer properties. However, not all cancer cells sensitive its analogs. study aimed determine whether polymorphism VDR is responsible for sensitivity human leukemia lymphoma calcitriol tacalcitol. impact tacalcitol on proliferation morphology nine different cell lines was determined. Only MV-4-11, Thp-1, HL-60 inhibition by showed changes. Subsequently, levels 1,25D3-MARRS...

To analyze if the prometastatic activity of calcitriol (active vitamin D3 metabolite), which was previously observed in a 4T1 breast cancer model, is also found other cancers, and to assess impact various schemes D supply, we used E0771 mouse metastatic 67NR nonmetastatic cells this study. BALB/c C57BL/6 healthy tumor-bearing mice were exposed control (1000 IU), low- (100 high- (5000 IU) diets. Additionally, from day 7 tumor transplantation, 1000 100 IU groups gavaged with (+cal). After 8...

Non-coding micro-RNA (miRNAs) regulate the protein expression responsible for cell growth and proliferation. miRNAs also play a role in cancer cells' response to drug treatment. Knowing that leukemia lymphoma cells show different responses active forms of vitamin D3, we decided investigate selected miRNA molecules regulated proteins, analyzing if there is correlation between proteins two calcitriol tacalcitol. A total nine human lines were analyzed: five leukemias: MV-4-1, Thp-1, HL-60,...

Vitamin D and its analogs are known for their role in the development of breast cancer immunomodulation. Our previous studies have shown pro-metastatic effect calcitriol tacalcitol (PRI-2191) young mice bearing 4T1 anti-metastatic aged ovariectomized (OVX) mice. Therefore, aim our work was to characterize Th17 cell population OVX tumors treated with PRI-2191. The expression genes typical cells examined splenocytes, as well splenocytes differentiated IL-6 TGF-β (iTh17). Expression encoding...

This study investigates the structural, vibrational, and biological properties of novel palladium(II) platinum(II) complexes with 5-chloro-7-azaindole-3-carbaldehyde (5ClL) 4-chloro-7-azaindole-3-carbaldehyde (4ClL) ligands. Infrared Raman spectroscopy, combined DFT (ωB97X-D) calculations, provided valuable information about metal–ligand interactions, cis or trans conformation aldehyde group in ligands, presence isomers metal obtained solid state. In vitro tests were used to evaluate...

A library of 21 novel chiral 1,2,3-triazole-based 2-azabicycloalkane conjugates was designed and synthesized using the copper(I)-catalyzed click reaction. The obtained hybrids were assessed for their antiproliferative potency against three selected human cancer cell lines: Hs294T (melanoma), MIA PaCa-2 (pancreas tumor) NCI-H1581 (lung tumor). majority compounds demonstrated moderate to potent activity, some them appeared more selective than cisplatin, with selectivity index exceeding 9.

In this paper we report the design and synthesis of novel derivatives 4H-3,1-benzothiazinone type heterocyclic analogues, i.e. benzofuro-, azolo- thieno-1,3-thiazin-4-ones possessing 2,4-dihydroxyphenyl substituent. The compounds were obtained by one-step reaction aminobenzamides or aminocarboxamides with aryl-modified sulfinylbis[(2,4-dihydroxyphenyl)methanethione]. Evaluation their antiproliferative potency against human cancer cell lines showed that activity some analogues was similar to...

Abstract A one‐pot synthesis of new 4‐(1,3‐thiazolo[5,4‐ b ]pyridin‐2‐yl)benzene‐1,3‐diols has been described. The compounds were prepared by the reaction sulfinylbis[(2,4‐dihydroxyphenyl)methanethione] derivatives, with various substituents in aryl rings, 2‐chloropyridin‐3‐amines. Their structures deduced from IR and, 1 H‐ and 13 C‐NMR spectroscopic, mass spectrometric, elemental analyses. antiproliferative properties some products against human cancer cell lines comparable to those...

Background/Aim: The study aimed to test the potential for increasing antiproliferative activity of 5-fluorouracil against breast cancer cells various molecular subtypes by vitamin D receptor (VDR) agonists, calcitriol and tacalcitol, used at a low concentration 10 nM. Materials Methods: Calcitriol tacalcitol were increase effect following human cell lines: MCF-7, T47D, BT-474 (luminal); JIMT-1, SKBR-3 (HER2-enriched); MDA-MB-231 (triple-negative/basal-B), non-malignant MCF-10A epithelial...