Xanthohumol (XN) and four minor hops prenylflavonoids: α,β-dihydroxanthohumol (2HXN), isoxanthohumol (IXN), 8-prenylnaringenin (8PN), 6-prenylnaringenin (6PN), were tested for antiproliferative activity towards human cancer normal cell lines. Nonprenylated naringenin (NG) was used as a model compound. Xanthohumol, the most active compounds. exhibited higher than cisplatin (CP) against five lines: ovarian resistant to A2780cis, breast MDA-MB-231 T-47D, prostate PC-3, colon HT-29....

Summary The effect of cultivation system on phenolic profile, antioxidant capacity and antiproliferation activity in black red currants was evaluated. Results from this study showed that Ribes fruit grown organic posses significantly higher total phenolics, especially anthocyanins, ( DPPH FRAP ) than conventional system. Phenolic compounds were systematically identified characterised by UPLC / MS Q‐ TOF . mean value polyphenol content organically similar but statistically compared with the...

Abstract Background Active vitamin D analogs that are less toxic than calcitriol can be useful in the combined treatment of patients suffering from colon cancer. In present study we demonstrate, for first time an vivo model system, biological effect therapy using 5-fluorouracil (5-FU) along with analog PRI-2191 (tacalcitol, 1,24-dihydroxyvitamin 3 ) or PRI-2205 (5,6-trans-isomer calcipotriol) on Methods We investigated influence anticancer activity 5-FU capecitabine mice bearing MC38 mouse...

Recent developments demonstrate that tumor-derived extracellular vesicles (EVs) could become a highly effective tool for delivery of antitumor factors. The main objective the study was to determine whether EVs secreted by MC38 colon carcinoma cells genetically engineered overproduction interleukin (IL-)12 and/or shRNA targeting TGF-β1 are effectively loaded with these molecules and obtained be an efficient therapy. Fractions released modified [both exosomes (mTEx) microvesicles (mTMv)] those...

In the present study, we evaluated antitumor effect of two synthetic analogs vitamin D, namely PRI-2191 [(24R)-1,24-dihydroxyvitamin D3] and PRI-2205 (5,6-trans calcipotriol), in combined human colon HT-29 cancer treatment with 5-fluorouracil (5-FU). Mice bearing tumors transplanted subcutaneously or orthotopically were injected D 5-FU various schedules. A statistically significant inhibition subcutaneous orthotopic tumor growth was observed as a result therapy. cells from vitro culture,...

The antiproliferative activity of xanthohumol (1), a major prenylated chalcone naturally occurring in hops, and its aurone type derivative (Z)-6,4′-dihydroxy-4-methoxy-7-prenylaurone (2) were investigated. Both flavonoids, as well cisplatin reference anticancer drug, tested vivo against ten human cancer cell lines (breast (MCF-7, SK-BR-3, T47D), colon (HT-29, LoVo, LoVo/Dx), prostate (PC-3, Du145), lung (A549) leukemia (MV-4-11) two normal (human microvascular endothelial (HLMEC)) murine...

The aim of this study was to develop a freeze-drying protocol facilitating successful processing plant material containing the small surface antigen hepatitis B virus (S-HBsAg) while preserving its VLP structure and immunogenicity. Freeze-drying in lettuce leaf tissue, without any isolation or purification step, investigated. Each process step consecutively evaluated best parameters were applied. Several drying profiles excipients tested. profile 20°C for 20 h primary 22°C 2 secondary as...

Common food flavonoids: chrysin, apigenin, luteolin, diosmetin, pinocembrin, naringenin, eriodictyol, hesperetin, and their analogues with an additional hydroxyl group at the C-8 position obtained via biotransformation were tested for antioxidant activity using ABTS, DPPH, ferric ion reducing power (FRAP) methods. They also antiproliferative against selected human cancer cell lines—MV-4-11 (biphenotypic B myelomonocytic leukemia), MCF7 (breast carcinoma), LoVo (colon cancer), LoVo/DX...

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...

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...

Numerous in vitro and vivo studies have demonstrated that calcitriol [1,25(OH)2D3] different vitamin D analogs possess antineoplastic activity, regulating proliferation, differentiation apoptosis, as well angiogenesis. Vitamin compounds been shown to exert synergistic effects when used combination with agents anticancer therapies cancer models. The aim of this study was evaluate the mechanisms cooperation [1,24(OH)2D3 (PRI‑2191) 1,25(OH)2D3] tyrosine kinase inhibitors (imatinib sunitinib)...

Cancer cell cross-talk with the host endothelium plays a crucial role in metastasis, but underlying mechanisms are still not fully understood. We studied involvement of protein disulphide isomerase A1 (PDIA1) human breast cancer (MCF-7 and MDA-MB-231) adhesion transendothelial migration. For comparison, PDIA1 proliferation, migration, cycle apoptosis was also assessed. Pharmacological inhibitor, bepristat 2a silencing were used to inhibit PDIA1. Inhibition by markedly decreased cells...

Analogs of 1,25-dihydroxyergocalciferol, modified in the side-chain and A-ring, were tested for their antiproliferative activity against a series human cancer cell lines vitro vivo toxicity. The proliferation inhibition caused by analogs was higher than that parent compounds, while toxicity, measured as serum calcium level, lower. All able to induce, HL-60 MV4-11 leukemic cells, G₀/G₁ cycle arrest differentiation expressed morphological signs typical monocytes. also induced expression CD11b...

Diastereomeric and geometric analogs of calcipotriol, PRI-2202 PRI-2205, were synthesized as advanced intermediates from vitamin D C-22 benzothiazoyl sulfones side-chain aldehydes using our convergent strategy. Calcitriol, calcipotriol (PRI-2201) tacalcitol (PRI-2191) used the reference compounds. Among a series tested diastereomeric analog showed strongest antiproliferative activity on human breast cancer cell line MCF-7, whereas PRI-2205 was weakest. Both less potent in against HL-60 cells...

6-Amino-2-thiouracil (1) was condensed with benzenesulfonyl chloride and p-toluenesulfonyl in presence of pyridine as an acid binder to give sulfonamides 2a, b, which could be methylated basic medium methylmercapto derivatives 3a, turn reacted bromine glacial acetic yield 5-bromo 4a, b. On the other hand, compounds b were cyclocondensed monochloroacetyl chloride, p-tolualdehyde acid/pyridine, ethyl bromoacetate corresponding thiazolopyrimidines 5a, 6a, 7a, respectively; also hydrazinolyzed...

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...

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...

Interactions between bacteriophages and mammals strongly affect possible applications of bacteriophages. This has created a need for tools that facilitate studies phage circulation deposition in tissues. Here, we propose red fluorescent protein (RFP)-labelled E. coli lytic phages as new tool the investigation interactions with cells The interaction RFP-labelled living eukaryotic (macrophages) was visualized after 20 min co-incubation. RFP-labeled were applied murine model vivo. Phages...

New vitamin D analogs are interesting candidates for anticancer treatment, including squamous cell carcinomas (SCCs), especially in combination with cytostatics. In order to evaluate the effect of combined application cisplatin, imatinib, or docetaxel and new [PRI-1906: (24E)-24a-homo-(1S)-1,25-dihydroxyergocalciferol, PRI-2191: (24R)-1,24-dihydroxyvitamin D3], against cells two human SCCs lines (SCC-25 FaDu), cytotoxic activity on cycle apoptosis were determined. The synergistic additive...