排序方式: 共有19条查询结果,搜索用时 375 毫秒
1.
Dr. Erika Lisztes Dr. Erika Mező Fruzsina Demeter Lilla Horváth Dr. Szilvia Bősze Dr. Balázs István Tóth Prof. Anikó Borbás Dr. Mihály Herczeg 《ChemMedChem》2021,16(9):1467-1476
The design and synthesis of heparin mimetics with high anticancer activity but no anticoagulant activity is an important task in medicinal chemistry. Herein, we present the efficient synthesis of five Glc-GlcA-Glc-sequenced and one Glc-IdoA-Glc-sequenced non-glycosaminoglycan, heparin-related trisaccharides with various sulfation/sulfonylation and methylation patterns. The cell growth inhibitory effects of the compounds were tested against four cancerous human cell lines and two non-cancerous cell lines. Two d -glucuronate-containing tetra-O-sulfated, partially methylated trisaccharides displayed remarkable and selective inhibitory effects on the growth of ovary carcinoma (A2780) and melanoma (WM35) cells. Methyl substituents on the glucuronide unit proved to be detrimental, whereas acetyl substituents were beneficial to the cytostatic activity of the sulfated derivatives. 相似文献
2.
3.
4.
Csaba D Andrs Bla Simndi Ferenc
rsi Charalambos Lambrou Doukeni Missopolinou‐Tatala Costas Panayiotou Jnos Domokos Fruzsina Doleschall 《Journal of the science of food and agriculture》2005,85(8):1415-1419
Pilot‐scale supercritical fluid extraction of okra seeds was carried out, using carbon dioxide as solvent, at temperatures of 40, 50 and 60 °C and pressures of 150, 300 and 450 bar. Laboratory‐scale Soxhlet extraction of the ground seeds was carried out with ethanol and n‐hexane. The yields of supercritical fluid extraction and n‐hexane Soxhlet extractions were similar. The ethanol Soxhlet extraction gave the highest yield, but the concentrations of β‐sitosterol and tocopherols in this extract were lower than in the supercritical fluid extraction product. The fatty acid profiles of the extracts were determined, and a high unsaturated/saturated ratio was observed. The fatty acid compositions were only slightly different for oils obtained by the different extraction methods. Copyright © 2005 Society of Chemical Industry 相似文献
5.
Fruzsina Szab Jnos Daru Dniel Simk Tibor Zs. Nagy Andrs Stirling Zoltn Novk 《Advanced Synthesis \u0026amp; Catalysis》2013,355(4):685-691
Palladium‐catalyzed cross‐dehydrogenative coupling between anilides and aromatic aldehydes was achieved under aqueous conditions. A wide variety of the desired benzophenone derivatives was isolated in good to excellent yield. The reaction rate acceleration effect of acid and detergent has been demonstrated. Mechanistic insight has been obtained from quantum chemical calculations. 相似文献
6.
7.
Rent Kovcs Fruzsina Nagy Zoltn Tth Lajos Forgcs Lilina Tth Gyrgyi Vradi Gbor K. Tth Karina Vadszi Andrew M. Borman Lszl Majoros Lszl Galgczy 《International journal of molecular sciences》2021,22(2)
Candida auris is a potential multidrug-resistant pathogen able to persist on indwelling devices as a biofilm, which serve as a source of catheter-associated infections. Neosartorya fischeri antifungal protein 2 (NFAP2) is a cysteine-rich, cationic protein with potent anti-Candida activity. We studied the in vitro activity of NFAP2 alone and in combination with fluconazole, amphotericin B, anidulafungin, caspofungin, and micafungin against C. auris biofilms. The nature of interactions was assessed utilizing the fractional inhibitory concentration index (FICI), a Bliss independence model, and LIVE/DEAD viability assay. NFAP2 exerted synergy with all tested antifungals with FICIs ranging between 0.312–0.5, 0.155–0.5, 0.037–0.375, 0.064–0.375, and 0.064–0.375 for fluconazole, amphotericin B, anidulafungin, caspofungin, and micafungin, respectively. These results were confirmed using a Bliss model, where NFAP2 produced 17.54 μM2%, 2.16 μM2%, 33.31 μM2%, 10.72 μM2%, and 111.19 μM2% cumulative synergy log volume in combination with fluconazole, amphotericin B, anidulafungin, caspofungin, and micafungin, respectively. In addition, biofilms exposed to echinocandins (32 mg/L) showed significant cell death in the presence of NFAP2 (128 mg/L). Our study shows that NFAP2 displays strong potential as a novel antifungal compound in alternative therapies to combat C. auris biofilms. 相似文献
8.
9.
Dr. Jennifer A. Miles Dr. Fruzsina Hobor Dr. Chi H. Trinh James Taylor Dr. Christian Tiede Dr. Philip R. Rowell Dr. Brian R. Jackson Fatima A. Nadat Pallavi Ramsahye Dr. Hannah F. Kyle Dr. Basile I. M. Wicky Prof. Jane Clarke Dr. Darren C. Tomlinson Prof. Andrew J. Wilson Dr. Thomas A. Edwards 《Chembiochem : a European journal of chemical biology》2021,22(1):232-240
Abstract : The BCL-2 family is a challenging group of proteins to target selectively due to sequence and structural homologies across the family. Selective ligands for the BCL-2 family regulators of apoptosis are useful as probes to understand cell biology and apoptotic signalling pathways, and as starting points for inhibitor design. We have used phage display to isolate Affimer reagents (non-antibody-binding proteins based on a conserved scaffold) to identify ligands for MCL-1, BCL-xL, BCL-2, BAK and BAX, then used multiple biophysical characterisation methods to probe the interactions. We established that purified Affimers elicit selective recognition of their target BCL-2 protein. For anti-apoptotic targets BCL-xL and MCL-1, competitive inhibition of their canonical protein-protein interactions is demonstrated. Co-crystal structures reveal an unprecedented mode of molecular recognition; where a BH3 helix is normally bound, flexible loops from the Affimer dock into the BH3 binding cleft. Moreover, the Affimers induce a change in the target proteins towards a desirable drug-bound-like conformation. These proof-of-concept studies indicate that Affimers could be used as alternative templates to inspire the design of selective BCL-2 family modulators and more generally other protein-protein interaction inhibitors. 相似文献
10.
Dániel Cossuta Béla Simándi Judit Hohmann Fruzsina Doleschall Tibor Keve 《Journal of the science of food and agriculture》2007,87(13):2472-2481
BACKGROUND: The goal of this work was to utilize the sea buckthorn pomace, which is the by‐product of a sea buckthorn juice process. Pilot plant supercritical fluid extraction (SFE) experiments were performed in a 5 × 10?3 m3 volume high‐pressure vessel. The effects of pressure and temperature on extraction yield and recoveries of biologically active components were studied using a 32 full factorial design. The pressure and temperature were varied over the ranges of 30–46 MPa and 313–353 K, respectively. The extract samples were analysed by TLC‐densitometry, UV/VIS spectrofotometry and HPLC methods. RESULTS: The obtained yields changed between 142–164 g kg?1, according to the solvent power of the supercritical fluid. The recoveries of the different minor components were (g minor components kg?1 dried raw material): 2.50–4.25 sitosterol, 0.20–1.60 ursolic acid, 0.04–0.18 carotenoid, 0.35–0.42 total tocopherol. CONCLUSION: By evaluation the designed experiments 46 MPa and 333 K were chosen as the optimum conditions. Copyright © 2007 Society of Chemical Industry 相似文献