TY - JOUR AU - Lorántfy, László AU - Rutterschmid, Dóra AU - Örkényi, Róbert Zoltán AU - Bakonyi, Dávid AU - Faragó, József AU - Dargó, Gergő AU - Könczöl, Árpád TI - Continuous Industrial-Scale Centrifugal Partition Chromatography with Automatic Solvent System Handling: Concept and Instrumentation JF - ORGANIC PROCESS RESEARCH & DEVELOPMENT J2 - ORG PROCESS RES DEV VL - 24 PY - 2020 IS - 11 SP - 2676 EP - 2688 PG - 13 SN - 1083-6160 DO - 10.1021/acs.oprd.0c00338 UR - https://m2.mtmt.hu/api/publication/31748109 ID - 31748109 LA - English DB - MTMT ER - TY - JOUR AU - Könczöl, Árpád AU - Dargó, Gergő TI - Brief overview of solubility methods: Recent trends in equilibrium solubility measurement and predictive models JF - DRUG DISCOVERY TODAY: TECHNOLOGIES J2 - DRUG DISCOVERY TODAY: TECHNOLOGIES VL - 27 PY - 2018 SP - 3 EP - 10 PG - 8 SN - 1740-6749 DO - 10.1016/j.ddtec.2018.06.001 UR - https://m2.mtmt.hu/api/publication/3399624 ID - 3399624 N1 - Cited By :7 Export Date: 8 September 2020 Correspondence Address: Könczöl, Á.; Compound Profiling Laboratory, Gedeon Richter Plc.Hungary; email: a.konczol@richter.hu Cited By :8 Export Date: 21 July 2021 Correspondence Address: Könczöl, Á.; Compound Profiling Laboratory, Hungary; email: a.konczol@richter.hu Cited By :8 Export Date: 14 August 2021 Correspondence Address: Könczöl, Á.; Compound Profiling Laboratory, Hungary; email: a.konczol@richter.hu LA - English DB - MTMT ER - TY - JOUR AU - Végh, Krisztina Emese AU - Riethmüller, Eszter AU - Levente, Hosszú AU - Darcsi, András AU - Judit, Müller AU - Alberti, Ágnes AU - Tóth, Anita AU - Béni, Szabolcs AU - Könczöl, Árpád AU - Balogh, György Tibor AU - Kéry, Ágnes TI - Three newly identified lipophilic flavonoids in Tanacetum parthenium supercritical fluid extract penetrating the Blood-Brain Barrier JF - JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS J2 - J PHARMACEUT BIOMED ANAL VL - 149 PY - 2018 SP - 488 EP - 493 PG - 6 SN - 0731-7085 DO - 10.1016/j.jpba.2017.11.029 UR - https://m2.mtmt.hu/api/publication/3293443 ID - 3293443 LA - English DB - MTMT ER - TY - JOUR AU - Ilkei, Viktor AU - Spaits, A AU - Prechl, A AU - Müller, Judit AU - Könczöl, Árpád AU - Lévai, S AU - Riethmüller, Eszter AU - Szigetvári, Á AU - Béni, Zoltán AU - Dékány, M AU - Martins, Ana AU - Hunyadi, Attila AU - Antus, Sándor AU - Szántay, Csaba (Ifj.) AU - Balogh, György Tibor AU - Kalaus, György AU - Bölcskei, Hedvig AU - Hazai, László TI - C8-selective biomimetic transformation of 5,7-dihydroxylated flavonoids by an acid-catalysed phenolic Mannich reaction: Synthesis of flavonoid alkaloids with quercetin and (–)-epicatechin skeletons JF - TETRAHEDRON J2 - TETRAHEDRON VL - 73 PY - 2017 IS - 11 SP - 1503 EP - 1510 PG - 8 SN - 0040-4020 DO - 10.1016/j.tet.2017.01.068 UR - https://m2.mtmt.hu/api/publication/3189432 ID - 3189432 N1 - Cited By :6 Export Date: 8 September 2020 CODEN: TETRA Correspondence Address: Ilkei, V.; Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Szt. Gellért tér 4, Hungary; email: vilkei@mail.bme.hu Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Szt. Gellért tér 4, Budapest, H-1111, Hungary Gedeon Richter Plc., Gyömrői út 19-21, Budapest, H-1103, Hungary Department of Medical Microbiology and Immunobiology, University of Szeged, Dóm tér 9, Szeged, H-6720, Hungary Institute of Pharmacognosy, Faculty of Pharmacy, University of Szeged, Eötvös utca 6, Szeged, H-6720, Hungary Department of Organic Chemistry, University of Debrecen, Egyetem tér 1, Debrecen, H-4032, Hungary Cited By :6 Export Date: 9 September 2020 CODEN: TETRA Correspondence Address: Ilkei, V.; Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Szt. Gellért tér 4, Hungary; email: vilkei@mail.bme.hu Chemicals/CAS: epicatechin, 490-46-0 LA - English DB - MTMT ER - TY - JOUR AU - Müller, Judit AU - Martins, Ana AU - Csábi, József AU - Fenyvesi, Ferenc AU - Könczöl, Árpád AU - Hunyadi, Attila AU - Balogh, György Tibor TI - BBB penetration-targeting physicochemical lead selection: Ecdysteroids as chemo-sensitizers against CNS tumors JF - EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES J2 - EUR J PHARM SCI VL - 96 PY - 2017 SP - 571 EP - 577 PG - 7 SN - 0928-0987 DO - 10.1016/j.ejps.2016.10.034 UR - https://m2.mtmt.hu/api/publication/3135904 ID - 3135904 N1 - Cited By :9 Export Date: 8 September 2020 CODEN: EPSCE Correspondence Address: Hunyadi, A.; Institute of Pharmacognosy, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, Hungary; email: hunyadi.a@pharm.u-szeged.hu AB - Abstract The anticancer potential of ecdysteroids, especially their chemo-sensitizing activity has recently gained a substantial scientific interest. A comprehensive physicochemical profiling was performed for a set of natural or semi-synthetic ecdysteroids (N = 37) to identify a lead compound against central nervous system (CNS) tumors. Calculated properties, such as lipophilicity (clogP), topological polar surface area (TPSA), brain-to-plasma ratio (clogBB) along with the measured blood-brain barrier specific in vitro permeability (logPe) were evaluated in parallel. Compounds with the highest CNS-availability predicted (clogBB > 0.0 and logPe > − 6.0) showed moderate to high lipophilicity (clogP = 3.89 − 5.25), relatively low TPSA (94.45 Å2), and shared a common apolar 2,3- and 20,22-diacetonide motif (25, 30–33). These ecdysteroids were selected for testing their capacity to sensitize SH-SY5Y neuroblastoma cells to vincristine. All of the five tested compounds exerted a remarkably strong, dose dependent chemo-sensitizing activity: at 2.5–10.0 μM ecdysteroids increased the cytotoxic activity of vincristine one to three orders of magnitude in (e.g., from IC50 = 39.5 ± 2.9 nM to as low as 0.056 ± 0.03 nM). Moreover, analysis of the combination index (CI) revealed outstanding synergism between ecdysteroids and vincristine (CI50 = 0.072 − 0.444). Thus, based on drug-likeness, physchem character and in vitro CNS activity, compound 25 was proposed as a lead for further in vivo studies. LA - English DB - MTMT ER - TY - JOUR AU - Ilkei, Viktor AU - Spaits, A AU - Prechl, A AU - Szigetvári, Á AU - Béni, Zoltán AU - Dékány, M AU - Szántay, Csaba (Ifj.) AU - Müller, Judit AU - Könczöl, Árpád AU - Szappanos, Ádám AU - Mándi, Attila AU - Antus, Sándor AU - Martins, Ana AU - Hunyadi, Attila AU - Balogh, György Tibor AU - Kalaus, György AU - Bölcskei, Hedvig AU - Hazai, László AU - Kurtán, Tibor TI - Biomimetic synthesis and HPLC–ECD analysis of the isomers of dracocephins A and B JF - BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY J2 - BEILSTEIN J ORG CHEM VL - 12 PY - 2016 SP - 2523 EP - 2534 PG - 12 SN - 1860-5397 DO - 10.3762/bjoc.12.247 UR - https://m2.mtmt.hu/api/publication/3143287 ID - 3143287 N1 - Funding Agency and Grant Number: OTKA/NKFIOrszagos Tudomanyos Kutatasi Alapprogramok (OTKA) [K-112951, K-105871, PD 121020] Funding text: The authors are grateful to Gedeon Richter Plc. for the financial support, and to Prof. Joseph Molnar (Department of Medical Microbiology and Immunobiology, University of Szeged, Szeged, Hungary) for generously providing cell lines for the bioassays. A. Szappanos, A. Mandi, S. Antus and T. Kurtan gratefully acknowledge the support provided by OTKA/NKFI (Grant Nos: K-112951, K-105871 and PD 121020) and the CPU time by the National Information Infrastructure Development Institute (NIIFI 10038). AB - Starting from racemic naringenin ((±)-1), a mixture of dracocephin A stereoisomers 6-(2”-pyrrolidinone-5”-yl)naringenin (±)-2a–d and its regioisomer, dracocephin B 8-(2”-pyrrolidinone-5”-yl)naringenin (±)-3a–d originally isolated from Dracocephalum rupestre, have been synthesized in a one-pot reaction. The separation of 2a–d and 3a–d was achieved by preparative HPLC. The four stereoisomers of each natural product were separated by analytical chiral HPLC and their absolute configuration was studied by the combination of HPLC–ECD measurements and TDDFT–ECD calculations. The synthesized flavonoid alkaloids were further characterized by physicochemical and in vitro pharmacological studies. LA - English DB - MTMT ER - TY - JOUR AU - Könczöl, Árpád AU - Rendes, Kata AU - Dékány, Miklós AU - Müller, Judit AU - Riethmüller, Eszter AU - Balogh, György Tibor TI - Blood-brain barrier specific permeability assay reveals N-methylated tyramine derivatives in standardised leaf extracts and herbal products of Ginkgo biloba JF - JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS J2 - J PHARMACEUT BIOMED ANAL VL - 131 PY - 2016 SP - 167 EP - 174 PG - 8 SN - 0731-7085 DO - 10.1016/j.jpba.2016.08.032 UR - https://m2.mtmt.hu/api/publication/3110098 ID - 3110098 N1 - WoS:hiba:000387628400023 2019-03-12 17:58 első szerző nem egyezik AB - Abstract The linkage between the central nervous system availability and neuropharmacological activity of the constituents of Ginkgo biloba L. extracts (GBE) is still incomplete. In this study, the in vitro blood-brain barrier (BBB) permeability profile of the standardised GBE was investigated by the parallel artificial membrane permeability assay (PAMPA). Biomarkers, such as terpene trilactones, flavonoid aglycones and ginkgotoxin exerted moderate or good BBB-permeability potential (BBB+), while glycosides and biflavones were predicted as unable to pass the BBB. N-methyltyramine (NMT) and N,N-dimethyltyramine or hordenine (Hor) were identified among BBB+ compounds, while subsequent direct HRMS analysis revealed tyramine (Tyr) and N,N,N-trimethyltyramine or candicine (Can) in GBE as trace constituents. Distribution of Tyr, NMT, Hor and Can was determined by a validated ion-exchange mechanism-based liquid chromatography–electrospray ionisation–mass spectrometry (LC-ESI–MS) method in G. biloba samples, such as herbal drugs and dietary supplements. The total content of the four tyramine derivatives in various GBEs ranged from 7.3 up to 6357 μg/g dry extract with NMT and Hor as most abundant ones. Considering the pharmacological activities and the revealed fluctuation in the concentration of the analysed adrenergic protoalkaloids, the presented rapid LC-ESI–MS method is proposed for monitoring of the levels of Tyr, NMT, Hor and Can in G. biloba products. LA - English DB - MTMT ER - TY - JOUR AU - Riethmüller, Eszter AU - Könczöl, Árpád AU - Bereczki-Szakál, Dorottya AU - Végh, Krisztina Emese AU - Balogh, György Tibor AU - Kéry, Ágnes TI - HPLC-DPPH Screening Method for Evaluation of Antioxidant Compounds in Corylus Species JF - NATURAL PRODUCT COMMUNICATIONS J2 - NAT PROD COMMUN VL - 11 PY - 2016 IS - 5 SP - 641 EP - 644 PG - 4 SN - 1934-578X DO - 10.1177/1934578x1601100522 UR - https://m2.mtmt.hu/api/publication/3065548 ID - 3065548 LA - English DB - MTMT ER - TY - JOUR AU - Hornok, Sándor AU - Kováts, Dávid AU - Flaisz, Barbara AU - Csörgő, Tibor AU - Könczöl, Árpád AU - Balogh, György Tibor AU - Csorba, Attila AU - Hunyadi, Attila TI - An unexpected advantage of insectivorism: insect moulting hormones ingested by song birds affect their ticks JF - SCIENTIFIC REPORTS J2 - SCI REP VL - 6 PY - 2016 PG - 8 SN - 2045-2322 DO - 10.1038/srep23390 UR - https://m2.mtmt.hu/api/publication/3030183 ID - 3030183 N1 - Department of Parasitology and Zoology, Faculty of Veterinary Science, Szent István University, Budapest, 1078, Hungary Department of Evolutionary Zoology and Human Biology, University of Debrecen, Debrecen, 4032, Hungary Ócsa Bird Ringing Station, Ócsa, 2364, Hungary Department of Anatomy, Cell-and Developmental Biology, Eötvös Loránt University, Budapest, 1117, Hungary Compound Profiling Laboratory, Gedeon Richter Plc., Budapest, 1103, Hungary Institute of Pharmacognosy, University of Szeged, Szeged, 6720, Hungary Cited By :13 Export Date: 15 November 2023 Correspondence Address: Hornok, S.; Department of Parasitology and Zoology, Hungary; email: Hornok.Sandor@aotk.szie.hu LA - English DB - MTMT ER - TY - CHAP AU - Maszler, P AU - Kupai, József AU - Balogh, György Tibor AU - Könczöl, Árpád ED - Bohner, Bíborka ED - Mesterházy, Edit TI - N,N-Dimetilanilin β-Deutérium izotópeffektusának mechanisztikus vizsgálata fordított fázisú folyadékkromatográfiával T2 - XXXVIII. Kémiai Előadói Napok PB - Magyar Kémikusok Egyesülete (MKE) CY - Szeged SN - 9789639970649 PY - 2015 SP - 34 EP - 38 PG - 5 UR - https://m2.mtmt.hu/api/publication/3038549 ID - 3038549 LA - Hungarian DB - MTMT ER -