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Book: Insulindetemir

Liebl, Andreas / Kaiser, Marcel / Lüddeke, Hans-Joachim

Insulintherapie bei Typ-2-Diabetikern frühzeitig einsetzen

(Thieme case report ; 2,7)

2010

Author's details	[Hrsg. und Autoren: Andreas Liebl (Hrsg.) ; Marcel Kaiser ; Hans-Joachim Lüddeke]
Series title	Thieme case report ; 2,7
Collection
Language	German
Size	11 S. : Ill., graph. Darst.
Publisher	Thieme
Publishing place	Stuttgart u.a.
Publishing country	Germany
Document type	Book
HBZ-ID	HT016643849
Database	Catalogue ZB MED Medicine, Health

In stock of ZB MED Cologne/Königswinter

Shelf mark	Loan status	Location
Zs A 6843 -2,7-	verfügbar in Königswinter	Königswinter

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Article: Fexinidazole for Human African Trypanosomiasis, the Fruit of a Successful Public-Private Partnership.

Bernhard, Sonja / Kaiser, Marcel / Burri, Christian / Mäser, Pascal

Diseases (Basel, Switzerland)

2022 Volume 10, Issue 4

Abstract: After 100 years of chemotherapy with impractical and toxic drugs, an oral cure for human African trypanosomiasis (HAT) is available: Fexinidazole. In this case, we review the history of drug discovery for HAT with special emphasis on the discovery, pre- ... ...

Abstract	After 100 years of chemotherapy with impractical and toxic drugs, an oral cure for human African trypanosomiasis (HAT) is available: Fexinidazole. In this case, we review the history of drug discovery for HAT with special emphasis on the discovery, pre-clinical development, and operational challenges of the clinical trials of fexinidazole. The screening of the Drugs for Neglected Diseases initiative (DNDi) HAT-library by the Swiss TPH had singled out fexinidazole, originally developed by Hoechst (now Sanofi), as the most promising of a series of over 800 nitroimidazoles and related molecules. In cell culture, fexinidazole has an IC
Language	English
Publishing date	2022-10-17
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2720869-2
ISSN	2079-9721
ISSN	2079-9721
DOI	10.3390/diseases10040090
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: In vitro antiplasmodial activity and cytotoxicity of extracts and chromatographic fractions of twigs from Pappea capensis EckI & Zeyh. (Sapindaceae).

Mabuza, J Mcebisi / Kaiser, Marcel / Bapela, M Johanna

Journal of ethnopharmacology

2022 Volume 298, Page(s) 115659

Abstract: Ethnopharmacological relevance: The Vha-Venda people of South Africa use Pappea capensis EckI & Zeyh. (Sapindaceae) twigs to treat malaria and its related symptoms.: Aim of study: The main aim of this study was to evaluate the antiplasmodial and ... ...

Abstract	Ethnopharmacological relevance: The Vha-Venda people of South Africa use Pappea capensis EckI & Zeyh. (Sapindaceae) twigs to treat malaria and its related symptoms. Aim of study: The main aim of this study was to evaluate the antiplasmodial and cytotoxic activity of P. capensis extracts and chromatographic fractions. Spectroscopy analysis was conducted using Materials and methods: Pappea capensis twigs were dried and then ground to fine powder. A solvent mixture of dichloromethane: methanol: water (1:0.5:0.5, v/v) was used to extract. The polar extract was separated from the non-polar. The organic extract was dried to yield a DCM (I = 60 g) extract. The methanol in the aqueous extract was evaporated using a rotary vapour and the remaining water freeze dried to yield a water extract (II = 287 g). Extract I was further partitioned using a solvent mixture of DCM: MeOH (1:1, v/v), separated and concentrated under vacuum to yield dichloromethane (III = 40 g) and methanol (IV = 15 g) extracts. A water-based decoction (V = 10 g) was also prepared to establish the clinical relevance of the preparation administered by Vha-Venda people in South Africa. Extracts II, III and IV were further subjected to silica column chromatography, eluting with a series of different solvents with increasing polarity to yield a total of 25 fractions (A - Y). In vitro antiplasmodial tests on Plasmodium falciparum (NF54) and cytotoxicity screens on mammalian L-6 rat skeletal myoblast cells were performed on all extracts and fractions. Selectivity indices (SI) were also computed for all tested extracts and fractions which were further subjected to Results: From the assayed extracts, only extract I (IC Conclusion: The study validates the ethnomedicinal use of P. capensis for malaria treatment. It demonstrated the potential of discovering novel antiplasmodial constituents that could serve as drug hits through dereplication approaches where known compounds with established antimalarial activity can be bypassed to focus on the unknown.
MeSH term(s)	Animals ; Antimalarials/therapeutic use ; Apiaceae ; Chromatography ; Humans ; Malaria/drug therapy ; Mammals ; Methanol/therapeutic use ; Methylene Chloride ; Plant Extracts/therapeutic use ; Plasmodium falciparum ; Rats ; Sapindaceae ; Solvents
Chemical Substances	Antimalarials ; Plant Extracts ; Solvents ; Methylene Chloride (588X2YUY0A) ; Methanol (Y4S76JWI15)
Language	English
Publishing date	2022-08-28
Publishing country	Ireland
Document type	Journal Article
ZDB-ID	134511-4
ISSN	1872-7573 ; 0378-8741
ISSN (online)	1872-7573
ISSN	0378-8741
DOI	10.1016/j.jep.2022.115659
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Article: In vitro antiplasmodial activity and cytotoxicity of extracts and chromatographic fractions of twigs from Pappea capensis EckI & Zeyh. (Sapindaceae)

Mabuza, J. Mcebisi / Kaiser, Marcel / Bapela, M. Johanna

Journal of ethnopharmacology. 2022 Aug. 16,

2022

Abstract: The Vha-Venda people of South Africa use Pappea capensis EckI & Zeyh. (Sapindaceae) twigs to treat malaria and its related symptoms. The main aim of this study was to evaluate the antiplasmodial and cytotoxic activity of P. capensis extracts and ... ...

Abstract	The Vha-Venda people of South Africa use Pappea capensis EckI & Zeyh. (Sapindaceae) twigs to treat malaria and its related symptoms. The main aim of this study was to evaluate the antiplasmodial and cytotoxic activity of P. capensis extracts and chromatographic fractions. Spectroscopy analysis was conducted using ¹H NMR and GC-MS to tentatively identify the major classes of compounds and phytoconstituents that can be attributed to the observed antiplasmodial bioactivity. Pappea capensis twigs were dried and then ground to fine powder. A solvent mixture of dichloromethane: methanol: water (1:0.5:0.5, v/v) was used to extract. The polar extract was separated from the non-polar. The organic extract was dried under to yield a DCM (I = 60 g). The methanol in the aqueous extract was evaporated using a rotary vapour and the remaining water freeze dried to yield a water extract (II = 287 g). Extract I was further partitioned using a solvent mixture of DCM: MeOH (1:1, v/v), separated and concentrated under vacuum to yield dichloromethane (III = 40 g) and methanol (IV = 15 g) extracts. A water-based decoction (V = 10 g) was also prepared to establish the clinical relevance of the preparation administered by Vha-Venda people in South Africa. Extracts II, III and IV were further subjected to silica column chromatography, eluting with a series of different solvents with increasing polarity to yield a total of 25 fractions (A – Y). In vitro antiplasmodial tests on Plasmodium falciparum (NF54) and cytotoxicity screens on mammalian L-6 rat skeletal myoblast cells were performed on all extracts and fractions. Selectivity indices (SI) were also computed for all tested extracts and fractions which were further subjected to ¹H NMR spectroscopy and GC-MS analysis for the identification of the major classes of compounds present in the extracts. From the assayed extracts, only extract I (IC₅₀ = 2.93 μg/ml; SI = 14), III (IC₅₀ = 2.59 μg/ml; SI = 21) and IV (IC₅₀ = 3.56 μg/ml; SI = 13) demonstrated the best antiplasmodial activity and selectivity. Of all assayed fractions, only N (0.6 μg/ml; SI = 91), D (0.85 μg/ml; SI = 37) and E (0.91 μg/ml; SI = 30) depicted the best antiplasmodial activity and selectivity. The ¹H NMR analysis of the extracts and fractions identified the prominent class of constituents to be aliphatic based which was tentatively identified as terpenoids. When further GC-MS analysis was conducted, the presence of lupin-3-one, lupeol acetate, α-amyrin, and β-amyrin phytoconstituents were tentatively confirmed. These constituents are triterpenoids with established antiplasmodial activity which can be tentatively attributed to the bioactivity observed in P. capensis twigs. The study validates the ethnomedicinal use of P. capensis for malaria treatment. It demonstrated the potential of discovering novel antiplasmodial constituents that could serve as drug hits through dereplication approaches where known compounds with established antimalarial activity can be bypassed to focus on the unknown.
Keywords	Plasmodium falciparum ; Sapindaceae ; acetates ; antimalarials ; antiplasmodial properties ; chemical constituents of plants ; cytotoxicity ; gel chromatography ; lupeol ; malaria ; methanol ; methylene chloride ; myoblasts ; nuclear magnetic resonance spectroscopy ; people ; rats ; solvents ; traditional medicine ; vapors ; South Africa
Language	English
Dates of publication	2022-0816
Publishing place	Elsevier B.V.
Document type	Article
Note	Pre-press version
ZDB-ID	134511-4
ISSN	1872-7573 ; 0378-8741
ISSN (online)	1872-7573
ISSN	0378-8741
DOI	10.1016/j.jep.2022.115659
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: In Vitro Drug Efficacy Testing Against Trypanosoma brucei.

Kaiser, Marcel / Mäser, Pascal

Methods in molecular biology (Clifton, N.J.)

2020 Volume 2116, Page(s) 781–789

Abstract: The recent endorsement of fexinidazole by the European Medicines Agency for the treatment of human African trypanosomiasis has demonstrated the high predictive value of cell-based assays for parasite chemotherapy. Here we describe three in vitro drug ... ...

Abstract	The recent endorsement of fexinidazole by the European Medicines Agency for the treatment of human African trypanosomiasis has demonstrated the high predictive value of cell-based assays for parasite chemotherapy. Here we describe three in vitro drug susceptibility tests with Trypanosoma brucei that have served as the basis for the identification of fexinidazole as a promising lead: (1) a standard assay with end-point measurement to determine drug efficacy; (2) a wash-out assay to test for reversibility and speed of drug action; (3) isothermal microcalorimetry for real-time measurement of onset of drug action and time to kill. Together, these assays allow to estimate pharmacodynamic parameters in vitro and to devise appropriate treatment regimens for subsequent in vivo experiments.
MeSH term(s)	Calorimetry/methods ; Drug Evaluation, Preclinical/methods ; Humans ; Life Cycle Stages/drug effects ; Nitroimidazoles/pharmacology ; Nitroimidazoles/therapeutic use ; Parasitic Sensitivity Tests/methods ; Trypanocidal Agents/pharmacology ; Trypanocidal Agents/therapeutic use ; Trypanosoma/drug effects ; Trypanosoma/physiology ; Trypanosomiasis, African/blood ; Trypanosomiasis, African/drug therapy ; Trypanosomiasis, African/parasitology
Chemical Substances	Nitroimidazoles ; Trypanocidal Agents ; fexinidazole (306ERL82IR)
Language	English
Publishing date	2020-03-27
Publishing country	United States
Document type	Journal Article
ISSN	1940-6029
ISSN (online)	1940-6029
DOI	10.1007/978-1-0716-0294-2_46
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Induced pluripotent stem cell-derived human macrophages as an infection model for Leishmania donovani.

Baert, Lore / Rudy, Serena / Pellisson, Mélanie / Doll, Thierry / Rocchetti, Romina / Kaiser, Marcel / Mäser, Pascal / Müller, Matthias

PLoS neglected tropical diseases

2024 Volume 18, Issue 1, Page(s) e0011559

Abstract: The parasite Leishmania donovani is one of the species causing visceral leishmaniasis in humans, a deadly infection claiming up to 40,000 lives each year. The current drugs for leishmaniasis treatment have severe drawbacks and there is an urgent need to ... ...

Abstract	The parasite Leishmania donovani is one of the species causing visceral leishmaniasis in humans, a deadly infection claiming up to 40,000 lives each year. The current drugs for leishmaniasis treatment have severe drawbacks and there is an urgent need to find new anti-leishmanial compounds. However, the search for drug candidates is complicated by the intracellular lifestyle of Leishmania. Here, we investigate the use of human induced pluripotent stem cell (iPS)-derived macrophages (iMACs) as host cells for L. donovani. iMACs obtained through embryoid body differentiation were infected with L. donovani promastigotes, and high-content imaging techniques were used to optimize the iMACs seeding density and multiplicity of infection, allowing us to reach infection rates up to 70% five days after infection. IC50 values obtained for miltefosine and amphotericin B using the infected iMACs or mouse peritoneal macrophages as host cells were comparable and in agreement with the literature, showing the potential of iMACs as an infection model for drug screening.
MeSH term(s)	Animals ; Humans ; Mice ; Antiprotozoal Agents/pharmacology ; Antiprotozoal Agents/therapeutic use ; Induced Pluripotent Stem Cells ; Leishmania donovani ; Leishmaniasis, Visceral/parasitology ; Macrophages/parasitology
Chemical Substances	Antiprotozoal Agents
Language	English
Publishing date	2024-01-02
Publishing country	United States
Document type	Journal Article
ZDB-ID	2429704-5
ISSN	1935-2735 ; 1935-2735
ISSN (online)	1935-2735
ISSN	1935-2735
DOI	10.1371/journal.pntd.0011559
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: New myxobacteria of the

Walesch, Sebastian / Garcia, Ronald / Mahmoud, Abdelhalim B / Panter, Fabian / Bollenbach, Sophie / Mäser, Pascal / Kaiser, Marcel / Krug, Daniel / Müller, Rolf

Microbiology spectrum

2024 Volume 12, Issue 3, Page(s) e0368923

Abstract: In the past century, microbial natural products have proven themselves to be substantial and fruitful sources of anti-infectives. In addition to the well-studied Actinobacteria, understudied bacterial taxa like the Gram-negative myxobacteria have ... ...

Abstract	In the past century, microbial natural products have proven themselves to be substantial and fruitful sources of anti-infectives. In addition to the well-studied Actinobacteria, understudied bacterial taxa like the Gram-negative myxobacteria have increasingly gained attention in the ongoing search for novel and biologically active natural products. In the course of a regional sampling campaign to source novel myxobacteria, we recently uncovered new myxobacterial strains MCy12716 and MCy12733 belonging to the
MeSH term(s)	Humans ; Myxococcales/genetics ; Antiparasitic Agents/pharmacology ; Pandemics ; Malaria, Falciparum ; Plasmodium falciparum ; Biological Products/pharmacology
Chemical Substances	Antiparasitic Agents ; Biological Products
Language	English
Publishing date	2024-02-01
Publishing country	United States
Document type	Journal Article
ZDB-ID	2807133-5
ISSN	2165-0497 ; 2165-0497
ISSN (online)	2165-0497
ISSN	2165-0497
DOI	10.1128/spectrum.03689-23
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Article: Trypanosoma cruzi

Fesser, Anna / Beilstein, Sabina / Kaiser, Marcel / Schmidt, Remo S / Mäser, Pascal

Pathogens (Basel, Switzerland)

2023 Volume 12, Issue 10

Abstract: Since the first published genome sequence ... ...

Abstract	Since the first published genome sequence of
Language	English
Publishing date	2023-10-04
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2695572-6
ISSN	2076-0817
ISSN	2076-0817
DOI	10.3390/pathogens12101217
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: [No title information]

Fesser, Anna / Kaiser, Marcel / Mäser, Pascal

Biospektrum : Zeitschrift der Gesellschaft fur Biologishe Chemie (GBCH) und der Vereinigung fur Allgemeine und Angewandte Mikrobiologie (VAAM)

2021 Volume 27, Issue 2, Page(s) 168–170

Abstract: Chagas disease is a zoonosis caused ... ...

Title translation	Neue Parameter für die Wirkstofftestung gegen
Abstract	Chagas disease is a zoonosis caused by
Language	German
Publishing date	2021-03-23
Publishing country	Germany
Document type	English Abstract ; Journal Article ; Review
ZDB-ID	2203536-9
ISSN	1868-6249 ; 0947-0867
ISSN (online)	1868-6249
ISSN	0947-0867
DOI	10.1007/s12268-021-1554-z
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Article ; Online: Incidence of antiepileptic drug therapy and factors associated with their prescribing in outpatients with diabetic polyneuropathy.

Jacob, Louis / Kaiser, Marcel / Kostev, Karel

Primary care diabetes

2021 Volume 15, Issue 3, Page(s) 535–540

Abstract: Aims: The goal of this retrospective cohort study was to analyze the incidence of, and factors associated with the antiepileptic drug (AED) therapy in the five years following the diagnosis of diabetic polyneuropathy in patients followed in Germany.: ... ...

Abstract	Aims: The goal of this retrospective cohort study was to analyze the incidence of, and factors associated with the antiepileptic drug (AED) therapy in the five years following the diagnosis of diabetic polyneuropathy in patients followed in Germany. Methods: The study included patients aged 18-80 years with an initial diagnosis of diabetic polyneuropathy in 1238 general and diabetologist practices in Germany between January 2008 and December 2017 (index date). The main outcome of the study was the incidence of the AED therapy in the five years following the diagnosis of diabetic polyneuropathy. Adjusted Cox regression analyses were conducted to investigate the association between study covariates and the incidence of the AED therapy. Results: The present study included 48,324 patients (mean [standard deviation] age 65.8 [10.6] years, 55.6% male). Within five years of the diagnosis of diabetic polyneuropathy, 16.4% of patients were prescribed at least one AED. The three most frequent drugs were pregabalin, gabapentin, and carbamazepine. Female sex (HR = 1.22), private health insurance coverage (HR = 1.22), follow-up in a general practice (HR = 1.85), HbA1c ≥10% (HR = 1.36), previous referral to a neurological practice (HR = 1.47), previous hospital admission (HR = 1.51) and depression (HR = 1.15) were positively associated with the incidence of the AED therapy. Conclusions: The incidence of the AED therapy was low in patients recently diagnosed with diabetic polyneuropathy in Germany. More research is warranted to understand the infrequent use of AEDs in diabetic polyneuropathy patients from this country.
MeSH term(s)	Aged ; Anticonvulsants/adverse effects ; Diabetes Mellitus/drug therapy ; Diabetic Neuropathies/diagnosis ; Diabetic Neuropathies/drug therapy ; Diabetic Neuropathies/epidemiology ; Epilepsy/drug therapy ; Female ; Humans ; Incidence ; Male ; Outpatients ; Retrospective Studies
Chemical Substances	Anticonvulsants
Language	English
Publishing date	2021-01-07
Publishing country	England
Document type	Journal Article
ZDB-ID	2273997-X
ISSN	1878-0210 ; 1751-9918
ISSN (online)	1878-0210
ISSN	1751-9918
DOI	10.1016/j.pcd.2020.12.005
Database	MEDical Literature Analysis and Retrieval System OnLINE

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