A5048349899- Natural product bioactivities and synthesis
- Sesquiterpenes and Asteraceae Studies
- Plant Toxicity and Pharmacological Properties
- Research on Leishmaniasis Studies
- Phytochemistry and Biological Activities
- Plant-derived Lignans Synthesis and Bioactivity
- Trypanosoma species research and implications
- Traditional and Medicinal Uses of Annonaceae
- Phytochemical compounds biological activities
- Insect Pest Control Strategies
- Plant biochemistry and biosynthesis
- Pharmacological Effects of Medicinal Plants
- Herbal Medicine Research Studies
- Phytochemicals and Antioxidant Activities
- Allelopathy and phytotoxic interactions
- Microbial Natural Products and Biosynthesis
- X-ray Diffraction in Crystallography
- Bioactive Compounds and Antitumor Agents
- Magnolia and Illicium research
- Crystallization and Solubility Studies
- Malaria Research and Control
- Biochemical and Molecular Research
- Crystallography and molecular interactions
- Natural Antidiabetic Agents Studies
- Computational Drug Discovery Methods
University of Münster
2016-2025
Maastricht University
2025
Medizinische Hochschule Hannover
2025
Amyris (United States)
2020
University of Illinois Chicago
2018
Leiden University
2018
Collaborative Research Group
2018
University of Lübeck
2014
University Hospital Schleswig-Holstein
2014
Tshwane University of Technology
2012
ABSTRACT Trypanosomiasis and leishmaniasis are important parasitic diseases affecting millions of people in Africa, Asia, South America. In a previous study, we identified several flavonoid glycosides as antiprotozoal principles from Turkish plant. Here surveyed large set aglycones glycosides, well panel other related compounds phenolic phenylpropanoid nature, for their vitro activities against Trypanosoma brucei rhodesiense , cruzi Leishmania donovani . The cytotoxicities more than 100...
The sesquiterpene lactone helenalin is a potent anti-inflammatory drug whose molecular mechanism of action remains unclear despite numerous investigations. We have previously shown that and other lactones selectively inhibit activation the transcription factor NF-κB, central mediator human immune response. These drugs must target step in NF-κB pathway, since they induction by four different stimuli. It has been reported exert their effect inhibiting degradation IκB, inhibitory subunit NF-κB....
Sesquiterpene lactones (SLs) have potent anti-inflammatory properties. We shown previously that they exert this effect in part by inhibiting activation of the transcription factor NF-κB, a central regulator immune response. proposed molecular mechanism for inhibition based on computer modeling data. In model, SLs directly alkylate p65 subunit thereby DNA binding. Nevertheless, an experimental evidence was lacking. Moreover, experiments using SL parthenolide, alternative mode action has been...
Infections with protozoan parasites are a major cause of disease and mortality in many tropical countries the world. Diseases caused by species genera Trypanosoma (Human African Trypanosomiasis Chagas Disease) Leishmania (various forms Leishmaniasis) among seventeen "Neglected Tropical Diseases" (NTDs) defined as such WHO due to neglect financial investment into research development new drugs large part pharmaceutical industry public awareness high income countries. Another is malaria...
Article Helenalin, an Anti-Inflammatory Sesquiterpene Lactone from Arnica, Selectively Inhibits Transcription Factor NF-κB was published on September 1, 1997 in the journal Biological Chemistry (volume 378, issue 9).
Infections with protozoan parasites are a major cause of disease and mortality in many tropical countries the world. Diseases caused by species genera Trypanosoma (Human African Trypanosomiasis Chagas Disease) Leishmania (various forms Leishmaniasis) among seventeen "Neglected Tropical Diseases" (NTDs) defined WHO. Furthermore, malaria (caused various Plasmodium species) can be considered neglected certain regard to availability affordability antimalarials. Living organisms, especially...
Natural rubber is a biopolymer with exceptional qualities that cannot be completely replaced using synthetic alternatives. Although several key enzymes in the biosynthetic pathway have been isolated, mainly from plants such as Hevea brasiliensis, Ficus spec. and desert shrub Parthenium argentatum, there no planta functional studies, e.g. by RNA interference, due to absence of efficient reproducible protocols for genetic engineering. In contrast, Russian dandelion Taraxacum koksaghyz, which...
Prompted by results of our previous studies where we found high activity some sesquiterpene lactones (STLs) against Trypanosoma brucei rhodesiense (which causes East African sleeping sickness), have now conducted a structure-(in-vitro)-activity study on set 40 STLs T. rhodesiense, cruzi, Leishmania donovani and Plasmodium falciparum. Furthermore, cytotoxic L6 rat skeletal myoblast cells was assessed. Some the compounds possess activity, especially (e.g. helenalin its esters with IC50-values...
This study deals with the cytotoxicity of helenanolide-type (10α-methylpseudoguaianolide) sesquiterpene lactones. We determined influence substitution patterns on toxicity 21 helenanolides to a cloned Ehrlich ascites tumor cell line, EN2. Within series helenalin esters, acetate (2) and isobutyrate (3) were more toxic than itself (1). Esters larger acyl groups (tiglate 4 isovalerate 5) exhibited decreased compared parent alcohol Similar relationships observed between 6,8-diastereomer...
The anti-trypanosomal activity of six sesquiterpene lactones (helenalin, mexicanin I, 11α,13-dihydrohelenalin acetate, chamissonolide, ivalin and isoalantolactone) against the African Trypanosoma brucei rhodesiense American T. cruzi was investigated. All tested compounds were found active towards both parasites, former being generally more sensitive. Helenalin most compound in series with IC50 values 0.051 0.695 μM cruzi, respectively. low value for b. indicates that helenalin type may be...
In vitro screening of the dichloromethane extracts 16 Asteraceae species native to Sudan for activity against major protozoan pathogens revealed that a Xanthium brasilicum Vell. [syn. X. strumarium var. (Vell.) Baker in Mart.] extract was most active Trypanosoma brucei rhodesiense, etiological agent East African human trypanosomiasis (IC50 = 0.1 µg/mL). This plant also exhibited noticeable activities T. cruzi (Chagas disease), Leishmania donovani (Kala-Azar) as well Plasmodium falciparum...
Activation of the serine/threonine kinase Akt is associated with aggressive clinical behavior prostate cancer. We found that human cancer cell lines LNCaP and PC-3 express predominantly Akt1 Akt2. Selective down-regulation Akt1, but not Akt2, by short-hairpin RNA reduced viability cells. In addition, structurally different inhibitors were cytotoxic for cells, confirming pathway indispensable their viability. have purified tetracyclic triterpenoids 3-oxo-tirucallic acid,...
Various natural products with the chromane and chromene scaffold exhibit high antiprotozoal activity. The product encecalin (7) served as key intermediate for synthesis of different ethers 9, amides 11, amines 12. analogues 14 phenols 15 were obtained by reductive amination ketones 13 6, respectively. Angelate 3, 11 did not show considerable However, derived 12, 14, revealed promising activity represent novel lead compounds. Whereas benzylamine 12a α-methylbenzylamine 12g active against P....