Plasma membrane imaging with a fluorescent benzothiadiazole derivative

• Pedro H. P. R. Carvalho,
• Jose R. Correa,
• Karen L. R. Paiva,
• Daniel F. S. Machado,
• Jackson D. Scholten and
• Brenno A. D. Neto

Beilstein J. Org. Chem. 2019, 15, 2644–2654, doi:10.3762/bjoc.15.257

• signal has then contributed to the image formation. Finally, the developed fluorophore was tested in additional cell lines to show its efficiency. A2780 (human ovarian carcinoma) cells, T47D (human breast tumor) cells and HUVEC (human umbilical vein endothelial) cells were tested and the results are

• umbilical vein endothelial cells, HUVEC. The cells were maintained according to ATCC (American type culture collection) recommendations at 37 °C in an atmosphere containing 5% CO2. Cell viability. For cell viability the synthesized compound BTD-4APTEG was tested at two different concentrations, 10 and 100

Drug targeting to decrease cardiotoxicity – determination of the cytotoxic effect of GnRH-based conjugates containing doxorubicin, daunorubicin and methotrexate on human cardiomyocytes and endothelial cells

• Livia Polgár,
• Eszter Lajkó,
• Pál Soós,
• Orsolya Láng,
• Marilena Manea,
• Béla Merkely,
• Gábor Mező and
• László Kőhidai

Beilstein J. Org. Chem. 2018, 14, 1583–1594, doi:10.3762/bjoc.14.136

• -conjugates containing doxorubicin, daunorubicin and methotrexate were investigated in this study. Their cytotoxicity was determined on primary human cardiac myocytes (HCM) and human umbilical vein endothelial cells (HUVEC) using the xCELLigence SP system, which measures impedance changes caused by adhering

• : cardiotoxicity; drug targeting; GnRH-conjugates; HCM; HUVEC; impedimetry; Introduction Gonadotropin-releasing hormone (GnRH) is a peptide hormone secreted by the hypothalamus, which stimulates the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary. Thus, it represents

• efficient conjugates but no further significant improvement was detected to the conjugate 5 with one Dau. Measurements on human endothelial cells (HUVEC) The effect of chemotherapeutic drugs (doxorubicin, daunorubicin, methotrexate) The effect of drugs used as chemotherapeutic agents was evaluated at seven

Use of costic acid, a natural extract from Dittrichia viscosa, for the control of Varroa destructor, a parasite of the European honey bee

• Kalliopi Sofou,
• Demosthenis Isaakidis,
• Apostolos Spyros,
• Anita Büttner,
• Athanassios Giannis and
• Haralambos E. Katerinopoulos

Beilstein J. Org. Chem. 2017, 13, 952–959, doi:10.3762/bjoc.13.96

• . Costic acid exhibited potent in vivo acaricidal activity against the parasite. Initial experiments showed that the compound is not toxic for human umbilical vein endothelial cells (HUVEC) at concentrations of up to 230 micromolar (μM), indicating that costic acid could be used as a safe, low-cost and

• treatment does not have a toxic effect on the host. The fact that the compound is also not toxic against human umbilical vein endothelial cells (HUVEC) indicates that it could be used as a safe, environment friendly, and low-cost efficient agent of controlling varroosis in Apis mellifera colonies

Interactions between cyclodextrins and cellular components: Towards greener medical applications?

• Loïc Leclercq

Beilstein J. Org. Chem. 2016, 12, 2644–2662, doi:10.3762/bjoc.12.261

• endothelial cells (HUVEC) [125]. The measurement of the residual cholesterol content of cells reveals that cholesterol was extracted in a dose dependent relationship. As expected, a correlation was obtained between the cytotoxicity and the affinity for cholesterol. The affinity of CDs for cholesterol was

Marine-derived myxobacteria of the suborder Nannocystineae: An underexplored source of structurally intriguing and biologically active metabolites

• Antonio Dávila-Céspedes,
• Peter Hufendiek,
• Max Crüsemann,
• Till F. Schäberle and
• Gabriele M. König

Beilstein J. Org. Chem. 2016, 12, 969–984, doi:10.3762/bjoc.12.96

• ), Candida albicans (DSM 1665) and Mucor hiemalis (DSM 2656, 33.3 μg mL−1 in each case). Significant cytotoxic activity was revealed for 22 towards SKOV-3 (IC50 = 2.4 μM), KB3-1 (IC50 = 5.3 μM), as well as A431 (IC50 = 8.45 μM), while 23 showed remarkable cytotoxicity against cell lines HUVEC and KB3-1 (IC50

Natural phenolic metabolites with anti-angiogenic properties – a review from the chemical point of view

• Qiu Sun,
• Jörg Heilmann and
• Burkhard König

Beilstein J. Org. Chem. 2015, 11, 249–264, doi:10.3762/bjoc.11.28

• enough to realistically speculate on the anti-angiogenic activity in vivo. As endothelial cells (ECs) have particular significance in angiogenesis, results from cellular assays using primary or immortalized ECs such as human umbilical vein endothelial cells (HUVEC) or human microvascular endothelial

• show in vitro anti-angiogenic activity with respect to Pazopanib in both HUVEC tube formation assay and the rat thoracic aorta ring test. They inhibited protein kinase B/Akt and ABL tyrosine kinase in the micromolar range. The preliminary structure–activity relationship is summarized in Figure 5. The

Synthesis of 5-(ethylsulfonyl)-2-methoxyaniline: An important pharmacological fragment of VEGFR2 and other inhibitors

• Miroslav Murár,
• Gabriela Addová and
• Andrej Boháč

Beilstein J. Org. Chem. 2013, 9, 173–179, doi:10.3762/bjoc.9.20

• determined enzymatic (IC50, VEGFR2) and cellular activities (IC50, hu-HUVEC/VEGF) were described. Among them N-(5-(ethylsulfonyl)-2-methoxyphenyl)-5-(3-(pyridin-2-yl)phenyl)oxazol-2-amine (AAZ) proved to be the most promising compound (IC50: 22 nM, VEGFR2) [4]. The binding mode of the AAZ ligand in the

An easily accessible sulfated saccharide mimetic inhibits in vitro human tumor cell adhesion and angiogenesis of vascular endothelial cells

• Grazia Marano,
• Claas Gronewold,
• Martin Frank,
• Anette Merling,
• Christian Kliem,
• Sandra Sauer,
• Manfred Wiessler,
• Eva Frei and
• Reinhard Schwartz-Albiez

Beilstein J. Org. Chem. 2012, 8, 787–803, doi:10.3762/bjoc.8.89

• cord vein endothelial cells (HUVEC) [19][43]. The influence of GSF on the adhesion of HBMEC-60 endothelial cells to ECM components was tested using plates coated with fibronectin, laminin or collagen. Addition of GSF to the cells in medium inhibited the adhesion of these cells to all three matrix

• matrigel assay, GSF also inhibited the sprouting of endothelial cells and their tubule formation in the long-term tube-formation assay of HUVEC cells cocultivated with fibroblasts in a dose-dependent manner (Figure 9B and Figure 9C). An inhibitory effect of GSF could be already observed at a concentration

Triterpenoid saponins from the roots of Acanthophyllum gypsophiloides Regel

• Elena A. Khatuntseva,
• Vladimir M. Men’shov,
• Alexander S. Shashkov,
• Yury E. Tsvetkov,
• Rodion N. Stepanenko,
• Raymonda Ya. Vlasenko,
• Elvira E. Shults,
• Genrikh A. Tolstikov,
• Tatjana G. Tolstikova,
• Dimitri S. Baev,
• Vasiliy A. Kaledin,
• Nelli A. Popova,
• Valeriy P. Nikolin,
• Pavel P. Laktionov,
• Anna V. Cherepanova,
• Tatiana V. Kulakovskaya,
• Ekaterina V. Kulakovskaya and
• Nikolay E. Nifantiev

Beilstein J. Org. Chem. 2012, 8, 763–775, doi:10.3762/bjoc.8.87

• 1 and 2 on the vessel endothelium was assessed via determination of interleukin-6 (IL-6) production in primary human umbilical vein endothelial cells (HUVEC). These cells were found to express various pattern-recognizing receptors (PRRs), including TLR4 [24], and can produce pro-inflammatory

• cytokines, including IL-6, IL-8 and IL-1β, upon stimulation with bacterial and viral components, such as lipopolysaccharides (LPS) and double-stranded RNA (dsRNA) [25]. HUVEC were cultivated in the presence of saponins 1 and 2 at nontoxic concentrations, i.e., 1 and 5 μg/mL, as determined by EZ4U test, and