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Essential Oils in Cancer Therapy
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
Carmen Trummer, Gerhard Buchbauer
Nagappan et al. (2011) evaluated the antiproliferative effects of three carbazole alkaloids (mahanine, mahanimbicine, and mahanimbine) and the EO from the leaves of Murraya koenigii L. (Rutaceae) against human breast (MCF-7), human cervical (HeLa), and murine leukemia cell lines (P388). From the EO of M. koenigii, 34 aromatic volatile constituents were identified. The two sesquiterpene hydrocarbons, β-caryophyllene (19.5%) and α-humulene (15.2%), represented the main volatile metabolites. To evaluate the anticancer activity, cells were treated with all compounds and the EOs dissolved in DMSO to a concentration of 30 μg/mL. The carbazole alkaloids and the EOs exhibit antiproliferative effects against all three tested cell lines in a dose-dependent manner: the higher the concentration of the tested compound, the lower the cell viability. Mahanimbine showed the most significant cytotoxic effects with IC50 values of 2.12, 5.00, and 1.98 μg/mL in the MCF-7, P388, and HeLa cell lines, respectively. These results could be important for the development of a new antitumor lead metabolite.
Biochemical Basis of Cervical Maturation
Published in Gabor Huszar, The Physiology and Biochemistry of the Uterus in Pregnancy and Labor, 2020
Kitamura et al.64 carefully analyzed human cervical glycosaminoglycan composition by a complex method in which glycosaminoglycans isolated by proteolytic digestion were first separated by ion exchange chromatography, then identified by two-dimensional electrophoresis and subjected to serial enzymatic and chemical degradation. The degradation products were separated by paper chromatography and quantitated by the carbazole reaction. The percentage of total glycosaminoglycan represented by hyaluronic acid increased 45% and the percentage that was heparan sulfate rose threefold, while the part that was dermatan sulfate and chondroitin 4-sulfate fell 45%.
Lectin
Published in Masahiko Mori, Histochemistry of the Salivary Glands, 2019
Treat sections with peroxidase conjugated swine antirabbit IgG (1:50) for 30 min. H2O2 and 3-amino-9-ethyl carbazole as a coupler were used. Alkaline phosphatase conjugated antibody to rabbit IgG (1:50) for 30 min and Naphthol AS-TR phosphate and Fast Red TR as a coupler were used. In case fluorescein antibody was used, examine sections with fluorescence microscopy promptly.
Design, synthesis, and biological evaluation of novel carbazole derivatives as potent DNMT1 inhibitors with reasonable PK properties
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Ennian Li, Kai Wang, Bei Zhang, Siqi Guo, Senhao Xiao, Qi Pan, Xiaowan Wang, Weiying Chen, Yunshan Wu, Hesong Xu, Xiangqian Kong, Cheng Luo, Shijie Chen, Bo Liu
In summary, a series of novel carbazole-based derivatives were designed, synthesised, and evaluated for their biological activity. The structure-activity relationship of their anti-proliferative activity was explored. Among these compounds, WK-22 and WK-23 displayed appreciable human DNMT1 inhibitory activity in the micromolar range (IC50 = 4.9 µM and 5.0 µM). Simultaneously, both WK-22 and WK-23 has promising anti-proliferative effect on A549 and HCT116 cell lines. In further in vivo pharmacokinetic study, WK-23 displayed a better plasma exposure and prolonged elimination half-life (T1/2 = 7.9 h), especially the more acceptable oral bioavailability of (F% = 37.1) than WK-22 (F% = 27.0). Concomitantly, the molecule docking showed the binding pattern of WK-23 with DNMT1 is similar to that of DC_517, forming stable binding to DNMT1.
Synthetic cannabinoid receptor agonists: classification and nomenclature
Published in Clinical Toxicology, 2020
A. J. Potts, C. Cano, S. H. L. Thomas, S. L. Hill
To our knowledge the expanded possible analogues of MDMB-CHMCZCA have not yet emerged on the recreational market (e.g. AB-CHMCZCA, etc), however the development of MDMB-CHMCZCA is a logical response to the progressive legislative changes throughout the UK and wider EU that have restricted bicyclic indole and indazole core compounds [3, 25]. Additionally, the recent emergence of several tricyclic γ-carbolinone (i.e. dihydro-1H-pyrido[4,3-b]indol-1-one)-derived compounds also highlight the shifting clandestine synthesis of bicyclic to tricyclic cores. The systematic core letters “PEGACLONE” are derived from the chemical fragment “pentyl‐gamma‐carbolin‐1‐one” [57]. Compounds (or their metabolites) including CUMYL-PeGaClone (also known as SGT-151) and 5 F-CUMYL-PeGaClone (5 F-SGT-151) have been detected in urine samples of recreational users [57–59] and reported to the EMCDDA [60]. Future work should establish basic pharmacological and toxicological data for potential analogue compounds of carbazole and γ-carbolinone, preferably before they are identified on the recreational market.
Have molecular hybrids delivered effective anti-cancer treatments and what should future drug discovery focus on?
Published in Expert Opinion on Drug Discovery, 2021
Carbazole is the pivotal structural motif of many biologically active compounds of both natural and synthetic origin. The compounds containing parent or derivatized carbazole, possess anti-cancer, anti-bacterial, anti-fungal, anti-inflammatory, anti-HIV, anti-protozoan anti-convulsant, anti-psychotic, and anti-diabetic properties [32]. Ellipticine and Celiptium are the initial carbazole derivatives which target cytochrome P450 and topoisomerase II, respectively, and used for treating metastatic breast cancer [33]. Inspired by their activities, the exploration of carbazole core in synthesis of new molecular frameworks has led to identification of a number of active anti-tumor hybrids.