Search results for " Antitumor"
showing 10 items of 416 documents
Two new sesquiterpene derivatives from the Tunisian endemic Ferula tunetana Pom.
2010
A new sesquiterpene ester, tunetanin A (1), a new sesquiterpene coumarin, tunetacoumarin A (2), together with eight known compounds, i.e., coladin (3), coladonin (4), isosmarcandin (5), 13-hydroxyfeselol (6), umbelliprenin (7) propiophenone (8), beta-sitosterol (9), and stigmasterol (10), were isolated from the roots of Ferula tunetana. Their structures were elucidated on the basis of extensive spectroscopic methods, including 1D- and 2D-NMR experiments and MS analysis, as well as by comparison with published data. The cytotoxicity of compounds 1-7 towards two human colon cancer cell lines, HT-29 and HCT 116, was evaluated. Compounds 3, 4, and 6 showed weak cytotoxic activities.
Unprecedented new nonadecylpara-hydroperoxycinnamate isolated fromErythrina excelsaand its cytotoxic activity
2014
A new unprecedented cinnamate derivative (1) was obtained from Erythrina excelsa (Leguminosae) and identified as nonadecyl para-hydroperoxycinnamate. This compound was isolated together with three known compounds, namely lupeol (2), mixture of sitosterol and stigmasterol (3), and isoneorautenol (4). Their structures were established on the basis of NMR and mass spectroscopic data in conjunction with those reported in the literature. Compound 1 was evaluated for its capability of inhibiting cancer cell lines and growth of a panel of microbial strains. It turned out that 1 is moderately to significantly cytotoxic against six cancer cell lines and shows weak to no antimicrobial activity.
Triterpene Saponins from Tupidanthus calyptratus
2001
Five new bisdesmosidic saponins (1--5) were isolated from the aerial parts of Tupidanthus calyptratus. Their structures were determined by (1)H--(1)H correlation spectroscopy (COSY, TOCSY, ROESY) and (1)H--(13)C correlation (HSQC, HMBC) NMR experiments, FABMS, and chemical data.
Bidentatoside I, a New Triterpene Saponin from Achyranthes bidentata
2001
Bidentatoside I (1) is a new triterpene saponin bearing an unusual dioxopropionic acid unit, isolated from the roots of Achyranthes bidentata. Structural elucidation was performed mainly by chemical and homo- and heteronuclear 2D NMR techniques. This compound did not show any potentiation of the in vitro cytotoxicity of cisplatin in the HT 29 human colon cancer cell line.
Cytotoxic steroidal glycosides from Allium flavum.
2014
Abstract Three new spirostane-type glycosides ( 1 – 3 ) were isolated from the whole plant of Allium flavum . Their structures were elucidated mainly by 2D NMR spectroscopic analysis and mass spectrometry as (20 S ,25 R )-2α-hydroxyspirost-5-en-3β-yl O -β- d -xylopyranosyl-(1 → 3)-[β- d -galactopyranosyl-(1→2)]-β- d -galactopyranosyl-(1→4)-β- d -galactopyranoside ( 1 ), (20 S ,25 R )-2α-hydroxyspirost-5-en-3β-yl O -β- d -xylopyranosyl-(1 → 3)-[β- d -glucopyranosyl-(1→2)]-β- d -galactopyranosyl-(1→4)-β- d -galactopyranoside ( 2 ), and (20 S ,25 R )-spirost-5-en-3β-yl O -α- l -rhamnopyranosyl-(1 → 4)-[β- d -glucopyranosyl-(1→2)]-β- d -glucopyranoside ( 3 ). The three saponins were evaluated f…
Deletion of 11q in Neuroblastomas Drives Sensitivity to PARP Inhibition
2017
AbstractPurpose: Despite advances in multimodal therapy, neuroblastomas with hemizygous deletion in chromosome 11q (20%–30%) undergo consecutive recurrences with poor outcome. We hypothesized that patients with 11q-loss may share a druggable molecular target(s) that can be exploited for a precision medicine strategy to improve treatment outcome.Experimental Design: SNP arrays were combined with next-generation sequencing (NGS) to precisely define the deleted region in 17 primary 11q-loss neuroblastomas and identify allelic variants in genes relevant for neuroblastoma etiology. We assessed PARP inhibitor olaparib in combination with other chemotherapy medications using both in vitro and in v…
The STAT3 Inhibitor Galiellalactone Reduces IL6-Mediated AR Activity in Benign and Malignant Prostate Models
2018
IL6/STAT3 signaling is associated with endocrine therapy resistance in prostate cancer, but therapies targeting this pathway in prostate cancer were unsuccessful in clinical trials so far. The mechanistic explanation for this phenomenon is currently unclear; however, IL6 has pleiotropic effects on a number of signaling pathways, including the androgen receptor (AR). Therefore, we investigated IL6-mediated AR activation in prostate cancer cell lines and ex vivo primary prostate tissue cultures in order to gain a better understanding on how to inhibit this process for future clinical trials. IL6 significantly increased androgen-dependent AR activity in LNCaP cells but importantly did not infl…
Dual disruption of aldehyde dehydrogenases 1 and 3 promotes functional changes in the glutathione redox system and enhances chemosensitivity in nonsm…
2020
AbstractAldehyde dehydrogenases (ALDHs) are multifunctional enzymes that oxidize diverse endogenous and exogenous aldehydes. We conducted a meta-analysis based on The Cancer Genome Atlas and Gene Expression Omnibus data and detected genetic alterations in ALDH1A1, ALDH1A3, or ALDH3A1, 86% of which were gene amplification or mRNA upregulation, in 31% of nonsmall cell lung cancers (NSCLCs). The expression of these isoenzymes impacted chemoresistance and shortened survival times in patients. We hypothesized that these enzymes provide an oxidative advantage for the persistence of NSCLC. To test this hypothesis, we used genetic and pharmacological approaches with DIMATE, an irreversible inhibito…
Functional Activation of Osteoclast Commitment in Chronic Lymphocytic Leukaemia: A Possible Role for RANK/RANKL Pathway
2017
AbstractSkeletal erosion has been found to represent an independent prognostic indicator in patients with advanced stages of chronic lymphocytic leukaemia (CLL). Whether this phenomenon also occurs in early CLL phases and its underlying mechanisms have yet to be fully elucidated. In this study, we prospectively enrolled 36 consecutive treatment-naïve patients to analyse skeletal structure and bone marrow distribution using a computational approach to PET/CT images. This evaluation was combined with the analysis of RANK/RANKL loop activation in the leukemic clone, given recent reports on its role in CLL progression. Bone erosion was particularly evident in long bone shafts, progressively inc…
Additive effects of cherlerythrine chloride combination with erlotinib in human non-small cell lung cancer cells
2017
Several studies implicate that lung cancer progression is governed by the interaction between epidermal growth factor receptor (EGFR) signaling and protein kinase C (PKC) pathways. Combined the targeting of EGFR and PKC may have an additive or synergistic effects in lung cancer treatment. The aim of this study is to explore the potential utility by inhibiting these two pathways with the combination of erlotinib and chelerythrine chloride in non-small cell lung cancer (NSCLC) cell lines. The erlotinib-less sensitive cell lines SK-MES-1 and A549 were treated with erlotinib or chelerythrine by themselves or in combination with each other. The cell viability, clonogenic survival, cell migration…