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unwind to release tubulin dimmers ( Liu et al., 2004 ; Sturdikova et al., 1986 ). The isolated taxane diterpenoids were assessed for their in vitro cytotoxic activity via arresting the cancer cells in mitosis. Tyrosine kinase enzyme possesses
Twenty land mosses were extracted by double maceration and ultrasonic extraction techniques using the mixture of 80% ethanol and water. The obtained extracts were analyzed using thin-layer chromatography (TLC) with silica gel (the mobile phase was consisted of ethyl acetate–formic acid–acetic acid–water, 14.0:1.5:1.5:2.0, v/v) and RP-18 (the composition of eluent methanol–water–formic acid, 7.0:2.5:0.5, v/v) chromatographic plates. After developing and drying, the plates were sprayed using the Naturstoff reagent, and after drying, the chromatograms were photographed and the obtained images were processed using the ImageJ program. Principal component analysis was performed to confirm the chemical similarity between the studied moss extracts. The cytotoxic activity of the ethanolic extracts of Bryophyta species was studied using the cell lines CCRF/CEM and CEM. For most of the moss samples, the cytotoxic activity was confirmed.
. Khanavi , M. , Nabavi , M. , Sadati , N. , Ardekani , M. S. , Sohrabipour , J. , Nabavi , S. M. B. , Ghaeli , P. , Ostad , S. N. ( 2010 ) Cytotoxic activity of some marine brown algae against cancer cell lines . Biol. Res. 43 , 31 – 37
Extensive research on Ficus species has shown their excellent cytotoxic potential which motivated the authors for further evaluation of its other species. In this article, the β-sitosterol content in the chloroform extract of the leaves of five Ficus species (Ficus carica [FCCE], Ficus nitida [FNCE], Ficus ingens [FICE], Ficus palmata [FPCE], and Ficus vasta [FVCE]) was estimated by a validated high-performance thin-layer chromatography (HPTLC) method along with cytotoxic activity. The chromatography was performed on glass-backed silica gel 60 F254 HPTLC plates with hexane and ethyl acetate (8:2, v/v) as the mobile phase. The developed plate was derivatized with p-anisaldehyde reagent, scanned, and quantified at λ = 550 nm. It furnished a compact and intense peak of β-sitosterol at R F = 0.17 ± 0.001. The contents of β-sitosterol (μg mg−1 of the dried weight of the extract) in the selected Ficus species were found as: FCCE (1.047 μg mg−1) > FVCE (0.771 μg mg−1) > FNCE (0.372 μg mg−1) > FPCE (0.309 μg mg−1), while it was absent in F. ingens. Methylthiazol tetrazolium (MTT) assay was used to compare the cytotoxic potential of all Ficus species against HepG2 (liver), HEK-293 (kidney), MCF-7 (breast), and MDA-MB 231 (breast) cell lines. The FCCE exhibited good cytotoxic property against HepG2, HEK-293, and MDA-MB-231 cells (IC50: 32.5, 41.4, and 47.3 μg mL−1, respectively), while FICE showed against HepG2 and MDA-MB-231 cells (IC50: 31.4 and 41.2 μg mL−1, respectively). The remaining Ficus extracts were found to be very less effective or insignificant. The cytotoxic property of FCCE is also supported by the HPTLC estimation of β-sitosterol which is reported to exhibit anticancer properties by interfering with multiple cell signaling pathways, including cell cycle, apoptosis, and proliferation. Our data suggest that the developed HPTLC method can be further employed in the analysis of marketed herbal formulations, and the active Ficus species can be further subjected to isolation of cytotoxic phytoconstituents.
A series of new (S,S)-ethylenediamine-N,N′-di-2-(3-cyclohexyl)propanoate esters has shown cytotoxic activity towards human leukemic cell lines. The aim of this study was to develop and validate a bioanalytical method for quantification of (S,S)-O,O-diethyl-ethylenediamine-N,N′-di-2-(3-cyclohexyl)propanoate dihydrochlorides (DE-EDCP) and its metabolite, substituted propanoic acid (EDCP), in mouse serum by ultra high-performance liquid chromatography—tandem mass spectrometry (UHPLC—MS/MS). Structural analog, derivative of 1,3-propanediamine, was used as an internal standard (IS). Sample preparation employed protein precipitation by acetonitrile and subsequent centrifugation. Optimal UHPLC separation conditions were set to achieve simultaneous determination of both compounds in a short run time of 6 min. Additionally, the selected reaction monitoring (SRM) mode developed in this method allowed a highly sensitive, accurate, and precise identification of compounds of interest. The lower limit of quantitation (LOQ) was 1.3 ng mL−1 for DE-EDCP and 0.3 μg mL−1 for EDCP. The calibration curves were linear over the concentration range of 1.3–26.7 ng mL−1 and 0.3–6.7 μg mL−1 for DE-EDCP and EDCP, respectively. Precision (%CV) and accuracy (%RE) for DE-EDCP and EDCP ranged from 3.5% to 16.0% and from 1.8% to 14.4%, respectively.
The validation process was performed in accordance with the regulatory guidance/guideline, and all of the obtained results met the established acceptance criteria. The newly developed and validated UHPLC—MS/MS method is rapid, sensitive, and selective, and it can be successfully applied to drug monitoring in nonclinical studies.
3. Damu , A. G. , Kou , P. C. , Su , C. R. , Kuo , T. H. , Chen , T. H. , Bastow , K. F. , Lee , K. H. , Wu , T. S. ( 2007 ) Isolation, structures, and structure–cytotoxic activity
New palladium(II) complexes with pyrazole ligands
Part II. Synthesis, spectral and thermal studies, and antitumor evaluation
cisplatin toward the MOLT-4 and C2C12 tumor cell lines [ 4 ]. Rocha et al. [ 5 ] have reported that the cytotoxic activity of the [PdI 2 (tdmPz)] compound (tdmPz = 1-thiocarbamoyl-3,5-dimethylpyrazole) towards mammary adenocarcinoma murine tumor cell line
species, but unexplored. The aim of the study was to determine the antiradical and cytotoxic activities of C. gambosa extracts and peptide fraction, which has not been studied before, and the chemical composition that includes the content of total
In this research, the phenolic composition, antioxidant, antibacterial and cytotoxic activities of the methanolic extracts obtained from Alyssum fulvescens var. fulvescens aerial parts known as Ege kuduzotu in western Turkey, were firstly investigated. The antioxidant activity of the extract was determined by DPPH, metal chelating, phosphomolybdenum, β-carotene/linoleic acid and ferric reducing power assays. Moreover, total phenolic and flavonoid contents in the extract were investigated. The brine shrimp (Artemia salina L.) lethality test was used to investigate for the possible cytotoxic activity of the extract. Microdilution broth method was used to study antibacterial potency of extract against Gram-positive and Gram-negative bacteria. The extract exhibited good biological activities. Total phenolic and flavonoid contents in the extract were significantly correlated with antioxidant potentials. HPLC analysis showed that chlorogenic acid was the major phenolic in extract tested. The results indicated that the extract of A. fulvescens var. fulvescens may be considered as a potential source of biological agents and in vivo investigations are needed to test the biological effects of A. fulvescens var. fulvescens.
The aim of the present study was to determine the expression of granzyme B in non-perforated appendicitis. Appendix biopsies were obtained from the patients with clinically diagnosed as acute appendicitis and subjects admitted for elective abdominal surgery. All biopsies from the patients were non-perforated and histologically divided into acute and non-acute appendicitis. Granzyme B expression was assessed immunohistochemically. The results showed that granzyme B expression in both acute and non-acute appendicitis was significantly lower than that in the control appendix tissues ( P <0.05). The expression of this cytotoxic protein in acute and non-acute appendicitis was comparable ( P >0.05). Therefore, the results of the present study suggest that reduced expression of granzyme B in non-perforated appendicitis may reflect low cytotoxic activities which may prevent tissue damage.
