Evaluation Of Antiproliferative Activity Research Articles

Identification and Antiproliferative Activity Evaluation of a Series of Triterpenoids Isolated from Flueggea virosa (Roxb. ex Willd.)

Problem statement: Medicinal plants derived anticancer were now being subjects of many research groups especially, the secondary metabolite triterpenoids trees which had enormous potential to inspire and influence modern antiproliferative research. The study aimed to investigate the chemical constitution and their potential use as antiproliferative activity of purified compounds derived from F. virosa. Approach: The F. virosa was selected and percolated with hexane, ethyl acetate, acetone and methanol. The extracts were purified and elucidated chemical structures. Furthermore, the isolated compounds were tested for biological activity. The bioassays were performed on two cancer cell lines, adriamycin-sensitive erythroleukemia cells (K562) and adriamycin-resistant erythroleukemia cells (K562/Adr) which overexpressed P-glycoprotein (MDR1/ABCB1). Results: Friedelin (1), epifriedelanol (3), stigmasterol (4) and betulinic acid (5) were isolated from the leaves and twigs of F. virosa. The molecular structures of these compounds were determined using several spectroscopic methods. The compounds i.e., 1, a chemically modified compound 1 heptanolide (2), 3 and 4 showed a limited cytotoxic activity towards human cancer cell lines mainly due to a low aqueous solubility which prevented their use in cell viability assays. Interestingly, compound 5 exhibited a high cytotoxicity characterized by an effective concentration value (IC50) equal to 9.7±2.1 µg.mL-1 (21.2±4.6 µM) and 7.1±0.7 µg.mL-1 (15.5±1.5 µM) for K562 and K562/Adr, respectively. Moreover, the antiproliferative activity of compound 5 was independent of the multidrug resistance phenotype exhibited by the K562/Adr cell line suggesting that compound 5 was not the effluxes out of the K562/Adr cells by MDR1 (ABCB1). Conclusion: The results clearly showed that the betulinic acid of the four isolated compounds from F. virosa could be considered as high potential source of cytotoxic activity.

Novel Isopentenyladenosine Analogues: Synthesis, Characterization, and Evaluation of Antiproliferative Activity on Bladder Carcinoma Cells

Isopentenyladenosine (iPA), a member of the cytokinin family of plant hormones, exerts a marked antiproliferative activity on some leukemic and epithelial cancer cell lines. To characterize the molecular moieties required for the in vitro antitumor activity of the molecule and to obtain cytostatic iPA derivatives potentially useful as chemotherapeutic agents, N9-acyclic analogues have been synthesized using regioselective Mitsunobu reaction and characterized by elemental analyses, 1H and 13C NMR. These compounds were analyzed for their activity on human bladder cancer cell lines. In this study, we report that iPA inhibited the proliferation but not the migration of human bladder cancer cells, while the newly synthesized analogues revealed no significant cytostatic activity apart from the compound with a saturated double bond of the isopentenyl chain. These results indicate that the integrity of the ribose ring is required for the cytostatic activity of iPA.

Semi-synthesis and anti-proliferative activity evaluation of novel analogues of Honokiol

A series of honokiol analogues were synthesized by modifying the 5- and/or 3′-position(s) of honokiol to assess their anti-tumor effects. Some compounds exerted more potent anti-proliferative activities than those of honokiol on K562 leukemia cells, A549 alveolar basal epithelial cells, SPC-A1 adenocarcinoma cells and A2780 human ovarian carcinoma cells in vitro. Compounds 2b, 3a, and 3c displayed most potent anti-proliferative activities against these tested cell strains and their anti-drug resistance effects were evaluated in vitro on cisplatin-resistant A2780 human ovarian carcinoma cells. The structure–activity relationship was also proposed.

Evaluation of Antiproliferative Activities and Action Mechanisms of Extracts from Two Species of Ganoderma on Tumor Cell Lines

The antiproliferative activities on tumoral cells, namely, human breast cancer (MCF-7 and MDA-MB-231), hepatoma (HepG2) and myeloid leukemia (HL-60), of ethanolic extracts from two species of Ganoderma, G. lucidum and G. sinense, were investigated. Though both extracts had certain antiproliferative activities, their chemical characteristics, including nucleosides, triterpenoids and sterols, were significantly different. Their effects on MDA-MB-231 cells were further studied using apoptotic detection and cell cycle analyses. As a result, both had apoptosis induction through the alternation of mitochondrial transmembrane depolarization, though no triterpenoids were detected in ethanolic extract of G. sinense. Furthermore, the two extracts from G. lucidum and G. sinense could arrest cell cycle at different phases. This study showed that ethanol extracts of both G. lucidum and G. sinense have antitumoral proliferation effect through both apoptosis pathway and cell cycle arrest effect, and some other compounds such as sterols and/or nucleosides may contribute to their activity besides triterpenoids.

Antiproliferative activity of lichen extracts on murine myeloma cells

In the present study we report some preliminary results concerning the evaluation of antiproliferative activity on murine myeloma cells (P3X63-Ag8.653) of crude extracts of two common lichen species, Evernia prunastri and Xanthoria parietina.

Evaluation of antiproliferative activities and apoptosis induction caused by copper(II)–benzothiazolesulfonamide complexes in Jurkat T lymphocytes and Caco-2 cells

Two copper(II) complexes with a benzothiazolesulfonamide ligand, [Cu(L)2(py)2] (1) and [Cu(en)2(L)2] (2) [HL is N-2-(4-methylbenzothiazole)toluenesulfonamide, py is pyridine, en is ethylenediamine], were prepared and then characterized with the aid of X-ray crystallography and spectroscopy. Whereas the copper(II) ion in 1 presents a square-planar geometry, in 2 it has a distorted octahedral environment. In addition, although the ligand is monodentate in both complexes, it exhibits different coordination behavior in each, interacting through the benzothiazole nitrogen atom in 1 and through the sulfonamide nitrogen atom in 2. The propensity for binding of 1 and 2 to calf thymus DNA was studied by thermal denaturation, viscosimetry, and cyclic voltammetry. The ability of the complexes to cleave DNA was studied in vitro through ascorbate activation and was tested by monitoring the expression of the yEGFP gene containing the RAD54 reporter. Moreover, their antiproliferative activity was verified in two cellular models: yeast and human tumor cells in culture. While 1 was found to be the more active cleaving agent in vitro, 2 showed a higher propensity for inflicting DNA damage at the cellular level. The biological studies carried out with human tumor cells, namely, colon adenocarcinoma Caco-2 cells (HTB-37) and leukemia Jurkat T lymphocytes (TIB-152), confirmed that both compounds inhibit the growth of these cell lines, although 2 is more effective. This difference is associated with the latter compound's greater ability to induce cell death by apoptosis.

Synthesis of psymberin analogues: probing a functional correlation with the pederin/mycalamide family of natural products.

In this letter we describe an efficient synthesis of "psympederin", a hybrid between the novel antitumor natural product psymberin and the blister beetle toxin pederin. Evaluation of antiproliferative activity reveals that the dihydroisocoumarin fragment is important for psymberin toxicity and the cyclic pederate fragment is important for pederin/mycalamide toxicity. On the basis of preliminary results described herein, we speculate that, despite their structural resemblance, psymberin and pederin/mycalamide induce toxicity through different mechanisms. [reaction: see text].

Design and synthesis of new pyranoxanthenones bearing a nitro group or an aminosubstituted side chain on the pyran ring. Evaluation of their growth inhibitory activity in breast cancer cells

Some new 2,6-disubstituted pyrano- and 1,2-dihydropyrano[2,3- c]xanthen-7-ones have been synthesized and their antiproliferative activity has been evaluated against MDA-MB-231 breast cancer cells. The antiproliferative activity evaluation of the compounds provided evidence that a dimethylamino substituted side chain and the presence of 1,2 double bond play a key role in cell growth inhibition. Among the tested derivatives the 6-dimethylaminoethylamino-2-nitropyranoxanthenone analogue possessed a significant inhibitory effect in a wide range of concentrations.

Evaluation of Antiproliferative Activity of Enoxacin on a Human Breast Cancer Cell Line

Breast cancer is the leading cause of cancer in women world wide both in the developed and developing countries. Thus effective treatment of breast cancer with potential anti-tumor drugs is importa...

Evaluation of Antiproliferative Activity of Enoxacin on a Human Breast Cancer Cell Line

Evaluation of Antiproliferative Activity of Enoxacin on a Human Breast Cancer Cell Line

Synthesis and evaluation of antiproliferative activity of a geldanamycin–Herceptin™ immunoconjugate

Geldanamycin was modified with 1,4-diaminobutane to introduce a primary amine that was subsequently employed to provide a maleimide for protein linkage. Monoclonal antibody Herceptin™ was then derivatized to generate thiol groups that reacted with the maleimide derivative to produce the immunoconjugate. The product showed antiproliferative activity greater than native Herceptin™.

In vitro effects of cholesteryl butyrate solid lipid nanospheres as a butyric acid pro-drug on melanoma cells: evaluation of antiproliferative activity and apoptosis induction.

Literature data show that butyric acid derivatives bear a dose-dependent differentiative anti-proliferative activity on cancer cell lines and that apoptosis induction may play a major role. Although it was recently shown that solid lipid nanospheres (SLNs) are a suitable tool for several in vivo drug administration routes, there is little available information on melanoma cell lines. This study was aimed at evaluating the anti-proliferative and apoptotic in vitro effects of cholesteryl butyrate (chol-but) SLNs on melanoma cells. Increasing concentrations of chol-but SLNs were used to test two melanoma cell lines. Both cell lines were treated with Na-butyrate (Na-but) and chol-but SLNs for viability. Those tested with chol-but SLNs were more effective than Na-butirate (3 to 72 h). The apoptotic effects of chol-but SLNs were evaluated between 3 and 72 h by annexin-V (ANX-V)/propidium iodide (PI) staining and the antiproliferative effect by PI staining. Apoptosis anti-proliferative-regulatory proteins as bcl-2, Fas/APO1 (CD95) and PCNA (PC10) were also investigated. Flow cytometric analyses evidenced a G(0/1)-S transition block and a 'sub-G(0/1)' apoptotic peak from 0.5 to 1.0 mM butyric acid. In ANX-V/PI flow cytometric staining, a dose- and time-dependent increase in the apoptotic cell percentage (ANX-V+) coupled with a down-regulation of PC10 and bcl-2 and a parallel up-regulation of Fas/APO1 (CD95) were found in both lines started after 3 to 24 h of chol-but SLNs treatment. Results show that chol-but SLNs exerts a dose/time-dependent effect in melanoma cell apoptosis induction between 3 and 24 h and a dose but not time-dependent effect after 24 h of treatment.