جستجوی مقالات مرتبط با کلیدواژه « cytotoxic effect » در نشریات گروه « پزشکی »

Candidiasis therapy is a complicated concern because of the occurrence of resistance to antifungal agents. We studied the anti-fungal effects of Ferula macrecolea essential oil (FME) against Candida albicans resistant and sensitive strains, as well as its cytotoxic effects against normal and cancer cell lines.

The minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) of F. macrecolea essential oil against C. albicans ATCC 5027 and C. albicans ATCC 76616 were studied by broth-microdilution approach. The cytotoxicities of FME on HGF1-PI (normal gingival cell line) and HepG2 (liver cancer cell line) cells were also studied.

The main components of essential oil were terpinolene (71.25%), n-nonanal (6.32%), and linalool (3.95%), respectively. The MIC and MFC of FME on C. albicans sensitive to nystatin were 1.6 and 2.0 μg/mL, respectively. The MIC and MFC of FME on nystatin-resistant strains were 3.3 and 4 μg/mL, respectively. The MIC and MFC of terpinolene on C. albicans sensitive to nystatin were 0.8 and 1.0 μg/mL, respectively. The MIC and MFC of terpinolene on nystatin-resistant strains were 2 and 2.4 μg/mL, respectively. The essential oil and terpinolene had no significant cytotoxic effects against normal cells.

We revealed the promising antifungal effect of F. macrecolea essential oil and its main component, terpinolene, against C. albicans sensitive and resistant to nystatin with no significant toxicity on normal cells.

 Developing a potent and safe scaffold is challenging in anti-cancer drug discovery.

 The study focused on developing novel series of compounds based on the inhibition of epidermal growth factor receptor tyrosine kinase (EGFR-TK) as one of the most promising compounds in cancer therapy.

 In this study, a novel series of quinazoline-2,4,6-triamine derivatives were designed and synthesized through intramolecular C-H activation reaction of para-nitro aniline, trichloroacetonitrile, and isocyanides employing a one-pot reaction.

 The in-vitro antitumor activities of the compounds which showed acceptable inhibitory effects were investigated against breast (MCF-7), lung (A-549), and colon (HT-29) cancer cell lines by employing MTT assay. All compounds had the most negligible cytotoxicity toward normal fibroblast human cell lines. Based on structural and thermodynamics analysis results, it was found that Met 769 is a key residue in interaction with all inhibitors through the formation of hydrogen bonds with high occupancies with the amine group on the quinazoline ring of inhibitors. Also, there was a good consistency between calculated ΔG binding and experimental IC50 values of compounds 10d, 10e, and erlotinib.

 Compound 10e had an extensive range of antitumor activity on three diverse cell lines comparable with erlotinib and doxorubicin reference drugs. Also, compound 10d showed selective cytotoxicity against cancerous lung cells (A-549). On the other side, computational studies confirmed that Met 769 is a crucial residue in interaction with all inhibitors.

Several lines of experimental evidence have shown that saffron has anticarcinogenic effects. This study aimed at evaluating the possible anticancer effect of saffron stigma aqueous extract on human prostate cancer (PC3) and mouse fibroblast cells (L929) as non-cancerous control cells.

Saffron stigma aqueous extract at concentrations of 100, 200, 400, 600, 800, 1600 and 3200 μg/mL were prepared. PC3 and L929 cells were incubated with different concentrations of saffron extracts in different time intervals (24, 48, 72, 96 and 144 hours). MTT assay was used for each cell line to investigate the cytotoxic effect of saffron. Morphological alterations were also observed under light inverted microscope.

In fibroblast cell line after 24 hours, Saffron extract did not affect significantly the normal cells and they were intact in morphologic view. After 96 hours in the cells with highest concentration (1600 μg/mL), cell death and cellular form changes as well as severe granulation was observed. In prostate cell line after 24 hours, the only changes were observed in cells with the concentration of 1600 μg/mL. The cells were granulated and the form of the cells were spherule. After 72 hours, in group with the concentration of 1600 μg/mL, severe granulation was observed and the cell count decreased and some cells were dead.

Saffron aqueous extract has an in vitro inhibitory effect on the proliferation of human prostate cell and mouse L929 cells which is dose-dependent.

Cancers in terms of morbidity and mortality are one of the major universal issues. New compounds of anticancer agents based on β-aryl-β-mercapto ketones scaffold possessing piperidinyl ethoxy or morpholinyl ethoxy groups were synthesized and evaluated as cytotoxic agents. Cytotoxic effects of synthesized compounds were measured against MCF-7, human ER-positive breast cancer cell lines, using MTT assay. The results indicated that all compounds had high cytotoxic activity on MCF-7 cancerous cells, even more than the reference drug Tamoxifen. Among them, compounds 3-(4-(2-morpholinoethoxy)phenyl)-1-phenyl-3-(phenylthio)propan-1-one (4a) and 1-(4-methoxyphenyl)-3-(3-(2-morpholinoethoxy)phenyl)-3-(phenylthio)propan-1-one (4h) had no significant cytotoxic effects on normal cells compared to Tamoxifen. Our results also indicated that adding tertiary amine basic side chain, found in Tamoxifen drug, to 1,3-diphenyl-3-(phenylthio)propan-1-ones improves the cytotoxic effects of these compounds on breast cancer cells.

Arum rupicola Boiss. (Araceae Family) is used by the native people of southern areas of Iran as a soup called "kardeh soup". Several flavonoids and phenol compounds have been identified from Arum species.

The aim of this study was to evaluate antioxidant effect and total phenol contents as well as cytotoxic activity of the leaves of A. rupicola.

Antioxidant activity of total methanol extract and fractions including n-hexane, chloroform, ethyl acetate and water residue were evaluated using FRAP and DPPH methods. Total phenol content was measured using Folin-Ciocalteu method. Cytotoxic activity of the extract and fractions were investigated against human breast cancer MCF-7, MDA-MB-231, and T47D cell lines by MTT assay. Further phytochemical isolation was done on the water residue using column chromatography.

According to the results, water residue showed the lowest IC50 value (186.7 µg/ml) and the total methanol extract showed the most antioxidant power (163.62 mmol FeSO4/100 g extract) and phenol content (135 µmol Gallic acid/g extract). The hexane fraction also showed the highest cytotoxic effect against MCF-7 breast cancer cell line with IC50 equal to 118.9 μg/ml. Phytochemical analysis of the water residue resulted in isolation and identification of three isoflavonoids named orobol, genistein and genistein 8-c-glucoside.

Based on the identification of isoflavonoid compounds in this plant, its ability to be used as a phytoestrogenic supplement can be considered in future studies.

Verbascum species showed various pharmacological activities including anti-inflammatory, antitussive, antiulcerogenic, immunomodulatory, antimicrobial, antimalarial, antioxidant, and anticancer activities.

The aim of this work was to evaluate cytotoxicity of different fractions of Verbascum alceoides, which belongs to this genus.

Aerial parts of this plant were collected from Doveiseh area in Kordestan province. The plant was extracted using a four-step extraction method with increasing solvent polarity (i.e., hexane, dichloromethane, chloroform-methanol [9:1], and methanol). The methanol extract was finally separated between water and butanol. Hexane, dichloromethane, chloroformmethanol, butanol, and aqueous partitions were then subjected to cytotoxicity evaluation. Showing the most potent cytotoxic effects, the butanolic partition was further fractionated by medium-performance liquid chromatography and similar eluates were pooled to prepare five final butanolic fractions, named A–E.

In vitro cytotoxicity of these fractions against human cervical epithelioid carcinoma (HeLa) and human umbilical vein endothelial cell (HUVEC) was evaluated using 3-(4,5-dimethyl-2- thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay. Fractions D, E, and A showed a significant and dose-dependent inhibition of cell proliferation (half maximal inhibitory concentration [IC50] of 30, 39.8, and 188.6 µg/mL, respectively). According to the preliminary thin-layer chromatography analysis, these cytotoxic effects may be mainly due to presence of saponin and flavonoid compounds.

Future studies will be aimed to isolate and purify active constituents and investigate the effect of them on more different kinds of cancer cells.

The 2-pyrazoline derivatives have a wide range of biological effects, such as anti-viral, anti-bacterial, anti-fungal, anti-depressant and anti-cancer effects. Studies have shown that compounds containing 2-pyrazoline along with another heterocycles may show more effective biological properties. In this study, a 2-pyrazoline derivative with a spiro-indenoquinoxaline ring at C3 position was synthesized by one-pot microwave-assisted method and its chemical structure was confirmed by 1H NMR spectroscopy. The cytotoxic effects of the compound were evaluated on the K562 cell line and phytohemagglutinin-activated peripheral blood mononuclear cells (PHA+PBMC) by MTT assay. Additionally, the cytotoxic effects of cisplatin on these cells were investigated and compared with those of 2-pyrazoline. The IC50 values obtained from the 2-pyrazoline derivative effects on the K562 cell line and PHA+PBMC cells were 45 and 55 μg/mL respectively, while cisplatin inhibited proliferation of the same cells with IC50 value 1.71 and 7.8 μg/mL respectively. The results of this study showed that the synthesized derivative had a cytotoxic activity on the K562 cancer cell line at higher concentrations than cisplatin.

Breast cancer cells with overexpression of HER2 are known to be more aggressive, invasive, and resistant to chemotherapeutic agent. Brazilin, the major compound in the Caesalpinia sappan L. (CS) heartwood, has been studied for it's anticancer activity. The purpose of this study was to investigate the cytotoxic and antimigratory activity of brazilin (Bi) in combination with doxorubicin (Dox) on MCF-7/HER2 cells. Cytotoxic activities of Bi individually and in combination with Dox were examined by MTT assay. Synergistic effects were analyzed by combination index (CI). Apoptosis and cell cycle profiles were observed by using flow cytometry. Migrating and invading cells were observed by using a Boyden chamber assay. Levels of MMP2 and MMP9 activity were observed by using a gelatin zymography assay. Levels of HER2, Bcl-2, Rac1, and p120 protein expression were observed by using an immunoblotting assay. The results of the MTT assay showed that Bi inhibited MCF-7/HER2 cell growth in a dose-dependent manner with an IC50 of 54 ± 3.7 µM. Furthermore, the combination of Bi and Dox showed a synergistic effect (CI <1). Flow cytometric analysis of Bi and its combination with Dox showed cellular accumulation in the G2/M phase and induction of apoptosis through suppression of Bcl-2 protein expression. In the Boyden chamber assay, gelatin zymography, and subsequent immunoblotting assay, the combination Bi and Dox inhibited migration, possibly through downregulation of MMP9, MMP2, HER2, Rac1, and p120 protein expression. We conclude that Bi enhanced cytotoxic activity of Dox and inhibited migration of MCF-7/HER2 cells. Therefore, we believe that it has strong potential to be developed for the treatment of metastatic breast cancer with HER2 overexpression.

Umbelliprenin is a sesquiterpene coumarin with vitro anti-carcinogenic activities. The aim of this study was to investigate the antitumor effects of umbelliprenin in animal models of colorectal cancer. The cytotoxic effects of umbelliprenin were explored on CT26 and L929by MTT assay. In this study, colorectal tumors developed in mice by intradermal injection of CT26 cell line. Tumor size, serum levels of IFN-γ and IL-4 by ELISA, and Ki-67, MMP2, MMP9, VEGF and E-cadherin markers by IHC method were evaluated. The results showed that umbelliprenin inhibited the cancer cells in a concentration-dependent manner. IC50 Evaluation showed that L929 cells were more resistant to Umbelliprenin than CT26 cells. Umbelliprenin treatment in both tumor-bearing mice and control normal mice showed significantly increased IFN-γ and decreased IL-4(P

Pterocarya fraxinifolia Lam. is a deciduous, fast-growing tree from walnut family. The stem barks and fruits of the plant have been used as diaphoretic in traditional medicine. Variation in the quantity and quality of the essential oil and extract of stems of the plant at different developmental stages was evaluated in addition to assessing the antimicrobial, cytotoxic and radical scavenging activities in the present study.

Different developmental stages of the plant’s stem (i.e. vegetative, flowering, immature fruit and mature fruit) were subjected to hydro-distillation for obtaining the essential oil. The methanol extract of the samples was obtained by Soxhlet apparatus. Chemical composition of the oils was analyzed by gas chromatography/mass spectroscopy (GC/MS). Antimicrobial activity of the oils and extracts were determined against three Gram-positive and five Gram-negative bacteria and two fungi by disc diffusion method. Antioxidant activity of the samples was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and β-carotene assays. Total phenolics content of extracts was determined using Folin-Ciocalteau reagent and cytotoxic effect was determined by brine shrimp lethality bioassay.

Hexadecanoic acid was one of the major components in all essential oil samples. All samples showed good antimicrobial activity against tested strains. Antioxidant activity of the extracts was comparable to the synthetic standard (butylated hydroxytoluene). The highest total phenolic content and cytotoxic effect were detected for the mature fruit stage of the plant extract and essential oil, respectively.

Showing considerable antioxidant and cytotoxic effects, suggested the plant as a good candidate for further investigations.

The current study was assigned to evaluate the total phenol, total flavonoid content (TPC, TFC) and antioxidant properties of extracts from the aerial parts of Scrophularia frigida (S. frigida). Extracts were also tested by preliminary phytochemical screening as well as cytotoxic activity against Artemia salina, MCF-7 (human breast carcinoma) and SW-480 (colon carcinoma) and L-929 (normal) cell lines along with antimicrobial characteristic. DPPH, MTT and Brine shrimp lethality tests and disc diffusion method were carried out to determine the biological activities of the different extracts of S. frigida. In addition, the extracts which had more potent antioxidant and antiproliferative activity were further analyzed by NMR and GC-MS. 40% methanol-water (from MeOH extract) fraction showed higher amounts of TPC, TFC and antioxidant property. Findings of the study for general toxicity effect showed that dichloromethane (DCM) and MeOH extracts had weak to moderate effects. Furthermore, DCM extract indicated the most potent anti-proliferative activity against cancer cell lines. No evidence of antibacterial activity was determined. On the other hand, analysis of the potent extract DCM in cytotoxic assay showed the presence of trans-phytol and cis-oleic acid in GC-MS. Furthermore, NMR analysis of potent methanolic fractions in antioxidant tests revealed the presence of iridoid and phenolics. Generally the results of TPC, TFC and antioxidant activity of extracts and fractions were in agreement with each other.

Leukemia is a blood disease which is caused by the inhibition of differentiation and an increased proliferation rate. Nature has been known as a rich source of medically useful substances. High diversity of bioactive molecules extracted from marine invertebrates, makes them ideal candidates for cancer researches. The study has been done to investigate cytotoxic effects of dichloromethane brittle star extract and doxorubicin on EL4 cancer cells. Blood cancer EL4 cells were cultured and treated by different concentrations of brittle star dichloromethane extract for 24, 48 and 72 h. Cell toxicity was studied using the MTT assay. Cell morphology was examined using an invert microscope. Further, apoptosis was examined using Annexin V-FITC, propodium iodide, DAPI and Acridine orange / propodium iodide staining. Eventually, the apoptosis pathways were analyzed using measurement of caspase-3 and -9 activities. The statistical analysis was performed using SPSS software, ANOVA test, Tukey post test. p

It is extensively supposed that vegetarian diet could affect cancer progress and increase the influence of formal chemotherapy.
The present study was designed to determine the effect of the ethanol Bane skin extract against chemo resistant prostate cancer PC3 cells.
PC3 and L929 cells were cultivated and then incubated in the ethanol Bane skin extract with various concentrations of 0.78, 1.5, 3.13, 6.25, 12.5 mg/mL in 3 times 24, 48, 72 hours. Cytotoxic effect of the ethanol Bane skin extract on PC3 and L929 cells was examined by MTT assay after 24, 48, and 72 hours. Morphology of PC3 cells was evaluated by Gimsa staining.
The ethanol Bane skin extract inhibited proliferation and caused cell death with IC50 values of 2.8 mg/mL on PC3 cells and the IC50 was 6.1 mg/mL on l929 cells. Morphological changes and apoptotic bodies were observed in PC3 cells faced with the ethanol Bane skin extract by staining with Gimsa.
The ethanol Bane skin extract could repress the growth of PC3 cell line. This inhibitory effect of the Bane extract depended on the dose and the time on PC3. The result of this study shows that the ethanol Bane skin extract includes photochemical and inhibitory function against proliferation and inducer of apoptosis in human prostate cancer PC3 cells and also has less cytotoxic effect on l929 than PC3 cells. The ethanol Bane skin extract might be a good candidate for the new herbal anticancer drug.

Iran owns a rich and prestigious heritage of medicinal herbs but the majority of these plants have not yet undergone chemical, pharmacological and toxicological studies. In the present study some species form northern parts of Iran were evaluated for cytotoxicity.

Sixteen medicinal plants were extracted with methanol and screened for their cytotoxic activities. The inhibition of cell growth for these extracts was evaluated against MCF-7, WEHI-164, HepG-2 and MDBK cell lines. Their 50% inhibitions of growth (IC50) were determined by MTT assay. Moreover, cytotoxic evaluation of different fractions of the most potent species was performed.

Among examined samples, the IC50 values of methanol extract of Centaurea bruguierana (DC.) Hand.-Mzt. on mentioned cell lines were found 47.30-87.40 µg/mL. In addition, the chloroform fraction of the species was cytotoxic with IC50 values 17.00-23.03 µg/mL.

It was concluded that the chloroform fraction of C. bruguierana was the best candidate for identification and isolation of active principles with cytotoxic effects. These results recommend further studies about this species.

In spermatogenesis, spermatogonial cells differentiate to the haploid gametes. It has been shown that spermatogenesis can be done at in vitro condition. In vitro spermatogenesis may provide an open window to treat male infertility.

The aim of this study was to evaluate the effects of a novel scaffold containing human serum albumin (HSA)/tri calcium phosphate nanoparticles (TCP NPs) on the mouse spermatogonial cell line (SCL).

First, TCP NPs were synthesized by reaction of calcium nitrate and diammonium phosphate at pH 13. Then, serial concentrations of TCP NPs were separately added to 500 mg/mL HSA, and incubated in the 100oC water for 30 min. In the next step, each scaffold was cut (2×2mm), placed into sterile well of microplate, and then incubated for 1, 2, and 3 days at 37oC with mouse SCL. After incubation, the cytotoxicity of the scaffolds was evaluated by different tests including 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyl-tetrazolium bromide (MTT) assay, lactate dehydrogenase (LDH) assay, vital staining, and cell counting. On the other hand, the release of TCP NPs and HSA from the scaffolds was measured.

Based on microscopic observation, the size of cavities for all scaffolds was near 200-500 µm, and the size of TCP NPs was near 50-100 nm. All toxicity tests showed that the increase of TCP concentration in the scaffold did not affect mouse SCL. It means that the percentage of cell viability, LDH release, vital cells, and cell quantity was 85%, 105%, 90%, and 110%, respectively. But, the increase of incubation time led to increase of LDH release (up to 115%) and cell count (up to 115%). Also, little decrease of cell viability and vital cells was seen when incubation time was increased. Here, no release of TCP NPs and HSA was seen after increase of TCP concentration and incubation time.

It can be concluded that the increase of TCP concentration in HSA/ TCP NPs scaffold does not lead to cytotoxicity. On the other hand, the increase of incubation time leads to increase of mouse SCL cell death. In this study, it was found that TCP NPs and HSA could not release from the scaffolds. In future, both proliferation and differentiation of mouse SCL on HSA/TCP NPs scaffold must be checked over more wide incubation times.