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

The Piper betleplant, known for its pharmacological properties, has been traditionally usedin Asian cultures. The objective of the current study is to assess the antioxidant, cytotoxic, antibacterial, and enzymatic inhibitions of leaf extracts of the P. betle. DPPH radicals were used to assess the antioxidant potential. The Lethality Assay for Brine Shrimp was used to assess the cytotoxic potential of plant extracts. The disc diffusion method was used to measure the leaves' antibacterial activity against various Gram stains. The inhibitory potential of four enzymes linked to different diseases was screened spectrophotometrically. Chromatographic procedures were used to isolate active substances, and their structures were determined using spectroscopic approaches. The results indicated that the P. betleleaves extracts to possess potent antioxidant activity, highest with the EAPB (ethylacetate, P. betle) followed by DCPB (dichloromethane, P. betle),HPB (n-hexane,P. betle), BPB (n-butanol, P. betle)and AQPB (aqueous P. betle). For cytotoxic activity, the EAPB has the most potent cytotoxic activity among the tested extracts. AQBP and HPB showed activity against all bacteria used, while (EAPB and DCPB displayed good activities against all organisms except Streptococcus aglaciate. For anti-diabetic activity, DCPB, and EAPB both showed high percent inhibition and low IC50. The identified compound, allylpyrocatechol, isolated from the EAPB fraction of betel leaf attributed higher inhibitory activity than the standard against α-glucosidase with an IC50 of 42.61 ± 1.27. For anti-ulcer activity, the DCPB had the highest urease % inhibition and the lowest IC50value, while (BPB) and AQBP fractions had lower levels of inhibition and higher IC50values. DCPB and EAPB exhibited neurodegenerative therapeutic potential by targeting prolyl endopeptidase with good activity having IC50values of 26.82 ± 0.36 and 52.92 ± 21.30μg/mL). Furthermore, these extracts were tested for their therapeutic potential for skin diseases by targeting the tyrosinaseenzyme. Interestingly, HPB and DCPB displayed good inhibitory capability with IC50 values of 36.14 ± 0.72, and 44.72 ± 1.28 μg/mL, respectively, compared to the standard kojic acid (IC50= 7.49 ± 0.21 μg/mL). In conclusion, crude extracts of Piper betle leaves exhibit potent antioxidant, antibacterial, and moderately cytotoxic effects. It also has strong anti-ulcer and anti-diabetic properties. Additionally, it exhibits strong anti-pigentation properties and good neurodegenerative potential

Cancer is one of the most prominent causes of death worldwide. Ocimum gratissimum Linn. (Lamiaceae) leaves are used in many countries as a spice or medicine. 

This study investigated the essential oil of the O. gratissimum leaves and its major constituent, thymol, for cytotoxic activity against breast (AU565) and cervical (HeLa) cancer cell lines. 

Preliminary screening was carried out using bench-top assay methods for cytotoxicity involving the use of tadpoles of Raniceps raninus (10-40 μg/mL) and brine shrimp of Artemia salina (10-1000 μg/mL) and growth inhibition using radicle of Sorghum bicolor seeds (1-30 mg/mL). Antiproliferation was verified by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Chromatographic separation of the oil resulted in fractions and sub-fractions, which were also subjected to biological testing. The components of the oil and active subfraction were further identified by gas chromatography-mass spectrometry (GC-MS). 

Remarkable cytotoxic activities were seen against R. raninus tadpoles and A. salina nauplii. Growth inhibitory activity on S. bicolor seed radicles was produced concentration-dependent. The subfraction possessed greater cytotoxic activity on the cell lines than the oil, with inhibitory action of +85.07% and +29.20% against AU565 and HeLa cells, respectively. Thymol was the major constituent of the oil (22.49%) and increased to 94.31% in the subfraction. 

O. gratissimum volatile oil showed little inhibitory activity against AU565 and no inhibition on HeLa cells. However, its major component, thymol, demonstrated high potency, especially on the AU565 cell line, making it a good candidate for further studies.

The reactivation of polyomavirus BK (BKPyV) contributes to increased morbidity and mortality rates of transplant patients, especially kidney transplant recipients (KTRs). CD4+ T cells are important immune cells active during BKPyV infection in KTRs. This research tried to examine the phenotype of CD4+ T cells in the stage of BKPyV activation in KTRs.The re cipients were separated into 2 groups of BKPyV-active and nonactive KTRs (10 patients in each group) and were compared with 10 healthy control subjects. The viral load was evaluated by Taq-man quantitative real-time PCR. The frequency of different CD4+ T cell subsets was determined by analyzing markers such as CD45RO, CCR7, CD27, CD107a, perforin, and granzyme B using flow cytometry. The gene expression levels of transcription factors, including TBX21, GATA3, STAT3, and STAT6, contributing to CD4+ T cell activation, were also assessed. A significantly higher proportion in CCR7+CD27+CD45RO-CD4+ T cell (naive Tcell) subsets was detected in BKPyV-active KTRs compared to nonactive ones. A significant increase was detected in the frequency of CD107a+, perforin+, and granzyme B+ CD4+ T cells in the BKPyV-active group compared to the nonactive group. In CD4+ T cells of KTRs, the mRNA expression of TBX21  and GATA3 was significantly increased in KTRs without BKPyV reactivation compared to BKPyV-active ones. This investigation focused on the CD4+ T cell as an immunodominant T cell type with potential cytotoxicity. Based on these results, BKPyV may have a direct influence on the repertoire of CD4+ T cell subsets. Particularly, cytotoxic CD4+ T cells need further investigation to be considered as a therapeutic approach for BKPyV infection.

The increased burden of cancer disease globally arouses the urgent need for the development of novel chemical agent with improved efficacy and potency which can provide selective therapeutic outcome to an individual cancer patient. In this connection the in-silico designing of novel scaffolds are greatly helpful evading the need for synthesizing and evaluating the series of large number compounds. We have constructed novel pyrazolopyrimidines with reference to existing fused pyrimidine standards like central aromatic heterocycles, spacers, hydrophobic heads and tails. We examined for the nature and biochemical targets, ADMET evaluations using various online tools and molecular docking analysis through Schrodinger suite studied binding affinities with reference to standards as well as co-crystals. We designed pyrazolopyrimidines 7a-j and 12a-j & molecular docking studies revealed that few were potential candidates compared to standard scores against various Ptarget kinases. The hydroxyl moiety in 7b & 7d, hydroxyl in 7e with 4-bromo showed more bonding affinity towards targets and remaining compounds produced mild to moderate affinities against various targets. GLU339, GLU51, LEU83, SER345, ASP404, ASN391and ASP348 are major residues for H-bonding interactions, PHE80, LEU83, GLN275 influenced hydrophobic bonding and ASP404 for nitro group, GLU339 for hydroxyl group, LYS89 for methoxy groups are key residues in binding affinity. We also identified the key residues of target proteins involved in the interaction with ligands at the active pocket. We believe that these results could benefit the future development of anticancer scaffold containing pyrazolopyrimidine motifs in the core structure.

Several chemotherapeutic agents have been associated with cancer treatment but with several undesirable effects. In this study, the cytotoxic and antioxidant effects of methanol extracts of ten selected plants from southwestern ethnomedicine were assessed as a probable source of natural products for the treatment of cancer. The phenolics and flavonoid contents, and in vitro antioxidant assays (DPPH, nitric oxide, total antioxidant capacity, ferric reducing antioxidant power, metal chelating, lipid peroxidation) on the plant extracts were evaluated. In vitro cytotoxic effects of the extracts on Brine Shrimps, Rhabdomyosarcoma (RD), Breast (MCF-7), and Cervical (HeLa) cancer cell lines were also evaluated. The plant extracts demonstrated a broad spectrum of antioxidant properties. All the extracts exhibited moderate toxicity on brine shrimp. Pacrilima nitida exhibited the highest inhibition on the growth of RD (CC50=17.97 µg/mL) and MCF-7 (CC50=38.79 µg/mL) cell lines while Cocos nucifera exhibited the highest inhibition on the growth of HeLa (CC50=24.16 µg/mL). These plants exhibited a relatively cytotoxic and antioxidant effect and thus could contribute to anticancer drug discovery and many other disease conditions due to their antioxidant properties.

Endometriosis is believed to be associated with dysfunction of the lymphocyte population and cytotoxicity of natural killer (NK) cells, induced by the production of interleukin-2 (IL-2).

This study aimed to investigate T lymphocytes and NK cell activity in the peripheral blood mononuclear cells (PBMCs) of women with endometriosis.

PBMCs were obtained from the peripheral venous blood samples of 14 women with and without endometriosis (n = 7 for each group). Then, the PBMCs were co-cultured for 4 days and were treated with recombinant IL-2 for cytotoxic activity toward target cells (Daudi and K562 cells). The cytotoxicity activity was determined using the 51 chromium release assay before and after stimulation. Flow cytometry measurement was used to examine the expression of T lymphocytes and NK cells before and after being treated with IL-2.

The concentration of CD3+CD28+ (co-stimulatory) was significantly lower in the endometriosis group (65.62 ± 5.38) compared to in its counterpart (50.24 ± 4.22) (p = 0.04) before stimulation. However, no significant differences were observed in any other T lymphocytes and NK cells. It was also found that there was a significant increase of CD3-CD28+ after treatment with IL-2 only in the healthy control but not in women with endometriosis.

Increased expression of CD160 and decreased CD28 play a role in inhibiting NK cell activation and T cell response in women with endometriosis.

In here, we introduced a rapid and green synthesis route to prepare pure zinc oxide (ZnO) and silver-doped zinc oxide (Ag-dop-ZnO) nanoparticles (NP) using Prosopis farcta extract. The physic-chemical property of the synthesized NPs was identified using PXRD, FESEM, FT-IR, UV-Vis, and EDX devices. According to the obtained outcomes of PXRD, UV-Vis, as well as EDX analysis, Ag was well doping into the ZnO structure. Moreover, spherical shape was observed with a mean size of 25-40 nm based on FESEM outcomes for the synthesized nanoparticles. The cytotoxic effect of the synthesized nanoparticles was assessed on glioblastoma (U87) cell line using an MTT test. The cytotoxic outcomes presented that the doped NPs have a more cytotoxic effect on the U87 cell line. The antibacterial activity of synthesized NP was studied against Streptococcus mutans bacterium through disk diffusion and microdilution method. Based on the outcomes of microdilution and disk diffusion assay and of the synthesized NP, Ag-dop-ZnO NP shows higher antibacterial activity against Streptococcus mutans than the pure NPs. Hence, the synthesized NPs can be suggested for disinfectant products and cancer treatment.

This paper presented the green synthesis of pure and 5% zinc doped cerium oxide nanoparticles (Zn-CeO2 NPs) by using the root extract of Prosopis farcta. Green synthesis is a method of synthesizing nanoparticles without the use of chemical solvents and is environmentally friendly and safe.The physic-chemical properties of the obtained nanoparticles were studied through the results of PXRD, UV-Vis, DRS, FESEM, EDX, and Raman techniques. The outcomes of EDX and PXRD confirmed the presence of doped zinc in the structure of cerium oxide. The particle sizes of pure and Zn-CeO2 NPs were 20 and 8 nm. Additionally, we evaluated the cytotoxic performance of synthesized nanoparticles on brain glioblastoma cells (U87), which resulted in displaying the stronger toxic effect of zinc doped nanoparticle when compared to pure cerium oxide nanoparticles. Therefore, it is indicated that zinc doped cerium oxide nanoparticles are capable of exhibiting a superior anti-cancer impact on U87 cells.

This study aimed to challenge the anticancer potency of pentagamavunone-1 (PGV-1) and obtain a new compound (Chemoprevention-Curcumin Analog 1.1, CCA-1.1) withimproved chemical and pharmacological properties.

CCA-1.1 was prepared by changing the ketone group of PGV-1 into a hydroxylgroup with NaBH4 as the reducing agent. The product was purified under preparative layerchromatography and confirmed with HPLC to show about 93% purity. It was tested for itssolubility, stability, and cytotoxic activities on several cancer cells. The structure of the productwas characterized using 1HNMR, 13C-NMR, FT-IR, and HR-mass spectroscopy.

Molecular docking analysis showed that CCA-1.1 performed similar or better interactionto NF-κB pathway-related signaling proteins (HER2, EGFR, IKK, ER-alpha, and ER-beta) andreactive oxygen species (ROS) metabolic enzymes (NQO1, NQO2, GSTP1, AKC1R1, andGLO1) compared with PGV-1, indicating that CCA-1.1 exhibits the same or better anticanceractivity than PGV-1. CCA-1.1 also showed better solubility and stability than PGV-1 in aqueoussolution at pH 1.0–7.4 under light exposure at room temperature. The cytotoxic activities ofCCA-1.1 against several (10) cancer cell lines revealed the same or better potency than PGV-1.

In conclusion, CCA-1.1 performs better chemical and anticancer properties thanPGV-1 and shows promise as an anticancer agent with high selectivity.

The genus Phlomis is a member of Lamiaceae (Labiatae) family. About 10 species of this genus, among more than 100 species, are endemic to Iran. Phlomis rigida Labill. can be used as antimicrobial, anti-inflammatory, wound healing and antioxidant in drug investigations, based on literature.

The aim of this study is to evaluate the composition, antioxidant, antibacterial and cytotoxic activity of essential oils and extract from leaves and flowers of P. rigida from Iran. The present study is the first research on P. rigida from Iran.

Essential oils of leaves and flowers of P. rigida were studied by GC-MS and GC-FID to evaluate the chemical compositions. DPPH free radical scavenging method was used to evaluate the antioxidant effect of leaves and flowers extracts. Antimicrobial properties of the essential oils and extracts were investigated against various microorganisms in brain heart infusion agar to evaluate the minimum inhibitory concentration. A brine shrimp test (BST) was done to study the cytotoxicity of methanol extracts and essential oils from leaves and flowers in different concentrations. The growth inhibitory effects of the methanol extract from leaves and flowers were assessed against four cancer cell lines including MCF-7, MDBK, HT-29 and A-549.

Essential oils analysis showed 34 compounds and the main compounds were (Z)-β-ocimene (25.6 %), isobornyl acetate (16.6 %), trans-verbenol (12.6 %) and α-pinene (7.6 %). As a result of analysis of methanol extracts from leaves, luteolin, luteolin-7-O-glucoside and rosmarinic acid were isolated and identification for the first time from P. rigida growing in Iran. Investigation of antibacterial properties of the essential oil of flowers also showed 16 mm diameters of inhibition zone against Proteus vulgaris.

The results of this study showed that the antibacterial effect of P. rigida essential oil could be due to the presence of its monoterpenes.

Soft corals of the genus Sinularia are well recognized as a rich source of steroidal compounds. These constituents have been reported as possessing antitumor, antimicrobial, and antiviral activities.

This study was designed to isolate and elucidate antibacterial and cytotoxic compounds from the soft coral Sinularia polydactila.

Structure elucidation of steroids was determined based on spectroscopic data through 1D and 2D NMR analyses and mass spectrometry, with the results compared to data in the literature. Antibacterial activity was determined using four human bacterial pathogens, namely B. subtilis (ATCC 6633), P. aeruginosa (ATCC 27853), S. aureus (ATCC 25923), and E. coli (ATCC 25922). Cytotoxic activity was evaluated using the human colon cancer cell HCT 116 and brine shrimp lethality assay (BSLA).

Two steroids (Compounds 1 - 2) were isolated from the Indonesian soft coral Sinularia polydactila. (22R,23R,24R)-22,23-methylene-24-methylcholest-6-en-5α,8α-epidioxy-3β-ol (1) and 5α,8α-Epidioxy-24(R)-methylcholesta-6,22-dien-3α-ol (2) showed moderate activity against colon carcinoma cancer HCT 116 at the concentrations of 24.8 and 27.3 μg/mL, respectively. Furthermore, compounds 1 and 2 showed cytotoxic activity using the brine shrimp lethality assay with the concentrations of 57.1 and 121.3 3 μg/mL, respectively. Compound 2 showed moderate activity against S. aureus and B. subtilis at the 250 μg/mL concentration.

Two steroids isolated from soft coral Sinularia polydactila were found to possess moderate cytotoxic and antibacterial activities.

Synthesis and investigation of pharmacological activity of novel compounds are time and money-consuming. However, computational techniques, docking, and in silico studies have facilitated drug discovery research to design pharmacologically effective compounds.

Experimental approach:

In this study, a series of quinazoline derivatives were applied to quantitative structure-activity relationship (QSAR) analysis. A collection of chemometric methods were conducted to provide relations between structural features and cytotoxic activity of a variety of quinazoline derivatives against breast cancer cell line. An in silico-screening was accomplished and new impressive lead compounds were designed to target the epidermal growth factor receptor (EGFR)-active site based on a new structural pattern. Molecular docking was performed to delve into the interactions, free binding energy, and molecular binding mode of the compounds against the EGFR target.

A comparison between different methods significantly indicated that genetic algorithm-partial least-squares were selected as the best model for quinazoline derivatives. In the current study, constitutional, functional, chemical, resource description framework, 2D autocorrelation, and charge descriptors were considered as significant parameters for the prediction of anticancer activity of quinazoline derivatives. In silico screening was employed to discover new compounds with good potential as anticancer agents and suggested to be synthesized. Also, the binding energy of docking simulation showed desired correlation with QSAR and experimental data.

Conclusion and implications:

 The results showed good accordance between binding energy and QSAR results. Compounds Q1</sub>-Q30 </sub>are desired to be synthesized and applied to in vitro evaluation.

This work is aimed to elucidate cytotoxic and apoptotic effects of Salvia syriaca essential oil and its chemical composition by GC-MS. The human colon cancer cells (Caco-2) were treated with different essential oil concentrations for 24 h. Crystal violet test was used to determine cell viability at 630 nm by using an ELISA reader. Apoptotic processes were measured by Annexin V-FITC Apoptosis Assay Kit. Germacrene D (21.77%), trans-β-ocimene (14.66%), β-pinene (9.07%), α-cadinol (8.19%) and α-pinene (6.50%) were the main components of oil determined by GC-MS. Moreover, we observed that the cytotoxic effect was increased with an increasing dose of essential oil. The EC50 value was calculated as 63.5 µg/mL. An increase in the percentage of apoptotic cells was observed after treatment of Caco-2 cells with S. syriaca essential oil revealed by image-based cytometry. A nearly 6-fold increase was found in annexin-positive cells after treatment. In terms of mRNA levels, RT-PCR analysis indicated that, although Bax and Caspase-3 were increased, Bcl-2 was decreased after oil treatment. According to our results, S. syriaca essential oil has promising phytochemicals that might be useful in cancer treatment due to their relatively cytotoxic and apoptotic activities in Caco-2 cells.

The development of effective anticancer drugs is a significant health issue. Previous studies showed that members of the benzimidazole family have anticancer effects on several cancers

The present study investigated the cytotoxic effect of flubendazole on A549 human lung cancer cells.

The A549 cells were treated with flubendazole at 1, 2, 5, and 10 µM concentrations for three days. Cell viability was measured by the MTT assay and Acridine orange staining. Also, the expressions of P62 and Beclin -1 were analyzed by qRT-PCR analysis.

Cell viability of A549 cells, in a concentration-dependent manner, showed significant differences between the treatment and control groups, and the IC50 value was determined to be 2 µM. Also, flubendazole reduced the expression of P62 and increased the expression of Beclin 1 in treated cells.

Flubendazole induces cell death in A549 cells in a dose and time-dependent manner and can offer new factors in lung cancer therapeutic strategies.

Many herbal remedies have been used in medical systems for the cure of diseases. One of these important applications is usage of them as cytotoxic agents for the treatment of cancers and tumors. Various studies have been conducted on several species of Caesalpinia genus including evaluation of antimicrobial, antitumor, anti-inflammatory, antipsoriatic, antidiabetic, antioxidant, antibacterial, immunomodulatory and hypoglycemic activities. Some reports have shown that these plants contain phytochemicals like polyphenols, glycosides, terpenoids, saponins and flavonoids.

The aim of this study was to find species of the Caesalpinia genus containing diterpene compounds with the structure cassane and norcassane with emphasis on cytotoxic properties.

In this study, keywords including Caesalpinia genus, cytotoxic and anticancer effects, and cassane and norcassane compounds were searched in Scopus and Science Direct databases.

Thirteen Caesalpinia species were investigated for phytochemical composition and biological effects. Different plant parts of the species including leaves, seeds, stems, roots and legumes contained diterpenes. Among these species, the cytotoxic effects on different cancer cell lines have been evaluated and some had significant cytotoxic effects.

Present study show that Caesalpinia genus has valuable cytotoxic activity but further studies are needed to investigate the active components and their possible development as new anticancer drugs.

Apiaceae fruits as common spices used for prevention of many chronic diseases including cancer.

The present study compared the biological effects of different fruits from various Apiaceae tribes to compare and find the fraction source(s) with potential characteristics for further investigation including cancer prevention.

Fruits of Apium graveolens L. (celery), Bunium persicum (Boiss.) B.Fedtsch. (black cumin), Petroselinum crispum (Mill.) Fuss (parsley), Pimpinella anisum L. (anise), Trachyspermum ammi (L.) Sprague (ajwain), Coriandrum sativum L. (coriander), Foeniculum vulgare Mill. (fennel), Anethum graveolens L. (dill), Heracleum persicum Desf. ex Fisch., C.A.Mey. & Avé-Lall. (Persian hogweed), Ferula assa-foetida L. (asafoetida), Cuminum cyminum L. (cumin) and Daucus carota L. (carrot) were extracted with 80 % methanol and fractionated by petroleum ether, chloroform, ethyl acetate and methanol, respectively. For different fractions and total extract of all 12 samples, cytotoxicity by brine shrimp test (BST) and MTT assay against cancer and normal cell (foreskin fibroblast cells), antioxidant effects by FRAP, and total phenols by Folin-Ciocalteu method were measured.

The general toxicity of ethyl acetate fractions (mean of data) was higher than others in the brine shrimp test (P < 0.05). The most cytotoxic fractions against colon carcinoma (HT-29), breast adenocarcinoma (MDA-MB-231) and alveolar basal epithelial adenocarcinoma (A549) cell lines were from Ammineae and Peucedaneae tribes while fruits fractions with high phenol contents and antioxidant powers were from Ammineae tribe.

The Apiaceae fruits have significant biological effects, therefore the isolation of phytochemical compounds from active fractions with cytotoxicity is suggested in future studies.

Neuroblastoma is one of the nervous system cancers, which approximately consists of 9% of childhood cancers. In this study, we evaluated the toxic effects of prenyl hydroxy coumarin derivatives on apoptosis of the neuroblastoma cell line N2A. N2a cells were cultured in DMEM medium, then the effects of different concentrations (0.75–200 μg/mL) of prenyl hydroxy coumarin derivatives during 24, 48, and 72 h were studied. Cell viability was quantified by MTT assay; apoptotic cells were determined using PI staining of DNA fragmentation by Flow cytometry (sub-G1 peak). The toxic effect of 3- farnesyl oxi coumarin in the N2A cell starts at 6.25 μg/ml and increases relatively depending on rising in concentration and time. The toxicity and apoptosis in 3- farnesyl and 6- farnesyl oxi coumarin is more than 3- Geranyl and 6-Geranyl oxi coumarin. Prenyl hydroxy coumarin induces peak sub-G1in flow cytometry compared to the control group, indicating prenyl hydroxy coumarin-induced toxicity, which is involved in apoptotic cell death. Different concentration of hydroxy coumarin derivatives (0.75-200) µg/mL in lymphocytes, did not induce any anti-proliferative effect in 24 h. In conclusion, prenyl hydroxy coumarin derivatives induce apoptotic effects in the N2A cell line. Thus prenyl hydroxy coumarin derivatives sound to be chemotherapeutic agents for the neuroblastoma cancer cells.