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1.
Bol. latinoam. Caribe plantas med. aromát ; 21(1): 1-40, ene. 2022. ilus, tab
Article in English | LILACS | ID: biblio-1370311

ABSTRACT

Cancer is an abnormal and uncontrolled growth of cells that spreads through cell division. There are different types of medicines available to treat cancers, but no drug is found to be fully effective and safe for humans. The major problem involved in the cancer treatments is the toxicity of the established drug and their side effects. Medicinal plants are used as folk medicines in Asian and African populations for thousands of years. 60% of the drugs for treating cancer are derived from plants. More than 3000 plants have anticancer activity. The present review aims at the study of a broad spectrum survey of plants having anticancer components for different type of cancers. This article consists of 364 medicinal plants and their different parts as potential Source of Anticancer Agents.


El cáncer es un crecimiento anormal y descontrolado de células que se disemina a través de la división celular. Hay diferentes tipos de medicamentos disponibles para tratar el cáncer, pero no se ha encontrado ningún medicamento que sea completamente efectivo y seguro para los seres humanos. El principal problema involucrado en los tratamientos del cáncer es la toxicidad del fármaco establecido y sus efectos secundarios. Las plantas medicinales se utilizan como medicinas populares en poblaciones asiáticas y africanas durante miles de años. El 60% de los medicamentos para el tratamiento del cáncer se derivan de plantas. Más de 3000 plantas tienen actividad anticancerígena. La presente revisión tiene como objetivo el estudio de un estudio de amplio espectro de plantas que tienen componentes anticancerígenos para diferentes tipos de cánceres. Este artículo consta de 364 plantas medicinales y sus diferentes partes como fuente potencial de agentes anticancerígenos.


Subject(s)
Plants, Medicinal/chemistry , Anticarcinogenic Agents/pharmacology , Phytochemicals/analysis , Cell Line, Tumor/drug effects , Phytochemicals/pharmacology
2.
Article | IMSEAR | ID: sea-210764

ABSTRACT

Geldanamycin (1) was isolated as a major compound from Streptomyces zerumbet W14. It was then used as a precursor tosynthesize two new geldanamycins: 17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5′-methoxytryptamine)-17-demethoxygeldanamycin (3). The cytotoxicity activity of these two new compounds was evaluated and comparedwith the cytotoxicity of compound 1. Cytotoxicity activity was evaluated against a normal cell line, and three cancercell lines using an 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) colorimetric assay. Thesolubility of these compounds was also determined. The solubility of compounds 2 and 3 in water was 290.69and 348.18 µM, higher than that of compound 1 by about 1.91 and 2.29 times, respectively. Compounds 2 and 3showed moderate cytotoxic activity on Vero and human cervical carcinoma cells with IC50 values of >200.00 µg/ml. The strongest cytotoxicity of compound 3 was observed in human breast carcinoma cells (MCF-7) and humanhepatocellular carcinoma cell line (HepG2) cells with IC50 values of 82.50 and 114.35 µg/ml, respectively, while theIC50 values of compound 2 against MCF-7 and HepG2 cells were 105.62 and 124.57 µg/ml, respectively. The findingsshowed that these new geldanamycin derivatives exhibited selective cytotoxicity toward some cancer cells at a lowerconcentration. Therefore, future studies on these compounds could be useful for the management of some cancers

3.
J Biosci ; 2020 Mar; : 1-12
Article | IMSEAR | ID: sea-214312

ABSTRACT

Non-small-cell lung cancer (NSCLC) is a complex disease which is influenced by multiple factors. Recentstudies demonstrated that long non-coding RNA (lncRNA) MIAT was involved in tumor metastasis. However,the underlying mechanism of MIAT in NSCLC remains largely unknown. In this study, MIAT, miR-139-5pand MMP2 expression were measured by quantitative reverse transcriptase PCR (QRT-PCR) or Westernblotting, respectively, and we found the expression of MIAT and MMP2 were elevated, while miR-139-5p wasdecreased in NSCLC tissues and cell lines. Transwell assay showed MIAT and MMP2 functioned as anoncogene to induce cell migration and invasion in NSCLC, but miR-139-5p served as a tumor suppressor inNSCLC to inhibit cell migration and invasion. Besides that, in vivo experiments also indicated MIAT deletioninhibited tumor growth. The relationship between miR-139-5p and MIAT or MMP2 was then confirmed byLuciferase reporter assay, and the results showed that MIAT directly interacted with miR-139-5p and miR-139-5p targetedly suppressed MMP2 in NSCLC cells. Furthermore, expression analysis showed that MIAT indirectly regulated MMP2 by sponging miR-139-5p. Finally, rescue assay suggested that miR-139-5p restorationreversed MIAT-overexpression-induced promotion on the migration and invasion of NSCLC cells. In conclusion, our results demonstrated that lncRNA MIAT modulated the migration and invasion of NSCLC byregulating miR-139-5p and MMP2.

4.
Article | IMSEAR | ID: sea-210698

ABSTRACT

Cancer is the most dreadful disease and the second main cause of death worldwide. The continuous developments havebeen going on in order to design potent molecules such that this leading cause of death can be dealt with. In order todecrease the level of toxicity and to improve the selectivity of drugs toward cancer targets, the development of hybridmolecules has become the center of research, and scientists are doing timeless efforts to generate such a hybrid whichhas got no comparison with the previous developments. The heterocyclic moiety Uracil and many of its derivativeswere already exposed as promising anticancer agents. Moreover, coupling of Uracil and 5-Fluorouracil (5-FU) withdifferent pharmacophores has been proven to be an excellent strategy against cancer. Hence, the present review is aneffort to collectively represent all the earlier and recent developments of Uracil and 5-FU hybrids reported to have asignificant anticancer profile. Expectantly, we can assure that this article can serve as the basis for further developmentsin Uracil and 5-FU hybrids and will surely motivate the medicinal chemists for producing unique anticancer drug

5.
Article in Chinese | WPRIM | ID: wpr-846652

ABSTRACT

Objective: To study bakuchiol and its derivatives of cyclohexane soluble part in 70% ethanol aqueous extract of Psoraleae Fructus and their inhibition on nitric oxide (NO) production in lipopolysaccharides (LPS)-activated murine macrophage RAW 264.7 cell lines. Methods: The compounds were separated and purified by silica gel column and high performance liquid chromatographies, and their structures were determined by spectroscopic data analyses. Using LPS-activated RAW 264.7 cell line models in vitro, all of the isolated compounds were evaluated for the inhibition against NO production. Results: Twelve compounds were obtained and identified as bakuchiol (1), 12,13-dihydro-12,13-epoxybakuchiol (2), Δ3,2-hydroxylbakuchiol (3), 12-oxobakuchiol (4), psoracorylifol B (5), psoracorylifol C (6), (12’S)-bisbakuchiol C (7), Δ1,3-bakuchiol (8), 13-methoxyisobakuchiol (9), bisbakuchiol B (10), bisbakuchiol A (11), and 12,13-dihydro-12,13-dihydroxybakuchiol (12), respectively. For the inhibition of NO production in the LPS-activated RAW 264.7 cell line model, a positive inhibitor, L-N6-(1-iminoethyl)-lysine (L-NIL), was used and showed the half maximal inhibitory concentration (IC50) value of (10.29 ± 1.10) μmol/L. The IC50 values of the assayed compounds 1, 3, 5, 10 and 11 were all more than 50 μmol/L, compounds 8, 9 and 12 were comparable to that of L-NIL, whereas the IC50 values of compounds 2, 4 and 7 were less than that of the positive inhibitor with statistically significance. Conclusion: Compound 4 is a new natural product. The results of the bioactivity assays indicated that compounds 2, 4, 7, 8, 9 and 12 are potential anti-inflammatory agents.

6.
Article in English | WPRIM | ID: wpr-823249

ABSTRACT

@#Aims: Urinary tract infection (UTI) is a common infection caused by many virulent bacteria. Multidrug resistance (MDR) by bacteria represents a major therapeutic challenge worldwide. MRD bacteria have different mechanisms to avoid antibiotics; one of them is horizontal gene transfer. Such genes, encoding antimicrobial resistance, are easily transferred from one bacterium to another. Magnesium and calcium chloride (MgCl2 and CaCl2) have an effect on the permeability of bacterial cell membrane. We aimed these chemical materials could increase the antibiotics efficiency on multidrug resistance bacteria. 250 UTI specimens were collected to isolate multidrug resistant bacteria. Depending on antibiotics resistance, we selected three species of virulent bacteria: Escherichia coli, Staphylococcus aureus and Proteus mirabilis. Then, we tested the effect of MgCl2 and CaCl2 on their antibiotics resistance. Methodology and results: The results showed that percentage of E. coli in UTI infection is the highest (45%), while Enterococcus faecalis is the lowest (3%). The effect of MgCl2 and CaCl2 on bacterial antibiotics resistance has been tested using different types of antibiotics. The findings showed that MgCl2 has significant effect to aid antibiotics against bacteria. In particular, nalidixic acid has shown more efficiency against E. coli and S. aureus but not P. mirabilis. Using different concentrations of CaCl2 increased the efficiency of gentamycin, amoxicillin and trimethoprim against S. aureus, while has increased the efficiency of ampicillin and nalidixic acid against E. coli. However, CaCl2 has no effect on the efficiency of antibiotics against P. mirabilis. In addition, MgCl2, and CaCl2 had no toxic effects in both T24 and 5637 urinary bladder cell lines. Finally, plasmids were isolated from these species to detect any antimicrobial resistance gene such as qnr-A. Conclusion, significance and impact of study: MDR distribution in the worldwide was increased, we highly recommend the avoidance of the random antibiotic usages. The salts CaCl2 and/or MgCl2 can be used at specific concentration to enhance the antibiotics permeability and therefore to decrease the antibiotic resistance.

7.
Article in Chinese | WPRIM | ID: wpr-815376

ABSTRACT

Objective@#To explore the effect of circ_0001273 on the proliferation, migration and invasion of oral squamous cell carcinoma(OSCC) cells and to provide a relevant research basis for the use of targeted therapy in OSCC. @*Methods@#Data from twelve patients with a clinical diagnosis of OSCC were collected from tumor specimens and adjacent tissues. qRT-PCR was used to detect the expression levels of circ_0001273, circ_0018569, circ_0027152, and circ_0001273 which had the highest difference in expression in cancer and adjacent tissues was selected. siRNA was used for the knockdown of circ_0001273 in two types of OSCC cell lines, UM1 and CAL27, and the effects on the proliferation, migration, and invasion of UM1 and CAL27 cells were measured by MTS and Transwell experiments, respectively. @*Results@#The expression of circ_0001273 was abnormally increased in the 12 OSCC tissues (P < 0.05). After knocking down circ_0001273 in UM1 and CAL27 cells, the proliferation, migration and invasion abilities of UM1 and CAL27 cells were significantly reduced (P < 0.05).@*Conclusion@#The knockdown of circ_0001273 can inhibit the proliferation, migration and invasion of OSCC cells.

8.
J. appl. oral sci ; 28: e20190558, 2020. graf
Article in English | LILACS, BBO | ID: biblio-1101249

ABSTRACT

Abstract Objective Ameloblastoma is a representative odontogenic tumor comprising several characteristic invasive forms, and its pathophysiology has not been sufficiently elucidated. A stable animal experimental model using immortalized cell lines is crucial to explain the factors causing differences among the subtypes of ameloblastoma, but this model has not yet been disclosed. In this study, a novel animal experimental model has been established, using immortalized human ameloblastoma-derived cell lines. Methodology Ameloblastoma cells suspended in Matrigel were subcutaneously transplanted into the heads of immunodeficient mice. Two immortalized human ameloblastoma cell lines were used: AM-1 cells derived from the plexiform type and AM-3 cells derived from the follicular type. The tissues were evaluated histologically 30, 60, and 90 days after transplantation. Results Tumor masses formed in all transplanted mice. In addition, the tumors formed in each group transplanted with different ameloblastoma cells were histologically distinct: the tumors in the group transplanted with AM-1 cells were similar to the plexiform type, and those in the group transplanted with AM-3-cells were similar to the follicular type. Conclusions A novel, stable animal experimental model of ameloblastoma was established using two cell lines derived from different subtypes of the tumor. This model can help clarify its pathophysiology and hasten the development of new ameloblastoma treatment strategies.


Subject(s)
Animals , Female , Mice , Ameloblastoma/pathology , Disease Models, Animal , Neoplasms, Experimental/pathology , Proteoglycans , Time Factors , Immunohistochemistry , Cells, Cultured , Reproducibility of Results , Collagen , Laminin , Cell Line, Tumor , Green Fluorescent Proteins/analysis , Drug Combinations
9.
Braz. arch. biol. technol ; 63: e20190408, 2020. tab
Article in English | LILACS | ID: biblio-1132168

ABSTRACT

Abstract Propolis is a resinous substance collected and processed by Apis mellifera from parts of plants, buds and exudates. In Minas Gerais (MG) state, Brazil, green propolis is produced from the collection of resinous substance found in shoot apices of Baccharis dracunculifolia. This paper aims to investigate the chemical composition and in vitro antioxidant, anti-Helicobacter pylori, antimycobacterial and antiproliferative activities of essential oil (EO) from Brazilian green propolis (BGP-EO). The oil showed high antibacterial activity against H. pylori (MIC = 6.25 µg/mL), Mycobacterium avium (MIC = 62.5 µg/mL) and M. tuberculosis (MIC = 64 µg/mL). Its antioxidant activity was evaluated in vitro by both DPPH (IC50 = 23.48 µg/mL) and ABTS (IC50 = 32.18 µg/mL) methods. The antiproliferative activity in normal (GM07492A, lung fibroblasts) and tumor cell lines (MCF-7, HeLa and M059J) was analyzed by the XTT assay. BGP-EO showed inhibition of normal cell growth at 68.93 ± 2.56 µg/mL. Antiproliferative activity was observed against human tumor cell lines, whose IC50 values were 56.17, 66.43 and -65.83 µg/mL for MCF-7, HeLa and M059J cells, respectively. Its major constituents, which were determined by GC-FID and GC-MS, were carvacrol (20.7 %), acetophenone (13.5 %), spathulenol (11.0 %), (E)-nerolidol (9.7 %) and β-caryophyllene (6.2 %). These results showed the effectiveness of BGP-EO as a natural product which has promising biological activities.


Subject(s)
Propolis/chemistry , Anti-Infective Agents/pharmacology , Antioxidants/pharmacology , Brazil , Oils, Volatile/therapeutic use , Helicobacter pylori/drug effects , Mycobacterium avium/drug effects , Mycobacterium tuberculosis/drug effects
10.
Biol. Res ; 53: 13, 2020. tab, graf
Article in English | LILACS | ID: biblio-1100919

ABSTRACT

BACKGROUND: Gallbladder cancer (GBC) is the most common tumor of the biliary tract. The incidence of GBC shows a large geographic variability, being particularly frequent in Native American populations. In Chile, GBC represents the second cause of cancer-related death among women. We describe here the establishment of three novel cell lines derived from the ascitic fluid of a Chilean GBC patient, who presented 46% European, 36% Mapuche, 12% Aymara and 6% African ancestry. RESULTS: After immunocytochemical staining of the primary cell culture, we isolated and comprehensively characterized three independent clones (PUC-GBC1, PUC-GBC2 and PUC-GBC3) by short tandem repeat DNA profiling and RNA sequencing as well as karyotype, doubling time, chemosensitivity, in vitro migration capability and in vivo tumorigenicity assay. Primary culture cells showed high expression of CK7, CK19, CA 19-9, MUC1 and MUC16, and negative expression of mesothelial markers. The three isolated clones displayed an epithelial phenotype and an abnormal structure and number of chromosomes. RNA sequencing confirmed the increased expression of cytokeratin and mucin genes, and also of TP53 and ERBB2 with some differences among the three cells lines, and revealed a novel exonic mutation in NF1. The PUC-GBC3 clone was the most aggressive according to histopathological features and the tumorigenic capacity in NSG mice. CONCLUSIONS: The first cell lines established from a Chilean GBC patient represent a new model for studying GBC in patients of Native American descent.


Subject(s)
Humans , Animals , Male , Middle Aged , Antigens, Tumor-Associated, Carbohydrate/genetics , Indians, South American/genetics , Gallbladder Neoplasms/genetics , Ascitic Fluid/metabolism , Tumor Cells, Cultured , Carcinogenicity Tests , Chile , DNA Fingerprinting , Tumor Suppressor Protein p53/genetics , Cisplatin/pharmacology , Mice, Inbred NOD , Clone Cells/drug effects , Clone Cells/metabolism , Sequence Analysis, RNA , Receptor, ErbB-2/genetics , Genes, erbB-2/genetics , Gene Expression Profiling , Cell Line, Tumor/drug effects , Cell Line, Tumor/metabolism , Deoxycytidine/analogs & derivatives , Deoxycytidine/pharmacology , Epithelial Cells/metabolism , Keratin-19/genetics , Keratin-7/genetics , Carcinogenesis/genetics , Gallbladder Neoplasms/metabolism , Antineoplastic Agents/pharmacology
11.
Article | IMSEAR | ID: sea-206274

ABSTRACT

In the world cancer is the major cause of death. Adansonia digitata L is commonly called as baobab belongs to Family Bombacaceae. Due to the high cost and toxic side effects like Bone marrow suppression, hepatotoxicity, nephrotoxicity, Immunosuppression, teratogenicity etc. of chemotherapeutic agents. So, for the proper controlling on cancer the trends of people are moving towards natural therapies. In light to above, in present research A. digitata L is selected for evaluation of in-vitro anticancer activity based on its reported phytoconstituents of fruit and quantitation of active principle of it. The extracts of fruit pulp, seed, and its combination were obtained using solvents like water, ethanol and n-hexane by maceration technique (Aqueous) and Soxhlet extraction method (organic). This extracts were used for further research possesses phytochemical constituents like Carbohydrates, tannins, Saponins, vitamins, alkaloids, terpenoids, phenol, glycoside flavonoids, steroids, etc. in-vitro antioxidant activity were evaluated via free scavenging assay by using DPPH assay method. Further in-vitro anticancer activity was evaluated against three human cancer cell lines MCF-7 (breast cancer cell line), Hep-G2 (liver cancer cell line) and COLO-205 (colon cancer cell line) using Brine Shrimp Lethality Assay (BSLA), Tryphan Blue Dye Cell Exclusion Assay (TBDCEA) and MTT assay. The quantitation of active ingredients Vit. C and Squalene from extracts was done by using titration method and HPLC method respectively. Formulation possesses highest percent antioxidant capacity (49.36). In BSLA formulation possesses highest rate of percent mortality than other extracts. In TBCE assay and in MTT assay formulation gives more significant effect in Hep-G2 liver cancer cell line than remaining cell lines. These findings introduce A. digitata L as potentially useful as anti-cancer agent. Further research is required to elucidate its specific mechanism of action and exact active principle responsible for action.

12.
Article | IMSEAR | ID: sea-210416

ABSTRACT

In the present work, we have designed short chain α-helical linear and cyclic peptide from cecropin B having samecharge, hydrophobicity, and helicity. The designed compounds were synthesized by using solution phase method.Elucidation of structure of newly synthesized peptides was done by proton nuclear magnetic resonance, Carbon-13nuclear magnetic resonance, Fourier-transform infrared spectroscopy, Fast atom bombardment mass spectrometry,and elemental analysis. Furthermore, the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltratrazolium bromide assay wasperformed for cytotoxicity of synthesized compounds against Dalton’s lymphoma ascites (DLA), Ehrlich’s ascitescarcinoma (EAC), and Michigan Cancer Foundation-7 cell lines using 5-FU as a reference compound. Biologicalevaluation showed that short chain cyclicpeptides were more potent than linear peptides against EAC and DLA celllines.

13.
Article | IMSEAR | ID: sea-195899

ABSTRACT

Background & objectives: Chikungunya virus (CHIKV), a mosquito-borne arthritogenic virus causes infections ranging from febrile illness to debilitating polyarthralgia in humans. Re-emergence of the virus has affected millions of people in Africa and Asia since 2004. During the outbreak, a new lineage of the virus has evolved as an adaptation for enhanced replication and transmission by Aedes albopictus mosquito. A study was designed to compare the susceptibility of four vertebrate cell lines, namely Vero E6 (African green monkey kidney), BHK-21 (Baby hamster kidney), RD (human rhabdomyosarcoma), A-549 (human alveolar basal epithelial cell) and C6/36 (Ae. albopictus) to Asian genotype and two lineages of East, Central and South African (E1:A226 and E1:A226V) of CHIKV. Methods: One-step growth kinetics of different CHIKV strains was carried out in the above five cell lines to determine the growth kinetics and virus yield. Virus titre was determined by 50 per cent tissue culture infectious dose assay and titres were calculated by the Reed and Muench formula. Growth and virus yield of the three strains in Ae. aegypti mosquitoes was studied by intrathoracic inoculation and virus titration in Vero E6 cell line. Results: Virus titration showed Vero E6, C6/36 and BHK-21 cell lines are high virus yielding with all the three lineages while RD and A-549 yielded low virus titres. C6/36 cell line was the most sensitive and yielded the maximum titre. Ae. aegypti mosquitoes, when inoculated with high titre virus, yielded an almost equal growth with the three strains while rapid growth of E1:A226V and Asian strain was observed with 1 log virus. Interpretation & conclusions: C6/36 cell line was found to be the most sensitive and high yielding for CHIKV irrespective of lineages while Vero E6 and BHK-21 cell lines yielded high titres and may find application for vaccine/diagnostic development. Infection of Ae. aegypti mosquitoes with the three CHIKV strains gave almost identical pattern of growth.

14.
Article | IMSEAR | ID: sea-210591

ABSTRACT

Longan (Dimocarpus longan Lour.) belongs to Sapindaceae family. We examined the antiproliferative activity oflongan leaf extracts against cancer-derived cell cell lines in vitro. The tested samples were water extract, ethanolextract, n-hexane fraction, ethyl acetate fraction, and water fraction of longan leaf. Cytotoxicity test is against brineshrimps that was screened using Brine Shrimp Lethality Test. Antiproliferative activity assay on WEHI-164 cells(mouse fibrosarcoma cancer cell), THP-1 cells (human peripheral blood acute monocyte cell), and vero cells (noncancer or normal cell) that was conducted using hemocytometer with Trypan Blue Dye exclusion. The 50% lethalityconcentration (LC50) value of water extract, ethanol extract, n-hexane fraction, ethyl acetate fraction, and waterfraction were 854.64, 305.81, 446.55, 1313.44, and 1621.8 µg/ml. Ethanol extract exhibited significant cytotoxicdue to the lowest LC50 value. Ethanol extract was then used for further examination. The highest antiproliferativeactivity was achieved 44.93% by 600 µg/ml ethanol extract on WEHI-164 and 57.45% by 500 µg/ml ethanol extracton THP-1. It was significantly equal to doxorubicin antiproliferative activity. Ethanol extract dose had low effect tovero cells. This present study confirmed that the longan leaf ethanol extract possess marked antiproliferative activityon cancer-derived cell lines.

15.
Journal of Medical Postgraduates ; (12): 1150-1157, 2019.
Article in Chinese | WPRIM | ID: wpr-818158

ABSTRACT

Objective The human glioblastoma (GBM) U87 cell line is employed as a model for studying the heterogeneity of GBM. This study was to examine the phenotypic profiles and genetic backgrounds of different monoclonal cells derived from the human GBM U87 cell line and explore the molecular mechanisms underlying the phenotypic difference. Methods Using the finite dilution method labeled with 5(6)-carboxyfluorescein diacetate N-hydroxy succinimidyl ester (CFSE), we constructed the monoclonal cell lines CF5 and G11 with typical morphological characteristics derived from the human GBM U87 cell line and identified them by short tandem repeat (STR). We detected the proliferation of the cells by CCK8 assay, EdU incorporation and colony-formation assay, their self-renewal capability by tumor sphere formation assay, their adhesion ability by immunofluorescence and CCK8 adhesion assay, their invasion ability with a 3D culture model, and their sensitivity to chemotherapeutic agents by Annexin V/PI double-staining flow cytometry. We performed transcriptome sequencing and bioinformatics analysis on the genetic profiles and determined the mRNA expressions of the representative differential genes in the enriched pathway by real-time quantitative PCR (qRT-PCR). Results The CF5 and G11 monoclonal cell lines morphologically typical of U87 were successfully constructed, the former small, short and thick, while the latter big, long and thin. Compared with the U87 and G11 cell lines, the CF5 cells showed a significantly higher proliferation ability (P < 0.01), though higher in the U87 than in the G11 cell line, a higher proportion of EdU-positive cells (0.35 ± 0.03 and 0.44 ± 0.03 vs 0.54 ± 0.05, P < 0.01), though higher in the U87 than in the G11 cell line, and a higher tumor-sphere formation ability (P < 0.01), though higher in the U87 than in the G11 cell line. In comparison with the U87 and CF5 cell lines, the G11 cells exhibited remarkably higher abilities of adhesion (P < 0.01) and invasion (P < 0.05), though both higher in the U87 than in the CF5 group. Totally, 159 genes were down-regulated and 303 up-regulated in the CF5 cells compared with those in the U87 and G11 cells, while 281 were down-regulated and 116 up-regulated in the G11 cells compared with those in the CF5 and U87 cells. The CF5 and G11 cells manifested the highest enrichment in the extracellular matrix-associated pathways, which were shown to be closely associated with the invasiveness and drug-resistance of the tumor. Conclusion We successfully constructed human GBM U87-derived monoclonal cell lines CF5 and G11 with different morphological features, phenotypic profiles and genetic backgrounds, which has paved the ground for further studies of the heterogeneity of GBM.

16.
Article in English | WPRIM | ID: wpr-780650

ABSTRACT

Aims@#The aim of this study was to evaluate some chemical properties and the cytotoxic effect of aqueous and ethanolic crude polysaccharides extracted from five Lentinus sp. on human cancer cell lines. It was hypothesized that other species of the genus Lentinus could show the pharmacological actions as presence in Lentinus edodes, especially anticancer properties. @*Methodology and results@#Crude extracts of dried fruit bodies and mycelia from L. edodes, Lentinus sajor-caju, Lentinus swartzii, Lentinus squarrosulus and Lentinus velutinus were extracted using two solvents, hot water and 95% ethanol, and evaluated for their total carbohydrates, proteins, reducing sugar, phenol contents, and cytotoxicity. The yield of crude extracts was 33.6-205.3 mg/g dry weight of a sample. Cytotoxicity was determined with 10 mg/mL of crude aqueous and 1 mg/mL of crude ethanolic extracts by using the [3-(4,5-dimethylthiazol-2-yl)-2, 5- diphenyltetrazolium bromide] (MTT) method. All extracts showed non-cytotoxicity against the normal cell lines, LLC-MK2 and L929 cells. While, the extracts of L. edodes, L. sajor-caju, L. squarrosulus and L. velutinus displayed the cytotoxicity against the human cancer cell lines. @*Conclusion, significance and impact of study@#The crude aqueous and ethanolic extract from fruit bodies of L. velutinus and the ethanolic extract from fruit bodies of L. sajor-caju and L. squarrosulus displayed the adverse effect against the human cancer cell lines. Hence, these extracts are a potential source of bioactive compounds for cancer treatment.

17.
Chinese Journal of Hematology ; (12): 204-208, 2019.
Article in Chinese | WPRIM | ID: wpr-804918

ABSTRACT

Objective@#To investigate the effects of artesunate combined with bortezomib on the proliferation, apoptosis and autophagy of human acute myeloid leukemia cell lines MV4-11, and its mechanisms.@*Methods@#MTT method was used to determine the anti-proliferation effect of different concentrations of artesunate, bortezomib and their combination on MV4-11 cells. The cell apoptosis were analyzed by flow cytometry. The expression of cleaved-Caspase-3, Bcl-2 family protein (Bcl-2, Mcl-1, Bim, Bax) and autophagy-related protein LC3B were assayed by Western blot.@*Results@#Artesunate displayed a proliferation inhibition effect on MV4-11 with dose- and time-dependent manner, the IC50 of artesunate on MV4-11 after 48 hours was 1.44 μg/ml. Bortezomib displayed a proliferation inhibition effect on MV4-11 with dose-dependent manner, the IC50 of bortezomib on MV4-11 after 48 hours was 8.97 nmol/L. The combination of artesunate (0.75, 1.0 μg/ml) and Bortezomib (6, 8 nmol/L) showed higher inhibition on MV4-11 than artesunate or bortezomib alone in the same concentration gradient after 48 hours (P<0.05) . The cooperation index of the two drugs were all less than 1. The 48 h apoptotic rate of artesunate (1.5 μg/ml) on MV4-11 was (15.27±2.18) %, (19.85±3.23) % of bortezomib (8 nmol/L) , (81.67±5.96) % of combination of the two drugs, significantly higher than the single group (P<0.05) . When combination of the two drugs on MV4-11 after 24 hours, the levels of pro-apoptotic protein Bim and the cleaved activation of Caspase-3 and autophagy-related protein LC3B were up-regulated and the anti-apoptotic protein Bcl-2 expressions was down-regulated.@*Conclusion@#Combination of artesunate with bortezomib shows a significant synergistic effects on proliferation, apoptosis and autophagy of MV4-11 cell lines, which may be associated with Bcl-2 family proteins expression.

18.
Rev. bras. farmacogn ; 28(1): 27-33, Jan.-Feb. 2018. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-898736

ABSTRACT

ABSTRACT Screening of medicinal plants from Iranian flora against human cancer cell-lines have shown that an hexane extract from roots of Salvia sahendica Boiss. & Buhse, Lamiaceae, is active against human cervical cancer (HeLa) and colorectal adenocarcinoma (Caco-2) cell-lines at the test concentration of 100 µg/ml (100% inhibition). Cytotoxicity of the extract was localized with the aid of HPLC-time-based activity profiling adapted to the tetrazolium colorimetric bioassay. Four abietane-type diterpenoids in active time-windows were identified as cytotoxic compounds namely: sahandone (1), sahandol (2), 12-deoxy-salvipisone (3) and sahandinone (4). Compound 1 showed the highest toxicity against HeLa cells (IC50 = 5.6 ± 0.1 µg/ml), which was comparable with betulinic acid (IC50 = 4.3 ± 1.2 µg/ml), the positive control. Compound 2 was active against the HeLa cells (IC50 = 8.9 ± 0.7 µg/ml) but not the Caco-2 cell-line. Compounds 1, 3 and 4 exhibited moderate activity (IC50 = 22.9-41.4 µg/ml) against the Caco-2 cells. This study reveals that the HeLa cells are more sensitive to all tested compounds than the Caco-2 cells. In silico molecular docking study showed a rigid binding of the compounds to tyrosine kinase pp60src, and proved their cytotoxic activity.

19.
Acta Pharmaceutica Sinica B ; (6): 252-260, 2018.
Article in English | WPRIM | ID: wpr-690913

ABSTRACT

In the present study, total membrane proteins from tumor cell lines including HepG2, Hep3B2, H226, Ovcar3 and N87 were extracted and digested with LysC and trypsin. The resulting peptide lysate were pre-fractionated and subjected to untargeted quantitative proteomics analysis using a high resolution mass spectrometer. The mass spectra were processed by the MaxQuant and the protein abundances were estimated using total peak area (TPA) method. A total of 6037 proteins were identified, and the analysis resulted in the identification of 2647 membrane proteins. Of those, tumor antigens and absorption, metabolism, disposition and elimination (ADME) proteins including UDP-glucuronosyltransferase, cytochrome P450, solute carriers and ATP-binding cassette transporters were detected and disclosed significant variations among the cell lines. The principal component analysis was performed for the cluster of cell lines. The results demonstrated that H226 is closely related with N87, while Hep3B2 aligned with HepG2. The protein cluster of Ovcar3 was apart from that of other cell lines investigated. By providing for the first time quantitative untargeted proteomics analysis, the results delineated the expression profiles of membrane proteins. These findings provided a useful resource for selecting targets of choice for anticancer therapy through advancing data obtained from preclinical tumor cell line models to clinical outcomes.

20.
Article in Chinese | WPRIM | ID: wpr-852059

ABSTRACT

Objective: To study the chemical constituents of 95% ethanol aqueous extract of Chuanxiong Rhizoma and the bioactivities of inhibition on nitric oxide (NO) production in lipopolysaccharides (LPS)-activated murine macrophage RAW264. 7 and mouse microglia BV2 cell lines. Methods: The compounds were separated and purified by silica gel column and high performance liquid chromatographies, and their structures were determined by spectroscopic data analysis. Using LPS-activated RAW264. 7 and BV2 cell line models in vitro, all of the isolated compounds were evaluated for the inhibition against NO production. Results: Three butylphthalide derivatives were obtained and identified as Z-3', 8', 3'a, 7'a-tetrahydro-6, 3', 7, 7'a-diligustilide-8'-one (1), Z, Z'-3.3'a, 7. 7'a-diligustilide (2), and chuanliguspirolide (3), respectively. For the inhibition of NO production in the LPS-activated two cell lines, the half inhibitory concentration (IC50) values of compounds 1-3 and indomethacin as a positive control drug in RAW 264. 7 cell line model were (31.60 ± 2.62), (21.20 ± 0.61), (30.12 ± 2.90), and (54.62 ± 7.53) μmol/L, respectively, while IC50 values of compounds 1-3 and curcumin as a positive control drug in BV2 cell line model were (21.99 ± 4.40), (15.43 ± 1.34), (12.20 ± 3.40), and (10.58 ± 1. 41) μmol/L, respectively. Conclusion: Compound 3 named as chuanliguspirolide is a new one. The results of bioactivity assays indicated that compounds 1-3 are potential anti-inflammatory agents.

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