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1.
Saudi J Biol Sci ; 28(1): 417-426, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33424325

RESUMO

Antibacterial and cytotoxic activities of Euphorbia balsamifera, fractions and pure compounds were evaluated. The cytotoxic assays for HCT116, HePG2 and MCF7 showed a significant IC50: 54.7 and 76.2 µg/mL of non-polar fraction "n-hexane" against HCT116 and HePG2, respectively. Antibacterial results revealed that plant fractions exhibited significant potential against the tested pathogens than the total extract where n-butanol and ethyl acetate fractions showed significant antibacterial activity (P < 0.05) against tested bacterial strains. Isolation and structure determination of compounds from n-hexane and n-butanol fractions were performed. From n-hexane fraction, 29-nor-cycloartanol (1), lanost-8-en-3-ol (2a), cycloartanol (2b) and kampferol-3,4'-dimethyl ether (3) were isolated and structurally identified, along with 24 compounds were tentatively identified by GC-MS. From the polar n-butanol fraction, 4-O-ß-D-glucopyranosyl-2-hydroxy-6-methoxyacetophenone (4), 4-O-α-L-rhamnosyl-(1 â†’ 6)-ß-D-glucopyranosyl-2-hydroxy-6methoxy-acetophenone (5), quercetin-3-O-glucopyranoside (6) and isoorientin (7) were assigned. Structures of the obtained compounds were determined by nuclear magnetic resonance (NMR) spectroscopy and mass spectrometry. Except compounds 1 and 5, all reported compounds announced antibacterial efficiency. Compound 2 showed selectively the highest activity against Enterococcus faecalis (22 ± 0.13 mm), meanwhile 4-O-ß-D-glucopyranosyl-2-hydroxy-6-methoxyacetophenone (4) showed broadly the highest antibacterial activity with MIC of 1.15-1.88 mg/mL against the test Gram-positive and Gram-negative bacteria. Cytotoxic assays indicated that kampferol-3,4'-dimethyl ether (3) exhibited the highest activity with matching IC50 values to doxorubicin; 111.46, 42.67 and 44.90 µM against HCT116, HePG2 and MCF7, respectively, however, it is toxic on retina normal cell line RPE1.

2.
Bioorg Med Chem Lett ; 25(7): 1398-402, 2015 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-25765907

RESUMO

A series of 2,5-disubstituted-1,3,4-thiadiazole derivatives 5a-5l, 7a-7e and 9 have been synthesised and screened for in vitro antimycobacterial activity against Mycobacterium smegmatis MC-155. In addition these compounds have also been screened for cytotoxic activity against cancer cell lines HT-29, MDA-MB-231 by MTT colorimetric assay. The compounds are well characterized by spectral analysis viz. (1)H NMR, (13)C NMR, FT-IR, mass and HRMS. Screening results indicate that compounds 5g, 7a possess good antitubercular activity with MIC value 65.74 and 40.86, respectively, compounds 5g, 7a, 7b, 7d, 7e and 9 displayed promising cytotoxic activity against the cell lines tested. 5g and 7a stand out to be potent antimycobacterial and anticancer agents among the tested series. Further the title compounds were also tested on human normal cells HEK293T and are found to be safer with lesser cytotoxicity. It is interesting to observe that compound 5g has come out to be safer, potent anticancer and antimycobacterial agent.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Mycobacterium smegmatis/efeitos dos fármacos , Antibacterianos/síntese química , Antibacterianos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cristalografia por Raios X , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células HEK293 , Células HT29 , Humanos , Testes de Sensibilidade Microbiana , Modelos Moleculares , Estrutura Molecular , Relação Estrutura-Atividade
4.
China Oncology ; (12)2001.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-675443

RESUMO

Purpose:To evaluate the feasibility, advantages and disadvantages of chemosensitivity test of human gastric cancer using MTT assay with short term culture tumor cells contaminated by nonmalignant cells compared with purifiedly primary culture tumor cells.Methods:Fifty nine fresh samples from patients with gastric cancer were obtained from operating rooms. Chemosensitivity results were provided by the MTT assay with short term culture cells. The primary culture cells were purified by means of a series of methods such as repeated cell attachment, differential trypsinization and natural purification which removed fibroblasts and other nonmalignant cells. The same MTT assay was conducted using purified cells. Chemosensitivity results between short term method and purification method were compared for seven antitumor drugs. Results:The success rate of short term method using the MTT assay for chemosensitivity testing was 81 4% (48 of 59 patients),and for the purification method it was 50.8(30 of 59 patients). The average was 20.2?9.5 days when primary cells were cultured into purified cancer cells. The optical density ( A ) value correlated directly with the the number of tumor cells with the two methods( P

5.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-581566

RESUMO

We used MTT assay to test the cellular cytotoxicity ( NK, LAK, CTL, Macrophage), cytokine activities ( 1L-1, 1L-2, 1L-6, TNF), proliferation of lymphocytes and chemosensitivity of tumor cells, and compared it with radioactive isotope assay. The results showed that the MTT assay may be used to test the cellular cytotoxicity, cytokine ac-tivity, proliferation of lymphocytes and chemosensitivity of tumor cells. We think it is a simple, rapid, economic and safety method.

6.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-594607

RESUMO

Objective To research the trichomonacidal effect of secnidazole benzoate in vitro.Methods Trichomonas vaginalis was cultured in liver extract medium in 96-well microplate.The culture suspension of Trichomonas vaginalis was divided into four groups:secnidazole benzoate, secnidazole, metronidazole and control, with medium as blank control.MTT colorimetric assay was applied to determine the inhibitory effect of secnidazole benzoate on the proliferation of Trichomonas vaginalis.The culture suspension was transfered into test tubes and divided into same groups to observe inhibitory effect by the classical microscopic counting method.Results After 24 h incubation, the proliferation of the parasites was concentration-dependent by secnidazole benzoate(t=9.02, P

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