A comparative study to elucidate the biological activities of crude extracts from rice bran and wheat bran in cell line models

We report herein the evaluation of various pyrido[2′,1′:2,3]imidazo[4,5-c]isoquinolin-5-amines as potential cytotoxic agents. These molecules were obtained by developing the multicomponent Groebke–Blackburn–Bienaymé reaction to yield various pyrido[2′,1′:2,3]imidazo[4,5-c]quinolines which are isosteres of ellipticine whose biological activities are well established. To evaluate the anticancer potential of these pyrido[2′,1′:2,3]imidazo[4,5-c]isoquinolin-5-amine derivatives in the human neuroblastoma cell line, the cytotoxicity was examined using the WST-1 assay after 72 h drug exposure. A clonogenic assay was used to assess the ability of treated cells to proliferate and form colonies. Protein expressions (Bax, bcl-2, cleaved caspase-3, cleaved PARP-1) were analyzed using Western blotting. The colony number decrease in cells was 50.54%, 37.88% and 27.12% following exposure to compounds 2d, 2g and 4b respectively at 10 μM. We also show that treating the neuroblastoma cell line with these compounds resulted in a significant alteration in caspase-3 and PARP-1 cleavage.

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Comparative study of a new composite biomaterial fluor-hydroxyapatite on fibroblast cell line NIH-3T3 by direct test

Biologia ◽

10.2478/s11756-008-0043-x ◽

2008 ◽

Vol 63 (2) ◽

Cited By ~ 6

Author(s):

Marica Theiszová ◽

Soňa Jantová ◽

Silvia Letašiová ◽

Ľuboš Valík ◽

Martin Palou

Keyword(s):

Comparative Study ◽

Cell Line ◽

Dna Content ◽

Fibroblast Cell ◽

Cell Number ◽

Fibroblast Cell Line ◽

3T3 Cells ◽

End Points ◽

Basal Cytotoxicity ◽

Nih 3T3

AbstractThe number of biomaterials used in biomedical applications has rapidly increased in the past two decades. Fluorapatite (FA) is one of the inorganic constituents of bone or teeth used for hard tissue repairs and replacements. Fluor-hydroxyapatite (FHA) is a new synthetically prepared composite that in its structure contains the same molecular concentration of OH− groups and F− ions. The aim of this experimental investigation was to use the embryonal mouse fibroblast cell line NIH-3T3 for comparative study of basal cytotoxicity of fluoridated biomaterials FHA and FA discs. Hydroxyapatite (HA) disc, high-density polyethylene as negative control and polyvinyl chloride (PVC) containing organotin stabilizer as positive control were used as standard biomaterials. The appropriateness of the use of NIH-3T3 cells and their sensitivity for tested biomaterials were evaluated on the basis of five cytotoxic end points: cell proliferation, cell morphology, lactate dehydrogenase (LDH) released, protein and DNA cell content. The basal cytotoxicity of FHA, FA and HA discs was measured by direct contact method. FHA composite, FA and HA demonstrated in cell line NIH-3T3 nearly similar basal cytotoxicity increasing with the time of treatment. After 72 h of biomaterials treatment, about 25% inhibition of cell number, unchanged morphology of dividing cells, 6.31–0.16% increase of released LDH, about 10% inhibition of cell protein content and about 20% inhibition of DNA content was found. On the other hand, from the growth rates it resulted that NIH-3T3 cells, affected by tested biomaterials, divided about 20% slowlier than the control (untreated cells). Using the linear regression analysis we found out that deviations in measurements of cytotoxicity by four methods were as follows: less than 10% for cell number, protein and DNA content methods and 12.4% for released LDH method. Based on a good correlation of the cytotoxicity of biomaterials obtained from all end points we could conclude that fibroblast NIH-3T3 cell line was appropriate for measuring the basal cytoxicity of tested biomaterials.

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Synthesis of a Series of Novel 2-Amino-5-Substituted 1,3,4-oxadiazole and 1,3,4-thiadiazole Derivatives as Potential Anticancer, Antifungal and Antibacterial Agents

Medicinal Chemistry ◽

10.2174/1573406417666210803170637 ◽

2021 ◽

Vol 17 ◽

Author(s):

Em Canh Pham ◽

Tuyen Ngoc Truong ◽

Nguyen Hanh Dong ◽

Duy Duc Vo ◽

Tuoi Thi Hong Do

Keyword(s):

Cell Line ◽

Biological Activities ◽

Chemical Properties ◽

Diffusion Method ◽

Anticancer Activities ◽

Molecular Docking Study ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Thiadiazole Derivatives ◽

Antibacterial And Antifungal

Background: Many compounds containing a five-membered heterocyclic ring display exceptional chemical properties and versatile biological activities. Objective: The objective of the present study was the desire to prepare the 5-substituted 2-amino-1,3,4-oxadiazole and 2-amino-1,3,4-thiadiazole derivatives and evaluate their potential anticancer, antibacterial and antifungal activities. Methods: Twenty-seven derivatives were synthesized by iodine-mediated cyclization of semicarbazones or thiosemicarbazones obtained from condensation of semicarbazide or thiosemicarbazide and aldehydes. The structures were confirmed by 1H-NMR, 13C-NMR and MS spectra. The antibacterial and antifungal activities were evaluated by diffusion method and the anticancer activities were evaluated by MTT assay. Results: Twenty-seven derivatives have been synthesized in moderate to good yields. A number of derivatives exhibited potential antibacterial, antifungal and anticancer activities. Conclusion: Compounds (1b, 1e and 1g) showed antibacterial activity against Streptococcus faecalis, MSSA and MRSA with MIC ranging between 4 to 64 µg/mL. Compound (2g) showed antifungal activity against Candida albicans (8 µg/mL) and Aspergillus niger (64 µg/mL). Compound (1o) exhibited high cytotoxic activity against HepG2 cell line (IC50 value 8.6 µM), which is comparable to the activity of paclitaxel, and is non-toxic on LLC-PK1 normal cell line. The structure activity relationship and molecular docking study of the synthesized compounds are also reported.

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Chemical Composition of Aegle marmelos: A Review

Asian Journal of Research in Pharmaceutical Science ◽

10.52711/2231-5659.2021.00044 ◽

2021 ◽

pp. 280-290

Author(s):

Yogita Chowdhary

Keyword(s):

Therapeutic Potential ◽

Biological Activities ◽

Chemical Constituents ◽

Biologically Active ◽

Fixed Dose ◽

Root Bark ◽

Preclinical Studies ◽

Aegle Marmelos ◽

Crude Extracts ◽

Anti Inflammatory

Aegle marmelos (Bilva) is being used in Ayurveda for the treatment of several inflammatory disorders. The plant is a member of a fixed dose combination of Dashamoola in Ayurveda. However, the usage of roots/root bark or stems is associated with sustainability concerns. Bael (Aegle marmelos (L.) Corr.) is an important medicinal plant of India. Leaves, fruits, stem and roots of A. marmelos have been used in ethno medicine to exploit its' medicinal properties including astringent, antidiarrheal antidysenteric, demulcent, antipyretic and anti-inflammatory activities. Compounds purified from bael have been proven to be biologically active against several major diseases including cancer, diabetes and cardiovascular diseases. Preclinical studies indicate the therapeutic potential of crude extracts of A. marmelos in the treatment of many microbial diseases, diabetes and gastric ulcer. This review covers the biological activities of some isolated chemical constituents of A. marmelos and preclinical studies on some crude extracts and pure compounds to explore novel bioactive compounds for therapeutic application. Aegle marmelos (L.) is a seasonal fruit that contains significant amounts of bioactives like, phenolic acids (gallic acids, 2,3-dihydroxy benzoic acid, chlorogenic acid, p-coumaric acid, vanillic acid), flavonoid (rutin), organic acids (oxalic acid, tartaric acid, malic acid, lactic acid, acetic acid, citric acid, propionic acid, succinic acid, fumaric acid), vitamin C, vitamin B group (thiamine, niacin, pyridoxine, pantothenic acid, biotin, cobalamins, riboflavin), tocopherols (α-tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol), carotenes (α-carotene, β-carotene, γ-carotene, δ-carotene) and also rich in essential minerals (potassium, calcium, phosphorus, sodium, iron, copper, manganese). Hence the use of aegle plays important role as anti-inflammatory.

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Antimicrobial activity of extracellular metabolites from antagonistic bacteria isolated from potato (Solanum phureja) crops

Summa Phytopathologica ◽

10.1590/0100-5405/1953 ◽

2014 ◽

Vol 40 (3) ◽

pp. 212-220 ◽

Cited By ~ 7

Author(s):

Sinar David Granada García ◽

Antoni Rueda Lorza ◽

Carlos Alberto Peláez

Keyword(s):

Antimicrobial Activity ◽

Cyclic Peptide ◽

Biological Activities ◽

Pathogenic Fungi ◽

Antagonistic Activity ◽

Solanum Phureja ◽

Dual Culture ◽

Crude Extracts ◽

Extracellular Metabolites

Microorganisms for biological control are capable of producing active compounds that inhibit the development of phytopathogens, constituting a promising tool toob tain active principles that could replace synthetic pesticides. This study evaluatedtheability of severalpotentialbiocontrol microorganismsto produce active extracellular metabolites. In vitro antagonistic capability of 50 bacterial isolates from rhizospheric soils of "criolla" potato (Solanum phureja) was tested through dual culture in this plant with different plant pathogenic fungi and bacteria. Isolates that showed significantly higher antagonistic activity were fermented in liquid media and crude extracts from the supernatants had their biological activities assessed by optical density techniques. Inhibitory effecton tested pathogens was observed for concentrations between 0.5% and 1% of crude extracts. There was a correlation between the antimicrobial activity of extracts and the use of nutrient-rich media in bacteria fermentation. Using a bioguided method, a peptidic compound, active against Fusarium oxysporum, was obtained from the 7ANT04 strain (Pyrobaculum sp.). Analysis by nuclear magnetic resonance and liquid chromatography coupled to mass detector evidenced an 11-amino acid compound. Bioinformatic software using raw mass data confirmed the presence of a cyclic peptide conformed by 11 mostly non-standard amino acids.

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Dietary Wheat Bran Oil Is Equally as Effective as Rice Bran Oil in Reducing Plasma Cholesterol

Journal of Agricultural and Food Chemistry ◽

10.1021/acs.jafc.7b06093 ◽

2018 ◽

Vol 66 (11) ◽

pp. 2765-2774 ◽

Cited By ~ 14

Author(s):

Lin Lei ◽

Jingnan Chen ◽

Yuwei Liu ◽

Lijun Wang ◽

Guohua Zhao ◽

...

Keyword(s):

Rice Bran ◽

Wheat Bran ◽

Rice Bran Oil ◽

Plasma Cholesterol ◽

Wheat Bran Oil

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New biological findings of ethanol and chloroform extracts of fungi Suillellus rubrosanguineus and Tylopilus felleus

Interdisciplinary Toxicology ◽

10.2478/intox-2018-0018 ◽

2018 ◽

Vol 11 (3) ◽

pp. 204-208

Author(s):

Ivana Šušaníková ◽

Adriána Kvasnicová ◽

Žofia Brzková ◽

Ondrej Ďuriška ◽

Pavel Mučaji

Keyword(s):

Cell Line ◽

Cell Lines ◽

Cancer Cell ◽

Biological Activities ◽

Cancer Cell Line ◽

Middle Europe ◽

Dragendorff Reagent ◽

Nih 3T3 ◽

Clinical Experiments ◽

Mcf 7

Abstract The aim of the research was to determine some basic biological activities of less biomedically studied but commonly known two fungi from the Boletaceae family Suillellus rubrosanguineus and Tylopilus felleus, which grow in the forests of Middle Europe. The cytotoxicity tests of the ethanol and chloroform extracts were carried out using NIH-3T3 and MCF-7 cell lines. The presence of alkaloids in the extracts was assessed by the reaction with Dragendorff reagent. In all of the extracts the positive reaction with the reagent was observed. In general, the extracts from Suillellus rubrosanguineus were more cytotoxic than the extracts from Tylopilus felleus and exhibited no selectivity of activities on healthy and cancer cell lines. However, the extracts from Tylopilus felleus proved to be selectively cytotoxic for cancer cell line. Tylopilus extracts or their isolated bioactive compounds could be considered for further study in pre-clinical experiments.

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Evaluation of the Biological Activities of Crude Extracts from PatagonianProsopisSeeds and Some of Their Active Principles

Journal of Herbal Pharmacotherapy ◽

10.1080/j157v03n02_04 ◽

2003 ◽

Vol 3 (2) ◽

pp. 31-37 ◽

Cited By ~ 4

Author(s):

M. Mazzuca ◽

W. Kraus ◽

V. Balzaretti

Keyword(s):

Biological Activities ◽

Crude Extracts

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Biological activity of gum Arabic-coated ferrous oxide nanoparticles

Modern Physics Letters B ◽

10.1142/s021798492150411x ◽

2021 ◽

pp. 2150411

Author(s):

Rania Hasan Huseen ◽

Ali A. Taha ◽

Ihab Q. Ali ◽

Oday Mahmmod Abdulhusein ◽

Selma M. H. Al-Jawad

Keyword(s):

Iron Oxide ◽

Cell Line ◽

Biological Activities ◽

Low Cost ◽

Gum Arabic ◽

Precipitation Method ◽

Oxide Nanoparticles ◽

Electron Microscopic ◽

Co Precipitation ◽

Mcf 7

In this study, iron oxide nanoparticles (NPs) had been prepared by co-precipitation method. In order to reduce their toxicity and increase stability, prepared iron oxide was coated with gum Arabic. Gum Arabic is preferred over synthetic materials due to their non-toxicity, low cost and availability. Characterization of coated and non-coated iron oxide NPs had been performed by spectrophotometer, Fourier transfer infra-red spectrophotometer (FTIR), Zeta potential, X-ray diffraction (XRD) and field emission scanning electron microscopic (FE-SEM). The fabricated nanoparticles appeared purity and crystalline nature by XRD, with diameter average of 27.01 nm and 55.12 nm for iron oxide NPs and iron oxide NPs coated with gum Arabic, respectively. On the other hand, four biological activities of coated and non-coated iron oxide had been investigated. High removal of methylene blue pollutant dye (46%) was observed with iron oxide NPs, while removal percentage was 22.6 performed by iron oxide NPs coated with gum Arabic within 72 h. Iron oxide NPs revealed high inhibition zones of 27.5 nm and 30 mm, at 1000 [Formula: see text]g/ml, against S. aureus and E. coli, respectively, while coated iron oxide NPs with gum Arabic revealed low antibacterial activity against both examined bacteria even when used at 1000 [Formula: see text]g/ml. The hemolytic activity of prepared NPs had been determined. The hemolytic percentage was increased whenever concentrations of nanoparticles increased. Lower hemolytic percentages were 69.76 and 50.98 for iron oxide NPs and iron oxide NPs coated with gum Arabic were observed at a concentration of 250 [Formula: see text]g/ml. Finally, cytotoxic activity was estimated against MCF-7 cell line and normal cell line WRL68 by MTT assay. A decrease in MCF-7 viability to 65.1% was observed when 400 [Formula: see text]g/ml of iron oxide NPs was used, while WRL68 viability was 75.03%. Iron oxide NPs coated with gum Arabic revealed significant reduction in MCF-7 and WRL68 viability to 69.90% and 80.05%, respectively, when 400 [Formula: see text]g/ml of nanoparticles was applied.

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In Vitro Screening for Cytotoxic, Anti-bacterial, Anti-HIV1-RT Activities and Chemical Constituents of Croton fluviatilis, Croton acutifolius, and Croton thorelii

The Natural Products Journal ◽

10.2174/2210315511666210119125611 ◽

2021 ◽

Vol 11 ◽

Author(s):

Charina Worarat ◽

Wilart Pompimon ◽

Phansuang Udomputtimekakul ◽

Sukee Sukdee ◽

Punchavee Sombutsiri ◽

...

Keyword(s):

Ethyl Acetate ◽

Ethyl Acetate Extract ◽

Biological Activities ◽

Chemical Constituents ◽

Bacterial Activity ◽

Cytotoxic Activities ◽

Separation And Purification ◽

Crude Extracts ◽

Cytotoxicity Activities

Background: Although the chemical constituents and biological activities of a large number of plants in the Croton genus have been studied, there are still recently discovered plants to be investigated. Objective: 1. To investigate the anti-bacterial, anti-HIV1-RT, and cytotoxicity activities of crude extracts from these plants. 2. To investigate the chemical constituents of Croton fluviatilis, Croton acutifolius, and Croton thorelii. Method: The anti-bacterial, anti-HIV1-RT, and cytotoxicity of the three plants were evaluated by standard techniques. Extraction, separation, and purification of extracts from the three plants were undertaken. Results: The ethyl acetate extract of C. fluviatilis showed low anti-bacterial activity against E. aerogenes, E. coli 0157: H7, and P. mirabilis, together with the ethyl acetate extract of C. acutifolius displayed low anti-bacterial activity against E. aerogenes, while all the crude extracts of C. thorelii were inactive. The ethyl acetate extracts of C. thorelii, and C. fluviatilis showed strong inhibited HIV1-RT, whereas the ethyl acetate extract of C. acutifolius, and the hexane extract of C. fluviatilis displayed moderate inhibited HIV1-RT. Cytotoxic properties of three Croton plants were specific to KKU-M213, MDA-MB-231, A-549, and MMNK-1. Especially, the ethyl acetate extract of C. acutifolius exhibited strong cytotoxic activities against MDA-MB-231, A-549, and MMNK-1. Furthermore, the ethyl acetate extract of C. thorelii showed high cytotoxic activities against KKU-M213, and MDA-MB-231. Compounds 1, and 4 were found in C. fluviatilis. Compounds 2 and 4 were also found in C. acutifolius. Moreover, compound 3 was only found in C. thorelii. Conclusion: The present study revealed that the three Croton species are good sources of flavonoid compounds and further investigation of the chemical constituents from these plants may prove to be fruitful to discover more active compounds to be tested as potential medicines.

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