scholarly journals Antioxidant and antiproliferative activity of Granny Smith apple pomace

2008 ◽  
pp. 201-212 ◽  
Author(s):  
Sladjana Savatovic ◽  
Gordana Cetkovic ◽  
Sonja Djilas ◽  
Vesna Tumbas ◽  
Jasna Canadanovic-Brunet ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Antioxidant Activities ◽  
Colorimetric Assay ◽  
Colon Adenocarcinoma ◽  
Apple Pomace ◽  
Breast Adenocarcinoma ◽  
Diphenyltetrazolium Bromide ◽  
Spin Resonance ◽  
Ht 29 ◽  
Antiproliferative Activities

Granny Smith apple pomace was subjected to evaluation as valuable source of antioxidant and anticancer phytochemicals on the basis of its content in phenolic compounds, antioxidant and antiproliferative activity. The total cotent of phenolics, flavonoids and flavan-3-ols in apple pomace determined spectrophotometrically, was 7.02 mg/g, 0.51 mg/g and 8.80 mg/g. Major phenolics (phenolic acids, flavan-3-ols, flavonoids and dihydrochalcons) in apple pomace were identified and quantified by HPLC. The antioxidant activity of apple pomace on stable 1,1-diphenyl-2-picrylhydrazyl (DPPH) and reactive hydroxyl radicals, was investigated by electron spin resonance (ESR) spectroscopy. The IC50 DPPH and IC50 OH values of Granny Smith apple pomace were 9.51 mg/ml and 29.17 mg/ml, respectively. The antiproliferative activities of apple pomace on cervix epitheloid carcinoma (HeLa), colon adenocarcinoma (HT-29) and breast adenocarcinoma (MCF7) cell lines were determined according to the MTT (3-(4,5-dimethylthiazol-2-yl)- 2,5-diphenyltetrazolium bromide) colorimetric assay. The IC50 HeLa , IC50 HT-29 and IC50 MCF7 values of Granny Smith apple pomace were 26.40 mg/ml, 22.47 mg/ml and 21.26 mg/ml, respectively. The significant correlations between antioxidant activities and antiproliferative activities were established (p<0.05).

scholarly journals Phenylpyrazalopyrimidines as Tyrosine Kinase Inhibitors: Synthesis, Antiproliferative Activity, and Molecular Simulations

Molecules ◽  
2020 ◽  
Vol 25 (9) ◽  
pp. 2135 ◽  
Author(s):  
Bhupender S. Chhikara ◽  
Sajda Ashraf ◽  
Saghar Mozaffari ◽  
Nicole St. Jeans ◽  
Dindyal Mandal ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Inhibitory Activity ◽  
Tyrosine Kinases ◽  
Kinase Inhibitors ◽  
Target Selection ◽  
Colon Adenocarcinoma ◽  
Human Leukemia ◽  
Ovarian Adenocarcinoma ◽  
Ht 29

N1-(α,β-Alkene)-substituted phenylpyrazolopyrimidine derivatives with acetyl and functionalized phenyl groups at α- and β-positions, respectively, were synthesized by the reaction of 3-phenylpyrazolopyrimidine (PhPP) with bromoacetone, followed by a chalcone reaction with differently substituted aromatic aldehydes. The Src kinase enzyme assay revealed modest inhibitory activity (half maximal inhibitory concentration, IC50 = 21.7–192.1 µM) by a number of PhPP derivatives. Antiproliferative activity of the compounds was evaluated on human leukemia (CCRF-CEM), human ovarian adenocarcinoma (SK-OV-3), breast carcinoma (MDA-MB-231), and colon adenocarcinoma (HT-29) cells in vitro. 4-Chlorophenyl carbo-enyl substituted 3-phenylpyrazolopyrimidine (10) inhibited the cell proliferation of HT-29 and SK-OV-3 by 90% and 79%, respectively, at a concentration of 50 µM after 96 h incubation. The compound showed modest inhibitory activity against c-Src (IC50 = 60.4 µM), Btk (IC50 = 90.5 µM), and Lck (IC50 = 110 µM), while it showed no activity against Abl1, Akt1, Alk, Braf, Cdk2, and PKCa. In combination with target selection and kinase profiling assay, extensive theoretical studies were carried out to explore the selectivity behavior of compound 10. Specific interactions were also explored by examining the changing trends of interactions of tyrosine kinases with the phenylpyrazolopyrimidine derivative. The results showed good agreement with the experimental selectivity pattern among c-Src, Btk, and Lck.

scholarly journals Evaluation of the antiproliferative activity of red propolis hydroalcoholic extract and its fractions obtained by partition

2020 ◽  
Vol 18 (2) ◽  
Author(s):  
Iara Squarisi ◽  
Karoline Soares De Freitas ◽  
Danieli Cristina Lemes ◽  
Gari Vidal Ccana Ccapatinta ◽  
Jennyfer Andrea Aldana Mejía ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Colorimetric Assay ◽  
Lung Fibroblasts ◽  
Breast Adenocarcinoma ◽  
Tumor Cell Lines ◽  
Hydroalcoholic Extract ◽  
Antitumor Potential ◽  
Significant Difference

Abstract. Squarisi IS, De Freitas KS, Lemes DC, Ccana-Ccapatinta GV, Mejia JAA, Bastos JK, Veneziani RCS, Ambrosio SR, Tavares DC. 2018. Evaluation of the antiproliferative activity of red propolis hydroalcoholic extract and its fractions obtained by partition. Biofarmasi J Nat Prod Biochem 18: 66-69. The present study aimed to evaluate the cytotoxicity of red propolis hydroalcoholic extract (RPHE) and its fractions obtained by partition, hexanes (HF), dichloromethane (DF), ethyl acetate (AF) and n-butanol (BF), on tumor and non-tumor cell lines. For this purpose, the XTT colorimetric assay was performed on human lung fibroblasts (GM07492A, non-tumor cell), breast adenocarcinoma (MCF-7), glioblastoma (U343) and cervix adenocarcinoma (HeLa) cells. The results showed that RPHE, HF and DF presented not only cytotoxic potential to all tumor cell lines but also to normal cell line, indicating selectivity absence. HF presented the lowest IC50 (half minimal inhibitory concentration; 33.8-133.3 µg/mL), with significant difference from those observed for RPHE (137.0-262.7 µg/mL). BF and AF revealed an IC50 which was higher than 1250 µg/mL in all cell lines. The results showed that red propolis has substances with antiproliferative activity, indicating that its hexanes fraction may have substances with antitumor potential.

scholarly journals Antibacterial and antiproliferative activities of the fresh leaf essential oil of Psidium guajava L. (Myrtaceae)

2019 ◽  
Vol 79 (4) ◽  
pp. 697-702 ◽  
Author(s):  
E. A. J. Silva ◽  
E. B. B. Estevam ◽  
T. S. Silva ◽  
H. D. Nicolella ◽  
R. A. Furtado ◽  
...  
Keyword(s):  
Essential Oil ◽  
Antiproliferative Activity ◽  
Biological Activities ◽  
Psidium Guajava ◽  
Lung Fibroblasts ◽  
Breast Adenocarcinoma ◽  
Moderate Activity ◽  
Broth Microdilution Method ◽  
Antiproliferative Activities ◽  
Mcf 7

Abstract This study evaluated the antibacterial and antiproliferative activities of the essential oil of Psidium guajava leaves (PG-EO), traditionally used in folk medicine. The essential oil was obtained from fresh leaves by hydrodistillation, using a modified Clevenger apparatus. The major PG-EO chemical constituents were identified by GC-MS and GC-FID as being β-caryophyllene (16.1%), α-humulene (11.9%), aromadendrene oxide (14.7%), δ-selinene (13.6%), and selin-11-en-4α-ol (12.5%). The antibacterial activity of the essential oil of P. guajava leaves was determined in terms of its minimum inhibitory concentrations (MIC) using the broth microdilution method in 96-well microplates. PG-EO had moderate activity against Streptococcus mutans (MIC = 200 µg/mL), S. mitis (MIC = 200 µg/mL), S. sanguinis (MIC = 400 µg/mL), S. sobrinus (MIC = 100 µg/mL), and S. salivarius (MIC = 200 µg/mL). The antiproliferative activity was evaluated against different tumor cell lines: breast adenocarcinoma (MCF-7), human cervical adenocarcinoma (HeLa), and human gliobastoma (M059J). A normal human cell line (GM07492A, lung fibroblasts) was included. The antiproliferative activity was evaluated using the XTT assay and the results were expressed as IC50. The essential oil showed significantly lower IC50 values against MCF-7 and M059J lines than that obtained for the normal line, showing selectivity. Our results suggest that the essential oil of Psidium guajava L. has promising biological activities and can be considered a new source of bioactive compounds.

Ligand-Based Drug Design: Synthesis and Biological Evaluation of Substituted Benzoin Derivatives as Potential Antitumor Agents

2019 ◽  
Vol 15 (4) ◽  
pp. 417-429 ◽  
Author(s):  
Dima A. Sabbah ◽  
Ameerah H. Ibrahim ◽  
Wamidh H. Talib ◽  
Khalid M. Alqaisi ◽  
Kamal Sweidan ◽  
...  
Keyword(s):  
Cell Lines ◽  
Antiproliferative Activity ◽  
Inhibitory Activity ◽  
Colon Adenocarcinoma ◽  
Human Colon ◽  
T47d Cell ◽  
Breast Adenocarcinoma ◽  
Glide Docking ◽  
Hct 116 ◽  
Mcf 7

Background: Phosphoinositide 3-kinase α (PI3Kα) has emerged as a promising target for anticancer drug design. Objectives: Target compounds were designed to investigate the effect of the p-OCH3 motifs on ligand/PI3Kα complex interaction and antiproliferative activity. Methods: Synthesis of the proposed compounds, biological examination tests against human colon adenocarcinoma (HCT-116), breast adenocarcinoma (MCF-7), and breast carcinoma (T47D) cell lines, along with Glide docking studies. Results: A series of 1,2-bis(4-methoxyphenyl)-2-oxoethyl benzoates was synthesized and characterized by means of FT-IR, 1H and 13C NMR, and by elemental analysis. Biological investigation demonstrated that the newly synthesized compounds exhibit antiproliferative activity in human colon adenocarcinoma (HCT-116), breast adenocarcinoma (MCF-7), and breast carcinoma (T47D) cell lines possibly via inhibition of PI3Kα and estrogen receptor alpha (ERα). Additionally, results revealed that these compounds exert selective inhibitory activity, induce apoptosis, and suppress VEGF production. Compound 3c exhibited promising antiproliferative activity in HCT-116 interrogating that hydrogen bond-acceptor mediates ligand/PI3Kα complex formation on m- position. Compounds 3e and 3i displayed high inhibitory activity in MCF-7 and T47D implying a wide cleft discloses the o-attachment. Furthermore, compound 3g exerted selective inhibitory activity against T47D. Glide docking studies against PI3Kα and ERα demonstrated that the series accommodate binding to PI3Kα and/or ERα. Conclusion: The series exhibited a potential antitumor activity in human carcinoma cell lines encoding PI3Kα and/or ERα.

scholarly journals Antiproliferative, antibacterial, and antioxidant activities of Bauhinia strychnifolia Craib aqueous extracts in gut and liver perspective

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Suranat Phonghanpot ◽  
Faongchat Jarintanan
Keyword(s):  
Traditional Medicine ◽  
Antioxidant Activities ◽  
Colon Adenocarcinoma ◽  
Gram Negative Bacteria ◽  
Aqueous Extracts ◽  
Gram Positive Bacteria ◽  
Ms Analysis ◽  
Diffusion Assay ◽  
Ht 29 ◽  
Free Radicals Scavenging

Abstract Background Bauhinia strychnifolia Craib is an herb in Thai traditional medicine. Its decoction is traditionally used as an anticancer, antidiarrheal, and hangover remedy for centuries. Several studies described bioactivities of its organic solvent extracts, however, only few demonstrated the usefulness of the decoction. Here, we aimed to determine the bioactivities of Bauhinia strychnifolia Craib root and stem aqueous extracts in gut and liver perspective. Methods To achieve the goal, we performed MTT test, microscopic analyses, disc diffusion assay, broth microdilution assay, free radicals scavenging assays, and LC-MS analysis. Results We found that the extracts inhibited the growth of human hepatocellular carcinoma (HepG2) and colon adenocarcinoma (HT-29) cell lines. Moreover, they also inhibited the growth of gram-positive bacteria Staphylococcus aureus and Bacillus cereus but not inhibited the growth of gram-negative bacteria Escherichia coli and Pseudomonas aeruginosa. Furthermore, the extracts exhibited moderate antioxidant activity and increased GSH production in HepG2 cell line when compared with untreated. Our LC-MS analysis confirmed the existence of anticancer and antioxidant; 3,5,7,3′,5′-pentahydroxyflavanonol-3-O-α-L-rhamnopyranoside and β-sitosterol, in the extracts. Conclusion The results from our study supported that the administration of Bauhinia strychnifolia Craib root and stem decoction would really aid colon or liver cancer patients and detoxify the alcoholic drunkard as it is claimed in Thai traditional medicine.

scholarly journals Chemical Composition and Assessment of Antimicrobial, Antioxidant and Antiproliferative Activities of Essential oil from Clinopodium sericeum, a Peruvian Medicinal Plant

2021 ◽  
Vol 15 (3) ◽  
pp. 175-186
Author(s):  
Buc Calderon Pedro ◽  
Julio Benites ◽  
David Rios ◽  
Angélica Guerrero-Castilla ◽  
Cinthya Enríquez ◽  
...  
Keyword(s):  
Essential Oil ◽  
Antioxidant Activities ◽  
Colorimetric Assay ◽  
Human Cancer ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Dose Range ◽  
Radical Scavenging ◽  
Antiproliferative Activities

Clinopodium sericeum is widely used in Peruvian folk medicine in the form of infusion to treat stomach distress, indigestion and antiflu. In this study, the essential oil from C. sericeum was obtained by hydrodistillation, analyzed by GC and GC/MS, and 73 compounds were identified. Major components of the oil were b-germacrene-D (15%), b-caryophyllene (13.8%), and sabinene (11.2%). Furthermore, we assessed the in vitro biological activities displayed by the oil obtained from the aerial parts of C. sericeum, namely the antioxidant, antimicrobial and antiproliferative activities. The antioxidant activities of the essential oil were evaluated by FRAP, CUPRAC, ABTS and DPPH radical scavenging activity. The essential oil displays antibacterial activity against Gram-negative and Gram-positive bacterial strains (MIC 50-200 µg/mL) in a dose-range close to standard antibiotics. Such activity may be related to the presence of terpene compounds. The antiproliferative activity of the essential oil was measured in vitro using the MTT colorimetric assay in healthy non-tumorigenic cells (HEK-293) and in three human cancer cell lines (T24, DU-145, and MCF-7). The calculated IC50 values were around 0.2 mg/mL. Since the essential oil was almost devoid of antioxidant activity, its anti-proliferative action is unlikely related to oxidative stress and relies on other unknown mechanisms.

Microwave-assisted Synthesis of Polymethoxychalcone Mannich Bases and Their Antiproliferative Activity

2019 ◽  
Vol 16 (2) ◽  
pp. 117-121 ◽  
Author(s):  
Peipei Han ◽  
Wenhua Zhou ◽  
Mingxia Chen ◽  
Qiuan Wang
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Mannich Base ◽  
Cancer Cell Lines ◽  
Secondary Amines ◽  
Conventional Heating ◽  
Microwave Assisted ◽  
Ic50 Values ◽  
Antiproliferative Activities

A series of eight polymethoxychalcone Mannich base derivatives 2a-2h was synthesized via the microwave-assisted Mannich reaction of natural product 2&#039;-hydroxy-3,4,4&#039;,5,6&#039;-pentamethoxychalcone (1) with various secondary amines and formaldehyde. Compared to conventional heating method (80&#176;C), the microwave-assisted method (700W, 65&#176;C) is efficient with short reaction time (0.5-1 h) and good yields (74-88%). The antiproliferative activities of eight Mannich base derivatives were evaluated in vitro on a panel of three human cancer cell lines (Hela, HCC1954 and SK-OV-3) by CCK-8 assay. The results showed that all of the Mannich base derivatives exhibited potential antiproliferative activities on tested cancer cell lines with the IC50 values of 9.13-48.51 &#181;M. Some active compounds exhibited more activity as compared to positive control cis-Platin. Among them, compound 2b revealed to have the strongest antiproliferative activity against all the three cancer cell lines with IC50 values ranging from 9.13 to 11.24 &#181;M.

scholarly journals The synergistic interference effect of silica nanoparticles concentration and the wavelength of ELISA on the colorimetric assay of cell toxicity

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Fariba Abbasi ◽  
Hassan Hashemi ◽  
Mohammad Reza Samaei ◽  
Amir SavarDashtaki ◽  
Abooalfazl Azhdarpoor ◽  
...  
Keyword(s):  
Mtt Assay ◽  
Interference Effect ◽  
Polynomial Regression ◽  
Colorimetric Assay ◽  
Synergistic Effects ◽  
Cell Toxicity ◽  
Diphenyltetrazolium Bromide ◽  
Nanoparticles Concentration ◽  
Artificial Neural Network Ann ◽  
First Time

AbstractThe 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay is the most common method for the determination of cell toxicity, but some factors limit the sensitivity of this method, such as pH. Less attention had been paid to the interference effect of optical and plasmonic properties of SiO2 nanoparticles (NPs) in the wavelength range assigned to MTT. This study investigated the synergistic interference effect of SiO2 NPs and wavelength on MTT assay for the first time. The examined variables included the type of SiO2 NPs concentrations (1, 10, and 100 mM) and different wavelengths (470, 490, 520, and 570 nm). The results showed that optical density (OD) increased (p < 0.05) when wavelength and the concentration of crystalline SiO2 NPs increased. So, the maximum OD at 10 and 100 mM were attributed to crystalline SiO2 NPs (p < 0.05) due to the functional group, whereas it was related to amorphous at 1 mM (p > 0.05). According to polynomial regression modeling (PRM), the maximum interference effect was predicted at crystalline SiO2 NPs and wavelength > 550 nm. Besides, the synergistic effects of SiO2 NPs, wavelength, and concentration of NPs had been a good fitting with first-order PRM. Thus, the concentration of SiO2 NPs had a confounder factor in colorimetric for MTT assay. The best artificial neural network (ANN) structure was related to the 3:7:1 network (Rall = 0.936, MSE = 0.0006, MAPE = 0.063). The correlation between the actual and predicted data was 0.88. As SiO2 NPs presence is an interfering factor in MTT assay concerning wavelength, it is suggested wavelength use with minimum confounding effect for MTT assay.

scholarly journals Biotransformation of Polyphenols in Apple Pomace Fermented by β-Glucosidase-Producing Lactobacillus rhamnosus L08

Foods ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1343
Author(s):  
Lihua Liu ◽  
Chenyi Zhang ◽  
Huimin Zhang ◽  
Guoqiang Qu ◽  
Chun Li ◽  
...  
Keyword(s):  
Lactic Acid ◽  
Food Industry ◽  
Antioxidant Activities ◽  
Lactobacillus Rhamnosus ◽  
Economic Benefits ◽  
Apple Pomace ◽  
High Cell ◽  
Bioactive Components ◽  
Glucosidase Activity ◽  
Phenolic Profiles

Apple pomace, the main by-product in apple processing, is a cheap source of bioactive compounds that could be used in the food industry. However, the value of this by-product is still far from being fully realized. In this study, 11 strains of Lactobacillus strains were assayed for β-glucosidase activity, and only Lactobacillus rhamnosus L08 (L. rhamnosus L08) showed high cell-membrane associated β-glucosidase activity. We then evaluated the effects of fermentation of apple pomace using the selected strain, focusing on the biotransformation of polyphenols and antioxidant capacity. We found that L. rhamnosus L08 fermentation significantly reduced the contents of quercitrin and phlorizin in apple pomace, while increasing the contents of quercetin and phloretin. The contents of gallic acid, epicatechin acid, caffeic acid, and ferulic acid were also increased in apple pomace after fermentation. In addition, the antioxidant activities of apple pomace were enhanced during fermentation, based on the bioconversion of phenolic profiles. Our results demonstrate that lactic acid bacteria fermentation is a promising approach to enhance the bioactivity of phenolic compounds in apple pomace. Moreover, this study demonstrates that, as a valuable processing by-product with bioactive components, apple pomace can be used in the food industry to provide economic benefits.

Sign in / Sign up

Export Citation Format

Share Document