scholarly journals ANTIOXIDANT POTENTIAL, ANTITUMOR ACTIVITY AND PHENOLIC PROFILE OF PHOENIX DACTYLIFERA LINN

2017 ◽  
Vol 9 (5) ◽  
pp. 130
Author(s):  
Manal Mortady Hamed ◽  
Mona Abdel Motagally Mohamed ◽  
Wafaa Sabry Ahmed
Keyword(s):  
Antitumor Activity ◽  
Phoenix Dactylifera ◽  
In Vitro Cytotoxicity ◽  
Antioxidant Potential ◽  
Butanol Extract ◽  
Chemical Structures ◽  
Total Antioxidant ◽  
Ic50 Values ◽  
Date Fruits

Objective: Phoenix dactylifera Linn (Fam.: arecaceae)or date fruits are commercial crops that notarized in holy quran. 70% aqueous MeOH extract of the fruits led to isolation of six compounds; its chemical structures were determined as, β-sitosterol (1), caffeic acid (2), ferulic acid (3), protocatechuic acid (4), p-hydroxybenzoic acid (5) and luteolin (6).Methods: The accurately weighed date fruits were washed, sliced and socked freshly in 70% methanol then exhaustively extracted under reflux for about 2 w and filtered, then fractionated by different solvent; finaly the butanol extract evaporated and fractionated on a polyamide glass column. Using Sephadex LH-20 column to purify the compounds obtained. In our preliminary study, the extracts and compounds were subjected to in vitro cytotoxicity against HepG2 cell line through the MTT assay and the antioxidant potential of the extracts and pure compounds were assayed through in vitro model using (DPPH) and phosphomolybdenum assays.Results: Compounds 2 and 3 exhibited promising antitumor activity with IC50 values of 6 and 10 μg/ml, respectively. Moreover compounds 1, 4, 5 and 6 showed cytotoxic activity with IC50 values of 13, 15, 21 and 35 μg/ml, respectively. The antioxidant potential of the compounds showed the inhibition percentage values (SC50) ranged from 4.36 to 10.25 μg/ml, while the total antioxidant capacity ranged from (583.66 to 702.00 mg AAE/g compound).Conclusion: Our study demonstrated that; dates constituents are powerful as antioxidant and antitumor; hence it is the best potential for pharmaceutical applications.

α-Glucosidase Inhibitory Activity of the Extracts and Major Phytochemical Components of Smilax glabra Roxb

2020 ◽  
Vol 10 (1) ◽  
pp. 26-32
Author(s):  
Phuong T.M. Nguyen ◽  
Quang V. Ngo ◽  
Minh T.H. Nguyen ◽  
Alan T. Maccarone ◽  
Stephen G. Pyne
Keyword(s):  
Inhibitory Activity ◽  
In Vitro Cytotoxicity ◽  
Antidiabetic Activity ◽  
Ca 125 ◽  
Chemical Structures ◽  
Glucosidase Inhibitors ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Phytochemical Components

Background: A therapeutic approach to treat diabetes is to decrease postprandial hyperglycemia. α-Glucosidase inhibitors from plant sources offer an attractive strategy for the control of hyperglycemia. Smilax glabra Roxb is a medicinal plant found in Asia, including Vietnam, which is used in the treatment of chronic diseases. However, the antidiabetic activity and the identification of α-glucosidase inhibitors from this plant have not been intensively investigated. This research was carried out to determine the α-glucosidase inhibitory activity of the extracts and that of the major phytochemical components of Smilax glabra Roxb. This could lead to further studies on the role of these compounds in hyperglycemia control, as well as identify their potential future applications. Methods: Column chromatography combined with crystallization procedures were used to isolate active fractions and two major compounds. The chemical structures of these compounds were determined by analysis of their NMR spectroscopic data, as well as MS data and comparisons made with the literature data. The α-glucosidase inhibitory activity was determined spectrophotometrically using p-nitrophenyl α-D-glucopyranoside as a substrate. The in vitro cytotoxicity of the isolated compounds and fractions was determined using the MTT assay. Results: The two major compounds, astilbin and 5-O-caffeoylshikimic acid together with two very active fractions, F7 and F8, were isolated from the rhizome. The two major compounds had α- glucosidase inhibitory activities with IC50 values of ca. 125 µg/mL and 38 µg/mL, respectively which are about 4 and 13 folds higher activity than the reference compound acarbose (IC50 of ca. 525 µg/mL). Fractions F7 and F8 showed very promising inhibitory activities towards α-glucosidase with IC50 values of 5.5 and 5.8 µg/mL, respectively. Cytotoxicity data on mouse fibroblast NIH3T3 cells indicated that the active compounds and fractions were not toxic at concentrations that are greater than their respective IC50 values. The α-glucosidase inhibitory activity of 5-Ocaffeoylshikimic acid and that of the two active fractions are reported here for the first time. Conclusion: The two major isolated compounds and fractions, F7 and F8, significantly contribute to the α-glucosidase inhibitory activity of S. glabra Roxb extract. Further work is needed to clarify their modes of action and potential application.

5-Nitro-Thiophene-Thiosemicarbazone Derivatives Present Antitumor Activity Mediated by Apoptosis and DNA Intercalation

2019 ◽  
Vol 19 (13) ◽  
pp. 1075-1091 ◽  
Author(s):  
Karla Mirella Roque Marques ◽  
Maria Rodrigues do Desterro ◽  
Sandrine Maria de Arruda ◽  
Luiz Nascimento de Araújo Neto ◽  
Maria do Carmo Alves de Lima ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Antitumor Activity ◽  
Cell Line ◽  
Mitochondrial Membrane ◽  
In Vitro Cytotoxicity ◽  
Dna Intercalation ◽  
Phase Cell ◽  
Fluorescence Studies ◽  
In Silico Studies

Background: Considering the need for the development of new antitumor drugs, associated with the great antitumor potential of thiophene and thiosemicarbazonic derivatives, in this work we promote molecular hybridization approach to synthesize new compounds with increased anticancer activity. Objective: Investigate the antitumor activity and their likely mechanisms of action of a series of N-substituted 2-(5-nitro-thiophene)-thiosemicarbazone derivatives. Methods: Methods were performed in vitro (cytotoxicity, cell cycle progression, morphological analysis, mitochondrial membrane potential evaluation and topoisomerase assay), spectroscopic (DNA interaction studies), and in silico studies (docking and molecular modelling). Results: Most of the compounds presented significant inhibitory activity; the NCIH-292 cell line was the most resistant, and the HL-60 cell line was the most sensitive. The most promising compound was LNN-05 with IC50 values ranging from 0.5 to 1.9 µg.mL-1. The in vitro studies revealed that LNN-05 was able to depolarize (dose-dependently) the mitochondrial membrane, induceG1 phase cell cycle arrest noticeably, promote morphological cell changes associated with apoptosis in chronic human myelocytic leukaemia (K-562) cells, and presented no topoisomerase II inhibition. Spectroscopic UV-vis and molecular fluorescence studies showed that LNN compounds interact with ctDNA forming supramolecular complexes. Intercalation between nitrogenous bases was revealed through KI quenching and competitive ethidium bromide assays. Docking and Molecular Dynamics suggested that 5-nitro-thiophene-thiosemicarbazone compounds interact against the larger DNA groove, and corroborating the spectroscopic results, may assume an intercalating interaction mode. Conclusion: Our findings highlight 5-nitro-thiophene-thiosemicarbazone derivatives, especially LNN-05, as a promising new class of compounds for further studies to provide new anticancer therapies.

Synthesis and Antitumor Activity Evaluation of New Phenanthrene-Based Tylophorine Derivatives

2019 ◽  
Vol 16 (6) ◽  
pp. 462-467
Author(s):  
Songtao Li ◽  
Hongling Zhao ◽  
Zhifeng Yin ◽  
Shuhua Deng ◽  
Yang Gao ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Antitumor Activities ◽  
Human Carcinoma ◽  
Carcinoma Cell Lines ◽  
Structure Activity ◽  
Human Carcinoma Cell ◽  
Ic50 Values ◽  
Relationship Of

A series of new phenanthrene-based tylophorine derivatives (PBTs) were synthesized in good yield and their structures were characterized by 1H-NMR spectroscopy and ESI MS. In vitro antitumor activity of these compounds against five human carcinoma cell lines, including HCT116 (colorectal), BGC-823 (gastric), HepG-2 (hepatic), Hela (cervical) and H460 (lung) cells, was evaluated by MTT assay. Among these PBTs, compound 6b showed the highest antitumor activities against HCT116 and HepG-2 cell lines with IC50 values of 6.1 and 6.4 μM, respectively, which were comparable to that of adriamycin hydrochloride. The structure-activity relationship of these compounds was also discussed based on the results of their antitumor activity.

scholarly journals New Antiproliferative Triflavanone from Thymelaea hirsuta—Isolation, Structure Elucidation and Molecular Docking Studies

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 739
Author(s):  
Sameh S. Elhady ◽  
Reda F. A. Abdelhameed ◽  
Mayada M. El-Ayouty ◽  
Amany K. Ibrahim ◽  
Eman S. Habib ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Liver Tumors ◽  
Fold Increase ◽  
In Vitro Cytotoxicity ◽  
Mitogen Activated Protein Kinase ◽  
Wild Plant ◽  
Cytotoxic Activities ◽  
Ic50 Values ◽  
Thymelaea Hirsuta

In this study isolates from Thymelaea hirsuta, a wild plant from the Sinai Peninsula of Egypt, were identified and their selective cytotoxicity levels were evaluated. Phytochemical examination of the ethyl acetate (EtOAc) fraction of the methanolic (MeOH) extract of the plant led to the isolation of a new triflavanone compound (1), in addition to the isolation of nine previously reported compounds. These included five dicoumarinyl ethers found in Thymelaea: daphnoretin methyl ether (2), rutamontine (3), neodaphnoretin (4), acetyldaphnoretin (5), and edgeworthin (6); two flavonoids: genkwanin (7) and trans-tiliroside (8); p-hydroxy benzoic acid (9) and β sitosterol glucoside (10). Eight of the isolated compounds were tested for in vitro cytotoxicity against Vero and HepG2 cell lines using a sulforhodamine-B (SRB) assay. Compounds 1, 2 and 5 exhibited remarkable cytotoxic activities against HepG2 cells, with IC50 values of 8.6, 12.3 and 9.4 μM, respectively, yet these compounds exhibited non-toxic activities against the Vero cells. Additionally, compound 1 further exhibited promising cytotoxic activity against both MCF-7 and HCT-116 cells, with IC50 values of 4.26 and 9.6 μM, respectively. Compound 1 significantly stimulated apoptotic breast cancer cell death, resulting in a 14.97-fold increase and arresting 40.57% of the cell population at the Pre-G1 stage of the cell cycle. Finally, its apoptosis-inducing activity was further validated through activation of BAX and caspase-9, and inhibition of BCL2 levels. In silico molecular docking experiments revealed a good binding mode profile of the isolates towards Ras activation/pathway mitogen-activated protein kinase (Ras/MAPK); a common molecular pathway in the development and progression of liver tumors.

scholarly journals Synthesis and In Vitro Antitumor Activity of Novel Bivalent β-Carboline-3-carboxylic Acid Derivatives with DNA as a Potential Target

2018 ◽  
Vol 19 (10) ◽  
pp. 3179 ◽  
Author(s):  
Hongling Gu ◽  
Na Li ◽  
Jiangkun Dai ◽  
Yaxi Xi ◽  
Shijun Wang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Apoptosis ◽  
Docking Studies ◽  
In Vitro Cytotoxicity ◽  
Dependent Manner ◽  
Cycle Arrest ◽  
Dna Binding Affinity ◽  
Dose Dependent ◽  
Mcf 7

A series of novel bivalent β-carboline derivatives were designed and synthesized, and in vitro cytotoxicity, cell apoptosis, and DNA-binding affinity were evaluated. The cytotoxic results demonstrated that most bivalent β-carboline derivatives exhibited stronger cytotoxicity than the corresponding monomer against the five selected tumor cell lines (A549, SGC-7901, Hela, SMMC-7721, and MCF-7), indicating that the dimerization at the C3 position could enhance the antitumor activity of β-carbolines. Among the derivatives tested, 4B, 6i, 4D, and 6u displayed considerable cytotoxicity against A549 cell line. Furthermore, 4B, 6i, 4D, and 6u induced cell apoptosis in a dose-dependent manner, and caused cell cycle arrest at the S and G2/M phases. Moreover, the levels of cytochrome C in mitochondria, and the expressions of bcl-2 protein, decreased after treatment with β-carbolines, which indicated that 6i and 6u could induce mitochondria-mediated apoptosis. In addition, the results of UV-visible spectral, thermal denaturation, and molecular docking studies revealed that 4B, 6i, 4D, and 6u could bind to DNA mainly by intercalation.

scholarly journals EXTRACTION, ISOLATION, AND CHARACTERIZATION OF BIOACTIVE COMPOUNDS AND ESSENTIAL OIL FROM SYZYGIUM JAMBOS

2017 ◽  
Vol 10 (8) ◽  
pp. 194
Author(s):  
Mosad Ahmed Ghareeb ◽  
Manal Mortady Hamed ◽  
Abdel-aleem Hassan Abdel-aleem ◽  
Amal Mohamed Saad ◽  
Mohamed Sayed Abdel-aziz ◽  
...  
Keyword(s):  
Essential Oil ◽  
Radical Scavenging ◽  
Agar Plate ◽  
Antimicrobial Activities ◽  
Butanol Extract ◽  
Syzygium Jambos ◽  
Isolation And Characterization ◽  
Total Antioxidant ◽  
Total Oil

Objectives: Over the past few decades, phenolic compounds become important due to it has been associated with protection against different diseasesand sensory point of vision. Hence, at the present study, there has been a growing interest to carry out structural elucidation and characterization ofthe pure isolates from Syzygium jambos.Methods: S. jambos dried powder leaves were extracted by soaking in 85% methanol solvent at room temperature 25±2°C. The antioxidative activityof the isolates was assessed according to 2,2’-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging and phosphomolybdenum assays.Results: A total of 8 compounds were isolated from the n-butanol extract of S. jambos (Family Myrtaceae) plant, they were identified as quercetin-3-O-rutinoside (1), prenylbenzoic acid 4-β-D-glucoside (2), morolic acid 3-O-caffeate (3), 5,4’-dihydroxy, 7-methoxy, 6-methyl-flavone (4),3,4,5-trihydroxybenzoic acid (5), quercetin (6), isoetin-7-O-β-D-glucopyranoside (7), and (4’-hydroxy-3’-methoxyphenol-β-D-[6-O-(4”-hydroxy-3”,5”-dimethoxylbenzoate)] glucopyranoside) (8). Compounds 5 and 6 showed the most radical scavengers among the tested compounds with SC50 values of5.50 and 4.30 μg/ml, respectively, compared to ascorbic acid as standard and the total antioxidant capacity (TAC) values of 605.0 and 680.59 mg ascorbicacid equivalent/g compound, respectively. In vitro antimicrobial activities of the isolated compounds were tested using disc agar plate method againstfour pathogenic microbial strains including Gram-positive, Gram-negative bacteria and yeast with inhibition zones from 9 to 19 mm. Gas chromatographymassspectrometry analysis for the essential oil provides twenty four identified components representing 92% of its total oil composition.Conclusion: The results supported that S. jambos could be attributed to sources of natural antioxidant and antimicrobial applications.

scholarly journals Evaluation of phytochemical, antioxidant and cytotoxic potential of Sesbania grandiflora Linn.

2018 ◽  
Vol 7 (2) ◽  
pp. 191-198
Author(s):  
Shruti Gupta ◽  
◽  
Kishori G Apte ◽  
◽  
Keyword(s):  
Brine Shrimp ◽  
Reducing Power ◽  
In Vitro Cytotoxicity ◽  
Total Phenolic ◽  
Asian Countries ◽  
Leaf Extracts ◽  
Sesbania Grandiflora ◽  
Total Antioxidant ◽  
Potent Drug

Sesbania grandiflora Linn. is perennial branching, small erect quick-growing short-lived soft-wooded tree, mostly cultivated in southeast Asian countries including India and grows primarily in hot, humid environments. This study investigated on phytochemical values- total phenolic flavonoid, tannins and saponin contents for Sesbania grandiflora leaf extracts. The total antioxidant capacity, DPPH, reducing power, superoxide scavenging and Iron chelating effects were examined by established methods. In-vitro cytotoxicity by brine shrimp bioassay. Both the extracts of Sesbania grandiflora were found to possess moderate to high amounts of phytochemical contents. The total phenolic, flavonoid and saponin contents were found significantly higher in EQSG whereas tannins were more in AQSG. The EQSG and AQSG possessed low IC50 for H2O2 Scavenging (32.9, 27.3µg/ml), TAC (35.6, 41.8µg/ml) and moderate for DPPH (114.9, 113µg/ml) and reducing power (176.3, 181.6µg/ml) respectively. The Brine shrimp lethality bioassay showed a significantly high LC50 value with EQSG (10313µg/ml) and AQSG (12773µg/ml) compared to cyclophosphamide (110µg/ml) in cytotoxic assay. The results evidenced the potential of Sesbania grandiflora Linn. as potent drug with antioxidant and cytotoxic activity and could be useful for preparation of nutraceuticals for pharmaceutical use in the treatment of various human diseases and its complications

scholarly journals SYNTHESIS AND ANTITUMOR ACTIVITY OF NEW MULTIFUNCTIONAL COUMARINS

2020 ◽  
Vol 17 (36) ◽  
pp. 871-883
Author(s):  
Moath Kahtan BASHIR ◽  
Yasser Fakri MUSTAFA ◽  
Mahmood Khudhayer OGLAH
Keyword(s):  
Schiff Base ◽  
Antitumor Activity ◽  
Human Cancer ◽  
Biological Activities ◽  
Cell Viability Assay ◽  
Chemical Structures ◽  
Viability Assay ◽  
Schiff Base Formation ◽  
Mcf 7

Cancer constitutes one of the most severe public health menaces worldwide. It is imperative to synthesize new compounds and explore their antitumor activity to find a potential resolution to this health problem. Synthesis of new scaffolds and evaluating their antitumor activity is a relevant approach for combating cancer development. Coumarins can exhibit diverse biological activities, and one of these is the antitumor activity. This study aimed to synthesize new coumarins by grafting their precursors to the aromatic amines via Schiff base formation and evaluating their introductory antitumor activity. New multifunctional coumarins (MC1-MC9) were prepared by integrating a functionalized coumarin with different toluidine derivatives via a Schiff-base linkage. Spectral characterization inspired by FTIR, 1H- and 13C- NMR spectroscopies has established the chemical structures of the synthesized products. The antitumor activity was explored in vitro versus four dominant human cancer lines, including HeLa, SKG, MCF-7, and AMN3. The outcomes acquired from the cell viability assay inspected by applying MTT dye have revealed that the synthesized multifunctional coumarins, particularly MC3, have a hopeful activity. It can be concluded that a similar trend of activity against the test cell lines was observed for the synthesized coumarins, with the best action being versus MCF-7 and the least one versus AMN3. This study not only affords a new scaffold of a significant antitumor activity but also provides some insights into its structureactivity relationship.

Six New neo-Clerodane Diterpenoids from Aerial Parts of Scutellaria barbata and Their Cytotoxic Activities

Planta Medica ◽  
2018 ◽  
Vol 84 (17) ◽  
pp. 1292-1299 ◽  
Author(s):  
Guo-Chun Yang ◽  
Jia-Hui Hu ◽  
Bing-Long Li ◽  
Huan Liu ◽  
Jia-Yue Wang ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Cytotoxic Activities ◽  
Scutellaria Barbata ◽  
Human Cancer Cell Lines ◽  
Aerial Parts ◽  
Ic50 Values ◽  
Clerodane Diterpenoids

AbstractSix new neo-clerodane diterpenoids (1–6), scutebatas X – Z, A1-C1, along with twelve known ones (7–18) were obtained via the phytochemical investigation of the aerial parts of Scutellaria barbata. Their structures were established by detailed spectroscopic analysis. The absolute configurations of 1 and 2, as the representative members of this type, were identified based on a circular dichroic exciton chirality method. Moreover, in vitro cytotoxicity of compounds 1–6 were evaluated against three human cancer cell lines (SGC-7901, MCF-7, and A-549) using the MTT method. Compound 6 showed cytotoxic activities against all the three cell lines with IC50 values of 17.9, 29.9, and 35.7 µM, respectively.

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