scholarly journals V. NEGUNDO, L. CAMARA AND B. VARIEGATA PLANTS LEAF EXTRACT EXHIBIT CONSIDERABLE IN VITRO ANTIOXIDANT AND ANTICANCER ACTIVITIES

2017 ◽  
Vol 9 (5) ◽  
pp. 227
Author(s):  
Nutan Badgujar ◽  
Kinnari Mistry ◽  
Jagdish Patel
Keyword(s):  
Anticancer Activity ◽  
Methanolic Extract ◽  
Assay Method ◽  
Human Neuroblastoma Cell ◽  
Anticancer Activities ◽  
Human Neuroblastoma ◽  
Antioxidant Power ◽  
Methanolic Extracts ◽  
Ic50 Value

Objective: The study was planned to investigate antioxidant and anticancer activities with the preliminary phytochemical analysis of methanolic extracts of Vitex negundo (V. negundo), Lantana camara (L. camara) and Bauhania variegata (B. variegata) plants leaf extracts.Methods: Phytochemical evaluation was performed for all the extracts, as per the standard methods. In vitro antioxidant activities were performed by using DPPH (2,2-Diphenyl-1-Picrylhydrazyl), ABTS (2, 2'-Azino-Bis-3-Ethylbenzothiazoline-6-Sulfonic Acid) and FRAP (Ferric reducing antioxidant power assay) method and compared with standard antioxidants. The anticancer activity of plant extract was assessed using MTT colorimetric assay.Results: The study of preliminary phytochemical proved the existence of alkaloids, flavonoids and phenolic types of phytochemicals in high amount. Methanolic extract of L. camara shows minimum IC50 value for DPPH assay (48.75±2.34 µg/ml) and FRAP assay (274.66±3.65 µg/ml). In ABTS assay B. variegata extract exhibit minimum IC50 value (60.48±3.01 µg/ml). Lower the IC50 value of extract, higher the effectiveness of the plant. Methanolic extract of all plants methanolic extracts showed anticancer activity against SH-SY-5Y cells (human neuroblastoma cell) but V. negundo was more effective against SH-SY-5Y cells with IC50 value (209 µg/ml) compared to remaining extracts.Conclusion: The current finding accomplished the in vitro activities, so that plant could be a superior source of antioxidant and anticancer drugs. But further in vivo assessment was needed before adding it into the pharma industry.

scholarly journals Antiproliferative Activity and Apoptotic Efficiency of Syzygium cumini Bark Methanolic Extract against EAC Cells In Vivo

2020 ◽  
Vol 20 ◽  
Author(s):  
Mst. Ayesha Siddika ◽  
Plabon K. Das ◽  
Saharia Y. Asha ◽  
Suraiya Aktar ◽  
Abu Rahyan M. Tareq ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Antiproliferative Activity ◽  
Methanolic Extract ◽  
Chemical Constituents ◽  
Antioxidant Properties ◽  
In Vitro Assays ◽  
Syzygium Cumini ◽  
Anticancer Activities ◽  
Eac Cells

Background: Syzygium cumini, one of the evidence-based traditional medicinal plant used in the treatment of various ailments. Objectives: Herein, the antioxidant property and anticancer property of Syzygium cumini against Ehrlich Ascites Carcinoma (EAC) were examined in search of effective chemotherapeutics. Methods: In vitro assays, phytochemical and chromatographic analysis were used to determine antioxidant properties and chemical constituents of Syzygium cummini bark methanolic extract (SCBME). Functional assays were used to measure the anticancer activity of SCBME. Fluorescence microscopy and RT-PCR were used to examine morphological and molecular changes of EAC cells followed by SCBME treatment. Results: Phytochemical and GC–MS analysis confirmed the presence of compounds with antioxidant and anticancer activities. Accordingly, we have noted a strong antioxidant activity of SCBME with an IC50 value of 10μg/ml. Importantly, SCBME exerted a dose-dependent anticancer activity with significant inhibition of EAC cell growth (71.08 ± 3.53%; p<0.001), reduction of tumour burden (69.50%; p<0.01) and increase of life span (73.13%; p<0.001) of EACbearing mice at 75mg/kg/day. Besides, SCBME restored the blood toxicity towards normal in EAC-bearing mice (p<0.05). SCBME treated EAC cells showed apoptotic features under a fluorescence microscope and fragment DNA in DNA laddering assay. Moreover, up-regulation of the tumour suppressor p53 and pro-apoptotic Bax and down-regulation of NF-κB and anti-apoptotic Bcl-2 genes, implied induction of apoptosis followed by SCBME treatment. Conclusion: The antiproliferative activity of SCBME against EAC cells is likely due to apoptosis, mediated by regulation of p53 and NF-κB signalling. Thus, SCBME can be considered as a useful resource in cancer chemotherapy.

scholarly journals SYNTHESIS, CHARACTERIZATION AND EVALUATION OF 4-HYDROXY-1-PHENYL/METHYL-3-(3-SUBSTITUTED-1-(SUBSTITUTEDIMINO) PROPYL) QUINOLINE-2(1H)-ONE DERIVATIVES AND 4-HYDROXY-1-PHENYL/METHYL-3-(1-(SUBSTITUEDIMINO) ETHYL) QUINOLINE-2(1H)-ONE DERIVATIVES AS POSSIBLE ANTICANCER AGENTS

2017 ◽  
Vol 9 (10) ◽  
pp. 240 ◽  
Author(s):  
S. N. Mamle Desai ◽  
Rudrax N. S. Priolkar ◽  
Harshank A. Naik Karmali ◽  
Prabhav D. Ambe ◽  
B. S. Biradar
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Mtt Assay ◽  
Anticancer Agents ◽  
K562 Cell ◽  
Assay Method ◽  
Substituted Anilines ◽  
Ic50 Value ◽  
Substituted 1

Objective: Synthesis, characterization and evaluation of quinolin-2-one derivatives as possible anticancer agents.Methods: A series of novel 4-hydroxy-1-phenyl/methyl-3-(3-substituted-1-(substitutedimino)propyl)quinolin-2(1H)-one derivatives IIa(1-5)/IIb(1-5) and 4-hydroxy-1-phenyl/methyl-3-(1-(substituedimino)ethyl)quinolin-2(1H)-one derivatives IIIa(1-3)/IIIb(1-3) were synthesised by nucleophilic addition of substituted anilines on 3-acetyl-4-hydroxy-1-phenyl/methylquinolin-2(1H)-one (a/b) and 4-hydroxy-3-(3-substitutedpropanoyl)-1-phenyl/methyl quinolin-2(1H)-one (Ia/Ib); respectively. The synthesised derivatives were characterised by spectral analysis and were tested for their in vitro anticancer activity against K562 and Hep 3b cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method.Results: The compounds were tested for their in vitro anticancer activity against K562 and Hep 3b cell lines at 10, 20, 25, 30 and 50 µg/ml concentration using MTT assay method. The compound 4-hydroxy-3-(3-morpholino-1-(phenylimino)propyl)-1-phenylquinolin-2(1H)-one (IIa-1) showed anticancer activity with IC50 value 20 µg as compared to the control against K562 cell lines. The compound 4-hydroxy-1-phenyl-3-(1-(phenylimino) ethyl) quinolin-2(1H)-one (IIIa-1) showed anticancer activity with IC50 value less than 10 µg.Conclusion: The proposed method for the synthesis of novel derivatives is convenient and gives a good yield. Some of the synthesised compounds showed promising anticancer activity against K562 and Hep 3b cell lines. Compound IIa-1 (R=-C6H5; R1= morpholine; R2= C6H5-NH-) exhibited most potent activity against K562 cell lines. Compound IIIa-1 (R=-C6H5; R3= C6H5-NH-) has been proved to be the most cytotoxic compound among the other derivatives against Hep 3b cell lines.

scholarly journals Evaluation of in vitro Antioxidant and Cytotoxic Effect of Methanol Extract from aerial parts of Myristica beddomei King ssp. ustulata W.J. de Wilde

2020 ◽  
pp. 115-121
Author(s):  
Neethu Joy ◽  
Mahesh Mohan
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Activity ◽  
Cytotoxic Effect ◽  
Total Phenolic ◽  
Ovarian Cancer Cells ◽  
Cytotoxicity Test ◽  
Antioxidant Power ◽  
Ic50 Value ◽  
Dpph Method

Plants are traditionally used for pharmacological activities because of its ability to produce bioactive compounds. Myristica beddomei King ssp. ustulata W.J. de Wilde is an ethnomedicinal plant and it is seen in South Western Ghats of Kerala, India. The present study assessed the phenolic content, flavonoid concentration, in vitro antioxidant and cytotoxic effect of different parts of Myristica beddomei King. The total phenolic contents in the extracts ranged from 96.29 (pericarp) to 314.47 (bark) mg g-1 gallic acid equivalent. The concentration of flavonoids in different plant part extracts ranged from 1.81   to 2.76 mg g-1 equivalent to quercetin. All the parts exhibited potential antioxidant activity with an IC50 value of 2.87 to 9.67 μg ml-1 when compared to the standard ascorbic acid with an IC50 value of 2 μg ml-1 in 1,1-diphenyl-2- picryl-hidrasil (DPPH) method. Bark showed highest activity in terms of DPPH radical scavenging (IC50 value of 2.87 µg ml-1), phosphomolybdenum test (2261.33 ± 1.65 mg g-1 trolox equivalent) and ferric ion reducing antioxidant power (FRAP) (113.1 ± 0.28 µmol Fe2+ µg-1) while pericarp showed low antioxidant activity. The in vitro screening results revealed that the seeds exhibited promising anticancer activity compared to PA1 (Ovarian Cancer) cells (50 % inhibition) were observed at a concentration 100.68 µg ml-1.  In cytotoxicity test L929 (Fibroblast) cell line compared to the other parts pericarp, mace and seed needed higher concentration (>240 µg ml-1) for LC50 value. It is a promising plant for further development of antioxidant agent as it got high content of phenolic compounds and potential antioxidant and anticancer activity.

scholarly journals Biotransformation of oleic acid and antimicrobial and anticancer activities of its biotransformatıon extracts

2019 ◽  
Vol 51 (2) ◽  
pp. 200-205
Author(s):  
Ö. Özşen Batur ◽  
Ö. Atlı ◽  
İ. Kıran
Keyword(s):  
Oleic Acid ◽  
Anticancer Activity ◽  
Cell Line ◽  
Clinical Isolate ◽  
Alternaria Alternata ◽  
Edible Oils ◽  
Biological Activities ◽  
Anticancer Activities ◽  
Ic50 Value

Oleic acid is an unsaturated fatty acid found in significant quantities in various edible oils. Scientific studies have shown that oleic acid and its derivatives exhibit a variety of biological activities including antimicrobial and anticancer activities. In the present work, biotransformation of oleic acid was carried out initially using 27 different microbial strains. Extracts obtained from biotransformation with Alternaria alternata (clinical isolate) and Aspergillus terreus var. africanus (clinical isolate) were used in antimicrobial and anticancer activity studies. The in vitro antimicrobial activities of the extracts were evaluated against 9 different pathogenic microorganisms. The results indicated that the microbial extracts were more active than oleic acid itself and showed good inhibitory activity against all tested microorganisms. In in vitro anticancer activity studies, extract 2 obtained from biotransformation with Alternaria alternata exhibited notable anticancer activity against A549 cell line with an IC50 value of 62.5 μg/ml whereas positive control cisplatin showed an IC50 value of 43.5 μg/ml. The anticancer activity of extract 2 was also found to be selective according to its higher IC50 value (122.7 μg/ml) obtained against the healthy cell line, mouse embryonic fibroblasts, NIH3T3. Due to its anticancer effect, extract 2 is considered to participate in further research.

scholarly journals SEAWEED EXTRACTS EXHIBIT ANTICANCER ACTIVITY AGAINST HeLa CELL LINES

2016 ◽  
Vol 9 (1) ◽  
pp. 114 ◽  
Author(s):  
Ashwini S. ◽  
Suresh Babut V. ◽  
Saritha . ◽  
Manjula Shantara Shantaram
Keyword(s):  
Anticancer Activity ◽  
Potential Candidate ◽  
Anticancer Activities ◽  
Vitro Assay ◽  
Anticancer Properties ◽  
Seaweed Extracts ◽  
Hela Cell Lines ◽  
Ic50 Value ◽  
Ethanol Extracts

Objective: This study was conducted to examine the anticancer activities in the extracts of marine seaweeds Gracilariacorticata.Methods: The acetone, chloroform, ethanol, methanol and aqueous extracts of collected seaweeds were tested for their anticancer properties in vitro against HeLa cancer cell lines.Results: The anticancer activity of the seaweed extracts was observed at 24hours, 48 hours and 72 h in which chloroform and ethanol extracts of G. corticata showed a greater activity with an IC50 value of 341.82 µg/ml and 244.7 µg/ml respectively for 48hours. P-values were determined by two-way analysis of variance (ANOVA). The morphology of the treated cells showed a great variation when compared to the control cells. Thus, the in vitro assay indicates that the extracts of seaweeds are the significant source of a noble anticancer agent.Conclusion: This study also infers that G. corticata could be a potential candidate for cancer therapy in the near future.

scholarly journals Methanolic Bark Extract of Abroma augusta (L.) Induces Apoptosis in EAC Cells through Altered Expression of Apoptosis Regulatory Genes

2020 ◽  
Vol 2020 ◽  
pp. 1-14
Author(s):  
Masum Miah ◽  
Ajmeri Sultana Shimu ◽  
Shafi Mahmud ◽  
Farjana-Binta Omar ◽  
Ratna Khatun ◽  
...  
Keyword(s):  
Hemolytic Activity ◽  
Methanolic Extract ◽  
Apoptotic Cell ◽  
Docking Simulation ◽  
Assay Method ◽  
Bark Extract ◽  
Anticancer Activities ◽  
Altered Expression ◽  
Eac Cells

Abroma augusta (L.), one of the herbal medicinal plants, is widely used for treatment of various maladies. The present study was initiated to determine the antioxidant, hemolytic, cytotoxicity, and anticancer activities of methanolic extract from the bark of the plant. The phytochemical screening was done by analyzing different phytochemicals present in the extract. We observed the presence of alkaloids, steroids, terpenoids, flavonoids, reducing sugars, and glycosides in the bark extract which showed the highest antioxidant capacity. Antioxidant potential of the methanolic extract was evaluated in vitro by DPPH (2,2-diphenyl-1-picrylhydrazyl) scavenging assay method. This extract showed prominent scavenging activity with IC50 value of 38.65 μg/ml. The hemolytic activity of the extract was evaluated at concentrations ranging from 250 to 1000 μg/ml. It was observed that the extract induced hemolysis percentage of 9.41% to 4.1%, which implies that the extract has no potent hemolytic activity. Cytotoxicity and anticancer activities were observed on Ehrlich ascites carcinoma (EAC) cells. In addition, the bark showed promising cytotoxicity with IC50 value of 329.41 μg/ml, and the study indicated that the extract was capable of inhibiting EAC cell growth by 75.5% when administered at 100 mg/kg/day body weight intraperitoneally for five consecutive days to Swiss albino mice. Morphological change of apoptotic cell was determined by fluorescence and optical microscopy. DNA fragmentation is another marker for apoptosis, and the bark extract-treated EAC cells showed smeared and fragmented DNA bands. Apoptosis correlated well with the upregulation of p53 and Bax and also with the downregulation of NF-κB and Bcl-2. Furthermore, activity and interaction of two A. augusta compounds were tested through molecular docking simulation study. In conclusion, our results suggest that A. augusta bark has the potential to be considered as an anticancer agent.

scholarly journals EVALUATION OF ANTIOXIDANT AND CHEMOPREVENTIVE POTENTIAL OF METHANOLIC EXTRACTS OF LEAF OF AEGLEMARMELOS ATTRIBUTES TOWARDS DUCTAL CARCINOMA STUDIED IN MCF7 CELLS

2018 ◽  
pp. 21-25
Author(s):  
B. Arirudran ◽  
B. Janani ◽  
U. S. Mahadeva Rao
Keyword(s):  
Nitric Oxide ◽  
Mcf7 Cell ◽  
Ductal Carcinoma ◽  
Methanolic Extract ◽  
Research Work ◽  
Antioxidant Potential ◽  
Mcf7 Cells ◽  
Methanolic Extracts ◽  
Ic50 Value

Objective: The objective of the present research work had been made to evaluate the antioxidant potential along with anti-cancer activity of methanolic extracts from the leaf of A. marmelos. Methods: Standard methods for antioxidant potential in terms of DPPH and nitric oxide scavenging assay, and anticancer activity in vitro method (Cytotoxicity/MTT assay and % of cell viability) by using MCF7 cell line. Results: Results of antioxidant efficacy revealed that the IC50 value for DPPH and nitric oxide scavenging assay was considered to be 62.032%, and 20.69% respectively. The methanolic extract of A. marmelos was found to possess enhanced anticancer potential against MCF7 cells. Cytotoxicity activity of MCF7 cells, when treated with methanolic extract of A. marmelos, was found to be 43.42% at 25µg, 52.31% at 50µg, 56.31% at 75µg, 58.38% at 100µg, 62.25% at 125µg. The IC50 value was found as 49.36µg. Toxicity was significantly increased with increased concentration and viability significantly decreased with the increased concentration of methanolic extract of leaf from A. marmelos for MCF7 cell when compared to cyclophosphamide. Conclusion: From the studies, it was postulated that methanolic extract of leaf from A. marmeloshas significant chemopreventive activity. These specific identities will be useful for the identification and authentication of raw drug.

p-Trifluoroacetophenone Oxime Ester Derivatives: Synthesis, Antimicrobial and Cytotoxic Evaluation and Molecular Modeling Studies

2020 ◽  
Vol 17 (2) ◽  
pp. 169-183 ◽  
Author(s):  
İrem Bozbey ◽  
Suat Sari ◽  
Emine Şalva ◽  
Didem Kart ◽  
Arzu Karakurt
Keyword(s):  
Molecular Modeling ◽  
Neuroblastoma Cell ◽  
Neuroblastoma Cells ◽  
Cytotoxic Agents ◽  
Human Neuroblastoma Cell ◽  
Human Neuroblastoma ◽  
Modeling Studies ◽  
Broth Microdilution Method ◽  
Molecular Modeling Studies

Background: Azole antifungals are among the first-line drugs clinically used for the treatment of systemic candidiasis, a deadly type of fungal infection that threatens mostly immunecompromised and hospitalized patients. Some azole derivatives were also reported to have antiproliferative effects on cancer cells. Objective: In this study, 1-(4-trifluoromethylphenyl)-2-(1H-imidazol-1-yl)ethanone (3), its oxime (4), and a series of its novel oxime ester derivatives (5a-v) were synthesized and tested for their in vitro antimicrobial activities against certain ATCC standard strains of Candida sp. fungi and bacteria. The compounds were also tested for their cytotoxic effects against mouse fibroblast and human neuroblastoma cell lines. Molecular modeling studies were performed to provide insights into their possible mechanisms for antifungal and antibacterial actions. Methods: The compounds were synthesized by the reaction of various oximes with acyl chlorides. Antimicrobial activity of the compounds was determined according to the broth microdilution method. For the determination of cytotoxic effect, we used MTS assay. Molecular docking and QM/MM studies were performed to predict the binding mechanisms of the active compounds in the catalytic site of C. albicans CYP51 (CACYP51) and S. aureus flavohemoglobin (SAFH), the latter of which was created via homology modeling. Results: 5d, 5l, and 5t showed moderate antifungal activity against C. albicans, while 3, 5c, and 5r showed significant antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa. Most of the compounds showed approximately 40-50% inhibition against the human neuroblastoma cells at 100 µM. In this line, 3 was the most potent with an IC50 value of 82.18 μM followed by 5a, 5o, and 5t. 3 and 5a were highly selective to the neuroblastoma cells. Molecular modelling results supported the hypothesis that our compounds were inhibitors of CAYP51 and SAFH. Conclusion: This study supports that oxime ester derivatives may be used for the development of new antimicrobial and cytotoxic agents.

(Substituted)-benzo[b]thiophene-4-carboxamide Synthesis and Antiproliferative Activity Study

2020 ◽  
Vol 17 (5) ◽  
pp. 563-573 ◽  
Author(s):  
Chandrakant Dhondiram Pawar ◽  
Dattatraya Navnath Pansare ◽  
Devanand Baburao Shinde
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Proliferative Activity ◽  
Thiophene Ring ◽  
Amide Group ◽  
Peptide Coupling ◽  
Ic50 Value ◽  
Important Building Block ◽  
Mcf 7

Background: Thiophene ring forms important building block in medicinal chemistry. Literature reveals that thiophene ring in combination with different groups shows different activity. By keeping these things in mind we have designed and synthesized a new series of amide and sulfonamide coupled thiophene. A series of novel substituted 3-sulfamoylbenzo[b]thiophene-4- carboxamide molecules containing sulfonamide and amide group were designed, synthesized and used for anti-proliferative activity study. Methods: The final compounds 16-36 were synthesized by using series of reactions comprising sulfonation, sulfonamide coupling, hydrolysis and peptide coupling. The yields of compounds 16- 36 are in the range of 90-98%. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, 13C NMR, LCMS and the purity was checked through HPLC analysis. The compounds were further tested for their in vitro anticancer activity against a series of cell lines A549, HeLa, MCF-7 and Du-145. Results: The intermediates 8-13, 15 and final compounds 16-36 were synthesized in good yields. The synthesized compounds were further tested for their anticancer activity and most of compounds showed moderate to good anticancer activity against all four cell lines. Conclusion: We have synthesized 21 compounds and were screened for anticancer activity against MCF-7, HeLa, A-549 and Du-145 cancer cell lines. Most of the compounds were active for tested cell lines with IC50 value in the range of 1.81 to 9.73 μM. The compounds 18, 19, 21, 25, 30, 31 and 33 are most active in cell line data with IC50 value in the range of 1.81 to 2.52 μM.

Phenolic constituents and inhibitory effects of the leaf of Rauvolfia vomitoria Afzel on free radicals, cholinergic and monoaminergic enzymes in rat’s brain in vitro

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Olubukola H. Oyeniran ◽  
Adedayo O. Ademiluyi ◽  
Ganiyu Oboh
Keyword(s):  
Lipid Peroxidation ◽  
Free Radicals ◽  
Methanolic Extract ◽  
Array Detector ◽  
Oh Radicals ◽  
Inhibitory Effects ◽  
Methanolic Extracts ◽  
Phenolic Constituents ◽  
Rauvolfia Vomitoria

AbstractObjectivesRauvolfia vomitoria is a medicinal plant used traditionally in Africa in the management of several human diseases including psychosis. However, there is inadequate scientific information on the potency of the phenolic constituents of R. vomitoria leaf in the management of neurodegeneration. Therefore, this study characterized the phenolic constituents and investigated the effects of aqueous and methanolic extracts of R. vomitoria leaf on free radicals, Fe2+-induced lipid peroxidation, and critical enzymes linked to neurodegeneration in rat’s brain in vitro.MethodsThe polyphenols were evaluated by characterizing phenolic constituents using high-performance liquid chromatography coupled with diode array detector (HPLC-DAD). The antioxidant properties were assessed through the extracts ability to reduce Fe3+ to Fe2+; inhibit ABTS, DPPH, and OH radicals and Fe2+-induced lipid peroxidation. The effects of the extracts on AChE and MAO were also evaluated.ResultsThe phenolic characterization of R. vomitoria leaf revealed that there were more flavonoids present. Both aqueous and methanolic extracts of R. vomitoria leaf had inhibitory effects with the methanolic extract having higher significant (p≤0.05) free radicals scavenging ability coupled with inhibition of monoamine oxidases. However, there was no significant (p≤0.05) difference obtained in the inhibition of lipid peroxidation and cholinesterases.ConclusionThis study suggests that the rich phenolic constituents of R. vomitoria leaf might contribute to the observed antioxidative and neuroprotective effects. The methanolic extract was more potent than the aqueous extract; therefore, extraction of R. vomitoria leaf with methanol could offer better health-promoting effects in neurodegenerative condition.

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