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 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 Anticancer Evaluation of Plants from Indonesian Tropical Rain Forests

2011 ◽  
Vol 2 (3) ◽  
pp. 310
Author(s):  
Jamilah Abbas
Keyword(s):  
Hela Cell ◽  
Anticancer Activity ◽  
Cell Line ◽  
Stem Bark ◽  
Tropical Rainforests ◽  
Hela Cell Line ◽  
Tropical Rain Forests ◽  
Rain Forests ◽  
Anticancer Activities ◽  
Ic50 Value

The anticancer activities of medicinal plants from Indonesia’s tropical rainforests were investigated against Hela cell line. Maytenfoliol from leaves of Calophyllumtetrapterum 3-epibetulinic acid from stem bark of C. tomentosum Wight and D.A-friedo-oleanan-3-on from stem bark of C. moonii showed anticancer activity. The compound 3-epibetulinic acid showed the more potent anticancer activity than maytenfoliol and D.A-friedo-oleanan-3- with thean IC50 value were 3.17 μg/mL, 4.89 μg/mL and 5.63 μg/mL, respectively.Keywords: Anticancer evaluation, Hela cell line, Calophyllumtetrapterum. C. tomentosum Wight and C. moonii

Anticancer Evaluation and Docking Study of New Bifunctional Phthalazine Derivatives

2018 ◽  
Vol 15 (3) ◽  
pp. 414-422 ◽  
Author(s):  
Marwa G. El-Gazzar ◽  
Hala M. Aly
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
Anticancer Agents ◽  
Active Site ◽  
Cancer Cell Line ◽  
Docking Study ◽  
Quinazoline Derivative ◽  
Spectroscopic Measurements ◽  
Ic50 Value

Aims and Objective: A series of novel phthalazine derivatives was synthesized with versatile, readily accessible electrophilic and nucleophilic reagents. The newly synthesized compounds were confirmed by the results of spectroscopic measurements. Hence, their potential clinical application investigated in particular for cancer treatment. Materials and Methods: The newly synthesized compounds were characterized by spectroscopic measurements and were tested for their in vitro anticancer activity by MTT assay against human liver cancer cell line. Docking study of all the synthesized compounds was performed within the active site of the enzyme VEGFR-2 (Vascular Endothelial Growth Factor Receptor-2). Results: The quinazoline derivative 12 emerged as the most potent compound in this study with an IC50 value of 5.4 µM. Docking study showed that the synthesized compounds were fit in the VEGFR-2 active site almost at the same position of sorafenib and vatalanib with comparable docking scores (-15.20 to -8.92 was kcal/mol). Conclusion: we have synthesized a novel series of phthalazine derivatives and evaluated their potential anticancer activity against HEPG2 cell line. The quinazoline derivative 12 emerged as the most potent compound in this study with an IC50 value of 5.4 µM. The SAR and docking studies pointed out that rigidification of the structure resulted in better activity and better binding within the active site of VEGFR-2 as in compounds 3, 5, 6 and 12. These results introduced new phthalazine derivatives having promising activity which could lead to the development of more potent anticancer agents.

scholarly journals Synthesis of Flavone Derivatives via N-Amination and Evaluation of Their Anticancer Activities

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2723 ◽  
Author(s):  
Ni Zhang ◽  
Jin Yang ◽  
Ke Li ◽  
Jun Luo ◽  
Su Yang ◽  
...  
Keyword(s):  
Cell Line ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Prostate Cancer Cell Line ◽  
Antibacterial Activities ◽  
Anticancer Activities ◽  
Structure Activity ◽  
Ic50 Value ◽  
Erythroleukemia Cell ◽  
Flavone Derivatives

Seventeen new flavone derivatives substituted at the 4′-OH position were designed, synthesized and evaluated for their anticancer and antibacterial activities. Among them, compounds 3, 4, 6f, 6e, 6b, 6c and 6k demonstrated the most potent antiproliferative activities against a human erythroleukemia cell line (HEL) and a prostate cancer cell line (PC3). The results also showed that the IC50 value of compounds 3, 4, 6f, 6e, 6b, 6c and 6k were close to that of the anticancer drug cisplatin (DDP) and lower than that of apigenin. All of the derivatives did not present antibacterial activities. The structure–activity relationships evaluation showed that the configuration of methyl amino acid might affect their biological activities.

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 The Influence of Different Oregano Species on the Antioxidant Activity Determined Using HPLC Postcolumn DPPH Method and Anticancer Activity of Carvacrol and Rosmarinic Acid

2017 ◽  
Vol 2017 ◽  
pp. 1-7 ◽  
Author(s):  
Juste Baranauskaite ◽  
Asta Kubiliene ◽  
Mindaugas Marksa ◽  
Vilma Petrikaite ◽  
Konradas Vitkevičius ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Activity ◽  
Cell Line ◽  
Triple Negative ◽  
Anticancer Activities ◽  
Origanum Vulgare ◽  
Dpph Method ◽  
Ethanol Extracts ◽  
Mb231 Cell

The aim of this study was to evaluate concentration-dependent antioxidant and anticancer activities of CA and RA in ethanol extracts of three different Oregano species (Origanum onites L., Origanum vulgare L., and Origanum vulgare ssp. hirtum). The study revealed the highest RA antioxidant activity in O. vulgare ssp. hirtum (9550±95 mmol/g) and the lowest in O. vulgare L. (2605±52 mmol/g) (p<0.05). The highest CA amount was present in O. onites L., which was 1.8 and 4.7 times higher (p<0.05) than in O. vulgare ssp. hirtum and O. vulgare L., respectively. The anticancer activity was evaluated on human glioblastoma (U87) and triple-negative breast cancer (MDA-MB231) cell lines in vitro. RA anticancer activity was negligible. CA and the extracts were about 1.5–2 times more active against MDA-MB231 cell line (p<0.05) compared to U87 cell line. The anticancer activities of three tested extracts were similar against U87 cell line (p>0.05) but they had different activities against MDA-MB231 cell line.

scholarly journals Synthesis and Anticancer Activity of Novel Benzofurancarboxamides

2020 ◽  
Vol 10 (6) ◽  
pp. 6597-6609
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
National Cancer Institute ◽  
Efficient Synthesis ◽  
Anticancer Activities ◽  
Developmental Therapeutics Program ◽  
Activity Evaluation ◽  
Developmental Therapeutics

In our present work, we presented an efficient synthesis and anticancer activity evaluation of some novel benzofurancarboxamides. Our proposed approaches provide the possibility to design benzofurans diversity with a considerable chemical novelty. The synthesized substances were selected by the National Cancer Institute (NCI) Developmental Therapeutics Program for the in vitro cell line screening to investigate their anticancer activity. The compounds with significant levels of anticancer activities have been found that can be used for further optimization.

scholarly journals Penentuan Aktivitas Antikanker Fraksi Etil Asetat Daun Bandotan (ageratum conyzoides linn.) Terhadap Cell Line Kanker Kolon WiDr

2020 ◽  
Vol 3 (2) ◽  
pp. 33-40
Author(s):  
Linda Lusiantika ◽  
Esti Wahyu Widowati ◽  
Miranda Adihimawati
Keyword(s):  
Ethyl Acetate ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cancer Cell Line ◽  
Colon Cancer Cell Line ◽  
Phytochemical Screening ◽  
Ageratum Conyzoides ◽  
Ic50 Value ◽  
Screening And Identification

 A research to test the anticancer activity of in vitro anticancer activity against colon cancer cell line WiDr Ageratum conyzoides Linn.leafs. The aims of this study are to determine anticancer activity using MTT method. The method used is the extraction of secondary metabolites using maceration with n-hexane, ethyl acetate and ethanol, followed by TLC. Crude extract maceration results that have the highest yield selected and separated by fractions using KKV. Fractions with the greatest weight was chosen to be tested anticancer activity against WiDr cell line by MTT assay. Phytochemical screening and identification of compounds by GC-MS carried out on the fraction which has the lowest IC50 value. Maceration results showed that crude ethyl acetate extract had the highest amount of yield at 7.31% and has the best separation results of TLC is characterized by the highest number of stains. Separation by KKV produce 21 fractions, 4 fractions were selected based on the weight of the total of the fraction 6, 13, 14 and 15. Test anticancer activity with a concentration of 62.5; 125; 250; 500 and 1000 mg mL-1 shows the fraction 6 has the lowest IC50 value is 251.48 mg mL-1. Based on this, the fraction 6 does not have anticancer activity. Although, the phytochemical screening showed alkaloids and terpenoids as well as the result of identification with GC-MS indicated the presence of compounds 2H-benzopyran and neophytadiene Keywords: Ageratum conyzoides Linn. leaves, Column Cromatography Vacuum, anticancer, phytochemical, GC-MS

Synthesis, Docking Study, Cytotoxicity, Antioxidant, and Anti-microbial Activities of Novel 2,4-Disubstituted Thiazoles Based on Phenothiazine

2020 ◽  
Vol 17 (2) ◽  
pp. 151-159
Author(s):  
Tran Nguyen Minh An ◽  
Pham Thai Phuong ◽  
Nguyen Minh Quang ◽  
Nguyen Van Son ◽  
Nguyen Van Cuong ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Antimicrobial Activities ◽  
Significant Activity ◽  
Thiazole Derivatives ◽  
Ligand Interaction ◽  
Ic50 Value ◽  
Mcf 7

: A series of novel 1,3-thiazole derivatives (5a-i) with a modified phenothiazine moiety were synthesized and tested against cancer cell line MCF-7 for their cytotoxicity. Most of them (5a-i) were less cytotoxic or had no activity against MCF-7 cancer cell line. Material and Methods: The IC50 value of compound (4) was 33.84 μM. The compounds (5a-i) were also evaluated for antimicrobial activities, but no significant activity was observed. The antioxidant activity was conducted for target compounds (5a-i). The IC50 value of compound (5b) was 0.151mM. Results: The total amount of energy, ACE (atomic contact energy), energy of receptor (PDB: 5G5J), and ligand interaction of structure (4) were found to be 22.448 Kcal.mol-1 , -247.68, and -91.91 Kcal.mol-1, respectively. The structure (4) is well binded with the receptor because the values of binding energy, steric energy, and the number of hydrogen bondings are -91.91, 22.448 kcal.mol-1, and 2, respectively. It shows that structure (4) has good cytotoxicity with MCF-7 in vitro. Conclusion: The increasing of docking ability of structures (5a-i) with the receptor is presented in increasing order as (5f)>(5e)>(5g)>(5a)>(5b)>(5d)>(5c)>(5i)>(5h). The structure bearing substitution as thiosemicarbazone (4), nitrogen heterocyclic (5f), halogen (5e), and azide (5g) showed good cytotoxicity activity in vitro.

(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.

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