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 Synthesis of Novel and Potential Antimicrobial, Antioxidant and Anticancer Chalcones and Dihydropyrazoles Bearing Isoxazole Scaffold

Proceedings ◽  
2020 ◽  
Vol 41 (1) ◽  
pp. 16
Author(s):  
Afzal Shaik ◽  
Palleapati Kishor ◽  
Venkata Kancharlapalli
Keyword(s):  
Antioxidant Activities ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Prostate Cancer Cell Line ◽  
Antifungal Compound ◽  
Anticancer Activities ◽  
Anticancer Properties ◽  
Structure Activity ◽  
Normal Human Cell ◽  
Normal Human

A series of isoxazole based (E)-1-(isoxazole-5-yl)-3-(substituted phenyl)-prop-2-en-1-ones (chalcones, 3a-3o) and 3-(isoxazol-5-yl)-5-(substituted phenyl)-4,5-dihydro-1H-pyrazole-1-carboxamide (dihydropyrazoles, 4a-4o) were synthesized, characterized and evaluated for their antimicrobial, antioxidant and anticancer properties. Chalcones exhibited excellent antibacterial and antioxidant activities whereas the dihydropyrazoles shown superior antifungal and anticancer activities. The compound 3l containing 3,4,5-trimethoxy phenyl ring showed the potent antibacterial activity (MIC = 1 µg/mL) as well as the antioxidant activity (IC50 = 5 µg/mL) whereas the dihydropyrazole, 4o (MIC = 0.5 µg/mL) bearing the 2-chloro-3,4-dimethoxyphenyl was the potent antifungal compound identified. The dihydropyrazoles 4n and 4h possessing 2-fluoro-3,4-dimethoxyphenyl and 3,4-dimethoxyphenyl substituents exhibited potent anticancer activity against prostate cancer cell line (DU-145) with MIC 2 and 4 µg/mL respectively. The structure activity relationships had shown that there is a marked influence of both electron withdrawing halogens and electron releasing methoxyl groups on the above biological activities. All the compounds were evaluated for toxicity on normal human cell lines (LO2) and found to be non-toxic. These studies could help to synthesize, explore and identify new isoxazole containing leads for antimicrobial, antioxidant and anticancer properties.

scholarly journals Quantitative Structure-Activity Relationship Study of Curcumin Analogues as Anti-proliferative Agents of Human Prostate Cancer Cell Line (PC-3)

KIMIKA ◽  
2013 ◽  
Vol 24 (1) ◽  
pp. 8-17
Author(s):  
Andrea Marie M. Reyes ◽  
Junie B. Billones
Keyword(s):  
Prostate Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Prostate Cancer Cell ◽  
Cancer Cell Line ◽  
Prostate Cancer Cell Line ◽  
Quantitative Structure Activity Relationship ◽  
Quantitative Structure ◽  
Curcumin Analogues ◽  
Structure Activity

A quantitative structure-activity relationship (QSAR) study has been performed on curcumin analogues in order to establish the effect of variation of structural, electronic and topological properties  on  the  anti-proliferative  activity  against  prostate  cancer  cell  line  PC-3.  The structure-based  properties  were  calculated  by  the  use  of  Hyperchem®  and  Dragon® softwares  and  the  multi-linear  regression  equations  were  generated  by  the  use  of  SPSS® software. Six models of PC-3 activity have been developed according to the types of QSAR descriptors.  All  models  were  cross-validated  using  leave-one-out  (LOO)  method.  The models  indicate  that  a  more  potent  curcumin  derivative  against  PC-3  should  have  smaller surface area, greater volume, lower polarizability, and fewer oxygen and multiple bonds.

scholarly journals In Vitro Phytochemical Screening, Cytotoxicity Studies of Curcuma longa Extracts with Isolation and Characterisation of Their Isolated Compounds

Molecules ◽  
2021 ◽  
Vol 26 (24) ◽  
pp. 7509
Author(s):  
Madhuri Grover ◽  
Tapan Behl ◽  
Aayush Sehgal ◽  
Sukhbir Singh ◽  
Neelam Sharma ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Curcuma Longa ◽  
Cancer Cell Line ◽  
Prostate Cancer Cell Line ◽  
Cytotoxic Potential ◽  
Healthy Cell ◽  
Vero Cell Line ◽  
Ic50 Value ◽  
Phytochemical Constituents

The Curcuma longa plant is endowed with multiple traditional and therapeutic utilities and is here explored for its phytochemical constituents and cytotoxic potential. Turmeric rhizomes were extracted from three different solvents and screened for the presence of different phytochemical constituents, observation of which indicated that the polar solvents favoured extraction of greater versatile phytochemical constituents. These extracts were investigated for their cytotoxic potential by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay on three different of cell lines including SCC-29B (oral cancer cell line), DU-145 (prostate cancer cell line) and the Vero cell line (healthy cell line/non-cancerous cell line). This assay was performed by taking three extracts from isolated curcuminoids and a pure bioactive compound bisdemethoxycurcumin (BD). Bisdemethoxycurcumin was isolated from curcuminoids and purified by column and thin-layer chromatography, and its structural characterisation was performed with different spectroscopic techniques such as FTIR, NMR (1H Proton and 13C Carbon-NMR) and LC-MS. Amongst the extracts, the ethanolic extracts exhibited stronger cytotoxic potential against the oral cancer cell line (SCC-29B) with an IC50value of 11.27 μg/mL,and that this was too low of a cytotoxicity against the Vero cell line. Although, curcuminoids have also shown a comparable cytotoxic potential against SCC-29B (IC50 value 16.79 μg/mL), it was not as potent against the ethanolic extract, and it was even found to be cytotoxic against healthy cell lines at a very low dose. While considering the isolated compound, bisdemethoxycurcumin, it also possessed a cytotoxic potential against the prostate cancer cell line (DU-145) (IC50 value of 93.28 μg/mL), but was quite safe for the healthy cell line in comparison to doxorubicin.

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 Anticancer activity of food grade nanoemulsions on hepatic cancer cells: a comparative study

2020 ◽  
Author(s):  
Sayyeda Hira Hassan ◽  
Muhammad Rehan Khan
Keyword(s):  
Olive Oil ◽  
Cell Line ◽  
Mtt Assay ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Flax Seed ◽  
Anticancer Activities ◽  
Ic50 Value ◽  
Flax Seeds

Abstract The current study was aimed to prepare stable NEs from plant oils to evaluate their cytotoxic effect on HepG2 cells. Oils form three different samples (flax seeds, cloves and olives) were extracted. NEs from these oils were prepared separately by ultrasonication method. After characterization of stable NEs, they were evaluated for their antioxidant and anticancer activities. Extracted oils and their NEs were applied separately to HepG2 cell line to construct a comparison and MTT assay was used for this purpose. Prepared NEs were found more effective against cancer cell line as compared to their respective oils. MTT assay showed efficacy of NEs in reducing cell viability with IC50 value of 10 µl (flax seed oil), 25 µl (clove oil NE) and 1 µl (olive oil NE), and was safe to normal cells. The results of the current study revealed that NEs prepared from flax seed, clove and olive oil have the potential for further development as anticancer agents.

ANTIOXIDANT AND ANTI-CANCER ACTVITY OF STANDARDIZED EXTRACTS OF THREE VARIETIES OF Ficus deltoidea’s LEAVES

2015 ◽  
Vol 77 (3) ◽  
Author(s):  
Husnul Hanani Soib ◽  
Ismail Ware ◽  
Harisun Yaakob ◽  
Hanafi Mukrish ◽  
Mohamad Roji Sarmidi
Keyword(s):  
Prostate Cancer ◽  
Cell Line ◽  
Antioxidant Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Cancer Cell Line ◽  
Prostate Cancer Cell Line ◽  
Total Phenolic ◽  
Ic50 Value ◽  
Anti Cancer

The present study was designed to evaluate the antioxidant and anti-cancer activities of aqueous extracts of three varieties of Ficus deltoidea (var. angustifolia, var. deltoidea, var. kunstleri) on prostate cancer DU145 cell line. The results showed that, F. deltoidea var. kunstleri contained the highest total phenolic (44.7 ± 0.022 mg GAE/10 g sample) and flavonoid contents (23.1 ± 0.005 mg CE/10 g sample) as well as the highest radical scavenging activity (IC50 0.039 mg/mL) followed by F. deltoidea var. deltoidea and F. deltoidea var. angustifolia. Similarly, based on anti-cancer activities, F. deltoidea var. kunstleri demonstrated the lowest IC50 value (93.11 mg/mL) followed by F. deltoidea var. deltoidea (204.17 mg/mL) and F. deltoidea var. angustifolia (429.54 mg/mL). Other than that, vitexin which is a bioactive marker was appeared to be the highest in F. deltoidea var. kunstleri compared to others. Hence, the results suggested that there might be an association between antioxidant activities and bioactive markers against prostate cancer cell line (DU145).

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.

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