scholarly journals Synthesis of Amino Acid Schiff Base Nickel (II) Complexes as Potential Anticancer Drugs In Vitro

2020 ◽  
Vol 2020 ◽  
pp. 1-15
Author(s):  
Yang Li ◽  
Jianfang Dong ◽  
Peiran Zhao ◽  
Ping Hu ◽  
Dawei Yang ◽  
...  
Keyword(s):  
Schiff Base ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Dependent Manner ◽  
X Ray Crystallography ◽  
M Phase ◽  
Ic50 Values ◽  
Esophageal Cancer Cell ◽  
Esophageal Cancer Cell Line

Three hexacoordinated octahedral nickel (II) complexes, [Ni (Trp-sal) (phen) (CH3OH)] (1), [Ni (Trp-o-van) (phen) (CH3OH)]•2CH3OH (2), and [Ni (Trp-naph) (phen) (CH3OH)] (3) (where Trp-sal = Schiff base derived from tryptophan and salicylaldehyde, Trp-o-van = Schiff base derived from tryptophan and o-vanillin, Trp-naph = Schiff base derived from tryptophan and 2-hydroxy-1-naphthaldehyde, phen = 1, 10-phenanthroline), have been synthesized and characterized as potential anticancer agents. Details of structural study of these complexes using single-crystal X-ray crystallography showed that distorted octahedral environment around nickel (II) ion has been satisfied by three nitrogen atoms and three oxygen atoms. All these complexes displayed moderate cytotoxicity toward esophageal cancer cell line Eca-109 with the IC50 values of 23.95 ± 2.54 μM for 1, 18.14 ± 2.39 μM for 2, and 21.89 ± 3.19 μM for 3. Antitumor mechanism studies showed that complex 2 can increase the autophagy, reactive oxygen species (ROS) levels, and decrease the mitochondrial membrane potential remarkably in a dose-dependent manner in the Eca-109 cells. Complex 2 can cause cell cycle arrest in the G2/M phase. Additionally, complex 2 can regulate the Bcl-2 family and autophagy-related proteins.

scholarly journals Synthesis and Evaluation of Triazolyl Dihydropyrimidines as Potential Anticancer Agents

2018 ◽  
Vol 10 (4) ◽  
pp. 18
Author(s):  
Rajanna Ajumeera ◽  
Ganapathi Thipparapu ◽  
Shireesha Boyapati ◽  
Bharath Singh Padya ◽  
Vijayalaxmi Venkatesan
Keyword(s):  
Anticancer Agents ◽  
Human Breast Cancer Cell ◽  
S Phase ◽  
Human Breast ◽  
Standard Drug ◽  
M Phase ◽  
Ic50 Values ◽  
Derivatives Of ◽  
Mcf 7

Novel N – triazolyl 3(a-f) and O-triazolyl (4a-f) derivatives of 4, 6-diaryl-1, 4-dihydropyrimidines were synthesized through mannich reaction. All compounds were characterized by physical and spectral data. These compounds were screened for in vitro efficiency in human breast cancer cell (MCF-7&MDA-MB-231) lines and found to have very good anti-proliferative activity.  Among all compounds of 4b, 3e, 4e endowed with lesser respective IC50 values of 31.94, 55.73, 55.03 µM in MCF-7 cells and 41.50, 35.28, 32.06 µM in MDA-MB 231 cells by MTT assay. In further studies, Compounds 4b, 3e, 4e were found to arrest cell growth at S phase in MCF-7 cells. In MDA-MB 231 cells, 4b, 4e were found to arrest the cells in S phase, and compound 3e found to arrest G2/M phase when compared to the standard drug tamoxifen, arrested S phase in MCF-7 cells and G0/G1 phase in MDA-MB 231 cells.

Two New Oxovanadium(IV) Compounds Containing Amino Acid Schiff Base and 1,10-Bathophenanthroline Ligands: Syntheses, Crystal Structures, and In Vitro Evaluation of the Anticancer Activities

2017 ◽  
Vol 70 (5) ◽  
pp. 608 ◽  
Author(s):  
Yaping Cao ◽  
Hongmei Liu ◽  
Zeli Yuan ◽  
Gang Wei
Keyword(s):  
Schiff Base ◽  
Anticancer Agents ◽  
High Resolution Mass Spectrometry ◽  
Hepatoma Cell ◽  
A549 Cells ◽  
Molar Conductance ◽  
Anticancer Activities ◽  
Human Hepatoma Cell ◽  
Ic50 Values

Two new oxovanadium(iv) compounds containing 1,10-bathophenanthroline (Bphen) and amino Schiff base derivatives [VO(hnd-napha)(Bphen)] (1) and [VO(o-van-met)(Bphen)] (2) were synthesised (where hnd-napha and o-van-met are N-Schiff bases derived from the reaction of 2-hydroxy-1-naphthaldehyde with 3-(1-naphthyl)-l-alanine and o-vanillin with l-methionine, respectively). These compounds were characterised by elemental analysis, infrared spectroscopy, high-resolution mass spectrometry, and single-crystal X-ray diffraction (XRD). Both compounds showed low molar conductance values, indicating that they are non-electrolytes. The XRD results showed that the VIV atoms in both compounds existed in the VO3N3 coordination geometry with Schiff base and Bphen ligands. The in vitro anticancer activities of compounds 1 and 2 were evaluated against A549 human lung carcinoma and HepG2 human hepatoma cell lines using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and the results revealed that both compounds were cytotoxic with half maximal inhibitory concentration (IC50) values in the range of 8.22 ± 1.0 to 94.89 ± 3.2 μmol L−1. Notably, compound 2 exhibited much better anticancer activity in vitro against A549 cells (8.22 ± 1 μmol L−1) than [VO(acac)2] (24 ± 6 μmol L−1) or any of our previously reported oxovanadium(iv) compounds, making it comparable in activity to cisplatin (3.1 ± 0.5 μmol L−1). These results therefore suggest that compound 2 could be used as a promising lead for the development of anticancer agents for the treatment of lung cancer.

scholarly journals Anticancer Effects of Five Biflavonoids from Ginkgo Biloba L. Male Flowers In Vitro

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1496 ◽  
Author(s):  
Li ◽  
Li ◽  
Xia ◽  
Tian ◽  
Zhang ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Hela Cells ◽  
Ginkgo Biloba ◽  
Morphological Changes ◽  
Dependent Manner ◽  
Anticancer Effects ◽  
Proapoptotic Protein ◽  
M Phase ◽  
Male Flowers

Ginkgo biloba L., an ancient dioecious gymnosperm, is now cultivated worldwide for landscaping and medical purposes. A novel biflavonoid—amentoflavone 7''-O-β-D-glucopyranoside (1)—and four known biflavonoids were isolated and identified from the male flowers of Ginkgo. The anti-proliferative activities of five biflavonoids were evaluated on different cancer lines. Bilobetin (3) and isoginkgetin (4) exhibited better anti-proliferative activities on different cancer lines. Their effects were found to be cell-specific and in a dose and time dependent manner for the most sensitive HeLa cells. The significant morphological changes validated their anticancer effects in a dose-dependent manner. They were capable of arresting the G2/M phase of the cell cycle, inducing the apoptosis of HeLa cells dose-dependently and activating the proapoptotic protein Bax and the executor caspase-3. Bilobetin (3) could also inhibit the antiapoptotic protein Bcl-2. These might be the mechanism underlying their anti-proliferation. In short, bilobetin (3) and isoginkgetin (4) might be the early lead compounds for new anticancer agents.

scholarly journals Synthesis and in vitro PDT evaluation of red emission polymer dots (R-CPDs) and pyropheophorbide-α conjugates

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Faiza Sajjad ◽  
Yi-Jia Yan ◽  
Davor Margetić ◽  
Zhi-Long Chen
Keyword(s):  
Cancer Cell Line ◽  
Ros Generation ◽  
One Pot ◽  
Red Emission ◽  
Vis Spectroscopy ◽  
Polymer Dots ◽  
Esophageal Cancer Cell ◽  
Esophageal Cancer Cell Line ◽  
Carbon Based

AbstractCarbon based polymer dots have piqued attention of researchers because of excellent biocompatibility, and good solubility. Most of the p-dots are able to generate ROS which is effective for photodynamic therapy for the treatment of cancer while some photosensitizers such as porphyrins possess some drawbacks such as hydrophobicity, and dark toxicity. Therefore in this study we conjugated red emission carbon based polymer with pyropheophorbide-α through amide condensation and π–π stacking. One pot synthesis of the conjugate was successfully achieved. Their photophysiological properties were studied and structures were characterized by FT-IR, TEM and 1HNMR. pH- sensitivity of the conjugates was confirmed using fluorescence and UV–vis spectroscopy. Photo toxicity and dark toxicity of the prepared conjugates were evaluated in human esophageal cancer cell line (Eca-109). Hemocompatibility of the synthesized conjugates was evaluated and proved that the conjugates are safe to use for the treatment of tumor. Our results showed the PS doped p-dots had less dark toxicity and increased light toxicity as well as ROS generation was high as compared to precursor drug. Therefore, incorporation of p-dots to porphyrin improved biocompatibility and enhanced the photodynamic effect.

scholarly journals Diverse Polyphenols from Hypericum faberi

2019 ◽  
Vol 9 (3) ◽  
pp. 215-221 ◽  
Author(s):  
Xin-Wen Zhang ◽  
Yan-Song Ye ◽  
Fan Xia ◽  
Xing-Wei Yang ◽  
Gang Xu
Keyword(s):  
Cell Line ◽  
Pancreatic Tumor ◽  
Cancer Cell Line ◽  
Tumor Cell Line ◽  
Detailed Comparison ◽  
Esophageal Cancer Cell ◽  
Esophageal Cancer Cell Line ◽  
Human Esophageal Cancer ◽  
Whole Plants

Abstract Six new polyphenols with different isoprenylated xanthones, isoprenylated acylphloroglucinols, and chromone architectures, hyperfaberols A–F (1–6), were isolated from the whole plants of Hypericum faberi along with seven other related known compounds. In which hyperfaberols A/B (1/2) and 12–13 were isoprenylated xanthones, hyperfaberols C–E (3–5) and 8–11 were seven isoprenylated acylphloroglucinol derivatives, while 6–7 were two chromones. Their structures were elucidated by comprehensive analysis of their spectroscopic data as well as detailed comparison with the literature data. Compounds 1 and 11 showed cytotoxities against the human esophageal cancer cell line (ECA-109) and the pancreatic tumor cell line (PANC-1) in vitro, respectively. Graphical Abstract

Synthesis and in vitro evaluation of substituted quinolines as new apoptosis inducers and anticancer agents: Pharmacophore-based design

2021 ◽  
Vol 18 ◽  
Author(s):  
Hiren Dayani ◽  
Abhishek Jha ◽  
Manjunath Ghate ◽  
Vivek K. Vyas
Keyword(s):  
Anticancer Agents ◽  
Caspase 3 ◽  
Cancer Cell Line ◽  
Pharmacophore Modeling ◽  
Design Synthesis ◽  
Substituted Quinolines ◽  
Activation Assay ◽  
Ic50 Values ◽  
Ft Ir

Background: Cancer is a global health burden and the leading cause of death across the world after cardiovascular disease. Objective: The objective of this work was the design, synthesis, and pharmacological evaluation of 2-phenylquinolin-4-amine derivatives as apoptosis inducers and anticancer agents. Method: In this study, we performed ligand-based pharmacophore modeling as a promising design strategy for the design of substituted quinoline derivatives as apoptosis inducers and anticancer agents. The designed compounds were synthesized as 2-phenylquinolin-4-amine derivatives and characterized by FT-IR, 1H-NMR, 13C-NMR, and Mass spectroscopy. Synthesized compounds were screened for apoptosis-inducing activity using caspase-3 activation and annexine-FITC assays and also screened against cancer cell line (HT-29) in an antiproliferative assay. Results: Synthesized compounds 7a and 7d demonstrated EC50 values of 6.06 and 6.69 µM in caspase-3 activation assay, respectively, and also showed late stage induction of apoptosis in annexine assay. Synthesized compounds 7a, 7d and 7i, also exhibited good antiproliferative activity with IC50 values of 8.12, 9.19, and 11.34 µM, respectively, which revealed that these are promising apoptosis inducers for the further development of new anticancer agents.

The Photodynamic Anti-Tumor Effects of New PPa-CDs Conjugate with pH Sensitivity and Improved Biocompatibility

2021 ◽  
Vol 21 ◽  
Author(s):  
Faiza Sajjada ◽  
Xu-Ying Liua ◽  
Yi-Jia Yanb ◽  
Xing-Ping Zhoua ◽  
Zhi-Long Chena
Keyword(s):  
Emission Spectra ◽  
Cancer Cell Line ◽  
In Vitro Cytotoxicity ◽  
Ph Sensitivity ◽  
Covalent Interaction ◽  
Esophageal Cancer Cell ◽  
Esophageal Cancer Cell Line ◽  
Good Biocompatibility ◽  
Human Esophageal Cancer

Background: Photodynamic therapy has been increasingly used to cope with the alarming problem of cancer. Porphyrins and its derivatives are widely used as potent photosensitizers (PS) for PDT. However, hydrophobicity of porphyrins poses a challenge for their use in clinics, while most of the carbon dots (CDs) are known for good biocompatibility, solubility, and pH sensitivity. Objective: To improve the properties/biocompatibility of the pyropheophorbide-α for PDT. Methods: Methods: PPa-CD conjugate was synthesized through covalent interaction using amide condensation. The structure of synthesized conjugate was confirmed by TEM, 1HNMR, and FTIR. The absorption and emission spectra were studied. In vitro, cytotoxicity of the conjugate was examined in the Human esophageal cancer cell line (Eca-109). Results: The results showed that the fluorescence of the drug was increased from its precursor. CD based conjugate could generate ROS as well as enhanced the biocompatibility by decreasing the cytotoxicity. The conjugated drug also showed pH sensitivity in different solutions. Conclusion: The dark toxicity, as well as hemocompatibility, were improved.

Chickpea (Cicer arietinum L.) Lectin Exhibit Inhibition of ACE-I, α-amylase and α-glucosidase Activity

2019 ◽  
Vol 26 (7) ◽  
pp. 494-501 ◽  
Author(s):  
Sameer Suresh Bhagyawant ◽  
Dakshita Tanaji Narvekar ◽  
Neha Gupta ◽  
Amita Bhadkaria ◽  
Ajay Kumar Gautam ◽  
...  
Keyword(s):  
Biological Effects ◽  
Exchange Chromatography ◽  
Health Concern ◽  
Carbohydrate Binding ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Ic50 Values ◽  
Chickpea Lectin

Background: Diabetes and hypertension are the major health concern and alleged to be of epidemic proportions. This has made it a numero uno subject at various levels of investigation. Glucosidase inhibitor provides the reasonable option in treatment of Diabetes Mellitus (DM) as it specifically targets post prandial hyperglycemia. The Angiotensin Converting Enzyme (ACE) plays an important role in hypertension. Therefore, inhibition of ACE in treatment of elevated blood pressure attracts special interest of the scientific community. Chickpea is a food legume and seeds contain carbohydrate binding protein- a lectin. Some of the biological properties of this lectin hitherto been elucidated. Methods: Purified by ion exchange chromatography, chickpea lectin was tested for its in vitro antioxidant, ACE-I inhibitory and anti-diabetic characteristic. Results: Lectin shows a characteristic improvement over the synthetic drugs like acarbose (oral anti-diabetic drug) and captopril (standard antihypertensive drug) when, their IC50 values are compared. Lectin significantly inhibited α-glucosidase and α-amylase in a concentration dependent manner with IC50 values of 85.41 ± 1.21 ҝg/ml and 65.05 ± 1.2 µg/ml compared to acarbose having IC50 70.20 ± 0.47 value of µg/ml and 50.52 ± 1.01 µg/ml respectively. β-Carotene bleaching assay showed antioxidant activity of lectin (72.3%) to be as active as Butylated Hydroxylanisole (BHA). In addition, lectin demonstrated inhibition against ACE-I with IC50 value of 57.43 ± 1.20 µg/ml compared to captopril. Conclusion: Lectin demonstrated its antioxidant character, ACE-I inhibition and significantly inhibitory for α-glucosidase and α-amylase seems to qualify as an anti-hyperglycemic therapeutic molecule. The biological effects of chickpea lectin display potential for reducing the parameters of medically debilitating conditions. These characteristics however needs to be established under in vivo systems too viz. animals through to humans.

scholarly journals Knigth's Move in the Periodic Table, From Copper to Platinum, Novel Antitumor Mixed Chelate Copper Compounds, Casiopeinas, Evaluated by an in Vitro Human and Murine Cancer Cell Line Panel

2001 ◽  
Vol 8 (1) ◽  
pp. 19-28 ◽  
Author(s):  
Isabel Gracia-Mora ◽  
Lena Ruiz-Ramírez ◽  
Celedonio Gómez-Ruiz ◽  
Mabel Tinoco-Méndez ◽  
Adriana Márquez-Quiñones ◽  
...  
Keyword(s):  
Cancer Cell ◽  
Anticancer Agents ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Drug Candidates ◽  
Control Drug ◽  
Copper Compounds ◽  
Structure Activity ◽  
Cell Line Panel

We synthesized a novel anticancer agents based on mixed chelate copper (II) complexes, named Casiopeínas® has of general formula [Cu(N-N)(N-O)H2O]NO3 (where, N-N = diimines as 1,10- phenanthroline, 2,2-bipyridine, or substituted and N-O=aminoeidate or [Cu(N-N)(O-O)H2O]NO3 (where NN= diimines as 10-phenanthroline, 2,2-bipyridine or substituted Casiopeínas I, II, IV, V, VI, VII VIII and O-O=acetylacetonate, salicylaldehidate Casiopínas III). We evaluated the in vitro antitumor activity using a human cancer cell panel and some nurine cancer cells. Eleven Casiopeinas are evaluated in order to acquire some structure-activity correlations and some monodentated Casiopeinäs analogues; cisplatinum was used as control drug. The 50% growth inhibition observed is, in all cases reach with concentrations of Casiopeina's 10 or 100 times lower than cisplatinum. In a previous work we reported the induction of apoptosis by Casiopeina II. The results indicate that Casiopeinass are a promising new anticancer drug candidates to be developed further toward clinical trials.

scholarly journals NBM-HD-1: A Novel Histone Deacetylase Inhibitor with Anticancer Activity

2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Wei-Jan Huang ◽  
Yu-Chih Liang ◽  
Shuang-En Chuang ◽  
Li-Ling Chi ◽  
Chi-Yun Lee ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Xenograft Model ◽  
Cyclin B1 ◽  
Dependent Manner ◽  
Cell Cycle Regulators ◽  
Anticancer Activities ◽  
Gene Expressions

HDAC inhibitors (HDACis) have been developed as promising anticancer agents in recent years. In this study, we synthesized and characterized a novel HDACi, termed NBM-HD-1. This agent was derived from the semisynthesis of propolin G, isolated from Taiwanese green propolis (TGP), and was shown to be a potent suppressor of tumor cell growth in human breast cancer cells (MCF-7 and MDA-MB-231) and rat glioma cells (C6), with an IC50ranging from 8.5 to 10.3 μM. Western blot demonstrated that levels of p21(Waf1/Cip1), gelsolin, Ac-histone 4, and Ac-tubulin markedly increased after treatment of cancer cells with NBM-HD-1. After NBM-HD-1 treatment for 1–4 h, p-PTEN and p-AKT levels were markedly decreased. Furthermore, we also found the anticancer activities of NBM-HD-1 in regulating cell cycle regulators. Treatment with NBM-HD-1,p21(Waf1/Cip1)gene expression had markedly increased whilecyclin B1andD1gene expressions had markedly decreased. On the other hand, we found that NBM-HD-1 increased the expressions of tumor-suppressor genep53in a dose-dependent manner. Finally, we showed that NBM-HD-1 exhibited potent antitumor activity in a xenograft model. In conclusion, this study demonstrated that this compound, NBM-HD-1, is a novel and potent HDACi with anticancer activityin vitroandin vivo.

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