A Venomics Approach to Identify and Characterize Biocactive Peptides (BAP) with Anti-Cancer Activity against Colorectal Cancer Cells from Animal Venoms (Preprint)

2021 ◽  
Author(s):  
Syeda Kiran Shahzadi ◽  
Noushad Karuvantevida ◽  
Yajnavalka Banerjee
Keyword(s):  
Colorectal Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Control Cell ◽  
Treatment Modalities ◽  
Health Issues ◽  
Anti Cancer ◽  
Pharmacologically Active ◽  
Animal Venoms ◽  
Cancer Activity

BACKGROUND Cancer is the third leading cause of death in the United Arab Emirates (UAE) after cardiovascular diseases and accidents. In UAE, colorectal cancer (CRC) is the first and fourth most common cancer in males and females respectively. Several treatment modalities have been employed for cancer treatment such as surgery, radiotherapy, chemotherapy, hormone replacement therapy, and immunotherapy. These treatment modalities often elicit adverse effects on normal cells, causing toxic side effects. To circumvent these toxicities, there has been an increased impetus towards the identification of alternate treatment strategies. Animal venoms are veritable gold mines of pharmacologically active polypeptides and proteins. OBJECTIVE In this proof-of-concept study, we avail a high throughput “Venomics” strategy to identify and characterize anticancer bioactive peptides (BAP) from 20 different animal venoms specifically targeting CRC. We chose to focus on CRC as it is one of the foremost health issues in the UAE. METHODS In initial study, we will screen 2500 different peptides derived from 20 different animal venoms for anticancer activity specifically directed against three CRC cell lines and two control cell lines employing the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) colorimetric assay for cytotoxicity. Three venoms of the 20, which exhibited specific and potent anticancer activity directed against the three CRC cell lines will be selected; and from these three venoms the specific peptide(s) with anti-CRC activity will be isolated and characterized. RESULTS This study is at the protocol development stage only, and as such, no results are available. CONCLUSIONS In summary, the proposed study will not only generate therapeutic leads to manage/treat one of the leading health issues in the UAE i.e., CRC, but is also of commercial interest as the identified BAP with specific anti-cancer activity against CRC can be patented for commercialization.

Synthesis and Anticancer Activity of 9-O-Pyrazole Alkyl Substituted Berberine Derivatives

2019 ◽  
Vol 18 (11) ◽  
pp. 1639-1648 ◽  
Author(s):  
Daipeng Xiao ◽  
Fen He ◽  
Dongming Peng ◽  
Min Zou ◽  
Junying Peng ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Molecular Docking ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Human Lung Cancer ◽  
Drug Candidate ◽  
Molecular Docking Study ◽  
Protective Function ◽  
Anti Cancer ◽  
Cancer Activity

Background: Berberine (BBR), an isoquinoline plant alkaloid isolated from plants such as Coptis chinensis and Hydrastis canadensis, own multiple pharmacological activities. Objective: In this study, seven BBR derivatives were synthesized and their anticancer activity against HeLa cervical and A549 human lung cancer cell lines were evaluated in vitro. Methods: The anti-cancer activity was measured by MTT assay, and apoptosis was demonstrated by the annexin V-FITC/PI staining assay. The intracellular oxidative stress was investigated through DCFH-DA assay. The molecular docking study was carried out in molecular operating environment (MOE). Results: Compound B3 and B5 showed enhanced anti-cancer activity compared with BBR, the IC50 for compound B3 and B5 were significantly lower than BBR, and compound B3 at the concentration of 64 or 128 µM induced apoptosis in HeLa and A549 cell lines. The reactive oxygen species (ROS) was generated in both cell lines when treated with 100 µM of all the compounds, and compound B3 and B5 induced higher activity in the generation of ROS, while compound B3 exhibited the highest activity, these results are in accordance with the cytotoxicity results, indicating the cytotoxicity were mostly generated from the oxidative stress. In addition, molecular docking analysis showed that compound B3 had the greatest affinity with Hsp90. Upon binding, the protective function of Hsp90 was lost, which might explain its higher cytotoxicity from molecular interaction aspect. Conclusion: All the results demonstrated that compound B3 and B5 showed significantly higher anti-cancer ability than BBR, and compound B3 is a promising anticancer drug candidate.

scholarly journals Liposomes Loaded with the Proteasome Inhibitor Z-Leucinyl-Leucinyl-Norleucinal Are Effective in Inducing Apoptosis in Colorectal Cancer Cell Lines

Membranes ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 91
Author(s):  
Katia Cortese ◽  
Silvia Marconi ◽  
Cinzia Aiello ◽  
Maria Cristina Gagliani ◽  
Serena Pilato ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Cell Lines ◽  
Egf Receptor ◽  
Acquired Resistance ◽  
Surface Expression ◽  
Developed Countries ◽  
Cell Surface Expression ◽  
Gamma Secretase ◽  
Anti Cancer ◽  
Cancer Activity

Colorectal cancer (CRC) is one of the main causes of cancer-related death in developed countries. Targeted therapies and conventional chemotherapeutics have been developed to help treat this type of aggressive cancer. Among these, the monoclonal antibodies cetuximab (Cxm) and panitumumab specifically target and inactivate the signaling of ERBB1 (EGF receptor), a key player in the development and progression of this cancer. Unfortunately, these antibodies are effective only on a small fraction of patients due to primary or secondary/acquired resistance. However, as ERBB1 cell surface expression is often maintained in resistant tumors, ERBB1 can be exploited as a target to deliver other drugs. Liposomes and immunoliposomes are under intensive investigation as pharmaceutical nanocarriers and can be functionalized with specific antibodies. In this study, we first investigated the anti-cancer activity of a cell permeable tripeptide, leucine-leucin-norleucinal (LLNle), an inhibitor of gamma-secretase and proteasome, in three different CRC cell lines that express ERBB1. We formulated LLNle-liposomes and Cxm-conjugated LLNle-loaded liposomes (LLNle-immunoliposomes) and evaluated their efficacy in inhibiting cell survival. Despite similar pro-apoptotic effects of free LLNle and LLNle-liposomes, immunoliposomes-LLNle were significantly less effective than their unconjugated counterparts. Indeed, immunoliposomes-LLNle were readily internalized and trafficked to lysosomes, where LLNle was likely trapped and/or inactivated. In conclusion, we demonstrated that LLNle was readily delivered to CRC cell lines by liposomes, but immunoliposomes-LLNle failed to show significant anti-cancer activity.

Phyto-Facilitated Bimetallic ZnFe2O4 Nanoparticles via Boswellia carteri: Synthesis, Characterization and Anti-Cancer Activity.

2020 ◽  
Vol 21 ◽  
Author(s):  
Amer Imraish ◽  
Afnan Al-Hunaiti ◽  
Tuqa Abu-Thiab ◽  
Abed Al-Qader Ibrahim ◽  
Eman Hwaitat ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Metallic Nanoparticles ◽  
Bimetallic Nanoparticles ◽  
Iron Chloride ◽  
Nano Particles ◽  
Adverse Side Effect ◽  
Wide Range ◽  
Anti Cancer ◽  
Znfe2o4 Nanoparticles

Background: The growing unsatisfaction toward the available traditional chemotherapeutic agents enhanced the need to develop new methods for obtaining materials with more effective and safe anti-cancer properties. Over the past few years, usage of metallic nanoparticles has been a target for researchers of different scientific and commercial fields due to their tiny sizes, environment friendly properties and wide range applications. To overcome the obstacles of traditional physical and chemical methods for synthesis of such nanoparticles, a new less expensive and eco-friendly method has been adopted using natural existing organisms as a reducing agent to mediate synthesis of the desired metallic nanoparticles from their precursors, a process called green biosynthesis of nanoparticles. Objective: Here in the present study, zinc iron bimetallic nanoparticles (ZnFe2O4) were synthesized via an aqueous extract of Boswellia Carteri resin mixed with zinc acetate and iron chloride precursors, and they were tested for their anticancer activity. Methods: Various analytic methods were applied for the characterization of the Phyto synthesized ZnFe2O4 and they were tested for their anticancer activity against MDA-MB-231, K562, MCF-7 cancer cell lines and normal fibroblasts. Results: Our results demonstrate the synthesis of cubic structured bimetallic nanoparticles ZnFe2O4 with an average diameter 10.54 nm. MTT cytotoxicity assay demonstrate that our phyto-synthesized ZnFe2O4 nanoparticles exhibited a selective and potent anticancer activity against K562 and MDA-MB-231 cell lines with IC50 values 4.53 µM and 4.19 µM, respectively. Conclusion: In conclusion, our bio synthesized ZnFe2O4 nano particles show a promising environmentally friendly of low coast chemotherapeutic approach against selective cancers with a predicted low adverse side effect toward normal cells. Further in vivo advanced animal research should be done to execute their applicability in living organisms.

SYNTHESIS AND ANTICANCER ACTIVITY EVALUATION OF SOME SCHIFF BASES OF 1, 3, 4-OXADIAZOLE

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (03) ◽  
pp. 12-17
Author(s):  
Manpreet Kaur ◽  
S. Singh ◽  
Keyword(s):  
Schiff Base ◽  
Growth Inhibition ◽  
Anticancer Activity ◽  
Maximum Growth ◽  
Schiff Base Derivatives ◽  
Control Growth ◽  
Anti Cancer ◽  
Oxadiazole Derivatives ◽  
Cancer Activity ◽  
Mcf 7

A new series of 2,5-disubstituted-1,3,4-oxadiazole derivatives has been synthesized with the help of different aromatic benzaldehydes and final compounds were characterized by FTIR and 1H NMR. 2,5- disubstituted-1,3,4-oxadiazole derivatives were synthesized by the reaction of Schiff base derivatives with 2,5-disubstituted-1,3,4-oxadiazoles. All the synthesized compounds were screened for their anticancer activity. These compounds were evaluated for their anticancer activity against various cancer cell lines. Five of the compounds possessed good to moderate anti-cancer activity. Three of the synthesized compounds i.e. 6a, 6f and 6g were found to possess maximum growth inhibition. The order for the % control growth inhibition of MCF-7 was found to be 6a>6f>6g>5b>6h, as shown in Table II-VI.

One Pot Synthesis, Quantum Chemical Stimulation and Anticancer Evaluation of Some New 8-Azacoumarin Derivatives

2021 ◽  
Author(s):  
Sameh Rizk ◽  
Mohamed Megahed ◽  
Monda Badawy ◽  
Mohamed Aly
Keyword(s):  
Liver Cancer ◽  
Cell Lines ◽  
Analytical Data ◽  
Liver Carcinoma ◽  
One Pot ◽  
Reference Drug ◽  
One Pot Synthesis ◽  
Ic50 Value ◽  
Anti Cancer ◽  
Cancer Activity

Abstract New anticancer agents are highly needed to overcome cancer cell resistance. Synthesis of newly pyrazole, derivatives via heterocyclic ring opening of azacoumarin promoted with grinding and ultrasonic reaction conditions. Efficient solvent less one pot synthesis can be well progressed to afford the good yield of new heterocyclic products that were characterized by IR, 1H-NMR, MS and micro-analytical data. Anticancer evaluation for the synthesized compounds exhibited good cytotoxiciy. The anti-liver cancer activity of all compounds was screened in vitro against hepatocellular carcinoma (HCC) cell lines (HepG-2) by viability assay. The synthesized compounds were evaluated for their anticancer activity and found to exhibit promising activities. All new compounds were tested for possible anti-cancer activity against HepG-2 cell lines in comparison to the reference drug doxorubicin (DOX). Compound 8 was the most active against the liver carcinoma cell line (HepG-2) giving promising half-maximal inhibitory concentration (IC50) value of 27.5 ± 1.3 μg/mL, compared with DOX with IC50 value of 0.36 ± 0.02 μg/mL. However it has weak cytotoxic effects against normal rat hepatocytes with 50% cytotoxic concentration (CC50) = 1820.5 µg/ml (= > 500 µg/ml). Compound 8 was selected to be tested in combination with ionizing gamma radiation. Gene expression levels of the cell cycle inhibitor p21 and caspase-3 was quantified. As well as, Oxidative stress was quantified by measuring the concentration of malondialdehyde (MDA), and antioxidant activity of reduced gluthatione (GSH). This study concluded that the new derivative of the azacomarin compound has an effective anti-cancer effect and it was found that using the new compound with ionizing radiation at a dose of 8 Gy improves the effectiveness of the compound on liver cancer cells.

scholarly journals Theophylline exhibits anti-cancer activity via suppressing SRSF3 in cervical and breast cancer cell lines

Oncotarget ◽  
2017 ◽  
Vol 8 (60) ◽  
pp. 101461-101474 ◽  
Author(s):  
Yung-Lung Chang ◽  
Yu-Juei Hsu ◽  
Ying Chen ◽  
Yi-Wen Wang ◽  
Shih-Ming Huang
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Cancer Cell Lines ◽  
Breast Cancer Cell Lines ◽  
Anti Cancer ◽  
Cancer Activity

scholarly journals Promising Anticancer Activity of [Bis(1,8-quinolato)palladium (II)] Alone and in Combination

2020 ◽  
Author(s):  
Md. Nur Alam ◽  
Mohammad Moni ◽  
Jun Yu ◽  
Philip Beale ◽  
Peter Turner ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Anticancer Activity ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antitumour Activity ◽  
Epigallocatechin Gallate ◽  
Cancer Cell Line ◽  
Resistant Cell ◽  
Colorectal Cancer Cell Line

Abstract Due to similar coordination chemistry of palladium and platinum, a large number of palladium compounds too have been investigated for their anticancer activity. In the present study we describe synthesis, characterization and anticancer activity of palladium complex [Bis(1,8-quinolato)palladium (II)], coded as NH3 against seven different cancer cell lines. NH3 is found to have higher antitumour activity than cisplatin against both parent ovarian A2780 cell line and cisplatin-resistant cell lines. Also, NH3 has the lowest IC50 value against HT-29 colorectal cancer cell line. The higher antitumour activity of NH3 is due to the presence of bulky 8-hydroxy-quinoline ligand thus reducing its reactivity. Proteomic study has identified significantly expressed proteins which have been validated through bioinformatics. NH3 has been found to be less toxic than cisplatin at 2.5 mg/kg and 5 mg/kg dosages on mice models. Binary combinations of NH3 with curcumin and epigallocatechin gallate (EGCG) have demonstrated dose and sequence dependent synergism in ovarian and colorectal cancer models. All of the preclinical studies indicate promising therapeutic potentiality of NH3 [Bis(1,8-quinolato)palladium (II) ] as an anticancer drug.

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