Synthesis of Functional Building Blocks for Type III-B Rotaxane Dendrimer

Second-generation type III-B rotaxane dendrons, equipped with succinimide and acetylene functional groups, were synthesized successfully and characterized by NMR spectroscopy and mass spectrometry. A cell viability study of a dendron with a normal cell line of L929 fibroblast cells revealed no obvious cytotoxicity at a range of 5 to 100 μM. The nontoxic properties of the sophisticated rotaxane dendron building blocks provided a choice of bio-compatible macromolecular machines that could be potentially developed into polymeric materials.

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Cytotoxic Effect of Pseudomonas aurogenosa Protease on Cancer Cells

International Journal of Pharmaceutical Quality Assurance ◽

10.25258/ijpqa.10.3.7 ◽

2019 ◽

Vol 10 (03) ◽

Author(s):

Ghanyia J. Shanyoor ◽

Fatima R. Abdul ◽

Nehad A. Taher ◽

Ihsan A. Raheem

Keyword(s):

Cell Line ◽

Normal Cell ◽

Cytotoxic Effect ◽

Human Cancer ◽

Skim Milk ◽

Exchange Chromatography ◽

Protease Production ◽

Normal Cell Line ◽

Protease Enzyme ◽

Embryonic Fibroblast

About (20) Pseudomonas rogenosa isolate were experienced for their ability of protease production by calculating the diameter of lysis area after developing on skim milk agar medium (qualitatively ) and the results exhibited that only isolate no (5), was higher isolate for protease making of (26mm) of lysis area. Then, the protein concentration also identified by Bradford method and it was found of 0.16 mg/ ml , then purification was done by using an ion- exchange chromatography with DEAE sephadex G- 100 column and the results showed the presence of 1 peak of enzyme with 50 Kd of molecular weight 2 peaks of other proteins . we tried to investigate the invitro Cytotoxic effect of purified enzyme against two human cancer lines, HeP2 (Human larynx epidermed carcinoma ) , RD ( Rabdo- Sarcoma ) , and one normal cell line Ref ( Rat embryonic fibroblast ) . The cancer and normal cells were treated with different concentrations of protease enzyme ranging from ( 0.05, 0.1, 0.2, 0.4,0.8and 0.16 mg/ml) then incubated for additional 48h at 37C0 and the results showed highest toxicity ( 80.28%) of protease enzyme on RD , moderate cytotoxicity (45.52%) on Hep andslight toxicity ( 37.12% ) on normal cell line (Ref) in a concentration (0.8mg/ml).

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Mass Spectrometry Techniques: Principles and Practices for Quantitative Proteomics

Current Protein and Peptide Science ◽

10.2174/1389203721666200921153513 ◽

2020 ◽

Vol 21 ◽

Author(s):

Rocco J. Rotello ◽

Timothy D. Veenstra

Keyword(s):

Mass Spectrometry ◽

Quantitative Proteomics ◽

Protein Identification ◽

Dynamic Nature ◽

Complete Coverage ◽

The Past ◽

Proteome Level ◽

A Cell ◽

Quantitative Changes ◽

Made In

: In the current omics-age of research, major developments have been made in technologies that attempt to survey the entire repertoire of genes, transcripts, proteins, and metabolites present within a cell. While genomics has led to a dramatic increase in our understanding of such things as disease morphology and how organisms respond to medications, it is critical to obtain information at the proteome level since proteins carry out most of the functions within the cell. The primary tool for obtaining proteome-wide information on proteins within the cell is mass spectrometry (MS). While it has historically been associated with the protein identification, developments over the past couple of decades have made MS a robust technology for protein quantitation as well. Identifying quantitative changes in proteomes is complicated by its dynamic nature and the inability of any technique to guarantee complete coverage of every protein within a proteome sample. Fortunately, the combined development of sample preparation and MS methods have made it capable to quantitatively compare many thousands of proteins obtained from cells and organisms.

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Novel 1,2,3-Triazole-functionalized pyrido[3',2':4,5]furo[3,2-d]pyrimidin- 4(3H)-one Derivatives: Synthesis, Anticancer Activity, CoMFA and CoMSIA Studies

Letters in Organic Chemistry ◽

10.2174/1570178617666200319124017 ◽

2020 ◽

Vol 17 (12) ◽

pp. 969-978

Author(s):

Balakishan Vadla ◽

Sailu Betala

Keyword(s):

Anticancer Activity ◽

Cell Line ◽

Normal Cell ◽

Rational Design ◽

Human Cancer ◽

Strong Basis ◽

Hek 293 ◽

Normal Cell Line ◽

Human Cancer Cell Lines ◽

Mcf 7

A series of novel triazole functionalized pyrido [3',2':4,5] furo[3,2-d] pyrimidin-4 (3H)-one derivatives 7a-p were prepared from ethyl furo[2,3-b]pyridine-2-carboxylate 3 on reaction with ammonia to afford furo[2,3-b]pyridine-2-carboxamide 4. This compound, on reaction with triethyl orthoformate TEOF, gave compound 5. Compound 5 on propargylation, followed by a reaction with substituted aryl azides under Sharpless reaction conditions, furnished triazole tagged pyrido [3',2':4,5]furo[3,2-d] pyrimidin-4(3H)-one derivatives. All the products 7a-p were screened against four human cancer cell lines, such as HeLa - Cervical cancer (CCL-2), COLO 205- Colon cancer (CCL-222), HepG2- Liver cancer (HB-8065), and MCF7 - Breast cancer (HTB-22) and one normal cell line (HEK 293). Compounds 7b, 7n, 7o and 7p, which showed promising anticancer activity, were identified and found to be non-toxic to normal cell line. Studies for HeLa, COLO205, HepG2, and MCF-7 using CoMFA and CoMSIA were carried out . Models from 3D-QSAR provided a strong basis for future rational design of more active and selective HeLa, COLO205, HepG2, and MCF-7 cell line inhibitors.

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Design, Synthesis and In Vitro Anti-Cancer Evaluation of Novel Derivatives of 2-(2-Methyl-1,5-diaryl-1H-pyrrol-3-yl)-2-oxo-N-(pyridin-3- yl)acetamide

Medicinal Chemistry ◽

10.2174/1573406415666190425153717 ◽

2020 ◽

Vol 16 (3) ◽

pp. 340-349

Author(s):

Ebrahim S. Moghadam ◽

Farhad Saravani ◽

Ernest Hamel ◽

Zahra Shahsavari ◽

Mohsen Alipour ◽

...

Keyword(s):

Cell Cycle ◽

Peripheral Neuropathy ◽

Cell Line ◽

Normal Cell ◽

Caspase 3 ◽

Annexin V ◽

Normal Cell Line ◽

Anti Cancer ◽

Mcf 7

Objective: Several anti-tubulin agents were introduced for the cancer treatment so far. Despite successes in the treatment of cancer, these agents cause toxic side effects, including peripheral neuropathy. Comparing anti-tubulin agents, indibulin seemed to cause minimal peripheral neuropathy, but its poor aqueous solubility and other potential clinical problems have led to its remaining in a preclinical stage. Methods: Herein, indibulin analogues were synthesized and evaluated for their in vitro anti-cancer activity using MTT assay (on the MCF-7, T47-D, MDA-MB231 and NIH-3T3 cell lines), annexin V/PI staining assay, cell cycle analysis, anti-tubulin assay and caspase 3/7 activation assay. Results: One of the compounds, 4a, showed good anti-proliferative activity against MCF-7 cells (IC50: 7.5 μM) and low toxicity on a normal cell line (IC50 > 100 μM). All of the tested compounds showed lower cytotoxicity on normal cell line in comparison to reference compound, indibulin. In the annexin V/PI staining assay, induction of apoptosis in the MCF-7 cell line was observed. Cell cycle analysis illustrated an increasing proportion of cells in the sub-G-1 phase, consistent with an increasing proportion of apoptotic cells. No increase in G2/M cells was observed, consistent with the absence of anti-tubulin activity. A caspase 3/7 assay protocol showed that apoptosis induction by more potent compounds was due to activation of caspase 3. Conclusion: Newly synthesized compounds exerted acceptable anticancer activity and further investigation of current scaffold would be beneficial.

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Constraints in Adoption ofModern Farm Machines by Tribal Farmers in Ramgarh District of Jharkhand

Journal of AgriSearch ◽

10.21921/jas.v6i03.16216 ◽

2019 ◽

Vol 6 (03) ◽

Author(s):

PK SUNDARAM ◽

BIKASH SARKAR ◽

UJJWAL KUMAR ◽

AP ANURAG ◽

DK RAGHAV ◽

...

Keyword(s):

Cell Line ◽

Normal Cell ◽

Human Cancer ◽

Skim Milk ◽

Exchange Chromatography ◽

Protease Production ◽

Normal Cell Line ◽

Protease Enzyme ◽

Tribal Farmers ◽

Embryonic Fibroblast

About (20) Pseudomonas rogenosa isolate were experienced for their ability of protease production by calculating the diameter of lysis area after developing on skim milk agar medium (qualitatively ) andamp; the results exhibited that only isolate no (5), was higher isolate for protease making of (26mm) of lysis area. Then, the protein concentration also identified by Bradford method andamp; it was found of 0.16 mg/ ml , then purification was done by using an ion- exchange chromatography with DEAE sephadex G- 100 column andamp; the results showed the presence of 1 peak of enzyme with 50 Kd of molecular weight 2 peaks of other proteins . we tried to investigate the invitro Cytotoxic effect of purified enzyme against two human cancer lines, HeP2 (Human larynx epidermed carcinoma ) , RD ( Rabdo- Sarcoma ) , andamp; one normal cell line Ref ( Rat embryonic fibroblast ). The cancer andamp; normal cells were treated with different concentrations of protease enzyme ranging from ( 0.05, 0.1, 0.2, 0.4,0.8andamp; 0.16 mg/ml) then incubated for additional 48h at 37C 0 andamp; the results showed highest toxicity ( 80.28%) of protease enzyme on RD , moderate cytotoxicity (45.52%) on Hep andamp;slight toxicity ( 37.12% )on normal cell line (Ref) in a concentration (0.8mg/ml).

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Development of Tunable Silk Fibroin/Xanthan Biopolymeric Scaffold for Skin Tissue Engineering Using L929 Fibroblast Cells

Journal of Bionic Engineering ◽

10.1007/s42235-021-0004-4 ◽

2021 ◽

Vol 18 (1) ◽

pp. 103-117

Author(s):

Shailendra Singh Shera ◽

Rathindra Mohan Banik

Keyword(s):

Tissue Engineering ◽

Silk Fibroin ◽

Skin Tissue ◽

Fibroblast Cells ◽

Skin Tissue Engineering ◽

L929 Fibroblast

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Algae-meditated route to cuprous oxide (Cu2O) nanoparticle: differential expression profile of MALAT1 and GAS5 LncRNAs and cytotoxic effect in human breast cancer

Cancer Nanotechnology ◽

10.1186/s12645-020-00066-4 ◽

2020 ◽

Vol 11 (1) ◽

Author(s):

Parisa Taherzadeh-Soureshjani ◽

Mohammad Chehelgerdi

Keyword(s):

Breast Cancer ◽

Electron Microscopy ◽

Antimicrobial Activity ◽

Cell Line ◽

Cell Lines ◽

Normal Cell ◽

Pathogenic Bacteria ◽

Control Cell ◽

Normal Cell Line ◽

Control Cell Line

Abstract Background Breast cancer (BC), as the most widely recognized disease in women worldwide, represents about 30% of all cancers impacting women. This study was aimed to synthesize Cu2O nanoparticles from the cystoseira myrica algae (CM-Cu2O NPs) assess their antimicrobial activity against pathogenic bacteria and fungi. We evaluated the expression levels of lncRNAs (MALAT1 and GAS5) and apoptosis genes (p53, p27, bax, bcl2 and caspase3), their prognostic roles. Methods In this study, CM-Cu2O NPs synthesized by cystoseira myrica algae extraction used to evaluate its cytotoxicity and apoptotic properties on MDA-MB-231, SKBR3 and T-47D BC cell lines compared to HDF control cell line. The CM-Cu2O NPs was characterized by UV–Vis spectroscopy, Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), Transmission electron microscopy (TEM) and Scanning electron microscopy (SEM). The antimicrobial activity of CM-Cu2O NPs was assessed against pathogenic bacteria, staphylococcus aureus (S. aureus) PTCC 1112 bacteria as a standard gram-positive bacteria and pseudomonas aeruginosa (P. aeruginosa) PTCC 1310 as a standard gram-negative bacterium. Expression profile of MALAT1 and GAS5 lncRNAs and apoptosis genes, i.e., p27, bax, bcl2 and caspase3 genes, were calculated utilizing qRT-PCR. The changes in the expression levels were determined using the DDCT method. Results MALAT1 was upregulated in MDA-MB-231, SKBR3 and T-47D BC (p < 0.01), while GAS5 was downregulated in SKBR3 and T-47D cell lines tested compared with HDF control cell line (p < 0.05) was found. The results revealed that, p27, bax and caspase3 were significantly upregulated in BC cell lines as compared with normal cell line. Bcl2 expression was also significantly increased in MDA-MB-231 and T47D cell lines compared with normal cell line, but bcl2 levels were downregulated in SKBR3 cell line. Conclusions Our results confirm the beneficial cytotoxic effects of green-synthesized CM-Cu2O NPs on BC cell lines. This nanoparticle decreased angiogenesis and induces apoptosis, so we conclude that CM-Cu2O NPs can be used as a supplemental drug in cancer treatments. Significantly, elevated circulating lncRNAs were demonstrated to be BC specific and could differentiate BC cell lines from the normal cell lines. It was demonstrated that lncRNAs used in this study and their expression profiles can be created as biomarkers for early diagnosis and prognosis of BC. Further studies utilizing patients would give recognizable identification of lncRNAs as key players in intercellular interactions.

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Simple technique for the pyrolysis-mass spectrometry of polymeric materials

The Analyst ◽

10.1039/an9770200143 ◽

1977 ◽

Vol 102 (1211) ◽

pp. 143 ◽

Cited By ~ 14

Author(s):

J. C. Hughes ◽

B. B. Wheals ◽

M. J. Whitehouse

Keyword(s):

Mass Spectrometry ◽

Simple Technique ◽

Polymeric Materials ◽

Pyrolysis Mass Spectrometry

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Diminished LcrV Secretion Attenuates Yersinia pseudotuberculosis Virulence

Journal of Bacteriology ◽

10.1128/jb.00936-07 ◽

2007 ◽

Vol 189 (23) ◽

pp. 8417-8429 ◽

Cited By ~ 18

Author(s):

Jeanette E. Bröms ◽

Matthew S. Francis ◽

Åke Forsberg

Keyword(s):

Type Iii Secretion ◽

Yersinia Pseudotuberculosis ◽

Signal Sequence ◽

Infection Model ◽

Target Cells ◽

Cell Infection ◽

Host Cell Membrane ◽

Type Iii ◽

A Cell

ABSTRACT Many gram-negative bacterial pathogenicity factors that function beyond the outer membrane are secreted via a contact-dependent type III secretion system. Two types of substrates are predestined for this mode of secretion, namely, antihost effectors that are translocated directly into target cells and the translocators required for targeting of the effectors across the host cell membrane. N-terminal secretion signals are important for recognition of the protein cargo by the type III secretion machinery. Even though such signals are known for several effectors, a consensus signal sequence is not obvious. One of the translocators, LcrV, has been attributed other functions in addition to its role in translocation. These functions include regulation, presumably via interaction with LcrG inside bacteria, and immunomodulation via interaction with Toll-like receptor 2. Here we wanted to address the significance of the specific targeting of LcrV to the exterior for its function in regulation, effector targeting, and virulence. The results, highlighting key N-terminal amino acids important for LcrV secretion, allowed us to dissect the role of LcrV in regulation from that in effector targeting/virulence. While only low levels of exported LcrV were required for in vitro effector translocation, as deduced by a cell infection assay, fully functional export of LcrV was found to be a prerequisite for its role in virulence in the systemic murine infection model.

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