scholarly journals Piperine analogs arrest c-myc gene leading to downregulation of transcription for targeting cancer

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Nirali Pandya ◽  
Amit Kumar
Keyword(s):  
Isothermal Calorimetry ◽  
Fluorescence Emission ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Cellular Level ◽  
Lung Cancer Cell Line ◽  
Hek 293 ◽  
Anticancer Properties ◽  
G4 Dna ◽  
G Quadruplex

AbstractG-quadruplex (G4) structures are considered a promising therapeutic target in cancer. Since Ayurveda, Piperine has been known for its medicinal properties. Piperine shows anticancer properties by stabilizing the G4 motif present upstream of the c-myc gene. This gene belongs to a group of proto-oncogenes, and its aberrant transcription drives tumorigenesis. The transcriptional regulation of the c-myc gene is an interesting approach for anticancer drug design. The present study employed a chemical similarity approach to identify Piperine similar compounds and analyzed their interaction with cancer-associated G-quadruplex motifs. Among all Piperine analogs, PIP-2 exhibited strong selectivity, specificity, and affinity towards c-myc G4 DNA as elaborated through biophysical studies such as fluorescence emission, isothermal calorimetry, and circular dichroism. Moreover, our biophysical observations are supported by molecular dynamics analysis and cellular-based studies. Our study showed that PIP-2 showed higher toxicity against the A549 lung cancer cell line but lower toxicity towards normal HEK 293 cells, indicating increased efficacy of the drug at the cellular level. Biological evaluation assays such as TFP reporter assay, quantitative real-time PCR (qRT- PCR), and western blotting suggest that the Piperine analog-2 (PIP-2) stabilizes the G-quadruplex motif located at the promoter site of c-myc oncogene and downregulates its expression. In conclusion, Piperine analog PIP-2 may be used as anticancer therapeutics as it affects the c-myc oncogene expression via G-quadruplex mediated mechanism.

scholarly journals Co-Crystals of Resveratrol and Polydatin with L-Proline: Crystal Structures, Dissolution Properties, and In Vitro Cytotoxicities

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5722
Author(s):  
Yijie Lou ◽  
Kaxi Yu ◽  
Xiajun Wu ◽  
Zhaojun Wang ◽  
Yusheng Cui ◽  
...  
Keyword(s):  
Cell Line ◽  
Chemical Properties ◽  
Cancer Cell Line ◽  
Lung Cancer Cell Line ◽  
Hek 293 ◽  
Dissolution Properties ◽  
Diphenyltetrazolium Bromide ◽  
Water Ph ◽  
Physical And Chemical

Resveratrol (RSV) and polydatin (PD) have been widely used to treat several chronic diseases, such as atherosclerosis, pulmonary fibrosis, and diabetes, among several others. However, their low solubility hinders their further applications. In this work, we show that the solubility of PD can be boosted via its co-crystallization with L-proline (L-Pro). Two different phases of co-crystals, namely the RSV-L-Pro (RSV:L-Pro = 1:2) and PD-L-Pro (PD:L-Pro = 1: 3), have been prepared and characterized. As compared to the pristine RSV and PD, the solubility and dissolution rates of PD-L-Pro in water (pH 7.0) exhibited a 15.8% increase, whereas those of RSV-L-Pro exhibited a 13.8% decrease. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay of pristine RSV, PD, RSV-L-Pro, and PD-L-Pro against lung cancer cell line A549 and human embryonic kidney cell line HEK-293 indicated that both compounds showed obvious cytotoxicity against A549, but significantly reduced cytotoxicity against HEK-293, with PD/PD-L-Pro further exhibiting better biological safety than that of RSV/RSV-L-Pro. This work demonstrated that the readily available and biocompatible L-Pro can be a promising adjuvant to optimize the physical and chemical properties of RSV and PD to improve their pharmacokinetics.

Development and Biological Evaluation of Imidazothiazole propenones as Tubulin Inhibitors that Effectively Triggered Apoptotic Cell Death in Alveolar Lung Cancer Cell Line

2017 ◽  
Vol 2 (22) ◽  
pp. 6480-6487 ◽  
Author(s):  
Ibrahim Bin Sayeed ◽  
Koteswara Rao Garikapati ◽  
Venkata Krishna Kanth Makani ◽  
Apoorva Nagarajan ◽  
Mohd Adil Shareef ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cell Death ◽  
Cell Line ◽  
Cancer Cell ◽  
Apoptotic Cell ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Lung Cancer Cell Line ◽  
Lung Cancer Cell ◽  
Tubulin Inhibitors

Spectroscopic Studies on the Binding Properties of Ofloxacin and Human Telomeric G-Quadruplex DNA

2013 ◽  
Vol 634-638 ◽  
pp. 1062-1065 ◽  
Author(s):  
Xu Jian Luo ◽  
Qi Pin Qin ◽  
Yu Lan Li ◽  
Yan Yang
Keyword(s):  
Spectral Analysis ◽  
Fluorescence Emission ◽  
Spectroscopic Studies ◽  
Binding Properties ◽  
Quadruplex Dna ◽  
G4 Dna ◽  
G Quadruplex ◽  
Shoulder Peak ◽  
Binding Intensity ◽  
Dna Complex

The binding of ofloxacin with human telomeric G-quadruplex DNA, Htel-G4-DNA and Htel-3-G4-DNA were examined by Fluorescence and CD spectroscopic methods. In the Fluorescence emission spectral analysis, the addition of ofloxacin induced significant quenching on the fluorescence emission of TO-G4-DNA complex. The fluorescence spectral analysis indicated that ofloxacin exhibited higher binding affinity and binding intensity to Htel-G4-DNA than Htel-3-G4-DNA. In the CD spectral analysis, the interaction with ofloxacin did not disturb the characteristic absorption of Htel-G4-DNA at 290 nm corresponding to its antiparallel form, and only slightly increased the positive absorption at 270 nm as shoulder peak, which suggests the antiparallel structure of G-quadruplex can remain stable in the presence of ofloxacin

scholarly journals Bioactivity Profiling of Plant Biodiversity of Panama by High Throughput Screening

2019 ◽  
Vol 14 (1) ◽  
pp. 1934578X1901400 ◽  
Author(s):  
Anuradha Roy ◽  
Peter McDonald ◽  
Barbara N. Timmermann ◽  
Mahabir Gupta ◽  
Rathnam Chaguturu
Keyword(s):  
National Parks ◽  
High Throughput ◽  
High Throughput Screening ◽  
Cancer Cell Line ◽  
Antioxidant Response ◽  
Lung Cancer Cell Line ◽  
High Throughput Analysis ◽  
Anticancer Properties ◽  
Methanolic Extracts ◽  
Anti Inflammatory

We report relative bioactivities of extracts prepared from a large collection of plants from three national parks in Panama. Over 181 plants were collected, taxonomically identified and their detannified dichloromethane (DCM)-methanolic extracts were used for profiling selected bioactivities. Assays were performed to evaluate the antioxidant activity of the extracts for Antioxidant Response Element (ARE) induction, total non-enzymatic antioxidant potential, anti-inflammatory and anticancer properties. The high throughput analysis of 280 extracts resulted in identification of 57.5% of the extracts that could induce ARE at one or more concentrations tested, 93.5% that harbored total antioxidant capacity, and 2.1% of the extracts that showed lung cancer cell line-specific cytotoxicity. Data from our profiling experiments indicate that a large number of extracts could be a source for further isolation and chemical identification of compounds that could serve as leads for discovery of antioxidant, anticancer and anti-inflammatory agents to prevent or treat complex diseases like cancer and neurodegenerative disorders.

scholarly journals Analysis and Identification of Tumorigenic Targets of MicroRNA in Cancer Cells by Photoreactive Chemical Probes

2020 ◽  
Vol 21 (4) ◽  
pp. 1545
Author(s):  
Zhiyu Su ◽  
Tsogzolmaa Ganbold ◽  
Huricha Baigude
Keyword(s):  
Cancer Cells ◽  
Target Identification ◽  
Cancer Cell Line ◽  
Cellular Level ◽  
Lung Cancer Cell Line ◽  
Luciferase Assay ◽  
Rna Seq ◽  
Chemical Probes ◽  
Covalent Crosslinking ◽  
Straightforward Method

Photoactive RNA probes have unique advantages in the identification of microRNA (miR) targets due to their ability for efficient conjugation to the target sequences by covalent crosslinking, providing stable miR-mRNA complexes for further analysis. Here, we report a highly efficient and straightforward method for miR target identification that is based on photo-reactive chemical probes and RNA-seq technology (denotes PCP-Seq). UV reactive probes were prepared by incorporating psoralen in the specific position of the seed sequence of miR. Cancer cells that were transfected with the miR probes were treated with UV, following the isolation of poly(A) RNA and sequencing of the transcriptome. Quantitative analysis of RNA-seq reads and subsequent validation by qPCR, dual luciferase assay as well as western blotting confirmed that PCP-Seq could highly efficiently identify multiple targets of different miRs in the lung cancer cell line, such as targets PTTG1 and PTGR1 of miR-29a and ILF2 of miR-34a. Collectively, our data showed that PCP-Seq is a robust strategy for miR targets identification, and unique in the identification of the targets that escape degradation by miRISC and maintain normal cellular level, although their translation is repressed.

Biological Evaluation of Curcumin and Related Diarylheptanoids

2006 ◽  
Vol 61 (9-10) ◽  
pp. 625-631 ◽  
Author(s):  
Faridah Abas ◽  
Lim Siang Hui ◽  
Syahida Ahmad ◽  
Johnson Stanslas ◽  
D. A. Israf ◽  
...  
Keyword(s):  
Free Radical ◽  
Cell Line ◽  
Cancer Cell ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Free Radical Scavenging ◽  
Lung Cancer Cell Line ◽  
Cytotoxic Activities

AbstractNine derivatives of three natural diarylheptanoids, curcumin, demethoxycurcumin and bisdemethoxycurcumin, were prepared. Their antioxidant, free radical scavenging, nitric oxide (NO) inhibitory and cytotoxic activities were evaluated and compared with those of the respective natural compounds. Curcumin (1), demethoxycurcumin (2), demethyldemethoxycurcumin (C3), diacetyldemethoxycurcumin (AC2) and triacetyldemethylcurcumin (AC5) exhibited higher antioxidant activity than quercetin while products from demethylation of 1 and 2 exhibited higher free radical scavenging activity. Compounds AC2 and AC5 were found to be most active in inhibiting breast cancer cells (MCF-7) proliferation with IC50 values of 6.7 and 3.6 μм, respectively. The activity of AC2 is almost doubled and of AC5 almost tripled as compared to curcumin. Their selectivity towards different cell lines is also more noticeable. Compounds AC2 and AC5 also showed increased activity against a human prostate cancer cell line (DU-145) and non-small lung cancer cell line (NCI-H460) with IC50 values of 20.4, 16.3 and 18.3, 10.7 μм, respectively.

scholarly journals Synthesis, Biological Evaluation and Docking Study of Etodolac-Triazole Conjugate

2020 ◽  
pp. 35-51
Author(s):  
Papigani Neeraja ◽  
Suryapeta Srinivas ◽  
Venkanna Banothu ◽  
Khagga Mukkanti ◽  
Pramod Kumar Dubey ◽  
...  
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Triazole Ring ◽  
Docking Study ◽  
Biological Evaluation ◽  
Lung Cancer Cell Line ◽  
Human Lung Cancer ◽  
High Yield ◽  
Diffusion Method

A new set of 15 compounds containing etodolac moiety and triazole ring were prepared by CuAAC reaction in moderate to high yield. All the synthesized compounds were purified by chromatographic techniques and characterized by spectral data IR, 1H and 13C NMR and mass spectrometry. The newly derived compounds were screened for their anti-bacterial activities against one gram-positive (S. aureus) and two gram-negative (E. coli, K. pneumoniae) bacteria using an agar-well diffusion method. Most of the compounds showed good to moderate antibacterial activities. Especially compound 4e having good activities against all the strains. The compound 4e displayed significant inhibitory potential with MIC 25 µg/mL against all the strains. The potential DNA gyrase inhibitory activity of this compound was investigated by using molecular docking studies carried out using Autodock Vina software. The compound 4e showed the lowest ΔGbind results (-7.7 Kcal/mol, -7.9Kcal/mol). The cytotoxic activity of the obtained compounds was determined using A549 cancer cell line by a MTT assay. They displayed promising activity against the human lung cancer cell line. Especially 4o, 4b, 4d shown lowest IC50 values.

scholarly journals Synthesis of Analogues of Dicoumarol and Their Biological Evaluation

2018 ◽  
Vol 10 (3) ◽  
pp. 1 ◽  
Author(s):  
Julie Obi ◽  
Tagbo Ezenwa
Keyword(s):  
Lung Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Lung Cancer Cell Line ◽  
Lung Cancer Cell ◽  
Inhibitory Potency ◽  
One Pot ◽  
Microwave Assisted

Both symmetrical (1a-f) and asymmetrical (2a-f) analogues of dicoumarol were synthesized in 20 – 86% yield by using microwave assisted one-pot protocol. Their ability to inhibit NAD (P)H:oxidorectase quinone 1 (NQO1) and cytotoxicity towards A549 small lung cancer cell line were evaluated. Interestingly, (E)-3-(2-hydroxynaphthalen-1-y)chroman-2,4-dione (2d) showed not only moderate inhibitory potency (IC50 = 20 ± 6 nM) towards NQO1 but also was toxic (IC50 = 9.2 ± 0.2 µM) towards the A549 small lung cancer cell line.

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