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High-throughput virtual screening of novel dihydropyrimidine monastrol analogs reveals robust structure-activity relationship to kinesin Eg5 binding thermodynamics

Shern et al. | Jan 20, 2021

High-throughput virtual screening of novel dihydropyrimidine monastrol analogs reveals robust structure-activity relationship to kinesin Eg5 binding thermodynamics

As cancer continues to take millions of lives worldwide, the need to create effective therapeutics for the disease persists. The kinesin Eg5 assembly motor protein is a promising target for cancer therapeutics as inhibition of this protein leads to cell cycle arrest. Monastrol, a small dihydropyrimidine-based molecule capable of inhibiting the kinesin Eg5 function, has attracted the attention of medicinal chemists with its potency, affinity, and specificity to the highly targeted loop5/α2/α3 allosteric binding pocket. In this work, we employed high-throughput virtual screening (HTVS) to identify potential small molecule Eg5 inhibitors from a designed set of novel dihydropyrimidine analogs structurally similar to monastrol.

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Phytochemical Analysis of Amaranthus spinosus Linn.: An in vitro Analysis

Sharma et al. | Mar 20, 2021

Phytochemical Analysis of <em>Amaranthus spinosus</em> Linn.: An <em>in vitro</em> Analysis

Mainstream cancer treatments, which include radiotherapy and chemotherapeutic drugs, are known to induce oxidative damage to healthy somatic cells due to the liberation of harmful free radicals. In order to avert this, physiological antioxidants must be complemented with external antioxidants. Here the authors performed a preliminary phytochemical screen to identify alkaloids, saponins, flavonoids, polyphenols, and tannins in all parts of the Amaranthus spinosus Linn. plant. This paper describes the preparation of this crude extract and assesses its antioxidant properties for potential use in complementary cancer treatment.

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Comparing the Effects of Different Natural Products on Reducing Tumor Growth in a Drosophila Model

Ganesh et al. | May 31, 2020

Comparing the Effects of Different Natural Products on Reducing Tumor Growth in a <i>Drosophila</i> Model

In this work, the authors compared the effects of common natural products, including sesame, cinnamon, garlic, moringa and turmeric on tumor growth in Drosophila eyes. The data showed that these natural products cannot be used to reduce tumor growth once it has completely formed. However, the data suggested that some natural products can reduce cancer cell growth when tumors are treated early.

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In vitro Comparison of Anticancer and Immunomodulatory Activities of Resveratrol and its Oligomers

Zhang et al. | Sep 02, 2020

<em>In vitro</em> Comparison of Anticancer and Immunomodulatory Activities of Resveratrol and its Oligomers

Resveratrol is a type of stillbenoid, a phenolic compound produced in plants, that is known for its anti-inflammatory and anticancer effects. Many oligomers of resveratrol have recently been isolated their bioactivities remain unknown. Here, authors compared the bioactivities of resveratrol with natural dimers (ε-viniferin and gnetin H) and trimers (suffruticosol B and C). Results provide preliminary evidence that resveratrol oligomers could be potential preventive or therapeutic agents for cancers and other immune-related diseases

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Evaluation of Tea Extract as an Inhibitor of Oxidative Stress in Prostate Cells

Zhang et al. | Jan 22, 2019

Evaluation of Tea Extract as an Inhibitor of Oxidative Stress in Prostate Cells

One important factor that contributes to human cancers is accumulated damage to cells' DNA due to the oxidative stress caused by free radicals. In this study, the authors investigate the effects of several different tea leaf extracts on oxidative stress in cultured human prostate cells to see if antioxidants in the tea leaves could help protect cells from this type of DNA damage. They found that all four types of tea extract (as well as direct application of the antioxidant EGCG) improved the outcomes for the cultured cells, with white tea extract having the strongest effect. This research suggests that tea extracts and the antioxidants that they contain may have applications in the treatment of the many diseases associated with cellular DNA damage, including cancer.

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Anticancer, anti-inflammatory, and apoptotic activities of MAT20, a poly-herbal formulation.

Kashyap Jha et al. | Mar 29, 2022

Anticancer, anti-inflammatory, and apoptotic activities of MAT20, a poly-herbal formulation.

Kashyap Jha et al. look at the formulation of MAT20, a crude extract of the moringa, amla, and tulsi leaves, as a potential complementary and alternative medicine. Using HeLa cells, they find MAT20 up-regulates expression of inflammation and cell cytotoxicity markers. Their data is important for understanding the anti-cancer and anti-inflammatory properties of MAT20.

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In silico modeling of emodin’s interactions with serine/threonine kinases and chitosan derivatives

Suresh et al. | Jan 10, 2022

<i>In silico</i> modeling of emodin’s interactions with serine/threonine kinases and chitosan derivatives

Here, through protein-ligand docking, the authors investigated the effect of the interaction of emodin with serine/threonine kinases, a subclass of kinases that is overexpressed in many cancers, which is implicated in phosphorylation cascades. Through molecular dynamics theyfound that emodin forms favorable interactions with chitosan and chitosan PEG (polyethylene glycol) copolymers, which could aid in loading drugs into nanoparticles (NPs) for targeted delivery to cancerous tissue. Both polymers demonstrated reasonable entrapment efficiencies, which encourages experimental exploration of emodin through targeted drug delivery vehicles and their anticancer activity.

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The Protective Antioxidant Effects of Sulforaphane on Germinating Radish Seeds Treated with Hydrogen Peroxide

Dasuri et al. | Feb 19, 2021

The Protective Antioxidant Effects of Sulforaphane on Germinating Radish Seeds Treated with Hydrogen Peroxide

Free radical chain reactions result when atoms containing unpaired electrons bind with biomolecules and alter their biological functions, contributing to the progression of diseases such as atherosclerosis, cancer, and diabetes. Antioxidants, such as vitamin E and sulforaphane, are effective neutralizers of free radicals and prevent cellular damage. This present study is conducted to determine the relative effectiveness of sulforaphane against free radicals generated by hydrogen peroxide (H2O2) compared with the known antioxidant vitamin E.

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Investigation of unknown causes of uveal melanoma uncovers seven recurrent genetic mutations

Nanda et al. | Aug 25, 2022

Investigation of unknown causes of uveal melanoma uncovers seven recurrent genetic mutations

Uveal melanoma (UM) is a rare subtype of melanoma but the most frequent primary cancer of the eye in adults. The goal of this study was to research the genetic causes of UM through a comprehensive frequency analysis of base-pair mismatches in patient genomes. Results showed a total of 130 genetic mutations, including seven recurrent mutations, with most mutations occurring in chromosomes 3 and X. Recurrent mutations varied from 8.7% to 17.39% occurrence in the UM patient sample, with all mutations identified as missense. These findings suggest that UM is a recessive heterogeneous disease with selective homozygous mutations. Notably, this study has potential wider significance because the seven genes targeted by recurrent mutations are also involved in other cancers.

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Herbal formulation, HF1 diminishes tumorigenesis: a cytokine study between MCF-7 and BM-MSCs.

Guru et al. | Apr 11, 2022

Herbal formulation, HF1 diminishes tumorigenesis: a cytokine study between MCF-7 and BM-MSCs.

The authors use HF-1, an herbal formation, on bone marrow derived cells as well as breast cancer cells to assess HF-1's ability to prevent tumorigenesis. As metastasis requires coordination of multiple cells in the tumor microenvironment, their findings that HF-1 augments cytokine expression such as VEGF & TGF-B show that HF-1 has potential application to therapeutics.

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