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Synthesis of a novel CCR1 antagonist for treatment of glioblastoma

Jan et al. | May 05, 2021

Synthesis of a novel CCR1 antagonist for treatment of glioblastoma

Glioblastoma is a brain cancer caused by the presence of a fast-growing, malignant tumor in the brain. As of now, this cancer is universally lethal due to lack of efficacious treatment options. C-C chemokine receptor 1 (CCR1) is a G-protein coupled receptor that controls chemotaxis, the movement of cells in response to chemical stimuli. This research aims to synthesize potential CCR1 antagonists by coupling carboxylic acids with a triazole core. We synthesized these compounds using a simple carboxylic acid coupling and confirmed the identity of the final compounds using nuclear magnetic resonance (NMR) spectroscopy.

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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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Expressional correlations between SERPINA6 and pancreatic ductal adenocarcinoma-linked genes

Selver et al. | Oct 06, 2021

Expressional correlations between <em>SERPINA6</em> and pancreatic ductal adenocarcinoma-linked genes

Pancreatic ductal adenocarcinoma (PDAC) is the most common form of pancreatic cancer, with early diagnosis and treatment challenges. When any of the genes KRAS, SMAD4, TP53, and BRCA2 are heavily mutated, they correlate with PDAC progression. Cellular stress, partly regulated by the gene SERPINA6, also correlates with PDAC progression. When SERPINA6 is highly expressed, corticosteroid-binding globulin inhibits the effect of the stress hormone cortisol. In this study, the authors explored whether there is an inverse correlation between the expression of SERPINA6 and PDAC-linked genes.

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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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The Effect of Ultraviolet Radiation and the Antioxidant Curcumin on the Longevity, Fertility, and Physical Structure of Drosophila melanogaster: Can We Defend Our DNA?

Lateef et al. | May 18, 2019

The Effect of Ultraviolet Radiation and the Antioxidant Curcumin on the Longevity, Fertility, and Physical Structure of <em>Drosophila melanogaster</em>: Can We Defend Our DNA?

Ultraviolet (UV) radiation is known to alter DNA structure and impair cellular function in all living organisms. In this study, Lateef et al examine the effects of UV radiation to determine whether antioxidant-enriched nutrition can combat the potential deleterious effects of UV radiation on Drosophila melanogaster. They found that UVB (320nm) radiation caused a 59% decrease in the Drosophila lifespan and mutagenic effects on flies' physical appearance, but did not significantly affect fertility. Curcumin significantly prolonged lifespan and enhanced fertility for both UV- and non-UV-exposed flies. The research demonstrates the positive potential of natural antioxidants as weapons against radiation-induced diseases including cancer.

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