Vehicle development, pharmacokinetics and toxicity of the anti-invasive agent 4-fluoro-3’,4’,5’-trimethoxychalcone in rodents

Mus, Liselot; Denecker, Geertrui; Speleman, Frank; Roman, Bart

doi:10.1371/journal.pone.0192548

Cited by 9 publications

(5 citation statements)

References 25 publications

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“…Moreover, the anticancer effect of chalcones in experimental animals has also been shown [ 27 , 28 ]. Additionally, in contrast to “classical” anticancer agents, chalcones are well tolerated as documented in animal as well as clinical studies [ 29 , 30 , 31 , 32 , 33 , 34 ].…”

Section: Introductionmentioning

confidence: 99%

Molecular Mechanisms of Antiproliferative Effects of Natural Chalcones

Michalková¹,

Mirossay²,

Gazdova³

et al. 2021

Cancers

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Although great progress has been made in the treatment of cancer, the search for new promising molecules with antitumor activity is still one of the greatest challenges in the fight against cancer due to the increasing number of new cases each year. Chalcones (1,3-diphenyl-2-propen-1-one), the precursors of flavonoid synthesis in higher plants, possess a wide spectrum of biological activities including antimicrobial, anti-inflammatory, antioxidant, and anticancer. A plethora of molecular mechanisms of action have been documented, including induction of apoptosis, autophagy, or other types of cell death, cell cycle changes, and modulation of several signaling pathways associated with cell survival or death. In addition, blockade of several steps of angiogenesis and proteasome inhibition has also been documented. This review summarizes the basic molecular mechanisms related to the antiproliferative effects of chalcones, focusing on research articles from the years January 2015–February 2021.

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Section: Introductionmentioning

confidence: 99%

Molecular Mechanisms of Antiproliferative Effects of Natural Chalcones

Michalková¹,

Mirossay²,

Gazdova³

et al. 2021

Cancers

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“…Studies have shown that oral administration of chalcones is well‐tolerated and do not cause toxicity at doses up to 300 mg/kg 22–25 . However, as this is the first study to evaluate the effects of systemic administration of Chalcone T4, we performed the in vivo toxicity experiment using mice prior to subsequent studies using rats because of the reduced body weight and consequently reduced amount of Chalcone T4 needed.…”

Section: Methodsmentioning

confidence: 99%

Chalcone T4, a novel chalconic compound, inhibits inflammatory bone resorption in vivo and suppresses osteoclastogenesis in vitro

Fernandes

Camilli

Maldonado

et al. 2021

J of Periodontal Research

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Objective This study aimed to assess the effect of a novel synthetic chalcone, Chalcone T4, on a murine model of periodontitis and on RANKL‐induced osteoclastogenesis in vitro. Background Chalcones are natural compounds with anti‐inflammatory properties, and its synthetic analogs with enhanced biological effects have potential as therapeutic agents. Periodontitis is characterized by chronic inflammation of the periodontium and alveolar bone resorption. Safe and effective anti‐inflammatory agents can have an important additive effect in the treatment in this disease. Methods Periodontitis was induced via the installation of a ligature around the first molar. Rats (n = 32) received Chalcone T4 (5 and 50 mg/kg) or distilled water by gavage daily for 15 days. Outcomes assessed were bone resorption (μCT), TNF‐α production (ELISA), cellular infiltrate, and collagen content (stereometric analysis, CD45+ cells by immunohistochemistry), and activation of NFATc1 and NF‐kB (immunohistochemistry). In vitro, RAW 264.7 were treated with Chalcone T4 and stimulated with RANKL for assessment of osteoclast differentiation (actin ring staining) and activity (pit assay). Results Chalcone T4 significantly reduced periodontitis‐associated bone resorption, as well as the cellular infiltrate, while increasing the collagen content. Production of TNF‐α, infiltration of CD45‐positive cells, and NF‐kB activation were markedly reduced. In vitro, chalcone T4 inhibited both osteoclast differentiation and activity. Conclusion Chalcone T4 significantly inhibited alveolar bone resorption and inflammation in vivo and RANKL‐induced osteoclastogenesis in vitro, suggesting a therapeutic role for this compound in the treatment of periodontitis.

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“…Environment of rats was maintained with temperature ranged 25 ± 5˚C and 12 hours day night cycle. Free excess to clean drinking water and standard rodent diet adlibitum were provided during the whole study period 9 . They were allocated randomly in two (02) groups with eight (08) rats in each group.…”

Section: Methodsmentioning

confidence: 99%

Evaluation of Chondroprotective Effects of Intra Articular Piroxicam in Post-Traumatic Osteoarthritis Model of Rat

Ishaq

Ali

Haider

et al. 2021

PAFMJ

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Objective: To evaluate the chondroprotective effect of piroxicam in post-traumatic osteoarthritis model of rat. Study Design: Laboratory based experimental study. Place and Duration of Study: Pharmacology department, Army Medical College, Rawalpindi, from Apr to Jun 2019. Methodology: Project included sixteen rats of Sprague Dawley breed. Osteoarthritis was induced in anesthetized rats by surgical removal of medial meniscus and anterior cruciate ligament resection. After that rats were randomly allocated in two groups with eight rats in each group. Rats of group I were positive control that received 0.2 ml saline intra articularly once weekly for four weeks. Meanwhile rats of group II (treatment group) received 50 µl piroxicam intra articularly once weekly for four weeks. One week after the drug intervention, radiograph of the right knee joint of all rats were taken. Animals were then sacrificed with inhaled chloroform and part of proximal tibia was obtained for histopathological analysis. Results: Comparison of radiographs of both groups depicted a significant p-value of <0.01. Meanwhile mean histopathological score of control group and treatment group were 11.50 ± 1.195 and 6.50 ± 1.195 respectively with a p-value of <0.01. Conclusion: Intra articular administration of piroxicam in post-traumatic Osteoarthritis model of rats resulted in improvement in radiographic grades and histopathology scores.

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Vehicle development, pharmacokinetics and toxicity of the anti-invasive agent 4-fluoro-3’,4’,5’-trimethoxychalcone in rodents

Cited by 9 publications

References 25 publications

Molecular Mechanisms of Antiproliferative Effects of Natural Chalcones

Molecular Mechanisms of Antiproliferative Effects of Natural Chalcones

Chalcone T4, a novel chalconic compound, inhibits inflammatory bone resorption in vivo and suppresses osteoclastogenesis in vitro

Evaluation of Chondroprotective Effects of Intra Articular Piroxicam in Post-Traumatic Osteoarthritis Model of Rat

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