Synthesis, Molecular Docking and Biological Evaluation of Novel Flavone Derivatives as Potential Anticancer Agents Targeting Akt

Abo-Salem, Heba M; Gibriel, Abdullah Ahmed; Al-Awady, Mohamed; Mandour, A. H.

doi:10.2174/1573406416666200306115035

Cited by 13 publications

(9 citation statements)

References 34 publications

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“…Steatosis is the earliest response to excessive drinking, which is characterized by fat deposition in liver. This phenomenon is reversible after stopping drinking, but long-term excessive drinking can lead to inflammation, fibrosis, and even cancer ( Abo-Salem et al, 2021 ; Ali et al, 2021 ; Mohamady et al, 2020 ). According to statistics, more than 90% of alcoholics show fat accumulation, and 30% of them develop severe ALD ( Gala and Vatsalya, 2020 ).…”

Section: Discussionmentioning

confidence: 99%

Jia-ga-song-tang protection against alcoholic liver and intestinal damage

Fang

Gan

et al. 2022

Front. Pharmacol.

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Gut-liver axis and cellular homeostasis play key roles in alcohol liver disease (ALD). Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) is a stress-sensitive guarantor of cellular homeostasis. We investigated whether the beneficial effects and underlying mechanisms of Jia-ga-song Tang (JGST) against ALD were associated with gut-liver axis and cellular homeostasis. A predictive network depicting the relationship between Jia-Ga-Song-Tang (JGST) and alcoholic liver disease (ALD) was designed by Network pharmacology. Next, 5% v/v Lieber-DeCarli alcohol liquid diet was used to establish the ALD. JGST protected the liver damage, repaired the intestines to alleviate the Two-hit on the liver, and balanced the cellular homeostasis. It was manifested in repairing the liver and intestinal pathological structure, reducing serum ALT, AST, and liver TG, TC, MDA, CAT, and increasing liver GSH, and intestine GSH-Px. JGST mainly inhibited the liver mRNA levels of HO-1, NQO1, GCLC, FASN, and PPARα and activated the intestinal mRNA levels of HO-1 and NQO1, while inhibiting the liver protein levels of HO-1, NQO1. Furthermore, LPS and LBP in the plasma and the expression of inflammatory factors such as IL-1β, TNF-α, IL-6, TGFβ1, CD14, and Myd88 were reduced after treatment to prove that JGST protects the liver from Two-hit. Ethanol was used to intervene in HepG2 and IEC-6 to establish an ALD cell model and treated by Germacrone, ML385, and TBHQ. repaired the intestinal barrier, and inhibited Nrf2 in IEC-6, but protect the HepG2 by activating Nrf2 to balance cellular homeostasis. Our results reinforce that JGST provides an effective protective method for alcoholic liver disease (ALD) by regulating Gut-liver axis and cellular homeostasis.

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Section: Discussionmentioning

confidence: 99%

Jia-ga-song-tang protection against alcoholic liver and intestinal damage

Fang

Gan

et al. 2022

Front. Pharmacol.

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“…Recently, several possible key player targets in cancer that have been linked to various cancer types such as Akt, Topo-isomerase II-B, CTLA4, STAT4, FXR. 45–48 …”

Section: Discussionmentioning

confidence: 99%

Expression and Clinical Values of Serum miR-155 and miR-224 in Chinese Patients with HCV Infection

X¹,

Zhang²,

Wang³

et al. 2022

IJGM

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Background To investigate the expression of serum miR-155 and miR-224 among patients with hepatitis C virus (HCV) infection and analyze their clinical values. Methods A total of 116 patients suffering from HCV infection admitted to our hospital and 70 healthy subjects were selected. According to the diagnostic results, patients with HCV infection were divided into 48 cases of chronic hepatitis C (CHC), 43 cases of liver cirrhosis and 25 cases of hepatocellular carcinoma (HCC). The expression signature for miR-155 and miR-224 was detected in serum samples. ROC curve and Pearson correlation test were conducted to investigate their diagnostic value and correlation. Results The expression extent for serum miR-155 and miR-224 increased along with the increase of malignancy (all P < 0.05). According to ROC curve, the area under the curve (0.918, 95% CI: 0.856–0.974) of miR-155 and miR-224 combined in the diagnosis of HCC was the largest, and its sensitivity and specificity were 93.0% and 86.2%. There is a positive relationship for expression level between miR-155 and miR-224 in CHC and HCC group (all P < 0.001). Conclusion miR-155 and miR-224 are remarkably increased in patients suffering from HCV infection. The combination of miR-155 and miR-224 has a good diagnostic value for HCC caused by HCV infection.

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“…Our data confirms a pattern that had already been suggested by the literature. Whereas flavonoids are anti-proliferative at high concentrations (Abosalem, Gibriel, Al-Awady, & Mandour, 2020;Ammendola et al, 2020) and thus have certain anti-carcinogenic properties, at lower concentrations their effect on precursor cells is more complex and appears to be activating rather than inhibitory. Indeed, we found that 25 µM quercetin increased cell cycle exit and promoted survival and differentiation of adult hippocampal precursor cells, both ex vivo and in vivo.…”

Section: Discussionmentioning

confidence: 99%

Apple peel and flesh contain pro-neurogenic compounds

Ichwan

Walker

Nicola

et al. 2020

Preprint

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AbstractAs mammals evolved exposed to particular diets, naturally abundant compounds may have become part of the set of environmental co-determinants that shaped brain structure and function. Here we investigated whether bioactive factors found in apples directly affect hippocampal neural stem cells and promote neurogenesis in the adult mouse. Whereas the consumption of apple juice per se neither altered adult hippocampal neurogenesis nor improved learning and memory, we did find specific direct effects of apple-derived factors on neural stem cell survival and differentiation. Our results revealed that quercetin, the most abundant flavanol in apple peel, was anti-proliferative at high concentrations but acted pro-neurogenically at low concentrations. This was confirmed in vivo, with intraperitoneally-delivered quercetin promoting survival and neuronal differentiation, without affecting proliferation, likely via the PI3 kinase-Akt and Nrf2-Keap1 pathways, respectively. Using a bio-assay-guided fractionation approach with high-resolution collision induced dissociation mass spectroscopy, we also identified additional pro-neurogenic compounds in apple flesh that were not related to flavonoids. In particular, we found that 3,5-dihydroxybenzoic acid, a weak agonist to the lactate receptor, significantly increased both in vitro and in vivo neural precursor cell proliferation and neurogenesis. Altogether, this work shows that both flavonoids and 3,5-dihydroxybenzoic acid are pro-neurogenic, not only by activating precursor cell proliferation but also through promoting cell cycle exit, cellular survival, and neuronal differentiation.

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Synthesis, Molecular Docking and Biological Evaluation of Novel Flavone Derivatives as Potential Anticancer Agents Targeting Akt

Cited by 13 publications

References 34 publications

Jia-ga-song-tang protection against alcoholic liver and intestinal damage

Jia-ga-song-tang protection against alcoholic liver and intestinal damage

Expression and Clinical Values of Serum miR-155 and miR-224 in Chinese Patients with HCV Infection

Apple peel and flesh contain pro-neurogenic compounds

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