Chrysin: A Promising Anticancer Agent its Current Trends and Future Perspectives

Mehdi, Syed Hassan; Nafees, Sana; Zafaryab,; Khan, Asad; Rizvi, Md. Moshahid Alam

doi:10.21767/2248-9215.100057

Cited by 18 publications

(18 citation statements)

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“…Therefore, the use of nutraceuticalbased drugs that can improve the effectiveness of Tmz at lower concentrations could reduce drug resistance and enhance the programmed cell death of GBM cells with minimal side effects. Chrysin, a natural avonoid found in various fruits and plants, including honey, possesses chemopreventive, antiproliferative, antimetastatic, and antineoplastic activities in various cancer models 20 . However, the potential role of chrysin in different GBM models are not fully explored.…”

Section: Discussionmentioning

confidence: 99%

Chrysin Promotes Temozolomide-induced Apoptosis by Activating p38 MAPK and Suppressing Akt and ERK1/2 in Human Glioblastoma.

Kamarudin¹,

Parhar²

2021

Preprint

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Temozolomide (Tmz) faces the challenges of high chemoresistance and high dose leading to various side-effects. Chrysin exhibits anticancer and adjuvant effects in various cancer models. Nevertheless, chrysin’s synergistic effect with Tmz against Tmz-sensitive and Tmz-resistant human glioblastoma has never been reported. Chrysin and Tmz reduced the viability of A172 and LN18 in concentration- and time-dependent manner, with chrysin exhibited IC50 values lower than Tmz. The combination of chrysin and Tmz enhanced cell death (CI indexes between 0.59–0.98), suggesting synergistic efficacy of chrysin at lower concentrations. Chrysin promoted Tmz-induced phosphatidylserine externalization and depolarization of mitochondrial membrane potential. Chrysin promoted Tmz-induced suppression of pAkt (Ser473) and pERK1/2 (Thr202/Tyr204) while enhanced the phosphorylation of p38 MAPK (Thr180/Tyr182). This further reduced the antiapoptotic proteins (Bcl-2, Bcl-xL, Mcl-1), elevated proapoptotic proteins (Bax, Bad, Bak, PUMA, Noxa), and activated caspase-9 and caspase-3 compared to Tmz treatment alone. Pretreatment with Z-LEHD-FMK and Z-VAD-FMK attenuated apoptosis and restored caspase-9 and − 3 levels. However, pretreatment with Z-IETD-FMK did not suppress the promotion of apoptosis. Collectively, chrysin promotes Tmz-induced apoptosis through p38 MAPK activation and suppression of Akt and ERK1/2. These results suggest chrysin as a potential therapeutic adjuvant to improve Tmz effects in Tmz-sensitive and -resistant GBM.

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Section: Discussionmentioning

confidence: 99%

Chrysin Promotes Temozolomide-induced Apoptosis by Activating p38 MAPK and Suppressing Akt and ERK1/2 in Human Glioblastoma.

Kamarudin¹,

Parhar²

2021

Preprint

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“…Chrysin is an apigenin analogue with high therapeutic potential favorable to intestinal membrane transport. However, its low bioavailability due to rapid metabolism and excretion renders its use less beneficial when compared to other flavonoid compounds [124,125]. Chrysin demonstrated high potency as an aromatase inhibitor in addition to its well-known role as an anti-inflammatory, antioxidant, and cancer chemo-preventive agent [126].…”

Section: Phytochemicalsmentioning

confidence: 99%

Flavonoids in Cancer and Apoptosis

Abotaleb

Samuel

Varghese

et al. 2018

Cancers

542

394

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Cancer is the second leading cause of death globally. Although, there are many different approaches to cancer treatment, they are often painful due to adverse side effects and are sometimes ineffective due to increasing resistance to classical anti-cancer drugs or radiation therapy. Targeting delayed/inhibited apoptosis is a major approach in cancer treatment and a highly active area of research. Plant derived natural compounds are of major interest due to their high bioavailability, safety, minimal side effects and, most importantly, cost effectiveness. Flavonoids have gained importance as anti-cancer agents and have shown great potential as cytotoxic anti-cancer agents promoting apoptosis in cancer cells. In this review, a summary of flavonoids and their effectiveness in cancer treatment targeting apoptosis has been discussed.

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“…5,7-Dihydroxyflavone is found abundantly in honey, fruits, bee pollen, propolis, and medical plants, such as Passiflora caerulea L. and Tilia tomentosa [165]. This flavonoid is an analog to apigenin but with lower bioavailability due to rapid excretion and metabolism [166]. Chrysin treatment in STZ-induced rats reported an elevation of glucose, MDA, TG, TC, LDL-C and a reduction of HDL-C, total protein, SOD, CAT, and GST [167].…”

Section: Anti-diabetic Effects Of Selected Flavonoidsmentioning

confidence: 99%

Flavonoids and Their Anti-Diabetic Effects: Cellular Mechanisms and Effects to Improve Blood Sugar Levels

et al. 2019

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Diabetes mellitus (DM) is a prevailing global health metabolic disorder, with an alarming incidence rate and a huge burden on health care providers. DM is characterized by the elevation of blood glucose due either to a defect in insulin synthesis, secretion, binding to receptor, or an increase of insulin resistance. The internal and external factors such as obesity, urbanizations, and genetic mutations could increase the risk of developing DM. Flavonoids are phenolic compounds existing as secondary metabolites in fruits and vegetables as well as fungi. Their structure consists of 15 carbon skeletons and two aromatic rings (A and B) connected by three carbon chains. Flavonoids are furtherly classified into 6 subclasses: flavonols, flavones, flavanones, isoflavones, flavanols, and anthocyanidins. Naturally occurring flavonoids possess anti-diabetic effects. As in vitro and animal model’s studies demonstrate, they have the ability to prevent diabetes and its complications. The aim of this review is to summarize the current knowledge addressing the antidiabetic effects of dietary flavonoids and their underlying molecular mechanisms on selected pathways: Glucose transporter, hepatic enzymes, tyrosine kinase inhibitor, AMPK, PPAR, and NF-κB. Flavonoids improve the pathogenesis of diabetes and its complications through the regulation of glucose metabolism, hepatic enzymes activities, and a lipid profile. Most studies illustrate a positive role of specific dietary flavonoids on diabetes, but the mechanisms of action and the side effects need more clarification. Overall, more research is needed to provide a better understanding of the mechanisms of diabetes treatment using flavonoids.

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Chrysin: A Promising Anticancer Agent its Current Trends and Future Perspectives

Cited by 18 publications

References 0 publications

Chrysin Promotes Temozolomide-induced Apoptosis by Activating p38 MAPK and Suppressing Akt and ERK1/2 in Human Glioblastoma.

Chrysin Promotes Temozolomide-induced Apoptosis by Activating p38 MAPK and Suppressing Akt and ERK1/2 in Human Glioblastoma.

Flavonoids in Cancer and Apoptosis

Flavonoids and Their Anti-Diabetic Effects: Cellular Mechanisms and Effects to Improve Blood Sugar Levels

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