Antidiabetic effects of trihydroxychalcone derivatives via activation of AMP-activated protein kinase

Shin, Jooseok; Jang, Mi; Park, Jin Chan; Koo, Young Do; Lee, Ji‐Young; Park, Kyong Soo; Chung, Sung Soo; Park, Kwangyong

doi:10.1016/j.jiec.2017.11.003

Cited by 11 publications

(10 citation statements)

References 30 publications

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“…20 Trihydroxychalcone derivatives A1, A2, B1, and B2 were synthesized by Claisen−Schmidt condensation of the corresponding acetophenones with benzaldehydes as following. 21 Ethanol (200 mL) was added to acetophenone A or B (3.9 mmol), benzaldehyde 1 or 2 (4.3 mmol), and KOH (4.0 mmol) in a round-bottomed flask under a nitrogen atmosphere. After the reaction mixture was stirred for 72 h at room temperature, it was quenched with 1% aqueous HCl.…”

Section: Methodsmentioning

confidence: 99%

“…Structure confirmation after synthesis was conducted via 1 H-NMR, 13 C-NMR, FT-IR, and UV−vis absorption in our previous report. 21 2.2. Cell Culture.…”

Section: Methodsmentioning

confidence: 99%

“…The product was purified by column chromatography to yield the corresponding 2′,4′,6′-trihydroxychalcone derivatives A1 , A2 , and B2 as a yellow powder in 78.5, 60.2, and 62.8% isolated yields, respectively. Structure confirmation after synthesis was conducted via 1 H-NMR, 13 C-NMR, FT-IR, and UV–vis absorption in our previous report …”

Section: Experimental Sectionmentioning

confidence: 99%

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In Vitro Osteogenic Differentiation and Antibacterial Potentials of Chalcone Derivatives

et al. 2018

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Chalcone derivatives have been investigated as therapeutic agents for the anticancer, antioxidant, and anti-inflammatory fields. In this study, we have synthesized four different types of chalcone derivatives and demonstrated in vitro bioactivities. We divided these derivatives into two groups of chalcones on the basis of similar substituents on the aromatic rings, and we tested cell viability and proliferation potentials, which indicated that the methoxy substituent on the A ring could enhance cytotoxicity and antiproliferation potential depending on the chalcone concentration. We also investigated osteogenic differentiation of C2C12 cells by ALP staining, the early marker for osteogenesis, which demonstrated that the chalcones could not only induce activity of BMP-2 but also inhibit the activity of noggin, a BMP antagonist. In addition, chalcone bearing hydroxyl groups at the 2-, 4-, and 6-position on the A ring inhibited treptococcus mutans growth, a major causative agent of dental caries. Therefore, we concluded that the chalcone derivatives synthesized in this research can be good candidates for therapeutic agents promoting bone differentiation, with an expectation of inhibiting S. mutans, in dentistry.

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Section: Methodsmentioning

confidence: 99%

“…Structure confirmation after synthesis was conducted via 1 H-NMR, 13 C-NMR, FT-IR, and UV−vis absorption in our previous report. 21 2.2. Cell Culture.…”

Section: Methodsmentioning

confidence: 99%

Section: Experimental Sectionmentioning

confidence: 99%

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In Vitro Osteogenic Differentiation and Antibacterial Potentials of Chalcone Derivatives

et al. 2018

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“…Chalcone derivatives (13a-h) and (19a-h) instreptozotocin-induced diabetic mice, compounds13e, 13g, and 19f reduced TG, TC, and Glu levels, respectively ( Zhu et al, 2018 ). Diabetic mice were treated with trihydroxychalcone derivatives, and therefore, chalcone 13 stimulated activation of AMP-activated protein kinase (AMPK), increased muscle FAO, improved tolerance to glucose, and decreased fat accumulation in the liver and skeletal muscles ( Shin et al, 2018 ). Hypoglycemic activity of sulfonylurea chalcones 1-3 was also exhibited in normoglycemic rabbits to show that all these chalcones have activity comparable to that of gliclazide ( Rao et al, 2014 ).…”

Section: Preclinical Pharmacological Activities Of Chalconesmentioning

confidence: 99%

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence

et al. 2021

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Chalcones are among the leading bioactive flavonoids with a therapeutic potential implicated to an array of bioactivities investigated by a series of preclinical and clinical studies. In this article, different scientific databases were searched to retrieve studies depicting the biological activities of chalcones and their derivatives. This review comprehensively describes preclinical studies on chalcones and their derivatives describing their immense significance as antidiabetic, anticancer, anti-inflammatory, antimicrobial, antioxidant, antiparasitic, psychoactive, and neuroprotective agents. Besides, clinical trials revealed their use in the treatment of chronic venous insufficiency, skin conditions, and cancer. Bioavailability studies on chalcones and derivatives indicate possible hindrance and improvement in relation to its nutraceutical and pharmaceutical applications. Multifaceted and complex underlying mechanisms of chalcone actions demonstrated their ability to modulate a number of cancer cell lines, to inhibit a number of pathological microorganisms and parasites, and to control a number of signaling molecules and cascades related to disease modification. Clinical studies on chalcones revealed general absence of adverse effects besides reducing the clinical signs and symptoms with decent bioavailability. Further studies are needed to elucidate their structure activity, toxicity concerns, cellular basis of mode of action, and interactions with other molecules.

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“…Protocols for synthesis of chalcones.activity of PTP1b by interacting strongly with it and giving a value of IC 50 ¼ 0.92 mM L À1 201. Scheme 3 depicted various synthesis protocols for chalcones.In this work, the IC 50 values for hCA I were determined to be between 13.58 and 18.72 nM, whereas those for hCA II were in between 9 62.…”

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confidence: 99%

Heterocyclic compounds as a magic bullet for diabetes mellitus: a review

Farwa

Raza

2022

RSC Adv.

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Antidiabetic effects of trihydroxychalcone derivatives via activation of AMP-activated protein kinase

Cited by 11 publications

References 30 publications

In Vitro Osteogenic Differentiation and Antibacterial Potentials of Chalcone Derivatives

In Vitro Osteogenic Differentiation and Antibacterial Potentials of Chalcone Derivatives

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence

Heterocyclic compounds as a magic bullet for diabetes mellitus: a review

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