New Thiazoline-Tetralin Derivatives and Biological Activity Evaluation

Turan-Zitouni, Gülhan; Yurttaş, Leyla; Tabbi, Aouatef; Çiftçi, Gülşen Akalın; Temel, Halide Edip; Kaplancıklı, Zafer Asım

doi:10.3390/molecules23010135

Cited by 19 publications

(11 citation statements)

References 40 publications

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“…Seven aromatic compounds were identified from the plant seed extract. Some of the biological activities previously reported for some of the identified compounds are their uses in the management of heart-related chest pain, heart failure, depression, HIV and melanoma (Yancy et al 2016;Aladeokin and Umukoro 2011;Kitamura et al 2012;Bata et al 2015;Turan-Zitouni et al 2018). Though the biological activity for Thiocarbamic acid, N,N-dimethyl, S-1,3-diphenyl-2-butenyl ester is not found in literatures at present, but urea based compounds are known to be derivatives of carbarmic acid (Serban 2019).…”

Section: Discussionmentioning

confidence: 99%

Tetracarpidium conophorum seed extract reduces intestinal absorption, and increases cellular trapping of glucose

2021

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Background Tetracarpidium conophorum is one of the numerous folklore medicinal plants for managing diabetes but the mode of action and bioactive compounds responsible for the antihyperglycemic property are missing in literatures. This study aimed at investigating the possible modes of its antihyperglycemic action using both in-vitro and ex-vivo methods. Powdered Tetracarpidium conophorum seed (TECOSE) was extracted with methanol using standard extraction procedure. Gas chromatography- Mass spectrometry (GCMS) analysis of the extract, and its effects on tissue glucose uptake, α-amylase, α-glucosidase and glucokinase enzymes were assessed using standard laboratory procedures. Results Seven heterocyclic compounds were identified by GCMS of which one is structurally related to sulphonylurea. TECOSE strongly inhibited α-glucosidase (IC50 = 1.90 mg/ml) but partially inhibited α-amylase (IC50 = 7.20 mg/ml) activities. Also, glucokinase activity and tissue glucose uptakes were significantly (p < 0.05) increased by TECOSE. Conclusions The results obtained deduced that antihyperglycemic action of TECOSE could be due to modulation of postprandial hyperglycaemia through inhibition of intestinal α-glucosidase, increasing glucokinase activity, improving peripheral glucose uptake by mimicking sulfonylurea action.

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Section: Discussionmentioning

confidence: 99%

Tetracarpidium conophorum seed extract reduces intestinal absorption, and increases cellular trapping of glucose

2021

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“…The MCF-7 cells were grown in Dulbecco’s Modified Eagle’s medium (DMEM, Gibco; Thermo Fisher Scientific, Inc.) supplemented with 100 μg/mL streptomycin, penicillin (Sigma-Aldrich; Merck KGaA, Darmstadt, Germany) and 10% ( v / v ) FBS (Gibco; Thermo Fisher Scientific, Inc.). The cells were cultured at 37 °C and 5% CO 2 in a humidified environment [32].…”

Section: Methodsmentioning

confidence: 99%

Novel Targeted Anti-Tumor Nanoparticles Developed from Folic Acid-Modified 2-Deoxyglucose

Jin

Guo³

et al. 2019

IJMS

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The glucose analog, 2-deoxyglucose (2-DG), specifically inhibits glycolysis of cancer cells and interferes with the growth of cancer cells. However, the excellent water solubility of 2-DG makes it difficult to be concentrated in tumor cells. In this study, a targeted nano-pharmacosome was developed with folic acid-modified 2-DG (FA-2-DG) by using amino ethanol as a cleavable linker. FA-2-DG was able to self-assemble, forming nano-particles with diameters of 10–30 nm. The biological effects were evaluated with cell viability assays and flow cytometry analysis. Compared with a physical mixture of folic acid and 2-DG, FA-2-DG clearly reduced cell viability and resulted in cell cycle arrest. A computational study involving docking simulation suggested that FA-2-DG can dock into the same receptor as folic acid, thus confirming that the structural modification did not affect the targeting performance. The results indicated that the nano-pharmacosome consisting of FA-2-DG can be used for targeting in a nano-drug delivery system.

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“…The tetralin ring also exists in the structures of some clinically used anticancer drugs, for example, the anthracycline antibiotics doxorubicin, daunorubicin, epirubicin, and idarubicin [3], and so on. Many studies have been performed on tetralin derivatives for use as efficient antitumor agents [4][5][6][7][8][9].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antiproliferative Evaluation of Novel Longifolene-Derived Tetralone Derivatives Bearing 1,2,4-Triazole Moiety

et al. 2020

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Seventeen novel 2-(5-amino-1-(substituted sulfonyl)-1H-1,2,4-triazol-3-ylthio)-6- isopropyl-4,4-dimethyl-3,4-dihydronaphthalen-1(2H)-one compounds were synthesized from the abundant and naturally renewable longifolene and their structures were confirmed by FT-IR, NMR, and ESI-MS. The in vitro cytotoxicity of the synthesized compounds was evaluated by standard MTT assay against five human cancer cell lines, i.e., T-24, MCF-7, HepG2, A549, and HT-29. As a result, compounds 6d, 6g, and 6h exhibited better and more broad-spectrum anticancer activity against almost all the tested cancer cell lines than that of the positive control, 5-FU. Some intriguing structure–activity relationships were found and are discussed herein by theoretical calculation.

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New Thiazoline-Tetralin Derivatives and Biological Activity Evaluation

Cited by 19 publications

References 40 publications

Tetracarpidium conophorum seed extract reduces intestinal absorption, and increases cellular trapping of glucose

Tetracarpidium conophorum seed extract reduces intestinal absorption, and increases cellular trapping of glucose

Novel Targeted Anti-Tumor Nanoparticles Developed from Folic Acid-Modified 2-Deoxyglucose

Synthesis and Antiproliferative Evaluation of Novel Longifolene-Derived Tetralone Derivatives Bearing 1,2,4-Triazole Moiety

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