Cream production and biological in vivo/in vitro activity assessment of a novel boron-based compound derived from quercetin and phenyl boronic acid

Temel, Hamdi; Atlan, Metin; Ertaş, Abdülselam; Yener, İsmail; Akdeniz, Mehmet; Yazan, Zehra; Yılmaz, Mustafa Abdullah; Doğanyiğit, Züleyha; Okan, Aslı; Akyüz, Enes

doi:10.1016/j.jtemb.2022.127073

Cited by 4 publications

(3 citation statements)

References 46 publications

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“…These flavonoids represent a vital component of the extract's chemical composition, contributing to its potential health-related properties. In support of our findings, Temel et al conducted a comprehensive study in which they reported that quercetin, a prominent flavonoid found in the 80% ethanolic extracts, plays a noteworthy role in the inhibition of BchE [39]. Their research reinforces the significance of quercetin and its potential therapeutic implications, particularly in the context of enzyme inhibition, further underlining the value of these flavonoid-rich extracts.…”

Section: Enzymes Inhibition Propertiessupporting

confidence: 86%

Evaluating Phytochemical Profiles, Cytotoxicity, Antiviral Activity, Antioxidant Potential, and Enzyme Inhibition of Vepris boiviniana Extracts

Bakar,

Nilofar,

Mohamed

et al. 2023

Molecules

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In the present study, we performed comprehensive LC-MS chemical profiling and biological tests of Vepris boiviniana leaves and stem bark extracts of different polarities. In total, 60 bioactive compounds were tentatively identified in all extracts. The 80% ethanolic stem bark extract exhibited the highest activity in the ABTS assay, equal to 551.82 mg TE/g. The infusion extract of stem bark consistently demonstrated elevated antioxidant activity in all assays, with values ranging from 137.39 mg TE/g to 218.46 mg TE/g. Regarding the enzyme inhibitory assay, aqueous extracts from both bark and leaves exhibited substantial inhibition of AChE, with EC50 values of 2.41 mg GALAE/g and 2.25 mg GALAE/g, respectively. The 80% ethanolic leaf extract exhibited the lowest cytotoxicity in VERO cells (CC50: 613.27 µg/mL) and demonstrated selective cytotoxicity against cancer cells, particularly against H1HeLa cells, indicating potential therapeutic specificity. The 80% ethanolic bark extract exhibited elevated toxicity in VERO cells but had reduced anticancer selectivity. The n-hexane extracts, notably the leaves’ n-hexane extract, displayed the highest toxicity towards non-cancerous cells with selectivity towards H1HeLa and RKO cells. In viral load assessment, all extracts reduced HHV-1 load by 0.14–0.54 log and HRV-14 viral load by 0.13–0.72 log, indicating limited antiviral activity. In conclusion, our research underscores the diverse bioactive properties of Vepris boiviniana extracts, exhibiting potent antioxidant, enzyme inhibitory, and cytotoxicity potential against cancer cells.

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Section: Enzymes Inhibition Propertiessupporting

confidence: 86%

Evaluating Phytochemical Profiles, Cytotoxicity, Antiviral Activity, Antioxidant Potential, and Enzyme Inhibition of Vepris boiviniana Extracts

Bakar,

Nilofar,

Mohamed

et al. 2023

Molecules

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show abstract

“…It was intended to prepare a new nanoethosomal gel that was based on quercetin and phenyl boronic acid because of these characteristics of boron compounds and quercetin. 9 For the treatment of diabetic neuropathy, nanoethosomal gel formulations have been prepared to augment transdermal drug delivery through the skin. The permeability and systemic availability of epalrestat increased by combining nanoethosomes and permeation enhancers.…”

Section: ■ Introductionmentioning

confidence: 99%

“…Lipid-based drug delivery systems are therefore highly desired to enhance the topical distribution of the medications. It was intended to prepare a new nanoethosomal gel that was based on quercetin and phenyl boronic acid because of these characteristics of boron compounds and quercetin . For the treatment of diabetic neuropathy, nanoethosomal gel formulations have been prepared to augment transdermal drug delivery through the skin.…”

Section: Introductionmentioning

confidence: 99%

Exploring the Potent Combination of Quercetin–Boronic Acid, Epalrestat, and Urea Containing Nanoethosomal Keratolytic Gel for the Treatment of Diabetic Neuropathic Pain: In Vitro and In Vivo Studies

et al. 2023

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Transdermal penetration of therapeutic moieties from topical dosage forms always remains a challenge due to the presence of permeation impeding keratin which should be addressed. The purpose of the study was to formulate quercetin and 4-formyl phenyl boronic acid (QB complex) used for the preparation of nanoethosomal keratolytic gel (EF3-G). The QB complex was confirmed by Fourier transform infrared spectroscopy while skin permeation, viscosity, and epalrestat entrapment efficiency were used for the optimization of nanoethosomal gel. The keratolytic effect of the proposed nanoethosomal gel with urea (QB + EPL + U) was calculated in rat and snake skin. The spherical shape of nanoethosomes was confirmed by scanning electron microscopy. According to the findings of stability studies, viscosity decreases as temperature increases, proving their thermal stability. The negative charge of optimized EF3 with 0.7 PDI proved narrow particle size distribution with homogeneity. Optimized EF3 showed two folds increase of epalrestat permeation in highly keratinized snake skin as compared to rats' skin after 24 h. Antioxidant behaviors of EF3 (QB) > QB complex > quercetin > ascorbic acid proved reduction of oxidative stress in DPPH reduction analysis. Interestingly, the hot plate and cold allodynia test in the diabetic neuropathic rat model reduced 3-fold pain as compared to the diabetic control group which was further confirmed by in vivo biochemical studies even after the eight week. Conclusively, ureal keratolysis, primary dermal irritation index reduction, and improved loading of epalrestat render the nanoethosomal gel (EF3-G) ideal for the treatment of diabetic neuropathic pain.

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In silico and biological activity evaluation of quercetin-boron hybrid compounds, anti-quorum sensing effect as alternative potential against microbial resistance

Temel

Atlan

Türkmenoğlu

et al. 2023

Journal of Trace Elements in Medicine and Biology

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Cream production and biological in vivo/in vitro activity assessment of a novel boron-based compound derived from quercetin and phenyl boronic acid

Cited by 4 publications

References 46 publications

Evaluating Phytochemical Profiles, Cytotoxicity, Antiviral Activity, Antioxidant Potential, and Enzyme Inhibition of Vepris boiviniana Extracts

Evaluating Phytochemical Profiles, Cytotoxicity, Antiviral Activity, Antioxidant Potential, and Enzyme Inhibition of Vepris boiviniana Extracts

Exploring the Potent Combination of Quercetin–Boronic Acid, Epalrestat, and Urea Containing Nanoethosomal Keratolytic Gel for the Treatment of Diabetic Neuropathic Pain: In Vitro and In Vivo Studies

In silico and biological activity evaluation of quercetin-boron hybrid compounds, anti-quorum sensing effect as alternative potential against microbial resistance

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