A violacein-producing bacterium was isolated from a mud sample collected near a hot spring on Kümbet Plateau in Giresun Province and named the GK strain. According to the phylogenetic tree constructed using 16S rRNA gene sequence analysis, the GK strain was identified and named Janthinobacterium sp. GK. The crude violacein pigments were separated into three different bands on a TLC sheet. Then violacein and deoxyviolacein were purified by vacuum liquid column chromatography and identified by NMR spectroscopy. According to the inhibition studies, the HIV-1 RT inhibition rate of 1 mM violacein from the GK strain was 94.28% and the CoV-2 spike RBD:ACE2 inhibition rate of 2 mM violacein was 53%. In silico studies were conducted to investigate the possible interactions between violacein and deoxyviolacein and three reference molecules with the target proteins: angiotensin-converting enzyme 2 (ACE2), HIV-1 reverse transcriptase, and SARS-CoV-2 spike receptor binding domain. Ligand violacein binds strongly to the receptor ACE2, HIV-1 reverse transcriptase, and SARS-CoV-2 spike receptor binding domain with a binding energy of −9.94 kcal/mol, −9.32 kcal/mol, and −8.27 kcal/mol, respectively. Deoxyviolacein strongly binds to the ACE2, HIV-1 reverse transcriptase, and SARS-CoV-2 spike receptor binding domain with a binding energy of −10.38 kcal/mol, -9.50 kcal/mol, and −8.06 kcal/mol, respectively. According to these data, violacein and deoxyviolacein bind to all the receptors quite effectively. SARS-CoV-2 spike protein and HIV-1-RT inhibition studies with violacein and deoxyviolacein were performed for the first time in the literature. Graphical abstract
Kiraz (Prunus avium) antosiyanin gibi immün sistem için faydalı olan flavonoidler açısından oldukça zengin bir bitkidir. Bu çalışmada amaç Prunus avium'dan ekstrakte edilen total antosiyaninlerin (TAP) in vitro antigenotoksik ve antisitotoksik etkilerini insan lenfositlerinde kromozomal anormallik (CA), tek hücre jel elektroforezi (Comet) ve Mikronükleus testleri (MN) ile değerlendirmektir. Çalışmamızda, insan lenfositlerinde mitomisin-C ve H2O2 ile indüklenen DNA hasarına karşı TAP'ın 50, 100, 200 and 400 µg/mL'lik konsantrasyonlarının koruyucu etkisi gözlemlenmiştir. Ayrıca, pozitif, negatif ve çözücü kontrol grupları da dahil edilmiştir. Pozitif kontrole göre TAP; 24 saatlik uygulamanın 200 ve 400 µg/mL'lik, 48 saatlik uygulamanın ise tüm konsantrasyonlarında anormal hücre yüzdesini ve CA/hücre frekansını istatistiksel olarak anlamlı bir şekilde azaltmıştır. Benzer şekilde TAP, mitotik indeksi istatistiksel olarak anlamlı bir şekilde 24 saatlik uygulamanın sadece 200 µg/mL'lik konsantrasyonunda artırırken, 48 saatlik uygulamanın ise tüm dozlarında (200 µg/mL'lik konsantrasyon hariç) artırmıştır. Bu sonuçlara paralel olarak TAP, MN frekansını da pozitif kontrole göre tüm konsantrasyonlarda istatistiksel olarak anlamlı bir şekilde azaltmıştır. Comet testinde yapılan TAP uygulamasıyla tüm dozlarda kuyruk uzunluğu, kuyruk momenti ve kuyruk yoğunluğunda da anlamlı bir azalma olduğu gözlemlenmiştir. Elde edilen bu sonuçlara göre, TAP'ın mitomisin-C ve H2O2 gibi genotoksik ajanlara karşı potansiyel antisitotoksik ve antigenotoksik koruyucu bir etkiye sahip olduğu gösterilmiştir.
The aim of present study, to evaluate the genotoxic potential of 1-(4-(3,3-dimethyl-1,6-dioxo-2,3,4,6,11,13-hexahydro-1H-indazolo[1,2b] phthalazine-13yl) phenyl)-2-phenylazetidine-3-yl-acetate which was synthesised assuming that it may be a pharmaceutical raw material and found to inhibit human carbonic anhydrase I, II isozymes. To determine the genotoxic potential of this phthalazine substituted β-lactam compound, chromosomal aberration (CA) and micronucleus (MN) tests were implemented in human peripheral blood lymphocytes. In these tests, lymphocyte cultures were treated with four concentrations (30, 15, 7.5, 3.75 μg/mL) of test compound and simultaneously with negative control (sterile distilled water), solvent control (DMSO) positive control (MMC). According to our results, CA frequencies were signifi cantly increased in two high applied concentrations (30, 15 μg/mL) compared with negative and solvent control. MN frequencies were signifi cantly increased in three applied concentrations (30, 15, 7.5 μg/ mL) except lowest concentration (3.75 μg/mL) compared with solvent control. Mitotic indices were also affected by treatment with test compound. The obtained results provide evidence to demonstrate that new phthalazine substituted β-lactam derivative can exert genotoxic and cytotoxic effects in peripheral human lymphocytes especially at high concentrations.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.