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2.
Fish Shellfish Immunol ; 129: 231-242, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36067907

RESUMO

The codon-optimized anti-lipopolysaccharide factor (ALF) sequence was introduced into pPICZαA vector and transformed into Pichia pastoris GS115. The recombinant ALF yeast supernatant (rALF-mix) was freeze-dried and evaluated as a feed additive for Litopenaeus vannamei. It was found by antibacterial activity test in vitro that the rALF-mix had antibacterial activity under different pH and temperature conditions. The 0, 0.00375%, 0.0075%, 0.015%, 0.03% and 0.06% of rALF-mix were added respectively to make the six experimental diets. After a 10-week feeding trial with shrimps (2.36 ± 0.02 g), it was found that the weight gain rate (WGR) and protein efficiency ratio (PER) of shrimp in the groups with 0.0075%, 0.015% and 0.03% of dietary rALF-mix supplementation were significantly higher than those in the control group (P < 0.05). Dietary rALF-mix supplementation significantly increased the total haemocyte count, respiratory burst, phagocytic activity, total anti-oxidative capacity (T-AOC), phenol oxidase activity, nitric oxide synthase activity, lysozyme (LYZ) activity, serum antibacterial capacity in the hemolymph and the T-AOC, LYZ in the hepatopancreas of shrimps (P < 0.05). The malondialdehyde contents in hemolymph and hepatopancreas were significantly decreased (P < 0.05). Meanwhile, the expression levels of toll, immune deficiency, heat shock protein 70, crustin and lipopolysaccharide-ß-glucan binding protein in the gill of shrimps were significantly increased (P < 0.05). After the challenge test, it was showed that dietary rALF-mix supplementation significantly improved the resistance of L. vannamei to Vibrio parahaemolyticus (P < 0.05). In conclusion, the rALF-mix can be used as a functional feed additive to improve the growth, immunity and disease resistance of shrimp. Based on the quadratic regression analysis for WGR, the optimal supplemental level of rALF-mix in diet for shrimp was estimated to be 0.02813%.


Assuntos
Ração Animal , Penaeidae , Ração Animal/análise , Animais , Antibacterianos/farmacologia , Dieta/veterinária , Suplementos Nutricionais/análise , Resistência à Doença , Proteínas de Choque Térmico HSP70 , Imunidade Inata/genética , Lipopolissacarídeos/farmacologia , Malondialdeído , Monofenol Mono-Oxigenase , Muramidase/metabolismo , Óxido Nítrico Sintase , Saccharomycetales
3.
Molecules ; 27(17)2022 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-36080217

RESUMO

BACKGROUND: The dysregulation of melanin production causes skin-disfiguring ultraviolet (UV)-associated hyperpigmented spots. Previously, we found that the activation of c-Jun N-terminal kinase (JNK), a mitogen-activated protein kinase (MAPK), inhibited melanogenesis. METHODS: We selected BCI-215 as it may modify MAPK expression via a known function of a dual-specificity phosphatase (DUSP) 1/6 inhibitor. B16F10 melanoma cells, Mel-ab cells, human melanocytes, and a coculture were used to assess the anti-melanogenic activity of BCI-215. The molecular mechanisms were deciphered by assaying the melanin content and cellular tyrosinase activity via immunoblotting and RT-PCR. RESULTS: BCI-215 was found to suppress basal and cAMP-stimulated melanin production and cellular tyrosinase activity in vitro through the downregulation of microphthalmia-associated transcription factor (MITF) protein and its downstream enzymes. The reduction in MITF expression caused by BCI-215 was found to be due to all three types of MAPK activation, including extracellular signal-regulated kinase (ERK), JNK, and p38. The degree of activation was greater in ERK. A phosphorylation of the ß-catenin pathway was also demonstrated. The melanin index, expression of MITF, and downstream enzymes were well-reduced in UVB-irradiated ex vivo human skin by BCI-215. CONCLUSIONS: As BCI-215 potently inhibits UV-stimulated melanogenesis, small molecules of DUSP-related signaling modulators may provide therapeutic benefits against pigmentation disorders.


Assuntos
Interfaces Cérebro-Computador , Fosfatases de Especificidade Dupla , Hiperpigmentação , Linhagem Celular Tumoral , Fosfatases de Especificidade Dupla/antagonistas & inibidores , MAP Quinases Reguladas por Sinal Extracelular/metabolismo , Humanos , Hiperpigmentação/metabolismo , Melaninas , Melanócitos/metabolismo , Monofenol Mono-Oxigenase , Pigmentação
4.
BMC Genom Data ; 23(1): 71, 2022 09 09.
Artigo em Inglês | MEDLINE | ID: mdl-36085015

RESUMO

BACKGROUND: Protein kinase C (PKC) is a multifunctional serine and PKC can phosphorylate serine residues in the cytoplasmic domain of tyrosinase, thereby regulating the activity of tyrosinase. Activated PKC is bound to the melanosome membrane, and unactivated PKC is free in the cytoplasm of melanocytes. In this study, we study the role of PKC gene in the melanin synthesis pathway and its effect on the color of the nacre of H. cumingii. RESULTS: In this study, a HcPKC gene in H. cumingii was cloned and its effects on melanin synthesis and nacre color were studied. HcPKC was expressed in both purple and white mussels, and the level of mRNA expression was higher in the purple mussels than in white mussels. Strong and specific mRNA signals were detected in the dorsal epithelial cells of the mantle pallial layer, indicating that HcPKC may be involved in nacre formation. After SNP association with inner shell color related traits, according to the principle that 0.25 < PIC < 0.5 is medium polymorphism and PIC < 0.25 is low polymorphism, the A + 332G site on the HcPKC gene was a site of moderate polymorphism, and the other four sites were low polymorphism sex sites. There was strong linkage disequilibrium among the five loci. A haplotype was constructed and it was found that the frequency of T1 (AGGAA)in the white population was significantly higher than that in the purple population (P < 0.05). CONCLUSION: The study found that HcPKC of H. cumingii can be used as a candidate gene related to inner shell color, and some of the SNP sites can be used for molecular-assisted breeding in the spinnaker mussel, providing a reference for cultivating high-quality freshwater pearls.


Assuntos
Bivalves , Nácar , Unionidae , Animais , Bivalves/genética , Expressão Gênica , Melaninas/genética , Monofenol Mono-Oxigenase/genética , Nácar/genética , Nucleotídeos/metabolismo , Proteína Quinase C/genética , RNA Mensageiro/genética , Serina/genética , Unionidae/genética
5.
Nat Commun ; 13(1): 5436, 2022 Sep 16.
Artigo em Inglês | MEDLINE | ID: mdl-36114194

RESUMO

Benzylisoquinoline alkaloid derived pharmaceuticals are widely applied in modern medicines. Recent studies on the microbial production of benzylisoquinolines have highlighted key biological syntheses towards these natural products. Routes to non-natural benzylisoquinolines have been less explored, particularly halogenated compounds which are more challenging. Here, we show the use of a tyrosinase, tyrosine decarboxylase, transaminase, and norcoclaurine synthase which are combined in a parallel cascade design, in order to generate halogenated benzylisoquinoline alkaloids in high enantiomeric excess. Notably, mutagenesis studies are applied to generate tyrosinase mutants, which enhance the acceptance of halogenated tyrosines for use in the biocatalytic cascades developed.


Assuntos
Alcaloides , Benzilisoquinolinas , Produtos Biológicos , Monofenol Mono-Oxigenase/genética , Preparações Farmacêuticas , Transaminases , Tirosina Descarboxilase
6.
Molecules ; 27(17)2022 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-36080207

RESUMO

We focused on the functional components, antioxidant activity, skin-whitening, and anti-wrinkle properties of subcritical and supercritical water (SCW)-treated rutin. Rutin treatments were performed at the following temperature and pressure conditions: 200 °C/15 bar, 300 °C/100 bar, and 400 °C/250 bar. ABTS and DPPH radical scavenging activities and reducing power presented their highest values (1193.72 mg AAE/g, 728.73 mg AAE/g, and 0.65, respectively) at 300 °C/100 bar. The tyrosinase inhibitory activity of SCW-treated rutin was 21.72-60.05% at 1 mg/mL. The ethyl acetate fraction showed 14.91% melanin inhibitory activity at a concentration of 10 µg/mL compared to the α-MSH treatment group. The protein expression inhibition rates of MITF, tyrosinase, TRP-1, and TRP-2 in the ethyl acetate fractions were 14.05%, 72%, 93.05%, and 53.44%, respectively, at a concentration of 10 µg/mL, compared to the control. These results indicate that SCW treatment could be used to develop cosmetic materials and functional food with physiological activity, and that SCW-treated rutin can be used as a skin-whitening cosmetic material.


Assuntos
Antioxidantes , Monofenol Mono-Oxigenase , Antioxidantes/química , Melaninas/metabolismo , Extratos Vegetais/química , Rutina/farmacologia , Água
7.
Molecules ; 27(17)2022 Aug 29.
Artigo em Inglês | MEDLINE | ID: mdl-36080324

RESUMO

We synthesized a series of quinazolinone derivates as tyrosinase inhibitors and evaluated their inhibition constants. We synthesized 2-(2,6-dimethylhepta-1,5-dien-1-yl)quinazolin-4(3H)-one (Q1) from the natural citral. The concentration, which led to 50% activity loss of Q1, was 103 ± 2 µM (IC50 = 103 ± 2 µM). Furthermore, we considered Q1 to be a mixed-type and reversible tyrosinase inhibitor, and determined the KI and KIS inhibition constants to be 117.07 µM and 423.63 µM, respectively. Our fluorescence experiment revealed that Q1 could interact with the substrates of tyrosine and L-DOPA in addition to tyrosinase. Molecular docking studies showed that the binding of Q1 to tyrosinase was driven by hydrogen bonding and hydrophobicity. Briefly, the current study confirmed a new tyrosinase inhibitor, which is expected to be developed into a novel pigmentation drug.


Assuntos
Agaricales , Monofenol Mono-Oxigenase , Agaricales/metabolismo , Inibidores Enzimáticos/química , Cinética , Simulação de Acoplamento Molecular , Quinazolinonas/farmacologia , Relação Estrutura-Atividade
8.
Molecules ; 27(17)2022 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-36080359

RESUMO

Green tea extract derived from the leaves of Camellia sinensis L. (CS), is a representative beverage with antioxidant, anti-cancer, and anti-viral properties. CS extract is also used in cosmetics. Colloidal gold is generally a sol or colloidal suspension of gold nanoparticles in water. Colloidal gold green tea (CGCS), cultivated as a fertilizer using this colloidal gold solution, contains gold minerals and possesses anti-inflammatory, analgesic, and anti-tumor properties. However, the skin bioactivity of CGCS has not yet been investigated. In this study, we investigated the effect of the CGCS extract on skin whitening. CGCS extract contained high levels of phenols and flavonoids and displayed 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity in a concentration-dependent manner. CGCS extract inhibited melanin synthesis and tyrosinase activity in B16F10 cells more effectively than the CS extract. Moreover, the CGCS extract decreased the expression levels of the melanogenesis-related proteins, tyrosinase, tyrosinase-related proteins (TRPs), and microphthalmia-associated transcription factor (MITF). In conclusion, our study showed that the CGCS extract inhibits the expression of tyrosinase, TRP-1, and TRP-2 via the downregulation of MITF, thereby inhibiting melanin synthesis. Therefore, CGCS can potentially be used as a skin-whitening ingredient in the cosmetic industry.


Assuntos
Camellia sinensis , Melanoma Experimental , Nanopartículas Metálicas , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Camellia sinensis/metabolismo , Linhagem Celular Tumoral , Ouro/farmacologia , Coloide de Ouro , Melaninas , Melanoma Experimental/metabolismo , Monofenol Mono-Oxigenase , Extratos Vegetais/farmacologia , Chá
9.
Molecules ; 27(17)2022 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-36080469

RESUMO

The enzyme tyrosinase plays a key role in the early stages of melanin biosynthesis. This study evaluated the inhibitory activity of anthocyanidin (1) and anthocyanins (2-6) on the catalytic reaction. Of the six derivatives examined, 1-3 showed inhibitory activity with IC50 values of 3.7 ± 0.1, 10.3 ± 1.0, and 41.3 ± 3.2 µM, respectively. Based on enzyme kinetics, 1-3 were confirmed to be competitive inhibitors with Ki values of 2.8, 9.0, and 51.9 µM, respectively. Molecular docking analysis revealed the formation of a binary encounter complex between 1-3 and the tyrosinase catalytic site. Luteolinidin (1) and petunidin 3-O-glucoside (2) may serve as tyrosinase inhibitors to block melanin production.


Assuntos
Agaricales , Monofenol Mono-Oxigenase , Antocianinas/farmacologia , Inibidores Enzimáticos/farmacologia , Glucosídeos/farmacologia , Cinética , Melaninas , Simulação de Acoplamento Molecular , Estrutura Molecular
10.
J Oleo Sci ; 71(9): 1403-1412, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36047244

RESUMO

Clove, a dried flower buds of Syzygium aromaticum, is used in traditional medicine, for culinary purposes, and in essential oil production. In our preliminary screening of crude drugs used in Japanese Kampo formulas, a methanol (MeOH) extract of clove buds was found to exhibit a melanin induction. To date, the effects of clove buds or their constituents on the activation of melanogenesis remain unclear. Thus, this study aimed to isolate active compounds from the MeOH extract of clove buds associated with melanin synthesis in melanoma cells and to investigate the molecular mechanism involved. The MeOH extract of clove buds increased melanin content in murine B16-F1 melanoma cells. To identify the active compounds responsible for melanin induction, the MeOH extract was suspended in water and successively partitioned using hexane, ethyl acetate (EtOAc), and n-butanol (n-BuOH). Comparative analysis revealed that the EtOAc fraction induced melanin synthesis. Bioassay-guided separation of the EtOAc fraction isolated three compounds including eugenol. The analysis of structure-activity relationships of eugenol and structurally related compounds indicated that eugenol was the most potent melanin inducer among the 11 compounds, and that a hydroxyl group at C-1 and a methoxy group at C-2 may contribute to melanin induction. Eugenol induced melanin synthesis in human HMV-II melanoma cells as well as in B16-F1 cells. Further analysis indicated that eugenol may invoke intracellular tyrosinase activity and expression of tyrosinase, tyrosinaserelated protein (TRP)-1, TRP-2, and microphthalmia-associated transcription factor (MITF). These results suggest that eugenol enhances melanin synthesis by upregulating the expression of MITF and subsequent expression of melanogenic enzymes, and that it may be a potent therapeutic agent for hypopigmentation.


Assuntos
Melanoma Experimental , Syzygium , Animais , Bioensaio , Eugenol/farmacologia , Eugenol/uso terapêutico , Humanos , Melaninas , Melanoma Experimental/metabolismo , Metanol , Camundongos , Monofenol Mono-Oxigenase/metabolismo , Extratos Vegetais/farmacologia , Syzygium/metabolismo
11.
Bull Exp Biol Med ; 173(4): 441-443, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-36058980

RESUMO

We studied the growth dynamics of Walker 256 carcinosarcoma in recombinant progeny of dihybrid crosses of Brattleboro and WAG rats. A mutation in the vasopressin gene determining hypothalamic diabetes insipidus was detected in Brattleboro rats. WAG rats are carriers of normal vasopressin gene. Another interlinear difference was linked to tyrosinase gene controlling melanin synthesis. WAG rats express mutant allele determining albino phenotype. Brattleboro rats had normal working tyrosinase gene. F2 segregation yielded phenotypic classes with two patterns of tumor growth: linear growth or regression. Tumors regression was not linked to tyrosinase activity and was observed only in rats with diabetes insipidus. Analysis of mutants in next generations F3 and F4 confirmed this regularity in the Walker 256 carcinosarcoma growth pattern.


Assuntos
Carcinoma 256 de Walker , Carcinossarcoma , Diabetes Insípido , Diabetes Mellitus , Animais , Carcinoma 256 de Walker/genética , Diabetes Insípido/genética , Melaninas , Monofenol Mono-Oxigenase , Ratos , Ratos Brattleboro , Vasopressinas
12.
Anal Chem ; 94(37): 12715-12722, 2022 Sep 20.
Artigo em Inglês | MEDLINE | ID: mdl-36076186

RESUMO

Inspired by the interpretation of two-dimensional (2D) nuclear magnetic resonance spectra, an efficient strategy was proposed for pinpointing bioactive components from complex natural products. An off-line comprehensive countercurrent chromatography (CCC) × high-performance liquid chromatography (HPLC) was employed to achieve a 2D chemical chromatogram, and 2D bioassay profilings were obtained from bioassays of the eluent of the first dimension (1D) CCC and the eluent of the second dimension (2D) HPLC. Then 2D chemical chromatograms and 2D bioassay profilings were matched for pinpointing bioactive natural components from complex matrices. Thus, bioactive components in a complex matrix could be efficiently analyzed, separated, and bioactivity-determined. This experimental scheme was successfully demonstrated with a traditional medicinal herb Polygonum cuspidatum Sieb. et Zucc. The feasibility of this 2D strategy was verified with tyrosinase inhibition assay, α-glucosidase inhibition assay, DPPH radical scavenging assay, and ABTS•+ decolorization assay. Eight natural inhibitors were successfully pinpointed and identified from P. cuspidatum. Both pieceid-2″-O-gallate (10) and vanicoside B (20) were screened and identified as natural tyrosinase inhibitors for the first time. Meanwhile, vanicoside B (20) was also found as the strongest α-glucosidase inhibitor among all the isolated components. Most of the compounds exhibited much higher radical scavenging activities. Compared with traditional methodology based on one-dimensional chromatographic separation, the present 2D strategy would be more precise, efficient, and convenient to screen and separate bioactive compounds from complex matrices.


Assuntos
Distribuição Contracorrente , Monofenol Mono-Oxigenase , Bioensaio , Cromatografia Líquida de Alta Pressão/métodos , Cinamatos , Distribuição Contracorrente/métodos , Inibidores de Glicosídeo Hidrolases , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Glucosidases
13.
J Am Chem Soc ; 144(37): 16720-16725, 2022 Sep 21.
Artigo em Inglês | MEDLINE | ID: mdl-36094431

RESUMO

Melanin is an organic material biosynthesized from tyrosine in pigment-producing cells. The present study reports a simple method to generate tailored functional materials in mammalian cells by chemically fabricating intracellular melanin. Our approach exploits synthetic tyrosine derivatives to hijack the melanin biosynthesis pathway in pigment-producing cells. Its application was exemplified by synthesizing and using a paramagnetic tyrosine derivative, m-YR, which endowed melanoma cells with responsiveness to external magnetic fields. The mechanical force generated by the magnet-responsive melanin forced the cells to elongate and align parallel to the magnetic power lines. Critically, even non-pigment cells were similarly remote-controlled by external magnetic fields once engineered to express tyrosinase and treated with m-YR, suggesting the versatility of the approach. The present methodology may potentially provide a new avenue for mechanobiology and magnetogenetic studies and a framework for magnetic control of specific cells.


Assuntos
Melaninas , Monofenol Mono-Oxigenase , Animais , Fenômenos Magnéticos , Mamíferos/metabolismo , Melaninas/metabolismo , Monofenol Mono-Oxigenase/metabolismo , Tirosina/metabolismo
14.
Fish Shellfish Immunol ; 129: 145-151, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36055556

RESUMO

Cadmium (Cd2+) and copper (Cu2+) are considered immunotoxic metals and their presence in combination in the aquatic environment may cause effects on shrimp species as Litopenaeus vannamei. Thus, this research evaluates the combined effects of Cd2+ and Cu2+ on shrimp inoculated with Vibrio harveyi bacteria. The experiments were performed at 96-h of exposure to sublethal concentrations of both metals. No mortality was observed in organisms exposed to the sum of Criterion of Continuous Concentration (ΣCCC) in Cd + Cu mixture and those inoculated with V. harveyi. Higher clotting times were recorded in Cd + Cu + V. harveyi treatment at higher metal concentrations. No significant differences (P > 0.05) were recorded in hemocyanin content between shrimp exposed to metals and those experimentally infected. Significantly higher (P < 0.05) total hemocyte count (THC) was recorded at 96 h exposure in the ΣCCC and 10% treatments of Cd + Cu + V. harveyi experiment. Regarding Cd + Cu + V. harveyi bioassay, the highest phenoloxidase (PO) activity was recorded in shrimp inoculated with V. harveyi (0.326 ± 0.031 PO units/mg protein) at 96-h exposure. The lowest PO activity was observed in organisms exposed to Cd + Cu + V. harveyi. Regarding superoxide dismutase (SOD) activity, shrimp exposed to higher metal concentrations at 96 h showed the lowest hemolymph activity (6.03 ± 0.62 SOD units/mL). Protein decrease was observed in organisms exposed to metal mixture. The results showed that L. vannamei could be more susceptible to V. harveyi when exposed to Cd + Cu.


Assuntos
Cádmio , Penaeidae , Animais , Cádmio/toxicidade , Cobre/toxicidade , Dronabinol/farmacologia , Hemocianinas/farmacologia , Monofenol Mono-Oxigenase , Superóxido Dismutase/farmacologia , Vibrio
15.
Molecules ; 27(17)2022 Aug 23.
Artigo em Inglês | MEDLINE | ID: mdl-36080131

RESUMO

Salvia is a potentially valuable aromatic herb that has been used since ancient times. The present work studied the chemical profile of three Salvia species essential oils (EO): S. officinalis, S. virgata and S. sclarea, as well as assessing their antioxidant and enzyme inhibitory activities. A total of 144 compounds were detected by GC-MS analysis, representing 91.1, 84.7 and 78.1% in S. officinalis, S. virgata and S. sclarea EOs, respectively. The major constituents were cis-thujone, 2,4-hexadienal and 9-octadecenoic acid, respectively. The principal component analysis (PCA) score plot revealed significant discrimination between the three species. The antioxidant activity of the EOs was evaluated using in vitro assays. Only S. virgata EO showed antioxidant activity in the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assay (26.6 ± 1.60 mg Trolox equivalent (TE)/g oil). Moreover, this oil exhibited the highest antioxidant activity in 2,2-azino bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cupric-reducing antioxidant capacity (CUPRAC) and ferric-reducing power (FRAP) assays in comparison with the other two EOs (190.1 ± 2.04 vs. 275.2 ± 8.50 and 155.9 ± 1.33 mg TE/g oil, respectively). However, S. virgata oil did not show any effect in the chelating ability assay, while in the PBD assay, S. officinalis had the best antioxidant activity (26.4 ± 0.16 mmol TE/g oil). Enzyme inhibitory effect of the EOs was assessed against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), tyrosinase, α-glucosidase and α-amylase. AChE enzyme was more sensitive to S. officinalis EO (4.2 ± 0.01 mg galantamine equivalent (GALAE)/g oil), rather than S. virgata EO, which was ineffective. However, S. virgata had the highest BChE effect (12.1 ± 0.16 mg GALAE/g oil). All studied oils showed good tyrosinase inhibitory activity, ranging between 66.1 ± 0.61 and 128.4 ± 4.35 mg kojic acid equivalent (KAE)/g oil). Moreover, the EOs did not exhibit any glucosidase inhibition and were weak or inefficient on amylase enzyme. Partial least squares regression (PLS-R) models showed that there is an excellent correlation between the antioxidant activity and the volatile profile when being compared to that of enzyme inhibitory activity. Thus, the studied Salvia essential oils are interesting candidates that could be used in drug discovery for the management of Alzheimer's and hyperpigmentation conditions.


Assuntos
Óleos Voláteis , Salvia , Acetilcolinesterase , Antioxidantes/química , Antioxidantes/farmacologia , Butirilcolinesterase , Cromatografia Gasosa-Espectrometria de Massas , Monofenol Mono-Oxigenase , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Extratos Vegetais/química , Salvia/química , Uzbequistão
16.
Fish Shellfish Immunol ; 129: 191-198, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36029945

RESUMO

Decitabine (DAC), an inhibitor of DNA methyltransferase, is typically used to reverse DNA methylation and is considered an epigenetic modifying drug. DNA methylation is crucial to the regulation of gene expression without altering genetic information. Our previous research showed that the DNA methylation levels of many immune-related genes changed after the pre-grafting condition in pearl production. In the present study, we evaluated the DNA methylation level and analyzed transcriptome, enzyme, and antimicrobial activities after DAC treatment to evaluate the effect of DAC on DNA methylation and immune system of pearl oyster Pinctada fucata martensii. Results showed that DAC significantly decreased the level of global DNA methylation in the hemocytes of the pearl oysters. Transcriptome analysis obtained 577 differentially expressed genes (DEGs) between the control and DAC treatment group. The DEGs were mainly enriched in the following pathways: "Relaxin signaling pathway," "Cytosolic DNA-sensing pathway," "Platelet activation," and "Peroxisome," and related genes were overexpressed after DAC treatment. DAC treatment resulted in a substantial increase in the levels of serum superoxide dismutase, interleukin-17, phenol oxidase, tumor necrosis factor, and antimicrobial activity, compared with the control. These results suggested that DAC can alter DNA methylation level, activate immune-related genes, and improve the level of humoral immunity in pearl oysters, thereby increasing our understanding of the mechanism underlying DNA methylation in immune regulation.


Assuntos
Anti-Infecciosos , Pinctada , Relaxina , Animais , Anti-Infecciosos/metabolismo , DNA/metabolismo , Decitabina/metabolismo , Imunidade Inata/genética , Interleucina-17/metabolismo , Metiltransferases/metabolismo , Monofenol Mono-Oxigenase/metabolismo , Relaxina/metabolismo , Superóxido Dismutase/metabolismo , Fatores de Necrose Tumoral/metabolismo
17.
Chem Biodivers ; 19(9): e202200272, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35938449

RESUMO

This study aimed to investigate the chemical composition of essential oils isolated from Acca sellowiana (feijoa) leaves and stems and elaborate on their relevance as natural anti-aging, coupled with molecular-docking studies. The isolated oils were analysed using gas chromatography-mass spectrometry analysis and investigated for inhibitory effects against acetylcholinesterase, ß-secretase, collagenase, elastase and tyrosinase. Molecular-modelling study was performed using MOE-Dock program to evaluate binding interactions of major components with the above-mentioned targets. The leaf oil revealed the predominance of caryophyllene oxide (24.3 %), linalool (7.9 %), and spathulenol (6.6 %), while the stem oil was presented by caryophyllene oxide (38.1 %), α-zingiberene (10.1 %) and humulene oxide II (6.0 %). The stem oil expressed superior inhibitory activities against acetylcholinesterase (IC50 =0.15±0.01 µg/mL), ß-secretase (IC50 =3.99±0.23 µg/mL), collagenase (IC50 =408.10±20.80 µg/mL), elastase (IC50 =0.17±0.01 µg/mL) and tyrosinase (IC50 =8.45±0.40 µg/mL). The valuable binding interactions and docking scores were observed for caryophyllene oxide and α-zingiberene with acetylcholinesterase. Besides, α-zingibirene followed by linalool and τ-cadinol revealed tight fitting with collagenase and elastase. Additionally, linalool, spathulenol and τ-cadinol showed the best binding energy to tyrosinase. This study provides valuable scientific data on A. sellowiana as potential candidates for the development of natural antiaging formulations. The current study provided scientific evidence for the potential use of feijoa essential oils in antiaging formulations and as an adjuvant for the prophylaxis against Alzheimer disease.


Assuntos
Feijoa , Óleos Voláteis , Acetilcolinesterase , Monoterpenos Acíclicos , Secretases da Proteína Precursora do Amiloide , Feijoa/química , Simulação de Acoplamento Molecular , Sesquiterpenos Monocíclicos , Monofenol Mono-Oxigenase/análise , Óleos Voláteis/química , Óxidos , Elastase Pancreática/análise , Folhas de Planta/química , Sesquiterpenos Policíclicos , Sesquiterpenos , Terpenos
18.
Fish Shellfish Immunol ; 128: 307-315, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35940541

RESUMO

This study investigated the effects of two probiotics, namely Lactobacillus paracasei and Bifidobacterium longum, as feed additives on growth performance, nonspecific immunity, immune-related gene expression, and disease resistance against Vibrio parahaemolyticus in Penaeus vannamei. The experimental diets were prepared using L. paracasei and B. longum at concentrations of 105 and 107 CFU/g; these diets were referred to as P5, P7, B5, and B7. After 8 weeks of the diets, regarding growth performance, the B7 group showed the highest weight gain rate (890.34 ± 103.65%), special growth rate (4.08 ± 0.19%), and feed conversion rate (1.52 ± 0.19%) compared with the other groups. Moreover, the total hemocyte counts were significantly increased (p < 0.05) in the P7 groups on day 14 during the 28-day feeding trial. The phagocytosis rate in all experimental groups was increased on day 14 and was persistently significantly activated to day 21, especially in the P7 and B5 group. The phagocytic index of the P7 group showed a significant increase on day 14 and persistent activation to day 21. In the analysis of respiratory burst activity and phenoloxidase activity, the P7 and B5 groups showed a significant increase on day 7 and persistent activation to day 21. The expression level of the immune-related genes of superoxide dismutase, clotting protein, Penaeidin2, Penaeidin3, Penaeidin4, anti-LPS factor, crustin, and lysozyme was significantly increased in the experimental groups, especially in the P7 group. Furthermore, the optimum conditions of feed additives were determined in challenge trials conducted using P7 and B5. Shrimps fed P7 and B5 showed an increased survival rate (72.73% and 66.67%) after the V. parahaemolyticus challenge. In sum, the results revealed that B. longum, as a feed additive at 107 CFU/g, enhanced growth performance. L. paracasei at 107 CFU/g and B. longum at 105 CFU/g can enhance nonspecific immune responses and immune-related gene expression, and 107 CFU/g L. paracasei has the highest resistance ability for V. parahaemolyticus. Thus, dietary supplementation with L. paracasei and B. longum may be a valuable approach in white shrimp aquaculture.


Assuntos
Bifidobacterium longum , Lactobacillus paracasei , Penaeidae , Vibrio parahaemolyticus , Ração Animal/análise , Animais , Bifidobacterium longum/metabolismo , Dieta/veterinária , Imunidade Inata , Lactobacillus paracasei/metabolismo , Monofenol Mono-Oxigenase , Muramidase/farmacologia , Superóxido Dismutase/metabolismo , Vibrio parahaemolyticus/fisiologia
19.
Chem Biodivers ; 19(9): e202200399, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35977918

RESUMO

Some bioactive derivatives of indeno[1,2-c]pyrazolones were synthesized through the reaction of phenylhydrazine, different aldehydes and indan-1,2,3-trione at room temperature in acetonitrile. Analytical and spectroscopic studies have confirmed the structural characteristics of the synthesized compounds. In addition, the target compounds were screened for the in-vitro antiproliferative properties against the B16F10 melanoma cancer cell lines by the standard MTT assay. The effect on inflammatory marker cyclooxygenase 2 and matrix metalloproteinase 2, 9 was also checked to determine the anti-inflammatory and anti-cell migratory properties of these compounds. The final compounds were also tested for their tyrosinase inhibitory activity. Among all compounds, screened for anticancer activity, three compounds 4e, 4f and 4h reduced the cell proliferation significantly comparable to that of the positive standard drug erlotinib (IC50 =418.9±1.54 µM) with IC50 values ranging from 20.72-29.35 µM. The compounds 4c-4h decreased the COX-2 expression whereas the MMP 2, 9 expressions were significantly reduced by 4a, 4b and 4h. This was confirmed by molecular docking studies, as 4e, 4f and 4h displayed good interactions with the active site of BRAF protein. The compounds 4b, 4f and 4h exhibited moderate tyrosinase inhibition effect as compared to α-MSH. Collectively, compound 4h can be considered as a candidate for further optimization in the development of anticancer therapies based on the results of biological investigations in this study.


Assuntos
Antineoplásicos , Pirazolonas , Acetonitrilas/farmacologia , Aldeídos/farmacologia , Anti-Inflamatórios/farmacologia , Antineoplásicos/química , Proliferação de Células , Ciclo-Oxigenase 2/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Cloridrato de Erlotinib/farmacologia , Indanos/farmacologia , Metaloproteinase 2 da Matriz/metabolismo , Metaloproteinase 2 da Matriz/farmacologia , Simulação de Acoplamento Molecular , Estrutura Molecular , Monofenol Mono-Oxigenase/metabolismo , Fenil-Hidrazinas/farmacologia , Proteínas Proto-Oncogênicas B-raf/metabolismo , Proteínas Proto-Oncogênicas B-raf/farmacologia , Pirazolonas/farmacologia , Relação Estrutura-Atividade , alfa-MSH/farmacologia
20.
Chem Biodivers ; 19(9): e202200282, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35983910

RESUMO

Blumea lacera (Burm. f.) DC. is attracting scientific interest due to the diverse biological activities of its various parts and its use in folk medicine. The present study was undertaken to investigate the tissue-specific differential expression pattern of its total bioactive compounds. The study was further extended to whole plant phenolics profiling, in vitro enzyme inhibition activities, followed by in silico enzyme inhibition analysis to assess its potential as herbal medicine. The amount of total phenolics in different tissues was followed in decreasing order as old leaf, flower bud, root, young leaf, flower, old stem, and young stem, while that for the flavonoids was old leaf, root, young leaf, flower bud, flower, young stem, and old stem. This study identified rosmarinic acid, quercetin, and kaempferol in this plant for the first time. The solvent extracts demonstrated strong inhibition of lipase and tyrosinase activity, along with varying degrees of inhibition of acetylcholinesterase and butyrylcholinesterase activity. Among the detected compounds, ten displayed strong in silico binding affinities with the tested enzymes. The findings provide a new insight into further investigation of the medicinal potential of this species against obesity, neurological disorders, and aberrant skin color.


Assuntos
Asteraceae , Polifenóis , Acetilcolinesterase/metabolismo , Antioxidantes/química , Antioxidantes/farmacologia , Asteraceae/metabolismo , Butirilcolinesterase , Flavonoides/química , Quempferóis/farmacologia , Lipase , Monofenol Mono-Oxigenase , Obesidade/tratamento farmacológico , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Quercetina/farmacologia , Solventes
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