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1.
Food Chem ; 366: 130633, 2022 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-34332421

RESUMO

The global market for imported, high-quality priced foods has grown dramatically in the last decade, as consumers become more conscious of food originating from around the world. Many countries require the origin label of food to protect consumers need about true characteristics and origin. Regulatory authorities are looking for an extended and updated list of the analytical techniques for verification of authentic oils and to support law implementation. This review aims to introduce the efforts made using various analytical tools in combination with the multivariate analysis for the verification of the geographical origin of oils. The popular analytical tools have been discussed, and scientometric assessment that underlines research trends in geographical authentication and preferred journals used for dissemination has been indicated. Overall, we believe this article will be a good guideline for food industries and food quality control authority to assist in the selection of appropriate methods to authenticate oils.


Assuntos
Alimentos , Óleos Vegetais , Qualidade dos Alimentos , Geografia , Análise Multivariada
2.
Molecules ; 26(16)2021 Aug 06.
Artigo em Inglês | MEDLINE | ID: mdl-34443352

RESUMO

Ruta L. is a typical genus of the citrus family, Rutaceae Juss. and comprises ca. 40 different species, mainly distributed in the Mediterranean region. Ruta species have long been used in traditional medicines as an abortifacient and emmenagogue and for the treatment of lung diseases and microbial infections. The genus Ruta is rich in essential oils, which predominantly contain aliphatic ketones, e.g., 2-undecanone and 2-nonanone, but lack any significant amounts of terpenes. Three Ruta species, Ruta chalepensis L., Ruta graveolens L., and Ruta montana L., have been extensively studied for the composition of their essential oils and several bioactivities, revealing their potential medicinal and agrochemical applications. This review provides a systematic evaluation and critical appraisal of publications available in the literature on the composition and bioactivities of the essential oils obtained from Ruta species and includes a brief outlook of the potential applications of nanotechnology and chitosan-based products of Ruta essential oils.


Assuntos
Óleos Voláteis/química , Óleos Voláteis/farmacologia , Ruta/química , Animais , Humanos , Nanomedicina
3.
Food Res Int ; 147: 110522, 2021 09.
Artigo em Inglês | MEDLINE | ID: mdl-34399500

RESUMO

Cancer has been listed as one of the world's five incurable diseases by the World Health Organization and causes tens of thousands of deaths every year. Unfortunately, anticancer agents either show limited efficacy or show serious side effects. The algae possess high nutritional value and their polysaccharides have a variety of biological activities, especially anti-cancer and immunomodulatory properties. Algal polysaccharides exert anti-cancer effects by inducing apoptosis, cell cycle arrest, anti-angiogenesis, and regulating intestinal flora and immune function. Algal polysaccharides can be combined with nanoparticles and other drugs to reduce the side effects caused by chemotherapy and increase the anticancer effects. This review shows the signal pathways related to the anti-cancer mechanisms of algal polysaccharides, including their influence on intestinal flora and immune regulation, the application of nanoparticles, and the effects on combination therapy and clinical trials of cancer treatments.


Assuntos
Antineoplásicos , Microbioma Gastrointestinal , Neoplasias , Suplementos Nutricionais , Humanos , Neoplasias/tratamento farmacológico , Polissacarídeos
4.
Metabolites ; 11(8)2021 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-34436430

RESUMO

The discovery and identification of novel natural products of medicinal importance in the herbal medicine industry becomes a challenge. The complexity of this process can be reduced by dereplication strategies. The current study includes a method based on high-performance liquid chromatography (HPLC), using the evaporative light scattering detector (ELSD) to identify the 12 most common secondary metabolites in plant extracts. Twelve compounds including rutin, taxifolin, quercetin, apigenin, kaempferol, betulinic acid, oleanolic acid, betulin, lupeol, stigmasterol, and ß-sitosterol were analyzed simultaneously. The polarity of the compounds varied greatly from highly polar (flavonoids) to non-polar (triterpenes and sterols). This method was also tested for HPLC-DAD and HPLC-ESI-MS/MS analysis. Oleanolic acid and ursolic acid could not be separated in HPLC-ELSD analysis but were differentiated using LC-ESI-MS/MS analysis due to different fragment ions. The regression values (R2 > 0.996) showed good linearity in the range of 50-1000 µg/mL for all compounds. The range of LOD and LOQ values were 7.76-38.30 µg/mL and 23.52-116.06 µg/mL, respectively. %RSD and % trueness values of inter and intraday studies were mostly <10%. This method was applied on 10 species of medicinal plants. The dereplication strategy has the potential to facilitate and shorten the identification process of common secondary metabolites in complex plant extracts.

5.
Mar Drugs ; 19(8)2021 Jul 22.
Artigo em Inglês | MEDLINE | ID: mdl-34436245

RESUMO

SARS-CoV-2 (severe acute respiratory syndrome coronavirus-2) is a novel coronavirus strain that emerged at the end of 2019, causing millions of deaths so far. Despite enormous efforts being made through various drug discovery campaigns, there is still a desperate need for treatments with high efficacy and selectivity. Recently, marine sulfated polysaccharides (MSPs) have earned significant attention and are widely examined against many viral infections. This article attempted to produce a comprehensive report about MSPs from different marine sources alongside their antiviral effects against various viral species covering the last 25 years of research articles. Additionally, these reported MSPs were subjected to molecular docking and dynamic simulation experiments to ascertain potential interactions with both the receptor-binding domain (RBD) of SARS CoV-2's spike protein (S-protein) and human angiotensin-converting enzyme-2 (ACE2). The possible binding sites on both S-protein's RBD and ACE2 were determined based on how they bind to heparin, which has been reported to exhibit significant antiviral activity against SARS CoV-2 through binding to RBD, preventing the virus from affecting ACE2. Moreover, our modeling results illustrate that heparin can also bind to and block ACE2, acting as a competitor and protective agent against SARS CoV-2 infection. Nine of the investigated MSPs candidates exhibited promising results, taking into consideration the newly emerged SARS CoV-2 variants, of which five were not previously reported to exert antiviral activity against SARS CoV-2, including sulfated galactofucan (1), sulfated polymannuroguluronate (SPMG) (2), sulfated mannan (3), sulfated heterorhamnan (8), and chondroitin sulfate E (CS-E) (9). These results shed light on the importance of sulfated polysaccharides as potential SARS-CoV-2 inhibitors.


Assuntos
Antivirais/farmacologia , Organismos Aquáticos/química , Polissacarídeos/farmacologia , SARS-CoV-2/química , Enzima de Conversão de Angiotensina 2/química , Enzima de Conversão de Angiotensina 2/metabolismo , Antivirais/química , Sítios de Ligação , Simulação por Computador , Heparina/química , Heparina/metabolismo , Humanos , Simulação de Acoplamento Molecular , Polissacarídeos/química , Ligação Proteica , SARS-CoV-2/genética , SARS-CoV-2/metabolismo , Glicoproteína da Espícula de Coronavírus/antagonistas & inibidores , Glicoproteína da Espícula de Coronavírus/química , Glicoproteína da Espícula de Coronavírus/metabolismo , Relação Estrutura-Atividade , Sulfatos/química
6.
Mar Drugs ; 19(7)2021 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-34356816

RESUMO

The coronavirus pandemic has affected more than 150 million people, while over 3.25 million people have died from the coronavirus disease 2019 (COVID-19). As there are no established therapies for COVID-19 treatment, drugs that inhibit viral replication are a promising target; specifically, the main protease (Mpro) that process CoV-encoded polyproteins serves as an Achilles heel for assembly of replication-transcription machinery as well as down-stream viral replication. In the search for potential antiviral drugs that target Mpro, a series of cembranoid diterpenes from the biologically active soft-coral genus Sarcophyton have been examined as SARS-CoV-2 Mpro inhibitors. Over 360 metabolites from the genus were screened using molecular docking calculations. Promising diterpenes were further characterized by molecular dynamics (MD) simulations based on molecular mechanics-generalized Born surface area (MM-GBSA) binding energy calculations. According to in silico calculations, five cembranoid diterpenes manifested adequate binding affinities as Mpro inhibitors with ΔGbinding < -33.0 kcal/mol. Binding energy and structural analyses of the most potent Sarcophyton inhibitor, bislatumlide A (340), was compared to darunavir, an HIV protease inhibitor that has been recently subjected to clinical-trial as an anti-COVID-19 drug. In silico analysis indicates that 340 has a higher binding affinity against Mpro than darunavir with ΔGbinding values of -43.8 and -34.8 kcal/mol, respectively throughout 100 ns MD simulations. Drug-likeness calculations revealed robust bioavailability and protein-protein interactions were identified for 340; biochemical signaling genes included ACE, MAPK14 and ESR1 as identified based on a STRING database. Pathway enrichment analysis combined with reactome mining revealed that 340 has the capability to re-modulate the p38 MAPK pathway hijacked by SARS-CoV-2 and antagonize injurious effects. These findings justify further in vivo and in vitro testing of 340 as an antiviral agent against SARS-CoV-2.


Assuntos
Antozoários/química , COVID-19/tratamento farmacológico , Proteases 3C de Coronavírus/antagonistas & inibidores , Inibidores de Protease de Coronavírus/farmacologia , Diterpenos/farmacologia , SARS-CoV-2/efeitos dos fármacos , Animais , COVID-19/virologia , Proteases 3C de Coronavírus/metabolismo , Inibidores de Protease de Coronavírus/química , Inibidores de Protease de Coronavírus/isolamento & purificação , Diterpenos/química , Diterpenos/isolamento & purificação , Humanos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Estrutura Molecular , SARS-CoV-2/enzimologia , SARS-CoV-2/patogenicidade , Relação Estrutura-Atividade
7.
Phytomedicine ; 91: 153676, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34339943

RESUMO

BACKGROUND: Despite advances in research on neurodegenerative diseases, the pathogenesis and treatment response of neurodegenerative diseases remain unclear. Recent studies revealed a significant role of carotenoids to treat neurodegenerative diseases. The aim of this study was to systematically review the neuroprotective potential of carotenoids in vivo and in vitro and the molecular mechanisms and pathological factors contributing to major neurodegenerative diseases (Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, and stroke). HYPOTHESIS: Carotenoids as therapeutic molecules to target neurodegenerative diseases. RESULTS: Aggregation of toxic proteins, mitochondrial dysfunction, oxidative stress, the excitotoxic pathway, and neuroinflammation were the major pathological factors contributing to the progression of neurodegenerative diseases. Furthermore, in vitro and in vivo studies supported the beneficiary role of carotenoids, namely lycopene, ß-carotene, crocin, crocetin, lutein, fucoxanthin and astaxanthin in alleviating disease progression. These carotenoids provide neuroprotection by inhibition of neuro-inflammation, microglial activation, excitotoxic pathway, modulation of autophagy, attenuation of oxidative damage and activation of defensive antioxidant enzymes. Additionally, studies conducted on humans also demonstrated that dietary intake of carotenoids lowers the risk of neurodegenerative diseases. CONCLUSION: Carotenoids may be used as drugs to prevent and treat neurodegenerative diseases. Although, the in vitro and in vivo results are encouraging, further well conducted clinical studies on humans are required to conclude about the full potential of neurodegenerative diseases.


Assuntos
Carotenoides , Doenças Neurodegenerativas , Fármacos Neuroprotetores , Antioxidantes , Carotenoides/farmacologia , Humanos , Doenças Neurodegenerativas/tratamento farmacológico , Neuroproteção , Fármacos Neuroprotetores/farmacologia , Estresse Oxidativo
8.
Sci Rep ; 11(1): 14716, 2021 07 19.
Artigo em Inglês | MEDLINE | ID: mdl-34282219

RESUMO

Imidacloprid (Imid), a systemic neonicotinoid insecticide, is broadly used worldwide. It is reported to contaminate aquatic systems. This study was proposed to evaluate oxidative stress and genotoxicity of Imid on Nile tilapia (Oreochromis niloticus) and the protective effect of ascorbic acid (Asc). O. niloticus juveniles (30.4 ± 9.3 g, 11.9 ± 1.3 cm) were divided into six groups (n = 10/replicate). For 21 days, two groups were exposed to sub-lethal concentrations of Imid (8.75 ppm, 1/20 of 72 h-LC50 and 17.5 ppm, 1/10 of 72 h-LC50); other two groups were exposed to Asc (50 ppm) in combination with Imid (8.75 and 17.5 ppm); one group was exposed to Asc (50 ppm) in addition to a group of unexposed fish which served as controls. Oxidative stress was assessed in the liver where the level of enzymatic activities including superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPX) in addition to mRNA transcripts and, Lipid peroxidation (LPO) were evaluated. Moreover, mitotic index (MI) and comet assay were performed, in addition, the erythrocytic micronucleus (MN), and nuclear abnormalities (NA) were observed to assess genotoxicity in fish. Imid exposure induced significant (p ˂ 0.05) changes in the antioxidant profile of the juveniles' liver by increasing the activities and gene expression of SOD, CAT and GPX as well as elevating the levels of LPO. DNA strand breaks in gill cells, erythrocytes and hepatocytes along with erythrocytic MN and NA were also significantly elevated in Imid-exposed groups. MI showed a significant (p ˂ 0.05) decrease associated with Imid exposure. Asc administration induced a significant amelioration towards the Imid toxicity (8.75 and 17.5 ppm). A significant protective potency against the genotoxic effects of Imid was evidenced in Asc co-treated groups. Collectively, results highlight the importance of Asc as a protective agent against Imid-induced oxidative stress and genotoxicity in O. niloticus juveniles.

9.
Nutrients ; 13(6)2021 May 31.
Artigo em Inglês | MEDLINE | ID: mdl-34072636

RESUMO

Bee pollen is a combination of plant pollen and honeybee secretions and nectar. The Bible and ancient Egyptian texts are documented proof of its use in public health. It is considered a gold mine of nutrition due to its active components that have significant health and medicinal properties. Bee pollen contains bioactive compounds including proteins, amino acids, lipids, carbohydrates, minerals, vitamins, and polyphenols. The vital components of bee pollen enhance different bodily functions and offer protection against many diseases. It is generally marketed as a functional food with affordable and inexpensive prices with promising future industrial potentials. This review highlights the dietary properties of bee pollen and its influence on human health, and its applications in the food industry.


Assuntos
Abelhas , Alimento Funcional , Pólen , Própole , Animais , Antioxidantes/análise , Glicemia , Carboidratos/análise , Humanos , Síndrome Metabólica , Camundongos , Valor Nutritivo , Ratos
10.
Artigo em Inglês | MEDLINE | ID: mdl-34070448

RESUMO

The COVID-19 pandemic is a serious challenge for societies around the globe as entire populations have fallen victim to the infectious spread and have taken up social distancing. In many countries, people have had to self-isolate and to be confined to their homes for several weeks to months to prevent the spread of the virus. Social distancing measures have had both negative and positive impacts on various aspects of economies, lifestyles, education, transportation, food supply, health, social life, and mental wellbeing. On other hands, due to reduced population movements and the decline in human activities, gas emissions decreased and the ozone layer improved; this had a positive impact on Earth's weather and environment. Overall, the COVID-19 pandemic has negative effects on human activities and positive impacts on nature. This study discusses the impact of the COVID-19 pandemic on different life aspects including the economy, social life, health, education, and the environment.


Assuntos
COVID-19 , Pandemias , Humanos , Distanciamento Físico , SARS-CoV-2
11.
Toxins (Basel) ; 13(3)2021 03 12.
Artigo em Inglês | MEDLINE | ID: mdl-33809401

RESUMO

Wasps, members of the order Hymenoptera, are distributed in different parts of the world, including Brazil, Thailand, Japan, Korea, and Argentina. The lifestyles of the wasps are solitary and social. Social wasps use venom as a defensive measure to protect their colonies, whereas solitary wasps use their venom to capture prey. Chemically, wasp venom possesses a wide variety of enzymes, proteins, peptides, volatile compounds, and bioactive constituents, which include phospholipase A2, antigen 5, mastoparan, and decoralin. The bioactive constituents have anticancer, antimicrobial, and anti-inflammatory effects. However, the limited quantities of wasp venom and the scarcity of advanced strategies for the synthesis of wasp venom's bioactive compounds remain a challenge facing the effective usage of wasp venom. Solid-phase peptide synthesis is currently used to prepare wasp venom peptides and their analogs such as mastoparan, anoplin, decoralin, polybia-CP, and polydim-I. The goal of the current review is to highlight the medicinal value of the wasp venom compounds, as well as limitations and possibilities. Wasp venom could be a potential and novel natural source to develop innovative pharmaceuticals and new agents for drug discovery.


Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Proteínas de Insetos/farmacologia , Nanotecnologia , Venenos de Vespas/farmacologia , Animais , Anti-Infecciosos/síntese química , Anti-Inflamatórios/síntese química , Antineoplásicos/síntese química , Humanos , Proteínas de Insetos/síntese química , Venenos de Vespas/síntese química
12.
Biomolecules ; 11(3)2021 03 07.
Artigo em Inglês | MEDLINE | ID: mdl-33800000

RESUMO

Cancer is a major burden of disease globally. Each year, tens of millions of people are diagnosed with cancer worldwide, and more than half of the patients eventually die from it. Significant advances have been noticed in cancer treatment, but the mortality and incidence rates of cancers are still high. Thus, there is a growing research interest in developing more effective and less toxic cancer treatment approaches. Curcumin (CUR), the major active component of turmeric (Curcuma longa L.), has gained great research interest as an antioxidant, anticancer, and anti-inflammatory agent. This natural compound shows its anticancer effect through several pathways including interfering with multiple cellular mechanisms and inhibiting/inducing the generation of multiple cytokines, enzymes, or growth factors including IκB kinase ß (IκKß), tumor necrosis factor-alpha (TNF-α), signal transducer, and activator of transcription 3 (STAT3), cyclooxygenase II (COX-2), protein kinase D1 (PKD1), nuclear factor-kappa B (NF-κB), epidermal growth factor, and mitogen-activated protein kinase (MAPK). Interestingly, the anticancer activity of CUR has been limited primarily due to its poor water solubility, which can lead to low chemical stability, low oral bioavailability, and low cellular uptake. Delivering drugs at a controlled rate, slow delivery, and targeted delivery are other very attractive methods and have been pursued vigorously. Multiple CUR nanoformulations have also been developed so far to ameliorate solubility and bioavailability of CUR and to provide protection to CUR against hydrolysis inactivation. In this review, we have summarized the anticancer activity of CUR against several cancers, for example, gastrointestinal, head and neck, brain, pancreatic, colorectal, breast, and prostate cancers. In addition, we have also focused on the findings obtained from multiple experimental and clinical studies regarding the anticancer effect of CUR in animal models, human subjects, and cancer cell lines.


Assuntos
Antineoplásicos/uso terapêutico , Curcumina/uso terapêutico , Extratos Vegetais/uso terapêutico , Animais , Linhagem Celular Tumoral , Curcuma/química , Ciclo-Oxigenase 1/metabolismo , Sistemas de Liberação de Medicamentos/métodos , Humanos , NF-kappa B/metabolismo , Extratos Vegetais/química , Fator de Transcrição STAT3/metabolismo , Transdução de Sinais/efeitos dos fármacos , Canais de Cátion TRPP/metabolismo
13.
Molecules ; 26(7)2021 Apr 05.
Artigo em Inglês | MEDLINE | ID: mdl-33916461

RESUMO

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent for the COVID-19 pandemic, which generated more than 1.82 million deaths in 2020 alone, in addition to 83.8 million infections. Currently, there is no antiviral medication to treat COVID-19. In the search for drug leads, marine-derived metabolites are reported here as prospective SARS-CoV-2 inhibitors. Two hundred and twenty-seven terpene natural products isolated from the biodiverse Red-Sea ecosystem were screened for inhibitor activity against the SARS-CoV-2 main protease (Mpro) using molecular docking and molecular dynamics (MD) simulations combined with molecular mechanics/generalized Born surface area binding energy calculations. On the basis of in silico analyses, six terpenes demonstrated high potency as Mpro inhibitors with ΔGbinding ≤ -40.0 kcal/mol. The stability and binding affinity of the most potent metabolite, erylosides B, were compared to the human immunodeficiency virus protease inhibitor, lopinavir. Erylosides B showed greater binding affinity towards SARS-CoV-2 Mpro than lopinavir over 100 ns with ΔGbinding values of -51.9 vs. -33.6 kcal/mol, respectively. Protein-protein interactions indicate that erylosides B biochemical signaling shares gene components that mediate severe acute respiratory syndrome diseases, including the cytokine- and immune-signaling components BCL2L1, IL2, and PRKC. Pathway enrichment analysis and Boolean network modeling were performed towards a deep dissection and mining of the erylosides B target-function interactions. The current study identifies erylosides B as a promising anti-COVID-19 drug lead that warrants further in vitro and in vivo testing.


Assuntos
Invertebrados/química , SARS-CoV-2/metabolismo , Terpenos/química , Proteínas da Matriz Viral/antagonistas & inibidores , Animais , Sítios de Ligação , COVID-19/tratamento farmacológico , COVID-19/virologia , Humanos , Ligação de Hidrogênio , Invertebrados/metabolismo , Lopinavir/química , Lopinavir/metabolismo , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Inibidores de Proteases/química , Inibidores de Proteases/isolamento & purificação , Inibidores de Proteases/uso terapêutico , Ligação Proteica , SARS-CoV-2/isolamento & purificação , Terpenos/isolamento & purificação , Terpenos/metabolismo , Terpenos/uso terapêutico , Termodinâmica , Proteínas da Matriz Viral/metabolismo
14.
Molecules ; 26(7)2021 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-33916714

RESUMO

Centaurothamnus maximus (family Asteraceae), is a leafy shrub indigenous to the southwestern Arabian Peninsula. With a paucity of phytochemical data on this species, we set out to chemically characterize the plant. From the aerial parts, two newly identified guaianolides were isolated: 3ß-hydroxy-4α(acetoxy)-4ß(hydroxymethyl)-8α-(4-hydroxy methacrylate)-1αH,5αH, 6αH-gual-10(14),11(13)-dien-6,12-olide (1) and 15-descarboxy picrolide A (2). Seven previously reported compounds were also isolated: 3ß, 4α, 8α-trihydroxy-4-(hydroxymethyl)-lαH, 5αH, 6ßH, 7αH-guai-10(14),11(13)-dien-6,12-olide (3), chlorohyssopifolin B (4), cynaropikrin (5), hydroxyjanerin (6), chlorojanerin (7), isorhamnetin (8), and quercetagetin-3,6-dimethyl ether-4'-O-ß-d-pyranoglucoside (9). Chemical structures were elucidated using spectroscopic techniques, including High Resolution Fast Atom Bombardment Mass Spectrometry (HR-FAB-MS), 1D NMR; 1H, 13C NMR, Distortionless Enhancement by Polarization Transfer (DEPT), and 2D NMR (1H-1H COSY, HMQC, HMBC) analyses. In addition, a biosynthetic pathway for compounds 1-9 is proposed. The chemotaxonomic significance of the reported sesquiterpenoids and flavonoids considering reports from other Centaurea species is examined.


Assuntos
Asteraceae/química , Lactonas/isolamento & purificação , Sesquiterpenos de Guaiano/isolamento & purificação , Vias Biossintéticas , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Flavonas/química , Flavonas/isolamento & purificação , Lactonas/química , Conformação Molecular , Espectroscopia de Prótons por Ressonância Magnética , Sesquiterpenos de Guaiano/química
15.
Antibiotics (Basel) ; 10(3)2021 Mar 03.
Artigo em Inglês | MEDLINE | ID: mdl-33802470

RESUMO

The genus Centaurea is recognized in folk medicine for anti-inflammatory, anti-itch, antitussive, purgative, astringent, and tonic activities. To study the chemical determinant for antimicrobial activity essential oils (EOs), five Centaurea species were analyzed including: C. scoparia, C. calcitrapa, C. glomerata, C. lipii and C. alexandrina. Conventional hydro-distillation (HD) and microwave-assisted extraction (MAE), as new green technologies, were compared for the extraction of essential oils. GC/MS analysis identified 120 EOs including mostly terpenoid except from C. lipii and C. alexandrina in which nonterpenoids were the major constituents. Major terpenoids included spathulenol, caryophyllene oxide and alloaromadendrene oxide-2. To probe antibacterial activity, potential EO inhibitors of a bacterial type II DNA topoisomerase, DNA gyrase B were screened via an in silico molecular docking approach. Spathulenol and alloaromadendrene oxide-2 possessed the best binding affinity in the ATP- binding pocket of Gyrase B enzyme. Principal component analysis and agglomerative hierarchical clustering were used for sample classification and revealed that sesquiterpenes contributed the most for accessions classification. In vitro antimicrobial activity against Staphylococcus aureus, Escherichia coli and Aspergillus niger for all EOs were also evaluated. EOs from C. lipii, C. glomerata and C. calcitrapa exhibited significant MIC against S. aureus with an MIC value of 31.25 µg/mL.

16.
Mar Drugs ; 19(5)2021 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-33923369

RESUMO

Cyanobacteria are photosynthetic prokaryotic organisms which represent a significant source of novel, bioactive, secondary metabolites, and they are also considered an abundant source of bioactive compounds/drugs, such as dolastatin, cryptophycin 1, curacin toyocamycin, phytoalexin, cyanovirin-N and phycocyanin. Some of these compounds have displayed promising results in successful Phase I, II, III and IV clinical trials. Additionally, the cyanobacterial compounds applied to medical research have demonstrated an exciting future with great potential to be developed into new medicines. Most of these compounds have exhibited strong pharmacological activities, including neurotoxicity, cytotoxicity and antiviral activity against HCMV, HSV-1, HHV-6 and HIV-1, so these metabolites could be promising candidates for COVID-19 treatment. Therefore, the effective large-scale production of natural marine products through synthesis is important for resolving the existing issues associated with chemical isolation, including small yields, and may be necessary to better investigate their biological activities. Herein, we highlight the total synthesized and stereochemical determinations of the cyanobacterial bioactive compounds. Furthermore, this review primarily focuses on the biotechnological applications of cyanobacteria, including applications as cosmetics, food supplements, and the nanobiotechnological applications of cyanobacterial bioactive compounds in potential medicinal applications for various human diseases are discussed.


Assuntos
Antivirais/farmacologia , COVID-19/tratamento farmacológico , COVID-19/virologia , Cianobactérias/química , Cianobactérias/fisiologia , SARS-CoV-2 , Antivirais/química , Organismos Aquáticos , Humanos
17.
Biomolecules ; 11(3)2021 02 25.
Artigo em Inglês | MEDLINE | ID: mdl-33669097

RESUMO

Alzheimer's disease (AD) is a gradually growing irreversible illness of the brain that almost affects every fifth person (aged > 80 years) in the world. World Health Organization (WHO) also revealed that the prevalence of this disease will enhance (upto double) significantly upto 2030. The poor cholinergic transmission at the synapse is considered to be one of the main reasons behind the progression and occurrence of this disorder. Natural inhibitors of acetylcholine (ACh) such as galanthamine and rivastigmine are used commercially in the treatmentof AD. The biomolecules such assesquiterpenes, possess a great structural diversity and are responsible for a plethora of pharmacological properties. The potential of various sesquiterpenes as anticholinesterase has been reviewed in this article. For this purpose, the various databases, mainly PubMed, Scopus, and Web of Science were investigatedwith different keywords such as "sesquiterpenes+acetylcholinesterase" and "sesquiterpenes+cholinesterase+inhibitors" in the surveyed time frame (2010-2020). A vast literature was evident in the last decade, which affirms the potential of various sesquiterpenes in the improvement of cholinergic transmission by inhibiting the AChE. After data analysis, it was found that 12 compounds out of a total of 58 sesquiterpenes were reported to possess IC50 < 9µM and can be considered as potential candidates for the improvement of learning and memory. Sesquiterpene is an important category of terpenoids, found to possess a large spectrum of biological activities. The outcome of the review clearly states that sesquiterpenes (such as amberboin, lipidiol,etc) from herbs could offer fresh, functional compounds for possible prevention and treatment of AD.


Assuntos
Acetilcolinesterase/metabolismo , Doença de Alzheimer/tratamento farmacológico , Inibidores da Colinesterase/uso terapêutico , Sesquiterpenos/química , Sesquiterpenos/uso terapêutico , Animais , Galantamina/uso terapêutico , Humanos , Rivastigmina/uso terapêutico
18.
Food Chem ; 353: 129372, 2021 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-33725540

RESUMO

Matcha tea is rich in taste and bioactive constituents, quality evaluation of matcha tea is important to ensure flavor and efficacy. Near-infrared spectroscopy (NIR) in combination with variable selection algorithms was proposed as a fast and non-destructive method for the quality evaluation of matcha tea. Total polyphenols (TP), free amino acids (FAA), and polyphenols-to-amino acids ratio (TP/FAA) were assessed as the taste quality indicators. Successive projections algorithm (SPA), genetic algorithm (GA), and simulated annealing (SA) were subsequently developed from the synergy interval partial least squares (SiPLS). The overall results revealed that SiPLS-SPA and SiPLS-SA models combined with NIR exhibited higher predictive capabilities for the effective determination of TP, FAA and TP/FAA with correlation coefficient in the prediction set (Rp) of Rp > 0.97, Rp > 0.98 and Rp > 0.98 respectively. Therefore, this simple and efficient technique could be practically exploited for tea quality control assessment.


Assuntos
Aminoácidos/análise , Polifenóis/análise , Pós/química , Paladar , Chá/química , Algoritmos , Antioxidantes/análise , Análise dos Mínimos Quadrados , Espectroscopia de Luz Próxima ao Infravermelho/métodos
19.
Anal Methods ; 13(13): 1625-1634, 2021 04 07.
Artigo em Inglês | MEDLINE | ID: mdl-33735352

RESUMO

Perchlorate is a new type of persistent pollutant, which interferes with the synthesis and secretion of thyroxine and affects human health. The EU's limit for perchlorate in tea is 750 µg kg-1. The surface-enhanced Raman scattering (SERS) technique has the characteristics of a simple pretreatment method, rapid detection, high sensitivity, high specificity and great stability in the detection of perchlorate. This study proposed a novel superhydrophobic SERS substrate, which can be used to detect perchlorate in tea. Firstly, a chemical deposition method was used to deposit a silver film on the surface of a thin layer of polydimethylsiloxane. After drying, the substrate was immersed in 1H,1H,2H,2H-perfluorodecyltriethoxysilane aqueous solution for 15 hours to make the surface of the substrate superhydrophobic. Then cysteine molecules were deposited on the surface of the silver film/polydimethylsiloxane by incubation. The superhydrophobic surface has a unique enrichment effect on the highly diluted solution, and perchlorate has a strong affinity for the amino group of cysteine. We collected the Raman spectra of 9 gradient concentrations (1-100 µmol L-1) of perchlorate-spiked tea samples on the hydrophobic substrate, and a linear model of the relationship between the SERS spectral intensity and the concentrations of perchlorate in tea was established. This method reached a good limit of detection of 0.0067 µmol L-1 (0.82 µg kg-1) in tea, which showed that the developed sensor has high sensitivity and could be used as a fast and simple technique for quantitative detection of perchlorate based on SERS technology.


Assuntos
Cisteína , Prata , Dimetilpolisiloxanos , Humanos , Percloratos , Chá
20.
Molecules ; 26(5)2021 Feb 26.
Artigo em Inglês | MEDLINE | ID: mdl-33652837

RESUMO

In search of anti-inflammatory compounds, novel scaffolds containing isonicotinoyl motif were synthesized via an efficient strategy. The compounds were screened for their in vitro anti-inflammatory activity. Remarkably high activities were observed for isonicotinates 5-6 and 8a-8b. The compound 5 exhibits an exceptional IC50 value (1.42 ± 0.1 µg/mL) with 95.9% inhibition at 25 µg/mL, which is eight folds better than the standard drug ibuprofen (11.2 ± 1.9 µg/mL). To gain an insight into the mode of action of anti-inflammatory compounds, molecular docking studies were also performed. Decisively, further development and fine tuning of these isonicotinates based scaffolds for the treatment of various aberrations is still a wide-open field of research.


Assuntos
Anti-Inflamatórios não Esteroides/síntese química , Inflamação/tratamento farmacológico , Ácidos Isonicotínicos/síntese química , Espécies Reativas de Oxigênio/antagonistas & inibidores , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Inibidores de Ciclo-Oxigenase 2/síntese química , Inibidores de Ciclo-Oxigenase 2/química , Inibidores de Ciclo-Oxigenase 2/farmacologia , Humanos , Ibuprofeno/química , Ácidos Isonicotínicos/química , Ácidos Isonicotínicos/farmacologia , Simulação de Acoplamento Molecular , Espécies Reativas de Oxigênio/química , Relação Estrutura-Atividade
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