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1.
Bioorg Med Chem Lett ; 27(4): 875-879, 2017 02 15.
Artigo em Inglês | MEDLINE | ID: mdl-28094186

RESUMO

Nardonaphthalenones A and B (1-2), one new apo-α-carotenone (3) and four new monoterpenoids (4, 8-9 and 11), along with six known compounds (5-7, 10, 12-13) were isolated from the dried roots and rhizomes of Nardostachys chinensis Batal. Their structures were elucidated by analysis of the spectroscopic data including NMR, HRESIMS and circular dichroism data. Furthermore, the serotonin transporter (SERT)-regulating activities of these isolates were evaluated, among them compound 3 showed the strongest enhancement activity while compound 12 showed a moderate inhibition activity on SERT.


Assuntos
Monoterpenos/química , Naftalenos/química , Nardostachys/química , Expressão Gênica/efeitos dos fármacos , Células HEK293 , Humanos , Espectroscopia de Ressonância Magnética , Conformação Molecular , Monoterpenos/isolamento & purificação , Monoterpenos/farmacologia , Naftalenos/isolamento & purificação , Naftalenos/farmacologia , Nardostachys/metabolismo , Raízes de Plantas/química , Raízes de Plantas/metabolismo , Rizoma/química , Rizoma/metabolismo , Proteínas da Membrana Plasmática de Transporte de Serotonina/química , Proteínas da Membrana Plasmática de Transporte de Serotonina/genética , Proteínas da Membrana Plasmática de Transporte de Serotonina/metabolismo
2.
Yao Xue Xue Bao ; 51(1): 100-4, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27405169

RESUMO

A new caffeate compound, (E)-erythro-syringylglyceryl caffeate (1), was isolated from the roots and rhizomes of Nardostachys chinensis Batal., together with nine known phenolic compounds, including (+)-licarin A (2), naringenin 4', 7-dimethyl ether (3), pinoresinol-4-O-ß-D-glucoside (4), caraphenol A (5), Z-miyabenol C (6), protocatechuic acid (7), caffeic acid (8), gallic acid (9) and vanillic acid (10). Their chemical structures were elucidated on the basis of spectroscopic data and physicochemical properties. Furthermore, this is the first report of compounds 2, 5 and 6 from Nardostachys genus.


Assuntos
Ácidos Cafeicos/isolamento & purificação , Nardostachys/química , Ácidos Cafeicos/química , Flavanonas/química , Flavanonas/isolamento & purificação , Furanos/química , Furanos/isolamento & purificação , Glucosídeos/química , Glucosídeos/isolamento & purificação , Hidroxibenzoatos/química , Hidroxibenzoatos/isolamento & purificação , Lignanas/química , Lignanas/isolamento & purificação , Raízes de Plantas/química , Rizoma/química , Ácido Vanílico/química , Ácido Vanílico/isolamento & purificação
3.
Front Pharmacol ; 13: 1003469, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36339571

RESUMO

The coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), epidemic poses a major global public health threat with more than one million daily new infections and hundreds of deaths. To combat this global pandemic, efficient prevention and management strategies are urgently needed. Together with the main characteristics of COVID-19, impaired coagulation with dysfunctions of the immune response in COVID-19 pathophysiology causes high mortality and morbidity. From recent clinical observations, increased expression of specific types of estrogen appears to protect patients from SARS-CoV-2 infection, thereby, reducing mortality. COVID-19 severity is less common in women than in men, particularly in menopausal women. Furthermore, estrogen levels are negatively correlated with COVID-19 severity and mortality. These findings suggest that estrogen plays a protective role in the pathophysiology of COVID-19. In this review, we discuss the potential roles of estrogen in blocking the SARS-CoV-2 from invading alveolar cells and replicating, and summarize the potential mechanisms of anti-inflammation, immune modulation, reactive oxygen species resistance, anti-thrombosis, vascular dilation, and vascular endothelium protection. Finally, the potential therapeutic effects of estrogen against COVID-19 are reviewed. This review provides insights into the role of estrogen and its use as a potential strategy to reduce the mortality associated with COVID-19, and possibly other viral infections and discusses the possible challenges and pertinent questions.

4.
Int J Biol Macromol ; 133: 1201-1209, 2019 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-30986466

RESUMO

A previously unknown, water-soluble polysaccharide, named DOTP-B, was isolated from the roots of the plant Dioscorea opposita Thunb, a well-known edible and medicinal plant in China. DOTP-B was found to be neutral in charge, with an average molecular weight of 5623 Da. Monosaccharide composition analysis by GC-MS revealed that DOTP-B was a hetero-polysaccharide consisting of glucose and galactose at a molar ratio of 14.6:1.0. Structural features of DOTP-B were investigated with a combination of chemical and instrumental methods, including complete acid hydrolysis, periodate oxidation, methylation, GC-MS, FTIR and several NMR spectra. Highly correlated results demonstrated that the main chain of DOTP-B consisted of →4)-α-d-glc(1 → residues, with about 6% internal →6)-ß-d-gal(1 → residues. The antioxidant activity of DOTP-B was also evaluated as the EC50 values against DPPH and PTIO radicals were 2.1 ±â€¯0.1 mg/mL and 1.6 ±â€¯0.1 mg/mL, respectively. Therefore, the polysaccharide DOTP-B could be possibly developed as a promising natural antioxidant for application in medical and food industries.


Assuntos
Antioxidantes/química , Antioxidantes/isolamento & purificação , Dioscorea/química , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Água/química , Sequência de Carboidratos , Monossacarídeos/análise , Raízes de Plantas/química , Solubilidade
5.
Sichuan Da Xue Xue Bao Yi Xue Ban ; 39(3): 347-50, 2008 May.
Artigo em Chinês | MEDLINE | ID: mdl-18575312

RESUMO

OBJECTIVE: To construct the recombinant plasmid containing the outer membrane protein LipL32 gene of Leptospira strain 017 and to study on the cytotoxicity of the expression protein. METHODS: By the polymerase chain reaction (PCR), the LipL32 gene was amplified from Leptospira strain 017 genome and cloned into pET32a(+) with enzyme digestion, then used to transform E. coli JM109. After induced with IPTG, the target protein was expressed and used to immunize New zealand white rabbit. Western Blotting identified the immunogenicity of the expressed protein. Then the purified and renatured protein was acted on ECV304 cell so as to get its cytotoxicity detected by examining the LDH and NO (nitrogen monoxide) release from cell. RESULTS: The full length of the LipL32 gene about 816 bp was obtained by PCR. The recombinant plasmid was identified by enzyme digestion, PCR and DNA sequencing. After induced with IPTG, the expressed protein existed mainly in the form of inclusion bodies about 52 x 10(3) (relative molecular mass) which was consistent with the expected size of the fused protein. After rabbit immunity, the titre of the produced multiclonal antibody reached 1 : 32 000 measured by ELISA. Western Blotting analysis found a positive band specifically in the target protein position. The release of the LDH and NO of the ECV304 cell treated with LipL32 had significant increase compared with the control group. CONCLUSION: The recombinant plasmid containing LipL32 gene is successfully constructed and can express the target protein in E. coli JM109. The expressed target protein has cytotoxicity.


Assuntos
Proteínas da Membrana Bacteriana Externa/imunologia , Lipoproteínas/imunologia , Plasmídeos/genética , Proteínas Recombinantes/imunologia , Animais , Anticorpos Antibacterianos/sangue , Proteínas da Membrana Bacteriana Externa/biossíntese , Proteínas da Membrana Bacteriana Externa/genética , Western Blotting , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Clonagem Molecular , Ensaio de Imunoadsorção Enzimática , Escherichia coli/genética , Humanos , Imunização , Lipoproteínas/biossíntese , Lipoproteínas/genética , Coelhos , Proteínas Recombinantes/biossíntese , Proteínas Recombinantes/farmacologia
6.
Sci Rep ; 7(1): 15114, 2017 11 08.
Artigo em Inglês | MEDLINE | ID: mdl-29118341

RESUMO

Serotonin transporter (SERT) is a classic target of drug discovery for neuropsychiatric and digestive disorders, and against those disorders, plants of Nardostachys genus have been valued for centuries in the systems of Traditional Chinese Medicine, Ayurvedic and Unani. Herein, chemical investigation on the roots and rhizomes of Nardostachys chinensis Batal. led to the isolation of forty sesquiterpenoids including six new aristolane-type sesquiterpenoids and six new nardosinane-type sesquiterprenoids. Their structures were elucidated by extensive spectroscopic methods, combined with analyses of circular dichroism and single-crystal X-ray diffraction data. To explore natural product scaffolds with SERT regulating activity, a high-content assay for measurement of SERT function in vitro was conducted to evaluate the SERT regulating properties of these isolates. In conclusion, eleven compounds could be potential natural product scaffolds for developing drug candidates targeting SERT. Among which, kanshone C of aristolane-type sesquiterpenoid inhibited SERT most strongly, while desoxo-nachinol A of nardosinane-type sesquiterpenoid instead enhanced SERT potently.


Assuntos
Nardostachys/química , Inibidores Seletivos de Recaptação de Serotonina/isolamento & purificação , Proteínas da Membrana Plasmática de Transporte de Serotonina/metabolismo , Sesquiterpenos/isolamento & purificação , Produtos Biológicos/química , Produtos Biológicos/isolamento & purificação , Produtos Biológicos/farmacologia , Transporte Biológico/efeitos dos fármacos , Dicroísmo Circular , Cristalografia por Raios X , Estrutura Molecular , Raízes de Plantas/química , Sesquiterpenos Policíclicos , Rizoma/química , Inibidores Seletivos de Recaptação de Serotonina/química , Inibidores Seletivos de Recaptação de Serotonina/farmacologia , Sesquiterpenos/química , Sesquiterpenos/farmacologia
7.
Eur J Radiol ; 82(2): e95-9, 2013 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-23079047

RESUMO

PURPOSE: Several studies suggest that iron deposition may play a role in multiple sclerosis (MS) pathology. Three-dimensional (3D) enhanced T2*-weighted angiography (ESWAN) at 3T was used to quantify iron deposition in the precentral grey matter in MS and its relationship with disease duration, atrophy and Expanded Disability Status Scale (EDSS) scores. METHODS: We recruited 33 patients with diagnosis of clinically definite MS and 31 age- and sex-matched healthy controls who underwent conventional brain MRI, 3D-ESWAN and 3D T1sequences. We obtained the mean phase values (MPVs) of the precentral grey matter on ESWAN-filtered phase images and volume of the precentral gyrus on 3D T1 images. We investigated the correlation between precentral grey matter MPVs, precentral gyrus volume, disease duration and EDSS scores of MS patients and healthy controls. RESULTS: The precentral grey matter MPVs in MS patients and controls were 1870.83 ± 56.61 and 1899.22 ± 51.73 respectively and had significant difference in the MS group vs. the control group (t=-2.09, P=0.04). There was significant negative correlation between precentral grey matter MPVs and disease duration (r=-0.365, P=0.03). No correlation was found between MPVs and EDSS scores. Mean precentral gyrus volume in MS patients was 4368.55 ± 867.78 whereas in controls was 5701.00 ± 1184.03 with significant difference between volume of the precentral gyrus in MS patients compared to healthy controls (t=-5.167, P<0.001). There was a positive correlation between MPVs and precentral gyrus volume (r=0.291, P=0.020). CONCLUSIONS: Our study demonstrated that quantitative assessment of abnormal iron deposition in the precentral grey matter in MS patients can be measured using 3D-ESWAN.


Assuntos
Lobo Frontal/metabolismo , Imageamento Tridimensional/métodos , Ferro/análise , Imageamento por Ressonância Magnética/métodos , Esclerose Múltipla/metabolismo , Neurônios/metabolismo , Adulto , Idoso , Feminino , Lobo Frontal/patologia , Humanos , Masculino , Pessoa de Meia-Idade , Esclerose Múltipla/patologia , Neurônios/patologia , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Distribuição Tecidual
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