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1.
J Asian Nat Prod Res ; 24(6): 528-534, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-34236260

RESUMO

A new pair of enantiomeric isoprenylated chromone derivatives, (±)-pestaloficiol X [(±)-1], along with a known compound pestaloficiol J (2), were isolated from the plant endophytic fungus Pestalotiopsis sp. The racemic mixture 1 was separated through chiral HPLC. The structures of new compounds (±)-1 were elucidated on the basis of extensive spectroscopic data and their absolute configurations were further configured through computational analysis of their electronic circular dichroism (ECD) spectra. Compound (+)-1 showed significant inhibitory potency against HL-60 and HEP-3B cell lines, with IC50 values of 1.35 ± 0.15 and 3.70 ± 0.33 µM, respectively, while compound (-)-1 showed significant inhibitory potency against HL-60 and HEP-3B cell lines, with IC50 values of 2.39 ± 0.26 and 2.99 ± 0.35 µM, respectively.


Assuntos
Antineoplásicos , Pestalotiopsis , Antineoplásicos/farmacologia , Cromonas/química , Estrutura Molecular , Estereoisomerismo
2.
Bioorg Med Chem Lett ; 30(12): 127193, 2020 06 15.
Artigo em Inglês | MEDLINE | ID: mdl-32334913

RESUMO

This study aims to investigate active phytochemicals isolated from Pyrola incarnata Fisch. (P. incarnata) and their protection against neuroinflammation induced by LPS. Betulin, accompanied with other 9 compounds, were isolated from P. incarnata and elucidated by spectroscopic analysis (1H-, 13C NMR). ELISA kits and the measurement of NO production based on Griess reaction showed that betulin (5) (250 µg/mL) could suppress LPS-induced activation of microglial cell BV-2 better than others by inhibiting inflammatory cytokines (TNF-α, IL-6, IL-1ß) expression and NO production. With the guidance of computer-aided drug design and the analysis of biological experiment, we demonstrated betulin could reduce LPS-induced iNOS expression, prevent JNKs pathways, and down-regulate the phosphorylation levels of NF-κB/p65. In conclusion, betulin isolated from P. incarnata possessed outstanding anti-neuroinflammation potential, presumably related to iNOS expression, JNKs and NF-κB/p65 pathways. Therefore, Pyrola incarnata may be a valuable natural resource and betulin is a potential drug for the treatment of neurodegenerative disorders by inhibiting inflammatory mediators.


Assuntos
Desenho de Fármacos , Mediadores da Inflamação/farmacologia , Inflamação/tratamento farmacológico , Lipopolissacarídeos/antagonistas & inibidores , Pyrola/química , Triterpenos/farmacologia , Animais , Linhagem Celular , Relação Dose-Resposta a Droga , Mediadores da Inflamação/química , Mediadores da Inflamação/isolamento & purificação , Lipopolissacarídeos/farmacologia , Camundongos , Conformação Molecular , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Óxido Nítrico Sintase Tipo II/metabolismo , Estereoisomerismo , Relação Estrutura-Atividade , Triterpenos/química , Triterpenos/isolamento & purificação
3.
Phytomedicine ; 104: 154241, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35749827

RESUMO

BACKGROUND: Non-alcoholic steatohepatitis (NASH) has replaced viral hepatitis as the main driver of the rising morbidity and mortality associated with cirrhosis and liver cancer worldwide, while no FDA-approved therapies are currently known. Kinsenoside (KD), naturally isolated from Anoectochilus roxburghii, possesses multiple biological activities, including lipolysis, anti-inflammation, and hepatoprotection. However, the effects of KD on NASH remain unclear. PURPOSE: This study aimed to explore the roles of KD in NASH and its engaged mechanisms. METHODS: Two typical animal models of NASH, mice fed a methionine-choline-deficient (MCD) diet (representing non-obese NASH) and mice fed a high-fat and -fructose diet (HFFD) (representing obese NASH), were used to investigate the effect of KD on NASH in vivo. Transcriptome sequencing was performed to elucidate the underlying mechanisms of KD. Lipopolysaccharide (LPS)-stimulated THP-1 cells and transforming growth factor ß1 (TGF-ß1)-activated LX-2 cells were applied to further explore the effects and mechanisms of KD in vitro. RESULTS: The intragastric administration of KD remarkably alleviated MCD/HFFD-induced murine NASH almost in a dose-dependent manner. Specifically, KD reduced lipid accumulation, inflammation, and fibrosis in the liver of NASH mice. KD ameliorated alanine aminotransferase (ALT), aspartate aminotransferase (AST), superoxide dismutase (SOD), and malondialdehyde (MDA) abnormalities. In addition, it decreased the level of serum proinflammatory factors (IL-12p70, IL-6, TNF-α, MCP-1, IFN-γ) and the hepatic expression of typical fibrosis-related molecules (α-SMA, Col-I, TIMP-1). Mechanically, KD attenuated the MCD/HFFD-induced NASH through the inhibition of the NF-κB/NLRP3 signaling pathway. Consistently, KD reduced inflammation stimulated by LPS in THP-1 cells via suppressing the NF-κB/NLRP3 pathway. Furthermore, it prevented the activation of LX-2 cells directly, by inhibiting the proliferation stimulated by TGF-ß1, and indirectly, by inactivating the NLRP3 inflammasome in macrophages. CONCLUSION: For the first time, the practical improvement of NASH by KD was revealed. Our study found that KD exerted its alleviative effects on NASH through the inhibition of the NF-κB/NLRP3 signaling pathway. Given its hepatoprotective and nontoxic properties, KD has the potential to be a novel and effective drug to treat NASH.


Assuntos
Hepatopatia Gordurosa não Alcoólica , 4-Butirolactona/análogos & derivados , Animais , Fibrose , Inflamação/metabolismo , Lipopolissacarídeos/farmacologia , Fígado , Metionina/metabolismo , Metionina/farmacologia , Camundongos , Camundongos Endogâmicos C57BL , Monossacarídeos , NF-kappa B/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Hepatopatia Gordurosa não Alcoólica/metabolismo , Transdução de Sinais , Fator de Crescimento Transformador beta1/metabolismo
4.
Drug Dev Ind Pharm ; 37(12): 1473-80, 2011 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-21721846

RESUMO

The objectives of this study were to prepare the amifostine polylactide-co-glycolide (PLGA) microsphere and investigate its irradiation protective to mouse through oral administration. Amifostine-loaded PLGA microsphere was formulated using a modified double emulsion-solvent evaporation technique. The microsphere particle was spherical with a mean diameter of 2.8 ± 0.1 µm. Release data of amifostine PLGA microsphere was tested in phosphate-buffered saline at 37°C using a dialysis method and its release profiles was biphasic, showing a relatively large burst effect (50%) over the first 6 h, followed by a slower release phase, which sustained with 80% amifostine released in 48 h and almost 100% release till 6 days (144 h). A diffusion-controlled release model (Higuchi equation, R² = 0.9725) was obtained for amifostine releasing from PLGA microsphere. The radiation experiment was performed by applied cobalt-60 γ-radiation source. One hour before γ-radiation exposure, the mouse was orally given free amifostine and PLGA microsphere, respectively. The irradiation effects, such as blood cell concentration, superoxidase dismutase (SOD) activity and malondialdehyde (MDA) level were monitored. The results indicated that amifostine PLGA microsphere was more irradiation protective to mouse than that of free amifostine under the same oral administration route.


Assuntos
Amifostina/administração & dosagem , Ácido Láctico/administração & dosagem , Ácido Poliglicólico/administração & dosagem , Protetores contra Radiação/administração & dosagem , Administração Oral , Amifostina/química , Análise de Variância , Animais , Portadores de Fármacos , Ácido Láctico/química , Masculino , Camundongos , Microesferas , Modelos Animais , Tamanho da Partícula , Ácido Poliglicólico/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Protetores contra Radiação/química , Distribuição Aleatória
5.
Zhongguo Zhong Yao Za Zhi ; 33(18): 2090-3, 2008 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-19160791

RESUMO

OBJECTIVE: To establish HPLC fingerprint of Prunella vulgarise for quality control of the herbal medicine. METHOD: A sunfire C18 analytical column was used. The mobile phase A was 1% acetic acid, and mobile phase B was methanol. The elution was in gradient mode and detection wavelength was set at 290 nm. The flow rate was 1.0 mL x min(-1) and the column temperature at 30 degrees C. The analysis time was 60 min. RESULT: The similarity of 10 batches of P. vulgaris was not lower than 0.810. The fingerprints of the herbal medicine were classified P. vulgaris on the results of cluster analysis. CONCLUSION: This method is available for quality evaluation and control the quality of P. vulgaris.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Prunella/química , Medicamentos de Ervas Chinesas/química
6.
Curr Med Sci ; 38(1): 11-18, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30074146

RESUMO

Kinsenoside is a main active component isolated from plants of the genus Anoectochilus, and exhibits many biological activities and pharmacological effects, including hepatoprotective, anti-hyperglycemic, anti-hyperliposis, anti-inflammatory, vascular protective and anti-osteoporosis effects and so on, which is contributing to its promising potency in disease treatments. This review aims to recapitulate the pharmacological functions of kinsenoside, as well as its source, extraction, identification, quantitative analysis, pharmacokinetics, synthesis and patent information. The data reported in this work can confirm the therapeutic potential of kinsenoside and provide useful information for further new drug development.


Assuntos
4-Butirolactona/análogos & derivados , Conservadores da Densidade Óssea/farmacologia , Conservadores da Densidade Óssea/farmacocinética , Hipoglicemiantes/farmacologia , Monossacarídeos/farmacologia , Orchidaceae/química , 4-Butirolactona/química , 4-Butirolactona/farmacocinética , 4-Butirolactona/farmacologia , Animais , Conservadores da Densidade Óssea/química , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/farmacocinética , Fígado/efeitos dos fármacos , Monossacarídeos/química , Monossacarídeos/farmacocinética
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