RÉSUMÉ
This study explores the effect of apigenin(APG), oxymatrine(OMT), and APG+OMT on the proliferation of non-small cell lung cancer cell lines and the underlying mechanisms. Cell counting kit-8(CCK-8) assay was used to detect the vitality of A549 and NCI-H1975 cells, and colony formation assay to evaluate the colony formation ability of the cells. EdU assay was employed to examine the proliferation of NCI-H1975 cells. RT-qPCR and Western blot were performed to detect the mRNA and protein expression of PLOD2. Molecular docking was carried out to explore the direct action ability and action sites between APG/OMT and PLOD2/EGFR. Western blot was used to study the expression of related proteins in EGFR pathway. The viability of A549 and NCI-H1975 cells was inhibited by APG and APG+OMT at 20, 40, and 80 μmol·L~(-1) in a dose-dependent manner. The colony formation ability of NCI-H1975 cells was significantly suppressed by APG and APG+OMT. The mRNA and protein expression of PLOD2 was significantly inhibited by APG and APG+OMT. In addition, APG and OMT had strong binding activity with PLOD2 and EGFR. In APG and APG+OMT groups, the expression of EGFR and proteins in its downstream signaling pathways was significantly down-regulated. It is concluded that APG in combination with OMT could inhibit non-small lung cancer, and the mechanism may be related to EGFR and its downstream signaling pathways. This study lays a new theoretical basis for the clinical treatment of non-small cell lung cancer with APG in combination with OMT and provides a reference for further research on the anti-tumor mechanism of APG in combination with OMT.
Sujet(s)
Humains , Carcinome pulmonaire non à petites cellules , Tumeurs du poumon , Apigénine , Simulation de docking moléculaire , Alcaloïdes , Quinolizines , ARN messager , Récepteurs ErbBRÉSUMÉ
This study aimed to explore the anti-inflammatory material basis and molecular mechanism of Artemisia stolonifera based on the analysis of the chemical components in different extracted fractions of A. stolonifera and their antioxidant and anti-inflammatory effects in combination with network pharmacology and molecular docking. Thirty-two chemical components were identified from A. stolonifera by ultra-performance liquid chromatography coupled to tandem quadrupole time-of-flight mass spectrometry(UPLC-Q-TOF-MS). Among them, there were 7, 21 and 22 compounds in water, n-butanol and ethyl acetate fractions, respectively. The antio-xidant capacity of different extracted fractions was evaluated by measuring their scavenging ability against 1,1-diphenyl-2-picrylhydrazyl radical 2,2-diphenyl-1-(2,4,6-trinitrophenyl) hydrazyl(DPPH) and 2,2'-azinobis-(3-ethylbenzthiazoline-6-sulphonic acid)(ABTS) free radicals and total antioxidant capacity [ferric reducing antioxidant power(FRAP) assay]. The inflammatory model of RAW264.7 cells was induced by lipopolysaccharide(LPS), and the levels of nitrite oxide(NO), tumor necrosis factor-α(TNF-α), interleukin-6(IL-6) in the supernatant and the mRNA expression of related inflammatory factors in cells were used to evaluate the anti-inflammatory effects. The results revealed that ethyl acetate fraction of A. stolonifera was the optimal antioxidant and anti-inflammatory fraction. By network pharmacology, it was found that flavonoids such as rhamnazin, eupatilin, jaceosidin, luteolin and nepetin could act on key targets such as TNF, serine/threonine protein kinase 1(AKT1), tumor protein p53(TP53), caspase-3(CASP3) and epidermal growth factor receptor(EGFR), and regulate the phosphatidylinositol-3-kinase-protein kinase B(PI3K-AKT) and mitogen-activated protein kinase(MAPK) signaling pathways to exert the anti-inflammatory effects. Molecular docking further indicated excellent binding properties between the above core components and core targets. This study preliminarily clarified the anti-inflammatory material basis and mechanism of ethyl acetate fraction of A. stolonifera, providing a basis for the follow-up clinical application of A. stolonifera and drug development.
Sujet(s)
Antioxydants/composition chimique , Simulation de docking moléculaire , Artemisia , Pharmacologie des réseaux , Phosphatidylinositol 3-kinases , Anti-inflammatoires/composition chimique , Médicaments issus de plantes chinoises/pharmacologie , Interleukine-6RÉSUMÉ
This paper aims to compare the difference of growth and quality between wild and cultivated Artemisia stolonifera, thereby providing references for further development and utilization of A. stolonifera. The wild and cultivated A. stolonifera from different altitudes were collected, and the agronomic characters, moxa yield, volatile components, flavonoids, and phenolic acids were determined. The results showed that the cultivated species were taller and stronger, with more leaves and branches, than the wild species. The moxa yield and combustion quality of wild products were higher than those of cultivated products. The content of main volatile components in cultivated products was higher than that in wild products. The content of flavonoids and phenolic acids in wild products was higher than that in cultivated products. At high altitude, the ignition performance, combustion persistence, comprehensive combustion performance, and heat release during combustion of the wild and cultivated A. stolonifera. were optimal. At middle altitude, the content of main characteristic volatile components and flavone phenolic acids in the leaves of the cultivated and wild A. stolonifera were the highest. At low altitude, the combustion quality and the content of the above components of the cultivated A. stolonifera decrease significantly. Considering the combustion quality and the content of the internal components of the leaf lint, the middle and high altitude areas are suitable for the artificial cultivation of A. stolonifera.
Sujet(s)
Artemisia , Agriculture , Flavonoïdes , Feuilles de plante , Médicaments issus de plantes chinoisesRÉSUMÉ
This study is based on ultra-high-performance liquid chromatography(UPLC), gas chromatography-mass spectrometry(GC-MS), and network pharmacology methods to analyze and predict potential quality markers(Q-markers) of Artemisiae Argyi Folium. First, UPLC and GC-MS techniques were used to analyze the content of 12 non-volatile components and 8 volatile components in the leaves of 33 Artemisia argyi germplasm resources as candidate Q-markers. Subsequently, network pharmacology was employed to construct a "component-target-pathway-efficacy" network to screen out core Q-markers, and the biological activity of the markers was validated using molecular docking. Finally, cluster analysis and principal component analysis were performed on the content of Q-markers in the 33 A. argyi germplasm resources. The results showed that 18 candidate components, 60 targets, and 185 relationships were identified, which were associated with 72 pathways related to the treatment of 11 diseases and exhibited 5 other effects. Based on the combination of freedom and component specificity, six components, including eupatilin, cineole, β-caryophyllene, dinatin, jaceosidin, and caryophyllene oxide were selected as potential Q-markers for Artemisiae Argyi Folium. According to the content of these six markers, cluster analysis divided the 33 A. argyi germplasm resources into three groups, and principal component analysis identified S14 as having the highest overall quality. This study provides a reference for exploring Q-markers of Artemisiae Argyi Folium, establishing a quality evaluation system, further studying its pharmacological mechanisms, and breeding new varieties.
Sujet(s)
Simulation de docking moléculaire , Pharmacologie des réseaux , Amélioration des plantes , Chromatographie en phase liquide à haute performance/méthodes , Chromatographie gazeuse-spectrométrie de masse , Artemisia/composition chimique , Médicaments issus de plantes chinoises/composition chimiqueRÉSUMÉ
The present study explored the effects and its underlying mechanisms of four active fractions of Camellia nitidissima(leaf polyphenols, leaf saponins, flower polyphenols, and flower saponins in C. nitidissima) in inhibiting the proliferation and migration of non-small cell lung cancer(NSCLC) by suppressing the epidermal growth factor receptor(EGFR). MTT assay was used to detect the effect of four active fractions on the proliferation of NCI-H1975 and HCC827 cells. Wound healing assay and Transwell assay were adopted to evaluate the effect of four active fractions on the migration of NSCLC. The effect of four active fractions on the enzyme activity of EGFR was detected. Molecular docking was carried out to explore the direct action capacity and action sites between representative components of the four active fractions and EGPR. Western blot assay was employed to investigate the effect of four active fractions on the protein expression in EGFR downstream signaling pathways. The results of the MTT assay indicated that the cell viability of NCI-H1975 and HCC827 cells was significantly inhibited by four active fractions at 50, 100, 150, and 200 μg·mL~(-1) in a dose-dependent manner. Wound healing assay and Transwell assay revealed that the migration of NCI-H1975 and HCC827 cells was significantly suppressed by four active fractions. In addition, the results of the protein activity assay showed that the enzyme activity of EGFR was significantly inhibited by four active fractions. The molecular docking results confirmed that various components in four active fractions possessed strong binding activity to EGFR enzymes. Western blot assay revealed that four active fractions down-regulated the protein expression of EGFR and its downstream signaling pathways. It is concluded that the four active fractions of C. nitidissima can inhibit NSCLC. The mechanism may be related to EGFR and its downstream signaling pathways. This study provides a new scientific basis for the clinical treatment of NSCLC with active fractions of C. nitidissima, which is of reference significance for further research on the anti-tumor mechanism of C. nitidissima.
Sujet(s)
Humains , Apoptose , Camellia , Carcinome pulmonaire non à petites cellules/traitement médicamenteux , Lignée cellulaire tumorale , Prolifération cellulaire , Récepteurs ErbB/génétique , Tumeurs du poumon/traitement médicamenteux , Simulation de docking moléculaireRÉSUMÉ
In order to explore the effect of different drying methods(drying-in-the-shade, sun-drying, and hot air drying) on appearance characteristics, internal structure and composition of Belamcandae Rhizoma, so as to provide a theoretical basis for screening out suitable drying methods for primary processing. In this study, the Belamcandae Rhizoma's dynamic changes of the moisture content ratio and drying rate with different drying time under different drying methods, as well as the effects of different drying methods on the appearance, drying rate, density, ash, extractives and the contents of six flavonoids(mangiferin, tectoridin, iridin, tectorigenin, irigenin, irisflorentin) were compared. The results showed that fresh Belamcandae Rhizoma consumed the longest time to reach the water balance point by traditional dry drying in the shade, whiche was about 311 h; that by sun drying was 19.3%, which was shorter than drying in the shade; both drying curves were smoother. The section color of the sun drying samples was the closest to that of fresh samples, but the interior is full of holes, with a low density and loose structure. Hot air drying(40, 60, 80 ℃) could save about 27% to 88% of the drying time, which was greatly shorter, with less pores, a larger density and compact structure. Compared with the traditional drying method, the drying rate of hot air drying was reduced by 13.7%. Ash was affected by temperature, the drying conditions under 40 ℃ and below were not significantly different from those of conventional drying. The ash content decreased by 7.73% to 18.5% compared with conventional drying at 60,80 ℃. After conventional drying and 40 ℃ hot air drying, the contents of tectoridin and iridin(glycosides) in the samples were significantly higher than those in 60,80 ℃ hot air drying, while the contents of tectorigenin, irigenin and irisflorentin(aglycones) dried at 60 ℃ were the best. Therefore, considering comprehensive appearance characteristics and content of medicinal ingredients, traditional Chinese medicinal materials after 60 ℃ hot air drying show a solid texture, tight internal structure, good appearance, appropriate reduction of toxic parasides and higher aglycone content.
Sujet(s)
Dessiccation , Médicaments issus de plantes chinoises , RhizomeRÉSUMÉ
Natural products have attracted a great deal of attention as significant resources in traditional Chinese medicine (TCM) and in chemical medicine, as well as in cosmetic ingredients, nutraceuticals and food products. Isochlorogenic acid (ICGA), which has medicinal value, has been discovered in various plants. As a widespread natural medicine, ICGA should be the subject of further research and development. However, there have been no systematic analyses of ICGA. According to our investigation, ICGA was initially isolated from green coffee extracts by Barnes et al. in 1950. To date, it has been discovered in a variety of tea, vegetables, medicinal diet and TCM materials. ICGA is used as a chemical marker for the quality control of these TCM materials. The metabolic process of ICGA has been studied in detail, conforming to be linear dynamics. Thus, the clear pharmacokinetics of ICGA offers a solid foundation for its research and development. ICGA has multiple biological and pharmacological effects, and studies have mainly focused on its antioxidant, anti-inflammatory, antimicrobial, hypoglycemic, neuroprotective, and cardiovascular protective effects, and hepatoprotective properties. The mechanisms underlying these effects are summarized in this review to provide scientific support and inspiration for the future research and development of ICGA and ICGA-rich natural products.
RÉSUMÉ
To investigate the effects of different habitat processing methods of Salviae Miltiorrhizae Radix et Rhizoma on acute myocardial ischemia induced by pituitrin in rats. In this experiment, the tail vein injection of pituitrin was used to induce acute myocardial ischemia in rats. Electrocardiograph(ECG) heart rate and ΔST changes were recorded, and the levels of creatine kinase isoenzyme(CK-MB), lactate dehydrogenase(LDH), superoxide dismutase(SOD) and malondialdehyde(MDA) in serum of rats were detected to comprehensively evaluate the effects of six processing methods of Salviae Miltiorrhizae Radix et Rhizoma on serum biochemical indexes of rats with acute myocardial injury. The ECG results showed that the Salviae Miltiorrhizae Radix et Rhizoma dried in a drying oven had a good effect on the improvement of heart rate and ΔST of electrocardiogram after ischemia, and all the other groups had some protective effects to different degrees. The results of biochemical indexes in serum of each group after ischemia showed that the activity of CK-MB decreased most significantly in Salviae Miltiorrhizae Radix et Rhizoma high-dose group with drying in a drying oven after sweating and losing weight in a drying oven, high-dose group with drying in the shade and low-dose group with drying in the shade. The activity of LDH decreased most significantly in Salviae Miltiorrhizae Radix et Rhizoma high-dose group with drying in the shade and low-dose group of drying in the shade. The activity of SOD increased most significantly in Salviae Miltiorrhizae Radix et Rhizoma low-dose group with drying in sun, low-dose group with drying in sun after sweating and losing weight in sun, and low-dose group with drying in a drying oven. The activity of MDA decreased most significantly in Salviae Miltiorrhizae Radix et Rhizoma low-dose group with drying in sun. The comprehensive scoring results showed that the highest score was obtained in Salviae Miltiorrhizae Radix et Rhizoma high-dose group with drying in the shade while the scores of other treatment groups were higher than that of the model group. It could be seen that the Salviae Miltiorrhizae Radix et Rhizoma dried in a drying oven had a good improvement effect on electrocardiograph indexes after acute myocardial injury, the Salviae Miltiorrhizae Radix et Rhizoma dried in the shade had a good improvement effect on serum myocardial enzymes after acute myocardial injury, and the other processing methods had a certain protective effect on myocardial injury. The six processing methods evaluated by pharmacodynamics showed that the Salviae Miltiorrhizae Radix et Rhizoma dried in the shade and dried in a drying oven had good efficacy.
Sujet(s)
Animaux , Rats , Médicaments issus de plantes chinoises , Écosystème , Ischémie myocardique , Rhizome , Salvia miltiorrhizaRÉSUMÉ
This study aimed to simultaneously determine the contents of astilbin and engeletin in dong medicine "sunl gaems" of Guizhou origin by quantitative analysis of multi-components by single marker (QAMS), with astilbin as the internal standard substance. On UPLC and HPLC chromatograms, different models of instruments were used to investigate relative correction factors (RCF), in order to discuss the interoperability of RCFs established in different chromatographic systems. The engeletin content was calculated based on the established RCFs and compared by the one point external standard method and the external standard working curve method, in order to verify the accuracy of QAMS. According to the result, in different chromatograms, the ratios between RCF and retention time of engeletin and astilbin had a good reproducibility, with RSD between 2.0% and 1.8%, both were less than 3%. The relative differences among results of QAMS, the external standard working curve method of dong medicine "sunl gaems" ranged between 1.6% and 3.9%, with RSD between 2.02%-0.80% in line with relevant requirements and Pearson correlation coefficient at 0.9998 (P <0.01). The findings showed that QAMS was an accurate, reliable and highly reproducible method to determine the contents of astilbin and engeletin in dong medicine "sunl gaems" of Guizhou origin and so could be used to control the inherent quality of the herb.
Sujet(s)
Chromatographie en phase liquide à haute performance , Méthodes , Médicaments issus de plantes chinoises , Flavonols , HétérosidesRÉSUMÉ
The paper is aimed to search more natural plant antioxidants and further research and develop new medicinal plant resources in Guizhou. The Guizhou special miao medicine "bod zangd dak" was extracted with 60% ethanol. The antioxidant activity of the different polarity components separated from the extract was tested by DPPH method with ascorbic acid as positive control. The results showed that the IC50 of the different polarity components was as following: ascorbic acid (0.033 4 g x L(-1)) < ethyl acetate components (0.052 3 g x L(-1)) < total tannins components (0.054 9 g x L(-1)) < 60% ethanol extraction components (0.076 7 g x L(-1)) < butanol extraction components (0.110 g x L(-1)) < water-soluble polysaccharides components (0.168 g x L(-1)) < water extraction components (0.174 g x L(-1)) < water components after extraction (0.226 g x L(-1)) < total polysaccharides components (0.645 g x L(-1)). It is concluded that the different polarity components have different free radical scavenging activity and that provides a scientific basis for further search of the active ingredients and the activive mechanism.