RESUMO
This paper investigated the effect of total saponins from Rhizoma Panacis Majoris on the proliferation, apoptosis, and autophagy of human cervical carcinoma HeLa cells. The saponin content was detected by ultraviolet-visible spectrophotometry. Cell coun-ting kit-8(CCK-8) assay, 4,6-diamidino-2-phenylindole(DAPI) staining, and flow cytometry were used to detect the effects of total saponins of Panacis Majoris Rhizoma on cell viability, morphology, cell cycle and apoptosis of HeLa cells. Western blot was used to detect the expression of apoptosis-related proteins B cell lymphoma-2(Bcl-2), Bcl-2-associated X protein(Bax), cleaved caspase-9, and cleaved caspase-3, autophagy-related proteins Beclin-1 and SQSTM1(p62), and the proteins related to the phosphatidylinositol 3-kinase/protein kinase B/mammalian target of rapamycin(PI3K/Akt/mTOR) and mitogen-activated protein kinase(MAPK) signaling pathways. It was found that the yield and saponin content of total saponins from Rhizoma Panacis Majoris were 6.3% and 78.3%, respectively. Total saponins from Rhizoma Panacis Majoris could significantly inhibit the proliferation(P<0.001), effect the nuclear morphology, block the G_0/G_1 cycle, and induce cell apoptosis in HeLa cells with a concentration-dependent manner. In addition, total saponins from Rhizoma Panacis Majoris up-regulated the expression of pro-apoptotic proteins Bax, cleaved caspase-9, and cleaved caspase-3, and autophagy-related protein p62(P<0.05), while down-regulated the expression of anti-apoptotic protein Bcl-2 and autophagy-related protein Beclin-1(P<0.01). Total saponins from Rhizoma Panacis Majoris could promote the expression of p-p38/p38, p-Jun N-terminal kinase(JNK)/JNK, p-PI3K/PI3K, p-Akt/Akt, p-mTOR/mTOR proteins in PI3K/Akt/mTOR and MAPK signaling pathways(P<0.05). In contrast, the effect on p-ERK/ERK expression was not obvious. Therefore, total saponins from Rhizoma Panacis Majoris may inhibit autophagy and promote apoptosis of HeLa cells through the activation of the PI3K/Akt/mTOR, c-JNK, and p38 MAPK signaling pathways, which indicates that total saponins from Rhizoma Panacis Majoris may have a potential role in cervical cancer treatment.
Assuntos
Apoptose , Autofagia , Proliferação de Células , Rizoma , Saponinas , Neoplasias do Colo do Útero , Humanos , Saponinas/farmacologia , Saponinas/química , Células HeLa , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Autofagia/efeitos dos fármacos , Rizoma/química , Neoplasias do Colo do Útero/tratamento farmacológico , Neoplasias do Colo do Útero/metabolismo , Neoplasias do Colo do Útero/patologia , Feminino , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/química , Transdução de Sinais/efeitos dos fármacos , Serina-Treonina Quinases TOR/metabolismo , Serina-Treonina Quinases TOR/genética , Sobrevivência Celular/efeitos dos fármacosRESUMO
Boiled lotus rhizome discs (BLRDs), as common processed products of lotus rhizome, have gained increasing attention from consumers and food manufacturers. However, the blue pigment formed during boiling affects its appearance and reduces the appetite of BLRDs. In this study, the effects of polyphenols and iron contents on blue pigment formation in BLRDs in different regions and months were investigated. Results revealed that blue variation was more serious in March and April of the second year in Wuhan, and polyphenols and iron contents in these two months were significantly higher than those in other months. Then, UPLC and UV-Vis analysis showed that polyphenols causing the formation of blue pigment in BLRDs were L-dopa, gallocatechin, catechin, epigallocatechin, chlorogenic acid and epicatechin, among which L-dopa (52.450 mg/100 g in fresh lotus rhizome (FLR)) and gallocatechin (36.210 mg/100 g in FLR) possessed the greatest effect. Moreover, the ESI-Q-TOF-MS analysis of L-dopa-iron chelate and gallocatechin-iron chelate suggested that the blue pigment of BLRDs was mainly in the form of bis-complexes under boiling conditions. The study on formation mechanism of blue pigment in BLRDs can provide a reference for lotus rhizome processing.
Assuntos
Ferro , Polifenóis , Rizoma , Rizoma/química , Polifenóis/química , Polifenóis/análise , Ferro/química , Quelantes de Ferro/química , Pigmentos Biológicos/química , Catequina/química , Catequina/análogos & derivados , Catequina/análise , Levodopa/química , Lotus/química , Cromatografia Líquida de Alta Pressão , Culinária , Temperatura Alta , Ácido Clorogênico/química , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
BACKGROUND: Ginseng Radix et Rhizoma (GS) is frequently used as an adjuvant therapy for patients with heart failure (HF). Metoprolol is widely used in patients with HF. However, there is no report on the combined effects of GS and metoprolol in patients with HF. OBJECTIVE: This study investigated the combined effects of GS and metoprolol in male C57BL/6J mice with HF and the underlying mechanisms. MATERIALS AND METHODS: We utilized a mouse myocardial HF model to measure the serum levels of creatine kinase (CK) and creatine kinase-MB form (CK-MB) using an automated biochemical analyzer. Lactate dehydrogenase (LDH) and cardiac troponin (cTnT) levels were determined using enzyme-linked immunosorbent assays. Autophagy of myocardial cells was evaluated using transmission electron microscopy, and changes in signal pathway proteins related to autophagy were analyzed by Western blotting. RESULTS: GS combined with metoprolol improved heart function, reduced heart damage, and decreased serum levels of CK, CK-MB, LDH, and cTnT. The combination of GS and metoprolol decreased autophagy in myocardial cells by reducing the levels of autophagy-related proteins (LC3, p62, Beclin1, and Atg5) and increasing the ratios of p-PI3K/PI3K, p-Akt/Akt, and p-mTOR/mTOR. CONCLUSION: GS enhanced the anti-heart failure effect of metoprolol. Its mechanism of action might be related to the inhibition of autophagy mediated by the activation of the PI3K/Akt/mTOR pathway.
Assuntos
Autofagia , Insuficiência Cardíaca , Metoprolol , Camundongos Endogâmicos C57BL , Panax , Animais , Masculino , Autofagia/efeitos dos fármacos , Insuficiência Cardíaca/tratamento farmacológico , Insuficiência Cardíaca/patologia , Insuficiência Cardíaca/metabolismo , Metoprolol/farmacologia , Camundongos , Panax/química , Transdução de Sinais/efeitos dos fármacos , Doença Crônica , Rizoma/química , Modelos Animais de Doenças , L-Lactato Desidrogenase/sangue , L-Lactato Desidrogenase/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Extratos Vegetais/farmacologia , Creatina Quinase/sangue , Sinergismo Farmacológico , Creatina Quinase Forma MB/sangueRESUMO
This study aims to reveal the effects of the herb pair Astragali Radix-Salviae Miltiorrhizae Radix et Rhizoma(AR-SMRR) on phosphatidylinositol 3-kinase/protein kinase B/mammalian target of rapamycin(PI3K/Akt/mTOR) pathway and autophagy in the lung tissue of the rat model of acute lung injury(ALI). Fifty adult male SD rats were randomized into sham, model, autophagy inhibition(intraperitoneal injection of chloroquine at 10 mg·kg~(-1)), autophagy induction(intraperitoneal injection of rapamycin at 15 mg·kg~(-1)), and AR-SMRR(5 g·kg~(-1), gavage) groups. The rats in the sham group received intratracheal instillation of normal saline, and those in other groups received intratracheal instillation of lipopolysaccharide(LPS, 5 mg·kg~(-1)) for the modeling of ALI. Seven days before the operation, the rats in the sham and model groups were administrated with normal saline, and those in other groups with corresponding drugs. Specimens were collected 24 h after modeling. The pathological changes of the lung tissue were observed under a light microscope. The lung wet/dry weight ratio and the lactate dehydrogenase(LDH) activity and total protein concentration in the bronchoalveolar lavage fluid(BALF) were measured. Western blot was employed to measure the protein levels of microtubule-associated protein 1-light chain 3(LC3), beclin-1, p62, PI3K, Akt, and mTOR. Compared with the sham group, the model group showed increased histopathological score of the lung tissue, lung wet/dry weight ratio, and LDH activity and protein concentration in BALF. Autophagy inhibition further increased these indicators compared with the model group, while autophagy induction and AR-SMRR lowered the levels. In addition, AR-SMRR up-regulated the protein levels of LC3-â ¡ and beclin-1, down-regulated the expression of p62, and inhibited the expression of p-PI3K, p-Akt, and p-mTOR in the lung tissue of ALI rats. The findings suggest that AR-SMRR can alleviate the lung injury and edema in the rat model of ALI induced by LPS by enhancing autophagy via down-regulating PI3K/Akt/mTOR signaling pathway.
Assuntos
Lesão Pulmonar Aguda , Autofagia , Medicamentos de Ervas Chinesas , Fosfatidilinositol 3-Quinases , Proteínas Proto-Oncogênicas c-akt , Ratos Sprague-Dawley , Transdução de Sinais , Serina-Treonina Quinases TOR , Animais , Lesão Pulmonar Aguda/tratamento farmacológico , Lesão Pulmonar Aguda/metabolismo , Masculino , Serina-Treonina Quinases TOR/metabolismo , Serina-Treonina Quinases TOR/genética , Ratos , Proteínas Proto-Oncogênicas c-akt/metabolismo , Proteínas Proto-Oncogênicas c-akt/genética , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/farmacologia , Autofagia/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/metabolismo , Fosfatidilinositol 3-Quinases/genética , Salvia miltiorrhiza/química , Astragalus propinquus/química , Rizoma/química , Pulmão/efeitos dos fármacos , Pulmão/metabolismo , Pulmão/patologia , HumanosRESUMO
Based on UHPLC-Q-Exactive Orbitrap HRMS coupled with the network pharmacology and molecular docking, the common material basis and molecular mechanisms of Bletillae Rhizoma for melasma, gastrointestinal hemorrhage, lung cancer and bronchoplumonary inflammation as "homotherapy for heteropathy" were explored. The fingerprint of 17 batches of Bletillae Rhizoma from different areas was established using HPLC, and the similarity analysis was carried out. The common chemical components of the 17 batches of Bletillae Rhizoma were identified using UHPLC-Q-Exactive Orbitrap HRMS. Depending on the bioavailability and drug-like properties of the common components, the active chemical components were screened, and then their protein targets were collected using the Traditional Chinese Medicine Database and Analysis Platform(TCMSP) and SwissTargetPrediction database. The protein targets related to diseases were retrieved from the databases DrugBank, TTD and GeneCards to produce a Venn diagram. The shared targets were obtained between drugs and diseases as "homotherapy for heteropathy" targets. The protein-protein interaction(PPI) was analyzed with the STRING database, and KEGG and GO analyses of the "homotherapy for heteropathy" targets were performed using the Bioconductor database. Cytoscape 3.7.2 software was employed to construct the "chemical components of Bletillae Rhizoma-homotherapy for heteropathy targets" network and PPI network, and topological analysis was conducted to screen out the key active chemical components and core targets. Finally, the affinity between the active components and core targets was evaluated using the molecular docking by AutoDock Vina 4.2.6, which verified the interaction between them. Thirteen common peaks were identified by fingerprint chromatography, and the similarity between different batches was 0.941-0.998. Fifty-three chemical components were identified by mass spectrometry in Bletillae Rhizoma, and 18 common chemical constituents were obtained in the 17 batches of Bletillae Rhizoma. Network pharmacologic screening showed that the pharmacodynamic substances of Bletillae Rhizoma for melasma, gastrointestinal hemo-rrhage, lung cancer and bronchoplumonary inflammation with "homotherapy for heteropathy" were 11 compounds, such as polysaccharides, biphenanthrenes, dihydrophenanthrenes and bibenzyls. There were 42 common targets identified for the treatment of different diseases. These targets were involved in biological processes such as cell response to chemical stress, reactive oxygen species and positive regulation of protein kinase B signal transduction. They were also involved in 121 signaling pathways, encompassing vital pathways such as PI3K-Akt, ErbB, Rap1, FoxO, MAPK and estrogen. Molecular docking results showed a strong affinity between the key active components and the core targets. This study provides a preliminary explanation of how Bletillae Rhizoma exerts its therapeutic effect on chloasma, gastrointestinal hemorrhage, lung cancer, and bronchopneumonic lesions as "homotherapy for heteropathy" through a combined action involving multiple components, targets, and pathways. These findings offer a certain theoretical basis for the further deve-lopment and application of Bletillae Rhizoma.
Assuntos
Medicamentos de Ervas Chinesas , Neoplasias Pulmonares , Simulação de Acoplamento Molecular , Farmacologia em Rede , Rizoma , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Cromatografia Líquida de Alta Pressão , Rizoma/química , Neoplasias Pulmonares/tratamento farmacológico , Hemorragia Gastrointestinal/tratamento farmacológico , Melanose/tratamento farmacológico , Orchidaceae/química , Inflamação/tratamento farmacológico , Espectrometria de MassasRESUMO
This study aims to explore the effect of Lycii Fructus and Salviae Miltiorrhizae Radix et Rhizoma(LFSMR), a drug pair possesses the function of nourishing Yin, promoting blood circulation, and brightening the eyes, in treating retinitis pigmentosa(RP)by inhibiting the gliosis of Müller cells(MCs) and inducing their reprogramming and differentiation into various types of retinal nerve cells. Twelve C57 mice were used as the normal control group, and 48 transgenic RP(rd10) mice were randomly divided into the model group, positive control group, and low and high dose LFSMR groups, with 12 mice in each group. HE staining was used to detect pathological changes in the retina, and an electroretinogram was used to detect retinal function. Retinal optical coherence tomography was used to detect retinal thickness and perform fundus photography, and laser speckle perfusion imaging was used to detect local retinal blood flow. Digital PCR was used to detect gene expression related to retinal nerve cells, and immunofluorescence was used to detect protein expression related to retinal nerve cells. LFSMR could significantly improve the pathological changes, increase the amplitude of a and b waves, increase the retinal thickness, restore retinal damage, and increase retinal blood flow in mice with RP lesions. LFSMR could also significantly inhibit the m RNA expression of the glial fibrillary acidic protein( GFAP) during the pathogenesis of RP and upregulate m RNA expression of sex determining region Y box protein 2(SOX2), paired box protein 6(Pax6),rhodopsin, protein kinase C-α(PKCα), syntaxin, and thymic cell antigen 1. 1(Thy1. 1). LFSMR could significantly inhibit GFAP protein expression and enhance protein expression of SOX2, Pax6, rhodopsin, PKCα, syntaxin, and Thy1. 1. It could also reverse the pathological changes in the retina of rd10 mice, improve retinal function and fundus performance, increase retinal thickness, enhance local retinal blood flow, and exert therapeutic effects on RP. The mechanism of action of LFSMR may be related to inhibiting the gliosis of MCs and promoting their reprogramming and differentiation into various types of retinal nerve cells.
Assuntos
Medicamentos de Ervas Chinesas , Células Ependimogliais , Lycium , Camundongos Endogâmicos C57BL , Retinose Pigmentar , Salvia miltiorrhiza , Animais , Camundongos , Células Ependimogliais/efeitos dos fármacos , Células Ependimogliais/metabolismo , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/administração & dosagem , Lycium/química , Retinose Pigmentar/tratamento farmacológico , Retinose Pigmentar/genética , Retinose Pigmentar/metabolismo , Retinose Pigmentar/fisiopatologia , Salvia miltiorrhiza/química , Masculino , Retina/efeitos dos fármacos , Rizoma/química , HumanosRESUMO
The present study aimed to evaluate the effect of dry turmeric rhizomes on in vitro biogas production and diet fermentability. Turmeric rhizomes were included at gradually increased levels: 0, 0.5, 1, 1.5 and 2% of a diet containing per kg dr matter (DM): 500 g concentrate feed mixture, 400 g berseem hay and 100 g rice straw, and incubated for 48 h. Gas chromatography-mass spectrometry analysis showed that ar-turmerone, α-turmerone and ß-turmerone were the major bioactive compounds in the rhizomes. Turmeric rhizomes increased (p < 0.01) asymptotic gas production (GP) and rate and lag of CH4 production and decreased (p < 0.01) rate of GP, lag of GP, asymptotic CH4 production and proportion of CH4 production. Turmeric rhizome administration linearly increased (p < 0.01) DM and fiber degradability and concentrations of total short-chain fatty acids, acetic and propionic acids and ammonia-N and quadratically (p < 0.05) decreased fermentation pH. It is concluded that including up to 2% turmeric rhizomes improved in vitro ruminal fermentation and decreased CH4 production.
Assuntos
Curcuma , Fermentação , Metano , Rizoma , Curcuma/química , Rizoma/química , Animais , Metano/metabolismo , Rúmen/metabolismo , Ração Animal/análise , Dieta/veterinária , Digestão/efeitos dos fármacosRESUMO
Isoxerophilusins A (1) and B (2), two unprecedented diterpene heterodimers biogenetically from ent-atisanes and abietanes, were isolated from the rhizomes of Isodon xerophilus. Their structures were determined by extensive spectroscopic analysis and single-crystal X-ray diffraction. Selective esterification of 1 generated 11 new derivatives. All derivatives showed excellent α-glucosidase inhibitory activity in comparison to acarbose. Compounds 12 and 13 demonstrated significant inhibition against α-glucosidase with IC50 values of 4.92 and 3.83 µM, respectively.
Assuntos
Diterpenos , Inibidores de Glicosídeo Hidrolases , Isodon , alfa-Glucosidases , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Diterpenos/química , Diterpenos/farmacologia , Diterpenos/isolamento & purificação , alfa-Glucosidases/metabolismo , Estrutura Molecular , Isodon/química , Dimerização , Cristalografia por Raios X , Relação Estrutura-Atividade , Rizoma/químicaRESUMO
Rhei Radix et Rhizoma and Magnoliae Officinalis Cortex have been used together to treat constipation in the clinical practices for more than 2000 years. Nonetheless, their compatibility mechanism is still unclear. In this study, the amelioration of Rhei Radix et Rhizoma combined with Magnoliae Officinalis Cortex on constipation was systematically and comprehensively evaluated. The results showed that their compatibility could markedly shorten gastrointestinal transport time, increase fecal water content and frequency of defecation, improve gastrointestinal hormone disorders and protect colon tissue of constipation rats compared with the single drug. Furthermore, according to 16S rRNA sequencing in conjunction with UPLC-Q-TOF/MS, the combination of two herbal medications could greatly raise the number of salutary bacteria (Lachnospiraceae, Romboutsia and Subdoligranulum) while decreasing the abundance of pathogenic bacteria (Erysipelatoclostridiaceae). And two herb drugs could markedly improve the disorder of fecal metabolic profiles. A total of 7 different metabolites associated with constipation were remarkably shifted by the compatibility of two herbs, which were mainly related to arachidonic acid metabolism, alpha-linolenic acid metabolism, unsaturated fatty acid biosynthesis and other metabolic ways. Thus, the regulation of intestinal microbiome and its metabolism could be a potential target for Rhei Radix et Rhizoma and Magnoliae Officinalis Cortex herb pair to treat constipation. Furthermore, the multi-omics approach utilized in this study, which integrated the microbiome and metabolome, had potential for investigating the mechanism of traditional Chinese medicines.
Assuntos
Constipação Intestinal , Medicamentos de Ervas Chinesas , Fezes , Microbioma Gastrointestinal , Magnolia , Ratos Sprague-Dawley , Rheum , Ratos , Animais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Magnolia/química , Microbioma Gastrointestinal/efeitos dos fármacos , Constipação Intestinal/tratamento farmacológico , Constipação Intestinal/metabolismo , Masculino , Rheum/química , Fezes/microbiologia , Fezes/química , Cromatografia Líquida de Alta Pressão , Metabolômica , Rizoma/química , Metaboloma/efeitos dos fármacos , MultiômicaRESUMO
The aim of the experiment was to determine the yield of Miscanthus × giganteus M 19 in the first three years of cultivation and its bioaccumulation of Zn and Ni in aboveground and underground parts in response to different doses of sewage sludge and substrate left after the production of white mushrooms. Miscanthus × giganteus is a grass species that adapts to different environmental conditions and can be grown in various climatic zones of Europe and North America. In April 2018 the experiment was established in a randomized block design and with four replications in central-eastern Poland. Waste organic materials (municipal sewage sludge and mushroom substrate) were applied to the soil in 2018 in the spring before the rhizomes of giant miscanthus were planted. Each year (from 2018 to 2020) biomass was harvested in December. The yield of fresh and dry matter and the total content of Zn and Ni, after wet mineralization of plant samples, were determined by optical emission spectrometry (ICP-OES). After the third year of cultivation, the content of Zn and Ni in rhizomes and in the soil was determined again. In relation to control, an increase in the yield of miscanthus biomass in response to organic waste materials was noted. Plants responded to mushroom substrate (SMS) with the highest average yield (16.89 Mgha-1DM), while on the control plot it was 13.86 Mg ha-1DM. After the third year of cultivation, rhizomes of Miscanthus x giganteus contained higher amounts of Zn (63.3 mg kg-1) and Ni (7.54 mg kg-1) than aboveground parts (40.52 and 2.07 mg kg-1), which indicated that heavy metals were retained in underground parts.
Assuntos
Biomassa , Níquel , Poaceae , Esgotos , Solo , Zinco , Poaceae/metabolismo , Níquel/análise , Zinco/análise , Zinco/metabolismo , Solo/química , Agaricales/metabolismo , Agaricales/química , Rizoma/metabolismo , Rizoma/química , PolôniaRESUMO
Among all types of cancer, breast cancer is the most aggressive, as it is responsible for most of the cancer related death of women. Though several medical therapies are available, the scenario of curing such disease is not favorable. Therefore, there is an urgent need to find alternatives to deal with it. The knowledge of ethnopharmacy might give some better solution to mitigate such deadly diseases. Here, we are using the rhizome of Curcuma caesia Roxb. (Black turmeric), as well as gold nanoparticles (GNPs) synthesized with it to check their specific cytotoxic potentiality against breast cancer cell lines. In our study, ethanolic extract was used to evaluate the cytotoxic effect of the rhizome. GNPs were synthesized by using the same extract and characterized by UV-Vis spectroscopy (UV-Vis), Transmission electron microscopy (TEM), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), and Thermo gravimetric analysis (TGA). The TEM, XRD, FTIR and TGA results revealed the successful synthesis and capping of GNPs. The UV-Vis Spectrum showed a sharp and narrow absorption peak at 550 nm and HRTEM confirmed both the stability and successful synthesis of the nanoparticles. The MTT assay of the crude extract revealed strong cytotoxicity against breast cancer cell lines viz. MCF-7 (ER+) and MDA MB-231 (Triple Negative Breast Cancer, TNBC) by showing IC50 values as 15.70 ± 0.029 and 21.57 ± 0.031 µg/mL respectively. For extract mediated GNPs, the IC50 values were found to be 6.44 ± 0.045 and 5.87 ± 0.031µg/mL respectively in both breast cancer cell lines. As the IC50 value for GNPs was found to be much lower than that of crude extract, it indicates a higher efficiency of the GNP. However, both the rhizome extract and its mediated GNPs showed more toxicity towards MDA MB-231 (TNBC) cell lines. It was also observed that the GNPs showed more toxicity towards TNBC cell lines compared to the rhizome extract. No toxicity was found in case of other cell lines such as L 929 and HeLa for both crude extract as well as for GNPs. These observations suggests that both the crude rhizome extract and its derived GNPs exhibit selective cytotoxic potential against breast cancer cell lines, which might be exploited for target specific treatment. Moreover, with an understanding of the mechanism behind the GNPs therapeutic efficiency, it can be developed as a personalized therapy to treat such type of cancers.
Assuntos
Neoplasias da Mama , Curcuma , Ouro , Nanopartículas Metálicas , Extratos Vegetais , Rizoma , Humanos , Curcuma/química , Ouro/química , Ouro/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Nanopartículas Metálicas/química , Rizoma/química , Feminino , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Linhagem Celular Tumoral , Células MCF-7 , Sobrevivência Celular/efeitos dos fármacos , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/química , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
Alpinia officinarum Hance is rich in carbohydrates and is flavored by natives. The polysaccharide fraction 30 is purified from the rhizome of A. officinarum Hance (AOP30) and shows excellent immunoregulatory ability when administered to regulate immunity. However, the effect of AOP30 on the intestinal epithelial barrier is not well understood. Therefore, the aim of this study is to investigate the protective effect of AOP30 on the intestinal epithelial barrier using a lipopolysaccharide (LPS)-induced intestinal epithelial barrier dysfunction model and further explore its underlying mechanisms. Cytotoxicity, transepithelial electrical resistance (TEER) values, and Fluorescein isothiocyanate (FITC)-dextran flux are measured. Simultaneously, the protein and mRNA levels of tight junction (TJ) proteins, including zonula occludens-1 (ZO-1), Occludin, and Claudin-1, are determined using Western blotting and reverse-transcription quantitative polymerase chain reaction methods, respectively. The results indicate that AOP30 restores the LPS-induced decrease in the TEER value and cell viability. Furthermore, it increases the mRNA and protein expression of ZO-1, Occludin, and Claudin-1. Notably, ZO-1 is the primary tight junction protein altered in response to LPS-induced intestinal epithelial dysfunction. Additionally, AOP30 downregulates the production of TNFα via the Toll-like receptor 4 (TLR4)/NF-κB signaling pathway. Collectively, the findings of this study indicate that AOP30 can be developed as a functional food ingredient or natural therapeutic agent for addressing intestinal epithelial barrier dysfunction. It sheds light on the role of AOP30 in improving intestinal epithelial function.
Assuntos
Alpinia , Mucosa Intestinal , Lipopolissacarídeos , NF-kappa B , Polissacarídeos , Rizoma , Transdução de Sinais , Receptor 4 Toll-Like , Receptor 4 Toll-Like/metabolismo , Humanos , NF-kappa B/metabolismo , Transdução de Sinais/efeitos dos fármacos , Rizoma/química , Polissacarídeos/farmacologia , Células CACO-2 , Alpinia/química , Mucosa Intestinal/efeitos dos fármacos , Mucosa Intestinal/metabolismo , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Junções Íntimas/efeitos dos fármacos , Junções Íntimas/metabolismoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: NOTOPTERYGII RHIZOMA ET RADIX (NRR), a traditional Chinese medicine (TCM), has been utilized in China for millennia. Thriving in high-altitude regions with cold climates, wild NRR has been heavily exploited for its significant economic worth, particularly in the medical sector. THE AIM OF THE REVIEW: This paper presents a comprehensive review of the botany, traditional uses, phytochemistry, analytical methods, quality control, processing methods, pharmacological effects, and pharmacokinetics of NRR. These findings offer valuable insights for future research endeavors and establish a solid groundwork for the judicious clinical utilization of NRR. MATERIALS AND METHOD: The related information for NRR comes from scientific databases (such as Baidu Scholar, CNKI, Google Scholar, PubMed, Science Direct, Web of Science, SciFinder Scholar, Chinese Herb Classics, Chinese Pharmacopoeia, PhD and MSC Dissertations, etc.). RESULTS: Currently, components isolated from NRR are identified as coumarins, volatile oils, organic acids, flavonoids, glycosides, polyacetylenes, and trace elements. Most compounds are analyzed using HPLC and GC techniques. NRR exhibits a broad spectrum of pharmacological effects, such as anti-inflammatory, analgesic, antipyretic, antitumor, antiviral, antibacterial, immunosuppressive activities, as well as promoting blood circulation, removing blood stasis, providing neuroprotection, and liver protection. CONCLUSION: The research on NRR in phytochemistry and pharmacology has made great progress, and some traditional uses have been proven by modern pharmacology. However, because the complex chemical composition of NRR has not been effectively related to its pharmacological action, its mechanism of action has not been clearly expounded. In this review, the processing methods of NRR are summarized, and the exploration of further strengthening the processing mechanism of NRR is put forward, which provides some theoretical help for the clinical application of NRR. Furthermore, the complex chemical composition of NRR makes quality control difficult, so we must study its quality control thoroughly. In order to better develop and utilize NRR, we should establish a reasonable, reliable, and accurate quality control standard, and focus on the relationship between its active components and pharmacodynamic indicators and the study of its mechanism of pharmacological effects.
Assuntos
Medicamentos de Ervas Chinesas , Medicina Tradicional Chinesa , Compostos Fitoquímicos , Medicamentos de Ervas Chinesas/farmacocinética , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/química , Humanos , Animais , Compostos Fitoquímicos/farmacocinética , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/análise , Apiaceae/química , Etnofarmacologia , Rizoma/química , Raízes de Plantas/química , FitoterapiaRESUMO
Seven undescribed benzoate glycosides (1-7) and five known ones (8-12) were isolated from the rhizomes of Gentiana scabra Bge. Their structures were characterized by comprehensive NMR and MS spectroscopic data analysis. The lipid-lowering effects of these compounds were evaluated by measuring the triglyceride (TG) contents and intracellular lipid droplets (LDs) in oleic acid (OA)-treated HepG2 cells. The results showed that compounds 1, 5, 7, and 11 significantly reduced the TG content at 20 µM, and the Bodipy staining displayed that OA enhanced the levels of LDs in the cell, while these compounds reversed the lipid accumulation caused by OA. These findings provide a basis for further development and utilization of G. scabra as a natural source of potential lipid-lowering agents.
Assuntos
Gentiana , Glicosídeos , Hipolipemiantes , Glicosídeos/farmacologia , Glicosídeos/química , Glicosídeos/isolamento & purificação , Humanos , Gentiana/química , Células Hep G2 , Hipolipemiantes/farmacologia , Hipolipemiantes/química , Hipolipemiantes/isolamento & purificação , Benzoatos/farmacologia , Benzoatos/química , Benzoatos/isolamento & purificação , Estrutura Molecular , Ácido Oleico/farmacologia , Ácido Oleico/química , Relação Estrutura-Atividade , Relação Dose-Resposta a Droga , Triglicerídeos , Rizoma/químicaRESUMO
In this experiment, the eutrophication system was established by adding sucrose and yeast powder, and the pH and dissolved oxygen were measured in a bioreactor in real time to study the effect of aerobic environment on the fermentation process of Polygonati Rhizoma extract by Lactiplantibacillus plantarum. To further analyze metabolic changes, UPLC-Q-Exactive MS was used for metabolomic analysis and metabolic profiling. Multivariate analysis was performed using principal component analysis and Orthogonal projections to latent structures discriminant analysis. Finally, 313 differential metabolites were selected, 196 of which were annotated through database matching. After fermentation, the content of short-chain fatty acids, lactic acid, and their derivatives increased significantly, and there were 13 kinds and 4 kinds, respectively. Both compounds and their derivatives are beneficial to the intestinal flora. Consequently, incorporating L. plantarum into the aerobic fermentation process of Polygonati Rhizoma extract within the eutrophic system is potentially advantageous in enhancing the impact of its fermentation solution on the gut microbiota and its effects on human health. Our findings for this kind of edible and medicinal material research and development offer useful insights.
Assuntos
Fermentação , Lactobacillus plantarum , Polygonatum , Rizoma , Polygonatum/química , Polygonatum/metabolismo , Rizoma/química , Lactobacillus plantarum/metabolismo , Eutrofização , Extratos Vegetais/metabolismo , Extratos Vegetais/química , Ácido Láctico/metabolismo , Ácidos Graxos Voláteis/metabolismo , Reatores Biológicos/microbiologia , Microbioma Gastrointestinal , MetabolômicaRESUMO
This paper presents the initial exploration of the free radical scavenging capabilities of peptides derived from protein hydrolysates (PPH) obtained from Zingiber cassumunar rhizomes (Phlai). To replicate the conditions of gastrointestinal digestion, a combination of pepsin and pancreatin proteolysis was employed to generate these hydrolysates. Subsequently, the hydrolysate underwent fractionation using molecular weight cut-off membranes at 10, 5, 3, and 0.65 kDa. The fraction with a molecular weight less than 0.65 kDa exhibited the highest levels ABTS, DPPH, FRAP, and NO radical scavenging activity. Following this, RP-HPLC was used to further separate the fraction with a molecular weight less than 0.65 kDa into three sub-fractions. Among these, the F5 sub-fraction displayed the most prominent radical-scavenging properties. De novo peptide sequencing via quadrupole-time-of-flight-electron spin induction-mass spectrometry identified a pair of novel peptides: Asp-Gly-Ile-Phe-Val-Leu-Asn-Tyr (DGIFVLNY or DY-8) and Ile-Pro-Thr-Asp-Glu-Lys (IPTDEK or IK-6). Database analysis confirmed various properties, including biological activity, toxicity, hydrophilicity, solubility, and potential allergy concerns. Furthermore, when tested on the human adenocarcinoma colon (Caco-2) cell line, two synthetic peptides demonstrated cellular antioxidant activity in a concentration-dependent manner. These peptides were also assessed using the FITC Annexin V apoptosis detection kit with PI, confirming the induction of apoptosis. Notably, the DY-8 peptide induced apoptosis, upregulated mRNA levels of caspase-3, -8, and -9, and downregulated Bcl-2, as confirmed by real-time quantitative polymerase chain reaction (RT-qPCR). Western blot analysis indicated increased pro-apoptotic Bax expression and decreased anti-apoptotic Bcl-2 expression in Caco-2 cells exposed to the DY-8 peptide. Molecular docking analysis revealed that the DY-8 peptide exhibited binding affinity with Bcl-2, Bcl-xL, and Mcl-1, suggesting potential utility in combating colon cancer as functional food ingredients.
Assuntos
Apoptose , Neoplasias do Colo , Peptídeos , Rizoma , Transdução de Sinais , Humanos , Apoptose/efeitos dos fármacos , Rizoma/química , Células CACO-2 , Transdução de Sinais/efeitos dos fármacos , Peptídeos/farmacologia , Peptídeos/química , Neoplasias do Colo/tratamento farmacológico , Neoplasias do Colo/patologia , Neoplasias do Colo/metabolismo , Zingiberaceae/química , Adenocarcinoma/tratamento farmacológico , Adenocarcinoma/patologia , Adenocarcinoma/metabolismo , Antineoplásicos/farmacologia , Antineoplásicos/química , Sequestradores de Radicais Livres/farmacologia , Sequestradores de Radicais Livres/químicaRESUMO
Ethnomedicinally, more than 2000 plants were found to be used in Nepal. Among them, the red colored rhizome of Angiopteris helferiana and the bark of Saurauia fasciculata have been used widely to treat muscle fatigue, bone pain, fever, postpartum hemorrhage, and thirst by healers in Kaski and Tanahun districts, Nepal. However, scientific evidence towards their traditional uses is lacking till December, 2023. Therefore, we report the phytochemicals, total phenolic content (TPC), total flavonoid content (TFC), total carbohydrate content (TCC), antioxidant and antibacterial activities of A. helferiana and S. fasciculata extracts. Phytochemical analysis indicated that A. helferiana and S. fasciculata extracts were potential sources of chemicals such as phenols, flavonoids, tannins, terpenoids, saponins, and carbohydrates. The TPC, TFC, and TCC of extracts were determined by using an ultraviolet visible spectrophotometer. Among the extracts tested, A. helferiana extracts showed the highest phenolic and carbohydrate contents of 208.33 ± 12.96 mg of gallic acid equivalent/g and 564.16 ± 2.92 mg of D-glucose equivalent/g of dry extract, respectively. Similarly, S. fasciculata revealed the highest flavonoid content of 30.35 ± 0.1 mg quercetin equivalent/g of dry extract. The extract of A. helferiana and S. fasciculata exhibited potent antioxidant activity by scavenging 2,2-diphenyl-1-picrylhydrazyl radicals with an IC50 of 25.9 µg/ml and 31.07 µg/ml, respectively. The antibacterial activity of the A. helferiana and S. fasciculata extract against Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli was determined using an agar-well diffusion protocol that revealed the potential antibacterial activity of A. helferiana against E. coli. The present study will help validate the traditional uses of A. helferiana rhizomes and S. fasciculata barks as a healing medicine and inspire the researcher towards further research, development, and formulation.
Assuntos
Antibacterianos , Antioxidantes , Compostos Fitoquímicos , Casca de Planta , Extratos Vegetais , Rizoma , Antioxidantes/farmacologia , Antioxidantes/química , Antibacterianos/farmacologia , Antibacterianos/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Casca de Planta/química , Rizoma/química , Nepal , Flavonoides/análise , Flavonoides/química , Testes de Sensibilidade Microbiana , Fenóis/análise , Fenóis/químicaRESUMO
BACKGROUND: Asthma is a complex disease with mechanisms involving multiple factors, and there is still a lack of highly effective and low-side-effect drugs. Traditional Chinese medicine Fagopyrum Dibotrys Rhizoma (FDR) has been applied for the treatment of acute and chronic bronchitis as well as bronchial asthma due to its favorable pharmacological activity. However, the exact mechanism of FDR remains unclear. OBJECTIVE: A mouse model of asthma was created using OVA and HDM. To investigate the mechanism of FDR in asthma treatment, a combination of network pharmacology, lipidomics, and molecular biology approaches was employed. METHODS: To evaluate the therapeutic effects of FDR on asthma, we established two distinct models of asthma in C57BL/6 J mice using OVA and HDM, respectively. We then employed LC-MS to analyze the major chemical constituents in FDR. Next, the network pharmacology approach was used to predict the potential targets and mechanisms of FDR in asthma treatment. Additionally, lipidomics analysis of mouse serum was conducted using LC-MS. Finally, the impact of FDR on the ERK -cPLA2 signaling pathway was investigated through Western Blotting assay. RESULTS: FDR treatment has been shown to improve histomorphological changes, lung function and inflammation in models of OVA and HDM-induced asthma. Using UPLC/LTQ-Orbitrap-MS, we were able to identify 12 potential active components. Network pharmacology analysis revealed that FDR shares 75 targets with asthma. Further analysis using GO and KEGG pathways demonstrated the involvement of key pathways such as PI3K-Akt, TNF, and MAPK. Additionally, lipidomics analysis of the serum from OVA and HDM induced asthma mice showed disturbances in lipid metabolism, which were effectively ameliorated by FDR treatment. Mechanistically, FDR inhibits ERK1/2-cPLA2, leading to a reduction in lysophospholipids and restoration of lipid balance, thereby aiding in the treatment of asthma. CONCLUSION: FDR has been shown to improve lipid metabolism disorder in the serum of asthmatic mice, thereby potentially serving as a treatment for asthma. This can be achieved by regulating the activation levels of ERK1/2 and p38MAPK. Consequently, the production of lysophosphatide is reduced, thereby alleviating the disorder of lipid metabolism and achieving the desired therapeutic effect in asthma treatment.
Assuntos
Asma , Modelos Animais de Doenças , Fagopyrum , Metabolismo dos Lipídeos , Camundongos Endogâmicos C57BL , Rizoma , Animais , Asma/tratamento farmacológico , Metabolismo dos Lipídeos/efeitos dos fármacos , Rizoma/química , Camundongos , Fagopyrum/química , Pulmão/efeitos dos fármacos , Pulmão/metabolismo , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Feminino , Medicamentos de Ervas Chinesas/farmacologia , Homeostase/efeitos dos fármacos , Lipidômica , Transdução de Sinais/efeitos dos fármacos , Farmacologia em Rede , Ovalbumina , Fosfolipases A2/metabolismoRESUMO
Green products such as plant tints are becoming more and more well-known worldwide due to their superior biological and ayurvedic properties. In this work, colorant from Amba Haldi (Curcuma aromatica) was isolated using microwave (MW), and bio-mordants were added to produce colorfast shades. Response surface methodology was used to develop a central composite design (CCD), which maximizes coloring variables statistically. The findings from 32 series of experiments show that excellent color depth (K/S = 12.595) was established onto MW-treated silk fabric (RS = 4 min) by employing 65 mL of radiated aqueous extract (RE = 4 min) of 5 pH cutting-edge the existence of 1.5 g/100 mL used sodium chloride at 75 °C for 45 min. It was discovered that acacia (keekar) extract (1%), pomegranate extract (2%), and pistachio extract (1.5%) were present before coloring by the use of bio-mordants. On the other hand, upon dyeing, acacia extract (1.5%), pomegranate extract (1.5%), and pistachio extract (2%) have all shown extremely strong colorfast colors. Comparatively, before dyeing, salts of Al3+ (1.5%), Fe2+ (2%), and TA (1.5%) gave good results; after dyeing, salts of Al3+ (1%) and Fe2+ (1.5%) and TA (2%) gave good results. When applied to silk fabric, MW radiation has increased the production of dyes recovered from rhizomes. Additionally, the right amount of chemical and biological mordants have been added, resulting in color fastness ratings ranging from outstanding to good. Therefore, the natural color extracted from Amba Haldi can be a sustainable option for the dyeing of silk fabric in the textile dyeing and finishing industries.
Assuntos
Corantes , Curcuma , Extratos Vegetais , Rizoma , Seda , Curcuma/química , Rizoma/química , Corantes/química , Extratos Vegetais/química , Seda/química , Micro-Ondas , Cor , Química Verde/métodosRESUMO
Tormentilla erecta (L.) Raeusch is a widespread plant in Europe and Western Asia. Its rhizomes (Tormentilae rhizoma) are the main ingredient of herbal alcoholic beverages and can be used as a natural preservative in beer production. Apart from its unique taste qualities, therapeutic properties in gastrointestinal tract ailments are attributed to the tincture obtained from Tormentillae rhizoma. The presented research aimed to determine the mutual relationship between the components of Tormentillae tincture, present in popular alcoholic beverages, and intestinal epithelium (Caco-2 cell monolayers). A comprehensive qualitative and quantitative analysis of the tincture was performed, including the determination of condensed and hydrolyzable tannins as well as triterpenoids (UHPLC-DAD-MS/MS). Incubation of the tincture with Caco-2 monolayers has shown that only triterpenes pass through the monolayer, while condensed tannins are mainly bound to the monolayer surface. Ellagic acid derivatives were the only components of the Tormentillae tinctura being metabolized by cell monolayers to the compounds not previously described in the literature, which may be crucial in the treatment of intestinal diseases with inflammatory background.