RESUMEN
Chronic obstructive pulmonary disease (COPD) is a common and frequently-occurring disease of the respiratory system, characterized by persistent respiratory symptoms and airflow restriction, which is prone to attack repeatedly and affect patients' quality of life seriously. At present, the combination of bronchodilators and inhaled corticosteroids is commonly used in clinic. Although these drugs can alleviate the symptoms of COPD patients, there are certain limitations of the difficulty in controlling the course of the disease effectively and reversing the decline of patients' lung function. Therefore, searching for safer and more effective therapeutic drugs has become a hot research topic nowadays. Traditional Chinese medicine (TCM) has remarkable curative effects and advantages in the prevention and therapy of COPD recently. Based on the increasing research and application of the active components of TCM in the therapy of COPD, studies on their pharmacodynamic mechanism are also more in depth. More and more studies have found that the active components of TCM can treat COPD patients effectively, and the mechanism involved mainly includes the anti-inflammatory, the antioxidant, and the inhibition of apoptosis. By searching and screening the domestic and foreign literatures on the treatment of COPD with the active components of TCM in recent years, the active components of TCM including flavonoids, terpenoids, phenols and saponins have been studied as the research objects, and their effects in improving the pulmonary function and oxidative stress, relieving inflammation and inhibiting apoptosis are expounded. Besides, the mechanism of action, signaling pathways and index molecules have been emphatically summarized, in order to provide the ideas for the clinical therapy and the basic research of COPD.
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Rheum palmatum L. (RPL) is a known traditional herbal medicine with the functions of "heat-clearing and damp-drying" in traditional Chinese medicine. Its anti-cancer effect against lung cancer has been confirmed previously, but the related mechanisms and active substances for its action has been little studied. This study adopted the network pharmacology, built the network map of drug ingredients and disease targets (DDN), and discussed the effective components of RPL and its possible mechanisms. All constituents of RPL were collected through database search and literature mining, and the potential active constituents were screened. The inverse pharmacophore matching model was used to predict the targets of active ingredients, and the method was supplemented by database retrieval and literature mining. Compounds-target data were inputted into Cytoscape software to build the DDN of RPL, and functional annotation analysis and pathway enrichment analysis were carried out. Finally, 20 active compounds were screened, which acted on 817 targets. A total of 22,418 lung cancer-related targets were collected, and 761 overlapped with drug targets. By bioinformatics annotation of these overlapping genes, a total of 235 gene ontology (GO) functional annotation analyses and 46 Kyoto Encyclopedia of Genes and Genomes (KEGG) pathways were obtained. It was found that the enrichment of GO and KEGG was associated with apoptosis, suggesting RPL plays an anti-lung cancer role via inducing cell apoptosis. Subsequent cell experiment results showed RPL and its active constituents inhibited the proliferation of A549 cells and reduced clone formation rate of A549 cells via induction of apoptosis. In this study, the pharmacodynamic basis and mechanism of RPL against lung cancer were studied from the perspective of systematic pharmacology, which would be beneficial for further elucidating the anticancer effect of RPL on lung cancer.
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OBJECTIVE@#Critical effective constituents were identified from Bufei Yishen formula (BYF), a traditional herbal compound and combined as effective-constituent compatibility (ECC) of BYF I, which may have potential bioactive equivalence to BYF.@*METHODS@#The active constituents of BYF were identified using four cellular models and categorised into Groups 1 (Bufeiqi), 2 (Bushen), 3 (Huatan) and 4 (Huoxue) according to Chinese medicinal theory. An orthogonal design and a combination method were used to determine the optimal ratios of effective constituents in each group and the ratios of "Groups 1 to 4" according to their pharmacological activity. We also comprehensively assessed bioactive equivalence between the BYF and the ECC of BYF I in a rat model of chronic obstructive pulmonary disease (COPD).@*RESULTS@#We identified 12 active constituents in BYF. The numbers of constituents in Groups 1 to 4 were 3, 2, 5 and 2, respectively. We identified the optimal ratios of effective constituents within each group. In Group 1, total ginsenosides:Astragalus polysaccharide:astragaloside IV ratio was 9:5:2. In Group 2, icariin:schisandrin B ratio was 100:12.5. In Group 3, nobiletin:hesperidin:peimine:peiminine:kaempferol ratio was 4:30:6.25:0:0. In Group 4, paeoniflorin:paeonol ratio was 4:1. An orthogonal design was then used to establish the optimal ratios of Group 1, Group 2, Group 3 and Group 4 in ECC of BYF I. The ratio for total ginsenosides:Astragalus polysaccharide:astragaloside IV:icariin:schisandrin B:nobiletin:hesperidin:peimine:paeoniflorin:paeonol was determined to be 22.5:12.5:5:100:12.5:4:30:6.25:25:6.25. A comprehensive evaluation confirmed that ECC of BYF I presented with bioactive equivalence to the original BYF.@*CONCLUSION@#Based on the ECC of traditional Chinese medicine formula method, the effective constituents of BYF were identified and combined in a fixed ratio as ECC of BYF I that was as effective as BYF itself in treating rats with COPD.
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The family Gentianaceae are found mostly on the Qinghai-Tibet Plateau in China, which have important medicinal properties. Based on 27 published complete chloroplast genome sequences from Gentiana, Swertia, Halenia, Menyanthes, and Nymphoides of Gentianaceae, the chloroplast genome structure was analyzed. The cp genome sizes of 27 taxa range from 137 to 154 kb, and they contain 101-114 unique genes, including 67-80 protein-coding genes, 30 tRNA genes and four rRNA genes. Also, a Bayesian phylogenetic tree was constructed based on the 27 cp genome sequences with Pentalinon luteum (Apocynaceae) as the outgroup. The tree was topologically consistent with the treatments of traditional taxonomy, and the cp genome sequences have genus- or section-level resolution. In addition, we reviewed the significance of species identification within the family. These cp genome sequences could provide basic data for the endangered species conservation, the genetic analysis and pharmacognostic researches of herbs from Gentianaceae.
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The aberrant activation of PI3K/Akt/mTOR signaling pathway plays an important role in the oncogenesis, prognosis and chemotherapy resistance of neuroblastoma. However, NVP-BEZ235, a potent dual PI3K and mTOR inhibitor have not shown beneficial effects on neuroblastoma especially in terms of apoptosis induction as a single agent. We therefore attempted to explore an effective combination regimen to enhance the anticancer activity of NVP-BEZ235. Interestingly, we found that oridonin, a natural biologically active compound extracted from the Chinese medicinal herb Rabdosia rubescens, combined with NVP-BEZ235 markedly induced apoptosis of neuroblastoma cells. Notably, the synergistic activation of the apoptotic pathway was accompanied with enhanced autophagy as evidenced by significant decreased p62 expression as well as upregulated conversion of LC3-II. Suppression of the Beclin-1, a core component of the autophagy machinery, by means of shRNA resulted in diminished synergistic antitumor effect. Furthermore, the co-treatment with oridonin and NVP-BEZ235 was also much more effective than either agent alone in inhibiting the growth of neuroblastoma xenografts and in inducing tumor cells apoptosis. Taken together, our results suggest that the combination of NVP-BEZ235 and oridonin is a novel and potential strategy for neuroblastoma therapy.
Asunto(s)
Autofagia/efectos de los fármacos , Diterpenos de Tipo Kaurano/administración & dosificación , Imidazoles/administración & dosificación , Neuroblastoma/tratamiento farmacológico , Quinolinas/administración & dosificación , Animales , Protocolos de Quimioterapia Combinada Antineoplásica , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Resistencia a Antineoplásicos/genética , Humanos , Ratones , Neuroblastoma/genética , Neuroblastoma/patología , Inhibidores de las Quinasa Fosfoinosítidos-3 , Serina-Treonina Quinasas TOR/antagonistas & inhibidores , Ensayos Antitumor por Modelo de XenoinjertoRESUMEN
Due to the complications of Chinese materia medica (CMM) and its preparations, traditional sampling methods have some limitations and affect the analysis on the ingredients of CMM. The review mainly introduced the principles, system compositions, characteristics of the microdialysis technique according to 70 literatures in the late 10 years, especially its applications on the analysis on CMM in vivo, such as in brain, skin, blood, eyes, intestinal, joint, liver, gallbladder kidney, and lung. Among these organs, brain and skin studies have more experiences. As a sampling method, microdialysis technique can not only reveal the change process of ingredients in CMM, but also can help the development of targeted drug delivery, which has the great value and good perspective in the modernization study on CMM.
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OBJECTIVE: To study optimum inclusion conditions for volatile oil from three medicinal slices in Xiongdan Xiaoyan capsules. METHOD: Saturated water solution method (agitation method), ultrasonic method and rubbing method were studied and compared. The preparation conditions of ultrasonic method were investigated by the orthogonal test. RESULT: The optimum inclusion conditions of ultrasonic method were established. CONCLUSION: The ultrasonic method can be used for production of inclusion complex in the factory with high inclusion rate and was effectiveness.