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The effect of vitamin K on clinical outcomes in patients receiving kidney transplantation is contested according to previous studies. This meta-analysis aimed to summarize the impact of vitamin K on all-cause mortality, renal function, inflammation, and vascular/bone health in patients receiving kidney transplantation. EMBASE, PubMed, and Cochrane were searched for literature concerning the effect of vitamin K on clinical outcomes of patients receiving kidney transplantation until December 2022. Normal vitamin K status/vitamin K supplementation was considered as the experimental group; while vitamin K deficiency/no vitamin K supplementation was considered as the control group. All-cause mortality, renal function indexes, C-reactive protein (CRP), and vascular/bone health indexes were extracted and analyzed. A total of seven studies with 1,101 patients in the experimental group and 651 patients in the control group were included. All-cause mortality was decreased in the experimental group vs. the control group [relative risk (95% confidence interval (CI)]: 0.72 (0.60-0.86), P<0.001]. Regarding renal function indexes, the estimated glomerular filtration rate was increased in the experimental group vs. the control group [mean difference (95% CI): 9.87 (1.48-18.26), P=0.021]; while creatinine and albumin remained unchanged between the two groups (both P>0.05). Moreover, CRP, systolic blood pressure, diastolic blood pressure, triglycerides, hemoglobin, calcium, and 25-hydroxyvitamin D were unchanged between the two groups (all P>0.05). Publication bias was low, and the robustness assessed by sensitivity analysis was generally acceptable. Thus vitamin K exerted a potential implication in reducing all-cause mortality and improving renal function in patients receiving kidney transplantation.
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The presence of microorganisms on biomedical devices and food packaging surfaces poses an important threat to human health. Superhydrophobic surfaces, a powerful tool to combat pathogenic bacterial adhesion, are threatened by their poor robustness. As a supplement, photothermal bactericidal surfaces may be expected to kill adhered bacteria. Using copper mesh as a mask, we prepared a superhydrophobic surface with a homogeneous conical array. The surface shows synergistic antibacterial properties, including a superhydrophobic character against bacterial adhesion and photothermal bactericidal activity. As a result of the excellent liquid repellency, the surface could highly repel the adherence of bacteria after immersing in a bacterial suspension for 10 s (95%) and 1 h (57%). Photothermal graphene can easily eliminate most adhered bacteria during the subsequent treatment of near-infrared (NIR) radiation. After a self-cleaning wash, the deactivated bacteria were easily rinsed off the surface. Furthermore, this antibacterial surface exhibited an approximately 99.9% resisted bacterial adhesion rate regardless of planar and various uneven surfaces. The results offer promising advancement of an antibacterial surface combining both adhesion resistance and photothermal bactericidal activity in fighting microbial infections.
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Antibacterianos , Aderência Bacteriana , Humanos , Antibacterianos/farmacologia , Antibacterianos/química , BactériasRESUMO
Quercetin (QR) has significant anti-respiratory syncytial virus (RSV) effects. However, its therapeutic mechanism has not been thoroughly explored. In this study, a lung inflammatory injury model caused by RSV was established in mice. Untargeted lung tissue metabolomics was used to identify differential metabolites and metabolic pathways. Network pharmacology was used to predict potential therapeutic targets of QR and analyze biological functions and pathways modulated by QR. By overlapping the results of the metabolomics and the network pharmacology analyses, the common targets of QR that were likely to be involved in the amelioration of RSV-induced lung inflammatory injury by QR were identified. Metabolomics analysis identified 52 differential metabolites and 244 corresponding targets, while network pharmacology analysis identified 126 potential targets of QR. By intersecting these 244 targets with the 126 targets, hypoxanthine-guanine phosphoribosyltransferase (HPRT1), thymidine phosphorylase (TYMP), lactoperoxidase (LPO), myeloperoxidase (MPO), and cytochrome P450 19A1 (CYP19A1) were identified as the common targets. The key targets, HPRT1, TYMP, LPO, and MPO, were components of purine metabolic pathways. The present study demonstrated that QR effectively ameliorated RSV-induced lung inflammatory injury in the established mouse model. Combining metabolomics and network pharmacology showed that the anti-RSV effect of QR was closely associated with purine metabolism pathways.
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Medicamentos de Ervas Chinesas , Lesão Pulmonar , Pneumonia Viral , Infecções por Vírus Respiratório Sincicial , Vírus Sincicial Respiratório Humano , Humanos , Camundongos , Animais , Quercetina/farmacologia , Quercetina/uso terapêutico , Farmacologia em Rede , Lesão Pulmonar/tratamento farmacológico , Pulmão/metabolismo , Metabolômica/métodos , Medicamentos de Ervas Chinesas/farmacologiaRESUMO
The evaluation of germplasm resources is the prerequisite for the development, utilization, and conservation of Chinese medicinal resources. The selection of excellent germplasm is the key to the breeding and orderly production of Pinellia ternata. In this study, 21 germplasm materials of P. ternata from major production areas in China were collected and analyzed for population diversity after phenotypic preliminary screening. The results have revealed that the P. ternata population has abundant phenotypic variation, and the phenotypic changes could be divided into five phenotypes in terms of organ trait variation. Further analysis of variation in 20 quantitative traits of the population revealed that the coefficient of variation for adenosine content(339.05%) was the largest, while the coefficient of variation for the underground plant height(16.35%) was the smallest. Correlation analysis showed that there was a strong correlation among various traits, with 52 pairs of traits showing highly significant correlation(P<0.01) and 19 pairs of traits showing a significant correlation(P<0.05). The 21 germplasms in the test could be classified into three major clusters by cluster analysis, with Cluster â ¡ having the highest number and content of nucleosides, making it suitable for the selection and breeding of P. ternata varieties with high content of nucleosides. The yield in Cluster â ¢ was higher than that in other groups, making it suitable for the selection and breeding of P. ternata varieties with a high yield. All trait indicators could be simplified into five principal component factors through principal component analysis, and the cumulative contribution rate was up to 86.04%. Further, comprehensive analysis using membership function and stepwise regression analysis identified nine traits, such as plant height, main leaf length, and underground plant height as characteristic indicators for the comprehensive evaluation of germplasm resources of P. ternata. BX007, BX008, and BX005 were identified as germplasms with both high yield and high uridine content, with BX007 having the highest uridine content of 479.51 µg·g~(-1). It belonged to the germplasm of P. ternata with double bulbils and could be cultivated as a potential good variety. Based on the phenotypic classification of P. ternata, systematic resource evaluation was carried out in this study, which could lay a foundation for the excavation of genetic resources and the breeding of new varieties of P. ternata.
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Pinellia , Plantas Medicinais , Pinellia/genética , Melhoramento Vegetal , Fenótipo , UridinaRESUMO
Salvia chinensia Benth (Shijianchuan in Chinese, SJC) has been used as a traditional anti-cancer herb. SJC showed good anti-esophageal cancer efficacy based on our clinical application. However, the current research on SJC is minimal, and its anti-cancer effect lacks scientific certification. This study aims to clarify the inhibitory effect of SJC on esophageal cancer and explore its underlying mechanism. Q-Orbitrap high-resolution LC/MS was used to identify the primary chemical constituents in SJC. Cell proliferation and colony formation assays showed that SJC could effectively inhibit the growth of esophageal tumor cells in vitro. To clarify its mechanism of action, proteomic and bioinformatic analyses were carried out by combining tandem mass labeling and two-dimensional liquid chromatography-mass spectrometry (LC-MS). Data are available via ProteomeXchange with identifier PXD035823. The results indicated that SJC could activate AMPK signaling pathway and effectively promote autophagy in esophageal cancer cells. Therefore, we further used western blotting to confirm that SJC activated autophagy in esophageal cancer cells through the AMPK/ULK1 signaling pathway. The results showed that P-AMPK and P-ULK1 were significantly up-regulated after the treatment with SJC. The ratio of autophagosomes marker proteins LC3II/I was significantly increased. In addition, the expression of the autophagy substrate protein P62 decreased with the degradation of autophagosomes. Using lentiviral transfection of fluorescent label SensGFP-StubRFP-LC3 protein and revalidation of LC3 expression before and after administration by laser confocal microscopy. Compared with the control group, the fluorescence expression of the SJC group was significantly enhanced, indicating that it promoted autophagy in esophageal cancer cells. Cell morphology and the formation of autophagosomes were observed by transmission electron microscopy. Our study shows that the tumor suppressor effect of SJC is related to promoting autophagy in esophageal tumor cells via the AMPK/ULK1 signaling pathway.
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Hepatocellular carcinoma (HCC) accounts for the predominant form of liver malignancy and presents a leading cause of cancer-related death globally. Sorafenib (SOR), a first-line targeted drug for advanced HCC treatment, has a battery of untoward side effects. Photothermal therapy (PTT) has been utilized as an effective adjuvant in synergy with other approaches. However, little is known about the tumoricidal efficacy of combining SOR with PTT for HCC. Herein, a novel versatile nanoparticle, Cu2-xSe@SOR@PEG (CSP), that is based on a photothermal Cu2-xSe core and SOR for simultaneously reinforcing PTT and reducing the adverse effects of SOR was constructed. The synthesized CSP exhibited a remarkably enhanced therapeutic effect upon 808 nm laser irradiation via dampening HCC cell propagation and metastasis and propelling cell apoptosis. The intravenous administration of CSP substantially suppressed tumor growth in a xenograft tumor mouse model. It was noted that the CSP manifested low toxicity and excellent biocompatibility. Together, this work indicates a promising and versatile tool that is based on synergistic PTT and molecular-targeted therapy for HCC management.
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Triple-negative breast cancer (TNBC) is the most aggressive breast cancer subtype with limited treatment options and a poor prognosis. TNBC exists widely reprogrammed lipid metabolism, and its metabolic-associated proteins and oncometabolites are promising as potential therapeutic targets. Dandelion (Taraxacum mongolicum) is a classical herbal medicine used to treat breast diseases based on traditional Chinese medicine theory and was reported to have antitumor effects and lipid regulatory capacities. Our previous study showed that dandelion extract was effective against TNBC. However, whether dandelion extract could regulate the lipid metabolisms of TNBC and exert its antitumor effects via interfering with lipids metabolism remained unclear. In this study, an integrated approach combined with network pharmacology and multi-omics techniques (including proteomics, metabolomics, and lipidomics) was performed to investigate the potential regulatory mechanisms of dandelion extract against TNBC. We first determined the antitumor effects of dandelion extract in vitro and in vivo. Then, network pharmacology analysis speculated the antitumor effects involving various metabolic processes, and the multi-omics results of the cells, tumor tissues, and plasma revealed the changes in the metabolites and metabolic-associated proteins after dandelion extract treatment. The alteration of glycerophospholipids and unsaturated fatty acids were the most remarkable types of metabolites. Therefore, the metabolism of glycerophospholipids and unsaturated fatty acids, and their corresponding proteins CHKA and FADS2, were considered the primary regulatory pathways and biomarkers of dandelion extract against TNBC. Subsequently, experimental validation showed that dandelion extract decreased CHKA expression, leading to the inhibition of the PI3K/AKT pathway and its downstream targets, SREBP and FADS2. Finally, the molecular docking simulation suggested that picrasinoside F and luteolin in dandelion extract had the most highly binding scores with CHKA, indicating they may be the potential CHKA inhibitors to regulate glycerophospholipids metabolisms of TNBC. In conclusion, we confirmed the antitumor effects of dandelion extract against TNBC cells in vitro and demonstrated that dandelion extract could interfere with glycerophospholipids and unsaturated fatty acids metabolism via downregulating the CHKA expression and inhibiting PI3K/AKT/SREBP/FADS2 axis.
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The current COVID-19 pandemic caused by SARS-Cov-2 is responsible for more than 6 million deaths globally. The development of broad-spectrum and cost-effective antivirals is urgently needed. Medicinal plants are renowned as a complementary approach in which antiviral natural products have been established as safe and effective drugs. Here, we report that the percolation extract of Spatholobus suberectus Dunn (SSP) is a broad-spectrum viral entry inhibitor against SARS-CoV-1/2 and other enveloped viruses. The viral inhibitory activities of the SSP were evaluated by using pseudotyped SARS-CoV-1 and 2, HIV-1ADA and HXB2 , and H5N1. SSP effectively inhibited viral entry and with EC50 values ranging from 3.6 to 5.1 µg/ml. Pre-treatment of pseudovirus or target cells with SSP showed consistent inhibitory activities with the respective EC50 value of 2.3 or 2.1 µg/ml. SSP blocked both SARS-CoV-2 spike glycoprotein and the host ACE2 receptor. In vivo studies indicated that there was no abnormal toxicity and behavior in long-term SSP treatment. Based on these findings, we concluded that SSP has the potential to be developed as a drug candidate for preventing and treating COVID-19 and other emerging enveloped viruses.
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Tratamento Farmacológico da COVID-19 , Virus da Influenza A Subtipo H5N1 , Antivirais/farmacologia , Humanos , Pandemias/prevenção & controle , SARS-CoV-2RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Marsdenia tenacissima (Roxb.) Wight et Arn. is a traditional Chinese herbal medicine, and its water-soluble ingredient Marsdenia tenacissima extract (MTE), was widely used for cancer treatment. The multi-pharmacological efficacies and mechanisms of MTE in directly inhibiting tumor cells have been extensively studied. However, the anti-tumor effects of MTE in the tumor-associated macrophages (TAMs) microenvironment remain unclear. AIM OF THE STUDY: To uncover the role of hepatoma-derived growth factor (HDGF) in the interaction between TAMs and non-small cell lung cancer (NSCLC) cells. To evaluate the anti-tumor effects of MTE on the vicious crosstalk between TAMs and NSCLC by targeting HDGF. MATERIALS AND METHODS: HDGF-overexpression PC-9 and H292 NSCLC cell lines were constructed and verified. RNA-sequencing (RNA-seq) was performed in HDGF-overexpression PC-9 cells to probe the differential expression of genes. THP-1-derived macrophages were characterized using specific markers after stimulation with phorbol-12-myristate 13-acetate (PMA) and rhIL-4 or rhHDGF. The role of HDGF both in NSCLC cells and TAMs was determined using approaches like Western blot, qRT-PCR, ELISA, and flow cytometry. The interaction between tumor cells and TAMs were assessed by indirect co-culture H1975, PC-9 cells with M2 type macrophages. The effects of MTE on anti-tumor and macrophage polarization were evaluated in vitro and in vivo. RESULTS: RNA-seq results identified IL-4 as a critical response to HDGF in NSCLC. HDGF induced macrophages polarizing toward M2 type, and promoted NSCLC cells proliferation, migration and invasion in vitro. On the one hand, HDGF dose-dependently promoted IL-4 expression in NSCLC cells. On the other hand, HDGF induced M2 macrophage polarization through the IL-4/JAK1/STAT3 signaling pathway. MTE treatment significantly decreased the expression and secretion of HDGF in NSCLC cells. Meanwhile, MTE treatment led to M2 macrophage repolarization, as evidenced by decreased expression of M2 markers and increased levels of M1 markers. Importantly, MTE treatment significantly suppressed tumor development in C57BL/6 mice bearing Lewis lung cancer (LLC) cells in vivo, accompanied by decreased plasma HDGF levels, reduced M2 macrophages infiltration and increased M1 macrophages proportion in mice tumor tissues. CONCLUSIONS: HDGF upregulated IL-4 expression in NSCLC cells, and promoted M2 polarization by the IL-4/JAK1/STAT3 signaling pathway in macrophages. MTE disturbed the interaction between NSCLC and TAMs in vitro, and inhibited tumor growth in vivo, at least in part, by suppressing HDGF. Therefore, our present study revealed a novel anti-tumor mechanism of MTE through inhibiting HDGF expression and enhancing macrophage polarization from M2 to M1 phenotype.
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Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Marsdenia , Animais , Carcinoma Pulmonar de Células não Pequenas/patologia , Linhagem Celular Tumoral , Peptídeos e Proteínas de Sinalização Intercelular , Interleucina-4 , Neoplasias Pulmonares/patologia , Camundongos , Camundongos Endogâmicos C57BL , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Microambiente Tumoral , Macrófagos Associados a TumorRESUMO
Although sorafenib, a multi-kinase inhibitor, has provided noteworthy benefits in patients with hepatocellular carcinoma (HCC), the inevitable side effects, narrow therapeutic window, and low bioavailability seriously affect its clinical application. To be clinically distinctive, innovative drugs must meet the needs of reaching tumor tissues and cause limited side effects to normal organs and tissues. Recently, photodynamic therapy, utilizing a combination of a photosensitizer and light irradiation, was selectively accumulated at the tumor site and taken up effectively via inducing apoptosis or necrosis of cancer cells. In this study, a nano-chemo-phototherapy drug was fabricated to compose an iridium-based photosensitizer combined with sorafenib (IPS) via a self-assembly process. Compared to the free iridium photosensitizer or sorafenib, the IPS exhibited significantly improved therapeutic efficacy against tumor cells because of the increased cellular uptake and the subsequent simultaneous release of sorafenib and generation of reactive oxygen species production upon 532 nm laser irradiation. To evaluate the effect of synergistic treatment, cytotoxicity detection, live/dead staining, cell proliferative and apoptotic assay, and Western blot were performed. The IPS exhibited sufficient biocompatibility by hemolysis and serum biochemical tests. Also, the results suggested that IPS significantly inhibited HCC cell proliferation and promoted cell apoptosis. More importantly, marked anti-tumor growth effects via inhibiting cell proliferation and promoting tumor cell death were observed in an orthotopic xenograft HCC model. Therefore, our newly proposed nanotheranostic agent for combined chemotherapeutic and photodynamic therapy notably improves the therapeutic effect of sorafenib and has the potential to be a new alternative option for HCC treatment.
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Antineoplásicos , Carcinoma Hepatocelular , Neoplasias Hepáticas , Nanocompostos , Fotoquimioterapia , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Apoptose , Carcinoma Hepatocelular/patologia , Linhagem Celular Tumoral , Proliferação de Células , Humanos , Irídio/farmacologia , Neoplasias Hepáticas/patologia , Nanocompostos/uso terapêutico , Fármacos Fotossensibilizantes/farmacologia , Fármacos Fotossensibilizantes/uso terapêutico , Sorafenibe/uso terapêuticoRESUMO
The antioxidant properties of Se-containing peptides from Cardamine enshiensis (SeCPPs) and their impact on gut microbiota were studied in d-galactose (d-gal)- injected mice and antibiotic-treated mice. The structures of SeCPPs were identified by UPLC-Q-Extractive Orbitrap MS. In d-gal ageing mice, SeCPPs were associated with significantly decreased acetyl cholinesterase (AchE) activity, malondialdehyde (MDA) content, increased glutathione peroxidase (GSH-Px) activity, downregulated tumour necrosis factor-α (TNF-α), interleukin-6 (IL-6) and interleukin-1ß (IL-1ß) levels (p < 0.05), and improved memory. In antibiotic-treated mice, SeCPPs were associated with reduced Proteobacteria and evaluated Akkermansia abundances (p < 0.01). Eighty-five Se-containing peptides were identified in SeCPPs. Peptides such as RV-SeM-I, RA-SeM-T and R-SeC-K showed low binding energy with 1,1-diphenyl-2-picrylhydrazyl (DPPH), and their binding affinities were confirmed by molecular docking. Overall, compared with Na2SeO3 and SeMet, SeCPPs showed superior antioxidant activity via their association with higher antioxidant enzyme activity, scavenging free radical properties and gut microbiome modulation.
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Cardamine , Microbioma Gastrointestinal , Selênio , Animais , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Cardamine/metabolismo , Galactose/metabolismo , Camundongos , Simulação de Acoplamento Molecular , Estresse Oxidativo , Peptídeos/metabolismo , Selênio/farmacologiaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The root of Angelica sinensis is widely used in traditional Chinese Medicine for relieving gynecological discomforts among the women population. However, its hormone-like effects have raised great attention on whether it is appropriate to use in breast cancer (BC) patients. Hence, this study aimed to investigate the tumorigenic effect of aqueous root extract of Angelica sinensis (AS) on estrogen receptor (ER)-positive BC growth through ER-induced stemness in-vitro and in-vivo. MATERIALS AND METHODS: The chemical composition of the AS was characterized by HPLC. Cell viability was detected by MTS assay. The in-vivo effect of AS was investigated by xenograft model, immunohistochemistry, histology, Western blot, and self-renewal ability assay. Target verification was used by shRNA construction and transfection. Mammosphere formation assay was performed by flow cytometry. RESULTS: AS significantly promoted the proliferation of MCF-7 cells and inhibited the growth of MDA-MB-231 cells. AS significantly induced tumor growth (2.5 mg/kg) in xenograft models and however tamoxifen treatment significantly suppressed the AS-induced tumor growth. AS induced ERα expression in both in-vivo and in-vitro and promoted cancer stem cell activity in ER-positive BC. CONCLUSION: AS shows the tumorigenic potential on ER-positive BC growth through ERα induced stemness, suggesting that the usage of AS is not recommended for BC in terms of safety measures.
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Angelica sinensis/química , Neoplasias da Mama/induzido quimicamente , Neoplasias da Mama/tratamento farmacológico , Carcinogênese/induzido quimicamente , Extratos Vegetais/efeitos adversos , Receptores de Estrogênio/metabolismo , Animais , Antineoplásicos/uso terapêutico , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Feminino , Humanos , Células MCF-7 , Camundongos , Camundongos Nus , Neoplasias Experimentais/induzido quimicamente , Neoplasias Experimentais/tratamento farmacológico , Células-Tronco Neoplásicas , Extratos Vegetais/uso terapêutico , Raízes de Plantas/química , Receptores de Estrogênio/genética , Tamoxifeno/uso terapêuticoRESUMO
Metabolic reprogramming, characterized by alterations of cellular metabolic patterns, is fundamentally important in supporting the malignant behaviors of cancer cells. It is considered as a promising therapeutic target against cancer. Traditional Chinese medicine (TCM) and its bioactive components have been used in cancer therapy for an extended period, and they are well-known for their multi-target pharmacological functions and fewer side effects. However, the detailed and advanced mechanisms underlying the anticancer activities of TCM remain obscure. In this review, we summarized the critical processes of cancer cell metabolic reprogramming, including glycolysis, mitochondrial oxidative phosphorylation, glutaminolysis, and fatty acid biosynthesis. Moreover, we systemically reviewed the regulatory effects of TCM and its bioactive ingredients on metabolic enzymes and/or signal pathways that may impede cancer progress. A total of 46 kinds of TCMs was reported to exert antitumor effects and/or act as chemosensitizers via regulating metabolic processes of cancer cells, and multiple targets and signaling pathways were revealed to contribute to the metabolic-modulating functions of TCM. In conclusion, TCM has its advantages in ameliorating cancer cell metabolic reprogramming by its poly-pharmacological actions. This review may shed some new light on the explicit recognition of the mechanisms of anticancer actions of TCM, leading to the development of natural antitumor drugs based on reshaping cancer cell metabolism.
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Antineoplásicos Fitogênicos/uso terapêutico , Medicamentos de Ervas Chinesas/uso terapêutico , Metabolismo Energético/efeitos dos fármacos , Medicina Tradicional Chinesa , Neoplasias/tratamento farmacológico , Animais , Antineoplásicos Fitogênicos/efeitos adversos , Medicamentos de Ervas Chinesas/efeitos adversos , Humanos , Neoplasias/metabolismo , Neoplasias/patologiaRESUMO
Gut microbiota is a complex microecosystem, which is called the second genome of the human body. Herbal medicine can balance tumor-suppressing bacteria and tumor-promoting bacteria and exert its anti-cancer effect by regulating gut microbiota. Traditional Chinese medicine (TCM) has a history of thousands of years in prevention and treatment of diseases in China. In recent decades, TCM has been shown to have an obvious advantage in prolonging the survival time and improving the living quality of patients with cancer. Notably, gut microbiota has become a new pathway to understanding TCM. In this review, we will focus on gut microbiota and tumor progression, especially the diversity, functionality and metabolites of gut microbiota affected by TCM in various cancer. We will also discuss the potential mechanism of gut microbiota for exploring TCM in anti-cancer effect. This article aims to comprehensively review the anti-cancer research of TCM by regulating gut microbiota, and address future perspectives and challenges of gut microbiota in TCM intervention for cancer.
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Medicamentos de Ervas Chinesas , Microbioma Gastrointestinal , Neoplasias , Plantas Medicinais , Medicamentos de Ervas Chinesas/uso terapêutico , Humanos , Medicina Tradicional Chinesa , Neoplasias/tratamento farmacológicoRESUMO
Two antimalaria alkaloids, febrifugine and isofebrifugine, were successfully separated from total alkaloids of Dichroa febrifuga roots by one-step preparative countercurrent chromatography with a selected biphasic solvent system. The selected biphasic solvent system was composed of chloroform: methanol: water (2:1:1, v/v) according to partition performance of the two target components. Selection of biphasic solvent system was conducted by high performance liquid chromatography combined with high performance thin layer chromatography, which greatly assisted the screening procedure for biphasic solvent system. Totally, 50 mg of total alkaloid was separated by one-step preparative countercurrent chromatography, yielding 12 mg of febrifugine and 9 mg of isofebrifugine with more than 98.0% purity, respectively.
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Alcaloides/isolamento & purificação , Distribuição Contracorrente/métodos , Hydrangea/química , Piperidinas/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Quinazolinas/isolamento & purificação , Alcaloides/química , Piperidinas/química , Extratos Vegetais/química , Raízes de Plantas/química , Quinazolinas/químicaRESUMO
OBJECTIVE: To observe the effect of electroacupuncture on postpartum uterine contraction pain and uterine involution. METHODS: A total of 80 patients with postpartum uterine contraction pain were randomly divided into an observation group and a control group, 40 cases in each group. The observation group was treated with electroacupuncture at Dahe (KI 12), Zhongzhu (KI 15), Hegu (LI 4), Xuehai (SP 10), etc. for 30 min, once a day, 3 days were as one course, and 2 courses with 1-day interval were required. The control group was treated with oral Xinshenghua tablet, 4 tablets each time, 3 times a day for 7 days. Before treatment, 24, 48, 72 h into treatment and after treatment, the visual analogue scale (VAS) score was observed; the maximum anteroposterior diameter of uterine hemorrhage, the area of hemorrhage, the space between uterus fundus and umbilical cord, and the summation of three diameters of uterus before and after treatment were compared, and the time of postpartum uterine contraction pain disappeared was recorded in the two groups. RESULTS: Compared before treatment, the VAS scores of 24, 48, 72 h into treatment and after treatment were decreased in both groups (P<0.05), and those in the observation group were lower than the control group (P<0.05). Compared before treatment, the maximum anteroposterior diameter of uterine hemorrhage, the area of hemorrhage and the summation of three diameters of uterus after treatment were decreased (P<0.05), the space between uterus fundus and umbilical cord was increased in both groups (P<0.05), and those in the observation group were superior to the control group (P<0.05). The number of days required to treat the uterine contraction pain in the observation group was shorter than the control group (P<0.05). CONCLUSION: Electroacupuncture can effectively relieve postpartum uterine contraction pain, accelerate the discharge of residual uterine hemorrhage in the uterine cavity, and promote uterine involution.
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Eletroacupuntura , Pontos de Acupuntura , Feminino , Humanos , Dor , Período Pós-Parto , Gravidez , Contração UterinaRESUMO
Soluble guanylate cyclase (sGC) is a clinically validated therapeutic target in the treatment of pulmonary hypertension. Modulators of sGC have the potential to treat diseases that are affected by dysregulation of the NO-sGC-cGMP signal transduction pathway. This letter describes the SAR efforts that led to the discovery of CYR715, a novel carboxylic acid-containing sGC stimulator, with an improved metabolic profile relative to our previously described stimulator, IWP-051. CYR715 addressed potential idiosyncratic drug toxicity (IDT) liabilities associated with the formation of reactive, migrating acyl glucuronides (AG) found in related carboxylic acid-containing analogs and demonstrated high oral bioavailability in rat and dose-dependent hemodynamic pharmacology in normotensive Sprague-Dawley rats.
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Ácidos Carboxílicos/química , Glucuronídeos/química , Hipertensão Pulmonar/tratamento farmacológico , Guanilil Ciclase Solúvel/metabolismo , Vasodilatadores/química , Administração Oral , Animais , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Glucuronídeos/administração & dosagem , Glucuronídeos/farmacocinética , Humanos , Masculino , Metaboloma , Modelos Moleculares , Óxido Nítrico/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Ligação Proteica , Ratos Sprague-Dawley , Transdução de Sinais , Relação Estrutura-Atividade , Vasodilatadores/administração & dosagem , Vasodilatadores/farmacocinéticaRESUMO
OBJECTIVE@#To compare the clinical therapeutic effect on painful diabetic peripheral neuropathy (PDPN) between dragon-tiger fighting needling and pregabalin capsules.@*METHODS@#A total of 60 patients with PDPN were randomized into an observation group and a control group, 30 cases in each one. On the base of treatment with routine anti-hyperglycaemic measures and nutritional neurotherapy, the dragon-tiger fighting needling was exerted at Sanyinjiao (SP 6), Zusanli (ST 36), Yinlingquan (SP 9) and Xuehai (SP 10) in the observation group, once daily. Pregabalin capsules were prescribed for oral administration in the control group, 75 mg, twice a day. The treatment for 2 weeks was as one course and 2 courses of treatment were required in total. The score of visual analogue scale (VAS), the score of MOS item short form health survey (SF-36) and nerve conduction velocity before and after treatment were compared between the two groups. The clinical therapeutic effect was evaluated in the two groups.@*RESULTS@#After treatment, VAS score was reduced as compared with before treatment in the two groups (@*CONCLUSION@#The dragon-tiger fighting needling therapy relieves painful symptoms, improves the quality of life and increases nerve conduction velocity in the patients with diabetic peripheral neuropathy, and the therapeutic effect is better than oral administration of pregabalin capsules.
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Animais , Humanos , Pontos de Acupuntura , Terapia por Acupuntura , Diabetes Mellitus , Neuropatias Diabéticas/tratamento farmacológico , Qualidade de Vida , Tigres , Resultado do TratamentoRESUMO
OBJECTIVE@#To observe the effect of electroacupuncture on postpartum uterine contraction pain and uterine involution.@*METHODS@#A total of 80 patients with postpartum uterine contraction pain were randomly divided into an observation group and a control group, 40 cases in each group. The observation group was treated with electroacupuncture at Dahe (KI 12), Zhongzhu (KI 15), Hegu (LI 4), Xuehai (SP 10), etc. for 30 min, once a day, 3 days were as one course, and 2 courses with 1-day interval were required. The control group was treated with oral @*RESULTS@#Compared before treatment, the VAS scores of 24, 48, 72 h into treatment and after treatment were decreased in both groups (@*CONCLUSION@#Electroacupuncture can effectively relieve postpartum uterine contraction pain, accelerate the discharge of residual uterine hemorrhage in the uterine cavity, and promote uterine involution.