RESUMO
Dendrobium nobile (Lindl.) have long been used as herbal tea and a traditional herbal medicine to treat Alzheimer's disease (AD). In the current study, nineteen compounds (1-19), including two new vitamin E homologues (1-2), one new sesquiterpene (6), and two new dendrobines (7, 8), were isolated and identified from stems of Dendrobium nobile. Their structures were elucidated on the basis of NMR, 13C NMR calculation, and DP4+ probability analyses. The absolute configurations of new compounds were determined by electronic circular dichroism (ECD) data analysis. Antioxidant, anti-inflammatory, and cytotoxic activities of isolated compounds were evaluated. Among them, compound 2 demonstrated significant antioxidant activity compared with ascorbic acid (VC), while compounds 2 and 4 also exhibited an equal effect to positive control cisplatin. This study on the biological activity of the new vitamin E homologues from Dendrobium nobile may indicate its potential application in the pharmaceutical and food industries.
RESUMO
Pectins have proven to be advantageous for human health as they regulate beneficial microbial communities and enhance immunity. The fruit of Clausena lansium (Lour.) Skeels (Wampee), also referred to as "treasure in fruit", is rich in pectin polysaccharides. In this study, a homogalacturonan-type pectin (CCP2) with a molecular weight of 8.9 × 104 Da and degree of esterification of 42.86% was isolated from Wampee fruit. The gut microbiota regulation and phagocytosis-enhancing properties of CCP2 were examined in vivo and in vitro, respectively. Oral administration of CCP2 dramatically decreased the abundance of Bacteroidetes and increased the abundance of Firmicutes in intestinal bacteria in mice. The content of short-chain fatty acids in the feces also significantly improved. Moreover, CCP2 exhibited excellent phagocytosis-enhancing activities on RAW 264.7 macrophages. These results suggested that CCP2 could be a potential gut microbiota regulator and phagocytosis-enhancer, which could be used in food products to promote health through beneficial manipulation of gut microbiota.
Assuntos
Clausena/metabolismo , Frutas/metabolismo , Microbioma Gastrointestinal/efeitos dos fármacos , Pectinas/uso terapêutico , Prebióticos/microbiologia , Animais , Animais não Endogâmicos , Camundongos , Células RAW 264.7RESUMO
OBJECTIVE: To observe the efficacy difference between conventional needling depth and deep needling for dyspepsia after ischemic stroke. METHODS: A total of 120 patients with dyspepsia after ischemic stroke were randomized into an observation group (60 cases, 4 cases dropped off) and a control group (60 cases, 3 cases dropped off). Basic treatment was given in the both groups. In the observation group, deep needling was applied at Zhongwan (CV 12), Tianshu (ST 25) and Liangmen (ST 21) for 60-70 mm, after even reinforcing-reducing manipulation of lifting-thrusting technique, the needles were withdrew to 35-50 mm. In the control group, the same acupoints as the observation group were selected and punctured for 25 mm. The needles were retained for 30 min, once a day, 6 times a week for 2 weeks in the both groups. The dyspepsia TCM symptom score was observed before treatment, 1 day and 1, 2 weeks into treatment, and the clinical efficacy was evaluated 2 weeks into treatment in the both groups. RESULTS: The effective rate was 92.9% (52/56) in the observation group, which was superior to 78.9% (45/57) in the control group (P<0.01). Compared before treatment, the total scores and sub-item scores of dyspepsia TCM symptom of 1, 2 weeks into treatment were decreased in the both groups (P<0.01, P<0.05). The total scores and abdominal fullness scores of dyspepsia TCM symptom of each time point into treatment and hiccup score of 2 weeks into treatment in the observation group were lower than those in the control group (P<0.01, P<0.05). The total scores of dyspepsia TCM symptom 1, 2 weeks into treatment in the mild patients and each time point into treatment in the moderate patients of the observation group were lower than those in the control group (P<0.01). CONCLUSION: Conventional needling depth and deep needling can both improve the clinical symptoms in patients with dyspepsia after ischemic stroke, and deep needling has faster and better efficacy.
Assuntos
Terapia por Acupuntura , Isquemia Encefálica , Dispepsia , AVC Isquêmico , Acidente Vascular Cerebral , Dispepsia/terapia , Humanos , Acidente Vascular Cerebral/complicações , Acidente Vascular Cerebral/terapiaRESUMO
OBJECTIVE: To observe the therapeutic effect of different needling depth for benign prostatic hyperplasia. METHODS: A total of 70 patients with benign prostatic hyperplasia were randomized into an elongated needle group (35 cases, 1 case dropped off) and a filiform needle group (35 cases, 2 cases dropped off). Basic treatment combined with acupuncture were adopted in both groups, acupuncture was applied at Guanyuan (CV 4), Zhongji (CV 3), Shuidao (ST 28), Sanyinjiao (SP 6), Taixi (KI 3), Zhigou (TE 6). In the elongated needle group, acupuncture was performed at Guanyuan (CV 4), Zhongji (CV 3), Shuidao (ST 28) by elongated needle, the needling depth was 60-73 mm. In the filiform needle group, acupuncture was performed at Guanyuan (CV 4), Zhongji (CV 3), Shuidao (ST 28) by filiform needle, the needling depth was 25-30 mm. The treatment was given once a day (except Sunday), 2 weeks as one course, 1 course was required in both groups. Before and after treatment, the international prostate symptom score(IPSS), quality of life (QOL) score and prostate volume were observed in the two groups, and the therapeutic effect was evaluated. RESULTS: Compared before treatment, the IPSS and QOL scores after 1, 2-week treatment were reduced (P<0.01), and the IPSS and QOL scores after 2-week treatment were lower than those after 1-week treatment in the two groups (P<0.01); the IPSS and QOL scores after 2-week treatment in the elongated needle group were lower than the filiform needle group (P<0.05, P<0.01). After 2-week treatment, the prostate volume was reduced in the two groups (P<0.01, P<0.05). The total effective rate was 91.2% (31/34) in the elongated needle group, which was superior to 72.7% (24/33) in the filiform needle group (P<0.05). CONCLUSION: Both elongated needle and filiform needle can improve the symptom and quality of life in patients with benign prostatic hyperplasia, and elongated needle has the better therapeutic effect.
Assuntos
Terapia por Acupuntura/métodos , Agulhas , Hiperplasia Prostática , Pontos de Acupuntura , Humanos , Masculino , Hiperplasia Prostática/terapia , Qualidade de Vida , Resultado do TratamentoRESUMO
Cerebral hypoperfusion is a common feature of cerebral small vascular disease (CSVD), which has been considered as one of the causes of cognitive decline in recent years. Epimedium flavonoids (EF) are the main ingredients extracted from Epimedium. The purpose of this study was to investigate the effects of EF on cognitive impairment, and the underlying mechanisms in rats with permanent occlusion of the bilateral common carotid artery (2VO). EF (50, 100, and 200 mg/kg) was intragastrically administered for 12 weeks starting 2 weeks after 2VO surgery. The results showed that EF treatment improved learning and memory impairment in 2VO rats evaluated by novel object recognition and Y-maze tests. NeuN immunohistochemical staining indicated that EF alleviated neuronal loss in the hippocampus and cerebral cortex of 2VO rats. MAP-2 immunofluorescence staining and western blotting showed that EF protected neuronal dendrites and increased the expression of cytoskeleton proteins MAP-2 and NF200 in the hippocampus of 2VO rats. Moreover, EF protected the synapse ultrastructure detected by transmission electron microscopy, and increased the expression of synaptic plasticity-related proteins, including synaptophysin, synaptotagmin-I, synapsin I, PSD-95, p-NMDA2B, and p-CaMKII-α in the hippocampus of 2VO rats. In addition, EF increased the expression of neuregulin-1 (NRG-1), p-ErbB4, brain-derived neurotrophic factor (BDNF), p-Fyn, PI3K, p-Akt, and p-CREB in the hippocampus of 2VO rats. These results suggest that EF may protect neurons and synapses by activating the NRG1/ErbB4, BDNF/Fyn, and P13 K/Akt/CREB pathways in the hippocampus and cerebral cortex, thus improving cognitive impairment induced by chronic cerebral hypoperfusion. EF may be a potential candidate drug for chronic cerebral hypoperfusion and CSVD therapy.
Assuntos
Fator Neurotrófico Derivado do Encéfalo/metabolismo , Doenças de Pequenos Vasos Cerebrais/metabolismo , Epimedium , Flavonoides/uso terapêutico , Neuregulina-1/metabolismo , Proteínas Proto-Oncogênicas c-fyn/metabolismo , Receptor ErbB-4/metabolismo , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Doenças de Pequenos Vasos Cerebrais/tratamento farmacológico , Circulação Cerebrovascular/efeitos dos fármacos , Circulação Cerebrovascular/fisiologia , Relação Dose-Resposta a Droga , Flavonoides/farmacologia , Masculino , Neurônios/efeitos dos fármacos , Neurônios/metabolismo , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Sprague-Dawley , Transdução de Sinais/efeitos dos fármacos , Transdução de Sinais/fisiologia , Sinapses/efeitos dos fármacos , Sinapses/metabolismoRESUMO
Chronic cerebral hypoperfusion is a common cause of cerebral small vascular disease (CSVD). White matter (WM) lesions are the typical pathological manifestation of CSVD and contribute to cognitive decline. Epimedium flavonoids (EF) are the main component in Epimedium brevicornu Maxim., which is commonly used in traditional Chinese medicine. The purpose of this study was to investigate the effects of EF on cognitive impairment and the underlying mechanisms in a CSVD rat model induced with chronic cerebral hypoperfusion. The model was established by permanent bilateral common carotid artery occlusion (2VO) in rats. EF (50, 100, and 200 mg/kg) was intragastrically administered once a day for 12 weeks starting 2 weeks after 2VO surgery. The learning and memory capacity of the rats were measured using the Morris water maze and step-through tests. WM lesions were observed by MRI-diffusion tensor imaging, transmission electron microscopy, and LFB staining. Oligodendrocytes were detected by immunohistochemistry. Western blotting assay was used to determine the level of protein expression. The results showed that EF significantly improved learning and memory impairment, alleviated WM nerve fiber injuries and demyelination, and increased the number of mature oligodendrocytes in the corpus callosum, subcortical WM, and periventricular WM in 2VO rats. Mechanistically, EF reduced the expression of Lingo-1 and ROCK2 and increased the levels of phosphorylated (p-) Fyn, brain-derived neurotrophic factor (BDNF), TrkB, neuregulin-1 (NRG-1), p-ErbB4, PI3K p85 and p110α, p-Akt, and p-CREB in the corpus callosum of 2VO rats. These results suggest that EF may improve cognitive impairment and WM lesions induced by chronic cerebral hypoperfusion through inhibiting the Lingo-1/Fyn/ROCK pathway and activating the BDNF/TrkB, NRG-1/ErbB4, and the downstream PI3K/Akt/CREB pathways in WM. Thus, EF can be used as a potential neuroprotective agent in CSVD therapy.
Assuntos
Encéfalo/efeitos dos fármacos , Doenças de Pequenos Vasos Cerebrais/patologia , Disfunção Cognitiva/etiologia , Medicamentos de Ervas Chinesas/farmacologia , Transdução de Sinais/efeitos dos fármacos , Substância Branca/efeitos dos fármacos , Animais , Encéfalo/metabolismo , Encéfalo/patologia , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Doenças de Pequenos Vasos Cerebrais/complicações , Doenças de Pequenos Vasos Cerebrais/metabolismo , Disfunção Cognitiva/metabolismo , Disfunção Cognitiva/patologia , Epimedium , Flavonoides/farmacologia , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Proteínas de Membrana/metabolismo , Proteínas do Tecido Nervoso/metabolismo , Neuregulina-1/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-fyn/metabolismo , Ratos , Ratos Sprague-Dawley , Substância Branca/patologia , Quinases Associadas a rho/metabolismoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Chong-lou (Paris polyphylla var. yunnanensis or P. polyphylla var. chinensis) is traditionally used as an anticancer medicine in China. It is also the material basis of some Chinese patent anticancer medicines, such as Gan-Fu-Le capsules, Bo-Er-Ning capsules, Lou-Lian capsules, Ruan-Jian oral liquid, and Qi-Zhen capsules. P. forrestii, a substitute for Chong-lou, is planted at a large scale in the Yunnan Province of China. AIM OF THE STUDY: To clarify the active chemical constituents of P. forrestii and evaluate the in vitro and in vivo anticancer activities of the total saponins from P. forrestii. MATERIALS AND METHODS: The total saponins of P. forrestii were extracted and separated to yield pure compounds by chromatographic techniques, and the structures of the isolates were elucidated by spectroscopic methods. The cytotoxicity of the crude extracts, total saponins, and chemical constituents were evaluated using an MTS assay. In vivo antitumor activities of the total saponins from P. forrestii were measured using H22 tumor-bearing mice by intraperitoneal (ip) administration. RESULTS: Eight compounds, including polyphyllin D (1), formosanin C (2), dioscin (3), diosgenin-3-O-α-l-rhamnopyranosyl-(1â2)-ß-d-glucopyranoside (4), paris saponin H (5), pennogenin-3-O-α-l-rhamnopyranosyl-(1â2)-[α-l-rhamnopyranosyl-(1â4)]-ß-d-glucopyranoside (6), pariposide A (7), and crustecdysone (8), were isolated from the total saponins of P. forrestii. The total saponins and compounds 1-6 showed significant inhibitory activity against the growth of the HL-60, SMMC-7721, A-549, MCF-7, and SW480 cell lines. The total saponins from P. forrestii had a tumor-inhibitory effect in H22 tumor-bearing mice upon ip (2.25â¯mg/kg dose) administration, with an inhibition rate of 42.6% compared with cisplatin (ip, 2â¯mg/kg dose, 53.9% inhibition rate). CONCLUSION: The results support that P. forrestii could be a substitute for P. polyphylla var. yunnanensis as an anticancer medicine.
Assuntos
Antineoplásicos Fitogênicos , Melanthiaceae , Saponinas , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/uso terapêutico , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Feminino , Humanos , Rim/efeitos dos fármacos , Fígado/efeitos dos fármacos , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Rizoma , Saponinas/análise , Saponinas/farmacologia , Saponinas/uso terapêutico , Baço/efeitos dos fármacos , Timo/efeitos dos fármacos , Carga Tumoral/efeitos dos fármacosRESUMO
Scaffolds with extracellular matrix-like fibrous morphology, suitable mechanical properties, biomineralization capability, and excellent cytocompatibility are desired for bone regeneration. In this work, fibrous and degradable poly(ester urethane)urea (PEUU) scaffolds reinforced with titanium dioxide nanoparticles (nTiO2) were fabricated to possess these properties. To increase the interfacial interaction between PEUU and nTiO2, poly(ester urethane) (PEU) was grafted onto the nTiO2. The scaffolds were fabricated by electrospinning and exhibited fiber diameter of <1µm. SEM and EDX mapping results demonstrated that the PEU modified nTiO2 was homogeneously distributed in the fibers. In contrast, severe agglomeration was found in the scaffolds with unmodified nTiO2. PEU modified nTiO2 significantly increased Young's modulus and tensile stress of the PEUU scaffolds while unmodified nTiO2 significantly decreased Young's modulus and tensile stress. The greatest reinforcement effect was observed for the scaffold with 1:1 ratio of PEUU and PEU modified nTiO2. When incubating in the simulated body fluid over an 8-week period, biomineralization was occurred on the fibers. The scaffolds with PEU modified nTiO2 showed the highest Ca and P deposition than pure PEUU scaffold and PEUU scaffold with unmodified nTiO2. To examine scaffold cytocompatibility, bone marrow-derived mesenchymal stem cells were cultured on the scaffold. The PEUU scaffold with PEU modified nTiO2 demonstrated significantly higher cell proliferation compared to pure PEUU scaffold and PEUU scaffold with unmodified nTiO2. The above results demonstrate that the developed fibrous nanocomposite scaffolds have potential for bone tissue regeneration.
Assuntos
Materiais Biomiméticos/farmacologia , Calcificação Fisiológica/efeitos dos fármacos , Células-Tronco Mesenquimais/citologia , Nanocompostos/química , Poliuretanos/farmacologia , Alicerces Teciduais/química , Titânio/farmacologia , Animais , Líquidos Corporais/química , Cálcio/análise , Proliferação de Células/efeitos dos fármacos , Hidroxiácidos/síntese química , Hidroxiácidos/química , Células-Tronco Mesenquimais/efeitos dos fármacos , Nanocompostos/ultraestrutura , Fósforo/análise , Poliuretanos/síntese química , Poliuretanos/química , Propionatos/síntese química , Propionatos/química , Ratos , Espectrometria por Raios X , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
AIM: Membranous nephropathy and minimal change disease (MCD) have been involved in mercury-induced nephrotic syndrome. IgA nephropathy is not known to be a common pathological type. In the present article, we report a case of IgA nephropathy with MCD following exposure to mercury-containing skin lightening cream. MATERIAL AND METHODS: The patient was a 39-year-old woman who presented with nephrotic syndrome. She had a 6-month history of using as many as 8 kinds of skin-lightening creams, and urinary mercury excretion was high. Renal biopsy revealed IgA nephropathy with MCD. The use of cosmetics was stopped and chelation therapy was given. After 4 courses (1 month) of chelation therapy, there was a complete remission of proteinuria and hematuria, and urine tests remained normal during the 5-year follow-up period. RESULTS AND CONCLUSIONS: The unique clinical and pathological features of IgA nephropathy with MCD had raised the controversial question of whether MCD and IgA deposition are separate entities or a common pathophysiology. Repeated renal biopsy and similar cases were helpful and should be carried out as far as possible.â©.
Assuntos
Glomerulonefrite por IGA/induzido quimicamente , Intoxicação por Mercúrio/complicações , Nefrose Lipoide/induzido quimicamente , Preparações Clareadoras de Pele/intoxicação , Adulto , Quelantes/uso terapêutico , Feminino , Glomerulonefrite por IGA/patologia , Glomerulonefrite por IGA/terapia , Hematúria/etiologia , Humanos , Rim/patologia , Rim/ultraestrutura , Intoxicação por Mercúrio/tratamento farmacológico , Nefrose Lipoide/patologia , Nefrose Lipoide/terapia , Síndrome Nefrótica/etiologia , Síndrome Nefrótica/terapia , Proteinúria/etiologia , Indução de Remissão , Preparações Clareadoras de Pele/química , Unitiol/uso terapêuticoRESUMO
Since the chromatographic fingerprint was introduced, it has been accepted by many countries to assess the quality and authenticity of Chinese herbal medicine (CHM). However, solely using the chromatographic fingerprint to assay numerous chemicals is not suitable for the assessment of the whole internal quality and pharmacodynamics of CHM. Consequently, it is necessary to develop a rational approach to connecting the chromatographic fingerprint with effective components to assess the internal quality of CHM. For this purpose, a spectrum-effect relationship theory was proposed and accepted as a new method for the assessment of CHM because of its potential use to screen effective components from CHM. In this paper, we systematically reviewed the application of the spectrum-effect relationship theory in the research of CHM, including research mentality, different chromatographic analysis techniques, data processing technologies, and structure determination.
Assuntos
Avaliação Pré-Clínica de Medicamentos/métodos , Medicamentos de Ervas Chinesas , Cromatografia , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacocinética , Modelos Estatísticos , Controle de QualidadeRESUMO
Mushroom Inonotus obliquus (I. obliquus), a folk medicine, has been widely used to treat several human malicious tumors since 16th century. In this study, three homogenous biomolecules (designated IOA1, IOA2 and IOA3) were prepared from the alkali extract of I. obliquus. Their molecular weights were measured to be 6.1 × 10(4), 2.9 × 10(4) and 3.5 × 10(4) g/mol respectively and all of them were characterized as lignin-carbohydrate complexes mainly comprised lignin as well as -25% carbohydrates. Antioxidant assays indicated that all of them exhibited pronounced reductive power and strong scavenging activities on DPPH and hydroxyl radicals in vitro. Immunological tests showed that they could also significantly stimulate nitric oxide production and phagocytic activity in RAW 264.7 macrophages. These results implied that the lignin-carbohydrate complexes extracted from I. obliquus might be used as novel natural antioxidants or immunostimulants in functional foods or pharmaceutical candidates.
Assuntos
Agaricales/química , Antioxidantes/química , Antioxidantes/farmacologia , Fatores Imunológicos/química , Fatores Imunológicos/farmacologia , Lignina/química , Lignina/farmacologia , Agaricales/metabolismo , Animais , Antioxidantes/metabolismo , Compostos de Bifenilo/química , Metabolismo dos Carboidratos , Humanos , Radical Hidroxila/química , Fatores Imunológicos/metabolismo , Ferro/química , Lignina/metabolismo , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Macrófagos/metabolismo , Camundongos , Óxido Nítrico/biossíntese , Fagocitose/efeitos dos fármacos , Picratos/química , Células RAW 264.7 , SolubilidadeRESUMO
Radix Paeoniae Alba is widely used in Chinese traditional medicine to treat various diseases such as gastrointestinal disorders, cancer, and other diseases. In this study, two polysaccharides RPAPW1 and RPAPW2 were isolated from Radix Paeoniae Alba by DEAE-52 cellulose chromatography and G-25 sephadex. According to physicochemical methods, NMR and methylation analysis, RPAPW1 and RPAPW2 were established to be α-glucans consisting of predominant 4-linked α- Glc residues branched at O-6 and contained trace amount of protein and uronic acid. Immunological tests indicated that RPAPW1, RPAPW2 and could promote splenocyte proliferation and RAW264.7 phagocytic activity. In vitro, RPAPW1 and RPAPW2 elicited a week reducing power, DPPH scavenging activity and could not protect the PC12 cells from H2O2 damage. These data implied polysaccharides RPAPW1 and RPAPW2 had the potential to be a natural immunopotentiating and antioxidant supplement for preparing functional foods and nutraceuticals.
Assuntos
Proliferação de Células/efeitos dos fármacos , Paeonia/química , Fagocitose/efeitos dos fármacos , Polissacarídeos , Baço/imunologia , Animais , Linhagem Celular , Masculino , Camundongos , Células PC12 , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia , Ratos , Baço/citologiaRESUMO
Medicinal values and their chemical bases of Paris (Trilliaceae) are reviewed. Paris plants include 40 species and varieties. Among them, 18 ones are medicinal plants with similarity in traditional uses. Fourteen species have been studied phytochemically, which led to isolation of 207 compounds including 121 steroidal saponins. These saponins are major active constituents from Paris plants, which can explain the traditional uses of the plants to treat cancer, malignant boil, bleeding, gastritis, and so on. The similarity in medicinal uses and chemical constituents of Paris plants implies the possibility of resource substitution among these species. It is worth to further investigate Paris plants in chemical constituents, pharmacological activity, biological property, and toxicology.
Assuntos
Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Magnoliopsida/química , Plantas Medicinais/química , Animais , Tratamento Farmacológico , HumanosRESUMO
Human xanthine oxidase is considered to be a target for therapy of hyperuricemia. Cichorium intybus is a Chinese plant medicine which widely used in Xinjiang against various diseases. In order to screen the inhibitors of xanthine oxidase from C. intybus and to explore main pharmacological actions of cichory a compound collection of C. intybus was built via consulting related references about chemical research on cichory. The three-dimensional crystal structure of xanthine oxidase (PDB code: 1N5X) from Protein Data Bank was downloaded.. Autodock 4.2 was employed to screen the inhibitors of xanthine oxidase from cichory 70 compounds were found to possess quite low binding free energy comparing with TEI (febuxostat). C. intybus contains constituents possessing potential inhibitive activity against xanthine oxidase. It can explain the main pharmacological actions of cichory which can significantly lower the level of serum uric acid.
Assuntos
Cichorium intybus/química , Medicamentos de Ervas Chinesas/química , Inibidores Enzimáticos/química , Xantina Oxidase/antagonistas & inibidores , Bases de Dados de Proteínas , Humanos , Simulação de Acoplamento Molecular , Estrutura Molecular , Xantina Oxidase/metabolismoRESUMO
The ethnomedical uses of Piper ( Hú Jiao) plants as anticancer agents, in vitro cytotoxic activity of both extracts and compounds from Piper plants, and in vivo antitumor activity and mechanism of action of selected compounds are reviewed in the present paper. The genus Piper (Piperaceae) contains approximately 2000 species, of which 10 species have been used in traditional medicines to treat cancer or cancer-like symptoms. Studies have shown that 35 extracts from 24 Piper species and 32 compounds from Piper plants possess cytotoxic activity. Amide alkaloids account for 53% of the major active principles. Among them, piplartine (piperlongumine) shows the most promise, being toxic to dozens of cancer cell lines and having excellent in vivo activity. It is worthwhile to conduct further anticancer studies both in vitro and in vivo on Piper plants and their active principles.
RESUMO
Two diarylheptanoids, musaitinerins A and B, one heterodimeric phenylphenalenone musaitinerone and four known phenylphenalenones, identified as 4-hydroxy-2-methoxy-9-phenyl-1H-phenalen-1-one, musanolone E, hydroxyanigorufone and irenolone were isolated from the fruits of Musa itinerans Cheesm. Their structures were elucidated using spectroscopic analyses. The antimicrobial activity of these compounds was evaluated against Escherichia coli, Staphylococcus aureus and Candida albicans; the cytotoxic activity of these compounds was also evaluated against human erythromyeloblastoid leukemia (K562) and human alveolar carcinoma epithelial (A549) cell lines, respectively. Musaitinerone and musanolone E exhibited weak effects against the A549 cell line, as compared with adriamycin. However, these two compounds did not exhibit any growth inhibition against K562 cells, S. aureus, E. coli or C. albicans. The other compounds were inactive against all of the tested cell lines and microorganisms, even at concentrations as high as 50 µM.
Assuntos
Diarileptanoides/química , Diarileptanoides/farmacologia , Frutas/química , Musa/química , Fenalenos/química , Fenalenos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos Fitogênicos , Candida albicans/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Humanos , Staphylococcus aureus/efeitos dos fármacosRESUMO
PURPOSE: To investigate the feasibility of interventional lipiodol embolism and multigene therapy in combination with focal chemotherapy in the treatment of VX2 liver cancer in rabbits. METHODS: Forty five rabbits with cancer larger than 2cm in diameter were randomly divided into five groups (n=9 per group). In Group 1, animals were treated with 0.9% sodium chloride. In Group 2, animals received lipiodol embolism. In Group 3, animals received lipiodol embolism and p53 gene therapy. In Group 4, animals received lipiodol embolism and TK/CD gene therapy. In Group 5, animals received lipiodol embolism and p53 and TK/CD gene therapy. Ultrasonography and CT were performed before and at ten days after interventional therapy. RESULTS: The VX2 model of liver cancer was successfully established in rabbits and interventional therapy smoothly performed. At ten days after interventional therapy, significant difference in the tumor volume was noted among five groups (p<0.05) and different treatments could inhibit the cancer growth. The inhibition of cancer growth was the most evident in the Group 5. Factorial analysis revealed gene therapy with p53 or TK/CD and lipiodol embolism independently exert significantly inhibitory effect on cancer growth. In addition, the suppression on tumor growth rate was the most obvious in the Group 5. CONCLUSIONS: Combination of gene therapy with lipiodol embolism can effectively inhibit the cancer growth and prolong the survival time. These findings demonstrate the effectiveness of multigene therapy in combination with lipiodol embolism in the treatment of liver cancer.
Assuntos
Antineoplásicos/uso terapêutico , Genes Transgênicos Suicidas/genética , Genes p53/fisiologia , Terapia Genética/métodos , Neoplasias Hepáticas/terapia , Animais , Terapia Combinada/métodos , Modelos Animais de Doenças , Embolização Terapêutica/métodos , Óleo Etiodado/uso terapêutico , Estudos de Viabilidade , Neoplasias Hepáticas/patologia , Coelhos , Distribuição Aleatória , Fatores de Tempo , Resultado do TratamentoRESUMO
PURPOSE: To investigate the feasibility of interventional lipiodol embolism and multigene therapy in combination with focal chemotherapy in the treatment of VX2 liver cancer in rabbits. METHODS: Forty five rabbits with cancer larger than 2cm in diameter were randomly divided into five groups (n=9 per group). In Group 1, animals were treated with 0.9% sodium chloride. In Group 2, animals received lipiodol embolism. In Group 3, animals received lipiodol embolism and p53 gene therapy. In Group 4, animals received lipiodol embolism and TK/CD gene therapy. In Group 5, animals received lipiodol embolism and p53 and TK/CD gene therapy. Ultrasonography and CT were performed before and at ten days after interventional therapy. RESULTS: The VX2 model of liver cancer was successfully established in rabbits and interventional therapy smoothly performed. At ten days after interventional therapy, significant difference in the tumor volume was noted among five groups (p<0.05) and different treatments could inhibit the cancer growth. The inhibition of cancer growth was the most evident in the Group 5. Factorial analysis revealed gene therapy with p53 or TK/CD and lipiodol embolism independently exert significantly inhibitory effect on cancer growth. In addition, the suppression on tumor growth rate was the most obvious in the Group 5. CONCLUSIONS: Combination of gene therapy with lipiodol embolism can effectively inhibit the cancer growth and prolong the survival time. These findings demonstrate the effectiveness of multigene therapy in combination with lipiodol embolism in the treatment of liver cancer.
OBJETIVO: Investigar a possibilidade de terapia multigênica e intervenção por embolização com lipiodol em combinação com quimioterapia focal no tratamento de câncer de fígado VX2 em coelhos. MÉTODOS: Quarenta e cinco coelhos com câncer maior do que 2cm de diâmetro foram distribuídos, aleatoriamente, em cinco grupos (n=9 por grupo). Grupo 1: animais foram tratados com cloreto de sódio 0,9% e no grupo 2 os animais receberam embolização com lipidol. Grupo 3: animais receberam embolização com lipiodol e terapia do gene p53 e grupo 4 animais receberam embolização com lipiodol e terapia do gene TK/CD. Grupo 5: animais receberam embolização com lipiodol e terapia do gene p53 e do gene TK/CD. Ultrassonografia e tomografia computadorizada foram realizadas antes e dez dias após a intervenção terapêutica. RESULTADOS: O modelo VX2 de câncer de fígado foi estabelecido com sucesso em coelhos e a terapia intervencionista foi bem executada. Dez dias após a intervenção terapêutica, uma diferença significativa no volume do tumor foi observada entre os cinco grupos (p<0,05) e diferentes tratamentos poderiam inibir o crescimento do câncer. A inibição do crescimento do cancer foi mais evidente no grupo 5. Análise fatorial revelou que a terapia com gene p53 ou TK/CD e embolia por lipiodol independentemente exerce um efeito inibidor significativo sobre o crescimento do câncer. Além disso, a supressão da taxa de crescimento do tumor foi mais evidente no Grupo 5. CONCLUSÕES: A combinação de terapia gênica com embolização com lipiodol pode inibir efetivamente o crescimento do câncer e prolongar o tempo de sobrevida. Estes resultados demonstram a eficácia da terapia multigênica em combinação com embolização com lipidol no tratamento de câncer hepático.
Assuntos
Animais , Coelhos , Antineoplásicos/uso terapêutico , Genes Transgênicos Suicidas/genética , /fisiologia , Terapia Genética/métodos , Neoplasias Hepáticas/terapia , Terapia Combinada/métodos , Modelos Animais de Doenças , Embolização Terapêutica/métodos , Óleo Etiodado/uso terapêutico , Estudos de Viabilidade , Neoplasias Hepáticas/patologia , Distribuição Aleatória , Fatores de Tempo , Resultado do TratamentoRESUMO
A new dihydroflavone, 5-carboxymethyl-7,4'-dihydroxyflavonone (1), and its glucoside 5-carboxymethyl-7,4'-dihydroxyflavonone-7-O-ß-D: -glucopyranoside (2), and one new monoterpene glucoside, (4Z,6E)-2,7-dimethyl-8-hydroxyocta-4,6-dienoic acid 8-O-ß-D: -glucopyranoside (3), were isolated from the whole plants of Selaginella moellendorffii. Their structures were determined by spectroscopic methods and chemical transformation. Compound 2 was evaluated for the ability to enhance glucose consumption in normal and insulin-resistant L6 muscle cells induced by high concentrations of insulin and glucose. Glucose consumption in insulin-resistant cells (but not in normal cells) was increased 15.2 ± 3.3% (p < 0.01) by compound 2 at a concentration of 0.1 µM in the presence of insulin (1 nM).