RESUMO
Neuropathic pain is a chronic debilitating symptom characterized by spontaneous pain and mechanical allodynia. It occurs in distinct forms, including brush-evoked dynamic and filament-evoked punctate mechanical allodynia. Potassium channel 2.1 (Kir2.1), which exhibits strong inward rectification, is and regulates the activity of lamina I projection neurons. However, the relationship between Kir2.1 channels and mechanical allodynia is still unclear. In this study, we first found that pretreatment with ML133, a selective Kir2.1 inhibitor, by intrathecal administration, preferentially inhibited dynamic, but not punctate, allodynia in mice with spared nerve injury (SNI). Intrathecal injection of low doses of strychnine, a glycine receptor inhibitor, selectively induced dynamic, but not punctate allodynia, not only in naïve but also in ML133-pretreated mice. In contrast, bicuculline, a GABA receptor antagonist, induced only punctate, but not dynamic, allodynia. These results indicated the involvement of glycinergic transmission in the development of dynamic allodynia. We further found that SNI significantly suppressed the frequency, but not the amplitude, of the glycinergic spontaneous inhibitory postsynaptic currents (gly-sIPSCs) in neurons on the lamina II-III border of the spinal dorsal horn, and pretreatment with ML133 prevented the SNI-induced gly-sIPSC reduction. Furthermore, 5 days after SNI, ML133, either by intrathecal administration or acute bath perfusion, and strychnine sensitively reversed the SNI-induced dynamic, but not punctate, allodynia and the gly-sIPSC reduction in lamina IIi neurons, respectively. In conclusion, our results suggest that blockade of Kir2.1 channels in the spinal dorsal horn selectively inhibits dynamic, but not punctate, mechanical allodynia by enhancing glycinergic inhibitory transmission.
Assuntos
Animais , Masculino , Bicuculina , Farmacologia , Modelos Animais de Doenças , Glicina , Metabolismo , Hiperalgesia , Tratamento Farmacológico , Metabolismo , Imidazóis , Farmacologia , Potenciais Pós-Sinápticos Inibidores , Fisiologia , Camundongos Endogâmicos C57BL , Neurônios , Metabolismo , Neurotransmissores , Farmacologia , Traumatismos dos Nervos Periféricos , Tratamento Farmacológico , Metabolismo , Fenantrolinas , Farmacologia , Canais de Potássio Corretores do Fluxo de Internalização , Metabolismo , Receptores de GABA-A , Metabolismo , Receptores de Glicina , Metabolismo , Estricnina , Farmacologia , Transmissão Sináptica , Fisiologia , Técnicas de Cultura de Tecidos , TatoRESUMO
The mechanisms of photosynthetic electron transport can be elucidated by inhibition of electron flow through the use of specific substances that, when combined with the chlorophyll chlorophyll a fluorescence emission was measured to investigate the effect of several inhibitors of the photosynthetic electron transport chain in canola leaf discs. Leaf discs were incubated in the dark for 2 hours in different solutions: (a) water control; (b) DCMU at 500 µM; (c) phenanthroline at 10 mM; and (d) hydroxylamine at 10, 50, 100 and 200 mM. Similar effects were observed between DCMU and phenanthroline, the initial fluorescence value was altered, but not the maximum fluorescence, with the disappearance of the IP phase. Hydroxylamine interacted and inhibited the oxygen evolving complex and caused an imbalance between the rate of QA reduction by photosystem II and the rate of QA oxidation by photosystem I.
Os mecanismos de transporte de elétrons podem ser elucidados pela inibição do fluxo de elétrons pelo uso de substâncias específicas que, juntamente com a técnica de fluorescência da clorofila, torna-se uma ferramenta importante para detalhar a cadeia de transporte de elétrons. Neste trabalho, a emissão da fluorescência da clorofila foi mensurada para investigar o efeito dos diferentes inibidores da cadeia de transporte de elétrons fotossintéticos de discos foliares de canola. Os discos foliares foram incubados no escuro durante 02 h em diferentes soluções: (a) água - controle, (b) 500 uM de DCMU, (c) 10 mM de fenantrolina, e (d) 10, 50, 100 e 200 mM de hidroxilamina. Foram observados efeitos similares entre DCMU e fenantrolina, o valor da fluorescência inicial foi alterado, contudo a fluorescência máxima não se alterou, havendo o desaparecimento da fase de IP. Hidroxilamina interagiu e inibiu o complexo de evolução de oxigênio e causou desequilíbrio entre a taxa de redução QA pelo fotossistema II e a taxa de oxidação QA pelo fotossistema I.
Assuntos
Brassica napus , Clorofila , Diurona , Hidroxilamina , Oxigênio , FenantrolinasRESUMO
<p><b>OBJECTIVE</b>To observe the effect of low molecular weight heparin calcium (LMWHC) combined Compound Danshen Injection (DI) on nephrotic syndrome patients with early onset severe preeclampsia.</p><p><b>METHODS</b>Totally 80 nephrotic syndrome patients with early onset severe pre-eclampsia were randomly assigned to four groups voluntarily, i.e., Group A (22 cases, treated by magnesium sulfate), B (19 cases, treated by magnesium sulfate plus LMWHC), C (21 cases, magnesium sulfate plus DI), D (18 cases, magnesium sulfate plus LMWHC and DI). Umbilical arterial S/D ratios, amniotic fluid index (AFI), prolonged gestational age, placenta weight, neonatal weight, and Apgar score were compared among the four groups.</p><p><b>RESULTS</b>Compared with before treatment in the same group, umbilical arterial S/D ratios decreased in the four groups (P <0. 05). AFI decreased in Group A, while it increased in Group B, C, and D (P<0. 05). Compared with Group A at the same time point, umbilical arterial S/D ratios decreased, and AFI increased in Group B, C, and D (P <0. 01 , P <0. 05). Prolonged gestational age and neonatal weight were increased in Group B, C, and D (P <0. 01, P <0. 05). Placenta weight were increased in Group B and D (P <0. 05). Apgar scores at 1 and 5 min were improved in Group D (P <0. 05). Compared with Group B and C at the same time point, umbilical arterial S/D ratios decreased, and AFI increased in Group D (P<0. 05). Compared with Group B, prolonged gestational age and placenta weight were decreased in Group C, but prolonged gestational age and placenta weight were increased in Group D (P <0.05). Compared with Group C, prolonged gestational age, placenta weight, and neonatal weight were increased in Group D (P <0. 05).</p><p><b>CONCLUSION</b>Treatment of nephrotic syndrome patients with early onset severe pre-eclampsia by LMWHC combined DI could prolong gestational ages, obviously improve prenatal outcomes, with better effect obtained than using any of them alone.</p>
Assuntos
Feminino , Humanos , Gravidez , Cálcio , Quimioterapia Combinada , Medicamentos de Ervas Chinesas , Usos Terapêuticos , Idade Gestacional , Heparina de Baixo Peso Molecular , Usos Terapêuticos , Sulfato de Magnésio , Síndrome Nefrótica , Tratamento Farmacológico , Fenantrolinas , Pré-Eclâmpsia , Tratamento Farmacológico , Salvia miltiorrhizaRESUMO
<p><b>OBJECTIVE</b>To study the effect of compound Danshen dripping pills and atorvastatin on restenosis after abdominal aorta angioplasty in rabbits.</p><p><b>METHODS</b>Rabbit models of abdominal aorta restenosis after angioplasty were established and treated with saline (group A), compound Danshen dripping pills (group B), atorvastatin (group C), or compound Danshen dripping pills plus atorvastatin (group D). HE staining was used to determine the thickness of arterial intimal hyperplasia and assess the morphological changes of the narrowed artery. Immunohistochemistry was employed to detect the expression of nuclear factor-κB (NF-κB) and monocyte chemoattractant protein-1 (MCP-1).</p><p><b>RESULTS</b>Compared with group A, the 3 treatment groups showed significant increased vascular cavity area and reduced intimal area and percentage of intimal hyperplasia (P<0.05). The vascular cavity area, intimal area and percentage of intimal hyperplasia levels differed significantly between group D and groups B and C (P<0.05). Immunohistochemistry showed a significant reduction of the expression rate of NF-κB and MCP-1 in the 3 treatment groups compared with group A (P<0.05), and the reduction was especially obvious in group D (P<0.05).</p><p><b>CONCLUTIONS</b>Compound danshen dripping pills combined with atorvastatin produces better effects than the drugs used alone in inhibiting vascular smooth muscle cell proliferation in rabbits after abdominal aorta angioplasty possibly due to a decreased expression of MCP-1 as a result of NF-κB inhibition.</p>
Assuntos
Animais , Coelhos , Angioplastia , Aorta , Patologia , Atorvastatina , Proliferação de Células , Quimiocina CCL2 , Metabolismo , Medicamentos de Ervas Chinesas , Farmacologia , Ácidos Heptanoicos , Farmacologia , Hiperplasia , Miócitos de Músculo Liso , NF-kappa B , Metabolismo , Fenantrolinas , Pirróis , Farmacologia , Salvia miltiorrhiza , Química , Túnica ÍntimaRESUMO
<p><b>OBJECTIVE</b>To observe the clinical efficacy difference on vegetative state in children between acupoint injection combined with plum-blossom needle and western medication based on basic treatment.</p><p><b>METHODS</b>Forty-eight children of vegetative state were randomized into an observation group and a control group, 24 cases in each one. On the basis of the treatment of transcranial magnetic stimulation apparatus, balancing treatment apparatus and massage, the acupoint injection and tapping method with plum-blossom needle were adopted in the observation group, in which Xingnaojing injection, mouse nerve growth factor (mNGF) injection, monosialotetrahexosylganglioside sodium injection (MSI), compound Danshen injection were divided in 6 pairs and were injected respectively in Baihui (GV 20), Yongquan (KI 1), Fengfu (GV 16), Yamen (GV 15) and the others, 0.5 mL in each acupoint, once a day for continuous 10 days. Additionally, the tapping method with plum-blossom needle was used on the Governor Vessel and Jiaji (EX-B 2) on the back. In the control group, the intravenous infusion was adopted with citicoline sodium injection, mannitol injection and dexamethasone injection. The treatment was given once a day, 20 days of treatment made one session and totally 3 sessions were required in the two groups. The clinical efficacy, the vegetative state score and the mean curing time were observed after 20 days, 40 days and 60 days of treatment between the two groups.</p><p><b>RESULTS</b>The effective rates were 58.3% (14/24), 70.8% (17/24) and 79.2% (19/24) in 20 days, 40 days and 60 days of treatment in the observation group and 20.8% (5/24), 45.8% (11/24) and 58.3% (14/24) in the control group respectively. The efficacy in the observation group was superior to those in the control group (P < 0.01, P < 0.05). The vegetative state score was improved apparently after 20 days, 40 days and 60 days of treatment as compared with those before treatment separately (all P < 0.05). It was improved obviously at the each time point after treatment in the observation group as compared with that in the control group (3.34 +/- 2.41 vs 2.64 +/- 11.56, 6.20 +/- 1.46 vs 4.34 +/- 1.64, 11.26 +/- 2.63 vs 8.75 +/- 2.18, all P < 0.05). The mean curing time was (45.67 +/- 16.24) days in the observation group, which was shorter apparently than that of (55.34 +/- 4.57) days in the control group (P < 0.05).</p><p><b>CONCLUSION</b>Based on basic treatment acupoint injection combined with tapping method of plum-blossom needle achieve the reliable efficacy on vegetative state in children.</p>
Assuntos
Animais , Pré-Escolar , Feminino , Humanos , Lactente , Masculino , Camundongos , Pontos de Acupuntura , Terapia por Acupuntura , Terapia Combinada , Medicamentos de Ervas Chinesas , Fator de Crescimento Neural , Estado Vegetativo Persistente , Tratamento Farmacológico , Terapêutica , Fenantrolinas , Resultado do TratamentoRESUMO
As traditional Chinese medicine (TCM) preparation products feature complex compounds and multiple preparation processes, the implementation of quality control in line with the characteristics of TCM preparation products provides a firm guarantee for the clinical efficacy and safety of TCM preparation products. Danshen infusion solution is a preparation commonly used in clinic, but its quality control is restricted to indexes of finished products, which can not guarantee its inherent quality. Our study group has proposed "multi-dimensional structure and process dynamics quality control system" on the basis of "component structure theory", for the purpose of controlling the quality of Danshen infusion solution at multiple levels and in multiple links from the efficacy-related material basis, the safety-related material basis, the characteristics of dosage form to the preparation process. This article, we bring forth new ideas and models to the quality control of TCM preparation products.
Assuntos
Animais , Humanos , Camundongos , Medicamentos de Ervas Chinesas , Química , Farmacologia , Padrões de Referência , Fenantrolinas , Química , Farmacologia , Padrões de Referência , Controle de Qualidade , Salvia miltiorrhiza , QuímicaRESUMO
<p><b>OBJECTIVE</b>To investigate the role of mitogen-activated protein kinases (MAPKs)-extracellular signal regulated kinase1/2 (ERK1/2) signal pathway in the regulation of Compound Danshen Injection (CDI) induced AQP3 expression in the human amniotic epithelial cells (hAECs).</p><p><b>METHODS</b>hAECs of term pregnancy with normal amniotic fluid volume (AFV) or isolated oligohydramnios were primarily cultured. And the cells were equally divided into four groups, i.e., the vehicle control group, the U0126 group, the CDI group, the CDI + U0126 group. The expressions of phosphorylated ERK1/2 (p-ERK1/2) and AQP3 in hAECs were detected using Western blot analysis.</p><p><b>RESULTS</b>(1) When compared with the control group, the expression level of p-ERK1/2 in hAECs in those with normal AFV and oligohydramnios obviously decreased in the U0126 group (P < 0.05). The expression level of p-ERK1/2 could be elevated in the CDI group (P < 0.05). The expression level of p-ERK1/2 in hAECs was higher in the CDI +U0126 group than in the U0126 group, but lower in the CDI + U0126 group than in the CDI group (P < 0.05). (2) There was no obvious change in AQP3 expression in hAECs with normal AFV between the U0126 group and the vehicle control group (P > 0.05). There was no statistical difference in the expression level of AQP3 between the CDI group and the U0126 +CDI group (P > 0.05), but they were higher than those in the vehicle control group (P < 0.05). (3) Compared with the vehicle control group, the expression level of AQP3 in hAECs with oligohydramnios significantly decreased in the U0126 group and increased in the CDI group (P < 0.05). The expression level of AQP3 was lower in the U0126 + CDI group than in the CDI group, but higher in the U0126 +CDI group than in the U0126 group (P < 0.05).</p><p><b>CONCLUSION</b>CDI could regulate AQP3 expression level in hAECs with oligohydramnios via activating the MAPK-ERK1/2 signal transduction pathway.</p>
Assuntos
Feminino , Humanos , Âmnio , Biologia Celular , Aquaporina 3 , Metabolismo , Células Cultivadas , Medicamentos de Ervas Chinesas , Farmacologia , Células Epiteliais , Metabolismo , Sistema de Sinalização das MAP Quinases , Fenantrolinas , FarmacologiaRESUMO
<p><b>OBJECTIVE</b>To investigate the effects of Danshen Injection (DSI) on the proliferation of rheumatoid arthritis fibroblast-like synoviocytes (RA FLSs) cultured in RA patients' serum.</p><p><b>METHODS</b>The RA FLSs harvested from RA patients' synovial fluid were primarily cultured by routines. The cells were cultured with 10% inactivated human serum (the healthy human serum and the RA patients' serum) for 24 h. Then DSI at the final concentration of 0. 4 mg/mL was added in the cells for further 24 h culture. By taking 10% fetal calf serum as the control, the morphological changes were observed under optical microscope. The proliferation was analyzed by MTT. The apoptosis was detected by flow cytometry. The total RNA was extracted and reverse transcription was performed. The Bax mRNA expression was detected by fluorescent quantitative PCR.</p><p><b>RESULTS</b>(1) After human serum was added in the healthy human serum and RA patients' serum, cells could grow adhering to the wall. Compared with the fetal calf serum group (FCS), the cell density was higher in the healthy human serum group than in the fetal calf serum group, with no obvious morphological changes. (2) MTT results showed that, compared with the fetal calf serum group, the absorbance value (OD) obviously increased in the healthy human serum group and the RA patients' serum group, showing statistical difference (P <0.01). After adding DSI at the final concentration of 0.4 mg/mL, cells from different serums were inhibited to various degrees (with OD significantly decreased, P <0.05). The OD value significantly increased more in the healthy human serum group and the RA patients' serum group than in the fetal calf serum group, showing statistical difference (P <0.01). There was statistical difference between the healthy human serum group and the RA patients' serum group (P <0.01). (3) The apoptosis rate in the RA patients' serum group obviously decreased with statistical difference, when compared with the Salvia miltiorrhiza free fetal calf serum group (P >0. 01). The apoptosis rate in the fetal calf serum group and the RA patients' serum group significantly increased after adding 0.4 mg/mL Salvia miltiorrhiza, showing statistical difference when compared with the Salvia miltiorrhiza free fetal calf serum group and the Salvia miltiorrhiza free RA patients' serum group (P <0.05). The FLSs were effected by 0.4 mg/mL Salvia miltiorrhiza, the apoptosis rate significantly decreased in the healthy human serum group and the RA patients' serum group, showing statistical difference when compared with the fetal calf serum group (P <0. 05, P <0.01). (4) The expression of Bax gene significantly increased in the RA patients' serum group and the fetal calf serum group after action of 0.4 mg/mL Salvia miltiorrhiza, showing statistical difference (P <0. 01). When 0.4 mg/mL Salvia miltiorrhiza was added, the expression of Bax mRNA obviously increased in the healthy human serum group and the RA patients' serum group, showing statistical difference when compared with the fetal calf serum group (P <0.01).</p><p><b>CONCLUSIONS</b>(1) Although healthy human serum can be favorable to the growth of RA FLSs, the fetal calf serum could reflect the actual results better in the cyto biological research on specific diseases (if there is no serum from patients with corresponding disease). (2) DSI could inhibit the proliferation of RA FLSs through promoting their apoptosis.</p>
Assuntos
Humanos , Apoptose , Artrite Reumatoide , Patologia , Proliferação de Células , Células Cultivadas , Meios de Cultura , Química , Medicamentos de Ervas Chinesas , Farmacologia , Fibroblastos , Biologia Celular , Fenantrolinas , Farmacologia , Salvia miltiorrhiza , Membrana Sinovial , Biologia CelularRESUMO
<p><b>OBJECTIVE</b>To explore the protective effects of danshen (Salvia Miltiorrhiza) on vascular endothelial cells in hypertension patients in the gestation period.</p><p><b>METHODS</b>The umbilical vein endothelial cells pre-incubated with Danshen solution at different concentrations (0, 100, 200, and 300 mg/L) were randomly divided into 3 groups, i.e., the blank control group (8 cases), the normal control group (14 cases, cultured in the serum from 14 normal pregnant women), and the observation group (14 cases, cultured in the serum from 14 pregnant women with severe pre-eclampsia). The levels of nitric oxide (NO) and endothelin-1 (ET-1) in each culture supernatant were detected respectively.</p><p><b>RESULTS</b>The ET-1 level was higher in 300 mg/L Danshen solution group than in 0 mg/L and 100 mg/L Danshen solution groups (P <0.05). The NO level was lower in the observation group than in the blank control group and the normal control group (P <0. 05). The NO level was higher in 200 mg/L Danshen solution group than in 0 mg/L Danshen solution group (P <0.05). The NO level was higher in 300 mg/L Danshen solution group than in 0 mg/L, 100 mg/L, and 200 mg/L Danshen solution groups (P <0.05).</p><p><b>CONCLUSION</b>Danshen could increase the secretion of NO from in vitro umbilical vein endothelial cells cultured in the serum from patients with pre-eclampsia, and reduce the secretion of ET-1.</p>
Assuntos
Feminino , Humanos , Gravidez , Células Cultivadas , Meios de Cultura , Química , Medicamentos de Ervas Chinesas , Farmacologia , Células Endoteliais , Biologia Celular , Secreções Corporais , Endotelina-1 , Metabolismo , Óxido Nítrico , Metabolismo , Fenantrolinas , Farmacologia , Pré-Eclâmpsia , Sangue , Metabolismo , Salvia miltiorrhiza , Química , Soro , Química , Veias Umbilicais , Biologia CelularRESUMO
<p><b>OBJECTIVE</b>To investigate the effect of active components of Danshen and Shanzha of different matching proportions on atherosclerosis (AS), in the expectation of obtaining the optimum combination method.</p><p><b>METHOD</b>Atherosclerotic rats were fed with high fat diet, and injected with vitamin D3 and ovalbumin. Aqueous extracts of Danshen (DSA) and Shanzha (SZA) and lipophilic extracts of danshen (DSL) were adopted for a low, medium and high-dose orthogonal experiment, to observe the effect of their different matching proportions on lipid level, oxidative stress, endothelial function and inflammatory reaction. The principal component analysis and cluster analysis were adopted for the multi-objective optimization of experimental results.</p><p><b>RESULT</b>Compared with the model group, all of samples with different proportions of DSA, DSL and SZA showed effect in lowering lipid level, scavenging free radicals, reducing endothelial dysfunction and inhibiting inflammation. According to the variance analysis, DSA2-SZA2-DSL1, DSA3-SZA2-DSL1, DSA3-SZA3 -DSL3 and DSA3-SZA1-DSL1 were the optimal proportions for lowering lipid level, scavenging free radicals, reducing endothelial dysfunction and inhibiting inflammation, respectively. According to the results of the multi-objective optimization, DSA2-SZA1-DSL2 was the optimal proportions of anti-AS.</p><p><b>CONCLUSION</b>All of active components of Danshen and Shanzha of different matching proportions show the anti-AS effect in rats to varying degrees, but with different focus in different matching proportions.</p>
Assuntos
Animais , Masculino , Ratos , Anti-Inflamatórios , Farmacologia , Antioxidantes , Farmacologia , Aterosclerose , Tratamento Farmacológico , Medicamentos de Ervas Chinesas , Usos Terapêuticos , Endotélio Vascular , Lipídeos , Sangue , Fenantrolinas , Usos Terapêuticos , Fitoterapia , Salvia miltiorrhiza , QuímicaRESUMO
Patent network of Chinese patent medicines is a patent group composed of several correlated patents around basic patents or core technologies characterized by traditional Chinese medicine technologies. With the clue of Tianjin Tasly Group's acquisition of seven compound Danshen patents characterized by extract feeds of Beijing Cairui Pharmaceutical Co., Ltd., we made an analysis on how Tasly builds a patent network themed on compound Danshen preparation products characterized by extract feeds, in hope of providing reference for other Chinese pharmaceutical enterprise to establish and improve key patent networks of traditional Chinese medicines.
Assuntos
Química Farmacêutica , Recursos Humanos , Métodos , China , Medicamentos de Ervas Chinesas , Medicina Tradicional Chinesa , Métodos , Patentes como Assunto , Fenantrolinas , Salvia miltiorrhiza , QuímicaRESUMO
Leishmanioses são um grupo de doenças com um largo espectro de manifestações clínicas, as quais variam desde lesões cutâneas até o envolvimento visceral severo, podendo levar ao ótibo. A leishmaniose é, ainda hoje, uma doença negligenciada, estando entre os agravos prioritários do programa de pesquisa sobre doenças da pobreza da Organização Mundial da Saúde (OMS). Além de não haver vacinas disponíveis, a terapia é baseada em medicamentos injetáveis que causam sérios efeitos colaterais, tornando o tratamento inviável para muitos países endêmicos. Drogas derivadas de metal representam um novo arsenal terapêutico antimicrobiano e anti-câncer. Os inibidores de peptidase/agentes quelantes tais como 1,10-fenantrolina e seus derivados, no estado livre de metal ou como ligantes com metais de transição, interferem com a função de vários sistemas biológicos. Em trabalhos anteriores, nosso grupo descreveu que o parasito L. braziliensis produziu moléculas gp63 sensíveis a 1,10-fenantrolina. No presente trabalho, demonstramos a distribuição celular da molécula gp63 em uma cepa virulenta de L. braziliensis por meio de análises bioquímicas e imuno-histoquímica. Depois disso, relatamos os efeitos inibitórios de três compostos derivados da 1,10-fenantrolina, 1,10-fenantrolina-5,6-dioma (phendio), [Cu(phendio)2] e [Ag(phendio)2], nas atividades metalopeptidases celulares e extracelulares produzidas por promastigotas de L. braziliensis, bem como as suas ações sobre a viabilidade do parasita e na interação com as células de macrófagos murinos. As moléculas gp63 foram detectadas em compartimentos de parasitos, incluindo membrana citoplasmatica e bolsa flagelar. O tratamento de promastigotas de L. braziliensis durante 1 hora com 1,10-fenantrolina e seus derivados resultou numa inibição significativa da viabilidade celular e mostrou um mecanismo de ação irreversível. Estes inibidores de metalopeptidases induziram apoptose em promastigotas de L. braziliensis, demonstrada através ...
Leishmaniasis is a group of diseases with a wide spectrum of clinical manifestations, which range from self-limited skin lesions to severe visceral involvement that can lead to death. Leishmaniasis is still a neglected disease, and it is among the priorities of the research program on diseases of poverty of World Health Organization (TDR/WHO). There is no available vaccine and the treatment is based on drugs that cause serious side effects, and are unaffordable in several endemic countries. Metal-based drugs represent a novel antimicrobial and anti-cancer therapeutics arsenal. Peptidase inhibitors/chelating agents such as 1,10-phenanthroline and its substituted derivatives, either the metal-free state or as ligands coordinated to transition metals, interfere with crucial functions of several biological systems. In previous works, our group described that L. braziliensis produced gp63 molecules sensible to 1,10-phenanthroline. Herein, we initially studied the cellular distribution of gp63 in a virulent strain of L. braziliensis by biochemical and immunocytochemical analyses. After that, we reported the inhibitory effects of three 1,10-phenanthroline derivative compounds, 1,10-phenanthroloine-5,6-dione (phendio), [Cu(phendio)2] and [Ag(phendio)2], on both cellular and extracellular metallopeptidase activities produced by L. braziliensis promastigotes as well as their actions on the parasite viability and on the interaction with murine macrophage cells. The gp63 molecules were detected in several parasite compartments, including cytoplasm, membrane lining the cell body and flagellum, and flagellar pocket. The treatment of L. braziliensis promastigotes for 1 hour with 1,10-phenanthroline and its derivatives resulted in a significant inhibition of cell viability and showed an irreversible mechanism of action. These metallopeptidase inhibitors induced apoptosis in L. braziliensis promastigotes as judged by annexin/propidium iodide staining and TUNEL assays ...
Assuntos
Animais , Masculino , Feminino , Ratos , Fenantrolinas/administração & dosagem , Fenantrolinas/uso terapêutico , Inibidores de Proteases/uso terapêutico , Leishmania braziliensis , Leishmania braziliensis/enzimologia , Antiprotozoários/uso terapêutico , Leishmaniose/tratamento farmacológico , Metais/química , Metaloproteases/antagonistas & inibidores , Quelantes/administração & dosagemRESUMO
<p><b>OBJECTIVE</b>To assess the effect of Danshen on liver regeneration capacity of carbon tetrachloride-induced liver injury rats.</p><p><b>METHOD</b>Computer retrieval of data from CJFD, CBM, Chinese science & technology journal full-text database and Chinese medical association digital journals, and such foreign databases as PubMed, EMBASE and SCI was included in the randomized controlled trials (RCT) of rat liver injury induced by carbon tetrachloride,with the search as at May 2012. A Meta analysis was made using Rev-Man 5.1 software. Using the GRADE system to addess five outcomes in stuay.</p><p><b>RESULT</b>Two hundred and fourteen rats got involved in seven randomized trials. Meta analysis showed there were statistical differences between the Danshen group and the control group in alanine aminotransferase (ALT), aspartate aminotransferase (AST), superoxide dismutase (SOD), tumor necrosis factor-alpha (TNF-alpha) and hyaluronic acid (HA) after rat liver injury induced by carbon tetrachloride. When we used system to each outcome, because of serious limitations and indirect, they are all very low quality.</p><p><b>CONCLUSION</b>Danshen shows certain promoting effect to liver regeneration in carbon tetrachloride-induced liver injury rats.</p>
Assuntos
Animais , Humanos , Ratos , Tetracloreto de Carbono , Doença Hepática Induzida por Substâncias e Drogas , Genética , Metabolismo , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas , Farmacologia , Regeneração Hepática , Fenantrolinas , Farmacologia , Salvia miltiorrhiza , QuímicaRESUMO
<p><b>OBJECTIVE</b>To analyze the clinical effectiveness of Compound Danshen Injection (CDI) in treating patients with early onset severe preeclampsia.</p><p><b>METHODS</b>One hundred and twenty patients with early onset severe preeclampsia were recruited and their gestational age ranged between 26 and 34 weeks. Sixty patients who volunteered to receive CDI were recruited as the treatment group, while 60 inpatients were recruited as the control group at the same time period. The routine therapy was given to those in the control group. CDI was intravenously dripped to those in the treatment group additionally by adding in 250 mL 5% glucose injection, once daily. The treatment for all lasted for 7 successive days. The D-dimer (DD), fibrinogen (Fg), hematocrit (HCT), tissue plasminogen activator (t-PA), plasminogen activator inhibitor-1 (PAI-1), mean arterial pressure (MAP), 24 h urine volume (UV), 24 h urine protein (24 hUP), triglyceride (TG), total cholesterol (TC), high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein A (apoA1), apolipoprotein B (apoB), umbilical arterial S/D ratio (S/D), and amniotic fluid index (AFI) were compared between the two groups before and after treatment. The placenta weight (PW), neonatal weight (NW), 1 min Apgar scoring were compared between the two groups before and after treatment.</p><p><b>RESULTS</b>There was no difference in DD, Fg, HCT, t-PA, PAI-1, MAP, UV, 24 hUP, TC, TG, HDL-C, LDL-C, apoA1, apoB, S/D, or AFI between the two groups before treatment (P>0.05). In the treatment group PAI-1, Fg, and 24 hUP decreased more after treatment, and they were lower than those of the control group after treatment. The UV and AFI increased and they were higher than those of the control group after treatment with statistical difference shown (P<0.05, P<0.01). In the control group the UV increased and 24 hUP decreased after treatment (P<0.01). There was no improvement in the rest indices (P>0.05). The PW, NW,and 1 min Apgar score > or = 7 were all higher in the treatment group than in the control group, showing statistical difference (P<0.05).</p><p><b>CONCLUSION</b>CDI was helpful to improve the high condensation state of patients with early onset severe preeclampsia, protect important organs of the mother, and improve the prognosis of neonates.</p>
Assuntos
Adulto , Feminino , Humanos , Gravidez , Adulto Jovem , Medicamentos de Ervas Chinesas , Usos Terapêuticos , Fenantrolinas , Usos Terapêuticos , Fitoterapia , Pré-Eclâmpsia , Tratamento FarmacológicoRESUMO
<p><b>OBJECTIVE</b>To study the effects of using Compound Danshen Injection (CDI) and low molecular weight heparin (LMWH) on early severe preeclampsia women.</p><p><b>METHODS</b>Retrospective analysis was carried out in 95 patients with early severe preeclampsia from October 2008 to January 2011. They were assigned to 3 groups based on anticoagulant drugs. The routine therapy of magnesium sulfate (MgSO4) was given to the MgSO4 group (40 cases); the MgSO4 + CDI was given to those in the CDI group (23 cases), the MgSO4 + LMWH group was given to those in the LMWH group (32 cases). The general data of all patients were collected to analyze their effects on labor, postpartum hemorrhage, reasons for terminating the pregnancy, and maternal complications.</p><p><b>RESULTS</b>(1) The average gestational week (weeks) of terminating the pregnancy was 31.7 +/- 1.9 in the MgSO4 group, 33.0 +/- 1.8 in the CDI group, and 32.8 +/- 1.7 in the LMWH group. The average weight of newborn babies (g) was 1 450.5 +/- 402.3 in the MgSO4 group, 1 582.2 +/- 332.5 in the CDI group, and 1 590.0 +/- 340.1 in the LMWH group. There was no obviously difference in the average gestational weeks or the average weight of newborn babies among the three groups. (2) The way of terminating the pregnancy was uterine-incision delivery. The main reasons for operation were sequenced as maternal complications, unsatisfied control of the blood pressure, and fetal distress. (3) The maternal complications in the three groups were sequenced as renal failure (12 cases), placental abruption (9 cases), hemolysis, increased liver enzymes and low platelet (HELLP) syndrome (8 cases). Sixteen (40.0%) had complications in the MgSO4 group, 12 (52.2%) in the CDI group, and 15 (46.9%) in the LMWH group. No statistic difference existed among the 3 groups.</p><p><b>CONCLUSIONS</b>LMWH and CDI were helpful to improving the therapeutic effects of severe preeclampsia patients. They did not increase adverse drug reactions. They seemingly had effects on prolonging the gestational week.</p>
Assuntos
Adulto , Feminino , Humanos , Gravidez , Medicamentos de Ervas Chinesas , Usos Terapêuticos , Heparina de Baixo Peso Molecular , Usos Terapêuticos , Sulfato de Magnésio , Usos Terapêuticos , Fenantrolinas , Usos Terapêuticos , Pré-Eclâmpsia , Tratamento Farmacológico , Resultado da Gravidez , Estudos RetrospectivosRESUMO
<p><b>OBJECTIVE</b>To establish a method for monitoring the quality of intermediates generated in each working procedure during the production process of traditional Chinese medicine (TCM) , in order to ensure the batch-to-batch quality consistency of TCM products.</p><p><b>METHOD</b>The multistage multivariate statistic quality control (MMSQC) was proposed to monitor production quality of TCMs based on multivariate data analysis technique. Hotelling T2 and SPE were adopted for monitoring the quality of intermediates generated in each working procedure. Danshen injection was taken as the example to introduce the application method of MMSQC.</p><p><b>RESULT</b>MMSQC can monitor the quality of intermediates generated in multiple working procedures, which is simpler and more accurate compared with single-indicator monitoring method.</p><p><b>CONCLUSION</b>MMSQC can be popularized to monitor quality of multistage production of TCMs.</p>
Assuntos
Medicamentos de Ervas Chinesas , Química , Padrões de Referência , Medicina Tradicional Chinesa , Padrões de Referência , Fenantrolinas , Química , Padrões de Referência , Controle de Qualidade , Salvia miltiorrhiza , QuímicaRESUMO
<p><b>OBJECTIVE</b>To compare the anaphylactoid effect of Danshen injection and its components on guinea pig.</p><p><b>METHOD</b>Applying active systemic anaphylaxis (ASA) tests, the corresponding experimental injections were administrated to guinea pigs to sensitized, and allergen with double doses was injected to stimulate in the 11 days after the last sensitized. The anaphylaxis situation of guinea pigs was observed.</p><p><b>RESULT</b>Danshen injection and its components are suspicion on guinea pigs, while negative reaction was observed on guinea pigs which injected by the liquid excipients of Danshen injection.</p><p><b>CONCLUSION</b>Danshen injection using the ultrafiltration method still have some antigenic impurities which cannot be removed completely, and this may be one of the reasons for anaphylactic reaction.</p>
Assuntos
Animais , Feminino , Masculino , Anafilaxia , Medicamentos de Ervas Chinesas , Toxicidade , Cobaias , Injeções , Métodos , Fenantrolinas , Toxicidade , Salvia miltiorrhiza , Química , ToxicidadeRESUMO
<p><b>OBJECTIVE</b>To observe the effect of Danshen Chuanxiongqin Injection (DCI) on the myocardial damage of unstable angina (UA) patients undergoing percutaneous coronary intervention (PCI).</p><p><b>METHODS</b>76 UA patients were randomly assigned to the test group (39 cases) and the control group (37 cases). Routine treatment of Western medicine and PCI were given to all patients. But 10 mL DCI was intravenously dripped to patients in the test group by adding in 250 mL normal saline three to five days before PCI, once daily, lasting for 7 to 10 days. Changes of platelet P-selectin positive expressions before and after medication, the thrombolysis in myocardial infarction (TIMI), myocardial perfusion (TMP) score, levels of creatine kinase-myocardial band (CK-MB) and troponin I (TnI) after PCI were observed in the two groups.</p><p><b>RESULTS</b>After medication the P-selectin positive expressions was lower in the test group than in the control group (2.45% +/- 1.42% vs 4.43% +/- 1.79%, P<0.05). After PCI the incidence of TMP 0/1, the levels of CK-MB and TnI were lower in the test group than in the control group at the same phase, showing statistical difference (P<0.05). No cardiac event occurred in the two groups during the hospital stay.</p><p><b>CONCLUSION</b>Administration of DCI before PCI could effectively inhibit the activation of platelets, improve post-operative myocardial blood perfusion, and lower the incidence of the myocardial damage.</p>
Assuntos
Adulto , Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Angina Instável , Sangue , Terapêutica , Creatina Quinase , Sangue , Medicamentos de Ervas Chinesas , Farmacologia , Miocárdio , Metabolismo , Patologia , Intervenção Coronária Percutânea , Fenantrolinas , Farmacologia , Pirazinas , Farmacologia , Troponina I , SangueRESUMO
<p><b>OBJECTIVE</b>To study the protective effects of nerve growth factor (NGF) and Danshen on hippocampal neurons in gerbils (Meriones unguiculatus) with global ischemia-reperfusion injury.</p><p><b>METHODS</b>Global ischemia-reperfusion model was established in 54 male Z:ZCLA gerbils by occlusion of the bilateral carotid arteries. The animal models were randomized into 3 groups to receive treatment with normal saline, NGF, and Danshen 30 min after the reperfusion. At 6 h, 3 and 7 days after the reperfusion, the survival of the hippocampal CA1 pyramidal neurons was observed using optical and electron microscopy, and immunohistochemistry was employed to detect the expressions of Bcl-2 and Bax in the neurons.</p><p><b>RESULTS</b>Neuronal apoptosis was not observed in the hippocampus 6 h after the reperfusion, but at 3 and 7 days, the number of apoptotic neurons increased significantly in the CA1 region. Compared with normal saline, treatments with NGF and Danshen both significantly reduced the number of apoptotic neurons at 3 and 7 days. The number of apoptotic neurons showed no significant difference between NGF and Danshen treatment groups at 3 days, but at 7 days, the apoptotic cell number was significantly lower in NGF group (P<0.05). Bcl-2 expression was the highest in NGF group, and its highest expression occurred at 6 h after the reperfusion; Bax expression was detected in saline group, and underwent no significant changes with the passage of time.</p><p><b>CONCLUSION</b>Both NGF and Danshen show protective effects against global ischemia-reperfusion injury. NGF has a stronger protective effect than Danshen, and this finding provides experimental evidence for selecting appropriate protective agents in the treatment of ischemic brain damage.</p>
Assuntos
Animais , Masculino , Isquemia Encefálica , Tratamento Farmacológico , Medicamentos de Ervas Chinesas , Farmacologia , Gerbillinae , Hipocampo , Biologia Celular , Metabolismo , Fator de Crescimento Neural , Farmacologia , Neurônios , Fármacos Neuroprotetores , Farmacologia , Fenantrolinas , Farmacologia , Traumatismo por Reperfusão , Tratamento Farmacológico , Salvia miltiorrhizaRESUMO
<p><b>OBJECTIVE</b>To study the effects of Compound Danshen Dripping Pill (CDDP) on the structure and functions of sternohyoid muscle in metabolic syndrome (MS) rats, and to study whether it has therapeutic effects on obstructive sleep apnea-hypopnea syndrome (OSAHS).</p><p><b>METHODS</b>Twenty-one healthy male SD rats were randomly divided into three groups, i.e., the normal control group (n = 6), the MS group (n = 8), and the CDDP group (n = 7). Rats in the normal control group were routinely fed. High lipid forage was given to rats in the rest two groups. Nine weeks later, CDDP (at the dose of 375 mg/kg) was additionally given to rats in the CDDP group by gastrogavage, and then rats in the CDDP group and the MS group were fed with the same high lipid forage for 12 successive weeks. The content of malondialdehyde (MDA) and the activities of superoxide dismutase (SOD) in the sternohyoid muscle were detected in the three groups. The capillary density, capillary-to-fiber ratio (C/F), the section area of type I muscle fiber were detected using myosin-ATPase histochemical assay. The contractile changes of isometric stemohyoid muscles were determined under electric stimulation by different frequencies.</p><p><b>RESULTS</b>The contents of MDA were obviously lower in the CDDP group than in the MS group, while the activities of SOD, the capillary density, C/F, the section area of type I muscle fiber, the tension of stemohyoid muscle at 10 -60 Hz, and the 1-5 min tension percentages of the stemohyoid muscle were higher in the CDDP group than in the MS group (P < 0.05, P < 0.01).</p><p><b>CONCLUSION</b>CDDP could improve oxidative stress induced intramuscularly microcirculation disturbance and changes of muscular fiber structures of the upper airway muscles, and elevate their contractile functions, thus possibly contributing to favorable effects on OSAHS.</p>