RESUMO
This research is to predict anti-Alzheimer's disease active constituents on the target of acetylcholinesterase(AChE) from Glycyrrhizae Radix et Rhizoma with the help of pharmacophore and molecular docking. AChE ligand-based pharmacophore model was set up and the molecular library of the constituents from Glycyrrhizae Radix et Rhizoma were established by collecting literature. Then the constituents from Glycyrrhizae Radix et Rhizoma were screen for the potential AChE inhibitory potency in silico through matching with the best pharmacophore model. The flexible docking was used to evaluate the interactions between compounds screened from pharmacophore model and AChE protein(PDB ID:4 EY7). The interactions were expressed including but not limited to CDOCKER interaction energy, hydrogen bonds and non-bonding interactions. The molecular library of Glycyrrhizae Radix et Rhizoma contains 44 chemical constituents. As for the pharmacophore model, six kinds of potential AChE inhibitory constituents from Glycyrrhizae Radix et Rhizoma were considered to be the promising compounds according to the results of searching 3 D database of pharmacophore model. The molecular docking was possessed and the interaction patterns were given to show the detail interactions. The compounds screening from the pharmacophore model were consistent with the existing studies to some degree, indicating that the virtual screen protocols of AChE inhibitory constituents from Glycyrrhizae Radix et Rhizoma based on pharmacophore and molecular docking was reliable.
Assuntos
Medicamentos de Ervas Chinesas , Glycyrrhiza , Triterpenos , Simulação de Acoplamento Molecular , RizomaRESUMO
This research is to predict anti-Alzheimer's disease active constituents on the target of acetylcholinesterase(AChE) from Glycyrrhizae Radix et Rhizoma with the help of pharmacophore and molecular docking. AChE ligand-based pharmacophore model was set up and the molecular library of the constituents from Glycyrrhizae Radix et Rhizoma were established by collecting literature. Then the constituents from Glycyrrhizae Radix et Rhizoma were screen for the potential AChE inhibitory potency in silico through matching with the best pharmacophore model. The flexible docking was used to evaluate the interactions between compounds screened from pharmacophore model and AChE protein(PDB ID:4 EY7). The interactions were expressed including but not limited to CDOCKER interaction energy, hydrogen bonds and non-bonding interactions. The molecular library of Glycyrrhizae Radix et Rhizoma contains 44 chemical constituents. As for the pharmacophore model, six kinds of potential AChE inhibitory constituents from Glycyrrhizae Radix et Rhizoma were considered to be the promising compounds according to the results of searching 3 D database of pharmacophore model. The molecular docking was possessed and the interaction patterns were given to show the detail interactions. The compounds screening from the pharmacophore model were consistent with the existing studies to some degree, indicating that the virtual screen protocols of AChE inhibitory constituents from Glycyrrhizae Radix et Rhizoma based on pharmacophore and molecular docking was reliable.
Assuntos
Medicamentos de Ervas Chinesas , Glycyrrhiza , Simulação de Acoplamento Molecular , Rizoma , TriterpenosRESUMO
This study aimed to extract and identify anthocyanins from Nitraria tangutorun Bobr. seed meal and establish a green analytical method of anthocyanins. Ultrasound-assisted extraction of anthocyanins from N. tangutorun seed meal was optimized using response surface methodology. Extraction at 70°C for 32.73 min using 51.15% ethanol rendered an extract with 65.04mg/100g of anthocyanins and 947.39mg/100g of polyphenols. An in vitro antioxidant assay showed that the extract exhibited a potent DPPH radical-scavenging capacity. Eight anthocyanins in N. tangutorun seed meal were identified by HPLC-MS, and the main anthocyanin was cyanidin-3-O-(trans-p-coumaroyl)-diglucoside (18.17mg/100g). A green HPLC-DAD method was developed to analyse anthocyanins. A mixtures of ethanol and a 5% (v/v) formic acid aqueous solution at a 20:80 (v/v) ratio was used as the optimized mobile phase. The method was accurate, stable and reliable and could be used to investigate anthocyanins from N. tangutorun seed meal.
Assuntos
Antocianinas/análise , Magnoliopsida/química , Extratos Vegetais/análise , Cromatografia Líquida de Alta Pressão/métodos , Espectrometria de Massas , Polifenóis/análise , Sementes/químicaRESUMO
Estrogen deficiency is one of the major causes of osteoporosis in postmenopausal women. Drynariae Rhizoma is a widely used traditional Chinese medicine for the treatment of bone diseases. In this study, we investigated the therapeutic effects of the total Drynariae Rhizoma flavonoids (DRTF) on estrogen deficiency-induced bone loss using an ovariectomized rat model and osteoblast-like MC3T3-E1 cells. Our results indicated that DRTF produced osteo-protective effects on the ovariectomized rats in terms of bone loss reduction, including decreased levels of bone turnover markers, enhanced biomechanical femur strength and trabecular bone microarchitecture deterioration prevention. In vitro experiments revealed that the actions of DRTF on regulating osteoblastic activities were mediated by the estrogen receptor (ER) dependent pathway. Our data also demonstrated that DRTF inhibited osteoclastogenesis via up-regulating osteoprotegrin (OPG), as well as down-regulating receptor activator of NF-κB ligand (RANKL) expression. In conclusion, this study indicated that DRTF treatment effectively suppressed bone mass loss in an ovariectomized rat model, and in vitro evidence suggested that the effects were exerted through actions on both osteoblasts and osteoclasts.
RESUMO
BACKGROUND: High- and low-flux hemodialysis (HFHD and LFHD, respectively) are dialysis procedures designed to eliminate blood toxins that accumulate in end-stage renal disease. HFHD may reduce vascular calcification by removing serum fibroblast growth factor 23 (FGF-23). However, whether HFHD is better than LFHD is still under debate. We therefore compared the efficacy of HFHD and LFHD in controlling FGF-23 and vascular calcification. MATERIAL AND METHODS: Fifty hemodialysis patients were recruited and randomly treated with either HFHD or LFHD. Fasting venous blood was collected at baseline, six months, and twelve months after the treatment. We then measured levels of FGF-23, calcium, phosphorus, parathyroid hormone, and alkaline phosphatase. Further, abdominal lateral radiographs were taken to calculate aorta abdominalis calcification scores (AACs). RESULTS: Compared to the LFHD group, FGF-23 and AACs in the HFHD group significantly decreased after 12 months treatment (p=0.049 and p=0.002, respectively). AACs were positively correlated with FGF-23 in all patients (p=0.004), the HFHD group alone (p=0.040), and the LFHD group alone (p=0.037). We also found that older patients, patients with higher blood phosphorus levels, and higher FGF-23 levels had an increased risk of aorta abdominalis calcification (p=0.048, p=0.003, p=0.001, respectively). HFHD was more able to reduce the risk of aorta abdominalis calcification than LFHD (p=0.003). CONCLUSIONS: FGF-23 is an independent risk factor for the development of vascular calcification. HFHD may benefit hemodialysis patients by reducing serum FGF-23 levels and controlling vascular calcification.
Assuntos
Fatores de Crescimento de Fibroblastos/sangue , Regulação da Expressão Gênica , Falência Renal Crônica/sangue , Insuficiência Renal Crônica/sangue , Calcificação Vascular/sangue , Adulto , Idoso , Fosfatase Alcalina/sangue , Fosfatase Alcalina/metabolismo , Aorta Abdominal/patologia , Cálcio/sangue , Feminino , Fator de Crescimento de Fibroblastos 23 , Humanos , Falência Renal Crônica/terapia , Masculino , Pessoa de Meia-Idade , Hormônio Paratireóideo/sangue , Fósforo/sangue , Radiografia Abdominal , Análise de Regressão , Diálise Renal , Insuficiência Renal Crônica/terapia , Fatores de RiscoRESUMO
OBJECTIVE: To compare the effects on anesthesia recovery between assisted-electroacupuncture fast tracking anesthesia and simple fast tracking anesthesia in patients with minim ally invasive percutaneous nephrolithotomy (mPCNL). METHODS: Eighty cases of mPCNL were selected and randomly divided into a treatment group and a control group. Fentanyl (1-2 microg/kg), sevoflurane (8%) and rocuronium (0.5 mg/kg) were applied to perform anesthesia induction in both groups, and endotracheal inhalation of sevoflurane and intravenous pump injection of remifentanil were adopted to main anesthesia status during the operation. 20 min before anesthesia induction, bilateral Neiguan (PC 6), Neimadian, Hegu (LI 4), Yangxi (LI 5), Zhongji (CV 3), Qichong (ST 30), Zuwuli (LR 10) were selected and punctured in the treatment group, and elecctroacupuncture was given after arrival of qi until 30 min after the wake-up from anesthesia and withdrawal of endotracheal tube. The dosage for anesthesia maintenance, recovery time of awareness, extubation time, incidences of nausea, vomiting and chill and irritation of urethral catheters were observed and recorded. RESULTS: (1) The dosages of remifentanil and sevoflurane in the treatment group during the operation were obviously less than those in the control group [remifentanil: (5. 27 +/-1.23) micro g/kg h vs (7.35+/-1.70) micro g/kg . h; sevoflurane: (1.12+/-0.43) vol% vs (2.35+/-0.87) vol% , both P<0. 001]. (2) The recovery time of awareness and extubation time in the treatment group were significantly earlier than those in the control group [recovery time of awareness: (5.65 +/- 2.34) min vs (8. 87 +/- 6. 84) min, P<0. 01; extubation time : (7. 23+/-4. 35) min vs (10. 62+/-8. 16) min, P<0. 05]. (3) The incidences of nausea, vomiting and chill in the treatment group were significantly less than those in the control group (all P<0. 05). (4) The irritation of urethral catheters on urethra in the treatment group was significantly less than that in the control group (P<0. 001). CONCLUSION: The assisted-electroacupuncture anesthesia could reduce the dosage of remifentanil and sevoflurane in mPCNL fast tracking anesthesia in urinary surgery, reduce the incidences of nausea, vomiting, chill and irritation of urethral catheters during recovery stage, and prompt recovery of mPCNL patients.
Assuntos
Período de Recuperação da Anestesia , Anestésicos Intravenosos/efeitos adversos , Eletroacupuntura , Náusea e Vômito Pós-Operatórios/terapia , Adolescente , Adulto , Anestésicos Intravenosos/administração & dosagem , Feminino , Fentanila/administração & dosagem , Fentanila/efeitos adversos , Humanos , Masculino , Éteres Metílicos/administração & dosagem , Éteres Metílicos/efeitos adversos , Pessoa de Meia-Idade , Nefrostomia Percutânea , Piperidinas/administração & dosagem , Piperidinas/efeitos adversos , Remifentanil , Sevoflurano , Adulto JovemRESUMO
<p><b>OBJECTIVE</b>To compare the effects on anesthesia recovery between assisted-electroacupuncture fast tracking anesthesia and simple fast tracking anesthesia in patients with minim ally invasive percutaneous nephrolithotomy (mPCNL).</p><p><b>METHODS</b>Eighty cases of mPCNL were selected and randomly divided into a treatment group and a control group. Fentanyl (1-2 microg/kg), sevoflurane (8%) and rocuronium (0.5 mg/kg) were applied to perform anesthesia induction in both groups, and endotracheal inhalation of sevoflurane and intravenous pump injection of remifentanil were adopted to main anesthesia status during the operation. 20 min before anesthesia induction, bilateral Neiguan (PC 6), Neimadian, Hegu (LI 4), Yangxi (LI 5), Zhongji (CV 3), Qichong (ST 30), Zuwuli (LR 10) were selected and punctured in the treatment group, and elecctroacupuncture was given after arrival of qi until 30 min after the wake-up from anesthesia and withdrawal of endotracheal tube. The dosage for anesthesia maintenance, recovery time of awareness, extubation time, incidences of nausea, vomiting and chill and irritation of urethral catheters were observed and recorded.</p><p><b>RESULTS</b>(1) The dosages of remifentanil and sevoflurane in the treatment group during the operation were obviously less than those in the control group [remifentanil: (5. 27 +/-1.23) micro g/kg h vs (7.35+/-1.70) micro g/kg . h; sevoflurane: (1.12+/-0.43) vol% vs (2.35+/-0.87) vol% , both P<0. 001]. (2) The recovery time of awareness and extubation time in the treatment group were significantly earlier than those in the control group [recovery time of awareness: (5.65 +/- 2.34) min vs (8. 87 +/- 6. 84) min, P<0. 01; extubation time : (7. 23+/-4. 35) min vs (10. 62+/-8. 16) min, P<0. 05]. (3) The incidences of nausea, vomiting and chill in the treatment group were significantly less than those in the control group (all P<0. 05). (4) The irritation of urethral catheters on urethra in the treatment group was significantly less than that in the control group (P<0. 001).</p><p><b>CONCLUSION</b>The assisted-electroacupuncture anesthesia could reduce the dosage of remifentanil and sevoflurane in mPCNL fast tracking anesthesia in urinary surgery, reduce the incidences of nausea, vomiting, chill and irritation of urethral catheters during recovery stage, and prompt recovery of mPCNL patients.</p>
Assuntos
Adolescente , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Adulto Jovem , Período de Recuperação da Anestesia , Anestésicos Intravenosos , Eletroacupuntura , Fentanila , Éteres Metílicos , Nefrostomia Percutânea , Piperidinas , Náusea e Vômito Pós-Operatórios , TerapêuticaRESUMO
Recent efforts to genetically engineer plants that contain fatty acid desaturases to produce valuable fatty acids have made only modest progress. Diacylglycerol acyltransferase 2 (DGAT2), which catalyzes the final step in triacylglycerol (TAG) assembly, might potentially regulate the biosynthesis of desired fatty acids in TAGs. To study the effects of tung tree (Vernicia fordii) vfDGAT2 in channeling the desired fatty acids into TAG, vfDGAT2 combined with the tung tree fatty acid desaturase-2 (vfFAD2) gene was co-introduced into Aspergillus fumigatus, an endophytic fungus isolated from healthy tung oilseed. Two transformants coexpressing vfFAD2 and vfDGAT2 showed a more than 6-fold increase in linoleic acid production compared to the original A. fumigatus strain, while a nearly 2-fold increase was found in the transformant expressing only vfFAD2. Our data suggest that vfDGAT2 plays a pivotal role in promoting linoleic acid accumulation in TAGs. This holds great promise for further genetic engineering aimed at producing valuable fatty acids.
Assuntos
Aspergillus fumigatus/genética , Diacilglicerol O-Aciltransferase/genética , Ácidos Graxos Dessaturases/genética , Genes Fúngicos , Óleos de Plantas , Sementes/microbiologia , Aspergillus fumigatus/isolamento & purificação , Sequência de Bases , Cromatografia Gasosa , Primers do DNA , Reação em Cadeia da PolimeraseRESUMO
BACKGROUND: Cardiopulmonary bypass may cause serious impairment of lung function. It has been reported that administration of mucosolvin can prevent acute respiratory insufficiency through the improvement of pulmonary surfactant. OBJECTIVES: This study aimed to explore the effects of high-dose mucosolvin on infant lungs following cardiopulmonary bypass. METHODS: One hundred infants were randomly divided into 2 groups. In Group 1, patients did not receive any respiratory drug perioperatively and underwent conventional mechanical ventilation postoperatively. In Group 2, patients were administered mucosolvin (15 mg/kg per day) perioperatively, and doxofylline (15 mg/kg per day) and ipratropium bromide solution (200 µg) were administrated postoperatively. Mechanical ventilation parameters, pulmonary surfactant-related protein (SP-B), and cytokines were evaluated after induction of anesthesia and 30 minutes, 24 hours, and 48 hours after CPB. RESULTS: At the end of CPB, all PaO2/FiO2 values in Group 2 were higher than those in Group 1. Postoperative SP-B levels in Group 1 decreased significantly compared to the baseline value (P < .05). There was no significant difference in hospitalization time between both groups, but both mechanical ventilation time and intensive care unit time of infants in Group 2 were significantly shorter than those in group 1 (P < .05). CONCLUSIONS: These findings indicate that high-dose mucosolvin has certain protective effects on respiratory functions in infants undergoing heart operations with CPB and that it that has no adverse effects.
Assuntos
Acetilcisteína/administração & dosagem , Procedimentos Cirúrgicos Cardíacos , Ponte Cardiopulmonar/efeitos adversos , Surfactantes Pulmonares/metabolismo , Insuficiência Respiratória/prevenção & controle , Doença Aguda , Método Duplo-Cego , Expectorantes/administração & dosagem , Feminino , Seguimentos , Humanos , Lactente , Masculino , Respiração Artificial , Insuficiência Respiratória/etiologia , Insuficiência Respiratória/metabolismo , Estudos Retrospectivos , Resultado do TratamentoRESUMO
Several nervous system injury models, such as sciatic crush and chronic cerebral hypoperfusion have been well studied in terms of neuroprotective effect of angelica injection. However, definitive experimental studies are lacking on diabetic peripheral neuropathy (DPN). This study sought to investigate the effects of angelica injection on DPN in type 1 diabetic rats. Diabetes was induced by single intraperitoneal injection of streptozotocin (STZ). To examine whether DPN model succeeded, tail-flick latency (TFL) and motor nerve conduction velocity (MNCV) were measured at 6 weeks after diabetes induction. Then, diabetic rats were treated with high- and low-dose angelica injection for 4 weeks. TFL, MNCV, morphology of sciatic nerve, myelinated nerve fiber density and the expressions of nerve growth factor (NGF) and brain derived neurotrophic factor (BDNF) in soleus and sciatic nerve were measured at 10 weeks after diabetes induction. The results showed the TFL was significantly shortened (p<0.001) and the MNCV was reduced (p<0.01) in diabetic rats compared with normal control rats at 6 weeks after diabetes induction. The TFL was obviously prolonged and the MNCV was further reduced in diabetic control group at 10 weeks after diabetes induction. TFL, MNCV and morphology of sciatic nerve were remarkably ameliorated and myelinated nerve fiber density and the expressions of NGF and BDNF in soleus and sciatic nerve were increased in the angelica treatment groups. This study suggests angelica injection has potential therapeutic effects on DPN, and the mechanism might be related to direct increase in NGF expression and direct or indirect increase in BDNF expression.
Assuntos
Angelica , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Diabetes Mellitus Experimental/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Fibras Nervosas Mielinizadas/efeitos dos fármacos , Fator de Crescimento Neural/metabolismo , Fitoterapia , Nervo Isquiático/efeitos dos fármacos , Análise de Variância , Animais , Western Blotting , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/patologia , Diabetes Mellitus Experimental/fisiopatologia , Masculino , Neurônios Motores/efeitos dos fármacos , Neurônios Motores/metabolismo , Músculo Esquelético/efeitos dos fármacos , Músculo Esquelético/metabolismo , Músculo Esquelético/patologia , Músculo Esquelético/fisiopatologia , Fibras Nervosas Mielinizadas/patologia , Condução Nervosa/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley , Recuperação de Função Fisiológica , Nervo Isquiático/metabolismo , Nervo Isquiático/patologia , Nervo Isquiático/fisiopatologiaRESUMO
This study assessed the neuroprotective effects of angelica injection in the rat sciatic nerve crush injury (SCI). Forty eight male Sprague Dawley rats were randomly divided into 4 groups: one was the sham group (S), which received sham surgery and given saline injection and the others were received SCI surgery and given saline injection, high and low dose angelica injection for 4 weeks, respectively. The sciatic functional index (SFI) in walking-track analysis, conductive velocity (CV), the number of fluorogold labeled motoneurons, and the expression patterns of brain derived neurotrophic factor (BDNF) and nerve growth factor (NGF) in the sciatic nerve and spine were examined. The results showed that SFI descended gradually on day 7, and dropped more quickly on day 28 in treatment groups (Low and High dose group). The CV in treatment groups was higher than control group (C). The numbers of motoneurons in treatment groups were larger than C group (P<0.05), but less than that in S group (P<0.01). The expressions of BDNF and NGF protein in the groups received SCI surgery were significantly lower than in S group, but the protein expressions in the groups received angelica injections were significantly higher than that in C group (P<0.01). These findings suggested that angelica injection can improve the sciatic nerve crush injury, and the mechanism might be through the increase of BDNF and NGF protein expression.
Assuntos
Angelica/química , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Regulação da Expressão Gênica/efeitos dos fármacos , Neurônios Motores/efeitos dos fármacos , Fatores de Crescimento Neural/metabolismo , Fitoterapia/métodos , Preparações de Plantas/administração & dosagem , Recuperação de Função Fisiológica/efeitos dos fármacos , Análise de Variância , Animais , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Masculino , Neurônios Motores/fisiologia , Condução Nervosa/efeitos dos fármacos , Condução Nervosa/fisiologia , Desempenho Psicomotor/efeitos dos fármacos , Ensaio de Radioimunoprecipitação/métodos , Ratos , Ratos Sprague-Dawley , Neuropatia Ciática/tratamento farmacológico , Neuropatia Ciática/patologia , Neuropatia Ciática/fisiopatologia , Estilbamidinas/metabolismo , Fatores de TempoRESUMO
The purpose of this study was to investigate the molecular mechanisms that are responsible for the antiinflammatory effect of usnic acid (UA). UA is one of the most common and abundant lichen metabolites. The present study examined the effects of UA on the tumor necrosis factor-alpha (TNF-alpha) and nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW264.7 macrophages and the underlying molecular mechanisms. UA decreased the TNF-alpha level in LPS-stimulated RAW264.7 macrophages in dose-dependent manner, the IC(50) value was 12.8 microM. RT-PCR analysis indicated that it inhibited TNF-alpha mRNA expression. Furthermore, it inhibited NO production in LPS-activated RAW264.7 macrophages, the IC(50) value was 4.7 microM. Western blot analysis showed that UA attenuated LPS-induced synthesis of iNOS protein and nuclear translocation of NF-kappaB p65 in the macrophages, in parallel. UA also inhibited LPS-mediated I-kappaBalpha degradation. Taken together, this suggests that UA has an antiinflammatory effect by inhibiting TNF-alpha and iNOS expression, possibly through suppression of nuclear translocation of NF-kappaB p65 and I-kappaBalpha degradation.
Assuntos
Anti-Inflamatórios/farmacologia , Benzofuranos/farmacologia , Lipopolissacarídeos/farmacologia , NF-kappa B/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Fator de Necrose Tumoral alfa/biossíntese , Análise de Variância , Animais , Linhagem Celular , Sobrevivência Celular , Regulação para Baixo , Regulação da Expressão Gênica , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Óxido Nítrico/biossíntese , RNA/genética , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Usnea/químicaRESUMO
OBJECTIVE: To study antioxidant activities of different extracts of Senecio argunensis. METHODS: The antioxidant activities of S. argunensis extracts with acetoacetate, n-Butanol and water were detected by DPPH * free radical-scavenging method and beta-carotene/linoleic acid system. RESULTS: The acetoacetate, n-Butanol and water extracts from S. argunensis eliminated DPPH * in dose-dependent manner, their EC50 values were 0.0198, 0.0219 and 0.092 mg/ml, respectively. The strength order of the antioxidant activities of the three parts in beta-carotene/linoleic acid system was acetoacetate, n-Butanol and water extracts. CONCLUSION: The extracts of the three parts of S. argunensis all have antioxidant activities. Among these extracts, extracts with acetoacetate have the highest antioxidant activity.
Assuntos
Antioxidantes/farmacologia , Asteraceae/química , Compostos de Bifenilo/metabolismo , Picratos/metabolismo , Extratos Vegetais/farmacologia , Acetoacetatos , Relação Dose-Resposta a Droga , Sequestradores de Radicais Livres , Ácido Linoleico , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Solventes , beta CarotenoRESUMO
The aim of this study was to screen for the anti-inflammatory activity of fractions and compounds from Atractylodes macrocephala Koidz. The rhizomes of Atractylodes macrocephala were treated with supercritical CO(2) fluid and the extract was separated by normal-phase and reverse-phase column chromatography. The separated samples were screened with white blood cell membrane (WBCM) chromatography (WBCM-C). The anti-inflammatory effects of these fractions and components were tested pharmacologically in vivo. The results indicated that the retention characteristics of the petrol-ether (1:1, v/v) fraction (BZC-2) of the supercritical CO(2) extract, the atractylenolide I and 14-acetoxy-12-senecioyloxytetradeca-2E,8E,10E-trien-4, 6-diyn-1-ol isolated from BZC-2 as active fractions and components were similar to that of dexamethasone in WBCM-C. Therefore, they may act on WBCM and its receptors. BZC-2 has shown anti-inflammatory effects in acute and chronic inflammation models in rats and mice. Oral administration of atractylenolide I and 14-acetoxy-12-senecioyloxytetradeca-2E,8E,10E-trien-4,6-diyn-1-ol produced significant anti-inflammatory effects in acute and chronic inflammation models in mice. The screening results with WBCM-C were correlated significantly with pharmacological effects in vivo. Atractylenolide I and 14-acetoxy-12-senecioyloxytetradeca-2E,8E,10E-trien-4,6-diyn-1-ol were the main components of Atractylodes macrocephala that were effective as anti-inflammatory agents.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Atractylodes/química , Ácido Acético/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Permeabilidade Capilar/efeitos dos fármacos , Carragenina , Membrana Celular/efeitos dos fármacos , Cromatografia , Fibra de Algodão , Dexametasona/farmacologia , Avaliação Pré-Clínica de Medicamentos , Edema/induzido quimicamente , Edema/prevenção & controle , Feminino , Granuloma/patologia , Granuloma/prevenção & controle , Leucócitos/química , Leucócitos/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Masculino , Extratos Vegetais/farmacologia , Raízes de Plantas/química , CoelhosRESUMO
In order to clarify the mechanism involved in the antiinflammatory activity of atractylenolide I and atractylenolide III from the rhizomes of Atractylodes macrocephala Koidz, their effects on tumor necrosis factor-alpha (TNF-alpha) and nitric oxide (NO) production in peritoneal macrophages were examined. Atractylenolide I and atractylenolide III decreased the TNF-alpha level in LPS-stimulated peritoneal macrophages in a dose-dependent manner, their IC(50) values were 23.1 microm and 56.3 microm, respectively. RT-PCR analysis indicated that they inhibited TNF-alpha mRNA expression. Furthermore, they inhibited NO production in LPS-activated peritoneal macrophages, the IC(50) value of atractylenolide I was 41.0 microm, and the inhibition ratio of 100 microm of atractylenolide III was 45.1% +/- 6.2%. The activity analysis of inducible nitric oxide synthase (iNOS) indicated that they could inhibit the activity of iNOS, their IC(50) values were 67.3 microm and 76.1 microm, respectively. Western blot analysis showed that atractylenolide I and atractylenolide III attenuated LPS-induced synthesis of iNOS protein in the macrophages, in parallel. These results imply that the antiinflammatory mechanism of atractylenolide I and atractylenolide III may be explained at least in part, by the inhibition of TNF-alpha and NO production. Atractylenolide I showed more potent inhibition than atractylenolide III in the production of TNF-alpha and NO in LPS-activated peritoneal macrophages. So, atractylenolide I could be a candidate for the development of new drugs to treat inflammatory diseases accompanied by the overproduction of TNF-alpha and NO.
Assuntos
Lactonas/farmacologia , Macrófagos Peritoneais/efeitos dos fármacos , Óxido Nítrico/metabolismo , Sesquiterpenos/farmacologia , Fator de Necrose Tumoral alfa/efeitos dos fármacos , Animais , Atractylodes/química , Sobrevivência Celular/efeitos dos fármacos , Lactonas/isolamento & purificação , Lipopolissacarídeos , Macrófagos Peritoneais/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Óxido Nítrico Sintase Tipo II/biossíntese , Óxido Nítrico Sintase Tipo II/efeitos dos fármacos , RNA Mensageiro/metabolismo , Rizoma/química , Sesquiterpenos/isolamento & purificação , Fator de Necrose Tumoral alfa/metabolismoRESUMO
OBJECTIVE: [corrected] To establish an HPLC method for the analysis of pharmacokinetics and tissue distribution of atractylenolide III in rats. METHODS: The biological samples were extracted with ether. The chromatographic conditions were as follows: Hypersil ODS column (150 mm x 4.6 mm, 5 microm) was used. The mobile phase was methnol/warter (67 : 33) with a flow rate of 1.0 ml/min under the column temperature of 25 degrees C, and the detection wavelength was set at 220 nm. RESULTS: The recovery of the method was 85.12% (RSD = 5.57%). The linear range was 0.2 microg/ml - 18.5 microg/ml (r = 0.9996) in rat plasma. The Lowest Limit of detection was 0.10 microg/ ml (S/N > 3). The within-day and between-day precision were from 0.98% to 6.19% and 12.95% to 15.48%, respectively. After oral administration of atractylenolide III (100 mg/kg), the concentration-time profiles of atractylenonlide III fit a two compartment model. In main effect tissues, the atractylenolide III concentration was followed as in order C(lung) > C(cerebellum) > C(heart) > C(cerebrum), and that was C(spleen) > C(liver) > C(kidney) in eliminated tissues. CONCLUSION: The method is accurate, stable and reliable, and can be used for the investigation of atractylenolide III in plasma and tissues of rats.
Assuntos
Atractylodes/química , Cromatografia Líquida de Alta Pressão/métodos , Lactonas/farmacocinética , Plantas Medicinais/química , Sesquiterpenos/farmacocinética , Animais , Área Sob a Curva , Estabilidade de Medicamentos , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacocinética , Feminino , Lactonas/isolamento & purificação , Pulmão/metabolismo , Masculino , Ratos , Ratos Sprague-Dawley , Sesquiterpenos/isolamento & purificação , Baço/metabolismo , Distribuição TecidualRESUMO
The tissue culture and plant regeneration of Bolbostemma paniculatum were studied and a large number of regenerated plantlets were obtained. The optimal compounding of medium that induced calli from stems and leaves were the MS medium supplemented with 2,4-D 2.0 mg/L, NAA 0.5 mg/L and BA 1.0 mg/L and the MS medium with 2,4-D 0.5 mg/L and NAA 2.0 mg/L, respectively. Numerous shoots could formed directly when leaf explants were cultured on the MS medium with BA 3.0 mg/L and NAA 1.0 mg/L and calli were cultured on the MS medium with BA 2.0 mg/L and IAA 1.0 mg/L. The MS medium supplemented with BA 2.0 mg/L, IAA 0.1 mg/L was optimal for shoots growth. For the root growth was 1/2 MS medium with 1.0 mg/L IBA. At pH 6.0 and 0.8% - 1.0% agar was optimal for callus and shoot formation, while pH 5.8 and 0.6% - 0.7% agar was optimal for root formation. The tube seedling can be successfully transplanted.
Assuntos
Cucurbitaceae/crescimento & desenvolvimento , Plantas Medicinais/crescimento & desenvolvimento , Regeneração , Técnicas de Cultura de Tecidos/métodos , Cucurbitaceae/fisiologia , Meios de Cultura , Reguladores de Crescimento de Plantas/farmacologia , Folhas de Planta/crescimento & desenvolvimento , Folhas de Planta/fisiologia , Caules de Planta/crescimento & desenvolvimento , Caules de Planta/fisiologia , Plântula/crescimento & desenvolvimentoRESUMO
OBJECTIVE: To study the method of callus induction and culturing of Bolbostemma paniculatum and its relationship with accumulation of tubeimoside. METHOD: Stem and leaf were selected as explants. The effects of growth substances and their combinations at different concentrations on callus formation and propagation on MS and B5 basic medium were studied. RESULT: The optimal compositions of medium that induced calli from stems and leaves were the MS medium supplemented with 2,4-D 2.0 mg x L(-1), NAA 0.5 mg x L(-1) and BA 1.0 mg x L(-1) and the MS medium supplemented with 2,4-D 0.5 mg x L(-1) and NAA 2.0 mg x L(-1), respectively. The calli cultured on the MS medium supplemented with 2,4-D 2.0 mg x L(-1), NAA 0.5 mg x L(-1) and BA 1.0 mg x L(-1) were optimal for the accumulation of tubeimoside. A uniform and stable callus line could be formed from the calli cultured repeatedly on B5 medium supplemented with 2,4-D 2.0 mg x L(-1), NAA 0.5 mg x L(-1) and BA 1.0 mg x L(-1). CONCLUSION: Using stem and leaf as explants, the method of the callus induction and culture of B. paniculatum was established and it could provide some references for the production of tubeimoside by tissue and cell culture.
Assuntos
Cucurbitaceae/crescimento & desenvolvimento , Plantas Medicinais/crescimento & desenvolvimento , Técnicas de Cultura de Tecidos/métodos , Cucurbitaceae/metabolismo , Meios de Cultura , Reguladores de Crescimento de Plantas/farmacologia , Folhas de Planta/crescimento & desenvolvimento , Folhas de Planta/metabolismo , Caules de Planta/crescimento & desenvolvimento , Caules de Planta/metabolismo , Plantas Medicinais/metabolismo , Saponinas/metabolismo , Triterpenos/metabolismoRESUMO
<p><b>OBJECTIVE</b>To study the method of callus induction and culturing of Bolbostemma paniculatum and its relationship with accumulation of tubeimoside.</p><p><b>METHOD</b>Stem and leaf were selected as explants. The effects of growth substances and their combinations at different concentrations on callus formation and propagation on MS and B5 basic medium were studied.</p><p><b>RESULT</b>The optimal compositions of medium that induced calli from stems and leaves were the MS medium supplemented with 2,4-D 2.0 mg x L(-1), NAA 0.5 mg x L(-1) and BA 1.0 mg x L(-1) and the MS medium supplemented with 2,4-D 0.5 mg x L(-1) and NAA 2.0 mg x L(-1), respectively. The calli cultured on the MS medium supplemented with 2,4-D 2.0 mg x L(-1), NAA 0.5 mg x L(-1) and BA 1.0 mg x L(-1) were optimal for the accumulation of tubeimoside. A uniform and stable callus line could be formed from the calli cultured repeatedly on B5 medium supplemented with 2,4-D 2.0 mg x L(-1), NAA 0.5 mg x L(-1) and BA 1.0 mg x L(-1).</p><p><b>CONCLUSION</b>Using stem and leaf as explants, the method of the callus induction and culture of B. paniculatum was established and it could provide some references for the production of tubeimoside by tissue and cell culture.</p>
Assuntos
Cucurbitaceae , Metabolismo , Meios de Cultura , Reguladores de Crescimento de Plantas , Farmacologia , Folhas de Planta , Metabolismo , Caules de Planta , Metabolismo , Plantas Medicinais , Metabolismo , Saponinas , Metabolismo , Técnicas de Cultura de Tecidos , Métodos , Triterpenos , MetabolismoRESUMO
OBJECTIVE: To investigate the effect of different preparation method on the quality of Shen-mai injection. METHOD: The Shen-mai injection samples were prepared using three different methods. Fingerprints of Shen-mai extracts red ginseng, and its intermediates were obtained using an HPLC analytical procedure. The contents of ginsenoside Rg1, Rc and Rb1, and the gross saponins of Shen-mai extract were quantitatively mensured with HPLC procedures. RESULT: There was significant difference in fingerprints and chemical contents of the injections prepared by the three different methods. CONCLUSION: The quality of Shen-mai injection was greatly influenced by the preparation method. HPLC fingerprinting method can be applied for the determination of the Shen-mai preparations.