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Aim To investigate the effeets of Dracocephalum Moldavica total flavonoids (TFDM) on the foaming lipoprotein (ox-LDL), and to further elucidate the mechanism of anti-atherosclerosis (AS) of TFDM. Methods RAW264. 7 maerophages were cultured in vitro and induced to become foam cells by ox-LDL stimulation, and inflammation of mouse monocyte macrophage leukemia cells (RAW264. 7) induced by oxi-dized low density TFDM(25, 50, 100 mg • L"
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To investigate the effect and mechanism of Dracocephalum moldovica total flavones (TFDM) on the formation of atherosclerosis ApoE-/- mice induced by high fat diet. A total of 40 SPF 8-week-old male ApoE-/- mice were fed with high fat diet and randomly divided into 5 groups. TFDM high, medium, low-dose group were given 21, 42, 84 mg•kg⁻¹•d⁻¹ by gavage; Simvastatin group was fed with simvastatin 3.5 mg•kg⁻¹•d⁻¹; and model group was given the same dose of normal saline. The other eight male C57BL/6J mice of the same genetic background and age were set up as control group and fed with common diet. All of the groups were intragastrically intervened for 12 weeks. The aortic pathologic changes were observed with HE; qRT-PCR was adopted to detect TGF-β1, Smad2, Smad3, MMP-2 and MMP-9 gene levels in tissues. Compared with model group, HE staining in TFDM group showed obvious relief of aortic atherosclerotic tissue injury; each TFDM group showed inhibition in mRNA expressions of TGF-β1, Smad2, Smad3, MMP-2 and MMP-9. This suggests that TFDM can inhibit atherosclerosis formation, which may be related to the intervention of TGF-β1/Smads signal transduction.
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<p><b>BACKGROUND</b>Pomegranate (punica granatum) belongs to the family Punicaceae, and its peel has been used as a traditional Chinese medicine because of its efficacy in restraining intestine, promoting hemostasis, and killing parasites. Pomegranate peel has been reported to possess wound-healing properties which are mainly attributed to its polyphenol extracts. The purpose of this study was to investigate the effect of pomegranate peel polyphenols (PPP) gel on cutaneous wound healing in diabetic rats.</p><p><b>METHODS</b>Alloxan-induced diabetic rats were given incisional wounds on each side of the mid-back and then treated daily with PPP gel (polyphenol mass fraction = 30%) post-wounding. Rats were sacrificed on days 4, 7, 14, and 21 post-wounding to assess the rates of wound closure, histological characteristics; and to detect the contents of hydroxyproline, production of nitric oxide (NO), and activities of NO synthase (NOS), as well as the expressions of transforming growth factor-β1 (TGF-β1), vascular endothelial growth factor (VEGF), and epidermal growth factor (EGF) in wound tissue.</p><p><b>RESULTS</b>Wound closure was significantly shortened when PPP gel was applied to the wounds of diabetic rats. Histological examination showed the ability of PPP gel to increase fibroblast infiltration, collagen regeneration, vascularization, and epithelialization in the wound area of diabetic rats. In addition, PPP gel-treated diabetic rats showed increased contents of hydroxyproline, production of NO, and activities of NOS and increased expressions of TGF-β1, VEGF, and EGF in wound tissues.</p><p><b>CONCLUSION</b>PPP gel may be a beneficial method for treating wound disorders associated with diabetes.</p>
Subject(s)
Animals , Female , Male , Rats , Alloxan , Diabetes Mellitus, Experimental , Pathology , Gels , Hydroxyproline , Nitric Oxide , Polyphenols , Pharmacology , Lythraceae , Rats, Wistar , Transforming Growth Factor beta1 , Physiology , Vascular Endothelial Growth Factor A , Physiology , Wound HealingABSTRACT
<p><b>OBJECTIVE</b>To study the intestinal absorption mechanism of tilianin in rats.</p><p><b>METHOD</b>The single-pass perfusion model was established in rats. The concentrations of tilianin with in situ intestinal perfusion were determined by HPLC. The impact factors, such as verapamil, reserpine, phloridzin and rifampicin, on Ka and Papp of tilianin in rat jejunum were investigated.</p><p><b>RESULT</b>Compared with the control group, Ka and Papp in rat jejunum were significantly higher after being added with verapamil and reserpine (P < 0.05). Papp of tilianin in rat jejunum was significantly lower after being added with phloridzin (P < 0.05). Compared with the control group, both Ka and Papp of tilianin in rat jejunum were not significantly higher after being added with rifampicin.</p><p><b>CONCLUSION</b>Tilianin is the substrate of P-gp, BCRP and SGLT1. The effluent effect of P-gp and BCRP is the main mechanism of tilianin in intestinal absorption, indicating that tilianin can realize intestinal absorption and transport by relying on SGLT1. Tilianin is not the substrate of bile salt transporter protein.</p>
Subject(s)
Animals , Female , Humans , Male , Rats , Caco-2 Cells , Drugs, Chinese Herbal , Pharmacokinetics , Flavonoids , Pharmacokinetics , Glycosides , Pharmacokinetics , Intestinal Absorption , Lamiaceae , Chemistry , Models, Biological , Perfusion , Rats, WistarABSTRACT
<p><b>OBJECTIVE</b>To investigate the change of circadian blood pressure variability (BPV) and plasma neopterin before and after surgery (uvulopalatopharyngoplasty) for patients with obstructive sleep apnea syndrome (OSAS).</p><p><b>METHODS</b>A total of 382 OSAS patients underwent uvulopalatopharyngoplasty were divided into three groups based on polysomnography (PSG) results: mild OSAS (n = 206), moderate OSAS (n = 108) and severe OSAS (n = 68). Plasma neopterin, 24-hour ambulatory blood pressure monitoring (ABPM), PSG were measured before and 3 months after surgery.</p><p><b>RESULTS</b>Plasma neopterin increased in proportion to severity of OSAS before surgery (15.08 nmol/L, 27.68 nmol/L and 37.32 nmol/L in patients with mild to severe OSAS) which were significantly reduced post surgery (9.92 ng/ml, 15.07 ng/ml and 18.54 ng/ml, all P < 0.05 vs. pre-surgery). The incidence of non-dipper curve in three OSAS groups were 50.2%, 72.7% and 86.5%, respectively before surgery and the values decreased to 34.8%, 48.2% and 49.2% after surgery (all P < 0.05 vs. pre-surgery). Relevance analysis indicates that D-value of nocturnal and diurnal blood pressure was negatively correlated with plasma neopterin.</p><p><b>CONCLUSION</b>Our findings indicated that plasma neopterin and the incidence of non-dipper could reliably reflect OSAS severity and could thus be used to evaluate the surgery efficacy. Plasma neopterin might be an important player in the pathophysiology of OSAS via modulating blood pressure variability.</p>
Subject(s)
Adult , Female , Humans , Male , Middle Aged , Blood Pressure , Blood Pressure Monitoring, Ambulatory , Circadian Rhythm , Neopterin , Blood , Otorhinolaryngologic Surgical Procedures , Sleep Apnea, Obstructive , Blood , General SurgeryABSTRACT
<p><b>OBJECTIVE</b>To explore the changes in plasma angiotensin II (Ang II) and circadian rhythm of blood pressure among hypertensive patients with sleep apnea syndrome (SAS) before and after continuous positive airway pressure (CPAP) or surgical treatment.</p><p><b>METHODS</b>A total of 180 essential hypertension patients were enrolled in our study. The determination of plasma Ang II concentration, ambulatory blood pressure (ABP), and polysomnography (PSG) monitoring were performed before and 3 months after CPAP or surgical treatment.</p><p><b>RESULTS</b>Patients were classified into three groups by their apnea-hypopnea index (AHI): essential hypertension group (EH group, n = 72; AHI< 5), essential hypertension with mild SAS group (EH+mild SAS group, n = 60, 5 ≤ AHI < 20), and essential hypertension with moderate and severe SAS group (EH + moderate-severe SAS group, n = 48, AHI ≥ 20). The concentrations of plasma Ang2 in the above three groups were 13.42 ± 3.27, 16.17 ± 3.82, and 18.73 ± 4.05 ng/mL respectively before treatment, and Ang2 concentration in EH patients combined with SAS was significantly higher than that in EH group (all P < 0.05). After treatment the values in the latter two groups significantly decreased to 14.67 ± 2.56 and 15.03 ± 3.41 ng/mL respectively (P < 0.05). The incidence of non-dipper blood pressure curve in EH patients was 31.9%, and those in hypertensive patients with mild SAS and moderate-severe SAS were 51.7% and 58.3%, respectively before treatment. The incidence of non-dipper blood pressure curve in the EH patients with mild SAS was significantly higher than that of patients with EH alone (P < 0.05). After CPAP treatment or surgery, the incidence of non-dipper blood pressure curve in the two SAS groups was significantly decreased to 38.3% and 39.6%, respectively (P < 0.05).</p><p><b>CONCLUSIONS</b>Ang II might play a role in blood pressure variability in patients with obstructive SAS. CPAP or surgical treatment can improve blood pressure disorder and decrease plasma Ang II level in patients with obstructive SAS.</p>
Subject(s)
Adult , Aged , Female , Humans , Male , Middle Aged , Angiotensin II , Blood , Blood Pressure , Physiology , Blood Pressure Monitoring, Ambulatory , Circadian Rhythm , Physiology , Continuous Positive Airway Pressure , Hypertension , Pharynx , General Surgery , Polysomnography , Sleep Apnea Syndromes , Blood , General Surgery , TherapeuticsABSTRACT
<p><b>OBJECTIVE</b>To establish the activation of NF-kappaB in middle ear cholesteatoma, discuss the relationship of NF-kappaB and the gene expression of IL-6 and explore the pathogenesis of middle ear cholesteatoma.</p><p><b>METHODS</b>Ten cases of cholesteatoma and 6 cases of normal external meatal skin were obtained from middle ear surgery. The NF-kappaB DNA binding activity and the mRNA level of IL-6 in these two kinds of tissues were detected by electrophoretic motility shift assay (EMSA) and Reverse transcription polymerase chain reaction (RT-PCR) respectively. The relationship of NF-kappaB DNA binding activity and the mRNA level of IL-6 were analyzed.</p><p><b>RESULTS</b>The NF-kappaB DNA binding activities of cholesteatoma [(15.9 +/- 8.2)%] were higher than those in normal skin [(1.36 +/- 0.94)%, t = 3.502, P < 0.05]. The expression of IL-6 mRNA was increased significantly in patients with cholesteatoma, as compared with that in the control specimens (t = 2.166, P < 0.05) and had a significant positive correlation with NF-kappaB DNA binding activity (r = 0.752, P < 0.05).</p><p><b>CONCLUSIONS</b>The IL-6 mRNA expression in cholesteatoma is closely related with the activity of NF-kappaB. It is tempting to speculate that NF-kappaB play a key role in the activation of cytokine in cholesteatoma.</p>
Subject(s)
Humans , Cholesteatoma, Middle Ear , Genetics , Metabolism , Gene Expression Regulation , Interleukin-6 , Genetics , Metabolism , NF-kappa B , Metabolism , RNA, Messenger , GeneticsABSTRACT
<p><b>OBJECTIVE</b>To optimize formulation of tanshinone II(A)-loaded PLGA nanoparticles and compare the difference of two methods in preparation and quality of nanoparticles.</p><p><b>METHOD</b>The two methods were nanoprecipitation method and emulsion-evaporation method. Single factor experiments and central composite design and response surface method were used to optimize the formulation of nanoparticles. The nanoparticles were characterized at size, morphology, entrapment efficiency, drug loading, drug recovery rate, crystallinity and drug release in vitro.</p><p><b>RESULT</b>The mean diameters were 225 nm and 183 nm, the entrapment efficiency were 95.49% and 87.99%, the drug loading were 2.03% and 0.16%, and the drug recovery rates were 38.42% and 17.59% respectively for nanoprecipitation method and emulsion-evaporation method.</p><p><b>CONCLUSION</b>Nanoprecipitation method was better than emulsion-evaporation method for preparation of tanshinone II(A)-loaded PLGA nanoparticles.</p>
Subject(s)
Chemical Precipitation , Crystallization , Abietanes , Emulsions , Lactic Acid , Chemistry , Nanoparticles , Chemistry , Particle Size , Phenanthrenes , Chemistry , Plant Roots , Chemistry , Plants, Medicinal , Chemistry , Polyglycolic Acid , Chemistry , Polymers , Chemistry , Quality Control , Salvia miltiorrhiza , Chemistry , Technology, Pharmaceutical , Methods , VolatilizationABSTRACT
<p><b>OBJECTIVE</b>To study the release feature of Res-nanoliposomes in vitro and clarify the difference in absorption of Res-nanoliposomes from varied intestinal segments and the absorptive mechanism in vivo.</p><p><b>METHOD</b>Dialytic method was used to determine resveratrol release rate of Res-nanoliposomes in vitro. An in situ rat perfusion method was used to investigate the intestinal absorption of Res-nanoliposomes.</p><p><b>RESULT</b>Resveratrol release from nanoliposomes in vitro fitted the log-normal distribution equation and had a property of sustained release. Compared with other intestinal segments, significantly high percentage of Res-nanoliposomes was absorbed in ileum (P < 0.001). The absorption rate constants (ka) of Res-nanoliposomes in intestine were not significantly different.</p><p><b>CONCLUSION</b>Res-nanoliposomes could sustain to release drug in vitro. The absorption was a first-order process with the passive diffusion mechanism. The Res-nanoliposomes could promote the absorption of Res in rat small intestine.</p>