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Objective: In this paper,the effect of microemulsion in Chuanqi ophthalmic microemulsion in situ gel was investigated. Method: The effect of microemulsion was confirmed by the parallel comparison between the Chuanqi microemulsion in situ gel and normal in situ gel,including study of pharmaceutical characterization and tissue distribution. Result: The average particle sizes of Chuanqi microemulsion in situ gel and normal in situ gel were (38.20±0.13) nm and (985±37) nm,respectively.Microemulsion could maintain the properties of nanocarrier in a microemulsion in situ gel composite system.The result of tissue distribution study showed that only ligustilide could be detected.This was related to the nature of these three indicator components(ligustrazine,ligustilide and astragaloside A).The common logarithm of oil and water partition coefficient of ligustilide(lgP) was 2.87,which was consistent with the range of lgP of ideal ophthalmic drugs(lgP=2.0-3.0).The ligustilide from Chuanqi microemulsion in situ gel could be detected in the cornea,vitreous body and retina,and this compound from normal in situ gel could only be detected in the cornea with low content.At the same time,microemulsion could increase the content of ligustilide in corneal tissues. Conclusion: The characteristics of microemulsion nanocarriers can increase the solubility of ligustilide,compared with normal in situ gel,it can be better distributed in the tears outside the corneal,it reaches the cornea with a higher concentration,and forms a corneal concentration gradient,and ligustilide is transported from the anterior ocular region to the posterior ocular region through the transocular barrier.
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OBJECTIVE@#To investigate the effects of salvianolic acid A (SAA) on cardiomyocyte apoptosis and mitochondrial dysfunction in response to hypoxia/reoxygenation (H/R) injury and to determine whether the Akt signaling pathway might play a role.@*METHODS@#An in vitro model of H/R injury was used to study outcomes on primary cultured neonatal rat cardiomyocytes. The cardiomyocytes were treated with 12.5, 25, 50 μg/mL SAA at the beginning of hypoxia and reoxygenation, respectively. Adenosine triphospate (ATP) and reactive oxygen species (ROS) levels were assayed. Cell apoptosis was evaluated by flow cytometry and the expression of cleaved-caspase 3, Bax and Bcl-2 were detected by Western blotting. The effects of SAA on mitochondrial dysfunction were examined by determining the mitochondrial membrane potential (△Ψm) and mitochondrial permeability transition pore (mPTP), followed by the phosphorylation of Akt (p-Akt) and GSK-3β (p-GSK-3β), which were measured by Western blotting.@*RESULTS@#SAA significantly preserved ATP levels and reduced ROS production. Importantly, SAA markedly reduced the number of apoptotic cells and decreased cleaved-caspase 3 expression levels, while also reducing the ratio of Bax/Bcl-2. Furthermore, SAA prevented the loss of △Ψm and inhibited the activation of mPTP. Western blotting experiments further revealed that SAA significantly increased the expression of p-Akt and p-GSK-3β, and the increase in p-GSK-3β expression was attenuated after inhibition of the Akt signaling pathway with LY294002.@*CONCLUSION@#SAA has a protective effect on cardiomyocyte H/R injury; the underlying mechanism may be related to the preservation of mitochondrial function and the activation of the Akt/GSK-3β signaling pathway.
Subject(s)
Animals , Rats , Adenosine Triphosphate , Animals, Newborn , Caffeic Acids , Pharmacology , Cell Hypoxia , Cells, Cultured , Glycogen Synthase Kinase 3 beta , Physiology , Lactates , Pharmacology , Mitochondria, Heart , Physiology , Mitochondrial Membrane Transport Proteins , Myocytes, Cardiac , Proto-Oncogene Proteins c-akt , Physiology , Rats, Sprague-Dawley , Reactive Oxygen Species , Metabolism , Signal Transduction , PhysiologyABSTRACT
<p><b>OBJECTIVE</b>To observe the contribution of Borneolum syntheticum to the intervention effect of Liuwei Dihuang Pill (, LDP) on experimental retinal degeneration, and initially investigate the mechanism of Borneolum syntheticum as meridian-lead-in drug.</p><p><b>METHODS</b>A total of 180 sodium iodateinduced retinital degeneration rats were randomly divided into three groups, including distilled water group, LDP group, and LDP+Borneolum syntheticum (LDP+BS) group. Twenty normal rats were fed regularly without any treatment as normal control. On day 7 and 14 after treatment, histopathological study and transferase-mediated deoxyuridine triphosphate-biotin nick end labeling (TUNEL) test were performed to evaluate the retinopathy. Claudin-5 expression at blood-retina barrier (BRB) was detected by Western blot at different time points from 0.5 to 8 h after gavage.</p><p><b>RESULTS</b>On day 7 and 14 after treatment, the retinal lesion grades were significantly different among the three groups (P<0.05). The grade in the LDP+BS group was significantly less than the LDP and distilled water groups (both P<0.05), no significant difference was observed between the LDP and distilled water groups (P>0.05). The apoptosis rates in the LDP+BS group was significantly less than the distilled water and LDP groups (both P<0.05), while there was no significant difference between LDP and distilled water groups (P>0.05). Expression of claudin-5 in LDP+BS group was significantly less than the other two groups at 0.5, 1 and 2 h after gavage (P<0.05). There was no apparent difference among the three groups at 4 and 8 h after gavage (P>0.05).</p><p><b>CONCLUSION</b>Borneolum syntheticum could strengthen the effect of LDP on experimental retinal degeneration, indicated that Borneolum syntheticum might play the role of meridian-lead-in drug in the formula. The mechanism may be due to Borneolum syntheticum could promote the physiologically openness of bloodretina barrier through transiently affecting the expression of claudin-5.</p>
Subject(s)
Animals , Apoptosis , Claudin-5 , Metabolism , Disease Models, Animal , Drugs, Chinese Herbal , Pharmacology , Therapeutic Uses , Rats, Sprague-Dawley , Retinal Degeneration , Drug Therapy , Pathology , Retinal Pigment Epithelium , Pathology , Time FactorsABSTRACT
In this review, the authors summarized the drugs in treatment of the age-related macular degeneration (AMD or ARMD), including the pathogenesis of the age-related macular degeneration at home and abroad, dosage forms used in the treatment, and the drugs research and development directions in the future. AMD disease is the third largest blinding diseases all over the world, with an incidence of 6.62%. The dosage form of the traditional medicine is mostly oral formulations, playing a role in body, while the newly dosage form is topical drug delivery formulation. Traditional Chinese medicine (TCM) has certain advantages in the treatment of AMD disease and the development of topical drug delivery preparations with newly preparation technologies would have a very bright prospect in the future.
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Age-related macular degeneration ( AMD ) is the main cause of blindness in the people older than 50 years old. In recent years, following the improvement of imaging techniques in ophthalmology, the pathogenesis of the disease, the level of diagnosis and efficacy evaluation ability greatly improved. In this paper, we reviewed and discussed the recent advancement on imaging research of age-relate d macular degeneration.
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AIM: To explore the effect of Bu Shen Yang Xue Ming Mu (BSYXMM) Formula on hydroquinone-induced oxidative stress injury in ARPE-19 cells.METHODS: The oxidative injury model of ARPE-19 cell was induced by exposure to various concentrations of hydroquinone (HQ) to determine the optimal concentration.Intestinal absorption solutions of BSYXMM Formula were prepared.Effect of intestinal absorption solutions of BSYXMM Formula on the cell viability was detected by CCK-8 assay,and the percentage of apoptotic cells was measured by TUNEL assay.The levels of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) in ARPE-19 cells were detected by means of chemical colorimetry.RESULTS: It was found that ARPE-19 cell viability significantly decreased when the concentration of HQ was higher than 90μmol/L.Compared with the model group,1% and 2% intestinal absorption solutions in the pre-treatment group could significantly alleviate HQ-induced injury (P<0.01) and 0.5% and 5% intestinal absorption solutions in the pre-treatment group could alleviate the injury in certain degree(P<0.05).While in the treatment group 1% and 2% intestinal absorption solutions could alleviate the injury to some extent (P<0.05).TUNEL results showed that the apoptosis rate decreased significantly in the pre-treatment group (P<0.01)and to some extent in the treatment group (P<0.05)compared with the model group.It was shown that both levels of SOD and GSH-Px in pre-treatment group and treatment group were markedly higher than that of model group(P<0.05),and pre-treatment group had more significant effect (P<0.01,P<0.05).CONCLUSION: BSYXMM Formula could protect against HQ-induced oxidative stress injury in ARPE-19 cells,which may be related with the increasing of antioxidant enzyme in the cells.
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?AlM: To explore the effects of the prescription of reinforcing kidney, nourishing blood, improving eyesight on the oxidative stress model of ARPE-19 cells induced by acrolein. ?METHODS:SD rats serum containing the prescription of reinforcing kidney, nourishing blood, improving eyesight and the content of distilled water in serum were prepared. The effects of the prescription and distilled water in serum at different concentration ( 2. 5%, 5%, 10%, 20% and 40%) on cell vitality was observed by cell counting kit ( CCK-8 ) assay. the logarithmic phase of ARPE-19 cells were pretreated by different concentrations (1. 25%, 2. 5%and 5%) of the prescription serum and distilled water in serum for 24h. Then it was treated with 75μmol/L acrolein for 24h. Cell vitality was observed by CCK-8 assay. The change of cell nucleus was detected by DAPl staining . ?RESULTS: 2. 5% and 5% serum had no effect on cell viability (P>0. 05), while 10%, 20%, 40% serum could inhibit cell viability (P ?CONCLUSlON: The prescription of reinforcing kidney, nourishing blood, improving eyesight has the protective effect on ARPE-19 cell damage induced by acrolein.
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Blood-eye barrier (BEB) is one of the most important structures of organism to maintain homeostasis of the eye. However, it is the major constraint for the medication of intraocular diseases. Traditional Chinese medicines have distinctive advantages for the treatment of intraocular diseases, which can be used to regulate the physiological function of human body with low toxicity. In this article, we have briefly summarized the feature of BEB, with the domestic and foreign literatures combined, and mainly reviewed current progress in the field of study on the permeability of traditional Chinese medicines and effective components in BEB and promoting methods.
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Background Mutation of the heat shock transcription factor 4 (HSF4) gene causes autosomal recessive hereditary cataract in lens opacity locus 11 (lop1 1) mouse,but the molecular mechanism of the pathogenesis has not been determined.Objective This study was to investigate the molecular mechanism of congenital cataract induced by HSF4 gene mutation in lop1 1 mouse.Methods Twenty-four lop1 1 mice and 24 wild type C57BL/6 mice were used in this study.The animals were sacrificed and the lenses were obtained on postnatal days 1,7 and 12.Regular pathological examination was carried out to evaluate the morphological changes of the lens and count the number of lens epithelial cells (LECs) in the mice.The αB-Crystallin (CRYAB) content in the lenses was detected in postnatal day 1 mice by Western blot.The expression of the fibroblast growth factor (FGF) mRNA in the lenses was assayed by quantitative PCR (q-PCR).The data were compared between the lop1 1 mice and wild type C57BL/6 mice with independent sample t test.The use and care of the experimental animals complied with the ARVO statement.Results The morphology and array of LECs were uniform and regular in the wild type C57BL/6 mice,while proliferation of LECs and disorder of lens fibers were seen in the lop11 mice on postnatal day 1.On postnatal day 7,vacuolar degeneration of the lens appeared in 7-day-old lop11 mice.The numbers of LECs were (417±19),(467±16) and (489±21) in lop11 mice on the postnatal day 1,7 and 12,respectively,and those of wild type C57BL/6 mice were (378 ± 13),(391 ±9) and (395 ±7),respectively,showing statistically significant differences between them (1 day:t=6.696,P=0.000;7 days:t=6.578,P=0.000;14 days:t=7.240,P=0.000).The expression of CRYAB in the lenses was evidently weaker in the 1-day-old lop11 mice compared with wild type C57BL/6 mice.The relative folds of expression of FGF-1,FGF-4,FGF-7 mRNA in the lenses were significantly higher in the lop11 mice than those in the wild type C57BL/6 mice (2.04±0.13 vs.1.037±0.06;2.03±0.08 vs.0.97± 0.08;4.59±0.12 vs.1.0±0.04) (FGF-1 mRNA:t=14.000,P＜0.001;FGF-4 mRNA:t=15.510,P＜0.01;FGF-7 mRNA:t =29.41,P＜0.01).Conclusions HSF4 mutation leads to the abnormal development of the lens in lop1 1 mice by arresting the expression of αB-Crystallin protein and increasing the expression of the FGF gene.
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Objective To develop a method for determination of catechins and alkaloids in brick-tea by high performance liquid chromatography(HPLC) with diode array detection(DAD),and to explore optimum extraction conditions for catechins and alkaloids components in brick-tea.Methods Catechins and alkaloids were separated and detected by HPLC.Orthogonal experiment and paired t test was carried out to compare the effect of water and alcohol as extraction solvents and to obtain optimum extraction conditions for extracting catechins and alkaloids components in brick-tea.Results Six kinds of catechins of catechin,epicatechin,gallocatechin,epigallocatechin,epicatechin gallate,epigallocatechin gallate and two kinds of alkaloids of caffeine and theobromine were separated and detected simultaneously.Calibration curves between peak areas and concentration of each component in bricktea were linear within a suitable concentration range,and coefficients of determination (R2) were between 0.9990-0.9999; spiked recoveries were from 83.78％ to 106.35％,and relative standard deviations(RSD) were between 0.50％-1.51％.The optimum extraction condition for catechins and alkaloids was 80％ ethanol,solid-liquid ratio of 1:10,temperature 80 ℃ and extraction time 30 min.Conclusion Alcohol as extraction solvents with optimal combination on HPLC,six kinds of catechins and two kinds of alkaloids are separated accurately,qualitatively,rapidly and sensitively.
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<p><b>OBJECTIVE</b>To investigate the prevalence rates of snoring disease and obstructive sleep apnea-hypopnea syndrome (OSAHS) and their risk factors among truck drivers in Guangzhou, China.</p><p><b>METHODS</b>A questionnaire survey was conducted in 374 truck drivers who were selected from 5 logistics companies in Guangzhou by cluster sampling. Those who had potential snoring disease or OSAHS underwent polysomnographic monitoring at night. The obtained data were analyzed to calculate the prevalence rates of snoring disease and OSAHS and determine the risk factors for OSAHS.</p><p><b>RESULTS</b>A total of 335 subjects completely questionnaires, with a response rate of 90%. Among the 335 subjects, 125 (37.3%) had habitual snoring, and 42 (12.5%) had OSAHS according to the diagnostic criterion (apnea-hypopnea index ≥ 5 times/h). The multiple stepwise regression analysis showed that the risk factors for OSAHS were age, alcohol use, family history of snoring, body mass index, and upper airway abnormality. Of the subjects with grade ≥ 2 snoring and OSAHS, 65.4% often felt sleepy when driving during daytime, and 42% had suffered or nearly suffered traffic accidents due to sleepiness when driving. Moreover, 95.5% (320) of the 335 truck drivers did not consider snoring a disease, and 98% did not think traffic accident might be related to snoring.</p><p><b>CONCLUSION</b>The prevalence rates of snoring disease and OSAHS among truck drivers are 37.3% and 12.5%, respectively. Therefore, prevention measures should be established according to the epidemiological characteristics to help the truck drivers realize the hazards of snoring disease and OSAHS, thus minimizing the prevalence and hazards of the diseases.</p>
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Adult , Female , Humans , Male , Middle Aged , Young Adult , Automobile Driving , China , Epidemiology , Prevalence , Risk Factors , Sleep Apnea, Obstructive , Epidemiology , Snoring , Epidemiology , Surveys and QuestionnairesABSTRACT
<p><b>OBJECTIVE</b>To investigate the effect of uvulopalatopharyngoplasty (UPPP) to obstructive sleep apnea hypopnea syndrome (OSAHS) in patients with resistant hypertension (RH).</p><p><b>METHODS</b>UPPP and modified UPPP were performed on 36 moderate and severe OSAHS patients, who also suffered from RH [who taking more than three kinds of antihypertensive drugs (including diuretics) and still not able to control blood pressure at 140/90 mm Hg (1 mm Hg = 0.133 kPa)]. Polysomnography monitoring, ambulatory blood pressure monitoring, apnea hypopnea index (AHI), lowest saturation of blood oxygen (SaO2) and the changes of antihypertensive medication dosage were performed to the patients before and 6 months after the surgery.</p><p><b>RESULTS</b>Six months after surgery,the total efficiency was 61.1% (22/36). The AHI median [25 quartile; 75 quartile] from 37.5 [26.0; 48.3]/h to 9.5 [9.0; 21.3]/h, the lowest the SaO2 average (x(-) ± s, the same below) increased from 0.655 ± 0.114 to 0.860 ± 0.037, the differences were statistically significant (P value < 0.05). 24 h systolic blood pressure, daytime systolic blood pressure, night contraction, diastolic and mean arterial pressure decreased from (160.8 ± 6.8), (170.5 ± 2.5), (163.6 ± 10.5), (100.8 ± 5.6) and (96.8 ± 7.5) mm Hg to (142.5 ± 7.3), (150.8 ± 7.6), (140.1 ± 6.4), (81.8 ± 7.4) and (93.7 ± 2.4) mm Hg, the differences were statistically significant (P < 0.05). The degrees of AHI descent and the average SaO2 improvement were concerned with the degree of systolic blood pressure, diastolic blood pressure decent (r > 0.80 and r(2) > 0.50). The average numbers of antihypertensive drugs decreased form (3.6 ± 0.5) to (2.9 ± 0.5) compared preoperatively and postoperatively, the difference was statistically significant (t = 5.537, P < 0.01). The use of antihypertensive medication reduced in 23 cases (23/36, 63.8%) compared preoperatively and postoperatively.</p><p><b>CONCLUSIONS</b>The blood pressure of the patients with OSAHS and RH dropped significantly after UPPP surgery. Recent follow-up shows that the varieties of antihypertensive drugs taken in these patients are reduced significantly after operation.</p>
Subject(s)
Adult , Female , Humans , Male , Middle Aged , Blood Pressure Monitoring, Ambulatory , Hypertension , General Surgery , Palate , General Surgery , Pharynx , General Surgery , Sleep Apnea, Obstructive , General Surgery , Uvula , General SurgeryABSTRACT
<p><b>OBJECTIVE</b>To study the protection of Zibu Piyin Recipe (ZBPYR) on the insulin signal pathway in the hippocampus of Pi-yin deficiency diabetic encephalopathy rats and to explore its possible mechanisms.</p><p><b>METHODS</b>The type 2 diabetic model was established using high fat diet and intraperitoneal injection of small dose streptozotocin (STZ). The Pi-yin deficiency model was established referring to classic compound factors. The learning and memory capabilities were tested in rats by the behavioral changes. The protein expressions of hippocampal IRE1alpha, JNK, and IRS-1 were detected using Western blot.</p><p><b>RESULTS</b>There was statistical difference in the learning and memory capabilities of Pi-yin deficiency rats when compared with the blank control group (P<0.05). The learning and memory capabilities could be improved by ZBPYR. The protein expressions of hippocampal phospho-IRS-1, phospho-JNK, and total IRE1alpha were enhanced (P<0.05). But they were weakened after treatment of ZBPYR.</p><p><b>CONCLUSIONS</b>ZBPYR could significantly improve the learning and memory capabilities of Pi-yin deficiency diabetic rats. Its functions might be correlated with improving the endoplasmic reticulum stress to regulate the insulin signaling pathway.</p>