1. Preparation and quality evaluation of tea tree oil microemulsion gel
Chinese Traditional and Herbal Drugs 2015;46(13):1892-1900
Objective: To study the prescription and preparation technology of tea tree oil (TTO) microemulsion gel. The quality and the stability were evaluated. Methods: The prescription and preparation technology were selected and optimized through the compatibility test and the pseudo-ternary phase diagram. TTO microemulsion gel was prepared by adding gelatin. The appearance, pH value, viscosity, moisture rate, and the drug concentration were evaluated. Results: The prescription composition of TTO microemulsion gel was TTO (0.6%), Cremophor RH-40 (1.2%), PEG 400 (0.2%), carbopol-980 (0.2%), glycerol (2%), with distilled water adding to 50 g. The optimum formulation exhibited clear and transparent, uniform exquisite, moderate viscosity, and well spreadable, with the particle diameter of (38.38 ± 2.30) nm, zeta potential of (-56.00 ± 5.82) mV, pH value of 5.52 ± 0.01, viscosity of (48 834 ± 5) Pa·s, moisture rate of (96.74 ± 0.52)%, and the drug-loaded of (5.79 ± 0.03) mg/g. The result of heat and cold resistance test showed that the preparation was needed to be stored at low-temperature. Conclusion: The preparation of TTO microemulsion gel is simple, corresponding to the main index of gelata for topical drug delivery preparation and offering the basis for further research and development.
2. Preparation and in vitro dissolution evaluation of tanshinone IIA for oral self-microemulsion
Chinese Traditional and Herbal Drugs 2014;45(22):3256-3265
Objective: To study the prescription and preparation technology of tanshinone IIA for oral self-microemulsifying drug delivery system. The quality, stability, and in vitro dissolution were evaluated. Methods: The prescription and preparation technology were selected and optimized through the solubility experiment, orthogonal design, and pseudo-ternary phase diagram method, using the self-emulsifying time, appearance, particle diameter, and stability as selection indexes. The droplet morphous, particle size, drug content, stability, and in vitro dissolution were evaluated after self-microemulsification. Results: The prescription composition of tanshinone IIA self microemulsion was aethylis oleas (50%), polysorbate 80 (40%), and PEG 400 (10%), with oil phase-aqueous phase of 1:50, drug-loaded of 3.0 mg/g, and self-emulsifying time of 1 min. The acquired tanshinone IIA self-microemulsion exhibitted uniform and transparent, with the particle diameter of (51.39 ± 1.50) nm, polydispersity index of 0.211 ± 0.022, Zeta potential of (-11.35 ± 1.19) mV. The results of in vitro dissolution indicated that the accumulative dissolution in 0.1 mol/L HCl solution was able to reach 96% after 30 min. The stability result showed that tanshinone IIA self-microemulsion was affected by high temperature and illumination, indicating having to be stored at 4℃ and protected from light. Conclusion: The preparation of tanshinone IIA self-microemulsion is simple, increasing the solubility in water, making it better absorption in the stomach and intestine, corresponding to the main index of oral drug delivery system and offering the basis for further development and research about tanshinone IIA.
3. Preparation of tea tree oil gel and its pharmacodynamic study and irritation evaluation
Chinese Traditional and Herbal Drugs 2018;49(21):5082-5092
Objective To study the prescription and preparation technology of tea tree oil gel, and evaluate its anti-inflammatory efficacy, antibacterial effect and the irritation. Methods The tea tree oil gel was prepared using the carbomer-940 as gel matrix, Cremophor RH-40 and 1,2-propylene glycol as solvents. The appearance characters, pH value, viscosity, moisture retention, drug content, and the stability were observed. The anti-inflammatory efficacy, the antibacterial effect and the irritation of tea tree oil gel were evaluated. Results The prescription of tea tree oil gel was selected as following tea tree oil (1.0%), Cremophor RH-40 (5.0%), 1,2-propylene glycol (5.0%), Carbomer-940 (0.6%), glycerol (8.0%), with distilled water 100 g, adjusting pH to 5.0 by triethanolamine. The gel exhibited transparent, well uniformity, appropriate viscosity and fine coating expansion performance, with pH value of 5.52 ± 0.03, viscosity at (48 782 ± 25) mPa•s, the moisture retaining rate of (93.32 ± 0.38)% for 24 h test, containing tea tree oil of (9.55 ± 0.10) mg/g. The inhibition rate of tea tree oil gel on the mouse auricle swelling was 46.15%, which was significantly different as compared to the negative control group (P < 0.01). The diameters of inhibition zone of the gel against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa respectively was (15.50 ± 0.96), (15.25 ± 2.36), and (15.75 ± 1.91) mm. The half hemolysis rate (LC50) and the hemoglobin degeneration index (DI) respectively were 456 157 mg/L and 157.98%. The tea tree oil gel had no eye irritation in rabbits based on the value of LC50/DI 2 887.44. Fourteen consecutive’days administration indicated that the tea tree oil gel had no skin irritation in rabbits. The illumination score of irritative reaction to the rabbit skin was 0.125 after a single administration, while that was 0.036 after successive administration experiment. The results of high speed centrifugalization cold- resistance and heat-resistance tests showed that the preparation exhibited good stability, which needed to be kept tightly in a cool place and protected from light. Conclusion The formulation design was reasonable, while the preparation technology was simple, corresponding to the main index of the gel for topical application, with good anti-inflammatory efficacy, antibacterial effect and safety, which offered the basis for further research and development of tea tree oil.
4.Study on the mechanism of action of total flavonoids of Litsea coreana for reducing blood glucose level in rat with type 2 diabetes mellitus.
Yu-Xiu SUN ; Yun-Xia LU ; Ling-Yun WANG
Chinese Journal of Integrated Traditional and Western Medicine 2010;30(6):617-621
OBJECTIVETo explore the possible mechanism of total flavonoids of Litsea coreana (TFLC) on reducing blood glucose level in rat with type 2 diabetes mellitus (T2DM).
METHODSMale SD rats of T2DM allocated in two groups were treated with 400 mg/kg TFLC or metformin respectively via gastrogavage for 6 weeks. Blood routine biochemical indices in rats were measured; pathology of rats' liver was examined with HE stain under transmission electron microscopy; levels of malondialdehyde (MDA) and superoxide dismutase (SOD) in liver homogenate were determined, and the expression of protein tyrosine phosphatase 1B (PTP1B) in liver was detected using RT-PCR at the terminal of the experiment.
RESULTSBiochemical measuring showed that the glucose tolerance of rats after treatment was markedly improved in both groups. Meantime, levels of fast blood glucose (FBG), glycohemoglobin (HbA1c), fast blood insulin (FINS), free fatty acid (FFA), total cholesterol (TC), triglyceride (TG) and low density lipoprotein-cholesterol (LDL-C), as well as MDA level in liver were decreased, while levels of high density lipoprotein-cholesterol (HDL-C) in blood and SOD in liver were significantly increased in both groups after treatment, showing insignificant difference between two treatment groups. Light microscopic examination showed markedly fatty degeneration of liver, and electron microscopic examination found mitochondria swelling and endoplasmic reticulum breakage in liver of T2DM rats, but these changes were ameliorated to some extent after treatment. The elevated PTP1B expression in liver of T2DM rats was decreased in the TFLC treated group, but unchanged in the metformin treated group.
CONCLUSIONTFLC can significantly decrease the blood levels of glucose and lipid and ameliorate oxidation stress in liver; its mechanism of action in improving insulin resistance might be related with its suppression on PTP1B expression in rat's liver to enhance the insulin signaling pathway.
Animals ; Blood Glucose ; metabolism ; Diabetes Mellitus, Experimental ; drug therapy ; Diabetes Mellitus, Type 2 ; drug therapy ; Flavonoids ; isolation & purification ; therapeutic use ; Hypoglycemic Agents ; therapeutic use ; Litsea ; chemistry ; Liver ; metabolism ; Male ; Oxidative Stress ; drug effects ; Protein Tyrosine Phosphatase, Non-Receptor Type 1 ; metabolism ; Rats ; Rats, Sprague-Dawley
5.Evaluation of 99Tcm-DTPA nuclear dynamic inaging in renal occupied disease
Guo-xiu LU ; Cai-xia NG ZHA ; Wei-na XU ; Shu-peng YU ; Jun XIN
Cancer Research and Clinic 2012;24(1):41-45
Objective To evaluate 99tcm-DTPA nuclear dynamic imaging in distinguishing the renal occupied disease.Methods A total of 164 in-patients with renal occupied disease who underwent surgery were included.According to the pathological diagnosis,119 patients had malignant tumors,and 45 patients had benign diseases.All patients’ imaging was retrospectively analyzed.Application of 99Tcm-DTPA nuclear dynamic imaging in renal occupied disease was compared with ultrasonography (US),computed tomography (CT),magnetic resonance imaging (MRI),intravenous pyelogram (IVP),and positron emission tomography (PET)-CT.Results The accuracy rates of different imaging methods in distinguishing between renal malignant and benign disease were 99Tcm-DTPA (84 %,45 %),US (72 %,64 %),CT ( 91%,92 %),MRI (50 %,67 %),IVP (50 %, 17 %), respectively.The diagnostic accuracy rate of PET-CT for malignant tumors was 67 %.The accuracy rates of 99Tcm-DTPA in distinguishing different phases of renal cell carcinoma were statistically significant (x 2 =83.4, P < 0.01), while the accuracy rates in distinguishing renal cyst from renal angiomyolipoma were not statistically different.With the greater diameter, the diagnostic accordance rate is higher (x 2 =16.05,P < 0.05).Conclusion 99Tcm-DTPA could be used not only to evaluate the renal function quantificationally,but also be helpful to distinguish renal malignant tumor from benign disease.
6.Free fatty acids regulate expression of adiponectin receptor gene in adipocytes
Yu WEN ; Hong-Wei WANG ; Jing WU ; Hui-Ling LU ; Xiu-Fen HU ; Zhi XIA ;
Chinese Journal of Endocrinology and Metabolism 2001;0(05):-
3T3-LI preadipocytes were induced to differentiate and 3T3-L1 adipocyte or preadipocytes were incubated with oleate or palmitate overnight.RT-PCR was used to measure adiponectin receptor(AdipoR)1 and AdipoR2 mRNA levels.The results showed that the AdipoRl and AdipoR2 expressions were differentiation- dependent.Oleate only suppressed AdipoR mRNA expression in preadipocyte but not in adipocyte.However,high concentration of palmitate reduced AdipoR mRNA expression in both 3T3-LI preadipocyte and adipocyte.
7.Application of high-resolution ultrasound and CDFI-guided minimally invasive operation for breast lesions
De-Zhan WEI ; Xiu-Ying LU ; Da-Jiang ZHU ; Yi-Ye DENG ; Hong-Xia LI ; Xiu-Zhen DENG ; Zhan-Kui LU ; Chao CHENG ;
Chinese Journal of Primary Medicine and Pharmacy 2006;0(07):-
Objective To evaluate the application and the good qualities of high-resolution ultrasound and CDFI-guided mammotome minimally invasive biopsy device in the diagnosis and treatment of breast lesions.Methods The common clinical operations and the lesions which were guided mammotome minimally invasive biopsy device by high-resolution ultrasound and CDFI were contrasted.The effects of treatment were evaluated.Results 307 le- sions of 102 patients were removed by this method,and the operational process was successful.Patients' skin lacera- tions were tiny.Only one lesion was clinically diagnosed as mild blood clot under skin,but without other complica- tions.Conclusion Contrasted with the common clinily operations.the high-resolution ultrasound and CDFI-guided mammotome minimally invasive biopsy device in the diagnosis and treatment of breast lesion is effective,and the scar is tiny.It releases patients' pain.
8.Isolation, identification and full-length genome sequence analysis of encephalomyocarditis virus from local aardvarks.
Hong-Tao CHANG ; Hui-Min LIU ; Xiu-Yuan HE ; Jun ZHAO ; Lu CHEN ; Xin-Wei WANG ; Xia YANG ; Hui-Xia YAO ; Chuan-Qing WANG
Chinese Journal of Virology 2014;30(4):375-381
Encephalomyocarditis virus (EMCV) is a natural epidemic zoonotic pathogen. However, no reports have been published regarding the isolation, identification and full-length genome of EMCV from a local aardvark population. In present study, an EMCV isolate HNXX13 was isolated from aardvarks named Huainan-pig in Henan Province. The systematic identification, full-length genome sequencing and molecular characteristic analysis of the isolate HNXX13 were conducted. The result showed that the isolate was spherical with a diameter of 24-30 nm, neither heat- nor acid-resistant, sensitive to trypsin, insensitive to chloroform, not protected by bivalent cationic, and the specific fluorescence was observed in the cytoplasm of BHK-21 cells infected with the isolate by using indirect fluorescence assay. The full-length genome of EMCV HNXX13 generated a 7 725bp sequence (GenBank: F771002), with 81.0%-99.9% nucleotide identity to reference strains from different animals, and 99.5% with a Chinese reference strain isolated earlier from a commercial pig herd. The phylogenetic tree based on the full-length genome and ORF sequences identified that all EMCV strains were divided into three groups G1, G2 and G3, and strain HNXX13 belonging to the G1 group with other Chinese reference strains. The result also identified that this EMCV infection could cause severe clinical signs in a local aardvark population, and enriches the molecular epidemiological data of EMCV in China. Regional differences exist in EMCV genome and transmission is limited within a certain area. However, the cross-infection and transmission of EMCV between aardvark and mice appears most likely. Mutations have occurred in some amino acids of EMCV strain HNXX13 during the transmission in local aardvark herd and these mutations might make the virus easier to infect the aardvark.
Animals
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Animals, Wild
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virology
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Cardiovirus Infections
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veterinary
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virology
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China
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Encephalomyocarditis virus
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classification
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genetics
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isolation & purification
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Genome, Viral
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Mice
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Molecular Sequence Data
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Phylogeny
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Xenarthra
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virology
9.NQO1 dependent non-canonical necroptosis mediated by ROS and RIP1/RIP3 in parallel in glioma cancer cells
Jie YU ; Xia-Xia WU ; Chang-Xi WANG ; Hong-Wei GAO ; Wen SUN ; Jin-Jian LU ; Xiu-Ping CHEN
Chinese Journal of Pharmacology and Toxicology 2018;32(4):326-327
OBJECTIVE Glioblastomas(GBM)are the most malignant brain tumors in humans and have a very poor prognosis. New therapeutics are urgently needed. Here, we reported 2-methoxy-6-acetyl-7-methyljuglone (MAM)-induced cell death in U87 and U251 glioma cancer cells. METHODS Cells were cultured and treated with MAM, the cell viability was determined by MTT assay and LDH assay. Intracellular reactive oxygen species (ROS) generation was observed by DCF fluorescence. The protein expression was determined by Western blotting. RESULTS MAM induced glioma cancer cell death without caspase activation. The cell death induced by MAM was attenuated by the pharmacological or genetic blockage of necroptosis signaling,including RIP1 inhibitor necrostatin-1s (Nec-1s)and siRNA-mediated gene silencing of RIP1 and RIP3,but was unaffected by caspase inhibitor z-vad-fmk or necrosis inhibitor 2-(1H-Indol-3-yl)-3-pentylamino-maleimide (IM54). MAM treated U87 and U251 glioma cancer cells induced RIP1/RIP3 complex formation, ROS level increased, ATP concentration decreased and loss of plasma membrane integrity, further confirmed this process was necroptosis.The essential role of ROS was confirmed by the protective effect of ROS scavenger NAC. Interestingly, MAM induced necroptosis both triggered by RIP1/RIP3 complex and ROS generation. Moreover, MAM induced necroptosis through cytosolic calcium (Ca2 +) accumulation and sustained c-Jun N-terminal kinase (JNK) activation. Both calcium chelator BAPTA-AM and JNK inhibitor SP600125 could attenuate cell death. Further, we found there exists a feedback loop between RIP1 and JNK activation.Finally,MAM induced necroptosis was inhibited by dicoumarol(a NQO1 inhibitor). Dicoumarol exposed glioma cancer cells were resistant to RIP1/RIP3 complex formation and ROS generation. MAM induced necroptosis was independent of MLKL. CONCLUSION MAM induced non-canonical necroptosis through the NQO1-dependent ROS and RIP1/RIP3 pathway.This study also provided new insights into the molecular regulation of necroptosis in human glioma cancer cells and a promising approach for GBM treatment.
10.Percutaneous balloon pulmonary valvuloplasty for critical pulmonary stenosis in infants under 6 months of age and short and medium term follow-up.
Fang LUO ; Wei-Ze XU ; Cheng-Sen XIA ; Li-Ping SHI ; Xiu-Jing WU ; Xiao-Lu MA ; Zheng CHEN
Chinese Journal of Pediatrics 2011;49(1):17-20
OBJECTIVETo evaluate the effect and results of short and medium periods of follow-up of percutaneous balloon pulmonary valvuloplasty for critical pulmonary stenosis of neonates and infants under 6 months of age.
METHODSBetween January 2002 and December 2008, 34 consecutive patients aged from 13 to 175 days with critical pulmonary valvular stenosis underwent percutaneous balloon valvuloplasty. Patients records, catheterization data, angiograms and echocardiograms were reviewed. Patients were followed up for 6 months to 4 years (mean 25.5 months) by means of clinical examination and Doppler echocardiography.
RESULTSThe pulmonary valvuloplasty was accomplished in 32 (94%) of 34 attempts. Immediately after dilation, right ventricular systolic pressure (RVSP) decreased from (96 ± 28) mm Hg (1 mm Hg = 0.133 kPa) (49 ± 20) mm Hg (P < 0.01), the transvalvular peak to peak systolic gradient (ΔP) decreased from (89 ± 25) mm Hg to (25 ± 12) mm Hg (P < 0.01), and the right ventricular/aortic systolic pressure ratio decreased from 1.2 ± 0.5 to 0.7 ± 0.3 (P < 0.01). One patient died because of cardiac tamponade following rupture of the pulmonary valve annulus, 2 patients developed pericardial effusion, 3 patients had infundibular spasm, 3 patients had a pre-dilation by small balloon and 1 patient had weakened femoral artery pollex. After a follow up period of 6 months to 4 years 3 of 31 patients lost to follow-up. Repeat valvuloplasty was performed in 5 patients (3 neonates), no patient required surgery, and the other 23 patients did not undergo further intervention, a mean peak systolic Doppler gradient of (20 ± 13) mm Hg was found and no significant pulmonary regurgitation was seen.
CONCLUSIONSPercutaneous balloon pulmonary valvuloplasty was effective and safe for the treatment of critical pulmonary stenosis of neonates and infants under 6 months of age with good short and medium term results.
Catheterization ; Female ; Follow-Up Studies ; Humans ; Infant ; Infant, Newborn ; Lost to Follow-Up ; Male ; Pulmonary Valve ; Pulmonary Valve Stenosis ; therapy ; Treatment Outcome