1.Relation between drug release and the drug status within curcumin-loaded microsphere.
De CHEN ; Yi LIU ; Kai-yan FAN ; Yi-qiao XIE ; An-an YU ; Zi-hua XIA ; Fan YANG
Acta Pharmaceutica Sinica 2016;51(1):140-146
To study the relation between drug release and the drug status within curcumin-loaded microsphere, SPG (shirasu porous glass) membrane emulsification was used to prepare the curcumin-PLGA (polylactic-co-glycolic acid) microspheres with three levels of drug loading respectively, and the in vitro release was studied with high-performance liquid chromatography (HPLC). The morphology of microspheres was observed with scanning electron microscopy (SEM), and the drug status was studied with X-ray diffraction (XRD), differential scanning calorimetry (DSC) and infrared analysis (IR). The drug loading of microspheres was (5.85 ± 0.21)%, (11.71 ± 0.39)%, (15.41 ± 0.40)%, respectively. No chemical connection was found between curcumin and PLGA. According to the results of XRD, curcumin dispersed in PLGA as amorphous form within the microspheres of the lowest drug loading, while (2.12 ± 0.64)% and (5.66 ± 0.07)% curcumin crystals was detected in the other two kinds of microspheres, respectively, indicating that the drug status was different within three kinds of microspheres. In the data analysis, we found that PLGA had a limited capacity of dissolving curcumin. When the drug loading exceeded the limit, the excess curcumin would exist in the form of crystals in microspheres independently. Meanwhile, this factor contributes to the difference in drug release behavior of the three groups of microspheres.
Calorimetry, Differential Scanning
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Curcumin
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chemistry
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Drug Liberation
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Lactic Acid
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Microscopy, Electron, Scanning
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Microspheres
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Polyglycolic Acid
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X-Ray Diffraction
2.Platelet phospholipase A2 mRNA content changes and cDNA cloning in rat blood with bacteria infection.
Tao-tao LIU ; Ning-sheng LIANG ; Fan YANG ; Yan LI ; Yi LU ; Zi-qing MENG
Acta Pharmaceutica Sinica 2003;38(5):321-324
AIMTo explore the changes of rat platelet phospholipase A2 (PLA2) mRNA content in bacteria infected rat and study the cDNA and amino acid sequences of the PLA2 structure to lay a good foundation for the development of new antibiotics.
METHODSThe PLA2 mRNA level in blood was determined by RT-PCR. The DNA sequence was cloned and analyzed.
RESULTSAfter injection of bacteria in rats, the mRNA level of PLA2 in blood increased markedly. The cDNA and amino acid sequence were highly homologous to other PLA2 cDNA from different tissues of the rat.
CONCLUSIONPlatelet PLA2 in blood responded quickly to bacteria infection in gene level. Therefore, the PLA2 protein was produced increasingly which was shown to control the infection with bacteria. Although there are little difference between PLA2 cDNA cloned from blood and other sources in DNA and amino acid sequences, the catalytic site for enzymatic activity and basic structure are identical.
Amino Acid Sequence ; Animals ; Base Sequence ; Cloning, Molecular ; DNA, Complementary ; metabolism ; Male ; Molecular Sequence Data ; Phospholipases A ; blood ; genetics ; metabolism ; Phospholipases A2 ; RNA, Messenger ; metabolism ; Rats ; Rats, Wistar ; Staphylococcal Infections ; blood ; Staphylococcus aureus
3.Cruciate ligament reconstruction using LARS artificial ligament under arthroscopy: 81 cases report.
Jian-ming HUANG ; Qian WANG ; Feng SHEN ; Zi-min WANG ; Yi-fan KANG
Chinese Medical Journal 2010;123(2):160-164
BACKGROUNDThere are many different materials used for ligament reconstruction. Currently, autograft, allograft, and artificial ligaments are used in the reconstruction. The objective of this study was to explore the clinical result of cruciate ligament reconstruction under arthroscopy.
METHODSEighty-one cases were reconstructed with the LARS ligament under arthroscopy, including 43 cases of anterior cruciate ligament (ACL) injury, 20 cases of posterior cruciate ligament (PCL) injury, and 18 cases of ACL combined with PCL injuries of the knee. The follow up period was 10 to 49 months. The International Knee Documentation Committee (IKDC) and Lysholm knee score scales were used for functional evaluation. We examined the anterior and posterior stability of the knee with KT-1000.
RESULTSAccording to the Lysholm knee function score scale, the average preoperative score of (44.6+/-1.4) increased to a postoperative score of (82.8+/-2.5) in the ACL group and from (46.6+/-2.3) to (80.8+/-2.0) in the PCL group. In the ACL combined with PCL injury group, the preoperative score increased from (45.2+/-1.2) to (85.5+/-2.3). According to IKDC score standards, in ACL group we evaluated 19 cases as C and 24 cases as D, preoperatively, and postoperatively 27 cases as A, 14 cases as B and two cases as C. In the preoperative PCL group, we had 11 cases defined as C and nine cases as D that resolved to 12 cases as A, seven as B and one case of C in postoperative evaluation. In the ACL combined with PCL injury group we defined four cases as C and 14 as D during preoperative scoring. These patients had postoperative grades of six cases as A, 10 as B, and two cases as C. All of the results have statistical significance.
CONCLUSIONSACL, PCL, or combined ACL and PCL reconstruction using the LARS ligament under arthroscopy is a minimally invasive, safe and effective method to treat cruciate ligament injuries of the knee. Clinical results are satisfactory in the short term.
Adolescent ; Adult ; Anterior Cruciate Ligament ; surgery ; Arthroscopy ; methods ; Female ; Humans ; Male ; Middle Aged ; Posterior Cruciate Ligament ; surgery ; Prostheses and Implants ; Reconstructive Surgical Procedures ; adverse effects ; methods ; Treatment Outcome ; Young Adult
4.Expression of JAK2V617F and MPLW515L/K mutation in 30 suspected cases of early myeloproliferative disorders.
Zheng FAN ; Ri ZHANG ; Yi-Min SHEN ; Hai-Rong FEI ; Zi-Ling ZHU ; Jian-Nong CEN
Chinese Journal of Hematology 2008;29(9):611-614
OBJECTIVETo investigate the prevalence of JAK2V617F and MPLW515L/K mutation in patients with slightly elevated platelets (BPC) or hemoglobin (Hb) not meeting the criteria of polycythemia vera (PV) or essential thrombocythemia (ET).
METHODSGenomic DNA from bone marrow or blood mononuclear cells was screened with allele specific polymerase chain reaction (AS-PCR) for JAK2V617F and MPLW515L/K mutation. The history of thrombosis was assessed retrospectively by patients files.
RESULTSOf 30 patients, 14 (46.7%) were positive for the JAK2V617F mutation, none of them had the MPLW515L/ K. Five of these 14 patients had a history of thrombosis. Follow-up results were available in 22 patients. Among them, 12 patients with JAK2V617F mutation turned out to be MPD in 6-24 months; only 2 out of 10 patients without this mutation evolved to MPD.
CONCLUSIONJAK2V617F mutation could be one of the diagnosis criteria of early MPD. No MPLW515L/K expression was found in early MPD.
Adolescent ; Adult ; Aged ; Aged, 80 and over ; Early Diagnosis ; Female ; Follow-Up Studies ; Humans ; Janus Kinase 2 ; genetics ; metabolism ; Male ; Middle Aged ; Mutation ; Myeloproliferative Disorders ; diagnosis ; genetics ; metabolism ; Receptors, Thrombopoietin ; genetics ; metabolism ; Young Adult
5.Median effective effect-site concentration of intravenous anesthetics for loss of consciousness in neoadjuvant chemotherapy patients.
Zi-jing HE ; Yong-hua HU ; Zhi-yi FAN
Chinese Medical Journal 2011;124(4):504-508
BACKGROUNDIn recent years, increasing numbers of patients are accepting neoadjuvant chemotherapy before their operation in order to get a better prognosis. But chemotherapy has many side-effects. We have observed that patients who accepted neoadjuvant chemotherapy are more sensitive to anesthetics. The aim of this study was to determine the median effective dose (EC(50)) of intravenous anesthetics for neoadjuvant chemotherapy patients to lose consciousness during target-controlled infusion.
METHODSTwo hundred and forty breast cancer patients undergoing elective operations were assigned to six groups according to treatment received before their operation and the use of intravenous anesthetics during anesthesia; non-adjuvant chemotherapy + propofol group (group NP, n = 40), Taxol + propofol group (group TP, n = 40), adriamycin + cyclophosphamide + 5-Fu + propofol group (group CP, n = 40), non-adjuvant chemotherapy + etomidate group (group NE, n = 40), taxol + etomidate group (group TE, n = 40), adriamycin + cyclophosphamide + 5-Fu + etomidate group (group CE, n = 40). We set the beginning effect-site concentration (Ce) of propofol as 3.0 µg/ml and etomidate as 0.2 µg/ml. The concentration was increased by steps until the patient was asleep, (OAAS class I-II), then gave fentanyl 3 µg/kg and rocuronium 0.6 mg/kg and intubated three minutes later. The patients' age, height, and weight were recorded. BIS was recorded before induction, at the initial effect-site concentration and at loss of consciousness. The effect-site concentration was recorded when patient lost consciousness.
RESULTSThere were no significant differences between groups in general conditions before treatment; such as BIS of consciousness, age, sex and body mass index. The EC(50) of propofol in the NP, TP and CP groups was 4.11 µg/ml (95%CI: 3.96 - 4.26), 2.94 µg/ml (95%CI: 3.36 - 3.47) and 2.91 µg/ml (95%CI: 3.35 - 3.86), respectively. The EC50 of etomidate in the NE, TE and CE groups was 0.61 µg/ml (95%CI: 0.55 - 0.67), 0.38 µg/ml (95%CI: 0.33 - 0.44), and 0.35 µg/ml (95%CI: 0.34 - 0.36), respectively. There was no significant difference of BIS level before induction or in BIS50 level in any group when patients lost consciousness.
CONCLUSIONSThe EC(50) of intravenous anesthetics to cause loss of consciousness in neoadjuvant chemotherapy groups is lower than in the control group. There was no significant difference of BIS level at which patients lost consciousness.
Adult ; Anesthetics, Intravenous ; therapeutic use ; Breast Neoplasms ; drug therapy ; surgery ; Cyclophosphamide ; therapeutic use ; Doxorubicin ; therapeutic use ; Etomidate ; therapeutic use ; Female ; Fluorouracil ; therapeutic use ; Humans ; Middle Aged ; Neoadjuvant Therapy ; adverse effects ; Paclitaxel ; therapeutic use ; Propofol ; therapeutic use ; Unconsciousness ; chemically induced
6.Influence of sea water immersion on inflammation and healing of the wounds in scalded rats.
Zi-feng FAN ; Jia-han WANG ; Zhi-qing LI ; Chao-hui YI
Chinese Journal of Burns 2006;22(3):215-217
OBJECTIVETo investigate the influence of sea water immersion on inflammation and healing of the wounds in scalded rats.
METHODSOne hundred and forty-four male Wistar rats with 10% TBSA superficial partial-thickness scald were randomly divided into A (n=72, with scald) and B (n=72, with seawater immersion for 4hrs immediately after scald) groups. The serum contents of K+, Na+, Cl- were determined at 0 post-scald hour (PSH), 6PSH, 12PSH and 24 PSH with electrocyte analysis apparatus, and the changes in serum interleukin-6 (IL-6) and tumor necrosis factor (TNF-alpha) levels were determined at 0 PSH, 6PSH and 12 PSH with enzyme-linked immunosorbent assay (ELISA). The histopathological changes in the rats of the two groups were observed, and wound healing time was respectively calculated.
RESULTSThe serum contents of K+, Na+, Cl- in B group were obviously higher than those in A group. And the serum content of TNF-alpha and IL-6 in B group at 6 PSH [(140 +/- 22) ng/L, (160 +/- 41) ng/L] were significantly higher than those before scald [(29 +/- 15) ng/L, (62 +/- 17)] ng/L and in A group [(120 +/- 12) ng/L, (124 +/- 22) ng/L, ( P < 0.05)]. Compared with A group, re-epithelization of the wound differentiation in all layers of epidermis were delayed in B group, with more severe wound swelling, exudation, and topical inflammatory response. The wound healing time in B group was (16.3 +/- 1.6) d, which was obviously longer than that in A group [(14.1 +/- 1.8) d, P < 0.05)].
CONCLUSIONSea water immersion combined with scald injury can aggravate the inflammatory response of the wound and delay the wound healing process.
Animals ; Burns ; pathology ; Disease Models, Animal ; Inflammation ; Interleukin-6 ; analysis ; Male ; Rats ; Rats, Wistar ; Seawater ; adverse effects ; Tumor Necrosis Factor-alpha ; analysis ; Wound Healing
7.Effect of diallyl disulfide on expression and secretion of VEGF in HL-60 leukemic cells.
Yi XIE ; Zi-Li FAN ; Chen-Jiao YAO ; San-Qin TAN ; Ya-Li ZHAO
Journal of Experimental Hematology 2006;14(2):212-216
The study was aimed to investigate the expression of VEGF mRNA and VEGF protein in HL-60 cells treated with diallyl disulfide (DADS), and to explore the antileukemic mechanism of DADS in respect of VEGF production. Semi-quantitative RT-PCR and ELISA were used to detect the expression of VEGF mRNA and secretion of VEGF protein in HL-60 cell lines treated by DADS respectively. The results showed that the expression of VEGF mRNA and secretion of VEGF protein were found in HL-60 cells. The expression of VEGF mRNA and secretion of VEGF protein in HL-60 cells could be down regulated by treatment with 0.625, 1.25, and 2.5 microg/mL DADS for 48 and 72 hours and the effects had a dose dependent relationship (r > 0.9, P < 0.01). The differences between DADS treated HL-60 cell groups and the control group were statistically significant (P < 0.01), there were also statistically significant differences among three DADS-treated HL-60 cell groups (P < 0.05). It is concluded that DADS effectively inhibits the proliferation of human leukemia cell line HL-60 cells; DADS exerts its antileukemic effects by reduction of the expression of VEGF mRNA and VEGF protein secretion.
Allyl Compounds
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pharmacology
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Antineoplastic Agents
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pharmacology
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Cell Proliferation
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drug effects
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Disulfides
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pharmacology
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HL-60 Cells
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Humans
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RNA, Messenger
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biosynthesis
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genetics
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Vascular Endothelial Growth Factor A
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biosynthesis
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genetics
8.Effect of carnosine on prevention of reperfusion liver injury during hemorrhagic shock and reperfusion in rats.
Feng-Yan FAN ; Ling-Zhi HUANG ; Guang-Yi WANG ; Wei ZHENG ; Bo WANG ; Hong ZHOU ; Zi-Ling WANG
Chinese Journal of Hepatology 2006;14(12):942-943
Animals
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Carnosine
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pharmacology
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therapeutic use
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Liver
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drug effects
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pathology
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Male
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Rats
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Rats, Wistar
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Reperfusion Injury
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prevention & control
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Shock, Hemorrhagic
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complications
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pathology
9.MicroRNAs expression in normal and dissected aortic tissue.
Zi-yang HU ; Jian-fang LUO ; Shi-long ZHONG ; Ling XUE ; Yi-fei CHEN ; Rui-xin FAN
Chinese Journal of Cardiology 2012;40(5):406-410
OBJECTIVESTo investigate if there is altered microRNAs (miRNAs) expression in aortic dissection (Debakey Type A) and normal aorta tissue.
METHODSTotal RNA was exacted from aorta of 5 patients with aortic dissection (AD) and four patients without aortic diseases (NA). miRNAs of the aortic tissues were analyzed by miRNA microarray. Reverse transcription polymerase chain reaction (RT-PCR) was performed to verify the expression of miRNAs in larger sample size (AD = 11 and NA = 9).
RESULTShsa-miR-146b-5p_st, hsa-miR-19a_st and hsa-miR-505_st were significantly upregulated while hsa-miR-1268_st and hsa-miR-939_st were significantly downregulated [fold change > 2, q-value (%) ≤ 5] in AD group compared with NA group. RT-PCR verified hsa-miR-146b-5p_st miRNAs change in AD group.
CONCLUSIONSAltered miRNAs expression might play an essential role in the pathogenesis of aortic dissection formation and hsa-miR-146b-5p_st might serve as a new diagnosis biomarker of aortic dissection.
Aneurysm, Dissecting ; genetics ; Gene Expression Profiling ; Humans ; MicroRNAs ; genetics ; metabolism ; Oligonucleotide Array Sequence Analysis ; Reverse Transcriptase Polymerase Chain Reaction
10.Effect of diallyl disulfide on the expression and secretion of VEGF in HL-60 cells.
Zi-Li FAN ; Zhen-Hua QI ; Yi XIE
Chinese Journal of Hematology 2006;27(9):626-629
OBJECTIVETo investigate the proliferation inhibition of human leukemic cell line HL-60 and the expression of vascular endothelial growth factor (VEGF) mRNA and secretion of VEGF protein in HL-60 cells treated with diallyl disulfide (DADS).
METHODSMTT was used to test the cell growth, semi-quantitative RT-PCR and ELISA to study the expression of VEGF mRNA and secretion of VEGF protein.
RESULTSDADS significantly inhibited proliferation of HL-60 cell and the inhibiting effects showed a dose (r > 0.9, P < 0.01) and time-dependent( r > 0.7, P < 0.01) manner. The expression of VEGF mRNA and secretion of VEGF protein could be down regulated by 0.625, 1.250, and 2.500 microg/mL DADS in HL-60 cells for 24,48 and 72 hours exposure and the effects also showed dose -dependence(r > 0.9, P < 0.01). The growth inhibition rates of DADS in HL-60 cells at three dosages for 24 hours were (8.19 +/- 3.34)%, (16.79 +/- 2.07)% and (21.30 +/- 2.72)%, those for 48 hours were (11.93 +/- 3.93)%, (22.81 +/- 2.31)% and (30.74 +/- 2.03)%, for 72 hours were (16.68 +/- 2.37)%, (28.54 +/- 3.26)% and (36.59 +/- 2.37)% respectively, The difference between the DADS-treated and untreated HL-60 cells was statistically significant (P < 0.01). There were also statistically significant differences among the three groups of different dosages (P < 0.01).
CONCLUSIONDADS can effectively inhibit the proliferation of HL-60 cells. DADS probably exerts its anti-leukemia effects by reducing the expression of VEGF mRNA and secretion of VEGF protein in HL-60 cells.
Allyl Compounds ; pharmacology ; Antineoplastic Agents ; pharmacology ; Disulfides ; pharmacology ; Dose-Response Relationship, Drug ; HL-60 Cells ; Humans ; RNA, Messenger ; biosynthesis ; Reverse Transcriptase Polymerase Chain Reaction ; Vascular Endothelial Growth Factor A ; biosynthesis ; drug effects ; secretion