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.Primary carcinoid tumors of the pancreas:CT findings
Can-Hui SUN ; Zi-Ping LI ; Quan-Fei MENG ; Shi-Ting FENG ; Miao FAN ; Zhen-Peng PENG ; Huan-Yi GUO ;
Chinese Journal of Radiology 1999;0(10):-
Objective To evaluate the CT findings of pancreatic carcinoid tumors.Methods The CT imaging data of five patients with pancreatic carcinoid tumors confirmed by pathology were retrospectively analyzed.Results The tumors ranged in maximum diameter from 2.0 to 11.0 cm with a mean of 6.4 cm. On unenhanced CT,the tumors were slightly hypodense relative to the pancreatic parenchyma,homogenous in 2 cases,and heterogenous in 3 cases.One tumor showed calcification.After contrast material injection, the solid component of the tumor showed marked heterogenous enhancement on the arterial phase scanning in 3 cases,and mild heterogenous enhancement in 2 cases.The degree of tumor enhancement was less intense than the surrounding pancreatic parenchyma due to necrosis of various degree,which led to the cystic appearance of the tumor in 1 ease.On the portal phase scanning,all tumors showed marked enhancement similar to that of the pancreatic parenchyma.On the delayed phase scanning,the degree of enhancement was more intense than the surrounding pancreatic parenchyma in 1 case.Liver metastases with retroperitoneal lymphadenopathy and peripancreatic vessels invasion were seen in 1 case.No dilatation of the biliary tract or pancreatic duct was present.Conclusion The CT features of pancreatic carcinoid tumors included infrequent dilatation of the biliary tract or pancreatic duct and unusual vascular involvement,calcification within the mass,marked enhancement similar to that of the surrounding pancreatic parenchyma during the portal phase scanning and more intense during the delayed phase scanning.
3.Protective effect ofα-mangostin on retinal light damage in mice
Yuan, FANG ; Tu, SU ; Ping, XIE ; Song-Tao, YUAN ; Wen, FAN ; Yi-Dan, XU ; Zi-Zhong, HU ; Qing-Huai, LIU
International Eye Science 2015;(7):1143-1147
AlM:To discuss the protective effect ofα-mangostin on retinal light damage in mice.METHODS:Totally 30 Balb/c mice, aged 6~8wk, were randomly divided into the control group, light-exposure group and α-mangostin group. Every group contained 10 mice. Mice of α-mangostin group were treated with alpha-mangostin at the dose of 30mg/( kg · d ) body weight by intragastric administration daily for 7d, and then exposed to white light at the 5th d. The light-exposure group and α-mangostin group were exposed to 5 000 ± 200lx white light-emmiting diodes (LEDs) for continuously 1h to establish the mice model of retinal light damage. Flash -electroretinograme was recorded 72h after light exposure. The changes in retinal morphology of mice were observed by light microscopy. Retinas were extracted to detect the malondialdhyde ( MDA ) content change of the retinal homogenate.RESULTS: Flash-electroretinogram ( F-ERG ) showed that retinal dysfunction was less severe in α-mangostin group than in light-exposure group ( P<0. 05 ). Light microscopy test showed that retina structural damage was less severe in α-mangostin group than in light-exposure group (P<0. 05). The level of MDA in retinal tissue of α-mangostin group was significantly lower when compared with light-exposure group (P<0. 05).CONCLUSlON: α-mangostin inhibits lipid peroxidation induced by light damage and protect retina against light damage.
4.Detection and clinical significance of JAK2 mutation in 412 patients with chronic myeloproliferative neoplasms.
Hong-Ying CHAO ; Zheng FAN ; Ri ZHANG ; Yi-Min SHEN ; Wan CHEN ; Hai-Rong FEI ; Zi-Ling ZHU ; Yu-Feng FENG ; Zi-Xing CHEN ; Yong-Quan XUE
Chinese Journal of Oncology 2009;31(7):510-514
OBJECTIVETo investigate the frequency of JAK2V617F mutation in Chinese patients with chronic myeloproliferative neoplasms (MPN) and to study the relationship between JAK2V617F mutation and clinical characteristics.
METHODSJAK2V617F mutation was screened by allele-specific polymerase chain reaction (AS-PCR).
RESULTSJAK2V617F mutation was detected in 277 of the 412 patients with MPN. The frequency of JAK2V617F mutation was similar among essential thrombocythemia (ET), idiopathic myelofibrosis (IMF) and chronic myeloproliferative disorders-unclassified (MPD-U) (P > 0.05), but it was significantly lower than that in polycythemia vera (PV) (P < 0.05). The presence of JAK2V617F was found to be significantly correlative with advanced age at diagnosis (P < 0.01) and with higher hemoglobin levels and higher leukocyte counts (P < 0.05). Significant difference was found in complication of vascular events between JAK2V617 positive and negative patients (P < 0.05). JAK2V617F positive MPD-U patients were more prone to progress into typical MPN compared with JAK2V617F negative MPD-U patients. The association between abnormal karyotype and JAK2V617F was not found in cytogenetical analysis of 301 patients.
CONCLUSIONThe presence of JAK2V617F in MPD-U is associated with the disease development. There is a correlation between JAK2V617F mutation in MPN and advanced age, higher leukocyte counts, hemoglobin level and vascular events.
Adolescent ; Adult ; Age Factors ; Aged ; Aged, 80 and over ; Female ; Follow-Up Studies ; Hemoglobins ; metabolism ; Humans ; Janus Kinase 2 ; genetics ; Leukocyte Count ; Male ; Middle Aged ; Mutation ; Myeloproliferative Disorders ; blood ; complications ; genetics ; Polycythemia Vera ; blood ; complications ; genetics ; Primary Myelofibrosis ; blood ; complications ; genetics ; Thrombocythemia, Essential ; blood ; complications ; genetics ; Thrombosis ; etiology ; Young Adult
5.Anti-angiogenesis effect of metronomic chemotherapy in multiple myeloma patients.
Lie-ping GUO ; Fan ZHOU ; Wei WEI ; Yi-zi ZHANG ; Hao-tian SHI ; Chen-hui LIN ; Lu LI ; Jian HOU
Chinese Journal of Hematology 2012;33(6):457-460
OBJECTIVETo investigate effects of low-dose cyclophosphamide and prednisone (CP) metronomic chemotherapy on microvessel density of bone marrow, serum vascular endothelial growth factor (VEGF) and platelet derived growth factor BB (PDGF-BB)in multiple myeloma (MM) patients.
METHODS54 refractory or relapsed MM patients were treated with CP metronomic chemotherapy consisted of oral cyclophosphamide (CTX, 50 mg/d) and prednisone (Pred, 15 mg/d). Bone marrow and peripheral blood of each patient were collected before and 2, 4, 6 months after treatment. Among the 37 assessable patients, 30 cases were responsive with the response rate of 81.08%. Another 17 cases were follow-uped less than 6 months or failure to obtain serum samples or lost to follow-up. Microvessel density of bone marrow was measured by immunohistochemistry and serum VEGF/PDGF-BB expression was analyzed by ELISA in the 37 assessable patients.
RESULTS2, 4, 6 months following CP metronomic chemotherapy, microvessel densities of bone marrow in the responders were 33.1 ± 4.8/HP, 24.8 ± 3.7/HP, 19.7 ± 2.1/HP respectively; the expressions of VEGF were (394 ± 57) ng/L, (268 ± 32) ng/L and (217 ± 20) ng/L respectively; the expressions of PDGF-BB were (304 ± 31) ng/L, (274 ± 31) ng/L and (196 ± 22) ng/L respectively. After CP metronomic chemotherapy, there were significantly lower of microvessel density, VEGF and PDGF-BB levels than pretreatment \[MVD 48.5 ± 5.9/HP, VEGF (517 ± 60) ng/L, PDGF-BB (484 ± 60) ng/L\]in the responders (P < 0.01). While in the non-responders, after treated by CP metronomic chemotherapy for 2 months, microvessel density, the expression of VEGF and the expression of PDGF-BB were 32.5 ± 4.7/HP, 512 ± 39 ng/L and (452 ± 39) ng/L respectively. There were no significant changes of MVD, VEGF and PDGF-BB levels compared with pretreatment \[MVD 33.2 ± 5.6/HP,VEGF (498 ± 55) ng/L, PDGF-BB (488 ± 44) ng/L\] (P > 0.05).
CONCLUSIONSOur findings suggested that continuous low-dose CP metronomic chemotherapy could decrease microvessel density of bone marrow in MM patients. Furthermore, it down-regulated expression of serum VEGF and PDGF-BB to exert its anti-angiogenesis in MM.
Aged ; Aged, 80 and over ; Angiogenesis Inhibitors ; administration & dosage ; Antineoplastic Combined Chemotherapy Protocols ; therapeutic use ; Cyclophosphamide ; administration & dosage ; Female ; Humans ; Male ; Microvessels ; drug effects ; Middle Aged ; Multiple Myeloma ; blood ; blood supply ; drug therapy ; Prednisone ; administration & dosage ; Proto-Oncogene Proteins c-sis ; blood ; Vascular Endothelial Growth Factor A ; blood
6.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
7.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
8.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
9.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
10.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