A novel drug delivery system combining oral fast dissolving film with sodium deoxycholate/phospholipid mixed micelles was prepared to increase the absorption of cucurbitacin B that is a poor aqueous solubility substance. Encapsulation efficiency, particle size, zeta potential, polydispersity coefficient, investigated the morphology, disintegration time of oral fast dissolving film and the pharmacodynamic properties of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles before and after solidified in mice were evaluated and compared. The oral fast dissolving film prepared in this study showed a homogeneous pale yellow and could completely disintegrated in the 30 s. It could meet the requirements of rapidly disintegrating fully. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles loaded in oral fast dissolving film were (43.36 +/- 2.12)%, (108.82 +/- 5.2) nm, (-34.18 +/- 1.07) mV, 0.088 +/- 0.012, respectively. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles in solution were (41.26 +/- 2.22)%, (181.82 +/- 4.48) nm, (-30.67 +/- 0.81) mV, 0.092 +/- 0.012, respectively. The difference of pharmacodynamics among film of cucurbitacin B-loaded micelles, cucurbitacin B-loaded micelles and free cucurbitacin B in vivo was compared. Solubility of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles has also been greatly improved. The tumor inhibition rate of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles was significantly improved and did not change significantly before and after solidified. These showed that the sodium deoxycholate/phospholipid-mixed micelles could enhance the antitumor activities of cucurbitacin B and the stability of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles was improved significantly after solidified by oral fast dissolving film technology without pharmacodynamic properties changed significantly.
Animals ; Antineoplastic Agents ; administration & dosage ; chemistry ; Cell Line, Tumor ; Deoxycholic Acid ; chemistry ; Drug Carriers ; chemistry ; Humans ; Male ; Mice ; Neoplasms ; drug therapy ; Phospholipids ; chemistry ; Solubility ; Triterpenes ; administration & dosage ; chemistry

Adult ; Anti-HIV Agents ; therapeutic use ; Familial Primary Pulmonary Hypertension ; HIV ; pathogenicity ; Hepacivirus ; pathogenicity ; Hepatitis B virus ; pathogenicity ; Humans ; Hypertension, Pulmonary ; drug therapy ; virology ; Male ; Sulfonamides ; therapeutic use

AIMTo establish a method for determinate of the inhibitory activity of angiotensin-converting enzyme inhibitor captopril by high performance capillary electrophoresis.

METHODSThe characteristic absorptive wavelength of hippuric acid determined by ultraviolet spectrophotometer is 228 nm. The method employed a melted capillary column, 50 mmol.L-1 phosphoric acid (pH 8.3) buffer solution, inject pressure 4.8 kPa, inject time 3 s, separation voltage 20 kV and detection wavelength 228 nm.

RESULTSThe reactant and resultant was separated completed within 7 min. IC50 of captopril was 0.019 mumol.L-1. Captopril is a competitive inhibitor, which was proved by enzyme reaction dynamics.

CONCLUSIONThe method was shown to be accurate, simple and rapid and can be used for determination of the inhibitory activity of captopril.

Angiotensin-Converting Enzyme Inhibitors ; pharmacology ; Captopril ; pharmacology ; Electrophoresis, Capillary ; methods ; Hippurates ; analysis ; Peptidyl-Dipeptidase A ; metabolism

OBJECTIVETo observe the efficacy of Sanjie Zhentong Capsule (SJC) in treating ovarian cyst after ovulation-induction.

METHODSFifty-eight patients with ovarian cyst were randomly assigned to two groups, 33 in the treated group treated with SJC and 25 in the control group treated with temporization for 1 month. Changes of estradiol (E2), luteinizing hormone (LH) and follicle stimulating hormone (FSH) level as well as condition of cyst before and after treatment were observed and compared. And the time for complete disappearance (TCD) of cyst and the pregnant rate within 4 months were followed-up.

RESULTSEffective rate (no fluid cyst sized over 1.0 cm could be found in bilateral ovary and E2 <280 pmol/L) in the treated group was 81.8% (27/33) and 52.0% (13/25) in the control group, showing significant difference between them (P <0.05). Level of E2 decreased in both groups, but the lowering was more significant in the treated group, after 1 month, it being 220.54 +/- 96.23 pmol/L vs 372.56 +/- 330.62 pmol/L (P <0.05). The changes of LH and FSH levels were of no statistical significance (P >0.05). TCD in the treated group was 1.18 +/- 0.46 months, which was shorter than that in the control group (1.96 +/- 1.34 months, P <0.05). The pregnant rate within 4 months in the two groups was 60.6% (20/ 33) and 32.0% (8/25) respectively, showing significant difference (P < 0.05).

CONCLUSIONSJC has good efficacy in treating ovarian cyst after ovulation-induction.

Adult ; Capsules ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Follicle Stimulating Hormone ; blood ; Humans ; Luteinizing Hormone ; blood ; Ovarian Cysts ; blood ; drug therapy ; therapy ; Ovulation Induction

This study was aimed to establish the approach of quantitative PCR (q-PCR) for diagnosis of invasive fungal infections (IFI) in patients with hematologic malignancies. Specimens from 40 patients with hematologic malignancies were chosen for q-PCR and galactomannan (GM) test. The 28S rRNA, a real high consensus sequence of fungi, was selected as target gene to design primer and probe. The DNA of fungal species was extracted from serum specimens. The results showed that q-PCR sensitivity, specificity, positive and negative predictive values were 0.89, 0.85, 0.89, 0.85 respectively; GM test sensitivity, specificity, positive and negative predictive values were 0.83, 0.80, 0.88, 0.73 respectively; as combined q-PCR with GM test, these values were 0.94, 0.85, 0.89, 0.92 respectively. It is concluded that the q-PCR assay can be used for early diagnosis for IFI in patients with hematologic malignancies, q-PCR combined with GM test can enhance the diagnosis sensitivity for IFI.
Adolescent ; Adult ; Aged ; Early Diagnosis ; Female ; Fungi ; Hematologic Neoplasms ; microbiology ; Humans ; Male ; Middle Aged ; Mycoses ; diagnosis ; Polymerase Chain Reaction ; methods ; Predictive Value of Tests ; Sensitivity and Specificity ; Young Adult

Objective To investigate the expression and clinical value of immunohistochemistry in endometrial stromal tumors.Methods Immunohistochemical technique(Envision method)was applied to de- tect the expression of CD_(10),SM-MHC,h-caldesmon,AE1/3,CD_(99),Ki-67,CD_(34),c-kit,ER and PR in 15 cases of endomertrial stromal sarcoma and 3 metastases.The clinical pathological data,including the histological characteristics,histochemical and immunohistochemical staining features,complication,differential diagnosis and prognosis of endometrial stromal tumours were analyzed.Results Among the 18 cases of endometrial stromal tumor,17 cases had shown positive for CD_(10),including 13 cases diffuse positive and 4 muitifocal,7 cases with smooth muscle differentiation,3 cases with epithelial differentiation,7 cases with sex-cord differ- entiation.13 cases of ER and 16 cases of PR were positive expression in endometrial stromal sarcoma.Ki-67 in range 36 %～78 %.Conclusion Endometrial stromal tumour can display multi-differentiation.They show various pathomorphological features,Smooth muscle and sex-coed differentiation,the most common types. CD_(10) can be expressed consistently in endometrial stromal tumors.CD_(10) with h-caldesmon and SM-MHC can be used to make differential diagnosis between the endometrial stromal tumors and cellular leiomy0ma.ER and PR should be routinely estimated and be a prognostic predictor for endometrial stromal sarcoma.

Leupaxin (LPXN) is a new member of the Paxillin superfamily, mainly located in focal adhesion plaques, involved in the transduction of multiple signaling pathways, and regulating the proliferation, adhesion and migration of tumor cells. In prostate cancer cells, LPXN is not only involved in the integrin signaling transduction pathway, regulating the proliferation, adhesion and migration of prostate cancer cells, but is also a new androgen receptor (AR) coactivator, regulating the transcription of nuclear AR effect genes, participating in AR signal transduction, and regulating the differentiation and invasion of prostate cancer cells. This review focuses on the molecular structure, special roles and molecular mechanisms of LPXN involved in prostatic carcinoma metastasis.
Cell Adhesion Molecules ; genetics ; metabolism ; Humans ; Male ; Neoplasm Metastasis ; Phosphoproteins ; genetics ; metabolism ; Prostatic Neoplasms ; genetics ; metabolism ; pathology ; Receptors, Androgen ; metabolism ; Signal Transduction

OBJECTIVETo confirm whether human MHC class I chain-related A (MICA) induces the amplification of V delta 1 gamma delta tumor-infiltrating lymphocytes (TILs) in vitro and to identify the cytotoxicity of MICA-reactive V delta 1 gamma delta TILs towards epithelial tumor cells.

METHODSMICA protein was prokaryoticly expressed and purified by molecular cloning technology. The purified recombined MICA (rMICA) was used to induce V delta 1 gamma delta T cells from tumor tissues in vitro and the cytotoxicity of these V delta 1 gamma delta TILs were tested by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT).

RESULTSThe rMICA was expressed in prokaryocyte with pET30 as a vector. The immobilized rMICA protein could markedly induce the amplification of V delta 1 gamma delta T cells from tumor tissue in vitro. These V delta 1 gamma delta T cells showed strong cytolytic activities towards tumor cell lines expressing MICA.

CONCLUSIONThe MICA-reactive V delta 1 gamma delta T cell may be a candidate for adoptive cellular therapy of tumors.

Adult ; Aged ; Female ; HeLa Cells ; pathology ; Histocompatibility Antigens Class I ; biosynthesis ; genetics ; Humans ; Immunotherapy, Adoptive ; Lymphocytes, Tumor-Infiltrating ; immunology ; Male ; Membrane Proteins ; biosynthesis ; genetics ; Middle Aged ; Ovarian Neoplasms ; immunology ; Receptors, Antigen, T-Cell, gamma-delta ; immunology ; Recombinant Proteins ; biosynthesis ; genetics ; T-Lymphocytes, Cytotoxic

Suppressor of cytokine signaling (SOCS) is a new family of proteins produced in cells. It may play an important role in classic negative feedback loop to regulate cytokine signal transduction. SOCS-1 was observed and confirmed firstly. Expression of SOCS-1 can inhibit cytokine signal transduction of some cytokines, such as IL-6, LIF, OSM, INF-gamma, GH, and so on, many immune responses are regulated by them in vivo. Abnormal expression of SOCS-1 is closely related to some human diseases. It plays an important role in the development of leukemia, rheumatoid arthritis, liver cirrhosis and liver cancer. In this review, the advances of research on the relationship between SOCS-1 and cytokine, and its correlation with some diseases were summarized.
DNA Methylation ; Humans ; Interleukin-6 ; biosynthesis ; Intracellular Signaling Peptides and Proteins ; Leukemia ; etiology ; genetics ; Leukemia Inhibitory Factor ; biosynthesis ; Suppressor of Cytokine Signaling 1 Protein ; Suppressor of Cytokine Signaling Proteins ; biosynthesis ; genetics ; physiology